期刊
CURRENT MEDICINAL CHEMISTRY
卷 27, 期 14, 页码 2257-2321出版社
BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/0929867325666181001112226
关键词
Anti-diabetic drugs; chalcones; Dipeptidyl Peptidase 4 (DPP-4); Glucose Transporter Type 4 (GLUT4); Sodium Glucose Cotransporter 2 (SGLT2); alpha-amylase; alpha-glucosidase; Aldose Reductase (ALR); Protein Tyrosine Phosphatase 1B (PTP1B); Peroxisome Proliferator-activated Receptor-gamma (PPAR.); Adenosine Monophosphate (AMP)-activated Protein Kinase (AMPK); Structure-activity Relationship (SAR)
资金
- European Union (FEDER funds) [POCI/01/0145/FEDER/007265]
- National Funds (FCT/MEC, Fundacao para a Ciencia e Tecnologia) [PT2020 UID/QUI/50006/2013]
- National Funds (FCT/MEC, Ministerio da Educacao e Ciencia) [PT2020 UID/QUI/50006/2013]
- Programa Operacional Competitividade e Internacionalizacao (COMPETE) [POCI-01-0145-FEDER-029241]
- QREN [NORTE-01-0145-FEDER000024]
The use of anti-diabetic drugs has been increasing worldwide and the evolution of therapeutics has been enormous. Still, the currently available anti-diabetic drugs do not present the desired efficacy and are generally associated with serious adverse effects. Thus, entirely new interventions, addressing the underlying etiopathogenesis of type 2 diabetes mellitus, are required. Chalcones, secondary metabolites of terrestrial plants and precursors of the flavonoids biosynthesis, have been used for a long time in traditional medicine due to their wide-range of biological activities, from which the anti-diabetic activity stands out. This review systematizes the information found in literature about the anti-diabetic properties of chalcones, in vitro and in vivo. Chalcones are able to exert these properties by acting in different therapeutic targets: Dipeptidyl Peptidase 4 (DPP-4); Glucose Transporter Type 4 (GLUT4), Sodium Glucose Cotransporter 2 (SGLT2), alpha-amylase, alpha-glucosidase, Aldose Reductase (ALR), Protein Tyrosine Phosphatase 1B (PTP1B), Peroxisome Proliferator-activated Receptor-gamma (PPAR.) and Adenosine Monophosphate (AMP)-activated Protein Kinase (AMPK). Chalcones are, undoubtedly, promising anti-diabetic agents, and some crucial structural features have already been established. From the Structure-Activity Relationships analysis, it can generally be stated that the presence of hydroxyl, prenyl and geranyl groups in their skeleton improves their activity for the evaluated anti-diabetic targets.
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