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PreprintCited by 5Bacterial biofilms and quorum sensingEssential Oils and Antimicrobial ActivityBioactive natural compounds

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In vitro activities of isobavachalcone against planktonic and persister cells and biofilm of Enterococcus faecalis

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Ouyang, Lili, Xu, Zhicao, Tang, Yuanyuan, Li, Duoyun, Yu, Zhijian, Wen, Zewen, Zhang, Haigang, Zhang, Chaoqin·2024·BMC Microbiology
DOI 10.21203/rs.3.rs-5317490/v1PMC PMC11869651

Preprint — published as 10.1186/s12866-025-03836-5 · Paper page

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Abstract

Background Mounting evidences have demonstrated the extensive pharmacological activities of the natural product isobavachalcone, including antimicrobial activity, inhibition of reverse transcriptase, antitubercular and antioxidant ability et al. However, the antibacterial and antibiofilm activity and its action mode of isobavachalcone against clinical E. faecalis isolates remain elusive. This study aims to evaluate the in vitro antibacterial and anti-biofilm activities of isobavachalcone on clinical E. faecalis isolates from China and further investigate the possible target site of isobavachalcone in E. faecalis. Results Our data suggested the MICs of isobavachalcone ranging from 6.25 to 12.5 µM against 220 E. faecalis strains. The robust inhibitory effect of isobavachalcone with sub-MIC concentration ( 1/2xMIC ) against the biofilm formation of E. faecalis was found. The rapid bactericidal effect of isobavachalcone against E. faecalis was demonstrated and more planktonic cells could be killed by isobavachalcone compared with vancomycin, linezolid, or ampicillin at 2, 4, 6, and 12h. No synergetic bactericidal activity of isobavachalcone combined with vancomycin, linezolid, or ampicillin was found. Furthermore, genetic mutation of isobavachalcone-resistant E. faecalis was compared with the parental strain by whole genome sequencing, showing that the functions of the mutated proteins were associated with the PurH and FlgJ proteins and other eight proteins involved in the cell wall or cell membrane biogenesis, DNA synthesis, and energy metabolism. Molecular docking analysis showed that FlgJ protein might serve as the potential target of isobavachalcone in E. faecalis. Other mutations are involved in the cell wall or cell membrane biogenesis, DNA synthesis, and energy metabolism. Conclusion This study discovered that isobavachalcone had an antibacterial effect on E. faecalis, and significantly inhibited the biofilm formation of E. faecalis at subinhibitory concentrations. In addition, antibacterial and antibiofilm activity against clinical E. faecalis isolates from China by targeting FlgJ protein.

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Metadata

Authors
Ouyang, L., Xu, Z., Tang, Y., Li, D., Yu, Z., Wen, Z., Zhang, H., & Zhang, C.
Affiliations
  • Shenzhen University (CN)
  • Shenzhen University Medical School
Corresponding author
  • Wen, Zewen
  • Zhang, Haigang
  • Zhang, Chaoqin
ORCID
Venue
BMC Microbiology
Publisher
Springer Science and Business Media LLC
Published
2024-11-06
Volume
25
Issue
1
Pages
105-105
ISSN
1471-2180 (ISSN-L)
DOI
10.21203/rs.3.rs-5317490/v1
PMC
PMC11869651
OpenAlex
W4408033643
Cited by
5
References
1
Citations by year
2026: 3 · 2025: 2
FWCI
1.50
Type
journal article
Language
en
Open access
Licence
Locations
  • BMC Microbiology (publishedVersion, cc-by-nc-nd)
  • Research Square (acceptedVersion, cc-by)
  • PubMed Central (publishedVersion, cc-by-nc-nd)
  • PubMed (publishedVersion)
  • DOAJ (DOAJ: Directory of Open Access Journals) (submittedVersion)
Funders
  • National Natural Science Foundation of China (82172283, 2022A1515110096)
  • Shenzhen University
  • Science, Technology and Innovation Commission of Shenzhen Municipality (JCYJ20220530141614034, JCYJ20220530141810023, JCYJ20220530142006015)
  • Sanming Project of Medicine in Shenzhen (SMGC202305029)
  • Basic and Applied Basic Research Foundation of Guangdong Province (2024A1515013276, 2022A1515110096)
Topics
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Bacterial biofilms and quorum sensing
  • Life Sciences › Agricultural and Biological Sciences › Food Science › Essential Oils and Antimicrobial Activity
  • Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Drug Discovery › Bioactive natural compounds
Keywords
isobavachalcone, Enterococcus faecalis, antibacterial activity, antibiofilm activity, biofilm inhibition, minimum inhibitory concentration, vancomycin resistance, ampicillin resistance, drug resistance mechanisms, molecular docking, clinical isolates, flavonoids
MeSH terms
Anti-Bacterial Agents, Bacterial Proteins, China, Humans, Microbial Sensitivity Tests, Enterococcus faecalis, Vancomycin, Gram-Positive Bacterial Infections, Biofilms, Chalcones, Molecular Docking Simulation

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