Maliar Tibor, Blažková Marcela, Polák Jaroslav, Maliarová Mária, Ürgeová Eva, Viskupičová Jana
Institute of Chemistry and Environmental Sciences, Faculty of Natural Sciences, University of Ss. Cyril and Methodius in Trnava, Nám. J. Herdu 2, 917 01 Trnava, Slovakia.
Institute of Biology and Biotechnology, Faculty of Natural Sciences, University of Ss. Cyril and Methodius in Trnava, Nám. J. Herdu 2, 917 01 Trnava, Slovakia.
Pharmaceuticals (Basel). 2024 Sep 24;17(10):1257. doi: 10.3390/ph17101257.
The balance between antioxidants and pro-oxidants plays a significant role in the context of oxidative stress, influenced by both physiological and non-physiological factors.
In this study, 18 prescribed antibiotics (including doxycycline hydrochloride, tigecycline, rifampicin, tebipenem, cefuroxime, cefixime, potassium clavulanate, colistin, ampicillin, amoxicillin, amikacin, nalidixic acid, azithromycin, pipemidic acid trihydrate, pivmecillinam, aztreonam, fosfomycin sodium, and ciprofloxacin) were subjected to simultaneous determination of antioxidant and pro-oxidant potential to assess if pro-oxidant activity is a dominant co-mechanism of antibacterial activity or if any antibiotic exhibits a balanced effect.
This study presents a recently developed approach for the simultaneous assessment of antioxidant and pro-oxidant potential on a single microplate in situ, applied to prescribed antibiotics.
Ten antibiotics from eighteen showed lower antioxidant or pro-oxidant potential, while five exhibited only mild potential with DPPH50 values over 0.5 mM. The pro-oxidant antioxidant balance index (PABI) was also calculated to determine whether antioxidant or pro-oxidant activity was dominant for each antibiotic. Surprisingly, three antibiotics-doxycycline hydrochloride, tigecycline, and rifampicin-showed significant measures of both antioxidant and pro-oxidant activities. Especially notable was tebipenem, a broad-spectrum, orally administered carbapenem, showed a positive PABI index ratio, indicating a dominant antioxidant over pro-oxidant effect.
These findings could be significant for both therapy, where the antibacterial effect is enhanced by radical scavenging activity, and biotechnology, where substantial pro-oxidant activity might limit microbial viability in cultures and consequently affect yield.
抗氧化剂和促氧化剂之间的平衡在氧化应激环境中起着重要作用，受到生理和非生理因素的影响。
在本研究中，对18种处方抗生素（包括盐酸多西环素、替加环素、利福平、替比培南、头孢呋辛、头孢克肟、克拉维酸钾、黏菌素、氨苄西林、阿莫西林、阿米卡星、萘啶酸、阿奇霉素、三水合吡哌酸、匹美西林、氨曲南、磷霉素钠和环丙沙星）进行抗氧化和促氧化潜力的同时测定，以评估促氧化活性是否是抗菌活性的主要共同机制，或者是否有任何抗生素表现出平衡效应。
本研究提出了一种最近开发的方法，用于在单个微孔板上原位同时评估抗氧化和促氧化潜力，并应用于处方抗生素。
18种抗生素中有10种显示出较低的抗氧化或促氧化潜力，而5种仅表现出轻度潜力，其DPPH50值超过0.5 mM。还计算了促氧化-抗氧化平衡指数（PABI），以确定每种抗生素的抗氧化或促氧化活性是否占主导地位。令人惊讶的是，三种抗生素——盐酸多西环素、替加环素和利福平——显示出显著的抗氧化和促氧化活性。特别值得注意的是替比培南，一种广谱口服碳青霉烯类抗生素，显示出正的PABI指数比，表明抗氧化作用优于促氧化作用。
这些发现对于治疗（其中自由基清除活性增强抗菌作用）和生物技术（其中大量的促氧化活性可能限制培养物中的微生物活力并因此影响产量）都可能具有重要意义。
