Metabolism Analysis of Alantolactone and Isoalantolactone in Rats by Oral Administration

Abstract

Alantolactone and isoalantolactone are the major active ingredients of Inulae Radix. Their metabolism in vivo and in vitro was investigated by UPLC-Q-TOF-MS for the first time. As a result, nine metabolites in vivo including cysteine conjugates, oxidates, dehydrogenates, and hydrates were detected in rat bile after oral administration. The metabolites produced in vitro by incubation with rat liver microsomes were found to be substantially identical to those detected in vivo. However, no metabolites were detected in the samples of plasma, feces, and urine or in the incubates of gastric juice, intestinal juice, and intestinal bacteria. These results reveal that the liver is the main metabolic organ for alantolactone and isoalantolactone, and the first pass effect of the liver appears to be the reason for the low oral bioavailability of the two lactones.

Synthesis of EPD, an established cytotoxic agent for ovarian cancer cells, and its efficacy in cisplatin and paclitaxel resistant tumor cells

“…However, there is still a signi cant knowledge gap regarding the involved signalling pathways of sesquiterpene lactones [19]. EPD has also been compared with Isoalantolactone (IATL) [20], a sesquiterpene lactone of the eudesmanolide group (Specs, Zoetermeer, The Netherlands). In the dose response curves, much higher concentrations (almost twice as much) of IATL were necessary compared with EPD for cell death.…”