关键词: Advanced glycation end products Alpha-amylase Alpha-glucosidase Dendrobium polyanthum Wall. ex Lindl. Kinetic study Molecular docking analysis

来  源:   DOI:10.1016/j.heliyon.2024.e34502   PDF(Pubmed)

Abstract:
Eight compounds, including one anthraquinone, two bibenzyls, one phenanthrene, three dihydrophenanthrenes, and one flavonoid, were isolated from the roots of Dendrobium polyanthum Wall. ex Lindl. Among these, six compounds were investigated for inhibitory activities against alpha-glucosidase, alpha-amylase, and advanced glycation end products (AGEs) production. Additionally, molecular docking was conducted to analyze the interactions of the test compounds with alpha-glucosidase. Moscatin, the only isolated phenanthrene, displayed the strongest anti-alpha-glucosidase activity with an IC50 of 32.45 ± 1.04 μM, approximately 10-fold smaller than that of acarbose. Furthermore, moscatilin most strongly inhibited alpha-amylase and AGEs production with IC50 values of 256.94 ± 9.87 and 67.89 ± 9.42 μM, respectively. Molecular docking analysis revealed the effective binding of all substances to alpha-glucosidase with smaller lowest binding energy values than acarbose. Moscatin was selected for kinetics studies, and it was identified as a non-competitive inhibitor with approximately 9-fold greater inhibitory capability than acarbose. This study represents the first report on the phytochemical constituents and antidiabetic potential of compounds derived from the roots of D. polyanthum Wall. ex Lindl.
摘要:
八个化合物,包括一个蒽醌,两个双苄基,一个菲,三个二氢菲,和一种类黄酮,从多花石斛壁的根中分离出来。前Lindl.其中,研究了六个化合物对α-葡萄糖苷酶的抑制活性,α-淀粉酶,和糖基化终产物(AGEs)的生产。此外,进行分子对接以分析测试化合物与α-葡萄糖苷酶的相互作用。摩司他汀,唯一分离的菲,显示最强的抗α-葡萄糖苷酶活性,IC50为32.45±1.04μM,大约比阿卡波糖小10倍。此外,moscatilin最强烈地抑制α-淀粉酶和AGEs的产生,IC50值为256.94±9.87和67.89±9.42μM,分别。分子对接分析显示所有物质与α-葡萄糖苷酶的有效结合具有比阿卡波糖更小的最低结合能值。选择莫司他进行动力学研究,它被鉴定为非竞争性抑制剂,其抑制能力比阿卡波糖高约9倍。这项研究代表了有关源自D.polyanthumWall根的化合物的植物化学成分和抗糖尿病潜力的第一份报告。前Lindl.
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