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Zheng X, Wang X, Ding Z, et al. Metabolic activation of deferiprone mediated by CYP2A6. Xenobiotica. 2021;51(11):1282-1291doi: 10.1080/00498254.2021.1931729.
Zheng, X., Wang, X., Ding, Z., Li, W., Peng, Y., & Zheng, J. (2021). Metabolic activation of deferiprone mediated by CYP2A6. Xenobiotica; the fate of foreign compounds in biological systems, 51(11), 1282-1291. https://doi.org/10.1080/00498254.2021.1931729
Zheng, Xiaojiao, et al. "Metabolic activation of deferiprone mediated by CYP2A6." Xenobiotica; the fate of foreign compounds in biological systems vol. 51,11 (2021): 1282-1291. doi: https://doi.org/10.1080/00498254.2021.1931729
Zheng X, Wang X, Ding Z, Li W, Peng Y, Zheng J. Metabolic activation of deferiprone mediated by CYP2A6. Xenobiotica. 2021 Nov;51(11):1282-1291. doi: 10.1080/00498254.2021.1931729. Epub 2021 Oct 28. PMID: 34006188.
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Xenobiotica. 2021 Nov;51(11):1282-1291. doi: 10.1080/00498254.2021.1931729. Epub 2021 Oct 28.

Metabolic activation of deferiprone mediated by CYP2A6.

Xenobiotica; the fate of foreign compounds in biological systems

Xiaojiao Zheng, Xu Wang, Zifang Ding, Wei Li, Ying Peng, Jiang Zheng

Affiliations

  1. Wuya College of Innovation, Shenyang Pharmaceutical University, Shenyang, P. R. China.
  2. State Key Laboratory of Functions and Applications of Medicinal Plants, Guizhou Provincial Key Laboratory of Pharmaceutics, Guizhou Medical University, Guiyang, P. R. China.
  3. Key Laboratory of Environmental Pollution, Monitoring and Disease Control, Ministry of Education, Guizhou Medical University, Guiyang, P. R. China.

PMID: 34006188 DOI: 10.1080/00498254.2021.1931729

Abstract

Deferiprone (DFP) is a metal chelating agent generally used to treat patients with thalassaemia, due to iron overload in clinical settings.Studies have revealed that long-term use of DFP can induce hepatotoxicity, however, mechanisms of its toxic action remain unclear. The present studies are aimed to characterize the reactive metabolite of DFP, to define the metabolic pathway, and to determine the P450 enzymes participating in the bioactivation.A demethylation metabolite (M1) was observed in rat liver microsomal incubations. Additionally, a glutathione (GSH) conjugate (M2) and an N-acetylcysteine (NAC) conjugate (M3) were detected in microsomal incubations fortified with DFP and GSH/NAC.Biliary M2 and urinary M3 were respectively found in animals administered DFP.CYP2A6 enzyme dominated the catalysis to bioactivate DFP.

Keywords: CYP2A6; Deferiprone; metabolic activation

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