The constituents of Anisomeles indica and their anti-inflammatory activities.

BACKGROUND

Anisomeles indica (L.) Kuntze. (Labiatae), popularly known as 'yu-chen-tsao', has been traditionally used as anti-inflammatory agent.

OBJECTIVE

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 CHCl(3) 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 microM, followed by pedalitin (1), scutellarein 7-O-beta-d-glucuronide methyl ester (6), and acteoside (12) at 40 microM (P<0.05). Furthermore, 2 microM of 3, and 20 microM of 1 and 6 significantly (P<0.05) arrested the cell cycle of Con A-stimulated spleen cells at the G0/G1 stage.

CONCLUSIONS

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.