Inhibition of purified human postheparin lipoprotein lipase by beta-adrenergic blockers in vitro.

We examined the effects of five beta-adrenergic blockers on the hydrolysis of phosphatidylcholine-stabilized triolein particles by purified human postheparin lipoprotein lipase (PHLpL) in order to evaluate the possible role of direct inhibition as a mechanism of drug-induced hypertriglyceridemia. The relative inhibitory potencies were observed in the following order: propranolol much greater than pindolol greater than metoprolol greater than atenolol greater than nadolol. There was a positive correlation between the octanol/water partition coefficients of these agents and their inhibition of lipoprotein lipase, suggesting that hydrophobicity may be one of the major determinants for PHLpL inhibition. The amount of the beta-adrenergic blockers required to produce 50% inhibition of human PHLpL was much greater than that required to inhibit purified bovine lipoprotein lipase.