The Nature of the Inhibition of Cholesterol Esterase by Δ^1-Tetrahydrocannabinol

Abstract
An improved assay for cholesterol esterase based on the use of fatty acid radiolabelled cholesterol esters has been developed. The method was used to demonstrate the effects of Δ^1-tetrahydrocannabinol on a crude Leydig cell esterase preparation and on crystalline pancreatic esterase. Both enzymes were inhibited and the K(m) values determined (6.6 μmol/1 for the Leydig cell esterase and 6.25 μmol/1 for the pancreatic enzyme). While the former exhibited a mixed type of inhibition, the latter clearly was competitive.