Abstract：
The antidiabetic action of traditional plants is mostly attributed to their antioxidant and anti-inflammatory properties. These plants are still having some secrets, making them an attractive source that allows for investigating new drugs or uncovering precise pharmacologic antidiabetic functions of their constituents. In diabetes, which is a lipid disease, long-term exposure of pancreatic islet beta cells to fatty acids (FAs) increases basal insulin release, reduces glucose-stimulated insulin secretion, causes islet beta cell inflammation, failure and apoptosis. Pancreatic islet beta cells express fatty acid binding protein 3 (FABP3) that receives long-chain FAs and traffics them throughout different cellular compartments to be metabolized and render their effects. Inhibition of this FABP3 may retard FA metabolism and protect islet beta cells. Since FAs interact with FABPs by their carboxylic group, some traditionally-known antidiabetic plants were reviewed in the present study, searching for their components that have common features of FABP ligands, namely carboxylic group and hydrophobic tail. Many of these carboxylic acids were computationally introduced into the ligand-binding pocket of FABP3 and some of them exhibited FABP3 ligand possibilities. Among others, the naturally occurring ferulic, cleomaldeic, caffeic, sinapic, hydroxycinnamic, 4-p-coumaroylquinic, quinoline-2-carboxylic, chlorogenic, 6-hydroxykynurenic, and rosmarinic acids in many plants are promising candidates for being FABP3-specific inhibitors. The study shed light on repurposing these phyto-carboxylic acids to function as FABP inhibitors. However, more in-depth biological and pharmacological studies to broaden the understanding of this function are needed.
摘要：
传统植物的抗糖尿病作用主要归因于它们的抗氧化和抗炎特性。这些植物仍然有一些秘密，使它们成为有吸引力的来源，可以研究新药或揭示其成分的精确药理抗糖尿病功能。在糖尿病中，这是一种脂质疾病，胰岛β细胞长期暴露于脂肪酸（FAs）会增加基础胰岛素的释放，减少葡萄糖刺激的胰岛素分泌，导致胰岛β细胞炎症，失败和凋亡。胰岛β细胞表达脂肪酸结合蛋白3（FABP3），该蛋白接受长链FA，并将其运送到不同的细胞区室进行代谢并发挥其作用。抑制该FABP3可以延缓FA代谢并保护胰岛β细胞。由于FAs通过羧基与FABP相互作用，本研究综述了一些传统上已知的抗糖尿病植物，寻找具有FABP配体共同特征的组分，即羧基和疏水尾部。这些羧酸中的许多通过计算被引入FABP3的配体结合袋中，其中一些表现出FABP3配体的可能性。其中,天然存在的阿魏酸，cleomaldeic,咖啡因，Sinapic,羟基肉桂酸，4-p-香豆酰基奎尼酸，喹啉-2-羧酸，绿原，6-羟基犬尿氨酸，和迷迭香酸在许多植物中是有希望的候选FABP3特异性抑制剂。该研究揭示了将这些植物羧酸重新用作FABP抑制剂。然而,需要更深入的生物学和药理学研究来拓宽对这一功能的理解。
