School of Pharmacy, College of Medicine, National Cheng Kung University, Tainan, 701, Taiwan, ROC.
School of Pharmacy, College of Medicine, National Cheng Kung University, Tainan, 701, Taiwan, ROC.
Eur J Med Chem. 2022 Jul 5;237:114405. doi: 10.1016/j.ejmech.2022.114405. Epub 2022 Apr 22.
Obesity is not only viewed as a chronic aggressive disorder but is also associated with an increased risk for various diseases. Nonetheless, new anti-obesity drugs are an urgent need since few pharmacological choices are available on the market. Natural compounds have served as templates for drug discovery, whereas modified molecules from the leads identified based on in vitro models often reveal noncorresponding bioactivity between in vitro and in vivo studies. Therefore, to provide inspiration for the exploration of innovative anti-obesity agents, recent discoveries of natural anti-obesity compounds with in vivo evidence have been summarized according to their chemical structures, and the comparable efficacy of these compounds is categorized using animal models. In addition, several synthetic derivatives optimized from the phytochemicals are also provided to discuss medicinal chemistry achievements guided by natural sources.
肥胖不仅被视为一种慢性侵袭性疾病，而且还与各种疾病的风险增加有关。然而，由于市场上可供选择的药物很少，因此急需新型减肥药。天然化合物一直是药物发现的模板，而基于体外模型确定的先导化合物的修饰分子，往往揭示了体外和体内研究之间没有对应的生物活性。因此，为了为探索创新型减肥药提供灵感，根据其化学结构总结了具有体内证据的天然减肥药的最新发现，并使用动物模型对这些化合物的可比功效进行了分类。此外，还提供了从植物化学物质中优化的几种合成衍生物，以讨论受天然来源指导的药物化学成就。
