Screening for anti-lipase properties of 37 traditional Chinese medicinal herbs.
BACKGROUND
To find new, crude anti-obesity drugs from natural sources through the inhibition of adsorption of dietary lipids, in vitro porcine pancreatic lipase (PPL; triacylglycerol lipase, EC 3.1.1.3) inhibitory tests were carried out on selected plants with weight-reducing or related potential, used in Chinese traditional medicine.


METHODS
The methanolic extracts of 37 traditional Chinese herbal medicines of different families were assayed for their in vitro activity against PPL by using spectrophotometry with 2,4-dinitrophenyl butyrate as a synthetic substrate. Coexistent phytochemicals, or those present in high levels, in the 3 most promising Chinese herbs were tested for their anti-lipase activity.


RESULTS
Extracts from 2 herbs, Prunella vulgaris L. (Labiatae) and Rheum palmatum L. (Polygonaceae), at a concentration of 200 mg/mL, significantly inhibited PPL-by 74.7% and 53.8%, respectively. Quercetin exhibited better activity (27.4%) than all the other phytochemicals at a final concentration of 25 mg/mL in the assay system, followed by luteolin, with an activity of 17.3%.


CONCLUSIONS
The results support the view that herbs represent a rich source of anti-lipase compounds. The screening of the methanolic extracts of 37 Chinese medicinal plants in vitro led to the identification of several extracts with potential activity against PPL, in particular, P. vulgaris and R. palmatum. We also found that several monomeric chemicals in these herbs exhibited good or moderate activity against PPL. To the best of our knowledge, these traditional Chinese herbal medicines or phytochemicals have not been previously screened for their lipase inhibitory activity.
Zheng
Cheng-Dong
CD
Research Centre for Natural Medicinal Chemistry, College of Science, Yangling, Shaanxi, China.
Duan
Ya-Qing
YQ
Gao
Jin-Ming
JM
Ruan
Zhi-Gang
ZG
D004353:Drug Evaluation, Preclinical; D004365:Drugs, Chinese Herbal / Q000032:analysis / Q000494:pharmacology*; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D008049:Lipase / Q000037:antagonists & inhibitors*; D008516:Medicine, Chinese Traditional
D004365:Drugs, Chinese Herbal; D004791:Enzyme Inhibitors; D008049:Lipase