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肌氨酸酰胺的2-氯乙基亚硝脲类似物在SK-MG-1人胶质瘤细胞系中的细胞毒性作为转运的一种可能指标。

The cytotoxicity of a 2-chloroethylnitrosourea analog of sarcosinamide in the SK-MG-1 human glioma cell line as a possible indicator for transport.

作者信息

Skalski V, Feindel W, Panasci L C

机构信息

Lady Davis Institute for Medical Research, Sir Mortimer B. Davis - Jewish General Hospital, Montreal, Quebec, Canada.

出版信息

J Neurooncol. 1989 Jul;7(2):189-93. doi: 10.1007/BF00165103.

Abstract

The cytotoxicities of a new sarcosinamide analog of chloroethylnitrosourea (SarCNU) and of BCNU were examined in the glioma cell line SK-MG-1 in the presence or absence of excess concentrations of amino acids and sarcosinamide. The cytotoxicity of SarCNU, but not of BCNU, was significantly reduced in the presence of excess sarcosinamide. The stability of SarCNU was not significantly altered by increasing concentrations of sarcosinamide. In order to investigate the possibility that sarcosinamide inhibits the uptake of SarCNU the transport of tritiated sarcosinamide was examined in SK-MG-1 cells. The uptake of 3H-sarcosinamide was inhibited by excess, unlabelled sarcosinamide and SarCNU but not by BCNU, glycine or sarcosine. These results suggest the existence of a carrier-mediated transport for sarcosinamide which can accomodate SarCNU in SK-MG-1 cells.

摘要

在有或没有过量氨基酸和肌氨酸酰胺存在的情况下,在胶质瘤细胞系SK-MG-1中检测了一种新的氯乙基亚硝基脲肌氨酸酰胺类似物(SarCNU)和卡莫司汀(BCNU)的细胞毒性。在存在过量肌氨酸酰胺的情况下,SarCNU的细胞毒性显著降低,但BCNU的细胞毒性未降低。增加肌氨酸酰胺的浓度对SarCNU的稳定性没有显著影响。为了研究肌氨酸酰胺抑制SarCNU摄取的可能性,在SK-MG-1细胞中检测了氚标记肌氨酸酰胺的转运。过量的未标记肌氨酸酰胺和SarCNU可抑制3H-肌氨酸酰胺的摄取,但卡莫司汀、甘氨酸或肌氨酸则不能。这些结果表明,在SK-MG-1细胞中存在一种可容纳SarCNU的肌氨酸酰胺载体介导转运。

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