Phenobarbital responsiveness as a uniquely sensitive indicator of hepatocyte differentiation status: requirement of dexamethasone and extracellular matrix in establishing the functional integrity of cultured primary rat hepatocytes.

We used a serum-free, highly defined primary hepatocyte culture model to investigate the mechanisms whereby dexamethasone (Dex) and extracellular matrix (ECM) coordinate cell differentiation and transcriptional responsiveness to the inducer, phenobarbital (PB). Low nanomolar levels of Dex and dilute concentrations of ECM overlay were essential in the maintenance of normal hepatocyte physiology, as assessed by cell morphology, LDH release, expression of the hepatic nuclear factors C/EBPalpha, -beta, -gamma, HNF-1alpha, -1beta, -4alpha, and RXRalpha, expression of prototypical hepatic marker genes, including albumin and transferrin, and ultimately, cellular capacity to respond to PB. The loss of hepatocyte integrity produced by deficiency of these components correlated with the activation of several stress signaling pathways including the MAPK, SAPK/JNK, and c-Jun signaling pathways, with resulting nuclear recruitment of the activated protein-1 (AP-1) complex. In Dex-deficient cultures, normal cellular function, including the PB induction response, was largely restored in a dose-dependent manner by reintroduction of nanomolar additions of the hormone, in the presence of ECM. Our results demonstrate critical and cooperative roles for Dex and ECM in establishing hepatocyte integrity and in the coordination of an array of liver-specific functions. These studies further establish the PB gene induction response as an exceptionally sensitive indicator of hepatocyte differentiation status.

[1]  C. Selden,et al.  What keeps hepatocytes on the straight and narrow? Maintaining differentiated function in the liver , 1999, Gut.

[2]  C. DiPersio,et al.  Extracellular signals that regulate liver transcription factors during hepatic differentiation in vitro , 1991, Molecular and cellular biology.

[3]  James R. Woodgett,et al.  Phosphorylation of c-jun mediated by MAP kinases , 1991, Nature.

[4]  A. Huang,et al.  Glucocorticoids Stimulate p21 Gene Expression by Targeting Multiple Transcriptional Elements within a Steroid Responsive Region of the p21 waf1/cip1 Promoter in Rat Hepatoma Cells* , 1998, The Journal of Biological Chemistry.

[5]  S. Boyle,et al.  PI3K inhibitors reverse the suppressive actions of insulin on CYP2E1 expression by activating stress-response pathways in primary rat hepatocytes. , 2001, Molecular pharmacology.

[6]  R. Gebhardt,et al.  Cell‐cell interactions: Clues to hepatocyte heterogeneity and beyond? , 1992, Hepatology.

[7]  M L Yarmush,et al.  Culture matrix configuration and composition in the maintenance of hepatocyte polarity and function. , 1996, Biomaterials.

[8]  R. Juliano Cooperation between soluble factors and integrin‐mediated cell anchorage in the control of cell growth and differentiation , 1996, BioEssays : news and reviews in molecular, cellular and developmental biology.

[9]  J. Gustafsson,et al.  The non-activated glucocorticoid receptor: structure and activation. , 1989, Journal of steroid biochemistry.

[10]  M. Negishi,et al.  Activation by diverse xenochemicals of the 51-base pair phenobarbital-responsive enhancer module in the CYP2B10 gene. , 1998, Molecular pharmacology.

[11]  A. Anderson,et al.  Localization of a phenobarbital-responsive element (PBRE) in the 5'-flanking region of the rat CYP2B2 gene. , 1995, Gene.

[12]  J. S. Sidhu,et al.  Forskolin-mediated induction of CYP3A1 mRNA expression in primary rat hepatocytes is independent of elevated intracellular cyclic AMP. , 1996, The Journal of pharmacology and experimental therapeutics.

[13]  T. Kawamoto,et al.  The Peptide Near the C Terminus Regulates Receptor CAR Nuclear Translocation Induced by Xenochemicals in Mouse Liver , 2001, Molecular and Cellular Biology.

[14]  A. Aplin,et al.  Signal transduction and signal modulation by cell adhesion receptors: the role of integrins, cadherins, immunoglobulin-cell adhesion molecules, and selectins. , 1998, Pharmacological reviews.

[15]  M. Weiss,et al.  Hepatocyte Nuclear Factor 4 Provokes Expression of Epithelial Marker Genes, Acting As a Morphogen in Dedifferentiated Hepatoma Cells , 1998, The Journal of cell biology.

[16]  M J Bissell,et al.  Tissue phenotype depends on reciprocal interactions between the extracellular matrix and the structural organization of the nucleus. , 1998, Proceedings of the National Academy of Sciences of the United States of America.

[17]  G. Firestone,et al.  Role of the CCAAT/Enhancer Binding Protein-α Transcription Factor in the Glucocorticoid Stimulation of p21 waf1/cip1 Gene Promoter Activity in Growth-arrested Rat Hepatoma Cells* , 1998, The Journal of Biological Chemistry.

[18]  F. Giancotti,et al.  Alpha3beta1-integrin as a critical mediator of the hepatic differentiation response to the extracellular matrix. , 1998, Hepatology.

[19]  J. Cidlowski,et al.  Mechanisms of Glucocorticoid-receptor-mediated Repression of Gene Expression , 1999, Trends in Endocrinology & Metabolism.

[20]  J. Maher,et al.  Cell-matrix interactions in liver. , 1993, Seminars in cell biology.

[21]  J. S. Sidhu,et al.  Influence of extracellular matrix overlay on phenobarbital-mediated induction of CYP2B1, 2B2, and 3A1 genes in primary adult rat hepatocyte culture. , 1993, Archives of biochemistry and biophysics.

[22]  S. Duncan,et al.  Mammalian hepatocyte differentiation requires the transcription factor HNF-4alpha. , 2000, Genes & development.

[23]  D. Jackson,et al.  The extracellular matrix coordinately modulates liver transcription factors and hepatocyte morphology , 1991, Molecular and cellular biology.

[24]  F. Giancotti,et al.  α3β1‐integrin as a critical mediator of the hepatic differentiation response to the extracellular matrix , 1998 .

[25]  J. Gustafsson,et al.  Mechanism of gene expression by the glucocorticoid receptor: Role of protein‐protein interactions , 1997, BioEssays : news and reviews in molecular, cellular and developmental biology.

[26]  D. Bissell,et al.  The role of extracellular matrix in normal liver. , 1988, Scandinavian journal of gastroenterology. Supplement.

[27]  G. Schütz,et al.  Synergistic action of the glucocorticoid receptor with transcription factors. , 1988, The EMBO journal.

[28]  W. Hong,et al.  All-trans-Retinoic Acid Inhibits Jun N-terminal Kinase-dependent Signaling Pathways* , 1998, The Journal of Biological Chemistry.

[29]  J. S. Sidhu,et al.  Protein Synthesis Inhibitors Exhibit a Nonspecific Effect on Phenobarbital-inducible Cytochome P450 Gene Expression in Primary Rat Hepatocytes* , 1998, The Journal of Biological Chemistry.

[30]  A. Manning,et al.  Multiple signals converging on NF-κB , 1999 .

[31]  D. Mischoulon,et al.  Cell-extracellular matrix interactions can regulate the switch between growth and differentiation in rat hepatocytes: reciprocal expression of C/EBP alpha and immediate-early growth response transcription factors , 1994, Molecular and cellular biology.

[32]  M. Weiss,et al.  Hepatocyte nuclear factor 4 expression overcomes repression of the hepatic phenotype in dedifferentiated hepatoma cells , 1997, Molecular and cellular biology.

[33]  K. Zaret The touch that hepatocytes seem to like , 1992, Hepatology.

[34]  N. Dean,et al.  Ser/Thr protein phosphatase type 5 (PP5) is a negative regulator of glucocorticoid receptor-mediated growth arrest. , 1999, Biochemistry.

[35]  G. Williams,et al.  Phenobarbital mechanistic data and risk assessment: enzyme induction, enhanced cell proliferation, and tumor promotion. , 1996, Pharmacology & therapeutics.

[36]  J. Pascussi,et al.  Dexamethasone enhances constitutive androstane receptor expression in human hepatocytes: consequences on cytochrome P450 gene regulation. , 2000, Molecular pharmacology.

[37]  M. Takiguchi,et al.  The gene for hepatocyte nuclear factor (HNF)‐4α is activated by glucocorticoids and glucagon, and repressed by insulin in rat liver , 2000, FEBS letters.

[38]  A. Manning,et al.  Multiple signals converging on NF-kappaB. , 1999, Current opinion in cell biology.

[39]  M. Schwartz,et al.  Coordinate signaling by integrins and receptor tyrosine kinases in the regulation of G1 phase cell-cycle progression. , 2001, Current opinion in genetics & development.

[40]  J. S. Sidhu,et al.  Insulin‐mediated modulation of cytochrome P450 gene induction profiles in primary rat hepatocyte cultures , 1999, Journal of biochemical and molecular toxicology.

[41]  J. S. Sidhu,et al.  cAMP-associated Inhibition of Phenobarbital-inducible Cytochrome P450 Gene Expression in Primary Rat Hepatocyte Cultures (*) , 1995, The Journal of Biological Chemistry.

[42]  M. Karin,et al.  AP-1--glucocorticoid receptor crosstalk taken to a higher level. , 2001, The Journal of endocrinology.

[43]  H. Moriwaki,et al.  Control of cyclins, cyclin-dependent kinase inhibitors, p21 and p27, and cell cycle progression in rat hepatocytes by extracellular matrix. , 2000, Journal of hepatology.

[44]  A. Y. Lu,et al.  Interindividual variability in inhibition and induction of cytochrome P450 enzymes. , 2001, Annual review of pharmacology and toxicology.

[45]  R. Wisdom,et al.  AP-1: one switch for many signals. , 1999, Experimental cell research.

[46]  M. Cobb,et al.  Mitogen-activated protein kinase pathways. , 1997, Current opinion in cell biology.

[47]  J. S. Sidhu,et al.  Modulation of xenobiotic-inducible cytochrome P450 gene expression by dexamethasone in primary rat hepatocytes. , 1995, Pharmacogenetics.

[48]  M. Imae,et al.  Gene expression of the three members of hepatocyte nuclear factor-3 is differentially regulated by nutritional and hormonal factors. , 2000, The Journal of endocrinology.

[49]  Miguel Beato,et al.  Steroid hormone receptors: Many Actors in search of a plot , 1995, Cell.

[50]  J. Yager,et al.  A morphological study of differentiated hepatocytes in vitro , 1995, Hepatology.

[51]  A. Ben-Ze'ev,et al.  Cell-cell and cell-matrix interactions differentially regulate the expression of hepatic and cytoskeletal genes in primary cultures of rat hepatocytes. , 1988, Proceedings of the National Academy of Sciences of the United States of America.

[52]  Experimental Cell Research , 1949, Nature.

[53]  C. Streuli,et al.  Extracellular Matrix Selectively Modulates the Response of Mammary Epithelial Cells to Different Soluble Signaling Ligands* , 1999, The Journal of Biological Chemistry.

[54]  R. Remmel,et al.  Concise review of the cytochrome P450s and their roles in toxicology. , 1999, Toxicological sciences : an official journal of the Society of Toxicology.

[55]  Suzanne D. Conzen,et al.  Glucocorticoid Receptor-mediated Protection from Apoptosis Is Associated with Induction of the Serine/Threonine Survival Kinase Gene, sgk-1 * , 2001, The Journal of Biological Chemistry.