Archives of Pharmacal Research

The Pharmaceutical Society of Korea (대한약학회)
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Pseudoguaianolides Isolated from Iunla britannica vats. chinenis as Inhibitory Constituents against Inducible Nitric Oxide Synthase

  • Lee, Hyun-Tai (Natural Products Chemistry Laboratory, College of Pharmacy, Ewha Womans University) ;
  • Yang, Seung-Won (College of Pharmacy ＆ Natural Products Research Institute, Seoul National Unversity) ;
  • Kim, Kyeong-Ho (College of Pharmacy, Kangwon National University) ;
  • Seo, Eun-Kyeong (Natural Products Chemistry Laboratory, College of Pharmacy, Ewha Womans University) ;
  • Mar, Woongchon (College of Pharmacy ＆ Natural Products Research Institute, Seoul National Unversity)
  • Published : 2002.04.01
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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 $IC_{50}$ value of 0.46 mM, which is about 8 times more potent than the known selective inhibitor of iNOS, $L-N^6-(1-iminoethyl)Iysine{\;}(IC_{50}{\;}3.49{\;}{\mu}M)$. 2,3-Dihydroaromaticin (2) and ergolide (3) also exhibited potent inhibitory activities on LPS-induced iNOS with $IC_{50}$ values of 1.05 and $0.69{\;}{\mu}M$, respectively.

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References

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