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Chemical Compound Review

Guggulsterone     (8R,9S,10R,13S,14S,17E)-17- ethylidene-10...

Synonyms: E-Guggulsteron, CHEMBL402063, CHEMBL410683, SureCN1650063, G5168_SIGMA, ...
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Disease relevance of Guggulsterones E


High impact information on Guggulsterones E

  • Guggulsterone suppressed DNA binding of NF-kappaB induced by tumor necrosis factor (TNF), phorbol ester, okadaic acid, cigarette smoke condensate, hydrogen peroxide, and interleukin-1 [1].
  • Guggulsterone inhibits NF-kappaB and IkappaBalpha kinase activation, suppresses expression of anti-apoptotic gene products, and enhances apoptosis [1].
  • Guggulsterone is a farnesoid X receptor antagonist in coactivator association assays but acts to enhance transcription of bile salt export pump [7].
  • Collectively, our results indicate that guggulsterone suppresses RANKL and tumor cell-induced osteoclastogenesis by suppressing the activation of NF-kappaB [2].
  • Guggulsterone also suppressed the differentiation of monocytes to osteoclasts in a dose-dependent and time-dependent manner [2].

Biological context of Guggulsterones E


Anatomical context of Guggulsterones E


Associations of Guggulsterones E with other chemical compounds


Gene context of Guggulsterones E


Analytical, diagnostic and therapeutic context of Guggulsterones E


  1. Guggulsterone inhibits NF-kappaB and IkappaBalpha kinase activation, suppresses expression of anti-apoptotic gene products, and enhances apoptosis. Shishodia, S., Aggarwal, B.B. J. Biol. Chem. (2004) [Pubmed]
  2. Guggulsterone inhibits osteoclastogenesis induced by receptor activator of nuclear factor-kappaB ligand and by tumor cells by suppressing nuclear factor-kappaB activation. Ichikawa, H., Aggarwal, B.B. Clin. Cancer Res. (2006) [Pubmed]
  3. The hypolipidemic natural product guggulsterone is a promiscuous steroid receptor ligand. Burris, T.P., Montrose, C., Houck, K.A., Osborne, H.E., Bocchinfuso, W.P., Yaden, B.C., Cheng, C.C., Zink, R.W., Barr, R.J., Hepler, C.D., Krishnan, V., Bullock, H.A., Burris, L.L., Galvin, R.J., Bramlett, K., Stayrook, K.R. Mol. Pharmacol. (2005) [Pubmed]
  4. The hypolipidemic natural product Commiphora mukul and its component guggulsterone inhibit oxidative modification of LDL. Wang, X., Greilberger, J., Ledinski, G., Kager, G., Paigen, B., Jürgens, G. Atherosclerosis (2004) [Pubmed]
  5. Caspase-dependent apoptosis induction by guggulsterone, a constituent of Ayurvedic medicinal plant Commiphora mukul, in PC-3 human prostate cancer cells is mediated by Bax and Bak. Singh, S.V., Zeng, Y., Xiao, D., Vogel, V.G., Nelson, J.B., Dhir, R., Tripathi, Y.B. Mol. Cancer Ther. (2005) [Pubmed]
  6. Guggulsterone-induced apoptosis in human prostate cancer cells is caused by reactive oxygen intermediate dependent activation of c-Jun NH2-terminal kinase. Singh, S.V., Choi, S., Zeng, Y., Hahm, E.R., Xiao, D. Cancer Res. (2007) [Pubmed]
  7. Guggulsterone is a farnesoid X receptor antagonist in coactivator association assays but acts to enhance transcription of bile salt export pump. Cui, J., Huang, L., Zhao, A., Lew, J.L., Yu, J., Sahoo, S., Meinke, P.T., Royo, I., Pelaez, F., Wright, S.D. J. Biol. Chem. (2003) [Pubmed]
  8. The ratio of constitutive androstane receptor to pregnane X receptor determines the activity of guggulsterone against the Cyp2b10 promoter. Ding, X., Staudinger, J.L. J. Pharmacol. Exp. Ther. (2005) [Pubmed]
  9. Bile acid signaling through FXR induces intracellular adhesion molecule-1 expression in mouse liver and human hepatocytes. Qin, P., Borges-Marcucci, L.A., Evans, M.J., Harnish, D.C. Am. J. Physiol. Gastrointest. Liver Physiol. (2005) [Pubmed]
  10. Guggulsterone activates multiple nuclear receptors and induces CYP3A gene expression through the pregnane X receptor. Brobst, D.E., Ding, X., Creech, K.L., Goodwin, B., Kelley, B., Staudinger, J.L. J. Pharmacol. Exp. Ther. (2004) [Pubmed]
  11. HPTLC method for guggulsterone. II. Stress degradation studies on guggulsterone. Agrawal, H., Kaul, N., Paradkar, A.R., Mahadik, K.R. Journal of pharmaceutical and biomedical analysis. (2004) [Pubmed]
  12. Thyroid stimulatory action of (Z)-guggulsterone: mechanism of action. Tripathi, Y.B., Tripathi, P., Malhotra, O.P., Tripathi, S.N. Planta Med. (1988) [Pubmed]
  13. Stimulation of low density lipoprotein receptor activity in liver membrane of guggulsterone treated rats. Singh, V., Kaul, S., Chander, R., Kapoor, N.K. Pharmacol. Res. (1990) [Pubmed]
  14. A natural product ligand of the oxysterol receptor, liver X receptor. Bramlett, K.S., Houck, K.A., Borchert, K.M., Dowless, M.S., Kulanthaivel, P., Zhang, Y., Beyer, T.P., Schmidt, R., Thomas, J.S., Michael, L.F., Barr, R., Montrose, C., Eacho, P.I., Cao, G., Burris, T.P. J. Pharmacol. Exp. Ther. (2003) [Pubmed]
  15. A natural product that lowers cholesterol as an antagonist ligand for FXR. Urizar, N.L., Liverman, A.B., Dodds, D.T., Silva, F.V., Ordentlich, P., Yan, Y., Gonzalez, F.J., Heyman, R.A., Mangelsdorf, D.J., Moore, D.D. Science (2002) [Pubmed]
  16. Simultaneous determination of the stereoisomers of guggulsterone in serum by high-performance liquid chromatography. Verma, N., Singh, S.K., Gupta, R.C. J. Chromatogr. B Biomed. Sci. Appl. (1998) [Pubmed]
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