The constituents of Anisomeles indica and their anti-inflammatory activities

Ethnopharmacological relevance: Anisomeles indica (L) Kuntze. (Labiatae), popularly known as 'yu-chen-tsao', has been traditionally used as anti-inflammatory agent. Aim of the study: Investigate the chemical constituents from the whole plants of Anisomeles indica, and evaluate their in vitro anti-inflammatory activities. Results: The combined MeOH extract was successively partitioned with CHCl3 and n-butanol. then submitted to several column chromatographic, and HPLC purification procedures which led to the isolation of one cembrane-type diterpenoid (3). two benzenoids (4 and 5), five flavonoids (1, 2,6,7 and 14), and six phenyl propanoids (8-13). The compounds 1-14 were examined for their inhibitory effects on inflammatory mediator's enhanced production from LPS/IFN-gamma-stimulated macrophages. Among these, ovatodiolide (3) exhibited potent inhibition on NO, TNF-alpha and IL-12 enhanced production at a concentration of 5 mu M, followed by pedalitin (1), scutellarein 7-O-beta-D-glucuronide methyl ester (6), and acteoside (12) at 40 mu M (P < 0.05). Furthermore, 2 mu M of 3, and 20 mu M of 1 and 6 significantly (P<0.05) arrested the cell cycle of Con A-stimulated spleen cells at the G0/G1 stage. Conclusion: This is the first report on the presence of compounds 1 and 4-13 in this plant and of the potent anti-inflammatory activity of 1, 3, 6 and 12 in vitro. These compounds may account for the use of Anisomeles indica in folk medicine to treat inflammation. (C) 2008 Elsevier Ireland Ltd. All rights reserved.