CS, CA inhibit mPGES-1 and 5-LO activity; in silico analyses provide support for their inhibitory role
WEDNESDAY, Aug. 3, 2016 (HealthDay News) — Two specific plant-derived compounds may be effective in treating inflammation and pain, according to a study published online July 27 in the British Journal of Pharmacology.
Francesco Maione, Ph.D., from the University of Naples Federico II in Italy, and colleagues examined the consequence of inhibition of key enzymes in eicosanoid biosynthesis in activated human primary monocytes and neutrophils. They analyzed molecular interactions and binding modes of carnosol (CS) and carnosic acid (CA) by docking studies.
The researchers found that, at four hours post injection of the stimuli, CS and CA had significant and dose-dependent anti-inflammatory and anti-nociceptive effects in carrageenan-induced mouse hyperalgesia; they also inhibited the analgesic response in the late phase of the formalin test. Potent inhibition of cell-free microsomal prostaglandin E2 synthase-1 (mPGES-1) and 5-lipoxygenase (5-LO) activity was seen for both compounds, with preferential suppression of the formation of mPGES-1 and 5-LO-derived products in cellular studies. In silico analyses provided support for CS and CA as dual 5-LO/mPGES-1 inhibitors.
“In summary, we propose that the combined inhibition of mPGES-1 and 5-LO by CS and CA essentially contributes to the bioactivity of these diterpenoids,” the authors write. “Our findings pave the way for a rational use of Salvia spp., traditionally used as anti-inflammatory remedy, in the continuous expanding context of nutraceuticals.”
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