The nature of the inhibition of cholesterol esterase by delta 1-tetrahydrocannabinol.
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 delta 1-tetrahydrocannabinol on a crude Leydig cell esterase preparation and on crystalline pancreatic esterase. Both enzymes were inhibited and the Km values determined (6.6 mumol/1 for the Leydig cell esterase and 6.25 mumol/1 for the pancreatic enzyme). While the former exhibited a mixed type of inhibition, the latter clearly was competitive.
D000818:Animals; D001665:Binding Sites; D002265:Carboxylic Ester Hydrolases / Q000037:antagonists & inhibitors*; D013759:Dronabinol / Q000494:pharmacology*; D007700:Kinetics; D007985:Leydig Cells / Q000201:enzymology*; D008297:Male; D010179:Pancreas / Q000201:enzymology*; D051381:Rats; D002787:Sterol Esterase / Q000032:analysis / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D013552:Swine
D013759:Dronabinol; D002265:Carboxylic Ester Hydrolases; D002787:Sterol Esterase