Self-defensive nano-assemblies from camptothecin-based antitumor drugs 5th China-Europe Symposium on Biomaterials in Regenerative Medicine(CESB 2015)Hangzhou,China April 7–10,2015  

作　　者：Si-Yong Qin Meng-Yun Peng Lei Rong Bin Li Shi-Bo Wang Si-Xue Cheng Ren-Xi Zhuo Xian-Zheng Zhang 

机构地区：[1]Key Laboratory of Biomedical Polymers of Ministry of Education&Department of Chemistry,Wuhan University,Wuhan 430072,People’s Republic of China [2]School of Chemistry and Materials Science,South-Central University for Nationalities,Wuhan 430074,People’s Republic of China

出　　处：《Regenerative Biomaterials》2015年第3期159-166,共8页再生生物材料（英文版）

基　　金：This work was supported by the National Natural Science Foundation of China(51125014,51233003 and 21474077);the Ministry of Science and Technology of China(2011CB606202).

摘　　要：Camptothecin(CPT)-based drugs always undergo the reversible,pH-dependent lactone ring-opening reaction,yielding the inactive but toxic carboxylate form.Self-assembly strategy provides an effective route for preserving their bio-stability.In this article,nano-sized self-assemblies from CPTbased antitumor drugs were simply built up by directly diluting the stock dimethylsulfoxide solutions of(S)-(t)-CPT,(S)-10-hydroxyl camptothecin and carboxylic CPT with water/phosphatebuffered saline solution.Because of their different molecular structures in A-ring or modification on the 20-OH group,CPT self-assembled into helical nano-ribbons,whereas 10-hydroxycamptothecin and carboxylic CPT self-aggregated into flat nano-ribbons and cylindric nano-rods,respectively.Attractively,the self-assembly of CPT-based drugs could occur within 1 min at a low concentration of 1×10^(-5)M.Adopting the J-type self-aggregation,self-assemblies were stable in aqueous solution and could effectively protect the CPT-based drugs from hydrolysis,which thereby kept their bioactivity for tumor therapy.

关 键 词：self-assembly camptothecin(CPT)-based drugs morphology hydrolysis 

分 类 号：O62[理学—有机化学]