Graduate Program in Biological Sciences-PPGCB, Federal University of Pernambuco-UFPE, Recife, PE, Brazil.
Laboratory of Semi-Arid Bioprospecting (LABSEMA), Regional University of Cariri-URCA, Crato, CE, Brazil.
Biomed Res Int. 2022 Jul 19;2022:1440996. doi: 10.1155/2022/1440996. eCollection 2022.
Efflux pumps are transmembrane proteins that expel drugs out of a bacterial cell contributing to microorganism drug resistance. Several studies addressing the use of natural products with medicinal properties have intensified given the above. Thus, the aim of the present study was to investigate the antibacterial activity and the O-eugenol potential in resistance reversal by efflux pump inhibition, as well as to evaluate its toxicity in the arthropod model. The broth microdilution method was used to determine the minimum inhibitory concentration (MIC) and the O-eugenol efflux pump inhibition. For the toxicity assays, mortality and locomotor system damage were performed using the fumigation method.
O-eugenol presented a MIC of 1024 g/mL against . The association of this compound with the antibiotic tetracycline demonstrated a synergistic effect ( < 0.0001), this also being observed when the antibiotic was associated with ethidium bromide ( < 0.0001); thus, these results may be attributable to an efflux pump inhibition. The mortality and geotaxis assays revealed the compound is toxic, with an EC of 18 g/mL within 48 hours of exposure.
While we can conclude that the tested product has an efflux pump inhibitory effect, further studies are needed to elucidate its mechanisms of action, in addition to assays using other strains to verify whether the substance has the same inhibitory effect.
外排泵是一种跨膜蛋白，可将药物从细菌细胞中排出，导致微生物耐药性。鉴于此，许多研究都集中在具有药用特性的天然产物的应用上。因此，本研究旨在研究 O-丁香酚的抗菌活性和逆转耐药性的潜力，通过抑制外排泵来逆转耐药性，并评估其在节肢动物模型中的毒性。采用肉汤微量稀释法测定最小抑菌浓度（MIC）和 O-丁香酚外排泵抑制作用。为了进行毒性试验，采用熏蒸法测定死亡率和运动系统损伤。
O-丁香酚对 的 MIC 为 1024μg/ml。该化合物与抗生素四环素联合使用表现出协同作用（<0.0001），与溴化乙锭联合使用时也观察到这种协同作用（<0.0001）；因此，这些结果可能归因于外排泵的抑制作用。死亡率和趋地性试验表明该化合物具有毒性，暴露于 18μg/ml 的化合物 48 小时内 EC 值为 18μg/ml。
虽然我们可以得出结论，测试的产品具有外排泵抑制作用，但需要进一步的研究来阐明其作用机制，以及使用其他菌株进行的测定，以验证该物质是否具有相同的抑制作用。
