Evidence map›Paper›PMID 24824618›Full record

ArticlePloS one2014

Rational design of berberine-based FtsZ inhibitors with broad-spectrum antibacterial activity.

Ning Sun, Fung-Yi Chan, Yu-Jing Lu, Marco A C Neves, Hok-Kiu Lui, Yong Wang, Ka-Yan Chow, Kin-Fai Chan, Siu-Cheong Yan, Yun-Chung Leung and 3 more

Open access · goldAbstract read
In one paragraph

Article in PloS one, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 55 papers.

0numbers the graph read from it
0cells of the map it votes in
55citing papers in PubMed
8.1field-weighted citation impact, top 2% of its field
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

55 citing papers in PubMed, 127 citations in OpenAlex.

  1. Article
  2. Article
  3. Review
  4. Review
  5. Article
  6. Article
  7. Article
  8. Review
  9. Berberine-styrene-RSC advances · 2024
    Article
  10. Article
  11. Article
  12. Article
  13. Review
  14. Article
  15. Review
  16. A Review ofMolecules (Basel, Switzerland) · 2023
    Review
  17. Synthesis and biological evaluation ofBeilstein journal of organic chemistry · 2023
    Article
  18. Article
  19. Review
  20. Review
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

13 authors at 3 institutions in 3 countries.

Ning SunDepartment of Applied Biology and Chemical Technology and the State Key Laboratory of Chirosciences, The Hong Kong Polytechnic University, Kowloon, Hong Kong, China.
Fung-Yi ChanDepartment of Applied Biology and Chemical Technology and the State Key Laboratory of Chirosciences, The Hong Kong Polytechnic University, Kowloon, Hong Kong, China; Skaggs School of Pharmacy & Pharmaceutical Sciences, University of California San Diego, La Jolla, California, United States of America.
Yu-Jing LuDepartment of Applied Biology and Chemical Technology and the State Key Laboratory of Chirosciences, The Hong Kong Polytechnic University, Kowloon, Hong Kong, China; School of Chemical Engineering and Light Industry, Guangdong University of Technology, Guangzhou, China.
Marco A C NevesSkaggs School of Pharmacy & Pharmaceutical Sciences, University of California San Diego, La Jolla, California, United States of America.
Hok-Kiu LuiDepartment of Applied Biology and Chemical Technology and the State Key Laboratory of Chirosciences, The Hong Kong Polytechnic University, Kowloon, Hong Kong, China.
Yong WangDepartment of Applied Biology and Chemical Technology and the State Key Laboratory of Chirosciences, The Hong Kong Polytechnic University, Kowloon, Hong Kong, China.
Ka-Yan ChowDepartment of Applied Biology and Chemical Technology and the State Key Laboratory of Chirosciences, The Hong Kong Polytechnic University, Kowloon, Hong Kong, China.
Kin-Fai ChanDepartment of Applied Biology and Chemical Technology and the State Key Laboratory of Chirosciences, The Hong Kong Polytechnic University, Kowloon, Hong Kong, China.
Siu-Cheong YanDepartment of Applied Biology and Chemical Technology and the State Key Laboratory of Chirosciences, The Hong Kong Polytechnic University, Kowloon, Hong Kong, China.
Yun-Chung LeungDepartment of Applied Biology and Chemical Technology and the State Key Laboratory of Chirosciences, The Hong Kong Polytechnic University, Kowloon, Hong Kong, China.
Ruben AbagyanSkaggs School of Pharmacy & Pharmaceutical Sciences, University of California San Diego, La Jolla, California, United States of America; Molsoft L.L.C, San Diego, California, United States of America.
Tak-Hang ChanDepartment of Applied Biology and Chemical Technology and the State Key Laboratory of Chirosciences, The Hong Kong Polytechnic University, Kowloon, Hong Kong, China.
Kwok-Yin WongDepartment of Applied Biology and Chemical Technology and the State Key Laboratory of Chirosciences, The Hong Kong Polytechnic University, Kowloon, Hong Kong, China.
Hong Kong Polytechnic University · HKUniversity of California, San Diego · USUniversity of Montana · US

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Inhibition of the functional activity of Filamenting temperature-sensitive mutant Z (FtsZ) protein, an essential and highly conserved bacterial cytokinesis protein, is a promising approach for the development of a new class of antibacterial agents. Berberine, a benzylisoquinoline alkaloid widely used in traditional Chinese and native American medicines for its antimicrobial properties, has been recently reported to inhibit FtsZ. Using a combination of in silico structure-based design and in vitro biological assays, 9-phenoxyalkyl berberine derivatives were identified as potent FtsZ inhibitors. Compared to the parent compound berberine, the derivatives showed a significant enhancement of antibacterial activity against clinically relevant bacteria, and an improved potency against the GTPase activity and polymerization of FtsZ. The most potent compound 2 strongly inhibited the proliferation of Gram-positive bacteria, including methicillin-resistant S. aureus and vancomycin-resistant E. faecium, with MIC values between 2 and 4 µg/mL, and was active against the Gram-negative E. coli and K. pneumoniae, with MIC values of 32 and 64 µg/mL respectively. The compound perturbed the formation of cytokinetic Z-ring in E. coli. Also, the compound interfered with in vitro polymerization of S. aureus FtsZ. Taken together, the chemical modification of berberine with 9-phenoxyalkyl substituent groups greatly improved the antibacterial activity via targeting FtsZ.

Indexed as

Models, MolecularAnti-Bacterial AgentsBacterial ProteinsBerberineCytoskeletal ProteinsEscherichia coliGram-Positive BacteriaMicrobial Sensitivity TestsMicroscopy, Electron, TransmissionMolecular StructureProtein ConformationAnti-Bacterial AgentsBacterial ProteinsBerberineCytoskeletal ProteinsFtsZ protein, Bacteria

Identifiers

PMID24824618
PMCPMC4019636
OpenAlexW2090218289

What OpenQuestion holds

Textmetadata
LicenceCC BY
Read underepoch 390

Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.