Metabolism Analysis of Alantolactone and Isoalantolactone in Rats by Oral Administration

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 i...

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Main Authors: Mengyue Wang, Renjie Xu, Ying Peng, Xiaobo Li
Format: Article
Language:English
Published: Wiley 2018-01-01
Series:Journal of Chemistry
Online Access:http://dx.doi.org/10.1155/2018/2026357
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author Mengyue Wang
Renjie Xu
Ying Peng
Xiaobo Li
author_facet Mengyue Wang
Renjie Xu
Ying Peng
Xiaobo Li
author_sort Mengyue Wang
collection DOAJ
description 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.
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publishDate 2018-01-01
publisher Wiley
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series Journal of Chemistry
spelling doaj-art-8883096129d94a59ba86a75e89b94cc22025-02-03T06:13:50ZengWileyJournal of Chemistry2090-90632090-90712018-01-01201810.1155/2018/20263572026357Metabolism Analysis of Alantolactone and Isoalantolactone in Rats by Oral AdministrationMengyue Wang0Renjie Xu1Ying Peng2Xiaobo Li3School of Pharmacy, Shanghai Jiao Tong University, Shanghai 200240, ChinaSchool of Pharmacy, Shanghai Jiao Tong University, Shanghai 200240, ChinaSchool of Pharmacy, Shanghai Jiao Tong University, Shanghai 200240, ChinaSchool of Pharmacy, Shanghai Jiao Tong University, Shanghai 200240, ChinaAlantolactone 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.http://dx.doi.org/10.1155/2018/2026357
spellingShingle Mengyue Wang
Renjie Xu
Ying Peng
Xiaobo Li
Metabolism Analysis of Alantolactone and Isoalantolactone in Rats by Oral Administration
Journal of Chemistry
title Metabolism Analysis of Alantolactone and Isoalantolactone in Rats by Oral Administration
title_full Metabolism Analysis of Alantolactone and Isoalantolactone in Rats by Oral Administration
title_fullStr Metabolism Analysis of Alantolactone and Isoalantolactone in Rats by Oral Administration
title_full_unstemmed Metabolism Analysis of Alantolactone and Isoalantolactone in Rats by Oral Administration
title_short Metabolism Analysis of Alantolactone and Isoalantolactone in Rats by Oral Administration
title_sort metabolism analysis of alantolactone and isoalantolactone in rats by oral administration
url http://dx.doi.org/10.1155/2018/2026357
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AT renjiexu metabolismanalysisofalantolactoneandisoalantolactoneinratsbyoraladministration
AT yingpeng metabolismanalysisofalantolactoneandisoalantolactoneinratsbyoraladministration
AT xiaoboli metabolismanalysisofalantolactoneandisoalantolactoneinratsbyoraladministration