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1.
Arch Biochem Biophys ; 593: 1-11, 2016 Mar 01.
Artigo em Inglês | MEDLINE | ID: mdl-26829674

RESUMO

Sugar induced cataractogenesis and visual impairment is more prominent ophthalmic problem in humans suffering from diabetes. Flavonoids have been identified as one of the therapeutically important class of phytochemicals possessing myriad of biological activities. Analyzing the anti-cataract effects of flavonoids from natural sources is an important aspect owing to their bioavailability in variety of dietary sources. In the present study a panel of ten dietary flavonoids like 3, 6-dihydroxy flavone, 3, 7-dihydroxy flavone, chrysin, 3-hydroxy-7-methoxy flavone, apigenin, genistein, baicalein, galangin, Biochanin-A, and diosmin were evaluated for their anti-cataract effects in sugar induced lens model studies. Series of parameters like role of flavonoids in glycation induced lens opacity, protein aggregation measurements, carbonyl group formation: a biochemical marker of glycation reaction, non-tryptophan fluorescence: a marker of formation of advanced glycation end products (AGEs) and assessment of (experimental and in silico) aldose reductase inhibition: a key enzyme of polyol pathway involved in cataractogenesis. The results of the study clearly demonstrated the impressive anti-cataract activity of chrysin followed by significant activity by apigenin, baicalein and genistein. The results of the present study may find applications in formulation of functional foods and neutraceuticals for the management of diabetic cataract.


Assuntos
Catarata/tratamento farmacológico , Flavonoides/farmacologia , Glucose , Cristalino/efeitos dos fármacos , Compostos Fitoquímicos/farmacologia , Aldeído Redutase/antagonistas & inibidores , Aldeído Redutase/química , Animais , Catarata/induzido quimicamente , Simulação por Computador , Carboidratos da Dieta , Proteínas do Olho/metabolismo , Flavonoides/química , Glicosilação , Cabras , Técnicas In Vitro , Cristalino/metabolismo , Cristalino/patologia , Simulação de Acoplamento Molecular , Compostos Fitoquímicos/química , Agregados Proteicos , Carbonilação Proteica , Relação Estrutura-Atividade
2.
J Enzyme Inhib Med Chem ; 28(3): 593-600, 2013 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-22380776

RESUMO

A series of novel carbazole chalcones has been synthesised and evaluated for radical scavenging activity, cytotoxicity and antimicrobial activities. Compounds 12m, 12o and 12c exhibited good 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activity, compounds 12e, 12m and 12d were excellent hydroxyl radical scavengers and compounds 12a, 12e, 12g, 12n and 12m have shown inhibition of oxidative DNA damage induced by 2,2'-azobis (2-amidinopropane hydrochloride). Compounds 12j, 12i, 12n, 12c, 12m and 12e were most active against the selected cancer cell lines. Compounds 12a, 12e and 12m showed good antibacterial activity and compounds 12h and 12m have shown good antifungal activity. All the compounds were subjected for absorption, distribution, metabolism and excretion (ADME) predictions by computational method and found that these molecules could be considered as potential candidates for oral drug development.


Assuntos
Anti-Infecciosos/síntese química , Anti-Infecciosos/farmacologia , Anticarcinógenos/síntese química , Anticarcinógenos/farmacologia , Carbazóis/química , Chalconas/química , Administração Oral , Anti-Infecciosos/química , Anti-Infecciosos/farmacocinética , Anticarcinógenos/química , Anticarcinógenos/farmacocinética , Antifúngicos/síntese química , Antifúngicos/química , Antifúngicos/farmacologia , Antioxidantes/síntese química , Antioxidantes/química , Antioxidantes/farmacologia , Linhagem Celular Tumoral , Técnicas de Química Sintética , Ensaios de Seleção de Medicamentos Antitumorais , Sequestradores de Radicais Livres/síntese química , Sequestradores de Radicais Livres/química , Sequestradores de Radicais Livres/farmacocinética , Sequestradores de Radicais Livres/farmacologia , Humanos , Relação Estrutura-Atividade , Distribuição Tecidual
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