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首页> 外文期刊>British Journal of Cancer >AQ4N: an alkylaminoanthraquinone N-oxide showing bioreductive potential and positive interaction with radiation in vivo
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AQ4N: an alkylaminoanthraquinone N-oxide showing bioreductive potential and positive interaction with radiation in vivo

机译：AQ4N：一种烷基氨基蒽醌N-氧化物，在体内具有生物还原能力并与放射线呈正相互作用

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摘要

AQ4N (1,4-bis([2-(dimethylamino-N-oxide)ethyl]amino)5,8-dihydroxy- anthracene-9,10-dione) is a novel alkylaminoanthraquinone N-oxide which, on reduction, forms a stable DNA affinic cytotoxic compound AQ4. The in vivo anti-tumour efficacy of AQ4N was investigated in B6D2F1 mice bearing the T50/80 mammary carcinoma. The effect of the drug was evaluated in combination with hypobaric hypoxia and with radiation (single and multiple fractions). Systemic toxicity was assessed by weight loss post treatment. This was low for AQ4N and was less than that obtained with the bioreductive drugs, RSU 1069 (1-[3-aziridinyl-2-hydroxypropyl]-2-nitroimidazole) and SR 4233 (Tirapazamine, 3-amino-1,2,4-benzotriazine-1,4-dioxide). The anti-tumour effect of AQ4N was potentiated in vivo by combination with hypobaric hypoxia with a dose enhancement ratio of 5.1. This is consistent with the proposal that AQ4N was reduced in vivo to AQ4, resulting in enhanced anti-tumour toxicity. When AQ4N (200 mg kg-1) was combined with single dose radiation (12 Gy) the drug was shown to have an additive interaction with radiation. This was obtained even if the drug was administered from 4 days before to 6 h after radiation treatment. Equivalent anti-tumour activity was also shown when both AQ4N (200 mg kg-1) and radiation (5 x 3 Gy) were administered in fractionated schedules. In conclusion, AQ4N shows significant potential as a bioreductive drug for combination with fractionated radiotherapy.
机译：AQ4N（1,4-双（[2-（二甲基氨基-N-氧化物）乙基]氨基）5,8-二羟基蒽-9,10-二酮）是一种新型的烷基氨基蒽醌N-氧化物，在还原时可形成稳定的DNA亲和细胞毒性化合物AQ4。在携带T50 / 80乳腺癌的B6D2F1小鼠中研究了AQ4N的体内抗肿瘤功效。结合低压缺氧和放射（单次或多次）评估了药物的疗效。通过治疗后体重减轻评估全身毒性。这对AQ4N来说很低，并且比用生物还原药RSU 1069（1- [3-叠氮基-2-羟丙基] -2-硝基咪唑）和SR 4233（替拉帕明，3-氨基-1,2,4）所获得的要低。 -苯并三嗪-1,4-二氧化物）。 AQ4N的抗肿瘤作用通过与低压缺氧联合以5.1的剂量增强比在体内得到增强。这与AQ4N在体内被还原为AQ4从而提高抗肿瘤毒性的提议是一致的。当AQ4N（200 mg kg-1）与单剂量辐射（12 Gy）结合使用时，表明该药物与辐射具有加性相互作用。即使从放疗前4天到放疗后6小时服用药物，也能达到这一目的。当按分次给药方案同时给予AQ4N（200 mg kg-1）和放射线（5 x 3 Gy）时，也显示出等效的抗肿瘤活性。总而言之，AQ4N作为结合分次放疗的生物还原药物显示出巨大潜力。

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