没食子酸羽扇烷醇酯的合成及其体外抗肿瘤活性

Synthesis and In Vitro Antitumor Activities of Lupanol Gallate

摘要: 在缩合剂N,N'-二环己基碳二亚胺(DCC)和催化剂4-二甲氨基吡啶(DMAP)的作用下，羽扇烷醇与过量的没食子酸在二氯甲烷中回流10 h，合成了新化合物没食子酸羽扇烷醇酯，产率为69.6%。研究了没食子酸羽扇烷醇酯体外对肿瘤细胞株A549、LAC和HepG2的抑制活性。结果表明，羽扇烷醇和顺铂作为阳性对照物，它们对上述3株肿瘤细胞株的增殖没有抑制作用，没食子酸羽扇烷醇酯对A549、LAC和HepG2的IC₅₀值分别是51.71、62.16和64.34 μM，其对肿瘤细胞株A549和LAC增殖的抑制作用不及阿霉素，而对HepG2增殖的抑制作用比阿霉素的强。

Abstract: Under the presence of N,N'-dicyclohexylcarbodiimide (DDC) as dehydrating agent and 4-dimethyl- aminopyridine (DMAP) as catalyst, lupanol was refluxed with excessive gallic acid for 10 h in di-chloromethane to give lupanol gallate as a new compound at 69.6% yield. The latter was explored for in vitro antitumor activities against A549, LAC and HepG2 cell lines. The results showed that lupanol and cisplatin as positive control compounds had no inhibitory abilities against the above three tested tumor cell lines. The IC₅₀ values of lupanol gallate against A549, LAC and HepG2 cells were 51.71 μM, 62.16 μM and 64.34 μM respectively. The antitumor activities of lupanol gallate against A549 and LAC cells were inferior to those of adriamycin, however its antitumor activity against HepG2 cell exceeded that of adriamycin.