Open AccessIdentification of Chromomoric Acid C-I as an Nrf2 Activator in Chromolaena odorata
Author(s) -
Elke H. Heiss,
Trần Thị Vân Anh,
Kristin Zimmermann,
Stefan Schwaiger,
Corina Vouk,
Barbara Mayerhofer,
Clemens Malainer,
Atanas G. Atanasov,
Hermann Stuppner,
Verena M. Dirsch
Publication year - 2014
Publication title -
journal of natural products
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.976
H-Index - 139
eISSN - 1520-6025
pISSN - 0163-3864
DOI - 10.1021/np400778m
Subject(s) - chromolaena odorata , activator (genetics) , cytotoxicity , heme oxygenase , heme , inflammation , endogeny , chemistry , biology , biochemistry , in vitro , microbiology and biotechnology , gene , botany , enzyme , immunology , weed
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 μM. When tested at 1-10 μM, 1 was able to induce the endogenous Nrf2 target gene heme oxygenase 1 (HO-1) in fibroblasts. Between 2 and 5 μM, 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.