Establishment of Caco-2 cell monolayer model and standard operation procedure for assessing intestinal absorption of chemical components of traditional Chinese medicine

Journal of Chinese Integrative Medicine

Volumn 5, Issue 6, 2007, Pages 634-641

  Yang, Xiu Wei ^a   Yang, Xiao Da ^a   Wang, Ying ^a   Ma, Lian ^a   Zhang, Yue ^a   Yang, Xiao Gai ^a   Wang, Kui ^a  

^a PEKING UNIVERSITY HEALTH SCIENCE CENTER   (China)

Author keywords

Biological transport; Caco 2 cells; Chinese herbal drugs; Intestinal absorption

Indexed keywords

ALKALINE PHOSPHATASE; ATENOLOL; CHINESE DRUG; PROPRANOLOL;

ARTICLE; CANCER CELL CULTURE; CELL DIFFERENTIATION; CELL MEMBRANE PERMEABILITY; CELL STRAIN CACO 2; CELL STRUCTURE; CELL TRANSPORT; CHEMICAL COMPOSITION; CHINESE MEDICINE; COLON ADENOCARCINOMA; DRUG ABSORPTION; ELECTRIC RESISTANCE; ENZYME ACTIVITY; HUMAN; HUMAN CELL; IN VITRO STUDY; INTESTINE ABSORPTION; MONOLAYER CULTURE; PROTEIN EXPRESSION; SCANNING ELECTRON MICROSCOPY;

BIOLOGICAL TRANSPORT; CACO-2 CELLS; CELL MEMBRANE PERMEABILITY; DRUGS, CHINESE HERBAL; FLAVONOIDS; HUMANS; INTESTINAL ABSORPTION; MODELS, BIOLOGICAL;

EID: 36549063536     PISSN: 16721977     EISSN: None     Source Type: Journal    
DOI: 10.3736/jcim20070607     Document Type: Article

References (33)

1. Yang XW. Discovery strategy for effective and active constituents of Chinese material medica based on the processes of metabolism and disposition in intra-body. Zhongguo Zhong Yao Za Zhi. 2007; 32(5): 365-370. Chinese with abstract in English.
2. Yang XW. Discovery strategy for toxic-invited constituents and toxic-effective substances on Chinese material medica based on the processes of metabolism and disposition in intra-body. Zhonghua Zhong Yi Yao Za Zhi. 2007; 22(2): 67-72. Chinese with abstract in English.
3. Yang XW. Key foundational science problem in experimental medicine study of Chinese materia medica: ascertainment of active and toxic constituents in Chinese materia medica. Zhong Xi Yi Jie He Xue Bao. 2005; 3 (2): 154-159. Chinese with abstract in English.
4. Yang XW. Relationship between confirmation of Chinese materia medica bioactive constituents and intra-intestinal and intra-hepatic behavior of Chinese materia medica active constituents. Zhong Cao Yao. 2004; 35 (Suppl): 1-5. Chinese.
5. Yang XW, Hao MR, Hattori M. Metabolite analysis for chemical constituents of traditional Chinese medicines. Beijing: China Medical-Pharmaceutical Science & Technology Publishing House. 2003. Chinese.
6. Zhou X. Study on in vitro models of drug absorption. Zhongguo Lin Chuang Yao Li Xue Yu Zhi Liao Xue. 2006; 11 (4): 379-384. Chinese with abstract in English.
7. Turowski GA, Rashid Z, Hong F, et al. Glutamine modulates phenotype and stimulates proliferation in human colon cancer cell lines. Cancer Res. 1994; 54 (22): 5974-5980.
8. Rashid Z, Basson MD. Topoisomerase II inhibition differentially modulates Caco-2 intestinal epithelial cell phenotype. Biochem Biophy Res Comm. 1996; 219(1): 82-88.
9. Yee SY. In vitro permeability across Caco-2 cells (colonic) can predict in vivo (small intestinal) absorption in man-fact or myth. Pharm Res. 1997; 14 (6): 763-766.
10. Chong S, Dando SA, Morrison RA. Evaluation of biocoat intestinal epithelium differentiation environment (3-day cultured Caco-2 cells) as an absorption screening model with improved productivity. Pharm Res. 1997; 14(12): 1835-1837.
11. Gao JN, Hugger ED, Beck-Westermeyer MS, et al. Estimating intestinal mucosal permeation of compounds using Caco-2 cell monolayer. In: Enna SJ. Current Protocols in Pharmacology. Chichester: John Wiley & Sons Inc. 2000: 7.2.1-7.2.23.
12. Walle UK, French KL, Walgren RA, et al. Transport of genistein-7-glucoside by human intestinal Caco-2 cells: Potential role for MRP2. Res Commun Mol Pathol Pharmacol. 1999; 103(1): 45-56
13. Tian XJ, Yang XD, Wang K, et al. The efflux of flavonoids morin, isorhamnetin-3-O-rutinoside and diosmetin-7-O-beta-D-xylopyranosyl-(1-6)-beta-D-glucopyranoside in the human intestinal cell line Caco-2. Pharm Res. 2006; 23(8): 1721-1728.
14. Yang XW, Guo QM, Wang Y, et al. Intestinal permeability of antivirus constituents from the fruits of Eucalyptus globulus Labill. in Caco-2 cell model. Bioorg Med Chem Lett. 2007; 17(4): 1107-1111.
15. Tian L, Yang XW, Wang Y, et al. Characteristics of uptake, transport and efflux of Z- and E-ajoenes in Caco-2 cell monolayers in vitro. Yao Xue Xue Bao. 2007; 42(1): 87-92. Chinese with abstract in English.
16. Yang XG, Yuan Lan, Wang K, et al. Comparison of intestinal absorption of two insulinmimic vanadyl complexes using Caco-2 monolayers as model system. Chin Sci Bull. 2003; 48(9): 876-881.
17. Zhang Y, Yang XD, Wang K, et al. The permeability and cytotoxicity of insulin-mimetic vanadium (III, IV, V)-dipicolinate complexes. J Inorg Biochem. 2006; 100 (1): 80-87.
18. Bohets H, Annaert P, Mannens G, et al. Strategies for absorption screening in drug discovery and development. Curr Top Med Chem. 2001; 1(5): 367-383.
19. Zhang ZQ, Lu B. Current advance on oral colon-specific drug delivery system. Zhongguo Yao Xue Za Zhi. 2000; 35(1): 221-223. Chinese.
20. Komura H, Shigemoto Y, Kawahara I, et al. High throughput screening of pharmacokinetics and metabolism in drug discovery (III) - investigation on in-silico model for membrane permeability and CYP1A2 inhibition. Yakugaku Zasshi. 2005; 125(1): 141-147.
21. 2+ across the model of Caco-2 cell monolayers. Baotou Yi Xue Yuan Xue Bao. 2006; 22(4): 358-360. Chinese with abstract in English.
22. 3. Mol Pharmacol. 1997; 51(5): 741-754.
23. Annaert P, Kinget R, Naesens L, et al. Transport, uptake, and metabolism of the bis (pivaloyloxymethyl)-ester prodrug of 9-(2-phosphonylmethoxyethyl) adenine in an in vitro cell culture system of the intestinal mucosa (Caco-2). Pharm Res. 1997; 14(4): 492-496.
24. Van Gelder J, Annaert P, Naesens L, et al. Inhibition of intestinal metabolism of the antiviral ester prodrug bis (POC)-PMPA by nature-identical fruit extracts as a strategy to enhance its oral absorption: an in vitro study. Pharm Res. 1999; 16(7): 1035-1040.
25. Bartels H, Korsiak E, Daniel H. Transport activity of the MDR1-gene product in monolayers of Caco-2 cells. Zeitschrift fur Gastroenterologie. 1994; 32: 15-18.
26. Dibas A, Wood J, Mia AJ, et al. The ATP-depleting reagent iodoacetamide induces the degradation of protein kinase C alpha (PKCalpha) in LLC-PK1 pig kidney cells. Life Sci. 1997; 61(17): 1697-1704.
27. Tsuruo T, Iida H, Tsukagoshi S, et al. Overcoming of vincristine resistance in P388 leukemia in vivo and in vitro through enhanced cytotoxicity of vincristine and vinblastine by verapamil. Cancer Res. 1981; 41(5): 1967-1972.
28. Roepe PD. The P-glycoprotein efflux pump: how does it transport drugs? J Membr Biol. 1997; 160(3): 161-175.
29. Leier I, Jedlitschky G, Buchholz U, et al. The MRP gene encodes an ATP-dependent export pump for leukotriene C4 and structurally related conjugates. J Biol Chem. 1994; 269(45): 27807-27810.
30. Jedlitschky G, Leier I, Buchholz U. ATP-dependent transport of glutathione S-conjugates by the multidrug resistance-associated protein. Cancer Res. 1994; 54 (18): 4833-4836.
31. Barrand MA, Bargrij T, Neo SY. Multidrug resistance-associated protein: A protein distinct from P-glycoprotein involved in cytotoxic drug expulsion. Gen Pharmacol. 1997; 28(5): 639-645.
32. Chen J, Lin H, Hu M. Absorption and metabolism of genistein and its five isoflavone analogs in the human intestinal Caco-2 model. Cancer Chemother Pharmacol. 2005; 55(2): 159-169.
33. Nikolic D, Li Y, Chadwick LR, et al. In vitro studies of intestinal permeability and hepatic and intestinal metabolism of 8-prenylnaringenin, a potent phytoestrogen from hops (Humulus lupulus L.). Pharm Res. 2006; 23(5): 864-872.