Human ACAT-1 and ACAT-2 Inhibitory Activities of Pentacyclic Triterpenes from the Leaves of Lycopus lucidus TURCZ.

Human Acyl-CoA: Cholesterol Acyltransferase Inhibitory Activities of Aliphatic Acid Amides from Zanthoxylum piperitum DC.

“…20) From the previous results, betulinic acid exhibited more potent hACAT-1 and -2 inhibitory activities than ursolic acid and oleanolic acid. 10) Manassantin A preferentially inhibited hACAT-2 than hACAT-1 and manassantin B dominantly inhibited hACAT-1, 9) whereas pyripyropene A inhibited only hACAT-2. 9,15) The selective inhibition of ACAT-1 and -2 provides evidence for uniqueness in structure and function of these two enzymes.…”

“…10) Microsomal fractions of Hi5 cells containing baculovirally expressed hACAT-1 or hACAT-2 were used as the sources of enzymes. 15) In brief, the reaction mixture, containing 32 mg microsomal protein, 0.1 M potassium-phosphate buffer (pH 7.4, 2 mM dithiothreitol), 6.7 mg/ml BSA (fatty acid free), 0.40 mg/ml cholesterol, and test sample in a total volume of 92 ml, was preincubated for 20 min at 37°C.…”

“…7) Thus, ACAT inhibitors are being investigated as potent therapeutic agents for the treatment of hypercholesterolemia and atherosclerosis. 8) In the course of a search for ACAT inhibitors from natural sources, 9,10) the ethanolic extracts (100 mg/ml) of stems and pericarps of Z. piperitum DC. exhibited hACAT-1 and -2 inhibitory activities with 73% and 21% for stems and 85% and 60% for pericarps, respectively.…”

Effect of corosolic acid on dietary hypercholesterolemia and hepatic steatosis in KK-Ay diabetic mice

“…Taken together, these results suggest that CA has some effects on the enzyme which is active when dietary cholesterol is high. Pentacyclic triterpenes, the group of compounds to which CA belongs, have been reported to exhibit various biological activities (12), and to inhibit ACAT-1 and ACAT-2 activities in an experiment using insect cells (Hi5 cells) containing baculovirally expressed ACAT-1 or ACAT-2 (19). In addition, ACAT inhibitors have been found to be effective in preventing hepatic cholesterol accumulation and hypercholesterolemia in animal models (11).…”

Physicochemical 2D-Qsar and 3D Molecular Docking Studies on N-Chlorosulfonyl Isocyanate Analogs as Sterol O-Acyl-Transferase-1 “Soat-1” Inhibitors

“…SOAT-1 is an essential isozyme for intracellular storage of cholesteryl esters [7]. SOAT-2 is expressed exclusively in the small intestine and liver [8,9]. In human liver, both of SOAT isozymes are expressed and may provide cholesteryl esters for very low density lipoprotein [10].…”