2-aminophenoxazine-3-one suppresses the growth of mouse malignant melanoma B16 cells transplanted into C57BL/6Cr slc mice
2-aminophenoxazine-3-one suppresses the growth of mouse malignant melanoma B16 cells transplanted into C57BL/6Cr slc mice
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DOI：
10.1248/bpb.29.2197
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发表时间：
2006-11-01
影响因子：
2
通讯作者：
Tomoda, Akio
中科院分区：
文献类型：
--
作者：
Miyano-Kurosaki, Naoko;Kurosaki, Kunihiko;Tomoda, Akio
由于吩恶嗪是放线菌素D的基本结构，具有很强的抗癌作用，我们研究了2-氨基吩恶嗪-3-酮（Phx-3）在体外和体内对小鼠恶性黑色素瘤B16细胞的抗癌作用。Phx-3对B16细胞的增殖有明显的抑制作用，并呈剂量依赖性。我们进一步研究了Phx-3对移植到雌性C57 BL/6Cr Sic小鼠中的小鼠恶性黑色素瘤B16细胞的体内作用。与对照组相比，用Phx-3（0.5mg/kg）处理完全抑制了移植到小鼠中的小鼠恶性黑素瘤B16细胞的生长。当用0.5 mg/kg剂量处理小鼠时，发现Phx-3在体重减轻、血液生化参数如天冬氨酸转氨酶（AST）、丙氨酸转氨酶（ALT）、血尿素氮（BUN）和肌酐的血清水平变化、通过病理方法检查的肝和肾功能障碍、竖毛和消瘦方面几乎没有副作用。这些结果表明，Phx-3可用于治疗恶性黑色素瘤患者的未来。
Since phenoxazine is an essential structure of actinomycin D, which exerts a strong anticancer effect, we examined the anticancer effect of 2-aminophenoxazine-3-one (Phx-3) on mouse malignant melanoma B16 cells in vitro and in vivo. Phx-3 inhibited proliferation of the B16 cells in a dose-dependent manner in vitro. We furthermore studied the in vivo effects of Phx-3 on mouse malignant melanoma B16 cells transplanted in female C57BL/6Cr Sic mice. Treatment with Phx-3 (0.5 mg/kg) completely suppressed the growth of mouse malignant melanoma B16 cells transplanted in mice as compared with the control group. Phx-3 was found to exert few adverse effects, in terms of bodyweight loss, changes in serum levels of blood biochemical parameters such as aspartate transaminase (AST), alanine transaminase (ALT), blood urea nitrogen (BUN) and creatinine, dysfunction of the liver and the kidney examined by pathological methods, piloerection and wasting, when mice were treated with a dose of 0.5 mg/kg. These results suggest that Phx-3 may be used to treat patients affected by malignant melanoma in future.