Anticariogenic properties of ent-pimarane diterpenes obtained by microbial transformation.
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 μg 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.
Nucleus of Research in Sciences and Technology, University of Franca, Franca, SP, Brazil.
Marcela E
ME
Severiano
Marília R
MR
Simão
Thiago S
TS
Porto
Carlos H G
CH
Martins
Rodrigo C S
RC
Veneziani
Niege A J C
NA
Furtado
Nilton S
NS
Arakawa
Suraia
S
Said
Dionéia C R
DC
de Oliveira
Wilson R
WR
Cunha
Luiz E
LE
Gregório
Sérgio R
SR
Ambrósio
D045784:Abietanes / Q000737:chemistry / Q000494:pharmacology*; D000900:Anti-Bacterial Agents / Q000737:chemistry / Q000494:pharmacology*; D003731:Dental Caries / Q000188:drug therapy* / Q000382:microbiology; D005658:Fungi; D006090:Gram-Negative Bacteria / Q000254:growth & development*; D006801:Humans
D045784:Abietanes; D000900:Anti-Bacterial Agents