hypolipidemic

Gemfibrozil (CI-719) interacts with peroxisome proliferator-activated receptors (PPARalpha) resulting in PPARalpha-mediated stimulation of fatty acid oxidation and an increase in lipoprotein lipase (LPL) synthesis. Gemfibrozil is a fibric acid derivative with hypolipidemic effects. This enhances triglyceride-rich lipoprotein clearance and reduces the expression of apolipoprotein C-III (apoC-III). The reduction in hepatic production of apoC-III result in the subsequent reduction of serum levels of very-low-density-lipoprotein cholesterol (VLDL-C). In addition, gemfibrozil-mediated PPARalpha stimulation of apoA-I and apoA-II expression results in an increase in high-density lipoprotein cholesterol (HDL-C).

Squalene (AddaVax) is a natural organic compound originally obtained for commercial purposes primarily from shark liver oil, though there are botanical sources as well, including rice bran, wheat germ, and olives. All higher organisms produce squalene, including humans. Squalene is an intermediate product in the synthesis of cholesterol and shows several pharmacological properties such as hypolipidemic, hepatoprotective, cardioprotective, antioxidant, and antitoxicant activity.

1. Berberine (Umbellatine) is a potent oral hypoglycemic agent with beneficial effects on lipid metabolism. 2. Berberine may as a broad-spectrum anti-microbial medicine, a complementary therapeutic agent for HIV/AIDS. 3. Berberine seems to act as an herbal antidepressant and a neuroprotector against neurodegenerative disorders. 4. Berberine is used in histology for staining heparin in mast cells. As a natural dye, berberine has a colour index of 7516. 5. Berberine reduces hepatic fat content in rats with nonalcoholic fatty liver disease; also prevents proliferation of hepatic stellate cells (HSCs), which are central for the development of fibrosis during liver injury. 6. Berberine can ameliorate proinflammatory cytokines-induced intestinal epithelial tight junction damage in vitro, and berberine may be one of the targeted therapeutic agents that can restore barrier function in intestinal disease states. 7. Berberine has antineoplastic effects, including breast cancer, leukemia, melanoma, epidermoid carcinoma, hepatoma, pancreatic cancer, oral carcinoma, tongue carcinoma, glioblastoma, prostate carcinoma and gastric carcinoma, etc.

Crocin is a water-soluble carotenoid pigment of saffron (Crocus sativus L.). Crocin has anti-inflammatory, anti-oxidative, anti-apoptotic, anti-asthma, anti-cancer, and hypolipidemic effects.

Lifibrol (U-83860) is an inhibitor of cholesterol synthesis.Lifibrol has anticholesterol and hypolipidemic properties and promotes the conversion of LDL Apo B-100 in patients with hypercholesterolemia and mixed hyperlipidemia.

BMS-212122 (UNII-0Z473OO6GB) is a potent inhibitor of microsomal triglyceride transfer protein (MTP) and has shown hypolipidemic effects in animal studies.BMS-212122 significantly reduced lipid content and monocyte-derived (CD68+) cells in atherosclerotic plaques.

Imanixil (HOE-402 free base) is an LDL receptor (LDLR) inducer, a hypolipidemic and hypocholesterolemic compound with antiatherogenic activity that inhibits the production of very low-density lipoproteins (VLDLs).Imanixil acts by stimulating the LDL receptor pathway.

Simvastatin (MK 733) is an HMG-CoA reductase inhibitor (Ki=0.2 nM) with oral activity. Simvastatin has hypolipidemic activity, inhibits hepatic production of cholesterol, and is also used for the prevention of cardiovascular disease.

Neoandrographolide (Neoandrographiside) has potent hypolipidemic effect and protects the cardiovascular without significant liver damage.Neoandrographolide has anti-inflammatory effect, might result from inhibition of iNOS and COX-2 expression through inhibiting p38 MAPKs activation.Neoandrographolide as chemosensitizer in S-Jurkat and X chromosome-linked inhibitor of apoptosis protein (XIAP)-overexpressing Jurkat cells, a model for chemoresistance.

Icariside E4 is a natural compound derived from Ulmus minor that acts via AMPK phosphorylation and inhibition of MID1IP2 hypolipidation in HepG1 cells.Icariside E4 has anti-injurious, antioxidant, anti-Alzheimer's and anti-inflammatory effects and inhibits SREBP-1c, liver X receptor-α (LXR) and FASN in Icariside E4 is an effective candidate for the treatment of fatty liver disease and has hypolipidemic potential in HepG1 cells.

Heteroatom-substituted fatty acids have been observed to modulate the extension and desaturating of fatty acids, and to influence their distribution within phospholipids pools. 10-Thiastearic acid inhibits desaturation of radiolabeled stearate to oleate in rat hepatocytes and hepatoma cells by more than 80% at a concentration of 25 μM. This activity is associated with a hypolipidemic effect, making this 10-thiastearic acid a useful tool for evaluating new anti-obesity therapeutics.

Xenalipin (BW 207U) has hypolipidemic. It reduces blood cholesterol and triglycerides in rats.

BM 15766 sulfate, an inhibitor of 7-dehydrocholesterol δ7-reductase, effectively reduces plasma cholesterol levels and functions as a hypolipidemic agent [1] [2].

Pirozadil shows hypolipidemic activity.

Cajanin has potential hypolipidemic effects,possibly via up-regulating the ABCA1 protein expression,subsequently resulting in increased macrophage cholesterol efflux and RCT, it can significantly improve basal glucose uptake in HepG2 cells, its improving effect is concentration dependent, it exhibits effects stronger than that of rosiglitazone, which has been used as an antidiabetic drug.

[10]-Shogaol (10-Shogaol) is an extract from ginger displaying antioxidant activity. It also may contain hypolipidemic and insulin-sensitizing effects.

Y-9738 is an agent of hypolipidemic.

Globularin has hypoglycaemic and hypolipidemic activities in normal and streptozotocin-induced diabetic rats.

Delphinidin-3-O-galactoside chloride has anti-obesity and hypolipidemic effects. Delphinidin-3-O-galactoside (D3G) is a water-soluble anthocyanin with antioxidant activity. D3G is capable of masking the EGCG-induced cytotoxicity and ER stress, presumably

Choline Fenofibrate (Trilipix) is a choline formulation of fenofibrate, a synthetic phenoxy-isobutyric acid derivate and prodrug with antihyperlipidemic activity.

Clofibrin is a kind of hypolipidemic drug, which can reduce Hypertriglyceride and hypercholesterolemia.

Dihydroberberine has anti-atherosclerotic, anti-inflammatory, hypolipidemic and antitumor activities. It inhibits human ether-a-go-go-related gene (hERG) channels and remarkably reduces Hsp90 expression and its interaction with hERG.

3-O-Methylgalangin (GALANGIN-3-METHYLETHER) has antibacterial activity, it has inhibitory effects on Pseudomonas aeruginosa. GALANGIN-3-METHYLETHER has hypolipidemic activity, the action is due to the inhibition of pancreatic lipase.

LXR antagonist 2 (compound 10rr) is a potent LXR (liver X receptor) inverse agonist, acting on LXRβ (IC50: 0.36 μM) and LXRα (IC50: 2.25 μM). LXR antagonist 2 is an adipogenesis inhibitor that downregulates LXR target genes SREBP-1c, ACC, FAS and SCD-1. LXR antagonist 2 exhibits hypolipidemic activity in Triton WR-1339-induced hyperlipidemic mice.

Phloracetophenone (1-(2,4,6-Trihydroxyphenyl)ethanone) has antiobesity and hypolipidemic effects, may be partly mediated by delaying the intestinal absorption of dietary fat by inhibiting pancreatic lipase activity.

Enniatin complex, a mixture of cyclohexadepsipeptides predominantly derived from various Fusarium species of fungi, exhibits inhibitory effects on enzymes such as acyl-CoA: cholesterol acyl transferase. Furthermore, it has demonstrated the ability to induce apoptosis in multiple cancer cell lines. In addition to these activities, the Enniatin complex possesses ionophoric, antibiotic, and in vitro hypolipidemic properties.

Acipimox (K-9321) is a niacin derivative and nicotinic acid analog with activity as a hypolipidemic agent. Acipimox has special application for the treatment of hyperlipidemia in non-insulin-dependent diabetic patients.

Etofylline clofibrate has a hypolipidemic and antithrombotic effect and it also has an agonistic interaction with intimal PGI2.

Hepronicate（Megrin） is a small molecule compound with hypolipidemic and vasodilatory activity.

7,4'-Di-O-methylapigenin (4',7-DIMETHOXY-5-HYDROXYFLAVONE) can inhibit α-glucosidase and α-amylase enzymes and enhance 2-NBDG uptake in L6 cells, it has hypolipidemic effect on mouse pre-adipocyte (3T3L1) cell lines.

Cetaben is a PPARα-independent peroxisome proliferator and is a non-fibrate hypolipidemic drug. It potent reduces the concentration of cholesterol and triglycerides.

Gardenia yellow (Crocin I) has anti atherosclerosis and hypolipidemic effects.

Pirinixil is a hypolipidemic low toxicity agent.

CP-868388 free base (CP-868388) is an orally active, potent and selective PPARα agonist with hypolipidemic and anti-inflammatory activity for the study of dyslipidemia.

Ligupurpuroside A has antioxidant,and hypolipidemic effects, it can significantly inhibit lipid accumulation in HepG2 cell at the concentration of 50 μMol/L.

Swertiamarin (Swertiamaroside) is a common secoiridoid found among the members of Gentianaceae with anti-inflammatory, anticancer, hypoglycemic and hypolipidemic activities.

JTT 130 is an agent of hypolipidemic. It inhibits microsomal triglyceride transfer protein.

SC 33459 is a hypolipidemic agent.

TA-1801 is an agent of hypolipidemic.

Berberine ursodeoxycholate (HTD1801) is an orally effective hypolipidemic agent, an ionic salt of Berberine and Ursodeoxycholic acid.Berberine ursodeoxycholate has a wide range of metabolic activity and significantly reduces liver fat content. Berberine ursodeoxycholate has been used in studies of hyperlipidemia, non-alcoholic steatohepatitis (NASH) and diabetes.

Bile acids are essential for solubilization and transport of dietary lipids, are the major products of cholesterol catabolism, and are physiological ligands for farnesoid X receptor (FXR), a nuclear receptor that regulates genes involved in lipid metabolism.1They are also inherently cytotoxic, as physiological imbalance contributes to increased oxidative stress.2,3Bile acid-controlled signaling pathways are promising novel targets to treat such metabolic diseases as obesity, type II diabetes, hyperlipidemia, and atherosclerosis.Guggulsterone, derived from resin of the guggul tree, is a competitive antagonist of FXR bothin vitroandin vivo.4Thecisstereoisomer of guggulsterone, (E)-guggulsterone, decreases chenodeoxycholic acid (CDCA)-induced FXR activation with an IC50value of 15 μM.5,6By inhibiting CDCA-induced transactivation of FXR, guggulsterone lowers low-density lipoprotein cholesterol and triglyceride levels in rodents fed a high cholesterol diet.4 1.Makishima, M., Okamoto, A.Y., Repa, J.J., et al.Identification of a nuclear receptor for bile acidsScience2841362-1365(1999) 2.Barbier, O., Torra, I.P., Sirvent, A., et al.FXR induces the UGT2B4 enzyme in hepatocytes: A potential mechanism of negative feedback control of FXR activityGastroenterology1241926-1940(2003) 3.Tan, K.P., Yang, M., and Ito, S.Activation of nuclear factor (erythroid-2 like) factor 2 by toxic bile acids provokes adaptive defense responses to enhance cell survival at the emergence of oxidative stressMol. Pharmacol.72(5)1380-1390(2007) 4.Urizar, N.L., Liverman, A.B., Dodds, D.T., et al.A natural product that lowers cholesterol as an anatagonist ligand for FXRScience296(5573)1703-1706(2002) 5.Cui, J., Huang, L., Zhao, A., et al.Guggulsterone is a farnesoid X receptor antagonist in coactivator association assays but acts to enhance transcription of bile salt export pumpThe Journal of Biological Chemisty278(12)10214-10220(2003) 6.Wu, J., Xia, C., Meier, J., et al.The hypolipidemic natural product guggulsterone acts as an antagonist of the bile acid receptorMolecular Endocrinology16(7)1590-1597(2002)

Axitirome, also known as CGS 26214, is a hypolipidemic agent.

Tiadenol is a Hypolipidemic Agent.