个人信息Personal Information
副教授
硕士生导师
性别:男
毕业院校:中科院大连化学物理研究所
学位:博士
所在单位:化工学院
学科:药物化学. 药物工程
办公地点:大连理工大学西部校区
联系方式:Office telephone:84986200
电子邮箱:wangss@dlut.edu.cn
Synergistic antiproliferative effect of chemo-phototherapy: Synthesis and photodynamic activity evaluation of novel Chlorin e6-artesunate conjugates as antiproliferative agents
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论文类型:期刊论文
发表时间:2017-10-01
发表刊物:BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
收录刊物:Scopus、SCIE、PubMed
卷号:27
期号:19
页面范围:4548-4551
ISSN号:0960-894X
关键字:Chlorin e6; Artesunate; Photosensitizer; Reactive oxygen species; Synergistic antiproliferative effect
摘要:In order to increase the photodynamic effect of Chlorin e6, four Chlorin e6-artesunate conjugates were designed and synthesized. Among them, three conjugates (3, 6, 9) contained single artesunate side chain at 152, 173 and 131 of Chlorin e6, respectively, and one conjugate (11) contained three artesunate side chains. In the in vitro evaluation of photodynamic effect, the four conjugates showed more potent phototoxicity against HepG2 cells than Chlorin e6. The introduction of artesunate side chain significantly increased the intracellular ROS production, although the production of singlet oxygen was not improved. Compound 11 exhibited much more potent phototoxicity than the other conjugates because the three artesunate side chains greatly enhanced the ROS production and cellular uptake. The results demonstrated that the conjugation of Chlorin e6 and artesunate could accomplish synergistic effects of chemo-phototherapy, and finally enhanced their antiproliferative effects. (C) 2017 Elsevier Ltd. All rights reserved.
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