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磷酸雌莫司汀(艾去适)对雌激素敏感和不敏感的大鼠乳腺肿瘤生长抑制作用的初步研究

Pilot study on the growth inhibition by estramustine phosphate (Estracyt) of rat mammary tumours sensitive and insensitive of oestrogen.

作者信息

Müntzing J, Jensen G, Högberg B

出版信息

Acta Pharmacol Toxicol (Copenh). 1979 Jan;44(1):1-6. doi: 10.1111/j.1600-0773.1979.tb02287.x.

Abstract

Rat mammary tumours induced by 7,12-dimethylbenz(a)anthracene had a higher concentration of 3H and 14C than muscle after injection of estramustine phosphate labelled with 3H in the oestrogen moiety and 14C in the alkylating moiety. Thin-layer chromatography showed that dephosphorylated estramustine phosphate was present in the tumours but no free oestradiol-17beta. The uptake of the drug in the tumours was parallelled by a dose dependant retardation of tumour growth and a prevention of tumour number increase. Estramustine phosphate also retarded growth of mammary tumours resistant to treatment with oestradiol-17 beta. It is concluded that estramustine phosphate has a greater effect on tumour growth than oestrogen.

摘要

在用雌激素部分标记有³H、烷化部分标记有¹⁴C的磷酸雌莫司汀注射后,7,12 - 二甲基苯并(a)蒽诱导的大鼠乳腺肿瘤中³H和¹⁴C的浓度高于肌肉。薄层色谱显示肿瘤中存在去磷酸化的磷酸雌莫司汀,但没有游离的雌二醇 - 17β。药物在肿瘤中的摄取与肿瘤生长的剂量依赖性延缓以及肿瘤数量增加的预防同时发生。磷酸雌莫司汀还能延缓对雌二醇 - 17β治疗耐药的乳腺肿瘤的生长。结论是磷酸雌莫司汀对肿瘤生长的影响比雌激素更大。

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