Fourth Department of Surgery, Tokyo Medical University, Ibaraki Medical Center, Ibaraki 300-0395, Japan.
Oncol Rep. 2010 Jun;23(6):1517-22. doi: 10.3892/or_00000790.
The present study investigated the anticancer activity of 2-aminophenoxazine-3-one (Phx-3) and 2-amino-4,4 alpha-dihydro-4 alpha,7-dimethyl-3H-phenoxazine-3-one (Phx-1), which were obtained by improved preparation methods using bovine erythrocyte suspension, on colon cancer cell lines COLO201, DLD1 and PMCO1 in vitro. The preparation methods for Phx-1 and Phx-3 had the advantages of extensively shortening reaction time and reducing sample volumes up to one-seventh during treatment, compared with the conventional method using bovine hemoglobin solution, resulting in extensive reduction of handling time. Phx-1 and Phx-3 thus obtained were identified as pure by the absorption spectra and NMR spectra. These phenoxazines exerted strong, dose-dependent anticancer activity against colon cancer cell lines COLO201, DLD1 and PMCO1 in vitro and induced apoptosis of these cells. The present results demonstrate that Phx-1 and Phx-3, which were prepared by extensively improved methods using bovine erythrocytes, may be useful as therapeutic drugs against colon cancer that is intractable to chemotherapy.
本研究采用改良的牛红细胞悬液制备方法，制备了 2-氨基苯并恶嗪-3-酮（Phx-3）和 2-氨基-4,4α-二氢-4α,7-二甲基-3H-苯并恶嗪-3-酮（Phx-1），并研究了它们对体外结肠癌细胞系 COLO201、DLD1 和 PMCO1 的抗癌活性。与使用牛血红蛋白溶液的传统方法相比，Phx-1 和 Phx-3 的制备方法具有显著缩短反应时间和减少处理样品体积的优势，处理时间减少了约七分之六。通过吸收光谱和 NMR 光谱鉴定，Phx-1 和 Phx-3 为纯品。这些苯并恶嗪对体外结肠癌细胞系 COLO201、DLD1 和 PMCO1 表现出强烈的、剂量依赖性的抗癌活性，并诱导这些细胞凋亡。本研究结果表明，采用改良的牛红细胞悬液制备方法制备的 Phx-1 和 Phx-3 可能成为治疗对化疗耐药的结肠癌的有效药物。
