Nano Center Indonesia, South Tangerang 15314, Indonesia.
Department of Chemistry, Faculty of Mathematics and Natural Sciences, Universitas Indonesia, Depok 16424, Indonesia.
Molecules. 2022 Jun 21;27(13):3972. doi: 10.3390/molecules27133972.
Propolis contains a wide range of pharmacological activities because of their various bioactive compounds. The beneficial effect of propolis is interesting for treating type-2 diabetes mellitus (T2DM) owing to dysregulation of multiple metabolic processes. In this study, 275 of 658 Asian propolis compounds were evaluated as potential anti-T2DM agents using the DIA-DB web server towards 18 known anti-diabetes protein targets. More than 20% of all compounds could bind to more than five diabetes targets with high binding affinity (<−9.0 kcal/mol). Filtering with physicochemical and pharmacokinetic properties, including ADMET parameters, 12 compounds were identified as potential anti-T2DM with favorable ADMET properties. Six of those compounds, (2R)-7,4′-dihydroxy-5-methoxy-8-methylflavone; (RR)-(+)-3′-senecioylkhellactone; 2′,4′,6′-trihydroxy chalcone; alpinetin; pinobanksin-3-O-butyrate; and pinocembrin-5-methyl ether were first reported as anti-T2DM agents. We identified the significant T2DM targets of Asian propolis, namely retinol-binding protein-4 (RBP4) and aldose reductase (AKR1B1) that have important roles in insulin sensitivity and diabetes complication, respectively. Molecular dynamic simulations showed stable interaction of selected propolis compounds in the active site of RBP4 and AKR1B1. These findings suggest that Asian propolis compound may be effective for treatment of T2DM by targeting RBP4 and AKR1B1.
蜂胶因其多种生物活性化合物而具有广泛的药理活性。由于多种代谢过程的失调,蜂胶对治疗 2 型糖尿病(T2DM)的有益作用引起了人们的兴趣。在这项研究中,使用 DIA-DB 网络服务器,对 658 种亚洲蜂胶化合物中的 275 种进行了评估,作为潜在的抗 T2DM 药物,针对 18 种已知的抗糖尿病蛋白靶标。超过 20%的化合物可以与 5 个以上的糖尿病靶标结合,具有高结合亲和力(<−9.0kcal/mol)。通过筛选物理化学和药代动力学特性,包括 ADMET 参数,确定了 12 种具有潜在抗 T2DM 作用和良好 ADMET 特性的化合物。其中 6 种化合物,(2R)-7,4′-二羟基-5-甲氧基-8-甲基黄酮;(RR)-(+)-3′-千里光酰基角鲨烯;2′,4′,6′-三羟基查耳酮;白杨素;松柏醇-3-O-丁酸酯;和 pinocembrin-5-甲醚,是首次被报道为抗 T2DM 药物。我们确定了亚洲蜂胶的重要 T2DM 靶标,即视黄醇结合蛋白-4(RBP4)和醛糖还原酶(AKR1B1),它们分别在胰岛素敏感性和糖尿病并发症中起着重要作用。分子动力学模拟显示,所选蜂胶化合物在 RBP4 和 AKR1B1 的活性部位的相互作用稳定。这些发现表明,亚洲蜂胶化合物可能通过靶向 RBP4 和 AKR1B1 有效治疗 T2DM。