青蒿素及其衍生物的抗肿瘤作用

青蒿的提取物青蒿素具有抗肿瘤作用。由于青蒿素难溶于水和油,几种半合成的水溶性衍生物如蒿甲醚、蒿乙醚和青蒿琥酯等便应运而生。青蒿素衍生物的主要活性代谢产物是二氢青蒿素。青蒿素及其衍生物主要通过抑制细胞增殖、诱导细胞凋亡和抑制血管生成发挥抗癌作用,对癌细胞有很强的靶向性,并可克服多药耐药,与传统化疗药无交叉耐药。因青蒿素安全低毒,有望成为新的广谱、高效、低毒的抗癌药物。

Antitumor effect of artemisinin and its derivatives

Artemisinin which is extractive of sweet wormwood has antitumor effect. Artemisinin is insoluble in oil and water,so several semi-synthetic water soluble derivatives are developed,including artemether, arteether, artesunate, and etc. Dihydroartemisinin is the main active metabolite of artemisinin derivatives. Artemisinin and its derivatives play anti-tumor roles through inhibition of proliferation, induction of apoptosis and an-ti- angiogenesis. They can selectively kill cancer cells, overcome multidrug resistance and do not encounter cross-resistance in any resistant cell lines. Known low toxicity indicates that artemisinin and its derivatives might be a promising candidate for cancer chemotherapy with wide-spectrum,high-efficiecy and low toxicity.