Planta Medica International Open 2017; 4(S 01): S1-S202
DOI: 10.1055/s-0037-1608159
Poster Session
Georg Thieme Verlag KG Stuttgart · New York

Pancreatic Lipase Inhibitors from Roselle – Natural Obesity Treatment

T Buchholz
1   Department of Pharmaceutical Biology, Freie Universitaet Berlin, 14195 Berlin, Germany
,
C Görick
1   Department of Pharmaceutical Biology, Freie Universitaet Berlin, 14195 Berlin, Germany
,
G Wolber
2   Department of Medicinal and Pharmaceutical Chemistry, Freie Universitaet Berlin, 14195 Berlin, Germany
,
MF Melzig
1   Department of Pharmaceutical Biology, Freie Universitaet Berlin, 14195 Berlin, Germany
› Author Affiliations
Further Information

Publication History

Publication Date:
24 October 2017 (online)

 

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.

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[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