Chukwuma Ifeoma F, Atikpoh Chidi E, Apeh Victor O, Nworah Florence N, Ezeanyika Lawrence Us
Department of Biochemistry, Faculty of Biological Sciences, University of Nigeria, Nsukka, Nigeria.
Department of Genetics and Biotechnology, Faculty of Biological Sciences, University of Nigeria, Nsukka, Nigeria.
Bioinform Biol Insights. 2024 Aug 23;18:11779322241271537. doi: 10.1177/11779322241271537. eCollection 2024.
Oxidative stress is implicated in several metabolic cascades involved in glucose control. Hence, investigating antioxidant and antidiabetic activities is crucial for discovering an effective diabetes mellitus (DM) agent. This study was aimed at probing the therapeutic efficacy of hydro-ethanolic extract of (HECP) and gas chromatography-flame ionization detector (GC-FID)-identified phytochemicals as novel agents for DM.
We determined the total phenols, flavonoids, and antioxidant vitamins in HECP using standard methods. A GC-FID was used to decipher phytochemicals of HECP. The antioxidant and antidiabetic activities of HECP were assessed using in vitro and in silico approaches.
The results revealed that HECP is affluent in phenols, flavonoids, and vitamin E and demonstrated engaging antioxidant activities in 1,1-diphenyl-2-picryl-hydroxyl (DPPH; IC = 0.83 µg/mL), thiobarbituric acid-reactive substances TBARS; IC = 2.28 µg/mL), and ferric-reducing antioxidant power assay (FRAP; IC = 2.89 µg/mL). Compared with the reference drug, acarbose, HECP exhibited good α-amylase and α-glucosidase inhibitory capacity, having IC values of 14.21 and 13.23 µg/mL, respectively, against 13.06 and 11.71 µg/mL recorded for acarbose. More so, the extract's top 6 scoring phytochemicals (rutin, kaempferol, epicatechin, ephedrine, naringenin, and resveratrol) had strong interactions with amino acid residues within and around α-amylase and α-glucosidase active site domains. All the compounds but rutin had favourable drug-like characteristics, pharmacokinetics, and safety profiles when compared with acarbose.
Altogether, our results vindicate the use of this herb in treating DM locally and reveal that it has pharmaceutically active components that could be used as novel leads in the development of DM drugs.
氧化应激与参与血糖控制的多个代谢级联反应有关。因此，研究抗氧化和抗糖尿病活性对于发现有效的糖尿病药物至关重要。本研究旨在探究[植物名称]水乙醇提取物（HECP）以及气相色谱-火焰离子化检测器（GC-FID）鉴定的植物化学物质作为新型糖尿病药物的治疗效果。
我们采用标准方法测定了HECP中的总酚、黄酮类化合物和抗氧化维生素。使用GC-FID解析HECP的植物化学物质。采用体外和计算机模拟方法评估HECP的抗氧化和抗糖尿病活性。
结果显示，HECP富含酚类、黄酮类化合物和维生素E，并在1,1-二苯基-2-苦基肼（DPPH；IC = 0.83μg/mL）、硫代巴比妥酸反应性物质（TBARS；IC = 2.28μg/mL）以及铁还原抗氧化能力测定（FRAP；IC = 2.89μg/mL）中表现出显著的抗氧化活性。与参考药物阿卡波糖相比，HECP表现出良好的α-淀粉酶和α-葡萄糖苷酶抑制能力，其IC值分别为14.21和13.23μg/mL，而阿卡波糖的IC值分别为13.06和11.71μg/mL。此外，提取物得分最高的6种植物化学物质（芦丁、山奈酚、表儿茶素、麻黄碱、柚皮素和白藜芦醇）与α-淀粉酶和α-葡萄糖苷酶活性位点结构域内及周围的氨基酸残基有强烈相互作用。与阿卡波糖相比，除芦丁外的所有化合物均具有良好的类药物特性、药代动力学和安全性。
总体而言，我们的结果证明了这种草药在当地治疗糖尿病的用途，并表明它具有可作为开发糖尿病药物新先导物的药学活性成分。
