Pseudoguaianolides isolated from Inula britannica var. chinenis as inhibitory constituents against inducible nitric oxide synthase |
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Authors: | Lee Hyun-Tai Yang Seung-Won Kim Kyeong Ho Seo Eun-Kyoung Mar Woongchon |
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Affiliation: | Natural Products Chemistry Laboratory, College of Pharmacy, Ewha Womans University, Seoul, Korea. |
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Abstract: | Three pseudoguaianolide type sesquiterpenes, bigelovin (1), 2,3-dihydroaromaticin (2), and ergolide (3) were isolated as inhibitory constituents against inducible nitric oxide synthase (iNOS) from the flowers of Inula britannica var. chinensis. Bigelovin (1) exhibited a highly potent inhibitory activity on lipopolysaccharide (LPS)-induced iNOS in murine macrophage RAW 264.7 cells with an IC50 value of 0.46 mM, which is about 8 times more potent than the known selective inhibitor of iNOS, L-N6-(1-iminoethyl)lysine (IC50 3.49 microM). 2,3-Dihydroaromaticin (2) and ergolide (3) also exhibited potent inhibitory activities on LPS-induced iNOS with IC50 values of 1.05 and 0.69 microM, respectively. |
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Keywords: | Inula britannica var. chinensis Bigelovin 2,3-Dihydroaromaticin Ergolide iNOS inhibitor |
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