Pancreatic lipase-inhibiting triterpenoid saponins from fruits of Acanthopanax senticosus.
Sixteen triterpenoid saponins were isolated from the fruits of Acanthopanax senticosus, including a new compound, acanthopanaxoside E (1), which was established as 3-O-beta-D-glucuronopyranosyl echinocystic acid 28-O-beta-D-glucopyranoside on the basis of various spectroscopic analyses and chemical degradation. By using a pancreatic lipase-inhibiting assay system, the crude saponin fraction showed inhibitory activity on pancreatic lipase, which is a key enzyme in lipid digestion. Among the isolated compounds, silphioside F (2), copteroside B (3), hederagenin 3-O-beta-D-glucuronopyranoside 6'-O-methyl ester (4) and gypsogenin 3-O-beta-D-glucuronopyranoside (5) showed inhibitory activity toward pancreatic lipase with IC(50) values of 0.22, 0.25, 0.26 and 0.29 mM, respectively, and the free carboxylic acid groups in position 28 within their chemical structures were required for enhancement of pancreatic lipase inhibition.
Li
Fang
F
Faculty of Pharmaceutical Sciences, Toho University, Miyama, Funabashi, Chiba, Japan.
Li
Wei
W
Fu
Hongwei
H
Zhang
Qingbo
Q
Koike
Kazuo
K
D004353:Drug Evaluation, Preclinical; D004365:Drugs, Chinese Herbal; D028001:Eleutherococcus / Q000737:chemistry*; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D005638:Fruit / Q000737:chemistry*; D008049:Lipase / Q000037:antagonists & inhibitors* / Q000737:chemistry; D015394:Molecular Structure; D010179:Pancreas / Q000201:enzymology*; D012503:Saponins / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D014315:Triterpenes / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*
D004365:Drugs, Chinese Herbal; D004791:Enzyme Inhibitors; D012503:Saponins; D014315:Triterpenes; C522661:acanthopanaxoside E; D008049:Lipase