二十二碳六烯酸双氢青蒿素酯的合成及其抗肿瘤活性的初步研究  

Synthesis and preliminary antitumor activity evaluation of docosahexaenoic acid-dihydroartemisinin conjugate

作　　者：孟丽丽[1] 匡永清[1] 肖义军[2] 宿亮[1] 向顺[1] 谢斌[1] 

机构地区：[1]湖南大学化学化工学院,湖南长沙410082 [2]福建师范大学生命科学学院,福建福州350108

出　　处：《化学研究与应用》2009年第1期123-126,共4页Chemical Research and Application

摘　　要：Dihydroartemisinin(DQHS)is obtained by reduction of artemisinin with NaBH4 as reductant,and then DHA-DQHS is prepared by esterification of docosahexaenoic acid with dihydroartemisinin in the presence of dicyclohexylcarbodiimide(DCC)and 4-dimethylaminopyridine(DMAP).Antitumor activity of DHA-DQHS against CA46,Molt4 and P388 cells is tested by MTT method in parallel with artemisinin and dihydroartemisinin.Results show that the 1H NMR and ESI-MS of DHA-DQHS are in agreement with its chmical structure.IC50 of DHA-DQHS on CA46,Molt4 and P388 cells are 0.024,0.076 and 0.105 mg·L-1 respectively,which are significantly lower than those of artemisinin and dihydroartemisinin,the reason for that is possibly owing to the tumor-targeting property of DHA.Dihydroartemisinin（DQHS） is obtained by reduction of artemisinin with NaBH4 as reductant,and then DHA-DQHS is prepared by esterification of docosahexaenoic acid with dihydroartemisinin in the presence of dicyclohexylcarbodiimide（DCC） and 4- dimethylaminopyridine（DMAP）. Antitumor activity of DHA-DQHS against CA46, Molt4 and P388 cells is tested by MTT method in parallel with artemisinin and dihydroartemisinin. Results show that the ^1H NMR and ESI-MS of DHA-DQHS are in agreement with its chnfical structure. IC50 of DHA-DQHS on CA46,Molt4 and P388 cells are 0.024,0.076 and 0. 105 mg.L^-1 respectively, which are significantly lower than those of artemisinin and dihydroartemisinin,the reason for that is possibly owing to the tumor-targeting property of DHA.

关 键 词：青蒿素 二十二碳六烯酸 DCC/DMAP法 抗肿瘤 靶向 

分 类 号：R914.5[医药卫生—药物化学] R965.1[医药卫生—药学]