The constituents of Anisomeles indica and their anti-inflammatory activities

Ethnopharmacological relevanceAnisomeles indica (L.) Kuntze. (Labiatae), popularly known as ‘yu-chen-tsao’, has been traditionally used as anti-inflammatory agent.Aim of the studyInvestigate the chemical constituents from the whole plants of Anisomeles indica, and evaluate their in vitro anti-inflammatory activities.ResultsThe 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-γ-stimulated macrophages. Among these, ovatodiolide (3) exhibited potent inhibition on NO, TNF-α and IL-12 enhanced production at a concentration of 5 μM, followed by pedalitin (1), scutellarein 7-O-β-d-glucuronide methyl ester (6), and acteoside (12) at 40 μM (P < 0.05). Furthermore, 2 μM of 3, and 20 μM of 1 and 6 significantly (P < 0.05) arrested the cell cycle of Con A-stimulated spleen cells at the G0/G1 stage.ConclusionThis 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 12in vitro. These compounds may account for the use of Anisomeles indica in folk medicine to treat inflammation.