Porphyrinogenic activity and ferrochelatase-inhibitory activity of sydnones in chick embryo liver cells

Autor: Sutherland, E.P., Marks, G.S., Grab, L.A., de Montellano, P.R.Ortiz
Zdroj: FEBS Letters; January 1986, Vol. 197 Issue: 1 p17-20, 4p
Abstrakt: 3-[2-(2,4,6-Trimethylphenyl)thioethyl]-4-methylsydnone was shown to be a potent porphyrinogenic agent in chick embryo liver cells. The accumulation of protoporphyrin IX was consistent with the finding that ferrochelatase activity was inhibited. 3-Benzyl-4-phenylsydnone did not inhibit ferrochelatase activity and protoporphyrin IX was found to constitute only a minor fraction of the porphyrins. These results support the idea that the porphyrinogenicity of 3-[2-(2,4,6-trimethylphenyl)thioethyl]-4-methylsydnone is due to its catalytic activation by cytochrome P-450 leading to heme alkylation and formation of N-vinylprotoporphyrin IX which inhibits ferrochelatase.
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