title: Chalcones and their therapeutic targets for the management of diabetes: structural and pharmacological perspectives.
abstract: Diabetes Mellitus (DM) is the fastest growing metabolic disorder affecting about 387 million people across the globe and is estimated to affect 592 million people by year 2030. The search for newer anti-diabetic agents is the foremost need to control the accelerating diabetic population. Several natural and (semi) synthetic chalcones deserve the credit of being potential candidates that act by modulating the therapeutic targets PPAR-γ, DPP-4, α-glucosidase, PTP1B, aldose reductase, and stimulate insulin secretion and tissue sensitivity. In this review, a comprehensive study (from January 1977 to October 2014) of anti-diabetic chalcones, their molecular targets, structure activity relationships (SARs), mechanism of actions (MOAs) and patents have been described. The compounds which showed promising activity and have a well-defined MOAs, SARs must be considered as prototype for the design and development of potential anti-diabetic agents. They should be evaluated critically at all clinical stages to ensure their therapeutic and toxicological profile to meet the demand of diabetics.
authors: Institute of Pharmaceutical Sciences, Guru Ghasidas Vishwavidyalaya (A Central University), Bilaspur 495009, Chhattisgarh, India.
authors: Debarshi Kar
authors: DK
authors: Mahapatra
authors: Institute of Pharmaceutical Sciences, Guru Ghasidas Vishwavidyalaya (A Central University), Bilaspur 495009, Chhattisgarh, India.
authors: Vivek
authors: V
authors: Asati
authors: Institute of Pharmaceutical Sciences, Guru Ghasidas Vishwavidyalaya (A Central University), Bilaspur 495009, Chhattisgarh, India. Electronic address: skbharti.ggu@gmail.com.
authors: Sanjay Kumar
authors: SK
authors: Bharti
mesh_terms: D047188:Chalcones / Q000737:chemistry / Q000627:therapeutic use*; D003920:Diabetes Mellitus / Q000188:drug therapy* / Q000378:metabolism; D065089:Glycoside Hydrolase Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D007004:Hypoglycemic Agents / Q000737:chemistry / Q000627:therapeutic use*; D015394:Molecular Structure; D013329:Structure-Activity Relationship; D000520:alpha-Glucosidases / Q000378:metabolism
chemical_list: D047188:Chalcones; D065089:Glycoside Hydrolase Inhibitors; D007004:Hypoglycemic Agents; D000520:alpha-Glucosidases
keywords: Chalcone; DPP-4; Diabetes; PPAR-γ; PTP1B; α-Glucosidase