(+)-Dehydroabietic Acid, an Abietane-Type Diterpene, Inhibits Staphylococcus aureus Biofilms in Vitro

International Journal of Molecular Sciences

Adyary Fallarero¹  Malena Skogman¹  Janni Kujala¹  Mohanathas Rajaratnam²  Vânia M. Moreira²  Jari Yli-Kauhaluoma² 

[1] Pharmaceutical Sciences, Department of Biosciences, Abo Akademi University, Artillerigatan 6 A, 3rd floor, Biocity, FI-20520, Turku, Finland; E-Mails:;Division of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Helsinki, Viikinkaari 5 E, P.O. Box 56, FI-00014, Helsinki, Finland; E-Mails:

关键词: anti-biofilm;    inhibitor;    biofilm;    Staphylococcus aureus;    abietic acid;    natural compounds;    phenotypic assays;    (+)-dehydroabietic acid;    screening;   

DOI  :  10.3390/ijms140612054

来源: mdpi

【 摘 要 】

Potent drugs are desperately needed to counteract bacterial biofilm infections, especially those caused by gram-positive organisms, such as Staphylococcus aureus. Moreover, anti-biofilm compounds/agents that can be used as chemical tools are also needed for basic in vitro or in vivo studies aimed at exploring biofilms behavior and functionability. In this contribution, a collection of naturally-occurring abietane-type diterpenes and their derivatives was tested against S. aureus biofilms using a platform consisting of two phenotypic assays that have been previously published by our group. Three active compounds were identified: nordehydroabietylamine (1), (+)-dehydroabietic acid (2) and (+)-dehydroabietylamine (3) that prevented biofilm formation in the low micromolar range, and unlike typical antibiotics, only 2 to 4-fold higher concentrations were needed to significantly reduce viability and biomass of existing biofilms. Compound 2, (+)-dehydroabietic acid, was the most selective towards biofilm bacteria, achieving high killing efficacy (based on log Reduction values) and it was best tolerated by three different mammalian cell lines. Since (+)-dehydroabietic acid is an easily available compound, it holds great potential to be used as a molecular probe in biofilms-related studies as well as to serve as inspirational chemical model for the development of potent drug candidates.

【 授权许可】

CC BY   
© 2013 by the authors; licensee MDPI, Basel, Switzerland