铑（II）配合物对荷艾氏瘤小鼠的抗肿瘤作用。

Antitumor effects of rhodium (II) complexes on mice bearing Ehrlich tumors.

作者信息

Reibscheid E M, Zyngier S, Maria D A, Mistrone R J, Sinisterra R D, Couto L G, Najjar R

机构信息

Departamento de Farmacologia, Universidade de São Paulo, Brasil.

出版信息

Braz J Med Biol Res. 1994 Jan;27(1):91-4.

PMID:8173534

Abstract

Rhodium (II) trifluoroacetate (TFARh), rhodium (II) trifluoroacetate adduct with sulfadiazine (TFARh.Sd) and rhodium (II) acetate adduct with sulfisoxazole (RhSx) were tested in mice for acute toxicity, antitumoral activity against Ehrlich ascites carcinoma and for viability of Ehrlich tumor cells in culture. At ip doses up to 60 mumol/kg (40-70 and 59 mg/kg, respectively), these compounds had no toxic effects up to 14 days. At ip doses of 10 mumol kg-1 day-1 for 5 days, TFARh and TFARh.Sd significantly increased the survival rate of mice bearing Ehrlich ascites cells (probability of survival to the end of 34th day, controls = 0.23, TFARh = 0.85, TFARh.Sd = 0.74). No significant effect was observed for RhSx. In vitro, these rhodium complexes at 40 microM significantly increased the number of dead cells in cultured Ehrlich tumor cells.

摘要

对三氟乙酸铑（II）（TFARh）、三氟乙酸铑（II）与磺胺嘧啶的加合物（TFARh.Sd）以及乙酸铑（II）与磺胺异恶唑的加合物（RhSx）进行了小鼠急性毒性试验、对艾氏腹水癌的抗肿瘤活性试验以及培养的艾氏肿瘤细胞活力试验。腹腔注射剂量高达60 μmol/kg（分别为40 - 70和59 mg/kg）时，这些化合物在14天内均无毒性作用。以10 μmol kg⁻¹ 天⁻¹ 的腹腔注射剂量连续注射5天，TFARh和TFARh.Sd显著提高了荷艾氏腹水细胞小鼠的存活率（存活至第34天结束的概率，对照组 = 0.23，TFARh = 0.85，TFARh.Sd = 0.74）。未观察到RhSx有显著作用。在体外，这些铑配合物在40 μM时显著增加了培养的艾氏肿瘤细胞中的死亡细胞数量。