MN-001 (tipelukast) is a novel, orally bioavailable small molecule compound thought to exert its effects through several mechanisms to produce its anti-inflammatory and anti-fibrotic activity in preclinical models, including leukotriene (LT) receptor antagonism, inhibition of phosphodiesterases (PDE) (mainly 3 and 4), and inhibition of
5-lipoxygenase (5-LO).
Melatonin inhibits the transcription of the
5-lipoxygenase gene, a gene involved in the onset of inflammation; therefore, we can say that darkness represses the expression of the
5-lipoxygenase gene.
Additionally, CMV infection is shown to increase
5-lipoxygenase (5-LO) and leukotriene B4 in vascular smooth muscle cells.
Currently, the anti-inflammatory non-steroid drugs present on the pharmaceutical market, reduces the conversion of arachidonic acid into prostaglandins by inhibiting the cyclooxygenase enzyme [18-23], however, does not inhibit
5-lipoxygenase enzyme.
When the animals were 12 months old, the equivalent of age 60 in humans, they were treated with zileuton, a drug that inhibits leukotriene formation by blocking the
5-lipoxygenase enzyme.
The reason being attributed principally to inhibition of biosynthesis of cytoprotective prostaglandins such as prostaglandin E and prostacyclin by inhibition of cyclooxygenase pathway of arachidonic acid metabolism, resulting in overproduction of leukotrienes and other products of
5-lipoxygenase pathway.
Flavocoxid, a dual inhibitor of cyclooxygenase and
5-lipoxygenase, blunts pro-inflammatory phenotype activation in endotoxin-stimulated macrophages.
MN-001 is a novel and orally bioavailable small molecule compound, which is believed to exercise its effects through various mechanisms to produce its anti-inflammatory and anti-fibrotic activity in preclinical models, including leukotriene receptor antagonism, inhibition of phosphodiesterases (PDE) (mainly three and four), and inhibition of
5-lipoxygenase.
Are Tolfenamic acid and tenidap dual inhibitors of
5-lipoxygenase and cyclo-oxygenase.
COX pathways consist of cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2), while
5-lipoxygenase (5-LOX), 12-lipoxygenase (12-LOX), and 15-lipoxygenase (15-LOX) are the examples of the LOX pathway.
To this, 50 [micro]l of the
5-lipoxygenase enzyme (400 units/ml cold 2 M borate buffer, pH 6.9) was added and incubated at room temperature for 5 min.