探索康柏提取物和经 GC-FID 鉴定的植物化学物质作为糖尿病新药的疗效

IF 2.3 Q3 BIOCHEMICAL RESEARCH METHODS Bioinformatics and Biology Insights Pub Date : 2024-08-23 eCollection Date: 2024-01-01 DOI:10.1177/11779322241271537
Ifeoma F Chukwuma, Chidi E Atikpoh, Victor O Apeh, Florence N Nworah, Lawrence Us Ezeanyika
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引用次数: 0

摘要

目的:氧化应激与涉及血糖控制的多个代谢级联有关。因此,研究抗氧化和抗糖尿病活性对于发现有效的糖尿病(DM)药物至关重要。本研究的目的是探究穇子的水乙醇提取物(HECP)和气相色谱-火焰离子化检测器(GC-FID)鉴定出的植物化学物质作为糖尿病新药的疗效:我们采用标准方法测定了 HECP 中的总酚、类黄酮和抗氧化维生素。采用气相色谱-质谱联用仪(GC-FID)破译 HECP 的植物化学成分。采用体外和硅学方法评估了 HECP 的抗氧化和抗糖尿病活性:结果表明,HECP富含酚类、黄酮类和维生素E,并在1,1-二苯基-2-吡啶-羟基(DPPH;IC50 = 0.83 µg/mL)、硫代巴比妥酸反应物质(TBARS;IC50 = 2.28 µg/mL)和铁还原抗氧化力测定(FRAP;IC50 = 2.89 µg/mL)中表现出良好的抗氧化活性。与参考药物阿卡波糖相比,HECP 对α-淀粉酶和α-葡萄糖苷酶具有良好的抑制能力,其 IC50 值分别为 14.21 和 13.23 µg/mL,而阿卡波糖的 IC50 值分别为 13.06 和 11.71 µg/mL。此外,提取物中得分最高的 6 种植物化学物质(芦丁、山柰酚、表儿茶素、麻黄素、柚皮苷和白藜芦醇)与α-淀粉酶和α-葡萄糖苷酶活性位点域内和周围的氨基酸残基有很强的相互作用。与阿卡波糖相比,除芦丁外,所有化合物都具有良好的类药物特性、药代动力学和安全性:总之,我们的研究结果证明了这种草药可用于局部治疗糖尿病,并揭示了它具有药物活性的成分,可作为开发糖尿病药物的新线索。
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Probing the Therapeutic Efficacy of Combretum paniculatum Extract and GC-FID-Identified Phytochemicals as Novel Agents for Diabetes Mellitus.

Objectives: 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 Combretum paniculatum (HECP) and gas chromatography-flame ionization detector (GC-FID)-identified phytochemicals as novel agents for DM.

Methods: 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.

Results: 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; IC50 = 0.83 µg/mL), thiobarbituric acid-reactive substances TBARS; IC50 = 2.28 µg/mL), and ferric-reducing antioxidant power assay (FRAP; IC50 = 2.89 µg/mL). Compared with the reference drug, acarbose, HECP exhibited good α-amylase and α-glucosidase inhibitory capacity, having IC50 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.

Conclusion: 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.

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来源期刊
Bioinformatics and Biology Insights
Bioinformatics and Biology Insights BIOCHEMICAL RESEARCH METHODS-
CiteScore
6.80
自引率
1.70%
发文量
36
审稿时长
8 weeks
期刊介绍: Bioinformatics and Biology Insights is an open access, peer-reviewed journal that considers articles on bioinformatics methods and their applications which must pertain to biological insights. All papers should be easily amenable to biologists and as such help bridge the gap between theories and applications.
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