Tripterin (Celastrol) is a proteasome inhibitor which potently and preferentially inhibits the chymotrypsin-like activity of a purified 20S proteasome with IC50 of 2.5 μM. Celastrol down-regulated the basal and DNA damaging agents-induced monoubiquitination of FANCD2, followed by proteolytic degradation. Celastrol treatment abrogated the G2 checkpoint induced by IR,and enhanced the ICL agents-induced DNA damage and inhibitory effects on lung cancer cells through depletion of FANCD2.Celastrol presented striking growth inhibition and apoptosis induction potency on DU145 cells in vitro in a time- and dose-dependent manner.Celastrol exhibits its antiprostate cancer effects partially through the downregulation of the expression level of hERG channel in DU145 cells,suggesting that celastrol may be a potential agent against prostate cancer with a mechanism of blocking the hERG channel.Celastrol ameliorates experimental colitis in IL-10 deficient mice via the up-regulation of autophagy by suppressing the PI3K/Akt/mTOR signaling pathway.Celastrol has the potential to inhibit cytochrome P450 activities and may cause the herb-drug interactions.Celastrol induces apoptosis in TNBC cells and indicated that apoptosis might be mediated through mitochondrial dysfunction and PI3K/Akt signaling pathway.
Front Microbiol. 2023 Mar 2;14:1120048.
Specific TLR-mediated HSP70 activation plays a potential role in host defense against the intestinal parasite Giardia duodenalis
Celastrol (Tripterin) purchased from AbMole
| Cell Experiment | |
|---|---|
| Cell lines | RPMI 8226, KATOIII, UM-SCC1, U251MG and MDA-MB-231 cells |
| Preparation method | Determining the anti-proliferative effect of celastrol on various human tumor cell lines by the MTT uptake method. Briefly, incubating 5×103 cells with Celastrol in triplicate in a 96-well plate at 37 ℃. Then adding MTT solution to each well. After a 2 hours incubation at 37 ℃, adding extraction buffer (20% SDS, 50% dimethylformamide) , incubating cells overnight at 37 ℃, and then measuring the optical density at 570 nm using a Tecan plate reader. |
| Concentrations | ~5 μM |
| Incubation time | 2 hours |
| Animal Experiment | |
|---|---|
| Animal models | nude mice bearing C4-2B tumors |
| Formulation | 10% DMSO, 70% Cremophor/ethanol (3:1), and 20% PBS |
| Dosages | 3 mg/kg |
| Administration | Intraperitoneal injection |
| Molecular Weight | 450.61 |
| Formula | C29H38O4 |
| CAS Number | 34157-83-0 |
| Solubility (25°C) | DMSO ≥ 30 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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