Year: 2020
Type: article
Abstract: Geldanamycin (1) was isolated as a major compound from Streptomyces zerumbet W14.It was then used as a precursor to synthesize 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 compared with the cytotoxicity of compound 1.Cytotoxicity activity was evaluated against a normal cell line, and three cancer cell lines using an 3-(4, 5-Dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide (MTT) colorimetric assay.The solubility of these compounds was also determined.The solubility of compounds 2 and 3 in water was 290.69 and 348.18 µM, higher than that of compound 1 by about 1.91 and 2.29 times, respectively.Compounds 2 and 3 showed 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 human hepatocellular carcinoma cell line (HepG2) cells with IC50 values of 82.50 and 114.35 µg/ml, respectively, while the IC50 values of compound 2 against MCF-7 and HepG2 cells were 105.62 and 124.57µg/ml, respectively.The findings showed that these new geldanamycin derivatives exhibited selective cytotoxicity toward some cancer cells at a lower concentration.Therefore, future studies on these compounds could be useful for the management of some cancers.
Institution: Silpakorn University
Language: English
Subfield: Applied Microbiology and Biotechnology
Field: Immunology and Microbiology
Domain: Life Sciences
Open Access status: diamond
OpenAlex ID: W4255074899