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Phytochemicals increase the antibacterial activity of antibiotics by acting on a drug efflux pump.

Ohene-Agyei T, Mowla R, Rahman T, Venter H - Microbiologyopen (2014)

Bottom Line: In silico screening was used to predict the bioactivity of plant compounds and to compare that with the known EPI, phe-arg-β-naphthylamide (PAβN).Subsequently, promising products have been tested for their ability to inhibit efflux.We demonstrated the feasibility of in silico screening to identify compounds that potentiate the action of antibiotics against drug-resistant strains and which might be potentially useful lead compounds for an EPI discovery program.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmacology, University of Cambridge, Tennis Court Road, Cambridge, CB2 1PD, United Kingdom.

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Structures of PAβN and the phytochemicals.
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fig02: Structures of PAβN and the phytochemicals.

Mentions: In silico screening of an in-house database of 50 phytochemicals identified five different compounds that could be docked in the binding pocket of AcrB similar to the known EPI PAβN. These were the naphthoquinones plumbagin from Plumbago indica and shikonin from Lithospermum erythrorhizon; the flavonoid quercetin which is found in many fruits and vegetables; the xanthonoid mangiferin from Mangifera indica (mango), and the antioxidant nordihydroguaretic acid (NDGA) from creosote bush (Fig. 2).


Phytochemicals increase the antibacterial activity of antibiotics by acting on a drug efflux pump.

Ohene-Agyei T, Mowla R, Rahman T, Venter H - Microbiologyopen (2014)

Structures of PAβN and the phytochemicals.
© Copyright Policy - open-access
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4263512&req=5

fig02: Structures of PAβN and the phytochemicals.
Mentions: In silico screening of an in-house database of 50 phytochemicals identified five different compounds that could be docked in the binding pocket of AcrB similar to the known EPI PAβN. These were the naphthoquinones plumbagin from Plumbago indica and shikonin from Lithospermum erythrorhizon; the flavonoid quercetin which is found in many fruits and vegetables; the xanthonoid mangiferin from Mangifera indica (mango), and the antioxidant nordihydroguaretic acid (NDGA) from creosote bush (Fig. 2).

Bottom Line: In silico screening was used to predict the bioactivity of plant compounds and to compare that with the known EPI, phe-arg-β-naphthylamide (PAβN).Subsequently, promising products have been tested for their ability to inhibit efflux.We demonstrated the feasibility of in silico screening to identify compounds that potentiate the action of antibiotics against drug-resistant strains and which might be potentially useful lead compounds for an EPI discovery program.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmacology, University of Cambridge, Tennis Court Road, Cambridge, CB2 1PD, United Kingdom.

Show MeSH
Related in: MedlinePlus