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1.
Bioorg Med Chem Lett ; 25(20): 4567-71, 2015 Oct 15.
Artigo em Inglês | MEDLINE | ID: mdl-26351039

RESUMO

Three series of prenylated and/or geranylated flavonoids were synthesized and evaluated for their α-glucosidase inhibitory activity. The 3',5'-digeranylated chalcone (16) was identified as a new α-glucosidase inhibitor whose activity (IC50=0.90 µM) was 50-fold more than that of acarbose (IC50=51.32 µM). Molecular docking studies revealed the existence of strong hydrophobic interaction and H-bonding between compound 16 and α-glucosidase's active site. The inhibitory mode analysis showed that 16 exhibited a competitive inhibitory mode.


Assuntos
Chalconas/farmacologia , Flavonas/farmacologia , Inibidores de Glicosídeo Hidrolases/farmacologia , Isoflavonas/farmacologia , Simulação de Acoplamento Molecular , alfa-Glucosidases/metabolismo , Chalconas/síntese química , Chalconas/química , Relação Dose-Resposta a Droga , Flavonas/síntese química , Flavonas/química , Inibidores de Glicosídeo Hidrolases/síntese química , Inibidores de Glicosídeo Hidrolases/química , Humanos , Isoflavonas/síntese química , Isoflavonas/química , Estrutura Molecular , Relação Estrutura-Atividade
2.
J Cardiothorac Surg ; 10: 60, 2015 Apr 25.
Artigo em Inglês | MEDLINE | ID: mdl-25907099

RESUMO

AIMS: The aim of this study is to investigate how the myocardial bridge oppression affects the hoop stress of mural coronary artery. METHODS: The "myocardial bridge - coronary artery" simulative device records the hoop stress which is changed by adjusting the external pressure of the simulated coronary artery and the oppression degree of the respectively. RESULTS: Simulation experiment in vitro indicates that the abnormal hoop stress mainly occurs in the proximal end of mural coronary artery. As the oppression degree of myocardial bridge increases, the mean and the oscillatory value (maximum-minimum) of hoop stress in the proximal end increase markedly. CONCLUSIONS: The "myocardial bridge - coronary artery" simulation device can provide an experiment method of studying the hoop stress influence on mural coronary artery in vitro.


Assuntos
Vasos Coronários , Modelos Anatômicos , Ponte Miocárdica/fisiopatologia , Pressão , Estresse Mecânico , Humanos , Técnicas In Vitro , Miocárdio
3.
Zhonghua Wei Chang Wai Ke Za Zhi ; 17(12): 1183-6, 2014 Dec.
Artigo em Chinês | MEDLINE | ID: mdl-25529948

RESUMO

OBJECTIVE: To explore the value of preoperative evaluation with three-dimensional endoanal ultrasonography (3D-EAUS) for anal fistula in order to provide preoperative assessment for anal fistula. METHODS: One hundred patients diagnosed with anal fistula undergoing surgery between March 2012 and March 2013 in our department were prospectively enrolled. All the patients were randomly divided into the ultrasound group and the control group with fifty patients in each group. The ultrasound group received 3D-EAUS and the control group received routine examinations (digital examination and probe) to assess the position of the internal opening, the type of fistula and secondary tracks, respectively. The concordance rate of the preoperative assessment and intraoperative exploration was evaluated between the two groups. RESULTS: The accuracy of identifying internal opening was 96.0% for the ultrasound group and 82.0% for the control group with statistically significant difference (P=0.02). The accuracy of identifying internal opening for simple anal fistula was similar (95.0% vs. 91.3%, P=1). For complex anal fistula, the accuracy was also higher in the ultrasound group (96.7% vs. 74.1%, P=0.025). The accuracy of fistula classification was 78.0% for the ultrasound group and 96.0% for the control group with significant difference (P=0.01). The accuracy of identifying a second track was higher in the ultrasound group (96.0% vs. 82.0%, P=0.025). CONCLUSIONS: It is significantly superior for 3D-EAUS to detect the internal opening, fistula classification and identification of a second track in complex anal fistulas as compared to conventional examination. 3D-EAUS should be recommended as a preoperative assessment for anal fistula, especially for complex one.


Assuntos
Endossonografia , Fístula Retal/diagnóstico por imagem , Humanos , Imageamento Tridimensional , Exame Físico , Fístula Retal/diagnóstico
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