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茂金属对肿瘤的抑制作用:二卤代二茂钛(C5H5)2TiX2(X = F、Cl、Br、I、NCS)的抗肿瘤活性及其在缓冲溶液中的应用作为一种抑制药物诱导副作用的方法。

Tumor inhibition by metallocenes: antitumor activity of titanocene dihalides (C5H5)2TiX2 (X=F, Cl, Br, I, NCS) and their application in buffered solutions as a method for suppressing drug-induced side effects.

作者信息

Köpf-Maier P, Hesse B, Voigtländer R, Köpf H

出版信息

J Cancer Res Clin Oncol. 1980;97(1):31-9. doi: 10.1007/BF00411276.

Abstract

The antitumor activity of titanocene dihalides (C5H5)2TiX2 with X=F, Cl, Br, I, NCS is investigated against Ehrlich ascites tumor in CF 1 mice. Varying doses of the compounds are applied as single i.p. injections 24 h p.t.t. both in non-buffered (pH 1.4-3.9) and buffered (pH 4.2-5.9) solutions or suspensions, all of the substances achieving in optimum doses cure rates of 100% on day 120 p.t.t. This corresponds to I.L.S. values of 600-750% referred to the untreated controls. Some drug-induced side effects, especially the appearance of postperitonitic symptoms several weeks after i.p. application of higher doses of titanocene dihalides, are strikingly reduced by pH elevation in the injected drug solutions.

摘要

研究了二卤化钛茂(C5H5)2TiX2(X = F、Cl、Br、I、NCS)对CF1小鼠艾氏腹水瘤的抗肿瘤活性。在接种肿瘤后24小时,将不同剂量的化合物以单次腹腔注射的方式,应用于非缓冲(pH 1.4 - 3.9)和缓冲(pH 4.2 - 5.9)溶液或悬浮液中。所有物质在最佳剂量下,在接种肿瘤后120天的治愈率为100%。这相当于相对于未治疗对照组的600 - 750%的生命延长率(ILS)。通过提高注射药物溶液的pH值,一些药物引起的副作用,特别是在腹腔注射高剂量二卤化钛茂几周后出现的腹膜炎后症状,显著减少。

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