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Transformation of verapamil by Cunninghamella blakesleeana.
Appl Environ Microbiol. 2004 May; 70(5):2722-7.AE

Abstract

A filamentous fungus, Cunninghamella blakesleeana AS 3.153, was used as a microbial model of mammalian metabolism to transform verapamil, a calcium channel antagonist. The metabolites of verapamil were separated and assayed by the liquid chromatography-ion trap mass spectrometry method. After 96 h of incubation, nearly 93% of the original drug was metabolized to 23 metabolites. Five major metabolites were isolated by semipreparative high-performance liquid chromatography and were identified by proton nuclear magnetic resonance and electrospray mass spectrometry. Other metabolites were characterized according to their chromatographic behavior and mass spectral data. The major metabolic pathways of verapamil transformation by the fungus were N dealkylation, O demethylation, and sulfate conjugation. The phase I metabolites of verapamil (introduction of a functional group) by C. blakesleeana paralleled those in mammals; therefore, C. blakesleeana could be a useful tool for generating the mammalian phase I metabolites of verapamil.

Authors+Show Affiliations

Laboratory of Drug Metabolism and Pharmacokinetics, Shenyang Pharmaceutical University, Shenyang 110016, People's Republic of China.No affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

15128524

Citation

Sun, Lu, et al. "Transformation of Verapamil By Cunninghamella Blakesleeana." Applied and Environmental Microbiology, vol. 70, no. 5, 2004, pp. 2722-7.
Sun L, Huang HH, Liu L, et al. Transformation of verapamil by Cunninghamella blakesleeana. Appl Environ Microbiol. 2004;70(5):2722-7.
Sun, L., Huang, H. H., Liu, L., & Zhong, D. F. (2004). Transformation of verapamil by Cunninghamella blakesleeana. Applied and Environmental Microbiology, 70(5), 2722-7.
Sun L, et al. Transformation of Verapamil By Cunninghamella Blakesleeana. Appl Environ Microbiol. 2004;70(5):2722-7. PubMed PMID: 15128524.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Transformation of verapamil by Cunninghamella blakesleeana. AU - Sun,Lu, AU - Huang,Hai-Hua, AU - Liu,Lei, AU - Zhong,Da-Fang, PY - 2004/5/7/pubmed PY - 2004/7/28/medline PY - 2004/5/7/entrez SP - 2722 EP - 7 JF - Applied and environmental microbiology JO - Appl. Environ. Microbiol. VL - 70 IS - 5 N2 - A filamentous fungus, Cunninghamella blakesleeana AS 3.153, was used as a microbial model of mammalian metabolism to transform verapamil, a calcium channel antagonist. The metabolites of verapamil were separated and assayed by the liquid chromatography-ion trap mass spectrometry method. After 96 h of incubation, nearly 93% of the original drug was metabolized to 23 metabolites. Five major metabolites were isolated by semipreparative high-performance liquid chromatography and were identified by proton nuclear magnetic resonance and electrospray mass spectrometry. Other metabolites were characterized according to their chromatographic behavior and mass spectral data. The major metabolic pathways of verapamil transformation by the fungus were N dealkylation, O demethylation, and sulfate conjugation. The phase I metabolites of verapamil (introduction of a functional group) by C. blakesleeana paralleled those in mammals; therefore, C. blakesleeana could be a useful tool for generating the mammalian phase I metabolites of verapamil. SN - 0099-2240 UR - https://www.unboundmedicine.com/medline/citation/15128524/Transformation_of_verapamil_by_Cunninghamella_blakesleeana_ L2 - http://aem.asm.org/cgi/pmidlookup?view=long&pmid=15128524 DB - PRIME DP - Unbound Medicine ER -