Department of Pharmaceutical Biology, Faculty of Pharmacy and Chemistry, University of Regensburg, Regensburg, Germany.
Department of Pharmacognosy and Chemistry of Natural Products, Faculty of Pharmacy, School of Health Sciences, National and Kapodistrian University of Athens, Athens, Greece.
Nat Prod Res. 2024 Jun;38(11):1855-1863. doi: 10.1080/14786419.2023.2226301. Epub 2023 Jun 24.
Sesquiterpene lactones are naturally occurring, highly active -specialised metabolites, which are biosynthesized by important medicinal plants, fulfilling many functions. The metabolism of parthenolide (), grosheimin (), carbetolide C (), 8-O-(3,4-dihydroxy--methylenebutanoyloxy)-dehydromelitensin () and arteludovicinolide A () was examined using human liver microsomes. Phase , phase (glucuronidation), as well as combined phase + metabolism were studied. Metabolites were identified 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.
倍半萜内酯是天然存在的、高度活跃的特殊代谢物,由重要的药用植物生物合成,具有多种功能。用人肝微粒体研究了小白菊内酯 (), 大根香叶烯二醇 (), 卡贝醇 C (), 8-O-(3,4-二羟基-亚甲基丁酰氧基)-脱水千里光菲灵 () 和阿替柳多威醇 A () 的代谢。研究了相 (), 相 (葡萄糖醛酸化), 以及相 + 联合代谢。通过液相色谱-高分辨四极杆飞行时间质谱联用技术鉴定了代谢产物。检测到单羟基化、水合、羧化、甲基化衍生物,以及相应的单葡萄糖醛酸苷,这表明倍半萜内酯的代谢由于结构特征和支架多样性而变化,尽管内酯环是主要的代谢部位。