Cytotoxicity activity of geldanamycin derivatives against various cancer cell lines

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dc.contributor.authorTaechowisan, Thongchaien_US
dc.contributor.authorTipparat, Samsawaten_US
dc.contributor.authorWinyou, Puckdeeen_US
dc.contributor.authorWaya, S. Phutdhawongen_US
dc.date.accessioned2020-10-16T08:56:57Z
dc.date.available2020-10-16T08:56:57Z
dc.date.issued2020-06
dc.description.abstractGeldanamycin (1) was isolated as a major compound from Streptomyces zerumbet W14. It was then used as a precursor tosynthesize two new geldanamycins: 17-(tryptamine)-17-demethoxygeldanamycin (2) and 17-(5′-methoxytryptamine)-17-demethoxygeldanamycin (3). The cytotoxicity activity of these two new compounds was evaluated and comparedwith the cytotoxicity of compound 1. Cytotoxicity activity was evaluated against a normal cell line, and three cancercell lines using an 3-(4, 5-Dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide (MTT) colorimetric assay. Thesolubility of these compounds was also determined. The solubility of compounds 2 and 3 in water was 290.69and 348.18 µM, higher than that of compound 1 by about 1.91 and 2.29 times, respectively. Compounds 2 and 3showed moderate cytotoxic activity on Vero and human cervical carcinoma cells with IC50 values of >200.00 µg/ml. The strongest cytotoxicity of compound 3 was observed in human breast carcinoma cells (MCF-7) and humanhepatocellular carcinoma cell line (HepG2) cells with IC50 values of 82.50 and 114.35 µg/ml, respectively, while theIC50 values of compound 2 against MCF-7 and HepG2 cells were 105.62 and 124.57 µg/ml, respectively. The findingsshowed that these new geldanamycin derivatives exhibited selective cytotoxicity toward some cancer cells at a lowerconcentration. Therefore, future studies on these compounds could be useful for the management of some cancersen_US
dc.identifier.affiliationsDepartment of Microbiology, Faculty of Science, Silpakorn University, Nakhon Pathom 7300, Thailand.en_US
dc.identifier.affiliationsDepartment of Microbiology, Faculty of Science, Silpakorn University, Nakhon Pathom 7300, Thailand.en_US
dc.identifier.affiliationsDepartment of Microbiology, Faculty of Science, Silpakorn University, Nakhon Pathom 7300, Thailand.en_US
dc.identifier.affiliationsDepartment of Chemistry, Faculty of Science Silpakorn University, Nakhon Pathom 7300, Thailand.en_US
dc.identifier.citationTaechowisan Thongchai, Tipparat Samsawat, Winyou Puckdee, Waya S. Phutdhawong. Cytotoxicity activity of geldanamycin derivatives against various cancer cell lines. Journal of Applied Pharmaceutical Science. 2020 Jun; 2020 Jun: 012-021en_US
dc.identifier.issn2231-3354
dc.identifier.placeIndiaen_US
dc.identifier.urihttps://imsear.searo.who.int/handle/123456789/210764
dc.languageenen_US
dc.publisherOpen Science Publishers LLPen_US
dc.relation.issuenumber6en_US
dc.relation.volume10en_US
dc.source.urihttps://dx.doi.org//10.7324/JAPS.2020.10603en_US
dc.subjectAnticancer activityen_US
dc.subjectcancer cell linesen_US
dc.subjectcytotoxicity activityen_US
dc.subjectsolubilityen_US
dc.subjecttryptamine-geldanamycin hybridsen_US
dc.titleCytotoxicity activity of geldanamycin derivatives against various cancer cell linesen_US
dc.typeJournal Articleen_US
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