An Anti-Inflammatory Composition of Boswellia serrata Resin Extracts Alleviates Pain and Protects Cartilage in Monoiodoacetate-Induced Osteoarthritis in Rats

Abstract

The boswellic acids, the active compounds in Boswellia serrata gum resin extract, are potent anti-inflammatory agents and are specific nonredox inhibitors of 5-Lipoxygenase (5-LOX). Here, we present the anti-osteoarthritis (OA) efficacy of LI13019F1 (also known as Serratrin®), a unique composition containing the acidic and nonacidic fractions of B. serrata gum resin. This composition strongly inhibited 5-LOX activity with the half-maximal inhibitory concentration (IC 50 ) of 43.35 ± 4.90 μ g/mL. Also, LI13019F1 strongly inhibited the leukotriene B 4 (IC 50 , 7.80 ± 2.40 μ g/mL) and prostaglandin E 2 (IC 50 , 6.19 ± 0.52 μ g/mL) productions in human blood-derived cells. Besides, LI13019F1 reduced TNF- α production with the IC 50 of 12.38 ± 0.423 μ g/mL. On average, 1, 2.5, and 5 μ g/mL doses of LI13019F1 protected 34.62, 47.66, and 62.29% SW1353 human chondrosarcoma cells from IL-1 β induced SOX-9 depletion, respectively. Further, a 28-day preclinical proof-of-concept study evaluated the pain relief efficacy of LI13019F1 in monoiodoacetate- (MIA-) induced Sprague-Dawley rats. At the end of the study, 150 and 300 mg/kg doses of LI13019F1 supplemented rats showed significant improvements (55.17 ± 5.81 g ( p p p p B. serrata gum resin extracts, reduces pain and protects articular cartilage from the damaging action of MIA in a rodent model.