Strategies for Solubility and Bioavailability Enhancement and Toxicity Reduction of Norcantharidin
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Published:2022-11-10
Issue:22
Volume:27
Page:7740
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ISSN:1420-3049
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Container-title:Molecules
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language:en
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Short-container-title:Molecules
Author:
Liu Qian,Sun Henglai,Li Xinyu,Sheng Huagang,Zhu Liqiao
Abstract
Cantharidin (CTD) is the main active ingredient isolated from Mylabris, and norcantharidin (NCTD) is a demethylated derivative of CTD, which has similar antitumor activity to CTD and lower toxicity than CTD. However, the clinical use of NCTD is limited due to its poor solubility, low bioavailability, and toxic effects on normal cells. To overcome these shortcomings, researchers have explored a number of strategies, such as chemical structural modifications, microsphere dispersion systems, and nanodrug delivery systems. This review summarizes the structure–activity relationship of NCTD and novel strategies to improve the solubility and bioavailability of NCTD as well as reduce the toxicity. This review can provide evidence for further research of NCTD.
Funder
Shandong Provincial Natural Science Foundation, China
Medical and Health Science and Technology Development Plan of Shandong Province, China
Subject
Chemistry (miscellaneous),Analytical Chemistry,Organic Chemistry,Physical and Theoretical Chemistry,Molecular Medicine,Drug Discovery,Pharmaceutical Science
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