Predicting in vivo anti-hepatofibrotic drug efficacy based on in vitro high-content analysis

PLoS ONE

Volumn 6, Issue 11, 2011, Pages

  Zheng, Baixue ^a,b,c   Tan, Looling ^b   Mo, Xuejun ^a,b   Yu, Weimiao ^g,i   Wang, Yan ^b,h   Tucker Kellogg, Lisa ^a,c   Welsch, Roy E ^a,k   So, Peter T C ^a,d,j   Yu, Hanry ^{a,b,c,d,e,f,j}  

^a NATIONAL UNIVERSITY OF SINGAPORE   (Singapore)

^b INSTITUTE OF BIOENGINEERING AND NANOTECHNOLOGY   (Singapore)

^c NATIONAL UNIVERSITY OF SINGAPORE   (Singapore)

^d SINGAPORE MIT ALLIANCE FOR RESEARCH AND TECHNOLOGY   (Singapore)

^e NATIONAL UNIVERSITY OF SINGAPORE   (Singapore)

^f NATIONAL UNIVERSITY OF SINGAPORE   (Singapore)

^g BIOINFORMATICS INSTITUTE   (Singapore)

^h SOUTHERN MEDICAL UNIVERSITY   (China)

ⁱ INSTITUTE OF MOLECULAR AND CELL BIOLOGY   (Singapore)

^j MASSACHUSETTS INSTITUTE OF TECHNOLOGY   (United States)

^k MASSACHUSETTS INSTITUTE OF TECHNOLOGY   (United States)

more..

Author keywords

[No Author keywords available]

Indexed keywords

16ALPHA CYANOPREGNENOLONE; ANTIFIBROTIC AGENT; BROXURIDINE; CAMOSTAT MESILATE; CARBON TETRACHLORIDE; CASPASE 3; COLCHICINE; COLLAGEN TYPE 3; CYCLIC AMP RESPONSIVE ELEMENT BINDING PROTEIN; DIMETHYLNITROSAMINE; EPIGALLOCATECHIN GALLATE; F ACTIN; GELATINASE A; HYDROETHIDINE; IMATINIB; MALOTILATE; MELATONIN; MINOXIDIL; OXYMATRINE; PIOGLITAZONE; PIRFENIDONE; ROSMARINIC ACID; SILYMARIN; SMAD3 PROTEIN; SOMATOSTATIN; TAURINE; TETRANDRINE; THALIDOMIDE; TISSUE INHIBITOR OF METALLOPROTEINASE 1; UNINDEXED DRUG; BIOLOGICAL MARKER;

APOPTOSIS; ARTICLE; AUTOMATION; CELL PROLIFERATION; CONTROLLED STUDY; DRUG EFFICACY; DRUG SCREENING; HIGH CONTENT ANALYSIS; HUMAN; HUMAN CELL; IMAGE PROCESSING; IMAGE RETRIEVAL; IN VITRO STUDY; LIVER FIBROSIS; MITOCHONDRIAL MEMBRANE POTENTIAL; PREDICTION; QUANTITATIVE ANALYSIS; STATISTICAL ANALYSIS; STELLATE CELL; ANIMAL; CELL LINE; CHEMICALLY INDUCED DISORDER; LIVER CIRRHOSIS; METABOLISM; RAT; VALIDATION STUDY;

RATTUS;

ANIMALS; BIOLOGICAL MARKERS; CARBON TETRACHLORIDE; CELL LINE; HUMANS; LIVER CIRRHOSIS; RATS;

EID: 80455179724     PISSN: None     EISSN: 19326203     Source Type: Journal    
DOI: 10.1371/journal.pone.0026230     Document Type: Article

References (52)

1. Mion F, Napoleon B, Berger F, Chevallier M, Bonvoisin S, et al. (1991) Azathioprine induced liver disease: nodular regenerative hyperplasia of the liver and perivenous fibrosis in a patient treated for multiple sclerosis. Gut 32: 715-717.
2. Jonker AM, Dijkhuis FWJ, Hardonk MJ, Moerkerk P, Tenkate J, et al. (1994) Immunohistochemical Study of Hepatic-Fibrosis Induced in Rats by Multiple Galactosamine Injections. Hepatology 19: 775-781.
3. Bonkowsky HL, Mudge GH, McMurtry RJ, (1978) Chronic Hepatic Inflammation and Fibrosis Due to Low-Doses of Paracetamol. Lancet 1: 1016-1018.
4. Lai CL, Chien RN, Leung NW, Chang TT, Guan R, et al. (1998) A one-year trial of lamivudine for chronic hepatitis B. Asia Hepatitis Lamivudine Study Group. N Engl J Med 339: 61-68.
5. Maher JJ, McGuire RF, (1990) Extracellular matrix gene expression increases preferentially in rat lipocytes and sinusoidal endothelial cells during hepatic fibrosis in vivo. J Clin Invest 86: 1641-1648.
6. Bachem MG, Meyer D, Melchior R, Sell KM, Gressner AM, (1992) Activation of rat liver perisinusoidal lipocytes by transforming growth factors derived from myofibroblastlike cells. A potential mechanism of self perpetuation in liver fibrogenesis. J Clin Invest 89: 19-27.
7. Butcher EC, (2005) Can cell systems biology rescue drug discovery? Nat Rev Drug Discov 4: 461-467.
8. Xu Q, Norman JT, Shrivastav S, Lucio-Cazana J, Kopp JB, (2007) In vitro models of TGF-beta-induced fibrosis suitable for high-throughput screening of antifibrotic agents. Am J Physiol Renal Physiol 293: F631-640.
9. Hu Q, Noor M, Wong YF, Hylands PJ, Simmonds MS, et al. (2009) In vitro anti-fibrotic activities of herbal compounds and herbs. Nephrol Dial Transplant 24: 3033-3041.
10. Dai L, Ji H, Kong XW, Zhang YH, (2010) Antifibrotic effects of ZK14, a novel nitric oxide-donating biphenyldicarboxylate derivative, on rat HSC-T6 cells and CCl4-induced hepatic fibrosis. Acta pharmacologica Sinica 31: 27-34.
11. Lee MK, Lee KY, Jeon HY, Sung SH, Kim YC, (2009) Antifibrotic activity of triterpenoids from the aerial parts of Euscaphis japonica on hepatic stellate cells. J Enzym Inhib Med Ch 24: 1276-1279.
12. Hashem MA, Jun KY, Lee E, Lim S, Choo HY, et al. (2008) A rapid and sensitive screening system for human type I collagen with the aim of discovering potent anti-aging or anti-fibrotic compounds. Mol Cells 26: 625-630.
13. Chen CZ, Peng YX, Wang ZB, Fish PV, Kaar JL, et al. (2009) The Scar-in-a-Jar: studying potential antifibrotic compounds from the epigenetic to extracellular level in a single well. Br J Pharmacol 158: 1196-1209.
14. Clinicaltrial.gov. Available:http://clinicaltrial.gov.
15. Rockey DC, (2008) Current and future anti-fibrotic therapies for chronic liver disease. Clin Liver Dis 12: 939-962, xi.
16. Langguth P, Buch P, Holm P, Thomassen JQ, Scherer D, et al. (2010) IVIVC for Fenofibrate Immediate Release Tablets Using Solubility and Permeability as In Vitro Predictors for Pharmacokinetics. J Pharm Sci 99: 4427-4436.
17. Yamaguchi H, Uchida K, Shimogawara K, (2011) Correlation of in vitro activity and in vivo efficacy of itraconazole intravenous and oral solubilized formulations by testing Candida strains with various itraconazole susceptibilities in a murine invasive infection. J Antimicrob Chemother 66: 626-634.
18. Sale S, Fong IL, de Giovanni C, Landuzzi L, Brown K, et al. (2009) APC10.1 cells as a model for assessing the efficacy of potential chemopreventive agents in the Apc(Min) mouse model in vivo. Eur J Cancer 45: 2731-2735.
19. Singh S, Miura K, Zhou H, Muratova O, Keegan B, et al. (2006) Immunity to recombinant plasmodium falciparum merozoite surface protein 1 (MSP1): protection in Aotus nancymai monkeys strongly correlates with anti-MSP1 antibody titer and in vitro parasite-inhibitory activity. Infect Immun 74: 4573-4580.
20. Yu W, Lee HK, Hariharan S, Bu W, Ahmed S, (2010) Evolving generalized Voronoi diagrams for accurate cellular image segmentation. Cytometry Part A 77: 379-386.
21. Friedman SL, (2000) Molecular regulation of hepatic fibrosis, an integrated cellular response to tissue injury. J Biol Chem 275: 2247-2250.
22. Schnabl B, Kweon YO, Frederick JP, Wang XF, Rippe RA, et al. (2001) The role of Smad3 in mediating mouse hepatic stellate cell activation. Hepatology 34: 89-100.
23. Massey FJ, (1951) The Kolmogorov-Smirnov Test for Goodness of Fit. J Am Stat Assoc 46: 68-78.
24. Deng ZY, Li J, Jin Y, Chen XL, Lu XW, (2009) Effect of oxymatrine on the p38 mitogen-activated protein kinases signalling pathway in rats with CCl4 induced hepatic fibrosis. Chin Med J (Engl) 122: 1449-1454.
25. Zhao XY, Wang BE, Li XM, Wang TL, (2008) Newly proposed fibrosis staging criterion for assessing carbon tetrachloride- and albumin complex-induced liver fibrosis in rodents. Pathol Int 58: 580-588.
26. Kershenobich D, Vargas F, Garcia-Tsao G, Perez Tamayo R, Gent M, et al. (1988) Colchicine in the treatment of cirrhosis of the liver. N Engl J Med 318: 1709-1713.
27. Ferenci P, Dragosics B, Dittrich H, Frank H, Benda L, et al. (1989) Randomized controlled trial of silymarin treatment in patients with cirrhosis of the liver. J Hepatol 9: 105-113.
28. Conover WJ, (1998) Practical Nonparametric Statistics: {John Wiley & Sons}.
29. Oakley F, Meso M, Iredale JP, Green K, Marek CJ, et al. (2005) Inhibition of inhibitor of kappaB kinases stimulates hepatic stellate cell apoptosis and accelerated recovery from rat liver fibrosis. Gastroenterology 128: 108-120.
30. de Gouville AC, Boullay V, Krysa G, Pilot J, Brusq JM, et al. (2005) Inhibition of TGF-beta signaling by an ALK5 inhibitor protects rats from dimethylnitrosamine-induced liver fibrosis. Br J Pharmacol 145: 166-177.
31. Soma J, Sugawara T, Huang YD, Nakajima J, Kawamura M, (2002) Tranilast slows the progression of advanced diabetic nephropathy. Nephron 92: 693-698.
32. van Rossum TG, Vulto AG, Hop WC, Schalm SW, (2001) Glycyrrhizin-induced reduction of ALT in European patients with chronic hepatitis C. Am J Gastroenterol 96: 2432-2437.
33. Gressner AM, Weiskirchen R, (2006) Modern pathogenetic concepts of liver fibrosis suggest stellate cells and TGF-beta as major players and therapeutic targets. J Cell Mol Med 10: 76-99.
34. Raetsch C, Jia JD, Boigk G, Bauer M, Hahn EG, et al. (2002) Pentoxifylline downregulates profibrogenic cytokines and procollagen I expression in rat secondary biliary fibrosis. Gut 50: 241-247.
35. Regev A, Berho M, Jeffers LJ, Milikowski C, Molina EG, et al. (2002) Sampling error and intraobserver variation in liver biopsy in patients with chronic HCV infection. Am J Gastroenterol 97: 2614-2618.
36. Aithal GP, Thomas JA, Kaye PV, Lawson A, Ryder SD, et al. (2008) Randomized, placebo-controlled trial of pioglitazone in nondiabetic subjects with nonalcoholic steatohepatitis. Gastroenterology 135: 1176-1184.
37. Schalm SW, van Rossum TGJ, Vulto AG, Hop WCJ, (2001) Glycyrrhizin-induced reduction of ALT in European patients with chronic hepatitis C. Am J Gastroenterol 96: 2432-2437.
38. Morgan TR, Weiss DG, Nemchausky B, Schiff ER, Anand B, et al. (2005) Colchicine treatment of alcoholic cirrhosis: A randomized, placebo-controlled clinical trial of patient survival. Gastroenterology 128: 882-890.
39. Pares A, Planas R, Torres M, Caballeria J, Viver JM, et al. (1998) Effects of silymarin in alcoholic patients with cirrhosis of the liver: results of a controlled, double-blind, randomized and multicenter trial. Journal of Hepatology 28: 615-621.
40. Hsu YC, Chiu YT, Cheng CC, Wu CF, Lin YL, et al. (2007) Antifibrotic effects of tetrandrine on hepatic stellate cells and rats with liver fibrosis. J Gastroenterol Hepatol 22: 99-111.
41. Chong LW, Hsu YC, Chiu YT, Yang KC, Huang YT, (2006) Anti-fibrotic effects of thalidomide on hepatic stellate cells and dimethylnitrosamine-intoxicated rats. J Biomed Sci 13: 403-418.
42. Lee SJ, Kim YG, Kang KW, Kim CW, Kim SG, (2004) Effects of colchicine on liver functions of cirrhotic rats: beneficial effects result from stellate cell inactivation and inhibition of TGF beta1 expression. Chem Biol Interact 147: 9-21.
43. Li GS, Jiang WL, Tian JW, Qu GW, Zhu HB, et al. (2010) In vitro and in vivo antifibrotic effects of rosmarinic acid on experimental liver fibrosis. Phytomedicine 17: 282-288.
44. Marek CJ, Tucker SJ, Konstantinou DK, Elrick LJ, Haefner D, et al. (2005) Pregnenolone-16alpha-carbonitrile inhibits rodent liver fibrogenesis via PXR (pregnane X receptor)-dependent and PXR-independent mechanisms. Biochem J 387: 601-608.
45. Dumont JM, Maignan MF, Janin B, Herbage D, Perrissoud D, (1986) Effect of malotilate on chronic liver injury induced by carbon tetrachloride in the rat. J Hepatol 3: 260-268.
46. Yuan GJ, Zhang ML, Gong ZJ, (2004) Effects of PPARg agonist pioglitazone on rat hepatic fibrosis. World J Gastroenterol 10: 1047-1051.
47. Tasci I, Mas MR, Vural SA, Deveci S, Comert B, et al. (2007) Pegylated interferon-alpha plus taurine in treatment of rat liver fibrosis. World J Gastroenterol 13: 3237-3244.
48. Tasci I, Mas N, Mas MR, Tuncer M, Comert B, (2008) Ultrastructural changes in hepatocytes after taurine treatment in CCl4 induced liver injury. World J Gastroenterol 14: 4897-4902.
49. Hong RT, Xu JM, Mei Q, (2009) Melatonin ameliorates experimental hepatic fibrosis induced by carbon tetrachloride in rats. World J Gastroenterol 15: 1452-1458.
50. Wu XL, Zeng WZ, Jiang MD, Qin JP, Xu H, (2008) Effect of Oxymatrine on the TGFbeta-Smad signaling pathway in rats with CCl4-induced hepatic fibrosis. World J Gastroenterol 14: 2100-2105.
51. Jeong DH, Lee GP, Jeong WI, Do SH, Yang HJ, et al. (2005) Alterations of mast cells and TGF-beta1 on the silymarin treatment for CCl(4)-induced hepatic fibrosis. World J Gastroenterol 11: 1141-1148.
52. Zhen MC, Wang Q, Huang XH, Cao LQ, Chen XL, et al. (2007) Green tea polyphenol epigallocatechin-3-gallate inhibits oxidative damage and preventive effects on carbon tetrachloride-induced hepatic fibrosis. J Nutr Biochem 18: 795-805.