Beberok Artur, Wrześniok Dorota, Otręba Michał, Buszman Ewa
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Medical University of Silesia, Sosnowiec, Poland.
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Medical University of Silesia, Sosnowiec, Poland.
Pharmacol Rep. 2015 Feb;67(1):38-43. doi: 10.1016/j.pharep.2014.07.015. Epub 2014 Aug 10.
Fluoroquinolones are a group of broad spectrum bactericidal antibiotics used to treat various infections of urinary and respiratory systems, as well as in ophthalmology and dermatology. This class of antibiotics causes toxic effects directed to pigmented tissues, what introduces a serious limitation to their use. The aim of this work was to examine the impact of sparfloxacin on melanogenesis and the antioxidant defense system in normal human epidermal melanocytes, adult, lightly pigmented (HEMa-LP).
The effect of sparfloxacin on cell viability was determined by WST-1 assay; melanin content, tyrosinase activity as well as antioxidant enzymes activity were measured spectrophotometrically.
Sparfloxacin induced the concentration - dependent loss in melanocytes viability. The value of EC50 was determined to be ∼0.25 mM. Sparfloxacin inhibited tyrosinase activity and reduced the melanin content in human melanocytes. To study the antioxidant defense system in melanocytes, the activities of superoxide dismutase (SOD), catalase (CAT) and glutathione peroxidase (GPx) in cells exposed to sparfloxacin were determined. It was observed that sparfloxacin caused depletion of the antioxidant status of melanocytes.
The observed sparfloxacin-dependent inhibition of melanogenesis and changes of antioxidant enzymes activities in human melanocytes give a new insight into the mechanism of fluoroquinolones toxicity directed to pigmented tissues.
氟喹诺酮类是一类广谱杀菌抗生素，用于治疗泌尿系统和呼吸系统的各种感染，以及眼科和皮肤科疾病。这类抗生素会对色素组织产生毒性作用，这严重限制了它们的使用。这项工作的目的是研究司帕沙星对正常人表皮黑素细胞（成人，轻度色素沉着，HEMa-LP）黑色素生成和抗氧化防御系统的影响。
通过WST-1测定法确定司帕沙星对细胞活力的影响；用分光光度法测量黑色素含量、酪氨酸酶活性以及抗氧化酶活性。
司帕沙星诱导黑素细胞活力呈浓度依赖性丧失。确定EC50值约为0.25 mM。司帕沙星抑制人黑素细胞中的酪氨酸酶活性并降低黑色素含量。为了研究黑素细胞中的抗氧化防御系统，测定了暴露于司帕沙星的细胞中超氧化物歧化酶（SOD）、过氧化氢酶（CAT）和谷胱甘肽过氧化物酶（GPx）的活性。观察到司帕沙星导致黑素细胞的抗氧化状态耗竭。
观察到的司帕沙星依赖性抑制黑色素生成以及人黑素细胞中抗氧化酶活性的变化，为氟喹诺酮类对色素组织毒性作用的机制提供了新的见解。
