SYNTHESIS AND CYTOTOXICITY OF POLYHYDROXYLATED CHOLESTEROL DERIVATIVES

Thu Thuy Thi Tran, Ha Thi Dinh, Phương Lan Doan, Long Quoc Pham, Quang Dai Ngo

Abstract


Eight polyhydroxylated cholesterol derivatives (1-8) were prepared from cholesterol, using oxidative reagents as SeO2, OsO4/NMO, HCOOH/H2O2 and BH3/ H2O2. Their structures were elucidated by using physical methods including NMR 1D and 2D. These compounds were evaluated against two cancer cell lines (Hep-G2, T98). Compounds 2, 4 and 8 inhibits human hepatocellular carcinoma cell line (Hep-G2) with IC50 4.69, 4.98 and 2.89 µg/mL, respectively. In addition, compound 8 exhibited strong cytotoxicity against T98 cell line (glioblastoma) with IC50 = 2.28 μM.


Keywords


cholesterol, cytotoxicity, polyhydroxylated derivative

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DOI: https://doi.org/10.15625/2525-2518/56/4/11710

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Published by Vietnam Academy of Science and Technology