Antibacterial and Antibiofilm Activities of Makaluvamine Analogs

Microorganisms
Bhavitavya NijampatnamSadanandan E Velu

Abstract

Streptococcus mutans is a key etiological agent in the formation of dental caries. The major virulence factor is its ability to form biofilms. Inhibition of S. mutans biofilms offers therapeutic prospects for the treatment and the prevention of dental caries. In this study, 14 analogs of makaluvamine, a marine alkaloid, were evaluated for their antibacterial activity against S. mutans and for their ability to inhibit S. mutans biofilm formation. All analogs contained the tricyclic pyrroloiminoquinone core of makaluvamines. The structural variations of the analogs are on the amino substituents at the 7-position of the ring and the inclusion of a tosyl group on the pyrrole ring N of the makaluvamine core. The makaluvamine analogs displayed biofilm inhibition with IC50 values ranging from 0.4 μM to 88 μM. Further, the observed bactericidal activity of the majority of the analogs was found to be consistent with the anti-biofilm activity, leading to the conclusion that the anti-biofilm activity of these analogs stems from their ability to kill S. mutans. However, three of the most potent N-tosyl analogs showed biofilm IC50 values at least an order of magnitude lower than that of bactericidal activity, indicating that the biofilm act...Continue Reading

References

Jan 1, 1988·Microbiology and Immunology·T OoshimaS Hamada
Jun 1, 1971·Kōkūbyō Gakkai zasshi. The Journal of the Stomatological Society, Japan·M Onisi
Dec 1, 1995·Journal of Natural Products·E W SchmidtD J Faulkner
Apr 1, 1997·Advances in Dental Research·G H Bowden, Y H Li
Jul 8, 1999·International Journal of Antimicrobial Agents·J W Costerton
Apr 27, 2000·Journal of Bacteriology·P Watnick, R Kolter
Feb 15, 2002·Advances in Dental Research·M Lenander-Lumikari, V Loimaranta
Mar 2, 2002·Applied and Environmental Microbiology·Zezhang T Wen, Robert A Burne
Oct 25, 2002·Proceedings of the National Academy of Sciences of the United States of America·Dragana AjdićJoseph J Ferretti
Feb 4, 2003·Nature Reviews. Drug Discovery·David Davies
Mar 17, 2004·FEMS Microbiology Letters·Ramona RozenGilad Bachrach
May 22, 2004·Caries Research·P D Marsh
Jul 13, 2005·Community Dentistry and Oral Epidemiology·David Beighton
Jan 9, 2007·Lancet·Robert H SelwitzNigel B Pitts
Mar 21, 2007·Bioorganic & Medicinal Chemistry Letters·Bidhan A ShinkreSadanandan E Velu
Nov 27, 2007·American Journal of Kidney Diseases : the Official Journal of the National Kidney Foundation·Elizabeth SelvinJosef Coresh
Dec 21, 2007·Bioorganic & Medicinal Chemistry·Bidhan A ShinkreSadanandan E Velu
Oct 16, 2009·Journal of Dental Research·K HojoN Maeda
Jul 27, 2012·Current Medicinal Chemistry·J-J QinR Zhang
Jan 10, 2014·International Dental Journal·David J Bradshaw, Richard J M Lynch

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Citations

Apr 15, 2014·International Journal of Systematic and Evolutionary Microbiology·Tomáš PánekIvan Čepička
Jul 3, 2016·Bioorganic & Medicinal Chemistry Letters·Bhavitavya NijampatnamSadanandan E Velu

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Methods Mentioned

BETA
column chromatography
nuclear magnetic resonance

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