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-inflammatory effects of...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-inflammatory effects of UP1304, a composite that contains a standardized blend of extracts from the rhizome of Curcuma /onga and the root bark of Morus a/ba, on rats with carrageenan-induced paw edema. METHODS： A plant library was screened for bradykinin receptor antagonists./n vivo, the anti- inflammatory 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, cycleoxygenase （COX） and lipoxygenase （LOX） inhibition assays were performed to evaluate the degree of inflammation. RESULTS： Statistically significant 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. /n vitro, UP1304 showed dose-dependent inhibition of the enzymatic activities of COX and LOX. A half-maximal inhibitory concentration of 9.6 tJg/mL for bradykinin B1 inhibition was calculated for the organic extract of C./onga. Curcumin showed Ki values of 2.73 and 58 IJg/mL for bradykinin receptors B1 and B2, respectively. CONCLUSION： Data presented here suggest that UP1304, analgesic and anti-inflammatory 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.展开更多
文摘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-inflammatory effects of UP1304, a composite that contains a standardized blend of extracts from the rhizome of Curcuma /onga and the root bark of Morus a/ba, on rats with carrageenan-induced paw edema. METHODS： A plant library was screened for bradykinin receptor antagonists./n vivo, the anti- inflammatory 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, cycleoxygenase （COX） and lipoxygenase （LOX） inhibition assays were performed to evaluate the degree of inflammation. RESULTS： Statistically significant 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. /n vitro, UP1304 showed dose-dependent inhibition of the enzymatic activities of COX and LOX. A half-maximal inhibitory concentration of 9.6 tJg/mL for bradykinin B1 inhibition was calculated for the organic extract of C./onga. Curcumin showed Ki values of 2.73 and 58 IJg/mL for bradykinin receptors B1 and B2, respectively. CONCLUSION： Data presented here suggest that UP1304, analgesic and anti-inflammatory 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.
