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某些氟喹诺酮类药物的辐射诱导体外光毒性潜力。

Radiation-induced in vitro phototoxic potential of some fluoroquinolones.

作者信息

Ray R S, Agrawal N, Misra R B, Farooq M, Hans R K

机构信息

Photobiology Division, Industrial Toxicology Research Centre, Lucknow, India.

出版信息

Drug Chem Toxicol. 2006 Jan;29(1):25-38. doi: 10.1080/01480540500408572.

Abstract

Photosensitizing drugs that can damage cellular biomolecules is a matter of concern. Lomefloxacin, norfloxacin, ofloxacin, and enoxacin (broad-spectrum antibiotics of fluoroquinolone group) are used for the treatment of Gram-positive and Gram-negative bacterial infections. Phototoxicity and possible mechanism of their action was assessed under the exposure of ambient levels of UV-A, UV-B, and sunlight at a concentration generally used in the treatment of various diseases. Singlet oxygen (1O2), superoxide anion radical (O2.-) generation, DNA damage, and lipid peroxidation in human blood were studied. All the fluoroquinolones tested in this study produced 1O2 and O2.- under exposure to UV-A, UV-B, and sunlight depending on the concentrations (0 to 60 microg/mL) of the drugs. Enoxacin showed a higher yield of 1O2 and O2.- than other drugs. These materials also degraded deoxyguanosine and induced lipid peroxidation in vitro under exposure to UV-A, UV-B, and sunlight (depending on the dose of radiation). The formation of the reactive oxygen species (ROS) by the photoexcited drugs may be considered as a possible mechanism of their action.

摘要

能够损害细胞生物分子的光敏药物是一个令人担忧的问题。洛美沙星、诺氟沙星、氧氟沙星和依诺沙星(氟喹诺酮类广谱抗生素)用于治疗革兰氏阳性和革兰氏阴性细菌感染。在通常用于治疗各种疾病的浓度下,在环境水平的紫外线A、紫外线B和阳光照射下,评估了它们的光毒性及其可能的作用机制。研究了人体血液中的单线态氧(1O2)、超氧阴离子自由基(O2.-)生成、DNA损伤和脂质过氧化。本研究中测试的所有氟喹诺酮类药物在紫外线A、紫外线B和阳光照射下,根据药物浓度(0至60微克/毫升)产生1O2和O2.-。依诺沙星产生的1O2和O2.-比其他药物更高。在紫外线A、紫外线B和阳光照射下(取决于辐射剂量),这些物质在体外也会降解脱氧鸟苷并诱导脂质过氧化。光激发药物产生活性氧(ROS)可能被认为是其作用的一种可能机制。

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