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Identification of new potent inhibitor of aldose reductase from Ocimum basilicum.
Bhatti, Huma Aslam; Tehseen, Yildiz; Maryam, Kiran; Uroos, Maliha; Siddiqui, Bina S; Hameed, Abdul; Iqbal, Jamshed.
Afiliação
  • Bhatti HA; H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi 75270, Pakistan. Electronic address: huma_aslam31@hotmail.com.
  • Tehseen Y; Center for Advanced Drug Research, COMSATS Institute of Information Technology, Abbottabad 22060, Pakistan.
  • Maryam K; Dr. Panjwani Center for Molecular Medicine and Drug Research, International Center for Chemical and Biological Sciences, University of Karachi, Karachi 75270, Pakistan.
  • Uroos M; Institute of Chemistry, The University of the Punjab, Lahore 54000, Pakistan.
  • Siddiqui BS; H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi 75270, Pakistan.
  • Hameed A; H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi 75270, Pakistan.
  • Iqbal J; Center for Advanced Drug Research, COMSATS Institute of Information Technology, Abbottabad 22060, Pakistan. Electronic address: drjamshed@ciit.net.pk.
Bioorg Chem ; 75: 62-70, 2017 12.
Article em En | MEDLINE | ID: mdl-28917123
Recent efforts to develop cure for chronic diabetic complications have led to the discovery of potent inhibitors against aldose reductase (AKR1B1, EC 1.1.1.21) whose role in diabetes is well-evident. In the present work, two new natural products were isolated from the ariel part of Ocimum basilicum; 7-(3-hydroxypropyl)-3-methyl-8-ß-O-d-glucoside-2H-chromen-2-one (1) and E-4-(6'-hydroxyhex-3'-en-1-yl)phenyl propionate (2) and confirmed their structures with different spectroscopic techniques including NMR spectroscopy etc. The isolated compounds (1, 2) were evaluated for in vitro inhibitory activity against aldose reductase (AKR1B1) and aldehyde reductase (AKR1A1). The natural product (1) showed better inhibitory activity for AKR1B1 with IC50 value of 2.095±0.77µM compare to standard sorbinil (IC50=3.14±0.02µM). Moreover, the compound (1) also showed multifolds higher activity (IC50=0.783±0.07µM) against AKR1A1 as compared to standard valproic acid (IC50=57.4±0.89µM). However, the natural product (2) showed slightly lower activity for AKR1B1 (IC50=4.324±1.25µM). Moreover, the molecular docking studies of the potent inhibitors were also performed to identify the putative binding modes within the active site of aldose/aldehyde reductases.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Fenilpropionatos / Benzopiranos / Aldeído Redutase / Ocimum basilicum / Inibidores Enzimáticos / Glucosídeos Tipo de estudo: Diagnostic_studies Idioma: En Revista: Bioorg Chem Ano de publicação: 2017 Tipo de documento: Article País de publicação: Estados Unidos

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Fenilpropionatos / Benzopiranos / Aldeído Redutase / Ocimum basilicum / Inibidores Enzimáticos / Glucosídeos Tipo de estudo: Diagnostic_studies Idioma: En Revista: Bioorg Chem Ano de publicação: 2017 Tipo de documento: Article País de publicação: Estados Unidos