Colchicine derivative-1
Colchicine derivative-1 is a colchicine derivative. Colchicine derivative-1 exhibits cytotoxicity against various cells. Colchicine derivative-1 arrests cancer cells at the G2/M phase of the cell cycle. Colchicine derivative-1 increases the levels of MMP-2, MMP-8, MMP-9, IL-2, IL-6, IL-17A, IL-22, IL-4, and IL-5 in the blood, inhibits the gene expression of hepatic fibrinogen α, β, γ and TGF-β1, and alleviates hepatic fibrosis symptoms in mice. Colchicine derivative-1 has antifibrotic activity and can be used in studies related to hepatic fibrosis.
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- Formule: C40H50N4O17
- Masse moléculaire:858.84
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
In Vitro
Colchicine derivative-1 (Compound 4) exhibits cytotoxicity in human endothelial cells, human cervical carcinoma cells, human embryonic kidney cells, human pancreatic carcinoma cells, human hepatic carcinoma cells, murine fibroblasts, and murine macrophages, with IC50 values of 180, 96, 16, 6, 10, 40, and 25 nM, respectively[1].
Colchicine derivative-1 (0.5 μM, 72 h) arrests human COLO357 cancer cells at the G2/M phase of the cell cycle[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HepG2, Eahy926, COLO357, PANC1, HeLa, HEK293, L929, RAW267
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Concentration:0.5 μM
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Incubation Time:72 h
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Result:Demonstrated cytotoxic activity comparable to parent colchicine, with variable IC50 values across individual cell lines.
Matched average activity of parent colchicine.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (female, 6-8 weeks old, liver fibrosis induced by intraperitoneal CCl4 mixed with olive oil injections every second or third day for 8 weeks)[1]
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Dosage:100 μM/ mouse
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Administration:i.v.; 5 total injections over 2 weeks
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Result:Increased blood levels of MMP-2, MMP-8, and MMP-9 significantly.
Stimulated production of group II chemokines (CXCL13, CCL22, CXCL5/6, IP-10) and group III chemokines (Eotaxin, MIP-1b).
Induced a pro-inflammatory cytokine response with 6-times higher IL-6 levels, plus elevated IL-2, IL-17A, and IL-22 compared to the CCl4 control group.
Partially normalized blood AST and ALT levels.
Sharply suppressed liver gene expression of fibrinogen α, β, γ, and TGF-β1.
Improved liver histology with finer fibrotic scars and reduced vascularization compared to the CCl4 control group.
- RT-PCR
- RNA extraction experimental
- Collagen: Sirius Red Staining
- Mitochondrial membrane-potential fluorescent assay
- Mammalian live/dead viability and cytotoxicity staining
- BrdU Incorporation Assay
- Connective Tissue: Masson's Trichrome/Collagen Trichrome Staining
- Protocol for Cell Cycle
- Real Time qPCR (Q-PCR)
- Cell Viability Determination by MTT Colorimetric Assay
- Fibrosis/Collagen Morphometry
- Cell Cytotoxicity Assay
- Flow cytometric DNA-content cell-cycle staining
- Mitochondrial membrane-potential and mitochondrial mass staining
Chemical Information
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Masse moléculaire 858.84
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Formule C40H50N4O17
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SMILES
O=C(OCC(N[C@H]1CCC2=CC(OC)=C(OC)C(OC)=C2C3=C1C=C(OCC4=C)C4=C3)=O)CCC5=CN([C@@H]6[C@H](O)[C@@H](O)[C@H](O[C@@H]7[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O7)[C@@H](CO)O6)N=N5
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Colchicine derivative-1 Related Classifications
HY-182795 Related Classifications
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