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 (IC50) of 43.35 ± 4.90 μg/mL. Also, LI13019F1 strongly inhibited the leukotriene B4 (IC50, 7.80 ± 2.40 μg/mL) and prostaglandin E2 (IC50, 6.19 ± 0.52 μg/mL) productions in human blood-derived cells. Besides, LI13019F1 reduced TNF-α production with the IC50 of 12.38 ± 0.423 μg/mL. On average, 1, 2.5, and 5 μg/mL doses of LI13019F1 protected 34.62, 47.66, and 62.29% SW1353 human chondrosarcoma cells from IL-1β 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 < 0.05), and 66.22 ± 6.30 g (p < 0.05), respectively, vs. MIA: 31.22 ± 7.15 g) in body-weight-bearing capacities. Concurrently, LI13019F1-150 and LI13019F1-300 rats substantially (p < 0.05) increased the threshold of pain sensitivity to pressure (26.98 ± 2.36 and 28.06 ± 2.72-gram force, respectively; vs. 18.63 ± 5.82 in MIA) and increased (p < 0.05) the latent time to withdraw the paw after a thermal stimulus (23.61 ± 2.73 and 28.18 ± 1.90 sec, respectively; vs. 16.56 ± 1.22 sec. in MIA). Besides, the histological observations on Safranin-O green stained articular cartilage revealed that LI13019F1 also prevented the MIA-induced structural damage of the cartilage and reduced the loss of the extracellular matrix (ECM) components in the experimental rats. In conclusion, the present observations suggest that LI13019F1, a new composition of B. serrata gum resin extracts, reduces pain and protects articular cartilage from the damaging action of MIA in a rodent model.
Highlights
Osteoarthritis (OA) is a debilitating disease, which primarily affects the hips and knees, the body-weight-bearing joints
We observed that LI13019F1 strongly inhibited PGE2 production (IC50, 6.19 ± 0.52 μg/mL) in LPS-induced human peripheral blood mononuclear cells (PBMCs) (Figure 2(b)). e cyclooxygenase (COX) pathway derived PGE2 is a potent mediator of inflammatory and neuropathic pain
Various preparations of the gum resin extracts of this plant are known to be anti-inflammatory [35,36,37], and these preparations alleviated the clinical symptoms of a variety of inflammatory ailments, including OA [13, 14]. e B. serrata gum resin extract-derived formulations are claimed to inhibit the 5-lipoxygenase pathway for their anti-inflammatory activities in the management of OA [15, 16, 38]
Summary
Osteoarthritis (OA) is a debilitating disease, which primarily affects the hips and knees, the body-weight-bearing joints. We assume from a consumer’s perspective that a product with a combined efficacy of pain relief and protection from articular cartilage damage might be the most attractive strategy in progressive OA management. A series of randomized, placebo-controlled clinical studies have established that various standardized preparations of B. serrata gum resin extracts are effective and safe alternative interventions for the management of OA pain [13,14,15, 23,24,25]. ® known as Serratrin ), containing the acidic and nonacidic fractions of B. serrata gum resin, standardized to six major BAs. Based on the assumptions, our primary focus of the study was to explore whether this composition could relieve pain and protects the articular cartilage in OA. A proof-of-concept study evaluated the ability of LI13019F1 in relieving pain and cartilage protection in the MIA-induced OA model of Sprague-Dawley rats
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