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Chemical Compound Review

celastrol     (4aR,6aS,6aR,14bR)-10- hydroxy-2,4a,6a,6a,9...

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Disease relevance of celastrol


Psychiatry related information on celastrol


High impact information on celastrol

  • Multiple assays using the animal tumor tissue samples from both early and end time points showed in vivo inhibition of the proteasomal activity and induction of apoptosis after Celastrol treatment [1].
  • Here, we report, for the first time, that Celastrol potently and preferentially inhibits the chymotrypsin-like activity of a purified 20S proteasome (IC(50) = 2.5 micromol/L) and human prostate cancer cellular 26S proteasome (at 1-5 micromol/L) [1].
  • Celastrol, an active compound extracted from the root bark of the Chinese medicine "Thunder of God Vine" (Tripterygium wilfordii Hook F.), was used for years as a natural remedy for inflammatory conditions [1].
  • Chronic inhibition of cardiac kir2.1 and HERG potassium channels by celastrol with dual effects on both ion conductivity and protein trafficking [5].
  • In contrast, celastrol has no effects on trafficking of either CD4 or CD8 membrane proteins [5].

Biological context of celastrol

  • Because the reduction of potassium channel activity is a common form of druginduced cardiotoxicity, the potent inhibition of cell surface expression by celastrol underscores a need to evaluate drug candidates for their chronic effects on biogenesis of potassium channels [5].
  • Celastrol can activate heat shock gene transcription synergistically with other stresses and exhibits cytoprotection against subsequent exposures to other forms of lethal cell stress [6].
  • We describe here characteristics of celastrol, a quinone methide triterpene and an active component from Chinese herbal medicine identified in a screen of bioactive small molecules that activates the human heat shock response [6].
  • Structural basis of potent antiperoxidation activity of the triterpene celastrol in mitochondria: effect of negative membrane surface charge on lipid peroxidation [7].
  • The anti-peroxidative effect of celastrol was very strong: its 50% inhibitory concentration was 7 microM, and it was about 15 times more effective than alpha-tocopherol [8].

Anatomical context of celastrol

  • Celastrol is suggested to inhibit the peroxidation of the outer and inner mitochondrial membrane by direct radical scavenging, and also to prevent the attack of oxygen radicals on the inner membrane by increasing its negative surface charge [7].
  • A 48% loss of dopaminergic neurons induced by MPTP in the substantia nigra pars compacta was significantly attenuated by celastrol treatment [9].
  • Quantitative-PCR and confocal analysis on a human monocytic cell line indicated that Celastrol acts at the transcriptional level by inhibiting LPS-induced NF-kappaB translocation [2].
  • In the present study, the effects of two isolated monomers from GTW, demethylzeylasteral and celastrol, on the Ca(2+) channels in mouse spermatogenic cells and on the sperm acrosome reaction were investigated by whole-cell patch-clamp recording and chlortetracycline staining methods, respectively [10].
  • In macrophage lineage cells and endothelial cells celastrol decreased induced but not constitutive NO production [3].

Associations of celastrol with other chemical compounds

  • Mice were treated with celastrol before and after injections of MPTP, a dopaminergic neurotoxin, which produces a model of PD [9].
  • Celastrol, a quinone methide triterpenoid, was isolated as an inhibitor of NF-kappaB from Celastrus orbiculatus [11].
  • The major terpenoid components, celastrol (6) and its methyl ester derivative, pristimerin (7), were significantly active against nine cancer cell lines, including A549, MCF-7, HCT-8, KB, KB-VIN, U-87-MG, PC-3, 1A9, and PTX10 cell lines, with ED(50) values ranging from 0.076 to 0.34 microg/mL [12].
  • A rapid, sensitive and reliable reverse-phase HPLC method (employing an external standard) was used for the determination of the cytotoxic triterpenoids, 20 alpha-hydroxymaytenin, 22 beta-hydroxymaytenin, maytenin, celastrol and pristimerin in each of the five types [13].

Gene context of celastrol


Analytical, diagnostic and therapeutic context of celastrol


  1. Celastrol, a triterpene extracted from the Chinese "Thunder of God Vine," is a potent proteasome inhibitor and suppresses human prostate cancer growth in nude mice. Yang, H., Chen, D., Cui, Q.C., Yuan, X., Dou, Q.P. Cancer Res. (2006) [Pubmed]
  2. Celastrol inhibits pro-inflammatory cytokine secretion in Crohn's disease biopsies. Pinna, G.F., Fiorucci, M., Reimund, J.M., Taquet, N., Arondel, Y., Muller, C.D. Biochem. Biophys. Res. Commun. (2004) [Pubmed]
  3. Celastrol, a potent antioxidant and anti-inflammatory drug, as a possible treatment for Alzheimer's disease. Allison, A.C., Cacabelos, R., Lombardi, V.R., Alvarez, X.A., Vigo, C. Prog. Neuropsychopharmacol. Biol. Psychiatry (2001) [Pubmed]
  4. Celastrol blocks neuronal cell death and extends life in transgenic mouse model of amyotrophic lateral sclerosis. Kiaei, M., Kipiani, K., Petri, S., Chen, J., Calingasan, N.Y., Beal, M.F. Neuro-degenerative diseases. (2005) [Pubmed]
  5. Chronic inhibition of cardiac kir2.1 and HERG potassium channels by celastrol with dual effects on both ion conductivity and protein trafficking. Sun, H., Liu, X., Xiong, Q., Shikano, S., Li, M. J. Biol. Chem. (2006) [Pubmed]
  6. Celastrols as inducers of the heat shock response and cytoprotection. Westerheide, S.D., Bosman, J.D., Mbadugha, B.N., Kawahara, T.L., Matsumoto, G., Kim, S., Gu, W., Devlin, J.P., Silverman, R.B., Morimoto, R.I. J. Biol. Chem. (2004) [Pubmed]
  7. Structural basis of potent antiperoxidation activity of the triterpene celastrol in mitochondria: effect of negative membrane surface charge on lipid peroxidation. Sassa, H., Kogure, K., Takaishi, Y., Terada, H. Free Radic. Biol. Med. (1994) [Pubmed]
  8. The triterpene celastrol as a very potent inhibitor of lipid peroxidation in mitochondria. Sassa, H., Takaishi, Y., Terada, H. Biochem. Biophys. Res. Commun. (1990) [Pubmed]
  9. Celastrol protects against MPTP- and 3-nitropropionic acid-induced neurotoxicity. Cleren, C., Calingasan, N.Y., Chen, J., Beal, M.F. J. Neurochem. (2005) [Pubmed]
  10. Effects of demethylzeylasteral and celastrol on spermatogenic cell Ca2+ channels and progesterone-induced sperm acrosome reaction. Bai, J.P., Shi, Y.L., Fang, X., Shi, Q.X. Eur. J. Pharmacol. (2003) [Pubmed]
  11. Inhibition of NF-kappaB activation through targeting IkappaB kinase by celastrol, a quinone methide triterpenoid. Lee, J.H., Koo, T.H., Yoon, H., Jung, H.S., Jin, H.Z., Lee, K., Hong, Y.S., Lee, J.J. Biochem. Pharmacol. (2006) [Pubmed]
  12. Antitumor agents. 228. five new agarofurans, Reissantins A-E, and cytotoxic principles from Reissantia buchananii. Chang, F.R., Hayashi, K., Chen, I.H., Liaw, C.C., Bastow, K.F., Nakanishi, Y., Nozaki, H., Cragg, G.M., Wu, Y.C., Lee, K.H. J. Nat. Prod. (2003) [Pubmed]
  13. Quantitative determination for cytotoxic Friedo-nor-oleanane derivatives from five morphological types of Maytenus ilicifolia (Celastraceae) by reverse-phase high-performance liquid chromatography. Buffa Filho, W., Corsino, J., Bolzani, d.a. .S.V., Furlan, M., Pereira, A.M., França, S.C. Phytochemical analysis : PCA. (2002) [Pubmed]
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