大豆异黄酮及其衍生物的合成及抗肿瘤活性研究  

STUDIES ON THE SYNTHESIS AND ANTITUMOR ACTIVITIES OF SOYBEAN ISOFLAVONES AND THEIR DERIVATIVES

作　　者：刘澎[1] 常俊标[1] 陈荣峰[1] 谢晶曦[2] 王强[1] 

机构地区：[1]河南省科学院化学研究所,河南郑州450002 [2]中国医学科学院,中国协和医科大学药物研究所,北京100050

出　　处：《药学学报》2000年第8期583-586,共4页Acta Pharmaceutica Sinica

摘　　要：目的　合成大豆异黄酮及其衍生物 ,对其抑制肿瘤的活性进行初步评价。方法　以多元酚和取代苯乙酸衍生物为主要原料经多步合成制备了大豆异黄酮及其衍生物 ,对所得化合物用蓝染法测定了在 5 0 μg·mL-1时体外抗肝癌H2 2 瘤株活性。结果　合成了 13个脱氧安息香和 14个异黄酮化合物 ,其中 5个 (1f～ 4f ,1h)为新化合物。结论　未发现有显著的抗肿瘤活性 ,其中化合物 1d和 1g样品在 2 4h ,10 0 μg·mL-1时蓝染率分别为 5 %和 10 %。对目的物抑制肿瘤转移评价方法的研究正在进行中。AIM To synthesize soybean isoflavones and their derivatives and to evaluate their antitumor activities preliminarily. METHODS Polyhydric phenols and p-substituted phenylacetic acid derivatives were used as the major reactants to obtain the target compounds by multi-step synthesis. Their antitumor activities against hepatoma H_ 22 tumor cell were tested by trypan blue exclusion method at the concentration of 50 μg·mL -1 . RESULTS Thirteen deoxybenzoins and fourteen isoflavones were synthesized, five of them (1f～4f,1h) are new compounds. CONCLUSION None of these compounds showed distinct antitumor activity against hepatoma H_ 22 tumor cell, among these samples 1c and 1d gave the blue-stained ratio 10% and 5% at the concentration of 100 ng·mL -1 , respectively. Further study on the biological evaluation of the synthesized soybean isoflavones and their derivatives, is now underway.

关 键 词：大豆异黄酮 黄豆苷元 染料木黄酮 衍生物 

分 类 号：R914.5[医药卫生—药物化学]