Potential lipase inhibitors from Chinese medicinal herbs.
BACKGROUND
Obesity has become a major health concern, and it places both personal and economic burdens on the world's population. Traditional Chinese medicinal herbs are rich source of lead compounds and are possible drug candidates, which may be used to treat this condition.


OBJECTIVE
This study screened potent pancreatic lipase inhibitors found in traditional Chinese medicinal herbs for ability to treat obesity.


METHODS
A porcine pancreatic lipase inhibition assay was established, and the inhibitory activity of 35 traditional Chinese medicinal herbs was evaluated at a concentration of 200 μg/mL. Two elutions of herbal extracts with strong lipase inhibitory activity were further fractionated by preparative high-performance liquid chromatography into 22 sub-fractions each, and these sub-fractions were tested for anti-lipase activity. Sub-fractions, which exhibited strong lipase inhibitory activity, were continuously fractionated into individual compounds. Two active compounds with potent anti-lipase activity were finally isolated and identified from two traditional Chinese medicinal herbs, respectively.


RESULTS
Among 35 traditional Chinese medicinal herbs, the 95% ethanol elutions of Panax notoginseng (Burk.) F.H. Chen (Araliaceae) and Magnolia officinalis Rehd. et Wils (Magnoliaceae) showed strong anti-lipase activity. Two compounds, including 20(S)-ginsenoside Rg3 and honokiol were identified using bioactivity-guided isolation with IC50=33.7 and 59.4 μg/mL, respectively.


CONCLUSIONS
20(S)-ginsenoside Rg3 and honokiol might be suitable candidates for the treatment of obesity.
a State Key Laboratory of New-Tech for Chinese Medicine Pharmaceutical Process , Jiangsu Kanion Pharmaceutical Co Ltd , Lianyungang , P.R. China.
Hongqiang
H
Fei
a State Key Laboratory of New-Tech for Chinese Medicine Pharmaceutical Process , Jiangsu Kanion Pharmaceutical Co Ltd , Lianyungang , P.R. China.
Mengxuan
M
Li
a State Key Laboratory of New-Tech for Chinese Medicine Pharmaceutical Process , Jiangsu Kanion Pharmaceutical Co Ltd , Lianyungang , P.R. China.
Wenjun
W
Liu
a State Key Laboratory of New-Tech for Chinese Medicine Pharmaceutical Process , Jiangsu Kanion Pharmaceutical Co Ltd , Lianyungang , P.R. China.
Lin
L
Sun
a State Key Laboratory of New-Tech for Chinese Medicine Pharmaceutical Process , Jiangsu Kanion Pharmaceutical Co Ltd , Lianyungang , P.R. China.
Na
N
Li
a State Key Laboratory of New-Tech for Chinese Medicine Pharmaceutical Process , Jiangsu Kanion Pharmaceutical Co Ltd , Lianyungang , P.R. China.
Liang
L
Cao
a State Key Laboratory of New-Tech for Chinese Medicine Pharmaceutical Process , Jiangsu Kanion Pharmaceutical Co Ltd , Lianyungang , P.R. China.
Zhaoqing
Z
Meng
a State Key Laboratory of New-Tech for Chinese Medicine Pharmaceutical Process , Jiangsu Kanion Pharmaceutical Co Ltd , Lianyungang , P.R. China.
Wenzhe
W
Huang
a State Key Laboratory of New-Tech for Chinese Medicine Pharmaceutical Process , Jiangsu Kanion Pharmaceutical Co Ltd , Lianyungang , P.R. China.
Gang
G
Ding
a State Key Laboratory of New-Tech for Chinese Medicine Pharmaceutical Process , Jiangsu Kanion Pharmaceutical Co Ltd , Lianyungang , P.R. China.
Zhenzhong
Z
Wang
a State Key Laboratory of New-Tech for Chinese Medicine Pharmaceutical Process , Jiangsu Kanion Pharmaceutical Co Ltd , Lianyungang , P.R. China.
Wei
W
Xiao
D000818:Animals; D004305:Dose-Response Relationship, Drug; D004365:Drugs, Chinese Herbal / Q000302:isolation & purification / Q000494:pharmacology*; D004791:Enzyme Inhibitors / Q000302:isolation & purification / Q000494:pharmacology*; D008049:Lipase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D010946:Plants, Medicinal; D013552:Swine
D004365:Drugs, Chinese Herbal; D004791:Enzyme Inhibitors; D008049:Lipase
20(S)-ginsenoside Rg3; bioactivity-guided isolation; honokiol; obesity