The cytotoxicity of a 2-chloroethylnitrosourea analog of sarcosinamide in the SK-MG-1 human glioma cell line as a possible indicator for transport.
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.
Skalski
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Lady Davis Institute for Medical Research, Sir Mortimer B. Davis - Jewish General Hospital, Montreal, Quebec, Canada.
Feindel
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W
Panasci
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LC
D000970:Antineoplastic Agents / Q000494:pharmacology*; D001692:Biological Transport; D001932:Brain Neoplasms / Q000188:drug therapy* / Q000473:pathology; D002330:Carmustine / Q000031:analogs & derivatives* / Q000493:pharmacokinetics / Q000494:pharmacology; D002460:Cell Line; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D005910:Glioma / Q000188:drug therapy* / Q000473:pathology; D006801:Humans; D012521:Sarcosine / Q000031:analogs & derivatives / Q000494:pharmacology; D014316:Tritium; D014407:Tumor Cells, Cultured
D000970:Antineoplastic Agents; D014316:Tritium; C039977:N-methylglycinamide; C044565:2-((((2-chloroethyl)nitrosoamino)carbonyl)amino)propanamide; D002330:Carmustine; D012521:Sarcosine