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姜黄素类似物的合成与抗氧化活性

Synthesis and antioxidant activity of curcumin analogs.

作者信息

Zheng Qu-Tong, Yang Ze-Hua, Yu Liu-Ying, Ren Yu-Yan, Huang Qiu-Xia, Liu Qiu, Ma Xiang-Yu, Chen Zi-Kang, Wang Zong-Bao, Zheng Xing

机构信息

a Institute of Pharmacy & Pharmacology , University of South China , Hengyang 421001 , China.

b Hunan Province Cooperative Innovation Center for Molecular Target New Drug Study , Hengyang 421001 , China.

出版信息

J Asian Nat Prod Res. 2017 May;19(5):489-503. doi: 10.1080/10286020.2016.1235562. Epub 2016 Oct 3.

DOI:10.1080/10286020.2016.1235562
PMID:27690628
Abstract

Numerous biological activities including antioxidant, antitumor, anti-inflammation, and antivirus of the natural product curcumin were reported. However, the clinical application of it was significantly limited by its instability, poor solubility, less body absorbing, and low bioavailability. This review focuses on the structure modification and antioxidant activity evaluation of curcumin. To study the structure-activity relationship (SAR), five series of curcumin analogs were synthesized and their antioxidant activity were evaluated in vitro. The results showed that electron-donating groups, especially the phenolic hydroxyl group are an essential component to improve the antioxidant activity.

摘要

已有报道称天然产物姜黄素具有多种生物活性,包括抗氧化、抗肿瘤、抗炎和抗病毒活性。然而,其临床应用因稳定性差、溶解度低、机体吸收少和生物利用度低而受到显著限制。本综述聚焦于姜黄素的结构修饰及抗氧化活性评价。为研究构效关系(SAR),合成了五个系列的姜黄素类似物,并对其体外抗氧化活性进行了评价。结果表明,供电子基团,尤其是酚羟基是提高抗氧化活性的重要组成部分。

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Synthesis and antioxidant activity of curcumin analogs.姜黄素类似物的合成与抗氧化活性
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