Binding of the Cain quinolinium, NSC 113089, to rat tissue lipid extracts.

Abstract

The binding characteristics of the cancer chemotherapeutic Cain's quinolinium 6-amino-1-ethyl-4-[p-[[p-[(1-ethylpyridinium-4-yl) amino] phenyl] carbamoyl]-anilino]-quinolinium dibromide (NSC 113089) to lipid extracts from rat kidney, liver, heart and skeletal muscle has been studied. Such binding is saturable with an apparent KD congruent to 1.6 microM. Drug binding to the lipid extracts is displaceable by spermine, spermidine, calcium ions and protons. Spermine is the best displacing agent, achieving half drug displacement from the lipid extracts at approximately 6.3 microM regardless of tissue. The inability of the displacing agents to displace all the NSC 113089 bound to the lipid extracts as well as differences in the amount of agent bound to as compared to amount of drug displaced from the lipid extracts indicate that a number of drug binding sites may be present in the lipid extracts. The similarities of drug binding by rat tissue lipids to similar lipids extracted from normal animal and tumor tissues is discussed.

• Authors: D W Yesair, M Callahan, M F McComish, R F Taylor
• Journal: Cancer biochemistry biophysics (Cancer Biochem Biophys) Vol. 3 Issue 4 Pg. 163-8 ( 1979) ISSN: 0305-7232 [Print] England
• PMID: 552904 (Publication Type: Journal Article, Research Support, U.S. Gov't, P.H.S.)

Chemical References

• Quinolinium Compounds
• Spermine
• Cain quinolinium
• Calcium
• Spermidine

Topics

• Animals
• Binding Sites
• Calcium (pharmacology)
• Female
• Kidney (metabolism)
• Kinetics
• Lipid Metabolism
• Liver (metabolism)
• Male
• Muscles (metabolism)
• Myocardium (metabolism)
• Quinolinium Compounds (metabolism)
• Rats
• Spermidine (pharmacology)
• Spermine (pharmacology)