Kidney proximal human tubule HK-2 cell line as a tool for the investigation of P-glycoprotein modulation by natural compounds;La línea celular de túbulo proximal de riñón humano HK-2 como una herramienta para la investigación de la modulación de P-glicoproteína por compuestos naturales

Boletin Latinoamericano y del Caribe de Plantas Medicinales y Aromaticas

Volumn 7, Issue 6, 2008, Pages 281-294

  Chieli, Elisabetta ^a   Romiti, Nadia ^a  

^a UNIVERSITY OF PISA   (Italy)

Author keywords

Calcein AM; HK 2 cell line; P glycoprotein; Phytochemicals; Rhodamine 123

Indexed keywords

APIGENIN; CALCEIN; CURCUMIN; ECHINACEA EXTRACT; FLAVONOID; GLYCOPROTEIN P; HYPERICUM PERFORATUM EXTRACT; KAEMPFEROL; NARINGENIN; NATURAL PRODUCT; RESVERATROL; RHODAMINE 123; VERAPAMIL;

BINDING AFFINITY; BINDING SITE; COMMON COLD; DEPRESSION; DOWN REGULATION; DRUG MECHANISM; DRUG POTENCY; DRUG PROTEIN BINDING; DRUG SCREENING; ECHINACEA; ENZYME ACTIVITY; ENZYME INHIBITION; ENZYME SUBSTRATE; FLU LIKE SYNDROME; GRAPEFRUIT JUICE; HERB DRUG INTERACTION; HK 2 CELL; HUMAN; HYPERICUM PERFORATUM; KIDNEY PROXIMAL TUBULE; NONHUMAN; PROTEIN ANALYSIS; PROTEIN EXPRESSION; PROTEIN FUNCTION; PROTEIN INTERACTION; REVIEW;

EID: 70350342448     PISSN: None     EISSN: 07177917     Source Type: Journal    
DOI: None     Document Type: Review

References (92)

1. Aszalos A. 2007a. Drug-drug interactions affected by the transporter protein, P-glycoprotein (ABCB1, MDR1) I. Preclinical aspects. Drug Discov Today 12:833-837.
2. Aszalos A. 2007b. Drug-drug interactions affected by the transporter protein, P-glycoprotein (ABCB1, MDR1) II. Clinical aspects. Drug Discov Today 12:838-843.
3. Barnes J, Anderson LA, Gibbons S, Phillipson JD. 2005. Echinacea species [Echinacea angustifolia (DC.) Hell., Echinacea pallida (Nutt.) Nutt., Echinacea purpurea L. (Moench)]: a review of their chemistry, pharmacology and clinical properties. J Pharm Pharmacol 57:929-954.
4. Berggren S, Gall C, Wollnitz N, Ekelund M, Karlbom U, Hoogstraate J, Schrenk D, Lennernäs H. 2007. Gene and protein expression of P-glycoprotein, MRP1, MRP2, and CYP3A4 in the small and large human intestine. Mol Pharm 4:252-257.
5. Chan LM, Lowes S, Hirst BH. 2004. The ABCs of drug transport in intestine and liver: efflux proteins limiting drug absorption and bioavailability. Eur J Pharm Sci 21:25-51.
6. Chearwae W, Anuchapreeda S, Nandigama K, Ambudkar SV, Limtrakul P. 2004. Biochemical mechanism of modulation of human P-glycoprotein (ABCB1) by curcumin I, II, and III purified from Turmeric powder. Biochem Pharmacol 68:2043-2052.
7. Chieli E, Romiti N, Cervelli F, Tongiani R. 1995. Effects of flavonols on P-glycoprotein activity in cultured rat hepatocytes. Life Sci 57:1741-1751.
8. Chieli E, Romiti N, Cervelli F, Tongiani R. 1998. Influence of some plant dietary compounds on P-glycoproteinmediated multidrug resistance. Cancer Detect Prev 22:214.
9. Chieli E, Romiti N, Tramonti G. 2002. Influence of drugs on P-gp-mediated transport in the human proximal tubular cell line HK-2. Nephrol Dial Transplant S1 17:55.
10. Choi BH, Kim CG, Lim Y, Shin SY, Lee YH. 2008. Curcumin down-regulates the multidrug-resistance mdr1b gene by inhibiting the PI3K/Akt/NFkappaB pathway. Cancer Lett 259:111-118.
11. Conseil G, Baubichon-Cortay H, Dayan G, Jault JM, Barron D, Di Pietro A. 1998. Flavonoids: a class of modulators with bifunctional interactions at vicinal ATP- and steroid-binding sites on mouse Pglycoprotein. Proc Natl Acad Sci USA 95:9831-9836.
12. Das DK, Maulik N. 2006. Resveratrol in cardioprotection: a therapeutic promise of alternative medicine. Mol Interv 6:36-47.
13. Dasgupta A, Hovanetz M, Olsen M, Wells A, Actor JK. 2007. Drug-herb interaction: effect of St. John's wort on bioavailability and metabolism of procainamide in mice. Arch Pathol Lab Med 131:1094-1098.
14. De Castro WV, Mertens-Talcott S, Derendorf H, Butterweck V. 2007. Grapefruit juice-drug interactions: Grapefruit juice and its components inhibit Pglycoprotein (ABCB1) mediated transport of talinolol in Caco-2 cells. J Pharm Sci 96:2808-2817.
15. Di Pietro A, Conseil G, Pérez-Victoria JM, Dayan G, Baubichon-Cortay H, Trompier D, Steinfels E, Jault JM, de Wet H, Maitrejean M, Comte G, Boumendjel A, Mariotte AM, Dumontet C, McIntosh DB, Goffeau A, Castanys S, Gamarro F, Barron D. 2002. Modulation by flavonoids of cell multidrug resistance mediated by P-glycoprotein and related ABC transporters. Cell. Mol Life Sci 59:307-322.
16. Dürr D, Stieger B, Kullak-Ublick GA, Rentsch KM, Steinert HC, Meier PJ, Fattinger K. 2000. St John's Wort induces intestinal P-glycoprotein/MDR1 and intestinal and hepatic CYP3A4. Clin Pharmacol Ther 68:598-604.
17. Endres CJ, Hsiao P, Chung FS, Unadkat JD. 2006. The role of transporters in drug interactions. Eur J Pharm Sci 27:501-17.
18. Eneroth A, Åström E, Hoogstraate J, Schrenk D, Conrad S, Kauffmann H-M, Gjellan K. 2001. Evaluation of a vincristine resistant Caco-2 cell line for use in a calcein-AM extrusion screening assay for Pglycoprotein interaction. Eur J Pharmaceut Sci 12:205-214.
19. Ernest S, Bello-Reuss E. 1998. P-glycoprotein functions and substrates: possible roles of MDR1 gene in the kidney. Kidney Int Suppl 65:S11-17.
20. Fromm MF. 2004. Importance of P-glycoprotein at bloodtissue barriers. Trends Pharmacol Sci 25:423-429.
21. Gödtel-Armbrust U, Metzger A, Kroll U, Kelber O, Wojnowski L. 2007. Variability in PXR-mediated induction of CYP3A4 by commercial preparations and dry extracts of St. John's wort. Naunyn Schmiedebergs Arch Pharmacol 375: 377-382.
22. Gottesman MM, Ling V. 2006. The molecular basis of multidrug resistance in cancer: the early years of Pglycoprotein research. FEBS Lett 580:998-1009.
23. Gurley BJ, Swain A, Williams DK, Barone G, Battu SK. 2008. Gauging the clinical significance of Pglycoprotein- mediated herb-drug interactions: Comparative effects of St. John's wort, Echinacea, clarithromycin, and rifampin on digoxin pharmacokinetics. Mol Nutr Food Res Jan 23 [Epub ahead of print]
24. Han Y, Tan TMC, Lim L-Y. 2006. Effects of capsaicin on P-gp function and expression in Caco-2 cells. Biochem Pharmacol 71:1727-1734.
25. Holló Z, Homolya L, Davis CW, Sarkadi B. 1994. Calcein accumulation as a fluorometric functional assay of the multidrug transporter. Biochim Biophys Acta 1191:384-388.
26. Holme AL, Pervaiz S.J. 2007. Resveratrol in cell fate decisions. Bioenerg Biomembr 39:59-63.
27. Honda Y, Ushigome F, Koyabu N, Morimoto S, Shoyama Y, Uchiumi T, Kuwano M, Ohtani H, Sawada Y. 2004. Effects of grapefruit juice and orange juice components on P-glycoprotein- and MRP2-mediated drug efflux. Br J Pharmacol 143:856-64.
28. Hu M, Chen J, Lin H. 2003. Metabolism of flavonoids via enteric recycling: mechanistic studies of disposition of apigenin in the Caco-2 cell culture model. J Pharmacol Exp Ther 307:314-321.
29. Hu Z, Yang X, Ho PC, Chan SY, Heng PW, Chan E, Duan W, Koh HL, Zhou S. 2005. Herb-drug interactions: a literature review. Drugs 65:1239-1282.
30. Huls M, Brown CD, Windass AS, Sayer R, van den Heuvel JJ, Heemskerk S, Russel FG, Masereeuw R. 2008. The breast cancer resistance protein transporter ABCG2 is expressed in the human kidney proximal tubule apical membrane. Kidney Int 73:220-225.
31. Inui KI, Masuda S, Saito H. 2000. Cellular and molecular aspects of drug transport in the kidney. Kidney Int 58:944-958.
32. Izzo AA, Ernst E. 2001. Interactions between herbal medicines and prescribed drugs: a systematic review. Drugs 61:2163-2175.
33. Izzo AA. 2005. Herb-drug interactions: an overview of the clinical evidence. Fundam Clin Pharmacol 19:1-16.
34. Jodoin J, Demeule M, Béliveau R. 2002. Inhibition of the multidrug resistance P-glycoprotein activity by green tea polyphenols. Biochim Biophys Acta 1542:149-159.
35. Kane GC, Lipsky JJ. 2000. Drug-grapefruit juice interactions. Mayo Clin Proc 75:933-942.
36. Keogh JP, Kunta JR. 2006. Development, validation and utility of an in vitro technique for assessment of potential clinical drug-drug interactions involving Pglycoprotein. Eur J Pharm Sci 27:543-554.
37. Kiani J, Imam SZ. 2007. Medicinal importance of grapefruit juice and its interaction with various drugs. Nutr J 6:33.
38. Kitagawa S, Nabekura T, Takahashi T, Nakamura Y, Sakamoto H, Tano H, Hirai M, Tsukahara G. 2005. Structure-activity relationships of the inhibitory effects of flavonoids on P-glycoprotein-mediated transport in KB-C2 cells. Biol Pharm Bull 28:2274-2278.
39. Kruidering M, Maasdam DH, Prins FA, de Heer E, Mulder GJ, Nagelkerke GF. 1994. Evaluation of nephrotoxicity in vitro using a suspension of highly purified porcine proximal tubular cells and characterization of the cells in primary culture. Exp Nephrol 2:324-44.
40. LeBlanc GA. 1994. Hepatic vectorial transport of xenobiotics. Chem Biol Interact 90:101-120.
41. Lee W, Kim RB. 2004. Transporters and renal drug elimination. Annu Rev Pharmacol Toxicol 44:137-166.
42. Li P, Callery PS, Gan LS, Balani SK. 2007. Esterase inhibition by grapefruit juice flavonoids leading to a new drug interaction. Drug Metab Dispos 35:1203-1208.
43. Limtrakul P. 2007. Curcumin as chemosensitizer. Adv Exp Med Biol 595:269-300.
44. Lin JH. 2003. Drug-drug interaction mediated by inhibition and induction of P-glycoprotein. Adv Drug Deliv Rev 55:53-81.
45. Lin JH. 2007. Transporter-mediated drug interactions: clinical implications and in vitro assessment. Expert Opin Drug Metab Toxicol 3:81-92
46. Linton K J. 2007. Structure and Function of ABC transporters. Physiology 22:122-130.
47. Liu YT, Hao HP, Liu CX, Wang GJ, Xie HG. 2007. Drugs as CYP3A probes, inducers, and inhibitors. Drug Metab Rev 39:699-721.
48. Lohner K, Schnäbele K, Daniel H, Oesterle D, Rechkemmer G, Göttlicher M, Wenzel U. 2007. Flavonoids alter P-gp expression in intestinal epithelial cells in vitro and in vivo. Mol Nutr Food Res 51:293-300.
49. Marchetti S, Mazzanti R, Beijnen JH, Schellens JH. 2007. Concise review: Clinical relevance of drug drug and herb drug interactions mediated by the ABC transporter ABCB1 (MDR1, P-glycoprotein). Oncologist 12:927-941.
50. Marzolini C, Paus E, Buclin T, Kim RB. 2004. Polymorphisms in human MDR1 (P-glycoprotein): recent advances and clinical relevance. Clin Pharmacol Ther 75:13-33.
51. Meijerman I, Beijnen JH, Schellens JHM. 2006. Herb-drug interactions in oncology: focus on mechanisms of induction. Oncologist 11:742-752.
52. Mertens-Talcott SU, Zadezensky I, De Castro WV, Derendorf H, Butterweck V. 2006. Grapefruit-drug interactions: can interactions with drugs be avoided? J Clin Pharmacol 46:1390-1416.
53. Modarai M, Gertsch J, Suter A, Heinrich M, Koertenkamp A. 2007. Cytochrome P450 inhibitory action of Echinacea preparations differs widely and co-varies with alkylamide content. J Pharm Pharmacol 59:567-573.
54. Molnar J, Gyemant N, Tanaka M, Hohmann J, Bergmannleitner E, Molnar P, Deli J, Didiziapetris R, Ferreira MJ. 2006. Inhibition of multidrug resistance of cancer cells by natural diterpenes, triterpenes and carotenoids. Curr Pharm Des 12:287-311.
55. Morris ME, Zhang S. 2006. Flavonoid-drug interactions: Effects of flavonoids on ABC transporters. Life Sci 78:2116-2130.
56. Nabekura T, Kamiyama S, Kitagawa S. 2005. Effects of dietary chemopreventive phytochemicals on Pglycoprotein function. Biochem Biophys Res Commun 18:866-870.
57. Nabekura T, Yamaki T, Ueno K, Kitagawa S. 2008. Inhibition of P-glycoprotein and multidrug resistance protein 1 by dietary phytochemicals. Cancer Chemother Pharmacol DOI 10.1007/s00280-007-0676- 4.
58. Nieri P, Romiti N, Adinolfi B, Chicca A, Massarelli I, Chieli E. 2006. Modulation of P-glycoprotein activity by cannabinoid molecules in HK-2 renal cells. Br J Pharmacol 148:682-687.
59. Pal D, Mitra AK. 2006. MDR- and CYP3A4-mediated drug-herbal interactions. Life Sci 78:2131-2145.
60. Patel D, Shukla S, Gupta S. 2007. Apigenin and cancer chemoprevention: progress, potential and promise. Int J Oncol 30:233-245.
61. Pellati F, Calo S, Benvenuti S, Adinolfi B, Nieri P, Melegari M. 2006. Isolation and structure elucidation of cytotoxic polyacetylenes and polyenes from Echinacea pallida. Phytochemistry 67:1359-1364.
62. Perloff MD, Störmer E, von Moltke LL, Greenblatt DJ. 2003. Rapid assessment of P-glycoprotein inhibition and induction in vitro. Pharm Res 20:1177-1183.
63. Prime-Chapman HM, Fearn RA, Cooper AE, Moore V, Hirst BH. 2004. Differential multidrug resistanceassociated protein 1 through 6 isoform expression and function in human intestinal epithelial Caco-2 cells. J Pharmacol Exp Ther 311:476-484.
64. Rautio J, Humphreys JE, Webster LO, Balakrishnan A, Keogh JP, Kunta JR, Serabjit-Singh CJ, Polli JW. 2006. In vitro P-glycoprotein inhibition assays for assessment of clinical drug interaction potential of new drug candidates: a recommendation for probe Substrates. Drug Metab Dispos 34:786-792.
65. Rodriguez-Proteau R, Mata JE, Miranda CL, Fan Y, Brown JJ, Buhler DR. 2006. Plant polyphenols and multidrug resistance: Effects of dietary flavonoids on drug transporters in Caco-2 and MDCKII-MDR1 cell transport models. Xenobiotica 36:41-58.
66. Romiti N, Pellati F, Nieri P, Benvenuti S, Adinolfi B, Chieli E. 2008. P-glycoprotein inhibitory activity of lipophilic constituents of Echinacea pallida roots in a human proximal tubular cell line. Planta Med 74:1-3.
67. Romiti N, Tongiani, Cervelli F, Chieli E. 1998. Effects of curcumin on P-glycoprotein in primary cultures of rat hepatocytes. Life Sci 62:2349-2358.
68. Romiti N, Tramonti G, Chieli E. 2001. Up-regulation of MDR1 P-Glycoprotein by 1,25(OH)2D3 in the proximal tubular cell line HK-2. J Am Soc Nephrol 10:689A.
69. Romiti N, Tramonti G, Chieli E. 2002. Influence of different chemicals on MDR-1 P-glycoprotein expression and activity in the HK-2 proximal tubular cell line. Toxicol Appl Pharmacol 183:83-91.
70. Romiti N, Tramonti G, Donati A, Chieli E. 2004. Effects of grapefruit juice on the multidrug transporter Pglycoprotein in the human proximal tubular cell line HK-2. Life Sci 76:293-302.
71. Ryan MJ, Johnson G, Kirk J, Fuerstenberg SM, Zager RA, Torok-Storb B. 1994. HK-2: an immortalized proximal tubule epithelial cell line from normal adult human kidney. Kidney Int 45:48-57.
72. Schinkel AH, Jonker JW. 2003. Mammalian drug efflux transporters of the ATP binding cassette (ABC) family: an overview. Adv Drug Deliv Rev 55:3-29.
73. Schlatter P, Gutmann H, Drewe J. 2006. Primary porcine proximal tubular cells as a model for transepithelial drug transport in human kidney. Eur J Pharmaceut Sci 28:141-154.
74. Schulz V. 2006. Safety of St. John's Wort extract compared to synthetic antidepressants. 2005. Phytomedicine 13:199-204.
75. Shankar S, Singh G, Srivastava RK. 2007. Chemoprevention by resveratrol: molecular mechanisms and therapeutic potential. Front Biosci 12:4839-4854.
76. Shapiro AB, Ling V. 1997. Effect of quercetin on Hoechst 33342 transport by purified and reconstituted Pglycoprotein. Biochem Pharmacol 53:587-596.
77. Shirasaka Y, Onishi Y, Sakurai A, Nakagawa H, Ishikawa T, Yamashita S. 2006. Evaluation of human Pglycoprotein (MDR1/ABCB1) ATPase activity assay method by comparing with in vitro transport measurements: Michaelis-Menten kinetic analysis to estimate the affinity of P-glycoprotein to drugs. Biol Pharm Bull. 29: 2465-2471.
78. Tanigawara Y. 2000. Role of P-glycoprotein in drug disposition. Ther Drug Monit 22:137-140.
79. Taub ME, Podila L, Ely D, Almeida I. 2005. Functional assessment of multiple P-glycoprotein (P-gp) probe substrates: influence of cell line and modulator concentration on P-gp activity. Drug Metab Dispos 33:1679-1687.
80. Tiberghien F, Loor F. 1996. Ranking of P-glycoprotein substrates and inhibitors by a calcein-AM fluorometry screening assay. Anticancer Drugs. 7:568-578.
81. Tramonti G, Romiti N, Norpoth M, Chieli E. 2001. Pglycoprotein in HK-2 proximal tubule cell line. Ren Fail 23:331-337.
82. Troutman MD, Thakker DR. 2003. Rhodamine 123 requires carrier-mediated influx for its activity as a Pglycoprotein substrate in Caco-2 cells. Pharm Res 20:1192-1199.
83. Varma MV, Ashokraj Y, Dey CS, Panchagnula R. 2003. Pglycoprotein inhibitors and their screening: a perspective from bioavailability enhancement. Pharmacol Res 48:347-359.
84. Wang Y, Hao D, Stein WD, Yang L. 2006. A kinetic study of Rhodamine123 pumping by P-glycoprotein. Biochim Biophys Acta 1758:1671-1676.
85. Woelkart K, Bauer R. 2007. The role of alkamides as an active principle of Echinacea. Planta Med 73:615-623.
86. Woelkart K, Marth E, Suter A, Schoop R, Raggam RB, Koidl C, Kleinhappl B, Bauer R. 2006. Bioavailability and pharmacokinetics of Echinacea purpurea preparations and their interaction with the immune system. Int J Clin Pharmacol Ther 44:401-408.
87. Yale SH, Glurich I. 2005. Analysis of the inhibitory potential of Ginkgo biloba, Echinacea purpurea, and Serenoa repens on the metabolic activity of cytochrome P450 3A4, 2D6, and 2C9. J Altern Complement Med 11:433-439.
88. Yao LH, Jiang YM, Shi J, Tomás-Barberán FA, Datta N, Singanusong R, Chen SS. 2004. Flavonoids in food and their health benefits. Plant Foods Hum Nutr 59:113-122.
89. Yu DK. 1999. The contribution of P-glycoprotein to pharmacokinetic drug-drug interactions. J Clin Pharmacol 39:1203-1211.
90. Zhang W, Tan TM, Lim LY. 2007. Impact of curcumininduced changes in P-glycoprotein and CYP3A expression on the pharmacokinetics of peroral celiprolol and midazolam in rats. Drug Metab Dispos 35:110-115.
91. Zhou S, Lim LY, Chowbay B. 2004. Herbal modulation of P-glycoprotein.Drug Metab Rev 36:57-104.
92. Zhou SF, Zhou ZW, Li CG, Chen X, Yu X, Xue CC, Herington A. 2007. Identification of drugs that interact with herbs in drug development. Drug Discov Today 12:664-673.