Please use this identifier to cite or link to this item: https://doi.org/10.1016/j.jpba.2009.04.022
DC FieldValue
dc.titlePharmacokinetics of prenylflavonoids and correlations with the dynamics of estrogen action in sera following ingestion of a standardized Epimedium extract
dc.contributor.authorWong, S.P.
dc.contributor.authorShen, P.
dc.contributor.authorLee, L.
dc.contributor.authorLi, J.
dc.contributor.authorYong, E.L.
dc.date.accessioned2011-09-15T08:21:36Z
dc.date.available2011-09-15T08:21:36Z
dc.date.issued2009
dc.identifier.citationWong, S.P., Shen, P., Lee, L., Li, J., Yong, E.L. (2009). Pharmacokinetics of prenylflavonoids and correlations with the dynamics of estrogen action in sera following ingestion of a standardized Epimedium extract. Journal of Pharmaceutical and Biomedical Analysis 50 (2) : 216-223. ScholarBank@NUS Repository. https://doi.org/10.1016/j.jpba.2009.04.022
dc.identifier.issn07317085
dc.identifier.urihttp://scholarbank.nus.edu.sg/handle/10635/25984
dc.description.abstractTo explore pharmacokinetic properties of prenylflavonoids from the Traditional Chinese Medicinal plant Epimedium, three doses of a standardized extract (100, 300 and 600 mg/kg body weight), were administered to ovariectomized rats and serial blood samples were obtained. Serum concentrations of the Epimedium prenylflavonoids icariin, icariside I, icariside II, icaritin and desmethylicaritin were determined by LC-MS/MS. Aliquots of sera were also applied to human cell lines that permanently express ERα and ERβ proteins for the ex vivo measurement of estrogenic activity. All five prenylflavonoids exhibit non-linear dose-dependent increases in the area under concentration versus time curves. Two distinct pharmacokinetic patterns were evident, an early phase wherein icariin and icariside II reached tmax 0.5-1 h, and a late phase wherein icariside I, icaritin and desmethylicaritin peaked at tmax 8 h. Total concentrations of icaritin and desmethylicaritin reached Cmax ∼2 μM and ∼0.25 μM respectively. Estrogenic activity in Epimedium-treated rat sera lagged by several hours compared to animals treated with control drug estradiol benzoate, corresponding to the appearance of bioactive metabolites desmethylicaritin, icaritin and icariside I. Following glucuronidase/sulphatase treatment, prolonged estrogenic activity at higher Epimedium doses (300 and 600 mg/kg of body weight) was evident, and correlated with the persistence of micromolar levels of icaritin at the 48-72 h sampling period. The depot effect resulted in time-concentration bioactivity profiles at the three Epimedium doses (area under curve 374, 543, and 771 pM E2 h-1) that exceeded that observed for estradiol benzoate (148 pM E2 h-1). Our study correlated the pharmacokinetics of prenylflavonoids with the dynamics of their estrogenic effects and reveals the potential estrogenicity of this Epimedium extract. This study may aid the development of prenylflavonoids as drugs for menopause and other conditions requiring estrogenic action. © 2009 Elsevier B.V. All rights reserved.
dc.description.urihttp://libproxy1.nus.edu.sg/login?url=http://dx.doi.org/10.1016/j.jpba.2009.04.022
dc.sourceScopus
dc.subjectEpimedium
dc.subjectEstrogen-responsive bioassay
dc.subjectLC-MS/MS
dc.subjectPharmacodynamics
dc.subjectPharmacokinetics
dc.subjectPrenylflavonoids
dc.typeArticle
dc.contributor.departmentOBSTETRICS & GYNAECOLOGY
dc.description.doi10.1016/j.jpba.2009.04.022
dc.description.sourcetitleJournal of Pharmaceutical and Biomedical Analysis
dc.description.volume50
dc.description.issue2
dc.description.page216-223
dc.identifier.isiut000267037700016
Appears in Collections:Staff Publications

Show simple item record
Files in This Item:
There are no files associated with this item.

SCOPUSTM   
Citations

52
checked on May 21, 2019

WEB OF SCIENCETM
Citations

52
checked on May 13, 2019

Page view(s)

173
checked on May 12, 2019

Google ScholarTM

Check

Altmetric


Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.