Molecular docking prediction and in vitro studies elucidate anti-inflammatory effect of Garcinia extract against inducible nitric oxide synthase and cyclooxygenase-2 targets

Abstract

Abstract Background Garcinia is a tropical plant that has been traditionally used in medicinal folklore for its potential antioxidant, antibacterial, anti-hyperlipidemic, anti-diabetic, hepatoprotective, etc. In this study, methanolic extract of Garcinia herbal supplement (GME) and its important phytoconstituents (Garcinol and hydroxycitric acid) were evaluated for their inhibitory action against important inflammatory markers iNOS and COX-2 in lipopolysaccharide-induced RAW 264.7 cells. iNOS and COX-2 play a major role in the process of inflammation, and inhibition of these molecules will help to alleviate the inflammatory process. The cells were pre-treated with two doses of GME (115 µg/ml and 230 µg/ml); Ggarcinol (6 µM and 12 µM); hydroxycitric acid (17.5 µg/ml and 35 µg/ml) followed by stimulation with 1 µg/ml of LPS for 24 h. Results The results of the study demonstrated that Garcinia and its active components Garcinol and HCA play an important role in suppressing LPS-induced relative mRNA expression of iNOS, COX-2, and subsequent reduction in the levels of total nitric oxide and prostaglandinE2. Molecular docking analysis of Ggarcinol and HCA with iNOS and COX-2 proteins showed potent interactions with negative binding energies. Conclusions This study suggests that Garcinia possess anti-inflammatory activity thus providing a possibility for drug designing as iNOS and COX-2 inhibitor. Graphical Abstract

Keywords

• Garcinia
• Lipopolysaccharide
• Inducible nitric oxide synthase
• Cyclooxygenase-2
• Garcinol
• Hydroxycitric acid