科研之友
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摘要
The decarbonization of lignan a and dihydroindene b were synthesized through alpha-asarone by acid-catalyzed. Compounds a/b were identified by H-1 NMR, C-13 NMR, MS and elemental analysis. The effects of catalysts, solvents and temperature on yields of a/b have been evaluated. The total yield of a/b reached 98% (a: 41%, b: 57%) with HCl as catalyst and ethanol as solvent at 45 degrees C. The yield of compound a was up to 75% with AlCl3 as catalyst and ethanol as solvent at 30 degrees C, b was not formed in this condition, and the selectivity of a was 100%. When using BF3 center dot Et2O as catalyst and methylene chloride as solvent at 45 degrees C, the yield of compound a was 20% and b was formed in yield of 60%. The cytotoxic activities of two compounds against MCF-7, Bel-7402, A549 and Hela were evaluated in vitro by the MTT assay. The results indicated that compounds a/b exhibited better cytotoxic activities against four cancer cells than 5-Fu. Especially, the IC50 values of a to MCF-7 and Hela reached 120.2 and 117.3 mu mol.L-1 as well as the IC50 of b to MCF-7 and A549 reached 66.1 and 72.4 mu mol.L-1, respectively. At the same time, the concentration of a/b and time of operation to influence inhibitory activity were explored.
- 出版日期2013-9
- 单位湖南大学
