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生物测定引导的提取物抗糖尿病组分的分离、活性化合物鉴定及预测的相互作用机制

Bioassay-Guided Isolation and Active Compounds Identification of the AntiDiabetic Fractions of Extract and the Predicted Interaction Mechanism.

作者信息

Kadhim Hayder Mohammed, Kadhim Yasir M, Fawzi Hayder Adnan, Abdul Khalik Zaid M, Jawad Ali Mohammed, Ghédira Kamel

机构信息

Pharmacognosy Laboratory, Faculty of Pharmacy, University of Monastir, Avicenna Street, Monastir 5000, Tunisia.

Department of Pharmaceutical Chemistry, College of Pharmacy, Al-Nahrain University, Baghdad 10006, Iraq.

出版信息

Molecules. 2025 May 30;30(11):2394. doi: 10.3390/molecules30112394.

Abstract

is a well-known plant with antioxidant, anti-proliferative, and antimicrobial properties. The plant contains various phenolic compounds, flavonoids, and other bioactive molecules contributing to its medicinal properties. However, little is known about its antidiabetic activity. The study's purpose is the isolation and identification of active compounds of aerial parts in diabetic rats induced by streptozotocin. The ethyl acetate extract (E2) was separated into eight subfractions by column chromatography. The subfractions were evaluated for their antidiabetic activity using diabetic-induced rats. The most active subtraction was purified, and the active compounds were identified using UV spectrophotometry, Fourier Transform Infrared Spectroscopy, Mass spectrophotometry, and HPLC. Subfraction E2-VIII showed the most effective reduction in blood glucose levels, comparable to metformin. In HPLC analysis, subfraction E2-VIII showed three main compounds: nepetin, kaempferide, and Luteolin. The nepetin flavonoid was examined using molecular docking, and it showed a high affinity to α-amylase. In conclusion, the aerial parts of extract and isolated compounds especially nepetin present promising antidiabetic agents this is probably mediated by its strong antioxidants and α-amylase inhibitory effect.

摘要

是一种具有抗氧化、抗增殖和抗菌特性的著名植物。该植物含有多种酚类化合物、黄酮类化合物和其他生物活性分子,这些成分赋予了它药用特性。然而,关于其抗糖尿病活性的了解却很少。该研究的目的是分离和鉴定链脲佐菌素诱导的糖尿病大鼠地上部分的活性化合物。乙酸乙酯提取物(E2)通过柱色谱法分离成八个亚组分。使用糖尿病诱导的大鼠评估这些亚组分的抗糖尿病活性。对活性最高的亚组分进行纯化,并使用紫外分光光度法、傅里叶变换红外光谱法、质谱分析法和高效液相色谱法鉴定活性化合物。亚组分E2-VIII显示出血糖水平降低最为有效,与二甲双胍相当。在高效液相色谱分析中,亚组分E2-VIII显示出三种主要化合物:荆芥内酯、山柰酚素黄酮和木犀草素。使用分子对接对荆芥内酯黄酮进行了检测,结果表明它对α-淀粉酶具有高亲和力。总之,提取物和分离出的化合物,尤其是荆芥内酯,其地上部分呈现出有前景的抗糖尿病药物,这可能是由其强大的抗氧化剂和α-淀粉酶抑制作用介导的。

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