1,2,3,4,6-penta-O-galloyl-β-D-glucose : A cholinesterase inhibitor from Terminalia chebula

Abstract

In the current era, natural products are gaining prime attention in the fields of cosmeceuticals and pharmaceuticals due to higher safety margins and biological functions, as they have a considerable amount of potential in treating different ailments. Thus, to find effective elastase and hyaluronidase inhibitors from natural resources, fifty Korean plants were screened, and the fruit of Terminalia chebula RETZIUS (Combretaceae) was selected for further structural isolation due to its potent efficacy. The methanol crude extract of the fruits showed 80% elastase and 87% hyaluronidase enzyme inhibition activities at 1 mg/mL. The crude extract, upon bioassay-directed fractionation, led to the isolation of compound 1, whose structure was found by spectral analysis to be 1,2,3,4,6-penta-O-galloyl-β-D-glucose (PGG). PGG displayed significant elastase and hyaluronidase inhibitory activities with IC50 values of 57 μg/mL and 0.86 mg/mL, respectively; also, treatment of PGG on rabbit articular chondrocytes significantly induced the type II collagen expression. Based on elastase and hyaluronidase inhibitions, and type II collagen expression, it could be suggested that PGG might have an influence on skin conditions when used cosmetically as an active anti-aging ingredient with no cytotoxicity; also, it might be beneficial in relieving painful joint conditions, and thus have relevance for treating arthritis. Therefore, it can be concluded that PGG may prove to be an active ingredient in cosmeceutical and pharmaceutical formulations, and that it definitely merits further in vivo investigations.