青蒿素及其衍生物的抗肿瘤作用

青蒿素及其衍生物在体外对多种动物和人体肿瘤细胞具有抗瘤作用 ,对移植性动物肿瘤亦有确切的抑瘤效果 ,但其具体的作用机制尚不清楚 ,调控细胞周期的某一关键性的蛋白可能是其作用的靶点 ;青蒿素及其衍生物不仅与传统化疗药不存在交叉耐药 ,而且能逆转肿瘤细胞的多药耐药现象。通过深入研究其构─效关系及抗瘤作用机制 ,可望开发出高效、低毒、价廉、广谱的抗癌新产品。

Antitumor activities of artemisinin and its derivatives

Artemisinin and its derivatives have antitumor activity both in vitro and in vivo. The detailed mechanism of antitumor activity of artemisinin derivaties has not been addressed.Some specific proteins involved in the cell cycle may be their targets.There was no cross drug-resistance between artemisinin derivatives and cytotoxic compounds used in the chemotherapy of cancer.Furthermore,artemisinin derivatives can reverse anticancer drug resistance by inhibiting the function of the glutathione S-transferases.By studying the detailed mechanism of its antitumor activity,artemisinin derivatives may become a novel,effective,and economic anticancer drug.