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首页> 外文期刊>Bioorganic and Medicinal Chemistry Letters >Cytotoxic activity of butane type of 1,7-seco-2,7′-cyclolignanes and apoptosis induction by Caspase 9 and 3
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Cytotoxic activity of butane type of 1,7-seco-2,7′-cyclolignanes and apoptosis induction by Caspase 9 and 3

机译：1,7-seco-2,7'-cyclolignanes型丁烷的细胞毒活性和Caspase 9和3诱导的凋亡

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摘要

All stereoisomers of methoxybutane and fluorobutane type of 1,7-seco-2,7′-cyclolignane were synthesized and cytotoxic activities of these compounds were compared with those of all stereoisomers of butane and butanol type compounds. Both enantiomers of butane type secocyclolignane showed higher cytotoxic activity (IC50 = 16-20 μM) than methoxy type compounds, whereas none was observed for all the stereoisomers of butanol type secocyclolignane, however, (-)-Kadangustin J showed stereospecific cytotoxic activity (IC50 = 47-67 μM). Since (R)-9′-fluoro derivative 23 was most potent (IC50 = 19 μM) among the corresponding fluoro stereoisomers, (R)-9′-alkyl derivatives were synthesized, hydrophobic 9′-heptyl derivative 27 showing highest activity (IC50 = 3.7 μM against HL-60, IC50 = 3.1 μM against HeLa) in this experiment. Apoptosis induction caused by Caspase 3 and 9 for (R)-9′-heptyl derivative 27 was observed in the research on the mechanism. A degradation of DNA into small fragments was also shown by DNA ladder assay.
机译：合成了所有甲氧基丁烷和氟丁烷类型的1,7-seco-2,7'-cyclolignane立体异构体，并将这些化合物的细胞毒性与丁烷和丁醇类化合物的所有立体异构体进行了比较。丁烷型癸二环戊烷的两种对映体均显示出比甲氧基型化合物更高的细胞毒活性（IC50 = 16-20μM），而丁醇型七环戊烷的所有立体异构体均未观察到，但是（-）-Kadangustin J表现出立体特异性的细胞毒活性（IC50 = 47-67μM）。由于在相应的氟立体异构体中（R）-9'-氟衍生物23最有效（IC50 = 19μM），因此合成了（R）-9'-烷基衍生物，因此疏水性9'-庚基衍生物27表现出最高的活性（IC50相对于HL-60为3.7μM，针对HeLa的IC50为3.1μM）。在机理研究中，观察到了胱天蛋白酶3和9引起的（R）-9'-庚基衍生物27的凋亡诱导。 DNA阶梯分析也显示了DNA降解成小片段的情况。

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