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Updated: Aug 18, 2026

Mass Spectrometry and Luminogenic-based Approaches to Characterize Phase I Metabolic Competency of In Vitro Cell Cultures
Published on: March 28, 2017
[Metabolism of bicyclol in rat and human liver microsomes in vitro]
1Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.
Aim:
To study the drug metabolizing enzymes involved in the metabolism of bicyclol and identify the major metabolites of bicyclol in rat and human liver microsomes.
Methods:
Bicyclol was incubated with rat and human liver microsomes. The metabolites of bicyclol were isolated by HPLC and identified by MS and 1H NMR.
Results:
The metabolic rate of bicyclol in DEX-induced rat liver microsomes was obviously higher than that in untreated microsomes, while it was much lower in human liver microsomes. Ketoconazole was capable to exhibit strong inhibition ( >90%) on bicyclol metabolism. Two metabolites of bicyclol were identified to be 4-hydroxy-4'-methoxy-6-hydroxy-methyl-6 '-methoxycarbonyl-2,3,2',3'-bis (methylene-dioxy) biphenyl and 4-methoxy-4'-hydroxy-6-hydroxymethyl-6'-methoxycarbonyl-2,3,2',3'-bis (methylene-dioxy) biphenyl.
Conclusion:
CYP3A was considered as the major catalyst involved in bicyclol metabolism in vitro and two metabolites of bicyclol in rats were identified as 4-hydroxy-4'-methoxy-6-hydroxy-methyl-6 '-methoxycarbonyl-2,3,2',3'-bis (methylene-dioxy) biphenyl and 4-methoxy-4'-hydroxy-6-hydroxymethyl-6'-methoxycarbonyl-2,3,2',3'-bis (methylenedioxy) biphenyl.
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