Pair Name | 2,3,5,6-Tetramethylpyrazine, Cisplatin | ||
Phytochemical Name | 2,3,5,6-Tetramethylpyrazine (PubChem CID: 14296 ) | ||
Anticancer drug Name | Cisplatin (PubChem CID: 5702198 ) | ||
Structure of Phytochemical |
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Structure of Anticancer Drug |
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Pair Name | 2,3,5,6-Tetramethylpyrazine, Cisplatin | |||
Disease Info | [ICD-11: 2C10] | Pancreatic cancer | Investigative | |
Biological Phenomena | Induction-->Ferroptosis | |||
Gene Regulation | Up-regulation | Expression | BAX | hsa581 |
Down-regulation | Expression | BCL2 | hsa596 | |
Up-regulation | Cleavage | CASP3 | hsa836 | |
Up-regulation | Cleavage | CASP9 | hsa842 | |
Up-regulation | Expression | CYCS | hsa54205 | |
Down-regulation | Expression | GPX4 | hsa2879 | |
Down-regulation | Expression | NFE2L2 | hsa4780 | |
Up-regulation | Cleavage | PARP1 | hsa142 | |
Down-regulation | Expression | SLC7A11 | hsa23657 | |
In Vitro Model | PANC-1/CDDP | Cisplatin-resistant pancreatic ductal adenocarcinoma | Homo sapiens (Human) | N.A. |
In Vivo Model | The mice were inoculated subcutaneously with PANC-1/CDDP cells (1×10⁷/mouse) into the right flanks to establish PANC-1/CDDP xenograft models. | |||
Result | A series of ligustrazine-derived chalcones-modified platinum(IV) complexes were synthesized and evaluated for their anti-proliferative potency and generated an optimal platinum(IV) complex 16a. The above-described results indicated that 16a obtained different anti-cancer mechanisms of CDDP, which could initiate mitochondria-dependent apoptosis and xCT-GPX4 axial-mediated ferroptosis in PANC-1/CDDP cells. |
No. | Title | Href |
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1 | Ligustrazine-Derived Chalcones-Modified Platinum(IV) Complexes Intervene in Cisplatin Resistance in Pancreatic Cancer through Ferroptosis and Apoptosis. J Med Chem. 2023 Oct 12;66(19):13587-13606. doi: 10.1021/acs.jmedchem.3c00922. | Click |