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.
Keywords:
Artesunate; Characterization; Cyclodextrin; Cytotoxicity; Polyrotaxane; Synthesis.
Copyright © 2015 Elsevier Ltd. All rights reserved.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Antineoplastic Agents / chemical synthesis
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / toxicity
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Artemisinins / administration & dosage*
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Artemisinins / chemical synthesis
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Artemisinins / toxicity
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Artesunate
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Calorimetry, Differential Scanning
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Cell Line, Tumor
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Colonic Neoplasms / metabolism
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Cyclodextrins / chemical synthesis*
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Cyclodextrins / chemistry*
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Cyclodextrins / toxicity
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Drug Delivery Systems*
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Drug Evaluation*
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Humans
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Magnetic Resonance Imaging
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Poloxamer / chemical synthesis*
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Poloxamer / chemistry*
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Poloxamer / toxicity
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Rotaxanes / chemical synthesis*
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Rotaxanes / chemistry*
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Rotaxanes / toxicity
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X-Ray Diffraction
Substances
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Antineoplastic Agents
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Artemisinins
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Cyclodextrins
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Rotaxanes
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polyrotaxane
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Poloxamer
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Artesunate
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artenimol