RESUMO
Factors II, V, VII and Xa have materialized as a key enzymes for the intervention of blood coagulation cascade and for the development of new anti thrombotic agents. The combined density functional quantum mechanical/molecular mechanical (QM/MM) approach has been used to access inhibition of prothrombin and thrombin production. The biological activities of coumarin derivatives as clotting factor inhibitors was quantitatively analyzed in terms of physicochemical parameters utilizing the principal component analysis. Structural requirements for maximal potency were derived from the results of a quantitative structure activity relationship analysis.
Assuntos
Anticoagulantes/química , Anticoagulantes/farmacologia , Cumarínicos/química , Cumarínicos/farmacologia , Modelos Químicos , Fenômenos Químicos , Análise Discriminante , Análise de Componente Principal , Protrombina/antagonistas & inibidores , Protrombina/biossíntese , Protrombina/metabolismo , Tempo de Protrombina , Relação Quantitativa Estrutura-Atividade , Teoria Quântica , Trombina/antagonistas & inibidores , Trombina/biossíntese , Trombina/químicaRESUMO
Present work describes the potent antidiabetic fraction from flowers of Cassia auriculata Linn. Hydromethanolic extract along with its ethyl acetate and n-butanol fractions were evaluated for antidiabetic activity in alloxan-induced diabetes in rats. The n-butanol fraction exhibited significant reduction (p<0.001) in blood glucose levels and was also found effective in restoring the blood lipids and proteins to normal level. The activity was found comparable with standard drug phenformin. The hydromethanolic extract and its fractions were subjected to preliminary qualitative chemical investigations which indicated the presence of phenolic compounds, carbohydrates, tannins, steroids and amino acids.