Exploring the Antidiabetic Potential of Heterophylliin A From Elaeocarpus grandis.

IF 3.6 3区医学 Q2 CHEMISTRY, MEDICINAL

Archiv der Pharmazie Pub Date : 2025-10-01 DOI:10.1002/ardp.70110

Sherif A Maher, Radwa Taher Mohie El-Dien, Muhamad Mustafa, Amgad I M Khedr, Ahmed M Sayed, Usama Ramadan Abdelmohsen, Mostafa A Fouad, Mohamed Salah Kamel

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引用次数: 0

Abstract

The antidiabetic efficacy of Elaeocarpus grandis, belonging to the Family Elaeocarpaceae, was investigated using the streptozotocin-induced hyperglycemia model. The ethyl acetate and petroleum ether fractions demonstrated a notable hypoglycemic impact in a rat model of type 2 diabetes mellitus (T2DM), compared to the negative control group. The chemical assessment of these fractions resulted in the isolation and identification of six known compounds (17-22). LC-HR-ESI-MS metabolomic profiling yielded the provisional identification of sixteen metabolites (1-16) across various chemical classes. In silico investigations, encompassing molecular docking and dynamics simulations, indicated that the compounds heterophylliin A (22), as well as habbemine A (12) and elaeocarpinoside (15), can interact with critical enzymes implicated in glucose metabolism, specifically dipeptidyl peptidase-IV and aldose reductase. Moreover, heterophylliin A (22) markedly decreased the expression of inflammatory markers (IL-1β, TNF-α, IL-6, and TGF-β) in diabetic rats. These findings prompt additional research on E. grandis, specifically its bioactive constituent heterophylliin A, which exhibits intriguing antidiabetic effects and warrants further exploration as a potential treatment agent for T2DM.

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巨腕树异茶碱A抗糖尿病作用的研究。

采用链脲佐菌素诱导的高血糖模型，研究了菖蒲属菖蒲科植物大菖蒲的降糖作用。与阴性对照组相比，乙酸乙酯和石油醚组分在2型糖尿病（T2DM）大鼠模型中表现出显著的降糖作用。这些馏分的化学评估导致分离和鉴定六种已知化合物（17-22）。LC-HR-ESI-MS代谢组学分析初步鉴定了不同化学类别的16种代谢物（1-16）。包括分子对接和动力学模拟在内的计算机研究表明，化合物异茶碱A（22）、哈比明A（12）和elaeocarpinoside（15）可以与葡萄糖代谢中涉及的关键酶相互作用，特别是二肽基肽酶- iv和醛糖还原酶。此外，异茶碱A（22）显著降低糖尿病大鼠炎症标志物（IL-1β、TNF-α、IL-6和TGF-β）的表达。这些发现促使人们进一步研究大叶菊，特别是其生物活性成分异茶碱A，它具有有趣的抗糖尿病作用，值得进一步探索作为T2DM的潜在治疗药物。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Archiv der Pharmazie 医学-化学综合

CiteScore

7.90

自引率

5.90%

发文量

176

审稿时长

3.0 months

期刊介绍： Archiv der Pharmazie - Chemistry in Life Sciences is an international journal devoted to research and development in all fields of pharmaceutical and medicinal chemistry. Emphasis is put on papers combining synthetic organic chemistry, structural biology, molecular modelling, bioorganic chemistry, natural products chemistry, biochemistry or analytical methods with pharmaceutical or medicinal aspects such as biological activity. The focus of this journal is put on original research papers, but other scientifically valuable contributions (e.g. reviews, minireviews, highlights, symposia contributions, discussions, and essays) are also welcome.