Biodistribution and toxicity of 2,4-divinyl-nido-o-carboranyldeuteroporphyrin IX in mice.
Biodistribution and toxicity of 2,4-divinyl-nido-o-carboranyldeuteroporphyrin IX in mice.
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2,4-二乙烯基-nido-o-碳硼烷基次卟啉 IX 在小鼠体内的生物分布和毒性。
DOI：
10.1016/0006-2952(92)90565-z
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发表时间：
1992
影响因子：
5.8
通讯作者：
Slatkin,DN
中科院分区：
文献类型：
--
作者：
Miura,M;Micca,PL;Heinrichs,JC;Gabel,D;Fairchild,RG;Slatkin,DN
对皮下移植KHJJ乳腺癌的BALB/c小鼠给予2，4-二乙烯-NIDO-0-Carboranyl-次卟啉IX(VCDP)，用于硼中子俘获治疗，以确定导致肿瘤最大硼摄取的剂量方案。总剂量为2 70±10μg/g体重，分4天多次给药(3次/d)，可获得30~50μg/g肿瘤。在这样的剂量后，检测血液中的血小板减少、粒细胞增多和肝酶水平的变化。注药后18小时至6天观察血硼清除情况。VCDP的毒性作用在最后一次注射后4-6天内消退。鉴于-gt；30μg/g的硼从VCDP在肿瘤中的峰值累积，以及随后VCDP的毒性迅速逆转，VCDP在小型哺乳动物中的进一步研究与其分布、毒性和肿瘤中子俘获治疗的潜在临床应用似乎是有必要的。
BALB/c mice with transplanted subcutaneous KHJJ mammary carcinomas were given 2,4-divinyl-nido-0-carboranyldeuteroporphyrin IX (VCDP), a prospective boron carrier for boron neutron-capture therapy, to determine the dose schedule that results in maximal boron uptake in tumor. A total dose of 270 ± 10 μg/g body weight given in a 4-day multiple intraperitoneal injection schedule (3/day) resulted in 30–50 μg boron/g tumor. After such a dose, thrombocytopenia, granulocytosis and altered liver enzyme levels were measured in the blood. Blood boron clearance was followed for an 18 hr to 6 day post-injection period. Toxic effects of VCDP subsided within 4–6 days after the last injection. In view of the > 30μg/g peak accumulation of boron in tumor from VCDP and the subsequent rapid reversal of VCDP toxicity, further studies of VCDP in small mammals relevant to its distribution, toxicity and potential clinical use for neutron-capture therapy of tumors appear warranted.