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Anna Ntsoaki Nyane

University of KwaZulu-Natal, South Africa

Title: Characterising Chalo-Naringenin analogs as putative therapeutic agents for type 2 diabetes

Biography

Biography: Anna Ntsoaki Nyane

Abstract

Type 2 diabetes (T2D) is characterized by impaired insulin secretion and peripheral insulin resistance. Despite many classes of drugs available, T2D is still projected to increase by 55% in 2035. Citrus fruit-derived fl avonoid, naringenin has been reported to have antidyslipidemic, anti-oxidant and more recently metformin-like antidiabetic eff ects. Metformin, the most commonly used drug for T2D management acts by activating adenosine monophosphate activated protein kinase (AMPK). Naringenin’s anti-diabetic effects could be mediated by AMPK activation. Although naringenin has been shown to have anti-diabetic properties, it is less lipophilic and has poor water solubility hence chalco-naringenin analogs with enhanced pharmacological activities were synthesized. A series of 11 compounds of 4-[(cyclopropylcarbonyl) amino] chalco-naringenin analogues were synthesized using Claisen-Schmidt and characterized by IR, 1H-NMR and 13 C-NMR. An intermediate compound, N-(3-acetylphenyl) cyclopropanecarboxamide synthesized was reacted with commercially available aldehydes to yield the fi nal amino-chalco-naringenin series. Th e synthesized compounds showed characteristic peaks on IR, 1H-NMR and 13 C-NMR and fi t very well in the hydrophobic binding pockets of
AMPK. Th ey also presented good binding affi nity to the enzyme as shown by computer simulation suggesting potential metforminlike antidiabetic eff ects. Further, in vitro and in vivo antidiabetic studies are suggested to elucidate the molecular mechanisms of these compounds.