Abstract
Vitamin D analogs 12 and 13 having a spiro ring in the side chain, various spirostanols 18– 21, 26, 27, 29 and 37, and furostanols 34– 36 having SCN and SeCN groups at the 26 position were prepared from diosgenin 1 via (20 S,22 R,25 R)-spirost-1α,2α-epoxy-4,6-dien-3-one 19 as a key intermediate. The cytotoxic activities of these derivatives as well as 1 on scarcely P-gp-expressed HCT 116 cells and P-gp-overexpressed Hep G2 cells were examined by MTT assay. Furostanols 34 (IC 50 value: 4.9 ± 0.3 μM) and 36 (IC 50 value: 1.3 ± 0.2 μM) exhibited marked cytotoxic effects on HCT 116 cells, and spirostanol 29 (IC 50 value: 2.4 ± 0.8 μM) and furostanol 36 (IC 50 value: 2.8 ± 0.4 μM) on Hep G2 cells. Furthermore, the effects of vitamin D analog 12, spirostanol 26 and furostanol 36 on apoptosis-signaling pathways were investigated. Compounds 12 and 26 overexpressed p53 and Bax mRNAs, while compound 36 overexpressed only Bax mRNA.
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