Intestinal permeability of antivirus constituents from the fruits of Eucalyptus globulus Labill. in Caco-2 Cell Model.
The uptake and transepithelial transport of the three main constituents macrocarpal A (M-A), macrocarpal B (M-B), and cypellocarpa C (Cy-C) from the fruits of Eucalyptus globulus Labill. were investigated. Monolayers of the human intestinal epithelial cancer cell line Caco-2 were incubated with M-A, M-B, and Cy-C to model its intestinal absorption and transport, respectively. The determination of compounds was performed by HPLC. The apparent permeability coefficients (P(app)) for M-A, M-B, and Cy-C in the apical-to-basolateral direction of a Caco-2 monolayer were (1.70+/-0.06)x10(-6), (1.99+/-0.10)x10(-6), and (6.08+/-0.41)x10(-6)cm/s, respectively. In the presence of iodoacetamide, the P(app) of Cy-C were both reducted in apical-to-basolateral and basolateral-to-apical directions. M-A and M-B appear to accumulate in the epithelial cells. The intestinal absorption of M-A, M-B, and Cy-C was passive diffusion as the dominating process and Cy-C was partly ATP-dependent.
Yang
Xiu-wei
XW
State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Beijing 100083, PR China. xwyang@bjmu.edu.cn
Guo
Qing-mei
QM
Wang
Ying
Y
Xu
Wei
W
Tian
Li
L
Tian
Xiao-juan
XJ
D000477:Alkylating Agents / Q000737:chemistry; D000998:Antiviral Agents / Q000302:isolation & purification / Q000493:pharmacokinetics*; D001682:Biological Availability; D018938:Caco-2 Cells; D002121:Calcium Channel Blockers / Q000494:pharmacology; D002462:Cell Membrane / Q000378:metabolism; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D002851:Chromatography, High Pressure Liquid; D005052:Eucalyptus / Q000737:chemistry*; D005638:Fruit / Q000737:chemistry*; D006801:Humans; D007408:Intestinal Absorption; D007460:Iodoacetamide / Q000494:pharmacology; D010696:Phloroglucinol / Q000031:analogs & derivatives / Q000737:chemistry / Q000493:pharmacokinetics; D011422:Propionates / Q000494:pharmacology; D011804:Quinolines / Q000494:pharmacology; D012717:Sesquiterpenes / Q000737:chemistry / Q000493:pharmacokinetics; D014700:Verapamil / Q000494:pharmacology
D000477:Alkylating Agents; D000998:Antiviral Agents; D002121:Calcium Channel Blockers; D011422:Propionates; D011804:Quinolines; D012717:Sesquiterpenes; C518771:macrocarpal A; C518772:macrocarpal B; C518773:macrocarpal C; C059141:verlukast; D014700:Verapamil; D010696:Phloroglucinol; D007460:Iodoacetamide