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Pharm Res. 1997 Oct;14(10):1449-54.

Biomimetic metabolism of artelinic acid by chemical cytochrome P-450 model systems.

Author information

1
Division of Experimental Therapeutics, Walter Reed Army Institute of Research, Washington, D.C. 20307-5100, USA. Dr._Remi_Idowu@wrsmtp-ccmail.army.mil

Abstract

PURPOSE:

To study the reaction of artelinic acid with chemical model systems of cytochrome P-450 as a means of obtaining authentic samples of the putative metabolites necessary for identification of the mammalian metabolites of artelinic acid.

METHODS:

Artelinic acid was reacted with different organic complexes of iron(II). The reaction products were isolated and characterized by NMR and thermospray mass spectroscopy.

RESULTS:

Five compounds which are putative metabolites of artelinic acid were isolated from these reactions and unambiguously identified, while the identity of two other compounds await final confirmation.

CONCLUSIONS:

Standards of possible metabolites of artelinic acid can be produced by the reaction of the compound with ferrous complexes that may simulate cytochrome P-450 catalyzed metabolism of xenobiotics. This approach may provide a simple and versatile method for the formation of metabolites of artemisinin compounds which is more advantageous than previous approaches with fungal-based systems.

PMID:
9358560
DOI:
10.1023/a:1012185124972
[Indexed for MEDLINE]

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