22,23-氧化豆甾烷衍生物的合成及细胞毒性评价
Synthesis and cytotoxicity evaluation of 22,23-oxygenated stigmastane derivatives.
作者信息
Misharin Alexander Yu, Mehtiev Arif R, Morozevich Galina E, Tkachev Yaroslav V, Timofeev Vladimir P
机构信息
V.N. Orekhovich Institute of Biomedical Chemistry, Russian Academy of Medical Sciences, Moscow, Russia.
出版信息
Bioorg Med Chem. 2008 Feb 1;16(3):1460-73. doi: 10.1016/j.bmc.2007.10.056. Epub 2007 Oct 22.
Starting from (22E)-3alpha,5alpha-cyclo-6beta-methoxystigmast-22-ene eighteen derivatives of (22S,23S)-22,23-oxidostigmastane, (22R,23R)-22,23-oxidostigmastane, and (22R,23R)-22,23-dihydroxystigmastane were synthesized and screened for cytotoxicity in human hepatoma Hep G2 cells and human breast carcinoma MCF-7 cells using MTT assay. Four compounds of this series exhibited high cytotoxicity in both cells; three compounds were selectively toxic in MCF-7 cells, one compound was toxic in Hep G2 cells, rather than in MCF-7 cells; four compounds at low concentrations increased MTT test values over the control.
以(22E)-3α,5α-环-6β-甲氧基豆甾-22-烯为起始原料，合成了(22S,23S)-22,23-氧化豆甾烷、(22R,23R)-22,23-氧化豆甾烷和(22R,23R)-22,23-二羟基豆甾烷的18种衍生物，并采用MTT法在人肝癌Hep G2细胞和人乳腺癌MCF-7细胞中对其细胞毒性进行了筛选。该系列中的4种化合物在两种细胞中均表现出高细胞毒性；3种化合物在MCF-7细胞中具有选择性毒性，1种化合物在Hep G2细胞中具有毒性，而在MCF-7细胞中无毒性；4种低浓度化合物的MTT测试值高于对照组。
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