Conjugating berberine to a multidrug efflux pump inhibitor creates an effective antimicrobial.

Conjugating berberine to a multidrug efflux pump inhibitor creates an effective antimicrobial. Research Abstract Details 

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Conjugating berberine to a multidrug efflux pump inhibitor creates an effective antimicrobial. Abstract Text:

Anthony R Ball,Gabriele Casadei,Siritron Samosorn,John B Bremner,Frederick M Ausubel,Terence I Moy,Kim Lewis,

In bacteria, multidrug-resistance pumps (MDRs) confer resistance to chemically unrelated amphipathic toxins. A major challenge in developing efficacious antibiotics is identifying antimicrobial compounds that are not rapidly pumped out of bacterial cells. The plant antimicrobial berberine, the active component of the medicinal plants echinacea and golden seal, is a cation that is readily extruded by bacterial MDRs, thereby rendering it relatively ineffective as a therapeutic agent. However, inhibition of MDR efflux causes a substantial increase in berberine antimicrobial activity, suggesting that berberine and potentially many other compounds could be more efficacious if an effective MDR pump inhibitor could be identified. Here we show that covalently linking berberine to INF 55 , an inhibitor of Major Facilitator MDRs, results in a highly effective antimicrobial that readily accumulates in bacteria. The hybrid molecule showed good efficacy in a Caenorhabditis elegans model of enterococcal infection, curing worms of the pathogen.

Conjugating berberine to a multidrug efflux pump inhibitor creates an effective antimicrobial. Publishing Authors By Initials

AR Ball,G Casadei,S Samosorn,JB Bremner,FM Ausubel,TI Moy,K Lewis,

For similar bacteria: gram-positive bacteria: gram-positive cocci: staphylococcaceae: staphylococcus: staphylococcus aureus research abstracts see: bacteria: gram-positive bacteria: gram-positive cocci: staphylococcaceae: staphylococcus: staphylococcus aureus research

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Conjugating berberine to a multidrug efflux pump inhibitor creates an effective antimicrobial. Journal Published:

PUBLICATION TYPE: Research Support, Non-U.S. Gov

Journal: ACS chemical biology

VOLUME: 1

Page Numbers: 594-600

Journal Abbreviation: ACS Chem. Biol.

ISSN: 1554-8937

DAY: 24

MONTH: Oct

YEAR: 2006

Conjugating berberine to a multidrug efflux pump inhibitor creates an effective antimicrobial. Information

Number of References:

LANGUAGE: eng

NlmUniqueID: 101282906

Conjugating berberine to a multidrug efflux pump inhibitor creates an effective antimicrobial. Keywords Mesh Terms:

KEYWORDS: Staphylococcus aureus

MESH TERMS: metabolism

Chemical & Substance for Abstract: Conjugating berberine to a multidrug efflux pump inhibitor creates an effective antimicrobial. Information

Substance Name: Berberine

Registry Number: 2086-83-1

Grant and Affiliation Information for Conjugating berberine to a multidrug efflux pump inhibitor creates an effective antimicrobial.

AFFILIATION: Department of Biology and Antimicrobial Discovery Center, Northeastern University, Boston, Massachusetts 02115, USA.

Country: United States

AGENCY: United States NIAID

GRANT: AI059483-01

ACRONYM: AI

MEDLINETA: ACS Chem Biol

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