含非甾体抗炎药的姜黄素衍生物的合成及其抗炎活性的生物学评价
Synthesis and biological evaluation of curcumin derivatives containing NSAIDs for their anti-inflammatory activity.
作者信息
Liu Wenfeng, Li Yonlian, Yue Yuan, Zhang Kun, Chen Qian, Wang Huaqian, Lu Yujing, Huang Mou-Tuan, Zheng Xi, Du Zhiyun
机构信息
Laboratory of Natural Medicinal Chemistry & Green Chemistry, Faculty of Light Industry and Chemical Engineering, Guangdong University of Technology, Guangzhou 510006, China.
Guangdong Industry Technical College, Guangzhou 510300, China.
出版信息
Bioorg Med Chem Lett. 2015 Aug 1;25(15):3044-51. doi: 10.1016/j.bmcl.2015.04.077. Epub 2015 May 11.
Oral administration of nonsteroidal anti-inflammatory drugs (NSAIDs) was frequently associated with serious adverse effects. Inspired by curcumin-a naturally traditional Chinese medicine, a series of curcumin derivatives containing NSAIDs, used for transdermal application, were synthesized and screened for their anti-inflammatory activities in vitro and in vivo. Compared with curcumin and parent NSAID (salicylic acid and salsalate), topical application of A11 and B13 onto mouse ear edema, prior to TPA treatment markedly suppressed the expression of IL-1β, IL-6 and TNF-α, respectively. Mechanistically, A11 and B13 blocked the phosphorylation of IκBα and suppressed the activation of p65 and IκBα. It was found that A11 and B13 may be potent anti-inflammatory agents for the treatment of inflammatory diseases.
口服非甾体抗炎药（NSAIDs）常常伴有严重的不良反应。受姜黄素（一种天然的传统中药）启发，合成了一系列含NSAIDs的姜黄素衍生物用于经皮给药，并对其体外和体内抗炎活性进行了筛选。与姜黄素和母体NSAIDs（水杨酸和双水杨酯）相比，在TPA处理前将A11和B13局部应用于小鼠耳部水肿，分别显著抑制了IL-1β、IL-6和TNF-α的表达。从机制上讲，A11和B13阻断了IκBα的磷酸化并抑制了p65和IκBα的激活。研究发现，A11和B13可能是治疗炎症性疾病的有效抗炎剂。
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