atherogenic

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

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.

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

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).

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].

Oxidized low-density lipoprotien (oxLDL) particles contain low molecular weight species which are cytotoxic and pro-atherogenic. Many of these substances were recently isolated and purified from oxLDL, and identified as phosphatidylcholine species containing a fragmented, oxidized short-chain fatty acid remnant at the sn-2 position. 1-(Palmitoyl)-2-(5-oxovaleroyl)-phosphatidylcholine, or POV-PC, is one of the oxLDL species derived from 2-arachidonoyl or eicosapentanoyl phospholipids. POV-PC confers CD36 scavenger receptor binding affinity more potently than any hydroperoxy PC species, and may be one of the more important structural determinants of oxLDL. Treatment of cultured endothelial cells with POV-PC stimulates monocyte binding, stimulates intracellular cAMP production, and strongly inhibits the LPS-induced binding of neutrophils.

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.

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

Oxidized low-density lipoprotein (oxLDL) particles contain low molecular weight species which are cytotoxic and pro-atherogenic. Many of these substances were recently isolated and purified from oxLDL, and identified as phosphatidylcholine species containing a fragmented, oxidized short-chain fatty acid remnant at the sn-2 position. KDdiA-PC is one of the most potent CD36 ligands among the oxLDL species. KDdiA-PC confers CD-36 scavenger receptor binding affinity to LDL at a frequency of only two to three KDdiA-PC molecules/LDL particle, and may be one of the more important structural determinants of oxLDL.

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.

Oxidized low-density lipoprotien (oxLDL) particles contain low molecular weight species which are cytotoxic and pro-atherogenic. Many of these substances were recently isolated and purified from oxLDL, and identified as phosphatidylcholine species containing a fragmented, oxidized short-chain fatty acid remnant at the sn-2 position. 1-(Palmitoyl)-2-(5-keto-6-octene-dioyl) phosphatidylcholine, or KOdiA-PC, is one of the most potent CD36 ligands among the oxLDL species. KOdiA-PC confers CD36 scavenger receptor binding affinity to LDL at a frequency of only 2 to 3 KOdiA-PC molecules/LDL particle, and may be one of the more important structural determinants of oxLDL.

Oxidized low-density lipoprotein (oxLDL) particles contain low molecular weight species that are cytotoxic and pro-atherogenic. Many of these substances were isolated and purified from oxLDL, identified as phosphatidylcholine species containing a fragmented, oxidized short-chain fatty acid remnant at the sn-2 position. PAz-PC is one of the predominant oxLDL species and may be an important structural determinant of oxLDL.

Oleuropein is an antioxidant polyphenol isolated from olive leaf.

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.

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

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].