This Article Full Text (PDF) Alert me when this article is cited Alert me if a correction is posted Services Email this article to a friend Similar articles in this journal Similar articles in PubMed Alert me to new issues of the journal Download to citation manager Citing Articles Citing Articles via Google Scholar Google Scholar Articles by Samy, T. S. A. Articles by Krishan, A. Search for Related Content PubMed PubMed Citation Articles by Samy, T. S. A. Articles by Krishan, A.

Experimental Pharmacology of Auromomycin in L1210 Tumor Cells in Vitro and in Vivo^{1, 2,}

Comprehensive Cancer Center for the State of Florida, Department of Oncology, University of Miami School of Medicine, Miami, Florida 33136

The antibiotic protein auromomycin (AUR) is composed of a chromophore and an apoprotein. The in vitro cytotoxic activity of AUR is associated with the chromophore, whereas the apoprotein is not cytotoxic. Exposure to AUR blocks cell cycle traverse in G₂-M phase. Both AUR and the chromophore exhibit antitumor activity against murine L1210 leukemia, both in vitro and in vivo. Similarly, neocarzinostatin and its chromophore also show antitumor activity against L1210 tumor cells in vitro and in vivo. AUR and neocarzinostatin apoproteins have no antitumor activity.

The pharmacokinetics of ¹²⁵I-labeled AUR in L1210 tumorbearing mice shows a triexponential drug decay and initial rapid clearance of drug from the blood. The distribution of AUR-associated radioactivity into various tissues is rapid, and at the end of 24 hr, there is little drug accumulation in the tissues. During the first hr, greater than 50% of the administered drug is eliminated in the urine.

As the chromophores alone possess antitumor activity, the effect of these antitumor proteins in cancer chemotherapy might be significantly increased by the administration of protein preparations containing biologically active and stable chromophores.

¹ Supported by American Cancer Society Grant CH-232.

² This paper is dedicated to the memory of our colleague, Hacer Ali Ozkazanci, D.V.M.

³ To whom requests for reprints should be addressed, at Department of Oncology, P. O. Box 016960 (R-71), University of Miami School of Medicine, Miami, FL 33101.

Received 8/ 5/83. Accepted 4/30/84.