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[α,β-不饱和醛的化学组成与对小鼠艾氏实体瘤的治疗活性之间的关系]

[Relationship between Chemical Constitution and Theraeutic Activity of alpha, beta-unsaturated Aldehydes in the Ehrlich-Solid-Tumor of the Mouse].

作者信息

Zollner H, Esterbauer H, Schauenstein E

出版信息

Z Krebsforsch Klin Onkol Cancer Res Clin Oncol. 1975;83(1):27-30. doi: 10.1007/BF00284399.

Abstract

Biochemical and biological effects and chemical properties of three alpha,beta-unsaturated aldehydes [acrolein (I), 4-hydroxypentenal (II), and 4-hydroxyundecenal (III)] were compared. These three substances inhibited the incorporation of -3H-thymidine in Ehrlich-ascites-tumor cells in vitro in the following order: I is greater than III is greater than II. For reactivities with glutathion in vitro the order was: I is greater than II is greater than III is greater than. We concluded there from that the high activity of I, as to its inhibition of thymidine incorporation and its toxicity, was related to its high activity against SH-groups. With respect to therapeutic effects and hydrophilia the following order: II is greater than I is greater than III was observed. In our opinion the high hydrophilia of II is responsible for the significant and good inhibition of tumour growth.

摘要

比较了三种α,β-不饱和醛[丙烯醛(I)、4-羟基戊烯醛(II)和4-羟基十一碳烯醛(III)]的生化和生物学效应以及化学性质。这三种物质在体外对艾氏腹水癌细胞中-3H-胸腺嘧啶核苷掺入的抑制作用顺序如下:I>III>II。对于它们在体外与谷胱甘肽的反应活性,顺序为:I>II>III。由此我们得出结论,I在抑制胸腺嘧啶核苷掺入及其毒性方面的高活性与其对SH基团的高活性有关。关于治疗效果和亲水性,观察到以下顺序:II>I>III。我们认为II的高亲水性是其对肿瘤生长有显著且良好抑制作用的原因。

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