作为抗糖尿病并发症药物线索的去甲氧基化姜黄素--硅学研究

O. S. Ajala, Dolapo Omolade INNOCENT-UGWU, Peace Udodiri Okechukwu, Olayinka Hannah Dada
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引用次数: 0

摘要

姜黄在传统上被用于治疗糖尿病和糖尿病并发症。抑制醛糖还原酶(ALR2)是治疗糖尿病并发症的一种可行策略。这项工作旨在对莪术植物化学物质的 ALR2 抑制潜力进行硅学评估。研究人员对 39 种莪术植物成分进行了一系列硅学筛选,包括分子对接、药物相似性和安全性分析,以确定 ALR2 抑制剂的先导物,并在 50 ns 模拟时间内通过分子动力学模拟验证其结合相互作用。硅学评估发现了两种去甲氧基姜黄素,即双去甲氧基姜黄素和去甲氧基姜黄素,它们是潜在的 ALR2 抑制剂,能形成稳定的 ALR2 复合物,其相对效力与去甲氧基程度相关。在此推荐将这两种姜黄素作为发现 ALR2 抑制性抗糖尿病并发症药物的线索。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
DEMETHOXYLATED CURCUMINOIDS AS ANTIDIABETIC COMPLICATION DRUG LEADS – IN SILICO STUDIES
Curcuma longa is used traditionally in the treatment of diabetes and diabetic complications. Aldose Reductase (ALR2) inhibition is a plausible therapeutic strategy against diabetic complications. This work was aimed at evaluating Curcuma longa phytochemicals, in silico, for their ALR2 inhibitory potentials. Thirty-nine (39) phytoconstituents of Curcuma longa were subjected to a succession of in silico screenings comprising molecular docking, drug-likeness and safety profiling to identify ALR2 inhibitor leads, validating their binding interactions with molecular dynamics simulations at 50 ns simulation time. The in silico evaluations afforded two demethoxylated curcuminoids, bisdemethoxycurcumin and demethoxycurcumin, as potential ALR2 inhibitor leads forming stable ALR2 complexes, their relative potencies correlating to their degrees of demethoxylation. The two curcuminoids are herein recommended as leads for the discovery of ALR2 inhibitory antidiabetic complication drug leads.
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