Institute of Pharmaceutical Sciences, Guru Ghasidas Vishwavidyalaya (A Central University), Bilaspur 495009, Chhattisgarh, India.
Institute of Pharmaceutical Sciences, Guru Ghasidas Vishwavidyalaya (A Central University), Bilaspur 495009, Chhattisgarh, India.
Eur J Med Chem. 2015 Mar 6;92:839-65. doi: 10.1016/j.ejmech.2015.01.051. Epub 2015 Jan 26.
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.
糖尿病（DM）是全球增长最快的代谢紊乱疾病，影响着约 3.87 亿人，预计到 2030 年将影响 5.92 亿人。寻找新的抗糖尿病药物是控制不断增长的糖尿病患者群体的首要需求。几种天然和（半）合成查耳酮被认为是有潜力的候选药物，它们通过调节治疗靶点 PPAR-γ、DPP-4、α-葡萄糖苷酶、PTP1B、醛糖还原酶，并刺激胰岛素分泌和组织敏感性来发挥作用。在这篇综述中，对具有抗糖尿病活性的查耳酮及其分子靶标、构效关系（SAR）、作用机制（MOA）和专利进行了全面的研究（从 1977 年 1 月到 2014 年 10 月）。对于那些显示出有前途的活性且具有明确 MOA 和 SAR 的化合物，应将其视为设计和开发潜在抗糖尿病药物的原型。在所有临床阶段都必须对它们进行严格评估，以确保其治疗和毒理学特征符合糖尿病患者的需求。
