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Biotransformation of metoprolol by the fungus Cunninghamella blakesleeana.
Acta Pharmacol Sin. 2007 Jul; 28(7):1067-74.AP

Abstract

AIM

To investigate the biotransformation of metoprolol, a beta1-cardioselective adrenoceptor antagonist, by filamentous fungus, and to compare the parallels between microbial transformation and mammalian metabolism.

METHODS

Five strains of Cunninghamella (C elegans AS 3.156, C elegans 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/MS(n)). The major metabolites were isolated by semipreparative HPLC and the structures were identified by a combination of LC/MS(n) 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.

Authors+Show Affiliations

Center for Drug Metabolism and Pharmacokinetics Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article

Language

eng

PubMed ID

17588344

Citation

Ma, Bin, et al. "Biotransformation of Metoprolol By the Fungus Cunninghamella Blakesleeana." Acta Pharmacologica Sinica, vol. 28, no. 7, 2007, pp. 1067-74.
Ma B, Huang HH, Chen XY, et al. Biotransformation of metoprolol by the fungus Cunninghamella blakesleeana. Acta Pharmacol Sin. 2007;28(7):1067-74.
Ma, B., Huang, H. H., Chen, X. Y., Sun, Y. M., Lin, L. H., & Zhong, D. F. (2007). Biotransformation of metoprolol by the fungus Cunninghamella blakesleeana. Acta Pharmacologica Sinica, 28(7), 1067-74.
Ma B, et al. Biotransformation of Metoprolol By the Fungus Cunninghamella Blakesleeana. Acta Pharmacol Sin. 2007;28(7):1067-74. PubMed PMID: 17588344.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Biotransformation of metoprolol by the fungus Cunninghamella blakesleeana. AU - Ma,Bin, AU - Huang,Hai-hua, AU - Chen,Xiao-yan, AU - Sun,Yu-ming, AU - Lin,Li-hong, AU - Zhong,Da-fang, PY - 2007/6/26/pubmed PY - 2009/4/21/medline PY - 2007/6/26/entrez SP - 1067 EP - 74 JF - Acta pharmacologica Sinica JO - Acta Pharmacol. Sin. VL - 28 IS - 7 N2 - AIM: To investigate the biotransformation of metoprolol, a beta1-cardioselective adrenoceptor antagonist, by filamentous fungus, and to compare the parallels between microbial transformation and mammalian metabolism. METHODS: Five strains of Cunninghamella (C elegans AS 3.156, C elegans 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/MS(n)). The major metabolites were isolated by semipreparative HPLC and the structures were identified by a combination of LC/MS(n) 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. SN - 1671-4083 UR - https://www.unboundmedicine.com/medline/citation/17588344/Biotransformation_of_metoprolol_by_the_fungus_Cunninghamella_blakesleeana_ L2 - http://dx.doi.org/10.1111/j.1745-7254.2007.00567.x DB - PRIME DP - Unbound Medicine ER -