Laboratory of Bioprospection of Semiarid and Alternative Methods of the Regional University of Cariri - LABSEMA, Crato, Ceará, Brazil.
Laboratory of Bioprospection of Semiarid and Alternative Methods of the Regional University of Cariri - LABSEMA, Crato, Ceará, Brazil; Graduate Program in Biological Sciences, Federal University of Pernambuco, Recife, Pernambuco, Brazil.
Life Sci. 2021 Jan 1;264:118675. doi: 10.1016/j.lfs.2020.118675. Epub 2020 Oct 28.
Among the bacterial resistance mechanisms, efflux pumps are responsible for expelling xenobiotics, including bacterial cell antibiotics. Given this problem, studies are investigating new alternatives for inhibiting bacterial growth or enhancing the antibiotic activity of drugs already on the market. With this in mind, this study aimed to evaluate the antibacterial activity of Estragole against the RN4220 Staphylococcus aureus strain, which carries the MsrA efflux pump, as well as Estragole's toxicity in the Drosophila melanogaster arthropod model. The broth microdilution method was used to perform the Minimum Inhibitory Concentration (MIC) tests. Estragole was used at a Sub-Inhibitory Concentration (MIC/8) in association with erythromycin and ethidium bromide to assess its combined effect. As for Estragole's toxicity evaluation over D. melanogaster, the fumigation bioassay and negative geotaxis methods were used. The results were expressed as an average of sextuplicate replicates. A Two-way ANOVA followed by Bonferroni's post hoc test was used. The present study demonstrated that Estragole did not show a direct antibacterial activity over the RN4220 S. aureus strain, since it obtained a MIC ≥1024 μg/mL. The association of estragole with erythromycin demonstrated a potentiation of the antibiotic effect, reducing the MIC from 512 to 256 μg/mL. On the other hand, when estragole was associated with ethidium bromide (EtBr), an antagonism was observed, increasing the MIC of EtBr from 32 to 50.7968 μg/mL, demonstrating that estragole did not inhibited directly the MsrA efflux pump mechanism. We conclude that estragole has no relevant direct effect over bacterial growth, however, when associated with erythromycin, this reduced its MIC, potentiating the effect of the antibiotic.
在细菌耐药机制中,外排泵负责排出包括抗生素在内的细菌细胞内的异源物质。鉴于这个问题,研究人员正在探索新的替代方案,以抑制细菌生长或增强市场上现有药物的抗生素活性。考虑到这一点,本研究旨在评估茴香脑对携带 MsrA 外排泵的 RN4220 金黄色葡萄球菌菌株的抗菌活性,以及茴香脑在黑腹果蝇节肢动物模型中的毒性。采用肉汤微量稀释法进行最低抑菌浓度(MIC)测试。茴香脑在亚抑菌浓度(MIC/8)下与红霉素和溴化乙锭联合使用,以评估其联合作用。至于茴香脑对 D. melanogaster 的毒性评估,采用熏蒸生物测定和负趋地性方法。结果表示为六次重复的平均值。采用双因素方差分析(ANOVA),然后进行 Bonferroni 事后检验。本研究表明,茴香脑对 RN4220 金黄色葡萄球菌菌株没有直接的抗菌活性,因为它的 MIC 大于等于 1024μg/ml。茴香脑与红霉素联合使用显示出抗生素作用的增强,使 MIC 从 512 降至 256μg/ml。另一方面,当茴香脑与溴化乙锭(EtBr)联合使用时,观察到拮抗作用,使 EtBr 的 MIC 从 32 增加到 50.7968μg/ml,表明茴香脑并没有直接抑制 MsrA 外排泵机制。我们得出结论,茴香脑对细菌生长没有明显的直接作用,但与红霉素联合使用时,可降低其 MIC,增强抗生素的作用。