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1,3,6-三没食子酰葡萄糖:一种源自Retz.水提取物的新型强效抗黏附剂

1,3,6-Trigalloylglucose: A Novel Potent Anti- Adhesion Agent Derived from Aqueous Extracts of Retz.

作者信息

Ou Ling, Zhu Zhixiang, Hao Yajie, Li Qingwei, Liu Hengrui, Chen Qingchang, Peng Chang, Zhang Chuqiu, Zou Yuanjing, Jia Junwei, Li Hui, Wang Yanhua, Su Bingmei, Lai Yuqian, Chen Meiyun, Chen Haobo, Feng Zhong, Zhang Guimin, Yao Meicun

机构信息

School of Pharmaceutical Sciences (Shenzhen), Sun Yat-sen University, Shenzhen 518107, China.

School of Medicine and Pharmacy (Qingdao), Ocean University of China, Qingdao 266003, China.

出版信息

Molecules. 2024 Mar 5;29(5):1161. doi: 10.3390/molecules29051161.

Abstract

1,3,6-Trigalloylglucose is a natural compound that can be extracted from the aqueous extracts of ripe fruit of Retz, commonly known as "". The potential anti- (HP) activity of this compound has not been extensively studied or confirmed in scientific research. This compound was isolated using a semi-preparative liquid chromatography (LC) system and identified through Ultra-high-performance liquid chromatography-MS/MS (UPLC-MS/MS) and Nuclear Magnetic Resonance (NMR). Its role was evaluated using Minimum inhibitory concentration (MIC) assay and minimum bactericidal concentration (MBC) assay, scanning electron microscope (SEM), inhibiting kinetics curves, urea fast test, Cell Counting Kit-8 (CCK-8) assay, Western blot, and Griess Reagent System. Results showed that this compound effectively inhibits the growth of HP strain ATCC 700392, damages the HP structure, and suppresses the Cytotoxin-associated gene A (Cag A) protein, a crucial factor in HP infection. Importantly, it exhibits selective antimicrobial activity without impacting normal epithelial cells GES-1. In vitro studies have revealed that 1,3,6-Trigalloylglucose acts as an anti-adhesive agent, disrupting the adhesion of HP to host cells, a critical step in HP infection. These findings underscore the potential of 1,3,6-Trigalloylglucose as a targeted therapeutic agent against HP infections.

摘要

1,3,6-三没食子酰葡萄糖是一种天然化合物,可从通常被称为“”的成熟果实的水提取物中提取。该化合物潜在的抗幽门螺杆菌(HP)活性尚未在科学研究中得到广泛研究或证实。使用半制备液相色谱(LC)系统分离该化合物,并通过超高效液相色谱-质谱/质谱(UPLC-MS/MS)和核磁共振(NMR)进行鉴定。使用最低抑菌浓度(MIC)测定、最低杀菌浓度(MBC)测定、扫描电子显微镜(SEM)、抑制动力学曲线、尿素快速试验、细胞计数试剂盒-8(CCK-8)测定、蛋白质免疫印迹和格里斯试剂系统评估其作用。结果表明,该化合物有效抑制HP菌株ATCC 700392的生长,破坏HP结构,并抑制细胞毒素相关基因A(Cag A)蛋白,这是HP感染中的一个关键因素。重要的是,它表现出选择性抗菌活性,而不影响正常上皮细胞GES-1。体外研究表明,1,3,6-三没食子酰葡萄糖作为一种抗黏附剂,破坏HP与宿主细胞的黏附,这是HP感染中的关键步骤。这些发现强调了1,3,6-三没食子酰葡萄糖作为针对HP感染的靶向治疗剂的潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ccab/10935070/2803cfecc672/molecules-29-01161-g001.jpg

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