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1.
Food Sci Nutr ; 8(10): 5259-5266, 2020 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-33133528

RESUMO

Dietary fiber is a nondigestible constituent of vegetal foods, formed by insoluble and soluble dietary fiber. The intake of dietary fiber, especially soluble dietary fiber, is limited and demands researcher's attention. The modification of cereal's dietary fiber, predominantly insoluble fiber, could be one possible solution. The current study evaluated the comparative effects of several thermal treatments on the modification of insoluble dietary fiber in barley and explored their therapeutic potential in vivo against hypercholesterolemia. The two cultivars of barley, Haider-93 and Jau-87, were thermally treated using different techniques, and dietary fiber was extracted. Successively, the intake of these dietary fibers was evaluated for its antilipidemic activity in normal and hypercholesterolemic rats. In the first phase, thermal treatments especially cooking without soaking increased the soluble fiber (68.08%). The roasting all increased the soluble fiber contents, however, at relatively lower rate (53.91%). The results of efficacy study revealed that biochemical parameters in control animals were within the normal clinical ranges, thus appraising the safe status of the experimental diets. The thermally treated barley fiber decreased total cholesterol (12.14%-12.63%), low-density lipoprotein (14.12%-14.85%), and triglycerides (2.25%-4.32%). The study recorded increasing trends for high-density lipoprotein in both normal and hypercholesterolemic rats. In the nutshell, thermal modification of dietary fiber increased the ratio of soluble to insoluble dietary fiber that improved its hypocholesterolemic potential. The thermally treated barley dietary fiber is effective in reducing the lipid profile in Sprague-dawley rats than untreated dietary fiber and, therefore, can be considered as a functional food and ingredient to cope different lifestyle diseases.

2.
Molecules ; 21(3): 266, 2016 Feb 25.
Artigo em Inglês | MEDLINE | ID: mdl-26927044

RESUMO

A new series of N-(6-arylbenzo[d]thiazol-2-yl)acetamides were synthesized by C-C coupling methodology in the presence of Pd(0) using various aryl boronic pinacol ester/acids. The newly synthesized compounds were evaluated for various biological activities like antioxidant, haemolytic, antibacterial and urease inhibition. In bioassays these compounds were found to have moderate to good activities. Among the tested biological activities screened these compounds displayed the most significant activity for urease inhibition. In urease inhibition, all compounds were found more active than the standard used. The compound N-(6-(p-tolyl)benzo[d]thiazol-2-yl)acetamide was found to be the most active. To understand this urease inhibition, molecular docking studies were performed. The in silico studies showed that these acetamide derivatives bind to the non-metallic active site of the urease enzyme. Structure-activity studies revealed that H-bonding of compounds with the enzyme is important for its inhibition.


Assuntos
Acetamidas/síntese química , Antibacterianos/síntese química , Antioxidantes/síntese química , Benzotiazóis/síntese química , Inibidores Enzimáticos/síntese química , Urease/antagonistas & inibidores , Acetamidas/farmacologia , Antibacterianos/farmacologia , Antioxidantes/farmacologia , Benzotiazóis/farmacologia , Células Cultivadas , Inibidores Enzimáticos/farmacologia , Eritrócitos/citologia , Eritrócitos/efeitos dos fármacos , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Negativas/crescimento & desenvolvimento , Bactérias Gram-Positivas/efeitos dos fármacos , Bactérias Gram-Positivas/crescimento & desenvolvimento , Hemólise/efeitos dos fármacos , Humanos , Testes de Sensibilidade Microbiana , Simulação de Acoplamento Molecular , Óxido Nítrico/antagonistas & inibidores , Phaseolus/química , Phaseolus/enzimologia , Proteínas de Plantas/antagonistas & inibidores , Proteínas de Plantas/química , Urease/química
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