Investigation of intestinal absorption and disposition of green tea catechins by Caco-2 monolayer model

被引：160

作者：

Zhang, L ^{[1
]}

Zheng, Y ^{[1
]}

Chow, MSS ^{[1
]}

Zuo, Z ^{[1
]}

机构：

[1] Chinese Univ Hong Kong, Sch Pharm, Fac Med, Shatin, Hong Kong, Peoples R China

来源：

INTERNATIONAL JOURNAL OF PHARMACEUTICS | 2004年 / 287卷 / 1-2期

关键词：

green tea catechins; caco-2; cells; efflux; absorption; metabolism;

D O I：

10.1016/j.ijpharm.2004.08.020

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

The current study was designed to investigate the absorption mechanism and identify the possible disposition pathways of green tea catechins (GTC), including epicatechin (EC), epigallocatechin (EGC), epicatechin gallate (ECG) and epigallocatechin gallate (EGCG), during their absorption across small intestine by Caco-2 monolayer model. The transport of each GTC from both apical to basolateral and basolateral to apical directions was measured in the absence and the presence of MK571, an MRP inhibitor. HPLC and LC/MS were employed to identify the possible metabolites of the four GTC formed during their bidirectional transport processes. The results indicated that the four GTC showed limited transepitheliat absorption with relatively small P,pp values. However, significant efflux mediated by MRP was observed during the secretion of GTC, especially the non-gallated catechins. Methylation and sulfation were the main biotransformation pathways of GTC during their secretion transport and the efflux of the related metabolites seem to be mediated by MRP. (C) 2004 Elsevier B.V. All rights reserved.

引用

页码：1 / 12

页数：12

共 32 条

[1] Isoflavones from Tofu are absorbed and metabolized in the isolated rat small intestine [J].

Andlauer, W ;

Kolb, J ;

Fürst, P .

JOURNAL OF NUTRITION, 2000, 130 (12) :3021-3027

[2] CORRELATION BETWEEN ORAL-DRUG ABSORPTION IN HUMANS AND APPARENT DRUG PERMEABILITY COEFFICIENTS IN HUMAN INTESTINAL EPITHELIAL (CACO-2) CELLS [J].

ARTURSSON, P ;

KARLSSON, J .

BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 1991, 175 (03) :880-885

[3] In vivo comparison of the bioavailability of (+)-catechin, (-)-epicatechin and their mixture in orally administered rats [J].

Baba, S ;

Osakabe, N ;

Natsume, M ;

Muto, Y ;

Takizawa, T ;

Terao, J .

JOURNAL OF NUTRITION, 2001, 131 (11) :2885-2891

[4]

Chen LS, 1997, DRUG METAB DISPOS, V25, P1045

[5] Stabilizing effect of ascorbic acid on green tea catechins [J].

Chen, ZY ;

Zhu, QY ;

Wong, YF ;

Zhang, ZS ;

Chung, HY .

JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY, 1998, 46 (07) :2512-2516

[6] Part of quercetin absorbed in the small intestine is conjugated and further secreted in the intestinal lumen [J].

Crespy, V ;

Morand, C ;

Manach, C ;

Besson, C ;

Demigne, C ;

Remesy, C .

AMERICAN JOURNAL OF PHYSIOLOGY-GASTROINTESTINAL AND LIVER PHYSIOLOGY, 1999, 277 (01) :G120-G126

[7] Effect of acute and chronic tea consumption on platelet aggregation in patients with coronary artery disease [J].

Duffy, SJ ;

Vita, JA ;

Holbrook, M ;

Swerdloff, PL ;

Keaney, JF .

ARTERIOSCLEROSIS THROMBOSIS AND VASCULAR BIOLOGY, 2001, 21 (06) :1084-1089

[8]

Eagling VA, 1999, BRIT J CLIN PHARMACO, V48, P543, DOI 10.1046/j.1365-2125.1999.00052.x

[9] Caco-2 permeability, P-glycoprotein transport ratios and brain penetration of heterocyclic drugs [J].

Faasen, F ;

Vogel, G ;

Spanings, H ;

Vromans, H .

INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2003, 263 (1-2) :113-122

[10] Identification of the major antioxidative metabolites in biological fluids of the rat with ingested (+)-catechin and (-)-epicatechin [J].

Harada, M ;

Kan, Y ;

Naoki, H ;

Fukui, Y ;

Kageyama, N ;

Nakai, M ;

Miki, W ;

Kiso, Y .

BIOSCIENCE BIOTECHNOLOGY AND BIOCHEMISTRY, 1999, 63 (06) :973-977

← 1 2 3 4 →