The pancreatic lipase inhibitory activity of the rhizome of Alpinia officinarum (AO) and its antihyperlipidemic activity were measured. When the water extract of AO was fractionated stepwise with organic solvents, the ethyl acetate fraction exhibited the most potent inhibition. 3-Methylethergalangin was isolated from that fraction as an inhibitor of pancreatic lipase with an IC50 value of 1.3 mg/ml (triolein as a substrate). AO and its ethyl acetate fraction significantly inhibited the serum TG level in corn oil feeding-induced triglyceridemic mice, and serum triglyceride (TG) and cholesterol in Triton WR-1339-induced hyperlipidemic mice. However, this compound and the AO ethyl acetate fraction did not show hypolipidemic activity in high cholesterol diet-induced hyperlipidemic mice. The results suggest that the hypolipidemic activity of AO and 3-methylethergalangin is due to the inhibition of pancreatic lipase.
2003 The Pharmaceutical Society of Japan