UP1306, a Botanical Composition with Analgesic and Anti-inflammatory Effect

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 IC(50) 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 IC(50) 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: [Image: see text] Pain is the most common clinical manifestations of arthritis. Carrageenan-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 nutraceuticals. Cyclooxygenase and lipoxygenase (LO) inhibition assays were carried out to determine the IC(50) 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.