目的从含有内酯环或α,β-不饱和酮基团的中药活性成分筛选出具有体外抗耐药肿瘤细胞活性的药物。方法采用MTT比色法,选择MCF-7/Adr、bel7402/5-fu、A549/taxol 3种多药耐药肿瘤细胞对13种中药活性成分进行体外抗肿瘤活性筛选。结果 10-羟基喜树碱、雷公藤甲素对3种耐药肿瘤细胞株都具有很好的抑制作用,而鬼臼毒素、地高辛和番荔枝内酯除了对肺癌耐药细胞株的抑制作用不明显之外,对其它2种耐药细胞株具有较好的抑制作用。结论该实验对于今后活性导向的化学成分分离具有一定的指导作用,10-羟基喜树碱、雷公藤甲素、鬼臼毒素、地高辛和番荔枝内酯在抑制多药耐药肿瘤方面具有较好的研究价值。 OBJECTIVE: To screen out drugs with antitumor activity against tumor cells in vitro from active ingredients of Chinese medicines containing lactone rings or α,β-unsaturated ketone groups. Methods MTT colorimetric assay was used to select three multidrug resistant tumor cells (MCF-7/Adr, bel7402/5-fu, and A549/taxol) for antitumor activity screening of 13 active ingredients of traditional Chinese medicine. Results 10-hydroxycamptothecine and triptolide had good inhibitory effects on three resistant tumor cell lines, while podophyllotoxin, digoxin and annononasin inhibited the growth of lung cancer-resistant cell lines. The effect was not obvious, but the other two kinds of drug-resistant cell lines had a good inhibitory effect. Conclusion This experiment has a certain guiding role in the separation of active-oriented chemical components in the future. 10-Hydroxycamptothecin, triptolide, podophyllotoxin, digoxigenin and annonobacte lactone have inhibitory effects on multidrug resistant tumors. Better research value.