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探索锯齿假杜鹃的降血糖潜力:分离、结构解析及α-葡萄糖苷酶抑制活性评价

Exploring anti-hyperglycemic potential of Pseuderanthemum crenulatum: isolation, structural elucidation and α-glucosidase inhibition evaluation.

作者信息

Ngo Dung V, Nguyen Le-Thu T, Ngo Ngoc T N, Nguyen Lien-Hoa D, Trinh Binh T D

机构信息

Faculty of Chemistry, VNUHCM-University of Science, 227 Nguyen Van Cu Street, District 5, Ho Chi Minh City, 700000, Vietnam.

Vietnam National University Ho Chi Minh City, Linh Trung Ward, Thu Duc City, Ho Chi Minh City, 700000, Vietnam.

出版信息

J Nat Med. 2025 Apr 23. doi: 10.1007/s11418-025-01907-5.

Abstract

Pseuderanthemum crenulatum (Acanthaceae) is a medicinal plant traditionally used to manage diabetes. However, its chemical constituents remain unexplored as no studies have been conducted on this species to date. This study aimed to chemically characterize and evaluate the anti-hyperglycemic activity of compounds isolated from the stems and roots of P. crenulatum. The isolation process involved utilizing column chromatography techniques, while structures were characterized mainly by 1D and 2D NMR experiments. Anti-hyperglycemic activity was evaluated by measuring their inhibitory effects on the α-glucosidase enzyme. Following this, a new abietane-type dinorditerpenoid, namely pseuderanthemone (1), along with ten known compounds (2-11), was isolated from an ethyl acetate extract of the stems and roots of P. crenulatum. The investigation into their anti-hyperglycemic effects revealed that compounds 1-3, and 6-10 showed higher α-glucosidase inhibitory activity than positive control, acarbose. Among them, compound 9 demonstrated the most potent activity, with an IC value nearly ten times lower than acarbose. Furthermore, kinetic analysis showed that compound 2 displayed mixed-type inhibition, and compound 3 demonstrated uncompetitive inhibition while the remaining compounds exhibited competitive inhibition.

摘要

锯齿假杜鹃(爵床科)是一种传统上用于治疗糖尿病的药用植物。然而,由于迄今为止尚未对该物种进行过研究,其化学成分仍未被探索。本研究旨在对从锯齿假杜鹃茎和根中分离出的化合物进行化学表征,并评估其降血糖活性。分离过程采用柱色谱技术,结构主要通过一维和二维核磁共振实验进行表征。通过测量它们对α-葡萄糖苷酶的抑制作用来评估降血糖活性。在此之后,从锯齿假杜鹃茎和根的乙酸乙酯提取物中分离出一种新的枞酸型二降二萜,即锯齿假杜鹃酮(1),以及十种已知化合物(2-11)。对它们降血糖作用的研究表明,化合物1-3和6-10表现出比阳性对照阿卡波糖更高的α-葡萄糖苷酶抑制活性。其中,化合物9表现出最有效的活性,其IC值比阿卡波糖低近十倍。此外,动力学分析表明,化合物2表现出混合型抑制,化合物3表现出非竞争性抑制,而其余化合物表现出竞争性抑制。

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