Investigations on Leucas cephalotes (Roth.) Spreng. for inhibition of LPS-induced pro-inflammatory mediators in murine macrophages and in rat model.

Silica gel column chromatography fractionation of the dichloromethane extract (LCD) of Leucas cephalotes (Roth.) Spreng. led to the isolation of five compounds namely beta-sitosterol (1) + stigmasterol (2), lupeol (3), oleanolic acid (4) and laballenic acid (5). Also, gas chromatography-mass spectrometry (GC-MS) analysis of sub-fraction (LCD-F1) of this extract showed the presence of eleven (6-16) compounds. In addition to this, 3-5 and LCD-F1 were evaluated for lipopolysachharide (LPS)-induced nitric oxide (NO), tumor necrosis factor (TNF)-alpha and interleukin (IL)-1 beta production in RAW 264.7 and J774A.1 cells. Results directed that 4 and 5 were found to inhibit these mediators at half maximal inhibitory concentration of 17.12 to 57.20 mu M while IC50 for LCD-F1 was found to be 15.56 to 31.71 mu g/mL. Furthermore, LCD at a dose of 50, 100 and 400 mg/Kg was found to reduce significantly LPS induced tumor necrosis factor (TNF)-alpha and interleukin (IL)-1 beta production in female Sprague Dawley (SD) rats. All the results findings evoked that the anti-inflammatory effects of Leucas cephalotes is partially mediated through the suppression of pro-inflammatory mediators and hence can be utilized for the development of anti-inflammatory candidates.