Intestinal Permeability of Sesquiterpenes in the Caco-2 Cell Monolayer Model

The intestinal permeability of eight sesquiterpenes which are active constituents of some traditional Chinese medicines, were studied by using the Caco-2 cell monolayer; they include tanacetin, artesin, magnolialide, crossostephin, atractylon, isocalamenediol (ICL), bisabolangelone (BSE) and (3R)-de...

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Bibliographic Details
Published in:Planta Medica
Main Authors: Wu, Qi, Zhao, Bo, Yang, Xiu-Wei, Xu, Wei, Zhang, Peng, Zou, Lei, Zhang, Lian-Xue
Other Authors: Yang, XW (reprint author), Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Dept Nat Med, 38 Xueyuan Rd, Beijing 100191, Peoples R China., Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Dept Nat Med, Beijing 100191, Peoples R China., Jilin Agr Univ, Coll Chinese Med Mat, Changchun, Peoples R China., Natl Pharmaceut R&D Co Ltd, Beijing, Peoples R China., Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Dept Nat Med, 38 Xueyuan Rd, Beijing 100191, Peoples R China.
Format: Journal/Newspaper
Language:English
Published: 药用植物 2010
Subjects:
sesquiterpenes
intestinal permeability
Caco-2 cell monolayer
ABSORPTION
TRANSPORT
CONSTITUENTS
INHIBITION
DML
Online Access:https://hdl.handle.net/20.500.11897/344775
https://doi.org/10.1055/s-0029-1186195
Description
Summary:The intestinal permeability of eight sesquiterpenes which are active constituents of some traditional Chinese medicines, were studied by using the Caco-2 cell monolayer; they include tanacetin, artesin, magnolialide, crossostephin, atractylon, isocalamenediol (ICL), bisabolangelone (BSE) and (3R)-des-O-methyllasiodiplodin (DML). The bidirectional permeability of the eight sesquiterpenes was studied from the apical (AP) side to the basolateral (BL) side or from the BL side to the AP side. The eight compounds were assayed by HPLC. Transport parameters and apparent permeability coefficients (P(app)) were then calculated. The bidirectional P(app) values of the eight compounds were compared with those of propranolol, a marker of high permeability and transcellular transport. The transport of the eight sesquiterpenes was concentration-dependent in the range of 10-200 mu M. Lower recoveries of ICL, BSE and DML than other sesquiterpenes were found during transport. The results indicated that all the sesquiterpenes are well absorbed mainly by the passive diffusion via the transcellular pathway and metabolism may be involved during the absorption of ICL, BSE and DML. Plant Sciences Chemistry, Medicinal Pharmacology & Pharmacy SCI(E) PubMed 4 ARTICLE 4 319-324 76

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