Nitrochalcones: Potential in vivo insulin secretagogues |
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| Authors: | Rosangela Guollo Damazio Ana Paula Zanatta Luisa Helena Cazarolli Alessandra Mascarello Louise Domeneghini Chiaradia Ricardo José Nunes Rosendo Augusto Yunes Fátima Regina Mena Barreto Silva |
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| Institution: | 1. Universidade Federal de Santa Catarina, Departamento de Bioquímica, Centro de Ciências Biológicas, Campus Universitário, Bairro Trindade, Cx. Postal 5069, CEP: 88040-970, Florianópolis, SC, Brazil;2. Universidade Federal de Santa Catarina, Departamento de Química, Centro de Ciências Físicas e Matemáticas, Campus Universitário, Bairro Trindade, CEP: 88040-900, Florianópolis, SC, Brazil;1. Department of Biochemistry, Sri Venkateswara University, Tirupati, Andhra Pradesh 517 502, India;2. Department of Chemistry, Sri Venkateswara University, Tirupati, Andhra Pradesh 517 502, India;1. Department of Chemistry, College of Science, Engineering and Technology, University of South Africa, Private Bag X06, Florida 1710, South Africa;2. Department of Life & Consumer Sciences, College of Agriculture and Environmental Sciences, University of South Africa, Private Bag X06, Florida 1710, South Africa;1. Department of Chemistry, Alzahra University, Vanak, Tehran, Iran;2. Department of Chemistry, Islamic Azad University, Shahrood Branch, Shahrood, Iran;1. Department of Chemistry, College of Science, Engineering and Technology, University of South Africa, PO Box 392, Pretoria 0003, South Africa;2. Computational Chemistry Group, Department of Chemistry, Faculty of Science, University of Mauritius, Réduit 80837, Mauritius |
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| Abstract: | In this study, the in vivo and in vitro anti-hyperglycemic activity of chalcone derivatives of 3,4-methylenedioxy, with a substituent electron-acceptor nitro group in the A or B ring, was investigated. As expected, the second generation sulfonylurea glipizide stimulated insulin secretion and reduced glycemia over the study period. Also, it was demonstrated for the first time that chalcones are able to increase insulin secretion and this event was coincident with serum glucose-lowering in the oral glucose tolerance test. Additionally, the chalcones studied had a similar effect on insulin secretion and serum glucose-lowering as glipizide. The effect of chalcones in terms of inducing insulin secretion was greater than that of glipizide after 30 min. Moreover, chalcones were not able to stimulate glucose uptake in soleus muscle, either in the presence of insulin or in the absence of this hormone. In addition, the oral treatment with chalcones did not alter glycemia in diabetic rats. These reports indicate that the effect of chalcones on serum glucose-lowering in hyperglycemic-normal rats is mainly a consequence of insulin secretion, highlighting these chalcones as novel compounds with strong anti-hyperglycemic properties. |
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