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(Reference retrieved automatically from Google Scholar through information on FAPESP grant and its corresponding number as mentioned in the publication by the authors.)

Anticariogenic Properties of ent-Pimarane Diterpenes Obtained by Microbial Transformation

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Author(s):
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Severiano, Marcela E. [1] ; Simao, Marilia R. [1] ; Porto, Thiago S. [1] ; Martins, Carlos H. G. [1] ; Veneziani, Rodrigo C. S. [1] ; Furtado, Niege A. J. C. [2] ; Arakawa, Nilton S. [3] ; Said, Suraia [2] ; de Oliveira, Dioneia C. R. [3] ; Cunha, Wilson R. [1] ; Gregorio, Luiz E. [2] ; Ambrosio, Sergio R. [2]
Total Authors: 12
Affiliation:
[1] Univ Franca, Franca, SP - Brazil
[2] Univ Sao Paulo, Fac Pharmaceut Sci Ribeirao Preto, BR-14049 Ribeirao Preto, SP - Brazil
[3] Vale do Paraiba Univ, Inst Res & Dev, Sao Jose Dos Campos, SP - Brazil
Total Affiliations: 3
Document type: Journal article
Source: Molecules; v. 15, n. 12, p. 8553-8566, 2010.
Web of Science Citations: 16
Abstract

In the present work, the anticariogenic activities of three pimarane-type diterpenes obtained by fungal biotransformation were investigated. Among these metabolites, ent-8(14), 15-pimaradien-19-ol was the most active compound, displaying very promising MIC values (ranging from 1.5 to 4.0 mu g mL(-1)) 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 ent-8(14), 15-pimaradien-19-ol against the primary causative agent S. mutans revealed that this compound only avoids growth of the inoculum in the first 12 h (bacteriostatic effect). However, its bactericidal effect is clearly noted thereafter (between 12 and 24 h). The curve profile obtained by combining ent-8(14), 15-pimaradien-19-ol and chlorhexidine revealed a significant reduction in the time necessary for killing S. mutans compared with each of these two chemicals alone. However, no synergistic effect was observed using the same combination in the checkerboard assays against this microorganism. In conclusion, our results point out that ent-8(14), 15-pimaradien-19-ol is an important metabolite in the search for new effective anticariogenic agents. (AU)

FAPESP's process: 07/54762-8 - Obtaining structural analogues of pimaradienoic acid through the process of fungal biotransformation and study of the effect of these metabolites on the activity of the TcDHODH enzyme and on the contraction of the vascular smooth muscle of the aorta artery of mice
Grantee:Sergio Ricardo Ambrosio
Support Opportunities: BIOTA-FAPESP Program - Young Investigators Grants