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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Exploring the Antidiabetic Potential of Heterophylliin A From Elaeocarpus grandis
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.
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.
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