A Cleavable Self-Inclusion Conjugate with Enhanced Biocompatibility and Antitumor Bioactivity

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外文摘要：The effective encapsulation of antitumor drugs by dynamic host-guest interactions at the submicromo-lar level remains a challenge.Herein,we report a cleavable self-inclusion camptothecin-cucurbit[7]uril(CPT-CB[7])conjugate.The binding affinity of CB[7]to CPT is greatly enhanced owing to the intramolecu-lar self-inclusion,demonstrating a concentration-independent encapsulation efficiency of nearly 100％.The disulfide linker of CPT-CB[7]conjugate can be cleaved in the reductive tumor microenviron-ment,transforming the self-inclusion into a binary host-guest complexation pattern,thus releasing the CPT thoroughly.The enhanced biocompatibility and antitumor bioactivity of the cleavable self-inclusion conjugate have been confirmed by in vitro and in vivo experiments.This line of research will open new hor-izons for supramolecular drug delivery systems oper-ating in diluted and competitive conditions.

外文关键词：

supramolecule chemistrydrug deliverycucurbiturilself-inclusion

作者：

Han Wu、Tian Xia、Feilong Qi、Shan Mei、Yu Xia、Jiang-Fei Xu、Xi Zhang

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作者单位：

Key Laboratory of Organic Optoelectronics and Molecular Engineering,Department of Chemistry,Tsinghua Univer-sity,Beijing 100084

MOE Key Laboratory of Bioorganic Phosphorus Chemistry and Chemical Biology,Department of Chemistry,Tsinghua University,Beijing 100084

基金：

科技部项目国家自然科学基金中国科学院战略规划重点项目

项目编号：

2018YFA020890021821001XDB36000000

出版年：

2023

DOI：

10.31635/ccschem.022.202202410

中国化学会会刊(英文)

CSCD

ISSN：

年,卷(期)：2023.5(4)

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