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Chemical Compound Review

Ciglitazona     5-[[4-[(1-methylcyclohexyl) methoxy]phenyl]...

Synonyms: Ciglitizone, ciglitazone, Ciglitazonum, UPCMLD-DP145, CHEMBL7002, ...
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Disease relevance of ciglitazone


High impact information on ciglitazone

  • Focusing our studies on the beta/delta39 cells, we have demonstrated that C/EBPbeta along with C/EBPdelta in the presence of dexamethasone induces PPARgamma, adipsin, and aP2 mRNA production; however, GLUT4 mRNA is only expressed in cells exposed to ciglitazone [7].
  • The enhanced migration of DC in the knockout mice could be blocked in vivo by anti-CCR7 antibodies and by the drug Ciglitazone, known to inhibit CCR7 expression [8].
  • LNO2 activation of PPARgamma via CV-1 cell luciferase reporter gene expression analysis revealed a ligand activity that rivals or exceeds synthetic PPARgamma agonists such as rosiglitazone and ciglitazone, is coactivated by 9 cis-retinoic acid and is inhibited by the PPARgamma antagonist GW9662 [9].
  • In addition, 15d-PGJ(2) but not ciglitazone reduces expression of CD69 in human NK cells, whereas CD44 expression is not affected [10].
  • In PPARgamma-positive NK cells, PPAR-gamma activation by 15d-PGJ(2) and ciglitazone (a synthetic ligand) leads to reduction in both mRNA and protein levels of IFN-gamma [10].

Chemical compound and disease context of ciglitazone


Biological context of ciglitazone


Anatomical context of ciglitazone


Associations of ciglitazone with other chemical compounds


Gene context of ciglitazone


Analytical, diagnostic and therapeutic context of ciglitazone

  • Ciglitazone, 5-[4-(1-methylcyclohexylmethoxy) benzyl]-thiazolidine-2,4-dione, is a new hypoglycemic agent orally active in the obese-hyperglycemic animal models [24].
  • Ciglitazone also suppressed HIV-1 mRNA levels as measured by reverse transcriptase PCR, in parallel with the decrease in reverse transcriptase activity [3].
  • Interestingly, only Thy-1(-), but not Thy-1(+) subsets differentiated to lipofibroblasts, as determined by the accumulation of cytoplasmic lipid droplets after treatment with 15-deoxy-Delta(12, 14)-PGJ(2) or ciglitazone [25].
  • Oral administration of ciglitazone, approximately 45 mg/kg per day for 4 weeks, induced significant reductions in plasma insulin levels (p < 0.001) and blood pressure (p < 0.05) [26].
  • Using ciglitazone as the model compound, the mechanism of the antiproliferative effect of PPARgamma activators on MAPK and specific cell cycle regulatory proteins were examined by Western blot analysis and transfection studies [27].


  1. Regulation of retinoic acid receptor beta expression by peroxisome proliferator-activated receptor gamma ligands in cancer cells. James, S.Y., Lin, F., Kolluri, S.K., Dawson, M.I., Zhang, X.K. Cancer Res. (2003) [Pubmed]
  2. Glitazones differentially regulate primary astrocyte and glioma cell survival. Involvement of reactive oxygen species and peroxisome proliferator-activated receptor-gamma. Pérez-Ortiz, J.M., Tranque, P., Vaquero, C.F., Domingo, B., Molina, F., Calvo, S., Jordán, J., Ceña, V., Llopis, J. J. Biol. Chem. (2004) [Pubmed]
  3. Peroxisome proliferator-activated receptor gamma agonists inhibit HIV-1 replication in macrophages by transcriptional and post-transcriptional effects. Hayes, M.M., Lane, B.R., King, S.R., Markovitz, D.M., Coffey, M.J. J. Biol. Chem. (2002) [Pubmed]
  4. Peroxisome proliferator activator receptor-gamma ligands, 15-deoxy-Delta(12,14)-prostaglandin J2 and ciglitazone, reduce systemic inflammation in polymicrobial sepsis by modulation of signal transduction pathways. Zingarelli, B., Sheehan, M., Hake, P.W., O'Connor, M., Denenberg, A., Cook, J.A. J. Immunol. (2003) [Pubmed]
  5. Neutral lipids and peroxisome proliferator-activated receptor-{gamma} control pulmonary gene expression and inflammation-triggered pathogenesis in lysosomal acid lipase knockout mice. Lian, X., Yan, C., Qin, Y., Knox, L., Li, T., Du, H. Am. J. Pathol. (2005) [Pubmed]
  6. The synthetic peroxisome proliferator-activated receptor-gamma agonist ciglitazone attenuates neuroinflammation and accelerates encapsulation in bacterial brain abscesses. Kielian, T., Syed, M.M., Liu, S., Phulwani, N.K., Phillips, N., Wagoner, G., Drew, P.D., Esen, N. J. Immunol. (2008) [Pubmed]
  7. PPARgamma induces the insulin-dependent glucose transporter GLUT4 in the absence of C/EBPalpha during the conversion of 3T3 fibroblasts into adipocytes. Wu, Z., Xie, Y., Morrison, R.F., Bucher, N.L., Farmer, S.R. J. Clin. Invest. (1998) [Pubmed]
  8. Accelerated chemokine receptor 7-mediated dendritic cell migration in Runx3 knockout mice and the spontaneous development of asthma-like disease. Fainaru, O., Shseyov, D., Hantisteanu, S., Groner, Y. Proc. Natl. Acad. Sci. U.S.A. (2005) [Pubmed]
  9. Nitrolinoleic acid: an endogenous peroxisome proliferator-activated receptor gamma ligand. Schopfer, F.J., Lin, Y., Baker, P.R., Cui, T., Garcia-Barrio, M., Zhang, J., Chen, K., Chen, Y.E., Freeman, B.A. Proc. Natl. Acad. Sci. U.S.A. (2005) [Pubmed]
  10. Peroxisome proliferator-activated receptor-gamma and its ligands attenuate biologic functions of human natural killer cells. Zhang, X., Rodriguez-Galán, M.C., Subleski, J.J., Ortaldo, J.R., Hodge, D.L., Wang, J.M., Shimozato, O., Reynolds, D.A., Young, H.A. Blood (2004) [Pubmed]
  11. Inhibitors of the arachidonic acid pathway and peroxisome proliferator-activated receptor ligands have superadditive effects on lung cancer growth inhibition. Avis, I., Martínez, A., Tauler, J., Zudaire, E., Mayburd, A., Abu-Ghazaleh, R., Ondrey, F., Mulshine, J.L. Cancer Res. (2005) [Pubmed]
  12. Reduction of insulin resistance in obese and/or diabetic animals by 5-[4-(1-methylcyclohexylmethoxy)benzyl]-thiazolidine-2,4-dione (ADD-3878, U-63,287, ciglitazone), a new antidiabetic agent. Fujita, T., Sugiyama, Y., Taketomi, S., Sohda, T., Kawamatsu, Y., Iwatsuka, H., Suzuoki, Z. Diabetes (1983) [Pubmed]
  13. Peroxisome proliferator-activated receptor gamma-independent ablation of cyclin D1 by thiazolidinediones and their derivatives in breast cancer cells. Huang, J.W., Shiau, C.W., Yang, Y.T., Kulp, S.K., Chen, K.F., Brueggemeier, R.W., Shapiro, C.L., Chen, C.S. Mol. Pharmacol. (2005) [Pubmed]
  14. Stimulation of peroxisome proliferator-activated receptors alpha and gamma blocks HIV-1 replication and TNFalpha production in acutely infected primary blood cells, chronically infected U1 cells, and alveolar macrophages from HIV-infected subjects. Skolnik, P.R., Rabbi, M.F., Mathys, J.M., Greenberg, A.S. J. Acquir. Immune Defic. Syndr. (2002) [Pubmed]
  15. Delayed activation of PPARgamma by LPS and IFN-gamma attenuates the oxidative burst in macrophages. Von Knethen A, A., Brüne, B. FASEB J. (2001) [Pubmed]
  16. The Peroxisome Proliferator-Activated Receptor {gamma} (PPAR{gamma}) Ligands 15-Deoxy-{Delta}12,14-Prostaglandin J2 and Ciglitazone Induce Human B Lymphocyte and B Cell Lymphoma Apoptosis by PPAR{gamma}-Independent Mechanisms. Ray, D.M., Akbiyik, F., Phipps, R.P. J. Immunol. (2006) [Pubmed]
  17. Peroxisome proliferator-activated receptor gamma-independent activation of p38 MAPK by thiazolidinediones involves calcium/calmodulin-dependent protein kinase II and protein kinase R: correlation with endoplasmic reticulum stress. Gardner, O.S., Shiau, C.W., Chen, C.S., Graves, L.M. J. Biol. Chem. (2005) [Pubmed]
  18. MAP kinase cascades are activated in astrocytes and preadipocytes by 15-deoxy-Delta(12-14)-prostaglandin J(2) and the thiazolidinedione ciglitazone through peroxisome proliferator activator receptor gamma-independent mechanisms involving reactive oxygenated species. Lennon, A.M., Ramaugé, M., Dessouroux, A., Pierre, M. J. Biol. Chem. (2002) [Pubmed]
  19. Divergent effects of peroxisome proliferator-activated receptor gamma agonists and tumor necrosis factor alpha on adipocyte ApoE expression. Yue, L., Rasouli, N., Ranganathan, G., Kern, P.A., Mazzone, T. J. Biol. Chem. (2004) [Pubmed]
  20. Ciglitazone, a new hypoglycemic agent. II. Effect on glucose and lipid metabolisms and insulin binding in the adipose tissue of C57BL/6J-ob/ob and -+/? mice. Chang, A.Y., Wyse, B.M., Gilchrist, B.J. Diabetes (1983) [Pubmed]
  21. Dependence of peroxisome proliferator-activated receptor ligand-induced mitogen-activated protein kinase signaling on epidermal growth factor receptor transactivation. Gardner, O.S., Dewar, B.J., Earp, H.S., Samet, J.M., Graves, L.M. J. Biol. Chem. (2003) [Pubmed]
  22. Inhibition of IFN-gamma-mediated inducible nitric oxide synthase induction by the peroxisome proliferator-activated receptor gamma agonist, 15-deoxy-delta 12,14-prostaglandin J2, involves inhibition of the upstream Janus kinase/STAT1 signaling pathway. Chen, C.W., Chang, Y.H., Tsi, C.J., Lin, W.W. J. Immunol. (2003) [Pubmed]
  23. Superoxide anion-dependent Raf/MEK/ERK activation by peroxisome proliferator activated receptor gamma agonists 15-deoxy-delta(12,14)-prostaglandin J(2), ciglitazone, and GW1929. Huang, W.C., Chio, C.C., Chi, K.H., Wu, H.M., Lin, W.W. Exp. Cell Res. (2002) [Pubmed]
  24. Ciglitazone, a new hypoglycemic agent. I. Studies in ob/ob and db/db mice, diabetic Chinese hamsters, and normal and streptozotocin-diabetic rats. Chang, A.Y., Wyse, B.M., Gilchrist, B.J., Peterson, T., Diani, A.R. Diabetes (1983) [Pubmed]
  25. Thy-1 expression in human fibroblast subsets defines myofibroblastic or lipofibroblastic phenotypes. Koumas, L., Smith, T.J., Feldon, S., Blumberg, N., Phipps, R.P. Am. J. Pathol. (2003) [Pubmed]
  26. Effects of ciglitazone on blood pressure and intracellular calcium metabolism. Pershadsingh, H.A., Szollosi, J., Benson, S., Hyun, W.C., Feuerstein, B.G., Kurtz, T.W. Hypertension (1993) [Pubmed]
  27. PPARgamma ligand attenuates PDGF-induced mesangial cell proliferation: role of MAP kinase. Ghosh, S.S., Gehr, T.W., Ghosh, S., Fakhry, I., Sica, D.A., Lyall, V., Schoolwerth, A.C. Kidney Int. (2003) [Pubmed]
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