RESUMO
Methyl, propyl and hexyl esters of rosmarinic, caffeic and p-coumaric acids were tested for antiallergic activity, and rosmarinic acid propyl ester exhibited the greatest ß-hexosaminidase release suppression (IC50, 23.7 µM). Quadratic correlations between pIC50 and cLogP (r(2) = 0.94, 0.98, and 1.00, respectively) were observed in each acid ester series. The antiallergic activity is modulated by hydrophobicity, and alkyl chain bulkiness.
Assuntos
Antialérgicos/química , Antialérgicos/farmacologia , Cinamatos/farmacologia , Depsídeos/farmacologia , Animais , Ácidos Cafeicos/química , Linhagem Celular/efeitos dos fármacos , Cinamatos/química , Ácidos Cumáricos/química , Depsídeos/química , Relação Dose-Resposta a Droga , Avaliação Pré-Clínica de Medicamentos/métodos , Ésteres/química , Interações Hidrofóbicas e Hidrofílicas , Mastócitos/imunologia , Mastócitos/metabolismo , Perilla/química , Propionatos , Ratos , Receptores de IgE/metabolismo , Relação Estrutura-Atividade , beta-N-Acetil-Hexosaminidases/metabolismo , Ácido RosmarínicoRESUMO
Rosmarinic acid extract with potent biological activities was successfully isolated by supramolecular technique and solvent extraction from Perilla leaves. By the supramolecular complex which was formed from flavocommelin and Perilla leaf extract as initial materials, the supernatant containing rosmarinic acid was isolated. Rosmarinic acid extract (62.9 ± 4.5% purity) was partly purified by partitioning ethyl acetate and water. Rosmarinic acid extract exhibited high total phenolic content of 433.9 ± 58.6 µg/mg of gallic acid equivalent, effective DPPH radical scavenging activity (SC50 of 5.5 ± 0.2 µg/mL), antiallergic activity (IC50 of 52.9 ± 6.7 µg/mL), and α-glucosidase inhibitory activity (IC50 of 0.23 ± 0.01 mg/mL). Rosmarinic acid extract shows high potential for diabetes mellitus and allergy treatments by inhibiting α-glucosidase activity and measuring ß-hexosaminidase, related to life-style disease.