对贝壳杉烯酸衍生物的抗龋活性进行评估。

Evaluation of ent-kaurenoic acid derivatives for their anticariogenic activity.

作者信息

de Andrade Bruna B, Moreira Monique R, Ambrosio Sérgio R, Furtado Niege A J C, Cunha Wilson R, Heleno Vladimir C G, Silva Aline N, Simão Marília R, da Rocha Erilda M P, Martins Carlos H G, Veneziani Rodrigo C S

机构信息

Núcleo de Pesquisas em Ciências Exatas e Tecnológicas, Universidade de Franca, Franca, SP, Brazil.

出版信息

Nat Prod Commun. 2011 Jun;6(6):777-80.

PMID:21815409

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.

摘要

对映贝壳杉-16(17)-烯-19-酸（贝壳杉烯酸，KA）是天然抗龋剂的四环二萜原型。制备了六种KA衍生物，并评估了它们对参与龋齿过程的主要微生物的抗菌活性。KA的钠盐（KA-Na）活性最强，对大多数病原体显示出非常有前景的最低抑菌浓度（MIC）值。针对龋齿主要致病菌（变形链球菌）的时间-杀菌试验表明，KA和KA-Na仅在前12小时抑制生长，提示有抑菌作用。在此之后（12 - 24小时），其杀菌作用明显。在针对变形链球菌的棋盘法试验中，KA和KA-Na与金标准抗龋剂（盐酸氯己定，CHD）联合使用时未显示协同作用。