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

IF 2.5 4区 医学 Q3 CHEMISTRY, MEDICINAL
Dung V Ngo, Le-Thu T Nguyen, Ngoc T N Ngo, Lien-Hoa D Nguyen, Binh T D Trinh
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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 IC50 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.

探讨假菊的降糖潜能:分离、结构鉴定及α-葡萄糖苷酶抑制作用评价。
假菊(棘科)是一种传统上用于治疗糖尿病的药用植物。然而,其化学成分仍未被探索,因为迄今为止还没有对该物种进行过研究。本研究旨在化学表征和评价从crenulatum茎和根中分离的化合物的抗高血糖活性。分离过程涉及柱层析技术,而结构主要通过一维和二维核磁共振实验表征。通过测定其对α-葡萄糖苷酶的抑制作用来评价其抗高血糖活性。在此基础上,从crenulatum茎和根的乙酸乙酯萃取物中分离出一种新的二萜类化合物pseudoeranthemone(1)和10个已知化合物(2-11)。对其抗高血糖作用的研究表明,化合物1 ~ 3和6 ~ 10比阳性对照阿卡波糖具有更高的α-葡萄糖苷酶抑制活性。其中化合物9的活性最强,IC50值比阿卡波糖低近10倍。此外,动力学分析表明,化合物2表现为混合型抑制,化合物3表现为非竞争性抑制,其余化合物表现为竞争性抑制。
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来源期刊
CiteScore
6.90
自引率
3.00%
发文量
79
审稿时长
1.7 months
期刊介绍: The Journal of Natural Medicines is an international journal publishing original research in naturally occurring medicines and their related foods and cosmetics. It covers: -chemistry of natural products -biochemistry of medicinal plants -pharmacology of natural products and herbs, including Kampo formulas and traditional herbs -botanical anatomy -cultivation of medicinal plants. The journal accepts Original Papers, Notes, Rapid Communications and Natural Resource Letters. Reviews and Mini-Reviews are generally invited.
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