B-ring-homo-tonghaosu, isolated from Chrysanthemum morifolium capitulum, acts as a peroxisome proliferator-activated receptor- γ agonist

AbstractThe capitula ofChrysanthemum morifolium andC. indicum are used to prepare Chrysanthemi Flos in traditional Japanese Kampo medicine. In our previous study, we reported on the agonistic effect of methanol extract ofC. indicum capitulum on peroxisome proliferator-activated receptor (PPAR)- γ. We further isolated (E)-tonghaosu fromC. indicum capitulum as one of the active ingredients. In the present study, we aimed to evaluate the PPAR- γ agonistic activity of a methanol extract ofC. morifolium capitulum (MCM) in which (E)-tonghaosu could not be detected. MCM exhibited PPAR- γ agonistic activity in a concentration-dependent manner, and at a dose of 100 µg/ml, it showed similar activity to pioglitazone (30 µM), a standard PPAR-γ agonist. Through activity-guided fractionation, we isolated two geometric isomers, (E)- (1) and (Z)-B-ring-homo-tonghaosu (2), as the active ingredients of MCM. Both compounds exerted concentration-dependent PPAR- γ agonistic effects, and1 had higher activity than2. At 1.4  µM,1 had similar activity to pioglitazone (30  µM), which was achieved by2 at a concentration of 140  µM. Thus,1 has the potential to become a lead compound for the drug discovery of PPAR- γ agonists. We compared the activities and the contents of (E)-, (Z)-tonghaosu,1, and2 among 13 commercial samples of Chrysanthemi Flos, including those derived from bothC. morifolium andC. indicum. Their PPAR- γ agonistic activities were not related to the contents of these c...
Source: Journal of Natural Medicines - Category: Drugs & Pharmacology Source Type: research