title: Structure elucidation and thermospray high-performance liquid chromatography/mass spectroscopy (HPLC/MS) of the microbial and mammalian metabolites of the antimalarial arteether.
abstract: Microbial metabolism studies of the antimalarial drug arteether (1) have shown that arteether is metabolized to six new metabolites in addition to those previously reported (3). Large-scale fermentations with Cunninghamella elegans (ATCC 9245) and Streptomyces lavendulae (L-105) have resulted in the characterization of these metabolites primarily by two-dimensional nuclear magnetic resonance (2D-NMR) methods as 9 beta-hydroxyarteether (2), a ring rearrangement metabolite (3), 3 alpha-hydroxy-11-epi-deoxydihydroartemisinin (4), 9 alpha-hydroxyarteether (5), 2 alpha-hydroxyarteether (6), and 14-hydroxyarteether (7). Thermospray mass spectroscopy/high-performance liquid chromatographic analyses have shown that four of these metabolites (2, 5, 6, 7) are also present in rat liver microsome preparations.
authors.affiliation: Department of Pharmacognosy, School of Pharmacy, University of Mississippi, University 38677.
authors.forename: C D
authors.initials: CD
authors.lastname: Hufford
authors.forename: I S
authors.initials: IS
authors.lastname: Lee
authors.forename: H N
authors.initials: HN
authors.lastname: ElSohly
authors.forename: H T
authors.initials: HT
authors.lastname: Chi
authors.forename: J K
authors.initials: JK
authors.lastname: Baker
mesh_terms: D000818:Animals; D000962:Antimalarials / Q000378:metabolism*; D037621:Artemisinins; D002851:Chromatography, High Pressure Liquid; D005285:Fermentation; D013058:Mass Spectrometry; D008862:Microsomes, Liver / Q000378:metabolism; D009090:Mucorales / Q000378:metabolism; D051381:Rats; D012717:Sesquiterpenes / Q000378:metabolism*; D013302:Streptomyces / Q000378:metabolism
chemical_list: D000962:Antimalarials; D037621:Artemisinins; D012717:Sesquiterpenes; C055141:artemotil