Gong Xiao-Shun, Jiang Rui-Jian, Liao Xia-Li, Xie Hu-Die, Ma Xue, Gao Chuan-Zhu, Yang Bo, Zhao Yu-Lin
Faculty of Life Science and Technology, Kunming University of Science and Technology, Kunming 650500, PR China.
Faculty of Life Science and Technology, Kunming University of Science and Technology, Kunming 650500, PR China.
Carbohydr Res. 2015 Aug 14;412:7-14. doi: 10.1016/j.carres.2015.04.021. Epub 2015 May 5.
A series of novel artesunate-polyrotaxanes (ATS-PRs) with folic acid capped, in which artesunate (ATS) was covalently bound to a cyclodextrin (CD) of the polyrotaxane (PR), were synthesized and were characterized by NMR, XRD, TG and DSC. The cytotoxicities of ATS-PRs on human colon cancer cell lines HT-29, SW480, HTC116 and DLD-1 showed that their antitumor activities were better than that of artesunate (ATS) and dihydroartemisinin (DHA). These ATS-PRs may provide a useful approach to the development of a highly effective drug candidate for the chemotherapy of human colon cancer.
合成了一系列叶酸封端的新型青蒿琥酯-聚轮烷（ATS-PRs），其中青蒿琥酯（ATS）与聚轮烷（PR）的环糊精（CD）共价结合，并通过核磁共振（NMR）、X射线衍射（XRD）、热重分析（TG）和差示扫描量热法（DSC）对其进行了表征。ATS-PRs对人结肠癌细胞系HT-29、SW480、HTC116和DLD-1的细胞毒性表明，它们的抗肿瘤活性优于青蒿琥酯（ATS）和双氢青蒿素（DHA）。这些ATS-PRs可能为开发用于人类结肠癌化疗的高效候选药物提供一种有用的方法。
