ABSTRACT
The anti-inflammatory and antinociceptive effects of the benzylated cubebin derivative, obtained by reaction of (-)-cubebin with benzyl bromide, were investigated using different animal models. The (-)-o-benzyl cubebin showed a low anti-inflammatory effect (16.2%) in relation to cubebin (57%) and indomethacin (77%) in the carrageenin-induced paw edema in rats, but on the other hand it was more effective (80%) than (-)-cubebin (41%) in inhibiting acetic acid-induced writhing in mice, producing dose-response correlation with doses of 10, 20 and 40 mg/kg, respectively. Moreover, this derivative compound did not show activity in both the hot plate and the cell migration test in rats. Overall, the results showed that the benzylation of cubebin were efficient in enhancing only its analgesic activity.
Subject(s)
Anti-Inflammatory Agents, Non-Steroidal/chemical synthesis , Anti-Inflammatory Agents, Non-Steroidal/pharmacology , Dioxoles/chemical synthesis , Dioxoles/pharmacology , Furans/chemical synthesis , Furans/pharmacology , Acetates , Animals , Carrageenan , Edema/chemically induced , Edema/prevention & control , Indicators and Reagents , Male , Pain Measurement/drug effects , Piper/chemistry , Rats , Rats, Wistar , Reaction Time/drug effectsABSTRACT
The anti-inflammatory and antinociceptive effects of the acetylated (2), methylated (3) and aminated (4) derivatives of cubebin (1), obtained by its reaction with acetic anhydride, methyl iodide and dimethylethylamine chloride, respectively, were investigated, using different animal models. The compound (2) was the most effective anti-inflammatory one in the carrageenin-induced paw edema in rats and was the only one which showed dose-response correlation for this assay with r = 0.993 and Y = 64.58x + 0.22. Besides, compounds (2) and (4) were more effective than cubebin in inhibiting acetic acid-induced writhing in mice, producing dose-response correlation with doses of 10, 20 and 30 mg/kg, respectively. Regarding the hot plate and the cell migration tests in rats, none of the four tested compounds showed activity. Overall, the results showed that the acetylation and amination of cubebin were efficient in enhancing its analgesic activity, as well as its anti-inflammatory activity.
Subject(s)
Analgesics , Anti-Inflammatory Agents, Non-Steroidal/pharmacology , Dioxoles/pharmacology , Furans/pharmacology , Lignans/chemistry , Acetic Acid/adverse effects , Acetic Acid/antagonists & inhibitors , Animals , Anti-Inflammatory Agents, Non-Steroidal/chemical synthesis , Carrageenan/adverse effects , Carrageenan/antagonists & inhibitors , Dioxoles/chemical synthesis , Dose-Response Relationship, Drug , Drug Evaluation, Preclinical , Furans/chemical synthesis , Lignans/chemical synthesis , Lignans/pharmacology , Male , Mice , Pain/chemically induced , Pain/drug therapy , Pain Measurement/drug effects , Rats , Rats, WistarABSTRACT
Three different concentrations (1, 10 and 50 microg/ml) of lyophilized hydroalcoholic crude extract of Pfaffia glomerata roots were assayed in vitro against strains of Trypanosoma cruzi (Y) and Leishmania braziliensis. It was observed that P. glomerata hydroalcoholic extract was relatively active within the tested concentrations for L. (V) braziliensis, but inactive against T. cruzi. Despite the fact that both protozoans belong to the Trypanosomatidae family, we suggest that the difference observed for activity should be related to the biological differences between the two parasite species.
