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Sample records for synthesis cytotoxic activity

  1. Synthesis, characterisation, nuclease and cytotoxic activity of ...

    Indian Academy of Sciences (India)

    GULZAR A BHAT

    2018-02-07

    Feb 7, 2018 ... 2 were evaluated for their nuclease and in vitro anti-tumor activities against human breast and colorectal cancer cell lines. The DNA ... tive chemotherapeutic agent for the treatment of ovarian, lung, testicular, colon, and neck ... coma, leukemia, Hodgkin's lymphoma, brain tumours and cancer of the cervix, ...

  2. '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.

  3. 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)

  4. 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) OBOR OECD: Biochemistry and molecular biology; Organic chemistry (UOCHB-X) Impact factor: 2.282, year: 2016

  5. Synthesis of novel kavain-like derivatives and evaluation of their cytotoxic activity

    Energy Technology Data Exchange (ETDEWEB)

    Amaral, Patricia de A.; Agustini, Taciane; Eifler-Lima, Vera L. [Universidade Federal do Rio Grande do Sul (UFRGS), Porto Alegre (Brazil). Faculdade de Farmacia. Lab. de Sintese Organica Medicinal; Petrignet, Julien; Cariou, Alexandre; Gree, Rene [Universite de Rennes 1, Rennes (France). Lab. de Chimie Therapeutique; Gouault, Nicolas; Lohezic-Ledevehat, Francoise; David, Michele [CNRS UMR, Universite de Rennes 1, Rennes (France). Lab. de Chimie et Photonique Moleculaires

    2009-07-01

    Palladium-catalyzed cross coupling reactions (Sonogashira-Hagihara, Suzuki-Miyaura, and Heck) coupling and nickel hydride-mediated tandem isomerization aldolisation have been used for the synthesis of three series of {delta}-valerolactones substituted in positions 3, 4, 5 and 6 of the lactone ring. The 26 kavaien-like derivatives were tested against three cell lines and five of them exhibited a weak cytotoxic activity. (author)

  6. Synthesis of racemic and chiral albicanol, albicanyl acetate and cyclozonarone: cytotoxic activity of ent-cyclozonarone

    International Nuclear Information System (INIS)

    Delgado, Virginia; Armstrong, Veronica; Cortes, Manuel; Barrero, Alejandro F.

    2008-01-01

    The total synthesis of racemic cyclozonarone ((±)-3) was achieved from E,E-farnesol (4) in an eight-step sequence in 6.6% overall yield. Albicanol ((±)-1) and its acetate ((±)-2) are intermediates. A similar sequence starting from natural (-)-drimenol (5) gave (+)-albicanol (1) and (+)-cyclozonarone (3) (42% and 11% yield, respectively). The cytotoxic activity of (+)-cyclozonarone was assayed and showed some selectivity towards MS-1 (mice endothelial cells). (author)

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

    Directory of Open Access Journals (Sweden)

    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.

  8. 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.

  9. Benzimidazole condensed ring systems 10 (1). Synthesis and cytotoxic activity of some pyrido[1,2-a]benzimidazoles.

    Science.gov (United States)

    Badawey, E S; Kappe, T

    1995-01-01

    As a part of research project on the synthesis of a number of pyrido[1,2-a]benzimidazole derivatives with possible antineoplastic activity and as a result of the interesting antineoplastic activity recorded for one such compounds (NSC 649900), some new pyrido[1,2-a]benzimidazoles were prepared and evaluated for such activity. Compound (11, NSC 660334) exhibited a moderate in vitro antineoplastic activity especially against most of the leukemia cell lines, while compound (10, VM30309) showed a good cytotoxic activity against Artina salina larvae (IC50 = 1.75 micrograms/ml).

  10. 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.

  11. 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.

  12. Synthesis, antibacterial and cytotoxic activities of new biflorin-based hydrazones and oximes.

    Science.gov (United States)

    da S Souza, Luciana G; Almeida, Macia C S; Lemos, Telma L G; Ribeiro, Paulo R V; de Brito, Edy S; Silva, Vera L M; Silva, Artur M S; Braz-Filho, Raimundo; Costa, José G M; Rodrigues, Fábio F G; Barreto, Francisco S; de Moraes, Manoel O

    2016-01-15

    Biflorin 1 is a biologically active quinone, isolated from Capraria biflora. Five new biflorin-based nitrogen derivatives were synthesized, of which two were mixtures of (E)- and (Z)- isomers: (Z)-2a, (Z)-2b, (Z)-3a, (Z)- and (E)-3b, (Z)- and (E)-3c. The antibacterial activity was investigated using the microdilution method for determining the minimum inhibitory concentration (MIC) against six bacterial strains. Tests have shown that these derivatives have potential against all bacterial strains. The cytotoxic activity was also evaluated against three strains of cancer cells, but none of the derivatives showed activity. Copyright © 2015. Published by Elsevier Ltd.

  13. Synthesis and potential cytotoxic activity of some new benzoxazoles, imidazoles, benzimidazoles and tetrazoles.

    Science.gov (United States)

    Arulmurugan, Subramaniyan; Kavitha, Helen P

    2013-06-01

    2 The present work deals with the synthesis of some novel heterocyclic compounds such as benzoxazoles , 7, 13 and 19, imidazoles 3, 8, 14 and 20, benzimidazoles 4, 9, 15 and 21, and tetrazoles 10, 16, and 22. The synthesized compounds were characterized by IR, 1H NMR, mass spectrometry and elemental analysis. The compounds were evaluated for cytotoxicity against human cancer cell lines such as MCF-7 (breast cancer) and HT-29 (colon cancer) by the MTT assay method. Among the tested compounds, 4,4'-sulfonylbis(N-(2-(1H-benzo[d]imidazol- -2-yl)ethyl)aniline (9), N-bis(2-(benzo[d]oxazol-2-yl)-ethyl)- 6-phenyl-1,3,5-triazine-2,4-diamine (13), N-bis(2-(1H-benzo[ d]imidazol-2-yl)ethyl)-6-phenyl-1,3,5-triazine-2,4-diamine (15) and N-tris(2-1H-benzo[d]imidazol-2-yl)ethyl)- 1,3,5-triazine-2,4,6-triamine (21) showed potent cytotoxicity.

  14. Synthesis, cytotoxicity and haemolytic activity of Pulsatilla saponin A, D derivatives.

    Science.gov (United States)

    Chen, Zhong; Duan, Huaqing; Wang, Minglei; Han, Li; Liu, Yanli; Zhu, Yongming; Yang, Shilin

    2015-06-15

    The strong haemolytic activity of Pulsatilla saponin A (PSA), D (PSD) hampered their clinical development of antitumor agents. In order to solve this problem, C-28 position modification derivatives of PSA/PSD were synthesized. The cytotoxicity and haemolytic activity of these compounds were evaluated. Structure-activity relationship and structure-toxicity relationship had been observed. The mice acute toxicity of compound 11 was reduced greatly than that of PSA. This study indicates that compound 11 may represent an interesting class of potent antitumor agents from triterpenoid saponins avoiding the haemolysis problem. The present study has important significance for the development of antitumor saponins. Copyright © 2015 Elsevier Ltd. All rights reserved.

  15. Novel 5-Fluorouracil Derivatives: Synthesis and Cytotoxic Activity of 2-Butoxy-4-Substituted 5-Fluoropyrimidines

    International Nuclear Information System (INIS)

    Sun, Jian; Zhou, Wei; Hu, Weixiao; Shan, Shang; Zhang, Shijie; Li, Haibo

    2013-01-01

    Twenty two new 5-fluorouracil (5-FU) derivatives, 2-butoxy-4-substituted 5-fluoropyrimidines, were synthesized and characterized by IR, 1 H NMR, MS, HRMS. All compounds were preliminarily evaluated by MTT assay on human liver BEL-7402 cancer cell line in vitro. Ten compounds were selected to test their cytotoxic activity against A549, HL-60 and MCF-7 cancer cell lines in vitro. These compounds were more sensitive to BEL-7402 than other cell lines, particularly, cytotoxic activity of compounds 6b, 6d-f, 6p, 6s-u were in sub-micromolar scale. The highest cytotoxic potency against A549, HL-60 and MCF-7 was shown by 2-butoxy-4-chloro-5-fluoropyrimidine (5) with IC 50 values of 0.10, 1.66 and 0.59 μM, respectively. Compounds 6d and 6e were effective against MCF-7 with IC 50 9.73 μM and HL-60 with IC 50 8.83 μM, respectively

  16. Extracellular synthesis of gold bionanoparticles by Nocardiopsis sp. and evaluation of its antimicrobial, antioxidant and cytotoxic activities.

    Science.gov (United States)

    Manivasagan, Panchanathan; Alam, Moch Syaiful; Kang, Kyong-Hwa; Kwak, Minseok; Kim, Se-Kwon

    2015-06-01

    Advancement of biological process for the synthesis of bionanoparticles is evolving into a key area of research in nanotechnology. The present study deals with the biosynthesis, characterization of gold bionanoparticles by Nocardiopsis sp. MBRC-48 and evaluation of their antimicrobial, antioxidant and cytotoxic activities. The gold bionanoparticles obtained were characterized by UV-visible spectroscopy, X-ray diffraction analysis, Fourier transform infrared spectroscopy, field emission scanning electron microscopy, energy dispersive X-ray analysis and transmission electron microscopy (TEM). The synthesized gold bionanoparticles were spherical in shape with an average of 11.57 ± 1.24 nm as determined by TEM and dynamic light scattering (DLS) particle size analyzer, respectively. The biosynthesized gold nanoparticles exhibited good antimicrobial activity against pathogenic microorganisms. It showed strong antioxidant activity as well as cytotoxicity against HeLa cervical cancer cell line. The present study demonstrated the potential use of the marine actinobacterial strain of Nocardiopsis sp. MBRC-48 as an important source for gold nanoparticles with improved biomedical applications including antimicrobial, antioxidant as well as cytotoxic agent.

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

    International Nuclear Information System (INIS)

    Gan, Lin Ling; Fang, Bo; Zhou, Cheng He

    2010-01-01

    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

  18. 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.

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

    Directory of Open Access Journals (Sweden)

    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.

  20. Machine learning prioritizes synthesis of primaquine ureidoamides with high antimalarial activity and attenuated cytotoxicity.

    Science.gov (United States)

    Levatić, Jurica; Pavić, Kristina; Perković, Ivana; Uzelac, Lidija; Ester, Katja; Kralj, Marijeta; Kaiser, Marcel; Rottmann, Matthias; Supek, Fran; Zorc, Branka

    2018-02-25

    Primaquine (PQ) is a commonly used drug that can prevent the transmission of Plasmodium falciparum malaria, however toxicity limits its use. We prepared five groups of PQ derivatives: amides 1a-k, ureas 2a-k, semicarbazides 3a,b, acylsemicarbazides 4a-k and bis-ureas 5a-v, and evaluated them for antimalarial activity in vitro against the erythrocytic stage of P. falciparum NF54. Particular substituents, such as trityl (in 2j and 5r) and methoxybenzhydryl (in 3b and 5v) were associated with a favorable cytotoxicity-to-activity ratio. To systematically link structural features of PQ derivatives to antiplasmodial activity, we performed a quantitative structure-activity relationship (QSAR) study using the Support Vector Machines machine learning method. This yielded a highly accurate statistical model (R 2  = 0.776 in cross-validation), which was used to prioritize novel candidate compounds. Seven novel PQ-ureidoamides 10a-g were synthesized and evaluated for activity, highlighting the benzhydryl ureidoamides 10e and 10f derived from p-chlorophenylglycine. Further experiments on human cell lines revealed that 10e and 10f are an order of magnitude less toxic than PQ in vitro while having antimalarial activity indistinguishable from PQ. The toxicity profile of novel compounds 10 toward human cells was particularly favorable when the glucose-6-phosphate dehydrogenase (G6PD) was inhibited, while toxicity of PQ was exacerbated by G6PD inhibition. Our work therefore highlights promising lead compounds for the development of effective antimalarial drugs that may also be safer for G6PD-deficient patients. In addition, we provide computational inferences of antimalarial activity and cytotoxicity for thousands of PQ-like molecular structures. Copyright © 2018 Elsevier Masson SAS. All rights reserved.

  1. Synthesis, antimicrobial and cytotoxic activity of novel azetidine-2-one derivatives of 1H-benzimidazole

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    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.

  2. Synthesis, structural characterization and cytotoxic activity of two new organoruthenium(II complexes

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    SANJA GRGURIC-SIPKA

    2008-06-01

    Full Text Available Two new p-cymene ruthenium(II complexes containing as additional ligands N-methylpiperazine ([(η6-p-cymeneRuCl2(CH3NH(CH24NH]PF6, complex 1 or vitamin K3-thiosemicarbazone ([(η6-p-cymeneRuCl2(K3tsc], complex 2 were synthesized starting from [(η6-p-cymene2RuCl2]2 and the corresponding ligand. The complexes were characterized by elemental analysis, IR, electronic absorption and NMR spectroscopy. The X-ray crystal structure determination of complex 1 revealed “piano-stool” geometry. The differences in the cytotoxic activity of the two complexes are discussed in terms of the ligand present.

  3. Tryptophan-Assisted Synthesis Reduces Bimetallic Gold/Silver Nanoparticle Cytotoxicity and Improves Biological Activity

    Directory of Open Access Journals (Sweden)

    Igor O. Shmarakov

    2014-10-01

    Full Text Available Aiming to reduce the potential in vivo hepato-and nephrotoxicity of Ag/Au bimetallic nanoparticles (NPs stabilized by sodium dodecyl sulphate (SDS, an approach involving a simultaneous reduction of silver nitrate and tetrachlorauratic acid using tryptophan (Trp as a reducing/stabilizing agent was applied during NP synthesis. The obtained Ag/Au/Trp NPs (5–15 nm sized were able to form stable aggregates with an average size of 370–450 nm and were potentially less toxic than Ag/Au/SDS in relation to a mouse model system based on clinical biochemical parameters and oxidative damage product estimation. Ag/Au/Trp NPs were shown to exhibit anticancer activity in relation to a Lewis lung carcinoma model. The data generated from the present study support the fact that the use of tryptophan in NP synthesis is effective in attenuating the potential hepatotoxicity and nephrotoxicity of NPs during their in vivo application.

  4. Curcumin coated gold nanoparticles: synthesis, characterization, cytotoxicity, antioxidant activity and its comparison with citrate coated gold nanoparticles

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    Elnaz Shaabani

    2017-04-01

    Full Text Available Objective(s: Biological applications of gold nanoparticles have limitations because of the toxic chemicals used in their synthesis. Curcumin can be used as reducing as well as capping agent in synthesis of GNPs to eliminate the cytotoxicity. Conjugation of curcumin to gold also helps in increasing its solubility and bioavailability. Materials and Methods: Here we report synthesis of gold nanoparticles coated with citrate and curcumin and of two different sizes via chemical routes. UV-Vis absorbance spectroscopy, Dynamic Light Scattering and Transmission Electron Microscopy were applied to study the average particle size, size stability of the samples and zeta potential. Fourier transform infrared, Raman Spectroscopy and Fluorescence Spectroscopy were applied for detection of curcumin on the surface of GNPs. The antioxidant activity was evaluated using DPPH assay and Cytotoxicity was evaluated by MTT assay.Results: Particles were synthesized of 6 and 16 nm size. The average particle size was found to be 21.7 ± 5.7 by TEM. The zeta potential on the surface of Cur-GNPs was negative and larger than 25 mV which is a sign of their high stability. The stability of these particles (with different coatings but with similar sizes at different time intervals (up to 3 months and also in different media like cell culture medium, different buffers, glucose and at different pH conditions have been investigated thoroughly. Appearance of functional groups assigned to curcumin in FTIR and SERS spectra are sign of presence of curcumin in the sample. The quenching of the fluorescence in the presence of GNPs reveals the clear indication of the capping and binding of curcumin with GNPs. Cur-GNP1 (16 nm were found to exhibit highest antioxidant activity than other gold nanoparticles. Cytotoxicity evaluation using MTT assay on L929 cell line proved curcumin coated gold nanoparticles were non-toxic up to 40 ppm.Conclusion: The results revealed that larger curcumin

  5. Facile green synthesis of fluorescent N-doped carbon dots from Actinidia deliciosa and their catalytic activity and cytotoxicity applications

    Science.gov (United States)

    Arul, Velusamy; Sethuraman, Mathur Gopalakrishnan

    2018-04-01

    Green synthesis of fluorescent nitrogen doped carbon dots (N-CDs) using Actinidia deliciosa (A. deliciosa) fruit extract as a carbon precursor and aqueous ammonia as a nitrogen dopant is reported here. The synthesized N-CDs were characterized by high resolution transmission electron microscopy (HR-TEM), energy dispersive spectroscopy (EDS), selected area electron diffraction (SAED), UV-Visible spectroscopy (UV-Vis), fluorescence spectroscopy, Fourier transform infrared spectroscopy (FT-IR), X-ray diffraction (XRD), Raman spectroscopy and X-ray photoelectron spectroscopy (XPS). The average size of the N-CDs was approximately 3.59 nm and the calculated inter layer distance was found to be 0.21 nm. Raman spectroscopy and SAED pattern revealed the graphitic nature of the synthesized N-CDs. The N-CDs were found to emit intense blue color at 405 nm under the excitation of 315 nm. The doping of nitrogen over the surface of the N-CDs was confirmed by EDS, FT-IR and XPS studies. The synthesized N-CDs were found to exhibit excellent catalytic activity in the reduction of Rhodamine-B using sodium borohydrate. The MTT assay was used to evaluate the cytotoxicity and biocompatibility of N-CDs towards L-929 and MCF-7 cells. From the results obtained, it was found that the N-CDs exhibit low cytotoxicity and superior biocompatibility on both L-929 and MCF-7 cells.

  6. Synthesis of selectively deuterated and tritiated lupane derivatives with cytotoxic activity

    Czech Academy of Sciences Publication Activity Database

    Vlk, M.; Urban, M.; Elbert, Tomáš; Šarek, J.

    2013-01-01

    Roč. 298, č. 2 (2013), s. 1149-1157 ISSN 0236-5731 Grant - others:GA ČR(CZ) GA305/09/1216 Institutional support: RVO:61388963 Keywords : isotopic labelling * tritium * deuterium * betulin * betulinic acid * cytotoxicity Subject RIV: CB - Analytical Chemistry, Separation Impact factor: 1.415, year: 2013

  7. Synthesis and cytotoxic activities of estrone and estradiol cis-dichloroplatinum(II) complexes

    Czech Academy of Sciences Publication Activity Database

    Kvasnica, Miroslav; Rárová, L.; Oklešťková, Jana; Buděšínský, Miloš; Kohout, Ladislav

    2012-01-01

    Roč. 20, č. 24 (2012), s. 6969-6978 ISSN 0968-0896 R&D Projects: GA MŠk 1M06030; GA AV ČR IAA400550801 Grant - others:GA MŠk(CZ) ED0007/01/01 Program:ED Institutional support: RVO:61388963 ; RVO:61389030 Keywords : steroids * estrone * estradiol * platinum complex * cytotoxicity Subject RIV: CC - Organic Chemistry Impact factor: 2.903, year: 2012

  8. Preparation of new 18alpha-oleanane alcohols: synthesis, characterization, and cytotoxic activity

    Czech Academy of Sciences Publication Activity Database

    Kvasnica, Miroslav; Rudovská, I.; Hajduch, M.; Šarek, J.

    2010-01-01

    Roč. 141, č. 2 (2010), s. 233-244 ISSN 0026-9247 R&D Projects: GA AV ČR KAN200200651 Grant - others:GA ČR(CZ) GP203/05/P025; GA ČR(CZ) GA305/09/1216 Institutional research plan: CEZ:AV0Z40550506 Keywords : reduction * hydride * ketone * configuration * cytotoxicity Subject RIV: CC - Organic Chemistry Impact factor: 1.356, year: 2010

  9. A Convenient Ultrasound-Promoted Synthesis of Some New Thiazole Derivatives Bearing a Coumarin Nucleus and Their Cytotoxic Activity

    Directory of Open Access Journals (Sweden)

    Sobhi M. Gomha

    2012-08-01

    Full Text Available Successful implementation of ultrasound irradiation for the rapid synthesis of a novel series of 3-[1-(4-substituted-5-(aryldiazenylthiazol-2-ylhydrazonoethyl]-2H-chromen-2-ones 5ah, via reactions of 2-(1-(2-oxo-2H-chromen-3-ylethylidene thiosemicarbazide (2 and the hydrazonoyl halides 3(4, was demonstrated. Also, a new series of 5-arylidene-2-(2-(1-(2-oxo-2H-chromen-3-ylethylidenehydrazinylthiazol-4(5H-ones 10ad were synthesized from reaction of 2 with chloroacetic acid and different aldehydes. Moreover, reaction of 2-cyano-N'-(1-(2-oxo-2H-chromen-3-ylethylidene-acetohydrazide (12 with substituted benzaldehydes gave the respective arylidene derivatives 13ac under the conditions employed. The structures of the synthesized compounds were assigned based on elemental analyses and spectral data. Also, the cytototoxic activities of the thiazole derivative 5a was evaluated against HaCaT cells (human keratinocytes. It was found that compound 5a possess potent cytotoxic activity.

  10. Novel enaminones as non-cytotoxic compounds with mild antibacterial activity: Synthesis and structure-activity correlations

    Science.gov (United States)

    Cindrić, Marina; Rubčić, Mirta; Hrenar, Tomica; Pisk, Jana; Cvijanović, Danijela; Lovrić, Jasna; Vrdoljak, Višnja

    2018-02-01

    Six non-symmetric enaminones 4-[(2-hydroxy-5-methylphenyl)amino]pent-3-en-2-one (H2L1), 4-[(2-hydroxy-4-methylphenyl)amino]pent-3-en-2-one (H2L2), 4-[(4-hydroxy-2-methylphenyl)amino)]pent-3-en-2-one (H2L3), 3-[(2-hydroxy-5-methylphenyl)amino]-1-phenylbut-2-en-1-one (H2L4), 3-[(2-hydroxy-4-methylphenyl)amino]-1-phenylbut-2-en-1-one (H2L5) and 3-[(4-hydroxy-2-methylphenyl)amino]-1-phenylbut-2-en-1-one (H2L6) have been prepared by solution based method. The enaminones were characterized by elemental and DSC analysis, NMR and IR spectroscopy. Crystal and molecular structures of H2L1, H2L2, H2L4 and H2L6 were determined via single crystal X-ray analysis. The prepared enaminones were screened against THP-1 and HepG2 cells, and Staphylococcus aureus, Enterococcus faecalis, Escherichia coli and Moraxella catarrhalis bacteria to assess their cytotoxic and antibacterial activity, respectively. All compounds proved to be non-cytotoxic and showed mild or no antibacterial activity. Quantum mechanical calculations suggest that the presence of hydroxy group in ortho position, combined with the methyl group on the same aromatic ring, has a significant impact on the biological activities.

  11. Synthesis, DNA Cleavage Activity, Cytotoxicity, Acetylcholinesterase Inhibition, and Acute Murine Toxicity of Redox-Active Ruthenium(II) Polypyridyl Complexes.

    Science.gov (United States)

    Alatrash, Nagham; Narh, Eugenia S; Yadav, Abhishek; Kim, Mahn-Jong; Janaratne, Thamara; Gabriel, James; MacDonnell, Frederick M

    2017-07-06

    Four mononuclear [(L-L) 2 Ru(tatpp)] 2+ and two dinuclear [(L-L) 2 Ru(tatpp)Ru(L-L) 2 ] 4+ ruthenium(II) polypyridyl complexes (RPCs) containing the 9,11,20,22-tetraazatetrapyrido[3,2-a:2',3'-c:3'',2''-l:2''',3'''-n]pentacene (tatpp) ligand were synthesized, in which L-L is a chelating diamine ligand such as 2,2'-bipyridine (bpy), 1,10-phenanthroline (phen), 3,4,7,8-tetramethyl-1,10-phenanthroline (Me 4 phen) or 4,7-diphenyl-1,10-phenanthroline (Ph 2 phen). These Ru-tatpp analogues all undergo reduction reactions with modest reducing agents, such as glutathione (GSH), at pH 7. These, plus several structurally related but non-redox-active RPCs, were screened for DNA cleavage activity, cytotoxicity, acetylcholinesterase (AChE) inhibition, and acute mouse toxicity, and their activities were examined with respect to redox activity and lipophilicity. All of the redox-active RPCs show single-strand DNA cleavage in the presence of GSH, whereas none of the non-redox-active RPCs do. Low-micromolar cytotoxicity (IC 50 ) against malignant H358, CCL228, and MCF7 cultured cell lines was mainly restricted to the redox-active RPCs; however, they were substantially less toxic toward nonmalignant MCF10 cells. The IC 50 values for AChE inhibition in cell-free assays and the acute toxicity of RPCs in mice revealed that whereas most RPCs show potent inhibitory action against AChE (IC 50 values <15 μm), Ru-tatpp complexes as a class are surprisingly well tolerated in animals relative to other RPCs. © 2017 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim.

  12. Synthesis, characterization and evaluation cytotoxic activity of silver nanoparticles synthesized by Chinese herbal Cornus officinalis via environment friendly approach.

    Science.gov (United States)

    He, Yangqing; Li, Xing; Wang, Ju; Yang, Qian; Yao, Binghua; Zhao, Yingjuan; Zhao, Aiming; Sun, Wenxing; Zhang, Qian

    2017-12-01

    Cornus officinalis has been widely used as a precious herb and as the tonic food to improve kidney function in China. Its fruits have been used in many traditional Chinese medicine prescriptions to treat kidney diseases, diabetes, cancer and shock. In this study, a new eco-friendly approach for green synthesis of silver nanoparticles (AgNPs) by using the fruits of Cornus officinalis aqueous extract as a reducing and stabilizing agent. The so-synthesized AgNPs showed quasi-spherical in shape with uniform dispersal and an average mean size of 11.7nm. Water soluble biomolecules such as flavonoids and/or anthocyanins from the extract played important roles in the nanoparticles formation. The AgNPs displayed distinctive cytotoxicity activities against human prostate cancer (PC-3) and human liver cancer (HepG2) cell lines. The results provided a low cost, nontoxic and eco-friendly approach for synthesizing metal nanoparticles to explore alternative anticancer agents on the way fighting against cancer in future. Copyright © 2017 Elsevier B.V. All rights reserved.

  13. Homodinuclear lanthanide complexes of phenylthiopropionic acid: Synthesis, characterization, cytotoxicity, DNA cleavage, and antimicrobial activity

    Science.gov (United States)

    Shiju, C.; Arish, D.; Kumaresan, S.

    2013-03-01

    Lanthanide complexes of La(III), Pr(III), Nd(III), Sm(III), and Ho(III) with phenylthiopropionic acid were synthesized and characterized by elemental analysis, mass, IR, electronic spectra, molar conductance, TGA, and powder XRD. The results show that the lanthanide complexes are homodinuclear in nature. The two lanthanide ions are bridged by eight oxygen atoms from four carboxylate groups. Thermal decomposition profiles are consistent with the proposed formulations. Powder XRD studies show that all the complexes are amorphous in nature. Antimicrobial studies indicate that these complexes exhibit more activity than the ligand itself. The DNA cleavage activity of the ligand and its complexes were assayed on Escherichia coli DNA using gel electrophoresis in the presence of H2O2. The result shows that the Pr(III) and Nd(III) complexes have completely cleaved the DNA. The anticancer activities of the complexes have also been studied towards human cervical cancer cell line (HeLa) and colon cancer cells (HCT116) and it was found that the La(III) and Nd(III) complexes are more active than the corresponding Pr(III), Sm(III), Ho(III) complexes, and the free ligand on both the cancer cells.

  14. Synthesis, Docking and Biological Activities of Novel Hybrids Celecoxib and Anthraquinone Analogs as Potent Cytotoxic Agents

    Directory of Open Access Journals (Sweden)

    Maha S. Almutairi

    2014-12-01

    Full Text Available Herein, novel hybrid compounds of celecoxib and 2-aminoanthraquinone derivatives have been synthesized using condensation reactions of celecoxib with 2-aminoanthraquinone derivatives or 2-aminoanthraquinon with celecoxib derivatives. Celecoxib was reacted with different acid chlorides, 2-chloroethylisocyanate and bis (2-chloroethyl amine hydrochloride. These intermediates were then reacted with 2-aminoanthraquinone. Also the same different acid chlorides and 2-chloroethylisocyanate were reacted with 2-aminoanthraquinone and the resulting intermediates were reacted with celecoxib to give isomers for the previous compounds. The antitumor activities against hepatic carcinoma tumor cell line (HEPG2 have been investigated in vitro, and all these compounds showed promising activities, especially compound 3c, 7, and 12. Flexible docking studies involving AutoDock 4.2 was investigated to identify the potential binding affinities and the mode of interaction of the hybrid compounds into two protein tyrosine kinases namely, SRC (Pp60v-src and platelet-derived growth factor receptor, PDGFR (c-Kit. The compounds in this study have a preferential affinity for the c-Kit PDGFR PTK over the non-receptor tyrosine kinase SRC (Pp60v-src.

  15. Synthesis, Docking and Biological Activities of Novel Hybrids Celecoxib and Anthraquinone Analogs as Potent Cytotoxic Agents

    Science.gov (United States)

    Almutairi, Maha S.; Hegazy, Gehan H.; Haiba, Mogedda E.; Ali, Hamed I.; Khalifa, Nagy M.; Soliman, Abd El-mohsen M.

    2014-01-01

    Herein, novel hybrid compounds of celecoxib and 2-aminoanthraquinone derivatives have been synthesized using condensation reactions of celecoxib with 2-aminoanthraquinone derivatives or 2-aminoanthraquinon with celecoxib derivatives. Celecoxib was reacted with different acid chlorides, 2-chloroethylisocyanate and bis (2-chloroethyl) amine hydrochloride. These intermediates were then reacted with 2-aminoanthraquinone. Also the same different acid chlorides and 2-chloroethylisocyanate were reacted with 2-aminoanthraquinone and the resulting intermediates were reacted with celecoxib to give isomers for the previous compounds. The antitumor activities against hepatic carcinoma tumor cell line (HEPG2) have been investigated in vitro, and all these compounds showed promising activities, especially compound 3c, 7, and 12. Flexible docking studies involving AutoDock 4.2 was investigated to identify the potential binding affinities and the mode of interaction of the hybrid compounds into two protein tyrosine kinases namely, SRC (Pp60v-src) and platelet-derived growth factor receptor, PDGFR (c-Kit). The compounds in this study have a preferential affinity for the c-Kit PDGFR PTK over the non-receptor tyrosine kinase SRC (Pp60v-src). PMID:25490139

  16. Synthesis of curcumin-loaded chitosan phosphate nanoparticle and study of its cytotoxicity and antimicrobial activity.

    Science.gov (United States)

    Deka, C; Aidew, L; Devi, N; Buragohain, A K; Kakati, D K

    2016-11-01

    Curcumin has acquired an important position in the treatment of various diseases. But its use, as a chemotherapeutic agent, is limited due to its low water solubility, poor bioavailability, and its sensitive nature at the physiological pH. To overcome this, curcumin was loaded into chitosan phosphate nanoparticles (CPNs). The loading efficiency was found to be 84%. DLS studies revealed the average particle size of CPNs and curcumin-loaded CPNs as 53 and 91 nm, respectively, and TEM results supplemented these values. A sustained release pattern was noticed and the amount of curcumin released in acidic pH was higher than at physiological pH. The curcumin nanoformulation exhibited proficient activity against both Gram-positive and Gram-negative bacteria as well as fungus. Cytocompatibility of the nanoformulations against peripheral blood mononuclear cells (PBMCs) and murine monocyte-macrophage cell line was confirmed by incubating with PBMCs and murine monocyte-macrophage cell line.

  17. 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.

  18. 7-Chloroquinolinotriazoles: synthesis by the azide-alkyne cycloaddition click chemistry, antimalarial activity, cytotoxicity and SAR studies.

    Science.gov (United States)

    Pereira, Guilherme R; Brandão, Geraldo Célio; Arantes, Lucas M; de Oliveira, Háliton A; de Paula, Renata Cristina; do Nascimento, Maria Fernanda A; dos Santos, Fábio M; da Rocha, Ramon K; Lopes, Júlio César D; de Oliveira, Alaíde Braga

    2014-02-12

    Twenty-seven 7-chloroquinolinotriazole derivatives with different substituents in the triazole moiety were synthesized via copper-catalyzed cycloaddition (CuAAC) click chemistry between 4-azido-7-chloroquinoline and several alkynes. All the synthetic compounds were evaluated for their in vitro activity against Plasmodium falciparum (W2) and cytotoxicity to Hep G2A16 cells. All the products disclosed low cytotoxicity (CC50 > 100 μM) and five of them have shown moderate antimalarial activity (IC50 from 9.6 to 40.9 μM). As chloroquine analogs it was expected that these compounds might inhibit the heme polymerization and SAR studies were performed aiming to explain their antimalarial profile. New structural variations can be designed on the basis of the results obtained. Copyright © 2013 Elsevier Masson SAS. All rights reserved.

  19. Synthesis and biological activity of chimeric structures derived from the cytotoxic natural compounds dolastatin 10 and dolastatin 15.

    Science.gov (United States)

    Poncet, J; Busquet, M; Roux, F; Pierré, A; Atassi, G; Jouin, P

    1998-04-23

    The natural cytotoxic compounds dolastatins 10 and 15 exhibit great similarities in structure and in their biological activity profiles. Two compounds (1 and 2) formed by interchanging the dolaisoleuine residue of dolastatin 10 and the MeVal-Pro dipeptide of dolastatin 15 were synthesized in order to evaluate the possible equivalence of these units. These compounds can be considered as chimeras of dolastatins 10 and 15 formed by the N-terminal part of the former and the C-terminal part of the latter and vice versa. Both analogues exhibited a marked decrease in their cytotoxic activity but showed similar differential cytotoxicity with regard to the cell lines assayed compared with the parent compounds. HT-29 cell line was the least sensitive one. However, this activity was in the nanomolar level and close to that of vincristine. The differences in their effect on tubulin polymerization were less pronounced. We confirmed the already known crucial role of the Dil residue in this assay. The nonequivalence of the Dil unit and the MeVal-Pro dipeptide probably reflects modification in the relative positions of the N-dimethylamino and the phenyl moieties.

  20. Green synthesis and characterization of silver nanoparticles using alcoholic flower extract of Nyctanthes arbortristis and in vitro investigation of their antibacterial and cytotoxic activities

    International Nuclear Information System (INIS)

    Gogoi, Nayanmoni; Babu, Punuri Jayasekhar; Mahanta, Chandan; Bora, Utpal

    2015-01-01

    Here we report the synthesis of silver nanoparticles using ethanolic flower extract of Nyctanthes arbortristis, UVvisible spectra and TEM indicated the successful formation of silver nanoparticles. Crystalline nature of the silver nanoparticles was confirmed by X-ray diffraction. Fourier Transform Infra-Red Spectroscopy analysis established the capping of the synthesized silver nanoparticles with phytochemicals naturally occurring in the ethanolic flower extract of N. arbortristis. The synthesized silver nanoparticles showed antibacterial activity against the pathogenic strain of Escherichia coli MTCC 443. Furthermore, cytotoxicity of the silver nanoparticles was tested on mouse fibroblastic cell line (L929) and found to be non-toxic, which thus proved their biocompatibility. Antibacterial activity and cytotoxicity assay carried out in this study open up an important perspective of the synthesized silver nanoparticles. - Highlights: • The present study depicts the green synthesis of AgNPs using Nyctanthes arbortristis. • AuNPs found to be biocompatible and can be used for biomedical applications. • The FTIR, TGA and DTA results showed that AgNPs are bounded by organic coating. • The synthesized AgNPs showed antibacterial activity on E. Coli MTCC 443. • We investigated the antioxidant activity for both EFE and AgNPs

  1. Synthesis and Characterization of Silver Nanoparticles Using Cannonball Leaves and Their Cytotoxic Activity against MCF-7 Cell Line

    International Nuclear Information System (INIS)

    Devaraj, P.; Kumari, P.; Aarti, Ch.; Renganathan, A.

    2013-01-01

    Cannonball (Couroupita guianensis) is a tree belonging to the family Lecythidaceae. Various parts of the tree have been reported to contain oils, keto steroids, glycosides, couroupitine, indirubin, isatin, and phenolic substances. We report here the synthesis of silver nanoparticles (AgNPs) using cannonball leaves. Green synthesized nanoparticles have been characterized by UV-Vis spectroscopy, SEM, TEM, and FTIR. Cannonball leaf broth as a reducing agent converts silver ions to AgNPs in a rapid and eco friendly manner. The UV-Vis spectra gave surface plasmon resonance peak at 434 nm. TEM image shows well-dispersed silver nanoparticles with an average particle size of 28.4 nm. FTIR showed the structure and respective bands of the synthesized nanoparticles and the stretch of bonds. Green synthesized silver nanoparticles by cannonball leaf extract show cytotoxicity to human breast cancer cell line (MCF-7). Overall, this environmentally friendly method of biological silver nanoparticles production provides rates of synthesis faster than or comparable to those of chemical methods and can potentially be used in various human contacting areas such as cosmetics, foods, and medical applications.

  2. Synthesis and Cytotoxicity of Novel Hexahydrothienocycloheptapyridazinone Derivatives

    Directory of Open Access Journals (Sweden)

    Irene Marchesi

    2009-09-01

    Full Text Available Designed as a new group of tricyclic molecules containing the thienocycloheptapyridazinone ring system, a number of 2N-substituted-hexahydrothienocycloheptapyridazinone derivatives were synthesized and their biological activity evaluated. Among the synthesized compounds, derivatives 7d and 7h were found to possess cytotoxic activity against non-small cell lung cancer and central nervous system cancer cell lines, respectively.

  3. Novel synthesis of nanosilver particles using plant active principle aloin and evaluation of their cytotoxic effect against Staphylococcus aureus

    Directory of Open Access Journals (Sweden)

    Thota Venkata Chaitanya Kumar

    2014-02-01

    Full Text Available Objective: To develop a reliable, eco-friendly and easy process for the synthesis of silver nanoparticles using aloin, the active principle of medicinal plant ‘Aloe vera ’ and to evaluate antimicrobial activity against Staphylococcus aureus (S. aureus, a causative organism of most of the diseases in livestock and to standardize the level of safety of synthesized silver nanoparticles. Methods: Characterization using UV-vis spectrophotometry, DLS technique, FT-IR and SEM. Tube dilution method was carried out to evaluate the MIC of the compound against S. aureus. MTT assay was performed to evaluate the level of safety of nanoparticles. Results: UV-vis absorption spectrum showed a maximum absorption around 200 nm for aloin mediated silver nanoparticles (ANS. The size of the particles as measured by DLS technique was 67.8 nm. The results of FT-IR analysis indicated the involvement of hydroxyl, carboxyl, amine and nitrile groups in the synthesis and stabilization of aloin mediated silver nanoparticles. SEM images showed that ANS with cubical, rectangular, triangular and spherical morphology and measured sizes of the agglomerated nanoparticles are in a range of 287.5 to 293.2 nm, however the average size of an individual particle is estimated to be approximately 70 nm. The compound (ANS showed a MIC of 21.8 ng/mL against S. aureus and showed an in vitro spleenocyte viability of more than 80% at the highest concentration of 87.5 mg/L per well. Conclusions: Aloin consists of functional groups which reduced Ag+ ions to Ago ions and helped in synthesis of silver nanoparticles. The synthesis process has further enhanced the antimicrobial activity of nanosilver. The compound is also proved to be safe at the level many times higher than the MIC.

  4. Synthesis, molecular docking, DFT calculations and cytotoxicity activity of benzo[g]quinazoline derivatives in choline chloride-urea

    Science.gov (United States)

    Lakshmanan, Sivalingam; Govindaraj, Dharman; Ramalakshmi, Narayanan; Antony, S. Arul

    2017-12-01

    Green and highly efficient one-pot three component approach for the synthesis of benzo[g]quinazoline derivatives (6a-g) using Choline chloride-urea (DES). Synthesized compounds 6b and 6g showed the most potent biological activity against A549 lung cancer cell line. Docking simulation was performed to position compounds 6b and 6g showed the greater affinity for anaplastic lymphoma kinase (ALK) receptor. Quantum chemical studies were carried out on these compounds to understand the structural features essential for activity using DFT/6-31G level of theory.

  5. Synthesis and characterization of silver nanoparticles using fruit extract of Momordica cymbalaria and assessment of their in vitro antimicrobial, antioxidant and cytotoxicity activities.

    Science.gov (United States)

    Swamy, Mallappa Kumara; Akhtar, Mohd Sayeed; Mohanty, Sudipta Kumar; Sinniah, Uma Rani

    2015-12-05

    Plant mediated synthesis of nanoparticles has been considered as green route and a reliable technique for the synthesis of nanoparticles due to its eco-friendly approach. In this study, we report a simple and eco-friendly approach for the synthesis of silver nanoparticles (AgNPs) using methanolic Momordica cymbalaria fruit extract as reducing agent. The fruit extract of M. cymbalaria exposed to AgNO3 solution showed the change in color from green to light yellow at room temperature within 1h of incubation confirms the synthesis of AgNPs. UV-vis spectra analysis revealed that the synthesized AgNPs had a sharp surface plasmon resonance at around 450 nm, while, the X-ray Diffraction (XRD) patterns confirmed distinctive peaks indices to the crystalline planes of the face centered cubic silver. The Atomic Force Microscopy (AFM) and Scanning Electron Microscopy (SEM) analysis results confirmed the presence of spherical shaped AgNPs by a huge disparity in the particle size distribution with an average size of 15.5 nm. The synthesized AgNPs showed strong antibacterial activity against all the tested multidrug resistant human pathogenic bacterial strains and also exhibited highest free radical scavenging activity (74.2%) compared to fruit extract (60.4%). Moreover, both fruit extract and the synthesized AgNPs showed the cytotoxicity towards Rat L6 skeletal muscle cell line at different concentrations, but the highest inhibition percentage was recorded for AgNPs at concentration of 100 μg/ml. Copyright © 2015. Published by Elsevier B.V.

  6. Synthesis and Characterization of New Palladium(II) Thiosemicarbazone Complexes and Their Cytotoxic Activity against Various Human Tumor Cell Lines

    Science.gov (United States)

    Hernández, Wilfredo; Paz, Juan; Carrasco, Fernando; Spodine, Evgenia; Manzur, Jorge; Sieler, Joachim; Blaurock, Steffen; Beyer, Lothar

    2013-01-01

    The palladium(II) bis-chelate complexes of the type [Pd(TSC1-5)2] (6–10), with their corresponding ligands 4-phenyl-1-(acetone)-thiosemicarbazone, HTSC1 (1), 4-phenyl-1-(2′-chloro-benzaldehyde)-thiosemicarbazone, HTSC2 (2), 4-phenyl-1-(3′-hydroxy-benzaldehyde)-thiosemicarbazone, HTSC3 (3), 4-phenyl-1-(2′-naphthaldehyde)-thiosemicarbazone, HTSC4 (4), and 4-phenyl-1-(1′-nitro-2′-naphthaldehyde)-thiosemicarbazone, HTSC5 (5), were synthesized and characterized by elemental analysis and spectroscopic techniques (IR and 1H- and 13C-NMR). The molecular structure of HTSC3, HTSC4, and [Pd(TSC1)2] (6) have been determined by single crystal X-ray crystallography. Complex 6 shows a square planar geometry with two deprotonated ligands coordinated to PdII through the azomethine nitrogen and thione sulfur atoms in a cis arrangement. The in vitro cytotoxic activity measurements indicate that the palladium(II) complexes (IC50 = 0.01–9.87 μM) exhibited higher antiproliferative activity than their free ligands (IC50 = 23.48–70.86 and >250 μM) against different types of human tumor cell lines. Among all the studied palladium(II) complexes, the [Pd(TSC3)2] (8) complex exhibited high antitumor activity on the DU145 prostate carcinoma and K562 chronic myelogenous leukemia cells, with low values of the inhibitory concentration (0.01 and 0.02 μM, resp.). PMID:24391528

  7. A New Series of Pyrrole-Based Chalcones: Synthesis and Evaluation of Antimicrobial Activity, Cytotoxicity, and Genotoxicity

    Directory of Open Access Journals (Sweden)

    Ahmet Özdemir

    2017-11-01

    Full Text Available In an effort to develop new potent antimicrobial and anticancer agents, new pyrrole-based chalcones were designed and synthesized via the base-catalyzed Claisen-Schmidt condensation of 2-acetyl-1-methylpyrrole with 5-(arylfurfural derivatives. The compounds were evaluated for their in vitro antimicrobial effects on pathogenic bacteria and Candida species using microdilution and ATP luminescence microbial cell viability assays. MTT assay was performed to determine the cytotoxic effects of the compounds on A549 human lung adenocarcinoma, HepG2 human hepatocellular carcinoma, C6 rat glioma, and NIH/3T3 mouse embryonic fibroblast cell lines. 1-(1-Methyl-1H-pyrrol-2-yl-3-(5-(4-chlorophenylfuran-2-ylprop-2-en-1-one (7 and 1-(1-methyl-1H-pyrrol-2-yl-3-(5-(2,5-dichlorophenylfuran-2-ylprop-2-en-1-one (9 were found to be the most potent antifungal agents against Candida krusei and therefore these compounds were chosen for flow cytometry analysis and Ames MPF assay. ATP bioluminescence assay indicated that the antifungal activity of compounds 7 and 9 against C. krusei was significantly higher than that of other compounds and the reference drug (ketoconazole, whereas flow cytometry analysis revealed that the percentage of dead cells treated with compound 7 was more than that treated with compound 9 and ketoconazole. According to Ames MPF assay, compounds 7 and 9 were found to be non-genotoxic against TA98 and TA100 with/without metabolic activation. MTT assay indicated that 1-(1-methyl-1H-pyrrol-2-yl-3-(5-(2-nitrophenylfuran-2-ylprop-2-en-1-one (3 showed more selective anticancer activity than cisplatin against the HepG2 cell line. On the other hand, 1-(1-methyl-1H-pyrrol-2-yl-3-(5-(4-nitrophenylfuran-2-ylprop-2-en-1-one (1 was found to be more effective and selective on the A549 cell line than cisplatin.

  8. Synthesis of 2,3-diyne-1,4-naphthoquinone derivatives and evaluation of cytotoxic activity against tumor cell lines

    International Nuclear Information System (INIS)

    Silva, Mauro G.; Camara, Celso A.; Silva, Tania M.S.; Feitosa, Anderson C.S.; Meira, Assuero S.; Pessoa, Claudia

    2013-01-01

    A series of 2,3-diyne-1,4-naphthoquinone derivatives was synthesized from 2,3-dibromo- 1,4-naphthoquinone and various functionalized terminal alkynes using palladium-catalyzed Sonogashira cross-coupling reaction. The diynes were evaluated as potential cytotoxic agents against three tumor cell lines: human ovarian adenocarcinoma (OVCAR-8), human metastatic prostate cancer (PC-3M) and human bronchoalveolar lung carcinoma (NCI-H358M), presenting, in general, satisfactory results for inhibition of cell growth. (author)

  9. Synthesis of 2,3-diyne-1,4-naphthoquinone derivatives and evaluation of cytotoxic activity against tumor cell lines

    Energy Technology Data Exchange (ETDEWEB)

    Silva, Mauro G.; Camara, Celso A.; Silva, Tania M.S., E-mail: ccelso@dcm.ufrpe.br [Universidade Federal Rural de Pernambuco (LSCB/UFRPE), Recife, PE (Brazil). Dept. de Ciencias Moleculares. Lab. de Sintese de Compostos Bioativos; Feitosa, Anderson C.S.; Meira, Assuero S.; Pessoa, Claudia [Universidade Federal do Ceara (LOE/UFC), Fortaleza, CE (Brazil). Dept. de Fisiologia e Farmacologia. Lab. de Oncologia Experimental

    2013-09-15

    A series of 2,3-diyne-1,4-naphthoquinone derivatives was synthesized from 2,3-dibromo- 1,4-naphthoquinone and various functionalized terminal alkynes using palladium-catalyzed Sonogashira cross-coupling reaction. The diynes were evaluated as potential cytotoxic agents against three tumor cell lines: human ovarian adenocarcinoma (OVCAR-8), human metastatic prostate cancer (PC-3M) and human bronchoalveolar lung carcinoma (NCI-H358M), presenting, in general, satisfactory results for inhibition of cell growth. (author)

  10. Green synthesis of silver nanoparticles using Pimpinella anisum seeds: antimicrobial activity and cytotoxicity on human neonatal skin stromal cells and colon cancer cells

    Directory of Open Access Journals (Sweden)

    AlSalhi MS

    2016-09-01

    Full Text Available Mohamad S AlSalhi,1,2 Sandhanasamy Devanesan,1,2 Akram A Alfuraydi,3 Radhakrishnan Vishnubalaji,4 Murugan A Munusamy,3 Kadarkarai Murugan,5 Marcello Nicoletti,6 Giovanni Benelli7 1Research Chair in Laser Diagnosis of Cancers, 2Department of Physics and Astronomy, 3Department of Botany and Microbiology, College of Science, 4Stem Cell Unit, Department of Anatomy, College of Medicine, King Saud University, Riyadh, Kingdom of Saudi Arabia; 5Division of Entomology, Department of Zoology, School of Life Sciences, Bharathiar University, Coimbatore, India; 6Department of Environmental Biology, Sapienza University of Rome, Rome, 7Department of Agriculture, Food and Environment, University of Pisa, Pisa, Italy Background: The present study focused on a simple and eco-friendly method for the synthesis of silver nanoparticles (AgNPs with multipurpose anticancer and antimicrobial activities. Materials and methods: We studied a green synthesis route to produce AgNPs by using an aqueous extract of Pimpinella anisum seeds (3 mM. Their antimicrobial activity and cytotoxicity on human neonatal skin stromal cells (hSSCs and colon cancer cells (HT115 were assessed. Results: A biophysical characterization of the synthesized AgNPs was realized: the morphology of AgNPs was determined by transmission electron microscopy, energy dispersive spectroscopy, X-ray powder diffraction, and ultraviolet-vis absorption spectroscopy. Transmission electron microscopy showed spherical shapes of AgNPs of P. anisum seed extracts with a 3.2 nm minimum diameter and average diameter ranging from 3.2 to 16 nm. X-ray powder diffraction highlighted the crystalline nature of the nanoparticles, ultraviolet-vis absorption spectroscopy was used to monitor their synthesis, and Fourier transform infrared spectroscopy showed the main reducing groups from the seed extract. Energy dispersive spectroscopy was used to confirm the presence of elemental silver. We evaluated the antimicrobial potential

  11. Copper(II) Complexes of Phenanthroline and Histidine Containing Ligands: Synthesis, Characterization and Evaluation of their DNA Cleavage and Cytotoxic Activity.

    Science.gov (United States)

    Leite, Sílvia M G; Lima, Luís M P; Gama, Sofia; Mendes, Filipa; Orio, Maylis; Bento, Isabel; Paulo, António; Delgado, Rita; Iranzo, Olga

    2016-11-21

    Copper(II) complexes have been intensely investigated in a variety of diseases and pathological conditions due to their therapeutic potential. The development of these complexes requires a good knowledge of metal coordination chemistry and ligand design to control species distribution in solution and tailor the copper(II) centers in the right environment for the desired biological activity. Herein we present the synthesis and characterization of two ligands HL1 and H 2 L2 containing a phenanthroline unit (phen) attached to the amino group of histidine (His). Their copper(II) coordination properties were studied using potentiometry, spectroscopy techniques (UV-vis and EPR), mass spectrometry (ESI-MS) and DFT calculations. The data showed the formation of single copper complexes, [CuL1] + and [CuL2], with high stability within a large pH range (from 3.0 to 9.0 for [CuL1] + and from 4.5 to 10.0 for [CuL2]). In both complexes the Cu 2+ ion is bound to the phen unit, the imidazole ring and the deprotonated amide group, and displays a distorted square pyramidal geometry as confirmed by single crystal X-ray crystallography. Interestingly, despite having similar structures, these copper complexes show different redox potentials, DNA cleavage properties and cytotoxic activity against different cancer cell lines (human ovarian (A2780), its cisplatin-resistant variant (A2780cisR) and human breast (MCF7) cancer cell lines). The [CuL2] complex has lower reduction potential (E pc = -0.722 V vs -0.452 V for [CuL1] + ) but higher biological activity. These results highlight the effect of different pendant functional groups (carboxylate vs amide), placed out of the coordination sphere, in the properties of these copper complexes.

  12. Synthesis, characterization, cytotoxic and antitubercular activities of new gold(I) and gold(III) complexes containing ligands derived from carbohydrates.

    Science.gov (United States)

    Chaves, Joana Darc Souza; Damasceno, Jaqueline Lopes; Paula, Marcela Cristina Ferreira; de Oliveira, Pollyanna Francielli; Azevedo, Gustavo Chevitarese; Matos, Renato Camargo; Lourenço, Maria Cristina S; Tavares, Denise Crispim; Silva, Heveline; Fontes, Ana Paula Soares; de Almeida, Mauro Vieira

    2015-10-01

    Novel gold(I) and gold(III) complexes containing derivatives of D-galactose, D-ribose and D-glucono-1,5-lactone as ligands were synthesized and characterized by IR, (1)H, and (13)C NMR, high resolution mass spectra and cyclic voltammetry. The compounds were evaluated in vitro for their cytotoxicity against three types of tumor cells: cervical carcinoma (HeLa) breast adenocarcinoma (MCF-7) and glioblastoma (MO59J) and one non-tumor cell line: human lung fibroblasts (GM07492A). Their antitubercular activity was evaluated as well expressed as the minimum inhibitory concentration (MIC90) in μg/mL. In general, the gold(I) complexes were more active than gold(III) complexes, for example, the gold(I) complex (1) was about 8.8 times and 7.6 times more cytotoxic than gold(III) complex (8) in MO59J and MCF-7 cells, respectively. Ribose and alkyl phosphine derivative complexes were more active than galactose and aryl phosphine complexes. The presence of a thiazolidine ring did not improve the cytotoxicity. The study of the cytotoxic activity revealed effective antitumor activities for the gold(I) complexes, being more active than cisplatin in all the tested tumor cell lines. Gold(I) compounds (1), (2), (3), (4) and (6) exhibited relevant antitubercular activity even when compared with first line drugs such as rifampicin.

  13. Synthesis, characterization, antioxidant and brine shrimp cytotoxic activity of novel 3-benzothioyl-1-(3-hydroxy-3-phenyl -3-propyl)-1-methylthiourea.

    Science.gov (United States)

    Shoaib, Mohammad; Ullah, Abid; Shah, Syed Wadood Ali; Tahir, Muhammad Nawaz

    2017-07-01

    In the present research work novel ephedrine based thiourea derivative, 3-benzothioyl-1-(3-hydroxy-3-phenyl -3-propyl)-1-methylthiourea 4is synthesized and then characterized elemental analyzed via various techniques i.e., Proton NMR, carbon13 NMR and fatherly confirmed via X-ray crystallography. Compound 4 was then screened for their possible antioxidant and cytotoxic potentials. Benzoyl chloride was treated with an equimolar potassium thiocyanate in acetone to achieve benzoyl isothiocyantes. It was then treated with an equimolar (1R, 2S)-(-)-Ephedrine to obtain the 3-benzothioyl-1-(3-hydroxy-3-phenyl-3-propyl)-1-methyl thiourea4. It was then screened for antioxidant and cytotoxic potentials. The compound 4 showed excellent antioxidant activity almost comparable to ascorbic acid (standard) and have significant cytotoxic activity with LC 50 value 05±0.58 ppm.

  14. Synthesis of dihydropyrimidin-2-one/thione library and cytotoxic activity against the human U138-MG and Rat C6 glioma cell lines

    International Nuclear Information System (INIS)

    Canto, Romulo F.S.; Eifler-Lima, Vera Lucia; Bernardi, Andressa; Battastini, Ana Maria O.; Russowsky, Dennis

    2011-01-01

    Two series of 4-aryl-3,4-dihydropyrimidin-2(1H)-(thio)ones including monastrol (1a), have been synthesized by an environment-friendly methodology based on the combined use of citric acid or oxalic acid and TEOF (triethylorthoformate). The library was evaluated as inhibitor of cell proliferation on two glioma cell lines (human-U138-MG and Rat-C6). The compounds derived from thiourea 1f and 1d were more cytotoxic than monastrol. The compound derived from urea 2d showed the highest cytotoxic activity among the analyzed compounds. (author)

  15. SYNTHESIS AND CYTOTOXICITY OF NOVEL LIGNANS

    NARCIS (Netherlands)

    Middel, O; Woerdenbag, H.J.; van Uden, W.; van Oeveren, A.; Jansen, J.F.G.A.; Feringa, B.L.; Konings, A.WT; Pras, N.; Kellogg, R.M

    1995-01-01

    In this study the syntheses of 11 novel lignans are described. Their cytotoxicities are studied in GLC(4), a human small cell lung carcinoma cell line, using the microculture tetrazolium (MTT) assay. Ten of these compounds were substituted with a menthyloxy group on the 5-position of the lactone.

  16. Chlorpromazine inhibits tumour necrosis factor synthesis and cytotoxicity in vitro.

    Science.gov (United States)

    Zinetti, M; Galli, G; Demitri, M T; Fantuzzi, G; Minto, M; Ghezzi, P; Alzani, R; Cozzi, E; Fratelli, M

    1995-11-01

    Chlorpromazine (CPZ) has been previously shown to protect against endotoxin [lipopolysaccharide (LPS)] lethality and inhibit the release of tumour necrosis factor in vivo. We investigated at the cellular level whether this was due to direct inhibition of tumour necrosis factor-alpha (TNF-alpha) synthesis, using LPS-stimulated THP-1 human monocytic leukemia cells. We also studied the effect of CPZ on human TNF-alpha action by assessing TNF-alpha cytotoxicity on mouse fibrosarcoma L929 cells. CPZ (1-100 microM) inhibited TNF-alpha production in THP-1 cells in a dose dependent manner by a maximum of 80%. This effect was comparable to that of two well-known inhibitory drugs, dexamethasone and cyclicAMP. Inhibition was also evident at the mRNA level. On the other hand CPZ (10-25 microM) also inhibited TNF-alpha activity: in fact it reduced the cytotoxicity of TNF-alpha on L929 cells (EC50 was increased four times) and could provide protection even as a post-treatment. CPZ inhibited TNF-induced apoptosis in L929 cells, as detected by analysis of nuclear morphology. However, since we showed that apoptosis was very limited, and was not the main mode of cell death in our conditions, this could not explain the overall protection. Since CPZ did not interfere with either the oligomerization state of TNF-alpha or its receptor binding, our data suggest that it reduced cytotoxicity by inhibiting some steps in the TNF-alpha signalling pathways.

  17. Synthesis, antimicrobial and cytotoxic activities of 5-benzylidene-2-[(pyridine-4-ylmethylenehydrazono]-thiazolidin-4-one and 2-[(pyridine-4-ylmethylene hydrazono]-thiazolidin-4-one derivatives

    Directory of Open Access Journals (Sweden)

    Danniel Delmondes Feitoza

    2012-01-01

    Full Text Available A new series of 5-benzylidene-2-[(pyridine-4-ylmethylenehydrazono]-thiazolidin-4-ones 4a-l have been synthesized. These compounds were designed by a molecular hybridization approach. 2-[(Pyridine-4-ylmethylenehydrazono]-thiazolidin-4-ones 3a-d were also obtained and used as intermediates to give the target compounds. The in vitro antimicrobial and cytotoxic activities were evaluated for both series. The intermediate 3b showed considerable antibiotic activity against B. subtilis and C. albicans. In the cytotoxic activity compounds 3b (IC50= 4.25 ± 0.36 µg/mL and 4l (IC50= 1.38 ± 0.04 µg/mL were effective for inhibition of human erythromyeloblastoid leukemia (K-562 and human lung carcinoma (NCI-H292 cell lines, respectively.

  18. Synthesis, antimicrobial and cytotoxic activities of 5-benzylidene-2-[(pyridine-4-ylmethylene)hydrazono]-thiazolidin-4-one and 2-[(pyridine-4-ylmethylene) hydrazono]-thiazolidin-4-one derivatives

    Energy Technology Data Exchange (ETDEWEB)

    Feitoza, Danniel Delmondes; Alves, Antonio Jose; Lima, Jose Gildo de, E-mail: jgildolima@gmail.com [Departamento de Ciencias Farmaceuticas, Universidade Federal de Pernambuco, Recife - PE (Brazil); Araujo, Janete Magali; Aguiar, Jaciana Santos; Rodrigues, Maria do Desterro; Silva, Teresinha Goncalves; Nascimento, Silene Carneiro do; Goes, Alexandre Jose da Silva [Departamento de Antibioticos, Universidade Federal de Pernambuco, Recife - PE (Brazil)

    2012-07-01

    A new series of 5-benzylidene-2-[(pyridine-4-ylmethylene)hydrazono]-thiazolidin-4-ones 4a-l have been synthesized. These compounds were designed by a molecular hybridization approach. 2-[(Pyridine-4-ylmethylene)hydrazono]-thiazolidin-4-ones 3a-d were also obtained and used as intermediates to give the target compounds. The in vitro antimicrobial and cytotoxic activities were evaluated for both series. The intermediate 3b showed considerable antibiotic activity against B. subtilis and C. albicans. In the cytotoxic activity compounds 3b (IC{sub 50} = 4.25 +- 0.36 {mu}g/mL) and 4l (IC{sub 50} = 1.38 +- 0.04 {mu}g/mL) were effective for inhibition of human erythromyeloblastoid leukemia (K-562) and human lung carcinoma (NCI-H292) cell lines, respectively. (author)

  19. Synthesis, in-vitro cytotoxicity of 1H-benzo[f]chromene derivatives and structure-activity relationships of the 1-aryl group and 9-position.

    Science.gov (United States)

    Mohamed, Hany M; Fouda, Ahmed M; Khattab, Essam S A E H; Agrody, Ahmed M El-; Afifi, Tarek H

    2017-05-01

    A series of 1H-benzo[f]chromene-2-carbonitriles was synthesized and evaluated for their cytotoxic activities against MCF-7, HCT-116, and HepG-2 cancer cells. The SAR studies reported that the substitution in the phenyl ring at 1-position of 1H-benzo[f]chromene nucleus with the specific group, H atom, or methoxy group at 9-position increases the ability of the molecule against the different cell lines.

  20. Improved synthesis of 1,3,4-thiadiazolium-2-phenylamines using microwave and ultrasound irradiation and investigation of their cytotoxic activity

    Energy Technology Data Exchange (ETDEWEB)

    Reis, Camilla Moretto dos; Miranda, Amanda Fraga; Echevarria, Aurea, E-mail: echevarr@ufrrj.b [Universidade Federal Rural do Rio de Janeiro (DQ/ICE/UFRRJ), Seropedica, RJ (Brazil). Inst. de Ciencias Exatas. Dept. de Quimica; Echevarria-Lima, Juliana [Universidade Federal do Rio de Janeiro (DI/IMPG/UFRJ), RJ (Brazil). Inst. de Microbiologia Paulo de Goes. Dept. de Imunologia

    2011-07-01

    A new and efficient synthesis of eight 1,3,4-thiadiazolium-2-phenylamine derivatives (1-8, where 8 is novel in the literature) was performed using thionyl chloride or trimethylsilyl chloride as catalysts under microwave or ultrasound irradiation. The target compounds were obtained in good yields and remarkably short times, 5 min under microwave irradiation and 10 min under ultrasound irradiation, where compared to traditional methodology (24 to 48 h at room temperature standing). The best yields were obtained using the microwave irradiation and, in general way, using thionyl chloride instead trimethylsilyl chloride. The cytotoxicity against K562 human leukemia and Daudi lymphoma lines was evaluated and showed promising results from the 4-phenyl-5-(4'-nitro-styryl)-1,3,4-thiadiazolium-2-phenylamine chloride derivative. (author)

  1. [Synthetic transformations of higher terpenoids. XXX. Synthesis and cytotoxic activity of betulonic acid amides with a piperidine or pyrrolidine nitroxide moiety].

    Science.gov (United States)

    Antimonova, A N; Petrenko, N I; Shults, E E; Polienko, Iu F; Shakirov, M M; Irtegova, I G; Pokrovskiĭ, M A; Sherman, K M; Grigor'ev, I A; Pokrovskiĭ, A G; Tolstikov, G A

    2013-01-01

    The reaction of betulonic acid chloride with 4-amino-2,2,6,6-tetramethylpeperidine-1-oxyl, 3-amino-2,2,5,5-tetramethylpyrrolidine-1-oxyl and 3-aminomethyl-2,2,5,5-tetramethylpyrrolidine-1-oxyl gave corresponding triterpenoid amides. It was found that new derivatives exhibit cytotoxic activity against tumor cells CEM-13, U-937, MT-4. CCID50 value for most activity compound--N-[3-oxolup-20(29)-en-30-yl]-(2,2,6,6-tetramethylpiperidine-4-yl)-1-oxyl--was 5.7-33.1 microM.

  2. The synthesis and characterization of poly(γ-glutamic acid)-coated magnetite nanoparticles and their effects on antibacterial activity and cytotoxicity

    International Nuclear Information System (INIS)

    Stephen Inbaraj, B; Kao, T H; Tsai, T Y; Chiu, C P; Kumar, R; Chen, B H

    2011-01-01

    Magnetite nanoparticles (MNPs) modified with sodium and calcium salts of poly(γ-glutamic acid) (NaPGA and CaPGA) were synthesized by the coprecipitation method, followed by characterization and evaluation of their antibacterial and cytotoxic effects. Superparamagnetic MNPs are particularly attractive for magnetic driving as well as bacterial biofilm and cell targeting in in vivo applications. Characterization of synthesized MNPs by the Fourier transform infrared spectra and magnetization curves confirmed the PGA coating on MNPs. The mean diameter of NaPGA- and CaPGA-coated MNPs as determined by transmission electron microscopy was 11.8 and 14 nm, respectively, while the x-ray diffraction pattern revealed the as-synthesized MNPs to be pure magnetite. Based on agar dilution assay, both NaPGA- and CaPGA-coated MNPs showed a lower minimum inhibitory concentration in Salmonella enteritidis SE 01 than the commercial antibiotics linezolid and cefaclor, but the former was effective against Escherichia coli ATCC 8739 and Staphylococcus aureus ATCC 10832, whereas the latter was effective against Escherichia coli O157:H7 TWC 01. An in vitro cytotoxicity study in human skin fibroblast cells as measured by MTT assay implied the as-synthesized MNPs to be nontoxic. This outcome demonstrated that both γ-PGA-modified MNPs are cytocompatible and possess antibacterial activity in vitro, and thereby should be useful in in vivo studies for biomedical applications.

  3. The synthesis and characterization of poly({gamma}-glutamic acid)-coated magnetite nanoparticles and their effects on antibacterial activity and cytotoxicity

    Energy Technology Data Exchange (ETDEWEB)

    Stephen Inbaraj, B; Kao, T H; Tsai, T Y; Chiu, C P; Kumar, R; Chen, B H, E-mail: 002622@mail.fju.edu.tw [Department of Food Science, Fu Jen University, Taipei 242, Taiwan (China)

    2011-02-18

    Magnetite nanoparticles (MNPs) modified with sodium and calcium salts of poly({gamma}-glutamic acid) (NaPGA and CaPGA) were synthesized by the coprecipitation method, followed by characterization and evaluation of their antibacterial and cytotoxic effects. Superparamagnetic MNPs are particularly attractive for magnetic driving as well as bacterial biofilm and cell targeting in in vivo applications. Characterization of synthesized MNPs by the Fourier transform infrared spectra and magnetization curves confirmed the PGA coating on MNPs. The mean diameter of NaPGA- and CaPGA-coated MNPs as determined by transmission electron microscopy was 11.8 and 14 nm, respectively, while the x-ray diffraction pattern revealed the as-synthesized MNPs to be pure magnetite. Based on agar dilution assay, both NaPGA- and CaPGA-coated MNPs showed a lower minimum inhibitory concentration in Salmonella enteritidis SE 01 than the commercial antibiotics linezolid and cefaclor, but the former was effective against Escherichia coli ATCC 8739 and Staphylococcus aureus ATCC 10832, whereas the latter was effective against Escherichia coli O157:H7 TWC 01. An in vitro cytotoxicity study in human skin fibroblast cells as measured by MTT assay implied the as-synthesized MNPs to be nontoxic. This outcome demonstrated that both {gamma}-PGA-modified MNPs are cytocompatible and possess antibacterial activity in vitro, and thereby should be useful in in vivo studies for biomedical applications.

  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. Synthesis, structure, DNA/protein binding, and cytotoxic activity of a rhodium(III) complex with 2,6-bis(2-benzimidazolyl)pyridine.

    Science.gov (United States)

    Esteghamat-Panah, Roya; Hadadzadeh, Hassan; Farrokhpour, Hossein; Simpson, Jim; Abdolmaleki, Amir; Abyar, Fatemeh

    2017-02-15

    A new mononuclear rhodium(III) complex, [Rh(bzimpy)Cl 3 ] (bzimpy = 2,6-bis(2-benzimidazolyl)pyridine), was synthesized and characterized by elemental analysis and spectroscopic methods. The molecular structure of the complex was confirmed by single-crystal X-ray crystallography. The interaction of the complex with fish sperm DNA (FS-DNA) was investigated by UV spectroscopy, emission titration, and viscosity measurement in order to evaluate the possible DNA-binding mode and to calculate the corresponding DNA-binding constant. The results reveal that the Rh(III) complex interacts with DNA through groove binding mode with a binding affinity on the order of 10 4 . In addition, the binding of the Rh(III) complex to bovine serum albumin (BSA) was monitored by UV-Vis and fluorescence emission spectroscopy at different temperatures. The mechanism of the complex interaction was found to be static quenching. The thermodynamic parameters (ΔH, ΔS, and ΔG) obtained from the fluorescence spectroscopy data show that van der Waals interactions and hydrogen bonds play a major role in the binding of the Rh(III) complex to BSA. For the comparison of the DNA- and BSA-binding affinities of the free bzimpy ligand with its Rh(III) complex, the absorbance titration and fluorescence quenching experiments of the free bzimpy ligand with DNA and BSA were carried out. Competitive experiments using eosin Y and ibuprofen as site markers indicated that the complex was mainly located in the hydrophobic cavity of site I of the protein. These experimental results were confirmed by the results of molecular docking. Finally, the in vitro cytotoxicity properties of the Rh(III) complex against the MCF-7, K562, and HT-29 cell lines were evaluated and compared with those of the free ligand (bzimpy). It was found that the complexation process improved the anticancer activity significantly. Copyright © 2016 Elsevier Masson SAS. All rights reserved.

  6. Synthesis and cytotoxicity evaluation of thiosemicarbazones and their thiazole derivatives

    Directory of Open Access Journals (Sweden)

    Saulo Feheiberg Pinto Braga

    Full Text Available ABSTRACT The aims of this study were to synthesize a series of thiosemicarbazones and their thiazole derivatives, to investigate their cytotoxic activity against three human cancers and normal (Vero cells cell lines, and to evaluate the pro-apoptotic potential of the most active compounds. Materials and Methods: The thiosemicarbazones were obtained by reacting an aromatic aldehyde with thiosemicarbazide (yield 71-96%, which were subjected to a cyclization with α-bromoacetophenone to yield the required thiazole heterocycles (yield 63-100%. All the synthesized compounds were screened at 50 µM concentration against three cell lines representing HL60 (promyelocytic leukemia, Jurkat (acute lymphoblastic leukemia, and MCF-7 (breast cancer. The pro-apoptotic effect was measured by flow cytometry as the percentage of cells with hypodiploid DNA. Results: Three thiazole compounds showed activity against at least one tumor cell line (IC50 = 43-76 µM and low cytotoxicity against Vero cells (IC50 > 100 M. The most active compound of this series induced 91% and 51% DNA fragmentation in HL60 and MCF-7 cell lines, respectively, suggesting that this compound triggered apoptosis in these cells. Conclusion: Among the synthesized compounds, one in particular was found to exert antiproliferative and pro-apoptotic activity on tumor cells and can be considered promising as a lead molecule for the design of new analogues with improved activity.

  7. Cytotoxicity and utility of 1-indanone in the synthesis of some new heterocycles.

    Science.gov (United States)

    Hegazi, Bahira; Mohamed, Hanan Ahmed; Dawood, Kamal Mohamed; Badria, Farid Abdel-Rahem

    2010-04-01

    Benzo[d]imidazole 3 and 1,2,4-triazin-5(2H)-one 6 were prepared by the reaction of starting ethyl (3-hydroxy-1H-inden-2-yl)(oxo)-acetate 2 with o-phenylenediamine and thiosemicarbazide respectively. Reaction of 1,4-dihydro-1-phenylindeno[1,2-c]pyrazole-3-carbohydrazide 8 with phenylisothiocyanate gave thiosemicarbazide 9, and its reaction with chloroacetic acid or phenacylbromides led to the formation of thiazolidinone-4-one 10 or 1,3-thiazoles 12a, b. The reactivity of hydrazide 8 towards fluorinated aldehyde, phthalic anhydride, and hydrazonoyl chlorides 15a, b was studied to give fluorinated hydrazones, imide bis-hydrazones 13-16. The newly synthesized compounds were screened for their cytotoxic activities and compounds 6, 8, 9 and 10 were found the most potentially cytotoxic. The detailed synthesis, spectroscopic and biological data are reported.

  8. Synthesis, antimicrobial and cytotoxicity evaluation of new cholesterol congeners

    Directory of Open Access Journals (Sweden)

    Mohamed Ramadan El Sayed Aly

    2015-10-01

    Full Text Available 3β-Azidocholest-5-ene (3 and (3β-3-(prop-2-yn-1-yloxycholest-5-ene (10 were prepared as substrates to synthesize a variety of three-motif pharmacophoric conjugates through CuAAC. Basically, these conjugates included cholesterol and 1,2,3-triazole moieties, while the third, the pharmacophore, was either a chalcone, a lipophilic residue or a carbohydrate tag. These compounds were successfully prepared in good yields and characterized by NMR, MS and IR spectroscopic techniques. Chalcone conjugate 6c showed the best antimicrobial activity, while the lactoside conjugate 27 showed the best cytotoxic effect in vitro.

  9. 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.

  10. Anti-inflammatory and cytotoxic activities of five Veronica species.

    Science.gov (United States)

    Harput, U Sebnem; Saracoglu, Iclal; Inoue, Makoto; Ogihara, Yukio

    2002-04-01

    Biological activities of five Veronica species (Scrophulariaceae), V. cymbalaria, V. hederifolia, V. pectinata var. glandulosa, V. persica and V. polita were studied for their anti-inflammatory and cytotoxic activities. Their methanol extracts showed both the inhibitory activity of nitric oxide (NO) production in lipopolysaccharide (LPS)-stimulated macrophages and cytotoxic activity against KB epidermoid carcinoma and B16 melanoma. When the methanol extracts were fractionated between water and chloroform, water fractions significantly inhibited NO production without any cytotoxicity, while chloroform fractions showed cytotoxicity dose-dependently. When the radical scavenging activity was determined using 2,2-diphenyl-1-picryl-hydrazyl (DPPH), water fractions of the five Veronica species scavenged free radicals effectively, suggesting that the inhibitory effect of this species on NO production was due to their radical scavenging activity. On the other hand, chloroform fractions of Veronica species except for V. cymbalaria showed similar cytotoxic activity against KB and B16 melanoma cells.

  11. 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 ...

  12. Cytotoxic activity of quassinoids from Eurycoma longifolia.

    Science.gov (United States)

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

    2010-07-01

    Twenty-four quassinoids isolated from Eurycoma longifolia Jack were investigated for their cytotoxicity against a panel of four different cancer cell lines, which includes three murine cell lines [colon 26-L5 carcinoma (colon 26-L5), B16-BL6 melanoma (B16-BL6), Lewis lung carcinoma (LLC)] and a human lung A549 adenocarcinoma (A549) cell line. Among the tested compounds, eurycomalactone (9) displayed the most potent activity against all the tested cell lines; colon 26-L5 (IC50 = 0.70 microM), B16-BL6 (IC50 = 0.59 microM), LLC (IC50 = 0.78 microM), and A549 (IC50 = 0.73 microM). These activities were comparable to clinically used anticancer agent doxorubicin (colon 26-L5, IC50 = 0.76 microM; B16-BL6, IC50 = 0.86 microM; LLC, IC50 = 0.80 microM; A549, IC50 = 0.66 microM).

  13. Synthesis of New Cytotoxic Aminoanthraquinone Derivatives via Nucleophilic Substitution Reactions

    Directory of Open Access Journals (Sweden)

    Hasimah Alimon

    2013-07-01

    Full Text Available Aminoanthraquinones were successfully synthesized via two reaction steps. 1,4-Dihydroxyanthraquinone (1 was first subjected to methylation, reduction and acylation to give an excellent yield of anthracene-1,4-dione (3, 1,4-dimethoxyanthracene-9,10-dione (5 and 9,10-dioxo-9,10-dihydroanthracene-1,4-diyl diacetate (7. Treatment of 1, 3, 5 and 7 with BuNH2 in the presence of PhI(OAc2 as catalyst produced seven aminoanthraquinone derivatives 1a, b, 3a, and 5a–d. Amination of 3 and 5 afforded three new aminoanthraquinones, namely 2-(butylaminoanthracene-1,4-dione (3a, 2-(butylaminoanthracene-9,10-dione (5a and 2,3-(dibutylaminoanthracene-9,10-dione (5b. All newly synthesised aminoanthraquinones were examined for their cytotoxic activity against MCF-7 (estrogen receptor positive human breast and Hep-G2 (human hepatocellular liver carcinoma cancer cells using MTT assay. Aminoanthraquinones 3a, 5a and 5b exhibited strong cytotoxicity towards both cancer cell lines (IC50 1.1–13.0 µg/mL.

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

    African Journals Online (AJOL)

    Erah

    that had maximum bactericidal activity against all the tested isolates, but showed < 30 % host cell cytotoxicity. Conclusion: The lysate of Acacia nilotica ... cytotoxic effects on human cells. EXPERIMENTAL. Plant material. Acacia nilotica Lam .... a detergent that permeabilizes eukaryotic cells and results in HBMEC damage.

  15. Facile synthesis of mPEG-luteolin-capped silver nanoparticles with antimicrobial activity and cytotoxicity to neuroblastoma SK-N-SH cells.

    Science.gov (United States)

    Qing, Weixia; Wang, Yong; Li, Xiao; Lu, Minghua; Liu, Xiuhua

    2017-12-01

    We firstly report a facile route for the green synthesis of mPEG-luteolin-capped silver nanoparticles (mPEG-luteolin-AgNPs) using mPEG-luteolin as both the reducer and stabilizer. The reaction was carried out in a stirred aqueous solution at 50°C without additional poisonous reagents. The prepared mPEG-luteolin-AgNPs was characterized by scanning electron microscope (SEM), transmission electron microscopy (TEM), fourier transform infrared spectroscopy (FTIR), X-ray powder diffraction (XRD), zeta potential and UV-vis (UV-vis) spectrum, respectively. The proportions of mPEG-luteolin capped silver nanoparticles is about 89.9%, and the content of silver is 6.65%. The mPEG-luteolin-AgNPs was evaluated the antimicrobial effects on Staphlococcus aureus, Extended spectrum β-Lactamases Staphlococcus aureus, Escherichia Coli and Extended spectrum β-Lactamases Escherichia Coli using drilling hole method. The results showed that both gram-positive and gram-negative bacteria were killed by the mPEG-luteolin-AgNPs at low concentration. Meanwhile, the cell viability assay demonstrated that mPEG-luteolin-AgNPs had toxic effects on human neuroblastoma SK-N-SH cells. Copyright © 2017 Elsevier B.V. All rights reserved.

  16. Design and synthesis of thienopyrimidine urea derivatives with potential cytotoxic and pro-apoptotic activity against breast cancer cell line MCF-7.

    Science.gov (United States)

    Abdelhaleem, Eman F; Abdelhameid, Mohammed K; Kassab, Asmaa E; Kandeel, Manal M

    2018-01-01

    A series of novel tetrahydrobenzothieno[2,3-d]pyrimidine urea derivatives was synthesized according to fragment-based design strategy. They were evaluated for their anticancer activity against MCF-7 cell line. Three compounds 9c, 9d and 11b showed 1.5-1.03 folds more potent anticancer activity than doxorubicin. In this study, a promising multi-sited enzyme small molecule inhibitor 9c, which showed the most potent anti-proliferative activity, was identified. The anti-proliferative activity of this compound appears to correlate well with its ability to inhibit topoisomerase II (IC 50  = 9.29 μM). Moreover, compound 9c showed excellent VEGFR-2 inhibitory activity, at the sub-micromolar level with IC 50 value 0.2 μM, which is 2.1 folds more potent than sorafenib. Moreover, activation of damage response pathway of the DNA leads to cell cycle arrest at G2/M phase, accumulation of cells in pre-G1 phase and annexin-V and propidium iodide staining, indicating that cell death proceeds through an apoptotic mechanism. Compound 9c showed potent pro-apoptotic effect through induction of the intrinsic mitochondrial pathway of apoptosis. This mechanistic pathway was confirmed by a significant increase in the expression of the tumor suppressor gene p53, elevation in Bax/BCL-2 ratio and a significant increase in the level of active caspase-3. Quantitative structure-activity relationship (QSAR) studies delivered equations of five 3D descriptors with R 2  = 0.814. This QSAR model provides an effective technique for understanding the observed antitumor properties and thus could be adopted for developing effective lead structures. Copyright © 2017 Elsevier Masson SAS. All rights reserved.

  17. 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.

  18. Synthesis and structure-activity relationship study of cytotoxic lupane-type 3 beta-O-monodesmosidic saponins with an extended C-28 side chain

    Czech Academy of Sciences Publication Activity Database

    Cmoch, P.; Korda, A.; Rárová, Lucie; Oklešťková, Jana; Strnad, Miroslav; Luboradzki, R.; Pakulski, Z.

    2014-01-01

    Roč. 70, č. 17 (2014), s. 2717-2730 ISSN 0040-4020 R&D Projects: GA MŠk(CZ) LO1204 Institutional support: RVO:61389030 Keywords : BETULIN DERIVATIVES * SECONDARY ALCOHOLS * ANTITUMOR-ACTIVITY Subject RIV: EB - Genetics ; Molecular Biology Impact factor: 2.641, year: 2014

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

    African Journals Online (AJOL)

    Materials and Methods: The plants were screened for the presence of coumarins, alkaloids, flavonoids, anthraquinones, steroids and terpenoids using thin layer chromatography. Anticancer screening was performed on a panel of three cancer cell lines, while cytotoxicity was determined using a human fibroblast cell line, ...

  20. Synthesis of Substituted Thieno[2,3-d]pyrimidin-4-ones and Their Testing for Evaluation of Cytotoxic Activity on Mammalian Cell Models

    Directory of Open Access Journals (Sweden)

    Kh. A. Bozorov

    2013-01-01

    Full Text Available From 2-amino-3-ethoxycarbonyl-4,5-dimethyl-, -polymethylenethiophenes (1-4 were synthesized 2,3-disubstituted thieno[2,3-d]dihydropyrrolo-, tetrahydropyrido-, and tetrahydroazepino[1,2-a]pyrimidin-4-ones (5-16 for pharmacological investigations. The 12 compounds (5-16 were individually evaluated for their antiproliferative activities on mammalian cancer cell models. All tested compounds showed weak affection on human cervix adenocarcinoma cells (HeLa whereas some of the tested compounds exhibited more consistent inhibition of cell growth on murine myeloma cells (P3X. In both cases some compounds enhanced cell proliferation.

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

    African Journals Online (AJOL)

    plant were tested for cytotoxicity against four cancer cells, viz, MCF-7 (oestrogen ... Results: The methanol extract showed the highest antioxidant activity (DPPH, half maximal inhibitory .... Total flavonoid content was determined using the.

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

    African Journals Online (AJOL)

    Antimycobacterial and cytotoxic activities of extracts from fungal isolates of Lake Magadi. Keno David Kowanga, Joan John Eliona Munissi, Rose Masalu, Stephen Samwel Nyandoro, Pax Masimba, Erastus Gatebe ...

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

    African Journals Online (AJOL)

    ISSN: 1596-5996 (print); 1596-9827 (electronic) ... Purpose: To evaluate the leishmanicidal and cytotoxic activity of alcohol and non-alcohol extracts and .... each) in a percolator at room temperature and ..... nitric oxide-dependent mechanism.

  4. Antiviral and cytotoxic activities of some Indonesian plants.

    Science.gov (United States)

    Lohézic-Le Dévéhat, F; Bakhtiar, A; Bézivin, C; Amoros, M; Boustie, J

    2002-08-01

    Ten methanolic extracts from eight Indonesian medicinal plants were phytochemically screened and evaluated for antiviral (HSV-1 and Poliovirus) and cytotoxic activities on murine and human cancer lines (3LL, L1210, K562, U251, DU145, MCF-7). Besides Melastoma malabathricum (Melastomataceae), the Indonesian Loranthaceae species among which Elytranthe tubaeflora, E. maingayi, E. globosa and Scurrula ferruginea exhibited attractive antiviral and cytotoxic activities. Piper aduncum (Piperaceae) was found active on Poliovirus. S. ferruginea was selected for further studies because of its activity on the U251 glioblastoma cells.

  5. 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.

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

    Directory of Open Access Journals (Sweden)

    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.

  7. Palladium(II)-Stabilized Pyridine-2-Diazotates: Synthesis, Structural Characterization, and Cytotoxicity Studies.

    Science.gov (United States)

    Tskhovrebov, Alexander G; Vasileva, Anna A; Goddard, Richard; Riedel, Tina; Dyson, Paul J; Mikhaylov, Vladimir N; Serebryanskaya, Tatiyana V; Sorokoumov, Viktor N; Haukka, Matti

    2018-02-05

    Well-defined diazotates are scarce. Here we report the synthesis of unprecedented homoleptic palladium(II) diazotate complexes. The palladium(II)-mediated nitrosylation of 2-aminopyridines with NaNO 2 results in the formation of metal-stabilized diazotates, which were found to be cytotoxic to human ovarian cancer cells.

  8. Cytotoxic activity and phytochemical analysis of Arum palaestinum Boiss.

    Directory of Open Access Journals (Sweden)

    Mai Mohammed Farid

    2015-11-01

    Conclusions: The present study is considered to be the first report on the cytotoxic activities carried out on different selected fractions and pure compounds of A. palaestinum to provide evidences for its strong antitumor activities. In addition, chrysoeriol and isovitexin compounds were isolated for the first time from the studied taxa.

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

    African Journals Online (AJOL)

    inverted microscopy and DNA fragmentation using agarose gel electrophoresis. Results: P. ... However, further studies are needed to isolate the active compounds responsible for the cytotoxic ..... D-E: TL at 500 and 4,000 μg/mL. Arrows ...

  10. Activation of cytotoxic lymphocytes in patients with scrub typhus

    NARCIS (Netherlands)

    de Fost, Maaike; Chierakul, Wirongrong; Pimda, Kriangsak; Dondorp, Arjen M.; White, Nicholas J.; van der Poll, Tom

    2005-01-01

    Thai patients with scrub typhus caused by the intracellular pathogen Orientia tsutsugamushi displayed elevated plasma concentrations of granzymes A and B, interferon-gamma (IFN)-gamma-inducible protein 10, and monokine induced by IFN-gamma. These data suggest that activation of cytotoxic lymphocytes

  11. 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 ...

  12. Synthesis, Characterization, and Cytotoxicity of Iron Oxide Nanoparticles

    Directory of Open Access Journals (Sweden)

    S. Kanagesan

    2013-01-01

    Full Text Available In order to study the response of human breast cancer cells' exposure to nanoparticle, iron oxide (α-Fe2O3 nanoparticles were synthesized by a simple low temperature combustion method using Fe(NO33·9H2O as raw material. X-ray diffraction studies confirmed that the resultant powders are pure α-Fe2O3. Transmission electron microscopy study revealed the spherical shape of the primary particles, and the size of the iron oxide nanoparticles is in the range of 19 nm. The magnetic hysteresis loops demonstrated that the sample exposed ferromagnetic behaviors with a relatively low coercivity. The cytotoxicity of α-Fe2O3 nanoparticle was also evaluated on human breast cancer cells to address the current deficient knowledge of cellular response to nanoparticle exposure.

  13. Synthesis, anti-microbial activity, cytotoxicity of some novel substituted (5-(3-(1H-benzo[d]imidazol-2-yl)-4-hydroxybenzyl)benzofuran-2-yl)(phenyl)methanone analogs.

    Science.gov (United States)

    Shankar, Bhookya; Jalapathi, Pochampally; Saikrishna, Balabadra; Perugu, Shaym; Manga, Vijjulatha

    2018-01-09

    There is a dire need for the discovery and development of new antimicrobial agents after several experiments for a better resistance of microorganisms towards antimicrobial agents become a serious health problem for a few years in the past. As benzimidazole possess various types of biological activities, it has been synthesized, in the present study, a new series of (5-(3-(1H-benzo[d]imidazol-2-yl)-4-hydroxybenzyl)benzofuran-2-yl)(phenyl)methanone analogs by using the condensation and screened for its in vitro antimicrobial activity and cytotoxicity. The synthesized (5-(3-(1H-benzo[d]imidazol-2-yl)-4-hydroxybenzyl) benzofuran-2-yl)(phenyl)methanone analogs were confirmed by IR, 1 H and 13 C-NMR, MS spectra and HRMS spectral data. The synthesized compounds were evaluated for their in vitro antimicrobial potential against Gram-positive (Bacillus subtilis, Bacillus megaterium, Staph aureus and Streptococcus pyogenes), Gram-negative (Escherichia coli, Proteus vulgaris, Proteus mirabilis and Enterobacter aerogenes) bacterial and fungal (Aspergillus niger, Candida albicans, Fusarium oxysporum, Fusarium solani) strains by disc diffusion method and the minimum inhibitory concentration (MIC) in which it has been recorded in microgram per milliliter in comparison to the reference drugs, ciprofloxacin (antibacterial) and nystatin (antifungal). Further, the cytotoxicity (IC 50 value) has also been assessed on human cervical (HeLa), Supt1 cancer cell lines by using MTT assay. The following screened compounds (4d), (4f), (4g), (4k), (4l), (4o) and (4u) were found to be the best active against all the tested bacterial and fungal strains among all the demonstrated compounds of biological study. The MIC determination was also carried out against bacteria and fungi, the compounds (4f) and (4u) are found to be exhibited excellent potent against bacteria and fungi respectively. The compounds (4f) and (4u) were shown non-toxic in nature after screened for cytotoxicity against the

  14. 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.

  15. Synthesis, spectroscopic characterization and in vitro cytotoxicities of new organometallic palladium complexes with biologically active β-diketones; Biological evaluation probing of the interaction mechanism with DNA/Protein and molecular docking

    Science.gov (United States)

    Karami, Kazem; Rafiee, Mina; Lighvan, Zohreh Mehri; Zakariazadeh, Mostafa; Faal, Ali Yeganeh; Esmaeili, Seyed-Alireza; Momtazi-Borojeni, Amir Abbas

    2018-02-01

    [Pd{(C,N)sbnd C6H4CH (CH3)NH}(CUR)] (3) and [Pd2{(C,N)sbnd C6H4CH(CH3)NH2}2(μ-N3CS2)] (4) [cur = 1,7-bis(4-hydroxy-3-methoxyphenyl)-1,6-heptadiene-3,5-dion] novel organometallic complexes with biologically active ligands have been prepared and characterized via elemental analysis, multinuclear spectroscopic techniques (1H, and 13C NMR and IR) and their biological activities, including antitumoral activity and DNA-protein interactions have been investigated. Fluorescence spectroscopy used to study the interaction of the complexes with BSA have shown the affinity of the complexes for these proteins with relatively high binding constant values and the changed secondary structure of BSA in the presence of the complexes. In the meantime, spectroscopy and competitive titration have been applied to investigate the interaction of complexes with Warfarin and Ibuprofen site markers for sites I and II, respectively, with BSA. The results have suggested that the locations of complexes 3 and 4 are sites II and I, respectively. UV-Vis spectroscopy, emission titration and helix melting methods have been used to study the interaction of these complexes with CT-DNA, indicating that complexes are bound to CT-DNA by intercalation binding mode. In addition, good cytotoxic activity against MCF-7 (human breast cancer) and JURKAT (human leukemia) cell line has been shown by both complexes whereas low cytotoxicity was exerted on normal peripheral blood mononuclear cells.

  16. Isolation, Synthesis and Structures of Cytotoxic Ginsenoside Derivatives

    Directory of Open Access Journals (Sweden)

    Yi-nan Zheng

    2007-09-01

    Full Text Available Four known ginsenosides: ginsenoside-Rb1 (1, Rb3 (2, Rd (3 and Re (4 were isolated from the methanolic extract of the traditional Chinese medicine Panax ginseng C. A. Meyer. Further enzyme reactions and chemical modifications led us to obtain ginsenoside-M1 (5 and synthesize three novel mono-esters of ginsenoside-M1, ginsenoside-DM1 (6, PM1 (7 and SM1 (8 30 - 50% of yield via a facile and green synthetic strategy. The structures were elucidated on the basis of extensive 1D- and 2DNMR, as well as high resolution ESI-TOF mass spectroscopic analyses. The isolated and synthetic compounds were tested in an anti-tumor bioassay, and compounds 5-8 showed considerable cytotoxicity (SRB against several human cancer cell lines (breast cancer MCF-7, skin melanoma SK-MEL-2 and human ovarian carcinoma B16, but moderate effects on lung carcinoma COR-L23. The other ginsenosides showed no effects.

  17. 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%.

  18. 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.

  19. Synthesis and Pharmacological Screening of Several Aroyl and Heteroaroyl Selenylacetic Acid Derivatives as Cytotoxic and Antiproliferative Agents

    Directory of Open Access Journals (Sweden)

    Carmen Sanmartín

    2009-09-01

    Full Text Available The synthesis and cytotoxic activity of a series of twenty six aroyl and heteroaroyl selenylacetic acid derivatives of general formula Ar-CO-Se-CH2-COOH or Heterar-CO-Se-CH2-COOH are reported. The synthesis was carried out by reaction of acyl chlorides with sodium hydrogen selenide, prepared in situ, and this led to the formation of sodium aroylselenides that subsequently reacted with α-bromoacetic acid to produce the corresponding selenylacetic acid derivatives. All of the compounds were tested against a prostate cancer cell line (PC-3 and some of the more active compounds were assessed against a panel of four human cancer cell lines (CCRF-CEM, HTB-54, HT-29, MCF-7 and one mammary gland-derived non-malignant cell line (184B5. Some of the compounds exhibited remarkable cytotoxic and antiproliferative activities against MCF-7 and PC-3 that were higher than those of the reference compounds doxorubicin and etoposide, respectively. For example, in MCF-7 when Ar = phenyl, 3,5-dimethoxyphenyl or benzyl the TGI values were 3.69, 4.18 and 6.19 μM. On the other hand, in PC-3 these compounds showed values of 6.8, 4.0 and 2.9 μM. Furthermore, benzoylselenylacetic acid did not provoke apoptosis nor did it perturb the cell cycle in MCF-7.

  20. Cytotoxic Activity of Coagulase-Negative Staphylococci in Bovine Mastitis

    Science.gov (United States)

    Zhang, Songlin; Maddox, Carol W.

    2000-01-01

    Secreted toxins play important roles in the pathogenesis of bacterial infections. In this study, we examined the presence of secreted cytotoxic factors of coagulase-negative staphylococci (CoNS) from bovine clinical and subclinical mastitis. A 34- to 36-kDa protein with cell-rounding cytotoxic activity was found in many CoNS strains, especially in Staphylococcus chromogenes strains. The protein caused cell detachment and cell rounding in several cell lines, including HEp-2, Int 407, CHO-K1, and Y-1 cells. Native protein recovered from nondenatured polyacrylamide gel electrophoresis showed both cytotoxic activity and casein hydrolysis activity. The purified protein had a pH optimal at 7.2 to 7.5 and a pI of 5.1 and was heat labile. The proteolytic activity could be inhibited by zinc and metal specific inhibitors such as 1,10-phenanthroline and EDTA, indicating that it is a metalloprotease. Protein mass analysis and peptide sequencing indicated that the protein is a novel metalloprotease. Different bacterial strains expressed variable levels of 34- to 36-kDa protease, which may provide an indication of strain virulence. PMID:10678913

  1. In vitro anthelmintic and cytotoxicity activities the Digitaria insularis (Poaceae).

    Science.gov (United States)

    Santos, Francianne Oliveira; de Lima, Hélimar Gonçalves; de Souza Santos, Nathália Silva; Serra, Taiane Menezes; Uzeda, Rosângela Soares; Reis, Isabella Mary Alves; Botura, Mariana Borges; Branco, Alexsandro; Batatinha, Maria José Moreira

    2017-10-15

    This study aimed to evaluate the in vitro activity of D. insularis extracts and fractions against gastrointestinal nematodes of goats and its cytotoxicity on Vero cells. The egg hatch (EHT) and larval motility (LMT) tests were conducted to investigate the anthelmintic effects of the crude hydroethanolic (CH), ethyl acetate (EA), butanolic (BT) and residual hydroethanolic (RH) extracts. The elution of the active extract (EA) on column chromatography (SiO 2 ) using organic solvents furnished six fractions (FR1 to FR6), which were also tested. Cytotoxicity was determined using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) and Trypan Blue exclusion assays. All extracts, FR2 and FR3, inhibited egg hatching in a concentration-dependent manner. The EHT led to EC 50 values (effective concentration 50%) of 0.64; 0.69; 0.77; 0.96; 0.27 and 0.65mg/mL for CH, EA, BT, RH, FR2 and FR3, respectively. However, the extracts exhibited low effect on the motility of L 3. In the cytotoxicity evaluation (MTT assay), the IC 50 (inhibitory concentration 50%) was 1.18 (EA), 1.65 (FR2) and 1.59mg/mL (FR3), which was relatively high (low toxicity) in comparison to the EC 50 values in EHT, mainly for FR2. The chemical analyses of most active fractions (FR2) by Liquid Chromatography coupled to Mass Spectrometry (LC-MS) led the characterization of the flavones tricin and diosmetin. These results showed the high anthelmintic effect and low cytotoxicity of D. insularis and also that the flavones can be probably responsible for the nematocidal activity of this plant. Copyright © 2017 Elsevier B.V. All rights reserved.

  2. CYTOTOXIC AND ANTIOXIDANT ACTIVITY OF BUCKWHEAT HULL EXTRACTS

    Directory of Open Access Journals (Sweden)

    Martina Danihelová

    2013-02-01

    Full Text Available Buckwheat contains many prophylactic compounds that are concentrated mainly in outer layers of buckwheat grain. The aim of this study was to prepare buckwheat hull extracts. Ten buckwheat cultivars were screened for their antioxidant and anticancer properties. Total polyphenol content was determined using Folin-Ciocalteau's reagent. Antioxidant activity was established by the method of binding free radical DPPH. Cytotoxic properties were measured on human cervical cancer cells HeLa using mitochondrial cytotoxic test (MTT. Total polyphenol content ranged from 166.67 to 635.31 mg GAE/100 g DW. The highest content displayed tartary buckwheat cultivar Madawaska (0.64% of hulls weight. Among common buckwheat the richest in polyphenols were cultivars Bamby and KASHO-2. The best free radical binding antioxidant activity was found for cultivars with highest polyphenol content. This relationship was not observed for cytotoxic action on human cervical cancer cells. The best growth inhibitory activity on HeLa cancer cells displayed common buckwheat cultivars Bamby and KASHO-2 (up to 50%, extract concentration 100 µg/ml. This was not found for tartary buckwheat cultivar Madawaska.

  3. Modification of the cytotoxic activity of mitomycin C

    International Nuclear Information System (INIS)

    Marshall, R.S.; Rauth, A.M.

    1985-01-01

    Utilizing a system in which oxygen levels could be altered and monitored during acute drug exposures, the authors have begun to characterize the cellular and molecular damage produced by MMC in CHO cells. The cytotoxic activity of MMC decreases sharply from 0 to 0.1% oxygen in solution, while from 0.1 to 20.0% there is little change. DNA crosslinking in cells was examined under these conditions by alkaline elution and found to be directly correlated with cell killing. While hypoxia increased crosslinking, significant levels were still observed under aerobic conditions. A cell-free assay for alkylation confirmed that overall levels increase in the absence of oxygen; however, negligible alkylation was observed under aerobic conditions. It was also noted that ascorbic acid present in the exposure medium (0.284 mM) increased the aerobic cytotoxicity without altering the hypoxic cytotoxicity. The present data suggest that MMC can be activated to an alkylating species by two mechanisms, one oxygen sensitive and one oxygen insensitive and that these two mechanisms may be independently modified

  4. Antimycobacterial and cytotoxicity activity of synthetic and natural compounds

    Directory of Open Access Journals (Sweden)

    Ana O. de Souza

    2007-01-01

    Full Text Available Antimycobacterial and cytotoxicity activity of synthetic and natural compounds. Secondary metabolites from Curvularia eragrostidis and Drechslera dematioidea, Clusia sp. floral resin, alkaloids from Pilocarpus alatus, salicylideneanilines, piperidine amides, the amine 1-cinnamylpiperazine and chiral pyridinium salts were assayed on Mycobacterium tuberculosis H37Rv. N-(salicylidene-2-hydroxyaniline was the most effective compound with a minimal inhibitory concentration (MIC of 8 µmol/L. Dihydrocurvularin was moderately effective with a MIC of 40 µmol/L. Clusia sp. floral resin and a gallocatechin-epigallocatechin mixture showed MIC of 0.02 g/L and 38 µmol/L, respectively. The cytotoxicity was evaluated for N-(salicylidene-2-hydroxyaniline, curvularin, dihydrocurvularin and Clusia sp. floral resin, and the selectivity indexes were > 125, 0.47, 0.75 and 5, respectively.

  5. Antiradical and cytotoxic activity of different Helichrysum plicatum flower extracts.

    Science.gov (United States)

    Bigović, Dubravka; Savikin, Katarina; Janković, Teodora; Menković, Nebojsa; Zdunić, Gordana; Stanojković, Tatjana; Djurić, Zorica

    2011-06-01

    Flowers of Helichrysum plicatum were extracted under different experimental conditions, and their antioxidant activity was determined by DPPH radical scavenging assay. Extracts obtained with higher concentration of ethyl acetate (90% or 100%) were found to contain the greatest amount of total phenolics (> 250 mg gallic acid equivalents/g of dried extract), and high correlation between total phenolic content and antiradical activity was observed (r = -0.79). Based on the total phenolic content and antiradical activity, some extracts were selected for investigation of cytotoxic activity toward PC3, HeLa and K562 human cancer cell lines in vitro. All tested extracts exhibited moderate activity against HeLa cells (41.9-42.1 microg/mL), whereas the extract obtained with 100% ethyl acetate was the most active against K562 and PC3 cell lines (25.9 and 39.2 microg/mL, respectively). Statistical analysis revealed significant correlation between total phenolic content and cytotoxic activity against PC3 and K562 cells. HPLC identification of phenolic compounds from the extracts indicated the presence of apigenin, naringenin and kaempferol as free aglycones, and glycosides of apigenin, naringenin, quercetin and kaempferol. Among aglycones, kaempferol displayed moderate cytostatic activity against all cell lines (24.8-64.7 microM).

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

    Directory of Open Access Journals (Sweden)

    GITTITH SÁNCHEZ

    2002-01-01

    Full Text Available 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 cytotoxycity 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.

  7. Trypanocide, cytotoxic, and antifungal activities of Momordica charantia.

    Science.gov (United States)

    Santos, Karla K A; Matias, Edinardo F F; Sobral-Souza, Celestina E; Tintino, Saulo R; Morais-Braga, Maria F B; Guedes, Glaucia M M; Santos, Francisco A V; Sousa, Ana Carla A; Rolón, Miriam; Vega, Celeste; de Arias, Antonieta Rojas; Costa, José G M; Menezes, Irwin R A; Coutinho, Henrique D M

    2012-02-01

    Chagas disease, caused by Trypanosoma cruzi, is a public health problem. Currently, chemotherapy is the only available treatment for this disease, and the drugs used, nifurtimox and benzonidazol, present high toxicity levels. An alternative for replacing these drugs are natural extracts from Momordica charantia L. (Cucurbitaceae) used in traditional medicine because of their antimicrobial and biological activities. In this study, we evaluated the extract of M. charantia for its antiepimastigote, antifungal, and cytotoxic activities. An ethanol extract of leaves from M. charantia was prepared. To research in vitro antiepimastigote activity, T. cruzi CL-B5 clone was used. Epimastigotes were inoculated at a concentration of 1 × 10(5) cells/mL in 200 µl tryptose-liver infusion. For the cytotoxicity assay, J774 macrophages were used. The antifungal activity was evaluated by microdilution using strains of Candida albicans, Candida tropicalis, and Candida krusei. The effective concentration capable of killing 50% of parasites (IC(50)) was 46.06 µg/mL. The minimum inhibitory concentration (MIC) was ≤ 1024 µg/mL. Metronidazole showed a potentiation of its antifungal effect when combined with an extract of M. charantia. Our results indicate that M. charantia could be a source of plant-derived natural products with antiepimastigote and antifungal-modifying activity with moderate toxicity.

  8. Rapid green synthesis of silver nanoparticles from Chrysanthemum indicum L and its antibacterial and cytotoxic effects: an in vitro study

    Directory of Open Access Journals (Sweden)

    Arokiyaraj S

    2014-01-01

    fibroblast cells (25 µg/mL; hence, these particles were safe to use.Keywords: antibacterial activity, Chrysanthemum indicum, green synthesis, silver nanoparticle, cytotoxic

  9. 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).

  10. 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.

  11. 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.

  12. Synthesis, structures, nuclease activity, cytotoxicity, DFT and molecular docking studies of two nitrato bridged homodinuclear (Cu-Cu, Zn-Zn) complexes containing 2,2'-bipyridine and a chalcone derivative.

    Science.gov (United States)

    Gaur, Ruchi; Choubey, Diksha Kumari; Usman, Mohammad; Ward, Benzamin D; Roy, Jagat Kumar; Mishra, Lallan

    2017-08-01

    Nitrato briged dinuclear complexes of type [Cu 2 (L) 2 (bpy) 2 (NO 3 )](NO 3 )·4H 2 O, 1 and [Zn 2 (L) 2 (bpy) 2 (NO 3 )](NO 3 )·4H 2 O, 2 (L=deprotonated form of free ligand LH, [1-(2-hydroxyphenyl)-3-(9-anthracenyl) propenone; bpy=2,2'bipyridine] are synthesized and characterized using a battery of physicochemical techniques and X-ray crystallography. A distorted square pyramidal geometry is assigned to them with N 2 O 3 coordination core around the metal ion. The co-ligand L binds the metal ions through its O,O' atoms in anti-syn mode. The metal centers in complexes 1 and 2 are separated via bridging nitrato group at a distance of 6.073Å and 5.635Å respectively. Their structures and absorption spectra are supported by the computational studies using density functional theory (DFT) and TD-DFT. Both complexes exhibit nuclease activity and cleave supercoiled (form I) DNA. The complex 1 preferentially binds major groove of DNA and follows an oxidative pathway whereas complex 2 binds with minor groove of DNA via hydrolytic pathway. Both complexes inhibit topoisomerase I relaxation activity with IC 50 values of 7 and 35μM. Molecular docking studies support the groove binding and topoisomerase I binding of the complexes. The complex 1 showed a significant cytotoxicity against HeLa cell lines (a cervical cancer cell lines) in vitro with IC 50 value calculated as 2.9±0.021μM as compared to 28.2±0. 044μΜ for complex 2. Complex 2 induces the cell apoptosis at a later-stage as compared to complex 1. The cell apoptosis and topoisomerase inhibition by complexes enable them to be potential candidates as future anticancer drugs. Copyright © 2017 Elsevier B.V. All rights reserved.

  13. 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 OBOR OECD: Organic chemistry Impact factor: 1.133, year: 2016 https://www.jstage.jst.go.jp/article/cpb/65/10/65_c17-00409/_html/-char/en

  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. Synthesis and cytotoxic evaluation of novel C-10 nitrate derivatives of colchicine

    International Nuclear Information System (INIS)

    Shen, L.H.; Wang, B.; Liu, S.M.

    2016-01-01

    In our continuing search for more potent anticancer agent, eight novel nitrates couple with C-10 colchicine nitric oxide-releasing derivatives (5a-f and 7a-b) were prepared. These target compounds were assayed for their anti-tumor activity in vitro against four cancer cell lines, including human hepatocellular carcinoma cells (BEL7402), human ovary carcinoma cells (A2780), human lung adenocarcinoma cells (A549) and human breast carcinoma cells (MCF7). Preliminary results indicated that most of them exhibited significant cytotoxic effect toward cancer cells. Compound 7a was investigated further for its more potent cytotoxicity than colchicine. (author)

  16. Dillapiole as antileishmanial agent: discovery, cytotoxic activity and preliminary SAR studies of dillapiole analogues.

    Science.gov (United States)

    Parise-Filho, Roberto; Pasqualoto, Kerly Fernanda Mesquita; Magri, Fátima Maria Motter; Ferreira, Adilson Kleber; da Silva, Bárbara Athayde Vaz Galvão; Damião, Mariana Celestina Frojuello Costa Bernstorff; Tavares, Maurício Temotheo; Azevedo, Ricardo Alexandre; Auada, Aline Vivian Vatti; Polli, Michelle Carneiro; Brandt, Carlos Alberto

    2012-12-01

    In this paper, the isolation of dillapiole (1) from Piper aduncum was reported as well as the semi-synthesis of two phenylpropanoid derivatives [di-hydrodillapiole (2), isodillapiole (3)], via reduction and isomerization reactions. Also, the compounds' molecular properties (structural, electronic, hydrophobic, and steric) were calculated and investigated to establish some preliminary structure-activity relationships (SAR). Compounds were evaluated for in vitro antileishmanial activity and cytotoxic effects on fibroblast cells. Compound 1 presented inhibitory activity against Leishmania amazonensis (IC(50)  = 69.3 µM) and Leishmania brasiliensis (IC(50)  = 59.4 µM) and induced cytotoxic effects on fibroblast cells mainly in high concentrations. Compounds 2 (IC(50)  = 99.9 µM for L. amazonensis and IC(50)  = 90.5 µM for L. braziliensis) and 3 (IC(50)  = 122.9 µM for L. amazonensis and IC(50)  = 109.8 µM for L. brasiliensis) were less active than dillapiole (1). Regarding the molecular properties, the conformational arrangement of the side chain, electronic features, and the hydrophilic/hydrophobic balance seem to be relevant for explaining the antileishmanial activity of dillapiole and its analogues. Copyright © 2012 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

  17. Synthesis and biological evaluations of cytotoxic and antiangiogenic triterpenoids-jacaranone conjugates

    DEFF Research Database (Denmark)

    Sun, Hua; Yue, Partick Y. K.; Wang, Shao Rong

    2016-01-01

    showed that these conjugates are more potent in both cytotoxic and antiangiogenic assays than their corresponding parent molecules, and are also selectively more active against melanoma cells B16 and metastatic B16BL6 than the two other cancer cell lines (A549 and MCF-7) tested. The predicted...

  18. Nyctanthes arbortristis mediated synthesis of silver nanoparticles: Cytotoxicity assay against THP-1 human leukemia cell lines

    Science.gov (United States)

    Kumari, Priti; Kumari, Niraj; Jha, Anal K.; Singh, K. P.; Prasad, K.

    2018-05-01

    Green synthesis, characterizations and applications of nanoparticles have become an important branch of nanotechnology now a day. In this paper, green synthesis of silver nanoparticles (AgNPs) using the aqueous extract of Nyctanthes arbortristis as a reducing and stabilizing agent, has been discussed. Present synthetic method is very handy, cost-effective and reproducible. Formation of AgNPs was characterized by X-ray diffraction, dynamic light scattering, scanning electron microscopy and UV-visible spectroscopy techniques. The phytochemicals responsible for nano-transformation were principally flavonoids, phenols and glycosides present in the leaves. Further, the dose dependent cytotoxicity assay of biosynthesized AgNPs against THP-1 human leukemia cell lines showed the encouraging results.

  19. Antioxidant and cytotoxic activities of 'acai' (Euterpe precatoria Mart.)

    International Nuclear Information System (INIS)

    Galotta, Ana Lucia Q.A.; Boaventura, Maria Amelia D.; Lima, Luciana A. R.S.

    2008-01-01

    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 β-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-β-D-glucopyranoside in the extracts can justify the use of the plant in traditional medicine. (author)

  20. Manzamine alkaloids: isolation, cytotoxicity, antimalarial activity and SAR studies.

    Science.gov (United States)

    Ashok, Penta; Ganguly, Swastika; Murugesan, Sankaranarayanan

    2014-11-01

    The infectious disease Malaria is caused by different species of the genus Plasmodium. Resistance to quinoline antimalarial drugs and decreased susceptibility to artemisinin-based combination therapy have increased the need for novel antimalarial agents. Historically, natural products have been used for the treatment of infectious diseases. Identification of natural products and their semi-synthetic derivatives with potent antimalarial activity is an important method for developing novel antimalarial agents. Manzamine alkaloids are a unique group of β-carboline alkaloids isolated from various species of marine sponge displaying potent antimalarial activity against drug-sensitive and -resistant strains of Plasmodium. In this review, we demonstrate antimalarial potency, cytotoxicity and antimalarial SAR of manzamine alkaloids. Copyright © 2014 Elsevier Ltd. All rights reserved.

  1. 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.

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

    Science.gov (United States)

    Aronsson, Per; Munissi, Joan J E; Gruhonjic, Amra; Fitzpatrick, Paul A; Landberg, Göran; Nyandoro, Stephen S; Erdelyi, Mate

    2016-01-15

    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 (IC 50 520-82.1 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 (IC 50 16.1, 29.7 and > 100 μg/mL, respectively), and for the methanol extract of the stem bark (IC 50 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.

  3. CdS/ZnS nanocomposites: from mechanochemical synthesis to cytotoxicity issues

    International Nuclear Information System (INIS)

    Baláž, Peter; Baláž, Matej; Dutková, Erika; Zorkovská, Anna; Kováč, Jaroslav; Hronec, Pavol; Kováč, Jaroslav; Čaplovičová, Mária; Mojžiš, Ján; Mojžišová, Gabriela; Eliyas, Alexander; Kostova, Nina G.

    2016-01-01

    CdS/ZnS nanocomposites have been prepared by a two-step solid-state mechanochemical synthesis. CdS has been prepared from cadmium acetate and sodium sulfide precursors in the first step. The obtained cubic CdS (hawleyite, JCPDS 00-010-0454) was then mixed in the second step with the cubic ZnS (sphalerite, JCPDS 00-005-0566) synthesized mechanochemically from the analogous precursors. The crystallite sizes of the new type CdS/ZnS nanocomposite, calculated based on the XRD data, were 3–4 nm for both phases. The synthesized nanoparticles have been further characterized by high-resolution transmission electron microscopy (HRTEM) and micro-photoluminescence (μPL) spectroscopy. The PL emission peaks in the PL spectra are attributed to the recombination of holes/electrons in the nanocomposites occurring in depth associated with Cd, Zn vacancies and S interstitials. Their photocatalytic activity was also measured. In the photocatalytic activity tests to decolorize Methyl Orange dye aqueous solution, the process is faster and its effectivity is higher when using CdS/ZnS nanocomposite, compared to single phase CdS. Very low cytotoxic activity (high viability) of the cancer cell lines (selected as models of living cells) has been evidenced for CdS/ZnS in comparison with CdS alone. This fact is in a close relationship with Cd(II) ions dissolution tested in a physiological solution. The concentration of cadmium dissolved from CdS/ZnS nanocomposites with variable Cd:Zn ratio was 2.5–5.0 μg.mL"−"1, whereas the concentration for pure CdS was much higher — 53 μg.ml"−"1. The presence of ZnS in the nanocrystalline composite strongly reduced the release of cadmium into the physiological solution, which simulated the environment in the human body. The obtained CdS/ZnS quantum dots can serve as labeling media and co-agents in future anti-cancer drugs, because of their potential in theranostic applications. - Highlights: • CdS/ZnS nanocomposites with crystallite size 3–4

  4. CdS/ZnS nanocomposites: from mechanochemical synthesis to cytotoxicity issues

    Energy Technology Data Exchange (ETDEWEB)

    Baláž, Peter; Baláž, Matej [Institute of Geotechnics, Slovak Academy of Sciences, 04001 Košice (Slovakia); Dutková, Erika, E-mail: dutkova@saske.sk [Institute of Geotechnics, Slovak Academy of Sciences, 04001 Košice (Slovakia); Zorkovská, Anna [Institute of Geotechnics, Slovak Academy of Sciences, 04001 Košice (Slovakia); Kováč, Jaroslav; Hronec, Pavol; Kováč, Jaroslav [Institute of Electronics and Photonics, Slovak University of Technology and International Laser Centre, 81219 Bratislava (Slovakia); Čaplovičová, Mária [STU Centre for Nanodiagnostics, Slovak University of Technology, Vazovova 5, 812 43 Bratislava (Slovakia); Mojžiš, Ján; Mojžišová, Gabriela [Faculty of Medicine, P. J. Šafárik University, 04011 Košice (Slovakia); Eliyas, Alexander; Kostova, Nina G. [Institute of Catalysis, Bulgarian Academy of Sciences, 1113 Sofia (Bulgaria)

    2016-01-01

    CdS/ZnS nanocomposites have been prepared by a two-step solid-state mechanochemical synthesis. CdS has been prepared from cadmium acetate and sodium sulfide precursors in the first step. The obtained cubic CdS (hawleyite, JCPDS 00-010-0454) was then mixed in the second step with the cubic ZnS (sphalerite, JCPDS 00-005-0566) synthesized mechanochemically from the analogous precursors. The crystallite sizes of the new type CdS/ZnS nanocomposite, calculated based on the XRD data, were 3–4 nm for both phases. The synthesized nanoparticles have been further characterized by high-resolution transmission electron microscopy (HRTEM) and micro-photoluminescence (μPL) spectroscopy. The PL emission peaks in the PL spectra are attributed to the recombination of holes/electrons in the nanocomposites occurring in depth associated with Cd, Zn vacancies and S interstitials. Their photocatalytic activity was also measured. In the photocatalytic activity tests to decolorize Methyl Orange dye aqueous solution, the process is faster and its effectivity is higher when using CdS/ZnS nanocomposite, compared to single phase CdS. Very low cytotoxic activity (high viability) of the cancer cell lines (selected as models of living cells) has been evidenced for CdS/ZnS in comparison with CdS alone. This fact is in a close relationship with Cd(II) ions dissolution tested in a physiological solution. The concentration of cadmium dissolved from CdS/ZnS nanocomposites with variable Cd:Zn ratio was 2.5–5.0 μg.mL{sup −1}, whereas the concentration for pure CdS was much higher — 53 μg.ml{sup −1}. The presence of ZnS in the nanocrystalline composite strongly reduced the release of cadmium into the physiological solution, which simulated the environment in the human body. The obtained CdS/ZnS quantum dots can serve as labeling media and co-agents in future anti-cancer drugs, because of their potential in theranostic applications. - Highlights: • CdS/ZnS nanocomposites with crystallite

  5. Synthesis, antimicrobial and cytotoxicity studies of some novel modified Strobilurin derivatives

    Energy Technology Data Exchange (ETDEWEB)

    Sridhara, Ajjanna M.; Gopinath, Vadiraj S.; Bose, Prosenjit; Goud, Sanath Kumar [Advinus Therapeutics Pvt. Ltd., Bangalore (India); Reddy, Kallam R. Venugopala, E-mail: venurashmi30@rediffmail.co [Advinus Therapeutics Pvt. Ltd., Bangalore (India). Dept. of Studies in Industrial Chemistry; Keshavayya, Jathi [Advinus Therapeutics Pvt. Ltd., Bangalore (India). Dept. of Studies in Chemistry; Ambika, Dasannana Malige S. [Kuvempu University, Jnana Sahyadri, Karnataka (India). Dept. of Biochemistry; Peethambar, Sanenahalli K. [Kuvempu University, Jnana Sahyadri, Karnataka (India). Dept. of Plant Pathology

    2011-07-01

    A series of some new 3-isoxazoline substituted methyl-3-methoxy-2-(4-oxo-3,4- dihydrophthalazine-1-yl)prop-2-enoate derivatives were designed and synthesized from methyl- (4-oxo-3,4-dihydrophthalazine-1-yl)acetate, which in turn was prepared from phthalic anhydride. The structures of synthesized new compounds were characterized by spectral data and studied for their antimicrobial activities and cytotoxicity. Several of these compounds showed good antimicrobial activity (author)

  6. 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

  7. Synthesis and biological evaluation of novel conjugates of camptothecin and 5-Flurouracil as cytotoxic agents

    Energy Technology Data Exchange (ETDEWEB)

    Yang, Liu, E-mail: yqliu@lzu.edu.c [Lanzhou Jiaotong University (China). Environmental and Municipal Engineering School; Chun-Yan Zhaob; Ying-Qian Liu [Lanzhou University (China). School of Pharmacy

    2011-07-01

    A series of novel conjugates of camptothecin and 5-fluorouracil were first synthesized and their cytotoxic activities against two human tumor cell lines (SGC-7901 and A-549) as well as in vitro pharmacokinetic determination of lactone stability were studied. Among these compounds, most tested conjugates showed comparable or superior cytotoxic activities to 2, but less potent compared with 1. Particularly, conjugates 10b and 10d were highly active against A-549 with IC{sub 50} values of 0.45 and 0.38 {mu}mol L{sup -1}, respectively. Also, the in vitro pharmacokinetic determination of lactone levels of representative compound 10b showed that the biological life span of their lactone forms in human and mouse plasma significantly increased compared with their mother compound 1. Quantitative structure-activity relationship (QSAR) method was then applied for developing linear models to predict the cytotoxic activities of these derivatives that have not yet been synthesized or experimentally tested. In addition, molecular docking was used to clarify the binding mode of these derivatives to human DNA topoisomerase I. The important hydrogen-bonding interactions were observed between these derivatives and their receptor. The results from molecular modeling and QSAR study can guide the design of novel conjugates with higher antitumor activity. (author)

  8. 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.

  9. Two new alkaloids from Portulaca oleracea and their cytotoxic activities.

    Science.gov (United States)

    Tian, Jin-Long; Liang, Xiao; Gao, Pin-Yi; Li, Dan-Qi; Sun, Qian; Li, Ling-Zhi; Song, Shao-Jiang

    2014-01-01

    Two new alkaloids named (3R)-3,5-bis(3-methoxy-4-hydroxyphenyl)-2,3-dihydro-2(1H)-pyridinone (1) and 1,5-dimethyl-6-phenyl-1,2-dihydro-1,2,4-triazin-3(2H)-one (2), together with two known compounds (7'R)-N-feruloyl normetanephrine (3) and N-trans-feruloyl tyramine (4) were isolated from the air-dried aerial parts of Portulaca oleracea L. Their structures and configurations were elucidated by spectroscopic methods including 1D NMR, 2D NMR, and HR-MS techniques. In addition, compounds 1-4 were tested for in vitro cytotoxic activities against human lung (K562 and A549) and breast (MCF-7 and MDA-MB-435) cancer cell lines.

  10. The antioxidant and cytotoxic activities of Sonchus oleraceus L. extracts.

    Science.gov (United States)

    Yin, Jie; Kwon, Gu-Joong; Wang, Myeong-Hyeon

    2007-01-01

    This study investigated in vitro antioxidant activity of Sonchus oleraceus L. by extraction solvent, which were examined by reducing power, hydroxyl radical-scavenging activity(HRSA) and 1, 1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging assays. 70% MeOH extract had the greatest reducing power while EtOH extract had the greatest HRSA. The antioxidant activity of S. oleraceus extracts was concentration dependent and its IC(50) values ranged from 47.1 to 210.5 microg/ml and IC(50) of 70% MeOH, boiling water and 70% EtOH extracts were 47.1, 52.7 and 56.5 microg/ml, respectively. 70% MeOH extract of S. oleraceus contained the greatest amount of both phenolic and flavonoid contents. The extracts tested had greater nitrite scavenging effects at lower pH conditions. The cytotoxic activity showed that EtOH extract had the best activity against the growth of stomach cancer cell. These results suggest that S. oleraceus extract could be used as a potential source of natural antioxidants.

  11. Sesquiterpene lactones: Mechanism of antineoplastic activity; relationship of cellular glutathione to cytotoxicity; and disposition

    International Nuclear Information System (INIS)

    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 α 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 3 H-plenolin, no radioactive drug and/or metabolite was sequestered in the organs of BDF 1 mice. Approximately 50% of 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

  12. Synthesis of hydantoin and thiohydantoin related compounds from benzil and study of their cytotoxicity

    Directory of Open Access Journals (Sweden)

    A. Kashem Liton and M. Rabiul Islam

    2006-06-01

    Full Text Available Condensation of benzil (1 with urea, monophenyl urea and diphenyl urea in the presence of absolute ethanol using 30% aqueous NaOH gave the products 1a, 1b and 1c respectively and also with thiourea, monomethyl thiourea, dimethyl thiourea and diethyl thiourea the products 2a, 2b, 2c and 2d were obtained. Methylation of the product, 2a in the presence of dimethyl formamide (DMF using K2CO3 formed 2. The compounds 1b, 1c, 2b, 2c and 2 showed highly cytotoxic activity and the compounds 1a, 2a, 2d showed relatively low cytotoxic activity against brine shrimp lethality bioassay.

  13. Biosynthesis of Silver Nanoparticles Using Taxus yunnanensis Callus and Their Antibacterial Activity and Cytotoxicity in Human Cancer Cells

    Directory of Open Access Journals (Sweden)

    Qian Hua Xia

    2016-09-01

    Full Text Available Plant constituents could act as chelating/reducing or capping agents for synthesis of silver nanoparticles (AgNPs. The green synthesis of AgNPs has been considered as an environmental friendly and cost-effective alternative to other fabrication methods. The present work described the biosynthesis of AgNPs using callus extracts from Taxus yunnanensis and evaluated their antibacterial activities in vitro and potential cytotoxicity in cancer cells. Callus extracts were able to reduce silver nitrate at 1 mM in 10 min. Transmission electron microscope (TEM indicated the synthesized AgNPs were spherical with the size range from 6.4 to 27.2 nm. X-ray diffraction (XRD confirmed the AgNPs were in the form of nanocrystals. Fourier transform infrared spectroscopy (FTIR suggested phytochemicals in callus extracts were possible reducing and capping agents. The AgNPs exhibited effective inhibitory activity against all tested human pathogen bacteria and the inhibition against Gram-positive bacteria was stronger than that of Gram-negative bacteria. Furthermore, they exhibited stronger cytotoxic activity against human hepatoma SMMC-7721 cells and induced noticeable apoptosis in SMMC-7721 cells, but showed lower cytotoxic against normal human liver cells (HL-7702. Our results suggested that biosynthesized AgNPs could be an alternative measure in the field of antibacterial and anticancer therapeutics.

  14. Synthesis, characterization and cytotoxicity of S-nitroso-mercaptosuccinic acid-containing alginate/chitosan nanoparticles

    Science.gov (United States)

    Seabra, Amedea B.; Fabbri, Giulia K.; Pelegrino, Milena T.; Silva, Letícia C.; Rodrigues, Tiago

    2017-06-01

    Nitric oxide (NO) is an endogenous free radical, which plays key roles in several biological processes including vasodilation, neurotransmission, inhibition of platelet adhesion, cytotoxicity against pathogens, wound healing, and defense against cancer. Due to the relative instability of NO in vivo (half-life of ca. 0.5 seconds), there is an increasing interest in the development of low molecular weight NO donors, such as S-nitrosothiols (RSNOs), which are able to prolong and preserve the biological activities of NO in vivo. In order to enhance the sustained NO release in several biomedical applications, RSNOs have been successfully allied to nanomaterials. In this context, this work describes the synthesis and characterization of the NO donor S-nitroso-mercaptosuccinic acid (S-nitroso-MSA), which belongs to the class of RSNOs, and its incorporation in polymeric biodegradable nanoparticles composed by alginate/chitosan. First, chitosan nanoparticles were obtained by gelation process with sodium tripolyphosphate (TPP), followed by the addition of the alginate layer, to enhance the nanoparticle protection. The obtained nanoparticles presented a hydrodynamic diameter of 343 ± 38 nm, polydispersity index (PDI) of 0.36 ± 0.1, and zeta potential of - 30.3 ± 0.4 mV, indicating their thermal stability in aqueous suspension. The negative zeta potential value was assigned to the presence of alginate chains on the surface of chitosan/TPP nanoparticles. The encapsulation efficiency of the NO donor into the polymeric nanoparticles was found to be 98 ± 0.2%. The high encapsulation efficiency value was attributed to the positive interactions between the NO donor and the polymeric content of the nanoparticles. Kinetics of NO release from the nanoparticles revealed a spontaneous and sustained release of therapeutic amounts of NO, for several hours under physiological temperature. The incubation of NO-releasing alginate/chitosan nanoparticles with human hepatocellular carcinoma

  15. Synthesis and in vitro cytotoxicity of mPEG-SH modified gold nanorods

    Science.gov (United States)

    Didychuk, Candice L.; Ephrat, Pinhas; Belton, Michelle; Carson, Jeffrey J. L.

    2008-02-01

    Plasmon-resonant gold nanorods show great potential as an agent for contrast-enhanced biomedical imaging or for phototherapeutics. This is primarily due to the high molar extinction coefficient at the absorption maximum and the dependence of the wavelength of the absorption maximum on the aspect ratio, which is tunable in the near-infrared (NIR) during synthesis. Although gold nanorods can be produced in high-yield through the seed-mediated growth technique, the presence of residual cetyltrimethylammonium bromide (CTAB), a stabilizing surfactant required for nanorod growth, interferes with cell function and causes cytotoxicity. To overcome this potential obstacle to in vivo use, we synthesized gold nanorods and conjugated them to a methoxy (polyethylene glycol)-thiol (mPEG (5000)-SH). This approach yielded mPEG-SH modified gold nanorods with optical and morphometric properties that were similar to raw (CTAB) nanorods. Both the CTAB and mPEG-SH nanorods were tested for cytotoxicity against the HL-60 human leukemia cell line by trypan blue exclusion, and the mPEG-SH modified gold nanorods were also tested against a rat insulinoma (RIN-38) and squamous cell carcinoma (SCCVII) cell line. Cells incubated for 24 h with the mPEG-SH modified nanorods had little change in cell viability compared to cells incubated with vehicle alone. This was in contrast to cytotoxicity of CTAB nanorods on HL-60 cells. These results suggest that mPEG-SH modified gold nanorods are better suited for cell loading protocols and injection into animals and facilitate their use for imaging and phototherapeutic purposes.

  16. Piper betle-mediated synthesis, characterization, antibacterial and rat splenocyte cytotoxic effects of copper oxide nanoparticles.

    Science.gov (United States)

    Praburaman, Loganathan; Jang, Jum-Suk; Muthusamy, Govarthanan; Arumugam, Sengottaiyan; Manoharan, Koildhasan; Cho, Kwang-Min; Min, Cho; Kamala-Kannan, Seralathan; Byung-Taek, Oh

    2016-09-01

    The study reports a simple, inexpensive, and eco-friendly synthesis of copper oxide nanoparticles (CuONPs) using Piper betle leaf extract. Formation of CuONPs was confirmed by UV-visible spectroscopy at 280 nm. Transmission electron microscopy (TEM) images showed that the CuONPs were spherical, with an average size of 50-100 nm. The scanning electron microscopy (SEM)-energy dispersive spectroscopy (EDS) peak was observed approximately at 1 and 8 keV. The X-ray diffraction (XRD) studies indicated that the particles were crystalline in nature. CuONPs effectively inhibited the growth of phytopathogens Ralstonia solanacearum and Xanthomonas axonopodis. The cytotoxic effect of the synthesized CuONPs was analyzed using rat splenocytes. The cell viability was decreased to 94% at 300 μg/mL.

  17. 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 (CTD 50 , 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.

  18. Pseudomonas aeruginosa invasion and cytotoxicity are independent events, both of which involve protein tyrosine kinase activity.

    Science.gov (United States)

    Evans, D J; Frank, D W; Finck-Barbançon, V; Wu, C; Fleiszig, S M

    1998-04-01

    Pseudomonas aeruginosa clinical isolates exhibit invasive or cytotoxic phenotypes. Cytotoxic strains acquire some of the characteristics of invasive strains when a regulatory gene, exsA, that controls the expression of several extracellular proteins, is inactivated. exsA mutants are not cytotoxic and can be detected within epithelial cells by gentamicin survival assays. The purpose of this study was to determine whether epithelial cell invasion precedes and/or is essential for cytotoxicity. This was tested by measuring invasion (gentamicin survival) and cytotoxicity (trypan blue staining) of PA103 mutants deficient in specific exsA-regulated proteins and by testing the effect of drugs that inhibit invasion for their effect on cytotoxicity. A transposon mutant in the exsA-regulated extracellular factor exoU was neither cytotoxic nor invasive. Furthermore, several of the drugs that inhibited invasion did not prevent cytotoxicity. These results show that invasion and cytotoxicity are mutually exclusive events, inversely regulated by an exsA-encoded invasion inhibitor(s). Both involve host cell protein tyrosine kinase (PTK) activity, but they differ in that invasion requires Src family tyrosine kinases and calcium-calmodulin activity. PTK inhibitor drugs such as genistein may have therapeutic potential through their ability to block both invasive and cytotoxicity pathways via an action on the host cell.

  19. Aporphine and tetrahydroprotoberberine alkaloids from the leaves of Guatteria friesiana (Annonaceae) and their cytotoxic activities

    International Nuclear Information System (INIS)

    Costa, Emmanoel Vilaca; Cruz, Pedro Ernesto O. da; Marques, Francisco A.; Barison, Andersson; Maia, Beatriz Helena L.N.S.; Pinheiro, Maria Lucia B.; Ruiz, Ana Lucia T.G.; Marchetti, Gabriela M.; Carvalho, Joao Ernesto de

    2013-01-01

    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 50 values lower than 20.0 μmol L - 1 (10.5and 16.2μmolL -1 , respectively), suggesting a selective cytotoxic action (author)

  20. 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)

  1. Pure and multi metal oxide nanoparticles: synthesis, antibacterial and cytotoxic properties.

    Science.gov (United States)

    Stankic, Slavica; Suman, Sneha; Haque, Francia; Vidic, Jasmina

    2016-10-24

    Th antibacterial activity of metal oxide nanoparticles has received marked global attention as they can be specifically synthesized to exhibit significant toxicity to bacteria. The importance of their application as antibacterial agents is evident keeping in mind the limited range and effectiveness of antibiotics, on one hand, and the plethora of metal oxides, on the other, along with the propensity of nanoparticles to induce resistance being much lower than that of antibiotics. Effective inhibition against a wide range of bacteria is well known for several nano oxides consisting of one metal (Fe 3 O 4 , TiO 2 , CuO, ZnO), whereas, research in the field of multi-metal oxides still demands extensive exploration. This is understandable given that the relationship between physicochemical properties and biological activity seems to be complex and difficult to generalize even for metal oxide nanoparticles consisting of only one metal component. Also, despite the broad scope that metal oxide nanoparticles have as antibacterial agents, there arise problems in practical applications taking into account the cytotoxic effects. In this respect, the consideration of polymetallic oxides for biological applications becomes even greater since these can provide synergetic effects and unify the best physicochemical properties of their components. For instance, strong antibacterial efficiency specific of one metal oxide can be complemented by non-cytotoxicity of another. This review presents the main methods and technological advances in fabrication of nanostructured metal oxides with a particular emphasis to multi-metal oxide nanoparticles, their antibacterial effects and cytotoxicity.

  2. Synthesis and Cytotoxic Evaluation of a Series of 2-Amino-Naphthoquinones against Human Cancer Cells

    Directory of Open Access Journals (Sweden)

    Thiago A. P. de Moraes

    2014-08-01

    Full Text Available The cytotoxicity of a series of aminonaphthoquinones resulting from the reaction of suitable aminoacids with 1,4-naphthoquinone was assayed against SF-295 (glioblastoma, MDAMB-435 (breast, HCT-8 (colon, HCT-116 (colon, HL-60 (leukemia, OVCAR-8 (ovarian, NCI-H358M (bronchoalveolar lung carcinoma and PC3-M (prostate cancer cells and also against PBMC (peripheral blood mononuclear cells. The results demonstrated that all the synthetic aminonaphthoquinones had relevant cytotoxic activity against all human cancer lines used in this experiment. Five of the compounds showed high cytotoxicity and selectivity against all cancer cell lines tested (IC50 = 0.49 to 3.89 µg·mL−1. The title compounds were less toxic to PBMC, since IC50 was 1.5 to eighteen times higher (IC50 = 5.51 to 17.61 µg·mL−1 than values shown by tumour cell lines. The mechanism of cell growth inhibition and structure–activity relationships remains as a target for future investigations.

  3. Antimicrobial activity, cytotoxicity and DNA binding studies of carbon dots

    Science.gov (United States)

    Jhonsi, Mariadoss Asha; Ananth, Devanesan Arul; Nambirajan, Gayathri; Sivasudha, Thilagar; Yamini, Rekha; Bera, Soumen; Kathiravan, Arunkumar

    2018-05-01

    In recent years, quantum dots (QDs) are one of the most promising nanomaterials in life sciences community due to their unexploited potential in biomedical applications; particularly in bio-labeling and sensing. In the advanced nanomaterials, carbon dots (CDs) have shown promise in next generation bioimaging and drug delivery studies. Therefore the knowledge of the exact nature of interaction with biomolecules is of great interest to designing better biosensors. In this study, the interaction between CDs derived from tamarind and calf thymus DNA (ct-DNA) has been studied by vital spectroscopic techniques, which revealed that the CDs could interact with DNA via intercalation. The apparent association constant has been deduced from the absorption spectral changes of ct-DNA-CDs using the Benesi-Hildebrand equation. From the DNA induced emission quenching experiments the apparent DNA binding constant of the CDs (Kapp) have also been evaluated. Furthermore, we have analyzed the antibacterial and antifungal activity of CDs using disc diffusion assay method which exhibited excellent activity against E. coli and C. albicans with inhibition zone in the range of 7-12 mm. The biocompatible nature of CDs was confirmed by an in vitro cytotoxicity test on L6 normal rat myoblast cells by using MTT assay. The cell viability is not affected till the high dosage of CDs (200 μg/mL) for >48 h. As a consequence of the work, future development of CDs for microbial control and DNA sensing among the various biomolecules is possible in view of emerging biofields.

  4. Cisplatin Induces Cytotoxicity through the Mitogen-Activated Protein Kinase Pathways ana Activating Transcription Factor 3

    Directory of Open Access Journals (Sweden)

    Carly St. Germain

    2010-07-01

    Full Text Available The mechanisms underlying the proapoptotic effect of the chemotherapeutic agent, cisplatin, are largely undefined. Understanding the mechanisms regulating cisplatin cytotoxicity may uncover strategies to enhance the efficacy of this important therapeutic agent. This study evaluates the role of activating transcription factor 3 (ATF3 as a mediator of cisplatin-induced cytotoxicity. Cytotoxic doses of cisplatin and carboplatin treatments consistently induced ATF3 expression in five tumor-derived cell lines. Characterization of this induction revealed a p53, BRCA1, and integrated stress response-independent mechanism, all previously implicated in stress-mediated ATF3 induction. Analysis of mitogenactivated protein kinase (MAPK pathway involvement in ATF3 induction by cisplatin revealed a MAPK-dependent mechanism. Cisplatin treatment combined with specific inhibitors to each MAPK pathway (c-Jun N-terminal kinase, extracellularsignal-regulated kinase, and p38 resulted in decreasedATF3 induction at the protein level. MAPK pathway inhibition led to decreased ATF3 messenger RNA expression and reduced cytotoxic effects of cisplatin as measured by the 3-(4,5-dimethylthiazol-2-ylF2,5-diphenyltetrazolium bromide cell viability assay. In A549 lung carcinoma cells, targeting ATF3 with specific small hairpin RNA also attenuated the cytotoxic effects of cisplatin. Similarly, ATF3-/murine embryonic fibroblasts (MEFs were shown to be less sensitive to cisplatin-induced cytotoxicity compared with ATF3+/+ MEFs. This study identifies cisplatin as a MAPK pathway-dependent inducer of ATF3, whose expression influences cisplatin’s cytotoxic effects.

  5. Synthesis of curcumin-functionalized gold nanoparticles and cytotoxicity studies in human prostate cancer cell line

    Science.gov (United States)

    Nambiar, Shruti; Osei, Ernest; Fleck, Andre; Darko, Johnson; Mutsaers, Anthony J.; Wettig, Shawn

    2018-03-01

    Gold nanoparticles synthesized using plant extracts with medicinal properties have gained traction in recent years, especially for their use in various biomedical applications. Colloidal stability of these nanoparticles in different environments is critical to retain the expected therapeutic/diagnostic efficacy and toxicological outcome. Any change in the colloidal stability leads to dramatic changes in the physico-chemical properties of the nanoparticles such as size and surface charge, which in turn may alter the biological activity of the particles. Such changes are imminent in physiologically-relevant environment wherein interactions with different biomolecules, such as serum proteins, may modify the overall properties of the nanoparticles. In this regard, we synthesized 15 nm sized gold nanoparticles using curcumin, a plant extract from turmeric root, to evaluate cytotoxicity, uptake, and localization in human prostate cancer cells using cell-culture medium supplemented with or without fetal bovine serum (FBS). The results indicate a dramatic difference in the cytotoxicity and uptake between cells treated with curcumin-functionalized gold nanoparticles (cur-AuNPs) in cell-culture medium with and without serum. The addition of FBS to the medium not only increased the stability of the nanoparticles but also enhanced the biocompatibility (i.e. minimal cytotoxicity for a wide range of cur-AuNP concentrations). We conclude that the presence of serum proteins significantly impact the therapeutic potential of cur-AuNPs.

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

    African Journals Online (AJOL)

    Blanco Leaf Extracts Against Human Prostate Cancer Cell. Lines ... Keywords: Ficus pseudopalma, Cytotoxicity, Apopotic, human prostate PRST2 cancer cell, Lupeol,. Quercetin. ..... apoptosis through Fas-receptor mediated pathway in a ...

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

    African Journals Online (AJOL)

    2015-10-30

    Oct 30, 2015 ... Objective: Denture base materials are susceptible to fungal adhesion, which is an important .... (Shimadzu Corp., Kyoto, Japan) to achieve a wavelength ..... assay for detection of cytotoxicity and prediction of acute toxicity.

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

    African Journals Online (AJOL)

    Erah

    Keywords: Acacia nilotica, ESBLs, MRSA, E. coli, Klebsiella, Antibacterial resistance, Cytotoxicity. Received: ... infectious diseases, is an age-long practice, especially ... used in a variety of infections. ... E. coli K1 [14] and MRSA [15] were used.

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

    OpenAIRE

    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 ma...

  10. Synthesis and Cytotoxic Evaluation of 1H-1,2,3-Triazol-1-ylmethyl-2,3-dihydronaphtho[1,2-b]furan-4,5-diones

    Directory of Open Access Journals (Sweden)

    INGRID C. CHIPOLINE

    2018-02-01

    Full Text Available ABSTRACT The 1,2-naphthoquinone compound was previously considered active against solid tumors. Moreover, glycosidase inhibitors such as 1,2,3-1H triazoles has been pointed out as efficient compounds in anticancer activity studies. Thus, a series of eleven 1,2-naphthoquinones tethered in C2 to 1,2,3-1H-triazoles 9a-k were designed, synthesized and their cytotoxic activity evaluated using HCT-116 (colon adenocarcinoma, MCF-7 (breast adenocarcinoma and RPE (human nontumor cell line from retinal epithelium. The chemical synthesis was performed from C-3 allylation of lawsone followed by iodocyclization with subsequent nucleophilic displacement with sodium azide and, finally, the 1,3-dipolar cycloaddition catalyzed by Cu(I with terminal alkynes led to the formation of 1H-1,2,3-Triazol-1-ylmethyl-2,3-dihydronaphtho[1,2-b]furan-4,5-diones in good yields. Compounds containing aromatic group linked to 1,2,3-triazole ring (9c, 9d, 9e, 9i presented superior cytotoxic activity against cancer cell lines with IC50 in the range of 0.74 to 4.4 µM indicating that the presence of aromatic rings substituents in the 1,2,3-1H-triazole moiety is probably responsible for the improved cytotoxic activity.

  11. 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

    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...... 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...

  12. Cytotoxic activity of methanol extracts from Basidiomycete mushrooms on murine cancer cell lines.

    Science.gov (United States)

    Tomasi, S; Lohézic-Le Dévéhat, F; Sauleau, P; Bézivin, C; Boustie, J

    2004-04-01

    Crude methanol extracts of 58 mushroom species were screened for their cytotoxic activities against two murine cancer cell lines, L1210 and 3LL, using the tetrazolium assay. A majority of extracts (74%) exhibited IC50 > 100 microg/ml against both cell lines. A most marked activity against one of the cell lines was noted for nine species (14% of the tested species). While Amanitales and Russulales tested were not found active, Polyporales and Boletales gave better results. Four species exhibited a significant cytotoxic activity (IC50 Suillus granulatus, S. luteus). The last one had never been investigated for its cytotoxic compounds before.

  13. Linalool Exhibits Cytotoxic Effects by Activating Antitumor Immunity

    Directory of Open Access Journals (Sweden)

    Mei-Yin Chang

    2014-05-01

    Full Text Available According to recent studies, the Plantaginaceae, which are traditional Chinese herbal remedies, have potential for use in viral infection treatment and cancer therapy. Linalool and p-coumaric acid are two of the biologically active compounds that can be isolated from the Plantaginaceae. This study mainly focused on investigating the bioactivity of linalool as well as the bioactivity of p-coumaric acid in terms of their cytotoxic effects on cancer cells. Whether the mechanisms of such effects are generated through apoptosis and immunoregulatory activity were also investigated. By using WST-1 analysis, it was shown that linalool and p-coumaric acid have good inhibitory effects against breast, colorectal and liver cancer cells. The IC50 values of linalool for those cancer cell types were 224 μM, 222 μM, and 290 μM, respectively, and the IC50 values of p-coumaric acid were 693 μM, 215 μM and 87 μM, respectively. Cell cycle analysis also confirmed that linalool and p-coumaric acid can lead to apoptosis. By using flow cytometry, it was determined that treatment with linalool rather than p-coumaric acid significantly increased the sub-G1 phase and that there were more cells concentrated in the G1 phase. Furthermore, by using cytokine array analysis, we found that linalool can stimulate IFN-γ, IL-13, IL-2, IL-21, IL-21R, IL-4, IL-6sR and TNF-α secretion. This demonstrated that in addition to the bidirectional regulation capabilities found in linalool, it also induces Th1 cellular immune response in T-47D cells. These results showed that linalool holds great potential for use in cancer therapy, and we believe that it could provide an alternative way to take action against tumors.

  14. Brassinosteroids: synthesis and biological activities

    Czech Academy of Sciences Publication Activity Database

    Oklešťková, Jana; Rárová, Lucie; Kvasnica, Miroslav; Strnad, Miroslav

    2015-01-01

    Roč. 14, č. 6 (2015), s. 1053-1072 ISSN 1568-7767 R&D Projects: GA MŠk(CZ) LO1204 Institutional support: RVO:61389030 Keywords : Brassinosteroids * Chemical synthesis * Plant biological activity Subject RIV: EB - Genetics ; Molecular Biology Impact factor: 2.686, year: 2015

  15. Synthesis and cytotoxicity study of magnesium ferrite-gold core-shell nanoparticles

    International Nuclear Information System (INIS)

    Nonkumwong, Jeeranan; Pakawanit, Phakkhananan; Wipatanawin, Angkana; Jantaratana, Pongsakorn; Ananta, Supon; Srisombat, Laongnuan

    2016-01-01

    In this work, the core-magnesium ferrite (MgFe_2O_4) nanoparticles were prepared by hydrothermal technique. Completed gold (Au) shell coating on the surfaces of MgFe_2O_4 nanoparticles was obtained by varying core/shell ratios via a reduction method. Phase identification, morphological evolution, optical properties, magnetic properties and cytotoxicity to mammalian cells of these MgFe_2O_4 core coated with Au nanoparticles were examined by using a combination of X-ray diffraction, scanning electron microscopy, transmission electron microscopy (TEM), energy-dispersive X-ray spectroscopy, UV–visible spectroscopy (UV–vis), vibrating sample magnetometry and resazurin microplate assay techniques. In general, TEM images revealed different sizes of the core-shell nanoparticles generated from various core/shell ratios and confirmed the completed Au shell coating on MgFe_2O_4 core nanoparticles via suitable core/shell ratio with particle size less than 100 nm. The core-shell nanoparticle size and the quality of coating influence the optical properties of the products. The UV–vis spectra of complete coated MgFe_2O_4-Au core-shell nanoparticles exhibit the absorption bands in the near-Infrared (NIR) region indicating high potential for therapeutic applications. Based on the magnetic property measurement, it was found that the obtained MgFe_2O_4-Au core-shell nanoparticles still exhibit superparamagnetism with lower saturation magnetization value, compared with MgFe_2O_4 core. Both of MgFe_2O_4 and MgFe_2O_4-Au core-shell also showed in vitro non-cytotoxicity to mouse areola fibroblast (L-929) cell line. - Highlights: • Synthesis of MgFe_2O_4-Au core-shell nanoparticles with particle size < 100 nm • Complete Au shell coating on the surfaces of MgFe_2O_4 nanoparticles • In vitro cytotoxicity study of complete coated MgFe_2O_4-Au core-shell nanoparticles

  16. Synthesis, characterization, and cytotoxicity of glutathione-PEG-iron oxide magnetic nanoparticles

    Energy Technology Data Exchange (ETDEWEB)

    Haddad, Paula S.; Santos, Marconi C. [Universidade Federal de São Paulo, UNIFESP, Exact and Earth Sciences Department (Brazil); Guzzi Cassago, Carolina Aparecida de [Universidade Estadual de Campinas, UNICAMP, Department of Biochemistry and Tissue Biology, Institute of Biology (Brazil); Bernardes, Juliana S. [National Nanotechnology Laboratory (LNNano), National Center for Energy and Materials (CNPEM) (Brazil); Jesus, Marcelo Bispo de [Universidade Estadual de Campinas, UNICAMP, Department of Biochemistry and Tissue Biology, Institute of Biology (Brazil); Seabra, Amedea B., E-mail: amedea.seabra@ufabc.edu.br [Universidade Federal de São Paulo, UNIFESP, Exact and Earth Sciences Department (Brazil)

    2016-12-15

    Recently, increasing interest is spent on the synthesis of superparamagnetic iron oxide nanoparticles, followed by their characterization and evaluation of cytotoxicity towards tumorigenic cell lines. In this work, magnetite (Fe{sub 3}O{sub 4}) nanoparticles were synthesized by the polyol method and coated with polyethylene glycol (PEG) and glutathione (GSH), leading to the formation of PEG-Fe{sub 3}O{sub 4} and GSH-PEG-Fe{sub 3}O{sub 4} nanoparticles. The nanoparticles were characterized by state-of-the-art techniques: dynamic light scattering (DLS), atomic force microscopy (AFM), X-ray diffraction (XRD), Fourier transform infrared (FTIR) spectroscopy, and superconducting quantum interference device (SQUID) magnetic measurements. PEG-Fe{sub 3}O{sub 4} and GSH-PEG-Fe{sub 3}O{sub 4} nanoparticles have crystallite sizes of 10 and 5 nm, respectively, indicating compression in crystalline lattice upon addition of GSH on the nanoparticle surface. Both nanoparticles presented superparamagnetic behavior at room temperature, and AFM images revealed the regular spherical shape of the nanomaterials and the absence of particle aggregation. The average hydrodynamic sizes of PEG-Fe{sub 3}O{sub 4} and GSH-PEG-Fe{sub 3}O{sub 4} nanoparticles were 69 ± 37 and 124 nm ± 75 nm, respectively. The cytotoxicity of both nanoparticles was screened towards human prostatic carcinoma cells (PC-3). The results demonstrated a decrease in PC-3 viability upon treatment with PEG-Fe{sub 3}O{sub 4} or GSH-PEG-Fe{sub 3}O{sub 4} nanoparticles in a concentration-dependent manner. However, the cytotoxicity was not time-dependent. Due to the superparamagnetic behavior of PEG-Fe{sub 3}O{sub 4} or GSH-PEG-Fe{sub 3}O{sub 4} nanoparticles, upon the application of an external magnetic field, those nanoparticles can be guided to the target site yielding local toxic effects to tumor cells with minimal side effects to normal tissues, highlighting the promising uses of iron oxide nanoparticles in

  17. Synthesis and cytotoxicity study of magnesium ferrite-gold core-shell nanoparticles

    Energy Technology Data Exchange (ETDEWEB)

    Nonkumwong, Jeeranan [Department of Chemistry, Faculty of Science, Chiang Mai University, Chiang Mai 50200 (Thailand); Pakawanit, Phakkhananan [Department of Physics and Materials Science, Faculty of Science, Chiang Mai University, Chiang Mai 50200 (Thailand); Wipatanawin, Angkana [Division of Biochemistry and Biochemical Technology, Department of Chemistry, Faculty of Science, Chiang Mai University, Chiang Mai 50200 (Thailand); Jantaratana, Pongsakorn [Department of Physics, Faculty of Science, Kasetsart University, Bangkok 11900 (Thailand); Ananta, Supon [Department of Physics and Materials Science, Faculty of Science, Chiang Mai University, Chiang Mai 50200 (Thailand); Srisombat, Laongnuan, E-mail: slaongnuan@yahoo.com [Department of Chemistry, Faculty of Science, Chiang Mai University, Chiang Mai 50200 (Thailand)

    2016-04-01

    In this work, the core-magnesium ferrite (MgFe{sub 2}O{sub 4}) nanoparticles were prepared by hydrothermal technique. Completed gold (Au) shell coating on the surfaces of MgFe{sub 2}O{sub 4} nanoparticles was obtained by varying core/shell ratios via a reduction method. Phase identification, morphological evolution, optical properties, magnetic properties and cytotoxicity to mammalian cells of these MgFe{sub 2}O{sub 4} core coated with Au nanoparticles were examined by using a combination of X-ray diffraction, scanning electron microscopy, transmission electron microscopy (TEM), energy-dispersive X-ray spectroscopy, UV–visible spectroscopy (UV–vis), vibrating sample magnetometry and resazurin microplate assay techniques. In general, TEM images revealed different sizes of the core-shell nanoparticles generated from various core/shell ratios and confirmed the completed Au shell coating on MgFe{sub 2}O{sub 4} core nanoparticles via suitable core/shell ratio with particle size less than 100 nm. The core-shell nanoparticle size and the quality of coating influence the optical properties of the products. The UV–vis spectra of complete coated MgFe{sub 2}O{sub 4}-Au core-shell nanoparticles exhibit the absorption bands in the near-Infrared (NIR) region indicating high potential for therapeutic applications. Based on the magnetic property measurement, it was found that the obtained MgFe{sub 2}O{sub 4}-Au core-shell nanoparticles still exhibit superparamagnetism with lower saturation magnetization value, compared with MgFe{sub 2}O{sub 4} core. Both of MgFe{sub 2}O{sub 4} and MgFe{sub 2}O{sub 4}-Au core-shell also showed in vitro non-cytotoxicity to mouse areola fibroblast (L-929) cell line. - Highlights: • Synthesis of MgFe{sub 2}O{sub 4}-Au core-shell nanoparticles with particle size < 100 nm • Complete Au shell coating on the surfaces of MgFe{sub 2}O{sub 4} nanoparticles • In vitro cytotoxicity study of complete coated MgFe{sub 2}O{sub 4}-Au core

  18. Green synthesis of zero valent colloidal nanosilver targeting A549 lung cancer cell: In vitro cytotoxicity

    Directory of Open Access Journals (Sweden)

    Minakshi Jha

    2018-06-01

    Full Text Available An eco-friendly green approach was proposed to synthesise stable, cytotoxic colloidal silver nanoparticles (AgNPs using Momordica charantia (M. charantia fruit extract. Bioinspired green method adopted for fabrication of AgNPs because of easy, fast, low-cost and benign bioprocess. Phytocomponents played the crucial role in capping, stabilisation and inherent cytotoxic potential of colloidal nanosilver. The physiochemical, crystalline, optical and morphological properties of AgNPs were characterized using UV-vis, FT-IR, XRD, SEM, TEM, EDX and AFM. FT-IR reveals the presence of carbonyl, methyl, polyphenol (flavonoid, primary and secondary amine (protein, carboxyl group, ester as major functional groups over the surface of nanomaterials. Mechanistic pathway for formation and stabilisation of colloidal nanosilver has been discussed. Average crystalline size of AgNPs was found to be 12.55 nm from XRD. TEM shows AgNPs nanosphere with size range 1–13.85 nm. Consistency in spherical morphology was also confirmed through Atomic Force Microscopy (AFM. AFM measurement provided image Rq value 3.62, image Ra 2.47, roughness Rmax 36.4 nm, skewness 1.99 and kurtosis 9.87. The SRB assay revealed substantial in vitro noticeable anti-cancer activity of colloidal nanosilver on A549 and HOP-62 human lung cancer cells in a dose dependent manner with IC50 value of 51.93 µg/ml and 76.92 µg/ml. In addition, M. charantia capped AgNPs were found to be more biocompatible in comparison to M. charantia FE. Our study demonstrated the integration of green chemistry principle in nanomaterials fabrication and focused on the potential use of M. charantia fruit extract as an efficient precursor for biocompatible AgNPs anodrug formulation with improved cytotoxic applications. Keywords: M. charantia, Silver nanoparticles, TEM, Anticancer activity, A549, HOP-62

  19. Pure and multi metal oxide nanoparticles: synthesis, antibacterial and cytotoxic properties

    Directory of Open Access Journals (Sweden)

    Slavica Stankic

    2016-10-01

    Full Text Available Abstract Th antibacterial activity of metal oxide nanoparticles has received marked global attention as they can be specifically synthesized to exhibit significant toxicity to bacteria. The importance of their application as antibacterial agents is evident keeping in mind the limited range and effectiveness of antibiotics, on one hand, and the plethora of metal oxides, on the other, along with the propensity of nanoparticles to induce resistance being much lower than that of antibiotics. Effective inhibition against a wide range of bacteria is well known for several nano oxides consisting of one metal (Fe3O4, TiO2, CuO, ZnO, whereas, research in the field of multi-metal oxides still demands extensive exploration. This is understandable given that the relationship between physicochemical properties and biological activity seems to be complex and difficult to generalize even for metal oxide nanoparticles consisting of only one metal component. Also, despite the broad scope that metal oxide nanoparticles have as antibacterial agents, there arise problems in practical applications taking into account the cytotoxic effects. In this respect, the consideration of polymetallic oxides for biological applications becomes even greater since these can provide synergetic effects and unify the best physicochemical properties of their components. For instance, strong antibacterial efficiency specific of one metal oxide can be complemented by non-cytotoxicity of another. This review presents the main methods and technological advances in fabrication of nanostructured metal oxides with a particular emphasis to multi-metal oxide nanoparticles, their antibacterial effects and cytotoxicity.

  20. Antibacterial and cytotoxic activities of the sesquiterpene lactones cnicin and onopordopicrin.

    Science.gov (United States)

    Bach, Sandra M; Fortuna, Mario A; Attarian, Rodgoun; de Trimarco, Juliana T; Catalán, César A N; Av-Gay, Yossef; Bach, Horacio

    2011-02-01

    The antimicrobial and cytotoxic activities of chloroform extracts from the weeds Centaurea tweediei and C. diffusa, and the main sesquiterpene lactones isolated from these species, onopordopicrin and cnicin, respectively, were assayed. Results show that the chloroform extracts from both Centaurea species possess antibacterial activities against a panel of Gram-positive and Gram-negative bacteria. Remarkable antibacterial activity against methicillin-resistant Staphylococcus aureus was also measured. Both the extracts and the purified sesquiterpene lactones show high cytotoxicity against human-derived macrophages. Despite this cytotoxicity, C. diffusa chloroform extract and cnicin are attractive candidates for evaluation as antibiotics in topical preparations against skin-associated pathogens.

  1. Cytotoxic activity of abietane diterpenoids from roots of Salvia sahendica by HPLC-based activity profiling

    Directory of Open Access Journals (Sweden)

    Fahimeh Moradi-Afrapoli

    Full Text Available ABSTRACT Screening of medicinal plants from Iranian flora against human cancer cell-lines have shown that an hexane extract from roots of Salvia sahendica Boiss. & Buhse, Lamiaceae, is active against human cervical cancer (HeLa and colorectal adenocarcinoma (Caco-2 cell-lines at the test concentration of 100 µg/ml (100% inhibition. Cytotoxicity of the extract was localized with the aid of HPLC-time-based activity profiling adapted to the tetrazolium colorimetric bioassay. Four abietane-type diterpenoids in active time-windows were identified as cytotoxic compounds namely: sahandone (1, sahandol (2, 12-deoxy-salvipisone (3 and sahandinone (4. Compound 1 showed the highest toxicity against HeLa cells (IC50 = 5.6 ± 0.1 µg/ml, which was comparable with betulinic acid (IC50 = 4.3 ± 1.2 µg/ml, the positive control. Compound 2 was active against the HeLa cells (IC50 = 8.9 ± 0.7 µg/ml but not the Caco-2 cell-line. Compounds 1, 3 and 4 exhibited moderate activity (IC50 = 22.9–41.4 µg/ml against the Caco-2 cells. This study reveals that the HeLa cells are more sensitive to all tested compounds than the Caco-2 cells. In silico molecular docking study showed a rigid binding of the compounds to tyrosine kinase pp60src, and proved their cytotoxic activity.

  2. Synthesis and Cytotoxic Effect of Some Novel 1,2-Dihydropyridin-3-carbonitrile and Nicotinonitrile Derivatives

    Directory of Open Access Journals (Sweden)

    Eman M. Flefel

    2015-12-01

    Full Text Available 1-(2,4-Dichlorophenyl-3-(4-fluorophenylpropen-1-one (1 was prepared and reacted with an active methylene compound (ethyl cyanoacetate in the presence of ammonium acetate to give the corresponding cyanopyridone 2. Compound 2 reacted with hydrazine hydrate, malononitrile, ethyl bromoacetate and phosphorous oxychloride to afford compounds 4 and 7–11, respectively. The 2-chloropyridine derivative 11 reacted with different primary amines, namely benzyl amine, piperonyl amine, 1-phenylethyl amine, and/or the secondary amines 2-methyl-pipridine and morpholine to give the corresponding derivatives 12–15. Hydrazinolysis of chloropyridine derivative 11 with hydrazine hydrate afforded the corresponding hydrazino derivative 17. Condensation of compound 17 with ethyl acetoacetate, acetylacetone, isatin and different aldehydes gave the corresponding derivatives 18–21. Some of newly synthesized compounds were screened for cytotoxic activity against three tumor cell lines. The results indicated that compounds 8 and 16 showed the best results, exhibiting the highest inhibitory effects towards the three tumor cell lines, which were higher than that of the reference doxorubicin and these compounds were non-cytotoxic towards normal cells (IC50 values > 100 μg/mL.

  3. Green synthesis of NiO nanoparticles using Moringa oleifera extract and their biomedical applications: Cytotoxicity effect of nanoparticles against HT-29 cancer cells.

    Science.gov (United States)

    Ezhilarasi, A Angel; Vijaya, J Judith; Kaviyarasu, K; Maaza, M; Ayeshamariam, A; Kennedy, L John

    2016-11-01

    Green protocols for the synthesis of nickel oxide nanoparticles using Moringa oleifera plant extract has been reported in the present study as they are cost effective and ecofriendly, moreover this paper records that the nickel oxide (NiO) nanoparticles prepared from green method shows better cytotoxicity and antibacterial activity. The NiO nanoparticles were characterized by X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FTIR), High resolution transmission electron microscopy (HRTEM), Energy dispersive X-ray analysis (EDX), and Photoluminescence spectroscopy (PL). The formation of a pure nickel oxide phase was confirmed by XRD and FTIR. The synthesized NiO nanoparticles was single crystalline having face centered cubic phase and has two intense photoluminescence emissions at 305.46nm and 410nm. The formation of nano- and micro-structures was confirmed by HRTEM. The in-vitro cytotoxicity and cell viability of human cancer cell HT-29 (Colon Carcinoma cell lines) and antibacterial studies against various bacterial strains were studied with various concentrations of nickel oxide nanoparticles prepared from Moringa oleifera plant extract. MTT assay measurements on cell viability and morphological studies proved that the synthesized NiO nanoparticles posses cytotoxic activity against human cancer cells and the various zones of inhibition (mm), obtained revealed the effective antibacterial activity of NiO nanoparticles against various Gram positive and Gram negative bacterial pathogens. Copyright © 2016 Elsevier B.V. All rights reserved.

  4. Cytotoxic 1,3-Thiazole and 1,2,4-Thiadiazole Alkaloids from Penicillium oxalicum: Structural Elucidation and Total Synthesis

    Directory of Open Access Journals (Sweden)

    Zheng Yang

    2016-02-01

    Full Text Available Two new thiazole and thiadiazole alkaloids, penicilliumthiamine A and B (2 and 3, were isolated from the culture broth of Penicillium oxalicum, a fungus found in Acrida cinerea. Their structures were elucidated mainly by spectroscopic analysis, total synthesis and X-ray crystallographic analysis. Biological evaluations indicated that compound 1, 3a and 3 exhibit potent cytotoxicity against different cancer cell lines through inhibiting the phosphorylation of AKT/PKB (Ser 473, one of important cancer drugs target.

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

    African Journals Online (AJOL)

    efficacy of the plant leaves for treatment of malaria. Key Words: Antiplasmodial, cytotoxicity, Vernonia amygdalina leave, in vitro, Plasmodium falciparum, vero cell line. INTRODUCTION. Malaria constitutes one of the major public health problems in the world, especially in tropical. Africa, Asia and Latin America. The World.

  6. Cytotoxic Effect and Antioxidant Activity of Bioassay- guided ...

    African Journals Online (AJOL)

    ... were investigated for their in vitro cytotoxic effect against various cancer cell lines using 3-(4, 5-dimethyl-2-thiazolyl)-2, 5- ... In MTT assay, fractions 1, 2 and 4 from methanol extract showed the ... plant is used as antitumourigenic, antioxidant,.

  7. 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 ...

  8. 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, ...

  9. Cytotoxic Activities of Several Geranyl-Substituted Flavanones

    Czech Academy of Sciences Publication Activity Database

    Šmejkal, K.; Svačinová, Jana; Šlapetová, T.; Schneiderová, K.; Dall’Acqua, S.; Innocenti, G.; Závalová, V.; Kollár, P.; Chudík, S.; Marek, R.; Julínek, O.; Urbanová, M.; Kartal, M.; Csöllei, M.; Doležal, Karel

    2010-01-01

    Roč. 73, č. 4 (2010), s. 568-572 ISSN 0163-3864 R&D Projects: GA MŠk(CZ) LC06030; GA ČR GD522/08/H003 Institutional research plan: CEZ:AV0Z50380511 Keywords : flavanones * geranyl * cytotoxicity Subject RIV: BO - Biophysics Impact factor: 2.872, year: 2010

  10. 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 ...

  11. 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.

  12. Synthesis, characterization, and cytotoxicity in human erythrocytes of multifunctional, magnetic, and luminescent nanocrystalline rare earth fluorides

    Science.gov (United States)

    Grzyb, Tomasz; Mrówczyńska, Lucyna; Szczeszak, Agata; Śniadecki, Zbigniew; Runowski, Marcin; Idzikowski, Bogdan; Lis, Stefan

    2015-10-01

    Multifunctional nanoparticles exhibiting red or green luminescence properties and magnetism were synthesized and thoroughly analyzed. The hydrothermal method was used for the synthesis of Eu3+- or Tb3+-doped GdF3-, NaGdF4-, and BaGdF5-based nanocrystalline materials. The X-ray diffraction patterns of the samples confirmed the desired compositions of the materials. Transmission electron microscope images revealed the different morphologies of the products, including the nanocrystal sizes, which varied from 12 nm in the case of BaGdF5-based nanoparticles to larger structures with dimensions exceeding 300 nm. All of the samples presented luminescence under ultraviolet irradiation, as well as when the samples were in the form of water colloids. The highest luminescence was observed for BaGdF5-based materials. The obtained nanoparticles exhibited paramagnetism along with probable evidence of superparamagnetic behavior at low temperatures. The particles' magnetic characteristics were also preserved for samples in the form of a suspension in distilled water. The cytotoxicity studies against the human erythrocytes indicated that the synthesized nanoparticles are non-toxic because they did not cause the red blood cells shape changes nor did they alter their membrane structure and permeabilization.

  13. Synthesis, characterization, and cytotoxicity in human erythrocytes of multifunctional, magnetic, and luminescent nanocrystalline rare earth fluorides

    International Nuclear Information System (INIS)

    Grzyb, Tomasz; Mrówczyńska, Lucyna; Szczeszak, Agata; Śniadecki, Zbigniew; Runowski, Marcin; Idzikowski, Bogdan; Lis, Stefan

    2015-01-01

    Multifunctional nanoparticles exhibiting red or green luminescence properties and magnetism were synthesized and thoroughly analyzed. The hydrothermal method was used for the synthesis of Eu 3+ - or Tb 3+ -doped GdF 3 -, NaGdF 4 -, and BaGdF 5 -based nanocrystalline materials. The X-ray diffraction patterns of the samples confirmed the desired compositions of the materials. Transmission electron microscope images revealed the different morphologies of the products, including the nanocrystal sizes, which varied from 12 nm in the case of BaGdF 5 -based nanoparticles to larger structures with dimensions exceeding 300 nm. All of the samples presented luminescence under ultraviolet irradiation, as well as when the samples were in the form of water colloids. The highest luminescence was observed for BaGdF 5 -based materials. The obtained nanoparticles exhibited paramagnetism along with probable evidence of superparamagnetic behavior at low temperatures. The particles’ magnetic characteristics were also preserved for samples in the form of a suspension in distilled water. The cytotoxicity studies against the human erythrocytes indicated that the synthesized nanoparticles are non-toxic because they did not cause the red blood cells shape changes nor did they alter their membrane structure and permeabilization

  14. Green synthesis of silver nanoparticles and investigation of their colorimetric sensing and cytotoxicity effects

    Science.gov (United States)

    Pahlavan Noghabi, Mohammad; Parizadeh, Mohammad Reza; Ghayour-Mobarhan, Majid; Taherzadeh, Danial; Hosseini, Hasan Ali; Darroudi, Majid

    2017-10-01

    The "Green" synthesis of metallic nanoparticles and investigation of their optical properties has become a useful application between nanoscience and medicine. In this work, silver nanoparticles (Ag-NPs) were successfully prepared through a facile and green method by treating silver ions with chitosan. Preparation of Ag-NPs in silver nitrate solution (0.01 M) resulted in small and spherical shapes of Ag-NPs with a mean diameter of 10.2 nm. The formation of Ag-NPs was approved by surface Plasmon resonance (SPR) absorption peaks, using UV-vis spectrophotometer, while Ag-NPs were successfully employed in colorimetric sensing of H2O2 via an analytical procedure. Degradation process of Ag-NPs, encouraged by the catalytic decomposition of H2O2, causes a significant change in the absorbance intensity of SPR band depending on the H2O2 concentration. The cytotoxicity effect of synthesized Ag-NPs was examined on HEK293 cell line. The results illustrate a concentration-dependent toxicity for the tested cells, while15.07 μg/mL of IC50 was obtained.

  15. Synthesis, characterization, and cytotoxicity evaluation of high-magnetization multifunctional nanoclusters

    Energy Technology Data Exchange (ETDEWEB)

    Petran, Anca; Radu, Teodora; Nan, Alexandrina [National Institute for Research and Development of Isotopic and Molecular Technologies (Romania); Olteanu, Diana; Filip, Adriana, E-mail: adrianafilip33@yahoo.com; Clichici, Simona; Baldea, Ioana [Iuliu Hatieganu University of Medicine and Pharmacy, Department of Physiology (Romania); Suciu, Maria; Turcu, Rodica, E-mail: rodica.turcu@itim-cj.ro [National Institute for Research and Development of Isotopic and Molecular Technologies (Romania)

    2017-01-15

    The paper presents the synthesis, characterization, and in vitro cytotoxicity tests of Fe{sub 3}O{sub 4} magnetic nanoclusters coated with ethylenediaminetetraacetic acid disodium salt (EDTA). Electron microscopy analysis (SEM) evidences that magnetite nanoparticles are closely packed into the clusters stabilized with EDTA with well-defined near spherical shapes and sizes in the range 100–200 nm. From XRD measurements, we determined the mean size of the crystallites inside the magnetic cluster about 36 nm. The saturation magnetization determined for the magnetic clusters stabilized with EDTA has high value, about 81.7 emu/g at 300 K. X-ray photoelectron spectroscopy has been used to determine both the elemental and chemical structure of the magnetic cluster surface. In vitro studies have shown that the magnetic clusters at low doses did not induce toxicity on human umbilical vein endothelial cells or lesions of the cell membrane. In contrast, at high doses, the magnetic clusters increased the lipid peroxidation and reduced the leakage of a cytoplasmic enzyme, lactate dehydrogenase (LDH), in parallel with increasing the antioxidant defense.

  16. Topological estimation of cytotoxic activity of some anti-HIV agents ...

    Indian Academy of Sciences (India)

    Unknown

    2Research Division, Laxmi Fumigation and Pest Control Pvt. Ltd., 3, Khatipura, Indore 452 007, ... Structural details and cytotoxic activity (pCC50) of the compounds (HEPT analogues) ..... The regression parameters and the quality of corre-.

  17. Synthesis, Cytotoxicity and Molecular Docking Study of Complexes Containing Thiazole Moiety

    Directory of Open Access Journals (Sweden)

    Mohammed Shafeeulla

    2017-07-01

    Full Text Available The ligand 5-methyl-2-phenyl-4-[(E-1,3-thiazol-2-yldiazenyl]-2,4-dihydro-3H-pyrazol-3-one (Dy has been synthesized by diazo coupling reactions of 5-methyl-2-phenyl- 2,4-dihydro-3H-pyrazol-3-one with 2-aminothiazole and ferric hydrogen sulfate (FHS, as a catalyst, under solvent-free conditions. A series of complexes of the ligand with Co(II, Ni(II, Cu(II, and Zn(II ions are synthesized and structurally characterized by 1H NMR, FTIR, and UV–Visible spectral techniques. The cytotoxic activity of the complexes and the uncoordinated ligand against human breast cancer (MCF-7 and chronic myelogenous leukemia cell line (human erythroleukemia (K-562 cell lines exhibits good viability in the range of 50.16–55.16% at a concentration of >100-110 µg/mL as compared to the inhibition in the untreated cells. Further, the metal complexes and ligand were screened against antibacterial strains of S. typhi, S. aureus, and E. coli. Both the cytotoxicity and antioxidant studies are correlated with computational docking analysis and powder XRD studies reviles that all complexes are in crystalline nature.

  18. Chromatogram Profiles and Cytotoxic Activity of Irradiated Mahkota Dewa (Phaleria Macrocarpa Scheff. Boerl Leaves

    Directory of Open Access Journals (Sweden)

    E. Katrin1

    2011-04-01

    Full Text Available Gamma irradiation has been used by the industries for preservation of herbal medicine, but it has not been studied the effect of gamma irradiation on their efficacy, especially their bioactivity as anticancer substances. The purpose of this research was to study the effect of gamma irradiation on the mahkota dewa leaves which has been claimed to contain potent anticancer substances. Maceration of dried mahkota dewa leaves successively with n-hexane, ethyl acetate, and ethanol gave crude extracts which the ethyl acetate was the most cytotoxic extract against leukemia L1210 cells with an inhibition concentration fifty (IC50 value of 10.3 µg/ml. Further separation of ethyl acetate extract by column chromatograph gave 7 fractions, and fraction 2 showed the most cytotoxic fraction exhibited the most cytotoxic extract against leukemia L1210 cells with an IC50 value of 1.9 µg/ml. Since, the fraction 2 of ethyl acetate extract was the most potent fraction, the irradiated samples were treated with the same procedure as treatment of fraction 2 from control sample. Cytotoxic activity test of fractions 2 from irradiated samples showed that the cytotoxic activity decreased depending on increasing of irradiation dose. Gamma irradiation dose up to 7.5 kGy on mahkota dewa leaves could decreased the cytotoxic activity of fraction 2 as the most cytotoxic-potential fraction against leukemia L1210 cells, but decreasing the cytotoxic activity has not exceeded the limit of the fraction declared inactive. So that the irradiation dose up to 7.5 kGy can be used for decontamination of bacteria and fungus/yeast without eliminating the cytotoxic activity. Gamma irradiation also caused changes in the thin layer chromatograph (TLC spots and HPLC chromatograms profiles of fraction 2 which was the most cytotoxic fraction in ethyl acetate extract of mahkota dewa leaves against leukemia L1210 cells. One of the main peaks (peak 1 on HPLC chromatograms decreased with increasing

  19. Chromatogram Profiles and Cytotoxic Activity of Irradiated Mahkota Dewa (Phaleria Macrocarpa (Scheff.) Boerl) Leaves

    International Nuclear Information System (INIS)

    Katrin, E.; Winarno, H.; Selvie

    2011-01-01

    Gamma irradiation has been used by the industries for preservation of herbal medicine, but it has not been studied the effect of gamma irradiation on their efficacy, especially their bioactivity as anticancer substances. The purpose of this research was to study the effect of gamma irradiation on the mahkota dewa leaves which has been claimed to contain potent anticancer substances. Maceration of dried mahkota dewa leaves successively with n-hexane, ethyl acetate, and ethanol gave crude extracts which the ethyl acetate was the most cytotoxic extract against leukemia L1210 cells with an inhibition concentration fifty (IC 50 ) value of 10.3 μg/ml. Further separation of ethyl acetate extract by column chromatograph gave 7 fractions, and fraction 2 showed the most cytotoxic fraction exhibited the most cytotoxic extract against leukemia L1210 cells with an IC 50 value of 1.9 μg/ml. Since, the fraction 2 of ethyl acetate extract was the most potent fraction, the irradiated samples were treated with the same procedure as treatment of fraction 2 from control sample. Cytotoxic activity test of fractions 2 from irradiated samples showed that the cytotoxic activity decreased depending on increasing of irradiation dose. Gamma irradiation dose up to 7.5 kGy on mahkota dewa leaves could decreased the cytotoxic activity of fraction 2 as the most cytotoxic-potential fraction against leukemia L1210 cells, but decreasing the cytotoxic activity has not exceeded the limit of the fraction declared inactive. So that the irradiation dose up to 7.5 kGy can be used for decontamination of bacteria and fungus/yeast without eliminating the cytotoxic activity. Gamma irradiation also caused changes in the thin layer chromatograph (TLC) spots and HPLC chromatograms profiles of fraction 2 which was the most cytotoxic fraction in ethyl acetate extract of mahkota dewa leaves against leukemia L1210 cells. One of the main peaks (peak 1) on HPLC chromatograms decreased with increasing the

  20. In vitro cytotoxicity of zinc oxide, iron oxide and copper nanopowders prepared by green synthesis

    Directory of Open Access Journals (Sweden)

    Saranya S.

    Full Text Available In vitro cytotoxic effects of ZnO, FeO and Cu metallic nanopowders (NPs on Vero (African green monkey kidney cell line, PK 15 (Pig kidney cell line and Madin Darby Bovine Kidney (MDBK cell lines were investigated at different time intervals (24 and 48 h. MTT (3-(4,5-dimethylthiazol-2-yl-2,5-diphenyltetrazolium bromide assay was used to determine the cytotoxic effects of green synthesized (plant based nanopowders. The comparative effects of exposure period and concentration of nanopowders on cell viability were studied. Green synthesized nanopowders showed varying activity on different type of cells and the effect was generally based on the concentration and exposure time. In MDBK cells, only ZnO nanopowder (NP showed significant effect on cell viability. The ZnO NP showed improved cell viability at lower concentration (10 μg/100 μl in all type of cells (Vero, PK 15 and MDBK cells. In contrast, FeO NP showed better activity at the concentration of 10 μg/100 μl, 50 μg/100 μl and 40 μg/100 μl after 24 h exposure time in Vero, PK 15 and MDBK cells respectively. However better cell viability was observed in Cu NP treated Vero, PK 15 and MDBK cells at 40 μg/100 μl, 20 μg/100 μl and 10 μg/100 μl correspondingly. These studies suggested that the activity of green synthesized NPs were highly dependent on concentration, exposure time and type of cells. Keywords: ZnO, FeO, Cu, Nanopowders, MTT, in vitro cytotoxicity

  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. Colloidal polyaniline dispersions: Antibacterial activity, cytotoxicity and neutrophil oxidative burst

    Czech Academy of Sciences Publication Activity Database

    Kuceková, Z.; Humpolíček, P.; Kašpárková, V.; Perečko, Tomáš; Lehocký, M.; Hauerlandova, I.; Saha, P.; Stejskal, Jaroslav

    Roč. 116, APR 2014 ( 2014 ), s. 411-417 ISSN 0927-7765 R&D Projects: GA ČR(CZ) GA13-08944S; GA MŠk(CZ) EE2.3.30.0030 Institutional support: RVO:68081707 ; RVO:61389013 Keywords : Cytotoxicity * Apoptosis * Necrosis Subject RIV: BO - Biophysics; CD - Macromolecular Chemistry (UMCH-V) Impact factor: 4.152, year: 2014

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

    African Journals Online (AJOL)

    mL and 495.6 - >2000μg/mL for DPPH and ABTS assay respectively. The cytotoxicity assay showed LC50 ranged between 26.47 to 93.64 μg/mL against Vero cells and 74.29 to 225.40 μg/mL against C3A. The results of this study show that the ...

  4. Green synthesis of graphene and its cytotoxic effects in human breast cancer cells

    Directory of Open Access Journals (Sweden)

    Gurunathan S

    2013-03-01

    Full Text Available Sangiliyandi Gurunathan, Jae Woong Han, Vasuki Eppakayala, Jin-Hoi Kim Department of Animal Biotechnology, Konkuk University, Seoul, South Korea Background: This paper describes an environmentally friendly (“green” approach for the synthesis of soluble graphene using Bacillus marisflavi biomass as a reducing and stabilizing agent under mild conditions in aqueous solution. In addition, the study reported here investigated the cytotoxicity effects of graphene oxide (GO and bacterially reduced graphene oxide (B-rGO on the inhibition of cell viability, reactive oxygen species (ROS generation, and membrane integrity in human breast cancer cells. Methods: The reduction of GO was characterized by ultraviolet–visible spectroscopy. Size distribution was analyzed by dynamic light scattering. Further, X-ray diffraction and high-resolution scanning electron microscopy were used to investigate the crystallinity of graphene and the morphologies of prepared graphene, respectively. The formation of defects further supports the bio-functionalization of graphene, as indicated in the Raman spectrum of B-rGO. Surface morphology and the thickness of the GO and B-rGO were analyzed using atomic force microscopy, while the biocompatibility of GO and B-rGO were investigated using WST-8 assays on MCF-7 cells. Finally, cellular toxicity was evaluated by ROS generation and membrane integrity assays. Results: In this study, we demonstrated an environmentally friendly, cost-effective, and simple method for the preparation of water-soluble graphene using bacterial biomass. This reduction method avoids the use of toxic reagents such as hydrazine and hydrazine hydrate. The synthesized soluble graphene was confirmed using various analytical techniques. Our results suggest that both GO and B-rGO exhibit toxicity to MCF-7 cells in a dose-dependent manner, with a dose > 60 µg/mL exhibiting obvious cytotoxicity effects, such as decreasing cell viability, increasing ROS

  5. Antimicrobial, Antioxidant and Cytotoxic Activity of Silver Nanoparticles Synthesized by Leaf Extract of Erythrina suberosa (Roxb.).

    Science.gov (United States)

    Mohanta, Yugal K; Panda, Sujogya K; Jayabalan, Rasu; Sharma, Nanaocha; Bastia, Akshaya K; Mohanta, Tapan K

    2017-01-01

    In this experiment, biosynthesized silver nanoparticles (AgNPs) were synthesized using aqueous leaf extract of Erythrina suberosa (Roxb.). The biosynthesis of silver nanoparticle was continuously followed by UV-vis spectrophotometric analysis. The response of the phytoconstituents resides in E. suberusa during synthesis of stable AgNPs were analyzed by ATR- fourier-transform infrared spectroscopy. Further, the size, charge, and polydispersity nature of AgNPs were studied using dynamic light scattering spectroscopy. The morphology of the nanoparticles was determined by scanning electron microscopy. Current result shows core involvement of plant extracts containing glycosides, flavonoids, and phenolic compounds played a crucial role in the biosynthesis of AgNPs. The antimicrobial activities of silver nanoparticles were evaluated against different pathogenic bacterium and fungi. The antioxidant property was studied by radical scavenging (DPPH) assay and cytotoxic activity was evaluated against A-431 osteosarcoma cell line by MTT assay. The characteristics of the synthesized silver nanoparticles suggest their application as a potential antimicrobial and anticancer agent.

  6. Activity-guided isolation of cytotoxic bis-bibenzyl constituents from Dumortiera hirsuta.

    Science.gov (United States)

    Toyota, Masao; Ikeda, Risa; Kenmoku, Hiromichi; Asakawa, Yoshinori

    2013-01-01

    Activity-guided fractionation of the ether extract of Dumortiera hirsute (Japanese liverwort), using cytotoxicity testing with cultured HL 60 and KB cells, resulted in the isolation of a new cytotoxic bis-bibenzyl compound, along with the two known bis-bibenzyls: isomarchantin C and isoriccardin C. The structural determination of the new bis-bibenzyl through extensive NMR spectral data indicated a derivative of marchantin A, which has been isolated from the liverwort Marchantia polymorpha. The cytotoxicity of the bis-bibenzyls was evaluated by the MTT (3-(4,5-di-methylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay using cultured HL 60 and KB cells.

  7. Silver(I) complexes with hydantoins and allantoin: synthesis, crystal and molecular structure, cytotoxicity and pharmacokinetics.

    Science.gov (United States)

    Puszyńska-Tuszkanow, Mariola; Grabowski, Tomasz; Daszkiewicz, Marek; Wietrzyk, Joanna; Filip, Beata; Maciejewska, Gabriela; Cieślak-Golonka, Maria

    2011-01-01

    Coordination polymers [Ag(L(1,3))](n) (L(1)=hydantoin, L(3)=5,5-dimethylhydantoin), {[Ag(L(2))](.)0.5H(2)O}(n) (L(2)=1-methylhydantoin) and [Ag(NH(3))(L(4))](n) (L(4)=allantoin) were prepared and characterized by elemental analysis, spectroscopic (IR, FTIR and NMR), thermal and mass spectrometry methods. The crystal structure of {[Ag(1-methylhydantoin)]·0,5H(2)O}(n) was determined and analyzed. Three 1-methylhydantoinate ligands create a T-shape (CN=3) coordination sphere around the Ag(+) ion. Additionally, a short Ag⋯Ag distance of 2.997Å was found in the structure resulting in the expanded [3+2] environment of a distorted square shape. The [Ag(L(2))] entities are bound to each other by the bridging organic ligands. Thus a two-dimensional coordination polymer is created with water molecules located between the layers. In contrast to hydantoins, the allantoin complex contains an additional ammonia molecule in the coordination sphere. Moreover, in the Ag-alla complex the M-organic ligand binding site is shifted to the N-atom of the ureid chain. Free ligands are cytotoxically inactive against human MCF-7 and A549 cancer cell lines and mouse fibroblasts Balb/3T3. The silver hydantoin complexes exhibit a very strong activity against these lines. (The introduction of the methyl groups to the ring slightly increases resistance only against the A549 cell line.) In contrast, the silver complex of allantoin shows only a weak activity which may be related to the presence of the cytotoxic ammonia group in the composition of the compound and/or the different binding site of the ligand. Calculated in silico physiochemical parameters are promising for the future application of the complexes as drugs. Copyright © 2010 Elsevier Inc. All rights reserved.

  8. An Efficient Sonochemical Synthesis of Novel Schiff’s Bases, Thiazolidine, and Pyrazolidine Incorporating 1,8-Naphthyridine Moiety and Their Cytotoxic Activity against HePG2 Cell Lines

    Directory of Open Access Journals (Sweden)

    N. S. Ahmed

    2014-01-01

    Full Text Available Novel Schiff’s bases 4a–e, 5a, 5b, and 6, thiazolidine 7a–d, and pyrazolidine 8 have been synthesized using the versatile synthon 4-hydroxy-2,7-dimethyl-1,8-naphthyridine 1. Reactions carried out under ultrasound irradiation showed higher rates and yields than those done under silent conditions. The newly synthesized compounds were evaluated for HepG2 cell growth inhibition. The results obtained revealed that the tested compounds possess inhibitory effect on the growth of HepG2 liver cancer cells. The results were compared to doxorubicin as a reference drug (IC50: 0.04. Compounds 4a and 7b showed the highest inhibition activity against the HepG2 cell line (IC50: 0.047 and 0.041 µM, resp. among all the tested compounds.

  9. Synthesis, DNA binding and cytotoxic activity of pyrimido[4',5':4,5]thieno(2,3-b)quinoline with 9-hydroxy-4-(3-diethylaminopropylamino) and 8-methoxy-4-(3-diethylaminopropylamino) substitutions.

    Science.gov (United States)

    KiranKumar, Hulihalli N; RohitKumar, Heggodu G; Advirao, Gopal M

    2018-01-01

    Two new derivatives of pyrimido[4',5';4,5]thieno(2,3-b)quinoline (PTQ), 9-hydroxy-4-(3-diethylaminopropylamino)pyrimido[4',5';4,5]thieno(2,3-b)quinoline (Hydroxy-DPTQ) and 8-methoxy-4-(3-diethylaminopropylamino)pyrimido[4',5';4,5]thieno(2,3-b)quinoline (Methoxy-DPTQ) were synthesized and their DNA binding ability was analyzed using spectroscopy (UV-visible, fluorescence and circular dichroism), ethidium bromide dye displacement assay, melting temperature (T m ) analysis and computational docking studies. The hypochromism in UV-visible spectrum and increased fluorescence emission of Hydroxy-DPTQ and Methoxy-DPTQ in the presence of DNA suggested the molecule-DNA interaction. The association constants calculated from UV-visible and spectral titrations were of the order 10 4 to 10 6 M -1 . Circular dichroism studies corroborated the induced conformational changes in DNA upon addition of molecules. The change in the ellipticity was observed both in negative and positive peak of DNA, thus, suggesting the intercalation of molecules. The observed displacement of ethidium bromide from the DNA and increased T m , upon addition of DNA confirmed the intercalative mode of binding. This was further validated by computational docking, which showed clear intercalation of molecules into the d(GpC)-d(CpG) site of the receptor DNA. Anticancer activities of these molecules are evaluated by using MTT assay. Both molecules showed antiproliferative activity against all the three cancer cells studied, with Hydroxy-DPTQ being more potential molecule among the two. IC 50 value of Hydroxy-DPTQ and Methoxy-DPTQ were in the range of 3-5μM and 130-250μM, respectively. Copyright © 2017 Elsevier B.V. All rights reserved.

  10. Lithium-Acetate-Mediated Biginelli One-Pot Multicomponent Synthesis under Solvent-Free Conditions and Cytotoxic Activity against the Human Lung Cancer Cell Line A549 and Breast Cancer Cell Line MCF7

    Directory of Open Access Journals (Sweden)

    Harshita Sachdeva

    2012-01-01

    Full Text Available Various Biginelli compounds (dihydropyrimidinones have been synthesized efficiently and in high yields under mild, solvent-free, and eco-friendly conditions in a one-pot reaction of 1,3-dicarbonyl compounds, aldehydes, and urea/thiourea/acetyl thiourea using lithium-acetate as a novel catalyst without the addition of any proton source. Comparative catalytic efficiency of lithium-acetate and polyphosphoric acid to catalyze Biginelli condensation is also studied under neat conditions. The reaction is carried out in the absence of any solvent and represents an improvement of the classical Biginelli protocol and an advantage in comparison with FeCl3·6H2O, NiCl2·6H2O and CoCl2·6H2O that were used with HCl as a cocatalyst. Compared to classical Biginelli reaction conditions, the present method has advantages of good yields, short reaction times, and experimental simplicity. The obtained products have been identified by spectral (1H NMR and IR data and their melting points. The prepared compounds are evaluated for anticancer activity against two human cancer cell lines (lung cancer cell line A549 and breast cancer cell line MCF7.

  11. New palladium(II) and platinum(II) 5,5-diethylbarbiturate complexes with 2-phenylpyridine, 2,2'-bipyridine and 2,2'-dipyridylamine: synthesis, structures, DNA binding, molecular docking, cellular uptake, antioxidant activity and cytotoxicity.

    Science.gov (United States)

    Icsel, Ceyda; Yilmaz, Veysel T; Kaya, Yunus; Samli, Hale; Harrison, William T A; Buyukgungor, Orhan

    2015-04-21

    Novel palladium(ii) and platinum(ii) complexes of 5,5-diethylbarbiturate (barb) with 2-phenylpyridine (Hppy), 2,2'-bipyridine (bpy) and 2,2'-dipyridylamine (dpya) have been prepared and characterized by elemental analysis, IR, UV-Vis, NMR and ESI-MS. Single-crystal diffraction measurements show that complex consists of binuclear [Pd2(μ-barb-κN,O)2(ppy-κN,C)2] moieties, while complexes are mononuclear, [M(barb-κN)2(L-κN,N')] (L = bpy or dpya). has a composition of [Pt(dpya-κN,N')2][Ag(barb-κN)2]2·4H2O and was assumed to have a structure of [Pt(barb-κN)(Hppy-κN)(ppy-κN,C)]·3H2O. The complexes were found to exhibit significant DNA binding affinity by a non-covalent binding mode, in accordance with molecular docking studies. In addition, complexes and displayed strong binding with supercoiled pUC19 plasmid DNA. Cellular uptake studies were performed to assess the subcellular localization of the selected complexes. A moderate radical scavenging activity of and was confirmed by DPPH and ABTS tests. Complexes , , and showed selectivity against HT-29 (colon) cell line.

  12. Aqueous Synthesis of PEGylated Quantum Dots with Increased Colloidal Stability and Reduced Cytotoxicity.

    Science.gov (United States)

    Ulusoy, Mehriban; Jonczyk, Rebecca; Walter, Johanna-Gabriela; Springer, Sergej; Lavrentieva, Antonina; Stahl, Frank; Green, Mark; Scheper, Thomas

    2016-02-17

    Ligands used on the surface of colloidal nanoparticles (NPs) have a significant impact on physiochemical properties of NPs and their interaction in biological environments. In this study, we report a one-pot aqueous synthesis of 3-mercaptopropionic acid (MPA)-functionalized CdTe/CdS/ZnS quantum dots (Qdots) in the presence of thiol-terminated methoxy polyethylene glycol (mPEG) molecules as a surface coordinating ligand. The resulting mPEG-Qdots were characterized by using ζ potential, FTIR, thermogravimetric (TG) analysis, and microscale thermophoresis (MST) studies. We investigated the effect of mPEG molecules and their grafting density on the Qdots photophysical properties, colloidal stability, protein binding affinity, and in vitro cellular toxicity. Moreover, cellular binding features of the resulting Qdots were examined by using three-dimensional (3D) tumor-like spheroids, and the results were discussed in detail. Promisingly, mPEG ligands were found to increase colloidal stability of Qdots, reduce adsorption of proteins to the Qdot surface, and mitigate Qdot-induced side effects to a great extent. Flow cytometry and confocal microscopy studies revealed that PEGylated Qdots exhibited distinctive cellular interactions with respect to their mPEG grafting density. As a result, mPEG molecules demonstrated a minimal effect on the ZnS shell deposition and the Qdot fluorescence efficiency at a low mPEG density, whereas they showed pronounced effect on Qdot colloidal stability, protein binding affinity, cytotoxicity, and nonspecific binding at a higher mPEG grafting amount.

  13. Serine esterase and hemolytic activity in human cloned cytotoxic T lymphocytes

    OpenAIRE

    1988-01-01

    Target cell lysis by most murine cytotoxic T lymphocytes appears to be mediated by a complement (C9)-like protein called perforin, contained in high-density cytoplasmic granules. These granules also contain high levels of serine esterase activity, which may also play a role in cytolysis. Analysis of 17 cloned human cytotoxic T lymphocytes revealed the presence of serine esterase that is very similar to its murine counterpart in substrate and inhibitor specificities, pH optimum, and molecular ...

  14. 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.

  15. Design, synthesis and cytotoxic activity of some novel compounds ...

    Indian Academy of Sciences (India)

    2.4a3-Methyl-1-phenyl-6-phenylaminomethyl-1,5-dihydro- pyrazolo [3, 4-d] pyrimidin-4-one (4a): White colour solids; yield: 58%; m.p. 223-225. ◦. C; IR (KBr, cm. −1): 3428, 2930, 2871, 1685, 1H-NMR (DMSO-d6) δ = 2.49 (s, 3H, CH3), 4.30-4.32 (d, 2H, CH2), 6.03–6.08. (t, 1H, NH, D2O exchangeable), 6.57–6.59 (t, 1H, C4 –.

  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 and antimicrobial activities of endophytic fungi isolated from Bacopa monnieri (L.) Pennell (Scrophulariaceae).

    Science.gov (United States)

    Katoch, Meenu; Singh, Gurpreet; Sharma, Sadhna; Gupta, Nidhi; Sangwan, Payare Lal; Saxena, Ajit Kumar

    2014-02-11

    Endophytes, which reside in plant tissues, have the potential to produce novel metabolites with immense benefits for health industry. Cytotoxic and antimicrobial activities of endophytic fungi isolated from Bacopa monnieri (L.) Pennell were investigated. Endophytic fungi were isolated from the Bacopa monnieri. Extracts from liquid cultures were tested for cytotoxicity against a number of cancer cell lines using the MTT assay. Antimicrobial activity was determined using the micro dilution method. 22% of the examined extracts showed potent (IC50 of <20 μg/ml) cytotoxic activity against HCT-116 cell line. 5.5%, 11%, 11% of the extracts were found to be cytotoxic for MCF-7, PC-3, and A-549 cell lines respectively. 33% extracts displayed antimicrobial activity against at least one test organism with MIC value 10-100 μg/ml. The isolate B9_Pink showed the most potent cytotoxic activity for all the cell lines examined and maximum antimicrobial activity against the four pathogens examined which was followed by B19. Results indicated the potential for production of bioactive agents from endophytes of Bacopa monnieri.

  18. Green synthesis of silver nanoparticles using Ganoderma neo-japonicum Imazeki: a potential cytotoxic agent against breast cancer cells

    Science.gov (United States)

    Gurunathan, Sangiliyandi; Raman, Jegadeesh; Malek, Sri Nurestri Abd; John, Priscilla A; Vikineswary, Sabaratnam

    2013-01-01

    Background Silver nanoparticles (AgNPs) are an important class of nanomaterial for a wide range of industrial and biomedical applications. AgNPs have been used as antimicrobial and disinfectant agents due their detrimental effect on target cells. The aim of our study was to determine the cytotoxic effects of biologically synthesized AgNPs using hot aqueous extracts of the mycelia of Ganoderma neo-japonicum Imazeki on MDA-MB-231 human breast cancer cells. Methods We developed a green method for the synthesis of water-soluble AgNPs by treating silver ions with hot aqueous extract of the mycelia of G. neo-japonicum. The formation of AgNPs was characterized by ultraviolet-visible absorption spectroscopy, X-ray diffraction, dynamic light scattering, and transmission electron microscopy. Furthermore, the toxicity of synthesized AgNPs was evaluated using a series of assays: such as cell viability, lactate dehydrogenase leakage, reactive oxygen species generation, caspase 3, DNA laddering, and terminal deoxynucleotidyl transferase deoxyuridine triphosphate nick-end labeling in human breast cancer cells (MDA-MB-231). Results The ultraviolet-visible absorption spectroscopy results showed a strong resonance centered on the surface of AgNPs at 420 nm. The X-ray diffraction analysis confirmed that the synthesized AgNPs were single-crystalline, corresponding with the result of transmission electron microscopy. Treatment of MDA-MB-231 breast cancer cells with various concentrations of AgNPs (1–10 μg/mL) for 24 hours revealed that AgNPs could inhibit cell viability and induce membrane leakage in a dose-dependent manner. Cells exposed to AgNPs showed increased reactive oxygen species and hydroxyl radical production. Furthermore, the apoptotic effects of AgNPs were confirmed by activation of caspase 3 and DNA nuclear fragmentation. Conclusion The results indicate that AgNPs possess cytotoxic effects with apoptotic features and suggest that the reactive oxygen species generated by

  19. Cytotoxic activity of some medicinal plants from hamedan district of iran.

    Science.gov (United States)

    Behzad, Sahar; Pirani, Atefeh; Mosaddegh, Mahmoud

    2014-01-01

    Medicinal plants have been investigated for possible anti-cancer effects. The aim of the present study was to examine the cytotoxic activity of several medicinal plants on different tumor cell lines. 11 selected plant species which have been used in folkloric prescriptions were collected from different sites of Hamedan district of Iran. The methanolic extracts of the plants were prepared and their cytotoxic effects on four human cancer cell lines (A549, human lung adenocarcinoma; MCF7, human breast adenocarcinoma; HepG2, hepatocellular carcinoma and HT-29, human colon carcinoma) and one normal cell line (MDBK, bovine kidney) were examined using the MTT assay. Three of these were exhibited antiproliferative activity against one or more of the cell lines. The extract from Primula auriculata demonstrated the highest cytotoxicity with IC50 of 25.79, 35.79 and 43.34 μg.mL-1 against MCF7, HepG2 and HT- 29 cells, respectively. For some of the plants, their traditional use was correlated with the cytotoxic results, whereas for others the results may support the non-cytotoxicity of species used traditionally as natural remedies. The cytotoxic species could be considered as potential of anticancer compounds.

  20. Antiplasmodial activities and cytotoxic effects of aqueous extracts and sesquiterpene lactones from Neurolaena lobata.

    Science.gov (United States)

    François, G; Passreiter, C M; Woerdenbag, H J; Van Looveren, M

    1996-04-01

    Aqueous and lipophilic extracts of Neurolaena lobata (Asteraceae), obtained from Guatemala, were tested against Plasmodium falciparum in vitro. Moreover, sesquiterpene lactones, of the germacranolide and furanoheliangolide type, isolated from N. lobata, were shown to be active against P. falciparum in vitro. In addition to their antiplasmodial activity, their cytotoxic effects on human carcinoma cell lines were evaluated. Structure-activity relationships are discussed.

  1. 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.

  2. Synthesis of Chromonylthiazolidines and Their Cytotoxicity to Human Cancer Cell Lines

    Directory of Open Access Journals (Sweden)

    Hoang Le Tuan Anh

    2015-01-01

    Full Text Available Nine new chromonylthiazolidine derivatives were successfully semi-synthesized from paeonol. All of the compounds, including starting materials, the intermediate compound and products, were evaluated for their cytotoxic effects toward eight human cancer cell lines. The synthesized chromonylthiazolidines displayed weak cytotoxic effects against the tested cancer cell lines, but selective cytotoxic effects were observed. Compounds 3a and 3b showed the most selective cytotoxic effects against human epidermoid carcinoma (IC50 44.1 ± 3.6 μg/mL and breast cancer (IC50 32.8 ± 1.4 μg/mL cell lines, respectively. The results suggest that chromoylthiazolidines are potential low-cost, and selective anticancer agents.

  3. The Cytotoxicity of Elderberry Ribosome-Inactivating Proteins Is Not Solely Determined by Their Protein Translation Inhibition Activity.

    Directory of Open Access Journals (Sweden)

    Chenjing Shang

    Full Text Available Although the protein translation inhibition activity of ribosome inactivating proteins (RIPs is well documented, little is known about the contribution of the lectin chain to the biological activity of these proteins. In this study, we compared the in vitro and intracellular activity of several S. nigra (elderberry RIPs and non-RIP lectins. Our data demonstrate that RIPs from elderberry are much more toxic to HeLa cells than to primary fibroblasts. Differences in the cytotoxicity between the elderberry proteins correlated with differences in glycan specificity of their lectin domain, cellular uptake efficiency and intracellular destination. Despite the fact that the bulk of the RIPs accumulated in the lysosomes and partly in the Golgi apparatus, we could demonstrate effective inhibition of protein synthesis in cellula. As we also observed cytotoxicity for non-RIP lectins, it is clear that the lectin chain triggers additional pathways heralding cell death. Our data suggest that one of these pathways involves the induction of autophagy.

  4. Cytotoxic activity of water extracts of Trichilia hirta leaves on human tumor cells

    International Nuclear Information System (INIS)

    Hernandez Sosa, Edgar; Mora Gonzalez, Nestor; Morris Quevedo, Humberto J

    2013-01-01

    Trichilia hirta L. (Meliaceae) is traditionally used by patients suffering from cancer as an antitumoral resource. Therefore, the objectives of this study were to evaluate the cytotoxic activity of water extracts of Trichilia hirta leaves on tumour cells and identify through a phytochemical screening the principal families of phytocomponents contained in these extracts. The cytotoxic activity of these extracts was also evaluated on human melanoma cells (SK-mel-3) and human breast carcinoma (T-47D). The African green monkey kidney (AGMK) cells Cercopithecus aethiops (Vero) were used as a non-tumour cells control. The results showed the presence of triterpenes/steroids, saponins, coumarins, reductor sugars, phenols and tannins, flavonoids and carbohydrates/glycosides in the extracts. The water leaf extracts showed cytotoxic activity mainly on tumour cells, which contributes to explain the referred recovery by patients suffering form cancer that traditionally consume these extracts

  5. 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...

  6. Brine shrimp cytotoxicity of Caesalpinia pulcherrima aerial parts, antimicrobial activity and characterisation of isolated active fractions.

    Science.gov (United States)

    Chanda, Sumitra; Baravalia, Yogesh

    2011-12-01

    Caesalpinia pulcherrima Swartz. is an ornamental plant, shrub or a small tree belonging to the family Caesalpiniaceae. The plant has been used for the treatment of inflammatory disorders, skin diseases and so on. In this study, the cytotoxicity of the methanol extract of the aerial parts of C. pulcherrima was tested using an Artemia salina (brine shrimp) bioassay. Further, the methanol extract was fractionated by silica gel column chromatography using a solvent gradient of hexane:ethyl acetate:methanol in different ratios and 56 fractions were collected. On the basis of thin layer chromatography profiles, 13 major fractions were obtained, which were tested for antimicrobial activity against 14 microorganisms using the agar disc diffusion method and also tested for their minimal inhibitory concentration and minimal bactericidal concentration values. In terms of cytotoxicity, the extract caused 26% mortality of brine shrimp larvae after 24 h at a concentration of 1000 µg mL(-1). Fractions 3, 9 and 10 showed significant antimicrobial activities. Phytochemical analysis of these three fractions led to the identification of 11 compounds, and their structures were established by means of gas chromatography-mass spectroscopy techniques. These findings suggest that these bioactive compounds may be useful as potential antimicrobials. Further investigation is needed to establish the mode of action of these bioactive compounds.

  7. Effect of combustion condition on cytotoxic and inflammatory activity of residential wood combustion particles

    Science.gov (United States)

    Jalava, Pasi I.; Salonen, Raimo O.; Nuutinen, Kati; Pennanen, Arto S.; Happo, Mikko S.; Tissari, Jarkko; Frey, Anna; Hillamo, Risto; Jokiniemi, Jorma; Hirvonen, Maija-Riitta

    2010-05-01

    Residential heating is an important local source of fine particles and may cause significant exposure and health effects in populations. We investigated the cytotoxic and inflammatory activity of particulate emissions from normal (NC) and smouldering (SC) combustion in one masonry heater. The PM 1-0.2 and PM 0.2 samples were collected from the dilution tunnel with a high-volume cascade impactor (HVCI). Mouse RAW 264.7 macrophages were exposed to the PM-samples for 24 h. Inflammatory mediators, (IL-6, TNFα and MIP-2), and cytotoxicity (MTT-test), were measured. Furthermore, apoptosis and cell cycle of macrophages were analyzed. The HVCI particulate samples were characterized for ions, elements and PAH compounds. Assays of elemental and organic carbon were conducted from parallel low volume samples. All the samples displayed mostly dose-dependent inflammatory and cytotoxic activity. SC samples were more potent than NC samples at inducing cytotoxicity and MIP-2 production, while the order of potency was reversed in TNFα production. SC-PM 1-0.2 sample was a significantly more potent inducer of apoptosis than the respective NC sample. After adjustment for the relative toxicity with emission factor (mg MJ -1), the SC-PM emissions had clearly higher inflammatory and cytotoxic potential than the NC-PM emissions. Thus, operational practice in batch burning of wood and the resultant combustion condition clearly affect the toxic potential of particulate emissions.

  8. Evaluation of anti-cholinesterase, antibacterial and cytotoxic activities of green synthesized silver nanoparticles using from Millettia pinnata flower extract.

    Science.gov (United States)

    Rajakumar, Govindasamy; Gomathi, Thandapani; Thiruvengadam, Muthu; Devi Rajeswari, V; Kalpana, V N; Chung, Ill-Min

    2017-02-01

    The aim of this study is to develop an easy and eco-friendly method for the synthesis of Ag-NPs using extracts from the medicinal plant, Millettia pinnata flower extract and investigate the effects of Ag-NPs on acetylcholinesterase (AChE), butyrylcholinesterase (BChE), antibacterial and cytotoxicity activity. UV-Vis peak at 438 nm confirmed the Ag-NPs absorbance. The SEM analysis results confirmed the presence of spherical shaped Ag-NPs by a huge disparity in the particle size distribution with an average size of 49 ± 0.9 nm. TEM images revealed the formation of Ag-NPs with spherical shape and sizes in the range between 16 and 38 nm. The Ag-NPs showed an excellent inhibitory efficacy against AChE and BChE. The highest antibacterial activity was found against Escherichia coli (20.25 ± 0.91 mm). These nanoparticles showed the cytotoxic effects against brine shrimp (artemia saliana) nauplii with a LD 50 value of 33.92. Copyright © 2016 Elsevier Ltd. All rights reserved.

  9. 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.

  10. 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.

  11. 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.

  12. Synthesis, cytotoxicity and molecular modelling studies of new phenylcinnamide derivatives as potent inhibitors of cholinesterases.

    Science.gov (United States)

    Saeed, Aamer; Mahesar, Parvez Ali; Zaib, Sumera; Khan, Muhammad Siraj; Matin, Abdul; Shahid, Mohammad; Iqbal, Jamshed

    2014-05-06

    The present study reports the synthesis of cinnamide derivatives and their biological activity as inhibitors of both cholinesterases and anticancer agents. Controlled inhibition of brain acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) may slow neurodegeneration in Alzheimer's diseases (AD). The anticholinesterase activity of phenylcinnamide derivatives was determined against Electric Eel acetylcholinesterase (EeAChE) and horse serum butyrylcholinesterase (hBChE) and some of the compounds appeared as moderately potent inhibitors of EeAChE and hBChE. The compound 3-(2-(Benzyloxy)phenyl)-N-(3,4,5-trimethoxyphenyl)acrylamide (3i) showed maximum activity against EeAChE with an IC50 0.29 ± 0.21 μM whereas 3-(2-chloro-6-nitrophenyl)-N-(3,4,5-trimethoxyphenyl)acrylamide (3k) was proved to be the most potent inhibitor of hBChE having IC50 1.18 ± 1.31 μM. To better understand the enzyme-inhibitor interaction of the most active compounds toward cholinesterases, molecular modelling studies were carried out on high-resolution crystallographic structures. The anticancer effects of synthesized compounds were also evaluated against cancer cell line (lung carcinoma). The compounds may be useful leads for the design of a new class of anticancer drugs for the treatment of cancer and cholinesterase inhibitors for Alzheimer's disease (AD). Copyright © 2014 Elsevier Masson SAS. All rights reserved.

  13. Flavonoids from Heliotropium subulatum exudate and their evaluation for antioxidant, antineoplastic and cytotoxic activities II.

    Science.gov (United States)

    Singh, Bharat; Sahu, Pooran M; Sharma, Ram A

    2017-02-01

    The flavonoids are the largest group of phenolic compounds isolated from a wide range of higher plants. These compounds work as antimicrobials, anti-insect agents and protect plants from other types of biotic and abiotic stresses. Various researchers have suggested that flavonoids possessed antioxidant, antineoplastic and cytotoxic activities. The main objective of this study was to test dichloromethane fraction of resinous exudate of Heliotropium subulatum for their antioxidant, antineoplastic and cytotoxic activities, as well as to search new antioxidant and antineoplastic agents for pharmaceutical formulations. Five flavonoids were isolated from resinous exudate of this plant species and screened for their in vitro and in vivo antioxidant models (DPPH radical scavenging, reducing power, superoxide anion scavenging, metal chelating scavenging systems, catalase and lipid peroxidation), antineoplastic (Sarcoma 180), and cytotoxic (Chinese hamster V79 cells) activities. Tricetin demonstrated maximum antioxidant activity against both in vitro and in vivo experimental systems while galangin exhibited maximum inhibition (78.35%) at a dose of 10 µg/kg/day against Sarcoma 180. Similarly, it was found that galangin also showed highest activity (21.1 ± 0.15%) at a concentration of 70 µg/ml to Chinese hamster V79 cells. The observed results suggest that tricetin has a potential to scavenge free radicals in both in vitro and in vivo models while the galangin could be considered as antitumor and cytotoxic agent.

  14. Surface active monomers synthesis, properties, and application

    CERN Document Server

    Borzenkov, Mykola

    2014-01-01

    This brief includes information on the background?of and development of synthesis of various types of surface active monomers. The authors explain the importance of utilization of surface active monomers for creation of surface active polymers? and the various biomedical applications of such compounds . This brief introduces techniques for the synthesis of novel types of surface active monomers, their colloidal and polymerizable properties and application for needs of medicine and biology.

  15. Cytotoxicity and genotoxicity of clothianidin in human lymphocytes with or without metabolic activation system.

    Science.gov (United States)

    Atlı Şekeroğlu, Zülal; Şekeroğlu, Vedat; Uçgun, Ebru; Kontaş Yedier, Seval; Aydın, Birsen

    2018-02-26

    Clothianidin (CHN) is a broad-spectrum neonicotinoid insecticide. Limited studies have been carried out on the cytotoxic and genotoxic effects of both CHN using different genotoxicity tests in human cells with or without human metabolic activation system (S9 mix). Therefore, the aim of this study is to investigate the cytotoxic and genotoxic effects of CHN and its metabolites on human lymphocyte cultures with or without S9 mix using chromosomal aberration (CA) and micronucleus (MN) tests. The cultures were treated with 25, 50, and 100 µg/ml of CHN in the presence (3 h treatment) and absence (48 h treatment) of S9 mix. Dimethyl sulfoxide (DMSO) was used as a solvent control. CHN showed cytotoxic and genotoxic effects due to significant decreases in mitotic index (MI) and nuclear division index (NDI), and significant increases in the CAs, aberrant cells, and MN formation in the absence of S9 mix when compared with solvent control. However, CHN did not significantly induce cytotoxicity and genotoxicity in the presence of S9 mix. Our results indicated that CHN has cytotoxic, cytostatic, and genotoxic potential on human peripheral blood lymphocyte cultures, but not its metabolites under the experimental conditions.

  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. Brosimacutins J-M, four new flavonoids from Brosimum acutifolium and their cytotoxic activity.

    Science.gov (United States)

    Takashima, Junko; Komiyama, Kanki; Ishiyama, Haruaki; Kobayashi, Jun'ichi; Ohsaki, Ayumi

    2005-07-01

    Four new flavonoids, brosimacutins J-M (1 - 4), were isolated from the bark of Brosimum acutifolium Huber together with a known flavan, brosimine A (5). The structures of compounds 1-4 were elucidated by spectroscopic means. 27 constituents of this plant including compounds 1-5 were evaluated for their cytotoxic activity against murine leukemia P388 cells. Although no compounds tested had any reversal effect on vincristine resistance, brocimacutins J-M (1-4) were cytotoxic to vincristine-resistant P388 cells (IC50 4.4 - 19 microg/mL).

  18. 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.

  19. Cytotoxic activity of ethanolic extract of the marine sponge Aaptos suberitoides against T47D cell

    Science.gov (United States)

    Nurhayati, Awik Puji Dyah; Prastiwi, Rarastoeti; Sukardiman, Wahyuningsih, Tri

    2018-04-01

    Aaptos suberitoides marine sponge produce many kinds of secondary metabolites. The purpose of this study were to examine the cytotoxic, proliferation inhibition and apoptosis induction of marine sponge A.suberitoides. The sponge was extracted with 96 % ethanol. Ethanol extract cytotoxicity assay were performed with MTT method (Microculture Tetrazolium) against to cell line of T47D. The proliferation inhibition were done by doubling time. The apoptosis induction by observing the treated cell morphology after staining with acrydine orange. The results show that cytotoxic activity of the ethanol extract was 153.109 µg/mL, inhibits cell proliferation cell lines of T47D at 24 hours of incubation and apoptosis induction.

  20. 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.

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

    African Journals Online (AJOL)

    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) was evaluated on leukaemic cancer cell line (K-562) and Mardin-Darby kidney cell line (MDBK) ...

  3. 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.

  4. 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 ...

  5. 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 ...

  6. The antioxidant and cytotoxic activities of Sonchus oleraceus L. extracts

    OpenAIRE

    Yin, Jie; Kwon, Gu-Joong; Wang, Myeong-Hyeon

    2007-01-01

    This study investigated in vitro antioxidant activity of Sonchus oleraceus L. by extraction solvent, which were examined by reducing power, hydroxyl radical-scavenging activity(HRSA) and 1, 1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging assays. 70% MeOH extract had the greatest reducing power while EtOH extract had the greatest HRSA. The antioxidant activity of S. oleraceus extracts was concentration dependent and its IC50 values ranged from 47.1 to 210.5 ?g/ml and IC50 of 70% MeOH, bo...

  7. Antimicrobial, antioxidant and cytotoxic activities of propolis from Melipona orbignyi (Hymenoptera, Apidae).

    Science.gov (United States)

    Campos, Jaqueline Ferreira; dos Santos, Uilson Pereira; Macorini, Luis Fernando Benitez; de Melo, Adriana Mary Mestriner Felipe; Balestieri, José Benedito Perrella; Paredes-Gamero, Edgar Julian; Cardoso, Claudia Andrea Lima; de Picoli Souza, Kely; dos Santos, Edson Lucas

    2014-03-01

    Propolis from stingless bees is well known for its biologic properties; however, few studies have demonstrated these effects. Therefore, this study aimed to investigate the chemical composition and antimicrobial, antioxidant and cytotoxic activities of propolis from the stingless bee Melipona orbignyi, found in Mato Grosso do Sul, Brazil. The chemical composition of the ethanol extract of propolis (EEP) indicated the presence of aromatic acids, phenolic compounds, alcohols, terpenes and sugars. The EEP was active against the bacterium Staphylococcus aureus and the fungus Candida albicans. The EEP showed antioxidant activity by scavenging free radicals and inhibiting hemolysis and lipid peroxidation in human erythrocytes incubated with an oxidizing agent. Additionally, EEP promoted cytotoxic activity and primarily necrotic death in K562 erythroleukemia cells. Taken together, these results indicate that propolis from M. orbignyi has therapeutic potential for the treatment and/or prevention of diseases related to microorganism activity, oxidative stress and tumor cell proliferation. Copyright © 2014 Elsevier Ltd. All rights reserved.

  8. 1 Antibacterial and cytotoxic activities of Terminalia stenostachya ...

    African Journals Online (AJOL)

    activities of extracts of Terminalia stenostachya Engl. & Diels and Terminalia ... leprosy, nosebleeds, oedema, pneumonia, skin diseases, sore throats, dental caries, ..... Helicobacter pylori and Candida spp. to the east African plant Terminalia ...

  9. Synthesis of novel chalcone derivatives by conventional and microwave irradiation methods and their pharmacological activities

    Directory of Open Access Journals (Sweden)

    Mohammed Rayees Ahmad

    2016-09-01

    Full Text Available Chalcones are abundant in edible plants and are considered to be the precursors of flavonoids and isoflavonoids. Chalcones belong to an important class of flavonoids, which may be prepared by Claisen–Schmidt condensation. They possess a wide range of biological activities and industrial applications. The cytotoxicity against tumour cell lines may be the result of disruption of the cell cycle, inhibition of angiogenesis, interference with p53-MDM2 interaction, mitochondrial uncoupling or induction of apoptosis. Chalcones are synthesized by conventional and microwave assisted synthesis methods. By microwave assisted synthesis, a considerable increase in the reaction rate has been observed and that too, with better yields. The compounds have been screened for cytotoxic activity and antioxidant activity.

  10. Short synthesis and antimalarial activity of fagaronine

    OpenAIRE

    Rivaud, M.; Mendoza, A.; Sauvain, Michel; Valentin, A.; Jullian, Valérie

    2012-01-01

    Herein, we report a new synthesis of fagaronine 1, inspired by the synthesis reported by Luo for nornitidine. The in vitro biological activity of fagaronine against malaria on several chloroquine-sensitive and resistant Plasmodium falciparum strains was confirmed, and the selectivity index compared to mammalian cells was calculated. Fagaronine was found to have very good antimalarial activity in vivo, comparable to the activity of the reference compound chloroquine. Therefore, fagaronine appe...

  11. 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

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

    Directory of Open Access Journals (Sweden)

    Susi Endrini

    2014-12-01

    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 ìg/ml and 14.678 mg/ml, respectively. Ethanolic pearl grass extract (PE showed similar results, with IC50 values of 65.011 mg/ml on 24-hour incubation time and 52.329 mg/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.

  13. 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.

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

    African Journals Online (AJOL)

    residue left after maceration of fresh fruits (RFW) showed moderate superoxide radical-scavenging activity relative ... become purplish red to dark purple depending on the level of ... mamao juice and wine, exhibited antioxidant potential ... regarding health benefits of Antidesma .... amount of total phenolic content, which was.

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

    African Journals Online (AJOL)

    SERVER

    2007-08-06

    Aug 6, 2007 ... four human liver cancer (7703, HepG2, 7721, PLC) and four human breast cancer (Bcap37, ZR75-30,. MCF-7, T-47D) cell lines ... Key words: Coriolus versicolor, fruit body, polysaccharide, anti-tumor. INTRODUCTION. Coriolus ... somewhat in structure, composition, and physiological activity. The present ...

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

    African Journals Online (AJOL)

    positive and Gram-negative bacteria, respectively. The bacterial plates were incubated at 37 °C for 24 h. After incubation, the diameter of the inhibition zone was measured to evaluate the anti- microbial activity. Each test was performed twice.

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

    African Journals Online (AJOL)

    Results: Two saponins were isolated from the ethyl acetate extract. The ethyl acetate ... 57.7 ± 12.1 µg/mL). Saponin 2 exhibited high activity against intracellular amastigotes ..... implication, and technological consideration. J Food Sci. 2007 ...

  18. Flavonoids, anti-inflammatory activity and cytotoxicity of Macfadyena ...

    African Journals Online (AJOL)

    kaempferol, 7-O, 8-C diglucoside and vicenin II were isolated, while 6, methoxy, acacetin 7-O glucoside; and quercitrin were isolated from ethanol extract. These compounds were characterized and identified by their physicochemical and spectral data. The crude ethanol extract exhibited significant anti-inflammatory activity ...

  19. 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

  20. 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 ...

  1. CYTOTOXIC, α-CHYMOTRYPSIN AND UREASE INHIBITION ACTIVITIES OF THE PLANT Heliotropium dasycarpum L.

    Science.gov (United States)

    Ghaffari, Muhammad Abuzar; Chaudhary, Bashir Ahmed; Uzair, Muhammad; Ashfaq, Khuram

    2016-01-01

    The aim of this study was to investigate Cytotoxic, α-Chymotrypsin and Urease inhibition activities of the plant Heliotropium dasycarpum . Dichloromethane and methanol extracts of the plant were evaluated for cytotoxic, α-Chymotrypsin and Urease inhibition by using in vivo Brine Shrimp lethality bioassay and in vitro enzymatic inhibition assays respectively. The methanol extract of the plant exhibited significant cytotoxic activity. Out of 30 brine shrimp larvae, 2 (6%), 26 (86%) and 28 (93%) larvae were survived at concentration of 1000μg/ml, 100μg/ml and 10μg/ml respectively with LD50; 215.837. Similarly 21 (70%), 25 (83%), 29 (96%) larvae were survived of dichloromethane plant extract with LD50; 6170.64. The methanol and dichloromethane extract exhibited 10.50±0.18% and 41.51±0.15% α-chymotrypsin enzyme inhibition respectively with IC 50 values of greater than 500 μmol. The methanol extract showed 24.39±0.21% Urease enzyme inhibition with IC 50 values of greater than 400 μmol While dichloromethane extract has 11.46±0.09% enzyme inhibition with IC 50 values of greater than 500 μmol. The results clearly indicated that Heliotropium dasycarpum has cytotoxic potential and enzyme inhibition properties. Further study is needed to screen out antitumor and anti-ulcerative agents.

  2. 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.

  3. 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.

  4. 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 OBOR OECD: Hematology Impact factor: 1.683, year: 2016

  5. Design, Synthesis and Cytotoxic Evaluation of o-Carboxamido Stilbene Analogues

    Directory of Open Access Journals (Sweden)

    Mohamad Nurul Azmi

    2013-11-01

    Full Text Available Resveratrol, a natural stilbene found in grapes and wines exhibits a wide range of pharmacological properties. Resveratrol is also known as a good chemopreventive agent for inhibiting carcinogenesis processes that target kinases, cyclooxygenases, ribonucleotide reductase and DNA polymerases. A total of 19 analogues with an amide moiety were synthesized and the cytotoxic effects of the analogues on a series of human cancer cell lines are reported. Three compounds 6d, 6i and 6n showed potent cytotoxicity against prostate cancer DU-145 (IC50 = 16.68 µM, colon cancer HT-29 (IC50 = 7.51 µM and breast cancer MCF-7 (IC50 = 21.24 µM, respectively, which are comparable with vinblastine. The resveratrol analogues were synthesized using the Heck method.

  6. Revealing the Cytotoxicity of Residues of Phosphazene Catalysts Used for Synthesis of Poly(ethylene oxide)

    KAUST Repository

    Xia, Yening

    2017-08-24

    We herein report a case study on the toxicity of residual catalyst in metal-free polymer. Eight-arm star-like poly(ethylene oxide)s were successfully synthesized via phosphazene-catalyzed ring-opening polymerization of ethylene oxide using sucrose as an octahydroxy initiator. The products were subjected to MTT assay using human cancer cell lines (MDA-MB-231 and A2780). Comparison between the crude and purified products clearly revealed that the residual phosphazenium salts were considerably cytotoxic regardless of the anionic species, and that the cytotoxicity of more bulky t-BuP4 salt was higher than that of t-BuP2 salt. Such results have therefore put forward the necessity for removal of the catalyst residues from PEO-based polymers synthesized through phosphazene catalysis for bio-related applications, and for the development of less or non-toxic organocatalysts for such polymers.

  7. Revealing the Cytotoxicity of Residues of Phosphazene Catalysts Used for Synthesis of Poly(ethylene oxide)

    KAUST Repository

    Xia, Yening; Shen, Jizhou; Alamri, Haleema; Hadjichristidis, Nikolaos; Zhao, Junpeng; Wang, Yucai; Zhang, Guangzhao

    2017-01-01

    We herein report a case study on the toxicity of residual catalyst in metal-free polymer. Eight-arm star-like poly(ethylene oxide)s were successfully synthesized via phosphazene-catalyzed ring-opening polymerization of ethylene oxide using sucrose as an octahydroxy initiator. The products were subjected to MTT assay using human cancer cell lines (MDA-MB-231 and A2780). Comparison between the crude and purified products clearly revealed that the residual phosphazenium salts were considerably cytotoxic regardless of the anionic species, and that the cytotoxicity of more bulky t-BuP4 salt was higher than that of t-BuP2 salt. Such results have therefore put forward the necessity for removal of the catalyst residues from PEO-based polymers synthesized through phosphazene catalysis for bio-related applications, and for the development of less or non-toxic organocatalysts for such polymers.

  8. Synthesis, cytotoxicity, cellular uptake and influence on eicosanoid metabolism of cobalt-alkyne modified fructoses in comparison to auranofin and the cytotoxic COX inhibitor Co-ASS.

    Science.gov (United States)

    Ott, Ingo; Koch, Thao; Shorafa, Hashem; Bai, Zhenlin; Poeckel, Daniel; Steinhilber, Dieter; Gust, Ronald

    2005-06-21

    Propargylhexacarbonyldicobalt complexes with fructopyranose ligands were prepared and investigated for cytotoxicity in the MCF-7 human breast cancer cell line. The antiproliferative effects depended on the presence of isopropylidene protecting groups in the carbohydrate ligand and correlated with the cellular concentration of the complexes. IC(50) values of > 20 microM demonstrated that the fructose derivatives were only moderately active compared to the references auranofin and the aspirin (ASS) derivative [2-acetoxy(2-propynyl)benzoate]hexacarbonyldicobalt (Co-ASS). In continuation of our studies on the mode of action of cobalt-alkyne complexes we studied the influence of the compounds on the formation of 12-HHT (COX-1 product) and 12-HETE (12-LOX product) by human platelets as an indication of the interference in the eicosanoid metabolism, which is discussed as a target system of cytostatics. Co-ASS was an efficient COX-1 inhibitor without LOX inhibitory activity and auranofin inhibited both COX-1 and 12-LOX eicosanoid production. The missing activity of the fructopyranose complexes at the 12-LOX and the only moderate effects at COX-1 indicate that COX/LOX inhibition may be in part responsible for the pharmacological effects of auranofin and Co-ASS but not for those of the fructopyranose complexes.

  9. Mn-Zn ferrite nanoparticles with silica and titania coatings: synthesis, transverse relaxivity and cytotoxicity

    Czech Academy of Sciences Publication Activity Database

    Kaman, Ondřej; Kuličková, Jarmila; Maryško, Miroslav; Veverka, Pavel; Herynek, V.; Havelek, R.; Královec, K.; Kubániová, D.; Kohout, J.; Dvořák, P.; Jirák, Zdeněk

    2017-01-01

    Roč. 53, č. 11 (2017), s. 1-8, č. článku 5300908. ISSN 0018-9464 R&D Projects: GA ČR GA16-04340S Institutional support: RVO:68378271 Keywords : amorphous titania * silica * magnetic nanoparticles * Mn-Zn ferrite * transverse relaxivity * cytotoxicity Subject RIV: BM - Solid Matter Physics ; Magnetism OBOR OECD: Condensed matter physics (including formerly solid state physics, supercond.) Impact factor: 1.243, year: 2016

  10. Synthesis and absolute configurations of the cytotoxic polyacetylenes isolated from the callus of Panax ginseng.

    Science.gov (United States)

    Fujimoto, Y; Satoh, M; Takeuchi, N; Kirisawa, M

    1990-06-01

    Panaxacol (1) and dihydropanaxacol (2), cytotoxic polyacetylenes isolated from the callus of Panax ginseng, were synthesized starting from D-(-)-diethyl tartrate. The absolute configuration of 1 was determined to be 9R, 10R and the absolute configuration at C-3 of 2 was tentatively assigned as 3S by the application of the R(+)-alpha-methoxy-alpha-(trifluoro methyl)phenylacetyl (MTPA) method.

  11. Nitric oxide-releasing nanoparticles: synthesis, characterization, and cytotoxicity to tumorigenic cells

    Energy Technology Data Exchange (ETDEWEB)

    Pelegrino, Milena T. [Universidade Federal de São Paulo, Exact and Earth Sciences Department (Brazil); Silva, Letícia C.; Watashi, Carolina M. [Universidade Federal do ABC, UFABC, Center of Natural and Human Sciences (Brazil); Haddad, Paula S. [Universidade Federal de São Paulo, Exact and Earth Sciences Department (Brazil); Rodrigues, Tiago; Seabra, Amedea B., E-mail: amedea.seabra@ufabc.edu.br [Universidade Federal do ABC, UFABC, Center of Natural and Human Sciences (Brazil)

    2017-02-15

    Nitric oxide (NO) is involved in several biological processes, including toxicity against tumor cells. The aim of this study was to synthesize, characterize, and evaluate the cytotoxicity of NO-releasing chitosan nanoparticles. A thiol-containing molecule, mercaptosuccinic acid (MSA), was encapsulated (encapsulation efficiency of 99%) in chitosan/sodium tripolyphosphate nanoparticles (CS NPs). The obtained nanoparticles showed an average hydrodynamic size of 108.40 ± 0.96 nm and polydispersity index of 0.26 ± 0.01. MSA-CS NPs were nitrosated leading to S-nitroso-MSA-CS NPs, which act as NO donor. The cytotoxicity of CS NPs, MSA-CS NPs, and S-nitroso-MSA-CS NPs were evaluated in several tumor cells, including human hepatocellular carcinoma (HepG2), mouse melanoma (B16F10), and human chronic myeloid leukemia (K562) cell lines and Lucena-1, a vincristine-resistant K562 cell line. Both CS NPs and MSA-CS NPs did not cause toxic effects in these cells, whereas S-nitroso-MSA-CS NPs caused potent cytotoxic effects in all the tested tumor cell lines. The half-maximal inhibitory concentration values of S-nitroso-MSA-CS NPs were 19.7, 10.5, 22.8, and 27.8 μg·mL{sup −1} for HepG2, B16F10, K562, and Lucena-1 cells, respectively. In contrast, S-nitroso-MSA-CS NPs exhibited lower cytotoxic to non-tumorigenic melanocytes (Melan-A) when compared with melanoma B16F10. Therefore, the results highlight the potential use of NO-releasing CS NPs in antitumor chemotherapy.

  12. Microbial-assisted synthesis and evaluation the cytotoxic effect of tellurium nanorods

    Energy Technology Data Exchange (ETDEWEB)

    Forootanfar, Hamid [Herbal and Traditional Medicines Research Center, Kerman University of Medical Sciences, Kerman (Iran, Islamic Republic of); Amirpour-Rostami, Sahar; Jafari, Mandana [Pharmaceutics Research Center, Institute of Neuropharmacology, Kerman University of Medical Sciences, Kerman (Iran, Islamic Republic of); Forootanfar, Amir [Department of Pharmacology and Toxicology, Faculty of Pharmacy, Mashhad University of Medical Sciences, Mashhad (Iran, Islamic Republic of); Yousefizadeh, Zahra [The Student Research Committee, Faculty of Pharmacy, Kerman University of Medical Sciences, Kerman (Iran, Islamic Republic of); Shakibaie, Mojtaba, E-mail: shakiba@kmu.ac.ir [Pharmaceutics Research Center, Institute of Neuropharmacology, Kerman University of Medical Sciences, Kerman (Iran, Islamic Republic of)

    2015-04-01

    The present study was designed to isolate bacterial strain capable of tellurium nanorods' (Te NRs) production followed by purification and evaluation of the cytotoxic effect of Te NRs. Among 25 environmental samples collected for screening of Te NR-producer bacterial strains one bacterial colony (isolated from hot spring and identified as Pseudomonas pseudoalcaligenes strain Te) was selected and applied for biosynthesis of Te NRs. Thereafter, an organic–aqueous partitioning system was applied for the purification of the biogenic Te NRs and the purified Te NRs were characterized using transmission electron microscopy (TEM), scanning electron microscopy (SEM), energy dispersive X-ray (EDX), X-ray diffraction spectroscopy (XRD), UV–visible spectroscopy, and Fourier transform infrared spectroscopy (FTIR) techniques. The cytotoxic effect of biologically synthesized Te NRs and potassium tellurite on four cell lines of MCF-7, HT1080, HepG2 and A549 was then determined using the MTT assay method. The obtained results revealed lower toxicity for the rod-shaped biogenic tellurium nanostructures (~ 22 nm diameter by 185 nm length) compared to K{sub 2}TeO{sub 3}. - Highlights: • Te NR producing bacterial strain were isolated from hot springs. • Organic–aqueous partitioning system was applied for purification of Te nanorods. • The rod-shaped biogenic Te NPs showed lower cytotoxicity compared to K{sub 2}TeO{sub 3}.

  13. Microbial-assisted synthesis and evaluation the cytotoxic effect of tellurium nanorods

    International Nuclear Information System (INIS)

    Forootanfar, Hamid; Amirpour-Rostami, Sahar; Jafari, Mandana; Forootanfar, Amir; Yousefizadeh, Zahra; Shakibaie, Mojtaba

    2015-01-01

    The present study was designed to isolate bacterial strain capable of tellurium nanorods' (Te NRs) production followed by purification and evaluation of the cytotoxic effect of Te NRs. Among 25 environmental samples collected for screening of Te NR-producer bacterial strains one bacterial colony (isolated from hot spring and identified as Pseudomonas pseudoalcaligenes strain Te) was selected and applied for biosynthesis of Te NRs. Thereafter, an organic–aqueous partitioning system was applied for the purification of the biogenic Te NRs and the purified Te NRs were characterized using transmission electron microscopy (TEM), scanning electron microscopy (SEM), energy dispersive X-ray (EDX), X-ray diffraction spectroscopy (XRD), UV–visible spectroscopy, and Fourier transform infrared spectroscopy (FTIR) techniques. The cytotoxic effect of biologically synthesized Te NRs and potassium tellurite on four cell lines of MCF-7, HT1080, HepG2 and A549 was then determined using the MTT assay method. The obtained results revealed lower toxicity for the rod-shaped biogenic tellurium nanostructures (~ 22 nm diameter by 185 nm length) compared to K 2 TeO 3 . - Highlights: • Te NR producing bacterial strain were isolated from hot springs. • Organic–aqueous partitioning system was applied for purification of Te nanorods. • The rod-shaped biogenic Te NPs showed lower cytotoxicity compared to K 2 TeO 3

  14. Screening of Baccaurea ramiflora (Lour.) extracts for cytotoxic, analgesic, anti-inflammatory, neuropharmacological and antidiarrheal activities.

    Science.gov (United States)

    Nesa, Mst Luthfun; Karim, S M Sajedul; Api, Khairunasa; Sarker, Md Moklesur Rahman; Islam, Md Monirul; Kabir, Asma; Sarker, Mithun Kumar; Nahar, Kamrun; Asadujjaman, Mohammad; Munir, Mohammad Sirajum

    2018-01-30

    It has been observed that the various part of Baccaurea ramiflora plant is used in rheumatoid arthritis, cellulitis, abscesses, constipation and injuries. This plant also has anticholinergic, hypolipidemic, hypoglycemic, antiviral, antioxidant, diuretic and cytotoxic activities. The present studyaimed to assess the cytotoxic, analgesic, anti-inflammatory, CNS depressant and antidiarrheal activities of methanol extract of Baccaurea ramiflora pulp and seeds in mice model. The cytotoxic activity was determined by brine shrimp lethality bioassay; anti-nociceptive activity was determined by acetic acid-induced writhing, formalin- induced licking and biting, and tail immersion methods. The anti-inflammatory, CNS depressant and anti-diarrheal activities were assessed by carrageenan-induced hind paw edema, the open field and hole cross tests, and castor oil-induced diarrheal methods, respectively. The data were analyzed by one way ANOVA (analysis of variance) followed by Dunnett's test. In brine shrimp lethality bioassay, the LC 50 values of the methanol extracts of Baccaurea ramiflora pulp and seed were 40 μg/mL and 10 μg/mL, respectively. Our investigation showed that Baccaurea ramiflora pulp and seed extracts (200 mg/kg) inhibited acetic acid induced pain 67.51 and 66.08%, respectively (p analgesic, anti-inflammatory, CNS depressant and antidiarrheal activities of methanol extract of Baccaurea ramiflora pulp and seeds (200 mg/kg).

  15. Anti-Melanogenic Activity and Cytotoxicity of Pistacia vera Hull on Human Melanoma SKMEL-3 Cells.

    Science.gov (United States)

    Sarkhail, Parisa; Salimi, Mona; Sarkheil, Pantea; Mostafapour Kandelous, Hirsa

    2017-07-01

    Pistacia vera seed is a common food and medicinal seed in Iran. It's hull (outer skin) as a significant byproduct of pistachio, is traditionally used as tonic, sedative and antidiarrheal and has been shown to be a rich source of antioxidants. The aim of the present study is to evaluate the anti-melanogenic activity of the pistachio hulls in order to discover a new alternative herbal agent to treat skin hyperpigmentation disorders. In this work, antioxidant and anti-tyrosinase activity of MeOH extract from Pistacia vera hull (MPH) were evaluated in vitro, respectively, by DPPH radical scavenging and mushroom tyrosinase activity assays. Then the effect of MPH on the melanin content, cellular tyrosinase activity and cytotoxicity (MTT assay) on human melanoma SKMEL-3 cell were determined followed by 72 h incubation. The results indicated that MPH had valuable DPPH radical scavenging effect and weak anti-tyrosinase activity when compared to the well-known antioxidant (BHT) and tyrosinase inhibitor (kojic acid), respectively. MPH, at a high dose (0.5 mg/mL), showed significant cytotoxic activity (~63%) and strong anti-melanogenic effect (~57%) on SKMEL-3 cells. The effect of MPH in the reduction of melanin content may be related to its cytotoxicity. The results obtained suggest that MPH can be used as an effective agent in the treatment of some skin hyperpigmentation disorders such as melanoma.

  16. Antioxidant, phytotoxic and cytotoxic activity of methanolic extract of Trigonella foenum-graecum

    Directory of Open Access Journals (Sweden)

    Amin Ullah

    2016-05-01

    Full Text Available Objective: To analyze the methanol extract of Trigonella foenum-graecum (T. foenumgraecum for antioxidant, phytotoxic and cytotoxic activity. Methods: The powder of T. foenum-graecum was extracted in diluted methanol with the help of random shaking method. All extracts of the plant were measured for cytotoxic activity (beside brine shrimp and antioxidant activity vs. 1, 1-diphenyl-2-picrylhydrazyl free radical. Results: Various concentrations of methanolic extract of T. foenum-graecum were observed as 36.16% to 54.12% with rising concentrations of 50 to 1000 μg/mL. Significantly phytotoxic activity (100 and 1000 μg/mL reduced the growth of roots (radicals and shoots (hypocotyls of rice when compared to control after 3 and 7 days’ treatment. At a concentration of 10 μg/ mL, the survival rate of cytotoxic activity of brine shrimp was maximum and at a concentration of 250 μg/mL, the death rate of brine shrimp was maximum. Conclusions: T. foenum-graecum has potential activity against free radical mediated sickness and thus it is possible to treat cancer.

  17. Antihyperlipidemic, Antioxidant and Cytotoxic Activities of Methanolic and Aqueous Extracts of Different Parts of Star Fruit.

    Science.gov (United States)

    Saghir, Sultan A M; Sadikun, Amirin; Al-Suede, Fouad S R; Majid, Amin M S A; Murugaiyah, Vikneswaran

    Star fruit (Averrhoa carambola) is a well-known plant in Malaysia which bears a great significance in traditional medicine. This study aimed to evaluate the antihyperlipidemic effect, antioxidant potential and cytotoxicity of aqueous and methanolic extracts of ripe and unripe fruits, leaves and stem of A. carambola. Antihyperlipidemic activity was assessed in poloxamer-407 (P-407) induced acute hyperlipidemic rat's model. The antioxidant activity was assessed in vitro using 2, 2'-azino-bis (3-ethylbenzthiazoline-6-sulphonic acid) (ABTS) radical scavenging, 1-diphenyl-2-dipicrylhydrazyl radical scavenging (DPPH) and ferric reducing antioxidant power (FRAP) assays. In addition, cytotoxicity of A. carambola extracts was assessed using MTS assay on four leukemic cell lines (human colon cancer, human promyeloid leukemia, erythroid leukemia, acute myeloid leukemia) and one normal cell (human umbilical vein endothelial cells). Methanolic extract of leaves had the most potent antihyperlipidemic activity in P-407 model, whereby it significantly reduced serum levels of total cholesterol (Pcarambola stem and leaves showed the strongest antioxidant activity. Total phenolic and flavonoid contents of the extracts exhibited significant correlations with antioxidant but not with antihyperlipidemic activities. All plant parts showed no cytotoxic effect on the selected cancer or normal cell lines. Antihyperlipidemic activity of different parts of A. carambola is greatly affected by extraction solvents used. Methanolic extract of A. carambola leaves exhibited higher antihyperlipidemic and antioxidant potentials compared to other parts of the plant.

  18. 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.

  19. 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

  20. Oxcarbazepine-induced cytotoxicity and genotoxicity in human lymphocyte cultures with or without metabolic activation.

    Science.gov (United States)

    Atlı Şekeroğlu, Zülal; Kefelioğlu, Haluk; Kontaş Yedier, Seval; Şekeroğlu, Vedat; Delmecioğlu, Berrin

    2017-03-01

    There has been considerable debate about the relationship between epilepsy and cancer. Oxcarbazepine (OXC) is used for treating certain types of seizures in patients with epilepsy. There have been no detailed investigations about genotoxicity of OXC and its metabolites. Therefore, the aim of this study is to investigate the cytotoxic and genotoxic effects of OXC and its metabolites on cultured human lymphocytes. The cytotoxicity and genotoxicity of OXC on human peripheral blood lymphocytes were examined in vitro by sister chromatid exchange (SCE), chromosomal aberration (CA) and micronucleus (MN) tests. Cultures were treated with 125, 250 and 500 μg/ml of OXC in the presence (3 h treatment) and absence (24 h and 48 h treatment) of a metabolic activator (S9 mix). Dimethyl sulfoxide (DMSO) was used as a solvent control. OXC showed cytotoxic activities due to significant decreases in mitotic index (MI), proliferation index (PI) and nuclear division index (NDI) in the absence of S9 mix when compared with solvent control. Metabolites of OXC also significantly reduced MI and PI in cultures with S9 mix. OXC significantly increased the CAs, aberrant cells, SCE and MN values in the presence and absence of S9 mix. Our results indicated that both OXC and its metabolites have cytotoxic, cytostatic and genotoxic potential on human peripheral blood lymphocyte cultures under the experimental conditions. Further studies are necessary to elucidate the relationship between cytotoxic, cytostatic and genotoxic effects, and to make a possible risk assessment in patients receiving therapy with this drug.

  1. Synthesis and Cytotoxicity Evaluation of 13-n-Alkyl Berberine and Palmatine Analogues as Anticancer Agents

    Directory of Open Access Journals (Sweden)

    Lei Zhang

    2012-09-01

    Full Text Available By introducing long carbon-chain alkyl groups at the C-13 position of berberine and palmatine, 13-n-hexyl/13-n-octyl berberine and palmatine chloride analogues 4ad were synthesized and examined by MTT assays for cytotoxic activity in seven human cancer cell lines (7701QGY, SMMC7721, HepG2, CEM, CEM/VCR, KIII, Lewis, yielding IC50 values of 0.02 ± 0.01–13.58 ± 2.84 μM. 13-n-Octyl palmatine (compound 4d gave the most potent inhibitor activity, with an IC50 of 0.02 ± 0.01 μM for SMMC7721. In all cases, the 13-n-alkyl berberine and palmatine analogues 4ad were more cytotoxic than berberine and palmatine. In addition, compounds 4ad also exhibited more potent cytotoxicity than berberine and palmatine in mice with S180 sarcoma xenografted in vivo. The primary screening results indicated that the 13-n-hexyl/13-n-octyl berberine and palmatine analogues might be valuable source for new potent anticancer drug candidates.

  2. Antioxidant and cytotoxic activity of new di- and polyamine caffeine analogues.

    Science.gov (United States)

    Jasiewicz, Beata; Sierakowska, Arleta; Jankowski, Wojciech; Hoffmann, Marcin; Piorońska, Weronika; Górnicka, Agnieszka; Bielawska, Anna; Bielawski, Krzysztof; Mrówczyńska, Lucyna

    2018-04-18

    A series of new di- and polyamine-caffeine analogues were synthesized and characterized by NMR, FT-IR and MS spectroscopic methods. To access stability of the investigated caffeine analogues Molecular Dynamic simulations were performed in NAMD 2.9 assuming CHARMM36 force field. To evaluate the antioxidant capacity of new compounds, three different antioxidant assays were used, namely 1,1-diphenyl-2-picryl-hydrazyl free radical (DPPH • ) scavenging activity, ferrous ions (Fe 2+ ) chelating activity and Fe 3+ →Fe 2+ reducing ability. In vitro, the ability of new derivatives to protect human erythrocytes against oxidative haemolysis induced by free radical from 2,2'-azobis(2-methylpropionamidine) dihydrochloride (AAPH) was estimated. The cytotoxic activity was tested using MCF-7 breast cancer cells and human erythrocytes. All compounds showed the antioxidant capacity depending mostly on their ferrous ions chelating activity. In the presence of AAPH, some derivatives were able to effectively inhibit the oxidative haemolysis. Two derivatives, namely 8-(methyl(2-(methylamino)ethyl)-amino)caffeine and 8-(methyl(3-(methylamino)propyl)amino)caffeine, showed cytotoxic activity against MCF-7 breast cancer cells but not against human erythrocytes. Therefore, it is concluded that the selected di- and polyamine caffeine analogues, depending on their chemical structure, were able to minimize the oxidative stress and to inhibit the tumour cell grow. The confirmed antioxidant and cytotoxic properties of some caffeine derivatives make them attractive for potential applications in food or pharmaceutical industries.

  3. Assessment of Antioxidant and Cytotoxicity Activities of Saponin and Crude Extracts of Chlorophytum borivilianum

    Science.gov (United States)

    Abd Aziz, Maheran; Stanslas, Johnson; Abdul Kadir, Mihdzar

    2013-01-01

    The present paper focused on antioxidant and cytotoxicity assessment of crude and total saponin fraction of Chlorophytum borivilianum as an important medicinal plant. In this study, three different antioxidant activities (2,2-diphenyl-1-picrylhydrazyl radical scavenging (DPPH), ferrous ion chelating (FIC), and β-carotene bleaching (BCB) activity) of crude extract and total saponin fraction of C. borivilianum tubers were performed. Crude extract was found to possess higher free radical scavenging activity (ascorbic acid equivalents 2578 ± 111 mg AA/100 g) and bleaching activity (IC50 = 0.7 mg mL−1), while total saponin fraction displayed higher ferrous ion chelating (EC50 = 1 mg mL−1). Cytotoxicity evaluation of crude extract and total saponin fraction against MCF-7, PC3, and HCT-116 cancer cell lines using 3-(4,5-dimethylthiazol-2-yl)-2,5 diphenyltetrazolium bromide (MTT) cell viability assay indicated a higher cytotoxicity activity of the crude extract than the total saponin fraction on all cell lines, being most effective and selective on MCF-7 human breast cancer cell line. PMID:24223502

  4. Polymeric nanoparticles affect the intracellular delivery, antiretroviral activity and cytotoxicity of the microbicide drug candidate dapivirine.

    Science.gov (United States)

    das Neves, José; Michiels, Johan; Ariën, Kevin K; Vanham, Guido; Amiji, Mansoor; Bahia, Maria Fernanda; Sarmento, Bruno

    2012-06-01

    To assess the intracellular delivery, antiretroviral activity and cytotoxicity of poly(ε-caprolactone) (PCL) nanoparticles containing the antiretroviral drug dapivirine. Dapivirine-loaded nanoparticles with different surface properties were produced using three surface modifiers: poloxamer 338 NF (PEO), sodium lauryl sulfate (SLS) and cetyl trimethylammonium bromide (CTAB). The ability of nanoparticles to promote intracellular drug delivery was assessed in different cell types relevant for vaginal HIV transmission/microbicide development. Also, antiretroviral activity of nanoparticles was determined in different cell models, as well as their cytotoxicity. Dapivirine-loaded nanoparticles were readily taken up by different cells, with particular kinetics depending on the cell type and nanoparticles, resulting in enhanced intracellular drug delivery in phagocytic cells. Different nanoparticles showed similar or improved antiviral activity compared to free drug. There was a correlation between increased antiviral activity and increased intracellular drug delivery, particularly when cell models were submitted to a single initial short-course treatment. PEO-PCL and SLS-PCL nanoparticles consistently showed higher selectivity index values than free drug, contrasting with high cytotoxicity of CTAB-PCL. These results provide evidence on the potential of PCL nanoparticles to affect in vitro toxicity and activity of dapivirine, depending on surface engineering. Thus, this formulation approach may be a promising strategy for the development of next generation microbicides.

  5. Cytotoxic and multidrug resistance reversal activity of a vegetable, 'Anastasia Red', a variety of sweet pepper.

    Science.gov (United States)

    Motohashi, Noboru; Wakabayashi, Hidetsugu; Kurihara, Teruo; Takada, Yuko; Maruyama, Shichiro; Sakagami, Hiroshi; Nakashima, Hideki; Tani, Satoru; Shirataki, Yoshiaki; Kawase, Masami; Wolfard, Kristina; Molnár, Joseph

    2003-04-01

    The vegetable, Anastasia Red, Capsicum annuum L. var. angulosum Mill. (Solanaceae) was successively extracted with hexane, acetone, methanol and 70% methanol, and the extracts were further separated into a total of 21 fractions by silica gel or octadecylsilane (ODS) column chromatography. The biological activities of extracts and fractions were determined. These extracts showed relatively higher cytotoxic activity against two human oral tumor cell lines (HSC-2, HSG) than against normal human gingival fibroblasts (HGF), suggesting a tumor-specific cytotoxic activity. The cytotoxic activity of these extracts was enhanced by fractionation on silica gel [H2, A2, M1-M3] or ODS column chromatography [70M]. Several fractions [H2, H4, H5, A1, A2, A3, A5, A6, A7, M2] reversed the multidrug resistance (MDR) phenotype with L5178 mouse lymphoma T cells, more efficiently than (+/-)-verapamil. The extracts and fractions did not show any detectable anti-human immunodeficiency virus (HIV) or anti-Helicobacter pylori activity. Thus, this study suggests the effective and selective antitumor potential of 'Anastasia Red' of sweet pepper for further phytochemical and biological investigation. Copyright 2003 John Wiley & Sons, Ltd.

  6. Differential Cytotoxic Activity of Essential Oil of Lippia citriodora from Different Regions in Morocco.

    Science.gov (United States)

    Oukerrou, Moulay Ali; Tilaoui, Mounir; Mouse, Hassan Ait; Bouchmaa, Najat; Zyad, Abdelmajid

    2017-07-01

    The aim of this work was to investigate the cytotoxic effect of the essential oil of dried leaves of Lippia citriodora (H.B. & K.) harvested in different regions of Morocco. This effect was evaluated against the P815 murine mastocytoma cell line using the MTT assay. Interestingly, this work demonstrated for the first time that these essential oils exhibited a strong cytotoxic activity against the P815 cell line, with IC 50 values ranging from 7.75 to 13.25 μg/ml. This cytotoxicity began early and increased in a dose- and time-dependent manner. The chemical profile of these essential oils was analyzed by gas chromatography coupled to mass spectrometry. Importantly, the difference in terms of major components' contents was not significant suggesting probably that the differential cytotoxicity between these essential oils could be attributed to the difference in the content of these essential oils in minor compounds, which could interact with each other or with the main molecules. Finally, this study demonstrated for the first time that essential oils of L. citriodora from different regions in Morocco induced apoptosis against P815 tumor cell line. © 2017 Wiley-VHCA AG, Zurich, Switzerland.

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

    Science.gov (United States)

    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. PMID:25574182

  8. ELISPOT Assay for Monitoring Cytotoxic T Lymphocytes (CTL Activity in Cancer Vaccine Clinical Trials

    Directory of Open Access Journals (Sweden)

    Thomas J. Sayers

    2012-05-01

    Full Text Available The profiling and monitoring of immune responses are key elements in the evaluation of the efficacy and development of new biotherapies, and a number of assays have been introduced for analyzing various immune parameters before, during, and after immunotherapy. The choice of immune assays for a given clinical trial depends on the known or suggested immunomodulating mechanisms associated with the tested therapeutic modality. Cell-mediated cytotoxicity represents a key mechanism in the immune response to various pathogens and tumors. Therefore, the selection of monitoring methods for the appropriate assessment of cell-mediated cytotoxicity is thought to be crucial. Assays that can detect both cytotoxic T lymphocytes (CTL frequency and function, such as the IFN-γ enzyme-linked immunospot assay (ELISPOT have gained increasing popularity for monitoring clinical trials and in basic research. Results from various clinical trials, including peptide and whole tumor cell vaccination and cytokine treatment, have shown the suitability of the IFN-γ ELISPOT assay for monitoring T cell responses. However, the Granzyme B ELISPOT assay and Perforin ELISPOT assay may represent a more direct analysis of cell-mediated cytotoxicity as compared to the IFN-γ ELISPOT, since Granzyme B and perforin are the key mediators of target cell death via the granule-mediated pathway. In this review we analyze our own data and the data reported by others with regard to the application of various modifications of ELISPOT assays for monitoring CTL activity in clinical vaccine trials.

  9. 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

    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...

  10. In-vitro cytotoxic activities of poly(2-ethyl-2-oxazoline-based amphiphilic block copolymers prepared by CuAAC click chemistry

    Directory of Open Access Journals (Sweden)

    S. Gulyuz

    2018-02-01

    Full Text Available Synthesis and characterization of well-defined amphiphilic block copolymers containing poly(2-ethyl-2-oxazoline as hydrophilic block and poly(ε-caprolactone or poly(L-lactide as hydrophobic block is achieved by copper-catalyzed azide-alkyne cycloaddition (CuAAC click chemistry. The clickable precursors, α-alkyne-functionalized poly(ε-caprolactone and poly(L-lactide and ω-azido-functionalized poly(2-ethyl-2-oxazoline are simply prepared and joined using copper sulfate/ascorbic acid catalyst system at room temperature. The structures of precursors and amphiphilic block copolymers are characterized by spectroscopic, chromatographic and thermal analyses. The cytotoxic activities of resulting amphiphilic block copolymers and their precursors are investigated in the prostate epithelial and cancer cells under in-vitro conditions. The treatment of the healthy prostate epithelial cell line PNT1A reveals that no significant cytotoxicity, whereas some significant toxic effects on the prostate cancer cell lines are observed.

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

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    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.

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

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    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

  13. 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

  14. Evaluation of morning glory (Jacquemontia tamnifolia (L.) Griseb) leaves for antioxidant, antinociceptive, anticoagulant and cytotoxic activities.

    Science.gov (United States)

    Hossain, Mohammad Shahadat; Reza, A S M Ali; Rahaman, Md Masudur; Nasrin, Mst Samima; Rahat, Mohammed Rasib Uddin; Islam, Md Rabiul; Uddin, Md Josim; Rahman, Md Atiar

    2018-01-05

    The present study was planned to investigate the phytochemical, antioxidant, antinociceptive, anticoagulant and cytotoxic activities of the Jacquemontia tamnifolia (L.) Griseb leaf methanol extract (MExJT) in the laboratory using both in vitro and in vivo methods. Phytochemical values, namely, total phenolic and flavonoid contents, 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging effect and FeCl3 reducing power effects, were studied by established methods. In vivo antinociceptive activity was performed by acidic acid-induced writhing test and formalin-induced pain test on Swiss albino mice at doses of 125, 250 and 500 mg/kg body weight. The clot lysis and brine shrimp lethality bioassay in vitro were used to evaluate the thrombolytic and cytotoxic activities of the plant extract, respectively. Phytochemical screening illustrates the presence of tannins, saponins, flavonoids, gums and carbohydrates, steroids, alkaloids and reducing sugars in the extract. The results showed the total phenolic content (146.33 g gallic acid equivalents/100 g extract) and total flavonoid content (133.33 g quercetin/100 g). Significant (pacetic acid-induced writhing test and formalin-induced pain models in Swiss albino mice with doses of 125, 250 and 500 mg/kg body weight. Significant (panalgesic activity. The results also demonstrate that MExJT has moderate thrombolytic and lower cytotoxic properties that may warrant further exploration.

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

    Directory of Open Access Journals (Sweden)

    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.

  16. Synthesis of Key Fragments of Amphidinolide Q — A Cytotoxic 12-membered Macrolide

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    Kohei Kawa

    2011-06-01

    Full Text Available b-Hydroxy aldehyde and alkyl ketone moieties were effectively synthesized as key intermediates of amphidinolide Q, a cytotoxic macrolide from the cultured dinoflagellate Amphidinium sp.. The asymmetric center of the former derivative was produced by Sharpless asymmetric epoxidation, followed by E-selective 1,4-addition to give the sp2 methyl group. Derivatization of the L-ascorbic acid derivative by Evans asymmetric alkylation and Peterson olefination provided the latter intermediate. The coupling reaction of the segments was examined.

  17. Synthesis and cytotoxicity of boronated fatty esters for BNCT of cervix cancer

    International Nuclear Information System (INIS)

    Tambunchong, C.; Prachayasittikul, S.; Picha, P.; Tumpum, C.

    2000-01-01

    Esterification reactions of o-carboranic acid with six fatty alcohols, palmitoleyl, stearyl, oleyl, elaidyl, linoleyl and linoelaidyl alcohols, proceeded smoothly under nitrogen atmosphere with dimethylamino pyrimidine as a catalyst. The reaction gave the corresponding esters in moderate yields. Most of the synthetic esters are stable at room temperature except the linoleyl carboranate and linoelaidyl carboranate which decomposed within two weeks. The in vitro studies on Hela cells showed relatively low cytotoxic. The IC 50 of boronated esters were in range of 36-83 micrograms/cm 3 . (author)

  18. "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.

  19. Cytotoxicity and antiviral activity of electrochemical - synthesized silver nanoparticles against poliovirus.

    Science.gov (United States)

    Huy, Tran Quang; Hien Thanh, Nguyen Thi; Thuy, Nguyen Thanh; Chung, Pham Van; Hung, Pham Ngoc; Le, Anh-Tuan; Hong Hanh, Nguyen Thi

    2017-03-01

    Silver nanoparticles (AgNPs) have been proven to have noticeable cytotoxicity in vitro and antiviral activity against some types of enveloped viruses. This paper presents the cytotoxicity and antiviral activity of pure AgNPs synthesized by the electrochemical method, towards cell culture and poliovirus (a non-enveloped virus). Prepared AgNPs were characterized by ultraviolet-visible spectroscopy, energy-dispersive X-ray spectroscopy and transmission electron microscopy. Before incubation with poliovirus, different concentrations of AgNPs were added to human rhabdomyosarcoma (RD) cell monolayers seeded in 96 well plates for testing their cytotoxicity. The in vitro cytotoxicity and anti-poliovirus activity of AgNPs were daily assessed for cytopathic effect (CPE) through inverted light microscopy. CPE in the tested wells was determined in comparison with those in wells of negative and positive control. Structure analysis showed that AgNPs were formed with a quasi-spherical shape with mean size about 7.1nm and high purity. No CPE of RD cells was seen in wells at the time point of 48h post-incubation with AgNPs at concentration up to 100ppm. The anti-poliovirus activity of AgNPs was determined at 3.13ppm corresponding to the viral concentration of 1TCID 50 (Tissue Culture Infective Dose) after 30min, and 10TCID 50 after 60min, the cell viability was found up to 98% at 48h post-infection, with no CPE found. Whereas, a strong CPE of RD cells was found at 48h post-infection with the mixture of AgNPs and poliovirus at concentration of 100TCID 50 , and in wells of positive controls. With mentioned advantages, electrochemical-synthesized AgNPs are promising candidate for advanced biomedical and disinfection applications. Copyright © 2016 Elsevier B.V. All rights reserved.

  20. 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.

  1. 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.

  2. Synthesis of Chalcones with Anticancer Activities

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    Syam Mohan

    2012-05-01

    Full Text Available Several chalcones were synthesized and their in vitro cytotoxicity against various human cell lines, including human breast adenocarcinoma cell line MCF-7, human lung adenocarcinoma cell line A549, human prostate cancer cell line PC3, human adenocarcinoma cell line HT-29 (colorectal cancer and human normal liver cell line WRL-68 was evaluated. Most of the compounds being active cytotoxic agents, four of them with minimal IC50 values were chosen and studied in detail with MCF-7 cells. The compounds 1, 5, 23, and 25 were capable in eliciting apoptosis in MCF-7 cells as shown by multiparameter cytotoxicity assay and caspase-3/7, -8, and -9 activities (p < 0.05. The ROS level showed 1.3-fold increase (p < 0.05 at the low concentrations used and thus it was concluded that the compounds increased the ROS level eventually leading to apoptosis in MCF-7 cells through intrinsic as well as extrinsic pathways.

  3. 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.

  4. Structure-activity relationship analysis of cytotoxic cyanoguanidines: selection of CHS 828 as candidate drug

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    Gullbo Joachim

    2009-06-01

    Full Text Available Abstract Background N-(6-(4-chlorophenoxyhexyl-N'-cyano-N''-4-pyridyl guanidine (CHS 828 is the first candidate drug from a novel group of anti-tumour agents – the pyridyl cyanoguanidines, shown to be potent compounds interfering with cellular metabolism (inhibition of nicotinamide phosphoribosyl transferase and NF-κB signalling. Substituted cyanoguanidines are also found in anti-hypertensive agents such as the potassium channel opener pinacidil (N-cyano-N'-(4-pyridyl-N''-(1,2,2-trimethylpropylguanidine and histamine-II receptor antagonists (e.g. cimetidine, N-cyano-N'-methyl-N''-[2-[[(5-methylimidazol-4-yl]methyl]thio]ethylguanidine. In animal studies, CHS 828 has shown very promising activity, and phase I and II studies resulted in further development of a with a water soluble prodrug. Findings To study the structural requirements for cyanoguanidine cytotoxicity a set of 19 analogues were synthesized. The cytotoxic effects were then studied in ten cell lines selected for different origins and mechanisms of resistance, using the fluorometric microculture cytotoxicity assay (FMCA. The compounds showed varying cytotoxic activity even though the dose-response curves for some analogues were very shallow. Pinacidil and cimetidine were found to be non-toxic in all ten cell lines. Starting with cyanoguanidine as the crucial core it was shown that 4-pyridyl substitution was more efficient than was 3-pyridyl substitution. The 4-pyridyl cyanoguanidine moiety should be linked by an alkyl chain, optimally a hexyl, heptyl or octyl chain, to a bulky end group. The exact composition of this end group did not seem to be of crucial importance; when the end group was a mono-substituted phenyl ring it was shown that the preferred position was 4-substitution, followed by 3- and, finally, 2-substitution as the least active. Whether the substituent was a chloro, nitro or methoxy substituent seemed to be of minor importance. Finally, the activity patterns in the

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

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    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.

  6. 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.

  7. Suppression of cytotoxic T lymphocytes by carrageenan-activated macrophage-like cells

    International Nuclear Information System (INIS)

    Yung, Y.P.; Cudkowicz, G.

    1978-01-01

    In the presence of 100 μg/ml of carrageenans (CAR), B6D2F 1 responder spleen cells failed to generate antiparent or anti-allogeneic cytotoxic T lymphocytes in vitro, but instead generated suppressor cells. Cultured CAR-treated cells added to mixtures of B6D2F 1 anti-B6 or B6D2F 1 anti-C3H cytotoxic effectors (induced in vitro) and the appropriate 51 Cr-labeled lymphoma targets reduced or abolished cytolysis (measured as 51 Cr release) depending on the ratio of suppressor to effector cells. Cultured spleen cells not exposed to CAR failed to inhibit both types of cytotoxicity. Presuppressor cells were associated with a splenic subpopulation independent of the thymus (i.e., present in spleens of athymic nude mice), were moderately adherent to Sephadex G-10 columns, but were not phagocytic or ''sticky'' to carbonyl iron particles. Activation of such cells by CAR was not prevented by in vitro exposure to 2000 rads of γ-rays before culture, nor facilitated by antigenic stimulation. The matured suppressor cells remained radioresistant and became strongly adherent to Sephadex G-10. The suppressors lacked surface Thy-1 alloantigen detectable by antibody and rabbit complement. Suppressor cell activity was not restricted by the immunologic specificity and major histocompatibility type of effectors

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

    International Nuclear Information System (INIS)

    Yu, Jing; Zhang, Shanshan; Dai, Yitong; Lu, Xiaoxing; Lei, Qunfang; Fang, Wenjun

    2016-01-01

    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_4]"− 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 "1H 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.

  9. Biocompatibility index of antiseptic agents by parallel assessment of antimicrobial activity and cellular cytotoxicity.

    Science.gov (United States)

    Müller, Gerald; Kramer, Axel

    2008-06-01

    To assess the suitability of an antiseptic agent, both the microbicidal activity and the cytotoxic effect must be taken into consideration to derive biocompatible antibacterial agents. We defined the biocompatibility index (BI) by measuring the antibacterial activity against the test organisms Escherichia coli and Staphylococcus aureus and, in parallel, the cytotoxicity on cultured murine fibroblasts. The antiseptic agents tested were benzalkonium chloride (BAC), cetylpyridinium chloride (CPC), chlorhexidine digluconate (CHX), mild silver protein (MSP), octenidine dihydrochloride (OCT), polyhexamethylene biguanide (PHMB), povidone iodine in solution [PVP-I(s)], povidone iodine in ointment [PVP-I(o)], silver nitrate (AgNO(3)), silver (I) sulfadiazine (SSD) and triclosan (TRI). Assays were carried out for 30 min of exposure at 37 degrees C in the presence of cell culture medium containing 10% fetal bovine serum. The resulting dimensionless BI was defined as the ratio of the concentration at which 50% of the murine fibroblasts are damaged and the microbicidal effect producing at least 3 log(10) (99.9%) reduction. The resulting rank ordering of BI for the ratio of fibroblast cytotoxicity to E. coli toxicity was OCT > PHMB > CHX > PVP-I(o) > PVP-I(s) > BAC > CPC > TRI > MSP and that to S. aureus was OCT > PHMB > CHX > CPC > PVP-I(o) > BAC > PVP(s) > TRI > MSP. OCT and PHMB were the most suitable agents with a BI greater than 1. The BI presented may be a useful tool to evaluate antiseptic agents for use in clinical practice.

  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. Essential Oil Composition, Antioxidant, Cytotoxic and Antiviral Activities of Teucrium pseudochamaepitys Growing Spontaneously in Tunisia

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    Saoussen Hammami

    2015-11-01

    Full Text Available The chemical composition, antioxidant, cytotoxic and antiviral activities of the essential oil obtained by hydrodistillation from the aerial parts of Teucrium pseudochamaepitys (Lamiaceae collected from Zaghouan province of Tunisia are reported. The essential oil was analyzed by gas chromatography equipped with a flame ionization detector (GC-FID and gas chromatography coupled with mass spectrometry (GC/MS. Thirty-one compounds were identified representing 88.6% of the total essential oil. Hexadecanoic acid was found to be the most abundant component (26.1% followed by caryophyllene oxide (6.3%, myristicin (4.9% and α-cubebene (3.9%. The antioxidant capacity of the oil was measured on the basis of the scavenging activity to the stable 2,2-diphenyl-1-picrylhydrazyl (DPPH. The IC50 value of the oil was evaluated as 0.77 mg·mL−1. In addition, the essential oil was found to possess moderate cytotoxic effects on the HEp-2 cell line (50% cytotoxic concentration (CC50 = 653.6 µg·mL−1. The potential antiviral effect was tested against Coxsackievirus B (CV-B, a significant human and mouse pathogen that causes pediatric central nervous system disease, commonly with acute syndromes. The reduction of viral infectivity by the essential oil was measured using a cytopathic (CPE reduction assay.

  12. Cytotoxic activity of kenaf (Hibiscus cannabinus L.) seed extract and oil against human cancer cell lines

    Science.gov (United States)

    Wong, Yu Hua; Tan, Wai Yan; Tan, Chin Ping; Long, Kamariah; Nyam, Kar Lin

    2014-01-01

    Objective To examine the cytotoxic properties of both the kenaf (Hibiscus cannabinus L.) seed extract and kenaf seed oil on human cervical cancer, human breast cancer, human colon cancer and human lung cancer cell lines. Methods The in vitro cytotoxic activity of the kenaf (Hibiscus cannabinus L.) seed extract and kenaf seed oil on human cancer cell lines was evaluated by using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide and sulforhodamine B assays. Cell morphological changes were observed by using an inverted light microscope. Results The kenaf seed extract (KSE) exhibited a lower IC50 than kenaf seed oil (KSO) in all of the cancer cell lines. Morphological alterations in the cell lines after KSE and KSO treatment were observed. KSE and KSO possessed effective cytotoxic activities against all the cell lines been selected. Conclusions KSE and KSO could be potential sources of natural anti-cancer agents. Further investigations on using kenaf seeds for anti-proliferative properties are warranted. PMID:25183141

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

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    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.

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

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    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.

  15. Secondary Metabolites from the Marine-Derived Fungus Dichotomomyces sp. L-8 and Their Cytotoxic Activity

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    Li-Hong Huang

    2017-03-01

    Full Text Available Bioassay-guided isolation of the secondary metabolites from the fungus Dichotomomyces sp. L-8 associated with the soft coral Lobophytum crassum led to the discovery of two new compounds, dichotones A and B (1 and 2, together with four known compounds including dichotocejpin C (3, bis-N-norgliovictin (4, bassiatin (5 and (3R,6R-bassiatin (6. The structures of these compounds were determined by 1D, 2D NMR and mass spectrometry. (3R,6R-bassiatin (6 displayed significant cytotoxic activities against the human breast cancer cell line MDA-MB-435 and the human lung cancer cell line Calu3 with IC50 values of 7.34 ± 0.20 and 14.54 ± 0.01 μM, respectively, while bassiatin (5, the diastereomer of compound 6, was not cytotoxic.

  16. 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.

  17. Synthesis, fluorescence properties and the promising cytotoxicity of pyrene-derived aminophosphonates.

    Science.gov (United States)

    Lewkowski, Jarosław; Rodriguez Moya, Maria; Wrona-Piotrowicz, Anna; Zakrzewski, Janusz; Kontek, Renata; Gajek, Gabriela

    2016-01-01

    A large series of variously substituted amino(pyren-1-yl)methylphosphonic acid derivatives was synthesized using a modified aza-Pudovik reaction in 20-97% yields. The fluorescence properties of the obtained compounds were investigated revealing that N-alkylamino(pyren-1-yl)methylphosphonic derivatives are stronger emissive compounds than the corresponding N-aryl derivatives. N-Benzylamino(pyren-1-yl)methylphosphonic acid displayed strong fluorescence (ΦF = 0.68) in phosphate-buffered saline (PBS). The influence of a series of derivatives on two colon cancer cell lines HT29 and HCT116 was also investigated. The most promising results were obtained for N-(4-methoxyphenyl)amino(pyren-1-yl)methylphosphonate, which was found to be cytotoxic for the HCT116 cancer cell line (IC50 = 20.8 μM), simultaneously showing weak toxicity towards normal lymphocytes (IC50 = 230.8 µM).

  18. Synthesis, fluorescence properties and the promising cytotoxicity of pyrene–derived aminophosphonates

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    Jarosław Lewkowski

    2016-06-01

    Full Text Available A large series of variously substituted amino(pyren-1-ylmethylphosphonic acid derivatives was synthesized using a modified aza-Pudovik reaction in 20–97% yields. The fluorescence properties of the obtained compounds were investigated revealing that N-alkylamino(pyren-1-ylmethylphosphonic derivatives are stronger emissive compounds than the corresponding N-aryl derivatives. N-Benzylamino(pyren-1-ylmethylphosphonic acid displayed strong fluorescence (ΦF = 0.68 in phosphate-buffered saline (PBS. The influence of a series of derivatives on two colon cancer cell lines HT29 and HCT116 was also investigated. The most promising results were obtained for N-(4-methoxyphenylamino(pyren-1-ylmethylphosphonate, which was found to be cytotoxic for the HCT116 cancer cell line (IC50 = 20.8 μM, simultaneously showing weak toxicity towards normal lymphocytes (IC50 = 230.8 µM.

  19. Synthesis, fluorescence properties and the promising cytotoxicity of pyrene–derived aminophosphonates

    Science.gov (United States)

    Rodriguez Moya, Maria; Wrona-Piotrowicz, Anna; Gajek, Gabriela

    2016-01-01

    Summary A large series of variously substituted amino(pyren-1-yl)methylphosphonic acid derivatives was synthesized using a modified aza-Pudovik reaction in 20–97% yields. The fluorescence properties of the obtained compounds were investigated revealing that N-alkylamino(pyren-1-yl)methylphosphonic derivatives are stronger emissive compounds than the corresponding N-aryl derivatives. N-Benzylamino(pyren-1-yl)methylphosphonic acid displayed strong fluorescence (ΦF = 0.68) in phosphate-buffered saline (PBS). The influence of a series of derivatives on two colon cancer cell lines HT29 and HCT116 was also investigated. The most promising results were obtained for N-(4-methoxyphenyl)amino(pyren-1-yl)methylphosphonate, which was found to be cytotoxic for the HCT116 cancer cell line (IC50 = 20.8 μM), simultaneously showing weak toxicity towards normal lymphocytes (IC50 = 230.8 µM). PMID:27559373

  20. 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.

  1. Synthesis, characterization and antimicrobial activity of mixed ...

    African Journals Online (AJOL)

    Synthesis, characterization and antimicrobial activity of mixed ascorbic acid - nicotinamide metal complexes. ... The result of the antimicrobial studies showed that the mixed complexes have higher inhibitory activity than the original ligands against the tested bacteria and fungi species. KEY WORDS: Ascorbic acid, ...

  2. Leishmanicidal and cytotoxic activity from plants used in Tacana traditional medicine (Bolivia).

    Science.gov (United States)

    Arévalo-Lopéz, Diandra; Nina, Nélida; Ticona, Juan C; Limachi, Ivan; Salamanca, Efrain; Udaeta, Enrique; Paredes, Crispin; Espinoza, Boris; Serato, Alcides; Garnica, David; Limachi, Abigail; Coaquira, Dayana; Salazar, Sarah; Flores, Ninoska; Sterner, Olov; Giménez, Alberto

    2018-04-24

    Thirty-eight Tacana medicinal plant species used to treat skin problems, including leishmania ulcers, skin infections, inflammation and wound healing, were collected in the community of Buena Vista, Bolivia, with the Tacana people. Twenty two species are documented for the first time as medicinal plants for this ethnic group living in the northern area of the Department of La Paz. To evaluate the leishmanicidal effect (IC 50 ) and cytotoxicity (LD 50 ) of the selected plants. To carry out bioguided studies on the active extracts. To assess the potential of Bolivian plant biodiversity associated with traditional knowledge in the discovery of alternative sources to fight leishmaniasis. Seventy three ethanol extracts were prepared from 38 species by maceration and were evaluated in vitro against promastigotes of Leishmania amazonensis and L. braziliensis. Active extracts (IC 50 ≤ 50 μg/mL) were fractionated by chromatography on Silica gel column and the fractions were assessed against the two Leishmania strains. The most active fractions and the crude extracts were evaluated against reference strains of L. amazonensis, L. braziliensis, L. aethiopica, two native strains (L. Lainsoni and L. braziliensis) and for cytotoxicity against HeLa cells. The chromatographic profile of the active fractions was obtained by reverse phase chromatography using HPLC. From the 73 extracts, 39 extracts (53.4%) were inactive and 34 showed activity. Thirteen species were sselected for bioguided studies. The crude extracts and their 36 fractions were evaluated against two Leishmania strains. The most active fraction were tested in a panel of five leishmania strains and for cytotoxicity. The Selective Index (SI = LD 50 /IC 50 ) was calculated, and were generally low. Retention time and UV spectra were recorded for the active fractions by HPLC-DAD using a reverse phase column. Profiles were very different from each other, showing the presence of different compounds. Bolivian traditional

  3. 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)

  4. Chemical Composition, Antioxidant, Antimicrobial and Cytotoxic Activities of Essential Oil from Premna microphylla Turczaninow.

    Science.gov (United States)

    Zhang, Han-Yu; Gao, Yang; Lai, Peng-Xiang

    2017-02-28

    Premna microphylla Turczaninow, an erect shrub, was widely used in Chinese traditional medicine to treat dysentery, appendicitis, and infections. In this study, the essential oil from P. microphylla Turcz. was obtained by hydrodistillation and analyzed by GC (Gas Chromatography) and GC-MS (Gas Chromatography-Mass Spectrometer). Fifty-six compounds were identified in the oil which comprised about 97.2% of the total composition of the oil. Major components of the oil were blumenol C (49.7%), β-cedrene (6.1%), limonene (3.8%), α-guaiene (3.3%), cryptone (3.1%), and α-cyperone (2.7%). Furthermore, we assessed the in vitro biological activities displayed by the oil obtained from the aerial parts of P. microphylla, namely the antioxidant, antimicrobial, and cytotoxic activities. The antioxidant activity of the essential oil was evaluated by 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging activity. For this, the IC50 value was estimated to be 0.451 mg/mL. The essential oil of P. microphylla exhibited considerable antibacterial capacity against Escherichia coli with an MIC (Minimum Inhibitory Concentration) value of 0.15 mg/mL, along with noticeable antibacterial ability against Bacillus subtilis and Staphylococcus aureus with an MIC value of 0.27 mg/mL. However, the essential oil did not show significant activity against fungus. The oil was tested for its cytotoxic activity towards HepG2 (liver hepatocellular cells) and MCF-7 Cells (human breast adenocarcinoma cell line) using the MTT (3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2-H-tetrazolium bromide) assay, and exerted cytotoxic activity with an IC50 of 0.072 and 0.188 mg/mL for 72 h. In conclusion, the essential oil from P. microphylla is an inexpensive but favorable resource with strong antibacterial capacity as well as cytotoxic activity. Thus, it has the potential for utilization in the cosmetics and pharmaceutical industries.

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

    Directory of Open Access Journals (Sweden)

    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.

  6. Chaetoglobosins from Chaetomium globosum, an endophytic fungus in Ginkgo biloba, and their phytotoxic and cytotoxic activities.

    Science.gov (United States)

    Li, He; Xiao, Jian; Gao, Yu-Qi; Tang, Jiang Jiang; Zhang, An-Ling; Gao, Jin-Ming

    2014-04-30

    In preceding studies, cultivation of Chaetomium globosum, an endophytic fungus in Ginkgo biloba, produced five cytochalasan mycotoxins, chaetoglobosins A, G, V, Vb, and C (1-5), in three media. In the present work, five known chaetoglobosins, C, E, F, Fex, and 20-dihydrochaetoglobosin A (5-9), together with the four known compounds (11-14), were isolated from the MeOH extracts of the solid culture of the same endophyte. The structures of these metabolites were elucidated on the basis of spectroscopic analysis. Treatment of chaetoglobosin F (7) with (diethylamino)sulfur trifluoride (DAST) in dichloromethane afforded an unexpected fluorinated chaetoglobosin, named chaetoglobosin Fa (10), containing an oxolane ring between C-20 and C-23. The phytotoxic effects of compounds 1, 3-8, and 10 were assayed on radish seedlings; some of these compounds (1, 3, and 6-8) significantly inhibited the growth of radish (Raphanus sativus) seedlings with inhibitory rates of >60% at a concentration of 50 ppm, which was comparable or superior to the positive control, glyphosate. In addition, the cytotoxic activities against HCT116 human colon cancer cells were also tested, and compounds 1 and 8-10 showed remarkable cytotoxicity with IC50 values ranging from 3.15 to 8.44 μM, in comparison to the positive drug etoposide (IC50 = 2.13 μM). The epoxide ring between C-6 and C-7 or the double bond at C-6(12) led to a drastically increased cytotoxicity, and chaetoglobosin Fa (10) displayed a markedly increased cytotoxicity but decreased phytotoxicity.

  7. 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

  8. Cytotoxic activity of Thai medicinal plants against human cholangiocarcinoma, laryngeal and hepatocarcinoma cells in vitro

    Directory of Open Access Journals (Sweden)

    Itharat Arunporn

    2010-09-01

    Full Text Available Abstract Background Cholangiocarcinoma is a serious public health in Thailand with increasing incidence and mortality rates. The present study aimed to investigate cytotoxic activities of crude ethanol extracts of a total of 28 plants and 5 recipes used in Thai folklore medicine against human cholangiocarcinoma (CL-6, human laryngeal (Hep-2, and human hepatocarcinoma (HepG2 cell lines in vitro. Methods Cytotoxic activity of the plant extracts against the cancerous cell lines compared with normal cell line (renal epithelial cell: HRE were assessed using MTT assay. 5-fluorouracil was used as a positive control. The IC50 (concentration that inhibits cell growth by 50% and the selectivity index (SI were calculated. Results The extracts from seven plant species (Atractylodes lancea, Kaempferia galangal, Zingiber officinal, Piper chaba, Mesua ferrea, Ligusticum sinense, Mimusops elengi and one folklore recipe (Pra-Sa-Prao-Yhai exhibited promising activity against the cholangiocarcinoma CL-6 cell line with survival of less than 50% at the concentration of 50 μg/ml. Among these, the extracts from the five plants and one recipe (Atractylodes lancea, Kaempferia galangal, Zingiber officinal, Piper chaba, Mesua ferrea, and Pra-Sa-Prao-Yhai recipe showed potent cytotoxic activity with mean IC50 values of 24.09, 37.36, 34.26, 40.74, 48.23 and 44.12 μg/ml, respectively. All possessed high activity against Hep-2 cell with mean IC50 ranging from 18.93 to 32.40 μg/ml. In contrast, activity against the hepatoma cell HepG2 varied markedly; mean IC50 ranged from 9.67 to 115.47 μg/ml. The only promising extract was from Zingiber officinal (IC50 = 9.67 μg/ml. The sensitivity of all the four cells to 5-FU also varied according to cell types, particularly with CL-6 cell (IC50 = 757 micromolar. The extract from Atractylodes lancea appears to be both the most potent and most selective against cholangiocarcinoma (IC50 = 24.09 μg/ml, SI = 8.6. Conclusions The

  9. Synthesis of novel pyrazolo[3,4-d]pyrimidinone derivatives as cytotoxic inhibitors

    Directory of Open Access Journals (Sweden)

    Ameur Rahmouni

    2014-02-01

    Full Text Available Various α-fonctionalized iminoethers 2 were easily prepared from ethyl 5-amino-3-substituted-1-phenyl-1H-pyrazole-4-carboxylate 1. The reaction of iminoethers 2 with ammonia afforded 3-substitued-1-phenyl-1H-pyrazolo[3,4-d] pyrimidin-4(5H-ones 3 which were also synthesized by the addition of formamide to ethyl 5-amino-3-substituted-1-phenyl-1H-pyrazole-4-carboxylate 1. The 5-amino-3-substitued-1-phenyl-1H-pyrazolo[3,4-d]pyrimidin-4(5H-ones 4 were obtained from hydrazonolysis of iminoethers 2. Otherwise, the condensation of these intermediates 2 with a series of some primary amines and hydroxylamine led respectively, to the corresponding 3,5-disubstitued-1-phenyl-1H-pyrazolo[3,4-d]pyrimidin-4(5H-ones 5 and the 3-substitued-5-hydroxy-1-phenyl-1H-pyrazolo[3,4-d] pyrimidin-4-(5H-ones 6. The synthesized compounds 1-6 were completely characterized by 1H NMR, 13C NMR, IR and HRMS. Some synthesized compounds were evaluated for their cytotoxic effect using the Human cervical adenocarcinoma Hela cell line.

  10. Cobalt nanoparticles for biomedical applications: Facile synthesis, physiochemical characterization, cytotoxicity behavior and biocompatibility

    Science.gov (United States)

    Ansari, S. M.; Bhor, R. D.; Pai, K. R.; Sen, D.; Mazumder, S.; Ghosh, Kartik; Kolekar, Y. D.; Ramana, C. V.

    2017-08-01

    Cobalt (Co) nanoparticles (NPs) were produced by a simple, one step hydrothermal method with the capping of oleic acid. Intrinsic structural, physiochemical and magnetic properties of Co NPs were investigated and demonstrated their applicability in biomedicine. X-ray diffraction, Raman spectroscopy and infrared (IR) spectroscopic studies confirm the single phase Co NPs with a high structural quality. The IR data revealed the capping of oleic acid via monodentate interaction. Small angle scattering studies suggest the existence of sticky hard sphere type of interaction among the Co NPs because of magnetic interaction which is further evidenced by electron microscopy imaging analyses. The Co NPs exhibit a ferromagnetic character over a wide range of temperature (20-300 K). The temperature dependence of magnetic parameters namely, saturation magnetization, remanent magnetization, coercivity and reduced remanent magnetization were determined and correlated with structure of Co NPs. The Cytotoxicity studies demonstrate that these Co NPs exhibit the mild anti-proliferative character against the cancer cells (cisplatin resistant ovarian cancer (A2780/CP70)) and safe nature towards the normal cells. Haemolytic behavior of human red blood cells (RBC) revealed (<5%) haemolysis signifying the compatibility of Co NPs with human RBC which is an essential feature in vivo biomedical applications without creating any harmful effects in the human blood stream.

  11. Positively charged gold nanoparticles capped with folate quaternary chitosan: Synthesis, cytotoxicity, and uptake by cancer cells.

    Science.gov (United States)

    Yen, Hui-Ju; Young, Yen-An; Tsai, Tsung-Neng; Cheng, Kuang-Ming; Chen, Xin-An; Chen, Ying-Chuan; Chen, Cheng-Cheung; Young, Jenn-Jong; Hong, Po-da

    2018-03-01

    In this study, we synthesized various quaternary chitosan derivatives and used them to stabilize gold nanoparticles (AuNPs). These chitosan derivatives comprised N-(2-hydroxy)propyl-3-trimethylammonium chitosan chloride (HTCC), folate-HTCC, galactosyl-HTCC, and their fluorescein isothiocyanate-conjugated derivatives. Various positively surface-charged AuNPs were prepared under alkaline conditions using glucose as a reducing agent in the presence of the HTCC derivatives (HTCCs). The effects of the concentration of NaOH, glucose, and HTCCs on the particles size, zeta potential, and stability were studied in detail. Cell cycle assays verify that none of the HTCCs or HTCCs-AuNPs was cytotoxic to human umbilical vein endothelial cells. Flow cytometry analysis showed that the folate HTCC-AuNPs were internalized in Caco-2, HepG2, and HeLa cancer cells to a significantly greater extent than AuNPs without folate. But, galactosyl HTCC-AuNPs only showed high cell uptake by HepG2 cells. Copyright © 2017 Elsevier Ltd. All rights reserved.

  12. Cytotoxic effects of new synthesis heterocyclic derivatives of Amoxicillin on some cancer cell lines

    Science.gov (United States)

    Al-Rawi, M. S.; Hussei, D. F.; Al-Taie, A. F.; Al-Halbosiy, M. M.; Hameed, B. A.

    2018-05-01

    A new Schiff base [I] was prepared by refluxing Amoxicillin trihydrate and 4-Hydroxy- 3,5-dimethoxybenzaldehyde in aqueous methanol solution using glacial acetic acid as a catalyst. The new 1,3-oxazepine derivative [II] was obtained by Diels- Alder reaction of Schiff base [I] with phthalic anhydride in dry benzene. The reaction of Schiff base [I] with thioglycolic acid in dry benzene led to the formation of thiazolidin-4-one derivative [III]. While the imidazolidin-4-one [IV] derivative was produced by reacting the mentioned Schiff base [I] with glycine and triethylamine in ethanol for 9 hrs. Tetrazole derivative [V] was synthesized by refluxing Schiff base [I] with sodium azide in dimethylformamid DMF. The structure of synthesized compounds[I-V] was characterized by their melting points, elemental analysis CHN-S and by their spectral data; FTIR and 1H NMR spectroscopy. Two cancer cell lines include: (RD) human pelvic rhabdomyosarcoma and (L20B) the mice intestines carcinoma cell line (which expresses the genes for human cellular receptor for Polio viruses) were used in this study. The cytotoxic effect of different concentrations of all the synthesized compounds for 48 hrs was examined. All compounds except [IV] and [V] showed less than 50% inhibition for (L20B), while these compounds exhibit inhibition more than 50% inhibition for (RD).

  13. Cobalt nanoparticles for biomedical applications: Facile synthesis, physiochemical characterization, cytotoxicity behavior and biocompatibility

    Energy Technology Data Exchange (ETDEWEB)

    Ansari, S.M. [Department of Physics, Savitribai Phule Pune University, Pune, 411007, Maharashtra (India); Bhor, R.D.; Pai, K.R. [Department of Zoology, Savitribai Phule Pune University, Pune, 411007, Maharashtra (India); Sen, D.; Mazumder, S. [Solid State Physics Division, Bhabha Atomic Research Centre, Mumbai, 400 085 (India); Ghosh, Kartik [Department of Physics, Astronomy and Materials Science, Missouri State University, Springfield, MO, 65897 (United States); Kolekar, Y.D., E-mail: ydkolekar@gmail.com [Department of Physics, Savitribai Phule Pune University, Pune, 411007, Maharashtra (India); Ramana, C.V., E-mail: rvchintalapalle@utep.edu [Department of Mechanical Engineering, University of Texas at El Paso, El Paso, TX, 79968 (United States)

    2017-08-31

    Cobalt (Co) nanoparticles (NPs) were produced by a simple, one step hydrothermal method with the capping of oleic acid. Intrinsic structural, physiochemical and magnetic properties of Co NPs were investigated and demonstrated their applicability in biomedicine. X-ray diffraction, Raman spectroscopy and infrared (IR) spectroscopic studies confirm the single phase Co NPs with a high structural quality. The IR data revealed the capping of oleic acid via monodentate interaction. Small angle scattering studies suggest the existence of sticky hard sphere type of interaction among the Co NPs because of magnetic interaction which is further evidenced by electron microscopy imaging analyses. The Co NPs exhibit a ferromagnetic character over a wide range of temperature (20–300 K). The temperature dependence of magnetic parameters namely, saturation magnetization, remanent magnetization, coercivity and reduced remanent magnetization were determined and correlated with structure of Co NPs. The Cytotoxicity studies demonstrate that these Co NPs exhibit the mild anti-proliferative character against the cancer cells (cisplatin resistant ovarian cancer (A2780/CP70)) and safe nature towards the normal cells. Haemolytic behavior of human red blood cells (RBC) revealed (<5%) haemolysis signifying the compatibility of Co NPs with human RBC which is an essential feature in vivo biomedical applications without creating any harmful effects in the human blood stream.

  14. Concanavalin A-mediated in vitro activation of a secondary cytotoxic T-cell response in virus-primed splenocytes

    DEFF Research Database (Denmark)

    Thomsen, Allan Randrup; Jensen, B L

    1980-01-01

    In a recent report it was shown that what appeared to be secondary cytotoxic T cells could be obtained from lymphocytic choriomeningitis virus (LCMV)-primed splenocytes after stimulation in vitro with the non-specific T cell mitogen concanavalin A (Con A). The present experiments attempt to chara......In a recent report it was shown that what appeared to be secondary cytotoxic T cells could be obtained from lymphocytic choriomeningitis virus (LCMV)-primed splenocytes after stimulation in vitro with the non-specific T cell mitogen concanavalin A (Con A). The present experiments attempt...... to characterize further these effector cells and, in particular, to establish whether the Con A-activated cytotoxic effectors are qualitatively different from the secondary cytotoxic T cells induced by restimulation with the homologous antigen. It was found that: (1) in vitro activation with Con A could......, since no evidence was found to indicate a role for other cell types or soluble (cytotoxic or arming) factors; (4) cytotoxicity was specific with regard to both virus and 'self'. By comparison with previous data on LCMV-induced cytotoxic T cells, it is concluded that Con A induces the generation...

  15. All-trans retinoic acid negatively regulates cytotoxic activities of nature killer cell line 92

    International Nuclear Information System (INIS)

    Li Ang; He Meilan; Wang Hui; Qiao Bin; Chen Ping; Gu Hua; Zhang Mengjie; He Shengxiang

    2007-01-01

    NK cells are key components of innate immune systems and their activities are regulated by cytokines and hormones. All-trans retinoic acid (ATRA), as a metabolite of vitamin A and an immunomodulatory hormone, plays an important role in regulating immune responses. In the present study, we investigated the effect of ATRA on human NK cell line NK92. We found that ATRA dose-dependently suppressed cytotoxic activities of NK92 cells without affecting their proliferation. To explore the mechanisms underlying the ATRA influence on NK92 cells, we examined the production of cytokines (TNF-α, IFN-γ), gene expression of cytotoxic-associated molecules (perforin, granzyme B, nature killer receptors (NCRs), and NKG2D), and the activation of NF-κB pathways related with immune response. Our results demonstrated that ATRA suppressed NF-κB activity and prevented IκBα degradation in a dose-dependent way, inhibited IFN-γ production and gene expression of granzyme B and NKp46. Our findings suggest that ATRA is a negative regulator of NK92 cell activation and may act as a potential regulator of anti-inflammatory functions in vivo

  16. 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.

  17. 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.

  18. 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

  19. Essential Oil from the Resin of Protium heptaphyllum: Chemical Composition, Cytotoxicity, Antimicrobial Activity, and Antimutagenicity.

    Science.gov (United States)

    de Lima, Ewelyne Miranda; Cazelli, Didley Sâmia Paiva; Pinto, Fernanda Endringer; Mazuco, Renata Alves; Kalil, Ieda Carneiro; Lenz, Dominik; Scherer, Rodrigo; de Andrade, Tadeu Uggere; Endringer, Denise Coutinho

    2016-01-01

    Protium heptaphyllum (Aubl.) March is popularly used as an analgesic and anti-inflammatory agent. This study aimed to evaluate the chemical composition of P. heptaphyllum essential oil, its cytotoxicity in a breast cancer cell line (MCF-7), antimicrobial activity, and its antimutagenicity in vivo. The chemical composition of the essential oil collected in three 3 years was determined by gas chromatography-mass spectrometry. The cytotoxicity was evaluated using a 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. Annexin V conjugated with fluorescein isothiocyanate, caspase-3, and tumor necrosis factor-alpha (TNF-α) assays were performed to evaluate apoptosis and inflammatory events. The antimutagenic activity at doses of 25, 50, and 100 mg/kg was determined using a micronucleus test in murine bone marrow. The essential oil showed a predominance of monoterpene compounds, being the terpinolene, p-cymene-8-ol, and p-cymene, present in the essential oil extracted in the 3 years. The essential oil showed a protection against cyclophosphamide-induced genotoxicity, and the cytotoxicity index polychromatic erythrocytes/normochromatic erythrocytes ratio in animals treated with oil at all doses (1.34 ± 0.33; 1.15 ± 0.1; 1.11 ± 0.13) did not differ from the negative control animal (1.31 ± 0.33), but from the cyclophosphamide group (0.61 ± 0.12). Cytotoxicity, at a concentration of 40.0 μg/mL, and antimicrobial activity were not observed for the essential oil (minimum inhibitory concentration ≥0.5 mg/mL). The essential oil did not change the levels of caspase-3 in the TNF-α level. The essential oil showed antimutagenic activity due to its chemical composition. Terpinolene, p-cymene-8-ol, and p-cymene are the main constituents of the essential oil of P. heptaphyllum collected within 3-yearsThe essential oil of P. heptaphyllum did not show antimicrobial activity (MIC >0.5 mg/mL) against E. coli, S. aureus, E. faecalis, and C. albicansThe essential oil

  20. Synthesis, antimicrobial, and antiproliferative activities of substituted phenylfuranylnicotinamidines

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    Youssef MM

    2016-03-01

    Full Text Available Magdy M Youssef,1,2 Reem K Arafa,3,4 Mohamed A Ismail1,21Department of Chemistry, College of Science, King Faisal University, Hofuf, Saudi Arabia; 2Department of Chemistry, Faculty of Science, Mansoura University, Mansoura, 3Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Cairo University, Cairo, 4Biomedical Sciences Program, University of Science and Technology, Zewail City of Science and Technology, Cairo, EgyptAbstract: This research work deals with the design and synthesis of a series of substituted phenylfuranylnicotinamidines 4a–i. Facile preparation of the target compounds was achieved by Suzuki coupling-based synthesis of the nitrile precursors 3a–i, followed by their conversion to the corresponding nicotinamidines 4a–i utilizing LiN(TMS2. The antimicrobial activities of the newly synthesized nicotinamidine derivatives were evaluated against the Gram-negative bacterial strains Escherichia coli and Pseudomonas aeruginosa as well as the Gram-positive bacterial strains Staphylococcus aureus and Bacillus megaterium. The minimum inhibitory concentration values of nicotinamidines against all tested microorganisms were in the range of 10–20 µM. In specific, compounds 4a and 4b showed excellent minimum inhibitory concentration values of 10 µM against Staphylococcus aureus bacterial strain and were similar to ampicillin as an antibacterial reference. On the other hand, selected nicotinamidine derivatives were biologically screened for their cytotoxic activities against a panel of 60 cell lines representing nine types of human cancer at a single high dose at National Cancer Institute, Bethesda, MD, USA. Nicotinamidines showing promising activities were further assessed in a five-dose screening assay to determine their compound concentration causing 50% growth inhibition of tested cell (GI50, compound concentration causing 100% growth inhibition of tested cell (TGI, and compound concentration causing 50% lethality of tested

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

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    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.

  2. Involvement of ER stress and activation of apoptotic pathways in fisetin induced cytotoxicity in human melanoma.

    Science.gov (United States)

    Syed, Deeba N; Lall, Rahul K; Chamcheu, Jean Christopher; Haidar, Omar; Mukhtar, Hasan

    2014-12-01

    The prognosis of malignant melanoma remains poor in spite of recent advances in therapeutic strategies for the deadly disease. Fisetin, a dietary flavonoid is currently being investigated for its growth inhibitory properties in various cancer models. We previously showed that fisetin inhibited melanoma growth in vitro and in vivo. Here, we evaluated the molecular basis of fisetin induced cytotoxicity in metastatic human melanoma cells. Fisetin treatment induced endoplasmic reticulum (ER) stress in highly aggressive A375 and 451Lu human melanoma cells, as revealed by up-regulation of ER stress markers including IRE1α, XBP1s, ATF4 and GRP78. Time course analysis indicated that the ER stress was associated with activation of the extrinsic and intrinsic apoptotic pathways. Fisetin treated 2-D melanoma cultures displayed autophagic response concomitant with induction of apoptosis. Prolonged treatment (16days) with fisetin in a 3-D reconstituted melanoma model resulted in inhibition of melanoma progression with significant apoptosis, as evidenced by increased staining of cleaved Caspase-3 in the treated constructs. However, no difference in the expression of autophagic marker LC-3 was noted between treated and control groups. Fisetin treatment to 2-D melanoma cultures resulted in phosphorylation and activation of the multifunctional AMP-activated protein kinase (AMPK) involved in the regulation of diverse cellular processes, including autophagy and apoptosis. Silencing of AMPK failed to prevent cell death indicating that fisetin induced cytotoxicity is mediated through both AMPK-dependent and -independent mechanisms. Taken together, our studies confirm apoptosis as the primary mechanism through which fisetin inhibits melanoma cell growth and that activation of both extrinsic and intrinsic pathways contributes to fisetin induced cytotoxicity.

  3. 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

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    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.

  4. Detection of tumor-specific cytotoxic drug activity in vitro using the fluorometric microculture cytotoxicity assay and primary cultures of tumor cells from patients.

    Science.gov (United States)

    Nygren, P; Fridborg, H; Csoka, K; Sundström, C; de la Torre, M; Kristensen, J; Bergh, J; Hagberg, H; Glimelius, B; Rastad, J

    1994-03-01

    The semi-automated fluorometric microculture cytotoxicity assay (FMCA), based on the measurement of fluorescence generated from cellular hydrolysis of fluorescein diacetate (FDA) by viable cells, was employed for cytotoxic drug sensitivity testing of tumor cells from patients with hematological or solid tumors. In total, 390 samples from 20 diagnoses were tested with up to 12 standard cytotoxic drugs. The technical success rate for different tumor types ranged from 67 to 95%. Fluorescence was linearly related to cell number but variably steep depending on tumor type. Samples from most solid tumors thus showed higher signal-to-noise ratios than hematological samples. A wide spectrum of in vitro drug activity was obtained, with acute leukemias and non-Hodgkin's lymphomas being sensitive to almost all tested drugs, whereas renal and adrenocortical carcinomas were essentially totally resistant. Between these extremes were samples of breast and ovarian carcinomas and sarcomas. When in vitro response was compared with known clinical response patterns, a good correspondence was observed. The results indicate that the FMCA is a rapid and efficient method for in vitro measurement of tumor-specific drug activity both in hematological and in solid tumors. The assay may be suitable for new drug development and direction of phase-2 trials to suitable patients.

  5. Synthesis, Characterization and In Vitro Anticancer Activity of C-5 Curcumin Analogues with Potential to Inhibit TNF-α-Induced NF-κB Activation

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    Amit Anthwal

    2014-01-01

    Full Text Available In a search of new compounds active against cancer, synthesis of a series of C-5 curcumin analogues was carried out. The new compounds demonstrated good cytotoxicity against chronic myeloid leukemia (KBM5 and colon cancer (HCT116 cell lines. Further, these compounds were found to have better potential to inhibit TNF-α-induced NF-κB activation in comparison to curcumin, which show their potential to act as anti-inflammatory agents. Some compounds were found to show higher cytotoxicity against cancer cell lines in comparison to curcumin used as standard.

  6. 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.

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

    Science.gov (United States)

    Salam, Nimaichand; Khieu, Thi-Nhan; Liu, Min-Jiao; Vu, Thu-Trang; Chu-Ky, Son; Quach, Ngoc-Tung; Phi, Quyet-Tien; Narsing Rao, Manik Prabhu; Fontana, Angélique; Sarter, Samira; Li, Wen-Jun

    2017-01-01

    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 IC 50 -values ranging between 3 and 33  μ g·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.

  8. Cytotoxicity, antimicrobial and antioxidant activity of eight compounds isolated from Entada abyssinica (Fabaceae).

    Science.gov (United States)

    Dzoyem, Jean P; Melong, Raduis; Tsamo, Armelle T; Tchinda, Alembert T; Kapche, Deccaux G W F; Ngadjui, Bonaventure T; McGaw, Lyndy J; Eloff, Jacobus N

    2017-03-06

    Entada abyssinica is a plant traditionally used against gastrointestinal bacterial infections. Eight compounds including three flavonoids, three terpenoids, a monoglyceride and a phenolic compound isolated from E. abyssinica were investigated for their cytotoxicity, antibacterial and antioxidant activity. Compounds 7 and 2 had remarkable activity against Salmonella typhimurium with the lowest respective minimum inhibitory concentration (MIC) values of 1.56 and 3.12 µg/mL. The antioxidant assay gave IC 50 values varied from 0.48 to 2.87 μg/mL in the 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay, from 2.53 to 17.04 μg/mL in the 2,2'-Azino-bis (3-ethylbenzothiazoline-6-sulphonic acid) diammonium salt (ABTS) assay and from 1.43 to 103.98 µg/mL in the FRAP assay. Compounds had relatively low cytotoxicity (LC 50 values ranging from 22.42 to 80.55 µg/mL) towards Vero cells. Ursolic acid had the most potent cytotoxicity against THP-1 and RAW 264.7 cells with LC 50 values of 9.62 and 4.56 μg/mL respectively, and selectivity index values of 7.32 and 15.44 respectively. Our findings suggest that among the terpenoid and flavonoid compounds studied, entadanin (compound 7) possess tremendous antibacterial activity against S. typhimurium and could be developed for the treatment of bacterial diseases.

  9. Phytochemical composition, anti-inflammatory activity and cytotoxic effects of essential oils from three Pinus spp.

    Science.gov (United States)

    Basholli-Salihu, Mimoza; Schuster, Roswitha; Hajdari, Avni; Mulla, Dafina; Viernstein, Helmut; Mustafa, Behxhet; Mueller, Monika

    2017-12-01

    Inflammation and cell differentiation lead to a number of severe diseases. In the recent years, various studies focused on the anti-inflammatory and anticancer activity of essential oils (EOs) of numerous plants, including different Pinus species. The phytochemical composition, anti-inflammatory and cytotoxic activity of EOs from needles and twigs of Pinus heldreichii Christ (Pinaceae) and P. peuce Griseb., and from needles, twigs and cones of P. mugo Turra were determined. For separation and identification of the EOs, gas chromatography/flame ion detector (GC/FID) and GC/mass spectrometry were performed. The amount of secreted IL-6 in a lipopolysaccharide (LPS)-stimulated macrophage model was quantified (concentration of oils: 0.0001-0.2%, 3 h incubation). Cytotoxicity on the cancer cell lines HeLa, CaCo-2 and MCF-7 were determined using a MTT (Thiazolyl Blue Tetrazolium Bromide) assay (concentration of oils: 0.001-0.1%, 24 h incubation). The most prominent members in the oils include: δ-3-carene, α-pinene and linalool-acetate (P. mugo); α-pinene, β-phellandrene and β-pinene (P. peuce); limonene, α-pinene and (E)-caryophyllene (P. heldreichii). EOs showed significant cytotoxic effects on cancer cell lines (IC 50 0.007 to >0.1%), with a reduction in cell viability with up to 90% at a concentration of 0.1%, and anti-inflammatory activity (IC 50 0.0008-0.02%) with a reduction of IL-6 secretion with up to 60% at a concentration of 0.01%. The EOs of needles and twigs from P. peuce and P. heldreichii as well as of needles, twigs and cones of P. mugo can be considered as promising agents for anticancer and anti-inflammatory drugs.

  10. Phytochemical screening, antioxidant and cytotoxic activity of fruit extracts of Calamus tenuis Roxb

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    Zaki Uddin Ahmed

    2014-08-01

    Full Text Available Objective: To investigate the antioxidant and cytotoxic activity of the fruits of Calamus tenuis Roxb. Methods: The preliminary phytochemical group tests were done, which revealed the presence of alkaloid, tannin, flavonoid and steroid. The dried fruit was extracted in soxhlet apparatus using petroleum ether, ethyl acetate and methanol. Antioxidant potential of each extract was evaluated using total phenol content, total flavonoid content, cupric reducing antioxidant capacity, 1,1-diphenyl-2-picrylhydrazyl radical scavenging activity, and total antioxidant capacity determinations. Results: The extracts were found to possess moderate to high amounts of phenolic and flavonoid contents. In cupric reducing antioxidant capacity assay the extracts showed moderate reducing power which increases with concentration. Scavenging of 1,1-diphenyl-2-picrylhydrazyl radical was found to rise with concentration with lowest IC50 value for methanol extract, which was confirmed by total antioxidant activity test that shows highest (95 mg/g of extract in ascorbic acid equivalent for methanol extract. In Brine shrimp lethality bioassay the methanol and petroleum ether extracts were found to be toxic to Brine shrimp nauplii, with LC50 of 25.53 µg/mL and 28.07 µg/mL respectively while the LC50 of the reference vincristine sulphate was 1.32 µg/mL. Ethyl acetate extract was found to be moderately cytotoxic showing LC50 of 47.79 µg/mL. Conclusions: The results of the present study suggest that the fruits of Calamus tenuis Roxb possess antioxidant and cytotoxic potential. Moreover, phytochemical screening reveals the presence of alkaloid, tannin, flavonoid and steroid, which may be responsible for the observed bioactivities.

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

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    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.

  12. Antioxidant, cytotoxic and alpha-glucosidase inhibition activities from the Mexican berry "Anacahuita" (Cordia boissieri).

    Science.gov (United States)

    Viveros-Valdez, Ezequiel; Jaramillo-Mora, Carlos; Oranday-Cardenas, Azucena; Mordn-Martinez, Javier; Carranza-Rosales, Pilar

    2016-09-01

    This study describes the total phenolic and flavonoid content as well as cytotoxic, alpha-glucosidase inhibition and antiradical/antioxidant potential of extracts obtained from the edible fruits of Cordia boissieri, which is widely distributed throughout northeastern Mexico. Phenolic and flavonoid content were evaluated by means of the Folin-Ciocalteu method and aluminum chloride colorimetric assay respectively. The antiradical/antioxidant activity was determined by the 2,2-diphenyl-1-picrylhydrazyl (DPPH) scavenging and Trolox Equivalent Antioxidant Capacity (TEAC) assays. Cytotoxic activity was assessed by means of human cancer cell lines (MCF-7 and HeLa), alpha-glucosidase inhibition was determined by colorimetric assay using p-Nitrophenyl a-D-glucopyranoside (PNPG) as a substrate. Results indicate that extract of C. boissieri fruit has a good antioxidant potential to show a EC₅₀: 137.76 ± 35 ptg/mL and 65 ±2 ltM/g in the DPPH and TEAC assays respectively, inhibitor of the enzyme alpha-glu- cosidase involved in sugar uptake (ICSO: 215.20 ± 35 μg/ mL), cytotoxic activities against MCF-7 (IC50: 310 ± 42 μg/mL) and HeLa (IC₅₀0: 450.4 ±21μgg/mL) cancer cell lines as well as an important phenolic content with 230 t 23 mg/1OOg and 54±11 mg100g g of phenols and flavonoids totals respectively. These results point towards an interesting potential for the fruits of C. boissieri as chemopreventive properties and expand the possibilities.

  13. Microbial degradation, cytotoxicity and antibacterial activity of polyurethanes based on modified castor oil and polycaprolactone.

    Science.gov (United States)

    Uscátegui, Yomaira L; Arévalo, Fabián R; Díaz, Luis E; Cobo, Martha I; Valero, Manuel F

    2016-10-11

    The objective of this study was to assess the effects of type of polyol and concentration of polycaprolactone (PCL) in polyurethanes (PUs) on microbial degradability, cytotoxicity, biological properties and antibacterial activity to establish whether these materials may have biomedical applications. Chemically modified and unmodified castor oil, PCL and isophorone diisocyanate in a 1:1 ratio of NCO/OH were used. PUs were characterized by stress/strain fracture tests and hardness (ASTM D 676-59). Hydrophilic character was determined by contact angle trials and morphology was evaluated by scanning electron microscopy. Degradability with Escherichia coli and Pseudomonas aeruginosa was evaluated by measuring variations in the weight of the polymers. Cytotoxicity was evaluated using the ISO 10993-5 (MTT) method with mouse embryonic fibroblasts L-929 (ATCC® CCL-1) in direct contact with the PUs and with NIH/3T3 cells (ATCC® CRL-1658) in indirect contact with the PUs. Antimicrobial activity against E. coli and P. aeruginosa was determined. PUs derived from castor oil modified (P0 and P1) have higher mechanical properties than PUs obtained from castor oil unmodified (CO). The viability of L-929 mouse fibroblasts in contact with polymers was greater than 70%. An assessment of NIH/3T3 cells in indirect contact with PUs revealed no-toxic degradation products. Finally, the antibacterial effect of the PUs decreased by 77% for E. coli and 56% for P. aeruginosa after 24 h. These results indicate that PUs synthesized with PCL have biocidal activity against Gram-negative bacteria and do not induce cytotoxic responses, indicating the potential use of these materials in the biomedical field.

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

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    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.

  15. Synthesis of Thiolated Alginate and Evaluation of Mucoadhesiveness, Cytotoxicity and Release Retardant Properties

    Science.gov (United States)

    Jindal, A. B.; Wasnik, M. N.; Nair, Hema A.

    2010-01-01

    Modification of polymers by covalent attachment of thiol bearing pendant groups is reported to impart many beneficial properties to them. Hence in the present study, sodium alginate–cysteine conjugate was synthesized by carbodiimide mediated coupling under varying reaction conditions and the derivatives characterized for thiol content. The thiolated alginate species synthesized had bound thiol content ranging from 247.8±11.03–324.54±10.107 ΅mol/g of polymer depending on the reaction conditions. Matrix tablets based on sodium alginate-cysteine conjugate and native sodium alginate containing tramadol hydrochloride as a model drug were prepared and mucoadhesive strength and in vitro drug release from the tablets were compared. Tablets containing 75 mg sodium alginate-cysteine conjugate could sustain release of 10 mg of model drug for 3 h, whereas 90% of the drug was released within 1 h from corresponding tablets prepared using native sodium alginate. An approximately 2-fold increase in the minimal detachment force of the tablets from an artificial mucin film was observed for sodium alginate–cysteine conjugate as compared to native sodium alginate. In vitro cytotoxicity studies in L-929 mouse fibroblast cells studied using an MTT assay revealed that at low concentrations of polymer, sodium alginate–cysteine conjugate was less toxic to L-929 mouse fibroblast cell line when compared to native sodium alginate. Hence, thiolation is found to be a simple route to improving polymer performance. The combination of improved controlled drug release and mucoadhesive properties coupled with the low toxicity of these new excipients builds up immense scope for the use of thiolated polymers in mucoadhesive drug delivery systems. PMID:21969750

  16. A new kaempferol triglycoside from Fagonia taeckholmiana: cytotoxic activity of its extracts.

    Science.gov (United States)

    Ibrahim, Lamyaa F; Kawashty, Salwa A; El-Hagrassy, Ali M; Nassar, Mahmoud I; Mabry, Tom J

    2008-01-14

    In addition to apigenin, apigenin 7-O-glucoside, kaempferol 3-O-glucoside, kaempferol 3,7-di-O-rhamnoside, quercetin, and quercetin 3-O-glucoside, the methanolic extract of Fagonia taeckholmiana afforded a new compound identified as kaempferol 3-O-beta-l-arabinopyranosyl-(1-->4)-alpha-l-rhamnopyranoside-7-O-alpha-l-rhamnopyranoside. Identification of the isolated compounds was based on chemical and spectroscopic analyses including UV, FABMS, (1)H, (13)C and 2D NMR, and DEPT. The cytotoxic activities of the compounds against several cancer cell lines were determined.

  17. 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

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

    Directory of Open Access Journals (Sweden)

    Ângela Sena-Lopes

    Full Text Available 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

  19. 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.

  20. Synthesis, characterization, antimicrobial activity and molecular ...

    African Journals Online (AJOL)

    Synthesis, characterization, antimicrobial activity and molecular docking studies of combined pyrazol-barbituric acid pharmacophores. Assem Barakat, Bandar M. Al-Qahtani, Abdullah M. Al-Majid, M. Ali Mohammed Rafi Shaik, Mohamed H.M. Al-Agamy, Abdul Wadood ...

  1. Synthesis, Characterization, Antimicrobial Activity and Antioxidant ...

    African Journals Online (AJOL)

    MBI

    2015-12-08

    Dec 8, 2015 ... Synthesis, Characterization, Antimicrobial Activity and Antioxidant. Studies of ... Transition metal complexes of Co(II) and Ni(II) with Schiff base ligand (HL) derived from condensation of 2- ..... 2-((5mercapto-1,3,4-thiadiazol-2-.

  2. Flow cytometric estimation on cytotoxic activity of leaf extracts from seashore plants in subtropical Japan: isolation, quantification and cytotoxic action of (-)-deoxypodophyllotoxin.

    Science.gov (United States)

    Masuda, Toshiya; Oyama, Yasuo; Yonemori, Shigetomo; Takeda, Yoshio; Yamazaki, Yuko; Mizuguchi, Shinichi; Nakata, Mami; Tanaka, Tomochika; Chikahisa, Lumi; Inaba, Yuzuru; Okada, Yoshihiko

    2002-06-01

    The cytotoxic activity of methanol extracts of leaves collected from 39 seashore plants in Iriomote Island, subtropical Japan was examined on human leukaemia cells (K562 cells) using a flow cytometer with two fluorescent probes, ethidium bromide and annexin V-FITC. Five extracts (10 microg/mL) from Hernandia nymphaeaefolia, Cerbera manghas, Pongamia pinnata, Morus australis var. glabra and Thespesia populnea greatly inhibited the growth of K562 cells. When the concentration was decreased to 1 microg/mL, only one extract from H. nymphaeaefolia still inhibited the cell growth. A cytotoxic compound was isolated from the leaves by bioassay-guided fractionation and was identified as (-)-deoxypodophyllotoxin (DPT). The fresh leaves of H. nymphaeaefolia contained a remarkably high amount of DPT (0.21 +/- 0.07% of fresh leaf weight), being clarified by a quantitative HPLC analysis. DPT at 70-80 pM started to inhibit the growth of K562 cells in an all-or-none fashion and at 100 pM or more it produced complete inhibition in all cases. Therefore, the slope of the dose-response curve was very steep. DPT at 100 pM or more decreased the cell viability to 50%-60% and increased the number of cells undergoing apoptosis (annexin V-positive cells). The results indicate that DPT contributes to the cytotoxic action of the extract from the leaves of H. nymphaeaefolia on K562 cells. Copyright 2002 John Wiley & Sons, Ltd.

  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. Structure-activity relationship of antiparasitic and cytotoxic indoloquinoline alkaloids, and their tricyclic and bicyclic analogues.

    Science.gov (United States)

    Van Baelen, Gitte; Hostyn, Steven; Dhooghe, Liene; Tapolcsányi, Pál; Mátyus, Péter; Lemière, Guy; Dommisse, Roger; Kaiser, Marcel; Brun, Reto; Cos, Paul; Maes, Louis; Hajós, György; Riedl, Zsuzsanna; Nagy, Ildikó; Maes, Bert U W; Pieters, Luc

    2009-10-15

    Based on the indoloquinoline alkaloids cryptolepine (1), neocryptolepine (2), isocryptolepine (3) and isoneocryptolepine (4), used as lead compounds for new antimalarial agents, a series of tricyclic and bicyclic analogues, including carbolines, azaindoles, pyrroloquinolines and pyrroloisoquinolines was synthesized and biologically evaluated. None of the bicyclic compounds was significantly active against the chloroquine-resistant strain Plasmodium falciparum K1, in contrast to the tricyclic derivatives. The tricyclic compound 2-methyl-2H-pyrido[3,4-b]indole (9), or 2-methyl-beta-carboline, showed the best in vitro activity, with an IC(50) value of 0.45 microM against P. falciparum K1, without apparent cytotoxicity against L6 cells (SI>1000). However, this compound was not active in the Plasmodium berghei mouse model. Structure-activity relationships are discussed and compared with related naturally occurring compounds.

  5. Cytotoxic and apoptosis-inducing activity of C21 steroids from the roots of Cynanchum atratum.

    Science.gov (United States)

    Zhang, Jian; Ma, Lin; Wu, Zheng-Feng; Yu, Shu-Le; Wang, Lei; Ye, Wen-Cai; Zhang, Qing-Wen; Yin, Zhi-Qi

    2017-06-01

    Two new (1-2) and two known C 21 steroids (3-4) were isolated from the roots of Cynanchum atratum. Their structures were elucidated by detailed 1D and 2D spectroscopic. The MTT assay showed that compounds 1-4 displayed obvious cytotoxic activities against HepG2 cells with IC 50 values ranging from 10.19μM to 76.12μM. Compounds 1-3 also exhibited cytotoxic effects in A549 cells with IC 50 values of 30.87-95.39μM. Compound 3 showed the antiproliferative activity via G0/G1 cell cycle arrest and proapoptosis in HepG2 cells by Flowcytometry analysis. Western blotting analysis revealed that compound 3 could induce HepG2 cell apoptosis via the mitochondrial pathway by downregulating Bcl-2 expression, upregulating Bax protein expression, and activating caspase-9 and caspase-3. Copyright © 2017 Elsevier Inc. All rights reserved.

  6. 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%.

  7. Neolignans from Nectandra megapotamica (Lauraceae Display in vitro Cytotoxic Activity and Induce Apoptosis in Leukemia Cells

    Directory of Open Access Journals (Sweden)

    Vitor Ponci

    2015-07-01

    Full Text Available Nectandra megapotamica (Spreng. Mez. (Lauraceae is a well-known Brazilian medicinal plant that has been used in folk medicine to treat several diseases. In continuation of our ongoing efforts to discover new bioactive natural products from the Brazilian flora, this study describes the identification of cytotoxic compounds from the MeOH extract of N. megapotamica (Lauraceae leaves using bioactivity-guided fractionation. This approach resulted in the isolation and characterization of eight tetrahydrofuran neolignans: calopeptin (1, machilin-G (2, machilin-I (3, aristolignin (4, nectandrin A (5, veraguensin (6, ganschisandrin (7, and galgravin (8. Different assays were conducted to evaluate their cytotoxic activities and to determine the possible mechanism(s related to the activity displayed against human leukemia cells. The most active compounds 4, 5 and 8 gave IC50 values of 14.2 ± 0.7, 16.9 ± 0.8 and 16.5 ± 0.8 µg/mL, respectively, against human leukemia (HL-60 tumor cells. Moreover, these compounds induced specific apoptotic hallmarks, such as plasma membrane bleb formation, nuclear DNA condensation, specific chromatin fragmentation, phosphatidyl-serine exposure on the external leaflet of the plasma membrane, cleavage of PARP as well as mitochondrial damage, which as a whole could be related to the intrinsic apoptotic pathway.

  8. Texas Native Plants Yield Compounds with Cytotoxic Activities against Prostate Cancer Cells.

    Science.gov (United States)

    Shaffer, Corena V; Cai, Shengxin; Peng, Jiangnan; Robles, Andrew J; Hartley, Rachel M; Powell, Douglas R; Du, Lin; Cichewicz, Robert H; Mooberry, Susan L

    2016-03-25

    There remains a critical need for more effective therapies for the treatment of late-stage and metastatic prostate cancers. Three Texas native plants yielded three new and three known compounds with antiproliferative and cytotoxic activities against prostate cancer cells with IC50 values in the range of 1.7-35.0 μM. A new sesquiterpene named espadalide (1), isolated from Gochnatia hypoleuca, had low micromolar potency and was highly effective in clonogenic assays. Two known bioactive germacranolides (2 and 3) were additionally isolated from G. hypoleuca. Dalea frutescens yielded two new isoprenylated chalcones, named sanjuanolide (4) and sanjoseolide (5), and the known sesquiterpenediol verbesindiol (6) was isolated from Verbesina virginica. Mechanistic studies showed that 1-4 caused G2/M accumulation and the formation of abnormal mitotic spindles. Tubulin polymerization assays revealed that 4 increased the initial rate of tubulin polymerization, but did not change total tubulin polymer levels, and 1-3 had no effects on tubulin polymerization. Despite its cytotoxic activity, compound 6 did not initiate changes in cell cycle distribution and has a mechanism of action different from the other compounds. This study demonstrates that new compounds with significant biological activities germane to unmet oncological needs can be isolated from Texas native plants.

  9. 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)

  10. 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

  11. Effects of human pharmaceuticals on cytotoxicity, EROD activity and ROS production in fish hepatocytes

    International Nuclear Information System (INIS)

    Laville, N.; Aiet-Aiessa, S.; Gomez, E.; Casellas, C.; Porcher, J.M.

    2004-01-01

    Pharmaceuticals are found in the aquatic environment but their potential effects on non-target species like fish remain unknown. This in vitro study is a first approach in the toxicity assessment of human drugs on fish. Nine pharmaceuticals were tested on two fish hepatocyte models: primary cultures of rainbow trout hepatocytes (PRTH) and PLHC-1 fish cell line. Cell viability, interaction with cytochrome P450 1A (CYP1A) enzyme and oxidative stress were assessed by using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrasodium bromide tetrazolium (MTT), 7-ethoxyresorufin-o-deethylase (EROD) and dichlorofluorescein (DCFH-DA) assays, respectively. The tested drugs were clofibrate (CF), fenofibrate (FF), carbamazepine (CBZ), fluoxetine (FX), diclofenac (DiCF), propranolol (POH), sulfamethoxazole (SFX), amoxicillin (AMX) and gadolinium chloride (GdCl 3 ). All substances were cytotoxic, except AMX at concentration up to 500 μM. The calculated MTT EC 50 values ranged from 2 μM (CF) to 651 μM (CBZ) in PLHC-1, and from 53 μM (FF) to 962 μM (GdCl 3 ) in PRTH. CF, FF, and FX were the most cytotoxic drugs and induced oxidative stress before being cytotoxic. Compared to hepatocytes from human and dog, fish hepatocytes seemed to be more susceptible to the peroxisome proliferators (PPs) CF and FF. In PLHC-1 cells none of the tested drugs induced the EROD activity whereas POH appeared as a weak EROD inducer in PRTH. Moreover, in PRTH, SFX, DiCF, CBZ and to a lesser extend, FF and CF inhibited the basal EROD activity at clearly sublethal concentrations which may be of concern at the biological and chemical levels in a multipollution context

  12. Antimicrobial Activity of Hippurate Nano composite and Its Cytotoxicity Effect in Combination with Cytarabine against HL-60

    International Nuclear Information System (INIS)

    Al Ali, S.H.H.; Al-Qubaisi, M.; Ismail, M.; El Zowalaty, M.; Hussein, M.Z.; Ismail, M.

    2013-01-01

    Hippuric acid (HA) was intercalated into a zinc-layered hydroxide (ZLH) by direct reaction of an aqueous suspension of zinc oxide with an aqueous solution of hippuric acid to obtain hippurate nano composite (HAN). Various concentrations of hippuric acid (0.05, 0.2, and 0.4 molar) were used for the synthesis of the nano composite. The as-synthesized HAN using 0.2 molar was found to give a well-ordered layered nano composite material with an increase in the basal spacing to 21.3 Å which indicated the insertion of hippurate organic moiety into the ZLH interlayers. The cytotoxicity of HAN in combination with cytarabine against human promyelocytic leukemia cells (HL-60) was tested using MTT cell viability assay and trypan blue dye exclusion assay. The combination of cytarabine with HAN showed higher tumor suppression efficiency as compared to that of cytarabine alone. The IC 50 values of HAN/cytarabine combination and cytarabine alone were μg/mL and μg/mL, respectively. DNA fragmentation was also studied, and the exposure of HL-60 cells to cytarabine produced % DNA fragmentation compared to % when cells were exposed to combination of cytarabine with HAN. The antimicrobial activity of hippuric acid and HAN nano composite was carried out against Gram-positive bacteria, Gram-negative bacteria, and yeasts. It was found that Pseudomonas aeruginosa and methicillin-resistant Staphylococcus aureus were more sensitive to HAN compared to Bacillus subtilis and Salmonella choleraesuis

  13. DNA and factor VII-activating protease protect against the cytotoxicity of histones

    NARCIS (Netherlands)

    Marsman, Gerben; von Richthofen, Helen; Bulder, Ingrid; Lupu, Florea; Hazelzet, Jan; Luken, Brenda M.; Zeerleder, Sacha

    2017-01-01

    Circulating histones have been implicated as major mediators of inflammatory disease because of their strong cytotoxic effects. Histones form the protein core of nucleosomes; however, it is unclear whether histones and nucleosomes are equally cytotoxic. Several plasma proteins that neutralize

  14. Antifungal, Antileishmanial, and Cytotoxicity Activities of Various Extracts of Berberis vulgaris (Berberidaceae) and Its Active Principle Berberine.

    Science.gov (United States)

    Mahmoudvand, Hossein; Ayatollahi Mousavi, Seyyed Amin; Sepahvand, Asghar; Sharififar, Fariba; Ezatpour, Behrouz; Gorohi, Fatemeh; Saedi Dezaki, Ebrahim; Jahanbakhsh, Sareh

    2014-01-01

    In this study, in vitro antidermatophytic activity against Trichophyton mentagrophytes, Trichophyton rubrum, Microsporum canis, and Microsporum gypseum was studied by disk diffusion test and assessment of minimum inhibitory concentration (MIC) using CLSI broth macrodilution method (M38-A2). Moreover, antileishmanial and cytotoxicity activity of B. vulgaris and berberine against promastigotes of Leishmania major and Leishmania tropica were evaluated by colorimetric MTT assay. The findings indicated that the various extracts of B. vulgaris particularly berberine showed high potential antidermatophytic against pathogenic dermatophytes tested with MIC values varying from 0.125 to >4 mg/mL. The results revealed that B. vulgaris extracts as well as berberine were effective in inhibiting L. major and L. tropica promastigotes growth in a dose-dependent manner with IC50 (50% inhibitory concentration) values varying from 2.1 to 26.6  μ g/mL. Moreover, it could be observed that berberine as compared with B. vulgaris exhibited more cytotoxicity against murine macrophages with CC50 (cytotoxicity concentration for 50% of cells) values varying from 27.3 to 362.6  μ g/mL. Results of this investigation were the first step in the search for new antidermatophytic and antileishmanial drugs. However, further works are required to evaluate exact effect of these extracts in animal models as well as volunteer human subjects.

  15. Ex-vivo expanded human NK cells express activating receptors that mediate cytotoxicity of allogeneic and autologous cancer cell lines by direct recognition and antibody directed cellular cytotoxicity

    Directory of Open Access Journals (Sweden)

    Campana Dario

    2010-10-01

    Full Text Available Abstract Background The possibility that autologous NK cells could serve as an effective treatment modality for solid tumors has long been considered. However, implementation is hampered by (i the small number of NK cells in peripheral blood, (ii the difficulties associated with large-scale production of GMP compliant cytolytic NK cells, (iii the need to activate the NK cells in order to induce NK cell mediated killing and (iv the constraints imposed by autologous inhibitory receptor-ligand interactions. To address these issues, we determined (i if large numbers of NK cells could be expanded from PBMC and GMP compliant cell fractions derived by elutriation, (ii their ability to kill allogeneic and autologous tumor targets by direct cytotoxitiy and by antibody-mediated cellular cytotoxicity and (iii defined NK cell specific receptor-ligand interactions that mediate tumor target cell killing. Methods Human NK cells were expanded during 14 days. Expansion efficiency, NK receptor repertoire before and after expansion, expression of NK specific ligands, cytolytic activity against allogeneic and autologous tumor targets, with and without the addition of chimeric EGFR monoclonal antibody, were investigated. Results Cell expansion shifted the NK cell receptor repertoire towards activation and resulted in cytotoxicity against various allogeneic tumor cell lines and autologous gastric cancer cells, while sparing normal PBMC. Blocking studies confirmed that autologous cytotoxicity is established through multiple activating receptor-ligand interactions. Importantly, expanded NK cells also mediated ADCC in an autologous and allogeneic setting by antibodies that are currently being used to treat patients with select solid tumors. Conclusion These data demonstrate that large numbers of cytolytic NK cells can be generated from PBMC and lymphocyte-enriched fractions obtained by GMP compliant counter current elutriation from PBMC, establishing the preclinical

  16. Synthesis, characterization, and cytotoxicity of the plasmid EGFP-p53 loaded on pullulan–spermine magnetic nanoparticles

    Energy Technology Data Exchange (ETDEWEB)

    Eslaminejad, Touba, E-mail: tslaminejad@yahoo.com [Pharmaceutics Research Centre, Institute of Neuropharmacology, Kerman University of Medical Sciences, Kerman (Iran, Islamic Republic of); Nematollahi-Mahani, Seyed Noureddin, E-mail: nnematollahi@kmu.ac.ir [Department of Anatomy, Afzalipour School of Medicine, Kerman University of Medical Sciences, Kerman (Iran, Islamic Republic of); Neuroscience Research Centre, Institute of Neuropharmacology, Kerman University of Medical Sciences, Kerman (Iran, Islamic Republic of); Afzal Research Institute, Kerman (Iran, Islamic Republic of); Ansari, Mehdi, E-mail: mansari@kmu.ac.ir [Pharmaceutics Research Centre, Institute of Neuropharmacology, Kerman University of Medical Sciences, Kerman (Iran, Islamic Republic of); Pharmaceutics Research Centre, Faculty of Pharmacy, Kerman University of Medical Sciences, Kerman (Iran, Islamic Republic of)

    2016-03-15

    Magnetic nanoparticles have been used as effective vehicles for the targeted delivery of therapeutic agents that can be controlled in their concentration and distribution to a desired part of the body by using externally driven magnets. This study focuses on the synthesis, characterization, and functionalization of pullulan–spermine (PS) magnetic nanoparticles for medical applications. Magnetite nanopowder was produced by thermal decomposition of goethite (FeOOH) in oleic acid and 1-octadecene; pullulan–spermine was deposited on the magnetite nanoparticles in the form of pullulan–spermine clusters. EGFP-p53 plasmid was loaded on functionalized iron oleate to transfer into cells. Synthesized nanoparticles were characterized by Fourier transform infrared spectroscopy (FTIR), dynamic light scattering (DLS), vibrating sample magnetometry (VSM), and transmission electron microscopy (TEM). The encapsulation efficiency and drug loading efficiency of the nanocomplexes were tested. FTIR studies showed the presence of oleic acid and 1-octadecene in the iron oleate nanopowder and verified the interaction between spermine and pullulan. The characteristic bands of PS in the spectrum of the pullulan–spermine-coated iron oleate (PSCFO) confirmed that PS covered the surface of the iron oleate particles. TEM studies showed the average size of the iron oleate nanopowder, the PSCFO, and the plasmid-carrying PSCFO (PSCFO/pEGFP-p53) to be 34±12 nm, 100±50 nm and 172±3 nm, respectively. Magnetic measurements revealed that magnetic saturation of the PSCFO was lower in comparison with the iron oleate nanopowder due to the presence of organic compounds in the former. In cytotoxicity tests performed using U87 cells as glioblastoma cells, a 92% survival rate was observed at 50 µg/µl of the plasmid-carrying PSCFO, with an IC{sub 50} value of 189 µg/µl. - Highlights: • Magnetite nanopowder was produced by thermal decomposition method. • TEM studies showed the average size of

  17. Synthesis, characterization, and cytotoxicity of the plasmid EGFP-p53 loaded on pullulan–spermine magnetic nanoparticles

    International Nuclear Information System (INIS)

    Eslaminejad, Touba; Nematollahi-Mahani, Seyed Noureddin; Ansari, Mehdi

    2016-01-01

    Magnetic nanoparticles have been used as effective vehicles for the targeted delivery of therapeutic agents that can be controlled in their concentration and distribution to a desired part of the body by using externally driven magnets. This study focuses on the synthesis, characterization, and functionalization of pullulan–spermine (PS) magnetic nanoparticles for medical applications. Magnetite nanopowder was produced by thermal decomposition of goethite (FeOOH) in oleic acid and 1-octadecene; pullulan–spermine was deposited on the magnetite nanoparticles in the form of pullulan–spermine clusters. EGFP-p53 plasmid was loaded on functionalized iron oleate to transfer into cells. Synthesized nanoparticles were characterized by Fourier transform infrared spectroscopy (FTIR), dynamic light scattering (DLS), vibrating sample magnetometry (VSM), and transmission electron microscopy (TEM). The encapsulation efficiency and drug loading efficiency of the nanocomplexes were tested. FTIR studies showed the presence of oleic acid and 1-octadecene in the iron oleate nanopowder and verified the interaction between spermine and pullulan. The characteristic bands of PS in the spectrum of the pullulan–spermine-coated iron oleate (PSCFO) confirmed that PS covered the surface of the iron oleate particles. TEM studies showed the average size of the iron oleate nanopowder, the PSCFO, and the plasmid-carrying PSCFO (PSCFO/pEGFP-p53) to be 34±12 nm, 100±50 nm and 172±3 nm, respectively. Magnetic measurements revealed that magnetic saturation of the PSCFO was lower in comparison with the iron oleate nanopowder due to the presence of organic compounds in the former. In cytotoxicity tests performed using U87 cells as glioblastoma cells, a 92% survival rate was observed at 50 µg/µl of the plasmid-carrying PSCFO, with an IC 50 value of 189 µg/µl. - Highlights: • Magnetite nanopowder was produced by thermal decomposition method. • TEM studies showed the average size of the

  18. Biocompatible transferrin-conjugated sodium hexametaphosphate-stabilized gold nanoparticles: synthesis, characterization, cytotoxicity and cellular uptake

    International Nuclear Information System (INIS)

    Parab, Harshala J; Huang, Jing-Hong; Liu, Ru-Shi; Lai, Tsung-Ching; Jan, Yi-Hua; Wang, Jui-Ling; Hsiao, Michael; Chen, Chung-Hsuan; Hwu, Yeu-Kuang; Tsai, Din Ping; Chuang, Shih-Yi; Pang, Jong-Hwei S

    2011-01-01

    The feasibility of using gold nanoparticles (AuNPs) for biomedical applications has led to considerable interest in the development of novel synthetic protocols and surface modification strategies for AuNPs to produce biocompatible molecular probes. This investigation is, to our knowledge, the first to elucidate the synthesis and characterization of sodium hexametaphosphate (HMP)-stabilized gold nanoparticles (Au-HMP) in an aqueous medium. The role of HMP, a food additive, as a polymeric stabilizing and protecting agent for AuNPs is elucidated. The surface modification of Au-HMP nanoparticles was carried out using polyethylene glycol and transferrin to produce molecular probes for possible clinical applications. In vitro cell viability studies performed using as-synthesized Au-HMP nanoparticles and their surface-modified counterparts reveal the biocompatibility of the nanoparticles. The transferrin-conjugated nanoparticles have significantly higher cellular uptake in J5 cells (liver cancer cells) than control cells (oral mucosa fibroblast cells), as determined by inductively coupled plasma mass spectrometry. This study demonstrates the possibility of using an inexpensive and non-toxic food additive, HMP, as a stabilizer in the large-scale generation of biocompatible and monodispersed AuNPs, which may have future diagnostic and therapeutic applications.

  19. Biocompatible transferrin-conjugated sodium hexametaphosphate-stabilized gold nanoparticles: synthesis, characterization, cytotoxicity and cellular uptake

    Energy Technology Data Exchange (ETDEWEB)

    Parab, Harshala J; Huang, Jing-Hong; Liu, Ru-Shi [Department of Chemistry, National Taiwan University, Taipei 106, Taiwan (China); Lai, Tsung-Ching; Jan, Yi-Hua; Wang, Jui-Ling; Hsiao, Michael; Chen, Chung-Hsuan [Genomics Research Center, Academia Sinica, Taipei 115, Taiwan (China); Hwu, Yeu-Kuang [Institute of Physics, Academia Sinica, Taipei 115, Taiwan (China); Tsai, Din Ping [Department of Physics, National Taiwan University, Taipei 106, Taiwan (China); Chuang, Shih-Yi; Pang, Jong-Hwei S, E-mail: rsliu@ntu.edu.tw, E-mail: mhsiao@gate.sinica.edu.tw [Graduate Institute of Clinical Medical Sciences, Chang Gung University, Tao-Yuan, Taiwan (China)

    2011-09-30

    The feasibility of using gold nanoparticles (AuNPs) for biomedical applications has led to considerable interest in the development of novel synthetic protocols and surface modification strategies for AuNPs to produce biocompatible molecular probes. This investigation is, to our knowledge, the first to elucidate the synthesis and characterization of sodium hexametaphosphate (HMP)-stabilized gold nanoparticles (Au-HMP) in an aqueous medium. The role of HMP, a food additive, as a polymeric stabilizing and protecting agent for AuNPs is elucidated. The surface modification of Au-HMP nanoparticles was carried out using polyethylene glycol and transferrin to produce molecular probes for possible clinical applications. In vitro cell viability studies performed using as-synthesized Au-HMP nanoparticles and their surface-modified counterparts reveal the biocompatibility of the nanoparticles. The transferrin-conjugated nanoparticles have significantly higher cellular uptake in J5 cells (liver cancer cells) than control cells (oral mucosa fibroblast cells), as determined by inductively coupled plasma mass spectrometry. This study demonstrates the possibility of using an inexpensive and non-toxic food additive, HMP, as a stabilizer in the large-scale generation of biocompatible and monodispersed AuNPs, which may have future diagnostic and therapeutic applications.

  20. Cytotoxic Activities, SAR and Anti-Invasion Effects of Butylphthalide Derivatives on Human Hepatocellular Carcinoma SMMC7721 Cells

    Directory of Open Access Journals (Sweden)

    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.

  1. 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.

  2. 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)

  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. 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.

  5. 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.

  6. Anti-Leishmania and cytotoxic activities of perillaldehyde epoxide synthetic positional isomers.

    Science.gov (United States)

    Keesen, Tatjana Souza Lima; da Silva, Larisse Virgolino; da Câmara Rocha, Juliana; Andrade, Luciana Nalone; Lima, Tamires Cardoso; de Sousa, Damião Pergentino

    2018-03-13

    Leishmaniasis belongs to a complex of zoonotic disease caused by protozoa of the genus Leishmania and is considered a major public health problem. Several essential oil chemical components have inhibitory effect against protozoa, including Leishmania donovani. Thus, the aim of this study was to evaluate for the first time the anti-Leishmania activity of two p-menthane monoterpene isomers (EPER-1: perillaldehyde 1,2-epoxide and EPER-2: perillaldehyde 8,9-epoxide) against L. donovani promastigotes as well as evaluating cytotoxic effect on mononuclear peripheral blood cells. Results of anti-Leishmania assay revealed that EPER-2 (IC 50  = 3.8 μg.mL -1 ) was 16-fold more potent than its isomer EPER-1 (IC 50  = 64.6 μg.mL -1 ). In contrast to PBMC cells, EPER-2 was not cytotoxic (IC 50  > 400 μg.mL -1 ) when compared to positive control. These data suggest that the disposition of epoxide group into the p-menthane skeleton affects the anti-Leishmania activity, being that the presence of the exocyclic epoxide group considerably increased potency. Thus, it was possible to observe that the location of the epoxide group into the p-menthane skeleton resulted in different potencies.

  7. Chemical Composition, Larvicidal and Cytotoxic Activities of the Essential Oils from two Bauhinia Species

    Directory of Open Access Journals (Sweden)

    Leôncio M. de Sousa

    2016-05-01

    Full Text Available The essential oils obtained by hydrodistilation from leaves of Bauhinia pulchella Benth. and Bauhinia ungulata L. were analysed by GC-FID and GC-MS. The major components of B. pulchella essential oil were identified as a -pinene (23.9%, caryophyllene oxide (22.4% and b -pinene (12.2%, while in the B. ungulata essential oil were caryophyllene oxide (23.0%, (E-caryophyllene (14.5% and a -copaene (7.2%. The essential oils were subsequently evaluated for their larvicidal and cytotoxic activities. Larval bioassay against Aedes aegypti of B. pulchella and B. ungulata essential oils showed LC 50 values of 105.9 ± 1.5 and 75.1 ± 2.8 m g/mL, respectively. The essential oils were evaluated against four human cancer cells lines: HL-60 (pro-myelocytic leukemia, MCF-7 (breast adenocarcinoma, NCI-H292 (lung carcinoma and HEP-2 ( cervical adenocarcinoma, showing IC 50 values in the range of 9.9 to 53.1 m g/mL. This is the first report on chemical composition of essential from leaves of B. pulchella and on larvicidal and cytotoxic activities of the essential oils.

  8. Cytotoxic activity of vitamins K1, K2 and K3 against human oral tumor cell lines.

    Science.gov (United States)

    Okayasu, H; Ishihara, M; Satoh, K; Sakagami, H

    2001-01-01

    Vitamin K1, K2 and K3 were compared for their cytotoxic activity, radical generation and O2- scavenging activity. Among these compounds, vitamin K3 showed the highest cytotoxic activity against human oral tumor cell lines (HSC-2, HSG), human promyelocytic leukemic cell line (HL-60) and human gingival fibroblast (HGF). Vitamin K3 induced internucleosomal DNA fragmentation in HL-60 cells, but not in HSC-2 or HSG cells. The cytotoxic activity of vitamins K2 and K1 was one and two orders lower, respectively, than K3. Vitamin K2, but not vitamin K3, showed tumor-specific cytotoxic action. ESR spectroscopy showed that only vitamin K3 produced radical(s) under alkaline condition and most potently enhanced the radical intensity of sodium ascorbate and scavenged O2- (generated by hypoxanthine-xanthine oxidase reaction system); vitamin K2 was much less active whereas vitamin K1 was inactive. These data suggest that the cytotoxic activity of vitamin K3 is generated by radical-mediated oxidation mechanism and that this vitamin has two opposing actions (that is, antioxidant and prooxidant), depending on the experimental conditions.

  9. Resistance of Pseudomonas aeruginosa isolates to hydrogel contact lens disinfection correlates with cytotoxic activity.

    Science.gov (United States)

    Lakkis, C; Fleiszig, S M

    2001-04-01

    One of the most common pathogens in infection of hydrogel contact lens wearers is Pseudomonas aeruginosa, which can gain access to the eye via contamination of the lens, lens case, and lens care solutions. Only one strain per species is used in current regulatory testing for the marketing of chemical contact lens disinfectants. The aim of this study was to determine whether P. aeruginosa strains vary in their susceptibility to hydrogel contact lens disinfectants. A method for rapidly screening bacterial susceptibility to contact lens disinfectants was developed, based on measurement of the MIC. The susceptibility of 35 P. aeruginosa isolates to two chemical disinfectants was found to vary among strains. MICs ranged from 6.25 to 100% for both disinfectants at 37 degrees C, and a number of strains were not inhibited by a 100% disinfectant concentration in the lens case environment at room temperature (22 degrees C). Resistance to disinfection appeared to be an inherent rather than acquired trait, since some resistant strains had been isolated prior to the introduction of the disinfectants and some susceptible P. aeruginosa strains could not be made more resistant by repeated disinfectant exposure. A number of P. aeruginosa strains which were comparatively more resistant to short-term disinfectant exposure also demonstrated the ability to grow to levels above the initial inoculum in one chemical disinfectant after long-term (24 to 48 h) disinfectant exposure. Resistance was correlated with acute cytotoxic activity toward corneal epithelial cells and with exsA, which encodes a protein that regulates cytotoxicity via a complex type III secretion system. These results suggest that chemical disinfection solutions may select for contamination with cytotoxic strains. Further investigation of the mechanisms and factors responsible for resistance may also lead to strategies for reducing adverse responses to contact lens wear.

  10. 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.

  11. Unsymmetrical Mesoporphyrinic Complexes of Copper (II and Zinc (II. Microwave-Assisted Synthesis, Spectral Characterization and Cytotoxicity Evaluation

    Directory of Open Access Journals (Sweden)

    Rica Boscencu

    2011-06-01

    Full Text Available New unsymmetrical mesoporphyrinic complexes, namely 5-(4-hydroxyphenyl-10,15,20–tris-(4-carboxymethylphenyl–21,23-Zn(II-porphine and 5-(4-hydroxyphenyl-10,15,20–tris-(4-carboxymethylphenyl–21,23-Cu(II-porphine, were synthesized using a microwave irradiation method. The structures of the porphyrinic complexes were confirmed using FT-IR, UV–Vis, EPR and NMR spectral data. The spectral absorption and emission properties of the porphyrinic complexes were studied in organic solvents of different polarities and the influence of solvent polarity on the wavelengths of the absorbance and fluorescence band maxima is described. The cytotoxicity evaluation of the porphyrinic complexes was performed on human colon adenocarcinoma cell line HT29 for different doses and incubation times. The obtained result indicates a lack of or low toxicity for both compounds, thus recommending them for further testing in light activation protocols.

  12. Isolation, Purification, and Characterization of Five Active Diketopiperazine Derivatives from Endophytic Streptomyces SUK 25 with Antimicrobial and Cytotoxic Activities.

    Science.gov (United States)

    Alshaibani, Muhanna; Zin, Noraziah; Jalil, Juriyati; Sidik, Nik; Ahmad, Siti Junaidah; Kamal, Nurkhalida; Edrada-Ebel, Ruangelie

    2017-07-28

    In our search for new sources of bioactive secondary metabolites from Streptomyces sp., the ethyl acetate extracts from endophytic Streptomyces SUK 25 afforded five active diketopiperazine (DKP) compounds. The aim of this study was to characterize the bioactive compounds isolated from endophytic Streptomyces SUK 25 and evaluate their bioactivity against multiple drug resistance (MDR) bacteria such as Enterococcus raffinosus, Staphylococcus aureus, Klebsiella pneumoniae, Acinetobacter baumanii, Pseudomonas aeruginosa, and Enterobacter spp., and their cytotoxic activities against the human hepatoma (HepaRG) cell line. The production of secondary metabolites by this strain was optimized through Thornton's medium. Isolation, purification, and identification of the bioactive compounds were carried out using high-performance liquid chromatography, high-resolution mass liquid chromatography-mass spectrometry, Fourier transform infrared spectroscopy, and nuclear magnetic resonance, and cryopreserved HepaRG cells were selected to test the cytotoxicity. The results showed that endophytic Streptomyces SUK 25 produces four active DKP compounds and an acetamide derivative, which were elucidated as cyclo -( L -Val- L -Pro), cyclo -( L -Leu- L -Pro), cyclo -( L -Phe- L -Pro), cyclo -( L -Val- L -Phe), and N -(7-hydroxy-6-methyl-octyl)-acetamide. These active compounds exhibited activity against methicillin-resistant S. aureus ATCC 43300 and Enterococcus raffinosus , with low toxicity against human hepatoma HepaRG cells. Endophytic Streptomyces SUK 25 has the ability to produce DKP derivatives biologically active against some MDR bacteria with relatively low toxicity against HepaRG cells line.

  13. 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.

  14. Silver nanoparticles with antimicrobial activities against Streptococcus mutans and their cytotoxic effect

    International Nuclear Information System (INIS)

    Pérez-Díaz, Mario Alberto; Boegli, Laura; James, Garth; Velasquillo, Cristina; Sánchez-Sánchez, Roberto; Martínez-Martínez, Rita-Elizabeth; Martínez-Castañón, Gabriel Alejandro; Martinez-Gutierrez, Fidel

    2015-01-01

    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

  15. Flavonoids and Ellagitannins Characterization, Antioxidant and Cytotoxic Activities of Phyllanthus acuminatus Vahl

    Directory of Open Access Journals (Sweden)

    Mirtha Navarro

    2017-12-01

    Full Text Available The phenolic composition of leaves from Phyllanthus acuminatus L., a plant commonly used in Costa Rica as traditional medicine, was studied using UPLC-ESI-MS on an enriched phenolic extract. A total of 20 phenolic compounds were identified, comprising eight flavonoids (two flavanones—pinocembrin isomers and six derivatives from apigenin, chrysin, quercetin, and kaempferol; seven ellagitannins, two flavan-3-ols (prodelphinidin B dimer and (epigallocatechin; and three phenolic acids (ellagic acid, trimethylellagic acid, and ferulic acid. All of these compounds are reported for the first time in P. acuminatus, while previously reported in the genus Phyllanthus. Antioxidant evaluation was performed for P. acuminatus phenolic extract obtaining DPPH results with a remarkably low IC50 value of 0.15 μg/mL. Also, cytotoxicity on gastric AGS and colon SW20 adenocarcinoma cell lines was evaluated, and highly promising results were obtained, with IC50 values of 11.3 μg/mL and 10.5 μg/mL, respectively. Furthermore, selectivity index values obtained when comparing cytotoxicity on normal Vero cells was SI > 20 for both cancer cell lines, indicating a particularly high selectivity. Additionally, Justicidin B, a metabolite extensively studied for its antitumoral activity, was isolated from a non-polar extract of P. acuminatus, and comparatively evaluated for both bioactivities. The DPPH value obtained for Justicidin B was moderate (IC50 = 14.28 μg/mL, while cytotoxicity values for both AGS (IC50 = 19.5 μg/mL and SW620 (IC50 = 24.8 μg/mL cell lines, as well as selectivity when compared with normal Vero cells (SI = 5.4 and 4.2 respectively, was good, but lower than P. acuminatus extract. These preliminary results suggest that P. acuminatus enriched phenolic extract containing flavonoids, ellagitannins, flavan-3-ols, and phenolic acids, reported for the first time in this plant, could be of interest for further cancer cytotoxicity studies to elucidate

  16. One-pot synthesis and cytotoxicity studies of new Mannich base derivatives of polyether antibiotic--lasalocid acid.

    Science.gov (United States)

    Huczyński, Adam; Rutkowski, Jacek; Borowicz, Izabela; Wietrzyk, Joanna; Maj, Ewa; Brzezinski, Bogumil

    2013-09-15

    Seven Mannich base derivatives of polyether antibiotic Lasalocid acid (2a-2g) were synthesized and screened for their antiproliferative activity against various human cancer cell lines. A novel chemoselective one-pot synthesis of these Mannich bases was developed. Compounds 2a-2c and 2g with sterically smaller dialkylamine substituent, displayed potent antiproliferative activity (IC50: 3.2-7.3 μM), and demonstrated higher than twofold selectivity for specific type of cancer. The nature of Mannich base substituent on C-2 atom at the aromatic ring may be critical in the search for selectivity towards a particular cancer cell. Copyright © 2013 Elsevier Ltd. All rights reserved.

  17. Green synthesis of NiO nanoparticles using Aegle marmelos leaf extract for the evaluation of in-vitro cytotoxicity, antibacterial and photocatalytic properties.

    Science.gov (United States)

    Angel Ezhilarasi, A; Judith Vijaya, J; Kaviyarasu, K; John Kennedy, L; Ramalingam, R Jothi; Al-Lohedan, Hamad A

    2018-03-01

    In the present study, we report the green synthesis of NiO nanoparticles using Aegle marmelos as a fuel and this method is ecofriendly and cost effective. The plant Aegle marmelos is used in the field of pharmaceuticals to cure diseases like chronic diarrhea, peptic ulcers and dysentery in India for nearly 5 centuries. The as-prepared nanoparticles were confirmed as pure face centered cubic phase and single crystalline in nature by XRD. The formation of agglomerated spherical nanoparticles was shown by HR-SEM and HR-TEM images. The particle size calculated from HR-SEM was in the range 8-10 nm and it matches with the average crystallite size calculated from the XRD pattern. NiO shows intense emission peaks at 363 and 412 nm in its PL spectra. The band gap of 3.5 eV is observed from DRS studies and the formation of pure NiO is confirmed by FT-IR spectra. The as-prepared NiO nanoparticles show super paramagnetic behavior, when magnetization studies are carried out. It is then evaluated for cytotoxic activity towards A549 cell culture, antibacterial activity and photocatalytic degradation (PCD) of 4‑chlorophenol (4‑CP), which is known as the endocrine disrupting chemical (EDC). From the results, it is found that the cell viability of A549 cells was effectively reduced and it showed better antibacterial activity towards gram positive bacterial strains. It is also proved to be an efficient and stable photocatalyst towards the degradation of 4‑CP. Copyright © 2018 Elsevier B.V. All rights reserved.

  18. 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.

  19. Cytotoxicity, Bactericidal, and Antioxidant Activity of Sodium Alginate Hydrosols Treated with Direct Electric Current

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    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.

  20. 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.

  1. Antioxidant, Cytotoxic, and Antiproliferative Activities and Total Polyphenol Contents of the Extracts of Geissospermum reticulatum Bark

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    Joanna J. Sajkowska-Kozielewicz

    2016-01-01

    Full Text Available Geissospermum species are medically important plants due to their health-promoting effects. The objective of this study was to determine the antioxidant ability and antiproliferative and cytotoxic effects of infusions, tinctures, and ethanolic extracts of Geissospermum reticulatum barks in relation to the contents of total phenolics and flavonoids. Seven samples of barks were collected in various regions of Peruvian Amazonia. We found that the amount of total phenolics in the studied products varied from 212.40 ± 0.69 to 1253.92 ± 11.20 mg GAE/kg. In our study there is a correlation (R2=0.7947 between the results of antioxidants assays: FRAP and ORAC for tinctures, infusions, and ethanolic extracts of G. reticulatum barks. We have also observed antiproliferative activities of the ethanolic extracts on normal T-cells. These extracts have caused death on malignant cell lines (THP-1 and HL-60 and this data correlates well with their antioxidant capacity measured by ORAC method. Interestingly, the highest concentration of the ethanolic extract was not toxic in the zebrafish embryo developmental assay. Our results indicate that G. reticulatum is rich in antioxidants and have cytotoxic and antiproliferative properties. The data suggests potential immunosuppressive role of the extracts. This is the first study presenting the results of chemical and biological analysis of multiple preparations from G. reticulatum.

  2. 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

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

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    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.

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

    Directory of Open Access Journals (Sweden)

    Koffi Koba

    2009-03-01

    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 myrc¨ne (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 toxicity of 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 synergy by neral and geranial in the overall toxicity showed by the citratus oil sample tested in this work.

  5. Trypanocidal and cytotoxic activities of essential oils from medicinal plants of Northeast of Brazil.

    Science.gov (United States)

    Borges, Andrezza Raposo; Aires, Juliana Ramos de Albuquerque; Higino, Taciana Mirely Maciel; de Medeiros, Maria das Graças Freire; Citó, Antonia Maria das Graças Lopes; Lopes, José Arimatéia Dantas; de Figueiredo, Regina Celia Bressan Queiroz

    2012-10-01

    Chagas disease, caused by Trypanosoma cruzi, is an important cause of mortality and morbidity in Latin America. There are no vaccines available, the chemotherapy used to treat this illness has serious side effects and its efficacy on the chronic phase of disease is still a matter of debate. In a search for alternative treatment for Chagas disease, essential oils extracted from traditional medicinal plants Lippia sidoides, Lippia origanoides, Chenopodium ambrosioides, Ocimum gratissimum, Justicia pectorales and Vitex agnus-castus were investigated in vitro for trypanocidal and cytotoxic activities. Essential Oils were extracted by hydrodistillation and submitted to chemical analysis by gas chromatography/mass spectrometry. The concentration of essential oils necessary to inhibit 50% of the epimastigotes or amastigotes growth (IC(50)) and to kill 50% of trypomastigote forms (LC(50)) was estimated. The most prevalent chemical constituents of these essential oils were monoterpenes and sesquiterpenes. All essential oils tested demonstrated an inhibitory effect on the parasite growth and survival. L. sidoides and L. origanoides essential oils were the most effective against trypomastigote and amastigote forms respectively. No significant cytotoxic effects were observed in mouse peritoneal macrophages incubated with essential oils which were more selective against the parasites than mammalian cells. Taken together, our results point towards the use of these essential oils as potential chemotherapeutic agent against T. cruzi. Copyright © 2012 Elsevier Inc. All rights reserved.

  6. Structure and cytotoxic activity of ulvan extracted from green seaweed Ulva lactuca.

    Science.gov (United States)

    Thanh, Thi Thu Thuy; Quach, Thi Minh Thu; Nguyen, Thi Nu; Vu Luong, Dang; Bui, Minh Ly; Tran, Thi Thanh Van

    2016-12-01

    The structure of an ulvan obtained by water extraction from green seaweed Ulva lactuca was elucidated by using IR, NMR, SEC-MALL and ESIMS methods. The ulvan was also evaluated for its cytotoxic effects on three human cancer cell lines. The results showed that the ulvan was composed of rhamnose, galactose, xylose, manose, glucose (with a mole ratio of Rha: Gal: Xyl: Man: Glu equal to 1: 0.03: 0.07: 0.01: 0.06), uronic acid (21.5%) and sulfate content (18.9%) with a molecular weight of 347000. This ulvan mainly consists of disaccharide [→4)-β-d-GlcA-(1→4)-α-l-Rha3S-(1→] and other minor disaccharide β-GlcA-(1→2)-α-Xyl and β-GlcA-(→2)-α-Rha. The ulvan showed a significant cytotoxic activity against hepatocellular carcinoma (IC 50 29.67±2.87μg/ml), human breast cancer (IC 50 25.09±1.36μg/ml), and cervical cancer (IC 50 36.33±3.84μg/ml). Copyright © 2016 Elsevier B.V. All rights reserved.

  7. Alkaloids from Prosopis juliflora leaves induce glial activation, cytotoxicity and stimulate NO production.

    Science.gov (United States)

    Silva, A M M; Silva, A R; Pinheiro, A M; Freitas, S R V B; Silva, V D A; Souza, C S; Hughes, J B; El-Bachá, R S; Costa, M F D; Velozo, E S; Tardy, M; Costa, S L

    2007-04-01

    Prosopis juliflora is used for feeding cattle and humans. Intoxication with the plant has been reported, and is characterized by neuromuscular alterations and gliosis. Total alkaloidal extract (TAE) was obtained using acid/basic-modified extraction and was fractionated. TAE and seven alkaloidal fractions, at concentrations ranging 0.03-30 microg/ml, were tested for 24h on astrocyte primary cultures derived from the cortex of newborn Wistar rats. The MTT test and the measure of LDH activity on the culture medium, revealed that TAE and fractions F29/30, F31/33, F32 and F34/35 were cytotoxic to astrocytes. The EC(50) values for the most toxic compounds, TAE, F31/33 and F32 were 2.87 2.82 and 3.01 microg/ml, respectively. Morphological changes and glial cells activation were investigated through Rosenfeld's staining, by immunocytochemistry for the protein OX-42, specific of activated microglia, by immunocytochemistry and western immunoblot for GFAP, the marker of reactive and mature astrocytes, and by the production of nitric oxide (NO). We observed that astrocytes exposed to 3 microg/ml TAE, F29/30 or F31/33 developed compact cell body with many processes overexpressing GFAP. Treatment with 30 microg/ml TAE and fractions, induced cytotoxicity characterized by a strong cell body contraction, very thin and long processes and condensed chromatin. We also observed that when compared with the control (+/-1.34%), the proportion of OX-42 positive cells was increased in cultures treated with 30 microg/ml TAE or F29/30, F31/33, F32 and F34/35, with values raging from 7.27% to 28.74%. Moreover, incubation with 3 microg/ml F32, 30 microg/ml TAE, F29/30, F31/33 or F34/35 induced accumulation of nitrite in culture medium indicating induction of NO production. Taken together these results show that TAE and fractionated alkaloids from P. juliflora act directly on glial cells, inducing activation and/or cytotoxicity, stimulating NO production, and may have an impact on neuronal

  8. Composition and cytotoxic and antioxidant activities of the oil of Piper aequale Vahl.

    Science.gov (United States)

    da Silva, Joyce Kelly R; Pinto, Laine C; Burbano, Rommel M R; Montenegro, Raquel C; Andrade, Eloísa Helena A; Maia, José Guilherme S

    2016-10-07

    Piper aequale Vahl is a small shrub that grows in the shadow of large trees in the Carajás National Forest, Municipality of Parauapebas, Para state, Brazil. The local people have used the plant against rheumatism and inflammation. The essential oil of the aerial parts was extracted and analyzed by GC and GC-MS. The MTT colorimetric assay was used to measuring the cytotoxic activity of the oil against human cancer lines. The determination of antioxidant activity of the oil was conducted by DPPH radical scavenging assay. The main constituents were δ-elemene (18.92 %), β-pinene (15.56 %), α-pinene (12.57 %), cubebol (7.20 %), β-atlantol (5.87 %), and bicyclogermacrene (5.51 %), totalizing 65.63 % of the oil. The oil displayed a strong in vitro cytotoxic activity against the human cancer cell lines HCT-116 (colon) and ACP03 (gastric) with IC 50 values of 8.69 μg/ml and 1.54 μg/ml, respectively. The oil has induced the apoptosis in a gastric cancer cells in all tested concentration (0.75-3.0 μg/ml), after 72 h of treatment, when compared to negative control (p < 0.001). Also, the oil showed a significant antioxidant activity (280.9 ± 22.2 mg TE/ml), when analyzed as Trolox equivalent, and a weak acetylcholinesterase inhibition, with a detection limit of 100 ng, when compared to the physostigmine standard (1.0 ng). The higher cell growth inhibition induced by the oil of P. aequale is probably due to its primary terpene compounds, which were previously reported in the proliferation inhibition, in stimulation of apoptosis and induction of cell cycle arrest in malignant cells.

  9. 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.

  10. 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.

  11. 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.

  12. Novel 3-(aminomethyl)naphthoquinone mannich base-platinum(IV) complexes: synthesis, characterization, electrochemical and cytotoxic studies

    Energy Technology Data Exchange (ETDEWEB)

    Silva, Gustavo B. da; Neves, Amanda P.; Vargas, Maria D., E-mail: mdvargas@vm.uff.br [Universidade Federal Fluminense (UFF), Niteroi, RJ (Brazil). Instituto de Quimica; Alves, Wagner A. [Universidade Federal Rural do Rio de Janeiro (UFRRJ), Seropedica, RJ (Brazil). Departamento de Quimica; Marinho-Filho, Jose D.B.; Pessoa, Claudia; Moraes, Manoel O.; Costa-Lotufo, Leticia V. [Universidade Federal do Ceara (UFCE), Fortaleza, CE (Brazil). Centro de Ciencias da Saude. Departamento de Fisiologia e Farmacologia

    2013-04-15

    Three novel platinum(IV) complexes cis,cis,trans-[Pt(HL1-3)Cl{sub 2}(OH){sub 2}] 1b-3b(HL = 2-hydroxy-3-[(R{sup 1} -amino)(pyridin-2-yl)methyl]-1,4-naphthoquinone, R{sup 1} = n-butyl, HL1; n-heptyl, HL2 and n-decyl, HL3) have been obtained from the oxidation of the respective precursors cis-[Pt(HL1-3)Cl{sub 2}] 1a-3a. Cyclic voltammetry studies of 1b-3b in MeCN showed the quasi reversible naphthoquinonate (NQO{sup -}, i.e., L{sup -}) redox process and irreversible process attributed to the reduction of the Pt{sup 4+}/Pt{sup 2+} pair, at potentials about 400 mV less negative than for the cisplatin precursor cis,cis,trans-[Pt(NH{sub 3}){sub 2}Cl{sub 2}(OH){sub 2}]. Hydrogen bond interaction between the naphthoquinone 2-hydroxyl group and an axially coordinated hydroxide ligand in 1b-3b has been proposed to favor the Pt{sup 4+}/Pt{sup 2+} reduction. The cytotoxicity studies against four human cancer cell lines have shown that in general the platinum(IV) and platinum(II)derivatives exhibit the same cytotoxic profile and are all more active than cisplatin. The lowest in vitro IC{sub 50} values have been observed for 2b-3b, which bear ligands with the largest R{sup 1} groups (HL2-HL3) being the most lipophilic. Furthermore similar IC{sub 50} values for platinum(II) and platinum(IV) complexes of the same ligands have been associated with rapid in vitro reduction of the latter complexes to afford 1a-3a. (author)

  13. Novel 3-(aminomethyl)naphthoquinone mannich base-platinum(IV) complexes: synthesis, characterization, electrochemical and cytotoxic studies

    International Nuclear Information System (INIS)

    Silva, Gustavo B. da; Neves, Amanda P.; Vargas, Maria D.; Alves, Wagner A.; Marinho-Filho, Jose D.B.; Pessoa, Claudia; Moraes, Manoel O.; Costa-Lotufo, Leticia V.

    2013-01-01

    Three novel platinum(IV) complexes cis,cis,trans-[Pt(HL1-3)Cl 2 (OH) 2 ] 1b-3b(HL = 2-hydroxy-3-[(R 1 -amino)(pyridin-2-yl)methyl]-1,4-naphthoquinone, R 1 = n-butyl, HL1; n-heptyl, HL2 and n-decyl, HL3) have been obtained from the oxidation of the respective precursors cis-[Pt(HL1-3)Cl 2 ] 1a-3a. Cyclic voltammetry studies of 1b-3b in MeCN showed the quasi reversible naphthoquinonate (NQO - , i.e., L - ) redox process and irreversible process attributed to the reduction of the Pt 4+ /Pt 2+ pair, at potentials about 400 mV less negative than for the cisplatin precursor cis,cis,trans-[Pt(NH 3 ) 2 Cl 2 (OH) 2 ]. Hydrogen bond interaction between the naphthoquinone 2-hydroxyl group and an axially coordinated hydroxide ligand in 1b-3b has been proposed to favor the Pt 4+ /Pt 2+ reduction. The cytotoxicity studies against four human cancer cell lines have shown that in general the platinum(IV) and platinum(II)derivatives exhibit the same cytotoxic profile and are all more active than cisplatin. The lowest in vitro IC 50 values have been observed for 2b-3b, which bear ligands with the largest R 1 groups (HL2-HL3) being the most lipophilic. Furthermore similar IC 50 values for platinum(II) and platinum(IV) complexes of the same ligands have been associated with rapid in vitro reduction of the latter complexes to afford 1a-3a. (author)

  14. Receptor-mediated photo-cytotoxicity: synthesis of a photoactivatable psoralen derivative conjugated to insulin.

    Science.gov (United States)

    Gasparro, F P; Knobler, R M; Yemul, S S; Bisaccia, E; Edelson, R L

    1986-12-15

    4'-Aminomethyl-4,5',8-trimethylpsoralen has been chemically conjugated to insulin using a carbodiimide derivative. The psoralen moiety retains its photochemical reactivity as evidenced by its ability to crosslink DNA after exposure to long wavelength ultraviolet light (UVA, 320-400 nm). This chimeric molecule has been used to selectively kill a population of lymphocytes whose expression of insulin receptors has been stimulated with phytohemagglutinin. Insulin carries the psoralen into the cell via receptor-mediated endocytosis, where it is subsequently activated by exposure to UVA light. The UVA induced activity of AMT-insulin can be blocked by the presence of native insulin. The viability of unstimulated lymphocytes was not affected by AMT-insulin and UVA light. The hybrid insulin-psoralen molecule may be a prototype for a family of phototoxic drugs which can be selectively delivered to subsets of lymphocytes.

  15. Spasmolytic, antimicrobial and cytotoxic activities of 5-phenylpentyl isothiocyanate, a new glucosinolate autolysis product from horseradish (Armoracia rusticana P. Gaertn., B. Mey. & Scherb., Brassicaceae).

    Science.gov (United States)

    Dekić, Milan S; Radulović, Niko S; Stojanović, Nikola M; Randjelović, Pavle J; Stojanović-Radić, Zorica Z; Najman, Stevo; Stojanović, Sanja

    2017-10-01

    Detailed analyses of horseradish autolysates led to the identification of a new natural product, 5-phenylpentyl isothiocyanate (PhPeITC). The structural assignment was corroborated by synthesis, and the identity unequivocally established by spectral means. The occurrence of PhPeITC is the first direct proof of the existence of a 5-phenylpentyl glucosinolate in the aerial parts of this species as one of the possible "mustard oil" precursors. To verify its possible contribution to the horseradish functional food status, horseradish above- and underground autolysates, together with five ω-phenylalkyl isothiocyanates were tested for their spasmolytic, cytotoxic and antimicrobial activities. Specifically, the cytotoxic effect on Caco-2, HeLa (cancer) and MDCK (non-cancer) cell lines was established. Additionally, the five tested ITCs exerted significant spasmolytic activity (on rat distal colon), with PhPeITC being almost 100 times more potent than papaverine. A non-selective antimicrobial activity of all ITCs was revealed in the case of 6 bacterial and 2 fungal strains. Copyright © 2017 Elsevier Ltd. All rights reserved.

  16. Ganoderma lucidum stimulates NK cell cytotoxicity by inducing NKG2D/NCR activation and secretion of perforin and granulysin.

    Science.gov (United States)

    Chang, Chih-Jung; Chen, Yi-Yuan M; Lu, Chia-Chen; Lin, Chuan-Sheng; Martel, Jan; Tsai, Sheng-Hui; Ko, Yun-Fei; Huang, Tsung-Teng; Ojcius, David M; Young, John D; Lai, Hsin-Chih

    2014-04-01

    Ganoderma lucidum (G. lucidum) is a medicinal mushroom long used in Asia as a folk remedy to promote health and longevity. Recent studies indicate that G. lucidum activates NK cells, but the molecular mechanism underlying this effect has not been studied so far. To address this question, we prepared a water extract of G. lucidum and examined its effect on NK cells. We observed that G. lucidum treatment increases NK cell cytotoxicity by stimulating secretion of perforin and granulysin. The mechanism of activation involves an increased expression of NKG2D and natural cytotoxicity receptors (NCRs), as well as increased phosphorylation of intracellular MAPKs. Our results indicate that G. lucidum induces NK cell cytotoxicity against various cancer cell lines by activating NKG2D/NCR receptors and MAPK signaling pathways, which together culminate in exocytosis of perforin and granulysin. These observations provide a cellular and molecular mechanism to account for the reported anticancer effects of G. lucidum extracts in humans.

  17. Antiglycopeptide Mouse Monoclonal Antibody LpMab-21 Exerts Antitumor Activity Against Human Podoplanin Through Antibody-Dependent Cellular Cytotoxicity and Complement-Dependent Cytotoxicity.

    Science.gov (United States)

    Kato, Yukinari; Kunita, Akiko; Fukayama, Masashi; Abe, Shinji; Nishioka, Yasuhiko; Uchida, Hiroaki; Tahara, Hideaki; Yamada, Shinji; Yanaka, Miyuki; Nakamura, Takuro; Saidoh, Noriko; Yoshida, Kanae; Fujii, Yuki; Honma, Ryusuke; Takagi, Michiaki; Ogasawara, Satoshi; Murata, Takeshi; Kaneko, Mika K

    2017-02-01

    The interaction between podoplanin (PDPN) and C-type lectin-like receptor 2 (CLEC-2) is involved in tumor malignancy. We have established many monoclonal antibodies (mAbs) against human podoplanin using the cancer-specific mAb (CasMab) technology. LpMab-21, one of the mouse antipodoplanin mAbs, is of the IgG 2a subclass, and its minimum epitope was determined to be Thr76-Arg79 of the human podoplanin. Importantly, sialic acid is linked to Thr76; therefore, LpMab-21 is an antiglycopeptide mAb (GpMab). In this study, we investigated whether LpMab-21 shows antibody-dependent cellular cytotoxicity (ADCC) and complement-dependent cytotoxicity (CDC) against human podoplanin-expressing cancer cell lines in vitro and also studied its antitumor activities using a xenograft model. LpMab-21 showed high ADCC and CDC activities against not only podoplanin-expressing Chinese hamster ovary cells but also LN319 glioblastoma cells and PC-10 lung cancer cells, both of which endogenously express podoplanin. Furthermore, LpMab-21 decreased tumor growth in vivo, indicating that LpMab-21 could be useful for antibody therapy against human podoplanin-expressing cancers.

  18. Synthesis and Cytotoxicity of 2,3-Enopyranosyl C-Linked Conjugates of Genistein

    Directory of Open Access Journals (Sweden)

    Wieslaw Szeja

    2014-05-01

    Full Text Available A series of glycoconjugates, derivatives of genistein containing a C-glycosylated carbohydrate moiety, were synthesized and their anticancer activity was tested in vitro in the human cell lines HCT 116 and DU 145. The target compounds 15–17 were synthesized by treating ω-bromoalkyl C-glycosides derived from L-rhamnal (1 with a tetrabutylammonium salt of genistein. The new, metabolically stable analogs of previously studied O-glycosidic genistein derivatives inhibited proliferation of cancer cell lines through inhibition of the cell cycle.

  19. Antithrombotic and cytotoxic activities of four Bangladeshi plants and PASS prediction of their isolated compounds.

    Science.gov (United States)

    Kabir, Mohammad Shah Hafez; Mahamoud, Md Sofi; Chakrabarty, Nishan; Ahmad, Shabbir; Masum, Md Abdullah Al; Hoque, Md Akramul; Hossain, Mohammed Munawar; Rahman, Md Mominur; Uddin, Mir Muhammad Nasir

    2016-11-01

    This study aims to investigate whether tested organic extracts possess antithrombotic properties with minimal or no toxicity and to predict the activity of some of their isolated compounds. An in vitro thrombolytic model was used to check the clot lysis effect of four Bangladeshi herbal extracts viz., roots of Curculigo recurvata W.T. Aiton (Satipata), leaf of Amorphophallus bulbifer Roxb. (Olkachu), leaf of Phyllanthus sikkimensis Muell. Arg., and whole plant of Thunbergia grandiflora Roxb. (Nillata) using streptokinase as a positive control and water as a negative control. Cytotoxicity was screened by brine shrimp lethality bioassay using vincristine sulfate as positive control. In silico prediction of activity spectra for substances (PASS) prediction was applied for phytoconstituents, namely, nyasicoside, glucomannan, grandifloric acid, serine, and alanine. Using an in vitro thrombolytic model, C. recurvata, A. bulbifer, P. sikkimensis, and T. grandiflora showed 28.10±1.64%, 42.47±1.96%, 32.86±1.92%, and 25.51±1.67% of clot lysis, respectively. Reference drug streptokinase exhibited 75.00±3.04% clot lysis. Examined herbs showed significant (p<0.001) percentage (%) of clot lysis compared to negative control. In brine shrimp cytotoxic assay, C. recurvata, A. bulbifer, P. sikkimensis, and T. grandiflora showed LC50 values 210.64±3.44, 98.51±1.47, 187.29±2.01, and 386.43±3.02 μg/mL, respectively, with reference to vincristine sulfate (LC50 0.76±0.04). PASS predicted that examined phytoconstituents have a wide range of biological activity. Through our study it was found that A. bulbifer and P. sikkimensis could be considered as very promising and beneficial thrombolytic agents.

  20. Melanogenesis-inhibitory and cytotoxic activities of diarylheptanoids from Acer nikoense bark and their derivatives.

    Science.gov (United States)

    Akihisa, Toshihiro; Takeda, Ayano; Akazawa, Hiroyuki; Kikuchi, Takashi; Yokokawa, Satoru; Ukiya, Motohiko; Fukatsu, Makoto; Watanabe, Kensuke

    2012-08-01

    Nine cyclic diarylheptanoids, 1-9, including two new compounds, i.e., 9-oxoacerogenin A (8) and 9-O-β-D-glucopyranosylacerogenin K (9), along with three acyclic diarylheptanoids, 10-12, and four phenolic compounds, 13-16, were isolated from a MeOH extract of the bark of Acer nikoense (Aceraceae). Acid hydrolysis of 9 yielded acerogenin K (17) and D-glucose. Two of the cyclic diarylheptanoids, acerogenin A (1) and (R)-acerogenin B (5), were converted to their ether and ester derivatives, 18-24 and 27-33, respectively, and to the dehydrated derivatives, 25, 26, 34, and 35. Upon evaluation of compounds 1-16 and 18-35 for their inhibitory activities against melanogenesis in B16 melanoma cells, induced with α-melanocyte-stimulating hormone (α-MSH), eight natural glycosides, i.e., six diarylheptanoid glycosides, 2-4, 6, 9, and 12, and two phenolic glycosides, 15 and 16, exhibited inhibitory activities with 24-61% reduction of melanin content at 100 μM concentration with no or almost no toxicity to the cells (88-106% of cell viability at 100 μM). In addition, when compounds 1-16 and 18-35 were evaluated for cytotoxic activity against human cancer cell lines, two natural acyclic diarylheptanoids, 10 and 11, ten ether and ester derivatives, 18-22 and 27-31, and two dehydrated derivatives, 34 and 35, exhibited potent cytotoxicities against HL60 human leukemia cell line (IC(50) 8.1-19.3 μM), and five compounds, 10, 11, 20, 29, and 30, against CRL1579 human melanoma cell line (IC(50) 10.1-18.4 μM). Copyright © 2012 Verlag Helvetica Chimica Acta AG, Zürich.

  1. 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.

  2. Synthesis of novel 1H-1,2,3-triazole tethered C-5 substituted uracil-isatin conjugates and their cytotoxic evaluation

    KAUST Repository

    Kumar, Kewal; Sagar, Sunil; Esau, Luke; Kaur, Mandeep; Kumar, Vipan

    2012-01-01

    The present manuscript describes the synthesis of uracil-isatin hybrids via azide-alkyne cycloadditions and their cytotoxic evaluation against three human cancer cell lines viz. HeLa (cervix), MCF-7 (breast) and DU145 (prostate) using MTT assay. The evaluation studies revealed the dependence of cytotoxicity on C-5 substituents of both uracil and isatin as well as the alkyl chain length with compounds 6g and 6k showing IC50 values 18.21 and 13.90 μM respectively against DU145 cell lines. Most of the synthesized conjugates exhibited considerable selectivity against MCF-7 and DU145 cell lines. © 2012 Elsevier Masson SAS. All rights reserved.

  3. Synthesis of novel 1H-1,2,3-triazole tethered C-5 substituted uracil-isatin conjugates and their cytotoxic evaluation

    KAUST Repository

    Kumar, Kewal

    2012-12-01

    The present manuscript describes the synthesis of uracil-isatin hybrids via azide-alkyne cycloadditions and their cytotoxic evaluation against three human cancer cell lines viz. HeLa (cervix), MCF-7 (breast) and DU145 (prostate) using MTT assay. The evaluation studies revealed the dependence of cytotoxicity on C-5 substituents of both uracil and isatin as well as the alkyl chain length with compounds 6g and 6k showing IC50 values 18.21 and 13.90 μM respectively against DU145 cell lines. Most of the synthesized conjugates exhibited considerable selectivity against MCF-7 and DU145 cell lines. © 2012 Elsevier Masson SAS. All rights reserved.

  4. Utilization of Cyanoacetohydrazide and Oxadiazolyl Acetonitrile in the Synthesis of Some New Cytotoxic Heterocyclic Compounds.

    Science.gov (United States)

    Shaker, Soheir A; Marzouk, Magda I

    2016-01-29

    A (pyridazinyl)acetate derivative was reacted with thiosemicarbazide and hydrazine hydrate to yield spiropyridazinone and acetohydrazide derivatives, respectively. The acetohydrazide derivative was used as a starting material for synthesizing some new heterocyclic compounds such as oxoindolinylidene, dimethylpyrazolyl, methylpyrazolyl, oxopyrazolyl, cyanoacetylacetohydrazide and oxadiazolylacetonitrile derivatives. The behavior of the cyanoacetylacetohydrazide and oxadiazolylacetonitrile derivatives towards nitrogen and carbon nucleophiles was investigated. The assigned structures of the prepared compounds were elucidated by spectral methods (IR, ¹H-NMR (13)C-NMR and mass spectroscopy). Some of the newly prepared compounds were tested in vitro against a panel of four human tumor cell lines, namely hepatocellular carcinoma (liver) HePG-2, colon cancer HCT-116, human prostate cancer PC3, and mammary gland breast MCF-7. Also they were tested as antioxidants. Almost all of the tested compounds showed satisfactory activity.

  5. Green synthesis, antimicrobial and cytotoxic effects of silver nanoparticles using Eucalyptus chapmaniana leaves extract.

    Science.gov (United States)

    Sulaiman, Ghassan Mohammad; Mohammed, Wasnaa Hatif; Marzoog, Thorria Radam; Al-Amiery, Ahmed Abdul Amir; Kadhum, Abdul Amir H; Mohamad, Abu Bakar

    2013-01-01

    To synthesize silver nanopaticles from leaves extract of Eucalyptus chapmaniana (E. chapmaniana) and test the antimicrobial of the nanoparticles against different pathogenic bacteria, yeast and its toxicity against human acute promyelocytic leukemia (HL-60) cell line. Ten milliliter of leaves extract was mixed with 90 mL of 0.01 mmol/mL or 0.02 mmol/mL aqueous AgNO3 and exposed to sun light for 1 h. A change from yellowish to reddish brown color was observed. Characterization using UV-vis spectrophotometery and X-ray diffraction analysis were performed. Antimicrobial activity against six microorganisms was tested using well diffusion method and cytoxicity test using 3-(4, 5-Dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide, a yellow tetrazole was obtained on the human leukemia cell line (HL-60). UV-vis spectral analysis showed silver surface plasmon resonance band at 413 nm. X-ray diffraction showed that the particles were crystalline in nature with face centered cubic structure of the bulk silver with broad beaks at 38.50° and 44.76°. The synthesized silver nanoparticles efficiently inhibited various pathogenic organisms and reduced viability of the HL-60 cells in a dose-dependent manner. It has been demonstrated that the extract of E. chapmaniana leaves are capable of producing silver nanoparticles extracellularly and the Ag nanoparticles are quite stable in solution. Further studies are needed to fully characterize the toxicity and the mechanisms involved with the antimicrobial and anticancer activity of these particles.

  6. Green synthesis,antimicrobial and cytotoxic effects of silver nanoparticles using Eucalyptus chapmaniana leaves extract

    Institute of Scientific and Technical Information of China (English)

    Ghassan; Mohammad; Sulaiman; Wasnaa; Hatif; Mohammed; Thorria; Radam; Marzoog; Ahmed; Abdul; Amir; Al-Amiery; Abdul; Amir; H.Kadhum; Abu; Bakar; Mohamad

    2013-01-01

    Objective:To synthesize silver nanopaticles from leaves extract of Eucalyptus chapmaniana(E.chapmaniana)and test the antimicrobial of the nanoparticles against different pathogenic bacteria,yeast and its toxicity against human acute promyelocytic leukemia(HL-60)cell line.Methods:Ten milliliter of leaves extract was mixed with 90 mL of 0.01 mmol/mL or 0.02 mmol/mL aqueous AgNO3 and exposed to sun light for 1 h.A change from yellowish to reddish brown color was observed.Characterization using UV-vis spectrophotometery and X-ray diffraction analysis were performed.Antimicrobial activity against six microorganisms was tested using well diffusion method and cytoxicity test using 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide,a yellow tetrazole was obtained on the human leukemia cell line(HL-60).Results:UV-vis spectral analysis showed silver surface plasmon resonance band at 413 nm.X-ray diffraction showed that the particles were crystalline in nature with face centered cubic structure of the bulk silver with broad beaks at 38.50°and 44.76°.The synthesized silver nanoparticles efficiently inhibited various pathogenic organisms and reduced viability of the HL-60 cells in a dose-dependent manner.Conclusions:It has been demonstrated that the extract of E.chapmaniana leaves are capable of producing silver nanoparticles extracellularly and the Ag nanoparticles are quite stable in solution.Further studies are needed to fully characterize the toxicity and the mechanisms involved with the antimicrobial and anticancer activity of these particles.

  7. Green synthesis, antimicrobial and cytotoxic effects of silver nanoparticles using Eucalyptus chapmaniana leaves extract

    Institute of Scientific and Technical Information of China (English)

    Ghassan Mohammad Sulaiman; Wasnaa Hatif Mohammed; Thorria Radam Marzoog; Ahmed Abdul Amir Al-Amiery; Abdul Amir H Kadhum; Abu Bakar Mohamad

    2013-01-01

    Objective: To synthesize silver nanopaticles from leaves extract of Eucalyptus chapmaniana (E. chapmaniana) and test the antimicrobial of the nanoparticles against different pathogenic bacteria, yeast and its toxicity against human acute promyelocytic leukemia (HL-60) cell line.Methods:Ten milliliter of leaves extract was mixed with 90 mL of 0.01 mmol/mL or 0.02 mmol/mL aqueous AgNO3 and exposed to sun light for 1 h. A change from yellowish to reddish brown color was observed. Characterization using UV-vis spectrophotometery and X-ray diffraction analysis were performed. Antimicrobial activity against six microorganisms was tested using well diffusion method and cytoxicity test using 3-(4, 5-Dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide, a yellow tetrazole was obtained on the human leukemia cell line (HL-60). Results: UV-vis spectral analysis showed silver surface plasmon resonance band at 413 nm. X-ray diffraction showed that the particles were crystalline in nature with face centered cubic structure of the bulk silver with broad beaks at 38.50 ° and 44.76 °. The synthesized silver nanoparticles efficiently inhibited various pathogenic organisms and reduced viability of the HL-60 cells in a dose-dependent manner. Conclusions: It has been demonstrated that the extract of E. chapmaniana leaves are capable of producing silver nanoparticles extracellularly and the Ag nanoparticles are quite stable in solution. Further studies are needed to fully characterize the toxicity and the mechanisms involved with the antimicrobial and anticancer activity of these particles.

  8. 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.

  9. Co-activation of AMPK and mTORC1 Induces Cytotoxicity in Acute Myeloid Leukemia

    Directory of Open Access Journals (Sweden)

    Pierre Sujobert

    2015-06-01

    Full Text Available AMPK is a master regulator of cellular metabolism that exerts either oncogenic or tumor suppressor activity depending on context. Here, we report that the specific AMPK agonist GSK621 selectively kills acute myeloid leukemia (AML cells but spares normal hematopoietic progenitors. This differential sensitivity results from a unique synthetic lethal interaction involving concurrent activation of AMPK and mTORC1. Strikingly, the lethality of GSK621 in primary AML cells and AML cell lines is abrogated by chemical or genetic ablation of mTORC1 signaling. The same synthetic lethality between AMPK and mTORC1 activation is established in CD34-positive hematopoietic progenitors by constitutive activation of AKT or enhanced in AML cells by deletion of TSC2. Finally, cytotoxicity in AML cells from GSK621 involves the eIF2α/ATF4 signaling pathway that specifically results from mTORC1 activation. AMPK activation may represent a therapeutic opportunity in mTORC1-overactivated cancers.

  10. Cymantrenyl-Nucleobases: Synthesis, Anticancer, Antitrypanosomal and Antimicrobial Activity Studies

    Directory of Open Access Journals (Sweden)

    Artur Jabłoński

    2017-12-01

    Full Text Available The synthesis of four cymantrene-5-fluorouracil derivatives (1–4 and two cymantrene-adenine derivatives (5 and 6 is reported. All of the compounds were characterized by spectroscopic methods and the crystal structure of two derivatives (1 and 6, together with the previously described cymantrene-adenine compound C was determined by X-ray crystallography. While the compounds 1 and 6 crystallized in the triclinic P-1 space group, compound C crystallized in the monoclinic P21/m space group. The newly synthesized compounds 1–6 were tested together with the two previously described cymantrene derivatives B and C for their in vitro antiproliferative activity against seven cancer cell lines (MCF-7, MCF-7/DX, MDA-MB-231, SKOV-3, A549, HepG2m and U-87-MG, five bacterial strains Staphylococcus aureus (methicillin-sensitive, methicillin-resistant and vancomycin-intermediate strains, Staphylococcus epidermidis, and Escherichia coli, including clinical isolates of S. aureus and S. epidermidis, as well as against the protozoan parasite Trypanosoma brucei. The most cytotoxic compounds were derivatives 2 and C for A549 and SKOV-3 cancer cell lines, respectively, with 50% growth inhibition (IC50 values of about 7 µM. The anticancer activity of the cymantrene compounds was determined to be due to their ability to induce oxidative stress and to trigger apoptosis and autophagy in cancer cells. Three derivatives (1, 4 and 5 displayed promising antitrypanosomal activity, with GI50 values in the low micromolar range (3–4 µM. The introduction of the 5-fluorouracil moiety in 1 enhanced the trypanocidal activity when compared to the activity previously reported for the corresponding uracil derivative. The antibacterial activity of cymantrene compounds 1 and C was within the range of 8–64 µg/mL and seemed to be the result of induced cell shrinking.

  11. Nine New Gingerols from the Rhizoma of Zingiber officinale and Their Cytotoxic Activities.

    Science.gov (United States)

    Li, Zezhi; Wang, Yanzhi; Gao, MeiLing; Cui, Wanhua; Zeng, Mengnan; Cheng, Yongxian; Li, Juan

    2018-02-02

    Nine new gingerols, including three 6-oxo-shogaol derivatives [( Z )-6-oxo-[6]-shogaol ( 1 ), ( Z )-6-oxo-[8]-shogaol ( 2 ), ( Z )-6-oxo-[10]-shogaol ( 3 )], one 6-oxoparadol derivative [6-oxo-[6]-paradol ( 4 )], one isoshogaol derivative [( E )-[4]-isoshogaol ( 5 )], and four paradoldiene derivatives [(4 E ,6 Z )-[4]-paradoldiene ( 8 ), (4 E ,6 E )-[6]-paradoldiene ( 9 ), (4 E ,6 E )-[8]-paradoldiene ( 10 ), (4 E ,6 Z )-[8]-paradoldiene ( 11 )], together with eight known analogues, were isolated from the rhizoma of Zingiber officinale . Their structures were elucidated on the basis of spectroscopic data. It was noted that the isolation of 6-oxo-shogaol derivatives represents the first report of gingerols containing one 1,4-enedione motif. Their structures were elucidated on the basis of spectroscopic and HRESIMS data. All the new compounds were evaluated for their cytotoxic activities against human cancer cells (MCF-7, HepG-2, KYSE-150).

  12. 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.

  13. A new ceramide from Suillus luteus and its cytotoxic activity against human melanoma cells.

    Science.gov (United States)

    León, Francisco; Brouard, Ignacio; Torres, Fernando; Quintana, José; Rivera, Augusto; Estévez, Francisco; Bermejo, Jaime

    2008-01-01

    A new phytosphingosine-type ceramide, suillumide (1), was isolated from the EtOH extract of the basidiomycete Suillus luteus (L.) S. F. Gray, along with ten known compounds: ergosta-4,6,8(14),22-tetraen-3-one, ergosterol, ergosterol peroxide, suillin, (E)-3,4,5-trimethoxycinnamic alcohol, 5 alpha,6 alpha-epoxyergosta-8,22-diene-3beta,7 beta-diol, (R)-1-palmitoylglycerol, ergosta-7,9(11),22-triene-3beta,5 alpha,6 beta-triol, cerevisterol, and 4-hydroxybenzoic acid. The structure of 1 was determined on the basis of spectroscopic and mass-spectrometric analyses, as well as by chemical methods. Compound 1 and its synthetic diacetyl derivative 2 were tested for their cytotoxic activities against the human melanoma cell line SK-MEL-1. Both drugs showed IC(50) values of ca. 10 microM after 72 h of exposure.

  14. Ti-GO-Ag nanocomposite: the effect of content level on the antimicrobial activity and cytotoxicity.

    Science.gov (United States)

    Jin, Jianfeng; Zhang, Li; Shi, Mengqi; Zhang, Yumei; Wang, Qintao

    2017-01-01

    Surface modification of titanium (Ti) implants are extensively studied in order to obtain prominent biocompatibility and antimicrobial activity, especially preventing implant-associated infection. In this study, Ti substrates surface were modified by graphene oxide (GO) thin film and silver (Ag) nanoparticles via electroplating and ultraviolet reduction methods so as to achieve this purpose. Microstructures, distribution, quantities and spectral peaks of GO and Ag loading on the Ti sheets surface were characterized. GO-Ag-Ti multiphase nanocomposite exhibited excellent antimicrobial ability and anti-adherence performance. Subsequently, morphology, membrane integrity, apoptosis and relative genes expression of bacteria incubated on the Ti samples surface were monitored to reveal the bactericidal mechanism. Additionally, the cytotoxicity of Ti substrates incorporating GO thin film and Ag nanoparticles were investigated. GO-Ag-Ti composite configuration that have outstanding antibacterial properties will provide the foundation to study bone integration in vitro and in vivo in the future.

  15. New flavonol glycoside from Scabiosa prolifera L. aerial parts with in vitro antioxidant and cytotoxic activities.

    Science.gov (United States)

    Al-Qudah, Mahmoud A; Otoom, Noor K; Al-Jaber, Hala I; Saleh, Ayman M; Abu Zarga, Musa H; Afifi, Fatma U; Abu Orabi, Sultan T

    2017-12-01

    Phytochemical investigation of the chemical constituents of the aerial parts of Scabiosa prolifera L. led to the isolation of one new flavonol glycoside, kaempferol-3-O-(4″,6″-di-E-p-coumaroyl)-β-D-galactopyranoside (1), along with ten other known compounds including luteolin-7-O-(2″-O-ethyl-β-glucopyranoside), β-sitosterol, β-sitosterylglucoside, ursolic acid, corosolic acid, ursolic acid 3-O-β-D-arabinopyranoside, apigenin, methyl-α-D-glucopyranoside, luteolin-7-O-β-glucopyranoside and isoorientin. The structures of all isolated compounds were established using chemical methods and spectroscopic methods including IR, UV, NMR (1D and 2D) and HRESIMS. All compounds were isolated for the first time from the plant. The antioxidant and cytotoxic activities of compounds 1 and 2 were also investigated.

  16. 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.

  17. In vitro evaluation of antioxidant and cytotoxic activities of lignin fractions extracted from Acacia nilotica.

    Science.gov (United States)

    Barapatre, Anand; Meena, Avtar Singh; Mekala, Sowmya; Das, Amitava; Jha, Harit

    2016-05-01

    Lignin is one of the most important phytomacromolecule with diverse therapeutic properties such as anticancer, antimicrobial, anti-inflammatory and immune-stimulatory. The present study was carried out to evaluate the in vitro antioxidant, free radical scavenging and anti-proliferative/cytotoxic activities of eleven different lignin fractions, extracted from the wood of Acacia nilotica by pressurized solvent extraction (PSE) and successive solvent extraction (SSE) methods. Results indicate that the PSE fractions have high polyphenolic content and reducing power. However, the antioxidant efficiency examined by DPPH and ABTS radical scavenging assay was higher in SSE fractions. All lignin fractions revealed a significant ability to scavenge nitric oxide, hydroxyl and superoxide radicals. The extracted lignin fractions display high ferric ion reducing capacity and also possess excellent antioxidant potential in the hydrophobic (linoleic acid) system. Fractions extracted by polar solvent has the highest iron (Fe(2+)) chelating activity as compared to other factions, indicating their effect on the redox cycling of iron. Four lignin fractions depicted higher cytotoxic potential (IC50: 2-15 μg/mL) towards breast cancer cell line (MCF-7) but were ineffective (IC50: ≥ 100 μg/mL) against normal primary human hepatic stellate cells (HHSteCs). These findings suggest that the lignin extracts of A. nilotica wood has a remarkable potential to prevent disease caused by the overproduction of radicals and also seem to be a promising candidate as natural antioxidant and anti-cancer agents. Copyright © 2016 Elsevier B.V. All rights reserved.

  18. Ti-GO-Ag nanocomposite: the effect of content level on the antimicrobial activity and cytotoxicity

    Directory of Open Access Journals (Sweden)

    Jin J

    2017-06-01

    Full Text Available Jianfeng Jin,1,2 Li Zhang,3 Mengqi Shi,3 Yumei Zhang,3 Qintao Wang11State Key Laboratory of Military Stomatology and National Clinical Research Center for Oral Diseases and Shaanxi Engineering Research Center for Dental Materials and Advanced Manufacture, Department of Periodontology, School of Stomatology, The Fourth Military Medical University, Xi’an, 2Department of General Dentistry, Kunming Municipal Stomatology Hospital, Kunming, 3State Key Laboratory of Military Stomatology and National Clinical Research Center for Oral Diseases and Shaanxi Key Laboratory of Stomatology, Department of Prosthodontics, School of Stomatology, The Fourth Military Medical University, Xi’an, People’s Republic of China Abstract: Surface modification of titanium (Ti implants are extensively studied in order to obtain prominent biocompatibility and antimicrobial activity, especially preventing implant-associated infection. In this study, Ti substrates surface were modified by graphene oxide (GO thin film and silver (Ag nanoparticles via electroplating and ultraviolet reduction methods so as to achieve this purpose. Microstructures, distribution, quantities and spectral peaks of GO and Ag loading on the Ti sheets surface were characterized. GO-Ag-Ti multiphase nanocomposite exhibited excellent antimicrobial ability and anti-adherence performance. Subsequently, morphology, membrane integrity, apoptosis and relative genes expression of bacteria incubated on the Ti samples surface were monitored to reveal the bactericidal mechanism. Additionally, the cytotoxicity of Ti substrates incorporating GO thin film and Ag nanoparticles were investigated. GO-Ag-Ti composite configuration that have outstanding antibacterial properties will provide the foundation to study bone integration in vitro and in vivo in the future.Keywords: GO-Ag-Ti multiphase nanocomposite, microstructure and quantities, antibacterial activity, bactericidal mechanism, cytotoxicity

  19. A non-cytotoxic N-dehydroabietylamine derivative with potent antimalarial activity.

    Science.gov (United States)

    Sadashiva, Maralinganadoddi P; Gowda, Raghavendra; Wu, Xianzhu; Inamdar, Gajanan S; Kuzu, Omer F; Rangappa, Kanchugarakoppal S; Robertson, Gavin P; Gowda, D Channe

    2015-08-01

    Malaria caused by the Plasmodium parasites continues to be an enormous global health problem owing to wide spread drug resistance of parasites to many of the available antimalarial drugs. Therefore, development of new classes of antimalarial agents is essential to effectively treat malaria. In this study, the efficacy of naturally occurring diterpenoids, dehydroabietylamine and abietic acid, and their synthetic derivatives was assessed for antimalarial activity. Dehydroabietylamine and its N-trifluoroacetyl, N-tribromoacetyl, N-benzoyl, and N-benzyl derivatives showed excellent activity against P. falciparum parasites with IC50 values of 0.36 to 2.6 µM. Interestingly, N-dehydroabietylbenzamide showed potent antimalarial activity (IC50 0.36), and negligible cytotoxicity (IC50 >100 µM) to mammalian cells; thus, this compound can be an important antimalarial drug. In contrast, abietic acid was only marginally effective, exhibiting an IC50 value of ~82 µM. Several carboxylic group-derivatives of abietic acid were moderately active with IC50 values of ~8.2 to ~13.3 µM. These results suggest that a detailed understanding of the structure-activity relationship of abietane diterpenoids might provide strategies to exploit this class of compounds for malaria treatment. Copyright © 2015 Elsevier Inc. All rights reserved.

  20. In Vitro Antiplasmodial Activity and Cytotoxic Effect of (Z-2-Benzylidene-4, 6-Dimethoxybenzofuran-3(2H-One Derivatives

    Directory of Open Access Journals (Sweden)

    Ali RAMAZANI

    2016-10-01

    Full Text Available Background: Aurones are naturally occurring compounds that belong to flavenoids family and have antiplasmodial effects. This study investigated some new aurones derivatives against chloroquine sensitive Plasmodium falciparum. Here we report the synthesis, in vitro antiplasmodial activity and cytotoxic evaluation of 11 compound from derivatives of (Z-2- benzylidene-4, 6-dimethoxybenzofuran-3(2H-one.Methods: The cytotoxic evaluations of active compounds were performed with MTT (3-[4, 5-dimethylthiazol-2-yl]-2, 5 diphenyltetrazolium bromide assay on human breast cancer cell lines; MCF7 and T47D.Results: From 11 compounds M3, M6 and M7 compounds showed good antiplasmodial effect against chloroquine-sensitive 3D strain of P. falciparum with IC50 (50% inhibitory concentration values of 7.82, 7.27 and 2.3 µM respectively. No noticeable toxicity was‌ observed with these compounds when tested against tested cell lines. Conclusion: The replacement of the 4 and 5 positions at ring B of aurone derivatives, with propoxy and bromide (Br respectively was revealed highly advantageous for their antiplasmodial effect.

  1. Evaluation of antioxidative and cytotoxic activities of Streptomyces pluripotens MUSC 137 isolated from mangrove soil in Malaysia

    Directory of Open Access Journals (Sweden)

    Hooi-Leng eSer

    2015-12-01

    Full Text Available A well characterized strain, Streptomyces pluripotens MUSC 137 was isolated from mangrove soil at Tanjung Lumpur, Malaysia. The biological activities of this particular strain of Streptomyces were then explored. For experimentation, the extract of fermentation was prepared by using solvent extraction method. The antioxidant activity was examined by using DPPH assay. The cytotoxicity activity of extract was assessed against selected human cancer cell lines, namely colon cancer cells (HCT-116, Caco-2, SW480 & HT-29, breast cancer cell (MCF-7, lung cancer cell (A549, prostate cancer cell (DU145 and cervical cancer cell (Ca Ski. The results showed MUSC 137 extract possessed significant antioxidant activity and cytotoxic effect against some of the tested cancer cell lines. Lowest IC50 was recorded in MCF-7 cells (61.33 ± 17.10 µg/mL, followed by HCT-116 and A549. Subsequently, the extract was subjected to chemical analysis using GC-MS, which led to the identification of chemical constituents present in the extract of MUSC 137. The analysis resulted in the identification of chemical constituents including deferoxamine and pyrrolizidines related-compounds which may responsible for antioxidant and cytotoxic activities observed. The result of the present investigation is the first report on the potential antioxidative and cytotoxic activities of Streptomyces pluripotens MUSC 137.

  2. Genotoxic and cytotoxic activity of green synthesized TiO2 nanoparticles

    Science.gov (United States)

    Koca, Fatih Doğan; Duman, Fatih

    2018-03-01

    Nowadays, nanomaterials that are smaller than 100 nm in size are very attractive owing to their enhanced physicochemical properties. Although they have been used widely for industrial applications, their toxicity still remains a problem. This article is a new record of the synthesis of titanium dioxide nanoparticles (TiO2 NPs) by a Mentha aquatica leaf extract and determination of its toxicity to rat marrow mesenchymal stem cells. In this study, we aimed to determine the genotoxic and cytotoxic effects of biologically synthetized TiO2 NPs. The characteristic peak of the nanomaterial was observed at 354 nm. The mean size of the nanomaterial was measured to be 69 nm from SEM images. According to zeta analysis, the surface charge of the nanomaterial was - 37.6 mV. The crystalline structure of the nanomaterial was determined using XRD analysis. It was concluded that the obtained nanomaterial was TiO2 The results of the FT-IR analysis showed that the functional groups that were found in the plant extract could play an important role in the formation and stabilization of TiO2 NPs. The effective size of the TiO2 NPs was found to be 304 nm using DLS analysis. The TGA analysis results showed that the total mass loss was 4% at 900 °C. According to DNA cleavage analysis results, TiO2 NPs cause damage to the plasmid pBR322 DNA in a concentration-dependant matter. It has been noted that TiO2 NPs lead to decreased cell viability during increased time and concentration of applications on rat marrow mesenchymal stem cells. It has also been determined that bulk TiO2 causes a greater reduction in the stem cell viability compared to the biosynthesized NPs. The obtained results could be useful for further application and toxicity studies.

  3. Synthesis and in vitro cytotoxicity of novel C-12 substituted-14-deoxy-andrographolide derivatives as potent anti-cancer agents.

    Science.gov (United States)

    Kandanur, Sai Giridhar Sarma; Golakoti, Nageswara Rao; Nanduri, Srinivas

    2015-12-15

    Andrographolide, the major labdane diterpenoid from Andrographis paniculata has been reported to be cytotoxic against various cancer cells in vitro. Our research efforts led to the discovery of novel 12-phenyl thio and 12-aryl amino-14-deoxy-andrographolide derivatives (III q and III r) with potent cytotoxic activity, 12-benzyl amino-14-deoxy-andrographolide analogues showing broad range of cytotoxic activity against most of the cell lines and 12-alkyl amino-14-deoxy-andrographolide derivatives being selective to few cell lines (PC-3 and HOP-92), when the selected analogues were evaluated against 60 human cancer cell line panel at National Cancer Institute (N.C.I.), USA. The SAR (structure activity relationship) studies demonstrated potent activity for the compounds containing the following functionalities at C-12: substituted aryl amino/phenyl thio>benzylamine>alkyl amine. The significant cytotoxic activity observed for compounds III q and III r suggest that these could serve as templates for further optimization. Copyright © 2015 Elsevier Ltd. All rights reserved.

  4. 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.

  5. 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.

  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 LD 50 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. Antiproliferative, Cytotoxic, Antioxidant Activity and Polyphenols Contents in Leaves of Four Staphylea L. Species

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    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.

  8. 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.

  9. Cytotoxic constituents from Brazilian red propolis and their structure-activity relationship.

    Science.gov (United States)

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

    2008-05-15

    Several classes of flavonoids [flavanoids (1-10), flavonol (11), isoflavones (12-18), isoflavanones (19-22), isoflavans (23-26), chalcones (27-30), auronol (31), pterocarpans (32-37), 2-arylbenzofuran (38), and neoflavonoid (39)] and lignans (40-42) isolated from the MeOH extract of Brazilian red propolis were investigated for their cytotoxic activity against a panel of six different cancer cell lines including murine colon 26-L5 carcinoma, murine B16-BL6 melanoma, murine Lewis lung carcinoma, human lung A549 adenocarcinoma, human cervix HeLa adenocarcinoma, and human HT-1080 fibrosarcoma cell lines. Based on the observed results, structure-activity relationships were discussed. Among the tested compounds, 7-hydroxy-6-methoxyflavanone (3) exhibited the most potent activity against B16-BL6 (IC(50), 6.66microM), LLC (IC(50), 9.29microM), A549 (IC(50), 8.63microM), and HT-1080 (IC(50), 7.94microM) cancer cell lines, and mucronulatol (26) against LLC (IC(50), 8.38microM) and A549 (IC(50), 9.9microM) cancer cell lines. These activity data were comparable to those of the clinically used anticancer drugs, 5-fluorouracil and doxorubicin, against the tested cell lines, suggesting that 3 and 26 are the good candidates for future anticancer drug development.

  10. 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...

  11. Cephalostatin analogues--synthesis and biological activity.

    Science.gov (United States)

    Flessner, Timo; Jautelat, Rolf; Scholz, Ulrich; Winterfeldt, Ekkehard

    2004-01-01

    Starting off in the early 90's the field of cephalostatin analogues has continually expanded over the last 10 years. First syntheses prepared symmetric analogues like 14b (119) and 26 (65), which were subsequently desymmetrized to provide analogues like beta-hydroxy ketone 31 (19). Importantly the straightforward approach provided already compounds with mu-molar potency and the same pattern of activity as cephalostatin 1 (1) (see Chapter 2.1). Chemically more demanding, two new methods for the directed synthesis of (bissteroidal) pyrazines were devised and subsequently applied to a wide variety of differently functionalized coupling partners. These new methods allowed for the synthesis of various analogues (Chapter 2.2.; and, last but not least, for the totals synthesis of several cephalostatin natural products; Chapter 1.). Functionalization and derivatization of the 12-position was performed (Chapter 2.1 and 3) and synthetic approaches to establish the D-ring double bond were successfully investigated (Chapter 3). [figure: see text] Dealing synthetically with the spiroketal moiety, novel oxidative opening procedures on monomeric delta 14, 15-steroids were devised as well as intensive studies regarding spiroketal synthesis and spiroketal rearrangements were conducted (Chapter 3.2. and 4.). Last but not least direct chemical modification of ritterazines and cephalostatins were studied, which provided a limited number of ritterazine analogues (Chapter 4.). All these synthetic activities towards analogues are summarized in Fig. 18. During this period of time the growing number of cephalostatins and ritterazines on the one hand and of analogues on the other hand provided several SAR trends, which can guide future analogue synthesis. The combined SAR findings are displayed in Fig. 19. So far it is apparent that: Additional methoxylations or hydroxylations in the steroidal A ring core structure (1-position) are slightly decreasing activity (compare cephalostatin 1 1 to

  12. Synthesis, characterization, photoluminescence and cytotoxic properties of novel luminescent Eu(III)complexes based on chromone Schiff base

    Science.gov (United States)

    Saif, M.; El-Shafiy, Hoda F.; Mashaly, Mahmoud M.; Eid, Mohamed F.; Nabeel, A. I.; Fouad, R.

    2018-06-01

    Three novel Eu(III) phosphor complexes, [Eu(HL)(OH2)2(C2H5OH)](NO3)2 (1), [Eu(HL)(Bpy)(NO3)2(EtOH)] (2) and [Eu(HL)(Phen)(NO3)2(H2O)] (3) (HL = (11E)-2-hydroxy-N/-((4-oxo-4H-chromen-3-yl)methylene)benzohydrazide; Bpy = 2,2/-bibyridyl and Phen = 1,10-phenanthroline) were prepared. Elemental, thermal, FT-IR and XRD methods were used to characterize their structural configuration. The HL behaves as a monoanionic tridentate ligand. The XRD analysis shows that the ligand and its Eu3+complexes are in nano domain. From fluorescence spectroscopy, all the prepared complexes are highly luminescent, having an impressive visual emission under UV excitation. The H2L and its Eu3+nano-complexes (1-3) were tested for their in vitro cytotoxicity against Ehrlich Ascites Carcinoma cell line (EAC). The Eu(III) nano-complexes (1-3) effectively inhibited EAC growth with IC50 value of 25 μM. The high antitumor activity of the Eu(III) nano-complexes (1-3) were attributed to its chemical structure, and nano size properties.

  13. New Approaches for the Synthesis, Cytotoxicity and Toxicity of Heterocyclic Compounds Derived from 2-Cyanomethylbenzo[c]imidazole.

    Science.gov (United States)

    Mohareb, Rafat M; Mohamed, Abeer A; Abdallah, Amira E M

    2016-01-01

    The reaction of ethyl cyanoacetate with o-phenylenediamine gave the 2-cyanomethylbenzo[c]imidazole (1). The latter compound was used as the key starting material to synthesise biologically active heterocyclic derivatives. Thus, the reaction of 1 with cyclohexanone and either of benzaldehyde, 4-methoxybenzaldehyde or 4-chlorobenzaldehyde gave the annulated derivatives 2a-c, respectively. The antitumor evaluations of the newly synthesized products against the three cancer cell lines MCF-7 (breast adeno-carcinoma), NCI-H460 (non-small cell lung cancer) and SF-268 (CNS cancer) showed that compounds 2b, 6, 11b, 11c, 12b, 16a, 16b and 18a exhibited optimal cytotoxic effect against cancer cell lines, with IC50 values in the nM range. Bioactive compounds are often toxic to shrimp larvae. Thus, in order to monitor these chemicals in vivo lethality to shrimp larvae (Artemia salina), Brine-Shrimp Lethality Assay was used. Compounds 11b, 12b and 16b showed no toxicity against the tested organisms.

  14. Copper(II Complexes Based on Aminohydroxamic Acids: Synthesis, Structures, In Vitro Cytotoxicities and DNA/BSA Interactions

    Directory of Open Access Journals (Sweden)

    Jia Zhang

    2018-05-01

    Full Text Available Four complexes, [Cu2(glyha(bpy2(H2O]·2ClO4·H2O (1, [Cu2(glyha(phen2]·2ClO4 (2, [Cu2(alaha(bpy2Cl]·Cl·4H2O (3, and [{Cu2(alaha(phen2}{Cu2(alaha(phen2(NO3}]·3NO3 (4 (glyha2− = dianion glycinehydroxamic acid, alaha2− = dianion alaninehydroxamic acid, bpy = 2,2′-bipyridine, phen = 1,10-phenanthroline have been successfully synthesized and characterized by X-ray single crystal diffraction. The interactions of these complexes with calf thymus DNA (CT-DNA were studied through UV spectroscopy, fluorescence spectroscopy, and circular dichroism. The results revealed that complexes 1–4 could interact with CT-DNA through intercalation. Interactions of all complexes with bovine serum albumin (BSA were confirmed by the docking study to quench the intrinsic fluorescence of BSA in a static quenching process. Furthermore, the in vitro cytotoxic effect of the complexes was also examined on four tumor cell lines, including human lung carcinoma cell line (A549, human colon carcinoma cell line (HCT-116, human promyelocytic leukemia cell (HL-60 and cervical cancer cell line (HeLa. All complexes exhibited different antitumor activities.

  15. The effect of gamma irradiation on cytotoxic activity of the flesh of Mahkota Dewa (Phaleria macrocarpa (Scheff) Boerl) Fruits

    International Nuclear Information System (INIS)

    Ermin K Winarno; Mazda; Hindra Rahmawati; Hendig Winarno

    2010-01-01

    Gamma irradiation had been used by herbs medicine industries for preservation of medicinal plants, but the effect of irradiation on their bioactivities has not been observed. The purpose of this research was to obtain the optimum radiation dose for the preservation of mahkota dewa flesh fruits without damaging their cytotoxic activities. To evaluate the effect of irradiation, dried samples of flesh fruit of mahkota dewa were irradiated at various doses of 0; 5; 7.5; 10; 15 and 20 kGy. Microbial contamination was tested using Indonesian National Standard method, which indicated that all microbes were killed at the dose of 5 kGy. Each sample was macerated with ethanol, and the extracts obtained were then fractionated with column chromatography, from which 8 fractions were obtained. Cytotoxicity test of the fractions against leukemia L1210 cells, showed that the Fr.3 was the most cytotoxic. To determine optimal irradiation dose to inhibit and to kill bacteria and yeast/mold in the mahkota dewa flesh fruit samples without decreasing cytotoxic activity, a thin layer chromatography (TLC) and high performance liquid chromatography (HPLC) analysis of the Fr.3 were done. The results showed that the doses of ≥ 5 kGy inhibited the growth and killed all the bacteria, yeast and mold without decreasing significantly the cytotoxic activity of ethanol extract against leukemia L1210 cell. The significant decrease of cytotoxic against leukemia L1210 of ethanol extract were occurred after ≥ 10 kGy irradiation of the samples. At the dose of 10 kGy, the cytotoxicity decreased even though it was not exceeded the limit of the fraction was declared inactive. Analysis of thin layer chromatogram profiles showed that the Fr.3 contained at least 10 components. Irradiation until the dose of 20 kGy decreased the major peak intensity. with the increasing of irradiation doses. It was concluded that the dose of 5 kGy to 10 kGy were the optimum dose for the preservation of flesh fruit of

  16. Cytotoxicity and anti-Leishmania amazonensis activity of Citrus sinensis leaf extracts.

    Science.gov (United States)

    Garcia, Andreza R; Amaral, Ana Claudia F; Azevedo, Mariana M B; Corte-Real, Suzana; Lopes, Rosana C; Alviano, Celuta S; Pinheiro, Anderson S; Vermelho, Alane B; Rodrigues, Igor A

    2017-12-01

    Leishmania amazonensis is the main agent of diffuse cutaneous leishmaniasis, a disease characterized by lesional polymorphism and the commitment of skin surface. Previous reports demonstrated that the Citrus genus possess antimicrobial activity. This study evaluated the anti-L. amazonensis activity of Citrus sinensis (L.) Osbeck (Rutaceae) extracts. Citrus sinensis dried leaves were subjected to maceration with hexane (CH), ethyl acetate (CEA), dichloromethane/ethanol (CD/Et - 1:1) or ethanol/water (CEt/W - 7:3). Leishmania amazonensis promastigotes were treated with C. sinensis extracts (1-525 μg/mL) for 120 h at 27 °C. Ultrastructure alterations of treated parasites were evaluated by transmission electron microscopy. Cytotoxicity of the extracts was assessed on RAW 264.7 and J774.G8 macrophages after 48-h treatment at 37 °C using the tetrazolium assay. In addition, Leishmania-infected macrophages were treated with CH and CD/Et (10-80 μg/mL). CH, CD/Et and CEA displayed antileishmanial activity with 50% inhibitory activity (IC 50 ) of 25.91 ± 4.87, 54.23 ± 3.78 and 62.74 ± 5.04 μg/mL, respectively. Parasites treated with CD/Et (131.2 μg/mL) presented severe alterations including mitochondrial swelling, lipid body formation and intense cytoplasmic vacuolization. CH and CD/Et demonstrated cytotoxic effects similar to that of amphotericin B in the anti-amastigote assays (SI of 2.16, 1.98 and 1.35, respectively). Triterpene amyrins were the main substances in CH and CD/Et extracts. In addition, 80 μg/mL of CD/Et reduced the number of intracellular amastigotes and the percentage of infected macrophages in 63% and 36%, respectively. The results presented here highlight C. sinensis as a promising source of antileishmanial agents.

  17. 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.

  18. Detection of Cytotoxic Activity of Lectin on Human Colon Adenocarcinoma (Sw480 and Epithelial Cervical Carcinoma (C33-A

    Directory of Open Access Journals (Sweden)

    Mirandeli Bautista

    2011-03-01

    Full Text Available Lectins comprise a heterogeneous class of proteins that recognize the carbohydrate moieties of glycoconjugates with high specificity. Numerous studies have shown that lectins are capable of recognizing specific carbohydrate moieties displayed by malignant cells or tissues. The present work was performed to investigate the effects of tepary bean (Phaseolus acutifolius lectins on proliferation, colony formation, and alteration of DNA synthesis of human malignant cells. Tepary bean lectin showed dose dependent  effects on the inhibition of viability as well as on colony formation in two human malignant cells lines (C33-A, Sw480; By contrast, tepary bean lectin only showed significant effects on DNA synthesis on Sw480 cells. Our results provide evidence of the anti- proliferative and cytotoxic effects of the tepary bean lectins on C33-A and Sw480 cells lines.

  19. Acute toxicity, brine shrimp cytotoxicity and relaxant activity of fruits of callistemon citrinus curtis

    Directory of Open Access Journals (Sweden)

    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

  20. 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.

  1. Phytochemicals from Kaempferia angustifolia Rosc. and Their Cytotoxic and Antimicrobial Activities

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    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.

  2. 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.

  3. Semi-synthetic salinomycin analogs exert cytotoxic activity against human colorectal cancer stem cells.

    Science.gov (United States)

    Klose, Johannes; Kattner, Sarah; Borgström, Björn; Volz, Claudia; Schmidt, Thomas; Schneider, Martin; Oredsson, Stina; Strand, Daniel; Ulrich, Alexis

    2018-01-01

    Salinomycin, a polyether antibiotic, is a well-known inhibitor of human cancer stem cells. Chemical modification of the allylic C20 hydroxyl of salinomycin has enabled access to synthetic analogs that display increased cytotoxic activity compared to the native structure. The aim of this study was to investigate the activity of a cohort of C20-O-acyl analogs of salinomycin on human colorectal cancer cell lines in vitro. Two human colorectal cancer cell lines (SW480 and SW620) were exposed to three C20-O-acylated analogs and salinomycin. The impact of salinomycin and its analogs on tumor cell number, migration, cell death, and cancer stem cell specifity was analyzed. Exposure of human colorectal cancer cells to the C20-O-acylated analogs of salinomycin resulted in reduced tumor cell number and impaired tumor cell migration at lower concentrations than salinomycin. When used at higher (micromolar) concentrations, these effects were accompanied by induction of apoptotic cell death. Salinomycin analogs further expose improved activity against cancer stem cells compared to salinomycin. Copyright © 2017 Elsevier Inc. All rights reserved.

  4. Antibacterial, cytotoxicity and anticoagulant activities from Hypnea esperi and Caulerpa prolifera marine algae.

    Science.gov (United States)

    Selim, Samy; Amin, Abeer; Hassan, Sherif; Hagazey, Mohamed

    2015-03-01

    Extracts from 2 algal species (Hypnea esperi and Caulerpa prolifera) from Suez Canal region, Egypt were screened for the production of antibacterial compounds against some pathogenic bacteria. The bacteria tested included Escherichia coli, Pseudomonas aeruginosa, Salmonella typhimurium, Aeromonas hydrophila, Bacillus subtilis and Staphylococcus aureus. Algal species displayed antibacterial activity. The methanolic extracts showed variable response by producing various zones of inhibition against studied bacteria. The tested Gram-negative bacteria were less affected by studied algal extracts than Gram-positive bacteria. We determined some biopotentials properties such as cytotoxicity and anticoagulant activity of most potent algal active extracts. The secondary metabolites of only Hypnea esperi algal extract effectively prevented the blood clotting to the extent of 120 seconds. Minimum inhibitory concentration (MIC) indicated that all potent tested algal extract C inhibits Bacillus subtilis and Staphylococcus aureus. Minimum bactericidal concentration (MBC) was between 1 and 1.4mg/ml. The algal isolates from Egypt have been found showing promising results against infectious bacteria instead of some synthetic antibiotics.

  5. Role of IL-2 and interferon in the generation of natural cytotoxic activity in influenza virus-stimulated PBL cultures: analysis with the use of prednisolone

    NARCIS (Netherlands)

    Braakman, E.; Treep-van Leeuwen, P.; ten Berge, R. J.; Schellekens, P. T.; Lucas, C. J.

    1988-01-01

    We have examined the role of interleukin 2, interferon-gamma and interferon-alpha in the generation of natural cytotoxic (NC) activity and cytotoxic T-lymphocyte (CTL) activity in peripheral blood lymphocyte cultures stimulated with influenza virus, using the immunosuppressive effects of

  6. Anti-Candida, Anti-Enzyme Activity and Cytotoxicity of 3,5-Diaryl-4,5-dihydro-1H-pyrazole-1-carboximidamides

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    Simone Oliveira

    2014-05-01

    Full Text Available Because of the need for more effective and less harmful antifungal therapies, and interest in the synthesis of new carboximidamides, the goal of this study was to determine the antifungal and anti-enzyme activities of some new pyrazole carboximidamides and their cytotoxicity. For this purpose, tests were performed to evaluate: minimum inhibitory concentration (MIC and minimum fungicidal concentration (MFC; production of proteinases and phospholipase, and cytotoxicity of the extracts. Data were analyzed by ANOVA and Tukey Tests (α = 5%. The results were: MIC and MFC ≥ 62.5 μg/mL (C. albicans, C. parapsilosis, C. famata, C. glabrata, and Rhodotorula mucillaginosa and MIC and MFC ≥ 15.6 μg/mL (C. lipolytica. The values of proteinase and phospholipase (Pz of C. albicans before and after exposure to the compounds were: 0.6 (±0.024 and 0.2 (±0.022 and 0.9 (±0.074 and 0.3 (±0.04, respectively. These proteinase results were not significant (p = 0.69, but those of phospholipase were (p = 0.01, and 15.6 μg/mL was the most effective concentration. The cytotoxicity means were similar among the tests (p = 0.32. These compounds could be useful as templates for further development through modification or derivatization to design more potent antifungal agents. Data from this study provide evidence that these new pyrazole formulations could be an alternative source for the treatment of fungal infections caused by Candida. However, a specific study on the safety and efficacy of these in vivo and clinical trials is still needed, in order to evaluate the practical relevance of the in vitro results.

  7. 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.

  8. 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.

  9. 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®

  10. Sesquiterpenes from the Saudi Red Sea: Litophyton arboreum with their cytotoxic and antimicrobial activities.

    Science.gov (United States)

    Abou El-Kassem, Lamia T; Hawas, Usama W; El-Desouky, Samy K; Al-Farawati, Radwan

    2018-01-26

    A new pseudoguaiane-type sesquiterpene named litopharbol (1) was isolated from the methanolic extract of the Red Sea soft coral Litophyton arboreum, along with known sesquiterpenoids alismol (2), alismorientol B (3), teuhetenone A (4), and calamusin I (5); steroid, 24-methyl-cholesta-5,24(28)-diene-3β-ol (6), alkyl glyceryl ether, chimyl alcohol (7); sphingolipid, erythro-N-dodecanoyl-docosasphinga-(4E,8E)-dienine (8); and nitrogenous bases, thymine (9) and thymidine (10). The structures were determined on the basis of nuclear magnetic resonance (NMR) spectroscopic (1D and 2D NMR data including heteronuclear single quantum coherence spectroscopy, heteronuclear multiple-bond correlation spectroscopy, and nuclear Overhauser effect spectroscopy) and mass spectrometric analyses. Compounds 1-5 were explored for antimicrobial activity and cancer cell line sensitivity tests. Compound 1 exhibited antibacterial activity against Bacillus cereus with a minimum inhibition concentration of 1.8 μg/mL, whereas compound 3 showed significant potent cytotoxic effect against MCF-7 (breast cancer cells) with IC50 4.32 μM.

  11. 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].

  12. 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.

  13. Composition, Cytotoxic and Antimicrobial Activities of Satureja intermedia C.A.Mey Essential Oil

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    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.

  14. 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.

  15. Cytotoxic T cells are preferentially activated in the duodenal epithelium from patients with florid coeliac disease.

    Science.gov (United States)

    Buri, Caroline; Burri, Philipp; Bähler, Peter; Straumann, Alex; Müller-Schenker, Beatrice; Birrer, Stefan; Mueller, Christoph

    2005-06-01

    Villous atrophy and increased numbers of intraepithelial T cells in duodenal biopsies represent a hallmark of coeliac disease. In the present study, an attempt has been made to define whether cytotoxic cell subsets are activated in situ in the affected mucosa of susceptible individuals early after ingestion of a gluten-containing diet. Duodenal biopsies from 11 patients with coeliac disease who repeatedly underwent endoscopic biopsy after ingestion of individually dosed amounts of gluten were used for immunohistochemistry and in situ hybridization. To identify the cell subsets expressing perforin mRNA and protein, in situ hybridization and FACS analyses were performed on cells isolated from fresh biopsies. Compared with normal mucosa, the number of intraepithelial lymphocytes containing perforin mRNA and protein increased significantly in tissue samples showing moderate or florid coeliac disease and closely paralleled the severity of morphological alteration, whereas the frequency of perforin-expressing lamina propria lymphocytes increased only moderately. Cells isolated from florid biopsies that expressed perforin mRNA and protein were preferentially T-cell receptor (TCR) alphabeta T cells. The increase in both the absolute number and the percentage of lymphocytes expressing perforin mRNA indicates in situ activation of lymphocytes within the epithelial compartment in florid coeliac disease upon ingestion of a gluten-containing diet in patients predisposed to coeliac disease. Copyright 2005 Pathological Society of Great Britain and Ireland

  16. Composition, Cytotoxic and Antimicrobial Activities of Satureja intermedia C.A.Mey Essential Oil.

    Science.gov (United States)

    Sharifi-Rad, Javad; Sharifi-Rad, Mehdi; Hoseini-Alfatemi, Seyedeh Mahsan; Iriti, Marcello; Sharifi-Rad, Majid; Sharifi-Rad, Marzieh

    2015-08-03

    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 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.

  17. Activation of Rho GTPases by Cytotoxic Necrotizing Factor 1 Induces Macropinocytosis and Scavenging Activity in Epithelial Cells

    Science.gov (United States)

    Fiorentini, Carla; Falzano, Loredana; Fabbri, Alessia; Stringaro, Annarita; Logozzi, Mariaantonia; Travaglione, Sara; Contamin, Stéphanette; Arancia, Giuseppe; Malorni, Walter; Fais, Stefano

    2001-01-01

    Macropinocytosis, a ruffling-driven process that allows the capture of large material, is an essential aspect of normal cell function. It can be either constitutive, as in professional phagocytes where it ends with the digestion of captured material, or induced, as in epithelial cells stimulated by growth factors. In this case, the internalized material recycles back to the cell surface. We herein show that activation of Rho GTPases by a bacterial protein toxin, the Escherichia coli cytotoxic necrotizing factor 1 (CNF1), allowed epithelial cells to engulf and digest apoptotic cells in a manner similar to that of professional phagocytes. In particular, we have demonstrated that 1) the activation of all Rho, Rac, and Cdc42 by CNF1 was essential for the capture and internalization of apoptotic cells; and 2) such activation allowed the discharge of macropinosomal content into Rab7 and lysosomal associated membrane protein-1 acidic lysosomal vesicles where the ingested particles underwent degradation. Taken together, these findings indicate that CNF1-induced “switching on” of Rho GTPases may induce in epithelial cells a scavenging activity, comparable to that exerted by professional phagocytes. The activation of such activity in epithelial cells may be relevant, in mucosal tissues, in supporting or integrating the scavenging activity of resident macrophages. PMID:11452003

  18. 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.

  19. Anti-Inflammatory, Antioxidant, Antibiotic, and Cytotoxic Activities of Tanacetum vulgare L. Essential Oil and Its Constituents

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    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.

  20. 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.

  1. 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.

  2. CHARACTERISTICS OF SIGNALING PATHWAYS MEDIATING A CYTOTOXIC EFFECT OF DENDRITIC CELLS UPON ACTIVATED Т LYMPHOCYTES AND NK CELLS

    Directory of Open Access Journals (Sweden)

    T. V. Tyrinova

    2012-01-01

    Full Text Available Abstract. Cytotoxic/pro-apoptogenic effects of IFNα-induced dendritic cells (IFN-DCs directed against Т-lymphocytes and NK cells were investigated in healthy donors. Using an allogenic MLC system, it was revealed that IFN-DCs induce apoptosis of both activated CD4+ and CD8+ T-lymphocytes, and NK cells. Apoptosis of CD4+ and CD8+ T-lymphocytes induced by their interaction with IFN-DCs was mediated by various signaling pathways. In particular, activated CD4+Т-lymphocytes were most sensitive to TRAIL- и Fas/ FasL-transduction pathways, whereas activated CD8+ T-lymphocytes were induced to apoptosis via TNFα-mediated pathway. PD-1/B7-H1-signaling pathway also played a distinct role in cytotoxic activity of IFNDCs towards both types of T lymphocytes and activated NK cells. The pro-apoptogenic/cytotoxic activity of IFN-DC against activated lymphocytes may be regarded as a mechanism of a feedback regulation aimed at restriction of immune response and maintenance of immune homeostasis. Moreover, upregulation of proapoptogenic molecules on DCs under pathological conditions may lead to suppression of antigen-specific response, thus contributing to the disease progression.

  3. Cytotoxic and apoptotic activities of black widow spiderling extract against HeLa cells.

    Science.gov (United States)

    Peng, Xiaozhen; Dai, Zhipan; Lei, Qian; Liang, Long; Yan, Shuai; Wang, Xianchun

    2017-06-01

    Black widow spiders contain toxic components not only in the venom glands but also in other parts of the spider body, including the legs and abdomen. Additionally, both the eggs and newborn spiderlings of the black widow spider contain venom. It is important to investigate their potential effects on cancer cells. In the present study, the effects of newborn black widow spiderling extract on human HeLa cells were evaluated in vitro . When applied at different concentrations, the total extract decreased HeLa cell viability in a dose-dependent manner, with an IC 50 value of 158 µg/ml. Flow cytometry indicated that treatment of HeLa cells with the total extract of the spiderlings induced apoptosis in HeLa cells in a dose-dependent manner and led to cell cycle arrest in the S-phase. Additionally, application of the total extract at different concentrations increased apoptosis-related caspase 3 activity in a dose-dependent manner. HeLa cells treated with the total extract appeared to be morphologically changed, exhibiting membrane blebbing, nuclear fragmentation and condensation of chromatin. Further separation and activity screening demonstrated that the cytotoxic and apoptotic activities of the total extract were attributable mainly to its high molecular mass proteins, one of which was purified and characterized to determine its anti-tumor activities on HeLa cells. The results of the present study therefore have expanded understanding regarding the effect of spider toxins on cancer cells and suggested that components of black widow spiderlings may be developed as a promising novel agent to treat cancer.

  4. 18F-fluorocholine production at Center of Nuclear Technology Development, Brazil: synthesis and in vitro cytotoxicity studies

    International Nuclear Information System (INIS)

    Costa, Flavia Mesquita

    2014-01-01

    18 F-fluorocholine ( 18 FCH) is promising biomarker for imaging of tumors using PET technology, being effective in the diagnosis of metastatic tumors and specific for the brain tumors, prostate, lung, among others. Despite already being used in some countries like France, Germany, Slovenia, Poland, Romania and Portugal, the 18 FCH is not yet produced or marketed in Brazil. This work proposed the development of a new radiopharmaceutical based on choline labeled with 18 F isotope for diagnostic PET imaging which is an increasing demand of the nuclear medicine national. It was also proposed the development of quality control assays in order to evaluate the radiopharmaceutical prior to its use in patients; in vitro test of toxicity in non-tumor cells (MRC-5), evaluating possible changes in cell proliferation caused by radiopharmaceutical impurities; and, to test the interaction's saturation of 18 FCH with the tumor cells (PC-3 and U-87) and the competition with HC-3 and DMAE, performed to characterize the efficiency of the radiotracer uptake by tumor cells that express the choline transporter CHT. 18 FCH was synthesized in two main steps, first by reaction with dibromomethane with fluoride-18, assisted by Kryptofix2.2.2, forming 18 F-fluorobromomethane ( 18 FBrCH 2 ) and, then, the 18 FBrCH 2 reacted with the second precursor DMAE generating the final product, 18 FCH. Synthesis duration was 45 minutes. 18 FCH was obtained in 4.68 - 8.32% radiochemical yield, radiochemical purity greater than 99% and it was stable for up to 8 hours after production. The tested analytical methodologies were suitable for routine use in the quality control of 18 FCH. The evaluation of the cytotoxic potential of impurities 18 FCH, by clonogenic assay, showed that at the concentrations evaluated, the components do not alter the proliferative capacity of human healthy cells. The interaction of 18 FCH with cell lines was saturable, with specific binding greater than 94%, attesting to the

  5. MDM2 antagonist Nutlin-3a potentiates antitumour activity of cytotoxic drugs in sarcoma cell lines

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    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. Sesquiterpenoids with PTP1B Inhibitory Activity and Cytotoxicity from the Edible Mushroom Pleurotus citrinopileatus.

    Science.gov (United States)

    Tao, Qiao-Qiao; Ma, Ke; Bao, Li; Wang, Kai; Han, Jun-Jie; Wang, Wen-Zhao; Zhang, Jin-Xia; Huang, Chen-Yang; Liu, Hong-Wei

    2016-05-01

    One new perhydrobenzannulated 5,5-spiroketal sesquiterpene, pleurospiroketal F (1), as well as six new modified bisabolene sesquiterpenes pleurotins A-F (2-7) were isolated from solid-state fermentation of Pleurotus citrinopileatus. The structures of compounds 1-7 were determined by NMR and MS spectroscopic analysis. The absolute configuration of 1 was determined by X-ray diffraction analysis, while the absolute configurations of 3-7 were assigned using the in situ dimolybdenum circular dichroism method and circular dichroism data comparison. Protein tyrosine phosphatase 1B plays a crucial role as a negative regulator of the insulin-dependent signal cascades. Therefore, the protein tyrosine phosphatase 1B inhibitor can be used for treating type 2 diabetes mellitus and obesity. Compounds 2 and 6 showed moderate inhibitory effects on protein tyrosine phosphatase 1B with IC50 s of 32.1 µM and 30.5 µM, respectively. The kinetic study confirmed compound 2 to be a noncompetitive inhibitor. Compounds 1-7 did not show cytotoxic activity against cancer cell lines (IC50 > 50 µM). Georg Thieme Verlag KG Stuttgart · New York.

  7. Antioxidant, Cytotoxic Activities and Total Phenolic Content of Four Indonesian Medicinal Plants

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    Waras Nurcholis

    2017-03-01

    Full Text Available The crude ethanol extracts of four Indonesian medicinal plants namely Curcuma xanthorrhiza Roxb.,Phyllanthus niruri Linn., Andrographis paniculata Ness., and Curcuma aeruginosa Roxb. wereexamined for their antioxidant (radical scavenging activity using 2, 2-diphenyl-2-picrylhydrazyl(DPPH free radical and cytotoxicity using brine shrimp lethality test (BSLT. The total phenoliccontent was used the Folin-Ciocalteu method. IC50 values for DPPH radical scavenging activityranged from 14.5 to 178.5 μg/ml, with P. niruri having the lowest value and therefore the mostpotent, and C. aeruginosa having the highest value. LC50 values for BSLT ranged from 210.3 to593.2 μg/ml, with C. xanthorrhiza and A. paniculata having the lowest and highest values,respectively. The total phenolic content of the Indonesian plants ranged from 133.0 ±3.7 to863.3±54.7 mg tannic acid equivalent per 1 g extract, with C. aeruginosa and P. niruri having thelowest and highest values, respectively. A positive correlation between free radical scavengingactivity and the content of phenolic compounds was found in the four of Indonesian medicinal plants.

  8. 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.

  9. Spectroscopic investigations, antimicrobial, and cytotoxic activity of green synthesized gold nanoparticles

    Science.gov (United States)

    Lokina, S.; Suresh, R.; Giribabu, K.; Stephen, A.; Lakshmi Sundaram, R.; Narayanan, V.

    2014-08-01

    The gold nanoparticles (AuNPs) were synthesized by using naturally available Punica Granatum fruit extract as reducing and stabilizing agent. The biosynthesized AuNPs was characterized by using UV-Vis, fluorescence, high resolution transmission electron microscopy (HRTEM), X-ray diffraction (XRD), Fourier transform infrared (FTIR) and thermogravimetric (TGA) analysis. The surface plasmon resonance (SPR) band at 585 nm confirmed the reduction of auric chloride to AuNPs. The crystalline nature of the biosynthesized AuNPs was confirmed from the HRTEM images, XRD and selected area electron diffraction (SAED) pattern. The HRTEM images showed the mixture of triangular and spherical-like AuNPs having size between 5 and 20 nm. The weight loss of the AuNPs was measured by TGA as a function of temperature under a controlled atmosphere. The biomolecules are responsible for the reduction of AuCl4- ions and the formation of stable AuNPs which was confirmed by FTIR measurement. The synthesized AuNPs showed an excellent antibacterial activity against Candida albicans (ATCC 90028), Aspergillus flavus (ATCC 10124), Staphylococcus aureus (ATCC 25175), Salmonella typhi (ATCC 14028) and Vibrio cholerae (ATCC 14033). The minimum inhibitory concentration (MIC) of AuNPs was recorded against various microorganisms. Further, the synthesized AuNPs shows an excellent cytotoxic result against HeLa cancer cell lines at different concentrations.

  10. 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.

  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. Fabrication of biodegradable Zn-Al-Mg alloy: Mechanical properties, corrosion behavior, cytotoxicity and antibacterial activities.

    Science.gov (United States)

    Bakhsheshi-Rad, H R; Hamzah, E; Low, H T; Kasiri-Asgarani, M; Farahany, S; Akbari, E; Cho, M H

    2017-04-01

    In this work, binary Zn-0.5Al and ternary Zn-0.5Al-xMg alloys with various Mg contents were investigated as biodegradable materials for implant applications. Compared with Zn-0.5Al (single phase), Zn-0.5Al-xMg alloys consisted of the α-Zn and Mg 2 (Zn, Al) 11 with a fine lamellar structure. The results also revealed that ternary Zn-Al-Mg alloys presented higher micro-hardness value, tensile strength and corrosion resistance compared to the binary Zn-Al alloy. In addition, the tensile strength and corrosion resistance increased with increasing the Mg content in ternary alloys. The immersion tests also indicated that the corrosion rates in the following order Zn-0.5Al-0.5MgAl-0.3MgAl-0.1MgAl. The cytotoxicity tests exhibited that the Zn-0.5Al-0.5Mg alloy presents higher viability of MC3T3-E1 cell compared to the Zn-0.5Al alloy, which suggested good biocompatibility. The antibacterial activity result of both Zn-0.5Al and Zn-0.5Al-Mg alloys against Escherichia coli presented some antibacterial activity, while the Zn-0.5Al-0.5Mg significantly prohibited the growth of Escherichia coli. Thus, Zn-0.5Al-0.5Mg alloy with appropriate mechanical properties, low corrosion rate, good biocompatibility and antibacterial activities was believed to be a good candidate as a biodegradable implant material. Copyright © 2016 Elsevier B.V. All rights reserved.

  13. 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.

  14. 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.

  15. Helichrysum gymnocephalum essential oil: chemical composition and cytotoxic, antimalarial and antioxidant activities, attribution of the activity origin by correlations.

    Science.gov (United States)

    Afoulous, Samia; Ferhout, Hicham; Raoelison, Emmanuel Guy; Valentin, Alexis; Moukarzel, Béatrice; Couderc, François; Bouajila, Jalloul

    2011-09-29

    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 IC(50) of 16 ± 2 mg/L. The essential oil was active against P. falciparum (IC(50) = 25 ± 1 mg/L). However, the essential oil exhibited a poor antioxidant activity in the DPPH (IC(50) value > 1,000 mg/L) and ABTS (IC(50) 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. Chemical Composition, Cytotoxic and Antibacterial Activities of the Essential Oil from the Tunisian Ononis angustissima L. (Fabaceae).

    Science.gov (United States)

    Ghribi, Lotfi; Ben Nejma, Aymen; Besbes, Malek; Harzalla-Skhiri, Fethia; Flamini, Guido; Ben Jannet, Hichem

    2016-01-01

    The chemical composition, cytotoxic and antibacterial activities of the hydrodistilled essential oil of the aerial parts of Ononis angustissima from south Tunisia has been evaluated. The oil yield was 0.04% (w/w). The chemical composition, determined by GC and GC-MS is reported for the first time. Forty-five components, accounting for 93.7% of the total oil have been identified. The oil was characterized by a high proportion of oxygenated sesquiterpenes (33.2%), followed by sesquiterpene hydrocarbons (6.3%) and apocarotenoids (10.3%). The main components of the oil were α-eudesmol (22.4%), 2-tridecanone (9.3%) and acetophenone (7.4%). The essential oil was tested for its possible cytotoxic activity towards the human cervical cell line HeLa using the MTT assay and the antibacterial activity against Pseudomonas aeruginosa, Escherichia coli, Enterococcus faecalis, Staphylococcus aureus and the clinical strain Acinetobacter sp. This oil exerted a cytotoxic activity with an IC50 of 0.53 ± 0.02 mg/mL and a significant antibacterial effect against P. aeruginosa and E. faecalis.

  17. Cytotoxicity of semiconductor nanoparticles in A549 cells is attributable to their intrinsic oxidant activity

    Energy Technology Data Exchange (ETDEWEB)

    Escamilla-Rivera, Vicente; Uribe-Ramirez, Marisela [Centro de Investigación y de Estudios Avanzados del IPN (CINVESTAV-IPN), Departamento de Toxicología (Mexico); Gonzalez-Pozos, Sirenia [CINVESTAV-IPN, Unidad de Microscopia Electrónica (LaNSE) (Mexico); Velumani, Subramaniam [CINVESTAV-IPN, Departamento de Ingeniería Eléctrica (Mexico); Arreola-Mendoza, Laura [Centro Interdisciplinario de Investigaciones y Estudios sobre Medio Ambiente y Desarrollo del Instituto Politécnico Nacional (CIIEMAD-IPN), Departamento de Biociencias e Ingeniería (Mexico); Vizcaya-Ruiz, Andrea De, E-mail: avizcaya@cinvestav.mx [Centro de Investigación y de Estudios Avanzados del IPN (CINVESTAV-IPN), Departamento de Toxicología (Mexico)

    2016-04-15

    Copper indium gallium diselenide (CIGS) and cadmium sulfide (CdS) nanoparticles (NP) are next generation semiconductors used in photovoltaic cells (PV). They possess high quantum efficiency, absorption coefficient, and cheaper manufacturing costs compared to silicon. Due to their potential for an industrial development and the lack of information about the risk associated in their use, we investigated the influence of the physicochemical characteristics of CIGS (9 nm) and CdS (20 nm) in relation to the induction of cytotoxicity in human alveolar A549 cells through ROS generation and mitochondrial dysfunction. CIGS induced cytotoxicity in a dose dependent manner in lower concentrations than CdS; both NP were able to induce ROS in A549. Moreover, CIGS interact directly with mitochondria inducing depolarization that leads to the induction of apoptosis compared to CdS. Antioxidant pretreatment significantly prevented the loss of mitochondrial membrane potential and cytotoxicity, suggesting ROS generation as the main cytotoxic mechanism. These results demonstrate that semiconductor characteristics of NP are crucial for the type and intensity of the cytotoxic effects. Our work provides relevant information that may help guide the production of a safer NP-based PV technologies, and would be a valuable resource on future risk assessment for a safer use of nanotechnology in the development of clean sources of renewable energy.

  18. The novel oral imatinib microemulsions: physical properties, cytotoxicity activities and improved Caco-2 cell permeability.

    Science.gov (United States)

    Gundogdu, Evren; Karasulu, Hatice Yesim; Koksal, Cinel; Karasulu, Ercüment

    2013-01-01

    The objective of this study was to formulate imatinib (IM) loaded to water-in-oil (w/o) microemulsions as an alternative formulation for cancer therapy and to evaluate the cytotoxic effect of microemulsions Caco-2 and MCF-7. Moreover, permeability studies were also performed with Caco-2 cells. W/o microemulsion systems were developed by using pseudo-ternary phase diagram. According to cytotoxicity studies, all formulations did not exert a cytotoxic effect on Caco-2 cells. Furthermore, all formulations had a significant cytotoxic effect on MCF-7 cells and the cytotoxic effect of M3IM was significantly more than that of other microemulsions and IM solution (p < 0.05). The permeability studies of IM across Caco-2 cells showed that permeability value from apical to basolateral was higher than permeability value of other formulations. In conclusion, the microemulsion formulations as a drug carrier, especially M3IM formulation, may be used as an effective alternative breast cancer therapy for oral delivery of IM.

  19. Studies on Cytotoxic Activity against HepG-2 Cells of Naphthoquinones from Green Walnut Husks of Juglans mandshurica Maxim.

    Science.gov (United States)

    Zhou, Yuanyuan; Yang, Bingyou; Jiang, Yanqiu; Liu, Zhaoxi; Liu, Yuxin; Wang, Xiaoli; Kuang, Haixue

    2015-08-26

    Twenty-seven naphthoquinones and their derivatives, including four new naphthalenyl glucosides and twenty-three known compounds, were isolated from green walnut husks, which came from Juglans mandshurica Maxim. The structures of four new naphthalenyl glucosides were elucidated based on extensive spectroscopic analyses. All of these compounds were evaluated for their cytotoxic activities against the growth of human cancer cells lines HepG-2 by MTT [3-(4,5-dimethylthiazo l-2-yl)-2,5 diphenyl tetrazolium bromide] assay. The results were shown that most naphthoquinones in an aglycone form exhibited better cytotoxicity in vitro than naphthalenyl glucosides with IC50 values in the range of 7.33-88.23 μM. Meanwhile, preliminary structure-activity relationships for these compounds were discussed.

  20. Secretory products from thrombin-stimulated human platelets exert an inhibitory effect on NK-cytotoxic activity

    DEFF Research Database (Denmark)

    Skov Madsen, P; Hokland, P; Hokland, M

    1987-01-01

    We have investigated the interaction between human platelets and the NK-system, with special emphasis on the action of secretory products from platelets in an NK assay with 51Cr-labelled K562 as target cells. Supernatants from thrombin-stimulated platelets added to the NK assay consistently...... decreased the NK-cytotoxicity by 40% +/- 4.3%, indicating the existence of secreted products from platelets as a source of NK-inhibiting substances. In contrast, no direct cytotoxic effect of these secretory products on the target cells (K562) was seen. Thus, normal human platelets, when stimulated...... with thrombin, are capable of secreting different, yet undefined factors, which significantly inhibit NK activity in vitro. The results also suggest that the role of products from contaminating in vitro activated platelets should be borne in mind when performing conventional NK assays. Udgivelsesdato: 1986-Oct...

  1. Influence of zinc oxide quantum dots in the antibacterial activity and cytotoxicity of an experimental adhesive resin.

    Science.gov (United States)

    Garcia, Isadora Martini; Leitune, Vicente Castelo Branco; Visioli, Fernanda; Samuel, Susana Maria Werner; Collares, Fabrício Mezzomo

    2018-06-01

    To evaluate the influence of zinc oxide quantum dots (ZnO QDs ) into an experimental adhesive resin regarding the antibacterial activity against Streptococcus mutans and the cytotoxicity against pulp fibroblasts. ZnO QDs were synthesized by sol-gel process and were incorporated into 2-hydroxyethyl methacrylate (HEMA). An experimental adhesive resin was formulated by mixing 66.6 wt.% bisphenol A glycol dimethacrylate (BisGMA) and 33.3 wt.% HEMA with a photoinitiator system as control group. HEMA containing ZnO QDs was used for test group formulation. For the antibacterial activity assay, a direct contact inhibition evaluation was performed with biofilm of Streptococcus mutans (NCTC 10449). The cytotoxicity assay was performed by Sulforhodamine B (SRB) colorimetric assay for cell density determination using pulp fibroblasts. Data were analyzed by Student's t-test (α = 0.05). The antibacterial activity assay indicated statistically significant difference between the groups (p = 0.003), with higher values of biofilm formation on the polymerized samples of control group and a reduction of more than 50% of biofilm formation on ZnO QDs group. No difference of pulp fibroblasts viability was found between the adhesives (p = 0.482). ZnO QDs provided antibacterial activity when doped into an experimental adhesive resin without cytotoxic effect for pulp fibroblasts. Thus, the use of ZnO QDs is a strategy to develop antibiofilm restorative polymers with non-agglomerated nanofillers. ZnO QDs are non-agglomerated nanoscale fillers for dental resins and may be a strategy to reduce biofilm formation at dentin/restoration interface with no cytotoxicity for pulp fibroblasts. Copyright © 2018 Elsevier Ltd. All rights reserved.

  2. Antibacterial, antidiarrhoeal, and cytotoxic activities of methanol extract and its fractions of Caesalpinia bonducella (L.) Roxb leaves

    OpenAIRE

    Billah, Muhammad Mutassim; Islam, Rafikul; Khatun, Hajera; Parvin, Shahnaj; Islam, Ekramul; Islam, SM Anisul; Mia, Akbar Ali

    2013-01-01

    Background Caesalpinia bonducella is an important medicinal plant for its traditional uses against different types of diseases. Therefore, the present study investigated the antimicrobial, antidiarrhoeal, and cytotoxic activities of the methanol extract and ethyl acetate, chloroform, and petroleum ether (pet. ether) fractions of C. bonducella leaves. Methods The antibacterial potentialities of methanol extract and its fractions of C. bonducella leaves were investigated by the disc diffusion m...

  3. Design, Synthesis, and Biological Evaluation of Isothiosemicarbazones with Antimycobacterial Activity

    Czech Academy of Sciences Publication Activity Database

    Novotná, E.; Waisser, K.; Kuneš, J.; Palát, K.; Skálová, L.; Szotáková, B.; Buchta, V.; Stolaříková, J.; Ulmann, V.; Pávová, Marcela; Weber, Jan; Komrsková, J.; Hašková, P.; Vokřál, I.; Wsól, V.

    2017-01-01

    Roč. 350, č. 8 (2017), č. článku e1700020. ISSN 0365-6233 Institutional support: RVO:61388963 Keywords : biological activity * cytotoxicity * isocitrate lyase * isothiosemicarbazone * tuberculosis Subject RIV: EE - Microbiology, Virology OBOR OECD: Microbiology Impact factor: 1.994, year: 2016

  4. Occurrence, biological activity and synthesis of drimane sesquiterpenoids

    NARCIS (Netherlands)

    Jansen, B.J.M.; Groot, de Æ.

    2004-01-01

    In this review the names, structures and occurrence of all new drimanes and rearranged drimanes, which have been published between January 1990 and January 2003 have been collected. Subjects that have been treated are biosynthesis, analysis, biological activities, with special attention to cytotoxic

  5. Antioxidant and cytotoxic activities of the essential oil and extracts of anisosciadium orientale

    International Nuclear Information System (INIS)

    Masroorbabanari, M.; Miri, R.; Firuzi, O.

    2014-01-01

    The essential oil of Anisosciadium orientale was analyzed by gas chromatography-flame ionization detector (GC-FID) and gas chromatography-mass spectrometry (GC-MS). The essential oil (EO) was rich in monoterpene hydrocarbons: terpinolene (19.7+-2.8%, 226.4+-27.6 mg/ g EO), limonene (21.0+-1.3%, 313.3+-22.9 mg/ g EO) and myrcene (5.6+-0.50 %, 65.4+-7.2 mg/ g EO); and the phenylpropanoid myristicin (30.6+-2.3%, 438.5+-40.0 mg/ g EO). The sesquiterpene germacrene D constituted 6.1+-0.8%, 91.8+-10.6 mg/ g EO of the oil. The essential oil and the plant's methanol and 80% methanol extracts were screened for antioxidant activity and total phenol content using 2, 2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging and Folin-Ciocalteu assays, respectively. The radical scavenging activity (lower IC50s; micro g EO or the plant material (PM) /ml 10-4 M DPPH solution) was positively correlated to total phenolic content expressed as mg equivalents of gallic acid (EG) in 1 g EO or in the PM (IC50 633.2+-0.2 micro g EO /ml DPPH; 8.5+-0.2 mg EG/g EO), the methanol extracts (IC50 400.0+-0.2 micro g PM /ml DPPH; 10.3+-0.5 mg EG/g PM), and 80% methanol extracts (IC50 220.0+-0 micro g PM /ml DPPH; 15.9+-0.2 mg EG/g PM), respectively. The cytotoxic activity of the essential oil was measured on 3 human cancer cell lines including K562 (human chronic myelogenous leukemia), LS180 (human colon adenocarcinoma) and MCF-7 (human breast adenocarcinoma) cells. The IC50 values of the oil on K562, LS180 and MCF-7 cells were 396.8 +-4.9, 183.2 +- 42.8 and 159.5 +-9.0 micro g/ml, respectively (mean +- SE), while the plant extracts were not active. (author)

  6. Design, Synthesis and Docking Studies of Flavokawain B Type Chalcones and Their Cytotoxic Effects on MCF-7 and MDA-MB-231 Cell Lines

    Directory of Open Access Journals (Sweden)

    Addila Abu Bakar

    2018-03-01

    Full Text Available Flavokawain B (1 is a natural chalcone extracted from the roots of Piper methysticum, and has been proven to be a potential cytotoxic compound. Using the partial structure of flavokawain B (FKB, about 23 analogs have been synthesized. Among them, compounds 8, 13 and 23 were found in new FKB derivatives. All compounds were evaluated for their cytotoxic properties against two breast cancer cell lines, MCF-7 and MDA-MB-231, thus establishing the structure–activity relationship. The FKB derivatives 16 (IC50 = 6.50 ± 0.40 and 4.12 ± 0.20 μg/mL, 15 (IC50 = 5.50 ± 0.35 and 6.50 ± 1.40 μg/mL and 13 (IC50 = 7.12 ± 0.80 and 4.04 ± 0.30 μg/mL exhibited potential cytotoxic effects on the MCF-7 and MDA-MB-231 cell lines. However, the methoxy group substituted in position three and four in compound 2 (IC50 = 8.90 ± 0.60 and 6.80 ± 0.35 μg/mL and 22 (IC50 = 8.80 ± 0.35 and 14.16 ± 1.10 μg/mL exhibited good cytotoxicity. The lead compound FKB (1 showed potential cytotoxicity (IC50 = 7.70 ± 0.30 and 5.90 ± 0.30 μg/mL against two proposed breast cancer cell lines. It is evident that the FKB skeleton is unique for anticancer agents, additionally, the presence of halogens (Cl and F in position 2 and 3 also improved the cytotoxicity in FKB series. These findings could help to improve the future drug discovery process to treat breast cancer. A molecular dynamics study of active compounds revealed stable interactions within the active site of Janus kinase. The structures of all compounds were determined by 1H-NMR, EI-MS, IR and UV and X-ray crystallographic spectroscopy techniques.

  7. Occupational Styrene Exposure Induces Stress-Responsive Genes Involved in Cytoprotective and Cytotoxic Activities

    Science.gov (United States)

    Strafella, Elisabetta; Bracci, Massimo; Staffolani, Sara; Manzella, Nicola; Giantomasi, Daniele; Valentino, Matteo; Amati, Monica; Tomasetti, Marco; Santarelli, Lory

    2013-01-01

    Objective The aim of this study was to evaluate the expression of a panel of genes involved in toxicology in response to styrene exposure at levels below the occupational standard setting. Methods Workers in a fiber glass boat industry were evaluated for a panel of stress- and toxicity-related genes and associated with biochemical parameters related to hepatic injury. Urinary styrene metabolites (MA+PGA) of subjects and environmental sampling data collected for air at workplace were used to estimate styrene exposure. Results Expression array analysis revealed massive upregulation of genes encoding stress-responsive proteins (HSPA1L, EGR1, IL-6, IL-1β, TNSF10 and TNFα) in the styrene-exposed group; the levels of cytokines released were further confirmed in serum. The exposed workers were then stratified by styrene exposure levels. EGR1 gene upregulation paralleled the expression and transcriptional protein levels of IL-6, TNSF10 and TNFα in styrene exposed workers, even at low level. The activation of the EGR1 pathway observed at low-styrene exposure was associated with a slight increase of hepatic markers found in highly exposed subjects, even though they were within normal range. The ALT and AST levels were not affected by alcohol consumption, and positively correlated with urinary styrene metabolites as evaluated by multiple regression analysis. Conclusion The pro-inflammatory cytokines IL-6 and TNFα are the primary mediators of processes involved in the hepatic injury response and regeneration. Here, we show that styrene induced stress responsive genes involved in cytoprotection and cytotoxicity at low-exposure, that proceed to a mild subclinical hepatic toxicity at high-styrene exposure. PMID:24086524

  8. Antiviral activity of viro care gz-08 against newcastle disease virus in poultry and its in-vitro cytotoxicity assay

    International Nuclear Information System (INIS)

    Rasool, M.H.; Afzal, A.M.

    2014-01-01

    Newcastle disease (ND), one of the most important disease of poultry throughout the World is caused by Newcastle Disease Virus (NDV). It is causing huge economic losses in poultry industry of Pakistan. Regardless of vaccination, other prevention and control measures are necessary to prevent ND outbreaks. Natural resources have been exploited to obtain antiviral compounds in several latest studies. In this study, the antiviral activity of Viro Care GZ-081 was checked up in-vitro, in-ovo and in-vivo. The cytotoxicity assay of the product was performed using Vero cell line. All the trials revealed that the stock solution and 1:2 dilution of GZ-08 had some antiviral activity as well as were cytotoxic. As the concentration decreased, cytotoxicity as well as antiviral activities were lost. Based on these findings, it was concluded that GZ-08 sanitizer or spray can be used as antiviral agent to clean or disinfect some non-living surfaces against different viruses in general and NDV in particular. However, in-vivo use of GZ-08 in poultry against NDV is recommended only as pre-treatment with ND vaccines as it significantly reduced morbidity and mortality as compared to the use of vaccines alone. However, further work is recommended in future on GZ-08 for its use as post-treatment of ND as well as on other antiviral compounds of natural origin to develop a novel antiviral drug against NDV in poultry. (author)

  9. Dark and Photoinduced Cytotoxic Activity of the New Chlorophyll-a Derivatives with Oligoethylene Glycol Substituents on the Periphery of Their Macrocycles

    OpenAIRE

    Yana I. Pylina; Dmitry M. Shadrin; Oksana G. Shevchenko; Olga M. Startseva; Igor O. Velegzhaninov; Dmitry V. Belykh; Ilya O. Velegzhaninov

    2017-01-01

    In the present work, we investigated the dark and photoinduced cytotoxic activity of the new chlorophyll-a derivatives which contain the substituents of oligoethylene glycol on the periphery of their macrocycles. These compounds were tested using human cell lines to estimate their potential as photosensitizers for photodynamic therapy of cancer. It was shown that all the tested compounds have expressed photoinduced cytotoxic activity in vitro. Detailed study of the biological activity of one ...

  10. The activation of autophagy protects neurons and astrocytes against bilirubin-induced cytotoxicity.

    Science.gov (United States)

    Qaisiya, Mohammed; Mardešić, Paula; Pastore, Beatrice; Tiribelli, Claudio; Bellarosa, Cristina

    2017-11-20

    Unconjugated bilirubin (UCB) neurotoxicity involves oxidative stress, calcium signaling and ER-stress. The same insults can also induce autophagy, a process of "self-eating", with both a pro-survival or a pro-apoptotic role. Our aim was to study the outcome of autophagy activation by UCB in the highly sensitive neuronal SH-SY5Y cells and in the resistant astrocytoma U87 cells. Upon treatment with a toxic dose of UCB, the conversion of LC3-I to LC3-II was detected in both cell lines. Inhibition of autophagy by E64d before UCB treatment increased SH-SY5Y cell mortality and made U87 cells sensitive to UCB. In SH-SY5Y autophagy related genes ATG8 (5 folds), ATG18 (5 folds), p62 (3 folds) and FAM 129A (4.5 folds) were induced 8h after UCB treatment while DDIT4 upregulation (13 folds) started at 4h. mTORC1 inactivation by UCB was confirmed by phosphorylation of 4EBP1. UCB induced LC3-II conversion was completely prevented by pretreating cells with the calcium chelator BAPTA and reduced by 65% using the ER-stress inhibitor 4-PBA. Pretreatment with the PKC inhibitor reduced LC3 mRNA by 70% as compared to cells exposed to UCB alone. Finally, autophagy induction by Trifluoroperazine (TFP) increased the cell viability of rat hippocampal primary neurons upon UCB treatment from 60% to 80%. In SH-SY5Y cells, TFP pretreatment blocked the UCB-induced cleaved caspase-3 protein expression, decreased LDH release from 50% to 23%, reduced the UCB-induction of HO1, CHOP and IL-8 mRNAs by 85%, 70% and 97%. Collectively these data indicate that the activation of autophagy protects neuronal cells from UCB cytotoxicity. The mechanisms of autophagy activation by UCB involves mTOR/ER-stress/PKC/calcium signaling. Copyright © 2017 Elsevier B.V. All rights reserved.

  11. Cytotoxic, trypanocidal activities and physicochemical parameters of nor-beta-lapachone-based 1,2,3-triazoles

    Energy Technology Data Exchange (ETDEWEB)

    Silva Junior, Eufranio N. da [Universidade Federal Fluminense (UFF), Niteroi , RJ (Brazil). Inst. de Quimica. Dept. de Quimica Organica; Moura, Maria Aline B. F. de [Universidade Federal de Alagoas (UFAL), Maceio, AL (Brazil). Inst. de Quimica e Biotecnologia; Pinto, Antonio V. [Universidade Federal do Rio de Janeiro (UFRJ), Rio de Janeiro, RJ (Brazil). Nucleo de Pesquisas de Produtos Naturais] (and others)

    2009-07-01

    The cytotoxicities of five nor-{beta}-lapachone-based 1,2,3-triazoles and the precursor azidonaphthoquinone were assayed against six neoplasic cancer cell lines: SF-295 (central nervous system), HCT-8 (colon), MDAMB-435 (melanoma), HL-60 (leukaemia), PC-3 (prostate) and B-16 (murine melanoma). IC{sub 50} values ranging from 0.43 to 9.48 {mu}M were obtained. 3-(4-(1-hydroxycyclohexyl)-{sup 1}H-1,2,3-triazol-1- yl)-2,2-dimethylnaphtho[1,2-b]furan-4,5-dione proved highly cytotoxic to MDAMB-435, with IC{sub 50} even lower than the one from doxorubicin (positive control). In an attempt to correlate physicochemical parameters (reduction potentials and calculated log P) with cytotoxic activity, electrochemical studies were conducted in acetate buffer, pH 4.5, using a vitreous carbon electrode and calculated log P values were obtained. Despite the absence of a structural conjugative interaction between the two systems (quinone and triazole), the heterocyclic group was found to influence the voltammetric behaviour, as indicated by anodic shifts in the reduction potentials. No correlation was found between Ep{sub Ic} and cytotoxicity. In contrast, a comparison of Ep{sub Ic} with previously reported trypanocidal activities reconfirmed the trend for higher activity coupled with better quinone electrophilicity (> Ep{sub Ic}). A leading term in the correlation of cytoxicity, despite the absence of a linear correlation, was the calculated log P: the lower the lipophilicity, the lower the cytoxicity (> IC{sub 50}). (author)

  12. p53-independent structure-activity relationships of 3-ring mesogenic compounds' activity as cytotoxic effects against human non-small cell lung cancer lines.

    Science.gov (United States)

    Fukushi, Saori; Yoshino, Hironori; Yoshizawa, Atsushi; Kashiwakura, Ikuo

    2016-07-25

    We recently demonstrated the cytotoxicity of liquid crystal precursors (hereafter referred to as "mesogenic compounds") in the human non-small cell lung cancer (NSCLC) cell line A549 which carry wild-type p53. p53 mutations are observed in 50 % of NSCLC and contribute to their resistance to chemotherapy. To develop more effective and cancer-specific agents, in this study, we investigated the structure-activity relationships of mesogenic compounds with cytotoxic effects against multiple NSCLC cells. The pharmacological effects of mesogenic compounds were examined in human NSCLC cells (A549, LU99, EBC-1, and H1299) and normal WI-38 human fibroblast. Analyses of the cell cycle, cell-death induction, and capsases expression were performed. The 3-ring compounds possessing terminal alkyl and hydroxyl groups (compounds C1-C5) showed cytotoxicity in NSCLC cells regardless of the p53 status. The compounds C1 and C3, which possess a pyrimidine at the center of the core, induced G2/M arrest, while the compounds without a pyrimidine (C2, C4, and C5) caused G1 arrest; all compounds produced caspase-mediated cell death. These events occurred in a p53-independent manner. Furthermore, it was suggested that compounds induced cell death through p53-independent DNA damage-signaling pathway. Compounds C2, C4, and C5 did not show strong cytotoxicity in WI-38 cells, whereas C1 and C3 did. However, the cytotoxicity of compound C1 against WI-38 cells was improved by modulating the terminal alkyl chain lengths of the compound. We showed the p53-indepdent structure-activity relationships of mesogenic compounds related to the cytotoxic effects. These structure-activity relationships will be helpful in the development of more effective and cancer-specific agents.

  13. Cytotoxic activity of the neurotoxin anatoxin-a on fish leukocytes in vitro and in vivo studies

    Directory of Open Access Journals (Sweden)

    Anna Rymuszka

    2012-01-01

    Full Text Available The aim of this study was to investigate the potential cytotoxic effects of different concentrations (0.01, 0.025, 0.05, 0.1 and 1 µg/ml medium of pure anato