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Antimicrobial Agents and Chemotherapy, May 2002, p. 1302-1309, Vol. 46, No. 5
0066-4804/02/$04.00+0     DOI: 10.1128/AAC.46.5.1302-1309.2002
Copyright © 2002, American Society for Microbiology. All Rights Reserved.

Effects of Compounds Found in Propolis on Streptococcus mutans Growth and on Glucosyltransferase Activity

Hyun Koo,1* Pedro L. Rosalen,2 Jaime A. Cury,2 Yong K. Park,3 and William H. Bowen1

Center for Oral Biology and Eastman Department of Dentistry, University of Rochester Medical Center, Rochester, New York,1 Department of Physiological Sciences, Faculty of Dentistry of Piracicaba,2 Department of Food Science, College of Food Engineering, State University of Campinas, Sao Paulo, Brazil3

Received 11 June 2001/ Returned for modification 30 October 2001/ Accepted 28 January 2002

Propolis, a resinous bee product, has been shown to inhibit the growth of oral microorganisms and the activity of bacterium-derived glucosyltransferases (GTFs). Several compounds, mainly polyphenolics, have been identified in this natural product. The present study evaluated the effects of distinct chemical groups found in propolis on the activity of GTF enzymes in solution and on the surface of saliva-coated hydroxyapatite (sHA) beads. Thirty compounds, including flavonoids, cinnamic acid derivatives, and terpenoids, were tested for the ability to inhibit GTFs B, C, and D from Streptococcus mutans and GTF from S. sanguinis (GTF Ss). Flavones and flavonols were potent inhibitors of GTF activity in solution; lesser effects were noted on insolubilized enzymes. Apigenin, a 4',5,7-trihydroxyflavone, was the most effective inhibitor of GTFs, both in solution (90.5 to 95% inhibition at a concentration of 135 µg/ml) and on the surface of sHA beads (30 to 60% at 135 µg/ml). Antibacterial activity was determined by using MICs, minimum bactericidal concentrations (MBCs), and time-kill studies. Flavanones and some dihydroflavonols, as well as the sesquiterpene tt-farnesol, inhibited the growth of S. mutans and S. sobrinus; tt-farnesol was the most effective antibacterial compound (MICs of 14 to 28 µg/ml and MBCs of 56 to 112 µg/ml). tt-Farnesol (56 to 112 µg/ml) produced a 3-log-fold reduction in the bacterial population after 4 h of incubation. Cinnamic acid derivatives had negligible biological activities. Several of the compounds identified in propolis inhibit GTF activities and bacterial growth. Apigenin is a novel and potent inhibitor of GTF activity, and tt-farnesol was found to be an effective antibacterial agent.

* Corresponding author. Mailing address: University of Rochester Medical Center, Center for Oral Biology, 601 Elmwood Ave., Box 611, Rochester, NY 14642. Phone: (716) 275-1433. Fax: (716) 473-2679. E-mail: Hyun_Koo{at}urmc.rochester.edu.

Antimicrobial Agents and Chemotherapy, May 2002, p. 1302-1309, Vol. 46, No. 5
0066-4804/02/$04.00+0     DOI: 10.1128/AAC.46.5.1302-1309.2002
Copyright © 2002, American Society for Microbiology. All Rights Reserved.



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