Description
ZLJ-6 is a dual inhibitor of COX and 5-lipoxygenase (5-LO) (IC50 = 0.73, 0.31, and 0.99 μM for COX-1, COX-2, and 5-LO, respectively, in whole blood). It reduces carrageenin-induced paw edema (inflammation) in rats and acetic acid-induced abdominal constriction (pain) in mice without causing gastrointestinal ulcers, a common side effect of non-selective COX inhibitors.
in vitro
zlj-6 was identified as a potent inhibitor of cyclooxygenase in human whole blood. it also inhibited the production of thromboxane b(2) and prostaglandin e(2) in calcium ionophore a23187-induced human and rat whole blood, and rat peritoneal leukocytes. zlj-6 suppressed the activity of 5-lipoxygenase in the rat basophilic leukemia (rbl-1) cell lysate and in intact cells and reduced the generation of leukotriene b(4) (ltb(4)) in a23187-stimulated human or rat whole blood, and rat peritoneal leukocytes [1].
in vivo
orally administered zlj-6 demonstrated potent anti-inflammatory activity in the carrageenin-induced paw oedema model in rats and showed analgesic activity in the acetic acid-induced abdominal construction model in mice. no gastrointestinal ulcers were found with the anti-inflammatory dose (30 mg/kg) in normal rats [1].
IC 50
0.73, 0.31, and 0.99 μm for cox-1, cox-2, and 5-lo, respectively
References
[1] li, l. ,ji, h.,sheng, l., et al. the anti-inflammatory effects of zlj-6, a novel dual cyclooxygenase/5-lipoxygenase inhibitor. european journal of pharmacology 607 (1-3), 244-250 (2009).
