RESUMO
The stem and branch extract of Tripterygium wilfordii (Celastraceae) afforded seven new dihydroagarofuran sesquiterpene polyesters [tripterysines A-G (1-7)] and eight known ones (8-15). The chemical structures of these new compounds were established based on combinational analysis of HR-ESI-MS and NMR techniques. The absolute configurations of tripterysines A-C (1-3) and E-G (5-7) were determined by X-ray crystallographic analysis and circular dichroism spectra. All the compounds were screened for their inhibitory effect on inflammation through determining their inhibitory effect on nitric oxide production in LPS-induced RAW 264.7 cells and the secretion of inflammatory cytokines TNF-α and IL-6 in LPS-induced BV2 macrophages. Compound 9 exhibited significant inhibitory activity on NO production with an IC50 value of 8.77 μmol·L-1. Moreover, compound 7 showed the strongest inhibitory effect with the secretion of IL-6 at 27.36%.
Assuntos
Tripterygium/química , Ésteres/farmacologia , Interleucina-6 , Lipopolissacarídeos/farmacologia , Folhas de Planta/química , Anti-Inflamatórios/química , Óxido Nítrico/análise , Sesquiterpenos/química , Estrutura MolecularRESUMO
With a view to investigate the ameliorative effects of sitosterol esters against degenerative effects of hypercholesterolemia brain antioxidant enzyme assays, brain lipid profile, brain phospholipid compositional change and brain neurotransmitter concentrates (glutamic acid, asparctic acid, glycine) were measured in hypercholesterolemic rats. The results indicated that phytosterol esters have a role in countering hypercholesterolemia-related changes in the brain by decreasing the cholesterol levels, increasing the phospholipid levels and increasing the level of antioxidant enzymes. The results suggest that phytosterol esters may be of therapeutic significance and may offer new and effective options for the treatment of hypercholesterolemia-induced changes in the brain.
Assuntos
Aminoácidos/metabolismo , Animais , Antioxidantes/metabolismo , Encéfalo/efeitos dos fármacos , Encéfalo/metabolismo , Cromatografia , Ácidos Docosa-Hexaenoicos/metabolismo , Ácido Eicosapentaenoico/metabolismo , Ésteres/farmacologia , Óleos de Peixe/metabolismo , Glutationa/metabolismo , Hipercolesterolemia/metabolismo , Masculino , Neurotransmissores/metabolismo , Fitosteróis/farmacologia , Ratos , Ratos Wistar , Sitosteroides/farmacologia , Ácido alfa-Linolênico/metabolismoRESUMO
In current research, nine basic esters of para-alkoxyphenylcarbamic acid with incorporated 4-(4fluoro-/3-trifluoromethylphenyl)piperazin-1-yl fragment, 6i-6m and 8f-8i, were screened for their in vitro antimicrobial activity against Candida albicans, Staphylococcus aureus and Escherichia coli, respectively. Taking into account the minimum inhibitory concentration assay (MIC), as the most active against given yeast was evaluated 8i (MIC = 0.20 mg/mL), the most lipophilic structure containing para-butoxy and trifluoromethyl substituents. Investigating the efficiency of the compounds bearing only a single atom of fluorine and appropriate para-alkoxy side chain against Candida albicans, the cut-off effect was observed. From evaluated homological series, the maximum of the effectiveness was noticed for the stucture 6 k (MIC = 0.39 mg/mL), containing para-propoxy group attached to phenylcarbamoyloxy fragment, beyond which the compounds ceased to be active. On the contrary, all the tested molecules were against Staphylococcus aureus and Escherichia coli (MICs > 1.00 mg/mL) practically inactive.
Assuntos
Anti-Infecciosos/farmacologia , Candida albicans/efeitos dos fármacos , Carbamatos/farmacologia , Escherichia coli/efeitos dos fármacos , Piperazinas/farmacologia , Staphylococcus aureus/efeitos dos fármacos , Anti-Infecciosos/química , Carbamatos/química , Ésteres/química , Ésteres/farmacologia , Testes de Sensibilidade Microbiana , Piperazinas/química , Relação Estrutura-AtividadeRESUMO
Vascular autonomic receptors in amphibians exhibit difference from more evolved mammalian species. Vascular perfusion studies in frog indicate constrictions by prominent muscarinic but rudimentary nicotinic constrictive regulation by cholinergic systems. Difference from classical effect-patterns of pharmacological interventions, observed in the study, make room to visualise complexity of additional regulatory mechanisms.