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二茂钛配合物的肿瘤抑制作用:对两种异种移植的人肺癌的影响

Tumor inhibition by titanocene complexes: influence upon two xenografted human lung carcinomas.

作者信息

Köpf-Maier P

出版信息

J Cancer Res Clin Oncol. 1987;113(4):342-8. doi: 10.1007/BF00397717.

Abstract

The influence of the organometallic complexes titanocene dichloride, titanocene dibromide, titanocene bis(hydrogenmaleinate), and titanocene bis(p-aminothiophenolate) bis(hydrochloride) on the development of a lung adenocarcinoma and a small cell lung carcinoma, both xenografted into athymic mice, was investigated in the present study. The tumors were growing s.c., and the substances administered i.p. as fivefold injections according to a Q2D X 5 (every 2 days X 5) or a Q3D X 5 schedule. In the case of lung adenocarcinoma, titanocene complexes inhibited tumor growth by more than 50% resulting in treated/control values of 20%-50%. The suppression remained stable beyond the end of the treatment period. In the case of small cell lung carcinoma, only those Q2D X 5 schedules, which corresponded to LD10 doses, effected considerable and stable growth inhibition to less than 50% of control values. Titanocene dichloride showed the greatest activity against both human tumors, followed by the p-aminothiophenolate, and hydrogenmaleinate derivatives.

摘要

本研究考察了有机金属配合物二氯二茂钛、二溴二茂钛、双(马来酸氢根)二茂钛和双(对氨基苯硫酚根)二茂钛双盐酸盐对移植到无胸腺小鼠体内的肺腺癌和小细胞肺癌生长的影响。肿瘤通过皮下生长,物质按Q2D X 5(每2天X 5次)或Q3D X 5方案腹腔注射给药。对于肺腺癌,二茂钛配合物抑制肿瘤生长超过50%,导致治疗组/对照组值为20%-50%。抑制作用在治疗期结束后仍保持稳定。对于小细胞肺癌,只有那些对应于LD10剂量的Q2D X 5方案才会对生长产生显著且稳定的抑制作用,使其低于对照组值的50%。二氯二茂钛对两种人类肿瘤的活性最高,其次是对氨基苯硫酚根和马来酸氢根衍生物。

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