Skip to main content
NCBI home page
Antimicrobial Agents and Chemotherapy logoLink to Antimicrobial Agents and Chemotherapy
. 1977 Dec;12(6):721–729. doi: 10.1128/aac.12.6.721

Structural Requirements of Guanide, Biguanide, and Bisbiguanide Agents for Antiplaque Activity

J M Tanzer 1, A M Slee 1, B A Kamay 1
PMCID: PMC430011  PMID: 931371

Abstract

The bactericidal efficacy of 16 guanide, biguanide, and bisbiguanide agents was studied in vitro against intact preformed plaques of four oral (plaque-forming) microorganisms: Streptococcus mutans, S. sanguis, Actinomyces viscosus, and A. naeslundii. The activities of these agents were examined in relation to their molecular configurations. These studies indicated that the bis- and biguanide configurations are important for efficacy, as is the length of the alkyl side chain. No structural moiety determined efficacy by itself. Furthermore, the activities of these agents were studied to determine the minimal conditions (concentration, duration, and frequency) of treatment required for likely clinical efficacy. At least six agents were judged to have equal or greater efficacy than the reference agent, chlorhexidine digluconate. A plaque bactericidal index was derived for the most potent agents, and comparison to the bactericidal properties of chlorhexidine was expressed as a chlorhexidine coefficient.

Full text

PDF
721

Selected References

These references are in PubMed. This may not be the complete list of references from this article.

  1. Bowden G. H., Hardie J. M. Commensal and pathogenic Actinomyces species in man. Soc Appl Bacteriol Symp Ser. 1973 Jan;2:277–299. [PubMed] [Google Scholar]
  2. Carlsson J. Presence of various types of non-haemolytic streptococci in dental plaque and in other sites of the oral cavity in man. Odontol Revy. 1967;18(1):55–74. [PubMed] [Google Scholar]
  3. Davies A. The mode of action of chlorhexidine. J Periodontal Res Suppl. 1973;12:68–75. doi: 10.1111/j.1600-0765.1973.tb02167.x. [DOI] [PubMed] [Google Scholar]
  4. De Stoppelaar J. D., Van Houte J., Backer Dirks O. The relationship between extracellular polysaccharide-producing streptococci and smooth surface caries in 13-year-old children. Caries Res. 1969;3(2):190–199. doi: 10.1159/000259582. [DOI] [PubMed] [Google Scholar]
  5. Duany L. F., Fitzgerald R. J., Llorente M., Zinner D. D. Effects of povidone-iodine and isotonic saline on the oral health of children. J Prev Dent. 1975 May-Jun;2(3):22–27. [PubMed] [Google Scholar]
  6. Emilson C. G., Krasse B., Rölla G. The effect of some bis-biguanides on experimental dental caries in the hamster. Caries Res. 1976;10(5):352–362. doi: 10.1159/000260216. [DOI] [PubMed] [Google Scholar]
  7. FITZGERALD R. J., JORDAN H. V., STANLEY H. R. Experimental caries and gingival pathologic changes in the gnotobiotic rat. J Dent Res. 1960 Sep-Oct;39:923–935. doi: 10.1177/00220345600390052701. [DOI] [PubMed] [Google Scholar]
  8. FITZGERALD R. J., KEYES P. H. Demonstration of the etiologic role of streptococci in experimental caries in the hamster. J Am Dent Assoc. 1960 Jul;61:9–19. doi: 10.14219/jada.archive.1960.0138. [DOI] [PubMed] [Google Scholar]
  9. Fisher R. G., Quintana R. P., Boulware M. A. Surface-chemical studies on chlorhexidine and related compounds: I. Effects at air-water, n-hexane-water, and hydroxyapatite-water interfaces. J Dent Res. 1975 Jan-Feb;54(1):20–24. doi: 10.1177/00220345750540012901. [DOI] [PubMed] [Google Scholar]
  10. Fisher R. G., Quintana R. P. Surface-chemical studies on chlorhexidine and related compounds: II. Interactions with monomolecular-film systems. J Dent Res. 1975 Jan-Feb;54(1):25–31. doi: 10.1177/00220345750540013001. [DOI] [PubMed] [Google Scholar]
  11. GIBBONS R. J. BACTERIOLOGY OF DENTAL CARIES. J Dent Res. 1964 Nov-Dec;43:SUPPL–SUPPL:1028. doi: 10.1177/00220345640430060301. [DOI] [PubMed] [Google Scholar]
  12. Garberoglio R., Brännström M. Scanning electron microscopic investigation of human dentinal tubules. Arch Oral Biol. 1976;21(6):355–362. doi: 10.1016/s0003-9969(76)80003-9. [DOI] [PubMed] [Google Scholar]
  13. Gibbons R. J., Depaola P. F., Spinell D. M., Skobe Z. Interdental localization of Streptococcus mutans as related to dental caries experience. Infect Immun. 1974 Mar;9(3):481–488. doi: 10.1128/iai.9.3.481-488.1974. [DOI] [PMC free article] [PubMed] [Google Scholar]
  14. Gibbons R. J., Kapsimalis B. Estimates of the overall rate of growth of the intestinal microflora of hamsters, guinea pigs, and mice. J Bacteriol. 1967 Jan;93(1):510–512. doi: 10.1128/jb.93.1.510-512.1967. [DOI] [PMC free article] [PubMed] [Google Scholar]
  15. Gjermo P., Baastad K. L., Rölla G. The plaque=inhibiting capacity of 11 antibacterial compounds. J Periodontal Res. 1970;5(2):102–109. doi: 10.1111/j.1600-0765.1970.tb00700.x. [DOI] [PubMed] [Google Scholar]
  16. Guggenheim B., König K. G., Mühlemann H. R. Modifications of the oral bacterial flora and their influence on dental caries in the rat. I. The effects of inoculating 4 labelled strains of streptococci. Helv Odontol Acta. 1965 Oct;9(2):121–129. [PubMed] [Google Scholar]
  17. Guggenheim B. Streptococci of dental plaques. Caries Res. 1968;2(2):147–163. doi: 10.1159/000259553. [DOI] [PubMed] [Google Scholar]
  18. Howell A., Jr, Jordan H. V., Georg L. K., Pine L. Odontomyces viscosus, gen. nov., spec. nov., a filamentous microorganism isolated from periodontal plaque in hamsters. Sabouraudia. 1965 Jun;4(2):65–68. doi: 10.1080/00362176685190181. [DOI] [PubMed] [Google Scholar]
  19. JORDAN H. V., FITZGERALD R. J., BOWLER A. E. Inhibition of experimental caries by sodium metabisulfite and its effect on the growth and metabolism of selected bacteria. J Dent Res. 1960 Jan-Feb;39:116–123. doi: 10.1177/00220345600390010501. [DOI] [PubMed] [Google Scholar]
  20. JORDAN H. V., KEYES P. H. AEROBIC, GRAM-POSITIVE, FILAMENTOUS BACTERIA AS ETIOLOGIC AGENTS OF EXPERIMENTAL PERIODONTAL DISEASE IN HAMSTERS. Arch Oral Biol. 1964 Jul-Aug;9:401–414. doi: 10.1016/0003-9969(64)90025-1. [DOI] [PubMed] [Google Scholar]
  21. Jordan H. V., Keyes P. H., Bellack S. Periodontal lesions in hamsters and gnotobiotic rats infected with actinomyces of human origin. J Periodontal Res. 1972;7(1):21–28. doi: 10.1111/j.1600-0765.1972.tb00627.x. [DOI] [PubMed] [Google Scholar]
  22. KEYES P. H., JORDAN H. V. PERIODONTAL LESIONS IN THE SYRIAN HAMSTER. III. FINDINGS RELATED TO AN INFECTIOUS AND TRANSMISSIBLE COMPONENT. Arch Oral Biol. 1964 Jul-Aug;9:377–400. doi: 10.1016/0003-9969(64)90024-x. [DOI] [PubMed] [Google Scholar]
  23. Lobene R. R., Soparkar P. M. The effect of an alexidine mouthwash on human plaque and gingivitis. J Am Dent Assoc. 1973 Oct;87(4):848–851. doi: 10.14219/jada.archive.1973.0512. [DOI] [PubMed] [Google Scholar]
  24. Löe H., Schiött C. R., Karring G., Karring T. Two years oral use of chlorhexidine in man. I. General design and clinical effects. J Periodontal Res. 1976 Jun;11(3):135–144. doi: 10.1111/j.1600-0765.1976.tb00061.x. [DOI] [PubMed] [Google Scholar]
  25. McCabe R. M., Keyes P. H., Howell A., Jr An in vitro method for assessing the plaque forming ability of oral bacteria. Arch Oral Biol. 1967 Dec;12(12):1653–1656. doi: 10.1016/0003-9969(67)90200-2. [DOI] [PubMed] [Google Scholar]
  26. Newman H. N., Poole D. F. Structural and ecological aspects of dental plaque. Soc Appl Bacteriol Symp Ser. 1974;3(0):111–134. [PubMed] [Google Scholar]
  27. Quintana R. P., Fisher R. G., Lasslo A. Surface-active factors in the efficacy of chlorhexidine against plaque. J Dent Res. 1972 Nov-Dec;51(6):1687–1687. doi: 10.1177/00220345720510064301. [DOI] [PubMed] [Google Scholar]
  28. Socransky S. S., Hubersak C., Propas D. Induction of periodontal destruction in gnotobiotic rats by a human oral strain of Actinomyces naeslundii. Arch Oral Biol. 1970 Oct;15(10):993–995. doi: 10.1016/0003-9969(70)90095-6. [DOI] [PubMed] [Google Scholar]
  29. Tanzer J. M., McCabe R. M. Selection of plaque-forming streptococci by the serial passage of wires through sucrose-containing broth. Arch Oral Biol. 1968 Jan;13(1):139–143. doi: 10.1016/0003-9969(68)90045-9. [DOI] [PubMed] [Google Scholar]
  30. Tanzer J. M., Reid Y., Reid W. Method for preclinical evaluation of antiplaque agents. Antimicrob Agents Chemother. 1972 May;1(5):376–380. doi: 10.1128/aac.1.5.376. [DOI] [PMC free article] [PubMed] [Google Scholar]
  31. Tanzer J. M., Slee A. M., Kamay B., Scheer E. R. In vitro evaluation of three iodine-containing compounds as antiplaque agents. Antimicrob Agents Chemother. 1977 Jul;12(1):107–113. doi: 10.1128/aac.12.1.107. [DOI] [PMC free article] [PubMed] [Google Scholar]
  32. Tanzer J. M., Wood W. I., Krichevsky M. I. Linear growth kinetics of plaque-forming streptococci in the presence of sucrose. J Gen Microbiol. 1969 Sep;58(1):125–133. doi: 10.1099/00221287-58-1-125. [DOI] [PubMed] [Google Scholar]
  33. Turesky S., Glickman I., Sandberg R. In vitro chemical inhibition of plaque formation. J Periodontol. 1972 May;43(5):263–269. doi: 10.1902/jop.1972.43.5.263. [DOI] [PubMed] [Google Scholar]
  34. Warner V. D., Mirth D. B., Turesky S. S., Glickman I. Synthesis and in vitro antiplaque activity of methylene homologs of chlorhexidine. J Pharm Sci. 1973 Jul;62(7):1189–1191. doi: 10.1002/jps.2600620729. [DOI] [PubMed] [Google Scholar]

Articles from Antimicrobial Agents and Chemotherapy are provided here courtesy of American Society for Microbiology (ASM)

RESOURCES