PG490, triptolide

| Name | Triptolide | ||
| PubChem CID | 107985 | ||
| Molecular Weight | 360.4g/mol | ||
| Synonyms |
PG490, triptolide |
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| Formula | C₂₀H₂₄O₆ | ||
| SMILES | CC(C)C12C(O1)C3C4(O3)C5(CCC6=C(C5CC7C4(C2O)O7)COC6=O)C | ||
| InChI | 1S/C20H24O6/c1-8(2)18-13(25-18)14-20(26-14)17(3)5-4-9-10(7-23-15(9)21)11(17)6-12-19(20,24-12)16(18)22/h8,11-14,16,22H,4-7H2,1-3H3/t11-,12-,13-,14-,16+,17-,18-,19+,20+/m0/s1 | ||
| InChIKey | DFBIRQPKNDILPW-CIVMWXNOSA-N | ||
| CAS Number | 38748-32-2 | ||
| ChEMBL ID | CHEMBL463763 | ||
| ChEBI ID | CHEBI:9747 | ||
| Herb ID | HBIN047173 | ||
| Drug Bank ID | DB12025 | ||
| KEGG ID | C09204 | ||
| Toxicity | Organism | Test Type | Route(Dose) |
| rat | LD50 | intraperitoneal(165 mg/kg) | |
| mouse | LD50 | intraperitoneal(254 mg/kg) | |
| rat | LD50 | oral(322 mg/kg) | |
| Structure |
Download
2D
MOL
3D
MOL
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| Chineses Pinyin | KunMingShanHaiTang | ||
| Use Part | Root | ||
| Habitat | ZheJiang, JiangXi, HuNan, SiChuan, GuiZhou, YunNan | ||
| Flavor | Bitter, Pungent | ||
| Meridian Tropism | Liver, Spleen, Kidney | ||
| 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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| Pair Name | Triptolide, Doxorubicin | |||
| Partner Name | Doxorubicin | |||
| Disease Info | [ICD-11: 2B33.4] | Leukemia | Investigative | |
| Biological Phenomena | Induction-->Ferroptosis | |||
| Gene Regulation | Down-regulation | Expression | NFE2L2 | hsa4780 |
| Down-regulation | Expression | GPX4 | hsa2879 | |
| In Vitro Model | K-562 | Blast phase chronic myelogenous leukemia | Homo sapiens (Human) | CVCL_0004 |
| HL-60 | Adult acute myeloid leukemia | Homo sapiens (Human) | CVCL_0002 | |
| Result | The present study indicated that Nrf2 served a critical role in leukemia cell resistance to DOX and triptolide‑induced ferroptosis and suggested a potential strategy of combination therapy using triptolide and DOX in leukemia treatment. | |||
| Pair Name | Triptolide, Carboplatin | |||
| Partner Name | Carboplatin | |||
| Disease Info | [ICD-11: 2C30] | Melanoma | Investigative | |
| Biological Phenomena | Induction-->DNA damage | |||
| Gene Regulation | Down-regulation | Activity | NR1H2 | hsa7376 |
| In Vitro Model | A-375 | Amelanotic melanoma | Homo sapiens (Human) | CVCL_0132 |
| B16 | Mouse melanoma | Mus musculus (Mouse) | CVCL_F936 | |
| In Vivo Model | A375 cells were resuspended in 40% Matrigel (BD Biosciences) on ice, and then injected subcutaneously into the right axilla of the nude mice. | |||
| Result | This study reveals the NER inhibitor TPL which has great potential in treating melanoma, either alone or in combination with CBP. | |||
| Pair Name | Triptolide, ABT-199 | |||
| Partner Name | ABT-199 | |||
| Disease Info | [ICD-11: 2A60.Z] | Acute myeloid leukemia | Investigative | |
| Biological Phenomena | Induction-->Apoptosis | |||
| Gene Regulation | Up-regulation | Expression | BID | hsa637 |
| Up-regulation | Expression | PMAIP1 | hsa5366 | |
| Up-regulation | Expression | BBC3 | hsa27113 | |
| Up-regulation | Expression | BCL2L11 | KEGG ID N.A. | |
| In Vitro Model | MV4-11 | Childhood acute monocytic leukemia | Homo sapiens (Human) | CVCL_0064 |
| MOLM-13 | Adult acute myeloid leukemia | Homo sapiens (Human) | CVCL_2119 | |
| U-937 | Adult acute monocytic leukemia | Homo sapiens (Human) | CVCL_0007 | |
| THP-1 | Childhood acute monocytic leukemia | Homo sapiens (Human) | CVCL_0006 | |
| KG-1a | Adult acute myeloid leukemia | Homo sapiens (Human) | CVCL_1824 | |
| In Vivo Model | 5-6 week-old female BALB/C nude mice (18–20 g; Beijing HFK bioscience Co. Ltd.) were injected subcutaneously with 5.8×10⁶ MOLM-13 cells at the right flank of mice. | |||
| Result | These findings suggest that the regimen combining TPL and ABT-199 might be active against AML by inducing robust apoptosis through reciprocal regulation of anti- and proapoptotic Bcl-2 family proteins, therefore providing a strong rationale for the clinical investigation of this combination regimen for the treatment of AML. | |||
| Pair Name | Triptolide, Gefitinib | |||
| Partner Name | Gefitinib | |||
| Disease Info | [ICD-11: 2C25.Z] | Lung cancer | Investigative | |
| Biological Phenomena | Inhibition-->Epithelial-mesenchymal transition | |||
| Gene Regulation | Up-regulation | Expression | CDH1 | hsa999 |
| Down-regulation | Expression | MMP9 | hsa4318 | |
| Down-regulation | Expression | SNAI1 | hsa6615 | |
| Down-regulation | Expression | VIM | hsa7431 | |
| In Vitro Model | A-549 | Lung adenocarcinoma | Homo sapiens (Human) | CVCL_0023 |
| Result | The present results indicated that the combination of TP and TKIs may be a promising therapeutic strategy to treat patients with NSCLCs harboring EGFR mutations. | |||
| Pair Name | Triptolide, Cetuximab | |||
| Partner Name | Cetuximab | |||
| Disease Info | [ICD-11: 2C25.Z] | Lung cancer | Investigative | |
| Gene Regulation | Down-regulation | Expression | EGFR | hsa1956 |
| In Vitro Model | A-549 | Lung adenocarcinoma | Homo sapiens (Human) | CVCL_0023 |
| NCI-H1299 | Lung large cell carcinoma | Homo sapiens (Human) | CVCL_0060 | |
| NCI-H520 | Lung squamous cell carcinoma | Homo sapiens (Human) | CVCL_1566 | |
| UM-SCC-6 | Tongue squamous cell carcinoma | Homo sapiens (Human) | CVCL_7773 | |
| In Vivo Model | To establish xenografts of cancer cell lines, a suspension of 5×10⁶ H1299, UM-SCC6 cancer cells in 0.1 mL RPMI 1640 was injected into the subcutaneous dorsa of mice at the proximal midline. | |||
| Result | Cet-TPL represents a potent targeting therapeutic agent against EGFR-overexpressing NSCLC and others. | |||
| No. | Title | Href |
|---|---|---|
| 1 | Cetuximab-Triptolide Conjugate Suppresses the Growth of EGFR-Overexpressing Lung Cancers through Targeting RNA Polymerase II. Mol Ther Oncolytics. 2020 Jul 6;18:304-316. doi: 10.1016/j.omto.2020.07.001. | Click |
| 2 | Triptolide promotes ferroptosis by suppressing Nrf2 to overcome leukemia cell resistance to doxorubicin. Mol Med Rep. 2023 Jan;27(1):17. doi: 10.3892/mmr.2022.12904. | Click |
| 3 | Triptolide enhances carboplatin-induced apoptosis by inhibiting nucleotide excision repair (NER) activity in melanoma. Front Pharmacol. 2023 Jun 1;14:1157433. doi: 10.3389/fphar.2023.1157433. | Click |
| 4 | Combining triptolide with ABT-199 is effective against acute myeloid leukemia through reciprocal regulation of Bcl-2 family proteins and activation of the intrinsic apoptotic pathway. Cell Death Dis. 2020 Jul 22;11(7):555. doi: 10.1038/s41419-020-02762-w. | Click |
| 5 | Triptolide inhibits epithelial‑mesenchymal transition and induces apoptosis in gefitinib‑resistant lung cancer cells. Oncol Rep. 2020 May;43(5):1569-1579. doi: 10.3892/or.2020.7542. | Click |