Hoefer Carrie C, Blair Rachael Hageman, Blanco Javier G
Department of Pharmaceutical Sciences, School of Pharmacy and Pharmaceutical Sciences, The State University of New York at Buffalo, Buffalo, New York 14260.
Department of Biostatistics, School of Public Health and Health Professions, The State University of New York at Buffalo, Buffalo, New York 14260.
J Pharm Sci. 2016 Jun;105(6):2005-2008. doi: 10.1016/j.xphs.2016.03.013. Epub 2016 Apr 23.
Daunorubicin (DAUN) and doxorubicin (DOX) are used to treat a variety of cancers. The use of DAUN and DOX is hampered by the development of cardiotoxicity. Clinical evidence suggests that patients with leukemia and Down syndrome are at increased risk for anthracycline-related cardiotoxicity. Carbonyl reductases and aldo-keto reductases (AKRs) catalyze the reduction of DAUN and DOX into cardiotoxic C-13 alcohol metabolites. Anthracyclines also exert cardiotoxicity by triggering mitochondrial dysfunction. In recent studies, a collection of heart samples from donors with and without Down syndrome was used to investigate determinants for anthracycline-related cardiotoxicity including cardiac daunorubicin reductase activity (DA), carbonyl reductase/AKRs protein expression, mitochondrial DNA content (mtDNA), and AKR7A2 DNA methylation status. In this study, the available demographic, biochemical, genetic, and epigenetic data were integrated through classification and regression trees analysis with the aim of pinpointing the most relevant variables for the synthesis of cardiotoxic daunorubicinol (i.e., DA). Seventeen variables were considered as potential predictors. Leave-one-out-cross-validation was performed for model selection and to estimate the generalization error. The classification and regression trees analysis model and variable importance measures suggest that cardiac mtDNA content, mtDNA(4977) deletion frequency, and AKR7A2 protein content are the most important variables in determining DA.
柔红霉素(DAUN)和阿霉素(DOX)用于治疗多种癌症。柔红霉素和阿霉素的使用因心脏毒性的发生而受到阻碍。临床证据表明,白血病和唐氏综合征患者发生蒽环类药物相关心脏毒性的风险增加。羰基还原酶和醛酮还原酶(AKRs)催化柔红霉素和阿霉素还原为具有心脏毒性的C-13醇代谢物。蒽环类药物还通过引发线粒体功能障碍发挥心脏毒性作用。在最近的研究中,收集了有或没有唐氏综合征的供体的心脏样本,以研究蒽环类药物相关心脏毒性的决定因素,包括心脏柔红霉素还原酶活性(DA)、羰基还原酶/AKRs蛋白表达、线粒体DNA含量(mtDNA)和AKR7A2 DNA甲基化状态。在本研究中,通过分类和回归树分析整合了可用的人口统计学、生化、遗传和表观遗传学数据,目的是找出合成具有心脏毒性的柔红霉素醇(即DA)最相关的变量。17个变量被视为潜在预测因子。采用留一法交叉验证进行模型选择并估计泛化误差。分类和回归树分析模型及变量重要性度量表明,心脏mtDNA含量、mtDNA(4977)缺失频率和AKR7A2蛋白含量是决定DA的最重要变量。