apoa1

Campesterol ((24R)-5-Ergosten-3β-ol) 是一种植物甾醇，具有降胆固醇和抗癌的活性。

GW694481 is a potent ApoA1 upregulator (EC170 = 500 nM).

Pinolenic acid is a polyunsaturated fatty acid found in Korean pine (Pinus orientalis) and maritime pine (Pinus pinaster) seed oils. Both oils have been found to have lipid-lowering properties. A diet containing maritime pine seed oil (MPSO) lowered high-density lipoprotein and ApoA1 levels in transgenic mice expressing human ApoA1. MPSO was found to diminish cholesterol efflux in vitro. Korean pine seed oil supplements may help in obesity by reduction of appetite. People taking this oil had an increase in the satiety hormones CCK and GLP-1 and a reduced desire to eat. The activity of the oil is attributed to pinolenic acid. Pinolenic acid is not converted to arachidonic acid metabolically and can reduce arachidonic acid levels in the phosphatidylinositol fraction of HepG2 cells from 15.9% to 7.0%. Pinolenic acid ethyl ester is a neutral, more lipophilic form of the free acid.

5(Z),11(Z),14(Z)-Eicosatrienoic acid is a polyunsaturated fatty acid found in various natural sources including maritime pine (Pinus pinaster) seed oil (MPSO), gymnospermae leaves and seeds, and freshwater gastropods. A diet containing MPSO lowered high-density lipoprotein and ApoA1 levels in transgenic mice expressing human ApoA1. MPSO was found to diminish cholesterol efflux in vitro. 5(Z),11(Z),14(Z)-Eicosatrienoic acid methyl ester, when topically applied, reduces inflammatory processes, potentially by displacing arachidonic acid from phospholipid pools and reducing downstream inflammatory products such as prostaglandin E2 and leukotrienes.

GW841819X is an analogue of (+)-JQ1 and a novel inhibitor of BET bromodomains. GW841819X was a single enantiomer but of undefined chirality at the 4-position of the benzodiazepine ring3. GW841819X and JQ1 were recently discovered that bind to the acetyl-lysine binding pocket of BET bromodomains with Kd ranges from 50 to 370 nM [1]. GW841819X bounded to both the individual BD1 and BD2 domains with affinities of 46 and 52.5 nM, respectively. GW841819X-Brd3 interaction was estimated to be around 70 nM4. GW841819X displayed activity in vivo against NUT-midline carcinoma, multiple myeloma, mixed-lineage leukemia, and acute myeloid leukemia1. It also potent induced the ApoA1 reporter gene with an EC50 of 440 nM. It had very little effect on LDL-R luciferase activity at the concentrations at which it induces ApoA1 expression, suggesting that the effect is indeed specific3. GW841819X competed directly with GATA1 site for BD1 binding and also specifically blocked the interaction between Brd3 and acetylated GATA14. Recent findings reported that GW841819X are chose as an interest compound to further develop into potential drugs against diseases including cancer, HIV infection and heart disease2.

Bambuterol is a prodrug of β2-agonist commonly used for the treatment of asthma and chronic obstructive pulmonary disease (COPD) with the advantage of once daily dosing and favorable side effect profile. Administration of a single-dose of R-bambuterol resulted in dose-dependent reductions in the levels of plasma LDL-C, high-density lipoprotein cholesterol (HDL-C), total cholesterol (TC), apolipoprotein B (ApoB) and apolipoprotein A1 (ApoA1) at Tmax. R-bambuterol can lower the plasma levels of LDL-C, and marginally raise the ratio of ApoA1 ApoB (indicator of HDL-C LDL-C) with both a single dose and multiple doses. R-bambuterol was more potent in LDL-C lowering than rac-bambutero

RG33是一种33个氨基酸的合成肽，与apolipoprotein A1 (ApoA1)的C-末端域中两个Y类螺旋的209-219和220-241氨基酸相对应。它能溶解含有1,2-dimyristoyl-sn-glycero-3-PC (DMPC)的多层囊泡(MLVs)，形成重组HDL。与脂质结合的RG33在J774巨噬细胞中诱导胆固醇外流。RG33 (12 mg/kg)可降低胰岛素抵抗性小鼠的血糖水平。