二十二碳六烯酸与10-羟基喜树碱共轭物的合成与评价
Synthesis and evaluation of a DHA and 10-hydroxycamptothecin conjugate.
作者信息
Wang Yuqiang, Li Lianfa, Jiang Wei, Larrick James W
机构信息
Institute of New Drug Research, Jinan University College of Pharmacy, Guangzhou 510632, China.
出版信息
Bioorg Med Chem. 2005 Oct 1;13(19):5592-9. doi: 10.1016/j.bmc.2005.06.039.
We have synthesized a conjugate of cis-4,7,10,13,16,19-docosahexenoic acid (DHA) and 10-hydroxycamptothecin (HCPT), DHA-HCPT. The antitumor activity of DHA-HCPT was evaluated in vitro against L1210 leukemia cells and in experimental animal tumor models including L1210 leukemia, Lewis lung carcinoma, and colon 38 adenocarcinoma. DHA-HCPT showed a greatly improved antitumor efficacy compared to HCPT.
我们合成了顺式-4,7,10,13,16,19-二十二碳六烯酸（DHA）与10-羟基喜树碱（HCPT）的偶联物，即DHA-HCPT。在体外对L1210白血病细胞以及在包括L1210白血病、Lewis肺癌和结肠38腺癌的实验动物肿瘤模型中评估了DHA-HCPT的抗肿瘤活性。与HCPT相比，DHA-HCPT显示出显著提高的抗肿瘤功效。
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