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1.
Biol Pharm Bull ; 43(1): 59-67, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-31902933

RESUMO

Grape extract (GE), which contains various polyphenolic compounds, exerts protective effects against lifestyle-related diseases, such as diabetes and hypertension. We pharmacologically investigated whether dietary supplements with an extract from Chardonnay exerted antihypertensive effects in deoxycorticosterone acetate (DOCA)-salt-induced hypertensive rats. GE increased nitric oxide (NO) production by activating the phosphatidylinositol 3-kinase (PI3K)/Akt pathway in cultured endothelial cells and induced vasorelaxation in the aorta and mesenteric artery via the same pathway. The development and progression of hypertension by the DOCA-salt treatment was significantly inhibited in GE-fed rats. Reduced vasoreactive responses to acetylcholine in the aorta of DOCA-salt rats were significantly ameliorated by the GE diet. Dietary GE supplements slightly diminished vascular superoxide anion production induced by the DOCA-salt treatment. On the other hand, dietary GE supplements had no effect on the progression of hypertension in rats in which NO synthase was pharmacologically and chronically suppressed. In addition, the oral administration of GE for 5 d in healthy rats enhanced endothelial NO synthase (eNOS) gene expression and vascular reactivity to acetylcholine in the aorta. Thus, GE has endothelium-dependent vasorelaxant properties that are mediated by the activation of endothelial NO synthase via the PI3K/Akt pathway, and this mechanism is conducive to the antihypertensive effects of GE observed in DOCA-salt-treated rats.


Assuntos
Hipertensão/tratamento farmacológico , Extratos Vegetais/uso terapêutico , Vasodilatadores/uso terapêutico , Vitis , Animais , Aorta Torácica/efeitos dos fármacos , Aorta Torácica/fisiologia , Linhagem Celular , Acetato de Desoxicorticosterona , Células Endoteliais/efeitos dos fármacos , Células Endoteliais/metabolismo , Endotélio Vascular/efeitos dos fármacos , Endotélio Vascular/fisiologia , Humanos , Hipertensão/induzido quimicamente , Hipertensão/genética , Hipertensão/fisiopatologia , Masculino , Artérias Mesentéricas/efeitos dos fármacos , Artérias Mesentéricas/fisiologia , Óxido Nítrico/metabolismo , Óxido Nítrico Sintase Tipo III/genética , Extratos Vegetais/farmacologia , Ratos Sprague-Dawley , Sementes , Vasodilatação/efeitos dos fármacos , Vasodilatadores/farmacologia
2.
Yakugaku Zasshi ; 126(5): 349-56, 2006 May.
Artigo em Japonês | MEDLINE | ID: mdl-16679743

RESUMO

Brand name confusion is one of the most common causes of drug-related errors. The aim of this study was to develop quantitative measures of similarity among brand names of drugs. We modified the fragmentary pattern-based measure, a measure of similarity for character strings based on the string resemblance system, to develop three novel measures of similarity, i.e., the head and tail-weighted fragmentary pattern-based measure (htfrag), visually weighted htfrag (vwhtfrag), and auditorily weighted htfrag (awhtfrag). The 227 pairs of brand names for which confusion errors have been reported were used as a positive control group. Ten sets of 2270 random pairs of brand names were generated as negative controls. Then we evaluated the measures developed by using the geometric mean of sensitivity and selectivity as an objective function, in comparison with two conventional measures of similarity based on the vector space model (cos1 and htco). The measures developed, htfrag, vwhtfrag, and awhtfrag, provided better discrimination with mean objective function values of 0.953, 0.962, and 0.940, respectively, which were higher than those for the conventional measures cos1 and htco (0.922 and 0.892, respectively). The rates of false-positives and false-negatives were 3.3-10.7% and 5.3-11.9% for cos1, respectively, while the rates for vwhtfrag were 4.8-5.9% and 2.2%, respectively. The measures of similarity developed may provide significant information to avoid drug-related errors associated with brand name confusion.


Assuntos
Erros de Medicação/prevenção & controle , Preparações Farmacêuticas , Terminologia como Assunto , Distribuição Aleatória
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