In vivo and in vitro anti-inflammatory and anti-nociceptive activities of lovastatin in rodents

Statins are among the most prescribed drugs in recent clinical practice. They are also known for their pleiotropic actions, which are independent of their lipid-lowering properties. The effect of lovastatin was investigated against carrageenan-induced paw edema in male Wistar rats (200-250 g) and on leukocyte migration, as measured by carrageenan-induced peritonitis in male Swiss mice (20-25 g), which are models of acute inflammation. Lovastatin (administered 1 h prior to carrageenan), at oral doses of 2, 5, and 10 mg/kg, markedly attenuated paw edema formation in rats at the 4th hour after carrageenan injection (25, 43, and 37 percent inhibition, respectively). Inhibitions of 20, 45 and 80 percent were observed in the leukocyte migration, as evaluated by carrageenan-induced peritonitis in mice with lovastatin doses of 0.5, 1 and 5 mg/kg, as compared to controls. Furthermore, lovastatin (administered 1 h before initiation) reduced the nociceptive effect of the formalin test in mice, at both phases, at doses of 2, 5, and 10 mg/kg: first phase (51, 65, and 70 percent, respectively) and second phase (73, 57, and 66 percent inhibition of licking time, respectively). The anti-nociceptive activity of lovastatin was inhibited by naloxone (3 mg/kg, sc). Lovastatin (0.01, 0.1, and 1 µg/mL) inhibited by 23, 79, and 86 percent, respectively, the release of myeloperoxidase from human neutrophils. Leukocyte (predominantly neutrophils) infiltration was almost completely reduced by lovastatin treatment, as observed in the model of acute paw edema with hematoxylin and eosin staining. In addition, lovastatin decreased the number of cells expressing tumor necrosis factor-α (TNF-α) and the inducible form of nitric oxide synthase (iNOS) activity. Therefore, the alterations in leukocyte activity and cytokine release could contribute to the anti-inflammatory activity of lovastatin.

Análise de timol por CLAE na tintura de Lippia sidoides Cham. (alecrim-pimenta) produzida em diferentes estágios de desenvolvimento da planta

O teor de timol, princípio ativo usado como marcador nas tinturas das folhas de Lippia sidoides Cham. (Verbenaceae) preparadas com material coletado antes, durante e após a floração e designadas como T1, T2 e T3, foi determinado por CLAE, utilizando-se cromatógrafo Shimadzu CLASS-VP, coluna RP-18 (Supelco), com fase móvel isocrática acetonitrila:água (78:22) e fluxo 0,8 ml/min com detecção em 254 nm. As amostras foram injetadas num volume de 20 μl e analisadas em triplicata. Os teores de timol encontrados foram 1,97 ± 0,07 em T1; 2,00 ± 0,03 em T2 e 2,34 ± 0,06 mg/ml em T3. Os resultados mostram discretas diferenças nas concentrações de timol nas tinturas das folhas de alecrim-pimenta preparadas em diferentes momentos de seu desenvolvimento. Contudo, observou-se que o melhor momento para a coleta da planta parece ser após a sua floração (T3), que mostrou o maior teor de timol.

Lippia sidoides Cham. (Verbenaceae) is popularly known in Northeast Brazil as "alecrim-pimenta". The goal of the present work is to perform a quantitative analysis of timol, used as a marker in phytomedicine prepared from the leaves of L. sidoides, collected before, during and after the flower. At least three samples of tincture of L. sidoides were analyzed by HPLC. Among the samples analyzed, the tincture produced from the leaves after the flower showed slightly high concentration of timol (2,34 ± 0,06 mg/ml) when compared with before (1,97 ± 0,07 mg/ml) or during the flower (2,00 ± 0,03 mg/ml). The best period to collect leaves of L. sidoides seems to be after the flower.