Exploring how structural changes to new Licarin A derivatives effects their bioactive properties against rapid growing mycobacteria and biofilm formation
| Autor: | Jamie Anthony Hawkes, Diogo Teixeira Carvalho, Lívia de Figueiredo Diniz Castro, Laira Maria Faria Matias, Dalila Junqueira Alvarenga, Fallon dos Santos Siqueira, Breno Vilas Boas Raimundo, Marli Matiko Anraku de Campos, Lucas Martins Oliveira, Luiz Paulo Melchior de Oliveira Leão, Thiago dos Santos |
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| Rok vydání: | 2020 |
| Předmět: |
0301 basic medicine
Antioxidant Sulfamethoxazole medicine.drug_class medicine.medical_treatment 030106 microbiology Microbial Sensitivity Tests Antimycobacterial Microbiology Lignans Mycobacterium Myristica Distribution system 03 medical and health sciences chemistry.chemical_compound Antibiotic resistance Clarithromycin medicine Molecular modification Rapid growing mycobacteria Cytotoxicity Biofilm Nontuberculous Mycobacteria Anti-Bacterial Agents 030104 developmental biology Infectious Diseases Biochemistry chemistry Biofilms |
| Zdroj: | Microbial Pathogenesis. 144:104203 |
| ISSN: | 0882-4010 |
| DOI: | 10.1016/j.micpath.2020.104203 |
| Popis: | Several species of rapidly growing mycobacteria (RGM) have been associated with biofilms in areas such as biomedical devices, water distribution systems, cosmetic surgery, and catheter-related blood infections. Biofilms which exhibit antimicrobial resistance such as those formed by the genus Mycobacterium pose a significant risk to health and are of particular interest to researchers. Licarin A (a neolignan found in numerous plant species e.g. nutmeg) has been reported to show a wide range of biological actions including anti-inflammatory, antioxidant, and antibacterial properties. The aim of this study was to prepare a set of Licarin A derivatives and investigate the impact of specific structural changes on its antimycobacterial ability, and its effect on the biofilm formation of RGM species. Initially, the phenolic sub-unit and alkenyl side chain of Licarin A were modified to create derivatives with a higher partition coefficient; as the activity of a compound against mycobacteria seems to be strongly influenced by its hydrophobicity. Further, polar groups were inserted into the side chain to change the hydrophilic-lipophilic profile of the molecules. Results showed variability in the susceptibility profile of mycobacteria against the Licarin A derivatives under analysis. A number of the derivatives showed significant inhibitory activity of planktonic growth of the three strains of mycobacteria used, with even lower MIC values than those observed with reference drugs and Licarin A itself. Cytotoxicity assays showed they also have low toxicity, confirming that structural modifications to the Licarin A have made improvements to its antimycobacterial properties. |
| Databáze: | OpenAIRE |
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