Métabolisme

Curcumin-β-D-glucuronide, a principal metabolite detected in hepatic tissue and portal blood following oral consumption of Curcumin, is utilized in colon cancer

(2E,9Z)-Octadeca-2,9-dienoic acid, a polyunsaturated fatty acid, is utilized in the study of lipoxygenase-dependent metabolism [1].

11β-Prostaglandin F2αethanolamide (11β-PGF2α-EA), posited as the hepatic metabolite derived from PGD2-EA during COX-2 metabolism of AEA—an endogenous cannabinoid present in brain, liver, and various mammalian tissues—is synthesized directly from AEA via COX-2 and specific prostaglandin synthase, leading to ethanolamide versions of classical prostaglandins. Additionally, PGD2-EA formation occurs in activated RAW 264.7 cells upon AEA treatment.

MK-8666, a partial GPCR agonist targeting GPR40, may treat type 2 diabetes by enhancing insulin secretion and lowering glucose safely.

12(Z),15(Z)-Heneicosadienoic acid, an ω-6 very long-chain polyunsaturated fatty acid, serves as a positional isomer of heneicosadienoic acid, which is scarcely found in living organisms.

1,2,3-Tripentadecanoyl glycerol, a triacylglycerol featuring pentadecanoic acid at the sn-1, sn-2, and sn-3 positions, occurs in various grapes. It serves as a standard in LC-MS for detecting triacylglycerols in human plasma.

LY433771 is a compound that inhibits the activity of Type X secretory phospholipase A2.

1,2-Dipalmitoyl-3-myristoyl-rac-glycerol, a triacylglycerol, incorporates palmitic acid at the sn-1 and sn-2 positions, along with myristic acid at the sn-3 position, and is identified in bovine milk fat.

1-Palmitoyl-2-Linoleoyl-sn-glycero-3-phosphatidylcholine (PC) is a phospholipid characterized by the incorporation of palmitic (16:0) and linoleic (18:2) acids at the sn-1 and sn-2 positions, respectively. It is utilized in the creation of micelles, liposomes, and various artificial membranes, playing a significant role in research on lipid peroxidation.

Tiracizine HCl, a new class I antiarrhythmic drug, was studied in patients with ischemic heart disease and shown to decrease myocardial contractile function.

17(R)-Resolvin D3 (17(R)-RvD3) is an aspirin-triggered epimer of resolvin D3, produced from docosahexaenoic acid (DHA) through the action of COX-2 in the presence of aspirin, via a 17(R)-hydroperoxy DHA (17(R)-HDHA) intermediary. Identified in mouse inflammatory exudates, 17(R)-RvD3 notably inhibits the transmigration of isolated human polymorphonuclear cells (PMNs) and fosters the efferocytosis of apoptotic PMNs by macrophages. Furthermore, in a mouse model of zymosan-induced peritonitis, 17(R)-RvD3 administration (10 ng/animal) significantly curtails neutrophil infiltration into the peritoneal cavity and modulates cytokine levels by reducing IL-6 and increasing IL-10 in the inflammatory exudate. It engages GPR32, evidenced by activation in a β-arrestin reporter assay and augments phagocytosis more effectively in CHO cells overexpressing GPR32 compared to controls. Additionally, 17(R)-RvD3 enhances the clearance of etoposide-induced tumor cell debris by monocyte-derived macrophages in H460 human lung carcinoma.

1-Palmitoyl-2-arachidoyl-3-oleoyl-rac-glycerol, a triacylglycerol, incorporates palmitic acid, arachidic acid, and oleic acid at the sn-1, sn-2, and sn-3 positions, respectively, and is identified in cod liver oil.

Aladotrilat is an inhibitor of neutral endopeptidase. Its prodrug is aladrotril.

Hemipyocyanine (528-71-2) is the virulence factor of Gram-negative, aerobic rod bacterium Pseudomonas aeruginosa. Hemipyocyanine is an α-Amylase inhibitor.

Compound 1e, also known as ALP/Carbonic anhydrase-IN-1, is a dual inhibitor targeting both carbonic anhydrase (CA) isozymes II, IX, and XII, as well as alkaline

Glucocerebrosidase-IN-1 (compound 11a) hydrochloride is a potent, selective GCase (glucocerebrosidase) inhibitor with IC50 and Ki values of 29.3 μM and 18.5 μM

Sezolamide is a carbonic anhydrase inhibitor.

3-Hydroxycarbofuran, a principal metabolite of Carbofuran, acts as a reversible inhibitor of acetylcholinesterase (AChE) [1].

OSMI-1: cell-permeable OGT inhibitor, blocks O-GlcNAcylation (IC50: 2.7 μM), no effect on other cell glycans.

1,2,3-Tri-γ-linolenoyl glycerol, a polyunsaturated triacylglycerol featuring γ-linolenoyl side chains at the C-1, C-2, and C-3 positions, occurs in multiple plant species such as blackcurrant, redcurrant, and borage.