Chen Pengting, Chen Meiyun, Peng Chang, Yan Jiahui, Shen Xue, Zhang Weijia, Yuan Yuemei, Gan Guoxing, Luo Xiaojun, Zhu Weixing, Yao Meicun
School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China.
School of Pharmaceutical Sciences (Shenzhen), Sun Yat-sen University, Shenzhen 518107, China.
J Ethnopharmacol. 2024 Jan 10;318(Pt B):116981. doi: 10.1016/j.jep.2023.116981. Epub 2023 Aug 11.
Sanguisorba officinalis L. (S. officinalis L.), known as Di Yu (DY) in Traditional Chinese Medicine (TCM), are used to treat burns, vomiting of blood, asthma, intestinal infections, and dermatitis. It has been reported that the root of DY has a significant inhibitory effect on Helicobacter pylori (H. pylori). However, there is currently little research on the composition analysis and anti-H. pylori infection properties of the non-medicinal parts of DY, such as its stems, leaves, and flowers.
The commonly used eradication therapies for H. pylori infection are antibiotic-based therapies. With the increasing antibiotic resistance of H. pylori, it is urgent to find effective alternative therapies. To find alternative therapies and increase the utilization of DY, this study aims to investigate the phytochemistry profile, in vitro anti-H. pylori activity, and preliminary antibacterial mechanism of the non-medicinal parts of DY.
The non-medicinal parts of DY extracts were obtained by using hot water reflux method. The chemical composition of these extracts was analyzed using colorimetric method, high-performance liquid chromatography (HPLC), and ultra-high-performance liquid chromatography-electrospray ionization-mass spectrometry (UPLC-ESI-MS). The in vitro anti-H. pylori activity was investigated using broth microdilution method, checkerboard dilution method, time-kill curve, time-inhibition curve, scanning electron microscopy, and transmission electron microscopy. Transcriptional sequencing technology was used to study the effect of DY stems and flowers on the gene expression of H. pylori and explore possible antibacterial mechanisms.
The non-medicinal parts of DY contain abundant phytochemicals, such as total phenols and total flavonoids, and possess strong inhibitory and bactericidal activity against both standard and clinical strains of H. pylori in vitro. The MIC was 80-1280 μg/mL and the MBC was 80-2560 μg/mL, and the strength of the antibacterial effects was dependent on the concentration of phytochemicals (total polyphenols, gallic acid and ellagic acid). In addition, the combination of non-medicinal parts of DY with antibiotics, such as amoxicillin, metronidazole, levofloxacin, and clarithromycin, did not result in any antagonistic effects. All of them could disrupt the morphology, internal microscopic and cell wall structures of H. pylori thereby acting as an inhibitor. The mechanism of action was found to be the disruption of H. pylori morphology, internal microstructure, and cell wall. Transcriptomic analysis showed that the non-medicinal parts of DY significantly regulated the gene expression of H. pylori, especially the metabolic pathway.
This study analyzed the chemical composition of the non-medicinal parts of DY and confirmed its inhibitory and bactericidal activities against H. pylori, both standard and clinical strains. Additional, the mechanism of inhibition involves disrupting the structure of H. pylori cells, altering gene expression, and interfering with bacterial metabolic pathways. This study provides a reference for further resource utilization and the development of H. pylori drugs using the non-medicinal parts of DY.
地榆在传统中医中被称为“地榆”,可用于治疗烧伤、吐血、哮喘、肠道感染和皮炎。据报道,地榆根对幽门螺杆菌有显著抑制作用。然而,目前关于地榆非药用部位(如茎、叶和花)的成分分析及抗幽门螺杆菌感染特性的研究较少。
幽门螺杆菌感染常用的根除疗法是以抗生素为基础的治疗方法。随着幽门螺杆菌抗生素耐药性的增加,迫切需要寻找有效的替代疗法。为了寻找替代疗法并提高地榆的利用率,本研究旨在研究地榆非药用部位的植物化学特征、体外抗幽门螺杆菌活性及初步抗菌机制。
采用热水回流法获得地榆非药用部位提取物。利用比色法、高效液相色谱法(HPLC)和超高效液相色谱-电喷雾电离-质谱法(UPLC-ESI-MS)分析这些提取物的化学成分。采用肉汤微量稀释法、棋盘稀释法、时间-杀菌曲线、时间-抑制曲线、扫描电子显微镜和透射电子显微镜研究体外抗幽门螺杆菌活性。利用转录测序技术研究地榆茎和花对幽门螺杆菌基因表达的影响并探索可能的抗菌机制。
地榆非药用部位含有丰富的植物化学物质,如总酚和总黄酮,对幽门螺杆菌标准菌株和临床菌株均具有较强的体外抑制和杀菌活性。最低抑菌浓度(MIC)为80 - 1280μg/mL,最低杀菌浓度(MBC)为80 - 2560μg/mL,抗菌效果强度取决于植物化学物质(总多酚、没食子酸和鞣花酸)的浓度。此外,地榆非药用部位与阿莫西林、甲硝唑、左氧氟沙星和克拉霉素等抗生素联合使用未产生任何拮抗作用。它们均可破坏幽门螺杆菌的形态、内部微观结构和细胞壁结构,从而起到抑菌作用。作用机制为破坏幽门螺杆菌的形态、内部微观结构和细胞壁。转录组分析表明,地榆非药用部位显著调节幽门螺杆菌的基因表达,尤其是代谢途径。
本研究分析了地榆非药用部位的化学成分,证实其对幽门螺杆菌标准菌株和临床菌株均具有抑制和杀菌活性。此外,抑制机制包括破坏幽门螺杆菌细胞结构、改变基因表达和干扰细菌代谢途径。本研究为进一步利用地榆非药用部位开发幽门螺杆菌药物提供了参考。