Celastrol, a potent antioxidant and anti-inflammatory drug, as a possible treatment for Alzheimer's disease

Allison, A. C.; Cacabelos, Ramón; Lombardi, Valter; Alvarez, X.A.; Vigo, Carmen

doi:10.1016/s0278-5846(01)00192-0

Cited by 331 publications

(254 citation statements)

References 24 publications

Supporting

Mentioning

247

Contrasting

Unclassified

Order By: Relevance

“…The compound produced some improvement in indicators of learning and memory in rats. These results suggested that 65 might be useful as a treatment for Alzheimer's (Allison et al, 2001). …”

Section: Neurodegenerative Diseasesmentioning

confidence: 90%

“…Celastrol (65) lowered production of both PGE 2 (Xu et al, 1991) and induced NO (Allison et al, 2001;Jin et al, 2002). However, in a mouse model of lupus, 65 increased levels of matrix metalloproteases-1 and -2 .…”

Section: Proinflammatory Enzymesmentioning

confidence: 99%

“…Proinflammatory cytokines and lymphocytes: Celastrol (65) has been found to reduce levels of cytokines including IL-1α and IL-1β (Lei and Li, 1991;Li et al, 1997;Takaishi et al, 1997;Huang et al, 1998), IL-2 (Lei and Li, 1991;Xu et al, 1991;Li et al, 1997), IL-6, IL-8 (He et al, 1998;Pinna et al, 2004), and TNF-α (Allison et al, 2001;Pinna et al, 2004). It also reduced antibody formation in mice (Lei and Li, 1991).…”

mentioning

confidence: 99%

See 2 more Smart Citations

Medicinal chemistry and pharmacology of genus Tripterygium (Celastraceae)

et al. 2007

View full text Add to dashboard Cite

Plants in the genus Tripterygium, such as Tripterygium wilfordii Hook. f., have a long history of use in traditional Chinese medicine. In recent years there has been considerable interest in the use of Tripterygium extracts and of the main bioactive constituent, the diterpene triepoxide triptolide (1), to treat a variety of autoimmune and inflammation-related conditions. The main mode of action of the Tripterygium extracts and triptolide (1) is the inhibition of expression of proinflammatory genes such as those for interleukin-2 (IL-2), inducible nitric oxide synthase (iNOS), tumor necrosis factor-α (TNF-α), cyclooxygenase-2 (COX-2) and interferon-gamma (IFN-γ). The efficacy and safety of certain types of Tripterygium extracts were confirmed in human clinical trials in the US and abroad. Over 300 compounds have been identified in the genus Tripterygium, and many of these have been evaluated for biological activity. The overall activity of the extract is based on the interaction between its components. Therefore, the safety and efficacy of the extract cannot be fully mimicked by any individual constituent. This review discusses the biochemical composition and biological and pharmacological activities of Tripterygium extracts, and their main bioactive components.

show abstract

“…The compound produced some improvement in indicators of learning and memory in rats. These results suggested that 65 might be useful as a treatment for Alzheimer's (Allison et al, 2001). …”

Section: Neurodegenerative Diseasesmentioning

confidence: 90%

Section: Proinflammatory Enzymesmentioning

confidence: 99%

mentioning

confidence: 99%

See 1 more Smart Citation

Medicinal chemistry and pharmacology of genus Tripterygium (Celastraceae)

et al. 2007

View full text Add to dashboard Cite

show abstract

“…2 Celastrol, a triterpenoid from the Celastracae family and extracted from the plant Tripterygium wilfordii, 3 has attracted interest, especially for its potential anti-inflammatory effects. 4 The in vivo anti-inflammatory effects of this triterpene have been demonstrated in animal models of collagen-induced arthritis, 5 Alzheimer disease, 6 asthma, 7 systemic lupus erythematosus, 8,9 and rheumatoid arthritis. 10 Celastrol is also known to inhibit the proliferation of a variety of tumor cells, including those from leukemia, 11 gliomas, 12 and prostate cancer.…”

Section: Introductionmentioning

confidence: 99%

“…10 Celastrol is also known to inhibit the proliferation of a variety of tumor cells, including those from leukemia, 11 gliomas, 12 and prostate cancer. 13 The ability of celastrol to modulate the expression of proinflammatory cytokines, 3,14,15 MHC-II antigen, 6 inducible nitric oxide (NO) synthase (iNOS), 16 adhesion molecules in endothelial cells, 17 proteasome activity, 13 topoisomerase II, 11 potassium channels, 18 and heat shock response 19 has been reported. However, the molecular mechanism underlying the anti-inflammatory and antiproliferative effects of celastrol is not yet fully understood.…”

Section: Introductionmentioning

confidence: 99%

Celastrol, a novel triterpene, potentiates TNF-induced apoptosis and suppresses invasion of tumor cells by inhibiting NF-κB–regulated gene products and TAK1-mediated NF-κB activation

Sethi

Ahn

Pandey

et al. 2006

Blood

299

239

View full text Add to dashboard Cite

Celastrol, a quinone methide triterpene derived from the medicinal plant Tripterygium wilfordii, has been used to treat chronic inflammatory and autoimmune diseases, but its mechanism is not well understood. Therefore, we investigated the effects of celastrol on cellular responses activated by TNF, a potent proinflammatory cytokine. Celastrol potentiated the apoptosis induced by TNF and chemotherapeutic agents and inhibited invasion, both regulated by NF-B activation. We found that TNF induced the expression of gene products involved in antiapoptosis (IAP1, IAP2, Bcl-2, Bcl-X L , c-FLIP, and survivin), proliferation (cyclin D1 and COX-2), invasion (MMP-9), and angiogenesis (VEGF) and that celastrol treatment suppressed their expression. Because these gene products are regulated by NF-B, we postulated that celastrol mediates its effects by modulating the NF-B pathway. We found that celastrol suppressed both inducible and constitutive NF-B activation. Celastrol was found to inhibit the TNF-induced activation of I B␣ kinase, I B␣ phosphorylation, I B␣ degradation, p65 nuclear trans- IntroductionModern targeted therapies for most chronic illnesses, including cancer, have been mostly unsuccessful because of their ineffectiveness, lack of safety, and cost. Although monotherapy was advocated at one time, recent experience indicates that agents that target multiple pathways have more potential in cancer treatment. This understanding has led to combination therapy. Although traditional therapies have been around for thousands of years, their active components and their mechanisms of action remain undefined. Identification of an active chemical entity and its molecular targets can lead to rediscovery of the clinical potential of such therapies, as in the case of paclitaxel, derived from Taxus (yew) species during a random screening of US Department of Agriculture collection of plants. 1 Celastrol, also known as tripterine, is one such compound that was originally identified from traditional Chinese medicine ("God of Thunder Vine") almost 3 decades ago and used for the treatment of cancer and other inflammatory diseases. 2 Celastrol, a triterpenoid from the Celastracae family and extracted from the plant Tripterygium wilfordii, 3 has attracted interest, especially for its potential anti-inflammatory effects. 4 The in vivo anti-inflammatory effects of this triterpene have been demonstrated in animal models of collagen-induced arthritis, 5 Alzheimer disease, 6 asthma, 7 systemic lupus erythematosus, 8,9 and rheumatoid arthritis. 10 Celastrol is also known to inhibit the proliferation of a variety of tumor cells, including those from leukemia, 11 gliomas, 12 and prostate cancer. 13 The ability of celastrol to modulate the expression of proinflammatory cytokines, 3,14,15 6 inducible nitric oxide (NO) synthase (iNOS), 16 adhesion molecules in endothelial cells, 17 proteasome activity, 13 topoisomerase II, 11 potassium channels, 18 and heat shock response 19 has been reported. However, the molecular mechanism underlying the ...

show abstract

Antiaging Agents

Cottam¹

2003

Kirk-Othmer Encyclopedia of Chemical Technology

View full text Add to dashboard Cite

The aging process in humans is extremely complex with many factors undoubtedly involved to some degree including environmental, dietary, and genetic influences. The process can be described as a physical decline and involves the buildup of cellular and molecular damage that increases our susceptibility to disease and infirmity as we grow older. The current view of scientists is that random damage that occurs within cells and among extracellular molecules is responsible for many of the age‐related changes that are observed in organisms. Molecular disorder occurs and accumulates within cells and their products because this occurrence outpaces the cell's repair mechanisms. This article summarizes recent literature reports of research efforts directed toward intervention in the aging process as well as changes and diseases associated with the aging process involving all the major organ systems in humans. Consideration is given to pharmacological treatment and prevention of such age‐related changes and conditions.

show abstract

Celastrol, a potent antioxidant and anti-inflammatory drug, as a possible treatment for Alzheimer's disease

Cited by 331 publications

References 24 publications

Medicinal chemistry and pharmacology of genus Tripterygium (Celastraceae)

Medicinal chemistry and pharmacology of genus Tripterygium (Celastraceae)

Celastrol, a novel triterpene, potentiates TNF-induced apoptosis and suppresses invasion of tumor cells by inhibiting NF-κB–regulated gene products and TAK1-mediated NF-κB activation

Antiaging Agents

Contact Info

Product

Resources

About