Flavonoids with iNOS inhibitory activity from Pogonatherum crinitum

Guei Jane Wang, Yi Min Chen, Zong-Huei Li, Ching Kuo Lee, Ke Jun Chen, Tzong Huei Lee

Research output: Contribution to journalArticle

40 Citations (Scopus)

Abstract

Pogonatherum crinitum has long been used as a folk remedy for the treatment of many inflammatory diseases in Taiwan, and till now there is still no report concerning its active principles as well as their pharmacological studies. That prompted us to investigate the bioactive constituents of Pogonatherum crinitum. Two novel chemical entities, luteolin 6-C-β-boivinopyranoside (1) and 6-trans-(2″-O-α-rhamnopyranosyl)ethenyl-5,7,3′,4′-tetrahydroxyflavone (2), along with luteolin (3), kaempferol (4), luteolin 6-C-β-fucopyranoside (5), kaempferol 3-O-α-l-rhamnopyranoside (6), luteolin 6-C-β-glucopyranoside (7), rutin (8) and kaempferol 3-O-rutinoside (9) were isolated from this plant, and identified by spectroscopic analysis. The effect of these compounds on the inhibition of NO production in LPS-activated macrophages was further evaluated. All these compounds inhibited NO production in activated RAW 264.7 cells to various degrees without affecting the cellular viability. Among the compounds examined, both compounds 1 and 2 suppressed LPS-induced NO production, with Emax values of 99.51 ± 0.23% and 92.41 ± 3.22%, respectively. The most potent compounds, 3 and 4, inhibited NO production with IC50 values of 10.41 ± 0.02 μM and 10.61 ± 0.44 μM, respectively. These effects were attributed to suppression of mRNA expression of inducible NO synthase (iNOS). Our results clearly demonstrated that these naturally occurring iNOS inhibitors may be beneficial to the treatment of inflammatory diseases associated with overproduction of NO, which provides an explanation, at least a part, for the anti-inflammatory property of Pogonatherum crinitum.

Original languageEnglish
Pages (from-to)71-78
Number of pages8
JournalJournal of Ethnopharmacology
Volume118
Issue number1
DOIs
Publication statusPublished - Jun 19 2008

Fingerprint

Flavonoids
Nitric Oxide Synthase
Luteolin
Rutin
Traditional Medicine
Taiwan
Inhibitory Concentration 50
Anti-Inflammatory Agents
Macrophages
Pharmacology
Messenger RNA
Therapeutics
luteolin 6-C-(6''-O-trans-caffeoylglucoside)
kaempferol

Keywords

  • Flavonoids
  • Gramineae
  • Inducible nitric oxide synthase
  • Nitric oxide
  • Pogonatherum crinitum

ASJC Scopus subject areas

  • Pharmacology

Cite this

Flavonoids with iNOS inhibitory activity from Pogonatherum crinitum. / Wang, Guei Jane; Chen, Yi Min; Li, Zong-Huei; Lee, Ching Kuo; Chen, Ke Jun; Lee, Tzong Huei.

In: Journal of Ethnopharmacology, Vol. 118, No. 1, 19.06.2008, p. 71-78.

Research output: Contribution to journalArticle

Wang, Guei Jane ; Chen, Yi Min ; Li, Zong-Huei ; Lee, Ching Kuo ; Chen, Ke Jun ; Lee, Tzong Huei. / Flavonoids with iNOS inhibitory activity from Pogonatherum crinitum. In: Journal of Ethnopharmacology. 2008 ; Vol. 118, No. 1. pp. 71-78.
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AB - Pogonatherum crinitum has long been used as a folk remedy for the treatment of many inflammatory diseases in Taiwan, and till now there is still no report concerning its active principles as well as their pharmacological studies. That prompted us to investigate the bioactive constituents of Pogonatherum crinitum. Two novel chemical entities, luteolin 6-C-β-boivinopyranoside (1) and 6-trans-(2″-O-α-rhamnopyranosyl)ethenyl-5,7,3′,4′-tetrahydroxyflavone (2), along with luteolin (3), kaempferol (4), luteolin 6-C-β-fucopyranoside (5), kaempferol 3-O-α-l-rhamnopyranoside (6), luteolin 6-C-β-glucopyranoside (7), rutin (8) and kaempferol 3-O-rutinoside (9) were isolated from this plant, and identified by spectroscopic analysis. The effect of these compounds on the inhibition of NO production in LPS-activated macrophages was further evaluated. All these compounds inhibited NO production in activated RAW 264.7 cells to various degrees without affecting the cellular viability. Among the compounds examined, both compounds 1 and 2 suppressed LPS-induced NO production, with Emax values of 99.51 ± 0.23% and 92.41 ± 3.22%, respectively. The most potent compounds, 3 and 4, inhibited NO production with IC50 values of 10.41 ± 0.02 μM and 10.61 ± 0.44 μM, respectively. These effects were attributed to suppression of mRNA expression of inducible NO synthase (iNOS). Our results clearly demonstrated that these naturally occurring iNOS inhibitors may be beneficial to the treatment of inflammatory diseases associated with overproduction of NO, which provides an explanation, at least a part, for the anti-inflammatory property of Pogonatherum crinitum.

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