Siegel D, Franklin W A, Ross D
Department of Pharmaceutical Sciences, School of Pharmacy, University of Colorado Health Sciences Center, Denver 80262, USA.
Clin Cancer Res. 1998 Sep;4(9):2065-70.
NAD(P)H:quinone oxidoreductase (NQO1) is a flavoenzyme that catalyzes the two-electron reduction of quinones and related compounds. With the use of biochemical assays, NQO1 has been shown to be overexpressed in many types of cancer, including non-small cell lung cancer (NSCLC). NQO1 can bioactivate antitumor quinones such as mitomycin C, and new quinone-based drugs are currently being developed to target this enzyme in tumors such as NSCLC. Because there is no information on the cell-specific expression of NQO1 in lung, the purpose of this study was to examine the expression of NQO1 in human NSCLC, small cell lung cancer, carcinoid lung tumors, and normal lung using immunohistochemistry. A high level of NQO1 protein expression was detected by immunohistochemistry in NSCLC (adenocarcinoma, squamous cell carcinoma, and bronchoalveolar carcinoma), but no NQO1 protein could be detected in small cell lung cancer or carcinoid lung tumors. In addition, NQO1 protein expression was examined by immunohistochemistry in normal lung tissue. A high level of NQO1 protein expression was detected by immunohistochemistry in normal lung respiratory epithelium, with the highest levels of expression observed in ciliated columnar epithelial cells. Significant amounts of NQO1 protein were also detected in the vascular endothelium and adipocytes. These data demonstrate that NQO1 is overexpressed in NSCLC. Cells in normal lung also contain marked NQO1 protein and may be damaged by drugs activated by NQO1. These data validate NSCLC as a target for NQO1-directed agents and suggest that the potential for lung toxicity be considered in the preclinical development of quinone-based antitumor drugs.
NAD(P)H:醌氧化还原酶(NQO1)是一种黄素酶,可催化醌类及相关化合物的双电子还原反应。通过生化分析已表明,NQO1在包括非小细胞肺癌(NSCLC)在内的多种癌症类型中均有过表达。NQO1可使抗肿瘤醌类如丝裂霉素C发生生物活化,目前正在研发新型基于醌类的药物,以靶向NSCLC等肿瘤中的该酶。由于尚无关于NQO1在肺中细胞特异性表达的信息,本研究旨在采用免疫组织化学方法检测NQO1在人非小细胞肺癌、小细胞肺癌、类癌性肺肿瘤及正常肺组织中的表达情况。免疫组织化学检测发现,非小细胞肺癌(腺癌、鳞状细胞癌和细支气管肺泡癌)中存在高水平的NQO1蛋白表达,但在小细胞肺癌或类癌性肺肿瘤中未检测到NQO1蛋白。此外,还采用免疫组织化学方法检测了正常肺组织中NQO1蛋白的表达情况。免疫组织化学检测发现,正常肺呼吸上皮中存在高水平的NQO1蛋白表达,其中以纤毛柱状上皮细胞中的表达水平最高。在血管内皮细胞和脂肪细胞中也检测到了大量的NQO1蛋白。这些数据表明,NQO1在非小细胞肺癌中过表达。正常肺组织中的细胞也含有显著的NQO1蛋白,可能会受到NQO1激活药物的损伤。这些数据证实非小细胞肺癌是NQO1导向药物的靶点,并提示在基于醌类的抗肿瘤药物临床前研发中应考虑肺毒性的可能性。