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OBJECTIVE:Though the initial etiologies of arthritis are multifactorial,clinically,patients share the prime complaints of the disease,pain.Here the authors assessed the analgesic and anti-infl ammatory effects of UP1304,a composite that contains a standardized blend of extracts from the rhizome of Curcuma longa and the root bark of Morus alba,on rats with carrageenan-induced paw edema.METHODS:A plant library was screened for bradykinin receptor antagonists.In vivo,the antiinfl ammatory and analgesic effects of the standardized composite,UP1304,were evaluated in rats with carrageenan-induced paw edema using oral dose ranges of 100–400 mg/kg.Ibuprofen,at a dose of 200 mg/kg,was used as a reference compound.In vitro,cyclooxygenase(COX)and lipoxygenase(LOX)inhibition assays were performed to evaluate the degree of infl ammation.RESULTS:Statistically signifi cant improvements in pain resistance and paw edema suppression were observed in animals treated with UP1304,when compared to vehicle-treated rats.Results from the highest dose of UP1304(400 mg/kg)were similar to those achieved by ibuprofen treatment at 200 mg/kg.In vitro,UP1304 showed dose-dependent inhibition of the enzymatic activities of COX and LOX.A h alf-maximal inhibitory concentration of 9.6 μg/m L for bradykinin B1 inhibition was calculated for the organic extract of C.longa.Curcumin showed Ki values of 2.73 and 58 μg/m L for bradykinin receptors B1 and B2,respectively.CONCLUSION:Data presented here suggest that UP1304,analgesic and anti-infl ammatory agent of botanical origin,acted as a bradykinin receptor B1 and B2 antagonist,and inhibited COX and LOX enzyme activities.This compound should be considered for the management of symptoms associated with arthritis.
OBJECTIVE: Though the initial etiologies of arthritis are multifactorial, clinically, patients share the prime complaints of the disease, pain. Here the authors assessed the analgesic and anti-infl ammatory effects of UP1 304, a composite that contains a standardized blend of extracts from the rhizome of Curcuma longa and the root bark of Morus alba, on rats with carrageenan-induced paw edema. METHODS: A plant library was screened for bradykinin receptor antagonists. In vivo, the antiinflammatory and analgesic effects of the standardized composite, UP1304, were used in rats with carrageenan-induced paw edema using oral dose ranges of 100-400 mg / kg. Ibuprofen, at a dose of 200 mg / kg, was used as a reference compound. In vitro, cyclooxygenase (COX) and lipoxygenase ) inhibition assays were performed to evaluate the degree of infl ammation. RESULTS: Statistically signifi cant improvements in pain resistance and paw edema suppression were observed in animals treated with UP1304, when compared to vehicle -treated rats. Results from the highest dose of UP1304 (400 mg / kg) were similar to those caused by ibuprofen treatment at 200 mg / kg.In vitro, UP1304 showed dose-dependent inhibition of the enzymatic activities of COX and LOX. A h alf-maximal inhibitory concentration of 9.6 μg / ml for bradykinin B1 inhibition was calculated for the organic extract of C. longa. Curcumin showed Ki values of 2.73 and 58 μg / ml for bradykinin receptors B1 and B2, respectively. CONCLUSION: Data presented here suggest that UP1304, analgesic and anti-infl ammatory agent of botanical origin, acted as a bradykinin receptor B1 and B2 antagonist, and inhibited COX and LOX enzyme activities. This compound should be considered for the management of symptoms associated with arthritis.