RESUMO
1-Phenyl-5-p-tolyl-1H-1, 2, 3-triazole (PPTA) was a synthesized compound. The result of acute toxicities to mice of PPTA by intragastric administration indicated that PPTA did not produce any significant acute toxic effect on Kunming strain mice. It exhibited the various potent inhibitory activities against two kinds of bananas pathogenic bacteria, black sigatoka and freckle, when compared with that of control drugs and the inhibitory rates were up to 64.14% and 43.46%, respectively, with the same concentration of 7.06 mM. The interaction of PPTA with human serum albumin (HSA) was studied using fluorescence polarization, absorption spectra, 3D fluorescence, and synchronous spectra in combination with quantum chemistry and molecular modeling. Multiple modes of interaction between PPTA and HSA were suggested to stabilize the PPTA-HSA complex, based on thermodynamic data and molecular modeling. Binding of PPTA to HSA induced perturbation in the microenvironment around HSA as well as secondary structural changes in the protein.
Assuntos
Anti-Infecciosos/farmacologia , Avaliação Pré-Clínica de Medicamentos/métodos , Albumina Sérica Humana/metabolismo , Triazóis/metabolismo , Triazóis/farmacologia , Animais , Sítios de Ligação , Feminino , Polarização de Fluorescência , Fungicidas Industriais/farmacologia , Humanos , Masculino , Camundongos , Modelos Moleculares , Musa/microbiologia , Estrutura Secundária de Proteína , Albumina Sérica Humana/química , Testes de Toxicidade Aguda , Triazóis/toxicidadeRESUMO
Two new phenylpropanoid glycosides, named ß-D-(1-O-acetyl-3,6-O-diferuloyl) fructofuranosyl ß-D-6'-O-acetylglucopyranoside (1) and ß-D-(1-O-acetyl-3,6-O-diferuloyl) fructofuranosyl α-D-glucopyranoside (2), along with two known analogues (3-4) and four glycerides (5-8), were isolated from the EtOAc extract of the leaves of Ananas comosus. Their structures were elucidated on the basis of 1D- and 2D-NMR analyses, as well as HR-ESI-MS experiments. Compounds 1-4 showed significant antibacterial activities against Staphylococcus aureus and Escherichia coli.
Assuntos
Ananas/química , Glicosídeos/química , Folhas de Planta/química , Antibacterianos/química , Antibacterianos/farmacologia , Bactérias/efeitos dos fármacos , Estrutura MolecularRESUMO
OBJECTIVE: To study the optimum preparation process of the volatile oil of Dalbergia odorifera-beta-cyclodextrin. METHODS: The saturated water solution mixing method was compared with microwave method and ultrasonic method by determining the ultilization ratio of the volatile oil in Dalbergia odorifera. The optimum preparation conditions were investigated by the orthogonal design. The quality of the volatile oil before and after included were analyzed by TLC. RESULTS: The optimum preparation conditions for inclusion were as follows: m(volatile oil of Dalbergia odorifera): m (beta-CD) = 1:10 (g/g), ultrasonic time was 1h, the temperature was 70 degrees C. The ultilization ratio of the volatile oil was 82.02%. CONCLUSION: Ultrasonic method is the best method.
