title: Evaluation of ent-kaurenoic acid derivatives for their anticariogenic activity.
abstract: Ent-kaur-16(17)-en-19-oic acid (kaurenoic acid, KA) is a tetracyclic diterpene prototype for natural anticaries agents. Six KA derivatives were prepared and their antimicrobial activity against the main microorganisms involved in the caries process evaluated. The sodium salt of KA (KA-Na) was the most active, displaying very promising MIC values for most pathogens. Time-kill assays against the primary causative agent of caries (Streptococcus mutans) indicated that KA and KA-Na only inhibited growth in the first 12 h, suggesting a bacteriostatic effect. After this period (12-24 h), their bactericidal effect was clearly noted. KA and KA-Na showed no synergy when combined with the gold standard anticariogenic (chlorhexidine dihydrochloride, CHD) in the checkerboard assays against S. mutans.
authors.affiliation: Núcleo de Pesquisas em Ciências Exatas e Tecnológicas, Universidade de Franca, Franca, SP, Brazil.
authors.forename: Bruna B
authors.initials: BB
authors.lastname: de Andrade
authors.forename: Monique R
authors.initials: MR
authors.lastname: Moreira
authors.forename: Sérgio R
authors.initials: SR
authors.lastname: Ambrosio
authors.forename: Niege A J C
authors.initials: NA
authors.lastname: Furtado
authors.forename: Wilson R
authors.initials: WR
authors.lastname: Cunha
authors.forename: Vladimir C G
authors.initials: VC
authors.lastname: Heleno
authors.forename: Aline N
authors.initials: AN
authors.lastname: Silva
authors.forename: Marília R
authors.initials: MR
authors.lastname: Simão
authors.forename: Erilda M P
authors.initials: EM
authors.lastname: da Rocha
authors.forename: Carlos H G
authors.initials: CH
authors.lastname: Martins
authors.forename: Rodrigo C S
authors.initials: RC
authors.lastname: Veneziani
mesh_terms: D000900:Anti-Bacterial Agents / Q000737:chemistry* / Q000494:pharmacology*; D003731:Dental Caries / Q000382:microbiology / Q000517:prevention & control*; D004224:Diterpenes / Q000737:chemistry* / Q000494:pharmacology*; D008826:Microbial Sensitivity Tests; D035742:Mikania / Q000737:chemistry; D015394:Molecular Structure; D018515:Plant Leaves / Q000737:chemistry; D013295:Streptococcus mutans / Q000187:drug effects*
chemical_list: D000900:Anti-Bacterial Agents; D004224:Diterpenes; C051436:kaurenoic acid