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利用液相色谱-四极杆飞行时间质谱法从皮埃尔叶中发现天然磷酸二酯酶5抑制剂

Discovery of Natural Phosphodiesterase 5 Inhibitors from Pierre Leaves Using LC-QTOF-MS.

作者信息

Chantakul Ruttanaporn, Girard Corine, Senejoux François, Ingkaninan Kornkanok, Nuengchamnong Nitra, Temkitthawon Prapapan

机构信息

Center of Excellence for Natural Health Product Innovation and Center of Excellence for Innovation in Chemistry, Faculty of Pharmaceutical Sciences, Naresuan University, Phitsanulok 65000, Thailand.

Université Marie et Louis Pasteur, EFS, INSERM, UMR RIGHT, F-25000 Besançon, France.

出版信息

Plants (Basel). 2025 May 29;14(11):1652. doi: 10.3390/plants14111652.

Abstract

The imbalance of phosphodiesterase 5 (PDE5) enzyme in the male body, or excessive PDE5 enzyme levels, can occur due to factors such as aging, diseases (e.g., cardiovascular disease, diabetes, depressive disorder), and physical behaviors (e.g., alcoholism, smoking, stress). PDE5 is directly associated with erectile dysfunction disease. Currently, many studies aim to find natural PDE5 inhibitors as an alternative to commercial drugs. This study is the first to demonstrate that the ethanolic leaf extract of exhibits potent PDE5-inhibitory activity. The PDE5-inhibitory activity of five plant parts was evaluated: leaf (IC = 1.53 ± 0.12 µg/mL), twig (3.37 ± 0.54), fruit (14.92 ± 2.85), heartwood (19.05 ± 5.60), and bark (16.03 ± 2.92). However, there is still uncertainty about which compounds in leaf extract are responsible for the PDE5 inhibition. Therefore, the purpose of this study is to identify the chemical constituents in the leaf of , including determining which of these compounds may act as PDE5 inhibitors. This study was achieved using at-line LC-QTOF-MS.

摘要

男性体内磷酸二酯酶5(PDE5)失衡或PDE5酶水平过高,可能是由衰老、疾病(如心血管疾病、糖尿病、抑郁症)和身体行为(如酗酒、吸烟、压力)等因素引起的。PDE5与勃起功能障碍疾病直接相关。目前,许多研究旨在寻找天然的PDE5抑制剂作为商业药物的替代品。本研究首次证明了[植物名称]的乙醇叶提取物具有强大的PDE5抑制活性。评估了该植物五个部位的PDE5抑制活性:叶(IC = 1.53 ± 0.12 µg/mL)、嫩枝(3.37 ± 0.54)、果实(14.92 ± 2.85)、心材(19.05 ± 5.60)和树皮(16.03 ± 2.92)。然而,叶提取物中哪些化合物负责PDE5抑制作用仍不确定。因此,本研究的目的是鉴定[植物名称]叶中的化学成分,包括确定这些化合物中哪些可能作为PDE5抑制剂。本研究使用在线LC-QTOF-MS完成。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/99a0/12157991/3b0fe91dceba/plants-14-01652-g001.jpg

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