Paul Saptadipa, Majumdar Mala
Department of Biotechnology, School of Sciences, JAIN (Deemed to Be University), #34,1st Cross, J C Road, Bangalore, 560027, India.
Appl Biochem Biotechnol. 2023 Apr;195(4):2261-2281. doi: 10.1007/s12010-022-04064-7. Epub 2022 Jul 7.
Antidiabetic polyherbal formulations (APH) are used in management of diabetes mellitus (DM). High glucose levels in DM are related to oxidative stress leading to its associated complications. Therefore, assessing antioxidant activity of various APH might unveil an antioxidant-rich formulation for management of DM and its associated complications. Subsequently selecting an antioxidant assessment method is a challenging aspect, considering various in vitro assays working with diverse mechanism of action. Therefore, present study aims to validate the sensitivity/capacity of different antioxidant assay, thereby assessing the antioxidant potential of 9-APH. Obtained results revealed the ABTS· values were higher compared to DPPH assay. I-9-HAE (DPPH: IC 53.31 µg/ml), NK-HAE (ABTS·: IC 2.71 µg/ml), and MN-HAE (FRAP and TAC) exhibited highest antioxidant capacity. A significant correlation was obtained between TPC-DPPH (r: 0.8187****). Furthermore, three APH with better antiradical potential was chosen for various in vitro and in silico method, for validating scientific antidiabetic propensities. Among the tested extracts, I-9-HAE (α-amylase inhibition: IC 831.84 µg/ml) and MN-HAE (α-glucosidase inhibition: IC 558.64 µg/ml and antiglycation: IC 883.74 µg/ml) have showed highest antihyperglycemic and antiglycation properties. Finally, the secondary-metabolites of selected APH were screened through literature search, Lipinski rule, ADMET, and ProTox-II. Subsequently, in molecular docking for the selected 9 secondary metabolites, highest binding affinity was observed in apigenin-7-glucuronide for DPPiv (- 9.6), GLP-1 (- 8.8), NADPH (- 8.7), and HSA (- 9.4). Thus, obtained result proposes synergistic interaction with high antioxidant potential of the selected 3-APH and can be considered an alternative for management of DM, where multiple secondary metabolites exert holistic biological effects. Furthermore, our study also provides data on sensitivity/capacity of different in vitro antioxidant assays.
抗糖尿病多草药配方（APH）用于糖尿病（DM）的管理。糖尿病中的高血糖水平与氧化应激有关，进而导致其相关并发症。因此，评估各种APH的抗氧化活性可能会揭示一种富含抗氧化剂的配方，用于管理糖尿病及其相关并发症。考虑到各种体外试验的作用机制不同，选择一种抗氧化评估方法是一个具有挑战性的方面。因此，本研究旨在验证不同抗氧化试验的灵敏度/能力，从而评估9-APH的抗氧化潜力。获得的结果显示，与DPPH试验相比，ABTS·值更高。I-9-HAE（DPPH：IC53.31µg/ml）、NK-HAE（ABTS·：IC2.71µg/ml）和MN-HAE（FRAP和TAC）表现出最高的抗氧化能力。TPC-DPPH之间获得了显著相关性（r：0.8187****）。此外，选择了三种具有更好抗自由基潜力的APH用于各种体外和计算机模拟方法，以验证其科学的抗糖尿病倾向。在测试的提取物中，I-9-HAE（α-淀粉酶抑制：IC831.84µg/ml）和MN-HAE（α-葡萄糖苷酶抑制：IC558.64µg/ml和抗糖化：IC883.74µg/ml）表现出最高的降血糖和抗糖化特性。最后，通过文献检索、Lipinski规则、ADMET和ProTox-II对所选APH的次生代谢产物进行了筛选。随后，在对所选9种次生代谢产物的分子对接中，芹菜素-7-葡萄糖醛酸对DPPiv（-9.6）、GLP-1（-8.8）、NADPH（-8.7）和HSA（-9.4）表现出最高的结合亲和力。因此，获得的结果表明所选3-APH具有高抗氧化潜力的协同相互作用，可被视为糖尿病管理的替代方案，其中多种次生代谢产物发挥整体生物学效应。此外，我们的研究还提供了不同体外抗氧化试验的灵敏度/能力数据。
