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目的:通过观察冷蒿中分离纯化的五种倍半萜内酯化合物对人子宫颈肿瘤细胞、人脑神经胶质瘤细胞、人肝癌细胞和人黑色素瘤细胞生长的影响,探讨这五种倍半萜内酯化合物的体外抑制人肿瘤细胞增殖作用,以及化合物结构与活性之间的构效关系。方法:利用四唑盐(MTT)比色法检测五种倍半萜内酯化合物对人肿瘤细胞增殖活性的影响。结果:去氢-姜黄烯(1)对子宫颈肿瘤细胞、人脑神经胶质瘤细胞、人肝癌细胞和人和色素瘤细胞的增殖均有明显的抑制作用,IC50分别为7.90 mol/L、37.78mol/L、22.50 mol/L和20.76 mol/L。二氢去氢木香内酯对各种实验用肿瘤细胞的增殖显示中等程度的抑制活性,其他三种试验用倍半萜内酯即使在100 mol/L的高浓度下,对四种肿瘤细胞的增殖不显示抑制活性。结论:实验结果初步推测,不饱和内酯是抑制肿瘤细胞增殖活性的必需基团,而环上的取代基对于抑制人肿瘤细胞增殖活性也有一定的影响。
OBJECTIVE: To observe the effect of five sesquiterpene lactones isolated and purified from Artemisia frigida on the growth of human cervical carcinoma cells, human glioma cells, human hepatoma cells and human melanoma cells, The inhibitory effect of the sesquiterpene lactones on the proliferation of human tumor cells in vitro and the structure-activity relationship between the structure and activity of the compounds. Methods: The effects of five sesquiterpene lactones on the proliferation of human tumor cells were assayed by MTT assay. Results: Dehydro-curcumin (1) significantly inhibited the proliferation of cervical cancer cells, human glioma cells, human hepatocellular carcinoma cells and human and pigmented tumor cells with IC50 of 7.90 mol / L, 37.78 mol / L, 22.50 mol / L and 20.76 mol / L. Dihydromodendrones showed moderate inhibitory activity on proliferation of various experimental tumor cells. The other three experiments showed that even at a high concentration of 100 mol / L, the sesquiterpene lactones inhibited the proliferation of four tumor cells The proliferation did not show inhibitory activity. CONCLUSION: The preliminary results suggest that unsaturated lactones are essential for inhibiting the proliferation activity of tumor cells, while the substituents on the ring also have some effects on inhibiting the proliferation of human tumor cells.