Biotransformation of metoprolol by the fungus Cunninghamella blakesleeana

Bin Ma, Hai Hua Huang, Xiao Yan Chen, Yu Ming Sun, Li Hong Lin, Da Fang Zhong

Research output: Contribution to journalArticlepeer-review

21 Scopus citations

Abstract

Aim: To investigate the biotransformation of metoprolol, a β1-cardioselective adrenoceptor antagonist, by filamentous fungus, and to compare the parallels between microbial transformation and mammalian metabolism. Methods: Five strains of Cunninghamella (Celegans AS 3.156, Celegans AS 3.2028, C echinulata AS 3.2004, C blakesleeana AS 3.153 and AS 3.910) were screened for the ability to transform metoprolol. The metabolites of metoprolol produced by C blakesleeana AS 3.153 were separated and assayed by liquid chromatography-tandem mass spectrometry (LC/MSn). The major metabolites were isolated by semipreparative HPLC and the structures were identified by a combination of LC/MSn and nuclear magnetic resonance analysis. Results: Metoprolol was transformed to 7 metabolites; 2 were identified as new metabolites and 5 were known metabolites in mammals. Conclusion: The microbial transformation of metoprolol was similar to the metabolism in mammals. The fungi belonging to Cunninghamella species could be used as complementary models for predicting in vivo metabolism and producing quantities of metabolite references for drugs like metoprolol.

Original languageEnglish (US)
Pages (from-to)1067-1074
Number of pages8
JournalActa Pharmacologica Sinica
Volume28
Issue number7
DOIs
StatePublished - Jul 2007

Keywords

  • Biotransformation
  • Cun-ninghamella blakesleeana
  • Liquid chromatography-tandem mass spectrometry
  • Metoprolol

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