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Sample records for capsaicin displays anti-proliferative

  1. Anti-proliferative effect of Ficus pumila Linn. on human leukemic cell lines

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    Christopher Larbie

    2015-04-01

    Conclusion: These findings suggest that crude extracts of FPS and FPL have anti-proliferative effect on the leukemia cells. The antioxidant properties of the plant including phenolics may be partly responsible for the anti-proliferative activity. Further studies are required to isolate chemical components of the plant and establish their anti-proliferative activities and mechanism of action. [Int J Basic Clin Pharmacol 2015; 4(2.000: 330-336

  2. Polyphenols with Anti-Proliferative Activities from Penthorum Chinense Pursh

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    Doudou Huang

    2014-07-01

    Full Text Available Two new polyphenols, penthorumin C (1 and 2,6-dihydroxyacetophenone-4-O- [4ꞌ,6ꞌ-(S-hexahydroxydiphenoyl]-β-D-glucose (2, along with four known polyphenolic acids, pinocembrin-7-O-[4ꞌꞌ,6ꞌꞌ-hexahydroxydiphenoyl]-β-D-glucose(3, pinocembrin-7-O-[3ꞌꞌ-O- galloyl- 4ꞌꞌ,6ꞌꞌ-hexahydroxydiphenoyl]-β-D-glucose (4, thonningianin A (5, and thonningianin B (6 were isolated from Penthourm chinense. All compounds were evaluated for their anti-proliferative activity in HSC-T6 cells, and 2 and 5 showed significant activity, with IC50 values of 12.7 and 19.2 μM, respectively.

  3. Anti proliferative activity of hydnophytum formicarium (sanola) extracts

    International Nuclear Information System (INIS)

    The whole plant of Hydnophytum formicarium Jack (Rubiaceae) locally known as sarang semut, was first extracted successively by petroleum-ether, followed by methanol (MeOH), chloroform, n-buthanol and distilled water and were tested for anti proliferative activity using a panel of human cancer cell lines. MeOH, n-buthanol and aqueous extracts showed anti proliferative effect towards KB-IV (EC50 methanol extract: 17.58 μg/ml; EC50 n-buthanol extract: 9.12 μg/ml and EC50 aqueous extract: 8.71 μg/ml) and only methanol extract showed positive activity towards Caov-3 (EC50: 14.79 μg/ml). No activity was observed in case of other extracts (i.e. petroleum ether and chloroform with EC50 >99 μg/ml). The methanolic extract was tested for its mechanism of action via apoptosis on Caov-3 by employing the TUNEL assay. In the present study, augmented levels of apoptosis were observed in Caov-3 cells treated with 15 μg/ml with apoptotic index of 43.3% and 78.8% in higher concentration (20 μg/ml), a significant different compared with control, which had apoptotic index of 2% only. In conclusion, there is a high possibility that the bioactive component in the methanol extract had selective anti proliferation effects on Caov-3 through apoptotic pathway. This finding may provide a new strategy and a promising approach to the discovery an effective anticancer drug. (Author)

  4. Anti-proliferative activity of Monensin and its tertiary amide derivatives.

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    Huczyński, Adam; Klejborowska, Greta; Antoszczak, Michał; Maj, Ewa; Wietrzyk, Joanna

    2015-10-15

    New tertiary amide derivatives of polyether ionophore Monensin A (MON) were synthesised and their anti-proliferative activity against cancer cell lines was studied. Very high activity (IC50=0.09 μM) and selectivity (SI=232) of MON against human biphenotypic myelomonocytic leukemia cell line (MV4-11) was demonstrated. The MON derivatives obtained exhibit interesting anti-proliferative activity, high selectivity index and also are able to break the drug-resistance of cancer cell line.

  5. Evaluation of the anti-proliferative and cytostatic effect of Citrus sinensis (orange) fruit juice

    OpenAIRE

    Chinedu, Enegide; Arome, David; Ameh, Solomon F; Ameh, Gift E

    2014-01-01

    Aim: This work has been designed to evaluate the anti-proliferative and cytostatic effects of Citrus sinensis (orange) fruit juice on rapidly proliferating cells. Materials and Methods: The study was carried out on the seeds of Sorghum bicolor for 72 h. The mean radicle length (mm) of the seeds was taken at 48 and 72 h. Result: The result showed that when compared with the control, methotrexate, the standard drug showed a significant (P < 0.001) anti-proliferative effect throughout the experi...

  6. Tristetraprolin mediates the anti-proliferative effects of metformin in breast cancer cells

    OpenAIRE

    Pandiri, Indira; Chen, Yingqing; Joe, Yeonsoo; Kim, Hyo Jeong; Park, Jeongmin; Chung, Hun Taeg; Park, Jeong Woo

    2016-01-01

    Metformin, which is a drug commonly prescribed to treat type 2 diabetes, has anti-proliferative effects in cancer cells; however, the molecular mechanisms underlying this effect remain largely unknown. The aim is to investigate the role of tristetraprolin (TTP), an AU-rich element-binding protein, in anti-proliferative effects of metformin in cancer cells. p53 wild-type and p53 mutant breast cancer cells were treated with metformin, and expression of TTP and c-Myc was analyzed by semi-quantit...

  7. Synthesis and anti-proliferative activity of fluoro-substituted chalcones.

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    Burmaoglu, Serdar; Algul, Oztekin; Anıl, Derya Aktas; Gobek, Arzu; Duran, Gulay Gulbol; Ersan, Ronak Haj; Duran, Nizami

    2016-07-01

    A series of novel fluoro-substituted chalcone derivatives have been synthesized. All synthesized compounds were characterized by (1)H nuclear magnetic resonance (NMR), (13)C NMR, and elemental analysis. Their anti-proliferative activities were evaluated against five cancer cells lines, namely, A549, A498, HeLa, A375, and HepG2 using the MTT method. Most of the compounds showed moderate to high activity with IC50 values in the range of 0.029-0.729μM. Of all the synthesized compounds, 10 and 19 exhibited the most potent anti-proliferative activities against cancer cells, and 10 was identified as the most promising compound. PMID:27217001

  8. Metformin Enhances Anti-proliferative Effect of Cisplatin in Cervical Cancer Cell Line

    OpenAIRE

    Ratih D. Yudhani; Riza N. Pesik; Dono Indarto

    2016-01-01

    Cervival cancer is one of the top rank of gynecological malignancy in the world, leading to high morbidity and mortality rates. Cisplatin is a chemotherapeutic agent that is generally used to treat cervical cancer but the use of this drug is limited because of serious side effects. Metformin, a diabetic drug, decreases not only blood glucose levels but also cell viability of some cancer cells. The aim of this study was to investigate the anti-proliferative effect of combination metformin and ...

  9. Quinazolinones-Phenylquinoxaline hybrids with unsaturation/saturation linkers as novel anti-proliferative agents.

    Science.gov (United States)

    Palem, Jyothsna Devi; Alugubelli, Gopi Reddy; Bantu, Rajashaker; Nagarapu, Lingaiah; Polepalli, Sowjanya; Jain, S Nishanth; Bathini, Raju; Manga, Vijjulatha

    2016-07-01

    A new series of novel quinazolinones with allylphenyl quinoxaline hybrids 9a-n were efficiently synthesized in good yields by the reaction of 3-allyl-2-methylquinazolin-4(3H)-one (5a-n) with bromophenyl)quinoxaline (8) utilizing Pd catalyzed Heck-cross coupling and evaluated for anti-proliferative activity against four cancer cell lines such as HeLa (cervical), MIAPACA (pancreatic), MDA-MB-231 (breast) and IMR32 (neuroblastoma). Compounds 9a, 9e, 9g and 9h exhibited promising anti-proliferative activity with GI50 values ranging from 0.06 to 0.2μM against four cell lines, while compounds 9e and 9k showed significant activity against HeLa and MIAPACA cell lines and compounds 9b, 9d, 9h and 9j showed selective potency against IMR32 and MDA-MB-231 cell lines. This is the first report on the synthesis and in vitro anti-proliferative evaluation of E-2-(4-substituted)-3-(3-(4-(quinoxalin-2-yl)phenyl)allyl)quinazolin-4(3H)-ones (9a-n). Docking results indicate a sign of good correlation between experimental activity and calculated binding affinity (dock score), suggesting that these compounds could act as promising DNA intercalates. PMID:27209232

  10. Comparative antitumor and anti-proliferative activities ofHippophae rhamnoidesL. leaves extracts

    Institute of Scientific and Technical Information of China (English)

    Javid Ali; Bashir Ahmad

    2015-01-01

    Objective:To evaluate the antitumor and anti-proliferative activities of methanol, aqueous, acetone, ethyl acetate, ethanol, chloroform andn-hexane extracts ofHippophae rhamnoides leaves. Methods: Antitumor activities were evaluated by using the antitumor potato disc assay by using inoculums (Agrobacterium tumefaciens) with three different concentrations of test samples (10, 100 and 1 000 mg/L). Anti-proliferative activity was evaluated by the given method of methyl thiazolyl tetrazolium assay. The concentrations of the extract ranging from 0.039 to 10 mg/mL were tested against HeLa cells. Results: Highest tumors inhibition activity (60.9% and 55.8%) was shown by methanol and ethanol extracts, with EC50 values of 424.41 and 434.61 mg/L respectively. At 10 mg/mL, The highest cell inhibition 75.61% was observed in methanol extract and the lowest 36.59% were calculated inn-hexane extract. The difference in tumor and cell inhibition (%) may be due to the different concentration of active compounds responsible for antitumor and anti-proliferative activities. All extracts have considerable level of tumor and cell inhibitiory effect in a dose dependent manner. Conclusions:Our finding showed thatHippophae rhamnoidesleaves are a potent natural source of antitumor and antiproliferative agent.

  11. Tristetraprolin mediates the anti-proliferative effects of metformin in breast cancer cells.

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    Pandiri, Indira; Chen, Yingqing; Joe, Yeonsoo; Kim, Hyo Jeong; Park, Jeongmin; Chung, Hun Taeg; Park, Jeong Woo

    2016-02-01

    Metformin, which is a drug commonly prescribed to treat type 2 diabetes, has anti-proliferative effects in cancer cells; however, the molecular mechanisms underlying this effect remain largely unknown. The aim is to investigate the role of tristetraprolin (TTP), an AU-rich element-binding protein, in anti-proliferative effects of metformin in cancer cells. p53 wild-type and p53 mutant breast cancer cells were treated with metformin, and expression of TTP and c-Myc was analyzed by semi-quantitative RT-PCR, Western blots, and promoter activity assay. Breast cancer cells were transfected with siRNA against TTP to inhibit TTP expression or c-Myc and, after metformin treatment, analyzed for cell proliferation by MTS assay. Metformin induces the expression of tristetraprolin (TTP) in breast cancer cells in a p53-independent manner. Importantly, inhibition of TTP abrogated the anti-proliferation effect of metformin. We observed that metformin decreased c-Myc levels, and ectopic expression of c-Myc blocked the effect of metformin on TTP expression and cell proliferation. Our data indicate that metformin induces TTP expression by reducing the expression of c-Myc, suggesting a new model whereby TTP acts as a mediator of metformin's anti-proliferative activity in cancer cells. PMID:26956973

  12. Quinazolinones-Phenylquinoxaline hybrids with unsaturation/saturation linkers as novel anti-proliferative agents.

    Science.gov (United States)

    Palem, Jyothsna Devi; Alugubelli, Gopi Reddy; Bantu, Rajashaker; Nagarapu, Lingaiah; Polepalli, Sowjanya; Jain, S Nishanth; Bathini, Raju; Manga, Vijjulatha

    2016-07-01

    A new series of novel quinazolinones with allylphenyl quinoxaline hybrids 9a-n were efficiently synthesized in good yields by the reaction of 3-allyl-2-methylquinazolin-4(3H)-one (5a-n) with bromophenyl)quinoxaline (8) utilizing Pd catalyzed Heck-cross coupling and evaluated for anti-proliferative activity against four cancer cell lines such as HeLa (cervical), MIAPACA (pancreatic), MDA-MB-231 (breast) and IMR32 (neuroblastoma). Compounds 9a, 9e, 9g and 9h exhibited promising anti-proliferative activity with GI50 values ranging from 0.06 to 0.2μM against four cell lines, while compounds 9e and 9k showed significant activity against HeLa and MIAPACA cell lines and compounds 9b, 9d, 9h and 9j showed selective potency against IMR32 and MDA-MB-231 cell lines. This is the first report on the synthesis and in vitro anti-proliferative evaluation of E-2-(4-substituted)-3-(3-(4-(quinoxalin-2-yl)phenyl)allyl)quinazolin-4(3H)-ones (9a-n). Docking results indicate a sign of good correlation between experimental activity and calculated binding affinity (dock score), suggesting that these compounds could act as promising DNA intercalates.

  13. Comparative antitumor and anti-proliferative activities of Hippophae rhamnoides L. leaves extracts

    Directory of Open Access Journals (Sweden)

    Javid Ali

    2015-03-01

    Full Text Available Objective: To evaluate the antitumor and anti-proliferative activities of methanol, aqueous, acetone, ethyl acetate, ethanol, chloroform and n-hexane extracts of Hippophae rhamnoides leaves. Methods: Antitumor activities were evaluated by using the antitumor potato disc assay by using inoculums (Agrobacterium tumefaciens with three different concentrations of test samples (10, 100 and 1 000 mg/L. Anti-proliferative activity was evaluated by the given method of methyl thiazolyl tetrazolium assay. The concentrations of the extract ranging from 0.039 to 10 mg/mL were tested against HeLa cells. Results: Highest tumors inhibition activity (60.9% and 55.8% was shown by methanol and ethanol extracts, with EC50 values of 424.41 and 434.61 mg/L respectively. At 10 mg/mL, The highest cell inhibition 75.61% was observed in methanol extract and the lowest 36.59% were calculated in n-hexane extract. The difference in tumor and cell inhibition (% may be due to the different concentration of active compounds responsible for antitumor and anti-proliferative activities. All extracts have considerable level of tumor and cell inhibitiory effect in a dose dependent manner. Conclusions: Our finding showed that Hippophae rhamnoides leaves are a potent natural source of antitumor and antiproliferative agent.

  14. In vitro anti-proliferative and anti-angiogenic activities of thalidomide dithiocarbamate analogs.

    Science.gov (United States)

    El-Aarag, Bishoy Y A; Kasai, Tomonari; Zahran, Magdy A H; Zakhary, Nadia I; Shigehiro, Tsukasa; Sekhar, Sreeja C; Agwa, Hussein S; Mizutani, Akifumi; Murakami, Hiroshi; Kakuta, Hiroki; Seno, Masaharu

    2014-08-01

    Inhibition of angiogenesis is currently perceived as a promising strategy in the treatment of cancer. The anti-angiogenicity of thalidomide has inspired a second wave of research on this teratogenic drug. The present study aimed to investigate the anti-proliferative and anti-angiogenic activities of two thalidomide dithiocarbamate analogs by studying their anti-proliferative effects on human umbilical vein endothelial cells (HUVECs) and MDA-MB-231 human breast cancer cell lines. Their action on the expression levels of IL-6, IL-8, TNF-α, VEGF165, and MMP-2 was also assessed. Furthermore, their effect on angiogenesis was evaluated through wound healing, migration, tube formation, and nitric oxide (NO) assays. Results illustrated that the proliferation of HUVECs and MDA-MB-231 cells was not significantly affected by thalidomide at 6.25-100μM. Thalidomide failed to block angiogenesis at similar concentrations. By contrast, thalidomide dithiocarbamate analogs exhibited significant anti-proliferative action on HUVECs and MDA-MB-231 cells without causing cytotoxicity and also showed powerful anti-angiogenicity in wound healing, migration, tube formation, and NO assays. Thalidomide analogs 1 and 2 demonstrated more potent activity to suppress expression levels of IL-6, IL-8, TNF-α, VEGF165, and MMP-2 than thalidomide. Analog 1 consistently, showed the highest potency and efficacy in all the assays. Taken together, our results support further development and evaluation of novel thalidomide analogs as anti-tumor and anti-angiogenic agents.

  15. Anti-proliferative effect of leaf extracts of Eucalyptus citriodora against human cancer cells in vitro and in vivo.

    Science.gov (United States)

    Bhagat, Madhulika; Sharma, Vikas; Saxena, Ajit Kumar

    2012-12-01

    Six different extracts from Eucalyptus citriodora leaves were investigated for their anticancer effect. Extracts were prepared using a range of polar and non-polar solvents to leach out maximum active components. Phytochemical analysis of the extracts revealed the presence of anthraquinones, cardiac glycosides, flavonoids, saponins and tannins. Cytotoxic activity of different extracts was tested in vitro against seven human cancer cell lines from seven different tissues, such as SW-620 (colon), HOP-62 (lung), PC-3 (prostate), OVCAR-5 (ovary), HeLa (cervix), IMR-32 (neuroblastoma) and HEP-2 (liver). The ethyl acetate, chloroform and 50% methanolic extract displayed highest anti-proliferative effect in a dose-dependent manner. In vivo anti-tumor activity was evaluated against murine tumor (solid) model of Ehrlich ascites carcinoma and Sarcoma 180. The results showed that ethyl acetate and aqueous extracts suppressed the growth of Ehrlich ascites carcinoma (29.79% and 18.48%, respectively), but showed little growth inhibition in case of Sarcoma 180 (13. 86% and 8.57%, respectively). The activity might be due to the flavonoids, tannins and saponins that are present in all the extracts of the plant. Further investigation is required for the isolation of active principle(s) from the ethyl acetate extract, which has shown significant in vitro and in vivo anticancer potential. PMID:23350280

  16. Evidence of Anti-Proliferative Activities in Blue Mussel (Mytilus edulis By-Products

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    Marie-Elise Carbonneau

    2013-03-01

    Full Text Available Shellfish waste components contain significant levels of high quality protein and are therefore a potential source for biofunctional high-value peptides. The feasibility of applying a pilot scale enzymatic hydrolysis process to whole Mytilus edulis and, by fractionation, recover hydrolysates presenting a biological activity of interest, was evaluated. Fractions were tested on four immortalized cancerous cell lines: A549, BT549, HCT15 and PC3. The 50 kDa fraction, enriched in peptides, presented anti-proliferative activity with all cell lines and results suggest a bioactive molecule synergy within the fraction. At a protein concentration of 44 µg/mL, the 50 kDa fraction induced a mortality of 90% for PC3, 89% for A549, 85% for HCT15 and of 81% for BT549 cell lines. At the low protein concentration of only 11 µg/mL the 50 kDa fraction still entails a cell mortality of 76% for A549 and 87% for PC3 cell lines. The 50 kDa fraction contains 56% of proteins, 3% of lipids and 6% of minerals on a dry weight basis and the lowest levels detected of taurine and methionine and highest levels of threonine, proline and glycine amino acids. The enzymatic hydrolysis process suggests that Mytilus edulis by-products should be viewed as high-valued products with strong potential as anti-proliferative agent and promising active ingredients in functional foods.

  17. Arctigenin in combination with quercetin synergistically enhances the anti-proliferative effect in prostate cancer cells

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    Wang, Piwen; Phan, Tien; Gordon, David; Chung, Seyung; Henning, Susanne M.; Vadgama, Jaydutt V.

    2014-01-01

    Scope We investigated whether a combination of two promising chemopreventive agents arctigenin and quercetin increases the anti-carcinogenic potency at lower concentrations than necessary when used individually in prostate cancer. Methods and results Androgen-dependent LAPC-4 and LNCaP prostate cancer cells were treated with low doses of arctigenin and quercetin alone or in combination for 48h. The anti-proliferative activity of arctigenin was 10-20 fold stronger than quercetin in both cell lines. Their combination synergistically enhanced the anti-proliferative effect, with a stronger effect in androgen receptor (AR) wild-type LAPC-4 cells than in AR mutated LNCaP cells. Arctigenin demonstrated a strong ability to inhibit AR protein expression in LAPC-4 cells. The combination treatment significantly inhibited both AR and PI3K/Akt pathways compared to control. A protein array analysis revealed that the mixture targets multiple pathways particularly in LAPC-4 cells including Stat3 pathway. The mixture significantly inhibited the expression of several oncogenic microRNAs including miR-21, miR-19b, and miR-148a compared to control. The mixture also enhanced the inhibition of cell migration in both cell lines compared to individual compounds tested. Conclusion The combination of arctigenin and quercetin, that target similar pathways, at low physiological doses, provides a novel regimen with enhanced chemoprevention in prostate cancer. PMID:25380086

  18. [Synthesis and anti-proliferative activity of fluoroquinolone (rhodanine unsaturated ketone) amide derivatives].

    Science.gov (United States)

    Gao, Liu-zhou; Xie, Yu-suo; Yan, Qiang; Wu, Shu-min; Ni, Li-li; Zhao, Hui; Huang, Wen-long; Hu, Guo-qiang

    2015-08-01

    To discover novel antitumor rhodanine unsaturated ketones, a series of fluoroquinolone (rhodanine α, β-unsaturated ketone) amine derivatives (5a-5r) were designed and synthesized with fluoroquinolone amide scaffold as a carrier. The structures of eighteen title compounds were characterized by elemental analysis, 1H NMR and MS. The in vitro anti-proliferative activity against Hep-3B, Capan-1 and HL60 cells was evaluated by MTT assay. The results showed that the title compounds not only had more significant anti-proliferative activity against three tested cancer cell lines than that of the parent ciprofloxacin 1, but also exhibited the highest activity against Capan-1 cells. The SAR revealed that some compounds carrying aromatic heterocyclic rings or phenyl attached to an electron-withdrawing carboxyl or sulfonamide substituent were comparable to or better than comparison doxorubicin against Capan-1 cells. As such, it suggests that fluoroquinolone (rhodanine α, β-unsaturated ketone) amines are promising leads for the development of novel antitumor fluoroquinolones or rhodanine analogues. PMID:26669001

  19. Synthesis and anti-proliferative activity of novel azazerumbone conjugates with chalcones.

    Science.gov (United States)

    Truong, Vuong Van; Nam, Tran Duy; Hung, Truong Ngoc; Nga, Nguyen Thi; Quan, Pham Minh; Chinh, Luu Van; Jung, Sang-Hun

    2015-11-15

    The conjugation of azazerumbone ((3E,7E,11E)-5,5,8,12-tetramethylazacyclododeca-3,7,11-trien-2-one (7)) and 2,4-dihydroxychalcones was carried out for the preparation of novel target compounds 9a-g with 1-ethylene-4-methylene-1,2,3-triazole linker and 10a-f with propylene linker between amide nitrogen of azazerumbone and 4-hydroxy group of chalcone. The anti-proliferative activity of these compounds against the LU-1, Hep-G2, MCF-7 and SW480 human cancer cell lines were significantly improved compared to those of azazerumbone or zerumbone. The anti-proliferative activities of (3E,7E,11E)-1-((1-(2-(3-hydroxy-4-((E)-3-(3-methoxyphenyl)acryloyl)phenoxy)ethyl)-1H-1,2,3-triazol-4-yl)methyl)-5,5,8,12-tetramethyl azacyclododeca-3,7,11-trien-2-one (9b) and (3E,7E,11E)-1-(3-(4-((E)-3-(3,4,5-trimethoxyphenyl)acryloyl)phenoxy)propyl)-5,5,8,12-tetramethylazacyclododeca-3,7,11-trien-2-one (10d) are nearly comparable to those of ellipticine. PMID:26459207

  20. Anti-proliferative activity of Fumaria vaillantii extracts on different cancer cell lines

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    Fatemeh Haji Abbas Tabrizi

    2016-01-01

    Full Text Available Plant-derived natural products are known to have cancer chemo-preventive and chemo-therapeutic properties. Plant extracts or their active constituents are used as folk medicine in traditional therapies by 80% of the world population. The aim of the present study was to determine the anti-proliferative potential of Fumaria vaillantii extracts on three different cancer cell lines including malignant melanoma SKMEL-3, human breast adenocarcinoma MCF-7 and human myelogenous leukemia K562 as well as human gingival fibroblast (HGF as normal cell line. Anti-proliferative activity was evaluated by 3-(4,5-dimethylthiazol-2-yl-2,5-diphenyltetrazolium bromide (MTT, flowcytometry and annexin methods. Total phenolics and flavonoids were determined by Folin-Ciocalteu and aluminum chloride methods. Chloroform fraction had the lowest IC 50 value at 72 h (0.1 μg/ml in MCF-7 cells. Flowcytometry and annexin-V analysis indicated that the chloroform fraction induced necrosis in MCF-7 cells. In addition, the colorimetric methods showed that the methanolic fraction possessed the highest amount of total phenolics (33.03 ± 0.75 mg/g of dry powder and flavonoids (10.5 ± 2.0 mg/g of dry powder.The collective data demonstrated that F. vaillantii chloroform fraction may contain effective compounds with chemo-therapeutic potential act through an apoptotic independent pathway.

  1. New ursane triterpenoids from Salvia urmiensis Bunge: Absolute configuration and anti-proliferative activity.

    Science.gov (United States)

    Farimani, Mahdi Moridi; Bahadori, Mir Babak; Koulaei, Sheyda Ahmadi; Salehi, Peyman; Ebrahimi, Samad Nejad; Khavasi, Hamid Reza; Hamburger, Matthias

    2015-10-01

    Two new triterpenoids, urmiensolide B (1) and urmiensic acid (2), with rare carbon skeletons together with three known compounds were isolated from the aerial parts of Salvia urmiensis Bunge, an endemic species of Iran. The structures were established by a combination of 1D and 2D NMR, and HRESIMS, and in the case of 2 and 3, their structures were confirmed by single-crystal X-ray analysis. The absolute configuration of 2 was established by electronic circular dichroism (ECD) spectra. The new compounds were evaluated for their anti-proliferative activities against A549 and MCF-7 human cancer cell lines. Compounds 1 and 2 showed IC50 values of 2.8 and 1.6 μM against MCF-7 cells, respectively. PMID:26254275

  2. Buformin exhibits anti-proliferative and anti-invasive effects in endometrial cancer cells

    Science.gov (United States)

    Kilgore, Joshua; Jackson, Amanda L; Clark, Leslie H; Guo, Hui; Zhang, Lu; Jones, Hannah M; Gilliam, Timothy P; Gehrig, Paola A; Zhou, Chunxiao; Bae-Jump, Victoria L

    2016-01-01

    Objective: Biguanides are anti-diabetic drugs that are thought to have anti-tumorigenic effects. Most pre-clinical studies have focused on metformin for cancer treatment and prevention; however, buformin may be potentially more potent than metformin. Given this, our goal was to evaluate the effects of buformin on cell growth, adhesion and invasion in endometrial cancer cell lines. Methods: The ECC-1 and Ishikawa endometrial cancer cell lines were used. Cell proliferation was assessed by MTT assay. Apoptosis and cell cycle analysis was performed by FITC Annexin V assay and propidium iodide staining, respectively. Adhesion was analyzed using the laminin adhesion assay. Invasion was assessed using the transwell invasion assay. The effects of buformin on the AMPK/mTOR pathway were determined by Western immunoblotting. Results: Buformin and metformin inhibited cell proliferation in a dose-dependent manner in both endometrial cancer cell lines. IC50s were 1.4-1.6 mM for metformin and 8-150 μM for buformin. Buformin induced cell cycle G1 phase arrest in the ECC-1 cells and G2 phase arrest in the Ishikawa cells. For both ECC-1 and Ishikawa cells, treatment with buformin resulted in induction of apoptosis, reduction in adhesion and invasion, activation of AMPK and inhibition of phosphorylated-S6. Buformin potentiated the anti-proliferative effects of paclitaxel in both cell lines. Conclusion: Buformin has significant anti-proliferative and anti-metastatic effects in endometrial cancer cells through modulation of the AMPK/mTOR pathway. IC50 values were lower for buformin than metformin, suggesting that buformin may be more potent for endometrial cancer treatment and worthy of further investigation. PMID:27398153

  3. Anti-Proliferative Effect of Rosmarinus officinalis L. Extract on Human Melanoma A375 Cells.

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    Lucia Cattaneo

    Full Text Available Rosemary (Rosmarinus officinalis L. has been used since ancient times in traditional medicine, while nowadays various rosemary formulations are increasingly exploited by alternative medicine to cure or prevent a wide range of health disorders. Rosemary's bioproperties have prompted scientific investigation, which allowed us to ascertain antioxidant, anti-inflammatory, cytostatic, and cytotoxic activities of crude extracts or of pure components. Although there is a growing body of experimental work, information about rosemary's anticancer properties, such as chemoprotective or anti-proliferative effects on cancer cells, is very poor, especially concerning the mechanism of action. Melanoma is a skin tumor whose diffusion is rapidly increasing in the world and whose malignancy is reinforced by its high resistance to cytotoxic agents; hence the availability of new cytotoxic drugs would be very helpful to improve melanoma prognosis. Here we report on the effect of a rosemary hydroalcoholic extract on the viability of the human melanoma A375 cell line. Main components of rosemary extract were identified by liquid chromatography coupled to tandem mass spectrometry (LC/ESI-MS/MS and the effect of the crude extract or of pure components on the proliferation of cancer cells was tested by MTT and Trypan blue assays. The effect on cell cycle was investigated by using flow cytometry, and the alteration of the cellular redox state was evaluated by intracellular ROS levels and protein carbonylation analysis. Furthermore, in order to get information about the molecular mechanisms of cytotoxicity, a comparative proteomic investigation was performed.

  4. Anti-Proliferative Effect of Rosmarinus officinalis L. Extract on Human Melanoma A375 Cells.

    Science.gov (United States)

    Cattaneo, Lucia; Cicconi, Rosella; Mignogna, Giuseppina; Giorgi, Alessandra; Mattei, Maurizio; Graziani, Giulia; Ferracane, Rosalia; Grosso, Alessandro; Aducci, Patrizia; Schininà, M Eugenia; Marra, Mauro

    2015-01-01

    Rosemary (Rosmarinus officinalis L.) has been used since ancient times in traditional medicine, while nowadays various rosemary formulations are increasingly exploited by alternative medicine to cure or prevent a wide range of health disorders. Rosemary's bioproperties have prompted scientific investigation, which allowed us to ascertain antioxidant, anti-inflammatory, cytostatic, and cytotoxic activities of crude extracts or of pure components. Although there is a growing body of experimental work, information about rosemary's anticancer properties, such as chemoprotective or anti-proliferative effects on cancer cells, is very poor, especially concerning the mechanism of action. Melanoma is a skin tumor whose diffusion is rapidly increasing in the world and whose malignancy is reinforced by its high resistance to cytotoxic agents; hence the availability of new cytotoxic drugs would be very helpful to improve melanoma prognosis. Here we report on the effect of a rosemary hydroalcoholic extract on the viability of the human melanoma A375 cell line. Main components of rosemary extract were identified by liquid chromatography coupled to tandem mass spectrometry (LC/ESI-MS/MS) and the effect of the crude extract or of pure components on the proliferation of cancer cells was tested by MTT and Trypan blue assays. The effect on cell cycle was investigated by using flow cytometry, and the alteration of the cellular redox state was evaluated by intracellular ROS levels and protein carbonylation analysis. Furthermore, in order to get information about the molecular mechanisms of cytotoxicity, a comparative proteomic investigation was performed. PMID:26176704

  5. Anti-proliferative effects of Bifidobacterium adolescentis SPM0212 extract on human colon cancer cell lines

    International Nuclear Information System (INIS)

    Lactic acid bacteria (LAB) are beneficial probiotic organisms that contribute to improved nutrition, microbial balance, and immuno-enhancement of the intestinal tract, as well as anti-tumor activity. The aim of the present work was to study the growth inhibition of tumor cells by butanol extract of Bifidobacterium adolescentis isolated from healthy young Koreans. The anti-proliferative activity of B. adolescentis isolates was assessed by XTT assays on three human colon cancer cell lines (Caco-2, HT-29, and SW480). The effects of B. adolescentis SPM0212 butanol extract on tumor necrosis factor-α (TNF-α) and nitric oxide (NO) production were tested using the murine macrophage RAW 264.7 cell line. The butanol extract of B. adolescentis SPM0212 dose-dependently inhibited the growth of Caco-2, HT-29, and SW480 cells by 70%, 30%, and 40%, respectively, at 200 μg/mL. Additionally, the butanol extract of B. adolescentis SPM0212 induced macrophage activation and significantly increased the production of TNF-α and NO, which regulate immune modulation and are cytotoxic to tumor cells. The butanol extract of B. adolescentis SPM0212 increased activity of the host immune system and may improve human health by helping to prevent colon cancer as a biological response modifier

  6. Two new diterpene derivatives from Euphorbia lunulata Bge and their anti-proliferative activities.

    Science.gov (United States)

    Liu, Chao; Liao, Zhi-xin; Liu, Shi-jun; Qu, Yan-bo; Wang, Heng-shan

    2014-07-01

    A new ent-abietane-type diterpene lactone (1) and a new jatrophane-type diterpenoid (2), together with twelve known compounds including three diterpenes (3-5), five triterpenes (6-10) and four sterides (11-14) were isolated from the ethanol extract of the whole plant of Euphorbia lunulata Bge. The structure of compounds 1 and 2 was elucidated on the basis of 1D and 2D NMR spectra and the HR-ESI-MS data. The structure of compound 2 was further analyzed by an X-ray crystallographic study. The in vitro anti-proliferative activities against MCF-7 and NCI-H460 cell lines for compounds 1-5 (diterpene) were evaluated. The results showed marked activity for compound 1 against the two cell lines with the IC50 values 19.5 (NCI-H460) and 18.6 (MCF-7) μM, while for cis-platinum (a positive cytotoxic control agent) 29.7 (NCI-H460) and 27.7 (MCF-7) μM. Compounds 2-5 exhibited moderate cytotoxic activities for the two cell lines with the IC50 values ranging from 32.1 to 58.2 μM.

  7. Biocatalytically Oligomerized Epicatechin with Potent and Specific Anti-proliferative Activity for Human Breast Cancer Cells

    Directory of Open Access Journals (Sweden)

    Ramaswamy Nagarajan

    2008-11-01

    Full Text Available Catechins, naturally occurring flavonoids derived from wine and green tea, are known to exhibit multiple health benefits. Epigallocatechin gallate (EGCG is one of the most widely investigated catechins, but its efficacy in cancer therapy is still inconsistent and limited. The poor stability of EGCG has contributed to the disparity in the reported anti-cancer activity and other beneficial properties. Here we report an innovative enzymatic strategy for the oligomerization of catechins (specifically epicatechin that yields stable, water-soluble oligomerized epicatechins with enhanced and highly specific anti-proliferative activity for human breast cancer cells. This one-pot oxidative oligomerization is carried out in ambient conditions using Horseradish Peroxidase (HRP as a catalyst yielding water-soluble oligo(epicatechins. The oligomerized epicatechins obtained exhibit excellent growth inhibitory effects against human breast cancer cells with greater specificity towards growth-inhibiting cancer cells as opposed to normal cells, achieving a high therapeutic differential. Our studies indicate that water-soluble oligomeric epicatechins surpass EGCG in stability, selectivity and efficacy at lower doses.

  8. Evaluation of the Anti-proliferative Effects of Ophiocoma erinaceus Methanol Extract Against Human Cervical Cancer Cells

    OpenAIRE

    Baharara, Javad; Amini, Elaheh; Namvar, Farideh

    2016-01-01

    Background: Marine organisms provide appreciable source of novel bioactive compounds with pharmacological potential. There is little information in correlation with anti-cancer activities of brittle star. In the present study, anti-neoplastic efficacy of Ophiocoma erinaceus methanol extract against human cervical cancer cells was investigated. Methods: The HeLa cells were cultured and exposed to brittle star methanol extract for 24 and 48 hr. The anti-proliferative properties were examined by...

  9. One-Pot Ugi/Aza-Michael Synthesis of Highly Substituted 2,5-Diketopiperazines with Anti-Proliferative Properties

    OpenAIRE

    Ulrike Holzgrabe; Gessner, Viktoria H.; Florian Seufert; Carsten Berges; Andreas Hartung

    2012-01-01

    The well-known Ugi reaction of aldehydes with amines, carboxylic acids and isocyanides leads to the formation of acyclic α-acylaminocarboxamides. Replacement of the carboxylic acid derivatives with β-acyl substituted acrylic acids gives access to highly substituted 2,5-diketopiperazines in one single reaction-step without additives or complex reaction procedures. The obtained diketopiperazines show anti-proliferative effects on activated T cells and represent therefore poten...

  10. Insulin-sensitizing and Anti-proliferative Effects of Argania spinosa Seed Extracts

    Directory of Open Access Journals (Sweden)

    Samira Samane

    2006-01-01

    Full Text Available Argania spinosa is an evergreen tree endemic of southwestern Morocco. Many preparations have been used in traditional Moroccan medicine for centuries to treat several illnesses including diabetes. However, scientific evidence supporting these actions is lacking. Therefore, we prepared various extracts of the argan fruit, namely keel, cake and argan oil extracts, which we tested in the HTC hepatoma cell line for their potential to affect cellular insulin responses. Cell viability was measured by Trypan Blue exclusion and the response to insulin evaluated by the activation of the extracellular regulated kinase (ERK1/2, ERK kinase (MEK1/2 and protein kinase B (PKB/Akt signaling components. None of the extracts demonstrated significant cytotoxic activity. Certain extracts demonstrated a bi-phasic effect on ERK1/2 activation; low doses of the extract slightly increased ERK1/2 activation in response to insulin, whereas higher doses completely abolished the response. In contrast, none of the extracts had any significant effect on MEK whereas only a cake saponin subfraction enhanced insulin-induced PKB/Akt activation. The specific action of argan oil extracts on ERK1/2 activation made us consider an anti-proliferative action. We have thus tested other transformed cell lines (HT-1080 and MSV-MDCK-INV cells and found similar results. Inhibition of ERK1/2 activation was also associated with decreased DNA synthesis as evidenced by [3H]thymidine incorporation experiments. These results suggest that the products of Argania spinosa may provide a new therapeutic avenue against proliferative diseases.

  11. Insulin-sensitizing and anti-proliferative effects of Argania spinosa seed extracts.

    Science.gov (United States)

    Samane, Samira; Noël, Josette; Charrouf, Zoubida; Amarouch, Hamid; Haddad, Pierre Selim

    2006-09-01

    Argania spinosa is an evergreen tree endemic of southwestern Morocco. Many preparations have been used in traditional Moroccan medicine for centuries to treat several illnesses including diabetes. However, scientific evidence supporting these actions is lacking. Therefore, we prepared various extracts of the argan fruit, namely keel, cake and argan oil extracts, which we tested in the HTC hepatoma cell line for their potential to affect cellular insulin responses. Cell viability was measured by Trypan Blue exclusion and the response to insulin evaluated by the activation of the extracellular regulated kinase (ERK1/2), ERK kinase (MEK1/2) and protein kinase B (PKB/Akt) signaling components. None of the extracts demonstrated significant cytotoxic activity. Certain extracts demonstrated a bi-phasic effect on ERK1/2 activation; low doses of the extract slightly increased ERK1/2 activation in response to insulin, whereas higher doses completely abolished the response. In contrast, none of the extracts had any significant effect on MEK whereas only a cake saponin subfraction enhanced insulin-induced PKB/Akt activation. The specific action of argan oil extracts on ERK1/2 activation made us consider an anti-proliferative action. We have thus tested other transformed cell lines (HT-1080 and MSV-MDCK-INV cells) and found similar results. Inhibition of ERK1/2 activation was also associated with decreased DNA synthesis as evidenced by [(3)H]thymidine incorporation experiments. These results suggest that the products of Argania spinosa may provide a new therapeutic avenue against proliferative diseases.

  12. Binding, Antioxidant and Anti-proliferative Properties of Bioactive Compounds of Sweet Paprika (Capsicum annuum L.).

    Science.gov (United States)

    Kim, Hong-Gi; Bae, Jong-Hyang; Jastrzebski, Zenon; Cherkas, Andriy; Heo, Buk-Gu; Gorinstein, Shela; Ku, Yang-Gyu

    2016-06-01

    The scope of this research was to determine the bioactive composition, antioxidant, binding, and anti-proliferative properties of red sweet paprika growing under artificial light. The amounts of carotenoids, chlorophyll, polyphenols, tannins, and flavonoids in red paprika (RP), cultivated in Korea, before and after light treatments under high pressure sodium (HPS) and lighting emitting plasma (LEP) lamps (RPControl, RPHPS, RPLEP), were analyzed in water (W) and ethanolic extracts (Et). Spectroscopic, radical scavenging assays, fluorescence and cytotoxicity measurements were applied. The results of this study showed that total chlorophyll and carotenes were the highest in RPHPS (10.50 ± 1.02 and 33.90 ± 3.26 μg/g dry weight (DW)). The strongest antioxidant capacity (μM TE/g DW) in a 2, 2'-azino-bis (3-ethyl-benzothiazoline-6-sulfonic acid) diammonium salt (ABTS(•+)) assay was in RPControlEt (24.34 ± 2.36), in a ferric-reducing/antioxidant power (FRAP) assay in RPHPSW (27.08 ± 2.4) and in a cupric reducing antioxidant (CUPRAC) in RPLEPW (70.99 ± 7.11). The paprika ethanolic extracts showed lower values in their bioactivity than the water ones. The binding and cytotoxicity abilities of extracted polyphenols correlated with their amounts. LEP treatment is better for plant growth characteristics than other conventional treatments. The investigated paprika samples can be used as a source of antioxidants. PMID:27184000

  13. Azithromycin Synergistically Enhances Anti-Proliferative Activity of Vincristine in Cervical and Gastric Cancer Cells

    Energy Technology Data Exchange (ETDEWEB)

    Zhou, Xuezhang; Zhang, Yuyan; Li, Yong; Hao, Xiujing; Liu, Xiaoming, E-mail: erc1080@gmail.com; Wang, Yujiong, E-mail: erc1080@gmail.com [Key Laboratory of the Ministry of Education for the Conservation and Utilization of Special Biological Resources of Western China, Yinchuan 750021, Ningxia (China); College of Life Science, Ningxia University, Yinchuan 750021, Ningxia (China)

    2012-12-04

    In this study, the anti-proliferative and anticancer activity of azithromycin (AZM) was examined. In the presence of AZM, cell growth was inhibited more effectively in Hela and SGC-7901 cancer cells, relative to transformed BHK-21 cells. The respective 50% inhibition of cell growth (IC{sub 50}) values for Hela, SGC-7901 and BHK-21 were 15.66, 26.05 and 91.00 µg/mL at 72 h post incubation, indicative of a selective cytotoxicity against cancer cells. Cell apoptosis analysis using Hoechst nuclear staining and annexin V-FITC binding assay further demonstrated that AZM was capable of inducing apoptosis in both cancer cells and transformed cells. The apoptosis induced by AZM was partly through a caspase-dependent mechanism with an up-regulation of apoptotic protein cleavage PARP and caspase-3 products, as well as a down-regulation of anti-apoptotic proteins, Mcl-1, bcl-2 and bcl-X1. More importantly, a combination of AZM and a low dose of the common anti-cancer chemotherapeutic agent vincristine (VCR), produced a selectively synergistic effect on apoptosis of Hela and SGC-7901 cells, but not BHK-21 cells. In the presence of 12.50 μg/mL of VCR, the respective IC{sub 50} values of Hela, SGC-7901 and BHK-21 cells to AZM were reduced to 9.47 µg/mL, 8.43 µg/mL and 40.15 µg/mL at 72 h after the incubation, suggesting that the cytotoxicity of AZM had a selective anti-cancer effect on cancer over transformed cells in vitro. These results imply that AZM may be a potential anticancer agent for use in chemotherapy regimens, and it may minimize side effects via reduction of dosage and enhancing the effectiveness common chemotherapeutic drugs.

  14. Insulin-sensitizing and anti-proliferative effects of Argania spinosa seed extracts.

    Science.gov (United States)

    Samane, Samira; Noël, Josette; Charrouf, Zoubida; Amarouch, Hamid; Haddad, Pierre Selim

    2006-09-01

    Argania spinosa is an evergreen tree endemic of southwestern Morocco. Many preparations have been used in traditional Moroccan medicine for centuries to treat several illnesses including diabetes. However, scientific evidence supporting these actions is lacking. Therefore, we prepared various extracts of the argan fruit, namely keel, cake and argan oil extracts, which we tested in the HTC hepatoma cell line for their potential to affect cellular insulin responses. Cell viability was measured by Trypan Blue exclusion and the response to insulin evaluated by the activation of the extracellular regulated kinase (ERK1/2), ERK kinase (MEK1/2) and protein kinase B (PKB/Akt) signaling components. None of the extracts demonstrated significant cytotoxic activity. Certain extracts demonstrated a bi-phasic effect on ERK1/2 activation; low doses of the extract slightly increased ERK1/2 activation in response to insulin, whereas higher doses completely abolished the response. In contrast, none of the extracts had any significant effect on MEK whereas only a cake saponin subfraction enhanced insulin-induced PKB/Akt activation. The specific action of argan oil extracts on ERK1/2 activation made us consider an anti-proliferative action. We have thus tested other transformed cell lines (HT-1080 and MSV-MDCK-INV cells) and found similar results. Inhibition of ERK1/2 activation was also associated with decreased DNA synthesis as evidenced by [(3)H]thymidine incorporation experiments. These results suggest that the products of Argania spinosa may provide a new therapeutic avenue against proliferative diseases. PMID:16951716

  15. Capsaicin from chili (Capsicum spp. inhibits vascular smooth muscle cell proliferation [v1; ref status: indexed, http://f1000r.es/4yk

    Directory of Open Access Journals (Sweden)

    Rongxia Liu

    2015-01-01

    Full Text Available Accelerated vascular smooth muscle cell (VSMC proliferation is implied in cardiovascular disease and significantly contributes to vessel lumen reduction following surgical interventions such as percutaneous transluminal coronary angioplasty or bypass surgery. Therefore, identification and characterization of compounds and mechanisms able to counteract VSMC proliferation is of potential therapeutic relevance. This work reveals the anti-proliferative effect of the natural product capsaicin from Capsicum spp. by quantification of metabolic activity and DNA synthesis in activated VSMC. The observed in vitro activity profile of capsaicin warrants further research on its mechanism of action and potential for therapeutic application.

  16. Bioavailability of capsaicin and its implications for drug delivery.

    Science.gov (United States)

    Rollyson, William D; Stover, Cody A; Brown, Kathleen C; Perry, Haley E; Stevenson, Cathryn D; McNees, Christopher A; Ball, John G; Valentovic, Monica A; Dasgupta, Piyali

    2014-12-28

    The dietary compound capsaicin is responsible for the "hot and spicy" taste of chili peppers and pepper extracts. It is a valuable pharmacological agent with several therapeutic applications in controlling pain and inflammation. Emerging studies show that it displays potent anti-tumor activity in several human cancers. On a more basic research level, capsaicin has been used as a ligand to activate several types of ion-channel receptors. The pharmacological activity of capsaicin-like compounds is dependent on several factors like the dose, the route of administration and most importantly on its concentration at target tissues. The present review describes the current knowledge involving the metabolism and bioavailability of capsaicinoids in rodents and humans. Novel drug delivery strategies used to improve the bioavailability and therapeutic index of capsaicin are discussed in detail. The generation of novel capsaicin-mimetics and improved drug delivery methods will foster the hope of innovative applications of capsaicin in human disease. PMID:25307998

  17. GTP depletion synergizes the anti-proliferative activity of chemotherapeutic agents in a cell type-dependent manner

    Energy Technology Data Exchange (ETDEWEB)

    Lin, Tao; Meng, Lingjun [Center for Cancer and Stem Cell Biology, Institute of Biosciences and Technology, Texas A and M Health Science Center, Houston, TX 77030 (United States); Tsai, Robert Y.L., E-mail: rtsai@ibt.tamhsc.edu [Center for Cancer and Stem Cell Biology, Institute of Biosciences and Technology, Texas A and M Health Science Center, Houston, TX 77030 (United States)

    2011-10-22

    Highlights: {yields} Strong synergy between mycophenolic acid (MPA) and 5-FU in MDA-MB-231 cells. {yields} Cell type-dependent synergy between MPA and anti-proliferative agents. {yields} The synergy of MPA on 5-FU is recapitulated by RNA polymerase-I inhibition. {yields} The synergy of MPA on 5-FU requires the expression of nucleostemin. -- Abstract: Mycophenolic acid (MPA) depletes intracellular GTP by blocking de novo guanine nucleotide synthesis. GTP is used ubiquitously for DNA/RNA synthesis and as a signaling molecule. Here, we made a surprising discovery that the anti-proliferative activity of MPA acts synergistically with specific chemotherapeutic agents in a cell type-dependent manner. In MDA-MB-231 cells, MPA shows an extremely potent synergy with 5-FU but not with doxorubicin or etoposide. The synergy between 5-FU and MPA works most effectively against the highly tumorigenic mammary tumor cells compared to the less tumorigenic ones, and does not work in the non-breast cancer cell types that we tested, with the exception of PC3 cells. On the contrary, MPA shows the highest synergy with paclitaxel but not with 5-FU in SCC-25 cells, derived from oral squamous cell carcinomas. Mechanistically, the synergistic effect of MPA on 5-FU in MDA-MB-231 cells can be recapitulated by inhibiting the RNA polymerase-I activity and requires the expression of nucleostemin. This work reveals that the synergy between MPA and anti-proliferative agents is determined by cell type-dependent factors.

  18. One-Pot Ugi/Aza-Michael Synthesis of Highly Substituted 2,5-Diketopiperazines with Anti-Proliferative Properties

    Directory of Open Access Journals (Sweden)

    Ulrike Holzgrabe

    2012-12-01

    Full Text Available The well-known Ugi reaction of aldehydes with amines, carboxylic acids and isocyanides leads to the formation of acyclic α-acylaminocarboxamides. Replacement of the carboxylic acid derivatives with β-acyl substituted acrylic acids gives access to highly substituted 2,5-diketopiperazines in one single reaction-step without additives or complex reaction procedures. The obtained diketopiperazines show anti-proliferative effects on activated T cells and represent therefore potential candidates for targeting unwanted T cell-mediated immune responses.

  19. In vitro antioxidant activities and anti-proliferative properties of the functional herb Abrus cantoniensis and its main alkaloid abrine.

    Science.gov (United States)

    Yang, Mei; Al Zaharna, Mazen; Chen, Yu-Shan; Li, Li; Cheung, Hon-Yeung

    2014-09-01

    Abrus cantoniensis is a common and popular vegetative food consumed as beverage, soup and folk medicine in the tropical and subtropical areas of Asia. It has been claimed valuable for cleansing toxicants in the liver. However, the functional effects of A. cantoniensis have not yet been scientifically explored. This study comprehensively evaluated the in vitro antioxidant and anti-proliferative capacities of the herbal extract and the main alkaloid abrine. Abrine was qualitatively and quantitatively determined in methanol extract (ME) using HPLC-DAD and LC-MS/MS. The results showed that ME, ethyl acetate fraction (EF) and abrine exhibited comparable ABTS radical cation scavenging activities and reducing power to two commercial antioxidants (BHT and Trolox). The EF exerted strong cellular antioxidant activity and selective cytotoxicity against three cancer cell lines in a dose-dependent manner. Biological assays revealed that the EF induced cell cycle arrest at G2/M and apoptosis in MCF-7 and Hep3B cells after 48 h of treatment. Thus, A. cantoniensis exerted potent cellular antioxidant and anti-proliferative properties, highlighting why it has been traditionally used as a functional food. PMID:25059572

  20. Synthesis, characterization, DNA interactions, DNA cleavage, radical scavenging activity, antibacterial, anti-proliferative and docking studies of new transition metal complexes.

    Science.gov (United States)

    Chennam, Kishan Prasad; Ravi, Mudavath; Ushaiah, B; Srinu, V; Eslavath, Ravi Kumar; Devi, Ch Sarala

    2016-01-01

    The compound N-(2-hydroxybenzylidene)-1-ethyl-1, 4-dihydro-7-methyl-4-oxo-1, 8 naphthyridine-3-carbohydrazide (LH) and its Cu (II), Co (II) and Zn (II) complexes were synthesized and characterized. The absorption spectral titrations and competitive DNA binding studies depicted those complexes of title compound bind to CT-DNA through intercalation. Interestingly [Cu (II)-(L2)] showed relatively high binding constant value (6.61 x 10(5) M(-1)) compared to [Co (II)-(L2)] (4.378× 10(5) M(-1)) and [Zn (II)-(L2)] (3.1x10(5) M(-1)). Ligand and its complexes were also examined for DNA nuclease activity against pBR-322 plasmid DNA, which showed that [Cu (II)-(L2)] had the best hydrolytic cleavage property displaying prominent double-strand DNA cleavage. In addition, antioxidant activities of the ligand and its metal complexes investigated through scavenging effects for DPPH radical in- vitro, indicated their potentiality as good antioxidants. The in vitro anti-bacterial study inferred the better anti-bacterial activity of [Cu (II)-(L2)] and this was also correlated theoretically by employing docking studies wherein [Cu (II)-(L2)] displayed good Gold score and Chem score. Finally the in vitro anti- proliferative activity of studied compounds was tested against HeLa and MCF-7 cell lines. Interestingly [Cu (II)-(L2)] displayed lower IC50 value and lower percentage of viability in both HeLa and MCF-7 cell lines.

  1. Cytotoxic Compounds from Juglans sinensis Dode Display Anti-Proliferative Activity by Inducing Apoptosis in Human Cancer Cells.

    Science.gov (United States)

    Lee, Yoo Jin; Cui, Jun; Lee, Jun; Han, Ah-Reum; Lee, Eun Byul; Jang, Ho Hee; Seo, Eun Kyoung

    2016-01-01

    Phytochemical investigation of the bark of Juglans sinensis Dode (Juglandaceae) led to the isolation of two active compounds, 8-hydroxy-2-methoxy-1,4-naphthoquinone (1) and 5-hydroxy-2-methoxy-1,4-naphthoquinone (2), together with 15 known compounds 3-17. All compounds were isolated from this plant for the first time. The structures of 1 and 2 were elucidated by spectroscopic data analysis, including 1D and 2D NMR experiments. Compounds 1-17 were tested for their cytotoxicity against the A549 human lung cancer cell line; compounds 1 and 2 exhibited significant cytotoxicity and additionally had potent cytotoxicity against six human cancer cell lines, MCF7 (breast cancer), SNU423 (liver cancer), SH-SY5Y (neuroblastoma), HeLa (cervical cancer), HCT116 (colorectal cancer), and A549 (lung cancer). In particular, breast, colon, and lung cancer cells were more sensitive to the treatment using compound 1. In addition, compounds 1 and 2 showed strong cytotoxic activity towards human breast cancer cells MCF7, HS578T, and T47D, but not towards MCF10A normal-like breast cells. They also inhibited the colony formation of MCF7, A549, and HCT116 cells in a dose-dependent manner. Flow cytometry analysis revealed that the percentage of apoptotic cells significantly increased in MCF7 cells upon the treatment with compounds 1 and 2. The mechanism of cell death caused by compounds 1 and 2 may be attributed to the upregulation of Bax and downregulation of Bcl2. These findings suggest that compounds 1 and 2 may be regarded as potential therapeutic agents against cancer.

  2. Furanodiene presents synergistic anti-proliferative activity with paclitaxel via altering cell cycle and integrin signaling in 95-D lung cancer cells.

    Science.gov (United States)

    Xu, Wen-Shan; Dang, Yuan-Ye; Chen, Xiu-Ping; Lu, Jin-Jian; Wang, Yi-Tao

    2014-02-01

    Furanodiene (FUR) is a natural terpenoid isolated from Rhizoma Curcumae, a well-known Chinese medicinal herb that presents anti-proliferative activities in several cancer cell lines. Recently, we found that the combined treatment of FUR with paclitaxel (TAX) showed synergetic anti-proliferative activities in 95-D lung cancer cells. Herein, we showed that FUR reduced the cell numbers distributed in mitosis phase induced by TAX while increased those in G1 phase. The protein levels of cyclin D1, cyclin B1, CDK6 and c-Myc were all down-regulated in the group of combined treatment. The dramatically down-regulated expression of integrin β4, focal adhesion kinase and paxillin might partially contribute to the synergic effect. Though FUR alone obviously induced endoplasmic reticulum stress, this signaling pathway may not contribute to the synergetic anti-proliferative effect as the protein expression of CHOP and BIP was similar in FUR alone and combined treatment group.

  3. Chemical Composition, Antioxidant, Anti-Inflammatory and Anti-Proliferative Activities of Essential Oils of Plants from Burkina Faso

    Science.gov (United States)

    Bayala, Bagora; Bassole, Imaël Henri Nestor; Gnoula, Charlemagne; Nebie, Roger; Yonli, Albert; Morel, Laurent; Figueredo, Gilles; Nikiema, Jean-Baptiste; Lobaccaro, Jean-Marc A.; Simpore, Jacques

    2014-01-01

    This research highlights the chemical composition, antioxidant, anti-inflammatory and anti-proliferative activities of essential oils from leaves of Ocimum basilicum, Ocimum americanum, Hyptis spicigera, Lippia multiflora, Ageratum conyzoides, Eucalyptus camaldulensis and Zingiber officinale. Essential oils were analyzed by gas chromatography–mass spectrometry and gas chromatography–flame ionization detector. Major constituents were α-terpineol (59.78%) and β-caryophyllene (10.54%) for Ocimum basilicum; 1, 8-cineol (31.22%), camphor (12.730%), α-pinene (6.87%) and trans α-bergamotene (5.32%) for Ocimum americanum; β-caryophyllene (21%), α-pinene (20.11%), sabinene (10.26%), β-pinene (9.22%) and α-phellandrene (7.03%) for Hyptis spicigera; p-cymene (25.27%), β-caryophyllene (12.70%), thymol (11.88), γ-terpinene (9.17%) and thymyle acetate (7.64%) for Lippia multiflora; precocene (82.10%)for Ageratum conyzoides; eucalyptol (59.55%), α-pinene (9.17%) and limonene (8.76%) for Eucalyptus camaldulensis; arcurcumene (16.67%), camphene (12.70%), zingiberene (8.40%), β-bisabolene (7.83%) and β-sesquiphellandrène (5.34%) for Zingiber officinale. Antioxidant activities were examined using 1,1-diphenyl-2-picryl-hydrazyl (DPPH) and 2,2′-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid (ABTS) methods. O. basilicum and L. multiflora exhibited the highest antioxidant activity in DPPH and ABTS tests, respectively. Anti-inflammatory properties were evaluated by measuring the inhibition of lipoxygenase activity and essential oil of Z. officinale was the most active. Anti-proliferative effect was assayed by the measurement of MTT on LNCaP and PC-3 prostate cancer cell lines, and SF-763 and SF-767 glioblastoma cell lines. Essential oils from A. conyzoides and L. multiflora were the most active on LNCaP and PC-3 cell lines, respectively. The SF-767 glioblastoma cell line was the most sensitive to O. basilicum and L. multiflora EOs while essential oil of A. conyzoides

  4. Chemical composition, antioxidant, anti-inflammatory and anti-proliferative activities of essential oils of plants from Burkina Faso.

    Science.gov (United States)

    Bayala, Bagora; Bassole, Imaël Henri Nestor; Gnoula, Charlemagne; Nebie, Roger; Yonli, Albert; Morel, Laurent; Figueredo, Gilles; Nikiema, Jean-Baptiste; Lobaccaro, Jean-Marc A; Simpore, Jacques

    2014-01-01

    This research highlights the chemical composition, antioxidant, anti-inflammatory and anti-proliferative activities of essential oils from leaves of Ocimum basilicum, Ocimum americanum, Hyptis spicigera, Lippia multiflora, Ageratum conyzoides, Eucalyptus camaldulensis and Zingiber officinale. Essential oils were analyzed by gas chromatography-mass spectrometry and gas chromatography-flame ionization detector. Major constituents were α-terpineol (59.78%) and β-caryophyllene (10.54%) for Ocimum basilicum; 1, 8-cineol (31.22%), camphor (12.730%), α-pinene (6.87%) and trans α-bergamotene (5.32%) for Ocimum americanum; β-caryophyllene (21%), α-pinene (20.11%), sabinene (10.26%), β-pinene (9.22%) and α-phellandrene (7.03%) for Hyptis spicigera; p-cymene (25.27%), β-caryophyllene (12.70%), thymol (11.88), γ-terpinene (9.17%) and thymyle acetate (7.64%) for Lippia multiflora; precocene (82.10%)for Ageratum conyzoides; eucalyptol (59.55%), α-pinene (9.17%) and limonene (8.76%) for Eucalyptus camaldulensis; arcurcumene (16.67%), camphene (12.70%), zingiberene (8.40%), β-bisabolene (7.83%) and β-sesquiphellandrène (5.34%) for Zingiber officinale. Antioxidant activities were examined using 1,1-diphenyl-2-picryl-hydrazyl (DPPH) and 2,2'-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid (ABTS) methods. O. basilicum and L. multiflora exhibited the highest antioxidant activity in DPPH and ABTS tests, respectively. Anti-inflammatory properties were evaluated by measuring the inhibition of lipoxygenase activity and essential oil of Z. officinale was the most active. Anti-proliferative effect was assayed by the measurement of MTT on LNCaP and PC-3 prostate cancer cell lines, and SF-763 and SF-767 glioblastoma cell lines. Essential oils from A. conyzoides and L. multiflora were the most active on LNCaP and PC-3 cell lines, respectively. The SF-767 glioblastoma cell line was the most sensitive to O. basilicum and L. multiflora EOs while essential oil of A. conyzoides

  5. Chemical composition, antioxidant, anti-inflammatory and anti-proliferative activities of essential oils of plants from Burkina Faso.

    Directory of Open Access Journals (Sweden)

    Bagora Bayala

    Full Text Available This research highlights the chemical composition, antioxidant, anti-inflammatory and anti-proliferative activities of essential oils from leaves of Ocimum basilicum, Ocimum americanum, Hyptis spicigera, Lippia multiflora, Ageratum conyzoides, Eucalyptus camaldulensis and Zingiber officinale. Essential oils were analyzed by gas chromatography-mass spectrometry and gas chromatography-flame ionization detector. Major constituents were α-terpineol (59.78% and β-caryophyllene (10.54% for Ocimum basilicum; 1, 8-cineol (31.22%, camphor (12.730%, α-pinene (6.87% and trans α-bergamotene (5.32% for Ocimum americanum; β-caryophyllene (21%, α-pinene (20.11%, sabinene (10.26%, β-pinene (9.22% and α-phellandrene (7.03% for Hyptis spicigera; p-cymene (25.27%, β-caryophyllene (12.70%, thymol (11.88, γ-terpinene (9.17% and thymyle acetate (7.64% for Lippia multiflora; precocene (82.10%for Ageratum conyzoides; eucalyptol (59.55%, α-pinene (9.17% and limonene (8.76% for Eucalyptus camaldulensis; arcurcumene (16.67%, camphene (12.70%, zingiberene (8.40%, β-bisabolene (7.83% and β-sesquiphellandrène (5.34% for Zingiber officinale. Antioxidant activities were examined using 1,1-diphenyl-2-picryl-hydrazyl (DPPH and 2,2'-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid (ABTS methods. O. basilicum and L. multiflora exhibited the highest antioxidant activity in DPPH and ABTS tests, respectively. Anti-inflammatory properties were evaluated by measuring the inhibition of lipoxygenase activity and essential oil of Z. officinale was the most active. Anti-proliferative effect was assayed by the measurement of MTT on LNCaP and PC-3 prostate cancer cell lines, and SF-763 and SF-767 glioblastoma cell lines. Essential oils from A. conyzoides and L. multiflora were the most active on LNCaP and PC-3 cell lines, respectively. The SF-767 glioblastoma cell line was the most sensitive to O. basilicum and L. multiflora EOs while essential oil of A. conyzoides showed the

  6. Platycodin D from Platycodonis Radix enhances the anti-proliferative effects of doxorubicin on breast cancer MCF-7 and MDA-MB-231 cells

    OpenAIRE

    Tang, Zheng-Hai; Li, Ting; Gao, Hong-wei; Sun, Wen; Chen, Xiu-Ping; Wang, Yi-Tao; Lu, Jin-jian

    2014-01-01

    Background It has been demonstrated that platycodin D (PD) exhibits anti-cancer activities. This study aims to investigate the anti-proliferative effects of the combination of PD and doxorubicin (DOX) on human breast cancer cells (MCF-7 and MDA-MB-231 cells). Methods The anti-proliferative effects of different dosages of PD, DOX, and PD + DOX on MCF-7 and MDA-MB-231 cells were determined by the MTT assay. The 10 μM PD, 5 μM DOX, and 10 μM PD + 5 μM DOX induced-protein expression of apoptosis-...

  7. The nontoxic natural compound Curcumin exerts anti-proliferative, anti-migratory, and anti-invasive properties against malignant gliomas

    International Nuclear Information System (INIS)

    New drugs are constantly sought after to improve the survival of patients with malignant gliomas. The ideal substance would selectively target tumor cells without eliciting toxic side effects. Here, we report on the anti-proliferative, anti-migratory, and anti-invasive properties of the natural, nontoxic compound Curcumin observed in five human glioblastoma (GBM) cell lines in vitro. We used monolayer wound healing assays, modified Boyden chamber trans-well assays, and cell growth assays to quantify cell migration, invasion, and proliferation in the absence or presence of Curcumin at various concentrations. Levels of the transcription factor phospho-STAT3, a potential target of Curcumin, were determined by sandwich-ELISA. Subsequent effects on transcription of genes regulating the cell cycle were analyzed by quantitative real-time PCR. Effects on apoptosis were determined by caspase assays. Curcumin potently inhibited GBM cell proliferation as well as migration and invasion in all cell lines contingent on dose. Simultaneously, levels of the biologically active phospho-STAT3 were decreased and correlated with reduced transcription of the cell cycle regulating gene c-Myc and proliferation marking Ki-67, pointing to a potential mechanism by which Curcumin slows tumor growth. Curcumin is part of the diet of millions of people every day and is without known toxic side effects. Our data show that Curcumin bears anti-proliferative, anti-migratory, and anti-invasive properties against GBM cells in vitro. These results warrant further in vivo analyses and indicate a potential role of Curcumin in the treatment of malignant gliomas

  8. Probing the GnRH receptor agonist binding site identifies methylated triptorelin as a new anti-proliferative agent

    Directory of Open Access Journals (Sweden)

    Robert P Millar

    2012-06-01

    Full Text Available D-amino acid substitutions at Glycine postion-6 in GnRH-I decapeptide can possess super-agonist activity and enhanced in vivo pharmacokinetics. Agonists elicit growth-inhibition in tumorigenic cells expressing the GnRH receptor above threshold levels. However, new agonists with modified properties are required to improve the anti-proliferative range. Effects of residue substitutions and methylations on tumourigenic HEK293[SCL60] and WPE-1-NB26-3 prostate cells expressing the rat GnRH receptor were compared. Peptides were ranked according to receptor binding affinity, induction of inositol phosphate production and cell growth-inhibition. Analogues possessing D-Trp6 (including Triptorelin, D-Leu6 (including Leuprolide, D-Ala6, D-Lys6, or D-Arg6 exhibited agonist and anti-proliferative activity. Residues His5 or His5,Trp7,Tyr8, corresponding to residues found in GnRH-II , were tolerated, with retention of sub-nanomolar/low nanomolar binding affinities and EC50s for receptor activation and IC50s for cell growth-inhibition. His5D-Arg6-GnRH-I exhibited reduced binding affinity and potency, effective in the mid-nanomolar range. However, all GnRH-II-like analogues were less potent than Triptorelin. By comparison, three methylated-Trp6 Triptorelin variants showed differential binding, receptor activation and anti-proliferation potency. Significantly, 5-Methyl-DL-Trp6-Triptorelin was equipotent to triptorelin. Subsequent studies should determine whether pharmacologically enhanced derivatives of Triptorelin can be developed by further alkylations, without substitutions or cleavable cytotoxic adducts, to improve the extent of growth-inhibition of tumour cells expressing the GnRH receptor.

  9. Anti-proliferative activity of hop-derived prenylflavonoids against human cancer cell lines.

    Science.gov (United States)

    Busch, Christian; Noor, Seema; Leischner, Christian; Burkard, Markus; Lauer, Ulrich M; Venturelli, Sascha

    2015-06-01

    Flavonoids form a substantial group of secondary plant metabolites that display several health-promoting effects. Therefore, prenylflavonoids, a subclass of flavonoids, have attracted increasing attention. Here, we investigated the possible anti-cancer potential of 6-prenylnaringenin (6-PN) and 8-prenylnaringenin (8-PN), two prenylflavonoids present in hops and beer and demonstrate an unexpectedly pronounced, dose-dependent reduction of cellular proliferation of human PC-3 prostate cancer and UO.31 renal carcinoma cells upon treatment. Based on these findings 6-PN and 8-PN are currently further clinically evaluated in detail. PMID:25925225

  10. Capsaicin for Rhinitis.

    Science.gov (United States)

    Fokkens, Wytske; Hellings, Peter; Segboer, Christine

    2016-08-01

    Rhinitis is a multifactorial disease characterized by symptoms of sneezing, rhinorrhea, postnasal drip, and nasal congestion. Non-allergic rhinitis is characterized by rhinitis symptoms without systemic sensitization of infectious etiology. Based on endotypes, we can categorize non-allergic rhinitis into an inflammatory endotype with usually eosinophilic inflammation encompassing at least NARES and LAR and part of the drug induced rhinitis (e.g., aspirin intolerance) and a neurogenic endotype encompassing idiopathic rhinitis, gustatory rhinitis, and rhinitis of the elderly. Patients with idiopathic rhinitis have a higher baseline TRPV1 expression in the nasal mucosa than healthy controls. Capsaicin (8-methyl-N-vanillyl-6-nonenamide) is the active component of chili peppers, plants of the genus Capsicum. Capsaicin is unique among naturally occurring irritant compounds because the initial neuronal excitation evoked by it is followed by a long-lasting refractory period, during which the previously excited neurons are no longer responsive to a broad range of stimuli. Patients with idiopathic rhinitis benefit from intranasal treatment with capsaicin. Expression of TRPV1 is reduced in patients with idiopathic rhinitis after capsaicin treatment. Recently, in a Cochrane review, the effectiveness of capsaicin in the management of idiopathic rhinitis was evaluated and the authors concluded that given that many other options do not work well in non-allergic rhinitis, capsaicin is a reasonable option to try under physician supervision. Capsaicin has not been shown to be effective in allergic rhinitis nor in other forms of non-allergic rhinitis like the inflammatory endotypes or other neurogenic endotypes like rhinitis of the elderly or smoking induced rhinitis. PMID:27485456

  11. Apocynaceae species with anti proliferative and/or antiplasmodial properties:a review of ten genera

    Institute of Scientific and Technical Information of China (English)

    Eric Wei Chiang Chan; Siu Kuin Wong; Hung Tuck Chan

    2016-01-01

    Apocynaceae is a large family of tropical trees, shrubs and vines with most species producing white latex. Major metabolites of species are triterpenoids, iridoids, alkaloids and cardenolides, which are known for a wide range of biological and pharmacological activities such as cardioprotective, hepatoprotective, neuroprotective, anti-infl ammatory, anticancer and antimalarial properties. Prompted by their anticancer and antimalarial properties, the current knowledge on ten genera (Allamanda,Alstonia,Calotropis, Catharanthus,Cerbera,Dyera,Kopsia,Nerium,Plumeria andVallaris) is updated. Major classes of metabolites are described using some species as examples. Species with antiproliferative (APF) and/or antiplasmodial (APM) properties have been identifi ed. With the exception of the genusDyera, nine genera of 22 species possess APF activity. Seven genera (Alstonia,Calotropis,Catharanthus,Dyera, Kopsia,PlumeriaandVallaris) of 13 species have APM properties. Among these species,Alstonia angustiloba,Alstonia macrophylla,Calotropis gigantea,Calotropis procera,Catharanthus roseus, Plumeria alba andValaris glabra displayed both APF and APM properties. The chemical constituents of these seven species are compiled for assessment and further research.

  12. Capsaicin, Nociception and Pain

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    Bárbara Frias

    2016-06-01

    Full Text Available Capsaicin, the pungent ingredient of the hot chili pepper, is known to act on the transient receptor potential cation channel vanilloid subfamily member 1 (TRPV1. TRPV1 is involved in somatic and visceral peripheral inflammation, in the modulation of nociceptive inputs to spinal cord and brain stem centers, as well as the integration of diverse painful stimuli. In this review, we first describe the chemical and pharmacological properties of capsaicin and its derivatives in relation to their analgesic properties. We then consider the biochemical and functional characteristics of TRPV1, focusing on its distribution and biological effects within the somatosensory and viscerosensory nociceptive systems. Finally, we discuss the use of capsaicin as an agonist of TRPV1 to model acute inflammation in slices and other ex vivo preparations.

  13. Capsaicin, Nociception and Pain.

    Science.gov (United States)

    Frias, Bárbara; Merighi, Adalberto

    2016-01-01

    Capsaicin, the pungent ingredient of the hot chili pepper, is known to act on the transient receptor potential cation channel vanilloid subfamily member 1 (TRPV1). TRPV1 is involved in somatic and visceral peripheral inflammation, in the modulation of nociceptive inputs to spinal cord and brain stem centers, as well as the integration of diverse painful stimuli. In this review, we first describe the chemical and pharmacological properties of capsaicin and its derivatives in relation to their analgesic properties. We then consider the biochemical and functional characteristics of TRPV1, focusing on its distribution and biological effects within the somatosensory and viscerosensory nociceptive systems. Finally, we discuss the use of capsaicin as an agonist of TRPV1 to model acute inflammation in slices and other ex vivo preparations. PMID:27322240

  14. Phytochemical profile of Rosmarinus officinalis and Salvia officinalis extracts and correlation to their antioxidant and anti-proliferative activity.

    Science.gov (United States)

    Kontogianni, Vassiliki G; Tomic, Goran; Nikolic, Ivana; Nerantzaki, Alexandra A; Sayyad, Nisar; Stosic-Grujicic, Stanislava; Stojanovic, Ivana; Gerothanassis, Ioannis P; Tzakos, Andreas G

    2013-01-01

    The goal of this study was to monitor the anti-proliferative activity of Rosmarinus officinalis and Salvia officinalis extracts against cancer cells and to correlate this activity with their phytochemical profiles using liquid chromatography/diode array detection/electrospray ion trap tandem mass spectrometry (LC/DAD/ESI-MS(n)). For the quantitative estimation of triterpenic acids in the crude extracts an NMR based methodology was used and compared with the HPLC measurements, both applied for the first time, for the case of betulinic acid. Both extracts exerted cytotoxic activity through dose-dependent impairment of viability and mitochondrial activity of rat insulinoma m5F (RINm5F) cells. Decrease of RINm5F viability was mediated by nitric oxide (NO)-induced apoptosis. Importantly, these extracts potentiated NO and TNF-α release from macrophages therefore enhancing their cytocidal action. The rosemary extract developed more pronounced antioxidant, cytotoxic and immunomodifying activities, probably due to the presence of betulinic acid and a higher concentration of carnosic acid in its phytochemical profile.

  15. Anti-proliferative and apoptotic effects of S1, a tetrandrine derivative, in human gastric cancer BGC-823 cells.

    Science.gov (United States)

    Lei, Rong-Rong; Hu, Hai-Feng; Bai, Fan; Liu, Ying; Wu, Chun-Zhen; Huang, Xiao-Xing; Xie, Li-Ping; Hu, You-Jia

    2016-07-01

    The aim of the study was to investigate the anti-proliferation and apoptosis-inducing effects of S1, a novel tetrandrine derivative, in human gastric cancer BGC-823 cells and explore the possible mechanism of action. The anti-proliferative activity was determined by MTT assay; the induction of cell cycle arrest and apoptosis were detected by flow cytometry. Quantitative real time RT-PCR and Western blotting were used to evaluate the mRNA and protein expression levels in mitochondrial pathway. S1 significantly reduced cell viability and induced a G2/M phase arrest and apoptosis in dose- and time-dependent manner. Further studies showed that S1 increased mRNA and protein expression of Bax and the Bax/Bcl-2 ratio. Moreover, S1 decreased the protein expression of procaspase-9 and procaspase-3, suggesting that the induction of apoptosis may be related to the alteration of the ratio of Bax/Bcl-2 and the activation of caspases. These findings suggested that S1 merits further investigation as a novel therapeutic agent for the treatment of human gastric cancer.

  16. Biological Characterization of Cynara cardunculus L. Methanolic Extracts: Antioxidant, Anti-proliferative, Anti-migratory and Anti-angiogenic Activities

    Directory of Open Access Journals (Sweden)

    Maria Duarte

    2012-12-01

    Full Text Available Cynara cardunculus (Cc is a multipurpose species; beyond its use in southwestern European cuisine, it is also used for the production of solid biofuel, seed oil, biodiesel, paper pulp and cheese, as well as animal feed. In addition, Cc has a long tradition of use in folk medicine as a diuretic and liver protector. The value of this species as a source of bioactive compounds is known; however, pharmacological use would further increase its cultivation. The main goal of the current work was to evaluate the potential of Cc as source of anti-carcinogenic phytochemicals. Different methanolic extracts obtained from wild and cultivated plants were tested for antioxidant activity and effect on breast tumor cell viability. The most effective extract, both as antioxidant and inhibition of tumor cell viability, was tested for effects on angiogenesis and tumor cell migration capacity. All the extracts tested had high antioxidant activity; however, only green leaves and dry head extracts exhibit anti-proliferative activity. Green cultivated leaves (GCL were the most effective extract both as antioxidant and inhibiting the proliferation of tumor cells; it is equally active inhibiting tumor cell migration and in vivo angiogenesis. GCL extract is an effective inhibitor of several key points in tumor development and thus a promising source of anti-carcinogenic phytochemicals.

  17. Biosynthesis of Anti-Proliferative Gold Nanoparticles Using Endophytic Fusarium oxysporum Strain Isolated from Neem (A. indica) Leaves.

    Science.gov (United States)

    Siddiqui, Ejaz Ahmad; Ahmad, Absar; Julius, Anju; Syed, Asad; Khan, Shadab; Kharat, Mahesh; Pai, Kalpana; Kadoo, Narendra; Gupta, Vidya

    2016-01-01

    Here we report a simple, rapid, environment friendly approach for the synthesis of gold nanoparticles using neem (Azadirachta indica A. Juss.) fungal endophyte, which based upon morphological and cultural characteristics was eventually identified as Fusarium oxysporum. The aqueous precursor (HAuCl4) solution when reacted with endophytic fungus resulted in the biosynthesis of abundant amounts of well dispersed gold nanoparticles of 10-40 nm with an average size of 22nm. These biosynthesized gold nanoparticles were then characterized by standard analytical techniques such as UV-Visible spectroscopy, X-ray diffraction, Transmission Electron Microscopy and Fourier Transform Infrared Spectroscopy. Cytotoxic activity of these nanoparticles was checked against three different cell types including breast cancer (ZR-75-1), Daudi (Human Burkitt's lymphoma cancer) and normal human peripheral blood mononuclear cells (PBMC), where it was found that our gold nanoparticles are anti-proliferative against cancer cells but completely safe toward normal cells. In addition to this, assessment of toxicity toward human RBC revealed less than 0.1 % hemolysis as compared to Triton X-100 suggesting safe nature of our biosynthesized gold nanoparticles on human cells. Also, our nanoparticles exhibited no anti-fungal (against Aspergillus niger) or anti-bacterial [against Gram positive (Bacillus subtilis & Staphylococcus aureus) and Gram negative (Escherichia coli & Pseudomonas aeruginosa) bacteria] activity thus suggesting their non-toxic, biocompatible nature. The present investigation opens up avenues for ecofriendly, biocompatible nanomaterials to be used in a wide variety of application such as drug delivery, therapeutics, theranostics and so on.

  18. A novel microtubule inhibitor 4SC-207 with anti-proliferative activity in taxane-resistant cells.

    Directory of Open Access Journals (Sweden)

    Elena Bausch

    Full Text Available Microtubule inhibitors are invaluable tools in cancer chemotherapy: taxanes and vinca alkaloids have been successfully used in the clinic over the past thirty years against a broad range of tumors. However, two factors have limited the effectiveness of microtubule inhibitors: toxicity and resistance. In particular, the latter is highly unpredictable, variable from patient to patient and is believed to be the cause of treatment failure in most cases of metastatic cancers. For these reasons, there is an increasing demand for new microtubule inhibitors that can overcome resistance mechanisms and that, at the same time, have reduced side effects. Here we present a novel microtubule inhibitor, 4SC-207, which shows strong anti-proliferative activity in a large panel of tumor cell lines with an average GI50 of 11 nM. In particular, 4SC-207 is active in multi-drug resistant cell lines, such as HCT-15 and ACHN, suggesting that it is a poor substrate for drug efflux pumps. 4SC-207 inhibits microtubule growth in vitro and in vivo and promotes, in a dose dependent manner, a mitotic delay/arrest, followed by apoptosis or aberrant divisions due to chromosome alignment defects and formation of multi-polar spindles. Furthermore, preliminary data from preclinical studies suggest low propensity towards bone marrow toxicities at concentrations that inhibit tumor growth in paclitaxel-resistant xenograft models. In summary, our results suggest that 4SC-207 may be a potential anti-cancer agent.

  19. Conformational study reveals amino acid residues essential for hemagglutinating and anti-proliferative activities of Clematis montana lectin.

    Science.gov (United States)

    Lu, Bangmin; Zhang, Bin; Qi, Wei; Zhu, Yanan; Zhao, Yan; Zhou, Nan; Sun, Rong; Bao, Jinku; Wu, Chuanfang

    2014-11-01

    Clematis montana lectin (CML), a novel mannose-binding lectin purified from C. montana Buch.-Ham stem (Ranunculaceae), has been proved to have hemagglutinating activity in rabbit erythrocytes and apoptosis-inducing activity in tumor cells. However, the biochemical properties of CML have not revealed and its structural information still needs to be elucidated. In this study, it was found that CML possessed quite good thermostability and alkaline resistance, and its hemagglutinating activity was bivalent metal cation dependent. In addition, hemagglutination test and fluorescence spectroscopy proved that GuHCl, urea, and sodium dodecyl sulfate could change the conformation of CML and further caused the loss of hemagglutination activity. Moreover, the changes of fluorescence spectrum indicated that the tryptophan (Trp) microenvironment conversion might be related to the conformation and bioactivities of CML. In addition, it was also found that Trp residues, arginine (Arg) residues, and sulfhydryl were important for the hemagglutinating activity of CML, but only Trp was proved to be crucial for the CML conformation. Furthermore, the Trp, Arg, and sulfhydryl-modified CML exhibited 97.17%, 76.99%, and 49.64% loss of its anti-proliferative activity, respectively, which was consistent with the alterations of its hemagglutinating activity. Given these findings, Trp residues on the surface of CML are essential for the active center to form substrate-accessible conformation and suitable environment for carbohydrate binding. PMID:25239139

  20. Hybrid surfactants decorated with copper ions: aggregation behavior, antimicrobial activity and anti-proliferative effect.

    Science.gov (United States)

    Kaur, Gurpreet; Kumar, Sandeep; Dilbaghi, Neeraj; Bhanjana, Gaurav; Guru, Santosh Kumar; Bhushan, Shashi; Jaglan, Sundeep; Hassan, P A; Aswal, V K

    2016-09-14

    In the present study, the emphasis is laid on the self aggregation behavior of copper based inorganic-organic hybrids in aqueous media. The two complexes, cationic hexadecyl pyridinium trichloro cuprate (1 : 1), [Cp](+)[CuCl3](-), and bishexadecylpyridinium tetrachloro cuprate (2 : 1), [Cp2](2+)[CuCl4](2-), were synthesized using the ligand insertion method. The complexes were characterized using elemental analysis, Fourier transform infrared spectroscopy (FTIR), X-ray diffraction (XRD), nuclear magnetic resonance (NMR) and thermogravimetric analysis. The copper complexes were found to be thermally stable, and in the solid state, they possessed the perovskite arrangement with [Cp2](2+)[CuCl4](2-) exhibiting superior stability and crystallinity. The self aggregation behavior of the prepared complexes was analyzed in solution phase (in aqueous medium) using surface tension, conductivity, XRD and small angle neutron scattering (SANS). The results show that the presence of copper as a co-ion in both the stoichiometries results in lower critical micellization concentrations than their precursor. Micellization was thermodynamically spontaneous and micelles formed were ellipsoidal in shape and underwent a prolate ellipsoidal growth with an increase in the concentration of metallosurfactant, as estimated from the SANS. Furthermore, these metallosurfactants were investigated for biocompatibility (using hemolytic assay), antimicrobial activity (fungus and bacteria) and cytotoxicity using human cancerous cells. The hemolysis activity was found to depend on the aggregated state of the metallosurfactants, displaying the highest activity in the monomeric state, and the minimum for post micellar concentrations. The surfactants were found to enhance the antibacterial activity by twofold or more, with the addition of metal in both the stoichiometries. On the contrary, for anticancer and antifungal activities, barely any regular trend or generalization could be obtained

  1. Hybrid surfactants decorated with copper ions: aggregation behavior, antimicrobial activity and anti-proliferative effect.

    Science.gov (United States)

    Kaur, Gurpreet; Kumar, Sandeep; Dilbaghi, Neeraj; Bhanjana, Gaurav; Guru, Santosh Kumar; Bhushan, Shashi; Jaglan, Sundeep; Hassan, P A; Aswal, V K

    2016-09-14

    In the present study, the emphasis is laid on the self aggregation behavior of copper based inorganic-organic hybrids in aqueous media. The two complexes, cationic hexadecyl pyridinium trichloro cuprate (1 : 1), [Cp](+)[CuCl3](-), and bishexadecylpyridinium tetrachloro cuprate (2 : 1), [Cp2](2+)[CuCl4](2-), were synthesized using the ligand insertion method. The complexes were characterized using elemental analysis, Fourier transform infrared spectroscopy (FTIR), X-ray diffraction (XRD), nuclear magnetic resonance (NMR) and thermogravimetric analysis. The copper complexes were found to be thermally stable, and in the solid state, they possessed the perovskite arrangement with [Cp2](2+)[CuCl4](2-) exhibiting superior stability and crystallinity. The self aggregation behavior of the prepared complexes was analyzed in solution phase (in aqueous medium) using surface tension, conductivity, XRD and small angle neutron scattering (SANS). The results show that the presence of copper as a co-ion in both the stoichiometries results in lower critical micellization concentrations than their precursor. Micellization was thermodynamically spontaneous and micelles formed were ellipsoidal in shape and underwent a prolate ellipsoidal growth with an increase in the concentration of metallosurfactant, as estimated from the SANS. Furthermore, these metallosurfactants were investigated for biocompatibility (using hemolytic assay), antimicrobial activity (fungus and bacteria) and cytotoxicity using human cancerous cells. The hemolysis activity was found to depend on the aggregated state of the metallosurfactants, displaying the highest activity in the monomeric state, and the minimum for post micellar concentrations. The surfactants were found to enhance the antibacterial activity by twofold or more, with the addition of metal in both the stoichiometries. On the contrary, for anticancer and antifungal activities, barely any regular trend or generalization could be obtained

  2. Anti-proliferative properties of commercial Pelargonium sidoides tincture, with cell-cycle G0/G1 arrest and apoptosis in Jurkat leukaemia cells.

    Science.gov (United States)

    Pereira, Andreia; Bester, Megan; Soundy, Puffy; Apostolides, Zeno

    2016-09-01

    Context Pelargonium sidoides DC (Geraniaceae) is an important medicinal plant indigenous to South Africa and Lesotho. Previous studies have shown that root extracts are rich in polyphenolic compounds with antibacterial, antiviral and immunomodulatory activities. Little is known regarding the anticancer properties of Pelargonium sidoides extracts. Objective This study evaluates the anti-proliferative effects of a Pelargonium sidoides radix mother tincture (PST). Materials and methods The PST was characterized by LC-MS/MS. Anti-proliferative activity was evaluated in the pre-screen panel of the National Cancer Institute (NCI-H460, MCF-7 and SF-268) and the Jurkat leukaemia cell line at concentrations of 0-150 μg/mL. The effect on cell growth was determined with sulphorhodamine B and 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assays after 72 h. The effect on cell cycle and apoptosis induction in Jurkat cells was determined by flow cytometry with propidium iodide and Annexin V: fluorescein isothiocyanate staining. Results Dihydroxycoumarin sulphates, gallic acid as well as gallocatechin dimers and trimers were characterized in PST by mass spectrometry. Moderate anti-proliferative effects with GI50 values between 40 and 80 μg/mL were observed in the NCI-pre-screen panel. Strong activity observed with Jurkat cells with a GI50 value of 6.2 μg/mL, significantly better than positive control 5-fluorouracil (GI50 value of 9.7 μg/mL). The PST arrested Jurkat cells at the G0/G1 phase of the cell cycle and increased the apoptotic cells from 9% to 21%, while the dead cells increased from 4% to 17%. Conclusion We present evidence that P. sidoides has cancer cell type-specific anti-proliferative effects and may be a source of novel anticancer molecules. PMID:26794080

  3. Role of VDR in anti-proliferative effects of calcitriol in tumor-derived endothelial cells and tumor angiogenesis in vivo

    OpenAIRE

    Chung, Ivy; Han, Guangzhou; Seshadri, Mukund; Gillard, Bryan M.; Yu, Wei-Dong; Barbara A Foster; Trump, Donald L.; Johnson, Candace S.

    2009-01-01

    Calcitriol (1, 25-dihydroxycholecalciferol), the major active form of vitamin D, is anti-proliferative in tumor cells and tumor-derived endothelial cells (TDEC). These actions of calcitriol are mediated at least in part by vitamin D receptor (VDR), which is expressed in many tissues including endothelial cells. To investigate the role of VDR in calcitriol effects on tumor vasculature, we established TRAMP-2 tumors subcutaneously into either VDR wild type (WT) or knockout (KO) mice. Within 30 ...

  4. Experimental and theoretical study of possible correlation between the electrochemistry of canthin-6-one and the anti-proliferative activity against human cancer stem cells

    Science.gov (United States)

    Cebrián-Torrejón, G.; Doménech-Carbó, A.; Scotti, M. T.; Fournet, A.; Figadère, B.; Poupon, E.

    2015-12-01

    This work presents an approach to study the performance of novel targets able to overcome cancer stem cell chemoresistance, based on the voltammetric data for microparticulate films of natural or synthetic alkaloids from the canthin-6-one series. A comparison of this voltammetric technique with conventional solution phase electrochemistry suggests the differences in the anti-proliferative activity of canthin-6-ones could be tentatively correlated to their different capacity to generate semiquinone radical anions. These data also match theoretical calculations.

  5. Anti-proliferative effects of raw and steamed extracts of Panax notoginseng and its ginsenoside constituents on human liver cancer cells

    Directory of Open Access Journals (Sweden)

    Neo Soek-Ying

    2011-01-01

    Full Text Available Abstract Background Panax notoginseng is a potential source of anticancer compounds. This study aims to investigate the effects of steaming on the chemical profile of P. notoginseng and the anti-proliferative effects of P. notoginseng on liver cancer cells. Methods Samples of powdered raw P. notoginseng roots were steamed for various durations. Extracts of the raw and steamed samples were subjected to ultra-high pressure liquid chromatography/mass spectrometry (UHPLC-MS analysis for chemical profiling. The anti-proliferative effects on three human liver cancer cells, namely SNU449, SNU182 and HepG2, were evaluated using colorimetric WST-1 assay. Results Steaming changed chromatographic and pharmacological profiles of P. notoginseng, causing differences in activities such as inhibition of cancer growth. Steamed P. notoginseng exhibited greater anti-proliferative effects against liver cancer cells (SNU449, SNU182 and HepG2 than its raw form; steaming up to 24 hours increased bioactivities. Steaming increased the concentrations of ginsenoside Rh2, Rk1, Rk3 and 20S-Rg3 and enhanced growth inhibition of liver cancer cells. Conclusion Steaming changes the chemical profile as well as anti-cancer biological activities of P. notoginseng. Steamed P. notoginseng contains potential compounds for the treatment of liver cancer.

  6. Biocatalytic polymer thin films: optimization of the multilayered architecture towards in situ synthesis of anti-proliferative drugs

    Science.gov (United States)

    Andreasen, Sidsel Ø.; Fejerskov, Betina; Zelikin, Alexander N.

    2014-03-01

    We report on the assembly of multi-layered polyelectrolyte thin films containing an immobilized enzyme to perform conversion of externally administered prodrugs and achieve delivery of the resulting therapeutics to adhering cells. Towards this goal, multi-layered coatings were assembled using poly(sodium styrene sulfonate) and poly(allylamine hydrochloride). Activity of the incorporated enzyme was quantified as a function of the assembly conditions, position of the enzyme within the multi-layered architecture, concentration of the enzyme in the adsorption solution, and concentration of the administered prodrug. Biocatalytic coatings exhibited sustained levels of enzymatic activity over at least one week of incubation in physiological buffers without signs of loss of activity of the enzyme. Developed enzyme-containing polymer films afforded zero-order release of the in situ synthesized cargo with kinetics of synthesis (nM per hour) covering at least 3 orders of magnitude. Internalization of the synthesized product by adhering cells was visualized using a fluorogenic enzyme substrate. Therapeutic utility of biocatalytic coatings was demonstrated using a myoblast cell line and a prodrug for the anti-proliferative agent, 5-fluorouridine. Taken together, this work presents a novel approach to delivery of small molecule drugs using multi-layered polymer thin films with utility in surface-mediated drug delivery, assembly of therapeutic implantable devices, and tissue engineering.We report on the assembly of multi-layered polyelectrolyte thin films containing an immobilized enzyme to perform conversion of externally administered prodrugs and achieve delivery of the resulting therapeutics to adhering cells. Towards this goal, multi-layered coatings were assembled using poly(sodium styrene sulfonate) and poly(allylamine hydrochloride). Activity of the incorporated enzyme was quantified as a function of the assembly conditions, position of the enzyme within the multi

  7. Imatinib mesylate exerts anti-proliferative effects on osteosarcoma cells and inhibits the tumour growth in immunocompetent murine models.

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    Bérengère Gobin

    Full Text Available Osteosarcoma is the most common primary malignant bone tumour characterized by osteoid production and/or osteolytic lesions of bone. A lack of response to chemotherapeutic treatments shows the importance of exploring new therapeutic methods. Imatinib mesylate (Gleevec, Novartis Pharma, a tyrosine kinase inhibitor, was originally developed for the treatment of chronic myeloid leukemia. Several studies revealed that imatinib mesylate inhibits osteoclast differentiation through the M-CSFR pathway and activates osteoblast differentiation through PDGFR pathway, two key cells involved in the vicious cycle controlling the tumour development. The present study investigated the in vitro effects of imatinib mesylate on the proliferation, apoptosis, cell cycle, and migration ability of five osteosarcoma cell lines (human: MG-63, HOS; rat: OSRGA; mice: MOS-J, POS-1. Imatinib mesylate was also assessed as a curative and preventive treatment in two syngenic osteosarcoma models: MOS-J (mixed osteoblastic/osteolytic osteosarcoma and POS-1 (undifferentiated osteosarcoma. Imatinib mesylate exhibited a dose-dependent anti-proliferative effect in all cell lines studied. The drug induced a G0/G1 cell cycle arrest in most cell lines, except for POS-1 and HOS cells that were blocked in the S phase. In addition, imatinib mesylate induced cell death and strongly inhibited osteosarcoma cell migration. In the MOS-J osteosarcoma model, oral administration of imatinib mesylate significantly inhibited the tumour development in both preventive and curative approaches. A phospho-receptor tyrosine kinase array kit revealed that PDGFRα, among 7 other receptors (PDFGFRβ, Axl, RYK, EGFR, EphA2 and 10, IGF1R, appears as one of the main molecular targets for imatinib mesylate. In the light of the present study and the literature, it would be particularly interesting to revisit therapeutic evaluation of imatinib mesylate in osteosarcoma according to the tyrosine-kinase receptor

  8. MicroRNA mir-16 is anti-proliferative in enterocytes and exhibits diurnal rhythmicity in intestinal crypts

    Energy Technology Data Exchange (ETDEWEB)

    Balakrishnan, Anita, E-mail: anita.balakrishnan@doctors.org.uk [Department of Surgery, Brigham and Women' s Hospital, Boston, MA 02115 (United States); Department of Surgery, Harvard Medical School, Boston, MA 02115 (United States); School of Clinical Sciences, Division of Gastroenterology, University of Liverpool, Liverpool L69 3GE (United Kingdom); Stearns, Adam T. [Department of Surgery, Brigham and Women' s Hospital, Boston, MA 02115 (United States); Department of Surgery, Harvard Medical School, Boston, MA 02115 (United States); Department of Physiology, Anatomy and Genetics, University of Oxford, Oxford OX1 2JD (United Kingdom); Park, Peter J. [Department of Medicine, Brigham and Women' s Hospital, Boston, MA 02115 (United States); Harvard Medical School, Center for Biomedical Informatics, Boston, MA 02115 (United States); Dreyfuss, Jonathan M. [Department of Medicine, Brigham and Women' s Hospital, Boston, MA 02115 (United States); Ashley, Stanley W. [Department of Surgery, Brigham and Women' s Hospital, Boston, MA 02115 (United States); Department of Surgery, Harvard Medical School, Boston, MA 02115 (United States); Rhoads, David B. [Department of Surgery, Harvard Medical School, Boston, MA 02115 (United States); Pediatric Endocrine Unit, MassGeneral Hospital for Children, Boston, MA 02114 (United States); Tavakkolizadeh, Ali, E-mail: atavakkoli@partners.org [Department of Surgery, Brigham and Women' s Hospital, Boston, MA 02115 (United States); Department of Surgery, Harvard Medical School, Boston, MA 02115 (United States)

    2010-12-10

    Background and aims: The intestine exhibits profound diurnal rhythms in function and morphology, in part due to changes in enterocyte proliferation. The regulatory mechanisms behind these rhythms remain largely unknown. We hypothesized that microRNAs are involved in mediating these rhythms, and studied the role of microRNAs specifically in modulating intestinal proliferation. Methods: Diurnal rhythmicity of microRNAs in rat jejunum was analyzed by microarrays and validated by qPCR. Temporal expression of diurnally rhythmic mir-16 was further quantified in intestinal crypts, villi, and smooth muscle using laser capture microdissection and qPCR. Morphological changes in rat jejunum were assessed by histology and proliferation by immunostaining for bromodeoxyuridine. In IEC-6 cells stably overexpressing mir-16, proliferation was assessed by cell counting and MTS assay, cell cycle progression and apoptosis by flow cytometry, and cell cycle gene expression by qPCR and immunoblotting. Results: mir-16 peaked 6 hours after light onset (HALO 6) with diurnal changes restricted to crypts. Crypt depth and villus height peaked at HALO 13-14 in antiphase to mir-16. Overexpression of mir-16 in IEC-6 cells suppressed specific G1/S regulators (cyclins D1-3, cyclin E1 and cyclin-dependent kinase 6) and produced G1 arrest. Protein expression of these genes exhibited diurnal rhythmicity in rat jejunum, peaking between HALO 11 and 17 in antiphase to mir-16. Conclusions: This is the first report of circadian rhythmicity of specific microRNAs in rat jejunum. Our data provide a link between anti-proliferative mir-16 and the intestinal proliferation rhythm and point to mir-16 as an important regulator of proliferation in jejunal crypts. This function may be essential to match proliferation and absorptive capacity with nutrient availability.

  9. Display

    OpenAIRE

    Gaskell, Ivan

    2011-01-01

    The display of religious objects takes many forms. While sculpture on the exterior of religious buildings is visible for the long term, relics, cult images, and masquerades are shown only occasionally. One way of emphasizing the potency of an object is to reveal it infrequently. In many religious systems display is restricted, for some things are dangerous to inappropriate viewers, while others are too powerful to be seen by anyone. When access is possible, viewers value intimate encounter, u...

  10. Medium Renewal Blocks Anti-Proliferative Effects of Metformin in Cultured MDA-MB-231 Breast Cancer Cells.

    Directory of Open Access Journals (Sweden)

    Maruša Rajh

    Full Text Available Epidemiological studies indicate that metformin, a widely used type 2 diabetes drug, might reduce breast cancer risk and mortality in patients with type 2 diabetes. Metformin might protect against breast cancer indirectly by ameliorating systemic glucose homeostasis. Alternatively, it might target breast cancer cells directly. However, experiments using MDA-MB-231 cells, a standard in vitro breast cancer model, produced inconsistent results regarding effectiveness of metformin as a direct anti-cancer agent. Metformin treatments in cultured MDA-MB-231 cells are usually performed for 48-96 hours, but protocols describing renewal of cell culture medium during these prolonged treatments are rarely reported. We determined whether medium renewal protocol might alter sensitivity of MDA-MB-231 cells treated with metformin. Using the MTS assay, BrdU incorporation and Hoechst staining we found that treatment with metformin for 48-72 hours failed to suppress viability and proliferation of MDA-MB-231 cells if low-glucose (1 g/L medium was renewed every 24 hours. Conversely, metformin suppressed their viability and proliferation if medium was not renewed. Without renewal glucose concentration in the medium was reduced to 0.1 g/L in 72 hours, which likely explains increased sensitivity to metformin under these conditions. We also examined whether 2-deoxy-D-glucose (2-DG reduces resistance to metformin. In the presence of 2-DG metformin reduced viability and proliferation of MDA-MB-231 cells with or without medium renewal, thus demonstrating that 2-DG reduces their resistance to metformin. In sum, we show that medium renewal blocks anti-proliferative effects of metformin during prolonged treatments in low-glucose medium. Differences in medium renewal protocols during prolonged treatments might therefore lead to apparently inconsistent results as regards effectiveness of metformin as a direct anti-cancer agent. Finally, our results indicate that co-therapy with

  11. Medium Renewal Blocks Anti-Proliferative Effects of Metformin in Cultured MDA-MB-231 Breast Cancer Cells.

    Science.gov (United States)

    Rajh, Maruša; Dolinar, Klemen; Miš, Katarina; Pavlin, Mojca; Pirkmajer, Sergej

    2016-01-01

    Epidemiological studies indicate that metformin, a widely used type 2 diabetes drug, might reduce breast cancer risk and mortality in patients with type 2 diabetes. Metformin might protect against breast cancer indirectly by ameliorating systemic glucose homeostasis. Alternatively, it might target breast cancer cells directly. However, experiments using MDA-MB-231 cells, a standard in vitro breast cancer model, produced inconsistent results regarding effectiveness of metformin as a direct anti-cancer agent. Metformin treatments in cultured MDA-MB-231 cells are usually performed for 48-96 hours, but protocols describing renewal of cell culture medium during these prolonged treatments are rarely reported. We determined whether medium renewal protocol might alter sensitivity of MDA-MB-231 cells treated with metformin. Using the MTS assay, BrdU incorporation and Hoechst staining we found that treatment with metformin for 48-72 hours failed to suppress viability and proliferation of MDA-MB-231 cells if low-glucose (1 g/L) medium was renewed every 24 hours. Conversely, metformin suppressed their viability and proliferation if medium was not renewed. Without renewal glucose concentration in the medium was reduced to 0.1 g/L in 72 hours, which likely explains increased sensitivity to metformin under these conditions. We also examined whether 2-deoxy-D-glucose (2-DG) reduces resistance to metformin. In the presence of 2-DG metformin reduced viability and proliferation of MDA-MB-231 cells with or without medium renewal, thus demonstrating that 2-DG reduces their resistance to metformin. In sum, we show that medium renewal blocks anti-proliferative effects of metformin during prolonged treatments in low-glucose medium. Differences in medium renewal protocols during prolonged treatments might therefore lead to apparently inconsistent results as regards effectiveness of metformin as a direct anti-cancer agent. Finally, our results indicate that co-therapy with 2-DG and

  12. In vitro anti-proliferative, anti-bacterial potential and induction of DNA strand break of partially purified Cuscuta reflexa Roxb.

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    Madhulika Bhagat

    2011-01-01

    Full Text Available Cuscuta reflexa is an important medicinal plant, mentioned in Ayurveda, an ancient Indian system of medicine. The plant is selected to evaluate the possibility for novel pharmaceuticals for anticancer and antibiotics drugs. Since most of these drugs had developed resisitance against currently used chemotherapeutics. This study describes the in vitro anti-proliferative, anti-bacterial and single stand DNA break of the holoprasitic plant Cuscuta reflexa. Bioassay-guided fractionation and partial purification of the plant were done and evaluated for antiproliferative activity against human cancer cell lines by SRB assay and single strand DNA break by comet assay. Further antibacterial activity was also performed by agar well diffusion assay. The alcoholic extract, chloroform fraction and partially purified ethylacetate-methanol (1:1 sub-fraction of C. reflexa showed anti-proliferative potential against IMR-32 and 502713 human cancer cell lines. Alcoholic extract exhibited anti-proliferative activity of 74% and 72%, chloroform fraction demonstrated 91% and 95% against neuroblastoma (IMR-32 and colon (502713 cancer cell lines at 100 μg/ml. Single strand DNA break of the chloroform fraction was also demonstrated using comet assay, indicating that possible mode of cell death may be apoptosis. Anti-microbial properties were evaluated against eight species of pathogenic and non-pathogenic microorganisms and maximum zone of inhibition for anti-bacterial activity was found against Staphylococcus aureus (22 mm by alcoholic extract, 21 mm by chloroform fraction and 12 mm by ethylacetate-methanol (1:1 sub-fraction. Minimum inhibitory concentration (MIC of the chloroform fraction was 1500 μg/ml for S. aureus. The plant was found to be equally effective against gram-positive and negative bacteria. Studies are well underway to isolate and identify active compounds from chloroform fraction and ethyl acetate:methanol (1:1 sub-fraction, which can be used as

  13. Lactobacillus casei Exerts Anti-Proliferative Effects Accompanied by Apoptotic Cell Death and Up-Regulation of TRAIL in Colon Carcinoma Cells.

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    Angeliki Tiptiri-Kourpeti

    Full Text Available Probiotic microorganisms such as lactic acid bacteria (LAB exert a number of strain-specific health-promoting activities attributed to their immunomodulatory, anti-inflammatory and anti-carcinogenic properties. Despite recent attention, our understanding of the biological processes involved in the beneficial effects of LAB strains is still limited. To this end, the present study investigated the growth-inhibitory effects of Lactobacillus casei ATCC 393 against experimental colon cancer. Administration of live Lactobacillus casei (as well as bacterial components thereof on murine (CT26 and human (HT29 colon carcinoma cell lines raised a significant concentration- and time-dependent anti-proliferative effect, determined by cell viability assays. Specifically, a dramatic decrease in viability of colon cancer cells co-incubated with 10(9 CFU/mL L. casei for 24 hours was detected (78% for HT29 and 52% for CT26 cells. In addition, live L. casei induced apoptotic cell death in both cell lines as revealed by annexin V and propidium iodide staining. The significance of the in vitro anti-proliferative effects was further confirmed in an experimental tumor model. Oral daily administration of 10(9 CFU live L. casei for 13 days significantly inhibited in vivo growth of colon carcinoma cells, resulting in approximately 80% reduction in tumor volume of treated mice. Tumor growth inhibition was accompanied by L. casei-driven up-regulation of the TNF-related apoptosis-inducing ligand TRAIL and down-regulation of Survivin. Taken together, these findings provide evidence for beneficial tumor-inhibitory, anti-proliferative and pro-apoptotic effects driven by this probiotic LAB strain.

  14. Lactobacillus casei Exerts Anti-Proliferative Effects Accompanied by Apoptotic Cell Death and Up-Regulation of TRAIL in Colon Carcinoma Cells.

    Science.gov (United States)

    Tiptiri-Kourpeti, Angeliki; Spyridopoulou, Katerina; Santarmaki, Valentina; Aindelis, Georgios; Tompoulidou, Evgenia; Lamprianidou, Eleftheria E; Saxami, Georgia; Ypsilantis, Petros; Lampri, Evangeli S; Simopoulos, Constantinos; Kotsianidis, Ioannis; Galanis, Alex; Kourkoutas, Yiannis; Dimitrellou, Dimitra; Chlichlia, Katerina

    2016-01-01

    Probiotic microorganisms such as lactic acid bacteria (LAB) exert a number of strain-specific health-promoting activities attributed to their immunomodulatory, anti-inflammatory and anti-carcinogenic properties. Despite recent attention, our understanding of the biological processes involved in the beneficial effects of LAB strains is still limited. To this end, the present study investigated the growth-inhibitory effects of Lactobacillus casei ATCC 393 against experimental colon cancer. Administration of live Lactobacillus casei (as well as bacterial components thereof) on murine (CT26) and human (HT29) colon carcinoma cell lines raised a significant concentration- and time-dependent anti-proliferative effect, determined by cell viability assays. Specifically, a dramatic decrease in viability of colon cancer cells co-incubated with 10(9) CFU/mL L. casei for 24 hours was detected (78% for HT29 and 52% for CT26 cells). In addition, live L. casei induced apoptotic cell death in both cell lines as revealed by annexin V and propidium iodide staining. The significance of the in vitro anti-proliferative effects was further confirmed in an experimental tumor model. Oral daily administration of 10(9) CFU live L. casei for 13 days significantly inhibited in vivo growth of colon carcinoma cells, resulting in approximately 80% reduction in tumor volume of treated mice. Tumor growth inhibition was accompanied by L. casei-driven up-regulation of the TNF-related apoptosis-inducing ligand TRAIL and down-regulation of Survivin. Taken together, these findings provide evidence for beneficial tumor-inhibitory, anti-proliferative and pro-apoptotic effects driven by this probiotic LAB strain. PMID:26849051

  15. Searching in mother nature for anti-cancer activity: anti-proliferative and pro-apoptotic effect elicited by green barley on leukemia/lymphoma cells.

    Directory of Open Access Journals (Sweden)

    Elisa Robles-Escajeda

    Full Text Available Green barley extract (GB was investigated for possible anti-cancer activity by examining its anti-proliferative and pro-apoptotic properties on human leukemia/lymphoma cell lines. Our results indicate that GB exhibits selective anti-proliferative activity on a panel of leukemia/lymphoma cells in comparison to non-cancerous cells. Specifically, GB disrupted the cell-cycle progression within BJAB cells, as manifested by G2/M phase arrest and DNA fragmentation, and induced apoptosis, as evidenced by phosphatidylserine (PS translocation to the outer cytoplasmic membrane in two B-lineage leukemia/lymphoma cell lines. The pro-apoptotic effect of GB was found to be independent of mitochondrial depolarization, thus implicating extrinsic cell death pathways to exert its cytotoxicity. Indeed, GB elicited an increase of TNF-α production, caspase-8 and caspase-3 activation, and PARP-1 cleavage within pre-B acute lymphoblastic leukemia Nalm-6 cells. Moreover, caspase-8 and caspase-3 activation and PARP-1 cleavage were strongly inhibited/blocked by the addition of the specific caspase inhibitors Z-VAD-FMK and Ac-DEVD-CHO. Furthermore, intracellular signaling analyses determined that GB treatment enhanced constitutive activation of Lck and Src tyrosine kinases in Nalm-6 cells. Taken together, these findings indicate that GB induced preferential anti-proliferative and pro-apoptotic signals within B-lineage leukemia/lymphoma cells, as determined by the following biochemical hallmarks of apoptosis: PS externalization, enhanced release of TNF-α, caspase-8 and caspase-3 activation, PARP-1 cleavage and DNA fragmentation Our observations reveal that GB has potential as an anti-leukemia/lymphoma agent alone or in combination with standard cancer therapies and thus warrants further evaluation in vivo to support these findings.

  16. Aplysinopsin Analogs: Synthesis and Anti-proliferative Activity of Substituted (Z)-5-(N-benzylindol-3-ylmethylene)imidazolidine-2,4-diones

    OpenAIRE

    Reddy, Y. Thirupathi; Reddy, P. Narsimha; Koduru, Srinivas; Damodaran, Chendil; Crooks, Peter A.

    2010-01-01

    A series of substituted (Z)-5-(N-benzylindol-3-ylmethylene)imidazolidine-2,4-dione (3) analogs structurally related to aplysinopsin, and that incorporate a variety of substituents in both the indole and N-benzyl moieties have been synthesized under microwave irradiation and conventional heating methods These analogs were evaluated for their anti-proliferative activity against MCF-7 and MDA-231 breast cancer cell lines, and A549 and H460 lung cancer cell lines. Two analogs, 3f and 3j had IC50 ...

  17. Korean Ginseng Berry Fermented by Mycotoxin Non-producing Aspergillus niger and Aspergillus oryzae: Ginsenoside Analyses and Anti-proliferative Activities.

    Science.gov (United States)

    Li, Zhipeng; Ahn, Hyung Jin; Kim, Nam Yeon; Lee, Yu Na; Ji, Geun Eog

    2016-01-01

    To transform ginsenosides, Korean ginseng berry (KGB) was fermented by mycotoxin non-producing Aspergillus niger and Aspergillus oryzae. Changes of ginsenoside profile and anti-proliferative activities were observed. Results showed that A. niger tended to efficiently transform protopanaxadiol (PPD) type ginsenosides such as Rb1, Rb2, Rd to compound K while A. oryzae tended to efficiently transform protopanaxatriol (PPT) type ginsenoside Re to Rh1 via Rg1. Butanol extracts of fermented KGB showed high cytotoxicity on human adenocarcinoma HT-29 cell line and hepatocellular carcinoma HepG2 cell line while that of unfermented KGB showed little. The minimum effective concentration of niger-fermented KGB was less than 2.5 µg/mL while that of oryzae-fermented KGB was about 5 µg/mL. As A. niger is more inclined to transform PPD type ginsenosides, niger-fermented KGB showed stronger anti-proliferative activity than oryzae-fermented KGB. PMID:27582326

  18. The Budding Yeast “Saccharomyces cerevisiae” as a Drug Discovery Tool to Identify Plant-Derived Natural Products with Anti-Proliferative Properties

    Directory of Open Access Journals (Sweden)

    Bouchra Qaddouri

    2011-01-01

    Full Text Available The budding yeast Saccharomyces cerevisiae is a valuable system to study cell-cycle regulation, which is defective in cancer cells. Due to the highly conserved nature of the cell-cycle machinery between yeast and humans, yeast studies are directly relevant to anticancer-drug discovery. The budding yeast is also an excellent model system for identifying and studying antifungal compounds because of the functional conservation of fungal genes. Moreover, yeast studies have also contributed greatly to our understanding of the biological targets and modes of action of bioactive compounds. Understanding the mechanism of action of clinically relevant compounds is essential for the design of improved second-generation molecules. Here we describe our methodology for screening a library of plant-derived natural products in yeast in order to identify and characterize new compounds with anti-proliferative properties.

  19. Anti Proliferative and Pro Apoptotic Effects of Flavonoid Quercetin Are Mediated by CB1 Receptor in Human Colon Cancer Cell Lines.

    Science.gov (United States)

    Refolo, Maria Grazia; D'Alessandro, Rosalba; Malerba, Natascia; Laezza, Chiara; Bifulco, Maurizio; Messa, Caterina; Caruso, Maria Gabriella; Notarnicola, Maria; Tutino, Valeria

    2015-12-01

    Quercetin, the major constituent of flavonoid and widely present in fruits and vegetables, is an attractive compound for cancer prevention due to its beneficial anti proliferative effects, showing a crucial role in the regulation of apoptosis and cell cycle signaling. In vitro studies have demonstrated that quercetin specifically influences colon cancer cell proliferation. Our experiments, using human colon adenocarcinoma cells, confirmed the anti proliferative effect of quercetin and gave intriguing new insight in to the knowledge of the mechanisms involved. We observed a significant increase in the expression of the endocannabinoids receptor (CB1-R) after quercetin treatment. CB1-R can be considered an estrogen responsive receptor and quercetin, having a structure similar to that of the estrogens, can interact with CB1-R leading to the regulation of cell growth. In order to clarify the contribution of the CB1-R to the quercetin action, we investigated some of the principal molecular pathways that are inhibited or activated by this natural compound. In particular we detected the inhibition of the major survival signals like the PI3K/Akt/mTOR and an induction of the pro apoptotic JNK/JUN pathways. Interestingly, the metabolism of β-catenin was modified by flavonoid both directly and through activated CB1-R. In all the experiments done, the quercetin action has proven to be reinforced by anandamide (Met-F-AEA), a CB1-R agonist, and partially counteracted by SR141716, a CB1-R antagonist. These findings open new perspectives for anticancer therapeutic strategies.

  20. Anti-Proliferative and Pro-Apoptotic Activities of 4-Methyl-2,6-bis(1-phenylethyl)phenol in Cancer Cells.

    Science.gov (United States)

    Sung, Nak Yoon; Kim, Seung Cheol; Kim, Yun Hwan; Kim, Gihyeon; Lee, Yunmi; Sung, Gi-Ho; Kim, Ji Hye; Yang, Woo Seok; Kim, Mi Seon; Baek, Kwang-Soo; Kim, Jong-Hoon; Cho, Jae Youl

    2016-07-01

    It has been found that 4-isopropyl-2,6-bis(1-phenylethyl)phenol (KTH-13), a novel compound isolated from Cordyceps bassiana, is able to suppress tumor cell proliferation by inducing apoptosis. To mass-produce this compound, we established a total synthesis method. Using those conditions, we further synthesized various analogs with structural similarity to KTH-13. In this study, we aimed to test their anti-cancer activity by measuring anti-proliferative and pro-apoptotic activities. Of 8 compounds tested, 4-methyl-2,6-bis(1-phenylethyl)phenol (KTH-13-Me) exhibited the strongest anti-proliferative activity toward MDA-MB 231 cells. KTH-13-Me also similarly suppressed the survival of various cancer cell lines, including C6 glioma, HCT-15, and LoVo cells. Treatment of KTH-13-Me induced several apoptotic signs in C6 glioma cells, such as morphological changes, induction of apoptotic bodies, and nuclear fragmentation and chromatin condensation. Concordantly, early-apoptotic cells were also identified by staining with FITC-Annexin V/PI. Moreover, KTH-13-Me highly enhanced the activation of caspase-3 and caspase-9, and decreased the protein level of Bcl-2. In addition, the phosphorylation levels of Src and STAT3 were diminished in KTH-13-Me-treated C6 cells. Therefore, these results suggest that KTH-13-Me can be developed as a novel anti-cancer drug capable of blocking proliferation, inducing apoptosis, and blocking cell survival signaling in cancer cells. PMID:27068261

  1. Anti-Proliferative and Pro-Apoptotic Activities of 4-Methyl-2,6-bis(1-phenylethyl)phenol in Cancer Cells

    Science.gov (United States)

    Sung, Nak Yoon; Kim, Seung Cheol; Kim, Yun Hwan; Kim, Gihyeon; Lee, Yunmi; Sung, Gi-Ho; Kim, Ji Hye; Yang, Woo Seok; Kim, Mi Seon; Baek, Kwang-Soo; Kim, Jong-Hoon; Cho, Jae Youl

    2016-01-01

    It has been found that 4-isopropyl-2,6-bis(1-phenylethyl)phenol (KTH-13), a novel compound isolated from Cordyceps bassiana, is able to suppress tumor cell proliferation by inducing apoptosis. To mass-produce this compound, we established a total synthesis method. Using those conditions, we further synthesized various analogs with structural similarity to KTH-13. In this study, we aimed to test their anti-cancer activity by measuring anti-proliferative and pro-apoptotic activities. Of 8 compounds tested, 4-methyl-2,6-bis(1-phenylethyl)phenol (KTH-13-Me) exhibited the strongest anti-proliferative activity toward MDA-MB 231 cells. KTH-13-Me also similarly suppressed the survival of various cancer cell lines, including C6 glioma, HCT-15, and LoVo cells. Treatment of KTH-13-Me induced several apoptotic signs in C6 glioma cells, such as morphological changes, induction of apoptotic bodies, and nuclear fragmentation and chromatin condensation. Concordantly, early-apoptotic cells were also identified by staining with FITC-Annexin V/PI. Moreover, KTH-13-Me highly enhanced the activation of caspase-3 and caspase-9, and decreased the protein level of Bcl-2. In addition, the phosphorylation levels of Src and STAT3 were diminished in KTH-13-Me-treated C6 cells. Therefore, these results suggest that KTH-13-Me can be developed as a novel anti-cancer drug capable of blocking proliferation, inducing apoptosis, and blocking cell survival signaling in cancer cells. PMID:27068261

  2. Role of VDR in anti-proliferative effects of calcitriol in tumor-derived endothelial cells and tumor angiogenesis in vivo

    Science.gov (United States)

    Chung, Ivy; Han, Guangzhou; Seshadri, Mukund; Gillard, Bryan M.; Yu, Wei-dong; Foster, Barbara A.; Trump, Donald L.; Johnson, Candace S.

    2008-01-01

    Calcitriol (1, 25-dihydroxycholecalciferol), the major active form of vitamin D, is anti-proliferative in tumor cells and tumor-derived endothelial cells (TDEC). These actions of calcitriol are mediated at least in part by vitamin D receptor (VDR), which is expressed in many tissues including endothelial cells. To investigate the role of VDR in calcitriol effects on tumor vasculature, we established TRAMP-2 tumors subcutaneously into either VDR wild type (WT) or knockout (KO) mice. Within 30 days post inoculation, tumors in KO mice were larger than those in WT (P<0.001). TDEC from WT expressed VDR and were able to transactivate a reporter gene whereas TDEC from KO mice were not. Treatment with calcitriol resulted in growth inhibition in TDEC expressing VDR. However, TDEC from KO mice were relatively resistant, suggesting that calcitriol-mediated growth inhibition on TDEC is VDR-dependent. Further analysis of the TRAMP-C2 tumor sections revealed that the vessels in KO mice were enlarged and had less pericyte coverage compared to WT (P<0.001). Contrast-enhanced MRI demonstrated an increase in vascular volume of TRAMP tumors grown in VDR KO mice compared to WT mice (P<0.001) and FITC-dextran permeability assay suggested a higher extent of vascular leakage in tumors from KO mice. Using ELISA and Western blot analysis, there was an increase of HIF-1 alpha, VEGF, Ang1 and PDGF-BB levels observed in tumors from KO mice. These results indicate that calcitriol-mediated anti-proliferative effects on TDEC are VDR dependent and loss of VDR can lead to abnormal tumor angiogenesis. PMID:19141646

  3. Dual Anti-Metastatic and Anti-Proliferative Activity Assessment of Two Probiotics on HeLa and HT-29 Cell Lines

    Directory of Open Access Journals (Sweden)

    Nouri Zahra

    2016-07-01

    Full Text Available Objective Lactobacilli are a group of probiotics with beneficial effects on prevention of cancer. However, there is scant data in relation with the impacts of probiotics in late-stage cancer progration, especially metastasis. The present original work was aimed to evaluate the anti-metastatic and anti-proliferative activity of lactobacillus rhamnosus supernatant (LRS and lactobacillus crispatus supernatant (LCS on the human cervical and colon adenocarcinoma cell lines (HeLa and HT-29, respectively. Materials and Methods In this experimental study, the anti-proliferative activities of LRS and LCS were determined through MTT assay. MRC-5 was used as a normal cell line. Expression analysis of CASP3, MMP2, MMP9, TIMP1 and TIMP2 genes was performed by quantitative reverse transcriptase-polymerase chain reaction (qRT-PCR, following the cell synchronization. Results Supernatants of these two lactobacilli had cytotoxic effect on HeLa, however LRS treatment was only effective on HT-29 cell line. In addition, LRS had no side-effect on normal cells. It was shown that CASP3 gene expression has been reduced after treatment with supernatants of two studied lactobacilli. According to our study, LRS and LCS are efficacious in the prevention of metastasis potency in HeLa cells with decreased expression of MMP2, MMP9 and increased expression of their inhibitors. In the case of HT-29 cells, only LRS showed this effect. Conclusion Herein, we have demonstrated two probiotics which have anti-metastatic effects on malignant cells and they can be administrated to postpone late-stage of cancer disease. LRS and LCS are effective on HeLa cell lines while only the effect of LRS is significant on HT-29, through cytotoxic and anti-metastatic mechanisms. Further assessments are required to evaluate our results on the other cancer cell lines, in advance to use these probiotics in other extensive trial studies.

  4. Differentiation-inducing and anti-proliferative activities of isoliquiritigenin and all-trans-retinoic acid on B16F0 melanoma cells: Mechanisms profiling by RNA-seq.

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    Chen, Xiaoyu; Yang, Ming; Hao, Wenjin; Han, Jichun; Ma, Jun; Wang, Caixia; Sun, Shiguo; Zheng, Qiusheng

    2016-10-30

    Melanoma is a cancer that arises from melanocytes, specialized pigmented cells that are found predominantly in the skin. The incidence of malignant melanoma has significantly increased over the last decade. With the development of therapy, the survival rate of some kind of cancer has been improved greatly. But the treatment of melanoma remains unsatisfactory. Much of melanoma's resistance to traditional chemotherapy is believed to arise intrinsically, by virtue of potent growth and cell survival-promoting genetic alteration. Therefore, significant attention has recently been focused on differentiation therapy, as well as differentiation inducer compounds. In previous study, we found isoliquiritigenin (ISL), a natural product extracted from licorice, could induce B16F0 melanoma cell differentiation. Here we investigated the transcriptional response of melanoma differentiation process induced by ISL and all-trans-retinoic acid (RA). Results showed that 390 genes involves in 201 biochemical pathways were differentially expressed in ISL treatment and 304 genes in 193 pathways in RA treatment. Differential expressed genes (DGEs, fold-change (FC)≥10) with the function of anti-proliferative and differentiation inducing indicated a loss of grade malignancy characteristic. Kyoto Encyclopedia of Genes and Genomes (KEGG) pathway analysis indicated glutathione metabolism, glycolysis/gluconeogenesis and pentose phosphate pathway were the top three relative pathway perturbed by ISL, and mitogen-activated protein kinase (MAPK) signaling pathway was the most important pathway in RA treatment. In the analysis of hierarchical clustering of DEGs, we discovered 72 DEGs involved in the process of drug action. We thought Cited1, Tgm2, Xaf1, Cd59a, Fbxo2, Adh7 may have critical role in the differentiation of melanoma. The evidence displayed herein confirms the critical role of reactive oxygen species (ROS) in melanoma pathobiology and provides evidence for future targets in the

  5. Capsaicin- resistant arterial baroreceptors

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    Andresen Michael C

    2006-05-01

    Full Text Available Abstract Background Aortic baroreceptors (BRs comprise a class of cranial afferents arising from major arteries closest to the heart whose axons form the aortic depressor nerve. BRs are mechanoreceptors that are largely devoted to cardiovascular autonomic reflexes. Such cranial afferents have either lightly myelinated (A-type or non-myelinated (C-type axons and share remarkable cellular similarities to spinal primary afferent neurons. Our goal was to test whether vanilloid receptor (TRPV1 agonists, capsaicin (CAP and resiniferatoxin (RTX, altered the pressure-discharge properties of peripheral aortic BRs. Results Periaxonal application of 1 μM CAP decreased the amplitude of the C-wave in the compound action potential conducting at 0.50 but completely inhibited discharge of an irregularly discharging BR (C-type. CAP at high concentrations (10–100 μM depressed BR sensitivity in regularly discharging BRs, an effect attributed to non-specific actions. RTX (≤ 10 μM did not affect the discharge properties of regularly discharging BRs (n = 7, p > 0.18. A CAP-sensitive BR had significantly lower discharge regularity expressed as the coefficient of variation than the CAP-resistant fibers (p Conclusion We conclude that functional TRPV1 channels are present in C-type but not A-type (A-δ myelinated aortic arch BRs. CAP has nonspecific inhibitory actions that are unlikely to be related to TRV1 binding since such effects were absent with the highly specific TRPV1 agonist RTX. Thus, CAP must be used with caution at very high concentrations.

  6. Quantitative analysis of the anti-proliferative activity of combinations of selected iron-chelating agents and clinically used anti-neoplastic drugs.

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    Eliska Potuckova

    Full Text Available Recent studies have demonstrated that several chelators possess marked potential as potent anti-neoplastic drugs and as agents that can ameliorate some of the adverse effects associated with standard chemotherapy. Anti-cancer treatment employs combinations of several drugs that have different mechanisms of action. However, data regarding the potential interactions between iron chelators and established chemotherapeutics are lacking. Using estrogen receptor-positive MCF-7 breast cancer cells, we explored the combined anti-proliferative potential of four iron chelators, namely: desferrioxamine (DFO, salicylaldehyde isonicotinoyl hydrazone (SIH, (E-N'-[1-(2-hydroxy-5-nitrophenylethyliden] isonicotinoyl hydrazone (NHAPI, and di-2-pyridylketone 4,4-dimethyl-3-thiosemicarbazone (Dp44mT, plus six selected anti-neoplastic drugs. These six agents are used for breast cancer treatment and include: paclitaxel, 5-fluorouracil, doxorubicin, methotrexate, tamoxifen and 4-hydroperoxycyclophosphamide (an active metabolite of cyclophosphamide. Our quantitative chelator-drug analyses were designed according to the Chou-Talalay method for drug combination assessment. All combinations of these agents yielded concentration-dependent, anti-proliferative effects. The hydrophilic siderophore, DFO, imposed antagonism when used in combination with all six anti-tumor agents and this antagonistic effect increased with increasing dose. Conversely, synergistic interactions were observed with combinations of the lipophilic chelators, NHAPI or Dp44mT, with doxorubicin and also the combinations of SIH, NHAPI or Dp44mT with tamoxifen. The combination of Dp44mT with anti-neoplastic agents was further enhanced following formation of its redox-active iron and especially copper complexes. The most potent combinations of Dp44mT and NHAPI with tamoxifen were confirmed as synergistic using another estrogen receptor-expressing breast cancer cell line, T47D, but not estrogen receptor

  7. Quantitative analysis of the anti-proliferative activity of combinations of selected iron-chelating agents and clinically used anti-neoplastic drugs.

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    Potuckova, Eliska; Jansova, Hana; Machacek, Miloslav; Vavrova, Anna; Haskova, Pavlina; Tichotova, Lucie; Richardson, Vera; Kalinowski, Danuta S; Richardson, Des R; Simunek, Tomas

    2014-01-01

    Recent studies have demonstrated that several chelators possess marked potential as potent anti-neoplastic drugs and as agents that can ameliorate some of the adverse effects associated with standard chemotherapy. Anti-cancer treatment employs combinations of several drugs that have different mechanisms of action. However, data regarding the potential interactions between iron chelators and established chemotherapeutics are lacking. Using estrogen receptor-positive MCF-7 breast cancer cells, we explored the combined anti-proliferative potential of four iron chelators, namely: desferrioxamine (DFO), salicylaldehyde isonicotinoyl hydrazone (SIH), (E)-N'-[1-(2-hydroxy-5-nitrophenyl)ethyliden] isonicotinoyl hydrazone (NHAPI), and di-2-pyridylketone 4,4-dimethyl-3-thiosemicarbazone (Dp44mT), plus six selected anti-neoplastic drugs. These six agents are used for breast cancer treatment and include: paclitaxel, 5-fluorouracil, doxorubicin, methotrexate, tamoxifen and 4-hydroperoxycyclophosphamide (an active metabolite of cyclophosphamide). Our quantitative chelator-drug analyses were designed according to the Chou-Talalay method for drug combination assessment. All combinations of these agents yielded concentration-dependent, anti-proliferative effects. The hydrophilic siderophore, DFO, imposed antagonism when used in combination with all six anti-tumor agents and this antagonistic effect increased with increasing dose. Conversely, synergistic interactions were observed with combinations of the lipophilic chelators, NHAPI or Dp44mT, with doxorubicin and also the combinations of SIH, NHAPI or Dp44mT with tamoxifen. The combination of Dp44mT with anti-neoplastic agents was further enhanced following formation of its redox-active iron and especially copper complexes. The most potent combinations of Dp44mT and NHAPI with tamoxifen were confirmed as synergistic using another estrogen receptor-expressing breast cancer cell line, T47D, but not estrogen receptor-negative MDA

  8. Green synthesis of bacterial mediated anti-proliferative gold nanoparticles: inducing mitotic arrest (G2/M phase) and apoptosis (intrinsic pathway)

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    Ganesh Kumar, C.; Poornachandra, Y.; Chandrasekhar, Cheemalamarri

    2015-11-01

    The physiochemical and biological properties of microbial derived gold nanoparticles have potential applications in various biomedical domains as well as in cancer therapy. We have fabricated anti-proliferative bacterial mediated gold nanoparticles (b-Au NPs) using a culture supernatant of Streptomyces clavuligerus and later characterized them by UV-visible, TEM, DLS, XRD and FT-IR spectroscopic techniques. The capping agent responsible for the nanoparticle formation was characterized based on SDS-PAGE and MALDI-TOF-MS analyses. They were tested for anticancer activity in A549, HeLa and DU145 cell lines. The biocompatibility and non-toxic nature of the nanoparticles were tested on normal human lung cell line (MRC-5). The b-Au NPs induced the cell cycle arrest in G2/M phase and also inhibited the microtubule assembly in DU145 cells. Mechanistic studies, such as ROS, MMP, Cyt-c, GSH, caspases 9, 8 and 3 activation and the Annexin V-FITC staining, along with the above parameters tested provided sufficient evidence that the b-Au NPs induced apoptosis through the intrinsic pathway. The results supported the use of b-Au NPs for future therapeutic application in cancer therapy and other biomedical applications.The physiochemical and biological properties of microbial derived gold nanoparticles have potential applications in various biomedical domains as well as in cancer therapy. We have fabricated anti-proliferative bacterial mediated gold nanoparticles (b-Au NPs) using a culture supernatant of Streptomyces clavuligerus and later characterized them by UV-visible, TEM, DLS, XRD and FT-IR spectroscopic techniques. The capping agent responsible for the nanoparticle formation was characterized based on SDS-PAGE and MALDI-TOF-MS analyses. They were tested for anticancer activity in A549, HeLa and DU145 cell lines. The biocompatibility and non-toxic nature of the nanoparticles were tested on normal human lung cell line (MRC-5). The b-Au NPs induced the cell cycle arrest in G2

  9. Lasiodiplodan, an exocellular (1→6)-β-D: -glucan from Lasiodiplodia theobromae MMPI: production on glucose, fermentation kinetics, rheology and anti-proliferative activity.

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    Alves da Cunha, Mário A; Turmina, Janaína A; Ivanov, Raphael C; Barroso, Roney R; Marques, Patrícia T; Fonseca, Eveline A I; Fortes, Zuleica B; Dekker, Robert F H; Khaper, Neelam; Barbosa, Aneli M

    2012-08-01

    Lasiodiplodan, an exopolysaccharide of the (1→6)-β-D: -glucan type, is produced by Lasiodiplodia theobromae MMPI when grown under submerged culture on glucose. The objective of this study was to evaluate lasiodiplodan production by examining the effects of carbon (glucose, fructose, maltose, sucrose) and nitrogen sources (KNO(3), (NH(4))(2)SO(4), urea, yeast extract, peptone), its production in shake flasks compared to a stirred-tank bioreactor, and to study the rheology of lasiodiplodan, and lasiodiplodan's anti-proliferative effect on breast cancer MCF-7 cells. Although glucose (2.05 ± 0.05 g L(-1)), maltose (2.08 ± 0.04 g L(-1)) and yeast extract (2.46 ± 0.06 g L(-1)) produced the highest amounts of lasiodiplodan, urea as N source resulted in more lasiodiplodan per unit biomass than yeast extract (0.74 ± 0.006 vs. 0.22 ± 0.008 g g(-1)). A comparison of the fermentative parameters of L. theobromae MMPI in shake flasks and a stirred-tank bioreactor at 120 h on glucose as carbon source showed maximum lasiodiplodan production in agitated flasks (7.01 ± 0.07 g L(-1)) with a specific yield of 0.25 ± 0.57 g g(-1) and a volumetric productivity of 0.06 ± 0.001 g L(-1) h(-1). A factorial 2(2) statistical design developed to evaluate the effect of glucose concentration (20-60 g L(-1)) and impeller speed (100-200 rpm) on lasiodiplodan production in the bioreactor showed the highest production (6.32 g L(-1)) at 72 h. Lasiodiplodan presented pseudoplastic behaviour, and the apparent viscosity increased at 60°C in the presence of CaCl(2). Anti-proliferative activity of lasiodiplodan was demonstrated in MCF-7 cells, which was time- and dose-dependent with an IC(50) of 100 μg lasiodiplodan mL(-1). PMID:22399240

  10. In vitro antioxidant and anti-proliferative activities of seed extracts of Nymphaea mexicana in different solvents and GC-MS analysis

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    Umar Shah

    2014-12-01

    Full Text Available A first attempt was made for the GC-MS profiling, anti-oxidant analysis cum DNA protective properties and anti-proliferative activities of a wild aquatic plant, Nymphaea mexicana found in Himalayan region and consumed for its peculiar taste and aroma. Three different solvents were used viz; methanol, ethanol and water. Extracts showed a dose dependent relationship with highest antioxidant potential in ethanol, however highest TPC was found in methanol (0.110 ± 0.05 GAE/g as compared to ethanol (0.095 ± 0.05 GAE/g and water (0.073 ± 0.05 GAE/g. Plant extracts showed efficient DNA damage protection (at concentrations > 30 μg/mL and maximum efficiency against DNA damage was seen in ethanolic solvent. The antiproliferative activities of the plant were noteworthy at a concentration of 20 mg/ mL but were significantly lower than standard (5-flourouracil. The plant is known for its specific taste and aroma hence GC-MS profiling were carried out and relative percentage of important compounds found was determined. GC-MS analysis confirmed some major aroma rendering compounds along with some major anti-oxidants.

  11. Foodomics study on the effects of extracellular production of hydrogen peroxide by rosemary polyphenols on the anti-proliferative activity of rosemary polyphenols against HT-29 cells.

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    Valdés, Alberto; García-Cañas, Virginia; Koçak, Engin; Simó, Carolina; Cifuentes, Alejandro

    2016-07-01

    A number of studies have demonstrated a strong association between the antioxidant properties of rosemary polyphenols and their chemoprotective activity. However, the prooxidant effects of rosemary polyphenols have been rarely reported. In this work, a foodomics study is performed to investigate the in vitro autooxidation of carnosic acid (CA), carnosol (CS) and a polyphenol-enriched rosemary extract (SC-RE) in cell culture conditions. The results revealed that rosemary polyphenols autooxidation in culture medium generated H2 O2 at different rates. Generated H2 O2 levels by SC-RE and CA, but not CS, were correlated with intracellular reactive oxygen species (ROS) generation in HT-29 cells, and were partially involved in their anti-proliferative effect in this cell line. These compounds also induced different effects on glutathione metabolism. Results also indicated that high extracellular H2 O2 concentrations, resulting of using high (45 μg/mL) SC-RE concentration in culture media, exerted some artifactual effects related with cell cycle, but they did not influence the expression of relevant molecular biomarkers of stress. PMID:26842614

  12. Anti-proliferative and ADMET screening of novel 3-(1H-indol-3-yl-1, 3-diphenylpropan-1-one derivatives

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    Manjunatha K. Siddappa

    2016-12-01

    Full Text Available Cancer tends to be one of the major diseases in the present century affecting global population, and proliferation of cancerous cells needs to be eliminated as the cell growth is uncontrolled. In this present study, a series of facile, high yielding 3-(1H-indol-3-yl-1, 3-diphenylpropan-1-ones 3(a–j was designed, synthesized and evaluated for anti-proliferative activity against different human cancer cell lines; MCF-7 (breast cancer, K562 (leukemic cancer, HeLa (cervical cancer, Colo205 (colorectal adreno carcinoma, HepG2 (Hepato cellular carcinoma cell lines. The compounds 3a, 3c, 3d, 3e, 3f, 3g and 3j exhibited an average inhibition of 35% against Hepatocellular Carcinoma (Hepg2 cell lines whereas, compounds 3a, 3c, 3d and 3e exhibited 33, 31, 35 and 33% inhibition, respectively, against HeLa cells at 10 μm concentrations. Doxorubicin was employed as a positive control. The ADME-TOX data was obtained by subjecting the molecules in silico to quantitatively predict the physicochemical properties. The structure of the title compounds were established by IR, 1H NMR, 13C NMR and Mass analysis.

  13. A new class of hybrid anticancer agents inspired by the synergistic effects of curcumin and genistein: Design, synthesis, and anti-proliferative evaluation.

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    Chen, Qiao-Hong; Yu, Kevin; Zhang, Xiaojie; Chen, Guanglin; Hoover, Andrew; Leon, Francisco; Wang, Rubing; Subrahmanyam, Nithya; Addo Mekuria, Ermias; Harinantenaina Rakotondraibe, Liva

    2015-10-15

    Inspired by the synergistic effects of dietary natural products with different scaffolds on the inhibition of cancer cell proliferation, incorporation of central (1E,4E)-1,4-penta-dien-3-one linker (an optimal substitute for the central metabolically unstable diketone linker of curcumin), 1-alkyl-1H-imidazol-2-yl (a promising bioisostere of terminal aryl group in curcumin), and chromone (the common pharmacophore in genistein and quercetin) into one chemical entity resulted in ten new hybrid molecules, 3-((1E,4E)-5-(1-alkyl-1H-imidazol-2-yl)-3-oxopenta-1,4-dien-1-yl)-4H-chromen-4-ones. They were synthesized through a three-step transformation using acid-catalyzed aldol condensation as key step. The WST-1 cell proliferation assay showed that they have greater anti-proliferative potency than curcumin, quercetin, and genistein on both androgen-dependent and androgen-independent human prostate cancer cells. PMID:26341135

  14. A novel dual-functioning ruthenium(II)-arene complex of an anti-microbial ciprofloxacin derivative - Anti-proliferative and anti-microbial activity.

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    Ude, Ziga; Romero-Canelón, Isolda; Twamley, Brendan; Fitzgerald Hughes, Deirdre; Sadler, Peter J; Marmion, Celine J

    2016-07-01

    7-(4-(Decanoyl)piperazin-1-yl)-ciprofloxacin, CipA, (1) which is an analogue of the antibiotic ciprofloxacin, and its ruthenium(II) complex [Ru(η(6)-p-cymene)(CipA-H)Cl], (2) have been synthesised and the x-ray crystal structures of 1·1.3H2O·0.6CH3OH and 2·CH3OH·0.5H2O determined. The complex adopts a typical pseudo-octahedral 'piano-stool' geometry, with Ru(II) π-bonded to the p-cymene ring and σ-bonded to a chloride and two oxygen atoms of the chelated fluoroquinolone ligand. The complex is highly cytotoxic in the low μM range and is as potent as the clinical drug cisplatin against the human cancer cell lines A2780, A549, HCT116, and PC3. It is also highly cytotoxic against cisplatin- and oxaliplatin-resistant cell lines suggesting a different mechanism of action. The complex also retained low μM cytotoxicity against the human colon cancer cell line HCT116p53 in which the tumour suppressor p53 had been knocked out, suggesting that the potent anti-proliferative properties associated with this complex are independent of the status of p53 (in contrast to cisplatin). The complex also retained moderate anti-bacterial activity in two Escherichia coli, a laboratory strain and a clinical isolate resistant to first, second and third generation β-lactam antibiotics.

  15. Umbelliprenin is cytotoxic against QU-DB large cell lung cancer cell line but anti-proliferative against A549 adenocarcinoma cells

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    Khaghanzadeh Narges

    2012-10-01

    Full Text Available Abstract Background Umbelliprenin is a natural compound, belonging to the class of sesquiterpene coumarins. Recently, umbelliprenin has attracted the researchers' attention for its antitumor activities against skin tumors. Its effect on lung cancer is largely unknown. The aim of our study was to investigate the effects of this natural compound, which is expected to have low adverse effects, on lung cancer. Methods The QU-DB large cell and A549 adenocarcinoma lung cancer cell lines were treated with umbelliprenin. IC50 values were estimated using methyl thiazolely diphenyl-tetrazolium bromide (MTT assay, in which a decrease in MTT reduction can occur as a result of cell death or cell proliferation inhibition. To quantify the rate of cell death at IC50 values, flow cytometry using Annexin V-FITC (for apoptotic cells, and propidium iodide (for necrotic cells dyes were employed. Results Data from three independent MTT experiments in triplicate revealed that IC50 values for QU-DB and A549 were 47 ± 5.3 μM and 52 ± 1.97 μM, respectively. Annexin V/PI staining demonstrated that umbelliprenin treatment at IC50 induced 50% cell death in QU-DB cells, but produced no significant death in A549 cells until increasing the umbelliprenin concentration to IC80. The pattern of cell death was predominantly apoptosis in both cell lines. When peripheral blood mononuclear cells were treated with 50 μM and less concentrations of umbelliprenin, no suppressive effect was observed. Conclusions We found cytotoxic/anti-proliferative effects of umbelliprenin against two different types of lung cancer cell lines.

  16. Umbelliprenin is Cytotoxic against QU-DB Large Cell Lung Cancer Cell Line but Anti-Proliferative against A549 Adenocarcinoma Cells

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    Abbas Ghaderi

    2012-10-01

    Full Text Available Background:Umbelliprenin is a natural compound, belonging to the class of sesquiterpene coumarins.Recently, umbelliprenin has attracted the researchers' attention for its antitumor activitiesagainst skin tumors. Its effect on lung cancer is largely unknown. The aim of our study was to investigate the effects of this natural compound, which is expected to have low adverse effects, on lung cancer.Methods:The QU-DB large cell and A549 adenocarcinoma lung cancer cell lines were treated with umbelliprenin. IC50 values were estimated using methyl thiazolely diphenyl-tetrazolium bromide (MTT assay, in which a decrease in MTT reduction can occur as a result of cell death or cell proliferation inhibition. To quantify the rate of cell death at IC50 values, flow cytometry using Annexin V-FITC (for apoptotic cells, and propidium iodide (for necrotic cells dyes were employed.Results:Data from three independent MTT experiments in triplicate revealed that IC50 values for QUDB and A549 were 47 ± 5.3 μM and 52 ± 1.97 μM, respectively. Annexin V/PI staining demonstrated that umbelliprenin treatment at IC50 induced 50% cell death in QU-DB cells,but produced no significant death in A549 cells until increasing the umbelliprenin concentration to IC80. The pattern of cell death was predominantly apoptosis in both cell lines. When peripheral blood mononuclear cells were treated with 50 μM and lessconcentrations of umbelliprenin, no suppressive effect was observed.Conclusions:We found cytotoxic/anti-proliferative effects of umbelliprenin against two different types of lung cancer cell lines.

  17. A novel dual-functioning ruthenium(II)-arene complex of an anti-microbial ciprofloxacin derivative - Anti-proliferative and anti-microbial activity.

    Science.gov (United States)

    Ude, Ziga; Romero-Canelón, Isolda; Twamley, Brendan; Fitzgerald Hughes, Deirdre; Sadler, Peter J; Marmion, Celine J

    2016-07-01

    7-(4-(Decanoyl)piperazin-1-yl)-ciprofloxacin, CipA, (1) which is an analogue of the antibiotic ciprofloxacin, and its ruthenium(II) complex [Ru(η(6)-p-cymene)(CipA-H)Cl], (2) have been synthesised and the x-ray crystal structures of 1·1.3H2O·0.6CH3OH and 2·CH3OH·0.5H2O determined. The complex adopts a typical pseudo-octahedral 'piano-stool' geometry, with Ru(II) π-bonded to the p-cymene ring and σ-bonded to a chloride and two oxygen atoms of the chelated fluoroquinolone ligand. The complex is highly cytotoxic in the low μM range and is as potent as the clinical drug cisplatin against the human cancer cell lines A2780, A549, HCT116, and PC3. It is also highly cytotoxic against cisplatin- and oxaliplatin-resistant cell lines suggesting a different mechanism of action. The complex also retained low μM cytotoxicity against the human colon cancer cell line HCT116p53 in which the tumour suppressor p53 had been knocked out, suggesting that the potent anti-proliferative properties associated with this complex are independent of the status of p53 (in contrast to cisplatin). The complex also retained moderate anti-bacterial activity in two Escherichia coli, a laboratory strain and a clinical isolate resistant to first, second and third generation β-lactam antibiotics. PMID:26993079

  18. BPR1K653, a novel Aurora kinase inhibitor, exhibits potent anti-proliferative activity in MDR1 (P-gp170-mediated multidrug-resistant cancer cells.

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    Chun Hei Antonio Cheung

    Full Text Available BACKGROUND: Over-expression of Aurora kinases promotes the tumorigenesis of cells. The aim of this study was to determine the preclinical profile of a novel pan-Aurora kinase inhibitor, BPR1K653, as a candidate for anti-cancer therapy. Since expression of the drug efflux pump, MDR1, reduces the effectiveness of various chemotherapeutic compounds in human cancers, this study also aimed to determine whether the potency of BPR1K653 could be affected by the expression of MDR1 in cancer cells. PRINCIPAL FINDINGS: BPR1K653 specifically inhibited the activity of Aurora-A and Aurora-B kinase at low nano-molar concentrations in vitro. Anti-proliferative activity of BPR1K653 was evaluated in various human cancer cell lines. Results of the clonogenic assay showed that BPR1K653 was potent in targeting a variety of cancer cell lines regardless of the tissue origin, p53 status, or expression of MDR1. At the cellular level, BPR1K653 induced endo-replication and subsequent apoptosis in both MDR1-negative and MDR1-positive cancer cells. Importantly, it showed potent activity against the growth of xenograft tumors of the human cervical carcinoma KB and KB-derived MDR1-positive KB-VIN10 cells in nude mice. Finally, BPR1K653 also exhibited favorable pharmacokinetic properties in rats. CONCLUSIONS AND SIGNIFICANCE: BPR1K653 is a novel potent anti-cancer compound, and its potency is not affected by the expression of the multiple drug resistant protein, MDR1, in cancer cells. Therefore, BPR1K653 is a promising anti-cancer compound that has potential for the management of various malignancies, particularly for patients with MDR1-related drug resistance after prolonged chemotherapeutic treatments.

  19. The anti-proliferative effect of L-carnosine correlates with a decreased expression of hypoxia inducible factor 1 alpha in human colon cancer cells.

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    Iovine, Barbara; Oliviero, Giorgia; Garofalo, Mariangela; Orefice, Maria; Nocella, Francesca; Borbone, Nicola; Piccialli, Vincenzo; Centore, Roberto; Mazzone, Massimiliano; Piccialli, Gennaro; Bevilacqua, Maria Assunta

    2014-01-01

    In recent years considerable attention has been given to the use of natural substances as anticancer drugs. The natural antioxidant dipeptide L-carnosine belongs to this class of molecules because it has been proved to have a significant anticancer activity both in vitro and in vivo. Previous studies have shown that L-carnosine inhibits the proliferation of human colorectal carcinoma cells by affecting the ATP and Reactive Oxygen Species (ROS) production. In the present study we identified the Hypoxia-Inducible Factor 1α (HIF-1α) as a possible target of L-carnosine in HCT-116 cell line. HIF-1α protein is over-expressed in multiple types of human cancer and is the major cause of resistance to drugs and radiation in solid tumours. Of particular interest are experimental data supporting the concept that generation of ROS provides a redox signal for HIF-1α induction, and it is known that some antioxidants are able to suppress tumorigenesis by inhibiting HIF-1α. In the current study we found that L-carnosine reduces the HIF-1α protein level affecting its stability and decreases the HIF-1 transcriptional activity. In addition, we demonstrated that L-carnosine is involved in ubiquitin-proteasome system promoting HIF-1α degradation. Finally, we compared the antioxidant activity of L-carnosine with that of two synthetic anti-oxidant bis-diaminotriazoles (namely 1 and 2, respectively). Despite these three compounds have the same ability in reducing intracellular ROS, 1 and 2 are more potent scavengers and have no effect on HIF-1α expression and cancer cell proliferation. These findings suggest that an analysis of L-carnosine antioxidant pathway will clarify the mechanism underlying the anti-proliferative effects of this dipeptide on colon cancer cells. However, although the molecular mechanism by which L-carnosine down regulates or inhibits the HIF-1α activity has not been yet elucidated, this ability may be promising in treating hypoxia-related diseases. PMID

  20. The anti-proliferative effect of L-carnosine correlates with a decreased expression of hypoxia inducible factor 1 alpha in human colon cancer cells.

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    Barbara Iovine

    Full Text Available In recent years considerable attention has been given to the use of natural substances as anticancer drugs. The natural antioxidant dipeptide L-carnosine belongs to this class of molecules because it has been proved to have a significant anticancer activity both in vitro and in vivo. Previous studies have shown that L-carnosine inhibits the proliferation of human colorectal carcinoma cells by affecting the ATP and Reactive Oxygen Species (ROS production. In the present study we identified the Hypoxia-Inducible Factor 1α (HIF-1α as a possible target of L-carnosine in HCT-116 cell line. HIF-1α protein is over-expressed in multiple types of human cancer and is the major cause of resistance to drugs and radiation in solid tumours. Of particular interest are experimental data supporting the concept that generation of ROS provides a redox signal for HIF-1α induction, and it is known that some antioxidants are able to suppress tumorigenesis by inhibiting HIF-1α. In the current study we found that L-carnosine reduces the HIF-1α protein level affecting its stability and decreases the HIF-1 transcriptional activity. In addition, we demonstrated that L-carnosine is involved in ubiquitin-proteasome system promoting HIF-1α degradation. Finally, we compared the antioxidant activity of L-carnosine with that of two synthetic anti-oxidant bis-diaminotriazoles (namely 1 and 2, respectively. Despite these three compounds have the same ability in reducing intracellular ROS, 1 and 2 are more potent scavengers and have no effect on HIF-1α expression and cancer cell proliferation. These findings suggest that an analysis of L-carnosine antioxidant pathway will clarify the mechanism underlying the anti-proliferative effects of this dipeptide on colon cancer cells. However, although the molecular mechanism by which L-carnosine down regulates or inhibits the HIF-1α activity has not been yet elucidated, this ability may be promising in treating hypoxia

  1. Persistent Respiratory Symptoms following Prolonged Capsaicin Exposure

    Directory of Open Access Journals (Sweden)

    K Nugent

    2013-10-01

    Full Text Available Capsaicin causes direct irritation of the eyes, mucous membranes, and respiratory tract. It is used in self-defense, in crowd control, and as a less lethal weapon in police work. Controlled trials suggest that capsaicin has minimal serious acute effects. Herein, we report a woman who had a 20-minute exposure to capsaicin during a jail riot. She subsequently developed episodic dyspnea and cough, and increased sensitivity to scents, perfumes, and cigarette smoke. She has not had wheezes on physical examination or abnormal pulmonary function tests. Her response to inhaled steroids and long-acting beta-agonists has been incomplete. She appears to have developed airway sensory hyperreactivity syndrome after the inhalation of capsaicin, which likely injured sensory nerves and/or caused persistent neurogenic inflammation.

  2. The role of capsaicin in dermatology.

    Science.gov (United States)

    Boyd, Katherine; Shea, Sofia M; Patterson, James W

    2014-01-01

    Neurogenic pain and pruritus are the common chief complaints at dermatology office visits. Unfortunately, they are also notoriously difficult conditions to treat. Topical capsaicin used as a single therapy or as an adjuvant offers a low-risk option for patients who do not achieve control on other therapies. This chapter presents the evidence behind topical capsaicin use in dermatologic conditions characterized by neurogenic pain or pruritus, including postherpetic neuralgia, notalgia paresthetica, brachioradial pruritus, lichen simplex chronicus, prurigo nodularis, pruritus ani, pruritus of hemodialysis, aquagenic pruritus, apocrine chromhidrosis, lipodermatosclerosis, alopecia areata, and psoriasis. It presents the most common capsaicin formulations, dosages, and durations of treatment for each condition. Additionally, the chapter addresses various adverse effects and limitations in the use of topical capsaicin in dermatology. PMID:24941674

  3. Capsaicin in Idiopathic Rhinitis A Hot Topic

    OpenAIRE

    van Rijswijk, J B

    2005-01-01

    textabstractIn chapter I the currently known causes for nonallergic noninfectious rhinitis and possible treatments are summarised. Also possible pathophysiological mechanisms underlying idiopathic rhinitis (IR) are discussed. In chapter II the aims of the studies are presented. This thesis comprises studies aimed at the therapeutic potential and safety of intranasal capsaicin in IR patients, developing a patient and physician friendly, effective intranasal capsaicin treatment regimen for IR a...

  4. Capsaicin induced cough in cryptogenic fibrosing alveolitis

    OpenAIRE

    Doherty, M.; Mister, R; Pearson, M.; Calverley, P.

    2000-01-01

    BACKGROUND—Cough is a common and troublesome symptom in cryptogenic fibrosing alveolitis (CFA) but the mechanisms responsible are not known. The cough threshold to inhaled capsaicin is increased in asthma and chronic obstructive pulmonary disease (COPD) where lung volumes are increased, but the relationship between cough response and symptom intensity has not been studied in CFA where lung volumes are reduced.
METHODS—Capsaicin challenge tests were performed on 15 subject...

  5. Dietary Capsaicin Protects Cardiometabolic Organs from Dysfunction.

    Science.gov (United States)

    Sun, Fang; Xiong, Shiqiang; Zhu, Zhiming

    2016-01-01

    Chili peppers have a long history of use for flavoring, coloring, and preserving food, as well as for medical purposes. The increased use of chili peppers in food is very popular worldwide. Capsaicin is the major pungent bioactivator in chili peppers. The beneficial effects of capsaicin on cardiovascular function and metabolic regulation have been validated in experimental and population studies. The receptor for capsaicin is called the transient receptor potential vanilloid subtype 1 (TRPV1). TRPV1 is ubiquitously distributed in the brain, sensory nerves, dorsal root ganglia, bladder, gut, and blood vessels. Activation of TRPV1 leads to increased intracellular calcium signaling and, subsequently, various physiological effects. TRPV1 is well known for its prominent roles in inflammation, oxidation stress, and pain sensation. Recently, TRPV1 was found to play critical roles in cardiovascular function and metabolic homeostasis. Experimental studies demonstrated that activation of TRPV1 by capsaicin could ameliorate obesity, diabetes, and hypertension. Additionally, TRPV1 activation preserved the function of cardiometabolic organs. Furthermore, population studies also confirmed the beneficial effects of capsaicin on human health. The habitual consumption of spicy foods was inversely associated with both total and certain causes of specific mortality after adjustment for other known or potential risk factors. The enjoyment of spicy flavors in food was associated with a lower prevalence of obesity, type 2 diabetes, and cardiovascular diseases. These results suggest that capsaicin and TRPV1 may be potential targets for the management of cardiometabolic vascular diseases and their related target organs dysfunction. PMID:27120617

  6. Dietary Capsaicin Protects Cardiometabolic Organs from Dysfunction

    Directory of Open Access Journals (Sweden)

    Fang Sun

    2016-04-01

    Full Text Available Chili peppers have a long history of use for flavoring, coloring, and preserving food, as well as for medical purposes. The increased use of chili peppers in food is very popular worldwide. Capsaicin is the major pungent bioactivator in chili peppers. The beneficial effects of capsaicin on cardiovascular function and metabolic regulation have been validated in experimental and population studies. The receptor for capsaicin is called the transient receptor potential vanilloid subtype 1 (TRPV1. TRPV1 is ubiquitously distributed in the brain, sensory nerves, dorsal root ganglia, bladder, gut, and blood vessels. Activation of TRPV1 leads to increased intracellular calcium signaling and, subsequently, various physiological effects. TRPV1 is well known for its prominent roles in inflammation, oxidation stress, and pain sensation. Recently, TRPV1 was found to play critical roles in cardiovascular function and metabolic homeostasis. Experimental studies demonstrated that activation of TRPV1 by capsaicin could ameliorate obesity, diabetes, and hypertension. Additionally, TRPV1 activation preserved the function of cardiometabolic organs. Furthermore, population studies also confirmed the beneficial effects of capsaicin on human health. The habitual consumption of spicy foods was inversely associated with both total and certain causes of specific mortality after adjustment for other known or potential risk factors. The enjoyment of spicy flavors in food was associated with a lower prevalence of obesity, type 2 diabetes, and cardiovascular diseases. These results suggest that capsaicin and TRPV1 may be potential targets for the management of cardiometabolic vascular diseases and their related target organs dysfunction.

  7. Impact of ABCB1 1236C > T-2677G > T-3435C > T polymorphisms on the anti-proliferative activity of imatinib, nilotinib, dasatinib and ponatinib

    Science.gov (United States)

    Dessilly, Géraldine; Panin, Nadtha; Elens, Laure; Haufroid, Vincent; Demoulin, Jean-Baptiste

    2016-01-01

    Overexpression of ABCB1 (also called P-glycoprotein) confers resistance to multiple anticancer drugs, including tyrosine kinase inhibitors (TKIs). Several ABCB1 single nucleotide polymorphisms affect the transporter activity. The most common ABCB1 variants are 1236C > T, 2677G > T, 3435C > T and have been associated with clinical response to imatinib in chronic myelogenous leukaemia (CML) in some studies. We evaluated the impact of these polymorphisms on the anti-proliferative effect and the intracellular accumulation of TKIs (imatinib, nilotinib, dasatinib and ponatinib) in transfected HEK293 and K562 cells. ABCB1 overexpression increased the resistance of cells to doxorubicin, vinblastine and TKIs. Imatinib anti-proliferative effect and accumulation were decreased to a larger extent in cells expressing the ABCB1 wild-type protein compared with the 1236T-2677T-3435T variant relatively to control cells. By contrast, ABCB1 polymorphisms influenced the activity of nilotinib, dasatinib and ponatinib to a much lesser extent. In conclusion, our data suggest that wild-type ABCB1 exports imatinib more efficiently than the 1236T-2677T-3435T variant protein, providing a molecular basis for the reported association between ABCB1 polymorphisms and the response to imatinib in CML. Our results also point to a weaker impact of ABCB1 polymorphisms on the activity of nilotinib, dasatinib and ponatinib. PMID:27405085

  8. The addition of GTN to capsaicin cream reduces the discomfort associated with application of capsaicin alone. A volunteer study.

    Science.gov (United States)

    McCleane, G J; McLaughlin, M

    1998-11-01

    In a double blind, placebo controlled trial of 40 volunteers, the burning discomfort associated with application of capsaicin cream (0.025%) was compared to placebo, GTN cream (1.33%) and to the combination of capsaicin cream (0.025%) plus GTN cream 1.33%. Median VAS for burning pain were 0 for the placebo, GTN and GTN + capsaicin groups and 3 for the capsaicin group after single application of each cream at daily intervals. This study demonstrates that after single application the addition of GTN to capsaicin significantly reduces the burning discomfort associated with application of capsaicin alone.

  9. Capsaicin-induced changes in LTP in the lateral amygdala are mediated by TRPV1.

    Directory of Open Access Journals (Sweden)

    Carsten Zschenderlein

    Full Text Available The transient receptor potential vanilloid type 1 (TRPV1 channel is a well recognized polymodal signal detector that is activated by painful stimuli such as capsaicin. Here, we show that TRPV1 is expressed in the lateral nucleus of the amygdala (LA. Despite the fact that the central amygdala displays the highest neuronal density, the highest density of TRPV1 labeled neurons was found within the nuclei of the basolateral complex of the amygdala. Capsaicin specifically changed the magnitude of long-term potentiation (LTP in the LA in brain slices of mice depending on the anesthetic (ether, isoflurane used before euthanasia. After ether anesthesia, capsaicin had a suppressive effect on LA-LTP both in patch clamp and in extracellular recordings. The capsaicin-induced reduction of LTP was completely blocked by the nitric oxide synthase (NOS inhibitor L-NAME and was absent in neuronal NOS as well as in TRPV1 deficient mice. The specific antagonist of cannabinoid receptor type 1 (CB1, AM 251, was also able to reduce the inhibitory effect of capsaicin on LA-LTP, suggesting that stimulation of TRPV1 provokes the generation of anandamide in the brain which seems to inhibit NO synthesis. After isoflurane anesthesia before euthanasia capsaicin caused a TRPV1-mediated increase in the magnitude of LA-LTP. Therefore, our results also indicate that the appropriate choice of the anesthetics used is an important consideration when brain plasticity and the action of endovanilloids will be evaluated. In summary, our results demonstrate that TRPV1 may be involved in the amygdala control of learning mechanisms.

  10. Resiniferatoxin and its analogs provide novel insights into the pharmacology of the vanilloid (capsaicin) receptor

    Energy Technology Data Exchange (ETDEWEB)

    Szallasi, A.; Blumberg, P.M. (National Institutes of Health, Bethesda, MD (USA))

    1990-01-01

    Capsaicin, the pungent constituent of chili peppers, represents the paradigm for the capsaicinoids or vanilloids, a family of compounds shown to stimulate and then desensitize specific subpopulations of sensory receptors, including C-polymodal nociceptors, A-delta mechanoheat nociceptors and warm receptors of the skin, as well as enteroceptors of thin afferent fibers. An exciting recent advance in the field has been the finding that resiniferatoxin (RTX), a naturally occurring diterpene containing a homovanillic acid ester, a key structural motif of capsaicin, functions as an ultrapotent capsaicin analog. For most of the responses characteristic of capsaicin, RTX is 100-10,000 fold more potent. Structure/activity analysis indicates, however, that RTX and related homovanillyl-diterpene esters display distinct spectra of activity. Specific ({sup 3}H)RTX binding provides the first direct proof for the existence of vanilloid receptors. We expect that the RTX class of vanilloids will promote rapid progress in understanding of vanilloid structure/activity requirements and mechanism.

  11. The Effect of Capsaicin on Salivary Gland Dysfunction.

    Science.gov (United States)

    Shin, Yong-Hwan; Kim, Jin Man; Park, Kyungpyo

    2016-01-01

    Capsaicin (trans-8-methyl-N-vanilyl-6-nonenamide) is a unique alkaloid isolated from hot chili peppers of the capsicum family. Capsaicin is an agonist of transient receptor potential vanilloid subtype 1 (TRPV1), which is expressed in nociceptive sensory neurons and a range of secretory epithelia, including salivary glands. Capsaicin has analgesic and anti-inflammatory properties in sensory neurons. Recently, increasing evidence has indicated that capsaicin also affects saliva secretion and inflammation in salivary glands. Applying capsaicin increases salivary secretion in human and animal models. Capsaicin appears to increase salivation mainly by modulating the paracellular pathway in salivary glands. Capsaicin activates TRPV1, which modulates the permeability of tight junctions (TJ) by regulating the expression and function of putative intercellular adhesion molecules in an ERK (extracelluar signal-regulated kinase) -dependent manner. Capsaicin also improved dysfunction in transplanted salivary glands. Aside from the secretory effects of capsaicin, it has anti-inflammatory effects in salivary glands. The anti-inflammatory effect of capsaicin is, however, not mediated by TRPV1, but by inhibition of the NF-κB pathway. In conclusion, capsaicin might be a potential drug for alleviating dry mouth symptoms and inflammation of salivary glands. PMID:27347918

  12. Simultaneous determination of capsaicin and dihydrocapsaicin for vegetable oil adulteration by immunoaffinity chromatography cleanup coupled with LC-MS/MS.

    Science.gov (United States)

    Ma, Fei; Yang, Qingqing; Matthäus, Bertrand; Li, Peiwu; Zhang, Qi; Zhang, Liangxiao

    2016-05-15

    Capsaicin and dihydrocapsaicin were selected as adulteration markers to authenticate vegetable oils. In this study, a method of immunoaffinity chromatography (IAC) combined with liquid chromatography-tandem mass spectrometry was established for the determination of capsaicin and dihydrocapsaicin in vegetable oils. In this method, immunosorbents were obtained by covalently coupling highly specific capsaicinoid polyclonal antibodieswith CNBr-activated Sepharose 4B, and then packed into a polyethylene column. In this paper, the major parameters affecting IAC extraction efficiency, including loading, washing and eluting conditions, were also investigated. The IAC column displayed high selectivity for capsaicin and dihydrocapsaicin with the maximum capacity of 240ng. The limit of detection (LOD) and limit of quantification (LOQ) for capsaicin were calculated as 0.02 and 0.08μgkg(-1), and for dihydrocapsaicin were 0.03 and 0.10μgkg(-1). The recoveries of capsaicin and dihydrocapsaicin in oil samples were in the range of 87.3-95.2% with the relative standard deviation (RSD) of less than 6.1%. The results indicated that capsaicinoid compounds could not be found in edible vegetable oils. Therefore, the proposed method is simple, reliable and adequate for routine monitoring of capsaicinoid compounds in vegetable oils and has an excellent potential for detection of adulteration with inedible waste oil. PMID:26739369

  13. New geranylated flavanones from the fruits of Paulownia catalpifolia Gong Tong with their anti-proliferative activity on lung cancer cells A549.

    Science.gov (United States)

    Gao, Tian-yang; Jin, Xing; Tang, Wen-zhao; Wang, Xiao-jing; Zhao, Yun-xue

    2015-09-01

    Three new geranylated flavanones, named as paucatalinone A (1), B (2), and isopaucatalinone B (3), were isolated from the fruits of Paulownia catalpifolia Gong Tong (Scrophulariaceae). Their structures were well determined by means of IR, MS, 1D and 2D NMR, and CD techniques. Paucatalinone A (1) is the first sample as a dimeric geranylated flavanone derivative isolated from natural products. Paucatalinone A (1) displayed good antiproliferative effects on human lung cancer cells A549 and resulted in a clear increase of the percentage of cells in G1 phase and a decrease in the percentage of cells in S and G2/M phases in comparison with control cells. PMID:26115572

  14. In Vitro and Sensory Evaluation of Capsaicin-Loaded Nanoformulations

    OpenAIRE

    Mathias Kaiser; Benedikt Kirsch; Hannah Hauser; Désirée Schneider; Ingrid Seuß-Baum; Francisco M Goycoolea

    2015-01-01

    Capsaicin has known health beneficial and therapeutic properties. It is also able to enhance the permeability of drugs across epithelial tissues. Unfortunately, due to its pungency the oral administration of capsaicin is limited. To this end, we assessed the effect of nanoencapsulation of capsaicin, under the hypothesis that this would reduce its pungency. Core-shell nanocapsules with an oily core and stabilized with phospholipids were used. This system was used with or without chitosan coati...

  15. In Vitro and Sensory Evaluation of Capsaicin-Loaded Nanoformulations

    OpenAIRE

    Kaiser, M.; Kirsch, B.; Hauser, H; Schneider, D; Seuß-Baum, I. (Ingrid); Goycoolea, F. M.

    2016-01-01

    Capsaicin has known health beneficial and therapeutic properties. It is also able to enhance the permeability of drugs across epithelial tissues. Unfortunately, due to its pungency the oral administration of capsaicin is limited. To this end, we assessed the effect of nanoencapsulation of capsaicin, under the hypothesis that this would reduce its pungency. Core-shell nanocapsules with an oily core and stabilized with phospholipids were used. This system was used with or without chitosan coati...

  16. An Overview about Versatile Molecule Capsaicin

    Directory of Open Access Journals (Sweden)

    Arora R

    2011-10-01

    Full Text Available Capsaicin is a pungent highly domesticated fat soluble alkaloid having its origin from Bolvia and Brazil. It is biosynthesized via phenylpropanoid pathway and branched chain fatty acid pathway. Mostly found in trans isomeric form. Its pungent analogues are synthesized using amidation reactions catalyzed by lipases and non-pungent analogues using acyl chain lengths and different substituent in aromatic ring. It acts by binding TRPV1 and shows wide applications in relief from pain, breast and prostate cancer, obesity, heart diseases and hair loses. Its increased intake may cause lesions of liver and kidney along with gastric cancer. A review is made of capsaicin research focusing mainly on its origin, biosynthesis, chemistry and pharmacology, including its toxicological aspects.

  17. [Capsaicin in treatment of neuropathic pain].

    Science.gov (United States)

    Kamchatnov, P R; Evzelman, M A; Abusueva, B A; Volkov, A I

    2014-01-01

    Treatment of neuropathic pain (NP) is a serious medical problem. Antiepileptic drugs and antidepressants, used to relief pain, act on the central pain mechanisms and cause several side-effects, thus substantially restricting possibilities of their clinical application.At the same time, NP often has a peripheral component. Ligand-associated channels, including vanilloid receptors TRPV1, play a key role in the development of regional NP syndromes. Capsaicin, a component of chili pepper and several other plants, is a highly selective ligand of TRPV1 receptors and has long been used in treatment of pain syndromes. However, its using is limited by short-term action and relatively low efficacy. Recently it has been shown that the local use of single high doses of capsaicin during 30-60 min causes a marked stable(> 12 weeks) effect. The decrease in NP (>50%) is seen in about half of patients. Current studies will allow to single out groups of patients with the maximal treatment effect of capsaicin. PMID:25629137

  18. Neural proliferation and restoration of neurochemical phenotypes and compromised functions following capsaicin-induced neuronal damage in the nodose ganglion of the adult rat.

    Directory of Open Access Journals (Sweden)

    Zachary Rex Gallaher

    2011-02-01

    Full Text Available We previously reported that neuronal numbers within adult nodose ganglia (NG were restored to normal levels 60 days following the capsaicin-induced destruction of nearly half of the neuronal population. However, the nature of this neuronal replacement is not known. Therefore, we aimed to characterize neural proliferation, neurochemical phenotypes, and functional recovery within adult rat NG neurons following capsaicin-induced damage. Sprague-Dawley rats received intraperitoneal injections of capsaicin or vehicle solution, followed by BrdU injections to reveal cellular proliferation. NG were collected at multiple times post-treatment (up to 300 days and processed for immunofluorescence, real-time RT-PCR, and dispersed cell cultures. Capsaicin-induced cellular proliferation, indicated by BrdU/Ki-67-labeled cells, suggests that lost neurons were replaced through cell division. NG cells expressed the stem cell marker, nestin, indicating that these ganglia have the capacity to generate new neurons. BrdU incorporation within beta-III tubulin-positive neuronal profiles following capsaicin suggests that proliferating cells matured to become neurons. NG neurons displayed decreased NMDAR expression up to 180 days post-capsaicin. However, both NMDAR expression within the NG and synaptophysin expression within the central target of NG neurons, the NTS, were restored to pre-injury levels by 300 days. NG cultures from capsaicin-treated rats contained bipolar neurons, normally found only during development. To test the functional recovery of NG neurons, we injected the satiety molecule, CCK. The effect of CCK on food intake was restored by 300 days post-capsaicin. This restoration may be due to the regeneration of damaged NG neurons or generation of functional neurons that replaced lost connections.

  19. Novel combination of sorafenib and celecoxib provides synergistic anti-proliferative and pro-apoptotic effects in human liver cancer cells.

    Directory of Open Access Journals (Sweden)

    Melchiorre Cervello

    Full Text Available Molecular targeted therapy has shown promise as a treatment for advanced hepatocellular carcinoma (HCC. Sorafenib, a multikinase inhibitor, recently received FDA approval for the treatment of advanced HCC. However, although sorafenib is well tolerated, concern for its safety has been expressed. Celecoxib (Celebrex® is a selective cyclooxygenase-2 (COX-2 inhibitor which exhibits antitumor effects in human HCC cells. The present study examined the interaction between celecoxib and sorafenib in two human liver tumor cell lines HepG2 and Huh7. Our data showed that each inhibitor alone reduced cell growth and the combination of celecoxib with sorafenib synergistically inhibited cell growth and increased apoptosis. To better understand the molecular mechanisms underlying the synergistic antitumor activity of the combination, we investigated the expression profile of the combination-treated liver cancer cell lines using microarray analysis. Combination treatment significantly altered expression levels of 1,986 and 2,483 transcripts in HepG2 and Huh7 cells, respectively. Genes functionally involved in cell death, signal transduction and regulation of transcription were predominantly up-regulated, while genes implicated in metabolism, cell-cycle control and DNA replication and repair were mainly down-regulated upon treatment. However, combination-treated HCC cell lines displayed specificity in the expression and activity of crucial factors involved in hepatocarcinogenesis. The altered expression of some of these genes was confirmed by semi-quantitative and quantitative RT-PCR and by Western blotting. Many novel genes emerged from our transcriptomic analyses, and further functional analyses may determine whether these genes can serve as potential molecular targets for more effective anti-HCC strategies.

  20. Late sensory function after intraoperative capsaicin wound instillation

    DEFF Research Database (Denmark)

    Aasvang, E K; Hansen, J B; Kehlet, H

    2010-01-01

    BACKGROUND: Intense capsaicin-induced C-fiber stimulation results in reversible lysis of the nerve soma, thereby making capsaicin wound instillation of potential interest for the treatment of post-operative pain. Clinical histological and short-term sensory studies suggest that the C-fiber function...

  1. Integrating TRPV1 Receptor Function with Capsaicin Psychophysics

    Directory of Open Access Journals (Sweden)

    Gregory Smutzer

    2016-01-01

    Full Text Available Capsaicin is a naturally occurring vanilloid that causes a hot, pungent sensation in the human oral cavity. This trigeminal stimulus activates TRPV1 receptors and stimulates an influx of cations into sensory cells. TRPV1 receptors function as homotetramers that also respond to heat, proinflammatory substances, lipoxygenase products, resiniferatoxin, endocannabinoids, protons, and peptide toxins. Kinase-mediated phosphorylation of TRPV1 leads to increased sensitivity to both chemical and thermal stimuli. In contrast, desensitization occurs via a calcium-dependent mechanism that results in receptor dephosphorylation. Human psychophysical studies have shown that capsaicin is detected at nanomole amounts and causes desensitization in the oral cavity. Psychophysical studies further indicate that desensitization can be temporarily reversed in the oral cavity if stimulation with capsaicin is resumed at short interstimulus intervals. Pretreatment of lingual epithelium with capsaicin modulates the perception of several primary taste qualities. Also, sweet taste stimuli may decrease the intensity of capsaicin perception in the oral cavity. In addition, capsaicin perception and hedonic responses may be modified by diet. Psychophysical studies with capsaicin are consistent with recent findings that have identified TRPV1 channel modulation by phosphorylation and interactions with membrane inositol phospholipids. Future studies will further clarify the importance of capsaicin and its receptor in human health and nutrition.

  2. Capsaicin-induced neurogenic inflammation in pig skin

    DEFF Research Database (Denmark)

    Di Giminiani, Pierpaolo; Petersen, Lars J; Herskin, Mette S

    2014-01-01

    Topical capsaicin is a well-established model of experimental hyperalgesia. Its application to the study of animals has been limited to few species. The effect of topical capsaicin on hyperalgesia in porcine skin was evaluated as part of a study of inflammatory pain in the pig. Two experiments we...

  3. Gastroprotection induced by capsaicin in healthy human subjects

    Institute of Scientific and Technical Information of China (English)

    Gyula Mózsik; János Szolcsányi; István Rácz

    2005-01-01

    AIM: To evaluate the gastro-protective effect of capsaicin against the ethanol- and indomethacin (IND)-induced gastric mucosal damage in healthy human subjects.METHODS: The effects of small doses (1-8 μg/mL,100 mL) of capsaicin on the gastric acid secretion basal acid output (BAO) and its electrolyte concentration,gastric transmucosal potential difference (GTPD),ethanol- (5 mL 300 mL/L i.g.) and IND- (3x25 mg/d)induced gastric mucosal damage were tested in a randomized, prospective study of 84 healthy human subjects. The possible role of desensitization of capsaicin-sensitive afferents was tested by repeated exposures and during a prolonged treatment.RESULTS: Intragastric application of capsaicin decreased the BAO and enhanced "non-parietal" component, GTPD in a dose-dependent manner. The decrease of GTPD evoked by ethanol was inhibited by the capsaicin application,which was reproducible. Gastric microbleeding induced by IND was inhibited by co-administration with capsaicin,but was not influenced by two weeks pretreatment with a daily capsaicin dose of 3x400 μg i.g.CONCLUSION: Capsaicin in low concentration range protects against gastric injuries induced by ethanol or IND, which is attributed to stimulation of the sensory nerve endings.

  4. Capsaicin modulates proliferation, migration, and activation of hepatic stellate cells.

    Science.gov (United States)

    Bitencourt, Shanna; Mesquita, Fernanda; Basso, Bruno; Schmid, Júlia; Ferreira, Gabriela; Rizzo, Lucas; Bauer, Moises; Bartrons, Ramon; Ventura, Francesc; Rosa, Jose Luis; Mannaerts, Inge; van Grunsven, Leo Adrianus; Oliveira, Jarbas

    2014-03-01

    Capsaicin, the active component of chili pepper, has been reported to have antiproliferative and anti-inflammatory effects on a variety of cell lines. In the current study, we aimed to investigate the effects of capsaicin during HSC activation and maintenance. Activated and freshly isolated HSCs were treated with capsaicin. Proliferation was measured by incorporation of EdU. Cell cycle arrest and apoptosis were investigated using flow cytometry. The migratory response to chemotactic stimuli was evaluated by a modified Boyden chamber assay. Activation markers and inflammatory cytokines were determined by qPCR, immunocytochemistry, and flow cytometry. Our results show that capsaicin reduces HSC proliferation, migration, and expression of profibrogenic markers of activated and primary mouse HSCs. In conclusion, the present study shows that capsaicin modulates proliferation, migration, and activation of HSC in vitro. PMID:23955514

  5. Capsaicin: From Plants to a Cancer-Suppressing Agent.

    Science.gov (United States)

    Chapa-Oliver, Angela M; Mejía-Teniente, Laura

    2016-01-01

    Capsaicinoids are plant secondary metabolites, capsaicin being the principal responsible for the pungency of chili peppers. It is biosynthesized through two pathways involved in phenylpropanoid and fatty acid metabolism. Plant capsaicin concentration is mainly affected by genetic, environmental and crop management factors. However, its synthesis can be enhanced by the use of elicitors. Capsaicin is employed as food additive and in pharmaceutical applications. Additionally, it has been found that capsaicin can act as a cancer preventive agent and shows wide applications against various types of cancer. This review is an approach in contextualizing the use of controlled stress on the plant to increase the content of capsaicin, highlighting its synthesis and its potential use as anticancer agent. PMID:27472308

  6. Antioxidant and antibacterial properties of capsaicine microemulsions

    OpenAIRE

    CRISTIAN DIMA; GIGI COMAN; MIHAELA COTÂRLEŢ; PETRU ALEXE; ŞTEFAN DIMA

    2013-01-01

    The aim of this study was to prepare capsaicin microemulsions and to assess their antioxidant and antibacterial properties. Pseudoternare phase diagrams were made and were highlighted O/W/S/CoS weight ratios corresponding to microemulsion states. The oil phase (O) was soybean oil and for the aqueous phase (W) was used a mixture of water and glycerol in a ratio of 4:1 (wt/wt). As a surfactant (S) was used Tween 40 and cosurfactant (CoS) was ethanol in the mass ratio S:CoS = 2:1. Viscosimetr...

  7. Treatment of notalgia paresthetica with capsaicin.

    Science.gov (United States)

    Leibsohn, E

    1992-05-01

    Twenty-four patients with notalgia paresthetica were treated with topical capsaicin (Zostrix) in a concentration of 0.025 percent for four months. In approximately 70 percent of the patients who remained in the study, relief of pruritus was achieved up to the 90 percent level. In the majority of these patients pruritus returned when use of the medication was stopped. The history, causes, and prevalence of the condition are reviewed. This treatment is the first described that is relatively effective. PMID:1521492

  8. Efeito anti-proliferativo das infusões de Achyrocline satureioides DC (Asteraceae sobre o ciclo celular de Allium cepa Anti-proliferative effect of infusions of Achyrocline satureioides on the Allium cepa cell cycle

    Directory of Open Access Journals (Sweden)

    Juliana M. Fachinetto

    2007-03-01

    Full Text Available Achyrocline satureioides (marcela é utilizada na medicina popular brasileira, na forma de chá, como tratamento de patologias digestivas e inflamatórias. O efeito anti-proliferativo de infusões de marcela sobre o ciclo celular da cebola foi avaliado, utilizando-se inflorescências de marcela recém coletadas (2005 e após armazenamento por 30 meses (2003. Preparou-se as infusões em duas concentrações: 5,0 mg/mL (concentração usual como chá e 20 mg/mL. Utilizaram-se 3 grupos de 6 bulbos de cebola para cada população de marcela. Retirou-se um grupo de bulbos controle de cada população. Todos os bulbos enraizados em água destilada foram transferidos para os extratos de marcela e permaneceram por 24 horas, (os bulbos controle permaneceram em água. As radículas foram coletadas, fixadas em etanol-ácido acético (3:1 por 24 h e estocadas em álcool 70%. Foram analisadas 6000 células por grupo de bulbos, e os índices mitóticos calculados submetidos a análise estatística pelo teste chi2 a 5%. Conclui-se que as infusões de marcela possuem ação antiproliferativa sobre o ciclo celular da cebola e que essa ação inibitória da divisão celular aumenta conforme aumento da concentração, bem como após o armazenamento.Achyrocline saturoides (marcela is used in Brazilian folk medicine as a tea in the treatment of digestive and inflammatory diseases. The anti-proliferative effect of infusions of marcela on onion cell cycle was evaluated by using the inflorescences of recently collected marcela and after the storage for 30 months. Marcela inflorescences were collected for the infusion preparations in 2003 and in 2005 (used still fresh. We prepared the infusions at two concentrations 5.0 mg/mL (concentration used as tea and 20 mg/mL. We used two groups of six onion bulbs for each population of marcela, and one group of bulbs of each population was withdrawn as a control group. All bulbs rooted in distilled water and after they were

  9. New steroidal 17β-carboxy derivatives present anti-5α-reductase activity and anti-proliferative effects in a human androgen-responsive prostate cancer cell line.

    Science.gov (United States)

    Amaral, Cristina; Varela, Carla; Correia-da-Silva, Georgina; Tavares da Silva, Elisiário; Carvalho, Rui A; Costa, Saul C P; Cunha, Sara C; Fernandes, José O; Teixeira, Natércia; Roleira, Fernanda M F

    2013-11-01

    The androgens testosterone (T) and dihydrotestosterone (DHT), besides playing an important role in prostate development and growth, are also responsible for the development and progression of benign prostate hyperplasia (BPH) and prostate cancer. Therefore, the actions of these hormones can be antagonized by preventing the irreversible conversion of T into DHT by inhibiting 5α-reductase (5α-R). This has been a useful therapeutic approach for the referred diseases and can be achieved by using 5α-reductase inhibitors (RIs). Steroidal RIs, finasteride and dutasteride, are used in clinic for BPH treatment and were also proposed for chemoprevention of prostate cancer. Nevertheless, due to the increase in bone and muscle loss, impotency and occurrence of high-grade prostate tumours, it is important to seek for other potent and specific molecules with lower side effects. In the present work, we designed and synthesized steroids with the 3-keto-Δ(4) moiety in the A-ring, as in the 5α-R substrate T, and with carboxamide, carboxyester or carboxylic acid functions at the C-17β position. The inhibitory 5α-R activity, in human prostate microsomes, as well as the anti-proliferative effects of the most potent compounds, in a human androgen-responsive prostate cancer cell line (LNCaP cells), were investigated. Our results showed that steroids 3, 4 and 5 are good RIs, which suggest that C-17β lipophylic amides favour 5α-R inhibition. Moreover, these steroids induce a decrease in cell viability of stimulated LNCaP cells, in a 5α-R dependent-manner, similarly to finasteride. PMID:23933094

  10. Characterization of capsaicin induced responses in mice vas deferens

    DEFF Research Database (Denmark)

    Sheykhzade, Majid; Gupta, Saurabh; Sørensen, Tinne;

    2011-01-01

    isolated preparations. The present study sets out to study and characterize the capsaicin as well as CGRP-induced responses in isolated mouse vas deferens. The effects of capsaicin and CGRP family of peptides were studied on electrically-induced twitch responses in the absence or presence of transient...... receptor potential cation channel vanilloid subfamily member 1 (TRPV1) antagonist and CGRP receptor antagonists. Twitch responses were attenuated by capsaicin (1nM-30nM) and CGRP family of peptides. The potency order was CGRP>intermedin-long (IMDL)~[Cys(Et)(2,7)]aCGRP~adrenomedullin (AM)>[Cys(ACM)(2,7)]a...

  11. Neonatal capsaicin causes compensatory adjustments to energy homeostasis in rats

    NARCIS (Netherlands)

    van de Wall, E. H. E. M.; Wielinga, P. Y.; Strubbe, J. H.; van Dijk, G.

    2006-01-01

    Several mechanisms involved in ingestive behavior and neuroendocrine activity rely on vagal afferent neuronal signaling. Seemingly contradictory to this idea are observations that vagal afferent neuronal ablation by neonatal capsaicin (CAP) treatment has relatively small effects on glucose homeostas

  12. EFFECT OF CAPSAICIN ON SUBSTANCE P IN PSORIASIS VULGARIS

    Institute of Scientific and Technical Information of China (English)

    王万卷; 谭升顺

    2003-01-01

    Objective To the investigate the mechanism of capsaicin in psoriasis vulgaris. Methods Substance P(SP) in psoriatic lesions before and 6 weeks after the treatment with capsaicin was detedted by radioimmunoassary. Results After 3 weeks and 6 weeks treatment with capsaicin, SP in psoriatic lesions was decreased (P<0.05), while it in the self-control group was not decreased; Overall the efficient incidence in therapeutic group was 78.8% , while it in the control group was 36.8%. There was significant difference between them (χ2=16.30, P<0.001). Conclusion Capsaicin inhibits dermal inflammatory responses and proliferation of keratinocytes by decreasing the expression of SP in psoriasis vulgaris.

  13. A novel, non-apoptotic role for Scythe/BAT3: a functional switch between the pro- and anti-proliferative roles of p21 during the cell cycle.

    Directory of Open Access Journals (Sweden)

    Sheila T Yong

    Full Text Available BACKGROUND: Scythe/BAT3 is a member of the BAG protein family whose role in apoptosis has been extensively studied. However, since the developmental defects observed in Bat3-null mouse embryos cannot be explained solely by defects in apoptosis, we investigated whether BAT3 is also involved in cell-cycle progression. METHODS/PRINCIPAL FINDINGS: Using a stable-inducible Bat3-knockdown cellular system, we demonstrated that reduced BAT3 protein level causes a delay in both G1/S transition and G2/M progression. Concurrent with these changes in cell-cycle progression, we observed a reduction in the turnover and phosphorylation of the CDK inhibitor p21, which is best known as an inhibitor of DNA replication; however, phosphorylated p21 has also been shown to promote G2/M progression. Our findings indicate that in Bat3-knockdown cells, p21 continues to be synthesized during cell-cycle phases that do not normally require p21, resulting in p21 protein accumulation and a subsequent delay in cell-cycle progression. Finally, we showed that BAT3 co-localizes with p21 during the cell cycle and is required for the translocation of p21 from the cytoplasm to the nucleus during the G1/S transition and G2/M progression. CONCLUSION: Our study reveals a novel, non-apoptotic role for BAT3 in cell-cycle regulation. By maintaining a low p21 protein level during the G1/S transition, BAT3 counteracts the inhibitory effect of p21 on DNA replication and thus enables the cells to progress from G1 to S phase. Conversely, during G2/M progression, BAT3 facilitates p21 phosphorylation by cyclin A/Cdk2, an event required for G2/M progression. BAT3 modulates these pro- and anti-proliferative roles of p21 at least in part by regulating cyclin A abundance, as well as p21 translocation between the cytoplasm and the nucleus to ensure that it functions in the appropriate intracellular compartment during each phase of the cell cycle.

  14. Capsaicin facilitates carotid sinus baroreceptor activity in anesthetized rats

    Institute of Scientific and Technical Information of China (English)

    HaoZHANG; Yi-xianLIU; Yu-mingWU; Ze-minWANG; Rui-rongHE

    2004-01-01

    AIM: To study the effect of capsaicin on carotid sinus baroreceptor activity (CBA). METHODS: The functional curve of carotid baroreceptor (FCCB) was constructed and the functional parameters of carotid sinus baroreceptor were measured by recording sinus nerve afferent discharge in anesthetized rats with perfused isolated carotid sinus. RESULTS: Low-concentration of capsaicin (0.2μmol/L) had no significant effect on CBA, while perfusion of the isolated carotid sinus with middle-concentration of capsaicin (1μmol/L) could shift FCCB to the left and upward,with peak slope (PS) increased from (2.47%±0.14%)/mmHg to (2.88%±0.10%)/mmHg (P<0.05) and peak integral value of carotid sinus nerve discharge (PIV) enhanced from 211%±5% to 238%±6% (P<0.01). The threshold pressure (TP) and saturation pressure (SP) were significantly decreased from 68.0±1.1 to 62.7±1.0mmHg (P<0.01) and from 171.0±1.6 to 165.0±0.6 mmHg (P<0.01). By perfusing with high-concentration of capsaicin (5μmol/L), FCCB was shifted to the left and upward further and the changes of the functional parameters such as PS, TP, and SP were concentration-dependent. Pretreatment with ruthenium red (100μmol/L), an antagonist of vanilloid receptor subtype 1 (VR1), blocked the effect of capsaicin on CBA. Preperfusion with glibenclamide(20μmol/L), a KATP channel blocker, could eliminate the effect of capsaicin on CBA. CONCLUSION: Capsaicin exerts a facilitatory role on the isolated carotid baroreceptor in a concentration-dependent manner. The facilitatory action of capsaicin may be attributed to the opening of KATP channels mediated by VR1.

  15. Capsaicin facilitates carotid sinus baroreceptor activity in anesthetized rats

    Institute of Scientific and Technical Information of China (English)

    Hao ZHANG; Yi-xian LIU; Yu-ming WU; Ze-min WANG; Rui-rong HE

    2004-01-01

    AIM: To study the effect of capsaicin on carotid sinus baroreceptor activity (CBA). METHODS: The functional curve of carotid baroreceptor (FCCB) was constructed and the functional parameters of carotid sinus baroreceptor were measured by recording sinus nerve afferent discharge in anesthetized rats with perfused isolated carotid sinus.RESULTS: Low-concentration of capsaicin (0.2 μmol/L) had no significant effect on CBA, while perfusion of the isolated carotid sinus with middle-concentration of capsaicin (1 μmol/L) could shift FCCB to the left and upward,with peak slope (PS) increased from (2.47 %±0.14 %)/mmHg to (2.88 %±0.10 %)/mmHg (P<0.05) and peak integral value of carotid sinus nerve discharge (PIV) enhanced from 211%±5 % to 238 %±6 % (P<0.01). The threshold pressure (TP) and saturation pressure (SP) were significantly decreased from 68.0±1.1 to 62.7±1.0mmHg (P<0.01) and from 171.0±1.6 to 165.0±0.6 mmHg (P<0.01). By perfusing with high-concentration of capsaicin (5 μmol/L), FCCB was shifted to the left and upward further and the changes of the functional parameters such as PS, TP, and SP were concentration-dependent. Pretreatment with ruthenium red (100 μmol/L), an antagonist of vanilloid receptor subtype 1 (VR1), blocked the effect of capsaicin on CBA. Preperfusion with glibenclamide(20 μmol/L), a KATp channel blocker, could eliminate the effect of capsaicin on CBA. CONCLUSION: Capsaicin exerts a facilitatory role on the isolated carotid baroreceptor in a concentration-dependent manner. The facilitatory action of capsaicin may be attributed to the opening of KATP channels mediated by VR1.

  16. A comprehensive review of the carcinogenic and anticarcinogenic potential of capsaicin.

    Science.gov (United States)

    Bley, Keith; Boorman, Gary; Mohammad, Bashir; McKenzie, Donald; Babbar, Sunita

    2012-08-01

    Human exposure to capsaicin, the most abundant pungent chili pepper component, is ubiquitous. Evaluation of capsaicin's carcinogenic potential has produced variable results in in vitro and in vivo genotoxicity and carcinogenicity assays. The capsaicin tested in older studies was often from pepper plant extracts and included other capsaicinoids and diverse impurities. Recent studies utilizing high-purity capsaicin and standardized protocols provide evidence that the genotoxic and carcinogenic potential of capsaicin is quite low and that the purity of capsaicin is important. Several small epidemiological studies suggest a link between capsaicin consumption and stomach or gall bladder cancer, but contamination of capsaicin-containing foods with known carcinogens renders their interpretation problematic. The postulated ability of capsaicin metabolites to damage DNA and promote carcinogenesis remains unsupported. Anticancer activities of capsaicin have been widely reported, as it inhibits the activity of carcinogens and induces apoptosis in numerous cancer cell lines in vitro and explanted into rodents. Diverse mechanisms have been postulated for capsaicin's anticancer properties. One hypothesis is that inhibition of cytochrome P450 enzymes-particularly CYP2E1-retards carcinogen activation but is contradicted by the low potency of capsaicin for CYP inhibition. The potential for dietary capsaicin to act as a chemopreventative is now widely postulated. PMID:22563012

  17. Similar itch and nociceptive sensations evoked by punctate cutaneous application of capsaicin, histamine and cowhage

    OpenAIRE

    Sikand, Parul; Shimada, Steven G.; Green, Barry G.; LaMotte, Robert H.

    2009-01-01

    Itch evoked by cowhage or histamine is reduced or blocked by capsaicin desensitization, suggesting that pruriceptive neurons are capsaicin-sensitive. Topical capsaicin can evoke both nociceptive sensations and itch, whereas intradermal injection of capsaicin evokes only burning pain. To dissociate the pruritic and nociceptive sensory effects caused by the chemical activation of sensory neurons, chemicals were applied in a punctiform manner to the skin of the forearm using individual, heat-ina...

  18. Putrescine facilitated enhancement of capsaicin production in cell suspension cultures of Capsicum frutescens.

    Science.gov (United States)

    Sudha, Govindaswamy; Ravishankar, Gokare A

    2003-04-01

    Putrescine treatment (0.1 mmol/L) influenced enhancement of growth and capsaicin production in the cell suspension cultures of C. frutescens. The administration of polyamine inhibitor DFMA (alpha-DL-difluoromethylarginine) resulted in a reduction of the growth, capsaicin content and the endogenous titres of polyamines (PAs). The capsaicin synthase activity was also higher in the putrescine (Put) treated cultures. Ethylene levels were lower in the cultures treated with putrescine. This study suggested that Put facilitates growth and capsaicin production.

  19. Use of Capsaicin to Treat Pain: Mechanistic and Therapeutic Considerations

    Directory of Open Access Journals (Sweden)

    Man-Kyo Chung

    2016-11-01

    Full Text Available Capsaicin is the pungent ingredient of chili peppers and is approved as a topical treatment of neuropathic pain. The analgesia lasts for several months after a single treatment. Capsaicin selectively activates TRPV1, a Ca2+-permeable cationic ion channel that is enriched in the terminals of certain nociceptors. Activation is followed by a prolonged decreased response to noxious stimuli. Interest also exists in the use of injectable capsaicin as a treatment for focal pain conditions, such as arthritis and other musculoskeletal conditions. Recently injection of capsaicin showed therapeutic efficacy in patients with Morton’s neuroma, a painful foot condition associated with compression of one of the digital nerves. The relief of pain was associated with no change in tactile sensibility. Though injection evokes short term pain, the brief systemic exposure and potential to establish long term analgesia without other sensory changes creates an attractive clinical profile. Short-term and long-term effects arise from both functional and structural changes in nociceptive terminals. In this review, we discuss how local administration of capsaicin may induce ablation of nociceptive terminals and the clinical implications.

  20. Hot Chili Peppers: Extraction, Cleanup, and Measurement of Capsaicin

    Science.gov (United States)

    Huang, Jiping; Mabury, Scott A.; Sagebiel, John C.

    2000-12-01

    Capsaicin, the pungent ingredient of the red pepper or Capsicum annuum, is widely used in food preparation. The purpose of this experiment was to acquaint students with the active ingredients of hot chili pepper (capsaicin and dihydrocapsaicin), the extraction, cleanup, and analysis of these chemicals, as a fun and informative analytical exercise. Fresh peppers were prepared and extracted with acetonitrile, removing plant co-extractives by addition to a C-18 solid-phase extraction cartridge. Elution of the capsaicinoids was accomplished with a methanol-acetic acid solution. Analysis was completed by reverse-phase HPLC with diode-array or variable wavelength detection and calibration with external standards. Levels of capsaicin and dihydrocapsaicin were typically found to correlate with literature values for a specific hot pepper variety. Students particularly enjoyed relating concentrations of capsaicinoids to their perceived valuation of "hotness".

  1. 美洛昔康抑制人结肠癌细胞增殖与Wnt/β-catenin信号的关系研究%Anti-proliferative effect of meloxicam and Wnt/β-catenin signal in colon cancer cells

    Institute of Scientific and Technical Information of China (English)

    周密; 何百成; 秧茂盛

    2015-01-01

    Aim To investigate the inhibitory effect of meloxicam ( Mel ) on human colon cancer LoVo cells and its mechanism. Methods Crystal violet staining assay and flow cytometry assay were performed to de-termine the anti-proliferative effect of Mel. Flow cy-tometry assay and H&E assay were used to evaluate the apoptotic effect of Mel. Luciferase reporter plasmid ISRE-Luc was employed to measure the effect of Mel on the activation of Wnt/β-catenin signaling transduc-tion. Western blot assay was used to detect effect of Mel on the expression level of β-catenin protein. Re-sults Compared with the control group, the inhibitory rate of cell proliferation at 72 h and 100 μmol · L-1 Mel was ( 57. 635 ± 3. 86 )% ( t = 10. 044 , P =0. 001);the cell apoptotic rate at 24 h and 60 μmol· L-1 Mel was ( 33. 6 ± 1. 7 )% ( t = 30. 166 , P =0. 001 );the transcriptional activities of TCF/LEF and Myc/Max at 24 h and 60 μmol · L-1 were ( 40. 05 ± 2. 79 )% ( t = 14. 864 , P = 0. 001 ) and ( 35. 9 ± 2. 38 )% ( t =16. 904 , P =0. 001 ) respectively; the levels of intracellular β-catenin protein at 24 h or 48 h and 40 μmol·L-1 were (71 ± 3. 78)%(t=7. 353,P=0. 003 ) or ( 52. 66 ± 3. 57 )% ( t = 11. 724 , P =0. 001 ) respectively. Conclusion Mel may inhibit proliferation and promote apoptosis of LoVo cells by in-hibiting Wnt/β-catenin pathway signaling transduction and decreasing intracellular β-catenin protein level.%目的:研究美洛昔康( meloxicam,Mel)对人结肠癌细胞LoVo增殖抑制作用及其机制。方法以人结肠癌细胞株LoVo为研究对象,体外药物敏感试验(结晶紫染色)和流式细胞术( FCM)分析Mel对细胞的增殖抑制作用;流式细胞术和HE染色检测Mel对细胞凋亡的影响;萤光素酶报告质粒检测Mel 对 Wnt/β-catenin 通路信号转导的影响;Western blot检测Mel对细胞内β-catenin蛋白水平的影响。结果与对照组相比,Mel能抑制LoVo细胞增殖,72 h、100μmol· L-1 Mel

  2. Natural Capsaicin in Capsicum chinense: Concentration vs. Origin

    Science.gov (United States)

    Capsaicin [N-vanillyl-8-methyl-6-(E) noneamide] is the most pungent of the group of compounds known as capsaicinoids in chili peppers. A survey was conducted to screen fruits of 307 hot pepper accessions of Capsicum chinense selected from the USDA germplasm collection for their major capsaicinoids c...

  3. Binding of Capsaicin to the TRPV1 Ion Channel.

    Science.gov (United States)

    Darré, Leonardo; Domene, Carmen

    2015-12-01

    Transient receptor potential (TRP) ion channels constitute a notable family of cation channels involved in the ability of an organisms to detect noxious mechanical, thermal, and chemical stimuli that give rise to the perception of pain, taste, and changes in temperature. One of the most experimentally studied agonist of TRP channels is capsaicin, which is responsible for the burning sensation produced when chili pepper is in contact with organic tissues. Thus, understanding how this molecule interacts and regulates TRP channels is essential to high impact pharmacological applications, particularly those related to pain treatment. The recent publication of a three-dimensional structure of the vanilloid receptor 1 (TRPV1) in the absence and presence of capsaicin from single particle electron cryomicroscopy experiments provides the opportunity to explore these questions at the atomic level. In the present work, molecular docking and unbiased and biased molecular dynamics simulations were employed to generate a structural model of the capsaicin-channel complex. In addition, the standard free energy of binding was estimated using alchemical transformations coupled with conformational, translational, and orientational restraints on the ligand. Key binding modes consistent with previous experimental data are identified, and subtle but essential dynamical features of the binding site are characterized. These observations shed some light into how TRPV1 interacts with capsaicin, and may help to refine design parameters for new TRPV1 antagonists, and potentially guide further developments of TRP channel modulators. PMID:26502196

  4. Biological Activities of Red Pepper (Capsicum annuum) and Its Pungent Principle Capsaicin: A Review.

    Science.gov (United States)

    Srinivasan, Krishnapura

    2016-07-01

    Capsaicin, the pungent alkaloid of red pepper (Capsicum annuum) has been extensively studied for its biological effects which are of pharmacological relevance. These include: cardio protective influence, antilithogenic effect, antiinflammatory, and analgesia, thermogenic influence, and beneficial effects on gastrointestinal system. Therefore, capsaicinoids may have the potential clinical value for pain relief, cancer prevention and weight loss. It has been shown that capsaicinoids are potential agonists of capsaicin receptor (TRPV1). They could exert the effects not only through the receptor-dependent pathway but also through the receptor-independent one. The involvement of neuropeptide Substance P, serotonin, and somatostatin in the pharmacological actions of capsaicin has been extensively investigated. Topical application of capsaicin is proved to alleviate pain in arthritis, postoperative neuralgia, diabetic neuropathy, psoriasis, etc. Toxicological studies on capsaicin administered by different routes are documented. Capsaicin inhibits acid secretion, stimulates alkali and mucus secretion and particularly gastric mucosal blood flow which helps in prevention and healing of gastric ulcers. Antioxidant and antiinflammatory properties of capsaicin are established in a number of studies. Chemopreventive potential of capsaicin is evidenced in cell line studies. The health beneficial hypocholesterolemic influence of capsaicin besides being cardio protective has other implications, viz., prevention of cholesterol gallstones and protection of the structural integrity of erythrocytes under conditions of hypercholesterolemia. Beneficial influences of capsaicin on gastrointestinal system include digestive stimulant action and modulation of intestinal ultrastructure so as to enhance permeability to micronutrients. PMID:25675368

  5. Hypolipidemic and antioxidant effects of curcumin and capsaicin in high-fat-fed rats.

    Science.gov (United States)

    Manjunatha, H; Srinivasan, K

    2007-06-01

    The beneficial hypolipidemic and antioxidant influences of the dietary spice compounds curcumin and capsaicin were evaluated. Curcumin, capsaicin, or their combination were included in the diet of high-(30%)-fat-fed rats for 8 weeks. Dietary high-fat-induced hypertriglyceridemia was countered by dietary curcumin, capsaicin, or their combination by 12%-20%. Curcumin, capsaicin, and their combination also produced a slight decrease in serum total cholesterol in these animals. Serum alpha-tocopherol content was increased by dietary curcumin, capsaicin, and their combination in high-fat-fed rats. Serum total thiol content in high-fat-fed animals and serum ascorbic acid in normal animals was elevated by the combination of curcumin and capsaicin. Hepatic glutathione was increased by curcumin, capsaicin, or their combination in normal animals. Hepatic glutathione and alpha-tocopherol were increased, whereas lipid peroxide level was reduced by dietary curcumin and combination of curcumin and capsaicin in high-fat-fed animals. Serum glutathione peroxidase and glutathione transferase in high-fat-fed rats were generally higher as a result of dietary curcumin, capsaicin, and the combination of curcumin and capsaicin. Hepatic glutathione reductase and glutathione peroxidase were significantly elevated by dietary spice principles in high-fat-fed animals. The additive effect of the 2 bioactive compounds was generally not evident with respect to hypolipidemic or antioxidant potential. However, the effectiveness of the combination was higher in a few instances.

  6. Attenuation of natural killer cell functions by capsaicin through a direct and TRPV1-independent mechanism.

    Science.gov (United States)

    Kim, Hun Sik; Kwon, Hyung-Joon; Kim, Gye Eun; Cho, Mi-Hyang; Yoon, Seung-Yong; Davies, Alexander J; Oh, Seog Bae; Lee, Heuiran; Cho, Young Keol; Joo, Chul Hyun; Kwon, Seog Woon; Kim, Sun Chang; Kim, Yoo Kyum

    2014-07-01

    The assessment of the biological activity of capsaicin, the compound responsible for the spicy flavor of chili pepper, produced controversial results, showing either carcinogenicity or cancer prevention. The innate immune system plays a pivotal role in cancer pathology and prevention; yet, the effect of capsaicin on natural killer (NK) cells, which function in cancer surveillance, is unclear. This study found that capsaicin inhibited NK cell-mediated cytotoxicity and cytokine production (interferon-γ and tumor necrosis factor-α). Capsaicin impaired the cytotoxicity of NK cells, thereby inhibiting lysis of standard target cells and gastric cancer cells by modulating calcium mobilization in NK cells. Capsaicin also induced apoptosis in gastric cancer cells, but that effect required higher concentrations and longer exposure times than those required to trigger NK cell dysfunction. Furthermore, capsaicin inhibited the cytotoxicity of isolated NK cells and of an NK cell line, suggesting a direct effect on NK cells. Antagonists of transient receptor potential vanilloid subfamily member 1 (TRPV1), a cognate capsaicin receptor, or deficiency in TRPV1 expression failed to prevent the defects induced by capsaicin in NK cells expressing functional TRPV1. Thus, the mechanism of action of capsaicin on NK cells is largely independent of TRPV1. Taken together, capsaicin may have chemotherapeutic potential but may impair NK cell function, which plays a central role in tumor surveillance. PMID:24743513

  7. Auditory Display

    DEFF Research Database (Denmark)

    volume. The conference's topics include auditory exploration of data via sonification and audification; real time monitoring of multivariate date; sound in immersive interfaces and teleoperation; perceptual issues in auditory display; sound in generalized computer interfaces; technologies supporting...... auditory display creation; data handling for auditory display systems; applications of auditory display....

  8. Intramuscular and intradermal injection of capsaicin: a comparison of local and referred pain

    DEFF Research Database (Denmark)

    Witting, Nanna; Svensson, Peter; Gottrup, Hanne;

    2000-01-01

    ), and one intradermal injection (i.d.): capsaicin 100 microg/20 microl. Local and referred pain intensities and areas were assessed from 0 to 60 min after injection. Intradermal capsaicin produced more intense local pain than i.m. capsaicin in the first min (skin: 68+/-6, muscle: 51+/-6 mm VASxmin, P...The present study compared capsaicin-induced muscle and skin pain in humans. Twelve healthy subjects received, in a randomised, balanced order, 3 intramuscular (i.m.) injections into the brachioradial muscle: capsaicin 100 microg/1 ml, capsaicin 100 microg/20 microl or 1 ml solvent (Tween 80....... The model with identical noxious stimulation of muscle and skin may be suitable for the study of differences in deep and superficial pain as seen in the clinic....

  9. Study on Vip protein expression in psoriatic epidermis with the topical treatment of capsaicin ointment

    Institute of Scientific and Technical Information of China (English)

    2006-01-01

    Objective: To investigate the mechanism of capsaicin in treating active psoriasis vulgaris. Methods: VIP protein in active psoriatic lesions before and 30 days after the treatment of capsaicin ointment was detected by immunohistochemistry. Results:There was positive expression of VIP in all layers of psoriatic lesions epidermis (95.5 % ), but after the treatment of capsaicin ointment,there was nearly no expression of VIP protein in epidermis(22.2% ). Conclusion: Capsaicin inhibits proliferation and induces the differentiation of keratinocytes through down-regulating the expression of VIP in psoriatic epidermis.

  10. Harnessing the Therapeutic Potential of Capsaicin and Its Analogues in Pain and Other Diseases.

    Science.gov (United States)

    Basith, Shaherin; Cui, Minghua; Hong, Sunhye; Choi, Sun

    2016-01-01

    Capsaicin is the most predominant and naturally occurring alkamide found in Capsicum fruits. Since its discovery in the 19th century, the therapeutic roles of capsaicin have been well characterized. The potential applications of capsaicin range from food flavorings to therapeutics. Indeed, capsaicin and few of its analogues have featured in clinical research covered by more than a thousand patents. Previous records suggest pleiotropic pharmacological activities of capsaicin such as an analgesic, anti-obesity, anti-pruritic, anti-inflammatory, anti-apoptotic, anti-cancer, anti-oxidant, and neuro-protective functions. Moreover, emerging data indicate its clinical significance in treating vascular-related diseases, metabolic syndrome, and gastro-protective effects. The dearth of potent drugs for management of such disorders necessitates the urge for further research into the pharmacological aspects of capsaicin. This review summarizes the historical background, source, structure and analogues of capsaicin, and capsaicin-triggered TRPV1 signaling and desensitization processes. In particular, we will focus on the therapeutic roles of capsaicin and its analogues in both normal and pathophysiological conditions. PMID:27455231

  11. The effects of Hot Pepper Extract and Capsaicin on Adipocyte Metabolism

    Directory of Open Access Journals (Sweden)

    Ching Sheng, Chu

    2008-03-01

    Full Text Available Objectives : The purpose of this study is to investigate the effects of hot pepper extract and capsaicin on the adipogenesis in 3T3-L1 cells, lipolysis in rat epididymal adipocytes and histological changes in porcine adipose tissue. Methods : Inhibiton of preadipocyte differentiation and/or stimulation of lipolysis play important roles in reducing obesity. 3T3-L1 preadipocytes were differentiated with adipogenic reagents by incubating for 3 days in the absence or presence of hot pepper extract or capsaicin ranging from 0.01 to 1㎎/㎖. The effects of hot pepper extract and capsaicin on adipogenesis were examined by measuring GPDH activity and by Oil Red O staining. Mature adipocytes from rat epididymal fat pad was incubated with hot pepper extract or capsaicin ranging from 0.01 to 1㎎/㎖ for 3 hrs. The effects of hot pepper extract and capsaicin on lipolysis were examined by measuring free glycerol released. Fat tissue from pig skin was injected with hot pepper extract or capsaicinCFP ranging from 0.1 to 10㎎/㎖ to examine the effects of hot pepper extract and capsaicin on histological changes under light microscopy. Results : The following results were obtained from present study on adipogenesis of preadipocytes, lipolysis of adipocytes and histological changes in fat tissue. 1. Hot pepper extract and capsaicin inhibited adipogenic differentiation at the concentration of 0.1 and 0.01㎎/㎖, respectively, indicating that capsaicin was more effective in inhibiting adipogenesis than hot pepper extract. 2. Hot pepper extract and capsaicin decreased the activity of glycerol-3-phosphate dehydrogenase(GPDH at the concentration of 0.1 and 0.01㎎/㎖, respectively, indicating that capsaicin was more effective in inhibiting adipogenic differentiation than hot pepper extract. 3. Hot pepper extract and capsaicin increased glycerol release at the concentration of 0.1㎎/㎖. There was no difference in lipolytic activity between hot pepper extract and

  12. Harnessing the Therapeutic Potential of Capsaicin and Its Analogues in Pain and Other Diseases

    Directory of Open Access Journals (Sweden)

    Shaherin Basith

    2016-07-01

    Full Text Available Capsaicin is the most predominant and naturally occurring alkamide found in Capsicum fruits. Since its discovery in the 19th century, the therapeutic roles of capsaicin have been well characterized. The potential applications of capsaicin range from food flavorings to therapeutics. Indeed, capsaicin and few of its analogues have featured in clinical research covered by more than a thousand patents. Previous records suggest pleiotropic pharmacological activities of capsaicin such as an analgesic, anti-obesity, anti-pruritic, anti-inflammatory, anti-apoptotic, anti-cancer, anti-oxidant, and neuro-protective functions. Moreover, emerging data indicate its clinical significance in treating vascular-related diseases, metabolic syndrome, and gastro-protective effects. The dearth of potent drugs for management of such disorders necessitates the urge for further research into the pharmacological aspects of capsaicin. This review summarizes the historical background, source, structure and analogues of capsaicin, and capsaicin-triggered TRPV1 signaling and desensitization processes. In particular, we will focus on the therapeutic roles of capsaicin and its analogues in both normal and pathophysiological conditions.

  13. Capsaicin-induced cell death in a human gastric adenocarcinoma cell line

    Institute of Scientific and Technical Information of China (English)

    Yi-Ching Lo; Yuan-Chen Yang; I-Chieh Wu; Fu-Chen Kuo; Chi-Ming Liu; Hao-Wei Wang; Chao-Hung Kuo; Jeng-Yi Wu; Deng-Chyang Wu

    2005-01-01

    AIM: Capsaicin, a pungent ingredient found in red pepper,has long been used in spices, food additives, and drugs.Cell death induced by the binding of capsaicin was examined in a human gastric adenocarcinoma cell line (AGS cells).METHODS: By using XTT-based cytotoxicityassay, flow cytometry using the TUNEL method, and quantitation of DNA fragmentation, both cell death and DNA fragmentation were detected in AGS cells treated with capsaicin. By using Western blotting methods, capsaicin reduced the expression of Bcl-2, the antiapoptotic protein, in AGS cells in a concentration-dependent manner.RESULTS: After incubation of AGS cells with capsaicin for 24 h, cell viability decreased significantly in a dose-dependent manner. After incubation of AGS cells with capsaicin for 24 h, apoptotic bodies also significantly increased, and were again correlated with the dose of capsaicin. When the concentration of capsaicin was 1 mmol/L, the amount of DNA fragments also increased. Similar results werealso in the lower traces.CONCLUSION: These results suggest that capsaicininduced cell death might be via a Bcl-2 sensitive apoptotic pathway. Therefore, capsaicin might induce protection from gastric cancer.

  14. Environmental risk assessment on capsaicin used as active substance for antifouling system on ships.

    Science.gov (United States)

    Wang, Jianbing; Shi, Ting; Yang, Xiaoling; Han, Wenya; Zhou, Yunrui

    2014-06-01

    Biodegradation experiments were carried out with capsaicin to evaluate its degradability. The results show that capsaicin was readily biodegradable under aerobic conditions. The values of Kow and the calculated bioconcentration factor indicate that capsaicin have a low potential for bioconcentration. The fish acute toxicity tests conducted with Brachydanio rerio show LC50 for capsaicin was 5.98 mg L(-1). The tests of alga growth inhibition conducted with Selenastrum capricornutum suggest EC50 for capsaicin was 114 mg L(-1). The calculated PNEC (Predicted No Effect Concentration) was 4.9×10(-4) mg L(-1). The average PEC (Predicted Environmental Concentration) for OECD-EU commercial harbor and marina were 3.99×10(-6) and 2.49×10(-5) mg L(-1), respectively. These indicate that the PEC was much less than the PNEC for capsaicin. The low Kp value of capsaicin suggests the data about the risk of capsaicin to sediment organisms can be waived. According to the results from the analysis of the degradation, bioaccumulation, toxicity and accumulation in sediment, it can be concluded that capsaicin used as active substance for antifouling system on ships poses relatively low risk to marine environment.

  15. Some like it hot: The emerging role of spicy food (capsaicin) in autoimmune diseases.

    Science.gov (United States)

    Deng, Yaxiong; Huang, Xin; Wu, Haijing; Zhao, Ming; Lu, Qianjin; Israeli, Eitan; Dahan, Shani; Blank, Miri; Shoenfeld, Yehuda

    2016-05-01

    Autoimmune diseases refer to a spectrum of diseases characterized by an active immune response against the host, which frequently involves increased autoantibody production. The pathogenesis of autoimmune diseases is multifactorial and the exploitation of novel effective treatment is urgent. Capsaicin is a nutritional factor, the active component of chili peppers, which is responsible for the pungent component of chili pepper. As a stimuli, capsaicin selectively activate transient receptor potential vanilloid subfamily 1(TRPV1) and exert various biological effects. This review discusses the effect of capsaicin through its receptor on the development and modulation of autoimmune diseases, which may shed light upon potential therapies in capsaicin-targeted approaches. PMID:26812350

  16. Human responses to inhaled capsaicin are not inhibited by granisetron.

    OpenAIRE

    Choudry, N B; McEwan, J. R.; Lavender, E A; Williams, A J; Fuller, R. W.

    1991-01-01

    Cough is a common respiratory symptom, the mechanism of which is poorly understood. In this study the role of 5-HT3 receptors was investigated. Capsaicin-induced cough and increase in airways resistance were measured in six male volunteers before and after infusion with granisetron 160 micrograms kg-1 or placebo. Neither cough nor the increase in respiratory resistance was altered by the active treatment. These results suggest that 5-HT3 receptors are not involved in these two respiratory res...

  17. Capsaicin: A Potent Inhibitor of Carbonic Anhydrase Isoenzymes

    Directory of Open Access Journals (Sweden)

    Betul Arabaci

    2014-07-01

    Full Text Available Carbonic anhydrase (CA, EC 4.2.1.1 is a zinc containing metalloenzyme that catalyzes the rapid and reversible conversion of carbon dioxide (CO2 and water (H2O into a proton (H+ and bicarbonate (HCO3– ion. On the other hand, capsaicin is the main component in hot chili peppers and is used extensively used in spices, food additives and drugs; it is responsible for their spicy flavor and pungent taste. There are sixteen known CA isoforms in humans. Human CA isoenzymes I, and II (hCA I and hCA II are ubiquitous cytosolic isoforms. In this study, the inhibition properties of capsaicin against the slow cytosolic isoform hCA I, and the ubiquitous and dominant rapid cytosolic isozymes hCA II were studied. Both CA isozymes were inhibited by capsaicin in the micromolar range. This naturally bioactive compound has a Ki of 696.15 µM against hCA I, and of 208.37 µM against hCA II.

  18. Combined treatment with capsaicin and resveratrol enhances neuroprotection against glutamate-induced toxicity in mouse cerebral cortical neurons

    NARCIS (Netherlands)

    Lee, J.G.; Yon, J.M.; Lin, C.; Jung, A.Y.; Jung, K.Y.; Nam, S.Y.

    2012-01-01

    Capsaicin and resveratrol as natural products have a variety of beneficial effects. However, capsaicin is also a neurotoxic agent, rendering its effect on the nervous system confusing. The aim of this study was to investigate whether capsaicin and/or resveratrol have a protective effect against glut

  19. CCK enhances response to gastric distension by acting on capsaicin-insensitive vagal afferents

    NARCIS (Netherlands)

    van de Wall, EHEM; Duffy, P; Ritter, RC

    2005-01-01

    Capsaicin treatment destroys vagal afferent C fibers and markedly attenuates reduction of food intake and induction of hindbrain Fos expression by CCK. However, both anatomical and electrophysiological data indicate that some gastric vagal afferents are not destroyed by capsaicin. Because CCK enhanc

  20. Extraction of capsaicins in aerosol defense sprays from fabrics.

    Science.gov (United States)

    Spicer, Oliver; Almirall, José R

    2005-08-15

    The use of aerosol defense sprays has increased as a means of self-defense and as a weapon in the commission of a crime. The residue of these sprays is often left behind as physical evidence on a victim's clothing or personal belongings. As the popularity of self-defense weaponry increases, so does the likelihood that it will be encountered in forensic casework. The extraction, recovery from fabrics, and identification of residue from defense sprays is described. The commonly used extraction method of liquid-liquid extraction is compared to solid phase microextraction (SPME) to recover capsaicin and dihydrocapsaicin from cotton swabs. The use of SPME resulted in lower limits of detection and greater recovery efficiency when compared to solvent extraction. SPME also provided more consistent recovery and less variability when compared to solvent extraction. The effect of use of various types of evidence packages on the preservation of this type of evidence is also reported. The collection and analysis of hand swabs after normal discharge of pepper spray canisters was studied indicating the low persistence of these compounds on the hands of the person conducting the spraying. Finally, the results of a real case whereby solvent-solvent extraction did not provide the necessary sensitivity for extracting the capsaicin compounds on the garments of a victim of an alleged spraying and the SPME extraction provided the recovery and identification of the compounds is also presented. PMID:18970178

  1. Capsaicin receptor immunoreactivity in the human trigeminal ganglion

    DEFF Research Database (Denmark)

    Hou, Mingyan; Uddman, Rolf; Tajti, Janos;

    2002-01-01

    ) in the human trigeminal ganglion (TG). In addition, RT-PCR confirmed the presence of VR1 mRNA in the human TG. It has been hypothesized that TG neuronal cell bodies are the source of capsaicin-stimulated release of calcitonin gene-related peptide (CGRP), and hence co-localization experiments were performed....... Around 10% of the VR1 receptor-ir is expressed on neurons that contain CGRP-ir (ten among 74) in the human TG, indicating that capsaicin may act through the VR1 receptor to modulate the release of CGRP and in turn to modulate pain. We observed that 8% of the VR1 receptor-ir neuronal cell bodies contain...... and protons, and therefore it is suggested as a molecular integrator of chemical and physical stimuli that elicit pain. In the present study, indirect immunofluorescence detected a small number of neurons that are VR1 receptor immunoreactive (ir) (171 versus 1038 or 16% of all neuronal cell bodies...

  2. Involvement of Endoplasmic Reticulum Stress in Capsaicin-Induced Apoptosis of Human Pancreatic Cancer Cells

    Directory of Open Access Journals (Sweden)

    Shengzhang Lin

    2013-01-01

    Full Text Available Capsaicin, main pungent ingredient of hot chilli peppers, has been shown to have anticarcinogenic effect on various cancer cells through multiple mechanisms. In this study, we investigated the apoptotic effect of capsaicin on human pancreatic cancer cells in both in vitro and in vivo systems, as well as the possible mechanisms involved. In vitro, treatment of both the pancreatic cancer cells (PANC-1 and SW1990 with capsaicin resulted in cells growth inhibition, G0/G1 phase arrest, and apoptosis in a dose-dependent manner. Knockdown of growth arrest- and DNA damage-inducible gene 153 (GADD153, a marker of the endoplasmic-reticulum-stress- (ERS- mediated apoptosis pathway, by specific siRNA attenuated capsaicin-induced apoptosis both in PANC-1 and SW1990 cells. Moreover, in vivo studies capsaicin effectively inhibited the growth and metabolism of pancreatic cancer and prolonged the survival time of pancreatic cancer xenograft tumor-induced mice. Furthermore, capsaicin increased the expression of some key ERS markers, including glucose-regulated protein 78 (GRP78, phosphoprotein kinase-like endoplasmic reticulum kinase (phosphoPERK, and phosphoeukaryotic initiation factor-2α (phospho-eIF2α, activating transcription factor 4 (ATF4 and GADD153 in tumor tissues. In conclusion, we for the first time provide important evidence to support the involvement of ERS in the induction of apoptosis in pancreatic cancer cells by capsaicin.

  3. The effects of chronic low-dose capsaicin treatment on substance P levels.

    Science.gov (United States)

    Erin, Nuray; Zik, Berrin; Sarigül, Münevver; Tütüncü, Serife

    2009-02-25

    Capsaicin, the pungent ingredient of red pepper, is consumed in varying amounts by many ethnic groups. It serves both therapeutically and as a specific tool to investigate sensory neurons. Although effects of high capsaicin doses are well-established, systemic effects of chronic low-dose capsaicin exposure are unknown. Sprague-Dawley rats (21-day old) were injected with capsaicin (0.5 mg/kg, ip) for 6 and 19 days. Changes in Substance P (SP) levels of lung and skin were measured. Two-step sequential acetic acid extraction was used to estimate neuronal and non-neuronal SP. Six-day, but not 19-day capsaicin treatment decreased SP levels in first as well as second extractions of both tissues. Because the cumulative dose used here was much lower than the neurotoxic doses of capsaicin, initial decrease of SP levels must be due to continuous release of SP from nerve endings as well as non-neuronal tissues. The fact that SP levels returned to control values at the end of 19-day treatment demonstrates that reactive increases in SP synthesis occurred. These findings suggest that systemic exposure to low-dose capsaicin enhances sensory nerve function and also increases SP in non-neuronal tissues. In addition, significantly decreased SP levels of both tissues were observed in 40-day, compared to 27-day old rats.

  4. Capsaicin and dihydrocapsaicin determination in chili pepper genotypes using ultra-fast liquid chromatography.

    Science.gov (United States)

    Usman, Magaji G; Rafii, Mohd Y; Ismail, Mohd R; Malek, Md Abdul; Latif, Mohammad Abdul

    2014-01-01

    Research was carried out to estimate the levels of capsaicin and dihydrocapsaicin that may be found in some heat tolerant chili pepper genotypes and to determine the degree of pungency as well as percentage capsaicin content of each of the analyzed peppers. A sensitive, precise, and specific ultra fast liquid chromatographic (UFLC) system was used for the separation, identification and quantitation of the capsaicinoids and the extraction solvent was acetonitrile. The method validation parameters, including linearity, precision, accuracy and recovery, yielded good results. Thus, the limit of detection was 0.045 µg/kg and 0.151 µg/kg for capsaicin and dihydrocapsaicin, respectively, whereas the limit of quantitation was 0.11 µg/kg and 0.368 µg/kg for capsaicin and dihydrocapsaicin. The calibration graph was linear from 0.05 to 0.50 µg/g for UFLC analysis. The inter- and intra-day precisions (relative standard deviation) were chili peppers studied except AVPP9703, AVPP0512, AVPP0307, AVPP0803 and AVPP0102 could serve as potential sources of capsaicin. On the other hand, only genotypes AVPP0506, AVPP0104, AVPP0002, C05573 and AVPP0805 gave a % capsaicin content that falls within the pungency limit that could make them recommendable as potential sources of capsaicin for the pharmaceutical industry. PMID:24853712

  5. Capsaicin: A novel chemopreventive molecule and its underlying molecular mechanisms of action

    Directory of Open Access Journals (Sweden)

    A A Oyagbemi

    2010-01-01

    Full Text Available Capsaicin (trans-8-methyl-N-vanillyl-6-nonenamide is the a principal pungent ingredient of hot red and chili peppers that belong to the plant genus Capsicum (Solanaceae. Capsaicin is a cancer-suppressing agent. It blocks the translocation of nuclear factor kappa B (NF-kB, activator protein 1 (AP-1, and signal transducer and activator of transcription (STAT3 signaling pathway that are required for carcinogenesis. The anti-inflammatory potential of capsaicin is attributed to its inhibitory effect on inducible COX-2 mRNA expression. Cytochrome P4502E1 mediates the activation of xenobiotics such as vinyl carbamate and dimethyl nitrosamine to their toxic metabolites. This metabolic activation of xenobiotics by Cytochrome P4502E1 has been shown to be inhibited by capsaicin. Capsaicin also generates reactive oxygen species in cells with resultant induction of apoptosis and cell cycle arrest, which is beneficial for cancer chemoprevention. Therefore, the use of capsaicin as a chemopreventive agent is of immense benefit for cancer chemoprevention. The search strategy included printed journals, pubmed, and medline, using the terms ′capsaicin′ and ′anticancer′ citations, relevant to anticancer properties of capsaicin.

  6. Capsaicin inhibits the Wnt/β-catenin signaling pathway by down-regulating PP2A.

    Science.gov (United States)

    Park, Dong-Seok; Yoon, Gang-Ho; Lee, Hyun-Shik; Choi, Sun-Cheol

    2016-09-01

    Xenopus embryo serves as an ideal model for teratogenesis assays to examine the effects of any substances on the cellular processes critical for early development and adult tissue homeostasis. In our chemical library screening with frog embryo, capsaicin was found to repress the Wnt/β-catenin signaling. Depending on the stages at which embryos became exposed to capsaicin, it could disrupt formation of dorsal or posterior body axis of embryo, which is associated with inhibition of maternal or zygotic Wnt signal in early development. In agreement with these phenotypes, capsaicin suppressed the expression of Wnt target genes such as Siamois and Chordin in the organizer region of embryo and in Wnt signals-stimulated tissue explants. In addition, the cellular level of β-catenin, a key component of Wnt pathway, was down-regulated in capsaicin-treated embryonic cells. Unlike wild-type β-catenin, its non-phosphorylatable mutant in which serine and threonine residues phosphorylated by GSK3 are substituted with alanine was not destabilized by capsaicin, indicative of the effect of this chemical on the phosphorylation status of β-catenin. In support of this, capsaicin up-regulated the level of GSK3- or CK1-phosphorylated β-catenin, concomitantly lowering that of its de-phosphorylated version. Notably, capsaicin augmented the phosphorylation of a phosphatase, PP2A at tyrosine 307, suggesting its repression of the enzymatic activity of the phosphatase. Furthermore, capsaicin still enhanced β-catenin phosphorylation in cells treated with a GSK3 inhibitor, LiCl but not in those treated with a phosphatase inhibitor, okadaic acid. Together, these results indicate that capsaicin inhibits the patterning of the dorso-ventral and anterior-posterior body axes of embryo by repressing PP2A and thereby down-regulating the Wnt/β-catenin signaling. PMID:27318088

  7. Repeated oral administration of capsaicin increases anxiety-like behaviours with prolonged stress-response in rats

    Indian Academy of Sciences (India)

    Y-J Choi; J Y Kim; S B Yoo; J-H Lee; J W Jahng

    2013-09-01

    This study was conducted to examine the psycho-emotional effects of repeated oral exposure to capsaicin, the principal active component of chili peppers. Each rat received 1 mL of 0.02% capsaicin into its oral cavity daily, and was subjected to behavioural tests following 10 daily administrations of capsaicin. Stereotypy counts and rostral grooming were significantly increased, and caudal grooming decreased, in capsaicin-treated rats during the ambulatory activity test. In elevated plus maze test, not only the time spent in open arms but also the percent arm entry into open arms was reduced in capsaicin-treated rats compared with control rats. In forced swim test, although swimming duration was decreased, struggling increased in the capsaicin group, immobility duration did not differ between the groups. Repeated oral capsaicin did not affect the basal levels of plasma corticosterone; however, the stress-induced elevation of plasma corticosterone was prolonged in capsaicin treated rats. Oral capsaicin exposure significantly increased c-Fos expression not only in the nucleus tractus of solitarius but also in the paraventricular nucleus. Results suggest that repeated oral exposure to capsaicin increases anxiety-like behaviours in rats, and dysfunction of the hypothalamic-pituitary-adrenal axis may play a role in its pathophysiology.

  8. Peripheral lidocaine, but not ketamine inhibit capsaicin-induced hyperalgesia in humans

    DEFF Research Database (Denmark)

    Gottrup, Hanne; Bach, Flemming Winther; Arendt-Nielsen, Lars;

    2000-01-01

    We examined the effect of the subcutaneous infiltration of ketamine, lidocaine and saline before injury on capsaicin-induced pain and hyperalgesia. Twelve healthy volunteers participated in two separate, randomized, double-blind, placebo-controlled crossover experiments. In experiment 1, 100...... micrograms capsaicin was injected intradermally in one volar forearm 10 min after the skin had been pretreated with lidocaine 20.0 mg in 2.0 ml or 0.9% saline 2.0 ml at the capsaicin injection site. In experiment 2, a similar capsaicin test was given 10 min after the skin had been pretreated with ketamine 5...... and brush stimuli, and areas of brush-evoked and punctate-evoked hyperalgesia. Lidocaine reduced all measures compared with placebo (P ketamine failed to change any measures. Pain scores and areas of hyperalgesia were not affected when the contralateral site was infiltrated with ketamine...

  9. Capsaicin-induced neurogenic inflammation in the skin in patients with symptoms induced by odorous chemicals

    DEFF Research Database (Denmark)

    Holst, Helle; Arendt-Nielsen, Lars; Mosbech, Holger;

    2011-01-01

    Intradermal injection of capsaicin induces the axonal release of neuropeptides, vasodilatation and flare, e.g. neurogenic inflammation. The spatial profile of neurogenic inflammation in the skin has been studied in various experimental models. Polarization spectroscopy imaging introduced recently...

  10. Lipopolysaccharide-induced hyperalgesia of intracranial capsaicin sensitive afferents in conscious rats

    NARCIS (Netherlands)

    Kemper, RHA; Spoelstra, MB; Meijler, WJ; Ter Horst, GJ

    1998-01-01

    Migraineous and non-migraineous headache is reported to be at highest intensity after an infection. This study investigated whether activation of the immune system can induce hyperalgesia in intracranial capsaicin sensitive afferents. The effects of intraperitoneal injected lipopolysaccharides (LPS)

  11. 75 FR 22788 - Garlic Oil and Capsaicin; Registration Review Proposed Decisions; Notice of Availability

    Science.gov (United States)

    2010-04-30

    .... Capsaicin is a naturally occurring polymer that comprises the principal active element of chili peppers..., Biopesticides and Pollution Prevention Division, Office of Pesticide Programs. BILLING CODE 6560-50-S...

  12. Capsaicin and Dihydrocapsaicin Determination in Chili Pepper Genotypes Using Ultra-Fast Liquid Chromatography

    Directory of Open Access Journals (Sweden)

    Magaji G. Usman

    2014-05-01

    Full Text Available Research was carried out to estimate the levels of capsaicin and dihydrocapsaicin that may be found in some heat tolerant chili pepper genotypes and to determine the degree of pungency as well as percentage capsaicin content of each of the analyzed peppers. A sensitive, precise, and specific ultra fast liquid chromatographic (UFLC system was used for the separation, identification and quantitation of the capsaicinoids and the extraction solvent was acetonitrile. The method validation parameters, including linearity, precision, accuracy and recovery, yielded good results. Thus, the limit of detection was 0.045 µg/kg and 0.151 µg/kg for capsaicin and dihydrocapsaicin, respectively, whereas the limit of quantitation was 0.11 µg/kg and 0.368 µg/kg for capsaicin and dihydrocapsaicin. The calibration graph was linear from 0.05 to 0.50 µg/g for UFLC analysis. The inter- and intra-day precisions (relative standard deviation were <5.0% for capsaicin and <9.9% for dihydrocapsaicin while the average recoveries obtained were quantitative (89.4%–90.1% for capsaicin, 92.4%–95.2% for dihydrocapsaicin, indicating good accuracy of the UFLC method. AVPP0705, AVPP0506, AVPP0104, AVPP0002, C05573 and AVPP0805 showed the highest concentration of capsaicin (12,776, 5,828, 4,393, 4,760, 3,764 and 4,120 µg/kg and the highest pungency level, whereas AVPP9703, AVPP0512, AVPP0307, AVPP0803 and AVPP0102 recorded no detection of capsaicin and hence were non-pungent. All chili peppers studied except AVPP9703, AVPP0512, AVPP0307, AVPP0803 and AVPP0102 could serve as potential sources of capsaicin. On the other hand, only genotypes AVPP0506, AVPP0104, AVPP0002, C05573 and AVPP0805 gave a % capsaicin content that falls within the pungency limit that could make them recommendable as potential sources of capsaicin for the pharmaceutical industry.

  13. The effect of codeine on the Urge-to-Cough response to inhaled capsaicin

    OpenAIRE

    Davenport, P.W.; Bolser, D. C.; Vickroy, T.; Berry, R.B.; Martin, A. D.; Hey, John A; Danzig, M.

    2006-01-01

    We have shown previously in normal subjects that a sensory measure, the Urge-to-Cough rating, increases at concentrations of inhaled capsaicin that are lower than those necessary to elicit reflex cough. This finding suggests that the Urge-to-Cough may represent an index of the cough response. Research on cough in the human has most often employed challenge with inhaled capsaicin to induce reflex cough. Current measures of cough sensitivity in the human provide no information regarding the int...

  14. Increased capsaicin-induced secondary hyperalgesia in patients with multiple chemical sensitivity

    DEFF Research Database (Denmark)

    Holst, Helle; Arendt-Nielsen, Lars; Mosbech, Holger;

    2011-01-01

    in experimental pain models to provoke peripheral and central sensitization. In patients with symptoms elicited by odorous chemicals capsaicin-induced secondary hyperalgesia and temporal summation were assessed as markers for abnormal central nociceptive processing together with neurogenic inflammation (flare).......the underlying cause of pathophysiological mechanisms triggering multiple chemical sensitivity (MCS) remains disputed.Recently, alterations in the central nervous system, for example,central sensitization, similar to various chronic pain disorders, have been suggested. Capsaicin is used...

  15. Differences in the chemesthetic subqualities of capsaicin, ibuprofen, and olive oil.

    Science.gov (United States)

    Bennett, Samantha M; Hayes, John E

    2012-06-01

    Chemesthetic sensations elicited by ibuprofen, extra-virgin olive oil, and capsaicin were compared to quantify perceptual differences between known agonists of TRPA1 and TRPV1. Extra virgin olive oil contains a phenolic compound, oleocanthal, which is thought to share unique chemesthetic qualities with the nonsteroidal anti-inflammatory drug, ibuprofen. Pilot work suggested participants had difficulty distinguishing between multiple chemesthetic subqualities (e.g., burn, sting, itch, tickle, etc.) in a multiattribute rating task. Here, we assessed overall irritation via direct scaling, and a check all that apply task was used to collect information about chemesthetic subqualities over time. Replicated ratings were collected at discrete intervals using the generalized labeled magnitude scale to generate time-intensity curves; maximum intensity (Imax) and area under the curve were extracted for each participant. Intensity responses varied substantially across participants, and within a participant, the relationship was strongest between ibuprofen and olive oil. However, there were also positive, albeit weaker, correlations between capsaicin and ibuprofen and capsaicin and olive oil. The correlation found between olive oil and capsaicin may suggest the presence of unknown TRPV1 agonists in olive oil. This view was also supported by the qualitative data: capsaicin was described most often as burning and warm/hot, whereas ibuprofen was numbing and tickling. Olive oil shared characteristics with both capsaicin (warm/hot) and ibuprofen (tickle). PMID:22281531

  16. The capsaicin cough reflex in eczema patients with respiratory symptoms elicited by perfume.

    Science.gov (United States)

    Elberling, Jesper; Dirksen, Asger; Johansen, Jeanne Duus; Mosbech, Holger

    2006-03-01

    Respiratory symptoms elicited by perfume are common in the population but have unclear pathophysiology. Increased capsaicin cough responsiveness has been associated with the symptoms, but it is unknown whether the site of the symptoms in the airways influences this association. The aim of this study was to investigate the association between the site of airway symptoms elicited by perfume and cough responsiveness to bronchial challenge with capsaicin. 21 eczema patients with respiratory symptoms elicited by perfume were compared with 21 healthy volunteers in a sex- and age-matched case control study. The participants completed a symptom questionnaire and underwent a bronchial challenge with capsaicin. Lower, but not upper, respiratory symptoms elicited by perfume were associated with increased capsaicin cough responsiveness. Having severe symptoms to perfume (n=11) did not relate to the site of the symptoms in the airways and was not associated with increased capsaicin cough responsiveness. In conclusion, respiratory symptoms elicited by perfume may reflect local hyperreactivity related to defensive reflexes in the airways, and measurements of the capsaicin cough reflex are relevant when patients with lower respiratory symptoms related to environmental perfume exposures are investigated.

  17. Display hardware

    International Nuclear Information System (INIS)

    To appreciate the limitations and possibilities of computer graphics it is necessary to have some acquaintance with the available technology. The aim of this chapter is to mention briefly the different display types and their 'ball-park' price ranges. It must be stressed that prices change rapidly, and so those quoted here are only intended to give an idea of the cost at the time of writing.

  18. Study on vasoactive intestinal polypeptide receptor 1 gene translation in psoriatic epidermis with the topical treatment of capsaicin ointment

    Institute of Scientific and Technical Information of China (English)

    2010-01-01

    Objective To investigate the mechanism of capsaicin in treating active psoriasis vulgaris.Methods A total of 42 patients with active psoriasis vulgaris diagnosed by histology and clinical features were given either placebo or 0.025% capsaicin ointment four times daily for 30 days randomly by double-blind method.Vasoactive intestinal polypeptide receptor 1(VIPR1)gene translation in active psoriatic lesions before and after treatment with capsaicin ointment was detected by in situ hybridization.Results There ...

  19. Comparison of in vitro metabolism and cytotoxicity of capsaicin and dihydrocapsaicin.

    Science.gov (United States)

    Halme, Mia; Pesonen, Maija; Salo, Heta; Söderström, Martin; Pasanen, Markku; Vähäkangas, Kirsi; Vanninen, Paula

    2016-01-15

    Capsaicin and dihydrocapsaicin are the major active components in pepper spray products, which are widely used for law enforcement and self-protection. The use of pepper sprays, due to their irreversible and other health effects has been under a strong debate. In this study, we compared metabolism and cytotoxicity of capsaicin and dihydrocapsaicin using human and pig liver cell fractions and human lung carcinoma cell line (A549) in vitro. Metabolites were screened and identified by liquid chromatography-tandem mass spectrometry (LC-MS/MS). Using liver cell fractions, a novel aliphatic hydroxylated metabolite (m/z 322) was detected to dihydrocapsaicin but no structure was found corresponding to capsaicin. Instead, a novel phase I metabolite of capsaicin, corresponding to the structure of aliphatic demethylation and dehydrogenation (m/z 294) was identified. In addition, two novel conjugates, glycine conjugates (m/z 363 and m/z 365) and bi-glutathione (GSH) conjugates (m/z 902 and m/z 904), were identified for both capsaicin and dihydrocapsaicin. The medium of the exposed A549 cells contained ω-hydroxylated (m/z 322) and alkyl dehydrogenated (m/z 304) forms, as well as a glycine conjugate of capsaicin. As to dihydrocapsaicin, an alkyl dehydrogenated (m/z 306) form, a novel alkyl hydroxylated form, and a novel glycine conjugate were found. In A549 cells, dihydrocapsaicin evoked vacuolization and decreased cell viability more efficiently than capsaicin. Furthermore, both compounds induced p53 protein and G1 phase cell cycle arrest. Usefulness of the found metabolites as biomarkers for capsaicinoid exposures will need further investigations with additional toxicity endpoints. PMID:26688344

  20. Characterization of cubosomes as a targeted and sustained transdermal delivery system for capsaicin

    Directory of Open Access Journals (Sweden)

    Peng X

    2015-08-01

    Full Text Available Xinsheng Peng,1* Yanfang Zhou,1* Ke Han,2,3 Lingzhen Qin,3 Linghui Dian,1 Ge Li,4 Xin Pan,3 Chuanbin Wu3 1Guangdong Medical University, Dongguan, 2The Second Affiliated Hospital of Guangzhou Medical University, 3School of Pharmaceutical Sciences, Sun Yat-Sen University, 4Guangzhou Neworld Pharmaceuticals Co. Ltd., Guangzhou, Guangdong, People’s Republic of China*These authors contributed equally to this work Abstract: Phytantriol- and glycerol monooleate-based cubosomes were produced and characterized as a targeted and sustained transdermal delivery system for capsaicin. The cubosomes were prepared by emulsification and homogenization of phytantriol (F1, glycerol monooleate (F2, and poloxamer dispersions, characterized for morphology and particle size distribution by transmission electron microscope and photon correlation spectroscopy. Their Im3m crystallographic space group was confirmed by small-angle X-ray scattering. An in vitro release study showed that the cubosomes provided a sustained release system for capsaicin. An in vitro diffusion study conducted using Franz diffusion cells indicated that the skin retention of capsaicin from cubosomes in the stratum corneum was much higher (2.75±0.22 µg versus 4.32±0.13 µg, respectively than that of capsaicin cream (0.72±0.13 µg. The stress testing showed that the cubosome formulations were stable under strong light and high temperature for up to 10 days. After multiapplications on mouse skin, the irritation of capsaicin cubosomes and cream was light with the least amount of side effects. Overall, the present study demonstrated that cubosomes may be a suitable skin-targeted and sustained delivery system for the transdermal administration of capsaicin. Keywords: cubosomes, skin-targeted delivery, capsaicin

  1. Inhibition of chronic pancreatitis and pancreatic intraepithelial neoplasia (PanIN) by capsaicin in LSL-KrasG12D/Pdx1-Cre mice

    OpenAIRE

    Bai, Han; Li, Haonan; Zhang, Wanying; Matkowskyj, Kristina A.; Liao, Jie; Srivastava, Sanjay K.; Yang, Guang-Yu

    2011-01-01

    Capsaicin is a major biologically active ingredient of chili peppers. Extensive studies indicate that capsaicin is a cancer-suppressing agent via blocking the activities of several signal transduction pathways including nuclear factor-kappaB, activator protein-1 and signal transducer and activator of transcription 3. However, there is little study on the effect of capsaicin on pancreatic carcinogenesis. In the present study, the effect of capsaicin on pancreatitis and pancreatic intraepitheli...

  2. A study on the comparison of antioxidant effects between hot pepper extract and capsaicin

    Directory of Open Access Journals (Sweden)

    Hyeon Min Gang

    2008-03-01

    Full Text Available Objective : The objective of this study was to compare the antioxidant effects of hot pepper extract and capsaicin. Methods : In vitro, antioxidant activities were examined by DPPH radical scavenging activity, total antioxidant capacity(TAC, oxygen radical scavenging capacity(ORAC, inhibition of induced lipid peroxidation using liver mitochonria and total phenolic contents. Results : 1. DPPH free radical scavenging actiivities at the concentrations of both 1 and 10㎎/㎖ were 1.2 to 1.9 times higher in capsaicin than in hot pepper extract. The concentration of capsaicin required for 50% radical scavenging was lower than that of hot pepper extract(3.9 vs 5.9㎎/㎖, indicating that capsaicin had higher DPPH radical scavenging activity than hot pepper extract. 2. Total antioxidant capacities of capsaicin at the concentrations of 0.1 and 1mg/ml(13.8 and 41.3 nmol Trolox equivalent were not significantly different from those at the concentrations of 1 and 10㎎/㎖(11.4 and 41.2nmol Trolox equivalent, indicating that capsaicin showed 10 times higher ABTS radical scavenging activity compared to hot pepper extract. 3. ORAC of capsaicin at the concentrations of 1, 5, 10 and 100 mg/ml were 0.04, 0.17, 0.29 and 1.74nmol gallic acid equivalent, respectively. On the other hand, ORAC of hot pepper extract at the concentrations of 1, 5, 10 and 100㎍/㎖ were 0.15, 0.44, 0.75 and 2.49nmol gallic acid equivalent, respectively, indicating that capsaicin showed higher peroxyl radical scavenging activity than hot pepper extract. 4. Inhibition of lipid peroxidation caused by hot pepper extract at the concentrations of 1 and 10mg/㎖ were 12.2 and 61.4%, respectively. Inhibition of lipid peroxidation caused by capsaicin at the concentrations of 1 and 10㎎/㎖l were 64.0 and 96.8%, respectively. Thus capsaicin showed 10 times stronger effect in inhibiton of lipid peroxidation than hot pepper extract. 5. Total phenolic contents of hot pepper extract at the

  3. Asthma exacerbation related with inhalation of hot peppers extract (capsaicin

    Directory of Open Access Journals (Sweden)

    Erkan Ceylan

    2013-09-01

    Full Text Available Objectives: In this study we aimed to prospectively investigate,asthma provoking factors and among thesefactors the place of Hot pepper (Isot during August-Septembermonths which are time period for processing isot.Methods: In this study, 73 female patients with exacerbationof asthma who applied to Chest Diseases OutpatientClinic and emergency department in the period of August-September (2010 were evaluated prospectively.Results: Seventy-three asthmatic female patients, meansage 34.7±6.1 (22-43 years were included. Patients withexacerbation of asthma provoking factors are; inhalationof isot pepper 28.8%, infections 23.3%, irregular use ofdrugs 16.4%, exposure to biomass and cigarette smoke13.7%, allergens 9.6%, emotional factors 5%, and gastroesophagealreflux 2.7%, physical exercise 1.4%.Conclusion: We observed that the most important asthmaprovoking factor was the inhalation of isot extract inasthmatic female patients in August-September (2010period in Sanliurfa. J Clin Exp Invest 2013; 4 (3: 331-334Key words: Asthma, hot pepper, Isot, capsaicin, Sanliurfa

  4. Role of Autophagy in Capsaicin-Induced Apoptosis in U251 Glioma Cells.

    Science.gov (United States)

    Liu, Ya-Ping; Dong, Fu-Xing; Chai, Xiang; Zhu, Shuang; Zhang, Bao-Le; Gao, Dian-Shuai

    2016-07-01

    In recent years, the role of capsaicin in cancer prevention and treatment has gained people's attention. However, the mechanism of anti-glioma cells by capsaicin has not been elucidated. Here, we discuss the mechanism of capsaicin in U251 cells. Cell viability was detected by MTT and extracellular LDH measurements, while immunofluorescence was performed to measure changes of LC3 in U251 cells. The expressions of LC3II, Puma-α, Beclin1, P62, Procaspase-3, and P53 were observed by immunoblotting. The cell viability decreased and the punctate patterns of LC3 in U251 cells were observed after Capsaicin treatment. Meanwhile, the expressions of Beclin1, P62, and Puma-α increased. After using 3-MA, the expressions of Beclin1 and Procaspase-3 were reduced while those of P53 and Puma-α increased. The expression of LC3II was increased after Pifithrin-α treatment. Therefore, we believed that capsaicin could induce apoptosis in U251 cells, and the inhibition of autophagy could contribute to apoptosis. PMID:26351174

  5. Hypolipidemic and antioxidant effects of dietary curcumin and capsaicin in induced hypercholesterolemic rats.

    Science.gov (United States)

    Manjunatha, H; Srinivasan, K

    2007-12-01

    Health beneficial hypolipidemic and antioxidant influences of dietary spice principles--curcumin, capsaicin alone and in combination included in the diet for 8 weeks were evaluated in induced hypercholesterolemic rats, in order to verify if there is any additive or synergistic effect of these two bioactive compounds. Dietary curcumin (0.2%), capsaicin (0.015%) or their combination significantly countered the hypercholesterolemia brought about by high cholesterol feeding. Hepatic cholesterol was lowered by dietary spice principles only in normal rats. Liver triglyceride levels were lowered in both normal and hypercholesterolemic rats by capsaicin. Curcumin and capsaicin lowered hepatic and blood lipid peroxides in hypercholesterolemic rats, while the effect in blood was additive with their combination. Hepatic ascorbic acid was enhanced by dietary spice principles in normal rats; glutathione was enhanced by their combination only in hypercholesterolemic rats. Activities of serum glutathione reductase, glutathione transferase and catalase and hepatic glutathione reductase in normal rats and serum glutathione peroxidase in hypercholesterolemic rats were enhanced by dietary spice principles. While dietary curcumin and capsaicin normalized the changes in the levels of antioxidant molecules and activities of antioxidant enzymes to a significant extent, this effect was not generally additive when given in combination, and was higher than the individual effects only in a few instances.

  6. The capsaicin cough reflex in eczema patients with respiratory symptoms elicited by perfume

    DEFF Research Database (Denmark)

    Elberling, Jesper; Dirksen, Asger; Johansen, Jeanne Duus;

    2006-01-01

    Respiratory symptoms elicited by perfume are common in the population but have unclear pathophysiology. Increased capsaicin cough responsiveness has been associated with the symptoms, but it is unknown whether the site of the symptoms in the airways influences this association. The aim of this st......Respiratory symptoms elicited by perfume are common in the population but have unclear pathophysiology. Increased capsaicin cough responsiveness has been associated with the symptoms, but it is unknown whether the site of the symptoms in the airways influences this association. The aim...... of this study was to investigate the association between the site of airway symptoms elicited by perfume and cough responsiveness to bronchial challenge with capsaicin. 21 eczema patients with respiratory symptoms elicited by perfume were compared with 21 healthy volunteers in a sex- and age-matched case...... control study. The participants completed a symptom questionnaire and underwent a bronchial challenge with capsaicin. Lower, but not upper, respiratory symptoms elicited by perfume were associated with increased capsaicin cough responsiveness. Having severe symptoms to perfume (n=11) did not relate...

  7. Capsaicin sensitizes TRAIL-induced apoptosis through Sp1-mediated DR5 up-regulation: Involvement of Ca2+ influx

    International Nuclear Information System (INIS)

    Although tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) induces apoptosis in various malignant cells, several cancers including human hepatocellular carcinoma (HCC) exhibit potent resistance to TRAIL-induced cell death. The aim of this study is to evaluate the anti-cancer potential of capsaicin in TRAIL-induced cancer cell death. As indicated by assays that measure phosphatidylserine exposure, mitochondrial activity and activation of caspases, capsaicin potentiated TRAIL-resistant cells to lead to cell death. In addition, we found that capsaicin induces the cell surface expression of TRAIL receptor DR5, but not DR4 through the activation Sp1 on its promoter region. Furthermore, we investigated that capsaicin-induced DR5 expression and apoptosis are inhibited by calcium chelator or inhibitors for calmodulin-dependent protein kinase. Taken together, our data suggest that capsaicin sensitizes TRAIL-mediated HCC cell apoptosis by DR5 up-regulation via calcium influx-dependent Sp1 activation. Highlights: ► Capsaicin sensitizes TRAIL-induced apoptosis through activation of caspases. ► Capsaicin induces expression of DR5 through Sp1 activation. ► Capsaicin activates calcium signaling pathway.

  8. Universal Numeric Segmented Display

    CERN Document Server

    Azad, Md Abul kalam; Kamruzzaman, S M

    2010-01-01

    Segmentation display plays a vital role to display numerals. But in today's world matrix display is also used in displaying numerals. Because numerals has lots of curve edges which is better supported by matrix display. But as matrix display is costly and complex to implement and also needs more memory, segment display is generally used to display numerals. But as there is yet no proposed compact display architecture to display multiple language numerals at a time, this paper proposes uniform display architecture to display multiple language digits and general mathematical expressions with higher accuracy and simplicity by using a 18-segment display, which is an improvement over the 16 segment display.

  9. The capsaicin cough reflex in patients with symptoms elicited by odorous chemicals

    DEFF Research Database (Denmark)

    Holst, H; Arendt-Nielsen, L; Mosbech, H;

    2010-01-01

    Patients with multiple chemical sensitivity and eczema patients with airway symptoms elicited by odorous chemicals have enhanced cough reflex to capsaicin when applying the tidal breathing method. The aims of the present study were to test whether the capsaicin induced cough reflex was enhanced...... when applying the single breath inhalation method in similar groups of patients with symptoms related to odorous chemicals e.g. other persons wearing of perfume; and to investigate to what extent the reporting of lower airway symptoms influenced the cough reflex. Sixteen patients fulfilling Cullen......'s criteria for multiple chemical sensitivity and 15 eczema patients with airway symptoms elicited by odorous chemicals were compared with 29 age-matched, healthy controls. We measured C5--the capsaicin concentration causing five coughs or more--using the single breath inhalation test. No difference was found...

  10. Gender differences in pain and secondary hyperalgesia after heat/capsaicin sensitization in healthy volunteers

    DEFF Research Database (Denmark)

    Jensen, Magnus Thorsten; Petersen, Karin Lottrup

    2006-01-01

    , but not total pain, during prolonged noxious thermal stimulation was higher in women. There was no gender difference in pain ratings during capsaicin sensitization or in heat pain detection thresholds. The results provided only limited support to the hypothesis that gender differences in clinical pain syndromes....../capsaicin sensitization, and heat pain detection thresholds. There was a trend toward smaller areas of secondary hyperalgesia in women. After adjusting for estimated gender differences in forearm surface area, areas to brush but not von Frey hair stimulation after capsaicin sensitization were larger in women. Peak pain...... can be explained by enhanced central sensitization in women. PERSPECTIVE: Our findings suggest that gender differences in nociceptive transmission and neuronal sensitization are small and provide only limited support to the hypothesis that gender differences in acute and chronic pain syndromes can...

  11. Improvement of symptoms of non-allergic chronic rhinitis by local treatment with capsaicin.

    Science.gov (United States)

    Lacroix, J S; Buvelot, J M; Polla, B S; Lundberg, J M

    1991-09-01

    Sixteen adult patients suffering from severe chronic non-allergic rhinitis with nasal vasoconstrictor abuse for more than a year, received, under local anaesthesia, an intranasal spray of capsaicin (3.3 x 10(-3) mol), the pungent agent in hot pepper, once weekly for 5 weeks. The subjective intensity of their nasal obstruction, rhinorrhoea and sneezing frequency were evaluated throughout the study and the vascular effects of capsaicin on the nasal mucosa were recorded by anterior rhinomanometry and laser Doppler flowmetry. Calcitonin gene-related peptide (CGRP) is a vasodilator agent present in sensory nerves and may play a major role in the vascular component of neurogenic inflammation. Therefore, the nasal mucosa content of CGRP-like immunoreactivity (CGRP-LI) was determined by radioimmunoassay in biopsies obtained before and after the capsaicin treatment. Intra-nasal capsaicin application evoked a larger vascular response in patients with rhinitis than in controls (P less than 0.05). Both nasal vascular responses and subjective discomfort following capsaicin were markedly reduced after the fifth application (P less than 0.01). In parallel, a 50% reduction of the CGRP-LI content in the nasal biopsies was observed. All symptoms were significantly improved throughout a 6 month follow-up period. No significant side-effects occurred and weaning from nasal vasoconstrictor agents was possible. Both the subjective symptom score and objective measurements of vascular reactivity suggest that repeated intra-nasal capsaicin application could be beneficial for patients with chronic rhinitis, possibly by reducing hyperreactive nasal reflexes. PMID:1742652

  12. Antilithogenic influence of dietary capsaicin and curcumin during experimental induction of cholesterol gallstone in mice.

    Science.gov (United States)

    Shubha, Malenahalli C; Reddy, Raghunatha R L; Srinivasan, Krishnapura

    2011-04-01

    Spice bioactive compounds, capsaicin and curcumin, were both individually and in combination examined for antilithogenic potential during experimental induction of cholesterol gallstones in mice. Cholesterol gallstones were induced by feeding mice a high-cholesterol (0.5%) diet for 10 weeks. Groups of mice were maintained on a lithogenic diet that was supplemented with 0.015% capsaicin/0.2% curcumin/0.015% capsaicin + 0.2% curcumin. The lithogenic diet that contained capsaicin, curcumin, or their combination reduced the incidence of cholesterol gallstones by 50%, 66%, and 56%, respectively, compared with lithogenic control. This was accompanied by reduced biliary cholesterol and a marginal increase in phospholipid in these spice-fed groups. Increased cholesterol saturation index and cholesterol : phospholipid ratio in the bile caused by the lithogenic diet was countered by the dietary spice compounds. The antilithogenic influence of spice compounds was attributable to the cholesterol-lowering effect of these dietary spices in blood and liver, as well as a moderate increase in phospholipids. Decreased activities of hepatic glutathione reductase and glutathione-S-transferase caused by the lithogenic diet were countered by the combination of capsaicin and curcumin. The increased lipid peroxidation and the decreased concentration of ascorbic acid in the liver that was caused by the lithogenic diet was countered by the dietary spice compounds, individually or in combination. Thus, while the capsaicin and curcumin combination did not have an additive influence in reducing the incidence of cholesterol gallstones in mice, their combination nevertheless was more beneficial in enhancing the activity of hepatic antioxidant enzyme ─ glutathione reductase in the lithogenic situation. The antioxidant effects of dietary spice compounds are consistent with the observed reduction in cholesterol gallstones formed under lithogenic condition.

  13. Capsaicin cough sensitivity and the association with clinical parameters in bronchiectasis.

    Directory of Open Access Journals (Sweden)

    Wei-jie Guan

    Full Text Available BACKGROUND: Cough hypersensitivity has been common among respiratory diseases. OBJECTIVE: To determine associations of capsaicin cough sensitivity and clinical parameters in adults with clinically stable bronchiectasis. METHODS: We recruited 135 consecutive adult bronchiectasis patients and 22 healthy subjects. History inquiry, sputum culture, spirometry, chest high-resolution computed tomography (HRCT, Leicester Cough Questionnaire scoring, Bronchiectasis Severity Index (BSI assessment and capsaicin inhalation challenge were performed. Cough sensitivity was measured as the capsaicin concentration eliciting at least 2 (C2 and 5 coughs (C5. RESULTS: Despite significant overlap between healthy subjects and bronchiectasis patients, both C2 and C5 were significantly lower in the latter group (all P<0.01. Lower levels of C5 were associated with a longer duration of bronchiectasis symptoms, worse HRCT score, higher 24-hour sputum volume, BSI and sputum purulence score, and sputum culture positive for P. aeruginosa. Determinants associated with increased capsaicin cough sensitivity, defined as C5 being 62.5 µmol/L or less, encompassed female gender (OR: 3.25, 95%CI: 1.35-7.83, P<0.01, HRCT total score between 7-12 (OR: 2.57, 95%CI: 1.07-6.173, P = 0.04, BSI between 5-8 (OR: 4.05, 95%CI: 1.48-11.06, P<0.01 and 9 or greater (OR: 4.38, 95%CI: 1.48-12.93, P<0.01. CONCLUSION: Capsaicin cough sensitivity is heightened in a subgroup of bronchiectasis patients and associated with the disease severity. Gender and disease severity, but not sputum purulence, are independent determinants of heightened capsaicin cough sensitivity. Current testing for cough sensitivity diagnosis may be limited because of overlap with healthy subjects but might provide an objective index for assessment of cough in future clinical trials.

  14. Activation of TRPV1 by dietary capsaicin improves endothelium-dependent vasorelaxation and prevents hypertension

    DEFF Research Database (Denmark)

    Yang, Dachun; Luo, Zhidan; Ma, Shuangtao;

    2010-01-01

    Some plant-based diets lower the cardiometabolic risks and prevalence of hypertension. New evidence implies a role for the transient receptor potential vanilloid 1 (TRPV1) cation channel in the pathogenesis of cardiometabolic diseases. Little is known about impact of chronic TRPV1 activation on the...... regulation of vascular function and blood pressure. Here we report that chronic TRPV1 activation by dietary capsaicin increases the phosphorylation of protein kinase A (PKA) and eNOS and thus production of nitric oxide (NO) in endothelial cells, which is calcium dependent. TRPV1 activation by capsaicin...

  15. Reaction to topical capsaicin in spinal cord injury patients with and without central pain

    DEFF Research Database (Denmark)

    Finnerup, Nanna Brix; Pedersen, Louise H.; Terkelsen, Astrid J.;

    2007-01-01

    Central neuropathic pain is a debilitating and frequent complication to spinal cord injury (SCI). Excitatory input from hyperexcitable cells around the injured grey matter zone is suggested to play a role for central neuropathic pain felt below the level of a spinal cord injury. Direct evidence...... of a spinal cord injury which already is hyperexcitable, would cause enhanced responses in patients with central pain at the level of injury compared to patients without neuropathic pain and healthy controls. Touch, punctuate stimuli, cold stimuli and topical capsaicin was applied above, at, and below injury...... at the level of injury. Keywords: Spinal cord injury; Neuropathic pain; Capsaicin; Neuronal hyperexcitability; Hyperalgesia; Blood flow...

  16. Spatial and Temporal Effects of Capsaicin and Menthol on Intraoral Somatosensory Sensitivity

    DEFF Research Database (Denmark)

    Lu, Shengyi; Baad-Hansen, Lene; Zhang, Zhenting;

    2015-01-01

    AIMS: To assess the spatial and temporal sensory effects of the topical application of capsaicin and menthol on the gingiva of healthy volunteers. METHODS: Capsaicin, menthol, and saline (control) were applied topically on the gingiva in the maxillary premolar area of healthy volunteers for 15...... minutes. Pain intensity was rated on a 0 to 10 visual analog scale (VAS). Before, immediately after, and 30 minutes after application, three mechanical stimuli were applied at 15 gingival sites: fixed-intensity stimuli were applied by 32 mN and 512 mN von Frey filaments, and stimuli of increasing...

  17. Inhibition of capsaicin and dihydrocapsaicin derivatives towards histone deacetylase and molecular docking studies

    Directory of Open Access Journals (Sweden)

    Pakit Kumboonma

    2016-08-01

    Full Text Available The natural products, capsaicin and dihydrocapsaicin, were modified at double-bond and phenolic moieties to provide twelve capsaicin and dihydrocapsaicin derivatives. The natural products and synthesized compounds were evaluated as histone deacetylase inhibitors via in vitro fluorometric assay at 500 mM concentrations. The results revealed that a methyl ester derivative and a silyl-protected dihydrocapsaicin were the best histone deacetylase inhibitors among the tested compounds with 87% and 85% inhibitions, respectively. Molecular docking experiments were conducted on the obtained compounds with the human HDAC8 enzyme. These data show a new method for providing putative histone deacetylase inhibitors from common natural products.

  18. Ultraviolet radiation-induced lipid peroxidation in liposomal membrane: modification by capsaicin

    International Nuclear Information System (INIS)

    Ultraviolet-radiation has been reported to cause lipid peroxidation in the liposomal membrane. In the present study, treatment with capsaicin, (8-methyl-n-vanillyl-6-nonenamide), the pungent principle of red hot pepper, was shown to modify UV-induced lipid peroxidation in the liposomal membrane. Treatment with low doses of capsaicin (less than 0.1 μg/mL of phosphatidyl choline liposome) produced a significant increase in UV-induced lipid peroxidation, while high doses (0.1-0.5 μg/mL of PC liposome) caused a significant decrease of UV-induced peroxidation

  19. Isolation,Identification and Cancer Cell Anti-proliferative Activity of Fomitopsis officinalis Fruit Body Constituents%药用拟层孔菌子实体的化学成分及其对肿瘤细胞增殖抑制

    Institute of Scientific and Technical Information of China (English)

    池梦怡; 贾力耕; 包海鹰

    2014-01-01

    Eight compounds,isolated and purified from Fomitopsis officinalis fruit bodies by silica gel column chromatography,Sephadex LH-20 column chromatography and recrystallization,were identified by NMR and mass spectrometry as 4,6,8 (14),22 (23)-tetraen-3-one-ergos-tane,ergosta-7,22,dien-3β-ol,3-keto-dehydrosulfurenic acid,dehydroeburicoic acid,dehydroeburiconic acid,and fomefficinic acids A,B and C. 4,6,8 (14),22 (23)-tetraen-3-one-ergostane has been isolated from F.officinalis fruit bodies for the first time.Fomefficinic acids A and C,3-keto-dehydrosulfurenic acid and dehydroeburicoic acid were obtained in high yield and tested for anti-proliferative activity against two human cancer cell lines.Fomefficinic acids A and C,and 3-keto-dehydrosulfurenic acid,inhibited the growth of MCF-7 human breast cancer cells,while fomefficinic acids A and C inhibited the growth of SMMC-7721 human liver cancer cells.%通过硅胶柱层析法、Sephadex LH-20凝胶柱层析法和重结晶法,分离纯化药用拟层孔菌(Fomitopsis officinalis)子实体中的化学成分,依据化合物的物理性质,运用核磁共振谱(nuclear magnetic resonance, NMR)、质谱(mass spectrometry,MS)等波谱法分析鉴定化合物结构,并选用得率较高的4种化合物进行体外抗肿瘤实验。共分离出8个化合物,为4,6,8(14),22(23)-四烯-3-酮-麦角甾烷、麦角甾-7,22-二稀-3β-醇、3-酮基-去氢硫色多孔菌酸、去氢齿孔酸、阿里红酸A、去氢齿孔酮酸、阿里红酸 C、阿里红酸 B。其中化合物4,6,8(14),22(23)-四烯-3-酮-麦角甾烷为首次从药用拟层孔菌子实体中分离得到。阿里红酸A、阿里红酸 C、3-酮基-去氢硫色多孔菌酸抑制人乳腺癌细胞MCF-7活性较好,阿里红酸A、阿里红酸 C 抑制人肝癌细胞 SMMC-7721活性较好。

  20. Synthesis of novel furozan-based nitric oxide-releasing derivatives of 1-oxo-oridonin with anti-proliferative activity%NO供体型呋咱类1-位氧代冬凌草甲素衍生物的合成及抗增殖活性

    Institute of Scientific and Technical Information of China (English)

    李达翃; 王磊; 蔡浩; 蒋博文; 张奕华; 孙益军; 徐进宜

    2012-01-01

    目的:为寻找新型一氧化氮(NO)供体型抗肿瘤候选药物,设计合成了一系列新型呋咱类1-位氧代冬凌草甲素衍生物.方法:首先合成不同呋咱类NO供体中间体(9a-i),再将它们与1-位氧代冬凌草甲素(2)的14-位羟基进行缩合,得到一系列NO供体型呋咱类1-位氧代冬凌草甲素衍生物;用Griess实验测试硝酸盐/亚硝酸盐的含量,从而间接测试了NO释放量;同时采用MTT法测定了目标化合物对4种人肿瘤细胞株增殖的抑制活性.结果:所有呋咱类NO供体衍生物在体外60 min时间点上都能释放大于19 μmol·L-1的NO.活性最好的目标化合物10h对Bel-7402细胞的增殖抑制活性IC50值达到0.74 μmol.L-1,优于阳性对照药紫杉醇;获得了初步构效关系信息.结论:利用NO供体和活性天然产物形成孪药分子有望成为发现新型抗肿瘤药物的途径之一.%AIM:To search for novel nitric oxide (NO) releasing anti-tumor agents,a series of furoxan-based nitric oxide-releasing derivatives of 1-oxo-oridonin were designed and synthesized.METHOD:Different furozan-based NO donors (ga-i) were synthesized and conjugated with the 14-hydroxyl of 1-oxo-oridonin (2).The level of nitrate/nitrite in the cell lysates was tested by Griess assay and the anti-proliferative activity of these derivatives against four human cancer cell lines was also determined.RESULTS:These furoxan-based NO-releasing derivatives could produce more than 19 μmol·L-1 of NO in vitro at the time point of 60 min.The most promising compound 10 h exhibited stronger activity than the positive control Taxol against the Bel-7402 cell line with an IC50 value 0.74 μmol.L-1.The structure-activity relationships were concluded based on the derived experimental data.CONCLUSION:These results suggested that NO-donor/natural product hybrids may provide a promising approach for the discovery of novel anti-tumor agents.

  1. Salinomycin对乳腺癌阿霉素耐药细胞株MCF-7/DOX的增殖抑制作用及机制%Anti-proliferative effect of salinomycin on doxorubicin-resistant human breast cancer MCF-7/DOX cells

    Institute of Scientific and Technical Information of China (English)

    刘浩; 卢敏莹; 贺智敏

    2015-01-01

    Aim To investigate the anti-proliferative effect of salinomycin on doxorubicin-resistant human breast cancer MCF-7 /DOX cells.Methods MCF-7 and MCF-7 /DOX cells were treated or untreated with salinomycin.Cell viability was detected by MTS assay. Cell apoptosis was detected by Annexin V-FITC /PI as-say.Reactive oxygen species (ROS)was measured by DCFH-DA staining.Mitochondrial membrane potential was measured by JC-1 assay.The expression of apopto-sis related proteins BAX, BCL-2, caspase-3, and caspase-9 were evaluated by Western blot analysis. Results The cell viability was significantly reduced by salinomycin treatment in a dose-dependent manner. The flow cytometry results showed that salinomycin in-duced MCF-7 /DOX cell apoptosis,increased ROS pro-duction,and decreased mitochondrial membrane poten-tial.Furthermore,salinomycin decreased the expres-sion of BCL-2,and increased the expression of BAX, cleaved caspase-3,and cleaved caspase-9.Moreover, the antioxidant N-acetylcysteine (NAC ) markedly blocked the above effects.Conclusions Our results suggest that salinomycin-induced apoptosis in MCF-7 /DOX is associated with induction of ROS production, and activation of mitochondria apoptosis pathway, which may become a potential chemotherapeutic agent for the therapy of doxorubicin resistant breast cancer.%目的:本研究旨在探讨 Salinomycin 对乳腺癌阿霉素耐药细胞株 MCF-7/DOX 增殖和凋亡的影响及可能作用机制。方法MTS 实验检测 Salinomycin 对 MCF-7/DOX 细胞增殖的影响;Annexin V-FITC /PI 染色检测 Salinomycin 对MCF-7/DOX 耐药细胞凋亡的影响;DCFH-DA 染色检测 Sali-nomycin 对 MCF-7/DOX 耐药细胞活性氧(reactive oxygen species,ROS)产生的影响;JC-1法测定细胞线粒体膜电位;Western blot 法检测细胞凋亡相关蛋白 BAX、BCL-2、caspase-3和 caspase-9的表达变化。结果Salinomycin 能明显抑制MCF-7/DOX 耐药细胞增殖,且具有浓度

  2. Capsaicin protects endothelial cells and macrophage against oxidized low-density lipoprotein-induced injury by direct antioxidant action.

    Science.gov (United States)

    Chen, Kuo-Shuen; Chen, Pei-Ni; Hsieh, Yih-Shou; Lin, Chin-Yin; Lee, Yi-Hsun; Chu, Shu-Chen

    2015-02-25

    Atherosclerosis is a chronic inflammatory vascular disease. It is characterized by endothelial dysfunction, lipid accumulation, leukocyte activation, and the production of inflammatory mediators and reactive oxygen species (ROS). Capsaicin, a biologically active compound of the red pepper and chili pepper, has several anti-oxidant, anti-inflammatory, anti-cancer, and hypolipidemic biological effects. However, its protective effects on foam cell formation and endothelial injury induced by oxidized low-density lipoprotein (oxLDL) remain unclear. In this study, we evaluated the anti-oxidative activity of capsaicin, and determined the mechanism by which capsaicin rescues human umbilical vein endothelial cells (HUVECs) from oxLDL-mediated dysfunction. The anti-oxidative activity of capsaicin was defined by Apo B fragmentation and conjugated diene production of the copper-mediated oxidation of LDL. Capsaicin repressed ROS generation, as well as subsequent mitochondrial membrane potential collapse, cytochrome c expression, chromosome condensation, and caspase-3 activation induced by oxLDL in HUVECs. Capsaicin also protected foam cell formation in macrophage RAW 264.7 cells. Our results suggest that capsaicin may prevent oxLDL-induced cellular dysfunction and protect RAW 264.7 cells from LDL oxidation. PMID:25603234

  3. Development, Characterization and Skin Interaction of Capsaicin-Loaded Microemulsion-Based Nonionic Surfactant.

    Science.gov (United States)

    Duangjit, Sureewan; Chairat, Wisuta; Opanasopit, Praneet; Rojanarata, Theerasak; Panomsuk, Suwannee; Ngawhirunpat, Tanasait

    2016-01-01

    The aim of this study was to develop novel microemulsions (MEs) for the transdermal delivery of capsaicin. Microemulsion-based nonionic surfactants consisting of isopropyl myristate as the oil phase, various nonionic surfactants as the surfactant (S), various glycols or alcohol as the co-surfactant (CoS), and reverse osmosis water as the aqueous phase were formulated. Based on the optimal ME obtained from Design Expert, MEs containing a fixed concentration of oil, water or surfactant were prepared while varying the amounts of the other two fractions. The results indicated that the skin permeation flux of low dose capsaicin (0.15% (w/w)) was significantly higher for the selected ME than the commercial product and capsaicin in ethanol (control) by approximately two- and four-fold, respectively. We successfully demonstrated the feasibility of the transdermal delivery of capsaicin-loaded ME using a low concentration of nonionic surfactant and ethanol. Moreover, the optimization using computer program helped to simplify the development of a pharmaceutical product. PMID:27040633

  4. Comparison of the effects of pelargonic acid vanillylamide and capsaicin on human vanilloid receptors.

    Science.gov (United States)

    Weiser, Thomas; Roufogalis, Basil; Chrubasik, Sigrun

    2013-07-01

    Pelargonic acid vanillylamide is like capsaicin a natural capsaicinoid from chili peppers and commonly used in food additives to create a hot sensation, even in self-defense pepper sprays and as an alternative to capsaicin in medical products for topical treatment of pain. Although the chemical structures of both compounds are similar, preclinical data suggest that capsaicin is the more potent compound. We therefore performed voltage-clamp recordings using cells transfected with the human vanilloid receptor TRPV1 in order to assess the responses of pelargonic acid vanillylamide and capsaicin at the receptor level. We provide evidence that at the molecular target TRPV1, the concentration-response curves, kinetics of current activation, as well as inhibition by the competitive antagonist capsazepine were not significantly different between the two capsaicinoids. We suggest that the different effects of the two capsaicinoids observed in previous studies may rather be due to different physicochemical or pharmacokinetic properties than to different pharmacological profiles at the receptor level. PMID:22961689

  5. Cardiovascular effects of substance P and capsaicin microinjected into the nucleus tractus solitarii of the rat

    NARCIS (Netherlands)

    Lukovic, L.; Jong, Wybren de; Wied, D. de

    1987-01-01

    This report deals with the effect of substance P (SP) and capsaicin on blood pressure and heart rate after administration into different sites of the nucleus tractus solitarii (NTS) of urethane-anesthetized rats. Microinjection of SP at 6 different coordinates throughout the NTS showed 3 sites where

  6. Comparison between Chemical Senses Thresholds for Capsaicin and Dihydrocapsaicin in Aqueous Solutions and Identification of the Area of Burning Sensation

    Directory of Open Access Journals (Sweden)

    D.J. Schneider

    2014-01-01

    Full Text Available In the present study, the pungency detection thresholds for capsaicin and dihydrocapsaicin in aqueous solutions containing an emulsifier (polysorbate 80 were determined and compared. Thresholds were measured for 21 students (12 chili “users” and 9 “non users” using a 3-Alternative Forced Choice sensory test with ascending concentrations of capsaicin and dihydrocapsaicin (0.025, 0.045, 0.090, 0.180 and 0.360 ppm, respectively. In addition, the panelists were asked where the irritation occurred (throat, tongue or both. The group Best Estimate Thresholds were 0.080 and 0.049 ppm for capsaicin and dihydrocapsaicin, respectively and differed significantly. Chili “users” and “non users” did not differ significantly in their perception of capsaicin and dihydrocapsaicin, suggesting that no desensitization effects occur. In accordance with previous studies, in most cases the first irritation was experienced in the throat.

  7. Molecularly imprinted polymers with synthetic dummy templates for the preparation of capsaicin and dihydrocapsaicin from chili peppers.

    Science.gov (United States)

    Ma, Xiuli; Ji, Wenhua; Chen, Lingxiao; Wang, Xiao; Liu, Jianhua; Wang, Xueyong

    2015-01-01

    In this work, dummy molecularly imprinted polymers with high selectivity and affinity to capsaicin and dihydrocapsaicin are designed using N-vanillylnonanamide as a dummy template. The performance of dummy molecularly imprinted polymers and nonimprinted polymers was evaluated using adsorption isotherms, adsorption kinetics, and selective recognition capacity. Dummy molecularly imprinted polymers were found to exhibit good site accessibility, taking just 20 min to achieve adsorption equilibrium; they were also highly selective toward capsaicin and dihydrocapsaicin. We successfully used dummy molecularly imprinted polymers as a specific sorbent for selectively enriching capsaicin and dihydrocapsaicin from chili pepper samples. In a scaled-up experiment, the selective recovery of capsaicinoids was calculated to be 77.8% using solid-phase extraction. To the best of our knowledge, this is the first example of the use of N-vanillylnonanamide as a dummy template in molecularly imprinted polymers to simultaneously enrich capsaicin and dihydrocapsaicin. PMID:25348490

  8. Reproducibility of the capsaicin-induced dermal blood flow response as assessed by laser Doppler perfusion imaging

    OpenAIRE

    Van der Schueren, B J; Hoon, J.N.; Vanmolkot, F H; van Hecken, A; Depre, M; Kane, S.A.; De Lepeleire, I; Sinclair, S R

    2007-01-01

    What is already known about this subjectCapsaicin rapidly produces local neurogenic inflammation (characterized by oedema and erythema) when locally administered to the human skin by binding to the TRPV1 receptor present on dermal sensory nerve endings.In nonhuman primates, a pharmacodynamic assay has been described and validated using capsaicin-induced dermal vasodilation measured by laser Doppler perfusion imaging to assess calcitonin gene-related peptide antagonist activity.Laser Doppler p...

  9. Protein phosphatase 2A regulates central sensitization in the spinal cord of rats following intradermal injection of capsaicin

    Directory of Open Access Journals (Sweden)

    Fang Li

    2006-03-01

    Full Text Available Abstract Background Intradermal injection of capsaicin into the hind paw of rats induces spinal cord central sensititzation, a process in which the responsiveness of central nociceptive neurons is amplified. In central sensitization, many signal transduction pathways composed of several cascades of intracellular enzymes are involved. As the phosphorylation state of neuronal proteins is strictly controlled and balanced by the opposing activities of protein kinases and phosphatases, the involvement of phosphatases in these events needs to be investigated. This study is designed to determine the influence of serine/threonine protein phosphatase type 2A (PP2A on the central nociceptive amplification process, which is induced by intradermal injection of capsaicin in rats. Results In experiment 1, the expression of PP2A protein in rat spinal cord at different time points following capsaicin or vehicle injection was examined using the Western blot method. In experiment 2, an inhibitor of PP2A (okadaic acid, 20 nM or fostriecin, 30 nM was injected into the subarachnoid space of the spinal cord, and the spontaneous exploratory activity of the rats before and after capsaicin injection was recorded with an automated photobeam activity system. The results showed that PP2A protein expression in the spinal cord was significantly upregulated following intradermal injection of capsaicin in rats. Capsaicin injection caused a significant decrease in exploratory activity of the rats. Thirty minutes after the injection, this decrease in activity had partly recovered. Infusion of a phosphatase inhibitor into the spinal cord intrathecal space enhanced the central sensitization induced by capsaicin by making the decrease in movement last longer. Conclusion These findings indicate that PP2A plays an important role in the cellular mechanisms of spinal cord central sensitization induced by intradermal injection of capsaicin in rats, which may have implications in

  10. Inactivation of capsaicin-sensitive nerves reduces pulmonary remodeling in guinea pigs with chronic allergic pulmonary inflammation

    OpenAIRE

    C.M. Prado; G.Z. da Rocha; E.A. Leick-Maldonado; C.M. Starling; V.L. Capelozzi; M. A. Martins; I.F.L.C. Tibério

    2011-01-01

    Pulmonary remodeling is an important feature of asthma physiopathology that can contribute to irreversible changes in lung function. Although neurokinins influence lung inflammation, their exact role in the extracellular matrix (ECM) remodeling remains to be determined. Our objective was to investigate whether inactivation of capsaicin-sensitive nerves modulates pulmonary ECM remodeling in animals with chronic lung inflammation. After 14 days of capsaicin (50 mg/kg, sc) or vehicle administrat...

  11. Intraluminal capsaicin does not affect fluid and electrolyte absorption in the human jejunum but does cause pain

    OpenAIRE

    Hammer, J.; Hammer, H; Eherer, A; Petritsch, W; Holzer, P.; Krejs, G

    1998-01-01

    Background—Stimulation of sensory nerves with capsaicin regulates ion transport in the small intestine in animal experiments. 
Aim—To investigate whether sensory nerves that are stimulated by capsaicin administration influence fluid and electrolyte absorption in the human jejunum in vivo. 
Method—Intestinal perfusion studies were performed in 12 healthy subjects using a four lumen tube with a proximal occlusion balloon and a plasma-like electrolyte solution. After an init...

  12. Identification of capsaicin-sensitive rectal mechanoreceptors activated by rectal distension in mice.

    Science.gov (United States)

    Spencer, N J; Kerrin, A; Singer, C A; Hennig, G W; Gerthoffer, W T; McDonnell, O

    2008-05-01

    Rodents detect visceral pain in response to noxious levels of rectal distension. However, the mechanoreceptors that innervate the rectum and respond to noxious levels of rectal distension have not been identified. Here, we have identified the mechanoreceptors of capsaicin-sensitive rectal afferents and characterized their properties in response to circumferential stretch of the rectal wall. We have also used the lethal spotted (ls/ls) mouse to determine whether rectal mechanoreceptors that respond to capsaicin and stretch may also develop in an aganglionic rectum that is congenitally devoid of enteric ganglia. In wild type (C57BL/6) mice, graded increases in circumferential stretch applied to isolated rectal segments activated a graded increase in firing of slowly-adapting rectal mechanoreceptors. Identical stimuli applied to the aganglionic rectum of ls/ls mice also activated similar graded increases in firing of stretch-sensitive rectal afferents. In both wild type and aganglionic rectal preparations, focal compression of the serosal surface using von Frey hairs identified mechanosensitive "hot spots," that were associated with brief bursts of action potentials. Spritzing capsaicin (10 microM) selectively onto each identified mechanosensitive hot spot activated an all or none discharge of action potentials in 32 of 56 identified hot spots in wild type mice and 24 of 62 mechanosensitive hot spots in the aganglionic rectum of ls/ls mice. Each single unit activated by both capsaicin and circumferential stretch responded to low mechanical thresholds (1-2 g stretch). No high threshold rectal afferents were ever recorded in response to circumferential stretch. Anterograde labeling from recorded rectal afferents revealed two populations of capsaicin-sensitive mechanoreceptor that responded to stretch: one population terminated within myenteric ganglia, the other within the circular and longitudinal smooth muscle layers. In the aganglionic rectum of ls/ls mice, only the

  13. Improved oral bioavailability of capsaicin via liposomal nanoformulation: preparation, in vitro drug release and pharmacokinetics in rats.

    Science.gov (United States)

    Zhu, Yuan; Wang, Miaomiao; Zhang, Jiajia; Peng, Wei; Firempong, Caleb Kesse; Deng, Wenwen; Wang, Qilong; Wang, Shicheng; Shi, Feng; Yu, Jiangnan; Xu, Ximing; Zhang, Weiming

    2015-04-01

    This study innovatively prepared an effective capsaicin-loaded liposome, a nanoformulation with fewer irritants, for oral administration. The in vitro and in vivo properties of the liposomal encapsulation were investigated and the potential possibility of oral administration evaluated. The liposomal agent composed of phospholipid, cholesterol, sodium cholate and isopropyl myristate was prepared using film-dispersion method. A level A in vitro-in vivo correlation (IVIVC) was established for the first time, which demonstrated an excellent IVIVC of both formulated and free capsaicin in oral administration. Physicochemical characterizations including mean particle size, zeta (ζ) potential and average encapsulation efficiency of capsaicin-loaded liposome were found to be 52.2 ± 1.3 nm, -41.5 ± 2.71 mv and 81.9 ± 2.43 %, respectively. In vivo, liposomal encapsulation allowed a 3.34-fold increase in relative bioavailability compared to free capsaicin. The gastric mucosa irritation studies indicated that the liposomal system was a safe carrier for oral administration. These results support the fact that capsaicin, an effective drug for the treatment of neuropathic pain, could be encapsulated in liposome for improved oral bioavailability. The excellent IVIVC of capsaicin-loaded liposome could also be a promising tool in liposomal formulation development with an added advantage of reduced animal testing. PMID:25231341

  14. Intravesical capsaicin in patients with detrusor hyper-reflexia--a placebo-controlled cross-over study

    DEFF Research Database (Denmark)

    Petersen, T; Nielsen, J B; Schrøder, H D

    1999-01-01

    The aim of this study was to determine whether intravesical treatment with capsaicin could block detrusor hyper-reflexia (DH) and alter the substance P content, nerve fibres and mucosa of the bladder. Twelve patients with spinal cord disease with DH and urinary incontinence resistant to anticholi......The aim of this study was to determine whether intravesical treatment with capsaicin could block detrusor hyper-reflexia (DH) and alter the substance P content, nerve fibres and mucosa of the bladder. Twelve patients with spinal cord disease with DH and urinary incontinence resistant...... to anticholinergic treatment underwent intravesical administration of 50 ml 2% lignocaine. followed by either 100 ml 1 mmol/l capsaicin or 100 ml physiological saline for 30 min. Cross-over to the alternative treatment took place after 4 weeks. Varying degrees of burning sensation were experienced by all but one...... patient during the capsaicin treatment and precluded the possibility of conducting studies of this type in a blind manner. No preference for capsaicin treatment was found, and micturition and VAS scores were unchanged after treatment with capsaicin. The mean volume of the contents of the bladder at which...

  15. Effects of capsaicin, green tea and CH-19 sweet pepper on appetite and energy intake in humans in negative and positive energy balance

    DEFF Research Database (Denmark)

    Reinbach, Helene Christine; Møller, P.; Smeets, A.;

    2009-01-01

    Summary Background & aims Bioactive ingredients have been shown to reduce appetite and energy intake. The magnitude of these effects might depend on energy balance why it was investigated how capsaicin, green tea, CH-19 sweet pepper as well as green tea and capsaicin affect appetite and energy...... intake during respectively negative and positive energy balance. Methods 27 subjects were randomized to three weeks of negative and three weeks of positive energy balance during which capsaicin, green tea, CH-19 sweet pepper, capsaicin + green tea or placebo was ingested on ten separate test days while...... the effects on appetite, energy intake, body weight and heart rate were assessed. Results CH-19 sweet pepper and a combination of capsaicin and green tea reduced energy intake during positive energy balance. Capsaicin and green tea suppressed hunger and increased satiety more during negative than during...

  16. Manipulation of culture strategies to enhance capsaicin biosynthesis in suspension and immobilized cell cultures of Capsicum chinense Jacq. cv. Naga King Chili.

    Science.gov (United States)

    Kehie, Mechuselie; Kumaria, Suman; Tandon, Pramod

    2014-06-01

    Manipulation of culture strategies was adopted to study the influence of nutrient stress, pH stress and precursor feeding on the biosynthesis of capsaicin in suspension and immobilized cell cultures of C. chinense. Cells cultured in the absence of one of the four nutrients (ammonium and potassium nitrate for nitrate and potassium stress, potassium dihydrogen orthophosphate for phosphorus stress, and sucrose for sugar stress) influenced the accumulation of capsaicin. Among the stress factors studied, nitrate stress showed maximal capsaicin production on day 20 (505.9 ± 2.8 μg g(-1) f.wt) in immobilized cell, whereas in suspension cultures the maximum accumulation (345.5 ± 2.9 μg g(-1) f.wt) was obtained on day 10. Different pH affected capsaicin accumulation; enhanced accumulation of capsaicin (261.6 ± 3.4 μg g(-1) f.wt) was observed in suspension cultures at pH 6 on day 15, whereas in case of immobilized cultures the highest capsaicin content (433.3 ± 3.3 μg g(-1) f.wt) was obtained at pH 5 on day 10. Addition of capsaicin precursors and intermediates significantly enhanced the biosynthesis of capsaicin, incorporation of vanillin at 100 μM in both suspension and immobilized cell cultures resulted in maximum capsaicin content with 499.1 ± 5.5 μg g(-1) f.wt on day 20 and 1,315.3 ± 10 μg g(-1) f.wt on day 10, respectively. Among the different culture strategies adopted to enhance capsaicin biosynthesis in cell cultures of C. chinense, cells fed with vanillin resulted in the maximum capsaicin accumulation. The rate of capsaicin production was significantly higher in immobilized cells as compared to freely suspended cells. PMID:24141419

  17. Manipulation of culture strategies to enhance capsaicin biosynthesis in suspension and immobilized cell cultures of Capsicum chinense Jacq. cv. Naga King Chili.

    Science.gov (United States)

    Kehie, Mechuselie; Kumaria, Suman; Tandon, Pramod

    2014-06-01

    Manipulation of culture strategies was adopted to study the influence of nutrient stress, pH stress and precursor feeding on the biosynthesis of capsaicin in suspension and immobilized cell cultures of C. chinense. Cells cultured in the absence of one of the four nutrients (ammonium and potassium nitrate for nitrate and potassium stress, potassium dihydrogen orthophosphate for phosphorus stress, and sucrose for sugar stress) influenced the accumulation of capsaicin. Among the stress factors studied, nitrate stress showed maximal capsaicin production on day 20 (505.9 ± 2.8 μg g(-1) f.wt) in immobilized cell, whereas in suspension cultures the maximum accumulation (345.5 ± 2.9 μg g(-1) f.wt) was obtained on day 10. Different pH affected capsaicin accumulation; enhanced accumulation of capsaicin (261.6 ± 3.4 μg g(-1) f.wt) was observed in suspension cultures at pH 6 on day 15, whereas in case of immobilized cultures the highest capsaicin content (433.3 ± 3.3 μg g(-1) f.wt) was obtained at pH 5 on day 10. Addition of capsaicin precursors and intermediates significantly enhanced the biosynthesis of capsaicin, incorporation of vanillin at 100 μM in both suspension and immobilized cell cultures resulted in maximum capsaicin content with 499.1 ± 5.5 μg g(-1) f.wt on day 20 and 1,315.3 ± 10 μg g(-1) f.wt on day 10, respectively. Among the different culture strategies adopted to enhance capsaicin biosynthesis in cell cultures of C. chinense, cells fed with vanillin resulted in the maximum capsaicin accumulation. The rate of capsaicin production was significantly higher in immobilized cells as compared to freely suspended cells.

  18. Transient activation of specific neurons in mice by selective expression of the capsaicin receptor

    Science.gov (United States)

    Güler, Ali D.; Rainwater, Aundrea; Parker, Jones G.; Jones, Graham L.; Argilli, Emanuela; Arenkiel, Benjamin R.; Ehlers, Michael D.; Bonci, Antonello; Zweifel, Larry s.; Palmiter, Richard D.

    2013-01-01

    The ability to control the electrical activity of a neuronal subtype is a valuable tool in deciphering the role of discreet cell populations in complex neural circuits. Recent techniques that allow remote control of neurons are either labor intensive and invasive or indirectly coupled to neural electrical potential with low temporal resolution. Here we show the rapid, reversible and direct activation of genetically identified neuronal subpopulations by generating two inducible transgenic mouse models. Confined expression of the capsaicin receptor, TRPV1, allows cell-specific activation after peripheral or oral delivery of ligand in freely moving mice. Capsaicin-induced activation of dopaminergic or serotonergic neurons reversibly alters both physiological and behavioural responses within minutes, and lasts ~10 min. These models showcase a robust and remotely controllable genetic tool that modulates a distinct cell population without the need for invasive and labour-intensive approaches. PMID:22434189

  19. Capsaicin failed in suppressing cortical processing of CO2 laser pain in migraine patients.

    Science.gov (United States)

    de Tommaso, Marina; Losito, Luciana; Difruscolo, Olimpia; Sardaro, Michele; Libro, Giuseppe; Guido, Marco; Lamberti, Paolo; Livrea, Paolo

    The aim of this study was to compare the properties of the nociceptive system in eight migraine without aura patients in the pain-free phase with 10 healthy controls, by evaluating the topography and the source of the CO2 laser-evoked potentials (LEPs) obtained by the right supraorbital skin, during and after capsaicin topical application. In healthy subjects the acute cutaneous pain induced by capsaicin reduced the amplitude of the vertex LEPs and induced a posterior shifting of the P2 wave dipolar source within the anterior cingulate cortex. These functional changes seemed significantly reduced in migraine patients, for a disturbed pattern of pain modulation at the cortical level, which may subtend the onset and persistence of migraine.

  20. A capsaicin (8%) patch in the treatment of severe persistent inguinal postherniorrhaphy pain

    DEFF Research Database (Denmark)

    Bischoff, Joakim M; Ringsted, Thomas K; Petersen, Marian;

    2014-01-01

    patch application, but the pain reduction was not significant (NRS, mean difference [95% CI]: 5.0 [0.09 to 9.9]; P = 0.046). No differences in SPID between treatments were observed at 2 and 3 months after patch application. Changes in IENFD on the pain side, from baseline to 1 month after patch...... application, did not differ between capsaicin and placebo treatment: 1.9 [-0.1 to 3.9] and 0.6 [-1.2 to 2.5] fibers/mm, respectively (P = 0.32). No significant changes in sensory function, sleep quality or psychological factors were associated with capsaicin patch treatment. CONCLUSIONS: The study did...

  1. Displaying gray shades in liquid crystal displays

    Indian Academy of Sciences (India)

    T N Ruckmongathan

    2003-08-01

    Quality of image in a display depends on the contrast, colour, resolution and the number of gray shades. A large number of gray shades is necessary to display images without any contour lines. These contours are due to limited number of gray shades in the display causing abrupt changes in grayness of the image, while the original image has a gradual change in brightness. Amplitude modulation has the capability to display a large number of gray shades with minimum number of time intervals [1,2]. This paper will cover the underlying principle of amplitude modulation, some variants and its extension to multi-line addressing. Other techniques for displaying gray shades in passive matrix displays are reviewed for the sake of comparison.

  2. Prostaglandin I2 enhances cough reflex sensitivity to capsaicin in the asthmatic airway

    OpenAIRE

    Ishiura, Yoshihisa; Fujimura, Masaki; Nobata, Kouichi; Oribe, Yoshitaka; Abo, Miki; Myou, Shigeharu

    2007-01-01

    Inflammatory mediators are involved in the pathogenesis of airway inflammation, but the role of prostaglandin I2 (PGI2) remains obscure. This study was designed to investigate the role of PGI2 in cough reflex sensitivity of the asthmatic airway, which is characterized by chronic eosinophilic airway inflammation. The effect of beraprost, a chemically and biologically stable analogue of PGI2, on cough response to inhaled capsaicin was examined in 21 patients with stable asthma in a randomized, ...

  3. In vivo and in vitro content of capsaicin in pepper(Capsicum annuum L.)

    OpenAIRE

    Koleva Gudeva, Liljana; Spasenoski, Mirko; Rafajlovska, Vesna

    2004-01-01

    From all groups of biological active-secondary metabolites, in the species of genus Capsicum the most importance have the alkaloids capsaicinoides, which are present only in the cultivars of genus Capsicum, and only they are responsible for the pungent of pepper. From all capsaicinoides only two compounds with 80-90% are responsible for the pungent of papper, and they are capsaicin and dihidrocapsaicin.

  4. The effects of Hot Pepper Extract and Capsaicin on Adipocyte Metabolism

    OpenAIRE

    Ching Sheng, Chu; Ki Rok, Kwon; Tae Jin, Rhim; Dong Heui, Kim

    2008-01-01

    Objectives : The purpose of this study is to investigate the effects of hot pepper extract and capsaicin on the adipogenesis in 3T3-L1 cells, lipolysis in rat epididymal adipocytes and histological changes in porcine adipose tissue. Methods : Inhibiton of preadipocyte differentiation and/or stimulation of lipolysis play important roles in reducing obesity. 3T3-L1 preadipocytes were differentiated with adipogenic reagents by incubating for 3 days in the absence or presence of hot pepper ...

  5. Cardiovascular effects of substance P and capsaicin microinjected into the nucleus tractus solitarii of the rat

    OpenAIRE

    Lukovic, L.; Jong, Wybren de; Wied, D. de

    1987-01-01

    This report deals with the effect of substance P (SP) and capsaicin on blood pressure and heart rate after administration into different sites of the nucleus tractus solitarii (NTS) of urethane-anesthetized rats. Microinjection of SP at 6 different coordinates throughout the NTS showed 3 sites where SP administration evoked changes in blood pressure and heart rate. The most sensitive sites where application of SP into the NTS evoked dose-dependent hypotension and bradycardia were at the level...

  6. Capsaicin treatment differentially affects feeding suppression by bombesin-like peptides

    OpenAIRE

    Ladenheim, Ellen E; Knipp, Susan

    2007-01-01

    Peripheral administration of bombesin (BN) and the related mammalian peptides, gastrin-releasing peptide (GRP) and neuromedin B (NMB), suppress food intake in rats. To examine whether all BN-like peptides utilize the same neural pathways to reduce feeding, rats were treated on postnatal day 2 with the injection vehicle or capsaicin, a neurotoxin that damages a subset of visceral afferent fibers. When rats reached adulthood, we compared the ability of a dose range of systemically administered ...

  7. Cough sensitivity and extrathoracic airway responsiveness to inhaled capsaicin in chronic cough patients.

    OpenAIRE

    Cho, You Sook; Lee, Chang-Keun; Yoo, Bin; Moon, Hee-Bom

    2002-01-01

    Enhanced cough response has been frequently observed in chronic cough. Recently, extrathoracic airway constriction to inhaled histamine was demonstrated in some chronic cough patients. However, relation between extrathoracic airway hyperresponsiveness (EAHR) and cough sensitivity determined by capsaicin inhalation is unclear in each etiological entity of chronic cough. Seventy-seven patients, with dry cough persisting for 3 or more weeks, normal spirometry and chest radiography, and 15 contro...

  8. A Bivalent Tarantula Toxin Activates the Capsaicin Receptor, TRPV1, by Targeting the Outer Pore Domain

    OpenAIRE

    Bohlen, Christopher J.; Priel, Avi; Zhou, Sharleen; King, David; Siemens, Jan; Julius, David

    2010-01-01

    Toxins have evolved to target regions of membrane ion channels that underlie ligand binding, gating, or ion permeation, and have thus served as invaluable tools for probing channel structure and function. Here we describe a peptide toxin from the Earth Tiger tarantula that selectively and irreversibly activates the capsaicin- and heat-sensitive channel, TRPV1. This high avidity interaction derives from a unique tandem repeat structure of the toxin that endows it with an antibody-like bivalenc...

  9. Effects of action of ultrasound with capsaicin in the treatment of post traumatic pathology

    Directory of Open Access Journals (Sweden)

    Ioan OSWALD

    2007-05-01

    Full Text Available There are numerous methods of administering drugs to the body,both passive and active. A recent review of the literature on phonophoresis reports that 75 % of the studies reviewed reported positive effects, ultrasound energy with drugs like gel or cream can travel through body tissue. Capsaicin was the active ingredient in hot chilli peppers has selection actions on unmyelinated C fibres and thinly myelinated A primary sensory neurones.

  10. Antiobese effects of capsaicin-chitosan microsphere (CCMS) in obese rats induced by high fat diet.

    Science.gov (United States)

    Tan, Sirong; Gao, Bing; Tao, Yi; Guo, Jiao; Su, Zheng-quan

    2014-02-26

    Chitosan (CTS) and capsaicin (CAP) are two kinds of effective ingredients for antiobesity, which are extracted from crab shells and Capsicum annuum. However, the strong taste of CAP makes it difficult to consume, and the antiobesity ability of CTS is limited. In this study, we prepared capsaicin-chitosan microspheres (CCMSs) by ion-cross-linking and spray drying and examined the antiobesity ability of CCMSs in obese rats. The effects of CCMSs on body weight, Lee's index, body fat, and serum lipids were investigated. The mRNA expression of PPARα, PPARγ, leptin, UCP2, GPR120, FTO, and adiponectin in the liver was determined by quantitative real-time PCR, and the protein expression of adiponectin, leptin, PPARα, UCP2, and hepatic lipase in serum was evaluated by enzyme-linked immunosorbent assay. CCMSs were prepared with 85.17% entrapment efficiency and 8.87% mean drug loading. Compared with chitosan microspheres, CAP, and Orlistat, the CCMSs showed better ability to control body weight, body mass index, organ index, body fat, proportion of fat to body weight, and serum lipids. The CCMSs upregulated the expressions of PPARα, PPARγ, UCP2, and adiponectin and downregulated the expression of leptin. CCMSs may thus be considered novel, safe, effective, and natural weight loss substances, and there is an additive effect between CTMS and capsaicin.

  11. Resiniferatoxin and piperine: capsaicin-like stimulators of oxygen uptake in the perfused rat hindlimb.

    Science.gov (United States)

    Eldershaw, T P; Colquhoun, E Q; Bennett, K L; Dora, K A; Clark, M G

    1994-01-01

    The naturally occurring capsaicin-like molecules, resiniferatoxin (RTX, Euphorbia spp.) and piperine (Piper nigrum), each stimulated oxygen uptake (VO2) in association with increased vascular resistance in a concentration-dependent manner when infused into the perfused rat hindlimb. 5 microM glyceryl trinitrate (GTN, a nitrovasodilator) significantly blocked the oxygen and pressure responses to both RTX and piperine, indicating a close relationship between changes in VO2 and the vasoconstriction. Concentrations greater than those required for maximal VO2 resulted in an inhibition of VO2, although perfusion pressure continued to increase. Time course studies showed that both RTX and piperine at high doses resulted in a tri-phasic response. An initial phase of transient VO2 stimulation was followed by a second phase of inhibition. A third phase involving an often larger but transient stimulation of VO2 followed removal of the agents and continued after the pressure returned to basal. The actions of RTX and piperine were similar to those of other active capsaicin-like molecules tested previously in this system, including capsaicinoids (Capsicum spp.), gingerols (Zingiber officinale), and shogoals (Zingiber officinale). RTX was the most potent, and piperine the least potent of this series. Although receptor involvement has yet to be unequivocally established, the data are consistent with the presence of a functional capsaicin-like (vanilloid) receptor in the vasculature of the rat hindlimb that mediates vasoconstriction and oxygen uptake. These findings may have implications for the future development of thermogenic agents. PMID:8035653

  12. Invisible Display in Aluminum

    DEFF Research Database (Denmark)

    Prichystal, Jan Phuklin; Hansen, Hans Nørgaard; Bladt, Henrik Henriksen

    2005-01-01

    Bang & Olufsen a/s has been working with ideas for invisible integration of displays in metal surfaces. Invisible integration of information displays traditionally has been possible by placing displays behind transparent or semitransparent materials such as plastic or glass. The wish...... for an integrated display in a metal surface is often ruled by design and functionality of a product. The integration of displays in metal surfaces requires metal removal in order to clear the area of the display to some extent. The idea behind an invisible display in Aluminum concerns the processing of a metal...

  13. Costs and benefits of capsaicin-mediated control of gut retention in dispersers of wild chilies.

    Science.gov (United States)

    Tewksbury, Joshua J; Levey, Douglas J; Huizinga, Meribeth; Haak, David C; Traveset, Anna

    2008-01-01

    A fundamental way in which animal-dispersed plants can influence the viability and distribution of dispersed seeds is through control of retention time in the guts of dispersers. Using two species of wild chilies and their dispersers, we examined how chemical and physical properties of fruits and seeds mediate this interaction. Capsicum chacoense is polymorphic for pungency, occurs in Bolivia, and is dispersed mostly by elaenias. Capsicum annuum is not polymorphic, occurs in Arizona (USA), and is dispersed mostly by thrashers. We first tested whether capsaicin, the substance responsible for the pungency of chilies, affects gut retention time of seeds in primary dispersers. Capsaicin slowed gut passage of seeds but did so in a manner that differed greatly between bird species because the constipative effects of capsaicin occurred only after an 80-minute time lag. Elaenias in Bolivia held only 6% of C. chacoense seeds for > 80 minutes, whereas thrashers in Arizona held 78% of C. annuum seeds for > 80 minutes. Next we examined the effects of retention time on seed viability and germination. Increased retention resulted in a greater proportion of seeds germinating in C. annuum, had no effects on non-pungent C. chacoense, and had negative effects on pungent C. chacoense. These divergent effects are explained by differences in seed coat morphology: seed coats of pungent C. chacoense are 10-12% thinner than those of the other two types of seeds. Thus, longer retention times damaged seeds with the thinnest seed coats. In C. annuum, seed viability remained high regardless of retention time, but germination increased with retention, suggesting a role for scarification. Thus, in C. annuum, fruit chemistry appears well matched with seed morphology and disperser physiology: capsaicin extends gut retention for most seeds, resulting in greater seed scarification and higher germination rates. Increased retention of pungent C. chacoense seeds is detrimental, but because the primary

  14. The effects of pregabalin and the glial attenuator minocycline on the response to intradermal capsaicin in patients with unilateral sciatica.

    Directory of Open Access Journals (Sweden)

    Nicole M Sumracki

    Full Text Available BACKGROUND: Patients with unilateral sciatica have heightened responses to intradermal capsaicin compared to pain-free volunteers. No studies have investigated whether this pain model can screen for novel anti-neuropathic agents in patients with pre-existing neuropathic pain syndromes. AIM: This study compared the effects of pregabalin (300 mg and the tetracycline antibiotic and glial attenuator minocycline (400 mg on capsaicin-induced spontaneous pain, flare, allodynia and hyperalgesia in patients with unilateral sciatica on both their affected and unaffected leg. METHODS/RESULTS: Eighteen patients with unilateral sciatica completed this randomised, double-blind, placebo-controlled, three-way cross-over study. Participants received a 10 µg dose of capsaicin into the middle section of their calf on both their affected and unaffected leg, separated by an interval of 75 min. Capsaicin-induced spontaneous pain, flare, allodynia and hyperalgesia were recorded pre-injection and at 5, 20, 40, 60 and 90 min post-injection. Minocycline tended to reduce pre-capsaicin injection values of hyperalgesia in the affected leg by 28% (95% CI 0% to 56%. The area under the effect time curves for capsaicin-induced spontaneous pain, flare, allodynia and hyperalgesia were not affected by either treatment compared to placebo. Significant limb differences were observed for flare (AUC (-38% in affected leg, 95% CI for difference -19% to -52%. Both hand dominance and sex were significant covariates of response to capsaicin. CONCLUSIONS: It cannot be concluded that minocycline is unsuitable for further evaluation as an anti-neuropathic pain drug as pregabalin, our positive control, failed to reduce capsaicin-induced neuropathic pain. However, the anti-hyperalgesic effect of minocycline observed pre-capsaicin injection is promising pilot information to support ongoing research into glial-mediated treatments for neuropathic pain. The differences in flare response between

  15. Spatial Distribution of the Cannabinoid Type 1 and Capsaicin Receptors May Contribute to the Complexity of Their Crosstalk

    Science.gov (United States)

    Chen, Jie; Varga, Angelika; Selvarajah, Srikumaran; Jenes, Agnes; Dienes, Beatrix; Sousa-Valente, Joao; Kulik, Akos; Veress, Gabor; Brain, Susan D.; Baker, David; Urban, Laszlo; Mackie, Ken; Nagy, Istvan

    2016-01-01

    The cannabinoid type 1 (CB1) receptor and the capsaicin receptor (TRPV1) exhibit co-expression and complex, but largely unknown, functional interactions in a sub-population of primary sensory neurons (PSN). We report that PSN co-expressing CB1 receptor and TRPV1 form two distinct sub-populations based on their pharmacological properties, which could be due to the distribution pattern of the two receptors. Pharmacologically, neurons respond either only to capsaicin (COR neurons) or to both capsaicin and the endogenous TRPV1 and CB1 receptor ligand anandamide (ACR neurons). Blocking or deleting the CB1 receptor only reduces both anandamide- and capsaicin-evoked responses in ACR neurons. Deleting the CB1 receptor also reduces the proportion of ACR neurons without any effect on the overall number of capsaicin-responding cells. Regarding the distribution pattern of the two receptors, neurons express CB1 and TRPV1 receptors either isolated in low densities or in close proximity with medium/high densities. We suggest that spatial distribution of the CB1 receptor and TRPV1 contributes to the complexity of their functional interaction. PMID:27653550

  16. Discovery of putative capsaicin biosynthetic genes by RNA-Seq and digital gene expression analysis of pepper

    Science.gov (United States)

    Zhang, Zi-Xin; Zhao, Shu-Niu; Liu, Gao-Feng; Huang, Zu-Mei; Cao, Zhen-Mu; Cheng, Shan-Han; Lin, Shi-Sen

    2016-01-01

    The Indian pepper ‘Guijiangwang’ (Capsicum frutescens L.), one of the world’s hottest chili peppers, is rich in capsaicinoids. The accumulation of the alkaloid capsaicin and its analogs in the epidermal cells of the placenta contribute to the pungency of Capsicum fruits. To identify putative genes involved in capsaicin biosynthesis, RNA-Seq was used to analyze the pepper’s expression profiles over five developmental stages. Five cDNA libraries were constructed from the total RNA of placental tissue and sequenced using an Illumina HiSeq 2000. More than 19 million clean reads were obtained from each library, and greater than 50% of the reads were assignable to reference genes. Digital gene expression (DGE) profile analysis using Solexa sequencing was performed at five fruit developmental stages and resulted in the identification of 135 genes of known function; their expression patterns were compared to the capsaicin accumulation pattern. Ten genes of known function were identified as most likely to be involved in regulating capsaicin synthesis. Additionally, 20 new candidate genes were identified related to capsaicin synthesis. We use a combination of RNA-Seq and DGE analyses to contribute to the understanding of the biosynthetic regulatory mechanism(s) of secondary metabolites in a nonmodel plant and to identify candidate enzyme-encoding genes. PMID:27756914

  17. Handbook of display technology

    CERN Document Server

    Castellano, Joseph A

    1992-01-01

    This book presents a comprehensive review of technical and commercial aspects of display technology. It provides design engineers with the information needed to select proper technology for new products. The book focuses on flat, thin displays such as light-emitting diodes, plasma display panels, and liquid crystal displays, but it also includes material on cathode ray tubes. Displays include a large number of products from televisions, auto dashboards, radios, and household appliances, to gasoline pumps, heart monitors, microwave ovens, and more.For more information on display tech

  18. Capsaicin sensitizes TRAIL-induced apoptosis through Sp1-mediated DR5 up-regulation: Involvement of Ca{sup 2+} influx

    Energy Technology Data Exchange (ETDEWEB)

    Moon, Dong-Oh [Department of Biology Education, Daegu University, Gyungsan, Gyeongbuk 712–714 (Korea, Republic of); Kang, Chang-Hee; Kang, Sang-Hyuck [Department of Marine Life Sciences, Jeju National University, Jeju 690–756 (Korea, Republic of); Choi, Yung-Hyun [Department of Biochemistry, College of Oriental Medicine, Dongeui University, Busan 614–054 (Korea, Republic of); Hyun, Jin-Won; Chang, Weon-Young; Kang, Hee-Kyoung; Koh, Young-Sang; Maeng, Young-Hee; Kim, Young-Ree [School of Medicine, Jeju National University, Jeju-si 690–756 (Korea, Republic of); Kim, Gi-Young, E-mail: immunkim@jejunu.ac.kr [Department of Marine Life Sciences, Jeju National University, Jeju 690–756 (Korea, Republic of)

    2012-02-15

    Although tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) induces apoptosis in various malignant cells, several cancers including human hepatocellular carcinoma (HCC) exhibit potent resistance to TRAIL-induced cell death. The aim of this study is to evaluate the anti-cancer potential of capsaicin in TRAIL-induced cancer cell death. As indicated by assays that measure phosphatidylserine exposure, mitochondrial activity and activation of caspases, capsaicin potentiated TRAIL-resistant cells to lead to cell death. In addition, we found that capsaicin induces the cell surface expression of TRAIL receptor DR5, but not DR4 through the activation Sp1 on its promoter region. Furthermore, we investigated that capsaicin-induced DR5 expression and apoptosis are inhibited by calcium chelator or inhibitors for calmodulin-dependent protein kinase. Taken together, our data suggest that capsaicin sensitizes TRAIL-mediated HCC cell apoptosis by DR5 up-regulation via calcium influx-dependent Sp1 activation. Highlights: ► Capsaicin sensitizes TRAIL-induced apoptosis through activation of caspases. ► Capsaicin induces expression of DR5 through Sp1 activation. ► Capsaicin activates calcium signaling pathway.

  19. Lunar Sample Display Locations

    Data.gov (United States)

    National Aeronautics and Space Administration — NASA provides a number of lunar samples for display at museums, planetariums, and scientific expositions around the world. Lunar displays are open to the public....

  20. A Compressive Superresolution Display

    KAUST Repository

    Heide, Felix

    2014-06-22

    In this paper, we introduce a new compressive display architecture for superresolution image presentation that exploits co-design of the optical device configuration and compressive computation. Our display allows for superresolution, HDR, or glasses-free 3D presentation.

  1. Management of Pervasive Displays

    OpenAIRE

    Tatiraju, Venkata

    2015-01-01

    Traditional signage is being replaced by digital displays that are directly connected to the Internet and show content from the cloud. These displays increasingly rely on a standard web-browser and HTML5 technologies for rendering rich media content. As the number of these displays increase, it is critical to provide user-friendly and efficient solutions for managing them remotely from the cloud. The remote management of such displays traditionally relies on proprietary native software soluti...

  2. Liquid crystal display

    International Nuclear Information System (INIS)

    An improved liquid crystal display device is described which can display letters, numerals and other necessary patterns in the night time using a minimized amount of radioactive material. To achieve this a self-luminous light source is placed in a limited region corresponding to a specific display area. (U.K.)

  3. The capsaicin receptor participates in artificial sweetener aversion.

    Science.gov (United States)

    Riera, Céline E; Vogel, Horst; Simon, Sidney A; Damak, Sami; le Coutre, Johannes

    2008-11-28

    Artificial sweeteners such as saccharin, aspartame, acesulfame-K, and cyclamate produce at high concentrations an unpleasant after-taste that is generally attributed to bitter and metallic taste sensations. To identify receptors involved with the complex perception of the above compounds, preference tests were performed in wild-type mice and mice lacking the TRPV1 channel or the T1R3 receptor, the latter being necessary for the perception of sweet taste. The sweeteners, including cyclamate, displayed a biphasic response profile, with the T1R3 mediated component implicated in preference. At high concentrations imparting off-taste, omission of TRPV1 reduced aversion. In a heterologous expression system the Y511A point mutation in the vanilloid pocket of TRPV1 did not affect saccharin and aspartame responses but abolished cyclamate and acesulfame-K activities. The results rationalize artificial sweetener tastes and off-tastes by showing that at low concentrations, these molecules stimulate the gustatory system through the hedonically positive T1R3 pathway, and at higher concentrations, their aversion is partly mediated by TRPV1. PMID:18804451

  4. A randomized, double-blind, placebo-controlled trial of injected capsaicin for pain in Morton's neuroma.

    Science.gov (United States)

    Campbell, Claudia M; Diamond, Eric; Schmidt, William K; Kelly, Margaret; Allen, Robert; Houghton, William; Brady, Kerrie L; Campbell, James N

    2016-06-01

    Intermetatarsal neuroma or Morton's neuroma is a painful condition of the foot resulting from an entrapment of the common digital nerve typically in the third intermetatarsal space. The pain can be severe and especially problematic with walking. Treatment options are limited and surgery may lead to permanent numbness in the toes. Capsaicin, the pungent ingredient of hot peppers, produces analgesia by inducing retraction of nociceptive afferents from the area of innervation and is effective in treating certain neuropathic pain disorders. A randomized double-blind placebo-controlled study was conducted to test the efficacy, tolerability, and safety of a single 0.1 mg dose of capsaicin vs placebo injected into the region of the neuroma. A total of 58 subjects diagnosed with Morton's neuroma with foot pain ≥4 (0-10 numerical pain rating scale) were injected with 2 mL of lidocaine into the intermetatarsal space proximal to the neuroma to provide local anesthesia. After 5 minutes, 0.1 mg capsaicin or placebo was injected into the intermetatarsal space containing the painful neuroma. Average foot pain was rated for 2 weeks before through 4 weeks after injection. At weeks 1 and 4, the decrease in pain was significantly greater in the subjects treated with capsaicin (P = 0.021 and P = 0.019, respectively). A trend toward significance was noted at weeks 2 and 3. Improvements in functional interference scores and reductions in oral analgesic use were also seen in the capsaicin-treated group. These findings suggest that injection of capsaicin is an efficacious treatment option for patients with painful intermetatarsal neuroma. PMID:26963851

  5. Capsaicin effects on blinking Efectos de la capsaicina en el parpadeo

    Directory of Open Access Journals (Sweden)

    Fidias E. Leon-Sarmiento

    2005-09-01

    Full Text Available Blinking is a normal human phenomenom involving trigeminal and facial patways. To gain understanding on the neurobiology of blinking, five normal subjects were investigated before and after application of transdermal capsaicin at the forehead for two weeks. No effects of topical capsaicin were detected in eye blink rates. However, when capsaicin was applied to a female subject with blepharospasm, she showed a dramatic restoration of her vision subsequent to blinking modification. Deactivation of abnormal A-to-C fibers cross talks at the trigeminal-facial pathways seems to be the most likely mechanism of such improvement.El parpadeo es un fenómeno normal en los humanos que involucra las vías trigéminas faciales. Con el fin de conocer un poco más la neurobiología de este fenómeno estudiamos cinco individuos normales antes y después de aplicar capsaicina trasdérmica en la frente de cada uno de ellos, por dos semanas. La frecuencia de parpadeo no se alteró con la aplicación de capsaicina tópica. Sin embargo, cuando la misma sustancia se aplicó a una paciente con blefaroespasmo hubo dramática restauración de su visión, la cual fue secundaria a la modificación de la actividad muscular palpebral. La desactivación del cruce patológico de información que pasa de las fibras A a las fibras C, pertenecientes a las vías trigémino-faciales, parece ser el mecanismo de acción relacionado con la aplicación de capsaicina, el que estaría directamente relacionado con la recuperación clínica observada en la paciente con blefaroespasmo.

  6. The Effect of Capsaicin-Containing Food on the Swallowing Response.

    Science.gov (United States)

    Shin, Satoko; Shutoh, Nobumichi; Tonai, Miho; Ogata, Naoko

    2016-04-01

    The purpose of this study was to determine the effect of regular ingestion of capsaicin-containing food that is easily available in everyday life on the latency of the swallowing response (LSR). Pickled Napa cabbage was selected as the food for the present study. One portion (10 g) of pickled Napa cabbage provides 1.5 µg of capsaicin. Participants ingested pickled Napa cabbage (10 g) before every meal for 20 days (days 1-20). LSR was measured pre-intervention (day 0) and post-intervention (day 21). The participants then followed their regular diet, without foods containing red pepper, from day 21 to day 27, and LSR was measured on day 28 (follow-up LSR). Sixteen elderly participants (two male, 14 female; age 81.6 ± 9.39 years) and 10 young participants (all female; age 21.6 ± 0.52 years) participated in the study. The pre-intervention LSR was 2.04 ± 1.60 s in elderly participants and 1.27 ± 0.27 s in young participants. In the elderly group, the post-intervention LSR (day 21) was 1.47 ± 1.05  the follow-up LSR (day 28) was 1.99 ± 1.80 s (p = 0.044 and 0.502, respectively, compared to pre-intervention). In the young group, the post-intervention and follow-up LSR values were 1.07 ± 0.20 s and 1.04 ± 0.10 s, respectively (p = 0.016 and 0.038, respectively, compared to pre-intervention). Swallowing function was improved by pickled Napa cabbage containing capsaicin, but capsaicin supplementation may need to be maintained to have an ongoing effect.

  7. Acute effects of capsaicin on energy expenditure and fat oxidation in negative energy balance.

    Directory of Open Access Journals (Sweden)

    Pilou L H R Janssens

    Full Text Available BACKGROUND: Addition of capsaicin (CAPS to the diet has been shown to increase energy expenditure; therefore capsaicin is an interesting target for anti-obesity therapy. AIM: We investigated the 24 h effects of CAPS on energy expenditure, substrate oxidation and blood pressure during 25% negative energy balance. METHODS: Subjects underwent four 36 h sessions in a respiration chamber for measurements of energy expenditure, substrate oxidation and blood pressure. They received 100% or 75% of their daily energy requirements in the conditions '100%CAPS', '100%Control', '75%CAPS' and '75%Control'. CAPS was given at a dose of 2.56 mg (1.03 g of red chili pepper, 39,050 Scoville heat units (SHU with every meal. RESULTS: An induced negative energy balance of 25% was effectively a 20.5% negative energy balance due to adapting mechanisms. Diet-induced thermogenesis (DIT and resting energy expenditure (REE at 75%CAPS did not differ from DIT and REE at 100%Control, while at 75%Control these tended to be or were lower than at 100%Control (p = 0.05 and p = 0.02 respectively. Sleeping metabolic rate (SMR at 75%CAPS did not differ from SMR at 100%CAPS, while SMR at 75%Control was lower than at 100%CAPS (p = 0.04. Fat oxidation at 75%CAPS was higher than at 100%Control (p = 0.03, while with 75%Control it did not differ from 100%Control. Respiratory quotient (RQ was more decreased at 75%CAPS (p = 0.04 than at 75%Control (p = 0.05 when compared with 100%Control. Blood pressure did not differ between the four conditions. CONCLUSION: In an effectively 20.5% negative energy balance, consumption of 2.56 mg capsaicin per meal supports negative energy balance by counteracting the unfavorable negative energy balance effect of decrease in components of energy expenditure. Moreover, consumption of 2.56 mg capsaicin per meal promotes fat oxidation in negative energy balance and does not increase blood pressure significantly. TRIAL REGISTRATION

  8. Small-fibre neuropathy in female Fabry patients: reduced allodynia and skin blood flow after topical capsaicin

    DEFF Research Database (Denmark)

    Møller, Anette Torvin; Feldt-Rasmussen, Ulla; Rasmussen, Åse K.;

    2006-01-01

    . The response to capsaicin was evaluated by laser Doppler imaging. We found that the female Fabry patients had a significantly smaller increase in blood flow (p = 0.0003) after capsaicin application. The area of static mechanical allodynia and dynamic mechanical hyperalgesia was also significantly smaller (p...... = 0.006) in female Fabry patients. This indicates that female Fabry patients have a significant loss of small-fibre function and demonstrates that it is possible to evaluate this by a non-invasive method....

  9. [Aural Stimulation with Capsaicin Ointment Improved the Swallowing Function in Patients with Dysphagia: Evaluation by the SMRC Scale].

    Science.gov (United States)

    Kondo, Eiji; Jinnouchi, Osamu; Ohnishi, Hiroki; Kawata, Ikuji; Takeda, Noriaki

    2015-11-01

    Cough and swallowing reflexes are important airway-protective mechanisms against aspiration. Angiotensin-converting enzyme (ACE) inhibitors, one of the side effects of which is cough, have been reported to reduce the incidence of aspiration pneumonia in hypertensive patients with stroke. ACE inhibitors have also been reported to improve the swallowing function in post-stroke patients. On the other hand, stimulation of the Arnold nerve, the auricular branch of the vagus, triggers the cough reflex (Arnold's ear-cough reflex). Capsaicin, an agonist of Transient Receptor Potential Vanilloid 1 (TRPV1), has been shown to activate the peripheral sensory C-fibers. Stimulation of the sensory branches of the vagus in the laryngotracheal mucosa with capsaicin induces the cough reflex and has been reported to improve the swallowing function in patients with dysphagia. In our previous study, we showed that aural stimulation of the Arnold nerve with 0.025% capsaicin ointment improved the swallowing function, as evaluated by the endoscopic swallowing score, in 26 patients with dysphagia. In the present study, the video images of swallowing recorded in the previous study were re-evaluated using the SMRC scale by an independent otolaryngologist who was blinded to the information about the patients and the endoscopic swallowing score. The SMRC scale is used to evaluate four aspects of the swallowing function: 1) Sensory: the initiation of the swallowing reflex as assessed by the white-out timing; 2) Motion: the ability to hold blue-dyed water in the oral cavity and induce laryngeal elevation; 3) Reflex: glottal closure and the cough reflex induced by touching the epiglottis or arytenoid with the endoscope; 4) Clearance: pharyngeal clearance of the blue-dyed water after swallowing. Accordingly, we demonstrated that a single application of capsaicin ointment to the external auditory canal of patients with dysphagia significantly improved the R, but not the S, M or C scores, and this

  10. Polyplanar optic display

    Energy Technology Data Exchange (ETDEWEB)

    Veligdan, J.; Biscardi, C.; Brewster, C.; DeSanto, L. [Brookhaven National Lab., Upton, NY (United States). Dept. of Advanced Technology; Beiser, L. [Leo Beiser Inc., Flushing, NY (United States)

    1997-07-01

    The Polyplanar Optical Display (POD) is a unique display screen which can be used with any projection source. This display screen is 2 inches thick and has a matte black face which allows for high contrast images. The prototype being developed is a form, fit and functional replacement display for the B-52 aircraft which uses a monochrome ten-inch display. The new display uses a 100 milliwatt green solid state laser (532 nm) as its optical source. In order to produce real-time video, the laser light is being modulated by a Digital Light Processing (DLP{trademark}) chip manufactured by Texas Instruments, Inc. A variable astigmatic focusing system is used to produce a stigmatic image on the viewing face of the POD. In addition to the optical design, the authors discuss the electronic interfacing to the DLP{trademark} chip, the opto-mechanical design and viewing angle characteristics.

  11. Scalable Resolution Display Walls

    KAUST Repository

    Leigh, Jason

    2013-01-01

    This article will describe the progress since 2000 on research and development in 2-D and 3-D scalable resolution display walls that are built from tiling individual lower resolution flat panel displays. The article will describe approaches and trends in display hardware construction, middleware architecture, and user-interaction design. The article will also highlight examples of use cases and the benefits the technology has brought to their respective disciplines. © 1963-2012 IEEE.

  12. Infringement of the barriers of cancer via dietary phytoconstituents capsaicin through novel drug delivery system.

    Science.gov (United States)

    Giri, Tapan Kumar; Alexander, Amit; Ajazuddin; Barman, Tapan Kumar; Maity, Subhasis

    2016-01-01

    Cancer is the major cause of fatality and the number of new cases is increasing incessantly. Conventional therapies and existing anticancer agents cause serious side effects and expand the patient's lifespan by a few years. There is the need to exploit alternative anticancer agents and novel drug delivery system to deliver these agents to the tumor site for the prevention of cancer. Recently, biologically active compounds isolated from plants used for the management of cancer have been the heart of interest. Capsaicin is a major pungent agent present in the chili peppers that is heavily consumed in the world. Capsaicin has demonstrated effectiveness as an anticancer agent, but a restraining factor is its pungency, extremely low aqueous solubility, and poor oral bioavailability which impede its use as an anticancer agent. Many technologies have been developed and applied to conquer this drawback. We bring to light the benefits of this phytoconstituent for treating different types of cancer. We also discussed some of the delivery approaches that have already made an impact by either delivering a drug to target tissue or increasing its bioavailability by many folds. PMID:26036845

  13. The Preparation of Capsaicin-Chitosan Microspheres (CCMS Enteric Coated Tablets

    Directory of Open Access Journals (Sweden)

    Jian Chen

    2013-12-01

    Full Text Available This study aimed to research the preparation and content determination of capsaicin-chitosan microspheres (CCMS enteric coated tablets. The core tablets were prepared with the method of wet granulation. Nine formulae were designed to determine the optimal formula of the core tablet. Eudragit L100 was used to prepare the CCMS enteric-coated tablets. The effect of enteric coated formulation variables such as content of talc (10%, 25% and 40%, plasticisers (TEC and DBS, dosage of plasticiser (10%, 20% and 30% and coating weight (2%, 3% and 5% were evaluated for drug release characteristics. The in vitro release was studied using 0.1 N HCl and pH 6.8 phosphate buffer. Enteric coated tablets without ruptures or swelling behaviour over 2 h in 0.1 N HCl indicated that these tablets showed acid resistance. The accumulated release rate in phosphate buffer (pH 6.8 revealed that the prepared tablets were able to sustain drug release into the intestine and a first-order release was obtained for capsaicin. This research is the first report of the preparation and content determination of CCMS enteric coated tablets. The sustained release behavior of enteric coated formulations in pH 6.8 phosphate buffer demonstrated that it would be a potential drug delivery platform for sustained delivery of gastric irritant drugs.

  14. Acid potentiation of the capsaicin receptor determined by a key extracellular site.

    Science.gov (United States)

    Jordt, S E; Tominaga, M; Julius, D

    2000-07-01

    The capsaicin (vanilloid) receptor, VR1, is a sensory neuron-specific ion channel that serves as a polymodal detector of pain-producing chemical and physical stimuli. The response of VR1 to capsaicin or noxious heat is dynamically potentiated by extracellular protons within a pH range encountered during tissue acidosis, such as that associated with arthritis, infarction, tumor growth, and other forms of injury. A molecular determinant for this important physiological activity was localized to an extracellular Glu residue (E600) in the region linking the fifth transmembrane domain with the putative pore-forming region of the channel. We suggest that this residue serves as a key regulatory site of the receptor by setting sensitivity to other noxious stimuli in response to changes in extracellular proton concentration. We also demonstrate that protons, vanilloids, and heat promote channel opening through distinct pathways, because mutations at a second site (E648) selectively abrogate proton-evoked channel activation without diminishing responses to other noxious stimuli. Our findings provide molecular evidence for stimulus-specific steps in VR1 activation and offer strategies for the development of novel analgesic agents. PMID:10859346

  15. JAVA Stereo Display Toolkit

    Science.gov (United States)

    Edmonds, Karina

    2008-01-01

    This toolkit provides a common interface for displaying graphical user interface (GUI) components in stereo using either specialized stereo display hardware (e.g., liquid crystal shutter or polarized glasses) or anaglyph display (red/blue glasses) on standard workstation displays. An application using this toolkit will work without modification in either environment, allowing stereo software to reach a wider audience without sacrificing high-quality display on dedicated hardware. The toolkit is written in Java for use with the Swing GUI Toolkit and has cross-platform compatibility. It hooks into the graphics system, allowing any standard Swing component to be displayed in stereo. It uses the OpenGL graphics library to control the stereo hardware and to perform the rendering. It also supports anaglyph and special stereo hardware using the same API (application-program interface), and has the ability to simulate color stereo in anaglyph mode by combining the red band of the left image with the green/blue bands of the right image. This is a low-level toolkit that accomplishes simply the display of components (including the JadeDisplay image display component). It does not include higher-level functions such as disparity adjustment, 3D cursor, or overlays all of which can be built using this toolkit.

  16. [Surfactant and water balance of lung in intracerebral hemorrhage at conditions of capsaicin blockade of vagus nerve].

    Science.gov (United States)

    Urakova, M A; Bryndina, I G

    2015-03-01

    It is known that intracranial hemorrhage (ICH) is accompanied by the development of neurogenic pulmonary edema and insufficiency of surfactant function. The present study was undertaken for evaluation of the role of vagal afferents in the mechanisms of ICH effects on pulmonary surfactant and water balance of the lung. We explored the surface activity and biochemical composition of surfactant, as well as blood supply, total, intravascular and extravascular fluid content in lung after ICH, simulated by intraventricular administration of autologous blood against the background of bilateral blockade of capsaicin-sensitive vagal affere its. The blockade was caused by the capsaicin application (50 mcmol) on the cervical part of the nerves. Intracerebralhemorrhage was accompanied by the decrease of surfactant activity which appeared by the enhancement of minimal, maximal and static surface tension of bronchoalveolar lavage fluid (BAL), the reduction of total phospholipids including their main fraction phosphatidylcholine, the increase of lysophosphatidyicholine content and hyperhydration of the lung. The level of total proteins in BAL elevated, confirmed the enhanced permeability of the alveolar-blood barrier. The exhaustion of neuropeptides in capsaicin-sensitive vagal afferents led to the partial restoration of surface active properties of lung, normalization of phospholipids and protein contents and water balance parameters. The obtained results suggest that capsaicin-sensitive vagal afferents play a pivotal role in the disturbances of surfactant function and water balance of the lung after ICH. PMID:26016324

  17. Electrochemical sensing platform amplified with a nanobiocomposite of L-phenylalanine ammonia-lyase enzyme for the detection of capsaicin.

    Science.gov (United States)

    Sabela, Myalowenkosi I; Mpanza, Thabani; Kanchi, Suvardhan; Sharma, Deepali; Bisetty, Krishna

    2016-09-15

    The present study involves the development of a sensitive electrochemical biosensor for the determination of capsaicin extracted from chilli fruits, based on a novel signal amplification strategy using enzyme technology. For the first time, platinum electrode modified with multiwalled carbon nanotubes where phenylalanine ammonia-lyase enzyme was immobilized using nafion was characterized by attenuated total reflectance infrared spectroscopy, transmittance electron microscopy and thermo-gravimetric analysis supported by computational methods. Cyclic and differential pulse voltammetry measurements were performed to better understand the redox mechanism of capsaicin. The performance of the developed electrochemical biosensor was tested using spiked samples with recoveries ranging from 98.9 to 99.6%. The comparison of the results obtained from bare and modified platinum electrodes revealed the sensitivity of the developed biosensor, having a detection limit (S/N=3) of 0.1863µgmL(-1) and electron transfer rate constant (ks) of 3.02s(-1). Furthermore, adsorption and ligand-enzyme docking studies were carried out to better understand the redox mechanisms supported by density functional theory calculations. These results revealed that capsaicin forms hydrogen bonds with GLU355, GLU541, GLU586, ARG and other amino acids of the hydrophobic channel of the binding sites thereby facilitating the redox reaction for the detection of capsaicin. PMID:27104584

  18. Increased visceral sensitivity to capsaicin after DSS-induced colitis in mice : spinal cord c-Fos expression and behavior

    NARCIS (Netherlands)

    Eijkelkamp, Niels; Kavelaars, Annemieke; Elsenbruch, Sigrid; Schedlowski, Manfred; Holtmann, Gerald; Heijnen, Cobi J.

    2007-01-01

    Increased visceral sensitivity to capsaicin after DSS-induced colitis in mice: spinal cord c-Fos expression and behavior. Am J Physiol Gastrointest Liver Physiol 293: G749-G757, 2007. First published July 26, 2007; doi:10.1152/ajpgi.00114.2007.During acute and chronic inflammation visceral pain perc

  19. Effective Monitor Display Design.

    Science.gov (United States)

    Harrell, William

    1999-01-01

    Describes some of the factors that affect computer monitor display design and provides suggestions and insights into how screen displays can be designed more effectively. Topics include color, font choices, organizational structure of text, space outline, and general principles. (Author/LRW)

  20. Polyplanar optical display electronics

    Energy Technology Data Exchange (ETDEWEB)

    DeSanto, L.; Biscardi, C. [Brookhaven National Lab., Upton, NY (United States). Dept. of Advanced Technology

    1997-07-01

    The Polyplanar Optical Display (POD) is a unique display screen which can be used with any projection source. The prototype ten inch display is two inches thick and has a matte black face which allows for high contrast images. The prototype being developed is a form, fit and functional replacement display for the B-52 aircraft which uses a monochrome ten-inch display. In order to achieve a long lifetime, the new display uses a 100 milliwatt green solid-state laser (10,000 hr. life) at 532 nm as its light source. To produce real-time video, the laser light is being modulated by a Digital Light Processing (DLP{trademark}) chip manufactured by Texas Instruments. In order to use the solid-state laser as the light source and also fit within the constraints of the B-52 display, the Digital Micromirror Device (DMD{trademark}) circuit board is removed from the Texas Instruments DLP light engine assembly. Due to the compact architecture of the projection system within the display chassis, the DMD{trademark} chip is operated remotely from the Texas Instruments circuit board. The authors discuss the operation of the DMD{trademark} divorced from the light engine and the interfacing of the DMD{trademark} board with various video formats (CVBS, Y/C or S-video and RGB) including the format specific to the B-52 aircraft. A brief discussion of the electronics required to drive the laser is also presented.

  1. Standardizing visual display quality

    NARCIS (Netherlands)

    Besuijen, Ko; Spenkelink, Gerd P.J.

    1998-01-01

    The current ISO 9241–3 standard for visual display quality and the proposed user performance tests are reviewed. The standard is found to be more engineering than ergonomic and problems with system configuration, software applications, display settings, user behaviour, wear and physical environment

  2. Helmet-Mounted Displays (HMD)

    Data.gov (United States)

    Federal Laboratory Consortium — The Helmet-Mounted Display labis responsible for monocular HMD day display evaluations; monocular HMD night vision performance processes; binocular HMD day display...

  3. Visual merchandising window display

    Directory of Open Access Journals (Sweden)

    Opris (Cas. Stanila M.

    2013-12-01

    Full Text Available Window display plays a major part in the selling strategies; it does not only include the simple display of goods, nowadays it is a form of art, also having the purpose of sustaining the brand image. This article wants to reveal the tools that are essential in creating a fabulous window display. Being a window designer is not an easy job, you have to always think ahead trends, to have a sense of colour, to know how to use light to attract customers in the store after only one glance at the window. The big store window displays are theatre scenes: with expensive backgrounds, special effects and high fashion mannequins. The final role of the displays is to convince customers to enter the store and trigger the purchasing act which is the final goal of the retail activity.

  4. Gingerol Reverses the Cancer-Promoting Effect of Capsaicin by Increased TRPV1 Level in a Urethane-Induced Lung Carcinogenic Model.

    Science.gov (United States)

    Geng, Shengnan; Zheng, Yaqiu; Meng, Mingjing; Guo, Zhenzhen; Cao, Ning; Ma, Xiaofang; Du, Zhenhua; Li, Jiahuan; Duan, Yongjian; Du, Gangjun

    2016-08-10

    Both gingerol and capsaicin are agonists of TRPV1, which can negatively control tumor progression. This study observed the long-term effects of oral administration of 6-gingerol alone or in combination with capsaicin for 20 weeks in a urethane-induced lung carcinogenic model. We showed that lung carcinoma incidence and multiplicity were 70% and 21.2 ± 3.6, respectively, in the control versus 100% and 35.6 ± 5.2 in the capsaicin group (P chili-pepper-rich diets to decrease the risk of cancer development. PMID:27436516

  5. Defense display market assessment

    Science.gov (United States)

    Desjardins, Daniel D.; Hopper, Darrel G.

    1998-09-01

    This paper addresses the number, function and size of principal military displays and establishes a basis to determine the opportunities for technology insertion in the immediate future and into the next millennium. Principal military displays are defined as those occupying appreciable crewstation real-estate and/or those without which the platform could not carry out its intended mission. DoD 'office' applications are excluded from this study. The military displays market is specified by such parameters as active area and footprint size, and other characteristics such as luminance, gray scale, resolution, angle, color, video capability, and night vision imaging system (NVIS) compatibility. Funded, future acquisitions, planned and predicted crewstation modification kits, and form-fit upgrades are taken into account. This paper provides an overview of the DoD niche market, allowing both government and industry a necessary reference by which to meet DoD requirements for military displays in a timely and cost-effective manner. The aggregate DoD market for direct-view and large-area military displays is presently estimated to be in excess of 242,000. Miniature displays are those which must be magnified to be viewed, involve a significantly different manufacturing paradigm and are used in helmet mounted displays and thermal weapon sight applications. Some 114,000 miniature displays are presently included within Service weapon system acquisition plans. For vendor production planning purposes it is noted that foreign military sales could substantially increase these quantities. The vanishing vendor syndrome (VVS) for older display technologies continues to be a growing, pervasive problem throughout DoD, which consequently must leverage the more modern display technologies being developed for civil- commercial markets.

  6. Is physician supervision of the capsaicin 8% patch administration procedure really necessary? An opinion from health care professionals

    Directory of Open Access Journals (Sweden)

    Kern KU

    2013-07-01

    Full Text Available Kai-Uwe Kern,1 Janice England,2 Andrea Roth-Daniek,3 Till Wagner3 1Institute for Pain Medicine/Pain Practice, Wiesbaden, Germany; 2Pain Medicine and Anaesthesia, The Christie National Health Service Foundation Trust, Manchester, UK; 3Pain Therapy and Palliative Care Department, Medizinisches Zentrum Städteregion Aachen, Aachen, Germany Abstract: Neuropathic pain is difficult to treat and can have a severe effect on quality of life. The capsaicin 8% patch is a novel treatment option that directly targets the source of peripheral neuropathic pain. It can provide pain relief for up to 12 weeks in patients with peripheral neuropathic pain. Treatment with the capsaicin 8% patch follows a clearly defined procedure, and patch application must be carried out by a physician or a health care professional under the supervision of a physician. Nonetheless, in our experience, nurses often take the lead role in capsaicin 8% patch application without the involvement of a physician. We believe that the nurse's key role is of benefit to the patients, as he or she may be better placed, because of time constraints and patient relationships, to support the patient through the application procedure than a physician. Moreover, a number of frequently prescribed drugs, including botulinum toxin and infliximab, can be administered by health care professionals without the requirement for physician supervision. Here we argue that current guidance should be amended to remove the requirement for physician supervision during application of the capsaicin 8% patch. Keywords: capsaicin, neuropathic pain, topical, health care professional, physician, nurse

  7. Perineural capsaicin induces the uptake and transganglionic transport of choleratoxin B subunit by nociceptive C-fiber primary afferent neurons.

    Science.gov (United States)

    Oszlács, O; Jancsó, G; Kis, G; Dux, M; Sántha, P

    2015-12-17

    The distribution of spinal primary afferent terminals labeled transganglionically with the choleratoxin B subunit (CTB) or its conjugates changes profoundly after perineural treatment with capsaicin. Injection of CTB conjugated with horseradish peroxidase (HRP) into an intact nerve labels somatotopically related areas in the ipsilateral dorsal horn with the exceptions of the marginal zone and the substantia gelatinosa, whereas injection of this tracer into a capsaicin-pretreated nerve also results in massive labeling of these most superficial layers of the dorsal horn. The present study was initiated to clarify the role of C-fiber primary afferent neurons in this phenomenon. In L5 dorsal root ganglia, analysis of the size frequency distribution of neurons labeled after injection of CTB-HRP into the ipsilateral sciatic nerve treated previously with capsaicin or resiniferatoxin revealed a significant increase in the proportion of small neurons. In the spinal dorsal horn, capsaicin or resiniferatoxin pretreatment resulted in intense CTB-HRP labeling of the marginal zone and the substantia gelatinosa. Electron microscopic histochemistry disclosed a dramatic, ∼10-fold increase in the proportion of CTB-HRP-labeled unmyelinated dorsal root axons following perineural capsaicin or resiniferatoxin. The present results indicate that CTB-HRP labeling of C-fiber dorsal root ganglion neurons and their central terminals after perineural treatment with vanilloid compounds may be explained by their phenotypic switch rather than a sprouting response of thick myelinated spinal afferents which, in an intact nerve, can be labeled selectively with CTB-HRP. The findings also suggest a role for GM1 ganglioside in the modulation of nociceptor function and pain. PMID:26520849

  8. Microlaser-based displays

    Science.gov (United States)

    Bergstedt, Robert; Fink, Charles G.; Flint, Graham W.; Hargis, David E.; Peppler, Philipp W.

    1997-07-01

    Laser Power Corporation has developed a new type of projection display, based upon microlaser technology and a novel scan architecture, which provides the foundation for bright, extremely high resolution images. A review of projection technologies is presented along with the limitations of each and the difficulties they experience in trying to generate high resolution imagery. The design of the microlaser based projector is discussed along with the advantage of this technology. High power red, green, and blue microlasers have been designed and developed specifically for use in projection displays. These sources, in combination with high resolution, high contrast modulator, produce a 24 bit color gamut, capable of supporting the full range of real world colors. The new scan architecture, which reduces the modulation rate and scan speeds required, is described. This scan architecture, along with the inherent brightness of the laser provides the fundamentals necessary to produce a 5120 by 4096 resolution display. The brightness and color uniformity of the display is excellent, allowing for tiling of the displays with far fewer artifacts than those in a traditionally tiled display. Applications for the display include simulators, command and control centers, and electronic cinema.

  9. Small - Display Cartography

    DEFF Research Database (Denmark)

    Nissen, Flemming; Hvas, Anders; Münster-Swendsen, Jørgen;

    This report comprises the work carried out in the work-package of small display cartography. The work-package has aimed at creating a general framework for the small-display cartography. A solid framework facilitates an increased use of spatial data in mobile devices - thus enabling, together...... Service Communication and finally, Part IV: Concluding remarks and topics for further research on small-display cartography. Part II includes a separate Appendix D consisting of a cartographic design specification. Part III includes a separate Appendix C consisting of a schema specification, a separate...

  10. Flexible displays, rigid designs?

    DEFF Research Database (Denmark)

    Hornbæk, Kasper

    2015-01-01

    Rapid technological progress has enabled a wide range of flexible displays for computing devices, but the user experience--which we're only beginning to understand--will be the key driver for successful designs....

  11. Stainless steel display evaluation

    Science.gov (United States)

    Hopper, Darrel G.; Meyer, Frederick M.; Longo, Sam J.; Trissell, Terry L.

    2007-04-01

    Active matrix organic light emitting diode (AMOLED) technology is one candidate to become a low power alternative in some applications to the currently dominant, active matrix liquid crystal display (AMLCD), technology. Furthermore, fabrication of the AMOLED on stainless steel (SS) foil rather than the traditional glass substrate, while presenting a set of severe technical challenges, opens up the potential for displays that are both lighter and less breakable. Also, transition to an SS foil substrate may enable rollable displays - large when used but small for stowage within gear already worn or carried or installed. Research has been initiated on AMOLED/SS technology and the first 320 x 240 color pixel 4-in. demonstration device has been evaluated in the AFRL Display Test and Evaluation Laboratory. Results of this evaluation are reported along with a research roadmap.

  12. Military display performance parameters

    Science.gov (United States)

    Desjardins, Daniel D.; Meyer, Frederick

    2012-06-01

    The military display market is analyzed in terms of four of its segments: avionics, vetronics, dismounted soldier, and command and control. Requirements are summarized for a number of technology-driving parameters, to include luminance, night vision imaging system compatibility, gray levels, resolution, dimming range, viewing angle, video capability, altitude, temperature, shock and vibration, etc., for direct-view and virtual-view displays in cockpits and crew stations. Technical specifications are discussed for selected programs.

  13. Raster graphics display library

    Science.gov (United States)

    Grimsrud, Anders; Stephenson, Michael B.

    1987-01-01

    The Raster Graphics Display Library (RGDL) is a high level subroutine package that give the advanced raster graphics display capabilities needed. The RGDL uses FORTRAN source code routines to build subroutines modular enough to use as stand-alone routines in a black box type of environment. Six examples are presented which will teach the use of RGDL in the fastest, most complete way possible. Routines within the display library that are used to produce raster graphics are presented in alphabetical order, each on a separate page. Each user-callable routine is described by function and calling parameters. All common blocks that are used in the display library are listed and the use of each variable within each common block is discussed. A reference on the include files that are necessary to compile the display library is contained. Each include file and its purpose are listed. The link map for MOVIE.BYU version 6, a general purpose computer graphics display system that uses RGDL software, is also contained.

  14. Adlea (ALGRX-4975), an injectable capsaicin (TRPV1 receptor agonist) formulation for longlasting pain relief.

    Science.gov (United States)

    Remadevi, Radhika; Szallisi, Arpad

    2008-02-01

    Anesiva Inc is developing Adlea (ALRGX-4975) - an injectable preparation of capsaicin, a TRPV1 (transient receptor potential vanilloid subfamily 1) receptor agonist - for the potential management of pain associated with osteoarthritis, tendonitiand postsurgical conditions, as well as for neuropathic pain occurring secondary to nerve injury. Adlea functions by desensitizing those neurons that conduct a long-lasting, throbbing form of pain. In phase II clinical trials, a single injection of Adlea significantly reduced pain levels in patients following total knee arthroplasty (TKA) or bunionectomy, and reduced pain in patients with osteoarthritis (OA) or Morton's neuroma. Phase II trials are ongoing to test Adlea in patients who are undergoing total hip arthroplasty or arthroscopic shoulder surgery and in patients with knee OA. Phase III clinical trials for the compound have been slated to begin in 2008 in patients following TKA or bunionectomy. Adlea appears to exhibit promise as a new medication in the treatment of conditions of chronic neuropathic pain. PMID:18240098

  15. N-[(1,3-Benzodioxol-5-ylmethyl]benzenesulfonamide: an analogue of capsaicin

    Directory of Open Access Journals (Sweden)

    Stella H. Maganhi

    2013-11-01

    Full Text Available The title compound, C14H13NO4S, an analogue of capsaicin, differs from the latter by having a 1,3-benzodioxole ring rather than a 2-methoxyphenol moiety, and having a benzenesulfonamide group instead of an aliphatic amide chain. The five-membered ring is in an envelope conformation with the methylene C atom lying 0.221 (6 Å out of the plane formed by the other four atoms. The dihedral angle between the phenyl ring and the mean plane of the 1,3-benzodioxole fused-ring system is 84.65 (4°. In the crystal, molecules aggregate into supramolecular layers in the ac plane through C—H...O, N—H...O and C—H...π interactions.

  16. The capsaicin receptor TRPV1 as a novel modulator of neural precursor cell proliferation.

    Science.gov (United States)

    Stock, Kristin; Garthe, Alexander; de Almeida Sassi, Felipe; Glass, Rainer; Wolf, Susanne A; Kettenmann, Helmut

    2014-12-01

    The capsaicin receptor (TRPV1, transient receptor potential vanilloid type 1) was first discovered in the peripheral nervous system as a detector of noxious chemical and thermal stimuli including the irritant chili pepper. Recently, there has been increasing evidence of TRPV1 expression in the central nervous system. Here, we show that TRPV1 is expressed in neural precursor cells (NPCs) during postnatal development, but not in the adult. However, expression of TRPV1 is induced in the adult in paradigms linked to an increase in neurogenesis, such as spatial learning in the Morris water maze or voluntary exercise. Loss of TRPV1 expression in knockout mice leads to an increase in NPC proliferation. Functional TRPV1 expression has been confirmed in cultured NPCs. Our results indicate that TRPV1 expression influences both postnatal and activity-induced neurogenesis in adulthood. PMID:25092424

  17. Phenylpyrazolone derivatives inhibit gastric emptying in rats by a capsaicin-sensitive afferent pathway

    Directory of Open Access Journals (Sweden)

    A.M. Vinagre

    2009-11-01

    Full Text Available Dipyrone (Dp, 4-aminoantipyrine (AA and antipyrine (At administered iv and Dp administered icv delay gastric emptying (GE in rats. The participation of capsaicin (Cps-sensitive afferent fibers in this phenomenon was evaluated. Male Wistar rats were pretreated sc with Cps (50 mg/kg or vehicle between the first and second day of life and both groups were submitted to the eye-wiping test. GE was determined in these animals at the age of 8/9 weeks (weight: 200-300 g. Ten minutes before the study, the animals of both groups were treated iv with Dp, AA or At (240 μmol/kg, or saline; or treated icv with Dp (4 μmol/animal or saline. GE was determined 10 min after treatment by measuring % gastric retention (GR of saline labeled with phenol red 10 min after orogastric administration. Percent GR (mean ± SEM, N = 8 in animals pretreated with Cps and treated with Dp, AA or At (35.8 ± 3.2, 35.4 ± 2.2, and 35.6 ± 2%, respectively did not differ from the GR of saline-treated animals pretreated with vehicle (36.8 ± 2.8% and was significantly lower than in animals pretreated with vehicle and treated with the drugs (52.1 ± 2.8, 66.2 ± 4, and 55.8 ± 3%, respectively. The effect of icv administration of Dp (N = 6 was not modified by pretreatment with Cps (63.3 ± 5.7% compared to Dp-treated animals pretreated with vehicle (62.3 ± 2.4%. The results suggest the participation of capsaicin-sensitive afferent fibers in the delayed GE induced by iv administration of Dp, AA and At, but not of icv Dp.

  18. Identifying the integrated neural networks involved in capsaicin-induced pain using fMRI in awake TRPV1 knockout and wild-type rats.

    Science.gov (United States)

    Yee, Jason R; Kenkel, William; Caccaviello, John C; Gamber, Kevin; Simmons, Phil; Nedelman, Mark; Kulkarni, Praveen; Ferris, Craig F

    2015-01-01

    In the present study, we used functional MRI in awake rats to investigate the pain response that accompanies intradermal injection of capsaicin into the hindpaw. To this end, we used BOLD imaging together with a 3D segmented, annotated rat atlas and computational analysis to identify the integrated neural circuits involved in capsaicin-induced pain. The specificity of the pain response to capsaicin was tested in a transgenic model that contains a biallelic deletion of the gene encoding for the transient receptor potential cation channel subfamily V member 1 (TRPV1). Capsaicin is an exogenous ligand for the TRPV1 receptor, and in wild-type rats, activated the putative pain neural circuit. In addition, capsaicin-treated wild-type rats exhibited activation in brain regions comprising the Papez circuit and habenular system, systems that play important roles in the integration of emotional information, and learning and memory of aversive information, respectively. As expected, capsaicin administration to TRPV1-KO rats failed to elicit the robust BOLD activation pattern observed in wild-type controls. However, the intradermal injection of formalin elicited a significant activation of the putative pain pathway as represented by such areas as the anterior cingulate, somatosensory cortex, parabrachial nucleus, and periaqueductal gray. Notably, comparison of neural responses to capsaicin in wild-type vs. knock-out rats uncovered evidence that capsaicin may function in an antinociceptive capacity independent of TRPV1 signaling. Our data suggest that neuroimaging of pain in awake, conscious animals has the potential to inform the neurobiological basis of full and integrated perceptions of pain. PMID:25745388

  19. Capsaicin causes inactivation and degradation of the androgen receptor by inducing the restoration of miR-449a in prostate cancer.

    Science.gov (United States)

    Zheng, Long; Chen, Jiaqi; Ma, Zhenkun; Liu, Wei; Yang, Fei; Yang, Zhao; Wang, Ke; Wang, Xinyang; He, Dalin; Li, Lei

    2015-08-01

    Capsaicin, a novel antitumor agent extracted from chili peppers, has been proven to induce growth inhibition in various types of cancer including prostate cancer. However, the detailed mechanisms remain largely undiscovered. In the present study, we explored the regulation of the androgen receptor (AR) by capsaicin and further researched the mechanisms of their interaction in AR-positive prostate cancer cells. In the present study, cell viability was assessed by MTT assay. Cell cycle distribution was determined using flow cytometry. Expression levels of cyclin D1, miR-449a, AR and prostate-specific antigen (PSA) were assessed by quantitative real-time polymerase chain reaction or western blot analysis. To further confirm the relationship among miR-449a, AR and prostate cancer proliferation, miR-449a was overexpressed by a lentivirus in prostate cancer cells. We discovered that capsaicin prevented tumor proliferation and cell cycle progression through inactivation and degradation of AR. We also found that restoration of miR-449a induced by capsaicin treatment resulted in the inhibition of AR signaling. Finally, we demonstrated that increased expression of miR-449a sensitized prostate cancer to capsaicin treatment. Finally, our experimental results indicated that capsaicin negatively modulates the activity of AR at the mRNA and protein levels by restoring miR-449a profiling in prostate cancer. In addition, increased expression of miR-449a may facilitate the sensitivity of prostate cancer to capsaicin treatment. Thus, capsaicin may be developed as a novel anti-AR drug for the therapy of prostate cancer.

  20. Identifying the Integrated Neural Networks Involved in Capsaicin-Induced Pain Using fMRI in Awake TRPV1 Knockout and Wild-Type Rats

    Directory of Open Access Journals (Sweden)

    Jason Richard Yee

    2015-02-01

    Full Text Available In the present study, we used functional MRI in awake rats to investigate the pain response that accompanies intradermal injection of capsaicin into the hindpaw. To this end, we used BOLD imaging together with a 3D segmented, annotated rat atlas and computational analysis to identify the integrated neural circuits involved in capsaicin-induced pain. The specificity of the pain response to capsaicin was tested in a transgenic model that contains a biallelic deletion of the gene encoding for the transient receptor potential cation channel subfamily V member 1 (TRPV1. Capsaicin is an exogenous ligand for the TRPV1 receptor, and in wild-type rats, activated the putative pain neural circuit. In addition, capsaicin-treated wild-type rats exhibited activation in brain regions comprising the Papez circuit and habenular system, systems that play important roles in the integration of emotional information, and learning and memory of aversive information, respectively. As expected, capsaicin administration to TRPV1-KO rats failed to elicit the robust BOLD activation pattern observed in wild-type controls. However, the intradermal injection of formalin elicited a significant activation of the putative pain pathway as represented by such areas as the anterior cingulate, somatosensory cortex, parabrachial nucleus, and periaqueductal gray. Notably, comparison of neural responses to capsaicin in wild-type versus knock-out rats uncovered evidence that capsaicin may function in an antinociceptive capacity independent of TRPV1 signaling. Our data suggest that neuroimaging of pain in awake, conscious animals has the potential to inform the neurobiological basis of full and integrated perceptions of pain.

  1. The Effects of Dietary Iron and Capsaicin on Hemoglobin, Blood Glucose, Insulin Tolerance, Cholesterol, and Triglycerides, in Healthy and Diabetic Wistar Rats

    OpenAIRE

    Márquez-Ibarra, Adriana; Huerta, Miguel; Villalpando-Hernández, Salvador; Ríos-Silva, Mónica; Díaz-Reval, María I.; Cruzblanca, Humberto; Mancilla, Evelyn; Trujillo, Xóchitl

    2016-01-01

    Objective Our aim was to assess the effects of dietary iron, and the compound capsaicin, on hemoglobin as well as metabolic indicators including blood glucose, cholesterol, triglycerides, insulin, and glucose tolerance. Materials and Methods Our animal model was the Wistar rat, fed a chow diet, with or without experimentally induced diabetes. Diabetic males were fed control, low, or high-iron diets, the latter, with or without capsaicin. Healthy rats were fed identical diets, but without the ...

  2. The effects of protein phosphatase inhibitors on the duration of central sensitization of rat dorsal horn neurons following injection of capsaicin

    Directory of Open Access Journals (Sweden)

    Fang Li

    2006-07-01

    Full Text Available Abstract Protein kinases and phosphatases catalyze opposing reactions of phosphorylation and dephosphorylation, which may modulate the function of crucial signaling proteins in central nervous system. This is an important mechanism in the regulation of intracellular signal transduction pathways in nociceptive neurons. To explore the role of protein phosphatase in central sensitization of spinal nociceptive neurons following peripheral noxious stimulation, using electrophysiological recording techniques, we investigated the role of two inhibitors of protein phosphatase type 2A (PP2A, fostriecin and okadaic acid (OA, on the responses of dorsal horn neurons to mechanical stimuli in anesthetized rats following intradermal injection of capsaicin. Central sensitization was initiated by injection of capsaicin into the plantar surface of the left paw. A microdialysis fiber was implanted in the spinal cord dorsal horn for perfusion of ACSF and inhibitors of PP2A, fostriecin and okadaic acid. We found that in ACSF pretreated animals, the responses to innocuous and noxious stimuli following capsaicin injection increased over a period of 15 min after injection and had mostly recovered by 60 min later. However, pre- or post-treatment with the phosphatase inhibitors, fostriecin or OA, significantly enhanced the effects of capsaicin injection by prolonging the responses to more than 3 hours. These results confirm that blockade of protein phosphatase activity may potentiate central sensitization of nociceptive transmission in the spinal cord following capsaicin injection and indicate that protein phosphatase type 2A may be involved in determining the duration of capsaicin-induced central sensitization.

  3. Phage and Yeast Display.

    Science.gov (United States)

    Sheehan, Jared; Marasco, Wayne A

    2015-02-01

    Despite the availability of antimicrobial drugs, the continued development of microbial resistance--established through escape mutations and the emergence of resistant strains--limits their clinical utility. The discovery of novel, therapeutic, monoclonal antibodies (mAbs) offers viable clinical alternatives in the treatment and prophylaxis of infectious diseases. Human mAb-based therapies are typically nontoxic in patients and demonstrate high specificity for the intended microbial target. This specificity prevents negative impacts on the patient microbiome and avoids driving the resistance of nontarget species. The in vitro selection of human antibody fragment libraries displayed on phage or yeast surfaces represents a group of well-established technologies capable of generating human mAbs. The advantage of these forms of microbial display is the large repertoire of human antibody fragments present during a single selection campaign. Furthermore, the in vitro selection environments of microbial surface display allow for the rapid isolation of antibodies--and their encoding genes--against infectious pathogens and their toxins that are impractical within in vivo systems, such as murine hybridomas. This article focuses on the technologies of phage display and yeast display, as these strategies relate to the discovery of human mAbs for the treatment and vaccine development of infectious diseases. PMID:26104550

  4. The Ultimate Display

    CERN Document Server

    Fluke, C J

    2016-01-01

    Astronomical images and datasets are increasingly high-resolution and multi-dimensional. The vast majority of astronomers perform all of their visualisation and analysis tasks on low-resolution, two-dimensional desktop monitors. If there were no technological barriers to designing the ultimate stereoscopic display for astronomy, what would it look like? What capabilities would we require of our compute hardware to drive it? And are existing technologies even close to providing a true 3D experience that is compatible with the depth resolution of human stereoscopic vision? We consider the CAVE2 (an 80 Megapixel, hybrid 2D and 3D virtual reality environment directly integrated with a 100 Tflop/s GPU-powered supercomputer) and the Oculus Rift (a low- cost, head-mounted display) as examples at opposite financial ends of the immersive display spectrum.

  5. Trigeminal ganglion neurons of mice show intracellular chloride accumulation and chloride-dependent amplification of capsaicin-induced responses.

    Directory of Open Access Journals (Sweden)

    Nicole Schöbel

    Full Text Available Intracellular Cl(- concentrations ([Cl(-](i of sensory neurons regulate signal transmission and signal amplification. In dorsal root ganglion (DRG and olfactory sensory neurons (OSNs, Cl(- is accumulated by the Na(+-K(+-2Cl(- cotransporter 1 (NKCC1, resulting in a [Cl(-](i above electrochemical equilibrium and a depolarizing Cl(- efflux upon Cl(- channel opening. Here, we investigate the [Cl(-](i and function of Cl(- in primary sensory neurons of trigeminal ganglia (TG of wild type (WT and NKCC1(-/- mice using pharmacological and imaging approaches, patch-clamping, as well as behavioral testing. The [Cl(-](i of WT TG neurons indicated active NKCC1-dependent Cl(- accumulation. Gamma-aminobutyric acid (GABA(A receptor activation induced a reduction of [Cl(-](i as well as Ca(2+ transients in a corresponding fraction of TG neurons. Ca(2+ transients were sensitive to inhibition of NKCC1 and voltage-gated Ca(2+ channels (VGCCs. Ca(2+ responses induced by capsaicin, a prototypical stimulus of transient receptor potential vanilloid subfamily member-1 (TRPV1 were diminished in NKCC1(-/- TG neurons, but elevated under conditions of a lowered [Cl(-](o suggesting a Cl(--dependent amplification of capsaicin-induced responses. Using next generation sequencing (NGS, we found expression of different Ca(2+-activated Cl(- channels (CaCCs in TGs of mice. Pharmacological inhibition of CaCCs reduced the amplitude of capsaicin-induced responses of TG neurons in Ca(2+ imaging and electrophysiological recordings. In a behavioral paradigm, NKCC1(-/- mice showed less avoidance of the aversive stimulus capsaicin. In summary, our results strongly argue for a Ca(2+-activated Cl(--dependent signal amplification mechanism in TG neurons that requires intracellular Cl(- accumulation by NKCC1 and the activation of CaCCs.

  6. Self-reported sleep duration associated with distraction analgesia, hyperemia, and secondary hyperalgesia in the heat-capsaicin nociceptive model

    OpenAIRE

    Campbell, Claudia M.; Bounds, Sara C.; Simango, Mpepera B.; Witmer, Kenneth R.; Campbell, James N.; Edwards, Robert R.; Haythornthwaite, Jennifer A; Smith, Michael T.

    2010-01-01

    Although sleep deprivation is known to heighten pain sensitivity, the mechanisms by which sleep modifies nociception are largely unknown. Few studies of sleep-pain interactions have utilized quantitative sensory testing models that implicate specific underlying physiologic mechanisms. One possibility, which is beginning to receive attention, is that differences in sleep may alter the analgesic effects of distraction. We utilized the heat-capsaicin nociceptive model to examine whether self-rep...

  7. Genetic variants involved in gallstone formation and capsaicin metabolism,and the risk of gallbladder cancer in Chilean women

    Institute of Scientific and Technical Information of China (English)

    Sergio; Báez; Yasuo; Tsuchiya; Alfonso; Calvo; Martha; Pruyas; Kazutoshi; Nakamura; Chikako; Kiyohara; Mari; Oyama; Masaharu; Yamamoto

    2010-01-01

    AIM:To determine the effects of genetic variants associated with gallstone formation and capsaicin (a pungent component of chili pepper) metabolism on the risk of gallbladder cancer (GBC).METHODS: A total of 57 patients with GBC, 119 patients with gallstones, and 70 controls were enrolled in this study. DNA was extracted from their blood or paraffi n block sample using standard commercial kits. The statuses of the genetic variants were assayed using Taqman SNP Genotyping Assays or Custom Taqman SNP Genotypi...

  8. NMDA receptors are involved in the antidepressant-like effects of capsaicin following amphetamine withdrawal in male mice.

    Science.gov (United States)

    Amiri, Shayan; Alijanpour, Sakineh; Tirgar, Fatemeh; Haj-Mirzaian, Arya; Amini-Khoei, Hossein; Rahimi-Balaei, Maryam; Rastegar, Mojgan; Ghaderi, Marzieh; Ghazi-Khansari, Mahmoud; Zarrindast, Mohammad-Reza

    2016-08-01

    Amphetamine withdrawal (AW) is accompanied by diminished pleasure and depression which plays a key role in drug relapse and addictive behaviors. There is no efficient treatment for AW-induced depression and underpinning mechanisms were not well determined. Considering both transient receptor potential cation channel, subfamily V, member 1 (TRPV1) and N-Methyl-d-aspartate (NMDA) receptors contribute to pathophysiology of mood and addictive disorders, in this study, we investigated the role of TRPV1 and NMDA receptors in mediating depressive-like behaviors following AW in male mice. Results revealed that administration of capsaicin, TRPV1 agonist, (100μg/mouse, i.c.v.) and MK-801, NMDA receptor antagonist (0.005mg/kg, i.p.) reversed AW-induced depressive-like behaviors in forced swimming test (FST) and splash test with no effect on animals' locomotion. Co-administration of sub-effective doses of MK-801 (0.001mg/kg, i.p.) and capsaicin (10μg/mouse, i.c.v) exerted antidepressant-like effects in behavioral tests. Capsazepine, TRPV1 antagonist, (100μg/mouse, i.c.v) and NMDA, NMDA receptor agonist (7.5mg/kg, i.p.) abolished the effects of capsaicin and MK-801, respectively. None of aforementioned treatments had any effect on behavior of control animals. Collectively, our findings showed that activation of TRPV1 and blockade of NMDA receptors produced antidepressant-like effects in male mice following AW, and these receptors are involved in AW-induced depressive-like behaviors. Further, we found that rapid antidepressant-like effects of capsaicin in FST and splash test are partly mediated by NMDA receptors. PMID:27167081

  9. The selective target of capsaicin on FASN expression and de novo fatty acid synthesis mediated through ROS generation triggers apoptosis in HepG2 cells.

    Directory of Open Access Journals (Sweden)

    Hathaichanok Impheng

    Full Text Available The inhibition of the mammalian de novo synthesis of long-chain saturated fatty acids (LCFAs by blocking the fatty acid synthase (FASN enzyme activity in tumor cells that overexpress FASN can promote apoptosis, without apparent cytotoxic to non-tumor cells. The present study aimed to focus on the potent inhibitory effect of capsaicin on the fatty acid synthesis pathway inducing apoptosis of capsaicin in HepG2 cells. The use of capsaicin as a source for a new FASN inhibitor will provide new insight into its possible application as a selective anti-cancer therapy. The present findings showed that capsaicin promoted apoptosis as well as cell cycle arrest in the G0/G1 phase. The onset of apoptosis was correlated with a dissipation of mitochondrial membrane potential (ΔΨm. Apoptotic induction by capsaicin was mediated by inhibition of FASN protein expression which was accompanied by decreasing its activity on the de novo fatty acid synthesis. The expression of FASN was higher in HepG2 cells than in normal hepatocytes that were resistant to undergoing apoptosis following capsaicin administration. Moreover, the inhibitory effect of capsaicin on FASN expression and activity was found to be mediated by an increase of intracellular reactive oxygen species (ROS generation. Treatment of HepG2 cells with capsaicin failed to alter ACC and ACLY protein expression, suggesting ACC and ACLY might not be the specific targets of capsaicin to induce apoptosis. An accumulation of malonyl-CoA level following FASN inhibition represented a major cause of mitochondrial-dependent apoptotic induction instead of deprivation of fatty acid per se. Here, we also obtained similar results with C75 that exhibited apoptosis induction by reducing the levels of fatty acid without any change in the abundance of FASN expression along with increasing ROS production. Collectively, our results provide novel evidence that capsaicin exhibits a potent anti-cancer property by targeting

  10. Digital holographic display

    Science.gov (United States)

    Lee, Cheok Peng; Chia, Yong Poo; Singh, Vijay Raj; Asundi, A.; Khoo, Xuan Jie; Tay, Kiat Long; Zhou, Junxiang

    2010-03-01

    This paper describes how a Digital Holographic Projector is designed and implemented to project two-dimension virtual images onto the volumetric display media. In this research, we focus on the method to create 3D models, diffractive algorithm and the display media. A 3D model is generated based on the 360° view with views at every 10° interval from a 3D perspective view software. The hologram interference fringes are re-producing from the Fraunhofer algorithm. In order to make more flexible and portable, a Compact Vision System is introduced to storage multiply interference fringes. At the same time, the fringes are sent out at 30 Hz frame by frame continually to the digital micro-mirror1. With the presence of Nd: YVO4 green laser and various optical components, the 3D 360° hologram images are dynamically reconstructed and projected onto the high speed rotating diffuser forming a 3D model at any viewing angle on the volumetric display media. Both volumetric display media, wet and dry methods are demonstrated to show their feasibility and convenience. Finally, the dry volumetric technique with vertical projection mounting is adopted and as the result shown that the speckle noise is significance reduced.

  11. Refreshing Refreshable Braille Displays.

    Science.gov (United States)

    Russomanno, Alexander; O'Modhrain, Sile; Gillespie, R Brent; Rodger, Matthew W M

    2015-01-01

    The increased access to books afforded to blind people via e-publishing has given them long-sought independence for both recreational and educational reading. In most cases, blind readers access materials using speech output. For some content such as highly technical texts, music, and graphics, speech is not an appropriate access modality as it does not promote deep understanding. Therefore blind braille readers often prefer electronic braille displays. But, these are prohibitively expensive. The search is on, therefore, for a low-cost refreshable display that would go beyond current technologies and deliver graphical content as well as text. And many solutions have been proposed, some of which reduce costs by restricting the number of characters that can be displayed, even down to a single braille cell. In this paper, we demonstrate that restricting tactile cues during braille reading leads to poorer performance in a letter recognition task. In particular, we show that lack of sliding contact between the fingertip and the braille reading surface results in more errors and that the number of errors increases as a function of presentation speed. These findings suggest that single cell displays which do not incorporate sliding contact are likely to be less effective for braille reading.

  12. Refreshing Refreshable Braille Displays.

    Science.gov (United States)

    Russomanno, Alexander; O'Modhrain, Sile; Gillespie, R Brent; Rodger, Matthew W M

    2015-01-01

    The increased access to books afforded to blind people via e-publishing has given them long-sought independence for both recreational and educational reading. In most cases, blind readers access materials using speech output. For some content such as highly technical texts, music, and graphics, speech is not an appropriate access modality as it does not promote deep understanding. Therefore blind braille readers often prefer electronic braille displays. But, these are prohibitively expensive. The search is on, therefore, for a low-cost refreshable display that would go beyond current technologies and deliver graphical content as well as text. And many solutions have been proposed, some of which reduce costs by restricting the number of characters that can be displayed, even down to a single braille cell. In this paper, we demonstrate that restricting tactile cues during braille reading leads to poorer performance in a letter recognition task. In particular, we show that lack of sliding contact between the fingertip and the braille reading surface results in more errors and that the number of errors increases as a function of presentation speed. These findings suggest that single cell displays which do not incorporate sliding contact are likely to be less effective for braille reading. PMID:25879973

  13. Analysis of capsaicin and dihydrocapsaicin in peppers and pepper sauces by solid phase microextraction-gas chromatography-mass spectrometry.

    Science.gov (United States)

    Peña-Alvarez, Araceli; Ramírez-Maya, Erika; Alvarado-Suárez, Luís Angel

    2009-04-01

    A simple method for the analysis of capsaicin and dihydrocapsaicin in peppers and pepper sauces by solid phase microextraction-gas chromatography-mass spectrometry has been developed. A novel device was designed for direct extraction solid phase microextraction in order to avoid damage to the fiber. The analysis was performed without derivatization for the gas chromatography-mass spectrometry analysis. Selection fiber, extraction temperature, extraction time and pH, were optimized. The method was linear in the range 0.109-1.323 microg/mL for capsaicin and 0.107-1.713 microg/mL for dihydrocapsaicin with correlation coefficient up to r=0.9970 for both capsaicinoids. The precision of the method was less than 10%. The method was applied to the analysis of 11 varieties of peppers and four pepper sauces. A broad range of capsaicin (55.0-25 459 microg/g) and dihydrocapsaicin (93-1 130 microg/g) was found in the pepper and pepper sauces samples (4.3-717.3 and 1.0-134.8 microg/g), respectively.

  14. Effects of intra-fourth ventricle injection of crocin on capsaicin-induced orofacial pain in rats

    Directory of Open Access Journals (Sweden)

    Esmaeal Tamaddonfard

    2015-08-01

    Full Text Available Objectives: Crocin, a constituent of saffron and yellow gardenia, possesses anti-nociceptive effects. In the present study, we investigated the effects of intra-fourth ventricle injection of crocin in a rat model of orofacial pain. The contribution of opioid system was assessed using intra-fourth ventricle injection of naloxone, an opioid receptor antagonist. Materials and Methods: A guide cannula was implanted into the fourth ventricle of brain in anesthetized rats. Orofacial pain was induced by subcutaneous (s.c. injection of capsaicin (1.5 µg/20 µl into the right vibrissa pad. The time spent face rubbing/grooming was recorded for a period of 20 min. Locomotor activity was measured using an open-field test. Results: Intra-fourth ventricle injection of crocin (10 and 40 µg/rat and morphine (10 and 40 µg/rat and their co-administration (2.5 and 10 µg/rat of each suppressed capsaicin-induced orofacial pain. The analgesic effect induced by 10 µg/rat of morphine, but not crocin (10 µg/rat, was prevented by 20 µg/rat of naloxone pretreatment. The above-mentioned chemical compounds did not affect locomotor activity. Conclusion: The results of this study showed that the injection of crocin into the cerebral fourth ventricle attenuates capsaicin-induced orofacial pain in rats. The anti-nociceptive effect of crocin was not attributed to the central opioid receptors.

  15. Tactile Displays with Parallel Mechanism

    OpenAIRE

    Kyung, Ki-Uk; Kwon, Dong-Soo

    2008-01-01

    This chapter deals with tactile displays and their mechanisms. We briefly reviewed research history of mechanical type tactile displays and their parallel arrangement. And this chapter mainly describes two systems including tactile displays. The 5x6 pin arrayed tactile display with parallel arrangement of piezoelectric bimorphs has been described in the section 3. The tactile display has been embedded into a mouse device and the performance of the device has been verified from pattern display...

  16. LED projection displays

    Science.gov (United States)

    Lee, Won Yong; Lee, Young Chol; Sokolov, Kirill; Lee, Hee Joong; Moon, Il

    2004-09-01

    In this paper a new illumination system with high power light emitting diode (LED) sources for projection displays is proposed. The prototype of a rear projection system has been developed by using red, green and blue (RGB) LEDs and three LCD panels. Four LEDs were used for each primary color. Parabola reflectors were used for collimating the LED lights and a new array style of LEDs and collimators were used. Integration rods were directly used between collimators and LCD panels without relay lens for uniform light distribution. A 40" projection display system was made with a light output about 25 lm on the screen and the projection engine was very small comparing to the original engine which uses an arc source.

  17. Unsolicited displays of insights

    DEFF Research Database (Denmark)

    Brouwer, Catherine E.

    2015-01-01

    This study is based on videorecorded interactional data from a specific type of institutional setting which consists of a variety of 'language stimulation activities' for bilingual children in Danish preschools. Bilingual children, with a variety of linguistic backgrounds, take part in these......) learning and contrasts it to the widely studied IRF/IRE pattern in educational contexts. The activities were videotaped, transcribed and analysed according to principles and procedures of Conversation Analysis.......: Unsolicited displays may lead to side sequences, they may lead to a shift in the main business of the talk, or they may be explicitly or implicitly ignored. The paper discusses whether and how these unsolicited displays of understanding then can be thought of as leading to opportunities for (language...

  18. Effects of aural stimulation with capsaicin ointment on swallowing function in elderly patients with non-obstructive dysphagia

    Directory of Open Access Journals (Sweden)

    Kondo E

    2014-10-01

    Full Text Available Eiji Kondo,1,2 Osamu Jinnouchi,3 Hiroki Ohnishi,3 Ikuji Kawata,3 Seiichi Nakano,2 Masakazu Goda,1 Yoshiaki Kitamura,1 Koji Abe,1 Hiroshi Hoshikawa,4 Hidehiko Okamoto,5 Noriaki Takeda1 1Department of Otolaryngology, University of Tokushima School of Medicine, Tokushima, Japan; 2Department of Otolaryngology, Kochi National Hospital, Kochi, Japan; 3Department of Otolaryngology, Anan Kyoei Hospital, Anan, Japan; 4Department of Otolaryngology, Kagawa University School of Medicine, Kagawa, Japan; 5Department of Sensori-Motor Integration, National Institute for Physiological Sciences, Okazaki, Japan Objective: In the present study, an attempt was made to examine the effects of aural ­stimulation with ointment containing capsaicin on swallowing function in order to develop a novel and safe treatment for non-obstructive dysphagia in elderly patients. Design: A prospective pilot, non-blinded, non-controlled study with case series evaluating a new treatment. Setting: Secondary hospitals. Patients and methods: The present study included 26 elderly patients with non-obstructive dysphagia. Ointment containing 0.025% capsaicin (0.5 g was applied to the external auditory canal with a cotton swab under otoscope only once or once a day for 7 days before swallowing of a bolus of colored water (3 mL, which was recorded by transnasal videoendoscopy and evaluated according to the endoscopic swallowing score. Results: After a single application of 0.025% capsaicin ointment to the right external auditory canal, the endoscopic swallowing score was significantly decreased, and this effect lasted for 60 minutes. After repeated applications of the ointment to each external auditory canal alternatively once a day for 7 days, the endoscopic swallowing score decreased significantly in patients with more severe non-obstructive dysphagia. Of the eight tube-fed patients of this group, three began direct swallowing exercises using jelly, which subsequently restored their oral

  19. Refrigerated display cabinets; Butikskyla

    Energy Technology Data Exchange (ETDEWEB)

    Fahlen, Per

    2000-07-01

    This report summarizes experience from SP research and assignments regarding refrigerated transport and storage of food, mainly in the retail sector. It presents the fundamentals of heat and mass transfer in display cabinets with special focus on indirect systems and secondary refrigerants. Moreover, the report includes a brief account of basic food hygiene and the related regulations. The material has been compiled for educational purposes in the Masters program at Chalmers Technical University.

  20. Activation of TRPV1 by capsaicin induces functional Kinin B1 receptor in rat spinal cord microglia

    Directory of Open Access Journals (Sweden)

    Talbot Sébastien

    2012-01-01

    Full Text Available Abstract Background The kinin B1 receptor (B1R is upregulated by pro-inflammatory cytokines and oxydative stress, which are enhanced by transient receptor potential vanilloid subtype 1 (TRPV1 activation. To examine the link between TRPV1 and B1R in inflammatory pain, this study aimed to determine the ability of TRPV1 to regulate microglial B1R expression in the spinal cord dorsal horn, and the underlying mechanism. Methods B1R expression (mRNA, protein and binding sites was measured in cervical, thoracic and lumbar spinal cord in response to TRPV1 activation by systemic capsaicin (1-50 mg/kg, s.c in rats pre-treated with TRPV1 antagonists (capsazepine or SB-366791, the antioxidant N-acetyl-L-cysteine (NAC, or vehicle. B1R function was assessed using a tail-flick test after intrathecal (i.t. injection of a selective B1R agonist (des-Arg9-BK, and its microglial localization was investigated by confocal microscopy with the selective fluorescent B1R agonist, [Nα-bodipy]-des-Arg9-BK. The effect of i.t. capsaicin (1 μg/site was also investigated. Results Capsaicin (10 to 50 mg/kg, s.c. enhanced time-dependently (0-24h B1R mRNA levels in the lumbar spinal cord; this effect was prevented by capsazepine (10 mg/kg, i.p.; 10 μg/site, i.t. and SB-366791 (1 mg/kg, i.p.; 30 μg/site, i.t.. Increases of B1R mRNA were correlated with IL-1β mRNA levels, and they were significantly less in cervical and thoracic spinal cord. Intrathecal capsaicin (1 μg/site also enhanced B1R mRNA in lumbar spinal cord. NAC (1 g/kg/d × 7 days prevented B1R up-regulation, superoxide anion production and NF-kB activation induced by capsaicin (15 mg/kg. Des-Arg9-BK (9.6 nmol/site, i.t. decreased by 25-30% the nociceptive threshold at 1 min post-injection in capsaicin-treated rats (10-50 mg/kg while it was without effect in control rats. Des-Arg9-BK-induced thermal hyperalgesia was blocked by capsazepine, SB-366791 and by antagonists/inhibitors of B1R (SSR240612, 10 mg/kg, p

  1. Visual Perception and Holographic Displays

    International Nuclear Information System (INIS)

    Holographic displays have the potential to reproduce the natural parallax and focusing affordances of real scenes. Although holographic displays are still far from maturity, no other display technologies have the potential to reproduce these affordances as accurately. This paper reviews visual human-factors considerations for current and future holographic displays.

  2. Handbook of Visual Display Technology

    CERN Document Server

    Cranton, Wayne; Fihn, Mark

    2012-01-01

    The Handbook of Visual Display Technology is a unique work offering a comprehensive description of the science, technology, economic and human interface factors associated with the displays industry. An invaluable compilation of information, the Handbook will serve as a single reference source with expert contributions from over 150 international display professionals and academic researchers. All classes of display device are covered including LCDs, reflective displays, flexible solutions and emissive devices such as OLEDs and plasma displays, with discussion of established principles, emergent technologies, and particular areas of application. The wide-ranging content also encompasses the fundamental science of light and vision, image manipulation, core materials and processing techniques, display driving and metrology.

  3. Book Display as Adult Service

    Directory of Open Access Journals (Sweden)

    Matthew S. Moore

    1997-03-01

    Full Text Available 無Book display as an adult service is defined as choosing and positioning adult books from the collection to increase their circulation. The author contrasts bookstore arrangement for sales versus library arrangement for access. The paper considers the library-as-a-whole as a display, examines the right size for an in-library display, and discusses mass displays, end-caps, on-shelf displays, and the Tiffany approach. The author proposes that an effective display depends on an imaginative, unifying theme, and that book displays are part of the joy of libraries.

  4. Application of Design Expert for the investigation of capsaicin-loaded microemulsions for transdermal delivery.

    Science.gov (United States)

    Duangjit, Sureewan; Chairat, Wisuta; Opanasopit, Praneet; Rojanarata, Theerasak; Ngawhirunpat, Tanasait

    2016-09-01

    Our previous study reported that the Design Expert® Software showed a beneficial role in the development of microemulsions (ME) for transdermal drug delivery. To fully confirm the reproducibility and the reliability of simultaneous optimal ME formulations, the optimal ME formulations predicted by the Design Expert® Software were experimentally formulated and verified for their skin permeability. Ternary phase diagrams were used to predict the optimal ME area, and the ME formulations selected from outside this area were considered as candidate ME systems. Our ME systems were formulated with isopropyl myristate (IPM) as the oil phase, cocamide diethanolamine (DEA) as the surfactant, ethanol as a co-surfactant and water as the aqueous phase. The droplet size, size distribution, electrical conductivity, pH, drug content and skin permeability of the candidate ME systems were monitored. Our findings indicated that the skin permeability of the optimal ME and all of the candidate ME formulations was significantly greater than that of the commercial capsaicin (CAP) product. Our study succeeded in predicting and developing the ME systems for the transdermal delivery of CAP. The simplex lattice design used in this study is experimentally useful for the development of pharmaceutical formulations.

  5. Effects of capsaicin on nitric oxide synthase isoforms in prepubertal rat ovary.

    Science.gov (United States)

    Zik, B; Altunbas, K; Tutuncu, S; Ozden, O; Ozguden Akkoc, C G; Peker, S; Sevimli, A

    2012-04-01

    Nitric oxide (NO) has emerged as an important intra-ovarian regulatory factor. We investigated effects of low dose capsaicin (CAP) treatment on the different NOS isoforms in prepubertal rat ovaries. Fifteen 21-day-old female Sprague-Dawley rats were divided randomly into three groups. The first group received no treatment, the second group received 0.5 mg/kg/day CAP dissolved in the vehicle, and the third group was treated with the vehicle only. The animals were euthanized by ether inhalation after 15 days and their ovaries were excised. Ovaries were fixed in 10% neutral buffered formalin and embedded in paraffin. Sections were processed for standard immunohistochemistry using the labeled streptavidin-biotin technique for expression of nNOS, eNOS and iNOS. We demonstrated that CAP induced expression of NOS isotypes including eNOS, iNOS and nNOS in prepubertal rat ovaries. CAP may lead to release of NO either directly from nerves or indirectly by evoking release from other cells via the action of neuropeptides that are released from afferent terminals and are involved in regulating female reproductive function.

  6. Development of Organogel-Derived Capsaicin Nanoemulsion with Improved Bioaccessibility and Reduced Gastric Mucosa Irritation.

    Science.gov (United States)

    Lu, Muwen; Cao, Yong; Ho, Chi-Tang; Huang, Qingrong

    2016-06-15

    Capsaicin (CAP) is the major active component in chili peppers with health-promoting benefits. However, the low bioavailability and irritating quality of CAP greatly limit its applications in functional foods. The objective of this study was to develop a food-grade nanoemulsion to increase the dissolution and bioaccessibility of CAP and to alleviate its irritating effects. To achieve this goal, CAP was first dissolved in medium-chain triacylglycerol (MCT), followed by the addition of sucrose stearate S-370 as organogelator to develop CAP-loaded organogel. The oil-in-water (O/W) emulsion was formed using organogel as the oil phase and Tween 80 as the emulsifier. After ultrasonication treatment, droplet sizes of emulsion were decreased to 168 nm with enhanced dissolution rate and bioaccessibility. In vivo study further confirmed the reduced rat gastric mucosa irritation caused by CAP. The organogel-derived nanoemulsion was proved to be an effective delivery system for CAP-based functional food products. PMID:27170269

  7. Liposomal topical capsaicin in post-herpetic neuralgia: a safety pilot study

    Directory of Open Access Journals (Sweden)

    Manoel Jacobsen Teixeira

    2015-03-01

    Full Text Available Topical treatments have gained popularity for general use as an adjunct to systemic drugs in neuropathic pain, but their use produces variable clinical results and local adverse events. Objective To evaluate the safety and analgesic effect of a formulation of liposomal capsaicin (LC (0.025% in patients with post herpetic neuralgia (PHN. Method Patients who remained symptomatic after first-and second-line treatment were randomized to receive LC for six weeks in a placebo-controlled, crossover design study. Clinical assessment was performed at baseline, in the second, fourth and sixth week of treatment. Results Thirteen patients completed both treatment periods. Visual Analog Scale (VAS was significantly decreased after the end of the study (p = 0.008, however the effect of treatment was not significant (p = 0.076. There was no difference on global impression of change and other pain characteristics. LC was safe and well tolerated. However, at the concentration used, its analgesic effects were marginal and not significant.

  8. Application of Design Expert for the investigation of capsaicin-loaded microemulsions for transdermal delivery.

    Science.gov (United States)

    Duangjit, Sureewan; Chairat, Wisuta; Opanasopit, Praneet; Rojanarata, Theerasak; Ngawhirunpat, Tanasait

    2016-09-01

    Our previous study reported that the Design Expert® Software showed a beneficial role in the development of microemulsions (ME) for transdermal drug delivery. To fully confirm the reproducibility and the reliability of simultaneous optimal ME formulations, the optimal ME formulations predicted by the Design Expert® Software were experimentally formulated and verified for their skin permeability. Ternary phase diagrams were used to predict the optimal ME area, and the ME formulations selected from outside this area were considered as candidate ME systems. Our ME systems were formulated with isopropyl myristate (IPM) as the oil phase, cocamide diethanolamine (DEA) as the surfactant, ethanol as a co-surfactant and water as the aqueous phase. The droplet size, size distribution, electrical conductivity, pH, drug content and skin permeability of the candidate ME systems were monitored. Our findings indicated that the skin permeability of the optimal ME and all of the candidate ME formulations was significantly greater than that of the commercial capsaicin (CAP) product. Our study succeeded in predicting and developing the ME systems for the transdermal delivery of CAP. The simplex lattice design used in this study is experimentally useful for the development of pharmaceutical formulations. PMID:25996630

  9. The role of nitric oxide in the phosphorylation of cyclic adenosine monophosphate-responsive element-binding protein in the spinal cord after intradermal injection of capsaicin.

    Science.gov (United States)

    Wu, Jing; Fang, Li; Lin, Qing; Willis, William D

    2002-06-01

    We investigated the involvement of nitric oxide (NO) in the phosphorylation of cyclic adenosine monophosphate-responsive element-binding protein (CREB) in the spinal cord of rats during central sensitization after intradermal capsaicin injection. CREB and phosphorylated CREB (p-CREB) were measured by immunoblotting. The level of p-CREB increased by 20 minutes, peaked between 20 and 60 minutes after capsaicin injection, and started to decrease after 150 minutes. CREB itself did not show an obvious change after capsaicin injection. The p-CREB expression on the ipsilateral side of the spinal dorsal horn, but not on the contralateral side, increased significantly after capsaicin injection. The increase in p-CREB induced by capsaicin injection was partially blocked by pretreatment with N(G)-nitro-L-arginine methyl ester (L-NAME), an NO synthase inhibitor, administered through a microdialysis fiber placed across the spinal cord. D-NAME, an inactive form of L-NAME, had no effect. CREB phosphorylation, not the level of CREB, was induced within 20 minutes by microdialysis administration of SIN-1, an NO donor. These results indicate that CREB phosphorylation in the spinal cord results from both endogenous and exogenous NO release and that p-CREB may play a role in central sensitization or in longer-term changes in gene expression induced by strong peripheral noxious stimulation. PMID:14622772

  10. Effect of capsaicin on the health of gastrointestinal tract%辣椒素对胃肠道健康的影响

    Institute of Scientific and Technical Information of China (English)

    苏昕峰; 文红丽; 刘雄

    2011-01-01

    As an important spice, the hot pepper has the important physiological function for human. The "hot" mainly dues to capsaicin in the hot pepper. Capsaicin has broad pharmacological effects, lots of researches has been made to explore the effects of capsaicin to the health of gastrointestinal. In order to make better use of capsaicin,this paper summarized the effects that made by capsaicin to gastrointestinal and their mechanisms.%辣椒是重要的香辛料,对人体有重要的生理作用.辣椒主要的辛辣成分是辣椒素,辣椒素药理作用广泛,国内外开展了大量关于辣椒素对胃肠道健康作用方面的研究.本文就辣椒素对胃肠道健康的影响及其机制进行了综述,以期为辣椒素的科学利用提供参考.

  11. Radiations from display devices

    International Nuclear Information System (INIS)

    45 display devices have been analyzed for X-ray emmission and for electrostatic - and low-frequency magnetic fields. 3 have been further analyzed for UV and visible light emmission. No emmissions above established risk levels have been found. For low-frequency magnetic fields very little is known of risks, so the levels have been compared with other commonly used devices. The measured levels correspond roughly to that which occur in the use of an electrical egg-beater, or a small hand electrical drill. Data are presented for the tested devices.(author)

  12. Anti-Proliferative Effect of an Aqueous Extract of Prunella vulgaris in Vascular Smooth Muscle Cells

    Directory of Open Access Journals (Sweden)

    Sun Mi Hwang

    2013-01-01

    Full Text Available The abnormal proliferation of vascular smooth muscle cells (VSMCs in arterial walls is an important pathogenic factor of vascular disorders such as diabetic atherosclerosis. We have reported the anti-inflammatory effect of an aqueous extract from Prunella vulgaris (APV in vascular endothelial cell. In the present study, APV exhibited inhibitory effects on high glucose-stimulated VSMC proliferation, migration, and invasion activities, inducing G1 cell cycle arrest with downregulation of cyclins and CDKs and upregulation of the CKIs, p21waf1/cip1 and p27kip1. Furthermore, APV dose dependently suppressed the high glucose-induced matrix metalloproteinase activity. High glucose-induced phosphorylation of ERK, p38 MAPK, was decreased by the pretreatment of APV. NF-κB activation by high glucose was attenuated by APV, as an antioxidant. APV attenuated the high glucose-induced decrease of nuclear factor E2-related factor-2 (Nrf2 translocation and heme oxygenase-1 (HO-1 expression. Intracellular cGMP level was also increased by APV treatment. These results demonstrate that APV may inhibit VSMC proliferation via downregulating ROS/NF-κB /ERK/p38 MAPK pathways. In addition, APV has a beneficial effect by the interaction of Nrf2-mediated NO/cGMP with HO-1, suggesting that Prunella vulgaris may be useful in preventing diabetic atherosclerosis.

  13. Anti-Proliferative Effect of Copper Oxide Nanorods Against Human Cervical Carcinoma Cells.

    Science.gov (United States)

    Pandurangan, Muthuraman; Nagajyothi, P C; Shim, Jaesool; Kim, Doo Hwan

    2016-09-01

    Metal oxide nanoparticles have been widely investigated for its use in the pharmacological field. The present study was aimed to investigate the cytotoxicity of copper oxide nanorods in human cervical carcinoma cells. The effect of copper oxide nanorods on cell viability was determined by sulforhodamine-B (SRB) assay. The fluorescence and confocal microscopy analyzes showed the cell rounding and nuclear fragmentation following exposure of copper oxide nanorods. Reactive oxygen species (ROS) was increased and could initiate membrane lipid peroxidation, which in turn regulate cytokinetic movements of cells. The messenger RNA (mRNA) expression of p53 and caspase 3 was increased, which further confirms the occurrence of apoptosis at the transcriptional level. Furthermore, caspase-3 enzyme activity was increased, which also confirms the occurrence of apoptosis in tumor cells at the translational level. Taking all our experimental results together, it may suggest that the copper oxide nanorods could be a potential anti-tumor agent to inhibit cancer cell proliferation. PMID:26811107

  14. Synergistic anti-proliferative effects of gambogic acid with docetaxel in gastrointestinal cancer cell lines

    Directory of Open Access Journals (Sweden)

    Zou Zhengyun

    2012-04-01

    Full Text Available Summary Background Gambogic acid has a marked anti-tumor effect for gastric and colorectal cancers in vitro and in vivo. However, recent investigations on gambogic acid have focused mainly on mono-drug therapy, and its potential role in cancer therapy has not been comprehensively illustrated. This study aimed to assess the interaction between gambogic acid and docetaxel on human gastrointestinal cancer cells and to investigate the mechanism of gambogic acid plus docetaxel treatment-induced apoptotic cell death. Methods MTT assay was used to determine IC50 values in BGC-823, MKN-28, LOVO and SW-116 cells after gambogic acid and docetaxel administration. Median effect analysis was applied for determination of synergism and antagonism. Synergistic interaction between gambogic acid and docetaxel was evaluated using the combination index (CI method. Furthermore, cellular apoptosis was analyzed by Annexin-V and propidium iodide (PI double staining. Additionally, mRNA expression of drug-associated genes, i.e., β-tublin III and tau, and the apoptosis-related gene survivin, were measured by quantitative reverse transcription polymerase chain reaction (qRT-PCR. Results Gambogic acid provided a synergistic effect on the cytotoxicity induced by docetaxel in all four cell lines. The combined application of gambogic acid and docetaxel enhanced apoptosis in gastrointestinal cancer cells. Moreover, gambogic acid markedly decreased the mRNA expression of docetaxel-related genes, including β-tubulin III, tau and survivin, in BGC-823 cells. Conclusions Gambogic acid plus docetaxel produced a synergistic anti-tumor effect in gastrointestinal cancer cells, suggesting that the drug combination may offer a novel treatment option for patients with gastric and colorectal cancers.

  15. Anti-proliferative and computational studies of two new pregnane glycosides from Desmidorchis flava.

    Science.gov (United States)

    Raees, Muhammad Adil; Hussain, Hidayat; Al-Rawahi, Ahmed; Csuk, René; Muhammad, Syed Aun; Khan, Husain Yar; Rehman, Najeeb Ur; Abbas, Ghulam; Al-Broumi, Mohammed Abdullah; Green, Ivan R; Elyassi, Ali; Mahmood, Talat; Al-Harrasi, Ahmed

    2016-08-01

    Two new pregnane glycosides named desmiflavasides C (1) and D (2) were isolated from the sap of Desmidorchis flava (N.E.Br.) Meve & Liede and have had their structures confirmed from 1D and 2D NMR spectroscopic techniques and mass spectrometry (ESIMS). Further, the effects of desmiflavasides C (1) and D (2) on the proliferation of breast and ovarian cancer cells as well as normal breast epithelial cells in culture were examined. Interestingly, desmiflavasides C (1) and D (2) were able to cause a substantial decline in the viability of cancer cells in a concentration-dependent manner. Moreover, treatment of normal cells with compound 2 resulted in no significant growth inhibition, indicating that its cytotoxicity was selective towards cancer cells. Furthermore, the activity of compound 2 against cancer as well as normal epithelial cells was found to be similar to that of a previously reported pregnane glycoside, nizwaside (3). Molecular docking studies of desmiflavasides C (1) and D (2) and nizwaside (3) were carried out to ascertain if it was possible to predict any important binding orientations required of small molecule drug candidates with suggested protein target molecules for the purposes of being able to predict the affinity and activity to an acceptable degree by such compounds. Desmiflavaside D (2) showed a relatively good binding affinity (-22.4449kcal/mol) as compared to the other two compounds viz., nizwaside (3) (-20.0319kcal/mol), and desmiflavaside C (1) (-19.4042kcal/mol). Docking results of the three pregnane glycosides viz., 1-3 revealed that these ligand molecules can accurately interact with the target protein. PMID:27299811

  16. In-vitro release of anti-proliferative paclitaxel from novel balloon-expandable polycaprolactone stents

    International Nuclear Information System (INIS)

    This report investigated the in-vitro release characteristics of paclitaxel from novel balloon-expandable polycaprolactone stents. Polycaprolactone stents were first manufactured by a lab-made micro-injection molding machine. Paclitaxel and polylactide-polyglycolide (PLGA) copolymer were dissolved in acetonitrile and were coated onto the surface of the stents by a spray coating device, which was designed and built especially for this study. An elution method was utilized to characterize the in-vitro release characteristics of paclitaxel. The high performance liquid chromatography (HPLC) analysis showed that biodegradable stents could provide sustained release of paclitaxel for more than 70 days. Various process parameters that controlled the release rate of paclitaxel were studied. The experimental results suggested that the total period of drug release could be prolonged by adopting 75:25 PLGA copolymers, employing multi-layer coatings, and increasing the drug loading. In addition, the effectiveness of eluted paclitaxel on cell behavior was examined. The results showed that the eluted drug could effectively inhibit the proliferation of smooth muscle cells. - Research Highlights: → We investigate the in-vitro release characteristics of paclitaxel from polycaprolactone stents. → Biodegradable stents provide sustained release of paclitaxel for more than 70 days. → The eluted drug effectively inhibits the proliferation of smooth muscle cells.

  17. Anti-Proliferative Effects of Siegesbeckia orientalis Ethanol Extract on Human Endometrial RL-95 Cancer Cells

    Directory of Open Access Journals (Sweden)

    Chi-Chang Chang

    2014-12-01

    Full Text Available Endometrial cancer is a common malignancy of the female genital tract. This study demonstrates that Siegesbeckia orientalis ethanol extract (SOE significantly inhibited the proliferation of RL95-2 human endometrial cancer cells. Treating RL95-2 cells with SOE caused cell arrest in the G2/M phase and induced apoptosis of RL95-2 cells by up-regulating Bad, Bak and Bax protein expression and down-regulation of Bcl-2 and Bcl-xL protein expression. Treatment with SOE increased protein expression of caspase-3, -8 and -9 dose-dependently, indicating that apoptosis was through the intrinsic and extrinsic apoptotic pathways. Moreover, SOE was also effective against A549 (lung cancer, Hep G2 (hepatoma, FaDu (pharynx squamous cancer, MDA-MB-231 (breast cancer, and especially on LNCaP (prostate cancer cell lines. In total, 10 constituents of SOE were identified by Gas chromatography-mass analysis. Caryophyllene oxide and caryophyllene are largely responsible for most cytotoxic activity of SOE against RL95-2 cells. Overall, this study suggests that SOE is a promising anticancer agent for treating endometrial cancer.

  18. Insulin-sensitizing and Anti-proliferative Effects of Argania spinosa Seed Extracts

    OpenAIRE

    Samira Samane; Josette Noël; Zoubida Charrouf; Hamid Amarouch; Pierre Selim Haddad

    2006-01-01

    Argania spinosa is an evergreen tree endemic of southwestern Morocco. Many preparations have been used in traditional Moroccan medicine for centuries to treat several illnesses including diabetes. However, scientific evidence supporting these actions is lacking. Therefore, we prepared various extracts of the argan fruit, namely keel, cake and argan oil extracts, which we tested in the HTC hepatoma cell line for their potential to affect cellular insulin responses. Cell viability was measu...

  19. Anti-proliferative action of silibinin on human colon adenomatous cancer HT-29 cells.

    Science.gov (United States)

    Akhtar, Reyhan; Ali, Mohd; Mahmood, Safrunnisa; Sanyal, Sankar Nath

    2014-02-01

    Antecedentes: Silibinina un flavonoide a partir de la leche de cardo mariano (Silybum marianum) exhiben una variedad de acciones farmacológicas, incluyendo actividades anti-proliferativos y apoptóticos contra varios tipos de cánceres en animales intactos y líneas celulares de cáncer. En el presente estudio, se estudió el efecto de silibinina en células humanas de cáncer de colon HT-29. Método: Las incubaciones de las células con diferentes concentraciones silibinin (0,783-1.600 ug/ml) para 24, 48 o 72 horas mostró un descenso progresivo de la viabilidad celular. Resultados: La pérdida de la viabilidad celular fue de tiempo de inhibición dependiente y óptima de crecimiento de las células (78%) se observó a las 72 horas. Bajo microscopio invertido, las células muertas fueron vistos como los agregados de células. IC50 (concentración de silibinina matar a las células 50%) los valores fueron 180, 110 y 40 ug/ml a las 24, 48 y 72 horas, respectivamente. Conclusión: Estos resultados volver a hacer cumplir la potenciales contra el cáncer de silibinina, como se informó anteriormente para varias otras líneas celulares de cáncer (Ramasamy y Agarwal (2008), Cancer Letters, 269: 352-62).

  20. In-vitro release of anti-proliferative paclitaxel from novel balloon-expandable polycaprolactone stents

    Energy Technology Data Exchange (ETDEWEB)

    Liu, Shih-Jung, E-mail: shihjung@mail.cgu.edu.tw [Department of Mechanical Engineering, Chang Gung University, Taiwan (China); Hsiao, Chao-Ying [Department of Mechanical Engineering, Chang Gung University, Taiwan (China); Chen, Jan-Kan [Department of Physiology and Pharmacology, Chang Gung University, Taiwan (China); Liu, Kuo-Sheng [Department of Mechanical Engineering, Chang Gung University, Taiwan (China); Department of Cardiovascular Surgery, Chang Gung Memorial Hospital, Taiwan (China); Lee, Cheng-Hung [Department of Mechanical Engineering, Chang Gung University, Taiwan (China); Second Section of Cardiology, Department of Internal Medicine, Chang Gung Memorial Hospital, Taiwan (China)

    2011-07-20

    This report investigated the in-vitro release characteristics of paclitaxel from novel balloon-expandable polycaprolactone stents. Polycaprolactone stents were first manufactured by a lab-made micro-injection molding machine. Paclitaxel and polylactide-polyglycolide (PLGA) copolymer were dissolved in acetonitrile and were coated onto the surface of the stents by a spray coating device, which was designed and built especially for this study. An elution method was utilized to characterize the in-vitro release characteristics of paclitaxel. The high performance liquid chromatography (HPLC) analysis showed that biodegradable stents could provide sustained release of paclitaxel for more than 70 days. Various process parameters that controlled the release rate of paclitaxel were studied. The experimental results suggested that the total period of drug release could be prolonged by adopting 75:25 PLGA copolymers, employing multi-layer coatings, and increasing the drug loading. In addition, the effectiveness of eluted paclitaxel on cell behavior was examined. The results showed that the eluted drug could effectively inhibit the proliferation of smooth muscle cells. - Research Highlights: {yields} We investigate the in-vitro release characteristics of paclitaxel from polycaprolactone stents. {yields} Biodegradable stents provide sustained release of paclitaxel for more than 70 days. {yields} The eluted drug effectively inhibits the proliferation of smooth muscle cells.

  1. A possible anti-proliferative and anti-metastatic effect of irradiated riboflavin in solid tumours

    NARCIS (Netherlands)

    de Souza Queiroz, Karla Cristiana; Zambuzzi, Willian Fernando; de Souza, Ana Carolina Santos; da Silva, Rodrigo Augusto; Machado, Daisy; Justo, Giselle Zenker; Carvalho, Hernandes F.; Peppelenbosch, Maikel P.; Ferreira, Carmen Verissima

    2007-01-01

    Riboflavin is a potent photosensitizer as well as part of the vitamin B complex. Recently we demonstrated that the products generated by irradiation of riboflavin have potential as anti-leukaemic therapy. The possible action, however, of the riboflavin photoproducts in solid cancers has not been add

  2. Xanthones from Garcinia paucinervis with in vitro anti-proliferative activity against HL-60 cells.

    Science.gov (United States)

    Li, Da-Hong; Li, Chen-Xi; Jia, Cui-Cui; Sun, Ya-Ting; Xue, Chun-Mei; Bai, Jiao; Hua, Hui-Ming; Liu, Xiao-Qiu; Li, Zhan-Lin

    2016-02-01

    Three new xanthones, paucinervins H-J (1-3), as well as eleven known compounds (4-14), were isolated from the leaves of Garcinia paucinervis. The structures of the new compounds (1-3) were elucidated by 1D, 2D NMR spectra and HR ESIMS. In vitro antiproliferative activity against human promyelocytic leukemia HL-60 cells was tested, among which, compounds 2, 5, 6 and 7 exhibited strong growth inhibitory effects with GI50 values ranging from 1.30 to 9.08 μM, respectively. Preliminary SARs were also discussed. PMID:26659874

  3. Anti-proliferative actions of T-type calcium channel inhibition in Thy1 nephritis.

    Science.gov (United States)

    Cove-Smith, Andrea; Mulgrew, Christopher J; Rudyk, Olena; Dutt, Neelanjana; McLatchie, Linda M; Shattock, Michael J; Hendry, Bruce M

    2013-08-01

    Aberrant proliferation of mesangial cells (MCs) is a key finding in progressive glomerular disease. TH1177 is a small molecule that has been shown to inhibit low-voltage activated T-type Ca(2+) channels (TCCs). The current study investigates the effect of TH1177 on MC proliferation in vitro and in vivo. The effect of Ca(2+) channel inhibition on primary rat MC proliferation in vitro was studied using the microculture tetrazolium assay and by measuring bromodeoxyuridine incorporation. In vivo, rats with Thy1 nephritis were treated with TH1177 or vehicle. Glomerular injury and average glomerular cell number were determined in a blinded fashion. Immunostaining for Ki-67 and phosphorylated ERK were also performed. The expression of TCC isoforms in healthy and diseased tissue was investigated using quantitative real-time PCR. TCC blockade caused a significant reduction in rat MC proliferation in vitro, whereas L-type inhibition had no effect. Treatment of Thy1 nephritis with TH1177 significantly reduced glomerular injury (P < 0.005) and caused a 49% reduction in glomerular cell number (P < 0.005) compared to the placebo. TH1177 also reduced Ki-67-positive and pERK-positive cells per glomerulus by 52% (P < 0.01 and P < 0.005, respectively). These results demonstrate that TH1177 inhibits MC proliferation in vitro and in vivo, supporting the hypothesis that TCC inhibition may be a useful strategy for studying and modifying MC proliferative responses to injury. PMID:23746655

  4. Latest development of display technologies

    Science.gov (United States)

    Gao, Hong-Yue; Yao, Qiu-Xiang; Liu, Pan; Zheng, Zhi-Qiang; Liu, Ji-Cheng; Zheng, Hua-Dong; Zeng, Chao; Yu, Ying-Jie; Sun, Tao; Zeng, Zhen-Xiang

    2016-09-01

    In this review we will focus on recent progress in the field of two-dimensional (2D) and three-dimensional (3D) display technologies. We present the current display materials and their applications, including organic light-emitting diodes (OLEDs), flexible OLEDs quantum dot light emitting diodes (QLEDs), active-matrix organic light emitting diodes (AMOLEDs), electronic paper (E-paper), curved displays, stereoscopic 3D displays, volumetric 3D displays, light field 3D displays, and holographic 3D displays. Conventional 2D display devices, such as liquid crystal devices (LCDs) often result in ambiguity in high-dimensional data images because of lacking true depth information. This review thus provides a detailed description of 3D display technologies.

  5. Effect of gibberellin, auxin and kinetin treatments combined with foliar applied NPK on the yield of Capsicum annuum L. fruits and their capsaicin content

    Directory of Open Access Journals (Sweden)

    Tomasz J. Nowak

    2013-12-01

    Full Text Available The Wrocław version of hydroponic culture was applied. Under optimal conditions of root fertilization the plants were sprayed with growth regulators sueh as gibberellins, auxins and kinetins, and .their mixtures. Each growth regulator treatment was applied with or without NPK added. The influence of these treatments on the fresh and dry weight of the fruit, percentage of ripe fruits and content and yield of capsaicin was studied. The highest yield of fruits and capsaicin. was obtained from plants sprayed with gibberellic acid and kinetin (in concentrations of 10 and 5 mg/l, respectively together with NPK foliar application. No influence of ,growth regulators and foliar-applied NPK was noted on capsaicin content and dry weight of fruits.

  6. Gastro-protective action of lafutidine mediated by capsaicin-sensitive afferent neurons without interaction with TRPV1 and involvement of endogenous prostaglandins

    Institute of Scientific and Technical Information of China (English)

    Kazuhiro Fukushima; Yoko Aoi; Shinichi Kato; Koji Takeuchi

    2006-01-01

    AIM: Lafutidine, a histamine H2 receptor antagonist,exhibits gastro-protective action mediated by capsaicinsensitive afferent neurons (CSN). We compared the effect between lafutidine and capsaicin, with respect to the interaction with endogenous prostaglandins (PG), nitric oxide (NO) and the afferent neurons, including transient receptor potential vanilloid subtype 1 (TRPV1).METHODS: Male SD rats and C57BL/6 mice, both wildtype and prostacyclin IP receptor knockout animals, were used after 18 h of fasting. Gastric lesions were induced by the po administration of HCI/ethanol (60% in 150 mmol/L HCI) in a volume of 1 mL for rats or 0.3 mL for mice.RESULTS: Both lafutidine and capsaicin (1-10 mg/kg,po) afforded dose-dependent protection against HCI/ethanol in rats and mice. The effects were attenuated by both the ablation of CSN and pretreatment with NG-nitroL-arginine methyl ester, yet only the effect of capsaicin was mitigated by prior administration of capsazepine, the TRPV1 antagonist, as well as indomethacin. Lafutidine protected the stomach against HCI/ethanol in IP receptor knockout mice, similar to wild-type animals, while capsaicin failed to afford protection in the animals lacking IP receptors. Neither of these agents affected the mucosal PGE2 or 6-keto PGF1α contents in rat stomachs. Capsaicin evoked an increase in [Ca2+]i in rat TRPV1-transfected HEK293 cells while lafutidine did not.CONCLUSION: These results suggest that although both lafutidine and capsaicin exhibit gastro-protective action mediated by CSN, the mode of their effects differs regarding the dependency on endogenous PGs/IP receptors and TRPV1. It is assumed that lafutidine interacts with CSN at yet unidentified sites other than TRPV1.

  7. Phα1β toxin prevents capsaicin-induced nociceptive behavior and mechanical hypersensitivity without acting on TRPV1 channels.

    Science.gov (United States)

    Castro-Junior, Celio J; Milano, Julie; Souza, Alessandra H; Silva, Juliana F; Rigo, Flávia K; Dalmolin, Geruza; Cordeiro, Marta N; Richardson, Michael; Barros, Alexandre G A; Gomez, Renato S; Silva, Marco A R; Kushmerick, Christopher; Ferreira, Juliano; Gomez, Marcus V

    2013-08-01

    Phα1β toxin is a peptide purified from the venom of the armed spider Phoneutria nigriventer, with markedly antinociceptive action in models of acute and persistent pain in rats. Similarly to ziconotide, its analgesic action is related to inhibition of high voltage activated calcium channels with more selectivity for N-type. In this study we evaluated the effect of Phα1β when injected peripherally or intrathecally in a rat model of spontaneous pain induced by capsaicin. We also investigated the effect of Phα1β on Ca²⁺ transients in cultured dorsal root ganglia (DRG) neurons and HEK293 cells expressing the TRPV1 receptor. Intraplantar or intrathecal administered Phα1β reduced both nocifensive behavior and mechanical hypersensitivity induced by capsaicin similarly to that observed with SB366791, a specific TRPV1 antagonist. Peripheral nifedipine and mibefradil did also decrease nociceptive behavior induced by intraplantar capsaicin. In contrast, ω-conotoxin MVIIA (a selective N-type Ca²⁺ channel blocker) was effective only when administered intrathecally. Phα1β, MVIIA and SB366791 inhibited, with similar potency, the capsaicin-induced Ca²⁺ transients in DRG neurons. The simultaneous administration of Phα1β and SB366791 inhibited the capsaicin-induced Ca²⁺ transients that were additive suggesting that they act through different targets. Moreover, Phα1β did not inhibit capsaicin-activated currents in patch-clamp recordings of HEK293 cells that expressed TRPV1 receptors. Our results show that Phα1β may be effective as a therapeutic strategy for pain and this effect is not related to the inhibition of TRPV1 receptors. PMID:23597507

  8. Moderate extracellular acidification inhibits capsaicin-induced cell death through regulating calcium mobilization, NF-{kappa}B translocation and ROS production in synoviocytes

    Energy Technology Data Exchange (ETDEWEB)

    Hu, Fen; Yang, Shuang; Zhao, Dan; Zhu, Shuyan; Wang, Yuxiang [Department of Biophysics, School of Physics and Key Laboratory of Bioactive Materials of Education Ministry, Nankai University, Tianjin 300071 (China); Li, Junying, E-mail: jyli04@nankai.edu.cn [Department of Biophysics, School of Physics and Key Laboratory of Bioactive Materials of Education Ministry, Nankai University, Tianjin 300071 (China)

    2012-07-20

    Highlights: Black-Right-Pointing-Pointer Moderate extracellular acidification regulates intracellular Ca{sup 2+} mobilization. Black-Right-Pointing-Pointer Moderate acidification activates NF-{kappa}B nuclear translocation in synoviocytes. Black-Right-Pointing-Pointer Moderate acidification depresses the ROS production induced by capsaicin. Black-Right-Pointing-Pointer Moderate acidification inhibits capsaicin-caused synoviocyte death. -- Abstract: We previously show the expression of transient receptor potential vanilloid 1 (TRPV1) in primary synoviocytes from collagen-induced arthritis (CIA) rats. Capsaicin and lowered extracellular pH from 7.4 to 5.5 induce cell death through TRPV1-mediated Ca{sup 2+} entry and reactive oxygen species (ROS) production. However, under the pathological condition in rheumatoid arthritis, the synovial fluid is acidified to a moderate level (about pH 6.8). In the present study, we examined the effects of pH 6.8 on the TRPV1-mediated cell death. Our finding is different or even opposite from what was observed at pH 5.5. We found that the moderate extracellular acidification (from pH 7.4 to 6.8) inhibited the capsaicin-induced Ca{sup 2+} entry through attenuating the activity of TRPV1. In the mean time, it triggered a phospholipse C (PLC)-related Ca{sup 2+} release from intracellular stores. The nuclear translocation of NF-{kappa}B was found at pH 6.8, and this also depends on PLC activation. Moreover, the capsaicin-evoked massive ROS production and cell death were depressed at pH 6.8, both of which are dependent on the activation of PLC and NF-{kappa}B. Taken together, these results suggested that the moderate extracellular acidification inhibited the capsaicin-induced synoviocyte death through regulating Ca{sup 2+} mobilization, activating NF-{kappa}B nuclear translocation and depressing ROS production.

  9. Characterization of cardiovascular reflexes evoked by airway stimulation with allylisothiocyanate, capsaicin, and ATP in Sprague-Dawley rats.

    Science.gov (United States)

    Hooper, J S; Hadley, S H; Morris, K F; Breslin, J W; Dean, J B; Taylor-Clark, T E

    2016-03-15

    Acute inhalation of airborne pollutants alters cardiovascular function and evidence suggests that pollutant-induced activation of airway sensory nerves via the gating of ion channels is critical to these systemic responses. Here, we have investigated the effect of capsaicin [transient receptor potential (TRP) vanilloid 1 (TRPV1) agonist], AITC [TRP ankyrin 1 (TRPA1) agonist], and ATP (P2X2/3 agonist) on bronchopulmonary sensory activity and cardiovascular responses of conscious Sprague-Dawley (SD) rats. Single fiber recordings show that allyl isothiocyanate (AITC) and capsaicin selectively activate C fibers, whereas subpopulations of both A and C fibers are activated by stimulation of P2X2/3 receptors. Inhalation of the agonists by conscious rats caused significant bradycardia, atrioventricular (AV) block, and prolonged PR intervals, although ATP-induced responses were lesser than those evoked by AITC or capsaicin. Responses to AITC were inhibited by the TRP channel blocker ruthenium red and the muscarinic antagonist atropine. AITC inhalation also caused a biphasic blood pressure response: a brief hypertensive phase followed by a hypotensive phase. Atropine accentuated the hypertensive phase, while preventing the hypotension. AITC-evoked bradycardia was not abolished by terazosin, the α1-adrenoceptor inhibitor, which prevented the hypertensive response. Anesthetics had profound effects on AITC-evoked bradycardia and AV block, which was abolished by urethane, ketamine, and isoflurane. Nevertheless, AITC inhalation caused bradycardia and AV block in paralyzed and ventilated rats following precollicular decerebration. In conclusion, we provide evidence that activation of ion channels expressed on nociceptive airway sensory nerves causes significant cardiovascular effects in conscious SD rats via reflex modulation of the autonomic nervous system. PMID:26718787

  10. Differential effects of systemically administered ketamine and lidocaine on dynamic and static hyperalgesia induced by intradermal capsaicin in humans

    DEFF Research Database (Denmark)

    Gottrup, Hanne; Hansen, Peter Orm; Arendt-Nielsen, Lars;

    2000-01-01

    the area of punctate-evoked hyperalgesia significantly. It tended to reduce VAS scores of spontaneous pain but had no effect on evoked pain. The differential effects of ketamine and lidocaine on static and dynamic hyperalgesia suggest that the two types of hyperalgesia are mediated by separate mechanisms......We have examined the effect of systemic administration of ketamine and lidocaine on brush-evoked (dynamic) pain and punctate-evoked (static) hyperalgesia induced by capsaicin. In a randomized, double-blind, placebo-controlled, crossover study, we studied 12 volunteers in three experiments...

  11. Positive allosteric modulation of GABA-A receptors reduces capsaicin-induced primary and secondary hypersensitivity in rats

    DEFF Research Database (Denmark)

    Hansen, Rikke Rie; Erichsen, Helle K; Brown, David T;

    2012-01-01

    GABA-A receptor positive allosteric modulators (PAMs) mediate robust analgesia in animal models of pathological pain, in part via enhancing injury-induced loss of GABA-A-α2 and -α3 receptor function within the spinal cord. As yet, a lack of clinically suitable tool compounds has prevented this...... concept being tested in humans. Prior to assessing the efficacy of GABA-A receptor PAMs in a human volunteer pain model we have compared compounds capable of variously modulating GABA-A receptor function in comparable rat models of capsaicin-induced acute nocifensive flinching behaviour and secondary...

  12. Study on Virulence of Capsaicine against Medlar Aphids%辣椒碱对枸杞蚜虫的毒性研究

    Institute of Scientific and Technical Information of China (English)

    陈学文

    2011-01-01

    [ Objective ] The study aimed to research the insecticidal activity of capsaicine against the medlar aphids. [ Method ] The load poison blade method indoor was used to determine the virulence of capsaicin at 5 concn. series of 12.5, 25.0, 37.5, 50.0 and 62.5 mg/L against the medlar aphids in the lab. [Result] Along with the increase of capsaicin concn., the insecticidal activity of the capsaiein was enhanced markedly. When the capsaicin was 12.5 mg/L the mortality of medlar aphids reached to 66.7% , and when capsaicin was 62.5 mg/Lthe medlar aphids were all in death. Virulence regression results showed that the LC5o for capsaicin was 13.21 mg/L, explaining that the capsaicin had the good control action on the medlar aphids, so it could be instead of the current-used organophosphate and pyrethrins chemical pesticides with great toxic and high residue. [ Conclusion] This research provided a theoretical basis for the capsaicin as new green pesticide to control the medlar aphids.%[目的]研究辣椒碱对枸杞蚜虫的杀虫活性.[方法]采用载毒叶片法室内测定辣椒碱12.5、25.0、37.5、50.0、62.5 mg/L 5个浓度系列对枸杞蚜虫的毒力.[结果]随着浓度的增大,辣椒碱的杀虫活性显著增强,在浓度为12.5 mg/L时枸杞蚜虫死亡率达到66.7%,当浓度为62.5 mg/L时,试虫全部死亡毒力回归结果表明,其LC50为13.21 mg/L,说明辣椒碱具有良好的防除枸杞蚜虫的作用,可代替目前所使用的毒性大、残留量高的有机磷、除虫菊醋类化学农药.[结论]该研究为辣椒碱作为新型绿色农药,防治枸杞蚜虫提供了理论依据.

  13. Roles of TRPV1 and neuropeptidergic receptors in dorsal root reflex-mediated neurogenic inflammation induced by intradermal injection of capsaicin

    Directory of Open Access Journals (Sweden)

    Zou Xiaoju

    2007-10-01

    Full Text Available Abstract Background Acute cutaneous neurogenic inflammation initiated by activation of transient receptor potential vanilloid-1 (TRPV1 receptors following intradermal injection of capsaicin is mediated mainly by dorsal root reflexes (DRRs. Inflammatory neuropeptides are suggested to be released from primary afferent nociceptors participating in inflammation. However, no direct evidence demonstrates that the release of inflammatory substances is due to the triggering of DRRs and how activation of TRPV1 receptors initiates neurogenic inflammation via triggering DRRs. Results Here we used pharmacological manipulations to analyze the roles of TRPV1 and neuropeptidergic receptors in the DRR-mediated neurogenic inflammation induced by intradermal injection of capsaicin. The degree of cutaneous inflammation in the hindpaw that followed capsaicin injection was assessed by measurements of local blood flow (vasodilation and paw-thickness (edema of the foot skin in anesthetized rats. Local injection of capsaicin, calcitonin gene-related peptide (CGRP or substance P (SP resulted in cutaneous vasodilation and edema. Removal of DRRs by either spinal dorsal rhizotomy or intrathecal administration of the GABAA receptor antagonist, bicuculline, reduced dramatically the capsaicin-induced vasodilation and edema. In contrast, CGRP- or SP-induced inflammation was not significantly affected after DRR removal. Dose-response analysis of the antagonistic effect of the TRPV1 receptor antagonist, capsazepine administered peripherally, shows that the capsaicin-evoked inflammation was inhibited in a dose-dependent manner, and nearly completely abolished by capsazepine at doses between 30–150 μg. In contrast, pretreatment of the periphery with different doses of CGRP8–37 (a CGRP receptor antagonist or spantide I (a neurokinin 1 receptor antagonist only reduced the inflammation. If both CGRP and NK1 receptors were blocked by co-administration of CGRP8–37 and spantide I

  14. Distinct BOLD fMRI Responses of Capsaicin-Induced Thermal Sensation Reveal Pain-Related Brain Activation in Nonhuman Primates.

    Directory of Open Access Journals (Sweden)

    Abu Bakar Ali Asad

    Full Text Available Approximately 20% of the adult population suffer from chronic pain that is not adequately treated by current therapies, highlighting a great need for improved treatment options. To develop effective analgesics, experimental human and animal models of pain are critical. Topically/intra-dermally applied capsaicin induces hyperalgesia and allodynia to thermal and tactile stimuli that mimics chronic pain and is a useful translation from preclinical research to clinical investigation. Many behavioral and self-report studies of pain have exploited the use of the capsaicin pain model, but objective biomarker correlates of the capsaicin augmented nociceptive response in nonhuman primates remains to be explored.Here we establish an aversive capsaicin-induced fMRI model using non-noxious heat stimuli in Cynomolgus monkeys (n = 8. BOLD fMRI data were collected during thermal challenge (ON:20 s/42°C; OFF:40 s/35°C, 4-cycle at baseline and 30 min post-capsaicin (0.1 mg, topical, forearm application. Tail withdrawal behavioral studies were also conducted in the same animals using 42°C or 48°C water bath pre- and post- capsaicin application (0.1 mg, subcutaneous, tail.Group comparisons between pre- and post-capsaicin application revealed significant BOLD signal increases in brain regions associated with the 'pain matrix', including somatosensory, frontal, and cingulate cortices, as well as the cerebellum (paired t-test, p<0.02, n = 8, while no significant change was found after the vehicle application. The tail withdrawal behavioral study demonstrated a significant main effect of temperature and a trend towards capsaicin induced reduction of latency at both temperatures.These findings provide insights into the specific brain regions involved with aversive, 'pain-like', responses in a nonhuman primate model. Future studies may employ both behavioral and fMRI measures as translational biomarkers to gain deeper understanding of pain processing and evaluate

  15. Capsaicin Supplementation Reduces Physical Fatigue and Improves Exercise Performance in Mice

    Science.gov (United States)

    Hsu, Yi-Ju; Huang, Wen-Ching; Chiu, Chien-Chao; Liu, Yan-Lin; Chiu, Wan-Chun; Chiu, Chun-Hui; Chiu, Yen-Shuo; Huang, Chi-Chang

    2016-01-01

    Chili pepper is used as a food, seasoning and has been revered for its medicinal and health claims. It is very popular and is the most common spice worldwide. Capsaicin (CAP) is a major pungent and bioactive phytochemical in chili peppers. CAP has been shown to improve mitochondrial biogenesis and adenosine triphosphate (ATP) production. However, there is limited evidence around the effects of CAP on physical fatigue and exercise performance. The purpose of this study was to evaluate the potential beneficial effects of CAP on anti-fatigue and ergogenic functions following physiological challenge. Female Institute of Cancer Research (ICR) mice from four groups (n = 8 per group) were orally administered CAP for 4 weeks at 0, 205, 410, and 1025 mg/kg/day, which were respectively designated the vehicle, CAP-1X, CAP-2X, and CAP-5X groups. The anti-fatigue activity and exercise performance was evaluated using forelimb grip strength, exhaustive swimming time, and levels of serum lactate, ammonia, glucose, BUN (blood urea nitrogen) and creatine kinase (CK) after a 15-min swimming exercise. The grip strength and exhaustive swimming time of the CAP-5X group were significantly higher than other groups. CAP supplementation dose-dependently reduced serum lactate, ammonia, BUN and CK levels, and increased glucose concentration after the 15-min swimming test. In addition, CAP also increased hepatic glycogen content, an important energy source for exercise. The possible mechanism was relevant to energy homeostasis and the physiological modulations by CAP supplementation. Therefore, our results suggest that CAP supplementation may have a wide spectrum of bioactivities for promoting health, performance improvement and fatigue amelioration. PMID:27775591

  16. Display Factors and Subjective Evaluation of Dynamic Text Display

    Science.gov (United States)

    So, Joey C. Y.; Chan, Alan H. S.

    2009-01-01

    Communications technology has exploded in past decades, leading to the question of which display method is the best to deliver electronic text messages. Many of these systems employ cathode ray tubes, liquid crystal displays, gas plasma displays, or light-emitting diodes as the output device. In order to overcome the limitations of screen size of the display units, numerous means of presenting dynamic display on screens have been invented. There are many factors that affect the readability of electronic text. This paper reviews some related empirical studies concerning the various display methods of dynamic text presentation, such as text display type, character type, text display direction, and text/background color combination, highlighting method and validity of highlighting. The subjective evaluation questionnaire is also discussed. According to the readability and preference ratings of the subjects given under different conditions, the best display method and color for comprehending the delivered messages were investigated. General recommendations of displaying dynamic information are made for the large display units which have been widely used for delivering important messages.

  17. Digital holography display (3)

    Science.gov (United States)

    Lee, Cheok Peng; Zheng, Huadong; Chia, Yong Poo; Cheng, Chee Yuen; Yu, Yang; Yu, Yingjie; Asundi, Anand

    2013-06-01

    This paper is to describe a color digital holographic projector and this system is comprised of RGB lasers, 3 units of Digital Micro-Mirror Device (DMD) and high speed rotating diffuser. In this research, we focused on colorings Digital holograms and synchronized RGB digital holograms versus rotated diffuser. To achieve this phenomenon, three of the holograms optical path need to be aligned to pass through a same beam splitter and eventually combined as one colored holograms output While, this colored hologram will be reconstructed on volumetric screen (rotated diffuser) at the floating manner in free space. To obtain these result 3 key factors is investigated: 1. To configured 1 master and 2 slaves digital micro mirror illumination time 2. To reconstructed holograms orientation angle diffuser versus rotating speed. 3. To synchronize rotating diffuser speed versus DMD frame-rate Last but not least, the team built a prototype Color Digital Holography Display but more developments are required to follow up such as, enhance system's reliability, robustness, compactness and 3D realistic images floating in the free air space.

  18. LHCb Event display

    CERN Document Server

    Trisovic, Ana

    2014-01-01

    The LHCb Event Display was made for educational purposes at the European Organization for Nuclear Research, CERN in Geneva, Switzerland. The project was implemented as a stand-alone application using C++ and ROOT, a framework developed by CERN for data analysis. This paper outlines the development and architecture of the application in detail, as well as the motivation for the development and the goals of the exercise. The application focuses on the visualization of events recorded by the LHCb detector, where an event represents a set of charged particle tracks in one proton-proton collision. Every particle track is coloured by its type and can be selected to see its essential information such as mass and momentum. The application allows students to save this information and calculate the invariant mass for any pair of particles. Furthermore, the students can use additional calculating tools in the application and build up a histogram of these invariant masses. The goal for the students is to find a $D^0$ par...

  19. Unique interactive projection display screen

    Energy Technology Data Exchange (ETDEWEB)

    Veligdan, J.T.

    1997-11-01

    Projection systems continue to be the best method to produce large (1 meter and larger) displays. However, in order to produce a large display, considerable volume is typically required. The Polyplanar Optic Display (POD) is a novel type of projection display screen, which for the first time, makes it possible to produce a large projection system that is self-contained and only inches thick. In addition, this display screen is matte black in appearance allowing it to be used in high ambient light conditions. This screen is also interactive and can be remotely controlled via an infrared optical pointer resulting in mouse-like control of the display. Furthermore, this display need not be flat since it can be made curved to wrap around a viewer as well as being flexible.

  20. Antioxidant and iron-binding properties of curcumin, capsaicin, and S-allylcysteine reduce oxidative stress in rat brain homogenate.

    Science.gov (United States)

    Dairam, Amichand; Fogel, Ronen; Daya, Santy; Limson, Janice L

    2008-05-14

    Research demonstrates that antioxidants and metal chelators may be of beneficial use in the treatment of neurodegenerative diseases, such as Alzheimer's disease (AD). This study investigated the antioxidant and metal-binding properties of curcumin, capsaicin, and S-allylcysteine, which are major components found in commonly used dietary spice ingredients turmeric, chilli, and garlic, respectively. The DPPH assay demonstrates that these compounds readily scavenge free radicals. These compounds significantly curtail iron- (Fe2+) and quinolinic acid (QA)-induced lipid peroxidation and potently scavenge the superoxide anion generated by 1 mM cyanide in rat brain homogenate. The ferrozine assay was used to measure the extent of Fe2+ chelation, and electrochemistry was employed to measure the Fe3+ binding activity of curcumin, capsaicin, and S-allylcysteine. Both assays demonstrate that these compounds bind Fe2+ and Fe3+ and prevent the redox cycling of iron, suggesting that this may be an additional method through which these agents reduce Fe2+-induced lipid peroxidation. This study demonstrates the antioxidant and metal-binding properties of these spice ingredients, and it is hereby postulate that these compounds have important implications in the prevention or treatment of neurodegenerative diseases such as AD.

  1. Sputtering effect of low-energy ions on biological target: The analysis of sputtering product of urea and capsaicin

    Energy Technology Data Exchange (ETDEWEB)

    Zhang, Lili [Key Laboratory of Ion Beam Bio-Engineering, Institute of Technical Biology and Agriculture Engineering of Chinese Academy of Sciences, Shushanhu Road 350, Hefei 230031 (China); Xu, Xue [Rice Research Institute, Anhui Academy of Agricultural Sciences, Nongke South Road 40, Hefei 230031 (China); Wu, Yuejin, E-mail: yjwu@ipp.ac.cn [Key Laboratory of Ion Beam Bio-Engineering, Institute of Technical Biology and Agriculture Engineering of Chinese Academy of Sciences, Shushanhu Road 350, Hefei 230031 (China)

    2013-08-01

    Sputtering is a process whereby atoms are ejected from a solid target material due to bombardment of the target by energetic particles. Recent years, ion implantation was successfully applied to biological research based on the fragments sputtering and form open paths in cell structure caused by ion sputtering. In this study, we focused on urea and chilli pepper pericarp samples implanted with N{sup +} and Ar{sup +} ions. To investigate the sputtering effect, we designed a collecting unit containing a disk sample and a glass pipe. The urea content and capsaicin content recovered from glass pipes were adopted to represent the sputtering product. The result of urea showed that the sputtering effect is positively correlated with the ion energy and dose, also affected by the ion type. The result of capsaicin was different from that of urea at 20 keV and possibly due to biological complex composition and structure. Therefore the sputtering yield depended on both the parameters of incident ions and the state of target materials. The sputtering yield of urea was also simulated by computational method achieved through the TRIM program. The trajectories of primary and recoiled atoms were calculated on the basis of the binary collision approximation using Monte Carlo method. The experimental results were much higher than the calculated results. The possible explanation is that in the physical model the target were assumed as a disordered lattice and independent atoms, which is much less complicated than that of the biological models.

  2. The effects of capsaicin and capsaicinoid analogs on metabolic molecular targets in highly energetic tissues and cell types.

    Science.gov (United States)

    Gannon, Nicholas P; Lambalot, Emily L; Vaughan, Roger A

    2016-05-01

    There is increasing interest in dietary chemicals that may provide benefits for pathologies such as diabetes and obesity. Capsaicinoids found in chili peppers and pepper extracts, are responsible for the "hot" or "spicy" sensation associated with these foods. Capsaicinoid consumption is also associated with enhanced metabolism, making them potentially therapeutic for metabolic disease by promoting weight loss. This review summarizes much of the current experimental evidence (ranging from basic to applied investigations) of the biochemical and molecular metabolic effects of capsaicinoids in metabolically significant cell types. Along with influencing metabolic rate, findings demonstrate capsaicinoids appear to alter molecular metabolic signaling, regulate hunger and satiety, blood metabolites, and catecholamine release. Notably, the majority of the experiments summarized herein utilized isolated supplemental or research grade capsaicinoids rather than natural food sources for experimental interventions. Additional work should be conducted using primary food sources of capsaicin to explore pharmacological, physiological, and metabolic benefits of both chronic and acute capsaicin consumption. © 2016 BioFactors, 42(3):229-246, 2016. PMID:26945685

  3. Display blocks: cubic displays for multi-perspective visualization

    OpenAIRE

    Pla i Conesa, Pol; Maes, Patricia

    2012-01-01

    We propose the design, implementation and evaluation of a set of tangible cubic displays. This novel approach to display technology consists of arranging six organic light emitting diode screens in a cubic form factor. We explore the possibilities that this type of display holds for data visualization, manipulation and exploration. We are especially interested in exploring how the physicality of the screen can be perceived as a cue to better interpret its contents. To this end, we propose a s...

  4. Augmenting digital displays with computation

    Science.gov (United States)

    Liu, Jing

    As we inevitably step deeper and deeper into a world connected via the Internet, more and more information will be exchanged digitally. Displays are the interface between digital information and each individual. Naturally, one fundamental goal of displays is to reproduce information as realistically as possible since humans still care a lot about what happens in the real world. Human eyes are the receiving end of such information exchange; therefore it is impossible to study displays without studying the human visual system. In fact, the design of displays is rather closely coupled with what human eyes are capable of perceiving. For example, we are less interested in building displays that emit light in the invisible spectrum. This dissertation explores how we can augment displays with computation, which takes both display hardware and the human visual system into consideration. Four novel projects on display technologies are included in this dissertation: First, we propose a software-based approach to driving multiview autostereoscopic displays. Our display algorithm can dynamically assign views to hardware display zones based on multiple observers' current head positions, substantially reducing crosstalk and stereo inversion. Second, we present a dense projector array that creates a seamless 3D viewing experience for multiple viewers. We smoothly interpolate the set of viewer heights and distances on a per-vertex basis across the arrays field of view, reducing image distortion, crosstalk, and artifacts from tracking errors. Third, we propose a method for high dynamic range display calibration that takes into account the variation of the chrominance error over luminance. We propose a data structure for enabling efficient representation and querying of the calibration function, which also allows user-guided balancing between memory consumption and the amount of computation. Fourth, we present user studies that demonstrate that the ˜ 60 Hz critical flicker fusion

  5. Advanced poly-LED displays

    Science.gov (United States)

    Childs, Mark; Nisato, Giovanni; Fish, D.; Giraldo, Andrea; Jenkins, A. J.; Johnson, Mark T.

    2003-05-01

    Philips have been actively developing polymer OLED (poly-LED) displays as a future display technology. Their emissive nature leads to a very attractive visual appearance, with wide viewing angle, high brightness and fast response speed. Whilst the first generation of poly-LED displays are likely to be passive-matrix driven, power reduction and resolution increase will lead to the use of active-matrix poly-LED displays. Philips Research have designed, fabricated and characterized five different designs of active-matrix polymer-LED display. Each of the five displays makes use of a distinct pixel programming- or pixel drive-technique, including current programming, threshold voltage measurement and photodiode feedback. It will be shown that hte simplest voltage-programmed current-source pixel suffers from potentially unacceptable brightness non-uniformity, and that advanced pixel circuits can provide a solution to this. Optical-feedback pixel circuits will be discussed, showing that they can be used to improve uniformity and compensate for image burn-in due to polymer-LED material degradation, improving display lifetime. Philips research has also been active in developing technologies required to implement poly-LED displays on flexible substrates, including materials, processing and testing methods. The fabrication of flexible passive-matrix poly-LED displays will be presented, as well as the ongoing work to assess the suitability of processing flexible next-generation poly-LED displays.

  6. Military display market segment: helicopters

    Science.gov (United States)

    Desjardins, Daniel D.; Hopper, Darrel G.

    2004-09-01

    The military display market is analyzed in terms of one of its segments: helicopter displays. Parameters requiring special consideration, to include luminance ranges, contrast ratio, viewing angles, and chromaticity coordinates, are examined. Performance requirements for rotary-wing displays relative to several premier applications are summarized. Display sizes having aggregate defense applications of 5,000 units or greater and having DoD applications across 10 or more platforms, are tabulated. The issue of size commonality is addressed where distribution of active area sizes across helicopter platforms, individually, in groups of two through nine, and ten or greater, is illustrated. Rotary-wing displays are also analyzed by technology, where total quantities of such displays are broken out into CRT, LCD, AMLCD, EM, LED, Incandescent, Plasma and TFEL percentages. Custom, versus Rugged commercial, versus commercial off-the-shelf designs are contrasted. High and low information content designs are identified. Displays for several high-profile military helicopter programs are discussed, to include both technical specifications and program history. The military display market study is summarized with breakouts for the helicopter market segment. Our defense-wide study as of March 2004 has documented 1,015,494 direct view and virtual image displays distributed across 1,181 display sizes and 503 weapon systems. Helicopter displays account for 67,472 displays (just 6.6% of DoD total) and comprise 83 sizes (7.0% of total DoD) in 76 platforms (15.1% of total DoD). Some 47.6% of these rotary-wing applications involve low information content displays comprising just a few characters in one color; however, as per fixed-wing aircraft, the predominant instantiation involves higher information content units capable of showing changeable graphics, color and video.

  7. Tolerability of the capsaicin 8% patch following pretreatment with lidocaine or tramadol in patients with peripheral neuropathic pain: A multicentre, randomized, assessor-blinded study

    NARCIS (Netherlands)

    Jensen, T.S.; Hoye, K.; Fricova, J.; Vanelderen, P.J.L.; Ernault, E.; Siciliano, T.; Marques, S.

    2014-01-01

    BACKGROUND: Application of the capsaicin 8% patch is associated with treatment-related discomfort. Consequently, pretreatment for 60 min with anaesthetic cream is recommended; however, this may be uncomfortable and time consuming. METHODS: We conducted a multicentre, randomized (1:1), assessor-blind

  8. Involvement of a CCK-dependent capsaicin-sensitive afferent pathway in the inhibitory effect of pinaverium bromide on the colonic motor response to eating in rats.

    Science.gov (United States)

    Fioramonti, J; Christen, M O; Dupre, I; Bueno, L

    1997-01-01

    The effects of pinaverium bromide on the stimulation of colonic motility induced by meal and cholecystokinin (CCK) were investigated in rats chronically fitted with intraparietal electrodes on the proximal colon and previously treated or not by capsaicin. Pinaverium bromide inhibited in a dose-related manner (2-50 mg/kg, per os) the increase in colonic spike burst frequency induced by a 3 g meal or CCK-8 (2 micrograms/kg, i.v.). The CCK-A and CCK-B antagonists, devazepide and L 365260 (100 micrograms/kg, i.p.), respectively, inhibited the postprandial colonic motor response while only L 365260 reduced the CCK-induced stimulation. The effects of pinaverium bromide and CCK antagonists were not observed in capsaicin-treated animals. Moreover, CCK-8 (2 micrograms/kg, i.v.) did not stimulate colonic motility after capsaicin treatment. The inhibition of postprandial colonic motility by pinaverium bromide, given orally at therapeutic doses, involves a CCK-dependent pathway which requires the integrity of capsaicin-sensitive afferents. PMID:9243254

  9. OLED displays for military applications

    Science.gov (United States)

    Mahon, Janice K.; Brown, Julie J.; Hack, Michael G.; Hewitt, Richard H.; Huffman, David C.

    2000-08-01

    Through the years, there has been a steady evolution of technology to ruggedize displays for harsh military environments. This work has spanned cathode-ray-tubes (CRTs) to present day active matrix liquid crystal displays (AMLCDs). Organic light emitting device (OLED) display technology has the potential to solve many of the inherent limitations of today's AMLCD technology and to provide the military system designer with a more cost effective solution. OLED technology offers bright, colorful emissive light with excellent power efficiency, wide viewing angle and video response rates; it is also demonstrating the requisite environmental robustness for a wide variety of display applications. OLED displays also have a very thin and lightweight form factor. Moreover, in full production, OLEDs are projected to be very cost-effective by comparison to AMLCDs. This paper will examine some of these advantages and the opportunities presented by the rapidly emerging OLED display technology for military applications.

  10. Laser illuminated flat panel display

    Energy Technology Data Exchange (ETDEWEB)

    Veligdan, J.T.

    1995-12-31

    A 10 inch laser illuminated flat panel Planar Optic Display (POD) screen has been constructed and tested. This POD screen technology is an entirely new concept in display technology. Although the initial display is flat and made of glass, this technology lends itself to applications where a plastic display might be wrapped around the viewer. The display screen is comprised of hundreds of planar optical waveguides where each glass waveguide represents a vertical line of resolution. A black cladding layer, having a lower index of refraction, is placed between each waveguide layer. Since the cladding makes the screen surface black, the contrast is high. The prototype display is 9 inches wide by 5 inches high and approximately I inch thick. A 3 milliwatt HeNe laser is used as the illumination source and a vector scanning technique is employed.

  11. Liquid crystal Fresnel lens display

    Science.gov (United States)

    Wang, Xiao-Qian; Abhishek Kumar, Srivastava; Alwin Tam, Ming-Wai; Zheng, Zhi-Gang; Shen, Dong; Vladimir, Chigrinov G.; Kwok, Hoi-Sing

    2016-09-01

    A novel see-through display with a liquid crystal lens array was proposed. A liquid crystal Fresnel lens display (LCFLD) with a holographic screen was demonstrated. The proposed display system has high efficiency, simple fabrication, and low manufacturing cost due to the absence of a polarizer and color filter. Project supported by Partner State Key Laboratory on Advanced Displays and Optoelectronics Technologies HKUST, China, the National Natural Science Foundation of China (Grant Nos. 61435008 and 61575063), and the Fundamental Research Funds for the Central Universities, China (Grant No. WM1514036).

  12. Maintenance Procedure Display: Head Mounted Display (HMD) Evaluations

    Science.gov (United States)

    Whitmore, Milrian; Litaker, Harry L., Jr.; Solem, Jody A.; Holden, Kritina L.; Hoffman, Ronald R.

    2007-01-01

    A viewgraph presentation describing maintenance procedures for head mounted displays is shown. The topics include: 1) Study Goals; 2) Near Eye Displays (HMDs); 3) Design; 4) Phase I-Evaluation Methods; 5) Phase 1 Results; 6) Improved HMD Mounting; 7) Phase 2 -Evaluation Methods; 8) Phase 2 Preliminary Results; and 9) Next Steps.

  13. The μ opioid agonist morphine modulates potentiation of capsaicin-evoked TRPV1 responses through a cyclic AMP-dependent protein kinase A pathway

    Directory of Open Access Journals (Sweden)

    Roberts-Thomson Sarah J

    2006-07-01

    Full Text Available Abstract Background The vanilloid receptor 1 (TRPV1 is critical in the development of inflammatory hyperalgesia. Several receptors including G-protein coupled prostaglandin receptors have been reported to functionally interact with the TRPV1 through a cAMP-dependent protein kinase A (PKA pathway to potentiate TRPV1-mediated capsaicin responses. Such regulation may have significance in inflammatory pain. However, few functional receptor interactions that inhibit PKA-mediated potentiation of TRPV1 responses have been described. Results In the present studies we investigated the hypothesis that the μ opioid receptor (MOP agonist morphine can modulate forskolin-potentiated capsaicin responses through a cAMP-dependent PKA pathway. HEK293 cells were stably transfected with TRPV1 and MOP, and calcium (Ca2+ responses to injection of the TRPV1 agonist capsaicin were monitored in Fluo-3-loaded cells. Pre-treatment with morphine did not inhibit unpotentiated capsaicin-induced Ca2+ responses but significantly altered capsaicin responses potentiated by forskolin. TRPV1-mediated Ca2+ responses potentiated by the direct PKA activator 8-Br-cAMP and the PKC activator Phorbol-12-myristate-13-acetatewere not modulated by morphine. Immunohistochemical studies confirmed that the TRPV1 and MOP are co-expressed on cultured Dorsal Root Ganglion neurones, pointing towards the existence of a functional relationship between the G-protein coupled MOP and nociceptive TRPV1. Conclusion The results presented here indicate that the opioid receptor agonist morphine acts via inhibition of adenylate cyclase to inhibit PKA-potentiated TRPV1 responses. Targeting of peripheral opioid receptors may therefore have therapeutic potential as an intervention to prevent potentiation of TRPV1 responses through the PKA pathway in inflammation.

  14. RPF151, a novel capsaicin-like analogue: in vitro studies and in vivo preclinical antitumor evaluation in a breast cancer model.

    Science.gov (United States)

    Ferreira, Adilson Kleber; Tavares, Maurício Temotheo; Pasqualoto, Kerly Fernanda Mesquita; de Azevedo, Ricardo Alexandre; Teixeira, Sarah Fernandes; Ferreira-Junior, Wilson Alves; Bertin, Ariane Matiello; de-Sá-Junior, Paulo Luiz; Barbuto, José Alexandre Marzagão; Figueiredo, Carlos Rogério; Cury, Yara; Damião, Mariana Celestina Frojuello Costa Bernstorff; Parise-Filho, Roberto

    2015-09-01

    Capsaicin, the primary pungent component of the chili pepper, has antitumor activity. Herein, we describe the activity of RPF151, an alkyl sulfonamide analogue of capsaicin, against MDA-MB-231 breast cancer cells. RPF151 was synthetized, and molecular modeling was used to compare capsaicin and RPF151. Cytotoxicity of RPF151 on MDA-MB-231 was also evaluated by the 3-[4,5-dimethylthiazol-2-yl]-2,5diphenyltetrazolium bromide (MTT) assay. Cell cycle analysis, by flow cytometry, and Western blot analysis of cycle-related proteins were used to evaluate the antiproliferative mechanisms. Apoptosis was evaluated by phosphatidyl-serine externalization, cleavage of Ac-YVAD-AMC, and Bcl-2 expression. The production of reactive oxygen species was evaluated by flow cytometry. RPF151 in vivo antitumor effects were investigated in murine MDA-MB-231 model. This study shows that RPF151 downregulated p21 and cyclins A, D1, and D3, leading to S-phase arrest and apoptosis. Although RPF151 has induced the activation of TRPV-1 and TRAIL-R1/DR4 and TRAIL-2/DR5 on the surface of MDA-MB-231 cells, its in vivo antitumor activity was TRPV-1-independent, thus suggesting that RPF151 should not have the same pungency-based limitation of capsaicin. In silico analysis corroborated the biological findings, showing that RPF151 has physicochemical improvements over capsaicin. Overall, the activity of RPF151 against MDA-MB-231 and its lower pungency suggest that it may have a relevant role in cancer therapy. PMID:25894379

  15. Updated defense display market assessment

    Science.gov (United States)

    Desjardins, Daniel D.; Hopper, Darrel G.

    1999-08-01

    This paper addresses the number, function and size of principal military displays and establishes a basis to determine the opportunities for technology insertion in the immediate future and into the next millennium. Principal military displays are defined as those occupying appreciable crewstation real-estate and/or those without which the platform could not carry out its intended mission. DoD 'office' applications are excluded from this study. The military displays market is specified by such parameters as active area and footprint size, and other characteristics such as luminance, gray scale, resolution, angle, color, video capability, and night vision imaging system compatibility. Funded, future acquisitions, planned and predicted crewstation modification kits, and form-fit upgrades are taken into account. This paper provides an overview of the DoD niche market, allowing both government and industry a necessary reference by which to meet DoD requirements for military displays in a timely and cost-effective manner. The aggregate DoD installed base for direct-view and large-area military displays is presently estimated to be in excess of 313,000. Miniature displays are those which must be magnified to be viewed, involve a significantly different manufacturing paradigm and are used in helmet mounted displays and thermal weapon sight applications. Some 114,000 miniature displays are presently included within future weapon system acquisition plans. For vendor production planning purposes it is noted that foreign military sales could substantially increase these quantities. The vanishing vendor syndrome (VVS) for older display technologies continues to be a growing, pervasive problem throughout DoD, which consequently must leverage the more modern, especially flat panel, display technologies being developed to replace older, especially cathode ray tube, technology for civil-commercial markets. Total DoD display needs (FPD, HMD) are some 427,000.

  16. Role of capsaicin-sensitive C-fiber afferents in neuropathic pain-induced synaptic potentiation in the nociceptive amygdala

    Directory of Open Access Journals (Sweden)

    Nakao Ayano

    2012-07-01

    Full Text Available Abstract Background Neurons in the capsular part of the central nucleus of the amygdala (CeC, a region also called "nociceptive amygdala," receive nociceptive information from the dorsal horn via afferent pathways relayed from the lateral parabrachial nucleus (LPB. As the central amygdala is known to be involved in the acquisition and expression of emotion, this pathway is thought to play central roles in the generation of affective responses to nociceptive inputs. Excitatory synaptic transmission between afferents arising from the LPB and these CeC neurons is potentiated in arthritic, visceral, neuropathic, inflammatory and muscle pain models. In neuropathic pain models following spinal nerve ligation (SNL, in which we previously showed a robust LPB-CeC potentiation, the principal behavioral symptom is tactile allodynia triggered by non-C-fiber low-threshold mechanoreceptor afferents. Conversely, recent anatomical studies have revealed that most of the spinal neurons projecting to the LPB receive C-fiber afferent inputs. Here, we examined the hypothesis that these C-fiber-mediated inputs are necessary for the full establishment of robust synaptic potentiation of LPB-CeC transmission in the rats with neuropathic pain. Results Postnatal capsaicin treatment, which has been shown to denervate the C-fibers expressing transient receptor potential vanilloid type-1 (TRPV1 channels, completely abolished eye-wiping responses to capsaicin eye instillation in rats, but this treatment did not affect mechanical allodynia in the nerve-ligated animals. However, the postnatal capsaicin treatment prevented LPB-CeC synaptic potentiation after SNL, unlike in the vehicle-treated rats, primarily due to the decreased incidence of potentiated transmission by elimination of TRPV1-expressing C-fiber afferents. Conclusions C-fiber-mediated afferents in the nerve-ligated animals may be a required facilitator of the establishment of nerve injury-evoked synaptic

  17. Capsaicin increases sensation of fullness in energy balance, and decreases desire to eat after dinner in negative energy balance.

    Science.gov (United States)

    Janssens, Pilou L H R; Hursel, Rick; Westerterp-Plantenga, Margriet S

    2014-06-01

    Addition of capsaicin (CAPS) to the diet has been shown to increase satiety; therefore, CAPS is of interest for anti-obesity therapy. We investigated the effects of CAPS on appetite profile and ad libitum energy intake in relation to energy balance. Fifteen subjects (seven women and eight men, age: 29.7 ± 10.8yrs, BMI: 23.3 ± 2.9 kg/m(2)) underwent four conditions in a randomized crossover design in 36 hour sessions in a respiration chamber; they received 100% of their daily energy requirements in the conditions "100%Control" and "100%CAPS", and 75% of their daily energy requirements in the conditions "75%Control" and "75%CAPS", followed by an ad libitum dinner. In the 100%CAPS and 75%CAPS conditions, CAPS was given at a dose of 2.56 mg (1.03 g of red chili pepper, 39,050 Scoville heat units) with every meal. Satiety (P < 0.05) and fullness (P = 0.01) were measured every waking hour and before and after every meal using visual analogue scales, and were higher in the 100%CAPS versus 100%Control condition. After dinner desire to eat, satiety and fullness did not differ between 75%CAPS and 100%Control, while desire to eat was higher (P < 0.05) and satiety (P = 0.06) and fullness (P = 0.06) tended to be lower in the 75%Control versus 100%Control condition. Furthermore, ad libitum intake (P = 0.07) and overconsumption (P = 0.06) tended to decrease in 100%CAPS versus 100%Control. In energy balance, addition of capsaicin to the diet increases satiety and fullness, and tends to prevent overeating when food intake is ad libitum. After dinner, capsaicin prevents the effects of the negative energy balance on desire to eat. PMID:24630935

  18. Flexible Bistable Cholesteric Reflective Displays

    Science.gov (United States)

    Yang, Deng-Ke

    2006-03-01

    Cholesteric liquid crystals (ChLCs) exhibit two stable states at zero field condition-the reflecting planar state and the nonreflecting focal conic state. ChLCs are an excellent candidate for inexpensive and rugged electronic books and papers. This paper will review the display cell structure,materials and drive schemes for flexible bistable cholesteric (Ch) reflective displays.

  19. Flat panel display - Impurity doping technology for flat panel displays

    Energy Technology Data Exchange (ETDEWEB)

    Suzuki, Toshiharu [Advanced Technology Planning, Sumitomo Eaton Nova Corporation, SBS Tower 9F, 10-1, Yoga 4-chome, Setagaya-ku, 158-0097 Tokyo (Japan)]. E-mail: suzuki_tsh@senova.co.jp

    2005-08-01

    Features of the flat panel displays (FPDs) such as liquid crystal display (LCD) and organic light emitting diode (OLED) display, etc. using low temperature poly-Si (LTPS) thin film transistors (TFTs) are briefly reviewed comparing with other FPDs. The requirements for fabricating TFTs used for high performance FPDs and system on glass (SoG) are addressed. This paper focuses on the impurity doping technology, which is one of the key technologies together with crystallization by laser annealing, formation of high quality gate insulator and gate-insulator/poly-Si interface. The issues to be solved in impurity doping technology for state of the art and future TFTs are clarified.

  20. INFORMATION DISPLAY: CONSIDERATIONS FOR DESIGNING COMPUTER-BASED DISPLAY SYSTEMS.

    Energy Technology Data Exchange (ETDEWEB)

    O' HARA,J.M.; PIRUS,D.; BELTRATCCHI,L.

    2004-09-19

    This paper discussed the presentation of information in computer-based control rooms. Issues associated with the typical displays currently in use are discussed. It is concluded that these displays should be augmented with new displays designed to better meet the information needs of plant personnel and to minimize the need for interface management tasks (the activities personnel have to do to access and organize the information they need). Several approaches to information design are discussed, specifically addressing: (1) monitoring, detection, and situation assessment; (2) routine task performance; and (3) teamwork, crew coordination, collaborative work.

  1. Flat panel display - Impurity doping technology for flat panel displays

    International Nuclear Information System (INIS)

    Features of the flat panel displays (FPDs) such as liquid crystal display (LCD) and organic light emitting diode (OLED) display, etc. using low temperature poly-Si (LTPS) thin film transistors (TFTs) are briefly reviewed comparing with other FPDs. The requirements for fabricating TFTs used for high performance FPDs and system on glass (SoG) are addressed. This paper focuses on the impurity doping technology, which is one of the key technologies together with crystallization by laser annealing, formation of high quality gate insulator and gate-insulator/poly-Si interface. The issues to be solved in impurity doping technology for state of the art and future TFTs are clarified

  2. BES monitoring and displaying system

    International Nuclear Information System (INIS)

    BES Monitoring and Displaying System (BESMDS) is projected to monitor and display the running status of DAQ and Slow Control systems of BES through the Web for worldwide accessing. It provides a real-time remote means of monitoring as well as an approach to study the environmental influence upon physical data taking. The system collects real-time data separately from BES Online subsystems by network sockets and stores the data into a database. People can access the system through its web site, which retrieves data on request from the database and can display results in dynamically reacted images. Its web address is http://besmds.ihep.ac.cn/

  3. 聚乳酸-辣椒素微胶囊的制备及性能%Preparation and Properties Research on the Microcapsules of PLA Coated Capsaicin

    Institute of Scientific and Technical Information of China (English)

    王锦成; 陈思浩; 徐子成; 徐楠; 潘鑫辰

    2011-01-01

    [Aims] The intensively pungent odor of the capsaicin is not only uncomfortable for the operator in the applied process but also its efficiency decreases for its quick release properties in a given environment. The preparation and properties research on the microcapsules of PLA coated capsaicin was carried out. [Methods] The microcapsule of capsaicin was prepared with polylactic acid (PLA) wall and capsaicin core by the solvent evaporation process. [Results] FTIR analysis showed that the capsaicin was covered successfully with the PLA resin. SEM and laser particle size methods revealed that the particle size of the microcapsule was in the range of 3-5 um. Thermal analysis illustrated that the melting point and thermal stability of the microcapsules was improved within a certain range. [Conclusions] Thus, the application field of the microcapsulated capsaicin may be expanded.%[目的]辣椒素具有强烈辛辣味而不利于生产者的操作,另外其持效性较差.微胶囊技术有利于克服这些缺点,对聚乳酸-辣椒素微胶囊的制备及性能进行了研究.[方法]以聚乳酸为囊壁、辣椒素为囊芯,采用溶剂挥发法制备了微胶囊化辣椒素.[结果]红外光谱分析表明聚乳酸已包覆到辣椒素上;扫描电镜和激光法粒径分布证明微胶囊化辣椒素的粒径范围为3~5 μm;差示扫描量热法和热失重法分析表明包覆聚乳酸后的辣椒素的熔融及热稳定性能在一定范围内得到了提高.[结论]经聚乳酸微胶囊化后的辣椒素的应用范围可得到进一步的拓展.

  4. 辣椒素对储粮害虫防治效果研究%Study on the effect of capsaicin in pests preventing for grain storage

    Institute of Scientific and Technical Information of China (English)

    欧阳建勋; 刘营营; 李忠海; 夏延斌; 罗凤莲; 王达能; 伍湘东; 项伟

    2012-01-01

    With 2% capsaicin ethanol solution sprayed on cargo rice e-venly, the effect was studied of capsaicin in Sitophilus zeamais and Tribolium castaneum preventing for grain storage. The results showed that according to the ratio of capsaicin to cargo rice 4 g/kg and 2 g/kg, Sitophilus zeamais and Tribolium castaneum appeared distinctly refusing feed effect. The damage rate of cargo rice in 30 days caused by Sitophilus zeamais were only 26. 4% and 35. 4% to that of blank controls, similarly Tribolium castaneum caused damage rate only 24. 8% and 30. 6% to that of blank controls. The reproduction number caused by Sitophilus zeamais and Tribolium castaneum was only 9. 23% and 26. 1 % of blank control, according to 0. 5 g capsaicin per 1 000 g cargo rice. When adding capsaicin 2 g per 1 000 g cargo rice, Sitophilus zeamais lived only 1 and Tribolium castaneum zero survived. The result showed that capsaicin had obvious reproduction effect on tested pests.%以2%辣椒素乙醇溶液均匀喷雾添加于糙米,研究辣椒素对储粮害虫玉米象和赤拟谷盗的拒食和增殖作用.结果表明:辣椒素添加量为4,2 g/kg·糙米时,玉米象和赤拟谷盗表现出明显的拒食现象,30 d内糙米的因虫损失率,玉米象两个浓度处理组仅为空白对照的26.4%和35.4%;赤拟谷盗处理组仅为空白对照的24.8%和30.6%;辣椒素的添加剂量为0.5 g/kg·糙米时,玉米象组、赤拟谷盗组增殖数量分别为空白组的9.23%,26.1%;辣椒素的添加剂量为2 g/kg·糙米时,玉米象组存活数仅1头,赤拟谷盗存活数为0.辣椒素的添加使玉米象和赤拟谷盗的增殖受到了明显抑制.

  5. Ultraminiature, Micropower Multipurpose Display Project

    Data.gov (United States)

    National Aeronautics and Space Administration — High information content electronic displays remain the most difficult element of the human-machine interface to effectively miniaturize. Mobile applications need a...

  6. Ten inch Planar Optic Display

    Energy Technology Data Exchange (ETDEWEB)

    Beiser, L. [Beiser (Leo) Inc., Flushing, NY (United States); Veligdan, J. [Brookhaven National Lab., Upton, NY (United States)

    1996-04-01

    A Planar Optic Display (POD) is being built and tested for suitability as a high brightness replacement for the cathode ray tube, (CRT). The POD display technology utilizes a laminated optical waveguide structure which allows a projection type of display to be constructed in a thin (I to 2 inch) housing. Inherent in the optical waveguide is a black cladding matrix which gives the display a black appearance leading to very high contrast. A Digital Micromirror Device, (DMD) from Texas Instruments is used to create video images in conjunction with a 100 milliwatt green solid state laser. An anamorphic optical system is used to inject light into the POD to form a stigmatic image. In addition to the design of the POD screen, we discuss: image formation, image projection, and optical design constraints.

  7. Color speckle in laser displays

    Science.gov (United States)

    Kuroda, Kazuo

    2015-07-01

    At the beginning of this century, lighting technology has been shifted from discharge lamps, fluorescent lamps and electric bulbs to solid-state lighting. Current solid-state lighting is based on the light emitting diodes (LED) technology, but the laser lighting technology is developing rapidly, such as, laser cinema projectors, laser TVs, laser head-up displays, laser head mounted displays, and laser headlamps for motor vehicles. One of the main issues of laser displays is the reduction of speckle noise1). For the monochromatic laser light, speckle is random interference pattern on the image plane (retina for human observer). For laser displays, RGB (red-green-blue) lasers form speckle patterns independently, which results in random distribution of chromaticity, called color speckle2).

  8. Assessment of PACS Display Systems

    OpenAIRE

    Aldrich, John E.; Rutledge, John D.

    2005-01-01

    This work describes our experience in reviewing the performance criteria for display systems and how we have implemented a practical approach to the assessment of the workstation environment in a large tertiary care hospital. The acceptance criteria contained in the draft report of Topic Group 18 of the American Association of Physicists in Medicine (AAPM) were used as a basis for assessment of primary and secondary displays. A telescopic photometer was used to measure the maximum luminance a...

  9. Quantitative determination of capsaicin, a transient receptor potential channel vanilloid 1 agonist, by liquid chromatography quadrupole ion trap mass spectrometry: evaluation of in vitro metabolic stability.

    Science.gov (United States)

    Beaudry, Francis; Vachon, Pascal

    2009-02-01

    Capsaicin is the most abundant pungent molecule present in red peppers and it is widely used for food flavoring, in pepper spray in self-defense devices and more recently in ointments for the relief of neuropathic pain. Capsaicin is a selective agonist of transient receptor potential channel, vanilloid subfamily member 1. A selective and sensitive quantitative method for the determination of capsaicin by LC-ESI/MS/MS was developed. The method consisted of a protein precipitation extraction followed by analysis using liquid chromatography electrospray quadrupole ion trap mass spectrometry. The chromatographic separation was achieved using a 100 x 2 mm C(18) Waters Symmetry column combined with a gradient mobile phase composed of acetonitrile and 0.1% formic acid aqueous solution at a flow rate of 220 microL/min. The mass spectrometer was operating in full-scan MS/MS mode using two-segment analysis. An analytical range of 10-5000 ng/mL was used in the calibration curve constructed in rat plasma. The interbatch precision and accuracy observed were 6.5, 6.7, 5.3 and 101.2, 102.7, 103.5% at 50, 500 and 5000 ng/mL, respectively. An in vitro metabolic stability study was performed in rat, dog and mouse liver microsomes and the novel analytical method was adapted and used to determine intrinsic clearance of capsaicin. Results suggest very rapid degradation with T(1/2) ranging from 2.3 to 4.1 min and high clearance values suggesting that drug bioavailability will be considerably reduced, consequently affecting drug response and efficacy. PMID:18816461

  10. Determination of capsaicin, dihydrocapsaicin, and nonivamide in self-defense weapons by liquid chromatography-mass spectrometry and liquid chromatography-tandem mass spectrometry.

    Science.gov (United States)

    Reilly, C A; Crouc, D J; Yost, G S; Fatah, A A

    2001-04-01

    Sensitive and selective liquid chromatography-mass spectrometry (LC-MS) and liquid chromatography-tandem mass spectrometry (LC-MS-MS) methods for the analysis of capsaicin, dihydrocapsaicin, and nonivamide in pepper spray products have been developed. Chromatographic separation of the capsaicinoid analogues was achieved using a reversed-phase HPLC column and a stepwise gradient of methanol and distilled water containing 0.1% (v/v) formic acid. Identification and quantification of the capsaicinoids was achieved by electrospray ionization single-stage mass spectrometry monitoring the protonated molecules of the internal standard (m/z 280), capsaicin (m/z 306), dihydrocapsaicin (m/z 308), and nonivamide (m/z 294) or by tandem mass spectrometry monitoring the appropriate precursor-to-product-ion transitions. The plot of concentration versus peak area ratio was linear over the range of 10-750 ng/ml using LC-MS and 10-500 ng/ml using LC-MS-MS. However, to accurately quantify the capsaicinoids in the pepper spray products calibration curves between 10 and 1000 ng were constructed and fit using a weighted quadratic equation. Using the quadratic curve, the accuracy of the assay ranged from 91 to 102% for all analytes. The intra-assay precision (RSD) for capsaicin was 2% at 25 ng/ml, 10% at 500 ng/ml, and 3% at 800 ng/ml. The inter-assay precision (RSD) for capsaicin was 6% at 25 ng/ml, 6% at 500 ng/ml, and 9% at 800 ng/ml. Similar values for inter- and intra-assay precision were experimentally obtained for both dihydrocapsaicin and nonivamide. The analysis of selected pepper spray products demonstrated that the capsaicinoid concentration in the products ranged from 0.7 to 40.5 microg/microl. PMID:11330795

  11. Exposure to Allergen Causes Changes in NTS Neural Activities after Intratracheal Capsaicin Application, in Endocannabinoid Levels and in the Glia Morphology of NTS

    OpenAIRE

    Giuseppe Spaziano; Livio Luongo; Francesca Guida; Stefania Petrosino; Maria Matteis; Enza Palazzo; Nikol Sullo; Vito de Novellis; Vincenzo Di Marzo; Francesco Rossi; Sabatino Maione; Bruno D’Agostino

    2015-01-01

    Allergen exposure may induce changes in the brainstem secondary neurons, with neural sensitization of the nucleus solitary tract (NTS), which in turn can be considered one of the causes of the airway hyperresponsiveness, a characteristic feature of asthma. We evaluated neurofunctional, morphological, and biochemical changes in the NTS of naive or sensitized rats. To evaluate the cell firing activity of NTS, in vivo electrophysiological experiments were performed before and after capsaicin cha...

  12. Considerable Variability in the Efficacy of 8% Capsaicin Topical Patches in the Treatment of Chronic Pruritus in 3 Patients with Notalgia Paresthetica

    OpenAIRE

    Andersen, Hjalte Holm; Sand, Carsten; Elberling, Jesper

    2016-01-01

    Notalgia paresthetica (NP) is a focal neuropathic itch con- dition manifesting in intense chronic or recurrent episodic itch in a hyperpigmented, macular, uni- or bilateral skin area located below and/or medially to the scapulae. Achieving satisfactory relieve in NP patients is challenging. In this case-series three female NP patients were treated with 8% capsaicin patches following a spatial quantification of their alloknetic area with a von Frey filament. The use of a von Frey filament in o...

  13. Implementation of PIC Based LED Displays

    OpenAIRE

    Htet Htet Thit San; Chaw Myat Nwe; Hla Myo Tun

    2014-01-01

    This paper explains the project which is a special kind of LED Display Board for performing dance movement according to the rhythm of music. Nowadays, LED display boards are widely used in advertising and other applications. LED display boards can also be used indoors or outdoors. The objective of this system is to design a display panel by using several dozens of LED matrix display. The display pattern can desire to be changed easily and modified by the user. This LED display...

  14. Exposure to Allergen Causes Changes in NTS Neural Activities after Intratracheal Capsaicin Application, in Endocannabinoid Levels and in the Glia Morphology of NTS.

    Science.gov (United States)

    Spaziano, Giuseppe; Luongo, Livio; Guida, Francesca; Petrosino, Stefania; Matteis, Maria; Palazzo, Enza; Sullo, Nikol; de Novellis, Vito; Di Marzo, Vincenzo; Rossi, Francesco; Maione, Sabatino; D'Agostino, Bruno

    2015-01-01

    Allergen exposure may induce changes in the brainstem secondary neurons, with neural sensitization of the nucleus solitary tract (NTS), which in turn can be considered one of the causes of the airway hyperresponsiveness, a characteristic feature of asthma. We evaluated neurofunctional, morphological, and biochemical changes in the NTS of naive or sensitized rats. To evaluate the cell firing activity of NTS, in vivo electrophysiological experiments were performed before and after capsaicin challenge in sensitized or naive rats. Immunohistochemical studies, endocannabinoid, and palmitoylethanolamide quantification in the NTS were also performed. This study provides evidence that allergen sensitization in the NTS induced: (1) increase in the neural firing response to intratracheal capsaicin application, (2) increase of endocannabinoid anandamide and palmitoylethanolamide, a reduction of 2-arachidonoylglycerol levels in the NTS, (3) glial cell activation, and (4) prevention by a Group III metabotropic glutamate receptor activation of neural firing response to intratracheal application of capsaicin in both naïve and sensitized rats. Therefore, normalization of ovalbumin-induced NTS neural sensitization could open up the prospect of new treatments based on the recovery of specific brain nuclei function and for extensive studies on acute or long-term efficacy of selective mGlu ligand, in models of bronchial hyperreactivity.

  15. BES Monitoring & Displaying System

    Institute of Scientific and Technical Information of China (English)

    MengWANG; BingyunZHANG; 等

    2001-01-01

    BES1 Monitoring & Displaying System(BESMDS)is projected to monitor and display the running status of DAQ and Slow Control systems of BES through the Web for worldwide accessing.It provides a real-time remote means of monitoring as well as an approach to study the environmental influence upon physical data taking.The system collects real-time data separately from BES online subsystems by network sockets and stores the data into a database.People can access the system through its web site.which retrieves data on request from the database and can display results in dynamically created images.Its web address in http:// besmds,ihep.ac.cn/

  16. Engineering antibodies by yeast display.

    Science.gov (United States)

    Boder, Eric T; Raeeszadeh-Sarmazdeh, Maryam; Price, J Vincent

    2012-10-15

    Since its first application to antibody engineering 15 years ago, yeast display technology has been developed into a highly potent tool for both affinity maturing lead molecules and isolating novel antibodies and antibody-like species. Robust approaches to the creation of diversity, construction of yeast libraries, and library screening or selection have been elaborated, improving the quality of engineered molecules and certainty of success in an antibody engineering campaign and positioning yeast display as one of the premier antibody engineering technologies currently in use. Here, we summarize the history of antibody engineering by yeast surface display, approaches used in its application, and a number of examples highlighting the utility of this method for antibody engineering.

  17. Color Video Laser Display Technology

    Institute of Scientific and Technical Information of China (English)

    ZHANG Yue; LIU Wei-qi; HAO Li; LIU Hua; WEI Zhong-lun

    2006-01-01

    The principle and technologies employed in laser color video display are introduced. The characteristics of techniologies and bottlenecks of restricting the development are analyzed .A novel technical approach to eliminating the laser interference, improving the uniformity of optical field, transforming the chromaticity and extending the virtual color is proposed. The principle device of laser display system has been developed on the basis of the blue,green and red diode-pumped solid state lasers .The wavelengths of the blue, green and red are 473nm, 532nm and 671nm, and the output powers of the lasers are 1.3W, 0.32W and 3.5W, respectively.

  18. Display standards for commercial flight decks

    Science.gov (United States)

    Lamberth, Larry S.; Penn, Cecil W.

    1994-06-01

    SAE display standards are used as guidelines for certifying commercial airborne electronic displays. The SAE document generation structure and approval process is described. The SAE committees that generate display standards are described. Three SAE documents covering flat panel displays (AS-8034, ARP-4256, and ARP-4260) are discussed with their current status. Head-Up Display documents are also in work.

  19. Colour displays for categorical images

    NARCIS (Netherlands)

    Glasbey, C.; Heijden, van der G.W.A.M.; Toh, V.F.K.; Gray, A.J.

    2007-01-01

    We propose a method for identifying a set of colours for displaying 2D and 3D categorical images when the categories are unordered labels. The principle is to find maximally distinct sets of colours. We either generate colours sequentially, to maximize the dissimilarity or distance between a new col

  20. Information retrieval and display system

    Science.gov (United States)

    Groover, J. L.; King, W. L.

    1977-01-01

    Versatile command-driven data management system offers users, through simplified command language, a means of storing and searching data files, sorting data files into specified orders, performing simple or complex computations, effecting file updates, and printing or displaying output data. Commands are simple to use and flexible enough to meet most data management requirements.

  1. Display Sharing: An Alternative Paradigm

    Science.gov (United States)

    Brown, Michael A.

    2010-01-01

    The current Johnson Space Center (JSC) Mission Control Center (MCC) Video Transport System (VTS) provides flight controllers and management the ability to meld raw video from various sources with telemetry to improve situational awareness. However, maintaining a separate infrastructure for video delivery and integration of video content with data adds significant complexity and cost to the system. When considering alternative architectures for a VTS, the current system's ability to share specific computer displays in their entirety to other locations, such as large projector systems, flight control rooms, and back supporting rooms throughout the facilities and centers must be incorporated into any new architecture. Internet Protocol (IP)-based systems also support video delivery and integration. IP-based systems generally have an advantage in terms of cost and maintainability. Although IP-based systems are versatile, the task of sharing a computer display from one workstation to another can be time consuming for an end-user and inconvenient to administer at a system level. The objective of this paper is to present a prototype display sharing enterprise solution. Display sharing is a system which delivers image sharing across the LAN while simultaneously managing bandwidth, supporting encryption, enabling recovery and resynchronization following a loss of signal, and, minimizing latency. Additional critical elements will include image scaling support, multi -sharing, ease of initial integration and configuration, integration with desktop window managers, collaboration tools, host and recipient controls. This goal of this paper is to summarize the various elements of an IP-based display sharing system that can be used in today's control center environment.

  2. JTEC panel on display technologies in Japan

    Science.gov (United States)

    Tannas, Lawrence E., Jr.; Glenn, William E.; Credelle, Thomas; Doane, J. William; Firester, Arthur H.; Thompson, Malcolm

    1992-01-01

    This report is one in a series of reports that describes research and development efforts in Japan in the area of display technologies. The following are included in this report: flat panel displays (technical findings, liquid crystal display development and production, large flat panel displays (FPD's), electroluminescent displays and plasma panels, infrastructure in Japan's FPD industry, market and projected sales, and new a-Si active matrix liquid crystal display (AMLCD) factory); materials for flat panel displays (liquid crystal materials, and light-emissive display materials); manufacturing and infrastructure of active matrix liquid crystal displays (manufacturing logistics and equipment); passive matrix liquid crystal displays (LCD basics, twisted nematics LCD's, supertwisted nematic LCD's, ferroelectric LCD's, and a comparison of passive matrix LCD technology); active matrix technology (basic active matrix technology, investment environment, amorphous silicon, polysilicon, and commercial products and prototypes); and projection displays (comparison of Japanese and U.S. display research, and technical evaluation of work).

  3. Capsaicin enhances anti-proliferation efficacy of pirarubicin via activating TRPV1 and inhibiting PCNA nuclear translocation in 5637 cells.

    Science.gov (United States)

    Zheng, Long; Chen, Jiaqi; Ma, Zhenkun; Liu, Wei; Yang, Fei; Yang, Zhao; Wang, Ke; Wang, Xinyang; He, Dalin; Li, Lei; Zeng, Jin

    2016-01-01

    The recurrence of bladder cancer after surgery with or without chemotherapy remains a major challenge in bladder cancer treatment. Previous studies have shown that transient receptor potential vanilloid 1 (TRPV1) acts as a tumor suppressor through inducing apoptosis in bladder cancer cells. However, whether activation of TRPV1 has any synergistic effects with pirarubicin (THP), one of main drugs used in urinary bladder instillation chemotherapy to improve chemotherapeutic efficacy has remained elusive. The present study verified that TRPV1 was differentially expressed in bladder cancer cell lines. Furthermore, activation of TRPV1 by capsaicin was shown to induce growth inhibition of 5637 cells in which TRPV1 was highly expressed, while the growth of T24 cells, which express TRPV1 at low levels, was not affected. In addition, the present study demonstrated that activation of TRPV1 enhanced the anti‑proliferative effects of pirarubicin using an MTT assay and cell cycle analysis. Finally, immunofluorescent microscopy revealed that activation of TRPV1 prevented the translocation of proliferating cell nuclear antigen to the nucleus. This phenomenon was reversed by pre‑treatment with capsazepine, a specific TRPV1 antagonist. In conclusion, the present study confirmed the anti‑tumor activity of TRPV1 against bladder cancer. Activation of TRPV1 may be applied as a novel strategy to treat bladder cancer or enhance the therapeutic efficacy of traditional chemotherapeutic drugs.

  4. Enhancing antibiofouling performance of Polysulfone (PSf) membrane by photo-grafting of capsaicin derivative and acrylic acid

    Science.gov (United States)

    Wang, Jian; Sun, Haijing; Gao, Xueli; Gao, Congjie

    2014-10-01

    Biofouling is a critical issue in membrane water and wastewater treatment. Herein, antibiofouling PSf membrane was prepared by UV-assisted graft polymerization of acrylic acid (AA) and a capsaicin derivative, N-(5-methyl-3-tert-butyl-2-hydroxy benzyl) acrylamide (MBHBA), on PSf membrane. AA and MBHBA were used as hydrophilic monomer and antibacterial monomer separately. The membranes were characterized by FTIR-ATR, contact angle, SEM, AFM, cross-flow filtration unit, antifouling and antibacterial measurements. Verification of MBHBA and AA that photo-chemically grafted onto the PSf membrane surface is confirmed by carbonyl stretching vibration at ∼1655 cm-1 and ∼1730 cm-1, separately. The increasing AA concentration accelerates the graft-polymerization of MBHBA and resulted in a more hydrophilic surface. Consequently, antifouling property of the membranes was improved on a large level. The flux recovery rate can achieve 100% during the cyclic test, which may be attributed to the more hydrophilic and smooth surface, as well as the decreased membrane pore size. Most importantly, the presence of AA in graft co-polymer does not affect the antibacterial activity of MBHBA. That may be induced by the increasing chain length and flexibility of the grafted polymer chains.

  5. Game engines and immersive displays

    Science.gov (United States)

    Chang, Benjamin; Destefano, Marc

    2014-02-01

    While virtual reality and digital games share many core technologies, the programming environments, toolkits, and workflows for developing games and VR environments are often distinct. VR toolkits designed for applications in visualization and simulation often have a different feature set or design philosophy than game engines, while popular game engines often lack support for VR hardware. Extending a game engine to support systems such as the CAVE gives developers a unified development environment and the ability to easily port projects, but involves challenges beyond just adding stereo 3D visuals. In this paper we outline the issues involved in adapting a game engine for use with an immersive display system including stereoscopy, tracking, and clustering, and present example implementation details using Unity3D. We discuss application development and workflow approaches including camera management, rendering synchronization, GUI design, and issues specific to Unity3D, and present examples of projects created for a multi-wall, clustered, stereoscopic display.

  6. Striations in Plasma Display Panel

    Institute of Scientific and Technical Information of China (English)

    OUYANG Ji-Ting; CAO Jing; MIAO Jin-Song

    2005-01-01

    @@ The phenomenon of striation has been investigated experimentally in a macroscopic ac-plasma display panel (PDP). The relationship between the characteristics of striation and the operation conditions including voltage, frequency, rib, and electrode configuration, etc is obtained experimentally. The origin of the striations is considered to be the ionization waves in the transient positive column near the dielectric surface in the anode area during the discharge, and the perturbation is caused by resonance kinetic effects in inert gas.

  7. A conformable active matrix LED display

    OpenAIRE

    Tripathi, Ashutosh; Smits, Edsger; van der Steen, Jan-Laurens; Cauwe, Maarten; Verplancke, Rik; Myny, Kris; Maas, Joris; Kusters, Roel; Sabik, Sami; Murata, Mitsuhiro; Tomita, Yoshihiro; Ohmae, Hideki; van den Brand, Jeroen; Gelinck, Gerwin

    2015-01-01

    Conformable and stretchable displays can be integrated on complex surfaces. Such a display can assume the shape of a conformed surface by simultaneous multi-dimensional stretching and bending. Such technology provides new opportunities in the field of display applications, for example wearable displays integrated or embedded in a textile or onto complex surfaces in automotive interiors. In this work we present a conformable active matrix display using LEDs mounted on an amorphous Indium-Galli...

  8. Recent Trend in Development of Olfactory Displays

    Science.gov (United States)

    Yanagida, Yasuyuki

    An olfactory display is a device that generates scented air with desired concentration of aroma, and delivers it to the user's olfactory organ. In this article, the nature of olfaction is briefly described from the view point of how to configure olfactory displays. Next, component technologies to compose olfactory displays, i.e., making scents and delivering scents, are categorized. Several existing olfactory display systems are introduced to show the current status of research and development of olfactory displays.

  9. Aumento del umbral tusígeno en sujetos sanos con el uso de Levodropropizina INCREASE OF THE COUGH THRESHOLD TO CAPSAICIN IN HEALTHY ADULTS BY ADMINISTERING LEVODROPROPIZINE

    Directory of Open Access Journals (Sweden)

    Patricia Schönffeldt G.

    2005-09-01

    Full Text Available Se diseñó un estudio aleatorio prospectivo, doble ciego cruzado contra placebo, para estudiar la reproducibilidad y las modificaciones del umbral tusígeno (UT inducido por capsaicina, luego de administrar placebo y Levodropropizina (un nuevo antitusivo sintético. Se determinó el UT basal (logaritmo de la concentración de capsaicina que induce al menos dos toses consecutivas en 20 voluntarios adultos sanos, no fumadores de ambos sexos con edad promedio de 34,9 años (rango: 18 a 57 años. El promedio del UT basal fue 2,240 µM (± 0,060 ES, sin haber diferencias significativas por sexo o edad (p: ns. En 11 de 18 sujetos el UT aumentó de 2,358 µM (± 0,044 ES con placebo a 2,469 µM (± 0,057 ES con Levodropropizina (p = 0,01. Dos sujetos fueron excluidos por presentar una enfermedad intercurrente no relacionada con el estudio. No hubo efectos adversos significativos. Conclusión: La capsaicina indujo reproduciblemente el reflejo tusígeno en 20 voluntarios sanos, y la Levodropropizina administrada por vía oral aumentó el umbral tusígenoA randomized, prospective, double blind and placebo controlled study was designed to evaluate in 20 non smoker healthy adult volunteers the reproducibility and modification of cough threshold (CT induced by capsaicin after placebo and Levodropropizine (a new synthetic drug. Adult volonteers of both sexes, mean age 34.9 years old (range: 18-57 years, inhaled increasing concentrations of capsaicin to determine the basal CT: log concentration of capsaicin that induced at least two consecutive coughs. The basal CT was 2.240 µM (± 0.060 SE, without differences by sex or age (p: ns, In 11 out of 18 subjects the CT increased from 2.358 (± 0,044 SE on placebo to 2.469 µM (± 0.057 after Levodropropizine (p = 0.01. Two subjects were excluded due to intercurrent disease, not related to the study. No significant adverse reactions were reported during the study. Conclusion: Capsaicin induced reproducible

  10. Considerable variability in the efficacy of 8% capsaicin topical patches in the treatment of chronic pruritus in 3 patients with notalgia paresthetica

    DEFF Research Database (Denmark)

    Andersen, Hjalte Holm; Sand, Carsten; Elberling, Jesper

    2016-01-01

    feasible. Although 8% topical capsaicin relieved itch in all three pa- tients, the duration of the effectiveness varied greatly from only 3 days to >2 months. The treatment was well tolerated in the patients and there appear to be no significant hin- drances to applying this treatment with NP...... as an indication, although it may only exhibit satisfactory effectiveness in cer- tain patients. Placebo-controlled double-blinded trials are needed to confirm the effectiveness of the treatment and as- sess predictive parameters of the treatment outcome...

  11. The effect of wound instillation of a novel purified capsaicin formulation on postherniotomy pain: A double-blind, randomized, placebo-controlled study

    DEFF Research Database (Denmark)

    Aasvang, Eske Kvanner; Hansen, J.B.; Malmstrom, J.;

    2008-01-01

    , preclinical, and clinical studies, and may be an effective adjunct to postoperative pain management. METHODS: We performed a single-center, randomized, double-blind, placebo-controlled study of the analgesic efficacy of a single intraoperative wound instillation of 1000 mu g ultrapurified capsaicin (ALGRX...... 4975) after open mesh groin hernia repair in 41 adult male patients. The primary end-point was average daily visual analog scale (VAS) pain scores during the first week after surgery assessed as area under the curve (AUC). Pain was recorded twice daily in a pain diary for 4 wk. Physical examination...

  12. Solid-state turn coordinator display

    Science.gov (United States)

    Meredith, B. D.; Crouch, R. K.; Kelly, W. L., IV

    1975-01-01

    A solid state turn coordinator display which employs light emitting diodes (LED's) as the display medium was developed to demonstrate the feasibility of such displays for aircraft applications. The input to the display is supplied by a fluidic inertial rate sensor used in an aircraft wing leveler system. The display is composed of the LED radial display face and the electronics necessary to address and drive the individual lines of LED's. Three levels of brightness are provided to compensate for the different amounts of ambient light present in the cockpit.

  13. Anti-proliferative effect of extremely low frequency electromagnetic field on preneoplastic lesions formation in the rat liver

    Directory of Open Access Journals (Sweden)

    Villa-Treviño Saúl

    2010-04-01

    Full Text Available Abstract Background Recently, extremely low frequency electromagnetic fields (ELF-EMF have been studied with great interest due to their possible effects on human health. In this study, we evaluated the effect of 4.5 mT - 120 Hz ELF-EMF on the development of preneoplastic lesions in experimental hepatocarcinogenesis. Methods Male Fischer-344 rats were subjected to the modified resistant hepatocyte model and were exposed to 4.5 mT - 120 Hz ELF-EMF. The effects of the ELF-EMF on hepatocarcinogenesis, apoptosis, proliferation and cell cycle progression were evaluated by histochemical, TUNEL assay, caspase 3 levels, immunohistochemical and western blot analyses. Results The application of the ELF-EMF resulted in a decrease of more than 50% of the number and the area of γ-glutamyl transpeptidase-positive preneoplastic lesions (P = 0.01 and P = 0.03, respectively and glutathione S-transferase placental expression (P = 0.01. The number of TUNEL-positive cells and the cleaved caspase 3 levels were unaffected; however, the proliferating cell nuclear antigen, Ki-67, and cyclin D1 expression decreased significantly (P ≤ 0.03, as compared to the sham-exposure group. Conclusion The application of 4.5 mT - 120 Hz ELF-EMF inhibits preneoplastic lesions chemically induced in the rat liver through the reduction of cell proliferation, without altering the apoptosis process.

  14. Mechanisms underlying the anti-proliferative effects of berry components in in vitro models of colon cancer.

    Science.gov (United States)

    Brown, Emma M; Gill, Chris I R; McDougall, Gordon J; Stewart, Derek

    2012-01-01

    Consumption of fruit and vegetables is associated with a decreased risk of several cancers, particularly colorectal cancer, possibly linked to their phytochemical content, which is of interest due to several proposed health benefits, including potential anticancer activity. Epidemiological data suggests that cancers of the digestive tract are most susceptible to dietary modification, possibly due to being in direct contact with bioactive food constituents and therefore investigating the effects of these bioactive compounds on the prevalent colorectal cancer is feasible. Berries are a common element of Western diets, with members of the Rubus, Fragria, Sorbus, Ribes and Vaccinum genus featuring in desserts, preserves, yoghurts and juices. These soft fruit are rich in bioactive phytochemicals including several classes of phenolic compounds such as flavonoids (anthocyanins, flavonols and flavanols) and phenolic acids (hydroxybenzoic and hydroxycinnamic acids). Whilst there is little data linking berry consumption to reduced risk of colorectal cancer, in vitro evidence from models representing colorectal cancer suggests that berry polyphenols may modulate cellular processes essential for cancer cell survival, such as proliferation and apoptosis. The exact mechanisms and berry constituents responsible for these potential anticancer activities remain unknown, but use of in vitro models provides a means to elucidate these matters.

  15. Anti-proliferative effect of a compound isolated from Cassia auriculata against human colon cancer cell line HCT 15.

    Science.gov (United States)

    Esakkirajan, M; Prabhu, N M; Arulvasu, C; Beulaja, M; Manikandan, R; Thiagarajan, R; Govindaraju, K; Prabhu, D; Dinesh, D; Babu, G; Dhanasekaran, G

    2014-01-01

    The compound was isolated from leaves of Cassia auriculata and its structure was characterized using high-performance liquid chromatography (HPLC), liquid chromatography mass spectrometry (LC-MS), UV-vis spectroscopy (UV-vis), fourier transform infrared spectroscopy (FT-IR) and nuclear magnetic resonance spectroscopy (NMR). 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay, cytotoxicity, nuclear morphology and lactate dehydrogenase assay of isolated compound was tested against human colon cancer cell line HCT 15. The isolated compound, 4-(4-chlorobenzyl)-2,3,4,5,6,7-hexahydro-7-(2-ethoxyphenyl)benzo[h][1,4,7]triazecin-8(1H)-one at 25μg/ml concentration and by 48h showed 50% inhibition of human colon cancer cells (HCT 15). The results suggest that isolated compound from C. auriculata has potential to prevent colon cancer cell line.

  16. Apoptosis mediated anti-proliferative effect of compound isolated from Cassia auriculata leaves against human colon cancer cell line

    Science.gov (United States)

    Esakkirajan, M.; Prabhu, N. M.; Manikandan, R.; Beulaja, M.; Prabhu, D.; Govindaraju, K.; Thiagarajan, R.; Arulvasu, C.; Dhanasekaran, G.; Dinesh, D.; Babu, G.

    2014-06-01

    A compound was isolated from Cassia auriculata leaves and characterized by high-performance liquid chromatography (HPLC), liquid chromatography mass spectrometry (LC-MS), UV-vis spectroscopy (UV-vis), Fourier transform infrared spectroscopy (FT-IR) and nuclear magnetic resonance spectroscopy (NMR). The in vitro anticancer effect of the compound isolated from C. auriculata was evaluated in human colon cancer cells HCT 15 by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay, cytotoxicity, nuclear morphology analysis and measurement of lactate dehydrogenase. The isolated compound 4-(2,5 dichlorobenzyl)-2,3,4,5,6,7 hexahydro7(4 methoxyphenyl)benzo[h][1,4,7] triazecin8(1H)-one showed 50% inhibition of HCT 15 cells when tested at 20 μg/ml after 24 h incubation. Cytotoxicity, nuclear morphology and lactate dehydrogenase assays clearly show potent anticancer activity of the isolated compound against colon cancer. Thus, the in vitro findings suggest that the compound isolated from C. auriculata leaves have potent anti-cancer properties with possible clinical applications.

  17. Anti-proliferative effect of rhein, an anthraquinone isolated from Cassia species, on Caco-2 human adenocarcinoma cells.

    Science.gov (United States)

    Aviello, Gabriella; Rowland, Ian; Gill, Christopher I; Acquaviva, Angela Maria; Capasso, Francesco; McCann, Mark; Capasso, Raffaele; Izzo, Angelo A; Borrelli, Francesca

    2010-07-01

    In recent years, the use of anthraquinone laxatives, in particular senna, has been associated with damage to the intestinal epithelial layer and an increased risk of developing colorectal cancer. In this study, we evaluated the cytotoxicity of rhein, the active metabolite of senna, on human colon adenocarcinoma cells (Caco-2) and its effect on cell proliferation. Cytotoxicity studies were performed using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT), neutral red (NR) and trans-epithelial electrical resistance (TEER) assays whereas (3)H-thymidine incorporation and Western blot analysis were used to evaluate the effect of rhein on cell proliferation. Moreover, for genoprotection studies Comet assay and oxidative biomarkers measurement (malondialdehyde and reactive oxygen species) were used. Rhein (0.1-10 microg/ml) had no significant cytotoxic effect on proliferating and differentiated Caco-2 cells. Rhein (0.1 and 1 microg/ml) significantly reduced cell proliferation as well as mitogen-activated protein (MAP) kinase activation; by contrast, at high concentration (10 microg/ml) rhein significantly increased cell proliferation and extracellular-signal-related kinase (ERK) phosphorylation. Moreover, rhein (0.1-10 microg/ml): (i) did not adversely affect the integrity of tight junctions and hence epithelial barrier function; (ii) did not induce DNA damage, rather it was able to reduce H(2)O(2)-induced DNA damage and (iii) significantly inhibited the increase in malondialdehyde and reactive oxygen species (ROS) levels induced by H(2)O(2)/Fe(2+). Rhein was devoid of cytotoxic and genotoxic effects in colon adenocarcinoma cells. Moreover, at concentrations present in the colon after a human therapeutic dosage of senna, rhein inhibited cell proliferation via a mechanism that seems to involve directly the MAP kinase pathway. Finally, rhein prevents the DNA damage probably via an anti-oxidant mechanism.

  18. Cold Atmospheric Plasma Treatment Induces Anti-Proliferative Effects in Prostate Cancer Cells by Redox and Apoptotic Signaling Pathways.

    Directory of Open Access Journals (Sweden)

    Martin Weiss

    Full Text Available One of the promising possibilities of the clinical application of cold plasma, so-called cold atmospheric plasma (CAP, is its application on malignant cells and cancer tissue using its anti-neoplastic effects, primarily through the delivery of reactive oxygen and nitrogen species (ROS, RNS. In this study, we investigated the impact of CAP on cellular proliferation and consecutive molecular response mechanisms in established prostate cancer (PC cell lines. PC cells showed a significantly reduced cell growth following CAP treatment as a result of both an immediate increase of intracellular peroxide levels and through the induction of apoptosis indicated by annexin V assay, TUNEL assay, and the evaluation of changes in nuclear morphology. Notably, co-administration of N-acetylcysteine (NAC completely neutralized CAP effects by NAC uptake and rapid conversion to glutathione (GSH. Vitamin C could not counteract the CAP induced effects on cell growth. In summary, relatively short treatments with CAP of 10 seconds were sufficient to induce a significant inhibition of cancer proliferation, as observed for the first time in urogenital cancer. Therefore, it is important to understand the mode of CAP related cell death and clarify and optimize CAP as cancer therapy. Increased levels of peroxides can alter redox-regulated signaling pathways and can lead to growth arrest and apoptosis. We assume that the general intracellular redox homeostasis, especially the levels of cellular GSH and peroxidases such as peroxiredoxins affect the outcome of the CAP treatment.

  19. Cold Atmospheric Plasma Treatment Induces Anti-Proliferative Effects in Prostate Cancer Cells by Redox and Apoptotic Signaling Pathways.

    Science.gov (United States)

    Weiss, Martin; Gümbel, Denis; Hanschmann, Eva-Maria; Mandelkow, Robert; Gelbrich, Nadine; Zimmermann, Uwe; Walther, Reinhard; Ekkernkamp, Axel; Sckell, Axel; Kramer, Axel; Burchardt, Martin; Lillig, Christopher H; Stope, Matthias B

    2015-01-01

    One of the promising possibilities of the clinical application of cold plasma, so-called cold atmospheric plasma (CAP), is its application on malignant cells and cancer tissue using its anti-neoplastic effects, primarily through the delivery of reactive oxygen and nitrogen species (ROS, RNS). In this study, we investigated the impact of CAP on cellular proliferation and consecutive molecular response mechanisms in established prostate cancer (PC) cell lines. PC cells showed a significantly reduced cell growth following CAP treatment as a result of both an immediate increase of intracellular peroxide levels and through the induction of apoptosis indicated by annexin V assay, TUNEL assay, and the evaluation of changes in nuclear morphology. Notably, co-administration of N-acetylcysteine (NAC) completely neutralized CAP effects by NAC uptake and rapid conversion to glutathione (GSH). Vitamin C could not counteract the CAP induced effects on cell growth. In summary, relatively short treatments with CAP of 10 seconds were sufficient to induce a significant inhibition of cancer proliferation, as observed for the first time in urogenital cancer. Therefore, it is important to understand the mode of CAP related cell death and clarify and optimize CAP as cancer therapy. Increased levels of peroxides can alter redox-regulated signaling pathways and can lead to growth arrest and apoptosis. We assume that the general intracellular redox homeostasis, especially the levels of cellular GSH and peroxidases such as peroxiredoxins affect the outcome of the CAP treatment.

  20. Anti-proliferative and angio-suppressive effect of Stoechospermum marginatum (C. Agardh) Kutzing extract using various experimental models.

    Digital Repository Service at National Institute of Oceanography (India)

    Vinayak, R.C.; Puttananjaiah, S.; Chatterji, A.; Salimath, B.

    , particularly in the regions surrounded by China, the Korean peninsula and Japan. By and large, plants possessing an extensive array of pharma- cological activities including antioxidant, anti-inflammatory, cardioprotective, and anticancer/antiangiogenic have..., triterpenes are more inclined to possess angiosuppressive activity. A number of studies have indicated that marine seaweeds from India exhibit potent antioxidant properties [12-15, 23-25]; however, they have not been systematically explored...

  1. Two New Oleanane-Type Saponins with Anti-Proliferative Activity from Camellia oleifera Abel. Seed Cake.

    Science.gov (United States)

    Zong, Jian-Fa; Peng, Yun-Ru; Bao, Guan-Hu; Hou, Ru-Yan; Wan, Xiao-Chun

    2016-01-01

    Two new oleanane-type saponins, named oleiferasaponins C₄ (1) and C₅ (2), were isolated from Camellia oleifera Abel. seed cake residue. Their respective structures were identified as 16α-hydroxy-22α-O-angeloyl-23α-aldehyde-28-dihydroxymethylene-olean-12-ene-3β-O-[β-d-galacto-pyranosyl-(1→2)]-[β-d-glucopyranosyl-(1→2)-β-d-galactopyranosy-(1→3)]-β-d-glucopyranosid-uronic acid methyl ester (1) and 16α-hydroxy-22α-O-angeloyl-23α-aldehyde-28-dihydroxy-methylene-olean-12-ene-3β-O-[β-d-galactopyranosyl-(1→2)]-[β-d-galactopyranosyl-(1→3)]-β-d-glucopyranosiduronic acid methyl ester (2) through 1D- and 2D-NMR, HR-ESI-MS, and GC-MS spectroscopic methods. The two compounds exhibited potent cytotoxic activities against five human tumor cell lines (BEL-7402, BGC-823, MCF-7, HL-60 and KB).

  2. Anti-proliferative effect of biogenic gold nanoparticles against breast cancer cell lines (MDA-MB-231 & MCF-7)

    Science.gov (United States)

    K. S., Uma Suganya; Govindaraju, K.; Ganesh Kumar, V.; Prabhu, D.; Arulvasu, C.; Stalin Dhas, T.; Karthick, V.; Changmai, Niranjan

    2016-05-01

    Breast cancer is a major complication in women and numerous approaches are being developed to overcome this problem. In conventional treatments such as chemotherapy and radiotherapy the post side effects cause an unsuitable effect in treatment of cancer. Hence, it is essential to develop a novel strategy for the treatment of this disease. In the present investigation, a possible route for green synthesis of gold nanoparticles (AuNPs) using leaf extract of Mimosa pudica and its anticancer efficacy in the treatment of breast cancer cell lines is studied. The synthesized nanoparticles were found to be effective in killing cancer cells (MDA-MB-231 & MCF-7) which were studied using various anticancer assays (MTT assay, cell morphology determination, cell cycle analysis, comet assay, Annexin V-FITC/PI staining and DAPI staining). Cell morphological analysis showed the changes occurred in cancer cells during the treatment with AuNPs. Cell cycle analysis revealed apoptosis in G0/G1 to S phase. Similarly in Comet assay, there was an increase in tail length in treated cells in comparison with the control. Annexin V-FITC/PI staining assay showed prompt fluorescence in treated cells indicating the translocation of phosphatidylserine from the inner membrane. PI and DAPI staining showed the DNA damage in treated cells.

  3. Anti-Proliferative Activity of Meroditerpenoids Isolated from the Brown Alga Stypopodium flabelliforme against Several Cancer Cell Lines

    Directory of Open Access Journals (Sweden)

    Patricia Valentao

    2011-05-01

    Full Text Available The sea constitutes one of the most promising sources of novel compounds with potential application in human therapeutics. In particular, algae have proved to be an interesting source of new bioactive compounds. In this work, six meroditerpenoids (epitaondiol, epitaondiol diacetate, epitaondiol monoacetate, stypotriol triacetate, 14-ketostypodiol diacetate and stypodiol isolated from the brown alga Stypopodium flabelliforme were tested for their cell proliferation inhibitory activity in five cell lines. Cell lines tested included human colon adenocarcinoma (Caco-2, human neuroblastoma (SH-SY5Y, rat basophilic leukemia (RBL-2H3, murine macrophages (RAW.267 and Chinese hamster fibroblasts (V79. Antimicrobial activity of the compounds was also evaluated against Staphylococcus aureus, Salmonella typhimurium, Proteus mirabilis, Bacillus cereus, Enterococcus faecalis and Micrococcus luteus. Overall, the compounds showed good activity against all cell lines, with SH-SY5Y and RAW.267 being the most susceptible. Antimicrobial capacity was observed for epitaondiol monoacetate, stypotriol triacetate and stypodiol, with the first being the most active. The results suggest that these molecules deserve further studies in order to evaluate their potential as therapeutic agents.

  4. Anti-proliferative lichen compounds with inhibitory activity on 12(S)-HETE production in human platelets.

    Science.gov (United States)

    Bucar, F; Schneider, I; Ogmundsdóttir, H; Ingólfsdóttir, K

    2004-11-01

    Several lichen compounds, i.e. lobaric acid (1), a beta-orcinol depsidone from Stereocaulon alpinum L., (+)-protolichesterinic acid (2), an aliphatic alpha-methylene-gamma-lactone from Cetraria islandica Laur. (Parmeliaceae), (+)-usnic acid (3), a dibenzofuran from Cladonia arbuscula (Wallr.) Rabenh. (Cladoniaceae), parietin (4), an anthraquinone from Xanthoria elegans (Link) Th. Fr. (Calaplacaceae) and baeomycesic acid (5), a beta-orcinol depside isolated from Thamnolia vermicularis (Sw.) Schaer. var. subuliformis (Ehrh.) Schaer. were tested for inhibitory activity on platelet-type 12(S)-lipoxygenase using a cell-based in vitro system in human platelets. Lobaric acid (1) and (+)-protolichesterinic acid (2) proved to be pronounced inhibitors of platelet-type 12(S)-lipoxygenase, whereas baeomycesic acid (5) showed only weak activity (inhibitory activity at a concentration of 100 microg/ml: (1) 93.4+/-6.62%, (2) 98,5+/-1.19%, 5 14.7+/-2.76%). Usnic acid (3) and parietin (4) were not active at this concentration. 1 and 2 showed a clear dose-response relationship in the range of 3.33-100 microg/ml. According to the calculated IC50 values the highest inhibitory activity was observed for the depsidone 1 (IC50 = 28.5 microM) followed by 2 (IC50 = 77.0 microM). The activity of 1 was comparable to that of the flavone baicalein, which is known as a selective 12(S)-lipoxygenase inhibitor (IC50 = 24.6 microM).

  5. Medium Renewal Blocks Anti-Proliferative Effects of Metformin in Cultured MDA-MB-231 Breast Cancer Cells

    OpenAIRE

    Maruša Rajh; Klemen Dolinar; Katarina Miš; Mojca Pavlin; Sergej Pirkmajer

    2016-01-01

    Epidemiological studies indicate that metformin, a widely used type 2 diabetes drug, might reduce breast cancer risk and mortality in patients with type 2 diabetes. Metformin might protect against breast cancer indirectly by ameliorating systemic glucose homeostasis. Alternatively, it might target breast cancer cells directly. However, experiments using MDA-MB-231 cells, a standard in vitro breast cancer model, produced inconsistent results regarding effectiveness of metformin as a direct ant...

  6. Anti-proliferative and proapoptotic effects of (-)-epigallocatechin-3-gallate on human melanoma: possible implications for the chemoprevention of melanoma.

    Science.gov (United States)

    Nihal, Minakshi; Ahmad, Nihal; Mukhtar, Hasan; Wood, Gary S

    2005-04-20

    Melanoma accounts for only about 4% of all skin cancer cases but most of skin cancer-related deaths. Standard systemic therapies such as interferon (IFN) have not been adequately effective in the management of melanoma. Therefore, novel approaches are needed for prevention and treatment of this disease. Chemoprevention by naturally occurring agents present in food and beverages has shown benefits in certain cancers including nonmelanoma skin cancers. Here, employing 2 human melanoma cell lines (A-375 amelanotic malignant melanoma and Hs-294T metastatic melanoma) and normal human epidermal melanocytes (NHEM), we studied the antiproliferative effects of epigallocatechin-3-gallate (EGCG), the major polyphenolic antioxidant present in green tea. EGCG treatment was found to result in a dose-dependent decrease in the viability and growth of both melanoma cell lines. Interestingly, at similar EGCG concentrations, the normal melanocytes were not affected. EGCG treatment of the melanoma cell lines resulted in decreased cell proliferation (as assessed by Ki-67 and PCNA protein levels) and induction of apoptosis (as assessed cleavage of PARP, TUNEL assay and JC-1 assay). EGCG also significantly inhibited the colony formation ability of the melanoma cells studied. EGCG treatment of melanoma cells resulted in a downmodulation of anti-apoptotic protein Bcl2, upregulation of proapoptotic Bax and activation of caspases -3, -7 and -9. Furthermore, our data demonstrated that EGCG treatment resulted in a significant, dose-dependent decrease in cyclin D1 and cdk2 protein levels and induction of cyclin kinase inhibitors (ckis) p16INK4a, p21WAF1/CIP1 and p27KIP1. Our data suggest that EGCG causes significant induction of cell cycle arrest and apoptosis of melanoma cells that is mediated via modulations in the cki-cyclin-cdk network and Bcl2 family proteins. Thus, EGCG, alone or in conjunction with current therapies, could be useful for the management of melanoma.

  7. New naphthalene derivatives and isoquinoline alkaloids from Ancistrocladus cochinchinensis with their anti-proliferative activity on human cancer cells.

    Science.gov (United States)

    Lien, Le Quynh; Linh, Tran My; Giang, Vu Huong; Mai, Nguyen Chi; Nhiem, Nguyen Xuan; Tai, Bui Huu; Cuc, Nguyen Thi; Anh, Hoang Le Tuan; Ban, Ninh Khac; Minh, Chau Van; Kiem, Phan Van

    2016-08-15

    Five new compounds, named ancistronaphtosides A and B (1 and 2), anciscochine (3), anciscochine 6-O-β-d-glucopyranoside (4), and 4'-methoxy-5-epi-ancistecrorine A1 (5), together with tortoside A (6) and 4-hydroxy-2-methoxyphenyl-6-O-syringoyl-β-d-glucopyranoside (7) were isolated from the methanolic extract of Ancistrocladus cochinchinensis. Their chemical structures were established using HR-ESI-MS, NMR spectroscopic, and chiroptical methods. Compound 5 significantly exhibited anti-proliferation against HL-60, LU-1, and SK-MEL-2 cells with IC50 values of 5.0±1.2, 6.5±1.6, and 6.8±2.0μg/mL, respectively. PMID:27423477

  8. Abrus agglutinin is a potent anti-proliferative and anti-angiogenic agent in human breast cancer.

    Science.gov (United States)

    Bhutia, Sujit K; Behera, Birendra; Nandini Das, Durgesh; Mukhopadhyay, Subhadip; Sinha, Niharika; Panda, Prashanta Kumar; Naik, Prajna Paramita; Patra, Samir K; Mandal, Mahitosh; Sarkar, Siddik; Menezes, Mitchell E; Talukdar, Sarmistha; Maiti, Tapas K; Das, Swadesh K; Sarkar, Devanand; Fisher, Paul B

    2016-07-15

    Abrus agglutinin (AGG), a plant lectin isolated from the seeds of Abrus precatorius, has documented antitumor and immunostimulatory effects in murine models. To examine possible antitumor activity against breast cancer, we established human breast tumor xenografts in athymic nude mice and intraperitoneally administered AGG. AGG inhibited tumor growth and angiogenesis as confirmed by monitoring the expression of Ki-67 and CD-31, respectively. In addition, TUNEL positive cells increased in breast tumors treated with AGG suggesting that AGG mediates anti-tumorigenic activity through induction of apoptosis and inhibition of angiogenesis. On a molecular level, AGG caused extrinsic apoptosis through ROS generation that was AKT-dependent in breast cancer cells, without affecting primary mammary epithelial cells, suggesting potential cancer specificity of this natural compound. In addition, using HUVECs, AGG inhibited expression of the pro-angiogenic factor IGFBP-2 in an AKT-dependent manner, reducing angiogenic phenotypes both in vitro and in vivo. Overall, the present results establish that AGG promotes both apoptosis and anti-angiogenic activities in human breast tumor cells, which might be exploited for treatment of breast and other cancers. PMID:26914517

  9. Efavirenz Has the Highest Anti-Proliferative Effect of Non-Nucleoside Reverse Transcriptase Inhibitors against Pancreatic Cancer Cells.

    Directory of Open Access Journals (Sweden)

    Markus Hecht

    Full Text Available Cancer prevention and therapy in HIV-1-infected patients will play an important role in future. The non-nucleoside reverse transcriptase inhibitors (NNRTI Efavirenz and Nevirapine are cytotoxic against cancer cells in vitro. As other NNRTIs have not been studied so far, all clinically used NNRTIs were tested and the in vitro toxic concentrations were compared to drug levels in patients to predict possible anti-cancer effects in vivo.Cytotoxicity was studied by Annexin-V-APC/7AAD staining and flow cytometry in the pancreatic cancer cell lines BxPC-3 and Panc-1 and confirmed by colony formation assays. The 50% effective cytotoxic concentrations (EC50 were calculated and compared to the blood levels in our patients and published data.The in vitro EC50 of the different drugs in the BxPC-3 pancreatic cancer cells were: Efavirenz 31.5 μmol/l (= 9944 ng/ml, Nevirapine 239 μmol/l (= 63,786 ng/ml, Etravirine 89.0 μmol/l (= 38,740 ng/ml, Lersivirine 543 μmol/l (= 168,523 ng/ml, Delavirdine 171 μmol/l (= 78,072 ng/ml, Rilpivirine 24.4 μmol/l (= 8941 ng/ml. As Efavirenz and Rilpivirine had the highest cytotoxic potential and Nevirapine is frequently used in HIV-1 positive patients, the results of these three drugs were further studied in Panc-1 pancreatic cancer cells and confirmed with colony formation assays. 205 patient blood levels of Efavirenz, 127 of Rilpivirine and 31 of Nevirapine were analyzed. The mean blood level of Efavirenz was 3587 ng/ml (range 162-15,363 ng/ml, of Rilpivirine 144 ng/ml (range 0-572 ng/ml and of Nevirapine 4955 ng/ml (range 1856-8697 ng/ml. Blood levels from our patients and from published data had comparable Efavirenz levels to the in vitro toxic EC50 in about 1 to 5% of all patients.All studied NNRTIs were toxic against cancer cells. A low percentage of patients taking Efavirenz reached in vitro cytotoxic blood levels. It can be speculated that in HIV-1 positive patients having high Efavirenz blood levels pancreatic cancer incidence might be reduced. Efavirenz might be a new option in the treatment of cancer.

  10. High cytotoxicity and anti-proliferative activity of algae extracts on an in vitro model of human hepatocellular carcinoma

    OpenAIRE

    Alves, Celso; Pinteus, Susete; Horta, André; Pedrosa, Rui

    2016-01-01

    Background: Cancer represents a serious threat for human health with high social and economic impacts worldwide. Therefore, the development of new anticancer drugs is of most importance. The aim of the present study was to evaluate the antitumor potential of twelve algae from Portugal coast on an in vitro model of human hepatocellular carcinoma (HepG-2 cells).Results: Both extracts of Asparagopsis armata (1000 µg/ml; 24 h) presented high cytotoxicity with 11.22 ± 2.98 and 1.51 ± 0.38 % of Hep...

  11. New Anti-Inflammatory and Anti-Proliferative Constituents from Fermented Red Mold Rice Monascus purpureus NTU 568

    Directory of Open Access Journals (Sweden)

    Yao-Haur Kuo

    2010-11-01

    Full Text Available Six azaphilonoid derivatives, including two new blue fluorescent monapurfluores A (1 and B (2, two known pyridine-containing molecules, monascopyridines C (3 and D (4, and two known monasfluores A (5 and B (6, were isolated and characterized from red mold rice fermented by Monascus purpureus NTU 568. Structural elucidation of new isolates was based on nuclear magnetic resonance (1H- NMR, 13C-NMR, COSY, HMQC, and HMBC and other spectroscopic analyses. Bioactivity evaluation indicated that 1-6 possessed anti-inflammatory activities with dose-dependent relationships for lipopolysaccharide (LPS-induced nitric oxide production. Furthermore, 1-4 also showed moderate antiproliferative effects against human laryngeal carcinoma (HEp-2 (IC50 = 14.81~20.06 μg/mL and human colon adenocarcinoma (WiDr (IC50 = 12.89~21.14 μg/mL.

  12. Anti-proliferative actions of 2-decylamino-5,8-dimethoxy-1,4-naphthoquinone in vascular smooth muscle cells

    Energy Technology Data Exchange (ETDEWEB)

    Lee, Jung-Jin [Department of Pharmacology, Chungnam National University College of Pharmacy, Daejeon 305-764 (Korea, Republic of); Institute of Drug Research and Development, Chungnam National University, Daejeon 305-764 (Korea, Republic of); Zhang, Wei-Yun; Yi, Hyoseok; Kim, Yohan; Kim, In-Su [Department of Pharmacology, Chungnam National University College of Pharmacy, Daejeon 305-764 (Korea, Republic of); Shen, Gui-Nan; Song, Gyu-Yong [Department of Medicinal Chemistry, Chungnam National University College of Pharmacy, Daejeon 305-764 (Korea, Republic of); Myung, Chang-Seon, E-mail: cm8r@cnu.ac.kr [Department of Pharmacology, Chungnam National University College of Pharmacy, Daejeon 305-764 (Korea, Republic of); Institute of Drug Research and Development, Chungnam National University, Daejeon 305-764 (Korea, Republic of)

    2011-07-22

    Highlights: {yields} 2-Decylamino-DMNQ inhibited PDGF-BB-induced VSMC proliferation in a dose-dependent manner with no apparent cytotoxicity. {yields} 2-Decylamino-DMNQ inhibited PDGF-BB-induced phosphorylation of Erk1/2 and PLC{gamma}1. {yields} 2-Decylamino-DMNQ arrested a G{sub 0}/G{sub 1} cell cycle progression in association with pRb phosphorylation and PCNA expression. {yields} Both U0126, an Erk inhibitor, and U73122, a PLC{gamma} inhibitor, arrested a G{sub 0}/G{sub 1} phase of the cell cycle. -- Abstract: Naphthoquinone derivatives have been reported to possess various pharmacological activities, such as antiplatelet, anticancer, antifungal, and antiviral properties. In this study, we investigated the effects of a newly-synthesized naphthoquinone derivative, 2-decylamino-5,8-dimethoxy-1,4-naphthoquinone (2-decylamino-DMNQ), on VSMC proliferation and examined the molecular basis of the underlying mechanism. In a dose-dependent manner, 2-decylamino-DMNQ inhibited PDGF-stimulated VSMC proliferation with no apparent cytotoxic effect. While 2-decylamino-DMNQ did not affect PDGF-R{beta} or Akt, it did inhibit the phosphorylation of Erk1/2 and PLC{gamma}1 induced by PDGF. Moreover, 2-decylamino-DMNQ suppressed DNA synthesis through the arrest of cell cycle progression at the G{sub 0}/G{sub 1} phase, including the suppression of pRb phosphorylation and a decrease in PCNA expression, which was related to the downregulation of cell cycle regulatory factors, such as cyclin D1/E and CDK 2/4. It was demonstrated that both U0126, an Erk1/2 inhibitor, and U73122, a PLC{gamma} inhibitor, increased the proportion of cells in the G{sub 0}/G{sub 1} phase of the cell cycle. Thus, these results suggest that 2-decylamino DMNQ has an inhibitory effect on PDGF-induced VSMC proliferation and the mechanism of this action is through cell cycle arrest at the G{sub 0}/G{sub 1} phase. This may be a useful tool for studying interventions for vascular restenosis in coronary revascularization procedures and stent implantation.

  13. Two New Oleanane-Type Saponins with Anti-Proliferative Activity from Camellia oleifera Abel. Seed Cake

    Directory of Open Access Journals (Sweden)

    Jian-Fa Zong

    2016-02-01

    Full Text Available Two new oleanane-type saponins, named oleiferasaponins C4 (1 and C5 (2, were isolated from Camellia oleifera Abel. seed cake residue. Their respective structures were identified as 16α-hydroxy-22α-O-angeloyl-23α-aldehyde-28-dihydroxymethylene-olean-12-ene-3β-O-[β-d-galacto-pyranosyl-(1→2]-[β-d-glucopyranosyl-(1→2-β-d-galactopyranosy-(1→3]-β-d-glucopyranosid-uronic acid methyl ester (1 and 16α-hydroxy-22α-O-angeloyl-23α-aldehyde-28-dihydroxy-methylene-olean-12-ene-3β-O-[β-d-galactopyranosyl-(1→2]-[β-d-galactopyranosyl-(1→3]-β-d-glucopyranosiduronic acid methyl ester (2 through 1D- and 2D-NMR, HR-ESI-MS, and GC-MS spectroscopic methods. The two compounds exhibited potent cytotoxic activities against five human tumor cell lines (BEL-7402, BGC-823, MCF-7, HL-60 and KB.

  14. Three new anti-proliferative Annonaceous acetogenins with mono-tetrahydrofuran ring from graviola fruit (Annona muricata).

    Science.gov (United States)

    Sun, Shi; Liu, Jingchun; Kadouh, Hoda; Sun, Xiuxiu; Zhou, Kequan

    2014-06-15

    Bioassay-guided fractionation of the fruit powder of graviola (Annona muricata) yielded three novel compounds: muricins J, K, and L. The compounds are all C35 Annonaceous acetogenins with a mono-tetrahydrofuran ring and four hydroxyls. Their structures were elucidated by spectral methods and chemical modification after isolation via chromatographic techniques and HPLC purification. These three acetogenins demonstrated an antiproliferative against human prostate cancer PC-3 cells.

  15. Discovery at the interface: Toward novel anti-proliferative agents targeting human estrogen receptor/S100 interactions.

    Science.gov (United States)

    Lee, David H; Asare, Bethany K; Rajnarayanan, Rajendram V

    2016-10-17

    Estrogen Receptor Alpha (ER) is expressed in about 70% of breast cancer and mediates various cellular signaling events including cell cycle. The antiestrogen tamoxifen is currently administered to patients in order to induce regression of the tumor growth of estrogen receptor positive (ER+) breast cancer. However, upon continued administration, patients develop resistance to tamoxifen. In addition, calcium binding proteins (EF-hand proteins) such as, Calmodulin and S100, are significantly overexpressed in breast cancer cells, can activate transcription of target genes by directly binding to ER in lieu of estrogen. Calmodulin antagonists (w7 and melatonin) have been shown to significantly inhibit ER mediated activities including cell proliferation and transcriptional activity. Furthermore, S100P is shown to mediate tamoxifen resistance and cell migration capacity in MCF-7 breast cancer cells. Molecules targeting specific ER-EF hand protein interfaces could potentially provide an alternative therapeutic strategy to combat these scenarios. Using theoretical 3D models of ER-S100 protein we identified ER conformation-sensing regions of the interacting EF hand proteins and evaluated their ability to bind to ER in silico and to inhibit breast cancer cell proliferation and viability in vitro. The recognition motif of the binding interface was sensitive to small changes in partner orientation as evidenced by significant anti cell proliferative activity of the short peptide derived from S100P residues 74-78, when compared with a longer peptide with altered orientation of the recognition motif derived from S100P 74-81. Structural clues and pharmacophores from peptide-ER interactions can be used to design novel anti-cancer agents. PMID:27580430

  16. Holographic Waveguided See-Through Display Project

    Data.gov (United States)

    National Aeronautics and Space Administration — To address the NASA need for lightweight, space suit-mounted displays, Luminit proposes a novel Holographic Waveguided See-Through Display. Our proposed Holographic...

  17. ProPath Display Process Overview

    Data.gov (United States)

    Department of Veterans Affairs — This API displays an overview of the process including the description, goals, associated roles (linked to their detailed information). It also displays all of the...

  18. OZ: An Innovative Primary Flight Display Project

    Data.gov (United States)

    National Aeronautics and Space Administration — The proposed SBIR project will develop OZ, an innovative primary flight display for aircraft. The OZ display, designed from "first principles" of vision science,...

  19. Projection/Reflection Heads-up Display

    Data.gov (United States)

    National Aeronautics and Space Administration — To address the NASA need for an EVA information display device, Physical Optics Corporation (POC) proposes to develop a new Projection/Reflection Heads-up Display...

  20. Display-centred applications in ubiquitous computing

    OpenAIRE

    José, Rui; Pinto, Helder

    2006-01-01

    Public displays can play an important enabling role in ubiquitous computing environments. This paper describes an on-going work for a multipurpose, multi-display infrastructure, designed to address the requirements of display-centred applications in ubiquitous computing environments. The system provides an infrastructure in which situated displays can act as portals to the physical space, allowing ubicomp applications to support their association with the physical world by providing them with...

  1. Holographic Helmet-Mounted Display Unit

    Science.gov (United States)

    Burley, James R., II; Larussa, Joseph A.

    1995-01-01

    Helmet-mounted display unit designed for use in testing innovative concepts for display of information to aircraft pilots. Operates in conjunction with computers generating graphical displays. Includes two ocular subunits containing miniature cathoderay tubes and optics providing 40 degrees vertical, 50 degrees horizontal field of view to each eye, with or without stereopsis. In future color application, each ocular subunit includes trichromatic holographic combiner tuned to red, green, and blue wavelengths of phosphors used in development of miniature color display devices.

  2. Capsaicin and N-arachidonoyl-dopamine (NADA) decrease tension by activating both cannabinoid and vanilloid receptors in fast skeletal muscle fibers of the frog.

    Science.gov (United States)

    Trujillo, Xóchitl; Ortiz-Mesina, Mónica; Uribe, Tannia; Castro, Elena; Montoya-Pérez, Rocío; Urzúa, Zorayda; Feria-Velasco, Alfredo; Huerta, Miguel

    2015-02-01

    Previous studies have indicated that vanilloid receptor (VR1) mRNA is expressed in muscle fibers. In this study, we evaluated the functional effects of VR1 activation. We measured caffeine-induced contractions in bundles of the extensor digitorum longus muscle of Rana pipiens. Isometric tension measurements showed that two VR1 agonists, capsaicin (CAP) and N-arachidonoyl-dopamine (NADA), reduced muscle peak tension to 57 ± 4 % and 71 ± 3% of control, respectively. The effect of CAP was partially blocked by a VR1 blocker, capsazepine (CPZ), but the effect of NADA was not changed by CPZ. Because NADA is able to act on cannabinoid receptors, which are also present in muscle fibers, we tested the cannabinoid antagonist AM281. We found that AM281 antagonized both CAP and NADA effects. AM281 alone reduced peak tension to 80 ± 6 % of control. With both antagonists, the CAP effect was completely blocked, and the NADA effect was partially blocked. These results provide pharmacological evidence of the functional presence of the VR1 receptor in fast skeletal muscle fibers of the frog and suggest that capsaicin and NADA reduce tension by activating both cannabinoid and vanilloid receptors.

  3. Considerable Variability in the Efficacy of 8% Capsaicin Topical Patches in the Treatment of Chronic Pruritus in 3 Patients with Notalgia Paresthetica.

    Science.gov (United States)

    Andersen, Hjalte H; Sand, Carsten; Elberling, Jesper

    2016-02-01

    Notalgia paresthetica (NP) is a focal neuropathic itch condition manifesting in intense chronic or recurrent episodic itch in a hyperpigmented, macular, uni- or bilateral skin area located below and/or medially to the scapulae. Achieving satisfactory relieve in NP patients is challenging. In this case-series three female NP patients were treated with 8% capsaicin patches following a spatial quantification of their alloknetic area with a von Frey filament. The use of a von Frey filament in order to delimit the precise area of itch sensitization and thus patch application, proved clinically feasible. Although 8% topical capsaicin relieved itch in all three patients, the duration of the effectiveness varied greatly from only 3 days to >2 months. The treatment was well tolerated in the patients and there appear to be no significant hindrances to applying this treatment with NP as an indication, although it may only exhibit satisfactory effectiveness in certain patients. Placebo-controlled double-blinded trials are needed to confirm the effectiveness of the treatment and assess predictive parameters of the treatment outcome. PMID:26848223

  4. Reconfigurable Full-Page Braille Displays

    Science.gov (United States)

    Garner, H. Douglas

    1994-01-01

    Electrically actuated braille display cells of proposed type arrayed together to form full-page braille displays. Like other braille display cells, these provide changeable patterns of bumps driven by digitally recorded text stored on magnetic tapes or in solid-state electronic memories. Proposed cells contain electrorheological fluid. Viscosity of such fluid increases in strong electrostatic field.

  5. 辣椒素理化性质及体外透皮性能的研究%Physical and Chemical Properties and Percutaneous Permeation of Capsaicin

    Institute of Scientific and Technical Information of China (English)

    刘然; 王承潇; 汤秀珍; 张皓; 韩伟

    2012-01-01

    OBJECTIVE To study the physical and chemical properties and transdermal delivery characteristics of, capsaicin. METHODS Equilibrium solubility method, ultraviolet spectrophotometry, bottle-shaking method, differential scanning caiorimetry ( DSC) and in vitro diffusion cell method were used to determine the apparent solubility, dissociation constant, apparent oil/water partition coefficient, melting point and percutaneous penetration of capsaicin, respectively. And the permeation characteristics were evaluated by lag time method. RESULTS Capsaicin was slightly dissolved in water, and the apparent solubility was ( 22. 85 ± 0. 06 ) mg · L-1. It was a weak base with a dissociation constant of( 10. 25 ±0. 11). The apparent oil/water partition coefficient of capsaicin changed with the pH value, and increased when pH was greater than 8. Its melting point was 60. 20 ℃. The residence time(tlag)was (2. 437 ± 0. 273 ) h, the permeability coefficient (P) (7. 012 ± 0. 341) × 10 -1 cm · h -1 , and the percutaneous penetration rate (Js) (4. 647 ±0. 226) μg · cm-2 · h-1. CONCLUSION Capsaicin possesses appropriate physical and chemical properties for percutaneous penetration and exhibits excellent percutaneous penetration.%目的 研究辣椒素的理化性质及体外透皮性能.方法 采用平衡溶解度法、紫外分光光度法、摇瓶法、差示扫描量热法和体外扩散池法,分别测定辣椒素的表观溶解度、解离常数、表观油/水分配系数、熔点和体外经皮渗透参数,并采用滞留时间法评价其经皮渗透特性.结果 辣椒素极微溶于水,表观溶解度为(22.85±0.06) mg·L-1;为弱碱,解离常数为(10.25±0.11);表观油/水分配系数随pH的增加而变化,当pH >8时lg P增加;熔点为60.20℃.辣椒素的滞留时间(tlag)为(2.437±0.273)h,体外经皮渗透参数(P)为(7.012±0.341)×10-2cm·h-1,渗透速率(Js)为(4.647±0.226) μg·cm-2·h-1.结论 辣椒素具有适宜经皮渗透的理化性质及较好的经皮渗透性能.

  6. 辣椒素/SiO_2微球的制备%Preparation of Capsaicin/SiO_2 microspheres and the optimization of its encapsulation efficiency

    Institute of Scientific and Technical Information of China (English)

    尚红梅; 马永梅; 孙睿; 李引乾; 陈辉玲; 童德文; 董玲玲; 曹新宇

    2012-01-01

    【Objective】 The study was conducted to prepare Capsaicin/SiO2 microspheres,and to optimize their preparation parameters.【Method】 Capsaicin/SiO2 microspheres were prepared by O/W/O multiple emulsion,and the encapsulation efficiency was detected by UV spectrophotometry.The preparation parameters,such as amount of the external oil stabilizer HPC,water phase stabilizer PEG,hydrophilic surfactant Tween 20 and lipophilic surfactant Span 80 were optimized by L9(34)orthogonal method according to the Capsaicin encapsulation efficiency.The morphology and size of the microspheres were characterized by SEM and optical microscopy.【Result】 Spherical hollow Capsaicin/SiO2 microspheres were prepared by O/W/O multiple emulsion.The average diameter of the microsphere was about(4.62±0.12) μm,and the dispersion coefficient(ε)was ca.0.76.If there was no cross-interaction,the optimal process parameters for high encapsulation efficiency should be:HPC and Span 80 contents should be 1.5% and 0.5% respectively of the external oil phase,and PEG and Tween 20 content should be 4.0% and 0.5% respectively of the water phase.【Conclusion】 The process parameters were optimized,by which Capsaicin/SiO2 microspheres with comparatively high encapsulation efficiency can be prepared.%【目的】制备辣椒素/SiO2微球,并对其制备参数进行优化。【方法】以油包水包油(O/W/O)复乳法制备辣椒素/SiO2微球,采用扫描电镜和光学显微镜检测微球形态和粒径,紫外分光光度法测定微球包封率。通过L9(34)正交试验,对外油相稳定剂羟丙基纤维素(HPC)、水相稳定剂聚乙二醇(PEG)、亲水性表面活性剂Tween 20和亲油性表面活性剂Span 80的用量进行优化。【结果】用O/W/O复乳法制得了具有中空结构的辣椒素/SiO2微球,微球平均粒径(4.62±0.12)μm,分散系数ε为0.76。在不考虑交互作用的条件下,优选出较高包封率的微球制备参数组合

  7. CERN students display their work

    CERN Multimedia

    Anaïs Schaeffer

    2011-01-01

    The first poster session by students working on the LHC experiments, organised by the LPCC, was a great success. Showcasing the talents of over a hundred young physicists from all over the world, it was an opportunity for everyone at CERN to check out the wide range of research work being done by the new generation of physicists at CERN.   At 5.30 p.m. on Wednesday 23 March, the first poster session by CERN students took place in Restaurant No.1, where no fewer than 87 posters went on public display. The students were split into 8 groups according to their research field* and all were on hand to answer the questions of an inquisitive audience. TH Department's Michelangelo Mangano, who is head of the LHC Physics Centre at CERN (LPCC) and is responsible for the initiative, confirms that nothing was left to chance, even the choice of date: "We wanted to make the most of the general enthusiasm around the winter conferences and the meeting of the LHC Experiments Committee to present the stud...

  8. Citizenship displayed by disabled people

    Directory of Open Access Journals (Sweden)

    Eliana Prado Carlino

    2010-12-01

    Full Text Available By investigating the processes by which successful teachers become activate citizens and by listening to the diversity and richness of their life and formation stories, this work became possible. Its aim is to display some of the utterances of two Down Syndrome individuals and their active-citizenship activities. Their stories were told in the reports of two teachers when describing their personal and professional history, and were considered to be an integral part of it. Thus, some of the utterances and perceptions with which these two individuals elaborate their references, their worldview and their active-citizenship activity are evidenced in this paper. This article is based on the language conceptions of Vygotsky and Bakhtin who defend the idea that the group and the social mentality are ingrain in the individual. Hence, the history of one person reveals that of many others, since there is a deep link between the individual and the social in the formation of a subjective worldview. As a result, it can be easily seen that the utterances expressed by the participants in this research cannot be considered strictly individual because enunciation is social in nature. Despite the fact that the utterances are those of individuals, they manifest a collective reality. This demonstrates the real advantages and possibilities that deficient people get from their participation and intervention in society.

  9. Irradiation from video display terminals

    International Nuclear Information System (INIS)

    Video display terminals (VDT's) are in common use by computer operators. In the last years this group of workers has expressed growing concern about their work environment and possible hazardious effects in connection with radiation emission from VDT's. Radiation types and levels of emission and possible biological effects have been the subject of research activity in Norway and in other countries. This report summarizes the various radiation types and their levels of emission from VDT's. An overview of recent epidemiological studies and animal experiments, and the conclusions given by the research groups are also presented. The conclusions drawn in this report based on the current knowledge are: Radiation, other than low frequency pulsed magnetic fields, have low and negligible emission levels and will not represent any health hazard to VDT-operator or to the foetus of pregnant operators. The biological effects of low frequency pulsed mangetic fields have been the subject of epidemiological studies and animal experiments. Epidemiological studies carried out in Canada, Finland, Sweden and Norway gave no support for any correlation between pregnancy complications and operation of VDT's. From animal experiments it has so far been impossible to assert an effect on pregnancy outcome from low frequency pulsed magnetic fields

  10. Ultrabarrier Flexible Substrates for Flat Panel Displays

    Energy Technology Data Exchange (ETDEWEB)

    Burrows, Paul E.; Graff, Gordon L.; Gross, Mark E.; Martin, Peter M.; Shi, Ming-Kun; Hall, Michael G.; Mast, Eric S.; Bonham, Charles C.; Bennett, Wendy D.; Sullivan, Michael B.

    2001-05-01

    We describe a flexible, transparent plastic substrate for flat panel display applications. Using roll-coating techniques, we apply a composite thin film barrier to commercially available polymers, which restricts moisture and oxygen permeation to undetectable levels. The barrier film can be capped with a thin film of transparent conductive oxide in the same roll-coater, yielding an engineered substrate (Barix™) for next generation, rugged, lightweight or flexible displays. The substrate is sufficiently impermeable to moisture and oxygen for application to moisture-sensitive display applications, such as organic light emitting displays (OLEDs). This enables, for the first time, lightweight and flexible emissive organic displays.

  11. Synthesis, characterization, in silico approach and in vitro antiproliferative activity of RPF151, a benzodioxole sulfonamide analogue designed from capsaicin scaffold

    DEFF Research Database (Denmark)

    Tavares, Mauricio T.; Pasqualoto, Kerly F. M.; van de Streek, Jacco;

    2015-01-01

    RPF151, an alkylsulfonamide capsaicin analogue, was synthesized by a simple and efficient one-step methodology. The compound was characterized by 1H and 13C NMR, elemental analysis, IR and melting point. The crystal structure of RPF151 was determined by X-ray powder diffraction and its experimental...

  12. Capsaicin-sensitive C- and A-fibre nociceptors control long-term potentiation-like pain amplification in humans.

    Science.gov (United States)

    Henrich, Florian; Magerl, Walter; Klein, Thomas; Greffrath, Wolfgang; Treede, Rolf-Detlef

    2015-09-01

    Long-term potentiation in the spinal dorsal horn requires peptidergic C-fibre activation in animals. Perceptual correlates of long-term potentiation following high-frequency electrical stimulation in humans include increased sensitivity to electrical stimuli at the high frequency stimulation site (homotopic pain-long-term potentiation) and increased sensitivity to pinprick surrounding the high frequency stimulation site (heterotopic pain-long-term potentiation, equivalent to secondary hyperalgaesia). To characterize the peripheral fibre populations involved in induction of pain-long-term potentiation, we performed two selective nerve block experiments in 30 healthy male volunteers. Functional blockade of TRPV1-positive nociceptors by high-concentration capsaicin (verified by loss of heat pain) significantly reduced pain ratings to high frequency stimulation by 47% (P pain-long-term potentiation by 71% (P pain-long-term potentiation by 92% (P pain to pinprick) significantly reduced pain ratings to high frequency stimulation by 37% (P pain-long-term potentiation (-5%). It had a marginal effect on heterotopic pain-long-term potentiation (-35%, P = 0.059), while the area of secondary hyperalgesia remained unchanged (-2%, P = 0.88). In conclusion, all nociceptor subclasses contribute to high frequency stimulation-induced pain (with a relative contribution of C > Aδ fibres, and an equal contribution of TRPV1-positive and TRPV1-negative fibres). TRPV1-positive C-fibres are the main inducers of both homotopic and heterotopic pain-long-term potentiation. TRPV1-positive A-fibres contribute substantially to the induction of heterotopic pain-long-term potentiation. TRPV1-negative C-fibres induce a component of homotopic self-facilitation but not heterotopic pain-long-term potentiation. TRPV1-negative A-fibres are the main afferents mediating pinprick pain and hyperalgesia, however, they do not appear to contribute to the induction of pain-long-term potentiation. These

  13. Military display market segment: wearable and portable

    Science.gov (United States)

    Desjardins, Daniel D.; Hopper, Darrel G.

    2003-09-01

    The military display market (MDM) is analyzed in terms of one of its segments, wearable and portable displays. Wearable and portable displays are those embedded in gear worn or carried by warfighters. Categories include hand-mobile (direct-view and monocular/binocular), palm-held, head/helmet-mounted, body-strapped, knee-attached, lap-born, neck-lanyard, and pocket/backpack-stowed. Some 62 fielded and developmental display sizes are identified in this wearable/portable MDM segment. Parameters requiring special consideration, such as weight, luminance ranges, light emission, viewing angles, and chromaticity coordinates, are summarized and compared. Ruggedized commercial versus commercial off-the-shelf designs are contrasted; and a number of custom displays are also found in this MDM category. Display sizes having aggregate quantities of 5,000 units or greater or having 2 or more program applications are identified. Wearable and portable displays are also analyzed by technology (LCD, LED, CRT, OLED and plasma). The technical specifications and program history of several high-profile military programs are discussed to provide a systems context for some representative displays and their function. As of August 2002 our defense-wide military display market study has documented 438,882 total display units distributed across 1,163 display sizes and 438 weapon systems. Wearable and portable displays account for 202,593 displays (46% of total DoD) yet comprise just 62 sizes (5% of total DoD) in 120 weapons systems (27% of total DoD). Some 66% of these wearable and portable applications involve low information content displays comprising just a few characters in one color; however, there is an accelerating trend towards higher information content units capable of showing changeable graphics, color and video.

  14. Display Blocks: a Set of Cubic Displays for Tangible, Multi-Perspective Data Exploration

    OpenAIRE

    Pla i Conesa, Pol; Maes, Patricia

    2013-01-01

    This paper details the design and implementation of a new type of display technology. Display Blocks are a response to two major limitations of current displays: dimensional compression and physical-digital disconnect. Each Display Block consists of six organic light emitting diode (OLED) screens, arranged in a cubic form factor. We explore the possibilities that this type of display holds for data visualization, manipulation and exploration. To this end, we accompany our design with a set of...

  15. Display elements and gaps: a comparison of flat panel display characteristics

    OpenAIRE

    Spenkelink, G.P.J.; Besuijen, J.

    1992-01-01

    The relation between typical flat panel display characteristics and display quality was studied. Subjective preferences were obtained with respect to simulated black-on-white flat panel displays. The displays differed in the sort of separation between the display elements and the shape of these elements. Further, the height/width ratio of the front was studied in relation with a fixed font matrix. The preferences were obtained through a paired comparison of all possible pairs of simulated dis...

  16. 微波碱法提取辣椒碱工艺研究%Study on Extraction Technology of Capsaicin by Microwave Alkal i Method

    Institute of Scientific and Technical Information of China (English)

    张容鹄; 窦志浩; 段宙位; 何艾; 谢辉

    2014-01-01

    The extraction technology of capsaicin from Capsicum chinense of Hainan is studied by microwave alkali method. The influence factors of sodium hydroxide solution concentration, extraction time,extraction temperature,extraction power are discussed and analyzed through single factor and orthogonal tests.Taking capsaicin extraction yield as evaluation index,the extraction conditions are optimized.The results show that the optimum extraction conditions are:Capsicum chinense after being dried,grinded and filtered with 30 mesh of sieve,under microwave extraction condition,the concentration of sodium hydroxide is 2%,solid-liquid ratio is 1∶14,extraction time is 15 min,extraction temperature is 50 ℃,power is 300 W,capsaicin compound optimization extraction rate is 1.103%,purity of crude product is 20.7%.%以黄灯笼辣椒粉为原料,研究微波碱法提取辣椒碱的工艺技术。以辣椒碱得率为指标,通过单因素试验和正交试验L9(34)探讨了氢氧化钠溶液的浓度、浸提时间、提取温度、提取功率对辣椒碱提取率的影响,优化了提取条件。结果表明最佳提取条件:黄灯笼辣椒干燥粉碎过30目筛后,在微波辅助下,氢氧化钠的浓度为2%,料液比为1∶14,提取时间为15 min,提取温度为50℃,功率为300 W,优化后提取的辣椒碱化合物得率为1.103%,得到粗品的纯度为20.7%。

  17. Pharmacodynamic analysis of the analgesic effect of capsaicin 8% patch (QutenzaTM in diabetic neuropathic pain patients: detection of distinct response groups

    Directory of Open Access Journals (Sweden)

    Martini C

    2012-03-01

    Full Text Available Christian Martini1,*, Ashraf Yassen2,*, Erik Olofsen1, Paul Passier2, Malcom Stoker3, Albert Dahan1 1Department of Anesthesiology, Leiden University Medical Center, Leiden, The Netherlands; 2Global Clinical Pharmacology and Exploratory Development, Astellas Pharma Global Development Europe, Leiderdorp, The Netherlands; 3Global Medical Sciences, Astellas Pharma Global Development Europe, Leiderdorp, The Netherlands*These authors contributed equally to this workAbstract: Treatment of chronic pain is associated with high variability in the response to pharmacological interventions. A mathematical pharmacodynamic model was developed to quantify the magnitude and onset/offset times of effect of a single capsaicin 8% patch application in the treatment of painful diabetic peripheral neuropathy in 91 patients. In addition, a mixture model was applied to objectively match patterns in pain-associated behavior. The model identified four distinct subgroups that responded differently to treatment: 3.3% of patients (subgroup 1 showed worsening of pain; 31% (subgroup 2 showed no change; 32% (subgroup 3 showed a quick reduction in pain that reached a nadir in week 3, followed by a slow return towards baseline (16% ± 6% pain reduction in week 12; 34% (subgroup 4 showed a quick reduction in pain that persisted (70% ± 5% reduction in week 12. The estimate of the response-onset rate constant, obtained for subgroups 1, 3, and 4, was 0.76 ± 0.12 week-1 (median ± SE, indicating that every 0.91 weeks the pain score reduces or increases by 50% relative to the score of the previous week (= t½. The response-offset rate constant could be determined for subgroup 3 only and was 0.09 ± 0.04 week-1 (t½ 7.8 weeks. The analysis allowed separation of a heterogeneous neuropathic pain population into four homogenous subgroups with distinct behaviors in response to treatment with capsaicin. It is argued that this model-based approach may have added value in analyzing

  18. Data display with the Q system

    International Nuclear Information System (INIS)

    The Q data-acquisition system for PDP-11 mini-computers at the Clinton P. Anderson Meson Physics Facility (LAMPF) provides experimenters with basic tools for on-line data display. Tasks are available to plot one- and two-parameter histograms on Tektronix 4000 series storage-tube terminals. The histograms to be displayed and the display format may be selected with simple keyboard commands. A task is also available to create and display live two-parameter scatter plots for any acquired or calculated quantities. Other tasks in the system manage the display data base, list display parameters and histogram contents on hardcopy devices, and save core histograms on disk or tape for off-line analysis. 8 figures

  19. Laser-driven polyplanar optic display

    Energy Technology Data Exchange (ETDEWEB)

    Veligdan, J.T.; Biscardi, C.; Brewster, C.; DeSanto, L. [Brookhaven National Lab., Upton, NY (United States). Dept. of Advanced Technology; Beiser, L. [Leo Beiser Inc., Flushing, NY (United States)

    1998-01-01

    The Polyplanar Optical Display (POD) is a unique display screen which can be used with any projection source. This display screen is 2 inches thick and has a matte-black face which allows for high contrast images. The prototype being developed is a form, fit and functional replacement display for the B-52 aircraft which uses a monochrome ten-inch display. The new display uses a 200 milliwatt green solid-state laser (532 nm) as its optical source. In order to produce real-time video, the laser light is being modulated by a Digital Light Processing (DLP) chip manufactured by Texas Instruments, Inc. A variable astigmatic focusing system is used to produce a stigmatic image on the viewing face of the POD. In addition to the optical design, the authors discuss the DLP chip, the optomechanical design and viewing angle characteristics.

  20. Three-dimensional Imaging, Visualization, and Display

    CERN Document Server

    Javidi, Bahram; Son, Jung-Young

    2009-01-01

    Three-Dimensional Imaging, Visualization, and Display describes recent developments, as well as the prospects and challenges facing 3D imaging, visualization, and display systems and devices. With the rapid advances in electronics, hardware, and software, 3D imaging techniques can now be implemented with commercially available components and can be used for many applications. This volume discusses the state-of-the-art in 3D display and visualization technologies, including binocular, multi-view, holographic, and image reproduction and capture techniques. It also covers 3D optical systems, 3D display instruments, 3D imaging applications, and details several attractive methods for producing 3D moving pictures. This book integrates the background material with new advances and applications in the field, and the available online supplement will include full color videos of 3D display systems. Three-Dimensional Imaging, Visualization, and Display is suitable for electrical engineers, computer scientists, optical e...

  1. Spectroradiometric characterization of autostereoscopic 3D displays

    Science.gov (United States)

    Rubiño, Manuel; Salas, Carlos; Pozo, Antonio M.; Castro, J. J.; Pérez-Ocón, Francisco

    2013-11-01

    Spectroradiometric measurements have been made for the experimental characterization of the RGB channels of autostereoscopic 3D displays, giving results for different measurement angles with respect to the normal direction of the plane of the display. In the study, 2 different models of autostereoscopic 3D displays of different sizes and resolutions were used, making measurements with a spectroradiometer (model PR-670 SpectraScan of PhotoResearch). From the measurements made, goniometric results were recorded for luminance contrast, and the fundamental hypotheses have been evaluated for the characterization of the displays: independence of the RGB channels and their constancy. The results show that the display with the lower angle variability in the contrast-ratio value and constancy of the chromaticity coordinates nevertheless presented the greatest additivity deviations with the measurement angle. For both displays, when the parameters evaluated were taken into account, lower angle variability consistently resulted in the 2D mode than in the 3D mode.

  2. Conceptual Design of Industrial Process Displays

    DEFF Research Database (Denmark)

    Pedersen, C.R.; Lind, Morten

    1999-01-01

    by a simple example from a plant with batch processes. Later the method is applied to develop a supervisory display for a condenser system in a nuclear power plant. The differences between the continuous plant domain of power production and the batch processes from the example are analysed and broad...... design method that matches the industrial practice of modular plant design and satisfies the needs of reusability of display design solutions. The main considerations in display design in the industry are to specify the operator's activities in detail, to extract the information the operators need from...... the plant design specification and documentation, and finally to present this information. The form of the display is selected from existing standardized display elements such as trend curves, mimic diagrams, ecological interfaces, etc. Further knowledge is required to invent new display elements. That is...

  3. Matrix silicon microcathodes for field emission displays

    Directory of Open Access Journals (Sweden)

    Druzhynin А. A.

    2009-11-01

    Full Text Available The existing and perspective types of flat displays are analyzed. The structure of field emission display pixel cell, materials of microcathodes and technologies of their manufacturing are considered. Matrix silicon microcathodes for field emission displays are offered and the sequence of base operations of their manufacturing on SOI-substrate is developed. The density of field emission current of the matrix microcathode is calculated.

  4. AMOLED as a green solution for display

    Science.gov (United States)

    Lin, Yu-Hsin; Hsu, Shih-Feng; Lee, Chung-Chun; Huang, Wei-Pang

    2009-08-01

    AMOLED(active matrix OLED) is known as the next generation display technology due to its better display quality, thin form factor, lower power consumption, etc. With increasing demand of environment-friendly technology, OLED had become a green solution for display. Additionally, due to its simple device structure, extra function could be easily integrated. In this paper, in-cell touch AMOLED is also described briefly.

  5. Pengaruh Display Produk pada Keputusan Pembelian Konsumen

    Directory of Open Access Journals (Sweden)

    Ina Melati

    2012-10-01

    Full Text Available Most of ritel outlet recently using product display as a one of their best marketing strategy, the reason is quiet easy to be understood, since consumers are too easy to be teased by those kind of beautiful product display that is being displayed by the retail outlet. The good retail outlets are trying their best to design and make the very good product display, so they can attract more consumers and make them not thinking twice to visit their store and purchase lots of thing. Clearly seeing that an attractive product design is able to influence a consumer to make a buying decision.

  6. Refreshable Braille displays using EAP actuators

    Science.gov (United States)

    Bar-Cohen, Yoseph

    2010-04-01

    Refreshable Braille can help visually impaired persons benefit from the growing advances in computer technology. The development of such displays in a full screen form is a great challenge due to the need to pack many actuators in small area without interferences. In recent years, various displays using actuators such as piezoelectric stacks have become available in commercial form but most of them are limited to one line Braille code. Researchers in the field of electroactive polymers (EAP) investigated methods of using these materials to form full screen displays. This manuscript reviews the state of the art of producing refreshable Braille displays using EAP-based actuators.

  7. Microencapsulated Electrophoretic Films for Electronic Paper Displays

    Science.gov (United States)

    Amundson, Karl

    2003-03-01

    Despite the dominance of liquid crystal displays, they do not perform some functions very well. While backlit liquid crystal displays can offer excellent color performance, they wash out in bright lighting and suffer from high power consumption. Reflective liquid crystal displays have limited brightness, making these devices challenging to read for long periods of time. Flexible liquid crystal displays are difficult to manufacture and keep stable. All of these attributes (long battery lifetime, bright reflective appearance, compatibility with flexible substrates) are traits that would be found in an ideal electronic paper display - an updateable substitute for paper that could be employed in electronic books, newspapers, and other applications. I will discuss technologies that are being developed for electronic-paper-like displays, and especially on particle-based technologies. A microencapsulated electrophoretic display technology is being developed at the E Ink corporation. This display film offers offer high brightness and an ink-on-paper appearance, compatibility with flexible substrates, and image stability that can lead to very low power consumption. I will present some of the physical and chemical challenges associated with making display films with high performance.

  8. Energy Awareness Displays - Making the Invisible Visible

    NARCIS (Netherlands)

    Börner, Dirk

    2011-01-01

    Börner, D. (2011). Energy Awareness Displays - Making the Invisible Visible. Presentation given at the Startbijeenkomst SURFnet Innovatieregeling Duurzaamheid & ICT. May, 13, 2011, Utrecht, The Netherlands.

  9. Capsaicin mimics mechanical load-induced intracellular signaling events: involvement of TRPV1-mediated calcium signaling in induction of skeletal muscle hypertrophy.

    Science.gov (United States)

    Ito, Naoki; Ruegg, Urs T; Kudo, Akira; Miyagoe-Suzuki, Yuko; Takeda, Shin'ichi

    2013-01-01

    Mechanical load-induced intracellular signaling events are important for subsequent skeletal muscle hypertrophy. We previously showed that load-induced activation of the cation channel TRPV1 caused an increase in intracellular calcium concentrations ([Ca ( 2+) ]i) and that this activated mammalian target of rapamycin (mTOR) and promoted muscle hypertrophy. However, the link between mechanical load-induced intracellular signaling events, and the TRPV1-mediated increases in [Ca ( 2+) ]i are not fully understood. Here we show that administration of the TRPV1 agonist, capsaicin, induces phosphorylation of mTOR, p70S6K, S6, Erk1/2 and p38 MAPK, but not Akt, AMPK or GSK3β. Furthermore, the TRPV1-induced phosphorylation patterns resembled those induced by mechanical load. Our results continue to highlight the importance of TRPV1-mediated calcium signaling in load-induced intracellular signaling pathways.

  10. Additive and subtractive transparent depth displays

    NARCIS (Netherlands)

    Kooi, F.L.; Toet, A.

    2003-01-01

    Image fusion is the generally preferred method to combine two or more images for visual display on a single screen. We demonstrate that perceptual image separation may be preferable over perceptual image fusion for the combined display of enhanced and synthetic imagery. In this context image separat

  11. Language Display: Authenticating Claims to Social Identity.

    Science.gov (United States)

    Eastman, Carol M.; Stein, Roberta F.

    1993-01-01

    Discusses "language display," a language use strategy whereby members of one group lay claims to attributes associated with another, conveying messages of social, professional, ethnic identity. Examples from academia, politics, business, and advertising reveal language display functions as artifact of crossing linguistic boundaries without…

  12. Imager displays free fall in stop action

    Science.gov (United States)

    Frazer, R. E.

    1981-01-01

    Microprocessor-controlled imaging system displays sequence of "frozen" images of free-falling object, using video cameras positioned along fall. Strobe lights flash as object passes each camera's viewfield. Sequence stored on video disk and displayed on television monitor is stop-action record of fall dynamics. With modification, system monitiors other high speed phenomena.

  13. New control system: displays on stations screens

    International Nuclear Information System (INIS)

    Setting applications display on control stations screens uses X-WINDOWS and graphic interface MOTIF. Representation of Y=f(x) and of data tables are displayed by the utilization P-GRAPHICS package using simplified functions of GOBE library routines. (A.B.). 1 fig

  14. Monitor displays in radiology: Part 2

    International Nuclear Information System (INIS)

    Monitor displays play an important role in modern radiology practice. Practicing radiologists need to be familiar with the various performance parameters of medical-grade displays. A certain amount of technical knowledge is useful when making purchasing decisions since the right choice of equipment can have a great impact on the accuracy, efficiency, and speed in the radiology department

  15. Monitor displays in radiology: Part 1

    International Nuclear Information System (INIS)

    Monitor displays are an integral part of today's radiology work environment, attached to workstations, USG, CT/MRI consoles and PACS terminals. For each modality and method of use, the correct display monitor needs to be deployed. It helps to have a basic understanding of how monitors work and what are the issues involved in their selection

  16. A duality theorem for Dieudonne displays

    OpenAIRE

    Lau, Eike

    2008-01-01

    We show that the Zink equivalence between p-divisible groups and Dieudonne displays over a complete local ring with perfect residue field of characteristic p is compatible with duality. The proof relies on a new explicit formula for the p-divisible group associated to a Dieudonne display.

  17. Recent progress in flexible OLED displays

    Science.gov (United States)

    Hack, Michael G.; Weaver, Michael S.; Mahon, Janice K.; Brown, Julie J.

    2001-09-01

    Organic light emitting device (OLED) technology has recently been shown to demonstrate excellent performance and cost characteristics for use in numerous flat panel display (FPD) applications. OLED displays emit bright, colorful light with excellent power efficiency, wide viewing angle and video response rates. OLEDs are also demonstrating the requisite environmental robustness for a wide variety of applications. OLED technology is also the first FPD technology with the potential to be highly functional and durable in a flexible format. The use of plastic and other flexible substrate materials offers numerous advantages over commonly used glass substrates, including impact resistance, light weight, thinness and conformability. Currently, OLED displays are being fabricated on rigid substrates, such as glass or silicon wafers. At Universal Display Corporation (UDC), we are developing a new class of flexible OLED displays (FOLEDs). These displays also have extremely low power consumption through the use of electrophosphorescent doped OLEDs. To commercialize FOLED technology, a number of technical issues related to packaging and display processing on flexible substrates need to be addressed. In this paper, we report on our recent results to demonstrate the key technologies that enable the manufacture of power efficient, long-life flexible OLED displays for commercial and military applications.

  18. A visual-display and storage device

    Science.gov (United States)

    Bosomworth, D. R.; Moles, W. H.

    1972-01-01

    Memory and display device uses cathodochromic material to store visual information and fast phosphor to recall information for display and electronic processing. Cathodochromic material changes color when bombarded with electrons, and is restored to its original color when exposed to light of appropiate wavelength.

  19. Three-dimensional hologram display system

    Science.gov (United States)

    Mintz, Frederick (Inventor); Chao, Tien-Hsin (Inventor); Bryant, Nevin (Inventor); Tsou, Peter (Inventor)

    2009-01-01

    The present invention relates to a three-dimensional (3D) hologram display system. The 3D hologram display system includes a projector device for projecting an image upon a display medium to form a 3D hologram. The 3D hologram is formed such that a viewer can view the holographic image from multiple angles up to 360 degrees. Multiple display media are described, namely a spinning diffusive screen, a circular diffuser screen, and an aerogel. The spinning diffusive screen utilizes spatial light modulators to control the image such that the 3D image is displayed on the rotating screen in a time-multiplexing manner. The circular diffuser screen includes multiple, simultaneously-operated projectors to project the image onto the circular diffuser screen from a plurality of locations, thereby forming the 3D image. The aerogel can use the projection device described as applicable to either the spinning diffusive screen or the circular diffuser screen.

  20. Interruption and Pausing of Public Display Games

    DEFF Research Database (Denmark)

    Feuchtner, Tiare; Walter, Robert; Müller, Jörg

    We present a quantitative and qualitative analysis of interruptions of interaction with a public display game, and explore the use of a manual pause mode in this scenario. In previous public display installations we observed users frequently interrupting their interaction. To explore ways...... of supporting such behavior, we implemented a gesture controlled multiuser game with four pausing techniques. We evaluated them in a field study analyzing 704 users and found that our pausing techniques were eagerly explored, but rarely used with the intention to pause the game. Our study shows...... that interactions with public displays are considerably intermissive, and that users mostly interrupt interaction to socialize and mainly approach public displays in groups. We conclude that, as a typical characteristic of public display interaction, interruptions deserve consideration. However, manual pause modes...

  1. The display of portable infrared measuring temperature

    Science.gov (United States)

    Qian, Yitao; Gu, Guohua; Sui, Xiubao

    2014-11-01

    In recent years based on security, quality supervision, inspection and medical for the urgent need of infrared temperature measurement and infrared display technology, coupled with embedded system to achieve rapid development, which is widely used in the electronic products and the field of intelligent instruments and industrial control, this paper has designed a kind of more comprehensive, more efficient and more intuitive infrared thermometer. Unlike previous handheld infrared thermometer, we regard an embedded Linux system as the system, with its open source code, support most mainstream hardware platforms, unified peripheral interface and can be customized, to build an embedded infrared system that has provided strong system support; the pseudocolor techniques and Qt interface display technology make the image more colorful and the picture function more diverse; With ARM microprocessor as the display and temperature measuring platform, it costs reduction and reduce volume and power consumption; the FrameBuffer interface technology and multithreading technology realize the smooth real-time display. And ultimately the display size of real-time infrared image is 640 * 480 at a speed of 25 frames / sec. What is more, display is equipped with the menu option so that thermometer can be required to complete the operation through the button. The temperature display system aims at small volume, easy to use and flexible. I believe this thermometer will have a good application prospect.

  2. Flexible display technology for the objective force

    Science.gov (United States)

    Pellegrino, John M.; Wood, Gary L.; Morton, David C.; Forsythe, Eric W.; Girolamo, Henry J.

    2003-09-01

    The Army has initiated a flexible display research program. This program is part of the Army's strategy to create technologies that will enable revolutionary designs and transformational weapons systems for the Objective Force. The ARL flexible display program is more general than just for the dismounted soldier-it will also have implications for air and vehicular crews, and for the other services, even though it is not a DoD tri-service program per se. "Flexible" is defined in the program as displays that operate under conditions from conformal applications, limited flexing, to rollable displays for compact storage. The Army program will include display manufacturing concepts that enable roll-to-roll processes reduce cost, to tap a strong U.S. domestic industrial strength, and, eventually, to enable fabrication of very large sizes. There is commercial interest in flexible displays for applications ranging from wearable electronics for road-warriors and gamers to large screen 71-in. 1920x1200 color pixel consumer high definition television sets for walls. Industry willingness to cost share will be a key criterion in identifying investment opportunities that are necessary and timely from among all that may be envisioned. Some anticipated military applications and a roadmap are presented that identify the technology barriers at the materials, device and manufacturing levels to the creation of flexible display technology.

  3. SNS online display technologies for EPICS

    International Nuclear Information System (INIS)

    The ubiquitousness of web clients from personal computers to cell phones results in a growing demand for web-based access to control system data. At the Oak Ridge National Laboratory Spallation Neutron Source (SNS) we have investigated different technical approaches to provide read access to data in the Experimental Physics and Industrial Control System (EPICS) for a wide variety of web client devices. The core web technology, HTTP, is less than ideal for online control system displays. Appropriate use of Ajax, especially the Long Poll paradigm, can alleviate fundamental HTTP limitations. The SNS Status web uses basic Ajax technology to generate generic displays for a wide audience. The Dashboard uses Long Poll and more client-side Java-Script to offer more customization and faster updates for users that need specialized displays. The Web OPI uses RAP for web access to any BOY display, offering utmost flexibility because users can create their own BOY displays in CSS. These three approaches complement each other. Users can access generic status displays with zero effort, invest time in creating their fully customized displays for the Web OPI, or use the Dashboard as an intermediate solution

  4. [Odor sensing system and olfactory display].

    Science.gov (United States)

    Nakamoto, Takamichi

    2014-01-01

    In this review, an odor sensing system and an olfactory display are introduced into people in pharmacy. An odor sensing system consists of an array of sensors with partially overlapping specificities and pattern recognition technique. One of examples of odor sensing systems is a halitosis sensor which quantifies the mixture composition of three volatile sulfide compounds. A halitosis sensor was realized using a preconcentrator to raise sensitivity and an electrochemical sensor array to suppress the influence of humidity. Partial least squares (PLS) method was used to quantify the mixture composition. The experiment reveals that the sufficient accuracy was obtained. Moreover, the olfactory display, which present scents to human noses, is explained. A multi-component olfactory display enables the presentation of a variety of smells. The two types of multi-component olfactory display are described. The first one uses many solenoid valves with high speed switching. The valve ON frequency determines the concentration of the corresponding odor component. The latter one consists of miniaturized liquid pumps and a surface acoustic wave (SAW) atomizer. It enables the wearable olfactory display without smell persistence. Finally, the application of the olfactory display is demonstrated. Virtual ice cream shop with scents was made as a content of interactive art. People can enjoy harmony among vision, audition and olfaction. In conclusion, both odor sensing system and olfactory display can contribute to the field of human health care.

  5. Transparent 3D display for augmented reality

    Science.gov (United States)

    Lee, Byoungho; Hong, Jisoo

    2012-11-01

    Two types of transparent three-dimensional display systems applicable for the augmented reality are demonstrated. One of them is a head-mounted-display-type implementation which utilizes the principle of the system adopting the concave floating lens to the virtual mode integral imaging. Such configuration has an advantage in that the threedimensional image can be displayed at sufficiently far distance resolving the accommodation conflict with the real world scene. Incorporating the convex half mirror, which shows a partial transparency, instead of the concave floating lens, makes it possible to implement the transparent three-dimensional display system. The other type is the projection-type implementation, which is more appropriate for the general use than the head-mounted-display-type implementation. Its imaging principle is based on the well-known reflection-type integral imaging. We realize the feature of transparent display by imposing the partial transparency to the array of concave mirror which is used for the screen of reflection-type integral imaging. Two types of configurations, relying on incoherent and coherent light sources, are both possible. For the incoherent configuration, we introduce the concave half mirror array, whereas the coherent one adopts the holographic optical element which replicates the functionality of the lenslet array. Though the projection-type implementation is beneficial than the head-mounted-display in principle, the present status of the technical advance of the spatial light modulator still does not provide the satisfactory visual quality of the displayed three-dimensional image. Hence we expect that the head-mounted-display-type and projection-type implementations will come up in the market in sequence.

  6. Brief history of electronic stereoscopic displays

    Science.gov (United States)

    Lipton, Lenny

    2012-02-01

    A brief history of recent developments in electronic stereoscopic displays is given concentrating on products that have succeeded in the market place and hence have had a significant influence on future implementations. The concentration is on plano-stereoscopic (two-view) technology because it is now the dominant display modality in the marketplace. Stereoscopic displays were created for the motion picture industry a century ago, and this technology influenced the development of products for science and industry, which in turn influenced product development for entertainment.

  7. Adscape: Harvesting and Analyzing Online Display Ads

    OpenAIRE

    Barford, Paul; Canadi, Igor; Krushevskaja, Darja; Ma, Qiang; Muthukrishnan, S.

    2014-01-01

    Over the past decade, advertising has emerged as the primary source of revenue for many web sites and apps. In this paper we report a first-of-its-kind study that seeks to broadly understand the features, mechanisms and dynamics of display advertising on the web - i.e., the Adscape. Our study takes the perspective of users who are the targets of display ads shown on web sites. We develop a scalable crawling capability that enables us to gather the details of display ads including creatives an...

  8. Display depth analyses with the wave aberration for the auto-stereoscopic 3D display

    Science.gov (United States)

    Gao, Xin; Sang, Xinzhu; Yu, Xunbo; Chen, Duo; Chen, Zhidong; Zhang, Wanlu; Yan, Binbin; Yuan, Jinhui; Wang, Kuiru; Yu, Chongxiu; Dou, Wenhua; Xiao, Liquan

    2016-07-01

    Because the aberration severely affects the display performances of the auto-stereoscopic 3D display, the diffraction theory is used to analyze the diffraction field distribution and the display depth through aberration analysis. Based on the proposed method, the display depth of central and marginal reconstructed images is discussed. The experimental results agree with the theoretical analyses. Increasing the viewing distance or decreasing the lens aperture can improve the display depth. Different viewing distances and the LCD with two lens-arrays are used to verify the conclusion.

  9. Study on the visibility of an electroluminescent display for automobiles; Jidoshayo EL display no shininsei

    Energy Technology Data Exchange (ETDEWEB)

    Matsumoto, N.; Harada, M.; Idogaki, T. [Denso Corp., Aichi (Japan)

    1997-10-01

    This report explores the visibility of an Electroluminescent (EL) display for automotive use. Displays for automobiles are exposed to the direct rays of the sun and forced to operate in wide temperature range. Therefore, luminous flux density by the lighting on EL display panel and operating environment temperature must be considered for the visibility evaluation. Sensory evaluation on the visibility and physical measurements such as contrast, chromaticity difference in accordance with the viewing angle change indicate that the visibility of the EL display for automobiles is advantageous over other displays. 6 refs., 11 figs., 1 tab.

  10. High Resolution Autostereoscopic Cockpit Display Project

    Data.gov (United States)

    National Aeronautics and Space Administration — During this Phase II program Dimension Technologies Inc. (DTI) proposes to design and build an autostereoscopic (glasses-free 3D) LCD based aircraft cockpit display...

  11. Predictive displays to improve situation awareness

    NARCIS (Netherlands)

    Breda, L. van

    1999-01-01

    Uit een simulator experiment bleek dat bij het varen met een geïntegreerd navigatie display op basis van de voorspelde manoeuvreer-marges de overschrijding van de minimum veiligheidsafstand tot andere verkeersdeelnemers met een factor vier reduceert

  12. Projection/Reflection Heads-up Display

    Data.gov (United States)

    National Aeronautics and Space Administration — To address the NASA need for an extravehicular activity (EVA) information display device, Physical Optics Corporation (POC) proposes to advance development of a new...

  13. Compressive multi-mode superresolution display

    KAUST Repository

    Heide, Felix

    2014-01-01

    Compressive displays are an emerging technology exploring the co-design of new optical device configurations and compressive computation. Previously, research has shown how to improve the dynamic range of displays and facilitate high-quality light field or glasses-free 3D image synthesis. In this paper, we introduce a new multi-mode compressive display architecture that supports switching between 3D and high dynamic range (HDR) modes as well as a new super-resolution mode. The proposed hardware consists of readily-available components and is driven by a novel splitting algorithm that computes the pixel states from a target high-resolution image. In effect, the display pixels present a compressed representation of the target image that is perceived as a single, high resolution image. © 2014 Optical Society of America.

  14. Three D displays in military applications

    Science.gov (United States)

    Trakalo, M.

    2009-05-01

    The evolution to 3D content is considered to be the next quantum leap in the movie industry, and is currently taking place. The prospect of the home entertainment industry adopting 3D is causing display manufacturers to develop 3D compatible products. In the past, 3D displays have often been limited by poor image quality. The current generation of 3D displays can have image quality that approaches that of their 2D counterparts. 3D content has found its way to the cinema and is seeking a way into the home, but will it have a place in the military environment? This paper discusses the current status of 3D display technology and its suitability to the military ground mobile environment. It includes an introduction to 3D visualization and examines issues such as implementation, image quality, and human factors.

  15. Introduction to tactile displays in military environments

    NARCIS (Netherlands)

    Erp, J.B.F. van; Self, B.P.

    2008-01-01

    Challenging situations, such as those encountered by military pilots, are often a major thrust for ergonomic innovation. Examples include the development of advanced, multimodal, and intuitive interface techniques to counteract the danger of visual, auditory, and cognitive overload. Tactile displays

  16. Night Vision Device and Cockpit Displays

    Data.gov (United States)

    Federal Laboratory Consortium — The Night Vision Device and Cockpit Display labevaluates night vision devices and certifies them for use in the fleet. Lab functions supported include: Analysis of...

  17. Are tiled display walls needed for astronomy?

    CERN Document Server

    Meade, Bernard F; Manos, Steven; Sinnott, Richard O

    2014-01-01

    Clustering commodity displays into a Tiled Display Wall (TDW) provides a cost-effective way to create an extremely high resolution display, capable of approaching the image sizes now gen- erated by modern astronomical instruments. Astronomers face the challenge of inspecting single large images, many similar images simultaneously, and heterogeneous but related content. Many research institutions have constructed TDWs on the basis that they will improve the scientific outcomes of astronomical imagery. We test this concept by presenting sample images to astronomers and non- astronomers using a standard desktop display (SDD) and a TDW. These samples include standard English words, wide field galaxy surveys and nebulae mosaics from the Hubble telescope. These experiments show that TDWs provide a better environment for searching for small targets in large images than SDDs. It also shows that astronomers tend to be better at searching images for targets than non-astronomers, both groups are generally better when em...

  18. Recent progress of flexible AMOLED displays

    Science.gov (United States)

    Pang, Huiqing; Rajan, Kamala; Silvernail, Jeff; Mandlik, Prashant; Ma, Ruiqing; Hack, Mike; Brown, Julie J.; Yoo, Juhn S.; Jung, Sang-Hoon; Kim, Yong-Cheol; Byun, Seung-Chan; Kim, Jong-Moo; Yoon, Soo-Young; Kim, Chang-Dong; Hwang, Yong-Kee; Chung, In-Jae; Fletcher, Mark; Green, Derek; Pangle, Mike; McIntyre, Jim; Smith, Randal D.

    2011-03-01

    Significant progress has been made in recent years in flexible AMOLED displays and numerous prototypes have been demonstrated. Replacing rigid glass with flexible substrates and thin-film encapsulation makes displays thinner, lighter, and non-breakable - all attractive features for portable applications. Flexible AMOLEDs equipped with phosphorescent OLEDs are considered one of the best candidates for low-power, rugged, full-color video applications. Recently, we have demonstrated a portable communication display device, built upon a full-color 4.3-inch HVGA foil display with a resolution of 134 dpi using an all-phosphorescent OLED frontplane. The prototype is shaped into a thin and rugged housing that will fit over a user's wrist, providing situational awareness and enabling the wearer to see real-time video and graphics information.

  19. Recent developments in DFD (depth-fused 3D) display and arc 3D display

    Science.gov (United States)

    Suyama, Shiro; Yamamoto, Hirotsugu

    2015-05-01

    We will report our recent developments in DFD (Depth-fused 3D) display and arc 3D display, both of which have smooth movement parallax. Firstly, fatigueless DFD display, composed of only two layered displays with a gap, has continuous perceived depth by changing luminance ratio between two images. Two new methods, called "Edge-based DFD display" and "Deep DFD display", have been proposed in order to solve two severe problems of viewing angle and perceived depth limitations. Edge-based DFD display, layered by original 2D image and its edge part with a gap, can expand the DFD viewing angle limitation both in 2D and 3D perception. Deep DFD display can enlarge the DFD image depth by modulating spatial frequencies of front and rear images. Secondly, Arc 3D display can provide floating 3D images behind or in front of the display by illuminating many arc-shaped directional scattering sources, for example, arcshaped scratches on a flat board. Curved Arc 3D display, composed of many directional scattering sources on a curved surface, can provide a peculiar 3D image, for example, a floating image in the cylindrical bottle. The new active device has been proposed for switching arc 3D images by using the tips of dual-frequency liquid-crystal prisms as directional scattering sources. Directional scattering can be switched on/off by changing liquid-crystal refractive index, resulting in switching of arc 3D image.

  20. The involvement of Smac/DIABLO, p53, NF-kB and MAPK pathways in apoptosis of keratinocytes from perilesional vitiligo skin: protective effects of curcumin and capsaicin

    OpenAIRE

    Becatti, M; F. Prignano; Fiorillo, C>; L. Pescitelli; P. Nassi; T Lotti; N. TADDEI

    2010-01-01

    Oxidative stress has been suggested as the initial pathogenetic event in melanocyte degeneration in vitiligo. Our previous results indicate that keratinocytes from perilesional skin show the features of damaged cells. In the present study, biopsies were taken from the perilesional skin of 12 patients suffering from nonsegmental vitiligo. The intracellular pathways involved in keratinocyte damage and apoptosis and the antioxidant protection of curcumin and capsaicin in these cells were investi...

  1. Interaction Analysis through Proteomic Phage Display

    OpenAIRE

    Sundell, Gustav N.; Ylva Ivarsson

    2014-01-01

    Phage display is a powerful technique for profiling specificities of peptide binding domains. The method is suited for the identification of high-affinity ligands with inhibitor potential when using highly diverse combinatorial peptide phage libraries. Such experiments further provide consensus motifs for genome-wide scanning of ligands of potential biological relevance. A complementary but considerably less explored approach is to display expression products of genomic DNA, cDNA, open readin...

  2. Beacon data acquisition and display system

    Science.gov (United States)

    Skogmo, David G.; Black, Billy D.

    1991-01-01

    A system for transmitting aircraft beacon information received by a secondary surveillance radar through telephone lines to a remote display includes a digitizer connected to the radar for preparing a serial file of data records containing position and identification information of the beacons detected by each sweep of the radar. This information is transmitted through the telephone lines to a remote computer where it is displayed.

  3. Emotional body language displayed by artificial agents

    OpenAIRE

    Beck A; Stevens B.; Bard K.A.; Canamero L.

    2012-01-01

    Complex and natural social interaction between artificial agents (computer generated or robotic) and humans necessitates the display of rich emotions in order to be believable, socially relevant and accepted, and to generate the natural emotional responses that humans show in the context of social interaction, such as engagement or empathy. Whereas some robots use faces to display (simplified) emotional expressions, for other robots such as Nao, body language is the best medium available give...

  4. Capsaicina tópica en el tratamiento del dolor neuropático Topical capsaicin for the management of neuropathic pain

    Directory of Open Access Journals (Sweden)

    M. A. Vidal

    2004-07-01

    sensación de quemazón en la zona de aplicación, que tiende a desaparecer después de la primera semana. Esta sensación de quemazón constituye, junto con la limitada efectividad clínica, la principal limitación de la aplicación tópica de capsaicina. La principal indicación del uso de la capsaicina tópica es la de coadyuvante de los antidepresivos y anticonvulsivantes en el tratamiento de los diversos cuadros de dolor neuropático, ya que como terapia única parece ser insuficiente. Es una opción a tener en cuenta en los pacientes añosos afectos de dolor neuropático, con lo que disminuiremos la incidencia de efectos secundarios sistémicos y de interacciones medicamentosas.Neuropathic pain is one of the most complex painful syndromes and one of the most difficult to treat. It is a symptom resulting from neurological damage (peripheral, central or both affecting the pain nervous transmission system. Several drugs have been used, but none of them has resulted effective enough and their side effects frequently deter the continuation of the treatment. It can show up in different situations, all of which are more frequent in aged patients. A powerful analgesic with as little number ofside effects as possible is needed. This paper is a bibliographic review performed through the Medline data base of the treatment with topical capsaicin in different cases of neuropathic pain: postherpetic neuralgia, diabetic neuropathy, neuropathic pain associated to AIDS, trigeminal neuralgia, post-mastectomy painful syndromes and regional complex pain. The topical administration of capsaicin 0.075%, has shown to be effective for the management of dysesthesic pain and hence it is a therapeutic alternative for this type of pain. Its mechanism of action appears to be based on the selective stimulation of the neurons of amyelinic fibers C, causing the release of substance P and perhaps of other neurotransmitters; and finally, a depletion of substance P, which would disturb pain

  5. Oil defect detection of electrowetting display

    Science.gov (United States)

    Chiang, Hou-Chi; Tsai, Yu-Hsiang; Yan, Yung-Jhe; Huang, Ting-Wei; Mang, Ou-Yang

    2015-08-01

    In recent years, transparent display is an emerging topic in display technologies. Apply in many fields just like mobile device, shopping or advertising window, and etc. Electrowetting Display (EWD) is one kind of potential transparent display technology advantages of high transmittance, fast response time, high contrast and rich color with pigment based oil system. In mass production process of Electrowetting Display, oil defects should be found by Automated Optical Inspection (AOI) detection system. It is useful in determination of panel defects for quality control. According to the research of our group, we proposed a mechanism of AOI detection system detecting the different kinds of oil defects. This mechanism can detect different kinds of oil defect caused by oil overflow or material deteriorated after oil coating or driving. We had experiment our mechanism with a 6-inch Electrowetting Display panel from ITRI, using an Epson V750 scanner with 1200 dpi resolution. Two AOI algorithms were developed, which were high speed method and high precision method. In high precision method, oil jumping or non-recovered can be detected successfully. This mechanism of AOI detection system can be used to evaluate the oil uniformity in EWD panel process. In the future, our AOI detection system can be used in quality control of panel manufacturing for mass production.

  6. SES cupola interactive display design environment

    Science.gov (United States)

    Vu, Bang Q.; Kirkhoff, Kevin R.

    1989-01-01

    The Systems Engineering Simulator, located at the Lyndon B. Johnson Space Center in Houston, Texas, is tasked with providing a real-time simulator for developing displays and controls targeted for the Space Station Freedom. These displays and controls will exist inside an enclosed workstation located on the space station. The simulation is currently providing the engineering analysis environment for NASA and contractor personnel to design, prototype, and test alternatives for graphical presentation of data to an astronaut while he performs specified tasks. A highly desirable aspect of this environment is to have the capability to rapidly develop and bring on-line a number of different displays for use in determining the best utilization of graphics techniques in achieving maximum efficiency of the test subject fulfilling his task. The Systems Engineering Simulator now has available a tool which assists in the rapid development of displays for these graphic workstations. The Display Builder was developed in-house to provide an environment which allows easy construction and modification of displays within minutes of receiving requirements for specific tests.

  7. RPF101, a new capsaicin-like analogue, disrupts the microtubule network accompanied by arrest in the G2/M phase, inducing apoptosis and mitotic catastrophe in the MCF-7 breast cancer cells

    Energy Technology Data Exchange (ETDEWEB)

    Sá-Júnior, Paulo Luiz de [Laboratory of Genetics, Butantan Institute, Vital Brasil Avenue 1500, Postal Code: 05503-900, Sao Paulo (Brazil); Pasqualoto, Kerly Fernanda Mesquita [Biochemistry and Biophysical Laboratory, Butantan Institute, Vital Brasil Avenue 1500, Postal Code: 05503-900, Sao Paulo (Brazil); Ferreira, Adilson Kleber [Laboratory of Genetics, Butantan Institute, Vital Brasil Avenue 1500, Postal Code: 05503-900, Sao Paulo (Brazil); Tavares, Maurício Temotheo; Damião, Mariana Celestina Frojuello Costa Bernstorff [Department of Pharmacy, School of Pharmaceutical Sciences, University of Sao Paulo, Prof. Lineu Prestes Avenue, 580, Postal Code: 05508-000, Sao Paulo (Brazil); Azevedo, Ricardo Alexandre de [Biochemistry and Biophysical Laboratory, Butantan Institute, Vital Brasil Avenue 1500, Postal Code: 05503-900, Sao Paulo (Brazil); Câmara, Diana Aparecida Dias; Pereira, Alexandre; Madeiro de Souza, Dener [Laboratory of Genetics, Butantan Institute, Vital Brasil Avenue 1500, Postal Code: 05503-900, Sao Paulo (Brazil); Parise Filho, Roberto, E-mail: roberto.parise@usp.br [Department of Pharmacy, School of Pharmaceutical Sciences, University of Sao Paulo, Prof. Lineu Prestes Avenue, 580, Postal Code: 05508-000, Sao Paulo (Brazil)

    2013-02-01

    Breast cancer is the world's leading cause of death among women. This situation imposes an urgent development of more selective and less toxic agents. The use of natural molecular fingerprints as sources for new bioactive chemical entities has proven to be a quite promising and efficient method. Capsaicin, which is the primary pungent compound in red peppers, was reported to selectively inhibit the growth of a variety tumor cell lines. Here, we report for the first time a novel synthetic capsaicin-like analogue, RPF101, which presents a high antitumor activity on MCF-7 cell line, inducing arrest of the cell cycle at the G2/M phase through a disruption of the microtubule network. Furthermore, it causes cellular morphologic changes characteristic of apoptosis and a decrease of Δψm. Molecular modeling studies corroborated the biological findings and suggested that RPF101, besides being a more reactive molecule towards its target, may also present a better pharmacokinetic profile than capsaicin. All these findings support the fact that RPF101 is a promising anticancer agent. -- Highlights: ► We report for the first time that RPF101 possesses anticancer properties. ► RPF101 induces apoptosis of human breast cancer cells. ► RPF 101 decreases mitochondrial potential and induces DNA fragmentation.

  8. Tolerability of NGX-4010, a capsaicin 8% patch, in conjunction with three topical anesthetic formulations for the treatment of neuropathic pain

    Directory of Open Access Journals (Sweden)

    Webster LR

    2012-01-01

    Full Text Available Lynn R Webster1, John F Peppin2, Frederick T Murphy3,4, Jeffrey K Tobias5, Geertrui F Vanhove51Lifetree Clinical Research and Pain Clinic, Lifetree Medical Inc, Salt Lake City, UT, USA; 2Clinical Research Division, The Pain Treatment Center of the Bluegrass, Lexington, KY, USA; 3Altoona Center for Clinical Research, Duncansville, PA, USA; 4University of Pennsylvania, School of Medicine, Philadelphia, PA, USA; 5NeurogesX Inc, San Mateo, CA, USABackground: The objective of this study was to assess the safety, tolerability, and preliminary efficacy of NGX-4010, a capsaicin 8% patch, following pretreatment with three different topical anesthetics in patients with peripheral neuropathic pain.Methods: This open-label, multicenter study enrolled 117 patients with post-herpetic neuralgia, HIV-associated distal sensory polyneuropathy, or painful diabetic neuropathy. Patients received pretreatment with one of three lidocaine 4%-based topical anesthetics (L.M.X.4® [Ferndale Laboratories Inc, Ferndale, MI], Topicaine® Gel [Estela Basso, Jupiter, FL], or Betacaine Enhanced Gel 4 [Tiberius Inc, Tampa, FL] for 60 minutes followed by a single 60- or 90-minute NGX-4010 application, and were followed for 12 weeks. Tolerability and safety measures included “pain now” Numeric Pain Rating Scale (NPRS scores, dermal assessments, medication use for treatment-related pain, adverse events (AEs, clinical laboratory parameters, physical examinations, and vital signs. The primary efficacy variable was the percentage change in mean NPRS scores for “average pain for the past 24 hours” from baseline to weeks 2 through 12.Results: Treatment with NGX-4010 following pretreatment with any of the three topical anesthetics was generally safe and well tolerated. Nearly all patients completed ≥90% of the planned NGX-4010 application duration. The most common treatment-related AEs, application-site burning and application-site pain, were transient, mostly mild or moderate

  9. Micro-needle electro-tactile display.

    Science.gov (United States)

    Tezuka, Mayuko; Kitamura, Norihide; Miki, Norihisa

    2015-08-01

    Haptic feedback is strongly demanded for high-precision robot-assisted surgery and teleoperation. The haptic feedback consists of force and tactile feedback, however tactile feedback has been little studied and the size and weight of the system poses challenges for practical applications. In this paper we propose a sheet-type wearable electro-tactile display which provides tactile sensations to the user as the feedback at a low voltage and power consumption. The display possesses needle-shaped electrodes, which can penetrate through the high-impedance stratum corneum. We developed the fabrication process and, as the first step, we investigated the tactile sensation that can be created to the fingertip by the display. Rough and smooth surfaces were successfully presented to the user. Then, we characterized the tactile display when used on the forearm, in particular, with respect to the spatial resolution. These tactile displays can be used to inform the user of the surface property of the parts of interest, such as tumor tissues, and to guide him in the manipulation of surgery robots. PMID:26737606

  10. Holographic display with tilted spatial light modulator.

    Science.gov (United States)

    Kozacki, Tomasz

    2011-07-10

    In this paper, we analyze a holographic display system utilizing a phase-only spatial light modulator (SLM) based on liquid crystal on silicon (LCoS). An LCoS SLM works in reflection, and, in some applications, it is convenient to use with an inclined illumination. Even with a highly inclined illumination, the holographic display is capable of good-quality image generation. We show that the key to obtain high-quality reconstructions is the tilt-dependent calibration and algorithms. Typically, an LCoS SLM is illuminated with a plane wave with normal wave vector. We use inclined illumination, which requires development of new algorithms and display characterization. In this paper we introduce two algorithms. The first one is designed to process a digital hologram captured in CCD normal configuration, so it can be displayed in SLM tilted geometry, while the second one is capable of synthetic hologram generation for tilted SLM configuration. The inclined geometry asymmetrically changes the field of view of a holographic display. The presented theoretical analysis of the aliasing effect provides a formula for the field of view as a function of SLM tilt. The incidence angle affects SLM performance. Both elements of SLM calibration, i.e., pixel phase response and wavefront aberrations, strongly depend on SLM tilt angle. The effect is discussed in this paper. All of the discussions are accompanied with experimental results. PMID:21743569

  11. Studies on the synthesis, pungency and anti-biofouling performance of capsaicin analogues%辣椒素同系物合成、辣度及海洋生物防污性能研究

    Institute of Scientific and Technical Information of China (English)

    彭必先; 张孝彬; 王俊莲; 彭争宏; 周圣泽; 王凤奇; 纪永亮; 叶章基; 周祥凤; 林童

    2011-01-01

    Ten capsaicin analogues were synthesized and their pungency degrees were determined through Scoville Organleptic Test. The relationship between the structure and pungency of these capsaicin analogues was discussed. Then four of these ten capsaicin analogues which are relatively more pungent were used as repellent in anti- biofouling paints to study their anti-biofouling performance by shallow sea buoyant raft hung-plate experimentation. The results showed that capsaicin and dihydrocapsaicin exhibited equally good anti-biofouling performance while nordihydrocapsaicin and Iv-vanillylnonanamide were apparently different in the performance. Experomenral results also showed that the paints with only 0.1% capsaicin or dihydrocapsaicin as repellent without any other biocides have already exhibited good anti-biofouling performance, which provided a new idea for developing novel, environment-friendly and Cu2O-free antifouling paints.%合成了十种辣椒碱同系物,用感官评定的方法对其辣度进行了测定,并将它们的结构与辣度进行了对比,探讨了影响辣椒碱同系物辣度的结构因子.选取其中辣度较大的四种辣椒碱同系物作为海洋生物防污涂料的驱赶剂,考察了它们的海洋生物防污性能.结果表明,辣椒碱和二氢辣椒碱都具有良好的防污性能,二者不相上下.降二氢辣椒碱和壬酸香草胺的防污性能与辣椒碱和二氢辣椒碱有明显区别.仅以辣椒碱或二氢辣椒碱为驱赶剂,且其含量仅为0.1%的情况下,漆膜也表现出较好的防污性能,这为研发新型的、环保的、不合氧化亚铜的防污涂料提供了新思路.

  12. Braille display device using soft actuator

    Science.gov (United States)

    Lee, Sangwon; Jung, Kwangmok; Koo, Jachoon; Lee, Sungil; Choi, Hoogon; Jeon, Jaewook; Nam, Jaedo; Choi, Hyoukryeol

    2004-07-01

    Tactile sensation is one of the most important sensory functions along with the auditory sensation for the visually impaired because it replaces the visual sensation of the persons with sight. In this paper, we present a tactile display device as a dynamic Braille display that is the unique tool for exchanging information among them. The proposed tactile cell of the Braille display is based on the dielectric elastomer and it has advantageous features over the existing ones with respect to intrinsic softness, ease of fabrication, cost effectiveness and miniaturization. We introduce a new idea for actuation and describe the actuating mechanism of the Braille pin in details capable of realizing the enhanced spatial density of the tactile cells. Finally, results of psychophysical experiments are given and its effectiveness is confirmed.

  13. Polarity effect in electrovibration for tactile display.

    Science.gov (United States)

    Kaczmarek, Kurt A; Nammi, Krishnakant; Agarwal, Abhishek K; Tyler, Mitchell E; Haase, Steven J; Beebe, David J

    2006-10-01

    Electrovibration is the tactile sensation of an alternating potential between the human body and a smooth conducing surface when the skin slides over the surface and where the current is too small to stimulate sensory nerves directly. It has been proposed as a high-density tactile display method, for example to display pictographic information to persons who are blind. Previous models for the electrovibration transduction mechanism are based on a parallel-plate capacitor in which the electrostatic force is insensitive to polarity. We present experimental data showing that electrovibratory perceptual sensitivity to positive pulses is less than that for negative or biphasic pulses and propose that this disparity may be due to the asymmetric electrical properties of human skin. We furthermore propose using negative pulses for insulated tactile displays based on electrovibration because their sensory thresholds were found to be more stable than for waveforms incorporating positive pulses.

  14. Large color gamut displays with diffraction gratings.

    Science.gov (United States)

    Aieta, Francesco; Morovič, Peter; Morovič, Ján; Fiorentino, Marco; Santori, Charles; Fattal, David

    2016-06-01

    The ability to display a broad variety of colors has great benefits not only in the context of entertainment but also as a means to streamline design in prototyping and manufacturing processes. Displays that use RGB filters or backlights cannot span all colors that occur in nature. To improve the accuracy of color reproduction, there have been attempts to include additional color primaries in displays. Existing solutions, however, have an impact on cost, scalability, and spatial resolution and are predominantly applicable to projection systems. We propose an approach based on combining diffraction grating extractors and the HANS imaging pipeline initially developed for printing. This combination offers unprecedented potential to attain large color gamuts with the same backlights commercially used today. PMID:27409441

  15. High performance visual display for HENP detectors

    CERN Document Server

    McGuigan, M; Spiletic, J; Fine, V; Nevski, P

    2001-01-01

    A high end visual display for High Energy Nuclear Physics (HENP) detectors is necessary because of the sheer size and complexity of the detector. For BNL this display will be of special interest because of STAR and ATLAS. To load, rotate, query, and debug simulation code with a modern detector simply takes too long even on a powerful work station. To visualize the HENP detectors with maximal performance we have developed software with the following characteristics. We develop a visual display of HENP detectors on BNL multiprocessor visualization server at multiple level of detail. We work with general and generic detector framework consistent with ROOT, GAUDI etc, to avoid conflicting with the many graphic development groups associated with specific detectors like STAR and ATLAS. We develop advanced OpenGL features such as transparency and polarized stereoscopy. We enable collaborative viewing of detector and events by directly running the analysis in BNL stereoscopic theatre. We construct enhanced interactiv...

  16. 辣椒素对微波辐射所致小鼠血液系统损伤的保护作用%Protective Effects of Capsaicin on Blood System Injured by Microwave Radiation in Mice

    Institute of Scientific and Technical Information of China (English)

    王瀚; 余智操; 魏卫; 李渊; 陈杨; 贾易臻; 梁向艳; 于军

    2012-01-01

    Objective To study the protective effects of capsaicin on the mice' s hematopoietic system injuries induced by microwave radiation.Methods Mice were randomly divided into control,radiation and capsaicin groups.The radiation group was exposed to 2450 MHz and 65 mW/cm2 microwave radiation 8 h per day for 3 consecutive days.The capsaicin group was treated with the same microwave radiation exposure as that of the radiation group,in addition 0.2 mL of 2.5 g/L capsaicin were poured into the stomach of mice twice a day.The count of red blood cells (RBCs),polychromatic erythrocyte micronucleus rate,serum superoxide dis-mutase (SOD) and erythropoietin (EPO) of each mouse were analyzed.Results The micronucleus rates increased and SOD and EPO decreased in the modeling group.While,in the capsaicin group,the micronucleus rates decreased to normal,EPO and counting of RBC increased obviously and SOD recovered to normal.Conclusion Capsaicin has a protective effect on the mouse' s blood system injuries caused by microwave radiation.The mechanism may be related to the capsaicin's antioxidalion function and the promotion of EPO secretion.%目的 研究辣椒素对微波辐射所致小鼠血液系统损伤的保护作用.方法 将小鼠随机分为3组:对照组;辐射组,用频率为2450 MHz、功率密度为65 mW/cm2的微波辐射,连续3d,每天8h;辣椒素组,在与辐射组相同的辐射下每天2次辣椒素灌胃,浓度为2.5 g/L,体积为0.2 mL.检测小鼠的红细胞(RBC)计数、嗜多染红细胞微核率、血清超氧化物歧化酶(SOD)与促红细胞生成素(EPO).结果 辐射组微核率升高,SOD,EPO降低,辣椒素组微核率下降至正常,EPO明显上升,RBC计数也明显上升,同时SOD也回升至正常.结论 辣椒素对微波所致小鼠血液系统损伤有保护作用,其机制可能与辣椒素的抗氧化作用和促进EPO分泌有关.

  17. Electromagnetic interference considerations for cockpit AMLCD displays

    Science.gov (United States)

    Case, Gary D.; Prache, Olivier

    1994-06-01

    OIS has developed various active matrix liquid crystal displays for the cockpits of several aircraft. Some of these displays have been tested for and are being designed for compliance with the military electromagnetic interference (EMI) requirements spelled out in MIL-STD- 461. Detailed analysis has also been performed on the addressed cell assembly and the flex circuitry to provide guidelines for EMI design. This paper presents the results of tests performed, steps which were taken to become EMI compliant and the results of the analysis.

  18. Displaying of Details in Subvoxel Accuracy

    Institute of Scientific and Technical Information of China (English)

    蔡文立; 陈天洲; 等

    1996-01-01

    Under the volume segmentation in voxel space,a lot of details,some fine and thin objects,are ignored.In order to accurately display these details,this paper has developed a methodology for volume segmentation in subvoxel space.In the subvoxel space,most of the “bridges”between adjacent layers are broken down.Based on the subvoxel space,an automatic segmentation algorithm reserving details is discussed.After segmentation,volume data in subvoxel space are reduced to original voxel space.Thus,the details with width of only one or several voxels are extracted and displayed.

  19. Variable parallax barrier spacing in autostereoscopic displays

    Science.gov (United States)

    Yoon, Seon Kyu; Khym, Sungwon; Kim, Hyun-Woo; Kim, Sung-Kyu

    2016-07-01

    In general, multi-view autostereoscopic displays can only provide autostereoscopic images with little crosstalk at the optimum viewing distance (OVD) in the depth direction, limiting the mobility of viewers. Therefore, this paper proposes a method of increasing viewer mobility in the depth direction by varying the distance separating the parallax barrier and the display. Computer simulations and experiments were conducted to verify changes in the OVD resulting from the application of the proposed method. The results showed that the proposed method is effective at changing the OVD with respect to changes in the viewing distance. Therefore this method minimizes changes in the 3D image quality due to the viewer's depth location.

  20. Next-generation head-mounted display

    Science.gov (United States)

    McGuire, James P., Jr.

    2010-02-01

    Head Mounted Displays (HMDs) have been utilized by the military for various applications since the 1980's. In the 1990's, this technology migrated to the consumer market. Most of these early systems suffered the major drawback that they were "look-at" versus "see through" systems, which prevented the user from seeing their environment. This reduced the utility of the devices and could potentially lead to safety issues. This presentation discusses the optical design of a novel see-through High Definition display device with a 40 degree field of view.