Lipoxygenase

Compound 3, known as 5-LOX/MAOs-IN-1, acts as an inhibitor of 5-LOX/MAOs and is an effective free radical scavenger, displaying antioxidant characteristics. It has demonstrated neuroprotective effects in cell models damaged by oxidative stress and is capable of activating the neurogenesis microenvironment in adult mouse neural stem cells. This compound is utilized in research focused on neurodegenerative diseases.

Applications 3-O-Acetyl-beta-boswellic acid possesses anti-inflammatory potential on key inflammatory mediators, TNF-α and IL-6. Main bioactive components of frankincense which is a fragrant resin obtained from plants of the genus Boswellia, acts as a cytotoxic agents. It is also a non-competitive 5-lipoxygenase and topoisomerase I and IIa. References Sharma, S., et al.: Bioorg. Med. Chem. Lett., 26, 695-698 (2016); Csuk, R., et al.: Tetrahedron, 71, 2025-2034 (2015); Csuk, R., et al.: Eur. J. Med. Chem., 100, 98-105 (2015);

Silychristin (Silicristin) is a plant growth regulator.

Applications Cytotoxic agent against cancer cell lines. Inhibitor of ornithine decarboxylase and protein tyrosine kinase. Found to be a specific inhibitor of the nuclear transcription factor, NF-kB. It has also been shown to significantly suppress the lipoxygenase pathway of arachidonic acid metabolism during inflammation. References Grunberger, D., et al.: Experientia, 44, 230 (1988), Fesen, M.R., et al.: Biochem. Pharmacol., 48, 595 (1994), Su, Z.Z., et al.: Cancer Res., 54, 1865 (1994), Zheng, Z.S., et al.: Oncol. Res., 7, 445 (1995), Mirzoeva, O.K. and Calder, P.C.: Essent. Fatty Acids, 55, 441 (1996)

Compound 10 (h15-LOX-2 inhibitor 2) suppresses h15-LOX activity, exhibiting IC 50 and K i values of 26.9 μM and 16.4 μM, respectively.

COX-2/15-LOX-IN-4 (compound 5i) is a dual inhibitor with IC50 values of 0.075 μM for COX-2 and 1.97 μM for 15-LOX.

Ruthenoleuton is a 5-lipoxygenase (5-LOX) inhibitor with an IC50 of 3.49 μM and a Ki of 0.80 μM. It possesses antioxidant properties and is applicable in research on inflammatory diseases.

Applications Lazbelled analogue of Acetone 2,4-Dinitrophenylhydrazone, a dinitrophenylhydrazone (DNPH) derivative of an aliphatic ketone found in mainstream cigarette smoke. Acetone 2,4-Dinitrophenylhydrazone showed inhibitory activity towards soybean lipoxygenase and renal prostaglandin synthetase. References Delgado, B. et al.: J. Liq. Chrom. Rel Technol., 31, 361 (2008); Miller, J.H. et al.: J. Chrom. Sci., 48, 12 (2010); Baumann, J. et al.: Agents Act., 12, 360 (1982);

2-TEDC: Potent LOX inhibitor, blocks 5-LOX, 12-LOX, 15-LOX (IC50: 0.09, 0.013, 0.5 μM); aids atherosclerosis research.

Croconazole exhibited dose-dependent inhibitory activity on the 5-lipoxygenase (5-LOX) of neutrophils.

Xanthatin exhibits cytotoxic, antibacterial, antifungal properties, may treat NSCLC, and inhibits melanoma by targeting Wnt/β-catenin and angiogenesis.