苦參堿來源于豆科植物苦豆子、苦參和越南槐等中藥,在結(jié)構(gòu)分類上屬于喹諾里西啶類生物堿,具有多種生物活性,其抗腫瘤活性是近年研究的熱點。苦參堿的抗腫瘤活性確切,但是強(qiáng)度不高,因此對其進(jìn)行結(jié)構(gòu)改造、提高生物利用度以提高抗腫瘤活性顯得尤為重要。綜述了目前苦參堿結(jié)構(gòu)改造及其抗腫瘤活性的研究進(jìn)展,希望有助于了解苦參堿的抗腫瘤構(gòu)效關(guān)系和指導(dǎo)抗腫瘤新藥物的研發(fā)。

Matrine is an alkaloid belonged to quinolizidine in structure which is from Sophora alopecuroides Linn., S. flavescens Alt. and S. tonkinensis Gagnep. Matrine could exhibit a variety of biological activities, especially antitumor activity in recent years. Its antitumor activity is assured, but probably weak. Thus it is necessary to do some structural modifications of it to improve the bioavailability as well as to improve the antitumor potency. This paper reviews the current progress of matrine analogs and their antitumor activities, in the hope to get insight into antitumor structure-activity relationships of matrine and also give tips to antitumor drug research and development.

天津市科技支撐計劃項目(12ZCDZSY11900);北京協(xié)和醫(yī)學(xué)院研究生創(chuàng)新基金資助項目(20131007021)