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| Product Name | Celastrol bulk powder |
| Synonyms | Tripterine;Tripterin |
| Botanical source | The God Vine(Tripterygium wilfordii hook.f) |
| CAS NO. | 34157-83-0 |
| Molecular Formula | C29H38O4 |
| Molecular Weight | 450.6g/mol |
| Appearance | Reddish orange crystal powder |
| Specification | 98% |
| Solubility | Soluble in organic solvents such as methanol and ethanol |
| Benefits | Anti-inflammatory, anti-obesity, Neuroprotection, anti-tumor |
What is Tripterygii Radix?
Celastrol Powder is the active ingredient in Tripterygii Radix, which is the dry root and rhizome of the God Vine. There are four species in total, namely Tripterygium wilfordii Hook.f, Tripterygium hypoglaucum Hutch, Tripterygium regelii Sprague et Takeda, and Tripterygium forresti Dicls.
Tripterygium wilfordii Hook. f. and its subspecies Tripterygium hypoglaucum Hutch are mainly used clinically in China. Lei Gong Teng is mainly distributed in Zhejiang, Fujian, Anhui, Jiangxi, Hunan, Taiwan, and other provinces south of the Yangtze River in China.
Radix Tripterygium wilfordii Hook F main active ingredient
Diterpenoids: triptolide(cas no.38748-32-2), Tripdiolide( cas no.38647-10-8), etc.
Triterpenoids: Celastrol(cas no.34157-83-0), Wilforlide A(cas no.84104-71-2), etc.
Alkaloids:Wilforgine(cas no.37239-47-7), Wolverine (cas no.11088-09-8), wilforidine, etc.
What is Celastrol?
Celastrol (Cel) is a highly active pentacyclic triterpene isolated from Lei Gong Teng, which has a variety of pharmacological activities, such as anti-inflammatory, immunosuppressive, anti-obesity, neuron protection, and anti-tumor activities.
Tripterine was listed as one of the five natural products most likely to be developed into medicine by the top international journal Cell in 2007.
In 2015, the Umut Ozcan team at Harvard University reported in Cell that research found that Celastrol could significantly reduce the weight of obese mice by increasing the sensitivity of leptin, reducing food intake, and becoming a potential new drug for weight loss, which attracted much attention.
Pharmacological effects of Celastrol
Anti-inflammation and immunosuppression
Plant extract Celastrol powder has already been used in clinical trials for inflammatory illnesses.
A randomized clinical trial showed that Tripterygium wilfordii Hook F(TwHF) is a suitable option for improving Psoriasis Vulgaris.115 patients were all enrolled (58 TwHF; 57 acitretin). The median PASI score increased in both the TwHF and acitretin groups by 50.4% and 42.7%, respectively.
Efficacy of Tripterygium wilfordii Hook F and acitretin. (a) PASI 25 response; (b) PASI 50 response; (c) PASI 75 response; (d) Percentage PASI improvement.
At week 8, the aspartate transaminase and triglyceride levels in the TwHF group were significantly higher than at baseline (P = 0.026 and P = 0.011, respectively).
Celastrol for Rheumatoid Arthritis
The anti-inflammatory properties of celastrol in this condition have so far been attributed to the following:
(i) regulation of cytokine and chemokine production;
(ii) regulation of inflammatory mediators’ expression;
(iii) modulation of inflammatory cell functions;
(iv) osteoclast modulation and bone damage control
Anti-obesity
In hyperleptinemic diet-induced obese (DIO) mice, control reduces food intake, prevents the decrease in energy expenditure, and causes up to 45% weight loss by raising leptin sensitivity.
By overexpressing the anorectic peptides proopioid melanocortin (POMC) and orexin [neuropeptide Y (NPY)/AgRP], celastrol can increase leptin sensitivity and restore leptin signaling in neurons.
Celastrol can improve mitochondrial function and HSF-1, a regulator of energy expenditure, through activating PGC1-dependent metabolic pathways in adipose tissue and muscle.
These findings indicate Celastrol’s ability to decrease obesity by enhancing leptin sensitivity.
Neuroprotection
Celastrol is a promising neuroprotective agent, such as Parkinson’s disease, Huntington’s disease, Alzheimer’s disease, and amyotrophic lateral sclerosis.
Celastrol induces a broader range of potentially neuroprotective HSPs in differentiated human neurons, including induction of HSP70.
Inhibits inflammation by binding to the regulatory NF-kappa-B essential modulator (NEMO) unit in the IKK complex, thereby reducing its activation; binds to TNF receptor-associated factor 6 (TRAF6) and suppresses multiple immune responses.
Therefore, celastrol has beneficial effects not only in neurodegenerative but also in inflammatory diseases.
Antineoplastic
Celastrol’s anticancer effects are related to its activation of cell death, suppression of angiogenesis, treatment, radiotherapy sensitizing action, and anti-invasive effect.
Celastrol’s ability to prevent HSP90 from interacting with its co-chaperone Cdc37 in pancreatic cancer cells causes it to inhibit HSP90.
Interacting with Cdc37 separates the HSP90-Cdc37 complex, possibly suppressing some carcinogenic proteins.
Bioavailability of Celastrol
The solubility of celastrol in water is low (13.25 0.83 mg/ml at 37℃). When Qi et al. (193) investigated the solubility of celastrol in several vehicles, they found that ethyl oleate, olive oil, the surfactants Labrasol and OP-10, and the cosurfactants PEG200, ethanol, butanol, and notably Transcutol P were suitable solvents with a solubility >20 mg/ml.
Celastrol-loaded lipid nanospheres, liposomal celastrol, and solid self-micro emulsifying dispersible celastrol tablets can significantly increase their oral bioavailability, effectiveness, and side effects.
Despite encouraging results from both in vitro and in vivo testing, no celastrol product has completed the research and entered the market.
Toxicity and dosage of Celastrol
The dose and toxicity of celastrol vary; mouse data at 3 mg/kg showed adverse events and 27% mortality, although other trials at this dose showed no harmful effects.
Additionally, studies have indicated an LD50 level of 20.5 mg/kg and a 40% fatality rate of 4 mg/kg. An extensive fresh study is also necessary for more exact data.
