Identification of Chromomoric Acid C-I as an Nrf2 Activator in Chromolaena odorata

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• 作者：Elke H. Heiss ; Thi Van Anh Tran ; Kristin Zimmermann ; Stefan Schwaiger ; Corina Vouk ; Barbara Mayerhofer ; Clemens Malainer ; Atanas G. Atanasov ; Hermann Stuppner ; Verena M. Dirsch
• 刊名：Journal of Natural Products
• 出版年：2014
• 出版时间：March 28, 2014
• 年：2014
• 卷：77
• 期：3
• 页码：503-508
• 全文大小：326K
• 年卷期：v.77,no.3(March 28, 2014)
• ISSN：1520-6025

文摘

Activation of nuclear factor-erythroid 2-related factor 2 (Nrf2) contributes to several beneficial bioactivities of natural products, including induction of an increased cellular stress resistance and prevention or resolution of inflammation. In this study, the potential of a crude leaf extract of Chromolaena odorata, traditionally used against inflammation and skin lesions, was examined for Nrf2 activation. Guided by an Nrf2-dependent luciferase reporter gene assay, the phytoprostane chromomoric acid C-I (1) was identified as a potent Nrf2 activator from C. odorata with a CD (concentration doubling the response of vehicle-treated cells) of 5.2 渭M. When tested at 1鈥?0 渭M, 1 was able to induce the endogenous Nrf2 target gene heme oxygenase 1 (HO-1) in fibroblasts. Between 2 and 5 渭M, compound 1 induced HO-1 in vascular smooth muscle cells (VSMC) and inhibited their proliferation in a HO-1-dependent manner, without eliciting signs of cytotoxicity.