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Sample records for cytotoxic nc activity

  1. Cytotoxicity of activated monocytes on endothelial cells.

    Science.gov (United States)

    Peri, G; Chiaffarino, F; Bernasconi, S; Padura, I M; Mantovani, A

    1990-02-15

    Unstimulated human monocytes did not express appreciable levels of cytotoxicity on normal human umbilical vein endothelial cells (EC) in a 24-48 hr TdR release assay. On activation with IFN-gamma and LPS, monocytes had appreciable cytotoxicity on EC. Monocyte cytotoxicity on EC was not dependent on the presence of contaminating lymphoid cells. Recombinant TNF, IL-1, and IL-6 as well as monocyte supernatants did not exert a cytotoxic effect on EC. Moreover, anti-TNF, anti-IL-1, and anti-IL-6 antibodies, as well as scavengers of reactive oxygen intermediates, did not affect the cytotoxicity of activated monocytes on EC. Antibodies against the beta-chain (CD18) of leukocyte integrins inhibited the adhesion and cytotoxicity of activated monocytes on EC. Pretreatment of EC with IL-1 augmented the adhesion of monocytes on EC. Normal monocytes were not cytotoxic on IL-1-pretreated EC and IL-1 treatment did not increase the susceptibility of EC to activated monocytes. Thus adhesion is necessary but not sufficient for monocyte killing of EC. Anti-alpha L (LFA-1) antibodies markedly reduced monocyte cytotoxicity on EC, although anti-alpha X (p150) antibodies had only a modest effect. Anti-alpha M (Mac-1/CR3) antibodies were intermediate inhibitors of EC killing by activated monocytes. Thus, alpha L, beta 2 (LFA-1), and, to a lesser extent, alpha M, beta 2 (Mac-1/CR3) and alpha X, beta 2 (p 150, 95) integrins are the main adhesive structures involved in the cytotoxic interaction of activated monocytes with EC. Monocyte-mediated damage of EC could play a role as a mechanism of tissue injury under conditions of local or systemic activation of mononuclear phagocytes.

  2. Cytotoxic Activities of Phytochemicals from Ferula Species

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    Seied Mojtaba Valiahdi

    2013-05-01

    Full Text Available Background:Ferula species are reputed in folk medicine for the treatment of a variety of disorders. There have been sporadic reports on the chemopreventive and chemosensitizing activities of some terpenoid coumarin derivatives from the genus Ferula. The present study investigated the cytotoxic activity of 11 phytochemicals (conferone, farnesiferol A, acantrifoside E, mogoltadone, diversin, galbanic acid, herniarin, 7-isopentenyloxycoumarin, umbelliprenin, stylosin and tschimgine from Ferula species together with a newly synthesized prenylated derivative of curcumin (gercumin II.Methods:Cytotoxic activity of phytochemicals was evaluated against ovarian carcinoma (CH1, lung cancer (A549 and melanoma (SK-MEL-28 cell lines using MTT assay.Results and conclusion:Overall, moderate cytotoxic activity was observed from the tested compounds with IC50 values in the micromolar range. The highest activity against CH1 and A549 lines was from conferone while stylosin and tschimgine were the most potent compounds against SK-MEL-28 line. In conclusion, the findings of the present investigation did not support a potent cytotoxic activity of the tested phytochemicals against CH1, A549 and SK-MEL-28 cell lines. With respect to previous reports, the beneficial impact of these phytochemicals in cancer therapy may be more attributable to their chemopreventive or chemosensitizing activity rather than direct cytotoxic effects.

  3. Antimycobacterial, Antioxidant and Cytotoxic activities of Essential ...

    African Journals Online (AJOL)

    SIFI IBRAHIM

    Background: The aim of this study was to assess the antimycobacterial, antioxidant and the cytotoxic activities of the essential oil from the gall part of Pistacia atlantica Desf from Algeria. Materials and Methods: The antimycobacterial activity was evaluated by the broth microdilution method against three species of ...

  4. Cytotoxic activity of four Mexican medicinal plants.

    Science.gov (United States)

    Vega-Avila, Elisa; Espejo-Serna, Adolfo; Alarcón-Aguilar, Francisco; Velasco-Lezama, Rodolfo

    2009-01-01

    Ibervillea sonorae Greene, Cucurbita ficifolia Bouché, Tagetes lucida Cav and Justicia spicigera Scheltdd are Mexican native plants used in the treatment of different illnesses. The ethanolic extract of J. spicigera and T. lucida as well as aqueous extracts from I. sonorae, C. ficifolia, T. lucida and J. spicigera were investigated using sulforhodamine B assay. These extracts were assessed using two cell line: T47D (Human Breast cancer) and HeLa (Human cervix cancer). Colchicine was used as the positive control. Data are presented as the dose that inhibited 50% control growth (ED50). All of the assessed extracts were cytotoxic (ED50 < 20 microg/ml) against T47D cell line, meanwhile only the aqueous extract from T. lucida and the ethanolic extract from J. spicigera were cytotoxic to HeLa cell line. Ethanolic extract from J. spicigera presented the best cytotoxic effect. The cytotoxic activity of J. spicigera correlated with one of the popular uses, the treatment of cancer.

  5. Cytotoxic activity of lignans from Justicia procumbens.

    Science.gov (United States)

    Jin, Hong; Yin, Hai-Long; Liu, Shi-Jun; Chen, Li; Tian, Ying; Li, Bin; Wang, Qiong; Dong, Jun-Xing

    2014-04-01

    Three new lignans, Pronaphthalide A (1), Procumbiene (2), and Procumbenoside J (3), along with a novel natural product Juspurpudin (4), and twelve other known lignans were isolated from Justicia procumbens. The structures of the new compounds were elucidated by extensive spectroscopic analyses and the data of 3 provided insight into the conformational equilibria existing in it. All compounds were evaluated for their in vitro cytotoxic activity against Human LoVo and BGC-823 cell lines except for compound 2, and eight of them were found to possess potent cytotoxicity. The structure-activity relationship (SAR) analysis revealed that (i) the parent structure of 2-carbonyl arylnaphthalide lactone attached with 6 and 7-OMe was the essential element; (ii) the polarity of substituents on C-4 might significantly affect the activity; (iii) a proper cyclic lipophilic group at the C-3″ and C-5″ of apiofuranose on C-4 might enhance the activity, which could optimize the application of 3 similar to VP-16. Copyright © 2014 Elsevier B.V. All rights reserved.

  6. Cytotoxicity of furoxans: quantitative structure-activity relationships study.

    Science.gov (United States)

    Boiani, Mariana; Cerecetto, Hugo; González, Mercedes

    2004-05-01

    Furoxans are interesting biological active compounds. Recent studies demonstrate that they are cytotoxic under aerobic conditions. This paper shows that this cytotoxicity could be related with E(LUMO), calculated LogP and Mulliken charge on heterocycle nitrogen 2 calculated at ab initio level (3-21G* basis). It was possible to propose a tentative mechanism of cytotoxicity and structural modifications to modulate the cytotoxic potency of furoxan derivatives. Copyright 2004 Elsevier SAS

  7. Antileishmanial activity and cytotoxicity of Brazilian plants.

    Science.gov (United States)

    Ribeiro, Tatiana G; Chávez-Fumagalli, Miguel A; Valadares, Diogo G; Franca, Juçara R; Lage, Paula S; Duarte, Mariana C; Andrade, Pedro H R; Martins, Vivian T; Costa, Lourena E; Arruda, Ana L A; Faraco, André A G; Coelho, Eduardo A F; Castilho, Rachel O

    2014-08-01

    Leishmaniasis is a major public health problem, and the alarming spread of parasite resistance has increased the importance of discovering new therapeutic products. The present study aimed to investigate the in vitro leishmanicidal activity from 16 different Brazilian medicinal plants. Stationary-phase promastigotes of Leishmania amazonensis and murine macrophages were exposed to 44 plant extracts or fractions for 48 h at 37°C, in order to evaluate their antileishmanial activity and cytotoxicity, respectively. The most potent extracts against L. amazonensis were the hexanic extract of Dipteryx alata (IC50 of 0.08 μg/mL), the hexanic extract of Syzygium cumini (IC50 of 31.64 μg/mL), the ethanolic and hexanic extracts of leaves of Hymenaea courbaril (IC50 of 44.10 μg/mL and 35.84 μg/mL, respectively), the ethanolic extract of H. stignocarpa (IC50 of 4.69 μg/mL), the ethanolic extract of Jacaranda caroba (IC50 of 13.22 μg/mL), and the ethanolic extract of J. cuspidifolia leaves (IC50 of 10.96 μg/mL). Extracts of D. alata and J. cuspidifolia presented higher selectivity index, with high leishmanicidal activity and low cytotoxicity in the mammalian cells. The capacity in treated infected macrophages using the extracts and/or fractions of D. alata and J. cuspidifolia was also analyzed, and reductions of 95.80%, 98.31%, and 97.16%, respectively, in the parasite burden, were observed. No nitric oxide (NO) production could be observed in the treated macrophages, after stimulation with the extracts and/or fractions of D. alata and J. cuspidifolia, suggesting that the biological activity could be due to mechanisms other than macrophage activation mediated by NO production. Based on phytochemistry studies, the classes of compounds that could contribute to the observed activities are also discussed. In conclusion, the data presented in this study indicated that traditional medicinal plant extracts present effective antileishmanial activity. Future studies could focus on

  8. Cytotoxic, anti-inflammatory and antioxidant activities of four different ...

    African Journals Online (AJOL)

    Purpose: To evaluate the cytotoxic, anti-inflammatory and antioxidant activities of four different solvent extracts obtained from the aerial parts of Galega officinalis L. Methods: The hexane, DCM, methanol and water extracts of G. officinalis were successively obtained by soxhlet extraction method. The cytotoxic activity of the ...

  9. Antibacterial and Cytotoxic Activities of Acacia nilotica Lam ...

    African Journals Online (AJOL)

    The bactericidal activity was heat-resistant and showed minimal cytotoxic effects on human brain microvascular endothelial cells. FPLC revealed eight peaks, with three of them representing compounds that had maximum bactericidal activity against all the tested isolates, but showed < 30 % host cell cytotoxicity. Conclusion: ...

  10. Cytotoxic activity of Agave lechuguilla Torr | Casillas | African ...

    African Journals Online (AJOL)

    The cytotoxic activity of extract and isolated saponin from leaves of Agave lechuguilla was investigated. Ethanol extract from leaves of A. lechuguilla exhibited cytotoxic activity against HeLa cells in vitro (50% inhibitory concentration (IC50) = 89 μg/ml). Bioassay-guided fractionation of this extract had led to the isolation of 5-β ...

  11. Cytotoxic Activity of Croton gibsonianus Nimm. Grah | Prashith ...

    African Journals Online (AJOL)

    The present study was designed to investigate the cytotoxic activity of methanol extract of Croton gibsonianus Nimm. Grah (Euphorbiaceae) leaves by brine shrimp lethality bioassay. The powdered leaf material was extracted with methanol. The cytotoxicity activity of methanol extract was tested using brine shrimp (Artemia ...

  12. Pharmacognostic profile and in vitro cytotoxic activity of Adenema ...

    African Journals Online (AJOL)

    Chloroform, ethyl acetate and ethanolic extracts were investigated for in vitro cytotoxic activity against nine different types of human cancer panel of 60 different strains of tumor cell lines using the sulforhodamine-B (SRB) binding assay. The chloroform extract showed potent cytotoxicity against non small cell lung cancer cell, ...

  13. Antimycobacterial and cytotoxic activities of extracts from fungal ...

    African Journals Online (AJOL)

    In this study, antimycobacterial and cytotoxic activities of ethyl acetate extracts of fungal isolates from Lake Magadi were evaluated. The extracts were tested against Mycobacterium madagascariense (MM) and M. indicus pranii (MIP), and cytotoxicity against brine shrimp (Artemia salina) larvae. Fungal strains were identified ...

  14. Cytotoxic activity of selected Nigerian plants | Sowemimo | African ...

    African Journals Online (AJOL)

    Cytotoxic activity of selected Nigerian plants. ... Abstract. Cancer is one of the most prominent human diseases which has stimulated scientific and commercial interest in the discovery of new anticancer agents from natural sources. The current study ... Keywords: Medicinal plants; Cytotoxicity; Cancer; Sapium; Combretum ...

  15. Cytotoxic and Antioxidant Activities of Antidesma thwaitesianum Müll ...

    African Journals Online (AJOL)

    Purpose: To investigate the cytotoxic and antioxidant activities of the fruit and fruit waste (residue and marc) extracts of Antidesma thwaitesianum Müll. Arg., known as mamao in Thai, using chemical and cell-based assays. Methods: The cytotoxicity of mamao fruit and fruit waste extracts obtained by expression, maceration ...

  16. Interleukin-2 activation of cytotoxic cells in postmastectomy seroma.

    Science.gov (United States)

    Gercel-Taylor, C; Hoffman, J P; Taylor, D D; Owens, K J; Eisenberg, B L

    1996-02-15

    Lymphocytes were isolated from breast seroma fluids and used to study the mechanism of activation of cytotoxic lymphocytes and possible role of immunological potentiation following surgery in breast cancer patients. Single or serial samples were obtained from patients who had undergone mastectomy or lumpectomy with axillary node dissection. Lymphocytes were activated with rIL-2 (interleukin-2) and their cytotoxic activity was studied against Daudi and K562 cells and against a breast tumor line (SKBr-3). All of the patients (21/21) responded to IL-2 stimulation by significant activation of cytotoxic activity. The unstimulated cytotoxic activity of these cells against NK targets was low with less than 10% specific release in cytotoxicity assays. In simultaneous experiments, autologous seroma fluid was included during activation of lymphocytes to study possible regulatory molecules that may be present. In 17/21 patients, the presence of their seroma fluid, during the activation period, enhanced or did not effect the cytotoxic potential of their lymphocytes; inhibition was observed when seroma fluids from 4/21 patients were included. Analysis of the cytotoxic population derived from combined IL-2 and seroma treatments indicates the presence of cells with increased expression of CD56, and CD2, as well as in some cases CD16 expression. Cytotoxic lymphocytes derived from IL-2 and seroma treatments appeared to be more effective killers. Modulation of CD2 expression with seroma alone appeared to result in the generation of this highly cytotoxic population. This study demonstrates the role of CD2 expression in the effectiveness of LAK cell killing and also potential benefit of an immunotherapeutic approach to the postoperative treatment of carcinoma of the breast.

  17. Randomized anticancer and cytotoxicity activities of Guibourtia ...

    African Journals Online (AJOL)

    African Journal of Traditional, Complementary and Alternative Medicines ... In light of this, there is a constant demand for new treatment regimens for cancer. ... Anticancer screening was performed on a panel of three cancer cell lines, while cytotoxicity was determined using a human fibroblast cell line, both using the SRB ...

  18. In vitro antifungal and cytotoxicity activities of selected Tanzanian ...

    African Journals Online (AJOL)

    Purpose: To evaluate the antifungal and cytotoxic activities of four medicinal plants from Tanzania, namely, Mystroxylon aethiopicum, Lonchocarpus capassa, Albizia anthelmentica and Myrica salicifolia. Methods: The plant materials were subjected to extraction using dichloromethane, ethyl acetate and distilled water.

  19. Effect of cerebral hemisphere decortication on the cytotoxic activity of natural killer and natural cytotoxic lymphocytes in the mouse.

    Science.gov (United States)

    Belluardo, N; Mudò, G; Cella, S; Bindoni, M

    1990-08-06

    A comparison was made of the effects of left and right cerebral decortication on cytotoxic activity of natural killer and natural cytotoxic lymphocytes in the mouse. Natural killer cytotoxic activity was significantly reduced after right decortication, whereas left decortication led to a less pronounced, though still significant fall. The cytotoxic activity of natural cytotoxic cells, on the other hand, was significantly increased, particularly 15 days after left decortication. These findings mirror the results of previously published personal findings following electrothermocoagulation of the hypothalamus. The suggestion is made that the cortex and the hypothalamus form an integrated system for the control of certain aspects of natural immunity.

  20. Role of the NC-loop in catalytic activity and stability in lipase from Fervidobacterium changbaicum.

    Directory of Open Access Journals (Sweden)

    Binchun Li

    Full Text Available Flexible NC-loops between the catalytic domain and the cap domain of the α/β hydrolase fold enzymes show remarkable diversity in length, sequence, and configuration. Recent investigations have suggested that the NC-loop might be involved in catalysis and substrate recognition in many enzymes from the α/β hydrolase fold superfamily. To foster a deep understanding of its role in catalysis, stability, and divergent evolution, we here systemically investigated the function of the NC-loop (residues 131-151 in a lipase (FClip1 from thermophilic bacterium Fervidobacterium changbaicum by loop deletion, alanine-scanning mutagenesis and site-directed mutagenesis. We found that the upper part of the NC-loop (residues 131-138 was of great importance to enzyme catalysis. Single substitutions in this region could fine-tune the activity of FClip1 as much as 41-fold, and any deletions from this region rendered the enzyme completely inactive. The lower part of the NC-loop (residues 139-151 was capable of enduring extensive deletions without loss of activity. The shortened mutants in this region were found to show both improved activity and increased stability simultaneously. We therefore speculated that the NC-loop, especially the lower part, would be a perfect target for enzyme engineering to optimize the enzymatic properties, and might present a hot zone for the divergent evolution of α/β hydrolases. Our findings may provide an opportunity for better understanding of the mechanism of divergent evolution in the α/β hydrolase fold superfamily, and may also guide the design of novel biocatalysts for industrial applications.

  1. Antibacterial activity and cytotoxicity of essential oil of Lantana ...

    African Journals Online (AJOL)

    The essential oil was tested for antibacterial activity against 6 strains, using disc diffusion method, and for cytotoxicity using brine-shrimp lethality assay. The oil showed moderate activity against Candida albican, Bacillus subtilis, Staphylococcus typhi, Pseudomonas aeruginosa and Bacillus aureus. These activities support ...

  2. Phytochemistry, cytotoxicity and antiviral activity of Eleusine indica (sambau)

    Science.gov (United States)

    Iberahim, Rashidah; Yaacob, Wan Ahmad; Ibrahim, Nazlina

    2015-09-01

    Goose grass also known as Eleusine indica (EI) is a local medicinal plant that displays antioxidant, antimicrobial and anticancer activities. The present study is to determine the phytochemical constituents, cytotoxicity and antiviral activities for both crude extract and fraction obtained from the plant. The crude extract contained more secondary metabolites compared to the hexane fraction as gauged using standard phytochemical tests. Cytotoxicity screening against Vero cells using MTT assay showed that the CC50 values for crude extract and hexane fraction were 2.07 and 5.62 mg/ml respectively. The antiviral activity towards Herpes Simplex Virus type 1 (HSV-1) was determined using plaque reduction assay. The selective indices (SI = CC50 / EC50) for both methanol extract and hexane fraction were 12.2 and 6.2 respectively. These results demonstrate that the extract prepared from E. indica possesses phytochemical compound that was non cytotoxic to the cell with potential antiviral activity.

  3. Cytotoxic activity of plants from East Azarbaijan province, Iran

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    M. Irani

    2017-11-01

    Full Text Available Background and objectives: Due to the high cancer mortality rates and side effects of different types of cancer treatments, discovering effective treatments without or with fewer side effects is the main purpose of many researchers all around the world. Plants play an important role in the discovery of new drugs. Iran owns rich and varied vegetation but the majority of these plants have not yet undergone chemical, pharmacological and toxicological studies. In the present study, some species from East Azarbaijan province of Iran were evaluated for cytotoxicity effects. Methods: Total methanol extract of 29 plants from 18 families were screened for their cytotoxic activities. The inhibition of cell growth for these extracts was evaluated against MCF-7, A-549, Hep-G2, HT-29 and MDBK cell lines. Their 50% inhibitions of growth (IC50 were determined by MTT assay. Moreover, cytotoxic evaluation of different fractions (ether de petrol, chloroform and methanol of the most potent species was performed. Results: Total extracts and fractions of Bryonia aspera, Centaurea salicifolia, Cuscuta chinensis, Ecbalium elaterium, Gypsophila ruscifolia, Ononis spinosa exhibited potent cytotoxic activity against one or more of the cell lines. Three of the mentioned total extracts presented cytotoxicity effects exclusively against HT-29 cells. Also three fractions (one ether de petrol and two chloroform fractions demonstrated selective cytotoxicity effects against MCF-7cells. Conclusion: It was concluded that these 6 potent species were proper candidates for identification and isolation of active ingredients with cytotoxic effects  and further studies about these species are recommended.

  4. Antimycobacterial, antioxidant and cytotoxic activities of essential oil ...

    African Journals Online (AJOL)

    Background: The aim of this study was to assess the antimycobacterial, antioxidant and the cytotoxic activities of the essential oil from the gall part of Pistacia atlantica Desf from Algeria. Materials and Methods: The antimycobacterial activity was evaluated by the broth microdilution method against three species of ...

  5. In vitro Antimalarial and Cytotoxic Activities of Leaf Extracts of ...

    African Journals Online (AJOL)

    The antiplasmodial and cytotoxic activity of leaf extracts of Vernonia amygdalina was studied. The plant leaves were prepared into three extract forms: ethanolic, aqueous, and hydroethanolic (50:50) using standard procedures. The extracts were evaluated in vitro for antiplasmodial activity using a. 3D7 chloroquine sensitive ...

  6. In vitro Antifungal, Antioxidant and Cytotoxic Activities of a Partially ...

    African Journals Online (AJOL)

    The cytotoxicity of these extracts was tested on Vero cell lines. Results: Both the aqueous extract and protein fraction (AMP III) of Atlantia monophylla leaf exhibited higher antifungal activity on Candida albicans than on Aspergillus fumigatus. AMP III fraction showed greater in vitro antioxidant activity than the aqueous extract ...

  7. Cytotoxic, anti-inflammatory and antioxidant activities of four different ...

    African Journals Online (AJOL)

    Purpose: To evaluate the cytotoxic, anti-inflammatory and antioxidant activities of four different solvent ... antioxidant activity with 2.33 ± 0.09 µmol Trolox/mg , 7.10 ± 0.9 g tannic acid equivalent (TAE), and IC50 ..... adenocarcinoma cell line. e WS1, human normal skin fibroblasts cell line. f Positive control. g An extract was.

  8. Chemical constituents of Lecythis pisonis and cytotoxic activity

    Directory of Open Access Journals (Sweden)

    Jocélia P. C. Oliveira

    2012-10-01

    Full Text Available The phytochemical investigation of the ethanol extract from leaves of Lecythis pisonis Cambess., Lecythidaceae, resulted in the isolation of seven triterpenes: α- and β-amyrin, uvaol and erythrodiol, ursolic and oleanolic acids and 3β-friedelinol, as well as a mixture of sitosterol and stigmasterol steroids and a diterpene (E-phytol. The structures of these compounds were identified by¹H and 13C NMR spectral analysis and compared with literature data. The mixture of triterpenes ursolic and oleanolic acids isolated from the active ethereal fraction showed moderate cytotoxic activity. This paper describes for the first time the phytochemical and cytotoxic study of Lecythis pisonis' leaves.

  9. Selective cytotoxic activity of new lipophilic hydroxytyrosol alkyl ether derivatives.

    Science.gov (United States)

    Calderón-Montaño, José Manuel; Madrona, Andrés; Burgos-Morón, Estefanía; Orta, Manuel Luis; Mateos, Santiago; Espartero, José Luis; López-Lázaro, Miguel

    2013-05-29

    Recent data suggest that hydroxytyrosol, a phenolic compound of virgin olive oils, has anticancer activity. This communication reports the synthesis of decyl and hexadecyl hydroxytyrosyl ethers, as well as the cytotoxic activity of hydroxytyrosol and a series of seven hydroxytyrosol alkyl ether derivatives against A549 lung cancer cells and MRC5 non-malignant lung fibroblasts. Hydroxytyrosyl dodecyl ether (HTDE) showed the highest selective cytotoxicity, and possible mechanisms of action were investigated; results suggest that HTDE can moderately inhibit glycolysis, induce oxidative stress, and cause DNA damage in A549 cells. The combination of HTDE with the anticancer drug 5-fluorouracil induced a synergistic cytotoxicity in A549 cancer cells but not in non-malignant MRC5 cells. HTDE also displayed selective cytotoxicity against MCF7 breast cancer cells versus MCF10 normal breast epithelial cells in the 1-30 μM range. These results suggest that the cytotoxicity of HTDE is more potent and selective than that of parent compound hydroxytyrosol.

  10. In vitro Cytotoxic, Antibacterial and Antiviral Activities of Triterpenes ...

    African Journals Online (AJOL)

    Purpose: To study the phytochemical composition of Siphonochalina siphonella sponge from the western coast of the Red Sea and to evaluate the isolates for possible in vitro cytotoxic, antibacterial and antiviral activities. Methods: The compounds obtained were isolated and purified by different chromatographic means.

  11. Studies on the antidiarrhoeal, antimicrobial and cytotoxic activities of ...

    African Journals Online (AJOL)

    This study screened the antidiarrhoeal, antimicrobial and cytotoxic effects of ethanol-extracted leaves of yellow oleander (Thevetia peruviana). The extract was tested against castor oil-induced diarrhoea in a model of albino rats and showed significant antidiarrhoeal activity (P<0.01). Disc diffusion technique was used to test ...

  12. Cytotoxicity and Apoptotic Activity of Ficus pseudopalma Blanco ...

    African Journals Online (AJOL)

    Purpose: To investigate the cytotoxic and apoptotic activities of Ficus pseudopalma (FP) Blanco leaf extracts against normal human FSE cells and human prostate PRST2 cancer cell line. Methods: FP leaves were extracted with 95 % ethanol, and partitioned with chloroform, ethylacetate, and water. The presence of ...

  13. Anti-leishmanial and cytotoxic activities of extracts from three ...

    African Journals Online (AJOL)

    Purpose: To evaluate the in vitro and in vivo anti-leishmanial and cytotoxic activities of extracts of different parts of Lawsonia Inermis, Morus nigra and Ziziphus mauritiana. Methods: The methanol extracts of all three plant materials at concentrations of 10 - 100 μg/mL were tested for their in vitro anti-leishmanial effects on L.

  14. In vitro antifungal and cytotoxicity activities of selected Tanzanian ...

    African Journals Online (AJOL)

    Abstract. Purpose: To evaluate the antifungal and cytotoxic activities of four medicinal plants from Tanzania, namely, Mystroxylon ... Methods: The plant materials were subjected to extraction using dichloromethane, ethyl acetate and distilled water. ...... leaves is highly recommended for sustainability of plants as the use of ...

  15. Cytotoxicity, Total Phenolic Contents and Antioxidant Activity of the ...

    African Journals Online (AJOL)

    The leaves of Annona muricata were extracted using ethanol and the extracts were evaluated for cytotoxicity using Brine Shrimp Lethality Assay, total phenolic content (TPC) and antioxidant activity using DPPH radical scavenging assay. The crude extract showed 73.33 % mortality at 1000 μg/mL concentration and its ...

  16. Cytotoxic activity of some Tanzanian medicinal plants | Runyoro ...

    African Journals Online (AJOL)

    Thirty-three aqueous methanolic extracts obtained from thirty plant species, belonging to seventeen families were screened for cytotoxic activity against HeLa (Human cervical carcinoma) cells. The ability of the extracts (10 g/ml and 1 g/ml) to inhibit proliferation of HeLa cells was determined using the 3-(4 ...

  17. Cytotoxic, anti-inflammatory and antioxidant activities of four different ...

    African Journals Online (AJOL)

    for incubation of all cells. Screening for cytotoxic activity. Growing cells were exponentially located in 96- well microplates (Costar, Corning Inc.) at a density of 5 × 103 cells per well in 100 µL of culture medium and were led to adhere for 16 h before application. All G. officinalis extracts were made in a series of eight two fold ...

  18. Leishmanicidal and cytotoxic activity of extracts and saponins from ...

    African Journals Online (AJOL)

    This compound showed similar leishmanicidal activity and cytotoxicity to meglumine antimoniate and amphotericin B, respectively, drugs currently used for the treatment of leishmaniasis. Conclusions: Based on these results, Ilex laurina is a potential source of compounds that can lead to the development of new therapeutic ...

  19. Cytotoxic activities of Coriolus versicolor (Yunzhi) extracts on human ...

    African Journals Online (AJOL)

    Cytotoxic activities of Coriolus versicolor (Yunzhi) extracts on human liver cancer and breast cancer cell line. ... African Journal of Biotechnology ... studies have demonstrated that CVP can inhibit the proliferation of cancer cells in vitro and in vivo, the different purity level of CVP has a different affect on various cancer cells.

  20. The antifungal activity and cytotoxicity of silver containing denture ...

    African Journals Online (AJOL)

    Objective: Denture base materials are susceptible to fungal adhesion, which is an important etiological issue in the pathogenesis of denture stomatitis. The purpose of this in vitro study was to evaluate the antifungal activity and cytotoxicity of denture base material containing silver microparticles. Materials and Methods: The ...

  1. Terpenoids from Ainsliaea latifolia and their cytotoxic activities.

    Science.gov (United States)

    Dong, Xue-Yun; Wang, Guo-Wei; Zhuo, Zhi-Guo; Lv, Chao; Fang, Xin; Shi, Zhi-Ran; Zeng, Ren-Tao; Shen, Yun-Heng; Zhang, Wei-Dong

    2016-01-01

    Two new compounds including one new sesquiterpenoid and one new monoterpenoid, together with 10 known compounds were isolated from the whole plants of Ainsliaea latifolia. The structures of these compounds were elucidated by analysis of spectroscopic data. All compounds were evaluated for their cytotoxic activities.

  2. Antiproliferative activity of cytotoxic tuber lectins from Solanum ...

    African Journals Online (AJOL)

    Twenty (20) kDa chitin-binding lectins from Solanum tuberosum tubers, STL-S and STL-D were purified through ion-exchange and affinity chromatographic methods, hemagglutinating activity and blood group specificity of the lectins were checked whereas the cytotoxicity was determined using brine shrimp (Artemia salina ...

  3. Anti-leishmanial and cytotoxic activities of extracts from three ...

    African Journals Online (AJOL)

    Purpose: To evaluate the in vitro and in vivo anti-leishmanial and cytotoxic activities of extracts of different parts of Lawsonia Inermis, Morus nigra and Ziziphus mauritiana. Methods: The methanol extracts of all three plant materials at concentrations of 10 - 100 µg/mL were tested for their in vitro anti-leishmanial effects on L.

  4. The Antifungal Activity and Cytotoxicity of Silver Containing Denture ...

    African Journals Online (AJOL)

    2015-10-30

    Oct 30, 2015 ... time- or silver-dependent cytotoxicity of PMMA denture base material containing ... dental materials.[14] Silver ions are biologically active,[15,16] so silver may have adverse effects on human cells.[17]. Although the literature reports various ..... vitro Candida colonization on acrylic resins and denture liners:.

  5. Cytotoxic activity of the Proteus hemolysin HpmA.

    OpenAIRE

    Swihart, K G; Welch, R. A.

    1990-01-01

    We previously showed that hpmA is the hemolysin determinant most commonly found among Proteus isolates. To assess the potential contribution of HpmA to virulence, we first characterized the toxic activities of this hemolysin. Hemolytic activity was present in total cell cultures and cell-free supernatants of Proteus clinical isolates as well as Escherichia coli containing cloned hpm genes. HpmA also possesses cytotoxic activity which was detected by a chromium release assay against a variety ...

  6. Immunomodulatory, Cytotoxicity, and Antioxidant Activities of Roots of Ziziphus mauritiana

    Science.gov (United States)

    Afzal, Samina; Batool, Murium; Ch, Bashir Ahmad; Ahmad, Ashfaq; Uzair, Muhammad; Afzal, Khurram

    2017-01-01

    Aims: The study is conducted to evaluate the immunomodulatory, cytotoxicity, and antioxidant potential of Ziziphus mauritiana (Rhamnaceae). Phytochemical analysis of Z. mauritiana revealed the presence of alkaloids, anthraquinone glycoside, cardiac glycoside, saponin, tannin, and flavonoids. Methodology: The cytotoxicity of the plant Z. mauritiana was evaluated by brine shrimp lethality test. Antioxidant parameters such as superoxide dismutase (SOD), total antioxidant capacity (T-AOC), and malondialdehyde (MDA) levels were calculated in the plasma of rats after chronic administration of 400 mg/kg of Z. mauritiana for 6 weeks. Results: The dichloromethane extract of the plant exhibited significant immunomodulatory activity, with inhibitory concentration 50% of 55.43 ± 7.9. The dichloromethane extracts of the plant showed 70% mortality at concentration 1000 μg/ml. SOD and T-AOC levels were increased while MDA level in the plasma was reduced in the plasma of rats treated with dichloromethane Z. mauritiana. Conclusion: This can be deduced that the root of Z. mauritiana has immunomodulatory, cytotoxic, and antioxidant potential. SUMMARY Roots of Z. mauritiana was exhibited immunomodulator, cytotoxic and antioxidant activitiesZ. mauritiana showed potential antioxidant activity in rats Abbreviations used: SOD: Superoxide dismutase; T-AOC: Total antioxidant capacity; MDA: Malondialdehyde; ZMRD: Z. mauritiana root extract of dichloromethane fraction; LD50: Z. mauritiana root extract of methanol fraction ZMRM, lethal dose 50. PMID:28808390

  7. 78 FR 13857 - Foreign-Trade Zone 93-Raleigh-Durham, NC; Authorization of Production Activity; Revlon Consumer...

    Science.gov (United States)

    2013-03-01

    ...; Revlon Consumer Products Corporation (Hair Coloring Products); Oxford, NC On October 10, 2012, Revlon... activity to the Foreign-Trade Zones (FTZ) Board on behalf of Revlon Consumer Products Corporation, within...

  8. Antioxidant, Antitubercular and Cytotoxic Activities of Piper imperiale

    Directory of Open Access Journals (Sweden)

    Sanjib Bhakta

    2012-04-01

    Full Text Available Phenolic compounds are widely distributed in Nature and act as pharmacologically active constituents in many herbal medicines. They have multiple biological properties, most notably antioxidant, antibacterial and cytotoxic activities. In the present study an attempt to correlate the phenolic composition of leaf, flower and wood extracts of Piper imperiale, with antioxidant, antitubercular and cytotoxic activities was undertaken. The total phenol content ranged from 1.98 to 6.94 mg GAE/gDW among ethanolic extracts, and gallic acid, catechin, epicatechin, ferulic acid, resveratrol and quercetin were identified and quantified by HPLC. DPPH and ABTS assays showed high antioxidant activity of the leaf extract (EC50ABTS = 15.6 µg/mL, EC50DPPH = 27.3 µg/mL with EC50 in the same order of magnitude as the hydroxyquinone (EC50ABTS = 10.2 µg/mL, EC50DPPH = 15.7 µg/mL. The flower extract showed strong antimicrobial activity against Mycobacterium tuberculosis H37Rv. All the extracts exhibited dose-dependent cytotoxic effects against MCF-7 cancer cells. This is the first time that a Piper extract has been found to be highly active against M. tuberculosis. This study shows the biological potential of Piper imperiale extracts and gives way to bio-guided studies with well-defined biological activities.

  9. Anticonvulsant, Antimicrobial and Cytotoxic Activities of Berberis ...

    African Journals Online (AJOL)

    Diazepam was used as standard drug. Antimicrobial activity of the extract against Bacillus subtilis, ... Conclusion: The plant is thus a potential source of new lead compounds for the development of new clinically effective anticonvulsant and antimicrobial compounds. Keywords: Berberis calliobotrys, Anticonvulsant, ...

  10. Anticonvulsant, Antimicrobial and Cytotoxic Activities of Berberis ...

    African Journals Online (AJOL)

    1University College of Pharmacy, University of the Punjab, Lahore-54000, 2Faculty of Pharmacy, University of Sargodha, ... was used as standard drug. Antimicrobial activity of the extract against Bacillus subtilis, Pseudomonas aeruginosa, Staphylococcus .... The anticonvulsant effect of plant crude extract and its various ...

  11. Cytotoxic and antioxidant activities of selected Lamiales species from Mexico.

    Science.gov (United States)

    Moreno-Escobar, J A; Bazald A, S; Villarreal, M L; Bonilla-Barbosa, J R; Mendoza, S; Rodríguez-López, V

    2011-12-01

    Methanol extracts obtained from eight species belonging to four families of the Lamiales order native to Mexico were investigated for biological action. Cytotoxicity and antioxidant activity of methanol extracts have been investigated. Cytotoxic activity was evaluated by the sulphorhodamine B protein staining assay against KB (nasopharyngeal), HEp-2 (larynx), HF-6 (colon), MCF7 (breast), PC-3 (prostate), and Ca Ski (cervix) carcinoma cell lines. To analyze the antioxidant activity, common stable radicals chromogens, 2,2-azino-bis(3-ethylbenzthiazoline-6-sulfonic acid (ABTS+) and DPPH (1,1-diphenyl-2-picrylhydrazyl) were used. The ferric reducing antioxidant power (FRAP) and the total phenolic content of the samples were also determined. Some of the extracts, such as Limosella aquatica L. (Scrophulariaceae), Mimulus glabratus Kunth. (Phrymaceae), Pedicularis mexicana Zucc. ex Benth. (Orobanchaceae), and Penstemon campanulatus (Cav.) Willd. (Plantaginaceae) displayed remarkably selective cytotoxic activity. However, the extract from Veronica americana (Raf.) Schwein (Plantaginaceae) showed the highest activity with IC₅₀ values of 1.46 and 0.169 g/ μL on PC-3 and HF-6 cells, respectively. With the exception of M. glabratus, all the extracts showed different degrees of antioxidant activity with IC₅₀ values from 0.89 up to 1.8 in the ABTS assay; from 0.49 up to 1.25 mg/mL in the DPPH assay and with the FRAP evaluation, 36 to 68 equivalents in mM of FeSO₄. V. americana also showed the highest antoxidant activity with IC₅₀ values from 0.491 and 0.892 mg/mL, on DPPH and ABTS assays, respectively. These findings demonstrated that the species studied have great potential cytotoxic and antioxidant activity.

  12. Cytotoxicity and trypanocidal activity of nifurtimox encapsulated in ethylcyanoacrylate nanoparticles.

    Science.gov (United States)

    Sánchez, Gittith; Cuellar, Daniela; Zulantay, Ines; Gajardo, Marta; González-Martin, Guillermo

    2002-01-01

    The aim of the present study was to study the trypanocidal activity of nanoparticles loaded with nifurtimox in comparison with the free drug against Trypanosoma cruzi, responsible for Chagas' disease. Ethylcyanoacrylate nanoparticles acted as the delivery system into cells. As the obligate replicative intracellular form is amastigote, in vitro studies were performed on this form of parasite as well as on cell culture derived trypomastigotes. The fluorescence method used here was very useful as it allowed for the simultaneous study of trypanocide activity and cytotoxicity by determining living or dead parasites within living or dead host cells. According to these results, the greatest trypanocide activity on cell culture-derived trypomastigotes was recorded for nifurtimox-loaded nanoparticles with a 50% inhibitory concentration (IC50) twenty times less than that of the free drug. The cytotoxicity of unloaded nanoparticles at low concentrations was similar to that obtained by free drug when evaluated on Vero cells. Furthermore, nifurtimox-loaded nanoparticles showed increased trypanocide activity on intracellular amastigotes with an IC50 thirteen times less than that of nifurtimox. We also observed that the unloaded nanoparticles possess the previously-described trypanocide activity, similar to the standard solution of nifurtimox, although the mechanism for this has not yet been elucidated. In conclusion, it was possible to establish in vitro conditions using nifurtimox encapsulated nanoparticles in order to decrease the doses of the drug and thus to obtain high trypanocidal activity on both free trypomastigotes and intracellular amastigotes with low cytotoxicity for the host cell.

  13. In vitro cytotoxic activity of Brazilian Middle West plant extracts

    Directory of Open Access Journals (Sweden)

    Talal Suleiman Mahmoud

    2011-06-01

    Full Text Available Cytotoxic activity of eight plant extracts, native from the Mid-West of Brazil comprising Cerrado, Pantanal and semideciduous forest, was evaluated for MDA-MB-435, SF-295, and HCT-8 cancer cell strains. A single 100 µg.mL-1 dose of each extract was employed with 72 h of incubation for all tests. Doxorubicin (1 µg.mL-1 was used as the positive control and the MTT method was used to detect the activity. Cytotoxicity of distinct polarities was observed in thirty extracts (46%, from different parts of the following species: Tabebuia heptaphylla (Vell. Toledo, Bignoniaceae, Tapirira guianensis Aubl., Anacardiaceae, Myracrodruon urundeuva Allemão, Anacardiaceae, Schinus terebinthifolius Raddi, Anacardiaceae, Gomphrena elegans Mart., Amaranthaceae, Attalea phalerata Mart. ex Spreng., Arecaceae, Eugenia uniflora L., Myrtaceae, and Annona dioica A. St.-Hil., Annonaceae. Extracts of at least two tested cell strains were considered to be highly active since their inhibition rate was over 75%.

  14. Antibacterial and Cytotoxic Activity of Compounds Isolated from Flourensia oolepis

    Directory of Open Access Journals (Sweden)

    Mariana Belén Joray

    2015-01-01

    Full Text Available The antibacterial and cytotoxic effects of metabolites isolated from an antibacterial extract of Flourensia oolepis were evaluated. Bioguided fractionation led to five flavonoids, identified as 2′,4′-dihydroxychalcone (1, isoliquiritigenin (2, pinocembrin (3, 7-hydroxyflavanone (4, and 7,4′-dihydroxy-3′-methoxyflavanone (5. Compound 1 showed the highest antibacterial effect, with minimum inhibitory concentration (MIC values ranging from 31 to 62 and 62 to 250 μg/mL, against Gram-positive and Gram-negative bacteria, respectively. On further assays, the cytotoxic effect of compounds 1–5 was determined by MTT assay on acute lymphoblastic leukemia (ALL and chronic myeloid leukemia (CML cell lines including their multidrug resistant (MDR phenotypes. Compound 1 induced a remarkable cytotoxic activity toward ALL cells (IC50 = 6.6–9.9 μM and a lower effect against CML cells (IC50 = 27.5–30.0 μM. Flow cytometry was used to analyze cell cycle distribution and cell death by PI-labeled cells and by Annexin V/PI staining, respectively. Upon treatment, 1 induced cell cycle arrest in the G2/M phase accompanied by a strong induction of apoptosis. These results describe for the first time the antibacterial metabolites of F. oolepis extract, with 1 being the most effective. This chalcone also emerges as a selective cytotoxic agent against sensitive and resistant leukemic cells, highlighting its potential as a lead compound.

  15. Evaluation of the cytotoxic activity of some Brazilian medicinal plants.

    Science.gov (United States)

    Ribeiro, Sandra S; de Jesus, Aline M; dos Anjos, Charlene S; da Silva, Thanany B; Santos, Alan D C; de Jesus, Jemmyson R; Andrade, Moacir S; Sampaio, Tais S; Gomes, Wesley F; Alves, Péricles B; Carvalho, Adriana A; Pessoa, Claudia; de Moraes, Manoel O; Pinheiro, Maria L B; Prata, Ana Paula N; Blank, Arie F; Silva-Mann, Renata; Moraes, Valeria R S; Costa, Emmanoel V; Nogueira, Paulo Cesar L; Bezerra, Daniel P

    2012-09-01

    Plants are promising sources of new bioactive compounds. The aim of this study was to investigate the cytotoxic potential of nine plants found in Brazil. The species studied were: Annona pickelii Diels (Annonaceae), Annona salzmannii A. DC. (Annonaceae), Guatteria blepharophylla Mart. (Annonaceae), Guatteria hispida (R. E. Fr.) Erkens & Maas (Annonaceae), Hancornia speciosa Gomes (Apocynaceae), Jatropha curcas L. (Euphorbiaceae), Kielmeyera rugosa Choisy (Clusiaceae), Lippia gracilis Schauer (Verbenaceae), and Hyptis calida Mart. Ex Benth (Lamiaceae). Different types of extractions from several parts of plants resulted in 43 extracts. Their cytotoxicity was tested against HCT-8 (colon carcinoma), MDA-MB-435 (melanoma), SF-295 (glioblastoma), and HL-60 (promielocitic leukemia) human tumor cell lines, using the thiazolyl blue test (MTT) assay. The active extracts were those obtained from G. blepharophylla, G. hispida, J. curcas, K. rugosa, and L. gracilis. In addition, seven compounds isolated from the active extracts were tested; among them, β-pinene found in G. hispida and one coumarin isolated from K. rugora showed weak cytotoxic activity. In summary, this manuscript contributes to the understanding of the potentialities of Brazilian plants as sources of new anticancer drugs. Georg Thieme Verlag KG Stuttgart · New York.

  16. Guanacastane-type diterpenoids with cytotoxic activity from Coprinus plicatilis.

    Science.gov (United States)

    Liu, Yuanzhen; Li, Yaoyao; Ou, Yixin; Xiao, Shuyan; Lu, Chunhua; Zheng, Zhonghui; Shen, Yuemao

    2012-08-01

    Four new guanacastane-type diterpenoids (1-4), together with the known compound, guanacastepene E (5), were isolated from a basidiomycete of the macro-fungi, Coprinus plicatilis 82. Their structures were elucidated on the basis of extensive spectroscopic analyses, including FT-ICR-MS, UV, IR and 1D and 2D NMR experiments. The in vitro cytotoxic activities of all compounds against the human cancer cell lines HepG2, HeLa, MDA-MB-231, BGC-823, HCT 116, and U2OS were evaluated, only compound 1 exhibited significant cytotoxicities with IC(50) values ranging from 1.2 to 6.0 μM. Copyright © 2012 Elsevier Ltd. All rights reserved.

  17. Cytotoxic Activity and G1 Cell Cycle Arrest of a Dienynone from Echinacea pallida

    DEFF Research Database (Denmark)

    Chicca, Andrea; Adinolfi, Barbara; Pellati, Federica

    2009-01-01

    In the present study, a further investigation of the cytotoxic activity of an acetylenic constituent of ECHINACEA PALLIDA roots, namely, pentadeca-(8 Z,13 Z)-dien-11-yn-2-one, was performed, revealing a concentration-dependent cytotoxicity on several human cancer cell lines, including leukemia...... that the cytotoxic activity can be attributed mainly to the genuine, not oxidized, molecule....

  18. Antimycobacterial and cytotoxic activity of selected medicinal plant extracts.

    Science.gov (United States)

    Nguta, Joseph M; Appiah-Opong, Regina; Nyarko, Alexander K; Yeboah-Manu, Dorothy; Addo, Phyllis G A; Otchere, Isaac; Kissi-Twum, Abena

    2016-04-22

    Tuberculosis (TB) caused by Mycobacterium tuberculosis remains an ongoing threat to human health. Several medicinal plants are used traditionally to treat tuberculosis in Ghana. The current study was designed to investigate the antimycobacterial activity and cytotoxicity of crude extracts from five selected medicinal plants. The microplate alamar blue assay (MABA) was used for antimycobacterial studies while the CellTiter 96® AQueous Assay, which is composed of solutions of a novel tetrazolium compound [3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium, inner salt; MTS] and an electron coupling reagent (phenazine methosulfate) PMS, was used for cytotoxic studies. Correlation coefficients were used to compare the activity of crude extracts against nonpathogenic strains and the pathogenic Mycobacterium tuberculosis subsp.tuberculosis. Results of the MIC determinations indicated that all the crude extracts were active on all the three tested mycobacterial strains. Minimum inhibitory concentration values as low as 156.3µg/mL against M. tuberculosis; Strain H37Ra (ATCC® 25,177™) were recorded from the leaves of Solanum torvum Sw. (Solanaceae). Cytotoxicity of the extracts varied, and the leaves from S. torvum had the most promising selectivity index. Activity against M. tuberculosis; Strain H37Ra was the best predictor of activity against pathogenic Mycobacterium tuberculosis subsp.tuberculosis (correlation coefficient=0.8). The overall results of the present study provide supportive data on the use of some medicinal plants for tuberculosis treatment. The leaves of Solanum torvum are a potential source of anti-TB natural products and deserve further investigations to develop novel anti-TB agents against sensitive and drug resistant strains of M. tuberculosis. Copyright © 2016 The Authors. Published by Elsevier Ireland Ltd.. All rights reserved.

  19. Antiprotozoal and cytotoxic activities in vitro of Colombian Annonaceae.

    Science.gov (United States)

    Osorio, Edison; Arango, Gabriel Jaime; Jiménez, Nora; Alzate, Fernando; Ruiz, Grace; Gutiérrez, David; Paco, Marco Antonio; Giménez, Alberto; Robledo, Sara

    2007-05-22

    Ethnobotanical and chemotaxonomical studies for antiparasitic activity of Colombian Annonaceae were carried out. In vitro antiprotozoal activity of 36 extracts obtained from six different species was determined against promastigotes of three Leishmania species, epimastigotes of Trypanosoma cruzi and both chloroquine sensitive (F32) and resistant (W2) Plasmodium falciparum. Cytotoxic activity was evaluated in U-937 cells. Active extracts were selected according their selectivity index (SI). Extracts from Annona muricata, Rollinia exsucca, Rollinia pittieri and Xylopia aromatica were active against Leishmania spp. and Trypanosoma cruzi showing IC50 values lower than 25 microg/ml. Hexane extract from Rollinia pittieri leaves was the most selective against Trypanosoma cruzi and Leishmania spp. (IS=10 and 16, respectively). The extracts from Desmopsis panamensis, Pseudomalmea boyacana, Rollinia exsucca and Rollinia pittieri showed good antiplasmodial activity (IC50 Annonaceae extracts. Results presented here also demonstrate which plants and/or plant parts could be useful in the treatment of leishmaniasis, Chagas' disease and malaria.

  20. Cytotoxic activity of chalcones isolated from lonchocarpus sericeus (pocr.) kunth.

    Science.gov (United States)

    Cunha, Geanne M de Andrade; Fontenele, Juvenia Bezerra; Nobre Júnior, Hélio V; De Sousa, Francisco C M; Silveira, Edilberto R; Nogueira, Nádia A P; De Moraes, Manoel Odorico; Viana, Glauce S B; Costa-Lotufo, Letícia V

    2003-02-01

    In the present study, it was demonstrated that the hexanic extract obtained from the roots of Lonchocarpus sericeus and one of its major components, derricin, but not lonchocarpin, show cytotoxic activity to fertilized sea urchin eggs. Both inhibited the first cleavage of sea urchin eggs in a dose-dependent manner with an IC(50) of 30.4 (26.2-35.3) microgram/mL for the crude extract and 51.2 (42.1-62.3) microgram/mL for derricin (n = 6, in both cases). Furthermore, the hexanic extract of L. sericeus, and the isolated compounds, derricin and lonchocarpin showed cytotoxicity against CEM leukaemic cell line (IC(50) = 17.6 (13.7-22.6), 13.0 (12.0-14.0) and 10.4 (5.6-19.1) microgram/ml (n = 6), respectively). When these substances (6.25 to 125 microgram/25 microL) were examined for antimicrobial activity against Escherichia coli, Staphylococcus aureus and Candida albicans, none of them were found to be active. Neither the hexanic extract, nor the isolated compounds derricin and lonchocarpin (0.5 to 250 microgram/mL) presented hemolytic activity. These results indicated a possible antimitotic activity of L. sericeus crude extract and their major constituents. Copyright 2003 John Wiley & Sons, Ltd.

  1. Cytotoxic Activity of Alkaloids from Papaver rhoeas growing in Lebanon

    Directory of Open Access Journals (Sweden)

    Mohamad Ali Hijazi

    2017-03-01

    Full Text Available This paper represents the phytochemical properties of Lebanese Papaver rhoeas, from which five protopine alkaloids are isolated, namely; stylopine (1, canadine (2, sinactine (3, berberine (4, and epiberberine (5. This is the first report for the isolation of epiberberine (5 from the genus Papaver and canadine (2 from Papaver rhoeas, suggesting a new chemotype of Papaver rhoeas growing in Lebanon. The cytotoxic activity of the total ethanolic extract and the isolated alkaloids were determined by MTT assay on human colon cancer cells (HCT116, breast cancer cells (MCF7, human keratinocyte cell line (HaCaT, and non-cancerous colon cells (NCM460. The compounds showed dose-dependent inhibitory effect with highest activity for compound 4 against all cell lines. The activity of the alkaloids varied between the various cell lines indicating cell type specificity and suggesting different cell-compound interactions. IC 50 values on normal cells was higher than cancer cell lines (>200 µM, indicating the selectivity of these compounds to cancer cells. It was noticed that the presence of methylenedioxy group at positions C-2 and C-3 rather than at position C-9 and C-10 potentiated the compound’s cytotoxic activity. Further studies are underway to explore the activity of these compounds at the molecular level.

  2. l282nc.m77t - MGD77 data file for Geophysical data from field activity L-2-82-NC in Off San Mateo, Northern California from 02/07/1982 to 02/12/1982

    Data.gov (United States)

    U.S. Geological Survey, Department of the Interior — Single-beam bathymetry, gravity, and magnetic data along with DGPS navigation data was collected as part of field activity L-2-82-NC in Off San Mateo, Northern...

  3. l477nc.m77t - MGD77 data file for Geophysical data from field activity L-4-77-NC in Northern California from 05/10/1977 to 05/21/1977

    Data.gov (United States)

    U.S. Geological Survey, Department of the Interior — Single-beam bathymetry, gravity, and magnetic data along with DGPS navigation data was collected as part of field activity L-4-77-NC in Northern California from...

  4. Antimicrobial and Cytotoxic Activities of Extracts from Laurus nobilis Leaves

    KAUST Repository

    Felemban, Shaza

    2011-05-01

    The cytotoxic activity and antimicrobial properties of crude extracts from Laurus nobilis were investigated. With the use of the organic solvents, methanol and ethanol, crude extracts were obtained. To determine the availability of active bio‐compounds, an analysis using liquid chromatography was conducted. The crude extract was also tested for antimicrobial activity. The disc diffusion method was used against the bacterium Escherichia coli. The results showed a weak antimicrobial activity against E. coli. For cytotoxicity testing, the crude extract was studied on four cell-­lines: human breast adenocarcinoma, human embryonic kidney, HeLa (human cervical adenocarcinoma), and human lung fibroblast. From the alamarBlue® assay results, the extracts most potently affected the cell-­lines of human breast adenocarcinoma and human embryonic kidney. Using the lactate dehydrogenase (LDH) assay, an effect on human embryonic kidney was most prominent. With these findings, a suggestion that the crude extract of Laurus nobilis may have antiproliferative properties is put forth, with the possibility of this mechanism being induction of apoptosis with the involvement of Nuclear Factor Kappa κB (NF κB).

  5. Stable expression of EBV-gp350 on the surface of NC37 cells confers natural killer (NK)-cell susceptibility or resistance, depending on the assay used to assess NK-mediated function.

    Science.gov (United States)

    Sumonwiriya, Manutsanun; Horhthongkham, Navin; Pattanapanyasat, Kovit; Ampol, Silawun; Sutthent, Reungpung; Kantakamalakul, Wannee

    2009-10-01

    NC37 cells containing the Epstein-Barr virus (EBV) genome do not express the viral glycoprotein-350 (gp350) on the cell surface. Despite being a cancer cell line, NC37 cells show resistance to natural killer (NK) cell cytotoxicity by the standard chromium ((51)Cr) release assay (CRA). EBV-gp350 has been identified as a ligand for antibody dependent cell-mediated cytotoxicity (ADCC). The stable expression of gp350 on the NC37 cell surface membrane could make this cell line a suitable target for measuring ADCC antibody. The pcDNA3.1-gp350 was transfected into the stably expressing enhanced green fluorescent protein (EGFP)-NC37 cell line. The transfected cells were then selected for expression of gp350 on the cell surface using immunomagnetic bead-based sorting. The gp350-EGFP-NC37 cell line was then re-examined for resistance to NK cytotoxicity, and compared with the standard K562 and EGFP-K562 cell lines using the CRA and a flow cytometric method, respectively. Surprisingly, the gp350-EGFP-NC37 cells, like the parental NC37 cell line, showed comparable resistance to NK cell-mediated cytotoxic activity by the CRA, while demonstrating susceptibility to NK cell cytotoxicity comparable to EGFP expressing K562 cells by the flow cytometric method. The susceptibility of gp350-EGFP-NC37 cells to NK cell cytotoxic activity is dependent on the type of assay.

  6. Cytotoxic and Antimigratory Activities of Phenolic Compounds from Dendrobium brymerianum

    Science.gov (United States)

    Klongkumnuankarn, Pornprom; Busaranon, Kesarin; Chanvorachote, Pithi; Sritularak, Boonchoo; Jongbunprasert, Vichien; Likhitwitayawuid, Kittisak

    2015-01-01

    Chromatographic separation of a methanol extract prepared from the whole plant of Dendrobium brymerianum led to the isolation of eight phenolic compounds. Among the isolated compounds (1–8), moscatilin (1), gigantol (3), lusianthridin (4), and dendroflorin (6) showed appreciable cytotoxicity against human lung cancer cell lines with IC50 values of 196.7, 23.4, 65.0, and 125.8 μg/mL, respectively, and exhibited antimigratory property at nontoxic concentrations. This study is the first report on the biological activities of this plant. PMID:25685168

  7. Direct Microbicidal Activity of Cytotoxic T-Lymphocytes

    Directory of Open Access Journals (Sweden)

    Paul Oykhman

    2010-01-01

    Full Text Available Cytotoxic T-lymphocytes (CTL are famous for their ability to kill tumor, allogeneic and virus-infected cells. However, an emerging literature has now demonstrated that CTL also possess the ability to directly recognize and kill bacteria, parasites, and fungi. Here, we review past and recent findings demonstrating the direct microbicidal activity of both CD4+ and CD8+ CTL against various microbial pathogens. Further, this review will outline what is known regarding the mechanisms of direct killing and their underlying signalling pathways.

  8. Cytotoxic and Antimigratory Activities of Phenolic Compounds from Dendrobium brymerianum

    Directory of Open Access Journals (Sweden)

    Pornprom Klongkumnuankarn

    2015-01-01

    Full Text Available Chromatographic separation of a methanol extract prepared from the whole plant of Dendrobium brymerianum led to the isolation of eight phenolic compounds. Among the isolated compounds (1–8, moscatilin (1, gigantol (3, lusianthridin (4, and dendroflorin (6 showed appreciable cytotoxicity against human lung cancer cell lines with IC50 values of 196.7, 23.4, 65.0, and 125.8 μg/mL, respectively, and exhibited antimigratory property at nontoxic concentrations. This study is the first report on the biological activities of this plant.

  9. Synthesis, Cytotoxicity and Antileishmanial Activity of Aza-stilbene derivatives

    Directory of Open Access Journals (Sweden)

    Elaine S. Coimbra

    2013-02-01

    Full Text Available Stilbenes are compounds found in numerous medicinal plants and food products with some known biological and even antileishmanial activity. This paper describes the preparation of Aza-stilbene derivatives and their in vitro biological activities against Leishmania species. Most of the compounds with hydroxyl groups (2a,2b, 2d, 2e and 2f showed interesting results against three Leishmania species tested. Compound 2f showed the best activity against intracellular forms of L. amazonensis, with IC50 of 7.48 µM, very similar when compared to reference drug Miltefosine. It not possible associate NO production with leishmanicidal activity for all azastilbene derivatives. It is noteworthy that none of compounds tested showed cytotoxicity against macrophages

  10. Antioxidant and Cytotoxic Activities of Centella asiatica (L) Urb.

    Science.gov (United States)

    Pittella, Frederico; Dutra, Rafael C.; Junior, Dalton D.; Lopes, Miriam T. P.; Barbosa, Nádia R.

    2009-01-01

    In the present study, the phenolic (Folin-Dennis) and flavonoid (colorimetric assay) constituents, antioxidant [2,2-diphenyl-2-picrylhydrazyl hydrate (DPPH) assay] and cytotoxic activities of an aqueous extract (AE) of Centella asiatica leaves were investigated. The aqueous extract (50 g/L) was obtained by infusion followed by cold maceration for 24 h. The levels of phenolic and flavonoid compounds were 2.86 g/100 g and 0.361 g/100 g, respectively. The AE showed elevated DPPH scavenging activity, with an IC50 value of 31.25 μg/mL. The AE had a promising activity against mouse melanoma (B16F1), human breast cancer (MDA MB-231) and rat glioma (C6) cell lines, with IC50 values of 698.0, 648.0 and 1000.0 μg/mL, respectively. A positive correlation was established between the level of flavonoids, antioxidant and antitumor activities. PMID:19865514

  11. Antioxidant and Cytotoxic Activities of Centella asiatica (L Urb.

    Directory of Open Access Journals (Sweden)

    Frederico Pittella

    2009-08-01

    Full Text Available In the present study, the phenolic (Folin-Dennis and flavonoid (colorimetric assay constituents, antioxidant [2,2-diphenyl-2-picrylhydrazyl hydrate (DPPH assay] and cytotoxic activities of an aqueous extract (AE of Centella asiatica leaves were investigated. The aqueous extract (50 g/L was obtained by infusion followed by cold maceration for 24 h. The levels of phenolic and flavonoid compounds were 2.86 g/100 g and 0.361 g/100 g, respectively. The AE showed elevated DPPH scavenging activity, with an IC50 value of 31.25 μg/mL. The AE had a promising activity against mouse melanoma (B16F1, human breast cancer (MDA MB-231 and rat glioma (C6 cell lines, with IC50 values of 698.0, 648.0 and 1000.0 μg/mL, respectively. A positive correlation was established between the level of flavonoids, antioxidant and antitumor activities.

  12. Anti-inflammatory and cytotoxic activities of Bursera copallifera.

    Science.gov (United States)

    Columba-Palomares, M F María C; Villareal, Dra María L; Acevedo Quiroz, M C Macdiel E; Marquina Bahena, M C Silvia; Álvarez Berber, Dra Laura P; Rodríguez-López, Dra Verónica

    2015-10-01

    The plant species Bursera copallifera (DC) bullock is used in traditional medicine to treat inflammation. The leaves of this plant can be prepared as an infusion to treat migraines, bronchitis, and dental pain. The purpose of this study was to determine the anti-inflammatory and cytotoxic activities of organic extracts from the stems, stem bark, and leaves of B. copallifera, which was selected based on the knowledge of its traditional use. We evaluated the ability of extracts to inhibit mouse ear inflammation in response to topical application of 12-O tetradecanoylphorbol-13-acetate. The extracts with anti-inflammatory activity were evaluated for their inhibition of pro-inflammatory enzymes. In addition, the in vitro cytotoxic activities of the organic extracts were evaluated using the sulforhodamine B assay. The hydroalcoholic extract of the stems (HAS) exhibited an anti-inflammatory activity of 54.3% (0.5 mg/ear), whereas the anti-inflammatory activity of the dichloromethane-methanol extract from the leaves (DMeL) was 55.4% at a dose of 0.1 mg/ear. Methanol extract from the leaves (MeL) showed the highest anti-inflammatory activity (IC50 = 4.4 μg/mL), hydroalcoholic extract of leaves, and DMeL also reduce the enzyme activity, (IC50 = 6.5 μg/mL, IC50 = 5.7 μg/mL), respectively, from stems HAS exhibit activity at the evaluated concentrations (IC50 =6.4 μg/mL). The hydroalcoholic extract of the stems exhibited the highest cytotoxic activity against a breast adenocarcinoma cell line (MCF7, IC50 = 0.90 μg/mL), whereas DMeL exhibited an IC50 value of 19.9 μg/mL. In conclusion, extracts from leaves and stems inhibited cyclooxygenase-1, which is the target enzyme for nonsteroidal anti inflammatory drugs, and some of these extracts demonstrated substantial antiproliferative effects against the MCF7 cell line. These results validate the traditional use of B. copallifera.

  13. Synthesis, antibacterial and cytotoxic activity evaluation of hydroxyurea derivatives.

    Science.gov (United States)

    Kos, Ivan; Jadrijević-Mladar, Milena; Butula, Ivan; Biruš, Mladen; Maravić-Vlahoviček, Gordana; Dabelić, Sanja

    2013-06-01

    5 Synthesis and biological evaluation of a series (N = 16) of cyclic and acyclic hydroxyurea derivatives, including benzotriazole-, isocyanuric acid- and biuret-containing compounds, are disclosed. 1-N-(benzyloxycarbamoyl)benzotriazole was used as a benzyloxyisocyanate donor, a useful intermediate in the preparation of substituted hydroxyurea. Antibacterial activities of synthesized hydroxyurea derivatives were tested on three E. coli strains, i.e., a strain susceptible to antibiotics, a strain resistant to macrolide antibiotics and a strain resistant to aminoglycoside antibiotics. Six compounds (three acyclic and three cyclic hydroxyureas) showed growth inhibition of the tested E. coli strains, with different specificity toward each strain. Results of the cytotoxic activity evaluation revealed that twelve out of sixteen test compounds were cytotoxic to human acute monocytic leukemia THP-1 and/or human acute T cell leukemia Jurkat cell line. 1-(N-hydroxycarbamoyl) benzotriazole () increased the metabolic activity of both cell lines. Two compounds, 1-(N-hydroxycarbamoyl) benzotriazole (5) and N,N',N''-trihydroxybiuret (15), were identified as potential NO donors.

  14. Antinociceptive, cytotoxic and antibacterial activities of Cleome viscosa leaves

    Directory of Open Access Journals (Sweden)

    Utpal Bose

    2011-02-01

    Full Text Available The methanol extract of the dried leaves of Cleome viscosa L., Cleomaceae, was investigated for its possible antinociceptive, cytotoxic and antibacterial activities in animal models. The extract produced significant writhing inhibition in acetic acid-induced writhing in mice at the oral doses of 250 and 500 mg/kg body weight (p<0.001 comparable to the standard drug diclofenac sodium at the dose of 25 mg/kg of body weight (p<0.001. The crude extract produced the most prominent cytotoxic activity against brine shrimp Artemia salina (LC50 28.18 μg/mL and LC90 112.20 μg/mL. The extract of C. viscosa L. exhibited significant in vitro antibacterial activity against Staphylococcus saprophyticus, Shigella sonnie, Salmonella typhi, Vibrio cholera, Streptococcus epidermidis, Shigella flexneri and Staphylococcus aureus with the zones of inhibition ranging from 10.76 to 16.34 mm. The obtained results provide a support for the use of this plant in traditional medicine and its further investigation.

  15. Trilobolide-steroid hybrids: Synthesis, cytotoxic and antimycobacterial activity.

    Science.gov (United States)

    Jurášek, Michal; Džubák, Petr; Rimpelová, Silvie; Sedlák, David; Konečný, Petr; Frydrych, Ivo; Gurská, Soňa; Hajdúch, Marián; Bogdanová, Kateřina; Kolář, Milan; Müller, Tomáš; Kmoníčková, Eva; Ruml, Tomáš; Harmatha, Juraj; Drašar, Pavel B

    2017-01-01

    Sesquiterpene lactone trilobolide is a sarco/endoplasmic reticulum Ca2+-ATPase (SERCA) inhibitor, thus depleting the Ins(1,4,5)P3-sensitive intracellular calcium stores. Here, we describe a synthesis of a series of 6 trilobolide-steroids conjugates (estradiol, pregnene, dehydroepiandrosterone, and testosterone). We found that the newly synthesized Tb-based compounds possess different remarkable biological activities. Cancer cell cytotoxicity and preferential selectivity is represented in our study by a Tb-pregnene derivative. The most cytotoxic clickates of estradiol and pregnene were studied by FACS where impact on cell cycle and RNA synthesis was observed; live-cell microscopy revealed the impact on cell organelle morphology particularly endoplasmic reticulum, mitochondria and nucleus. Further, we have studied the estrogenic and androgenic properties of the clickate molecules using cell-based luciferase assays. Finally, antimycobacterial tests revealed that testosterone and estradiol derivatives potentiated the antimycobacterial activity up to IC50 of 10.6μM. Copyright © 2016 Elsevier Inc. All rights reserved.

  16. Antioxidant and cytotoxic activity of mono- and bissalicylic acid derivatives

    Directory of Open Access Journals (Sweden)

    Đurendić Evgenija A.

    2014-01-01

    Full Text Available A simple synthesis of mono- and bis-salicylic acid derivatives 1-10 by the transesterification of methyl salicylate (methyl 2-hydroxybenzoate with 3-oxapentane-1,5-diol, 3,6- dioxaoctane-1,8-diol, 3,6,9-trioxaundecane-1,11-diol, propane-1,2-diol or 1-aminopropan- 2-ol in alkaline conditions is reported. All compounds were tested in vitro on three malignant cell lines (MCF-7, MDA-MB-231, PC-3 and one non-tumor cell line (MRC- 5. Strong cytotoxicity against prostate PC-3 cancer cells expressed compounds 3, 4, 6, 9 and 10, all with the IC50 less than 10 μmol/L, which were 11-27 times higher than the cytotoxicity of antitumor drug doxorubicin. All tested compounds were not toxic against the non-tumor MRC-5 cell line. Antioxidant activity of the synthesized derivatives was also evaluated. Compounds 2, 5 and 8 were better OH radical scavengers than commercial antioxidants BHT and BHA. The synthesized compounds showed satisfactory scavenger activity, which was studied by QSAR modeling. A good correlation between the experimental variables IC50 DPPH and IC50 OH and MTI (molecular topological indices molecular descriptors and CAA (accessible Connolly solvent surface area for the new compounds 1, 3, and 5 was observed.

  17. Synthesis and Cytotoxic Activities of Difluoro-Dimethoxy Chalcones.

    Science.gov (United States)

    Yamali, Cem; Gul, Halise Inci; Ozgun, Dilan Ozmen; Sakagam, Hiroshi; Umemura, Naoki; Kazaz, Cavit; Gul, Mustafa

    2017-01-01

    Although anticancer chemotherapeutics are available in markets, side effects related to the drugs in clinical use lead to researchers to investigate new drug candidates which are more safe, potent and selective than others. Chalcones are popular with their anticancer activities with the several reported mechanisms including inhibition of angiogenesis, inhibition of tubulin polymerization, and induction of apoptosis etc. This study was focused on to synthesize of 1-(2,4/2,6-difluorophenyl)-3-(2,3/2,4/2,5/3,4- dimethoxyphenyl)-2-propen-1-ones (1-8) and investigate their cytotoxic properties with possible mechanism of action. The compounds were synthesized by Claisen-Schmidt condensation. The chemical structures were confirmed by 1H NMR, 13C NMR, DEPT, COSY, HMQC, HMBC, 19F NMR and HRMS. In vitro cytotoxic effects of the compounds against human tumour cell lines [gingival carcinoma (Ca9-22), oral squamous cell carcinoma (HSC-2)] and human normal oral cells [gingival fibroblasts (HGF), periodontal ligament fibroblasts (HPLF)] were evaluated via MTT test. All compounds had higher cytotoxicity than reference compound 5-Fluorouracil (5-FU). The compounds 3-7 had higher potency selectivity expression values (PSE) than 5-FU and PSE values of the compounds were over 100. All chalcone derivatives seem good candidates for further studies according to very remarkable and high PSE values. It was clearly demonstrated that compound 7 can induce early apoptosis at a concentration of 10 µM and dose-dependent late apoptosis starting at 10 µM. Compound 7 induced cleavage of the apoptosis marker PARP. The results indicate that new chalcones reported here can promote apoptosis in human tumour cell lines. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.

  18. Neuroprotective Activity of (--Epigallocatechin Gallate against Lipopolysaccharide-Mediated Cytotoxicity

    Directory of Open Access Journals (Sweden)

    Jin-Biao Liu

    2016-01-01

    Full Text Available Lipopolysaccharide- (LPS- mediated systemic inflammation plays a critical role in neurodegenerative diseases. The present study was conducted to evaluate the protective effects of epigallocatechin gallate (EGCG, the major component in green tea, on LPS-mediated inflammation and neurotoxicity. LPS treatment of macrophages induced expression of proinflammatory cytokines (TNF-α, IL-1β, and IL-6. However, EGCG pretreatment of macrophages significantly inhibited LPS-mediated induction of these cytokines. In addition, EGCG significantly diminished LPS-induced inflammatory cytokines in the peripheral mononuclear blood cells (PBMCs. Supernatant from EGCG-pretreated and LPS-activated macrophage cultures was found to be less cytotoxic to neurons than that from non-EGCG-pretreated and LPS-activated macrophage cultures. Furthermore, EGCG treatment of neurons could inhibit LPS-induced production of reactive oxygen species (ROS. Thus EGCG represents a potent and useful neuroprotective agent for inflammation-mediated neurological disorders.

  19. Phytoconstituents with Radical Scavenging and Cytotoxic Activities from Diospyros shimbaensis

    Directory of Open Access Journals (Sweden)

    Per Aronsson

    2016-01-01

    Full Text Available As part of our search for natural products having antioxidant and anticancer properties, the phytochemical investigation of Diospyros shimbaensis (Ebenaceae, a plant belonging to a genus widely used in East African traditional medicine, was carried out. From its stem and root barks the new naphthoquinone 8,8′-oxo-biplumbagin (1 was isolated along with the known tetralones trans-isoshinanolone (2 and cis-isoshinanolone (3, and the naphthoquinones plumbagin (4 and 3,3′-biplumbagin (5. Compounds 2, 4, and 5 showed cytotoxicity (IC50 520–82.1 μM against MDA-MB-231 breast cancer cells. Moderate to low cytotoxicity was observed for the hexane, dichloromethane, and methanol extracts of the root bark (IC50 16.1, 29.7 and > 100 μg/mL, respectively, and for the methanol extract of the stem bark (IC50 59.6 μg/mL. The radical scavenging activity of the isolated constituents (1–5 was evaluated on the 2,2-diphenyl-1-picrylhydrazyl (DPPH radical scavenging assay. The applicability of the crude extracts and of the isolated constituents for controlling degenerative diseases is discussed.

  20. Cyclotide structure-activity relationships: qualitative and quantitative approaches linking cytotoxic and anthelmintic activity to the clustering of physicochemical forces

    National Research Council Canada - National Science Library

    Park, Sungkyu; Strömstedt, Adam A; Göransson, Ulf

    2014-01-01

    .... Cyclotides exert much of their biological activity via interactions with cell membranes. In this work, we qualitatively and quantitatively analyze the cytotoxic and anthelmintic membrane activities of cyclotides...

  1. Antioxidant, antimicrobial, cytotoxic and analgesic activities of ethanolic extract of Mentha arvensis L.

    Directory of Open Access Journals (Sweden)

    Nripendra Nath Biswas

    2014-10-01

    Conclusions: These results suggest that the ethanolic extract of Mentha arvensis L. has potential antioxidant, antibacterial, cytotoxic and analgesic activities that support the ethnopharmacological uses of this plant.

  2. Cytotoxic activity of marine algae against cancerous cells

    Directory of Open Access Journals (Sweden)

    Élica A. C. Guedes

    2013-09-01

    Full Text Available This paper presents an investigation on the cytotoxic activity in human tumor cell from dichloromethane, chloroform, methanol, ethanol, water extracts, and hexane and chloroform fractions from green, brown and red algae collected at Riacho Doce Beach, north coast of Alagoas, Brazil, against the cancer cells K562 (chronic myelocytic leukemia, HEp-2 (laryngeal epidermoid carcinoma and NCI-H292 (human lung mucoepidermoid carcinoma through the MTT colorimetric method. The dichloromethane extract and chloroform fraction of Hypnea musciformis showed the best cytotoxic activity against K562 (3.8±0.2 µg.mL-1 and 6.4±0.4 µg.mL-1, respectively. Dichloromethane extracts of Dictyota dichotoma (16.3±0.3 µg.mL-1 and the chloroform fraction of H. musciformis (6.0±0.03 µg.mL-1 and chloroform fraction of P. gymnospora (8.2±0.4 were more active against HEp-2 as well as ethanol extracts of P. gymnospora (15.9±2.8 µg.mL-1 and chloroform fraction of H. musciformis (15.0±1.3 µg.mL-1 against the cell NCI-H292. The constituents with higher anticancer action are present in the extracts of dichloromethane and chloroform and in the chloroform fraction of H. musciformis, Digenea simplex, P. gymnospora, and D.dichotoma. In the case of the seaweed S. vulgare, the anticancer constituents are present in the aqueous extract.

  3. Synthesis of geranylhydroquinone derivatives with potencial cytotoxic activity

    Directory of Open Access Journals (Sweden)

    Evelyn Baeza

    2012-01-01

    Full Text Available Natural geranylhydroquinone 1 and geranyl-p-methoxyphenol 2 were prepared by Electrophilic Aromatic Substitution (EAS reactions between geraniol and 1,4-hydroquinone or p-methoxyphenol respectively, using BF3∙Et2O as a catalyst. Furthermore, natural geranylquinone 3, geranyl-1,4-dimethoxyquinone 4 and the new geranyl-4-methoxyphenyl acetate 5 were obtained by chemical transformations of 1 and 2. The compounds were evaluated for their in vitro cytotoxicity activities against cultured human cancer cells of PC-3 human prostate cancer, MCF-7 and MDA-MB-231 breast carcinoma, and Dermal Human Fibroblasts DHF. IC50 values were in the µM range.

  4. Synthesis of geranylhydroquinone derivatives with potential cytotoxic activity

    Energy Technology Data Exchange (ETDEWEB)

    Baeza, Evelyn; Catalan, Karen; Pena-Cortes, Hugo; Espinoza, Luis, E-mail: luis.espinozac@usm.cl [Departamento de Quimica, Universidad Tecnica Federico Santa Maria, Valparaiso (Chile); Villena, Joan [Facultad de Medicina, Universidad de Valparaiso, Centro Regional de Estudios en Alimentos Saludables, Valparaiso (Chile); Carrasco, Hector [Departamento de Ciencias Quimicas, Universidad Andres Bello, Campus Vina del Mar (Chile)

    2012-07-01

    Natural geranylhydroquinone 1 and geranyl-p-methoxyphenol 2 were prepared by Electrophilic Aromatic Substitution (EAS) reactions between geraniol and 1,4-hydroquinone or p-methoxyphenol respectively, using BF{sub 3} {center_dot}Et{sub 2}O as a catalyst. Furthermore, natural geranylquinone 3, geranyl-1,4-dimethoxyquinone 4 and the new geranyl-4-methoxyphenyl acetate 5 were obtained by chemical transformations of 1 and 2. The compounds were evaluated for their in vitro cytotoxicity activities against cultured human cancer cells of PC-3 human prostate cancer, MCF-7 and MDA-MB-231 breast carcinoma, and Dermal Human ibroblasts DHF. IC{sub 50} values were in the {mu}M range. (author)

  5. Sesquiterpene lactones with potent cytotoxic activities from Vernonia chinensis.

    Science.gov (United States)

    Chen, Xin; Zhan, Zha-Jun; Zhang, Xiong-Wen; Ding, Jian; Yue, Jian-Min

    2005-10-01

    Five new sesquiterpene lactones, namely vernchinilides A-E (1-5), along with five known compounds, 8 beta-(2-methylacryloyloxy)hirsutinolide 13-O-acetate (6), 8 alpha-(2-methylacryloyloxy)-1beta,4beta-epoxy-1alpha-methoxy-13-O-acetate-10 betaH-germacra-5 E,7(11)-dien-12,6-olide (7), 8 beta-(2-hydroxymethylacryloyloxy)hirsutinolide 13-O-acetate (8), 8 alpha-tigloyloxyhirsutinolide 13-O-acetate ( 9) and vernolide-B (10) were isolated from Vernonia chinensis. The structures of these new compounds were elucidated on the basis of spectral data, especially 2D-NMR techniques. Compounds 2, 5 and 6 exhibited potent cytotoxic activities against P-388 and A-549 tumor cell lines.

  6. 'Chocolate' silver nanoparticles: Synthesis, antibacterial activity and cytotoxicity.

    Science.gov (United States)

    Chowdhury, Neelika Roy; MacGregor-Ramiasa, Melanie; Zilm, Peter; Majewski, Peter; Vasilev, Krasimir

    2016-11-15

    Silver nanoparticles (AgNPs) have emerged as a powerful weapon against antibiotic resistant microorganisms. However, most conventional AgNPs syntheses require the use of hazardous chemicals and generate toxic organic waste. Hence, in recent year's, plant derived and biomolecule based synthetics have has gained much attention. Cacao has been used for years for its medicinal benefits and contains a powerful reducing agent - oxalic acid. We hypothesized that, due to the presence of oxalic acid, cacao extract is capable of reducing silver nitrate (AgNO3) to produce AgNPs. In this study, AgNPs were synthesized by using natural cacao extract as a reducing and stabilizing agent. The reaction temperature, time and reactant molarity were varied to optimize the synthesis yield. UV-visible spectroscopy (UV-vis), dynamic light scattering (DLS) and transmission electron microscopy (TEM) characterization demonstrated that the synthesized AgNPs were spherical particles ranging in size from 35 to 42.5nm. The synthesized AgNPs showed significant antibacterial activity against clinically relevant pathogens such as Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus and Staphylococcus epidermidis. Importantly, these green AgNPs are not cytotoxic to human dermal fibroblasts (HDFs) at concentrations below 32μg/ml. We conclude that cacao-based synthesis is a reproducible and sustainable method for the generation of stable antimicrobial silver nanoparticles with low cytotoxicity to human cells. The AgNPs synthesized in this work have promising properties for applications in the biomedical field. Copyright © 2016 Elsevier Inc. All rights reserved.

  7. free radical scavenging and cytotoxic activity of standardized extracts

    African Journals Online (AJOL)

    Ledy

    susceptible to polifenoles (Matić et al., 2010). Our results confirm the cytotoxic effect for the red wine extract on. HeLa cells, and it will be interesting to discover the mechanisms involved in the cytotoxic effect. As shown in. Figure 1G, the red wine extract completely destroyed the cell monolayer, and because the method used ...

  8. Pharmacognostic profile and in vitro cytotoxic activity of Adenema ...

    African Journals Online (AJOL)

    The chloroform extract showed potent cytotoxicity against non small cell lung cancer cell, leukemia cell, ovarian cancer cell, prostate cancer cell and breast cancer ... Ethyl acetate extract exhibited potent cytotoxicity against non small cell lung cancer cell, colon, melanoma, renal and breast cancer cell lines with the GI50 of ...

  9. Cytotoxic and free radical scavenging activities of Zingiberaceous rhizomes

    Directory of Open Access Journals (Sweden)

    Niwat Keawpradub

    2005-07-01

    Full Text Available Methanol extracts, water extracts and volatile oils of the fresh rhizomes of Alpinia galanga, Boesenbergia pandurata, Curcuma longa, Kaempferia galanga and Zingiber officinale have been assessed for free radical scavenging activity against 1,1-diphenyl-2-picrylhydrazyl (DPPH radical and cytotoxic activity against MCF7 (breast adenocarcinoma and LS174T (colon adenocarcinoma cell lines. Methanol extract of C. longa exhibited the most pronounced radical scavenging activity with an EC50 value of 9.7 μg/ml, whereas the water extracts and volatile oils showed weak activity. All volatile oils and the methanol extract of C. longa showed strong activity against MCF7 and LS174T with IC50 less than 50 μg/ml. The oils of A. galanga (AGV, B. pandurata (BPV, C. longa (CLV, K. galanga (KGV and Z. officinale (ZOV were analyzed by GC/MS. Trans-3-acetoxy-1,8-cineole, camphor, ar-turmerone, ethyl cinnamate and geranial (E-citral were detected as main compounds in AGV, BPV, CLV, KGV and ZOV, respectively. The novel compound, pcoumaryl- 9-methyl ether, was isolated from methanol extract of A. galanga. ar-Turmerone, curcumin, demethoxycurcumin and bisdemethoxycurcumin were isolated from the methanol extract of C. longa while 6-shogaol, 6-dehydrogingerdione (or 1-dehydrogingerdione and 6-gingerol were isolated from the methanol extract of Z. officinale. Curcumin was the most potent compound for free radical scavenging activity with an EC50 value of 2.0 μg/ml. Demethoxycurcumin was found to be the most active compound against LS174T with an IC50 value of 0.8 μg/ml and 6-shogaol was the most potent compound against MCF7 with an IC50 value of 1.7 μg/ml.

  10. Phenolic compounds from Glycyrrhiza pallidiflora Maxim. and their cytotoxic activity.

    Science.gov (United States)

    Shults, Elvira E; Shakirov, Makhmut M; Pokrovsky, Mikhail A; Petrova, Tatijana N; Pokrovsky, Andrey G; Gorovoy, Petr G

    2017-02-01

    Twenty-one phenolic compounds (1-21) including dihydrocinnamic acid, isoflavonoids, flavonoids, coumestans, pterocarpans, chalcones, isoflavan and isoflaven, were isolated from the roots of Glycyrrhiza pallidiflora Maxim. Phloretinic acid (1), chrysin (6), 9-methoxycoumestan (8), isoglycyrol (9), 6″-O-acetylanonin (19) and 6″-O-acetylwistin (21) were isolated from G. pallidiflora for the first time. Isoflavonoid acetylglycosides 19, 21 might be artefacts that could be produced during the EtOAc fractionation process of whole extract. Compounds 2-4, 10, 11, 19 and 21 were evaluated for their cytotoxic activity with respect to model cancer cell lines (CEM-13, MT-4, U-937) using the conventional MTT assays. Isoflavonoid calycosin (4) showed the best potency against human T-cell leukaemia cells MT-4 (CTD50, 2.9 μM). Pterocarpans medicarpin (10) and homopterocarpin (11) exhibit anticancer activity in micromolar range with selectivity on the human monocyte cells U-937. The isoflavan (3R)-vestitol (16) was highly selective on the lymphoblastoid leukaemia cells CEM-13 and was more active than the drug doxorubicin.

  11. Aloe arborescens Polysaccharides: In Vitro Immunomodulation and Potential Cytotoxic Activity.

    Science.gov (United States)

    Nazeam, Jilan A; Gad, Haidy A; Esmat, Ahmed; El-Hefnawy, Hala M; Singab, Abdel-Naser B

    2017-05-01

    Different polysaccharides were isolated from the leaves of Aloe arborescens using the gradient power of hydrogen followed by antitumor and immunomodulatory assay. The total polysaccharide content of different fractions, water-soluble polysaccharide (WAP), acid-soluble polysaccharide (ACP), and alkaline-soluble polysaccharide (ALP), was estimated using a phenol-sulfuric acid spectrophotometric method. WAP possessed a higher content of mannose and glucose than either ACP or ALP. In vitro antitumor activity was investigated in three different cancer cell lines, and in vitro immunomodulatory potential was assessed through phagocytosis and lymphocyte transformation assay. The results showed that WAP and ALP exhibited the most significant cytotoxicity against HepG2 human liver cancer cells, with IC 50 values of 26.14 and 21.46 μg/mL, respectively. In contrast, ALP was able to enhance lymphocyte transformation, whereas WAP had the most potent phagocytic activity. Molecular weight, total sugar and uronic acid content, Fourier transform-infrared analysis, and linkage type of bioactive polysaccharides were investigated. These findings revealed that the potential antitumor activity of the natural agents WAP and ALP was through an immunomodulation mechanism, which verifies the use of the plant as adjuvant supplement for cancer patients suffering immunosuppression during chemotherapy.

  12. Follicular lymphoma: in vitro effects of combining lymphokine-activated killer (LAK) cell-induced cytotoxicity and rituximab- and obinutuzumab-dependent cellular cytotoxicity (ADCC) activity.

    Science.gov (United States)

    García-Muñoz, Ricardo; López-Díaz-de-Cerio, Ascensión; Feliu, Jesus; Panizo, Angel; Giraldo, Pilar; Rodríguez-Calvillo, Mercedes; Grande, Carlos; Pena, Esther; Olave, Mayte; Panizo, Carlos; Inogés, Susana

    2016-04-01

    Follicular lymphoma (FL) is a disease of paradoxes-incurable but with a long natural history. We hypothesized that a combination of lymphokine-activated killer (LAK) cells and monoclonal antibodies might provide a robust synergistic treatment and tested this hypothesis in a phase II clinical trial (NCT01329354). In this trial, in addition to R-CHOP, we alternated the administration of only rituximab with rituximab and autologous LAK cells that were expanded ex vivo. Our objective was to determine the in vitro capability of LAK cells generated from FL patients to produce cytotoxicity against tumor cell lines and to determine rituximab- and obinutuzumab-induced cytotoxicity via antibody-dependent cellular cytotoxicity (ADCC) activity. We analyzed the LAK cell-induced cytotoxicity and rituximab (R)- and obinutuzumab (GA101)-induced ADCC activity. We show that LAK cells generated from FL patients induce cytotoxicity against tumor cell lines. R and GA101 enhance cytolysis through ADCC activity of LAK cells. Impaired LAK cell cytotoxicity and ADCC activity were detected in 50 % of patients. Percentage of NK cells in LAK infusions were correlated with the R- and GA101-induced ADCC. Our results indicate that the combination of R or GA101 and LAK cells should be an option as frontline maintenance therapy in patients with FL.

  13. Induction of specific cytotoxic T-cell activity against xenogeneic target cells in carp (Cyprinus carpio).

    Science.gov (United States)

    Yamamoto, K; Mukamoto, M; Watarai, S; Kodama, H; Nakayasu, C; Okamoto, N

    2001-04-01

    To investigate the induction of cytotoxic T cells in carp (Cyprinus carpio) after inoculation of fish with 2 xenogeneic line cells and to examine specificity of the cytotoxic activity. 22 carp. Fish were inoculated with mouse myeloma line cells P3.NS-1/1Ag4.1 (NS-1) or chicken Marek's disease tumor-derived lymphoma line cells (MDCC MSB-1). Cytotoxic activity of immune lymphocytes was evaluated by incubating effector cells with homologous and heterologous target cells. Populations of effector cells were identified by blocking T-lymphocytes from effector cells, using anti-carp T-cell monoclonal antibody and complement. Lymphocytes in blood, spleen, and head kidney of carp inoculated with NS-1 cells or MDCC MSB-1 cells had dose-dependent cytotoxic effects against homologous target cells but not against heterologous target cells. Lymphocytes from noninoculated carp did not have cytotoxic effects. Depletion of T-lymphocytes in spleen cells from NS-1-inoculated carp resulted in a decrease of cytotoxic activity against NS-1 cells. Cytotoxic activity of spleen lymphocytes from NS-1-inoculated or noninoculated carp was not evident when cytotoxic tests were performed after addition of anti-NS-1 carp serum. Inoculation with xenogeneic target cells induces a specific cytotoxic T-cell response in carp. Thus, cell-mediated immunity plays a role in defense against infection of parasitic organisms such as protozoa and helminths.

  14. In Vitro Cytotoxic Activity of the Essential Oil Extracted from Artemisia Absinthium

    OpenAIRE

    Mahboubeh Taherkhani

    2014-01-01

    Background: Essential oils are found to have multiple active components which can show in vitro cytotoxic action against various cancerous cell lines. This study reports the in vitro cytotoxic effects of the essential oil from Artemisia absinthium L. (Asteraceae) growing wild in Iran. Methods: Water-distilled essential oil of A. absinthium collected from Ardabil, north-western Iran, was examined for its cytotoxic effects using a modified MTT assay. Air-dried aerial parts of A. absinthium w...

  15. Antibacterial and cytotoxic activity of Brazilian plant extracts - Clusiaceae

    Directory of Open Access Journals (Sweden)

    Ivana B Suffredini

    2006-05-01

    Full Text Available Twelve extracts obtained from nine plants belonging to six different genera of Clusiaceae were analyzed against Gram-negative (Escherichia coli and Pseudomonas aeruginosa and Gram-positive (Staphylococcus aureus and Enterococcus faecalis bacteria using the microdilution broth assay. Tovomita aff. longifolia, T. brasiliensis, Clusia columnaris, Garcinia madruno, Haploclathra paniculata, and Caraipa grandifolia extracts showed significant results against the bacteria. The organic extract obtained from the leaves of T. aff. longifolia showed minimal inhibitory concentration (MIC = 70 µg/ml and minimal bactericidal concentration (MBC = 90 µg/ml against E. faecalis and the organic extract made with the stem of C. columnaris showed MIC = 180 µg/ml and MBC = 270 µg/ml against P. aeruginosa. None of the antibacterial extracts showed lethal activity against brine shrimp nauplii. On the other hand, both aqueous and organic extracts obtained from the aerial organs of Vismia guianensis that were cytotoxic to brine shrimp nauplii did not show a significant antibacterial activity in the assay.

  16. Antioxidant and Cytotoxic Activity of Phyllanthus acidus Fruit Extracts

    Science.gov (United States)

    Andrianto, D.; Widianti, W.; Bintang, M.

    2017-03-01

    Phyllanthus acidus is an Indonesian plant belonging to the Euphorbiaccae family. Extraction of P. acidus was performed using the maceration method. Four-solvent extraction process by ethanol, 70% ethanol, 30% ethanol, and water was used. The antioxidant activity from this extract was determined using 2,2-diphenyl-1-pikrilhidrazil (DPPH) and cytotoxicity (biological potency from this extract) using Brine Shrimp Lethality Test (BSLT) method. We found that the extraction yields of samples ranging from 1.13% to 20.25%. The ethanol extract showed the highest yield, while the lowest yield was reported in the water extract of P. acidus fruit. Among the samples, water extract of P. acidus exhibited high antioxidant activity with IC50 26.06 μg/mL. LC50 values for BSLT ranging from 473.26 to 908.98 μg/mL, with the water extract having the lowest value and therefore the most potent, and the ethanol extract having the highest value

  17. Molecular modelling evaluation of the cytotoxic activity of podophyllotoxin analogues

    Science.gov (United States)

    Afroz Alam, Md.; Naik, Pradeep Kumar

    2009-04-01

    Podophyllotoxin and its structural derivatives, a class of tubulin polymerization inhibitors, have been the objective of numerous studies to prepare better and safer anti-cancer drugs. A library of podophyllotoxin analogues has been designed consisting of 154 analogues. Their molecular interactions and binding affinities with tubulin protein (1SA1) have been studied using the docking-molecular mechanics based on generalized Born/surface area (MM-GBSA) solvation model. Quantitative structure activity relationships were developed between the cytotoxic activity (pIC50) of these compounds and molecular descriptors like docking score and binding free energy. For both the cases the r 2 was in the range of 0.642-0.728 indicating good data fit and r cv 2 was in the range of 0.631-0.719 indicating that the predictive capabilities of the models were acceptable. In addition, a linear correlation was observed between the predicted and experimented pIC50 for the validation data set with correlation coefficient r2 of 0.806 and 0.887, suggesting that the docked structure orientation and the interaction energies are reasonable. Low levels of root mean square error for the majority of inhibitors establish the docking and Prime/MM-GBSA based prediction model as an efficient tool for generating more potent and specific inhibitors of tubulin protein by testing rationally designed lead compounds based on podophyllotoxin derivatization.

  18. Enhancement of human natural cytotoxicity by Plasmodium falciparum antigen activated lymphocytes

    DEFF Research Database (Denmark)

    Theander, T G; Pedersen, B K; Bygbjerg, I C

    1987-01-01

    stimulation enhanced the cytotoxic activity and induced strong proliferative responses in all MNC preparations. The role of NK cells in the protection against malaria is unknown, but they play a role in the protection against virus infection and in the immune surveillance against cancer. Our findings indicate...... cell (NK cell) sensitive cell line, K562, were measured. It was found that SPag stimulation enhanced cytotoxic activity of MNC from donors whose lymphocytes exhibited a strong proliferative response to the antigen. MNC with low proliferative responsiveness showed increased cytotoxic activity if the MNC...... that malaria antigens either directly or through the activation of immunoregulatory cells enhance the NK cell activity....

  19. Antioxidant, cytotoxic and antimicrobial activities of green synthesized silver nanoparticles from crude extract of Bergenia ciliata

    Directory of Open Access Journals (Sweden)

    Abdul-Rehman Phull

    2016-06-01

    Conclusion: Green synthesized BCAgNPs showed enhanced biological activities. Present results also support the advantages of using bio-green method for the production of nanoparticles having the potential of antimicrobial and cytotoxic activities.

  20. l1381nc.m77t - MGD77 data file for Geophysical data from field activity L-13-81-NC in Northern California from 10/09/1981 to 10/23/1981

    Data.gov (United States)

    U.S. Geological Survey, Department of the Interior — Single-beam bathymetry data along with DGPS navigation data was collected as part of field activity L-13-81-NC in Northern California from 10/09/1981 to 10/23/1981,...

  1. l785nc.m77t - MGD77 data file for Geophysical data from field activity l-7-85-nc in Southern Pacific from 12/28/1983 to 01/03/1984

    Data.gov (United States)

    U.S. Geological Survey, Department of the Interior — Single-beam bathymetry data along with transit satellite navigation data was collected as part of field activity L-7-85-NC in Northern California from 09/23/1985 to...

  2. l585nc.m77t - MGD77 data file for Geophysical data from field activity L-5-85-NC in Northern California from 08/10/1985 to 08/31/1985

    Data.gov (United States)

    U.S. Geological Survey, Department of the Interior — Single-beam bathymetry and magnetics data along with DGPS navigation data was collected as part of field activity L-5-85-NC in Northern California from 08/10/1985 to...

  3. Quantitative structure-activity relationship of sesquiterpene lactones with cytotoxic activity.

    Science.gov (United States)

    Scotti, Marcus T; Fernandes, Mariane B; Ferreira, Marcelo J P; Emerenciano, Vicente P

    2007-04-15

    Some sesquiterpene lactones (SLs) are the active compounds of a great number of traditionally medicinal plants from the Asteraceae family and possess considerable cytotoxic activity. Several studies in vitro have shown the inhibitory activity against cells derived from human carcinoma of the nasopharynx (KB). In this study, we investigated a set of 37 different sesquiterpene lactones, represented by 4 skeletons (14 germacranolides, 6 elemanolides, 9 guaianolides and nor-derivatives, and 8 pseudoguaianolides), in what it says respect of their cytotoxic properties. The experimental results were submitted to a QSAR study. A single model for the entire data set was described using 3D molecular descriptors and genetic algorithms establishing structure-activity relationships among the compounds. Important properties for the inhibition potency are discussed for the whole data set and for subsets of the different structural skeletons.

  4. Twisted Amides: From Obscurity to Broadly Useful Transition-Metal-Catalyzed Reactions by N-C Amide Bond Activation.

    Science.gov (United States)

    Liu, Chengwei; Szostak, Michal

    2017-05-29

    The concept of using amide bond distortion to modulate amidic resonance has been known for more than 75 years. Two classic twisted amides (bridged lactams) ingeniously designed and synthesized by Kirby and Stoltz to feature fully perpendicular amide bonds, and as a consequence emanate amino-ketone-like reactivity, are now routinely recognized in all organic chemistry textbooks. However, only recently the use of amide bond twist (distortion) has advanced to the general organic chemistry mainstream enabling a host of highly attractive N-C amide bond cross-coupling reactions of broad synthetic relevance. In this Minireview, we discuss recent progress in this area and present a detailed overview of the prominent role of amide bond destabilization as a driving force in the development of transition-metal-catalyzed cross-coupling reactions by N-C bond activation. © 2017 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim.

  5. Silver nanoparticles: Antibacterial activity against wound isolates & invitro cytotoxic activity on Human Caucasian colon adenocarcinoma

    Directory of Open Access Journals (Sweden)

    J. Saraniya Devi

    2012-05-01

    Full Text Available Objective: To synthesize the silver nanoparticles (AgNPs using the extracts of Hypnea sp. and to investigate the antibacterial activity against Eshcherichia coli, Staphylococcus aureus and invitro cytotoxic activity on HT-29. Methods: In the present study, AgNPs were synthesized using the aqueous extract of marine macro-algae, and were characterized using UV-visible spectroscopy, Fourrier Transform Infra red (FT-IR spectroscopy, X-ray diffraction (XRD analysis and Transmission Electron Microscopy (TEM analysis. Further these synthesized AgNPs were evaluated for their antibacterial activity with the clinical isolates from wound specimens. The isolates were characterized by different tests viz., microscopical observation, colony morphology, biochemical & sugar fermentation tests. The synthesized AgNPs were tested for its antibacterial activity against the isolates by agar well diffussion method. The AgNPs were assessesd for its cytotoxic activity on Human Caucasian colon adenocarcinoma (HT-29 cell lines. Results: In this study, it is clear that the synthesized AgNPs were spherical measuring 10-20nm and was found to be more bactericidal against Gram-negative bacteria (E. coli than Gram-positive bacteria (Staphylococcus aureus isolated from wound specimen. The invitro screening of the AgNPs showed potential cytotoxic activity against the colon cancer cell lines. Conclusions: Proteins can bind to nanoparticles either through the electrostatic attraction of negatively charged carboxylate groups in Hypnea sp. and stabilization of the AgNPs by protein occurs. The antimicrobial activities of AgNPs are influenced by the dimensions of the particles the smaller the particles, the greater antimicrobial effect. The cytotoxic activity may be due to the presence of alkaloids present in the Hypnea sp.

  6. Antiplasmodial activity, cytotoxicity and structure-activity relationship study of cyclopeptide alkaloids

    OpenAIRE

    Emmy Tuenter; Karen Segers; Kyo Bin Kang; Johan Viaene; Sang Hyun Sung; Paul Cos; Louis Maes; Yvan Vander Heyden; Luc Pieters

    2017-01-01

    Abstract: Cyclopeptide alkaloids are polyamidic, macrocyclic compounds, containing a 13-, 14-, or 15-membered ring. The ring system consists of a hydroxystyrylamine moiety, an amino acid, and a β-hydroxy amino acid; attached to the ring is a side chain, comprised of one or two more amino acid moieties. In vitro antiplasmodial activity was shown before for several compounds belonging to this class, and in this paper the antiplasmodial and cytotoxic activities of ten more cyclopeptide alkaloids...

  7. Cytotoxic activity of interferon alpha induced dendritic cells as a biomarker of glioblastoma

    Science.gov (United States)

    Mishinov, S. V.; Stupak, V. V.; Tyrinova, T. V.; Leplina, O. Yu.; Ostanin, A. A.; Chernykh, E. R.

    2016-08-01

    Dendritic cells (DCs) are the most potent antigen presenting cells that can play direct role in anti-tumor immune response as killer cells. DC tumoricidal activity can be stimulated greatly by type I IFN (IFNα and IFNβ). In the present study, we examined cytostatic and cytotoxic activity of monocyte-derived IFNα-induced DCs generated from patients with brain glioma and evaluated the potential use of these parameters in diagnostics of high-grade gliomas. Herein, we demonstrated that patient DCs do not possess the ability to inhibit the growth of tumor HEp-2 cell line but low-grade and high-grade glioma patients do not differ significantly in DC cytostatic activity. However, glioma patient DCs are characterized by reduced cytotoxic activity against HEp-2 cells. The impairment of DC cytotoxic function is observed mainly in glioblastoma patients. The cytotoxic activity of DCs against HEp-2 cells below 9% is an informative marker for glioblastomas.

  8. Enhancement of human natural cytotoxicity by Plasmodium falciparum antigen activated lymphocytes.

    Science.gov (United States)

    Theander, T G; Pedersen, B K; Bygbjerg, I C; Jepsen, S; Larsen, P B; Kharazmi, A

    1987-12-01

    Mononuclear cells (MNC) isolated from malaria immune donors and from donors never exposed to malaria were stimulated in vitro with soluble purified Plasmodium falciparum antigens (SPag) or PPD. After 7 days of culture the proliferative response and the cytotoxic activity against the natural killer cell (NK cell) sensitive cell line, K562, were measured. It was found that SPag stimulation enhanced cytotoxic activity of MNC from donors whose lymphocytes exhibited a strong proliferative response to the antigen. MNC with low proliferative responsiveness showed increased cytotoxic activity if the MNC were preincubated with interleukin 2 (IL-2) for one hour before the start of the cytotoxic assay. SPag activation did not enhance the cytotoxic activity of MNC which did not respond to the antigen in the proliferation assay, and preincubation of these cells with IL-2 did not increase the activity. PPD stimulation enhanced the cytotoxic activity and induced strong proliferative responses in all MNC preparations. The role of NK cells in the protection against malaria is unknown, but they play a role in the protection against virus infection and in the immune surveillance against cancer. Our findings indicate that malaria antigens either directly or through the activation of immunoregulatory cells enhance the NK cell activity.

  9. NcGRA2 as a molecular target to assess the parasiticidal activity of toltrazuril against Neospora caninum.

    Science.gov (United States)

    Strohbusch, M; Müller, N; Hemphill, A; Greif, G; Gottstein, B

    2008-08-01

    The treatment of Neospora caninum infection in the bovine host is still at an experimental stage. In contrast to the in vivo situation, a wide range of compounds have been intensively investigated in cell-culture-based assays. Tools to demonstrate efficacy of treatment have remained conventional including morphological and cell biological criteria. In this work, we present a molecular assay that allows the distinction between live and dead parasites. Live parasites can be detected by measuring the mRNA level of specific genes, making use of the specific mRNA available in live cells. The NcGra2 gene of N. caninum, which is known to be expressed in both tachyzoites and bradyzoites, was used to establish a quantitative real-time RT-PCR, for monitoring parasite viability. Validation of the system in vitro was achieved using Neospora-infected cells that had been treated for 2-20 days with 30 microg/ml toltrazuril. NcGRA2-RT-real time PCR demonstrated that a 10-day toltrazuril-treatment exerted parasitostatic activity, as assessed by the presence of NcGRA2-transcripts, whereas after a 14-day treatment period no NcGRA2-transcripts were detected, showing that the parasites were no longer viable. Concurrently, extended culture for a period of 4 weeks in the absence of the drug following the 14-day toltrazuril treatment did not lead to further parasite proliferation, confirming the parasiticidal effect of the treatment. This assay has the potential to be widely used in the development of novel drugs against N. caninum, with a view to distinguishing between parasiticidal and parasitostatic efficacy of given compounds.

  10. Cytotoxic and antibacterial activity of the mixture of olive oil and lime cream in vitro conditions.

    Science.gov (United States)

    Sumer, Zeynep; Yildirim, Gulay; Sumer, Haldun; Yildirim, Sahin

    2013-01-01

    The mixture of olive oil and lime cream has been traditionally used to treat external burns in the region of Hatay/Antakya and middle Anatolia. Olive oil and lime cream have been employed by many physicians to treat many ailments in the past. A limited number of studies have shown the antibacterial effect of olive oil and that it does not have any toxic effect on the skin. But we did not find any reported studies on the mixture of olive oil and lime cream. The aim of this paper is to investigate the cytotoxic and antibacterial activity of olive oil and lime cream individually or/and in combination in vitro conditions, by using disk-diffusion method and in cell culture. The main purpose in using this mixture is usually to clear burns without a trace. Agar overlay, MTT (Cytotoxicity assay) and antibacterial susceptibility tests were used to investigate the cytotoxic and antibacterial activity of olive oil and lime cream. We found that lime cream has an antibacterial activity but also cytotoxic on the fibroblasts. On the other hand olive oil has limited or no antibacterial effect and it has little or no cytotoxic on the fibroblasts. When we combined lime cream and olive oil, olive oil reduced its cytotoxic impact. These results suggest that mixture of olive oil and lime cream is not cytotoxic and has antimicrobial activity.

  11. Anticancer Constituents and Cytotoxic Activity of Methanol-Water ...

    African Journals Online (AJOL)

    This study was specifically designed to identify anticancer constituents in methanol-water extract of Polygonum bistorta L. and evaluate its cytotoxicity. For this purpose methanol-water (40:60 v/v) extract was subjected to conventional preparative high pressure liquid chromatography and 13 fractions were obtained.

  12. In vitro anticancer activity and cytotoxicity of some papaver alkaloids ...

    African Journals Online (AJOL)

    Materials and Methods: The Vero and HeLa cell lines were treated with various concentrations (1-300 μg/mL) of alkaloids for 48 h. Values for cytotoxicity measured by MTT assay were expressed as the concentration that causes a 50% decrease in cell viability (IC50) (μg/mL). Results: Berberine and macranthine were the ...

  13. Chemical composition, cytotoxicity and antioxidant activities of the ...

    African Journals Online (AJOL)

    The species of the genus Citrus (Rutaceae) have been widely used in traditional medicine. In this study, the essential oil was extracted from the leaves of Citrus aurantium and its cytotoxicity effect on six tumor cell lines and a normal cell line was studied. Furthermore, antioxidant potential of the oil was tested by 2, ...

  14. Cytotoxic activity and apoptotic induction of some edible Thai local ...

    African Journals Online (AJOL)

    Until recently, cancer patients have been treated with combinations of several therapies: chemotherapy, cytotoxic drugs, radiation, and surgical resection. However, these combined treatments, in particular, chemotherapeutic drugs produce significant side effects from which patients often suffer more than the from the cancer ...

  15. Cytotoxic Activity of Hexane Extracts of Psidium Guajava L ...

    African Journals Online (AJOL)

    HP

    Faculty of Pharmacy, University of Benin, ... Purpose: The cytotoxic effects of hexane extracts of Cassia alata and Psidium guajava leaves were ... hexane extracts of C.alata and P. guajava leaves in OV2008 and Kasumi-1 cell lines, respectively. EXPERIMENTAL. Plant material. The P. guajava and C. alata plants were.

  16. Cytotoxic Activity of Hexane Extracts of Psidium guajava L ...

    African Journals Online (AJOL)

    Purpose: The cytotoxic effects of hexane extracts of Cassia alata and Psidium guajava leaves were evaluated in OV2008 ovarian and Kasumi-1 leukemia cancer cell lines, respectively. Methods: The cancer cells were exposed to various concentrations of either C. alata (100 – 180 μg/ml) or P. guajava (100 – 500 μg/ml) leaf ...

  17. In vitro Cytotoxic and Antioxidant Activity of Leaf Extracts of ...

    African Journals Online (AJOL)

    Methods: Four different solvent (hexane, chloroform, ethyl acetate and methanol) leaf extracts of the plant were tested for cytotoxicity against four cancer cells, viz, MCF-7 (oestrogen positive breast cancer cell line), MDA-MB-231 (triple negative breast cancer cell line), SK-BR-3 (breast adenocarcinoma) and ACHN (renal ...

  18. Cytotoxicity and antimicrobial activity of Salvia officinalis L. flowers ...

    African Journals Online (AJOL)

    In this study a comparison of the Cytotoxicity and antimicrobial action of the aqueous and 70% methanol extracts from the flower of the herbal species Salvia officinalis L. (Lamiaceae), originating from Sudan was carried out. Material and Methods: Aqueous, and aquatic methanolic extracts of S. officinalis was investigated for ...

  19. Antioxidant and cytotoxic activities of three different fractions of Lonicera quinquelocularis (Translucent Honeysuckle plant

    Directory of Open Access Journals (Sweden)

    MUHAMMAD IMRAN K.

    2014-08-01

    Full Text Available The cytotoxic and antioxidant activities of a plant count for its effectiveness against various lethal and sever diseases such as cancer, Parkinson Alzheimer and Diabetics etc. Free radicals in the form of reactive oxygen species and reactive nitrogen species may be the main cause of these severe health issues. Medicinal plants with antioxidant and cytotoxic properties have been proved to be the most reliable method of treatment of the mentioned diseases. In the present study antioxidant and cytotoxic potential of three different fractions i.e. ethanol, chloroform and ethyl acetate extracted from Lonicera quinquelocularis (Translucent Honeysuckle plant were tested. The ethanolic and ethyl acetate fraction showed highest scavenging ability than chloroform fraction against DPPH and ABTS free radicals. In cytotoxic assays, chloroform fraction showed highest lethal effects than ethanolic and ethyl acetate fraction. The data obtained from the experimental work revealed that all the three fractions isolated from Lonicera quinquelocularis (Translucent Honeysuckle possess antioxidant and cytotoxic properties. Key Words:

  20. EPR demonstration of iron-nitrosyl complex formation by cytotoxic activated macrophages.

    OpenAIRE

    Lancaster, J R; Hibbs, J B

    1990-01-01

    Activated macrophage cytotoxicity is characterized by loss of intracellular iron and inhibition of certain enzymes that have catalytically active nonheme-iron coordinated to sulfur. This phenomenon involves the oxidation of one of the terminal guanidino nitrogen atoms of L-arginine, which results in the production of citrulline and inorganic nitrogen oxides (NO2-, NO3-, and NO). We report here the results of an electron paramagnetic resonance spectroscopic study performed on cytotoxic activat...

  1. Cytotoxic Activity of Selected Iranian Traditional Medicinal Plants on Colon, Colorectal and Breast Cancer Cell Lines

    Directory of Open Access Journals (Sweden)

    Leila Mohammad Taghizadeh Kashani

    2014-11-01

    Full Text Available Background: Many natural products from plants have been recognized to exert anticancer activity. In this study, ethanolic extracts of selected medicinal herbs from Iranian flora including Alyssum homolocarpum Fisch. (from seeds, Urtica dioica L. (from aerial parts, Cichorium intybus L. (from roots and Solanum nigrum L. (from fruits, were evaluated for their cytotoxic effect on different cell lines.Methods: Cytotoxic effect of these extracts was studied on three different cancer cell lines; colon carcinoma (HT-29, colorectal adenocarcinoma (Caco-2 and breast ductal carcinoma (T47D. In addition, Swiss mouse embryo fibroblasts (NIH 3T3 were used as normal nonmalignant cells. MTT assay (3-(4,5-dimethylthiazol-2-yl-2,5-diphenyltetrazolium bromide was utilized for calculating the cytotoxicity of extracts on cell lines.Results: Results showed the potent cytotoxic activity of U. dioica ethanolic extract against T47D cell line with IC50 value of 46.14±4.55 µg/ml. Other extracts showed poor activity with IC50>100 µg/ml.Conclusions: Cytotoxic activity recorded in the present study revealed high potential antiproliferative activity of U. dioica ethanolic extract against T47D cell line. The real IC50 values of this extract may be considerably lower than the IC50 measured in our study if its pharmacological active compounds become pure. The results emphasize the importance of studies on U. dioica ethanolic extract to characterize potential components as cytotoxic natural medicines.

  2. Predominant involvement of CD8+CD28- lymphocytes in human immunodeficiency virus-specific cytotoxic activity.

    Science.gov (United States)

    Fiorentino, S; Dalod, M; Olive, D; Guillet, J G; Gomard, E

    1996-01-01

    Distinct functional CD8+ T-cell populations have been observed during human immunodeficiency virus (HIV) infection. One of these functions is the inhibition of viral replication by a noncytotoxic mechanism, which was shown to be mediated by the CD8+CD28+ subpopulation. On the other hand, CD8+ T cells exert an HIV-specific cytotoxic activity. The present study shows that CD8+CD28- lymphocytes display this HIV-specific cytotoxic activity, which is detectable immediately after the cells are purified from peripheral blood. The CD28- population is also able to proliferate and to retain its cytotoxic activity after in vitro restimulation with autologous blast cells. Finally, HIV-specific cytotoxic T cells can be obtained in vitro from the CD8+CD28+ population. PMID:8627730

  3. [The significance of cytotoxic activity of maternal lymphocytes for the etiology of intrauterine growth retardation].

    Science.gov (United States)

    Varga, P; Scharl, A; Szekeres-Bartho, J; Bolte, A; Szereday, Z

    1989-01-01

    Natural lymphocyte cytotoxicity of 99 pregnant women delivering intrauterine growth retarded (IUGR) babies was compared to that of 460 women with normal pregnancies. Lymphocytes separated from maternal blood were used as effectors in the in vitro cytotoxicity test using human embryonic fibroblast cells as target. The cytotoxicity test was based on the assessment of endogenous alkaline phosphatase activity of the target cells. A definite shift towards IUGR pregnancies was observed in the distribution of patients when analyzed according to step by step increase of lymphocyte cytotoxicity values. The incidence of increased cytotoxic activity (greater than or equal to 40%) was three times higher in the group of women with IUGR pregnancies than that in the control group. Within the group of women showing increased immunoreactivity during pregnancy the participation of IUGR pregnancies was 40.4%, while only 9.7% of the women with normal cytotoxicity belonged to the IUGR group. Combined analysis of ponderal indices and cytotoxicity values suggests that increased immunoreactivity is associated with a nutritive insufficiency resulting in the disproportionate form of IUGR.

  4. Brine shrimp cytotoxic activities of Hippophae rhamnoides Linn leaves extracts

    Directory of Open Access Journals (Sweden)

    Javid Ali

    2015-04-01

    Full Text Available Objective: To evaluate brine shrimp lethality assay of solvent extracts (aqueous, methanol, ethanol, acetone, ethyl acetate, chloroform and n-hexane of Hippophae rhamnoides (H. rhamnoides leaves. Methods: Brine shrimp cytotoxicity assay was used to assess the cytotoxic potential of H. rhamnoides leaves extracts. Three vials for concentration of each extract were made and 10 shrimps per vial (30 shrimps per dilution were transferred to specific concentration of each extract. Results: The mortality of aqueous extract was 46.7%, methanol extract was 46.7%, ethanolic extract was 50.0%, ethyl acetate was 26.7%, acetone extract was 33.3%, chloroform extract was 40.0% and n-hexane extract was 33.3%. The lowest LD50 was found in methanol extracts (1199.97 µg/mL. Brine shrimp cytotoxicity of tested extracts of H. rhamnoides showed that mortality rate was concentration dependent. Conclusions: It is concluded that bioactive components are present in all leaves extracts of H. rhamnoides, which could be accounted for its pharmacological effects. Thus, the results support the uses of this plant species in traditional medicine.

  5. Structure-activity relationships of novel salicylaldehyde isonicotinoyl hydrazone (SIH) analogs: iron chelation, anti-oxidant and cytotoxic properties

    National Research Council Canada - National Science Library

    Potůčková, Eliška; Hrušková, Kateřina; Bureš, Jan; Kovaříková, Petra; Špirková, Iva A; Pravdíková, Kateřina; Kolbabová, Lucie; Hergeselová, Tereza; Hašková, Pavlína; Jansová, Hana; Macháček, Miloslav; Jirkovská, Anna; Richardson, Vera; Lane, Darius J R; Kalinowski, Danuta S; Richardson, Des R; Vávrová, Kateřina; Šimůnek, Tomáš

    2014-01-01

    ...). Their structure-activity relationships were assessed with respect to their stability in plasma, iron chelation efficacy, redox effects and cytotoxic activity against MCF-7 breast adenocarcinoma cells...

  6. Intestinal intraepithelial lymphocytes exert potent protective cytotoxic activity during an acute virus infection.

    Science.gov (United States)

    Müller, S; Bühler-Jungo, M; Mueller, C

    2000-02-15

    After systemic infection of mice with 104 PFU of lymphocytic choriomeningitis virus (LCMV), infected cells are detected simultaneously in various organs, including spleen and intestinal mucosa. Most notably, virus-infected cells are also present among CD11c+ dendritic cells in the subepithelial area of the small intestinal mucosa. Some of these virus-infected cells are in close spatial association with intestinal intraepithelial lymphocytes (IEL). Therefore, we compared virus-specific cytotoxic activity of CD8 splenocytes with that of IEL subsets. While ex vivo isolated TCRalphabeta+CD8alphaalpha+ IEL exert only minimal virus-specific cytotoxicity, maximum specific killing mediated by TCRalphabeta+CD8alphabeta+ IEL on day 8 postinfection exceeds maximum cytotoxic activity observed with CD8 splenocytes when assessed in vitro. Maximum cytotoxic activity of IEL is preceded by peak perforin and granzyme B mRNA expression in IEL around day 6 postinfection, suggesting a recent activation in situ. The antivirus cytotoxicity of in vivo primed IEL is further demonstrated by the protection from virus production in the spleen of mice infected with LCMV 10 h before adoptive cell transfer. These data indicate a potent priming of LCMV-specific IEL in situ after systemic LCMV infection and suggest that cytotoxic IEL markedly contribute to the elimination of virus-infected cells in the intestinal mucosa.

  7. Structure-activity relationships of novel heteroaryl-acrylonitriles as cytotoxic and antibacterial agents.

    Science.gov (United States)

    Saczewski, Franciszek; Stencel, Agnieszka; Bieńczak, Andrzej M; Langowska, Karolina A; Michaelis, Martin; Werel, Władysław; Hałasa, Rafał; Reszka, Przemyslaw; Bednarski, Patrick J

    2008-09-01

    Eighteen new 2,6-disubstituted acrylonitriles and two new (benzimidazol-1-yl)-acetamide derivatives were prepared and screened for antibacterial and cytotoxic activities on 12 human cancer cell lines. Based on the lead structure 2-(benzimidazol-2-yl)-3-(5-nitrothiophen-2-yl) acrylonitrile it was found that placement of methyl groups at the 5,6 positions of the benzimidazole ring lead to a 3-fold increase in overall cytotoxic activity. Replacing the nitrothiophene for pyridine reduced cytotoxic activity as did replacing the nitro group for a methoxy group. Cytotoxic activity was only slightly reduced when the benzimidazole ring was replaced by a imidazo[4,5-b]pyridine or a benzthiazole ring but replacement by benzoxazole led to a substantial decrease in activity. Moving the acrylonitrile group from position 2 to position 1 of the benzimidazole ring also resulted in moderately active compounds. (Benzimidazol-1-yl)acetamides showed only modest activity. The structure-activity relationships found in the cytotoxicity studies are mirrored in the results of the antibacterial experiments.

  8. In Vitro Cytotoxic Activity of the Essential Oil Extracted from Artemisia Absinthium

    Directory of Open Access Journals (Sweden)

    Mahboubeh Taherkhani

    2014-09-01

    Full Text Available Background: Essential oils are found to have multiple active components which can show in vitro cytotoxic action against various cancerous cell lines. This study reports the in vitro cytotoxic effects of the essential oil from Artemisia absinthium L. (Asteraceae growing wild in Iran. Methods: Water-distilled essential oil of A. absinthium collected from Ardabil, north-western Iran, was examined for its cytotoxic effects using a modified MTT assay. Air-dried aerial parts of A. absinthium was subjected to hydrodistillation using a clevenger-type apparatus. Cytotoxicity of the essential oil was measured against Hela and human healthy peripheral blood cells. Results: The 50% cytotoxic concentrations were found to be 48.59 µg/ml and 5456.07 µg/ml for Hela cells and human lymphocytes, respectively. The volatile oil displayed good cytotoxic action against the human tumor cell line. Conclusion: The IC50 shows that cytotoxicity of the oil against human tumor cell line is much higher than that required for healthy human cells. These results indicate low adverse effects for this oil. The findings of this study necessitate the need for further consideration of this essential oil in anti-neoplastic chemotherapy.

  9. Evaluation of cytotoxicity and gelatinases activity in 3T3 fibroblast cell by root repair materials

    OpenAIRE

    Varol Basak; Tuna Elif Bahar; Karsli Emine; Kasimoglu Yelda; Koruyucu Mine; Seymen Figen; Nurten Rustem

    2016-01-01

    The aim of this study was to investigate the effects of calcium silicate-based products on cytotoxicity in the 3T3 fibroblast and gelatinolytic activity of matrix metalloproteinases (MMPs). 3T3 fibroblasts were incubated directly with Ortho Mineral trioxide aggregate (MTA), BioAggregate, Biodentine, MTA Plus, MTA Angelus and MTA Cerkamed for 24 hours and seven days. The cytotoxicity was determined using an MTT assay. Supernatants were collected to determine MMP-2 and MMP-9. Data were analysed...

  10. A STUDY ON CYTOTOXIC AND ANTHELMINTIC ACTIVITIES OF CRUDE EXTRACTS OF LEAVES OF CLERODENDRUM VISCOSUM

    OpenAIRE

    Islam Md. Shamsul; Moghal Md. Mizanur Rahman; Ahamed Sayed Koushik; Ahmed Jamiuddin; Islam Md. Ariful

    2013-01-01

    This study describes the biological investigations of Clerodendrum viscosum – a plant belonging to the family Verbenaceae. The leaf of Clerodendrum viscosum was extracted with methanol and water. The crude extract of methanol of Clerodendrum viscosum was screened for cytotoxic activity using brine shrimp lethality bioassay. A reputed cytotoxic agent vincristine sulphate was used as a positive control. From the result of the brine shrimp lethality bioassay it can be well predicted that methano...

  11. Listeriolysin o is strongly immunogenic independently of its cytotoxic activity.

    Directory of Open Access Journals (Sweden)

    Javier A Carrero

    Full Text Available The presentation of microbial protein antigens by Major Histocompatibility Complex (MHC molecules is essential for the development of acquired immunity to infections. However, most biochemical studies of antigen processing and presentation deal with a few relatively inert non-microbial model antigens. The bacterial pore-forming toxin listeriolysin O (LLO is paradoxical in that it is cytotoxic at nanomolar concentrations as well as being the source of dominant CD4 and CD8 T cell epitopes following infection with Listeria monocytogenes. Here, we examined the relationship of LLO toxicity to its antigenicity and immunogenicity. LLO offered to antigen presenting cells (APC as a soluble protein, was presented to CD4 T cells at picomolar to femtomolar concentrations- doses 3000-7000-fold lower than free peptide. This presentation required a dose of LLO below the cytotoxic level. Mutations of two key tryptophan residues reduced LLO toxicity by 10-100-fold but had no effect on its presentation to CD4 T cells. Thus there was a clear dissociation between the cytotoxic properties of LLO and its very high antigenicity. Presentation of LLO to CD8 T cells was not as robust as that seen in CD4 T cells, but still occurred in the nanomolar range. APC rapidly bound and internalized LLO, then disrupted endosomal compartments within 4 hours of treatment, allowing endosomal contents to access the cytosol. LLO was also immunogenic after in vivo administration into mice. Our results demonstrate the strength of LLO as an immunogen to both CD4 and CD8 T cells.

  12. Trilobolide-steroid hybrids: Synthesis, cytotoxic and antimycobacterial activity

    Czech Academy of Sciences Publication Activity Database

    Jurášek, M.; Džubák, P.; Rimpelová, S.; Sedlák, David; Konečný, P.; Frydrych, I.; Gurska, S.; Hajdúch, M.; Bogdanová, K.; Kolář, M.; Muller, Tomáš; Kmoníčková, Eva; Ruml, T.; Harmatha, Juraj; Drašar, P. B.

    2017-01-01

    Roč. 117, JAN (2017), s. 97-104 ISSN 0039-128X R&D Projects: GA MŠk(CZ) LO1304; GA MŠk LO1220; GA MŠk LM2015063 Grant - others:GA ČR(CZ) GA14-04329S Institutional support: RVO:68378050 ; RVO:68378041 ; RVO:61388963 Keywords : Trilobolide * Steroids * Click chemistry * Cytotoxicity * sar * Steroid receptor Subject RIV: EB - Genetics ; Molecular Biology; CC - Organic Chemistry (UOCHB-X) Impact factor: 2.282, year: 2016

  13. Chemical and enzymatic reductive activation of acylfulvene to isomeric cytotoxic reactive intermediates.

    Science.gov (United States)

    Pietsch, Kathryn E; Neels, James F; Yu, Xiang; Gong, Jiachang; Sturla, Shana J

    2011-11-21

    Acylfulvenes (AFs), a class of semisynthetic analogues of the sesquiterpene natural product illudin S, are cytotoxic toward cancer cells. The minor structural changes between illudin S and AFs translate to an improved therapeutic window in preclinical cell-based assays and xenograft models. AFs are, therefore, unique tools for addressing the chemical and biochemical basis of cytotoxic selectivity. AFs elicit cytotoxic responses by alkylation of biological targets, including DNA. While AFs are capable of direct alkylation, cytosolic reductive bioactivation to an electrophilic intermediate is correlated with enhanced cytotoxicity. Data obtained in this study illustrate chemical aspects of the process of AF activation. By tracking reaction mechanisms with stable isotope-labeled reagents, enzymatic versus chemical activation pathways for AF were compared for reactions involving the NADPH-dependent enzyme prostaglandin reductase 1 (PTGR1) or sodium borohydride, respectively. These two processes resulted in isomeric products that appear to give rise to similar patterns of DNA modification. The chemically activated isomer has been newly isolated and chemically characterized in this study, including an assessment of its relative stereochemistry and stability at varying pH and under bioassay conditions. In mammalian cancer cells, this chemically activated analogue was shown to not rely on further cellular activation to significantly enhance cytotoxic potency, in contrast to the requirements of AF. On the basis of this study, we anticipate that the chemically activated form of AF will serve as a useful chemical probe for evaluating biomolecular interactions independent of enzyme-mediated activation.

  14. Antioxidant, prooxidant and cytotoxic activity of hydroxylated resveratrol analogues: structure-activity relationship.

    Science.gov (United States)

    Murias, Marek; Jäger, Walter; Handler, Norbert; Erker, Thomas; Horvath, Zsuzsanna; Szekeres, Thomas; Nohl, Hans; Gille, Lars

    2005-03-15

    Resveratrol (trans-3,4',5-trihydroxystilbene), a naturally occurring hydroxystilbene, is considered an essential antioxidative constituent of red wine possessing chemopreventive properties. However, resveratrol and even more its metabolite piceatannol were reported to have also cytostatic activities. In order to find out whether this is related to antioxidative properties of those compounds, we synthesized five other polyhydroxylated resveratrol analogues and studied structure-activity relationships between pro-/antioxidant properties and cytotoxicity. Radical scavenging experiments with O(2)(*-) (5,5-dimethyl-1-pyrroline-N-oxide/electron spin resonance (DMPO/ESR)) and 2,2-diphenyl-1-picrylhydrazyl (DPPH) (photometry) revealed that 3,3',4',5-tetrahydroxystilbene (IC(50): 2.69microM; k(9): 443000M(-1)s(-1)), 3,4,4',5-tetrahydroxystilbene (IC(50): 41.5microM; k(9): 882000M(-1)s(-1)) and 3,3',4,4',5,5'-hexahydroxystilbene (IC(50): 5.02microM), exerted a more than 6600-fold higher antiradical activity than resveratrol and its two other analogues. Furthermore, in HL-60 leukemic cells hydroxystilbenes with ortho-hydroxyl groups exhibited a more than three-fold higher cytostatic activity compared to hydroxystilbenes with other substitution patterns. Oxidation of ortho-hydroxystilbenes in a microsomal model system resulted in the existence of ortho-semiquinones, which were observed by ESR spectroscopy. Further experiments revealed that these intermediates undergo redox-cycling thereby consuming additional oxygen and forming cytotoxic oxygen radicals. In contrast to compounds with other substitution patterns hydroxystilbenes with one or two resorcinol groups (compounds 1 and 3) did not show an additional oxygen consumption or semiquinone formation. These findings suggest that the increased cytotoxicity of ortho-hydroxystilbenes is related to the presence of ortho-semiquinones formed during metabolism or autoxidation.

  15. Synthesis and topoisomerase II inhibitory and cytotoxic activity of oxiranylmethoxy- and thiiranylmethoxy-chalcone derivatives.

    Science.gov (United States)

    Na, Younghwa; Nam, Jung-Min

    2011-01-01

    In order to find potential anticancer drug candidate targeting topoisomerases enzyme, we have designed and synthesized oxiranylmethoxy- and thiiranylmethoxy-retrochalcone derivatives and evaluated their pharmacological activity including topoisomerases inhibitory and cytotoxic activity. Of the compounds prepared compound 25 showed comparable or better cytotoxic activity against cancer cell lines tested. Compound 25 inhibited MCF7 (IC(50): 0.49 ± 0.21 μM) and HCT15 (IC(50): 0.23 ± 0.02 μM) carcinoma cell growth more efficiently than references. In the topoisomerases inhibition test, all the compounds were inactive to topoisomerase I but moderate inhibitors to topoisomerase II enzyme. Especially, compound 25 inhibited topoisomerase II activity with comparable extent to etoposide at 100 μM concentrations. Correlation between cytotoxicity and topoisomerase II inhibitory activity implies that compound 25 can be a possible lead compound for anticancer drug impeding the topoisomerase II function. Copyright © 2010 Elsevier Ltd. All rights reserved.

  16. Cytotoxic active constituents of essential oils of Curcuma longa and Curcuma zanthorrhiza.

    Science.gov (United States)

    Schmidt, Erich; Ryabchenko, Boris; Wanner, Juergen; Jäger, Walter; Jirovetz, Leopold

    2015-01-01

    The polar and apolar fractions of Curcuma longa and C. zanthorriza enriched by ar-turmerone, ar-curcumene and xanthorrizol were screened for cytotoxic activity against the HeLa cell line. Actinomycin D and curcumin were used as reference samples, both known for their cytotoxic properties. Amongst all fractions tested, the xanthorrizol fraction (CC50: 26.1 ± 1.9 μM) showed the strongest cytotoxic properties similar to those of curcumin (CC50: 8.1 ± 1.7 μM). Further studies also revealed that the cytotoxic effects of the extracts and pure compounds are caused by apoptosis induction identified by the cleaved form of PARP protein.

  17. Cytotoxic activities of some mono and bis Mannich bases derived from acetophenone in brine shrimp bioassay.

    Science.gov (United States)

    Gul, Halise Inci; Gul, Mustafa; Hänninen, Osmo

    2002-01-01

    Some mono Mannich bases (1-phenyl-3-amino-1-propanone salts) and bis Mannich bases (1-phenyl-3-amino-2-amino-methyl-1-propanone salts) derived from acetophenone and a few representative quaternary derivatives were synthesised and their cytotoxicity was tested using the brine shrimp bioassay. This assay may serve as an intermediate test before further in vivo animal experiments in large scale, since brine shrimp nauplii as whole organisms were used in this test. Mono Mannich bases were generally more cytotoxic than their corresponding bis Mannich bases. Mannich bases synthesised were cytotoxic in both brine shrimp bioassay in this study and cell culture tests using Jurkat and Renca cells in a previous study. However, the order of the cytotoxic potency of the compounds were reverse, which may result from faster deamination of bis derivatives than optimal level, and different species and test media used in the two test systems. Faster deamination of bis derivatives might have led to elimination of active metabolites before reaching its target. The cytotoxicity of the compounds might have been altered by amino acids and proteins present in cell culture medium but not in sea water used in brine shrimp bioassay affecting their transport through the cell membrane and metabolism in the cell by binding with the compounds. With higher cytotoxic activity compared with 5-fluorouracil (CAS 51-21-8) in brine shrimp bioassay, mono Mannich base 1 and its quaternary derivative 4 and quaternary bis derivative 8 seem to be candidate compounds for further drug design.

  18. Synthesis, evaluation and quantitative structure-activity relationship (QSAR) analysis of Wogonin derivatives as cytotoxic agents.

    Science.gov (United States)

    Bian, Jinlei; Li, Tinghan; Weng, Tianwei; Wang, Jubo; Chen, Yu; Li, Zhiyu

    2017-02-15

    A novel series of 49 wogonin derivatives were synthesized by introducing group at 7-, 8- or B ring of wogonin. The cytotoxic activities against HepG2, A549 and BCG-823 cancer cell lines were also investigated in vitro. Several of them showed obvious cytotoxic activities and compound 3h possessed the highest potency against HepG2, A549, and BCG-823 with IC50 values of 1.07μM, 1.74μM and 0.98μM, respectively. A quantitative structure-activity relationship (QSAR) study of these synthetic derivatives as well as wogonin indicated that high solubility and low octanol/water partition coefficient are favorable, and excessive electrostatic properties and refractivity are unfavorable for the cytotoxic activities of these wogonin derivatives. These findings and results provide a base for further investigations. Copyright © 2017 Elsevier Ltd. All rights reserved.

  19. Pentasaccharide resin glycosides from Ipomoea cairica and their cytotoxic activities.

    Science.gov (United States)

    Yu, Bangwei; Luo, Jianguang; Wang, Junsong; Zhang, Dongming; Yu, Shishan; Kong, Lingyi

    2013-11-01

    Six partially acylated pentasaccharide resin glycosides, cairicosides A-F, were isolated from the aerial parts of Ipomoea cairica. These compounds were characterized as a group of macrolactones of simonic acid A, partially acylated with different organic acids. The lactonization site of 11S-hydroxyhexadecanoic acid (jalapinolic acid) was bound to the second saccharide moiety at C-3 in cairicosides A-E, while at C-2 in cairicoside F. Structures were established by spectroscopic and chemical methods. Compounds cairicosides A-E exhibited moderate cytotoxicity against a small panel of human tumor cell lines with IC50 values in the range of 4.28-14.31μM. Copyright © 2013 Elsevier Ltd. All rights reserved.

  20. Chemodiversity Associated with Cytotoxicity and Antimicrobial Activity of Piper aduncum var. ossanum.

    Science.gov (United States)

    Gutiérrez, Yamilet; Montes, Rodny; Scull, Ramón; Sánchez, Arturo; Cos, Paul; Monzote, Lianet; Setzer, William N

    2016-12-01

    Chemical analysis, antimicrobial activity and cytotoxic effects of essential oils (EOs) from leaves of Piper aduncum var. ossanum from two localities Bauta (EO-B) and Ceiba (EO-C), Artemisa Province, Cuba, were determined. EOs were obtained by hydrodistillation and analyzed by gas chromatography/mass spectrometry. EO-B demonstrated higher activity against S. aureus and L. amazonensis; while a lower cytotoxicity on mammalian cells was observed. Both EOs displayed the same activity against Plasmodium falciparum, Trypanosoma cruzi, Trypanosoma brucei, and Leishmania infantum. Both EOs were inactive against Escherichia coli and Candida albicans. © 2016 Wiley-VHCA AG, Zurich, Switzerland.

  1. Cytotoxic and antifungal activities of melleolide antibiotics follow dissimilar structure-activity relationships.

    Science.gov (United States)

    Bohnert, Markus; Nützmann, Hans-Wilhelm; Schroeckh, Volker; Horn, Fabian; Dahse, Hans-Martin; Brakhage, Axel A; Hoffmeister, Dirk

    2014-09-01

    The fungal genus Armillaria is unique in that it is the only natural source of melleolide antibiotics, i.e., protoilludene alcohols esterified with orsellinic acid or its derivatives. This class of natural products is known to exert antimicrobial and cytotoxic effects. Here, we present a refined relationship between the structure and the antimicrobial activity of the melleolides. Using both agar diffusion and broth dilution assays, we identified the Δ(2,4)-double bond of the protoilludene moiety as a key structural feature for antifungal activity against Aspergillus nidulans, Aspergillus flavus, and Penicillium notatum. These findings contrast former reports on cytotoxic activities and may indicate a different mode of action towards susceptible fungi. We also report the isolation and structure elucidation of five melleolides (6'-dechloroarnamial, 6'-chloromelleolide F, 10-hydroxy-5'-methoxy-6'-chloroarmillane, and 13-deoxyarmellides A and B), along with the finding that treatment with an antifungal melleolide impacts transcription of A. nidulans natural product genes. Copyright © 2014 Elsevier Ltd. All rights reserved.

  2. Caryophyllene-rich essential oil of Didymocarpus tomentosa: chemical composition and cytotoxic activity.

    Science.gov (United States)

    Gowda, Prameela Javarayi; Ramakrishnaiah, Hanumanthaiah; Krishna, Venkatarangaiah; Narra, Sivakrishna; Jagannath, Nataraj

    2012-11-01

    The essential oil from the leaves of Didymocarpus tomentosa was extracted by hydrodistillation and analyzed by GC/FID and GC/MS. Twenty five constituents amounting to 81.6% of the oil were identified. The leaf oil contained 78.7% sesquiterpenes and 2.9% monoterpenes. The leaf essential oil of D. tomentosa is a unique caryophyllene-rich natural source containing beta-caryophyllene, caryophyllene oxide, a-humulene and humulene oxide. The cytotoxic activity of the oil was determined by the BSLT using shrimp larva and the MTT assay using HeLa tumor cell line. The oil showed significant cytotoxic activity with LC50 and IC50 values of 12.26 and 11.4 microg/mL, respectively. This is the first report on the chemical composition and cytotoxic activity of the essential oil of D. tomentosa.

  3. Leishmanicidal, antiplasmodial and cytotoxic activity of indole alkaloids from Corynanthe pachyceras

    DEFF Research Database (Denmark)

    Staerk, D; Lemmich, E; Christensen, J

    2000-01-01

    -NMR resonances by COSY and NOESY experiments. These and related alkaloids showed pronounced activity against Leishmania major promastigotes (IC50 at the micromolar level) but no significant in vitro antiplasmodial activity (against chloroquine-sensitive Plasmodium falciparum). Cytotoxicity assessed with drug...

  4. SCREENING OF ANTIMICROBIAL, CYTOTOXIC AND PESTICIDAL ACTIVITIES OF COCCINIA GRANDIS (L. VOIGT

    Directory of Open Access Journals (Sweden)

    Md. Faruk Hasan

    2016-06-01

    Full Text Available This study was undertaken to assess the antibacterial, antifungal, cytotoxic and pesticidal activities of Coccinia grandis roots extract. The antimicrobial activity was evaluated using disc diffusion method against some pathogenic microorganisms. Cytotoxicity was determined using brine shrimp lethality bioassay method. The plant extract was screened for pesticidal activity towards Sitophilus oryzae adults. Minimum inhibitory concentration (MIC was also studied against test organisms, using serial dilution technique to determine the antibacterial potency. In antibacterial screening, large inhibition zones were observed against the tested gram-positive (Bacillus subtilis, Sarcina lutea and Stapphylococcus aureus and gram-negative (Salmonella typhi and Shigella dysenteriae bacteria. In antifungal screening, the extract showed moderate antifungal activities against the tested fungi (Candida albicans and Colletotrichum falcatum. In cytotoxicity activity test, LC50 (lethal concentration, 50% of the extract against brine shrimp nauplii was 15.00µg/ml. The plant extract also showed moderate pesticidal activities towards S. oryzae adults. These results suggested that the plant extract has significant antibacterial activity against the tested bacteria, moderate antifungal, cytotoxic and pesticidal activity towards the tested fungi, brine shrimp nauplii and S. oryzae adults, respectively.

  5. Human recombinant anti-thyroperoxidase autoantibodies: in vitro cytotoxic activity on papillary thyroid cancer expressing TPO.

    Science.gov (United States)

    Rebuffat, S A; Morin, M; Nguyen, B; Castex, F; Robert, B; Péraldi-Roux, S

    2010-03-02

    Thyroid cancers are difficult to treat due to their limited responsiveness to chemo- and radiotherapy. There is thus a great interest in and a need for alternative therapeutic approaches. We studied the cytotoxic activity of anti-thyroperoxidase autoantibodies (anti-TPO aAbs, expressed in baculovirus/insect cell (B4) and CHO cells (B4') or purified from patients' sera) against a papillary thyroid cancer (NPA) cell line. Anti-TPO aAbs from patients' sera led to a partial destruction of NPA cell line by complement-dependent cytotoxicity (CDC) and antibody-dependent cell-mediated cytotoxicity (ADCC) and exhibited an anti-proliferative activity. Comparison of the cytotoxic activity of anti-TPO aAbs shows that B4' induced an anti-proliferative effect and a better ADCC than B4, but a lower one than anti-TPO aAbs from patients' sera. Antibody-dependent cell-mediated cytotoxicity was increased when human peripheral blood mononuclear cells were used as effector cells, suggesting that FcgammaRs, CD64, CD32 and CD16 are involved. Indeed, anti-TPO aAbs from patients' sera, but not B4 and B4', exhibited CDC activity. These data indicate that anti-TPO aAbs display moderate ADCC and anti-proliferative activities on NPA cells; IgG glycosylation appears to be important for cytotoxic activity and ADCC efficiency depends on FcgammaR-bearing cells. Finally, recombinant human anti-TPO aAbs cannot yet be considered as an optimal tool for the development of a novel therapeutic approach for thyroid cancer.

  6. CYTOTOXIC AND DNA-DAMAGE ACTIVITY OF THE PREBIOTIC SUBSTANCES

    Directory of Open Access Journals (Sweden)

    L. A. Safronova

    2013-12-01

    Full Text Available Due to the widespread of the ecological disorders and diseases of the gastrointestinal tract of humans and animals there is an increased interest in probiotic products (probiotics, prebiotics and synbiotic, which showed its efficacy and safety in their treatment and prevention. Yeast Saccharomyces cerevisiae and cell culture of a human larynx cancer НЕр-2 were used to study cyto- and DNA-damage effects of several polysaccharides (arabinogalactan and nanobiocomposite of arabinogalactan with flavonoids, karraginan, galactomannan and their hydrolyzed derivatives, which are new perspective prebiotic substances. Cytotoxic potential of substances was determined from MTT-assay and DNA-damage effects were determined by morphological and structural features of cell nuclei. The synergic action of the polysaccharides with chemical triggers of cellular damages (hydrogen peroxide, acetic acid, nitrosomethylurea was evaluated. The studied substances possessed no cyto- and DNA-damage action on the yeast and mammalian cells. It was shown that polysaccharides were able to enhance the effects of hydrogen peroxide, acetic acid and nitrosomethylurea. Nature of the marked effects remains unclear, but it may be assumed that the studied prebiotic substances can be used to enhance the effects of some chemical compounds and appear promising for use in integrated biomedical preparations of varied spectrum.

  7. Cytotoxic activity of coumarins from the fruits of Cnidium monnieri on leukemia cell lines.

    Science.gov (United States)

    Yang, Ling-Ling; Wang, Min-Chieh; Chen, Lih-Geeng; Wang, Ching-Chiung

    2003-12-01

    Cnidii monnieri Fructus [CmF; Cnidium monnieri (L.) Cusson] is used as a tonic agent in traditional Chinese medicine. In a previous Chinese herb-cytotoxicity screening test, the ethanol extract of CmF exhibited strong effects on human leukemia (HL-60), cervical carcinoma (HeLa) and colorectal carcinoma (CoLo 205) cells. Then, the CmF extract was subjected to silica gel column chromatography and recrystallization to give five coumarins: osthol, imperatorin, bergapten, isopimpinellin, and xanthotoxin. Among these compounds, osthol showed the strongest cytotoxic activity on tumor cell lines. The structure-activity relationship established from the results indicated that the prenyl group has an important role in the cytotoxic effects. However, imperatorin showed the highest sensitivity to HL-60 cells and the least cytotoxicity to normal PBMCs. Osthol and imperatorin both caused apoptotic bodies, DNA fragmentation, and enhanced PARP degradation in HL-60 cells by biochemical analysis. These results indicate that osthol and imperatorin can induce apoptosis in HL-60 cells. Therefore, osthol and imperatorin are cytotoxic marker substances in the fruits of Cnidium monnieri.

  8. Antioxidant, Antibacterial, and Cytotoxic Activities of the Ethanolic Origanum vulgare Extract and Its Major Constituents

    Directory of Open Access Journals (Sweden)

    John Coccimiglio

    2016-01-01

    Full Text Available Oregano is a perennial shrub that grows in the mountains of the Mediterranean and Euro/Irano-Siberian regions. This study was conducted to identify the major constituents of the ethanolic Origanum vulgare extract and examine the cytotoxic, antioxidant, and antibacterial properties of the extract but more importantly the contribution of its specific major constituent(s or their combination to the overall extract biological activity. Gas chromatography/mass spectroscopy analysis showed that the extract contained monoterpene hydrocarbons and phenolic compounds, the major ones being carvacrol and thymol and to a lesser extent p-cymene, 1-octacosanol, creosol, and phytol. A549 epithelial cells challenged with the extract showed a concentration-dependent increase in cytotoxicity. A combination of thymol and carvacrol at equimolar concentrations to those present in the extract was less cytotoxic. The A549 cells pretreated with nonlethal extract concentrations protected against hydrogen-peroxide-induced cytotoxicity, an antioxidant effect more effective than the combination of equimolar concentrations of thymol/carvacrol. Inclusion of p-cymene and/or 1-octacosanol did not alter the synergistic antioxidant effects of the carvacrol/thymol mixture. The extract also exhibited antimicrobial properties against Gram-positive and Gram-negative bacterial strains including clinical isolates. In conclusion, the oregano extract has cytotoxic, antioxidant, and antibacterial activities mostly attributed to carvacrol and thymol.

  9. Antioxidant, Antibacterial, and Cytotoxic Activities of the Ethanolic Origanum vulgare Extract and Its Major Constituents.

    Science.gov (United States)

    Coccimiglio, John; Alipour, Misagh; Jiang, Zi-Hua; Gottardo, Christine; Suntres, Zacharias

    2016-01-01

    Oregano is a perennial shrub that grows in the mountains of the Mediterranean and Euro/Irano-Siberian regions. This study was conducted to identify the major constituents of the ethanolic Origanum vulgare extract and examine the cytotoxic, antioxidant, and antibacterial properties of the extract but more importantly the contribution of its specific major constituent(s) or their combination to the overall extract biological activity. Gas chromatography/mass spectroscopy analysis showed that the extract contained monoterpene hydrocarbons and phenolic compounds, the major ones being carvacrol and thymol and to a lesser extent p-cymene, 1-octacosanol, creosol, and phytol. A549 epithelial cells challenged with the extract showed a concentration-dependent increase in cytotoxicity. A combination of thymol and carvacrol at equimolar concentrations to those present in the extract was less cytotoxic. The A549 cells pretreated with nonlethal extract concentrations protected against hydrogen-peroxide-induced cytotoxicity, an antioxidant effect more effective than the combination of equimolar concentrations of thymol/carvacrol. Inclusion of p-cymene and/or 1-octacosanol did not alter the synergistic antioxidant effects of the carvacrol/thymol mixture. The extract also exhibited antimicrobial properties against Gram-positive and Gram-negative bacterial strains including clinical isolates. In conclusion, the oregano extract has cytotoxic, antioxidant, and antibacterial activities mostly attributed to carvacrol and thymol.

  10. Antioxidant and cytotoxic activity of Tecoma stans against lung cancer cell line (A549

    Directory of Open Access Journals (Sweden)

    Jayachandran Philip Robinson

    2017-07-01

    Full Text Available ABSTRACT Human have been constantly using plants and plant products to overcome many diseases. The antioxidant property of the plant sources is studied to obtain an efficacious drug against cancer. The objectives of the present study is to evaluate the antioxidant and cytotoxic activity of the Tecoma stans extracts against lung cancer cell line in comparison with vincristine drug. The antioxidant activity was studied using the standard DPPH assay and the cytotoxic activity using MTT assay. DPPH assay results show that methanolic extract of T. stans in higher concentration show better antioxidant potential than the standard L-ascorbic acid. They exhibited strong antioxidant potential at 20 µg/mL concentration. The absorbance at 517 nm showed that in the range of 0.201-0.0203 compared to that of absorbance of ascorbic acid at 0.023.Cytotoxic activity was studied using MTT assay which showed that the increase in concentration of extract increases the cell death. At 100µg/mL concentration there is an increased cytotoxic activity, i.e., 99% of cell inhibition. The results of antioxidant and anticancerous activity may be positively correlated.

  11. In Vitro antibacterial and in Vivo cytotoxic activities of Grewia paniculata

    Directory of Open Access Journals (Sweden)

    Mahmuda Nasrin

    2015-02-01

    Full Text Available Objectives: Grewia paniculata (Family: Malvaceae has been used to treat inflammation, respiratory disorders and fever. It is additionally employed for other health conditions including colds, diarrhea and as an insecticide in Bangladesh. The aim of the present study was to investigate the antibacterial and cytotoxic activities of different extracts of Grewia paniculata. Materials and Methods: The antibacterial activity was evaluated against both gram negative and gram positive bacteria using disc diffusion method by determination of the diameter of zone of inhibition. Cytotoxic activity was performed by brine shrimp (Artemia salina lethality bioassay. Results: In disc diffusion method, all the natural products (400 μg/disc showed moderate to potent activity against all the tested bacteria. The ethanol extract of bark (EEB and ethanol fraction of bark (EFB (400 μg/disc exhibited highest activity against Shigella dysenteriae with a zone of inhibition of 23±1.63 mm and  23±1.77 mm respectively. In the brine shrimp lethality bioassay all the extracts showed moderate cytotoxic activity when compared with the standard drug vincristin sulphate. For example, LC50 value of the ethanol fraction of bark (EFB was 3.01 μg/ml while the LC50 of vincristine sulphate was 0.52 μg/ml. Conclusions: The results suggest that all the natural products possess potent antibacterial and moderate cytotoxic.

  12. Antimicrobial and Cytotoxic Activity of Three Bitter Plants-Enhydra fluctuans, Andrographis Peniculata and Clerodendrum Viscosum.

    Directory of Open Access Journals (Sweden)

    M. Ruhul Amin

    2012-08-01

    Full Text Available Purpose: In this study, three important medicinal plants (Enhydra fluctuans Lour, Clerodendrum viscosum Vent and Andrographis peniculata Wall of Bangladesh were investigated to analyze their antimicrobial and cytotoxic activities against some pathogenic microorganisms and Artemia salina (brine shrimp nauplii. Methods: The coarse powder material of leaves of each plant was extracted separately with methanol and acetone to yield methanol extracts of leaves of Enhydra fluctuans (MLE, Clerodendrum viscosum (MLC and Andrographis peniculata (MLA, and acetone extracts of leaves of Enhydra fluctuans (ALE, Clerodendrum viscosum (ALC and Andrographis peniculata (ALA. The disc diffusion method and the method described by Meyer were used to determine the antimicrobial and cytotoxic activities of each plant extract. Results: Among the test samples, MLE and ALE showed comparatively better antimicrobial activity against a number of bacteria and fungi with inhibition zones in the range of 06-15 mm and according to the intensity of activity, the efficacy against microorganisms were found in the order of Enhydra fluctuans> Andrographi speniculata> Clerodendrum viscosum. In cytotoxicity assay, all samples were found to be active against brine shrimp nauplii (Artemia salina and ALA produced lowest LC50 value (7.03 μg/ml. Conclusion: Enhydra fluctuans and Andrographi speniculata possesses significant antimicrobial and cytotoxic activities.

  13. A novel method for producing target cells and assessing cytotoxic T lymphocyte activity in outbred hosts

    Directory of Open Access Journals (Sweden)

    Bendinelli Mauro

    2009-03-01

    Full Text Available Abstract Background Cytotoxic T lymphocytes play a crucial role in the immunological control of microbial infections and in the design of vaccines and immunotherapies. Measurement of cytotoxic T lymphocyte activity requires that the test antigen is presented by target cells having the same or compatible class I major hystocompatibility complex antigens as the effector cells. Conventional assays use target cells labeled with 51chromium and infer cytotoxic T lymphocyte activity by measuring the isotope released by the target cells lysed following incubation with antigen-specific cytotoxic T lymphocytes. This assay is sensitive but needs manipulation and disposal of hazardous radioactive reagents and provides a bulk estimate of the reporter released, which may be influenced by spontaneous release of the label and other poorly controllable variables. Here we describe a novel method for producing target in outbred hosts and assessing cytotoxic T lymphocyte activity by flow cytometry. Results The method consists of culturing skin fibroblasts, immortalizing them with a replication defective clone of simian virus 40, and finally transducing them with a bicistronic vector encoding the target antigen and the reporter green fluorescent protein. When used in a flow cytometry-based assay, the target cells obtained with this method proved valuable for assessing the viral envelope protein specific cytotoxic T lymphocyte activity in domestic cats acutely or chronically infected with feline immunodeficiency virus, a lentivirus similar to human immunodeficiency virus and used as animal model for AIDS studies. Conclusion Given the versatility of the bicistronic vector used, its ability to deliver multiple and large transgenes in target cells, and its extremely wide cell specificity when pseudotyped with the vesicular stomatitis virus envelope protein, the method is potentially exploitable in many animal species.

  14. Novel hemagglutinating, hemolytic and cytotoxic activities of the intermediate subunit of Entamoeba histolytica lectin.

    Science.gov (United States)

    Kato, Kentaro; Yahata, Kazuhide; Gopal Dhoubhadel, Bhim; Fujii, Yoshito; Tachibana, Hiroshi

    2015-09-10

    Galactose and N-acetyl-D-galactosamine (Gal/GalNAc) inhibitable lectin of Entamoeba histolytica, a common protozoan parasite, has roles in pathogenicity and induction of protective immunity in mouse models of amoebiasis. The lectin consists of heavy (Hgl), light (Lgl), and intermediate (Igl) subunits. Hgl has lectin activity and Lgl does not, but little is known about the activity of Igl. In this study, we assessed various regions of Igl for hemagglutinating activity using recombinant proteins expressed in Escherichia coli. We identified a weak hemagglutinating activity of the protein. Furthermore, we found novel hemolytic and cytotoxic activities of the lectin, which resided in the carboxy-terminal region of the protein. Antibodies against Igl inhibited the hemolytic activity of Entamoeba histolytica trophozoites. This is the first report showing hemagglutinating, hemolytic and cytotoxic activities of an amoebic molecule, Igl.

  15. Cytotoxic, antibacterial and antioxidant activities of extracts of the bark of Melia azedarach (China Berry).

    Science.gov (United States)

    Zahoor, Muhammad; Ahmed, Manzoor; Naz, Sumaira; Ayaz, Musarrat

    2015-01-01

    Nature provides a variety of drugs and medicinal agents derived from plants. This study was conducted to determine antimicrobial, antioxidant and cytotoxic activities of extracts of Melia azedarach bark with methanol/water (9:1 v/v), chloroform, butanol, hexane, water and ethyl acetate. For the determination of the antimicrobial activities, the agar well diffusion method was employed. Cytotoxicity was studied by brine shrimp lethality assay; antioxidant activities were measured using 1,1-diphenyl-2-picrylhydrazyl. The chloroform extract was active against Enterobacter aerogenes and Proteus mirabilis, the ethyl acetate extract had highest antibacterial spectrum against Pseudomonas aeruginosa, the n-hexane extract had highest inhibition against E. aerogenes, the aqueous extract showed highest activities against P. mirabilis, the butanol fraction showed highest activities against E. aerogenes and the methanolic extract was highly active against P. mirabilis.

  16. Antiplasmodial Activity, Cytotoxicity and Structure-Activity Relationship Study of Cyclopeptide Alkaloids

    Directory of Open Access Journals (Sweden)

    Emmy Tuenter

    2017-02-01

    Full Text Available Cyclopeptide alkaloids are polyamidic, macrocyclic compounds, containing a 13-, 14-, or 15-membered ring. The ring system consists of a hydroxystyrylamine moiety, an amino acid, and a β-hydroxy amino acid; attached to the ring is a side chain, comprised of one or two more amino acid moieties. In vitro antiplasmodial activity was shown before for several compounds belonging to this class, and in this paper the antiplasmodial and cytotoxic activities of ten more cyclopeptide alkaloids are reported. Combining these results and the IC50 values that were reported by our group previously, a library consisting of 19 cyclopeptide alkaloids was created. A qualitative SAR (structure-activity relationship study indicated that a 13-membered macrocyclic ring is preferable over a 14-membered one. Furthermore, the presence of a β-hydroxy proline moiety could correlate with higher antiplasmodial activity, and methoxylation (or, to a lesser extent, hydroxylation of the styrylamine moiety could be important for displaying antiplasmodial activity. In addition, QSAR (quantitative structure-activity relationship models were developed, using PLS (partial least squares regression and MLR (multiple linear regression. On the one hand, these models allow for the indication of the most important descriptors (molecular properties responsible for the antiplasmodial activity. Additionally, predictions made for interesting structures did not contradict the expectations raised in the qualitative SAR study.

  17. Antiplasmodial Activity, Cytotoxicity and Structure-Activity Relationship Study of Cyclopeptide Alkaloids.

    Science.gov (United States)

    Tuenter, Emmy; Segers, Karen; Kang, Kyo Bin; Viaene, Johan; Sung, Sang Hyun; Cos, Paul; Maes, Louis; Heyden, Yvan Vander; Pieters, Luc

    2017-02-02

    Cyclopeptide alkaloids are polyamidic, macrocyclic compounds, containing a 13-, 14-, or 15-membered ring. The ring system consists of a hydroxystyrylamine moiety, an amino acid, and a β-hydroxy amino acid; attached to the ring is a side chain, comprised of one or two more amino acid moieties. In vitro antiplasmodial activity was shown before for several compounds belonging to this class, and in this paper the antiplasmodial and cytotoxic activities of ten more cyclopeptide alkaloids are reported. Combining these results and the IC50 values that were reported by our group previously, a library consisting of 19 cyclopeptide alkaloids was created. A qualitative SAR (structure-activity relationship) study indicated that a 13-membered macrocyclic ring is preferable over a 14-membered one. Furthermore, the presence of a β-hydroxy proline moiety could correlate with higher antiplasmodial activity, and methoxylation (or, to a lesser extent, hydroxylation) of the styrylamine moiety could be important for displaying antiplasmodial activity. In addition, QSAR (quantitative structure-activity relationship) models were developed, using PLS (partial least squares regression) and MLR (multiple linear regression). On the one hand, these models allow for the indication of the most important descriptors (molecular properties) responsible for the antiplasmodial activity. Additionally, predictions made for interesting structures did not contradict the expectations raised in the qualitative SAR study.

  18. Thermally-activated delayed fluorescence in Y3N@C80 endohedral fullerene: time resolved luminescence and electron paramagnetic resonance studies.

    Science.gov (United States)

    Zalibera, Michal; Krylov, Denis S; Karagiannis, Dimitrios; Will, Paul-Anton; Ziegs, Frank; Schiemenz, Sandra; Lubitz, Wolfgang; Reineke, Sebastian; Savitsky, Anton; Popov, Alexey Alexandrovich

    2017-11-09

    Endohedral fullerene Y3N@C80 exhibits luminescence with reasonable quantum yield and extraordinary long lifetime. By variable-temperature steady-state and time-resolved luminescence spectroscopy, we demonstrate that above 60 K the Y3N@C80 exhibits thermally-activated delayed fluorescence with maximum emission at 120 K and a negligible prompt fluorescence. Below 60 K, a phosphorescence with a lifetime of 192 ms is observed. Spin distribution and dynamics in the triplet excited state is investigated with X- and W-band EPR and ENDOR spectroscopies and DFT computations. Finally, electroluminescence of the Y3N@C80/PFO film is demonstrated opening the possibility for red-emitting fullerene-based organic light-emitting diodes (OLEDs). © 2017 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

  19. Honatisine, a novel diterpenoid alkaloid, and six known alkaloids from Delphinium honanense and their cytotoxic activity.

    Science.gov (United States)

    He, Yang Qing; Ma, Zhan Ying; Wei, Xiao Mei; Liu, Dong Jie; Du, Bao Zhong; Yao, Bing Hua; Gao, Li Ming

    2011-11-01

    A novel diterpene alkaloid named honatisine (1) has been isolated from the whole plants of Delphinium honanense, along with six known alkaloids, siwanine E (2), isoatisine (3), atisine (4), delcorinine (5), uraphine (6), and nordhagenine A (7). Their structures were deduced on the basis of their spectral data. All of them were evaluated by a SRB assay for their cytotoxicity, and compound 1 showed a significant cytotoxic activity (IC(50) =3.16 μM) against the MCF-7 cell line. Copyright © 2011 Verlag Helvetica Chimica Acta AG, Zürich.

  20. Differential cytotoxic activity of the petroleum ether extract and its furanosesquiterpenoid constituents from Commiphora molmol resin.

    Science.gov (United States)

    Ayyad, Seif-Eldin N; Hoye, Thomas R; Alarif, Walied M; Al Ahmadi, Sana'a M; Basaif, Salim A; Ghandourah, Mohamed A; Badria, Farid A

    2015-01-01

    This study revealed a differential cytotoxic activity of the petroleum ether extract (IC₅₀ =5 μg/mL) of the resinous exudates of Commiphora molmol against two mouse cell lines KA31T and NIH3T3 (untransformed and transformed mouse fibroblasts, respectively). Four new compounds (1-4) and five known compounds (5-9) were isolated from the petroleum ether extract. The identity of these new compounds was determined as γ-elemane lactone (1), 5-αH,8-βH-eudesma-1,3,7(11)-trien-8,12-olide (2), 2-hydroxy-11,12-dihydrofuranodiene (3), and 2-hydroxyfuranodiene (4). 1 and 2 displayed the highest cytotoxic activity against NIH3T3 cells. 7 and 9 exhibited moderate cytotoxic activity against KA31T cells. Compounds 3-6 showed weak cytotoxic activities against both cell lines. These results may explain the high efficacy of the petroleum ether fraction in several myrrh-derived pharmaceutical preparations.

  1. In vitro cytotoxic and in silico activity of piperine isolated from Piper nigrum fruits Linn.

    Science.gov (United States)

    Paarakh, Padmaa M; Sreeram, Dileep Chandra; D, Shruthi S; Ganapathy, Sujan P S

    2015-12-01

    Piper nigrum [Piperaceae], commonly known as black pepper is used as medicine fairly throughout the greater part of India and as a spice globally. To isolate piperine and evaluate in vitro cytotoxic [antiproliferative] activity and in silico method. Piperine was isolated from the fruits of P.nigrum. Piperine was characterized by UV,IR, (1)H-NMR, (13)C-NMR and Mass spectrum. Standardization of piperine was done also by HPTLC fingerprinting. In vitro cytotoxic activity was done using HeLa cell lines by MTT assay at different concentrations ranging from 20 to 100 μg/ml in triplicate and in silico docking studies using enzyme EGFR tyrosine kinase. Fingerprinting of isolated piperine were done by HPTLC method. The IC50 value was found to be 61.94 ± 0.054 μg/ml in in vitro cytotoxic activity in HeLa Cell lines. Piperine was subjected to molecular docking studies for the inhibition of the enzyme EGFR tyrosine kinase, which is one of the targets for inhibition of cancer cells. It has shown -7.6 kJ mol(-1) binding and 7.06 kJ mol(-1) docking energy with two hydrogen bonds. piperine has shown to possess in vitro cytotoxic activity and in silico studies.

  2. Comparison of Cytotoxic Activity in Leukemic Lineages Reveals Important Features of β-Hairpin Antimicrobial Peptides.

    Science.gov (United States)

    Buri, Marcus V; Torquato, Heron F Vieira; Barros, Carlos Castilho; Ide, Jaime S; Miranda, Antonio; Paredes-Gamero, Edgar J

    2017-07-01

    Several reports described different modes of cell death triggered by antimicrobial peptides (AMPs) due to direct effects on membrane disruption, and more recently by apoptosis and necrosis-like patterns. Cytotoxic curves of four β-hairpin AMPs (gomesin, protegrin, tachyplesin, and polyphemusin) were obtained from several human leukemic lineages and normal monocytes and Two cell lines were then selected based on their cytotoxic sensitivity. One was sensitive to AMPs (K562) and the other resistant (KG-1) and their effect compared between these lineages. Thus, these lineages were chosen to further investigate biological features related with their cytotoxicities to AMPs. Stimulation with AMPs produced cell death, with activation of caspase-3, in K562 lineage. Increase on the fluidity of plasmatic membrane by reducing cholesterol potentiated cytotoxicity of AMPs in both lineages. Quantification of internal and external gomesin binding to the cellular membrane of both K562 and KG-1 cells showed that more peptide is accumulated inside of K562 cells. Additionally, evaluation of multi-drug resistant pumps activity showed that KG-1 has more activity than K562 lineage. A comparison of intrinsic gene patterns showed great differences between K562 and KG-1, but stimulation with gomesin promoted few changes in gene expression patterns. Differences in internalization process through the plasma membrane, multidrug resistance pumps activity, and gene expression pattern are important features to AMPs regulated cell death. J. Cell. Biochem. 118: 1764-1773, 2017. © 2016 Wiley Periodicals, Inc. © 2016 Wiley Periodicals, Inc.

  3. Synthesis and In Vitro Cytotoxic Activity of Novel Chalcone-Like Agents

    Directory of Open Access Journals (Sweden)

    Bahram letafat

    2013-11-01

    We described synthesis and cytotoxic activity of poly-functionalized 3-benzylidenechroman-4-ones as new chalcone-like agents. These compounds can be considered as conformationally constrained congeners of chalcones to tolerate the poly-functionalization on the core structures for further optimization.

  4. Cytotoxic and anti-HIV activities of some Tanzanian Garcinia species

    African Journals Online (AJOL)

    lmboera

    In the course of our ongoing search for bioactive extracts/compounds from natural sources, nine Garcinia species growing in Tanzania have been screened for their cytotoxic and anti-HIV-1 viral replication activities. This paper reports the evaluation of crude extracts of nine Garcinia plants against HIV-1 NL4−3 viral strain on ...

  5. Cytotoxic Activity of the Leaf and Stem Extracts of Hibiscus rosa ...

    African Journals Online (AJOL)

    562 cancer cell line. Methods: The crude petroleum ether, ethyl acetate and methanol extracts of the leaf and stem of Hibiscus rosa sinensis were prepared using cold extraction method. The in vitro cytotoxic activity of the extracts (20 - 100 μg/ml) ...

  6. Antioxidant Activity and Cytotoxic Effect of Ventilago denticulata Willd Leaves Extracts.

    Science.gov (United States)

    Pongjanta, Anursara; Pangjit, Kanjana; Srichairatanakool, Somdet

    2016-01-01

    Oxidative stress is characterized by an imbalance between the antioxidant defense systems and the formation of reactive oxygen species (ROS). The excess of ROS can damage biomolecules and leading to several chronic conditions and diseases such as diabetes, antherosclerosis, ischemic injury, inflammation and carcinogenesis. Plant extracts and their constituents as a natural source of antioxidants have been extensively studied. The study aimed to investigate the antioxidant and cytotoxicity of aqueous and ethanolic Rhang Dang (entilago denticulata Willd) leaves extract. The aqueous and ethanolic extracts of Rhang Dang leaves were preliminary analyzed for their phenolic profile (total phenolics and total flavonoids). These extracts were evaluated for their antioxidant properties by different methods such as DPPH radical scavenging andperoxyl radical scavenging activity generated by AAPH (2,2'-Azobis (2-methylpropionamidine) dihydrochloride). Their cytotoxic effects on hepatocellular carcinoma cell line (HepG2) and peripheral blood mononuclear cells (PBMC) were determined by MTT assay. Anti-hemolytic activity was examined using spectrophotometrical method. The ethanolic extract from Rhang Dang leaves exhibited a strong antioxidant activity and prevented hemolysis. It showed the highest amount of phenolics (91.03 ± 12.43 mg of gallic acid equivalents/g extract) and flavonoid compound (69.76 ± 10.84 mg of catechin equivalents/g). Interestingly, this extract was more cytotoxic to HepG2 cells than PBMC. The ethanolic extract from Rhang Dang leaves had strong antioxidant activity and cytotoxic effect on cancer cells.

  7. Antioxidant Activity and Cytotoxicity of the Leaf and Bark Extracts of ...

    African Journals Online (AJOL)

    Purpose: To investigate the antioxidant potential and cytotoxicity of the leaf and bark extracts of Tarchonanathus campharatus.. Methods: The antioxidant activity of the aqueous leaf extract (Aq LF), methanol leaf extract (MET LF), dichloromethane leaf extract (DCM LF), methanol bark extract (MET BK), dichloromethane bark ...

  8. In vitro Cytotoxic Activity of Four Plants Used in Persian Traditional Medicine

    Directory of Open Access Journals (Sweden)

    Fatemeh Zare Shahneh

    2013-08-01

    Full Text Available Purpose: The aim of this study was to investigate in vitro cytotoxic activity of four methanolic crude plant extracts against panel cell lines. Methods: Methanolic extracts were tested for their possible antitumor activity and cytotoxicity using the 3-(4,5-dimetylthiazol-2-yl-2,5- diphenyltetrazolium bromide (MTT assay on six cancer cell lines; non-Hodgkin’s B-cell lymphoma (Raji, human leukemic monocyte lymphoma (U937, human acute myelocytic leukemia (KG-1A, human breast carcinoma (MCF-7 cells, human Prostate Cancer (PC3 and mouse fibrosarcoma (WEHI-164 cell lines and one normal cell line; Human Umbilical Vein Endothelial Cells (HUVEC. Results: All species showed dose dependent inhibition of cell proliferation. IC50 values ranging from 25.66±1.2 to 205.11±1.3 μg/ml. The highest cytotoxic activity Chelidonium majus L> Ferulago Angulata DC> Echinophora platyloba DC> Salvia officinalis L, respectively. Conclusion: all extracts demonstrate promising cytotoxicity activity as a natural resource for future bio-guided fractionation and isolation of potential antitumor agents.

  9. In Vitro and In Vivo Cytotoxicities and Antileishmanial Activities of Thymol and Hemisynthetic Derivatives

    Science.gov (United States)

    Robledo, Sara; Osorio, Edison; Muñoz, Diana; Jaramillo, Luz Marina; Restrepo, Adriana; Arango, Gabriel; Vélez, Iván

    2005-01-01

    The in vitro and in vivo antileishmanial and cytotoxic activities of thymol and structural derivatives in comparison to those of Glucantime were studied. The results showed here suggest that thymol and hemisynthetic derivatives have promising antileishmanial potential and could be considered as new lead structures in the search for novel antileishmanial drugs. PMID:15793164

  10. Phytochemical screening, cytotoxicity and antiviral activity of hexane fraction of Phaleria macrocarpa fruits

    Science.gov (United States)

    Ismaeel, Mahmud Yusef Yusef; Yaacob, Wan Ahmad; Tahir, Mariya Mohd.; Ibrahim, Nazlina

    2015-09-01

    Phaleria macrocarpa fruits have been widely used in the traditional medicine for the treatment of several infections. The current study was done to determine the phytochemical content, cytotoxicity and antiviral activity of the hexane fraction (HF) of P. macrocarpa fruits. In the hexane fraction of P. macarocarpa fruits, phytochemical screening showed the presence of terpenoids whereas saponins, alkaloids, tannins and anthraquinones were not present. Evaluation on Vero cell lines by using MTT assay showed that the 50% cytotoxic concentration (CC50) value was 0.48 mg/mL indicating that the fraction is not cytotoxic. Antiviral properties of the plant extracts were determined by plaque reduction assay. The effective concentration (EC50) was 0.18 mg/mL. Whereas the selective index (SI = CC50/EC50) of hexane fraction is 2.6 indicating low to moderate potential as antiviral agent.

  11. In vitro Antiplasmodial Activity and Cytotoxicity of Vincadifformine and Its Semisynthetic Derivatives

    OpenAIRE

    Mustofa M; Michèle Mallié; Alexis Valentin; Guy Lewin

    2015-01-01

    An indole alkaloid with aspidospemane structure possessing a potential antiplasmodial activity,vincadifformine, has been isolated from Aspidosperma pyrifolium Mart. Moreover, 10 derivatives were preparedfrom the vincadifformine. The study was conducted to evaluate the in vitro antiplasmodial and cytotoxic activity ofthe vincadifformine and their semisynthetic derivatives. The in vitro antiplasmodial activity was evaluated onPlasmodium falciparum chloroquine-resistant (FcM ) and –sensiti...

  12. DETECTION OF BACTERIAL CYTOTOXIC ACTIVITIES FROM WATER-DAMAGED CEILING TILE MATERIAL FOLLOWING INCUBATION ON BLOOD AGAR

    Science.gov (United States)

    Samples of ceiling tiles with high levels of bacteria exhibited cytotoxic activities on a HEP-2 tissue culture assay. Ceiling tiles containing low levels of bacterial colonization did not show cytotoxic activities on the HEP-2 tissue culture assay. Using a spread plate procedure ...

  13. Cytotoxicity of MEIC chemicals Nos. 11-30 in 3T3 mouse fibroblasts with and without microsomal activation

    DEFF Research Database (Denmark)

    Rasmussen, Eva

    1999-01-01

    in other studies on microsomal modulation of the cytotoxicity of the test substances. Moderate to good correlations were found between the cytotoxicity data and rodent lethality data, and the addition of microsomes slightly improved the in vitro/in vivo concordance. The evidence to support the relevance......The cytotoxicity of MEIC chemicals Nos, 11-30 was evaluated by determination of neutral red uptake in Balb/c 3T3 mouse fibroblasts with and without the addition of a microsomal activation mixture. The use of microsomes significantly decreased the cytotoxicity of malathion, 2,4-dichlorophenoxyacetic...... acid, propranolol, thioridazine, lithium sulfate, copper sulfate and thallium sulfate, whereas the cytotoxicity of 1,1,1-trichloroethylene, phenol, nicotine, and paraquat was significantly increased by use of the microsomal activation mixture. These cytotoxicity data are in line with observations...

  14. Comparative antimalarial and cytotoxic activities of two Vernonia ...

    African Journals Online (AJOL)

    ... vitro and in vivo activities and a good therapeutic index than V. cinerea subsp vialis endemic to Madagascar, thus validate scientifically the efficacy and safety of Vernonia amygdalina in the traditional treatment of malaria in Congo DR. Using chemotaxonomic approach, we also detected moderate antiplasmodial activities ...

  15. Alloimmune activation promotes anti-cancer cytotoxicity after rat liver transplantation.

    Directory of Open Access Journals (Sweden)

    Stéphanie Lacotte

    Full Text Available Liver transplantation for hepatocellular carcinoma (HCC results in a specific condition where the immune response is potentially directed against both allogeneic and cancer antigens. We have investigated the level of anti-cancer immunity during allogeneic immune response. Dark Agouti-to-Lewis and Lewis-to-Lewis rat liver transplantations were performed and the recipients anti-cancer immunity was analysed at the time of alloimmune activation. The occurrence of rejection in the allogeneic recipients was confirmed by a shorter survival (p<0.01, increased liver function tests (p<0.01, the presence of signs of rejection on histology, and a donor-specific ex vivo mixed lymphocyte reaction. At the time of alloimmune activation, blood mononuclear cells of the allogeneic group demonstrated increased anti-cancer cytotoxicity (p<0.005, which was related to an increased natural killer (NK cell frequency (p<0.05 and a higher monocyte/macrophage activation level (p<0.01. Similarly, liver NK cell anti-cancer cytotoxicity (p<0.005, and liver monocyte/macrophage activation levels (p<0.01 were also increased. The alloimmune-associated cytotoxicity was mediated through the NKG2D receptor, whose expression was increased in the rejected graft (p<0.05 and on NK cells and monocyte/macrophages. NKG2D ligands were expressed on rat HCC cells, and its inhibition prevented the alloimmune-associated cytotoxicity. Although waiting for in vivo validation, alloimmune-associated cytotoxicity after rat liver transplantation appears to be linked to increased frequencies and levels of activation of NK cells and monocyte/macrophages, and is at least in part mediated through the NKG2D receptor.

  16. Cytotoxic activity of methanolic extract of Mentha longifolia and Ocimum basilicum against human breast cancer.

    Science.gov (United States)

    Al-Ali, Khalil H; El-Beshbishy, Hesham A; El-Badry, Ayman A; Alkhalaf, Moussa

    2013-12-01

    Labiatae family is represented in Saudi Arabia. The aim of the present study was to go insight to investigate the anticancer activity and antioxidative potentials of methanolic extracts of Mentha longifolia L. (ML) and Ocimum basilicum L. (OB) that grown in Madina province, western region, Saudi Arabia. OB exhibited the greater phenolic contents as mg gallic acid equivalent/g weight (mg GAE/g) for a value of 105 +/- 5.5 mg GAE/g. On the other hand, ML produced 29 +/- 3.12 mg GAE/g. The standard antioxidant vitamin E used in this experiment elicited a value of total phenolic contents equal 22 +/- 2.2 mg GAE/g. The percentage scavenging activity of against diphenylpicrylhydrazyl (DPPH) was 850 and 160% for OB and ML extracts, respectively. Vitamin E elicited% scavenging activity of against DPPH equal to 198%. Brine shrimp cytotoxic assay clearly indicated the cytotoxic effects of either ML or OB extract. The brine shrimp survival is inversely proportional to the concentration of either ML or OB extract used with LD50 191.23 and 235.50 ppm, respectively. Toxic effects on brine shrimps indicated the anticancer potential of ML or OB extract. The ML or OB extract was unable to produce pbluescript (pBS) plasmid DNA damage, while the plasmid DNA treated with EcoRI produced a single band as a result of DNA damage. Also, both ML and OB extract exhibited marked cytotoxic activity against MCF-7 cells at various concentrations (20, 40, 80, 160 and 320 microg mL(-1)). The 160 and 320 microg mL(-1) showed more cytotoxic effect against MCF-7 cells. Based on results achieved, we can concluded that, OB and ML extracts have the potency to act as powerful antioxidants and protect against DNA damage and have cytotoxic activity against MCF-7 cell line.

  17. Cytotoxic and Anti-Inflammatory Activities of Garcinia xanthochymus Extracts on Cell Lines

    Directory of Open Access Journals (Sweden)

    Hanisuhana Hamidon

    2016-01-01

    Full Text Available Objective: Garcinia xanthochymus extract has been reported to have several pharmacological properties. This study was conducted to evaluate cytotoxic and anti-inflammatory activities of G. xanthochymus extracts on cell lines. Methods: The roots and stem barks of plant were extracted using maceration method with n-hexane, dichloromethane and methanol, successively. Cytotoxic activity of the extracts was tested against MCF-7 breast adenocarcinoma using MTT assay. Anti-inflammatory study was evaluated using RAW 264.7 mouse macrophage cells. The nitric oxide production in LPS-stimulated cells was measured using Griess reagent. Results: The results of cytotoxic and anti-inflammatory study showed that dichloromethane and n-hexane extracts of root and stem bark exhibited cytotoxic activity in dose-dependent manner. Meanwhile, for anti-inflammatory study, all root extracts together with stem bark dichloromethane and n-hexane extracts reduce NO production in LPS-stimulated cells in dose dependent manner. Conclusions: This finding indicated that G. xanthochymus extracts might become interesting candidate for treatment of cancer and inflammation.

  18. Radical scavenging, antioxidant and cytotoxic activity of Brazilian Caatinga plants.

    Science.gov (United States)

    David, Juceni P; Meira, Marilena; David, Jorge M; Brandão, Hugo N; Branco, Alexsandro; de Fátima Agra, M; Barbosa, M Regina V; de Queiroz, Luciano P; Giulietti, Ana M

    2007-04-01

    Extracts of 32 plants from the Brazilian northeastern semi-arid region called Caatinga were evaluated through DPPH radical scavenging assay, beta-carotene bleaching, and brine shrimp lethality tests (BST). Among the extracts studied Byrsonima cf. gardneriana, Mascagnia coriacea, Cordia globosa, Diodia apiculata and Hypenia salzmannii showed the highest activities in DPPH radical scavenging test. In the beta-carotene bleaching test the highest activities were observed for Passiflora cincinnata, Chamaecrista repens, B. cf. gardneriana, Rollinia leptopetala, Serjania glabrata, Diospyros gaultheriifolia, C. globosa, Mimosa ophtalmocentra, M. coriacea and Lippia cf. microphylla. In contrast, R. leptopetala, Zornia cf. brasiliensis and Leonotis nepetifolia were the most active species in the BST.

  19. Cellular redox status influences both cytotoxic and NF-kappa B activation in natural killer cells.

    Science.gov (United States)

    Valle Blázquez, M; Luque, I; Collantes, E; Aranda, E; Solana, R; Peña, J; Muñoz, E

    1997-01-01

    The role of cellular redox status in both cytotoxic activity and NF-kappa B activation in natural killer (NK) cells was investigated. The results indicate that stimulation of NK cells, either freshly isolated from peripheral blood lymphocytes (PBL) or long-term cultured NK clones, with specific cell targets results in an increased binding activity of NF-kappa B and AP-1 transcription factors measured by gel retardation. Pretreatment of NK cells with the antioxidant pyrrolidine dithiocarbarmate (PDTC) leads to the inhibition of NF-kappa B activation but the AP-1 binding to DNA was superinduced. The inhibition of NF-kappa B by PDTC paralleled with an inhibition of spontaneous cytotoxicity mediated by NK cells. Moreover, the inhibitors of serine proteases, N-alpha-tosyl-L-lysine chloromethyl ketone and N-alpha-tosyl-L-phenylalanine chloromethyl ketone, also blocked the cytolytic activity of NK cells against the sensitive target K562. In contrast, NK activity was not affected by pretreatment of the effector cells with the proteasome inhibitor N-acetyl-leu-leu-norleucinal which selectively inhibits NF-kappa B activation. Altogether, these results support the hypothesis that the activation of NK cells involved transcriptional and post-transcriptional events, and that reactive intermediates may play an important role in the molecular processes related with the generation of a cytotoxic response by NK cells. Images Figure 1 Figure 2 Figure 3 Figure 4 PMID:9155655

  20. Cytotoxicity and antitumoral activity of dichloromethane extract and its fractions from Pothomorphe umbellata

    Directory of Open Access Journals (Sweden)

    J.L. Sacoman

    2008-05-01

    Full Text Available The cytotoxicity of the dichloromethane crude extract (DCE, obtained from the aerial parts of Pothomorphe umbellata (L. Miq (Piperaceae, was evaluated against nine human cancer cell lines (MCF-7, NCI-ADR/RES, OVCAR-3, PC-3, HT-29, NCI-H460, 786-O, UACC-62, K-562. The DCE presented antiproliferative activity with good potency against all cell lines at low concentrations (between 4.0 and 9.5 µg/mL and with selectivity (1.55 µg/mL for the leukemia cell line (K-652. DCE (100, 200, 300 and 400 mg/kg, ip was also evaluated in the Ehrlich ascites tumor model. Both the survival number and the life span of the animals that died increased by at least 45 and 50%, respectively (8 animals per group, demonstrating P. umbellata extract potential anticancer activity. The results of the in vivo antitumor activity prompted the fractionation of the crude extract. The crude extract was submitted to dry column chromatography with dichloromethane-methanol (99:1. The column effluent fractions were extracted with methanol, dried under vacuum yielding fractions FR1 (less polar, FR2 (medium polarity, and FR3 (polar, which were analyzed for their growth inhibition or cytotoxic properties by a 48-h sulforhodamine B cell viability assay by measuring the total protein content. FR1 demonstrated high potency and cytotoxicity, a result compatible with the high toxicity of oxalic acid; FR2, containing 4-nerolidylcathecol, presented the lowest cytotoxic activity compared to the other two fractions but with selectivity for prostate cancer cell line; FR3, containing a mixture of steroids described in the literature as possessing various biological activities, also presented potent anticancer in vitro activity. These results suggest that P. umbellata DCE in vivo antitumor activity may be a consequence of the activity of different active principles.

  1. Annona muricata leaves have strongest cytotoxic activity against breast cancer cells

    Directory of Open Access Journals (Sweden)

    Susi Endrini

    2015-12-01

    Full Text Available BACKGROUND Plant-derived herbal compounds have a long history of clinical use, better patient tolerance and acceptance. They are freely available natural compounds that can be safely used to prevent various ailments. Plants have been the basis of traditional medicine throughout the world for thousands of years and are providing mankind with new remedies. The objective of this study was to determine the cytotoxicity of soursop (Anona muricata Linn leaves and pearl grass (Hedyotis corymbosa (L. Lam. on the hormone-dependent human breast carcinoma Michigan Cancer Foundation-7 (MCF-7 cell line. METHODS This study used two types of solvents (water and ethanol in the extraction process and two incubation times (24 hours and 48 hours in the MTT assays to analyze the cytotoxic effects of both plants. RESULTS Preliminary results showed that the ethanolic extract of soursop leaves (SE displayed cytotoxic effects against MCF-7 on 24- and 48-hour incubation times with IC50 values of 88.788 μg/ml and 14.678 μg/ml, respectively. Ethanolic pearl grass extract (PE showed similar results, with IC50 values of 65.011 μg/ ml on 24-hour incubation time and 52.329 μg/ml on 48-hour incubation time against MCF-7 cell line. However, the water extract of both plants displayed lower cytotoxic effect against MCF-7 cell line. CONCLUSION The ethanolic extract of both plants displayed cytotoxic effect against MCF-7. Soursop (Anona muricata Linn leaves have the strongest cytotoxic activity against MCF-7 breast cancer cell line.

  2. Antiproliferative, Cytotoxic, and Apoptotic Activity of Steroidal Oximes in Cervicouterine Cell Lines

    Directory of Open Access Journals (Sweden)

    Luis Sánchez-Sánchez

    2016-11-01

    Full Text Available Steroidal sapogenins have shown antiproliferative effects against several tumor cell lines; and their effects on human cancer cells are currently under study. Changes in the functionality on the steroidal structure make it possible to modify the biological activity of compounds. Herein, we report the synthesis and in vitro antitumor activity of two steroidal oxime compounds on cervical cancer cells. These derivatives were synthesized from the steroidal sapogenin diosgenin in good yields. The in vitro assays show that the steroidal oximes show significant antiproliferative activity compared to the one observed for diosgenin. Cell proliferation, cell death, and the cytotoxic effects were determined in both cervical cancer cells and human lymphocytes. The cancer cells showed apoptotic morphology and an increased presence of active caspase-3, providing the notion of a death pathway in the cell. Significantly, the steroidal oximes did not exert a cytotoxic effect on lymphocytes.

  3. Design, Synthesis and Cytotoxic Activities of Novel Aliphatic Amino-Substituted Flavonoids

    Directory of Open Access Journals (Sweden)

    Guannan Liu

    2013-11-01

    Full Text Available A series of flavonoids 9a–f, 13b, 13d, 13e and 14a–f bearing diverse aliphatic amino moieties were designed, synthesized and evaluated for their cytotoxic activities against the ECA-109, A-549, HL-60, and PC-3 cancer cell lines. Most of the compounds exhibited moderate to good activities. The structure-activity relationships were studied, revealing that the chalcone skeleton is the most preferable for cytotoxic activities. Chalcone 9d was the most promising compound due to its high potency against the examined cancer cell lines (its IC50 values against ECA-109, A549, HL-60 and PC-3 cells were 1.0, 1.5, 0.96 and 3.9 μM, respectively.

  4. Cytotoxic and antioxidant activity of selected marine sponges

    Directory of Open Access Journals (Sweden)

    Chairman K

    2012-06-01

    Full Text Available Objective: To evaluate the anticancer activity of the crude extracts of Rhabdastrella globostellata (R. globostellata and Spirastrella inconstans (S. inconstans var. moeandrina Dendy. Methods: Soxhlet extraction method was used to extract the secondary metabolites and various assays antioxidant, anticancer and various assays were carried out. The extract were tested anticancer activity against a HeLa, Raw 264.7 and Hek-293. Results: The sponge extracts tested exhibited from median to high toxicity in at least one of the toxicity bioassays performed. The antioxidant activity of the isolated metabolite in ethylacetate solution was assessed by SOD and GTH assays and compared with that of other known natural antioxidants. Conclusions: Potent antioxidants have been detected among both phenolic metabolites and alkaloids. Antioxidant effects of tested compounds have been attributed to their action as chain-breaking antioxidants and/or as scavengers of radicals

  5. Chemical composition of Schinus molle essential oil and its cytotoxic activity on tumour cell lines.

    Science.gov (United States)

    Díaz, Cecilia; Quesada, Silvia; Brenes, Oscar; Aguilar, Gilda; Cicció, José F

    2008-01-01

    The leaf essential oil hydrodistilled from Schinus molle grown in Costa Rica was characterised in terms of its chemical composition, antioxidant activity, ability to induce cytotoxicity and the mechanism of cell death involved in the process. As a result, 42 constituents, accounting for 97.2% of the total oil, were identified. The major constituents of the oil were beta-pinene and alpha-pinene. The antioxidant activity showed an IC(50) of 36.3 microg mL(-1). The essential oil was cytotoxic in several cell lines, showing that it is more effective on breast carcinoma and leukemic cell lines. The LD(50) for cytotoxicity at 48 h in K562 corresponded to 78.7 microg mL(-1), which was very similar to the LD(50) obtained when apoptosis was measured. The essential oil did not induce significant necrosis up to 200 microg mL(-1), which together with the former results indicate that apoptosis is the main mechanism of toxicity induced by S. molle essential oil in this cell line. In conclusion, the essential oil tested was weak antioxidant and induced cytotoxicity in different cell types by a mechanism related to apoptosis. It would be interesting to elucidate the role that different components of the oil play in the effect observed here, since some of them could have potential anti-tumoural effects, either alone or in combination.

  6. Evaluation of anti-inflammatory, antibacterial and cytotoxic activities ...

    African Journals Online (AJOL)

    Anti-inflammatory activity was determined using a LOX-inhibitor screening assay kit according to the manufacturer's instructions. A broth serial micro dilution method was used to determine the minimum inhibitory concentration (MIC) against, Gram-positive and Gram-negative bacteria and Mycobacterium species.

  7. Cytotoxicity and antileishmanial activity of Annona muricata pericarp.

    Science.gov (United States)

    Jaramillo, M C; Arango, G J; González, M C; Robledo, S M; Velez, I D

    2000-04-01

    Hexane, ethyl acetate and methanol extracts of Annona muricata pericarp were tested in vitro against Leishmania braziliensis and L. panamensis promastigotes, and against cell line U-937. The ethyl acetate extract was more active than the other extracts and even of Glucantime used as reference substance. Its fractionation led to the isolation of three acetogenins--annonacin, annonacin A and annomuricin A.

  8. Antimicrobial and cytotoxic activity of Streptomyces sp. from Lonar ...

    African Journals Online (AJOL)

    Antibacterial substances from actinomycetes were isolated from marine environment of Lonar Lake and characterized. Out of the 24 isolates subjected to secondary screening, 12 isolates were active against. Bacillus subtilis, 13 against Staphylococcus aureus, 7 against Escherichia coli, 3 against Proteus vulgaris and 4 ...

  9. Anti-bacterial, free radical scavenging activity and cytotoxicity of ...

    African Journals Online (AJOL)

    2017-09-03

    Sep 3, 2017 ... Quantitative analysis of the scavenging ability showed that acetone extracts exhibited good free radical scavenging activity in a dose-dependent manner. The berries extract had the highest LC50 (lowest toxicity) of 551.68 68 µg/mL. Conclusion: Acetone extract of leaves and roots of Grewia flava contain ...

  10. Antimycobacterial and cytotoxic activities of extracts from fungal ...

    African Journals Online (AJOL)

    10.1007/978-3-662-. 07656-9_7. Jouda JB, Mawabo IK, Notedji A, Mbazoa. CD, Nkenfou J, Wandji J, Nkenfou CN. 2016. Anti-mycobacterial activity of polyketides from Penicillium sp. endophyte isolated from Garcinia nobilis against Mycobacterium ...

  11. Free radical scavenging and cytotoxic activity of five commercial ...

    African Journals Online (AJOL)

    Polygonum cuspidatum), and pomegranate (Punica granatum). It shows radical scavenging activity in the following order, according to their median effective concentration (EC

  12. In vitro Antifungal, Antioxidant and Cytotoxic Activities of a Partially ...

    African Journals Online (AJOL)

    Purpose: To determine the in vitro antifungal and antioxidant activities of the aqueous extract and protein fraction of Atlantia monophylla Linn (Rutaceae) leaf. Methods: Ammonium sulphate (0 – 80 %) precipitation method was used to extract protein from the leaves of A. monophylla Linn (Rutaceae). In vitro antifungal ...

  13. CD107a as a marker of activation in chicken cytotoxic T cells

    DEFF Research Database (Denmark)

    Wattrang, Eva; Dalgaard, Tina Sørensen; Norup, Liselotte Rothmann

    2015-01-01

    The study aimed to evaluate cell surface mobilisation of CD107a as a general activation marker on chicken cytotoxic T cells (CTL). Experiments comprised establishment of an in vitro model for activation-induced CD107a mobilisation and design of a marker panel for the detection of CD107a...... be a useful tool for studies of chicken CTL cytolytic potential both in vivo and in vitro....

  14. Semisynthetic Esters of 17-Hydroxycativic Acid with in Vitro Cytotoxic Activity against Leukemia Cell Lines

    Czech Academy of Sciences Publication Activity Database

    Cavallaro, V.; Řezníčková, Eva; Jorda, Radek; Alza, N.P.; Murray, A.P.; Kryštof, Vladimír

    2017-01-01

    Roč. 40, č. 11 (2017), s. 1923-1928 ISSN 0918-6158 R&D Projects: GA MŠk(CZ) LO1204 Institutional support: RVO:61389030 Keywords : biological evaluation * derivatives * andrographolide * apoptosis * cancer * agents * diterpenes * inhibition * activation * chemistry * diterpenoid * 17-hydroxycativic acid * cytotoxic activity * human cancer cell * apoptosis Subject RIV: EB - Genetics ; Molecular Biology Impact factor: 1.683, year: 2016

  15. Evolutionary Significance of an Algal Gene Encoding an [FeFe]-Hydrogenase with F-Domain Homology and Hydrogenase Activity in Chlorella Variabilis NC64A

    Energy Technology Data Exchange (ETDEWEB)

    Meuser, J. E.; Boyd, E. S.; Ananyev, G.; Karns, D.; Radakovits, R.; Murthy, U. M. N.; Ghirardi, M. L.; Dismukes, G. C.; Peters, J. W.; Posewitz, M. C.

    2011-10-01

    [FeFe]-hydrogenases (HYDA) link the production of molecular H{sub 2} to anaerobic metabolism in many green algae. Similar to Chlamydomonas reinhardtii, Chlorella variabilis NC64A (Trebouxiophyceae, Chlorophyta) exhibits [FeFe]-hydrogenase (HYDA) activity during anoxia. In contrast to C. reinhardtii and other chlorophycean algae, which contain hydrogenases with only the HYDA active site (H-cluster), C. variabilis NC64A is the only known green alga containing HYDA genes encoding accessory FeS cluster-binding domains (F-cluster). cDNA sequencing confirmed the presence of F-cluster HYDA1 mRNA transcripts, and identified deviations from the in silico splicing models. We show that HYDA activity in C. variabilis NC64A is coupled to anoxic photosynthetic electron transport (PSII linked, as well as PSII-independent) and dark fermentation. We also show that the in vivo H{sub 2}-photoproduction activity observed is as O2 sensitive as in C. reinhardtii. The two C. variabilis NC64A HYDA sequences are similar to homologs found in more deeply branching bacteria (Thermotogales), diatoms, and heterotrophic flagellates, suggesting that an F-cluster HYDA is the ancestral enzyme in algae. Phylogenetic analysis indicates that the algal HYDA H-cluster domains are monophyletic, suggesting that they share a common origin, and evolved from a single ancestral F-cluster HYDA. Furthermore, phylogenetic reconstruction indicates that the multiple algal HYDA paralogs are the result of gene duplication events that occurred independently within each algal lineage. Collectively, comparative genomic, physiological, and phylogenetic analyses of the C. variabilis NC64A hydrogenase has provided new insights into the molecular evolution and diversity of algal [FeFe]-hydrogenases.

  16. Sulforaphane composition, cytotoxic and antioxidant activity of crucifer vegetables

    Directory of Open Access Journals (Sweden)

    Mohamed A. Farag

    2010-01-01

    Full Text Available Sulphur compounds in sulphur rich food have been shown to significantly reduce the risk of cancer development. One such compound is sulforaphane (SF, a cancer chemopreventive agent identified in broccoli (F. cruciferae. In this study, SF content was assessed in extracts of several crucifer vegetables including broccoli, brussels sprout, green cabbage, red cabbage, Chinese kale and turnip, in parallel with anticancer and antioxidant activity. Among tested crucifers, cabbage demonstrated a pronounced anticancer effect against A-549 lung cancer cells, with an IC50 value of 38 μg mL−1, and correlated with high SF levels at 540 μg g−1. Except for red cabbage and kale, crucifer extracts displayed moderate to weak activity in scavenging 2,2-diphenyl-1-picrylhydrazyl (DDPH free radicals relative to vitamin E standard.

  17. Soybean Extract Antioxidant Protective Activity Against Copper-Induced Cytotoxicity

    OpenAIRE

    Mansour I. Almansour

    2008-01-01

    The antioxidant activity of soybean crude extract against induced oxidative damage has been achieved through quails Coturnix coturnix treatment with various copper sulphate concentrations alone or with a protective dose of soybean crude extract. Several parameters of oxidative stress together with liver and kidney function tests in serum and liver tissue homogenate were studied. Hematologic indices and liver copper content were determined. Obtained data showed a significant increase in...

  18. Synthesis, Cytotoxic and Antimalarial Activities of Benzoyl Thiosemicarbazone Analogs of Isoquinoline and Related Compounds

    Directory of Open Access Journals (Sweden)

    Somsak Ruchirawat

    2010-02-01

    Full Text Available Thiosemicarbazone analogs of papaveraldine and related compounds 1–6 were synthesized and evaluated for cytotoxic and antimalarial activities. The cytotoxic activity was tested against HuCCA-1, HepG2, A549 and MOLT-3 human cancer cell lines. Thiosemicarbazones 1–5 displayed cytotoxicity toward all the tested cell lines, while compounds 2–5 selectively showed potent activity against the MOLT-3 cell lines. Significantly, N(4-phenyl-2-benzoylpyridine thiosemicarbazone 4 exhibited the most potent activity against HuCCA-1, HepG2, A549 and MOLT-3 cell lines with IC50 values of 0.03, 4.75, 0.04 and 0.004 µg/mL, respectively. In addition, 2-benzoylpyridine thio-semicarbazones 3 and 4 showed antimalarial activity against Plasmodium falciparum with IC50 of 10-7 to < 10-6 M. The study demonstrates the quite promising activity of analog 4 as a lead molecule for further development.

  19. Antimicrobial activity and cytotoxicity of 3 photosensitizers activated with blue light.

    Science.gov (United States)

    Bulit, Florence; Grad, Iwona; Manoil, Daniel; Simon, Stéphane; Wataha, John C; Filieri, Anna; Feki, Anis; Schrenzel, Jacques; Lange, Norbert; Bouillaguet, Serge

    2014-03-01

    Pulp repair is less likely to occur when dentin or pulpal tissue remains infected after caries excavation. Yet there are currently few options to kill residual bacteria without damaging resident cells. The current study has evaluated the effect of 3 blue light-activated chemicals on the viability of lactobacilli, odontoblast-like cells (MDPC-23), undifferentiated pulp cells (OD21), and human embryonic stem cells (hESC H1). Bacteria were incubated for 15 minutes with curcumin, eosin Y, or rose bengal and then irradiated with blue light (240 seconds). Bacteria were labeled with LIVE/DEAD BacLight Bacterial Viability kit, and viability was assessed by fluorescence-activated cell sorting. Cytotoxicity assays were performed on MDPC-23 cells, OD21, and hESC H1 cells grown in 24-well plates and exposed to the same photosensitizer-light combination. After 24 hours, cellular response was measured by using the methyl-thiazol-diphenyl-tetrazolium assay. Results were statistically analyzed by using one-way analysis of variance and Tukey multiple comparison intervals (α = 0.05). Bacterial viability was significantly reduced after exposure to different combinations of light and photosensitizers; mitochondrial activity of cultured cells remained unaffected when exposed to the same conditions, suggesting a good therapeutic index in vitro. Blue light-mediated disinfection is promising for the development of new treatment strategies designed to promote pulp repair after carious exposure. Copyright © 2014 American Association of Endodontists. Published by Elsevier Inc. All rights reserved.

  20. [Studies on coumarins from fruit of Cnidium monnieri and their cytotoxic activities].

    Science.gov (United States)

    Duan, Xu-hong; Zhang, Yu-zhuo; He, Pei; Ma, Zong-min; Pei, Lin

    2015-09-01

    This study is to study is to investigate the coumarins from Fruit of Cnidium monnieri and their cytotoxic activities. The constituents were separated by column chromatography, and their structures were elucidated by spectroscopic data analyses. The isolated compounds were evaluated for their cytoxic activities by MTT method. Eleven compounds were isolated and identified as osthole (1), bergaptan (2), xanthotoxol (3), xanthotoxin (4), imperatorin (5), isopimpinellin (6), osthenol (7), psoralen (8), 5,7-dimethoxycoumarin (9), oxypeucedaninhydrate (10), and swietenocoumarin F (11). Compounds 7, 9-11 were isolated from the Cnidium genus for the first time. Compounds 1,5,10 and 11 showed significant cytotoxic activities against L1210 cell lines at a concentration of 1 x 10(-5) mol x L(-1) with inhibitory rates of were 70.13, 63.10, 55.77, and 75.08% respectively.

  1. Synthesis and Cytotoxic Activity of Some New 2,6-Substituted Purines

    Directory of Open Access Journals (Sweden)

    Nageswara Rao Kode

    2011-07-01

    Full Text Available A seriesof twenty four acyclic unsaturated 2,6-substututed purines 5a-20b were synthesized. These compounds were evaluated for cytotoxic activity against NCI-60 DTP human tumor cell line screen at 10µMconcentration. N9-[(Z-4'-chloro-2'-butenyl-1'-yl]-2,6-dichloropurine(5a, N9-[4'-chloro-2'-butynyl-1'-yl]-2,6-dichloropurine(10a, N9-[(E-2',3'-dibromo-4'-chloro-2'-butenyl-1'-yl]-6-methoxypurine(14and N9-[4'-chloro-2'-butynyl-1'-yl]-6-(4-methoxyphenyl-purine(19exhibited highly potent cytotoxic activity with GI50 values in the 1–5 µM range for most human tumor cell lines. Other compounds exhibited moderate activity.

  2. Cytotoxicity and L-amino acid oxidase activity of crude insect drugs.

    Science.gov (United States)

    Ahn, M Y; Ryu, K S; Lee, Y W; Kim, Y S

    2000-10-01

    The cytotoxicity of crude insect drugs was measured using HeLa cells originating from human cervix and uterine cancer, using the dye uptake assay in order to find potential anticancer agents. Three kinds of extracts (buffer, methanol and ethylacetate) were prepared from 26 insects and used as raw materials for the activity assay. Among these, the buffer extracts from Tabanus, Mylabris and Huechys showed a potent anticancer activity, and those from Catharsius, Red ant, Scorpion, Tabanus and Vespae Nidus showed a strong L-amino acid oxidase (AAO) activity as well as cytotoxicity. In contrast, buffer extracts from Gryllotalpa orientalis and Apriona germari larvae showed greater/more rapid Hela cell growth than that of other insects.

  3. ANTIFUNGAL AND CYTOTOXIC ACTIVITIES OF FIVE TRADITIONALLY USED INDIAN MEDICINAL PLANTS

    Directory of Open Access Journals (Sweden)

    Adhikarimayum Haripyaree

    2013-02-01

    Full Text Available Hexane, Methanol and Distilled water extracts of five Indian Medicinal plants viz., Mimosa pudica L, Vitex trifolia Linn, Leucas aspera Spreng, Centella asiatica (L Urban and Plantago major Linn belonging to different families were subjected to preliminary antimicrobial screening against six standard organisms viz., Ceratocystis paradoxa, Aspergillus niger, Penicillium citrinum, Macrophomina phaseoli, Trichoderma viride and Rhizopus nigricans. To evaluate antifungal activity agar well diffusion method was used. In addition LD50 of the same plant extracts were determined by using Range test on Mus musculus for cytotoxic activity. Methanolic extract of M. pudica showed the highest and significant inhibitory effect against some fungal species. Again, methanolic extract of M. pudica displayed the greatest cytotoxic activity.

  4. Study of the Cytotoxic and Antifungal Activities of Neolignans 8.O.4´ and Structurally Related Compounds

    Directory of Open Access Journals (Sweden)

    P. Matyus

    2000-03-01

    Full Text Available In the present work we report the antifungal and cytotoxic activities of a neolignan 8.O.4´series. The most active antifungal compounds show a significant cytotoxic effect which might be related.

  5. Antimicrobial and cytotoxic activity of red propolis: an alert for its safe use.

    Science.gov (United States)

    Lopez, B G-C; de Lourenço, C C; Alves, D A; Machado, D; Lancellotti, M; Sawaya, A C H F

    2015-09-01

    Red propolis is a resinous product popularly consumed in Brazil as it improves health, and it is considered a nutraceutical. The objective of this study was to test the antimicrobial activity of eight samples of red propolis from Brazil and Cuba to assess the possibility of application of this natural product as an antimicrobial agent, along with a study of its cytotoxic activity against non-tumor cell lines to evaluate at which concentrations it could be safely used. The chemical profile of the samples was evaluated by UHPLC-MS. All the samples presented antimicrobial activity which was tested using agar diffusion and serial dilution methods; and these samples displayed a better activity against most Gram-negative bacteria with minimum inhibitory concentration (MIC) in the range between 6·25 μg ml(-1) and 500 μg ml(-1). However our studies also revealed an inherent cytotoxic effect against HaCaT human keratinocytes and BALBc 3T3. To have a noncytotoxic and safe use of red propolis, it is necessary to use a concentration below the IC50 cytotoxic values. The traditional use of propolis does not necessarily guarantee its safety. The evaluation of the safety of bioactive natural products should always be considered together with the evaluation of the activity. © 2015 The Society for Applied Microbiology.

  6. Synthesis, cytotoxic activity evaluation and HQSAR study of novel isosteviol derivatives as potential anticancer agents.

    Science.gov (United States)

    Liu, Cong-Jun; Yu, Shu-Ling; Liu, Yan-Ping; Dai, Xing-Jie; Wu, Ya; Li, Rui-Jun; Tao, Jing-Chao

    2016-06-10

    A series of novel isosteviol derivatives bearing amino alcohol and thiourea fragments have been stereo-selectively synthesized and screened for their in vitro cytotoxic activities against three human cancer cell lines (HCT-116, HGC-27 and JEKO-1). The results demonstrated that these compounds exhibited prominent cytotoxicities. Especially, the compound Iw displayed the most potent anticancer activities against HCT-116 cell with IC50 value of 1.450 μM. On the basis of this bioassay results, these derivatives were further investigated by the hologram quantitative structure-activity relationship (HQSAR) technique. The optimal HQSAR model with q(2) = 0.663, r(2) = 0.895, SEE = 0.179 was generated using A/B/H/Ch as fragment distinction parameters and 4-7 as fragment size. This model was employed to predict the cytotoxic activities of test set compounds, and the predicted values were in good agreement with the experimental results. The contribution maps derived from the optimal model explained the individual atomic contribution to the total activity of single molecule. Copyright © 2016 Elsevier Masson SAS. All rights reserved.

  7. Study of cytotoxic activity, podophyllotoxin, and deoxypodophyllotoxin content in selected Juniperus species cultivated in Poland.

    Science.gov (United States)

    Och, Marek; Och, Anna; Cieśla, Łukasz; Kubrak, Tomasz; Pecio, Łukasz; Stochmal, Anna; Kocki, Janusz; Bogucka-Kocka, Anna

    2015-06-01

    The demand for podophyllotoxin and deoxypodophyllotoxin is still increasing and commercially exploitable sources are few and one of them, Podophyllum hexandrum Royle (Berberidaceae), is a "critically endangered" species. The first aim was to quantify the amount of podophyllotoxin and deoxypodophyllotoxin in 61 Juniperus (Cupressaceae) samples. Cytotoxic activity of podophyllotoxin and ethanolic leaf extracts of Juniperus scopulorum Sarg. "Blue Pacific" and Juniperus communis L. "Depressa Aurea" was examined against different leukemia cell lines. Ultra-performance liquid chromatography (UPLC) analysis was performed with the use of a Waters ACQUITY UPLC(TM) system (Waters Corp., Milford, MA). The peaks of podophyllotoxin and deoxypodophyllotoxin were assigned on the basis of their retention data and mass-to-charge ratio (m/z). Trypan blue assay was performed to obtain IC50 cytotoxicity values against selected leukemia cell lines. Juniperus scopulorum was characterized with the highest level of podophyllotoxin (486.7 mg/100 g DW) while Juniperus davurica Pall. contained the highest amount of deoxypodophyllotoxin (726.8 mg/100 g DW). Podophyllotoxin IC50 cytotoxicity values against J45.01 and CEM/C1 leukemia cell lines were 0.0040 and 0.0286 µg/mL, respectively. Juniperus scopulorum extract examined against J45.01 and HL-60/MX2 leukemia cell lines gave the respective IC50 values: 0.369-9.225 µg/mL. Juniperus communis extract was characterized with the following IC50 cytotoxity values against J45.01 and U-266B1 cell lines: 3.310-24.825 µg/mL. Juniperus sp. can be considered as an alternative source of podophyllotoxin and deoxypodophyllotoxin. Cytotoxic activity of podophyllotoxin and selected leaf extracts of Juniperus sp. against a set of leukemia cell lines was demonstrated.

  8. In Vitro Screening for Cytotoxic Activity of Herbal Extracts

    Directory of Open Access Journals (Sweden)

    Valter R. M. Lombardi

    2017-01-01

    Full Text Available Experimental studies have shown that a variety of chemopreventive plant components affect tumor initiation, promotion, and progression and the main difference, between botanical medicines and synthetic drugs, resides in the presence of complex metabolite mixtures shown by botanical medicine which in turn exert their action on different levels and via different mechanisms. In the present study, we performed an in vitro screening of ethanol extracts from commercial plants in order to investigate potential antitumor activity against human tumor cell lines. Experimental results obtained through a variety of methods and techniques indicated that extracts of I. verum, G. glabra, R. Frangula, and L. usitatissimum present significant reduction in in vitro tumor cell proliferation, suggesting these extracts as possible chemotherapeutical adjuvants for different cancer treatments.

  9. Cytotoxic Activities against Breast Cancer Cells of Local Justicia gendarussa Crude Extracts.

    Science.gov (United States)

    Ayob, Zahidah; Mohd Bohari, Siti Pauliena; Abd Samad, Azman; Jamil, Shajarahtunnur

    2014-01-01

    Justicia gendarussa methanolic leaf extracts from five different locations in the Southern region of Peninsular Malaysia and two flavonoids, kaempferol and naringenin, were tested for cytotoxic activity. Kaempferol and naringenin were two flavonoids detected in leaf extracts using gas chromatography-flame ionization detection (GC-FID). The results indicated that highest concentrations of kaempferol and naringenin were detected in leaves extracted from Mersing with 1591.80 mg/kg and 444.35 mg/kg, respectively. Positive correlations were observed between kaempferol and naringenin concentrations in all leaf extracts analysed with the Pearson method. The effects of kaempferol and naringenin from leaf extracts were examined on breast cancer cell lines (MDA-MB-231 and MDA-MB-468) using MTT assay. Leaf extract from Mersing showed high cytotoxicity against MDA-MB-468 and MDA-MB-231 with IC50 values of 23 μg/mL and 40 μg/mL, respectively, compared to other leaf extracts. Kaempferol possessed high cytotoxicity against MDA-MB-468 and MDA-MB-231 with IC50 values of 23 μg/mL and 34 μg/mL, respectively. These findings suggest that the presence of kaempferol in Mersing leaf extract contributed to high cytotoxicity of both MDA-MB-231 and MDA-MB-468 cancer cell lines.

  10. Evaluation of cytotoxicity and gelatinases activity in 3T3 fibroblast cell by root repair materials

    Directory of Open Access Journals (Sweden)

    Varol Basak

    2016-09-01

    Full Text Available The aim of this study was to investigate the effects of calcium silicate-based products on cytotoxicity in the 3T3 fibroblast and gelatinolytic activity of matrix metalloproteinases (MMPs. 3T3 fibroblasts were incubated directly with Ortho Mineral trioxide aggregate (MTA, BioAggregate, Biodentine, MTA Plus, MTA Angelus and MTA Cerkamed for 24 hours and seven days. The cytotoxicity was determined using an MTT assay. Supernatants were collected to determine MMP-2 and MMP-9. Data were analysed using IBM SPSS 22. Seventh day extracts of Ortho MTA and Biodentine showed reduced cell viability. Specific characterization of MMPs in cell culture demonstrated that MMP-2 (62 kPa in the cell culture supernatants by gelatin zymography showed induced expression in four out of seven groups by 3T3 cells. No MMP-9 expression was observed. The cytotoxicity of materials revealed a significant difference in cell viability between the groups on the first and seventh days. The results of this study revealed minor cytotoxic effects for Ortho MTA and Biodentine. This study suggests that endodontic sealers induced production of MMP-2. MMP-9 might be expressed in small amounts when compared with MMP-2.

  11. Antiviral and Cytotoxic Activities of Extracts from the Cell Cultures and Respective Parts of Some Turkish Medicinal Plants

    OpenAIRE

    SÖKMEN, ATALAY

    2001-01-01

    Extracts from respective parts and cell cultures of some Turkish medicinal plants have been assessed for their antiviral and cytotoxic properties. None of the extracts tested showed notable activity against herpes simplex viruses (HSV-I and II), but a slight antiretroviral activity against HIV-I was determined in an extract from Hypericum capitatum cell cultures. On the other hand, according to cytotoxic activity test results against brine shrimp (Artemia salina), an activity level of LD50 a...

  12. Cytotoxicity and Radiosensitising Activity of Synthesized Dinitrophenyl Derivatives of 5-Fluorouracil

    Directory of Open Access Journals (Sweden)

    Khosrou Abdi

    2012-07-01

    Full Text Available Background and the purpose of the study: Dual functional agents in which nitroaromatic or nitroheterocyclic compounds are attached through a linker unit to mustards and aziridines have shown higher cytotoxicities than the corresponding counterparts to both aerobic and hypoxic cells and enhanced radiosensitizing activity. In thepresent investigation cytotoxicity and radiosensitizing activity of 2,4-dinitrobenzyl, 2,4-dinitrobenzoyl, and 2,4-dinitrophenacetyl derivatives of 5-fluorouracil which was assumed to release cytotoxic active quinone methidide,and 5-fluorouracil under hypoxic conditions on HT-29 cell line under both aerobic and hypoxic conditions wasinvestigated.Methods: 5-fluorouracil derivative X-XIII were prepared by the reaction of the corresponding di-nitro substitutedbenzyl, benzoyl and phenacetyl halides with 5-fluorouracil protected at N-1 with di-t-butoxydicarbonate (BOC in dimethyl formamide (DMF in the presence of the potassium carbonate followed by hydrolysis of the blocking,group by potassium carbonate in methanol. Cytotoxicity of fluorouracil VIII and tested compounds X-XIII against HT-29cell line under both aerobic and hypoxic conditions after 48 hrs incubation were measured by determination of the percent of the survival cells using 3-(4,5-Dimethylthiazol-2-yl-2,5-diphenyltetrazolium bromide (MTT assay and percent of the dead cells using propidium iodide(PI-digitonine assay and results were used to calculate the corresponding IC50 values. Radiosensitization experiments were carried out by irradiation of the incubations with a 60Co source and clonogenic assay was performed to determine the cell viabilities following treatment with the tested compounds and/or radiation. Sensitization Enhancement Ratio (SER of each tested compound was obtained from the radiation survival curves in the absence and presence of each sensitizer for 37% survival respectively.Results and major conclusion: Findings of the present study showed that

  13. Cytotoxicity and radiosensitising activity of synthesized dinitrophenyl derivatives of 5-fluorouracil

    Directory of Open Access Journals (Sweden)

    Khoshayand Mohammad

    2012-07-01

    Full Text Available Abstract Background and the purpose of the study Dual functional agents in which nitroaromatic or nitroheterocyclic compounds are attached through a linker unit to mustards and aziridines have shown higher cytotoxicities than the corresponding counterparts to both aerobic and hypoxic cells and enhanced radiosensitizing activity. In the present investigation cytotoxicity and radiosensitizing activity of 2,4-dinitrobenzyl, 2,4-dinitrobenzoyl, and 2,4-dinitrophenacetyl derivatives of 5-fluorouracil which was assumed to release cytotoxic active quinone methidide and 5-fluorouracil under hypoxic conditions on HT-29 cell line under both aerobic and hypoxic conditions was investigated. Methods 5-fluorouracil derivative X-XIII were prepared by the reaction of the corresponding di-nitro substituted benzyl, benzoyl and phenacetyl halides with 5-fluorouracil protected at N-1 with di-t-butoxydicarbonate (BOC in dimethyl formamide (DMF in the presence of the potassium carbonate followed by hydrolysis of the blocking group by potassium carbonate in methanol. Cytotoxicity of fluorouracil VIII and tested compounds X-XIII against HT-29 cell line under both aerobic and hypoxic conditions after 48 hrs incubation were measured by determination of the percent of the survival cells using 3-(4,5-Dimethylthiazol-2-yl-2,5-diphenyltetrazolium bromide (MTT assay and percent of the dead cells using propidium iodide(PI-digitonine assay and results were used to calculate the corresponding IC50 values. Radiosensitization experiments were carried out by irradiation of the incubations with a 60Co source and clonogenic assay was performed to determine the cell viabilities following treatment with the tested compounds and/or radiation. Sensitization Enhancement Ratio (SER of each tested compound was obtained from the radiation survival curves in the absence and presence of each sensitizer for 37% survival respectively. Results and major conclusion Findings of the present study

  14. Cytotoxic and cytoprotective activities of curcumin. Effects on paracetamol-induced cytotoxicity, lipid peroxidation and glutathione depletion in rat hepatocytes

    NARCIS (Netherlands)

    Donatus, I A; Sardjoko,; Vermeulen, N P

    1990-01-01

    The cytoprotective effect of curcumin, a natural constituent of Curcuma longa, on the cytotoxicity of paracetamol in rat hepatocytes was studied. Paracetamol was selected as a model-toxin, since it is known to be bioactivated by 3-methylcholanthrene inducible cytochromes P450 presumably to

  15. Glucosinolates profile, volatile constituents, antimicrobial, and cytotoxic activities of Lobularia libyca.

    Science.gov (United States)

    Al-Gendy, Amal A; Nematallah, Khaled A; Zaghloul, Soumaya S; Ayoub, Nahla A

    2016-12-01

    Brassicaceae plants are associated with protection against cancers due to their glucosinolate contents. We investigate fresh leaves, roots and ripe seeds of Lobularia libyca (Viv.) C.F.W. Meissn. (Brassicaceae) to identify their glucosinolate constituents, antimicrobial and cytotoxic activities Materials and methods: The glucosinolates were identified using GC-MS analysis of their hydrolysis products and LC-MS analysis in the case of seeds. Disc diffusion (1 mg/disc) and minimum inhibitory concentration (0-160 μg/mL) methods were used to evaluate the antimicrobial activity of seed hydrolysate. In vitro cytotoxicity against colorectal HCT-116, hepatic HUH-7, breast MCF-7 and lung A-549 cells was evaluated for seed hydrolysate (0.01-100 μg/mL) using the sulforhodamine B assay and doxorubicin as a standard Results: Three glucosinolates were identified for the first time in this plant and genus Lobularia. Glucoiberverin was the major compound accumulated in the seeds and leaves, while glucoiberin and glucoerucin were detected only in the seeds. No glucosinolates were detected in roots under the same experimental conditions. Other volatile constituents, e.g., terpenes and fatty acids were only identified in the seeds. The seed hydrolysate showed significant antimicrobial activities against Candida albicans and Pseudomonas aeruoginosa (MIC = 64 and 82 μg/mL, respectively). The seed hydrolysate exhibited a marked selective cytotoxicity in vitro against colorectal, hepatic and breast cancer cell lines. The IC50 values were 0.31, 2.25 and 37 μg/mL, respectively. The results indicated the antimicrobial activity of L. libyca and the selective effect of the seed hydrolysate as a cytotoxic drug that is potentially more active than doxorubicin against HCT-116.

  16. SYNTHESIS AND CYTOTOXIC ACTIVITY OF CHALCONE DERIVATIVES ON HUMAN BREAST CANCER CELL LINES

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    Nuraini Harmastuti

    2012-12-01

    Full Text Available Chalcone, an α,β-unsaturated ketone, has been shown have many biological activities such as anticancer and antifungi. This research was conducted to synthesize the chalcone derivatives and to obtain their cytotoxic activity on human cervix cancer cell lines. Synthesis of chalcone and its derivatives, 4II-methylchalcone, 4II-methoxychalcone, and 3II,4II-dichlorochalcone was carried out using starting materials of benzaldehide and acetofenon, p-methylacetophenone, p-methoxyacetophenone, as well as m,p-dichloroacetophenone through Claisen Schmidt condensation catalized by NaOH in ethanol at 15 °C. The purity of synthesized compounds were analyzed by thin layer chromatography, melting range, and gas chromatography. Structure elucidations were conducted by UV spectrophotometer, IR spectrometer, 1H-NMR spectrometer, as well as mass spectrometer. Cytotoxic activities were determined by 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide (MTT microculture tetrazolium viability assay. The results showed that chalcone and derivatives compounds have been able to be synthesized and purified and had the same structure as a predicted structure. Chalcone had highest cytotoxic activity compared to that of its derivatives, with the IC50 values of chalcone, 4II-methylchalcone, 4II-methoxychalcone, and 3II,4II-dichlorochalcone were 9.49, 14.79, 11.48, and 24.26 µg/mL respectively. It was concluded that methyl, methoxy as well as chlorine substitution at 3 II and 4II position decrease the cytotoxic activity of chalcone.

  17. Cytotoxicity and Antiproliferative Activity Assay of Clove Mistletoe (Dendrophthoe pentandra (L. Miq. Leaves Extracts

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    Vida Elsyana

    2016-01-01

    Full Text Available Clove mistletoe (Dendrophthoe pentandra (L. Miq. is a semiparasitic plant that belongs to Loranthaceae family. Clove mistletoe was traditionally used for cancer treatment in Indonesia. In the present study, we examined cytotoxicity of clove mistletoe leaves extracts against brine shrimps and conducted their antiproliferative activity on K562 (human chronic myelogenous leukemia and MCM-B2 (canine benign mixed mammary cancer cell lines in vitro. The tested samples were water extract, ethanol extract, ethanol fraction, ethyl acetate fraction, and n-hexane fraction. Cytotoxicity was screened using Brine Shrimp Lethality Test (BSLT. Antiproliferative activity was conducted using Trypan Blue Dye Method and cells were counted using haemocytometer. The results showed that n-hexane fraction exhibited significant cytotoxicity with LC50 value of 55.31 μg/mL. The n-hexane fraction was then considered for further examination. The n-hexane fraction of clove mistletoe could inhibit growth of K562 and MCM-B2 cancer cell lines in vitro. The inhibition activity of clove mistletoe n-hexane fraction at concentration of 125 μg/mL on K562 cancer cell lines was 38.69%, while on MCM-B2 it was 41.5%. Therefore, it was suggested that clove mistletoe had potential natural anticancer activity.

  18. Cytotoxic activity of N, N'-Bis (2-hydroxybenzyl) ethylenediamine derivatives in human cancer cell lines.

    Science.gov (United States)

    Musa, Musiliyu A; Badisa, Veera L D; Latinwo, Lekan M

    2014-04-01

    Compounds containing ethylenediamine (-NCH2CH2N-) moiety are known to exhibit antimicrobial, -fungal, -bacterial, -tuberculosis and -cancer activities. In the present study, we evaluated the in vitro cytotoxic activity of N,N'-bis(2-hydroxybenzyl)- (6), N,N'-bis(5-bromo-2-hydroxybenzyl)- (7) and N,N'-bis(5-chloro-2-hydroxybenzyl) (8)- ethylenediamine dihydrochlorides; and N,N'-bis(2-hydroxybenzyl)- (9), N,N'-bis(5-bromo-2-hydroxybenzyl)- (10) and N,N'-bis(5-chloro-2-hydroxybenzyl) (11)- ethylenediamine toward human lung (A549), breast (MDA-MB-231) and prostate (PC3) cancer cell lines after 24-h treatment using crystal violet dye binding assay. Effects on the cell cycle the using flow cytometry, and mitochondrial membrane potential using rhodamine-123 florescent dye were also evaluated. Compounds 7 and 8 exhibit cytotoxic activity, causing cell arrest at different phases of the cell cycle and loss of mitochondrial membrane potential in the above cancer cell lines. These findings clearly demonstrate, to our knowledge for the first time, that ethylenediamine dihydrochloride salts-compounds 7 and 8-exhibit concentration-dependent cytotoxic activity towards A549, MDA-MB-231 and PC3 cancer cell lines, which may serve as a basis for future work on novel therapeutic agents.

  19. Synthesis, cytotoxicity, and antileishmanial activity of N,N'-disubstituted ethylenediamine and imidazolidine derivatives.

    Science.gov (United States)

    de Carvalho, Gustavo S G; Machado, Patrícia A; de Paula, Daniela T S; Coimbra, Elaine S; da Silva, Adilson D

    2010-09-01

    This paper describes the preparation of N,N'-disubstituted ethylenediamine and imidazolidine derivatives and their in vitro biological activities against Leishmania species. Of the nine synthesized compounds, five displayed a good activity in both L. amazonensis and L. major promastigotes. The compounds 1,2-Bis(p-methoxybenzyl) ethylenediamine (4) and 1,3-Bis(p-methoxybenzyl)imidazolidines (5) showed the best activity on intracellular amastigotes, with IC50 values of 2.0 and 9.4 microgram/mL, respectively. In addition, none of compounds were cytotoxic against mammalian cells. The leishmanicidal activity can be related with inhibition of polyamine synthesis and cellular penetration within biological membranes.

  20. Properties and limits of some essential oils: chemical characterisation, antimicrobial activity, interaction with antibiotics and cytotoxicity.

    Science.gov (United States)

    Scazzocchio, Francesca; Garzoli, Stefania; Conti, Cinzia; Leone, Claudia; Renaioli, Clio; Pepi, Federico; Angiolella, Letizia

    2016-09-01

    Because of the emergence of multi-drug resistance bacteria and fungi, alternatives to conventional antimicrobial therapy are needed. This study aims to evaluate in vitro the antimicrobial activity of: Mirtus communis, Coriandrum sativum, Pelargonium capitatum, Cuminum cyminum, Ocimum basilicum, Citrus aurantium amara, Cymbopogon. winterianus, Cymbopogon martini, Salvia sclarea, Melaleuca alternifolia and Mentha suaveolens essential oils on bacteria and fungi, in relation to their chemical composition. The potential interaction of M. alternifolia (TTO), C. sativum (CDO) and M. suaveolens (EOMS) essential oils when used in combination with gentamicin and fluconazole has been evaluated. The results obtained showed a synergic effect on some bacteria and fungi, with FICI values ≤5. The cytotoxicity of TTO, CDO and EOMS was investigated towards HeLa cells. Only EOMS did not result cytotoxic at the active concentrations on micro-organisms. Further studies are necessary to obtain optimal ratios and dosing regimens for higher therapeutic efficacy and to decrease toxicological profiles.

  1. "Proliferation of cytotoxic and activated T cells during acute Epstein-Barr virus induced Infectious Mononucleosis "

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    Mansoori SD

    2002-05-01

    Full Text Available The immune responses that develop following Epstien-Barr Virus (EBV infection are complex and involve both humoral and to a greater extent cell-mediated immune mechanisms. To evaluate the immune response, flow cytometric analysis of the peripheral blood of six patients during the acute phase of EBV infection was performed. This analysis revealed a significant increase in the percentages and the absolute number of CD8+cytotoxic and activated (HLA-DR+ - T lymphocytes and in some cases with a concomitan decrease in the percentages of B (CD19+ lymphocytes and T helper (CD4+ lymphocytes. These patient invariably had inverted CD4/CD8 ratio. All changes reversed to normal level during the recovery phase of infection. It is therefore concluded that EBV specific cytotoxic and activated T lymphocytes are essential in controlling acute EBV infection presented by the infected B cells.

  2. The inhibition effect of non-protein thiols on dentinal matrix metalloproteinase activity and HEMA cytotoxicity.

    Science.gov (United States)

    Nassar, Mohannad; Hiraishi, Noriko; Shimokawa, Hitoyata; Tamura, Yukihiko; Otsuki, Masayuki; Kasugai, Shohei; Ohya, Keiichi; Tagami, Junji

    2014-03-01

    Phosphoric acid (PA) etching used in etch-and-rinse adhesives is known to activate host-derived dentinal matrix-metalloproteinases (MMPs) and increase dentinal permeability. These two phenomena will result, respectively; in degradation of dentine-adhesive bond and leaching of some monomers especially 2-hydroxyethyl methacrylate (HEMA) into the pulp that would negatively affect the viability of pulpal cells. This study is the first to investigate the inhibitory effect of non-protein thiols (NPSH); namely reduced glutathione (GSH) and N-acetylcysteine (NAC) on dentinal MMPs and compare their effects on HEMA cytotoxicity. Dentine powder was prepared from human teeth, demineralized with 1% PA and then treated with 2% GSH, 2% NAC or 2% chlorhexidine (CHX). Zymographic analysis of extracted proteins was performed. To evaluate the effect of GSH, NAC and CHX on HEMA cytotoxicity, solutions of these compounds were prepared with or without HEMA and rat pulpal cells were treated with the tested solutions for (6 and 24h). Cells viability was measured by means of 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Cytotoxicity data were analysed by one-way ANOVA and Tukey post hoc tests (peffect of GSH and NAC on dentinal MMPs was confirmed. GSH showed similar effectiveness to NAC regarding HEMA cytotoxicity inhibition. NPSH were effective to inhibit dentinal MMPs and HEMA cytotoxicity. The tested properties of NPSH provide promising clinical use of these agents which would enhance dentine-bond durability and decrease post-operative sensitivity. Copyright © 2013 Elsevier Ltd. All rights reserved.

  3. Cytotoxic activity of isolated constituents from leaves of Premna serratifolia on MCF-7 and HT-29 cell lines

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    Mahesh Biradi

    2015-03-01

    Full Text Available Premna serratifolia (Syn: Premna integrifolia is an important medicinal herb known as “Agnimantha” in Ayurveda and traditionally used for anticancer activity. The objective of present study was to isolate the cytotoxic phytoconstituents from the n-hexane soluble fraction of P. serratifolia leaf extract. Unsaponifiable portion of n-hexane soluble fraction was subjected to silica based column chromatography. The major constituents present in all the sub-fractions were identified by TLC and phytochemical tests. Two constituents were isolated and they were purified. Sub-fractions with isolates were tested for cytotoxic effect by BSL bioassay. Two isolates were found to be active and which were tested on cancer cell lines MCF-7 and HT-29 for their cytotoxicity. Among two isolates, one compound has shown significant cytotoxicity. From the results we conclude that the plant isolates showed cytotoxicity against selected human cancer cell lines.

  4. Antimicrobial, Antiparasitic, Anti-Inflammatory, and Cytotoxic Activities of Lopezia racemosa

    OpenAIRE

    Cruz Paredes, Carla; Bolívar Balbás, Paulina; Gómez-Velasco, Anaximandro; Juárez, Zaida Nelly; Sánchez Arreola, Eugenio; Hernández, Luis Ricardo; Bach, Horacio

    2013-01-01

    The present study investigates the potential benefits of the Mexican medicinal plant Lopezia racemosa (Onagraceae). Extracts and fractions from aerial parts of this plant were assessed to determine their antibacterial, antifungal, antiparasitic, anti-inflammatory and cytotoxic activities in vitro. Aerial parts of the plant were extracted with various solvents and fractionated accordingly. Extracts and fractions were tested against a panel of nine bacterial and four fungal species. The antipar...

  5. INHIBITION OF THE NKG2D ACTIVATING RECEPTOR EXPRESSION ON CYTOTOXIC LYMPHOCYTES BY RECOMBINANT MICA PROTEIN

    OpenAIRE

    E. V. Abakushina; E. Yu. Lyssuk; A. V. Posvyatenko; A. V. Kibardin

    2017-01-01

    Genome instability of transformed cells, being the most common factor of malignancy, may result into production of abnormal proteins in these cells. Normally, the newly formed proteins are recognized by immune system, thus causing elimination of the transformed cells. Nevertheless, the phenotypic instability promotes formation of specific transformed cells which suppress effector immune reactions and/or are unrecognizable by cytotoxic lymphocytes. NKG2D is one of the most important activating...

  6. Antioxidant activity and cytotoxicity of solubilized C60 and its conjugates with butylated hydroxytoluene

    OpenAIRE

    Nunes, A. S.; Matias, A.; Caetano, Liliana Aranha; Graça, Anabela; Simplício, Ana Luísa

    2011-01-01

    It has been described that fullerenes (C60) present interesting properties with potential application in clinical conditions related to oxidative stress. One of the most prominent features of fullerenes is the ability to quench free radicals. However, because of its poor solubility, this has been studied mostly in organic solutions, while the antioxidant activity and cytotoxicity of fullerenes and their derivates in aqueous medium is not well characterized. The antioxidant capacity of s...

  7. Cytotoxic activity of Piper cubeba extract in breast cancer cell lines.

    Science.gov (United States)

    Graidist, Potchanapond; Martla, Mananya; Sukpondma, Yaowapa

    2015-04-10

    This study aimed to evaluate the cytotoxicity of a crude extract of Piper cubeba against normal and breast cancer cell lines. To prepare the extract, P. cubeba seeds were ground, soaked in methanol and dichloromethane and isolated by column chromatography. Fractions were tested for cytotoxicity effects on normal fibroblast (L929), normal breast (MCF-12A) and breast cancer cell lines (MCF-7, MDA-MB-468 and MDA-MB-231). The most effective fraction was selected for DNA fragmentation assay to detect apoptotic activity. The results showed that the methanolic crude extract had a higher cytotoxic activity against MDA-MB-468 and MCF-7 than a dichloromethane crude extract. Then, the methanolic crude extract was separated into six fractions, designated A to F. Fraction C was highly active against breast cancer cell lines with an IC50 value less than 4 μg/mL. Therefore, Fraction C was further separated into seven fractions, CA to CG. The 1H-NMR profile showed that Fraction CE was long chain hydrocarbons. Moreover, Fraction CE demonstrated the highest activity against MCF-7 cells with an IC50 value of 2.69 ± 0.09 μg/mL and lower cytotoxicity against normal fibroblast L929 cells with an IC50 value of 4.17 ± 0.77 μg/mL. Finally, DNA fragmentation with a ladder pattern characteristic of apoptosis was observed in MCF-7, MDA-MB-468, MDA-MB-231 and L929 cells, but not in MCF-12A cells.

  8. Flavonoid constituents and cytotoxic activity of Erucaria hispanica (L. Druce growing wild in Egypt

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    M.M. Marzouk

    2016-09-01

    Full Text Available Thirteen flavonoid compounds were isolated for the first time from the aerial parts of Erucaria hispanica (L. Druce growing in Egypt. Their structures were established on the basis of detailed chromatographic and spectroscopic techniques (UV, 1D and 2D NMR and ESIMS. The cytotoxic activity of the methanol extract as well as some isolated compounds against four human carcinoma cell lines; breast (MCF7, liver (HEPG2, cervix (HELA and colon (HCT116 were evaluated.

  9. A new flavone and cytotoxic activity of flavonoid constituents isolated from Miliusa balansae (Annonaceae).

    Science.gov (United States)

    Huong, D T; Luong, D V; Thao, T T P; Sung, T V

    2005-08-01

    A new flavone named miliufavol [8-(2-hydroxybenzyl)-5-hydroxy-2-(4-hydroxy-3-methoxyphenyl)-3,7-dimethoxy-4H-chromen-4-one or 8-C-(o)-hydroxybenzylpachypodol] from Miliusa balansae (Annonaceae) was isolated and structurally elucidated by spectroscopic means besides four known flavones: ombuine, chrysosplenol B, pachypodol and chrysosplenol C. These flavonoids exhibited interesting cytotoxic activity against three human cell lines (KB, Hep-G2, RD) with IC50 values < 5 microg/ml.

  10. Chemical Composition, Antimicrobial, Cytotoxic and Antiplasmodial Activities of Three Sponges from Buton Islands, Indonesia

    OpenAIRE

    Masteria Yunovilsa Putra; Tri Aryono Hadi

    2017-01-01

    GC-MS analysis of the crude extracts of three different species of Indonesian marine sponges has been carried out for identification of bioactive compounds. The GC-MS analysis from Haliclona (Gellius) sp., Lamellodysidea herbacea, and Spheciospongia inconstans revealed the presence of 23, 21, 19 various compounds, respectively and mainly sterols and fatty acids. All the sponge species has been evaluated for antimicrobial activities, cytotoxicity using brine shrimp lethality bioassay and heme ...

  11. Cytotoxic Activity of Methanol Fraction Hydroids Aglaophenia cupressina Lamoureoux Against HeLa Tumor Cells

    OpenAIRE

    Eva Johannes; Sjafaraenan; Magdalena Litaay; Nur Haedar

    2017-01-01

    Bioactive compounds from marine organisms widely explored in an effort to get raw material of anti tumor or cancer that until now still leading cause of death in the world. In medicine, basic materials drug search of antitumor from nature are generally focused on active compound that has ability to suppress tumor cell proliferation, have effect of cytotoxic and antimitotic, and has no side effects. Hydroids Aglaophenia cupressina Lamoureoux is a marine invertebrate animals that live attached ...

  12. Screening of Venezuelan medicinal plant extracts for cytostatic and cytotoxic activity against tumor cell lines.

    Science.gov (United States)

    Taylor, Peter; Arsenak, Miriam; Abad, María Jesús; Fernández, Angel; Milano, Balentina; Gonto, Reina; Ruiz, Marie-Christine; Fraile, Silvia; Taylor, Sofía; Estrada, Omar; Michelangeli, Fabian

    2013-04-01

    There are estimated to be more than 20,000 species of plants in Venezuela, of which more than 1500 are used for medicinal purposes by indigenous and local communities. Only a relatively small proportion of these have been evaluated in terms of their potential as antitumor agents. In this study, we screened 308 extracts from 102 species for cytostatic and cytotoxic activity against a panel of six tumor cell lines using a 24-h sulphorhodamine B assay. Extracts from Clavija lancifolia, Hamelia patens, Piper san-vicentense, Physalis cordata, Jacaranda copaia, Heliotropium indicum, and Annona squamosa were the most cytotoxic, whereas other extracts from Calotropis gigantea, Hyptis dilatata, Chromolaena odorata, Siparuna guianensis, Jacaranda obtusifolia, Tapirira guianensis, Xylopia aromatica, Protium heptaphyllum, and Piper arboreum showed the greatest cytostatic activity. These results confirm previous reports on the cytotoxic activities of the above-mentioned plants as well as prompting further studies on others such as C. lancifolia and H. dilatata that have not been so extensively studied. Copyright © 2012 John Wiley & Sons, Ltd.

  13. Effect of shark cartilage on the cytotoxic activity of NK cells immune system

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    Afshar Bargahi

    2009-12-01

    Full Text Available Background: On the basis of traditional medicine Shark cartilage have been used in the treatment of cancer especially immune related cancers. Then, we hypotheses that shark cartilage contains immune stimulatory ingredients. Methods: The immune stimulatory effect of shark cartilage derived proteins on the cytotoxic activity of natural killer cells(NK cells from healthy human peripheral blood mononuclear cells (hPBMN was studied. Shark cartilage proteins were purified by ion-exchange chromatography and ultra filtration. The effect of each protein fraction on the modulation of cytotoxicity of NK cells, as effectors, against K562, as target cells, was assayed by enzymatic LDH test. Results: The results from cytotoxic assay of NK cells and SDS- Polyacrylamide gell electrophoresis of shark cartilage protein fractions indicated that AR10 fraction, containing proteins with molecular weight of about 14.5 KDa is the most active ingredients of shark cartilage. Conclusion: Shark cartilage contains a 14.5 KDa protein that modulates NK cells activity of human immune system.

  14. Extracts from Fermented Black Soybean Milk Exhibit Antioxidant and Cytotoxic Activities

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    Kuan-Chen Cheng

    2011-01-01

    Full Text Available In this study, ethanol extracts from 2-day fermented black soybean milk (FBE by immobilized Rhizopus oligosporus NTU5 have been evaluated for both antioxidant and cytotoxic activities. The results reveal that a 2-day FBE had strong 2,2-diphenyl-1-picrylhydrazyl (DPPH scavenging effect (76 %. The extracts were further fractionated by silica gel column chromatography and an unknown compound, FBE5-A, was obtained, which exhibited strong antioxidant activity. IC50 of the DPPH scavenging effect of FBE5-A was 7.5 μg/mL, which is stronger than a commonly used antioxidant, vitamin E (α-tocopherol; 17.4 μg/mL, and similar to vitamin C (ascorbic acid; 7.6 μg/mL. The cytotoxic test demonstrated that extracts of 2-day fermented broth exhibited selective cytotoxic activity towards human carcinoma cells, Hep 3B (IC50=150.2 μg/mL, and did not affect normal human lung fibroblasts, MRC-5 (p<0.05. The results indicate the potential applications of fermented black soybean milk as functional food, pharmaceutical or cancer therapy formula.

  15. Phytochemical screening, antiproliferative and cytotoxic activities of the mosses Rhytidiadelphus triquetrus (Hedw.) Warnst. and Tortella tortuosa (Hedw.) Limpr.

    OpenAIRE

    Muhammet Şamil Yağlıoğlu; Gökhan Abay; Ibrahim DemirtaŞ; Ayşe Şahin Yağlıoğlu

    2017-01-01

    The paper presents information about the phytochemical analysis, antiproliferative and cytotoxic activities of Rhytidiadelphus triquetrus and Tortella tortuosa extracts. The cytotoxic activities of some extracts shows highest antiproliferative activities were detected with Lactate Dehydrogenase Leakage Assay. Sixteen components obtained from hexane extracts were determined by GC/MS. Palmitic acid was identified as the main component. The phenolic components of the other extracts were determin...

  16. In vitro evaluation of cytotoxic activity of flower, leaf, stem and root extracts of five Artemisia species.

    Science.gov (United States)

    Gordanian, B; Behbahani, M; Carapetian, J; Fazilati, M

    2014-01-01

    The present study was carried out to investigate cytotoxic activity of flower, leaf, stem and root extracts of five Artemisia species against breast cancer cell line (MCF7) and human embryonic kidney normal cell line (HEK293). The studied Artemisia species were A. absinthium, A. vulgaris, A. incana, A. fragrans and A. spicigera. The cytotoxic activity was measured by MTT assay at different concentrations (62.5, 125, 250, 500 μg/ml). Among these five species, methanol extracts of flower, leaf, stem and root of A. absinthium and A. vulgaris exhibited considerable cytotoxic activity. The flower extracts of these two species were found to have higher cytotoxic effect on MCF7 cell with an IC50 value of 221.5 and >500 μg/ml, respectively. Leaf methanol extract of A. incana also showed cytotoxic activity. Cytotoxic activity of different extracts of A. absinthium, A. vulgaris and A. incana against MCF7 was 10%-40% more than HEK293 cells. Not only the extracts of A. spicigera and A. fragrans did not show any cytotoxic effect against both cell lines, but also increased the number of cells. This study revealed that A. absinthium and A. vulgaris may have a great potential to explore new anticancer drugs.

  17. Chemical composition and cytotoxicity activity of the essential oil of Pterodon emarginatus

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    Rafael C. Dutra

    2012-10-01

    Full Text Available Pterodon emarginatus Vogel, Fabaceae, is a native aromatic tree distributed by central region of Brazil. Hydroalcoholic infusions of the seeds are used in folk medicine for their anti-rheumatic and anti-inflammatory properties. The objective of this work was identified the chemical components and verify the cytotoxic effect of the essential oil (EO from P. emarginatus seeds. Thus, the EO of P. emarginatus seeds was analyzed by GC/MS analysis followed by brine shrimp lethality test and cytotoxic activity against tumor cell lines and human peripheral mononuclear blood cells (PBMC. The cancer cell lines tested were C6 (rat glioma, MeWo (human melanoma, CT26.WT (mouse colon carcinoma, MDA (human breast cancer, A549 (human lung carcinoma, B16-F1 (mouse melanoma, CHO-K1 (hamster ovary cell and BHK-21 (hamster kidney fibroblast. Eleven compounds were identified by GC and CG/MS analyses. The main compounds with concentrations higher than 5% were β-elemene (15.3%, trans-caryophyllene (35.9%, α-humulene (6.8%, germacrene-D (9.8%, bicyclo germacrene (5.5% and spathulenol (5.9%. The EO of P. emarginatus seeds showed toxicity to Artemia salina (LC50 1.63 µg/mL and was active against all the cell lines tested. The potent cytotoxic activity had IC50 values ranging from 24.9 to 47 µg/mL. However, EO (1-100 µg/mL had less cytotoxicity in PBMCs isolated from a healthy subject. In summary, the present study showed the potential antiproliferative of the EO of P. emarginatus seeds.

  18. Synthesis, cytotoxicity and antifungal activity of 5-nitro-thiophene-thiosemicarbazones derivatives.

    Science.gov (United States)

    de Araújo Neto, Luiz Nascimento; do Carmo Alves de Lima, Maria; de Oliveira, Jamerson Ferreira; de Souza, Edson Rubhens; Buonafina, Maria Daniela Silva; Vitor Anjos, Mayara Nunes; Brayner, Fábio André; Alves, Luiz Carlos; Neves, Rejane Pereira; Mendonça-Junior, Francisco Jaime Bezerra

    2017-06-25

    In the present work, twelve N-substituted 2-(5-nitro-thiophene)-thiosemicarbazones derivatives (L1-12) were synthesized, characterized and their in vitro cytotoxic and antifungal activities were evaluated against Candida sp. and Cryptococcus neoformans. The probable mechanisms of action have been investigated by sorbitol and ergosterol assays. Additionally, ultrastructural study by Scanning Electron Microscopy was performed with the L10 compound. All compounds were obtained in good yield and their chemical structures were characterized on basis of their physico-chemical and Nuclear Magnetic Resonance - NMR, Spectrophotometric Absorption in the Infrared - IR and High-resolution Mass Spectrometry - HRMS data. The results showed that all strains were more sensitive to the compound L10 except Candida tropicalis URM 6551. On the other hand, the cytotoxicity assay by incorporation of tritiated thymidine showed moderate cytotoxic activity on L8 of the 50 μg/mLat which had the best MIC-cytotoxicity relationship. Concerning the study of the possible mechanism of action, the compounds were not able to bind to ergosterol in the membrane, do not act by inhibiting the synthesis of fungal cell wall (sorbitol assay). However, the Scanning Electron Microscopy - SEM analysis shows significant morphological changes in shape, size, number of cells and hyphae, and cell wall indicating a possible mechanism of action by inhibition of enzymes related to the ergosterol biosynthesis pathway. Our results demonstrate that N-substituted 2-(5-nitro-thiophene)-thiosemicarbazones derivatives are potential antifungal agents with activity associated with inhibition of enzymes related to biosynthesis of ergosterol. Copyright © 2017 Elsevier B.V. All rights reserved.

  19. Characterization of antimicrobial activity against Listeria and cytotoxicity of native melittin and its mutant variants.

    Science.gov (United States)

    Wu, Xi; Singh, Atul K; Wu, Xiaoyu; Lyu, Yuan; Bhunia, Arun K; Narsimhan, Ganesan

    2016-07-01

    Antimicrobial peptides (AMPs) are relatively short peptides that have the ability to penetrate the cell membrane, form pores leading to cell death. This study compares both antimicrobial activity and cytotoxicity of native melittin and its two mutants, namely, melittin I17K (GIGAVLKVLTTGLPALKSWIKRKRQQ) with a higher charge and lower hydrophobicity and mutant G1I (IIGAVLKVLTTGLPALISWIKRKRQQ) of higher hydrophobicity. The antimicrobial activity against different strains of Listeria was investigated by bioassay, viability studies, fluorescence and transmission electron microscopy. Cytotoxicity was examined by lactate dehydrogenase (LDH) assay on mammalian Caco-2 cells. The minimum inhibitory concentration of native, mutant I17K, mutant G1I against Listeria monocytogenes F4244 was 0.315±0.008, 0.814±0.006 and 0.494±0.037μg/ml respectively, whereas the minimum bactericidal concentration values were 3.263±0.0034, 7.412±0.017 and 5.366±0.019μg/ml respectively. Lag time for inactivation of L. monocytogenes F4244 was observed at concentrations below 0.20 and 0.78μg/ml for native and mutant melittin I17K respectively. The antimicrobial activity against L. monocytogenes F4244 was in the order native>G1I>I17K. Native melittin was cytotoxic to mammalian Caco-2 cells above concentration of 2μg/ml, whereas the two mutants exhibited negligible cytotoxicity up to a concentration of 8μg/ml. Pore formation in cell wall/membrane was observed by transmission electron microscopy. Molecular dynamics (MD) simulation of native and its mutants indicated that (i) surface native melittin and G1I exhibited higher tendency to penetrate a mimic of bacterial cell membrane and (ii) transmembrane native and I17K formed water channel in mimics of bacterial and mammalian cell membranes. Copyright © 2016 Elsevier B.V. All rights reserved.

  20. Sesquiterpene lactones from the extracts of two Balkan endemic Laserpitium species and their cytotoxic activity.

    Science.gov (United States)

    Popović, Višnja; Heyerick, Arne; Petrović, Silvana; Van Calenbergh, Serge; Karalić, Izet; Niketić, Marjan; Deforce, Dieter

    2013-03-01

    Chloroform extracts of the underground parts of two Balkan endemic Laserpitium species, Laserpitium zernyi Hayek and Laserpitium ochridanum Micevski, were chemically investigated. Five unknown guaianolides from the class of slovanolides, of which four were additionally 2β-esterified, as well as two lactones, previously identified in other Laserpitium species, were isolated from the L. ochridanum extract. From the L. zernyi extract one slovanolide derivative was isolated for the first time in the genus Laserpitium. In addition, the phenylpropanoid latifolone and six known sesquiterpene lactones, characterised as derivatives of slovanolide and silerolide, were isolated from the extracts of both species. The cytotoxic activities of the total extracts and the isolated compounds were tested using MTT and SRB assays on the two human breast cancer cell lines, MCF 7/6 and MCF 7/AZ. The extracts exerted cytotoxic activities with the IC(50) values ranging 65.21-348.25 μg/mL. The L. ochridanum extract was most potent in the MTT test with IC(50) values of 65.21 and 66.09 μg/mL in the MCF 7/AZ and MCF 7/6 cell lines, respectively. The highest cytotoxic activity exerted 2β,8α-di-angeloyloxy-10β-hydroxy-6αH-guaian-3,(7-11)-dien-12,6-olide, a slovanolide derivative with an additional double bond in lactone ring, on highly invasive MCF 7/6 cell line, with IC(50) value 0.7 μM in both assays tested. Generally, guaianolides with a higher number of ester moieties at the positions 2β, 8α, 10β or 11α exhibited IC(50) values in the micromolar range, while eudesmanolides and guaianolides with a lower number of esters did not induce significant cytotoxicity. Copyright © 2012 Elsevier Ltd. All rights reserved.

  1. Investigation of antimalarial activity, cytotoxicity and action mechanism of piperazine derivatives of betulinic acid.

    Science.gov (United States)

    Silva, Gloria N S; Schuck, Desirée C; Cruz, Laura N; Moraes, Miriam S; Nakabashi, Myna; Gosmann, Grace; Garcia, Célia R S; Gnoatto, Simone C B

    2015-01-01

    To semisynthesise piperazine derivatives of betulinic acid to evaluate antimalarial activity, cytotoxicity and action mechanism. The new derivatives were evaluated against the CQ-sensitive Plasmodium falciparum 3D7 strain by flow cytometry (FC) using YOYO-1 as stain. Cytotoxicity of 4a and 4b was performed with HEK293T cells for 24 and 48 h by MTT assay. The capability of compound 4a to modulate Ca(2+) in the trophozoite stage was investigated. The trophozoites were stained with Fluo4-AM and analysed by spectrofluorimetry. Effect on mitochondrial membrane potential (ΔΨm) was tested for 4a by FC with DiOC6 (3) as stain. For β-haematin assay, 4a was incubated for 24 h with reagents such as haemin, and the fluorescence was measured by FlexStation at an absorbance of 405 nm. Antimalarial activity of 4a and 4b was IC50 = 1 and 4 μm, respectively. Compound 4a displayed cytotoxicity with IC50 = 69 and 29 μm for 24 and 48 h, respectively, and 4b was not cytotoxic at the tested concentrations. Addition of 4a leads to an increase in cytosolic Ca(2+) . We have measured ΔΨm after treating parasites with the compound. Data on Figure 4a show that mitochondria were not affected. The action mechanism for 4a, inhibition of β-haematin formation (17%), was lower than CQ treatment (83%; IC50 = 3 mm). Compound 4a showed excellent antimalarial activity, and its action mechanism is involved in Ca(2+) pathway(s). © 2014 John Wiley & Sons Ltd.

  2. Biological Activities and Cytotoxicity of Eperua oleifera Ducke Oil-resin

    Science.gov (United States)

    Alves Gomes, Fernanda Torlania; Boleti, Ana Paula de Araújo; Leandro, Lidiam M.; Squinello, Diego; Aranha, Ellen S. P.; Vasconcelos, Marne C.; Cos, Paul; Veiga-Junior, Valdir F.; Lima, Emerson Silva

    2017-01-01

    Background: The oil-resin of Eperua oleifera Ducke has been used in popular medicine similarly to the copaiba oil (Copaifera spp.). Objective: This study aimed to investigate the effects of the acid fraction of E. oleifera oil-resin (AFEOR) on cell proliferation, collagen production in human fibroblasts, inhibition of metalloproteinases, and cytotoxicity against tumor cell lines. Materials and Methods: Acid fraction of E. oleifera was fractionated in the ion exchange column chromatography. Cytotoxicity and genotoxicity were evaluated by Alamar Blue® and Cometa assay. The inhibition of metalloproteinases was performed by zymography and Western blotting. Results: The predominant acidic diterpenes in the AFEOR were copalic and hardwickiic acids. AFEOR caused morphology alteration and decrease of proliferation at concentrations higher than 5 μg/mL. It also caused significant collagen proliferation in fibroblasts. It showed cytotoxicity against tumoral and nontumoral cell lines, with IC50 values ranging from 13 to 50 μg/mL, and a hemolytic activity with an IC50 value of 38.29 μg/mL. AFEOR inhibited collagenase activity, with an IC50 value of 46.64 μg/mL, and matrix metalloproteinase-2 (MMP)-2 and MMP-9 in HaCaT cells or MMP-1 expression in MRC-5 cells. AFEOR induced genotoxicity in MRC-5 cells with a DNA damage index between 40% and 60% when compared to the negative controls (0%–20%). Conclusion: For the first time, biological activities from oil-resin E. oleifera demonstrated ratifying somehow its popular use. SUMMARY Analysis of crude oil-resin and fractionation of diterpenic fraction was performance using selective ion-exchange column chromatographyCytotoxicity analysis and morphology were performed with different cell linesCollagen production in human fibroblasts, inhibition of metalloproteinases were demonstrated by zymography and Western blotting. Abbreviations used: AFEOR: Eperua oleifera oil-resin. PMID:29200711

  3. In Vitro Parallel Evaluation of Antibacterial Activity and Cytotoxicity of Commercially Available Silver-Containing Wound Dressings.

    Science.gov (United States)

    Yunoki, Shunji; Kohta, Masushi; Ohyabu, Yoshimi; Iwasaki, Tetsuji

    2015-01-01

    This study evaluated the in vitro antibacterial activity and cytotoxicity of various commercially available silver-containing dressings (Ag dressing). Biohesive Ag (hydrocolloid, silver sulfadiazine), Aquacel® Ag (nonwoven fabric, ionic silver [Ag]), Algisite™ Ag (nonwoven fabric, Ag), Mepilex® Ag (foam, silver sulfate), and PolyMem® Ag (foam, nanocrystalline silver) were tested for characteristics of Ag release, antibacterial activity, and cytotoxicity. The release of Ag was investigated in cell culture medium at immersion periods of 6, 24, and 48 hours. The antibacterial activity against Staphylococcus aureus and Pseudomonas aeruginosa were accessed by a disc diffusion test. The cytotoxicity was evaluated using V79 cells, by an extraction method. The cytotoxicity was not a monotonic function of the antibacterial activity among the Ag dressings and could not be simply explained by Ag-release properties. Biohesive Ag was regarded as a slow-release Ag dressing, showing the lowest cytotoxicity, while the antibacterial activity was classified as "strong" or "significant" against the two species of bacteria. Aquacel Ag and Algisite Ag showed higher antibacterial activity and cytotoxic effects, which were supported by the higher Ag release. Mepilex Ag showed the highest release of Ag, and the cytotoxicity was the highest among the Ag dressings. However, the antibacterial activity was classified as "significant" or "no activity" for P. aeruginosa and S. aureus, respectively. PolyMem Ag showed the lowest Ag release, and the antibacterial activity classified as "significant" or "no activity" for S. aureus and P. aeruginosa, respectively, whereas the cytotoxicity was similar to those of Aquacel Ag and Algisite Ag. The efficacy and adverse effects of the Ag dressings revealed differences that should be considered by clinicians during wound management.

  4. Antimicrobial, antiparasitic, anti-inflammatory, and cytotoxic activities of Lopezia racemosa.

    Science.gov (United States)

    Cruz Paredes, Carla; Bolívar Balbás, Paulina; Gómez-Velasco, Anaximandro; Juárez, Zaida Nelly; Sánchez Arreola, Eugenio; Hernández, Luis Ricardo; Bach, Horacio

    2013-01-01

    The present study investigates the potential benefits of the Mexican medicinal plant Lopezia racemosa (Onagraceae). Extracts and fractions from aerial parts of this plant were assessed to determine their antibacterial, antifungal, antiparasitic, anti-inflammatory and cytotoxic activities in vitro. Aerial parts of the plant were extracted with various solvents and fractionated accordingly. Extracts and fractions were tested against a panel of nine bacterial and four fungal species. The antiparasitic activity was tested against Leishmania donovani, whereas the anti-inflammatory activity of the compounds was determined by measuring the secretion of interleukin-6 from human-derived macrophages. The same macrophage cell line was used to investigate the cytotoxicity of the compounds. Various extracts and fractions showed antibacterial, antifungal, antiparasitic, and anti-inflammatory activities. The hexanic fraction HF 11-14b was the most interesting fraction with antimicrobial, and anti-inflammatory activities. The benefit of L. racemosa as a traditional medicinal plant was confirmed as shown by its antibacterial, antifungal and anti-inflammatory activities. To the best of our knowledge, this is the first study reporting the biological activities of L. racemosa, including antiparasitic and anti-inflammatory activities.

  5. Antimicrobial, Antiparasitic, Anti-Inflammatory, and Cytotoxic Activities of Lopezia racemosa

    Science.gov (United States)

    Cruz Paredes, Carla; Bolívar Balbás, Paulina; Juárez, Zaida Nelly; Sánchez Arreola, Eugenio; Hernández, Luis Ricardo

    2013-01-01

    The present study investigates the potential benefits of the Mexican medicinal plant Lopezia racemosa (Onagraceae). Extracts and fractions from aerial parts of this plant were assessed to determine their antibacterial, antifungal, antiparasitic, anti-inflammatory and cytotoxic activities in vitro. Aerial parts of the plant were extracted with various solvents and fractionated accordingly. Extracts and fractions were tested against a panel of nine bacterial and four fungal species. The antiparasitic activity was tested against Leishmania donovani, whereas the anti-inflammatory activity of the compounds was determined by measuring the secretion of interleukin-6 from human-derived macrophages. The same macrophage cell line was used to investigate the cytotoxicity of the compounds. Various extracts and fractions showed antibacterial, antifungal, antiparasitic, and anti-inflammatory activities. The hexanic fraction HF 11-14b was the most interesting fraction with antimicrobial, and anti-inflammatory activities. The benefit of L. racemosa as a traditional medicinal plant was confirmed as shown by its antibacterial, antifungal and anti-inflammatory activities. To the best of our knowledge, this is the first study reporting the biological activities of L. racemosa, including antiparasitic and anti-inflammatory activities. PMID:23843731

  6. Antimicrobial, Antiparasitic, Anti-Inflammatory, and Cytotoxic Activities of Lopezia racemosa

    Directory of Open Access Journals (Sweden)

    Carla Cruz Paredes

    2013-01-01

    Full Text Available The present study investigates the potential benefits of the Mexican medicinal plant Lopezia racemosa (Onagraceae. Extracts and fractions from aerial parts of this plant were assessed to determine their antibacterial, antifungal, antiparasitic, anti-inflammatory and cytotoxic activities in vitro. Aerial parts of the plant were extracted with various solvents and fractionated accordingly. Extracts and fractions were tested against a panel of nine bacterial and four fungal species. The antiparasitic activity was tested against Leishmania donovani, whereas the anti-inflammatory activity of the compounds was determined by measuring the secretion of interleukin-6 from human-derived macrophages. The same macrophage cell line was used to investigate the cytotoxicity of the compounds. Various extracts and fractions showed antibacterial, antifungal, antiparasitic, and anti-inflammatory activities. The hexanic fraction HF 11-14b was the most interesting fraction with antimicrobial, and anti-inflammatory activities. The benefit of L. racemosa as a traditional medicinal plant was confirmed as shown by its antibacterial, antifungal and anti-inflammatory activities. To the best of our knowledge, this is the first study reporting the biological activities of L. racemosa, including antiparasitic and anti-inflammatory activities.

  7. A Quantum Chemical and Statistical Study of Cytotoxic Activity of Compounds Isolated from Curcuma zedoaria

    Directory of Open Access Journals (Sweden)

    Omer Abdalla Ahmed Hamdi

    2015-04-01

    Full Text Available A series of 21 compounds isolated from Curcuma zedoaria was subjected to cytotoxicity test against MCF7; Ca Ski; PC3 and HT-29 cancer cell lines; and a normal HUVEC cell line. To rationalize the structure–activity relationships of the isolated compounds; a set of electronic; steric and hydrophobic descriptors were calculated using density functional theory (DFT method. Statistical analyses were carried out using simple and multiple linear regressions (SLR; MLR; principal component analysis (PCA; and hierarchical cluster analysis (HCA. SLR analyses showed that the cytotoxicity of the isolated compounds against a given cell line depend on certain descriptors; and the corresponding correlation coefficients (R2 vary from 0%–55%. MLR results revealed that the best models can be achieved with a limited number of specific descriptors applicable for compounds having a similar basic skeleton. Based on PCA; HCA and MLR analyses; active compounds were classified into subgroups; which was in agreement with the cell based cytotoxicity assay.

  8. Vectorized ferrocenes with estrogens and vitamin D2: synthesis, cytotoxic activity and docking studies†

    Science.gov (United States)

    Vera, José; Gao, Li Ming; Santana, Alberto; Matta, Jaime

    2015-01-01

    Three ferrocene complexes vectorized with estrogens and vitamin D2 were synthesized and fully characterized by spectroscopic, electrochemical and computational methods. The synthesis of these esters was accomplished by reacting ferrocenoyl chloride with the corresponding ROH groups (R = ergocalciferol, estradiol, estrone). The cytotoxicity of these complexes in HT-29 colon cancer and MCF-7 breast cancer cell lines was investigated in vitro. Only ferrocenoyl 17β-hydroxy-estra-1,3,5(10)-trien-3-olate showed good cytotoxic activity in both cell lines, exceeding those of ferrocenium and ferrocene. In MCF-7, ferrocenoyl 17β-hydroxy-estra-1,3,5(10)-trien-3-olate exhibited remarkable IC50, in the low micromolar range. This may be attributed to the presence of the estradiol vector. Docking studies between alpha-estrogen receptor ligand binding site and ferrocenoyl 17β-hydroxy-estra-1,3,5(10)-trien-3-olate revealed some key hydrophobic interactions that might explain the cytotoxic activity of this ester. PMID:21850331

  9. Antimicrobial activity and cytotoxicity of piperazinium- and guanidinium-based ionic liquids

    Energy Technology Data Exchange (ETDEWEB)

    Yu, Jing; Zhang, Shanshan; Dai, Yitong; Lu, Xiaoxing; Lei, Qunfang; Fang, Wenjun, E-mail: qflei@zju.edu.cn

    2016-04-15

    Highlights: • Twelve piperazinium- and guanidinium-based ionic liquids were synthesized and characterized. • Antimicrobial activities of the ionic liquids against E. coli and S. aureus were investigated. • Cytotoxicity on the rat C6 glioma cells (C6) and human embryonic kidney cells (HEK-293) were evaluated. • The ionic liquids with the [BF{sub 4}]{sup −} anion and with benzene ring on cation exhibit relatively high toxicity. - Abstract: Twelve piperazinium- and guanidinium-based ionic liquids (ILs) were synthesized, and characterized by {sup 1}H nuclear magnetic resonance (NMR), thermal gravimetric analyzer (TGA) and differential scanning calorimetry (DSC). The antimicrobial activity and cytotoxicity have been investigated to provide the information whether the newly synthesized ILs are toxic or not. The antimicrobial effects of these ILs on gram negative and gram positive bacteria are evaluated on the basis of the minimum inhibitory concentration (MIC) measurements. The membrane damages of bacteria in the presence of ILs are observed by scanning electron microscopy (SEM). The cytotoxicity data of the ILs on HEK-293 and C6 cells are obtained by MTT cell viability assay. The disruption of cell cycle is analyzed by the flow cytometry. The results show that most of the ILs exhibit low toxicity, and the ILs with tetrafluoroborate anion and with benzene ring on cation are the species with relatively high toxicity among the studied ILs. The fundamental data and results can provide some useful information for the further studies and applications of the ILs.

  10. Cytotoxic constituents of propolis from Myanmar and their structure-activity relationship.

    Science.gov (United States)

    Li, Feng; Awale, Suresh; Tezuka, Yasuhiro; Kadota, Shigetoshi

    2009-12-01

    Thirteen cycloartane-type tritepenes (1-13) and four prenylated flavanones (14-17) isolated from propolis collected in Myanmar, were evaluated for their cytotoxic activity against a panel of six different cancer cell lines; three murine cancer cell lines (colon 26-L5 carcinoma, B16-BL6 melanoma, and Lewis lung carcinoma) and three human cancer cell lines (lung A549 adenocarcinoma, cervix HeLa adenocarcinoma and HT-1080 fibrosarcoma). Among them, a cycloartane-type triterpene, 3alpha,27-dihydroxycycloart-24E-en-26-oic acid (3), showed the most potent cytotoxicity against B16-BL6 cells with an IC(50) value of 5.91 microM, comparable to those of positive controls, doxorubicin (IC(50), 5.66 microM) and 5-fluorouracil (IC(50), 4.88 microM). In addition, (2S)-5,7-dihydroxy-4'-methoxy-8,3'-diprenylflavanone (14) exhibited strong cytotoxicity against all the tested cancer cell lines with the IC(50) values ranging from 14.0 to 26.4 microM. Based on the observed results, the structure-activity relationships are discussed.

  11. Particle Size-Dependent Antibacterial Activity and Murine Cell Cytotoxicity Induced by Graphene Oxide Nanomaterials

    Directory of Open Access Journals (Sweden)

    Lin Zhao

    2016-01-01

    Full Text Available Recent studies have indicated that graphene and its derivative graphene oxide (GO engage in a wide range of antibacterial activities with limited toxicity to human cells. Here, we systematically evaluate the dependence of GO toxicity on the size of the nanoparticles used in treatments: we compare the cytotoxic effects of graphene quantum dots (GQDs, <15 nm, small GOs (SGOs, 50–200 nm, and large GOs (LGOs, 0.5–3 μm. We synthesize the results of bacterial colony count assays and SEM-based observations of morphological changes to assess the antibacterial properties that these GOs bring into effect against E. coli. We also use Live/Dead assays and morphological analysis to investigate changes to mammalian (Murine macrophage-like Raw 264.7 cells induced by the presence of the various GO particle types. Our results demonstrate that LGOs, SGOs, and GQDs possess antibacterial activities and cause mammalian cell cytotoxicity at descending levels of potency. Placing our observations in the context of previous simulation results, we suggest that both the lateral size and surface area of GO particles contribute to cytotoxic effects. We hope that the size dependence elucidated here provides a useful schematic for tuning GO-cell interactions in biomedical applications.

  12. Sirtuin 1-dependent resveratrol cytotoxicity and pro-differentiation activity on breast cancer cells.

    Science.gov (United States)

    Deus, Cláudia M; Serafim, Teresa L; Magalhães-Novais, Silvia; Vilaça, Andreia; Moreira, Ana C; Sardão, Vilma A; Cardoso, Susana M; Oliveira, Paulo J

    2017-03-01

    Sirtuins regulate several processes associated with tumor development. Resveratrol was shown to stimulate sirtuin 1 and 3 (SIRT1/3) activities and to result in cytotoxicity for some tumor types. The relationship between modulation of sirtuin activities, cellular metabolic remodeling and resveratrol cytotoxicity mechanism on breast cancer cells is still an open question. Here, we evaluated whether sirtuin 1 and 3 are involved in resveratrol toxicity and whether resveratrol leads to a metabolic remodeling and cell differentiation. Results using the Extracellular Flux Analyzer indicated that resveratrol inhibits mitochondrial respiration in breast cancer cells. We also demonstrated here for the first time that resveratrol cytotoxic effects on breast cancer cells were modulated by SIRT1 and also involved mitochondrial complex I inhibition. Importantly, we also demonstrated that resveratrol reduced the pool of breast cancer cells with stemness markers through a SIRT1-dependent mechanism. Our data highlights the role of SIRT1 in regulating resveratrol induced differentiation and/or toxicity in breast cancer cells.

  13. The effects of accelerated electrons on Escherichia Coli enterobacteria cytotoxic activity

    Science.gov (United States)

    Oproiu, C.; Martin, D.; Marghitu, S.; Popescu, A. S.; Butan, C.; Toma, M.; Hategan, A.; Dima, V.

    1999-01-01

    Electron beam effects of the cytotoxic capacity of enterotoxin Escherichia coli on “in vitro” cell colonies have been studied. The VERO cell colonies and tumoral epithelial cells HeLa-2 were treated with different concentrations of irradiated and natural entherotoxin (1-1000 μg/mL). The radiation doses used range from 1 to 35 kGy. The irradiation was carried out with ALIN-10 linear accelerator and the dose was measured with calorimetric devices and cellulose triacetate dosimetric films. The accelerated electrons effects were estimated by means of the effect of different absorbed radiation doses on the enterotoxin and on the protein synthesis in cell colonies treated with irradiated enterotoxin. The following results were obtained: a) there is a definite dependence between the electron beam irradiation and effects on cytotoxic activity of the enterotoxin; b) strong inhibition of protein synthesis is produced in cell colonies treated with large amounts of enterotoxin; c) the cytotoxic activity of treated enterotoxin with 35 kGy accelerated electrons is fully suppressed; d) the VERO cells are more sensitive against natural and irradiated enterotoxin, as compared with tumoral epithelial cells HeLa-2.

  14. Cytotoxic Effects of Re-Activated Lunar Dust Stimulant on Human Lung Cells

    Science.gov (United States)

    Upadhyaya, Krishna

    2009-01-01

    Lunar dust has been of significant concern due to various problems observed on the Apollo missions. Reports from astronauts have shown that the dust may have caused eye and nasal irritation as well as possible hay fever like symptoms. As NASA hopes to go to the Moon within the next few years, we hope to understand the possible toxic effects the dust might have. In these studies, we are looking at the effect of "re-activated" lunar dust stimulant on human bronchial cells. A simple grinding analog as a method of simulating micrometeorite crushing on the moon is used to "activate" the dust stimulant, i.e. capable of producing hydroxyl radicals. These radicals could then interact with human cells and may lead to a loss in membrane integrity and cell death. (Castranova, 1994) Cells are exposed to the dust for 6 and 24 hour intervals to assess cytotoxicity. Cytotoxicity is measured by looking at the production of inflammatory cytokines. Cells are exposed to ground and unground stimulant and compared to cytokine production from cells exposed to quartz which have a known toxicity. Here we look at the cytotoxicity of the lunar dust stimulant relative to quartz by measuring the production of inflammatory cytokines.

  15. Comparative analysis of antioxidant, antimicrobiological and cytotoxic activities of native and fermented chamomile ligulate flower extracts.

    Science.gov (United States)

    Cvetanović, Aleksandra; Švarc-Gajić, Jaroslava; Zeković, Zoran; Savić, Saša; Vulić, Jelena; Mašković, Pavle; Ćetković, Gordana

    2015-09-01

    The work investigated differences in apigenin content, as well as in other compounds, and examined the chemical profiles, antioxidant, antimicrobial and cytotoxic effects of extracts obtained from native and fermented chamomile ligulate flowers. Chamomile (Chamomilla recutita L.) has a long history of being used as a medicinal plant due to many health benefits, including antiinflammatory, anticancer, antispasmodic, radical-scavenging effects and others. Apigenin is recognized as one of the most bioactive phenolic compounds in chamomile. In comparison to its bound forms, which include mostly apigenin-7-O-β-glucoside and various acylated forms, the aglycone is attributed with much higher bioactivity. Due to this fact, in this work ligulate florets of chamomile anthodium were subjected to a fermentation process using native chamomile enzymes to hydrolyze bound forms of apigenin to free aglycone. The contents of apigenin and apigenin-7-O-β-glucoside were determined in both fermented and nonfermented samples by UHPLC-MS-MS analysis to define the efficiency of conversion. After defining their chemical profiles, the extracts of fermented and nonfermented chamomile samples were also compared with respect to their antioxidant, antimicrobial and cytotoxic effects. The antioxidant effects of the obtained extracts were defined by electron spin resonance analysis for hydroxyl and superoxide radicals. The antimicrobial activity was defined for eight microbial strains, whereas cytotoxic activity was evaluated using two human cell lines (human cervix carcinoma and human rhabdomyosarcoma) and murine fibroblasts.

  16. Phytochemical study and evaluation of the antimicrobial activity and cytotoxicity of Cuscuta racemosa

    Directory of Open Access Journals (Sweden)

    Helena O. Ferraz

    2011-02-01

    Full Text Available Cuscuta racemosa Mart. is a parasitic plant of the Convolvulaceae family, used in popular medicine as an anti-inflammatory and a diuretic, for stomach and hepatic disorders, and for treating fresh wounds. This plant is popularly known as "cipó-chumbo" and "fios-de-ovos". In this study, it was chemically investigated and tested for its antimicrobial activity and cytotoxicity. The flavonoid and tannin content of the dried plant were 2.79% and 2.01%, respectively. Furthermore, the 4'-methoxyquercetin flavanoid compound was isolated from the ethanolic fraction. The minimum inhibiting concentration in the antimicrobial test was 2.0 mg/ml for Staphylococcus aureus, and a DL50 of 0.231 mg/mL was obtained in the cytotoxicity experiment. The fraction directed to alkaloids was able to eliminate 100% of the brine shrimp used for the test.

  17. Four new steroidal glycosides from Solanum torvum and their cytotoxic activities.

    Science.gov (United States)

    Lu, Yuanyuan; Luo, Jianguang; Huang, Xuefeng; Kong, Lingyi

    2009-01-01

    Two novel C-22 steroidal lactone saponins, namely solanolactosides A, B (1, 2) and two new spirostanol glycosides, namely torvosides M, N (3, 4) were isolated from ethanol extract of aerial parts of Solanum torvum. Their structures were characterized as solanolide 6-O-[alpha-l-rhamnopyranosyl-(1-->3)-O-beta-d-quinovopyranoside] (1), solanolide 6-O-[beta-d-xylopyranosyl-(1-->3)-O-beta-d-quinovopyranoside] (2), yamogenin 3-O-[beta-d-glucopyranosyl-(1-->6)-O-beta-d-glucopyranoside] (3) and neochlorogenin 3-O-[beta-d-glucopyranosyl-(1-->6)-O-beta-d-glucopyranoside] (4) on the basis of spectroscopic analysis. The cytotoxicities of the saponins (1-4) were evaluated in vitro against a panel of human cancer cell lines. Compounds 3 and 4 showed significant cytotoxic activity with the cell lines.

  18. Phytochemical study and evaluation of the antimicrobial activity and cytotoxicity of Cuscuta racemosa

    Directory of Open Access Journals (Sweden)

    Helena O. Ferraz

    2010-11-01

    Full Text Available Cuscuta racemosa Mart. is a parasitic plant of the Convolvulaceae family, used in popular medicine as an anti-inflammatory and a diuretic, for stomach and hepatic disorders, and for treating fresh wounds. This plant is popularly known as "cipó-chumbo" and "fios-de-ovos". In this study, it was chemically investigated and tested for its antimicrobial activity and cytotoxicity. The flavonoid and tannin content of the dried plant were 2.79% and 2.01%, respectively. Furthermore, the 4'-methoxyquercetin flavanoid compound was isolated from the ethanolic fraction. The minimum inhibiting concentration in the antimicrobial test was 2.0 mg/ml for Staphylococcus aureus, and a DL50 of 0.231 mg/mL was obtained in the cytotoxicity experiment. The fraction directed to alkaloids was able to eliminate 100% of the brine shrimp used for the test.

  19. A new coumarin and cytotoxic activities of constituents from Cinnamomum cassia.

    Science.gov (United States)

    Ngoc, Tran Minh; Nhiem, Nguyen Xuan; Khoi, Nguyen Minh; Son, Doan Cao; Hung, Tran Viet; Van Kiem, Phan

    2014-04-01

    A new coumarin derivative, coumacasia (1) and eight known compounds, coumarin (2), cinnamaldehyde (3), 2-methoxycinnamaldehyde (4), 2-hydroxycinnamaldehyde (5), coniferaldehyde (6), cinnamic acid (7), 2-hydroxycinnamic acid (8), and cinnamic alcohol (9), were isolated from the methanol extract of Cinnamomum cassia. Their structures were elucidated by spectral data and by comparison with the reported literature. The cytotoxic activities of compounds 1-9 were evaluated with two human cancer cell lines, HL-60 and A-549. Compound 1 showed growth inhibitory effects in the HL-60 and A-549 cell lines with IC50 values of 8.2 +/- 0.5 and 11.3 +/- 1.1 microM, respectively. Compounds 3-6, and 8 exhibited moderate cytotoxicity with IC50 values ranging from 20.5 to 65.6 microM.

  20. Cytotoxicity and antiviral activities of Asplenium nidus, Phaleria macrocarpa and Eleusine indica

    Science.gov (United States)

    Tahir, Mariya Mohd; Ibrahim, Nazlina; Yaacob, Wan Ahmad

    2014-09-01

    Three local medicinal plants namely Asplenium nidus (langsuyar), Eleusine indica (sambau) and Phaleria macrocarpa (mahkota dewa) were screened for the cytotoxicity and antiviral activities. Six plant extracts were prepared including the aqueous and methanol extracts from A. nidus leaf and root, aqueous extract from dried whole plant of E. indica and methanol extract from P. macrocarpa fruits. Cytotoxicity screening in Vero cell line by MTT assay showed that the CC50 values ranged from 15 to 60 mg/mL thus indicating the safety of the extracts even at high concentrations. Antiviral properties of the plant extracts were determined by plaque reduction assay. The EC50 concentrations were between 3.2 to 47 mg/mL. The selectivity indices (SI = CC50/EC50) of each tested extracts ranged from 4.3 to 63.25 indicating the usefulness of the extracts as potential antiviral agents.

  1. Monoterpenoid Indole Alkaloids from Alstonia yunnanensis and Their Cytotoxic and Anti-inflammatory Activities

    Directory of Open Access Journals (Sweden)

    Guobiao Liang

    2012-11-01

    Full Text Available The 80% ethanol extract of Alstonia yunnanensis afforded five new monoterpenoid indole alkaloids: 11-hydroxy-6,7-epoxy-8-oxo-vincadifformine (1, 14-chloro-15-hydroxy- vincadifformine (2, perakine N4-oxide (3, raucaffrinoline N4-oxide (4, and vinorine N1,N4-dioxide (5, together with three known compounds: 11-methoxy-6,7-epoxy-8-oxo- vincadifformine (6, vinorine N4-oxide (7 and vinorine (8. The structures of the isolated compounds were established based on 1D and 2D (1H-1H-COSY, HMQC, HMBC, and ROESY NMR spectroscopy, in addition to high resolution mass spectrometry. The isolated compounds were tested in vitro for cytotoxic potential against seven tumor cell lines and anti-inflammatory activities. Compounds 3, 4 and 7 exhibited weak cytotoxicity against the tested cell lines and selective inhibition of Cox-2 (>85%.

  2. Silver nanoparticles: Antimicrobial activity, cytotoxicity, and synergism with N-acetyl cysteine.

    Science.gov (United States)

    Hamed, Selwan; Emara, Mohamed; Shawky, Riham M; El-Domany, Ramadan A; Youssef, Tareq

    2017-08-01

    The fast progression of nanotechnology has led to novel therapeutic interventions. Antimicrobial activities of silver nanoparticles (Ag NPs) were tested against standard ATCC strains of Staphylococcus aureus (ATCC 9144), Escherichia coli (O157:H7), Pseudomonas aeruginosa (ATCC 27853), and Candida albicans (ATCC 90028) in addition to 60 clinical isolates collected from cancer patients. Antimicrobial activity was tested by disk diffusion method and MIC values for Ag NPs alone and in combination with N-acetylcysteine (NAC) against tested pathogens were determined by broth microdilution method. Ag NPs showed a robust antimicrobial activity against all tested pathogens and NAC substantially enhanced the antimicrobial activity of Ag NPs against all tested pathogens. Synergism between Ag NPs and NAC has been confirmed by checkerboard assay. The effect of Ag NPs on tested pathogens was further scrutinized by Transmission Electron Microscope (TEM) which showed disruption of cell wall in both bacteria and fungi. Ag NPs abrogated the activity of respiratory chain dehydrogenase of all tested pathogens and released muramic acid content from S. aureus in culture. The cytotoxic effect of Ag NPs alone and in combination with NAC was examined using human HepG2 cells and this revealed no cytotoxicity at MIC values of Ag NPs and interestingly, NAC reduced the cytotoxic effect of Ag NPs at concentrations higher than their MIC values. Taken together, Ag NPs have robust antimicrobial activity and NAC substantially enhances their antimicrobial activities against MDR pathogens which would provide a novel safe, effective, and inexpensive therapeutic approach to control the prevalence of MDR pathogens. © 2017 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

  3. In Vitro Cytotoxic Activity of Origanum vulgare L. on HCT-116 and MDA-MB-231 Cell Lines

    Science.gov (United States)

    Grbović, Filip; Stanković, Milan S.; Ćurčić, Milena; Đorđević, Nataša; Šeklić, Dragana; Topuzović, Marina; Marković, Snežana

    2013-01-01

    In the present investigation, we examined the cytotoxic effect of methanolic extract from Origanum vulgare on HCT-116 and MDA-MB-231 cell line in vitro. In order to determine the cytotoxic effects we used an MTT viability assay. The results showed that cell growth is significantly lower in extract treated cells compared to untreated control. The effect of inhibition of cell growth was higher in the treatment of HCT-116 cell line than in MDA-MB-231. Based on the results it is determined that O. vulgare is a significant source of biologically active substances that have cytotoxic and antiproliferative activity in vitro. PMID:27137381

  4. Mutagenic, Anti-Mutagenic and Cytotoxic Activities of Artediffusin (Tehranolide, in vitro, extracted from Artemisia diffusa

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    Mahboubeh Taherkhani

    2015-06-01

    Full Text Available Background: Artediffusin is a sesquiterpene lactone with an endoperoxide group which has been isolated from Artemisia diffusa. Artemisia has always been of great botanical and pharmaceutical interest and is useful in traditional medicines for the treatment of a variety of diseases and complaints. The aims of the present study were to evaluate the cytotoxic, mutagenic and anti-mutagenic activities of Artediffusin (Tehranolide extracted from Artemisia diffusa. Methods: Cytotoxicity was measured using a modified MTT assay on normal human lymphocytes and cancer cells. The mutagenic and anti-mutagenic activities of Artediffusin were evaluated using the Salmonella typhimurium tester strains TA98 and TA100 with and without metabolic activation S9. Results: 28μg/ml concentration of Artediffusin inactivated 77.73±0.78% of HeLa cells activity and 5600µg/ml concentration of Artediffusin inactivated 28.79±1.82% of lymphocytes activity. The maximum percentage of anti-mutagenic activity of Artediffusin was observed in the strain of S. typhimurium TA98, with the presence of metabolic activation S9. Conclusion: Artediffusin may be exploited as a natural anti-cancer and anti-mutagenic agent with low adverse side effects.

  5. Chemical Composition, Antimicrobial, Cytotoxic and Antiplasmodial Activities of Three Sponges from Buton Islands, Indonesia

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    Masteria Yunovilsa Putra

    2017-08-01

    Full Text Available GC-MS analysis of the crude extracts of three different species of Indonesian marine sponges has been carried out for identification of bioactive compounds. The GC-MS analysis from Haliclona (Gellius sp., Lamellodysidea herbacea, and Spheciospongia inconstans revealed the presence of 23, 21, 19 various compounds, respectively and mainly sterols and fatty acids. All the sponge species has been evaluated for antimicrobial activities, cytotoxicity using brine shrimp lethality bioassay and heme polymerization inhibitory activity assay for antiplasmodial activity. In this study, all the sponge species showed antimicrobial activities against at leastone of the test strains. Among them, the extract of sponge Lamellodysidea herbacea displayed activity against two Gram-positive bacteria (S. aureus and B. subtilis and the Gram-negative bacteria V. cholerae, with inhibition zones of 10.3, 9.2 and 9.5 mm, respectively. The sponge Haliclona (Gellius sp., showed significant activity against fungal pathogen C. albicans. The sponge Haliclona (Gellius sp., displayed the ability to inhibit heme polymerization indicating an anti-Plasmodium function and also showed potent cytotoxic activity against the brine shrimp Artemia sp.   Keywords: GC-MS analysis, antimicrobial, sponges,bioactive

  6. Cytotoxicity and hemolytic activity of jellyfish Nemopilema nomurai (Scyphozoa: Rhizostomeae) venom.

    Science.gov (United States)

    Kang, Changkeun; Munawir, Al; Cha, Mijin; Sohn, Eun-Tae; Lee, Hyunkyoung; Kim, Jong-Shu; Yoon, Won Duk; Lim, Donghyun; Kim, Euikyung

    2009-07-01

    The recent bloom of a giant jellyfish Nemopilema nomurai has caused a danger to sea bathers and fishery damages in the waters of China, Korea, and Japan. The present study investigated the cytotoxic and hemolytic activities of crude venom extract of N. nomurai using a number of in vitro assays. The jellyfish venom showed a much higher cytotoxic activity in H9C2 heart myoblast than in C2C12 skeletal myoblast (LC(50)=2 microg/mL vs. 12 microg/mL, respectively), suggesting its possible in vivo selective toxicity on cardiac tissue. This result is consistent with our previous finding that cardiovascular function is a target of the venom. In order to determine the stability of N. nomurai venom, its cytotoxicity was examined under the various temperature and pH conditions. The activity was relatively well retained at low environmental temperature (or=60 degrees C). In pH stability test, the venom has abruptly lost its activity at low pH environment (pHactivity was not significantly affected even at the highest pH environment tested (pHactivity of the venom was examined using the erythrocytes of cat, dog, human, rabbit and rat. Venom concentration-dependent hemolysis could be observed from 10 microg/mL of protein equivalents or higher with variable potencies in different species, among which dog erythrocyte was the most susceptible to the venom (EC(50)=151 microg/mL). SDS-PAGE analysis of N. nomurai venom showed the molecules of 20-40 kDa and 10-15 kDa appeared to be the major protein components of the venom.

  7. Amazon emulsions as cavity cleansers: antibacterial activity, cytotoxicity and changes in human tooth color

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    Cristiane Coelho De Bari

    Full Text Available ABSTRACT The copaiba oleoresin, Copaifera multijuga Hayne, Fabaceae, is a phytotherapeutic agent with antimicrobial activity. This study evaluated the antibacterial activity and cytotoxicity of, and tooth color changes caused by four copaiba oil emulsions (Emulsion 1, 10% CM; Emulsion 2, 10% C. multijuga + 1% biotech product; Emulsion 3, 30% C. multijuga; and Emulsion 4, 30% C. multijuga + 1% biotech product. The antibacterial activities against microorganisms causing dental caries (Streptococcus mutans ATCC25175, S. oralis ATCC10557, S. salivarius ATCC7073, and Lactobacillus casei ATCC7469 were tested using three parameters: minimum inhibitory concentration, minimum bactericidal concentration, and cell viability by fluorescence microscopy. The emulsions were assessed for cytotoxicity by means of the hemolytic assay and cell culture (murine fibroblast cells NHI3T3 using Alamar BlueTM. The dentin color change caused by the emulsions was examined at 10 s, 30 s, and 10 min. The emulsions showed antibacterial activity against the microorganisms tested with an MIC of 125 µl/ml. The minimum bactericidal concentration was higher than minimum inhibitory concentration for the tested microorganism and the fluorescence confirmed that the cells were viable at minimum inhibitory concentration values. The emulsions had a hemolytic activity of 71.16% (Emulsion 3 and 44.67% (Emulsion 4 at a concentration of 30 µl/ml. In cell culture assay, NHI-3T3 cells treated with the emulsions showed 6–16% viability. Emulsion 1 caused clinically imperceptible color change in dentin at 10 s (ΔE = 3.21, Emulsion 2 at 30 s (ΔE = 2.70 and 10 min (ΔE = 3.08, and Emulsion 4 at 10 min (ΔE = 3.03. Emulsion 3 caused color change at all times tested. This research documented positive data regarding antibacterial activity, cytotoxicity, and tooth color changes when using copaiba oleoresin emulsions, showing its potential for use in dentistry.

  8. Comparative Analysis of Immune Cells Activation and Cytotoxicity upon Exposure Pathogen and Glycoconjugates

    Science.gov (United States)

    Saheb, Entsar; Tarasenko, Olga

    2010-04-01

    Peripheral mononuclear cells (PMNC) including macrophages are key players in the immune responses against pathogens. Any infection could be attenuated if PMNC would be activated and capable to kill pathogen on exposure. It was shown that glycoconjugates (GCs) play an important role in adhesion to, activation, and recognition of pathogens. Nitric oxide (NO) is a regulatory molecule released by immune cells against pathogens that include bacteria, protozoa, helminthes, and fungi. NO is a highly reactive and diffusible molecule that controls replication or intracellular killing of pathogens during infection and immune responses against infections caused by pathogens. Avirulent Bacillus anthracis Sterne spores were used as a model in our study. The purpose of this study was two-fold: A) to analyze PMNC activation through NO production and B) to determine the cytotoxicity effect based on lactate dehydrogenase (LDH) upon exposure to pathogen exerted by GCs. The latter were used "prior to," "during," and "following" PMNC exposure to pathogen in order to modulate immune responses to spores during phagocytosis. Post-phagocytosis study involved the assessment of NO and LDH release by macrophages upon exposure to spores. Results have shown that untreated PMNC released low levels of NO. However, in the presence of GCs, PMNC were activated and produced high levels of NO under all experimental conditions. In addition, the results showed that GC1, GC3 are capable of increasing PMNC activity as evidenced by higher NO levels under the "prior," "during" and "following" to pathogen exposure conditions. On the other hand, GCs were capable of controlling cytotoxicity and decreased LDH levels during phagocytosis of spores. Our findings suggest that GCs stimulate NO production by activating PMNC and decrease cytotoxicity caused by pathogens on PMNC.

  9. Alterations in Activation, Cytotoxic Capacity and Trafficking Profile of Peripheral CD8 T Cells in Young Adult Binge Drinkers

    OpenAIRE

    José Luis Zaldivar Fujigaki; América Guadalupe Arroyo Valerio; Juan Carlos López Alvarenga; Esperanza Gabriela Gutiérrez Reyes; David Kershenobich; Joselin Hernández Ruiz

    2015-01-01

    Background Excess of alcohol consumption is a public health problem and has documented effects on the immune system of humans and animals. Animal and in vitro studies suggest that alcohol abuse changes CD8 T cell (CD8) characteristics, however it remains unknown if the CD8 profile of binge drinkers is different in terms of activation, trafficking and cytotoxic capacity. Aim To analyze the peripheral CD8 cytotoxic capacity, activation and trafficking phenotypic profile of Mexican young adults ...

  10. Role of phenylalanine and valine10 residues in the antimicrobial activity and cytotoxicity of piscidin-1.

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    Eunjung Lee

    Full Text Available Piscidin-1 (Pis-1 is a linear antibacterial peptide derived from mast cells of aquacultured hybrid striped bass that comprises 22 amino acids with a phenylalanine-rich amino-terminus. Pis-1 exhibits potent antibacterial activity against pathogens but is not selective for distinguishing between bacterial and mammalian cells. To determine the key residues for its antibacterial activity and those for its cytotoxicity, we investigated the role of each Phe residue near the N-terminus as well as the Val10 residue located near the boundary of the hydrophobic and hydrophilic sectors of the helical wheel diagram. Fluorescence dye leakage and tryptophan fluorescence experiments were used to study peptide-lipid interactions, showing comparable depths of insertion of substituted peptides in different membranes. Phe2 was found to be the most deeply inserted phenylalanine in both bacterial- and mammalian-mimic membranes. Each Phe was substituted with Ala or Lys to investigate its functional role. Phe2 plays key roles in the cytotoxicity as well as the antibacterial activities of Pis-1, and Phe6 is essential for the antibacterial activities of Pis-1. We also designed and synthesized a piscidin analog, Pis-V10K, in which Lys was substituted for Val10, resulting in an elevated amphipathic α-helical structure. Pis-V10K showed similar antibacterial activity (average minimum inhibitory concentration (MIC  = 1.6 µM to Pis-1 (average MIC  = 1.5 µM. However, it exhibited much lower cytotoxicity than Pis-1. Lys10-substituted analogs, Pis-F1K/V10K, Pis-F2K/V10K, and Pis-F6K/V10K in which Lys was substituted for Phe retained antibacterial activity toward standard and drug-resistant bacterial strains with novel bacterial cell selectivity. They exert anti-inflammatory activities via inhibition of nitric oxide production, TNF-α secretion, and MIP-1 and MIP-2 production. They may disrupt the binding of LPS to toll-like receptors, eventually suppressing MAPKs

  11. Blainvillea rhomboidea: chemical constituents and cytotoxic activity; Blainvillea rhomboidea: constituintes quimicos e atividade citotoxica

    Energy Technology Data Exchange (ETDEWEB)

    Gomes, Regina Ferreira; Santos, Helcio Silva dos; Albuquerque, Maria Rose Jane R., E-mail: rjane_7@hotmail.co [Universidade Estadual Vale do Acarau, Sobral, CE (Brazil). Centro de Ciencias Exatas e Tecnologia. Coord. de Quimica; Pessoa, Otilia Deusdenia L. [Universidade Federal do Ceara (DQOI/UFC), Fortaleza (Brazil). Dept. de Quimica Organica e Inorganica; Lotufo, Leticia V. Costa; Pessoa, Claudia do O; Moraes, Manoel Odorico de; Rodrigues, Felipe A. R. [Universidade Federal do Ceara (UFC), Fortaleza (Brazil). Dept. de Fisiologia e Farmacologia

    2010-07-01

    The phytochemical investigation of the ethanol extract from the aerial parts of Blainvillea rhomboidea (Asteraceae) resulted in the isolation and characterization of 8-tigloyloxy-grazielia acid, together with the flavonoids derrone, acacetin, luteolin and luteolin 7-methyl ether, and p-(1-methyl-ethan-1-ol)-phenol. The structures of all compounds were determined by spectroscopic methods ({sup '}H and {sup 13}C NMR and HREIMS) and comparison with published spectral data. The flavonoids luteolin and 7-O-metyl-luteolin, isolated from the active dichloromethane fraction, showed moderate cytotoxic activity. (author)

  12. Quinones and coumarins from Ajania salicifolia and their radical scavenging and cytotoxic activity.

    Science.gov (United States)

    Wu, Hong-Ru; Zhang, Wei; Pang, Xiao-Yan; Gong, Yuan; Obulqasim, Xian Muxinuer U; Li, Hong-Fang; Zhu, Ying

    2015-01-01

    1,4-Naphthoquinone (1) and a new coumarin (3) were isolated from Ajania salicifolia, together with two known compounds (2, 4). The structures and stereochemistry of new compounds were elucidated using spectroscopic methods. Two compounds exhibited potent ABTS cation radical scavenging activities with IC50 values ranging 7.97-8.44 μM. Two quinones (1, 2) exhibited moderate cytotoxic activity against the human cancer cell lines (Hela, HepG2, and K562) with IC50 values of 11.24-35.15 μM in vitro. This is the first report of naphthoquinone in the genus Ajania.

  13. Evaluation of cytotoxic and anti-inflammatory activities of extracts and lectins from Moringa oleifera seeds.

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    Larissa Cardoso Corrêa Araújo

    Full Text Available BACKGROUND: The extract from Moringa oleifera seeds is used worldwide, especially in rural areas of developing countries, to treat drinking water. M. oleifera seeds contain the lectins cmol and WSMoL, which are carbohydrate-binding proteins that are able to reduce water turbidity because of their coagulant activity. Studies investigating the ability of natural products to damage normal cells are essential for the safe use of these substances. This study evaluated the cytotoxic and anti-inflammatory properties of the aqueous seed extract, the extract used by population to treat water (named diluted seed extract in this work, and the isolated lectins cmol and WSMoL. METHODOLOGY/PRINCIPAL FINDINGS: The data showed that the aqueous seed extract and cmol were potentially cytotoxic to human peripheral blood mononuclear cells, while WSMoL and diluted seed extract were not cytotoxic. The M. oleifera aqueous seed extract and the lectins cmol and WSMoL were weakly/moderately cytotoxic to the NCI-H292, HT-29 and HEp-2 cancer cell lines and were not hemolytic to murine erythrocytes. Evaluation of acute toxicity in mice revealed that the aqueous seed extract (2.000 mg/kg did not cause systemic toxicity. The aqueous seed extract, cmol and WSMoL (6.25 µg/mL and diluted seed extract at 50 µg/mL exhibited anti-inflammatory activity on lipopolyssaccharide-stimulated murine macrophages by regulating the production of nitric oxide, TNF-α and IL-1β. The aqueous seed extract reduced leukocyte migration in a mouse model of carrageenan-induced pleurisy; the myeloperoxidase activity and nitric oxide, TNF-α and IL-1β levels were similarly reduced. Histological analysis of the lungs showed that the extract reduced the number of leukocytes. CONCLUSION/SIGNIFICANCE: This study shows that the extract prepared according to folk use and WSMoL may be non-toxic to mammalian cells; however, the aqueous seed extract and cmol may be cytotoxic to immune cells which may explain

  14. Evaluation of cytotoxic and anti-inflammatory activities of extracts and lectins from Moringa oleifera seeds.

    Science.gov (United States)

    Araújo, Larissa Cardoso Corrêa; Aguiar, Jaciana Santos; Napoleão, Thiago Henrique; Mota, Fernanda Virgínia Barreto; Barros, André Luiz Souza; Moura, Maiara Celine; Coriolano, Marília Cavalcanti; Coelho, Luana Cassandra Breitenbach Barroso; Silva, Teresinha Gonçalves; Paiva, Patrícia Maria Guedes

    2013-01-01

    The extract from Moringa oleifera seeds is used worldwide, especially in rural areas of developing countries, to treat drinking water. M. oleifera seeds contain the lectins cmol and WSMoL, which are carbohydrate-binding proteins that are able to reduce water turbidity because of their coagulant activity. Studies investigating the ability of natural products to damage normal cells are essential for the safe use of these substances. This study evaluated the cytotoxic and anti-inflammatory properties of the aqueous seed extract, the extract used by population to treat water (named diluted seed extract in this work), and the isolated lectins cmol and WSMoL. The data showed that the aqueous seed extract and cmol were potentially cytotoxic to human peripheral blood mononuclear cells, while WSMoL and diluted seed extract were not cytotoxic. The M. oleifera aqueous seed extract and the lectins cmol and WSMoL were weakly/moderately cytotoxic to the NCI-H292, HT-29 and HEp-2 cancer cell lines and were not hemolytic to murine erythrocytes. Evaluation of acute toxicity in mice revealed that the aqueous seed extract (2.000 mg/kg) did not cause systemic toxicity. The aqueous seed extract, cmol and WSMoL (6.25 µg/mL) and diluted seed extract at 50 µg/mL exhibited anti-inflammatory activity on lipopolyssaccharide-stimulated murine macrophages by regulating the production of nitric oxide, TNF-α and IL-1β. The aqueous seed extract reduced leukocyte migration in a mouse model of carrageenan-induced pleurisy; the myeloperoxidase activity and nitric oxide, TNF-α and IL-1β levels were similarly reduced. Histological analysis of the lungs showed that the extract reduced the number of leukocytes. This study shows that the extract prepared according to folk use and WSMoL may be non-toxic to mammalian cells; however, the aqueous seed extract and cmol may be cytotoxic to immune cells which may explain the immunosuppressive potential of the extract.

  15. Evaluation of Cytotoxic and Anti-Inflammatory Activities of Extracts and Lectins from Moringa oleifera Seeds

    Science.gov (United States)

    Araújo, Larissa Cardoso Corrêa; Aguiar, Jaciana Santos; Napoleão, Thiago Henrique; Mota, Fernanda Virgínia Barreto; Barros, André Luiz Souza; Moura, Maiara Celine; Coriolano, Marília Cavalcanti; Coelho, Luana Cassandra Breitenbach Barroso; Silva, Teresinha Gonçalves; Paiva, Patrícia Maria Guedes

    2013-01-01

    Background The extract from Moringa oleifera seeds is used worldwide, especially in rural areas of developing countries, to treat drinking water. M. oleifera seeds contain the lectins cmol and WSMoL, which are carbohydrate-binding proteins that are able to reduce water turbidity because of their coagulant activity. Studies investigating the ability of natural products to damage normal cells are essential for the safe use of these substances. This study evaluated the cytotoxic and anti-inflammatory properties of the aqueous seed extract, the extract used by population to treat water (named diluted seed extract in this work), and the isolated lectins cmol and WSMoL. Methodology/Principal Findings The data showed that the aqueous seed extract and cmol were potentially cytotoxic to human peripheral blood mononuclear cells, while WSMoL and diluted seed extract were not cytotoxic. The M. oleifera aqueous seed extract and the lectins cmol and WSMoL were weakly/moderately cytotoxic to the NCI-H292, HT-29 and HEp-2 cancer cell lines and were not hemolytic to murine erythrocytes. Evaluation of acute toxicity in mice revealed that the aqueous seed extract (2.000 mg/kg) did not cause systemic toxicity. The aqueous seed extract, cmol and WSMoL (6.25 µg/mL) and diluted seed extract at 50 µg/mL exhibited anti-inflammatory activity on lipopolyssaccharide-stimulated murine macrophages by regulating the production of nitric oxide, TNF-α and IL-1β. The aqueous seed extract reduced leukocyte migration in a mouse model of carrageenan-induced pleurisy; the myeloperoxidase activity and nitric oxide, TNF-α and IL-1β levels were similarly reduced. Histological analysis of the lungs showed that the extract reduced the number of leukocytes. Conclusion/Significance This study shows that the extract prepared according to folk use and WSMoL may be non-toxic to mammalian cells; however, the aqueous seed extract and cmol may be cytotoxic to immune cells which may explain the

  16. In vitro cytotoxic and antioxidant activities of phenolic components of Algerian Achillea odorata leaves

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    Hanane Boutennoun

    2017-03-01

    Full Text Available In this study, methanol extract from Achillea odorata was evaluated for its phenolic contents using Folin–Ciocalteu reagent, and antioxidant activity using: 1,1-diphenyl-2-picrylhidrazyl (DPPH radical scavenging activity, reducing activity of H2O2 and ferric reducing power assay. The total phenolic content was determined as gallic acid (GAE equivalent. Flavonoids and flavonols contents were determined as quercetin (QE equivalents. The cytotoxicity of the plant extract was tested against three tumor cell lines: MCF-7, Hep2 and WEHI using 3-(4,5-dimethyl thiazol-2-yl-2,5-diphynyl tetrazolium bromide (MTT assay. Preliminary screening was concluded in the presence of substances with large therapeutic values. The total phenolic content confirmed the presence of total phenolics in the extract and showed strong association with antioxidant activity. An important content of flavonoids and flavonols was also detected. The results of the antioxidant activities obtained indicate that A. odorata recorded a good capacity. For the cytotoxic activity, the results showed the plant extract significantly inhibited tumor cell growth and colony formation at various concentrations.

  17. Kinetics and mechanism of antibacterial activity and cytotoxicity of Ag-RGO nanocomposite.

    Science.gov (United States)

    Moghayedi, Marjan; Goharshadi, Elaheh K; Ghazvini, Kiarash; Ahmadzadeh, Hossein; Ranjbaran, Laleh; Masoudi, Raheleh; Ludwig, Ralf

    2017-08-04

    Nowadays, nanomaterials with remarkable antibacterial activity and low cytotoxicity attract much interest in research. By considering the antibacterial activity of Ag and graphene oxide (GO), the Ag-RGO nanocomposite was prepared by a one-pot and facile technique and it was used to evaluate its antibacterial activity and cytotoxicity against Escherichia coli and glioblastoma cancer cells (U87MG), respectively. The antibacterial activity was studied by micro-dilution and colony counting methods to investigate cell viability. The viability of glioblastoma cells was determined using MTT assay. Since MIC and MBC values of the nanocomposite are 20 and 40μg/mL, respectively, it acts as a bactericidal agent. The antibacterial properties of nanocomposite are time and concentration dependent. The kinetics and mechanism of the antibacterial activity of the nanocomposite were investigated. The antibacterial activity for Ag-RGO nanocomposite is induced by capturing-killing process. From the results, we concluded that Ag-RGO nanocomposite can simultaneously induce apoptosis. Our results bring up a new plan for the use of silver nanoparticles in the form of nanocomposite with reduced graphene oxide in antibacterial applications. Also, Ag-RGO nanocomposite can reduce the viability of U87MG in a dose dependent manner which may show its anticancer potential. Copyright © 2017 Elsevier B.V. All rights reserved.

  18. Diarylheptanoid from Pleuranthodium racemigerum with in vitro prostaglandin E(2) inhibitory and cytotoxic activity.

    Science.gov (United States)

    Wohlmuth, Hans; Deseo, Myrna A; Brushett, Don J; Thompson, Dion R; Macfarlane, Graham; Stevenson, Lesley M; Leach, David N

    2010-04-23

    Bioactivity-guided fractionation of an ethanolic extract of the rhizome of Pleuranthodium racemigerum, a tropical Zingiberaceae species from Northeastern Australia, resulted in the isolation and structural elucidation of 1-(4''-methoxyphenyl)-7-(4'-hydroxyphenyl)-(E)-hept-2-ene (1), a new diarylheptanoid related to curcumin. Compound 1 was a fairly potent inhibitor of prostaglandin E(2) production in 3T3 murine fibroblasts (IC(50) approximately 34 microM) and also displayed moderate cytotoxicity against this cell line (IC(50) = 52.8 microM). The compound also demonstrated cytotoxic activity against the P388D1 murine lymphoblast cell line (IC(50) = 117.0 microM) and four human cell lines: Caco-2 colonic adenocarcinoma (IC(50) = 44.8 microM), PC3 prostate adenocarcinoma (IC(50) = 23.6 microM), HepG2 hepatocyte carcinoma (IC(50) = 40.6 microM), and MCF7 mammary adenocarcinoma (IC(50) = 56.9 microM). The cytotoxicity of compound 1 closely resembled that of curcumin, in terms of both IC(50) values and dose-response curves.

  19. Volatile compounds analysis and antioxidant, antimicrobial and cytotoxic activities of Mindium laevigatum

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    Abdolrasoul Haghir Ebrahimabadi

    2016-12-01

    Full Text Available Objective(s: Mindium laevigatum is an endemic plant of Iran and Turkey and is widely used as blood purifier, antiasthma and antidyspnea in traditional medicine. Chemical composition of volatile materials of the plant and its antioxidant, antimicrobial and cytotoxic activities were reported in this study. Materials and Methods: Simultaneous distillation-extraction (SDE and GC-Mass-FID analysis were used for the plant volatile materials chemical composition identification and quantification. Several antioxidant tests including DPPH radical scavenging, hydrogen peroxide scavenging, reducing power determination, β-carotene-linoleic acid and total phenolic content tests were used for antioxidant activity evaluation. Antimicrobial and anticancer activities were also estimated using microbial strains, cancer cell lines and brine shrimp larva. Results: GC-Mass-FID analysis of volatile samples showed a total of 74 compounds of which palmitic acid (7.4-33.7%, linoleic acid (6.6-18.6%, heneicosane (1.3-9.6% and myristic acid (1.4-6.0% were detected as main volatile components. Moderate to good results were recorded for the plant in              β-carotene-linoleic acid test. Total phenolic content of the extracts as gallic acid equivalents were estimated in the range of 15.7 to 79.6 μg/mg. Some microbial strains showed moderate sensitivities to plant extracts. Brine shrimp lethality test and cytotoxic cancer cell line assays showed mild cytotoxic activities for the plant. Conclusion: Moderate to good antioxidant activities in β-carotene-linoleic acid test and presence of considerable amounts of unsaturated hydrocarbons may explain the plant traditional use in asthma and dyspnea. These findings also candidate it as a good choice for investigating its possible modern medical applications.

  20. Antioxidant, antibacterial, cytotoxic, and apoptotic activity of stem bark extracts of Cephalotaxus griffithii Hook. f.

    Science.gov (United States)

    Moirangthem, Dinesh Singh; Talukdar, Narayan Chandra; Kasoju, Naresh; Bora, Utpal

    2012-04-03

    Cephalotaxus spp. are known to possess various therapeutic potentials. Cephalotaxus griffithii, however, has not been evaluated for its biological potential. The reason may be the remoteness and inaccessibility of the habitat where it is distributed. The main aim of this study was to: (1) evaluate multiple biological potentials of stem bark of C. griffithii, and (2) identify solvent extract of stem bark of C. griffithii to find the one with the highest specific biological activity. Dried powder of stem bark of C. griffithii was exhaustively extracted serially by soaking in petroleum ether, acetone and methanol to fractionate the chemical constituents into individual fractions or extracts. The extracts were tested for total phenolic and flavonoid content, antioxidant (DPPH radical scavenging, superoxide radical scavenging, and reducing power models), antibacterial (disc diffusion assay on six bacterial strains), cytotoxic (MTT assay on HeLa cells), and apoptotic activity (fluorescence microscopy, DNA fragmentation assay, and flow cytometry on HeLa cells). Among the three extracts of stem bark of C. griffithii, the acetone extract contained the highest amount of total phenolics and flavonoids and showed maximum antioxidant, antibacterial, cytotoxic (IC50 of 35.5 ± 0.6 μg/ml; P activity, followed by the methanol and petroleum ether extracts. However, there was no significant difference observed in IC50 values (DPPH scavenging assay) of the acetone and methanol extracts and the positive control (ascorbic acid). In contrast, superoxide radical scavenging assay-based antioxidant activity (IC50) of the acetone and methanol extracts was significantly lower than the positive control (P phenolic and flavonoid content present in stem bark of C. griffithii extracts was responsible for the high antioxidant, cytotoxic, and apoptotic activity (P extract of stem bark of C. griffithii for specific bioactivity.

  1. Large-scale isolation and cytotoxicity of extracellular vesicles derived from activated human natural killer cells.

    Science.gov (United States)

    Jong, Ambrose Y; Wu, Chun-Hua; Li, Jingbo; Sun, Jianping; Fabbri, Muller; Wayne, Alan S; Seeger, Robert C

    2017-01-01

    Extracellular vesicles (EVs) have been the focus of great interest, as they appear to be involved in numerous important cellular processes. They deliver bioactive macromolecules such as proteins, lipids, and nucleic acids, allowing intercellular communication in multicellular organisms. EVs are secreted by all cell types, including immune cells such as natural killer cells (NK), and they may play important roles in the immune system. Currently, a large-scale procedure to obtain functional NK EVs is lacking, limiting their use clinically. In this report, we present a simple, robust, and cost-effective method to isolate a large quantity of NK EVs. After propagating and activating NK cells ex vivo and then incubating them in exosome-free medium for 48 h, EVs were isolated using a polymer precipitation method. The isolated vesicles contain the tetraspanin CD63, an EV marker, and associated proteins (fibronectin), but are devoid of cytochrome C, a cytoplasmic marker. Nanoparticle tracking analysis showed a size distribution between 100 and 200 nm while transmission electron microscopy imaging displayed vesicles with an oval shape and comparable sizes, fulfilling the definition of EV. Importantly, isolated EV fractions were cytotoxic against cancer cells. Furthermore, our results demonstrate for the first time that isolated activated NK (aNK) cell EVs contain the cytotoxic proteins perforin, granulysin, and granzymes A and B, incorporated from the aNK cells. Activation of caspase -3, -7 and -9 was detected in cancer cells incubated with aNK EVs, and caspase inhibitors blocked aNK EV-induced cytotoxicity, suggesting that aNK EVs activate caspase pathways in target cells. The ability to isolate functional aNK EVs on a large scale may lead to new clinical applications. Abbreviations: NK: natural killer cells; activated NK (aNK) cells; EVs: extracellular vesicles; ALL: acute lymphoblastic leukaemia; aAPC: artificial antigen-presenting cell; TEM: transmission electron

  2. Cytotoxic activities of amentoflavone against human breast and cervical cancers are mediated by increasing of PTEN expression levels due to peroxisomes proliferate-activated receptor {gamma} activation

    Energy Technology Data Exchange (ETDEWEB)

    Lee, Eunjung; Shin, Soyoung; Lee, Jeeyoung; Lee, So Jung; Kim, Jinkyoung; Yoon, Doyoung; Kim, Yangmee [Konkuk Univ., Seoul (Korea, Republic of); Woo, Eunrhan [Chosun Univ., Gwangju (Korea, Republic of)

    2012-07-15

    Human peroxisomes proliferate-activated receptor gamma (hPPAR{gamma}) has been implicated in numerous pathologies, including obesity, diabetes, and cancer. Previously, we verified that amentoflavone is an activator of hPPAR{gamma} and probed the molecular basis of its action. In this study, we investigated the mechanism of action of amentoflavone in cancer cells and demonstrated that amentoflavone showed strong cytotoxicity against MCF-7 and HeLa cancer cell lines. We showed that hPPAR{gamma} expression in MCF-7 and HeLa cells is specifically stimulated by amentoflavone, and suggested that amentoflavone-induced cytotoxic activities are mediated by activation of hPPAR{gamma} in these two cancer cell lines. Moreover, amentoflavone increased PTEN levels in these two cancer cell lines, indicating that the cytotoxic activities of amentoflavone are mediated by increasing of PTEN expression levels due to hPPAR{gamma} activation.

  3. Cytotoxic and Antibacterial Activity of an Extract from a Saudi Traditional Medicinal Plant Equisetum Arvense

    KAUST Repository

    Aldaas, Salsabil

    2011-05-01

    Background:Many ancient civilizations have used plants for medicinal purposes and indeed research has suggested that plant-derived compounds can be useful for treating many ailments, including cancer and infectious diseases. One such plant, Equisetum arvense, commonly known as horsetail, is a herbal plant that grows in Saudi Arabia and is traditionally used as a diuretic. Objective (s): We sought to determine whether horsetail extract exhibits 1) cytotoxic activity on cell lines and 2) antibacterial activity on the bacterial strain Escherichia coli. Materials and Methods: Using dried aerial part of the horsetail plant, a methanolic extract was prepared for screening. This extract was examined for its cytotoxic effect on the following cell lines: cervical adenocarcinoma and breast adenocarcinoma as a cancer cell model; lung fibroblast as a normal cell model; and human embryonic kidney. After 72 hours of treatment, the cells were assayed to determine the relative percentages of dead and live cells. Microscopical examination was used to give approximate percentages and a general overview of the effect on cell morphology. The LIVE⁄DEAD® Viability⁄Cytotoxicity kit was used to determine viability of cells in the population by using two dyes: the green-fluorescent calcein-AM which stains living cells, and the red-fluorescent ethidium homodimer-1 which stains dead cells. The alamarBlue® assay, based on a fluorometric/colorimetric growth indicator that detects metabolic activity, was used to establish a relative percentage of the living cells in a population treated with the plant extract compared to untreated cells (control). To determine antibacterial activity, the disc diffusion method was used. Results: Preliminary screening suggests that the horsetail extract induces death on the four tested cell lines with the greatest effect on human embryonic kidney cells followed by breast adenocarcinoma. The extract also displayed antibacterial activity at the highest

  4. Glutamine Assimilation and Feedback Regulation of L-acetyl-N-glutamate Kinase Activity in Chlorella variabilis NC64A Results in Changes in Arginine Pools.

    Science.gov (United States)

    Minaeva, Ekaterina; Forchhammer, Karl; Ermilova, Elena

    2015-11-01

    Glutamine is a metabolite of central importance in nitrogen metabolism of microorganisms and plants. The Chlorella PII signaling protein controls, in a glutamine-dependent manner, the key enzyme of the ornithine/arginine biosynthesis pathway, N-acetyl-L-glutamate kinase (NAGK) that leads to arginine formation. We provide evidence that glutamine promotes effective growth of C. variabilis strain NC64A. The present study shows that externally supplied glutamine directly influences the internal pool of arginine in NC64A. Glutamine synthetase (GS) catalyzes the ATP-dependent conversion of glutamate and ammonium to glutamine. The results of this study demonstrate that glutamine acts as a negative effector of GS activity. These data emphasize the importance of glutamine-dependent coupling of metabolism and signaling as components of an efficient pathway allowing the maintenance of metabolic homeostasis and sustaining growth of Chlorella. Copyright © 2015 Elsevier GmbH. All rights reserved.

  5. Antibiotic, cytotoxic and enzyme inhibitory activity of crude extracts from Brazilian marine invertebrates

    Directory of Open Access Journals (Sweden)

    Mirna H. R. Seleghim

    Full Text Available Herein we present the results of a screening with 349 crude extracts of Brazilian marine sponges, ascidians, bryozoans and octocorals, against 16 strains of susceptible and antibiotic-resistant bacteria, one yeast (Candida albicans, Mycobacterium tuberculosis H37Rv, three cancer cell lines MCF-7 (breast, B16 (murine melanoma and HCT8 (colon, and Leishmania tarentolae adenine phosphoribosyl transferase (L-APRT enzyme. Less than 15% of marine sponge crude extracts displayed antibacterial activity, both against susceptible and antibiotic-resistant bacteria. Up to 40% of marine sponge crude extracts displayed antimycobacterial activity against M. tuberculosis H37Rv. Cytotoxicity was observed for 18% of marine sponge crude extracts. Finally, less than 3% of sponge extracts inhibited L-APRT. Less than 10% of ascidian crude extracts displayed antibacterial activity. More than 25% of ascidian crude extracts were active against M. tuberculosis and the three cancer cell lines. Only two crude extracts from the ascidian Polysyncraton sp. collected in different seasons (1995 and 1997 displayed activity against L-APRT. Less than 2% of bryozoan and octocoral crude extracts presented antibacterial activity, but a high percentage of crude extracts from bryozoan and octororal displayed cytotoxic (11% and 30%, respectively and antimycobacterial (60% activities. The extract of only one species of bryozoan, Bugula sp., presented inhibitory activity against L-APRT. Overall, the crude extracts of marine invertebrates herein investigated presented a high level of cytotoxic and antimycobacterial activities, a lower level of antibacterial activity and only a small number of crude extracts inhibited L-APRT. Taxonomic analysis of some of the more potently active crude extracts showed the occurrence of biological activity in taxa that have been previously chemically investigated. These include marine sponges belonging to genera Aaptos, Aplysina, Callyspongia, Haliclona

  6. Palladium-catalyzed Suzuki-Miyaura coupling of amides by carbon-nitrogen cleavage: general strategy for amide N-C bond activation.

    Science.gov (United States)

    Meng, Guangrong; Szostak, Michal

    2016-06-15

    The first palladium-catalyzed Suzuki-Miyaura cross-coupling of amides with boronic acids for the synthesis of ketones by sterically-controlled N-C bond activation is reported. The transformation is characterized by operational simplicity using bench-stable, commercial reagents and catalysts, and a broad substrate scope, including substrates with electron-donating and withdrawing groups on both coupling partners, steric-hindrance, heterocycles, halides, esters and ketones. The scope and limitations are presented in the synthesis of >60 functionalized ketones. Mechanistic studies provide insight into the catalytic cycle of the cross-coupling, including the first experimental evidence for Pd insertion into the amide N-C bond. The synthetic utility is showcased by a gram-scale cross-coupling and cross-coupling at room temperature. Most importantly, this process provides a blueprint for the development of a plethora of metal catalyzed reactions of typically inert amide bonds via acyl-metal intermediates. A unified strategy for amide bond activation to enable metal insertion into N-C amide bond is outlined ().

  7. Chemical composition, and cytotoxic, antioxidant and antibacterial activities of the essential oil from ginseng leaves.

    Science.gov (United States)

    Jiang, Rui; Sun, Liwei; Wang, Yanbing; Liu, Jianzeng; Liu, Xiaodan; Feng, Hao; Zhao, Daqing

    2014-06-01

    Panax ginseng C.A.Meyer is one of the most valuable traditional Chinese medicines. In this study, the essential oil of ginseng leaves (EOGL), collected using hydrodistillation and analyzed by GC/MS, contained a complex mixture of aliphatic (69.0%), terpenoid (21.5%) and aromatic compounds (2.4%). Among 54 components identified, the major ones were palmitic acid (36.1%), beta-farnesene (15.4%), linoleic acid (9.8%) and phytol (5.6%). In the cytotoxicity study, EOGL exhibited obvious cytotoxic activities against different cancer cell lines, including Hela, A549, ZR-75-1, HT-29, SGC7901 and B16 cells. Furthermore, Annexin V-FITC/PI staining assay indicated that EOGL can induce late apoptosis of ZR-75-1 cells, and the percentage of apoptotic cells increased in a concentration-dependent manner (0.9% to 5.6% and 67.4%). In addition to this, we also found that EOGL exhibited weak DPPH radical scavenging (12.0 +/- 0.4 mg/mL) and ABTS radical scavenging activities (1.6 +/- 0.1 mg/mL), and showed antibacterial activity against the Gram-positive bacteria, Staphylococcus aureus and Bacillus subtilis, and the Gram-negative bacterium, Escherichia coli. The data suggest that EOGL, which possesses important biological activities, especially significant anticancer activity, could be a potential medicinal resource.

  8. Dehydroleucodine, a Sesquiterpene Lactone from Gynoxys verrucosa, Demonstrates Cytotoxic Activity against Human Leukemia Cells.

    Science.gov (United States)

    Ordóñez, Paola E; Sharma, Krishan K; Bystrom, Laura M; Alas, Maria A; Enriquez, Raul G; Malagón, Omar; Jones, Darin E; Guzman, Monica L; Compadre, Cesar M

    2016-04-22

    The sesquiterpene lactones dehydroleucodine (1) and leucodine (2) were isolated from Gynoxys verrucosa, a species used in traditional medicine in southern Ecuador. The activity of these compounds was determined against eight acute myeloid leukemia (AML) cell lines and compared with their activity against normal peripheral blood mononuclear cells. Compound 1 showed cytotoxic activity against the tested cell lines, with LD50 values between 5.0 and 18.9 μM. Compound 2 was inactive against all of the tested cell lines, demonstrating that the exocyclic methylene in the lactone ring is required for cytotoxic activity. Importantly, compound 1 induced less toxicity to normal blood cells than to AML cell lines and was active against human AML cell samples from five patients, with an average LD50 of 9.4 μM. Mechanistic assays suggest that compound 1 has a similar mechanism of action to parthenolide (3). Although these compounds have significant structural differences, their lipophilic surface signatures show striking similarities.

  9. Synthesis of Azole-containing Piperazine Derivatives and Evaluation of their Antibacterial, Antifungal and Cytotoxic Activities

    Energy Technology Data Exchange (ETDEWEB)

    Gan, Lin Ling; Fang, Bo; Zhou, Cheng He [Southwest University, Chongqing (China)

    2010-12-15

    A series of azole-containing piperazine derivatives have been designed and synthesized. The obtained compounds were investigated in vitro for their antibacterial, antifungal and cytotoxic activities. The preliminary results showed that most compounds exhibited moderate to significant antibacterial and antifungal activities in vitro. 1-(4-((4-chlorophenyl) (phenyl)methyl)piperazin-1-yl)-2-(1H-imidazol-1-yl)ethanone and 1-(4-((4-Chlorophenyl)(phenyl)methyl)piperazin-1- yl)-2-(2-phenyl-1H-imidazol-1-yl)ethanone gave remarkable and broad-spectrum antimicrobial efficacy against all tested strains with MIC values ranging from 3.1 to 25 μg/mL, and exhibited comparable activities to the standard drugs chloramphenicol and fluconazole in clinic. Moreover, 2-((4-((4-chlorophenyl)(phenyl)methyl)piperazin-1-yl)methyl)- 1H-benzo[d]imidazole was found to be the most effective in vitro against the PC-3 cell line, reaching growth inhibition values (36.4, 60.1 and 76.5%) for each tested concentration: 25 μM, 50 μM and 100 μM in dose-dependent manner. The results also showed that the azole ring had noticeable effect on their antimicrobial and cytotoxic activities, and imidazole and benzimidazole moiety were much more favourable to biological activity than 1,2,4-triazole.

  10. Evaluation of cytotoxicity, immune compatibility and antibacterial activity of biogenic silver nanoparticles.

    Science.gov (United States)

    Składanowski, M; Golinska, P; Rudnicka, K; Dahm, H; Rai, M

    2016-12-01

    The study was focused on assessment of antibacterial activity, cytotoxicity and immune compatibility of biogenic silver nanoparticles (AgNPs) synthesized from Streptomyces sp. NH28 strain. Nanoparticles were biosynthesized and characterized by UV-Vis spectroscopy, transmission electron microscopy, Fourier transform infrared spectroscopy, nanoparticle tracking analysis system and zeta potential. Antibacterial activity was tested against Gram-positive and Gram-negative bacteria; minimal inhibitory concentration was recorded. Cytotoxicity was estimated using L929 mouse fibroblasts via 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide test. Biocompatibility of AgNPs was performed using THP1-XBlue™ cells. Biogenic AgNPs presented high antibacterial activity against all tested bacteria. Minimum inhibitory concentration of AgNPs against bacterial cells was found to be in range of 1.25-10 μg/mL. Silver nanoparticles did not show any harmful interaction to mouse fibroblast cell line, and no activation of nuclear factor kappa-light-chain-enhancer of activated B (NF-κB) cells was observed at concentration below 10 µg/mL. The half-maximal inhibitory concentration (IC 50 ) value was established at 64.5 μg/mL. Biological synthesis of silver can be used as an effective system for formation of metal nanoparticles. Biosynthesized AgNPs can be used as an antibacterial agent, which can be safe for eukaryotic cells.

  11. Antioxidant, Anti-Inflammatory, and Cytotoxic Activities of Garcinia nervosa (Clusiaceae

    Directory of Open Access Journals (Sweden)

    N. M. U. Seruji

    2013-01-01

    Full Text Available In our continuing interest on Sarawak Garcinia species, we carried out the evaluation of antioxidant, anti-inflammatory and cytotoxic activities on the methanolic extracts of Garcinia nervosa. The extracts were prepared from its air-dried grounded leaves and barks. The evaluation of antioxidant activities was done using the (2,2-diphenyl-1-picrylhydrazyl DPPH radical scavenging assay and the result showed high radical scavenging activities. Meanwhile, the anti-inflammatory evaluation was performed using the lipoxygenase assay, hyaluronidase assay, and xanthine oxidase assay which showed, both of these extracts exhibited high anti-inflammatory properties. The lipoxygenase assay showed a high inhibition of enzyme activity for the barks extracts and a moderate enzyme activity for the leaves extracts. However, there were low inhibitions for both extracts in the hyaluronidase assay and only the barks extracts exhibited moderate antigout properties in the xanthine oxidase assay. For the cytotoxic assay, the extracts exhibited positive responses against the three cancer cell lines, the HeLa cell lines, MCF-7 cell lines, and HT-29 cell lines. Thus, Garcinia nervosa contains high antioxidativeand anti-inflammation properties, which have great potential in the development of pharmaceutical and dermatological products.

  12. Antiobesity, antioxidant and cytotoxicity activities of newly synthesized chalcone derivatives and their metal complexes.

    Science.gov (United States)

    El Sayed Aly, Mohamed Ramadan; Abd El Razek Fodah, Hamadah Hamadah; Saleh, Sherif Yousef

    2014-04-09

    Four sets of rationally designed chalcones were prepared for evaluation of their antiobesity, antioxidant and cytotoxicity activities. These sets include nine oleoyl chalcones as mimics of oleoyl estrone, three monohydroxy chalcones (chalcone ligands), Schiff base-derived chalcones and four copper as well as zinc complexes. Oleoyl chalcones 4d, 4e and particularly 6a as an isosteric isomer of oleoyl estrone, were as active as Orlistat on weight loss and related metabolic parameters using male SD rats in vivo. Chalcone ligands 10a-c and Schiff base-derived chalcones 11 and 14a,b were weakly antioxidants, while, the copper and zinc complexes 15a-d were good antioxidants with zinc chelates 15b,d being more active than their copper analogues 15a,cin vitro. Compounds 10c and 14a showed good cytotoxicity activities as Doxorubicin against PC3 cancer cell line in vitro, while, the copper complex 15c showed promising activity with IC₅₀ value of 5.95 μM. The estimated IC₅₀ value for Doxorubicin was 8.7 μM. Chalcones 14a,b are bifunctional probes for potential investigations in cancer diagnosis and radiotherapy by complexation with Gd(3+) or metal radioisotopes followed by posttranslation of Shiga toxin B-subunits that target globotriosyl ceramide expressing cancer cells. Copyright © 2014 Elsevier Masson SAS. All rights reserved.

  13. Cytotoxic Activity of the Methanolic Extract of Turnera diffusa Willd on Breast Cancer Cells

    Science.gov (United States)

    Avelino-Flores, María del Carmen; Cruz-López, María del Carmen; Jiménez-Montejo, Fabiola E.; Reyes-Leyva, Julio

    2015-01-01

    Abstract Turnera diffusa Willd, commonly known as Damiana, is employed in traditional medicine as a stimulant, aphrodisiac, and diuretic. Its leaves and stems are used for flavoring and infusion. Damiana is considered to be safe for medicinal use by the FDA. Pharmacological studies have established the hypoglycemic, antiaromatase, prosexual, estrogenic, antibacterial, and antioxidant activity of T. diffusa. The aim of the present study was to evaluate the possible cytotoxic effect of extracts and organic fractions of this plant on five tumor cell lines (SiHa, C-33, Hep G2, MDA-MB-231, and T-47D) and normal human fibroblasts. The results show that the methanolic extract (TdM) displayed greater activity on MDA-MB-231 breast cancer cells (with an IC50 of 30.67 μg/mL) than on the other cancer cell lines. Four organic fractions of this extract exhibited activity on this cancer cell line. In the most active fraction (F4), two active compounds were isolated, arbutin (1) and apigenin (2). This is the first report of a cytotoxic effect by T. diffusa on cancer cells. The IC50 values suggest that the methanolic extract of T. diffusa has potential as an anticancer therapy. PMID:25299247

  14. Evaluation of selected lichens from iceland for cancer chemopreventive and cytotoxic activity.

    Science.gov (United States)

    Ingólfsdóttir, K; Kook Lee, S; Bhat, K P; Lee, K; Chai, H B; Kristinsson, H; Song, L L; Gills, J; Gudmundsdóttir, J T; Mata-Greenwood, E; Jang, M S; Pezzuto, J M

    2000-01-01

    Cancer chemopreventive effects of organic extracts from 29 species of lichens collected in Iceland were evaluated using a panel of in vitro bioassays whereby extracts were tested for potential to induce quinone reductase (QR) and differentiation of human promyelocytic leukemia (HL-60) cells, inhibit cyclooxygenase-1 (COX-1), phorbol ester-induced ornithine decarboxylase (ODC), aromatase and sulfatase, as well as for antioxidant, estrogenic/anti-estrogenic and antiproliferative activity. In addition, the extracts were tested for cytotoxicity against 12 cancer cell lines. The most significant results were exhibited by extracts from Xanthoria elegans and Alectoria nigricans , which respectively, induced QR activity (concentration to double activity = 4.8 µg/ml) and inhibited phorbol ester-induced ODC activity with mouse 308 cells in culture (IC 50 = 2.6 µg/ml). Moderate inhibition of [ 3 H]thymidine incorporation with HL-60 cells was exhibited by the Peltigera leucophlebia extract. Several extracts prevented estrogen formation from estrogen precursors by inhibiting the enzymatic activities of aromatase ( Sphaerophorus globosus , Cetrariella delisei , Melanelia hepatizon ) and sulfatase ( Cladonia gracilis , Sphaerophorus fragilis , S. globosus ). None of the extracts demonstrated significant cytotoxic effects with selected cell lines.

  15. Phenolic content, antioxidant effect and cytotoxic activity of Leea indica leaves

    Directory of Open Access Journals (Sweden)

    Reddy Nidyaletchmy

    2012-08-01

    Full Text Available Abstract Background The leaves of Leea indica (Vitaceae, commonly known as ‘Huo Tong Shu’ in Malaysia, have been traditionally used as natural remedy in folk medicine by the locals. The current study reports the outcome of antioxidant and cytotoxic investigation of L. indica leaves. To the best of our knowledge, this is the first report of L. indica leaf crude ethanol and its fractionated extracts (hexane, ethyl acetate and water for evaluation of total phenolic content, antioxidant effect and cytotoxic activity against colon cancer cell lines. Methods In the present study, L. indica leaf crude ethanol and its fractionated extracts (hexane, ethyl acetate and water were firstly prepared prior to phenolic content, antioxidant effect and cytotoxic activity assessment. Folin-Ciocalteau’s method was used for the measurement of total phenolic content of the extracts. The antioxidant activity was measured by employing three different established testing systems, such as scavenging activity on DPPH (1,1-diphenyl-2-picrylhydrazyl radicals, reducing power assay and SOD (superoxide dismutase activity assay. The cytotoxic activity of the extracts were evaluated against three colon cancer cell lines with varying molecular characteristics (HT-29, HCT-15 and HCT-116 by MTT [3-(4,5-dimethylthiazol-2-yl-2,5-diphenyltetrazolium bromide] assay. Results The total phenolic content and antioxidant capabilities differed significantly among the L. indica leaf extracts. A strong correlation between total phenolic content and antioxidant properties was found, indicating that phenolic compounds are the major contributor to the antioxidant properties of these extracts. Among the crude ethanol and its fractionated extracts, fractionated water extract showed significantly the highest total phenolic content and strongest antioxidant effect in all the antioxidant testing systems employed in this study. All the four extracts exert no damage to the selected colon cancer

  16. Cytotoxic, Cytostatic and HIV-1 PR Inhibitory Activities of the Soft Coral Litophyton arboreum

    Directory of Open Access Journals (Sweden)

    Mona S. Ellithey

    2013-12-01

    Full Text Available Bioassay-guided fractionation using different chromatographic and spectroscopic techniques in the analysis of the Red Sea soft coral Litophyton arboreum led to the isolation of nine compounds; sarcophytol M (1, alismol (2, 24-methylcholesta-5,24(28-diene-3β-ol (3, 10-O-methyl alismoxide (4, alismoxide (5, (S-chimyl alcohol (6, 7β-acetoxy-24-methylcholesta-5-24(28-diene-3,19-diol (7, erythro-N-dodecanoyl-docosasphinga-(4E,8E-dienine (8, and 24-methylcholesta-5,24 (28-diene-3β,7β,19-triol (9. Some of the isolated compounds demonstrated potent cytotoxic- and/or cytostatic activity against HeLa and U937 cancer cell lines and inhibitory activity against HIV-1 protease (PR. Compound 7 was strongly cytotoxic against HeLa cells (CC50 4.3 ± 0.75 µM, with selectivity index of SI 8.1, which was confirmed by real time cell electronic sensing (RT-CES. Compounds 2, 7, and 8 showed strong inhibitory activity against HIV-1 PR at IC50s of 7.20 ± 0.7, 4.85 ± 0.18, and 4.80 ± 0.92 µM respectively. In silico docking of most compounds presented comparable scores to that of acetyl pepstatin, a known HIV-1 PR inhibitor. Interestingly, compound 8 showed potent HIV-1 PR inhibitory activity in the absence of cytotoxicity against the cell lines used. In addition, compounds 2 and 5 demonstrated cytostatic action in HeLa cells, revealing potential use in virostatic cocktails. Taken together, data presented here suggest Litophyton arboreum to contain promising compounds for further investigation against the diseases mentioned.

  17. Amish burn ointment and burdock leaf dressings: assessments of antimicrobial and cytotoxic activities.

    Science.gov (United States)

    Rieman, Mary T; Neely, Alice N; Boyce, Steven T; Kossenjans, William J; Durkee, Paula J; Zembrodt, Jacquelyn M; Puthoff, Barbara K; Kagan, Richard J

    2014-01-01

    Amish burn wound ointment (ABO) contains honey, lanolin, oils, glycerin, bees wax, and other natural additives. Although there are many anecdotal reports that this ointment covered with a burdock leaf (BL) dressing promotes burn wound healing, little scientific testing of this treatment has occurred. The goal of this study was to evaluate in vitro some of the components of this treatment modality for antimicrobial and cytotoxic activities. The ABO was tested for sterility using standard microbiological techniques. Because of the semisolid, lipid-based nature of the salve, the at-use product could not be tested in bioassays. Samples of BL and the dry ingredients (DI) used in the ointment were provided by the Amish vendor. Aqueous extracts of the DI and of the BL were prepared and freeze dried. The freeze-dried extracts were reconstituted, filtered, and tested separately on keratinocyte and fibroblast cell cultures for cytotoxicity (growth inhibition assay) and against a panel of susceptible and resistant microbes for antimicrobial activity (Nathan's agar-well diffusion assay) in a series of concentrations (% wt/vol). Neither DI nor BL extracts demonstrated antimicrobial activity against any of organisms tested. The DI extract inhibited growth of both keratinocytes and fibroblasts at the 0.1% concentration. The 0.1 and 0.03% concentrations of the BL extract were cytotoxic to both keratinocytes and fibroblasts. Although tests for microbial growth from the at-use preparation of the ABO were negative, extracts of the DI and BL did not demonstrate any antimicrobial activity. Additionally, both extracts inhibited the growth of skin cells in vitro at higher concentrations. These results suggest caution in the use of ABO and BL dressings if there is more than a minimal risk of complications from the burn injury.

  18. Physicochemical Properties, Antioxidant and Cytotoxic Activities of Crude Extracts and Fractions from Phyllanthus amarus

    Directory of Open Access Journals (Sweden)

    Van Tang Nguyen

    2017-06-01

    Full Text Available Background: Phyllanthus amarus (P. amarus has been used as a medicinal plant for the prevention and treatment of chronic ailments such as diabetes, hepatitis, and cancer. Methods: The physicochemical properties, antioxidant and cytotoxic activities of crude extracts and fractions from P. amarus were determined using spectrophotometric method. Results: The P. amarus methanol (PAM extract had lower levels of residual moisture (7.40% and water activity (0.24 and higher contents of saponins, phenolics, flavonoids, and proanthocyanidins (1657.86 mg escin equivalents, 250.45 mg gallic acid equivalents, 274.73 mg rutin equivalents and 61.22 mg catechin equivalents per g dried extract, respectively than those of the P. amarus water (PAW extract. The antioxidant activity of PAM extract was significantly higher (p < 0.05 than that of the PAW extract, PAM fractions, and phyllanthin (known as a major compound in the P. amarus. Higher cytotoxic activity of PAM extract based on MTT assay on different cell lines including MiaPaCa-2 (pancreas, HT29 (colon, A2780 (ovarian, H460 (lung, A431 (skin, Du145 (prostate, BE2-C (neuroblastoma, MCF-7 (breast, MCF-10A (normal breast, and U87, SJ-G2, SMA (glioblastoma was observed in comparison to the PAW extract and PAM fractions. The cytotoxic potential of the PAW extract (200 μg/mL, based on the CCK-8 assay on a pancreatic cancer cell line (MiaCaPa2 was significantly lower (p < 0.05 than those of gemcitabine (50 nM and a saponin-enriched extract from quillajia bark at 200 μg/mL (a commercial product, but was significantly higher than that of phyllanthin at 2 μg/mL. Conclusions: The results achieved from this study reveal that the PA extracts are a potential source for the development of natural antioxidant products and/or novel anticancer drugs.

  19. COMPARATIVE ANALYSIS OF CYTOTOXIC AND ANTIOXIDANT ACTIVITIES OF LEAF AND BARK EXTRACTS OF CLERODENRUM VISCOSUM AND CLERODENDRUM PHLOMIDIS

    OpenAIRE

    Bhatnagar, Sunita; Pattanaik, Soumya Ranjan

    2012-01-01

    Cytotoxic and antioxidant potential of leaf and bark extracts of two Clerodendrum sps namely C. phlomidis and  C. viscosum was investigated. Solvent extracts   hexane, chloroform, acetone and methanol were tested for their cytotoxic potential using brine shrimp motility assay and antioxidant potential was ascertained using DPPH and FRAP assays.             Cytotoxic activity of all the solvent extracts was tested at four doses 25, 50,100 and 200µl/ml. All the extracts showed d...

  20. Evaluation of In vitro Anthelmintic Activity, Total Phenolic Content and Cytotoxic Activity of Crinum latifolium L. (Family: Amaryllidaceae

    Directory of Open Access Journals (Sweden)

    Abdul Aziz

    2014-03-01

    Full Text Available Purpose: Crinum latifolium is a widely used plant in Asian folk and traditional medicine.In the present study, we have tried to find out the anthelmintic activity, total phenolic contents and cytotoxicity of the methanolic extract of the target plant. Methods: Anthelmintic activity was assessed applying five different concentrations of the plant extract and recording the time of paralysis and death. Total phenolic contents were determined using Folin-Ciocaltu method, using Gallic acid as standard; while brine shrimp lethality test (BSLT method was used to evaluate the cytotoxicity of the plant extract, where vincristine sulphate and DMSO was used as positive and negative control respectively. Result: The lowest time for paralysis and death of worms, for test sample at highest concentration (50mg/ml, were found 24±0.45 and 46.4±0.60 min respectively, which gradually increased with the decrease of concentration. On the other hand, albendazole, which was used as standard, caused paralysis and death of worms at 56.2±0.20 min and 77.4±0.24 min respectively; whereas no mortality of the worms was observed, when distilled water was used as control. The crude methanolic extract exhibited lower amount of total phenolic content (17.50±2.64 mg/ml. In case of cytotoxicity measurement, the crude methanolic extract showed positive result (with LC50 15.652 µg/ml compared to standard Vincristine sulphate (0.839 µg/ml; which indicated that the leaves of Crinum latifolium possess mild cytotoxic principles. Conclusion: Therefore, further studies are suggested to evaluate the possible mechanism of action and the active compounds responsible for the biological activities of the plant extract.

  1. Anti-Trypanosoma cruzi and cytotoxic activities of Eugenia uniflora L.

    Science.gov (United States)

    Santos, Karla K A; Matias, Edinardo F F; Tintino, Saulo R; Souza, Celestina E S; Braga, Maria F B M; Guedes, Gláucia M M; Rolón, Miriam; Vega, Celeste; de Arias, Antonieta Rojas; Costa, José G M; Menezes, Irwin R A; Coutinho, Henrique D M

    2012-05-01

    Chagas disease is caused by Trypanosoma cruzi, being considered a public health problem. An alternative to combat this pathogen is the use of natural products isolated from fruits such as Eugenia uniflora, a plant used by traditional communities as food and medicine due to its antimicrobial and biological activities. Ethanolic extract from E. uniflora was used to evaluate in vitro anti-epimastigote and cytotoxic activity. This is the first record of anti-Trypanosoma activity of E. uniflora, demonstrating that a concentration presenting 50% of activity (EC(50)) was 62.76 μg/mL. Minimum inhibitory concentration (MIC) was ≤ 1024 μg/mL. Our results indicate that E. uniflora could be a source of plant-derived natural products with anti-epimastigote activity with low toxicity. Copyright © 2012 Elsevier Inc. All rights reserved.

  2. Medicinal Mushroom Extracts Possess Differential Antioxidant Activity and Cytotoxicity to Cancer Cells.

    Science.gov (United States)

    Elbatrawy, Eman Nasr; Ghonimy, Eglal AbdAllah; Alassar, Mahomud Mohammed; Wu, Fang-Sheng

    2015-01-01

    Many species of edible mushrooms are known to contain a wide array of compounds with high nutritional and medicinal values. However, these values vary widely among mushroom species because of the wide diversity of compounds with different solubilities to solvents used in extraction. We report here the comparison of antioxidant activity and cytotoxicity against cancer cells in extracts of Pleurotus ostreatus, P. sajor-caju, Agaricus campestris, and A. bisporus from 7 different solvents, including water, ethanol, ethyl acetate, acetone, chloroform, hexane, and petroleum ether. The extracts were analyzed for their antioxidant activities using the % DPPH (2,2-diphenyl-1-picrylhydrazylhydrate) scavenging activity method. Our results revealed that the water extracts exhibited the highest % DPPH scavenging activity in comparison to all other solvent extracts. The highest value was obtained from the water extract of P. sajor-caju (78.1%), and the lowest one was from the hexane extract of A. bisporus (0.8%). In general, extracts from nonpolar solvents exhibited much lower antioxidant activities than those from polar solvents. The cytotoxic effects of these extracts were evaluated using 2 cancer cell lines of larynx carcinoma (HEp-2) and breast carcinoma (MCF-7). When added into Hep-2 cells, the hexane extracts from P. ostreatus, P. sajor-caju, A. bisporus, and A. campestris yielded the highest IC50 values of 1.7 ± 1.56, 2.1 ± 2.82, 4.4 ± 1.71, and 2.2 ± 1.34 μg/mL, respectively, in comparison to all other solvent extracts. Similar IC50 values were obtained when the MCF-2 cancer cells were tested, suggesting that hexane is the preferred solvent to extract the anticancer compounds from these mushrooms. Our results also indicated that extracts from solvents with nonpolar or intermediate polarity were more potent than those with high polarity in their cytotoxicity against cancer cells, and extracts from different mushrooms by the same solvent possessed varied degrees of

  3. Antimicrobial and cytotoxic activities of 1,2,3-triazole-sucrose derivatives.

    Science.gov (United States)

    Petrova, Krasimira T; Potewar, Taterao M; Correia-da-Silva, Paula; Barros, M Teresa; Calhelha, Ricardo C; Ćiric, Ana; Soković, Marina; Ferreira, Isabel C F R

    2015-11-19

    A library of 1-(1',2,3,3',4,4',6-hepta-O-acetyl-6'-deoxy-sucros-6'-yl)-1,2,3-triazoles have been investigated for their antibacterial, antifungal and cytotoxic activities. Most of the target compounds showed good inhibitory activity against a variety of clinically and food contaminant important microbial pathogens. In particular, 1-(1',2,3,3',4,4',6-hepta-O-acetyl-6'-deoxy-sucros-6'-yl)-4-(4-pentylphenyl)-1,2,3-triazole (5) was highly active against all the tested bacteria with minimal inhibitory concentrations (MICs) ranging between 1.1 and 4.4 µM and bactericidal concentrations (MBCs) from 2.2 and 8.4 µM. The compound 1-(1',2,3,3',4,4',6-hepta-O-acetyl-6'-deoxy-sucros-6'-yl)-4-(4-bromophenyl)-1,2,3-triazole (3) showed antifungal activity with MICs from 0.6 to 4.8 µM and minimal fungicidal concentrations (MFCs) ranging between 1.2 and 8.9 µM. Furthermore, some of the compounds possessed moderate cytotoxicity against human breast, lung, cervical and hepatocellular carcinoma cell lines, without showing toxicity for non-tumor liver cells. The above mentioned derivatives represent promising leads for the development of new generation of sugar-triazole antifungal agents. Copyright © 2015 Elsevier Ltd. All rights reserved.

  4. Cytotoxic, thrombolytic, membrane stabilizing and anti-oxidant activities of Hygrophila schulli

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    Md. Abu Sufian

    2015-08-01

    Full Text Available The crude methanol extract of Hygrophila schulli and its petroleum ether, chloroform, ethyl acetate and aqueous soluble Kupchan partitionates were investigated for in vitro cytotoxic, thrombolytic, membrane stabilizing and anti-oxidant activities. In the brine shrimp lethality bioassay, the petroleum ether soluble extract of H. schulli showed significant cytotoxicity (LC50 = 0.1 µg/mL and LC90 = 15 µg/mL as compared to vincristine sulfate (LC50 = 0.4 µg/mL and LC90 = 9 µg/mL. Among all the partitionates, chloroform soluble fraction demonstrated the highest thrombolytic activity with 10.5% clot lyses. Moreover, in hypotonic- and heat-induced conditions, the chloroform soluble extractive inhibited hemolysis of human erythrocyte by 113.7% and 14.3%, respectively as compared to 71.9% and 42.2% demonstrated by standard acetylsalicylic acid. On the other hand, in anti-oxidant activity test, chloroform soluble fraction revealed mild antioxidant activity (IC50 = 195.1 µg/mL as compared to standard tert-butyl-1-hydroxytoluene (IC50 = 27.5 µg/mL.

  5. Endophytic Actinobacteria Associated with Dracaena cochinchinensis Lour.: Isolation, Diversity, and Their Cytotoxic Activities

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    Nimaichand Salam

    2017-01-01

    Full Text Available Dracaena cochinchinensis Lour. is an ethnomedicinally important plant used in traditional Chinese medicine known as dragon’s blood. Excessive utilization of the plant for extraction of dragon’s blood had resulted in the destruction of the important niche. During a study to provide a sustainable way of utilizing the resources, the endophytic Actinobacteria associated with the plant were explored for potential utilization of their medicinal properties. Three hundred and four endophytic Actinobacteria belonging to the genera Streptomyces, Nocardiopsis, Brevibacterium, Microbacterium, Tsukamurella, Arthrobacter, Brachybacterium, Nocardia, Rhodococcus, Kocuria, Nocardioides, and Pseudonocardia were isolated from different tissues of D. cochinchinensis Lour. Of these, 17 strains having antimicrobial and anthracyclines-producing activities were further selected for screening of antifungal and cytotoxic activities against two human cancer cell lines, MCF-7 and Hep G2. Ten of these selected endophytic Actinobacteria showed antifungal activities against at least one of the fungal pathogens, of which three strains exhibited cytotoxic activities with IC50-values ranging between 3 and 33 μg·mL−1. Frequencies for the presence of biosynthetic genes, polyketide synthase- (PKS- I, PKS-II, and nonribosomal peptide synthetase (NRPS among these 17 selected bioactive Actinobacteria were 29.4%, 70.6%, and 23.5%, respectively. The results indicated that the medicinal plant D. cochinchinensis Lour. is a good niche of biologically important metabolites-producing Actinobacteria.

  6. Evaluation of antimicrobial, Cytotoxic and genotoxic activities of Ganoderma lucidum (Reishi mushroom).

    Science.gov (United States)

    Ergun, Bulent

    2017-09-01

    Ganoderma lucidum (GL) is a mushroom used as a traditional remedy for the treatment of various infections since ancient times. This study, was aimed to investigate antimicrobial activity potential of GL against Staphylococcus aureus, Enterococcus faecalis, Listeria monocytogenes, Klebsiella pneumoniae, Pseudomonas aeruginosa, Escherichia coli, Candida albicans, Candida glabrata, Candida krusei, and Candida parapsilopsis. Furthermore, it was also aimed to evaluate the toxicity potential of GL. Antimicrobial activities were screened by using microbroth dilution method. With regard to toxicity studies, cytotoxicity was evaluated by using XTT method against NIH3T3 cell lines, whereas genotoxicity study was conducted by Ames MPF 98/100 mutagenicity assay. Obtained data indicated that minimal inhibitory concentration values of the extract against the tested microorganisms ranged from 200 to 400μg/ml. No cytotoxic activity was observed related to the Ganoderma lucidum administrations. However, results of the Ames test pointed out a genetic damage with metabolic activation against TA98. At the highest concentration (5mg/ml) the extract showed 2.71 fold increase over the baseline significantly. (p<0.05). In conclusion, in spite of significant antimicrobial effect potential, Ganoderma lucidum should be used carefully because of its genotoxicity potential.

  7. In Vitro Antioxidant and Cytotoxic Activities of Some Marine Sponges Collected off Misamis Oriental Coast, Philippines

    Directory of Open Access Journals (Sweden)

    A. P. Rivera

    2012-01-01

    Full Text Available The phosphomolybdenum method for total antioxidant activity determination showed that the hexane, dichloromethane and ethyl acetate extracts of five marine sponge species collected off misamis oriental coast-Aaptos suberitoides, Dactylospongia elegans, Stylissa massa, Haliclona sp. and an unidentified species coded as KL-05, have varying degrees of antioxidant capacity. Expressed as ascorbic acid equivalents in μg/mL of extract, the hexane extract of Dactylospongia elegans (DeH and the ethyl acetate extract of Aaptos suberitoides (AsE showed the highest antioxidant capacity. Although the hexane extract of KL-05 (KL-05H has considerable antioxidant activity, the ethyl acetate extract (KL-05E showed no antioxidant activity. The brine shrimp assay for cytotoxicity indicated high bioactivity, with Haliclona sp., Dactylospongia elegans, Aaptos suberitoides and Stylissa massa exhibiting high % mortality and low LC50 values. The antioxidant and cytotoxic activities of the marine sponges may be attributed to the zoochemicals present. All sponge species contain alkaloids, saponins, tannins, and flavonoids. Terpenoids are present only in Haliclona sp. and the cardiac glycosides, only in Aaptos suberitoides and Haliclona sp.

  8. Low-Cytotoxic Synthetic Bromorutaecarpine Exhibits Anti-Inflammation and Activation of Transient Receptor Potential Vanilloid Type 1 Activities

    Directory of Open Access Journals (Sweden)

    Chi-Ming Lee

    2013-01-01

    Full Text Available Rutaecarpine (RUT, the major bioactive ingredient isolated from the Chinese herb Evodia rutaecarpa, possesses a wide spectrum of biological activities, including anti-inflammation and preventing cardiovascular diseases. However, its high cytotoxicity hampers pharmaceutical development. We designed and synthesized a derivative of RUT, bromo-dimethoxyrutaecarpine (Br-RUT, which showed no cytotoxicity at 20 μM. Br-RUT suppressed nitric oxide (NO production and tumor necrosis factor-α release in concentration-dependent (0~20 μM manners in lipopolysaccharide (LPS-treated RAW 264.7 macrophages; protein levels of inducible NO synthase (iNOS and cyclooxygenase-2 induced by LPS were downregulated. Br-RUT inhibited cell migration and invasion of ovarian carcinoma A2780 cells with 0~48 h of treatment. Furthermore, Br-RUT enhanced the expression of transient receptor potential vanilloid type 1 and activated endothelial NOS in human aortic endothelial cells. These results suggest that the synthetic Br-RUT possesses very low cytotoxicity but retains its activities against inflammation and vasodilation that could be beneficial for cardiovascular disease therapeutics.

  9. Pentachlorophenol-Induced Cytotoxic, Mitogenic, and Endocrine-Disrupting Activities in Channel Catfish, Ictalurus punctatus

    Directory of Open Access Journals (Sweden)

    Paul B. Tchounwou

    2004-09-01

    Full Text Available Pentachlorophenol (PCP is an organochlorine compound that has been widely used as a biocide in several industrial, agricultural, and domestic applications. Although it has been shown to induce systemic toxicity and carcinogenesis in several experimental studies, the literature is scarce regarding its toxic mechanisms of action at the cellular and molecular levels. Recent investigations in our laboratory have shown that PCP induces cytotoxicity and transcriptionally activates stress genes in human liver carcinoma (HepG2 cells [1]. In this research, we hypothesize that environmental exposure to PCP may trigger cytotoxic, mitogenic, and endocrine-disrupting activities in aquatic organisms including fish. To test this hypothesis, we carried out in vitro cultures of male channel catfish hepatocytes, and performed the fluorescein diacetate assay (FDA to assess for cell viability, and the Western Blot analysis to assess for vitellogenin expression following exposure to PCP. Data obtained from FDA experiments indicated a strong dose-response relationship with respect to PCP cytotoxicity. Upon 48 hrs of exposure, the chemical dose required to cause 50% reduction in cell viability (LD50 was computed to be 1,987.0 + 9.6 μg PCP/mL. The NOAEL and LOAEL were 62.5 + 10.3 μg PCP/mL and 125.0+15.2 μg PCP/mL, respectively. At lower levels of exposure, PCP was found to be mitogenic, showing a strong dose- and time-dependent response with regard to cell proliferation. Western Blot analysis demonstrated the potential of PCP to cause endocrine-disrupting activity, as evidenced by the up regulation of the 125-kDa vitellogenin protein the hepatocytes of male channel catfish.

  10. Alpha- and Beta-Cyclodextrin Inclusion Complexes with 5-Fluorouracil: Characterization and Cytotoxic Activity Evaluation

    Directory of Open Access Journals (Sweden)

    Cristina Di Donato

    2016-12-01

    Full Text Available Cyclodextrins are natural macrocyclic oligosaccharides able to form inclusion complexes with a wide variety of guests, affecting their physicochemical and pharmaceutical properties. In order to obtain an improvement of the bioavailability and solubility of 5-fluorouracil, a pyrimidine analogue used as chemotherapeutic agent in the treatment of the colon, liver, and stomac cancers, the drug was complexed with alpha- and beta-cyclodextrin. The inclusion complexes were prepared in the solid state by kneading method and characterized by Fourier transform-infrared (FT-IR spectroscopy and X-ray powder diffractometry. In solution, the 1:1 stoichiometry for all the inclusion complexes was established by the Job plot method and the binding constants were determined at different pHs by UV-VIS titration. Furthermore, the cytotoxic activity of 5-fluorouracil and its complexation products were evaluated using the 3-(4,5-dimethylthiazol-2-yl-2,5-diphenyltetrazolium bromide (MTT assay on MCF-7 (breast cancer cell line, Hep G2 (hepatocyte carcinoma cell line, Caco-2 (colon adenocarcinoma cell line, and A-549 (alveolar basal epithelial carcinoma cell line. The results showed that both inclusion complexes increased the 5-fluorouracil capability of inhibiting cell growth. In particular, 5-fluorouracil complexed with beta-cyclodextrin had the highest cytotoxic activity on MCF-7; with alpha-cyclodextrin the highest cytotoxic activity was observed on A-549. The IC50 values were equal to 31 and 73 µM at 72 h, respectively. Our results underline the possibility of using these inclusion complexes in pharmaceutical formulations for improving 5-fluorouracil therapeutic efficacy.

  11. Alpha- and Beta-Cyclodextrin Inclusion Complexes with 5-Fluorouracil: Characterization and Cytotoxic Activity Evaluation.

    Science.gov (United States)

    Di Donato, Cristina; Lavorgna, Margherita; Fattorusso, Roberto; Isernia, Carla; Isidori, Marina; Malgieri, Gaetano; Piscitelli, Concetta; Russo, Chiara; Russo, Luigi; Iacovino, Rosa

    2016-12-01

    Cyclodextrins are natural macrocyclic oligosaccharides able to form inclusion complexes with a wide variety of guests, affecting their physicochemical and pharmaceutical properties. In order to obtain an improvement of the bioavailability and solubility of 5-fluorouracil, a pyrimidine analogue used as chemotherapeutic agent in the treatment of the colon, liver, and stomac cancers, the drug was complexed with alpha- and beta-cyclodextrin. The inclusion complexes were prepared in the solid state by kneading method and characterized by Fourier transform-infrared (FT-IR) spectroscopy and X-ray powder diffractometry. In solution, the 1:1 stoichiometry for all the inclusion complexes was established by the Job plot method and the binding constants were determined at different pHs by UV-VIS titration. Furthermore, the cytotoxic activity of 5-fluorouracil and its complexation products were evaluated using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay on MCF-7 (breast cancer cell line), Hep G2 (hepatocyte carcinoma cell line), Caco-2 (colon adenocarcinoma cell line), and A-549 (alveolar basal epithelial carcinoma cell line). The results showed that both inclusion complexes increased the 5-fluorouracil capability of inhibiting cell growth. In particular, 5-fluorouracil complexed with beta-cyclodextrin had the highest cytotoxic activity on MCF-7; with alpha-cyclodextrin the highest cytotoxic activity was observed on A-549. The IC 50 values were equal to 31 and 73 µM at 72 h, respectively. Our results underline the possibility of using these inclusion complexes in pharmaceutical formulations for improving 5-fluorouracil therapeutic efficacy.

  12. New Benzimidazole-1,2,4-Triazole Hybrid Compounds: Synthesis, Anticandidal Activity and Cytotoxicity Evaluation

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    Hülya Karaca Gençer

    2017-03-01

    Full Text Available Owing to the growing need for antifungal agents, we synthesized a new series 2-((5-(4-(5-substituted-1H-benzimidazol-2-ylphenyl-4-substituted-4H-1,2,4-triazol-3-ylthio-1-(substitutedphenylethan-1-one derivatives, which were tested against Candida species. The synthesized compounds were characterized and elucidated by FT-IR, 1H-NMR, 13C-NMR and HR-MS spectroscopies. The synthesized compounds were screened in vitro anticandidal activity against Candida species by broth microdiluation methods. In vitro cytotoxic effects of the final compounds were determined by MTT assay. Microbiological studies revealed that compounds 5m, 5o, 5r, 5t, 5y, 5ab, and 5ad possess a good antifungal profile. Compounds 5w was the most active derivative and showed comparable antifungal activity to those of reference drugs ketoconazole and fluconazole. Cytotoxicity evaluation of compounds 5m, 5o, 5r, 5w, 5y, 5ab and 5ad showed that compounds 5w and 5ad were the least cytotoxic agents. Effects of these two compounds against ergosterol biosynthesis were observed by LC-MS-MS method, which is based on quantification of ergosterol level in C. albicans. Compounds 5w and 5d inhibited ergosterol biosynthesis concentration dependently. A fluorescence microscopy study was performed to visualize effect of compound 5w against C. albicans at cellular level. It was determined that compound 5w has a membrane damaging effect, which may be related with inhibition of biosynthesis of ergosterol.

  13. Study on the Cytotoxic Activity of Drimane Sesquiterpenes and Nordrimane Compounds against Cancer Cell Lines

    Directory of Open Access Journals (Sweden)

    Ivan Montenegro

    2014-11-01

    Full Text Available Twelve drimanes, including polygodial (1, isopolygodial (2, drimenol (3, confertifolin (4, and isodrimenin (5, were obtained from natural sources. Semi-synthetic derivatives 6–12 were obtained from 1 and 2, and cytotoxic activity was evaluated in vitro against cancer cell lines (HT-29, MDA-MB231, DHF, MCF-7, PC-3, DU-145, and CoN. IC50 values were determined at concentrations of 12.5–100 µM of each compound for 72 h. In addition, it was found that polygodial (1, 8, and 12 induced changes in mitochondrial membrane permeability in CoN, MCF-7, and PC-3 cells.

  14. Chemical composition, immunostimulatory, cytotoxic and antiparasitic activities of the essential oil from Brazilian red propolis.

    Science.gov (United States)

    Sena-Lopes, Ângela; Bezerra, Francisco Silvestre Brilhante; das Neves, Raquel Nascimento; de Pinho, Rodrigo Barros; Silva, Mara Thais de Oliveira; Savegnago, Lucielli; Collares, Tiago; Seixas, Fabiana; Begnini, Karine; Henriques, João Antonio Pêgas; Ely, Mariana Roesch; Rufatto, Luciane C; Moura, Sidnei; Barcellos, Thiago; Padilha, Francine; Dellagostin, Odir; Borsuk, Sibele

    2018-01-01

    Most studies of Brazilian red propolis have explored the composition and biological properties of its ethanolic extracts. In this work, we chemically extracted and characterized the essential oil of Brazilian red propolis (EOP) and assessed its adjuvant, antiparasitic and cytotoxic activities. The chemical composition of EOP was analyzed using gas chromatography with mass spectrometry (GC-MS). EOP was tested for in vitro activity against Trichomonas vaginalis (ATCC 30236 isolate); trophozoites were treated with different concentrations of EOP (ranging from 25 to 500 μg/mL) in order to establish the MIC and IC50 values. A cytotoxicity assay was performed in CHO-K1 cells submitted to different EOP concentrations. BALB/c mice were used to test the adjuvant effect of EOP. The animals were divided in 3 groups and inoculated as follows: 0.4 ng/kg BW EOP (G1); 50 μg of rCP40 protein (G2); or a combination of 0.4 ng/kg BW EOP and 50 μg of rCP40 (G3). Total IgG, IgG1 and IgG2a levels were assessed by ELISA. The major constituent compounds of EOP were methyl eugenol (13.1%), (E)-β-farnesene (2.50%), and δ-amorphene (2.3%). Exposure to EOP inhibited the growth of T. vaginalis, with an IC50 value of 100 μg/mL of EOP. An EOP concentration of 500 μg/mL was able to kill 100% of the T. vaginalis trophozoites. The EOP kinetic growth curve showed a 36% decrease in trophozoite growth after a 12 h exposure to 500 μg/mL of EOP, while complete parasite death was induced at 24 h. With regard to CHO-K1 cells, the CC50 was 266 μg/mL, and 92% cytotoxicity was observed after exposure to 500 μg/mL of EOP. Otherwise, a concentration of 200 μg/mL of EOP was able to reduce parasite proliferation by 70% and was not cytotoxic to CHO-K1 cells. As an adjuvant, a synergistic effect was observed when EOP was combined with the rCP40 protein (G3) in comparison to the administration of each component alone (G1 and G2), resulting in higher concentrations of IgG, IgG1 and IgG2a. EOP is

  15. Main constituents from the seeds of Vietnamese Cnidium monnieri and cytotoxic activity.

    Science.gov (United States)

    Dien, Pham Huu; Nhan, Nguyen Thi; Le Thuy, Hoang Thi; Quang, Dang Ngoc

    2012-01-01

    From the ethyl acetate extract of the seeds of Vietnamese Cnidium monnieri L., three coumarins, osthole (1), xanthotoxin (2), imperatorin (3) and a sterol, daucosterol (4) have been purified. Their structures were elucidated by spectroscopic analysis. Furthermore, 8-(3-hidroxy-3-methylbutyl)-7-methoxycoumarin (5) was synthesised from osthole (1) with a good yield (80%). In addition, compound 1 and its synthesis product (5) show moderate and non-selective cytotoxic activities against four cancer cells, KB (a human epidermal carcinoma), MCF7 (human breast carcinoma), SK-LU-1 (human lung carcinoma) and HepG2 (hepatocellular carcinoma).

  16. Synthesis and evaluation of cytotoxic activities of new guanidines derived from carbazoles.

    Science.gov (United States)

    Caruso, Anna; Sinicropi, Maria Stefania; Lancelot, Jean-Charles; El-Kashef, Hussein; Saturnino, Carmela; Aubert, Geneviève; Ballandonne, Céline; Lesnard, Aurélien; Cresteil, Thierry; Dallemagne, Patrick; Rault, Sylvain

    2014-01-15

    Several new alkylguanidines derived from carbazole have been synthesized in a simple one-pot reaction starting from 3-aminocarbazole derivatives. The aminocarbazoles were reacted with ethoxycarbonylisothiocyanate, to give thiourea intermediates, followed by the addition of an alkylamine and HgCl2 to give ethoxycarbonylguanidine intermediates. The reaction mixture was then heated at 160 °C to give the N-(1,4-dimethyl-9H-carbazol-3-yl)-N'-alkylguanidines. The cytotoxic activity of all the synthesized guanidines was evaluated against different cell lines. Copyright © 2013 Elsevier Ltd. All rights reserved.

  17. Leishmanicidal and cytotoxic activities of extracts and naturally-occurring compounds from two Lauraceae species.

    Science.gov (United States)

    Sánchez-Suárez, Jeysson; Coy-Barrera, Ericsson; Cuca, Luis Enrique; Delgado, Gabriela

    2011-02-01

    The in vitro leishmanicidal effects of ethanolic extracts and fifteen naturally-occurring compounds (five lignans, eight neolignans, a diterpene and a dihydrochalcone), obtained from Pleurothyrium cinereum and Ocotea macrophylla, were evaluated on promastigotes of Leishmania panamensis and L. braziliensis. In addition, in order to determine the selective action on Leishmania species as a safety principle, in vitro cytotoxicity on J774 cells was also evaluated for test compounds and extracts. One extract and seven compounds showed activity against Leishmania parasites at different levels. Dihydroflavokawin B (8) was found to be the most potent antileishmanial compound on both parasites, whilst (+)-otobaphenol (14), was found to be the most selective compound on L. panamensis.

  18. In vitro cytotoxic activity of Cymbopogon citratus L. and Cymbopogon nardus L. essential oils from Togo

    OpenAIRE

    Koffi Koba; Komla Sanda; Catherine Guyon; Christine Raynaud; Jean-Pierre Chaumont; Laurence Nicod

    2009-01-01

    The leaf essential oils of Cymbopogon citratus L. and Cymbopogon nardus L. (Poaceae) from Togo were steam-distilled, analyzed for percentage composition and investigated in vitro for their potential cytotoxic activity on human epidermic cell line HaCat. The percentage composition showed that the main constituents of essential oils samples were respectively geranial (45.2%), neral (32.4%) and myrc¨ne (10.2%) for C. citratus essential oil and citronellal (35.5%), geraniol (27.9%) and citronello...

  19. Pharmacological screening of Hypericum androsaemum extracts for antioxidant, anti-lipid peroxidation, antiglycation and cytotoxicity activity.

    Science.gov (United States)

    Saddiqe, Zeb; Maimoona, Alya; Abbas, Ghulam; Naeem, Ismat; Shahzad, Muhammad

    2016-03-01

    Oxidative stress and glycation processes have a combined effect on diabetes related complications. Crude plant extracts and plant derived compounds possessing both antiglycation and antioxidant activities have a high therapeutic potential for treating these complications. Antioxidant, antiglycation, anti-lipid per oxidation and cytotoxic activities of crude methanol extract and solvent fractions of Hypericum androsaemum L. (Hypericaceae) were evaluated and correlated with total content of phenolics and flavonoids. Significant radical scavenging activity was observed for the methanol extract against 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical used as a basis for antioxidant activity with IC50 value of 92.70±2.85 μg mL(-1) (96.20±2.34% inhibition at 500 μg mL(-1)). In case of anion scavenging activity the results were not very significant (33.20±1.22% inhibition at 500 μg mL(-1)). Anti-lipid per oxidation activity was highest for n-hexane fraction (67.83±1.33% inhibition at 500 μg mL(-1)) while the ethyl acetate fraction had the highest antiglycation activity (62.77±2.54% inhibition at 500 μg mL(-1)). Statistically significant correlation was determined for antioxidant and antiglycation activity and phenolic and flavonoid contents. In cytotoxicity assay all the extracts had IC50 values >30 μg mL(-1) as compared to the standard cycloheximide (IC50 value 0.084±0.1 μg mL(-1)). The polar extracts of H. androsaemum can be a good source of non-toxic compounds with antioxidant, anti-lipid per oxidation and antiglycation activities.

  20. Synthesis and cytotoxic activity of two novel 1-dodecylthio-2-decyloxypropyl-3-phosphatidic acid conjugates with gemcitabine and cytosine arabinoside.

    Science.gov (United States)

    Alexander, Richard L; Morris-Natschke, Susan L; Ishaq, Khalid S; Fleming, Ronald A; Kucera, Gregory L

    2003-09-11

    Cytosine arabinoside (ara-C) and gemcitabine (dFdC) are two standard chemotherapy drugs used in the treatment of patients with various cancers. To alter the pharmacokinetic and pharmacodynamic properties of these molecules, we conjugated a synthetic phospholipid to both ara-C and dFdC and investigated their chemotherapeutic potential. The dFdC conjugate had greater cytotoxic activity compared with the ara-C conjugate and demonstrated notable cytotoxicity against all human cell lines tested.

  1. Chemical Composition and Cytotoxic and Antibacterial Activities of the Essential Oil of Aloysia citriodora Palau Grown in Morocco

    OpenAIRE

    Moulay Ali Oukerrou; Mounir Tilaoui; Hassan Ait Mouse; Inass Leouifoudi; Abdeslam Jaafari; Abdelmajid Zyad

    2017-01-01

    The aim of this work is to investigate the in vitro cytotoxic and antibacterial effects of the essential oils of Aloysia citriodora Palau, harvested in different regions of Morocco. The chemical profile was established using gas chromatography-mass spectrometry analysis. The cytotoxic activity against P815, MCF7, and VERO cell lines as well as the normal human peripheral blood mononuclear cells (PBMCs) was evaluated using the MTT assay. Standard, ATCC, strains of bacteria (Escherichia coli, S...

  2. Design, synthesis and cytotoxic activity of certain novel chalcone analogous compounds.

    Science.gov (United States)

    El-Meligie, S; Taher, Azza T; Kamal, Aliaa M; Youssef, A

    2017-01-27

    A series of chalcone analogous compounds were designed and synthesized. Replacing/substituting the enone or ethylenic bridge of the parent chalcone with rigid heterocyclic moieties or substituted aromatic amines gave nineteen target compounds. Their cytotoxic activities were screened against both breast and liver cancer cells as well as breast and liver normal cells. Target compounds were also evaluated for their inhibition activity of tubulin beta polymerization. Target compound 2e, 3a, 3b, 3c, 4a-4d, 5a, 5b and 6 showed broad spectrum excellent anticancer activity against both MCF-7 and HepG2. Compound 4a showed the most TUBb inhibition activity. Copyright © 2016 Elsevier Masson SAS. All rights reserved.

  3. Antimalarial, antimicrobial, cytotoxic, DNA interaction and SOD like activities of tetrahedral copper(II) complexes

    Science.gov (United States)

    Mehta, Jugal V.; Gajera, Sanjay B.; Patel, Mohan N.

    2015-02-01

    The mononuclear copper(II) complexes with P, O-donor ligand and different fluoroquinolones have been synthesized and characterized by elemental analysis, electronic spectra, TGA, EPR, FT-IR and LC-MS spectroscopy. An antimicrobial efficiency of the complexes has been tested against five different microorganisms in terms of minimum inhibitory concentration (MIC) and displays very good antimicrobial activity. The binding strength and binding mode of the complexes with Herring Sperm DNA (HS DNA) have been investigated by absorption titration and viscosity measurement studies. The studies suggest the classical intercalative mode of DNA binding. Gel electrophoresis assay determines the ability of the complexes to cleave the supercoiled form of pUC19 DNA. Synthesized complexes have been tested for their SOD mimic activity using nonenzymatic NBT/NADH/PMS system and found to have good antioxidant activity. All the complexes show good cytotoxic and in vitro antimalarial activities.

  4. Antimicrobial activity and cytotoxicity of triterpenes isolated from leaves of Maytenus undata (Celastraceae).

    Science.gov (United States)

    Mokoka, Tsholofelo Abednego; McGaw, Lyndy Joy; Mdee, Ladislaus Kakore; Bagla, Victor Patrick; Iwalewa, Ezekiel Olugbenga; Eloff, Jacobus Nicolaas

    2013-05-20

    Plants of the genus Maytenus belong to the family Celastraceae and are widely used in folk medicine as anti-tumour, anti-asthmatic, analgesic, anti-inflammatory, antimicrobial and anti-ulcer agents, and as a treatment for stomach problems. The aim of this study was to isolate and identify active compounds with antifungal activity from Maytenus undata after a preliminary study highlighted promising activity in crude extracts. Sequential extracts of M. undata leaves prepared using hexane, dichloromethane (DCM), acetone and methanol (MeOH) were tested for activity against Cryptococcus neoformans, a fungal organism implicated in opportunistic infections. Bioassay-guided fractionation of the hexane extract using C. neoformans as test organism was carried out to isolate antifungal compounds. The cytotoxicity of compounds isolated in sufficient quantities was evaluated using a tetrazolium-based colorimetric cellular assay (MTT) and a haemagglutination assay (HA). The hexane extract was most active with an MIC of 20 μg/ml against C. neoformans. The triterpene compounds friedelin (1), epifriedelanol (2), taraxerol (3), 3-oxo-11α-methoxyolean-12-ene-30-oic acid (4), 3-oxo-11α-hydroxyolean-12-ene-30-oic acid (5) and 3,11-dihydroxyolean-12-ene-30-oic acid (6) were isolated. Compound 6 was isolated for the first time from a plant species. The antimicrobial activity of compounds 1, 3, 5 and 6 was determined against a range of bacteria and fungi implicated in opportunistic and nosocomial infections. Compounds 5 and 6 were the most active against all the tested microorganisms with MIC values ranging between 24 and 63 μg/ml, except against Staphylococcus aureus which was relatively resistant. Compounds 1 and 3 had a low toxicity with an LC50 > 200 μg/ml towards Vero cells in the MTT assay. Compounds 5 and 6 were toxic with LC50 values of 6.03±0.02 and 2.98±0.01 μg/ml, respectively. Compounds 1 and 3 similarly were not toxic to the red blood cells (RBCs) but compounds 5 and

  5. Bufadienolides with cytotoxic activity from the skins of Bufo bufo gargarizans.

    Science.gov (United States)

    Li, Bao-Jing; Tian, Hai-Yan; Zhang, Dong-Mei; Lei, Yu-He; Wang, Lei; Jiang, Ren-Wang; Ye, Wen-Cai

    2015-09-01

    Twelve new bufadienolides (1-12), along with fourteen known analogues (13-26) were isolated from the skins of Bufo bufo gargarizans Cantor. Their chemical structures were elucidated on the basis of NMR, HRESIMS and X-ray diffraction analysis. Compound 1 was an unusual bufadienolide with 3,19-epoxy moiety and A/B trans ring junction. Compounds 2-4 were rare bufadienolides possessing 10-H or 10-carboxyl units. All the isolated compounds were tested for their cytotoxic effects on HepG2, A549 and HeLa cells. Six new compounds (2, 3, 5, 6, 10 and 12) displayed significant anti-proliferative activities with IC50 values ranging from 0.049 to 1.856 μM. Arenobufagin (24) exhibited the most potent cytotoxic activity with IC50 value 0.011 μM. In addition, the present data provided more insight into the structure-activity relationships of bufadienolides. Copyright © 2015 Elsevier B.V. All rights reserved.

  6. Composition, antimicrobial activity and in vitro cytotoxicity of essential oil from Cinnamomum zeylanicum Blume (Lauraceae).

    Science.gov (United States)

    Unlu, Mehmet; Ergene, Emel; Unlu, Gulhan Vardar; Zeytinoglu, Hulya Sivas; Vural, Nilufer

    2010-11-01

    The essential oil from the bark of Cinnamomum zeylanicum Blume was analyzed by GC-MS and bioassays were carried out. Nine constituents representing 99.24% of the oil were identified by GC-MS. The major compounds in the oil were (E)-cinnamaldehyde (68.95%), benzaldehyde (9.94%) and (E)-cinnamyl acetate (7.44%). The antimicrobial activity of the oil was investigated in order to evaluate its efficacy against 21 bacteria and 4 Candida species, using disc diffusion and minimum inhibitory concentration methods. The essential oil showed strong antimicrobial activity against all microorganisms tested. The cytotoxic and apoptotic effects of the essential oil on ras active (5RP7) and normal (F2408) fibroblasts were examined by MTT assay and acridine orange/ethidium bromide staining, respectively. The cytotoxicity of the oil was quite strong with IC(50) values less than 20 μg/mL for both cell lines. 5RP7 cells were affected stronger than normal cells. Morphological observation of apoptotic cells indicated the induction of apoptosis at the high level of the oil, especially in 5RP7 cells. The present study showed the potential antimicrobial and anticarcinogenic properties of the essential oil of cinnamon bark, indicating the possibilities of its potential use in the formula of natural remedies for the topical treatment of infections and neoplasms. Copyright © 2010 Elsevier Ltd. All rights reserved.

  7. Limonoids from the fruits of Melia azedarach and their cytotoxic activities.

    Science.gov (United States)

    Akihisa, Toshihiro; Pan, Xin; Nakamura, Yasuhiro; Kikuchi, Takashi; Takahashi, Nami; Matsumoto, Masahiro; Ogihara, Eri; Fukatsu, Makoto; Koike, Kazuo; Tokuda, Harukuni

    2013-05-01

    Thirty-one limonoids and one tirucallane-type triterpenoid were isolated from the fruits of Melia azedarach (Meliaceae). The structures of 14 of these isolated compounds were elucidated on the basis of spectroscopic analyses and comparison with literature. All of these compounds were evaluated for their cytotoxic activities against HL60, A549, AZ521, and SK-BR-3 human cancer cell lines. Meliarachin C (IC50 0.65 μM) and 3-O-deacetyl-4'-demethyl-28-oxosalannin (IC50 2.8 μM) exhibited potent cytotoxic activity against HL60 cells, and this was demonstrated mainly due to the induction of apoptosis by flow cytometry. Western blot analysis suggested that both compounds induced apoptosis via both the mitochondrial and death receptor-mediated pathways. In addition, 25 compounds were evaluated for their inhibitory effects against the Epstein-Barr virus early antigen (EBV-EA) activation induced by 12-O-tetradecanoylphorbol-13-acetate (TPA) in Raji cells. Copyright © 2013 Elsevier Ltd. All rights reserved.

  8. ANTIBACTERIAL AND CYTOTOXIC ACTIVITY OF BACILLUS METHYLOTROPHICUS-SCS2012 ISOLATED FROM SOIL

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    Subed Chandra Dev Sharma

    2013-02-01

    Full Text Available The strain Bacillus methylotrophycus-SCS2012 (Bacillus sp. SCS2012 identified by 16S rRNA gene sequencing was isolated from soil. Ethyl acetate extract of B. methylotrophycus-SCS2012 showed antibacterial activity against both Gram positive and Gram negative bacteria. The crude metabolite extracted from B. methylotrophycus-SCS2012 exhibited strong antibacterial activity against Streptococcus agalactae, Bacillus cereus, Escherichia coli, Shigella sonnei and Shigella dysenteriae with the zone of inhibition range 28.33 to 32.16 mm at 100μg/disc. Minimum inhibitory concentration (MIC of the extract against Streptococcus agalactae, Bacillus cereus, Escherichia coli, Shigella sonnei and Shigella dysenteriae was found to be 156, 156, 312, 312 and 625µg/ml respectively. The ethyl acetate extract also exhibited cytotoxic effects on brine shrimp lethality bioassay with LC50 value of 10.78 g/ml. Thus the ethyl acetate extract of Bacillus methylotrophycus-SCS2012 has broad spectrum activity with moderate cytotoxicity.

  9. Synthesis and Cytotoxic Activity of Biphenylurea Derivatives Containing Indolin-2-one Moieties

    Directory of Open Access Journals (Sweden)

    Wagdy M. Eldehna

    2016-06-01

    Full Text Available In our endeavor towards the development of potent anticancer agents, two different sets of biphenylurea-indolinone conjugates, 5a–s and 8a,b were synthesized. The in vitro cytotoxicity of the synthesized compounds was examined in two human cancer cell lines, namely MCF-7 breast cancer and PC-3 prostate cancer cells using the sulforhodamine B (SRB colorimetric assay. In particular, the MCF-7 cancer cell line was more susceptible to the synthesized compounds. Compound 5o (IC50 = 1.04 ± 0.10 μM emerged as the most active member in this study against MCF-7, with 7-fold increased activity compared to the reference drug, doxorubicin (IC50 = 7.30 ± 0.84 μM. Compounds 5l, 5q and 8b also exhibited superior cytotoxic activity against MCF-7 with IC50 values of 1.93 ± 0.17, 3.87 ± 0.31 and 4.66 ± 0.42 μM, respectively. All of the tested compounds were filtered according to the Lipinski and Veber rules and all of them passed the filters. Additionally, several ADME descriptors for the synthesized compounds 5a–s and 8a,b were predicted via a theoretical kinetic study performed using the Discovery Studio 2.5 software.

  10. Imidazole Alkaloids from the South China Sea Sponge Pericharax heteroraphis and Their Cytotoxic and Antiviral Activities

    Directory of Open Access Journals (Sweden)

    Kai-Kai Gong

    2016-01-01

    Full Text Available Marine sponges continue to serve as a rich source of alkaloids possessing interesting biological activities and often exhibiting unique structural frameworks. In the current study, chemical investigation on the marine sponge Pericharax heteroraphis collected from the South China Sea yielded one new imidazole alkaloid named naamidine J (1 along with four known ones (2–5. Their structures were established by extensive spectroscopic methods and comparison of their data with those of the related known compounds. All the isolates possessed a central 2-aminoimidazole ring, substituted by one or two functionalized benzyl groups in some combination of the C4 and C5 positions. The cytotoxicities against selected HL-60, HeLa, A549 and K562 tumor cell lines and anti-H1N1 (Influenza a virus (IAV activity for the isolates were evaluated. Compounds 1 and 2 exhibited cytotoxicities against the K562 cell line with IC50 values of 11.3 and 9.4 μM, respectively. Compound 5 exhibited weak anti-H1N1 (influenza a virus, IAV activity with an inhibition ratio of 33%.

  11. Stilbenes with anti-inflammatory and cytotoxic activity from the rhizomes of Bletilla ochracea Schltr.

    Science.gov (United States)

    Li, Jin-Yu; Kuang, Meng-Ting; Yang, Liu; Kong, Qing-Hua; Hou, Bo; Liu, Zhen-Hua; Chi, Xiao-Qian; Yuan, Ming-Yan; Hu, Jiang-Miao; Zhou, Jun

    2018-02-05

    Four new dihydrophenanthrenofuran, bleochranols A-D (1-4), along with 21 known compounds including phenanthrenes (5-14) and bibenzyls (15-25) were isolated and elucidated from the rhizomes of Bletilla ochracea. Combination of 1D/2D NMR techniques and the Electronic Circular Dichroism (ECD) spectroscopy based on the empirical helicity rules, chemical structure of those isolates were determined. All the compounds were evaluated for cytotoxicity against HL-60, SMMC-7721, A-549, MCF-7 and SW480 human cancer cell lines by MTS assay and anti-inflammatory activity by nitric oxide (NO) production in LPS-stimulated RAW 264.7 macrophages. Among the 25 tested compounds, bleochranol A (1) showed remarkable cytotoxic activity against HL-60, A-549, and MCF-7 with IC 50 values of 0.24 ± 0.03, 3.51 ± 0.09 and 3.30 ± 0.99 μM respectively. The anti-inflammatory assay showed that compound 12 exhibited most potential activity against NO production in RAW 264.7 macrophages with IC 50 2.86 ± 0.17 μM. The results indicated that the main chemical constituents of B. ochracea were phenanthrene and bibenzyl and similar to that of B. striata. Copyright © 2018 Elsevier B.V. All rights reserved.

  12. LC-ESI-MS/MS and cytotoxic activity of three Pistacia species.

    Science.gov (United States)

    Kirollos, F N; Elhawary, S S; Salama, O M; Elkhawas, Y A

    2018-01-28

    LC-ESI-MS/MS was used for a comprehensive characterisation of ethanol extract from the leaves of three Pistacia species. After optimisation of the method and the use of the negative ionisation mode, a total of 42 different compounds were identified, of which 22 were tentatively characterised in P. chinensis Bunge, 33 in P. khinjuk stocks and 25 in P. lentiscus L. leaves. Flavonoids, phenolic acids, and their derivatives were the most abundant identified compounds. LC-ESI-MS/MS revealed identification of 15, 18 and 6 not previously detected compounds in P. chinensis Bunge, P. khinjuk Stocks and P. lentiscus L., respectively. The three extracts were also tested for their cytotoxic activities against human PC3 prostate cancer, A549 lung cancer, MCF7 breast cancer and HepG2 liver cancer. Generally, all the extracts have a moderate cytotoxic activity against lung, breast and prostate cancer, with different IC50. However, only P. lentiscus L. showed moderate activity against liver cancer.

  13. In vitro evaluation of triazenes: DNA cleavage, antibacterial activity and cytotoxicity against acute myeloid leukemia cells

    Energy Technology Data Exchange (ETDEWEB)

    Domingues, Vanessa O.; Hoerner, Rosmari; Reetz, Luiz G.B.; Kuhn, Fabio, E-mail: rosmari.ufsm@gmail.co [Universidade Federal de Santa Maria (UFSM), RS (Brazil). Dept. de Analises Clinicas e Toxicologicas; Coser, Virginia M.; Rodrigues, Jacqueline N.; Bauchspiess, Rita; Pereira, Waldir V. [Hospital Universitario de Santa Maria, RS (Brazil). Dept. de Hematologia-Oncologia; Paraginski, Gustavo L.; Locatelli, Aline; Fank, Juliana de O.; Giglio, Vinicius F.; Hoerner, Manfredo, E-mail: hoerner.manfredo@gmail.co [Universidade Federal de Santa Maria (UFSM), RS (Brazil). Dept. de Quimica

    2010-07-01

    The asymmetric diazoamines 1-(2-chlorophenyl)-3-(4-carboxyphenyl)triazene (1), 1-(2-fluorophenyl)-3-(4-carboxyphenyl)triazene (2) and 1-(2-fluorophenyl)-3-(4-amidophenyl) triazene (3) were evaluated for their ability to cleave pUC18 and pBSKII plasmid DNA, antibacterial activity and in vitro cytotoxicity against acute myeloid leukemia cells and normal leukocytes using the bioassay of reduction of 3-(4,5-dimethylthiazole-2-yl)-2,5-diphenyltetrazolium bromide (MTT). The triazenes showed ability to cleave the two types of plasmid DNA: triazene 1 at pH 8.0 and 50 deg C; triazene 2 at pH 6.5 and 37 and 50 deg C; triazene 3 at pH 6.5 and 37 deg C. The compounds presented cytotoxic activity against myeloid leukemia cells. Compound 1 showed high activity against B. cereus (MIC = 32 {mu}g mL{sup -1}). The observation of intermolecular hydrogen bonding in the solid state of compound 3, based on the structural analysis by X-ray crystallography, as well as the results of IR and UV-Vis spectroscopic analyses of compounds 1, 2 and 3 are discussed in the present work. (author)

  14. Screening of indigenous Palestinian medicinal plants for potential anti-inflammatory and cytotoxic activity.

    Science.gov (United States)

    Kaileh, Mary; Vanden Berghe, Wim; Boone, Elke; Essawi, Tamer; Haegeman, Guy

    2007-09-25

    Organic extracts of 24 selected plant species, used by Palestinian traditional healers to treat different illnesses and diseases, were tested for their anti-inflammatory and anti-tumoral activities. The plant selection was based on existing ethnobotanic information and interviews with local healers. The extracts of the plants under investigation were tested for their potential anti-tumor (cytotoxic) effect on the murine fibrosarcoma L929sA cells, and on the human breast cancer cells MDA-MB231 and MCF7. Cytotoxicity screening models provide important preliminary data to select plant extracts with potential antineoplastic properties. MTT (Tetrazolium blue) colorimetric assay was used to evaluate the reduction of viability of cell cultures in the presence or absence of the extracts. The extract from Withania somnifera, L. Dunal (Solanaceae) presented an IC(50) value at 24h of 150 and 60 microg/ml, on L929sA and MCF7 cells, respectively, while the extract from Psidium guajava L. (Myrtaceae) presented an IC(50) value at 24h of 55 microg/ml on MCF7 cells. Other extracts examined, like Laurus nobilis L. (Lauraceae) and Salvia fruticosa M. (Labiatae), also displayed a remarkable activity. Additionally, as the nuclear transcription factor NFkappaB regulates the expression of various genes that play critical roles in apoptosis and immunomodulation, we further investigated the effect of nine promising plant extracts, withheld from the first cell viability screening on NFkappaB activation. The extracts showed variable degrees of NFkappaB-inhibitory activity. Whereas Withania somnifera extract demonstrated the strongest NFkappaB-inhibitory activity, other extracts derived from Laurus nobilis, Psidium guajava and Foeniculum vulgare M. (Umbiliferrae) also revealed immunomodulatory NFkappaB activities. These species are good candidates for further activity-monitored fractionation to identify active constituents.

  15. Cytotoxicity and acetylcholinesterase inhibitory activity of an isolated crinine alkaloid from Boophane disticha (Amaryllidaceae).

    Science.gov (United States)

    Adewusi, Emmanuel Adekanmi; Fouche, Gerda; Steenkamp, Vanessa

    2012-09-28

    Boophane disticha of the family Amaryllidaceae is used traditionally in southern Africa in the treatment of several neurological disorders. Although acetylcholinesterase (AChE) inhibitory activity has been reported for this plant, the aim of the study was to identify and characterise the compound responsible for this activity using bioassay guided fractionation. Toxicity of the isolated compound was also assessed. Bioassay guided isolation of the active compound from the methanol extract was carried out using column chromatography, TLC and preparative thin layer chromatography. Structural elucidation was carried out using high field 1D and 2D NMR and mass spectroscopy. AChE inhibitory activity was determined using the Ellman's colorimetric method. Cytotoxicity assessment was determined in human neuroblastoma (SH-SY5Y) cells using the MTT and neutral red uptake assays. The data obtained from the integration of the (1)H spectra confirmed the compound to be a 3:1 mixture of two epimers, with epimer A, 6α-hydroxycrinamine as the major epimer. The IC(50) value for AChE inhibitory activity of the compound was 445 μM. The compound was observed to be cytotoxic in both the MTT and neutral red assays with IC(50) values of 54.5 and 61.7 μM, respectively. The present study describes for the first time, the isolation of 6-hydroxycrinamine, a crinine alkaloid, from the methanol extract of the bulbs of B. disticha. Although this compound possessed AChE inhibitory activity, it was found to be toxic to the neuroblastoma cells. Quantitative structure-activity relationship studies could be carried out to modify the structure in order to make it less toxic and improve its activity. Copyright © 2012 Elsevier Ireland Ltd. All rights reserved.

  16. Cytotoxic Activities, SAR and Anti-Invasion Effects of Butylphthalide Derivatives on Human Hepatocellular Carcinoma SMMC7721 Cells

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    Yihan Hu

    2015-11-01

    Full Text Available A series of butylphthalide derivatives (BPDs 1–8 were isolated from the extract of the dried rhizome of Ligusticum chuanxiong Hort. (Umbelliferae. The cytotoxic activities of BPDs 1–8 were evaluated using a panel of human cancer cell lines. In addition, the SAR analysis and potential anti-invasion activities were investigated. The sp2 carbons at C-7 and C-7a appeared to be essential for the cytotoxic activities of BPDs. BPDs 5 and 6 remarkably inhibited the migration and invasion of cancer cells. The anti-invasion activity of dimer 6 was demonstrated to be significantly higher than monomer 5.

  17. Novel relationship between the antifungal activity and cytotoxicity of marine-derived metabolite xestoquinone and its family.

    Science.gov (United States)

    Nakamura, Mitsuhiro; Kakuda, Takahiko; Qi, Jianhua; Hirata, Masayuki; Shintani, Tomoaki; Yoshioka, Yukio; Okamoto, Tetsuji; Oba, Yuichi; Nakamura, Hideshi; Ojika, Makoto

    2005-09-01

    Xestoquinone and related metabolites (the xestoquinone family) occur in marine sponges and are known to show a variety of biological activities. In this study, the first comprehensive evaluation of antifungal activity was performed for xestoquinone and nine natural and unnatural analogues in comparison with their cytotoxicity. The cytotoxicity against two human squamous cell carcinoma cell lines, A431 and Nakata, indicated that the terminal quinone structure of the polycyclic molecules was important (xestoquinone, etc.) and that the presence of a ketone group at C-3 of the opposite terminus dramatically diminished the activity (halenaquinone, etc.). In contrast, a ketone group at C-3 enhanced the antifungal activity against the plant pathogen, Phytophthora capsici, regardless of the presence of a quinone moiety. The cytotoxicity and antifungal activity of the xestoquinone family were negatively correlated with each other.

  18. Antioxidant and cytotoxic activities of 'acai' (Euterpe precatoria Mart.)

    Energy Technology Data Exchange (ETDEWEB)

    Galotta, Ana Lucia Q.A. [Universidade Federal do Amazonas (UFAM), Manaus, AM (Brazil). Inst. de Ciencias Exatas. Dept. de Quimica; Boaventura, Maria Amelia D.; Lima, Luciana A. R.S. [Universidade Federal de Minas Gerais (UFMG), Belo Horizonte, MG (Brazil). Dept. de Quimica

    2008-07-01

    Decoction of roots of the Amazonian palm acai (Euterpe precatoria Mart.) is widely used by Brazilian and Peruvian people as an anti-inflammatory, to heal kidney and liver diseases and against snake bites. In this study, the antioxidant activity of extracts and flavonoids (quercetin, catechin, epicatechin, rutin and astilbin) isolated from roots and leaf stalks of E. precatoria was investigated using {beta}-carotene in TLC plates and DPPH radical scavenging in a spectrophotometric bioassay. All extracts and flavonoids showed activity. Also, the cytotoxic activity of these extracts was evaluated by the brine shrimp (Artemia salina) larvicide bioassay and was lower than that of lapachol, used as control. The presence of flavonoids and sitosterol-3-O-{beta}-D-glucopyranoside in the extracts can justify the use of the plant in traditional medicine. (author)

  19. Chemical Composition, Biological and Cytotoxic Activities of Plant Extracts and Compounds Isolated from Ferula lutea

    Directory of Open Access Journals (Sweden)

    Mansour Znati

    2014-02-01

    Full Text Available The present work describes the phytochemical study on Ferula lutea flowers. Total phenolics and flavonoids of the n-butanol and ethyl acetate extracts were quantified (phenolics [40.68–52.29 mg gallic acid equivalent/g of dry weight], flavonoids [12.38–14.72 mg quercitin/g dry weight]. Two diastereoisomers were isolated and identified using spectroscopic techniques (1D, 2D NMR and GC-MS. The extracts and diastereoisomers were tested for antioxidant, antiacetylcholinesterase, antimicrobial, antidiabectic, cytotoxic (leukemia cell line activities and allelopathic potentialities. The strongest antioxidant activity was obtained for the ethyl acetate extract (IC50 = 12.8 ± 1.29 µg/mL. The two extracts exhibited high antidiabetic activity (54.1 and 52.1% at 40 µg/mL.

  20. In vitro antiplasmodial and cytotoxic activities of sesquiterpene lactones from Vernonia fimbrillifera Less. (Asteraceae).

    Science.gov (United States)

    Bordignon, Annélise; Frédérich, Michel; Ledoux, Allison; Campos, Pierre-Eric; Clerc, Patricia; Hermann, Thomas; Quetin-Leclercq, Joëlle; Cieckiewicz, Ewa

    2017-07-10

    Due to the in vitro antiplasmodial activity of leaf extracts from Vernonia fimbrillifera Less. (Asteraceae), a bioactivity-guided fractionation was carried out. Three sesquiterpene lactones were isolated, namely 8-(4'-hydroxymethacrylate)-dehydromelitensin (1), onopordopicrin (2) and 8α-[4'-hydroxymethacryloyloxy]-4-epi-sonchucarpolide (3). Their structures were elucidated by spectroscopic methods (1D and 2D NMR and MS analyses) and by comparison with published data. The isolated compounds exhibited antiplasmodial activity with IC50 values ≤ 5 μg/mL. Cytotoxicity of the compounds against a human cancer cell line (HeLa) and a mouse lung epithelial cell line (MLE12) was assessed to determine selectivity. Compound 3 displayed promising selective antiplasmodial activity (SI > 10).

  1. Effects of sulfate group in red seaweed polysaccharides on anticoagulant activity and cytotoxicity.

    Science.gov (United States)

    Liang, Wanai; Mao, Xuan; Peng, Xiaohui; Tang, Shunqing

    2014-01-30

    In this paper, the structural effects of two main red seaweed polysaccharides (agarose and carrageenan) and their sulfated derivatives on the anticoagulant activity and cytotoxicity were investigated. The substitution position rather than the substitution degree of sulfate groups shows the biggest impact on both the anticoagulant activity and the cell proliferation. Among them, C-2 of 3,6-anhydro-α-d-Galp is the most favorable position for substitution, whereas C-6 of β-d-Galp is the most disadvantageous. Moreover, the secondary structures of glycans also play a key role in biological activities. These demonstrations warrant that the red seaweed polysaccharides should be seriously considered in biomedical applications after carefully tailoring the sulfate groups. Copyright © 2013 Elsevier Ltd. All rights reserved.

  2. Stability and Antioxidant Activity of Semi-synthetic Derivatives of 4-Nerolidylcatechol

    Directory of Open Access Journals (Sweden)

    Emerson Silva Lima

    2012-12-01

    Full Text Available 4-nerolidylcatechol (4-NC is an unstable natural product that exhibits important antioxidant, anti-inflammatory and other properties. It is readily obtainable on a multi-gram scale through straightforward solvent extraction of the roots of cultivated Piper peltatum or P. umbellatum, followed by column chromatography on the resulting extract. Semi-synthetic derivatives of 4-NC with one or two substituent groups (methyl, acetyl, benzyl, benzoyl on the O atoms have been introduced that have increased stability compared to 4-NC and significant in vitro inhibitory activity against the human malaria parasite Plasmodium falciparum. Antioxidant and anti-inflammatory properties may be important for the antiplasmodial mode of action of 4-NC derivatives. Thus, we decided to investigate the antioxidant properties, cytotoxicity and stability of 4-NC derivatives as a means to explore the potential utility of these compounds. 4-NC showed high antioxidant activity in the DPPH and ABTS assays and in 3T3-L1 cells (mouse embryonic fibroblast, however 4-NC was more cytotoxic (IC50 = 31.4 µM and more unstable than its derivatives and lost more than 80% of its antioxidant activity upon storage in solution at −20 °C for 30 days. DMSO solutions of mono-O-substituted derivatives of 4-NC exhibited antioxidant activity and radical scavenging activity in the DPPH and ABTS assays that was comparable to that of BHA and BHT. In the cell-based antioxidant model, most DMSO solutions of derivatives of 4-NC were less active on day 1 than 4-NC, quercetin and BHA and more active antioxidants than BHT. After storage for 30 days at −20 °C, DMSO solutions of most of the derivatives of 4-NC were more stable and exhibited more antioxidant activity than 4-NC, quercetin and BHA and exhibited comparable antioxidant activity to BHT. These findings point to the potential of derivatives of 4-NC as antioxidant compounds.

  3. Antibacterial and Cytotoxic Activity of Extracts and Isolated Compounds from Myrciariaferruginea (Myrtaceae

    Directory of Open Access Journals (Sweden)

    Cinthia Costa de Lima

    2017-01-01

    Full Text Available This study evaluated for the first time the antibacterial activity, cell viability and migration ability on 3T3 murine fibroblast cells of extracts and isolated compounds [lupeol (1, hexamethylcoruleoellagic acid (2 and a mixture of 1 and betulinaldehyde (3] of Myrciaria ferruginea. In antibacterial assays extracts were susceptible only against S. aureus (MIC 500 μg/mL and S. epidermidis (MIC ranging from 7.8 to 500 μg/mL and compounds 1-3have shown no significant activity. In trials for c ell viability, with exception of MeOH-H 2O fraction from leaves (viable cells > 90%, both the crude extract and other fractions showed inhibition of cell growth (viable cells ≤ 80% at 15.625 and 31.25 μg/mL; while the samples from stems, with the exception of CHCl 3 fraction that showed strong cytotoxic effect at the lowest concentration tested (15.625 μg/mL, the other fractions were not cytotoxic. Compounds (1-3 inhibited cell viability in dose dependent manner (15.625 to 500 μg/mL. Mixture containing 1 and 3 showed inhibitions only in concentrations greater than 62.5 μg/mL while compound 2 decreased from the lowest concentration tested. In scratch wound assay, these compoundsnot increased the population of fibroblasts at concentrations less than 62.5 μg/mL.

  4. Sesquiterpene lactones: Mechanism of antineoplastic activity; relationship of cellular glutathione to cytotoxicity; and disposition

    Energy Technology Data Exchange (ETDEWEB)

    Grippo, A.A.

    1987-01-01

    Helenalin, a sesquiterpene lactone, inhibited the growth of P388 lymphocytic and L1210 lymphoid leukemia, and Ehrlich ascites and KB carcinoma cells. The L1210 leukemia cells were most sensitive to the cytotoxic effects of helenalin. Helenalin's antineoplastic effects were due to inhibition of DNA synthesis by suppressing the activities of enzymes involved in this biosynthetic pathway; i.e., IMP dehydrogenase, ribonucleoside diphosphate reductase, thioredoxin complex, GSH disulfide oxidoreductase and DNA polymerase {alpha} activities. The relationship of reduced glutathione (GSH) to the cytotoxic effects of helanalin was evaluated. L1210 cells, which were more sensitive to helenalin's toxicity, contained lower basal concentrations of GSH. Helenalin decreased the concentration of reduced glutathione in both L1210 and P388 leukemia cells. Concurrent administration of helanalin with agents reported to raise GSH concentrations did not substantially effect GSH levels, nor were survival times of tumor-bearing mice enhanced. Following intraperitoneal administration of {sup 3}H-plenolin, no radioactive drug and/or metabolite was sequestered in the organs of BDF{sub 1} mice. Approximately 50% of {sup 3}H-plenolin and/or its metabolites were eliminated via urine while lesser amounts of radioactive drug and/or metabolites were eliminated in the feces.

  5. Antibacterial Activity, in Vitro Cytotoxicity, and Cell Cycle Arrest of Gemini Quaternary Ammonium Surfactants.

    Science.gov (United States)

    Zhang, Shanshan; Ding, Shiping; Yu, Jing; Chen, Xuerui; Lei, Qunfang; Fang, Wenjun

    2015-11-10

    Twelve gemini quaternary ammonium surfactants have been employed to evaluate the antibacterial activity and in vitro cytotoxicity. The antibacterial effects of the gemini surfactants are performed on Escherichia coli (E. coli) and Staphylococcus aureus (S. aureus) with minimum inhibitory concentrations (MIC) ranging from 2.8 to 167.7 μM. Scanning electron microscopy (SEM) analysis results show that these surfactants interact with the bacterial cell membrane, disrupt the integrity of the membrane, and consequently kill the bacteria. The data recorded on C6 glioma and HEK293 human kidney cell lines using an MTT assay exhibit low half inhibitory concentrations (IC50). The influences of the gemini surfactants on the cell morphology, the cell migration ability, and the cell cycle are observed through hematoxylin-eosin (HE) staining, cell wound healing assay, and flow cytometric analyses, respectively. Both the values of MIC and IC50 decrease against the growth of the alkyl chain length of the gemini surfactants with the same spacer group. In the case of surfactants 12-s-12, the MICs and IC50s are found to decrease slightly with the spacer chain length changing from 2 to 8 and again to increase at higher spacer length (s = 10-12). All of the gemini surfactants show great antibacterial activity and cytotoxicity, and they might exhibit potential applications in medical fields.

  6. Cetuximab Enhanced the Cytotoxic Activity of Immune Cells during Treatment of Colorectal Cancer

    Directory of Open Access Journals (Sweden)

    Lin Wang

    2017-11-01

    Full Text Available Background/Aims: Cetuximab is a chimeric IgG1 monoclonal antibody which targets the extracellular domain of epidermal growth factor receptor. This antibody is widely used for colorectal cancer (CRC treatment but its influence on the immune system is incompletely understood. Methods: The immune influence of cetuximab therapy in CRC patients was investigated by analyzing peripheral blood mononuclear cells using flow cytometry. We undertook in vitro cytotoxicity and cytokine-profile assays to ascertain the immunomodulatory effect of cetuximab treatment. Results: The number of CD3+ T, CD8+ T, and natural killer (NK cells was increased significantly and T-regulatory cells reduced gradually after cetuximab treatment. Percentage of CD4+ T, natural killer T (NKT-like, invariant NKT, and dendritic cells was similar between baseline patients and cetuximab patients. Expression of CD137 on NK and CD8+ T cells was increased significantly after 4 weeks of cetuximab therapy. In vitro cetuximab treatment markedly increased expression of CD137 and CD107a on NK and CD8+ T cells. Cetuximab treatment promoted the cytotoxic activity of NK and CD8+ T cells against tumor cells. Conclusion: Cetuximab treatment promotes activation of the immune response but alleviates immunosuppression: this might be the underlying anti-CRC effect of cetuximab.

  7. Calcium phosphate coating containing silver shows high antibacterial activity and low cytotoxicity and inhibits bacterial adhesion

    Energy Technology Data Exchange (ETDEWEB)

    Ando, Yoshiki, E-mail: andoy@jmmc.jp [Division of Microbiology, Department of Pathology and Microbiology, Faculty of Medicine, Saga University, 5-1-1 Nabeshima, Saga 849-8501 (Japan); Research Department, Japan Medical Materials Corporation, Uemura Nissei Bldg.9F 3-3-31 Miyahara, Yodogawa-ku, Osaka 532-0003 (Japan); Miyamoto, Hiroshi [Division of Microbiology, Department of Pathology and Microbiology, Faculty of Medicine, Saga University, 5-1-1 Nabeshima, Saga 849-8501 (Japan); Noda, Iwao; Sakurai, Nobuko [Research Department, Japan Medical Materials Corporation, Uemura Nissei Bldg.9F 3-3-31 Miyahara, Yodogawa-ku, Osaka 532-0003 (Japan); Akiyama, Tomonori [Division of Microbiology, Department of Pathology and Microbiology, Faculty of Medicine, Saga University, 5-1-1 Nabeshima, Saga 849-8501 (Japan); Yonekura, Yutaka; Shimazaki, Takafumi; Miyazaki, Masaki; Mawatari, Masaaki; Hotokebuchi, Takao [Department of Orthopaedic Surgery, Faculty of Medicine, Saga University, 5-1-1 Nabeshima, Saga 849-8501 (Japan)

    2010-01-01

    Surgical site infection is one of the serious complications of orthopedic implants. In order to reduce the incidence of implant-associated infections, we developed a novel coating technology of calcium phosphate (CP) containing silver (Ag), designated Ag-CP coating, using a thermal spraying technique. In this study, we evaluated the antibacterial efficacy and biological safety of this coating. In vitro antibacterial activity tests showed that the growths of Escherichia coli, Staphylococcus aureus and methicillin-resistant S. aureus (MRSA) are completely suppressed on Ag-CP coating. In vitro bacterial adherence tests revealed that the number of adherent bacteria on the surface of this coating is significantly less (p < 0.02) than that on the surface of the CP coating. Moreover, the Ag-CP coating completely inhibits MRSA adhesion [<10 colony-forming units (CFU)] when 10{sup 2} CFU MRSA is inoculated. On the other hand, V79 Chinese hamster lung cells were found to grow on the Ag-CP coating as well as on the CP coating in a cytotoxicity test. These results indicate that the Ag-CP coating on the surface of orthopedic implants exhibits antibacterial activity and inhibits bacterial adhesion without cytotoxicity.

  8. Cytotoxic and Apoptotic Activities of Prunus spinosa Trigno Ecotype Extract on Human Cancer Cells

    Directory of Open Access Journals (Sweden)

    Stefania Meschini

    2017-09-01

    Full Text Available The aim of this work was to demonstrate that a natural compound, not-toxic to normal cells, has cytotoxic and sensitizing effects on carcinoma cells, with the final goal of combining it with chemotherapeutic drugs to reduce the overall dose. Prunus spinosa Trigno ecotype (PsT drupe extract with a nutraceutical activator complex (NAC made of amino acids, vitamins and mineral salt blends, has shown in vitro anticancer activity. The cytotoxic effect of (PsT + NAC® has been evaluated on human cancer cells, with an initial screening with colorectal, uterine cervical, and bronchoalveolar cells, and a subsequent focus on colon carcinoma cells HCT116 and SW480. The viability reduction of HCT116 and SW480 after treatment with (PsT 10 mg/mL + NAC® was about 40% (p < 0.05, compared to control cells. The cell’s survival reduction was ineffective when the drug vehicle (NAC was replaced with a phosphate buffer saline (PBS or physiological solution (PS. The flow cytometry evaluation of cancer cells’ mitochondrial membrane potential showed an increase of 20% depolarized mitochondria. Cell cycle analysis showed a sub G1 (Gap 1 phase peak appearance (HCT116: 35.1%; SW480: 11.6%, indicating apoptotic cell death induction that was confirmed by Annexin V assay (HCT116: 86%; SW480: 96%. Normal cells were not altered by (PsT + NAC® treatments.

  9. Synthesis, antimicrobial and cytotoxic activity of novel azetidine-2-one derivatives of 1H-benzimidazole

    Directory of Open Access Journals (Sweden)

    Malleshappa Noolvi

    2014-04-01

    Full Text Available A series of 1-methyl-N-[(substituted-phenylmethylidene-1H-benzimidazol-2-amines (4a–4g were prepared via the formation of 1-methyl-1H-benzimidazol-2-amine (3, which was prepared by the cycloaddition of o-phenylenediamine (1 with cyanogen bromide in the presence of aqueous base followed by N-methylation with methyl iodide in the presence of anhydrous potassium carbonate in dry acetonitrile. Moreover, the four-membered β-lactam ring was introduced by the cycloaddition of 4a–4g and chloroacetyl chloride in the presence of triethylamine catalyst to give 3-chloro-1-(1-methyl-1H-benzimidazol-2-yl-(4′-substituted-phenylazetidin-2-one 5a–5g. A total of 14 compounds were synthesized and characterized by IR, 1H NMR, 13C NMR and Mass spectral technique, in addition they were evaluated for anti-bacterial and cytotoxic properties. Among the chemicals tested 4a, 4b, 5a, 5b, 5g exhibited good antibacterial activity and 5f, 5g shown good cytotoxic activity in vitro.

  10. Antimicrobial activity, cytotoxicity and inflammatory response of novel plastics embedded with silver nanoparticles.

    Science.gov (United States)

    Martínez-Gutiérrez, Fidel; Guajardo-Pacheco, Jesús M; Noriega-Trevino, María E; Thi, Emily P; Reiner, Neil; Orrantia, Erasmo; Av-Gay, Yossef; Ruiz, Facundo; Bach, Horacio

    2013-03-01

    Infections associated with medical devices are an important cause of morbidity and mortality. Microorganisms are responsible for catheter infections that may then result in the local or systemic dissemination of the microorganism into the bloodstream. The aim of this study was to evaluate the antimicrobial activity of silver nanoparticles (AgNPs) embedded in polyurethane plastics, commonly used for catheter fabrication. AgNPs in the range of 25-30 nm were synthesized and embedded in polyurethane plastics at different concentrations. The antimicrobial activities of these plastics were tested against the three pathogenic microorganisms, Escherichia coli, Staphylococcus epidermidis and Candida albicans, frequently associated with catheter infections. The cytotoxicity of the plastics was evaluated on human-derived macrophages using propidium iodide and the secretion of the pro- and anti-inflammatory cytokines IL-6, IL-10 and TNF-a was measured using ELISA. A significant reduction of 6- to 7-log in the number of bacteria was measured, while a reduction of 90% was measured in the case of C. albicans. Neither cytotoxic effect on macrophages nor immunological response was observed. Plastics embedded with AgNPs have great potential to limit microbial colonization of implanted medical devices.

  11. [Cytotoxicity of Naja Naja Actra Venom Component combined with activated immune cells on leukemia cell line KG1a].

    Science.gov (United States)

    He, Yan-Jie; Li, Yu-Hua; Tu, San-Fang; Wu, Hai-Yan; Guo, Kun-Yuan

    2013-10-01

    This study was aimed to investigate the cytotoxic effect of the Naja Naja Actra Venom Component (NNAVC) combined with activated immune cells on human acute myeloblastic leukemia line KG1a cells. The cytotoxic effects of NNAVC at different concentrations on KG1a cells were measured by CCK-8 method. LDH releasing assay was used to detect the cytotoxic effects of activated immune cells, NNAVC combined with activated immune cells on KG1a cells and the sensitivity of KG1a treated with NNAVC to activated immune cells. The results showed that the inhibitory rate of NNAVC on KG1a cells increased with the concentration enhancement, the cytotoxicity of activated immune cells at the different effector to target (E:T) ratios(6.25:1, 12.5:1, 25:1) on KG1a cells were 12.30%, 24.85% and 52.26%. The cytotoxicity of NNAVC combined with activated immune cells at the different E:T cell ratios (10:1, 20: 1) on KG1a cells were 56.21% and 85.59%, which were higher than that of NNAVC or activated immune cells alone. The cytotoxicity of activated immune cells at the E: T cell ratio of 10:1 on KG1a cells treated with NNAVC at different concentrations were 25.65%, 31.33%, 28.63% and 16.78%, respectively, and that at the E:T cell ratio of 20: 1 were 40.62%, 44.70%, 44.62% and 40.72%. It is concluded that:both of NNAVC and activated immune cells have lethal effect on KG1a cells, and the combination of NNAVC and activated immune cells can strengthen their effect on KG1a.

  12. Cytotoxic and Nitric Oxide Inhibition Activities of Propolis Extract along with Microencapsulation by Complex Coacervation.

    Science.gov (United States)

    Onbas, Rabia; Kazan, Aslihan; Nalbantsoy, Ayse; Yesil-Celiktas, Ozlem

    2016-09-01

    In this study, cytotoxicity of ethanol extract of propolis (EEP) originating from Sivas, Turkey was screened against several cancer cell lines, namely PC-3, U87MG, A-549, mPANC96, CaCo-2, MCF-7, HeLa, MDA-MB-231 and a non-tumor cell line HEK293 by MTT assay. The inhibition levels of inducible nitric oxide synthase (iNOS) were also determined by using RAW 264.7 macrophage cells following lipopolysaccharide (LPS) treatment. EEP exhibited significant cytotoxic nitric oxide inhibition activities with an IC50 value of 0.1 ± 0.1 μg/ml indicating a high potential as an anti-inflammatory agent. In spite of these promising results and the fact that propolis is a highly nutritive substance, its low solubility and bitter taste limit the applications as a natural supplement. Encapsulation might serve as a good strategy in order to overcome these problems. Complex coacervation was applied where the main focus was on surfactant type, polymer ratio (alginate:gelatin), stirring rate and concentration of core material. The mean particle size of unloaded microparticles were 22.62 μm obtained with gelatin:alginate ratio of 1:1 at a stirring rate of 1400 rpm with 2 ml of 1 % (w/v) sodium carboxymethyl cellulose (Na-CMC), whereas addition of EEP at a concentration of 100 mg/ml increased the mean particle size to 36.44 μm and yielded an encapsulation efficiency of 98.77 %. The cytotoxicities of EEP loaded microparticles were also assessed both on MCF-7 and MDA-MB-231 where similar results were achieved as free EEP which can enhance the possible use of propolis extract in the industry as a natural supplement.

  13. Novel molecular, cytotoxical, and immunological study on promising and selective anticancer activity of Mung bean sprouts

    Directory of Open Access Journals (Sweden)

    Hafidh Rand R

    2012-11-01

    Full Text Available Abstract Background The anticancer and immunomodulatory activity of mung bean sprouts (MBS and the underlying mechanisms against human cervical and hepatocarcinoma cancer cells were explored. Methods MBS cytotoxicity and MBS-induced anticancer cytokines, TNF-α and IFN-β from cancer cells, and immunological cytokines, IL-4, IFN-γ, and IL-10 from peripheral mononuclear cells (PMNC were assessed by MTS and ELISA assays. Apoptotic cells were investigated by flow cytometry. The expression level of apoptotic genes (Bax, BCL-2, Capsases 7–9 and cell cycle regulatory genes (cyclin D, E, and A and tumor suppressor proteins (p27, p21, and p53 was assessed by real-time qPCR in the cancer cells treated with extract IC50. Results The cytotoxicity on normal human cells was significantly different from HeLa and HepG2 cells, 163.97 ± 5.73, 13.3 ± 0.89, and 14.04 ± 1.5 mg/ml, respectively. The selectivity index (SI was 12.44 ± 0.83 for HeLa and 11.94 ± 1.2 for HepG2 cells. Increased levels of TNF-α and IFN-β were observed in the treated HeLa and HepG2 culture supernatants when compared with untreated cells. MBS extract was shown to be an immunopolarizing agent by inducing IFNγ and inhibiting IL-4 production by PBMC; this leads to triggering of CMI and cellular cytotoxicity. The extract induced apoptosis, in a dose and time dependent manner, in treated HeLa and HepG2, but not in untreated, cells (P Conclusion MBS extract was shown to be a potent anticancer agent granting new prospects of anticancer therapy using natural products.

  14. Gene cloning, characterization, and cytotoxic activity of methionine γ-lyase from Clostridium novyi.

    Science.gov (United States)

    Kulikova, Vitalia V; Morozova, Elena A; Revtovich, Svetlana V; Kotlov, Mikhail I; Anufrieva, Natalya V; Bazhulina, Natalya P; Raboni, Samanta; Faggiano, Serena; Gabellieri, Edi; Cioni, Patrizia; Belyi, Yury F; Mozzarelli, Andrea; Demidkina, Tatyana V

    2017-09-01

    The exploitation of methionine-depleting enzyme methionine γ-lyase (MGL) is a promising strategy against specific cancer cells that are strongly dependent on methionine. To identify MGL from different sources with high catalytic activity and efficient anticancer action, we have expressed and characterized MGL from Clostridium novyi and compared its catalytic efficiency with the previously studied MGL from Citrobacter freundii. The purified recombinant MGL exhibits kcat and kcat /Km for methionine γ-elimination reaction that are 2.4- and 1.36-fold higher than C. freundii enzyme, respectively, whereas absorption, fluorescence, and circular dichroism spectra are very similar, as expected on the basis of 87% sequence identity and high conservation of active site residues. The reactivity of cysteine residues with DTNB and iodoacetamide was investigated as well as the impact of their chemical modification on catalytic activity. This information is relevant because for increasing bioavailability and reducing immunogenity, MGL should be decorated with polyethylene glycol (PEG). It was found that Cys118 is a faster reacting residue, which results in a significant decrease in the γ-elimination activity. Thus, the protection of Cys118 before conjugation with cysteine-reacting PEG represents a valuable strategy to preserve MGL activity. The anticancer action of C. novyi MGL, evaluated in vitro against prostate (PC-3), chronic myelogenous leucemia (K562), and breast (MDA-MB-231 and MCF7) cancer cells, exhibits IC50 of 1.3 U mL-1 , 4.4 U mL-1 , 1.2 U mL-1 , and 3.4 U mL-1 , respectively. A higher cytotoxicity of C. novyi MGL was found against cancer cells with respect to C. freundii MGL, with the exception of PC-3, where a lower cytotoxicity was observed. © 2017 IUBMB Life, 69(9):668-676, 2017. © 2017 International Union of Biochemistry and Molecular Biology.

  15. Anti-Mycobacterium tuberculosis activity and cytotoxicity of Calophyllum brasiliense Cambess (Clusiaceae

    Directory of Open Access Journals (Sweden)

    Claudia Terencio Agostinho Pires

    2014-06-01

    Full Text Available We evaluated the in vitro anti-Mycobacterium tuberculosis activity and the cytotoxicity of dichloromethane extract and pure compounds from the leaves of Calophyllum brasiliense. Purification of the dichloromethane extract yielded the pure compounds (- mammea A/BB (1, (- mammea B/BB (2 and amentoflavone (3. The compound structures were elucidated on the basis of spectroscopic and spectrometric data. The contents of bioactive compounds in the extracts were quantified using high performance liquid chromatography coupled to an ultraviolet detector. The anti-M. tuberculosis activity of the extracts and the pure compounds was evaluated using a resazurin microtitre assay plate. The cytotoxicity assay was performed in J774G.8 macrophages using the 3-(4,5-dimethyl thiazol-2-yl-2,5-diphenyl tetrazolium bromide colourimetric method. The quantification of the dichloromethane extract showed (1 and (2 at concentrations of 31.86 ± 2.6 and 8.24 ± 1.1 µg/mg of extract, respectively. The dichloromethane and aqueous extracts showed anti-M. tuberculosis H37Rv activity of 62.5 and 125 µg/mL, respectively. Coumarins (1 and (2 showed minimal inhibitory concentration ranges of 31.2 and 62.5 µg/mL against M. tuberculosis H37Rv and clinical isolates. Compound (3 showed no activity against M. tuberculosis H37Rv. The selectivity index ranged from 0.59-1.06. We report the activity of the extracts and coumarins from the leaves of C. brasiliense against M. tuberculosis.

  16. Silver nanoparticles with antimicrobial activities against Streptococcus mutans and their cytotoxic effect

    Energy Technology Data Exchange (ETDEWEB)

    Pérez-Díaz, Mario Alberto [Facultad de Ciencias Químicas, UASLP, Álvaro Obregón 64, San Luis Potosí (Mexico); Boegli, Laura; James, Garth [Center for Biofilm Engineering, Montana State University, Bozeman, MT (United States); Velasquillo, Cristina; Sánchez-Sánchez, Roberto [Laboratorio de Biotecnología, Instituto Nacional de Rehabilitación (Mexico); Martínez-Martínez, Rita-Elizabeth; Martínez-Castañón, Gabriel Alejandro [Facultad de Estomatología, Universidad Autónoma de San Luis Potosí (Mexico); Martinez-Gutierrez, Fidel, E-mail: fidel@uaslp.mx [Facultad de Ciencias Químicas, UASLP, Álvaro Obregón 64, San Luis Potosí (Mexico)

    2015-10-01

    Microbial resistance represents a challenge for the scientific community to develop new bioactive compounds. The goal of this research was to evaluate the antimicrobial activity of silver nanoparticles (AgNPs) against a clinical isolate of Streptococcus mutans, antibiofilm activity against mature S. mutans biofilms and the compatibility with human fibroblasts. The antimicrobial activity of AgNPs against the planktonic clinical isolate was size and concentration dependent, with smaller AgNPs having a lower minimum inhibitory concentration. A reduction of 2.3 log in the number of colony-forming units of S. mutans was observed when biofilms grown in a CDC reactor were exposed to 100 ppm of AgNPs of 9.5 ± 1.1 nm. However, AgNPs at high concentrations (> 10 ppm) showed a cytotoxic effect upon human dermal fibroblasts. AgNPs effectively inhibited the growth of a planktonic S. mutans clinical isolate and killed established S. mutans biofilms, which suggests that AgNPs could be used for prevention and treatment of dental caries. Further research and development are necessary to translate this technology into therapeutic and preventive strategies. - Highlights: • Biological activities of silver nanoparticles for dental caries purposes • Antimicrobial activity of AgNPs on planktonic cell was size and concentration dependent. • Reduction in the S. mutans biofilm formation was statistically significant. • AgNPs at high concentrations showed a cytotoxic effect upon human dermal fibroblasts. • AgNPs could be used for prevention and treatment of dental caries.

  17. Essential oils: in vitro activity against Leishmania amazonensis, cytotoxicity and chemical composition.

    Science.gov (United States)

    Andrade, Milene Aparecida; Azevedo, Clênia Dos Santos; Motta, Flávia Nader; Santos, Maria Lucília Dos; Silva, Camila Lasse; Santana, Jaime Martins de; Bastos, Izabela M D

    2016-11-08

    The current chemotherapy for cutaneous leishmaniosis (CL) has a series of drug limitations such as toxic side effects, long duration, high costs and drug resistance, which requires the development of new drugs or effective alternatives to the CL treatment. Essential oils (EOs) are complex mixtures of secondary metabolites from various plants. It has been shown that several EOs, or their constituents, have inhibitory activity against protozoa. Thus, this study aims to evaluate the biological activity of different essential oils (EOs) on Leishmania (L.) amazonensis promastigotes forms, as well as their cytotoxicity on mammalian cells and chemical composition. Sixteen EOs were evaluated by mean of IC 50 /24 h and cytotoxicity against L6 cells (CC 50 /24 h) using Resazurin assay. Only those EOs that presented better results for IC 50 /24 h were submitted to GC-MS analysis to determine their chemical constitution. The EO from Cinnamodendron dinisii, Matricaria chamomilla, Myroxylon peruiferum, Salvia sclarea, Bulnesia sarmientoi, Ferula galbaniflua, Siparuna guianensis and Melissa officinalis were the most active against L. amazonensis with IC50/24 h ranging from 54.05 to 162.25 μg/mL. Analysis of EOs by GC-MS showed mainly the presence of β-farnesene (52.73 %) and bisabolol oxide (12.09 %) for M. chamomilla; α-copaene (13.41 %), safrole (8.35 %) and δ-cadinene (7.08 %) for M. peruiferum; linalool (28.80 %) and linalyl acetate (60.08 %) for S. sclarea; guaiol (48.29 %) and 2-undecanone (19.49 %) for B. sarmientoi; ethyl phthalate (13.09 %) and methyl-8-pimaren-18-oate (41.82 %) for F. galbaniflua; and neral (37.18 %) and citral (5.02 %) for M. officinalis. The EO from F. galbaniflua showed to be effective against L. amazonensis promastigotes forms and presented low cytotoxic activity against L6 cells. Thus, it represents a strong candidate for future studies aiming its molecular activity on these pathogenic parasites.

  18. Assessment of phytochemicals, antimicrobial and cytotoxic activities of extract and fractions from Fagonia olivieri (Zygophyllaceae).

    Science.gov (United States)

    Rashid, Umbreen; Khan, Muhammad Rashid; Jan, Shumaila; Bokhari, Jasia; Shah, Naseer Ali

    2013-07-10

    In Pakistan Fagonia olivieri (Zygophyllaceae) is commonly used in the indigenous system of medicine for treatment of conditions like diabetes, cancer, fever, asthma, toothache, stomach troubles and kidney disorders. This study evaluated the crude methanol extract of F. olivieri (FOM) and its derived fractions for their antimicrobial and cytotoxic activities as well as the classes of phytochemical. Dried powder of whole plant of F. olivieri was extracted with methanol (FOM) and the resultant was fractionated to give n-hexane fraction (FOH), chloroform fraction (FOC), ethyl acetate fraction (FOE), n-butanol fraction (FOB) and residual aqueous fraction (FOA). Methanol extract and its derived fractions were subjected to phytochemical screening using standard procedures. Also the extract and fractions were assayed for antibacterial, antifungal and cytotoxic activities using agar well diffusion technique, agar tube dilution method and brine shrimps lethality test, respectively. The results obtained for phytochemical analysis indicate the presence of saponins and alkaloids in all the tested extract and fractions while anthraquinones were not detected. The results showed that all the bacterial strains tested in this study were susceptible to at least one of the fractions tested. However, FOE and FOB were the best antibacterial fractions and showed antibacterial activity against maximum number of bacterial strains. The results showed that Escherichia coli was the most sensitive bacterium while Bordetella bronchiseptica and Enterobacter aerogenes were less susceptible against various fractions. Maximum percent inhibition for growth was recorded for the fungus Aspergillus flavus with FOE whereas growth of Aspergillus fumigatus and Fusarium solani was inhibited by FOM and its all derived fractions. Minimum LC50 (24.07 mg/L) for brine shrimp assay was recorded for FOE followed by LC50 of FOC (26.1 mg/L) and FOB (30.05 mg/L) whereas maximum LC50 was exhibited by FOH (1533 mg

  19. Distribution of cytotoxic and DNA ADP-ribosylating activity in crude extracts from butterflies among the family Pieridae

    Science.gov (United States)

    Matsumoto, Yasuko; Nakano, Tsuyoshi; Yamamoto, Masafumi; Matsushima-Hibiya, Yuko; Odagiri, Ken-Ichi; Yata, Osamu; Koyama, Kotaro; Sugimura, Takashi; Wakabayashi, Keiji

    2008-01-01

    Cabbage butterflies, Pieris rapae and Pieris brassicae, contain strong cytotoxic proteins, designated as pierisin-1 and -2, against cancer cell lines. These proteins exhibit DNA ADP-ribosylating activity. To determine the distribution of substances with cytotoxicity and DNA ADP-ribosylating activity among other species, crude extracts from 20 species of the family Pieridae were examined for cytotoxicity in HeLa cells and DNA ADP-ribosylating activity. Both activities were detected in extracts from 13 species: subtribes Pierina (Pieris rapae, Pieris canidia, Pieris napi, Pieris melete, Pieris brassicae, Pontia daplidice, and Talbotia naganum), Aporiina (Aporia gigantea, Aporia crataegi, Aporia hippia, and Delias pasithoe), and Appiadina (Appias nero and Appias paulina). All of these extracts contained substances recognized by anti-pierisin-1 antibodies, with a molecular mass of ≈100 kDa established earlier for pierisin-1. Moreover, sequences containing NAD-binding sites, conserved in ADP-ribosyltransferases, were amplified from genomic DNA from 13 species of butterflies with cytotoxicity and DNA ADP-ribosylating activity by PCR. Extracts from seven species, Appias lyncida, Leptosia nina, Anthocharis scolymus, Eurema hecabe, Catopsilia pomona, Catopsilia scylla, and Colias erate, showed neither cytotoxicity nor DNA ADP-ribosylating activity, and did not contain substances recognized by anti-pierisin-1 antibodies. Sequences containing NAD-binding sites were not amplified from genomic DNA from these seven species. Thus, pierisin-like proteins, showing cytotoxicity and DNA ADP-ribosylating activity, are suggested to be present in the extracts from butterflies not only among the subtribe Pierina, but also among the subtribes Aporiina and Appiadina. These findings offer insight to understanding the nature of DNA ADP-ribosylating activity in the butterfly. PMID:18256183

  20. Antioxidant activity, cytotoxic activity and metabolic profiling of juices obtained from saffron (Crocus sativus L.) floral by-products.

    Science.gov (United States)

    Tuberoso, Carlo I G; Rosa, Antonella; Montoro, Paola; Fenu, Maurizio Antonio; Pizza, Cosimo

    2016-05-15

    Juices obtained from cold-pressed saffron (Crocus sativus L.) floral by-products were evaluated as a potential source of compounds with antioxidant and cytotoxic activities. Floral by-products were split in two batches for extraction 24 and 48h after flower harvesting, respectively. The in vitro anti-oxidant activity of these extracts was tested using the FRAP and DPPH assays, and two biological models of lipid oxidation (activity in preventing cholesterol degradation and protection against Cu(2+)-mediated degradation of the liposomal unsaturated fatty acids). The cytotoxic activity was evaluated using the MTT assay. The results show that extracts obtained 48h post-harvest contained higher levels of total polar phenols and had the highest antioxidant activity in all of the performed assays. The LC-DAD and LC-ESI-(HR)MS(n) metabolic profiles showed high levels of kaempferol derivatives and anthocyanins. This study suggests that juices from saffron floral by-products could potentially be used to develop new products for the food and health industry. Copyright © 2015 Elsevier Ltd. All rights reserved.

  1. Cytotoxicity and aryl hydrocarbon receptor-mediated activity of n-heterocyclic polycyclic aromatic hydrocarbons: structure-activity relationships.

    Science.gov (United States)

    Sovadinová, Iva; Bláha, Ludĕk; Janosek, Jaroslav; Hilscherová, Klára; Giesy, John P; Jones, Paul D; Holoubek, Ivan

    2006-05-01

    Toxic effects of many persistent organic pollutants (e.g., polychlorinated biphenyls or polychlorinated dibenzo-p-dioxins and furans) are mediated via the aryl hydrocarbon receptor (AhR). Although polycyclic aromatic hydrocarbons (PAHs) and their derivatives also activate AhR, their toxic effects remain to be fully elucidated. In the present study, we used the in vitro H4IIE-luc transactivation cell assay to investigate cytotoxicity and potencies to activate AhR by 29 individual PAHs and their N-heterocyclic derivatives (aza-PAHs). The aza-PAHs were found to be significantly more cytotoxic and more potent inducers of AhR than their unsubstituted analogues. Several aza-PAHs, such as dibenz[a,h]acridine or dibenz[a,i]acridine, activated AhR within picomolar concentrations, comparable to the effects of reference 2,3,7,8-tetrachlorodibenzo-p-dioxin. Ellipsoidal volume, molar refractivity, and molecular size were the most important descriptors derived from the modeling of quantitative structure-activity relationships for potencies to activate AhR. Comparable relative toxic potencies (induction equivalency factors) for individual aza-PAHs are derived, and their use for evaluation of complex contaminated samples is discussed.

  2. Cytotoxic activity screening of some medicinal plants from south of Iran

    Directory of Open Access Journals (Sweden)

    S. Esmaeili

    2014-10-01

    Full Text Available Background and objectives: Cancer is a public health problem all over the world. Herbal medicines have a vital role in the prevention and treatment of cancer and large numbers of plants and their isolated constituents have shown potential anticancer activity. Methods: Twenty seven medicinal plants from southern Iran provinces have been extracted with methanol and screened for their cytotoxic activity against MCF-7, WEHI-164, HepG-2, MDBK and A-549 cell lines by MTT assay. Results: The methanol extracts of two species, Calotropis procera andJuniperus excelsa, demonstrated to be more effective compared to other extracts. Conclusion: The above species are proper candidates for further cancer studies.  

  3. Cytotoxic and Hypoglycemic Activity of Triterpenoid Saponins from Camellia oleifera Abel. Seed Pomace.

    Science.gov (United States)

    Di, Tai-Mei; Yang, Shao-Lan; Du, Feng-Yu; Zhao, Lei; Xia, Tao; Zhang, Xin-Fu

    2017-09-21

    One new and three known triterpenoid saponins were isolated and identified from Camellia oleifera seeds through IR, NMR, HR-ESI-MS and GC-MS spectroscopic methods, namely oleiferasaponin A₃, oleiferasaponin A₁, camelliasaponin B₁, and camelliasaponin B₂. The structure of oleiferasaponin A₃ was elucidated as 16α-hydroxy-21β- O -angeloyl-22α- O -cinnamoyl-23α-aldehyde-28-dihydroxymethylene-olean-12-ene-3β- O -[β-d-galactopyranosyl-(1→2)]-[β-d-xylopyranosyl-(1→2)-β-d-galactopyranosyl-(1→3)]-β-d-gluco-pyranosiduronic acid. Camelliasaponin B₁ and camelliasaponin B₂ exhibited potent cytotoxic activity on three human tumour cell lines (human lung tumour cells (A549), human liver tumour cells (HepG2), cervical tumour cells (Hela)). The hypoglycemic activity of oleiferasaponin A₁ was testified by protecting pancreatic β-cell lines from high-glucose damage.

  4. Chemical composition, antioxidant and cytotoxicity activities of the essential oils of Myristica fragrans and Morinda citrifolia.

    Science.gov (United States)

    Piaru, Suthagar Pillai; Mahmud, Roziahanim; Abdul Majid, Amin Malik Shah; Ismail, Sabariah; Man, Che Nin

    2012-02-01

    In this study the chemical composition, antioxidant activities and cytotoxic effect of the essential oils of Myristica fragrans (nutmeg) and Morinda citrifolia (mengkudu) were determined. Thirty-eight compounds in nutmeg oil and six compounds in mengkudu oil were identified by gas chromatography–mass spectrometry. The free radical scavenging activity of nutmeg oil was superior of that mengkudu oil. The MTT assay of nutmeg oil on human colorectal carcinoma (HCT-116) and human breast carcinoma (MCF-7) cell lines showed IC₅₀ values of 78.61 and 66.45 µg mL⁻¹, respectively. The mengkudu oil exhibited IC₅₀ values of 91.46 and 78.15 µg mL⁻¹ for HCT-116 and MCF-7, respectively. The results showed that nutmeg oil can be developed as potent anti-cancer and antioxidant drugs. Copyright © 2011 Society of Chemical Industry.

  5. Naphthoquinones from the leaves of Rhinacanthus nasutus having acetylcholinesterase inhibitory and cytotoxic activities.

    Science.gov (United States)

    Boonyaketgoson, Sirada; Rukachaisirikul, Vatcharin; Phongpaichit, Souwalak; Trisuwan, Kongkiat

    2018-01-01

    Four new naphthoquinones (1-4), named rhinacanthins S (1), T (2), U (3) and V (4), together with 13 known naphthoquinones were isolated from the leaf extract of Rhinacanthus nasutus. The structures of isolated compounds were elucidated by spectroscopic methods, especially 1D and 2D NMR spectroscopy and mass spectrometry. Rhinacanthin S (1) exhibited acetylcholinesterase inhibition activity with a % inhibition value of 48.04±3.25. The known rhinacanthin A (5) showed cytotoxicity against a MCF-7 cell line with an IC 50 value of 8.79μM, while rhinacanthin N (15) was active against the NCI-H187 cell line with an IC 50 =2.24μM and Vero cells (IC 50 =3.00μM). Copyright © 2017 Elsevier B.V. All rights reserved.

  6. Unsaturated fatty acids lactose esters: cytotoxicity, permeability enhancement and antimicrobial activity.

    Science.gov (United States)

    Lucarini, Simone; Fagioli, Laura; Campana, Raffaella; Cole, Hannah; Duranti, Andrea; Baffone, Wally; Vllasaliu, Driton; Casettari, Luca

    2016-10-01

    Sugar based surfactants conjugated with fatty acid chains are an emerging broad group of highly biocompatible and biodegradable compounds with established and potential future applications in the pharmaceutical, cosmetic and food industries. In this work, we investigated absorption enhancing and antimicrobial properties of disaccharide lactose, monoesterified with unsaturated fatty acids through an enzymatic synthetic approach. After chemical and cytotoxicity characterizations, their permeability enhancing activity was demonstrated using intestinal Caco-2 monolayers through transepithelial electrical resistance (TEER) and permeability studies. The synthesized compounds, namely lactose palmitoleate (URB1076) and lactose nervonate (URB1077), were shown to exhibit antimicrobial activity versus eight pathogenic species belonging to Gram-positive, Gram-negative microorganisms and fungi. Copyright © 2016 Elsevier B.V. All rights reserved.

  7. Cytotoxicity of cis-platinum(II) conjugate models. The effect of chelating arms and leaving groups on cytotoxicity: a quantitative structure-activity relationship approach.

    Science.gov (United States)

    Monti, Elena; Gariboldi, Marzia; Maiocchi, Alessandro; Marengo, Emilio; Cassino, Claudio; Gabano, Elisabetta; Osella, Domenico

    2005-02-10

    Thirteen newly synthesized or resynthesized diamine-platinum(II) complexes were characterized, and their cytotoxic activities (IC50) were tested on parental and resistant ovarian cancer cell lines. They represent models of conjugates between biologically active vectors and cytotoxic Pt(II) moieties within the "drug targeting and delivery strategy". Three drugs, routinely employed in the clinical treatment of cancer, namely, cisplatin, carboplatin, and oxaliplatin, were also included in the study as controls. The quantitative structure-activity relationship approach provides simple regression models able to predict log(1/IC50) of diamine-platinum(II) complexes on both parental and resistant ovarian cancer cell lines. The 16 complexes were characterized using 197 molecular descriptors, after which the best regression models relating a subset of these descriptors to the log(1/IC50) in the two cancer cell lines were calculated. Models with four variables proved to be endowed with very good predictive ability Q2(LMO-50%) > or = 85.6%, making it possible to discard 50% of the molecules from the test set following for cross-validation procedure. A four-variable regression model also proved effective in predicting the resistance index RI, Q2(LMO-50%) = 84.4%.

  8. Evaluation of cytotoxic, apoptotic, mutagenic, and chemopreventive activities of semi-synthetic esters of gallic acid.

    Science.gov (United States)

    Silva, I C; Polaquini, C R; Regasini, L O; Ferreira, H; Pavan, F R

    2017-07-01

    Gallic acid and its derivatives are phenolic compounds widely used as food supplements in the form of capsules, liquid extracts, and ointments owing to their good antioxidant properties. Besides, these compounds are potent inhibitors of fungi, bacteria, and some viruses and possess strong antiproliferative and chemopreventive activities. However, gallic acid derivatives are also known to exert harmful effects like mutagenicity and cytotoxicity. The present study aimed to understand and explore the toxicological risks of these compounds. For this, a series of alkyl gallates with side chains varying from five to eight carbons (pentyl, hexyl, heptyl, and octyl gallates) were evaluated for their cytotoxic and pro-apoptotic potential. In addition, the genotoxic effects of alkyl gallates were measured in HepG2 cells using the single cell gel electrophoresis (SCGE)/comet assay and the cytokinesis-blocked micronucleus (CBMN) test. In both the tests, the substances did not induce any significant differences when compared to the control group. In addition, alkyl gallates exhibited a chemopreventive effect, thereby considerably reducing the mutagenicity caused by H2O2. In conclusion, our results suggest that alkyl gallates are non-genotoxic, non-mutagenic, and pro-apoptotic agents, which may serve as suitable and promising candidates for preventing chemically-induced chromosomal damage. Copyright © 2017 Elsevier Ltd. All rights reserved.

  9. Nanoencapsulation of gallic acid and evaluation of its cytotoxicity and antioxidant activity.

    Science.gov (United States)

    de Cristo Soares Alves, Aline; Mainardes, Rubiana Mara; Khalil, Najeh Maissar

    2016-03-01

    Gallic acid is an important polyphenol compound presenting various biological activities. The objective of this study was to prepare, characterize and evaluate poly(lactic-co-glycolic acid) (PLGA) nanoparticles coated or not with polysorbate 80 (PS80) containing gallic acid. Nanoparticles coated or not with PS80 were produced by emulsion solvent evaporation method and presented a mean size of around 225 nm, gallic acid encapsulation efficiency of around 26% and zeta potential of -22 mV. Nanoparticle formulations were stable during storage, except nanoparticles coated with PS80 stored at room temperature. In vitro release profile demonstrated a quite sustained gallic acid release from nanoparticles and PS80-coating decreased drug release. Cytotoxicity over red blood cells was assessed and gallic acid-loaded PLGA nanoparticles at all analyzed concentrations demonstrated lack of hemolysis, while PS80-nanoparticles containing gallic acid were cytotoxic only in higher concentrations. Antioxidant potential of nanoparticles containing gallic acid was assessed and PLGA uncoated nanoparticles presented greater efficacy than PS80-coated PLGA nanoparticles. Copyright © 2015 Elsevier B.V. All rights reserved.

  10. Antimalarial and cytotoxic activities of roots and fruits fractions of Astrodaucus persicus extract

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    Saied Goodarzi

    2017-12-01

    Full Text Available Objective(s:Astrodaucus persicus (Apiaceae is one of the two species of this genus which grows in different parts of Iran. Roots of this plant were rich in benzodioxoles and used as food additive or salad in Iran and near countries. The aim of present study was evaluation of antimalarial and cytotoxic effects of different fractions of A. persicus fruits and roots extracts. Materials and Methods: Ripe fruits and roots of A. persicuswere extracted and fractionated by hexane, chloroform, ethyl acetate and methanol, separately. Antimalarial activities of fractions were performed based on Plasmodium berghei suppressive test in mice model and percentage of parasitemia and suppression were determined for each sample. Cytotoxicity of fruits and roots fractions were investigated against human breast adenocarcinoma (MCF-7, colorectal carcinoma (SW480 and normal (L929 cell lines by MTT assay and IC50 of them were measured. Results: Hexane fraction of roots extract (RHE and ethyl acetate fraction of fruits extract (FEA of A. persicus demonstrated highest parasite inhibition (73.3 and 72.3%, respectively at 500 mg/kg/day which were significantly different from negative control group (P

  11. Cytotoxicity, Bactericidal, and Antioxidant Activity of Sodium Alginate Hydrosols Treated with Direct Electric Current

    Directory of Open Access Journals (Sweden)

    Żaneta Król

    2017-03-01

    Full Text Available The aim of the study was to investigate the effect of using direct electric current (DC of 0, 200, and 400 mA for five minutes on the physiochemical properties, cytotoxicity, antibacterial, and antioxidant activity of sodium alginate hydrosols with different sodium chloride concentrations. The pH, oxidation-reduction potential (ORP, electrical conductivity (EC, and available chlorine concentration (ACC were measured. The effect of sodium alginate hydrosols treated with DC on Staphylococcus aureus, Listeria monocytogenes, Bacillus cereus, Micrococcus luteus, Escherichia coli, Salmonella enteritidis, Yersinia enterocolitica, Pseudomonas fluorescence, and RAW 264.7 and L929 cells was investigated. Subsequently, the antioxidant properties of hydrosols were evaluated by determining the scavenging ability of 1,1-diphenyl-2-picrylhydrazyl free radical (DPPH and ferric reducing antioxidant power (FRAP. The results have shown that after applying 400 mA in hydrosol samples with 0.1% and 0.2% NaCl all tested bacteria were inactivated. The ACC concentration of C400 samples with NaCl was equal to 13.95 and 19.71 mg/L, respectively. The cytotoxicity analysis revealed that optimized electric field conditions and the addition of sodium chloride allow for the avoidance of toxicity effects on normal cells without disturbing the antibacterial effects. Due to the presence of oxidizing substances, the DPPH of variants treated with DC was lower than the DPPH of control samples.

  12. Dendritic cell subsets require cis-activation for cytotoxic CD8 T cell induction

    Science.gov (United States)

    Desch, A. Nicole; Gibbings, Sophie L.; Clambey, Eric T.; Janssen, William J.; Slansky, Jill E.; Kedl, Ross M.; Henson, Peter M.; Jakubzick, Claudia

    2014-01-01

    Dendritic cells (DCs) are required for the induction of cytotoxic T cells (CTL). In most tissues, including the lung, the resident DCs fall into two types, respectively expressing the integrin markers, CD103 and CD11b. The current supposition is that DC function is predetermined by lineage, designating the CD103+ DC as the major cross-presenting DC able to induce CTL. Here we show that Poly I:C (TLR3 agonist) or R848 (TLR7 agonist) do not activate all endogenous DCs. CD11b+ DCs can orchestrate a CTL response in vivo in the presence of TLR7 agonist but not TLR3 agonist, whereas CD103+ DCsrequire ligation of TLR3 for this purpose. This selectivity does not extend to antigen cross-presentation for T cell proliferation but is required for induction of cytotoxicity. Thus, we demonstrate that the ability of DCsto induce functional CTLs isspecific to the nature of the pathogen associated molecular pattern (PAMP) encountered by endogenous DC. PMID:25135627

  13. Isolation and Identification of Cytotoxic and Biological Active Toxin from the Puffer Fish Arothron stellatus.

    Science.gov (United States)

    Veeruraj, Anguchamy; Pugazhvendan, Sampath Renuga; Ajithkumar, Thipramalai Thankappan; Arumugam, Muthuvel

    2016-07-01

    This study is to investigate the biological, biochemical and cytotoxic effects of puffer fish (Arothron stellatus) toxin extracts under in-vitro condition. Extracted toxins from various organs of puffer fish were purified by using active charcoal column, and Bio-gel-P2 column chromatography. The lethality of toxin was tested in crabs, which consists of neurotoxic compounds. The degree of the brine shrimp lethality assay was found directly proportional to the concentration of the toxin extracts, which was well supported by hemolytic assay. The experimental results suggested that the gonad was found higher toxins than the liver and muscles. The mortality rate of brine shrimp nauplii was increased with the raise of concentrations of toxin level. Among the different doses and time dependent cytotoxic effect of human cervical carcinoma (HeLa) cells were showed 4.0 μg/mL of toxin, which was effectively inhibited cancer cell proliferation. HPLC and TLC analysis was revealed that the A. stellatus toxin contains tetrodotoxin (TTX), related compounds 4-epi TTX and anhydro-TTX. The present results suggested that the A. stellatus contain TTX as a major and anh-TTX as a minor toxin. It could be the potential candidate in the field of anticancer drug discovery against human cervical cancer cells. The present data is confirming that the puffer fish toxin as an interesting source of novel bioactive natural compounds with potent applications in pharmacology.

  14. Antimicrobial activity, cytotoxicity, and phytochemical screening of Voacanga globosa (Blanco) Merr. leaf extract (Apocynaceae).

    Science.gov (United States)

    Vital, Pierangeli G; Rivera, Windell L

    2011-10-01

    To determine the antibacterial, antifungal, antiprotozoal, cytotoxic, and phytochemical properties of ethanol extracts of leaves of Voacanga globosa (Blanco) Merr. (V. globosa). The extracts were tested against bacteria and fungus through disc diffusion assay; against protozoa through growth curve determination, antiprotozoal and cytotoxicity assays. The extract revealed antibacterial activities, inhibiting the growth of Staphylococcus aureus, Bacillus cereus, Pseudomonas aeruginosa, Micrococcus luteus, and Salmonella typhimurium. Antifungal assay showed that it inhibited Candida albicans. The antiprotozoal assay against Trichomonas vaginalis and Entamoeba histolytica showed that V. globosa can inhibit the parasites, wherein the action can be comparable to metronidazole. With the in situ cell death detection kit, Trichomonas vaginalis and Entamoeba histolytica exposed to V. globosa leaf extract was observed to fluoresce simultaneously in red and yellow signals signifying apoptotic-like changes. Preliminary phytochemical screening revealed the chemical composition of plant extract containing alkaloids, saponins, 2-deoxysugars, and hydrolysable tannins. Thus, this study provides scientific evidence on the traditional use of V. globosa leaf extract in treating microbial diseases. Further, the leaf extract can possibly be used to produce alternative forms of antimicrobials. Copyright © 2011 Hainan Medical College. Published by Elsevier B.V. All rights reserved.

  15. Composition and Cytotoxic Activity of Essential Oils fromCroton matourensis and Croton micans from Venezuela

    Directory of Open Access Journals (Sweden)

    Reinaldo S. Compagnone

    2010-04-01

    Full Text Available The chemical composition and cytotoxic activity of the essential oils extracted from leaves of Croton matourensis and flowers and leaves of Croton micans were investigated. GC-FID and GC-MS analysis revealed that forty six compounds comprised 95.5 % of C. matourensis essential oil, with the main components being fenchyl acetate (19.5%, methyleugenol (14.2%, isoelemicine (11.3%, elemicine (7.6%, spathulenol (6.9% and valencene (5.8%. In the analysis of C. micans oils, 63 compounds that comprised 98.9% were identified from the flower oil, the principal being fenchyl acetate (41.6%, α-caryophyllene (12.6%, β-cubebene (5.0%, β-caryophyllene (5.5%, α-cubebene (5.3%, β-elemene (4.7% and valencene (4.6%. The oil from leaves gave fenchyl acetate (25.3% α-caryophyllene (20.7%, α-selinene (12.8% and β-bourbene (9.3% as major constituents. The cytoxicity of these oils was screened by the MTT method against three human tumour cell lines and primary culture of human dermis fibroblasts (normal control cells. The results indicate that the oils have a moderate cytotoxicity against LoVo (colon carcinoma, X-17 (colon carcinoma, HeLa (cervical cancer, and control cells.

  16. Cytotoxic Activity of Laserpitium latifolium L. Extract and Its Daucane and Phenylpropanoid Constituents

    Directory of Open Access Journals (Sweden)

    Višnja Popović

    2013-05-01

    Full Text Available In the search for novel cytotoxic agents, sesquiterpenoids and phenylpropanoids have provided interesting lead compounds. From the chloroform extract of the underground parts of Laserpitium latifolium , the daucane sesquiterpenoids laserpitin and acetyldesoxodehydrolaserpitin, and the phenylpropanoids laserin and latifolon were isolated as the major compounds. Acetyldesoxodehydrolaserpitin is identified for the first time in the genus Laserpitium. Using a MTT and a sulforhodamine B (SRB assay, the cytotoxic and antiproliferative activity of the extract and compounds laserpitin, acetyldesoxodehydrolaserpitin and laserin was tested in two closely related human breast adenocarcinoma cell lines, ie. the invasive MCF 7/6 and the non-invasive MCF 7/AZ. The IC 50 values of the extract were in the range of 184.72 – 397.16 μg/mL, with the most potent effect observed in the MTT test on the MCF 7/6 line. Among the tested compounds, acetyldesoxodehydrolaserpitin exerted a most potent, concentration-dependent effect (IC 50 values of 0.60 and 0.51 m M in the MCF 7/6 cell line, and 2.29 m M and 31.87 m M in the MCF 7/AZ cell line in the MTT and SRB test, respectively. The effect of laserin was more pronounced in the MTT test (IC 50 of 4.57 and 2.46 m M in the MCF 7/6 and MCF 7/AZ, respectively.

  17. Cytotoxic activity of marine sponge extracts from the sub-Antarctic Islands and the Southern Ocean

    Directory of Open Access Journals (Sweden)

    Elisabeth K. Olsen

    2016-11-01

    Full Text Available Over the past 50 years, marine invertebrates, especially sponges, have proven to be a valuable source of new and/or bioactive natural products that have the potential to be further developed as lead compounds for pharmaceutical applications. Although marine benthic invertebrate communities occurring off the coast of South Africa have been explored for their biomedicinal potential, the natural product investigation of marine sponges from the sub-Antarctic Islands in the Southern Ocean for the presence of bioactive secondary metabolites has been relatively unexplored thus far. We report here the results for the biological screening of both aqueous and organic extracts prepared from nine specimens of eight species of marine sponges, collected from around Marion Island and the Prince Edward Islands in the Southern Ocean, for their cytotoxic activity against three cancer cell lines. The results obtained through this multidisciplinary collaborative research effort by exclusively South African institutions has provided an exciting opportunity to discover cytotoxic compounds from sub-Antarctic sponges, whilst contributing to our understanding of the biodiversity and geographic distributions of these cold-water invertebrates. Therefore, we acknowledge here the various contributions of the diverse scientific disciplines that played a pivotal role in providing the necessary platform for the future natural products chemistry investigation of these marine sponges from the sub- Antarctic Islands and the Southern Ocean.

  18. In vitro cytotoxic activity of Cymbopogon citratus L. and Cymbopogon nardus L. essential oils from Togo

    Directory of Open Access Journals (Sweden)

    Koffi Koba

    2009-06-01

    Full Text Available The leaf essential oils of Cymbopogon citratus L. and Cymbopogon nardus L.(Poaceae from Togo were steam-distilled, analyzed for percentage composition and investigated in vitro for their potential cytotoxic activity on human epidermic cell line HaCat. The percentage composition showed that the main constituents of essential oils samples were respectively geranial (45.2%, neral(32.4% and myrcène (10.2% for C. citratus essential oil and citronellal (35.5%, geraniol (27.9% and citronellol (10.7% for that of C. nardus. The in vitro cytotoxicity bioassays on human epidermic cell line HaCaT revealed that the toxicityof the essential oil from C. citratus (IC50: 150 μL.mL-1 was higher than that of the essential oil from C. nardus (IC50: 450 μL.mL-1. Pure commercial neral, geranial, and citronellal standards showed respectively the following IC50 values: 100, 250 and 300 μL.mL-1. Conversely, pure citronellol standard appeared almost non-toxic (IC50>1000 μL.mL-1, proving the major role played in synergyby neral and geranial in the overall toxicity showed by the citratus oil sample tested in this work.

  19. Aporphine and tetrahydroprotoberberine alkaloids from the leaves of Guatteria friesiana (Annonaceae) and their cytotoxic activities

    Energy Technology Data Exchange (ETDEWEB)

    Costa, Emmanoel Vilaca; Cruz, Pedro Ernesto O. da, E-mail: emmanoelvc@gmail.com [Universidade Federal de Sergipe (UFSE), Sao Cristovao, SE (Brazil). Departamento de Quimica; Marques, Francisco A.; Barison, Andersson; Maia, Beatriz Helena L.N.S. [Universidade Federal do Parana (UFPR), Curitiba, PR (Brazil). Centro Politecnico. Departamento de Quimica; Pinheiro, Maria Lucia B. [Universidade Federal do Amazonas (UFAM), Manaus, AM (Brazil). Departamento de Quimica; Ruiz, Ana Lucia T.G.; Marchetti, Gabriela M.; Carvalho, Joao Ernesto de [Universidade Estadual de Campinas (UNICAMP), SP (Brazil). Centro Pluridisciplinar de Pesquisas Quimicas, Biologicas e Agricolas. Divisao de Farmacologia e Toxicologia

    2013-05-15

    Phytochemical investigation of the leaves of Guatteria friesiana (Annonaceae) afforded three new isoquinoline alkaloids, 13-hydroxy-discretinine, 6,6a-dehydroguatteriopsiscine and 9-dehydroxy-1-methoxy-dihydroguattouregidine. Eight known alkaloids were also isolated, 13-hydroxy-2,3,9,10-tetramethoxyprotoberberine, guatteriopsiscine, lysicamine, liriodenine, atherospermidine, lanuginosine, 7,8-dihydro-8-hydroxypalmatine and palmatine. 13-Hydroxy- 2,3,9,10-tetramethoxyprotoberberine was only obtained by synthesis and is being reported as a natural product for the first time. The structures of the isolated alkaloids were established by extensive analysis of 1D and 2D nuclear magnetic resonance (NMR) and mass spectrometric (MS) data, as well as by comparison with data reported in the literature. The in vitro cytotoxic activity of the major alkaloids was evaluated against tumor and non-tumor cell lines. All of the alkaloids evaluated were determined to be inactive based on National Cancer Institute (NCI/USA) criteria. However, the alkaloid palmatine exhibited a cytostatic effect on MCF-7 (breast) and U251 (glioma) human tumor cell lines, with GI{sub 50} values lower than 20.0 Greek-Small-Letter-Mu mol L{sup -}1 (10.5and 16.2 Greek-Small-Letter-Mu molL{sup -1}, respectively), suggesting a selective cytotoxic action (author)

  20. Anthelmintic, Antibacterial and Cytotoxicity Activity of Imidazole Alkaloids from Pilocarpus microphyllus Leaves.

    Science.gov (United States)

    Rocha, Jefferson A; Andrade, Ivanilza M; Véras, Leiz M C; Quelemes, Patrick V; Lima, David F; Soares, Maria J S; Pinto, Pedro L S; Mayo, Simon J; Ivanova, Galya; Rangel, Maria; Correia, Manuela; Mafud, Ana Carolina; Mascarenhas, Yvonne P; Delerue-Matos, Cristina; de Moraes, Josué; Eaton, Peter; Leite, José R S A

    2017-04-01

    Pilocarpus microphyllus Stapf ex Wardlew (Rutaceae), popularly known as jaborandi, is a plant native to the northern and northeastern macroregions of Brazil. Several alkaloids from this species have been isolated. There are few reports of antibacterial and anthelmintic activities for these compounds. In this work, we report the antibacterial and anthelmintic activity of five alkaloids found in P. microphyllus leaves, namely, pilosine, epiisopilosine, isopilosine, epiisopiloturine and macaubine. Of these, only anthelmintic activity of one of the compounds has been previously reported. Nuclear magnetic resonance, HPLC and mass spectrometry were combined and used to identify and confirm the structure of the five compounds. As regards the anthelmintic activity, the alkaloids were studied using in vitro assays to evaluate survival time and damaged teguments for Schistosoma mansoni adult worms. We found epiisopilosine to have anthelmintic activity at very low concentrations (3.125 μg mL-1 ); at this concentration, it prevented mating, oviposition, reducing motor activity and altered the tegument of these worms. In contrast, none of the alkaloids showed antibacterial activity. Additionally, alkaloids displayed no cytotoxic effect on vero cells. The potent anthelmintic activity of epiisopilosine indicates the potential of this natural compound as an antiparasitic agent. Copyright © 2017 John Wiley & Sons, Ltd. Copyright © 2017 John Wiley & Sons, Ltd.

  1. Antimicrobial, Anti-Inflammatory, Antiparasitic, and Cytotoxic Activities of Laennecia confusa

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    María G. Martínez Ruiz

    2012-01-01

    Full Text Available The current paper investigated the potential benefit of the traditional Mexican medicinal plant Laennecia confusa (Cronquist G. L. Nesom (Asteraceae. Fractions from the hexane, chloroform, methanol, and aqueous extracts were analyzed for antibacterial, antifungal, anti-inflammatory, and antiparasitic activities. The antimicrobial activity of the extracts and fractions was assessed on bacterial and fungal strains, in addition to the protozoa Leishmania donovani, using a microdilution assay. The propensity of the plant's compounds to produce adverse effects on human health was also evaluated using propidium iodine to identify damage to human macrophages. The anti-inflammatory activity of the extracts and fractions was investigated by measuring the secretion of interleukin-6. Chemical analyses demonstrated the presence of flavonoids, cyanogenic and cardiotonic glycosides, saponins, sesquiterpene lactones, and triterpenes in the chloroform extract. A number of extracts and fractions show antibacterial activity. Of particular interest is antibacterial activity against Staphylococcus aureus and its relative methicillin-resistant strain, MRSA. Hexanic and chloroformic fractions also exhibit antifungal activity and two extracts and the fraction CE 2 antiparasitic activity against Leishmania donovani. All bioactive extracts and fractions assayed were also found to be cytotoxic to macrophages. In addition, the hexane and methane extracts show anti-inflammatory activity by suppressing the secretion of interleukine-6.

  2. Cytotoxic and melanogenesis-inhibitory activities of limonoids from the leaves of Azadirachta indica (Neem).

    Science.gov (United States)

    Takagi, Mio; Tachi, Yosuke; Zhang, Jie; Shinozaki, Takuro; Ishii, Kenta; Kikuchi, Takashi; Ukiya, Motohiko; Banno, Norihiro; Tokuda, Harukuni; Akihisa, Toshihiro

    2014-03-01

    Seventeen limonoids (tetranortriterpenoids), 1-17, including three new compounds, i.e., 17-defurano-17-(2,5-dihydro-2-oxofuran-3-yl)-28-deoxonimbolide (14), 17-defurano-17-(2ξ-2,5-dihydro-2-hydroxy-5-oxofuran-3-yl)-28-deoxonimbolide (15), and 17-defurano-17-(5ξ-2,5-dihydro-5-hydroxy-2-oxofuran-3-yl)-2',3'-dehydrosalannol (17), were isolated from an EtOH extract of the leaf of neem (Azadirachta indica). The structures of the new compounds were elucidated on the basis of extensive spectroscopic analyses and comparison with literature. Upon evaluation of the cytotoxic activities of these compounds against leukemia (HL60), lung (A549), stomach (AZ521), and breast (SK-BR-3) cancer cell lines, seven compounds, i.e., 1-3, 12, 13, 15, and 16, exhibited potent cytotoxicities with IC50 values in the range of 0.1-9.9 μM against one or more cell lines. Among these compounds, cytotoxicity of nimonol (1; IC50 2.8 μM) against HL60 cells was demonstrated to be mainly due to the induction of apoptosis by flow cytometry. Western blot analysis suggested that compound 1 induced apoptosis via both the mitochondrial and death receptor-mediated pathways in HL60 cells. In addition, when compounds 1-17 were evaluated for their inhibitory activities against melanogenesis in B16 melanoma cells, induced with α-melanocyte-stimulating hormone (α-MSH), seven compounds, 1, 2, 4-6, 15, and 16, exhibited inhibitory activities with 31-94% reduction of melanin content at 10 μM concentration with no or low toxicity to the cells (82-112% of cell viability at 10 μM). All 17 compounds were further evaluated for their inhibitory effects against the EpsteinBarr virus early antigen (EBV-EA) activation induced by 12-O-tetradecanoylphorbol-13-acetate (TPA) in Raji cells. Copyright © 2014 Verlag Helvetica Chimica Acta AG, Zürich.

  3. Comparative study of anti-inflammatory, ulcerogenic and cytotoxic activities of racemate and S-ibuprofen

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    Flavio Henrique Nuevo Benez

    2013-08-01

    Full Text Available Ibuprofen is widely commercialized in racemic form. Although metabolic chiral inversion occurs through the conversion of R(--ibuprofen to S(+-ibuprofen and the latter enantiomer is considered the active form, clinical trials involving the administration of a racemate to S-enantiomer dosage ratio of 1:0.5 have demonstrated that S(+-ibuprofen is as efficacious as the racemic formulation. Moreover, the R(--enantiomer has been implicated in adverse gastrointestinal effects found with the racemic form, but the mechanisms involved in this process are not yet fully understood. The aim of the present study was to evaluate the anti-inflammatory activity of a racemate to S(+-ibuprofen dosage ratio of 1:0.5 using the carrageenan air pouch model of inflammation and determine both ulcerogenic activity and the chiral conversion rate in rats. An in vitro study of the cytotoxicity of racemate and S(+-ibuprofen in gastric cells was also performed. Although the plasma level of S(+-ibuprofen was raised after racemate administration, no significant difference was found in anti-inflammatory activity, as assessed by exudate formation, PGE2 production and leukocyte migration to the air pouches. Fewer gastric lesions were found after S(+-ibuprofen administration, despite the low gastric PGE2 content. In the in vitro study, the racemic compound proved more cytotoxic than S(+-ibuprofen. The present findings suggest that the S-enantiomer of ibuprofen could be considered a therapeutic alternative to minimize gastrointestinal side effects, since the chiral inversion of R(--ibuprofen to S(+-ibuprofen did not result in an improved anti-inflammatory response.

  4. EPR demonstration of iron-nitrosyl complex formation by cytotoxic activated macrophages.

    Science.gov (United States)

    Lancaster, J R; Hibbs, J B

    1990-02-01

    Activated macrophage cytotoxicity is characterized by loss of intracellular iron and inhibition of certain enzymes that have catalytically active nonheme-iron coordinated to sulfur. This phenomenon involves the oxidation of one of the terminal guanidino nitrogen atoms of L-arginine, which results in the production of citrulline and inorganic nitrogen oxides (NO2-, NO3-, and NO). We report here the results of an electron paramagnetic resonance spectroscopic study performed on cytotoxic activated macrophage (CAM) effector cells, which develop the same pattern of metabolic inhibition as their targets. Examination of activated macrophages from mice infected with Mycobacterium bovis (strain bacillus Calmette-Guérin) that were cultured in medium with lipopolysaccharide and L-arginine showed the presence of an axial signal at g = 2.039, which is similar to previously described iron-nitrosyl complexes formed from the destruction of iron-sulfur centers by nitric oxide (NO). Inhibition of the L-arginine-dependent pathway by addition of NG-monomethyl-L-arginine (methyl group on a terminal guanidino nitrogen) inhibits the production of nitrite, nitrate, citrulline, and the g = 2.039 signal. Comparison of the hyperfine structure of the signal from cells treated with L-arginine with terminal guanidino nitrogen atoms of natural abundance N14 atoms or labeled with N15 atoms showed that the nitrosyl group in this paramagnetic species arises from one of these two atoms. These results show that loss of iron-containing enzyme function in CAM is a result of the formation of iron-nitrosyl complexes induced by the synthesis of nitric oxide from the oxidation of a terminal guanidino nitrogen atom of L-arginine.

  5. EPR demonstration of iron-nitrosyl complex formation by cytotoxic activated macrophages

    Energy Technology Data Exchange (ETDEWEB)

    Lancaster, J.R. Jr.; Hibbs, J.B. Jr. (Utah State Univ., Logan (USA))

    1990-02-01

    Activated macrophage cytotoxicity is characterized by loss of intracellular iron and inhibition of certain enzymes that have catalytically active nonheme-iron coordinated to sulfur. This phenomenon involves the oxidation of one of the terminal guanidino nitrogen atoms of L-arginine, which results in the production of citrulline and inorganic nitrogen oxides (NO2-, NO3-, and NO). We report here the results of an electron paramagnetic resonance spectroscopic study performed on cytotoxic activated macrophage (CAM) effector cells, which develop the same pattern of metabolic inhibition as their targets. Examination of activated macrophages from mice infected with Mycobacterium bovis (strain bacillus Calmette-Guerin) that were cultured in medium with lipopolysaccharide and L-arginine showed the presence of an axial signal at g = 2.039, which is similar to previously described iron-nitrosyl complexes formed from the destruction of iron-sulfur centers by nitric oxide (NO). Inhibition of the L-arginine-dependent pathway by addition of NG-monomethyl-L-arginine (methyl group on a terminal guanidino nitrogen) inhibits the production of nitrite, nitrate, citrulline, and the g = 2.039 signal. Comparison of the hyperfine structure of the signal from cells treated with L-arginine with terminal guanidino nitrogen atoms of natural abundance N14 atoms or labeled with N15 atoms showed that the nitrosyl group in this paramagnetic species arises from one of these two atoms. These results show that loss of iron-containing enzyme function in CAM is a result of the formation of iron-nitrosyl complexes induced by the synthesis of nitric oxide from the oxidation of a terminal guanidino nitrogen atom of L-arginine.

  6. Lovastatin inhibits VEGFR and AKT activation: synergistic cytotoxicity in combination with VEGFR inhibitors.

    Directory of Open Access Journals (Sweden)

    Tong T Zhao

    Full Text Available BACKGROUND: In a recent study, we demonstrated the ability of lovastatin, a potent inhibitor of mevalonate synthesis, to inhibit the function of the epidermal growth factor receptor (EGFR. Lovastatin attenuated ligand-induced receptor activation and downstream signaling through the PI3K/AKT pathway. Combining lovastatin with gefitinib, a potent EGFR inhibitor, induced synergistic cytotoxicity in a variety of tumor derived cell lines. The vascular endothelial growth factor receptor (VEGFR and EGFR share similar activation, internalization and downstream signaling characteristics. METHODOLOGY/PRINCIPAL FINDINGS: The VEGFRs, particularly VEGFR-2 (KDR, Flt-1, play important roles in regulating tumor angiogenesis by promoting endothelial cell proliferation, survival and migration. Certain tumors, such as malignant mesothelioma (MM, also express both the VEGF ligand and VEGFRs that act in an autocrine loop to directly stimulate tumor cell growth and survival. In this study, we have shown that lovastatin inhibits ligand-induced VEGFR-2 activation through inhibition of receptor internalization and also inhibits VEGF activation of AKT in human umbilical vein endothelial cells (HUVEC and H28 MM cells employing immunofluorescence and Western blotting. Combinations of lovastatin and a VEGFR-2 inhibitor showed more robust AKT inhibition than either agent alone in the H28 MM cell line. Furthermore, combining 5 µM lovastatin treatment, a therapeutically relevant dose, with two different VEGFR-2 inhibitors in HUVEC and the H28 and H2052 mesothelioma derived cell lines demonstrated synergistic cytotoxicity as demonstrated by MTT cell viability and flow cytometric analyses. CONCLUSIONS/SIGNIFICANCE: These results highlight a novel mechanism by which lovastatin can regulate VEGFR-2 function and a potential therapeutic approach for MM through combining statins with VEGFR-2 inhibitors.

  7. Antioxidant, antimicrobial, antitumor, and cytotoxic activities of an important medicinal plant (Euphorbia royleana from Pakistan

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    Aisha Ashraf

    2015-03-01

    Full Text Available The aim of present study was to evaluate antioxidant, antimicrobial, and antitumor activities of methanol, hexane, and aqueous extracts of fresh Euphorbia royleana. Total phenolic and flavonoid contents were estimated as gallic acid and querectin equivalents, respectively. Antioxidant activity was assessed by scavenging of free 2,2′- diphenyl-1-picrylhydrazyl radicals and reduction of ferric ions, and it was observed that inhibition values increase linearly with increase in concentration of extract. The results of ferric reducing antioxidant power assay showed that hexane extract has maximum ferric reducing power (12.70 ± 0.49 mg gallic acid equivalents/g of plant extract. Maximum phenolic (47.47 ± 0.71 μg gallic acid equivalents/mg of plant extract and flavonoid (63.68 ± 0.43 μg querectin equivalents/mg of plant extract contents were also found in the hexane extract. Furthermore, we examined antimicrobial activity of the three extracts (methanol, hexane, aqueous against a panel of microorganisms (Escherichia coli, Bacillus subtillis, Pasteurella multocida, Aspergillus niger, and Fusarium solani by disc-diffusion assay, and found the hexane extract to be the best antimicrobial agent. Hexane extract was also observed as to be most effective in a potato disc assay. As hexane extract showed potent activity in all the investigated assays, it was targeted for cytotoxic assessment. Maximum cytotoxicity (61.66% by hexane extract was found at 800 μg/mL. It is concluded that investigated extracts have potential for isolation of antioxidant and antimicrobial compounds for the pharmaceutical industry.

  8. Expression and cytoprotective activity of the small GTPase RhoB induced by the Escherichia coli cytotoxic necrotizing factor 1

    DEFF Research Database (Denmark)

    Huelsenbeck, Stefanie C; Roggenkamp, Dennis; May, Martin

    2013-01-01

    B expression, based on the inactivation of Rho/Ras proteins. In this study, we report on a long lasting expression of RhoB in cultured cells upon activation of Rho proteins by the cytotoxic necrotizing factor 1 (CNF1) from Escherichia coli. The observations of this study highlight a new pathway involving Rac1......RhoB is the only member of the Rho subfamily of small GTPases, which is classified as an immediate early gene product. RhoB is up-regulated in response to growth factors as well as cytotoxic and genotoxic agents. Clostridial glucosylating toxins have been reported to evoke pronounced Rho......, which positively regulates the activity of the rhoB promoter and RhoB expression. Conversely, the isomeric cytotoxic necrotizing factor from Yersinia pseudotuberculosis (CNFy) drives GTP-loading of basal RhoB but fails to cause activation of the rhoB promoter and thus its expression. CNF1 inhibits...

  9. Flavonoid Derivatives from the Aerial Parts of Trifolium trichocephalum M. Bieb. and Their Antioxidant and Cytotoxic Activity

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    Gülin Renda

    2017-09-01

    Full Text Available Trifolium L. species with a rich isoflavone content have been used as expectorant, analgesic, antiseptic, tonic, and wound-healer in folk medicine. The aim of the study is to evaluate pharmacological properties of the extracts and isolated compounds of T. tricocephalum. Phytochemical investigation of the aerial parts of T. trichocephalum led to the isolation of daidzein, genistein, quercetin, and daidzein 4'-O-β-glucoside for the first time from this species. Isolated compounds along with the methanol extract, water, ethyl acetate and chloroform subextracts were tested for their radical scavenging and cytotoxic activity which was evaluated by MTT assay. According to the results of activity tests, extracts showed a concentration-dependent radical scavenging activity as well as cytotoxic effect on HepG2 cells at 400 μg/mL, whereas the compounds did not exert any obvious cytotoxic effect at tested concentrations.

  10. Antibacterial activity and cytotoxicity of Pterocarpus erinaceus Poir extracts, fractions and isolated compounds.

    Science.gov (United States)

    Tittikpina, Nassifatou Koko; Nana, Frédéric; Fontanay, Stéphane; Philippot, Stéphanie; Batawila, Komlan; Akpagana, Koffi; Kirsch, Gilbert; Chaimbault, Patrick; Jacob, Claus; Duval, Raphaël Emmanuel

    2018-02-15

    Pterocarpus erinaceus has been chosen based on ethnobotanical surveys carried out in the Tchamba district of the Republic of Togo. Investigation of the antibacterial as well as cytotoxic activities of whole extracts, fractions and compounds isolated from the leaves, trunk bark and roots of Pterocarpus erinaceus. Bio-guided fractionation of the raw extracts of plant parts and subsequent isolation of compounds from active fractions using normal phase open column chromatography. The broth microdilution method was used to evaluate the antibacterial activity, based on the determination of Minimal Inhibitory Concentrations (MICs) against several bacterial species representative of the most commonly encountered infectious diseases worldwide. The cytotoxicity of the raw extract and the most active fractions on a human non-cancerous cell (namely MRC-5) was estimated with a MTT assay. The chemical structure of the compounds isolated was elucidated using a combination of advanced Nuclear Magnetic Resonance (NMR) and Mass Spectrometry (MS). All extracts and fractions tested have shown good activities against Gram-positive bacteria (including Methicillin-Resistant Staphylococcus aureus, MRSA) and against Pseudomonas aeruginosa with MIC values ranging from 32µg/mL to 256µg/mL. In contrast, extracts were not toxic to MRC-5 cells. Four compounds have been isolated: Compound 1 (friedeline); Compound 2 (2,3 dihydroxypropyloctacosanoate); Compound 3 (a mixture of β-sitosterol, stigmasterol and campesterol); Compound 4 (β-sitosteryl-β-D-glucopyranoside) and shown to be active against some of the bacteria tested. They were active with MIC equal to 4µg/mL against strains of S. aureus (including MRSA). To the best of our knowledge, all of them except friedeline have never been reported in this plant species. P. erinaceus is confirmed as a plant harboring promising antibacterial activity with activities against serious human pathogens at very low concentrations. Some of the

  11. Confinement at Large Nc

    NARCIS (Netherlands)

    Hooft, G. 't

    2004-01-01

    A discussion is given of the confinement mechanism in terms of the Abelian projection scheme, for a general number Nc of colors. There is a difficulty in the Nc to infinity limit that requires a careful treatment, as the charges of the condensing magnetic monopoles tend to infinity. We suggest that

  12. Chemical Composition and Cytotoxic and Antibacterial Activities of the Essential Oil of Aloysia citriodora Palau Grown in Morocco.

    Science.gov (United States)

    Oukerrou, Moulay Ali; Tilaoui, Mounir; Mouse, Hassan Ait; Leouifoudi, Inass; Jaafari, Abdeslam; Zyad, Abdelmajid

    2017-01-01

    The aim of this work is to investigate the in vitro cytotoxic and antibacterial effects of the essential oils of Aloysia citriodora Palau, harvested in different regions of Morocco. The chemical profile was established using gas chromatography-mass spectrometry analysis. The cytotoxic activity against P815, MCF7, and VERO cell lines as well as the normal human peripheral blood mononuclear cells (PBMCs) was evaluated using the MTT assay. Standard, ATCC, strains of bacteria (Escherichia coli, Staphylococcus aureus, and Pseudomonas aeruginosa) were cultivated in Muller Hinton media. Then, agar disc diffusion, minimum inhibitory concentrations (MICs), and minimal bactericidal concentrations (MBCs) were determined using microdilution method. The essential oils obtained were predominantly composed of β-spathulenol (15.61%), Ar-curcumene (14.15%), trans-caryophyllene oxide (14.14%), and neral (10.02%). The results of the assays showed that the cytotoxic effect of the essential oil of A. citriodora was high on P815 and moderate on MCF7 and on VERO cell lines. However, no cytotoxic effect was observed on PBMCs. On the other hand, essential oils showed a significant antimicrobial activity against both Gram-negative and Gram-positive bacteria. MICs ranged between 2.84 and 8.37 mg/ml. Essential oil of A. citriodora leaves possesses significant antibacterial effect and cytotoxic activity against tumor cell lines.

  13. Chemical Composition and Cytotoxic and Antibacterial Activities of the Essential Oil of Aloysia citriodora Palau Grown in Morocco

    Directory of Open Access Journals (Sweden)

    Moulay Ali Oukerrou

    2017-01-01

    Full Text Available The aim of this work is to investigate the in vitro cytotoxic and antibacterial effects of the essential oils of Aloysia citriodora Palau, harvested in different regions of Morocco. The chemical profile was established using gas chromatography-mass spectrometry analysis. The cytotoxic activity against P815, MCF7, and VERO cell lines as well as the normal human peripheral blood mononuclear cells (PBMCs was evaluated using the MTT assay. Standard, ATCC, strains of bacteria (Escherichia coli, Staphylococcus aureus, and Pseudomonas aeruginosa were cultivated in Muller Hinton media. Then, agar disc diffusion, minimum inhibitory concentrations (MICs, and minimal bactericidal concentrations (MBCs were determined using microdilution method. The essential oils obtained were predominantly composed of β-spathulenol (15.61%, Ar-curcumene (14.15%, trans-caryophyllene oxide (14.14%, and neral (10.02%. The results of the assays showed that the cytotoxic effect of the essential oil of A. citriodora was high on P815 and moderate on MCF7 and on VERO cell lines. However, no cytotoxic effect was observed on PBMCs. On the other hand, essential oils showed a significant antimicrobial activity against both Gram-negative and Gram-positive bacteria. MICs ranged between 2.84 and 8.37 mg/ml. Essential oil of A. citriodora leaves possesses significant antibacterial effect and cytotoxic activity against tumor cell lines.

  14. Chemical composition and cytotoxicity of extracts of marjoram and rosemary and their activity against Sporothrix brasiliensis.

    Science.gov (United States)

    Waller, Stefanie Bressan; Madrid, Isabel Martins; Hoffmann, Jéssica Fernanda; Picoli, Tony; Cleff, Marlete Brum; Chaves, Fábio Clasen; Faria, Renata Osório de; Meireles, Mário Carlos Araújo; Braga de Mello, João Roberto

    2017-07-01

    Motivated by increasing reports of antifungal resistance in human and animal sporotrichosis, this study evaluated the chemical composition, cytotoxicity and anti-Sporothrix brasiliensis activity of extracts of marjoram (Origanum majorana) and rosemary (Rosmarinus officinalis). Ten (INF10) and 60 min (INF60) infusions, a decoction and a hydroalcoholic extract (HAE, 70 %) were prepared from both plants (10 % w/v). The extract composition was analysed by liquid chromatography/mass spectrometry and the cytotoxicity was evaluated using a colorimetric assay in canine and feline kidney cells. Using a broth microdilution assay (CLSI M38-A2) adapted to the extracts, 30 Sporothrix brasiliensis isolates from dogs, cats and humans, and one Sporothrix schenckii were tested.Results/Key findings. The predominant phenolic compounds found in all extracts were 4-hydroxybenzoic acid, caffeic acid and chlorogenic acid. Luteolin was also one of the predominant compounds, but only in the HAE of marjoram. Extracts of marjoram maintained cell viability in concentrations up to 2.5 mg ml-1 for the feline cell line and up to 10 mg ml-1 for the canine cell line, whereas in rosemary, the cell viability for both kidney lines was maintained with concentrations up to 5 mg ml-1. The activity of rosemary extracts was low or absent. Among the marjoram extracts, HAE was highlighted and had fungistatic activity against Sporothrix brasiliensis (MIC5040 mg ml-1), including in all itraconazole-resistant isolates. S. schenckiisensu stricto was sensitive to marjoram extracts (MIC/MFC ≤5 mg ml-1), with the exception of INF10. These findings support the potential usefulness of the HAE of marjoram in the treatment of sporotrichosis.

  15. Antioxidant, 5-Lipoxygenase Inhibitory and Cytotoxic Activities of Compounds Isolated from the Ferula lutea Flowers

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    Mansour Znati

    2014-10-01

    Full Text Available A phytochemical investigation of the Ferula lutea (Poir. Maire flowers has led to the isolation of a new compound, (E-5-ethylidenefuran-2(5H-one-5-O-β-D-glucopyranoside (1, designated ferunide, 4-hydroxy-3-methylbut-2-enoic acid (2, reported for the first time as a natural product, together with nine known compounds, verbenone-5-O-β-D-glucopyranoside (3, 5-O-caffeoylquinic acid (4, methyl caffeate (5, methyl 3,5-O-dicaffeoylquinate (6, 3,5-O-dicaffeoylquinic acid (7, isorhamnetin-3-O-α-L-rhamnopyranosyl(1→6-β-D-glucopyranoside, narcissin (8, (−-marmesin (9, isoimperatorin (10 and 2,3,6-trimethylbenzaldehyde (11. Compounds 3–10 were identified for the first time in Ferula genus. Their structures were elucidated by spectroscopic methods, including 1D and 2D NMR experiments, mass spectroscopy and X-ray diffraction analysis (compound 2, as well as by comparison with literature data. The antioxidant, anti-inflammatory and cytotoxic activities of isolated compounds were evaluated. Results showed that compound 7 exhibited the highest antioxidant activity with IC50 values of 18 ± 0.5 µmol/L and 19.7 ± 0.7 µmol/L by DPPH radical and ABTS radical cation, respectively. The compound 6 exhibited the highest anti-inflammatory activity with an IC50 value of 5.3 ± 0.1 µmol/L against 5-lipoxygenase. In addition, compound 5 was found to be the most cytotoxic, with IC50 values of 22.5 ± 2.4 µmol/L, 17.8 ± 1.1 µmol/L and 25 ± 1.1 µmol/L against the HCT-116, IGROV-1 and OVCAR-3 cell lines, respectively.

  16. Antioxidant and Cytotoxic Activities and Phytochemical Analysis of Euphorbia wallichii Root Extract and its Fractions.

    Science.gov (United States)

    Ul-Haq, Ihsan; Ullah, Nazif; Bibi, Gulnaz; Kanwal, Simab; Sheeraz Ahmad, Muhammad; Mirza, Bushra

    2012-01-01

    Euphorbia wallichii a perennial herb growing mainly in Himalayas has been widely used in folk medicines for its medicinal properties. In the present study, the crude methanolic root extract (CME) and its fractions; n-Hexane Fraction (NHF), n-Butanol Fraction (NBF), Chloroform Fraction (CHF), Ethyl acetate Fraction (EAF) and Aqueous Fraction (AQF) of this plant specie were investigated for antioxidant and cytotoxic activities and phytochemical analysis. Antioxidant activity was determined by using 2,2-diphenyl-1-picryl-hydrazyl free radical (DPPH) and DNA protection assay performed on pBR322 plasmid DNA. In both these assays, promising results were obtained for CME as well as other fractions. The IC50 values for DPPH assay were in a range of 7.89 to 63.35 μg/ml in which EAF showed the best anti-oxidant potential and almost all the tested samples showed certain level of DNA protection. The cytotoxic activity was assessed by using Sulforhodamine B (SRB) assay on human cell lines; H157 (Lung Carcinoma) and HT144 (Malignant Melanoma). The IC50 values of the tested samples ranged from 0.18 to 1.4 mg/mL against H157 cell line whereas against HT144 cell line the IC50 values ranged from 0.46 to 17.88 mg/mL with NBF fraction showing maximum potential for both. Furthermore, the phytochemical analysis of CME and its fractions showed the presences of flavonoids, saponins, tannins, terpenoides and cardiac glycosides with varying concentrations.

  17. Green Adeptness in the Synthesis and Stabilization of Copper Nanoparticles: Catalytic, Antibacterial, Cytotoxicity, and Antioxidant Activities

    Science.gov (United States)

    Din, Muhammad Imran; Arshad, Farhan; Hussain, Zaib; Mukhtar, Maria

    2017-12-01

    Copper nanoparticles (CuNPs) are of great interest due to their extraordinary properties such as high surface-to-volume ratio, high yield strength, ductility, hardness, flexibility, and rigidity. CuNPs show catalytic, antibacterial, antioxidant, and antifungal activities along with cytotoxicity and anticancer properties in many different applications. Many physical and chemical methods have been used to synthesize nanoparticles including laser ablation, microwave-assisted process, sol-gel, co-precipitation, pulsed wire discharge, vacuum vapor deposition, high-energy irradiation, lithography, mechanical milling, photochemical reduction, electrochemistry, electrospray synthesis, hydrothermal reaction, microemulsion, and chemical reduction. Phytosynthesis of nanoparticles has been suggested as a valuable alternative to physical and chemical methods due to low cytotoxicity, economic prospects, environment-friendly, enhanced biocompatibility, and high antioxidant and antimicrobial activities. The review explains characterization techniques, their main role, limitations, and sensitivity used in the preparation of CuNPs. An overview of techniques used in the synthesis of CuNPs, synthesis procedure, reaction parameters which affect the properties of synthesized CuNPs, and a screening analysis which is used to identify phytochemicals in different plants is presented from the recent published literature which has been reviewed and summarized. Hypothetical mechanisms of reduction of the copper ion by quercetin, stabilization of copper nanoparticles by santin, antimicrobial activity, and reduction of 4-nitrophenol with diagrammatic illustrations are given. The main purpose of this review was to summarize the data of plants used for the synthesis of CuNPs and open a new pathway for researchers to investigate those plants which have not been used in the past.

  18. Antibacterial activity and cytotoxicity analysis of halistanol trisulphate from marine sponge Petromica citrina.

    Science.gov (United States)

    Marinho, Palloma R; Simas, Naomi Kato; Kuster, Ricardo Machado; Duarte, Rafael Silva; Fracalanzza, Sergio Eduardo Longo; Ferreira, Davis Fernandes; Romanos, Maria Teresa Villela; Muricy, Guilherme; Giambiagi-Demarval, Marcia; Laport, Marinella Silva

    2012-10-01

    An aqueous extract and fraction from the marine sponge Petromica citrina have antibacterial activity. We performed a chemical and biological characterization of the antibiotic substance from P. citrina and investigated its mode of action on Staphylococcus aureus cells. The inhibitory activity of the aqueous extract of P. citrina was determined against 14 bacteria belonging to type strains and clinical antibiotic-resistant strains. The aqueous extract was fractionated under bioassay guidance and the bioactive substance was identified by its (1)H-NMR, (13)C-NMR and mass spectra. The MIC and the MBC of this substance were determined. This substance was also subjected to cytotoxic bioassays. The mode of action on S. aureus cells was investigated by light and transmission electron microscopy analysis. P. citrina showed a large spectrum of activity against type strains and resistant-bacteria such as S. aureus, Staphylococcus epidermidis, Enterococcus faecalis, Mycobacterium fortuitum and Neisseria gonorrhoeae. The aqueous extract was fractionated and halistanol trisulphate (24ε,25-dimethylcholestane-2β,3α,6α-triol trisodium sulphate) was isolated for the first time from P. citrina. Halistanol trisulphate had a bactericidal effect on exponentially growing S. aureus cells at the MIC (512 mg/L). Cytotoxicity biossays showed moderate toxicity against cancer cell line L929 (fibrosarcoma). This substance apparently acts by damaging the cell membrane, with subsequent cell lysis. Halistanol trisulphate is a broad-spectrum antibiotic isolated from P. citrina with a mode of action involving disruption of the cytoplasmic membrane. It is a new candidate for research on antibacterial substances.

  19. In vitro parallel evaluation of antibacterial activity and cytotoxicity of commercially available silver-containing wound dressings

    Directory of Open Access Journals (Sweden)

    Yunoki S

    2015-01-01

    Full Text Available Shunji Yunoki,1 Masushi Kohta,2 Yoshimi Ohyabu,1 Tetsuji Iwasaki2 1Biotechnology Group, Tokyo Metropolitan Industrial Technology Research Institute, 2Medical Engineering Laboratory, ALCARECo., Ltd, Tokyo, Japan Purpose: This study evaluated the in vitro antibacterial activity and cytotoxicity of various commercially available silver-containing dressings (Ag dressing. Methods: Biohesive Ag (hydrocolloid, silver sulfadiazine, Aquacel® Ag (nonwoven fabric, ionic silver [Ag+], Algisite™ Ag (nonwoven fabric, Ag+, Mepilex® Ag (foam, silver sulfate, and PolyMem® Ag (foam, nanocrystalline silver were tested for characteristics of Ag+ release, antibacterial activity, and cytotoxicity. The release of Ag+ was investigated in cell culture medium at immersion periods of 6, 24, and 48 hours. The antibacterial activity against Staphylococcus aureus and Pseudomonas aeruginosa were accessed by a disc diffusion test. The cytotoxicity was evaluated using V79 cells, by an extraction method. Results: The cytotoxicity was not a monotonic function of the antibacterial activity among the Ag dressings and could not be simply explained by Ag+-release properties. Biohesive Ag was regarded as a slow-release Ag dressing, showing the lowest cytotoxicity, while the antibacterial activity was classified as “strong” or “significant” against the two species of bacteria. Aquacel Ag and Algisite Ag showed higher antibacterial activity and cytotoxic effects, which were supported by the higher Ag+ release. Mepilex Ag showed the highest release of Ag+, and the cytotoxicity was the highest among the Ag dressings. However, the antibacterial activity was classified as “significant” or “no activity” for P. aeruginosa and S. aureus, respectively. PolyMem Ag showed the lowest Ag+ release, and the antibacterial activity classified as “significant" or "no activity” for S. aureus and P. aeruginosa, respectively, whereas the cytotoxicity was similar to those of Aquacel

  20. Cytotoxic activity of two natural sesquiterpene lactones, isobutyroylplenolin and arnicolide D, on human colon cancer cell line HT-29.

    Science.gov (United States)

    Huang, Xuedan; Awano, Yurika; Maeda, Eri; Asada, Yoshihisa; Takemoto, Hiroaki; Watanabe, Takashi; Kojima-Yuasa, Akiko; Kobayashi, Yoshinori

    2014-01-01

    In this study, we found that two sesquiterpene lactones, isobutyroylplenolin and arnicolide D, from Centipeda minima L. (Compositae) exerted stronger cytotoxic activity than cisplatin on the human colon carcinoma HT-29 cell line. Furthermore, the cytotoxicity of these two compounds on normal cells was weaker than that of cisplatin. Treatment with isobutyroylplenolin and arnicolide D increased the levels of intracellular reactive oxygen species and decreased the levels of nuclear factor-κB protein, resulting in cell cycle arrest in G1 phase and apoptosis. We also discuss the difference in structure and activity between these two compounds.

  1. Improved antioxidative and cytotoxic activities of chamomile (Matricaria chamomilla) florets fermented by Lactobacillus plantarum KCCM 11613P*

    OpenAIRE

    Park, Eun-Hye; Bae, Won-young; Eom, Su-Jin; Kim, Kee-Tae; Paik, Hyun-Dong

    2017-01-01

    Antioxidative and cytotoxic effects of chamomile (Matricaria chamomilla) fermented by Lactobacillus plantarum were investigated to improve their biofunctional activities. Total polyphenol (TP) content was measured by the Folin-Denis method, and the antioxidant activities were assessed by the 1,1-diphenyl-2-picrylhydrazyl (DPPH) method and β-carotene bleaching method. AGS, HeLa, LoVo, MCF-7, and MRC-5 (normal) cells were used to examine the cytotoxic effects by 3-(4,5-dimethylthiazol-2-yl)-2,5...

  2. Biosurfactants production potential of native strains of Bacillus cereus and their antimicrobial, cytotoxic and antioxidant activities.

    Science.gov (United States)

    Basit, Madiha; Rasool, Muhammad Hidayat; Naqvi, Syed Ali Raza; Waseem, Muhammad; Aslam, Bilal

    2018-01-01

    Present study was designed to evaluate the biosurfactant production potential by native strains of Bacillus cereus as well as determine their antimicrobial and antioxidant activities. The strains isolated from garden soil were characterized as B. cereus MMIC 1, MMIC 2 and MMIC 3. Biosurfactants were extracted as grey white precipitates. Optimum conditions for biosurfactant production were 37°C, the 7th day of incubation, 0.5% NaCl, pH 7.0. Moreover, corn steep liquor was the best carbon source. Biuret test, Thin Layer Chromatography (TLC), agar double diffusion and Fourier Transform Infrared Spectroscopy (FTIR) characterized the biosurfactants as cationic lipopeptides. Biosurfactants exhibited significant antibacterial and antifungal activity against S. aureus, E. coli, P. aeruginosa, K. pneumoniae, A. niger and C. albicans at 30 mg/ml. Moreover, they also possessed antiviral activity against NDV at 10 mg/ml. Cytotoxicity assay in BHK-21 cell lines revealed 63% cell survival at 10 mg/ml of biosurfactants and thus considered as safe. They also showed very good antioxidant activity by ferric-reducing activity and DPPH scavenging activity at 2 mg/ml. Consequently, the study offers an insight for the exploration of new bioactive molecules from the soil. It was concluded that lipopeptide biosurfactants produced from native strains of B. cereus may be recommended as safe antimicrobial, emulsifier and antioxidant agent.

  3. Synthesis, Antimycobacterial Activity and In Vitro Cytotoxicity of 5-Chloro-N-phenylpyrazine-2-carboxamides

    Directory of Open Access Journals (Sweden)

    Jan Zitko

    2013-12-01

    Full Text Available 5-Chloropyrazinamide (5-Cl-PZA is an inhibitor of mycobacterial fatty acid synthase I with a broad spectrum of antimycobacterial activity in vitro. Some N-phenylpyrazine-2-carboxamides with different substituents on both the pyrazine and phenyl core possess significant in vitro activity against Mycobacterium tuberculosis. To test the activity of structures combining both the 5-Cl-PZA and anilide motifs a series of thirty 5-chloro-N-phenylpyrazine-2-carboxamides with various substituents R on the phenyl ring were synthesized and screened against M. tuberculosis H37Rv, M. kansasii and two strains of M. avium. Most of the compounds exerted activity against M. tuberculosis H37Rv in the range of MIC = 1.56–6.25 µg/mL and only three derivatives were inactive. The phenyl part of the molecule tolerated many different substituents while maintaining the activity. In vitro cytotoxicity was decreased in compounds with hydroxyl substituents, preferably combined with other hydrophilic substituents. 5-Chloro-N-(5-chloro-2-hydroxyphenylpyrazine-2-carboxamide (21 inhibited all of the tested strains (MIC = 1.56 µg/mL for M. tuberculosis; 12.5 µg/mL for other strains. 4-(5-Chloropyrazine-2-carboxamido-2-hydroxybenzoic acid (30 preserved good activity (MIC = 3.13 µg/mL M. tuberculosis and was rated as non-toxic in two in vitro models (Chinese hamster ovary and renal cell adenocarcinoma cell lines; SI = 47 and 35, respectively.

  4. NEW SEMISYNTHETIC DERIVATIVES OF A BENZYLISOTHIOCYANATE ISOLATED FROM Moringa oleifera AND EVALUATION OF THEIR CYTOTOXIC ACTIVITY

    Directory of Open Access Journals (Sweden)

    Diana Kelly C. de Almeida

    Full Text Available From the natural product 4-(4'-O-acetyl-α-L-rhamnosyloxybenzylisothiocyanate (1, isolated from the flowers of Moringa oleifera Lam (Moringaceae, four new semisynthetic derivatives, N-[4-(4'-O-acetyl-α-L-rhamnosyloxybenzyl]-2-(pyridinil-4-carbonilhydrazine-1-carbothioamide (3, 4-(4'-O-acetyl-2',3'-dimesyloxy-α-L-rhamnosyloxybenzylisothiocyanate (4, N-[(4'-O-acetyl-α-L-rhamnosyloxybenzyl]hydrazinecarbothioamide (5, 4-[4'-O-acetyl-2',3'-O-bis(decanoiloxy-α-L-rhamnosyloxy]benzylisothiocianate (6, and the known compound 4-(2',3',4'-O-triacetyl-α-L-rhamnosyloxybenzylisothiocyanate (2, were obtained. All compounds were tested for their cytotoxicity against the tumor cell lines SF-295, HL-60, HCT-116 e PC-3. The natural product 1 and the semisynthetic derivatives 2 and 4 were the most active compounds (IC50 from16.0 to 3.7 µmol L-1 against all tumor cell lines.

  5. X-Ray structure and cytotoxic activity of a picolinate ruthenium(II–arene complex

    Directory of Open Access Journals (Sweden)

    IVANKA IVANOVIĆ

    2011-01-01

    Full Text Available A ruthenium(II–arene complex with picolinic acid, [(η6-p-cymeneRuCl(pico]∙H2O, was prepared by the reaction of [(η6-p-cymeneRuCl2]2 with picolinic acid in a 1:2 molar ratio in 2-propanol. The compound was characterized by elemental analysis, and IR and NMR spectroscopy. X-ray diffraction analysis showed that the molecule adopts a “three-leg piano-stool” geometry, which is common for this type of complexes. The cytotoxic activity of the complex was tested in two human cancer cell lines HeLa (cervix and FemX (melanoma by MTT assay. The IC50 values were at 82.0 and 36.2 µmol dm-3 for HeLa and FemX cells, respectively.

  6. Studies of Antiviral Activity and Cytotoxicity of Wrightia tinctoria and Morinda citrifolia

    Science.gov (United States)

    Selvam, P.; Murugesh, N.; Witvrouw, M.; Keyaerts, E.; Neyts, J.

    2009-01-01

    Different extracts of leaf parts of Wrightia tinctoria and fruit powder of Morinda citrifolia have been studied against replication of HIV-1(IIIB) in MT-4 cells and HCV in Huh 5.2 cells. Chloroform extract of Wrightia tinctoria exhibited a maximum protection of 48% against the cytopathic effect of HIV-1(IIIB) in MT-4 cells. Fruit juice of Morinda citrifolia exhibited a displayed marked cytotoxic activity in lymphocyte (MT-4) cells (CC50: 0.19 mg/ml). The 50% effective concentration for inhibition of HCV subgenomic replicon replication in Huh 5-2 cells by Morinda citrifolia was 0.98 μg/ml and by chloroform extract of Wrightia tinctoria was 10 μg/ml. The concentration that reduced the growth of exponentially proliferating Huh 5-2 cells by 50% was greater than 50 μg/ml. PMID:20376221

  7. Synthesis and evaluation of arylamidine derivatives for new antimicrobial and cytotoxic activities

    Directory of Open Access Journals (Sweden)

    ZENAIDE S. MONTE

    Full Text Available ABSTRACT A series of arylamidines 3a-j was designed, synthesized and investigated for antimicrobial activity. Structures of the compounds were confirmed by IR, 1H-NMR and 13C-NMR and a 2D spectroscopic study was performed. A preliminary screening of the antimicrobial tests clearly showed that three out of ten arylamidines, viz, 3f, 3g and 3i, were effective against all the gram-negative bacteria: Klebsiella pneumoniae, Pseudomonas aeruginosa and Salmonella enteric; and against the yeast, candida albicans. Further, the Minimum Inhibitory Concentrations (MIC against the bacteria and yeast were determined. All compounds 3a-d, 3f, 3g, 3i and 3j were also investigated for their low cytotoxic effects on tested cell lines. Compounds 3d and 3f were the most effective derivatives against HL-60 and HEp-2 cells, respectively, with IC50 value (2µg/mL, and low normal cells toxicity.

  8. Synthesis and evaluation of arylamidine derivatives for new antimicrobial and cytotoxic activities.

    Science.gov (United States)

    Monte, Zenaide S; Silva, Amanda M; Lima, Gláucia M S; Silva, Teresinha G DA; Marques, Karla M R; Rodrigues, Maria D; Falcão, Emerson P S; Melo, Sebastião J

    2017-01-01

    A series of arylamidines 3a-j was designed, synthesized and investigated for antimicrobial activity. Structures of the compounds were confirmed by IR, 1H-NMR and 13C-NMR and a 2D spectroscopic study was performed. A preliminary screening of the antimicrobial tests clearly showed that three out of ten arylamidines, viz, 3f, 3g and 3i, were effective against all the gram-negative bacteria: Klebsiella pneumoniae, Pseudomonas aeruginosa and Salmonella enteric; and against the yeast, candida albicans. Further, the Minimum Inhibitory Concentrations (MIC) against the bacteria and yeast were determined. All compounds 3a-d, 3f, 3g, 3i and 3j were also investigated for their low cytotoxic effects on tested cell lines. Compounds 3d and 3f were the most effective derivatives against HL-60 and HEp-2 cells, respectively, with IC50 value (2µg/mL), and low normal cells toxicity.

  9. Conjugates of methylated cyclodextrin derivatives and hydroxyethyl starch (HES: Synthesis, cytotoxicity and inclusion of anaesthetic actives

    Directory of Open Access Journals (Sweden)

    Lisa Markenstein

    2014-12-01

    Full Text Available The mono-6-deoxy-6-azides of 2,6-di-O-methyl-β-cyclodextrin (DIMEB and randomly methylated-β-cyclodextrin (RAMEB were conjugated to propargylated hydroxyethyl starch (HES by Cu+-catalysed [2 + 3] cycloaddition. The resulting water soluble polymers showed lower critical solution temperatures (LCST at 52.5 °C (DIMEB-HES and 84.5 °C (RAMEB-HES, respectively. LCST phase separations could be completely avoided by the introduction of a small amount of carboxylate groups at the HES backbone. The methylated CDs conjugated to the HES backbone exhibited significantly lower cytotoxicities than the corresponding monomeric CD derivatives. Since the binding potentials of these CD conjugates were very high, they are promising candidates for new oral dosage forms of anaesthetic actives.

  10. Asterosaponins and glycosylated polyhydroxysteroids from the starfish Culcita novaeguineae and their cytotoxic activities.

    Science.gov (United States)

    Ngoan, Bui Thi; Hanh, Tran Thi Hong; Vien, Le Thi; Diep, Chau Ngoc; Thao, Nguyen Phuong; Thao, Do Thi; Thanh, Nguyen Van; Cuong, Nguyen Xuan; Nam, Nguyen Hoai; Thung, Do Cong; Kiem, Phan Van; Kim, Young Ho; Minh, Chau Van

    2015-01-01

    Using combined chromatographic methods, two asterosaponins (compounds 1 and 2), including a new compound novaeguinoside E (compound 1), and six glycosylated polyhydroxysteroids (compounds 3-8) were isolated from a methanol extract of the starfish Culcita novaeguineae. Their structures were determined on the basis of spectroscopic data ((1)H and (13)C NMR, HSQC, HMBC, (1)H-(1)H COSY, ROESY, and HRESI-MS) and by comparison with the literature values. The new compound 1 represents the third example of asterosaponins containing the 5α-cholesta-9(1l)-en-3β,6α,20,22-tetraol aglycone. Among isolated compounds, 4-7 exhibited moderate to weak cytotoxic activities against five human cancer cell lines such as Hep-G2 (hepatoma), KB (epidermoid carcinoma), LNCaP (prostate cancer), MCF7 (breast cancer), and SK-Mel2 (melanoma).

  11. Cytotoxic Activity of Holothuria leucospilota Extract against Leishmania infantum In Vitro

    Directory of Open Access Journals (Sweden)

    Shahram Khademvatan

    2016-01-01

    Full Text Available Leishmaniasis is a tropical parasitic infection. The resistance and toxicity issues are the major complications and remain significant consequences related to the treatment of leishmaniasis with the recent and classical drugs. Thus there is an immediate requirement to develop new compounds for the treatment of this protozoan disease. Sea cucumbers or holothurians are potentially presented as the marine sources of antimicrobial and cytotoxic compounds. The aim of this study was investigation of in vitro antileishmanial activity of methanol extract of body wall, coelomic fluid, and cuvierian organs of Holothuria leucospilota obtained from coastal parts of Persian Gulf against Leishmania infantum promastigotes and axenic amastigotes. The colorimetric MTT assay was used to determine L. infantum promastigotes and axenic amastigotes viability at different concentrations of the extracts and drug control (Glucantime® at time dependent manner and the results are represented as IC50 (50% of inhibitory concentration. Coelomic fluid was the most active extract among the three different extracts of H. leucospilota against L. infantum promastigotes and axenic amastigotes with IC50s of 62.33 μg/mL and 22.4 μg/mL and 73 μg/mL and 46 μg/mL at 48 and 72 hours after treatment, respectively. Cuvierian organs extract showed less toxicity with IC50s more than 1000 μg/mL for both Leishmania infantum axenic amastigotes and promastigotes forms after 48 and 72 hours of exposure. Results acquired from the present study propose that the sea cucumber H. leucospilota may be a provoking source of antileishmanial compounds and could be a lead source in the development of the potent antileishmanial and cytotoxic drugs.

  12. Cytotoxic Activity of Holothuria leucospilota Extract against Leishmania infantum In Vitro.

    Science.gov (United States)

    Khademvatan, Shahram; Eskandari, Alborz; Saki, Jasem; Foroutan-Rad, Masoud

    2016-01-01

    Leishmaniasis is a tropical parasitic infection. The resistance and toxicity issues are the major complications and remain significant consequences related to the treatment of leishmaniasis with the recent and classical drugs. Thus there is an immediate requirement to develop new compounds for the treatment of this protozoan disease. Sea cucumbers or holothurians are potentially presented as the marine sources of antimicrobial and cytotoxic compounds. The aim of this study was investigation of in vitro antileishmanial activity of methanol extract of body wall, coelomic fluid, and cuvierian organs of Holothuria leucospilota obtained from coastal parts of Persian Gulf against Leishmania infantum promastigotes and axenic amastigotes. The colorimetric MTT assay was used to determine L. infantum promastigotes and axenic amastigotes viability at different concentrations of the extracts and drug control (Glucantime®) at time dependent manner and the results are represented as IC50 (50% of inhibitory concentration). Coelomic fluid was the most active extract among the three different extracts of H. leucospilota against L. infantum promastigotes and axenic amastigotes with IC50s of 62.33 μg/mL and 22.4 μg/mL and 73 μg/mL and 46 μg/mL at 48 and 72 hours after treatment, respectively. Cuvierian organs extract showed less toxicity with IC50s more than 1000 μg/mL for both Leishmania infantum axenic amastigotes and promastigotes forms after 48 and 72 hours of exposure. Results acquired from the present study propose that the sea cucumber H. leucospilota may be a provoking source of antileishmanial compounds and could be a lead source in the development of the potent antileishmanial and cytotoxic drugs.

  13. Characterization and cytotoxic activity of sulfated derivatives of polysaccharides from Agaricus brasiliensis

    Science.gov (United States)

    Cardozo, F. T. G. S.; Camelini, C. M.; Cordeiro, M. N. S.; Mascarello, A.; Malagoli, B. G.; Larsen, I.; Rossi, M. J.; Nunes, R. J.; Braga, F. C.; Brandt, C.R.; Simões, C. M. O.

    2014-01-01

    Agaricus brasiliensis cell-wall polysaccharides isolated from fruiting body (FR) and mycelium (MI) and their respective sulfated derivatives (FR-S and MI-S) were chemically characterized using elemental analysis, TLC, FT-IR, NMR, HPLC, and thermal analysis. Cytotoxic activity was evaluated against A549 tumor cells by MTT and sulforhodamine assays. The average molecular weight (Mw) of FR and MI was estimated to be 609 and 310 kDa, respectively. FR-S (127 kDa) and MI-S (86 kDa) had lower Mw, probably due to hydrolysis occurred during the sulfation reaction. FR-S and MI-S presented ~14 % sulfur content in elemental analysis. Sulfation of samples was characterized by the appearance of two new absorption bands at 1253 and 810 cm−1 in the infrared spectra, related to S=O and C-S-O sulfate groups, respectively. Through 1H and 13C NMR analysis FR-S was characterized as a (1→6)-(1→3)-β-D-glucan fully sulfated at C-4 and C-6 terminal and partially sulfated at C-6 of (1→3)-β-D-glucan moiety. MI-S was shown to be a (1→3)-β-D-gluco-(1→2)-β-D-mannan, partially sulfated at C-2, C-3, C-4, and C-6, and fully sulfated at C-6 of the terminal residues. The combination of high degree of sulfation and low molecular weight was correlated with the increased cytotoxic activity (48 h of treatment) of both FR-S (EC50=605.6 μg/mL) and MI-S (EC50=342.1 μg/mL) compared to the non-sulfated polysaccharides FR and MI (EC50>1500 μg/mL). PMID:23511057

  14. Anti-inflammatory, anti-bacterial, and cytotoxic activity of fibrous clays.

    Science.gov (United States)

    Cervini-Silva, Javiera; Nieto-Camacho, Antonio-; Ramírez-Apan, María Teresa; Gómez-Vidales, Virginia; Palacios, Eduardo; Montoya, Ascención; Ronquillo de Jesús, Elba

    2015-05-01

    Produced worldwide at 1.2m tons per year, fibrous clays are used in the production of pet litter, animal feed stuff to roof parcels, construction and rheological additives, and other applications needing to replace long-fiber length asbestos. To the authors' knowledge, however, information on the beneficial effects of fibrous clays on health remains scarce. This paper reports on the anti-inflammatory, anti-bacterial, and cytotoxic activity by sepiolite (Vallecas, Spain) and palygorskite (Torrejon El Rubio, Spain). The anti-inflammatory activity was determined using the 12-O-tetradecanoylphorbol-13-acetate (TPA) and myeloperoxidase (MPO) methods. Histological cuts were obtained for quantifying leukocytes found in the epidermis. Palygorkite and sepiolite caused edema inhibition and migration of neutrophils ca. 68.64 and 45.54%, and 80 and 65%, respectively. Fibrous clays yielded high rates of infiltration, explained by cleavage of polysomes and exposure of silanol groups. Also, fibrous clays showed high inhibition of myeloperoxidase contents shortly after exposure, but decreased sharply afterwards. In contrast, tubular clays caused an increasing inhibition of myeloperoxidase with time. Thus, clay structure restricted the kinetics and mechanism of myeloperoxidase inhibition. Fibrous clays were screened in vitro against human cancer cell lines. Cytotoxicity was determined using the protein-binding dye sulforhodamine B (SRB). Exposing cancer human cells to sepiolite or palygorskite showed growth inhibition varying with cell line. This study shows that fibrous clays served as an effective anti-inflammatory, limited by chemical transfer and cellular-level signals responding exclusively to an early exposure to clay, and cell viability decreasing significantly only after exposure to high concentrations of sepiolite. Copyright © 2015 Elsevier B.V. All rights reserved.

  15. In vitro evaluation of the cytotoxic and trypanocidal activities of Ampelozizyphus amazonicus (Rhamnaceae

    Directory of Open Access Journals (Sweden)

    L.V. Rosas

    2007-05-01

    Full Text Available Ampelozizyphus amazonicus Ducke is a tree commonly found in the Amazon region and an extract of its stem bark is popularly used as an antimalarial and anti-inflammatory agent and as an antidote to snake venom. Ursolic acid; five lupane type triterpenes: betulin, betulinic acid, lupenone, 3ß-hydroxylup-20(29-ene-27,28-dioic acid, and 2a,3ß-dihydroxylup-20(29-ene-27,28-dioic acid, and three phytosteroids: stigmasterol, sitosterol and campesterol, have been isolated from stem extracts of A. amazonicus Ducke. Their structures were characterized by spectral data including COSY and HMQC. In an in vitro biological screening of the isolated compounds, 3ß-hydroxylup-20(29-ene-27,28-dioic acid was cytotoxic against the SKBR-3 human adenocarcinoma cell line (1 to 10 mg/mL, while 2a,3ß-dihydroxylup-20(29-ene-27,28-dioic acid exhibited cytotoxicity against both SKBR-3 human adenocarcinoma and C-8161 human melanoma tumor cell lines (>0.1 mg/mL. In the present study, different extracts and some fractions of this plant were also investigated for trypanocidal activity due to the presence of pentacyclic triterpenes. The triterpene classes are potent against Trypanosoma cruzi. The bioassays were carried out using blood collected from Swiss albino mice by cardiac puncture during the parasitemic peak (7th day after infection with the Y strain of T. cruzi. The results obtained showed that A. amazonicus is a potential source of bioactive compounds since its extracts and fractions isolated from it exhibited in vitro parasite lysis against trypomastigote forms of T. cruzi at concentrations >100 µg/mL. Fractions containing mainly betulin, lupenone, 3ß-hydroxylup-20(29-ene-27,28-dioic acid, and 2a,3ß-dihydroxylup-20(29-ene-27,28-dioic acid showed more activity than crude extracts.

  16. MULTIVALENT DISPLAY OF PENDANT PRO-APOPTOTIC PEPTIDES INCREASES CYTOTOXIC ACTIVITY

    Science.gov (United States)

    Chu, David S.H.; Bocek, Michael J.; Shi, Julie; Ta, Anh; Ngambenjawong, Chayanon; Rostomily, Robert C.; Pun, Suzie H.

    2015-01-01

    Several cationic antimicrobial peptides have been investigated as potential anti-cancer drugs due to their demonstrated selective toxicity towards cancer cells relative to normal cells. For example, intracellular delivery of KLA, a pro-apoptotic peptide, results in toxicity against a variety of cancer cell lines; however, the relatively low activity and small size leads to rapid renal excretion when applied in vivo, limiting its therapeutic potential. In this work, apoptotic peptide-polymer hybrid materials were developed to increase apoptotic peptide activity via multivalent display. Multivalent peptide materials were prepared with comb-like structure by RAFT copolymerization of peptide macromonomers with N-(2-hydroxypropyl) methacrylamide (HPMA). Polymers displayed a GKRK peptide sequence for targeting p32, a protein often overexpressed on the surface of cancer cells, either fused with or as a comonomer to a KLA macromonomer. In three tested cancer cell lines, apoptotic polymers were significantly more cytotoxic than free peptides as evidenced by an order of magnitude decrease in IC50 values for the polymers compared to free peptide. The uptake efficiency and intracellular trafficking of one polymer construct was determined by radiolabeling and subcellular fractionation. Despite their more potent cytotoxic profile, polymeric KLA constructs have poor cellular uptake efficiency (<1%). A significant fraction (20%) of internalized constructs localize with intact mitochondrial fractions. In an effort to increase cellular uptake, polymer amines were converted to guanidines by reaction with O-methylisourea. Guanidinylated polymers disrupted function of isolated mitochondria more than their lysine-based analogs, but overall toxicity was decreased, likely due to inefficient mitochondrial trafficking. Thus, while multivalent KLA polymers are more potent than KLA peptides, these materials can be substantially improved by designing next generation materials with improved

  17. Chemical and enzymatic reductive activation of acylfulvene to isomeric cytotoxic reactive intermediates

    OpenAIRE

    Pietsch, Kathryn E.; Neels, James F.; Yu, Xiang; Gong, Jiachang; Sturla, Shana J.

    2011-01-01

    Acylfulvenes, a class of semisynthetic analogues of the sesquiterpene natural product illudin S, are cytotoxic towards cancer cells. The minor structural changes between illudin S and AFs translate to an improved therapeutic window in preclinical cell-based assays and xenograft models. AFs are, therefore, unique tools for addressing the chemical and biochemical basis of cytotoxic selectivity. AFs elicit cytotoxic responses by alkylation of biological targets, including DNA. While AFs are capa...

  18. Composition of essential oil from Tagetes minuta and its cytotoxic, antioxidant and antimicrobial activities.

    Science.gov (United States)

    Ali, Nasser A Awadh; Sharopov, Farukh S; Al-Kaf, Ali G; Hill, Gabrielle M; Arnold, Norbert; Al-Sokari, Saeed S; Setzer, William N; Wessjohann, Ludger

    2014-02-01

    The essential oil from the leaves of Tagetes minuta L., growing wild in Yemen, was obtained by hydrodistillation and analyzed by gas chromatography-mass spectrometry. A total of 28 compounds were identified representing 74.2% of total oil composition. Major components of the essential oil were (Z)-ocimenone (15.9%), (E)-ocimenone (34.8%), (Z)-beta-ocimene (8.3%), limonene (2.3%), (Z)-tagetone (1.8%), dihydrotagetone (1.4%) and an unidentified dimethylvinylketone derivative (20.6%). The oil showed moderate cytotoxic activity against MCF-7 breast tumor cells, with an IC50 of 54.7 +/- 6.2 microg/mL. In the DPPH radical scavenging assay, T. minuta oil showed potent antiradical activity with an IC50 value of 36 microg/mL. Antimicrobial activity was also investigated on several microorganisms, and the essential oil exhibited high activity against methicillin-resistant Staphylococcus aureus (MRSA) with an inhibition zone of 23 mm. It also exhibited remarkable antifungal activity against Candida albicans with an inhibition zone of 26 mm.

  19. Quantitative Structure-Activity Relationship Analysis of Xanthone Derivates as Cytotoxic Agents in Liver Cancer Cell Line HepG2

    OpenAIRE

    Isnatin Miladiyah; Iqmal Tahir; Jumina Jumina; Sofia Mubarika; Mustofa Mustofa

    2016-01-01

    The study of xanthone derivatives as cytotoxic agents in cancer is increasing. This study was conducted to explore the Quantitative Structure-Activity Relationship (QSAR) of xanthones as cytotoxic agents in HepG2 cells, to find compounds with better potency. The data set were taken from the previous study, involving 26 xanthone derivates and their cytotoxic activities in Inhibitory Concentration 50% (IC50). The parameters (descriptors) were obtained from quantum mechanics calculation using se...

  20. Expression of JAK3 Sensitive Na+ Coupled Glucose Carrier SGLT1 in Activated Cytotoxic T Lymphocytes

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    Shefalee K. Bhavsar

    2016-09-01

    Full Text Available Background: Similar to tumor cells, activated T-lymphocytes generate ATP mainly by glycolytic degradation of glucose. Lymphocyte glucose uptake involves non-concentrative glucose carriers of the GLUT family. In contrast to GLUT isoforms, Na+-coupled glucose-carrier SGLT1 accumulates glucose against glucose gradients and is effective at low extracellular glucose concentrations. The present study explored expression and regulation of SGLT1 in activated murine splenic cytotoxic T cells (CTLs and human Jurkat T cells. Methods: FACS analysis, immunofluorescence, confocal microscopy, chemiluminescence and Western blotting were employed to estimate SGLT1 expression, function and regulation in lymphocytes, as well as dual electrode voltage clamp in SGLT1 ± JAK3 expressing Xenopus oocytes to quantify the effect of janus kinase3 (JAK3 on SGLT1 function. Results: SGLT1 is expressed in murine CTLs and also in human Jurkat T cells. 2-(N-(7-nitrobenz-2-oxa-1,3-diazol-4-ylamino-2-deoxyglucose uptake was significantly decreased by SGLT1-blocker phloridzin (0.2 mM and by pharmacological inhibition of JAK3 with WHI-P131 (156 µM, WHI-P154 (11.2 µM and JAK3 inhibitor VI (0.5 µM. Electrogenic glucose transport (Iglucose in Xenopus oocytes expressing human SGLT1 was increased by additional expression of human wild type JAK3, active A568VJAK3 but not inactive K851AJAK3. Coexpression of JAK3 enhanced the maximal transport rate without significantly modifying affinity of the carrier. Iglucose in SGLT1+JAK3 expressing oocytes was significantly decreased by WHI-P154 (11.2 µM. JAK3 increased the SGLT1 protein abundance in the cell membrane. Inhibition of carrier insertion by brefeldin A (5 µM in SGLT1+JAK3 expressing oocytes resulted in a decline of Iglucose, which was similar in presence and absence of JAK3. Conclusions: SGLT1 is expressed in murine cytotoxic T cells and human Jurkat T cells and significantly contributes to glucose uptake in those cells post

  1. NC10 bacteria in marine oxygen minimum zones

    DEFF Research Database (Denmark)

    Padilla, Cory C; Bristow, Laura A; Sarode, Neha

    2016-01-01

    Bacteria of the NC10 phylum link anaerobic methane oxidation to nitrite denitrification through a unique O2-producing intra-aerobic methanotrophy pathway. A niche for NC10 in the pelagic ocean has not been confirmed. We show that NC10 bacteria are present and transcriptionally active in oceanic....... rRNA and mRNA transcripts assignable to NC10 peaked within the OMZ and included genes of the putative nitrite-dependent intra-aerobic pathway, with high representation of transcripts containing the unique motif structure of the nitric oxide (NO) reductase of NC10 bacteria, hypothesized...

  2. Antioxidant, Cytotoxic, and Toxic Activities of Propolis from Two Native Bees in Brazil: Scaptotrigona depilis and Melipona quadrifasciata anthidioides.

    Science.gov (United States)

    Bonamigo, Thaliny; Campos, Jaqueline Ferreira; Alfredo, Tamaeh Monteiro; Balestieri, José Benedito Perrella; Cardoso, Claudia Andrea Lima; Paredes-Gamero, Edgar Julian; de Picoli Souza, Kely; Dos Santos, Edson Lucas

    2017-01-01

    Propolis is a natural mixture of compounds produced by various bee species, including stingless bees. This compound has been shown to exhibit antioxidant, antiproliferative, and antitumor activities. The present study aimed to determine the chemical constituents as well as the antioxidant, cytotoxic, and toxic activities of ethanol extracts of propolis obtained from the stingless bees Scaptotrigona depilis and Melipona quadrifasciata anthidioides, which are found in Brazil. Phytosterols, terpenes, phenolic compounds, and tocopherol were identified in the ethanol extracts of propolis (EEPs) in different concentrations. The compounds stigmasterol, taraxasterol, vanilic acid, caffeic acid, quercetin, luteolin, and apigenin were found only in EEP-M. The EEPs were able to scavenge the free radicals 2,2-diphenyl-1-picrylhydrazyl and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) and protected human erythrocytes against lipid peroxidation, with the latter effect being demonstrated by their antihemolytic activity and inhibition of malondialdehyde formation. The EEPs showed cytotoxic activity against erythroleukemic cells and necrosis was the main mechanism of death observed. In addition, the concentrations at which the EEPs were cytotoxic were not toxic against Caenorhabditis elegans. In this context, it is concluded that EEP-S and EEP-M show antioxidant and cytotoxic activities and are promising bioactive mixtures for the control of diseases associated with oxidative stress and tumor cell proliferation.

  3. Antioxidant, Cytotoxic, and Toxic Activities of Propolis from Two Native Bees in Brazil: Scaptotrigona depilis and Melipona quadrifasciata anthidioides

    Directory of Open Access Journals (Sweden)

    Thaliny Bonamigo

    2017-01-01

    Full Text Available Propolis is a natural mixture of compounds produced by various bee species, including stingless bees. This compound has been shown to exhibit antioxidant, antiproliferative, and antitumor activities. The present study aimed to determine the chemical constituents as well as the antioxidant, cytotoxic, and toxic activities of ethanol extracts of propolis obtained from the stingless bees Scaptotrigona depilis and Melipona quadrifasciata anthidioides, which are found in Brazil. Phytosterols, terpenes, phenolic compounds, and tocopherol were identified in the ethanol extracts of propolis (EEPs in different concentrations. The compounds stigmasterol, taraxasterol, vanilic acid, caffeic acid, quercetin, luteolin, and apigenin were found only in EEP-M. The EEPs were able to scavenge the free radicals 2,2-diphenyl-1-picrylhydrazyl and 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid and protected human erythrocytes against lipid peroxidation, with the latter effect being demonstrated by their antihemolytic activity and inhibition of malondialdehyde formation. The EEPs showed cytotoxic activity against erythroleukemic cells and necrosis was the main mechanism of death observed. In addition, the concentrations at which the EEPs were cytotoxic were not toxic against Caenorhabditis elegans. In this context, it is concluded that EEP-S and EEP-M show antioxidant and cytotoxic activities and are promising bioactive mixtures for the control of diseases associated with oxidative stress and tumor cell proliferation.

  4. Cytotoxic activity of metformin in vitro does not correlate with its antitumor action in vivo.

    Science.gov (United States)

    Pyaskovskaya, O N; Kolesnik, D L; Fedorchuk, A G; Gorbik, G V; Solyanik, G I

    2017-12-01

    It is known that metformin is a hypoglycemic drug used to treat type II diabetes mellitus. Recently active studies of its antitumor activity in relation to different types of malignant cells are conducted. To determine the relationship between cytotoxic activity of metformin in vitro and its antitumor activity in vivo. The rat C6 glioma cell line and mouse Lewis lung carcinoma cells (LLC) were used in this work. The number of living cells in the cytotoxic test was evaluated using sulforhodamine B. Parameters of tumor cell susceptibility to metformin activity in vitro were calculated using nonlinear and linear regression of experimental data. The antitumor action of metformin in vivo was evaluated routinely by the extension of survival time (ST) (in rats with intracerebral C6 glioma) and its effect on the volume of the primary tumor, the number and volume of metastases (in mice with LLC). In cultured LLC cells in vitro, the proportions of metformin-resistant (A1, %) and metformin-sensitive (A2, %) subpopulations were 10.0 ± 2.2% and 92.0 ± 3.5%, respectively, in terms of the total number of living cells. Parameter t, which characterizes the sensitivity of cancer cells to metformin action (the lower is the value of this parameter the higher is sensitivity of cells to metformin cytotoxicity), for metformin-resistant and metformin-sensitive subpopulations was: t1(mM) = ∞ and t2(mM) = 2.9 ± 0.3, correspondingly. For metformin-sensitive subpopulation of LLC cells IC50 (mM) = 2.42 ± 0.34. The volume of the primary tumor, the amount and volume of metastases in mice receiving metformin at a dose of Dmin (0.15 g/kg) and Dmax (0.3 g/kg) values did not significantly differ from those in the control. However, in the case of Dmin, there was a tendency to increased volume of the primary tumor, in the case of Dmax, there was a tendency to increased volume of metastases. The analogical parameters (A1, A2, b1, b2, IC50 (1), IC50 (2)) characterizing cell sensitivity

  5. Antiproliferative, Cytotoxic, Antioxidant Activity and Polyphenols Contents in Leaves of Four Staphylea L. Species

    Directory of Open Access Journals (Sweden)

    Daniel Grancai

    2009-08-01

    Full Text Available Staphylea has been used for long time in Traditional Chinese Medicine (TCM and by Native Americans in a number of therapeutical indications. The present study describes in vitro antiproliferative, cytotoxic properties (MTT and LDH test and antioxidant activities (reduction of DPPH radical and peroxynitrite radical of Staphylea colchica Stev. (SC, S. elegans Zab. (SC, S. holocarpa Hemsl. (SH and S. pinnata L. (SP leave water extracts. Time- (24 and 72 h and dose- (1-150 μg/mL dependent effects of the above extracts were tested at the mitochondrial (MTT test and plasma membrane level (LDH leakage in A431 human skin carcinoma cells. Screening of these properties has shown time and dose dependent increase of harmful effects, the highest activity was observed for the SE, while the less active was the SH extract. The ED50 values for the mitochondrial and membrane damage were nearly identical for the SE and very similar for SH extract. These findings indicate simultaneous injury of both cell compartments by SE and SH extracts. The highest antioxidant potential of SE species is accompanied by the highest content of flavones/flavonols and polyphenols. Only flavonoid contents are associated with antiproliferative effects and cell membrane injury, while antioxidant properties are the result of polyphenol content. The data clearly demonstrate that individual Staphylea L. species differ, not only in the amount of biologically active compounds, but also by the extent of harmful and beneficial effects.

  6. Antiplasmodial activity and cytotoxicity of ethanol extract of Zea mays root.

    Science.gov (United States)

    Okokon, Jude Efiom; Antia, Bassey Sunday; Azare, Bala Adamu; Okokon, Patience Jude

    2017-01-01

    Zea mays root decoction that has been traditionally used for the treatment of malaria by various tribes in Nigeria, was evaluated for antimalarial potential against malaria parasites using in vivo and in vitro models. The root extract of Zea mays was investigated for antimalarial activity against Plasmodium berghei in mice using rodent malaria models; suppressive, prophylactic and curative tests and in vitro antiplasmodial activity against chloroquine-sensitive (Pf 3D7) and resistant (Pf INDO) strains of Plasmodium falciparum using SYBR green assay method. Median lethal dose and cytotoxic activity against HeLa and HEKS cells were assessed and phytochemical screening was also carried out using standard procedures. The LD50 value of root extract was found to be 474.34 mg/kg. The crude extract (45-135 mg/kg, p.o) showed significant (p100 μg/ml against both HeLa and HEKS cell lines. These results suggest that the root extract of Zea mays possesses antimalarial activity against both chloroquine-sensitive and resistant malaria and these data justify its use in ethnomedicine to treat malaria infections.

  7. Cytotoxic activity of phenolic constituents from Echinochloa crus-galli against four human cancer cell lines

    Directory of Open Access Journals (Sweden)

    Sayed Gad El Molla

    Full Text Available Abstract Echinochloa crus-galli (L. P. Beauv., Poaceae, grains are used as a feed for birds and millet for humans. The sulforhodamine B assay was used to assess its cytotoxicity against four human cancer cell lines. The ethanolic extract (70% proved to be most active against HCT-116 and HELA cell lines (IC50 = 11.2 ± 0.11 and 12.0 ± 0.11 µg/ml, respectively. On the other hand, the chloroform and ethyl acetate fractions exhibited their highest activities against HCT-116 cell lines. The chloroform and ethyl acetate fractions were subjected to several chromatographic separations to render pure phenolic compounds (1-8. Compounds 1-8 were identified as: 5,7-dihydroxy-3′,4′,5′-trimethoxy flavone, 5,7,4′-trihydroxy-3′,5′-dimethoxy flavone (tricin, quercetin, flavone, apigenin-8-C-sophoroside, 2-methoxy-4-hydroxy cinnamic acid, p-coumaric acid and quercetin-3-O-glucoside. All the isolated phenolic compounds exhibited various significant activities against the four human carcinoma where the methoxylated flavones (1 and 2 were the most active, in a way comparable to the anticancer drug Doxorubicin®. Thus, these methoxylated flavonoids may be considered as lead compounds for the treatment of cancer, which supports previous claims of E. crus-galli traditional use. This is the first report of the occurrence of these phenolic compounds in E. crus-galli.

  8. Antiplasmodial activity and cytotoxicity of ethanol extract of Zea mays root

    Science.gov (United States)

    Okokon, Jude Efiom; Antia, Bassey Sunday; Azare, Bala Adamu; Okokon, Patience Jude

    2017-01-01

    Objective: Zea mays root decoction that has been traditionally used for the treatment of malaria by various tribes in Nigeria, was evaluated for antimalarial potential against malaria parasites using in vivo and in vitro models. Materials and Methods: The root extract of Zea mays was investigated for antimalarial activity against Plasmodium berghei in mice using rodent malaria models; suppressive, prophylactic and curative tests and in vitro antiplasmodial activity against chloroquine-sensitive (Pf 3D7) and resistant (Pf INDO) strains of Plasmodium falciparum using SYBR green assay method. Median lethal dose and cytotoxic activity against HeLa and HEKS cells were assessed and phytochemical screening was also carried out using standard procedures. Results: The LD50 value of root extract was found to be 474.34 mg/kg. The crude extract (45-135 mg/kg, p.o) showed significant (p100 μg/ml against both HeLa and HEKS cell lines. Conclusion: These results suggest that the root extract of Zea mays possesses antimalarial activity against both chloroquine-sensitive and resistant malaria and these data justify its use in ethnomedicine to treat malaria infections. PMID:28748174

  9. Antiplasmodial activity and cytotoxicity of ethanol extract of Zea mays root

    Directory of Open Access Journals (Sweden)

    Jude Efiom Okokon

    2017-04-01

    Full Text Available Objective:Zea mays root decoction that has been traditionally used for the treatment of malaria by various tribes in Nigeria, was evaluated for antimalarial potential against malaria parasites using in vivo and in vitro models. Materials and Methods: The root extract of Zea mays was investigated for antimalarial activity against Plasmodium berghei in mice using rodent malaria models; suppressive, prophylactic and curative tests and in vitro antiplasmodial activity against chloroquine-sensitive (Pf 3D7 and resistant (Pf INDO strains of Plasmodium falciparum using SYBR green assay method. Median lethal dose and cytotoxic activity against HeLa and HEKS cells were assessed and phytochemical screening was also carried out using standard procedures. Results: The LD50 value of root extract was found to be 474.34 mg/kg. The crude extract (45-135 mg/kg, p.o showed significant (p100 μg/ml against both HeLa and HEKS cell lines. Conclusion: These results suggest that the root extract of Zea mays possesses antimalarial activity against both chloroquine-sensitive and resistant malaria and these data justify its use in ethnomedicine to treat malaria infections.

  10. INHIBITION OF THE NKG2D ACTIVATING RECEPTOR EXPRESSION ON CYTOTOXIC LYMPHOCYTES BY RECOMBINANT MICA PROTEIN

    Directory of Open Access Journals (Sweden)

    E. V. Abakushina

    2017-01-01

    Full Text Available Genome instability of transformed cells, being the most common factor of malignancy, may result into production of abnormal proteins in these cells. Normally, the newly formed proteins are recognized by immune system, thus causing elimination of the transformed cells. Nevertheless, the phenotypic instability promotes formation of specific transformed cells which suppress effector immune reactions and/or are unrecognizable by cytotoxic lymphocytes. NKG2D is one of the most important activating receptors expressed by NK cells. It serves as a major recognition receptor for detection and elimination of tumor and infected cells. The ligands for NKG2D include surface or circulating non-canonical MICA/B molecules from class I major histocompatibility complex (MHC class I chain–related proteins A and B. MICA and MICB are expressed scarcely, if at all, by the most normal cells, being, however, upregulated in cancer cells and virus-infected cells.NKG2D receptor-ligand interaction is important for regulation of anti-tumor immune reactions. The soluble form of MICA accumulated in blood due to proteolytic shedding from tumor cell membranes is able to inhibit the NKG2D mediated anti-tumor cytotoxicyty and, therefore, promote the immune escape. The aim of our study was to estimate blocking effects of soluble recombinant human MICA protein (rhsMICA upon NKG2D receptor of NK cells.Mononuclear cells were isolated from peripheral blood, followed by incubation with of rhsMICA at different concentrations (0, 1, 5, or 10 µg/ml, staining with anti-CD314 (NKG2D mAbs on the CD3- CD56+NK cells, and flow cytometry analysis. A similar treatment protocol was applied for IL2- and IL15-activated mononuclear cells isolated from the melanoma patients.It has been shown that brief incubation of lymphocytes with rhsMICA caused a significantly reduced expression of NKG2D receptor on the surface of cytotoxic lymphocytes, both from healthy donors and melanoma patients. These

  11. A cytotoxic type-2 ribosome inactivating protein (from leafless mistletoe) lacking sugar binding activity.

    Science.gov (United States)

    Das, Mrinal Kumar; Sharma, Radhey Shyam; Mishra, Vandana

    2011-12-01

    Articulatin-D, a 66 kDa ribosome inactivating protein (RIP) comprised of 29 kDa A-chain linked to 35 kDa B-chain, is purified from leafless mistletoe (Viscum articulatum) parasitic on Dalbergia sp. from Western Ghats (India). N-terminal sequence and LC-MS/MS analyses of A- and B-chain confirmed that articulatin-D is a type-2 RIP having high homology with other mistletoe lectins. Translation inhibition and diagnostic N-glycosidase activity of articulatin-D illustrate the presence of catalytically active A-chain. Its inability to: (i) bind to acid treated Sepharose CL-6B column, (ii) agglutinate trypsin-treated and untreated RBCs of human (A, B, O, AB), mice, rat, rabbit, buffalo, porcine, pigeon, cock, fish, sheep and goat even with 10mg/ml of purified articulatin-D, (iii) show change in circular dichroism spectra after addition of sugar to the native protein, (iv) bind to different sugars (galactose, lactose, gal-NAc, rhamnose, arabinose, fucose and mannose) immobilized on Sepharose 4B matrix, and (v) show change in enthalpy during titration with galactose confirm that the B-chain of articulatin-D lacks sugar binding activity. Despite this, articulatin-D is highly toxic as characterized with low IC(50) against different cancer cell lines (Jurkat: 0.31 ± 0.02 nM, MOLT-4: 0.51 ± 0.03 nM, U-937: 0.64 ± 0.07 nM, HL-60: 0.79 ± 0.11 nM, Raji: 1.45 ± 0.09 nM). Toxicity of RIPs has been ascribed to the absence/presence of B-chain with sugar binding activity. Identification of articulatin-D, the first cytotoxic RIP with B-chain lacking sugar binding activity opens new vistas in understanding cytotoxic action of RIPs. Copyright © 2011 Elsevier B.V. All rights reserved.

  12. Synthesis, molecular structure, spectral analysis and cytotoxic activity of two new aroylhydrazones

    Science.gov (United States)

    Singh, Ravindra Kumar; Singh, Ashok Kumar; Siddiqui, Sahabjada; Arshad, Mohammad; Jafri, Asif

    2017-05-01

    Two new aroylhydrazones viz 4-nitro-N‧-(1-(pyridin-2-yl)ethylidene)benzohydrazide, NPHY (4) and 4-nitro-N‧-(1-(thiophen-2-yl)ethylidene)benzohydrazide, NPHT (5) have been prepared and characterized by 1H NMR, 13C NMR, FT-IR, UV-Visible spectroscopy and mass spectrometry. All quantum calculations were performed at DFT level of theory using B3LYP functional and 6-31G (d,p) as basis set. TD-DFT calculated electronic transitions are found to be in good agreement with experimental findings. The assignments for normal vibrational modes have been done by computing Potential Energy Distribution (PED) using Gar2ped. HOMO-LUMO analysis was performed and reactivity descriptors were also computed. Global electrophilicity index (ω) of 6.12-6.26 eV shows these aroylhydrazones to be strong electrophiles. Intramolecular interactions were analyzed by 'Atoms in molecule' (AIM) approach. Also, the computed first static hyperpolarizabilities (β0) of these hydrazones indicate their future application as an attractive non-linear optical (NLO) material. Cytotoxicity evaluated by MTT assay, suggested that the synthesized aroylhydrazones significantly reduce the cell viability of breast cancer cell lines (MCF7) and human prostate adenocarcinoma (DU145) in a dose dependent manner. Cytotoxic potencies (IC50) of these hydrazones against MCF7 and DU145 cell lines were found in range of 54.67-85.67 μM. The result of ROS activity provides supportive data for molecular mechanism of these hydrazones, which is related to apoptotic cellular death. Nuclear condensation assay performed by DAPI staining shows fragmented and condensed nuclei in MCF7 cells, suggesting cell death by apoptosis.

  13. Chemical constituents from Sonneratia ovata Backer and their in vitro cytotoxicity and acetylcholinesterase inhibitory activities.

    Science.gov (United States)

    Nguyen, Thi-Hoai-Thu; Pham, Huu-Viet-Thong; Pham, Nguyen-Kim-Tuyen; Quach, Ngo-Diem-Phuong; Pudhom, Khanitha; Hansen, Poul Erik; Nguyen, Kim-Phi-Phung

    2015-06-01

    Sonneratia ovata Backer, Sonneratiaceae, is a widespread plant in mangrove forests in Vietnam, Cambodia, Thailand, Indonesia. Sonneratia ovata's chemical composition remains mostly unknown. Therefore, we now report on the structural elucidation of three new phenolics, sonnerphenolic A (1), sonnerphenolic B (2), and sonnerphenolic C (23), a new cerebroside, sonnercerebroside (3) together with nineteen known compounds, including nine lignans (5-13), two steroids (14, 15), two triterpenoids (16, 17), three gallic acid derivatives (18-20), two phenolic derivatives (4, 22) and a 1-O-benzyl-β-d-glucopyranose (21) isolated from the leaves of Sonneratia ovata. Their chemical structures were established by spectroscopic data, as well as high resolution mass spectra and comparison with literature data. The in vitro acetylcholinesterase (AChE) inhibition and cytotoxic activities against HeLa (human epithelial carcinoma), NCI-H460 (human lung cancer), MCF-7 (human breast cancer) cancer cell lines and PHF (primary human fibroblast) cell were evaluated on some extracts and purified compounds at a concentration of 100 μg/mL. Compounds (5, 6, 23) exhibited cytotoxicity against the MCF-7 cell line with the IC50 values of 146.9±9.0, 114.5±7.2, and 112.8±9.4 μM, respectively, while they showed nontoxic with the normal cell (PHF) with IC50s >277 μM. Among 15 tested compounds, (S)-rhodolatouchol (22) showed inhibition against AChE with an IC50 value of 96.1±14.5 μM. Copyright © 2015 Elsevier Ltd. All rights reserved.

  14. Antimicrobial and Cytotoxic Activity of Cuminum Cyminum as an Intracanal Medicament Compared to Chlorhexidine Gel.

    Science.gov (United States)

    Abbaszadegan, Abbas; Gholami, Ahmad; Ghahramani, Yasamin; Ghareghan, Razieh; Ghareghan, Marzieh; Kazemi, Aboozar; Iraji, Aida; Ghasemi, Younes

    2016-01-01

    The aims of this study were i) to define the chemical constituents of Cuminum cyminum (cumin) essential oil, ii) to compare the antimicrobial activity of this oil to that of chlorhexidine (CHX) and co-trimoxazole on planktonic and biofilm forms of bacteria isolated from the teeth with persistent endodontic infection and iii ) to compare the cytotoxicity of these medicaments on L929 fibroblasts. Three groups of microorganisms [aerobic bacterial mixture, anaerobic bacterial mixture and Enterococcus faecalis (E .faecalis)] were isolated from the teeth with persistent apical periodontitis. Zone of inhibition (ZOI), minimum inhibitory concentration (MIC), minimum bactericidal concentration (MBC), minimum biofilm inhibitory concentration (MBIC) and time-kill tests were performed to assess the antimicrobial efficacy of the medicaments. Further, a cytocompatibility analysis of the medicaments was performed on L929 fibroblasts. The results obtained from disc diffusion test and mean cell viability values of the experimental medicaments were analyzed using two-way and one-way analysis of variance (ANOVA). Seventeen constituents were recognized in cumin oil (predominantly cumin aldehyde and γ-terpinene). Co-trimoxazole showed the greatest ZOI followed by cumin and CHX. The smallest MIC and MBC belonged to co-trimoxazole followed by cumin and CHX for all groups of bacteria except for E. faecalis for which the MBC of cumin was smaller than co-trimoxazole. The results of time-kill assay revealed that all medicaments totally inhibited the bacterial growth in all groups after 24 h. CHX was the most cytotoxic solution while there were no significant differences between the cytocompatibility of different concentrations of cumin essential oil and co-trimoxazole. Cumin exhibited a strong antimicrobial efficiency against the microbial flora of the teeth with failed endodontic treatments and it was biocompatible for L929 mouse fibroblasts.

  15. Synthesis of 4-aminoantipyrine derived Schiff bases and their evaluation for antibacterial, cytotoxic and free radical scavenging activity

    Directory of Open Access Journals (Sweden)

    Mohammad Shoaib

    2015-06-01

    Full Text Available The work was aimed to synthesize 4-Aminoantipyrine derived Schiff bases in economical way and to screen it for study the effect of nitro group on its antibacterial potential, conduct antitumor preliminary study, the effects of group presence in benzylidene phenyl ring on the cytotoxic potentials and study the effects of electron withdrawing and donating group on antioxidant potential. We used green method with 75% reduction in general synthesis time of Schiff bases. Synthesized compound possess antibacterial potentials and nitro group presence enhances this potential. G2, G3, G4, G5, G6, G7 and G8 have significant cytotoxic and no significant antioxidant activity.

  16. Concanavalin A-induced activation of lymphocytic choriomeningitis virus memory lymphocytes into specifically cytotoxic T cells

    DEFF Research Database (Denmark)

    Marker, O; Thomsen, Allan Randrup; Andersen, G T

    1977-01-01

    When spleen cells, which have been primed to Lymphocytic Choriomeningitis (LCM) virus during a primary infection several months previously, are stimulated in vitro with Con A. highly specific secondary cytotoxic effector cells are generated. The degree of cytotoxicity revealed by such Con A...

  17. 5,6-Dihydropyrrolo[2,1-a]isoquinolines as Alternative of New Drugs with Cytotoxic Activity

    Czech Academy of Sciences Publication Activity Database

    Chávez-Santos, R. M.; Reyes Gutierrez, Paul Eduardo; Torres-Ochoa, R. O.; Ramírez-Apan, M. T.; Martínez, R.

    2017-01-01

    Roč. 65, č. 10 (2017), s. 973-981 ISSN 0009-2363 Institutional support: RVO:61388963 Keywords : pyrrolo[2,1-a]isoquinoline * synthesis * cytotoxic activity Subject RIV: CC - Organic Chemistry Impact factor: 1.133, year: 2016 https://www.jstage.jst.go.jp/article/cpb/65/10/65_c17-00409/_html/-char/en

  18. LC–MS characterization, anti-kinetoplastide and cytotoxic activities of natural products from Eugenia jambolana Lam. and Eugenia uniflora

    Directory of Open Access Journals (Sweden)

    Celestina Elba Sobral de Souza

    2017-09-01

    Conclusions: The species E. jambolana and E. uniflora presented antiparasitic activity against all tested parasite strains, indicating that these species can serve as an alternative therapy as they were efficient in the tests performed. The E. uniflora extract and the E. jambolana flavonoid fraction presented a low cytotoxicity, opening the floor for new biological studies.

  19. Cytotoxic and cell transforming activities of the fungicide methyl thiophanate on BALB/c 3T3 cells in vitro.

    Science.gov (United States)

    Perocco, P; Del Ciello, C; Mazzullo, M; Rocchi, P; Ferreri, A M; Paolini, M; Pozzetti, L; Cantelli-Forti, G

    1997-11-27

    Cytotoxic and cell-transforming activities of methyl thiophanate a systemic fungicide capable of entering plant cells and thus controlling fungal diseases that have already started were studied in an in vitro medium-term (6-8 weeks) experimental model utilizing BALB/c 3T3 cells. Cells were exposed to the chemical, dissolved in dimethyl sulfoxide, in the absence or presence of an exogenous metabolizing system derived from rat livers supplemented with cofactors (S9 mix). In the absence of metabolic activation, methyl thiophanate exerted cytotoxic activity, evidenced through the formation of cell colonies, at low doses (> 10 micrograms/ml). However, the cytotoxic activity was greatly reduced by the S9 mix-induced metabolic activation of the chemical. Without bioactivation, cell-transforming potential, evidenced through the induction of transformation foci, was observable only at the highest (weakly toxic) dose employed (25 micrograms/ml). On the contrary, in the presence of metabolic activation, the cell-transforming activity was detectable at all tested doses (i.e. from 20 to 200 micrograms/ml) and it was particularly evident in a level-II transformation amplification test when the cells were allowed to perform active proliferative activity. These results, providing further information on the activity of methyl thiophanate in multistep carcinogenesis as possible genotoxic and/or co-carcinogenic agent, may contribute to better evaluate the oncogenic risk to man.

  20. Limonoids from Azadirachta indica var. siamensis extracts and their cytotoxic and melanogenesis-inhibitory activities.

    Science.gov (United States)

    Manosroi, Aranya; Kitdamrongtham, Worapong; Ishii, Kenta; Shinozaki, Takuro; Tachi, Yosuke; Takagi, Mio; Ebina, Kodai; Zhang, Jie; Manosroi, Jiradej; Akihisa, Rima; Akihisa, Toshihiro

    2014-04-01

    Six new limonoids, 7-benzoyl-17-epinimbocinol (5), 3-acetyl-7-tigloylnimbidinin (8), 1-isovaleroyl-1-detigloylsalanninolide (15), 2,3-dihydro-3α-methoxynimbolide (16), deacetyl-20,21-epoxy-20,22-dihydro-21-deoxyisonimbinolide (26), and deacetyl-20,21,22,23-tetrahydro-20,22-dihydroxy-21,23-dimethoxynimbin (27), along with 28 known limonoids, 1-4, 6, 7, 9-14, 17-25, and 28-34, and two known flavonoids, 35 and 36, have been isolated from the extracts of bark, leaves, roots, and seeds of Azadirachta indica A. Juss. var. siamensis Valeton (Siamese neem tree; Meliaceae). The structures of the new compounds were elucidated on the basis of extensive spectroscopic analysis and comparison with literature data. All of these compounds were evaluated for their cytotoxic activities against leukemia (HL60), lung (A549), stomach (AZ521), and breast (SK-BR-3) cancer cell lines. Eleven compounds, 1, 2, 4-7, 13, 16, 17, 29, and 30, exhibited potent cytotoxicities against one or more cell lines with IC50 values in the range of 0.1-9.3 μM. Compound 16 induced apoptotic cell death in AZ521 cells upon evaluation of the apoptosis-inducing activity by flow cytometric analysis. Western blot analysis on AZ521 cells revealed that compound 16 activated caspases-3, -8, and -9, while increasing the ratio of Bax/Bcl-2. This suggested that 16 induced apoptosis via both mitochondrial and death receptor pathways in AZ521. In addition, upon evaluation of all compounds against the melanogenesis in B16 melanoma cells induced with α-melanocyte-stimulating hormone (α-MSH), 20 limonoids, i.e., 1-3, 6, 9-11, 18, 19, 21-29, 32, and 34, and two flavonoids, 35 and 36, exhibited melanogenesis-inhibitory activities, with no, or almost no, toxicities to the cells at lower and/or higher concentrations, which were more potent than the reference arbutin, a known melanogenesis inhibitor. Western blot analysis showed that nimbin (18) reduced the protein levels of microphtalmia-associated transcription factor

  1. Virus-specific cytotoxic T cells in chronic active Epstein-Barr virus infection.

    Science.gov (United States)

    Shibayama, Haruna; Imadome, Ken-Ichi; Onozawa, Erika; Tsuzura, Akiho; Miura, Osamu; Koyama, Takatoshi; Arai, Ayako

    2017-01-01

    Chronic active Epstein-Barr virus infection (CAEBV) is a disease characterized by clonally proliferating and activated EBV-infected T or NK cells accompanied by chronic inflammation and T- or NK-cell neoplasms. However, the mechanism for developing CAEBV has not been clarified to date. Because the decreased number or inactivation of EBV-specific cytotoxic T lymphocytes (CTLs) resulted in the development of EBV-positive B-cell neoplasms, we investigated the number of CTLs in CAEBV patients using the tetrameric complexes of HLA-restricted EBV-specific peptides. Among the seven patients examined, EBV-specific CTLs were detected in the peripheral blood mononuclear cells (PBMCs) of four cases but were not detected in three cases. The ratio of EBV-specific CTLs in PBMCs tended to be higher in the patients with active disease than in those with inactive disease. In two patients in whom EBV-specific CTLs had not been detected, CTLs appeared after the eradication of EBV-infected T cells by allogeneic bone marrow transplantation. These results suggested that the failure of CTLs had a role in developing CAEBV, although the induction number and function of EBV-specific CTLs might vary in each patient.

  2. Antibacterial and Cytotoxic Activities of Diterpenoids Isolated from Indian Plectranthus coesta

    Directory of Open Access Journals (Sweden)

    Shobha Waldia

    2013-08-01

    Full Text Available Plectranthus is known for its medicinal value . The paper describes the antibacterial and cytotoxic activity of diterpenoids ent -7-hydroxykaur-15,16-en-19-oic acid (1, 17-oxokaur-15,16-en-19-oic acid (2 and ent-7-hydroxy-15,16-epoxykauran-19-oic acid (3, isolated from the shade-dried and powdered leaves of Indian Plactranthus coesta. Diterpenoid 3 was isolated for the first time from Indian P. coesta . Diterpenoid 1, shows potent activity against E. coli (15.6 µg/mL, P. aureginosa (17 µg/mL and K. planticola (32.5 µg/mL, while diterpenoid 2, also showed good activity against E. coli (61 µg/mL, P. aureginosa (61 µg/mL, K. planticola (61 µg/mL and S. epidermidis (125 µg/mL. Diterpenoids 1-3 were found to be more efficacious on U87 cancer cells and less toxic on normal human HEK and HeLa cells.

  3. Carbohydrate-conjugate heterobimetallic complexes: synthesis, DNA binding studies, artificial nuclease activity and in vitro cytotoxicity.

    Science.gov (United States)

    Tabassum, Sartaj; Khan, Rais Ahmad; Arjmand, Farukh; Aziz, Mubashira; Juvekar, Aarti S; Zingde, Surekha M

    2011-12-27

    New carbohydrate-conjugated heterobimetallic complexes [C(32)H(62)N(10)O(8)NiSn(2)Cl(4)]Cl(2)(1) and [C(32)H(62)N(10)O(8)CuSn(2)Cl(4)]Cl(2) (2) were synthesized and characterized by spectroscopic (IR, (1)H, (13)C, and (119)Sn NMR, EPR, UV-vis, ESI-MS) and analytical methods. The interaction studies of 2 with CT DNA were studied by using various biophysical techniques, which showed high binding affinity of 2 toward CT DNA. The extent of interaction was further confirmed by the interaction of 2 with the nucleotides viz.; 5'-AMP, 5'-CMP, 5'-GMP, and 5'-TMP, by absorption titration. (1)H, (31)P, (119)Sn NMR spectroscopy further validated the interaction mode of 2 with 5'-GMP. The electrophoresis pattern observed for 2 with supercoiled pBR322 DNA, exhibited significantly good nuclease activity following oxidative pathway. The preferential selectivity of 2 toward the major groove was observed on interaction of 2 with pBR322 DNA, in the presence of standard groove binders viz.; DAPI and methyl green. Additionally, in vitro antitumor activity of 2 was evaluated on a panel of human cancer cell lines, exhibiting remarkable cytotoxicity activity against Colo205 (colon) and MCF7 (breast) cell lines with GI(50) values <10 μg/mL. Copyright © 2011 Elsevier Ltd. All rights reserved.

  4. Regioselective synthesis and preliminary cytotoxic activity properties of tetrazole appendage N-substituted piperazine derivatives

    Directory of Open Access Journals (Sweden)

    Kommula Dileep

    2017-08-01

    Full Text Available A series of 1-(4-substituted-4-(3-((1-(substituted-1H-tetrazol-5-ylthiopropylpiperazine derivatives were ( 6a-t synthesized by KF-Al2O3 mediated S-alkylation of 5-thio-substituted tetrazole with 1-(3-chloropropyl-4-(4-substitutedpiperazine. The structures of the newly synthesized compounds were characterized by NMR and MS spectral data. Further, the regioselective formation of C-S bond was unambiguously confirmed by single crystal X- ray diffraction. All the synthesized compounds were screened for their in vitro cytotoxic activities against two cancer cell lines: DU-145 (prostate cancer and HeLa (cervical cancer. These cell lines were utilized in MTT assays and the obtained results were compared to doxorubicin, and their IC 50 values were determined. Among the compounds tested, 6f, 6j, 6m, 6n, 6o, 6q, 6r and 6t showed considerable potent activity, while the compound 6p exhibited significant potent activity against DU-145 and HeLa cancer cell lines compare to standard Doxorubicin.

  5. Phytochemicals from Kaempferia angustifolia Rosc. and Their Cytotoxic and Antimicrobial Activities

    Directory of Open Access Journals (Sweden)

    Sook Wah Tang

    2014-01-01

    Full Text Available Phytochemical investigation on rhizomes of Kaempferia angustifolia has afforded a new abietene diterpene, kaempfolienol (1 along with crotepoxide (2, boesenboxide (3, 2′-hydroxy-4,4′,6′-trimethoxychalcone (4, zeylenol (5, 6-methylzeylenol (6, (24S-24-methyl-5α-lanosta-9(11, 25-dien-3β-ol (7, sucrose, β-sitosterol, and its glycoside (8. The structures of the compounds were elucidated on the basis of spectroscopic methods (IR, MS, and NMR. Isolation of 6-methylzeylenol (6, (24S-24-methyl-5α-lanosta-9(11, 25-dien-3β-ol (7, and β-sitosterol-3-O-β-D-glucopyranoside (8 from this plant species has never been reported previously. The spectroscopic data of (7 is firstly described in this paper. Cytotoxic screening indicated that most of the pure compounds tested showed significant activity with (4 showing the most potent activity against HL-60 (human promyelocytic leukemia and MCF-7 (human breast cancer cell lines. However, all extracts and most of the pure compounds tested were found to be inactive against HT-29 (human colon cancer and HeLa (human cervical cancer cell lines. Similarly, none of the extracts or compounds showed activity in the antimicrobial testing.

  6. Phytochemicals from Kaempferia angustifolia Rosc. and their cytotoxic and antimicrobial activities.

    Science.gov (United States)

    Tang, Sook Wah; Sukari, Mohd Aspollah; Neoh, Bee Keat; Yeap, Yunie Soon Yu; Abdul, Ahmad Bustamam; Kifli, Nurolaini; Ee, Gwendoline Cheng Lian

    2014-01-01

    Phytochemical investigation on rhizomes of Kaempferia angustifolia has afforded a new abietene diterpene, kaempfolienol (1) along with crotepoxide (2), boesenboxide (3), 2'-hydroxy-4,4',6'-trimethoxychalcone (4), zeylenol (5), 6-methylzeylenol (6), (24S)-24-methyl-5α-lanosta-9(11), 25-dien-3β-ol (7), sucrose, β-sitosterol, and its glycoside (8). The structures of the compounds were elucidated on the basis of spectroscopic methods (IR, MS, and NMR). Isolation of 6-methylzeylenol (6), (24S)-24-methyl-5α-lanosta-9(11), 25-dien-3β-ol (7), and β-sitosterol-3-O-β-D-glucopyranoside (8) from this plant species has never been reported previously. The spectroscopic data of (7) is firstly described in this paper. Cytotoxic screening indicated that most of the pure compounds tested showed significant activity with (4) showing the most potent activity against HL-60 (human promyelocytic leukemia) and MCF-7 (human breast cancer) cell lines. However, all extracts and most of the pure compounds tested were found to be inactive against HT-29 (human colon cancer) and HeLa (human cervical cancer) cell lines. Similarly, none of the extracts or compounds showed activity in the antimicrobial testing.

  7. In vitro cytotoxic activity of chitosan-bullfrog oil microemulsion against melanoma cells.

    Science.gov (United States)

    Bonatto, Cínthia Caetano; Joanitti, Graziella Anselmo; Silva, Luciano Paulino

    2015-08-01

    Microemulsion-based animal oils, alone or associated with polymers have been extensively used in pharmacy, medicine and cosmetics, since the major lipid constituents of the oils show several biological activities. Despite showing antimicrobial activity, there are no reports in the literature regarding the effects of bullfrog oil on cytotoxic activity against tumor cells. The aim of the present study was to synthesize, characterise and evaluate the in vitro effects on melanoma cell line (B16F10) of bullfrog oil microemulsions associated or not with chitosan, surfactant and bullfrog oil (CSBO) and surfactant and bullfrog oil (SBO), respectively. The microemulsions were developed and their physical-chemical characteristics were evaluated by light microscopy, dynamic light scattering, atomic force microscopy and zeta potential. The microemulsions showed regular spherical shapes, high polydispersity and excellent (+82.2 ± 1.0 mV) to low (-16.0 ± 0.5 mV), colloidal stability. The systems significantly decreased the in vitro cell viability of melanoma skin cancer by up to 90.2% (CSBO) and 91.8% (SBO); while free bullfrog oil showed no effects. The results obtained from microemulsions of bullfrog oil indicate the potential of the microemulsions developed, alone or in combination with other chemotherapeutic agents, for future use in biomedical approaches aiming towards cancer therapy.

  8. Silver nanoparticles with antimicrobial activities against Streptococcus mutans and their cytotoxic effect.

    Science.gov (United States)

    Pérez-Díaz, Mario Alberto; Boegli, Laura; James, Garth; Velasquillo, Cristina; Sánchez-Sánchez, Roberto; Martínez-Martínez, Rita-Elizabeth; Martínez-Castañón, Gabriel Alejandro; Martinez-Gutierrez, Fidel

    2015-10-01

    Microbial resistance represents a challenge for the scientific community to develop new bioactive compounds. The goal of this research was to evaluate the antimicrobial activity of silver nanoparticles (AgNPs) against a clinical isolate of Streptococcus mutans, antibiofilm activity against mature S. mutans biofilms and the compatibility with human fibroblasts. The antimicrobial activity of AgNPs against the planktonic clinical isolate was size and concentration dependent, with smaller AgNPs having a lower minimum inhibitory concentration. A reduction of 2.3 log in the number of colony-forming units of S. mutans was observed when biofilms grown in a CDC reactor were exposed to 100 ppm of AgNPs of 9.5±1.1 nm. However, AgNPs at high concentrations (>10 ppm) showed a cytotoxic effect upon human dermal fibroblasts. AgNPs effectively inhibited the growth of a planktonic S. mutans clinical isolate and killed established S. mutans biofilms, which suggests that AgNPs could be used for prevention and treatment of dental caries. Further research and development are necessary to translate this technology into therapeutic and preventive strategies. Copyright © 2015 Elsevier B.V. All rights reserved.

  9. Acute toxicity, brine shrimp cytotoxicity and relaxant activity of fruits of callistemon citrinus curtis

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    Shah Ismail

    2011-10-01

    Full Text Available Abstract Background Callistemon citrinus Curtis belongs to family Myrtaceae that has a great medicinal importance. In our previous work, fruits of Callistemon citrinus were reported to have relaxant (antispasmodic activity. The current work describes the screening of fractions of the crude methanol extract for tracing spasmolytic constituents so that it shall help us for isolation of bioactive compounds. Acute toxicity and brine shrimp cytotoxicity of crude methanol extract are also performed to standardize it. Methods The crude methanol extract was obtained by maceration with distilled water (500 ml three times and fractionated successively with n-hexane, chloroform, ethyl acetate and n-butanol (300 ml of each solvent. Phytochemical analysis for crude methanol extract was performed. Acute toxicity studies were performed in mice. Brine shrimp cytotoxicity studies were performed to determine its cytotoxicity and standardize it. In other series of experiments, rabbits' jejunum preparations were used in screening for possible relaxant activities of various fractions. They were applied in concentrations of 0.01, 0.03, 0.1, 0.3, 1.0, 3.0, 5.0 and 10.0 mg/ml on spontaneous rabbits' jejunum preparations. In similar fashion, fractions were also tested on KCl (80 mM -induced contractions. Calcium chloride curves were constructed in K-rich Tyrode's solution. The effects of various fractions were tested on calcium chloride curves at concentrations 1.0, 3.0, 5.0 and 10.0 mg/ml. Curves of verapamil used as reference drug at concentration 0.1 μM and 0.3 μM were also constructed. The curves were compared with their respective controls for possible right shift. Results Methanol extract tested strongly positive for saponins and tannins. However, it tested mild positive for presence of proteins, amino acids, carbohydrates and phenolic compounds. LD50 value for crude methanol extract is 476.25 ± 10.3 (470-481, n = 4 mg/ml. Similarly, EC50 value for brine shrimp

  10. Acute toxicity, brine shrimp cytotoxicity and relaxant activity of fruits of callistemon citrinus curtis.

    Science.gov (United States)

    Ali, Niaz; Ahmed, Ghayour; Shah, Syed Wadood Ali; Shah, Ismail; Ghias, Mehreen; Khan, Imran

    2011-10-24

    Callistemon citrinus Curtis belongs to family Myrtaceae that has a great medicinal importance. In our previous work, fruits of Callistemon citrinus were reported to have relaxant (antispasmodic) activity. The current work describes the screening of fractions of the crude methanol extract for tracing spasmolytic constituents so that it shall help us for isolation of bioactive compounds. Acute toxicity and brine shrimp cytotoxicity of crude methanol extract are also performed to standardize it. The crude methanol extract was obtained by maceration with distilled water (500 ml) three times and fractionated successively with n-hexane, chloroform, ethyl acetate and n-butanol (300 ml of each solvent). Phytochemical analysis for crude methanol extract was performed. Acute toxicity studies were performed in mice. Brine shrimp cytotoxicity studies were performed to determine its cytotoxicity and standardize it. In other series of experiments, rabbits' jejunum preparations were used in screening for possible relaxant activities of various fractions. They were applied in concentrations of 0.01, 0.03, 0.1, 0.3, 1.0, 3.0, 5.0 and 10.0 mg/ml on spontaneous rabbits' jejunum preparations. In similar fashion, fractions were also tested on KCl (80 mM) -induced contractions. Calcium chloride curves were constructed in K-rich Tyrode's solution. The effects of various fractions were tested on calcium chloride curves at concentrations 1.0, 3.0, 5.0 and 10.0 mg/ml. Curves of verapamil used as reference drug at concentration 0.1 μM and 0.3 μM were also constructed. The curves were compared with their respective controls for possible right shift. Methanol extract tested strongly positive for saponins and tannins. However, it tested mild positive for presence of proteins, amino acids, carbohydrates and phenolic compounds. LD(50) value for crude methanol extract is 476.25 ± 10.3 (470-481, n = 4) mg/ml. Similarly, EC(50) value for brine shrimp cytotoxicity is 65.5 ± 7.28 (60.8- 69.4, n

  11. Acute toxicity, brine shrimp cytotoxicity and relaxant activity of fruits of callistemon citrinus curtis

    Science.gov (United States)

    2011-01-01

    Background Callistemon citrinus Curtis belongs to family Myrtaceae that has a great medicinal importance. In our previous work, fruits of Callistemon citrinus were reported to have relaxant (antispasmodic) activity. The current work describes the screening of fractions of the crude methanol extract for tracing spasmolytic constituents so that it shall help us for isolation of bioactive compounds. Acute toxicity and brine shrimp cytotoxicity of crude methanol extract are also performed to standardize it. Methods The crude methanol extract was obtained by maceration with distilled water (500 ml) three times and fractionated successively with n-hexane, chloroform, ethyl acetate and n-butanol (300 ml of each solvent). Phytochemical analysis for crude methanol extract was performed. Acute toxicity studies were performed in mice. Brine shrimp cytotoxicity studies were performed to determine its cytotoxicity and standardize it. In other series of experiments, rabbits' jejunum preparations were used in screening for possible relaxant activities of various fractions. They were applied in concentrations of 0.01, 0.03, 0.1, 0.3, 1.0, 3.0, 5.0 and 10.0 mg/ml on spontaneous rabbits' jejunum preparations. In similar fashion, fractions were also tested on KCl (80 mM) -induced contractions. Calcium chloride curves were constructed in K-rich Tyrode's solution. The effects of various fractions were tested on calcium chloride curves at concentrations 1.0, 3.0, 5.0 and 10.0 mg/ml. Curves of verapamil used as reference drug at concentration 0.1 μM and 0.3 μM were also constructed. The curves were compared with their respective controls for possible right shift. Results Methanol extract tested strongly positive for saponins and tannins. However, it tested mild positive for presence of proteins, amino acids, carbohydrates and phenolic compounds. LD50 value for crude methanol extract is 476.25 ± 10.3 (470-481, n = 4) mg/ml. Similarly, EC50 value for brine shrimp cytotoxicity is 65.5

  12. Antimicrobial, antioxidant, antitumour-promoting and cytotoxic activities of different plant part extracts of Garcinia atroviridis griff. ex T. anders.

    Science.gov (United States)

    Mackeen, M M; Ali, A M; Lajis, N H; Kawazu, K; Hassan, Z; Amran, M; Habsah, M; Mooi, L Y; Mohamed, S M

    2000-10-01

    Crude extracts (methanol) of various parts, viz. the leaves, fruits, roots, stem and trunk bark, of Garcinia atroviridis were screened for antimicrobial, cytotoxic, brine shrimp toxic, antitumour-promoting and antioxidant activities. The crude extracts exhibited predominantly antibacterial activity with the root extract showing the strongest inhibition against the test bacteria at a minimum inhibitory dose (MID) of 15.6 microg/disc. Although all the extracts failed to inhibit the growth of most of the test fungi, significant antifungal activity against Cladosporium herbarum was exhibited by most notably the fruit (MID: 100 microg), and the leaf (MID: 400 microg) extracts. None of the extracts were significantly cytotoxic, and lethal towards brine shrimps. The root, leaf, trunk and stem bark extracts (except for the fruits) showed strong antioxidant activity exceeding that of the standard antioxidant, alpha-tocopherol. Antitumour-promoting activity (>95% inhibition) was shown by the fruit, leaf, stem and trunk bark extracts.

  13. Rapamycin Synergizes with Cisplatin in Antiendometrial Cancer Activation by Improving IL-27–Stimulated Cytotoxicity of NK Cells

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    Wen-Jie Zhou

    2018-01-01

    Full Text Available Natural killer (NK cell function is critical for controlling initial tumor growth and determining chemosensitivity of the tumor. A synergistic relationship between rapamycin and cisplatin in uterine endometrial cancer (UEC in vitro has been reported, but the mechanism and the combined therapeutic strategy for endometrial cancer (EC are still unknown. We found a positive correlation between the level of IL-27 and the differentiated stage of UEC. The increase of IL-27 in uterine endometrial cancer cell (UECC lines (Ishikawa, RL95-2 and KLE led to a high cytotoxic activity of NK cells to UECC in the co-culture system. Exposure with rapamycin enhanced the cytotoxicity of NK cells by upregulating the expression of IL-27 in UECC and IL-27 receptors (IL-27Rs: WSX-1 and gp130 on NK cells and further restricted the growth of UEC in Ishikawa-xenografted nude mice. In addition, treatment with rapamycin resulted in an increased autophagy level of UECC, and IL-27 enhanced this ability of rapamycin. Cisplatin-mediated NK cells' cytotoxic activity and anti-UEC activation were independent of IL-27; however, the combination of rapamycin and cisplatin led to a higher cytotoxic activity of NK cells, smaller UEC volume and longer survival rate in vivo. These results suggest that rapamycin and cisplatin synergistically activate the cytotoxicity of NK cells and inhibit the progression of UEC in both an IL-27–dependent and –independent manner. This provides a scientific basis for potential rapamycin-cisplatin combined therapeutic strategies targeted to UEC, especially for the patients with low differentiated stage or abnormally low level of IL-27.

  14. Structure-activity relationships of novel salicylaldehyde isonicotinoyl hydrazone (SIH analogs: iron chelation, anti-oxidant and cytotoxic properties.

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    Eliška Potůčková

    Full Text Available Salicylaldehyde isonicotinoyl hydrazone (SIH is a lipophilic, tridentate iron chelator with marked anti-oxidant and modest cytotoxic activity against neoplastic cells. However, it has poor stability in an aqueous environment due to the rapid hydrolysis of its hydrazone bond. In this study, we synthesized a series of new SIH analogs (based on previously described aromatic ketones with improved hydrolytic stability. Their structure-activity relationships were assessed with respect to their stability in plasma, iron chelation efficacy, redox effects and cytotoxic activity against MCF-7 breast adenocarcinoma cells. Furthermore, studies assessed the cytotoxicity of these chelators and their ability to afford protection against hydrogen peroxide-induced oxidative injury in H9c2 cardiomyoblasts. The ligands with a reduced hydrazone bond, or the presence of bulky alkyl substituents near the hydrazone bond, showed severely limited biological activity. The introduction of a bromine substituent increased ligand-induced cytotoxicity to both cancer cells and H9c2 cardiomyoblasts. A similar effect was observed when the phenolic ring was exchanged with pyridine (i.e., changing the ligating site from O, N, O to N, N, O, which led to pro-oxidative effects. In contrast, compounds with long, flexible alkyl chains adjacent to the hydrazone bond exhibited specific cytotoxic effects against MCF-7 breast adenocarcinoma cells and low toxicity against H9c2 cardiomyoblasts. Hence, this study highlights important structure-activity relationships and provides insight into the further development of aroylhydrazone iron chelators with more potent and selective anti-neoplastic effects.

  15. Poly(lactic acid) nanoparticles loaded with ursolic acid: Characterization and in vitro evaluation of radical scavenging activity and cytotoxicity.

    Science.gov (United States)

    Antônio, Emilli; Antunes, Osmar Dos Reis; de Araújo, Isis Souza; Khalil, Najeh Maissar; Mainardes, Rubiana Mara

    2017-02-01

    The purpose of this study was to develop poly(lactic acid) (PLA) nanoparticles containing ursolic acid (UA) by an emulsification-solvent evaporation technique and evaluate the radical scavenging activity over hypochlorous acid (HOCl) and cytotoxicity over erythrocytes and tumor cells. Nanoparticles were successfully obtained and presented mean size of 246nm with spherical or slightly oval morphology, negative zeta potential and 96% of UA encapsulation efficiency. Analyses of FTIR, XRD and DSC-DTG suggest interaction/complexation of UA with PLA matrix and drug amorphization promoted by nanoencapsulation process. Stability study showed that room temperature was the best condition for nanoparticles storage. The in vitro release study showed UA was released from the polymeric matrix over two constants (α, β), suggesting a second order kinetics. After 120h of assay, 60% of UA were released by diffusion. In the HOCl scavenging activity, after 72h of assay UA-loaded nanoparticles presented the same efficacy of free drug. In cytotoxicity test over red blood cells, UA-loaded nanoparticles showed less toxicity on cells than free drug. The cytotoxicity assay over melanoma cells line (B16-F10) showed after 72h that nanoparticles were able to reduce the cell viability in 70%. PLA nanoparticles showed be potential carriers for UA maintaining the antioxidant and antitumor activity of the UA and decreasing its cytotoxicity over normal cells. Copyright © 2016 Elsevier B.V. All rights reserved.

  16. Induction of Apoptosis and Cytotoxic Activities of Iranian Orthodox Black Tea Extract (BTE Using in vitro Models

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    Amirala Aghbali

    2014-05-01

    Full Text Available Purpose: Plant-derivate therapeutic agents can perform cancer chemotherapeutic activity through triggering apoptotic cell death. Our aim was to investigate the cytotoxic effects, induction of apoptosis, and the mechanism of cell death of Iranian orthodox black tea extracts (BTEs and hydro methanolic purified fractions (40, 60, 80 and 100% in KB cells (oral squamous cell carcinoma. Methods: In order to analyze the cytotoxic activity of the BTEs, MTT (3-(4, 5- dimetylthiazol-2-yl-2, 5 diphenyltetrazolium bromide and Trypan-blue assays were performed in oral squamous cell carcinoma (KB. Furthermore, the apoptosis inducing action of the extracts was determined by TUNEL, DNA fragmentation and cell death detection analysis. Results: Dichloromethane BTE and hydro methanol fractions (40 and 60% extract showed no cytotoxic effects; however, hydro methanol crude and hydro methanol fractions of BTE (80 and 100% significantly inhibited cell growth and viability in a dose and time dependent manner. In addition, Cell death assay, TUNEL, and DNA fragmentation indicated induction of apoptosis by hydro methanol 80 and 100% fractions of BTE in KB cells. Statistical significance was determined by analysis of variance (ANOVA, followed by Duncan test and p value ≤0.05 was considered significant. Conclusion: The results from the present study suggests that the hydro methanol crude and hydro methanol fractions of BTE (80 and 100% are significant source of compounds with the anti proliferative and cytotoxic activities, and this may be useful for developing potential chemo preventive substances.

  17. Natural Killer Cell Receptors and Cytotoxic Activity in Phosphomannomutase 2 Deficiency (PMM2-CDG.

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    Roberto García-López

    Full Text Available PMM2-CDG is the most common N-glycosylation defect and shows an increased risk of recurrent and/or severe, sometimes fatal, infections in early life. We hypothesized that natural killer (NK cells, as important mediators of the immune response against microbial pathogens and regulators of adaptive immunity, might be affected in this genetic disorder.To evaluate possible defects on PMM2-CDG NK peripheral blood cell number, killing activity and expression of membrane receptors.We studied fresh and activated NK cells from twelve PMM2-CDG cells. The number and expression of lymphoid surface receptors were studied by flow cytometry. The NK responsiveness (frequency of degranulated NK cells and killing activity against K562 target cells was determined in the NK cytotoxicity assay.We found an increase of blood NK cells in three patients with a severe phenotype. Two of them, who had suffered from moderate/severe viral infections during their first year of life, also had reduced T lymphocyte numbers. Patient activated NK cells showed increased expression of CD54 adhesion molecule and NKG2D and NKp46 activating receptors. NKp46 and 2B4 expression was inversely correlated with the expression of NKG2D in activated PMM2-CDG cells. Maximal NK activity against K562 target cells was similar in control and PMM2-CDG cells. Interestingly, the NK cell responsiveness was higher in patient cells. NKG2D and specially CD54 increased surface expression significantly correlated with the increased NK cell cytolytic activity according to the modulation of the killer activity by expression of triggering receptors and adhesion molecules.Our results indicate that hypoglycosylation in PMM2-CDG altered NK cell reactivity against target cells and the expression of CD54 and NKG2D, NKp46 and 2B4 activating receptors during NK cell activation. This suggests a defective control of NK cell killing activity and the overall anti-viral immune response in PMM2-CDG patients. The present

  18. Substituted N-aminothioglycolurils containing thiosemicarbazone moiety and their cytotoxic activity in vitro.

    Science.gov (United States)

    Gazieva, Galina A; Anikina, Lada V; Pukhov, Sergei A; Karpova, Tatyana B; Nelyubina, Yulia V; Kravchenko, Angelina N

    2016-11-01

    A library of hybrid molecules bearing thioglycoluril and (hetero)aromatic aldehyde thiosemicarbazone moieties was synthesized via a tandem hydrazone formation-ring contraction reaction of 5,7-dialkyl-3-thioxoperhydroimidazo[4,5-e]-1,2,4-triazin-6-ones with (hetero)aromatic aldehydes. All synthesized compounds were tested for their cytotoxic activity against rhabdomyosarcoma, A549, and MS human cancer cell lines by MTT-assay. Among the derivatives, (E)-4-benzylideneamino-1,3-dimethyl-5-thioxohexahydroimidazo[4,5-d]imidazol-2(1H)-one 1f was found to have the most marked antiproliferative activity toward the tested cell lines (1f: IC[Formula: see text] 23.7, and 6.4 [Formula: see text]M, respectively). The IC[Formula: see text] value of thioglycoluril 1f against normal human embryonic kidney cells HEK293 was 72.5 [Formula: see text]M, which appeared to be 3-11-fold higher than IC[Formula: see text] values of 1f against human cancer cells.

  19. EVALUATION OF ANTIMICROBIAL AND CYTOTOXIC ACTIVITIES OF PLANT EXTRACTS FROM SOUTHERN MINAS GERAIS CERRADO

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    Juliana Moscardini Chavasco

    2014-01-01

    Full Text Available The antimicrobial activity of plant hidroethanolic extracts on bacteria Gram positive, Gram negative, yeasts, Mycobacterium tuberculosis H37 and Mycobacterium bovis was evaluated by using the technique of Agar diffusion and microdilution in broth. Among the extracts evaluated by Agar diffusion, the extract of Bidens pilosa leaf presented the most expressive average of haloes of growth inhibition to the microorganisms, followed by the extract of B. pilosa flower, of Eugenia pyriformis' leaf and seed, of Plinia cauliflora leaf which statistically presented the same average of haloes inhibitory formation on bacteria Gram positive, Gram negative and yeasts. The extracts of Heliconia rostrata did not present activity. Mycobacterium tuberculosis H37 and Mycobacterium bovis (BCG appeared resistant to all the extracts. The susceptibility profile of Candida albicans and Saccharomyces cerevisiae fungi were compared to one another and to the Gram positive Bacillus subtilis, Enterococcus faecalis and the Gram negative Salmonella typhimurium bacteria (p > 0.05. The evaluation of cytotoxicity was carried out on C6-36 larvae cells of the Aedes albopictus mosquito. The extracts of stem and flower of Heliconia rostrata, leaf and stem of Plinia cauliflora, seed of Anonna crassiflora and stem, flower and root of B. pilosa did not present toxicity in the analyzed concentrations. The highest rates of selectivity appeared in the extracts of stem of A. crassiflora and flower of B. pilosa to Staphylococcus aureus, presenting potential for future studies about a new drug development.

  20. Antiproliferative and cytotoxic effects of purple pitanga (Eugenia uniflora L.) extract on activated hepatic stellate cells.

    Science.gov (United States)

    Denardin, Cristiane C; Parisi, Mariana M; Martins, Leo A M; Terra, Silvia R; Borojevic, Radovan; Vizzotto, Márcia; Perry, Marcos L S; Emanuelli, Tatiana; Guma, Fátima T C R

    2014-01-01

    The presence of phenolic compounds in fruit- and vegetable-rich diets has attracted researchers' attention due to their health-promoting effects. The objective of this study was to evaluate the effects of purple pitanga (Eugenia uniflora L.) extract on cell proliferation, viability, mitochondrial membrane potential, cell death and cell cycle in murine activated hepatic stellate cells (GRX). Cell viability by 3-(4,5-dimethylthiazolyl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) assay was significantly decreased on cells treated with 50 and 100 µg ml(-1) of purple pitanga extract for 48 and 72 h, and the percentage of dead cell stained with 7-amino-actinomycin D was significantly higher in treated cells. The reduction of cell proliferation was dose dependent, and we also observed alterations on cell cycle progression. At all times studied, GRX cells treated with 50 and 100 µg ml(-1) of purple pitanga showed a significant reduction in cellular mitochondrial content as well as a decrease in mitochondrial membrane potential. Furthermore, our results indicated that purple pitanga extract induces early and late apoptosis/necrosis and necrotic death in GRX cells. This is the first report describing the antiproliferative, cytotoxic and apoptotic activity for E. uniflora fruits in hepatic stellate cells. The present study provides a foundation for the prevention and treatment of liver fibrosis, and more studies will be carried to elucidate this effect. Copyright © 2013 John Wiley & Sons, Ltd.

  1. Chemical composition, antibacterial activity and cytotoxicity of essential oils of Tanacetum parthenium in different developmental stages.

    Science.gov (United States)

    Mohsenzadeh, F; Chehregani, A; Amiri, H

    2011-09-01

    Tanacetum parthenium Schultz Bip. (Asteraceae) is an aromatic perennial plant, widely distributed in the northern hemisphere. This species traditionally has been used in insecticides, cosmetics, balsams, dyes, medicines and preservatives. The essential oil of T. parthenium was obtained by hydrodistillation in three developmental stages and analyzed by gas chromatography-mass spectrometry. The antibacterial activity of the oils was investigated against four Gram-positive and four Gram-negative bacteria. The oil was tested for cytotoxicity against THP-1 cells using the Trypan blue assay. Twenty-nine components were identified in the essential oil; the highest amount was extracted at the flowering stage. The main component, in the flowering stage, was camphor (18.94%) and other major components were bornyl acetate (18.35%), camphene (13.74%), bornyl isovalerate (3.15%), borneol (10.93%), juniper camphor (6.23%) and β-eudesmol (2.65%). Minimum inhibitory concentration of essential oil was evaluated from 4 µL mL(-1) against Staphylococcus subtilis to 38 µL mL(-1) against Entrobacter aerogenes. Toxicity assay showed that the oil has no significant toxicity at 5-15% v/v concentrations on THP-1 cells. This study demonstrates the occurrence of camphor/bornyl acetate chemotype of T. parthenium in western regions of Iran. The finding showed also the studied oils have relatively good antibacterial activity without significant toxicity, thus have great potentiality to be used as natural health product.

  2. Regio- and enantioselective microbial hydroxylation and evaluation of cytotoxic activity of β-cyclocitral-derived halolactones.

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    Marcelina Mazur

    Full Text Available Three β-cyclocitral-derived halolactones, which exhibit antifeedant activity towards storage product pests, were subjected to microbial transformation processes. Among the thirty tested strains of filamentous fungi and yeast, the most effective biocatalysts were Absidia cylindrospora AM336, Mortierella isabellina AM212 and Mortierella vinaceae AM149. As a result of regio- and enantioselective hydroxylation four new oxygenated derivatives were obtained. Regardless of the biocatalyst applied, the δ-iodo- and δ-bromo-γ-lactones were hydroxylated in an inactivated position C-5 of cyclohexane ring. The analogous transformation of chlorolactone was observed in Mortierella isabellina AM212 culture but in the case of two other biocatalysts the hydroxy group was introduced at C-3 position. All obtained hydroxylactones were enantiomerically pure (ee = 100% or enriched (ee = 50%. The highest enantioselectivity of hydroxylation was observed for M. isabellina AM212. The cytotoxic activity of halolactones was also examined by WST-1 assay wherein tested compounds did not exhibit significant effect on the viability of tumor HeLa and normal CHO-K1 cells.

  3. Non-cytotoxic nanomaterials enhance antimicrobial activities of cefmetazole against multidrug-resistant Neisseria gonorrhoeae.

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    Lan-Hui Li

    Full Text Available The emergence and spread of antibiotic-resistant Neisseria gonorrhoeae has led to difficulties in treating patients, and novel strategies to prevent and treat this infection are urgently needed. Here, we examined 21 different nanomaterials for their potential activity against N. gonorrhoeae (ATCC 49226. Silver nanoparticles (Ag NPs, 120 nm showed the greatest potency for reducing N. gonorrhoeae colony formation (MIC: 12.5 µg/ml and possessed the dominant influence on the antibacterial activity with their properties of the nanoparticles within a concentration range that did not induce cytotoxicity in human fibroblasts or epithelial cells. Electron microscopy revealed that the Ag NPs significantly reduced bacterial cell membrane integrity. Furthermore, the use of clinical isolates of multidrug-resistant N. gonorrhoeae showed that combined treatment with 120 nm Ag NPs and cefmetazole produced additive effects. This is the first report to screen the effectiveness of nanomaterials against N. gonorrhoeae, and our results indicate that 120 nm Ag NPs deliver low levels of toxicity to human epithelial cells and could be used as an adjuvant with antibiotic therapy, either for topical use or as a coating for biomaterials, to prevent or treat multidrug-resistant N. gonorrhoeae.

  4. Chemical Characterization and Cytotoxic Activity of Blueberry Extracts (cv. Misty) Cultivated in Brazil.

    Science.gov (United States)

    Massarotto, Giovana; Barcellos, Thiago; Garcia, Charlene Silvestrin Celi; Brandalize, Ana Paula Carneiro; Moura, Sidnei; Schwambach, Joséli; Henriques, João Antonio Pêgas; Roesch-Ely, Mariana

    2016-08-01

    Vaccinium corymbosum (L.) varieties cultivation is relatively recent in Brazil, but its production has been intensified given its good adaptability to the Southern Brazil climate. Blueberries are a rich source of phenolic compounds and contain significant levels of anthocyanins, flavonols, chlorogenic acids, and procyanidins, which lead to different biological activities. Chemical identification of skin and whole hydroalcoholic blueberry extracts (ExtSB and ExtWB) revealed the presence of anthocyanins concentrated in the skin and others chemicals compounds as quercetin glycosides, proanthocyanins dimers, citric, and chlorogenic acid in the pulp. Selectivity for tumor cell lines (Hep-2, HeLa, HT-29) using ExtSB and ExtWB extracts was observed through MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay after 24 h of treatment when compared to nontumor cells (MRC-5). Morphological changes and late stages of apoptotic and necrosis process were seen in HT-29 cell line after ExtWB treatment, compared to nontumor cell line MRC-5. These results are in agreement with other studies that indicate the activity of compounds such as anthocyanins and other molecules found in Southern Highbush blueberry variety, attributed to promote beneficial effects on health that may respond as cytotoxic natural agent and contribute to cancer treatment. © 2016 Institute of Food Technologists®

  5. Antioxidant, Anti-Lipoxygenase and Cytotoxic Activity of Leptadenia pyrotechnica (Forssk. Decne Polyphenolic Constituents

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    Nael M. Fawzi

    2011-09-01

    Full Text Available Leptadenia pyrotechnica Forssk is a traditional medicinal herb used for treatment of inflammatory diseases and cancer. In this research, the aqueous ethanolic crude extract of Leptadenia pyrotechnica aerial parts, along with its ethyl acetate, n-butanol and water partitioning fractions were evaluated for their antioxidant capacity, polyphenolic content, anti-inflammatory and anti-cancer properties. The total antioxidant capacity was estimated by the FRAP, DPPH, ABTS and β-carotene bleaching assays.The ethyl acetate fraction exhibited the highest polyphenolic content (252.27 mg gallic acid/g and the best antioxidant activity (1.2, 0.57, 0.45 mmol ascorbic acid equivalent/g in the FRAP, ABTS and DPPH assays, respectively. Furthermore, the same extract showed appreciable anti-inflammatory via lipoxygenase (LOX inhibitory activity (IC50 = 1.41 µg/mL. Moreover, the ethyl acetate fraction also showed the strongest cytotoxic effect (IC50 = 43.16 µg/mL against MCF-7 human breast cancer cell line. These results suggest that this plant may be considered an interesting source of compounds with antioxidant, anti-inflammatory and anti-cancer properties for therapeutic, nutraceutical and functional food applications.

  6. Secondary metabolites of ponderosa lemon (Citrus pyriformis) and their antioxidant, anti-inflammatory, and cytotoxic activities.

    Science.gov (United States)

    Hamdan, Dalia; El-Readi, Mahmoud Zaki; Tahrani, Ahmad; Herrmann, Florian; Kaufmann, Dorothea; Farrag, Nawal; El-Shazly, Assem; Wink, Michael

    2011-01-01

    Column chromatography of the dichloromethane fraction from an aqueous methanolic extract of fruit peel of Citrus pyriformis Hassk. (Rutaceae) resulted in the isolation of seven compounds including one coumarin (citropten), two limonoids (limonin and deacetylnomilin), and four sterols (stigmasterol, ergosterol, sitosteryl-3-beta-D-glucoside, and sitosteryl-6'-O-acyl-3-beta-D-glucoside). From the ethyl acetate fraction naringin, hesperidin, and neohesperidin were isolated. The dichloromethane extract of the defatted seeds contained three additional compounds, nomilin, ichangin, and cholesterol. The isolated compounds were identified by MS (EI, CI, and ESI), 1H, 13C, and 2D-NMR spectral data. The limonoids were determined qualitatively by LC-ESI/MS resulting in the identification of 11 limonoid aglycones. The total methanolic extract of the peel and the petroleum ether, dichloromethane, and ethyl acetate fractions were screened for their antioxidant and anti-inflammatory activities. The ethyl acetate fraction exhibited a significant scavenging activity for DPPH free radicals (IC50 = 132.3 microg/mL). The petroleum ether fraction inhibited 5-lipoxygenase with IC50 = 30.6 microg/mL indicating potential anti-inflammatory properties. Limonin has a potent cytotoxic effect against COS7 cells [IC50 = (35.0 +/- 6.1) microM] compared with acteoside as a positive control [IC50 = (144.5 +/- 10.96) microM].

  7. Composition, Cytotoxic and Antimicrobial Activities of Satureja intermedia C.A.Mey Essential Oil

    Directory of Open Access Journals (Sweden)

    Javad Sharifi-Rad

    2015-08-01

    Full Text Available In this study, the essential oil (EO constituents from the aerial parts of Satureja intermedia C.A.Mey were detected by GC and GC/MS. The antimicrobial activity of EO on oral pathogens and its cytotoxicity to human cancer cells were determined by the microbroth dilution method and the crystal violet staining method, respectively. Thirty-nine compounds were identified and the main EO constituents were γ-terpinene (37.1%, thymol (30.2%, p-cymene (16.2%, limonene (3.9%, α-terpinene (3.3%, myrcene (2.5%, germacrene B (1.4%, elemicine (1.1% and carvacrol (0.5%. The S. intermedia EO showed a concentration-dependent decrease in viability of Hep-G2 (hepatocellular carcinoma and MCF-7 (breast adenocarcinoma human cancer cell lines (p < 0.05. Antimicrobial screening of S. intermedia EO demonstrated slight antibacterial and antifungal activities against Streptococcus mutants, S. salivarius, Enterococcus faecalis, Staphylococcus aureus, Candida albicans and C. glabrata. Further preclinical studies are needed to assess the efficacy and safety of S. intermedia EO as a new promising anticancer agent.

  8. Antimicrobial, Antioxidant and Cytotoxic Activity of MarineStreptomyces parvulus VITJS11 Crude Extract

    Directory of Open Access Journals (Sweden)

    S. Jemimah Naine

    2015-04-01

    Full Text Available The main aim of the study was to evaluate the bioactive properties of ethyl acetate crude extract of Streptomyces parvulus VITJS11 with a view to assess their therapeutic potential. The biological activity of ethyl acetate extract was tested against fungal and bacterial pathogens. The free radical scavenging potential of the crude extract was determined by DPPH assay. The chemo preventive properties of S. parvulus VITJS11 ethyl acetate extract was examined by MTT assay on HepG2 cells. The morphological, physiological and the biochemical properties of the strain S. parvulus VITJS11 was confirmed by conventional methods. Genotypic characterization was done using 16S r-DNA partial gene amplification and sequencing. The authenticity of the crude chemical constitutes were determined by the GC-MS. The ethyl acetate extract of VITJS11 showed maximum antifungal activity against three Aspergillus species and prominent antibacterial activity against two Gram positive and Gram negative bacteria at 20 mg/mL. The antioxidant potential of the crude extract exhibited strong reducing power activity at 5mg/ mL with 85% inhibition and the cytotoxic effect was found with IC50 of 500µg/ mL on HepG2 cell lines. The GC-MS analysis and the chromatogram patterns revealed 16 peaks, indicating the presence of bioactive constituents, which included several important organic compounds, namely 9-(2',2'-dimethylpropanoilhydrazono-3,6-dichloro-2,7-Bis-[2-(diethylamino-ethoxy]fluorine (23.1 Dotriacontylpentafluoropropionate,(25.0 Octadecanoic acid, (20.0; Trans-2-methyl-4-n-butylthiane, S, S-dioxide.(19.0. The results showed the benefit of ethyl acetate extract from S. parvulus VITJS11 in treating microbial infections and indicated their broad spectrum of activity with beneficial virtues for therapeutic use.

  9. Anti-Inflammatory, Antioxidant, Antibiotic, and Cytotoxic Activities of Tanacetum vulgare L. Essential Oil and Its Constituents

    Directory of Open Access Journals (Sweden)

    Héloïse Coté

    2017-05-01

    Full Text Available Background: Tanacetum vulgare L. (Asteraceae is a perennial herb that has been used to treat multiple ailments. Regional variability of the chemical composition of T. vulgare essential oils is well-known. Despite these regional chemotypes, most relevant studies did not analyze the complete chemical composition of the T. vulgare essential oil and its constituents in relation to their biological activities. Here, we assess the anti-inflammatory, antioxidant, antibacterial, and cytotoxic activities of T. vulgare collected from northern Quebec (Saguenay-Lac-St-Jean, Canada. Methods: Essential oil was extracted from plants by steam distillation and analyzed using GC-FID. Biological activities of essential oil and its main constituents were evaluated in vitro. Results: We identified the major compounds as camphor, borneol, and 1,8-cineole. The oil possesses anti-inflammatory activity inhibiting NO production. It also inhibits intracellular DCFH oxidation induced by tert-butylhydroperoxide. Anti-inflammatory activity of essential oil appears driven mainly by α-humulene while antioxidant activity is provided by α-pinene and caryophyllene oxide. Essential oil from T vulgare was active against both Escherichia coli and Staphylococcus aureus with camphor and caryophyllene oxide responsible for antibacterial activity. Finally, T. vulgare essential oil was slightly cytotoxic against the human healthy cell line WS1 while α-humulene and caryophyllene oxide were moderately cytotoxic against A-549, DLD-1, and WS1. Conclusion: We report, for the first time, links between the specific compounds found in T. vulgare essential oil and anti-inflammatory, antioxidant, antibacterial, and cytotoxic activities. T. vulgare essential oil possesses interesting biological properties.

  10. In vitro antioxidant, anti-inflammatory, cytotoxic activities against prostate cancer of extracts from Hibiscus sabdariffa leaves.

    Science.gov (United States)

    Worawattananutai, Patsorn; Itharat, Arunporn; Ruangnoo, Srisopa

    2014-08-01

    Hibiscus sabdariffa (HS) leaves are a vegetable, which is used as a healthy sour soup for protection against chronic diseases in Thai traditional medicine. To investigate antioxidant, anti-inflammatory and cytotoxic activities of Hibiscus sabdariffa leave extracts from diferent extraction methods. Fresh and dry Hibiscus sabdariffa leaves were extracted by various methods such as maceration with 95% and 50% ethanol, squeeze, and boiling with water or decoction. All extracts were testedfor antioxidant activity by using DPPH radical scavenging assay, anti-inflammatory activity by determination on inhibitory effect of nitric oxide production on RAW264. 7 cell. Cytotoxic activity also tested against human prostate cancer cell line (PC-3) by using sulforhodamine B (SRB) assay. Total phenolic content determined by the Folin-Ciocalteu colorimetric method. The results found that the 95% ethanolic extract of Hibiscus sabdariffa dried leaves (HSDE95) showed the highest antioxidant activity with an EC50 of 34.51±2.62 μg/ml and had the highest phenolic content (57.00±3.73 mg GAE/g). HSDE95 also showed potent cytotoxicity against prostate cancer cell line with an IC50 of 8.58±0.68 μg/ml whereas HSDE95 and all of extracts ofHibiscus sabdariffa leaves had no anti-inflammatory activity. The obtained results revealed that HSDE95 extract showedpotent cytotoxic activity against prostate cancer cells but low antioxidant and anti-inflammatory activities. This extract should be further isolated as active compounds against prostate cancer.

  11. Anti-Inflammatory, Antioxidant, Antibiotic, and Cytotoxic Activities of Tanacetum vulgare L. Essential Oil and Its Constituents.

    Science.gov (United States)

    Coté, Héloïse; Boucher, Marie-Anne; Pichette, André; Legault, Jean

    2017-05-25

    Background:Tanacetum vulgare L. (Asteraceae) is a perennial herb that has been used to treat multiple ailments. Regional variability of the chemical composition of T. vulgare essential oils is well-known. Despite these regional chemotypes, most relevant studies did not analyze the complete chemical composition of the T. vulgare essential oil and its constituents in relation to their biological activities. Here, we assess the anti-inflammatory, antioxidant, antibacterial, and cytotoxic activities of T. vulgare collected from northern Quebec (Saguenay-Lac-St-Jean), Canada. Methods: Essential oil was extracted from plants by steam distillation and analyzed using GC-FID. Biological activities of essential oil and its main constituents were evaluated in vitro. Results: We identified the major compounds as camphor, borneol, and 1,8-cineole. The oil possesses anti-inflammatory activity inhibiting NO production. It also inhibits intracellular DCFH oxidation induced by tert-butylhydroperoxide. Anti-inflammatory activity of essential oil appears driven mainly by α-humulene while antioxidant activity is provided by α-pinene and caryophyllene oxide. Essential oil from T vulgare was active against both Escherichia coli and Staphylococcus aureus with camphor and caryophyllene oxide responsible for antibacterial activity. Finally, T. vulgare essential oil was slightly cytotoxic against the human healthy cell line WS1 while α-humulene and caryophyllene oxide were moderately cytotoxic against A-549, DLD-1, and WS1. Conclusion: We report, for the first time, links between the specific compounds found in T. vulgare essential oil and anti-inflammatory, antioxidant, antibacterial, and cytotoxic activities. T. vulgare essential oil possesses interesting biological properties.

  12. Concanavalin A-induced activation of lymphocytic choriomeningitis virus memory lymphocytes into specifically cytotoxic T cells

    DEFF Research Database (Denmark)

    Marker, O; Thomsen, Allan Randrup; Andersen, G T

    1977-01-01

    When spleen cells, which have been primed to Lymphocytic Choriomeningitis (LCM) virus during a primary infection several months previously, are stimulated in vitro with Con A. highly specific secondary cytotoxic effector cells are generated. The degree of cytotoxicity revealed by such Con A-stimu......-stimulated cells is higher than that of non-incubated spleen cells harvested nine days following the primary infection, and the effect is totally inhibited by anti-theta serum plus complement treatment of the effector cells immediately before the cytotoxic test....

  13. Phytochemical screening, antiproliferative and cytotoxic activities of the mosses Rhytidiadelphus triquetrus (Hedw. Warnst. and Tortella tortuosa (Hedw. Limpr.

    Directory of Open Access Journals (Sweden)

    Muhammet Şamil Yağlıoğlu

    2017-06-01

    Full Text Available The paper presents information about the phytochemical analysis, antiproliferative and cytotoxic activities of Rhytidiadelphus triquetrus and Tortella tortuosa extracts. The cytotoxic activities of some extracts shows highest antiproliferative activities were detected with Lactate Dehydrogenase Leakage Assay. Sixteen components obtained from hexane extracts were determined by GC/MS. Palmitic acid was identified as the main component. The phenolic components of the other extracts were determined by HPLC-TOF/MS. 4-hydroxy benzoic acid, salicylic acid, gallic acid, caffeic acid, and gensitic acid were detected as the main components in all extracts. The hexane, chloroform, ethyl acetate extracts of studied mosses and the EtOAc and hexane extracts of R. triquetrus showed statistically significant antiproliferative activities.

  14. Synthesis and pharmacophore modeling of naphthoquinone derivatives with cytotoxic activity in human promyelocytic leukemia HL-60 cell line.

    Science.gov (United States)

    Pérez-Sacau, Elisa; Díaz-Peñate, Raquel G; Estévez-Braun, Ana; Ravelo, Angel G; García-Castellano, Jose M; Pardo, Leonardo; Campillo, Mercedes

    2007-02-22

    Catalyst/HypoGen pharmacophore modeling approach and three-dimensional quantitative structure-activity relationship (3D-QSAR)/comparative molecular similarity indices analysis (CoMSIA) methods have been successfully applied to explain the cytotoxic activity of a set of 51 natural and synthesized naphthoquinone derivatives tested in human promyelocytic leukemia HL-60 cell line. The computational models have facilitated the identification of structural elements of the ligands that are key for antitumoral properties. The four most salient features of the highly active beta-cycled-pyran-1,2-naphthoquinones [0.1 microM active 1,4-naphthoquinone derivatives accurately fulfill only three of these features. The results of our study provide a valuable tool in designing new and more potent cytotoxic analogues.

  15. Antimicrobial, Antioxidant, and Cytotoxic Activities of Ocimum forskolei and Teucrium yemense (Lamiaceae) Essential Oils

    Science.gov (United States)

    Ali, Nasser A. Awadh; Chhetri, Bhuwan K.; Dosoky, Noura S.; Shari, Khola; Al-Fahad, Ahmed J. A.; Wessjohann, Ludger; Setzer, William N.

    2017-01-01

    Background: Ocimum forskolei and Teucrium yemense (Lamiaceae) are used in traditional medicine in Yemen. Methods: The chemical composition, antimicrobial, antioxidant and cytotoxic activities of the essential oils isolated from the leaves of Ocimum forskolei Benth. (EOOF) and two different populations of Teucrium yemense Deflers., one collected from Dhamar province (EOTY-d), and another collected from Taiz (EOTY-t) were investigated. The antimicrobial activities of the oils were evaluated against several microorganisms with the disc diffusion test or the broth microdilution test. The essential oils were screened for in-vitro cytotoxic activity against human tumor cells. EOOF and EOTY-d were screened for free-radical-inhibitory activity using the DPPH radical scavenging assay. Results: Sixty-four compounds were identified in (EOOF) representing 100% of the oil content with endo-fenchol (31.1%), fenchone (12.2%), τ-cadinol (12.2%), and methyl (E)-cinnamate (5.1%) as the major compounds. In EOTY-d, 67 compounds were identified, which made up 91% of the total oil. The most abundant constituents were (E)-caryophyllene (11.2%), α-humulene (4.0.%), γ-selinene (5.5%), 7-epi-α-selinene (20.1%), and caryophyllene oxide (20.1%), while the major compounds in EOTY-t were α-pinene (6.6%), (E)-caryophyllene (19.1%) α-humulene (6.4%), δ-cadinene (6.5%), caryophyllene oxide (4.3%), α-cadinol (9.5%), and shyobunol (4.6%). The most sensitive microorganisms for EOOF were B. subtilis, S. aureus, and C. albicans with inhibition zones of 34, 16, and 24 mm and MIC values of, 4.3 mg/mL, 4.3 mg/mL, and 8.6 mg/mL, respectively. EOTY-t showed antimicrobial activity against S. aureus, B. cereus, A. niger, and B. cinerea with MIC values of 0.156, 0.156, 0.313 and 0.313 mg/mL, respectively. Neither essential oil showed remarkable radical inhibition (IC50 = 31.55 and 31.41 μL/mL). EOTY-d was active against HT-29 human colorectal adenocarcinoma cell lines with IC50 = 43.7

  16. CHEMICAL CHARACTERIZATION AND EVALUATION OF ANTIBACTERIAL, ANTIFUNGAL, ANTIMYCOBACTERIAL, AND CYTOTOXIC ACTIVITIES OF Talinum paniculatum

    Directory of Open Access Journals (Sweden)

    Luis F.C. DOS REIS

    2015-10-01

    Full Text Available SUMMARY In this study, the bioactivity of Talinum paniculatum was evaluated, a plant widely used in folk medicine. The extract from the T. paniculatum leaves (LE was obtained by percolation with ethanol-water and then subjecting it to liquid-liquid partitions, yielding hexane (HX, ethyl acetate (EtOAc, butanol (BuOH, and aqueous (Aq fractions. Screening for antimicrobial activity of the LE and its fractions was evaluated in vitro through broth microdilution method, against thirteen pathogenic and non-pathogenic microorganisms, and the antimycobacterial activity was performed through agar diffusion assay. The cytotoxic concentrations (CC90 for LE, HX, and EtOAc were obtained on BHK-21 cells by using MTT reduction assay. The LE showed activity against Serratia marcescens and Staphylococcus aureus, with Minimum Inhibitory Concentration (MIC values of 250 and 500 µg/mL, respectively. Furthermore, HX demonstrated outstanding activity against Micrococcus luteus and Candida albicans with a MIC of 31.2 µg/mL in both cases. The MIC for EtOAc also was 31.2 µg/mL against Escherichia coli. Conversely, BuOH and Aq were inactive against all tested microorganisms and LE proved inactive against Mycobacterium tuberculosisand Mycobacterium bovisas well. Campesterol, stigmasterol, and sitosterol were the proposed structures as main compounds present in the EF and HX/EtOAc fractions, evidenced by mass spectrometry. Therefore, LE, HX, and EtOAc from T. paniculatumshowed potential as possible sources of antimicrobial compounds, mainly HX, for presenting low toxicity on BHK-21 cells with excellent Selectivity Index (SI = CC90/MIC of 17.72 against C. albicans.

  17. Enhancing the Anti-Tumor Activity of Breast Cancer-Specific Cytotoxic T Lymphocytes

    National Research Council Canada - National Science Library

    Malek, Thomas

    2001-01-01

    .... Our goals were to engineer the interleukin-2-receptor (IL-2R) in cytotoxic T cells (CTL) to control signal transduction through this receptor and to improve the in vivo efficacy of adoptive CTL immunotherapy...

  18. Topological estimation of cytotoxic activity of some anti-HIV agents ...

    Indian Academy of Sciences (India)

    Unknown

    hydroxyethoxy) methyl]-6-(phenylthio)-thymine) analogues have been discussed. The molecular descriptors used being van der Waals volume (Vw) and equalized electronegativity (χeq). The in vitro cytotoxicities (pCC50) were modelled using these ...

  19. Topological estimation of cytotoxic activity of some anti-HIV agents ...

    Indian Academy of Sciences (India)

    hydroxyethoxy) methyl]-6-(phenylthio)-thymine) analogues have been discussed. The molecular descriptors used being van der Waals volume () and equalized electronegativity (eq). The in vitro cytotoxicities (50) were modelled using these ...

  20. Resveratrol exhibits a strong cytotoxic activity in cultured cells and has an antiviral action against polyomavirus: potential clinical use

    Directory of Open Access Journals (Sweden)

    Galati Gaspare

    2009-07-01

    Full Text Available Abstract Background Resveratrol is a non flavonoid polyphenol compound present in many plants and fruits and, at especially high concentrations, in the grape berries of Vitis vinifera. This compound has a strong bioactivity and its cytoprotective action has been demonstrated, however at high concentrations the drug exhibits also an effective anti-proliferative action. We recently showed its ability to abolish the effects of oxidative stress in cultured cells. In this work we assayed the bioactivity of resveratrol as antiproliferative and antiviral drug in cultured fibroblasts. Studies by other Authors showed that this natural compound inhibits the proliferation of different viruses such as herpes simplex, varicella-zoster and influenza A. The results presented here show an evident toxic activity of the drug at high concentrations, on the other hand at sub-cytotoxic concentrations, resveratrol can effectively inhibit the synthesis of polyomavirus DNA. A possible interpretation is that, due to the damage caused by resveratrol to the plasma membrane, the transfer of the virus from the endoplasmic reticulum to the nucleus, may be hindered thus inhibiting the production of viral DNA. Methods The mouse fibroblast line 3T6 and the human tumor line HL60 were used throughout the work. Cell viability and vital cell count were assessed respectively, by the MTT assay and Trypan Blue staining. Cytotoxic properties and evaluation of viral DNA production by agarose gel electrophoresis were performed according to standard protocols. Results Our results show a clear dose dependent both cytotoxic and antiviral effect of resveratrol respectively at high and low concentrations. The cytotoxic action is exerted towards a stabilized cell-line (3T6 as well as a tumor-line (HL60. Furthermore the antiviral action is evident after the phase of virion entry, therefore data suggest that the drug acts during the synthesis of the viral progeny DNA. Conclusion Resveratrol is

  1. Cyclotide Structure–Activity Relationships: Qualitative and Quantitative Approaches Linking Cytotoxic and Anthelmintic Activity to the Clustering of Physicochemical Forces

    Science.gov (United States)

    Park, Sungkyu; Strömstedt, Adam A.; Göransson, Ulf

    2014-01-01

    Cyclotides are a family of plant-derived proteins that are characterized by a cyclic backbone and a knotted disulfide topology. Their cyclic cystine knot (CCK) motif makes them exceptionally resistant to thermal, chemical, and enzymatic degradation. Cyclotides exert much of their biological activity via interactions with cell membranes. In this work, we qualitatively and quantitatively analyze the cytotoxic and anthelmintic membrane activities of cyclotides. The qualitative and quantitative models describe the potency of cyclotides using four simple physicochemical terms relevant to membrane contact. Specifically, surface areas of the cyclotides representing lipophilic and hydrogen bond donating properties were quantified and their distribution across the molecular surface was determined. The resulting quantitative structure-activity relation (QSAR) models suggest that the activity of the cyclotides is proportional to their lipophilic and positively charged surface areas, provided that the distribution of these surfaces is asymmetric. In addition, we qualitatively analyzed the physicochemical differences between the various cyclotide subfamilies and their effects on the cyclotides' orientation on the membrane and membrane activity. PMID:24682019

  2. Synthesis, Leishmanicidal and Cytotoxic Activity of Triclosan-Chalcone, Triclosan-Chromone and Triclosan-Coumarin Hybrids

    Directory of Open Access Journals (Sweden)

    Elver Otero

    2014-08-01

    Full Text Available Twelve hybrids derived from triclosan were obtained via Williamson etherification of O-triclosan alkyl bromide plus chalcone and O-coumarin or O-chromone alkyl bromide plus triclosan, respectively. Structures of the products were elucidated by spectroscopic analysis. The synthesized compounds were evaluated for antileishmanial activity against L. (V panamensis amastigotes. Cytotoxic activity was also evaluated against mammalian U-937 cells. Compounds 7–9 and 17, were active against Leishmania parasites (EC50 = 9.4; 10.2; 13.5 and 27.5 µg/mL, respectively and showed no toxicity toward mammalian cells (>200 µg/mL. They are potential candidates for antileishmanial drug development. Compounds 25–27, were active and cytotoxic. Further studies using other cell types are needed in order to discriminate whether the toxicity shown by these compounds is against tumor or non-tumor cells. The results indicate that compounds containing small alkyl chains show better selectivity indices. Moreover, Michael acceptor moieties may modify both the leishmanicidal activity and cytotoxicity. Further studies are required to evaluate if the in vitro activity against Leishmania panamensis demonstrated here is also observed in vivo.

  3. Inhibition of human lymphocyte natural cytotoxicity and antibody-dependent cell-mediated cytotoxicity by K-76 COONa, a reagent that blocks complement activity.

    Science.gov (United States)

    Hudig, D; Redelman, D; Minning, L; Carine, K

    1984-07-01

    K-76 COONa is a 440 m.w. fungal product that can inhibit complement activity of C5 and Factor I. K-76 COONa abrogated both human natural killer (NK) cell activity and antibody-dependent cell-mediated cytotoxicity (ADCC) (ID50 approximately 1.5 mM). To be effective, K-76 COONa had to be present during the assay, because pretreatment of lymphocytes with highly inhibitory concentrations of K-76 COONa did not inhibit cytolysis. The monocarboxylic K-76 derivative was more inhibitory to NK than the dicarboxylic derivative. This relative efficacy is similar to that observed for inhibition of complement lysis. K-76 COONa inhibited NK when added before NK conjugate formation, but had little effect when added after conjugate formation. The compound also inhibited the formation of conjugates by NK and K cells. Therefore, this reagent selectively affected events that occurred between the initial effector-target cell interactions and the formation of stable conjugates. It had little influence on the post-binding "lethal hit" stage of cytolysis. These data imply a) that if any molecules similar to C5 are activated during the "lethal hit" stage of cytolysis, then they are inaccessible to K-76 COONa , and b) that C3bi-like molecules may be involved in lymphocyte binding.

  4. Chemical Constituents and Evaluation of Antimicrobial and Cytotoxic Activities of Kielmeyera coriacea Mart. & Zucc. Essential Oils

    Directory of Open Access Journals (Sweden)

    Carla de M. Martins

    2015-01-01

    Full Text Available Many essential oils (EOs of different plant species possess interesting antimicrobial effects on buccal microorganisms and cytotoxic properties. EOs of Kielmeyera coriacea Mart. & Zucc. were analyzed by gas chromatography coupled to mass spectrometry (GC-MS. The EO from leaves is rich in sesquiterpenes hydrocarbons and oxygenated sesquiterpenes. The three major compounds identified were germacrene-D (24.2%, (E-caryophyllene (15.5%, and bicyclogermacrene (11.6%. The inner bark EO is composed mainly of sesquiterpenes hydrocarbons and the major components are alpha-copaene (14.9% and alpha-(E-bergamotene (13.0%. The outer bark EO is composed mainly of oxygenated sesquiterpenes and long-chain alkanes, and the major components are alpha-eudesmol (4.2% and nonacosane (5.8%. The wood EO is mainly composed of long-chain alkanes and fatty acids, and the major components are nonacosane (9.7% and palmitic acid (16.2%. The inner bark EO showed the strongest antimicrobial activity against the anaerobic bacteria Prevotella nigrescens (minimum inhibitory concentration-MIC of 50 µg mL−1. The outer bark and wood EOs showed MICs of 100 µg mL−1 for all aerobic microorganisms tested. The EOs presented low toxicity to Vero cells. These results suggest that K. coriacea, a Brazilian plant, provide initial evidence of a new and alternative source of substances with medicinal interest.

  5. MDM2 antagonist Nutlin-3a potentiates antitumour activity of cytotoxic drugs in sarcoma cell lines

    Directory of Open Access Journals (Sweden)

    Lothe Ragnhild A

    2011-05-01

    Full Text Available Abstract Background Frequent failure and severe side effects of current sarcoma therapy warrants new therapeutic approaches. The small-molecule MDM2 antagonist Nutlin-3a activates the p53 pathway and efficiently induces apoptosis in tumours with amplified MDM2 gene and overexpression of MDM2 protein. However, the majority of human sarcomas have normal level of MDM2 and the therapeutic potential of MDM2 antagonists in this group is still unclear. We have investigated if Nutlin-3a could be employed to augment the response to traditional therapy and/or reduce the genotoxic burden of chemotherapy. Methods A panel of sarcoma cell lines with different TP53 and MDM2 status were treated with Nutlin-3a combined with Doxorubicin, Methotrexate or Cisplatin, and their combination index determined. Results Clear synergism was observed when Doxorubicin and Nutlin-3a were combined in cell lines with wild-type TP53 and amplified MDM2, or with Methotrexate in both MDM2 normal and amplified sarcoma cell lines, allowing for up to tenfold reduction of cytotoxic drug dose. Interestingly, Nutlin-3a seemed to potentiate the effect of classical drugs as Doxorubicin and Cisplatin in cell lines with mutated TP53, but inhibited the effect of Methotrexate. Conclusion The use of Nutlin in combination with classical sarcoma chemotherapy shows promising preclinical potential, but since clear biomarkers are still lacking, clinical trials should be followed up with detailed tumour profiling.

  6. Annonalide and derivatives: Semisynthesis, cytotoxic activities and studies on interaction of annonalide with DNA.

    Science.gov (United States)

    Marques, Ricardo A; Gomes, Akenaton O C V; de Brito, Maria V; Dos Santos, Ana L P; da Silva, Gladyane S; de Lima, Leandro B; Nunes, Fátima M; de Mattos, Marcos C; de Oliveira, Fátima C E; do Ó Pessoa, Cláudia; de Moraes, Manoel O; de Fátima, Ângelo; Franco, Lucas L; Silva, Marina de M; Dantas, Maria Dayanne de A; Santos, Josué C C; Figueiredo, Isis M; da Silva-Júnior, Edeíldo F; de Aquino, Thiago M; de Araújo-Júnior, João X; de Oliveira, Maria C F; Leslie Gunatilaka, A A

    2018-02-01

    The cytotoxic activity of the pimarane diterpene annonalide (1) and nine of its semisynthetic derivatives (2-10) was investigated against the human tumor cell lines HL-60 (leukemia), PC-3 (prostate adenocarcinoma), HepG2 (hepatocellular carcinoma), SF-295 (glioblastoma) and HCT-116 (colon cancer), and normal mouse fibroblast (L929) cells. The preparation of 2-10 involved derivatization of the side chain of 1 at C-13. Except for 2, all derivatives are being reported for the first time. Most of the tested compounds presented IC 50 s below 4.0 μM, being considered potential antitumor agents. The structures of all new compounds were elucidated by spectroscopic analyses including 2D NMR and HRMS. Additionally, the interaction of annonalide (1) with ctDNA was evaluated using spectroscopic techniques, and the formation of a supramolecular complex with the macromolecule was confirmed. Competition assays with fluorescent probes (Hoechst and ethidium bromide) and theoretical studies confirmed that 1 interacts preferentially via DNA intercalation with stoichiometric ratio of 1:1 (1:ctDNA). The ΔG value was calculated as -28.24 kJ mol -1 , and indicated that the interaction process occurs spontaneously. Docking studies revealed that van der Walls is the most important interaction in 1-DNA and EB-DNA complexes, and that both ligands (1 and EB) interact with the same DNA residues (DA6, DA17 and DT19). Copyright © 2018. Published by Elsevier B.V.

  7. Cytotoxic activity of Flavobacterium psychrophilum in skeletal muscle cells of rainbow trout (Oncorhynchus mykiss).

    Science.gov (United States)

    Iturriaga, Mathias; Espinoza, Marlen Brisa; Poblete-Morales, Matías; Feijoo, Carmen Gloria; Reyes, Ariel E; Molina, Alfredo; Avendaño-Herrera, Ruben; Valdés, Juan Antonio

    2017-10-01

    Flavobacterium psychrophilum is the etiologic agent of bacterial coldwater disease (BCWD) and rainbow trout fry syndrome (RTFS), which cause significant worldwide losses in aquaculture. Juvenile rainbow trout are particularly susceptible to F. psychrophilum infection, the main external clinical signs of which are extensive necrotic myositis and ulcerative lesions. Despite the economic relevance of this pathogen in aquaculture, little is known about the molecular mechanisms underlying F. psychrophilum infection and pathogenesis. In this study, cultured skeletal muscle cells from rainbow trout (Oncorhynchus mykiss) were co-incubated with the virulent strain of F. psychrophilum JIP02/86 (ATCC 49511). Trypan blue exclusion analysis at 48h post-incubation revealed decreased cellular viability. Direct bacteria-myoblast contact was found a key factor in inducing F. psychrophilum cytotoxicity. Apoptosis was characterized by nuclear DNA fragmentation, decreased plasma membrane integrity, increased caspase activity, and the proteolytic cleavage of poly(ADP-ribose)polymerase-1 (PARP-1). Moreover, bacterial infection induced an early inhibition of NF-κB signaling, as well as a differential expression of the pro- and anti-apoptotic genes, bax and bcl-2. These findings suggest that F. psychrophilum induces rainbow trout muscle apoptosis through the modulation of the NF-κB signaling as a mechanism for nutrient acquisition and survival. Copyright © 2017 Elsevier B.V. All rights reserved.

  8. Different antibacterial activity of novel theophylline-based ionic liquids - Growth kinetic and cytotoxicity studies.

    Science.gov (United States)

    Borkowski, Andrzej; Ławniczak, Łukasz; Cłapa, Tomasz; Narożna, Dorota; Selwet, Marek; Pęziak, Daria; Markiewicz, Bartosz; Chrzanowski, Łukasz

    2016-08-01

    The aim of this study was to investigate novel theophylline-based ionic liquids and their cytotoxic effects towards model Gram-positive and Gram-negative bacteria (Bacillus cereus and Escherichia coli, respectively). Growth kinetics, respiratory rates and dehydrogenase activities were studied in the presence of ionic liquids at concentrations ranging from 10 to 1000mg/L. Additionally, the influence of ionic liquids on bacterial cells associated with specific interactions based on the structure of cell wall was evaluated. This effect was assessed by viability tests and scanning electron microscope observations. The obtained results confirmed that ionic liquids exhibit different levels of toxicity in relation to Gram-positive and Gram-negative bacteria. Those effects are associated with the chemical structure of the cationic species of the ionic liquids and their critical micelle concentration value. It was established that the presence of an alkyl or allyl group increased the toxicity, whereas the presence of an aryl group in the cation decreased the toxic effect of ILs. Results presented in this study also revealed unexpected effects of self-aggregation of E. coli cells. Overall, it was established that the studied ILs exhibited higher toxicity towards Gram-positive bacteria due to different interactions between the ILs and the cell membranes. These findings may be of importance for the design of ILs with targeted antimicrobial properties. Copyright © 2016 Elsevier Inc. All rights reserved.

  9. Activation of cytotoxic and regulatory functions of NK cells by Sindbis viral vectors.

    Science.gov (United States)

    Granot, Tomer; Venticinque, Lisa; Tseng, Jen-Chieh; Meruelo, Daniel

    2011-01-01

    Oncolytic viruses (OVs) represent a relatively novel anti-cancer modality. Like other new cancer treatments, effective OV therapy will likely require combination with conventional treatments. In order to design combinatorial treatments that work well together, a greater scrutiny of the mechanisms behind the individual treatments is needed. Sindbis virus (SV) based vectors have previously been shown to target and kill tumors in xenograft, syngeneic, and spontaneous mouse models. However, the effect of SV treatment on the immune system has not yet been studied. Here we used a variety of methods, including FACS analysis, cytotoxicity assays, cell depletion, imaging of tumor growth, cytokine blockade, and survival experiments, to study how SV therapy affects Natural Killer (NK) cell function in SCID mice bearing human ovarian carcinoma tumors. Surprisingly, we found that SV anti-cancer efficacy is largely NK cell-dependent. Furthermore, the enhanced therapeutic effect previously observed from Sin/IL12 vectors, which carry the gene for interleukin 12, is also NK cell dependent, but works through a separate IFNγ-dependent mechanism, which also induces the activation of peritoneal macrophages. These results demonstrate the multimodular nature of SV therapy, and open up new possibilities for potential synergistic or additive combinatorial therapies with other treatments.

  10. The role of membrane fusion activity of a whole inactivated influenza virus vaccine in (re)activation of influenza-specific cytotoxic T lymphocytes

    NARCIS (Netherlands)

    Budimir, Natalija; Meijerhof, Tjarko; Wilschut, Jan; Huckriede, Anke; de Haan, Aalzen

    2010-01-01

    Induction of cytotoxic T lymphocyte (CTL) activity against conserved influenza antigens, e.g. nucleoprotein (NP) could be a step towards cross-protective influenza vaccine. The major challenge for non-replicating influenza vaccines aiming for activation of CTLs is targeting of antigen to the MHC

  11. Proinflammatory effects of bacterial lipoprotein on human neutrophil activation status, function and cytotoxic potential in vitro.

    LENUS (Irish Health Repository)

    Power, C

    2012-02-03

    Bacterial lipoprotein (BLP) is the most abundant protein in gram-negative bacterial cell walls, heavily outweighing lipopolysaccharide (LPS). Herein we present findings demonstrating the potent in vitro effects of BLP on neutrophil (PMN) activation status, function, and capacity to transmigrate an endothelial monolayer. PMNs are the principal effectors of the initial host response to injury or infection and constitute a significant threat to invading bacterial pathogens. The systemic inflammatory response syndrome (SIRS) is characterised by significant host tissue injury mediated, in part, by uncontrolled regulation of PMN cytotoxic activity. We found that BLP-activated human PMN as evidenced by increased CD11b\\/CD18 (Mac-1) expression. Up-regulation of PMN Mac-1 in response to BLP occurred independently of membrane-bound CD14 (mCD14). A similar up-regulation of intercellular adhesion molecule-1 (ICAM-1) on endothelial cells was observed whilst E-Selectin expression was unaffected. PMN transmigration across a human umbilical vein endothelial cell (HUVEC) monolayer was markedly increased after treating either PMN\\'s or HUVEC independently with BLP. This increased transmigration did not occur as a result of any direct effect of BLP on HUVEC monolayer permeability, assessed objectively using the passage of FITC-labeled Dextran-70. BLP primed PMN for enhanced respiratory burst and superoxide anion production in response to PMA, but did not influence phagocytosis of opsonized Escherichia coli. BLP far exceeds LPS as a gram-negative bacterial wall component, these findings therefore implicate BLP as an additional putative mediator of SIRS arising from gram-negative infection.

  12. Cytotoxicity and anti-Sporothrix brasiliensis activity of the Origanum majorana Linn. oil.

    Science.gov (United States)

    Waller, Stefanie Bressan; Madrid, Isabel Martins; Ferraz, Vanny; Picoli, Tony; Cleff, Marlete Brum; de Faria, Renata Osório; Meireles, Mário Carlos Araújo; de Mello, João Roberto Braga

    The study aimed to evaluate the anti-Sporothrix sp. activity of the essential oil of Origanum majorana Linn. (marjoram), its chemical analysis, and its cytotoxic activity. A total of 18 fungal isolates of Sporothrix brasiliensis (n: 17) from humans, dogs and cats, and a standard strain of Sporothrix schenckii (n: 1) were tested using the broth microdilution technique (Clinical and Laboratory Standard Institute - CLSI M27-A3) and the results were expressed in minimal inhibitory concentration (MIC) and minimal fungicidal concentration (MFC). The MIC50 and MIC90 of itraconazole against S. brasiliensis were 2μg/mL and 8μg/mL, respectively, and the MFC50 and MFC90 were 2μg/mL and >16μg/mL, respectively, with three S. brasiliensis isolates resistant to antifungal. S. schenckii was sensitive at MIC of 1μg/mL and MFC of 8μg/mL. For the oil of O. majorana L., all isolates were susceptible to MIC of ≤2.25-9mg/mL and MFC of ≤2.25-18mg/mL. The MIC50 and MIC90 were ≤2.25mg/mL and 4.5mg/mL, respectively, and the MFC50/90 values were twice more than the MIC. Twenty-two compounds were identified by gas chromatography with a flame ionization detector (CG-FID) and 1,8-cineole and 4-terpineol were the majority. Through the colorimetric (MTT) assay, the toxicity was observed in 70-80% of VERO cells between 0.078 and 5mg/mL. For the first time, the study demonstrated the satisfactory in vitro anti-Sporothrix sp. activity of marjoram oil and further studies are needed to ensure its safe and effective use. Copyright © 2016 Sociedade Brasileira de Microbiologia. Published by Elsevier Editora Ltda. All rights reserved.

  13. Cytotoxicity and anti-Sporothrix brasiliensis activity of the Origanum majorana Linn. oil

    Directory of Open Access Journals (Sweden)

    Stefanie Bressan Waller

    Full Text Available Abstract The study aimed to evaluate the anti-Sporothrix sp. activity of the essential oil of Origanum majorana Linn. (marjoram, its chemical analysis, and its cytotoxic activity. A total of 18 fungal isolates of Sporothrix brasiliensis (n: 17 from humans, dogs and cats, and a standard strain of Sporothrix schenckii (n: 1 were tested using the broth microdilution technique (Clinical and Laboratory Standard Institute - CLSI M27-A3 and the results were expressed in minimal inhibitory concentration (MIC and minimal fungicidal concentration (MFC. The MIC50 and MIC90 of itraconazole against S. brasiliensis were 2 µg/mL and 8 µg/mL, respectively, and the MFC50 and MFC90 were 2 µg/mL and >16 µg/mL, respectively, with three S. brasiliensis isolates resistant to antifungal. S. schenckii was sensitive at MIC of 1 µg/mL and MFC of 8 µg/mL. For the oil of O. majorana L., all isolates were susceptible to MIC of ≤2.25-9 mg/mL and MFC of ≤2.25-18 mg/mL. The MIC50 and MIC90 were ≤2.25 mg/mL and 4.5 mg/mL, respectively, and the MFC50/90 values were twice more than the MIC. Twenty-two compounds were identified by gas chromatography with a flame ionization detector (CG-FID and 1,8-cineole and 4-terpineol were the majority. Through the colorimetric (MTT assay, the toxicity was observed in 70-80% of VERO cells between 0.078 and 5 mg/mL. For the first time, the study demonstrated the satisfactory in vitro anti-Sporothrix sp. activity of marjoram oil and further studies are needed to ensure its safe and effective use.

  14. Isolation of a New Natural Product and Cytotoxic and Antimicrobial Activities of Extracts from Fungi of Indonesian Marine Habitats

    Directory of Open Access Journals (Sweden)

    Norbert Arnold

    2011-02-01

    Full Text Available In the search for bioactive compounds, 11 fungal strains were isolated from Indonesian marine habitats. Ethyl acetate extracts of their culture broth were tested for cytotoxic activity against a urinary bladder carcinoma cell line and for antifungal and antibacterial activities against fish and human pathogenic bacteria as well as against plant and human pathogenic fungi. The crude extract of a sterile algicolous fungus (KT31, isolated from the red seaweed Kappaphycus alvarezii (Doty Doty ex P.C. Silva exhibited potent cytotoxic activity with an IC50 value of 1.5 µg/mL. Another fungal strain (KT29 displayed fungicidal properties against the plant pathogenic fungus Cladosporium cucumerinum Ell. et Arth. at 50 µg/spot. 2-Carboxy-8-methoxy-naphthalene-1-ol (1 could be isolated as a new natural product.

  15. Helichrysum gymnocephalum Essential Oil: Chemical Composition and Cytotoxic, Antimalarial and Antioxidant Activities, Attribution of the Activity Origin by Correlations

    Directory of Open Access Journals (Sweden)

    François Couderc

    2011-09-01

    Full Text Available Helichrysum gymnocephalum essential oil (EO was prepared by hydrodistillation of its leaves and characterized by GC-MS and quantified by GC-FID. Twenty three compounds were identified. 1,8-Cineole (47.4%, bicyclosesquiphellandrene (5.6%, γ-curcumene (5.6%, α-amorphene (5.1% and bicyclogermacrene (5% were the main components. Our results confirmed the important chemical variability of H. gymnocephalum. The essential oil was tested in vitro for cytotoxic (on human breast cancer cells MCF-7, antimalarial (Plasmodium falciparum: FcB1-Columbia strain, chloroquine-resistant and antioxidant (ABTS and DPPH assays activities. H. gymnocephalum EO was found to be active against MCF-7 cells, with an IC50 of 16 ± 2 mg/L. The essential oil was active against P. falciparum (IC50 = 25 ± 1 mg/L. However, the essential oil exhibited a poor antioxidant activity in the DPPH (IC50 value > 1,000 mg/L and ABTS (IC50 value = 1,487.67 ± 47.70 mg/L assays. We have reviewed the existing results on the anticancer activity of essential oils on MCF-7 cell line and on their antiplasmodial activity against the P. falciparum. The aim was to establish correlations between the identified compounds and their biological activities (antiplasmodial and anticancer. β-Selinene (R² = 0.76, α-terpinolene (R² = 0.88 and aromadendrene (R² = 0.90 presented a higher relationship with the anti-cancer activity. However, only calamenene (R² = 0.70 showed a significant correlation for the antiplasmodial activity.

  16. Antibacterial, Antifungal and Cytotoxic Activities of 3,5-Diacetyltambulin Isolated from Amorphophallus Campanulatus Blume ex. Decne

    Directory of Open Access Journals (Sweden)

    M.S Islam

    2008-09-01

    Full Text Available Background and purpose of the study: Amorphophallus campanulatus is widely distributed in Bangladesh, India, and Africa and the tuberous roots of the plant has many traditional uses and is an important source of biologically active compounds. In the present study in vitro antibacterial, antifungal and cytotoxic activities of 3,5-diacetyltambulin which is a flavonoid isolated from Amorphophallus campanulatus was studied. Materials and Methods: In vitro antibacterial and antifungal activities was evaluated by disc diffusion and MICs technique was determined by serial dilution technique. Cytotoxicity was determined against brine shrimp nauplii. Results and Major conclusion: The compound showed significant antibacterial activities against four Gram-positive bacteria (Bacillus subtilis, Bacillus megaterium, Staphylococcus aureus, Streptococcus β-haemolyticus and six Gram-negative bacteria (Escheichia coli, Shigella dysenteriae, Shigella sonnei, Shigella flexneri, Pseudomonus aeruginosa, Salmonella typhi. The MIC values against these bacteria ranged from 8 to 64 µg/ml but had weak antifungal activity against a number of fungi. In cytotoxicity determination, LC50 of the compound against brine shrimp nauplii was 10.02 μg/ml.

  17. Semisynthesis, cytotoxicity, antiviral activity, and drug interaction liability of 7-O-methylated analogues of flavonolignans from milk thistle.

    Science.gov (United States)

    Althagafy, Hanan S; Graf, Tyler N; Sy-Cordero, Arlene A; Gufford, Brandon T; Paine, Mary F; Wagoner, Jessica; Polyak, Stephen J; Croatt, Mitchell P; Oberlies, Nicholas H

    2013-07-01

    Silymarin, an extract of the seeds of milk thistle (Silybum marianum), is used as an herbal remedy, particularly for hepatoprotection. The main chemical constituents in silymarin are seven flavonolignans. Recent studies explored the non-selective methylation of one flavonolignan, silybin B, and then tested those analogues for cytotoxicity and inhibition of both cytochrome P450 (CYP) 2C9 activity in human liver microsomes and hepatitis C virus infection in a human hepatoma (Huh7.5.1) cell line. In general, enhanced bioactivity was observed with the analogues. To further probe the biological consequences of methylation of the seven major flavonolignans, a series of 7-O-methylflavonolignans were generated. Optimization of the reaction conditions permitted selective methylation at the phenol in the 7-position in the presence of each metabolite's 4-5 other phenolic and/or alcoholic positions without the use of protecting groups. These 7-O-methylated analogues, in parallel with the corresponding parent compounds, were evaluated for cytotoxicity against Huh7.5.1 cells; in all cases the monomethylated analogues were more cytotoxic than the parent compounds. Moreover, parent compounds that were relatively non-toxic and inactive or weak inhibitors of hepatitis C virus infection had enhanced cytotoxicity and anti-HCV activity upon 7-O-methylation. Also, the compounds were tested for inhibition of major drug metabolizing enzymes (CYP2C9, CYP3A4/5, UDP-glucuronsyltransferases) in pooled human liver or intestinal microsomes. Methylation of flavonolignans differentially modified inhibitory potency, with compounds demonstrating both increased and decreased potency depending upon the compound tested and the enzyme system investigated. In total, these data indicated that monomethylation modulates the cytotoxic, antiviral, and drug interaction potential of silymarin flavonolignans. Copyright © 2013 Elsevier Ltd. All rights reserved.

  18. Evaluation of phytochemical content, antimicrobial, cytotoxic and antitumor activities of extract from Rumex hastatus D. Don roots.

    Science.gov (United States)

    Sahreen, Sumaira; Khan, Muhammad Rashid; Khan, Rahmat Ali; Hadda, Taibi Ben

    2015-07-03

    Being a part of Chinese as well as ayurdic herbal system, roots of Rumex hastatus D. Don (RH) is highly medicinal, used to regulated blood pressure. It is also reported that the plant is diuretic, laxative, tonic, used against microbial skin diseases, bilious complaints and jaundice. The present study is conducted to evaluate phytochemical, antimicrobial, antitumor and cytotoxic activities of extract obtained from R. hastatus roots. RH roots were powdered and extracted with methanol to get crude extract. Crude extract was further fractioned on the basis of increasing polarity, with n-hexane (HRR), chloroform (CRR), ethyl acetate (ERR), n-butanol (BRR) and residual aqueous fraction (ARR). Methanol extract and its derived fractions were subjected to phytochemical screening and assayed for antibacterial activities via agar well diffusion method. Antifungal activities were checked through agar tube dilution method whereas potato disc assay was employed for the determination of antitumor activity. On the other hand cytotoxic activities were conducted using brine shrimps procedures. The results obtained from phytochemical analysis indicate the presence of alkaloids, anthraquinones, flavonoids and saponins in all the fractions. Most of the plant fractions showed substantial antimicrobial activities, which is in accordance with the spacious use of tested plant samples in primary healthcare center. Fractions of R. hastatus roots for cytotoxicity were tested as an effective cytotoxic was found as BRR > MRR > CRR > ARR > ERR > HRR. Ranking order of fractions of R. hastatus roots for effective antitumor screening was found as MRR > BRR > ARR > CRR > ERR > HRR. These results showed that R. hastatus appeared as an important source for the discovery of new antimicrobial drugs and antitumor agents; verify its traditional uses and its exploitation as therapeutic agent.

  19. Hepatocellular apoptosis associated with cytotoxic T/natural killer-cell infiltration in chronic active EBV infection.

    Science.gov (United States)

    Nomura, Yuko; Kimura, Hiroshi; Karube, Kennosuke; Yoshida, Shiro; Sugita, Yasuo; Niino, Daisuke; Shimizu, Kei; Kimura, Yoshizo; Aoki, Ryosuke; Kiyasu, Junichi; Takeuchi, Masanori; Hashikawa, Keiko; Hirose, Shinichi; Ohshima, Koichi

    2009-07-01

    The aim of the present study was to identify the mechanism of hepatocellular apoptosis induced by EBV-infected cytotoxic T/natural killer (NK) cells in chronic active EBV infection (CAEBV). Eight patients with CAEBV were studied, and infected T-cell expansion and NK-cell expansion were detected in four patients each. Biopsy or necropsy was performed on lymph node, liver, or spleen, and each specimen was subjected to immunohistochemical double staining of CD3 plus caspase-3 with the addition of cytotoxic markers of T-cell restricted intracellular antigen-1 (TIA-1), perforin, and granzyme B, as well as EBV in situ hybridization (EBV-ISH). In the liver, some of the infiltrating CD3-positive lymphocytes stained positively for EBV-ISH and cytotoxic markers. Double staining of CD3 plus caspase-3 indicated caspase-3 positive hepatocytes with apoptotic features, accompanied by extensive infiltration of CD3-positive cells, which were directly attached to the apoptotic caspase-3 positive hepatocytes. In contrast, far fewer cells stained positive for caspase-3 in lymph node and spleen than in liver. The present findings suggest that in patients with CAEBV, cytotoxic T/NK cells may directly induce hepatocytes to undergo apoptosis more frequently than they do cells in other organs of the reticulo-endothelial system.

  20. Cytotoxicity mechanism of α-MMC in normal liver cells through LRP1 mediated endocytosis and JNK activation.

    Science.gov (United States)

    Wang, Ling; Shen, Fubing; Zhang, Min; He, Qianchuan; Zhao, Hui; Yu, Xiaoping; Yang, Shuxia; Liu, Yang; Deng, Nianhua; Zheng, Juecun; Zhu, Lixia; Liu, Xiaolan

    2016-05-16

    Alpha-momorcharin (α-MMC), a type I ribosome-inactivating protein isolated from Momordica charantia, is a potential drug candidate with strong anti-tumor activity. However, α-MMC has a severe hepatotoxicity when applied in vivo, which may greatly hinders its use in clinic in the future. The biological mechanism of hepatotoxicity induced by α-MMC is largely unknown, especially the mechanism by which α-MMC enters the hepatocytes. In this study, we investigated α-MMC-induced cytotoxicity in normal liver L02 cell line as well as the mechanism underlying it. As expected, α-MMC is more toxic in L02 cells than in various normal cells from other organs. The cytotoxic effect of α-MMC on L02 cells is found to be mediated through cell apoptosis as detected by flow cytometry and fluorescence microscopy. Importantly, α-MMC was shown to bind to a specific receptor on cell membrane, as the density of the cell membrane receptor is closely related to both the amount of α-MMC endocytosed and the cytotoxicity in different cell lines. By using LRP1 competitive inhibitor α2-M or siRNA targeting LRP1, we further identified that LRP1 protein served as the membrane receptor for α-MMC. Both α2-M and siRNA targeting LRP1 can significantly inhibit α-MMC's endocytosis as well as its cytotoxicity in L02 cells. In addition, it was found that α-MMC can activate the JNK signalling pathways via LRP1 in L02 cells. As JNK activation often leads to cell apoptosis, the activation of JNK may play an important role in α-MMC-induced cytotoxicity. To our knowledge, this is the first report showing that LRP1 mediates the cytotoxicity of α-MMC through (1) endocytosis and induced apoptosis and (2) the activation of the JNK pathway. Our findings shed light on the fundamental mechanism of hepatotoxicity of α-MMC and offer reference to understand its mechanism of lymphocytotoxicity and neurotoxicity. Copyright © 2016 Elsevier Ireland Ltd. All rights reserved.