atherogenic

Seladelpar (MBX 8025) has been used in trials studying the treatment of Hyperlipidemia.

MBX-8025 is an agonist of peroxisome proliferator-activated receptor δ (PPARδ).1 It is greater than 750- and 2,500-fold selective for PPARδ over PPARα and PPARγ. MBX-8025 (10 mg/kg per day for eight weeks) reduces increases in fasting blood glucose and serum insulin levels, and decreases insulin resistance in Alms1 mutant (foz/foz) mice fed an atherogenic diet as a model of diet-induced obesity, type 2 diabetes, and non-alcoholic steatohepatitis (NASH).2 It also decreases serum alanine transaminase (ALT), as well as serum and hepatic cholesterol and triglyceride, levels and reduces markers of NASH in the same model. |1. Bays, H.E., Schwartz, S., Littlejohn, T., 3rd, et al. MBX-8025, a novel peroxisome proliferator receptor-δ agonist: Lipid and other metabolic effects in dyslipidemic overweight patients treated with and without atorvastatin. J. Clin. Endocrinol. Metab. 96(9), 2889-2897 (2011).|2. Haczeyni, F., Wang, H., Barn, V., et al. The selective peroxisome proliferator-activated receptor-delta agonist seladelpar reverses nonalcoholic steatohepatitis pathology by abrogating lipotoxicity in diabetic obese mice. Hepatol. Commun. 1(7), 663-674 (2017).

Pitavastatin (NK-104) sodium is a potent inhibitor of hydroxymethylglutaryl-CoA (HMG-CoA) reductase and an inducer of the hepatocyte low-density lipoprotein cholesterol (LDL-C) receptor. It inhibits acetate synthesis of cholesterol in HepG2 cells and exhibits anti-atherogenic, anti-osteoarthritic, anti-asthmatic, anti-tumour, neuroprotective, hepatoprotective, and nephroprotective effects.

Pactimibe sulfate (CS-505) is a dual ACAT1 2 inhibitor, acting on ACAT1 (IC50: 4.9 μM) and ACAT2 (IC50: 3.0 μM). It inhibits oleoyl-CoA non-competitively (Ki: 5.6 μM) and significantly inhibits cholesterol ester formation (IC50: 6.7 μM). Pactimibe sulfate reduces plasma cholesterol activity and has anti-atherogenic potential.

Oleuropein is an antioxidant polyphenol isolated from olive leaf.

G* peptide, also known as LVGRQLEEFL (mouse) TFA, is a segment corresponding to amino acids 113 to 122 ([113,122] apoJ) of apolipoprotein J. This compound possesses both anti-inflammatory and anti-atherogenic qualities. When combined with an apoJ mimetic, it constitutes the HM-10 10 peptide, a novel chimeric high-density lipoprotein mimetic peptide. The HM-10 10 peptide is notable for safeguarding retinal pigment epithelium (RPE) and photoreceptors from oxidant-induced cell death as referenced in sources [1] [2].

G* Peptide, also denoted as LVGRQLEEFL (mouse), represents the amino acid sequence 113 to 122 ([113,122] apoJ) found in apolipoprotein J. This compound displays both anti-inflammatory and anti-atherogenic characteristics. When incorporated into an apoJ mimetic, it results in the formation of the HM-10 10 peptide, which functions as a novel chimeric high-density lipoprotein. The HM-10 10 peptide has been shown to confer protection to the retinal pigment epithelium (RPE) and photoreceptors against oxidant-induced cell death [1] [2].

Gastric inhibitory peptide (GIP) (22-51), a pro-atherogenic peptide comprised of 30 amino acids from the residues 22-51 of its precursor protein proGIP, is present in human plasma. It activates the degradation of IκB-α and the nuclear translocation of NF-κB in both macrophage-differentiated THP-1 cells and human aortic endothelial cells at a concentration of 1 µM. Additionally, in ApoE-/- mice, GIP (22-51) escalates the area of atherosclerotic lesions and plaque development in vivo.

Tormentic acid is a natural product. It has anticancer, anti-inflammatory, anti-atherogenic , anti-allodynic, and hepatoprotective properties,

Momordicosides K and L, the main bitter taste triterpene glycosides in Bitter melon; and bitter melon has been reported to have hypoglycemic, anti atherogenic and anti HIV activities.

3',4'-Dimethoxyflavone is a standard flavonoid compound with numerous medicinal activities.

KRES peptide, an apolipoprotein with four amino acid residues, interacts with lipids, reduces lipoprotein lipid hydroperoxides (LOOH), activates antioxidant enzymes associated with high-density lipoprotein, and exhibits anti-inflammatory and anti-atherogenic properties. KRES peptide is also orally active [1].

Arglabin ((+)-Arglabin) is a natural product isolated from Artemisia glabella, is a NLRP3 inflammasome inhibitor, has anti-atherogenic and anticancer effects.

Miquelianin (Quercetin 3-glucuronide) is a potent stilbene oxidase inhibitor, it has antioxidant, anti-atherogenic, and anti-inflammatory activities.