A study was conducted to investigate the inhibitory effects of Pleurospermum lindleyanum and its active components on pancreatic lipase, α-glucosidase, and angiotensin-converting enzyme. In this paper, the extract of P. lindleyanum was purified by macroporous adsorption resin, and the activity inhibition rates of P. lindleyanum and its active components against the three enzymes were determined. The results showed that the contents of five active components, chlorogenic acid, luteolin-7-O-glucoside, luteolin, bergapten, and oxypeucedanin, in the ethanol extract of P. lindleyanum were all higher than those in the aqueous extract. After purification, the contents of each active component in the purified product were significantly increased. The best inhibitory effects on the three enzymes were exerted by the purified product of P. lindleyanum, with IC₅₀ values of 0.594, 0.469 and 0.746 mg/mL. Among the active components, significant inhibitory effects on all three enzymes were exhibited by chlorogenic acid and luteolin, with IC₅₀ values of 0.145, 0.131, 0.136, 0.159, 0.134 and 0.140 mg/mL. Good inhibitory effects on pancreatic lipase and angiotensin-converting enzyme were shown by oxypeucedanin, with IC₅₀ values of 0.392 and 0.152 mg/mL. Respectively, moderate inhibitory effects on pancreatic lipase and angiotensin-converting enzyme were exhibited by luteolin-7-O-glucoside and bergapten, with IC₅₀ values of 0.225 and 0.258 mg/mL. Therefore, P. lindleyanum was demonstrated to possess good lipid-lowering, hypoglycemic and antihypertensive activities, which could provide a theoretical basis for the prevention and treatment of metabolic syndrome by P. lindleyanum.