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选择10种番荔枝内酯类化合物对耐紫杉醇肺癌细胞A549/Taxol的活性,并分析其构效关系。采用MTT比色法,检测10种番荔枝内酯类化合物和阳性药对A549/Taxol细胞的抑制活性,分别为uvariamicin-Ⅲ(1),uvariamicin-Ⅱ(2),annosquacin D(3),desacetyluvaricin(4),annosquatin A(5),squamostatin D(6),bullatacin(7),squamocin(8),motrilin(9),annosquatin B(10),维拉帕米和顺铂。番荔枝内酯类化合物对A549/Taxol细胞有很好的抑制作用,且抑制活性比阳性药维拉帕米和顺铂强。番荔枝内酯类化合物中的四氢呋喃环与内酯环之间的碳数越长,化合物的活性越强;在邻双四氢呋喃型番荔枝内酯类化合物中,链上含有2个羟基的化合物的活性强于链上含有3个羟基的;在间双四氢呋喃型番荔枝内酯类化合物中,链上含有3个羟基的活性强于链上含有4个羟基的。
Ten kinds of annona ester compounds were selected for the activity of paclitaxel-resistant lung cancer A549 / Taxol cells, and their structure-activity relationship was analyzed. MTT colorimetric assay was used to detect the inhibitory activity of 10 kinds of annona and lactones on A549 / Taxol cells. The inhibitory activities of uvariamicin-Ⅲ (1), uvariamicin-Ⅱ (2), annosquacin D (3), desacetyluvaricin (4), annosquatin A (5), squamostatin D (6), bullatacin (7), squamocin (8), motrilin (9), annosquatin B (10), verapamil and cisplatin. Annona lactone compounds have a good inhibitory effect on A549 / Taxol cells, and inhibitory activity than the positive drug verapamil and cisplatin. The longer the carbon number between the tetrahydrofuran ring and the lactone ring in the annona ester compounds, the stronger the activity of the compound. In ortho-tetrahydrofuran type annona esters, the activity of a compound containing two hydroxyl groups in the chain Stronger than the chain containing three hydroxyl groups; in inter-tetrahydrofuran-type annona lactones, the chain contains three hydroxyl groups stronger than the chain contains four hydroxyl groups.