Anti-inflammatory principles from Heritiera littoralis bark

Compounds from the hexane, dichloromethane and acetone extracts of Heritiera littoralis bark were investigated for their nitric oxide (NO) inhibitory effects using RAW264.7 macrophage cells. The result indicated that ergosterol peroxide (13) exhibited the highest activity against NO release with an IC(50) value of 2.5 mu M, followed by 6-alpha-hydroxystigmast-4-en-3-one (11, IC(50) = 9.5 mu M) and stigmast-4-en-3-one (9. IC(50) = 15.9 mu M), whereas other compounds showed moderate and mild effects (25.4- > 100 mu M). Ergosterol peroxide (13) and 6-alpha-hydroxystigmast-4-en-3-one (11) were also tested against prostaglandin E(2) (PGE(2)) and tumor necrosis factor alpha (TNF-alpha) releases. It was found that ergosterol peroxide (13) possessed marked activity against PGE(2) release with an IC(50) value of 28.7 mu M, while 6-alpha-hydroxystigmast-4-en-3-one (11) was 86.7 mu M. However, these two compounds were inactive towards TNF-alpha release (IC(50) > 100 mu M). The mechanism in transcriptional level of ergosterol peroxide (13) was found to down regulate mRNA expressions of iNOS and COX-2 in dose-dependent manners. (C) 2010 Elsevier GmbH. All rights reserved.