Mechanistic insights into Helicobacter pylori urease inhibition by poplar propolis ethanol extract.
Propolis, a resinous mixture from plant exudates, is widely used in traditional ethnomedicine for gastrointestinal infections, implying anti- Helicobacter pylori (H. pylori) potential. However, its molecular mechanisms targeting H. pylori urease (HPU), a key virulence factor, remain unclear. This st...
| Publicado en: | Journal of Ethnopharmacology Vol. 365 |
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| Autores principales: | , , , , , , , |
| Formato: | research Journal Article |
| Publicado: |
Elsevier B.V.
Jun2026
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| Acceso en línea: | Ver este registro en EBSCOhost |
| fields | @attributes: recordID: 1 pdfLink: plink: https://search.ebscohost.com/login.aspx?direct=true&db=ccm&AN=192840445&site=ehost-live header: @attributes: shortDbName: ccm uiTerm: 192840445 longDbName: CINAHL Complete uiTag: AN controlInfo: bkinfo: dissinfo: jinfo: jid: 03788741 3MS jtl: Journal of Ethnopharmacology issn: 03788741 maglogo: N pubinfo: dt: Jun2026 vid: 365 pid: 1004 pub: Elsevier B.V. artinfo: ui: 192840445 192840445 192840445 10.1016/j.jep.2026.121596 192840445 ppct: 1 formats: tig: atl: Mechanistic insights into Helicobacter pylori urease inhibition by poplar propolis ethanol extract. aug: au: Yuan, Jie Li, Ting Gao, Shuangshuang Tang, Yujing Ma, Shuling Lee, Hai Yen Chin, Kim Ling Xuan, Hongzhuan affil: College of Agriculture and Biology, Liaocheng University, Liaocheng, People's Republic of China sug: subj: Helicobacter Pylori Urease Enzyme Inhibitors Propolis Therapeutic Use Gastrointestinal Diseases Plant Extracts Pharmacodynamics Ethanol Pharmacodynamics Medicine, Herbal Human Kinetics Antibiotics Therapeutic Use Flavonoids Phenols ab: Propolis, a resinous mixture from plant exudates, is widely used in traditional ethnomedicine for gastrointestinal infections, implying anti- Helicobacter pylori (H. pylori) potential. However, its molecular mechanisms targeting H. pylori urease (HPU), a key virulence factor, remain unclear. This study aimed to characterize the inhibitory activity and kinetic properties of poplar propolis ethanol extract (PPEE) against HPU and jack bean urease (JBU), and to elucidate the underlying molecular mechanisms. UPLC–MS/MS-based metabolomics was used to identify PPEE's potential bioactive candidates. Enzyme activity assays, kinetic analysis, thiol/Ni2+ protection assays, transcriptional profiling of urease-related genes, and molecular docking were applied for mechanistic exploration. Bacterial growth curve assays and PI staining verified its antibacterial activity. PPEE, enriched in flavonoids and phenolic acids, exhibited significant dose-dependent and reversible inhibition on HPU, with superior potency to JBU. Mechanistically, PPEE acted synergistically by competitively binding to HPU's substrate pocket, disrupting thiol-Ni2+ coordination, inducing slow-binding conformational stabilization, and perturbing tertiary structure. It also downregulated ureA / ureB , nixA , and ureH / ureI , forming a multi-layered mode of "direct enzyme inhibition + blocking synthesis/assembly". Urease inhibition was the core anti- H. pylori mechanism, with auxiliary urease-independent activity. Molecular docking confirmed stable interactions between PPEE components and HPU's active center/substrate pocket. Experimental validation showed that quercetin and taxifolin inhibited HPU in a dose-dependent manner. PPEE specifically inhibits HPU via multi-targeted synergistic mechanisms, providing molecular evidence for propolis-derived anti- H. pylori agents and laying a foundation for subsequent SAR and in vivo studies. Poplar propolis ethanol extract (PPEE) inhibits Helicobacter pylori (H. pylori) through multi-target urease modulation. PPEE competitively inhibits H. pylori urease (HPU), targets thiol groups for reversible inhibition, disrupts urease tertiary structure, and downregulates urease-related genes, thereby blocking enzyme assembly. These combined effects result in antibacterial activity via both urease-dependent and auxiliary urease-independent mechanisms. [Display omitted] pubtype: Academic Journal doctype: research Journal Article ougenre: Article language: English refInfo: holdings: @attributes: islocal: N |
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