Overweight and obesity are leading risk factors for a number of chronic diseases such as diabetes mellitus type II [1,2]. Due to rapid lifestyle changes, their prevalence has increased in recent years [3].
In order to find new, plant based pancreatic lipase (PL, pancreatic triacylglycerol lipase (EC: 3.1.1.3)) inhibitors for the treatment of obesity, in vitro tests and in silico docking experiments were carried out. Initially, methanolic and aqueous extracts of 23 medicinal plants with weight-reducing, serum glucose-reducing, or related potential were investigated for anti-lipase activity in vitro. Our findings have shown that both the aqueous and methanolic extract of Hibiscus sabdariffa L. (Malvaceae) showed a very strong inhibition (IC50: 35.8 ± 0.8 µg/mL) of the enzyme. Subsequently, the methanolic extract of the plant was analyzed by HPLC and ESI-Q-TOF-MS for isolation and identification of inhibitory active compounds. Hibiscus acid and hibiscus acid glucoside were identified by comparison with literature data. In silico docking experiments of hibiscus acid to the crystal structure of porcine pancreatic lipase (PDB code: 1ETH) showed strong interactions with the active site of the enzyme.
[1] Kopelman PG. Nature 2000; 404: 635–643
[2] Trigueros L, Pena S, Ugidos AV, Sayas-Barbera E, Perez-Alvarez JA, Sendra EJ. Food Sci. Nutr. 2013; 53: 929–942
[3] World Health Organization. 2015; Factsheet 311