Alkyl‐bisbiguanides as in vitro inhibitors of bacterial growth and dental plaque formation

Baker, Pamela J.; Coburn, Robert A.; Genco, Robert J.; Evans, R. T.

doi:10.1111/j.1600-0765.1979.tb00799.x

Cited by 7 publications

(5 citation statements)

References 18 publications

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“…These additional properties include penetration of pre-formed plaque and substantivity. All of these new agents had previously been shown by us to be substantive to salivary-pellicle-covered enamel surfaces (Baker et al, 1979). Hence, these agents can be expected to bind to mucous membranes and teeth with salivary pellicles and to be released inactive form for prolonged periods of time.…”

Section: Discussionmentioning

confidence: 97%

“…They may thus exert significant antibacterial effects in the oral cavity with intermittent use such as in a dentifrice or oral rinse. Substantivity studies (Baker et al, 1979) have also shown that the less lipophilic compounds 8 and 9 were among the most effective antiplaque agents. Tanzer et al (1977) Vol.…”

Section: Discussionmentioning

confidence: 97%

“…Alkyl bisbiguanides, in which the p-chlorophenyl groups of chlorhexidine have been replaced by straight or branched alkyl terminal moieties, are known to be as substantive as chlorhexidine and to prevent in vitro plaque formation (Baker et al, 1979). Various alkyl bisbiguanides, most notably alexidine (1,6-bis(2'ethylhexyl)biguanidohexane), have been shown to inhibit dental plaque and to reduce the level of gingivitis in clinical studies (Lobene and Soparkar, 1973;Spolsky and Forsythe, 1977).…”

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confidence: 99%

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Structural Determinants of Activity of Chlorhexidine and Alkyl Bisbiguanides Against the Human Oral Flora

Baker¹,

Coburn

Genco³

et al. 1987

J Dent Res

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We assayed chlorhexidine and a series of its analogues, in which the chlorophenyl terminal substituents were replaced with alkyl chains, for their in vitro antimicrobial activity against the Gram-negative and Gram-positive oral bacteria. Changes in antimicrobial activity were correlated with changes in agent structure for identification of structural criteria which may be important in the optimization of agent activity. Chlorhexidine showed substantial antimicrobial activity against the Gram-negative as well as the Gram-positive oral bacteria. The alkyl agents were comparable with chlorhexidine in their activity against Bacteroides gingivalis and Bacteroides intermedius, black-pigmented Gram-negative obligate anaerobes associated with periodontal disease in adults. Alkyl agents alexidine, heptihexidine (1,6-bis-n-heptylbiguanidohexane), hexoctidine (1,8-bis-n-hexylbiguanidoctane), and hexhexidine (1,6-bis-n-hexylbiguanidohexane), as well as chlorhexidine, were active against Actinobacillus actinomycetemcomitans, a Gram-negative organism associated with localized juvenile periodontitis. Hexidecidine (1,10-bis-n-hexylbiguanidodecane) and heptoctidine (1,8-bis-n-heptylbiguanidooctane) were more active, and hexhexidine was as active as chlorhexidine against Fusobacterium nucleatum, also associated with periodontal disease. Seven of the agents were more active than chlorhexidine against Actinomyces species. All test agents were active against Streptococcus mutans, a Gram-positive coccus associated with dental caries. Hexidecidine had activity equal to that of chlorhexidine when evaluated against the entire battery of organisms. Analysis of structure-activity relationships revealed that alkyl chains could replace chlorophenyl groups with retention or improvement of antimicrobial activity.(ABSTRACT TRUNCATED AT 250 WORDS)

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Section: Discussionmentioning

confidence: 97%

Section: Discussionmentioning

confidence: 97%

mentioning

confidence: 99%

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Structural Determinants of Activity of Chlorhexidine and Alkyl Bisbiguanides Against the Human Oral Flora

Baker¹,

Coburn

Genco³

et al. 1987

J Dent Res

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“…Greater adsorption of chlorhexidine digluconate may be needed to reach a meaningful antimicrobial effect in vivo. Another possibility may be that bisbiguanides, like chiorhexidine digiuconate, may be inactivated upon adsorption to the tooth in vivo and consequently may not exert any antimicrobial effect (Baker et al 1979). The obvious lack of antimicrobial activity from root surfaces immersed in chlorhexidine digluconate is also supported by observations from clinical studies using subgingival irrigation protocols (MacAipine et al i985, Braatz et al 1985.…”

Section: Discussionmentioning

confidence: 98%

“…1992). These observations may be explained by findings suggesting that only 10% adsorption of chlorhexidine digluconate to tooth surfaces may be expected following a 2-min exposure in vitro (Baker et al 1979). Greater adsorption of chlorhexidine digluconate may be needed to reach a meaningful antimicrobial effect in vivo.…”

Section: Discussionmentioning

confidence: 99%

Antimicrobial properties of human dentin impregnated with tetracycline HCI or chlorhexidine

Stabholz

Kettering

Aprecio

et al. 1993

J Clinic Periodontology

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Substantivity of tetracycline HCl and chlorhexidine digluconate to human root dentin was assessed in vitro. 51 extracted single-rooted teeth, their crowns removed, were assigned to 1 of 4 treatments in groups of 12. A control groups included 3 roots. Each group was divided into 3 subgroups to allow evaluation of drug exposure for 1, 3 or 5 min. The roots were immersed in tetracycline HCl (10 or 50 mg/ml) or chlorhexidine digluconate (0.12 or 0.2%) solutions following root planning. Control roots were immersed in sterile saline (0.9%). Following drug immersion, the roots were transferred to tubes containing 2 ml tris buffered saline. The tubes were incubated at room temperature for 22 days. Desorption media were replaced at 24-h intervals. Removed media were examined for antimicrobial activity using a microtiter assay in which bacterial growth was evaluated by optical density readings. Roots immersed in tetracycline HCl 50 mg/ml released antimicrobial activity to successive desorption media for 14 days. Tetracycline HCl 10 mg/ml activity lasted 4 days. Roots subjected to chlorhexidine digluconate released antimicrobial activity for 24 h only. Within each treatment, there were no differences between the 3 exposure intervals of 1, 3 or 5 min. Our findings suggest usage of the periodontally exposed instrumented root as a depot for sustained release of tetracycline HCl, but not chlorhexidine digluconate, to the subgingival environment. The substantiveness of tetracycline HCl seems related to drug concentration rather than the exposure interval. Clinical trials are needed to confirm the clinical significance of these in vitro observations.

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Correlation Between theIn VivoAndIn VitroAntimicrobial Properties of Commercially Available Mouthwash Preparations

Moneib

El-Said²,

Shibl³

1992

Journal of Chemotherapy

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The effectiveness of six commercially available mouthwashes against common buccal organisms was studied. The minimum inhibitory concentrations (MIC) for two of the studied mouthwashes (Corsodyl and Oraldene) against buccal organisms were determined in Todd Hewitt medium with or without 5% serum. The concentration of the active substance in these two mouthwashes was in excess of the corresponding MIC. When the medium was supplemented with serum, lower MIC values were observed. Kill-time determinations, used at half the concentration of the normal preparation, revealed a rapid lethal effect for all tested mouthwashes. The slowest lethal effect was observed with Fluocaril mouthwash. When mouthwashes were tested in volunteers, an immediate significant fall in salivary bacterial counts was produced by all except Fluocaril. With the latter mouthwash the decrease was significant 2-30 minutes after rinsing. The bacterial levels returned to pre-rinse levels after 30 minutes for Listerine, after 90 minutes for both Oraldene and Mint and after 180 minutes for Corsodyl, Fluocaril and Sansilla mouthwashes. The results indicate that there is a good correlation between in vivo efficacy and in vitro determination of all mouthwash preparations.

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Alkyl‐bisbiguanides as in vitro inhibitors of bacterial growth and dental plaque formation

Cited by 7 publications

References 18 publications

Structural Determinants of Activity of Chlorhexidine and Alkyl Bisbiguanides Against the Human Oral Flora

Structural Determinants of Activity of Chlorhexidine and Alkyl Bisbiguanides Against the Human Oral Flora

Antimicrobial properties of human dentin impregnated with tetracycline HCI or chlorhexidine

Correlation Between theIn VivoAndIn VitroAntimicrobial Properties of Commercially Available Mouthwash Preparations

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