Onoue Satomi, Hosoi Kazuhiro, Wakuri Shinobu, Iwase Yumiko, Yamamoto Toshinobu, Matsuoka Naoko, Nakamura Kazuichi, Toda Tsuguto, Takagi Hironori, Osaki Naoto, Matsumoto Yasuhiro, Kawakami Satoru, Seto Yoshiki, Kato Masashi, Yamada Shizuo, Ohno Yasuo, Kojima Hajime
Department of Pharmacokinetics and Pharmacodynamics, School of Pharmaceutical Sciences, University of Shizuoka, 52-1 Yada, Suruga-ku, Shizuoka, 422-8526, Japan.
J Appl Toxicol. 2013 Nov;33(11):1241-50. doi: 10.1002/jat.2776. Epub 2012 Jun 13.
A reactive oxygen species (ROS) assay was previously developed for photosafety evaluation of pharmaceuticals, and the present multi-center study aimed to establish and validate a standard protocol for ROS assay. In three participating laboratories, two standards and 42 coded chemicals, including 23 phototoxins and 19 nonphototoxic drugs/chemicals, were assessed by the ROS assay according to the standardized protocol. Most phototoxins tended to generate singlet oxygen and/or superoxide under UV-vis exposure, but nonphototoxic chemicals were less photoreactive. In the ROS assay on quinine (200 µm), a typical phototoxic drug, the intra- and inter-day precisions (coefficient of variation; CV) were found to be 1.5-7.4% and 1.7-9.3%, respectively. The inter-laboratory CV for quinine averaged 15.4% for singlet oxygen and 17.0% for superoxide. The ROS assay on 42 coded chemicals (200 µm) provided no false negative predictions upon previously defined criteria as compared with the in vitro/in vivo phototoxicity, although several false positives appeared. Outcomes from the validation study were indicative of satisfactory transferability, intra- and inter-laboratory variability, and predictive capacity of the ROS assay.
先前已开发出一种用于药物光安全性评估的活性氧(ROS)检测方法,本多中心研究旨在建立并验证ROS检测的标准方案。在三个参与实验室中,根据标准化方案,通过ROS检测对两种标准品和42种编码化学品进行了评估,其中包括23种光毒素和19种非光毒性药物/化学品。大多数光毒素在紫外-可见光照射下倾向于产生单线态氧和/或超氧化物,但非光毒性化学品的光反应性较低。在对典型光毒性药物奎宁(200µm)进行的ROS检测中,日内和日间精密度(变异系数;CV)分别为1.5-7.4%和1.7-9.3%。奎宁的实验室间CV,单线态氧平均为15.4%,超氧化物为17.0%。对42种编码化学品(200µm)进行的ROS检测,与体外/体内光毒性相比,在先前定义的标准下未出现假阴性预测,尽管出现了一些假阳性。验证研究的结果表明,ROS检测具有令人满意的可转移性、实验室内和实验室间变异性以及预测能力。