title: Synthesis, characterization and in vitro evaluation of a series of novel polyrotaxane-based delivery system for artesunate.
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.
authors.affiliation: Faculty of Life Science and Technology, Kunming University of Science and Technology, Kunming 650500, PR China.
authors.forename: Xiao-Shun
authors.initials: XS
authors.lastname: Gong
authors.affiliation: Faculty of Life Science and Technology, Kunming University of Science and Technology, Kunming 650500, PR China.
authors.forename: Rui-Jian
authors.initials: RJ
authors.lastname: Jiang
authors.affiliation: Faculty of Life Science and Technology, Kunming University of Science and Technology, Kunming 650500, PR China.
authors.forename: Xia-Li
authors.initials: XL
authors.lastname: Liao
authors.affiliation: Faculty of Life Science and Technology, Kunming University of Science and Technology, Kunming 650500, PR China.
authors.forename: Hu-Die
authors.initials: HD
authors.lastname: Xie
authors.affiliation: Faculty of Life Science and Technology, Kunming University of Science and Technology, Kunming 650500, PR China.
authors.forename: Xue
authors.initials: X
authors.lastname: Ma
authors.affiliation: Faculty of Life Science and Technology, Kunming University of Science and Technology, Kunming 650500, PR China.
authors.forename: Chuan-Zhu
authors.initials: CZ
authors.lastname: Gao
authors.affiliation: Faculty of Life Science and Technology, Kunming University of Science and Technology, Kunming 650500, PR China. Electronic address: yangbo6910@sina.com.
authors.forename: Bo
authors.initials: B
authors.lastname: Yang
authors.affiliation: Faculty of Chemical Engineering, Kunming University of Science and Technology, Kunming 650500, PR China. Electronic address: zhaoyulin919@sina.com.
authors.forename: Yu-Lin
authors.initials: YL
authors.lastname: Zhao
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000633:toxicity; D037621:Artemisinins / Q000008:administration & dosage* / Q000138:chemical synthesis / Q000633:toxicity; D000077332:Artesunate; D002152:Calorimetry, Differential Scanning; D045744:Cell Line, Tumor; D003110:Colonic Neoplasms / Q000378:metabolism; D003505:Cyclodextrins / Q000138:chemical synthesis* / Q000737:chemistry* / Q000633:toxicity; D016503:Drug Delivery Systems; D004341:Drug Evaluation; D006801:Humans; D008279:Magnetic Resonance Imaging; D020442:Poloxamer / Q000138:chemical synthesis* / Q000737:chemistry* / Q000633:toxicity; D043862:Rotaxanes / Q000138:chemical synthesis* / Q000737:chemistry* / Q000633:toxicity; D014961:X-Ray Diffraction
chemical_list: D000970:Antineoplastic Agents; D037621:Artemisinins; D003505:Cyclodextrins; D043862:Rotaxanes; C475673:polyrotaxane; D020442:Poloxamer; D000077332:Artesunate; C039060:artenimol
keywords: Artesunate; Characterization; Cyclodextrin; Cytotoxicity; Polyrotaxane; Synthesis