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Identification of chromomoric acid C-I as an Nrf2 activator in Chromolaena odorata.


ABSTRACT: 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 ?M. When tested at 1-10 ?M, 1 was able to induce the endogenous Nrf2 target gene heme oxygenase 1 (HO-1) in fibroblasts. Between 2 and 5 ?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.

SUBMITTER: Heiss EH 

PROVIDER: S-EPMC3971763 | biostudies-literature | 2014 Mar

REPOSITORIES: biostudies-literature

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Identification of chromomoric acid C-I as an Nrf2 activator in Chromolaena odorata.

Heiss Elke H EH   Tran Thi Van Anh TV   Zimmermann Kristin K   Schwaiger Stefan S   Vouk Corina C   Mayerhofer Barbara B   Malainer Clemens C   Atanasov Atanas G AG   Stuppner Hermann H   Dirsch Verena M VM  

Journal of natural products 20140129 3


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 chromomori  ...[more]

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