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
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
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
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
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
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
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.