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Transport and metabolism of (+/-)-praeruptorin A in Caco-2 cell monolayers
Jing, W. H.1; Song, Y. L.1; Yan, R.1; Bi, H. C.1,2; Li, P. T.3; Wang, Y. T.1,4
Source PublicationXENOBIOTICA


(+/-)-Praeruptorin A (dl-PA) is one of the main pyranocoumarins of Peucedani Radix and the chemical marker for quality control of the herb in China. This study investigated the transport and metabolism of dl-PA, for the first time, in Caco-2 cell monolayers. 

PA enantiomers of dl-PA in the transport study were simultaneously determined using a simple and rapid enantio-selective high performance liquid chromatography-UV method. 

Both dextrorotatory (d-PA) and levorotatory (l-PA) enantiomers traversed Caco-2 monolayer rapidly in both directions (absorptive P(app): 2.01-3.03 x 10
PA enantiomers were incompletely recovered after the transport study. Nonspecific binding to the Transwell inserts, irreversible binding to cellular components and metabolism within the cells accounted for the loss. 

dl-PA was partially hydrolyzed in Caco-2 monolayers and yielded two stereoisomers via removal of the acetyl group from C-4' position. Both phenylmethylsulphonyl fluoride (a nonspecific esterase inhibitor) and bis(p-nitrophenyl) phosphate sodium salt (a specific inhibitor of carboxylesterases) completely abolished dl-PA hydrolysis. 

In summary, PA enantiomers were rapidly transported across Caco-2 cells and partially hydrolyzed by carboxylesterases during permeation. These findings provide mechanistic understanding of in vivo pharmacokinetic properties of dl-PA.

KeywordIntestinal-absorption Gene-expression Drug Transport Human Liver Permeability Carboxylesterases Enantiomers Ester
URLView the original
WOS Research AreaPharmacology & Pharmacy ; Toxicology
WOS SubjectPharmacology & Pharmacy ; Toxicology
WOS IDWOS:000285196500007
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Cited Times [WOS]:18   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionInstitute of Chinese Medical Sciences
Affiliation1.Univ Macau, Inst Chinese Med Sci, Taipa, Peoples R China
2.Sun Yat Sen Univ, Sch Pharmaceut Sci, Inst Clin Pharmacol, Guangzhou 510275, Guangdong, Peoples R China
3.Beijing Univ Chinese Med, Dongzhimen Hosp, Beijing, Peoples R China
4.Beijing Univ Chinese Med, Sch Chinese Mat Med, Beijing, Peoples R China
First Author AffilicationUniversity of Macau
Recommended Citation
GB/T 7714
Jing, W. H.,Song, Y. L.,Yan, R.,et al. Transport and metabolism of (+/-)-praeruptorin A in Caco-2 cell monolayers[J]. XENOBIOTICA,2011,41(1):71-81.
APA Jing, W. H.,Song, Y. L.,Yan, R.,Bi, H. C.,Li, P. T.,&Wang, Y. T..(2011).Transport and metabolism of (+/-)-praeruptorin A in Caco-2 cell monolayers.XENOBIOTICA,41(1),71-81.
MLA Jing, W. H.,et al."Transport and metabolism of (+/-)-praeruptorin A in Caco-2 cell monolayers".XENOBIOTICA 41.1(2011):71-81.
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