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The aim of the present study was to characterize the pharmacokinetic,pharmacodynamic,and efficacy profiles of ergosta-4,6,8(14),22-tetraen-3-one (ergone) from Polyporus umbellatus.The pharmacokinetic study was carried out to determine plasma concentration of ergone in rats after oral administration at a dose of 20 mg/kg.The amount of ergone in plasma was measured by HPLC/MS.The pharmacodynamic study was carried out to evaluate the diuretic effects after oral/intraperitoneal administration of 2.5,20 mg/kg of ergone.