Núcleo de Pesquisa em Ciências Exatas e Tecnológicas, Universidade de Franca, Franca, SP, Brazil.
Phytother Res. 2011 Feb;25(2):215-20. doi: 10.1002/ptr.3244.
In the present work, the anticariogenic activities of nine labdane type-diterpenes and four sesquiterpenes were investigated. Among these metabolites, (-)-copalic acid (CA) was the most active compound displaying MIC values very promising (ranging from 2.0 to 6.0 µg/mL) against the main microorganisms responsible for dental caries: Streptococcus salivarius, S. sobrinus, S. mutans, S. mitis, S. sanguinis and Lactobacillus casei. Time kill assays performed with CA against the primary causative agent (S. mutans) revealed that, in the first 12 h, this compound only inhibits the growth of the inoculum (bacteriostatic effect). However, its bactericidal effect is clearly noted thereafter (between 12 and 24 h). Also, CA did not show a synergistic effect when combined with the anticariogenic gold standard (chlorhexidine, CHD) in the checkerboard assays against S. mutans. In conclusion, the results points out CA as an important metabolite in the search for new effective anticariogenic agents.
在本工作中，研究了 9 种贝壳杉烷型二萜和 4 种倍半萜的抗龋活性。在这些代谢物中，(-)-粘康酸（CA）是最具活性的化合物，对导致龋齿的主要微生物具有非常有前景的 MIC 值（范围为 2.0 至 6.0 μg/mL）：唾液链球菌、变形链球菌、变形链球菌、米氏链球菌、血链球菌和干酪乳杆菌。用 CA 对主要病原体（变形链球菌）进行的时间杀伤试验表明，在最初的 12 小时内，该化合物仅抑制接种物的生长（抑菌作用）。然而，此后明显注意到其杀菌作用（在 12 至 24 小时之间）。此外，在棋盘试验中，CA 与抗龋金标准（洗必泰，CHD）联合使用时，对变形链球菌没有协同作用。总之，结果表明 CA 是寻找新的有效抗龋剂的重要代谢物。
