Synthesis, characterization and in vitro evaluation of a series of novel polyrotaxane-based delivery system for artesunate. (14th August 2015)

• Record Type: Journal Article
• Authors: Gong, Xiao-Shun; Jiang, Rui-Jian; Liao, Xia-Li; Xie, Hu-Die; Ma, Xue; Gao, Chuan-Zhu; Yang, Bo; Zhao, Yu-Lin
• Is Part Of: Carbohydrate research. Volume 412(2015)
• Page Start: 7
• Page End: 14
• Publication Date: 2015-08-14
• Subjects: Polyrotaxane -- Cyclodextrin -- Artesunate -- Synthesis -- Characterization -- Cytotoxicity; Carbohydrates -- Periodicals; Chemistry, Organic -- Periodicals; Biochemistry -- Periodicals; Carbohydrates -- Periodicals; Chimie organique -- Périodiques; Glucides -- Périodiques; Biochemistry; Carbohydrates; Chemistry, Organic; Periodicals; Electronic journals; 507.78
• DOI: 10.1016/j.carres.2015.04.021
• Languages: English
• ISSNs: 0008-6215

Abstract

Abstract: 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. Graphical abstract: Highlights: A series of novel artesunate-polyrotaxanes (ATS-PRs) were prepared and characterized. The ATS-PRs had higher antiproliferative activities than free ATS and DHA. The ATS-PRs are potentially useful for their application on human colon cancer chemotherapies.