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三茂铁盐作为V79细胞体外和KHT肿瘤体内放射增敏剂的高效性。

High efficiency of ferricenium salts as radiosensitizers of V79 cells in vitro and the KHT tumor in vivo.

作者信息

Joy A M, Goodgame D M, Stratford I J

机构信息

Chemistry Department, Imperial College of Science and Technology, London, U.K.

出版信息

Int J Radiat Oncol Biol Phys. 1989 Apr;16(4):1053-6. doi: 10.1016/0360-3016(89)90914-0.

DOI:10.1016/0360-3016(89)90914-0
PMID:2703386
Abstract

Ferricenium salts (Fc+X-) can act as radiosensitizers of hypoxic cells in vitro and of KHT tumor cells in vivo. Sensitization is manifest by a removal of the shoulder of the hypoxic radiation survival curve in vitro. This results in a dose modification factor (DMF) of 2.0 when measured at a surviving fraction of 0.1, for 10 mumol dm-3 FcPF6. In comparison, little sensitization is seen in air. The toxicity of these metal complexes, but not their radiosensitizing ability, can be decreased by including protein (Bovine serum albumin) in the medium. This may be related to the fact that the ferricenium complexes react readily with nucleophiles to generate OH radicals. Ferricenium trichloracetate, when given at a dose of 200 mg/kg to mice with the KHT tumor gives an enhancement ratio of 1.3.

摘要

铁鎓盐(Fc⁺X⁻)在体外可作为缺氧细胞的放射增敏剂,在体内可作为KHT肿瘤细胞的放射增敏剂。在体外,放射增敏表现为缺氧辐射存活曲线的肩部消失。对于10 μmol dm⁻³的FcPF₆,当存活分数为0.1时测量,剂量修正因子(DMF)为2.0。相比之下,在空气中几乎看不到增敏作用。通过在培养基中加入蛋白质(牛血清白蛋白),可以降低这些金属配合物的毒性,但不会降低其放射增敏能力。这可能与铁鎓配合物容易与亲核试剂反应生成羟基自由基这一事实有关。将三氯乙酸铁以200 mg/kg的剂量给予患有KHT肿瘤的小鼠时,增强比为1.3。

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1
High efficiency of ferricenium salts as radiosensitizers of V79 cells in vitro and the KHT tumor in vivo.三茂铁盐作为V79细胞体外和KHT肿瘤体内放射增敏剂的高效性。
Int J Radiat Oncol Biol Phys. 1989 Apr;16(4):1053-6. doi: 10.1016/0360-3016(89)90914-0.
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Oral (po) dosing with RSU 1069 or RB 6145 maintains their potency as hypoxic cell radiosensitizers and cytotoxins but reduces systemic toxicity compared with parenteral (ip) administration in mice.在小鼠中,与肠胃外(腹腔内)给药相比,口服(经口)给予RSU 1069或RB 6145可维持其作为乏氧细胞放射增敏剂和细胞毒素的效力,但能降低全身毒性。
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