Grafakou, Maria-Eleni and Barda, Christina and Skaltsa, Helen and Heilmann, Joerg (2023) Study on the metabolism of natural sesquiterpene lactones in human liver microsomes using LC-Q-TOF-MS/MS. NATURAL PRODUCT RESEARCH. ISSN 1478-6419, 1478-6427
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Sesquiterpene lactones are naturally occurring, highly active specialised metabolites, which are biosynthesized by important medicinal plants, fulfilling many functions. The in vitro metabolism of parthenolide (1), grosheimin (2), carbetolide C (3), 8a-O(3,4-dihydroxy-methylenebutanoyloxy)- dehydromelitensin (4) and arteludovicinolide A (5) was examined using human liver microsomes. Phase I, phase II (glucuronidation), as well as combined phase I + II metabolism were studied. Metabolites were identified via liquid chromatography-high resolution quadrupole time-of-flight mass spectrometry. Monohydroxylated, hydrated, carboxylated, methylated derivatives, together with corresponding monoglucuronides were detected, suggesting that the metabolism of sesquiterpene lactones is changeable due to structural features and scaffold diversity, though the lactone ring is the main site of metabolism.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | PARTHENOLIDE; CONSTITUENTS; Sesquiterpene lactones; asteraceae; parthenolide; grosheimin; human liver microsomes; metabolism; LC-MS |
| Subjects: | 600 Technology > 615 Pharmacy |
| Divisions: | Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical Biology (Prof. Heilmann) |
| Depositing User: | Dr. Gernot Deinzer |
| Date Deposited: | 20 Mar 2024 06:03 |
| Last Modified: | 20 Mar 2024 06:03 |
| URI: | https://pred.uni-regensburg.de/id/eprint/59764 |
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