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二卤二茂钛对移植到无胸腺小鼠体内的人结肠癌的活性。

Activity of titanocene dihalides against a human colon carcinoma heterotransplanted to athymic mice.

作者信息

Köpf-Maier P, Moormann A, Köpf H

出版信息

Eur J Cancer Clin Oncol. 1985 Jul;21(7):853-7. doi: 10.1016/0277-5379(85)90225-1.

Abstract

The antitumor activity of cis-diamminedichloroplatinum (II) and of two metallocene derivatives, titanocene dichloride (C5H5)2TiCl2 and titanocene dibromide (C5H5)2TiBr2, was investigated against a human colon adenocarcinoma heterotransplanted to athymic mice. The substances were administered at various doses on a Q2DX5 or a Q3DX5 schedule. Whereas cis-diamminedichloroplatinum (II) induced an only marginal tumor-inhibiting effect, both titanocenes markedly suppressed tumor development (T/C values: 23-40%) and caused stagnation and relative decrease of tumor growth, when they were applied in subtoxic doses far below the LD10 level. The results are remarkable with respect to the general insensitivity of human colorectal carcinomas to cytostatic agents.

摘要

研究了顺二氯二氨铂(II)以及两种茂金属衍生物二氯二茂钛(C5H5)2TiCl2和二溴二茂钛(C5H5)2TiBr2对移植到无胸腺小鼠体内的人结肠腺癌的抗肿瘤活性。这些物质以不同剂量按照Q2DX5或Q3DX5方案给药。顺二氯二氨铂(II)仅产生微弱的肿瘤抑制作用,而两种二茂钛在远低于LD10水平的亚毒性剂量下应用时,均显著抑制肿瘤发展(T/C值:23 - 40%),并导致肿瘤生长停滞和相对减缓。鉴于人类结直肠癌对细胞抑制剂普遍不敏感,这些结果值得关注。

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