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泼尼莫司汀及其分子成分苯丁酸氮芥和泼尼松龙对大鼠乳腺肿瘤的抑制作用及亚急性毒性

Mammary tumour inhibition and subacute toxicity in rats of prednimustine and of its molecular components chlorambucil and prednisolone.

作者信息

Fredholm B, Gunnarsson K, Jensen G, Müntzing J

出版信息

Acta Pharmacol Toxicol (Copenh). 1978 Mar;42(3):159-63. doi: 10.1111/j.1600-0773.1978.tb02185.x.

Abstract

Prednimustine, a chlorambucil ester of pregnisolone, retarded growth of DMBA-induced mammary tumours in rats and reduced the number of tumours. A combination of chlorambucil and prednisolone (C + P) in the same proportion as in prednimustine, had similar effects, 8 and 26 mg per kg of the C + P combination being equipotnet to 16 and 64 mg per kg of prednimustine, respectively. The mortality figures suggested that prednimustine was considerably less toxic than equipotent doses of C + P. This toxicity difference was confirmed in a parallel investigation of the subacute toxicity in rats of prednimustine and C + P. This study showed that the mortality, reduction of lymphocytes and platelets, and bone marrow depression was much lower after pregnimustine than after equimolar amounts of the C + P combination. The results suggest that the low toxicity of prednimustine makes this drug a better cytostatic agent than the C + P combination treatment.

摘要

泼尼莫司汀是泼尼松龙的苯丁酸氮芥酯,可抑制二甲基苯并蒽诱导的大鼠乳腺肿瘤生长并减少肿瘤数量。与泼尼莫司汀中相同比例的苯丁酸氮芥和泼尼松龙组合(C + P)具有相似的效果,每千克体重8毫克和26毫克的C + P组合分别与每千克体重16毫克和64毫克的泼尼莫司汀等效。死亡率数据表明,泼尼莫司汀的毒性远低于等效剂量的C + P。在对泼尼莫司汀和C + P在大鼠中的亚急性毒性进行的平行研究中证实了这种毒性差异。该研究表明,泼尼莫司汀给药后,死亡率、淋巴细胞和血小板减少以及骨髓抑制程度均远低于等摩尔量的C + P组合给药后。结果表明,泼尼莫司汀的低毒性使其成为比C + P联合治疗更好的细胞抑制剂。

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