8-Acetonyldihydronitidine
8‑Acetonyldihydronitidine is a naturally occurring benzophenanthridine alkaloid with antibacterial, antifungal, and anti-proliferative activities against colorectal cancer cells. 8‑Acetonyldihydronitidine inhibits Staphylococcus aureus and exerts a potent antifungal effect against Cladosporium cladosporioides. 8‑Acetonyldihydronitidine activates the p53 signaling pathway, upregulates the expression of target genes including p21, BAX, and FAS, downregulates cyclin A and cyclin B, and induces cell cycle arrest and apoptosis, thereby suppressing the proliferation of colorectal cancer cells. 8‑Acetonyldihydronitidine is used in research related to colorectal cancer, fungal infections, and bacterial infections.
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- CAS No.: 80330-39-8
- Formule: C24H23NO5
- Masse moléculaire:405.45
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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
- Pureté et documentation
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Activité biologique
Description
IC50 & Target
[1]|
CDK1/cyclin A |
CDK2(C118L/A144C-Cyclin B) |
Caspase 3 |
Bax |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| HCT-116 | IC50 |
5.38 μM
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Antiproliferative activity against human HCT116 colorectal cancer cells assessed as reduction in cell viability incubated for 48 h by MTT assay.
Antiproliferative activity against human HCT116 colorectal cancer cells assessed as reduction in cell viability incubated for 48 h by MTT assay.
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j.ejphar.2019.03.042 |
| LoVo | IC50 |
5.81 μM
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Antiproliferative activity against human LOVO colorectal cancer cells assessed as reduction in cell viability incubated for 48 h by MTT assay.
Antiproliferative activity against human LOVO colorectal cancer cells assessed as reduction in cell viability incubated for 48 h by MTT assay.
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j.ejphar.2019.03.042 |
| HCT-15 | IC50 |
12.91 μM
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Antiproliferative activity against human HCT15 colorectal cancer cells assessed as reduction in cell viability incubated for 48 h by MTT assay.
Antiproliferative activity against human HCT15 colorectal cancer cells assessed as reduction in cell viability incubated for 48 h by MTT assay.
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j.ejphar.2019.03.042 |
| SW480 | IC50 |
9.33 μM
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Antiproliferative activity against human SW480 colorectal cancer cells assessed as reduction in cell viability incubated for 48 h by MTT assay.
Antiproliferative activity against human SW480 colorectal cancer cells assessed as reduction in cell viability incubated for 48 h by MTT assay.
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j.ejphar.2019.03.042 |
In Vitro
8-Acetonyldihydronitidine (8-AHN) (0-80 µM; 48 h) effectively inhibits the proliferation of HCT116, LOVO, HCT15, and SW480 human colorectal cancer cells, with the lowest IC50 of 5.38 µM observed in HCT116 cells[1].
8-Acetonyl dihydronitidine (5 µM; 0-48 h) induces G2/M phase cell cycle arrest in synchronized HCT116 human colorectal cancer cells in a time-dependent manner[1].
8-Acetonyl dihydronitidine (0-8 µM; 24 h) downregulates cyclin A and cyclin B at both the protein and mRNA levels in HCT116 and LOVO human colorectal cancer cells[1].
8-Acetonyl dihydronitidine (2-10 µM; 0-48 h) induces apoptosis in HCT116 human colorectal cancer cells in a time- and dose-dependent manner, and the level of cleaved caspase-3 increases after treatment at a concentration of 8 µM for 24 h[1].
8-Acetonyldihydronitidine enhances the expression and transcriptional activity of p53 in HCT116 human colorectal cancer cells, and upregulates the p53 target genes p21, BAX and FAS after 24 h of treatment[1].
8-Acetonyl dihydronitidine (compound 1) inhibits the growth of Staphylococcus aureus, with an MIC of 1.56 μg/mL and an MBC of 25 μg/mL[2].
8-Acetonydihydronitidine exhibits potent antifungal activity against Cladosporium cladosporioides (100 mm2 inhibition zone at 2 mg), and inhibits more than 90% of conidial germination of Colletotrichum gloeosporioides after 6 h of treatment at a concentration of 200 μg/mL[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT116, HCT15, LOVO, SW480 human colorectal cancer cell lines
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Concentration:0, 0.25, 0.5, 1, 2.5, 5, 10, 20, 40, 80 µM
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Incubation Time:48 h
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Result:Suppressed proliferation in all four cell lines in a concentration-dependent manner.
Exhibited IC50 values of 5.38 µM for HCT116 cells, 5.81 µM for LOVO cells, 12.91 µM for HCT15 cells, and 9.33 µM for SW480 cells.
Showed the highest sensitivity in HCT116 and LOVO cells.
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Cell Line:synchronized HCT116 human colorectal cancer cells
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Concentration:5 µM
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Incubation Time:0 h, 24 h, 48 h
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Result:Caused a time-dependent increase in the proportion of cells in the G2/M phase.
Increased G2/M phase proportion from 29.2% at 0 h to 53.1% at 24 h and 57.9% at 48 h.
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Cell Line:HCT116 and LOVO human colorectal cancer cells
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Concentration:0, 2, 4, 6, 8, 10 µM
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Incubation Time:24 h
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Result:Decreased the protein levels of cyclin A and cyclin B in both HCT116 and LOVO cells in a dose-dependent manner.
Significantly increased the protein level of cleaved caspase-3 at the 8 µM dose along with other cleaved apoptotic markers in a dose-dependent manner after 24 h.
Significantly increased protein level of p53 transcriptional targets p21, BAX, and FAS upon treatment.
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Cell Line:HCT116 and LOVO human colorectal cancer cells
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Concentration:0, 4, 8 µM
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Incubation Time:24 h
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Result:Reduced mRNA expression of both cyclin B and cyclin A within 24 h of treatment in a dose-dependent manner.
Significantly increased mRNA level of p53 transcriptional targets p21, BAX, and FAS upon treatment.
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Cell Line:HCT116 human colorectal cancer cells
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Concentration:5 µM
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Incubation Time:0 h, 24 h, 48 h
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Result:Increased the combined percentage of early and late apoptotic cells from 2.35% at 0 h to 21.49% at 24 h and 31.57% at 48 h at 5 µM.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude mice (male; 5 weeks old; 15-18 g; HCT116 human colorectal cancer cell subcutaneous xenograft)[1]
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Dosage:10 mg/kg
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Administration:i.p.; every other day; 2 weeks
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Result:Significantly inhibited the growth of HCT116 xenograft tumors.
Reduced average excised tumor weight to 300 mg.
Decreased tumor volume relative to the vehicle control group.
Did not cause significant body weight loss in treated animals.
Increased expression of BAX and p53 in tumor sections.
Decreased expression of cyclin B and PCNA in tumor sections.
Showed no major organ-related toxicities in lung and liver.
Chemical Information
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CAS No. 80330-39-8
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Masse moléculaire 405.45
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Formule C24H23NO5
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SMILES
O=C(C)CC1C2=CC(OC)=C(OC)C=C2C=3C=CC4=CC=5OCOC5C=C4C3N1C
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Structure Classification
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Initial Source
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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)
8-Acetonyldihydronitidine Related Classifications
HY-N21597 Related Classifications
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