Whelan H T, Williams M B, Bajic D M, Segura A D, McAuliffe T L, Chitambar C R
Department of Neurology, Medical College of Wisconsin, Milwaukee 53226.
Pediatr Neurol. 1994 May;10(3):217-20. doi: 10.1016/0887-8994(94)90026-4.
In vitro and in vivo studies have established gallium nitrate as an effective chemotherapeutic agent against human medulloblastoma. In vitro, gallium nitrate reduced cell proliferation and DNA synthesis of medulloblastoma Daoy. Gallium inhibits the availability of 59Fe to ribonucleotide reductase and has a direct effect on the enzyme itself. In vivo, gallium demonstrated similar effects on the medulloblastoma Daoy cell line in nude mice. Tumor growth rate and actual size were decreased; however, severe nephrotoxicity and mortality were observed. In our study, intradermal injections of medulloblastoma Daoy cells were given to nude mice and then tumors were allowed to grow. Tumor-bearing mice received a 15-day gallium (50 mg/kg/day) regimen, 20-day rest, 7-day gallium (66.5 mg/kg/day) dose escalation regimen beginning when tumor size exceeded 8-10 mm in diameter. All treated and control mice received saline hyperhydration during both treatment sessions. Our study resulted in the prevention of severe toxicity and an inhibition of tumor growth. No toxicity occurred with gallium nitrate at 50 mg/kg/day. Severe morbidity and mortality were observed at the higher gallium dose level (66.5 mg/kg/day), suggesting that the 50 mg/kg/day dose is the appropriate level when investigating gallium nitrate as a chemotherapy agent in nude mice.
体外和体内研究已证实硝酸镓是一种有效的抗人髓母细胞瘤化疗药物。在体外,硝酸镓可降低髓母细胞瘤Daoy细胞的增殖和DNA合成。镓会抑制核糖核苷酸还原酶对59Fe的摄取,并对该酶本身产生直接影响。在体内,镓对裸鼠体内的髓母细胞瘤Daoy细胞系也表现出类似作用。肿瘤生长速率和实际大小均降低;然而,观察到严重的肾毒性和死亡率。在我们的研究中,将髓母细胞瘤Daoy细胞皮内注射到裸鼠体内,然后让肿瘤生长。荷瘤小鼠接受为期15天的镓(50毫克/千克/天)给药方案,休息20天,当肿瘤直径超过8 - 10毫米时开始为期7天的镓剂量递增给药方案(66.5毫克/千克/天)。在两个治疗阶段,所有治疗组和对照组小鼠均接受生理盐水补液。我们的研究实现了预防严重毒性并抑制肿瘤生长。50毫克/千克/天的硝酸镓未出现毒性。在较高的镓剂量水平(66.5毫克/千克/天)观察到严重的发病率和死亡率,这表明在将硝酸镓作为裸鼠化疗药物进行研究时,50毫克/千克/天的剂量是合适的水平。