Planta Med 2015; 81 - PW_92
DOI: 10.1055/s-0035-1565716

In vitro screening of Traditional Chinese Medical (TCM) plants for pancreatic lipase and α-amylase inhibitory activities

T Buchholz 1, XY Zhang 2, 3, MF Melzig 1
  • 1Institute of Pharmacy, Department of Pharmaceutical Biology, Freie Universitaet Berlin, Berlin, Germany
  • 2College of Veterinary Medicine, Northwest A&F University, Yangling, China
  • 3College of Biological Science and Engineering, Shaanxi University of Technology, Hanzhong, China

Inhibition of digestive enzymes is one of the most widely studied mechanisms for the treatment of obesity and its associated diseases as diabetes mellitus, coronary heart diseases or sleep-breathing disorders [1, 2]. The use of plant based resources as a potential platform for discovery and development of new drugs has become a lucrative research field in this context.

For finding new compounds with pancraetic lipase (triacylglycerol acylhydrolase, EC 3.1.1.3) and α-amylase (1,4-alpha-D-glucan glucanohydrolase, EC 3.2.1.1) inhibitory activities several TCM plants have been screened. Methanolic and water extracts of the plants were evaluated. To determine the pancreatic lipase activity, an enzymatic in vitro assay based on the hydrolysis kinetic of 4-methylumbelliferyl oleate (4-MUO) was used. For the determination of α-amylase activity the fluorescence-based EnzChek® Ultra Amylase Assay Kit (Molecular Probes™) was used. This in vitro enzyme assay is based on the hydrolytic cleavage of a modified starch derivative. Methanolic extracts from Crataegus pinnatifida Bunge Var. Major N.E.Br. (Rosaceae), Rehmannia glutinosa Libosch (Plantaginaceae), Cornus officinalis Siebold & Zucc. (Cornaceae) and Dioscorea opposita Thunb. (Dioscoreaceae) showed the best inhibitory effect to both enzymes (IC50< 2.0 mg/mL). Further identification, isolation and characterization of active compounds responsible for enzyme inhibitory effects is required to evaluate the therapeutic potential of these plants.

References:

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[2] Foster-Schubert KE, Cummings DE. Emerging Therapeutic Strategies for Obesity. Endocr Rev 2006; 27: 779 – 793