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

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

Effects of Ethanolic and Aqueous Extracts of Garcinia gardneriana Leaves in an In Vivo Experimental Model Induced by a Hyperlipidic Diet

“…After collection, the leaves were placed in an air ventilation oven at 40 °C in the laboratory of the Food Science Unit (Unical-UFMS-Campo Grande-MS-Brazil) of the Faculty of Pharmaceutical Sciences, Food and Nutrition (Facfan UFMS-Campo Grande-MS-Brazil) of the Federal University of Mato Grosso do Sul (UFMS), then ground and homogenized in a Turrax™ mixer. It was labelled and conserved in dark packages until the preparation of the extracts [ 24 ].…”

“…To date, there are no studies that show the effect of such properties; moreover, there is no evidence of the possible beneficial effect of Garcinia gardneriana (Planchon and Triana) Zappi. (Clusiaceae) [ 11 ] against obesity and its metabolic disorders [ 23 , 24 ]. Thus, the objective of this research was to evaluate the therapeutic effects of ethanolic and aqueous extracts of G. gardneriana in animals receiving a high-fat diet.…”

Binding Affinity Screening of Polyphenolic Compounds in Stachys Affinis extract (SAE) for their Potential Antioxidant and Anti- inflammatory Effects

“…This result shows that there is a significant correlation between the molecular docking results and the competitive reactivity. inflammation, and research combining molecular docking is actively in progress [30].…”