UP1306, a botanical composition with analgesic and anti-inflammatory effect

Abstract

Background:Pain, one of the cardinal signs of inflammation, is the most common clinical manifestations of arthritis. Conventional pain relief therapy heavily relies on the use of prescription and over the counter nonsteroidal anti-inflammatory drugs as the first line of defense where their long-term usage causes deleterious gastrointestinal and cardiovascular-related side-effects. Hence, there is an equivocal need for evidence-based safer and efficacious alternatives from natural sources to overcome the most prominent and disabling symptoms of arthritis.Materials and Methods:Carrageenan-induced rat paw edema and abdominal constriction (writhing's) assays in mouse were used to evaluate the anti-inflammatory and analgesic effects of UP1306, a composition that contains a standardized blend of extracts from the heartwood of Acacia catechu and the root bark of Morus alba administered orally at dose ranges of 100–300 mg/kg. Cyclooxygenase (COX) and lipoxygenase (LOX) inhibition assays were carried out to determine the IC50 of Acacia and Morus extracts. The merit of combining these two extracts was also assessed.Results:Statistically significant improvement in pain resistance and suppression of edema were observed in animals treated with UP1306, when compared to vehicle-treated diseased rats and mice. Results from the high dose of UP1306 (300 mg/kg) were similar to those achieved by ibuprofen treatment at a dose of 200 mg/kg in early hours of treatment. In vitro, UP1306 showed dose-dependent inhibition of the enzymatic activities of COX and LO with IC50 values of 20.9 μg/mL, 49.2 μg/mL, and 11.1 μg/mL in COX-1, COX-2, and 5’-LO, respectively.Conclusions:These data suggest that UP1306, analgesic, and anti-inflammatory agent of botanical origin with dual COX-LO inhibition activity, could potentially be used to alleviate symptom associated to osteoarthritis.SUMMARY Pain is the most common clinical manifestations of arthritisCarrageenan-induced rat paw edema and abdominal constriction (writhing's) assays in mouse are among the widely used models to evaluate the anti-inflammatory and analgesic effects of nutraceuticalsCyclooxygenase and lipoxygenase (LO) inhibition assays were carried out to determine the IC50 of Acacia and Morus extracts.Efficacy of UP1306, a composition containing a blend of two standardized extracts from the heartwood of Acacia catechu and root bark of Morus alba, was evaluated in the above models.UP1306 demonstrated its enhanced significance by improving the major cardinal signs of arthritis in vivo and inflammation markers in vitro.UP1306 could potentially be considered as a dietary supplement product for the management of arthritis.

Cartilage Protection and Analgesic Activity of a Botanical Composition Comprised of Morus alba, Scutellaria baicalensis, and Acacia catechu

“…Previously, both UP1306 and UP446 were tested in multiple animal models mainly focused on their symptomatic relief in inflammation and pain. Both showed good anti-inflammatory and antipain activity (Burnett et al, 2007; Tseng-Crank et al, 2010; Altavilla et al, 2009; [ 5 ]). Inflammation plays a central role in osteoarthritis (OA) pathology.…”

“…Recently we reported a botanical composition designated as UP1306 (a proprietary blend of two bioflavonoid standardized extracts from the heartwood of Acacia catechu and root bark of Morus alba ) with analgesic and anti-inflammatory effects [ 5 ]. UP1306 resulted in 46.3%–53.3% reductions in paw edema and 43.6%–54.8% reductions in pain sensitivity in the carrageenan induced rat paw edema model as well as a 34.4% reduction in visceral pain sensitivity in Writhing's model in mice [ 5 ]. IC 50 (concentration causing 50% inhibition) values of 20.9 μ g/mL, 49.2 μ g/mL, and 11.1 μ g/mL in cyclooxygenase 1 (COX-1), cyclooxygenase 2 (COX-2), and 5-lipoxygenase (5-LOX), respectively, were documented for UP1306 [ 5 ].…”

“…UP1306 resulted in 46.3%–53.3% reductions in paw edema and 43.6%–54.8% reductions in pain sensitivity in the carrageenan induced rat paw edema model as well as a 34.4% reduction in visceral pain sensitivity in Writhing's model in mice [ 5 ]. IC 50 (concentration causing 50% inhibition) values of 20.9 μ g/mL, 49.2 μ g/mL, and 11.1 μ g/mL in cyclooxygenase 1 (COX-1), cyclooxygenase 2 (COX-2), and 5-lipoxygenase (5-LOX), respectively, were documented for UP1306 [ 5 ]. Collectively, these findings suggest that UP1306 may be considered for OA management.…”

The role of miR-320a and IL-1β in human chondrocyte degradation

“…1,2 The most common symptoms of OA are pain, joint stiffness, crepitation on motion and limitation of joint motion, and OA leads to a significantly reduced quality of life. 3 Main risk factors of OA include age, mechanical injury, obesity, joint infection and osteochondrosis.…”

Reflections about osteoarthritis and Curcuma longa

“…[11115] Studies conducted by Yeh et al . [11] showed that levels of MMP-1 mRNA, MMP-3, and MMP-13 in human chondrocytes receiving curcumin for 6 h were decreased compared with the control group, showing the reduction of the metalloproteinases synthesis caused by curcumin.…”