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Sample records for considerations inhibitory effects

  1. Inhibitory Effect of Furosemide on Carbonic Anhydrase

    Institute of Scientific and Technical Information of China (English)

    CUI Jianli; ZHAO Tongjin; JIANG Yan; ZHOU Haimeng

    2006-01-01

    This study investigated the inhibitory effect of a high efficiency diuretic, furosemide, on carbonic anhydrase (CA). First, comparing the inhibitory effect of acetazolamide, a low efficiency diuretic, on CA, shows that furosemide or acetazolamide can quickly make CA inactive when its concentration is close to the enzyme concentration, different from the usual inhibitory kinetics in which the concentration of the inhibitor is far higher than the enzyme concentration. Secondly, the reaction of the enzyme indicates that the inhibitory effect of furosemide or acetazolamide on carbonic anhydrase is quickly reversible. Finally, the degree of the inhibitory effect of furosemide and of acetazolamide on CA are compared. The results show that furosemide inhibits CA less than acetazolamide.

  2. Inhibitory effects of antimicrobial agents against Fusarium species.

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    Kawakami, Hideaki; Inuzuka, Hiroko; Hori, Nobuhide; Takahashi, Nobumichi; Ishida, Kyoko; Mochizuki, Kiyofumi; Ohkusu, Kiyofumi; Muraosa, Yasunori; Watanabe, Akira; Kamei, Katsuhiko

    2015-08-01

    We investigated the inhibitory effects of antibacterial, biocidal, and antifungal agents against Fusarium spp. Seven Fusarium spp: four F. falciforme (Fusarium solani species complex), one Fusarium spp, one Fusarium spp. (Fusarium incarnatum-equiseti species complex), and one F. napiforme (Gibberella fujikuroi species complex), isolated from eyes with fungal keratitis were used in this study. Their susceptibility to antibacterial agents: flomoxef, imipenem, gatifloxacin, levofloxacin, moxifloxacin, gentamicin, tobramycin, and Tobracin® (contained 3,000 μg/ml of tobramycin and 25 μg/ml of benzalkonium chloride (BAK), a biocidal agent: BAK, and antifungal agents: amphotericin B, pimaricin (natamycin), fluconazole, itraconazole, miconazole, voriconazole, and micafungin, was determined by broth microdilution tests. The half-maximal inhibitory concentration (IC50), 100% inhibitory concentration (IC100), and minimum inhibitory concentration (MIC) against the Fusarium isolates were determined. BAK had the highest activity against the Fusarium spp. except for the antifungal agents. Three fluoroquinolones and two aminoglycosides had inhibitory effects against the Fusarium spp. at relatively high concentrations. Tobracin® had a higher inhibitory effect against Fusarium spp. than tobramycin alone. Amphotericin B had the highest inhibitory effect against the Fusarium spp, although it had different degrees of activity against each isolate. Our findings showed that fluoroquinolones, aminoglycosides, and BAK had some degree of inhibitory effect against the seven Fusarium isolates, although these agents had considerably lower effect than amphotericin B. However, the inhibitory effects of amphotericin B against the Fusarium spp. varied for the different isolates. Further studies for more effective medications against Fusarium, such as different combinations of antibacterial, biocidal, and antifungal agents are needed. © The Author 2015. Published by Oxford University Press on

  3. Inhibitory effect of cyanide on wastewater nitrification ...

    Science.gov (United States)

    The effect of CN- (CN-) on nitrification was examined with samples from nitrifying wastewater enrichments using two different approaches: by measuring substrate (ammonia) specific oxygen uptake rates (SOUR), and by using RT-qPCR to quantify the transcripts of functional genes involved in nitrification. The nitrifying bioreactor was operated as a continuous reactor with a 24 h hydraulic retention time. The samples were exposed in batch vessels to cyanide for a period of 12 h. The concentrations of CN- used in the batch assays were 0.03, 0.06, 0.1 and 1.0 mg/L. There was considerable decrease in SOUR with increasing dosages of CN-. A decrease of more than 50% in nitrification activity was observed at 0.1 mg/L CN-. Based on the RT-qPCR data, there was notable reduction in the transcript levels of amoA and hao for increasing CN- dosage, which corresponded well with the ammonia oxidation activity measured via SOUR. The inhibitory effect of cyanide may be attributed to the affinity of cyanide to bind ferric heme proteins, which disrupt protein structure and function. The correspondence between the relative expression of functional genes and SOUR shown in this study demonstrates the efficacy of RNA based function-specific assays for better understanding of the effect of toxic compounds on nitrification activity in wastewater. Nitrification is the first step of nitrogen removal is wastewater, and it is susceptible to inhibition by many industrial chemical. We looked at

  4. Pancreatic Lipase Inhibitory Effects of Mangosteen Pericarps

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    Xinjie Lin

    2014-03-01

    Full Text Available Pancreatic lipase plays a key role in the digestion and absorption of lipids, inhibition of Pancreatic Lipase (PL is considered as a new approach to obesity treatment. The objective of the present study was to find PL inhibitors from natural food sources. Eighteen natural food products sampled from local supermarkets in Zhuhai were tested for PL inhibitory activity using a copper-soap photometric method. Among the samples tested, the crude extracts from mangosteen pericarp, lemon pulp, celery, cucumber and dry longan were found to be able to suppress the PL activity to different extents, while dry red chili, fresh green chili and dry clove exhibited a promotion effect on the PL. Shiitake mushroom, green bell pepper, lemon peel and spices (ginger, oregano leaf, bay leaf, cinnamon and dry tangerine showed no significant influence either on the inhibition or promotion. The crude extract of mangosteen pericarp was further fractioned to trace active fractions. It was found that the n-butanol fraction was the major contributor to the PL-inhibitory effect of mangosteen pericarp and the inhibition rate was 43.9% at the concentration of 1 mg/mL, the IC50 value was 0.918 mg/mL. Mangosteen pericarp is worthy of utilization as functional food constituents for the prevention and treatment of obesity.

  5. Inhibitory effect and mechanism of chuanxiongzine on multiplication of VSMC

    Institute of Scientific and Technical Information of China (English)

    Qingxian Li; Yuhua Liao; Huiling Zhang; Yanying Jiang; Yanfu Wang

    2007-01-01

    Objective: To study the inhibitory effect of chuanxiongzine on vascular smooth muscle cell (VSMC) proliferation and explore its molecular biology basis. Methods: we selected the VSMC cultured 4~8 generation from rat aorta thoracalis as research object.The objects were divided into four groups( Ⅰ )control group, ( Ⅱ )chuanxiongzine(50 μg/ml)group, ( Ⅲ )chuanxiongzine (100 μg/ml) group and( Ⅳ ) chuanxiongzine (200 μg/ml) group. The inhib itory effect of chuanxiongzine on VSMC proliferation was investigated by cell counting, MTT and 3H-TdR incorporation assay. In order to illuminate the molecular biology mechanism of chuanxiongzine inhibiting VSMCs proliferation, the expression of proliferating cell nuclear antigen (PCNA) and C-myc were detected.Results: Chuanxiongzine could inhibit the proliferation of VSMC significantly in a dose- and time-dependent manner, compared with control group (P < 0.05). The expression of PCNA and c-myc were inhibited obviously and correlated with the concentration of chuanxiongzine (P < 0.05). Conclusion: Chuanxiongzine may play a considerable role in VSMC proliferation process. The inhibitory effect of chuanxiongzine in a dose- and time-dependent manner can be realized via down regulating the expression of PCNA and c-myc. In this study, The great theoretical fundament about Chinese medicine, which is used to treat atherosclerosis (AS), has been obtained.

  6. Further considerations of spallation effects

    Science.gov (United States)

    Dyer, C.

    1973-01-01

    Trapped photon and cosmic ray effects on spallation in the UK-5 (hard X ray telescope) central crystal were measured. Both low dose and high dose effects were considered. Decay results are presented in tables.

  7. Inhibitory effect of burdock leaves on elastase and tyrosinase activity

    Science.gov (United States)

    Horng, Chi-Ting; Wu, Hsing-Chen; Chiang, Ni-Na; Lee, Chiu-Fang; Huang, Yu-Syuan; Wang, Hui-Yun; Yang, Jai-Sing; Chen, Fu-An

    2017-01-01

    Burdock (Arctium lappa L.) leaves generate a considerable amount of waste following burdock root harvest in Taiwan. To increase the use of burdock leaves, the present study investigated the optimal methods for producing burdock leaf extract (BLE) with high antioxidant polyphenolic content, including drying methods and solvent extraction concentration. In addition, the elastase and tyrosinase inhibitory activity of BLE was examined. Burdock leaves were dried by four methods: Shadow drying, oven drying, sun drying and freeze-drying. The extract solution was then subjected to total polyphenol content analysis and the method that produced BLE with the highest amount of total antioxidant components was taken forward for further analysis. The 1,1-diphenyl-2-pycrylhydrazyl scavenging, antielastase and antityrosinase activity of the BLE were measured to enable the evaluation of the antioxidant and skin aging-associated enzyme inhibitory activities of BLE. The results indicated that the total polyphenolic content following extraction with ethanol (EtOH) was highest using the freeze-drying method, followed by the oven drying, shadow drying and sun drying methods. BLE yielded a higher polyphenol content and stronger antioxidant activity as the ratio of the aqueous content of the extraction solvent used increased. BLE possesses marked tyrosinase and elastase inhibitory activities, with its antielastase activity notably stronger compared with its antityrosinase activity. These results indicate that the concentration of the extraction solvent was associated with the antioxidant and skin aging-associated enzyme inhibitory activity of BLE. The reactive oxygen species scavenging theory of skin aging may explain the tyrosinase and elastase inhibitory activity of BLE. In conclusion, the optimal method for obtaining BLE with a high antioxidant polyphenolic content was freeze-drying followed by 30–50% EtOH extraction. In addition, the antielastase and antityrosinase activities of the

  8. COX-1 inhibitory effect of medicinal plants of Ghana

    DEFF Research Database (Denmark)

    Larsen, Birgitte HV; Soelberg, Jens; Jäger, Anna

    2015-01-01

    Plants used to treat inflammatory ailments, pain, fever and infections in Ghana, were tested for COX-1 inhibitory activity. Ethanolic extracts of 17 species were tested in a COX-1 assay. The extracts of Gardenia ternifolia, Thonningia sanguinea, Triumfetta rhomboidea, and the root of Zanthoxylum...... zanthoxyloides showed an inhibitory effect over 90% in the final concentration 0.1 μg/μL. The HPLC profiles indicated that the extracts of the four active species did not contain tannins. The observed in vitro activities support the use of some of the plant species in the traditional medicine system in Ghana....

  9. Synthesis and urease enzyme inhibitory effects of some dicoumarols.

    Science.gov (United States)

    Khan, Khalid M; Iqbal, Sajid; Lodhi, Muhammad A; Maharvi, Ghulam M; Perveen, Shahnaz; Choudhary, M I; Atta-Ur-Rahman; Chohan, Zahid H; Supuran, Claudiu T

    2004-08-01

    Dicoumarols 1-10 with substituted phenyl residues at C-11 were synthesized and screened for their urease inhibition effects. All synthesized compounds showed varying degree of urease inhibitory activity ranging from IC50 = 74.30-91.35 microM.

  10. Inhibitory effects of acetylsalicylic acid on exocrine pancreatic carcinogenesis.

    Science.gov (United States)

    Yıldız, H; Oztas, H; Yıldız, D; Koc, A; Kalipci, E

    2013-05-01

    We investigated short (6 months) and long (12 months) term inhibitory effects of low (200 ppm) and high (400 ppm) dosages of acetylsalicylic acid (aspirin) on exocrine pancreatic carcinogenesis. It is known that exocrine pancreatic carcinogenesis can be detected by the presence of atypical acinar cell foci (AACF) in pancreas. We investigated possible inhibitory effects of acetylsalicylic acid in an azaserine-treated rat model. AACF were produced in rats by injection with azaserine according to previous studies. Our findings showed that the number, volume and diameter of pancreatic AACF were reduced after acetylsalicylic acid application. These observations suggest that acetylsalicylic acid may exert a protective effect against neoplastic development of pancreatic acinar cells in azaserine injected rats. Our findings corroborate reports in the literature concerning the effects of aspirin in reducing neoplastic development.

  11. Inhibitory Effects of 5,6,7-Trihydroxyflavones on Tyrosinase

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    Jun Kawabata

    2007-01-01

    Full Text Available Baicalein (1, 6-hydroxyapigenin (6, 6-hydroxygalangin (13 and 6-hydroxy-kaempferol (14, which are naturally occurring flavonoids from a set of 14 hydroxy-flavones tested, exhibited high inhibitory effects on tyrosinase with respect to L-DOPA,while each of the 5,6,7-trihydroxyflavones 1, 6, 13 or 14 acted as a cofactor tomonophenolase. Moreover, 6-hydroxykaempferol (14 showed the highest activity andwas a competitive inhibitor of tyrosinase compared to L-DOPA. 5,6,7-Trihydroxyflavones 1, 6, 13 or 14 showed also high antioxidant activities. Hence, weconclude that the 5,6,7-trihydroxy-flavones are useful as good depigmentation agentswith inhibitory effects in addition to their antioxidant properties.

  12. Inhibitory effect of piperidinoethylesters of alkoxyphenylcarbamic acids on photosynthesis.

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    Král'ová, K; Sersen, E; Cizmárik, J

    1992-06-01

    Piperidinoethylesters of 2-, 3- and 4-alkoxysubstituted phenylcarbamic acids (alkoxy = methoxy - decyloxy) inhibit photosynthetic processes in algae and plant chloroplasts. The inhibitory activity is strongly dependent on the alkyl chain length of the alkoxy-substituent showing a typical quasi-parabolic dependence with maximum effect at 6-8 carbon atoms in the alkyl chain. The alkoxy-substitution in position 2 decreases the inhibitory activity of a compound when compared with its 3- and 4-substituted analogues. ESR studies of spinach chloroplasts confirm that the compounds studied cause destruction of PS II whereby, in the presence of the most effective of the derivatives tested, Mn2+ ions are released from the protein complex.

  13. Probing inhibitory effects of nanocrystalline cellulose: inhibition versus surface charge

    Science.gov (United States)

    Male, Keith B.; Leung, Alfred C. W.; Montes, Johnny; Kamen, Amine; Luong, John H. T.

    2012-02-01

    NCC derived from different biomass sources was probed for its plausible cytotoxicity by electric cell-substrate impedance sensing (ECIS). Two different cell lines, Spodoptera frugiperda Sf9 insect cells and Chinese hamster lung fibroblast V79, were exposed to NCC and their spreading and viability were monitored and quantified by ECIS. Based on the 50%-inhibition concentration (ECIS50), none of the NCC produced was judged to have any significant cytotoxicity on these two cell lines. However, NCC derived from flax exhibited the most pronounced inhibition on Sf9 compared to hemp and cellulose powder. NCCs from flax and hemp pre-treated with pectate lyase were also less inhibitory than NCCs prepared from untreated flax and hemp. Results also suggested a correlation between the inhibitory effect and the carboxylic acid contents on the NCC.

  14. Effect of craving induction on inhibitory control in opiate dependence.

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    Verdejo-García, Antonio; Lubman, Dan I; Schwerk, Anne; Roffel, Kim; Vilar-López, Raquel; Mackenzie, Trudi; Yücel, Murat

    2012-01-01

    Current neurobiological models of addiction posit that drug seeking is much more likely to occur during emotionally charged states (such as craving), as deficits in inhibitory control become more pronounced during heightened motivational states. The purpose of this study was to examine the effect of cue-induced craving states on attention and inhibitory control within addicted individuals. We tested the performance of 39 opiate-dependent individuals on cognitive measures of attention (Digit Span, Digit Symbol, and Telephone Search) and inhibitory control (Counting Stroop and Go-No-Go) both before and after exposure to an autobiographical craving script. A non-drug using healthy control group (n = 19) performed the same tasks before and after listening to a relaxation tape. Following craving induction, opiate-dependent individuals demonstrated improved performance on tests of processing speed and attentional span (consistent with the practice effect observed in controls) and increased their response errors on the Stroop task (in contrast to controls), while selective attention was unaffected. Individual differences in compulsivity mediated the association between craving and Stroop performance, such that low-compulsive (but not high-compulsive) individuals committed more response errors after craving induction. These findings challenge the notion of cue-induced craving as a primary trigger of disrupted cognition and drug-seeking behavior in addicted individuals, and raise the need to explore individual differences in compulsivity when addressing the links between craving and loss of control within research and clinical settings.

  15. Inhibitory effect of ginsenoside Rg3 on ovarian cancer metastasis

    Institute of Scientific and Technical Information of China (English)

    XU Tian-min; CUI Man-hua; XIN Ying; GU Li-ping; JIANG Xin; SU Man-man; WANG Ding-ding; WANG Wen-jia

    2008-01-01

    Background Ginsenosides are main components extracted from ginseng, and ginsenoside Rg3 is one of the most important parts. Ginsenoside Rg3 has been found to inhibit several kinds of tumor growth and metastasis. The present study was undertaken to investigate the effect of ginsenoside Rg3 on human ovarian cancer metastasis and the possible mechanism.Methods The experimental lung metastasis models of ovarian cancer SKOV-3 and the assay of tumor-induced angiogenesis were used to observe the inhibitory effects of Rg3 on tumor metastasis and angiogenesis. The effect of Rg3 on invasive ability of SKOV-3 cells in vitro was detected by Boyden chamber, and immunofluorescence staining was used to recognize the expression of matrix metalloproteinase 9 (MMP-9) in SKOV-3 cells.Results In the experimental lung metastasis models of ovarian cancer, the number of tumor colonies in the lung and vessels oriented toward the tumor mass in each ginsenoside Rg3 group, was lower than that of control group. The invasive ability and MMP-9 expression of SKOV-3 cells decreased significantly after treatment with ginsenoside Rg3.Conclusions Ginsenoside Rg3 can significantly inhibit the metastasis of ovarian cancer. The inhibitory effect is partially due to inhibition of tumor-induced angiogenesis and decrease of invasive ability and MMP-9 expression of SKOV-3 cells.

  16. Inhibitory effects of monoterpenes on seed germination and seedling growth.

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    Kordali, Saban; Cakir, Ahmet; Sutay, Sunay

    2007-01-01

    Monoterpenes, the chemical constituents of essential oils found in plants, are known biologically active compounds. The present study was conducted to investigate the inhibitory effects of 30 monoterpenes including monoterpene hydrocarbons and oxygenated monoterpenes on seed germination and seedling growth of Amaranthus retroflexus, Chenopodium album and Rumex crispus under laboratory conditions. The monoterpenes were applied at contents of 10 and 20 microl for liquid compounds and 10 and 20 microg for solid compounds. The results show that most of the monoterpenes significantly inhibited seed germination and seedling growth of the tested plants. Oxygenated monoterpenes including beta-citronellol, nerol and terpinen-4-ol completely inhibited seed germination and seedling growth of all tested plants. Their inhibitory effects were also stronger than that of the herbicide 2,4-D. In general, monoterpenes were less effective against seed germination and seedling growth of C. album as compared with R. crispus and A. retroflexus. Phytotoxic effects of monoterpene hydrocarbons were found to be lower than those of oxygenated monoterpenes. The alcohol derivatives of oxygenated monoterpenes were also found to be more phytotoxic as compared with their acetate derivatives. Based on the present results, it can be concluded that the oxygenated monoterpenes can be used as potential bio-herbicides.

  17. Antioxidative properties and inhibitory effect of Bifidobacterium adolescentis on melanogenesis.

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    Huang, Huey-Chun; Chang, Tsong-Min

    2012-09-01

    Melanin is a dark pigment produced by melanocytes. Tyrosinase is a key enzyme which catalyzes the rate-limiting step of melanogenesis. However, accumulation of melanin leads to various skin hyperpigmentation disorders. To find a novel skin-whitening agent, the antioxidant capacity of Bifidobacterium adolescentis culture filtrate and inhibitory effect on melanogenesis were investigated. The antioxidant effects of B. adolescentis culture filtrate include 2,2-diphenyl-1-picryl-hydrazyl (DPPH) radical scavenging capacity, 2,2'-azino-bis (3-ethylbenzthiazoline-6-sulphonic acid)(ABTS) radical cation scavenging activity and reducing power were measured spectrophotometrically. The reducing power is a useful index for the evaluation of potential antioxidants which carry out reduction of ferricyanide to ferrocyanide. Furthermore, the inhibitory effects of the bacterial culture filtrate on mushroom tyrosinase, B16F10 intracellular tyrosinase activity and melanin content were also determined. The results revealed that B. adolescentis culture filtrate (2.5, 5.0 and 7.5 %; v/v) effectively scavenged DPPH and ABTS radicals, and lower concentrations of the bacterial culture filtrates (0.5, 1.0 and 1.5 %; v/v) showed potent reducing power in a dose-dependent pattern. Additionally, the bacterial culture filtrate suppressed murine tyrosinase activity and decreased the amount of melanin in a dose-dependent manner. Our results demonstrated that B. adolescentis culture filtrate decreases the melanogenesis process of melanoma cells by inhibiting tyrosinase activity, which we suggest may be mediated through its antioxidant activity.

  18. Proteome Analysis of Inhibitory Effect of Gadolinium on Sinorhizobium fredii

    Institute of Scientific and Technical Information of China (English)

    2007-01-01

    The inhibitory effect of gadolinium on Sinorhizobium fredii USDA 205 was studied on a global scale using two-dimensional gel electrophoresis and MALDI-TOF MS. The results indicated that 22 proteins were significantly affected by 1 mmol·L-1 Gd3+ treatment when compared with an untreated control. Among these proteins, nine were up-regulated and thirteen were down-regulated. The differently expressed proteins were classified into 8 functional categories based on their functions, including transporters, proteins for cellular defence, and proteins involved in metabolism.

  19. Inhibitory effect of calcitonin on pure human pancreatic secretion.

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    Tanaka,Juntaro

    1989-06-01

    Full Text Available The inhibitory effect of calcitonin on human pancreatic secretion was evaluated to examine whether the different results reported earlier between humans, cats and dogs can be ascribed to the different sensitivity of these species to calcitonin, as suggested by some investigators. Pancreatic juice was obtained by endoscopic cannulation of the pancreatic duct from 11 patients with relapsing pancreatitis during intravenous infusion of secretin (1 U/kg/h plus caerulein (0.04 microgram/kg/h. After steady secretion was attained 20 min after the beginning of collection, five 2-min fractions were obtained before, and ten 2-min fractions were obtained after intravenous infusion of calcitonin (1 IU/kg/h. The pre- and post-calcitonin fractions from each patient were compared by Student's t-test. Calcitonin inhibited the secretory volume (26.8 to 65.6% and bicarbonate secretion (21.4 to 62.0% in 8 patients, and amylase (48.4 to 89.5% and lipase secretion (47.4 to 90.5% in all patients. The present studies reconfirmed that prominent inhibition of enzyme secretion occurs in humans. A new finding was that significant inhibition of the secretory volume and bicarbonate secretion occurs in humans. The inhibitory effects of calcitonin in humans did not appear to differ from those in cats and dogs, when evaluated similarly with the use of pure pancreatic juice.

  20. Effect of Inhibitory Substances on Microbiospora Isolated from Soil under Cultivation of Curcuma Longa L.

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    A. P. Kamble

    2012-01-01

    Full Text Available Problem statement: Soil Pollution is major problem because different types of pesticides are used to control plant pest. The residual component of pesticide diffuses into the soil. It is necessary to check whether actinomycetes degrade these components and control the soil pollution. Approach: In Ayurved system of medicine the rhizome portion of Curcuma longa L. was used as an anti-inflammatory and antiseptic. Antimicrobial substances released from these plants diffuse into the surrounding soil area of the plant. Actinomycete which grow in these area were resistant to these substances. Hence considerable attention had been given in studying the effect of inhibitory substances on actinomycetes especially Microbiospora isolated from soil under cultivation of Curcuma longa L. Results: The present study deals with effect of inhibitory substances like dettol, phenol, sodium azide, lysol and crystal violet. The results were recorded on the basis of presence or absence of growth. All five isolates of Microbiospora were found sensitive against dettol. One strain of Microbiospora was found resistant to phenol. Conclusion/Recommendations: From the study performed we conclude that Microbiospora which is resistant to phenol and other inhibitory substances can be used to degrade the residual components of pesticide which are released into the soil. It may have better option to prevent soil pollution.

  1. Inhibitory effects of berberine on ion channels of rat hepatocytes

    Institute of Scientific and Technical Information of China (English)

    Fang Wang; Hong-Yi Zhou; Gang Zhao; Li-Ying Fu; Lan Cheng; Jian-Guo Chen; Wei-Xing Yao

    2004-01-01

    AIM: To examine the effects of berberine, an isoquinoline alkaloid with a long history used as a tonic remedy for liver and heart, on ion channels of isolated rat hepatocytes.METHODS: Tight-seal whole-cell patch-clamp techniques were performed to investigate the effects of berberine on the delayed outward potassium currents (IK), inward rectifier potassium currents (IK1) and Ca2+ release-activated Ca2+currents (ICRAC) in enzymatically isolated rat hepatocytes.RESULTS: Berberine 1-300 nmol/L reduced IK in a concentration dependent manner with EC50 of 38.86±5.37 μmol/L and nH of 0.82±0.05 (n = 8). When the bath solution was changed to tetraethylammonium (TEA) 8 mmol/L, IK was inhibited.Berberine 30 μmol/L reduced IK at all examined membrane potentials, especially at potentials positive to +60 mV (n = 8,P<0.05 or P<0.01 vs control). Berberine had mild inhibitory effects on IK1 in rat hepatocytes. Berberine 1-300 μmol/L also inhibited ICRAC in a concentration-dependent fashion.The fitting parameters were EC50 = 47.20±10.86 μmol/L,nH = 0.71±0.09 (n = 8). The peak value of ICRAC in the Ⅰ-Ⅴrelationship was decreased by berberine 30 μmol/L at potential negative to -80 mV (n = 8, P<0.05 vscontrol). But the reverse potential of ICRAC occurred at voltage 0 mV in all cells.CONCLUSION: Berberine has inhibitory effects on potassium and calcium currents in isolated rat hepatocytes, which may be involved in hepatoprotection.

  2. Acetylcholinesterase inhibitory effect of lignans isolated from Schizandra chinensis.

    Science.gov (United States)

    Hung, Tran Manh; Na, MinKyun; Min, Byung Sun; Ngoc, Tran Minh; Lee, IkSoo; Zhang, XinFeng; Bae, KiHwan

    2007-06-01

    The hexane extract of the fruit of Schizandra chinensis (Schisandraceae) was found to show significant inhibition of the activity of acetylcholinesterase enzyme (AChE). In further studies, fourteen lignans were isolated, and evaluated for their inhibitory effect on AChE. The compounds having both aromatic methylenedioxy and hydroxyl groups on their cyclooctadiene ring, such as gomisin C (6), gomisin G (7), gomisin D (8), schisandrol B (11) and gomisin A (13), entirely inhibited AChE in dose dependent manners, with IC50 values of 6.71 +/- 0.53, 6.55 +/- 0.31, 7.84 +/- 0.62, 12.57 +/- 1.07 and 13.28 +/- 1.68 microM, respectively. These results indicate that the lignans could potentially be a potent class of AChE inhibitors.

  3. Steve Woods's contribution to research on amylin's eating inhibitory effect.

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    Lutz, Thomas Alexander

    2011-04-18

    Amylin is secreted by pancreatic beta-cells and seems to function as a physiological signal of satiation and possibly also as an adiposity signal. Amylin's satiating effect is mediated via a direct action at area postrema (AP) neurons. The central pathways mediating amylin's effects rely on connections from the AP to the nucleus of the solitary tract and lateral parabrachial nucleus. Amylin was shown to interact, probably at the brainstem, with other satiating signals, namely cholecystokinin, glucagon-like peptide 1 and peptide YY, and other adiposity signals, namely leptin and insulin. The interaction with leptin, which is thought to involve the hypothalamus, may have important implications for the development of new and improved hormonal anti-obesity treatments. Steve Woods has contributed to the recent literature on amylin's eating inhibitory effect by some frequently cited publications. Steve's work concentrated more on the central administration of amylin and on amylin's potential role as an adiposity signal. His work will be reviewed here and discussed in the context of other important findings on amylin's role in the control of energy homeostasis.

  4. Inhibitory effects of the ferment liquids on sarcoma

    Institute of Scientific and Technical Information of China (English)

    Ming Lu; Yunqing Cai; Yan Zhao; Juanhua Xu; Xiaoli Wu

    2005-01-01

    Objective: To study the anti-tumor effects of the ferment liquid (FL) and to explore the anti-mutagenic effects induced by cyclophosphamide (CP). Methods: Anti-tumor effects and Anti-mutagenic effects induced by cyclophosphamide (CP) of the ferment liquid were observed in tumor-bearing mice in vivo. Spleen lymphocytes proliferation of mice was stimulated by ConA and NK cell activity was analyzed by the lactate dehydrogenase (LDH) release assay. Results: FL Ⅰ ,FL Ⅱ and FL Ⅲ of 16.7, 33.3 and 66.6ml/kg inhibited growth of Sarcoma 180 sighificanth by 11.6%, 24.2%, 28.0%, 4.8%, 15.2%, 2.2% and 2.1%, 8.5%, 5.2%respectively. Polychromatic erythrocytes (PCE) at all doses of FL Ⅰ and FL Ⅱ were greatly decreased compared with control group ( P <0.05), but FL Ⅲ has no inhibition effents( P > 0.05). Production of IL-2 showed no significant difference between all treatment groups.The NK cell killing activity in all treated mice increased by FL Ⅰ and FL Ⅱ was significantly potentiated compared to controls ( P <0.05). Lymphocytes proliferation of ICR mice were stimulated by ConA 2.5 ml/L and there were no differences between groups.Conclusion: The present data suggested that three kinds of ferment liquid used as health drink have anti-mutagenesis, immune enhancement effects and showed certain inhibitory effects on S180 tumor growth in vivo.

  5. Acetylcholinesterase inhibitory effects of some plants from Rosaceae

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    S. Esmaeili

    2015-10-01

    Full Text Available Background and objectives: Alzheimer's disease (AD is an age dependent disorder. AD is associated with decrease of brain acetylcholine level. Nowadays, one of the methods for progression inhibition of AD is using acetylcholinesterase inhibitors. Rosaceae is a large plant family. Different biological effects of some species of this family have been reported. The aim of the present study was to assess the acetylcholinesterase inhibitory (AChEI activity of the selected plants belonging to Rosaceae family. Methods: AChEI activity of six species from Rosaceae including Cotoneaster nummularia, Cerasus microcarpa, Amygdalus scoparia, Agrimonia eupatoria, Rosa canina and Rosa damascena were evaluated based on Ellman’s method in concentration of 300 µg/mL using total extracts and methanol fractions which were obtained by maceration. Results: The results showed that the total extract and methanol fraction of the aerial parts of A. eupatoria demonstrated significant AChEI activity with 46.5% and 56.2% inhibition of the enzyme, respectively. Conclusion: According to the results of the AChEI activity of the methanol fraction of A. eupatoria, it seems that the polar components of the species such as flavonoids may be responsible for its effectiveness.

  6. Inhibitory effect of common microfluidic materials on PCR outcome

    KAUST Repository

    Kodzius, Rimantas

    2013-10-10

    In this study, we established a simple method for evaluating the PCR compatibility of various common materials employed when fabricating microfluidic chips, including silicon, several kinds of silicon oxide, glasses, plastics, wax, and adhesives. Two-temperature PCR was performed with these materials to determine their PCR-inhibitory effect. In most cases, adding bovine serum albumin effectively improved the reaction yield. We also studied the individual PCR components from the standpoint of adsorption. Most of the materials did not inhibit the DNA, although they noticeably interacted with the polymerase. We provide a simple method of performing PCR-compatibility testing of materials using inexpensive instrumentation that is common in molecular biology laboratories. Furthermore, our method is direct, being performed under actual PCR conditions with high temperature. Our results provide an overview of materials that are PCR-friendly for fabricating microfluidic devices. The PCR reaction, without any additives, performed best with pyrex glass, and it performed worst with PMMA or acrylic glue materials.

  7. Inhibitory Effect of Natural Phenolic Compounds on Aspergillus parasiticus Growth

    Directory of Open Access Journals (Sweden)

    Romina P. Pizzolitto

    2015-01-01

    Full Text Available Considering the impact of Aspergillus species on crops, it appears to be highly desirable to apply strategies to prevent their growth, as well as to eliminate or reduce their presence in food products. For this reason, the aims of this investigation were to evaluate the effects of ten natural phenolic compounds on the Aspergillus parasiticus growth and to determine which physicochemical properties are involved in the antifungal activity. According to the results of minimum inhibitory concentration (MIC values of the individual compounds, isoeugenol, carvacrol, and thymol were the most active phenolic components (1.26 mM, 1.47 mM, and 1.50 mM, resp., followed by eugenol (2.23 mM. On the other hand, creosol, p-cresol, o-cresol, m-cresol, vanillin, and phenol had no effects on fungal development. Logarithm of the octanol/water partition coefficient (log P, refractivity index (RI, and molar volume (MV were demonstrated to be the descriptors that best explained the antifungal activity correlated to lipophilicity, reactivity of the components, and steric aspect. These findings make an important contribution to the search for new compounds with antifungal activity.

  8. The Inhibitory Effects of Arresten Protein on Tumor Formation

    Institute of Scientific and Technical Information of China (English)

    Yi Lv; Jin-ping Zheng

    2012-01-01

    To examine the inhibitory effects of recombinant purified arresten on tumor formation.Methods Purified arresten protein was incubated with human umbilical vein endothelial cells (HUVECs) and HeLa cells in vitro.The effect on proliferation of HUVECs and HeLa cells was examined using 3-(4,5)-dimethylthiahiazo (-z-y1)-3,5-di-phenytetrazoliumromide assay,and apoptosis of these cells monitored by flow cytometry.The effect on migration of HUVECs and HeLa cells was examined by Boyden chamber.Twenty colon carcinoma-bearing C67BL/6 mice were used to investigate the antitumor effects of arresten protein.The mice were randomly divided into arresten treatment group (n=10) and control group (n=10).The microvessel densities of the tumors were measured by immunohistochemical staining with anti-CD31 monoclonal antibody.Results Arresten inhibited the proliferation and migration of HUVECs in a dose-dependent manner while promoting apoptosis.However,arresten had no significant effects on the proliferation and apoptosis of HeLa cells.The migration of HeLa cells was modestly inhibited by arresten.The arresten treatment group of mice showed no weight loss or unusual behavior during the course of treatment,and the tumor growth was significantly decreased; in contrast,the control group of mice exhibited rapidly growing tumors and cachexia.A dramatically decreased microvessel density in tumor tissues was found in arresten-treated mice compared with that in the control mice.Conclusion Arresten can inhibit tumor growth through inhibition of tumor angiogenesis.

  9. The inhibitory effects of silver diamine fluorides on cysteine cathepsins.

    Science.gov (United States)

    Mei, May L; Ito, L; Cao, Y; Li, Q L; Chu, C H; Lo, Edward C M

    2014-03-01

    The expression of cysteine cathepsins in human carious dentine suggests that this enzyme contributes to the collagen degradation in caries progress. This study investigated whether silver diamine fluoride (SDF) inhibited the activity of cysteine cathepsins. Three commercial SDF solutions with concentrations at 38%, 30% and 12% were studied. Two fluoride solutions with the same fluoride ion (F(-)) concentrations as the 38% and 12% SDF solutions, and 2 silver solutions with the same silver ion (Ag(+)) concentrations as the 38% and 12% SDF solutions were prepared. Five samples of each experimental solution were used to study their inhibitory effect on two cathepsins (B and K) using cathepsin assay kits. Positive control contained assay buffer and cathepsins dilution was used to calculate the percentage inhibition (difference between the mean readings of the test solution and control solution divided by that of the control group). The percentage inhibition of 38%, 30% and 12% SDF on cathepsin B were 92.0%, 91.5% and 90.3%, respectively (pF(-) (pF(-) only (p<0.01). According to this study, SDF solution at all 3 tested concentrations significantly inhibited the activity of cathepsin B and K. Copyright © 2013 The Authors. Published by Elsevier Ltd.. All rights reserved.

  10. Inhibitory effects of ionic liquids on the lactic dehydrogenase activity.

    Science.gov (United States)

    Dong, Xing; Fan, Yunchang; Zhang, Heng; Zhong, Yingying; Yang, Yang; Miao, Juan; Hua, Shaofeng

    2016-05-01

    Ionic liquids (ILs) were widely used in scientific and industrial application and have been reported to possess potential toxicity to the environment and human health. The effects of six typical N-methylimidazolium-based ILs ([Cnmim]X, n=4, 6, 8; X=Br(-), Cl(-), BF4(-), CF3SO3(-)) on the lactic dehydrogenase (LDH) activity and the molecular interaction mechanism of ILs and the LDH were investigated with the aid of spectroscopic techniques. Experimental results showed that the LDH activity was inhibited in the presence of ILs. For the ILs with the same anion but different cations, their inhibitory ability on the LDH activity increased with increasing the alkyl chain length on the IL cation. Thermodynamic parameters, enthalpy change (ΔH) and entropy change (ΔS) were obtained by analyzing the fluorescence behavior of LDH with the addition of ILs. Both positive ΔH and ΔS suggested that hydrophobicity was the major driven force in the interaction process as expected.

  11. Galectin-1 exerts inhibitory effects during DENV-1 infection.

    Directory of Open Access Journals (Sweden)

    Karina Alves Toledo

    Full Text Available Dengue virus (DENV is an enveloped RNA virus that is mosquito-transmitted and can infect a variety of immune and non-immune cells. Response to infection ranges from asymptomatic disease to a severe disorder known as dengue hemorrhagic fever. Despite efforts to control the disease, there are no effective treatments or vaccines. In our search for new antiviral compounds to combat infection by dengue virus type 1 (DENV-1, we investigated the role of galectin-1, a widely-expressed mammalian lectin with functions in cell-pathogen interactions and immunoregulatory properties. We found that DENV-1 infection of cells in vitro exhibited caused decreased expression of Gal-1 in several different human cell lines, suggesting that loss of Gal-1 is associated with virus production. In test of this hypothesis we found that exogenous addition of human recombinant Gal-1 (hrGal-1 inhibits the virus production in the three different cell types. This inhibitory effect was dependent on hrGal-1 dimerization and required its carbohydrate recognition domain. Importantly, the inhibition was specific for hrGal-1, since no effect was observed using recombinant human galectin-3. Interestingly, we found that hrGal-1 directly binds to dengue virus and acts, at least in part, during the early stages of DENV-1 infection, by inhibiting viral adsorption and its internalization to target cells. To test the in vivo role of Gal-1 in DENV infection, Gal-1-deficient-mice were used to demonstrate that the expression of endogenous Galectin-1 contributes to resistance of macrophages to in vitro-infection with DENV-1 and it is also important to physiological susceptibility of mice to in vivo infection with DENV-1. These results provide novel insights into the functions of Gal-1 in resistance to DENV infection and suggest that Gal-1 should be explored as a potential antiviral compound.

  12. [Inhibitory effects of natural medicines on the enzymes related to the skin].

    Science.gov (United States)

    Sawabe, Y; Yamasaki, K; Iwagami, S; Kajimura, K; Nakagomi, K

    1998-09-01

    In this paper, we investigated the inhibitory effects of water extracts from sixty-six natural medicines on the enzymes related to the skin, which were tyrosinase, hyaluronidase and collagenase. To clarify the inhibitory components in water extracts, tannin quantity and the inhibitory activity of the water extracts after removal of phenolic compounds using polyclar AT, were measured. Twelve kinds of natural medicines were found to have tyrosinase inhibitory activity. Six of them showed that tannin, which contains sufficient amounts in extracts, might be major inhibitory compounds due to a significant decrease of inhibition by these samples after removal of phenolic compounds. The inhibitory compound of Aurantii fructus immaturus was thought phenolic compounds except tannin. The inhibitory compounds may include Armeniacae semen, Perillae folium and Persicae semen besides a phenolic compound. Twenty-seven species among the natural medicines studied showed inhibitory activity on hyaluronidase. Phenolic compounds in these extracts except Artemisiae argyi folium, could not be candidates for hyaluronidase inhibitors. Seven kinds of the natural medicines have inhibitory activity on collagenase. It was estimated that these inhibitory compounds were phenolic compounds. These results are to be expected for finding novel compounds for skin disease or skin-care cosmetics.

  13. Effects of Response Preparation on Developmental Improvements in Inhibitory Control

    Science.gov (United States)

    Ordaz, Sarah; Stephanie, Davis; Luna, Beatriz

    2010-01-01

    Studies in adults indicate that response preparation is crucial to inhibitory control, but it remains unclear whether preparation contributes to improvements in inhibitory control over the course of childhood and adolescence. In order to assess the role of response preparation in developmental improvements in inhibitory control, we parametrically manipulated the duration of the instruction period in an antisaccade (AS) task given to participants ages 8 to 31 years. Regressions showing a protracted development of AS performance were consistent with existing research, and two novel findings emerged. First, all participants showed improved performance with increased preparation time, indicating that response preparation is crucial to inhibitory control at all stages of development. Preparatory processes did not deteriorate at even the longest preparatory period, indicating that the youngest participants were able to sustain preparation at even the longest interval. Second, developmental trajectories did not differ for different preparatory period lengths, highlighting that the processes supporting response preparation continue to mature in tandem with improvements in AS performance. Our findings suggest that developmental improvements are not simply due to an inhibitory system that is faster to engage but may also reflect qualitative changes in the processes engaged during the preparatory period. PMID:20347061

  14. Strategic eclecticism in hypnotherapy: effectiveness research considerations.

    Science.gov (United States)

    Amundson, Jon K; Nuttgens, Simon A

    2008-01-01

    Hypnosis is attempting to come to grips with the EST (Empirically Supported Therapy) revolution in mental health practice. However, there are ways to account for outcome outside of simple empirical validation of treatment models. In this light, strategic eclecticism as a broader research-based consideration is used to illustrate empirical principles within Eriksonian hypnotherapeutic approaches.

  15. Inhibitory effect of common microfluidic materials on PCR outcome

    KAUST Repository

    Kodzius, Rimantas

    2012-02-20

    compatibility of various materials commonly used while producing microfluidic devices is also pertinent and beneficial to other enzymatic reactions in microfluidic devices. Most PCR-friendly materials exhibit similar signals regardless of the inclusion or not of BSA in the PCR mixture; these materials are PP, PTFE, PDMS, wax (Tm 80°C), SiO2 quartz, pyrex and soda-lime glasses, NOA68, and mineral oil. Our results showed that there was near total adsorption of template DNA when the wax (Tm 60°C) was used (RBI = 9.2×101). In contrast, when NOA61, mineral oil and acrylic glue materials were employed, significant adsorption occurred (RBI < 1.5×103). The polymerase-inhibition experiments indicate that following materials do not have strong effects (RBI > 1.1×103) on polymerase: PC, PP, PTFE, PDMS, silicon with a layer of 560 nm SiO2, SiO2 quartz, pyrex, and soda-lime glass. Slight polymerase inhibition (RBI < 9.2×102) was observed with PMMA, PVC, waxes (Tm 56°C and 80°C), silicon, and NOA68. A very strong or near total inhibition (RBI < 1.8×102) was observed with wax (Tm 60°C), ITO glass, SU-8, NOA61, metal tubes, mineral oil, epoxy, and the acrylic glues. \\tOur results show that material selection for microfluidic PCR chips, which are characterized by large SAVR, is a vital part of optimizing PCR outcome. This study of the inhibitory effect of various common microfluidics materials has provided a new rapid testing method using only a PCR cycler, and it has confirmed and expanded the list of tested materials. The type of PCR compatibility test enables the most effectual choice of materials for use in biology-related experiments.

  16. Inhibitory Effects of Quercetin on Angiogenesis of Experimental Mammary Carcinoma

    Institute of Scientific and Technical Information of China (English)

    Lingquan Kong; Kainan Wu; Hui Lin

    2005-01-01

    OBJECTIVE To explore the inhibitory effects of quercetin on angiogenesis of experimental mammary carcinoma.METHODS A 7,12-dimethylbenzanthracene (DMBA)-induced animal model of mammary carcinoma was established in rats. Seventy-nine female Sprague-Dawly rats were randomized into 4 groups namely, DMBA, DMBA with tamoxifen (TAM), DMBA with quercetin and control agents identified as group A, B, C and D respectively. Treatment was for 28 weeks. Samples of breast tissues were collected for histopathological observation and microvessel density (MVD) estimation by light microscopy. The expression of basic fibroblast growth factor (bFGF), vascular endothelial growth factor (VEGF), and the protein product of H-ras were examined by immunohistochemical staining.tumor diameter of group A (76.2%, 2.37cm) were significantly higher than that in group B (40.9%, 1.82cm), C (45.5%, 1.71cm) and D (0%, 0cm) (P<0.05). There was no significant difference between groups B and C (P >0.05), which indicated that quercetin inhibited the incidence and growth of ing for VEGF, bFGF and the H-ras protein product showed significant differences between groups A and B, as well as groups A and C (P < 0.05), but no significant difference between groups B and C (P>0.05).CONCLUSION Quercetin can reduce the DMBA- induced mammary carcinoma incidence and tumor growth.The following mechanisms may be recausing inhibition of proliferation of the tumor cells and tumor angiogenesis.as VEGF and bFGF, so that angiogenesis in the mammary carcinomas is suppressed, with decreased mammary MVD in the rats receiving quercetin treatment.

  17. Synthesis of 2-Heterocyclomethyl-5-diphenylmethylenecyclopentanone Hydrochlorides and their Inhibitory Effect on Tumor Cell Growth

    Institute of Scientific and Technical Information of China (English)

    Yun Hai ZHANG; Lin Xiang ZHAO; Zhen Jun BIAN; Rui WANG; Fu Yuan SUN

    2006-01-01

    Sixteen new 2-heterocyclomethyl-5-diphenylmethylenecyclopentanone hydrochlorides were designed and synthesized. The growth inhibitory effect of these compounds in vitro was conducted using a MTT assay in human breast cancer T47D cells.

  18. Microbial contamination and inhibitory effect against Streptococcus mutans from fifth-generation bonding systems.

    Science.gov (United States)

    Pinheiro, Sérgio L; Soares, Herbert H; Ribeiro, Mariângela C

    2010-01-01

    The aim of this study was to evaluate microbial contamination and inhibitory effect against Streptococcus mutans (SM) of Prime & Bond (PB), Single Bond (SB) and Excite (EX) bonding systems before use, and after 10 and 20 applications. The bonding material was collected by applying a drop of the material directly on broth brain-heart infusion. The samples were homogenized, diluted and seeded on blood agar plates. To evaluate the inhibitory effect on SM, a drop of each bonding material was dispensed on filter discs and placed on blood agar plates. The Cochran statistical analysis was used to evaluate the total amount of viable bacteria among the different bonding systems. Comparisons between the inhibitory effects on SM were made using the Kruskal-Wallis test. Adhesives SB and EX presented microbial contamination (pcomposition, solvent and application technique of the bonding systems had an influence on contamination by the total number of bacteria and on the inhibitory effect on SM.

  19. Inhibitory effect of ketamine on lighting amygdala of rats

    Institute of Scientific and Technical Information of China (English)

    Jiguo Zhang; Bin Yang; Jing Zhang; Feng Zhang; Wang Yue

    2006-01-01

    BACKGROUND: Ketamine is a noncompetitive antagonist of N-methyl-D-aspartic acid receptor. Some researchers suggest that N-methyl-D-aspartic acid (NMDA) receptor is closely related to epileptic attack.OBJECTIVE: To observe inhibitory effect of ketamine on lighting amygdala of rats and analyze pathway of anti-lighting.DESIGN: Randomized controlled animal study.SETTING: Department of Pharmacology and Department of Management, Pharmacological College of Taishan Medical College; Department of Pharmacology, Medical College of Qingdao University.MATERIALS: Sixty adult female Wistar rats, of clean grade, weighing 180-200 g, were provided by Animal Center of Qingdao Institute of Drug Control. Ketamine hydrochloride was provided by the First Pharmacological Factory of the First Biochemical Pharmacology Company of Shanghai, and nicardipine, an antagonist of calcium ions, was provided by Sigma Company.METHODS: The experiment was completed in the Department of Pharmacology, Medical College of Qingdao University from March to November 2004. ① Model establishing: After anesthesia, left and right amygdalas were inserted with double electrodes. The top was separated about 0.25 mm, and the other end was welded with a micro-plug, respectively. Electrode and micro-plug were fixed with dental base acrylic resin powder at the surface of cranium. Two weeks after recovery, right amygdala was stimulated with constant current once a day. According to Racine technique, attacking intensity was divided into 5 grades: grade I:closing eyes, a little tingling of beards and twitching face; grade Ⅱ: nodding, chewing accompanying with twitching face; grade Ⅲ: raising one of a forelimb and clonus; grade Ⅳ: standing accompanying with bilateral forelimbs; grade Ⅴ: standing accompanying with falling down. Rats with grades Ⅳ and Ⅴ were used to establish secondarily generalized epilepsy. If 3 successive attacks of grade Ⅴ were observed, the lighting was to be successful. ② Effect of

  20. Cholinestrase inhibitory effects of geranylated flavonoids from Paulownia tomentosa fruits.

    Science.gov (United States)

    Cho, Jung Keun; Ryu, Young Bae; Curtis-Long, Marcus J; Ryu, Hyung Won; Yuk, Heung Joo; Kim, Dae Wook; Kim, Hye Jin; Lee, Woo Song; Park, Ki Hun

    2012-04-15

    Alzheimer's disease is rapidly becoming one of the most prevalent human diseases. Inhibition of human acetylcholinestrase (hAChE) and butyrylcholinestrase (BChE) has been linked to amelioration of Alzheimer's symptoms and research into inhibitors is of critical importance. Purification of the methanol extract of Paulownia tomentosa fruits yielded potent hAChE and BChE inhibitory flavonoids (1-9). A comparative activity screen indicated that a geranyl group at C6 is crucial for both hAChE and BChE. For example, diplacone (8) showed 250-fold higher efficacy than its parent eriodictyol (12). IC(50)s of diplacone (8) were 7.2 μM for hAChE and 1.4 μM for BChE. Similar trends were also observed for 4'-O-methyldiplacone (4) (vs its parent, hesperetin 10) and mimulone (7) (vs its parent, naringenin 11). Representative inhibitors (1-8) showed mixed inhibition kinetics as well as time-dependent, reversible inhibition toward hAChE. The binding affinities of these compounds to hAChE were investigated by monitoring quenching of inherent enzyme fluorescence. The affinity constants (K(SA)) increased in proportion to inhibitory potencies.

  1. Inhibitory Effects of Ginsenoside-Rb2 on Nicotinic Stimulation-Evoked Catecholamine Secretion

    Science.gov (United States)

    Lim, Hyo-Jeong; Lee, Hyun-Young

    2014-01-01

    The aim of the present study was to investigate whether ginsenoside-Rb2 (Rb2) can affect the secretion of catecholamines (CA) in the perfused model of the rat adrenal medulla. Rb2 (3~30 µM), perfused into an adrenal vein for 90 min, inhibited ACh (5.32 mM)-evoked CA secretory response in a dose- and time-dependent fashion. Rb2 (10 µM) also time-dependently inhibited the CA secretion evoked by DMPP (100 µM, a selective neuronal nicotinic receptor agonist) and high K+ (56 mM, a direct membrane depolarizer). Rb2 itself did not affect basal CA secretion (data not shown). Also, in the presence of Rb2 (50 µg/mL), the secretory responses of CA evoked by veratridine (a selective Na+ channel activator (50 µM), Bay-K-8644 (an L-type dihydropyridine Ca2+ channel activator, 10 µM), and cyclopiazonic acid (a cytoplasmic Ca2+-ATPase inhibitor, 10 µM) were significantly reduced, respectively. Interestingly, in the simultaneous presence of Rb2 (10 µM) and L-NAME (an inhibitor of NO synthase, 30 µM), the inhibitory responses of Rb2 on ACh-evoked CA secretory response was considerably recovered to the extent of the corresponding control secretion compared with the inhibitory effect of Rb2-treatment alone. Practically, the level of NO released from adrenal medulla after the treatment of Rb2 (10 µM) was greatly elevated compared to the corresponding basal released level. Collectively, these results demonstrate that Rb2 inhibits the CA secretory responses evoked by nicotinic stimulation as well as by direct membrane-depolarization from the isolated perfused rat adrenal medulla. It seems that this inhibitory effect of Rb2 is mediated by inhibiting both the influx of Ca2+ and Na+ into the adrenomedullary chromaffin cells and also by suppressing the release of Ca2+ from the cytoplasmic calcium store, at least partly through the increased NO production due to the activation of nitric oxide synthase, which is relevant to neuronal nicotinic receptor blockade. PMID:25352764

  2. Inhibitory Effect of Capparis spinosa Extract on Pancreatic Alpha-Amylase Activity

    Directory of Open Access Journals (Sweden)

    Mostafa Selfayan

    2016-04-01

    Full Text Available Background Diabetes mellitus is a metabolic disorder characterized by high blood glucose level caused due to deficiency of insulin secretion or insulin function. The inhibition of carbohydrate hydrolyzing enzymes such as α-amylase can be an important strategy for decrease postprandial blood glucose level in patients with type II diabetes. Plants contains different chemical constituents with potential for inhibition of α-amylase and hence maybe used as therapeutic. Objectives The aim of the present study is to investigate the effect of the ethanolic extract of Capparis spinosa on pancreatic α-amylase activities to find out the relevance of the plant in controlling blood sugar. Materials and Methods In this experimental study, root and leaves of C. spinosa were tested for α-amylase inhibition. Different concentrations (1.56, 3.12, 6.25, 12.5 and 25 mg/mL of extracts were incubated with enzyme substrate solution and the spectrometric method used for measure enzyme activity. Also acarbose was used as the standard inhibitor. Results Both root and leaves extracts showed inhibition of α-amylase (root = 97.31% and leaves = 98.92%. The root and leaves extracts of C. spinosa exhibited appreciable α-amylase inhibitory activity with an IC50 values 5.93 mg/mL and 3.89 mg/mL respectively, when compared with acarbose (IC50 value 0.038 mg/mL. Conclusions This study supports that root and leaves extracts of C. spinosa exhibit considerable α-amylase inhibitory activities. These results could be useful for developing functional foods by combination of plant-based foods for treatment of diabetes mellitus.

  3. Inhibitory effect of Lactobacillus salivarius on Streptococcus mutans biofilm formation.

    Science.gov (United States)

    Wu, C-C; Lin, C-T; Wu, C-Y; Peng, W-S; Lee, M-J; Tsai, Y-C

    2015-02-01

    Dental caries arises from an imbalance of metabolic activities in dental biofilms developed primarily by Streptococcus mutans. This study was conducted to isolate potential oral probiotics with antagonistic activities against S. mutans biofilm formation from Lactobacillus salivarius, frequently found in human saliva. We analysed 64 L. salivarius strains and found that two, K35 and K43, significantly inhibited S. mutans biofilm formation with inhibitory activities more pronounced than those of Lactobacillus rhamnosus GG (LGG), a prototypical probiotic that shows anti-caries activity. Scanning electron microscopy showed that co-culture of S. mutans with K35 or K43 resulted in significantly reduced amounts of attached bacteria and network-like structures, typically comprising exopolysaccharides. Spot assay for S. mutans indicated that K35 and K43 strains possessed a stronger bactericidal activity against S. mutans than LGG. Moreover, quantitative real-time polymerase chain reaction showed that the expression of genes encoding glucosyltransferases, gtfB, gtfC, and gtfD was reduced when S. mutans were co-cultured with K35 or K43. However, LGG activated the expression of gtfB and gtfC, but did not influence the expression of gtfD in the co-culture. A transwell-based biofilm assay indicated that these lactobacilli inhibited S. mutans biofilm formation in a contact-independent manner. In conclusion, we identified two L. salivarius strains with inhibitory activities on the growth and expression of S. mutans virulence genes to reduce its biofilm formation. This is not a general characteristic of the species, so presents a potential strategy for in vivo alteration of plaque biofilm and caries.

  4. Thermodynamics of the Casimir Effect Asymptotic Considerations

    CERN Document Server

    Mitter, H

    1998-01-01

    We study the Casimir effect with different temperatures between the plates ($T$) resp. outside of them ($T'$). If we consider the inner system as the black body radiation for a special geometry, then contrary to common belief the temperature approaches a constant value for vanishing volume during isentropic processes. This means: the reduction of the degrees of freedom can not be compensated by a concentration of the energy during an adiabatic contraction of the two-plate system. Looking at the Casimir pressure, we find one unstable equilibrium point for isothermal processes with $T > T'$. For isentropic processes there is additionally one stable equilibrium point for larger values of the distances between the two plates.}

  5. Inhibitory effects of chitosan on superoxide anion radicals and lipid free radicals

    Institute of Scientific and Technical Information of China (English)

    2002-01-01

    With the electron spin resonance (ESR) technique, the inhibitory effects of chitosan on superoxide anion radicals and linoleic acid lipid radicals were found. The inhibitory ratio E for these two kinds of radicals is in proportion to the concentration of chitosan. It was also observed that E for linoleic acid lipid radicals increased with the increase of the degree of deacetylation and decreased with the increase of the molecular weight of chitosan.

  6. Melatonin nephroprotective action in Zucker diabetic fatty rats involves its inhibitory effect on NADPH oxidase.

    Science.gov (United States)

    Winiarska, Katarzyna; Dzik, Jolanta M; Labudda, Mateusz; Focht, Dorota; Sierakowski, Bartosz; Owczarek, Aleksandra; Komorowski, Lukasz; Bielecki, Wojciech

    2016-01-01

    Excessive activity of NADPH oxidase (Nox) is considered to be of importance for the progress of diabetic nephropathy. The aim of the study was to elucidate the effect of melatonin, known for its nephroprotective properties, on Nox activity under diabetic conditions. The experiments were performed on three groups of animals: (i) untreated lean (?/+) Zucker diabetic fatty (ZDF) rats; (ii) untreated obese diabetic (fa/fa) ZDF rats; and (iii) ZDF fa/fa rats treated with melatonin (20 mg/L) in drinking water. Urinary albumin excretion was measured weekly. After 4 wk of the treatment, the following parameters were determined in kidney cortex: Nox activity, expression of subunits of the enzyme, their phosphorylation and subcellular distribution. Histological studies were also performed. Compared to ?/+ controls, ZDF fa/fa rats exhibited increased renal Nox activity, augmented expression of Nox4 and p47(phox) subunits, elevated level of p47(phox) phosphorylation, and enlarged phospho-p47(phox) and p67(phox) content in membrane. Melatonin administration to ZDF fa/fa rats resulted in the improvement of renal functions, as manifested by considerable attenuation of albuminuria and some amelioration of structural abnormalities. The treatment turned out to nearly normalize Nox activity, which was accompanied by considerably lowered expression and diminished membrane distribution of regulatory subunits, that is, phospho-p47(phox) and p67(phox) . Thus, it is concluded that: (i) melatonin beneficial action against diabetic nephropathy involves attenuation of the excessive activity of Nox; and (ii) the mechanism of melatonin inhibitory effect on Nox is based on the mitigation of expression and membrane translocation of its regulatory subunits.

  7. Piracetam counteracts the effects of amitriptyline on inhibitory avoidance in CD1 mice.

    Science.gov (United States)

    Everss, Estrella; Arenas, M Carmen; Vinader-Caerols, Concepción; Monleón, Santiago; Parra, Andrés

    2005-04-30

    The purpose of the present work was to study the effects of amitriptyline on animal cognition in relation to some characteristics of its therapeutic effects. The modulation of acute and chronic effects of amitriptyline on inhibitory avoidance in male and female mice by piracetam was investigated. In Experiment 1, mice were subjected to the training phase of inhibitory avoidance conditioning 60 min after acute piracetam (100 mg/kg) or physiological saline administration. Immediately after the behavioural task, they received a single injection of the tricyclic antidepressant amitriptyline (30 mg/kg) or physiological saline. Twenty-four hours later, subjects were tested for avoidance. In Experiment 2, the same doses of amitriptyline and piracetam were chronically administered. Mice were subjected to the training phase of inhibitory avoidance on the 22nd day, and to the test phase 24 h later. Forty-five minutes after test, subjects explored the elevated plus-maze for 5 min in order to assess whether the effects of amitriptyline on avoidance performance may reflect general behavioural changes. Results obtained were that: (a) acute and chronic amitriptyline impaired inhibitory avoidance of male and female mice, (b) piracetam counteracted the effect of acutely administered amitriptyline on inhibitory avoidance, and (c) piracetam counteracted the effects of chronically administered amitriptyline in males but not females in the same learning task. These effects do not seem to be mediated by non-specific drug effects on spontaneous motor activity or anxiety.

  8. Inhibitory effects of pomegranate extracts on recombinant human maltase-glucoamylase.

    Science.gov (United States)

    Kawakami, Kayoko; Li, Peng; Uraji, Misugi; Hatanaka, Tadashi; Ito, Hideyuki

    2014-09-01

    α-Glucosidase inhibitors are currently used in the treatment of type 2 diabetes. In this study, we investigated the inhibitory activities of aril and pericarp extracts from pomegranates obtained various regions against recombinant human maltase-glucoamylase (MGAM). The inhibitory activities of the aril extracts tended to be stronger than those of the pericarp extracts. The Iranian aril extract was the most effective inhibitor. We investigated the polyphenol content of the pomegranate extracts using the Folin-Ciocalteu method. Among the aril extracts, the Iranian aril extract showed the highest polyphenol content. We further evaluated inhibitory activity against α-glucosidase from the rat small intestine. Pomegranate extract used in this study showed slightly different inhibitory activities according to α-glucosidase origin. Iranian aril extract was the most effective inhibitor of α-glucosidases, especially recombinant human MGAM. Bioassay-guided fractionation of the pomegranate arils led to identification of punicalagin and oenothein B as potent inhibitors of α-glucosidase. Oenothein B showed inhibitory activity with a half-maximal inhibitory concentration (IC(50)) value of 174 μM. Its potency was comparable to that of the α-glucosidase inhibitor acarbose with an IC(50) value of 170 μM. Dixon plot kinetic analysis of oenothein B showed a noncompetitive inhibition with a K(i) value of 102 μM. These results suggest that pomegranate arils would be useful for suppressing postprandial hyperglycemia.

  9. Inhibitory effect of agmatine on proliferation of tumor cells by modulation of polyamine metabolism

    Institute of Scientific and Technical Information of China (English)

    Ji-fang WANG; Rui-bin SU; Ning WU; Bo XU; Xin-qiang LU; Yin LIU; Jin LI

    2005-01-01

    Aim: To assess the inhibitory effect of agmatine on tumor growth in vivo and tumor cell proliferation in vitro. Methods: The transplanted animal model,[3H]thymidine incorporation assay, 3- [4,5-dimethythiazol-2-yl]-2,5-diphenyltetrazo lium assay, and lactate dehydrogenase (LDH) release assay were performed.Results: Agmatine, at doses of 5-40 mg/kg, suppressed the S180 sarcoma tumor growth dose-dependently in mice in vivo and the highest inhibitory ratio reached 31.3% in Kunming mice and 50.0% in Balb/c mice, respectively. Similar results were obtained in the transplanted B16 melanoma tumor model. Agmatine (1-1000 μmol/L) was able to attenuate the proliferation of cultured MCF-7 human breast cancer cells in vitro in a concentration-dependent manner and the highest inhibitory ratio reached 50.3% in the [3H]thymidine incorporation assay.Additionally, in the LDH release assay, spermine (20 μmol/L) and spermidine (20 μmol/L) increased the LDH release significantly, but agmatine (1-1000 μmol/L) did not, indicating that the inhibitory effect of agmatine on the proliferation of MCF was not related to cellular toxicity. In the [3H]thymidine incorporation assay,putrescine (12.5-100.0 μmol/L) could reverse the inhibitory effect of agmatine on the proliferation of MCF concentration-dependently, suggesting that the inhibitory effect of agmatine on the proliferation of MCF might be associated with a decreased level of the intracellular polyamines pool. Conclusion: Agmatine had significant inhibitory effect on transplanted tumor growth in vivo and proliferation of tumor cells in vitro, and the mechanism might be a result of inducing decrease of intracellular polyamine contents.

  10. Anterograde effects of a single electroconvulsive shock on inhibitory avoidance and on cued fear conditioning

    Directory of Open Access Journals (Sweden)

    Oliveira M.G.M.

    1998-01-01

    Full Text Available A single electroconvulsive shock (ECS or a sham ECS was administered to male 3-4-month-old Wistar rats 1, 2, and 4 h before training in an inhibitory avoidance test and in cued classical fear conditioning (measured by means of freezing time in a new environment. ECS impaired inhibitory avoidance at all times and, at 1 or 2 h before training, reduced freezing time before and after re-presentation of the ECS. These results are interpreted as a transient conditioned stimulus (CS-induced anxiolytic or analgesic effect lasting about 2 h after a single treatment, in addition to the known amnesic effect of the stimulus. This suggests that the effect of anterograde learning impairment is demonstrated unequivocally only when the analgesic/anxiolytic effect is over (about 4 h after ECS administration and that this impairment of learning is selective, affecting inhibitory avoidance but not classical fear conditioning to a discrete stimulus.

  11. The Inhibitory Effect of Propranolol and Isoproterenol on Human Plasma Cholinesterase

    Directory of Open Access Journals (Sweden)

    Ali Awsat Mellati

    2002-10-01

    Full Text Available The effect of propranolol and isoproterenol on the hydrolysis of 4- nitrophenylbutyrate (PNPB by the purified human plasma cholinesterase was studied. During the hydrolysis of PNPB, enzyme obeyed to Michaelis-Menten model. Propranolol was found to be a competitive inhibitor, and isoproterenol yielded a complex inhibition pattern. It could be explained that the inhibitory effect of propranolol shows noncooperativity between subunits of human plasma cholinesterase upon binding of PNPB. In contrast, isoproternol inhibitory effects indicate more than one type of binding sites on this enzyme.

  12. Inhibitory effect of coated mannan against the adhesion of Candida biofilms to denture base resin.

    Science.gov (United States)

    Sato, Maki; Ohshima, Tomoko; Maeda, Nobuko; Ohkubo, Chikahiro

    2013-01-01

    The adherence of Candida on dentures is related to diseases such as denture stomatitis and aspiration pneumonia. Mannan is a major component of the Candida cell surface, and contributes to the cell adherence. A previous report indicated that the adherence of C. albicans to culture dishes was inhibited by the coating them with mannan. The purpose of this study was to examine the adhesion inhibitory effect of mannan coating on acrylic denture surfaces against C. albicans and C. glabrata. The amount of Candida attached on the acrylic surfaces coated with mannan was calibrated by culture methods. Mannan showed significant inhibitory effects on Candida adhesion in both the yeast and hyphal form in a concentration-dependent manner, and the durability of the inhibitory effect continued for three days. These results suggest that mannan coating on the denture base acrylic can prevent Candida adhesion on the denture.

  13. Inhibitory effect of ethanol, acetic acid, propionic acid and butyric acid on fermentative hydrogen production

    Energy Technology Data Exchange (ETDEWEB)

    Wang, Bo; Wan, Wei; Wang, Jianlong [Laboratory of Environmental Technology, INET, Tsinghua University, Beijing 100084 (China)

    2008-12-15

    The inhibitory effect of added ethanol, acetic acid, propionic acid and butyric acid on fermentative hydrogen production by mixed cultures was investigated in batch tests using glucose as substrate. The experimental results showed that, at 35 C and initial pH 7.0, during the fermentative hydrogen production, the substrate degradation efficiency, hydrogen production potential, hydrogen yield and hydrogen production rate all trended to decrease with increasing added ethanol, acetic acid, propionic acid and butyric acid concentration from 0 to 300 mmol/L. The inhibitory effect of added ethanol on fermentative hydrogen production was smaller than those of added acetic acid, propionic acid and butyric acid. The modified Han-Levenspiel model could describe the inhibitory effects of added ethanol, acetic acid, propionic acid and butyric acid on fermentative hydrogen production rate in this study successfully. The modified Logistic model could describe the progress of cumulative hydrogen production. (author)

  14. Inhibitory Effect of Gamma-Irradiated Chitosan on the Growth of Denitrifiers

    Directory of Open Access Journals (Sweden)

    Javier Vilcáez

    2009-01-01

    Full Text Available In order to find an environmentally benign substitute to hazardous inhibitory agents, the inhibitory effect of -irradiated chitosans against a mixed culture of denitrifying bacteria was experimentally evaluated. Unlike other studies using pure aerobic cultures, the observed effect was not a complete inhibition but a transient inhibition reflected by prolonged lag phases and reduced growth rates. Raw chitosan under acid conditions (pH 6.3 exerted the strongest inhibition followed by the 100 kGy and 500 kGy irradiated chitosans, respectively. Therefore, because the molecular weight of chitosan decreases with the degree of -irradiation, the inhibitory properties of chitosan due to its high molecular weight were more relevant than the inhibitory properties gained due to the modification of the surface charge and/or chemical structure by -irradiation. High dosage of -irradiated appeared to increase the growth of mixed denitrifying bacteria in acid pH media. However, in neutral pH media, high dosage of -irradiation appeared to enhance the inhibitory effect of chitosan.

  15. Involvement of the insular cortex in regulating glucocorticoid effects on memory consolidation of inhibitory avoidance training

    Directory of Open Access Journals (Sweden)

    Raquel eFornari

    2012-03-01

    Full Text Available Glucocorticoids are known to enhance the consolidation of memory of emotionally arousing experiences by acting upon a network of interconnected brain regions. Although animal studies typically do not consider the insular cortex (IC to be part of this network, the present findings indicate that the IC is importantly involved in regulating glucocorticoid effects on memory consolidation of emotionally arousing inhibitory avoidance training. The specific glucocorticoid receptor agonist RU 28362 (3 or 10 ng in 0.5 l infused bilaterally into the IC of male Sprague-Dawley rats immediately after one-trial inhibitory avoidance training dose-dependently enhanced 48-h retention performance. Moreover, training on the inhibitory avoidance task increased neuronal activity of the IC, as assessed by an increased number of cells expressing immunoreactivity for phosphorylated extracellular signal-regulated kinase 1/2 (pERK1/2. However, systemic administration of a memory-enhancing dose of corticosterone (1 mg/kg after inhibitory avoidance training rapidly reduced the number of pERK1/2-positive cells in the IC, suggesting that glucocorticoid administration reduces overall neuronal activity of the IC. To investigate which components of the inhibitory avoidance training experience were influenced by the intra-IC glucocorticoid administration, in the last experiment rats were trained on a modified inhibitory avoidance task in which context exposure and footshock training occur on two sequential days. RU 28362 administration into the IC enhanced later retention when infused immediately after either the context or footshock training. Thus, these findings indicate that the IC mediates glucocorticoid effects on the consolidation of memory of different components of inhibitory avoidance training and suggest that the IC might be an important element of the rodent brain network involved in emotional regulation of learning and memory.

  16. [Experimental study of the virus inhibitory effect of chuan-kang-ping granule].

    Science.gov (United States)

    Li, Z; Dong, G; Li, Z

    2001-03-01

    To explore the virus inhibitory effect of Chuan-Kang-Ping Granule. Using tissue culture technique, the maximal non-toxic concentration of the drugs in Hep-2 cell culture were measured and the virus inhibitory index of the drugs on the respiratory syncytial virus (RSV), the coxackie B3 virus (Cox B3) and the influenza A1 virus (A1) was calculated. In addition, the degrees of inhibition of the drugs on the cytopathic effect of viruses in cell culture was observed by changing sequence of adding the viruses and the drugs. The maximal non-toxic concentration of Chuan-Kang-Ping Granule was 1:16. The virus inhibitory index on RSV, CoxB3, A1 was 8.8 and 2, respectively. The maximal non-toxic concentration of Shuang-Huang-Lian oral administration Liquid was 1:32. The virus inhibitory index on RSV, CoxB3, A1 was 8, 16 and 2, respectively. The degrees of cytopathic effect were different when changing sequence of adding the viruses and the drugs. Chuan-Kang-Ping Granule inhibited the replication of RSV, CoxB3, A1 in cultured cells. The inhibitory effect of the drugs were the same or nearly the same with Shuang-Huang-Lian oral administration liquid. The mechanism of the inhibitory effects of the drugs on the viruses was probably the direct killing effect in vitro, or the drugs might inhibit some key link of the replication of the viruses in cultured cells.

  17. Inhibitory effects of rapamycin on proliferation of chronic myelogenous leukemia cells and its mechanism

    Institute of Scientific and Technical Information of China (English)

    李杰

    2012-01-01

    Objective To explore the inhibitory effects of rapamycin on proliferation of chronic myelogenous leukemia (CML) cells and its possible mechanism. Methods The effects of rapamycin at various concentrations on cell proliferation of CML cell line K562 cells were analyzed by MTT. The expressions

  18. Inhibitory effects of whisky congeners on melanogenesis in mouse B16 melanoma cells.

    Science.gov (United States)

    Ohguchi, Kenji; Koike, Minako; Suwa, Yoshihide; Koshimizu, Seiichi; Mizutani, Yuki; Nozawa, Yoshinori; Akao, Yukihiro

    2008-04-01

    We examined the effect of whisky congeners, substances other than ethanol in whisky, on melanogenesis in mouse B16 melanoma cells. Treatment with whisky congeners significantly blocked melanogenesis. Our results indicate that the inhibitory effects of whisky congeners on melanogenesis is due to direct inhibition of tyrosinase activity and to suppression of tyrosinase protein levels.

  19. Characterization of the inhibitory effect of growth hormone on primary preadipocyte differentiation

    DEFF Research Database (Denmark)

    Hansen, L. H.; Madsen, B; Teisner, Børge

    1998-01-01

    . A possible role for Pref-1/FA1 in mediating the antiadipogenic effect of GH was indicated by the observation that FA1 inhibited differentiation as effectively as GH. These data suggest that GH exerts its inhibitory activity in adipocyte differentiation at a step after the induction of ADD1 but before...... the induction of genes required for terminal differentiation....

  20. Acute alcohol effects on inhibitory control and implicit cognition: implications for loss of control over drinking

    NARCIS (Netherlands)

    M. Field; R.W. Wiers; P. Christiansen; M.T. Fillmore; J.C. Verster

    2010-01-01

    Alcohol impairs inhibitory control, and it alters implicit alcohol cognitions including attentional bias and implicit associations. These effects are seen after doses of alcohol which do not lead to global impairments in cognitive performance. We review studies which demonstrate that the effects of

  1. Triglyceride accumulation inhibitory effects of new chromone glycosides from Drynaria fortunei.

    Science.gov (United States)

    Han, Lifeng; Zheng, Fang; Zhang, Yi; Liu, Erwei; Li, Wei; Xia, Minghui; Wang, Tao; Gao, Xiumei

    2015-01-01

    Two new chromone glycosides, drynachromosides C (1) and D (2), along with five known chromones (3-7), were isolated from the rhizomes of Drynaria fortunei. The structures of the two new compounds were elucidated on the basis of physico-chemical property and spectroscopic data. Triglyceride (TG) accumulation inhibitory effects of the obtained chromones on 3T3-L1 cells were investigated. The results showed that 1, 2 and 5 exhibited inhibitory activity on TG accumulation. Effects of compounds 1 and 2 on mRNA expression of PPARγ, C/EBPα and aP2 in 3T3-L1 cells were also investigated.

  2. Inhibitory Effect of Lactobacillus reuteri on Some Pathogenic Bacteria Isolated From Women With Bacterial Vaginosis

    Directory of Open Access Journals (Sweden)

    Eslami

    2014-08-01

    Full Text Available Background Considering the high prevalence of bacterial vaginosis and its association with urinary tract infection in women and treatment of gynecologic problems occur when a high recurrence of bacterial vaginosis is often treated with antibiotics. Objectives The purpose of this study was to investigate the inhibitory effect of Lactobacillus reuteri on pathogenic bacteria isolated from women with bacterial vaginosis. Materials and Methods Ninety-six samples were obtained from vaginal discharge of women with bacterial vaginosis by a gynecologist with a Dacron swab and put in sterile tubes containing TSB broth and Thioglycollate broth. Then were immediately sent to the laboratory in cold chain for further assessment. Afterward, culture was transferred on blood agar, EMB, Palcam and differential diagnosis environments. Then cultures were incubated for 24 hours at 37 °C. Lactobacillus reuteri strains were cultured in MRS environment and transferred to laboratory. After purification of pathogenic bacteria, Lactobacillus reuteri inhibitory effect on pathogenic bacteria was evaluated by minimum inhibitory concentration (MIC and antibiogram. Statistical analysis was performed using SPSS software v.16. Results The results of this study demonstrated the inhibitory effect of Lactobacillus reuteri on some pathogenic bacteria that cause bacterial, including Staphylococcus aureus, Staphylococcus epidermidis, Staphylococcus saprophyticus, Streptococcus agalactiae, Enterococcus, Listeria monocytogenes and E. coli. Microscopic examination of stained smears of most Lactobacillus and pathogenic bacteria showed reduced. The prevalence of abnormal vaginal discharge, history of drug use, contraceptive methods and douching were 61%, 55%, 42% and 13%, respectively. Significant difference was observed between the use and non-use of IUD in women with bacterial. Conclusions Our findings indicated the inhibitory effect of Lactobacillus reuteri on pathogenic bacteria that

  3. An impedance response model for inhibitory effect of antibiotics on bacterial growth in biometallurgy

    Institute of Scientific and Technical Information of China (English)

    陶菡; 魏万之; 张书芬; 张进忠; 毛友安

    2004-01-01

    An impedance response model reflecting the inhibitory effect of antibiotics on bacterial growth in biometallurgy was established. Three inhibition parameters, i.e. the maximum amount inhibitory constant of the bacterial growth(K1 ), the maximum specific growth inhibitory constant(K2 ) and the lag time inhibitory constant(K3 ), were included in the model. The influence of these parameters on the response curve was discussed in detail. By fitting experimental data towards the proposed model, three growth parameters (A, μm and λ) in the presence of antibiotics were gained and compared. The results show that the growth ability of bacteria is decreased due to the influence of antibiotics. The experimental and fitted curves have goodness-of-fit in the range of 0. 987 - 1. 008. Moreover, the kinetic growth parameters obtained from this model are closed to those from the Logistics popular growth model.These results show that the proposed model is validity to reflect the inhibitory effect of antibiotics on bacteria.

  4. Inhibitory effects of silver zeolite on in vitro growth of fish egg pathogen, Saprolegnia sp.

    Institute of Scientific and Technical Information of China (English)

    Seyed Ali Johari; Mohammad Reza Kalbassi; Il Je Yu

    2014-01-01

    Objective:To investigate the effects of powdered silver zeolite (SZ) on the in vitro growth of the fish pathogen Saprolegnia sp. Methods: The antifungal activity of SZ was evaluated by determining the minimum inhibitory concentrations using two-fold serial dilutions of powdered SZ in a glucose yeast extract agar at 22 °C. The growth of Saprolegnia sp. on the SZ agar treatments was compared to that on SZ-free agar controls. Results:The results showed that SZ had an inhibitory effect on the in vitro growth of the tested fungi. The minimum inhibitory concentration of SZ for Saprolegnia sp. was also calculated at 600 mg/L, which is equal to 0.06 percent. Conclusions:SZ is a potential good candidate to replace teratogenic and toxic agents, such as malachite green in aquaculture systems.

  5. The inhibitory effect of disodium cromoglycate on the growth of Chlamydophila (Chlamydia) pneumoniae in vitro.

    Science.gov (United States)

    Yamazaki, Tsutomu; Yamaguchi, Tetsuya; Sasaki, Nozomu; Inoue, Miyuki; Sato, Kozue; Kishimoto, Toshio

    2006-04-01

    Chlamydophila (Chlamydia) pneumoniae is associated with asthma and several other respiratory illnesses. Disodium cromoglycate (DSCG) is known to inhibit both immediate and late asthmatic responses. In this study, the inhibitory effect of DSCG on the growth of C. pneumoniae was examined by minimum inhibitory concentration (MIC) and pre-inoculation minimal cidal concentration (MCC) assays using HL cells and C. pneumoniae AR-39. DSCG below the clinically relevant concentration inhibited the growth of C. pneumoniae in a dose-dependent manner in both the MCC and MIC assays. The inhibitory effect was also time-dependent in the MCC assay at 20 mg/ml of DSCG. These results warrant further clinical study on the connection between C. pneumoniae infections and use of DSCG.

  6. Inhibitory effects of Citrus hassaku extract and its flavanone glycosides on melanogenesis.

    Science.gov (United States)

    Itoh, Kimihisa; Hirata, Noriko; Masuda, Megumi; Naruto, Shunsuke; Murata, Kazuya; Wakabayashi, Keitaro; Matsuda, Hideaki

    2009-03-01

    The 50% ethanolic extract (CH-ext) obtained from the unripe fruit of Citrus hassaku exhibited significant tyrosinase inhibitory activity. The CH-ext showed antioxidant activity, such as superoxide dismutase (SOD)-like activity and 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical-scavenging activity. Activity-guided fractionation of the CH-ext indicated that flavanone glycoside-rich fractions showed potent tyrosinase inhibitory activity. Further examination revealed that the tyrosinase inhibitory activity and antioxidant activity of the CH-ext were attributable to naringin and neohesperidin, respectively. The CH-ext showed inhibition of melanogenesis without any effects on cell proliferation in cultured murine B16 melanoma cells after glucosamine exposure. The topical application of the CH-ext to the dorsal skin of brownish guinea pigs showed in vivo preventive effects against UVB-induced pigmentation.

  7. Inhibitory effects of sudanese medicinal plant extracts on hepatitis C virus (HCV) protease.

    Science.gov (United States)

    Hussein, G; Miyashiro, H; Nakamura, N; Hattori, M; Kakiuchi, N; Shimotohno, K

    2000-11-01

    One hundred fifty-two methanol and water extracts of different parts of 71 plants commonly used in Sudanese traditional medicine were screened for their inhibitory effects on hepatitis C virus (HCV) protease (PR) using in vitro assay methods. Thirty-four extracts showed significant inhibitory activity (>/=60% inhibition at 100 microg/mL). Of these, eight extracts, methanol extracts of Acacia nilotica, Boswellia carterii, Embelia schimperi, Quercus infectoria, Trachyspermum ammi and water extracts of Piper cubeba, Q. infectoria and Syzygium aromaticum, were the most active (>/=90% inhibition at 100 microg/mL). From the E. schimperi extract, two benzoquinones, embelin (I) and 5-O-methylembelin (II), were isolated and found as potent HCV-PR inhibitors with IC(50) values of 21 and 46 microM, respectively. Inhibitory activities of derivatives of I against HCV-PR as well as their effects on other serine proteases were also investigated.

  8. Life course models: improving interpretation by consideration of total effects.

    Science.gov (United States)

    Green, Michael J; Popham, Frank

    2016-12-28

    Life course epidemiology has used models of accumulation and critical or sensitive periods to examine the importance of exposure timing in disease aetiology. These models are usually used to describe the direct effects of exposures over the life course. In comparison with consideration of direct effects only, we show how consideration of total effects improves interpretation of these models, giving clearer notions of when it will be most effective to intervene. We show how life course variation in the total effects depends on the magnitude of the direct effects and the stability of the exposure. We discuss interpretation in terms of total, direct and indirect effects and highlight the causal assumptions required for conclusions as to the most effective timing of interventions.

  9. Bacterial mechanisms to overcome inhibitory effects of dietary tannins

    NARCIS (Netherlands)

    Smith, A.H.; Zoetendal, E.G.; Mackie, R.I.

    2005-01-01

    High concentrations of tannins in fodder plants inhibit gastrointestinal bacteria and reduce ruminant performance. Increasing the proportion of tannin-resistant bacteria in the rumen protects ruminants from antinutritional effects. The reason for the protective effect is unclear, but could be elucid

  10. INHIBITORY EFFECTS OF PERCHLOROETHYLENE ON HUMAN NEURONAL NICOTINIC ACETYLCHOLINE RECEPTORS.

    Science.gov (United States)

    Perchloroethylene (PERC) is a volatile organic solvent with a variety of industrial uses. PERC exposure has been shown to cause adverse neurological effects including deficits in vision and memory in exposed individuals. Despite knowledge of these effects, the mechanisms by whi...

  11. Bacterial mechanisms to overcome inhibitory effects of dietary tannins

    NARCIS (Netherlands)

    Smith, A.H.; Zoetendal, E.G.; Mackie, R.I.

    2005-01-01

    High concentrations of tannins in fodder plants inhibit gastrointestinal bacteria and reduce ruminant performance. Increasing the proportion of tannin-resistant bacteria in the rumen protects ruminants from antinutritional effects. The reason for the protective effect is unclear, but could be

  12. Inhibitory Effects of Daiokanzoto (Da-Huang-Gan-Cao-Tang on P-Glycoprotein

    Directory of Open Access Journals (Sweden)

    Yuka Watanabe

    2012-01-01

    Full Text Available We have studied the effects of various Kampo medicines on P-glycoprotein (P-gp, a drug transporter, in vitro. The present study focused on Daiokanzoto (Da-Huang-Gan-Cao-Tang, which shows the most potent inhibitory effects on P-gp among the 50 Kampo medicines studied, and investigated the P-gp inhibitory effects of Daiokanzoto herbal ingredients (rhubarb and licorice root and their components by an ATPase assay using human P-gp membrane. Both rhubarb and licorice root significantly inhibited ATPase activity, and the effects of rhubarb were more potent than those of licorice root. The content of rhubarb in Daiokanzoto is double that in licorice root, and the inhibition patterns of Daiokanzoto and rhubarb involve both competitive and noncompetitive inhibition, suggesting that the inhibitory effects of Daiokanzoto are mainly due to rhubarb. Concerning the components of rhubarb, concentration-dependent inhibitory effects were observed for (−-catechin gallate, (−-epicatechin gallate, and (−-epigallocatechin gallate. In conclusion, rhubarb may cause changes in the drug dispositions of P-gp substrates through the inhibition of P-gp. It appears that attention should be given to the interactions between these drugs and Kampo medicines containing rhubarb as an herbal ingredient.

  13. Simulated inhibitory effects of typical byproducts of biomass ...

    African Journals Online (AJOL)

    Aghomotsegin

    2015-07-29

    Jul 29, 2015 ... Saccharomyces cerevisiae and bioethanol production ... the effect of inhibitors on the viability of S. cerevisiae and ethanol productivity does not last and can ..... producing yeast and bacteria by degradation products produced.

  14. Inhibitory effect and mechanism of acarbose combined with gymnemic acidon maltose absorption in rat intestine

    Institute of Scientific and Technical Information of China (English)

    Hong Luo; Le Feng Wang; Toshiaki Imoto; Yasutaka Hiji

    2000-01-01

    AIM The control of diet regimen and nutrient intake, aiming to avoid the evaggerated levels of glucose andanabolic hormone is broadly accepted as basic treatment of diabetes mellitus. Maltose is an importanthydrolysate of starch, main source of nutrition. Acarbose is an alpha-D-glucosidase inhibitor but with a shortinhibitory duration. Gymnemic acid (GA), a group of triterpene glucuronides, inhibits glucose absorptionwith a longer effective duration but it needs a longer time to achieve its maximum effect. To determinewhether nutrient control in diabetic care can be improved by combination of them, we compared thecombinative and individual effect of acarbose and GA on maltose absorption and hydrolysis in smallintestine.METHODS The absorption and hydrolysis of maltose were studied by re-cyclic perfusion of intestinal loopsin situ and motility of the intestine was recorded with the intestinal loop in vitro, of Wistar rat.RESULTS The total inhibitory rate of maltose absorption was improved by the combination of GA (0.1 -1.0 mg/mL) and acarbose (0.1- 2.0 mmol/L) throughout their effective duration (P<0.05, U test ofMann-Whitney), although the improvement only could be seen in the low dosages during the first hour. Withthe combination, inhibitory duration of acarbose on maltose absorption was prolonged to 3 hours and theonset of GA inhibitory effect was fastened to 15 minutes. GAsuppressed the intestinal mobility with a goodcorrelation (r = 0.98) to the inhibitory effect of GA on maltose absorption and the inhibitory effect of2 mmol/L (higher dose) acarbose on maltose hydrolysis was dual modulated by 1 mg/mL GA in vivoindicating that the combined effects involved the functional alteration of intestinal barriers.CONCLUSION There are augmented effects of acarbose and GA, which involve pre-cellular andparacellular barriers. Furthermore, diabetic care can be improved by employing this combination.

  15. Potent Inhibitory Effect of Chinese Dietary Spices on Fatty Acid Synthase.

    Science.gov (United States)

    Jiang, Bing; Liang, Yan; Sun, Xuebing; Liu, Xiaoxin; Tian, Weixi; Ma, Xiaofeng

    2015-09-01

    Dietary spices have been adopted in cooking since ancient times to enhance flavor and also as food preservatives and disease remedies. In China, the use of spices and other aromatic plants as food flavoring is an integral part of dietary behavior, but relatively little is known about their functions. Fatty acid synthase (FAS) has been recognized as a remedy target, and its inhibitors might be applied in disease treatment. The present work was designed to assess the inhibitory activities on FAS of spices extracts in Chinese menu. The in vitro inhibitory activities on FAS of 22 extracts of spices were assessed by spectrophotometrically monitoring oxidation of NADPH at 340 nm. Results showed that 20 spices extracts (90.9 %) exhibited inhibitory activities on FAS, with half inhibition concentration (IC(50)) values ranging from 1.72 to 810.7 μg/ml. Among them, seven spices showed strong inhibitory effect with IC(50) values lower than 10 μg/ml. These findings suggest that a large proportion of the dietary spices studied possess promising inhibitory activities on FAS, and subsequently might be applied in the treatment of obesity and obesity-related human diseases.

  16. Effect of Jatropha curcas Peptide Fractions on the Angiotensin I-Converting Enzyme Inhibitory Activity

    Directory of Open Access Journals (Sweden)

    Maira R. Segura-Campos

    2013-01-01

    Full Text Available Hypertension is one of the most common worldwide diseases in humans. Angiotensin I-converting enzyme (ACE plays an important role in regulating blood pressure and hypertension. An evaluation was done on the effect of Alcalase hydrolysis of defatted Jatropha curcas kernel meal on ACE inhibitory activity in the resulting hydrolysate and its purified fractions. Alcalase exhibited broad specificity and produced a protein hydrolysate with a 21.35% degree of hydrolysis and 34.87% ACE inhibition. Ultrafiltration of the hydrolysate produced peptide fractions with increased biological activity (24.46–61.41%. Hydrophobic residues contributed substantially to the peptides’ inhibitory potency. The 5–10 and <1 kDa fractions were selected for further fractionation by gel filtration chromatography. ACE inhibitory activity (% ranged from 22.66 to 45.96% with the 5–10 kDa ultrafiltered fraction and from 36.91 to 55.83% with the <1 kDa ultrafiltered fraction. The highest ACE inhibitory activity was observed in F2 ( μg/mL from the 5–10 kDa fraction and F1 ( μg/mL from the <1 kDa fraction. ACE inhibitory fractions from Jatropha kernel have potential applications in alternative hypertension therapies, adding a new application for the Jatropha plant protein fraction and improving the financial viability and sustainability of a Jatropha-based biodiesel industry.

  17. The Divergent Effects of Fear and Disgust on Inhibitory Control: An ERP Study

    Science.gov (United States)

    Xu, Mengsi; Li, Zhiai; Ding, Cody; Zhang, Junhua; Fan, Lingxia; Diao, Liuting; Yang, Dong

    2015-01-01

    Negative emotional stimuli have been shown to attract attention and impair executive control. However, two different types of unpleasant stimuli, fearful and disgusting, are often inappropriately treated as a single category in the literature on inhibitory control. Therefore, the present study aimed to investigate the divergent effects of fearful and disgusting distracters on inhibitory control (both conscious and unconscious inhibition). Specifically, participants were engaged in a masked Go/No-Go task superimposed on fearful, disgusting, or neutral emotional contexts, while event-related potentials were measured concurrently. The results showed that for both conscious and unconscious conditions, disgusting stimuli elicited a larger P2 than fearful ones, and the difference waves of P3 amplitude under disgusting contexts were smaller than that under fearful contexts. These results suggest that disgusting distracters consume more attentional resources and therefore impair subsequent inhibitory control to a greater extent. This study is the first to provide electrophysiological evidence that fear and disgust differently affect inhibitory control. These results expand our understanding of the relationship between emotions and inhibitory control. PMID:26030871

  18. Cellular target recognition of perfluoroalkyl acids: In vitro evaluation of inhibitory effects on lysine decarboxylase

    Energy Technology Data Exchange (ETDEWEB)

    Wang, Sufang; Lv, Qiyan; Yang, Yu, E-mail: yuyang@rcees.ac.cn; Guo, Liang-Hong, E-mail: LHGuo@rcees.ac.cn; Wan, Bin; Zhao, Lixia

    2014-10-15

    Perfluoroalkyl acids (PFAAs) have been shown to bind with hepatic peroxisome proliferator receptor α, estrogen receptors and human serum albumin and subsequently cause some toxic effects. Lysine decarboxylase (LDC) plays an important role in cell growth and developmental processes. In this study, the inhibitory effect of 16 PFAAs, including 13 perfluorinated carboxylic acids (PFCAs) and 3 perfluorinated sulfonic acids (PFSAs), on lysine decarboxylase (LDC) activity was investigated. The inhibition constants obtained in fluorescence enzyme assays fall in the range of 2.960 μM to 290.8 μM for targeted PFCAs, and 41.22 μM to 67.44 μM for targeted PFSAs. The inhibitory effect of PFCAs increased significantly with carbon chain (7–18 carbons), whereas the short chain PFCAs (less than 7 carbons) did not show any effect. Circular dichroism results showed that PFAA binding induced significant protein secondary structural changes. Molecular docking revealed that the inhibitory effect could be rationalized well by the cleft binding mode as well as the size, substituent group and hydrophobic characteristics of the PFAAs. At non-cytotoxic concentrations, three selected PFAAs inhibited LDC activity in HepG2 cells, and subsequently resulted in the decreased cadaverine level in the exposed cells, suggesting that LDC may be a possible target of PFAAs for their in vivo toxic effects. - Highlights: • Inhibitory effects of PFAAs on lysine decarboxylase activity were evaluated. • Four different methods were employed to investigate the mechanisms. • The long chain PFAAs showed inhibitory effect compare with 4–6 carbon chain. • The long chain PFAAs bound with LDC differently from the short ones. • The results in cells correlate with those obtained from fluorescence assay.

  19. Withanolides from Physalis minima and their inhibitory effects on nitric oxide production.

    Science.gov (United States)

    Guan, Yu-Zhou; Shan, Si-Ming; Zhang, Wei; Luo, Jian-Guang; Kong, Ling-Yi

    2014-04-01

    Six new withanolides (1-6), including two uncommon 1,10-seco withanolides (1 and 2), together with five known withanolides (7-11), were isolated from the whole plants of Physalis minima Linn.. The structures of new compounds were elucidated through spectroscopic methods, including (1)H, (13)C NMR, 2D-NMR, HRESIMS and circular dichroism (CD). Inhibitory effects of the isolates on nitric oxide (NO) production in lipopolysaccaride-activated RAW264.7 macrophages were evaluated. Compounds 2 and 5 showed strong inhibitory activities with IC50 values of 8.04 and 10.01 μM, respectively. Compounds 1, 9 and 10 exhibited moderate inhibitory activities with IC50 values from 25.54 to 43.58 μM.

  20. Inhibitory effect of puerarin on proliferation of retinoblastoma cells ...

    African Journals Online (AJOL)

    Methods: The effect of puerarin was examined on human retinoblastoma Y79 cells ... International Pharmaceutical Abstract, Chemical Abstracts, Embase, Index Copernicus, EBSCO, African. Index Medicus, JournalSeek, Journal Citation Reports/Science Edition, ..... Hou SZ, Su ZR, Chen SX, Ye MR, Huang S, Liu L, Lai. XP.

  1. In vitro evaluation of inhibitory effect of Phoenix dactylifera bark ...

    African Journals Online (AJOL)

    dactylifera bark extract on rat lipid peroxidation and blood hemolysis ... proteins, lipids, and DNA of the cell. Compared ... Free radicals increase the oxidation of unsaturated fatty acids ... food in central Asia and North Africa. ... brain were analyzed as follows: One gram of .... effect of sesame oil against lipid peroxidation and.

  2. Inhibitory Effects of seco-Triterpenoids from Acanthopanax sessiliflorus Fruits on HUVEC Invasion and ACE Activity.

    Science.gov (United States)

    Lee, Jin-Won; Baek, Nam-In; Lee, Dae-Young

    2015-09-01

    This study was conducted to investigate the effects of the crude extract from Acanthopanax sessiliflorus fruits and the isolated seco-triterpenoids from the crude extract on blood flow in human umbilical vein endothelial cell (HUVEC) invasion assay and angiotensin converting enzyme (ACE) inhibitory activity assay. On the basis of DMSO, the extent of HUVECs' invasion was remarkably decreased with crude extract concentrations of 400 and 1000 pg/mL. Additionally, the extent of the HUVEC invasion inhibitory effect in 400 and 1000 µg/mL of acanthosessilioside F were 55.8% and 72.4%, respectively. In addition, the maximum extent of the HUVEC invasion inhibitory effect of 22-α-hydroxychiisanoside was 88.9%. The IC50 value of the inhibitory effect on ACE activity in the crude extract was 4 µg/mL. The isolated seco-triterpenoids, 22α-hydroxychiisanogenin, 3,4-seco-lupan-20(30)-en-3,28-dioic acid, (lR)-1,4-epoxy-11α,22α-hydroxy-3,4-seco-lupan-20(30)-en-3,28-dioicacid, (+)-divaroside, and chiisanosidehad showed very high inhibitory effects on ACE activity, ranging from 1.8 to 2.9 µg/mL, which is much higher than the 150.0 µg/mL effect of aspirin. These results suggest that the crude extract from Acanthopanax sessiliflorus fruits and the isolated seco-triterpenoids from the crude extract enhance the blood flow effect by decreasing ACE activity.

  3. In vivo hypotensive effect and in vitro inhibitory activity of some Cyperaceae species

    Directory of Open Access Journals (Sweden)

    Monica Lacerda Lopes Martins

    2013-12-01

    Full Text Available In 1820, French naturalist August Saint Hillaire, during a visit in Espírito Santo (ES, a state in southeastern Brazil, reported a popular use of Cyperaceae species as antidote to snake bites. The plant may even have a hypotensive effect, though it was never properly researched. The in vitro inhibitory of the angiotensin converting enzyme (ACE activity of eigth ethanolic extracts of Cyperaceae was evaluated by colorimetric assay. Total phenolic and flavonoids were determined using colorimetric assay. The hypotensive effect of the active specie (Rhychonospora exaltata, ERE and the in vivo ACE assay was measured in vivo using male Wistar Kyoto (ERE, 0.01-100mg/kg, with acetylcholine (ACh as positive control (5 µg/kg, i.v.. The evaluation of ACE in vivo inhibitory effect was performed comparing the mean arterial pressure before and after ERE (10 mg/kg in animals which received injection of angiotensin I (ANG I; 0,03, 03 and 300 µg/kg, i.v.. Captopril (30 mg/kg was used as positive control. Bulbostylis capillaris (86.89 ± 15.20% and ERE (74.89 ± 11.95%, ERE were considered active in the in vitro ACE inhibition assay, at 100 µg/mL concentration. ACh lead to a hypotensive effect before and after ERE's curve (-40±5% and -41±3%. ERE showed a dose-dependent hypotensive effect and a in vivo ACE inhibitory effect. Cyperaceae species showed an inhibitory activity of ACE, in vitro, as well as high content of total phenolic and flavonoids. ERE exhibited an inhibitory effect on both in vitro and in vivo ACE. The selection of species used in popular medicine as antidotes, along with the in vitro assay of ACE inhibition, might be a biomonitoring method for the screening of new medicinal plants with hypotensive properties.

  4. Inhibitory Effect of Helicteres gardneriana Ethanol Extract on Acute Inflammation

    Directory of Open Access Journals (Sweden)

    Juliana Oliveira de Melo

    2012-01-01

    Full Text Available The anti-inflammatory effect of an ethanol extract of Helicteres gardneriana (Nees Castiglioni was assayed in experimental models of pleurisy and microcirculation in situ. Treatment of animals with 500 mg/kg body weight reduced the exudate volume (35% reduction induced by intrapleural injection of carrageenan and the migration of polymorphonuclear cells into the inflamed pleural cavity of rats (40%. Additionally, rolling and adhesion of leukocytes and the number of leukocytes that migrated toward the perivascular space in response to the carrageenan injection were decreased by the extract (500 mg/kg. These data demonstrate the anti-inflammatory effect of the ethanol extract of Helicteres gardneriana and imply that inhibition of leukocyte-endothelial interactions is important in the extract's mechanism of action.

  5. Inhibitory effects of 3-bromopyruvate in human nasopharyngeal carcinoma cells.

    Science.gov (United States)

    Zou, Xue; Zhang, Mengxiao; Sun, Yiming; Zhao, Surong; Wei, Yingmei; Zhang, Xudong; Jiang, Chenchen; Liu, Hao

    2015-10-01

    Tumor cells depend on aerobic glycolysis for adenosine triphosphate (ATP) production, which is therefore targeted by therapeutic agents. The compound 3-bromopyruvate (3-BrPA), a strong alkylating agent and hexokinase inhibitor, inhibits tumor cell glycolysis and the production of ATP, causing apoptosis. 3-BrPA induces apoptosis of nasopharyngeal carcinoma (NPC) cell lines HNE1 and CNE-2Z, which may be related to its molecular mechanisms. In the present study, we investigated the effects of 3-BrPA on the viability, reactive oxygen species (ROS), apoptosis and other types of programmed cell death in NPC cells in vitro and in vivo. PI staining showed significant apoptosis in NPC cells accompanied by the overproduction of ROS and downregulation of mitochondrial membrane potential (MMP, ΔΨm) by 3-BrPA. However, the ROS scavenger N-acetyl-L-cysteine (NAC) significantly reduced 3-BrPA-induced apoptosis by decreasing ROS and facilitating the recovery of MMP. We elucidated the molecular mechanisms underlying 3-BrPA activity and found that it caused mitochondrial dysfunction and ROS production, leading to necroptosis of NPC cells. We investigated the effects of the caspase inhibitor z-VAD-fmk, which inhibits apoptosis but promotes death domain receptor (DR)-induced NPC cell necrosis. Necrostatin-1 (Nec-1) inhibits necroptosis, apparently via a DR signaling pathway and thus abrogates the effects of z-VAD‑fmk. In addition, we demonstrated the effective attenuation of 3-BrPA-induced necrotic cell death by Nec-1. Finally, animal studies proved that 3-BrPA exhibited significant antitumor activity in nude mice. The present study is the first demonstration of 3-BrPA-induced non-apoptotic necroptosis and ROS generation in NPC cells and provides potential strategies for developing agents against apoptosis‑resistant cancers.

  6. Deflections of Nanowires with Consideration of Surface Effects

    Institute of Scientific and Technical Information of China (English)

    LI He; YANG Zhou; ZHANG Yi-Min; WEN Bang-Chun

    2010-01-01

    @@ The elementary beam model is modified to include the surface effects and used to analyze the deflections of nanowires under different boundary conditions.The results show that compared to deflections of nanowires without consideration of surface effects,the surface effects can enlarge or reduce deflections of nanowires,and nanowire buckling occurs under certaJn conditions.This study might be helpful for design of nanowire-based nanoelectromechanical systems.

  7. Inhibitory Effects of Soyeum Pharmacopuncture (SPP on LPS-induced Inflammation Related Cytokine Expressions of RAW 264.7 cells

    Directory of Open Access Journals (Sweden)

    Yoon Mi-Young

    2007-12-01

    Full Text Available Aim : This study was done to investigate whether SPP has inhibitory effects on the activation of RAW 264.7 cells. Method : In tumor necrosis factor-a (TNF-a/ interleukin-1b (IL-1b and IL-6, the mRNA expression of molecular indicators related to inflammatory changes of the Reumatoid Arthritis (RA were examined using quantitative real-time PCR. Results : The treatment of SPP significantly suppressed the expression of proinflammatory cytokines and chemokines such as TNF-a, IL-1b, IL-6 compared with the control. The expression of NOS-II was considerably reduced, which was accompanied by a reduction in the production of nitric oxide (NO. It also reduced the expression of TNF-αin serum of Balb/c mice compared with control group. Conclusion : SPP is an effective herbal material for suppressing the inflammation related cytokines of RAW 264.7 cells.

  8. Inhibitory effects of the macrolide antimicrobial tylosin on anaerobic treatment.

    Science.gov (United States)

    Shimada, Toshio; Zilles, Julie L; Morgenroth, Eberhard; Raskin, Lutgarde

    2008-09-01

    A laboratory-scale anaerobic sequencing batch reactor (ASBR) was operated using a glucose-based synthetic wastewater to study the effects of tylosin, a macrolide antimicrobial commonly used in swine production, on treatment performance. The experimental period was divided into three consecutive phases with different influent tylosin concentrations (0, 1.67, and 167 mg/L). The addition of 1.67 mg/L tylosin to the reactor had negligible effects on the overall treatment performance, that is, total methane production and effluent chemical oxygen demand did not change significantly (P tylosin was added. The addition of 167 mg/L tylosin to the reactor resulted in a gradual decrease in methane production and the accumulation of propionate and acetate. Subsequent inhibition of methanogenesis was attributed to a decrease in the pH of the reactor. After the addition of 167 mg/L tylosin to the reactor, an initial decrease in the rate of glucose uptake during the ASBR cycle followed by a gradual recovery was observed. In batch tests, the specific biogas production with the substrate butyrate was completely inhibited in the presence of tylosin. This study indicated that tylosin inhibited propionate- and butyrate-oxidizing syntrophic bacteria and fermenting bacteria resulting in unfavorable effects on methanogenesis.

  9. Telomerase inhibitory effects of medicinal mushrooms and lichens, and their anticancer activity.

    Science.gov (United States)

    Xu, Baojun; Li, Chantian; Sung, Changkeun

    2014-01-01

    Telomerase has been widely accepted as a cancer marker and a promising therapeutic target for novel anticancer drugs. The aim of this study was to investigate the in vitro telomerase inhibitory effects of mushrooms and their anticancer properties. The inhibitory effects of mushrooms and lichens against telomerase activity of HL-60 cells were systematically assessed using polymerase chain reaction based on assay of telomeric repeat amplification protocol. Telomerase inhibitory samples were further tested for antiproliferation effects against the gastric cell line SNU-1 using the MTT method. Ethyl acetate extract of Pleurotus ostreatus, ethyl acetate and water extracts of Lasiosphaera fenzlii, hexane extract of Strobilomyces floccopus, water extract of Sarcodon aspratus, and hexane, ethyl acetate, and water extracts from Umbilicaria esculenta showed strong positive telomerase inhibitory activity. Hexane extract of S. floccopus and water extracts from the edible lichen U. esculenta exhibited strong anticancer effects against SNU-1 cells through antiproliferation assay. The water extract of U. esculenta has a great potential to be developed into an anticancer agent that targets telomerase.

  10. Selective Attention and Inhibitory Deficits in ADHD: Does Subtype or Comorbidity Modulate Negative Priming Effects?

    Science.gov (United States)

    Pritchard, Verena E.; Neumann, Ewald; Rucklidge, Julia J.

    2008-01-01

    Selective attention has durable consequences for behavior and neural activation. Negative priming (NP) effects are assumed to reflect a critical inhibitory component of selective attention. The performance of adolescents with Attention Deficit/Hyperactivity Disorder (ADHD) was assessed across two conceptually based NP tasks within a selective…

  11. The effect of aging on fronto-striatal reactive and proactive inhibitory control

    NARCIS (Netherlands)

    Kleerekooper, I.; van Rooij, S.J.H; van den Wildenberg, W.P.M.; de Leeuw, M.; Kahn, R.S.; Vink, M.

    2016-01-01

    Inhibitory control, like most cognitive processes, is subject to an age-related decline. The effect of age on neurofunctional inhibition processing remains uncertain, with age-related increases as well as decreases in activation being reported. This is possibly because reactive (i.e., outright stopp

  12. α-Amylase and α-glucosidase inhibitory effects of Sclerocarya birrea ...

    African Journals Online (AJOL)

    ajl yemi

    2011-10-26

    Oct 26, 2011 ... stem-bark extracts. Mogale, M. A1, Lebelo, S. L.1, Thovhogi, N1, de Freitas A. N.1 and Shai, L. J2* ... hyperglycemia associated with type 2 diabetes mellitus. In vitro inhibitory ... gastrointestinal carbohydrate hydrolyzing enzymes such ..... low inhibition of α-amylase could be potentially used as an effective ...

  13. Inhibitory effects of propofol on excitatory synaptic transmission in supraoptic nucleus neurons in vitro.

    Science.gov (United States)

    Zhang, Huan-Huan; Zheng, Chao; Wang, Bang-An; Wang, Meng-Ya

    2015-12-25

    The present study was designed to investigate the inhibitory effects of intravenous general anesthetic propofol (0.1-3.0 mmol/L) on excitatory synaptic transmission in supraoptic nucleus (SON) neurons of rats, and to explore the underlying mechanisms by using intracellular recording technique and hypothalamic slice preparation. It was observed that stimulation of the dorsolateral region of SON could elicit the postsynaptic potentials (PSPs) in SON neurons. Of the 8 tested SON neurons, the PSPs of 7 (88%, 7/8) neurons were decreased by propofol in a concentration-dependent manner, in terms of the PSPs' amplitude (P EPSPs) of 7 cells increased in the condition of picrotoxin (30 µmol/L, a GABA(A) receptor antagonist) pretreatment. On this basis, the inhibitory effects of propofol on EPSPs were decreased. These data indicate that the presynaptic and postsynaptic mechanisms may be both involved in the inhibitory effects of propofol on excitatory synaptic transmission in SON neurons. The inhibitory effects of propofol on excitatory synaptic transmission of SON neurons may be related to the activation of GABA(A) receptors, but at a high concentration, propofol may also act directly on glutamate receptors.

  14. INHIBITORY EFFECTS OF VOLATILE ORGANIC COMPOUNDS ON NEURONAL NICOTINIC ACETYLCHOLINE RECEPTORS.

    Science.gov (United States)

    INHIBITORY EFFECTS OF VOLATILE ORGANIC COMPOUNDS ON NEURONAL NICOTINIC ACETYLCHOLINE RECEPTORS. A.S. Bale*; P.J. Bushnell; C.A. Meacham; T.J. Shafer Neurotoxicology Division, NHEERL, ORD, US Environmental Protection Agency, Research Triangle Park, NC, USA Toluene (TOL...

  15. Inhibitory Effect of Lactobacillus reuteri on Some Pathogenic Bacteria Isolated From Women With Bacterial Vaginosis

    OpenAIRE

    Eslami; Karimiravesh; Taheri; Azargashb

    2014-01-01

    Background Considering the high prevalence of bacterial vaginosis and its association with urinary tract infection in women and treatment of gynecologic problems occur when a high recurrence of bacterial vaginosis is often treated with antibiotics. Objectives The purpose of this study was to investigate the inhibitory effect of Lactobacillus reuteri on pathogenic bacteria isolated from women with bacterial vaginosis. ...

  16. Enzyme inhibitory and radical scavenging effects of some antidiabetic plants of Turkey

    Directory of Open Access Journals (Sweden)

    Nilüfer Orhan

    2014-06-01

    Full Text Available Objective(s:Ethnopharmacological field surveys demonstrated that many plants, such as Gentiana olivieri, Helichrysum graveolens, Helichrysum plicatum ssp. plicatum, Juniperus oxycedrus ssp. oxycedrus, Juniperus  communis var. saxatilis, Viscum album (ssp. album, ssp. austriacum, are used as traditional medicine for diabetes in different regions of Anatolia. The present study was designed to evaluate the in vitro antidiabetic effects of some selected plants, tested in animal models recently. Materials and Methods: α-glucosidase and α-amylase enzyme inhibitory effects of the plant extracts were investigated and Acarbose was used as a reference drug. Additionally, radical scavenging capacities were determined using 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid ABTS radical cation scavenging assay and total phenolic content of the extracts were evaluated using Folin Ciocalteu method. Results: H. graveolens ethanol extract exhibited the highest inhibitory activity (55.7 % ± 2.2 on α-amylase enzyme. Additionally, J. oxycedrus hydro-alcoholic leaf extract had potent α-amylase inhibitory effect, while the hydro-alcoholic extract of J. communis fruit showed the highest α-glucosidase inhibitory activity (IC50: 4.4 μg/ml. Conclusion:Results indicated that, antidiabetic effect of hydro-alcoholic extracts of H. graveolens capitulums, J. communis fruit and J. oxycedrus leaf might arise from inhibition of digestive enzymes.

  17. Inhibitory Effect of Cantharidin on Proliferation of A549 Cells

    Institute of Scientific and Technical Information of China (English)

    WANG Xiao-hua; YIN Yuan-qin; SUI Cheng-guang; MENG Fan-dong; MA Ping; JIANG You-hong

    2007-01-01

    Objective: To study the inhibition of Cantharidin against the proliferation of human lung cancer A549 cells and its mechanism. Methods: MTT assay was employed to determine the inhibition of Cantharidin against proliferation of A549 cells and flow Cytometry was applied to analyze A549 cell cycle and the effect of Cantharidin on cell cycle. Results: Cantharidin showed inhibition against the proliferation of A549 cells, and the inhibition was mediated by blocking A549 cell cycle at G2/M phase significantly. Conclusion: Cantharidin exhibits inhibition against the proliferation of human lung cancer A549 cells.

  18. Inhibitory effects of beryllium chloride on rat liver microsomal enzymes.

    Science.gov (United States)

    Teixeira, C F; Yasaka, W J; Silva, L F; Oshiro, T T; Oga, S

    1990-04-30

    A single i.v. dose (0.1 mmol Be2+/kg) of beryllium chloride prolonged the duration of pentobarbital-induced sleep and zoxazolamine-induced paralysis, in rats. The effects are correlated with changes of the pharmacokinetic parameters and with the in vitro inhibition of both aliphatic and aromatic hydroxylation of pentobarbital and zoxazolamine. In vitro N-demethylation of meperidine and aminopyrine was partially inhibited while O-demethylation of quinidine was unaffected by liver microsomes of rats pretreated with beryllium salt. The findings give clues that beryllium chloride inhibits some forms of cytochrome P-450, especially those responsible for hydroxylation of substrates, like pentobarbital and zoxazolamine.

  19. Inhibitory effect of Patrinia scabiosaefolia on acute pancreatitis

    Institute of Scientific and Technical Information of China (English)

    Sang-Wan Seo; Hyung-Min Kim; Sung-Joo Park; Cheung-Seog Park; Seung-Heon Hong; Kang-Beom Kwon; Hyoung-Chul Moon; Bong-keun Song; Kyung-Yo Kim; Young-Min Park; Ho-Joon Song

    2006-01-01

    AIM: To investigate the effect of Patrinia scabiosaefolia (PS) on the cholecystokinin (CCK) octapeptide- induced acute pancreatitis (AP) in rats.METHODS: Wistar rats weighing 240-260 g were divided into three groups: (1) Normal saline-treated group;(2) treatment with PS at 100 mg/kg group, in which PS was administered orally, followed by subcutaneous administration of 75 μg/kg CCK octapeptide three times after 1, 3 and 5 h, and this whole procedure was repeated for 5 d; (3) treatment with saline group,in which the protocols were the same as in treatment group with PS. We determined the pancreatic weight/body weight ratio, the levels of pancreatic HSP60,HSP72 and the secretion of pro-inflammatory cytokines.Repeated CCK octapeptide treatment resulted in the typical laboratory findings of experimentally induced pancreatitis.RESULTS: PS reduced the pancreatic weight/body weight ratio, the levels of serum amylase and lipase,and inhibited expressions of pro-inflammatory cytokines in the CCK octapeptide-induced AP. Furthermore, PS pretreatment increased the pancreatic levels of HSP60and HSP72.CONCLUSION: Pretreatment with PS has an antiinflammatory effect on CCK octapeptide-induced AP.

  20. The inhibitory effect of calcium on Cylindrospermopsis raciborskii (cyanobacteria metabolism

    Directory of Open Access Journals (Sweden)

    Ronaldo Leal Carneiro

    2011-12-01

    Full Text Available Cylindrospermopsis raciborskii (Woloszynska Seenaya & Subba Raju is a freshwater cyanobacterium of worldwide distribution. In the North-eastern region of Brazil many eutrophic water reservoirs are characterized by the dominance of C. raciborskii, with recurrent occurrence of blooms. These water bodies have high conductivity due to a high ionic concentration, and are defined as hard (with high values of CaCO3. In this study, we investigated the long-term effect (12 days of high calcium concentration (8 mM Ca2+ on C. raciborskii (T3 strain growth, morphology, toxin content, and metabolism. Changes in protein expression profiles were investigated by proteomic analysis using 2D gel electrophoresis and mass spectrometry. A continued exposure to calcium had a pronounced effect on C. raciborskii (T3: it limited growth, decreased thricome length, increased chlorophyll-a content, altered toxin profile (although did not affect PST content, saxitoxin + neosaxitoxin, and inhibited the expression of proteins related to primary metabolism.

  1. The inhibitory effect of propofol on bovine lactoperoxidase.

    Science.gov (United States)

    Sişecioğlu, Melda; Cankaya, Murat; Gülçin, Ilhami; Ozdemir, Hasan

    2009-01-01

    Propofol (2,6-diisopropylphenol) is a hypnotic intravenous agent with in vivo antioxidant properties. This study was undertaken to examine the in vitro effect of propofol on lactoperoxidase (LPO; E.C. 1.11.1.7) obtained from bovine milk. Lactoperoxidase was purified with three purification steps: Amberlite CG-50 resin, CM-Sephadex C-50 ion-exchange chromatography and Sephadex G-100 gel filtration chromatography, respectively. Lactoperoxidase was purified with a yield of 21.6%, a specific activity of 34 EU/mg proteins and 14.7-fold purification. One enzyme unit is defined as the oxidation of 1 micromol ABTS per min under the assay condition (25( degrees )C, pH: 6.0). To determine enzyme purity, sodium dodecyl sulphate-polyacrylamide gel electrophoresis (SDS-PAGE) was performed and single band was observed. The effect of propofol on lactoperoxidase were determined using 2,2'-azino-bis (3-ethylbenzthiazoline-6 sulfonic acid) diammonium salt (ABTS) as a chromogenic substrate. The IC(50) value of propofol was found as 15.97 microM. Also, K(i) constant for propofol was 3.72 microM and propofol was found as competitive inhibitor.

  2. Dual inhibitory effect of Glycyrrhiza glabra (GutGard™) on COX and LOX products.

    Science.gov (United States)

    Chandrasekaran, C V; Deepak, H B; Thiyagarajan, P; Kathiresan, S; Sangli, Gopal Krishna; Deepak, M; Agarwal, Amit

    2011-02-15

    Glycyrrhiza glabra and its phytoconstituents have been known to possess widespread pharmacological properties as an anti-inflammatory, anti-viral, antitumour and hepatoprotective drug. In this study, we examined the inhibitory potential of extract of G. glabra (GutGard™) root and its phytoconstituents (glabridin, glycyrrhizin, and isoliquiritigenin) on both cyclooxygenase (COX) and lipoxygenase (LOX) products in order to understand the mechanism of its anti-inflammatory action. Inhibitory effect of GutGard™ and its phytoconstituents on lipopolysaccharide (LPS) induced prostaglandin E(2) (PGE(2)), calcimycin (A23187) induced thromboxane (TXB(2)), and leukotriene (LTB(4)) release was studied using murine macrophages (J774A.1) and human neutrophil (HL-60) cells. Results revealed that, G. glabra and glabridin significantly inhibited PGE(2), TXB(2) (COX) and LTB(4) (LOX), while, isoliquiritigenin exerted inhibitory effect only against COX products but failed to suppress LOX product. However, glycyrrhizin at the tested concentrations failed to exhibit inhibitory effect on both COX and LOX products. Here, we report for the first time that G. glabra (almost devoid of glycyrrhizin) exhibits anti-inflammatory property likely through the inhibition of PGE(2), TXB(2) and LTB(4) in mammalian cell assay system, which could be influenced in part by glabridin and isoliquiritigenin.

  3. THE INHIBITORY EFFECT OF MELATONIN ON THE GROWTH OF HUMAN BLADDER CARCINOMA T24 CELL LINE

    Institute of Scientific and Technical Information of China (English)

    白艳红; 慕慧; 赵晏; 蔡晓宏; 王中秋; 郭瑗

    2004-01-01

    Objective To study the inhibitory effects of melatonin and its inhibitory mechanism on the growth of human bladder carcinoma T24. Methods The inhibitory effects of melatonin with various concentrations on the human bladder carcinoma T24 lines in vitro were determined by MTT assay. The mechanism of the inhibition was observed by flow cytometry (FCM) and transmission electron microscopy (TEM). Results The 30% inhibition concentration (IC30) value was 0.71mmol·L-1 and the 50% inhibition concentration (IC50) value was 1.20mmol·L-1. The population doubling time of T24 cells treated with melatonin at 0.71mmol·L-1 was 43.2 hours, which was significant different from that of 34.6 hours of the control group. Using FCM, we found that the cell percentage increased during the G1 phase, but decreased during the S stage. The degenerated ultra-structure of the cell treated with melatonin was also observed by TEM. Conclusion The results suggest that melatonin can inhibit the growth of human bladder carcinoma T24. The inhibitory effects of melatonin might be the prolonging of the staging from G1 to S in the cell cycle.

  4. Alpha-glucosidase inhibitory effect and inorganic constituents of Phyllanthus amarus Schum. & Thonn. ash

    Directory of Open Access Journals (Sweden)

    Malinee Wongnawa

    2014-10-01

    Full Text Available This study investigated the -glucosidase inhibitory effect and determined the concentration of some inorganic constituents in P. amarus ash. Oral glucose and sucrose tolerance test were performed on normal mice. In vitro -glucosidase inhibitory activity was evaluated by using yeast a-glucosidase. The element concentrations were measured by inductively coupled plasma (ICP spectroscopy. Single oral administration of P. amarus ash did not show antihyperglycemic effect after glucose administration, but decreased blood glucose level after sucrose administration. The ash showed -glucosidase inhibitory activity in vitro with IC50 of 982 mg/mL. The concentrations of K, Ca, Mg, Mn, Fe, Zn, Cu, Pb, Cr, Ni and Co in P. amarus ash were 35049.80±340.64, 3337.24±52.10, 1368.52±13.29, 90.81±1.34, 87.68±1.15, 18.28±0.22, 4.69±0.07, 1.07±0.15, 0.29±0.03, 0.20±0.04 and 0.10±0.02 mg/g, respectively. These results indicate that the antihyperglycemic effect of P. amarus ash might be partly due to the -glucosidase inhibitory activity of the inorganic constituents.

  5. Algal testing of titanium dioxide nanoparticles - Testing considerations, inhibitory effects and modification of cadmium bioavailability

    DEFF Research Database (Denmark)

    Hartmann, Nanna Isabella Bloch; von der Kammer, F.; Hofmann, T.

    2010-01-01

    The ecotoxicity of three different sizes of titanium dioxide (TiO(2)) particles (primary particles sizes: 10, 30, and 300 nm) to the freshwater green alga Pseudokirchneriella subcapitata was investigated in this study. Algal growth inhibition was found for all three particle types...... surfaces. It is also believed that heteroaggregation, driven by algal exopolymeric exudates, is occurring and could influence the concentration-response relationship. The ecotoxicity of cadmium to algae was investigated both in the presence and absence of 2 mg/LTiO(2). The presence of TiO(2) in algal tests...

  6. Inhibitory effects of antibiofilm compound 1 against Staphylococcus aureus biofilms.

    Science.gov (United States)

    Shrestha, Looniva; Kayama, Shizuo; Sasaki, Michiko; Kato, Fuminori; Hisatsune, Junzo; Tsuruda, Keiko; Koizumi, Kazuhisa; Tatsukawa, Nobuyuki; Yu, Liansheng; Takeda, Kei; Sugai, Motoyuki

    2016-03-01

    A novel benzimidazole molecule that was identified in a small-molecule screen and is known as antibiofilm compound 1 (ABC-1) has been found to prevent bacterial biofilm formation by multiple bacterial pathogens, including Staphylococcus aureus, without affecting bacterial growth. Here, the biofilm inhibiting ability of 156 μM ABC-1 was tested in various biofilm-forming strains of S. aureus. It was demonstrated that ABC-1 inhibits biofilm formation by these strains at micromolar concentrations regardless of the strains' dependence on Polysaccharide Intercellular Adhesin (PIA), cell wall-associated protein dependent or cell wall- associated extracellular DNA (eDNA). Of note, ABC-1 treatment primarily inhibited Protein A (SpA) expression in all strains tested. spa gene disruption showed decreased biofilm formation; however, the mutants still produced more biofilm than ABC-1 treated strains, implying that ABC-1 affects not only SpA but also other factors. Indeed, ABC-1 also attenuated the accumulation of PIA and eDNA on cell surface. Our results suggest that ABC-1 has pleotropic effects on several biofilm components and thus inhibits biofilm formation by S. aureus.

  7. Inhibitory effect of chlorogenic acid on digestion of potato starch.

    Science.gov (United States)

    Karim, Zida; Holmes, Melvin; Orfila, Caroline

    2017-02-15

    The effect of the chlorogenic acid isomer 5-O-caffeoylquinic acid (5-CQA) on digestion of potato starch by porcine pancreatic alpha amylase (PPAA) was investigated using isolated starch and cooked potato tuber as substrates. In vitro digestion was performed on five varieties of potato with varying phenolic content. Co- and pre-incubation of PPAA with 5-CQA significantly reduced PPAA activity in a dose dependent manner with an IC50 value of about 2mgmL(-1). Lineweaver-Burk plots indicated that 5-CQA exerts a mixed type inhibition as km increased and Vmax decreased. The total polyphenol content (TPC) of peeled tuber tissue ranged from 320.59 to 528.94mg 100g(-1)dry weight (DW) in raw tubers and 282.03-543.96mg 100g(-1)DW in cooked tubers. With the exception of Désirée, TPC and 5-CQA levels decreased after cooking. Principle component analysis indicated that digestibility is affected by multiple factors including phenolic, dry matter and starch content.

  8. Inhibitory effects of cefotaxime on the activity of mushroom tyrosinase.

    Science.gov (United States)

    Hu, Yong-Hua; Zhuang, Jiang-Xing; Yu, Feng; Cui, Yi; Yu, Wen-Wen; Yan, Chong-Ling; Chen, Qing-Xi

    2016-04-01

    Tyrosinase (EC 1.14.18.1) catalyzes both the hydroxylation of tyrosine into o-diphenols and the oxidation of o-diphenols into o-quinones that form brown or black pigments. In the present paper, cefotaxime, a cephalosporin antibacterial drug, was tested as an inhibitor of tyrosinase. The results show that cefotaxime inhibits both the monophenolase and diphenolase activities of tyrosinase. For the monophenolase activity, cefotaxime increased the lag time and decreased the steady-state activity with an IC50 of 3.2 mM. For the diphenolase activity, the inhibition by cefotaxime is reversible and mix-I type with an IC50 of 0.14 mM. The inhibition constants (K(I) and K(IS)) were determined to be 0.14 and 0.36 mM, respectively. The molecular mechanism of inhibition of tyrosinase by cefotaxime was determined by fluorescence quenching and molecular docking. The results demonstrated that cefotaxime was a static quencher of tyrosinase and that cefotaxime could dock favorably in the active site of tyrosinase. This research may offer a lead for designing and synthesizing novel and effective tyrosinase inhibitors in the future.

  9. Inhibitory Effect of Bursa Propolis on Dental Caries Formation in Rats Inoculated with Streptococcus sobrinus

    OpenAIRE

    ERDEM, Gamze BOZCUK

    2004-01-01

    The effect of propolis on the growth of Lactobacillus casei RSKK 591, Streptococcus mutans NCTC 10449 and Streptococcus sobrinus DSN sobrinus 20742 was investigated in vitro. Bursa propolis had the most inhibitory effect on S. sobrinus. The effect of Bursa propolis on rats inoculated with S. sobrinus was also studied. In rats inoculated with the bacteria and given propolis, the severity of sulcal enamel and superficial dentine lesions was significantly less than that in the control group, but...

  10. Stimulatory and inhibitory effects of inorganic lead on calcineurin.

    Science.gov (United States)

    Kern, M; Audesirk, G

    2000-09-07

    Calcineurin is a phosphatase with activity dependent on both Ca(2+)/calmodulin binding to the catalytic A subunit and Ca(2+) binding to the regulatory B subunit. We have previously shown that Pb(2+) activates calmodulin with a threshold of about 100 pM free Pb(2+), and that Pb(2+) and Ca(2+) are roughly additive in calmodulin activation (Kern et al., NeuroToxicology 21, 353-364 (2000)). In the present study, we evaluated the effects of Pb(2+), with and without Ca(2+) and calmodulin, on calcineurin activity. In calmodulin-containing, Ca(2+)-free solutions, Pb(2+) activated calcineurin with a threshold of about 100 pM free Pb(2+). Maximum calcineurin activity (comparable to that induced by 10 microM Ca(2+)) was reached at about 200 pM free Pb(2+). Higher Pb(2+) concentrations reduced activity, although some activity remained even at 2000 pM free Pb(2+). Combined with subsaturating Ca(2+) concentrations, as little as 20 pM free Pb(2+) enhanced calcineurin activity, but free Pb(2+) concentrations greater than 200 pM still reduced activity below maximum. Extremely high Ca(2+) concentrations (10 microM) completely reversed the inhibition of activity by 2000 pM free Pb(2+). In the absence of calmodulin, Ca(2+) slightly stimulated calcineurin activity. Pb(2+) did not substitute for Ca(2+) in calmodulin-free activation; in fact, high concentrations of Pb(2+) inhibited Ca(2+)-mediated activation. We tentatively conclude that low concentrations of free Pb(2+) activate calcineurin by activating calmodulin. Higher concentrations reduce calcineurin activity, perhaps by binding to the B subunit.

  11. The inhibitory effect of selenium nanoparticles on protein glycation in vitro

    Science.gov (United States)

    Yu, Shaoxuan; Zhang, Wentao; Liu, Wei; Zhu, Wenxin; Guo, Ruochen; Wang, Yashan; Zhang, Daohong; Wang, Jianlong

    2015-04-01

    Selenium nanoparticles (Se NPs) possess well-known excellent biological activities and low toxicity, and have been employed for numerous applications except as inhibitors to protein glycation. Herein, the present study is carried out to investigate the inhibitory effect of Se NPs on protein glycation in a bovine serum albumin (BSA)/glucose system. By measuring the amount of glucose covalently bound onto BSA, the formation of fructosamine and fluorescent products, it is found that Se NPs can hinder the development of protein glycation in a dose-dependent but time-independent manner under the selected reaction conditions (55 °C, 40 h). And after comparing the increase of inhibitory rate in different stages, it is observed that Se NPs show the greatest inhibitory effect in the early stage, then in the advanced stage, but no effect in the intermediate stage. Fourier transform infrared spectroscopy characterization of Se NPs collected after glycation and determination of ·OH influence and glyoxal formation show that the mechanism for the inhibitory efficacy of Se NPs is related to their strong competitive activity against available amino groups in proteins, their great scavenging activity on reactive oxygen species and their inhibitory effect on α-dicarbonyl compounds’ formation. In addition, it is proved that Se NPs protect proteins from structural modifications in the system and they do not exhibit significant cytotoxicity towards BV-2 and BRL-3A cells at low concentrations (10 and 50 μg mL-1). Consequently, Se NPs may be suitable for further in vivo studies as novel anti-glycation agents.

  12. Inhibitory effect of Ca2+ on in vivo gene transfer by electroporation

    Institute of Scientific and Technical Information of China (English)

    Yong-gang ZHAO; Hui-li LU; Jin-liang PENG; Yu-hong XU

    2006-01-01

    Aim:To investigate the specific effects of Ca2+ on transgene expression during electroporation-mediated gene transfer in mice.Methods:Skeletal muscle and skin were subjected to in vivo electroporation with a luciferase reporter plasmid,with or Without Ca2+ and various other ions.Resuits:For in vivo electroporation,the presence of just 10 mmol/L Ca2+ in the DNA solution drastically reduced the resulting transgene expression,to less than 5% of control values.Only Ca2+,not other ions,caused inhibition,and the effect was not tissue specific.More surprisingly.even when Ca2+ ions were delivered by electroporation before or after DNA administration,similar effects were still observed.Conelusion:The inhibitory effect of Ca2+ on in vivo gene transfer by electroporation is specific,ie,the inhibitory effect may be related to the cell membrane properties after electroporation and the subsequent resealing event.

  13. Environmental effects consideration: A case study - Lessons learned

    Science.gov (United States)

    Vaughan, William W.; Anderson, B. J.

    1992-01-01

    This paper discusses the importance for serious consideration of environmental effects and associated risks by management early in the development cycle of a facility. A case study on the Space Shuttle provides information with regard to some of the environmental effects issues encountered and the lesson learned. The importance of early management action to enable the acceptance of known environmental risks, or to make program adjustments to avoid their potential consequences, is emphasized.

  14. [Experimental study of the inhibitory effects of Chelidonium majus L. extractive on Streptococcus mutans in vitro].

    Science.gov (United States)

    Cheng, Rui-bo; Chen, Xu; Liu, Shu-jie; Zhang, Xiao-fang; Zhang, Guang-he

    2006-06-01

    To study the inhibitory effects of Chelidonium majus L. extractive on the growth of Streptococcus mutans in vitro, and to explore its mechanism in caries prevention. Streptococcus mutans 25175 was chosen as the experimental bacterium. The Chelidonium majus L. extractives chelidonine and chelerythrine were double diluted to different concentrations by two-fold dilution. The inhibitory effect of Streptococcus mutans was measured by slip diffusion method. The minimal inhibitory concentration(MIC) was also determined. 0.16% liquor hibitane was used as positive control. Spearman correlation was used for statistical analysis. Inhibition zone of Streptococcus mutans appeared in some concentration of chelerythrine, but no inhibition zone in each concentration of chelidonine. The MIC of chelerythrine was 0.78 mg/ml which determined by liquid culture medium. The concentration of chelerythrine was highly related to the inhibitory zone of Streptococcus mutans (r=0.99, PChelidonium majus L. extractive chelerythrine on Streptococcus mutans was significant,and the antibacterial activity of the concentration 100 mg/ml was higher than that of 0.16% liquor hibitane (19.4 mm), indicating that chelerythrine can be used as an agent for prevention of dental caries.

  15. Effect of sugar positions in ginsenosides and their inhibitory potency on Na+/K+-ATPase activity

    Institute of Scientific and Technical Information of China (English)

    Ronald JY CHEN; Tse-yu CHUNG; Feng-yin LI; Nan-hei LIN; Jason TC TZEN

    2009-01-01

    Aim: To determine whether ginsenosides with various sugar attachments may act as active components responsible for the cardiac therapeutic effects of ginseng and sanqi (the roots of Panax ginseng and Panax notoginseng) via the same molecular mechanism triggered by cardiac glycosides, such as ouabain and digoxin. Methods: The structural similarity between ginsenosides and ouabain was analyzed. The inhibitory potency of ginseno-sides and ouabain on Na+/K+-ATPase activity was examined and compared. Molecular modeling was exhibited for the docking of ginsenosides to Na+/K+-ATPase. Results: Ginsenosides with sugar moieties attached only to the C-3 position of the steroid-like structure, equivalent to the sugar position in cardiac glycosides, and possessed inhibitory potency on Na+/K+-ATPase activity. However, their inhibi-tory potency was significantly reduced or completely abolished when a monosaccharide was linked to the C-6 or C-20 posi-tion of the steroid-like structure; replacement of the monosaccharide with a disaccharide molecule at either of these posi-tions caused the disappearance of the inhibitory potency. Molecular modeling and docking confirmed that the difference in Na+/K+-ATPase inhibitory potency among ginsenosides was due to the steric hindrance of sugar attachment at the C-6 and C-20 positions of the steroid-like structure. Conclusion: The cardiac therapeutic effects of ginseng and sanqi should be at least partly attributed to the effective inhi-bition of Na+/K+-ATPase by their metabolized ginsenosides with sugar moieties attached only to the C-3 position of the steroid-like structure.

  16. Effects of essential oils from herbal plants and citrus fruits on DNA polymerase inhibitory, cancer cell growth inhibitory, antiallergic, and antioxidant activities.

    Science.gov (United States)

    Mitoshi, Mai; Kuriyama, Isoko; Nakayama, Hiroto; Miyazato, Hironari; Sugimoto, Keiichiro; Kobayashi, Yuko; Jippo, Tomoko; Kanazawa, Kazuki; Yoshida, Hiromi; Mizushina, Yoshiyuki

    2012-11-14

    In this study, the biological activity of 20 essential oils (EOs) from herbal plants and citrus fruits were investigated in terms of mammalian DNA polymerase (pol) inhibitory activity, cancer cell (human colon carcinoma, HCT116) growth inhibitory activity, antiallergic activity, as anti-β-hexosaminidase release activity in rat basophilic leukemia RBL-2H3 cells treated with calcium ionophore A23187, and antioxidant activity by a lipophilic-oxygen radical absorbance capacity method. These EOs showed patterns of inhibition of pol α, a DNA replicative pol, similar to their cancer cell growth inhibitory activity, and their inhibitory activity on pol λ, a DNA repair/recombination pol, by the EOs showed correlation with anti-β-hexosaminidase release activity. Among these EOs, chamomile (Matricaria chamomilla L.) was the strongest inhibitor of pols α and λ and showed significant effects on both cancer cell growth and mast cell degranulation. On the basis of these results, chamomile EO can be recommended as a potentially useful, bioactive candidate for therapeutic applications.

  17. The growth inhibitory effects of cadmium and copper on the MDA-MB468 human breast cancer cells

    Directory of Open Access Journals (Sweden)

    Mojtaba Panjehpour

    2010-01-01

    Full Text Available Background: Cadmium chloride is an important occupational and environmental pollutant. However, it can also be anti-carcinogenic under certain conditions. Copper, an essential trace element, has the ability to generate reactive oxygen species and induce cell apoptosis. This study was aimed to determine the growth inhibitory effects of cadmium and copper on the MDA-MB468 human breast cancer cells. Methods: By using MTT cell viability test, treatment of monolayer cell cultures with different metal concentrations (1-1000 μM showed a significant dose dependent decrease (p < 0.05 of viable cells in different times. Results: A considerable cytotoxicity was observed for CdCl2 at 200 μM and 1 μM after 48 and 72 hours incubations, respectively. The highest concentration of CuCl2 (1000 μM had little cytotoxic effects after 48 hours incubation period, but 1 μM of CuCl2 revealed a considerable cytotoxicity after 72 hours. The maximum synergic cytotoxic effect was observed at 0.5 μM of both metals. Conclusions: The results of the present study indicate that cytotoxic effect of CuCl2 is somehow lesser than that of CdCl2. This may be due to vital role of copper which is not known for cadmium so far.

  18. The neural basis of inhibitory effects of semantic and phonological neighbors in spoken word production.

    Science.gov (United States)

    Mirman, Daniel; Graziano, Kristen M

    2013-09-01

    Theories of word production and word recognition generally agree that multiple word candidates are activated during processing. The facilitative and inhibitory effects of these "lexical neighbors" have been studied extensively using behavioral methods and have spurred theoretical development in psycholinguistics, but relatively little is known about the neural basis of these effects and how lesions may affect them. This study used voxel-wise lesion overlap subtraction to examine semantic and phonological neighbor effects in spoken word production following left hemisphere stroke. Increased inhibitory effects of near semantic neighbors were associated with inferior frontal lobe lesions, suggesting impaired selection among strongly activated semantically related candidates. Increased inhibitory effects of phonological neighbors were associated with posterior superior temporal and inferior parietal lobe lesions. In combination with previous studies, these results suggest that such lesions cause phonological-to-lexical feedback to more strongly activate phonologically related lexical candidates. The comparison of semantic and phonological neighbor effects and how they are affected by left hemisphere lesions provides new insights into the cognitive dynamics and neural basis of phonological, semantic, and cognitive control processes in spoken word production.

  19. Essential Oils from Ugandan Aromatic Medicinal Plants: Chemical Composition and Growth Inhibitory Effects on Oral Pathogens.

    Science.gov (United States)

    Ocheng, Francis; Bwanga, Freddie; Joloba, Moses; Softrata, Abier; Azeem, Muhammad; Pütsep, Katrin; Borg-Karlson, Anna-Karin; Obua, Celestino; Gustafsson, Anders

    2015-01-01

    The study assessed the growth inhibitory effects of essential oils extracted from ten Ugandan medicinal plants (Bidens pilosa, Helichrysum odoratissimum, Vernonia amygdalina, Hoslundia opposita, Ocimum gratissimum, Cymbopogon citratus, Cymbopogon nardus, Teclea nobilis, Zanthoxylum chalybeum, and Lantana trifolia) used traditionally in the management of oral diseases against oral pathogens. Chemical compositions of the oils were explored by GC-MS. Inhibitory effects of the oils were assessed on periodontopathic Porphyromonas gingivalis and Aggregatibacter actinomycetemcomitans and cariogenic Streptococcus mutans and Lactobacillus acidophilus using broth dilution methods at concentrations of 1%, 0.1%, and 0.01%. The most sensitive organism was A. actinomycetemcomitans. Its growth was markedly inhibited by six of the oils at all the concentrations tested. Essential oil from C. nardus exhibited the highest activity with complete growth inhibition of A. actinomycetemcomitans and P. gingivalis at all the three concentrations tested, the major constituents in the oil being mainly oxygenated sesquiterpenes. Most of the oils exhibited limited effects on L. acidophilus. We conclude that essential oils from the studied plants show marked growth inhibitory effects on periodontopathic A. actinomycetemcomitans and P. gingivalis, moderate effects on cariogenic S. mutans, and the least effect on L. acidophilus. The present study constitutes a basis for further investigations and development of certain oils into alternative antiplaque agents.

  20. Essential Oils from Ugandan Aromatic Medicinal Plants: Chemical Composition and Growth Inhibitory Effects on Oral Pathogens

    Directory of Open Access Journals (Sweden)

    Francis Ocheng

    2015-01-01

    Full Text Available The study assessed the growth inhibitory effects of essential oils extracted from ten Ugandan medicinal plants (Bidens pilosa, Helichrysum odoratissimum, Vernonia amygdalina, Hoslundia opposita, Ocimum gratissimum, Cymbopogon citratus, Cymbopogon nardus, Teclea nobilis, Zanthoxylum chalybeum, and Lantana trifolia used traditionally in the management of oral diseases against oral pathogens. Chemical compositions of the oils were explored by GC-MS. Inhibitory effects of the oils were assessed on periodontopathic Porphyromonas gingivalis and Aggregatibacter actinomycetemcomitans and cariogenic Streptococcus mutans and Lactobacillus acidophilus using broth dilution methods at concentrations of 1%, 0.1%, and 0.01%. The most sensitive organism was A. actinomycetemcomitans. Its growth was markedly inhibited by six of the oils at all the concentrations tested. Essential oil from C. nardus exhibited the highest activity with complete growth inhibition of A. actinomycetemcomitans and P. gingivalis at all the three concentrations tested, the major constituents in the oil being mainly oxygenated sesquiterpenes. Most of the oils exhibited limited effects on L. acidophilus. We conclude that essential oils from the studied plants show marked growth inhibitory effects on periodontopathic A. actinomycetemcomitans and P. gingivalis, moderate effects on cariogenic S. mutans, and the least effect on L. acidophilus. The present study constitutes a basis for further investigations and development of certain oils into alternative antiplaque agents.

  1. Inhibitory effects of xanthohumol from hops (Humulus lupulus L.) on human hepatocellular carcinoma cell lines.

    Science.gov (United States)

    Ho, Yi-Chien; Liu, Chi-Hsien; Chen, Chien-Nan; Duan, Kow-Jen; Lin, Ming-Tse

    2008-11-01

    Xanthohumol is one of the main flavonoids in hop extracts and in beer. Very few investigations of xanthohumol have studied hepatocellular carcinoma. In this study, the inhibitory effects of xanthohumol on human hepatocellular carcinoma cell lines were investigated. The IC(50) values of xanthohumol for two hepatocellular carcinoma cell lines and one normal hepatocyte cell line were 108, 166 and 211 microm, respectively. Normal murine hepatocyte cell line had more resistance to xanthohumol than hepatocellular carcinoma cell lines. Besides, the inhibitory effects of xanthohumol on human hepatocellular carcinoma cell lines were attributed to apoptosis as indicated in the results of flow cytometry, fluorescent nuclear staining and electrophoresis of oligonucleosomal DNA fragments. Hop xanthohumol was more efficient in the growth inhibition of hepatocellular carcinoma cell lines than the flavonoids silibinin and naringin from thistle and citrus. It was shown for the first time that xanthohumol from hops effectively inhibits proliferation of human hepatocellular carcinoma cells in vitro.

  2. Inhibitory effects of pepstatin A and mefloquine on the growth of Babesia parasites.

    Science.gov (United States)

    Munkhjargal, Tserendorj; AbouLaila, Mahmoud; Terkawi, Mohamad Alaa; Sivakumar, Thillaiampalam; Ichikawa, Madoka; Davaasuren, Batdorj; Nyamjargal, Tserendorj; Yokoyama, Naoaki; Igarashi, Ikuo

    2012-10-01

    We evaluated the inhibitory effects of pepstatin A and mefloquine on the in vitro and in vivo growths of Babesia parasites. The in vitro growth of Babesia bovis, B. bigemina, B. caballi, and B. equi was significantly inhibited (P mefloquine (50% inhibitory concentrations = 59.7, 56.7, 20.7, and 4 μM, respectively). Furthermore, both reagents either alone at a concentration of 5 mg/kg or in combinations (2.5/2.5 and 5/5 mg/kg) for 10 days significantly inhibited the in vivo growth of B. microti in mice. Mefloquine treatment was highly effective and the combination treatments were less effective than other treatments. Therefore, mefloquine may antagonize the actions of pepstatin A against babesiosis and aspartic proteases may play an important role in the asexual growth cycle of Babesia parasites.

  3. Inhibitory effects of Ruta graveolens L. extract on guinea pig liver aldehyde oxidase.

    Science.gov (United States)

    Pirouzpanah, Saieed; Saieed, Pirouzpanah; Rashidi, Mohammad Reza; Reza, Rashidi Mohammad; Delazar, Abbas; Abbas, Delazar; Razavieh, Seyyed-Vali; Seyyedvali, Razavieh; Hamidi, Aliasghar; Aliasghar, Hamidi

    2006-01-01

    Ruta graveolens L. is a flavonoid-containing medicinal plant with various biological properties. In the present study, the effects of R. graveolens extract on aldehyde oxidase, a molybdenum hydroxylase, are investigated. Aldehyde oxidase was partially purified from liver homogenates of mature male guinea pigs by heat treatment and ammonium sulphate precipitation. The total extract was obtained by macerating the aerial parts of R. graveolens in MeOH 70% and the effect of this extract on the enzyme activity was assayed using phenanthridine, vanillin and benzaldehyde as substrates. Quercetin and its glycoside form, rutin were isolated, purified and identified from the extract and their inhibitory effects on the enzyme were investigated. R. graveolens extract exhibited a high inhibition on aldehyde oxidase activity (89-96%) at 100 microg/ml which was comparable with 10 microM of menadione, a specific potent inhibitor of aldehyde oxidase. The IC50 values for the inhibitory effect of extract against the oxidation of benzaldehyde, vanillin and phenanthridine were 10.4, 10.1, 43.2 microg/ml, respectively. Both quercetin and rutin at 10 microM caused 70-96% and 27-52% inhibition on the enzyme activity, respectively. Quercetin was more potent inhibitor than rutin, but both flavonols exerted their inhibitory effects mostly in a linear mixed-type.

  4. Inhibitory Effect of Long-Chain Fatty Acids on Biogas Production and the Protective Effect of Membrane Bioreactor

    Science.gov (United States)

    Dasa, Kris Triwulan; Westman, Supansa Y.; Cahyanto, Muhammad Nur; Niklasson, Claes

    2016-01-01

    Anaerobic digestion of lipid-containing wastes for biogas production is often hampered by the inhibitory effect of long-chain fatty acids (LCFAs). In this study, the inhibitory effects of LCFAs (palmitic, stearic, and oleic acid) on biogas production as well as the protective effect of a membrane bioreactor (MBR) against LCFAs were examined in thermophilic batch digesters. The results showed that palmitic and oleic acid with concentrations of 3.0 and 4.5 g/L resulted in >50% inhibition on the biogas production, while stearic acid had an even stronger inhibitory effect. The encased cells in the MBR system were able to perform better in the presence of LCFAs. This system exhibited a significantly lower percentage of inhibition than the free cell system, not reaching over 50% at any LCFA concentration tested. PMID:27699172

  5. The effect of attention to distractor on inhibitory processes in selective attention

    Institute of Scientific and Technical Information of China (English)

    GENG Haiyan; SONG Qianlan; LI Yunfeng; ZHU Ying

    2005-01-01

    Selective attention has been viewed as a dualprocess mechanism, that is, exciting targets and inhibiting distractors. Most early studies concentrated mainly on the target-excitation, whereas recent investigations began to pay more attention to the inhibitory selective attention mechanism. A measure named negative priming (NP) was extensively employed to probe into the inhibitory processes. The Houghton and Tipper Model put forward a notion: the inhibition that feeds back to the distractor is reactive. That means, the level of inhibition is determined by the activation state of the distractor. Distractors that are more salient and intrude into the control of action receive greater inhibitory feedbacks than less salient distractors. Because increasing attention to an object would enhance the early processing of this object, we thus hypothesized that augmenting the level of attention to a distractor might lead to a higher level of inhibition, revealed as a corresponding augmentation in the magnitude of NP effect. To test this assumption, an object- based identification task was then applied, and participants were asked to make the animate/inanimate categorization. Attention level was manipulated by varying the relative spatial locations of target and distractor (overlapped or separated). A reliable greater NP effect was found in the overlapped than separated condition, indicating that distractors under the high-level attention condition (overlapped) got greater initial excitation, and then evoked greater subsequent inhibitory feedbacks, therefore resulting in a larger NP effect. These results provide direct evidence for the reactive inhibition suggested by the Houghton and Tipper model. Meanwhile a coincident greater positive priming (PP) effect was obtained under the overlapped than separated condition, which could be attributed to the higher level of target activation in the overlapped condition. The covariation of NP and PP effects further confirmed that the way of

  6. Inhibitory effect of strychnine on acetylcholine receptor activation in bovine adrenal medullary chromaffin cells.

    Science.gov (United States)

    Kuijpers, G A; Vergara, L A; Calvo, S; Yadid, G

    1994-01-01

    1. Strychnine, which is known as a potent and selective antagonist of the inhibitory glycine receptor in the central nervous system, inhibits the nicotinic stimulation of catecholamine release from bovine cultured adrenal chromaffin cells in a concentration-dependent (1-100 microM) manner. At 10 microM nicotine, the IC50 value for strychnine is approximately 30 microM. Strychnine also inhibits the nicotine-induced membrane depolarization and increase in intracellular Ca2+ concentration. 2. The inhibitory action of strychnine is reversible and is selective for nicotinic stimulation, with no effect observed on secretion elicited by a high external K+ concentration, histamine or angiotensin II. 3. Strychnine competes with nicotine in its effect, but not modify the apparent positive cooperatively of the nicotine binding sites. In the absence of nicotine, strychnine has no effect on catecholamine release. Glycine does not affect catecholamine release nor the inhibitory action of strychnine on this release. 4. These results suggest that strychnine interacts with the agonist binding site of the nicotinic acetylcholine receptor in chromaffin cells, thus exerting a pharmacological effect independently of the glycine receptor. PMID:7834198

  7. Inhibitory effects of active fraction and its main components of Shaofu Zhuyu decoction on uterus contraction.

    Science.gov (United States)

    Su, Shulan; Hua, Yongqing; Duan, Jin-Ao; Zhou, Wei; Shang, Erxin; Tang, Yuping

    2010-01-01

    Shaofu Zhuyu decoction is a famous formula for treating primary dysmenorrhea in China since the Qing dynasty. In this paper, the inhibitory effects of active-guided fraction and its main bioactive components of Shaofu Zhuyu decoction on a model of non-pregnant mice uterine contraction induced by oxytocin in vitro were investigated. Qualitative and quantitative chemical analyses were used to correlate the chemical composition of active fraction with the spasmolytic effects. Seven ingredients in the active fraction were identified and quantified by HPLC-DAD. Three ingredients, ferulic acid, vanillic acid, and typhaneoside, were evaluated for their effects on mice isolated uterine contraction induced by oxytocin in vitro. The ED(50) of them were 63.0 microg/ml, 57.6 microg/ml, 109.7 microg/ml, respectively. Furthermore, the inhibitory activity of the combination of these three compounds was prior to the fraction and seven compounds group. The ED(50) was 65.5 microg/ml. The data stated that ferulic acid, vanillic acid, and typhaneoside were possibly the main active components in the bioactive fraction of Shaofu Zhuyu decoction. The study also implied that Shaofu Zhuyu decoction may have direct inhibitory effects on the contractility of the mice uterus and justified the traditional use of the prescription for treating the uterine cramping associated dysmenorrhea.

  8. [Experimental study on inhibitory effect of ganlu xiaodu Dan on coxackie virus in vitro].

    Science.gov (United States)

    He, Y; Wu, C; Zhao, G

    1998-12-01

    To observe the Coxackie virus inhibitory effect of Ganlu Xiaodu Dan (GLXDD), including complete recipe, incomplete recipe and supplemented recipe of it. Using tissue culture technique, the maximal non-toxic concentration of drug on cultured cells, the influence of drug on proliferation of virus in cultured cells and the virus inhibitory effect in different time of action were observed. The maximal non-toxic concentration of GLXDD was 1:40 (25 g/L), no matter whether the recipe was complete, incomplete or supplementary. CLXDD in that concentration could inhibit significantly the proliferation of Coxackie virus B2, B3 and B4 strains, the inhibition index being over 2 and the output of these strains treated with complete recipe of GLXDD was lower significantly than that of the control group (P Coxackie virus in cultured cells.

  9. Inhibitory effect of vanillin on cellulase activity in hydrolysis of cellulosic biomass.

    Science.gov (United States)

    Li, Yun; Qi, Benkun; Wan, Yinhua

    2014-09-01

    Pretreatment of lignocellulosic material produces a wide variety of inhibitory compounds, which strongly inhibit the following enzymatic hydrolysis of cellulosic biomass. Vanillin is a kind of phenolics derived from degradation of lignin. The effect of vanillin on cellulase activity for the hydrolysis of cellulose was investigated in detail. The results clearly showed that vanillin can reversibly and non-competitively inhibit the cellulase activity at appropriate concentrations and the value of IC50 was estimated to be 30 g/L. The inhibition kinetics of cellulase by vanillin was studied using HCH-1 model and inhibition constants were determined. Moreover, investigation of three compounds with similar structure of vanillin on cellulase activity demonstrated that aldehyde group and phenolic hydroxyl groups of vanillin had inhibitory effect on cellulase. These results provide valuable and detailed information for understanding the inhibition of lignin derived phenolics on cellulase.

  10. Electrochemical evaluation of the inhibitory effects of acetic acid on Saccharomyces cerevisiae

    Institute of Scientific and Technical Information of China (English)

    Yuan Zhenhong; Zhao Jinsheng; Yan Yongjie; Yang Zhengyu

    2006-01-01

    A mediated electrochemical method was proposed for toxic evaluation of acetic acid on S. cerevisiae AS.380, and menadione/ferricyanide was chosen as the mediator system. The variance in electrochemical response in the absence and presence of increasing concentrations of acetic acid were used to indicate the inhibitory effects of weak acid on the yeast. The inhibitory effects of acetic acid on glucose consumption during menadione mediated reduction of ferricyanide were also measured for comparison purpose. The relative limiting current and the glucose consumption were reduced by 64.5 % and 61%, respectively, in the presence of 4g/L acetic acid at pH 4.0. The results showed that the electrochemical method can provide us with an appropriate and convenient tool for cytotoxic evaluation.

  11. Inhibitory Effect and Possible Mechanism of Intraurethral Stimulation on Overactive Bladder in Female Rats.

    Science.gov (United States)

    Tian, Yu; Liao, Limin; Wyndaele, Jean Jacques

    2015-09-01

    To investigate the inhibitory effect and possible mechanism of intraurethral stimulation on overactive bladder (OAB) induced by acetic acid irritation. Cystometry was performed in 13 urethane-anesthetized female rats. Intravesical infusion of 0.5% acetic acid was used to irritate the bladder and induce OAB. Multiple cystometrograms were performed with mirabegron, continuous stimulation, mirabegron plus continuous stimulation, and β3-adrenoceptor antagonist plus continuous stimulation to determine the mechanism underlying the inhibitory effect by intraurethral stimulation. Infusion of acetic acid significantly decreased bladder capacity. Intraurethral stimulation at 2.5 Hz plus mirabegron significantly increased bladder capacity and decreased the nonvoiding contraction count. The changes were strongly inhibited after the β3-adrenoceptor antagonist was administered. Activation of urethral afferent nerves can reverse OAB, which activates C-fiber afferent nerves. This animal study indicates that intraurethral stimulation may interfere with OAB through hypogastric nerve activation and pudendal nerve neuromodulation.

  12. Novel Inhibitory Effect of N-(2-Hydroxycyclohexylvaliolamine on Melanin Production in a Human Skin Model

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    Bum-Ho Bin

    2014-07-01

    Full Text Available Hyper-pigmentation causes skin darkness and medical disorders, such as post-inflammatory melanoderma and melasma. Therefore, the development of anti-melanogenic agents is important for treating these conditions and for cosmetic production. In our previous paper, we demonstrated that the anti-diabetic drug voglibose, a valiolamine derivative, is a potent anti-melanogenic agent. In addition, we proposed an alternative screening strategy to identify valiolamine derivatives with high skin permeability that act as anti-melanogenic agents when applied topically. In this study, we synthesized several valiolamine derivatives with enhanced lipophilicity and examined their inhibitory effects in a human skin model. N-(2-hydroxycyclohexylvaliolamine (HV possesses a stronger inhibitory effect on melanin production than voglibose in a human skin model, suggesting that HV is a more potent anti-melanogenic agent for the skin.

  13. Inhibitory effects of citrus essential oils and their components on the formation of N-nitrosodimethylamine.

    Science.gov (United States)

    Sawamura, M; Sun, S H; Ozaki, K; Ishikawa, J; Ukeda, H

    1999-12-01

    Twenty-eight kinds of citrus essential oils and their components were studied for inhibitory effects on the formation of N-nitrosodimethylamine (NDMA). The reaction mixture consisted of dimethylamine and sodium nitrite adjusted at pH 3.6, in addition to essential oils and an emulsifying agent. The quantification was determined by high-performance liquid chromatography monitored at 220 nm. All of the essential oils inhibited the formation of NDMA in the range of 20-85%. The oils of ujukitsu (Citrus ujukitsu Hort. ex Shirai), yuzu (C. junos Tanaka), mochiyu (C. inflata Hort. ex Tanaka), and ponkan (C. reticulata Blanco cv. F-2426) inhibited the formation of NDMA much more effectively than other citrus oils. The inhibitory proportions of components of citrus essential oils such as myrcene, alpha-terpinene, and terpinolene were as high as 80%.

  14. α-glucosidase and glycation inhibitory effects of costus speciosus leaves

    OpenAIRE

    Perera, Handunge Kumudu Irani; Premadasa, Walgama Kankanamlage Vindhya Kalpani; Poongunran, Jeyakumaran

    2016-01-01

    Background Hyperglycaemia is a salient feature of poorly controlled diabetes mellitus. Rate of protein glycation is increased with hyperglycaemia leading to long term complications of diabetes. One approach of controlling blood glucose in diabetes targets at reducing the postprandial spikes of blood glucose. The objectives of this study were to assess the in vitro inhibitory effects of Costus speciosus (COS) leaves on α-amylase and α-glucosidase activities, fructosamine formation, protein gly...

  15. A comparison about the inhibitory effect of curcunmin and Avastin on the rat corneal neovascularization

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    Yi Wu

    2013-06-01

    Full Text Available AIM: To compare the inhibitory effect of curcunmin and Avastin on the rat corneal neovascularization(CNV, and approach the mechanism of the curcunmin's inhibition. METHODS: CNV was established in thirty SD rats by alkaline burning. Rats were divided equally to group A and group B at random. In group A, right eyes were experimental group A1, treated by 40μmol/L curcunmin solution, and left eyes were control group A2, treated by 0.09% sodium chloride. In group B, right eyes were experimental group group B1, treated by 5g/L avastin, and left eyes were control group B2, treated by 0.09% sodium chloride. Cornea and aqueous humor were collected by time spot. The capillary vessels were study, and the expressions of VEGF were detected by Enzyme-Linked immunosorbnent Assay(ELISA. RESULTS: No toxic effects of the drugs were found. The capillary vessels in experimental group were less than those of control group(P<0.01. No statistical different of the capillary vessels between two drugs were found. The expressions of VEGF in experimental group were less than those in control group(P<0.01. The expressions of VEGF in B1 group were less than in group A1. CONCLUSION: The inhibitory effect to CNV of curcunmin and avastin have no statistical different in the experiment, but curcunmin has the less inhibitory effect to the expressions of VEGF than avastin. Curcunmin may have other mechanism in the inhibitory action on CNV.

  16. Inhibitory effect of a hot water extract of coffee "silverskin" on hyaluronidase.

    Science.gov (United States)

    Furusawa, Mina; Narita, Yusaku; Iwai, Kazuya; Fukunaga, Taiji; Nakagiri, Osamu

    2011-01-01

    Coffee "silverskin" (CS) is a by-product of the roasting procedure for coffee beans. A CS extract (CS-ext) was found to have a high inhibitory effect against hyaluronidase. It seems that the higher-molecular-weight substances in CS-ext contributed most to the hyaluronidase inhibition, while acidic polysaccharides mainly composed of uronic acid played a major role in this hyaluronidase inhibition by CS-ext.

  17. Effects of nanosuspension and inclusion complex techniques on the in vitro protease inhibitory activity of naproxen

    OpenAIRE

    Dharmalingam, Senthil Rajan; Chidambaram, Kumarappan; Ramamurthy, Srinivasan; Nadaraju,Shamala

    2014-01-01

    This study investigated the effects of nanosuspension and inclusion complex techniques on in vitro trypsin inhibitory activity of naproxen—a member of the propionic acid derivatives, which are a group of antipyretic, analgesic, and non-steroidal anti-inflammatory drugs. Nanosuspension and inclusion complex techniques were used to increase the solubility and anti-inflammatory efficacy of naproxen. The evaporative precipitation into aqueous solution (EPAS) technique and the kneading metho...

  18. Analysis of glycation induced protein cross-linking inhibitory effects of some antidiabetic plants and spices

    OpenAIRE

    Perera, Handunge Kumudu Irani; Handuwalage, Charith Sandaruwan

    2015-01-01

    Background Protein cross-linking which occurs towards the latter part of protein glycation is implicated in the development of chronic diabetic complications. Glycation induced protein cross-linking inhibitory effects of nine antidiabetic plants and three spices were evaluated in this study using a novel, simple, electrophoresis based method. Methods Methanol extracts of thirteen plants including nine antidiabetic plants and three spices were used. Lysozyme and fructose were incubated at 37 °...

  19. Inhibitory effect of Lactobacillus rhamnosus on pathogenic bacteria isolated from women with bacterial vaginosis

    OpenAIRE

    Gita Eslami; Sudabeh Taheri; Eznollah Azargashb; raheleh karimiravesh

    2014-01-01

    Background: Considering the high prevalence of bacterial vaginosis and its association with urinary tract infection in women and treatment of gynecologic problems occur when a high recurrence of bacterial vaginosis is often treated with antibiotics. The purpose of this study is to investigate the inhibitory effect of Lactobacillus rhamnosus on pathogenic bacteria isolated from women with bacterial vaginosis, respectively.Materials and Methods: 96 samples from women with bacterial vaginosis di...

  20. Inhibitory Effects of Garcinia cambogia Extract on CYP2B6 Enzyme Activity.

    Science.gov (United States)

    Yu, Jun Sang; Choi, Min Sun; Park, Jong Suk; Rehman, Shaheed Ur; Nakamura, Katsunori; Yoo, Hye Hyun

    2017-03-13

    This study assessed the inhibitory effects of Garcinia cambogia extract on the cytochrome P450 enzymes in vitro. G. cambogia extract was incubated with cytochrome P450 isozyme-specific substrates in human liver microsomes and recombinant CYP2B6 isozyme, and the formation of the marker metabolites was measured to investigate the inhibitory potential on cytochrome P450 enzyme activities. The results showed that G. cambogia extract has significant inhibitory effects on CYP2B6 activity in a concentration-dependent manner. Furthermore, the inhibition was potentiated following preincubation with NADPH, indicating that G. cambogia extract is a time-dependent inhibitor of CYP2B6. Meanwhile, hydroxycitric acid, the major bioactive ingredient of G. cambogia extract, did not exhibit significant inhibition effects on cytochrome P450 enzyme activities. G. cambogia extract could modulate the pharmacokinetics of CYP2B6 substrate drugs and lead to interactions with those drugs. Therefore, caution may be required with respect to concomitant intake of dietary supplements containing G. cambogia extract with CYP2B6 substrates.

  1. DNA damage inhibitory effect and phytochemicals of fermented red brown rice extract

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    Ee-Ling Kong

    2015-09-01

    Full Text Available Objective: To determine the polyphenol compounds (phenolic and flavonoid compounds, antioxidant activity [1,1-diphenylpicryl-2-picrylhydrazyl (DPPH radical scavenging activity] and DNA damage inhibitory effect of fermented local red brown rice. Methods: DNA nicking assay was employed to determine the antioxidant activity of the fermented rice extract. Phytochemical screening was completed using standard methods and DPPH radical assays were used to confirm the antioxidant properties of the extracts. Results: After four days of fermentation, fermented red brown rice had more polyphenol compounds compared to unfermented counterpart. Fermented red brown rice showed greater antioxidant properties with EC50 value of DPPH radical scavenging of 43.00 mg extract/mL or 8 mg quercetin equivalent antioxidant activity. In addition, fermented rice extract showed DNA damage inhibitory effect to a certain extent. It protected DNA from reactive oxygen species; however, at high concentration it might induce reductive damage to DNA, whereas, unfermented red brown rice showed weak DNA damage inhibitory effect. Conclusions: Fermented red brown rice could protect DNA from oxidative damage but might induce reductive damage to DNA at high concentrations.

  2. Inhibitory Effect of Waste Glass Powder on ASR Expansion Induced by Waste Glass Aggregate

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    Shuhua Liu

    2015-10-01

    Full Text Available Detailed research is carried out to ascertain the inhibitory effect of waste glass powder (WGP on alkali-silica reaction (ASR expansion induced by waste glass aggregate in this paper. The alkali reactivity of waste glass aggregate is examined by two methods in accordance with the China Test Code SL352-2006. The potential of WGP to control the ASR expansion is determined in terms of mean diameter, specific surface area, content of WGP and curing temperature. Two mathematical models are developed to estimate the inhibitory efficiency of WGP. These studies show that there is ASR risk with an ASR expansion rate over 0.2% when the sand contains more than 30% glass aggregate. However, WGP can effectively control the ASR expansion and inhibit the expansion rate induced by the glass aggregate to be under 0.1%. The two mathematical models have good simulation results, which can be used to evaluate the inhibitory effect of WGP on ASR risk.

  3. Inhibitory effect of two Indian medicinal plants on aldose reductase of rat lensin vitro

    Institute of Scientific and Technical Information of China (English)

    Rajesh Kumar; Dinesh Kumar Patel; Damiki Laloo; Krishnamurthy Sairam; Siva Hemalatha

    2011-01-01

    Objective:To assesse the inhibitory effect of alcoholic extract of two Indian medicinal plants namelyCeasalpinia digyna Rottler and, Alangium lamarckii Thwaits on aldose reductase(AR) of rat lens.Methods: Rats lens were enucleated through posterior approach and their homogenate was prepared and centrifuged to obtain a clear supernatant for the determination ofAR activity and protein content.Results:The alcoholic extract of Ceasalpinia digyna andAlangium lamarckii had a potent inhibitory effect on the lensAR enzyme. TheIC50 values of alcoholic extract of the selected plants were calculated and were (46.29±11.17)and(106.00±5.11) μg/mL, respectively. Quercetin was used as a positive control and itsIC50value was (2.95±1.53)μg/mL.Conclusions:Thus, it is concluded that alcoholic extracts of the selected plant exhibit significant inhibitory effects on AR in the rat lensin vitro.

  4. Acute neuropharmacological effects of atomoxetine on inhibitory control in ADHD children: A fNIRS study

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    Masako Nagashima

    2014-01-01

    Full Text Available The object of the current study is to explore the neural substrate for effects of atomoxetine (ATX on inhibitory control in school-aged children with attention deficit hyperactivity disorder (ADHD using functional near-infrared spectroscopy (fNIRS. We monitored the oxy-hemoglobin signal changes of sixteen ADHD children (6–14 years old performing a go/no-go task before and 1.5 h after ATX or placebo administration, in a randomized, double-blind, placebo-controlled, crossover design. Sixteen age- and gender-matched normal controls without ATX administration were also monitored. In the control subjects, the go/no-go task recruited the right inferior and middle prefrontal gyri (IFG/MFG, and this activation was absent in pre-medicated ADHD children. The reduction of right IFG/MFG activation was acutely normalized after ATX administration but not placebo administration in ADHD children. These results are reminiscent of the neuropharmacological effects of methylphenidate to up-regulate reduced right IFG/MFG function in ADHD children during inhibitory tasks. As with methylphenidate, activation in the IFG/MFG could serve as an objective neuro-functional biomarker to indicate the effects of ATX on inhibitory control in ADHD children. This promising technique will enhance early clinical diagnosis and treatment of ADHD in children, especially in those with a hyperactivity/impulsivity phenotype.

  5. Oxytocin enhances the inhibitory effects of diazepam in the rat central medial amygdala.

    Science.gov (United States)

    Viviani, D; Terrettaz, T; Magara, F; Stoop, R

    2010-01-01

    Oxytocin is a neuropeptide that can reduce neophobia and improve social affiliation. In vitro, oxytocin induces a massive release of GABA from neurons in the lateral division of the central amygdala which results in inhibition of a subpopulation of peripherally projecting neurons in the medial division of the central amygdala (CeM). Common anxiolytics, such as diazepam, act as allosteric modulators of GABA(A) receptors. Because oxytocin and diazepam act on GABAergic transmission, it is possible that oxytocin can potentiate the inhibitory effects of diazepam if both exert their pre, - respectively postsynaptic effects on the same inhibitory circuit in the central amygdala. We found that in CeM neurons in which diazepam increased the inhibitory postsynaptic current (IPSC) decay time, TGOT (a specific oxytocin receptor agonist) increased IPSC frequency. Combined application of diazepam and TGOT resulted in generation of IPSCs with increased frequency, decay times as well as amplitudes. While individual saturating concentrations of TGOT and diazepam each decreased spontaneous spiking frequency of CeM neurons to similar extent, co-application of the two was still able to cause a significantly larger decrease. These findings show that oxytocin and diazepam act on different components of the same GABAergic circuit in the central amygdala and that oxytocin can facilitate diazepam effects when used in combination. This raises the possibility that neuropeptides could be clinically used in combination with currently used anxiolytic treatments to improve their therapeutic efficacy.

  6. Inhibitory Effect of Waste Glass Powder on ASR Expansion Induced by Waste Glass Aggregate

    Science.gov (United States)

    Liu, Shuhua; Wang, Shu; Tang, Wan; Hu, Ningning; Wei, Jianpeng

    2015-01-01

    Detailed research is carried out to ascertain the inhibitory effect of waste glass powder (WGP) on alkali-silica reaction (ASR) expansion induced by waste glass aggregate in this paper. The alkali reactivity of waste glass aggregate is examined by two methods in accordance with the China Test Code SL352-2006. The potential of WGP to control the ASR expansion is determined in terms of mean diameter, specific surface area, content of WGP and curing temperature. Two mathematical models are developed to estimate the inhibitory efficiency of WGP. These studies show that there is ASR risk with an ASR expansion rate over 0.2% when the sand contains more than 30% glass aggregate. However, WGP can effectively control the ASR expansion and inhibit the expansion rate induced by the glass aggregate to be under 0.1%. The two mathematical models have good simulation results, which can be used to evaluate the inhibitory effect of WGP on ASR risk. PMID:28793603

  7. α-Glucosidase Inhibitory Effect and Simultaneous Quantification of Three Major Flavonoid Glycosides in Microctis folium

    Directory of Open Access Journals (Sweden)

    Wen-Cai Ye

    2013-04-01

    Full Text Available Microctis Folium, the leaves of Microcos paniculata L., is a commonly used herbal tea material. The methanol extract of Microctis Folium and its principle compounds vitexin (1, isovitexin (2 and isorhamnetin 3-O-β-D-rutinoside (3 were investigated for their α-glucosidase inhibitory effects. The extract showed strong α-glucosidase inhibitory effect (IC50 = 61.30 μg/mL and the three flavonoid glycosides 1–3 exerted satisfactory α-glucosidase inhibitory effects, with IC50 values of 244.0 μM, 266.2 μM and 275.4 μM, respectively. A simple and reliable HPLC-DAD method was developed for the quantification of the three flavonoid glycosides in Microctis Folium and applied successfully to determine contents of these components in samples collected from different locations. This study suggested that Microctis Folium may be a promising candidate for development of herbal antidiabetes drugs, and vitexin, isovitexin and isorhamnetin 3-O-β-D-rutinoside can be the biomarkers and chemical markers for this plant substance.

  8. The effect of somatostatin on release and insulinotropic action of gastric inhibitory polypeptide.

    Science.gov (United States)

    Pederson, R A; Dryburgh, J R; Brown, J C

    1975-12-01

    Studies were carried out in conscious dogs in which the effect of intravenous somatostatin on immunoreactive gastric inhibitory polypeptide (IR-GIP) release was investigated. In addition, the inhibitory action of somatostatin on the insulin response to pure porcine GIP was assessed. Intravenous administration of somatostatin resulted in a delayed IR-GIP and immunoreactive insulin (IRI) response to oral glucose. Somatostatin also delayed the IR-GIP response to the ingestion of fat. In both types of experiments, initial depression of IRI levels was followed by a sharp rise in IRI release. Intravenous infusion of somatostatin produced 80% inhibition of the IRI response to pure porcine GIP. It was concluded that somatostatin inhibits the physiological release of IR-GIP and the insulinotropic action of exogenous porcine GIP.

  9. Sex Differences in COMT Polymorphism Effects on Prefrontal Inhibitory Control in Adolescence

    Science.gov (United States)

    White, Thomas P; Loth, Eva; Rubia, Katya; Krabbendam, Lydia; Whelan, Robert; Banaschewski, Tobias; Barker, Gareth J; Bokde, Arun LW; Büchel, Christian; Conrod, Patricia; Fauth-Bühler, Mira; Flor, Herta; Frouin, Vincent; Gallinat, Jürgen; Garavan, Hugh; Gowland, Penny; Heinz, Andreas; Ittermann, Bernd; Lawrence, Claire; Mann, Karl; Paillère, Marie-Laure; Nees, Frauke; Paus, Tomas; Pausova, Zdenka; Rietschel, Marcella; Robbins, Trevor; Smolka, Michael N; Shergill, Sukhwinder S; Schumann, Gunter

    2014-01-01

    Catecholamine-0-methyl-transferase (COMT) gene variation effects on prefrontal blood oxygenation-level-dependent (BOLD) activation are robust; however, despite observations that COMT is estrogenically catabolized, sex differences in its prefrontal repercussions remain unclear. Here, in a large sample of healthy adolescents stratified by sex and Val158Met genotype (n=1133), we examine BOLD responses during performance of the stop-signal task in right-hemispheric prefrontal regions fundamental to inhibitory control. A significant sex-by-genotype interaction was observed in pre-SMA during successful-inhibition trials and in both pre-SMA and inferior frontal cortex during failed-inhibition trials with Val homozygotes displaying elevated activation compared with other genotypes in males but not in females. BOLD activation in the same regions significantly mediated the relationship between COMT genotype and inhibitory proficiency as indexed by stop-signal reaction time in males alone. These sexually dimorphic effects of COMT on inhibitory brain activation have important implications for our understanding of the contrasting patterns of prefrontally governed psychopathology observed in males and females. PMID:24820538

  10. Inhibitory effect against pathogenic and spoilage bacteria of Pseudomonas strains isolated from spoiled and fresh fish.

    Science.gov (United States)

    Gram, L

    1993-01-01

    The antibacterial effects of 209 Pseudomonas strains isolated from spoiled iced fish and newly caught fish were assessed by screening target organisms in agar diffusion assays. One-third (67 strains) inhibited the growth of one or several of six target organisms (Escherichia coli, Shewanella putrefaciens, Aeromonas sobria, Pseudomonas fluorescens, Listeria monocytogenes, and Staphylococcus aureus), of which S. aureus and A. sobria were the most sensitive. The inhibitory action was most pronounced among the strains producing siderophores, and the presence of iron eliminated the antibacterial effect of two-thirds of the inhibitory strains. Siderophore-mediated competition for iron may explain the inhibitory activity of these strains. All but nine of the inhibiting strains were found to inhibit the growth of 38 psychrotrophic S. putrefaciens strains isolated from spoiling fish and fish products. Siderophore-containing Pseudomonas culture supernatants inhibited growth of S. putrefaciens, as did the addition of iron chelators (ethylenediamine dihydroxyphenylacetic acid [EDDHA]). In particular, Pseudomonas strains isolated from newly caught and spoiled Nile perch (Lates niloticus) inhibited S. putrefaciens. This suggests that microbial interaction (e.g., competition or antagonism) may influence the selection of a microflora for some chilled food products. PMID:8357253

  11. Controlled versus automatic processes: which is dominant to safety? The moderating effect of inhibitory control.

    Directory of Open Access Journals (Sweden)

    Yaoshan Xu

    Full Text Available This study explores the precursors of employees' safety behaviors based on a dual-process model, which suggests that human behaviors are determined by both controlled and automatic cognitive processes. Employees' responses to a self-reported survey on safety attitudes capture their controlled cognitive process, while the automatic association concerning safety measured by an Implicit Association Test (IAT reflects employees' automatic cognitive processes about safety. In addition, this study investigates the moderating effects of inhibition on the relationship between self-reported safety attitude and safety behavior, and that between automatic associations towards safety and safety behavior. The results suggest significant main effects of self-reported safety attitude and automatic association on safety behaviors. Further, the interaction between self-reported safety attitude and inhibition and that between automatic association and inhibition each predict unique variances in safety behavior. Specifically, the safety behaviors of employees with lower level of inhibitory control are influenced more by automatic association, whereas those of employees with higher level of inhibitory control are guided more by self-reported safety attitudes. These results suggest that safety behavior is the joint outcome of both controlled and automatic cognitive processes, and the relative importance of these cognitive processes depends on employees' individual differences in inhibitory control. The implications of these findings for theoretical and practical issues are discussed at the end.

  12. The Inhibitory Effect of Prunella vulgaris L. on Aldose Reductase and Protein Glycation

    Directory of Open Access Journals (Sweden)

    Hong Mei Li

    2012-01-01

    Full Text Available To evaluate the aldose reductase (AR enzyme inhibitory ability of Prunella vulgaris L. extract, six compounds were isolated and tested for their effects. The components were subjected to in vitro bioassays to investigate their inhibitory assays using rat lens aldose reductase (rAR and human recombinant AR (rhAR. Among them, caffeic acid ethylene ester showed the potent inhibition, with the IC50 values of rAR and rhAR at 3.2±0.55 μM and 12.58±0.32 μM, respectively. In the kinetic analyses using Lineweaver-Burk plots of 1/velocity and 1/concentration of substrate, this compound showed noncompetitive inhibition against rhAR. Furthermore, it inhibited galactitol formation in a rat lens incubated with a high concentration of galactose. Also it has antioxidative as well as advanced glycation end products (AGEs inhibitory effects. As a result, this compound could be offered as a leading compound for further study as a new natural products drug for diabetic complications.

  13. Effect of toothpaste on the plaque inhibitory properties of a cetylpyridinium chloride mouth rinse.

    Science.gov (United States)

    Sheen, S; Eisenburger, M; Addy, M

    2003-03-01

    Cetylpyridinium chloride (CPC) mouth rinses have moderate plaque inhibitory activity when used alone but rarely have shown adjunctive benefits to tooth brushing with toothpaste. Several explanations for this apparent anomaly can be proferred, including loss of antiseptic activity due to interactions with toothpaste ingredients. The aim of this study was to measure the effect of toothpaste on the plaque inhibitory properties of a CPC mouth rinse using paired rinses of CPC, toothpaste slurry (TP) and water (W). The study was a single blind, randomised, seven-treatment, cross over design balanced for residual effects, involving 21 healthy, dentate subjects. The paired rinses were: W-CPC, CPC-W, TP-CPC, CPC-TP, W-TP, TP-W and W-W. Rinsing with solutions or slurries was done for 60 s twice per day. On day 1, subjects were rendered plaque free, suspended tooth cleaning and commenced the allocated rinse regimen. On day 5, plaque was scored by index. A 2(1/2) day wash out of normal oral hygiene was allowed between each regimen. The order from lowest to highest plaque scores was as follows: W-CPC = CPC-W mouth rinse adversely affected the plaque inhibitory action of this antiseptic. This in part may explain the reported lack of adjunctive benefits of CPC rinses to normal oral hygiene practices and supports the suggestion, made for chlorhexidine rinses, that their use should follow toothpaste by at least 60 min.

  14. Controlled versus automatic processes: which is dominant to safety? The moderating effect of inhibitory control.

    Science.gov (United States)

    Xu, Yaoshan; Li, Yongjuan; Ding, Weidong; Lu, Fan

    2014-01-01

    This study explores the precursors of employees' safety behaviors based on a dual-process model, which suggests that human behaviors are determined by both controlled and automatic cognitive processes. Employees' responses to a self-reported survey on safety attitudes capture their controlled cognitive process, while the automatic association concerning safety measured by an Implicit Association Test (IAT) reflects employees' automatic cognitive processes about safety. In addition, this study investigates the moderating effects of inhibition on the relationship between self-reported safety attitude and safety behavior, and that between automatic associations towards safety and safety behavior. The results suggest significant main effects of self-reported safety attitude and automatic association on safety behaviors. Further, the interaction between self-reported safety attitude and inhibition and that between automatic association and inhibition each predict unique variances in safety behavior. Specifically, the safety behaviors of employees with lower level of inhibitory control are influenced more by automatic association, whereas those of employees with higher level of inhibitory control are guided more by self-reported safety attitudes. These results suggest that safety behavior is the joint outcome of both controlled and automatic cognitive processes, and the relative importance of these cognitive processes depends on employees' individual differences in inhibitory control. The implications of these findings for theoretical and practical issues are discussed at the end.

  15. Inhibitory effects of butyrate on biological hydrogen production with mixed anaerobic cultures.

    Science.gov (United States)

    Zheng, Xian-Jun; Yu, Han-Qing

    2005-01-01

    In this study batch experiments were conducted to investigate the inhibitory effects of butyrate addition on hydrogen production from glucose by using anaerobic mixed cultures. Experimental results showed that addition of butyrate at 4.18 and 6.27 g/l only slightly inhibited hydrogen production, and addition of butyrate at 8.36-12.54 g/l imposed a moderate inhibitory effect on hydrogen production. At addition of 25.08 g/l, butyrate had a strong inhibitory influence on substrate degradation and hydrogen production. The distribution of the volatile fatty acids produced from the acidogeneisis of glucose was significantly influenced by the addition of butyrate. The inhibition of butyrate addition on hydrogen production was described well by a non-competitive and non-linear inhibition model, with the maximum hydrogen production rate of 59.3 ml/g-SS/h, critical added butyrate concentration of 25.08 g/l, and inhibition degree of 0.323, respectively. The C(I,50) values (the butyrate concentration at which bioactivity is reduced by 50%) for hydrogen production rate and yield were estimated as 19.39 and 20.78 g/l of added butyrate, respectively.

  16. Effect of phlorotannins isolated from Ecklonia cava on angiotensin I-converting enzyme (ACE) inhibitory activity.

    Science.gov (United States)

    Wijesinghe, W A J P; Ko, Seok-Chun; Jeon, You-Jin

    2011-04-01

    Inhibition of angiotensin I-converting enzyme (ACE) activity is the most common mechanism underlying the lowering of blood pressure. In the present study, five organic extracts of a marine brown seaweed Ecklonia cava were prepared by using ethanol, ethyl acetate, chloroform, hexane, and diethyl ether as solvents, which were then tested for their potential ACE inhibitory activities. Ethanol extract showed the strongest ACE inhibitory activity with an IC(50) value of 0.96 mg/ml. Five kinds of phlorotannins, phloroglucinol, triphlorethol-A, eckol, dieckol, and eckstolonol, were isolated from ethanol extract of E. cava, which exhibited potential ACE inhibition. Dieckol was the most potent ACE inhibitor and was found to be a non-competitive inhibitor against ACE according to Lineweaver-Burk plots. Dieckol had an inducible effect on the production of NO in EAhy926 cells without having cytotoxic effect. The results of this study indicate that E. cava could be a potential source of phlorotannins with ACE inhibitory activity for utilization in production of functional foods.

  17. Inhibitory effects of Curcuma aromatica oil on proliferation of hepatoma in mice

    Institute of Scientific and Technical Information of China (English)

    Wan Yin Wu; Qin Xu; Ling Chun Shi; Wei Bin Zhang

    2000-01-01

    AIM To reveal the inhibitory effects of Curcuma aromatica oil ( CAO ) on cell proliferation of hepatoma in mice. METHODS Two tumor inhibitory experiments of CAO on hepatoma in mice were conducted.The inhibitory effects of CAO on proliferation of hepatoma in mice were evaluated by DNA image cytometry and immunohistochemical staining of proliferating cell nuclear antigen (PCNA).RESULTS The tumor inhibitory rates of CAO were 52% and 51% in two experiments,respectively. Compared with those of the salinetreated control groups, both differences were statistically significant (P < 0.01). In the group of mice treated with CAO, the cellular nuclear DNA OD value (249 ± 70), areas (623μnm2 ±228 μm2) and DNA (2.38 ± 0.67) index of hepatic carcinomas were significantly lower than those of the control group (430 ± 160, 1073μm2 ± 101 um2 and 4.48 ± 0.71 ). CAO also could increase diploidy cell rates (29.00% ± 9.34% vs 2.97% ± 5.69%, P<0.01 ) and decrease pentaploidy cell exceeding rate (30.04% ± 15.10% vs 70.89%±14.94%, P<0.01). In the group of mice treated with CAO, the labeling indexes of proliferating cell nuclear antigen (PCNA-LI) were 30% ± 4%, which were significantly lower than 40% ± 6% of the control group (P<0.01). CONCLUSION The inhibition of CAO on the growth of hepatoma in mice might be associated with its depression on cellular proliferative activity.

  18. Inhibitory effects of some plant essential oils against Arcobacter butzleri and potential for rosemary oil as a natural food preservative.

    Science.gov (United States)

    Irkin, Reyhan; Abay, Secil; Aydin, Fuat

    2011-03-01

    We investigated the inhibitory activity of commercially marketed essential oils of mint, rosemary, orange, sage, cinnamon, bay, clove, and cumin against Arcobacter butzleri and Arcobacter skirrowii and the effects of the essential oil of rosemary against A. butzleri in a cooked minced beef system. Using the disc diffusion method to determine the inhibitory activities of these plant essential oils against strains of Arcobacter, we found that those of rosemary, bay, cinnamon, and clove had strong inhibitory activity against these organisms, whereas the essential oils of cumin, mint, and sage failed to show inhibitory activity against most of the Arcobacter strains tested. The 0.5% (vol/wt) essential oil of rosemary was completely inhibitory against A. butzleri in the cooked minced beef system at 4°C. These essential oils may be further investigated as a natural solution to the food industry by creating an additional barrier (hurdle technology) to inhibit the growth of Arcobacter strains.

  19. Inhibitory effects of chickpea and Tribulus terrestris on lipase, α-amylase and α-glucosidase.

    Science.gov (United States)

    Ercan, Pınar; El, Sedef Nehir

    2016-08-15

    The total saponin content and its in vitro bioaccessibilities in Tribulus terrestris and chickpea were determined by a static in vitro digestion method (COST FA1005 Action INFOGEST). Also, in vitro inhibitory effects of the chosen food samples on lipid and starch digestive enzymes were determined by evaluating the lipase, α-amylase and α-glucosidase activities. The tested T. terrestris and chickpea showed inhibitory activity against α-glucosidase (IC50 6967 ± 343 and 2885 ± 85.4 μg/ml, respectively) and α-amylase (IC50 343 ± 26.2 and 167 ± 6.12 μg/ml, respectively). The inhibitory activities of T. terrestris and chickpea against lipase were 15.3 ± 2.03 and 9.74 ± 1.09 μg/ml, respectively. The present study provides the first evidence that these food samples (T. terrestris, chickpea) are potent inhibitors of key enzymes in digestion of carbohydrates and lipids in vitro.

  20. Inhibitory effects of Colocasia esculenta (L.) Schott constituents on aldose reductase.

    Science.gov (United States)

    Li, Hong Mei; Hwang, Seung Hwan; Kang, Beom Goo; Hong, Jae Seung; Lim, Soon Sung

    2014-01-01

    The goal of this study was to determine the rat lens aldose reductase-inhibitory effects of 95% ethanol extracts from the leaves of C. esculenta and, its organic solvent soluble fractions, including the dichloromethane (CH2Cl2), ethyl acetate (EtOAc), n-butanol (BuOH) and water (H2O) layers, using dl-glyceraldehyde as a substrate. Ten compounds, namely tryptophan (1), orientin (2), isoorientin (3), vitexin (4), isovitexin (5), luteolin-7-O-glucoside (6), luteolin-7-O-rutinoside (7), rosmarinic acid (8), 1-O-feruloyl-d-glucoside (9) and 1-O-caffeoyl-d-glucoside (10) were isolated from the EtOAc and BuOH fractions of C. esculenta. The structures of compounds 1-10 were elucidated by spectroscopic methods and comparison with previous reports. All the isolates were subjected to an in vitro bioassay to evaluate their inhibitory activity against rat lens aldose reductase. Among tested compounds, compounds 2 and 3 significantly inhibited rat lens aldose reductase, with IC50 values of 1.65 and 1.92 μM, respectively. Notably, the inhibitory activity of orientin was 3.9 times greater than that of the positive control, quercetin (4.12 μM). However, the isolated compounds showed only moderate ABTS+ [2,29-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid)] activity. These results suggest that flavonoid derivatives from Colocasia esculenta (L.) Schott represent potential compounds for the prevention and/or treatment of diabetic complications.

  1. Evaluation of Traditional Indian Antidiabetic Medicinal Plants for Human Pancreatic Amylase Inhibitory Effect In Vitro

    Directory of Open Access Journals (Sweden)

    Sudha Ponnusamy

    2011-01-01

    Full Text Available Pancreatic α-amylase inhibitors offer an effective strategy to lower the levels of post prandial hyperglycemia via control of starch breakdown. Eleven Ayurvedic Indian medicinal plants with known hypoglycemic properties were subjected to sequential solvent extraction and tested for α-amylase inhibition, in order to assess and evaluate their inhibitory potential on pancreatic α-amylase. Analysis of 91 extracts, showed that 10 exhibited strong Human Pancreatic Amylase (HPA inhibitory potential. Of these, 6 extracts showed concentration dependent inhibition with IC50 values, namely, cold and hot water extracts from Ficus bengalensis bark (4.4 and 125 μgmL-1, Syzygium cumini seeds (42.1 and 4.1 μgmL-1, isopropanol extracts of Cinnamomum verum leaves (1.0 μgmL-1 and Curcuma longa rhizome (0.16 μgmL-1. The other 4 extracts exhibited concentration independent inhibition, namely, methanol extract of Bixa orellana leaves (49 μgmL-1, isopropanol extract from Murraya koenigii leaves (127 μgmL-1, acetone extracts from C. longa rhizome (7.4 μgmL-1 and Tribulus terrestris seeds (511 μgmL-1. Thus, the probable mechanism of action of the above fractions is due to their inhibitory action on HPA, thereby reducing the rate of starch hydrolysis leading to lowered glucose levels. Phytochemical analysis revealed the presence of alkaloids, proteins, tannins, cardiac glycosides, flavonoids, saponins and steroids as probable inhibitory compounds.

  2. The effects of inhibitory control training for preschoolers on reasoning ability and neural activity

    DEFF Research Database (Denmark)

    Liu, Qian; Zhu, Xinyi; Ziegler, Albert

    2015-01-01

    /week, for 3 weeks. Several cognitive tasks (involving inhibitory control, working memory, and fluid intelligence) were used to evaluate the transfer effects, and electroencephalography (EEG) was performed during a go/no-go task. Progress on the trained game was significant, while performance on a reasoning...... task (Raven’s Progressive Matrices) revealed a trend-level improvement from pre- to post-test. EEG indicated that the N2 effect of the go/no-go task was enhanced after training for girls. This study is the first to show that pure response inhibition training can potentially improve reasoning ability...

  3. Effect of stimulus parameters and contraction level on inhibitory responses in human jaw-closing muscles: Implications for contingent stimulation

    DEFF Research Database (Denmark)

    Jadidi, F; Wang, K; Arendt-Nielsen, Lars

    2009-01-01

      Objective: Examine the effect of stimulus duration as well as stimulus intensity and level of muscle contraction on the inhibitory responses in human jaw-closing muscles. Design: The inhibitory jaw-reflexes, ES1 and ES2, were recorded in the surface electromyogram (EMG) of masseter and temporalis...... results suggest that the ES2 reflex response is associated with the duration of the electrical stimuli, the intensity level but not the contraction level. In contrast, the inhibitory effects of ultra-long stimuli (450 ms) are not specifically related to the intensity level suggesting that this is a non...

  4. Inhibitory effect of fruit juices on the doxorubicin metabolizing activity of carbonyl reductase 1.

    Science.gov (United States)

    Miura, Takeshi; Nagai, Katsutoshi; Kaneshiro, Shingo; Taketomi, Ayako; Nakabayashi, Toshikatsu; Konishi, Hiroki; Nishinaka, Toru; Terada, Tomoyuki

    2017-03-09

    Doxorubicin, an anthracycline anti-cancer drug, is effective for breast cancer and childhood lymphoma. Chronic cardiotoxicity has been known as a critical adverse effect of doxorubicin and is attributed to its metabolite doxorubicinol produced by carbonyl reductase 1 (CBR1, SDR21C1). Some flavonoids have been reported to act as inhibitors for CBR1, therefore, commercially available juices containing flavonoids are likely to be applicable as a prophylactic treatment against doxorubicin-induced cardiotoxicity by suppression doxorubicinol production. In the study, fruit juices containing flavonoids were investigated on inhibitory effects for CBR1. Recombinant CBR1 protein was subjected to in vitro enzymatic assays with/without juices. An apple juice and a grapefruit juice were selected in the present study as candidates capable of inhibiting CBR1. The enzymatic assays revealed that both juices potently inhibit the CBR1-mediated metabolic conversion of doxorubicin to doxorubicinol in concertation-dependent manners. The concentrations required for obtaining 50% inhibition (IC50) were 0.0012% (v/v) and 0.0014% (v/v) for apple and grapefruit juices, respectively. Additionally, it is worth noting that these juices showed inhibitory effects on doxorubicin metabolism by CBR1 even at very low concentrations (0.0001% (v/v)). An apple juice and a grape fruit juice showed strong inhibitory effects on doxorubicin metabolism by CBR1 in vitro. These results suggest that the intake of flavonoid-containing juices can be promising measure for the protection against doxorubicin-induced cardiac toxicity, enabling patients to keep higher adherence with routine use in light of safety, economic performance and stable supply to market. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.

  5. The signaling of amitriptyline-induced inhibitory effect on electrical field stimulation response in colon smooth muscle.

    Science.gov (United States)

    Zaw, Tin Sandar; Khin, Phyu Phyu; Sohn, Uy Dong

    2016-09-01

    Amitriptyline, a well-known antidepressant, exerts inhibitory effect on electrically stimulated rat colon smooth muscle contraction. In this study, we investigated the signaling pathway of amitriptyline-induced inhibitory effect. Changes in isometric force of colon muscle were recorded on polygraph, and data were analyzed by measuring the inhibitory extent induced by amitriptyline. Firstly, muscles were contracted by stimulation with electric field stimulation (EFS), and then, amitriptyline was added cumulatively to determine its influence effect on EFS. Amitriptyline significantly inhibited EFS-induced contraction dose dependently. Then, the mechanism of inhibitory effect of amitriptyline was evaluated by pretreating with various antagonists such as L-NAME, methylene blue, atropine, 5-HT receptors blockers, guanethidine, prazosin, guanabenz, isoprenaline, Y27632 (Rho-kinase inhibitor), ML9 (myosin light chain kinase (MLCK) inhibitor), U73122 (PLC inhibitor), and chelerythrine (PKC inhibitor). Then, Ca(2+) channel blocker (nifedipine) and K(+)channel blockers, tetraethylammonium (TEA), 4-aminopyridine (4-AP), and glybenclamide, were used to determine the involvement of ion channels. L-NAME, guanabenz, 5HT4 receptor blocker, ML9, and Y27632 enhanced the effect of amitriptyline. Meanwhile, methylene blue, atropine, guanethidine, prazosin, methylsergide, ondansetron, U73122, and chelerythrine blocked its effect. It was also shown that nifedipine enhanced but TEA and glybenclamide blocked amitriptyline-induced inhibitory effect on EFS. Our results indicated that amitriptyline may exert inhibitory effect in response to EFS by inhibiting muscarinic receptors and then PLC-mediated PKC pathway leading to opening of ATP-sensitive potassium channel.

  6. Inhibitory Effect of Curcumin on Candida-albicans compared with Nystatin: an in-vitro Study

    Directory of Open Access Journals (Sweden)

    Neda Babaii

    2016-10-01

    Full Text Available Introduction: Curcumin is the active ingredient in the traditional herbal remedy and dietary spice turmeric (Curcuma longa. Curcumin has a surprisingly wide range of beneficial properties, including anti-inflammatory, antioxidant, chemopreventive and chemotherapeutic activity. on basis of recent studies; it has antifungal and antibacterial effects. The aim of this study was in-vitro evaluation of antifungal effect of curcumin on candida albicans and comparing it with nystatin. Methods: after preparing curcumin powder, 3 laboratory methods were used to evaluate antifungal effect. The first method was cell count technique, used to evaluate the amount of candida albicans after time, in different concentrations of curcumin in Dimethyl sulfoxide (DMSO. The second was cup bioassay, in which inhibitory a zone of curcumin in DMSO was evaluated in sabouraud culture plates; and in third method, inhibitory zones of dried disks; which contained curcumin in DMSO were evaluated. Results: the result of all three methods showed that curcumin has antifungal effect and this effect increases in more concentrations. Conclusion: curcumin has apparent and dose dependent antifungal effect on candida albicans.

  7. Clinical considerations for an effective medical therapy in Wilson's disease.

    Science.gov (United States)

    Weiss, Karl Heinz; Stremmel, Wolfgang

    2014-05-01

    Wilson's disease is an autosomal recessively inherited copper overload disorder that leads to hepatic and/or neurologic symptoms. More than a century after the first description of Wilson's disease, the available medical treatment options have not been standardized. The efficacy of the commonly used drugs is satisfactory for hepatic disease, but disappointing in the neurologic patients, including the risk of neurologic deterioration after the initiation of chelation therapy. An approach to overcome this problem is the careful and systematic assessment of biochemical response patterns and the quantitative monitoring of symptoms using validated rating scales. Standardized dosage strategies that address changes in copper pools might improve adherence and reduce side effects. Such an approach may reduce long-term morbidity. In this paper, we discuss considerations for an effective medical treatment and requirements for future studies in Wilson's disease.

  8. Inhibitory effects of genistein and resveratrol on guinea pig gallbladder contractility in vitro

    Institute of Scientific and Technical Information of China (English)

    Long-De Wang; Xiao-Qing Qiu; Zhi-Feng Tian; Ying-Fu Zhang; Hong-Fang Li

    2008-01-01

    AIM:To observe and compare the effects of phytoestrogen genistein,resveratrol and 17β-estradiol on the tonic contraction and the phasic contraction of isolated gallbladder muscle strips and to study the underlying mechanisms.METHODS:Isolated strips of gallbladder muscle from guinea pigs were suspended in organ baths containing Kreb's solution,and the contractilities of strips were measured before and after incubation with genistein,resveratrol and 17β-estradiol respectively.RESULTS:Similar to 17β-estradiol,genistein and resveratrol could dose-dependently inhibit the phasic contractile activities,they decreased the mean contractlie amplitude and the contractlie frequencies of gallbladder muscle strips,and also produced a marked reduction in resting tone.The blocker of estrogen receptor ICI 182780 failed to alter the inhibitory effects induced by genistein and resveratrol,but potassium bisperoxo(1,10 phenanthroline)oxovanadate bpV(phen),a potent protein tyrosine phosphatase inhibitor,markedly attenuated the inhibitory effects induced by genistein and resveratrol.In calcium-free Kreb's solution containing 0.01 mmol/L egtazic acid(EGTA),genistein and resveratrol inhibited the first phasic contraction induced by acetylcholine(Ach),but did not affect the second contraction induced by CaCl2.In addition,genistein,resveratrol and 17β-estradiol also could reduce the contractile responses of Ach and KCI,and shift their cumulative concentration-response curves rightward.CONCLUSION:Phytoestrogen genistein and resveratrol can directly inhibit the contractile activity of isolated gallbladder muscle both at rest and in response to stimulation.The mechanisms responsible for the inhibitory effects probably due mainly to inhibition of tyrosine kinase,Ca2+ influx through potential-dependent calcium channels(PDCs)and Ca2+ release from sarcoplasmic reticulum(SR),but were not related to the estrogen receptors.

  9. The inhibitory effects of Silso-San-Gami on atherosclerosis in KHC rabbits.

    Science.gov (United States)

    Park, Won-Hwan; Shin, Sang-Seub; Lee, Young-Choon; Kim, Cheorl-Ho

    2004-01-01

    Silsosangami is a dried decoction of a mixture of seven Korean herbal medicines, consisting of Typhae pollen, Pteropi faeces, Paeoniae radicis rubra, Cnidii rhizoma, Persicae semen, Carthami flos, and Curcumae tuber. The inhibitory effect of this traditional herbal medicine, Silsosangami-water extract (SSG), on the progression of the atherosclerotic diseases was examined using the spontaneous familial hypercholesterolemia (FH) model, Kurosawa and Kusanagi-hypercholesterolemic (KHC) rabbits. Changes in blood chemistry, pathology and low-density lipoprotein (LDL) oxidation were measured in a control group and a SSG-administrated group. In the control group, the area of atheromatous aortic plaques progressed between 4 weeks (30.43%) and 8 weeks (47.48%). This progressin of atherosclerotic disease was not observed in the SSG-treated group between 4 weeks (22.65%) and 8 weeks (23.23%). Antioxidative effects on LDL were observed in the SSG group at 12 and 14 weeks. SSG improved hypercholestrolemia in the KHC rabbits. These results suggest that SSG has inhibitory effects on the development of atheromatous plaques in spontaneous FH model rabbits. The antioxidative effects of SSG on LDL appear to be the source of the beneficial effects observed in this study.

  10. Inhibitory effects of 1-methyl-4-phenylpyridinium on glutamate uptake into cultured C6 glioma cells

    Institute of Scientific and Technical Information of China (English)

    Hong-hong YAO; Jian-hua DING; Hai-rong HE; Gang HU

    2004-01-01

    To investigate the effect of 1-methyl-4-phenylpyridinium (MPP+) on the glutamate uptake into cultured C6glioma cells. METHODS: The glutamate uptake into C6 glioma cells was measured by radio-ligand binding assay method. The effect of MPP+ on the morphology of C6 glioma cells was observed under phase contrast microscopy;apoptosis of C6 glioma cells were measured by FITC-labeled Annexin V staining and flow cytometry. Cell viability was measured by MTT method. RESULTS: MPP+ inhibited glutamate uptake into C6 glioma cells. However,MPP+ failed to induce any morphological changes of C6 glioma cells, and exposure to MPP+ had no effect on the viability and the apoptotic percentage of C6 glioma cells. Incubation with 12-O-tetradecanoylphorbol -13-acetate (TPA), a protein kinase C activator, caused a significant increase in glutamate uptake and completely reversed MPP+-induced inhibitory effect on glutamate uptake. CONCLUSION: The present results indicate that glutamate transporters may have important pathogenetic implications in Parkinson disease. MPP+-induced inhibition of glutamate uptake was due to the dysfunction of glutamate transporters; TPA enhanced glutamate uptake and completely reversed the inhibitory effect of MPP+.

  11. Inhibitory effect of Lactobacillus rhamnosus on pathogenic bacteria isolated from women with bacterial vaginosis

    Directory of Open Access Journals (Sweden)

    Gita Eslami

    2014-06-01

    Full Text Available Background: Considering the high prevalence of bacterial vaginosis and its association with urinary tract infection in women and treatment of gynecologic problems occur when a high recurrence of bacterial vaginosis is often treated with antibiotics. The purpose of this study is to investigate the inhibitory effect of Lactobacillus rhamnosus on pathogenic bacteria isolated from women with bacterial vaginosis, respectively.Materials and Methods: 96 samples from women with bacterial vaginosis discharge referred to health centers dependent Shahid Beheshti University in 91-92 were taken by a gynecologist with a dacron swab and put in sterile tubes containing TSB broth and Thioglycollate broth and were immediately sent to the lab location in cold chain for the next stages of investigation. From Thioglycollate and TSB medium was cultured on blood agar and EMB and Palkam and Differential diagnosis environments, and then incubated for 24 h at 37°C. Strains of Lactobacillus rhamnosus were cultured in MRSA environment and were transfered to the lab. After purification of pathogenic bacteria, MIC methods and antibiogram, Lactobacillus rhamnosus inhibitory effect on pathogenic bacteria is checked. Statistical analysis was done by SPSS software v.16.Results: The results of this study show the inhibitory effect of Lactobacillus rhamnosus on some pathogenic bacteria that cause bacterial vaginosis, including Staphylococcus aureus, Staphylococcus epidermidis, Staphylococcus saprophyticus, Streptococcus agalactiae, Entrococcus, Listeria monocytogenes and E.Coli. Microscopic examination of stained smears of the large number of Lactobacillus and pathogenic bacteria showed reduced. The prevalence of abnormal vaginal discharge, history of drug use means of preventing pregnancy and douching, respectively, 61%, 55%, 42% and 13% respectively. Significant difference was observed between the use and non-use of IUD in women with bacterial vaginosis infection

  12. Inhibitory effect of kaolin minerals compound against hepatitis C virus in Huh-7 cell lines.

    Science.gov (United States)

    Ali, Liaqat; Idrees, Muhammad; Ali, Muhammad; Hussain, Abrar; Ur Rehman, Irshad; Ali, Amjad; Iqbal, Syed Abbas; Kamel, Eyad Hassan

    2014-04-17

    Hepatitis C virus (HCV) is estimated to infect 200 million individuals in the globe, including approximately 10 million in Pakistan causing both acute and chronic hepatitis. The standard treatment against HCV is pegylated interferon therapy in combination with a nucleoside analogue ribavirin. In addition, several herbal extracts and phytochemicals derivatives are used traditionally in the treatment of liver diseases as well as HCV infection. The present study determines the inhibitory effect of kaolin minerals compound against hepatitis C virus in Huh-7 cell lines. Huh-7 cell lines were used for the in vitro HCV replication by using HCV positive sera from different patients with known HCV genotypes and viral titer/load. Total RNA was extracted from these infected cells and was quantified by real-time polymerase chain reaction (Real-time PCR). The viral titer was compared with the control samples to determine the anti-HCV activity of kaolin derived compounds. Kaolin is a group of clay minerals, with the chemical composition Al2 Si2O5 (OH)4. The results showed promising effectiveness of local kaolin derived anti-HCV compounds by causing 28% to 77% decrease in the HCV titer, when applied to infected Huh-7 cell lines. This study provides the basis for future work on these compounds especially to determine the specific pathway and mechanism for inhibitory action in the replicon systems of viral hepatitis. Kaolin mineral derivatives show promising inhibitory effects against HCV genotypes 3a and 1a infection, which suggests its possible use as complementary and alternative medicine for HCV viral infection.

  13. Inhibitory effects of Aphanizomenon flos-aquae constituents on human UDP-glucose dehydrogenase activity.

    Science.gov (United States)

    Scoglio, Stefano; Lo Curcio, Valeria; Catalani, Simona; Palma, Francesco; Battistelli, Serafina; Benedetti, Serena

    2016-12-01

    The purpose of this study was to investigate the in vitro inhibitory effects of the edible microalga Aphanizomenon flos-aquae (AFA) on human UDP-α-d-glucose 6-dehydrogenase (UGDH) activity, a cytosolic enzyme involved both in tumor progression and in phytochemical bioavailability. Both the hydrophilic and ethanolic AFA extracts as well as the constitutive active principles phycocyanin (PC), phycocyanobilin (PCB) and mycosporine-like amino acids (MAAs) were tested. Among AFA components, PCB presented the strongest inhibitory effect on UGDH activity, acting as a competitive inhibitor with respect to UDP-glucose and a non-competitive inhibitor with respect to NAD(+). In preliminary experiments, AFA PCB was also effective in reducing the colony formation capacity of PC-3 prostate cancer cells and FTC-133 thyroid cancer cells. Overall, these findings confirmed that AFA and its active principles are natural compounds with high biological activity. Further studies evaluating the effects of AFA PCB in reducing tumor cell growth and phytochemical glucuronidation are encouraged.

  14. Experimental Study on the Inhibitory Effects of Verapamil on the Proliferation of Meningiomas Cells

    Institute of Scientific and Technical Information of China (English)

    CHEN Jian; ZHANG Hongtao; WANG Heping

    2007-01-01

    In order to investigate the effects of verapamil on the proliferation of meningiomas cells in vitro and in vivo, the cultured meningiomas cells were cultured with verapamil at different concentrations for 24 h and the inhibitory effects of verapamii on cell proliferation were observed by MTT method. The meningiomas model was established by implanting the newly removed tumor fragments into the nude mice subcutaneously. The nude mice with tumors were divided into two groups: verapamil-treated group and control group. Tumor volumes were measured and after 12 weeks the tumors were taken out and examined histologically. The expression of proliferating cell nuclear antigen (PCNA) in the tumors was detected by using immunohistochemistry. It was found that verapamil could inhibit the growth of cultured meningiomas cells in a concentration-dependant manner. The inhibitory effect could be observed in the concentration of 1 μmol/L verapamil and the most obvious effects appeared in the concentration of 100 μmol/L. Tumor volume in the verapamiltreated group was obviously smaller than that in the control group (211.40±5.50 vs 163.94±3.62, P<0.01) and theexpression of PCNA was also lower (1.52±0.24 vs 2.86±0.53, P<0.05). Tumor inhibition rate was about 22.45%. It was suggested that verapamil could inhibit the proliferation and growth of meningiomas cells in vitro and in vivo.

  15. Inhibitory effects of jujuboside A on EEG and hippocampal glutamate in hyperactive rat

    Institute of Scientific and Technical Information of China (English)

    LU Ying-jun; ZHOU Jun; ZHANG Shao-min; ZHANG Heng-yi; ZHENG Xiao-xiang

    2005-01-01

    In this study, the inhibitory effect ofjujuboside A (JuA) on a penicillin sodium (Na-PCN) induced hyperactivity model was investigated. Cortical EEG (electroencephalogram) and the concentration of hippocampal Glutamate (Glu) were monitored simultaneously in vivo as indicators of rat's excitatory state. Power spectral density (PSD) and gravity frequency of PSD were calculated. JuA (0.05 g/L and 0.1 g/L) inhibited the EEG excitation effect caused by Na-PCN by increasing the power of δ1 and δ2bands (P<0.01 vs model) and lowering the gravity frequency of PSD (P<0.01 vs model). JuA also remarkably reduced the Glu elevation induced by Na-PCN (P<0.05 vs model). Diazepam also depressed Glu concentration and lowered the gravity frequency,but it showed a different EEG pattern in increased β2-activity (P<0.01 vs model). EEG excitation caused by Na-PCN correlated with Glu elevation during the first hour. Neurophysiological inhibitory effects of JuA and diazepam were more persistent than their Glu inhibitoty effects.

  16. Mechanistic Study of the Inhibitory Effect of Kaempferol on Uterine Fibroids In Vitro.

    Science.gov (United States)

    Li, Yanxia; Ding, Zhaoxia; Wu, Chuanzhong

    2016-12-08

    BACKGROUND This study examined the effect of kaempferol on uterine fibroids in vitro and the underlying mechanism, and investigated the potential of kaempferol as a clinical drug for the treatment of uterine fibroids. MATERIAL AND METHODS Uterine fibroid tissue and surrounding smooth muscle tissue were collected for primary culture. Different concentrations of kaempferol (12 μM, 24 μM, and 48 μM) were used to treat the cells for 24, 48, and 72 hours. Ethanol was used in the control group. A CCK-8 colorimetric assay was used to detect cell proliferation. Real-time PCR and immunoblot were used to detect estrogen receptor (ER), insulin-like growth factor-1 (IGF-1), and vascular endothelial growth factor (VEGF) levels in mRNA and protein. RESULTS The differences in proliferation at different time points and concentrations of kaempferol were statistically significant. The inhibitory effect of kaempferol on mRNA levels of ER and IGF, and protein levels of ER, VEGF, and IGF-1 were positively correlated with kaempferol concentration. Changes in kaempferol concentration showed no effect on VEGF mRNA expression. Treatment with kaempferol significantly lowered myocardin levels in uterine fibroid tissue compared to normal uterine smooth muscle (PKaempferol might be used for clinical treatment of uterine fibroids due to its inhibitory effect on the proliferation of uterine fibroids cells.

  17. Inhibitory Effect of Chrysanthemum zawadskii Herbich var. latilobum Kitamura Extract on RANKL-Induced Osteoclast Differentiation

    Directory of Open Access Journals (Sweden)

    Dong Ryun Gu

    2013-01-01

    Full Text Available Chrysanthemum zawadskii Herbich var. latilobum Kitamura, known as “Gujulcho” in Korea, has been used in traditional medicine to treat various inflammatory diseases, including rheumatoid arthritis. However, these effects have not been tested on osteoclasts, the bone resorbing cells that regulate bone metabolism. Here, we investigated the effects of C. zawadskii Herbich var. latilobum Kitamura ethanol extract (CZE on osteoclast differentiation induced by treatment with the receptor activator of NF-κB ligand (RANKL. CZE inhibited osteoclast differentiation and formation in a dose-dependent manner. The inhibitory effect of CZE on osteoclastogenesis was due to the suppression of ERK activation and the ablation of RANKL-stimulated Ca2+-oscillation via the inactivation of PLCγ2, followed by the inhibition of CREB activation. These inhibitory effects of CZE resulted in a significant repression of c-Fos expression and a subsequent reduction of NFATc1, a key transcription factor for osteoclast differentiation, fusion, and activation in vitro and in vivo. These results indicate that CZE negatively regulates osteoclast differentiation and may be a therapeutic candidate for the treatment of various bone diseases, such as postmenopausal osteoporosis, rheumatoid arthritis, and periodontitis.

  18. Increasing Pain Sensation Eliminates the Inhibitory Effect of Depression on Evoked Pain in Rats

    Science.gov (United States)

    Wang, Ning; Li, Sheng-Guang; Lin, Xiao-Xiao; Su, Yuan-Lin; Qi, Wei-Jing; Wang, Jin-Yan; Luo, Fei

    2016-01-01

    Although previous studies have suggested that depression may be associated with inhibition of evoked pain but facilitation of spontaneous pain, the mechanisms underlying these relationships are unclear. The present study investigated whether the difference between evoked and spontaneous pain on sensory (descending inhibition) and affective (avoidance motivation) components contributes to the divergent effects of depression on them. Depressive-like behavior was produced in male Wistar rats by unpredictable chronic mild stress (UCMS). Tone-laser conditioning and formalin-induced conditioned place avoidance (F-CPA) were used to explore avoidance motivation in evoked and spontaneous pain, respectively. Behavioral pharmacology experiments were conducted to examine descending inhibition of both evoked (thermal stimulation) and spontaneous pain behavior (formalin pain). The results revealed that the inhibitory effect of depression on evoked pain was eliminated following repeated thermal stimuli. Avoidance behavior in the tone-laser conditioning task was reduced in UCMS rats, relative to controls. However, avoidance motivation for formalin pain in the UCMS group was similar to controls. 5-HT1A receptor antagonism interfered with inhibition of pain responses over time. The present study demonstrated that the inhibitory effect of depression on evoked pain dissipates with increased nociception and that the sensory-discriminative and affective-motivational components of pain are jointly involved in the divergent effects of depression on pain. PMID:27733820

  19. Inhibitory effects of arabitol on caries-associated microbiologic parameters of oral Streptococci and Lactobacilli.

    Science.gov (United States)

    Loman, Abdullah Al; Ju, Lu-Kwang

    2015-12-01

    The aim of this study was to compare arabitol with its better studied isomer xylitol for their inhibitory effects on cell growth and acid production of oral bacteria. Streptococcus mutans, Streptococcus salivarius and Streptococcus sobrinus were used as representatives of oral streptococci and Lactobacillus acidophilus and Lactobacillus fermentum were used for oral lactobacilli. Growth was followed by measuring the absorbance at 660nm, acid production by pH change. Sensitivity of these oral bacteria to arabitol and xylitol was first compared at 1% (65mM) additive concentration with glucose as sugar substrate. For all bacteria tested, the inhibitory effects of the two polyols were comparable; both were significantly stronger on streptococci (with 20-60% inhibition) than on lactobacilli (with 5-10% inhibition). Effects of arabitol and xylitol were also compared for S. mutans and S. salivarius in media with 1% of different sugar substrates: glucose (55mM), fructose (55mM), galactose (55mM) and sucrose (30mM). Inhibition occurred for all sugars: stronger on glucose and galactose (60-65%) than on fructose and sucrose (40-45%). Inhibition dependency on the arabitol/xylitol concentration from 0.01% (0.65mM) to 2% (130mM) was further determined for S. mutans and S. salivarius. Regardless of the concentration, sugar substrate and bacterial species tested, arabitol showed very similar inhibition effects to its isomer xylitol.

  20. The Inhibitory Effect of Haloxylon salicornicum on Contraction of the Mouse Uterus

    Directory of Open Access Journals (Sweden)

    Nabila H. Saleem

    2013-01-01

    Full Text Available Haloxylon salicornicum (H. salicornicum is a plant that is frequently taken as a tea by Bedouin women in Egypt who are experiencing difficulties during pregnancy, as well as to provide relief from dysmenorrhoea. Despite its medical use, there has been no detailed evaluation of the effect of this plant on uterine tissue. Therefore, the initial aim of this study was to determine whether H. salicornicum affected the contraction of the mouse uterus in vitro. The crude aqueous extract of H. salicornicum was found to inhibit the spontaneous contractions of the uterus, with the effect being rapid in onset and completely reversible upon washout. Subsequent purification of the plant extract resulted in the identification of synephrine and N-methyltyramine, both of which were found to have inhibitory effects on the spontaneous contractions of the uterus. The EC50 for the purified constituent identified as synephrine was 0.82 ± 0.24 μg/mL. The inhibitory activity of crude H. salicornicum, as well as the isolated constituents, could be prevented by pretreatment of the uterus with the β-adrenoceptor antagonist propranolol. In conclusion, the use of H. salicornicum during preterm labour appears to be justified, and its pharmacologic effect is consistent with it acting as a β-adrenoceptor agonist.

  1. Inhibitory effect of melatonin on testosterone synthesis is mediated via GATA-4/SF-1 transcription factors.

    Science.gov (United States)

    Qin, Fenju; Zhang, Jie; Zan, Linsen; Guo, Weiqiang; Wang, Jin; Chen, Lili; Cao, Yi; Shen, Ouxi; Tong, Jian

    2015-11-01

    The aim of the present study was to elucidate whether the GATA-4/SF-1 signalling pathway is involved in the inhibitory effects of melatonin on testosterone production in both the TM3 Leydig cell line and in C57BL/6J mice. In-vitro experiments demonstrated that melatonin treatment significantly reduced testosterone levels in cell culture medium (P SF-1 (NR5A1), StAR, P450SCC (CYP11A1) and 3β-HSD (P SF-1 (P SF-1 expression.

  2. [The inhibitory effects of antioxidant vitamins on serum oxLDL and experimental atherosclerosis of rabbits].

    Science.gov (United States)

    Chen, D; Yang, T; Song, F; Ruan, G; Liu, S

    1997-12-01

    In order to study the inhibitory effects of antioxidant vitamins on serum (low oxidative density lipoproteins, oxLDL) and experimental atherosclerosis in rabbits, 20 rabbits were fed on cholesterol rich diet and antioxidant vitamins (vitamin E, vitamin C and beta carotene) for 12 weeks. oxLDL were tested by ELISA at the beginning of experiment and after 4 weeks 8 weeks. The results showed that supplement of antioxidant vitamins can decrease the oxLDL level significantly and inhibited development of atherosclerosis lesion around aorta in rabbits.

  3. Inhibitory effect of mycoplasma-released arginase. Activity in mixed-lymphocyte and tumour cell cultures

    DEFF Research Database (Denmark)

    Claesson, M H; Tscherning, T; Nissen, Mogens Holst

    1990-01-01

    Non-fermenting mycoplasma species deplete culture media for arginine through arginase activity linked to their arginine deiminase pathway, resulting in proliferation arrest and cell death in mycoplasma-contaminated cell cultures. The presence of only 2-3 Mycoplasma (M.) arginini-contaminated T...... inhibition can be reversed by addition of excess arginine to the culture medium. Antisera raised against non-fermenting, but not against fermenting, mycoplasma species block the inhibitory effect of MAE. SDS-PAGE separation of MAE disclosed a broad band at 60 kDa which contained arginase activity when...

  4. Inhibitory Effect of Nisin on Listeria monocytogenes Inoculated into Surimi and Minced Meat

    Directory of Open Access Journals (Sweden)

    Masoud Rezaei

    2012-02-01

    Full Text Available Background & Objective: Listeria monocytogenes has already established as an important food born pathogen which induce listeriosis in human. Use of bacteriocins to provide food safety has been increased dramatically. Nisin has a wide spectrum inhibitory effect than the other bacteriocins and inhibits food-borne pathogens such as L. monocytogenes and many other Gram-positive spoilage microorganisms. The purpose of this study was to investigate the inhibitory effect of Nisin on population of Listeria monocytogenes and the role of changes in food components on the antilisterial properties of Nisin. Materials & Methods: The minced meat and surimi samples were inoculated by 1×104 cfu/g of L. monocytogenes. Then samples exposed to Nisin at the levels of 500 or 1000 IU/g were prepared. All treatments after packaging in plastic bags were kept for 12 days at refrigerator temperature. Samples were cultured on CHROMagarTM Listeria every 2 days and the number of listeria monocytogenes was counted. Results: two different concentrations of Nisin (500 or 1000 IU/g was not able to inhibit L. monocytogenes below the acceptable level for raw food (100 cells per g in minced meat and surimi of silver carp. But the number of bacteria reduces more in fish surimi as compared to the mince meal. Also, antilisterial activity of Nisin was reduced during the storage period. Conclusion: Inhibitory property of Nisin against L. monocytogenes in surimi significantly was higher than the minced (P<0.05. So it is possible the antilisterial properties of Nisin will increase by elimination of some enzymes during processing.

  5. The Inhibitory Effect of Oridonin on the Growth of Fifteen Human Cancer Cell Lines

    Institute of Scientific and Technical Information of China (English)

    Junhui Chen; Shaobin Wang; Dongyang Chen; Guisheng Chang; Qingfeng Xin; Shoujun Yuan; Zhongying Shen

    2007-01-01

    OBJECTIVE To study the inhibitory effect of oridonin on the growth of cancer cells.METHODS Fifteen human cancer cell lines were subjected to various concentrations of oridonin in culture medium.The inhibitory rate of cell growth was measured by the MTT assay.and compared with a negative control and 5-Fu-positive control.RESULTS The 50% inhibiting concentration (IC50) and maximal inhibi tion (Imax) of oridonin shown by studying the growth of the cancer cell lines were as follows:leukemias (HL60 cells:3.9 μg/ml and 73.8%.K562 cells:4.3 μg/ml and 76.2%):esophageal cancers (SHEEC cells:15.4 μg/ml and 99.2%,Eca109 cells:15.1 μg/ml and 84.6%,TE1 cells:4.0 μg/ml and 70.2%):gastric cancers (BGC823 cells:7.6 μg/ml and 98.7%,SGC7901 cells:12.3 μg/ml and 85.7%):colon cancers (HT29 cells:13.6 μg/ml and 97.2%,HCT cells:14.5 μg/ml and 96.5%):liver cancers (Bel7402 cells:15.2 μg/ml and 89.2%,HepG2 cells:7.1 μg/ml and 88.3%):pancreatic cancer (PC3 cells:11.3 μg/ml and 68.4%):lung cancer (A549 cells:18.6 μg/ml and 98.0%):breast cancer (MCF7 cells:18.4 μg/ml and 84.7%):uterine cervix cancer (Hela cells:13.7μg/ml and 98.5%).CONCLUSION Oridonin had a relatively wide anti-tumor spectrum,and a relatively strong inhibitory effect on the growth of the 15 human cancer cells.Inhibitory effects were concentration dependent.

  6. Inhibitory effect of herpes simplex virus type 1 on type 2 virus replication.

    Science.gov (United States)

    Zelená, D; Roubal, J; Vonka, V

    1976-11-01

    Simultaneous infection with herpes simplex type I and type 2 viruses of chick embryo fibroblasts (CEF), which are only permissive for type 2 virus, or rabbit embryo fibroblasts (REF), which are permissive for both virus types, resulted in a marked reduction of type 2 virus production. This effect was dependent on the m.o.i. of type I, being expressed at a high rather than a low m.o.i. The rate of interference decreased with the prolongation of the interval between infection with type 2 and type I viruses. No evidence suggestive of interferon involvement was obtained. Partial inactivation of type 2 virus by ultraviolet irradiation enhanced the inhibitory effect of type I virus. On the other hand, u.v. irradiation of type I virus resulted in a progressive loss of inhibitory activity. The results of the present experiments suggest that a type I genome function is responsible for the interfering effect, and that an early step in the growth of type 2 virus is sensitive to the particular type I virus product involved.

  7. Role of histamine in the inhibitory effects of phycocyanin in experimental models of allergic inflammatory response

    Directory of Open Access Journals (Sweden)

    D. Remirez

    2002-01-01

    Full Text Available It has recently been reported that phycocyanin, a biliprotein found in the blue-green microalgae Spirulina, exerts anti-inflammatory effects in some animal models of inflammation. Taking into account these findings, we decided to elucidate whether phycocyanin might exert also inhibitory effects in the induced allergic inflammatory response and on histamine release from isolated rat mast cells. In in vivo experiments, phycocyanin (100, 200 and 300 mg/kg post-orally (p.o. was administered 1 h before the challenge with 1 μg of ovalbumin (OA in the ear of mice previously sensitized with OA. One hour later, myeloperoxidase activity and ear edema were assessed. Phycocyanin significantly reduced both parameters. In separate experiments, phycocyanin (100 and 200 mg/kg p.o. also reduced the blue spot area induced by intradermal injections of histamine, and the histamine releaser compound 48/80 in rat skin. In concordance with the former results, phyco-cyanin also significantly reduced histamine release induced by compound 48/80 from isolated peritoneal rat mast cells. The inhibitory effects of phycocyanin were dose dependent. Taken together, our results suggest that inhibition of allergic inflammatory response by phycocyanin is mediated, at least in part, by inhibition of histamine release from mast cells.

  8. The α-amylase and α-glucosidase inhibitory effects of Irish seaweed extracts.

    Science.gov (United States)

    Lordan, Sinéad; Smyth, Thomas J; Soler-Vila, Anna; Stanton, Catherine; Ross, R Paul

    2013-12-01

    To date, numerous studies have reported on the antidiabetic properties of various plant extracts through inhibition of carbohydrate-hydrolysing enzymes. The objective of this research was to evaluate extracts of seaweeds for α-amylase and α-glucosidase inhibitory effects. Cold water and ethanol extracts of 15 seaweeds were initially screened and from this, five brown seaweed species were chosen. The cold water and ethanol extracts of Ascophyllum nodosum had the strongest α-amylase inhibitory effect with IC50 values of 53.6 and 44.7 μg/ml, respectively. Moreover, the extracts of Fucus vesiculosus Linnaeus were found to be potent inhibitors of α-glucosidase with IC50 values of 0.32 and 0.49 μg/ml. The observed effects were associated with the phenolic content and antioxidant activity of the extracts, and the concentrations used were below cytotoxic levels. Overall, our findings suggest that brown seaweed extracts may limit the release of simple sugars from the gut and thereby alleviate postprandial hyperglycaemia. Copyright © 2013. Published by Elsevier Ltd.

  9. Inhibitory Effects of Spices on Biogenic Amine Accumulation during Fish Sauce Fermentation.

    Science.gov (United States)

    Zhou, Xuxia; Qiu, Mengting; Zhao, Dandan; Lu, Fei; Ding, Yuting

    2016-04-01

    The presence of high levels of biogenic amines is detrimental to the quality and safety of fish sauce. This study investigated the effects of ethanol extracts of spices, including garlic, ginger, cinnamon, and star anise extracts, in reducing the accumulation of biogenic amines during fish sauce fermentation. The concentrations of biogenic amines, which include histamine, putrescine, tyramine, and spermidine, all increased during fish sauce fermentation. When compared with the samples without spices, the garlic and star anise extracts significantly reduced these increases. The greatest inhibitory effect was observed for the garlic ethanolic extracts. When compared with controls, the histamine, putrescine, tyramine, and spermidine contents and the overall biogenic amine levels of the garlic extract-treated samples were reduced by 30.49%, 17.65%, 26.03%, 37.20%, and 27.17%, respectively. The garlic, cinnamon, and star anise extracts showed significant inhibitory effects on aerobic bacteria counts. Furthermore, the garlic and star anise extracts showed antimicrobial activity against amine producers. These findings may be helpful for enhancing the safety of fish sauce.

  10. The effects of inhibitory control training for preschoolers on reasoning ability and neural activity.

    Science.gov (United States)

    Liu, Qian; Zhu, Xinyi; Ziegler, Albert; Shi, Jiannong

    2015-09-23

    Inhibitory control (including response inhibition and interference control) develops rapidly during the preschool period and is important for early cognitive development. This study aimed to determine the training and transfer effects on response inhibition in young children. Children in the training group (N = 20; 12 boys, mean age 4.87 ± 0.26 years) played "Fruit Ninja" on a tablet computer for 15 min/day, 4 days/week, for 3 weeks. Children in the active control group (N = 20; 10 boys, mean age 4.88 ± 0.20 years) played a coloring game on a tablet computer for 10 min/day, 1-2 days/week, for 3 weeks. Several cognitive tasks (involving inhibitory control, working memory, and fluid intelligence) were used to evaluate the transfer effects, and electroencephalography (EEG) was performed during a go/no-go task. Progress on the trained game was significant, while performance on a reasoning task (Raven's Progressive Matrices) revealed a trend-level improvement from pre- to post-test. EEG indicated that the N2 effect of the go/no-go task was enhanced after training for girls. This study is the first to show that pure response inhibition training can potentially improve reasoning ability. Furthermore, gender differences in the training-induced changes in neural activity were found in preschoolers.

  11. Some dipeptides reverse the inhibitory effect of GABA on /sup 35/S-TBPS binding

    Energy Technology Data Exchange (ETDEWEB)

    Squires, R.F.; Saederup, E.

    1987-05-01

    All known GABA-A receptor blocker reverse the inhibitory effect of GABA on /sup 35/S-t-butylphosphorothionate (TBPS) binding to rat brain membranes in vitro. This system has already been used to identify several novel GABA antagonists. The authors now report that 12 out of 52 dipeptides tested (all containing L-amino acids), at 1 mM, significantly reverse the inhibitory effect of 1 ..mu..M GABA, which inhibits specific /sup 35/S-TBPS binding about 60%. Most of the active dipeptides contain an aromatic and a basic amino acid. Tryptophan usually conferred greater activity than phe or tyr, while arg usually conferred greater activity than lys or his. Several larger peptides containing the HFRW sequence found in ACTH were also GABA antagonists; ACTH(1-24), ACTH(1-18), ACTH(1-13), ACTH(4-10) and ..gamma..-MSH while ACTH(11-24) was inactive. The excitatory effects of these later peptides may be in part due to blockade of GABA-A receptors.

  12. Inhibitory Effect of Lactococcin BZ Against Listeria innocua and Indigenous Microbiota of Fresh Beef.

    Science.gov (United States)

    Yıldırım, Zeliha; Yerlikaya, Sabire; Öncül, Nilgün; Sakin, Tuba

    2016-09-01

    In this study, the effect of lactococcin BZ on microbiological quality of fresh beef is investigated. For this purpose, the meat samples were treated with various amounts of lactococcin BZ (200-2500 AU/mL), a bacteriocin produced by Lactococcus lactis spp. lactis BZ, and kept at 4-5 °C for 12 days. During storage, the microbiological properties of the meat samples with or without lactococcin BZ were determined. Inhibitory effect of lactococcin BZ depended on its amount. The higher the amount of lactococcin BZ, the higher the inhibitory activity. Treatment with lactococcin BZ at the level of 2500 AU/mL resulted in 4.87, 3.50 and 3.94 log cycle decrease in the counts of mesophilic, psychrotrophic and lactic acid bacteria, respectively, and 1.90·10(4) and 1.04·10(2) CFU/g reduction in coliform and faecal coliform bacteria, respectively, at the end of storage as compared to their initial numbers in the control sample. However, the counts of these bacteria in control samples increased during storage. Also, lactococcin BZ at 1600 AU/mL showed very strong antilisterial effect against Listeria innocua in fresh meat and reduced the cell numbers from 6.04 log CFU/g to undetectable level on the 6th day of storage. In conclusion, lactococcin BZ has a potential use as a biopreservation agent to improve safety and shelf life of raw beef.

  13. Inhibitory Effect of Lactococcin BZ Against Listeria innocua and Indigenous Microbiota of Fresh Beef

    Science.gov (United States)

    Yerlikaya, Sabire; Öncül, Nilgün; Sakin, Tuba

    2016-01-01

    Summary In this study, the effect of lactococcin BZ on microbiological quality of fresh beef is investigated. For this purpose, the meat samples were treated with various amounts of lactococcin BZ (200–2500 AU/mL), a bacteriocin produced by Lactococcus lactis spp. lactis BZ, and kept at 4–5 °C for 12 days. During storage, the microbiological properties of the meat samples with or without lactococcin BZ were determined. Inhibitory effect of lactococcin BZ depended on its amount. The higher the amount of lactococcin BZ, the higher the inhibitory activity. Treatment with lactococcin BZ at the level of 2500 AU/mL resulted in 4.87, 3.50 and 3.94 log cycle decrease in the counts of mesophilic, psychrotrophic and lactic acid bacteria, respectively, and 1.90·104 and 1.04·102 CFU/g reduction in coliform and faecal coliform bacteria, respectively, at the end of storage as compared to their initial numbers in the control sample. However, the counts of these bacteria in control samples increased during storage. Also, lactococcin BZ at 1600 AU/mL showed very strong antilisterial effect against Listeria innocua in fresh meat and reduced the cell numbers from 6.04 log CFU/g to undetectable level on the 6th day of storage. In conclusion, lactococcin BZ has a potential use as a biopreservation agent to improve safety and shelf life of raw beef. PMID:27956863

  14. Inhibitory effects of Leucaena leucocephala on the metastasis and invasion of human oral cancer cells.

    Science.gov (United States)

    Chung, Hsiao-Hang; Chen, Mu-Kuan; Chang, Yu-Chao; Yang, Shun-Fa; Lin, Chia-Chieh; Lin, Chiao-Wen

    2017-02-09

    Oral cancer is one of the most common cancers worldwide, and metastasis is recognized as a major factor causing its low survival rate. The inhibition of metastasis progress and the improvement of the survival rate for oral cancer are critical research objectives. Leucaena leucocephala from the mimosa branch Leucaena genus is native to Central and South America and has been used as a traditional remedy for treating various disorders. Previous studies have demonstrated antioxidant, anti-inflammatory as well as anticancer properties of L. leucocephala plant materials. However, the molecular mechanism underlying the anticancer effect induced by L. leucocephala remains unclear. In this study, we investigated the effect of L. leucocephala extract (LLE) on SCC-9 and SAS oral cancer cells and examined the potential inhibitory mechanisms involved. The results indicated that LLE attenuated the migration and invasion abilities of both SCC-9 and SAS cells by reducing the activity and protein expression of matrix metalloproteinases-2 (MMP-2). Regarding mitogen-activated protein kinase (MAPK) pathways, the phosphorylation of ERK1/2 and p38 exhibited a significant inhibitory effect in the presence of LLE. The application of ERK inhibitor and p38 inhibitor confirmed that both signalling transduction pathways were involved in the inhibition of cell metastasis. These data indicate that L. leucocephala could be a potent therapeutic agent for the prevention and treatment of oral cancer and a prominent plant source for anticancer research in the future.

  15. Inhibitory effects of kale ingestion on metabolism by cytochrome P450 enzymes in rats.

    Science.gov (United States)

    Yamasaki, Izumi; Yamada, Masayoshi; Uotsu, Nobuo; Teramoto, Sachiyuki; Takayanagi, Risa; Yamada, Yasuhiko

    2012-01-01

    Kale (Brassica oleracea L. var acephala DC) is a leafy green vegetable belonging to the cabbage family (Brassicaceae) that contains a large amount of health-promoting phytochemicals. There are any reports about the effects of kale ingestion on the chemoprevention function and mechanism, but the interactions between kale and drugs have not been researched. We investigated the effects of kale intake on cytochrome P450 (CYP) metabolism by using cocktail probe drugs, including midazolam (for CYP3A4), caffeine (for CYP1A2), dextromethorphan (for CYP2D6), tolbutamide (for CYP2C9), omeprazole (for CYP2C19), and chlorzoxazone (for CYP2E1). Cocktail drugs were administered into rats treated with kale and cabbage (2000 mg/kg) for a week. The results showed that kale intake induced a significant increase in plasma levels and the AUC of midazolam, caffeine, and dextromethorphan. In addition, the plasma concentration and AUC of omeprazole tended to increase. Additionally, no almost differences in the mRNA expression levels of CYP enzymes in the liver were observed. In conclusion, kale ingestion was considered to have an inhibitory effect on the activities of CYP3A4, 1A2, 2D6, and 2C19 for a reason competitive inhibition than inhibitory changes in the mRNA expressions.

  16. Effects of nanosuspension and inclusion complex techniques on the in vitro protease inhibitory activity of naproxen

    Energy Technology Data Exchange (ETDEWEB)

    Dharmalingam, Senthil Rajan; Chidambaram, Kumarappan; Srinivasan, Ramamurthy; Nadaraju, Shamala, E-mail: dsenthilrajan@yahoo.co.in [School of Pharmacy, International Medical University, Bukit Jalil, Kuala Lumpur (Malaysia)

    2014-01-15

    This study investigated the effects of nanosuspension and inclusion complex techniques on in vitro trypsin inhibitory activity of naproxen—a member of the propionic acid derivatives, which are a group of antipyretic, analgesic, and non-steroidal anti-inflammatory drugs. Nanosuspension and inclusion complex techniques were used to increase the solubility and anti-inflammatory efficacy of naproxen. The evaporative precipitation into aqueous solution (EPAS) technique and the kneading methods were used to prepare the nanosuspension and inclusion complex of naproxen, respectively. We also used an in vitro protease inhibitory assay to investigate the anti-inflammatory effect of modified naproxen formulations. Physiochemical properties of modified naproxen formulations were analyzed using UV, IR spectra, and solubility studies. Beta-cyclodextrin inclusion complex of naproxen was found to have a lower percentage of antitryptic activity than a pure nanosuspension of naproxen did. In conclusion, nanosuspension of naproxen has a greater anti-inflammatory effect than the other two tested formulations. This is because the nanosuspension formulation reduces the particle size of naproxen. Based on these results, the antitryptic activity of naproxen nanosuspension was noteworthy; therefore, this formulation can be used for the management of inflammatory disorders. (author)

  17. Sub-inhibitory and post-antibiotic effects of spiramycin and erythromycin on Staphylococcus aureus.

    Science.gov (United States)

    Webster, C; Ghazanfar, K; Slack, R

    1988-07-01

    The antibacterial responses of clinical isolates of Staphylococcus aureus to spiramycin and erythromycin were compared. Conventional MICs showed erythromycin-sensitive strains to be 16-32 times less sensitive to spiramycin. MBCs were only four to eight times higher for spiramycin. Erythromycin resistant S. aureus were more frequently encountered. Concentrations of both macrolides at 1/4 MIC produced antibacterial effects. Post-antibiotic effects were more marked with spiramycin. After 3 h exposure to 4 x MIC of antibiotic the delay in regrowth of S. aureus was 5 h for erythromycin and 9 h for spiramycin. In a continuous cultivation model, spiramycin produced an inhibitory effect on S. aureus for 12 h whereas the effect of erythromycin was only apparent for 6 h. In conclusion, spiramycin is more active against staphylococci in vitro than would be expected by its modest MICs.

  18. Considerations for modeling thin cirrus effects via brightness temperature differences

    Science.gov (United States)

    Schmidt, E. O.; Arduini, R. F.; Wielicki, B. A.; Stone, R. S.; Tsay, S.-C.

    1995-01-01

    Brightness temperature difference (BTD) values are calculated for selected Geostationary Operational Environmental Satellite (GOES-6) channels (3.9, 12.7 micrometer) and Advanced Very High Resolution Radiometer channels (3.7, 12.0 micrometer). Daytime and nighttime discrimination of particle size information is possible given the infrared cloud extinction optical depth and the BTD value. BTD values are presented and compared for cirrus clouds composed of equivalent ice spheres (volume, surface area) versus randomly oriented hexagonal ice crystals. The effect of the hexagonal ice crystals is to increase the magnitude of the BTD values calculated relative to equivalent ice sphere (volume, surface area) BTDs. Equivalent spheres (volume or surface area) do not do a very good job of modeling hexagonal ice crystal effects on BTDs; however, the use of composite spheres improves the simulation and offers interesting prospects. Careful consideration of the number of Legendre polynomial coefficients used to fit the scattering phase functions is crucial to realistic modeling of cirrus BTDs. Surface and view-angle effects are incorporated to provide more realistic simulation.

  19. Inhibitory effects of cryptoporus polysaccharide on airway constriction, eosinophil release, and chemotaxis in guinea pigs

    Institute of Scientific and Technical Information of China (English)

    Xiao-yan ZHAO; Qiang-min XIE; Ji-qiang CHEN; Chuan-kui KE

    2004-01-01

    AIM: To study effects of cryptoporus polysaccharide (CP) on antigen-induced bronchoconstriction, eosinophil peroxidase (EPO) release in vivo, and on platelet activating factor (PAF)-induced eosinophil chemotaxis in vitro in guinea pig. METHODS: The asthma model of guinea pig was formed with ovalbumin (OVA). The changes of lung resistance (RL) and dynamic lung compliance (Cdyn), EPO level in bronchoalveolar lavage fluids (BALF) and eosinophil migration were determined. RESULTS: Pretreatment of CP at doses of 3, 9, and 27 mg/kg by intragastric gavage (ig), qd for 10 d, inhibited early asthma response in a dose-dependent manner. Inhibitory rates of mean increase value from 1 to 30 min of RL were 34.8 %, 74.4 % (P<0.05), and 79.6 % (P<0.05), respectively. Inhibitory rate of mean reduction value of Cdyn were 22.9 %, 40.5 % (P<0.01), and 66.5 % (P<0.01), respectively.Pretreatment of CP at doses of 3, 9, and 27 mg/kg also inhibited late asthma response, and the reduction of EPO level in BALF were 3.1%, 16.9 % (P<0.01), and 20.1% (P<0.01), respectively. The inhibitory rates of CP at concentrations of 0.13, 1.3, 13, 130 nmol/L to eosinophil migration induced by PAF were 6.8 %, 17.2 % (P<0.05),29.6 % (P<0.01), and 35.9 % (P<0.01). CONCLUSION: CP protects lung against increase of RL and reduction of Cdyn, decreases EPO level in the asthma model, and inhibits eosinophil chemotaxis induced by PAF. The results suggest that CP may be a novel antiinflammatory agent for the treatment of asthma and allergic diseases.

  20. Inhibitory Effects of Colocasia esculenta (L. Schott Constituents on Aldose Reductase

    Directory of Open Access Journals (Sweden)

    Hong Mei Li

    2014-08-01

    Full Text Available The goal of this study was to determine the rat lens aldose reductase-inhibitory effects of 95% ethanol extracts from the leaves of C. esculenta and, its organic solvent soluble fractions, including the dichloromethane (CH2Cl2, ethyl acetate (EtOAc, n-butanol (BuOH and water (H2O layers, using dl-glyceraldehyde as a substrate. Ten compounds, namely tryptophan (1, orientin (2, isoorientin (3, vitexin (4, isovitexin (5, luteolin-7-O-glucoside (6, luteolin-7-O-rutinoside (7, rosmarinic acid (8, 1-O-feruloyl-d-glucoside (9 and 1-O-caffeoyl-d-glucoside (10 were isolated from the EtOAc and BuOH fractions of C. esculenta. The structures of compounds 1–10 were elucidated by spectroscopic methods and comparison with previous reports. All the isolates were subjected to an in vitro bioassay to evaluate their inhibitory activity against rat lens aldose reductase. Among tested compounds, compounds 2 and 3 significantly inhibited rat lens aldose reductase, with IC50 values of 1.65 and 1.92 μM, respectively. Notably, the inhibitory activity of orientin was 3.9 times greater than that of the positive control, quercetin (4.12 μM. However, the isolated compounds showed only moderate ABTS+ [2,29-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid] activity. These results suggest that flavonoid derivatives from Colocasia esculenta (L. Schott represent potential compounds for the prevention and/or treatment of diabetic complications.

  1. Naltrexone does not reverse the inhibitory effect of chronic restraint on gonadotropin secretion in the intact male rat.

    Science.gov (United States)

    González-Quijano, M I; Ariznavarreta, C; Martín, A I; Treguerres, J A; López-Calderón, A

    1991-11-01

    There is considerable evidence suggesting that endogenous opioids may play an important role in acute stress-induced decreases in luteinizing hormone (LH) release. Studies were undertaken to analyze the role of endogenous opioids in chronic stress-induced decrease in circulating LH and follicle-stimulating hormone (FSH). Chronic restraint (6 h daily over 4 days) evoked a decrease in circulating LH and FSH. Naltrexone treatment, (2 mg/kg three times daily) during the 4 days of restraint, caused an increase in plasma concentrations of LH and FSH, and antagonized the LH suppressory effect of morphine (10 mg/kg) administration. Despite this, naltrexone treatment was ineffective in preventing the inhibitory effect of chronic restraint stress on circulating LH and FSH. Chronic restraint also induced a decrease in hypothalamic LH-releasing hormone (LHRH) content in saline-treated rats. On the contrary, in naltrexone-treated rats, chronic restraint evoked an increase in hypothalamic LHRH content. Thus endogenous opioids and chronic stress seem to act by different mechanisms on the hypothalamic LHRH neuron. In unstressed orchidectomized rats, naltrexone administration did not modify circulating LH, but increased plasma concentrations of LH in acutely restrained rats. These data suggest that endogenous opioids may mediate gonadotropin secretion during acute stress, but not during chronic stress.

  2. Inhibitory effect of leflunomide on hepatic fibrosis induced by CC14 in rats

    Institute of Scientific and Technical Information of China (English)

    Hong-wei YAO; Jun LI; Ji-qiang CHEN; Shu-yun XU

    2004-01-01

    AIM: To study the effect of leflunomide on CCl4-induced hepatic fibrosis in rats. METHODS: Hepatic fibrosis was induced by subcutaneous injection with 50 % CCl4 in Sprague-Dawley rats. The amount of CCl4 administered was 1 mg/kg. The alanine aminotransferase (ALT), aspartate aminotransferase (AST), nitric oxide (NO) levels in plasma and hydroxyproline (Hyp) contents in liver tissue were assayed by spectrophotometry. The hyaluronic acid (HA) and procollagen III (PC III) were assessed by radioimmunoassay. The transforming growth factor-β1(TGF-β1) in serum was determined by ELISA. The nuclear factor-kappa B (NF-κB) in liver tissue was examined by immunohistochemistry. Liver samples collected after 12 weeks of CCl4 treatment were stained with hematoxylin and eosin. RESULTS: Leflunomide (1, 3, and 9 mg/kg) significantly decreased indices of liver and spleen, the serum transaminase (AST, ALT) activities, HA and PC III levels, and Hyp contents in liver tissue in rats of hepatic fibrosis. Histopathological examination showed leflunomide had inhibitory effect on fibrogenesis and formation of pseudolobulus. Furthermore, leflunomide significantly inhibited NF-κB expression in liver tissue, and reduced elevated serum TGF-β1 and NO levels in rats of hepatic fibrosis. CONCLUSION: Leflunomide showed inhibitory action on hepatic fibrosis induced by CC14 in rats.

  3. Inhibitory effect of oxymatrine on serum hepatitis B virus DNA in HBV transgenic mice

    Institute of Scientific and Technical Information of China (English)

    Lun-Gen Lu; Min-De Zeng; Yi-Min Mao; Jing-Yuan Fang; Yu-Lin Song; Zhao-Hui Shen; Ai-Ping Cao

    2004-01-01

    AIM: To study the inhibitory effect of oxymatrine on serum hepatitis B virus (HBV) DNA in HBV transgenic mice.METHODS: HBV transgenic mice model was established by microinjection, and identified by HBV DNA integration and replication. Transgenic mice with replicating HBV were divided into 3 groups, and injected with normal saline (group A, n=9), 50 mg/kg (group B, n=8) and 100 mg/kg (group C, n=9) oxymatrine intraperitoneally once a day for 30 d, respectively. Quantitation of serum HBV DNA in HBV transgenic mice was performed by competitive polymerase chain reaction (PCR) in combination with DNA hybridization quantitative detection technique before and after treatment.RESULTS: Compared with pre-treatment, the serum HBV DNA in group A (F=1.04, P=0.9612) and group B (F=1.13,P=0.8739) had no changes after treatment. However, in group C serum HBV DNA was significantly decreased (F=13.97,P=0.0012). The serum HBV DNA after treatment was lower in group C than in groups B and A (F=8.65, P=0.0068;F=12.35, P=0.0018; respectively). The serum HBV DNA after treatment was lower in group B than in group A, but there was no statistical significance (F=1.43, P=0.652).CONCLUSION: Oxymatrine has inhibitory effects on serum HBV DNA in HBV transgenic mice.

  4. Two new prenylflavonoids from Epimedii Herba and their inhibitory effects on advanced glycation end-products.

    Science.gov (United States)

    Nakashima, Keisuke; Miyashita, Hiroyuki; Yoshimitsu, Hitoshi; Fujiwara, Yukio; Nagai, Ryoji; Ikeda, Tsuyoshi

    2016-04-01

    Because inhibitors of advanced glycation end-products (AGEs), for example pyridoxamine, significantly inhibit the development of retinopathy and neuropathy in rats with streptozotocin-induced diabetes, treatment with AGE inhibitors is believed to be a potential strategy for the prevention of lifestyle-related diseases such as diabetic complications. In the present study, the MeOH extract of Epimedii Herba (EH; aerial parts of Epimedium spp.) was found to inhibit the formation of N (ε) -(carboxymethyl)lysine (CML) and N (ω) -(carboxymethyl)arginine (CMA) during incubation of collagen-derived gelatin with ribose. Furthermore, compounds with inhibitory effects against CML and CMA formation were isolated from EH. Two new prenylflavonoids (compounds 1 and 2) and two known compounds (3 and 4) were found to significantly inhibit the formation of both CML and CMA; compound 4 (epimedokoreanin B) had the strongest inhibitory effect of the isolated compounds. These data suggest that epimedokoreanin B could prevent clinical complications of diabetes by inhibiting AGEs.

  5. Inhibitory effect of the essential oil from Eugenia caryophyllata Thumb leaves on coalho cheese contaminating microorganisms

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    Vinicius Nogueira Trajano

    2010-12-01

    Full Text Available Coalho cheese (a firm but very lightweight cheese produced in Brazil is widely produced and consumed in the Brazilian Northeast and its production has been mainly related to small farmers. This food has been frequently characterized as having high microbial load posing a risk for the health of consumers. This study aimed to indentify the chemical compounds of the essential oil from Eugenia caryophyllata leaves; to evaluate the inhibitory effect of the oil against coalho cheese contaminating microorganisms; and to assess its efficacy in inhibiting the autochthonous microflora of the cheese during refrigerated storage. Eugenol (74% was found to be the most prevalent compound in the essential oil. Minimum Inhibitory Concentration (MIC and Minimum Cidal Concentration (MCC in laboratorial broth were in the range of 2.5-5 and 5-20 µg.mL-1, respectively. Vaccum packed coalho cheese added with 5, 10, and 20 µg.g-1 of oil showed a lower growth rate (like-static effect against mesophilic bacteria during the time intervals evaluated. On the other hand, 2.5-10 µg.g-1 of oil provided a prominent decrease toward fungi count in cheese samples during storage. These results reveal the interesting antimicrobial property of the essential oil from E. caryophyllata leaves against a range of coalho cheese-related microorganisms in laboratorial media and in food matrix.

  6. Experimental study on the inhibitory effect of MSCs on radiation-induced thymoma in mice

    Institute of Scientific and Technical Information of China (English)

    Wen-Long Zhang

    2016-01-01

    Objective:To study the inhibitory effect of MSCs on radiation-induced thymoma in mice. Methods:C57BL/6 mice were selected as the research objects, model group and MSCs group induced thymoma by radiation, and MSCs group received intravenous injection of mesenchymal stem cell for therapy. Six months after treatment, macroscopic morphology of thymus tissue, contents of T lymphocyte subsets as well as expression of tumor suppressor gene PTEN and proliferation marker molecule Ki-67 were detected.Results:(1) macroscopic morphology: thymus tissue weight of model group was significantly greater than that of control group and thymus tissue weight of MSCs group was lower than that of control group; (2) cells and molecules: compared with control group, contents of CD4-CD8-, CD4+CD8- and CD4-CD8+ T cells as well as expression of PTEN in thymus tissue of model group significantly decreased, and CD4+CD8+ T cell content as well as Ki-67 expression significantly increased; compared with model group, contents of CD4-CD8-, CD4+CD8- and CD4-CD8+ T cells as well as expression of PTEN in thymus tissue of MSCs group significantly increased, and CD4+CD8+ T cell content as well as Ki-67 expression significantly decreased.Conclusions:MSCs have inhibitory effect on radiation-induced thymoma in mice, manifested as promoting CD4+CD8- and CD4-CD8+ T cell maturation as well as inhibiting cell proliferation.

  7. Inhibitory Effects of Ginsenoside Rb1 on Apoptosis Caused by HSV-1 in Human Glioma Cells

    Institute of Scientific and Technical Information of China (English)

    Yuan-Yuan Liang; Bin Wang; Dong-Meng Qian; Ling Li; Zhi-Hao Wang; Ming Hu; Xu-Xia Song

    2012-01-01

    To investigate the inhibitory effects of Ginsenoside Rb1 (GRb1) on apoptosis caused by Herpes Simplex Virus-1 (HSV-1) in Human Glioma Cells (U251),U251 cells were infected by HSV-1 at a multiplicity of infection of 5 and GRb1,GRb1+HSV-1,HSV-1 and control groups.MTT and cell apoptosis assays were used to detect the inhibitory effects of GRbl on the apoptosis of U251 cells that caused by HSV-1 infection for various concentrations of drug and virus treatments by MTT assay.We found that in the 400 μg/mL GRbl and 400 μg/mL GRbl+HSV-1 groups,MTT values were higher than control group at all times (P<0.05).Moreover,the apoptosis rate in the 400 μg/mL GRb1+HSV-1 group was lower than the HSV-1 group (P<0.05).These results confirmed that,at appropriate concentrations,GRb 1 could inhibit nerve cell apoptosis in HSV-1 infections.

  8. Excitatory and inhibitory cholinergic effects of yohimbine on isolated guinea-pig small intestine.

    Science.gov (United States)

    Del Tacca, M; Tadini, P; Blandizzi, C; Bernardini, M C

    1988-08-01

    The interaction of yohimbine with the cholinergic intestinal system was investigated in the isolated guinea-pig ileum using a wide range of drug concentrations from 3 x 10(-13) to 2 x 10(-4) g/ml. Low concentrations of yohimbine (3 x 10(-13) to 3 x 10(-11) g/ml) caused dose-dependent contractions of the ileal longitudinal muscle, which were potentiated by eserine 1 x 10(-8) g/ml and prevented by tetrodotoxin 1 x 10(-6) g/ml or by atropine 1 x 10(-12) g/ml; methysergide and diphenydramine were ineffective up to 3 x 10(-7) g/ml dose. Submaximal stimulatory responses evoked by twitch stimulation or by acetylcholine were significantly potentiated by the same concentrations of yohimbine (3 x 10(-13) to 3 x 10(-11) g/ml) and blocked by atropine 1 x 10(-12) g/ml. By contrast, high concentrations of yohimbine (1 x 10(-6) to 2 x 10(-4) g/ml) displayed dose-dependent inhibitory effects on cholinergic responses. The stimulant effect of yohimbine seems to be indirect and mediated by the increase in the release of acetylcholine, while the inhibitory action may be due to a molecular interaction with the muscarinic receptors allowing non-specific receptor blockade.

  9. Inhibitory effects of Lactobacillus fermentum on microbial growth and biofilm formation.

    Science.gov (United States)

    Rybalchenko, Oxana V; Bondarenko, Viktor M; Orlova, Olga G; Markov, Alexander G; Amasheh, S

    2015-10-01

    Beneficial effects of Lactobacilli have been reported, and lactic bacteria are employed for conservation of foods. Therefore, the effects of a Lactobacillus fermentum strain were analyzed regarding inhibitory effects on staphylococci, Candida albicans and enterotoxigenic enterobacteria by transmission electron microscopy (TEM). TEM of bacterial biofilms was performed using cocultures of bacteriocin-producing L. fermentum 97 with different enterotoxigenic strains: Staphylococcus epidermidis expressing the ica gene responsible for biofilm formation, Staphylococcus aureus producing enterotoxin type A, Citrobacter freundii, Enterobacter cloaceae, Klebsiella oxytoca, Proteus mirabilis producing thermolabile and thermostable enterotoxins determined by elt or est genes, and Candida albicans. L. fermentum 97 changed morphological features and suppressed biofilm formation of staphylococci, enterotoxigenic enterobacteria and Candida albicans; a marked transition to resting states, a degradation of the cell walls and cytoplasm, and a disruption of mature bacterial biofilms were observed, the latter indicating efficiency even in the phase of higher cell density.

  10. Inhibitory effect of substituted dextrans on MCF7 human breast cancer cell growth in vitro.

    Science.gov (United States)

    Morere, J F; Letourneur, D; Planchon, P; Avramoglou, T; Jozefonvicz, J; Israel, L; Crepin, M

    1992-12-01

    Substituted dextrans can reproduce some of the properties of heparin and can thus be used to alter cellular growth. We studied the effect of heparin (H108), dextran (D), carboxymethylbenzylamide dextran (CMDB) and carboxymethylbenzylamide sulfonate dextran (CMDBS) on the growth of human mammary cells of the MCF7 tumor line. The cells were cultured in minimum Eagle's medium containing 2% fetal calf serum without biopolymer, or with increasing concentrations of H108, D, CMDB or CMDBS. Growth curves were accurately based on cell counting using a Coulter counter. Cell distribution in the various phases of the cycle was analyzed by flow cytometry. Dose-dependent growth inhibitory effects (400-4000 micrograms/ml) were observed. The effect on MCF7 tumor cells was most apparent with CMDBS. The percentage of cells in the S phase decreased with preferential blocking in the G0/G1 phase. Pre-clinical studies can be anticipated as there is an absence of in vivo toxicity.

  11. THE INHIBITORY EFFECT OF ASTRAGALUS MEMBRANACEUS ON COXSACKIE B-3 VIRUS RNA REPLICATION

    Institute of Scientific and Technical Information of China (English)

    彭天庆; 杨英珍; HelgaRiesemann; ReinhardKandolf

    1995-01-01

    Using mice infected with coxsackie B-3 virus (CVB3) as a viral myocarditis model,we observed the inhibitory effect of Astragalus membranaceus (AM) on CVB3-RNA replication in myocardial tissue of mice by RNA-RNA in situ hybridization with negative-strand RNA probes labelled with 35S and quantitative imaging analysis of positive signals.The mechanism of its effect on CVB3-RNA replication has been inves-tigated by detection of beta-interferon (β-IFN) as well.Results showed that the copy numbers of CVB3-RNA as well as the histologic scores (necrosis) in myocardial tissues of infected-AM treated mice were sig-nificantly lower than those in infected and normal saline treated mice,suggesting that AM could inhibit the replication of CVB3-RNA,but its effect on CVB3-RNA replication had no correlation with induction of β-IFN.

  12. Effective Assistive Technology Consideration and Implications for Diverse Students

    Science.gov (United States)

    Jones, Vita L.; Hinesmon-Matthews, Lezlee J.

    2014-01-01

    Often the consideration of assistive technology devices and services during the individualized education program (IEP) process is overlooked. Because the Individuals with Disabilities Education Act (IDEA) authorized this consideration, IEP team members must be keenly aware of the importance they hold in providing this valuable input. Thus, IEP…

  13. Cholecystokinin receptor-1 mediates the inhibitory effects of exogenous cholecystokinin octapeptide on cellular morphine dependence

    Directory of Open Access Journals (Sweden)

    Wen Di

    2012-06-01

    Full Text Available Abstract Background Cholecystokinin octapeptide (CCK-8, the most potent endogenous anti-opioid peptide, has been shown to regulate the processes of morphine dependence. In our previous study, we found that exogenous CCK-8 attenuated naloxone induced withdrawal symptoms. To investigate the precise effect of exogenous CCK-8 and the role of cholecystokinin (CCK 1 and/or 2 receptors in morphine dependence, a SH-SY5Y cell model was employed, in which the μ-opioid receptor, CCK1/2 receptors, and endogenous CCK are co-expressed. Results Forty-eight hours after treating SH-SY5Y cells with morphine (10 μM, naloxone (10 μM induced a cAMP overshoot, indicating that cellular morphine dependence had been induced. The CCK receptor and endogenous CCK were up-regulated after chronic morphine exposure. The CCK2 receptor antagonist (LY-288,513 at 1–10 μM inhibited the naloxone-precipitated cAMP overshoot, but the CCK1 receptor antagonist (L-364,718 did not. Interestingly, CCK-8 (0.1-1 μM, a strong CCK receptor agonist, dose-dependently inhibited the naloxone-precipitated cAMP overshoot in SH-SY5Y cells when co-pretreated with morphine. The L-364,718 significantly blocked the inhibitory effect of exogenous CCK-8 on the cAMP overshoot at 1–10 μM, while the LY-288,513 did not. Therefore, the CCK2 receptor appears to be necessary for low concentrations of endogenous CCK to potentiate morphine dependence in SH-SY5Y cells. An additional inhibitory effect of CCK-8 at higher concentrations appears to involve the CCK1 receptor. Conclusions This study reveals the difference between exogenous CCK-8 and endogenous CCK effects on the development of morphine dependence, and provides the first evidence for the participation of the CCK1 receptor in the inhibitory effects of exogenous CCK-8 on morphine dependence.

  14. Inhibitory effect of mTOR activator MHY1485 on autophagy: suppression of lysosomal fusion.

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    Yeon Ja Choi

    Full Text Available Autophagy is a major degradative process responsible for the disposal of cytoplasmic proteins and dysfunctional organelles via the lysosomal pathway. During the autophagic process, cells form double-membraned vesicles called autophagosomes that sequester disposable materials in the cytoplasm and finally fuse with lysosomes. In the present study, we investigated the inhibition of autophagy by a synthesized compound, MHY1485, in a culture system by using Ac2F rat hepatocytes. Autophagic flux was measured to evaluate the autophagic activity. Autophagosomes were visualized in Ac2F cells transfected with AdGFP-LC3 by live-cell confocal microscopy. In addition, activity of mTOR, a major regulatory protein of autophagy, was assessed by western blot and docking simulation using AutoDock 4.2. In the result, treatment with MHY1485 suppressed the basal autophagic flux, and this inhibitory effect was clearly confirmed in cells under starvation, a strong physiological inducer of autophagy. The levels of p62 and beclin-1 did not show significant change after treatment with MHY1485. Decreased co-localization of autophagosomes and lysosomes in confocal microscopic images revealed the inhibitory effect of MHY1485 on lysosomal fusion during starvation-induced autophagy. These effects of MHY1485 led to the accumulation of LC3II and enlargement of the autophagosomes in a dose- and time-dependent manner. Furthermore, MHY1485 induced mTOR activation and correspondingly showed a higher docking score than PP242, a well-known ATP-competitive mTOR inhibitor, in docking simulation. In conclusion, MHY1485 has an inhibitory effect on the autophagic process by inhibition of fusion between autophagosomes and lysosomes leading to the accumulation of LC3II protein and enlarged autophagosomes. MHY1485 also induces mTOR activity, providing a possibility for another regulatory mechanism of autophagy by the MHY compound. The significance of this study is the finding of a novel

  15. Inhibitory Effect of Arctigenin from Fructus Arctii Extract on Melanin Synthesis via Repression of Tyrosinase Expression.

    Science.gov (United States)

    Park, Hwayong; Song, Kwang Hoon; Jung, Pil Mun; Kim, Ji-Eun; Ro, Hyunju; Kim, Mi Yoon; Ma, Jin Yeul

    2013-01-01

    To identify the active compound arctigenin in Fructus Arctii (dried seed of medicinal plant Arctium lappa) and to elucidate the inhibitory mechanism in melanogenesis, we analyzed melanin content and tyrosinase activity on B16BL6 murine melanoma and melan-A cell cultures. Water extracts of Fructus Arctii were shown to inhibit tyrosinase activity in vitro and melanin content in α -melanocyte stimulating hormone-stimulated cells to similar levels as the well-known kojic acid and arbutin, respectively. The active compound arctigenin of Fructus Arctii displayed little or no cytotoxicity at all concentrations examined and decreased the relative melanin content and tyrosinase activity in a dose-dependent manner. Melanogenic inhibitory activity was also identified in vivo with zebrafish embryo. To determine the mechanism of inhibition, the effects of arctigenin on tyrosinase gene expression and tyrosinase promoter activity were examined. Also in addition, in the signaling cascade, arctigenin dose dependently decreased the cAMP level and promoted the phosphorylation of extracellular signal-regulated kinase. This result suggests that arctigenin downregulates cAMP and the tyrosinase enzyme through its gene promoter and subsequently upregulates extracellular signal-regulated kinase activity by increasing phosphorylation in the melanogenesis signaling pathway, which leads to a lower melanin content.

  16. Effects of multiple inhibitory components on anaerobic treatment processes in municipal solid waste incineration leachate.

    Science.gov (United States)

    Lei, Yuqing; Dang, Yan; Lan, Zhangheng; Sun, Dezhi

    2016-06-01

    This study served to investigate the comparative and combined effects of calcium, ammonia nitrogen, and aquatic humic substances (AHS) on specific methanogenic activity (SMA) in municipal solid waste leachate at mesophilic conditions. Using orthogonal experiments, anaerobic granular sludge was cultured with different concentrations combinations of the three added components for 13 days. The combination of 6000 mg/L calcium, 400 mg/L ammonia nitrogen, and 4000 mg/L AHS was the most inhibitory combination on the SMA of granular sludge, with a calculated 4.49 mL (standard temperature and atmospheric pressure) (STP) CH4/(gVSS·d) of SMA. The SMA with the addition of the inhibitory components was much lower than the control group's (1000 mg/L calcium, 200 mg/L ammonia nitrogen and 2000 mg/L AHS) with a calculated 12.97 mL (STP) CH4/(gVSS·d) of SMA. Calcium was the major inhibitor among the three components followed by AHS. High concentrations of calcium significantly inhibited the utilization of propionate and butyrate in the substrate and further affected the methanogenic process.

  17. Inhibitory effects of polycyclic aromatic hydrocarbons (PAHs) on photosynthetic performance are not related to their aromaticity.

    Science.gov (United States)

    Jajoo, Anjana; Mekala, Nageswara Rao; Tomar, Rupal Singh; Grieco, Michele; Tikkanen, Mikko; Aro, Eva-Mari

    2014-08-01

    Polycyclic aromatic hydrocarbons (PAHs) are very toxic and highly persistent environmental pollutants which accumulate in soil and affect growth of the plants adversely. This study aims to investigate inhibitory effects of 3 major PAH particularly on photosynthetic processes in Arabidopsis thaliana grown in soil treated with PAH. The 3 PAH chosen differ from each other in aromaticity (number of rings) comprising their structure (2 rings: naphthalene, 3 rings: anthracene and 4 rings: pyrene). Several growth parameters and Chlorophyll a fluorescence was monitored in PAH treated plants. BN-PAGe analysis was done in order to get information about change in the protein conformation. PAH treatment led to increased value of Fo which collaborated with increase in the amount of free LHC as seen through BN-Page analysis. Thus PAH were found to inhibit PS II photochemistry and caused distinct change in pigment composition. However the results led us to infer that 3-ring anthracence is more inhibitory as compared to 2-ring naphthalene and 4-ring pyrene. This indicates that aromaticity of PAH is unrelated to their response on photosynthetic processes.

  18. β-Secretase (BACE1) inhibitory and neuroprotective effects of p-terphenyls from Polyozellus multiplex.

    Science.gov (United States)

    Chon, So-Hyun; Yang, Eun-Ju; Lee, Taeho; Song, Kyung-Sik

    2016-09-14

    Alzheimer's disease (AD), a major neurodegenerative disorder, is associated with the enzymatic reaction of β-secretase (BACE1) on the amyloid precursor protein (APP) for the generation of neurotoxic amyloid-β (Aβ). Therefore, Aβ accumulation and oxidative stress-induced neuronal cell death are the pathogenic hallmarks of AD. In this study, we tried to identify BACE1 inhibitors and neuroprotectants from natural products, in particular, from the Korean mushroom Polyozellus multiplex. Four p-terphenyls were identified from the ethanolic extract of P. multiplex; polyozellin (1), thelephoric acid (2), polyozellic acid (3), and kynapcin-12 (4). Compounds 1-4 effectively inhibited BACE1 activity with a half-maximal inhibitory concentration (IC50) of 3.08, 3.50, 4.78, and 15.79 μM, respectively. Compounds 1-3 reduced the production of neurotoxic Aβ1-42 production in APPswe-N2a cells in a concentration-dependent manner. When HT22 cells were stressed with 5 mM glutamate, compounds 2 and 3 significantly recovered cell viability. It was correlated with their inhibitory properties against glutamate-mediated Ca(2+) influx, intracellular reactive oxygen species (ROS) generation, lipid peroxidation, reduction in Bcl-2 and Bid levels, and enhanced phosphorylation of mitogen-activated protein kinase (MAPK). Thus, P. multiplex and the isolated p-terphenyls might be useful in the development of lead compounds for the prevention of neurodegenerative diseases, especially AD.

  19. Comparative inhibitory effects of niflumic acid and novel synthetic derivatives on the rat isolated stomach fundus.

    Science.gov (United States)

    Criddle, David N; Meireles, AnaVanescaP; Macêdo, Liana B; Leal-Cardoso, José H; Scarparo, Henrique C; Jaffar, Mohammed

    2002-02-01

    Novel derivatives of 2-[3-(trifluoromethyl)-analino]nicotinic acid (niflumic acid) were synthesized. The compounds were compared for their inhibitory effects on 5-hydroxytryptamine (5-HT)- and KCI-induced contraction of the rat fundus. The aim was to assess structure-activity relationships regarding the selectivity and potency of these compounds. Niflumic acid (1-100 microM) concentration-dependently inhibited 5-HT-induced tonic contractions with an IC50 value (concentration reducing the control contractile response by 50%, calculated from semi-log graphs) of 0.24 x 10(4) M (n = 9). In contrast, it was significantly less potent at inhibiting KCl-induced responses (IC50 = 1.49 x 10(4) M, n = 9). The methyl ester (NFAme) and amido (NFAm) analogues showed no selectivity between 5-HT- and KCl-induced contractions with IC50 values of 1.64 x 10(-4) M (n = 8) and 1.87 x 10(-4) M (n = 9) for 5-HT responses, and 2.61 x 10(-4) M (n = 8) and 2.55 x 10(-4) M (n = 7) for KCl-induced responses, respectively. Our results suggest that alteration of the carboxylic acid moiety of niflumic acid reduces the selectivity and potency of its inhibitory action on 5-HT-induced contractile responses of the rat fundus, possibly via a reduced interaction with calcium-activated chloride channels.

  20. Inhibitory Effect of Camptothecin against Rice Bacterial Brown Stripe Pathogen Acidovorax avenae subsp. avenae RS-2

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    Qiaolin Dong

    2016-07-01

    Full Text Available Camptothecin (CPT has anticancer, antiviral, and antifungal properties. However, there is a dearth of information about antibacterial activity of CPT. Therefore, in this study, we investigated the inhibitory effect of CPT on Acidovorax avenae subsp. avenae strain RS-2, the pathogen of rice bacterial brown stripe, by measuring cell growth, DNA damage, cell membrane integrity, the expression of secretion systems, and topoisomerase-related genes, as well as the secretion of effector protein Hcp. Results indicated that CPT solutions at 0.05, 0.25, and 0.50 mg/mL inhibited the growth of strain RS-2 in vitro, while the inhibitory efficiency increased with an increase in CPT concentration, pH, and incubation time. Furthermore, CPT treatment affected bacterial growth and replication by causing membrane damage, which was evidenced by transmission electron microscopic observation and live/dead cell staining. In addition, quantitative real-time PCR analysis indicated that CPT treatment caused differential expression of eight secretion system-related genes and one topoisomerase-related gene, while the up-regulated expression of hcp could be justified by the increased secretion of Hcp based on the ELISA test. Overall, this study indicated that CPT has the potential to control the bacterial brown stripe pathogen of rice.

  1. Growth inhibitory effects of endotoxins from Bacteroides gingivalis and intermedius on human gingival fibroblasts in vitro

    Energy Technology Data Exchange (ETDEWEB)

    Layman, D.L.; Diedrich, D.L.

    1987-06-01

    Purified endotoxin or lipopolysaccharide from Bacteroides gingivalis and Bacteroides intermedius caused a similar dose-dependent inhibition of growth of cultured human gingival fibroblasts as determined by /sup 3/H-thymidine incorporation and direct cell count. Approximately 200 micrograms/ml endotoxin caused a 50% reduction in /sup 3/H-thymidine uptake of logarithmically growing cells. Inhibition of growth was similar in cultures of fibroblasts derived from either healthy or diseased human gingiva. When examining the change in cell number with time of exposure in culture, the rate of proliferation was significantly suppressed during the logarithmic phase of growth. However, the cells recovered so that the rate of proliferation, although reduced, was sufficient to produce a cell density similar to the control cells with prolonged culture. The endotoxins were characterized by sodium dodecyl sulfate-polyacrylamide gel electrophoresis. The profiles of the Bacteroides endotoxins were different. B. gingivalis endotoxin showed a wide range of distinct bands indicating a heterogeneous distribution of molecular species. Endotoxin from B. intermedius exhibited a few discrete low molecular weight bands, but the majority of the lipopolysaccharides electrophoresed as a diffuse band of high molecular weight material. The apparent heterogeneity of the two Bacteroides endotoxins and the similarity in growth inhibitory capacity suggest that growth inhibitory effects of these substances cannot be attributed to any polysaccharide species of endotoxin.

  2. Inhibitory Effect of Arctigenin from Fructus Arctii Extract on Melanin Synthesis via Repression of Tyrosinase Expression

    Science.gov (United States)

    Park, Hwayong; Song, Kwang Hoon; Jung, Pil Mun; Kim, Ji-Eun; Kim, Mi Yoon; Ma, Jin Yeul

    2013-01-01

    To identify the active compound arctigenin in Fructus Arctii (dried seed of medicinal plant Arctium lappa) and to elucidate the inhibitory mechanism in melanogenesis, we analyzed melanin content and tyrosinase activity on B16BL6 murine melanoma and melan-A cell cultures. Water extracts of Fructus Arctii were shown to inhibit tyrosinase activity in vitro and melanin content in α-melanocyte stimulating hormone-stimulated cells to similar levels as the well-known kojic acid and arbutin, respectively. The active compound arctigenin of Fructus Arctii displayed little or no cytotoxicity at all concentrations examined and decreased the relative melanin content and tyrosinase activity in a dose-dependent manner. Melanogenic inhibitory activity was also identified in vivo with zebrafish embryo. To determine the mechanism of inhibition, the effects of arctigenin on tyrosinase gene expression and tyrosinase promoter activity were examined. Also in addition, in the signaling cascade, arctigenin dose dependently decreased the cAMP level and promoted the phosphorylation of extracellular signal-regulated kinase. This result suggests that arctigenin downregulates cAMP and the tyrosinase enzyme through its gene promoter and subsequently upregulates extracellular signal-regulated kinase activity by increasing phosphorylation in the melanogenesis signaling pathway, which leads to a lower melanin content. PMID:23781272

  3. Flavonoids from Machilus japonica Stems and Their Inhibitory Effects on LDL Oxidation

    Directory of Open Access Journals (Sweden)

    Se-Jin Joo

    2014-09-01

    Full Text Available Stems of Machilus japonica were extracted with 80% aqueous methanol (MeOH and the concentrated extract was successively extracted with ethyl acetate (EtOAc, normal butanol (n-BuOH, and water. Six flavonoids were isolated from the EtOAc fraction: (+-taxifolin, afzelin, (−-epicatechin, 5,3'-di-O-methyl-(−-epicatechin, 5,7,3'-tri-O-methyl-(−-epicatechin, and 5,7-di-O-methyl-3',4'-methylenedioxyflavan-3-ol. The chemical structures were identified using spectroscopic data including NMR, mass spectrometry and infrared spectroscopy. This is the first report of isolation of these six compounds from M. japonica. The compounds were evaluated for their diphenyl picryl hydrazinyl scavenging activity and inhibitory effects on low-density lipoprotein oxidation. Compounds 1 and 3–6 exhibited DPPH antioxidant activity equivalent with that of ascorbic acid, with half maximal inhibitory concentration (IC50 values of 0.16, 0.21, 0.17, 0.15 and 0.07 mM, respectively. The activity of compound 1 was similar to the positive control butylated hydroxytoluene, which had an IC50 value of 1.9 µM, while compounds 3 and 5 showed little activity. Compounds 1, 3, and 5 exhibited LDL antioxidant activity with IC50 values of 2.8, 7.1, and 4.6 µM, respectively.

  4. Influence of the spacer on the inhibitory effect of different polycarbophil-protease inhibitor conjugates.

    Science.gov (United States)

    Marschütz, M K; Veronese, F M; Bernkop-Schnürch, A

    2001-09-01

    Within the present study various polycarbophil (PCP)-serine protease inhibitor conjugates were synthesized and the influence of different spacers on their inhibitory efficacy was evaluated in vitro. Results demonstrated that 4.2+/-0.15 units (n=3; +/-SD) of alpha-chymotrypsin were inhibited by 50% utilizing 0.86% (w/v) of a PCP-tetramethylenediamine (TMDA)-chymostatin 20:1 conjugate. In contrast, only 0.6+/-0.05 units (n=3; +/-SD) of alpha-chymotrypsin were inhibited by a corresponding PCP-poly(ethylene glycol) (PEG)-chymostatin conjugate. Inhibitory effects of PCP-TMDA-antipain and -elastatinal conjugates towards trypsin and elastase, respectively, were also significantly higher (P<0.05) than those of corresponding PCP-PEG-inhibitor conjugates. Hence, the great impact of the molecular size as well as the structure of the spacer on resulting polymer-inhibitor conjugates could be demonstrated. The small and rigid C4-spacer TMDA (molecular weight (MW) 161.1) was thereby shown to be highly advantageous over a long, hydrophilic and flexible PEG-diamine spacer (MW 3400). Results obtained should provide helpful basic knowledge for the development of mucoadhesive polymer-inhibitor conjugates used as auxiliary agents for the oral administration of peptide drugs.

  5. Inhibitory Effect of Arctigenin from Fructus Arctii Extract on Melanin Synthesis via Repression of Tyrosinase Expression

    Directory of Open Access Journals (Sweden)

    Hwayong Park

    2013-01-01

    Full Text Available To identify the active compound arctigenin in Fructus Arctii (dried seed of medicinal plant Arctium lappa and to elucidate the inhibitory mechanism in melanogenesis, we analyzed melanin content and tyrosinase activity on B16BL6 murine melanoma and melan-A cell cultures. Water extracts of Fructus Arctii were shown to inhibit tyrosinase activity in vitro and melanin content in α-melanocyte stimulating hormone-stimulated cells to similar levels as the well-known kojic acid and arbutin, respectively. The active compound arctigenin of Fructus Arctii displayed little or no cytotoxicity at all concentrations examined and decreased the relative melanin content and tyrosinase activity in a dose-dependent manner. Melanogenic inhibitory activity was also identified in vivo with zebrafish embryo. To determine the mechanism of inhibition, the effects of arctigenin on tyrosinase gene expression and tyrosinase promoter activity were examined. Also in addition, in the signaling cascade, arctigenin dose dependently decreased the cAMP level and promoted the phosphorylation of extracellular signal-regulated kinase. This result suggests that arctigenin downregulates cAMP and the tyrosinase enzyme through its gene promoter and subsequently upregulates extracellular signal-regulated kinase activity by increasing phosphorylation in the melanogenesis signaling pathway, which leads to a lower melanin content.

  6. Inhibitory effect of schisandrin B on gastric cancer cells in vitro

    Institute of Scientific and Technical Information of China (English)

    2007-01-01

    AIM: To investigate the inhibitory effect and possible mechanism of action of schisandrin B in SC-B on gastric cancer cells in vitro.METHODS: SC-B consisted of schisandrin B, aloeemodin, and Astragalus polysaccharides. Exponentially growing human gastric cancer SGC-7901 cells were divided into six treatment groups: (1) control group (RPMI 1640 medium); (2) negative control group (2% DMSO);(3) positive control group (50 mg/L 5-Fluorouracil,5-FU); (4) low-dose group (LSC, final concentration of schisandrin B, 25 mg/L); (5) moderate-dose group (MSC,final concentration of schisandrin B, 50 mg/L); (6) high-dose group (HSC, final concentration of schisandrin B,100 mg/L). Follow-up was done at 12-48 h. An MTT (Methylthiazolyldiphenyl-tetrazolium bromide) assay was used to examine the inhibitory effect of SC-B on gastric cancer cells. The mitosis index was assessed using an inverted microscope. Flow cytometry was used to visualize the cell cycle. An RT-PCR (Reverse transcription-Polymerase chain reaction) -based assay was used to detect mRNA expression for cyclin D1 and glyceraldehyde-3-phosphate dehydrogenase (GAPDH).RESULTS: The MTT assay showed that the number of living cells in the LSC, MSC and HSC groups was significantly smaller than that in the DMSO-treated group (P < 0.05) at 12-48 h. The inhibitory rate (IR) of the LSC group was 41.15% ± 3.86%, 59.24% ± 5.34% and 69.93% ± 7.81% at 12, 24 and 48 h, respectively. The IR of the MSC group was 42.82% ± 4.94%, 62.68% ± 7.58% and 71.79% ± 8.12% at 12, 24 and 48 h,respectively. The IR of the HSC group was 37.50% ± 3.21%, 40.34% ± 2.98% and 61.99% ± 4.88% at 12,24 and 48 h, respectively. These results suggested that a moderate dosage had the most obvious inhibitory efficacy at 48 h. Compared to the DMSO group, the mitosis index of the LSC, MSC, HSC groups was greatly decreased (P < 0.05) at all time points. Any dose of SC-B suppressed mitosis within 12-48 h. Compared to the DMSO group, the percentage of cells

  7. Inhibitory effects of the essential oil of Mentha pulegium on the isolated rat myometrium.

    Science.gov (United States)

    Soares, P M; Assreuy, A M S; Souza, E P; Lima, R F; Silva, T O; Fontenele, S R; Criddle, D N

    2005-03-01

    The effects of the essential oil of Mentha pulegium L. (EOMP), a plant commonly known as "pennyroyal" or "poejo" that is used in folk medicine as an abortifaceant, were assessed on the isolated rat myometrium. Myometrial strips were stimulated with 10 nM oxytocin or 10 microM PGF (2alpha). EOMP (10 - 300 microg/mL) concentration-dependently and reversibly inhibited the amplitude of oscillatory contractions, being approximately 3-fold more active against contractions stimulated by oxytocin than those by PGF (2alpha) (IC (50) values of 45.7 +/- 5.6 microg/mL and 160.9 +/- 5.9 microg/mL , respectively), although the maximal inhibitory effect occurred at the same concentration (300 microg/mL ) in both cases. This action was shared by pulegone (30 - 300 microM), the principal component of the essential oil (IC (50) values of 21.8 +/- 2.1 microg/mL and 12.7 +/- 4.6 microg/mL , respectively). Nifedipine (30 nM - 30 microM) also abolished agonist-stimulated contractions, and was approximately twice and 12 times as potent as EOMP in inhibiting oxytocin- and prostaglandin F (2alpha) (PGF (2alpha))-stimulated contractions, respectively. In conclusion, our results show that the essential oil of the abortifaceant plant Mentha pulegium exerts an inhibitory effect on the contractile activity of the isolated rat myometrium. This oil shares a common effect with the voltage-dependent calcium channel (VDCC) blocker nifedipine, although ostensibly acting via a different mechanism. It thus appears that EOMP and pulegone do not exert direct toxic effects on the myometrium per se that would cause abortion, and other possibilities such as systemic metabolism of plant constituents may rather underlie the abusive use of Mentha pulegium in popular medicine.

  8. Inhibitory effect of Disulfiram/copper complex on non-small cell lung cancer cells

    Energy Technology Data Exchange (ETDEWEB)

    Duan, Lincan [Department of Thoracic Surgery, The Third Affiliated Hospital of Kunming Medical University, Kunming (China); Shen, Hongmei [Cancer Center of Integrative Medicine, The Third Affiliated Hospital of Kunming Medical University, Kunming (China); Zhao, Guangqiang [Department of Thoracic Surgery, The Third Affiliated Hospital of Kunming Medical University, Kunming (China); Yang, Runxiang [Cancer Chemotherapy Center, The Third Affiliated Hospital of Kunming Medical University, Kunming (China); Cai, Xinyi [Colorectal Cancer Center, The Third Affiliated Hospital of Kunming Medical University, Kunming (China); Zhang, Lijuan [Department of Pathology, The Third Affiliated Hospital of Kunming Medical University, Kunming (China); Jin, Congguo [Cancer Institute, The Third Affiliated Hospital of Kunming Medical University, Kunming (China); Huang, Yunchao, E-mail: daliduanlincan@163.com [Department of Thoracic Surgery, The Third Affiliated Hospital of Kunming Medical University, Kunming (China)

    2014-04-18

    Highlights: • Disulfiram and copper synergistically inhibit lung cancer cell proliferation. • Lung cancer cell colony formation ability is inhibited by Disulfiram/copper. • Disulfiram/copper increases the sensitivity of cisplatin to lung cancer cells. • Lung cancer stem cells are specifically targeted by Disulfiram/copper complex. - Abstract: Non-small cell lung cancer (NSCLC) is the most common cause of cancer-related death in both men and women worldwide. Recently, Disulfiram has been reported to be able to inhibit glioblastoma, prostate, or breast cancer cell proliferation. In this study, the synergistic effect of Disulfiram and copper on NSCLC cell growth was investigated. Inhibition of cancer cell proliferation was detected by 1-(4,5-Dimethylthiazol-2-yl)-3,5-diphenylformazan (MTT) assay and cell cycle analysis. Liquid colony formation and tumor spheroid formation assays were used to evaluate their effect on cancer cell clonogenicity. Real-time PCR was performed to test the mRNA level of cancer stem cell related genes. We found that Disulfiram or copper alone did not potently inhibit NSCLC cell proliferation in vitro. However, the presence of copper significantly enhanced inhibitory effect of Disulfiram on NSCLC cell growth, indicating a synergistic effect between Disulfiram and copper. Cell cycle analysis showed that Disulfiram/copper complex caused NSCLC cell cycle arrest in G2/M phase. Furthermore, Disulfiram/copper significantly increased the sensitivity of cisplatin in NSCLC cells tested by MTT assay. Liquid colony formation assay revealed that copper dramatically increased the inhibitory effect of Disulfiram on NSCLC cell colony forming ability. Disulfiram combined with copper significantly attenuated NSCLC cell spheroid formation and recuded the mRNA expression of lung cancer stem cell related genes. Our data suggest that Disulfiram/copper complex alone or combined with other chemotherapy is a potential therapeutic strategy for NSCLC patients.

  9. Inhibitory effect of Disulfiram/copper complex on non-small cell lung cancer cells.

    Science.gov (United States)

    Duan, Lincan; Shen, Hongmei; Zhao, Guangqiang; Yang, Runxiang; Cai, Xinyi; Zhang, Lijuan; Jin, Congguo; Huang, Yunchao

    2014-04-18

    Non-small cell lung cancer (NSCLC) is the most common cause of cancer-related death in both men and women worldwide. Recently, Disulfiram has been reported to be able to inhibit glioblastoma, prostate, or breast cancer cell proliferation. In this study, the synergistic effect of Disulfiram and copper on NSCLC cell growth was investigated. Inhibition of cancer cell proliferation was detected by 1-(4,5-Dimethylthiazol-2-yl)-3,5-diphenylformazan (MTT) assay and cell cycle analysis. Liquid colony formation and tumor spheroid formation assays were used to evaluate their effect on cancer cell clonogenicity. Real-time PCR was performed to test the mRNA level of cancer stem cell related genes. We found that Disulfiram or copper alone did not potently inhibit NSCLC cell proliferation in vitro. However, the presence of copper significantly enhanced inhibitory effect of Disulfiram on NSCLC cell growth, indicating a synergistic effect between Disulfiram and copper. Cell cycle analysis showed that Disulfiram/copper complex caused NSCLC cell cycle arrest in G2/M phase. Furthermore, Disulfiram/copper significantly increased the sensitivity of cisplatin in NSCLC cells tested by MTT assay. Liquid colony formation assay revealed that copper dramatically increased the inhibitory effect of Disulfiram on NSCLC cell colony forming ability. Disulfiram combined with copper significantly attenuated NSCLC cell spheroid formation and recuded the mRNA expression of lung cancer stem cell related genes. Our data suggest that Disulfiram/copper complex alone or combined with other chemotherapy is a potential therapeutic strategy for NSCLC patients.

  10. Carbon tetrachloride-induced hepatic and renal damages in rat: inhibitory effects of cacao polyphenol.

    Science.gov (United States)

    Suzuki, Koichiro; Nakagawa, Kiyotaka; Yamamoto, Takayuki; Miyazawa, Taiki; Kimura, Fumiko; Kamei, Masanori; Miyazawa, Teruo

    2015-01-01

    Here, we investigated the protective effect of cacao polyphenol extract (CPE) on carbon tetrachloride (CCl4)-induced hepato-renal oxidative stress in rats. Rats were administered CPE for 7 days and then received intraperitoneal injection of CCl4. Two hours after injection, we found that CCl4 treatment significantly increased biochemical injury markers, lipid peroxides (phosphatidylcholine hydroperoxide (PCOOH) and malondialdehyde (MDA)) and decreased glutathione peroxidase activity in kidney rather than liver, suggesting that kidney is more vulnerable to oxidative stress under the present experimental conditions. CPE supplementation significantly reduced these changes, indicating that this compound has antioxidant properties against CCl4-induced oxidative stress. An inhibitory effect of CPE on CCl4-induced CYP2E1 mRNA degradation may provide an explanation for CPE antioxidant property. Together, these results provide quantitative evidence of the in vivo antioxidant properties of CPE, especially in terms of PCOOH and MDA levels in the kidneys of CCl4-treated rats.

  11. Effect of adsorption of an inhibitory factor on raw starch hydrolysis by glucoamylase.

    Science.gov (United States)

    Towprayoon, S; Fujio, Y; Ueda, S

    1990-12-01

    An inhibitory factor (IF) produced byAspergillus niger strain 19, and which inhibits the action of glucoamylase on starch, has the ability to be tightly adsorbed on to various raw starches, though the amount differs from starch to starch. Based on the hydrolysis of the IF-starch complex by glucoamylase, the inhibitions per unit IF adsorbed are similar for some varieties of starch. The effectiveness ratio of IF (% hydrolysis inhibition per % IF adsorbed on raw starch) for corn, sweet potato, waxy rice and waxy corn starches are 1.1, 1.0, 0.85 and 0.96, respectively. These results support the hypothesis that both glucoamylase and IF are adsorbed on to a common binding site on raw starch. However, the effectiveness ratio of IF for cassava and wheat starches are 0.71 and 1.65, respectively, which differ significantly from other varieties of starch.

  12. Inhibitory effect for proliferation of oral bacteria in dogs by tooth brushing and application of toothpaste

    Science.gov (United States)

    WATANABE, Kazuhiro; KIJIMA, Saku; NONAKA, Chie; MATSUKAWA, Yuki; YAMAZOE, Kazuaki

    2016-01-01

    To investigate inhibitory effect for oral bacterial proliferation, we divided 12 dogs into 3 groups; scaling alone (C; control group), brushing (B) and application of toothpaste (P). Before scaling (Pre) and at 0 to 8 weeks after scaling (0–8 w), we collected oral bacteria from the dental surface every week and counted them using a bacterial counter. The results demonstrated a significant reduction in the number of oral bacteria for group B relative to Pre and group C, as well as for group P relative to group C at 5–7 w. Consequently, brushing may inhibit an increase in the number of oral bacteria, and toothpaste may be effective at a certain level, although not more than that of brushing. PMID:27062999

  13. Oxidative damage involves in the inhibitory effect of nitric oxide on spore germination of Penicillium expansum.

    Science.gov (United States)

    Lai, Tongfei; Li, Boqiang; Qin, Guozheng; Tian, Shiping

    2011-01-01

    The effects of nitric oxide (NO) on spore germination of Penicillium expansum were investigated and a possible mechanism was evaluated. The results indicated that NO released by sodium nitroprusside (SNP) significantly suppressed fungal growth. With the use of an oxidant sensitive probe and Western blot analysis, an increased level of intracellular reactive oxygen species (ROS) and enhanced carbonylation damage were detected in spores of P. expansum under NO stress. Exogenous superoxide dismutase (SOD) and ascorbic acid (Vc) could increase the resistance of the spore to the inhibitory effect of NO. The activities of SOD and catalase (CAT), as well as ATP content in spores under NO stress were also lower than those in the control. We suggest that NO in high concentration induces the generation of ROS which subsequently causes severe oxidative damage to proteins crucial to the process of spore germination of P. expansum.

  14. Critical considerations on the evaluation of macroseismic effects

    Directory of Open Access Journals (Sweden)

    M. C. SPADEA

    1980-06-01

    Full Text Available The definition of some of the standards used for evaluating local effects
    and optimizing the relative macroseismic procedures are critically
    considered, also from the different interpretative points of view to have
    come out of the « Earthquake Catalogue » work group of the Italian Geodynamics
    Projetc (PFG. Particular stress has been laid on the significance
    and reliability of the main macroseismic parameters which depend
    most directly on the investigative criteria used and on their ability to
    characterize efficiently the interaction of earthquakes and environment.
    Essentially, the analysis is of critical considerations and field-observations,
    the fruit of macroseismic investigations carried out prevalently in
    the Calabro-Peloritan Arc region. The seismic intensity, the use of macroseismic
    scales, the investigatory criteria, the macroseismic field and its anomalies are the topics chosen for a study which — even if limited from
    certain aspects — it is hoped will stimulate further thought and evaluations.

  15. High potassium intake enhances the inhibitory effect of 11,12-EET on ENaC.

    Science.gov (United States)

    Sun, Peng; Lin, Dao-Hong; Yue, Peng; Jiang, Houli; Gotlinger, Katherine H; Schwartzman, Michal L; Falck, John R; Goli, Mohan; Wang, Wen-Hui

    2010-10-01

    High dietary potassium stimulates the renal expression of cytochrome P450 (CYP) epoxygenase 2C23, which metabolizes arachidonic acid (AA). Because the AA metabolite 11,12-epoxyeicosatrienoic acid (11,12-EET) can inhibit the epithelial sodium channel (ENaC) in the cortical collecting duct, we tested whether dietary potassium modulates ENaC function. High dietary potassium increased 11,12-EET in the isolated cortical collecting duct, an effect mimicked by inhibiting the angiotensin II type I receptor with valsartan. In patch-clamp experiments, a high potassium intake or treatment with valsartan enhanced AA-induced inhibition of ENaC, an effect mediated by a CYP-epoxygenase-dependent pathway. Moreover, high dietary potassium and valsartan each augmented the inhibitory effect of 11,12-EET on ENaC. Liquid chromatography/mass spectrometry showed that the rate of EET conversion to dihydroxyeicosatrienoic acids (DHET) was lower in renal tissue obtained from rats on a high-potassium diet than from those on a control diet, but this was not a result of altered expression of soluble epoxide hydrolase (sEH). Instead, suppression of sEH activity seemed to be responsible for the 11,12-EET-mediated enhanced inhibition of ENaC in animals on a high-potassium diet. Patch-clamp experiments demonstrated that 11,12-DHET was a weak inhibitor of ENaC compared with 11,12-EET, whereas 8,9- and 14,15-DHET were not. Furthermore, inhibition of sEH enhanced the 11,12-EET-induced inhibition of ENaC similar to high dietary potassium. In conclusion, high dietary potassium enhances the inhibitory effect of AA and 11,12-EET on ENaC by increasing CYP epoxygenase activity and decreasing sEH activity, respectively.

  16. Inhibitory effects of recombinant neurotoxin BmK IM on seizures induced by pentylenetetrazol in Rats

    Institute of Scientific and Technical Information of China (English)

    何小华; 彭方; 章军建; 李文鑫; 曾宪春; 刘辉

    2003-01-01

    Objective To elucidate the inhibitory effects of recombinant Chinese scorpion neurotoxin BmK IM on seizures induced by pentylenetetrazol (PTZ) and the possible mechanism.Methods After purifying recombinant BmK IM from an E. coli cell line, its toxicity (both LD50 and minimum lethal dose) on rats was determined. BmK IM was then microinjected into the CA3 region of the right hippocampus and its ability to inhibit the effects of an intraperitoneal injection of PTZ was assessed. The effects of BmK IM on the electrophysiological properties of isolated CA3 pyramidal neurons were then studied using whole-cell patch clamp techniques.Results BmK IM can significantly prolong the latent period of epileptic seizures, decrease the degree of seizures, and decrease the frequency of epileptiform discharges induced by PTZ. At the same time, 24h after injection of BmK IM into the hippocampal tissue, BmK IM significantly reduces the concentration of the neurotransmitter glutamate and alleviates PTZ-induced lesions in the hippocampus. Whole-cell patch clamp recordings indicate that BmK IM inhibits INa of rat hippocampal neurons in a dose-dependent manner. BmK IM significantly shifts the activation curve of INa in a positive direction, indicating that BmK IM enhances the threshold potential of INa.Conclusions BmK IM has significant anti-epileptic properties, and may prove useful as a drug in the therapy of epilepsy. The inhibitory effects of BmK IM on seizures caused by pentylenetetrazol might depend on reductions in the release of presynaptic glutamate via the blocking of Na+ channels.

  17. The effect of gastric inhibitory polypeptide on intestinal glucose absorption and intestinal motility in mice

    Energy Technology Data Exchange (ETDEWEB)

    Ogawa, Eiichi [Department of Diabetes and Clinical Nutrition, Graduate School of Medicine, Kyoto University (Japan); Hosokawa, Masaya [Department of Diabetes and Clinical Nutrition, Graduate School of Medicine, Kyoto University (Japan); Faculty of Human Sciences, Tezukayama Gakuin University, Osaka (Japan); Harada, Norio; Yamane, Shunsuke; Hamasaki, Akihiro; Toyoda, Kentaro; Fujimoto, Shimpei; Fujita, Yoshihito; Fukuda, Kazuhito [Department of Diabetes and Clinical Nutrition, Graduate School of Medicine, Kyoto University (Japan); Tsukiyama, Katsushi; Yamada, Yuichiro [Department of Diabetes and Clinical Nutrition, Graduate School of Medicine, Kyoto University (Japan); Department of Internal Medicine, Division of Endocrinology, Diabetes and Geriatric Medicine, Akita University School of Medicine, Akita (Japan); Seino, Yutaka [Department of Diabetes and Clinical Nutrition, Graduate School of Medicine, Kyoto University (Japan); Kansai Electric Power Hospital, Osaka (Japan); Inagaki, Nobuya, E-mail: inagaki@metab.kuhp.kyoto-u.ac.jp [Department of Diabetes and Clinical Nutrition, Graduate School of Medicine, Kyoto University (Japan); CREST of Japan Science and Technology Cooperation (JST), Kyoto (Japan)

    2011-01-07

    Research highlights: {yields} Exogenous GIP inhibits intestinal motility through a somatostatin-mediated pathway. {yields} Exogenous GIP inhibits intestinal glucose absorption by reducing intestinal motility. {yields} The GIP-receptor-mediated action in intestine does not involve in GLP-1-mediated pathway. -- Abstract: Gastric inhibitory polypeptide (GIP) is released from the small intestine upon meal ingestion and increases insulin secretion from pancreatic {beta} cells. Although the GIP receptor is known to be expressed in small intestine, the effects of GIP in small intestine are not fully understood. This study was designed to clarify the effect of GIP on intestinal glucose absorption and intestinal motility. Intestinal glucose absorption in vivo was measured by single-pass perfusion method. Incorporation of [{sup 14}C]-glucose into everted jejunal rings in vitro was used to evaluate the effect of GIP on sodium-glucose co-transporter (SGLT). Motility of small intestine was measured by intestinal transit after oral administration of a non-absorbed marker. Intraperitoneal administration of GIP inhibited glucose absorption in wild-type mice in a concentration-dependent manner, showing maximum decrease at the dosage of 50 nmol/kg body weight. In glucagon-like-peptide-1 (GLP-1) receptor-deficient mice, GIP inhibited glucose absorption as in wild-type mice. In vitro examination of [{sup 14}C]-glucose uptake revealed that 100 nM GIP did not change SGLT-dependent glucose uptake in wild-type mice. After intraperitoneal administration of GIP (50 nmol/kg body weight), small intestinal transit was inhibited to 40% in both wild-type and GLP-1 receptor-deficient mice. Furthermore, a somatostatin receptor antagonist, cyclosomatostatin, reduced the inhibitory effect of GIP on both intestinal transit and glucose absorption in wild-type mice. These results demonstrate that exogenous GIP inhibits intestinal glucose absorption by reducing intestinal motility through a somatostatin

  18. Zinc enhances the inhibitory effects of strychnine-sensitive glycine receptors in mouse hippocampal neurons.

    Science.gov (United States)

    Zhang, Hai Xia; Thio, Liu Lin

    2007-12-01

    Although extracellular Zn(2+) is an endogenous biphasic modulator of strychnine-sensitive glycine receptors (GlyRs), the physiological significance of this modulation remains poorly understood. Zn(2+) modulation of GlyR may be especially important in the hippocampus where presynaptic Zn(2+) is abundant. Using cultured embryonic mouse hippocampal neurons, we examined whether 1 microM Zn(2+), a potentiating concentration, enhances the inhibitory effects of GlyRs activated by sustained glycine applications. Sustained 20 microM glycine (EC(25)) applications alone did not decrease the number of action potentials evoked by depolarizing steps, but they did in 1 microM Zn(2+). At least part of this effect resulted from Zn(2+) enhancing the GlyR-induced decrease in input resistance. Sustained 20 microM glycine applications alone did not alter neuronal bursting, a form of hyperexcitability induced by omitting extracellular Mg(2+). However, sustained 20 microM glycine applications depressed neuronal bursting in 1 microM Zn(2+). Zn(2+) did not enhance the inhibitory effects of sustained 60 microM glycine (EC(70)) applications in these paradigms. These results suggest that tonic GlyR activation could decrease neuronal excitability. To test this possibility, we examined the effect of the GlyR antagonist strychnine and the Zn(2+) chelator tricine on action potential firing by CA1 pyramidal neurons in mouse hippocampal slices. Co-applying strychnine and tricine slightly but significantly increased the number of action potentials fired during a depolarizing current step and decreased the rheobase for action potential firing. Thus Zn(2+) may modulate neuronal excitability normally and in pathological conditions such as seizures by potentiating GlyRs tonically activated by low agonist concentrations.

  19. In vitro cholinesterase inhibitory and antioxidant effect of selected coniferous tree species.

    Science.gov (United States)

    Senol, Fatma Sezer; Orhan, Ilkay Erdogan; Ustun, Osman

    2015-04-01

    To explore cholinesterase inhibitory and antioxidant effect of six coniferous trees (Abies bornmulleriana, Picea pungens, Juniperus communis, Cedrus libani, Taxus baccata, and Cupressus sempervirens var. horizantalis). Acetone (Ace), ethyl acetate (EtOAc), and ethanol (EtOH) extracts prepared from the needles and shoots of the six coniferous trees were screened for their acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activity at 100 μg/mL. Antioxidant activity of the extracts was tested using 2,2-diphenyl-1-picrylhydrazyl (DPPH) and N,N-dimethyl-p-phenylendiamine (DMPD) radical scavenging, metal-chelation capacity, ferric-(FRAP) and phosphomolibdenum-reducing antioxidant power (PRAP) assays. All of the assays were performed in ELISA microplate reader. Total phenol and flavonoid amounts in the extracts were determined spectrophotometrically. Among thirty-six extracts in total, the shoot-Ace extract of Cupressus sempervirens var. horizantalis exerted the highest inhibition against AChE [(54.84±2.51)%], while the needle-Ace extract of Cedrus libani was the most effective in inhibiting BChE [(67.54±0.30)%]. The highest DPPH radical scavenging effect, FRAP and PRAP was observed in the shoot-Ace and EtOAc extracts from Taxus baccata, whereas all the extracts showed a variable degree of scavenging effect against DPMD radical. The shoot-EtOAc extract of Cedrus libani had the highest metal-chelation capacity [(58.04±0.70)%]. The shoot extracts of Taxus baccata were determined to have the richest total phenol content, which may contribute to its marked antioxidant activity. The conifer species screened in this study may contain cholinesterase-inhibiting and antioxidant properties, which might be useful against Alzheimer's disease. Copyright © 2015 Hainan Medical College. Production and hosting by Elsevier B.V. All rights reserved.

  20. In vitro cholinesterase inhibitory and antioxidant effect of selected coniferous tree species

    Institute of Scientific and Technical Information of China (English)

    Fatma Sezer Senol; Ilkay Erdogan Orhan; Osman Ustun

    2015-01-01

    Objective: To explore cholinesterase inhibitory and antioxidant effect of six coniferous trees (Abies bornmulleriana, Picea pungens, Juniperus communis, Cedrus libani, Taxus baccata, and Cupressus sempervirens var. horizantalis). Methods: Acetone (Ace), ethyl acetate (EtOAc), and ethanol (EtOH) extracts prepared from the needles and shoots of the six coniferous trees were screened for their acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activity at 100 μg/mL. Antioxidant activity of the extracts was tested using 2,2-diphenyl-1-picrylhydrazyl (DPPH) and N,N-dimethyl-p-phenylendiamine (DMPD) radical scavenging, metal-chelation capacity, ferric-(FRAP) and phosphomolibdenum-reducing antioxidant power (PRAP) assays. All of the assays were performed in ELISA microplate reader. Total phenol and flavonoid amounts in the extracts were determined spectrophotometrically. Results: Among thirty-six extracts in total, the shoot-Ace extract of Cupressus sempervirens var. horizantalis exerted the highest inhibition against AChE [(54.84±2.51)%], while the needle-Ace extract of Cedrus libani was the most effective in inhibiting BChE [(67.54±0.30)%]. The highest DPPH radical scavenging effect, FRAP and PRAP was observed in the shoot-Ace and EtOAc extracts from Taxus baccata, whereas all the extracts showed a variable degree of scavenging effect against DPMD radical. The shoot-EtOAc extract of Cedrus libani had the highest metal-chelation capacity [(58.04±0.70)%]. The shoot extracts of Taxus baccata were determined to have the richest total phenol content, which may contribute to its marked antioxidant activity. Conclusions: The conifer species screened in this study may contain cholinesterase-inhibiting and antioxidant properties, which might be useful against Alzheimer’s disease.

  1. The inhibitory effect of magnolol on cutaneous permeability in mice is probably mediated by a nonselective vascular hyporeactivity to mediators.

    Science.gov (United States)

    Wang, J P; Raung, S L; Chen, C C; Kuo, J S; Teng, C M

    1993-12-01

    In the present study, we demonstrated the inhibitory effect of magnolol on the plasma leakage in passive cutaneous anaphylactic (PCA) reaction, neurogenic inflammation, dorsal skin and ear edema in mice. Hind-paw skin plasma extravasation caused by antidromic stimulation of the saphenous nerve was reduced in mice pretreated with magnolol, diphenydramine or methysergide, but not with indomethacin. Ear edema formation in the PCA reaction was reduced by magnolol in dose-dependent manner. In addition, histamine-, serotonin-, compound 48/80-, bradykinin- and substance P-induced ear edema in mice was also suppressed by magnolol. A dose- and time-dependency of the inhibitory effect of magnolol was demonstrated in histamine- and compound 48/80-induced dorsal skin edema. The maximal inhibitory effect produced by a single dose of magnolol (10 mg/kg) persisted for 1 h, and significant suppression lasted for at least 3 h. In compound 48/80-pretreated mice, the histamine content of the ear was greatly reduced. Bradykinin- and substance P-induced ear edema in compound 48/80-pretreated mice was less severe than that seen in normal mice, but was still significantly reduced by magnolol pretreatment. Moreover, the inhibitory effect of magnolol was more marked than that of diphenhydramine combined with methysergide. These results suggest that the inhibitory effect of magnolol on local edema formation probably occurs through a nonselective inhibition on vascular tissue to prevent the permeability change caused by various mediators.

  2. PERTINENT DRY NEEDLING CONSIDERATIONS FOR MINIMIZING ADVERSE EFFECTS - PART TWO.

    Science.gov (United States)

    Halle, John S; Halle, Rob J

    2016-10-01

    Dry needling (DN) is an evidence based treatment technique that is accepted and used by physical therapists in the United States. This clinical commentary is the second in a two-part series outlining some of the pertinent anatomy and other issues that are needed for optimal utilization of this treatment modality. Part one was an overview of the thorax with a summary of reported adverse effects (AEs) and the underlying anatomy that could be used to minimize patient risk. As is the case with any intervention, the technique of dry needling has some inherent patient risk. The incidence of AEs with this procedure is typically low, ranging from zero to approximately 10 percent. Knowledge of the underlying anatomy can be a key factor associated with decreasing the likelihood of an AE. The second part of this clinical commentary goes beyond the thorax, to explore the anatomy associated with dry needling the abdomen, pelvis, and back. In the abdomen, pelvis and back, dry needling can penetrate the peritoneal cavity or adjacent organs, resulting in AEs. A physiological reaction that is an AE secondary to a needle insertion, pain or fear, is an autonomic vasovagal response. Additionally, suggestions for dealing with the fearful patient, the obese patient, universal precautions, and other clinical considerations, are discussed. The purpose of parts one and part two of this clinical commentary is to minimize the risk of a dry needling AE. Dry needling is an effective adjunctive treatment procedure that is within the recognized scope of practice of the physical therapist. An evidence-based implementation of the procedure must be based on a thorough understanding of the underlying anatomy and the potential risks, with risks communicated to patients via informed consent. Level 5.

  3. Inhibitory effect of aqueous dandelion extract on HIV-1 replication and reverse transcriptase activity

    Directory of Open Access Journals (Sweden)

    Han Huamin

    2011-11-01

    Full Text Available Abstract Background Acquired immunodeficiency syndrome (AIDS, which is caused by the human immunodeficiency virus (HIV, is an immunosuppressive disease that results in life-threatening opportunistic infections. The general problems in current therapy include the constant emergence of drug-resistant HIV strains, adverse side effects and the unavailability of treatments in developing countries. Natural products from herbs with the abilities to inhibit HIV-1 life cycle at different stages, have served as excellent sources of new anti-HIV-1 drugs. In this study, we aimed to investigate the anti-HIV-1 activity of aqueous dandelion extract. Methods The pseudotyped HIV-1 virus has been utilized to explore the anti-HIV-1 activity of dandelion, the level of HIV-1 replication was assessed by the percentage of GFP-positive cells. The inhibitory effect of the dandelion extract on reverse transcriptase activity was assessed by the reverse transcriptase assay kit. Results Compared to control values obtained from cells infected without treatment, the level of HIV-1 replication and reverse transcriptase activity were decreased in a dose-dependent manner. The data suggest that dandelion extract has a potent inhibitory activity against HIV-1 replication and reverse transcriptase activity. The identification of HIV-1 antiviral compounds from Taraxacum officinale should be pursued. Conclusions The dandelion extract showed strong activity against HIV-1 RT and inhibited both the HIV-1 vector and the hybrid-MoMuLV/MoMuSV retrovirus replication. These findings provide additional support for the potential therapeutic efficacy of Taraxacum officinale. Extracts from this plant may be regarded as another starting point for the development of an antiretroviral therapy with fewer side effects.

  4. In vitro and in vivo inhibitory effect of stiripentol on clobazam metabolism.

    Science.gov (United States)

    Giraud, Carole; Treluyer, Jean-Marc; Rey, Elisabeth; Chiron, Catherine; Vincent, Jean; Pons, Gérard; Tran, Agnès

    2006-04-01

    A metabolic interaction between stiripentol (STP), an anticonvulsant agent that inhibits the activity of several cytochromes P450 (P450s), and clobazam (CLB), a 1,5-benzodiazepine, used in association with STP in severe myoclonic epilepsy in infancy was observed in vivo. This interaction was characterized in vitro using cDNA-expressed CYP3A4 and CYP2C19 (main P450 involved in CLB metabolism) to calculate K(i) and IC(50) of stiripentol in comparison with ketoconazole (CYP3A4 inhibitor) and omeprazole (CYP2C19 inhibitor). STP inhibited N-demethylation of CLB to N-desmethylclobazam (NCLB) mediated by CYP3A4 (noncompetitively) and CYP2C19 (competitively) with K(i) = 1.59 +/- 0.07 and 0.516 +/- 0.065 microM and IC(50) = 1.58 microM [95% confidence interval (CI95%) = 1.20-2.08] and 3.29 microM (CI95% = 1.87-5.79), respectively. STP inhibited also more strongly the 4'-hydroxylation of NCLB to 4'-hydroxy-N-desmethylclobazam by CYP2C19 [competitive interaction with K(i) = 0.139 +/- 0.025 microM and IC(50) = 0.276 microM (CI95% = 0.206-0.371)]. The inhibitory effect of STP on CLB demethylation by CYP3A4 was much weaker than that of ketoconazole [IC(50) = 0.023 microM (CI95% = 0.016-0.033)], whereas its effect on NCLB hydroxylation by CYP2C19 was much higher than that of omeprazole [IC(50) = 2.99 microM (CI95% = 2.11-4.24)]. The major in vitro inhibitory effect of STP on CLB metabolism and mostly on NCLB biotransformation is consistent with the changes in vivo in CLB and NCLB plasma concentrations in children treated by the association CLB/STP.

  5. Inhibitory effect of corcin on aggregation of 1N/4R human tau protein in vitro

    Directory of Open Access Journals (Sweden)

    Ali Mohammadi Karakani

    2015-05-01

    Full Text Available Objective(s:Alzheimer's disease (AD is the most common age-related neurodegenerative disorder. One of the hallmarks of AD is an abnormal accumulation of fibril forms of tau protein which is known as a microtubule associated protein. In this regard, inhibition of tau aggregation has been documented to be a potent therapeutic approach in AD and tauopathies. Unfortunately, the available synthetic drugs have modest beneficial efficacy with several side effects. Therefore, pipeline drugs from natural sources with anti-aggregation properties can be useful in the prevention and treatment of AD. Among medicinal plants, saffron (Crocus sativus, L., as a traditional herbal medicine has different pharmacological properties and can be used as treatment for several nervous system impairment including depression and dementia. Crocin as a major constituent of saffron is the glycosylated form of crocetin. Materials and Methods:  In this study, we investigated the inhibitory effect of crocin on aggregation of recombinant human tau protein 1N/4R isoform using biochemical methods and cell culture. Results:  Results revealed that tau protein under the fibrillation condition and in the presence of crocin had enough stability with low tendency for aggregation. Crocin inhibited tau aggregation with IC50 of 100 µg/ml.  Furthermore, transmission electron microscopy images confirmed that crocin could suppress the formation of tau protein filaments. Conclusion: Inhibitory effect of crocin could be related to its interference with nucleation phase that led to increases in monomer species of tau protein. Based on our results, crocin is recommended as a proper candidate to be used in AD treatment.

  6. Synthesis of C-4-Substituted Steviol Derivatives and Their Inhibitory Effects against Hepatitis B Virus.

    Science.gov (United States)

    Lin, Shwu-Jiuan; Su, Ta-Chi; Chu, Chin-Nan; Chang, Yi-Chih; Yang, Li-Ming; Kuo, Yu-Cheng; Huang, Tsurng-Juhn

    2016-12-23

    ent-13-Hydroxykaur-16-ene-19-N-butylureide (6) was one of 33 synthesized C-4-substituted steviol derivatives that were evaluated for their effects on hepatitis B virus (HBV) surface antigen (HBsAg) secretion. The IC50 (16.9 μM) and SI (57.7) values for inhibiting HBV DNA replication of compound 6 were greater than those of the reference compound, lamivudine (3-TC; IC50: 107.5 μM; SI: 22.0). Thus, the anti-HBV mechanism of 6 was investigated, and it specifically inhibited viral gene expression and reduced viral DNA levels, as well as potently attenuated all of the viral promoter activity of HBV-expressing Huh7 cells. Examination of cellular signaling pathways found that 6 inhibited the activities of the nuclear factor (NF)-κB- and activator protein (AP)-1 element-containing promoters, but had no effects on AP-2 or interferon-stimulated response element (ISRE)-containing promoters in HBV-expressing cells. Meanwhile, it significantly eliminated NF-κB and extracellular signal-regulated kinase (ERK)/mitogen-activated protein kinase (MAPK) signaling-related protein levels and inhibited their phosphorylation in HBV-transfected Huh7 cells. The inhibitory potency of 6 against HBV DNA replication was reversed by cotransfecting the NF-κB p65 expression plasmid. Using the MAPK-specific activator anisomycin also reversed the inhibitory effect of 6 on viral DNA replication. The present findings suggest that the anti-HBV mechanism of 6 is partly mediated through the NF-κB and MAPK signaling pathways.

  7. Comparison of inhibitory effects between acetaminophen-glutathione conjugate and reduced glutathione in human glutathione reductase.

    Science.gov (United States)

    Nýdlová, Erika; Vrbová, Martina; Cesla, Petr; Jankovičová, Barbora; Ventura, Karel; Roušar, Tomáš

    2014-09-01

    Acetaminophen overdose is the most frequent cause of acute liver injury. The main mechanism of acetaminophen toxicity has been attributed to oxidation of acetaminophen. The oxidation product is very reactive and reacts with glutathione generating acetaminophen-glutathione conjugate (APAP-SG). Although this conjugate has been recognized to be generally nontoxic, we have found recently that APAP-SG could produce a toxic effect. Therefore, the aim of our study was to estimate the toxicity of purified APAP-SG by characterizing the inhibitory effect in human glutathione reductase (GR) and comparing that to the inhibitory effect of the natural inhibitor reduced glutathione. We used two types of human GR: recombinant and freshly purified from red blood cells. Our results show that GR was significantly inhibited in the presence of both APAP-SG and reduced glutathione. For example, the enzyme activity of recombinant and purified GR was reduced in the presence of 4 mm APAP-SG (with 0.5 mm glutathione disulfide) by 28% and 22%, respectively. The type of enzyme inhibition was observed to be competitive in the cases of both APAP-SG and glutathione. As glutathione inhibits GR activity in cells under physiological conditions, the rate of enzyme inhibition ought to be weaker in the case of glutathione depletion that is typical of acetaminophen overdose. Notably, however, enzyme activity likely remains inhibited due to the presence of APAP-SG, which might enhance the pro-oxidative status in the cell. We conclude that our finding could reflect some other pathological mechanism that may contribute to the toxicity of acetaminophen.

  8. Studies on the mechanism of the inhibitory effects of erucylcarnitine in rat heart mitochondria.

    Science.gov (United States)

    Christophersen, B O; Christiansen, R Z

    1975-06-23

    1. The mechanism of the inhibitory effect of erucylcarnitine on palmityl-carnitine oxidation in rat heart mitochondria was studied. 2. Erucylcarnitine inhibited in the same time the oxidation of [U-14-C]-palmitylcarnitine and the total rate of oxygen uptake. Other acylcarnitines competed as well for the oxidation with radioactive palmitylcarnitine, but they were well oxidized themselves, so that the total oxygen uptake did not decrease. 3. The presence of erucylcarnitine did not change the distribution pattern of Krebs cycle intermediates derived from [U-minus 14 C] palmitylcarnitine except that succinate/malate ratio increased. 4. The presence of erucylcarnitine did not lead to the formation of any beta-oxidation cycle intermediates from [U-minus 14 C] palymitylcarnitine. The formation of beta-hydroxy-palmityl derivative when rotenon was included into the incubation medium, decreased in the presence of erucylcarnitine. 5. It is postulated, that the inhibited entrance of palmityl groups into the beta-oxidation cycle is due to the fact that erucylcarnitine and palmitylcarnitine behave as substrate-competitive inhibitors for long chain acyl-CoA dehydrogenase. 6. There was observed a latency of 1-2 min in the effect of erucylcarnitine on the palmitylcarnitine oxidation, which seems to correspond to the time required for the formation of high amounts of intramitochondrial erucyl-CoA. 7. Erucylcarnitine inhibited the total oxygen uptake with long, medium and short chain acylcarnitines, pyruvate and alpha-ketoglutarate as substrates, while the oxidation of succinate was not affected. 8. Sequestration of free CoA in the form of very slowly metabolized erucyl-CoA is proposed as the partial explanation of the observed inhibitory effects of erucylcarnitine on the oxidation of CoA-dependent substrates (alternatively to the inhibition at the level of acyl-CoA dehydrogenases in case of acylcarnitines).

  9. Inhibitory effect of selenium against Penicillium expansum and its possible mechanisms of action.

    Science.gov (United States)

    Wu, Zhi-Lin; Yin, Xue-Bin; Lin, Zhi-Qing; Bañuelos, Gary S; Yuan, Lin-Xi; Liu, Ying; Li, Miao

    2014-08-01

    Some organic and inorganic salts could inhibit the growth of many pathogens. Selenium (Se), as an essential micronutrient, was effective in improving the plant resistance and antioxidant capacity at a low concentration. Penicillium expansum is one of the most important postharvest fungal pathogens, which can cause blue mold rot in various fruits and vegetables. In this study, the inhibitory effect of Se against P. expansum was evaluated. The result showed that Se strongly inhibited spore germination, germ tube elongation, and mycelial spread of P. expansum in the culture medium. The inhibitory effect was positively related to the concentration of Se used. Fluorescence microscopy observation of P. expansum conidia stained with propidium iodide (PI) indicated that the membrane integrity decreased to 37 % after the conidia were treated with Se (20 mg/l) for 9 h. With the use of an oxidant-sensitive probe 2,7-dichlorofluorescin (DCHF-DA), we found that Se at 15 mg/l could induce the generation of intracellular reactive oxygen species (ROS). Furthermore, methane dicarboxylic aldehyde (MDA) content, hydrogen peroxide (H2O2), and superoxide anion (O2 (-)) production rate in P. expansum spores exposed to Se increased markedly. Compared with the control, the activities of superoxide dismutase (SOD) and the content of glutathione (GSH) were reduced, confirming that damage of Se to cellular oxygen-eliminating system is the main reason. These results suggest that Se might serve as a potential alternative to synthetic fungicides for the control of the postharvest disease of fruit and vegetables caused by P. expansum.

  10. Inhibitory effect of Xenorhabdus nematophila TB on plant pathogens Phytophthora capsici and Botrytis cinerea in vitro and in planta.

    Science.gov (United States)

    Fang, Xiangling; Zhang, Manrang; Tang, Qian; Wang, Yonghong; Zhang, Xing

    2014-03-06

    Entomopathogenic bacteria Xenorhabdus spp. produce secondary metabolites with potential antimicrobial activity for use in agricultural productions. This study evaluated the inhibitory effect of X. nematophila TB culture on plant pathogens Botrytis cinerea and Phytophthora capsici. The cell-free filtrate of TB culture showed strong inhibitory effects (>90%) on mycelial growth of both pathogens. The methanol-extracted bioactive compounds (methanol extract) of TB culture also had strong inhibitory effects on mycelial growth and spore germinations of both pathogens. The methanol extract (1000 μg/mL) and cell-free filtrate both showed strong therapeutic and protective effects (>70%) on grey mold both in detached tomato fruits and plants, and leaf scorch in pepper plants. This study demonstrates X. nematophila TB produces antimicrobial metabolites of strong activity on plant pathogens, with great potential for controlling tomato grey mold and pepper leaf scorch and being used in integrated disease control to reduce chemical application.

  11. Inhibitory control in bilinguals and musicians: event related potential (ERP) evidence for experience-specific effects

    National Research Council Canada - National Science Library

    Moreno, Sylvain; Wodniecka, Zofia; Tays, William; Alain, Claude; Bialystok, Ellen

    2014-01-01

    Bilinguals and musicians exhibit behavioral advantages on tasks with high demands on executive functioning, particularly inhibitory control, but the brain mechanisms supporting these differences are unclear...

  12. Inhibitory effects of (-)-epigallocatechin-3-gallate from green tea on the growth of Babesia parasites.

    Science.gov (United States)

    Aboulaila, M; Yokoyama, N; Igarashi, I

    2010-04-01

    (-)-Epigallocatechin-3-gallate (EGCG) is the major tea catechin and accounts for 50-80% of the total catechin in green tea. (-)-Epigallocatechin-3-gallate has antioxidant, anti-inflammatory, anti-microbial, anti-cancer, and anti-trypanocidal activities. This report describes the inhibitory effect of (-)-Epigallocatechin-3-gallate on the in vitro growth of bovine Babesia parasites and the in vivo growth of the mouse-adapted rodent babesia B. microti. The in vitro growth of the Babesia species was significantly (Pparasites showed no re-growth at 25 microM for B. bovis and B. bigemina in the subsequent viability test. The drug significantly (Pparasites completely cleared on day 14 and 16 post-inoculation in the 5 and 10 mg/kg treated groups, respectively. These findings highlight the potentiality of (-)-Epigallocatechin-3-gallate as a chemotherapeutic drug for the treatment of babesiosis.

  13. STUDY ON THE INHIBITORY EFFECT OF ANTISENSE ETAR OLIGODEOXYNUCLEOTIDES ON THE PROLIFERATION OF VASCULAR SMOOTH CELLS

    Institute of Scientific and Technical Information of China (English)

    张岚; 张柏根; 张纪蔚; 钱济先; 张皓; 黄晓钟

    2002-01-01

    Objective To study the inhibitory effect of antisense endothelin receptor A (ETAR) on the proliferation of the vascular smooth muscle cells. Methods The sense, antisense and mismatched ODNs for ETAR were designed and synthetized. The study was carried out using MTT method and binding assays.Results ETAR-ODNs could move successfully across VSMC membranes. Photo-absorption in the MTT test was reduced significantly (P<0.05) in the antisense group at 5μmol/L; the reduction of CPM also occurred in the 125I-ET-1 specific binding assay; and the sense and mismatched ODNs groups did not show this reduction. Conclusion Our study suggested that the antisense oligomers inhibited the proliferation of VSMCs by hindering the translation of target mRNA and by reducing the production of related protein.

  14. Inhibitory Effect of Plant Manilkara subsericea against Biological Activities of Lachesis muta Snake Venom

    Directory of Open Access Journals (Sweden)

    Eduardo Coriolano De Oliveira

    2014-01-01

    Full Text Available Snake venom is composed of a mixture of substances that caused in victims a variety of pathophysiological effects. Besides antivenom, literature has described plants able to inhibit injuries and lethal activities induced by snake venoms. This work describes the inhibitory potential of ethanol, hexane, ethyl acetate, or dichloromethane extracts and fractions from stem and leaves of Manilkara subsericea against in vivo (hemorrhagic and edema and in vitro (clotting, hemolysis, and proteolysis activities caused by Lachesis muta venom. All the tested activities were totally or at least partially reduced by M. subsericea. However, when L. muta venom was injected into mice 15 min first or after the materials, hemorrhage and edema were not inhibited. Thus, M. subsericea could be used as antivenom in snakebites of L. muta. And, this work also highlights Brazilian flora as a rich source of molecules with antivenom properties.

  15. Inhibitory effects of whisky polyphenols on melanogenesis in mouse B16 melanoma cells.

    Science.gov (United States)

    Yoshioka, Sayaka; Terashita, Takao; Yoshizumi, Hajime; Shirasaka, Norifumi

    2011-01-01

    Whisky exerts an inhibitory effect on melanogenesis in B16 cells, the anti-melanogenic activity being positively correlated with the aging period and anti-oxidative activity of whisky. We examined the correlation between the inhibition of melanogenesis and the concentration of each compound in various whiskies to evaluate the importance of 11 different whisky polyphenols, including ellagic acid, gallic acid and lyoniresinol, in the anti-melanogenic activity of whisky. The concentration of all the compounds was positively correlated with the anti-melanogenic activity of whisky. Ellagic acid, gallic acid and lyoniresinol were the predominant polyphenols in the whiskies measured by HPLC. These three compounds also significantly inhibited the melanogenesis and tyrosinase activity in B16 cells. Ellagic acid, gallic acid and lyoniresinol were confirmed as the major participants in the anti-melanogenic activity of whisky.

  16. Inhibitory effect of plant Manilkara subsericea against biological activities of Lachesis muta snake venom.

    Science.gov (United States)

    De Oliveira, Eduardo Coriolano; Fernandes, Caio Pinho; Sanchez, Eladio Flores; Rocha, Leandro; Fuly, André Lopes

    2014-01-01

    Snake venom is composed of a mixture of substances that caused in victims a variety of pathophysiological effects. Besides antivenom, literature has described plants able to inhibit injuries and lethal activities induced by snake venoms. This work describes the inhibitory potential of ethanol, hexane, ethyl acetate, or dichloromethane extracts and fractions from stem and leaves of Manilkara subsericea against in vivo (hemorrhagic and edema) and in vitro (clotting, hemolysis, and proteolysis) activities caused by Lachesis muta venom. All the tested activities were totally or at least partially reduced by M. subsericea. However, when L. muta venom was injected into mice 15 min first or after the materials, hemorrhage and edema were not inhibited. Thus, M. subsericea could be used as antivenom in snakebites of L. muta. And, this work also highlights Brazilian flora as a rich source of molecules with antivenom properties.

  17. INHIBITORY EFFECT OF CHITOSAN OLIGOSACCHARIDE ON HUMAN HEPATOMA CELLS IN VITRO.

    Science.gov (United States)

    Liu, Likun; Xin, Yi; Liu, Jia; Zhang, Ershao; Li, Weiling

    2017-01-01

    Chitosan oligosaccharide, the degradation products of chitin, was reported to have a wide range of physiological functions and biological activities. In this study, we explored the inhibitory effect of Chitosan oligosaccharide on human hepatoma cells. MTT assay was applied to detect cell viability of the human hepatoma cells treated with Chitosan oligosaccharide. Flow cytometric analysis was used to investigate the apoptosis of the human hepatoma cells treated with Chitosan oligosaccharide. We employed western blot to investigate the underlying mechanisms involved in the apoptosis. Our data indicated that chitosan oligosaccharide dose-dependently inhibited the growth of hepatoma cells and induced apoptosis. On the molecular level, chitosan oligosaccharide decreased Bcl-2 and increased Caspase-3 expression which may be related to the apoptosis of hepatoma cells. Our results provide an experimental basis for the clinical development of Chitosan oligosaccharide as a novel anti-hepatoma drug.

  18. Inhibitory Effect of Triterpenoids from Panax ginseng on Coagulation Factor X

    Directory of Open Access Journals (Sweden)

    Lingxin Xiong

    2017-04-01

    Full Text Available Enzymes involved in the coagulation process have received great attention as potential targets for the development of oral anti-coagulants. Among these enzymes, coagulation factor Xa (FXa has remained the center of attention in the last decade. In this study, 16 ginsenosides and two sapogenins were isolated, identified and quantified. To determine the inhibitory potential on FXa, the chromogenic substrates method was used. The assay suggested that compounds 5, 13 and 18 were mainly responsible for the anti-coagulant effect. Furthermore, these three compounds also possessed high thrombin selectivity in the thrombin inhibition assay. Furthermore, Glide XP from Schrödinger was employed for molecular docking to clarify the interaction between the bioactive compounds and FXa. Therefore, the chemical and biological results indicate that compounds 5 (ginsenoside Rg2, 13 (ginsenoside Rg3 and 18 (protopanaxtriol, PPT are potential natural inhibitors against FXa.

  19. Inhibitory effect of sulfated lentinan and lentinan against tobacco mosaic virus (TMV) in tobacco seedlings.

    Science.gov (United States)

    Wang, Jie; Wang, Hong-Yan; Xia, Xiao-Ming; Li, Peng-peng; Wang, Kai-Yun

    2013-10-01

    The antiviral activities of sulfated lentinan (sLNT) and lentinan (LNT) against tobacco mosaic virus (TMV) in tobacco seedlings and the underlying mechanism were investigated. Compared with LNT, sLNT showed significantly higher inhibitory effects on viral infection and TMV multiplication in a dose-dependent way, which might be due to its binding with TMV coat protein. In addition, both sLNT and LNT induced the transient production of H2O2 and expression of some defense-related genes (stilbene synthase, glucanase, acidic chitinase class IV, phenylalanine ammonia-lyase and 5-epi-aristolochene synthase) both locally and systemically. These results suggested that sLNT and LNT could control TMV incidence and the action mechanism might be associated with the affinity towards TMV coat protein and activation of some defense genes. Copyright © 2013 Elsevier B.V. All rights reserved.

  20. Inhibitory effects on cytochrome p450 enzymes of pentamidine and its amidoxime pro-drug.

    Science.gov (United States)

    Bürenheide, Anja; Kunze, Thomas; Clement, Bernd

    2008-07-01

    Pentamidine is an antimicrobial drug, intravenously used in the treatment of trypanosomiasis, leishmaniasis or pneumocystis pneumonia. To elucidate potential drug interactions with pentamidine and N,N'-dihydroxypentamidine, respectively, the cytochrome P450 (CYP450) inhibitory properties of these compounds were determined. The study was performed in vitro by using human liver microsomes and marker substrates of several CYP450 isoenzymes. Marker activities were investigated by high-performance liquid chromatography in presence of known selective inhibitors or at different concentrations of pentamidine and N,N'-dihydroxypentamidine, respectively. No or only minor influence on CYP1A2, 2A6, 2C9, 2C19, 2D6, 2E1 and 3A4 marker activities could be observed, suggesting that neither of the tested substances would exert a significant effect on hepatic CYP450 isoenzymes responsible for the metabolism of co-administrated drugs in vivo. However, in vivo studies are needed before final conclusions can be drawn.

  1. Preparation of six quinazoline schiff bases and their inhibitory effect on HHCC and Bcap-37 cells

    Institute of Scientific and Technical Information of China (English)

    陈惠; 孙晓莉; 刘志红; 张生勇; 药立波

    2003-01-01

    Objective: To prepare six quinazoline schiff bases by six steps of chemistry organic synthesis and test their inhibitory effect on hepatomacellular carcinoma cells HHCC and mammary cancer cell Bcap-37, furthmore,to compare their antitumor activities on these two kinds of cells. Methods: 2-Amino-5-nitro-benzylcarbonitrile was the initial material, and it was under the reaction of hydrolysis, ring-closing, halogenation, addition, reduction and substitution in turn to get the six quinazoline schiff bases, MTT method was adopted to compare their anticancer activities against the two cancer cells. Result and Conclusion: Six 6-imine-4-halo substituted anilinoquinozolines were prepared. The anticancer activities against both HHCC and Bcap-37were found, furthermore, they have more potency that on HHCC than on Bcap-37. In the six compounds, the schiff base Ⅵ is the most potent compound.

  2. Characterization of polysaccharides with marked inhibitory effect on lipid accumulation in Pleurotus eryngii.

    Science.gov (United States)

    Chen, Jingjing; Yong, Yangyang; Xing, Meichun; Gu, Yifan; Zhang, Zhao; Zhang, Shizhu; Lu, Ling

    2013-09-12

    Mushrooms have a great potential for the production of useful bioactive metabolites. To explore the bioactive compounds from edible mushrooms for interfering with the development of macrophage-derived foam cells, which is recognized as the hallmark of early atherosclerosis, eight types of mushrooms polysaccharides had been selected to be tested. Consequently, different mushrooms polysaccharides displayed diverse component profiles. Of polysaccharides that we tested, the Pleurotus eryngii polysaccharide had the strongest inhibitory effect on lipid accumulation. Furthermore, through fractionation of DEAE-52 and Sephadex G-100, the polysaccharide from P. eryngii had been successfully purified and identified. By the analysis of IR, GC, and HPLC, the purified polysaccharide was estimated to be 30-38 kDa for the average molecular weight with the monosaccharide composition mainly composed of D-types of mannose, glucose and galactose. Findings presented in this report firstly provide direct evidence, which links the purified polysaccharide moiety with the biological function in foam-cell model.

  3. In vitro inhibitory effect on pancreatic lipase activity of subfractions from ethanol extracts of fermented Oats (Avena sativa L.) and synergistic effect of three phenolic acids.

    Science.gov (United States)

    Cai, Shengbao; Wang, Ou; Wang, Mengqian; He, Jianfeng; Wang, Yong; Zhang, Di; Zhou, Feng; Ji, Baoping

    2012-07-25

    The purpose of the present work is to study the pancreatic lipase inhibitory effects of different subfractions (n-hexane, ethyl acetate (EA), n-butanol, and water) from ethanol extracts of nonfermented and fungi-fermented oats and to delineate the interactions of three primary phenolic acids in the EA subfractions. The EA subfraction showed the highest inhibitory effect on pancreatic lipase activity at 1.5 mg/mL compared to the other subfractions, regardless of whether the oats were fermented. Meanwhile, both of the EA subfractions of two fungi-fermented oats demonstrated more effective inhibitory activity than that of nonfermented oats. A positive correlation between the total phenolics content and inhibitory activity was found. The inhibitory ability of the EA subfraction from nonfermented or fermented oats also displayed a dose-dependent effect. The standards of caffeic, ferulic, and p-coumaric acids, mainly included in EA subfractions of fermented oats, also displayed a dose-dependent inhibitory effect. A synergistic effect of each binary combination of p-coumaric, ferulic, and caffeic acids was observed, especially at 150.0 μg/mL. Those results indicate that fungi-fermented oats have a more effective inhibitory ability on pancreatic lipase and polyphenols may be the most effective component and could be potentially used for dietary therapy of obesity.

  4. In vitro inhibitory effects of asiaticoside and madecassoside on human cytochrome P450.

    Science.gov (United States)

    Winitthana, T; Niwattisaiwong, N; Patarapanich, C; Tantisira, M H; Lawanprasert, S

    2011-06-01

    The inhibitory effects and types of inhibition of asiaticoside and madecassoside on human CYPs were studied in vitro using recombinant human CYPs. The median inhibitory concentrations (IC50) of asiaticoside and madecassoside were determined for CYP1A2, CYP2C9, CYP2C19, CYP2D6, CYP2E1 and CYP3A4. Asiaticoside inhibited CYP2C19 (IC50 = 412.68 ± 15.44 μM) and CYP3A4 (IC50=343.35 ± 29.35 μM). Madecassoside also inhibited CYP2C19 (IC50 = 539.04 ± 14.18 μM) and CYP3A4 (IC50 = 453.32 ± 39.33 μM). Asiaticoside and madecassoside had no effect on the activities of CYP1A2, CYP2C9 and CYP2D6 and CYP2E1. Assessment of mechanism-based inhibition and the type of inhibition were performed for asiaticoside and madecassoside with CYP2C19 and CYP3A4. These results suggested that madecassoside is a mechanism-based inhibitor of CYP2C19 and CYP3A4. Assessment of mechanism-based inhibition by asiaticoside was limited by its low solubility. Asiaticoside exhibited non-competitive inhibition of CYP2C19 (Ki=385.24 ± 8.75 μM) and CYP3A4 (Ki = 535.93 ± 18.99 μM). Madecassoside also showed non-competitive inhibition of CYP2C19 (Ki = 109.62 ± 6.14 μM) and CYP3A4 (Ki = 456.84 ± 16.43 μM). These results suggest that asiaticoside and madecassoside could cause drug-drug interactions via inhibition of CYP2C19 and CYP3A4. An in vivo study is needed to examine this further.

  5. [Inhibitory effect of thalidomide combined with interferon on the proliferation of Kasumi-1 cells].

    Science.gov (United States)

    Xu, Hao; Mi, Ruihua; Fan, Ruihua; Yin, Qingsong; Wang, Xiaojiao; Wei, Xudong

    2015-09-01

    To explore the inhibitory effect of thalidomide combined with interferon (IFN) on the human acute myeloid leukemia cell line Kasumi- 1 and its mechanism. The inhibitiory effect of Kasumi- 1 cells by thalidomide, interferon or combination was detected by CCK- 8 method, the apoptosis by flow cytometry, the expression of apoptosis related proteins by Western blot, vascular endothelial growth factor (VEGF) concentration in culture supernatant by ELISA. Thalidomide inhibited the proliferation of Kasumi- 1 in a dose- dependent manner from 50 μg/ml to 500 μg/ml with an IC₅₀ of (451.13 ± 6.92)μg/ml at 24 h and (362.50 ± 14.52)μg/ml at 48 h. IFN also demonstrated the inhibitory capacity in a dose-dependent manner from 500 U/ml to 5 000 U/ml, with an IC₅₀ of (2 209 ± 127) U/ml at 24 h and (1 393±63) U/ml at 48 h. The apoptosis rates of Kasumi-1 cells treated with thalidomide 350 μg/ml or IFN 1 400 U/ml for 48 h were (14.68 ± 2.61) % and (21.71 ± 0.71)%, respectively, significantly higher than control group (PKasumi-1 cells decreased, while p-P38, Bax, cytochrome C, cleaved-Caspase-3, 8, 9 increased after treated with thalidomide 350 μg/ml or IFN 1 400 U/ml for 48 h. When treated with the combination agents, the expression of Bcl-2 further decreased and p-P38, Bax, cytochrome C, cleaved-Caspase-3, 8, 9 further increased as compared with each single agent (P Kasumi-1 cells probably through inducing apoptosis via the mitochondrial pathway, death receptor pathway and P38 MAPK pathway, as well as inhibiting VEGF secretion.

  6. [Inhibitory effect of DMPP on soil nitrification as affected by soil moisture content, pH and organic matter].

    Science.gov (United States)

    Xue, Yan; Wu, Zhi-Jie; Zhang, Li-Li; Gong, Ping; Dong, Xin-Xin; Nie, Yan-Xia

    2012-10-01

    A laboratory incubation test with meadow brown soil was conducted to study the inhibitory effect of 3,4-dimethylpyrazole phosphate (DMPP) on soil nitrification as affected by soil moisture content (40%, 60% and 80% of the maximum field capacity), pH (4, 7 and 10), and organic matter (retained and removal). With the decrease of soil moisture content, the degradation of DMPP in soil tended to slow down, and the oxidation of soil NH4+ was more inhibited. At pH 10, more DMPP was remained in soil, and had the greatest inhibitory effect; at pH 7 and pH 4, the DMPP was lesser remained, with a smaller inhibitory effect. The removal of organic matter prolonged the remaining time of DMPP in soil, and decreased the apparent soil nitrification rate significantly.

  7. Concentration-dependent inhibitory and stimulating effects of amphiphilic ammonium salts upon photosynthetic activity of spinach chloroplasts.

    Science.gov (United States)

    Sersen, F; Král'ová, K

    1996-02-01

    The effects of piperidinopropylesters of 2-, 3- and 4-alkoxy substituted phenylcarbamic acids (PPACs) on oxygen evolution rate (OER) in spinach chloroplasts were investigated. PPAGs show concentration-dependent effects, namely OER inhibition at higher effector concentrations and OER stimulation at lower concentrations, i.e. below the inhibitory concentration range. The inhibitory efficiency of PPACs showed dependence on the alkyl chain length of the alkoxy substituent as well as on the position of this substituent on the benzene ring. Using EPR spectroscopy and fluorescence measurements it was confirmed that the site of PPAC inhibitory action is the donor side of photosystem 2, where D1 and D2 proteins are situated, namely the intermediates Z+/Y+, and the manganese cluster containing protein as well. The stimulating effects of PPACs on OER in spinach chloroplasts at relatively low effector concentrations are caused by photophosphorylation uncoupling due to protonophore properties of the effectors.

  8. Inhibitory effect of aqueous extract of Echinacea purpurea and Nerium oleander on HSV-1 multiplication

    Directory of Open Access Journals (Sweden)

    Maliheh Farahani

    2014-02-01

    Full Text Available Background: Treatment of HSV-1 infections with the available chemical drugs may have some problems such as drug resistance and virus latency. Therefore, there is a requirement for new antiherpes drugs in today's world. The present study was carried out to analyze the inhibitory effect of Echinacea purpurea and Nerium oleander plants with ethnomedical background on HSV-1 replication. Methods: Plants were extracted by decoction method to obtain aqueous extract. These extracts were screened for their cytotoxicity against Hep-2 cell line by CPE (cytopathic effect assay. Antiviral effect of the plant extracts were determined by the virus cytopathic effect inhibition assay. Results: Nerium oleander extract had the highest toxicity (>0.1 μg/ml on Hep-2 cells and Echinacea purpurea extract exhibited significant antiherpes effect at nontoxic concentrations used on the cell lines. Findings indicated that Echinacea purpurea extract inhibited HSV-1 multiplication at concentrations >400 μg/ml. Conclusion: Echinacea purpurea plant had no any effect on cells at nontoxic concentrations and inhibited HSV-1 multiplication at concentrations >400 μg/ml. Further research is needed to find out the anti herpetic mechanism of this plant.

  9. 43 CFR 46.115 - Consideration of past actions in the analysis of cumulative effects.

    Science.gov (United States)

    2010-10-01

    ... Environmental Quality § 46.115 Consideration of past actions in the analysis of cumulative effects. When... Memorandum on Consideration of Past Actions in Cumulative Effects Analysis” dated June 24, 2005, or any... 43 Public Lands: Interior 1 2010-10-01 2010-10-01 false Consideration of past actions in...

  10. Multilingual Stroop Performance: Effects of Trilingualism and Proficiency on Inhibitory Control

    Science.gov (United States)

    Marian, Viorica; Blumenfeld, Henrike K.; Mizrahi, Elena; Kania, Ursula; Cordes, Anne-Kristin

    2013-01-01

    Previous research suggests that multilinguals' languages are constantly co-activated and that experience managing this co-activation changes inhibitory control function. The present study examined language interaction and inhibitory control using a colour-word Stroop task. Multilingual participants were tested in their three most proficient…

  11. Mechanisms underlying the inhibitory effect of the feed contaminant deoxynivalenol on glucose absorption in broiler chickens.

    Science.gov (United States)

    Awad, W A; Ghareeb, K; Zentek, J

    2014-10-01

    Deoxynivalenol (DON), a major contaminant of cereals and grains, is of public health concern worldwide and has been shown to reduce the electrogenic transport of glucose. However, the full effects of Fusarium mycotoxins on nutrient absorption are still not clear. The aim of this study was to investigate whether decreased nutrient absorption was due to specific effects on transporter trafficking in the intestine and whether inhibition of phosphoinositol-3-kinase (PI-3-kinase) affected the electrogenic jejunal transport of glucose. Jejunal mucosa of 6-week-old broiler chickens were mounted in Ussing chambers and treated with DON, wortmannin (a specific inhibitor of PI-3-kinase), DON + wortmannin, phlorizin and cytochalasin B. DON was found to decrease the short-circuit current (Isc) after glucose addition. A similar decline in Isc after glucose addition was observed following pre-application of wortmannin, or phlorizin (Na(+)/glucose co-transporter, SGLT1 inhibitor). The results indicate that DON decreased glucose absorption in the absence of wortmannin or phlorizin but had no additional effect on glucose absorption in their presence. Glucose transport was not affected by cytochalasin B (facilitative glucose transporter, GLUT2 inhibitor). The study provides evidence that the suppressive effect of DON on the electrogenic transport of glucose may be due to an inhibitory activity of the PI3 kinase pathway and intestinal SGLT1. Furthermore, the effect of cytochalasin B on glucose transport in chicken tissues differs from that in mammals.

  12. Inhibitory Effects of Gymnema (Gymnema sylvestre Leaves on Tumour Promotion in Two-Stage Mouse Skin Carcinogenesis

    Directory of Open Access Journals (Sweden)

    Ken Yasukawa

    2014-01-01

    Full Text Available Ethanol extracts of gymnema (Gymnema sylvestre leaves exhibited marked antitumour-promoting activity in an in vivo two-stage carcinogenesis test in mice using 7,12-dimethylbenz[a]anthracene as an initiator and 12-O-tetradecanoylphorbol-13-acetate (TPA as a promoter. From the active fraction of the ethanol extract of the gymnema leaves, three triterpenoids were isolated and identified. These compounds were evaluated for their inhibitory effects on TPA-induced inflammation (1 µg/ear in mice. The tested compounds showed marked anti-inflammatory effects, with a 50% inhibitory dose of 50–555 nmol/ear.

  13. Inhibitory Effects of Gymnema (Gymnema sylvestre) Leaves on Tumour Promotion in Two-Stage Mouse Skin Carcinogenesis.

    Science.gov (United States)

    Yasukawa, Ken; Okuda, Sakiko; Nobushi, Yasuhito

    2014-01-01

    Ethanol extracts of gymnema (Gymnema sylvestre) leaves exhibited marked antitumour-promoting activity in an in vivo two-stage carcinogenesis test in mice using 7,12-dimethylbenz[a]anthracene as an initiator and 12-O-tetradecanoylphorbol-13-acetate (TPA) as a promoter. From the active fraction of the ethanol extract of the gymnema leaves, three triterpenoids were isolated and identified. These compounds were evaluated for their inhibitory effects on TPA-induced inflammation (1 µg/ear) in mice. The tested compounds showed marked anti-inflammatory effects, with a 50% inhibitory dose of 50-555 nmol/ear.

  14. [Inhibitory effect of imperatorin and isoimperatorin on activity of cytochrome P450 enzyme in human and rat liver microsomes].

    Science.gov (United States)

    Cao, Yan; Zhong, Yu-Huan; Yuan, Mei; Li, Hua; Zhao, Chun-Jie

    2013-04-01

    Imperatorin (IM) and isoimperatorin (ISOIM) are major active components of common herbal medicines from Umbelliferae plants, and widely used in clinic. This article studies the inhibitory effect of IM and ISOIM on the activity of cytochrome P450 (CYP) enzyme, and assesses their potential drug-drug interaction. IM and ISOIM were incubated separately with human or rat liver microsomes for 30 min, with phenacetin, bupropion, tolbutamide, S-mephenytoin, dextromethorphan and midazolam as probe substrates. Metabolites of the CYP probe substrates were determined by LC-MS/MS, and IC50 values were calculated to assess the inhibitory effect of the two drugs on human CYP1A2, 2B6, 2C9, 2C19, 2D6 and 3A4 enzymes, as well as on rat CYP1A2, 2B6, 2D2 and 3A1/2, and grade their inhibitory intensity. In human liver microsomes, IM and ISOIM showed different inhibitory effects on all of the six CYP isoenzymes. They were strong inhibitors for 1A2 and 2B6. The IC50 values were 0.05 and 0.20 micromol x L(-1) for 1A2, and 0.18 and 1.07 micromol x L(-1) for 2B6, respectively. They also showed moderate inhibitory effect on 2C19, and weak effect on 2C9, 2D6 and 3A4. In rat liver microsomes, IM and ISOIM were identified as moderate inhibitors for 1A2, with IC50 values of 1.95 and 2.98 micromol x L(-1). They were moderate and weak inhibitors for 2B6, with IC50 values of 6.22 and 21.71 micromol x L(-1), respectively. They also had weaker inhibitory effect on 2D2 and 3A1/2. The results indicated that IM and ISOIM had extensive inhibitory effects on human CYP enzymes. They are strong inhibitors of CYP1 A2 and 2B6 enzymes. However, it is worth noting the interaction arising from the inhibitory effect of CYP enzymes in clinic.

  15. Fungal inhibitory effect of Citrus Limon peel essential oil on Candida albicans

    Directory of Open Access Journals (Sweden)

    Iwan Hernawan

    2015-06-01

    Full Text Available Background: Oral candidiasis is an opportunistic infections due to Candida albicans that often found in people with HIV/AIDS. Anti-fungi, polyne and azole, are used in the treatment of oral candidiasis, but often cause persistence and recurrence. Citrus Limon peel contains terpenoids capable of inhibiting the synthesis of ergosterol, a component of the fungal cell wall that helps to maintain cell membrane permeability. Essential oil derived from citrus limon peel, thus, is expected to inhibit the growth of Candida albicans. Purpose: This research was aimed to know how essential oil derived from citrus Limon peel can inhibit the growth of Candida albicans. Method: This research was a laboratory experimental research carried out in three phases. First, essential oil was made with cold pressing method, and then the concentration of 100% was diluted to 50%, 12.5%, 6.25%, 3.125%, 1.56% and 0.78%. A test was conducted on the culture of Candida albicans in Sabouraud broth, accompanied by control (+ and (-. Second, the dilution of essential oil was conducted to alter the concentration with inhibitory power, from the strongest one to the weakest one, and then it was tested on the culture of Candida albicans. Third, spreading was carried out from liquid culture to agar media in order to measure the number of colonies. Result: Candida albicans did not grow on media with 100% essential oil treatment, but it grew on media with 50% essential oil treatment. In the second phase, dilution of 100%, 90%, 80%, 70%, 60% and 50% was conducted. The growth of Candida albicans was found on the treatment media of 60% and 50%. On the agar media, the growth occurred in the cultured medium treated with 70%. Conclusion: The minimum inhibitory power of essential oil derived from citrus Limon peel against Candida albicans was in the concentration of 80%. Essential oil derived from citrus Limon peel has antifungal effect and potential as a therapeutic agent for oral candidiasis.

  16. Does Acupuncture Needling Induce Analgesic Effects Comparable to Diffuse Noxious Inhibitory Controls?

    Directory of Open Access Journals (Sweden)

    Juerg Schliessbach

    2012-01-01

    Full Text Available Diffuse noxious inhibitory control (DNIC is described as one possible mechanism of acupuncture analgesia. This study investigated the analgesic effect of acupuncture without stimulation compared to nonpenetrating sham acupuncture (NPSA and cold-pressor-induced DNIC. Forty-five subjects received each of the three interventions in a randomized order. The analgesic effect was measured using pressure algometry at the second toe before and after each of the interventions. Pressure pain detection threshold (PPDT rose from 299 kPa (SD 112 kPa to 364 kPa (SD 144, 353 kPa (SD 135, and 467 kPa (SD 168 after acupuncture, NPSA, and DNIC test, respectively. There was no statistically significant difference between acupuncture and NPSA at any time, but a significantly higher increase of PPDT in the DNIC test compared to acupuncture and NPSA. PPDT decreased after the DNIC test, whereas it remained stable after acupuncture and NPSA. Acupuncture needling at low pain stimulus intensity showed a small analgesic effect which did not significantly differ from placebo response and was significantly less than a DNIC-like effect of a painful noninvasive stimulus.

  17. The inhibitory effect of locally injected dexmedetomidine on carrageenan-induced nociception in rats.

    Science.gov (United States)

    Honda, Yuka; Higuchi, Hitoshi; Matsuoka, Yoshikazu; Yabuki-Kawase, Akiko; Ishii-Maruhama, Minako; Tomoyasu, Yumiko; Maeda, Shigeru; Morimatsu, Hiroshi; Miyawaki, Takuya

    2015-10-05

    Recent studies showed that the administration of dexmedetomidine relieved hyperalgesia in the presence of neuropathic pain. These findings have led to the hypothesis that the local administration of dexmedetomidine is useful for relieving acute inflammatory nociception, such as postoperative pain. Thus, we evaluated the inhibitory effect of locally injected dexmedetomidine on acute inflammatory nociception. Acute inflammatory nociception was induced by an intraplantar injection of 1% carrageenan into the hindpaws of rats, and dexmedetomidine was also injected combined with carrageenan. The paw withdrawal threshold based on von Frey filament stimulation was measured until 12 h after injection. We compared the area under the time-curve (AUC) between carrageenan and carrageenan with dexmedetomidine. To clarify that the action of dexmedetomidine was via α2-adrenoceptors, we evaluated the effect of yohimbine, a selective antagonist of α2-adrenoceptors, on the anti-nociception of dexmedetomidine. As the results, the intraplantar injection of carrageenan with over 10 μM dexmedetomidine significantly increased AUC, compared to that with only carrageenan injection. This effect of dexmedetomidine was reversed by the addition of yohimbine to carrageenan and dexmedetomidine. These results demonstrated that the locally injected dexmedetomidine was effective against carrageenan-induced inflammatory nociception via α2-adrenoceptors. The findings suggest that the local injection of dexmedetomidine is useful for relieving local acute inflammatory nociception.

  18. Hemolytic activity and platelet aggregation inhibitory effect of vipoxin's basic sPLA2 subunit

    Science.gov (United States)

    Goranova, Yana; Pantcheva, Ivayla; Atanasov, Vasil; Danchev, Dobri; Petrova, Svetla

    2013-01-01

    In the present study we evaluated the effect of secreted phospholipase A2 (sPLA2) (the toxic subunit of the heterodimeric neurotoxin vipoxin, isolated from the Bulgarian long-nosed viper Vipera ammodytes meridionalis) on hemolysis, erythrocyte morphology and platelet aggregation. Hemolytic activity of sPLA2 was examined in the presence of saturated (palmitic) and unsaturated (oleic) fatty acids and it was found that oleic acid increased the hemolytic activity of sPLA2 in a concentration-dependent manner, compared to the effect of palmitic acid and controls. The addition of heparin to red blood cells (RBC) suspension containing sPLA2 or mixture of sPLA2 and the corresponding fatty acid led to an inhibition of hemolytic activity. The effect of sPLA2 on RBC morphology resulted in formation of echinocytes (spherocyte subtype), suggesting that RBC could be the possible targets attacked by sPLA2. Vipoxin sPLA2 inhibited (in a dose-dependent manner) platelet aggregation when arachidonic acid and collagen were used as inducers, while in the case of ADP its inhibitory effect was inappreciable. PMID:24678250

  19. Is harsh caregiving effective in toddlers with low inhibitory control? An experimental study in the food domain.

    Science.gov (United States)

    Rigal, Natalie; Rubio, Bérengère; Monnery-Patris, Sandrine

    2016-05-01

    The aim of our study is to evaluate the validity of the "Caregiving×Temperament Paradigm" in the food domain. In this study, two prototypes of caregiving control have been contrasted: Harsh (forceful measures to curve the child's behavior) versus Gentle control (supportive measures to direct the child's behavior). In food domain, the most effective control to help a child to overcome initial dislike is repeated exposure. Our first objective was to test whether the repeated exposure displayed in a gentle context has a more benefical effect on dislike shifting than the one displayed in a harsh context. Our second objective was to assess whether this effect was moderated by a temperamental characteristic (child's inhibitory control). A randomized experimental protocol was used in day care-centers, involving 98 children aged 21-41 months. Children were asked to consume an initially rejected target food on five occasions either with a Gentle or a Harsh instruction. Children's dislike for the target food was assessed via intake before and after the familiarization phase. Inhibitory control level was measured in 78 of these children using validated questionnaire. Four groups were created: Instructions (Gentle vs Harsh)×Inhibitory control (Lower vs Higher). After the familiarization phase, the consumption of the target food increased in all groups, but with a higher increase in children with high Inhibitory control with Gentle instruction, than for children with low Inhibitory control with Harsh instruction, the two other groups being in between. Our data fit a model of cumulative effects, and show that both gentle control strategies and high inhibitory control in children contribute to regulate disgusts experienced in some feeding contexts.

  20. Inhibitory effects of Zengshengping fractions on DMBA-induced buccal pouch carcinogenesis in hamsters

    Institute of Scientific and Technical Information of China (English)

    GUAN Xiao-bing; SUN Zheng; CHEN Xiao-xin; WU Hong-ru; ZHANG Xin-yan

    2012-01-01

    Background Zengshengping (ZSP) tablets had inhibitory effects on oral precancerous lesions by reducing the incidence of oral cancer.However,the severe liver toxicity caused by systemic administration of ZSP limits the long-term use of this anti-cancer drug.The purpose of this study was to evaluate the tumor inhibitory effects due to the topical application of extracts from ZSP,a Chinese herbal drug,on 7,12-dimethlbenz(a)anthracene (DMBA) induced oral tumors in hamsters.The study also investigated the anti-cancer mechanisms of the ZSP extracts on oral carcinogenesis.Methods DMBA (0.5%) was applied topically to the buccal pouches of Syrian golden hamsters (6-8 weeks old) three times per week for six weeks in order to induce the development of oral tumors.Different fractions of ZSP were either applied topically to the oral tumor lesions or fed orally at varying dosages to animals with oral tumors for 18 weeks.Tumor volume was measured by histopathological examination.Tumor cell proliferation was evaluated by counting BrdU labeled cells and by Western blotting for mitogen-activated protein kinase (MAPK) protein levels.The protein levels of apoptosis marker Caspase-3 and regulator Bcl-2 protein were also measured by Western blotting.Results Topical application of DMBA to the left pouch of hamsters induced oral tumor formation.Animals treated with DMBA showed a loss in body weight while animals treated with ZSP maintained normal body weights.Both the ZSP n-butanol fraction and water fraction significantly reduced tumor volume by 32.6% (P <0.01) and 22.9% (P <0.01)respectively.Topical application of ZSP also markedly decreased the BrdU-positive cell numbers in oral tumor lesions and reduced the expression level of MAPK.In addition,ZSP promoted tumor cell apoptosis by increasing Caspase-3 expression but decreasing Bcl-2 protein production.Conclusion The n-butanol and water fractions of ZSP are effective at inhibiting tumor cell proliferation and stimulating

  1. Re-188 Enhances the Inhibitory Effect of Bevacizumab in Non-Small-Cell Lung Cancer

    Directory of Open Access Journals (Sweden)

    Jie Xiao

    2016-09-01

    Full Text Available The malignant behaviors of solid tumors such as growth, infiltration and metastasis are mainly nourished by tumor neovascularization. Thus, anti-angiogenic therapy is key to controlling tumor progression. Bevacizumab, a humanized anti-vascular endothelial growth factor (VEGF antibody, plus chemotherapy or biological therapy can prolong survival for cancer patients, but treatment-related mortality is a concern. To improve inhibitory effect and decrease side-effects on non-small-cell lung cancer (NSCLC, we used Re-188, which is a β emitting radionuclide, directly labeled with bevacizumab for radioimmunotherapy in a human A549 tumor model. Cytotoxic assay data showed that, after 188ReO4− or 188Re-bevacizumab at different concentration for 4 and 24 h, a time- and radioactivity does-dependent reduction in cell viability occurred. Also, an apoptosis assay conformed great apoptosis in the 188Re-bevacizumab group compared with controls and other treatment groups. In vivo, tumor volumes in the 188Re-bevacizumab (11.1 MBq/mice group were not reduced but growth was delayed compared with other groups. Thus, 188Re-bevacizumab enhanced the therapeutic effect of bevacizumab, suggesting a potential therapeutic strategy for NSCLC treatment.

  2. Inhibitory effect of chlorophyllin on the Propionibacterium acnes-induced chemokine expression.

    Science.gov (United States)

    Kang, Mi-Sun; Kim, Jin-Hee; Shin, Boo-Ahn; Lee, Hyun-Chul; Kim, Youn-Shin; Lim, Hae-Soon; Oh, Jong-Suk

    2013-12-01

    Chlorophyllin (CHL), a chlorophyll-derivative, exhibits several beneficial properties, including antibacterial, antioxidant, and anticancer activities. However, its antibacterial and anti-inflammatory activities against Propionibacterium acnes have not been described. The antibacterial activity of this compound was evaluated in vitro using the broth microdilution method. CHL had an inhibitory effect on the growth of P. acnes (MIC = 100 μM). In a real-time reverse transcription-polymerase chain reaction and an enzyme-linked immunosorbent assay, CHL significantly decreased interleukin-8 (IL-8) and monocyte chemoattractant protein-1 (MCP-1) production in a dose-dependent manner, decreasing both mRNA and protein levels for these chemokines in THP-1 cells indicating the anti-inflammatory effects of it. To investigate the molecular mechanisms underlying the anti-inflammatory properties of CHL in THP-1 cells stimulated by P. acnes, we used western blotting to analyze the effect of CHL on activation of the nuclear factor (NF)-κB. CHL inhibited P. acnes-induced IL-8 and MCP-1 production via blockade of NF-κB activation in THP-1 cells. Therefore, based on these results, we suggest that CHL is a useful agent to control the growth of P. acnes involved in acne inflammation and prevent acne.

  3. Inhibitory effect of essential oils against Trichosporon ovoides causing Piedra Hair Infection.

    Science.gov (United States)

    Saxena, Seema; Uniyal, Veena; Bhatt, R P

    2012-10-01

    Piedra, is an asymptomatic fungal infection of the hair shaft, resulting in the formation of nodules of different hardness on the infected hair. The infection also known as Trichomycosis nodularis is a superficial fungal infection arising from the pathogen being restricted to the stratum corneum with little or no tissue reaction. The nodules are a concretion of hyphae and fruiting bodies of the fungus. Two varieties of Piedra may be seen, Black Piedra and White Piedra. The fungus Trichosporon ovoides is involved in the occurrence of both types of Piedras. The purpose of this study was to examine the effectiveness of selected essential oils for the control of growth of the fungus and to determine whether the antifungal effect was due to the major compounds of the oils. Two screening methods viz. Agar well diffusion assay and Minimum Inhibitory Concentration were adopted for the study. MIC and MFC were determined by tube dilution method. Essential oils from Eucalyptus, Ocimum basilicum, Mentha piperita, Cymbopogon flexuosus, Cymbopogon winterians, Trachyspermum ammi, Zingiber officinalis, Citrus limon, Cinnamomon zeylanicum, Salvia sclarea, Citrus aurantifolia, Melaleuca alternifolia, Citrus aurantium, Citrus bergamia, Pogostemon pathchouli, Cedrus atlantica, Jasminum officinale, Juniperus communis, Abelmoschus moschatus, Cyperus scariosus, Palargonium graveolens, Boswellia carterii, Rosa damascene, Veteveria zizanoides and Commiphora myrrha were evaluated. The essential oils of Cymbopogon winterians, Mentha piperita, Cinnamomum zeylanicum, Melaleuca alternifolia and Eucalyptus globulus were proved to be most effective against the fungus Trichosporon ovoides.

  4. Inhibitory effects of antihistamines, diphenhydramine and chlorpheniramine, on proton currents in BV2 microglial cells.

    Science.gov (United States)

    Kim, Jiwon; Song, Jin-Ho

    2017-03-05

    Microglial NADPH oxidase is a major source of toxic reactive oxygen species produced during chronic neuroinflammation. Voltage-gated proton channel (HV1) functions to maintain the intense activity of NADPH oxidase, and channel inhibition alleviates the pathology of neurodegenerative diseases such as ischemic stroke and multiple sclerosis associated with oxidative neuroinflammation. Antagonists of histamine H1 receptors have beneficial effects against microglia-mediated oxidative stress and neurotoxicity. We examined the effects of the H1 antihistamines, diphenhydramine and chlorpheniramine, on proton currents in BV2 microglial cells recorded using the whole-cell patch clamp technique. Diphenhydramine and chlorpheniramine reduced the proton currents with almost the same potency, yielding IC50 values of 42 and 43μM, respectively. Histamine did not affect proton currents, excluding the involvement of histamine receptors in their action. Neither drug shifted the voltage-dependence of activation or the reversal potential of the proton currents, even though diphenhydramine slowed the activation and deactivation kinetics. The inhibitory effects of the two antihistamines on proton currents could be utilized to develop therapeutic agents for neurodegenerative diseases and other diseases associated with HV1 proton channel abnormalities. Copyright © 2017 Elsevier B.V. All rights reserved.

  5. The inhibitory effect of vitamin K on RANKL-induced osteoclast differentiation and bone resorption.

    Science.gov (United States)

    Wu, Wei-Jie; Kim, Min Seuk; Ahn, Byung-Yong

    2015-10-01

    To further understand the correlation between vitamin K and bone metabolism, the effects of vitamins K1, menaquinone-4 (MK-4), and menaquinone-7 (MK-7) on RANKL-induced osteoclast differentiation and bone resorption were comparatively investigated. Vitamin K2 groups (MK-4 and MK-7) were found to significantly inhibit RANKL-medicated osteoclast cell formation of bone marrow macrophages (BMMs) in a dose-dependent manner, without any evidence of cytotoxicity. The mRNA expression of specific osteoclast differentiation markers, such as c-Fos, NFATc1, OSCAR, and TRAP, as well as NFATc1 protein expression and TRAP activity in RANKL-treated BMMs were inhibited by vitamin K2, although MK-4 exhibited a significantly greater efficiency compared to MK-7. In contrast, the same dose of vitamin K1 had no inhibitory effect on RANKL-induced osteoclast cell formation, but increased the expression of major osteoclastogenic genes. Interestingly, vitamins K1, MK-4 and MK-7 all strongly inhibited osteoclastic bone resorption (p vitamins K1, MK-4 and MK-7 have anti-osteoporotic properties, while their regulation effects on osteoclastogenesis are somewhat different.

  6. Medium effects on minimum inhibitory concentrations of nylon-3 polymers against E. coli.

    Science.gov (United States)

    Choi, Heejun; Chakraborty, Saswata; Liu, Runhui; Gellman, Samuel H; Weisshaar, James C

    2014-01-01

    Minimum inhibitory concentrations (MICs) against E. coli were measured for three nylon-3 polymers using Luria-Bertani broth (LB), brain-heart infusion broth (BHI), and a chemically defined complete medium (EZRDM). The polymers differ in the ratio of hydrophobic to cationic subunits. The cationic homopolymer is inert against E. coli in BHI and LB, but becomes highly potent in EZRDM. A mixed hydrophobic/cationic polymer with a hydrophobic t-butylbenzoyl group at its N-terminus is effective in BHI, but becomes more effective in EZRDM. Supplementation of EZRDM with the tryptic digest of casein (often found in LB) recapitulates the LB and BHI behavior. Additional evidence suggests that polyanionic peptides present in LB and BHI may form electrostatic complexes with cationic polymers, decreasing activity by diminishing binding to the anionic lipopolysaccharide layer of E. coli. In contrast, two natural antimicrobial peptides show no medium effects. Thus, the use of a chemically defined medium helps to reveal factors that influence antimicrobial potency of cationic polymers and functional differences between these polymers and evolved antimicrobial peptides.

  7. Inhibitory effect of submaximal doses of ghrelin on gonadotropin secretion in women.

    Science.gov (United States)

    Messini, C I; Dafopoulos, K; Malandri, M; Georgoulias, P; Anifandis, G; Messinis, I E

    2014-01-01

    The effect of ghrelin on gonadotropin secretion has been equivocal. Recent data have shown an inhibitory effect of repeated injections of ghrelin on nocturnal LH and FSH secretion in women. The aim of this study was to investigate the effect of submaximal doses of ghrelin on the diurnal secretion of gonadotropins. Ten normally cycling women received 2 consecutive dosages of ghrelin (0.15 μg/kg and 0.30 μg/kg) intravenously in the early and late follicular phases of the cycle. Saline was injected in the preceding cycle. Blood samples in relation to ghrelin or saline administration (time 0 and 90 min) were taken at -15, 0, 30, 90, 120, 150, and 180 min. Serum estradiol concentrations were significantly higher in the late than in the early follicular phase. Following ghrelin administration, serum LH and FSH levels decreased significantly, in relation to the saline injection, in the late (pghrelin on diurnal gonadotropin secretion throughout the follicular phase of the cycle.

  8. Inhibitory effect of essential oils against Trichosporon ovoides causing Piedra Hair Infection

    Directory of Open Access Journals (Sweden)

    Seema Saxena

    2012-12-01

    Full Text Available Piedra, is an asymptomatic fungal infection of the hair shaft, resulting in the formation of nodules of different hardness on the infected hair. The infection also known as Trichomycosis nodularis is a superficial fungal infection arising from the pathogen being restricted to the stratum corneum with little or no tissue reaction. The nodules are a concretion of hyphae and fruiting bodies of the fungus. Two varieties of Piedra may be seen, Black Piedra and White Piedra. The fungus Trichosporon ovoides is involved in the occurrence of both types of Piedras. The purpose of this study was to examine the effectiveness of selected essential oils for the control of growth of the fungus and to determine whether the antifungal effect was due to the major compounds of the oils. Two screening methods viz. Agar well diffusion assay and Minimum Inhibitory Concentration were adopted for the study. MIC and MFC were determined by tube dilution method. Essential oils from Eucalyptus, Ocimum basilicum, Mentha piperita, Cymbopogon flexuosus, Cymbopogon winterians, Trachyspermum ammi, Zingiber officinalis, Citrus limon, Cinnamomon zeylanicum, Salvia sclarea, Citrus aurantifolia, Melaleuca alternifolia, Citrus aurantium, Citrus bergamia, Pogostemon pathchouli, Cedrus atlantica, Jasminum officinale, Juniperus communis, Abelmoschus moschatus, Cyperus scariosus, Palargonium graveolens, Boswellia carterii, Rosa damascene, Veteveria zizanoides and Commiphora myrrha were evaluated. The essential oils of Cymbopogon winterians, Mentha piperita, Cinnamomum zeylanicum, Melaleuca alternifolia and Eucalyptus globulus were proved to be most effective against the fungus Trichosporon ovoides.

  9. Inhibitory Effect of Sophorolipid on Candida albicans Biofilm Formation and Hyphal Growth.

    Science.gov (United States)

    Haque, Farazul; Alfatah, Md; Ganesan, K; Bhattacharyya, Mani Shankar

    2016-03-31

    Candida albicans causes superficial and life-threatening systemic infections. These are difficult to treat often due to drug resistance, particularly because C. albicans biofilms are inherently resistant to most antifungals. Sophorolipid (SL), a glycolipid biosurfactant, has been shown to have antimicrobial and anticancer properties. In this study, we investigated the effect of SL on C. albicans biofilm formation and preformed biofilms. SL was found to inhibit C. albicans biofilm formation as well as reduce the viability of preformed biofilms. Moreover, SL, when used along with amphotericin B (AmB) or fluconazole (FLZ), was found to act synergistically against biofilm formation and preformed biofilms. Effect of SL on C. albicans biofilm formation was further visualized by scanning electron microscopy (SEM) and confocal laser scanning microscopy (CLSM), which revealed absence of hyphae, typical biofilm architecture and alteration in the morphology of biofilm cells. We also found that SL downregulates the expression of hypha specific genes HWP1, ALS1, ALS3, ECE1 and SAP4, which possibly explains the inhibitory effect of SL on hyphae and biofilm formation.

  10. Inhibitory Effects of Kojic Acid on Phenoloxidase of Diamondback Moth Plutella xylostella

    Institute of Scientific and Technical Information of China (English)

    WANG Shu-dong; LUO Wan-chun; GAO Xing-xiang; DING Qi

    2004-01-01

    The effects of kojic acid on phenoloxidase (PO) of Plutella xylostella were investigated, when it had been partially purified by 40% saturated [(NH4)2SO4] and Sephadex G-100 gel filtration. Kojic acid showed inhibitory effects on both monophenolase and o-diphenolase activity of the PO. The inhibitor concentrations leading to 50% (IC50) activity lost were estimated to be 0.07 mmol L-1 for monophenolase and 1 mmol L-1 for diphenolase, respectively. Kojic acid can also prolong the lag time of PO for oxidation of L-tyrosine. The inhibition kinetics were analyzed by Lineweaver-Burk plots and kojic acid was found to be a reversible competitive inhibitor with the Ki of 0.47 mmol L-1. The ability of kojic acid to inhibit the enzyme activity may be associated with its ability to chelate copper at the active site. In addition, the iron ion was found to shorten the lag time obviously, but have no important effect on the monophenolase activity.

  11. Effect of pretreatment on enzymatic hydrolysis of bovine collagen and formation of ACE-inhibitory peptides

    DEFF Research Database (Denmark)

    Zhang, Yuhao; Olsen, Karsten; Grossi, Alberto Blak

    2013-01-01

    Bovine collagen was pre-treated (boiled or high pressure (HP)-treated) and then hydrolysed by 6 proteases. The degree of hydrolysis (DH) and the angiotensin-converting enzyme (ACE)-inhibitory activity of hydrolysates were measured. All enzymes used were able to partly degrade collagen and release...... ACEinhibitory peptides. The highest ACE-inhibitory activity was obtained with Alcalase. Pretreatment significantly influenced the DH and ACE-inhibition. For most enzymes, boiling for 5 min resulted in a significantly higher DH and ACE-inhibitory activity. With Alcalase and collagenase, hydrolysis and release...

  12. Inhibitory effect of leaf extract of Newbouldia laevis on the metabolic activities of alpha-glucosidase and alpha-amylase

    Directory of Open Access Journals (Sweden)

    Oyetunji T. Kolawole

    2013-12-01

    Full Text Available In this study, the effect of ethanol extract of the leaves of Newbouldia laevis on the activity of α-amylase and α-glucosidase was investigated. Inhibitory effect of N. laevis extract on α-glucosidase was tested in vitro using baker’s yeast α-glucosidase and rat intestinal α-glucosidase while α-amylase inhibitory effect was assayed using rat pancreatic α-amylase. α-Glucosidase inhibitory effect of the extract was also tested in vivo in diabetic and non-diabetic rats. N. laevis extract exhibited good α-glucosidase inhibitory activity in vitro with IC50 values of 2.2 µg/mL and 43.5 µg/mL for baker’s yeast and rat intestinal α-glucosidase respectively. The extract also inhibited rat pancreatic α-amylase activity with IC50 value of 58.7 µg/mL. In both diabetic and non-diabetic rats, N. laevis extract caused a significant reduction in postprandial blood glucose level after oral sucrose load. The results of this study indicate that N. laevis extract exerts its glucose-lowering effect through inhibition of α-glucosidase and α-amylase.

  13. Five Withanolides from the Leaves of Datura metel L. and Their Inhibitory Effects on Nitric Oxide Production

    Directory of Open Access Journals (Sweden)

    Bing-You Yang

    2014-04-01

    Full Text Available Four new withanolides named dmetelins A–D (compounds 1–4, along with the known compound 7α,27-dihydroxy-1-oxo-witha-2,5,24-trienolide (5 were isolated from the leaves of Datura metel L. (Solanaceae. Their structures were elucidated on the basis of detailed analysis of 1D and 2D NMR and mass spectrometry data. All the compounds were evaluated for their inhibitory effects on lipopolysaccharide (LPS-induced nitric oxide (NO production in RAW264.7 cells. Compounds 1, 4 and 5 showed significant inhibitory activities, and compounds 2 and 3 showed moderate inhibitory activities with IC50 values of 17.8, 11.6, 14.9, 33.3 and 28.6 μM, respectively.

  14. Inhibitory Effects of Hydroethanolic Leaf Extracts of Kalanchoe brasiliensis and Kalanchoe pinnata (Crassulaceae) against Local Effects Induced by Bothrops jararaca Snake Venom

    National Research Council Canada - National Science Library

    Fernandes, Júlia Morais; Félix-Silva, Juliana; da Cunha, Lorena Medeiros; Gomes, Jacyra Antunes dos Santos; Siqueira, Emerson Michell da Silva; Gimenes, Luisa Possamai; Lopes, Norberto Peporine; Soares, Luiz Alberto Lira; Fernandes-Pedrosa, Matheus de Freitas; Zucolotto, Silvana Maria

    2016-01-01

    .... Studies evaluating the anti-venom activity of these species are scarce. This study aims to characterize the chemical constituents and evaluate the inhibitory effects of hydroethanolic leaf extracts of K. brasiliensis and K...

  15. Inhibitory effects of acyclic nucleoside phosphonates on human hepatitis B virus and duck hepatitis B virus infections in tissue culture

    NARCIS (Netherlands)

    R.A. Heijtink; J. Kruining; G.A. de Wilde; J. Balzarini; E. de Clercq; S.W. Schalm (Solko)

    1994-01-01

    textabstractThe inhibitory effects of the 9-(2-phosphonylmethoxyethyl)adenine-related compounds (S)-9-(3-hydroxy-2-phosphonylmethoxypropyl)-adenine, (S)-9-(3-fluoro-2-phosphonylmethoxypropyl)adenine, (R)-9-(2-phosphonylmethoxypropyl)adenine, (R)-9-(2-phosphony

  16. The molecular mechanisms of Curcuma Wenyujin extract-mediated inhibitory effects on human esophageal carcinoma cells in Vitro

    Institute of Scientific and Technical Information of China (English)

    景钊

    2012-01-01

    Objective To study the molecular mechanisms of Curcuma Wenyujin extract-mediated inhibitory effects on human esophageal carcinoma cells. Methods The Curcuma Wenyujin extract was obtained by supercritical carbon dioxide extraction. TE-1 cells were divided into 4 groups after adherence.

  17. The plaque inhibitory effect of a CPC mouthrinse in a 3-day plaque accumulation model - a cross-over study

    NARCIS (Netherlands)

    Versteeg, P.A.; Rosema, N.A.M.; Hoenderdos, N.L.; Slot, D.E.; van der Weijden, G.A.

    2010-01-01

    Objective:  To test the plaque inhibitory effect of an experimental 0.07% cetylpyridinium chloride (CPC) mouthrinse in a 3-day plaque accumulation model in a cross-over design. Material and Methods:  A total of 30 subjects (non-dental students), ≥18 years of age, were randomly assigned to use one of

  18. Phenylethanoids in the herb of Plantago lanceolata and inhibitory effect on arachidonic acid-induced mouse ear edema.

    Science.gov (United States)

    Murai, M; Tamayama, Y; Nishibe, S

    1995-10-01

    The five phenylethanoids, acteoside (1), cistanoside F (2), lavandulifolioside (3), plantamajoside (4) and isoacteoside (5) were isolated from the herb of Plantago lanceolata L. (Plantaginaceae). Compounds 1, the major phenylethanoid in the herb of P. lanceolata L., and 4, the major phenylethanoid in the herb of P. asiatica L., showed inhibitory effects on arachidonic acid-induced mouse ear edema.

  19. The effects of environmental enrichment and age-related differences on inhibitory avoidance in zebrafish (Danio rerio Hamilton)

    NARCIS (Netherlands)

    Manuel, R.; Gorissen, M.; Stokkermans, M.; Zethof, J.; Ebbesson, L.O.E.; Vis, van de J.W.; Flik, G.; Bos, van den R.

    2015-01-01

    The inhibitory avoidance paradigm allows the study of mechanisms underlying learning and memory formation in zebrafish (Danio rerio Hamilton). For zebrafish, the physiology and behavior associated with this paradigm are as yet poorly understood. We therefore assessed the effects of environmental enr

  20. In vitro evaluation of capsaicin inhibitory effects on zonula occludens toxin in vibrio cholerae ATCC14035 strain

    Directory of Open Access Journals (Sweden)

    Soroor Erfanimanesh

    2014-10-01

    Conclusion: Capsaicin is one of the active compounds of red chili that can drastically suppress zot gene expression and shows promising inhibitory effect against V. cholerae zot production. Thus, routine intake of red chilli, which is easily available and inexpensive, may be an alternative approach to prevent and control symptoms of cholera.

  1. Central inhibitory effect of α-methyldopa on blood pressure, heart rate and body temperature of renal hypertensive rats

    NARCIS (Netherlands)

    Nijkamp, F.P.; Ezer, Joseph; Jong, Wybren de

    The central inhibitory effect of α-methyldopa on blood pressure, heart rate and body temperature was studied in conscious renal hypertensive rats. Systemic administration of α-methyldopa decreased mean arterial blood pressure and body temperature and caused a short lasting increase in heart rate

  2. Mechanical wounding under field conditions: A potential tool to increase the allelopathic inhibitory effect of cover crops on weeds?

    NARCIS (Netherlands)

    Kruidhof, H.M.; Dam, van N.M.; Ritz, C.; Lotz, L.A.P.; Kropff, M.J.; Bastiaans, L.

    2014-01-01

    To increase the inhibitory effect of soil-incorporated cover crop residues on germination and early growth of weeds, the allelochemical content of the cover crop at the time of soil incorporation should be maximal. We investigated whether mechanical damaging in spring induced the production of allel

  3. Central inhibitory effect of α-methyldopa on blood pressure, heart rate and body temperature of renal hypertensive rats

    NARCIS (Netherlands)

    Nijkamp, F.P.; Ezer, Joseph; Jong, Wybren de

    1975-01-01

    The central inhibitory effect of α-methyldopa on blood pressure, heart rate and body temperature was studied in conscious renal hypertensive rats. Systemic administration of α-methyldopa decreased mean arterial blood pressure and body temperature and caused a short lasting increase in heart rate fol

  4. Inhibitory effects of acyclic nucleoside phosphonates on human hepatitis B virus and duck hepatitis B virus infections in tissue culture

    NARCIS (Netherlands)

    R.A. Heijtink; J. Kruining; G.A. de Wilde; J. Balzarini; E. de Clercq; S.W. Schalm (Solko)

    1994-01-01

    textabstractThe inhibitory effects of the 9-(2-phosphonylmethoxyethyl)adenine-related compounds (S)-9-(3-hydroxy-2-phosphonylmethoxypropyl)-adenine, (S)-9-(3-fluoro-2-phosphonylmethoxypropyl)adenine, (R)-9-(2-phosphonylmethoxypropyl)adenine, (R)-9-(2-phosphony

  5. The inhibitory effect of a chewing task on a human jaw reflex

    NARCIS (Netherlands)

    Maillou, P.; Cadden, S.W.; Lobbezoo, F.

    2010-01-01

    This study was undertaken to investigate whether an inhibitory jaw reflex could be modulated by experimentally controlled conditions that mimicked symptoms of temporomandibular disorders. Reflecting on previous work, we anticipated that these conditions might suppress the reflex. Electromyographic r

  6. The Inhibitory Effect of Astilbin on the Arteriosclerosis of Murine Thoracic Aorta Transplant

    Institute of Scientific and Technical Information of China (English)

    Jinping ZHAO; Ping LI; Yunfeng ZHANG; Xianguo WANG; Qilin AO; Sihai GAO

    2009-01-01

    The inhibitory effect of astilbin on transplant arteriosclerosis in murine model of thoracic aorta transplantation was examined.Model of rat thoracic aorta transplantation was established.Ninety rats were divided into three groups.In isograft group,the thoracic aorta of Brown Norway (BN) rat was anastomosed with the abdominal aorta of another BN rat.In allograft group,the thoracic aorta of BN rat was anastomosed with the abdominal aorta of Lewis rat.In astilbin group,the rats receiving allo-transplantation were given astiibin 5 mg/kg per day for a time of 28 days.The donor thoracic aorta and the recipient abdominal aorta were anastomosed by means of a polyethylene cannula (inner diameter:1.5 mm,length:3 mm length).The grafts were histologically examined for structural changes.The areas of arterial lumen and endatrium were calculated.Our results showed that,in the allograft group,28 days after aliografting,conspicuous proliferation of smooth muscles and infiltration with a great number of inflammatory cells were found in the tunica intima and tunica media.Astilbin significantly inhibited the proliferation of smooth muscles and ameliorated the infiltration of inflammatory cells thereyby prevent against the development of transplant arteriosclerosis.It is concluded that asltilbin can effectively prevent the development of arteriosclerosis in allotrausplant by inhibiting the proliferation of smooth muscles and inhibit the proliferation of smooth muscles in tunica of intima and media and reducing infiltration of the inflammatory cells.

  7. Inhibitory effects of silver nanoparticles against adenovirus type 3 in vitro.

    Science.gov (United States)

    Chen, Nana; Zheng, Yang; Yin, Jianjian; Li, Xiujing; Zheng, Conglong

    2013-11-01

    Adenoviruses are associated with respiratory, ocular, or gastrointestinal disease. With various species and high morbidity, adenoviruses are increasingly recognized as significant viral pathogen among pediatric and immunocompromised patients. However, there is almost no specific drug for treatment. Silver nanoparticles are demonstrated to be virucidal against influenza A (H1N1) virus, human immunodeficiency virus and Hepatitis B virus. Currently, there is no data regarding whether the silver nanoparticles inhibit the adenovirus or not. The aim of this study is to investigate the effect of silver nanoparticles on adenovirus type 3 (Ad3). The results revealed that HeLa cells infected with silver nanoparticles treated Ad3 did not show obvious CPE. The viability of HeLa cells infected with silver nanoparticles treated Ad3 was significantly higher than that of cells infected with untreated Ad3. There was a significant difference of fluorescence intensity between the cells infected with silver nanoparticles treated and untreated Ad3. The transmission electron microscopy (TEM) showed that silver nanoparticles could directly damage the structure of Ad3 particle. The PCR amplification products of DNA isolated from silver nanoparticles treated Ad3 was decreased in a dose-dependent manner. The decreased DNA loads were also confirmed by real-time PCR experiment. The present study indicates silver nanoparticles exhibit remarkably inhibitory effects on Ad3 in vitro, which suggests silver nanoparticles could be a potential antiviral agent for inhibiting Ad3 infection. Copyright © 2013 Elsevier B.V. All rights reserved.

  8. Inhibitory effects of capsaicin on hepatic stellate cells and liver fibrosis.

    Science.gov (United States)

    Yu, Fu-Xiang; Teng, Yin-Yan; Zhu, Qian-Dong; Zhang, Qi-Yu; Tang, Yin-He

    2014-10-01

    Hepatic stellate cells (HSCs) play an important role in the process of liver fibrosis. In this study, we investigated the inhibitory effects of capsaicin on HSCs and liver fibrosis. Cultured HSCs were incubated with various concentrations of capsaicin. Cell proliferation was examined using a cell counting kit. Production of hydrogen peroxide was determined using a 2',7'-dichlorofluorescin diacetate (DCFH-DA) assay. The mRNA and protein expression of target genes was analyzed by reverse transcription PCR and Western blot analysis, respectively. Cell apoptosis was evaluated by annexin V-FITC and propidium iodide (PI) costaining followed by flow cytometric analysis. A CCl4 rat liver fibrosis model was used to assess in vivo effects of capsaicin by histological examination and measurement of liver fibrosis markers, including hydroxyproline content, serum type III collagen, and hyaluronic acid (HA) levels. Our results show that capsaicin dose-dependently inhibited cell proliferation, suppressed cell activation, and decreased hydrogen peroxide production in cultured HSCs. Capsaicin reduced the mRNA levels of tissue inhibitors of metalloproteinase 1 (TIMP-1) and transforming growth factor-β1 (TGF-β1) in HSCs. Moreover, capsaicin-induced cell apoptosis was associated with increased expression of Bax, cytochrome c (cyt c), and caspase-3, but reduced levels of Bcl-2. The animal studies further revealed that capsaicin efficiently reduced the extent of liver fibrosis, inhibited HSC proliferation, and promoted cell apoptosis. Our findings suggest that capsaicin might inhibit fibrogenesis by inhibiting the activities of HSCs.

  9. Antioxidant and tyrosinase inhibitory effects of neolignan glycosides from Crataegus pinnatifida seeds.

    Science.gov (United States)

    Huang, Xiao-Xiao; Liu, Qing-Bo; Wu, Jie; Yu, Li-Hong; Cong, Qian; Zhang, Yan; Lou, Li-Li; Li, Ling-Zhi; Song, Shao-Jiang

    2014-12-01

    In our efforts to find an inhibitor of melanin formation and develop potential depigmenting agents for skin-protecting cosmetics and medicinal products from natural resources, we focused on the seeds of Crataegus pinnatifida which showed antioxidant and tyrosinase-inhibiting activities. By activity-guided fractionation of an extract of C. pinnatifida seeds, four new neolignan glycosides, pinnatifidaninsides A-D (1-4), along with two known compounds (5-6), were isolated. Their structures were elucidated by spectroscopic analyses, especially 1D, 2D NMR and CD spectra. The antioxidant and tyrosinase-inhibiting activities of all isolates were assayed. Compound 6 showed good activity against 2,2-diphenyl-1-pikrylhydrazyl, while compounds 1, 2, 5, and 6 exhibited strong 2,2'-azino-bis (3-ethylbenzothiazoline-6-sulphonic acid) free radical scavenging activity, being as effective as, or even more effective than the positive control Trolox. Moreover, compounds 5 and 6 displayed a moderate mushroom tyrosinase inhibitory activity. Georg Thieme Verlag KG Stuttgart · New York.

  10. Inhibitory effects of Iranian Thymus vulgaris extracts on in vitro growth of Entamoeba histolytica.

    Science.gov (United States)

    Behnia, Maryam; Haghighi, Ali; Komeylizadeh, Hossein; Tabaei, Seyyed-Javadi Seyyed; Abadi, Alireza

    2008-09-01

    One of the most common drugs used against a wide variety of anaerobic protozoan parasites is metronidazole. However, this drug is mutagenic for bacteria and is a potent carcinogen for rodents. Thymus vulgaris is used for cough suppression and relief of dyspepsia. Also it has antibacterial and antifungal properties. The aim of this study was to investigate antiamebic effect of Thymus vulgaris against Entamoeba histolytica in comparison with metronidazole. One hundred gram air-dried T. vulgaris plant was obtained and macerated at 25 degrees C for 14 days using n-hexane and a mixture of ethanol and water. For essential oil isolation T. vulgaris was subjected to hydrodistillation using a clevenger-type apparatus for 3 hr. E. histolytica, HM-1: IMSS strain was used in all experiments. It was found that the minimal inhibitory concentration (MIC) for T. vulgaris hydroalcoholic, hexanic extracts, and the essential oil after 24 hr was 4 mg/mL, 4 mg/mL, and 0.7 mg/mL, respectively. After 48 hr the MIC for T. vulgaris hydroalcoholic and hexanic extracts was 3 and 3 mg/mL, respectively. Therefore, it can be concluded that the Iranian T. vulgaris is effective against the trophozoites of E. histolytica.

  11. Inhibitory effect of Raphanobrassica on Helicobacter pylori-induced gastritis in Mongolian gerbils.

    Science.gov (United States)

    Yamada, Takanori; Wei, Min; Toyoda, Takeshi; Yamano, Shoutaro; Wanibuchi, Hideki

    2014-08-01

    Helicobacter pylori (H. pylori) infection is well known to be associated with chronic gastritis and also development of gastric cancer. Raphanobrassica (RB) is an intergeneric hybrid of the genera Raphanus (radish) and Brassica (cabbages) containing appreciable amounts of glucoraphanin (GR) and glucoraphenin (GRe), which are actively hydrolyzed by the enzyme myrosinase to sulforaphane and sulforaphene, respectively. Both of these metabolites exert antimicrobial and anti-inflammatory activity. The purpose of the present study was to investigate the effect of two freeze-dried products of RB (RB1 and RB2) on H. pylori-induced gastritis in Mongolian gerbils. Six-week-old male Mongolian gerbils were inoculated orally with H. pylori (ATCC 43504), and 2weeks later were fed diets containing no additives or diets supplemented with 2% RB1 (containing both GR and GRe) or 2% RB2 (containing GR only) for 10weeks. In the RB1, but not the RB2 group, mononuclear cell infiltration, mRNA expression of IL-6, and cell proliferation in the gastric mucosa were significantly suppressed. These results indicate that RB1 containing both GR and GRe exerted significant inhibitory effects on H. pylori-induced gastritis in Mongolian gerbils apparently mediated via suppression of IL-6 expression and chronic inflammation.

  12. [Study on inhibitory effect of EGCG on Calcium oxalate nephrolithiasis in rats and its related mechanism].

    Science.gov (United States)

    Zhou, Yong; Wang, Shuo; Tang, Chun-bo

    2015-04-01

    In the study, the inhibitory effect of epigallocatechin gallate (EGCG) on Calcium oxalate nephrolithiasis and its possible mechanism were investigated. The rat Calcium oxalate nephrolithiasis model was induced through the combined oral administration of ethylene glycol and ammonium chloride, which was intervened with EGCG. Rat blood samples were collected to detect blood creatinine (Cr), blood urea nitrogen (BUN) and blood calcium. Rat urine samples were collected to observe and compare 24-hour urine volume, oxalic acid (Ox) and calcium in urine. Renal samples were collected to prepare tissue slices and observe the pathological changes in Calcium oxalate nephrolithiasis. The expression of osteopontin (OPN) in renal tissues was evaluated by Real-time PCR and Western blot. According to the results, compared with normal rats, rats in the nephrolithiasis model showed significant increases in Cr, BUN, urine Calcium, urine Ox and renal OPN expression (P nephrolithiasis, those processed with EGCG revealed remarkable declines in Cr, BUN, urine Calcium and urine Ox (P nephrolithiasis rats showed significant pathological changes in Calcium oxalate calculus. After ECCG treatment, the renal pathological changes and OPN expression attenuated significantly in a concentration-dependent manner. The results showed that EGCG inhibits the formation of calcium oxalate nephrolithiasis in rats and shows a notable protective effect on renal functions.

  13. Stimulus-response incompatibility eliminates inhibitory cueing effects with saccadic but not manual responses.

    Science.gov (United States)

    Eng, Vivian; Lim, Alfred; Kwon, Simon; Gan, Su Ren; Jamaluddin, S Azrin; Janssen, Steve M J; Satel, Jason

    2017-05-01

    There are thought to be two forms of inhibition of return (IOR) depending on whether the oculomotor system is activated or suppressed. When saccades are allowed, output-based IOR is generated, whereas input-based IOR arises when saccades are prohibited. In a series of 4 experiments, we mixed or blocked compatible and incompatible trials with saccadic or manual responses to investigate whether cueing effects would follow the same pattern as those observed with more traditional peripheral onsets and central arrows. In all experiments, an uninformative cue was displayed, followed by a cue-back stimulus that was either red or green, indicating whether a compatible or incompatible response was required. The results showed that IOR was indeed observed for compatible responses in all tasks, whereas IOR was eliminated for incompatible trials-but only with saccadic responses. These findings indicate that the dissociation between input- and output-based forms of IOR depends on more than just oculomotor activation, providing further support for the existence of an inhibitory cueing effect that is distinct to the manual response modality.

  14. Effect of polymorphism in the leukemia inhibitory factor gene on litter size in Large White pigs.

    Science.gov (United States)

    Lin, H C; Liu, G F; Wang, A G; Kong, L J; Wang, X F; Fu, J L

    2009-09-01

    DNA polymorphism of the porcine leukemia inhibitory factory (LIF) was investigated and used to study the effects on litter size in Large White pigs. A total of 2,167 litter records from 420 sows genotyped at two SNP loci (LIF1 and LIF2) within LIF gene were analyzed to determine whether LIF influenced total number born (TNB) and number born alive (NBA). The results indicated that B allele at LIF1 locus and A allele at LIF2 locus seem to have advantageous effects on litter size. However, the combined analyzed results demonstrated that genotype AAAA, ABBB, and BBBB are better than genotype AAAB, AABB, and ABAB for TNB and NBA in either third to eighth parity or all parities. In all parities, the sows with AAAA genotype had an advantage of 1.76 piglets (P NBA per litter over the AAAB sows, respectively. The results in this study demonstrated that LIF gene was significantly associated with litter size in pigs.

  15. Inhibitory Effect of Heracleum persicum and Ziziphus jujuba on Activity of Alpha-Amylase

    Directory of Open Access Journals (Sweden)

    Reza Afrisham

    2015-01-01

    Full Text Available Postprandial hyperglycemia plays an important role in the development of type 2 diabetes. Inhibition of alpha-amylase was led to a delay in breaks down of starch and glycogen and prevented a rapid rise in blood sugar. Alpha-amylase was isolated by gel filtration chromatography Sephadex G-75 from bovine pancreas. Then, total methanolic extracts of plants were prepared and IC50 values of extracts on alpha-amylase were obtained and compared with acarbose IC50. The polyphenolic content of extracts and antioxidant capacity were determined by Folin-Ciocalteu test and DPPH test, respectively. The specific activity of alpha-amylase was 48.2 U/mg. For inhibition of alpha-amylase, IC50 values of H. persicum, Z. jujuba, and acarbose were 307, 827, and 113 μg/ml, respectively. For inhibition of DPPH radical, IC50 values of extracts were 235 and 701 μg/ml. Total phenolic contents of methanol extracts were 73.8±3.2 and 44.2±1.8 μg tannic acid equivalent/mg extract. Acarbose causes gastrointestinal symptoms and liver toxicity, but H. persicum and Z. jujuba decrease these side effects and prevent gastrointestinal disorders. Due to the high polyphenolic content and antioxidant capacity of these plants and significant inhibitory effect of the plants on alpha-amylase, these plants can be proposed for treatment of diabetic patients.

  16. An Inhibitory Effect of MAD1 on Bladder Tumor Cellular Proliferation in Vivo

    Institute of Scientific and Technical Information of China (English)

    Hongbo Hu; Chunli Luo; Xiaozhong Cai; Lin Zou; Pei Zhao; Xiouhou Wu

    2006-01-01

    OBJECTIVE To observe the inhibitory effect on bladder tumor proliveration after transfection with the expression plasmid pcDNA3.1 (+)/Mad1.METHODS Bladder tumors were induced in SD rats by intravesical instillation of MNU . The tumor-bearing rats were randomly divided into 3groups: group A, transfected with pcDNA3.1 (+)/Mad1, group B, transfected with an empty vector and group C, transfected with saline. Rat body weight (RBW), bladder absolute weight (BAW) and bladder relative weight (BRW) were measured and expression levels of Mad1 and TERT were assayed. Flow cytometer analysis was used to observe the effect of Mad1 on the bladder tumors.RESULTS Comparions of RBW among the 3 groups showed there were no differences (P>0.05). But the BAW and BRW for group A were significantly decreased (P<0.01, P<0.05, respectively) comparded to groups B and C. In group A, the Mad1 mRNA expression level was markedly improved, while the TERT mRNA expression level was decreased. Flow cytometry showed an increase in G0/G1-phase cells and a decrease of Sphase cells after transfection with Mad1.CONCLUSION Over expression of Mad1 can inhibit the cellular proliferation of bladder tumors.

  17. Increased sink strength offsets the inhibitory effect of sucrose on sugarcane photosynthesis.

    Science.gov (United States)

    Ribeiro, Rafael V; Machado, Eduardo C; Magalhães Filho, José R; Lobo, Ana Karla M; Martins, Márcio O; Silveira, Joaquim A G; Yin, Xinyou; Struik, Paul C

    2017-01-01

    Spraying sucrose inhibits photosynthesis by impairing Rubisco activity and stomatal conductance (gs), whereas increasing sink demand by partially darkening the plant stimulates sugarcane photosynthesis. We hypothesized that the stimulatory effect of darkness can offset the inhibitory effect of exogenous sucrose on photosynthesis. Source-sink relationship was perturbed in two sugarcane cultivars by imposing partial darkness, spraying a sucrose solution (50mM) and their combination. Five days after the onset of the treatments, the maximum Rubisco carboxylation rate (Vcmax) and the initial slope of A-Ci curve (k) were estimated by measuring leaf gas exchange and chlorophyll fluorescence. Photosynthesis was inhibited by sucrose spraying in both genotypes, through decreases in Vcmax, k, gs and ATP production driven by electron transport (Jatp). Photosynthesis of plants subjected to the combination of partial darkness and sucrose spraying was similar to photosynthesis of reference plants for both genotypes. Significant increases in Vcmax, gs and Jatp and marginal increases in k were noticed when combining partial darkness and sucrose spraying compared with sucrose spraying alone. Our data also revealed that increases in sink strength due to partial darkness offset the inhibition of sugarcane photosynthesis caused by sucrose spraying, enhancing the knowledge on endogenous regulation of sugarcane photosynthesis through the source-sink relationship. Copyright © 2016 Elsevier GmbH. All rights reserved.

  18. Binding and Inhibitory Effect of the Dyes Amaranth and Tartrazine on Amyloid Fibrillation in Lysozyme.

    Science.gov (United States)

    Basu, Anirban; Suresh Kumar, Gopinatha

    2017-02-16

    Interaction of two food colorant dyes, amaranth and tartrazine, with lysozyme was studied employing multiple biophysical techniques. The dyes exhibited hypochromic changes in the presence of lysozyme. The intrinsic fluorescence of lysozyme was quenched by both dyes; amaranth was a more efficient quencher than tartrazine. The equilibrium constant of amaranth was higher than that of tartarzine. From FRET analysis, the binding distances for amaranth and tartrazine were calculated to be 4.51 and 3.93 nm, respectively. The binding was found to be dominated by non-polyelectrolytic forces. Both dyes induced alterations in the microenvironment surrounding the tryptophan and tyrosine residues of the protein, with the alterations being comparatively higher for the tryptophans than the tyrosines. The interaction caused significant loss in the helicity of lysozyme, the change being higher with amaranth. The binding of both dyes was exothermic. The binding of amaranth was enthalpy driven, while that of tartrazine was predominantly entropy driven. Amaranth delayed lysozyme fibrillation at 25 μM, while tartrazine had no effect even at 100 μM. Nevertheless, both dyes had a significant inhibitory effect on fibrillogenesis. The present study explores the potential antiamyloidogenic property of these azo dyes used as food colorants.

  19. Growth inhibitory effect of grape phenolics against wine spoilage yeasts and acetic acid bacteria.

    Science.gov (United States)

    Pastorkova, E; Zakova, T; Landa, P; Novakova, J; Vadlejch, J; Kokoska, L

    2013-02-15

    This paper investigates the in vitro antimicrobial potential of 15 grape phenolic compounds of various chemical classes (phenolic acids, stilbenes and flavonoids) using the broth microdilution method against yeasts and acetic acid bacteria frequently occurring in deteriorated wine. Pterostilbene (MICs=32-128 μg/mL), resveratrol (MICs=256-512 μg/mL) and luteolin (MICs=256-512 μg/mL) are among six active compounds that possessed the strongest inhibitory effects against all microorganisms tested. In the case of phenolic acids, myricetin, p-coumaric and ferulic acids exhibited selective antimicrobial activity (MICs=256-512 μg/mL), depending upon yeasts and bacteria tested. In comparison with potassium metabisulphite, all microorganisms tested were more susceptible to the phenolics. The results revealed the antibacterial and antiyeast effects against wine spoilage microorganisms of several highly potent phenolics naturally occurring in grapes. These findings also provide arguments for further investigation of stilbenes as prospective compounds reducing the need for the use of sulphites in winemaking.

  20. Effect of leukemia inhibitory factor on embryonic stem cell differentiation: implications for supporting neuronal differentiation

    Institute of Scientific and Technical Information of China (English)

    Zhao HE; Jing-jing LI; Chang-hong ZHEN; Lin-ying FENG; Xiao-yan DING

    2006-01-01

    Aim: Leukemia inhibitory factor (LIF), a pleiotropic cytokine, has been used extensively in the maintenance of mouse embryonic stem cell pluripotency. In this current work, we examined the effect of the LIF signaling pathway in embryonic stem (ES) cell differentiation to a neural fate. Methods: In the presence of LIF (1000 U/mL), the production of neuronal cells derived from embryoid bodies (EB)was tested under various culture conditions. Inhibition of the LIF pathway was examined with specific inhibitors. The effects of cell apoptosis and proliferation on neural differentiation were examined. ES cell differentiation into three-gem layers was compared. Results: Under various culture conditions, neuronal differentiation was increased in the presence of LIF. Blocking the LIF-activated STAT3signaling pathway with specific inhibitors abolished the neuronal differentiation of ES cells, whereas inhibition of the LIF-activated MEK signaling pathway impaired the differentiation of ES cells toward a glial fate. LIF suppressed cell apoptosis and promoted cell proliferation during ES cell differentiation. LIF inhibited the differentiation of ES cells to both mesoderm and extraembryonic endoderm fates, but enhanced the determination of neural progenitors. Conclusion:These results suggest that LIF plays a positive role during the differentiation of ES cells into neuronal cells.

  1. Inhibitory effect of naringin on microcystin-LR uptake in the freshwater snail Sinotaia histrica.

    Science.gov (United States)

    Xie, Liqiang; Hanyu, Tamami; Futatsugi, Noriko; Komatsu, Masaharu; Steinman, Alan D; Park, Ho-Dong

    2014-09-01

    Gastropods are an important food source for aquatic animals, and have been demonstrated to transfer microcystin (MC) to higher trophic levels through the food web. In this study, we performed an oral administration experiment to evaluate whether naringin can inhibit MC-LR uptake in the freshwater snail Sinotaia histrica. We also observed the effect of MC-LR on the organizational pathology of the hepatopancreas in S. histrica. Following exposure to cells of Microcystis ichthyoblabe, S. histrica showed vacuolization and separation of the basal lamina from cells in the hepatopancreas. Initial treatment with 1mM naringin resulted in the prevention of MC-LR uptake rate by approximately 60% over 8days, whereas initial treatment with 10mM naringin suppressed microcystin uptake in 2days, despite an increase in MC-LR levels in the snail from days 5 to 8. With continuous treatment of 10mM naringin, the uptake prevention rate was 100%. Overall, we observed a strong inhibitory effect against MC-LR with naringin treatment. This study provides a potential mechanism to prevent the uptake of microcystin in the aquatic food web, thereby limiting its toxicity in cyanobacterial bloom-polluted areas where the environment can be controlled and may have further applications in the aquaculture of gastropods.

  2. Cytokines can counteract the inhibitory effect of MEK-i on NK-cell function

    Science.gov (United States)

    Manzini, Claudia; Venè, Roberta; Cossu, Irene; Gualco, Marina; Zupo, Simonetta; Dono, Mariella; Spagnolo, Francesco; Queirolo, Paola; Moretta, Lorenzo; Mingari, Maria Cristina; Pietra, Gabriella

    2016-01-01

    Oncogene-targeted therapies based on mutated BRAF- and/or MEK-specific inhibitors have been developed for melanoma treatment. Although these drugs induce tumor regression in a high percentage of patients, clinical responses are frequently limited in time and tumors often recur. Recent studies suggested that the combination of BRAF/MEK inhibition with immunotherapy could represent a promising strategy for the cure of melanoma. NK cells are suitable effectors for tumor immunotherapy. Here we show that PLX4032 (a mutant BRAFV600 inhibitor) had no effect on the functional properties of NK cells cultured in the presence of IL-2 or IL-15. In contrast, PD0325901 (a MEK inhibitor) induced the down-regulation of the main activating NK receptors and inhibited NK cell function. Importantly, PD0325901 did not affect the anti-tumor activity of NK cells that had been exposed to a combination of IL-15 and IL-18. In addition, both PLX4032 and PD0325901 did not exert any inhibitory effect on in vitro IL-2 or IL-15 pre-activated NK cells. Our data may provide a rationale for future clinical protocols that combine IL-15/IL-18 cytokine administration with MEK inhibitors. In addition, they suggest that oncogene-targeting drugs are compatible with NK-based adoptive therapy. PMID:27563819

  3. Cafestol has a weaker inhibitory effect on osteoclastogenesis than kahweol and promotes osteoblast differentiation.

    Science.gov (United States)

    Fukuma, Yutaka; Sakai, Eiko; Nishishita, Kazuhisa; Okamoto, Kuniaki; Tsukuba, Takayuki

    2015-01-01

    Bone homeostasis is regulated by a balance between osteoclast (OCL)-mediated bone resorption and osteoblast (OBL)-mediated bone formation. Thus, developing a compound that simultaneously inhibits OCL function and promotes OBL function would be useful as a new medical therapy for bone diseases. Here, we examined the effects of cafestol, a coffee diterpene, on the differentiation of OCLs and OBLs. Cafestol prevented OCL formation in a dose-dependent manner and suppressed the bone-resorbing activity of OCLs. Interestingly, the viability of OCLs treated with 10-50 µM cafestol was significantly higher than that of untreated cells. At the molecular level, cafestol markedly decreased RANKL-induced phosphorylation of extracellular signal-regulated kinase (Erk) and inhibitor of nuclear factor kappa B alpha (IκBα). Compared to kahweol, another coffee-specific diterpene, the inhibitory effects of cafestol were milder on OCL differentiation, and cafestol and kahweol showed different characteristics in induction of the phase ΙΙ antioxidant enzymes and sensitivities in nuclear factor-erythroid 2-related factor 2 (Nrf2)-deficient BMMs. In addition to inhibiting OCLs, cafestol enhanced the differentiation of osteoblastic cells by increasing the mRNA levels of differentiation markers. Thus, cafestol inhibits OCL differentiation and promotes OBL differentiation, suggesting that cafestol may be a novel agent for bone diseases.

  4. Direct inhibitory effects of pioglitazone on hepatic fetuin-A expression.

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    Akinobu Ochi

    Full Text Available Fetuin-A, a circulating glycoprotein synthesized in the liver, is involved in insulin resistance and type 2 diabetes. However, regulation of fetuin-A synthesis has remained obscure. We previously reported that pioglitazone treatment significantly reduced serum fetuin-A levels in patients with type 2 diabetes. To clarify whether pioglitazone can directory inhibit hepatic fetuin-A synthesis, we investigated the effects of pioglitazone on fetuin-A expression both in vitro and in vivo. Pioglitazone treatment suppressed mRNA and protein expression of fetuin-A in Fao hepatoma cells. Interestingly, rosiglitazone but not metformin, also inhibited fetuin-A expression. In addition, GW 9662, an inhibitor of peroxisome proliferator-activated receptor (PPAR γ, reversed pioglitazone-induced suppression of fetuin-A, suggesting that thiazolidinedione derivatives may have common characteristics with regard to fetuin-A suppression, possibly through PPARγactivation. Finally, oral administration of pioglitazone to mice for 8 weeks resulted in suppression of hepatic fetuin-A mRNA. These findings suggest that pioglitazone may partially ameliorate insulin resistance through its direct inhibitory effects on fetuin-A expression in the liver.

  5. Direct inhibitory effects of pioglitazone on hepatic fetuin-A expression.

    Science.gov (United States)

    Ochi, Akinobu; Mori, Katsuhito; Emoto, Masanori; Nakatani, Shinya; Morioka, Tomoaki; Motoyama, Koka; Fukumoto, Shinya; Imanishi, Yasuo; Koyama, Hidenori; Ishimura, Eiji; Inaba, Masaaki

    2014-01-01

    Fetuin-A, a circulating glycoprotein synthesized in the liver, is involved in insulin resistance and type 2 diabetes. However, regulation of fetuin-A synthesis has remained obscure. We previously reported that pioglitazone treatment significantly reduced serum fetuin-A levels in patients with type 2 diabetes. To clarify whether pioglitazone can directory inhibit hepatic fetuin-A synthesis, we investigated the effects of pioglitazone on fetuin-A expression both in vitro and in vivo. Pioglitazone treatment suppressed mRNA and protein expression of fetuin-A in Fao hepatoma cells. Interestingly, rosiglitazone but not metformin, also inhibited fetuin-A expression. In addition, GW 9662, an inhibitor of peroxisome proliferator-activated receptor (PPAR) γ, reversed pioglitazone-induced suppression of fetuin-A, suggesting that thiazolidinedione derivatives may have common characteristics with regard to fetuin-A suppression, possibly through PPARγactivation. Finally, oral administration of pioglitazone to mice for 8 weeks resulted in suppression of hepatic fetuin-A mRNA. These findings suggest that pioglitazone may partially ameliorate insulin resistance through its direct inhibitory effects on fetuin-A expression in the liver.

  6. Composition Analysis and Inhibitory Effect of Sterculia lychnophora against Biofilm Formation by Streptococcus mutans

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    Yang Yang

    2016-01-01

    Full Text Available Pangdahai is a traditional Chinese drug, specifically described in the Chinese Pharmacopoeia as the seeds of Sterculia lychnophora Hance. Here, we separated S. lychnophora husk and kernel, analyzed the nutrient contents, and investigated the inhibitory effects of S. lychnophora ethanol extracts on cariogenic properties of Streptococcus mutans, important bacteria in dental caries and plaque formation. Ethanol extracts of S. lychnophora showed dose-dependent antibacterial activity against S. mutans with significant inhibition at concentrations higher than 0.01 mg/mL compared with the control group (p 0.03 mg/mL, while bacterial viability was decreased dose-dependently at high concentrations (0.04, 0.08, 0.16, and 0.32 mg/mL. Preliminary phytochemical analysis of the ethanol extract revealed a strong presence of alkaloid, phenolics, glycosides, and peptides while the presence of steroids, terpenoids, flavonoids, and organic acids was low. The S. lychnophora husk had higher moisture and ash content than the kernel, while the protein and fat content of the husk were lower (p<0.05 than those of the kernel. These results indicate that S. lychnophora may have antibacterial effects against S. mutans, which are likely related to the alkaloid, phenolics, glycosides, and peptides, the major components of S. lychnophora.

  7. Inhibitory effect of esterified lactoferin and lactoferrin against tobacco mosaic virus (TMV) in tobacco seedlings.

    Science.gov (United States)

    Wang, Jie; Wang, Hong-Yan; Xia, Xiao-Ming; Li, Peng-peng; Wang, Kai-Yun

    2013-01-01

    The inhibitory effects of esterified lactoferrin (ELF) and lactoferrin (LF) against tobacco mosaic virus (TMV) in tobacco seedlings and the underlying mechanism were investigated. ELF and LF significantly inhibited viral infection and TMV multiplication in tobacco plants. ELF showed a higher inhibition effect against TMV than LF treatment in a dose and time-dependent way. Moreover, ELF induced a higher increase in the levels of transcription of pathogenesis-related (PR) protein genes [acidic PRs (PR-1a, PR-2, PR-3, PR-5) and basic PR-1] and defense-related enzymes [phenylalanine ammonia lyase (PAL, EC 4.3.1.5), and 5-epi-aristolochene synthase (EAS, EC 2.5.1.35)] both locally and systemically, in correlation with the induction of resistance against tobacco mosaic virus. Furthermore, ELF also induced accumulation of salicylic acid, SA 2-O-β-D-glucoside and H2O2. These results suggested that ELF and LF could control TMV incidence and the mechanism might attribute to activate the expression of a number of defense genes. Copyright © 2012 Elsevier Inc. All rights reserved.

  8. Inhibitory Effects of Constituents from the Aerial Parts of Rosmarinus officinalis L. on Triglyceride Accumulation.

    Science.gov (United States)

    Li, Jian; Adelakun, Tiwalade Adegoke; Wang, Sijian; Ruan, Jingya; Yang, Shengcai; Li, Xiaoxia; Zhang, Yi; Wang, Tao

    2017-01-17

    Sixteen flavonoids (1-16) including two new ones, named officinoflavonosides A (1) and B (2) were obtained from the aerial parts of Rosmarinus officinalis. Among the known ones, 6, 10, and 13 were isolated from the rosmarinus genus for the first time. Their structures were elucidated by chemical and spectroscopic methods. Moreover, the effects on sodium oleate-induced triglyceride accumulation (TG) in HepG2 cells of the above-mentioned compounds and 16 other isolates (17-32) reported previously to have been obtained in the plant were analyzed. Results show that eight kinds of flavonoids (compounds 1, 2, 3, 6-9 and 11) and seven kinds of other known isolates (compounds 17-20, 23, 26 and 31) possessed significant inhibitory effects on intracellular TG content in HepG2 cells. Among them, the activities of compounds 1 and 20 were comparable to that of orlistat, which suggested that these compounds in this plant might be involved in lipid metabolism.

  9. Differential effects of lead and zinc on inhibitory avoidance learning in mice

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    F.S. de Oliveira

    2001-01-01

    Full Text Available We studied the effects of chronic intoxication with the heavy metals lead (Pb2+ and zinc (Zn2+ on memory formation in mice. Animals were intoxicated through drinking water during the pre- and postnatal periods and then tested in the step-through inhibitory avoidance memory task. Chronic postnatal intoxication with Pb2+ did not change the step-through latency values recorded during the 4 weeks of the test (ANOVA, P>0.05. In contrast, mice intoxicated during the prenatal period showed significantly reduced latency values when compared to the control group (day 1: q = 4.62, P<0.05; day 7: q = 4.42, P<0.05; day 14: q = 5.65, P<0.05; day 21: q = 3.96, P<0.05, and day 28: q = 6.09, P<0.05. Although chronic postnatal intoxication with Zn2+ did not alter a memory retention test performed 24 h after training, we noticed a gradual decrease in latency at subsequent 4-week intervals (F = 3.07, P<0.05, an effect that was not observed in the control or in the Pb2+-treated groups. These results suggest an impairment of memory formation by Pb2+ when the animals are exposed during the critical period of neurogenesis, while Zn2+ appears to facilitate learning extinction.

  10. Inhibitory effect of yuzu essential oil on the formation of N-nitrosodimethylamine in vegetables.

    Science.gov (United States)

    Sawamura, Masayoshi; Wu, Yingxia; Fujiwara, Chikako; Urushibata, Masato

    2005-05-18

    The inhibitory effect of yuzu (Citrus junos Tanaka) essential oil on the formation of N-nitrosodimethylamine (NDMA) in the presence of vegetables (31 species) or saliva was investigated by HPLC. Most vegetable extracts enhanced the formation of NDMA. However, the formation ratio of NDMA in vegetable extracts was decreased by yuzu oil in the range of 59 to 22%. In the presence of yuzu oil and saliva, its ratio ranged between 62 and 24%. These results indicated that yuzu oil inhibited the formation of NDMA even in vegetables and saliva. The contents of ascorbic acid, nitrate, and nitrite in the 31 vegetable species were 0.3-65 mg/100 g, 3-581 mg/100 g, and 10-750 microg/100 g, respectively. Ascorbic acid and nitrite had little effect on the inhibition or formation of NDMA at their intact levels. Nitrate accelerated the formation of NDMA, and the addition of saliva further enhanced it. The mechanism of inhibition of NDMA formation by alpha-terpinene was studied. It was assumed from the results of LC-MS that a new compound formed by the reaction of alpha-terpinene with nitrite would be a derivative of alpha-terpinene with dinitroso groups. The molecular weight of this compound was 194. It is suggested that terpene hydrocarbons in citrus essential oils would contribute to the decrease of NDMA formation.

  11. The inhibitory effect of shakuyakukanzoto on K+ current in H9c2 cells.

    Science.gov (United States)

    Suganami, Azusa; Sakamoto, Kazuho; Ono, Tomoyuki; Watanabe, Hirotake; Hijioka, Nahoko; Murakawa, Masahiro; Kimura, Junko

    2014-01-01

    Shakuyakukanzoto (shao-yao-gan-cao-tang) is a commonly used Chinese traditional herbal medicine for the treatment of acute pain with muscle cramp. However, its mechanism of action is unclear. We previously reported that a low concentration of Kanzo (licorice) and isoliquiritigenin, a component of licorice, inhibited the potassium (K(+)) current in H9c2 cells. Therefore, in the present study, we examined the effects of Shakuyakukanzoto, Shakuyaku or Kanzo on the K(+) current (IKur) in H9c2 cells. Shakuyakukanzoto inhibited IKur in a concentration-dependent manner. The half-maximal concentration of Shakuyakukanzoto was approximately 1.3 mg/mL and the Hill coefficient was 1.2. The order of potency of inhibiting IKur was Kanzo>Shakuyakukanzoto>Shakuyaku. Glycyrrhizin, a major component of licorice, had no inhibitory effect on IKur. A small interfering RNA experiment indicated that IKur was most likely to be Kv2.1 in H9c2 cells. Our results suggest that Shakuyakukanzoto may normalize intracellular and extracellular K(+) balance by inhibiting IKur and reducing K(+) efflux, while the Na(+)-K(+) pump promotes K(+) influx into myofibers. Consequently, excess K(+) may be reduced from external space of myofibers. This may be a part of the Shakuyakukanzoto mechanism for improving muscle pain.

  12. Inhibitory effects of extracellular adenosine triphosphate on growth of esophageal carcinoma cells

    Institute of Scientific and Technical Information of China (English)

    Ming-Xia Wang; Lei-Ming Ren; Bao-En Shan

    2005-01-01

    AIM: To study the growth inhibitory effects of ATP on TE-13 human squamous esophageal carcinoma cells in vitro.METHODS: MTT assay was used to determine the inhibition of proliferation of ATP or adenosine (ADO) on TE-13 cell line. The morphological changes of TE-13 cells induced by ATP or ADO were observed under fluorescence light microscope by acridine orange (AO)/ethidium bromide (EB) double stained cells. The intemudeosomal fragmentation of genomic DNA was detected by agarose gel electrophoresis.The apoptotic rate and cell cycle after treatment with ATP or ADO were determined by flow cytometry.RESULTS: ATP and ADO produced inhibitory effects on TE-13 cells at the concentration between 0.01 and 1.0 mmol/L.The IC50 of TE-13 cells exposed to ATP or ADO for 48 and 72 h was 0.71 or 1.05, and 0.21 or 0.19 mmol/L, respectively.The distribution of cell cycle phase and proliferation index (PI) value of TE-13 cells changed, when being exposed to ATP or ADO at the concentrations of 0.01, 0.1, and 1 mmol/L for 48 h. ATP and ADO inhibited the cell proliferation by changing the distribution of cell cycle phase via either G0/G1 phase (ATP or ADO, 1 mmol/L) or S phase (ATP, 0.1 mmol/L)arrest. Under light microscope, the tumor cells exposed to 0.3 mmol/L ATP or ADO displayed morphological changes of apoptosis. A ladder-like pattern of DNA fragmentation was obtained from TE-13 cells treated with 0.1-1 mmol/L ATP or ADO in agarose gel electrophoresis. ATP and ADO induced apoptosis of TE-13 cells in a dose-dependent manner at the concentration between 0.03 and 1 mmol/L.The maximum apoptotic rate of TE-13 cells exposed to ATP or ADO for 48 h was 16.63% or 16.9%, respectively.CONCLUSION: ATP and ADO inhibit cell proliferation,arrest cell cycle, and induce apoptosis of TE-13 cell line.

  13. Inhibitory noise

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    Alain Destexhe

    2010-03-01

    Full Text Available Cortical neurons in vivo may operate in high-conductance states, in which the major part of the neuron's input conductance is due to synaptic activity, sometimes several-fold larger than the resting conductance. We examine here the contribution of inhibition in such high-conductance states. At the level of the absolute conductance values, several studies have shown that cortical neurons in vivo are characterized by strong inhibitory conductances. However, conductances are balanced and spiking activity is mostly determined by fluctuations, but not much is known about excitatory and inhibitory contributions to these fluctuations. Models and dynamic-clamp experiments show that, during high-conductance states, spikes are mainly determined by fluctuations of inhibition, or by inhibitory noise. This stands in contrast to low-conductance states, in which excitatory conductances determine spiking activity. To determine these contributions from experimental data, maximum likelihood methods can be designed and applied to intracellular recordings in vivo. Such methods indicate that action potentials are indeed mostly correlated with inhibitory fluctuations in awake animals. These results argue for a determinant role for inhibitory fluctuations in evoking spikes, and do not support feed-forward modes of processing, for which opposite patterns are predicted.

  14. The Inhibitory Effect of Quercetin on IL-6 Production by LPS-Stimulated Neutrophils

    Institute of Scientific and Technical Information of China (English)

    Jiajia Liu; Xin Li; Yang Yue; Juan Li; Tao He; Yanzheng He

    2005-01-01

    Quercetin is a herbal flavonoid derived from various foods of plant origin and plays a role in anti-inflammation. Although a number of researches in the field have been done, the mechanism of anti-inflammatory effect of quercetin should be further clarified. In the present study, we investigated the effects of quercetin on IL-6 production by LPS-stimulated neutrophils in human. Neutrophils were were pre-treated with quercetin at the final concentrations of ranging from 0-80 μM for 30 min, or not treated, and then incubated in the presence or absence of lipopolysaccharide (LPS) at a final concentration of 100 ng/ml for indicated time. The secretion level of IL-6 in the culture supernatants was assayed by ELISA, the intracellular level of IL-6 was detected by flow cytometry and the expression of IL-6 mRNA was analyzed by RT-PCR. The experiment results showed that neutrophils cultured with medium or quercetin alone did not express IL-6, but LPS (100 ng/ml) induced IL-6 expression of neutrophils. However, after pre-treatment of neutrophils with quercetin (40 μM) for 30 min, the inducible effects of LPS on the increase of IL-6 secretion, intracellular IL-6 level and IL-6 mRNA expression by neutrophils were abrogated. IL-6 is one of the important pro-inflammatory factors, especially in early phage of inflammation. Thus, our data suggested that quercetin might exert its anti-inflammatory effect through negatively modulating pro-inflammatory factors, such as IL-6. The inhibitory effects of quercetin on IL-6 production by neutrophils may provide a theoretical basis on future therapy of inflammation.

  15. The effect of STDP temporal kernel structure on the learning dynamics of single excitatory and inhibitory synapses.

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    Yotam Luz

    Full Text Available Spike-Timing Dependent Plasticity (STDP is characterized by a wide range of temporal kernels. However, much of the theoretical work has focused on a specific kernel - the "temporally asymmetric Hebbian" learning rules. Previous studies linked excitatory STDP to positive feedback that can account for the emergence of response selectivity. Inhibitory plasticity was associated with negative feedback that can balance the excitatory and inhibitory inputs. Here we study the possible computational role of the temporal structure of the STDP. We represent the STDP as a superposition of two processes: potentiation and depression. This allows us to model a wide range of experimentally observed STDP kernels, from Hebbian to anti-Hebbian, by varying a single parameter. We investigate STDP dynamics of a single excitatory or inhibitory synapse in purely feed-forward architecture. We derive a mean-field-Fokker-Planck dynamics for the synaptic weight and analyze the effect of STDP structure on the fixed points of the mean field dynamics. We find a phase transition along the Hebbian to anti-Hebbian parameter from a phase that is characterized by a unimodal distribution of the synaptic weight, in which the STDP dynamics is governed by negative feedback, to a phase with positive feedback characterized by a bimodal distribution. The critical point of this transition depends on general properties of the STDP dynamics and not on the fine details. Namely, the dynamics is affected by the pre-post correlations only via a single number that quantifies its overlap with the STDP kernel. We find that by manipulating the STDP temporal kernel, negative feedback can be induced in excitatory synapses and positive feedback in inhibitory. Moreover, there is an exact symmetry between inhibitory and excitatory plasticity, i.e., for every STDP rule of inhibitory synapse there exists an STDP rule for excitatory synapse, such that their dynamics is identical.

  16. Inhibitory effects of oolong tea polyphenols on pancreatic lipase in vitro.

    Science.gov (United States)

    Nakai, Masaaki; Fukui, Yuko; Asami, Sumio; Toyoda-Ono, Yoshiko; Iwashita, Takashi; Shibata, Hiroshi; Mitsunaga, Tohru; Hashimoto, Fumio; Kiso, Yoshinobu

    2005-06-01

    Fifty-four polyphenols isolated from tea leaves were evaluated for their inhibitory activities against pancreatic lipase, the key enzyme of lipid absorption in the gut. (-)-Epigallocatechin 3-O-gallate (EGCG), which is one of major polyphenols in green tea, showed lipase inhibition with an IC50 of 0.349 microM. Moreover, flavan-3-ol digallate esters, such as (-)-epigallocatechin-3,5-digallate, showed higher activities of inhibition on lipase with an IC50 of 0.098 microM. On the other hand, nonesterified flavan-3-ols, such as (+)-catechin, (-)-epicatechin, (+)-gallocatechin, and (-)-epigallocatechin, showed zero and/or the lowest activities against pancreatic lipase (IC50 > 20 microM). These data suggested that the presence of galloyl moieties within the structure was required for enhancement of pancreatic lipase inhibition. It is well-known that flavan-3-ols are polymerized by polyphenol oxidase and/or heating in a manufacturing process of oolong tea. Oolonghomobisflavans A and B and oolongtheanin 3'-O-gallate, which are typical in oolong tea leaves, showed strong inhibitory activities with IC50 values of 0.048, 0.108, and 0.068 microM, respectively, even higher than that of EGCG. The oolong tea polymerized polyphenols (OTPP) were prepared for the assay from oolong tea extract, from which the preparation effectively subtracted the zero and/or less-active monomeric flavan-3-ols by preparative high-performance liquid chromatography. The weight-average molecular weight (Mw) and number-average molecular-weight (Mn) values of OTPP were 2017 and 903, respectively, by using gel permeation choromatography. OTPP showed a 5-fold stronger inhibition against pancreatic lipase (IC50 = 0.28 microg/mL) by comparison with that of the tannase-treated OTPP (IC50 = 1.38 microg/mL). These data suggested that the presence of galloyl moieties within their chemical structures and/or the polymerization of flavan-3-ols were required for enhancement of pancreatic lipase inhibition.

  17. The Inhibitory Effects of Low-Dose Ionizing Radiation in IgE-Mediated Allergic Responses.

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    Hae Mi Joo

    Full Text Available Ionizing radiation has different biological effects according to dose and dose rate. In particular, the biological effect of low-dose radiation is unclear. Low-dose whole-body gamma irradiation activates immune responses in several ways. However, the effects and mechanism of low-dose radiation on allergic responses remain poorly understood. Previously, we reported that low-dose ionizing radiation inhibits mediator release in IgE-mediated RBL-2H3 mast cell activation. In this study, to have any physiological relevance, we investigated whether low-dose radiation inhibits allergic responses in activated human mast cells (HMC-1(5C6 and LAD2 cells, mouse models of passive cutaneous anaphylaxis and the late-phase cutaneous response. High-dose radiation induced cell death, but low-dose ionizing radiation of <0.5 Gy did not induce mast cell death. Low-dose ionizing radiation that did not induce cell death significantly suppressed mediator release from human mast cells (HMC-1(5C6 and LAD2 cells that were activated by antigen-antibody reaction. To determine the inhibitory mechanism of mediator released by low-dose ionizing radiation, we examined the phosphorylation of intracellular signaling molecules such as Lyn, Syk, phospholipase Cγ, and protein kinase C, as well as the intracellular free Ca2+ concentration ([Ca2+]i. The phosphorylation of signaling molecules and [Ca2+]i following stimulation of FcεRI receptors was inhibited by low dose ionizing radiation. In agreement with its in vitro effect, ionizing radiation also significantly inhibited inflammatory cells infiltration, cytokine mRNA expression (TNF-α, IL-4, IL-13, and symptoms of passive cutaneous anaphylaxis reaction and the late-phase cutaneous response in anti-dinitrophenyl IgE-sensitized mice. These results indicate that ionizing radiation inhibits both mast cell-mediated immediate- and delayed-type allergic reactions in vivo and in vitro.

  18. Inhibitory effect on Streptococcus mutans and mechanical properties of the chitosan containing composite resin

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    Ji-Sun Kim

    2013-02-01

    Full Text Available Objectives This study evaluated the antibacterial effect and mechanical properties of composite resins (LCR, MCR, HCR incorporating chitosan with three different molecular weights (L, Low; M, Medium; H, High. Materials and Methods Streptococcus (S. mutans 100 mL and each chitosan powder were inoculated in sterilized 10 mL Brain-Heart Infusion (BHI solution, and was centrifuged for 12 hr. Absorbance of the supernatent was measured at OD660 to estimate the antibacterial activities of chitosan. After S. mutans was inoculated in the disc shaped chitosan-containing composite resins, the disc was cleansed with BHI and diluted with serial dilution method. S. mutans was spread on Mitis-salivarius bacitracin agar. After then, colony forming unit (CFU was measured to verify the inhibitory effect on S. mutans biofilm. To ascertain the effect on the mechanical properties of composite resin, 3-point bending and Vickers hardness tests were done after 1 and 3 wk water storage, respectively. Using 2-way analysis of variance (ANOVA and Scheffe test, statistical analysis was done with 95% significance level. Results All chitosan powder showed inhibition effect against S. mutans. CFU number in chitosan-containing composite resins was smaller than that of control resin without chitosan. The chitosan containing composite resins did not show any significant difference in flexural strength and Vickers hardness in comparison with the control resin. However, the composite resin, MCR showed a slightly decreased flexural strength and the maximum load than those of control and the other composite resins HCR and LCR. Conclusions LCR and HCR would be recommended as a feasible antibacterial restorative due to its antibacterial nature and mechanical properties.

  19. General anesthetics have differential inhibitory effects on gap junction channels and hemichannels in astrocytes and neurons.

    Science.gov (United States)

    Liu, Xinhe; Gangoso, Ester; Yi, Chenju; Jeanson, Tiffany; Kandelman, Stanislas; Mantz, Jean; Giaume, Christian

    2016-04-01

    Astrocytes represent a major non-neuronal cell population actively involved in brain functions and pathologies. They express a large amount of gap junction proteins that allow communication between adjacent glial cells and the formation of glial networks. In addition, these membrane proteins can also operate as hemichannels, through which "gliotransmitters" are released, and thus contribute to neuroglial interaction. There are now reports demonstrating that alterations of astroglial gap junction communication and/or hemichannel activity impact neuronal and synaptic activity. Two decades ago we reported that several general anesthetics inhibited gap junctions in primary cultures of astrocytes (Mantz et al., (1993) Anesthesiology 78(5):892-901). As there are increasing studies investigating neuroglial interactions in anesthetized mice, we here updated this previous study by employing acute cortical slices and by characterizing the effects of general anesthetics on both astroglial gap junctions and hemichannels. As hemichannel activity is not detected in cortical astrocytes under basal conditions, we treated acute slices with the endotoxin LPS or proinflammatory cytokines to induce hemichannel activity in astrocytes, which in turn activated neuronal hemichannels. We studied two extensively used anesthetics, propofol and ketamine, and the more recently developed dexmedetomidine. We report that these drugs have differential inhibitory effects on gap junctional communication and hemichannel activity in astrocytes when used in their respective, clinically relevant concentrations, and that dexmedetomidine appears to be the least effective on both channel functions. In addition, the three anesthetics have similar effects on neuronal hemichannels. Altogether, our observations may contribute to optimizing the selection of anesthetics for in vivo animal studies.

  20. The Inhibitory Effects of Low-Dose Ionizing Radiation in IgE-Mediated Allergic Responses.

    Science.gov (United States)

    Joo, Hae Mi; Kang, Su Jin; Nam, Seon Young; Yang, Kwang Hee; Kim, Cha Soon; Lee, In Kyung; Kim, Ji Young

    2015-01-01

    Ionizing radiation has different biological effects according to dose and dose rate. In particular, the biological effect of low-dose radiation is unclear. Low-dose whole-body gamma irradiation activates immune responses in several ways. However, the effects and mechanism of low-dose radiation on allergic responses remain poorly understood. Previously, we reported that low-dose ionizing radiation inhibits mediator release in IgE-mediated RBL-2H3 mast cell activation. In this study, to have any physiological relevance, we investigated whether low-dose radiation inhibits allergic responses in activated human mast cells (HMC-1(5C6) and LAD2 cells), mouse models of passive cutaneous anaphylaxis and the late-phase cutaneous response. High-dose radiation induced cell death, but low-dose ionizing radiation of Low-dose ionizing radiation that did not induce cell death significantly suppressed mediator release from human mast cells (HMC-1(5C6) and LAD2 cells) that were activated by antigen-antibody reaction. To determine the inhibitory mechanism of mediator released by low-dose ionizing radiation, we examined the phosphorylation of intracellular signaling molecules such as Lyn, Syk, phospholipase Cγ, and protein kinase C, as well as the intracellular free Ca2+ concentration ([Ca2+]i). The phosphorylation of signaling molecules and [Ca2+]i following stimulation of FcεRI receptors was inhibited by low dose ionizing radiation. In agreement with its in vitro effect, ionizing radiation also significantly inhibited inflammatory cells infiltration, cytokine mRNA expression (TNF-α, IL-4, IL-13), and symptoms of passive cutaneous anaphylaxis reaction and the late-phase cutaneous response in anti-dinitrophenyl IgE-sensitized mice. These results indicate that ionizing radiation inhibits both mast cell-mediated immediate- and delayed-type allergic reactions in vivo and in vitro.

  1. Growth inhibitory effects produced by the cypress, Cupressus lusitanica (Cupressaceae) in Bosque de La Hoja, Heredia, Costa Rica.

    OpenAIRE

    2014-01-01

    ABSTRACT: Growth inhibitory effects produced by the cypress, Cupressus lusitanica (Cupressaceae) in Bosque de La Hoja, Heredia, Costa Rica. In Costa Rica, Cupressus lusitanica is an introduced tree that may produce negative effects in the plants surrounding it. This study sought to compare light, soil humidity and acidity provided by cypress trees and the effect on the distribution and growth of pioneer and dicotyledonous plants around them in El Bosque de la Hoja, Heredia Province, Costa Ric...

  2. Inhibitory control in bilinguals and musicians: event related potential (ERP evidence for experience-specific effects.

    Directory of Open Access Journals (Sweden)

    Sylvain Moreno

    Full Text Available Bilinguals and musicians exhibit behavioral advantages on tasks with high demands on executive functioning, particularly inhibitory control, but the brain mechanisms supporting these differences are unclear. Of key interest is whether these forms of experience influence cognition through similar or distinct information processing mechanisms. Here, we recorded event-related potentials (ERPs in three groups - bilinguals, musicians, and controls - who completed a visual go-nogo task that involved the withholding of key presses to rare targets. Participants in each group achieved similar accuracy rates and responses times but the analysis of cortical responses revealed significant differences in ERP waveforms. Success in withholding a prepotent response was associated with enhanced stimulus-locked N2 and P3 wave amplitude relative to go trials. For nogo trials, there were altered timing-specific ERP differences and graded amplitude differences observed in the neural responses across groups. Specifically, musicians showed an enhanced early P2 response accompanied by reduced N2 amplitude whereas bilinguals showed increased N2 amplitude coupled with an increased late positivity wave relative to controls. These findings demonstrate that bilingualism and music training have differential effects on the brain networks supporting executive control over behavior.

  3. Inhibitory Control in Bilinguals and Musicians: Event Related Potential (ERP) Evidence for Experience-Specific Effects

    Science.gov (United States)

    Moreno, Sylvain; Wodniecka, Zofia; Tays, William; Alain, Claude; Bialystok, Ellen

    2014-01-01

    Bilinguals and musicians exhibit behavioral advantages on tasks with high demands on executive functioning, particularly inhibitory control, but the brain mechanisms supporting these differences are unclear. Of key interest is whether these forms of experience influence cognition through similar or distinct information processing mechanisms. Here, we recorded event-related potentials (ERPs) in three groups – bilinguals, musicians, and controls – who completed a visual go-nogo task that involved the withholding of key presses to rare targets. Participants in each group achieved similar accuracy rates and responses times but the analysis of cortical responses revealed significant differences in ERP waveforms. Success in withholding a prepotent response was associated with enhanced stimulus-locked N2 and P3 wave amplitude relative to go trials. For nogo trials, there were altered timing-specific ERP differences and graded amplitude differences observed in the neural responses across groups. Specifically, musicians showed an enhanced early P2 response accompanied by reduced N2 amplitude whereas bilinguals showed increased N2 amplitude coupled with an increased late positivity wave relative to controls. These findings demonstrate that bilingualism and music training have differential effects on the brain networks supporting executive control over behavior. PMID:24743321

  4. The inhibitory effect of dihydroartemisinin on the growth of neuroblastoma cells

    Institute of Scientific and Technical Information of China (English)

    Ling Qi; Yang Yang; Yu-Cui Liu; Tian-Xin Zhu; Song Jin; Lin Zang; Yu-Ying Zhang; Kuang Ren

    2016-01-01

    Objective:To evaluate the inhibitory effect of dihydroartemisinin on neuroblastoma cell line SH-SY5 Y,explore the possible mechanism of dihydroartemisinin against neuroblastoma cells.Methods:The cell viability of dihydroartemisinin treated SH-SY5 Y cells was examined by MTT assay and morphology of cells was observed by using inverted microscope.Cell cycle was examined with flowcytometry assay,then cyclin D1 and caspase-3 proteins expression was detected by ELISA and western blotting assay.Results:MTT analysis results showed that cell viability significantly decreased after exposure to 0.05,0.50,5.00 and 50.00 mmol/L dihydroartemisinin in a dose-dependent manner,and the lower density of cells was observed in treated groups.The number of cells in sub-G1 phase was increased after treatment with different doses of dihydroartemisinin compared with the control group.The expression of cyclin D1 protein was decreased,while the expression of caspase-3 protein was increased in treated group.Conclusions:Dihydroartemisinin could inhibit the proliferation through stopping the cell cycle and inducing the apoptosis in neuroblastoma SH-SY5 Y cells.

  5. Inhibitory effect of leonurine on the formation of advanced glycation end products.

    Science.gov (United States)

    Huang, Lianqi; Yang, Xin; Peng, Anlin; Wang, Hui; Lei, Xiang; Zheng, Ling; Huang, Kun

    2015-02-01

    Long-term hyperglycemia is a typical symptom of diabetes mellitus (DM) which can cause a high level of protein glycation and lead to the formation of advanced glycation end products (AGEs). The accumulation of AGEs in turn deteriorates DM and its complications. Insulin, the only hormone that directly decreases blood sugar in vivo, is vulnerable to glycation which causes the loss of its biological activity. In this study, we used a porcine insulin (PI)-methylglyoxal (MGO) model to investigate the inhibitory effect of leonurine (LN), a natural alkaloid extracted from Herba leonuri, on AGE formation. Assays including AGE-specific fluorescence, and fructosamine level and carbonyl group content determination showed that LN can dose-dependently suppress PI glycation. A significantly decreased cross-linking level on the glycated PI was also proven by SDS-PAGE electrophoresis. A further liquid chromatography-mass spectrometry study suggested that LN may inhibit PI glycation through trapping MGO and keeping it from reacting with PI. Our results thus indicate that LN is a promising anti-glycation agent for the prevention of diabetes and its complications via inhibiting AGE formation.

  6. Inhibitory Effects of Several Essential Oils towards Salmonella typhimurium, Salmonella paratyphi A and Salmonella paratyphi B

    Directory of Open Access Journals (Sweden)

    S.F. Mazhar

    2014-09-01

    Full Text Available Plant essential oils are natural products extracted from plants and because of their antimicrobial properties can be used as natural additives in foods. They are also useful for decontamination of food-borne pathogens and can be a safe additive in foods. The antimicrobial activities of essential oils belonging to Saturiea hortensis, Thymus vulgaris, Mentha polegium, Cuminum cyminum, Lavandula officinalis and Mentha viridis L. (spearmint were investigated at different concentrations (0.1, 0.3, 0.5, 1, 2, 5 and 10%v/v against Salmonella typhimurium, Salmonella paratyphi A and Salmonella paratyphi B by using the agar well diffusion method. Essential oils showed inhibitory effect on Salmonella spp. in the agar well diffusion assay. In addition, the capability of essential oils for decontamination of minced row beef, ground beef, minced raw chicken and minced raw fish inoculated with Salmonella spp. at 0.1 and 0.5%v/v were assessed. Reduction of the Salmonella spp. population was observed following the inoculation of the cultures with 0.1 and 0.5%v/v essential oils.

  7. Synthesis of 4-(2-substituted hydrazinyl)benzenesulfonamides and their carbonic anhydrase inhibitory effects.

    Science.gov (United States)

    Gul, Halise Inci; Kucukoglu, Kaan; Yamali, Cem; Bilginer, Sinan; Yuca, Hafize; Ozturk, Iknur; Taslimi, Parham; Gulcin, Ilhami; Supuran, Claudiu T

    2016-08-01

    In this study, 4-(2-substituted hydrazinyl)benzenesulfonamides were synthesized by microwave irradiation and their chemical structures were confirmed by (1)H NMR, (13)CNMR, and HRMS. Ketones used were: Acetophenone (S1), 4-methylacetophenone (S2), 4-chloroacetophenone (S3), 4-fluoroacetophenone (S4), 4-bromoacetophenone (S5), 4-methoxyacetophenone (S6), 4-nitroacetophenone (S7), 2-acetylthiophene (S8), 2-acetylfuran (S9), 1-indanone (S10), 2-indanone (S11). The compounds S9, S10 and S11 were reported for the first time, while S1-S8 was synthesized by different method than literature reported using microwave irradiation method instead of conventional heating in this study. The inhibitory effects of 4-(2-substituted hydrazinyl)benzenesulfonamide derivatives (S1-S11) against hCA I and II were studied. Cytosolic hCA I and II isoenzymes were potently inhibited by new synthesized sulphonamide derivatives with Kis in the range of 1.79 ± 0.22-2.73 ± 0.08 nM against hCA I and in the range of 1.72 ± 0.58-11.64 ± 5.21 nM against hCA II, respectively.

  8. Inhibitory effects of apoptotic cell ingestion upon endotoxin-driven myeloid dendritic cell maturation.

    Science.gov (United States)

    Stuart, Lynda M; Lucas, Mark; Simpson, Cathy; Lamb, Jonathan; Savill, John; Lacy-Hulbert, Adam

    2002-02-15

    Dendritic cells (DCs) are the sentinels of the immune system, able to interact with both naive and memory T cells. The recent observation that DCs can ingest cells dying by apoptosis has raised the possibility that DCs may, in fact, present self-derived Ags, initiating both autoimmunity and tumor-specific responses, especially if associated with appropriate danger signals. Although the process of ingestion of apoptotic cells has not been shown to induce DC maturation, the exact fate of these phagocytosing DCs remains unclear. In this paper we demonstrate that DCs that ingest apoptotic cells are able to produce TNF-alpha but have a diminished ability to produce IL-12 in response to external stimuli, a property that corresponds to a failure to up-regulate CD86. By single-cell analysis we demonstrate that these inhibitory effects are restricted to those DCs that have engulfed apoptotic cells, with bystander DCs remaining unaffected. These changes were independent of the production of anti-inflammatory cytokines TGF-beta1 and IL-10 and corresponded with a diminished capacity to stimulate naive T cells. Thus, the ingestion of apoptotic cells is not an immunologically null event but is capable of modulating DC maturation. These results have important implications for our understanding of the role of clearance of dying cells by DCs not only in the normal resolution of inflammation but also in control of subsequent immune responses to apoptotic cell-derived Ags.

  9. GROWTH-INHIBITORY EFFECTS OF CURCUMIN ON Raji CELLS AND ITS MECHANISMS

    Institute of Scientific and Technical Information of China (English)

    CHEN Yan; WU Qing; LI Xin-gang

    2005-01-01

    Objective: To study the growth-inhibitory effects of curcumin on B-NHL cell line Raji cells in vitro and its molecular mechanisms. Methods: The growth inhibition rates of Raji cells, after being treated with 6.25 μmol/L~50 μmol/L curcumin for 12 h ~ 48 h, were examined by MTT assay. The apoptosis rate was detected by flow cytometry (FCM), the protein expression levels of bcl-2 and p53 in Raji cells were examined by SP immunohistochemistry. The expression of p53 in Raji cell were checked by RT-PCR. Results: After being treated by various concentrations of curcumin, the growth of Raji cells was inhibited significantly. The rates of apoptosis were 11.8% ~79.7% (P<0.01), the down regulation of p53 expression was observed within 24 h after the treatment of curcumin by RT-PCR. The expression of bcl-2 and p53 was decreased, which depended on the action time. Conclusion: Curcumin could significantly inhibit the growth of Raji cells. The induction of apoptosis by down-regulating the expression of bcl-2 and p53 was probably one of its molecular mechanisms.

  10. Inhibitory effects of Lactobacillus rhamnosus and Lactobacillus casei on Candida biofilm of denture surface.

    Science.gov (United States)

    Song, Young-Gyun; Lee, Sung-Hoon

    2017-04-01

    Candida albicans biofilm is associated with denture-related stomatitis and oral candidiasis of elderly. Probiotics are beneficial bacteria and have antibacterial activity against pathogenic bacteria. The purpose of this study was to investigate the antifungal activity of various probiotics against C. albicans and the inhibitory effects of probiotics on Candida biofilm on the denture surface. The spent culture media of various probiotics were investigated the antifungal efficacy against C. albicans. Candida biofilm was formed on a denture base resin and was then treated with Lactobacillus rhamnosus and Lactobacillus casei. Also, the biofilms of L. rhamnosus and L. casei were formed and were sequentially treated with C. albicans. Colony-forming units of C. albicans on the denture surface were counted after spreading on agar plate. The denture base resin was treated with the spent culture media for 30days, after which the denture surface roughness was analyzed with an atomic force microscope. L. rhamnosus and L. casei exhibited stronger antifungal activity than other probiotics. The spent culture medium of L. rhamnosus and L. casei exhibited the antifungal activity against blastoconidia and biofilm of C. albicans. L. rhamnosus and L. casei showed the antifungal activity against Candida biofilm, and the biofilm of L. rhamnosus and L. casei inhibited formation of Candida biofilm on denture surface. Neither of the probiotics affected the surface roughness of the denture base resin. L. rhamnosus and L. casei may be the ideal probiotics for the prevention and treatment of denture-related stomatitis. Copyright © 2017 Elsevier Ltd. All rights reserved.

  11. [Inhibitory effect of kaempferol on inflammatory response of lipopolysaccharide-stimulated human mast cells].

    Science.gov (United States)

    Zhou, Yun-jiang; Wang, Hu; Li, Li; Sui, He-huan; Huang, Jia-jun

    2015-06-01

    This study is to investigate the inhibitory effect of kaempferol on inflammatory response of lipopolysaccharide(LPS)-stimulated HMC-1 mast cells. The cytotoxicity of kaempferol to HMC-1 mast cells were analyzed by using MTT assay and then the administration concentrations of kaempferol were established. Histamine, IL-6, IL-8, IL-1β and TNF-α were measured using ELISA assay in activated HMC-1 mast cells after incubation with various concentrations of kaempferol (10, 20 and 40 µmol.L-1). Western blot was used to test the protein expression of p-IKKβ, IκBα, p-IκBα and nucleus NF-κB of LPS-induced HMC-1 mast cells after incubation with different concentrations of kaempferol. The optimal concentrations of kaempferol were defined as the range from 5 µmol.L-1 to 40 µmol.L-1. Kaempferol significantly decreased the release of histamine, IL-6, IL-8, IL-1β and TNF-α of activated HMC-1 mast cells (Pkaempferol, the protein expression of p-IKKβ, p-IKBa and nucleus NF-κB (p65) markedly reduced in LPS-stimulated HMC-1 mast cells (Pkaempferol markedly inhibit mast cell-mediated inflammatory response. At the same time, kaempferol can inhibit the activation of IKKβ, block the phosphorylation of IκBα, prevent NF-KB entering into the nucleus, and then decrease the release of inflammatory mediators.

  12. Multiscale modeling reveals inhibitory and stimulatory effects of caffeine on acetaminophen-induced toxicity in humans.

    Science.gov (United States)

    Thiel, C; Cordes, H; Baier, V; Blank, L M; Kuepfer, L

    2017-02-01

    Acetaminophen (APAP) is a widely used analgesic drug that is frequently co-administered with caffeine (CAF) in the treatment of pain. It is well known that APAP may cause severe liver injury after an acute overdose. However, the understanding of whether and to what extent CAF inhibits or stimulates APAP-induced hepatotoxicity in humans is still lacking. Here, a multiscale analysis is presented that quantitatively models the pharmacodynamic (PD) response of APAP during co-medication with CAF. Therefore, drug-drug interaction (DDI) processes were integrated into physiologically based pharmacokinetic (PBPK) models at the organism level, whereas drug-specific PD response data were contextualized at the cellular level. The results provide new insights into the inhibitory and stimulatory effects of CAF on APAP-induced hepatotoxicity for crucially affected key cellular processes and individual genes at the patient level. This study might facilitate the risk assessment of drug combination therapies in humans and thus may improve patient safety in clinical practice. © 2017 The Authors CPT: Pharmacometrics & Systems Pharmacology published by Wiley Periodicals, Inc. on behalf of American Society for Clinical Pharmacology and Therapeutics.

  13. Multiscale modeling reveals inhibitory and stimulatory effects of caffeine on acetaminophen‐induced toxicity in humans

    Science.gov (United States)

    Thiel, C; Cordes, H; Baier, V; Blank, LM

    2017-01-01

    Acetaminophen (APAP) is a widely used analgesic drug that is frequently co‐administered with caffeine (CAF) in the treatment of pain. It is well known that APAP may cause severe liver injury after an acute overdose. However, the understanding of whether and to what extent CAF inhibits or stimulates APAP‐induced hepatotoxicity in humans is still lacking. Here, a multiscale analysis is presented that quantitatively models the pharmacodynamic (PD) response of APAP during co‐medication with CAF. Therefore, drug‐drug interaction (DDI) processes were integrated into physiologically based pharmacokinetic (PBPK) models at the organism level, whereas drug‐specific PD response data were contextualized at the cellular level. The results provide new insights into the inhibitory and stimulatory effects of CAF on APAP‐induced hepatotoxicity for crucially affected key cellular processes and individual genes at the patient level. This study might facilitate the risk assessment of drug combination therapies in humans and thus may improve patient safety in clinical practice. PMID:28130915

  14. Inhibitory effects of tetradecanoylphorbol acetate and diacylglycerol on erythropoietin production in human renal carcinoma cell cultures

    Energy Technology Data Exchange (ETDEWEB)

    Hagiwara, Masamichi; Nagakura, Kazuhiko; Ueno, Munehisa; Fisher, J.W. (Tulane Univ., New Orleans, LA (United States))

    1987-11-01

    A human renal carcinoma from a patient with an erythrocytosis, serially transplanted into athymic nude mice, was grown in primary monolayer cell cultures. After reaching confluency the cultured cells formed multicellular hemicysts (domes) which became more abundant as the cultures approached saturation density. Erythropoietin (Ep) production by this renal carcinoma in culture was only slightly increased at the time of semiconfluency but showed a marked increase in Ep levels in the culture medium after the cultures reached confluency, in parallel with an increase in dome formation. The phorbol ester tumor promoter 12-O-tetradecanoylphorbol-13-acetate (TPA) showed a significant dose-related inhibitory effect on Ep production and dome formation in the renal carcinoma cell cultures, suggesting an important role of protein kinase C, the only known receptor for TPA, in inhibiting the expression of differentiated phenotypes in the renal carcinoma cells. These studies suggest a role of the inositol-lipid second messenger path and protein kinase C in the regulation of Ep production.

  15. Inhibitory effect of cucurbitacin B on imiquimod-induced skin inflammation

    Energy Technology Data Exchange (ETDEWEB)

    Li, Zheng Jun; Shin, Jung-Min; Choi, Dae-Kyoung; Lim, Seul Ki [Department of Dermatology, School of Medicine, Chungnam National University, Daejeon (Korea, Republic of); Yoon, Tae-Jin [Department of Dermatology, School of Medicine, Gyeongsang National University, Jinju (Korea, Republic of); Lee, Young Ho [Department of Anatomy, School of Medicine, Chungnam National University, Daejeon (Korea, Republic of); Sohn, Kyung-Cheol; Im, Myung; Lee, Young; Seo, Young-Joon; Kim, Chang Deok [Department of Dermatology, School of Medicine, Chungnam National University, Daejeon (Korea, Republic of); Lee, Jeung-Hoon, E-mail: jhoon@cnu.ac.kr [Department of Dermatology, School of Medicine, Chungnam National University, Daejeon (Korea, Republic of); Skin Med Company, Daejeon (Korea, Republic of)

    2015-04-17

    Psoriasis is a common skin disease, of which pathogenesis involves the increase of inflammatory reaction in epidermal cells. In an attempt to find therapeutics for psoriasis, we found that cucurbitacin B has an inhibitory potential on imiquimod-induced inflammation of keratinocytes. Cucurbitacin B significantly inhibited imiquimod-induced expression of crucial psoriatic cytokines, such as IL-8 and CCL20, via down-regulation of NF-κB and STAT3 signaling pathway in human keratinocytes. In addition, keratinocyte proliferation was markedly inhibited by cucurbitacin B. The potential beneficial effect of cucurbitacin B on psoriasis was further validated in imiquimod-induced psoriasiform dermatitis of experimental animal. Topical application of cucurbitacin B resulted in significant reduction of epidermal hyperplasia and inflammatory cytokines production, and ameliorated the psoriatic symptom. Taken together, these results suggest that cucurbitacin B may be a potential candidate for the treatment of psoriasis. - Highlights: • Cucurbitacin B has a potential for inhibiting the growth of keratinocytes. • Cucurbitacin B inhibits imiquimod-induced inflammatory reaction in keratinocytes. • Cucurbitacin B inhibits imiquimod-induced psoriasiform dermatitis in experimental animal.

  16. Inhibitory effects of schisandrin A and schisandrin B on CYP3A activity.

    Science.gov (United States)

    Li, W L; Xin, H W; Su, M W; Xiong, L

    2010-04-01

    Our aim was to investigate the inhibitory effects of schisandrin A and schisandrin B on cytochrome P450 (CYP3A) activity in rat liver microsomes and the mechanism of this interaction. 1'-Hydroxy midazolam and midazolam 1-hydroxylation catalyzed by CYP3A were analyzed by high performance liquid chromatography (HPLC). Results showed that schisandrin A and schisandrin B inhibited CYP3A activity with IC(50) values of 6.60 and 5.51 microM and K(i) values of 5.83 and 4.24 microM, respectively. A dilution assay plot of each inhibitor gave a slope value of up to 91% that of the control samples. The inactivation of CYP3A activity by schisandrin A and schisandrin B was found to be both time-and concentration-dependent (schisandrin A: K(I) = 4.51 microM, K(inact) = 0.134/min; schisandrin B: K(I) = 3.01 microM, K(inact) = 0.112/min). We conclude that the inhibition of CYP3A activity in rat liver microsomes by schisandrin A and schisandrin B is mostly attributed to a mixed noncompetitive and complete inhibition.

  17. Inhibitory effects of alkaloids from Sophora alopecuroids on feeding,development and reproduction of Clostera anastomosis

    Institute of Scientific and Technical Information of China (English)

    Yang Zhende; Zhao Boguang; Zhu Lin; Fang Jie; Xia Luqing

    2006-01-01

    Alkaloids from Sophora alopecuroids were bioassayed with Clostera anastomosis for their antifeedant and growth inhibitory effects.The antifeedant rate in choice test reached 62%-86% at the dose 2.5 mg/mL,while in non-choice bioassay the rate was only 20%-29%.In choice bioassay,the anfifeedant rate increased with larval instars of C anastomosis and did not in non-choice experiment.The alkaloids also imposed a strong influence on the growth of C anastomosis larvae,i.e.,after feeding on the leaves treated with alkaloid,the larvae lost their weight,weight gain,and relative growth rate (RGR) significantly when compared with the controls.In the second day after treatment with the dose at 10 mg/mL of the alkaloid,the RGR reduced by 39.8%,and the food intake and the feces weight were respectively 57.7% and 57.4% of the controls.The approximate digestibility (AD) increased significantly,and the efficiency in converting digested food (ECD),and the efficiency in converting ingested food (ECI) decreased greatly after feeding the treated leaves.Moreover,the eggs laid per female were also inhibited by this alkaloid.The significance and prospect of the alkaloids in controlling forest insect pests were also discussed.

  18. Inhibitory effect of Allium sativum and Zingiber officinale extracts on clinically important drug resistant pathogenic bacteria

    Directory of Open Access Journals (Sweden)

    Gull Iram

    2012-04-01

    Full Text Available Abstract Background Herbs and spices are very important and useful as therapeutic agent against many pathological infections. Increasing multidrug resistance of pathogens forces to find alternative compounds for treatment of infectious diseases. Methods In the present study the antimicrobial potency of garlic and ginger has been investigated against eight local clinical bacterial isolates. Three types of extracts of each garlic and ginger including aqueous extract, methanol extract and ethanol extract had been assayed separately against drug resistant Escherichia coli, Pseudomonas aeruginosa, Bacillus subtilis, Staphylococcus aureus, Klebsiella pneumoniae, Shigella sonnei, Staphylococcusepidermidis and Salmonella typhi. The antibacterial activity was determined by disc diffusion method. Results All tested bacterial strains were most susceptible to the garlic aqueous extract and showed poor susceptibility to the ginger aqueous extract. The (minimum inhibitory concentration MIC of different bacterial species varied from 0.05 mg/ml to 1.0 mg/ml. Conclusion In the light of several socioeconomic factors of Pakistan mainly poverty and poor hygienic condition, present study encourages the use of spices as alternative or supplementary medicine to reduce the burden of high cost, side effects and progressively increasing drug resistance of pathogens.

  19. Oxytocin's inhibitory effect on food intake is stronger in obese than normal-weight men.

    Science.gov (United States)

    Thienel, M; Fritsche, A; Heinrichs, M; Peter, A; Ewers, M; Lehnert, H; Born, J; Hallschmid, M

    2016-11-01

    Animal studies and pilot experiments in men indicate that the hypothalamic neuropeptide oxytocin limits food intake, and raise the question of its potential to improve metabolic control in obesity. We compared the effect of central nervous oxytocin administration (24 IU) via the intranasal route on ingestive behaviour and metabolic function in 18 young obese men with the results in a group of 20 normal-weight men. In double-blind, placebo-controlled experiments, ad libitum food intake from a test buffet was examined in fasted subjects 45 min after oxytocin administration, followed by the assessment of postprandial, reward-driven snack intake. Energy expenditure was repeatedly assessed by indirect calorimetry and blood was sampled to determine concentrations of blood glucose and hormones. Oxytocin markedly reduced hunger-driven food intake in the fasted state in obese but not in normal-weight men, and led to a reduction in snack consumption in both groups, whereas energy expenditure remained generally unaffected. Hypothalamic-pituitary-adrenal axis secretion and the postprandial rise in plasma glucose were blunted by oxytocin in both groups. Oxytocin exerts an acutely inhibitory impact on food intake that is enhanced rather than decreased in obese compared with normal-weight men. This pattern puts it in contrast to other metabolically active neuropeptides and bodes well for clinical applications of oxytocin in the treatment of metabolic disorders.

  20. Inhibitory Effect of Furanic and Phenolic Compounds on Exoelectrogenesis in a Microbial Electrolysis Cell Bioanode.

    Science.gov (United States)

    Zeng, Xiaofei; Borole, Abhijeet P; Pavlostathis, Spyros G

    2016-10-18

    The objective of this study was to systematically investigate the inhibitory effect of furfural (FF), 5-hydroxymethylfurfural (HMF), syringic acid (SA), vanillic acid (VA), and 4-hydroxybenzoic acid (HBA), which are problematic lignocellulose-derived byproducts, on exoelectrogenesis in the bioanode of a microbial electrolysis cell. The five compound mixture at an initial total concentration range from 0.8 to 8.0 g/L resulted in an up to 91% current decrease as a result of exoelectrogenesis inhibition; fermentative, nonexoelectrogenic biotransformation pathways of the five compounds were not affected. Furthermore, the parent compounds at a high concentration, as opposed to their biotransformation products, were responsible for the observed inhibition. All five parent compounds contributed to the observed inhibition of the mixture. The IC50 (i.e., concentration resulting in 50% current decrease) of individually tested parent compounds was 2.7 g/L for FF, 3.0 g/L for HMF, 1.9 g/L for SA, 2.1 g/L for VA and 2.0 g/L for HBA. However, the parent compounds, when tested below their respective noninhibitory concentration, jointly resulted in significant inhibition as a mixture. Catechol and phenol, which were persistent biotransformation products, inhibited exoelectrogenesis only at high concentrations, but to a lesser extent than the parent compounds. Exoelectrogenesis recovery from inhibition by all compounds was observed at different rates, with the exception of catechol, which resulted in irreversible inhibition.

  1. PHYSIOLOGICAL INHIBITORY EFFECT OF OCS IN ARACHIDONIC ACID-RICH PARIETOCHLORIS INCISA (TREBOUXIOPHYCEAE, CHLOROPHYTA)

    Institute of Scientific and Technical Information of China (English)

    刘建国; 张成武; ZviCohen; AmosRichmond

    2002-01-01

    Parietochloris incisa is an arachidonic acid-rich snow green alga. The main physiological profiles, such as ash free dry weight (AFDW), chlorophyll, carotenoid, protein and total fatty acids (TFA), in this alga exposed to old culture supernatant (OCS) at the decline phase or its crude ethyl acetate extracts (CEAE) were investigated by using tubular photobioreactors of different diameters. Results showed that both OCS and CEAE had strong inhibitory effect on the above physiological parameters. The longer the culture was exposed to OCS and the more CEAE were added into the algal culture, the more the above physiological properties were inhibited. Arachidonic acid (AA), the dominant component of fatty acids in this alga, was also seriously inhibited with respect to total TFA, AFDW of cell mass, or culture volume, due to a prebable reduction of enzymes activities catalyzing chain elongation from C18:1ω9 to AA. These results incontestably evidenced that some CEAE dissolving substances existing in OCS, like auto-inhibitors, inhibited P. incisa growth through feedback. Hence, any efficient removal of auto-inhibitors from algal culture to decrease their bioactivity could be good for maximal production of desired products like AA.

  2. Inhibitory effect of Ferula asafoetida L. (Umbelliferae) on Blastocystis sp. subtype 3 growth in vitro.

    Science.gov (United States)

    El Deeb, Hala K; Al Khadrawy, Faisal M; Abd El-Hameid, Ayman K

    2012-09-01

    Asafoetida is an oleo-gum-resin obtained from many Ferula species and frequently used in traditional medicine. The current study aimed to evaluate the activity of asafoetida against the in vitro growth of Blastocystis sp. Asafoetida as powder-form (Ap) and oil-form (Ao) extracts at concentrations of 2, 4, 8, 16, and 20 mg/ml and 5, 10, 25, 40, and 50 mg/ml, respectively were incubated with isolates of Blastocystis sp. subtype 3 for 24, 72, and 144 h and compared to the reference antiprotozoan drug metronidazole at concentrations of 10, 100, and 500 μg/ml. Asafoetida either as Ap or Ao decreased counts and viability of all tested isolates of Blastocystis sp. subtype 3 which was confirmed by microscopy. The degree of the inhibitory effect was dependent on the concentration, form, as well as the time of incubation with asafoetida extracts. The lowest concentrations of Ap and Ao that caused complete (100 %) inhibition of Blastocystis growth and highest (100 %) percentage inhibition of multiplication was 16 and 40 mg/ml, respectively; mean counts at these concentrations either did not differ or decreased significantly when compared to metronidazole control (p < 0.05). Also, the parasites did not resume growth after re-cultivation in asafoetida-free medium when examined further after 48, 72, and 144 h of cultivation. These findings demonstrate the potential of phytomedicine asafoetida as a potent natural alternative for treatment of Blastocystis sp.infection.

  3. Inhibitory Effects of Pretreatment with Radon on Acute Alcohol-Induced Hepatopathy in Mice

    Directory of Open Access Journals (Sweden)

    Teruaki Toyota

    2012-01-01

    Full Text Available We previously reported that radon inhalation activates antioxidative functions in the liver and inhibits carbon tetrachloride-induced hepatopathy in mice. In addition, it has been reported that reactive oxygen species contribute to alcohol-induced hepatopathy. In this study, we examined the inhibitory effects of radon inhalation on acute alcohol-induced hepatopathy in mice. C57BL/6J mice were subjected to intraperitoneal injection of 50% alcohol (5 g/kg bodyweight after inhaling approximately 4000 Bq/m3 radon for 24 h. Alcohol administration significantly increased the activities of glutamic oxaloacetic transaminase (GOT, glutamic pyruvic transaminase (GPT in serum, and the levels of triglyceride and lipid peroxide in the liver, suggesting acute alcohol-induced hepatopathy. Radon inhalation activated antioxidative functions in the liver. Furthermore, pretreatment with radon inhibited the depression of hepatic functions and antioxidative functions. These findings suggested that radon inhalation activated antioxidative functions in the liver and inhibited acute alcohol-induced hepatopathy in mice.

  4. PHYSIOLOGICAL INHIBITORY EFFECT OF OCS IN ARACHIDONIC ACID-RICH PARIETOCHLORIS INCISA (TREBOUXIOPHYCEAE,CHLOROPHYTA)

    Institute of Scientific and Technical Information of China (English)

    2002-01-01

    Parietochloris incisa is an arachidonic acid-rich snow green alga. The main phy siological profiles, such as ash free dry weight (AFDW), chlorophyll, carotenoid , protein and total fatty acids (TFA), in this alga exposed to old culture super natant (OCS) at the decline phase or its crude ethyl acetate extracts (CEAE) wer e investigated by using tubular photobioreactors of different diameters. Results showed that both OCS and CEAE had strong inhibitory effect on the above physiol ogical parameters. The longer the culture was exposed to OCS and the more CEAE w ere added into the algal culture, the more the above physiological properties we re inhibited. Arachidonic acid (AA), the dominant component of fatty acids in th is alga, was also seriously inhibited with respect to total TFA, AFDW of cell ma ss, or culture volume, due to a probable reduction of enzymes activities catalyz ing chain elongation from C18:1ω9 to AA. These results incontestably evidenced t hat some CEAE dissolving substances existing in OCS, like auto-inhibitors, inhi bited P. incisa growth through feedback. Hence, any efficient removal of aut o-i nhibitors from algal culture to decrease their bioactivity could be good for max imal production of desired products like AA.

  5. Physiological inhibitory effect of ocs in arachidonic acid-rich Parietochloris incisa (trebouxiophyceae, chlorophyta)

    Science.gov (United States)

    Liu, Jian-Guo; Zhang, Cheng-Wu; Cohen, Zvi; Richmond, Amos

    2002-09-01

    Parietochloris incisa is an arachidonic acid-rich snow green alga. The main physiological profiles, such as ash free dry weight (AFDW), chlorophyll, carotenoid, protein and total fatty acids (TFA), in this alga exposed to old culture supernatant (OCS) at the decline phase or its crude ethyl acetate extracts (CEAE) were investigated by using tubular photobioreactors of different diameters. Results showed that both OCS and CEAE had strong inhibitory effect on the above physiological parameters. The longer the culture was exposed to OCS and the more CEAE were added into the algal culture, the more the above physiological properties were inhibited. Arachidonic acid (AA), the dominant component of fatty acids in this alga, was also seriously inhibited with respect to total TFA, AFDW of cell mass, or culture volume, due to a probable reduction of enzymes activities catalyzing chain elongation from C18; 1ω9 to AA. These results incontestably evidenced that some CEAE dissolving substances existing in OCS. like auto-inhibitors, inhibited P. incisa growth through feedback. Hence, any efficient removal of auto-inhibitors from algal culture to decrease their bioactivity could be good for maximal production of desired products like AA.

  6. Inhibitory effects of furan derivatives and phenolic compounds on dark hydrogen fermentation.

    Science.gov (United States)

    Lin, Richen; Cheng, Jun; Ding, Lingkan; Song, Wenlu; Zhou, Junhu; Cen, Kefa

    2015-11-01

    The inhibitory effects of furan derivatives [i.e. furfural and 5-hydroxymethylfurfural (5-HMF)] and phenolic compounds (i.e. vanillin and syringaldehyde) on dark hydrogen fermentation from glucose were comparatively evaluated. Phenolic compounds exhibited stronger inhibition on hydrogen production and glucose consumption than furan derivatives under the same 15mM concentration. Furan derivatives were completely degraded after 72h fermentation, while over 55% of phenolic compounds remained unconverted after 108h fermentation. The inhibition coefficients of vanillin (14.05) and syringaldehyde (11.21) were higher than those of 5-HMF (4.35) and furfural (0.64). Vanillin exhibited the maximum decrease of hydrogen yield (17%). The consumed reducing power by inhibitors reduction from R-CHO to RCH2OH was a possible reason contributed to the decreased hydrogen yield. Vanillin exhibited the maximum delay of peak times of hydrogen production rate and glucose consumption. Soluble metabolites and carbon conversion efficiency decreased with inhibitors addition, which were consistent with hydrogen production.

  7. Effect of fibronectin and leu- kaemia inhibitory factor on matrix metalloproteinases in mouse blastocyst

    Institute of Scientific and Technical Information of China (English)

    2001-01-01

    This study was designed to detect the effects of fibronectin (FN) and leukaemia inhibitory factor (LIF) on matrix metallopoteinases (MMPs) of mouse blastocysts. The experiments comprised four groups: first, blastocysts grew on the dishes with FN-coated; the second, without FN-coated; the third group, without FN coated, but with 20 ng/mL LIF added to culture medium; and the fourth group, with both FN-coated and 20 ng/mL LIF added. Using MMP-2 and MMP-9 primers respectively, the expressions of MMP-2 and MMP-9 were detected by RT-PCR and cloning identification. The results showed that in the first group, MMP-2 and MMP-9 were produced after 12 and 24 h culturing; in the third group, there were both MMP-2 and MMP-9 bands when blastocysts were cultured for 24 h; and in the fourth group, MMP-2 and MMP-9 bands appeared when blasto-cysts were cultured for 6, 12 and 24 h. But in the second group no MMP-2 or MMP-9 band appeared. These results show that FN may initiate the transcription of MMP-2 and MMP-9 genes to mRNA through signal transduction path-way mediated by integrin receptor and LIF may promote the expression of MMPs mRNA, which guaranteed the accuracy of embryo implantation by associating the invasive blasto-cysts with the receptive endometrium.

  8. The inhibitory effect of IFN-γ on protease HTRA1 expression in rheumatoid arthritis.

    Science.gov (United States)

    Hou, Yuzhu; Lin, Haijiang; Zhu, Linnan; Liu, Zhaoting; Hu, Fanlei; Shi, Jianfeng; Yang, Tao; Shi, Xiaoyun; Guo, Huifang; Tan, Xiaotian; Zhang, Lianfeng; Wang, Qiang; Li, Zhanguo; Zhao, Yong

    2014-07-01

    The high temperature requirement A1 (HTRA1) is a potent protease involved in many diseases, including rheumatoid arthritis (RA). However, the regulatory mechanisms that control HTRA1 expression need to be determined. In this study, we demonstrated that IFN-γ significantly inhibited the basal and LPS-induced HTRA1 expression in fibroblasts and macrophages, which are two major cells for HTRA1 production in RA. Importantly, the inhibitory effect of IFN-γ on HTRA1 expression was evidenced in collagen-induced arthritis (CIA) mouse models and in human RA synovial cells. In parallel with the enhanced CIA incidence and pathological changes in IFN-γ-deficient mice, HTRA1 expression in the joint tissues was also increased as determined by real-time PCR and Western blots. IFN-γ deficiency increased the incidence of CIA and the pathological severity in mice. Neutralization of HTRA1 by Ab significantly reversed the enhanced CIA frequency and severity in IFN-γ-deficient mice. Mechanistically, IFN-γ negatively controls HTRA1 expression through activation of p38 MAPK/STAT1 pathway. Dual luciferase reporter assay and chromatin immunoprecipitation analysis showed that STAT1 could directly bind to HTRA1 promoter after IFN-γ stimulation. This study offers new insights into the molecular regulation of HTRA1 expression and its role in RA pathogenesis, which may have significant impact on clinical therapy for RA and possibly other HTRA1-related diseases, including osteoarthritis, age-related macular degeneration, and cancer.

  9. Antifungal properties and inhibitory effects upon aflatoxin production of Thymus vulgaris L. by Aspergillus flavus Link.

    Science.gov (United States)

    Kohiyama, Cássia Yumie; Yamamoto Ribeiro, Milene Mayumi; Mossini, Simone Aparecida Galerani; Bando, Erika; Bomfim, Natália da Silva; Nerilo, Samuel Botião; Rocha, Gustavo Henrique Oliveira; Grespan, Renata; Mikcha, Jane Martha Graton; Machinski, Miguel

    2015-04-15

    The antifungal and antiaflatoxigenic properties of Thymus vulgaris essential oil (TEO) were evaluated upon Aspergillus flavus "in vitro". Suspension containing 10(6) of A. flavus were cultivated with TEO in concentrations ranging from 50 to 500 μg/mL. TEO reached minimum inhibitory concentration (MIC) and minimum fungicidal concentration (MFC) at 250 μg/mL. Inhibition of ergosterol biosynthesis was detected at a concentration of 100 μg/mL of TEO. Morphological evaluation performed by both light microscopy and scanning electron microscopy showed that antifungal activity of TEO could be detected starting at a concentration of 50 μg/mL and the fungicide effect at a concentration of 250 μg/mL. TEO completely inhibited production of both B1 and B2 aflatoxins (AFB1 and AFB2) at a concentration of 150 μg/mL. This way, fungal biomass development and aflatoxin production were dependent on TEO concentration. Therefore, TEO was capable of controlling the growth of A. flavus and its production of aflatoxins.

  10. Evaluation of Inhibitory Effect of the Plant Phyllanthus amarus Against Dermatophytic Fungi Microsporum gypseum

    Institute of Scientific and Technical Information of China (English)

    ANURAG AGRAWAL; SHALINI SRIVASTAVA; J. N. SRIVASTAVA; M. M. SRIVASAVA

    2004-01-01

    The antifungal activity of various solvent extracts (such as ether, chloroform, ethyl acetate and ethyl alcohol) of the plant Phyllanthus amarus against dermatophytic fungi Microsporum gypseum was observed. Method Antifungal bioassay in terms of reduction in weight, colony diameter and sporulation of the target fungal colony was carried out using Broth Dilution method. Results Root part of the plant, extracted in various organic solvents did not show any noticeable antifungal activity. The percentage inhibition observed in different solvent extracts of aerial part was found as reduction in weight: chloroform [50.3%], ethyl acetate [27.7%] and ethyl alcohol [12.1%], reduction in colony diameter: chloroform [53.4%], ethyl acetate [31.4%] and ethyl alcohol [15.0%] and reduction in sporulation: maximum inhibition in chloroform extract, at test concentration of 4000 ppm at incubation period of 8 days. Conclusion Chloroform fraction of the aerial part of the plant P. amarus shows significant inhibitory effect against dermatophytic fungi M. gypseum and requires chemical characterization for its bioactive principle.

  11. In vitro inhibitory effects of plant-derived by-products against Cryptosporidium parvum

    Directory of Open Access Journals (Sweden)

    Teichmann Klaus

    2016-01-01

    Full Text Available Disposal of organic plant wastes and by-products from the food or pharmaceutical industries usually involves high costs. In the present study, 42 samples derived from such by-products were screened in vitro against Cryptosporidium parvum, a protozoan parasite that may contaminate drinking water and cause diarrhoea. The novel bioassay was previously established in the microtitre plate format. Human ileocaecal adenocarcinoma (HCT-8 cell cultures were seeded with C. parvum oocysts and parasite development was monitored by an indirect fluorescent antibody technique (IFAT and microscopic assessment for clusters of secondary infection (CSI. Minimum inhibitory concentrations (MICs and potential detrimental effects on the host cells were determined. An ethanolic extract from olive (Olea europaea pomace, after oil pressing and phenol recovery, reproducibly inhibited C. parvum development (MIC = 250–500 μg mL−1, IC50 = 361 (279–438 μg mL−1, IC90 = 467 (398–615 μg mL−1. Accordingly, tyrosol, hydroxytyrosol, trans-coniferyl alcohol and oleuropein were selected as reference test compounds, but their contributions to the observed activity of the olive pomace extract were insignificant. The established test system proved to be a fast and efficient assay for identifying anti-cryptosporidial activities in biological waste material and comparison with selected reference compounds.

  12. In vitro inhibitory effects of plant-derived by-products against Cryptosporidium parvum

    Science.gov (United States)

    Teichmann, Klaus; Kuliberda, Maxime; Schatzmayr, Gerd; Pacher, Thomas; Zitterl-Eglseer, Karin; Joachim, Anja; Hadacek, Franz

    2016-01-01

    Disposal of organic plant wastes and by-products from the food or pharmaceutical industries usually involves high costs. In the present study, 42 samples derived from such by-products were screened in vitro against Cryptosporidium parvum, a protozoan parasite that may contaminate drinking water and cause diarrhoea. The novel bioassay was previously established in the microtitre plate format. Human ileocaecal adenocarcinoma (HCT-8) cell cultures were seeded with C. parvum oocysts and parasite development was monitored by an indirect fluorescent antibody technique (IFAT) and microscopic assessment for clusters of secondary infection (CSI). Minimum inhibitory concentrations (MICs) and potential detrimental effects on the host cells were determined. An ethanolic extract from olive (Olea europaea) pomace, after oil pressing and phenol recovery, reproducibly inhibited C. parvum development (MIC = 250–500 μg mL−1, IC50 = 361 (279–438) μg mL−1, IC90 = 467 (398–615) μg mL−1). Accordingly, tyrosol, hydroxytyrosol, trans-coniferyl alcohol and oleuropein were selected as reference test compounds, but their contributions to the observed activity of the olive pomace extract were insignificant. The established test system proved to be a fast and efficient assay for identifying anti-cryptosporidial activities in biological waste material and comparison with selected reference compounds. PMID:27627637

  13. Inhibitory effect of Hydrex anti-scalant on calcium scale deposition from seawater under multiple-effect distillers' conditions

    Directory of Open Access Journals (Sweden)

    Aiman Eid Al-Rawajfeh

    2015-09-01

    Full Text Available In this work, the inhibitory effect of a commercial anti-scalant (Veolia Hydrex® 9209 on the calcium minerals of carbonate, sulfate and hydrocalumite (Ca/Al clay deposition from seawater has been investigated. Different concentration factors and anti-scalant doses were studied by analyzing the water hardness and turbidity. The inhibitory effect of the investigated anti-scalant was efficient even at lower concentrations. The percentage inhibition decreases with increasing the temperature and increases with increasing the dose/amount of the anti-scalant. The carbonate scale inhibition was >99% and 98–99% at 50 and 70 °C, respectively. The percentage inhibition of sulfate from hemihydrate was ranged from 80% to 87% for 2 and 8 ppm anti-scalant at 50 °C. The inhibition of Ca/Al hydrocalumite deposition increases from 70% to 90% upon increasing the dose from 3 to 5 ppm, respectively. A recommended useful dose of antiscalant for seawater is 5 ppm.

  14. Promotion and computation of inhibitory effect on tyrosinase activity of herbal cream by incorporating indigenous medicinal plants.

    Science.gov (United States)

    Sahu, Ram Kumar; Roy, Amit; Dwivedi, Jaya; Jha, Arvind Kumar

    2014-01-01

    Herbal cream imparts a chief role in regulating melanin production of skin. The phytoconstituents present in herbal cream impact biological functions of skin and contribute nutrients required for the healthy skin. In the present study, it was envisaged to prepare three batches of herbal cream (HC1, HC2 and HC3) containing ethanol extracts of Emblica officinalis (fruits), Daucus carota (root), Mangifera indica (leaves), Mentha arvensis (leaves), Terminalia arjuna (bark) and Cucumis sativus (fruits) and investigated the prepared cream for inhibitory effect on tyrosinase activity. The herbal cream was formulated by incorporating different ratio of extracts, by using cream base. Each formulation HC1, HC2 and HC3 were segregated into three different formulations (HC1.1, HC1.2, HC1.3, HC2.1, HC2.2, HC2.3, HC3.1, HC3.2 and HC3.3) by incorporating increasing ratio of extract in formulation. The HC3.2 cream produces highest tyrosinase inhibitory effect 65.23 +/- 0.07%, while the HC2.1 exhibited minimum tyrosinase inhibitory effect 26.19 +/- 0.08% compared to other prepared cream. Comparison of the inhibitory activity of the formulations demonstrated that the rank order was HC3.2 > HC3.3 > HC1.2 > HC1.3 > HC3.1 > HC1.1 > HC2.3 > HC2.2 > HC2.1. It has been observed from the result that the formulations of antityrosinase activity were not concentrate dependent. This finding suggests that decrease in antityrosinase activity of HC1 and HC3 might be considering that the incompatibility of the higher extract content with the base of cream. The HC3 produce the maximum inhibitory effects on tyrosinase activity might be due to higher level of polyphenol and flavonoids present in extracts.

  15. A cyclohexanecarboxamide derivative with inhibitory effects on Schistosoma mansoni cercarial serine protease and penetration of mice skin by the parasite.

    Science.gov (United States)

    Bahgat, Mahmoud; Aboul-Enein, Mohamed N; El Azzouny, Aida A; Maghraby, Amany; Ruppel, Andreas; Soliman, Wael M

    2009-01-01

    A cyclohexanecarboxamide derivative, N-phenyl-N-[1-(piperidine-1-carbonyl)cyclohexyl] benzamide (MNRC-5), was evaluated for its inhibitory effects on Schistosoma mansoni cercarial serine protease activity and cercarial penetration. MNRC-5 exerted an inhibitory effect on S. mansoni cercarial serine protease at serial concentrations of the specific chromogenic substrate Boc-Val-Leu-Gly-Arg-PNA for such enzyme family and the inhibitory coefficient (Ki) value was deduced. Moreover, topical treatment of mice tails with the most potent inhibitory concentration of MNRC-5 formulated in jojoba oil successfully blocked cercarial penetration as demonstrated by a significant reduction (75%; p jojoba oil base containing no MNRC-5. In addition, the IgM and IgG reactivities to crude S. mansoni cercarial, worm and egg antigens were generally lower in sera from treated infected mice than untreated infected mice. In conclusion, we report on a new serine protease inhibitor capable for blocking penetration of host skin by S. mansoni cercariae as measured by lowering worm burden and decrease in the levels of both IgM and IgG towards different bilharzial antigens upon topical treatment.

  16. Effect of chronic restraint stress on inhibitory gating in the auditory cortex of rats.

    Science.gov (United States)

    Ma, Lanlan; Li, Wai; Li, Sibin; Wang, Xuejiao; Qin, Ling

    2017-05-01

    A fundamental adaptive mechanism of auditory function is inhibitory gating (IG), which refers to the attenuation of neural responses to repeated sound stimuli. IG is drastically impaired in individuals with emotional and cognitive impairments (i.e. posttraumatic stress disorder). The objective of this study was to test whether chronic stress impairs the IG of the auditory cortex (AC). We used the standard two-tone stimulus paradigm and examined the parametric qualities of IG in the AC of rats by recording the electrophysiological signals of a single-unit and local field potential (LFP) simultaneously. The main results of this study were that most of the AC neurons showed a weaker response to the second tone than to the first tone, reflecting an IG of the repeated input. A fast negative wave of LFP showed consistent IG across the sampled AC sites, whereas a slow positive wave of LFP had less IG effect. IG was diminished following chronic restraint stress at both, the single-unit and LFP level, due to the increase in response to the second tone. This study provided new evidence that chronic stress disrupts the physiological function of the AC. Lay Summary The effects of chronic stress on IG were investigated by recording both, single-unit spike and LFP activities, in the AC of rats. In normal rats, most of the single-unit and N25 LFP activities in the AC showed an IG effect. IG was diminished following chronic restraint stress at both, the single-unit and LFP level.

  17. Inhibitory Effect of Sodium Selenite on Microsatellite Instability of RER+ Colorectal Cancer Cells

    Institute of Scientific and Technical Information of China (English)

    2001-01-01

    Objective Investigation of the effects of sodium selenite on genetic instability of human tumor cells via its role in alteration of microsatellite sequence(MS) of RER+ (replication error) colon cancer cell line. Methods RER+ and RER- human colon cancer cell lines, RKO or SW480, were used as hosts for lipofection with pcmv-car in which a foreign(CA)14 repeat was inserted in the coding sequence of LacZ reporter gene, resulting in misreading LacZ frame. Any mutation which makes the base number of (CA)14 tract to be 3-fold will resume the normal reading frame of the reporter gene, and thus lead to expression and production of bioactive β-galactosidase. To test the effect of selenite on MI(microsatellite instability) of tumor cells, a series of concentrations of selenite were administered in cell culture in vitro. Variable expression of bioactive β-galactosidase of transfectant cells resulted from selenite administration was measured by A reading at λ410 after X-gal staining; Results Mutations of the exogenous(CA)14 developed and maintained in pcmv-car transfectant RKO cells but not in SW480 cells. It was found that blue cell frequency of RKO transfectant cells was markedly reduced after incubation of cells with 5 μmol/L of selenite for 5 days, at which concentration it was not toxic to cell growth. However, selenite at lower concentration of 1μmol/L didn′t exhibit suppression of blue cell rate until cell′s exposure to it for a longer period up to 5 weeks or more. Conclusion Our data showed that selenite displayed inhibitory effect on MI of human cancer cells and thus demonstrated its beneficial role in stabilization of human genomic DNA.

  18. Inhibitory effect of oxytocin on accelerated colonic motility induced by water-avoidance stress in rats.

    Science.gov (United States)

    Matsunaga, M; Konagaya, T; Nogimori, T; Yoneda, M; Kasugai, K; Ohira, H; Kaneko, H

    2009-08-01

    Recent studies have indicated that brain and gut activities are interrelated and exposure to several stressors, such as water-avoidance stress, stimulates the motor function of the gut through corticotropin-releasing factor (CRF)-signalling pathways in the brain. Central oxytocin is known to attenuate stress responses, including CRF expression in the brain. Here, we examined whether central oxytocin attenuated the acceleration of colonic motility induced by water-avoidance stress. A force transducer was attached to the distal colon of male rat, and the colonic motility and faecal pellet output were recorded while the rats were exposed to water-avoidance stress. Intracerebroventricular (i.c.v.) injections of oxytocin (5, 50 and 500 pmol) and the oxytocin receptor antagonist tocinoic acid (25 microg) were administered before exposure to water-avoidance stress, and the effect of oxytocin on colonic motor function was determined. Centrally administered oxytocin inhibited the accelerated colonic motility induced by water-avoidance stress. The effective dose ranged between 5 and 50 pmol on i.c.v. injection. Oxytocin also decreased the number of CRF-positive cells in the paraventricular nucleus and corticosterone release. The inhibitory effect of oxytocin on accelerated colonic motility was blocked by pretreatment with oxytocin receptor antagonist. Furthermore, centrally administered tocinoic acid enhanced the acceleration of colonic motility. These results suggested that endogenous central oxytocin may contribute to the regulation of colonic function and inhibit the brain CRF-signalling pathways targeting the gut, resulting in the inhibition of stress-induced colonic contractions.

  19. Inhibitory effects of Satureja hortensis L. essential oil on growth and aflatoxin production by Aspergillus parasiticus.

    Science.gov (United States)

    Razzaghi-Abyaneh, Mehdi; Shams-Ghahfarokhi, Masoomeh; Yoshinari, Tomoya; Rezaee, Mohammad-Bagher; Jaimand, Kamkar; Nagasawa, Hiromichi; Sakuda, Shohei

    2008-04-30

    In an effort to screen the essential oils of some Iranian medicinal plants for novel aflatoxin (AF) inhibitors, Satureja hortensis L. was found as a potent inhibitor of aflatoxins B1 (AFB1) and G1(AFG1) production by Aspergillus parasiticus NRRL 2999. Fungal growth was also inhibited in a dose-dependent manner. Separation of the plant inhibitory substance(s) was achieved using initial fractionation of its effective part (leaf essential oil; LEO) by silica gel column chromatography and further separation by reverse phase-high performance liquid chromatography (RP-HPLC). These substances were finally identified as carvacrol and thymol, based on the interpretation of 1H and 13C NMR spectra. Microbioassay (MBA) on cell culture microplates contained potato-dextrose broth (PDB) medium (4 days at 28 degrees C) and subsequent analysis of cultures with HPLC technique revealed that both carvacrol and thymol were able to effectively inhibit fungal growth, AFB1 and AFG1 production in a dose-dependent manner at all two-fold concentrations from 0.041 to 1.32 mM. The IC50 values for growth inhibition were calculated as 0.79 and 0.86 mM for carvacrol and thymol, while for AFB1 and AFG1, it was reported as 0.50 and 0.06 mM for carvacrol and 0.69 and 0.55 mM for thymol. The results obtained in this study clearly show a new biological activity for S. hortensis L. as strong inhibition of aflatoxin production by A. parasiticus. Carvacrol and thymol, the effective constituents of S. hortensis L., may be useful to control aflatoxin contamination of susceptible crops in the field.

  20. The Inhibitory Effect of Chinese Tea and Its Polyphenols on in vitro and in vivo N—Nitrosation

    Institute of Scientific and Technical Information of China (English)

    WUYong-Ning; WANGHuai-Zhou; 等

    1993-01-01

    The objective of this study is to evaluate the possible role of Chinese tea as a natrural inhibitor of N-nitrosation,and to compare the relative inhibitory potency of various kinds of Chinese tea in vitro and in vivo.Studies on the inhibitory effect of 145 samples of Chinese tea on the formation of N-nitrosomorpholine(NMOR)showed that the inhibitory potency of the 7 types of Chinese tea differed greatly,the average blocking rate of green ta(89.04%,n=60),crush,tear,and curl(CTC)black tea(86.99%,n=13),brick tea(85.40%,n=7),fasmine tea (84.99%,n=21),Oolong tea(82.37%,n=9),sun-dried tea(61.99%,n=13)and Chinese Gongfu black tea(54.98%,n=22),wre ositively correlated with thir polyphenols contents.The inhibitory effect of greeen tea and black tea on endogenous N-nitrosation was also confirmed in 3 human volunteer experiments.Drinking tea after meal had a greatr effect than drinking it before meal.It is concluded that Chinese tea can exert a relatively strong inhibitory potency for N-Nitroso compounds(NOC)formation both in vitro and in humans,and the active constitutents may be related to their polyphenols contents,especially the tea catechin derivatives.The results also demonstrated that the amounts of NMOR formed in vitro depended on the molecular structure of tea catechin derivatives and their molar rations to nitrite.

  1. Comparison of Inhibitory Effect of Gripe Mixture and Caraway Mixture on Acetylcholine Induced Spasm in Rat jejunum

    Directory of Open Access Journals (Sweden)

    F. Zeraati

    2003-10-01

    Full Text Available In comparison of effects of various drugs with the same indications produced by different companies or comparing drugs manufactured in Iran with their foreign counterparts may result in producing drugs with higher qualities in our country. In this study the spasmolithic effect of two herbal drugs , gripe mixture and caraway mixture , that are prescribed as spasmolithic and carminative in infants were compared. 2 cm of rat jejunum was placed in a organ bath containing tyrode solution (37 C , 100% O2 . The jejunum was contracted because of acetylcholine (1 ml. when the muscle contraction reached the plateau the different volumes of drug were added to the organ bath. The inhibitory effect of drug indicated by physiograph , the intestine was washed two times. When the intestine reached the basal tonicity , the different volumes of second drug were tested. The results were compared using paired t.test The results show that both drugs inhibit the spasm induced by acetylcholine in rat jejunum . This inhibitory effect was dose dependent. The caraway mixture showed a higher effect in comparison with gripe mixture (P<0.05. The caraway mixture has a higher inhibitory effect on acetylcholine induced spasm in rat jejunum . It seems that it has the same effect on human.

  2. Inhibitory effect of putranjivain A on allergic inflammation through suppression of mast cell activation

    Energy Technology Data Exchange (ETDEWEB)

    Kim, Hui-Hun; Park, Seung-Bin; Lee, Soyoung [CMRI, Department of Pharmacology, School of Medicine, Kyungpook National University, Daegu 700-422 (Korea, Republic of); Kwon, Taeg Kyu [Department of Immunology, School of Medicine, Keimyung University, Daegu 704-701 (Korea, Republic of); Shin, Tae-Yong [College of Pharmacy, Woosuk University, Jeonju 565-701 (Korea, Republic of); Park, Pil-Hoon; Lee, Seung-Ho [College of Pharmacy, Youngnam University, Kyungsan 712-749 (Korea, Republic of); Kim, Sang-Hyun, E-mail: shkim72@knu.ac.kr [CMRI, Department of Pharmacology, School of Medicine, Kyungpook National University, Daegu 700-422 (Korea, Republic of)

    2014-02-01

    A great number of people are suffering from allergic inflammatory disease such as asthma, atopic dermatitis, and sinusitis. Therefore discovery of drugs for the treatment of these diseases is an important subject in human health. Putranjivain A (PJA), member of ellagitannin, is known to possess beneficial effects including anti-cancer and anti-viral activities. The aim of the present study was to elucidate whether PJA modulates the allergic inflammatory reaction and to study its possible mechanisms of action using mast cell-based in vitro and in vivo models. The study was performed in anaphylaxis mouse model and cultured mast cells. PJA inhibited the expression of pro-inflammatory cytokines in immunoglobulin E-stimulated mast cells. PJA reduced this expression by inhibiting nuclear factor (NF)-κB and nuclear factor of activated T cell. The oral administration of PJA reduced systemic and cutaneous anaphylaxis, the release of serum histamine, and the expression of the histamine H{sub 1} receptor. In addition, PJA attenuated the activation of mast cells. PJA inhibited the release of histamine from various types of mast cells by the suppression of intracellular calcium. The inhibitory activity of PJA on the allergic reaction was similar to that of disodium cromoglycate, a known anti-allergic drug. These results suggest that PJA can facilitate the prevention or treatment of allergic inflammatory diseases mediated by mast cells. - Highlights: • PJA reduced the degranulation of mast cells. • PJA inhibited the production of inflammatory cytokines. • The effect of PJA on allergic reaction was comparable to the DSCG. • PJA might be a candidate for the treatment of allergic inflammatory diseases.

  3. In vitro and in vivo assessment of inhibitory effect of stevioside on pro-inflammatory cytokines

    Science.gov (United States)

    Noosud, Jatuporn; Lailerd, Narissara; Kayan, Autchara; Boonkaewwan, Chaiwat

    2017-01-01

    Objective: Stevioside is a natural non-caloric sweetener which has been reported to have anti-inflammatory activity. The aim of the present study was to examine in vitro and in vivo effects of stevioside on rats plasma levels of tumor necrosis factor- α (TNF-α), interleukin-1β (IL-1β), TNF-α and IL-1β release from lipopolysaccharide(LPS)-stimulated rat peripheral blood mononuclear cells (PBMCs). Materials and Methods: Male wistar rats weighing between 170-220 g were given stevioside (0, 500 and 1000 mg/kg BW/day) for 6 weeks. Mononuclear cells were separated from peripheral blood samples. TNF-α and IL-1β levels in plasma and the release of TNF-α and IL-1β from PBMCs were determined using rat enzyme-linked immunosorbent assay (ELISA) kits. Results: Plasma levels of TNF-α and IL-1β were found to be non-detectable in control and groups treated with 500 and 1000 mg/kg of stevioside. Regarding TNF-α release from LPS-stimulated PBMCs, rats that were orally fed with 500 and 1000 mg/kg of stevioside were significantly different (p<0.05) from those in LPS-treated control group (186.8+18.6 and 151.4 + 15.4 vs 248.6+21.4 pg/ml). Additionally, IL-1β levels in rats treated with 500 and 1000 mg/kg of stevioside were significantly different (p<0.05) from those in LPS-treated control group (220.0+12.1 and 158.1 + 22.6 vs 294.4+16.1 pg/ml). Conclusion: Consumption of stevioside has an inhibitory effect on the release of TNF-α and IL-1β from LPS-stimulated PBMCs in rats.

  4. Interferon Regulatory Factor-1 Exerts Inhibitory Effect on Neointimal Formation after Vascular Injury

    Institute of Scientific and Technical Information of China (English)

    Zhen Li; Zhong-gao Wang; Ce Bian; Xiao-dong Chen; Jian-wen Li; Xiu Chen; Bing Han; Gao-feng Hou; Jian Chu; Qi Cui

    2009-01-01

    To investigate the effect of interferon regulatory factors (IRFs) on neointimal formation after vascular injury in the mouse, and its possible mechanism.Methods Vascular injury was induced by polyethylene cuff placement around the left femoral artery of IRF-1-deficient mice and C57BL/6J mice. The mRNA expressions of IRF-1, IRF-2, angiotensin Ⅱ type 2 (AT) receptor, interleukin-1β converting enzyme (ICE), inducible nitric oxide synthase (iNOS) were detected by RT-PCR and immunohistochemical staining.Results Neointimal formation after vascular injury was significantly greater in IRF-1-deficient mice than that in C57BL/6J mice (P<0.05). In contrast, TUNEL-positive nuclei to total nuclei in the neointima and media in vascular smooth muscle cell (VSMC) in the injured artery significantly attenuated in IRF-1-deficient mice compared to C57BL/6J mice (P<0.05). The expressions of AT2 receptor as well as pro-apoptotic genes such as ICE and iNOS in C57BL/6J mice were up-regulated in response to vascular injury, but this upregulation was attenuated in IRF-1-deficient mice.Conclusions Our results suggest that IRF-1 induces VSMC apoptosis and inhibits neointimal formation after vascular injury at least partly due to the upregulation of AT2 receptor, ICE and iNOS expressions. These results indicate that IRF-1 exerts an inhibitory effect on neointimal formation through the induction of apoptosis inVSMCs.

  5. An evaluation of the inhibitory effects against rotavirus infection of edible plant extracts

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    Knipping Karen

    2012-07-01

    Full Text Available Abstract Background Rotaviruses are the single most important cause of severe diarrhea in young children worldwide. The developments of specific, potent and accessible antiviral treatments that restrain rotavirus infection remain important to control rotavirus disease. Methods 150 plant extracts with nutritional applications were screened in vitro on MA-104 cells for their antiviral activity against rhesus rotavirus (RRV. One extract (Aspalathus linearis (Burm.f. R.Dahlgren was also tested for its effect on the loss of transepithelial resistance (TER of Caco-2 cells caused by simian rotavirus (SA-11 infection. Results Aqueous extracts of Nelumbo nucifera Gaertn. fruit, Urtica dioica L. root, Aspalathus linearis (Burm.f. R.Dahlgren leaves, Glycyrrhiza glabra L. root and Olea europaea L. leaves were found to have strong significant antiviral activity with a 50% inhibitory concentration (IC50 Glycyrrhiza glabra was found to have the strongest antiviral activity (IC50 46 μM, followed by luteolin and vitexin from Aspalathus linearis (IC50 respectively 116 μM and 129 μM and apigenin-7-O-glucoside from Melissa officinalis (IC50 150 μM. A combination of Glycyrrhiza glabra L. + Nelumbo nucifera Gaertn. and Urtica dioica L. + Nelumbo nucifera Gaertn. showed synergy in their anti-viral activities. Aspalathus linearis (Burm.f. R.Dahlgren showed no positive effect on the maintenance of the TER. Conclusions These results indicate that nutritional intervention with extracts of Nelumbo nucifera Gaertn., Aspalathus linearis (Burm.f. R.Dahlgren, Urtica dioica L., Glycyrrhiza glabra L. and Olea europaea L. might be useful in the treatment of diarrhea caused by rotavirus infection.

  6. Inhibitory effect of interferon gamma on frequency of Ehrlichia canis-infected cells in vitro.

    Science.gov (United States)

    Tajima, Tomoko; Wada, Makoto

    2013-12-15

    Ehrlichia canis is an obligate intracellular bacterium that infects the macrophage-monocyte cells of dogs, causing canine monocytic ehrlichiosis. Interferon-γ (IFN-γ), along with other cytokines, mediates the immune response to such intracellular bacterial invasions. To determine the role of IFN-γ in the immunity of dogs to E. canis infection, peripheral blood mononuclear cells (PBMC) and white blood cells (WBC) were collected from E. canis-infected dogs and added to a culture of E. canis in DH82 cells. The number of E. canis inclusion-positive cells was significantly reduced in cultures containing PBMC and WBC from E. canis-infected dogs compared to uninfected dogs. However, this resistance was inhibited by the addition of an anti-dog IFN-γ antibody. Resistance was also observed when PBMC were added to the Cell Culture Inserts, which prohibited contact of PBMC to DH82 cells, while allowed the diffusion of soluble cell products. The results of this study indicate that resistance was not dependent on cell to cell contact, but was associated with soluble cell products, such as IFN-γ. The addition of recombinant canine IFN-γ to the E. canis culture also reduced the number of infected cells. A commercial recombinant canine IFN-γ, which is sold in Japan, was also effective at reducing E. canis-infected cell number. These results indicate that IFN-γ has an inhibitory effect on the frequency of E. canis-infected cells in vitro and that contact between effector and target cells is not necessary for the resistance.

  7. Inhibitory effects of cortisone and hydrocortisone on human Kv1.5 channel currents.

    Science.gov (United States)

    Yu, Jing; Park, Mi-Hyeong; Jo, Su-Hyun

    2015-01-05

    Glucocorticoids are the primary hormones that respond to stress and protect organisms from dangerous situations. The glucocorticoids hydrocortisone and its dormant form, cortisone, affect the cardiovascular system with changes such as increased blood pressure and cardioprotection. Kv1.5 channels play a critical role in the maintenance of cellular membrane potential and are widely expressed in pancreatic β-cells, neurons, myocytes, and smooth muscle cells of the pulmonary vasculature. We examined the electrophysiological effects of both cortisone and hydrocortisone on human Kv1.5 channels expressed in Xenopus oocytes using a two-microelectrode voltage clamp technique. Both cortisone and hydrocortisone rapidly and irreversibly suppressed the amplitude of Kv1.5 channel current with IC50 values of 50.2±4.2μM and 33.4±3.2μM, respectively, while sustained the current trace shape of Kv1.5 current. The inhibitory effect of cortisone on Kv1.5 decreased progressively from -10mV to +30mV, while hydrocortisone׳s inhibition of the channel did not change across the same voltage range. Both cortisone and hydrocortisone blocked Kv1.5 channel currents in a non-use-dependent manner and neither altered the channel׳s steady-state activation or inactivation curves. These results show that cortisone and hydrocortisone inhibited Kv1.5 channel currents differently, and that Kv1.5 channels were more sensitive to hydrocortisone than to cortisone. Copyright © 2014 Elsevier B.V. All rights reserved.

  8. Inhibitory effect of zinc oxide nanoparticles on pseudomonas aeruginosa biofilm formation

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    Mohammad Hassani Sangani

    2015-04-01

    Full Text Available Objective(s: Bacterial biofilm formation causes many persistent and chronic infections. The matrix protects biofilm bacteria from exposure to innate immune defenses and antibiotic treatments. The purpose of this study was to evaluate the biofilm formation of clinical isolates of Pseudomonas aeruginosa and the activity of zinc oxide nanoparticles (ZnO NPs on biofilm. Materials and Methods: After collecting bacteria from clinical samples of hospitalized patients, the ability of organisms were evaluated to create biofilm by tissue culture plate (TCP assay. ZnO NPs were synthesized by sol gel method and the efficacy of different concentrations (50- 350 µg/ml of ZnO NPs was assessed on biofilm formation and also elimination of pre-formed biofilm by using TCP method. Results:The average diameter of synthesized ZnO NPs was 20 nm. The minimum inhibitory concentration of nanoparticles was 150- 158 μg/ml and the minimum bactericidal concentration was higher (325 µg/ml. All 15 clinical isolates of P. aeruginosa were able to produce biofilm. Treating the organisms with nanoparticles at concentrations of 350 μg/ml resulted in more than 94% inhibition in OD reduction%. Molecular analysis showed that the presence of mRNA of pslA gene after treating bacteria with ZnO NPs for 30 minutes. Conclusion: The results showed that ZnO NPs can inhibit the establishment of P. aeruginosa biofilms and have less effective in removing pre-formed biofilm. However the tested nanoparticles exhibited anti-biofilm effect, but mRNA of pslA gene could be still detected in the medium by RT-PCR technique after 30 minutes treatment with ZnO.

  9. Inhibitory effect of aroma on the bitterness of branched-chain amino acid solutions.

    Science.gov (United States)

    Mukai, Junji; Tokuyama, Emi; Ishizaka, Toshihiko; Okada, Sachie; Uchida, Takahiro

    2007-11-01

    Nutritional products for patients with liver failure available on the Japanese market contain many branched-chain amino acids (BCAAs) such as L-leucine, L-isoleucine, and L-valine, which not only have a bitter taste but also strong, unpleasant odours, leading to low palatability. The palatability of these nutritional products can be significantly improved by the addition of flavoured powders containing various kinds of tastants (sucrose, citric acid, etc.) and odourants (fruit, coffee aromas, etc.). The specific effects of the aroma of flavoured powders have not yet been clearly evaluated. In the present article, the inhibitory effect of aroma on the bitterness of BCAA solutions was examined. The bitterness intensity of a BCAA solution at the same concentration as Aminoleban EN was defined as 3.5 (measured by a previously described gustatory sensation method). The bitterness threshold of a BCAA standard solution without added aroma was estimated to be 1.87, while those of BCAA solutions containing green-tea, coffee, apple, vanilla, or strawberry aromas were 2.02, 1.98, 2.35, 2.40 and 2.87, respectively, when evaluated by the probit method. This shows that the addition of an aroma can elevate the bitterness threshold in human volunteers. The green-tea and coffee aromas predominantly evoked bitterness, while the vanilla aroma predominantly evoked sweetness. Apple and strawberry aromas evoked both sweetness and sourness, with the apple aroma having stronger sourness and the strawberry aroma stronger sweetness. Thus, a 'sweet' aroma suppresses the bitterness of BCAA, with coexisting sourness also participating in the bitterness inhibition.

  10. Inhibitory Effect of Endostar on Specific Angiogenesis Induced by Human Hepatocellular Carcinoma

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    Qing Ye

    2015-01-01

    Full Text Available To investigate the effect of endostar on specific angiogenesis induced by human hepatocellular carcinoma, this research systematically elucidated the inhibitory effect on HepG2-induced angiogenesis by endostar from 50 ng/mL to 50000 ng/mL. We employed fluorescence quantitative Boyden chamber analysis, wound-healing assay, flow cytometry examination using a coculture system, quantitative analysis of tube formation, and in vivo Matrigel plug assay induced by HCC conditioned media (HCM and HepG2 compared with normal hepatocyte conditioned media (NCM and L02. Then, we found that endostar as a tumor angiogenesis inhibitor could potently inhibit human umbilical vein endothelial cell (HUVEC migration in response to HCM after four- to six-hour action, inhibit HCM-induced HUVEC migration to the lesion part in a dose-dependent manner between 50 ng/mL and 5000 ng/mL at 24 hours, and reduce HUVEC proliferation in a dose-dependent fashion. Endostar inhibited HepG2-induced tube formation of HUVECs which peaked at 50 ng/mL. In vivo Matrigel plug formation was also significantly reduced by endostar in HepG2 inducing system rather than in L02 inducing system. It could be concluded that, at cell level, endostar inhibited the angiogenesis-related biological behaviors of HUVEC in response to HCC, including migration, adhesion proliferation, and tube formation. At animal level, endostar inhibited the angiogenesis in response to HCC in Matrigel matrix.

  11. Inhibitory Effects of Probiotic Lactobacillus on the Growth of Human Colonic Carcinoma Cell Line HT-29

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    Zhung-Yuan Chen

    2017-01-01

    Full Text Available This study was conducted to investigate the inhibitory effect of Lactobacillus cells and supernatants on the growth of the human colon cancer cell line HT-29. Our study results indicated that the PM153 strain exhibits the best adhesion ability and the highest survival in the gastrointestinal tract simulation experiment. Furthermore, after an 8-h co-culture of PM153 and HT-29 cells, the PM153 strain can induce the secretion of nitric oxide from the HT-29 cells. In addition, after the co-culture of the BCRC17010 strain (109 cfu/mL and HT-29 cells, the Bax/Bcl-2 ratio in the HT-29 cells was 1.19, which showed a significant difference from the other control and LAB groups (p < 0.05, which therefore led to the inference that the BCRC17010 strain exerts a pro-apoptotic effect on the HT-29 cells. Upon co-culture with HT-29 cells for 4, 8 and 12 h, the BCRC14625 strain (109 cfu/mL demonstrated a significant increase in lactate dehydrogenase (LDH activity (p < 0.05, causing harm to the HT-29 cell membrane; further, after an 8-h co-culture with the HT-29 cells, it induced the secretion of nitric oxide (NO from the HT-29 cells. Some lactic acid bacteria (LAB strains have ability to inhibit the growth of the colorectal cancer cell line HT-29 Bax/Bcl-2 pathway or NO production. In summary, we demonstrated that the BCRC17010 strain, good abilities of adhesion and increased LDH release, was the best probiotic potential for inhibition of HT-29 growth amongst the seven LAB strains tested in vitro.

  12. Inhibitory Effect of Progesterone on Inflammatory Factors After Experimental Traumatic Brain Injury

    Institute of Scientific and Technical Information of China (English)

    2007-01-01

    Traumatic brain injury (TBI) is one of the leading causes of morbidity and mortality in young people. Inflammatory cytokines play an important part in the pathophysiology of TBI. Recent studies demonstrate that progesterone significantly reduces cerebral edema and enhances functional recovery from TBI and stroke in several animal models. This study was designed to investigate the inhibitory effect of progesterone on inflammatory response after traumatic brain injury. Methods Progesterone was injected intraperitoneally using rats as a model of traumatic brain injury,and Western blot technique was applied to detect the expression of three inflammation-related factors:nuclear factor kappa B p65 (NFk B p65),glial fibrillary acidic protein (GFAP),and tumor necrosis factor-α (TNF-α). The water content of injured brain was also examined. A neurological severity score was recorded to evaluate the effect of progesterone on neurodeficit recovery. Results NFk B p65,GFAP,and TNF-α were increased in all injured animals. In rats treated with progesterone,the expression level of NFkB p65 and TNF-α were reduced significantly in comparison with vehicle-treated rats. However,progesterone did not alter the expression of GFAP in the injured rats. Progesterone also reduced the water content of injured brain and the lesion volume. In addition,progesterone-treated injured rats showed significant improvements in the Neurological Severity Score test,compared with vehicle-treated ones.Conclusions Progesterone inhibits the inflammatory response after experimental traumatic brain injury and mitigates the severity of brain damage.

  13. Effect of vancomycin minimal inhibitory concentration on the outcome of methicillin-susceptible Staphylococcus aureus endocarditis.

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    Cervera, Carlos; Castañeda, Ximena; de la Maria, Cristina Garcia; del Rio, Ana; Moreno, Asunción; Soy, Dolors; Pericas, Juan Manuel; Falces, Carlos; Armero, Yolanda; Almela, Manel; Ninot, Salvador; Pare, Juan Carlos; Mestres, Carlos A; Gatell, Jose M; Marco, Francesc; Miro, Jose M

    2014-06-01

    Staphylococcus aureus endocarditis has a high mortality rate. Vancomycin minimum inhibitory concentration (MIC) has been shown to affect the outcome of methicillin-resistant S. aureus bacteremia, and recent data point to a similar effect on methicillin-susceptible S. aureus bacteremia. We aimed to evaluate the effect of vancomycin MIC on left-sided S. aureus infective endocarditis (IE) treated with cloxacillin. We analyzed a prospectively collected cohort of patients with IE in a single tertiary-care hospital. Vancomycin, daptomycin, and cloxacillin MIC was determined by E-test. S. aureus strains were categorized as low vancomycin MIC (<1.5 µg/mL) and high vancomycin MIC (≥1.5 µg/mL). The primary endpoint was in-hospital mortality. We analyzed 93 patients with left-sided IE treated with cloxacillin, of whom 53 (57%) had a vancomycin MIC < 1.5 µg/mL and 40 (43%) a vancomycin MIC ≥ 1.5 µg/mL. In-hospital mortality was 30% (n = 16/53) in patients with a low vancomycin MIC and 53% (n = 21/40) in those with a high vancomycin MIC (P = .03). No correlation was found between oxacillin MIC and vancomycin or daptomycin MIC. Logistic regression analysis showed that higher vancomycin MIC increased in-hospital mortality 3-fold (odds ratio, 3.1; 95% confidence interval, 1.2-8.2) after adjustment for age, year of diagnosis, septic complications, and nonseptic complicated endocarditis. Our results indicate that vancomycin MIC could be used to identify a subgroup of patients with methicillin-susceptible S. aureus IE at risk of higher mortality. The worse outcome of staphylococcal infections with a higher vancomycin MIC cannot be explained solely by suboptimal pharmacokinetics of antibiotics. © The Author 2014. Published by Oxford University Press on behalf of the Infectious Diseases Society of America. All rights reserved. For Permissions, please e-mail: journals.permissions@oup.com.

  14. Extracellular vesicles from malignant effusions induce tumor cell migration: inhibitory effect of LMWH tinzaparin.

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    Gamperl, Hans; Plattfaut, Corinna; Freund, Annika; Quecke, Tabea; Theophil, Friederike; Gieseler, Frank

    2016-10-01

    Elevated levels of extracellular vesicles (EVs) have been correlated with inflammatory diseases as well as progressive and metastatic cancer. By presenting tissue factor (TF) on their membrane surface, cellular microparticles (MPs) activate both the coagulation system and cell-signaling pathways such as the PAR/ERK pathway. We have shown before that malignant effusions are a rich source of tumor cell-derived EVs. Here, we used EVs from malignant effusions from three different patients after serial low-speed centrifugation steps as recommended by the ISTH (lsEV). Significant migration of human pancreatic carcinoma cells could be induced by lsEVs and was effectively inhibited by pre-incubation with tinzaparin, a low-molecular-weight heparin. Tinzaparin induced tissue factor pathway inhibitor (TFPI) release from tumor cells, and recombinant TFPI inhibited EV-induced tumor cell migration. EVs also induced ERK phosphorylation, whereas inhibitors of PAR2 and ERK suppressed EV-induced tumor cell migration. LsEVs have been characterized by high-resolution flow cytometry and, after elimination of smaller vesicles including exosomes, by further high-speed centrifugation (hsEV). The remaining population consisting primarily of MPs is indeed the main migration-inducing population with tenase activity. Compared to other LMWHs, tinzaparin is suggested to have high potency to induce TFPI release from epithelial cells. The migration-inhibitory effect of TFPI and the interruption of tumor cell migration by inhibitors of PAR2 and ERK suggest that lsEVs induce tumor cell migration by activating the PAR2 signaling pathway. Tinzaparin might inhibit this process at least partly by inducing the release of TFPI from tumor cells, which blocks PAR-activating TF complexes. The clinical relevance of the results is discussed.

  15. Inhibitory effects of prostaglandin E1 on activation of hepatic stellate cells in rabbits with schistosomiasis

    Institute of Scientific and Technical Information of China (English)

    Wei-Long Zou; Zhen Yang; Yun-Jin Zang; Dong-Jian Li; Zhi-Peng Liang; Zhong-Yang Shen

    2007-01-01

    BACKGROUND:Liver ifbrosis is the result of an imbalance between synthesis and degradation of extracellular matrix proteins of the liver. At the cellular and molecular levels, this progressive process is mainly characterized by activation of hepatic stellate cells (HSCs). Schistosoma japonica is one of the most prevalent causes of liver ifbrosis in China. It is characterized by hepatocyte damage, inlfammation, and chronic parasite egg-induced granuloma formation leading to ifbrosis. This study aimed to investigate the inhibitory effects of prostaglandin E1 (PGE1) on activation of HSCs and the alteration of type Ⅰ and Ⅲ collagen in rabbits with schistosomiasis. The study may promote the clinical application of praziquantel and PGE1 as a combined therapy to reverse hepatic ifbrosis caused by schistosomiasis. METHODS: Rabbits were percutaneously infected with cercaria of S. japonicum. Seven rabbits were subjected to intravenous injections of PGE1 (2.5 μg/kg daily) from days 60 to 120 after infection. The ultrastructural changes in activated HSCs were observed under transmission electron microscopy. The expression ofα-smooth muscle actin (α-SMA) was detected by immunohistochemistry. Fibril-forming collagens were detected by picrosirius staining. RESULTS: Activation of HSCs was a characteristic alteration in schistosome-induced hepatic ifbrosis. The expression of contraction-related α-SMA and the content of collagens were increased. Exogenous PGE1 markedly inhibited the activation of HSCs and reduced the expression of α-SMA around the hepatic sinusoids (P CONCLUSIONS:Activation of HSCs may play a key role in the progress of schistosome-induced hepatic ifbrosis. PGE1 effectively protects rabbit liver from ifbrosis, at least in part by inhibiting the activation of HSCs.

  16. Stimulatory and inhibitory effects of forskolin on adenylate cyclase in rat normal hepatocytes and hepatoma cells.

    Science.gov (United States)

    Miyamoto, K; Sanae, F; Koshiura, R; Matsunaga, T; Takagi, K; Satake, T; Hasegawa, T

    1989-02-01

    Forskolin synergistically potentiated adenosine 3',5'-cyclic monophosphate formation by prostaglandin E1 (PGE1) in rat normal hepatocytes freshly prepared by collagenase digestion and rat ascites hepatoma AH66 cells, but dose-dependently inhibited the accumulation by PGE1 in AH66F cells. Forskolin activated adenylate cyclase in a dose-dependent manner in homogenates of all cell lines. In normal hepatocytes and AH66 cells, simultaneous addition of forskolin and other adenylate cyclase activators [isoproterenol (IPN), PGE1, guanosine 5'-triphosphate sodium salt (GTP), 5'-guanylylimidodiphosphate sodium salt (Gpp (NH)p), NaF, cholera toxin, islet activating protein and MnCl2] gave greater than additive responses. On the other hand, in AH66F cells, the effect of forskolin on adenylate cyclase was hardly influenced by GTP, but forskolin diminished the activities induced by high concentrations of GTP to that by the diterpene alone. Forskolin also significantly inhibited the PGE1-stimulated and the guanine nucleotide binding regulatory protein-stimulated activities. Because AH66F cells were insensitive to IPN, the combination with forskolin and IPN gave similar activity to that obtained with the diterpene alone. The effect of forskolin on the activation by manganese ion was neither synergistic nor inhibitory but was additive in AH66F cells. These results suggest that forskolin promotes the interaction between the stimulatory guanine nucleotide binding regulatory protein and the catalytic unit in normal hepatocytes and AH66 cells, but in AH66F cells forskolin interferes with the coupling of the two components of adenylate cyclase.

  17. Inhibitory effects of Ponciri Fructus on testosterone-induced benign prostatic hyperplasia in rats.

    Science.gov (United States)

    Jeon, Woo-Young; Kim, Ohn Soon; Seo, Chang-Seob; Jin, Seong Eun; Kim, Jung-Ae; Shin, Hyeun-Kyoo; Kim, Yong-Ung; Lee, Mee-Young

    2017-08-03

    Benign prostatic hyperplasia (BPH) is non-cancerous condition of enlargement of the prostate, a common occurrence in older men. The immature fruits of Poncirus trifoliata (L.) Rafinesque (Rutaceae), Ponciri Fructus are widely used in traditional oriental medicine for the therapy of various diseases. However, little is known about the mechanism underlying the pathogenesis of BPH. In the present study, we investigated the protective effects of a Ponciri Fructus extract (PFE) on the development of BPH in a in a rat model of BPH induced by testosterone propionate (TP). Male Sprague Dawley rats were used as a model of BPH after its induction by daily subcutaneous injections of TP/corn oil, for a period of four weeks. PFE was administrated daily 1 h before TP/corn oil injection by oral gavage at a dose level of 200 mg/kg during the 4 weeks of TP/corn oil injections. All rats were sacrificed at the end of the experiment, we measured the relative prostate weight, the levels of testosterone and dihydrotestosterone (DHT), histological changes, activities of antioxidant enzymes (catalase, glutathione peroxidase, glutathione reductase, and superoxide dismutase), and expression of proliferating cell nuclear antigen (PCNA). In addition, we also measured the inhibition (%) of 5α-reductase in the prostatic tissue. Our findings indicate that PFE significantly inhibited the development of BPH; decreased the relative prostate weight, the level of testosterone and DHT in serum and prostatic tissue, prostatic hyperplasia, expression of PCNA, and increased the antioxidant enzymes. Moreover, PFE showed a weak inhibitory activity on 5α-reductase. These results suggest that PFE may be used as a therapeutic agent for BPH via antiproliferative and antioxidant effects.

  18. The effect of Helicobacter pylori eradication on macrophage migration inhibitory factor, C-reactive protein and fetuin-a levels

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    Levent Kebapcilar

    2010-06-01

    Full Text Available OBJECTIVES: To determine the effect of Helicobacter pylori (H. pylori eradication on blood levels of high-sensitivity C-reactive protein (hs-CRP, macrophage migration inhibitory factor and fetuin-A in patients with dyspepsia who are concurrently infected with H. pylori. METHODS: H.pylori infection was diagnosed based on the 14C urea breath test (UBT and histology. Lansoprazole 30 mg twice daily, amoxicillin 1 g twice daily, and clarithromycin 500 mg twice daily were given to all infected patients for 14 days; 14C UBT was then re-measured. In 30 subjects, migration inhibitory factor, fetuin-A and hs-CRP levels were examined before and after the eradication of H. pylori infection and compared to levels in 30 healthy subjects who tested negative for H. pylori infection. RESULTS: Age and sex distribution were comparable between patients and controls. Migration inhibitory factor and hs-CRP levels were higher, and fetuin-A levels were lower, in H. pylori-infected patients (p0.05. CONCLUSION: These findings suggest that H. pylori eradication reduces the levels of pro-inflammatory cytokines such as migration inhibitory factor and hs-CRP and also results in a significant increase in anti-inflammatory markers such as fetuin-A.

  19. The effect of domestication on inhibitory control: wolves and dogs compared.

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    Marshall-Pescini, Sarah; Virányi, Zsófia; Range, Friederike

    2015-01-01

    Inhibitory control i.e. blocking an impulsive or prepotent response in favour of a more appropriate alternative, has been suggested to play an important role in cooperative behaviour. Interestingly, while dogs and wolves show a similar social organization, they differ in their intraspecific cooperation tendencies in that wolves rely more heavily on group coordination in regard to hunting and pup-rearing compared to dogs. Hence, based on the 'canine cooperation' hypothesis wolves should show better inhibitory control than dogs. On the other hand, through the domestication process, dogs may have been selected for cooperative tendencies towards humans and/or a less reactive temperament, which may in turn have affected their inhibitory control abilities. Hence, based on the latter hypothesis, we would expect dogs to show a higher performance in tasks requiring inhibitory control. To test the predictive value of these alternative hypotheses, in the current study two tasks; the 'cylinder task' and the 'detour task', which are designed to assess inhibitory control, were used to evaluate the performance of identically raised pack dogs and wolves. Results from the cylinder task showed a significantly poorer performance in wolves than identically-raised pack dogs (and showed that pack-dogs performed similarly to pet dogs with different training experiences), however contrary results emerged in the detour task, with wolves showing a shorter latency to success and less perseverative behaviour at the fence. Results are discussed in relation to previous studies using these paradigms and in terms of the validity of these two methods in assessing inhibitory control.

  20. The effect of domestication on inhibitory control: wolves and dogs compared.

    Directory of Open Access Journals (Sweden)

    Sarah Marshall-Pescini

    Full Text Available Inhibitory control i.e. blocking an impulsive or prepotent response in favour of a more appropriate alternative, has been suggested to play an important role in cooperative behaviour. Interestingly, while dogs and wolves show a similar social organization, they differ in their intraspecific cooperation tendencies in that wolves rely more heavily on group coordination in regard to hunting and pup-rearing compared to dogs. Hence, based on the 'canine cooperation' hypothesis wolves should show better inhibitory control than dogs. On the other hand, through the domestication process, dogs may have been selected for cooperative tendencies towards humans and/or a less reactive temperament, which may in turn have affected their inhibitory control abilities. Hence, based on the latter hypothesis, we would expect dogs to show a higher performance in tasks requiring inhibitory control. To test the predictive value of these alternative hypotheses, in the current study two tasks; the 'cylinder task' and the 'detour task', which are designed to assess inhibitory control, were used to evaluate the performance of identically raised pack dogs and wolves. Results from the cylinder task showed a significantly poorer performance in wolves than identically-raised pack dogs (and showed that pack-dogs performed similarly to pet dogs with different training experiences, however contrary results emerged in the detour task, with wolves showing a shorter latency to success and less perseverative behaviour at the fence. Results are discussed in relation to previous studies using these paradigms and in terms of the validity of these two methods in assessing inhibitory control.

  1. HIV-1 protease inhibitory effects of some selected plants in Caesalpiniaceae and Papilionaceae families

    Directory of Open Access Journals (Sweden)

    Pranee Rattanasuwan

    2003-07-01

    Full Text Available Fifty-two ethanol and water extracts of the plants in Caesalpiniaceae and Papilionaceae families were screened for their HIV-1 protease (HIV-1 PR inhibitory activities using high performance liquid chromatography (HPLC technique. Among the tested extracts, Cassia garrettiana (wood, water extract showed the most potent inhibitory activity against HIV-1 PR, followed by Cassia garrettiana (wood, EtOH extract and Caesalpinia sappan (wood, EtOH extract with IC50 of 18, 32 and 75 μg/ml, respectively. The isolation of active substances against HIV-1 PR of these two plants will be further investigated.

  2. The inhibitory effect of Penicillium camemberti and Geotruchum candidum on the associated funga of white mould cheese

    DEFF Research Database (Denmark)

    Decker, Marianne; Nielsen, P.V.

    2005-01-01

    The diameter of pinpoint inoculated cheese contaminates (Cladosporium herbarum, Penicillium roqueforti, Penicillium caseifulvum and Penicillium commune), isolated from either the dairy environment or directly from cheese, were inoculated 24 h after inoculation of the secondary starters to simulate...... contamination at the critical point of the salt brine. Pure P. camemberti had the largest inhibitory effect on the C. herbarum contaminant. Adding G. candidum in mixed cultures weakened the inhibitory effect of P. camemberti on C. herbarum. Low levels of G. candidum (10(3) spore/ml) promoted visible growth....... candidum in the mixed cultures seems to decrease the suppressing effect of pour-plated P. camemberti. No correlation of any kind was found in the pour-plated spore concentration totals by the inhibition of the C. herbarum and P. roqueforti contaminants whereas R. caseifulvum and P commune were sensitive...

  3. Inhibitory effects of matrine on electrical signals and amino acid neurotransmitters in hippocampal brain slices

    Institute of Scientific and Technical Information of China (English)

    Xuping Wang; Jiping Chen; Guizhi Zhao; Dan Shou; Xuezhi Hong; Jianmin Zhang

    2009-01-01

    -dose groups were separately injected with 58.5, 39.0, and 19.5 mg/kg matrine via caudal vein, respectively. No intervention was administered to the normal group.MAIN OUTCOME MEASURES: The field potential value in the CA1 region of penicillin-induced rat hippocampal brain slices was analyzed using the evoked field potential technique; chromatography was utilized to determine y-aminobutyric acid and glutamic acid content in the mouse hippocampus.RESULTS: (1) Both 0.1 g/L and 0.05 g/L matrine reduced the number of evoked field potentials in the penicillin-induced rat hippocampal brain slices (P<0.05 or P<0.01). In addition, 0.1 g/L matrine led to a reduction of evoked field potential amplitude (P<0.05). (2) Compared with normal mice,y-aminobutyric levels were dramatically increased at 20 minutes after high-dose matdne treatment (P<0.05). In addition, significantly increased y-aminobutyric acid levels were observed at 40 minutes after medium- and low-dose matrine treatments (P<0.05 or P<0.01). The glutamic acid/V-aminobutyric acid ratio was significantly less at 20 minutes after high-dose matrine treatment compared with the normal mice group (P<0.05).CONCLUSION: Matrine exerts a central inhibitory effect via increased inhibitory neurotransmitter y-aminobutyric acid levels in the hippocampus.

  4. Inhibitory effect of silver diamine fluoride on dentine demineralisation and collagen degradation.

    Science.gov (United States)

    Mei, May L; Ito, L; Cao, Y; Li, Q L; Lo, Edward C M; Chu, C H

    2013-09-01

    To investigate the inhibitory effects of 38% silver diamine fluoride (SDF) on demineralised dentine. Human dentine blocks were demineralised and allocated to four groups: SF, F, S and W. The blocks in group SF received a topical application of 38% SDF solution (253,900ppm Ag, 44,800ppm F), group F received a 10% sodium fluoride solution (44,800ppm F), group S received a 42% silver nitrate solution (253,900ppm Ag) and group W received deionised water (control). They were subjected to pH cycling using demineralisation solution (pH 5) and remineralisation solution (pH 7) for 8 days. The surface morphology, crystal characteristics, lesion depth and collagen matrix degradation of the specimens were investigated by scanning electron microscopy (SEM), X-ray diffraction (XRD), micro-CT testing and spectrophotometry with a hydroxyproline assay. The surface morphology under SEM showed evident demineralisation with exposed collagen in groups S and W, but not in group SF. Clusters of granular spherical grains were observed in the cross-sections of specimens in groups SF and F. XRD revealed precipitates of silver chloride in groups SF and S. The mean lesion depths (±SD) of groups SF, F, S and W were 182 ± 32μm, 204 ± 26μm, 259 ± 42μm and 265 ± 40μm, respectively (SDF, FF and W (p<0.01). The use of 38% SDF inhibited demineralisation and preserved collagen from degradation in demineralised dentine. SDF application positively influences dentine remineralization. Copyright © 2013 Elsevier Ltd. All rights reserved.

  5. The Effects of Excitatory and Inhibitory Social Cues on Cocaine-Seeking Behavior

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    Mark Andrew Smith

    2016-11-01

    Full Text Available Social partners influence the likelihood of using drugs, developing a substance use disorder, and relapse to drug use after a period of abstinence. Preclinical studies report that social cues influence the acquisition of cocaine use, the escalation of cocaine use over time, and the compulsive patterns of cocaine use that emerge during an extended binge. The purpose of this study was to examine the effects of social cues on the reinstatement of cocaine-seeking behavior after a period of abstinence. Male rats were obtained at weaning, assigned to triads (3 rats/cage, reared to adulthood, and implanted with intravenous catheters. Rats from each triad were then assigned to one of three conditions: (1 test rats were trained to self-administer cocaine and were tested for reinstatement, (2 cocaine partners were trained to self-administer cocaine and were predictive of response-contingent cocaine delivery, and (3 abstinent partners were not given access to cocaine and were predictive of extinction. Test rats alternated social partners every 5 days for 20 days such that responding was reinforced with cocaine in the presence of the cocaine partner (S+ for 10 days and not reinforced with cocaine in the presence of the abstinent partner (S- for 10 days. Responding of the test rats was then extinguished over 7 days under isolated conditions. Tests of reinstatement were then conducted in the presence of the cocaine partner and abstinent partner under extinction conditions. Neither social partner reinstated responding relative to that observed on the final day of extinction; however, responding was greater in the presence of the cocaine partner (S+ than the abstinent partner (S- during the reinstatement test. These data fail to demonstrate that a social partner reinstates cocaine-seeking behavior after a period of abstinence, but they do indicate that social partners can serve as either excitatory or inhibitory discriminative stimuli to influence drug

  6. Modelling the inhibitory effect of copper sulfate on the growth of Penicillium expansum and Botrytis cinerea.

    Science.gov (United States)

    Judet-Correia, D; Charpentier, C; Bensoussan, M; Dantigny, P

    2011-11-01

    This study aimed to investigate the effect of copper sulfate (from 0 to 8 mmol kg(-1)) on radial growth rate and lag time of two moulds responsible for vine grapes spoilage: Penicillium expansum strain 25·03 and Botrytis cinerea, strains BC1 and BC2. A new model was developed to describe tailing and shoulders in the inhibition curves. Because of tailing, the minimum inhibitory concentration (MIC), was not defined as the concentration at which no growth was observed, but as the concentration at which the lag time was infinite. The concentrations at which μ = μ(opt)/2, (Cu50), were in the range of 2·2-2·6 mmol kg(-1). Radial growth rate of P. expansum and the reciprocal of the lag time were linearly correlated (r = 0·84). In contrast, in the range 0-4 mmol kg(-1), an inhibition of growth of B. cinerea was observed whereas germination remained unaffected (i.e. the lag time was constant). In the range 4-8 mmol kg(-1) , the radial growth rate of B. cinerea was almost constant (c. 1 mm day(-1)), but germination was inhibited (i.e. the lag time was increased). The MIC values were 4·7 mmol kg(-1) for P. expansum, 8·2 and 7·3 mmol kg(-1) for B. cinerea strain BC1 and BC2, respectively, demonstrating that some isolates of these moulds are resistant to copper. Copper concentrations at 4 mmol kg(-1) would be sufficient to control the development of these isolates, but the toxicity of copper should be extended to other isolates and evaluated in vineyards. © 2011 The Authors. Letters in Applied Microbiology © 2011 The Society for Applied Microbiology.

  7. The Effects of Excitatory and Inhibitory Social Cues on Cocaine-Seeking Behavior

    Science.gov (United States)

    Smith, Mark A.; Zhang, Huailin; Robinson, Andrea M.

    2016-01-01

    Social partners influence the likelihood of using drugs, developing a substance use disorder and relapse to drug use after a period of abstinence. Preclinical studies report that social cues influence the acquisition of cocaine use, the escalation of cocaine use over time, and the compulsive patterns of cocaine use that emerge during an extended binge. The purpose of this study was to examine the effects of social cues on the reinstatement of cocaine-seeking behavior after a period of abstinence. Male rats were obtained at weaning, assigned to triads (three rats/cage), reared to adulthood and implanted with intravenous catheters. Rats from each triad were then assigned to one of three conditions: (1) test rats were trained to self-administer cocaine and were tested for reinstatement; (2) cocaine partners were trained to self-administer cocaine and were predictive of response-contingent cocaine delivery; and (3) abstinent partners were not given access to cocaine and were predictive of extinction. The test rats alternated social partners every 5 days for 20 days such that responding was reinforced with cocaine in the presence of the cocaine partner (S+) for 10 days and not reinforced with cocaine in the presence of the abstinent partner (S−) for 10 days. Responding of the test rats was then extinguished over 7 days under isolated conditions. Tests of reinstatement were then conducted in the presence of the cocaine partner and abstinent partner under extinction conditions. Neither social partner reinstated responding relative to that observed on the final day of extinction; however, responding was greater in the presence of the cocaine partner (S+) than the abstinent partner (S−) during the reinstatement test. These data fail to demonstrate that a social partner reinstates cocaine-seeking behavior after a period of abstinence, but they do indicate that social partners can serve as either excitatory or inhibitory discriminative stimuli to influence drug

  8. Inhibitory Effect of Electroacupuncture on Murine Collagen Arthritis and its Possible Mechanisms

    Directory of Open Access Journals (Sweden)

    Jian-Qiao Fang

    2001-02-01

    Full Text Available The influence of electroacupuncture (EA, a traditional Chinese medical treatment, on type Ⅱ collagen-induced arthritis (CIA was examined in DBA/1J mice in vivo. Mice were immunized intradermally twice at the 3-week interval with bovine type Ⅱ collagen(C Ⅱ. EA stimulation, begun on the 21 simultaneously with the second immunization, was applied at the acupoint equivalent to GV4 three times a week for 3 weeks. The results showed that EA delayed the onset, attenuated the severity of arthritis, and reduced the anti-collagen antibody level. Furthermore, we investigated the impact of EA on the productions of endogenous (IL-1 beta and prostaglandin E2 (PGE2, and the levels of IL-1 beta mRNA in splenocytes and synovial tissues from C Ⅱ immunized mice on the 45 and cyclooxygenase-2 (COX-2 mRNA in lipopolysaccharide (LPS-stimulated macrophages of normal mice by using reverse transcriptase-polymerase chain reaction (RT-PCR. EA stimulation significant inhibited the concentrations of splenic endogenous IL-1 beta and serum PGE2. The expression of IL-1 beta mRNA in spleen cells was obviously down-regulated and that in synovial tissues was modestly affected by EA. COX-2 mRNA was highly expressed in cultured peritoneal macrophages when stimulated with LPS. Previous treatment with EA also reduced LPS-stimulated induction of COX-2 mRNA. These data suggest that EA has an inhibitory effect on murine CIA, and the partial mechanism of its therapeutic result may be attributed to inhibiting the productions of IL-1 beta and PGE2 by suppression the IL-1 beta and COX-2 gene activations.

  9. Inhibitory Effect of Bridged Nucleosides on Thermus aquaticus DNA Polymerase and Insight into the Binding Interactions.

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    Sung-Kun Kim

    Full Text Available Modified nucleosides have the potential to inhibit DNA polymerases for the treatment of viral infections and cancer. With the hope of developing potent drug candidates by the modification of the 2',4'-position of the ribose with the inclusion of a bridge, efforts were focused on the inhibition of Taq DNA polymerase using quantitative real time PCR, and the results revealed the significant inhibitory effects of 2',4'-bridged thymidine nucleoside on the polymerase. Study on the mode of inhibition revealed the competitive mechanism with which the 2',4'-bridged thymidine operates. With a Ki value of 9.7 ± 1.1 μM, the 2',4'-bridged thymidine proved to be a very promising inhibitor. Additionally, docking analysis showed that all the nucleosides including 2',4'-bridged thymidine were able to dock in the active site, indicating that the substrate analogs reflect a structural complementarity to the enzyme active site. The analysis also provided evidence that Asp610 was a key binding site for 2',4'-bridged thymidine. Molecular dynamics (MD simulations were performed to further understand the conformational variations of the binding. The root-mean-square deviation (RMSD values for the peptide backbone of the enzyme and the nitrogenous base of the inhibitor stabilized within 0.8 and 0.2 ns, respectively. Furthermore, the MD analysis indicates substantial conformational change in the ligand (inhibitor as the nitrogenous base rotated anticlockwise with respect to the sugar moiety, complemented by the formation of several new hydrogen bonds where Arg587 served as a pivot axis for binding formation. In conclusion, the active site inhibition of Taq DNA polymerase by 2',4'-bridged thymidine suggests the potential of bridged nucleosides as drug candidates.

  10. Inhibitory effects of Tripterygium wilfordii multiglycoside on benign prostatic hyperplasia in rats.

    Science.gov (United States)

    Shen, Hai-Nan; Xu, Yuan; Jiang, Zhen-Zhou; Huang, Xin; Zhang, Lu-Yong; Wang, Tao

    2015-06-01

    The present study was designed to evaluate the inhibitory effects of Tripterygium wilfordii multiglycoside (GTW) against testosterone-induced benign prostatic hyperplasia (BPH) in rats. A total of 45 rats were randomly divided into five groups: Group I, vehicle control group (sham-operated and treated with vehicle); Group II, BPH group; Group III, BPH rats treated with finasteride at a dose of 5 mg·kg(-1); and Groups IV and V, BPH rats treated with GTW at dose levels of 10 and 20 mg·kg(-1), respectively. The drugs were administered orally once a day for 14 days. Prostate weight, prostatic index, and the testosterone and dihydrotestosterone (DHT) levels in serum and prostate, and the serum prostate specific antigen (PSA) levels were measured; prostate tissues were taken for histopathological examination; and serum biochemical analysis was also performed. The BPH rats displayed an increase in prostate weight, prostatic index with increased testosterone and DHT levels in both the serum and prostate, and increased serum PSA levels. GTW treatment at both doses resulted in significant reductions in prostate weight, prostatic index, testosterone and DHT levels in both the serum and prostate, and serum PSA levels, compared with BPH group. Histopathological examination also indicated that GTW treatment at both doses inhibited testosterone-induced prostatic hyperplasia. Serum biochemical analysis showed that the liver and renal functions were normal. In conclusion, GTW inhibited testosterone-induced prostatic hyperplasia in rats, without host toxicity, providing a basis for the development of GTW as a novel therapy for BPH.

  11. Cytotoxic and growth inhibitory effects of the methanol extract Struchium sparganophora Ktze (Asteraceae leaves

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    B A Ayinde

    2010-01-01

    Full Text Available Background: Global research into medicinal plants used in treating tumor-related ailments has become imperative due to the emergence of various forms of cancer diseases. Usually consumed as a vegetable, Struchium sparganophora is indicated in traditional herbal medicine as one of the plants used in treating tumor-related ailments. Materials and Methods: This claim was examined using bench-top assay methods involving the cytotoxicity of the methanol extract of the leaves to tadpoles of Raniceps ranninus at 10, 20, 40 and 80 μg/ml. Also, the growth inhibitory effects of the extract on guinea corn radicle at 0.5, 1.0, 2 and 4 mg/ml in addition to evaluation of the phytochemical constituents of the leaves was performed. After 24 h, the crude extract and the chloroform fraction produced the highest cytotoxicity of 96.67 ± 4.71%, each at a concentration of 80 μg/ml, while the aqueous fraction produced 100% cytotoxicity at a concentration of 20 μg/ml. Results: The crude extract had an LC50 of 26 μg/ml, the chloroform fraction had 6.25 while the aqueous fraction had 5 μg/ml. On the inhibition of the guinea corn radicle growth, after 96 h, the controls had an average length of 67.81 ± 2.6 mm, whereas the seeds treated with 4 mg/ml of the crude extract had an average length of 35.83 ±1.75 mm, indicating 47.81% reduction in length. At the same concentration, the chloroform and the aqueous fractions showed 32.51 and 43.81% inhibitions. The plant material was observed to contain alkaloids, tannins, saponins and flavonoids, with no traces of anthracene derivatives. Conclusion: The results suggest the probable use of the plant in preparing recipes for tumor-related ailments.

  12. Phenolic acids in some cereal grains and their inhibitory effect on starch liquefaction and saccharification.

    Science.gov (United States)

    Kandil, Amin; Li, Jihong; Vasanthan, Thava; Bressler, David C

    2012-08-29

    The presence of phenolic acids in cereal grain is thought to influence starch hydrolysis during liquefaction and saccharification of grain flours in the bioethanol industry. As a basis for remodeling starch hydrolysis systems and understanding inhibition mechanisms, the composition and concentration of phenolic acids in whole grain flours of triticale, wheat, barley, and corn were analyzed by high-performance liquid chromatography. The total phenolic acid contents (sum of nine phenolic acids) in the four grains were 1.14, 1.70, 0.90, and 1.25 mg/g, respectively, with more than 90% found in the bound form. Ferulic, coumaric, and protocatechuic acids were the major phenolic acids in triticale and wheat. Gallic acid was also rich in triticale. Ferulic, coumaric, hydroxybenzoic, and gallic acids were predominant in barley. In corn, ferulic, coumaric, gallic, and syringic acids were abundant. On the basis of these profiles, pure phenolic acids were added individually and collectively to isolated starches at amounts either equivalent to or 3 times those in the whole grains for hydrolysis. The degree of starch hydrolysis with α-amylase and amyloglucosidase decreased up to 8% when individual phenolic acids were present in cooked starch slurry. The decreases were more pronounced when phenolic acids were added collectively (4-5% with α-amylase and 9-13% with sequential α-amylase and amyloglucosidase). The study of a phenolic acid-starch-enzyme model system indicated that the interactions of phenolic acid-enzyme and phenolic acid-starch significantly contributed to the inhibitory effect of starch hydrolysis. Heating facilitated the interactions. Phenolic acids thus play a significant role in the resistance of starch to enzyme and/or the loss of enzyme activity during starch hydrolysis.

  13. The inhibitory effect of antimicrobial zeolite on the biofilm of Acidithiobacillus thiooxidans.

    Science.gov (United States)

    Haile, Tesfaalem; Nakhla, George

    2010-02-01

    The inhibitory effect of antimicrobial zeolite coated concrete specimens (Z2) against Acidithiobacillus thiooxidans was studied by measuring biomass dry cell weight (DCW), biological sulphate generation, and oxygen uptake rates (OURs). Uncoated (UC), and blank zeolite coated without antimicrobial agent (ZC) concrete specimens were used as controls. The study was undertaken by exposing inoculated basal nutrient medium (BNM) to the various specimens. The coating material was prepared by mixing zeolite, epoxy and cure with ratios, by weight of 2:2:1. Concrete specimens were characterized before and after exposure to inoculated or sterile BNM by field emission-scanning electron microscopy (FE-SEM). Gypsum, which was absent in the other test concrete specimens, was detected in uncoated specimens exposed to the bacterium. In UC and ZC, the growth of the bacteria increased throughout the duration of the experiment. However, significant biomass inhibition was observed in experiments where Z2 was used. The overall biomass growth rate in suspension before the specimens were placed ranged from 3.18 to 3.5 mg DCW day(-1). After the bacterium was exposed to UC and ZC, growth continued with a corresponding value of 4 + or - 0.4 and 5.5 + or - 0.6 mg DCW day(-1), respectively. No biomass growth was observed upon exposure of the bacterium to Z2. Similarly, while biological sulphur oxidation rates in UC and ZC were 88 + or - 13 and 238 + or - 25 mg SO(4)(2-) day(-1), respectively, no sulphate production was observed in experiments where Z2 concrete specimens were used. Peak OURs for UC and ZC ranged from 2.6 to 5.2 mg l(-1) h(-1), and there was no oxygen uptake in those experiments where Z2 was used. The present study revealed that the antimicrobial zeolite inhibits the growth of both planktonic as well as biofilm populations of Acidithiobacillus thiooxidans.

  14. Extraction of protoporphyrin disodium and its inhibitory effects on HBV-DNA

    Institute of Scientific and Technical Information of China (English)

    Chao-Pin Li; Li-Fa Xu; Qun-Hong Liu; Chao Zhang; Jian Wang; Yu-Xia Zhu

    2004-01-01

    AIM: To explore an ideal method for extracting protoporphyrin disodium (PPN) from unanticoagulated animal blood, and to study the inhibitory effects of PPN on HBV-DNA duplication and its cytotoxicity to 2.2.15 cell strain.METHODS: Protoporphyrin methyl ester and other intermediate products were prepared with protoheme separated from protein hydrolysates of coagulated animal blood, which were finally made into PPN and detected quantitatively with an ultraviolet fluorescent analyzer.Ten μg/ml, 20 μg/ml, 40 μg/ml, 80 μg/ml and 160 μg/ml of PPN-aqueous solution were added into culture medium for 2.2.15 cells respectively. Eight days later, the drug concentration in supernatant from the culture medium was detected when inhibition rate of HBeAg, cell Survival rate when inhibition rate of HBeAg was 50% (ID50), and when survival cells in experimental group were 50% of those in control group (CD50), and the therapeutic index (TI) was also detected. PPN with different concentration of 10 μg/ml,20 μg/ml, 40 μg/ml, 80 μg/ml and 160 μg/ml was respectively mixed and cultivated with HepG2 2.2.15 cell suspension,and then the inhibition of PPN against HBV-DNA was judged by PCR.RESULTS: The extract of henna crystal was identified to be PPN. When the concentrations of PPN were 160 μg/ml and 80 μg/ml, the inhibition rates of HBeAg were 89.8% and 82.4%, and the cell survival rates were 98.7% and 99.2%.CONCLUSION: It is suggested that PPN can be extracted from unanticoagulated animal blood. PPN can inhibit HBV-DNA expression and duplication ih vitro, and has no cytotoxicity to liver cells. Further study and application of PPN are warranted.

  15. Inhibitory Effect of Nasal Intermittent Positive Pressure Ventilation on Gastroesophageal Reflux.

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    Danny Cantin

    Full Text Available Non-invasive intermittent positive pressure ventilation can lead to esophageal insufflations and in turn to gastric distension. The fact that the latter induces transient relaxation of the lower esophageal sphincter implies that it may increase gastroesophageal refluxes. We previously reported that nasal Pressure Support Ventilation (nPSV, contrary to nasal Neurally-Adjusted Ventilatory Assist (nNAVA, triggers active inspiratory laryngeal closure. This suggests that esophageal insufflations are more frequent in nPSV than in nNAVA. The objectives of the present study were to test the hypotheses that: i gastroesophageal refluxes are increased during nPSV compared to both control condition and nNAVA; ii esophageal insufflations occur more frequently during nPSV than nNAVA. Polysomnographic recordings and esophageal multichannel intraluminal impedance pHmetry were performed in nine chronically instrumented newborn lambs to study gastroesophageal refluxes, esophageal insufflations, states of alertness, laryngeal closure and respiration. Recordings were repeated without sedation in control condition, nPSV (15/4 cmH2O and nNAVA (~ 15/4 cmH2O. The number of gastroesophageal refluxes recorded over six hours, expressed as median (interquartile range, decreased during both nPSV (1 (0, 3 and nNAVA [1 (0, 3] compared to control condition (5 (3, 10, (p < 0.05. Meanwhile, the esophageal insufflation index did not differ between nPSV (40 (11, 61 h-1 and nNAVA (10 (9, 56 h-1 (p = 0.8. In conclusion, nPSV and nNAVA similarly inhibit gastroesophageal refluxes in healthy newborn lambs at pressures that do not lead to gastric distension. In addition, the occurrence of esophageal insufflations is not significantly different between nPSV and nNAVA. The strong inhibitory effect of nIPPV on gastroesophageal refluxes appears identical to that reported with nasal continuous positive airway pressure.

  16. Inhibitory effect of ubiquitin-proteasome pathway on proliferation of esophageal carcinoma cells

    Institute of Scientific and Technical Information of China (English)

    Wei-Guo Zhang; Jie-Ping Yu; Qing-Ming Wu; Qiang Tong; Sheng-Bao Li; Xiao-Hu Wang; Guo-Jian Xie

    2004-01-01

    AIM: To investigate the inhibitory effect of ubiquitinproteasome pathway (UPP) on proliferation of esophageal carcinoma cells.METHODS: Esophageal carcinoma cell strain EC9706 was treated with MG-132 to inhibit its UPP specificity. Cell growth suppression was evaluated with 3-(4,5-dimethylthiazole2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay. DNA synthesis was evaluated by 3H-thymidine (3H-TdR)incorporation. Morphologic changes of cells were observed under microscope. Activity of telomerase was examined by telomeric repeat amplification protocol (TRAP) of PCRELISA. Cell cycle and apoptosis were detected by flow cytometry (FCM). DNA fragment analysis was used to confirm the presence of apoptosis. Expression of p27kip1was detected by immunocytochemical technique.RESULTS: After exposed to MG-132, the growth and value of 3H-TdR incorporation of EC9706 cells were obviously inhibited. Cells became round, small and exfoliative under microscope. TRAP PCR-ELISA showed that light absorption of cells gradually decreased after exposed to 5 μmol/L of MG-132 for 24, 48, 72 and 96 h (P<0.01). The percentage of cells at G0/G1 phase was increased and that at S and G2/M was decreased (P<0.01). The rate of apoptotic cells treated with 5 μmol/L of MG-132 for 48 and 96 h was 31.7%and 66.4%, respectively. Agarose electrophoresis showed marked ladders. In addition, the positive signals of p27kip1were located in cytoplasm and nuclei in MG-132 group in contrast to cytoplasm staining in control group.CONCLUSION: MG-132 can obviously inhibit proliferation of EC9706 cells and induce apoptosis. The mechanisms include upregulation of p27kip1 expression, G1 arrest and depression of telomerase activity. The results indicate that inhibiting UPP is a novel strategy for esophageal carcinoma therapy.

  17. The Inhibitory Effect of Ziziphora clinopodioides Lam. on Gastric Acid Output at Basal, Vagotomized and Vagal Stimulated Conditions in Rat

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    Saeed Niazmand

    2010-04-01

    Full Text Available Objective(sZiziphora clinopodioides Lam. is a plant widely used in Iranian traditional medicine for gastrointestinal disorders. Several reports have demonstrated antibacterial (Helicobacteria pylori, antioxidant and anti-inflammatory properties of Z. clinopodioides. The aim of this study was to investigate the effects of aqueous-ethanol extract of Z. clinopodioides on rat’s gastric acid output in basal, vagotomized (VX and vagal stimulated conditions.Materials and MethodsA total of 24 male Wistar rats weighed 200-250 g were randomly divided into two groups: control and test. Tracheostomy and gastroduodenostomy procedures were performed for each rat. In the vagotomized condition the vagus nerve in the cervical region was dissected and in the vagal stimulation condition the distal portion of the vogues nerve stimulated. Gastric content was collected for 15 min by wash out technique. A volume of 1 ml of three doses (0.5, 1 and 2 mg/kg was introduced into the stomach (i.g. of each rat in the test group and the same volume of saline was used in the control group. Total titratable acid was measured by a titrator.ResultsThe extract inhibited acid secretion significantly at basal condition. At VX condition not only this inhibitory effect on acid secretion disappeared but also a stimulatory effect at the dose of 2 mg/kg was shown. In vagal stimulation condition the extract showed a significant inhibitory effect at 1 mg/kg dose. ConclusionTaking together our data resulted from comparison of three conditions showed that the extract exerted an inhibitory effect on acid secretion in basal and vagal stimulation. Also, according to our results this inhibitory effect of the extract could be exerted via gastric vagal parasympathetic nerve.

  18. Correlation of inhibitory effects of polymers on indomethacin precipitation in solution and amorphous solid crystallization based on molecular interaction.

    Science.gov (United States)

    Chauhan, Harsh; Kuldipkumar, Anuj; Barder, Timothy; Medek, Ales; Gu, Chong-Hui; Atef, Eman

    2014-02-01

    To correlate the polymer's degree of precipitation inhibition of indomethacin in solution to the amorphous stabilization in solid state. Precipitation of indomethacin (IMC) in presence of polymers was continuously monitored by a UV spectrophotometer. Precipitates were characterized by PXRD, IR and SEM. Solid dispersions with different polymer to drug ratios were prepared using solvent evaporation. Crystallization of the solid dispersion was monitored using PXRD. Modulated differential scanning calorimetry (MDSC), IR, Raman and solid state NMR were used to explore the possible interactions between IMC and polymers. PVP K90, HPMC and Eudragit E100 showed precipitation inhibitory effects in solution whereas Eudragit L100, Eudragit S100 and PEG 8000 showed no effect on IMC precipitation. The rank order of precipitation inhibitory effect on IMC was found to be PVP K90 > Eudragit E100 > HPMC. In the solid state, polymers showing precipitation inhibitory effect also exhibited amorphous stabilization of IMC with the same rank order of effectiveness. IR, Raman and solid state NMR studies showed that rank order of crystallization inhibition correlates with strength of molecular interaction between IMC and polymers. Correlation is observed in the polymers ability to inhibit precipitation in solution and amorphous stabilization in the solid state for IMC and can be explained by the strength of drug polymer interactions.

  19. The Doppler Effect: A Consideration of Quasar Redshifts.

    Science.gov (United States)

    Gordon, Kurtiss J.

    1980-01-01

    Provides information on the calculation of the redshift to blueshift ratio introduced by the transverse Doppler effect at relativistic speeds. Indicates that this shift should be mentioned in discussions of whether quasars are "local" rather than "cosmological" objects. (GS)

  20. The Doppler Effect: A Consideration of Quasar Redshifts.

    Science.gov (United States)

    Gordon, Kurtiss J.

    1980-01-01

    Provides information on the calculation of the redshift to blueshift ratio introduced by the transverse Doppler effect at relativistic speeds. Indicates that this shift should be mentioned in discussions of whether quasars are "local" rather than "cosmological" objects. (GS)

  1. Inhibitory effect of hexane fraction from Myagropsis myagroides on pancreatic α-amylase in vitro.

    Science.gov (United States)

    Pak, Won-Min; Kim, Koth-Bong-Woo Ri; Kim, Min-Ji; Cho, Ji-Young; Ahn, Dong-Hyun

    2015-03-01

    A Myagropsis myagroides (Mm) methanol extract showed α-amylase inhibitory activity of 13% at a concentration of 5 mg/ml. Results showed that the hexane fraction from the Mm methanol extract exhibited α-amylase inhibitory activity with an IC50 value of 4.24 mg/ml. The hexane fraction was separated using silica-gel column chromatography, and six subfractions were obtained. The fraction eluted with CHCl3:MeOH = 50:1 showed the highest α-amylase inhibitory activity with an IC50 value of 0.72 mg/ml. This fraction was purified using Sephadex LH-20 column chromatography and an octadecyl silica (ODS) Sepak cartridge, obtaining seven subfractions. Fraction (Fr.) 4 also showed a strong α-amylase inhibitory activity with an IC50 value of 0.75 mg/ml. Fr. 4 was purified by Sephadex LH-20 column chromatography and ODS Sepak cartridge, obtaining six subfractions. Fr. 4-2 was identified as sargachromanol I with an IC50 value of 0.40 mg/ml, and the inhibition pattern analyzed from Lineweaver-Burk plots revealed it to be an uncompetitive inhibitor. These results suggest that Mm has potential as a natural antidiabetes agent.

  2. Lignan dicarboxylates and terpenoids from the flower buds of Cananga odorata and their inhibitory effects on melanogenesis.

    Science.gov (United States)

    Matsumoto, Takahiro; Nakamura, Seikou; Nakashima, Souichi; Fujimoto, Katsuyoshi; Yoshikawa, Masayuki; Ohta, Tomoe; Ogawa, Keiko; Matsuda, Hisashi

    2014-04-25

    The methanolic extract from the flower buds of Cananga odorata showed an inhibitory effect on melanogenesis in theophylline-stimulated murine B16 melanoma 4A5 cells. From the methanolic extract, two new lignan dicarboxylates, canangalignans I and II, three new terpenoids, canangaterpenes I, II, and III, and eight known compounds were isolated. The structures of these compounds were elucidated on the basis of chemical/physicochemical evidence. Several mono- and sesquiterpene analogues significantly inhibited melanogenesis. In particular, canangaterpene I and (3R,3aR,8aS)-3-isopropyl-8a-methyl-8-oxo-1,2,3,3a,6,7,8,8a-octahydroazulene-5-carbaldehyde exhibited a potent inhibitory effect on melanogenesis [inhibition (%): 34.7±4.2 (pterpenoid derivatives may be promising therapeutic agents for the treatment of several skin disorders.

  3. The effects of safety behaviors during exposure therapy for anxiety: Critical analysis from an inhibitory learning perspective.

    Science.gov (United States)

    Blakey, Shannon M; Abramowitz, Jonathan S

    2016-11-01

    In the context of clinical anxiety, safety behaviors are actions performed to prevent, escape, or minimize feared catastrophes and/or associated distress. Research consistently implicates safety behaviors in the development and maintenance of anxiety disorders; accordingly, safety behaviors are traditionally eliminated during exposure treatments for pathological anxiety. The notion that safety behaviors are ubiquitously deleterious in the context of exposure has recently been challenged, yet findings regarding safety behaviors' effects on exposure outcomes are limited, mixed, and controversial. Furthermore, developments in explanatory models for exposure's effectiveness (e.g., inhibitory learning theory) highlight other possible consequences of safety behaviors performed during exposure. Unfortunately, these theoretical advances are neglected in experimental research. The present review critically examines the literature addressing the role of safety behaviors in exposure therapy from an inhibitory learning perspective. Limitations, future directions, and clinical recommendations are also discussed.

  4. Effects of chloroquine, mefloquine and quinine on natural killer cell activity in vitro. An analysis of the inhibitory mechanism

    DEFF Research Database (Denmark)

    Pedersen, B K; Bygbjerg, I C; Theander, T G

    1986-01-01

    Natural killer (NK) cell activity against K 562 target cells was inhibited by pharmacological concentrations of chloroquine, mefloquine and quinine. The most potent were mefloquine and quinine. The drug-induced inhibition of the NK cell activity was abolished by addition of alpha-interferon (IF......) or interleukin 2 (Il-2); preincubation of mononuclear cells with IF or Il-2 followed by addition of anti-malarial drugs decreased the inhibitory effects of the drugs. The drug-induced inhibition of the NK cell activity was not dependent on the presence of monocytes. Using monocyte depleted Percoll fractionated...... NK cell enriched populations in a single cell agarose assay, it was shown that the inhibitory effects of mefloquine, but not of chloroquine and quinine were due to an inhibition of the formation of effector/target cell conjugates....

  5. Methodological considerations in the analysis of cost effectiveness in dentistry.

    Science.gov (United States)

    Antczak-Bouckoms, A A; Tulloch, J F; White, B A; Capilouto, E I

    1989-01-01

    Cost-effectiveness analysis is a technique applied with increasing frequency to help make rational decisions in health care resource allocation. This article reviews the ten general principles of cost-effectiveness analysis outlined by the Office of Technology Assessment of the US Congress and describes a model for such analyses used widely in medicine, but only recently applied in dentistry. The imperative for the formulation of the best current information on both the effectiveness of dental practices and their costs is made more urgent because of the now universally recognized belief that resources available to meet the demands for health care are limited. Today's environment requires critical allocation decisions within categorical health problems, across diseases, or relative to other health problems. If important health benefits or cost savings are to be realized, then these analytic approaches must become widely understood, accepted, and appropriately applied by key decision makers in the dental health sector.

  6. New 5-deoxyflavonoids and their inhibitory effects on protein tyrosine phosphatase 1B (PTP1B) activity

    DEFF Research Database (Denmark)

    Nguyen, Phi Hung; Dao, Trong Tuan; Kim, Jayeon;

    2011-01-01

    , MS, CD, 1D- and 2D-NMR) and physicochemical analyses. All isolates exhibited moderate inhibitory effects on the enzyme assay with IC₅₀ values ranging from 14.9 ± 1.6 to 98.1 ± 11.3 μM. Compounds with prenyl and methoxy groups in the B ring (1, 2, 4, 8, and 13) possessed strong activity (IC(50) 14...

  7. Inhibitory Effect of Three C-glycosylflavonoids from Cymbopogon citratus (Lemongrass) on Human Low Density Lipoprotein Oxidation

    OpenAIRE

    Elba Leiva; José Cheel; Roxana Orrego

    2009-01-01

    This study assessed the inhibitory effect of three C-glycosylflavonoids from Cymbopogon citratus leaves - isoorientin (1), swertiajaponin (2) and isoorientin 2"-Orhamnoside (3) - on human LDL oxidation. Isolated LDL was incubated with compounds 1-3 and the kinetics of lipid peroxidation were assessed by conjugated diene and malondialdehyde-thiobarbituric acid reactive substances (MDA-TBARS) formation after addition of copper ions. Significant differences (p < 0.05) between the lag time pha...

  8. Inhibitory effect of salvianolate on human cytochrome P450 3A4 in vitro involving a noncompetitive manner

    OpenAIRE

    Qin, Chong-Zhen; Ren, Xian; Zhou, Hong-Hao; Mao, Xiao-Yuan; Liu, Zhao-qian

    2015-01-01

    Salvianolic acid B (Sal B), which is purified from Danshen, is a popular herb extract. Sal B has anti-oxidative, anti-inflammatory, anti-hypoxic, anti-arteriosclerotic and anti-apoptotic properties. This substance can also ameliorate brain injury or neurodegenerative diseases. The listed drug Salvianolate, which contains a substantial amount of Sal B, has been used for the treatment of coronary heart disease. Our present work aimed to evaluate the inhibitory effect of salvianolate on seven cy...

  9. Inhibitory effect of Zataria multiflora Boiss. essential oil, alone and in combination with monolaurin, on Listeria monocytogenes

    OpenAIRE

    Raeisi, Mojtaba; Tajik, Hossein; Razavi Rohani, Seyed Mehdi; Bektas TEPE; Kiani, Hossein; Khoshbakht, Rahem; Shirzad Aski, Hesamaddin; Tadrisi, Hamed

    2016-01-01

    Listeria monocytogenes is one of the major causes of infections in developing countries. In this study, chemical composition and anti-listerial effect of the essential oil of Zataria multiflora Boiss. alone and in combination with monolaurin were evaluated at different pH values (5, 6, and 7) and temperatures (5 ˚C and 30 ˚C). Chemical composition of Zataria multiflora Boiss. essential oil was evaluated by gas chromatography-mass spectrometry (GC-MS) analysis. Minimum inhibitory concentration...

  10. Inhibitory effect of celecoxib combined with cisplatin on growth of human tongue squamous carcinoma Tca8113 cell xenograft tumor

    Institute of Scientific and Technical Information of China (English)

    Weizhong Li; Xiaoyan Wang; Zuguo Li; Yanqing Ding

    2010-01-01

    Objective:The aim of this study was to observe the inhibitory effect of application of COX-2 inhibitor,celecoxib,combined with cisplatin on the growth of human tongue squamous carcinoma Tca8113 cell xenograft by animal experiment.Methods:The nude mice were transplanted subcutaneously with Tca 8113 cells,and then were administrated with celecoxib,cisplatin or celecoxib combined with cisplatin respectively,and were sacrificed after 35 days.The weight of xenograft was measured to calculate the tumor inhibition rate.The histological change was studied under light and electron microscope.The COX-2 protein expression was observed by immunohistological staining.And the COX-2 mRNA expression was determined by RT-PCR.Results:Celecoxib,the COX-2 inhibitor,could not only inhibit the growth of Tca8113 cell xenograft tumor and COX-2 protein expression,but also enhance the inhibitory effect cisplatin on xenograft tumor growth significantly.The tumor inhibition rates of celecoxib group,cisplatin group and celecoxib plus cisplatin group were 15.63%,37.50% and 82.81%respectively that was statistically significant compared to control group(P < 0.01).The combined application of celecoxib and dsplatin could inhibit tumor growth more significantly than that of separated application(P < 0.01).The inhibitory effect of celecoxib on COX-2 mRNA expression of Tca 8113 cell was weaker and not significant(P= 0.073).Conclusion:Celecoxib can not only inhibit xenograft tumor growth in nude mice,but also enhance the inhibitory effect of CDDP on Tca 8113 trans planted tumor growth in nude mice.The mechanism maybe related to inhibition of COX-2 protein expression,which offers beneficial reference to further explore the mechanism between inhibition of COX-2 enzyme activity and prevention of head and neck tumor.

  11. In Vitro Inhibitory Effects of Scutellarin on Six Human/Rat Cytochrome P450 Enzymes and P-glycoprotein

    Directory of Open Access Journals (Sweden)

    Yong-Long Han

    2014-05-01

    Full Text Available Inhibition of cytochrome P450 (CYP and P-glycoprotein (P-gp are regarded as the most frequent and clinically important pharmacokinetic causes among the various possible factors for drug-drug interactions. Scutellarin is a flavonoid which is widely used for the treatment of cardiovascular diseases. In this study, the in vitro inhibitory effects of scutellarin on six major human CYPs (CYP1A2, CYP2C8, CYP2C9, CYP2C19, CYP2D6, and CYP3A4 and six rat CYPs (CYP1A2, CYP2C7, CYP2C11, CYP2C79, CYP2D4, and CYP3A2 activities were examined by using liquid chromatography-tandem mass spectrometry. Meanwhile, the inhibitory effects of scutellarin on P-gp activity were examined on a human metastatic malignant melanoma cell line WM-266-4 by calcein-AM fluorometry screening assay. Results demonstrated that scutellarin showed negligible inhibitory effects on the six major CYP isoenzymes in human/rat liver microsomes with almost all of the IC50 values exceeding 100 μM, whereas it showed values of 63.8 μM for CYP2C19 in human liver microsomes, and 63.1 and 85.6 μM for CYP2C7 and CYP2C79 in rat liver microsomes, respectively. Scutellarin also showed weak inhibitory effect on P-gp. In conclusion, this study demonstrates that scutellarin is unlikely to cause any clinically significant herb-drug interactions in humans when co-administered with substrates of the six CYPs (CYP1A2, CYP2C8, CYP2C9, CYP2C19, CYP2D6, and CYP3A4 and P-gp.

  12. INHIBITORY EFFECTS OF MIFEPRISTONE ON THE GROWTH OF HUMAN GASTRIC CANCER CELL LINE MKN-45 IN VITRO AND IN VIVO

    Institute of Scientific and Technical Information of China (English)

    Da-qiang Li; Li-hua Pan; Zhi-min Shao

    2004-01-01

    Objective To explore the effects of mifepristone on the growth of human gastric cancer cell line MKN-45 and its possible mechanisms.Methods In situ hybridization was used to detect the expression of progesterone receptor (PR) mRNA in MKN-45cells. Proliferation, cell cycle distribution, and the expression of Bcl-xL and vascular endothelial growth factor (VEGF) of MKN-45 cells incubated with various concentrations of mifepristone (1, 5, 10, and 20 μmol/L) were analyzed using MTT reduction assay, flow cytometry, reverse transcription-polymerase chain reaction (RT-PCR), and enzyme-linked immunoabsorbent assay (ELISA), respectively. After transplantation of MKN-45 cells underneath the skin of athymic mice, mifepristone proliferating cell nuclear antigen (PCNA) in xenografted tumors were detected using transmission electron microscopy and immunohistochemical staining, respectively.Results PR mRNA was highly expressed in cultured MKN-45 cell. Mifepristone dose-dependently inhibited the proliferation of MKN-45 cells, and the inhibitory rate was dramatically increased from 7.21% to 47.23%. The inhibitory effect was accompanied by a dose-dependent increase in the percentage of cells in G0/G1 phase, and with a concurrent decrease in the proportion of S- and G2/M-phase cells and the proliferative index from 57.65% to 24.54%. Meanwhile,mifepristone dom-regulated the expression of Bcl-xL and VEGF in a dose-dependent manner. In vivo, mifepristone effectively inhibited the growth of xenografted tumors in nude mice (55.14% for inhibitory rate), induced apoptosis, and down-regulated PCNA expression in gastric cancer.Conclusion Mifepristone exerts significant growth inhibitory effects on PR-positive human MKN-45 gastric cancer cells via multiple mechanisms, and may be a beneficial agent against the tumor.

  13. In Vitro Antioxidant Properties, HIV-1 Reverse Transcriptase and Acetylcholinesterase Inhibitory Effects of Traditional Herbal Preparations Sold in South Africa

    OpenAIRE

    2010-01-01

    The antioxidant potentials for fourteen multipurpose traditional herbal preparations sold in South Africa were determined using the DPPH radical scavenging, ferric reducing power and β-carotene-linoleic acid model system, the anti-HIV-1 reverse transcriptase (RT) enzyme inhibitory effects using an ELISA kit and acetylcholinesterase (AChE) enzyme inhibition using the microtitre plate assay. Nine of the herbal mixtures (Umzimba omubi, Umuthi wekukhwehlela ne zilonda, Mvusa ukunzi, Umpatisa inko...

  14. Cooperative inhibitory effects of antisense oligonucleotide of cell adhesion molecules and cimetidine on cancer cell adhesion

    Institute of Scientific and Technical Information of China (English)

    Nan-Hong Tang; Yan-Ling Chen; Xiao-Qian Wang; Xiu-Jin Li; Feng-Zhi Yin; Xiao-Zhong Wang

    2004-01-01

    AIM: To explore the cooperative effects of antisense oligonucleotide (ASON) of cell adhesion molecules and cimetidine on the expression of E-selectin and ICAM-1 in endothelial cells and their adhesion to tumor cells.METHODS: After treatment of endothelial cells with ASON and/or cimetidine and induction with TNF-α, the protein and mRNA changes of E-selectin and ICAM-1 in endothelial cells were examined by flow cytometry and RT-PCR,respectively. The adhesion rates of endothelial cells to tumor cells were measured by cell adhesion experiment.RESULTS: In comparison with TNF-α inducing group, lipoASON and lipo-ASON/cimetidine could significantly decrease the protein and mRNA levels of E-selectin and ICAM-1 in endothelial cells, and lipo-ASON/cimetidine had most significant inhibitory effect on E-selectin expression (from 36.37±1.56% to 14.23±1.07%, P<0.001). Meanwhile,cimetidine alone could inhibit the expression of E-selectin (36.37±1.56% vs 27.2±1.31%, P<0.001), but not ICAM-1 (69.34±2.50% vs68.07±2.10%,P>O.05)and the two kinds of mRNA, either. Compared with TNF-αα inducing group, the rate of adhesion was markedly decreased in lipo-E-selectin ASON and lipo-E-selectin ASON/cimetidine treated groups(P<0.05),and Jipo-E-selectin ASON/cimetidine worked better than lipo-E-selectin ASON alone except for HepG2/ECV304 group(P<0.05). However, the decrease of adhesion was not significant in lipo-ICAM-1 ASON and lipo-ICAM-1 ASON/cimetidine treated groups except for HepG2/ECV304 group (P >0.05).CONCLUSION: These data demonstrate that ASON in combination with cimetidine in vitro can significantly reduce the adhesion between endothelial cells and hepatic or colorectal cancer cells, which is stronger than ASON or cimetidine alone. This study provides some useful proofs for gene therapy of antiadhesion.

  15. Consideration of pavement roughness effects on vehicle-pavement interaction

    CSIR Research Space (South Africa)

    Steyn, WJvdM

    2001-07-01

    Full Text Available and AT VISSER* CSIR Transportek, PO Box 395, Pretoria, 0001 *University of Pretoria, Department of Civil Engineering, Pretoria, 0002 ABSTRACT Current mechanistic pavement design and analysis techniques use several simplifications to enable... the process to be practical and cost-effective. These include equivalent vehicle loads, linear elastic analysis and static vehicle load and pavement response analysis. These simplifications allow the process of pavement design and analysis to be applied...

  16. PERTINENT DRY NEEDLING CONSIDERATIONS FOR MINIMIZING ADVERSE EFFECTS - PART ONE.

    Science.gov (United States)

    Halle, John S; Halle, Rob J

    2016-08-01

    Dry needling is an evidence-based treatment technique that is accepted and used by physical therapists in the United States. This treatment approach focuses on releasing or inactivating muscular trigger points to decrease pain, reduce muscle tension, and assist patients with an accelerated return to active rehabilitation. While commonly used, the technique has some patient risk and value of the treatment should be based on benefit compared to the potential risk. Adverse effects (AEs) with dry needling can be mild or severe, with overall incidence rates varying from zero to rates of approximately 10 percent. While mild AEs are the rule, any procedure that involves a needle insertion has the potential for an AE, with select regions and the underlying anatomy increasing the risk. Known significant AEs from small diameter needle insertion include pneumothorax, cardiac tamponade, hematoma, infection, central nervous system injury, and other complications. Underlying anatomy across individuals has variability, requiring an in-depth knowledge of anatomy prior to any needle placement. This commentary is an overview of pertinent anatomy in the region of the thorax, with a 'part two' that addresses the abdomen, pelvis, back, vasovagal response, informed consent and other pertinent issues. The purpose of the commentary is to minimize the risk of a dry needling AE. Dry needling is an effective adjunct treatment procedure that is within the recognized scope of physical therapy practice. Physical therapy education and training provides practitioners with the anatomy, basic sciences, and clinical foundation to use this intervention safely and effectively. A safe and evidenced-based implementation of the procedure is based on a thorough understanding of the underlying anatomy and the potential risks, with risks coordinated with patients via informed consent. Level 5.

  17. Diabetes attenuates the inhibitory effects of endomorphin-2, but not endomorphin-1 on gastrointestinal transit in mice.

    Science.gov (United States)

    Wang, Chang-lin; Diao, Yu-xiang; Xiang, Qiong; Ren, Yu-kun; Gu, Ning

    2014-09-05

    Diabetes affects the entire gastrointestinal tract from the esophagus to the anus. In the present study, the charcoal meal test was undertaken to evaluate and compare the effects of intracerebroventricular (i.c.v.) administration of endomorphins (EMs) on gastrointestinal transit in non-diabetic and diabetic mice. Significantly delayed gastrointestinal transit was found in both 4 and 8 weeks alloxan-induced diabetes compared to non-diabetes. Moreover, i.c.v. EM-1 and EM-2 dose-dependently delayed gastrointestinal transit in non-diabetes and diabetes. The EM-1-induced inhibitory effects of gastrointestinal transit in 4 weeks diabetes were qualitatively similar to those of non-diabetes. However, at higher doses, the EM-1-induced effects in 8 weeks diabetes were largely enhanced. Different to EM-1, the EM-2-induced inhibition of gastrointestinal transit in diabetic mice was significantly attenuated compared to non-diabetic mice. Moreover, these effects were further decreased in 8 weeks diabetes. The delayed gastrointestinal transit effects caused by EM-1 may be primarily mediated by μ2-opioid receptor in both non-diabetes and 4 weeks diabetes. Interestingly, in 8 weeks diabetes, these effects were mediated by μ2- and δ-receptors. However, the inhibitory effects of EM-2 were mediated by μ1-opioid receptor, which exerted a reduced function in diabetes. Also, poor blood glucose control might result in the attenuated effects of EM-2. Our present results demonstrated that diabetes attenuates the inhibitory effects of EM-2, but not EM-1 on gastrointestinal transit in mice. The different effects of EM-1 and EM-2 on gastrointestinal transit in diabetes may be due to changes of opioid receptor subtypes and their functional responses.

  18. Growth inhibitory effect of polyunsaturated fatty acids (PUFAs on colon cancer cells via their growth inhibitory metabolites and fatty acid composition changes.

    Directory of Open Access Journals (Sweden)

    Chengcheng Zhang

    Full Text Available Colorectal cancer is common. Polyunsaturated fatty acids (PUFAs exert growth-inhibitory and pro-apoptotic effects on colon cancer cells. Metabolites of PUFAs such as prostaglandins (PGs, leukotrienes (LTs and lipoxins (LXs play a significant role in colon cancer.Human colon cancer LoVo and RKO cells were cultured with different concentration of PUFAs and 5-fluorouracil (5-FU in vitro. Cell morphological changes, fatty acid composition, formation of PGE2, LTB4 and LXA4 and expression of COX-2, ALOX5, PGD synthase (PGDS, microsomal prostaglandin E synthase (mPGES were assessed in LoVo and RKO cells when supplemented with PUFAs and 5-FU.PUFAs and 5-FU inhibited growth of LoVo and RKO cells to the same extent at the doses used and produced significant alterations in their shape. As expected, higher concentrations of supplemented PUFAs were noted in the cells compared to control. LA, GLA, AA, ALA and EPA supplementation to LoVo cells suppressed production of PGE2, LTB4,and ALOX5, mPGES expression, but enhanced that of LXA4; whereas DHA enhanced PGE2 and LXA4 synthesis but decreased LTB4 formation and COX-2, ALOX5, mPGES expression. In contrast, 5-FU enhanced formation of PGE2, LTB4 and mPGES expression, but suppressed LXA4 synthesis and COX-2 expression. PGE2, LTB4 synthesis and ALOX5 expression was suppressed by LA, GLA, ALA and DHA; whereas AA, EPA and 5-FU enhanced PGE2 but paradoxically AA decreased and EPA and 5-FU enhanced LTB4 synthesis in RKO cells. All the PUFAs tested enhanced, while 5-FU decreased LXA4 formation in RKO cells; whereas GLA, AA, and 5-FU augmented while LA, ALA, EPA and DHA enhanced COX-2 expression in RKO cells.Tumoricidal action of PUFAs on colorectal LoVo and RKO cancer cells in vitro was associated with increased formation of LXA4, decreased synthesis of PGE2 and LTB4 and suppressed expression of COX-2, ALOX5, mPGES, whereas 5-FU produced contrasting actions on these indices.

  19. C-Methylated Flavonoids from Cleistocalyx operculatus and Their Inhibitory Effects on Novel Influenza A (H1N1) Neuraminidase

    DEFF Research Database (Denmark)

    Dao, Trong-Tuan; Tung, Bui-Thanh; Nguyen, Phi-Hung

    2010-01-01

    As part of an ongoing study focused on the discovery of anti-influenza agents from plants, four new (1-4) and 10 known (5-14) C-methylated flavonoids were isolated from a methanol extract of Cleistocalyx operculatus buds using an influenza H1N1 neuraminidase inhibition assay. Compounds 4, 7, 8......, and 14, with a chalcone skeleton, showed significant inhibitory effects on the viral neuraminidases from two influenza viral strains, H1N1 and H9N2. Compound 4 showed the strongest inhibitory activity against the neuraminidases from novel influenza H1N1 (WT) and oseltamivir-resistant novel H1N1 (H274Y...... as neuraminidase inhibitors for novel influenza H1N1....

  20. Inhibitory effect of organic acids on arcobacters in culture and their use for control of Arcobacter butzleri on chicken skin.

    Science.gov (United States)

    Skřivanová, Eva; Molatová, Zuzana; Matěnová, Michaela; Houf, Kurt; Marounek, Milan

    2011-01-05

    The inhibitory effects of 17 organic acids (C₂-C₁₆ fatty acids, sorbic, benzoic, phenylacetic, fumaric, succinic, lactic, malic and citric) on Arcobacter butzleri, Arcobacter cryaerophilus and Arcobacter skirrowii were investigated by determining their IC₅₀ values, defined as the concentration of acid at which the target DNA sequence was expressed at 50% of the positive control level in cultures incubated at 30°C for 24 h. DNA was analysed by real-time PCR. The Arcobacter strains tested were inhibited by all the organic acids, with the sensitivities in the order A. skirrowii > A. cryaerophilus > A. butzleri. Eight acids with IC₅₀ values of arcobacters on Muller-Hinton agar. All eight tested acids suppressed bacterial proliferation. The highest inhibitory activities were observed for benzoic, citric, malic and sorbic acids. Subsequent sensory analysis revealed benzoic acid to be the most suitable organic acid for chicken skin treatment.

  1. INHIBITORY EFFECTS OF THE ALKALOIDS FROM Radix Caulophylli ON THE PROLIFERATION OF HUMAN VASCULAR ENDOTHELIAL CELL

    Institute of Scientific and Technical Information of China (English)

    2005-01-01

    Objective To find an angiogenetic inhibitor from Radix Caulophylli (RC). Methods The extract of Radix Caulophylli was obtained by using 95% alcohol in water as solvent. Then, the total alkaloids of Radix Caulophylli was isolated from the extract by using a positive ion exchange resin column. An active part was found by a screening model of cell membrane chromatography (CMC) and further tested by the MTT method with emodin as a control. Results The total alkaloids of Radix Caulophylli was the active part by CMC and could significantly inhibit proliferation of ECV304 cells in MTT test. The inhibitory rate was 56.06% while the concentration of the total alkaloids of Radix Caulophylli was 19.63μg/mL. Conclusion The total alkaloids from Radix Caulophylli may be a new angiogenetic inhibitor, and mechanism of the total alkaloids on inhibitory angiogenesis still need to be further investigated.

  2. Inhibitory effects of constituents of Morinda citrifolia seeds on elastase and tyrosinase.

    Science.gov (United States)

    Masuda, Megumi; Murata, Kazuya; Fukuhama, Akiko; Naruto, Shunsuke; Fujita, Tadashi; Uwaya, Akemi; Isami, Fumiyuki; Matsuda, Hideaki

    2009-07-01

    A 50% ethanolic extract (MCS-ext) from seeds of Morinda citrifolia ("noni" seeds) showed more potent in vitro inhibition of elastase and tyrosinase, and 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging activity than extracts of M. citrifolia leaves or flesh. Activity-guided fractionation of MCS-ext using in vitro assays led to the isolation of ursolic acid as an active constituent of elastase inhibitory activity. 3,3'-Bisdemethylpinoresinol, americanin A, and quercetin were isolated as active constituents having both tyrosinase inhibitory and radical scavenging activities. Americanin A and quercetin also showed superoxide dismutase (SOD)-like activity. These active compounds were isolated from noni seeds for the first time.

  3. Inhibitory Effect of Isoflavones on Prostate Cancer Cells and PTEN Gene

    Institute of Scientific and Technical Information of China (English)

    2006-01-01

    Objective To explore the mechanisms by which genistein and daidzein inhibit the growth of prostate cancer cells. Methods LNCaP and PC-3 cells were exposed to genistein and daidzein and cell viability was determined by MTT assay and cytotoxicity of the drugs by LDH test. Flow cytometry (FCM) was used to assess the cell cycle in LNCaP and PC-3 cells.Reverse transcription-polymerase chain reaction (RT-PCR) was applied to examine the expression of PTEN gene (a tumor suppressor gene), estrogen receptor alpha gene (Erα), estrogen receptor beta gene (Erβ), androgen receptor gene (AR) and vascular endothelial growth factor gene (VEGF). Results The viability of PC-3 and LNCaP cells decreased with increasing concentrations and exposure time of genistein and daidzein. Genistein increased G2/M phase cells in PC-3 cells while decreased S phase cells in LNCaP cells in a dose-dependent manner. Daidzein exerted no influence on the cell cycle of LNCaP and PC-3 cells, but the apoptosis percentage of LNCaP cells was elevated significantly by daidzein. Genistein induced the expression of PTEN gene in PC-3 and LNCaP cells. Daidzein induced the expression of PTEN gene in LNCaP but not in PC-3 cells. The expression of VEGF, Erα and Erβ genes decreased and AR gene was not expressed after incubation with genistein and daidzein in PC-3 cells. In LNCaP cells, the expression of VEGF and AR gene decreased but there was no change in the expression of Erα and Erβ gene after incubation with genistein and daidzein. Conclusion Genistein and daidzein exert a time- and dose-dependent inhibitory effect on PC-3 and LNCaP cells. The down-regulation of ER gene by daidzein influences the growth of PC-3 cells directly. The inhibition of PC-3 cells by genistein and that of LNCaP cells by genistein and daidzein may be via Akt pathway that is repressed by PTEN gene, which subsequently down-regulates the expression of AR and VEGF genes. Our results suggest that the expression of PTEN gene plays a key

  4. Inhibitory effects of fasudil on renal interstitial fibrosis induced by unilateral ureteral obstruction.

    Science.gov (United States)

    Baba, Itsuko; Egi, Yasuhiro; Utsumi, Hiroyuki; Kakimoto, Tetsuhiro; Suzuki, Kazuo

    2015-12-01

    Renal fibrosis is the major cause of chronic kidney disease, and the Rho/Rho-associated coiled-coil kinase (ROCK) signaling cascade is involved in the renal fibrotic processes. Several studies have reported that ROCK inhibitors attenuate renal fibrosis. However, the mechanism of this process remains to be fully elucidated. The present study assessed the inhibitory effect of fasudil, a ROCK inhibitor using immunohistochemistry, reverse transcription-quantitative polymerase chain reaction and western blot analyses, in vivo and in vitro, to elucidate the mechanisms underlying renal interstitial fibrosis. In mice induced with unilateral ureteral obstruction (UUO), collagen accumulation, the expression of fibrosis‑associated genes and the content of hydroxyproline in the kidney increased 3, 7, and 14 days following UUO. Fasudil attenuated the histological changes, and the production of collagen and extracellular matrix in the UUO kidney. The expression of α‑smooth muscle actin (α‑SMA) and the transforming growth factor‑β (TGFβ)‑Smad signaling pathway, and macrophage infiltration were suppressed by fasudil in the kidneys of the UUO mice. The present study also evaluated the role of intrinsic renal cells and infiltrated macrophages using NRK‑52E, NRK‑49F and RAW264.7 cells. The mRNA and protein expression levels of collagen I and α‑SMA increased in the NRK‑52E and NRK‑49F cells stimulated by TGF‑β1. Hydroxyfasudil, a bioactive metabolite of fasudil, attenuated the increase in the mRNA and protein expression levles of α‑SMA in the two cell types. However, the reduction in the mRNA expression of collagen I was observed in the NRK‑49F cells only. Hydroxyfasudil decreased the mRNA expression of monocyte chemoattractant protein‑1 (MCP‑1) induced by TGF‑β1 in the NRK‑52E cells, but not in the NRK‑49F cells. In the RAW264.7 cells, the mRNA expression levels of MCP‑1, interleukin (IL)‑1β, IL‑6 and tumor necrosis factor

  5. Inhibitory effects of carbon dioxide insufflation on pneumoperitoneum and bowel distension after percutaneous endoscopic gastrostomy

    Institute of Scientific and Technical Information of China (English)

    Shinji Nishiwaki; Hiroshi Araki; Motoshi Hayashi; Jun Takada; Masahide Iwashita; Atsushi Tagami; Hiroo Hatakeyama

    2012-01-01

    AIM:To evaluate the inhibitory effects of carbon dioxide (CO2) insufflation on pneumoperitoneum and bowel distension after percutaneous endoscopic gastrostomy (PEG).METHODS:A total of 73 consecutive patients who were undergoing PEG were enrolled in our study.After eliminating 13 patients who fitted our exclusion criteria,60 patients were randomly assigned to either CO2 (30patients) or air insufflation (30 patients) groups.PEG was performed by pull-through technique after three-point fixation of the gastric wall to the abdominal wall using a gastropexy device.Arterial blood gas analysis was performed immediately before and after the procedure.Abdominal X-ray was performed at 10 min and at 24 h after PEG to assess the extent of bowel distension.Abdominal computed tomography was performed at 24 h after the procedure to detect the presence of pneumoperitoneum.The outcomes of PEG for 7 d post-procedure were also investigated.RESULTS:Among 30 patients each for the air and the CO2 groups,PEG could not be conducted in 2 patients of the CO2 group,thus they were excluded.Analyses of the remaining 58 patients showed that the patients' backgrounds were not significantly different between the two groups.The elevation values of arterial partial pressure of CO2 in the air group and the CO2 group were 2.67 mmHg and 3.32 mmHg,respectively (P =0.408).The evaluation of bowel distension on abdominal X ray revealed a significant decrease of small bowel distension in the CO2 group compared to the air group (P < 0.001) at 10 min and 24 h after PEG,whereas there was no significant difference in large bowel distension between the two groups.Pneumoperitoneum was observed only in the air group but not in the CO2 group (P =0.003).There were no obvious differences in the laboratory data and clinical outcomes after PEG between the two groups.CONCLUSION:There was no adverse event associated with CO2 insufflation.CO2 insufflation is considered to be safer and more comfortable for PEG patients

  6. Inhibitory effects of PIN1 antisense gene on the proliferation of human osteosarcoma cells

    Institute of Scientific and Technical Information of China (English)

    2006-01-01

    Objective: To evaluate the inhibitory effects of PIN1 antisense gene on the proliferation of human osteosarcoma cells. Methods: Different doses of antisense PIN1 gene (0,20,50,100,200,250μl) were transfected into osteosarcoma MG-63 cells. The cells and the culture supernatants before and after transfection were collected. The cell growth curve was made using MTT method. The cell growth cycle and apoptosis were detected by FCM. The expression of PIN1 was detected by Western blot. The expression of PIN1 mRNA was detected by reverse transcription polymerase chain reaction (RT-PCR). Results: MTT and FCM assays indicated that the transfection of antisense PIN1 gene could inhibit proliferation of MG-63 cells and lead to cell apoptosis. Western-blot assays revealed the MG-63 cells transfected with antisense PIN1 gene had weaker expression than those without transfection with antisense PIN1 gene, and the band intensity was negatively related with doses. The cells transfected with different doses of gene (0,20,50,100,200,250 μl) had different absorbance rate(0.854 ± 0.136,0. 866 ± 0. 138,0. 732 ± 0. 154, 0. 611 ± 0. 121,0. 547 ± 0. 109,0. 398 ± 0. 113,0. 320 ± 0. 151 ), with significant difference assessed by F and q test ( P < 0.05). The absorbance rate of PINI mRNA was 0. 983 ± 0.125,0.988 ± 0.127, 0.915 ± 0.157,0.786 ± 0.125,0.608 ± 0.124,0.433 ± 0.130,0.410 ± 0. 158 respectively ( P < 0.05). Conclusion: The expression of PINlmRNA in MG-63 cells could be inhibited by antisense PIN1 gene, and then the expression of PIN1 was reduced and depressed, and so the proliferation of human osteosarcoma cells MG-63 was inhibited.

  7. Empirical prediction and validation of antibacterial inhibitory effects of various plant essential oils on common pathogenic bacteria.

    Science.gov (United States)

    Akdemir Evrendilek, Gulsun

    2015-06-02

    In this study, fractional compound composition, antioxidant capacity, and phenolic substance content of 14 plant essential oils-anise (Pimpinella anisum), bay leaves (Laurus nobilis), cinnamon bark (Cinnamomum verum), clove (Eugenia caryophyllata), fennel (Foeniculum vulgare), hop (Humulus lupulus), Istanbul oregano (Origanum vulgare subsp. hirtum), Izmir oregano (Origanum onites), mint (Mentha piperita), myrtus (Myrtus communis), orange peel (Citrus sinensis), sage (Salvia officinalis), thyme (Thymbra spicata), and Turkish oregano (Origanum minutiflorum)--were related to inhibition of 10 bacteria through multiple linear or non-linear (M(N)LR) models-four Gram-positive bacteria of Listeria innocua, coagulase-negative staphylococci, Staphylococcus aureus, and Bacillus subtilis, and six Gram-negative bacteria of Yersinia enterocolitica, Salmonella Enteritidis, Salmonella Typhimurium, Proteus mirabilis, Escherichia coli O157:H7, and Klebsiella oxytoca. A total of 65 compounds with different antioxidant capacity, phenolic substance content and antibacterial properties were detected with 14 plant essential oils. The best-fit M(N)LR models indicated that relative to anise essential oil, the essential oils of oreganos, cinnamon, and thyme had consistently high inhibitory effects, while orange peel essential oil had consistently a low inhibitory effect. Regression analysis indicated that beta-bisabolene (Turkish and Istanbul oreganos), and terpinolene (thyme) were found to be the most inhibitory compounds regardless of the bacteria type tested. Copyright © 2015 Elsevier B.V. All rights reserved.

  8. Inhibitory effect of Zataria multiflora Boiss. essential oil, alone and in combination with monolaurin, on Listeria monocytogenes.

    Science.gov (United States)

    Raeisi, Mojtaba; Tajik, Hossein; Razavi Rohani, Seyed Mehdi; Tepe, Bektas; Kiani, Hossein; Khoshbakht, Rahem; Shirzad Aski, Hesamaddin; Tadrisi, Hamed

    2016-01-01

    Listeria monocytogenes is one of the major causes of infections in developing countries. In this study, chemical composition and anti-listerial effect of the essential oil of Zataria multiflora Boiss. alone and in combination with monolaurin were evaluated at different pH values (5, 6, and 7) and temperatures (5 ˚C and 30 ˚C). Chemical composition of Zataria multiflora Boiss. essential oil was evaluated by gas chromatography-mass spectrometry (GC-MS) analysis. Minimum inhibitory concentration (MIC) of the essential oil and monolaurin were determined using microbroth dilution method and the interactions of essential oil and monolaurin were determined by the evaluation of fractional inhibitory concentrations (FIC) index. Carvacrol (63.20%) and thymol (15.10%) were found as the main components of the essential oil. The MIC values of the oil and monolaurin at pH 7 and 30 ˚C were measured as 312.50 µg mL(-1) and 125.00 µg mL(-1), respectively. Combination of monolaurin and Z. multiflora essential oil were found to act synergistically (FIC index monolaurin and the essential oil. The lowest MIC value of monolaurin and essential oil was observed at pH 5 and 5 ˚C. According to our results, the oil alone or in combination with monolaurin at low pH and temperature conditions showed a promising inhibitory effect on L. monocytogenes.

  9. Two New Monoterpene Glycosides from Qing Shan Lu Shui Tea with Inhibitory Effects on Leukocyte-Type 12-Lipoxygenase Activity

    Directory of Open Access Journals (Sweden)

    Ding Zhi Fang

    2013-04-01

    Full Text Available We evaluated the inhibitory effect of 12 Chinese teas on leukocyte-type 12-lipoxygenase (LOX activity. Tea catechins such as epigallocatechin gallate have been known to exhibit leukocyte-type 12-LOX inhibition. Qing Shan Lu Shui, which contains lower catechin levels than the other tested teas, suppressed leukocyte-type 12-LOX activity. To characterize the bioactive components of Qing Shan Lu Shui, leukocyte-type 12-LOX inhibitory activity–guided fractionation of the aqueous ethanol extract of the tea was performed, resulting in the isolation of two new monoterpene glycosides: liguroside A (1 and B (2. The structures of compounds 1 and 2 were characterized as (2E,5E-7-hydroperoxy-3,7-dimethyl-2,5-octadienyl-O-(α-L-rhamnopyranosyl-(1″→3′-(4′″-O-trans-p-coumaroyl-β-D-glucopyranoside and (2E,5E-7-hydroperoxy-3,7-dimethyl-2,5-octa-dienyl- O-(α-L-rhamnopyranosyl-(1″→3′-(4′″-O-cis-p-coumaroyl-β-D-glucopyranoside, respectively, based on spectral and chemical evidence. Ligurosides A (1 and B (2 showed inhibitory effects on leukocyte-type 12-LOX activity, with IC50 values of 1.7 and 0.7 μM, respectively.

  10. Degradation products of mangiferin by gamma irradiation with inhibitory effects on NO production.

    Science.gov (United States)

    Jo, Cheorun; Yoon, Kyung Young; Jang, Eun Jin; Kim, Tae Hoon

    2016-10-01

    The xanthone glucoside mangiferin (1) was converted by γ-irradiation into three new compounds, mangiferdiol (2), mangiferinol (3), and isomangiferinol (4). The new compound 2 containing two hydroxymethyl groups instead of a ketone moiety exhibited significantly improved inhibitory activity against nitric oxide production in lipopolysaccharide-stimulated RAW264.7 cells with IC50 value 47.1 ± 1.7 μM, compared to the mother mangiferin.

  11. Modelling inhibitory effects of long chain fatty acids in the anaerobic digestion process

    OpenAIRE

    Flotats Ripoll, Xavier

    2013-01-01

    Mathematical modelling of anaerobic digestion process has been used to give new insights regarding dynamics of the long chain fatty acids (LCFA) inhibition. Previously published experimental data, including batch tests with clay mineral bentonite additions, were used for parameter identification. New kinetics were considered to describe the bio-physics of the inhibitory process, including: i) adsorption of LCFA over granular biomass and ii) specific LCFA substrate (saturated/unsaturated) a...

  12. Cognitive-electrophysiological indices of attentional and inhibitory processing in adults with ADHD: familial effects

    OpenAIRE

    McLoughlin, G; Asherson, P.; Albrecht, B.; Banaschewski, T.; Rothenberger, A.; Brandeis, D; Kuntsi, J.

    2011-01-01

    Background Attention deficit hyperactivity disorder (ADHD) is a common neurodevelopmental disorder that starts in childhood and frequently persists in adults. In a comparison of adults with ADHD and a matched control sample, we previously showed that abnormal inhibitory processing is typically preceded or accompanied by other processing deficits in adult ADHD. We now compare these data further to additional data from first-degree relatives (fathers) of children with ADHD to identify whether t...

  13. Cognitive-electrophysiological indices of attentional and inhibitory processing in adults with ADHD: familial effects

    OpenAIRE

    McLoughlin Gráinne; Asherson Philip; Albrecht Bjoern; Banaschewski Tobias; Rothenberger Aribert; Brandeis Daniel; Kuntsi Jonna

    2011-01-01

    Abstract Background Attention deficit hyperactivity disorder (ADHD) is a common neurodevelopmental disorder that starts in childhood and frequently persists in adults. In a comparison of adults with ADHD and a matched control sample, we previously showed that abnormal inhibitory processing is typically preceded or accompanied by other processing deficits in adult ADHD. We now compare these data further to additional data from first-degree relatives (fathers) of children with ADHD to identify ...

  14. Inhibitory effect of oolong tea polyphenols on glycosyltransferases of mutans Streptococci.

    OpenAIRE

    Nakahara, K; Kawabata, S.; Ono, H; Ogura, K.; Tanaka, T.; Ooshima, T; Hamada, S

    1993-01-01

    Oolong tea extract (OTE) was found to inhibit the water-insoluble glucan-synthesizing enzyme, glucosyltransferase I (GTase-I), of Streptococcus sobrinus 6715. The GTase-inhibitory substance in the OTE was purified successive adsorption chromatography on Diaion HP-21 and HP-20 columns; this was followed by further purification by Sephadex LH-20 column chromatography. A major fraction that inhibited GTase activity (fraction OTF10) was obtained, and the chemical analysis of OTF10 indicated that ...

  15. Effect of subinihibitory and inhibitory concentrations of Plectranthus amboinicus (Lour.) Spreng essential oil on Klebsiella pneumoniae.

    Science.gov (United States)

    Gonçalves, Thially Braga; Braga, Milena Aguiar; de Oliveira, Francisco F M; Santiago, Gilvandete M P; Carvalho, Cibele B M; Brito e Cabral, Paula; de Melo Santiago, Thiago; Sousa, Jeanlex S; Barros, Eduardo Bedê; do Nascimento, Ronaldo Ferreira; Nagao-Dias, Aparecida T

    2012-08-15

    We evaluated the antimicrobial activity and some mechanisms used by subinhibitory and inhibitory concentrations of the essential oil, obtained from leaves of Plectranthus amboinicus, against a standard strain of Klebsiella pneumoniae and 5 multiresistant clinical isolates of the bacteria. The minimal inhibitory concentration (MIC) and minimal bactericidal concentration (MBC), the rate of kill and the pH sensitivity of the essential oil were determined by microdilution tests performed in 96-well plates. Subinhibitory and inhibitory concentrations of the essential oil were tested in order to check its action on K. pneumoniae membrane permeability, capsule expression, urease activity and cell morphology. The MIC and MBC of the essential oil were 0.09±0.01%. A complete inhibition of the bacterial growth was observed after 2 h of incubation with twice the MIC of the essential oil. A better MIC was found when neutral or alkaline pH broth was used. Alteration in membrane permeability was found by the increase of crystal violet uptake when the bacteria were incubated with twice the MIC levels of the essential oil. The urease activity could be prevented when all the subinhibitory concentrations were tested in comparison to the untreated group (pamboinicus can be a good candidate for future research.

  16. Inhibitory effect of natural organic matter or other background constituents on photocatalytic advanced oxidation processes: Mechanistic model development and validation.

    Science.gov (United States)

    Brame, Jonathon; Long, Mingce; Li, Qilin; Alvarez, Pedro

    2015-11-01

    The ability of reactive oxygen species (ROS) to interact with priority pollutants is crucial for efficient water treatment by photocatalytic advanced oxidation processes (AOPs). However, background compounds in water such as natural organic matter (NOM) can significantly hinder targeted reactions and removal efficiency. This inhibition can be complex, interfering with degradation in solution and at the photocatalyst surface as well as hindering illumination efficiency and ROS production. We developed an analytical model to account for various inhibition mechanisms in catalytic AOPs, including competitive adsorption of inhibitors, scavenging of produced ROS at the surface and in solution, and the inner filtering of the excitation illumination, which combine to decrease ROS-mediated degradation. This model was validated with batch experiments using a variety of ROS producing systems (OH-generating TiO2 photocatalyst and H2O2-UV; (1)O2-generating photosensitive functionalized fullerenes and rose bengal) and inhibitory compounds (NOM, tert-butyl alcohol). Competitive adsorption by NOM and ROS scavenging were the most influential inhibitory mechanisms. Overall, this model enables accurate simulation of photocatalytic AOP performance when one or more inhibitory mechanisms are at work in a wide variety of application scenarios, and underscores the need to consider the effects of background constituents on degradation efficiency.

  17. Inhibitory effect of bacteriocin-producing lactic acid bacteria against histamine-forming bacteria isolated from Myeolchi-jeot

    Directory of Open Access Journals (Sweden)

    Eun-Seo Lim

    2016-12-01

    Full Text Available Abstract The objectives of this study were to identify the histamine-forming bacteria and bacteriocin- producing lactic acid bacteria (LAB isolated from Myeolchi-jeot according to sequence analysis of the 16S rRNA gene, to evaluate the inhibitory effects of the bacteriocin on the growth and histamine accumulation of histamine-forming bacteria, and to assess the physico-chemical properties of the bacteriocin. Based on 16S rRNA gene sequences, histamine-forming bacteria were identified as Bacillus licheniformis MCH01, Serratia marcescens MCH02, Staphylococcus xylosus MCH03, Aeromonas hydrophila MCH04, and Morganella morganii MCH05. The five LAB strains identified as Pediococcus acidilactici MCL11, Leuconostoc mesenteroides MCL12, Enterococcus faecium MCL13, Lactobacillus sakei MCL14, and Lactobacillus acidophilus MCL15 were found to produce an antibacterial compound with inhibitory activity against the tested histamine-producing bacteria. The inhibitory activity of these bacteriocins obtained from the five LAB remained stable after incubation at pH 4.0–8.0 and heating for 10 min at 80 °C; however, the bacteriocin activity was destroyed after treatment with papain, pepsin, proteinase K, α-chymotrypsin, or trypsin. Meanwhile, these bacteriocins produced by the tested LAB strains also exhibited histamine-degradation ability. Therefore, these antimicrobial substances may play a role in inhibiting histamine formation in the fermented fish products and preventing seafood-related food-borne disease caused by bacterially generated histamine.

  18. PTP1B inhibitory effects of tridepside and related metabolites isolated from the Antarctic lichen Umbilicaria antarctica.

    Science.gov (United States)

    Seo, Changon; Choi, Yun-Hyeok; Ahn, Jong Seog; Yim, Joung Han; Lee, Hong Kum; Oh, Hyuncheol

    2009-10-01

    The selective inhibition of PTP1B has been widely recognized as a potential drug target for the treatment of type 2 diabetes and obesity. In the course of screening for PTP1B inhibitory natural products, the MeOH extract of the dried sample of the Antarctic lichen Umbilicaria antarctica was found to exhibit significant inhibitory effect, and the bioassay-guided fractionation and purification afforded three related lichen metabolites 1-3. Compounds 1-3 were identified as gyrophoric acid (1), lecanoric acid (2), and methyl orsellinate (3) mainly by analysis of NMR and MS data. These compounds inhibited PTP1B activity with 50% inhibitory concentration values of 3.6 +/- 0.04 microM, 31 +/- 2.7 microM, and 277 +/- 8.6 microM, respectively. Furthermore, the kinetic analysis of PTP1B inhibition by compound 1 suggested that the compound inhibited PTP1B activity in a non-competitive manner.

  19. microRNA-145 Mediates the Inhibitory Effect of Adipose Tissue-Derived Stromal Cells on Prostate Cancer.

    Science.gov (United States)

    Takahara, Kiyoshi; Ii, Masaaki; Inamoto, Teruo; Nakagawa, Takatoshi; Ibuki, Naokazu; Yoshikawa, Yuki; Tsujino, Takuya; Uchimoto, Taizo; Saito, Kenkichi; Takai, Tomoaki; Tanda, Naoki; Minami, Koichiro; Uehara, Hirofumi; Komura, Kazumasa; Hirano, Hajime; Nomi, Hayahito; Kiyama, Satoshi; Asahi, Michio; Azuma, Haruhito

    2016-09-01

    Adipose-derived stromal cell (ASC), known as one of the mesenchymal stem cells (MSCs), is a promising tool for regenerative medicine; however, the effect of ASCs on tumor growth has not been studied sufficiently. We investigated the hypothesis that ASCs have an inhibitory effect on metastatic tumor progression. To evaluate the in vitro inhibitory effect of ASCs on metastatic prostate cancer (PCa), direct coculture and indirect separate culture experiments with PC3M-luc2 cells and human ASCs were performed, and ASCs were administered to PC3M-luc2 cell-derived tumor-bearing nude mice for in vivo experiment. We also performed exosome microRNA (miRNA) array analysis to explore a mechanistic insight into the effect of ASCs on PCa cell proliferation/apoptosis. Both in vitro and in vivo experiments exhibited the inhibitory effect of ASCs on PC3M-luc2 cell proliferation, inducing apoptosis and PCa growth, respectively. Among upregulated miRNAs in ASCs compared with fibroblasts, we focused on miR-145, which was known as a tumor suppressor. ASC-derived conditioned medium (CM) significantly inhibited PC3M-luc2 cell proliferation, inducing apoptosis, but the effect was canceled by miR-145 knockdown in ASCs. ASC miR-145 knockdown CM also reduced the expression of Caspase 3/7 with increased antiapoptotic protein, BclxL, expression in PC3M-luc2 cells. This study provides preclinical data that ASCs inhibit PCa growth, inducing PCa cell apoptosis with reduced activity of BclxL, at least in part, by miR-145, including exosomes released from ASCs, suggesting that ASC administration could be a novel and promising therapeutic strategy in patients with PCa.

  20. Structure-dependent inhibitory effects of green tea catechins on insulin secretion from pancreatic β-cells.

    Science.gov (United States)

    Kaneko, Yukiko K; Takii, Miki; Kojima, Yumiko; Yokosawa, Hiroko; Ishikawa, Tomohisa

    2015-01-01

    The effects of green tea catechins on glucose-stimulated insulin secretion (GSIS) were investigated in the β-cell line INS-1D. Epigallocatechin gallate (EGCG) at 10 µM or gallocatechin gallate (GCG) at 30 µM caused significant inhibitory effects on GSIS, and each of these at 100 µM almost abolished it. In contrast, epicatechin (EC) or catechin (CA) had no effect on GSIS at concentrations up to 100 µM. We thus investigated the structure-activity relationship by using epigallocatechin (EGC) and gallocatechin (GC) containing a trihydroxyl group in the B-ring, and epicatechin gallate (ECG) and catechin gallate (CG) containing the gallate moiety. EGC, GC, and ECG caused an inhibition of GSIS, although significant effects were obtained only at 100 µM. At this concentration, EGC almost abolished GSIS, whereas GC and ECG partially inhibited it. In contrast, CG did not affect GSIS at concentrations up to 100 µM. EGCG also abolished the insulin secretion induced by tolbutamide, an ATP-sensitive K(+) channel blocker, and partially inhibited that induced by 30 mM K(+). Moreover, EGCG, but not EC, inhibited the oscillation of intracellular Ca(2+) concentration induced by 11.1 mM glucose. These results suggest that some catechins at supraphysiological concentrations have inhibitory effects on GSIS, the potency of which depends on their structure; the order of potency was EGCG>GCG>EGC>GC≈ECG. The inhibitory effects seem to be mediated by the inhibition of voltage-dependent Ca(2+) channels, which is caused, at least in part, by membrane hyperpolarization resulting from the activation of K(+) channels.

  1. Inhibitory effect of Huangqi Zhechong decoction on liver fibrosis in rat

    Institute of Scientific and Technical Information of China (English)

    Shuang-Suo Dang; Xiao-Li Jia; Yan-An Cheng; Yun-Ru Chen; En-Qi Liu; Zong-Fang Li

    2004-01-01

    AIM: To assess the inhibitory effect of Huangqi Zhechong decoction on hepatic fibrosis in rats induced by CCl4 plus alcohol and high fat low protein diet.METHODS: Male SD rats were randomly divided into hepatic fibrosis model group, control group and 3 treatment groups consisting of 12 rats in each group. Except for the normalcontrol group, all the rats were subcutaneously injected with CCl4 at a dosage of 3 mL/kg. In 3 treated groups, either high-dose group (9 mL/kg), or medium-dose group (6 mL/kg),or low-dose group (3 mL/kg) was daily gavaged with Huangqi Zhechong decoction, and saline vehicle was given to model and normal control rats. Enzyme-linked immunosorbent assay (ELISA) and biochemical examinations were used to determine the changes of alanine aminotransferase (ALT),aspartate aminotransferase (AST), hyaluronic acid (HA),laminin (LN), type-T-procollagen-N-peptide (PITIP), and type Ⅳ collagen content in serum, and hydroxyproline (Hyp)content in liver after sacrificing the rats. Pathologic changes,particularly fibrosis were examined by hematoxylin and eosin (HE) and Van Gieson staining. RESULTS: Compared with the model control group; serumALT, AST, HA, LN, PITIP and type Ⅳ collagen levels dropped markedly in Huangqi Zhechong decoction groups, especially in the medium-dose Huangqi Zhechong decoction group (1 954±576 U/L vs 759±380 U/L, 2 735±786 U/L vs 1 259±829 U/L, 42.74±7.04 ng/mL vs 20.68±5.85 ng/mL,31.62±5.84 ng/mL vs 14.87±1.45 ng/mL, 3.26±0.69 ng/mL vs 1.47±0.46 ng/mL, 77.68±20.23 ng/mL vs 25.64±4.68 ng/mL, respectively) (P<0.05). The Hyp content in liver tissue was also markedly decreased (26.47±11.24 mg/mgprot vs 9.89±3.74 mg/mgprot) (P<0.01). Moreover, the stage of the rat liver fibrosis in Huangqi Zhechong decoction groups was lower than that in model group, and more dramatic drop was observed in medium-dose Huangqi Zhechong decoction group (P<0.01).CONCLUSION: Huangqi Zhechong decoction can inhibit hepatic fibrosis resulted

  2. Inhibitory effect of three C-glycosylflavonoids from Cymbopogon citratus (Lemongrass) on human low density lipoprotein oxidation.

    Science.gov (United States)

    Orrego, Roxana; Leiva, Elba; Cheel, José

    2009-09-30

    This study assessed the inhibitory effect of three C-glycosylflavonoids from Cymbopogon citratus leaves--isoorientin (1), swertiajaponin (2) and isoorientin 2"-Orhamnoside (3)--on human LDL oxidation. Isolated LDL was incubated with compounds 1-3 and the kinetics of lipid peroxidation were assessed by conjugated diene and malondialdehyde-thiobarbituric acid reactive substances (MDA-TBARS) formation after addition of copper ions. Significant differences (p isoorientin (1) is an effective inhibitor of in vitro LDL oxidation. As oxidative damage to LDL is a key event in the formation of atherosclerotic lesions, the use of this natural antioxidant may be beneficial to prevent or attenuate atherosclerosis.

  3. Effects of sub-inhibitory concentrations of German chamomile (Matricaria recotita extracts on the activity of catalase enzyme of S. aureus

    Directory of Open Access Journals (Sweden)

    gholamreza Goudarzi

    2005-12-01

    Findings: The extract showed growth inhibitory effect at dilution of and at dilution of showed bactericidal effect on standard strain. Dilutions of and as sub-inhibitory concentrations, decreased catalase activity prominently. Conclusion: Significant decrease of catalase activity at sub-inhibitory concentrations of this extract shows that this extract affects the production of catalase at different levels such as transcription, translation or transport and etc. Therefore, it is necessary to further study this extract. This enzyme can be a new target for production of novel antimicrobial agents.

  4. Inhibitory effects of synthetic cannabinoid WIN55, 212-2 on nicotine-activated currents in rat trigeminal ganglion neurons

    Institute of Scientific and Technical Information of China (English)

    Yongli Lu; Changjin Liu; Hongwei Yang

    2011-01-01

    Cannabinoid and nicotinic acetylcholine receptors are strongly associated with algesia. Previous studies in our laboratory have reported inhibitory effects of synthetic cannabinoid WIN55, 212-2 on nicotine-activated currents (/nic), but the underlying mechanisms remain poorly understood. The present study used whole-cell patch clamp techniques to investigate the modulatory effects of synthetic cannabinoid WIN55, 212-2 on /nic in cultured rat trigeminal ganglion neurons. The results revealed several major findings: WIN55, 212-2 inhibited /nic in rat trigeminal ganglion neurons. In addition, when WIN55, 212-2 (3 μmol/L) was applied simultaneously with nicotine (100 μmol/L), the inhibition of WIN55, 212-2 on /nic was reversible, concentration-dependent and voltage-independent. This effect was not mediated by CB1, CB2 or VR1 receptors; neither the selective CB1 receptor antagonist AM281, CB2 receptor antagonist AM630 nor VR1 receptor antagonist capsazepine reduced the inhibitory effect of WIN55, 212-2. Further, the inhibition of nicotinic responses by WIN55, 212-2 was not sensitive to the membrane permeable cyclic adenosine monophosphate (cAMP) analog 8-Br-cAMP. The G-protein inhibitor GDP-β-S (1 mmol/L) did not block the inhibitory effects of WIN55, 212-2 on /nic, excluding the involvement of G-protein mediation. The results suggested that WIN55, 212-2 inhibits/nic directly via the neuronal nicotinic acetylcholine receptor, and that this inhibition is non-competitive. WIN55, 212-2 did not act as an open channel blocker of the neuronal nicotinic acetylcholine receptor, and did not affect the desensitization of /nic. The results suggest that nicotine receptors may be physically plugged from outside the membrane by drugs containing WIN55, 212-2.

  5. Glycolic acid chemical peeling improves inflammatory acne eruptions through its inhibitory and bactericidal effects on Propionibacterium acnes.

    Science.gov (United States)

    Takenaka, Yuko; Hayashi, Nobukazu; Takeda, Mikiko; Ashikaga, Sayaka; Kawashima, Makoto

    2012-04-01

    Glycolic acid chemical peeling is effective for treating comedones, and some clinical data show that it also improves inflammatory eruptions. The purpose of this study was to identify the mechanism of glycolic acid chemical peeling to improve inflammatory acne. To assess growth inhibitory and bactericidal effects of glycolic acid on Propionibacterium acnes in vitro, we used an agar diffusion method and a time-kill method. To reveal bactericidal effects in vivo, we established an agar-attached method which correlated well with the ordinary swab-wash method, and we used the agar-attached method to compare the numbers of propionibacteria on the cheek treated with glycolic acid chemical peeling. Our results show that 30% glycolic acid (at pH 1.5, 3.5 and 5.5) formed growth inhibitory circles in the agar diffusion method, but the diameters of those circles were smaller than with 1% nadifloxacin lotion or 1% clindamycin gel. In the time-kill method, 30% glycolic acid (at pH 1.5 and 3.5) or 1% nadifloxacin lotion reduced the number of P. acnes to less than 100 CFU/mL within 5 min. In contrast, in 30% glycolic acid (at pH 5.5) or in 1% clindamycin gel, P. acnes survived for more than 4 h. Chemical peeling with 35% glycolic acid (at pH 1.2) decreased the number of propionibacteria on the cheeks of patients compared with untreated controls (P glycolic acid has moderate growth inhibitory and bactericidal effects on P. acnes, and that chemical peeling with glycolic acid works on inflammatory acne via those effects.

  6. Evaluation of commercial boric acid containing vials for urine culture: low risk of contamination and cost effectiveness considerations.

    Science.gov (United States)

    Appannanavar, Suma B; Biswal, Manisha; Rajkumari, Nonika; Mohan, Balvinder; Taneja, Neelam

    2013-01-01

    Urine culture is a gold standard in the diagnosis of urinary tract infection. Clean catch midstream urine collection and prompt transportation is essential for appropriate diagnosis. Improper collection and delay in transportation leads to diagnostic dilemma. In developing countries, higher ambient temperatures further complicate the scenario. Here, we have evaluated the role of boric acid as a preservative for urine samples prior to culture in female patients attending outpatient department at our center. Consecutive 104 urine samples were cultured simultaneously in plain uricol (Control-C) and boric acid containing tubes from Becton Dickinson urine culture kit (Boric acid group-BA). In the real-time evaluation, we found that in almost 57% (59/104) of the urine samples tested, it was more effective in maintaining the number of the organisms as compared to samples in the container without any preservative. Our in vitro study of simulated urine cultures revealed that urine samples could be kept up to 12 h before culture in the preservative without any inhibitory effect of boric acid. Though the use of boric acid kit may marginally increase the initial cost but has indirect effects like preventing delays in treatment and avoidance of false prescription of antibiotics. If the man-hours spent on repeat investigations are also taken into consideration, then the economic cost borne by the laboratory would also decrease manifold with the use of these containers.

  7. Evaluation of commercial boric acid containing vials for urine culture: Low risk of contamination and cost effectiveness considerations

    Directory of Open Access Journals (Sweden)

    Suma B Appannanavar

    2013-01-01

    Full Text Available Background: Urine culture is a gold standard in the diagnosis of urinary tract infection. Clean catch midstream urine collection and prompt transportation is essential for appropriate diagnosis. Improper collection and delay in transportation leads to diagnostic dilemma. In developing countries, higher ambient temperatures further complicate the scenario. Here, we have evaluated the role of boric acid as a preservative for urine samples prior to culture in female patients attending outpatient department at our center. Materials and Method: Consecutive 104 urine samples were cultured simultaneously in plain uricol (Control-C and boric acid containing tubes from Becton Dickinson urine culture kit (Boric acid group-BA. Results: In the real-time evaluation, we found that in almost 57% (59/104 of the urine samples tested, it was more effective in maintaining the number of the organisms as compared to samples in the container without any preservative. Our in vitro study of simulated urine cultures revealed that urine samples could be kept up to 12 h before culture in the preservative without any inhibitory effect of boric acid. Though the use of boric acid kit may marginally increase the initial cost but has indirect effects like preventing delays in treatment and avoidance of false prescription of antibiotics. If the man-hours spent on repeat investigations are also taken into consideration, then the economic cost borne by the laboratory would also decrease manifold with the use of these containers.

  8. Geranylated flavanones from Paulownia coreana and their inhibitory effects on nitric oxide production.

    Science.gov (United States)

    Jin, Qinghao; Lee, Chul; Lee, Jin Woo; Lee, Dongho; Kim, Youngsoo; Hong, Jin Tae; Kim, Jin Sook; Kim, Joo-Hwan; Lee, Mi Kyeong; Hwang, Bang Yeon

    2015-01-01

    The activity-guided fractionation of the MeOH extract of the flower of Paulownia coreana led to the isolation of a new geranylated flavanone, 3'-O-methyl-5'-hydroxydiplacol (1), along with 10 known compounds (2-11). Their structures were determined using spectroscopic techniques, which included one and two dimensional (1- and 2D)-NMR. Among the isolates, compounds 1-6 showed potent inhibitory activities against lipopolysaccharide (LPS)-induced nitric oxide production with IC50 values ranging 1.48 to 16.66 µM.

  9. NONLINEAR PROPERTY MEMBRANE RECTIFIER POTASSIUM CHANNEL AND INHIBITORY EFFECTS OF OXYGEN FREE RADICAL

    Institute of Scientific and Technical Information of China (English)

    鲍光宏; 于德洁; 刘宇; 刘东梅

    1996-01-01

    There are at least eight kinds of different potassium chennels on cardiac cell membrane. This paperpresents a nonlinear property membrane outward; current going rectifying potassium channel and the in-hibitory efeets of oxygen free radical on this channel. The current-vohage relation of this nonlimmr-mem-brahe can be defined by an equation I=8a3/(0.01v2+4a2)2 and the maximum conductance of this channel is-75.3pS.

  10. Anacardium occidentale Linn. (Anacardiaceae) stem bark extract induces hypotensive and cardio-inhibitory effects in experimental animal models.

    Science.gov (United States)

    Tchikaya, Francis Olivier; Bantsielé, Guy Bernard; Kouakou-Siransy, Gisèle; Datté, Jacques Yao; Yapo, Paul Angoue; Zirihi, Noel Guedé; Offoumou, Michel Atté

    2011-01-01

    Anacardium occidentale Linn. (Anacardiaceae) is a plant largely used in Africa for the treatment of different diseases. In Côte d'Ivoire it's commonly used for the treatment of hypertension. The present study was carried out in order to assess the effects of Anacardium occidentale extract (ANOE) on cardiovascular parameters in animal models. A mercury manometer kymograph of Ludwig was used to measure the blood pressure of normotensive rabbits in control conditions (normal physiological solution) and under the influence of ANOE. The contractile activity of an isolated rat heart was also measured in control conditions and under the influence of ANOE in different physiological media using a modified Langendhorff (1895) apparatus. The aqueous Anacardium occidentale (ANOE) bark extract applied intravenously in different doses (12, 40, 90, and 167 mg/kg b.w.), produced a significant dose-dependent decrease in blood pressure of previously normotensive rabbits (up to 89% vs control). Atropine (1 mg/ml) pre-treatment failed to reverse the hypotensive effects elicited by the extract. ANOE applied to isolated rat heart preparations in different concentrations (0.01, 0.1, 1.0, and 10 µg/ml) induced negative inotropic and chronotropic effects. Atropine pre-treatment of heart preparations (0.1 µg/ml) failed to reverse the negative effects induced by ANOE. The extract's action on heart contractile activity studied in modified culture media further confirmed its cardio-inhibitory effects. ANOE induced strong hypotensive and cardio-inhibitory effects in animal models.

  11. Papain-like protease (PLpro) inhibitory effects of cinnamic amides from Tribulus terrestris fruits.

    Science.gov (United States)

    Song, Yeong Hun; Kim, Dae Wook; Curtis-Long, Marcus John; Yuk, Heung Joo; Wang, Yan; Zhuang, Ningning; Lee, Kon Ho; Jeon, Kwon Seok; Park, Ki Hun

    2014-01-01

    Tribulus terrestris fruits are well known for their usage in pharmaceutical preparations and food supplements. The methanol extract of T. terrestris fruits showed potent inhibition against the papain-like protease (PLpro), an essential proteolylic enzyme for protection to pathogenic virus and bacteria. Subsequent bioactivity-guided fractionation of this extract led to six cinnamic amides (1-6) and ferulic acid (7). Compound 6 emerged as new compound possessing the very rare carbinolamide motif. These compounds (1-7) were evaluated for severe acute respiratory syndrome coronavirus (SARS-CoV) PLpro inhibitory activity to identify their potencies and kinetic behavior. Compounds (1-6) displayed significant inhibitory activity with IC50 values in the range 15.8-70.1 µM. The new cinnamic amide 6 was found to be most potent inhibitor with an IC50 of 15.8 µM. In kinetic studies, all inhibitors exhibited mixed type inhibition. Furthermore, the most active PLpro inhibitors (1-6) were proven to be present in the native fruits in high quantities by HPLC chromatogram and liquid chromatography with diode array detection and electrospray ionization mass spectrometry (LC-DAD-ESI/MS).

  12. Effective Suppression of Pathological Synchronization in Cortical Networks by Highly Heterogeneous Distribution of Inhibitory Connections

    Science.gov (United States)

    Kada, Hisashi; Teramae, Jun-Nosuke; Tokuda, Isao T.

    2016-01-01

    Even without external random input, cortical networks in vivo sustain asynchronous irregular firing with low firing rate. In addition to detailed balance between excitatory and inhibitory activities, recent theoretical studies have revealed that another feature commonly observed in cortical networks, i.e., long-tailed distribution of excitatory synapses implying coexistence of many weak and a few extremely strong excitatory synapses, plays an essential role in realizing the self-sustained activity in recurrent networks of biologically plausible spiking neurons. The previous studies, however, have not considered highly non-random features of the synaptic connectivity, namely, bidirectional connections between cortical neurons are more common than expected by chance and strengths of synapses are positively correlated between pre- and postsynaptic neurons. The positive correlation of synaptic connections may destabilize asynchronous activity of networks with the long-tailed synaptic distribution and induce pathological synchronized firing among neurons. It remains unclear how the cortical network avoids such pathological synchronization. Here, we demonstrate that introduction of the correlated connections indeed gives rise to synchronized firings in a cortical network model with the long-tailed distribution. By using a simplified feed-forward network model of spiking neurons, we clarify the underlying mechanism of the synchronization. We then show that the synchronization can be efficiently suppressed by highly heterogeneous distribution, typically a lognormal distribution, of inhibitory-to-excitatory connection strengths in a recurrent network model of cortical neurons. PMID:27803659

  13. Cognitive-electrophysiological indices of attentional and inhibitory processing in adults with ADHD: familial effects

    Directory of Open Access Journals (Sweden)

    McLoughlin Gráinne

    2011-07-01

    Full Text Available Abstract Background Attention deficit hyperactivity disorder (ADHD is a common neurodevelopmental disorder that starts in childhood and frequently persists in adults. In a comparison of adults with ADHD and a matched control sample, we previously showed that abnormal inhibitory processing is typically preceded or accompanied by other processing deficits in adult ADHD. We now compare these data further to additional data from first-degree relatives (fathers of children with ADHD to identify whether this pattern of abnormal processing shares familial influences with ADHD in adults. Methods Using a family design, we compared 20 fathers of children with the combined subtype of ADHD with 21 adults with ADHD combined subtype and 20 controls in event-related potential indices of preparatory states and subsequent response inhibition processing as elicited by a cued continuous performance task. Results Fathers of children with ADHD exhibited significantly weaker orienting attention to cues and inhibitory processing than the controls but not the ADHD sample. Conclusions These findings provide evidence for the familial association of attentional orienting and response inhibition processes with ADHD in adults and indicate a familial and neurobiological link between ADHD in children and adults.

  14. Cytotoxic and Growth Inhibitory Effects of the Methanol Extract of Tridax procumbens Linn (Asteraceae

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    Olowojoba J

    2013-05-01

    Full Text Available Research into medicinal plants used in treating tumor-related ailments has become imperative due to the emergence of various forms of cancer diseases. Tridax procubens is one of such medicinal plants indicated in traditional herbal medicine as one of the plants used in treating tumor-related ailments. This claim was examined using bench-top assay methods involving the cytotoxicity of the methanol extract of the plant to tadpoles of Raniceps ranninus for a period of 24 hr at concentrations between 10-400 µg/ml and the growth inhibitory assay between 1-30 µg/ml. After 24 h, the crude methanol extract and the chloroform fraction produced the highest cytotoxicity of 63.33 ± 1.33 and 100 % respectively at 400 μg/ml. On the growth inhibitory assay, after 96 h, the controls had an average length of 58.12 ± 5.68 mm, whereas the seeds treated with 30mg/ml of the crude extract had an average length of 1.63 ± 0.32 mm, indicating 97.19 % reduction in length. At the same concentration, the chloroform and the aqueous fractions showed 86.58 and 100 % inhibitions. The plant material was observed to contain tannins, saponins and flavonoids, cardiac glycosides and anthraquinone. The result of this work supports the ethno-medicinal use of the plant in preparing recipes for tumor-related ailments.

  15. Antibacterial and COX-1 Inhibitory Effect of Medicinal Plants from the Pamir Mountains, Afghanistan

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    Anne S. Jeppesen

    2012-10-01

    Full Text Available Plants used to treat inflammatory ailments, pain, fever and infections in the Pamir Mountains in northeastern Afghanistan, were tested for antibacterial and COX-1 inhibitory activity. Water and ethanol extracts of 20 species were tested for antibacterial activity against two gram positive and two gram negative bacteria. The ethanol extract of Arnebia guttata inhibited Staphylococcus aureus with a MIC of 6 µg/mL. Water and ethanol extracts of Ephedra intermedia and the ethanol extracts of Lagochilus cabulicus and Peganum harmala inhibited Staphylococcus aureus at 0.5 mg/mL, and the P. harmala extract further inhibited the growth of Bacillus subtilis and E. coli, also with MICs of 0.5 mg/mL. Ethanol extracts of Artemisia persica (IC50: 0.5 µg/mL, Dragocephalum paulsenii (IC50: 0.5 µg/mL, Ephedra intermedia (IC50: 3.8 µg/mL, Hyoscyamus pusillus, Nepeta parmiriensis (IC50: 0.7 µg/mL and Rumex patientia subsp. pamiricus (IC50: 3.5 µg/mL exhibited COX-1 inhibitory activity. The observed in vitro activities support the use of some of the plant species in the traditional medicine systems of the Pamir Mountains.

  16. Hypocholesterolemic Effect and In Vitro Pancreatic Lipase Inhibitory Activity of an Opuntia ficus-indica Extract.

    Science.gov (United States)

    Padilla-Camberos, Eduardo; Flores-Fernandez, Jose Miguel; Fernandez-Flores, Ofelia; Gutierrez-Mercado, Yanet; Carmona-de la Luz, Joel; Sandoval-Salas, Fabiola; Mendez-Carreto, Carlos; Allen, Kirk

    2015-01-01

    Cholesterol control is fundamental for prevention of cardiovascular disorders. In this work, the hypocholesterolemic activity of an aqueous Opuntia ficus-indica extract (AOE) was tested in triton-induced mice. The inhibitory activity on pancreatic lipase enzyme was evaluated in vitro by the same extract. Furthermore, polyphenol content of the extract was evaluated. Hypercholesterolemia was induced in three groups of mice by intraperitoneal administration of Triton WR-1339. After induction of hypercholesterolemia, the groups were treated with an AOE (500 mg/kg) and saline solution and the positive control group with orlistat, respectively. Cholesterol levels were measured 24 h later in peripheral blood. The levels of blood cholesterol after administration of AOE significantly decreased compared to negative control. The inhibitory activity of AOE on pancreatic lipase enzyme was evaluated at concentrations from 60 to 1000 μg/mL. The AOE inhibited the pancreatic lipase with an IC50 = 588.5 μg/mL. The AOE had a high content of polyphenolic compounds. These results show that AOE is able to prevent hypercholesterolemia by pancreatic lipase inhibition, in part due to its polyphenolic compounds.

  17. α-Glucosidase inhibitory activity and cytotoxic effects of some cyclic urea and carbamate derivatives.

    Science.gov (United States)

    Popović-Djordjević, Jelena B; Jevtić, Ivana I; Grozdanić, Nadja Dj; Šegan, Sandra B; Zlatović, Mario V; Ivanović, Milovan D; Stanojković, Tatjana P

    2017-12-01

    The inhibitory activities of selected cyclic urea and carbamate derivatives (1-13) toward α-glucosidase (α-Gls) in in vitro assay were examined in this study. All examined compounds showed higher inhibitory activity (IC50) against α-Gls compared to standard antidiabetic drug acarbose. The most potent was benzyl (3,4,5-trimethoxyphenyl)carbamate (12) with IC50 = 49.85 ± 0.10 µM. In vitro cytotoxicity of the investigated compounds was tested on three human cancer cell lines HeLa, A549 and MDA-MB-453 using MTT assay. The best antitumour activity was achieved with compound 2 (trans-5-phenethyl-1-phenylhexahydro-1H-imidazo[4,5-c]pyridin-2(3H)-one) against MDA-MB-453 human breast cancer cell line (IC50 = 83.41 ± 1.60 µM). Cyclic ureas and carbamates showed promising anti-α-glucosidase activity and should be further tested as potential antidiabetic drugs. The PLS model of preliminary QSAR study indicated that, in planing the future synthesis of more potent compounds, the newly designed should have the substituents capable of polar interactions with receptor sites in various positions, while avoiding the increase of their lipophilicity.

  18. Hypocholesterolemic Effect and In Vitro Pancreatic Lipase Inhibitory Activity of an Opuntia ficus-indica Extract

    Directory of Open Access Journals (Sweden)

    Eduardo Padilla-Camberos

    2015-01-01

    Full Text Available Cholesterol control is fundamental for prevention of cardiovascular disorders. In this work, the hypocholesterolemic activity of an aqueous Opuntia ficus-indica extract (AOE was tested in triton-induced mice. The inhibitory activity on pancreatic lipase enzyme was evaluated in vitro by the same extract. Furthermore, polyphenol content of the extract was evaluated. Hypercholesterolemia was induced in three groups of mice by intraperitoneal administration of Triton WR-1339. After induction of hypercholesterolemia, the groups were treated with an AOE (500 mg/kg and saline solution and the positive control group with orlistat, respectively. Cholesterol levels were measured 24 h later in peripheral blood. The levels of blood cholesterol after administration of AOE significantly decreased compared to negative control. The inhibitory activity of AOE on pancreatic lipase enzyme was evaluated at concentrations from 60 to 1000 μg/mL. The AOE inhibited the pancreatic lipase with an IC50 = 588.5 μg/mL. The AOE had a high content of polyphenolic compounds. These results show that AOE is able to prevent hypercholesterolemia by pancreatic lipase inhibition, in part due to its polyphenolic compounds.

  19. Hypocholesterolemic Effect and In Vitro Pancreatic Lipase Inhibitory Activity of an Opuntia ficus-indica Extract

    Science.gov (United States)

    Flores-Fernandez, Jose Miguel; Fernandez-Flores, Ofelia; Gutierrez-Mercado, Yanet; Carmona-de la Luz, Joel; Sandoval-Salas, Fabiola; Mendez-Carreto, Carlos

    2015-01-01

    Cholesterol control is fundamental for prevention of cardiovascular disorders. In this work, the hypocholesterolemic activity of an aqueous Opuntia ficus-indica extract (AOE) was tested in triton-induced mice. The inhibitory activity on pancreatic lipase enzyme was evaluated in vitro by the same extract. Furthermore, polyphenol content of the extract was evaluated. Hypercholesterolemia was induced in three groups of mice by intraperitoneal administration of Triton WR-1339. After induction of hypercholesterolemia, the groups were treated with an AOE (500 mg/kg) and saline solution and the positive control group with orlistat, respectively. Cholesterol levels were measured 24 h later in peripheral blood. The levels of blood cholesterol after administration of AOE significantly decreased compared to negative control. The inhibitory activity of AOE on pancreatic lipase enzyme was evaluated at concentrations from 60 to 1000 μg/mL. The AOE inhibited the pancreatic lipase with an IC50 = 588.5 μg/mL. The AOE had a high content of polyphenolic compounds. These results show that AOE is able to prevent hypercholesterolemia by pancreatic lipase inhibition, in part due to its polyphenolic compounds. PMID:26078966

  20. Analysis of the Inhibitory Effect of Gypenoside on Na+,K+-ATPase in Rats' Heart and Brain and Its Kinetics

    Institute of Scientific and Technical Information of China (English)

    HAN Xiao-yan; WEI Hong-bo; ZHANG Fu-cheng

    2007-01-01

    ObjectiYe: To study the effects of gypenoside (Gyp) on the activity of microsomal Na+,K+-ATPase in rat's heart and brain in vitro. Methods: The microsomal Na+, K+-ATPase was prepared from rat's heart and brain by differential centrifugation. The activity of microsomal Na+, K+-ATPase was assayed by colorimetric technique. Enzyme kinetic analysis method was used to analyze the effect of Gyp on the microsomal Na+, K+-ATPase of rats. Results: Gyp reversibly inhibited the brain and heart's microsomal Na+, K+-ATPase in a concentration-dependent manner, and showed a more potent effect on enzyme in the brain. The IC50 of Gyp for the heart and brain were 58.79± 8.05 mg/L and 52.07 ±6.25 mg/L, respectively. The inhibition was enhanced by lowering the Na+, or K+ concentrations or increasing the ATP concentration. Enzyme kinetic studies indicated that the inhibitory effect of Gyp on the enzyme is like that of competitive antagonist of Na+, the counter-competitive inhibitor for the substrate ATP, and the mixed-type inhibitor for K+. Conclusion: Gyp displays its cardiotonic and central inhibitory effects by way of inhibiting heart and brain's microsomal Na+, K+-ATPase activities in rats.

  1. THE ROLE OF BRAIN-STEM DISCENDING INHIBITORY SYSTEM IN THE ANTINOCICEPTIVE EFFECT ELICITED BY MUSCLE SPINDLE AFFERENTS

    Institute of Scientific and Technical Information of China (English)

    2001-01-01

    Objective To analyse the antinociceptive effect of muscle spindle afferents and the involved mechanism.Methods The single unit of wide dynamic range(WDR) neurons in the spinal cord dorsal horn were recorded extracelluarly.The effects of muscle spindle afferents elicited by intravenous administration of succinylcholine (Sch) on nociceptive responses (C-fibres-evoked responses,C-responses) of WDR neurons were observed before and after bilateral lesions of ventrolateral periaqueduct gray (PAG).And the effects of muscle spindle afferents on the spontaneous discharge of the tail-flick related cell in the rostral ventro medial medulla (RVM) and on the spontaneous discharge of the PAG neurons were observed.Results The C-responses of WDR neurons were significantly inhibited by muscle spindle afferents,and the inhibitory effects were reduced by bilateral lesions of ventrolateral PAG.The spontaneous discharge of the off-cell in the RVM was excited while the on-cell was inhibited by intravenous administration of Sch.The spontaneous discharge of the PAG neurons were excited by muscle spindle afferents.Conclusion Muscle spindle afferents show a distinct effect of antinociception.PAG-RVM descending inhibitory system may play an important role in this nociceptive modulative mechanism.

  2. In vitro α-amylase inhibitory activity and in vivo hypoglycemic effect of methanol extract of Citrus macroptera Montr. fruit

    Institute of Scientific and Technical Information of China (English)

    Nizam Uddin; Md. Rakib Hasan; Md. Monir Hossain; Arjyabrata Sarker; A.H.M. Nazmul Hasan; A.F.M. Mahmudul Islam; Mohd. Motaher H. Chowdhury; Md. Sohel Rana

    2014-01-01

    Objective: To investigate the therapeutic effects of methanol extract of Citrus macroptera Montr. fruit in α-amylase inhibitory activity (in vitro) and hypoglycemic activity in normal and glucose induced hyperglycemic rats (in vivo). Methods: Fruits of Citrus macroptera without rind was extracted with pure methanol following cold extraction and tested for presence of phytochemical constituents, α-amylase inhibitory activity, and hypoglycemic effect in normal rats and glucose induced hyperglycemic rats.Results:showed that fruit extract had moderate α-amylase inhibitory activity [IC50 value=(3.638±0.190) mg/mL] as compared to acarbose. Moreover at 500 mg/kg and 1 000 mg/kg doses fruit extract significantly (P<0.05 and P<0.01 respectively) reduced fasting blood glucose level in normal rats as compared to glibenclamide (5 mg/kg). In oral glucose tolerance test, 500 mg/kg dose significantly reduced blood glucose level (P<0.05) at 2 h but 1000 mg/kg dose significantly reduced blood glucose level at 2 h and 3 h (P<0.05 and P<0.01 respectively) whereas glibenclamide (5 mg/kg) significantly reduced glucose level at every hour after administration. Overall time effect is also considered extremely significant with F value=23.83 and P value=0.0001 in oral glucose tolerance test.Conclusion:These findings suggest that the plant may be a potential source for the development Presence of saponin, steroid and terpenoid were identified in the extract. The results of new oral hypoglycemic agent.

  3. INHIBITORY EFFECT OF BOSCHNIAKIA ROSSICA ON DEN-INDUCED PRECANCEROUS HEPATIC FOCI AND ITS ANTIOXIDATIVE ACTIVITIES IN RATS

    Institute of Scientific and Technical Information of China (English)

    YIN Zong-zhu; JIN Hai-ling; SHEN Ming-hua; LI Tian-zhu; QUAN Ji-shu

    1999-01-01

    Objective: To investigate the inhibitory effect of Boschniakia rossica(BR) on rat precancerous hepatic foci induced by diethylnitrosamine (DEN) and its antioxidative activities. Methods: The expression of tumor markerplacental form glutathione S-transferase (GST-P), p53 and p21 protein were investigated by immunohistochemistry techniques using ABC method. TNF-α was measured by ELISA and antioxidative activities of SOD, MDA, GSH-Px,GST and CAT were investigated by colorimetric method in rat serum and mitochondria of liver cells. Results: The 500 mg/kg of BR-H2O extract fraction from BR-methanol extract had inhibitory effect on the formation of DEN-induced GST-P-positive foci in rat liver and the expression of mutant p53 and p21 protein was lower than that of hepatic precancerous lesions. The serum TNF-α was increased by the administration of BR extract in the early stage of chemical hepatocarcinogenesis in rat livers. The serum and liver cells mitochondria activities of SOD and GSH-Px rose again in rats administered with BR-H2O extract and the increasing activity of GST and content of MDA in the hepatic precancerous were decreased by the BR-H2O extract. Conclusion: These results indicated that BR-H2O extract has inhibitory effect on DEN-induced precancerous hepatic foci in rats and induced TNF-α production in rats. The antioxidative action was exhibited by the administration of BR-H2O extract in the early stage of chemical hepatocarcinogenesis in rat livers.

  4. General and Food-Specific Inhibitory Control As Moderators of the Effects of the Impulsive Systems on Food Choices.

    Science.gov (United States)

    Zhang, Xuemeng; Chen, Shuaiyu; Chen, Hong; Gu, Yan; Xu, Wenjian

    2017-01-01

    The present study aimed to extend the application of the reflective-impulsive model to restrained eating and explore the effect of automatic attention (impulsive system) on food choices. Furthermore, we examined the moderating effects of general inhibitory control (G-IC) and food-specific inhibitory control (F-IC) on successful and unsuccessful restrained eaters (US-REs). Automatic attention was measured using "the EyeLink 1000," which tracked eye movements during the process of making food choices, and G-IC and F-IC were measured using the Stop-Signal Task. The results showed that food choices were related to automatic attention and that G-IC and F-IC moderated the predictive relationship between automatic attention and food choices. Furthermore, among successful restrained eaters (S-REs), automatic attention to high caloric foods did not predict food choices, regardless of whether G-IC or F-IC was high or low. Whereas food choice was positively correlated with automatic attention among US-REs with poor F-IC, this pattern was not observed in those with poor G-IC. In conclusion, the S-REs had more effective self-management skills and their food choices were affected less by automatic attention and inhibitory control. Unsuccessful restrained eating was associated with poor F-IC (not G-IC) and greater automatic attention to high caloric foods. Thus, clinical interventions should focus on enhancing F-IC, not G-IC, and on reducing automatic attention to high caloric foods.

  5. General and Food-Specific Inhibitory Control As Moderators of the Effects of the Impulsive Systems on Food Choices

    Directory of Open Access Journals (Sweden)

    Xuemeng Zhang

    2017-05-01

    Full Text Available The present study aimed to extend the application of the reflective-impulsive model to restrained eating and explore the effect of automatic attention (impulsive system on food choices. Furthermore, we examined the moderating effects of general inhibitory control (G-IC and food-specific inhibitory control (F-IC on successful and unsuccessful restrained eaters (US-REs. Automatic attention was measured using “the EyeLink 1000,” which tracked eye movements during the process of making food choices, and G-IC and F-IC were measured using the Stop-Signal Task. The results showed that food choices were related to automatic attention and that G-IC and F-IC moderated the predictive relationship between automatic attention and food choices. Furthermore, among successful restrained eaters (S-REs, automatic attention to high caloric foods did not predict food choices, regardless of whether G-IC or F-IC was high or low. Whereas food choice was positively correlated with automatic attention among US-REs with poor F-IC, this pattern was not observed in those with poor G-IC. In conclusion, the S-REs had more effective self-management skills and their food choices were affected less by automatic attention and inhibitory control. Unsuccessful restrained eating was associated with poor F-IC (not G-IC and greater automatic attention to high caloric foods. Thus, clinical interventions should focus on enhancing F-IC, not G-IC, and on reducing automatic attention to high caloric foods.

  6. Inhibitory effects of Citrus flavonoids on starch digestion and antihyperglycemic effects in HepG2 cells.

    Science.gov (United States)

    Shen, Wei; Xu, Ying; Lu, Yan-Hua

    2012-09-26

    Flavonoids are a class of important bioactive natural products and are being extensively used in functional foods. In the present study, the effects