Antimicrobial activity of kaurane diterpenes against oral pathogens.
Two kaurane diterpenes, ent-kaur-16(17)-en-19-oic acid (KA) and 15-beta-isovaleryloxy-ent-kaur-16(17)-en-19-oic acid (KA-Ival), isolated from Aspilia foliacea, and the methyl ester derivative of KA (KA-Me) were evaluated against oral pathogens. KA was the most active compound, with MIC values of 10 microg mL(-1) against the following microorganisms: Streptococcus sobrinus, Streptococcus mutans, Streptococcus mitis, Streptococcus sanguinis, and Lactobacillus casei. However, KA did not show significant activity against Streptococcus salivarius and Enterococcus faecalis, with MIC values equal to 100 and 200 microg mL(-1), respectively. Our results show that KA has potential to be used as a prototype for the discovery of new effective anti-infection agents against microorganisms responsible for caries and periodontal diseases. Moreover, these results allow to conclude that minor structural differences among these diterpenes significantly influence their antimicrobial activity, bringing new perspectives to studies on the structure-activity relationship of this type of metabolites with respect to caries and periodontal diseases.
Ambrosio
Sergio R
SR
Núcleo de Pesquisas em Ciências Exatas e Tecnológicas, Universidade de Franca, Franca, SP, Brazil.
Furtado
Niege A J C
NA
de Oliveira
Dionéia C R
DC
da Costa
Fernando B
FB
Martins
Carlos H G
CH
de Carvalho
Tatiane C
TC
Porto
Thiago S
TS
Veneziani
Rodrigo C S
RC
D000900:Anti-Bacterial Agents / Q000302:isolation & purification* / Q000494:pharmacology; D019659:Asteraceae / Q000737:chemistry; D045786:Diterpenes, Kaurane / Q000302:isolation & purification* / Q000494:pharmacology*; D006801:Humans; D007780:Lacticaseibacillus casei / Q000187:drug effects*; D008826:Microbial Sensitivity Tests; D009055:Mouth / Q000382:microbiology*; D010936:Plant Extracts / Q000302:isolation & purification / Q000494:pharmacology; D018517:Plant Roots / Q000737:chemistry; D013291:Streptococcus / Q000187:drug effects*
D000900:Anti-Bacterial Agents; D045786:Diterpenes, Kaurane; D010936:Plant Extracts