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  1. General Info
  2. Source Info
  3. Effects Info
  4. Reference
Phytochemical Details
01. General Information
Name Triptolide
PubChem CID 107985
Molecular Weight 360.4g/mol
Synonyms

PG490, triptolide

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 2D-img
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2D MOL 3D MOL
02. Source Information of Phytochemical
(1) Tripterygium hypoglaucum Warm
Chineses Pinyin KunMingShanHaiTang
Use Part Root
Habitat ZheJiang, JiangXi, HuNan, SiChuan, GuiZhou, YunNan
Flavor Bitter, Pungent
Meridian Tropism Liver, Spleen, Kidney
(2) Tripterygium wilfordii Cool
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
03. Combinatorial Therapeutic Effect(s)
Synergistic Effect
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Drug(s) whose efficacy can be enhanced by this phytochemical
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Combination Pair ID: 154
Pair Name Triptolide, Doxorubicin
Partner Name Doxorubicin
Disease Info [ICD-11: 2B33.4] Leukemia Investigative
Biological Phenomena Induction-->Ferroptosis
Gene Regulation Down-regulation Expression GPX4 hsa2879
Down-regulation Expression NFE2L2 hsa4780
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.
Combination Pair ID: 156
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.
Combination Pair ID: 157
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 BBC3 hsa27113
Up-regulation Expression BCL2L11 KEGG ID N.A.
Up-regulation Expression BID hsa637
Up-regulation Expression PMAIP1 hsa5366
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.
Drug(s) whose resistance can be reversed by this phytochemical
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Combination Pair ID: 153
Pair Name Triptolide, Gefitinib
Partner Name Gefitinib
Disease Info [ICD-11: 2C25] 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.
Drug(s) whose toxicity can be decreased by this phytochemical
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Combination Pair ID: 155
Pair Name Triptolide, Cetuximab
Partner Name Cetuximab
Disease Info [ICD-11: 2C25] 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.
04. Reference
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
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