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Chemical Compound Review:

Benzaron (2-ethylbenzofuran-3-yl)-(4...

Synonyms: Fragivil, Fragivix, Benzarona, Benzarone, Fagivil, ...

de Vries, J.X. et al., Kaufmann, P. et al., Filipovic, I. et al., Hautekeete, M.L. et al., Gehenot, M. et al., et al.

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Disease relevance of Fragivix

Chronic active hepatitis caused by benzarone [1].
Our cases constitute the most severe cases of benzarone hepatotoxicity reported so far, and comprise the first cases of (sub)fulminant hepatitis and cirrhosis related to benzarone [2].

High impact information on Fragivix

In isolated rat hepatocytes, amiodarone, benzarone, and benzbromarone (20 micromol/L) decreased mitochondrial membrane potential by 23%, 54% or 81%, respectively [3].
At the same concentrations, amiodarone, benzarone, and benzbromarone induced apoptosis and necrosis of isolated rat hepatocytes [3].
Enzymatic hydrolysis of plasma with pure beta-glucuronidase or arylsulphatase showed that the relative amounts of unconjugated, glucuronidated, and sulphated benzarone were 6, 12 and 82% respectively, for both plasma and urine [4].
In cultured human arterial smooth muscle cells 0.03 mmol/l benzarone stimulates the incorporation of [14C]-acetate and [3H]-palmitate into the cellular lipids while the receptor mediated uptake of homologous low-density lipoproteins (LDL) by the cells and their release are not influenced [5].

Analytical, diagnostic and therapeutic context of Fragivix

Subfulminant hepatitis requiring liver transplantation after benzarone administration [6].
Determination of benzarone in human plasma and urine by high-performance liquid chromatography and gas chromatography-mass spectrometry. Identification of the conjugates [4].

References

Chronic active hepatitis caused by benzarone. Babany, G., Larrey, D., Pessayre, D., Degott, C., Rueff, B., Benhamou, J.P. J. Hepatol. (1987) [Pubmed]
Severe hepatotoxicity related to benzarone: a report of three cases with two fatalities. Hautekeete, M.L., Henrion, J., Naegels, S., DeNeve, A., Adler, M., Deprez, C., Devis, G., Klöppel, G. Liver (1995) [Pubmed]
Mechanisms of benzarone and benzbromarone-induced hepatic toxicity. Kaufmann, P., Török, M., Hänni, A., Roberts, P., Gasser, R., Krähenbühl, S. Hepatology (2005) [Pubmed]
Determination of benzarone in human plasma and urine by high-performance liquid chromatography and gas chromatography-mass spectrometry. Identification of the conjugates. de Vries, J.X., Walter-Sack, I., van de Loo, A., Kocher, J. J. Chromatogr. (1986) [Pubmed]
The effect of 2-ethyl-3-(4-hydroxybenzoyl)-benzofuran (benzarone) on the metabolism of arterial tissue and cultured arterial smooth muscle cells. Filipovic, I., Buddecke, E. Arzneimittel-Forschung. (1979) [Pubmed]
Subfulminant hepatitis requiring liver transplantation after benzarone administration. Gehenot, M., Horsmans, Y., Rahier, J., Geubel, A.P. J. Hepatol. (1994) [Pubmed]

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