背景:传统上,FicusbenghalensisL.用于治疗代谢紊乱,并且也记录在印度的阿育吠陀药典中。本研究旨在评估水醇提取物/部分的抗糖尿病特性。在体外,和离体方法。
方法:酶抑制活性,大鼠半膈的葡萄糖摄取,和葡萄糖通透性,和吸附测定使用适用的体外和离体方法进行。Further,PASS用于鉴定可能的铅酶抑制剂。通过LC-MS确认了预测的酶抑制剂的存在。同样,使用autodock4.0进行配体与各自靶标的对接。
结果:富含黄酮的部分具有最高的α-淀粉酶,和α-葡萄糖苷酶抑制活性,其次是对大鼠隔膜中葡萄糖摄取的最大功效。同样,水醇提取物对葡萄糖扩散的抑制作用最高。同样,预测3,4-二羟基苯甲酸对α-淀粉酶的药理活性最高,用于PTP1B的熊果酸,和芹菜素分别抑制α-葡萄糖苷酶。LC-MS分析还鉴定了上述命中分子在水醇提取物中的存在。
结论:3,4-二羟基苯甲酸的类似物,芹菜素,熊果酸可以选择铅作为α-淀粉酶,α-葡萄糖苷酶,和PTP1B抑制剂。此外,来自F.benghalensis的水醇提取物的大多数次生代谢产物可能参与增强葡萄糖摄取以支持糖发生过程。
BACKGROUND: Traditionally, Ficus benghalensis L. is used to treat metabolic disorders and is also recorded in the Ayurvedic pharmacopeia of India. The present study aimed to evaluate the anti-diabetic property of hydroalcoholic extract/fraction(s) of F. benghalensis L. bark via in silico, in vitro, and ex vivo approach.
METHODS: Enzyme inhibitory activity, glucose uptake in rat hemidiaphragm, and glucose permeability, and adsorption assays were performed using in vitro and ex vivo methods as applicable. Further, the PASS was used to identify the probable lead enzyme inhibitors. The presence of predicted enzyme inhibitors was confirmed via the LC-MS. Similarly, the docking of ligands with respective targets was performed using autodock4.0.
RESULTS: Flavonoids rich fraction possessed the highest α-amylase, and α-glucosidase inhibitory activity followed by maximum efficacy for glucose uptake in rat hemidiaphragm. Similarly, the hydroalcoholic extract showed the highest efficacy to inhibit glucose diffusion. Likewise, 3,4-dihydroxybenzoic acid was predicted for the highest pharmacological activity for α-amylase, ursolic acid for PTP1B, and apigenin for α-glucosidase inhibition respectively. The LC-MS analysis also identified the presence of the above hit molecules in the hydroalcoholic extract.
CONCLUSIONS: The analogs of 3,4-dihydroxybenzoic acid, apigenin, and ursolic acid could be the choice of lead hits as the α-amylase, α-glucosidase, and PTP1B inhibitors respectively. Additionally, the majority of secondary metabolites from the hydroalcoholic extract of F. benghalensis may be involved in enhancing the glucose uptake to support the process of glycogenesis.