rat acat

Enniatin A1, a cyclic hexadepsipeptide composed of alternating D-α-hydroxyisovaleric acids and N-methyl-L-amino acids isolated from Fusarium mycotoxins, exhibits anticarcinogenic effects through the induction of apoptosis and disruption of the ERK signaling pathway. It also inhibits ACAT in rat liver microsomes with an IC50 of 49 μM.

RP 70676 is a potent ACAT inhibitor(rat and rabbit ACAT with IC50 of 25 and 44 nM ).

Enniatin A, a Fusarium mycotoxin, inhibits acyl-CoA: cholesterol acyltransferase (ACAT) with an IC50 of 22 μM in rat liver microsome enzyme assays.

Enniatins B decreases the activation of ERK (p44 p42). Enniatin B is a Fusarium mycotoxin. Enniatin B inhibits acyl-CoA: cholesterol acyltransferase (ACAT) activity with an IC50 of 113 μM in an enzyme assay using rat liver microsomes.

Enniatin B1, a Fusarium mycotoxin, crosses the blood-brain barrier, decreases the activation of ERK (p44 p42), and inhibits moderately TNF-α-induced NF-κB activation. Furthermore, it inhibits acyl-CoA: cholesterol acyltransferase (ACAT) activity, exhibiting an IC50 of 73 μM in rat liver microsome enzyme assays.

Beauvericin, a Fusarium mycotoxin, inhibits acyl-CoA:cholesterol acyltransferase (ACAT) in rat liver microsomal enzyme assays with an IC50 value of 3 μM.

Eflucimibe is an ACAT inhibitor. Eflucimibe regulates endogenous hypercholesterolemia in a synergistic manner in New Zealand rabbits fed a casein-enriched diet. In vivo, orally administered Eflucimibe displayed high potency and efficacy as an antihypercholesterolemic compound in different cholesterol-fed animals (guinea-pig, rat, rabbit).

Terpendole C is an indole diterpene alkaloid fungal metabolite originally isolated from A. yamanashiensis and an inhibitor of acyl-coenzyme A:cholesterol acyltransferase (ACAT; IC50 = 2.1 μM in rat liver microsomes). It also inhibits ACAT in J774 macrophages (IC50 = 0.46 μM) without affecting cell growth.

Phenylpyropene A is a fungal metabolite originally isolated from P. griseofulvum that has enzyme inhibitory and insecticidal activities.1,2,3 It inhibits acyl-coenzyme A:cholesterol acyltransferase (ACAT; IC50 = 0.8 μM).1 Phenylpyropene A inhibits diacylglycerol acyltransferase (DGAT) in rat liver microsomes (IC50 = 78.7 μM). It induces mortality in 100% of M. persicae when used at a concentration of 5 ppm.3 |1. Kwon, O.E., Rho, M.C., Song, H.Y., et al. Phenylpyropene A and B, new inhibitors of acyl-CoA: Cholesterol acyltransferase produced by Penicillium griseofulvum F1959. J. Antibiot. (Tokyo) 55(11), 1004-1008 (2002).|2. Lee, S.W., Rho, M.C., Choi, J.H., et al. Inhibition of diacylglycerol acyltransferase by phenylpyropenes produced by Penicillium griseofulvum F1959. J. Microbiol. Biotechnol. 18(11), 1785-1788 (2008).|3. Horikoshi, R., Goto, K., Mitomi, M., et al. Identification of pyripyropene A as a promising insecticidal compound in a microbial metabolite screening. J. Antibiot. (Tokyo) 70(3), 272-276 (2017).

Gypsetin inhibits the activity of acyl-CoA:cholesterol acyltransferase (ACAT), showing inhibitory effects on rat liver microsomal ACAT with an IC50 of 18 μM, and competes with oleoyl-CoA substrate, possessing a Ki value of 5.5 μM. Additionally, Gypsetin prevents the formation of cholesterol esters from oleic acid with an IC50 of 0.65 μM.

Epicochlioquinone A inhibits rat liver microsomal ACAT with an IC50 of 1.7 μM and inhibits plasma lecithin-cholesterol acyltransferase (LCAT) with an IC50 of 15.8 μM. At a dosage of 75 mg/kg, it can reduce cholesterol absorption in rats by 50%.

5-Methylcytosine is a methylated nucleotide base found in eukaryotic DNA. It is an epigenetic modification formed by the action of DNA methyltransferases.

Yakuchinone B is an acyl-CoA:cholesterol O-acyltransferase (ACAT) inhibitor with cholesterol-lowering activity, identified in the seeds of the Zingiberaceae family. It inhibits rat liver ACAT with an IC50 value of 20.6 μM. Yakuchinone B is a potential candidate for research into hypercholesterolemia and atherosclerosis.

Helminthosporol is a natural plant growth regulator that promotes the growth of rice and lettuce seedlings. It also inhibits the activity of acyl-CoA:cholesterol acyltransferase (ACAT) in rat liver microsomes and the synthesis of cholesterol esters in macrophages.