3-hydroxy-24-nor-2-oxo-1(10),3,5,7-friedelatetraen-29-oic acid, celastrol, tripterin, tripterine
| Name | Celastrol | ||
| PubChem CID | 122724 | ||
| Molecular Weight | 450.6g/mol | ||
| Synonyms |
3-hydroxy-24-nor-2-oxo-1(10),3,5,7-friedelatetraen-29-oic acid, celastrol, tripterin, tripterine |
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| Formula | C₂₉H₃₈O₄ | ||
| SMILES | CC1=C(C(=O)C=C2C1=CC=C3C2(CCC4(C3(CCC5(C4CC(CC5)(C)C(=O)O)C)C)C)C)O | ||
| InChI | 1S/C29H38O4/c1-17-18-7-8-21-27(4,19(18)15-20(30)23(17)31)12-14-29(6)22-16-26(3,24(32)33)10-9-25(22,2)11-13-28(21,29)5/h7-8,15,22,31H,9-14,16H2,1-6H3,(H,32,33)/t22-,25-,26-,27+,28-,29+/m1/s1 | ||
| InChIKey | KQJSQWZMSAGSHN-JJWQIEBTSA-N | ||
| CAS Number | 34157-83-0 | ||
| ChEMBL ID | CHEMBL301982 | ||
| ChEBI ID | CHEBI:63959 | ||
| Herb ID | HBIN020031 | ||
| Structure | 
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Download
2D
MOL
3D
MOL
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| Chineses Pinyin | LeiGongTeng | ||
| Use Part | Root, Leaf, Flower | ||
| Habitat | HuNan, JiangXi, ZheJiang, FuJian, GuangDong, GuiZhou, YunNan, HaiNan, XiZang, TaiWan, ChongQing | ||
| Flavor | Pungent, Bitter | ||
| Meridian Tropism | Heart, Liver | ||
| Species |
>Kingdom: Viridiplantae
-->Phylum: Streptophyta
-->Class: Equisetopsida
-->Order: Celastrales
-->Family: Celastraceae
-->Genus: Tripterygium
-->Species: Tripterygium wilfordii
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| Chineses Pinyin | NanSheTeng | ||
| Use Part | Stem Vine | ||
| Habitat | China | ||
| Flavor | Bitter, Pungent | ||
| Meridian Tropism | Liver, Bladder | ||
| Species |
>Kingdom: Viridiplantae
-->Phylum: Streptophyta
-->Class: Equisetopsida
-->Order: Celastrales
-->Family: Celastraceae
-->Genus: Celastrus
-->Species: Celastrus orbiculatus
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| Pair Name | Celastrol, Histone deacetylase inhibitor | |||
| Partner Name | Histone deacetylase inhibitor | |||
| Disease Info | [ICD-11: 2C25] | Lung cancer | Investigative | |
| Gene Regulation | Up-regulation | Acetylation | H4K16 | KEGG ID N.A. |
| In Vitro Model | A-549 | Lung adenocarcinoma | Homo sapiens (Human) | CVCL_0023 |
| NCI-H1299 | Lung large cell carcinoma | Homo sapiens (Human) | CVCL_0060 | |
| LL/2 (LLC1) | Malignant tumors of the mouse pulmonary system | Mus musculus (Mouse) | CVCL_4358 | |
| HeLa | Human papillomavirus-related cervical adenocarcinoma | Homo sapiens (Human) | CVCL_0030 | |
| Result | Celastrol treatment significantly enhanced the suppressive effects of HDACi on lung cancer cell allografts in mice, with significant H4K16ac upregulation, indicating that a combination of celastrol and HDACi is a potential novel therapeutic approach for patients with lung cancer. | |||
| Pair Name | Celastrol, Tamoxifen | |||
| Partner Name | Tamoxifen | |||
| Disease Info | [ICD-11: 2C60] | Breast cancer | Investigative | |
| Biological Phenomena | Induction-->Blockade of cell cycle in G0/G1 phase | |||
| Gene Regulation | Down-regulation | Phosphorylation | AKT1 | hsa207 |
| Up-regulation | Expression | MAP1LC3B | hsa81631 | |
| Down-regulation | Phosphorylation | MTOR | hsa2475 | |
| Up-regulation | Expression | SQSTM1 | hsa8878 | |
| In Vitro Model | MCF-7 | Invasive breast carcinoma of no special type | Homo sapiens (Human) | CVCL_0031 |
| Result | The Synergistic Effects of Celastrol in combination with Tamoxifen on Apoptosis and Autophagy in MCF-7 Cells | |||
| Pair Name | Celastrol, Docetaxel | |||
| Partner Name | Docetaxel | |||
| Disease Info | [ICD-11: 2C60] | Breast cancer | Investigative | |
| Biological Phenomena | Inhibition-->Cell metastasis | |||
| Gene Regulation | Down-regulation | Expression | CBLL1 | hsa79872 |
| Up-regulation | Expression | CDH1 | hsa999 | |
| In Vitro Model | MDA-MB-231 | Breast adenocarcinoma | Homo sapiens (Human) | CVCL_0062 |
| MDA-MB-468 | Breast adenocarcinoma | Homo sapiens (Human) | CVCL_0419 | |
| Result | Our results showing anti-migratory/anti-invasive effects of celastrol and associated mechanisms provide new evidence for the development of celastrol as a potential anti-metastatic compound against highly aggressive breast cancer, and celastrol in combination with docetaxel might potentially be used as a novel regimen for the treatment of TNBC. | |||
| Pair Name | Celastrol, Afatinib | |||
| Partner Name | Afatinib | |||
| Disease Info | [ICD-11: 2C25] | Lung cancer | Investigative | |
| Biological Phenomena | Induction-->Paraptosis | |||
| In Vitro Model | NCI-H23 | Lung adenocarcinoma | Homo sapiens (Human) | CVCL_1547 |
| NCI-H292 | Lung mucoepidermoid carcinoma | Homo sapiens (Human) | CVCL_0455 | |
| Result | These findings suggest that the depletion of intracellular glutathione by quercetin and sulforaphane could strengthen the anti-cancer efficacy of oxaliplatin. | |||
| Pair Name | Celastrol, TNF-related apoptosis inducing ligand | |||
| Partner Name | TNF-related apoptosis inducing ligand | |||
| Disease Info | [ICD-11: 2C25] | Lung cancer | Investigative | |
| Biological Phenomena | Induction-->Apoptosis | |||
| Gene Regulation | Up-regulation | Activity | CASP3 | hsa836 |
| Up-regulation | Activity | CASP8 | hsa841 | |
| Up-regulation | Expression | MAP1LC3A | hsa84557 | |
| Up-regulation | Expression | SQSTM1 | hsa8878 | |
| In Vitro Model | A-549 | Lung adenocarcinoma | Homo sapiens (Human) | CVCL_0023 |
| HCC15 | Lung squamous cell carcinoma | Homo sapiens (Human) | CVCL_2057 | |
| Calu-3 | Lung adenocarcinoma | Homo sapiens (Human) | CVCL_0609 | |
| Result | The combined use of TRAIL with celastrol may serve as a safe and adequate therapeutic technique for the treatment of TRAIL‑resistant lung cancer, suggesting that celastrol‑mediated autophagy flux inhibition sensitized TRAIL‑initiated apoptosis via regulation of ROS and ΔΨm. | |||
| Pair Name | Celastrol, TNF-related apoptosis inducing ligand | |||
| Partner Name | TNF-related apoptosis inducing ligand | |||
| Disease Info | [ICD-11: 2A00] | Glioblastoma multiforme | Investigative | |
| Biological Phenomena | Induction-->Apoptosis | |||
| Gene Regulation | Up-regulation | Cleavage | CASP3 | hsa836 |
| Up-regulation | Cleavage | CASP8 | hsa841 | |
| Up-regulation | Cleavage | PARP1 | hsa142 | |
| In Vitro Model | U-87MG ATCC | Glioblastoma | Homo sapiens (Human) | CVCL_0022 |
| U-251MG | Astrocytoma | Homo sapiens (Human) | CVCL_0021 | |
| LN-229 | Glioblastoma | Homo sapiens (Human) | CVCL_0393 | |
| Result | The results of our study demonstrate that celastrol sensitizes glioma cells to TRAIL via the death receptor pathway and that DR5 plays an important role in the effects of this cotreatment. The results indicate that this cotreatment is a promising tumor-killing therapeutic strategy with high efficacy and low toxicity. | |||
| Pair Name | Celastrol, Tamoxifen | |||
| Partner Name | Tamoxifen | |||
| Disease Info | [ICD-11: 2C60] | Breast cancer | Investigative | |
| Biological Phenomena | Induction-->Mitochondria-mediated apoptosis | |||
| Gene Regulation | Up-regulation | Expression | BAX | hsa581 |
| Down-regulation | Expression | BCL2 | hsa596 | |
| Up-regulation | Cleavage | CASP3 | hsa836 | |
| Up-regulation | Expression | CYCS | hsa54205 | |
| In Vitro Model | MDA-MB-231 | Breast adenocarcinoma | Homo sapiens (Human) | CVCL_0062 |
| In Vivo Model | The cell concentration was adjusted to 4×10⁷ pieces/mL. The single cell suspension was injected under the fourth pair of breast pads on the right side of nude mice, 0.1 mL for each. | |||
| Result | CEL can promote apoptosis and enhance the TAM sensitivity in TNBC treatment through a mitochondria-mediated pathway. | |||
| Pair Name | Celastrol, Cisplatin | |||
| Partner Name | Cisplatin | |||
| Disease Info | [ICD-11: 2B72] | Gastric cancer | Investigative | |
| Biological Phenomena | Induction-->Apoptosis | |||
| Gene Regulation | Down-regulation | Expression | ABCB1 | hsa5243 |
| Down-regulation | Expression | ABCC1 | hsa4363 | |
| Down-regulation | Expression | ABCG2 | hsa9429 | |
| Down-regulation | Expression | MTOR | hsa2475 | |
| In Vitro Model | SGC-7901 | Human papillomavirus-related cervical adenocarcinoma | Homo sapiens (Human) | CVCL_0520 |
| Result | Celastrol can inhibit the proliferation of the SGC7901/DDP cells, induce their apoptosis, and reduce the expression of drug resistance genes, probably by inhibiting the expression of the proteins related to the mTOR signaling pathway | |||
| No. | Title | Href |
|---|---|---|
| 1 | Celastrol inhibits lung cancer growth by triggering histone acetylation and acting synergically with HDAC inhibitors. Pharmacol Res. 2022 Nov;185:106487. doi: 10.1016/j.phrs.2022.106487. | Click |
| 2 | The Synergistic Effects of Celastrol in combination with Tamoxifen on Apoptosis and Autophagy in MCF-7 Cells. J Immunol Res. 2021 Jul 22;2021:5532269. doi: 10.1155/2021/5532269. | Click |
| 3 | Celastrol inhibits the migration and invasion and enhances the anti-cancer effects of docetaxel in human triple-negative breast cancer cells. Med Oncol. 2022 Sep 7;39(12):189. doi: 10.1007/s12032-022-01792-y. | Click |
| 4 | Celastrol acts synergistically with afatinib to suppress non-small cell lung cancer cell proliferation by inducing paraptosis. J Cell Physiol. 2021 Jun;236(6):4538-4554. doi: 10.1002/jcp.30172. | Click |
| 5 | Autophagy flux inhibition mediated by celastrol sensitized lung cancer cells to TRAIL‑induced apoptosis via regulation of mitochondrial transmembrane potential and reactive oxygen species. Mol Med Rep. 2019 Feb;19(2):984-993. doi: 10.3892/mmr.2018.9757. | Click |
| 6 | Celastrol enhances TRAIL-induced apoptosis in human glioblastoma via the death receptor pathwayCelastrol enhances TRAIL-induced apoptosis in human glioblastoma via the death receptor pathway. Cancer Chemother Pharmacol. 2019 Oct;84(4):719-728. doi: 10.1007/s00280-019-03900-8. | Click |
| 7 | Celastrol enhances tamoxifen sensitivity in the treatment of triple negative breast cancer via mitochondria mediated apoptosis pathway. Am J Transl Res. 2023 Apr 15;15(4):2703-2715. | Click |
| 8 | Celastrol Inhibits the Proliferation and Decreases Drug Resistance of Cisplatin- Resistant Gastric Cancer SGC7901/DDP Cells. Anticancer Agents Med Chem. 2022;22(2):270-279. doi: 10.2174/1871520621666210528144006. | Click |
