Americanin A
Americanin A is a Neolignan. Americanin A can be isolated from the seeds of Phytolacca americana. Americanin A activates ATM and ATR, initiating the subsequent signal transduction cascades that include Chk1, Chk2, and tumor suppressor p53. Americanin A targets selectively Skp2 for degradation and thereby stabilizes p27. Americanin A suppresses the activity of Cyclin B1 and its partner cdc2 to prevent entry into Mitosis. Americanin A induces Apoptosis by producing excessive ROS. Americanin A has anti-cancer activity against colorectal cancer.
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- CAS No.: 69506-79-2
- Formule: C18H16O6
- Masse moléculaire:328.32
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Stockage:
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Activité biologique
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Activité biologique
Description
IC50 & Target
[1]|
Chk1 |
Chk2 |
ATM |
ATR |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| A549 | IC50 |
39.1 μM
Compound: 1
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Antiproliferative activity against human A549 cells after 24 to 72 hrs by SRB assay
Antiproliferative activity against human A549 cells after 24 to 72 hrs by SRB assay
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[PMID: 26595875] |
In Vitro
Americanin A (24–72 h) selectively inhibits proliferation of human cancer cells (IC50 9.0–66.4 μM) with no significant effect on MRC-5 normal cells, and inhibits HCT116 cells in a concentration- and time-dependent manner[1].
Americanin A (7.5-30 μM; 24 h) induces G2/M cell-cycle arrest in HCT116 cells, with 30 μM increasing G2/M phase cells to 38.9%[1].
Americanin A (7.5–30 μM; 24 h) induces DNA damage in HCT116 cells, as indicated by increased phosphorylated H2A.X and decreased acetylated H3[1].
Americanin A (7.5–30 μM; 48 h) induces apoptosis in HCT116 cells after 48 h treatment, with 30 μM increasing sub-G1 cells to 52.0%[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A549, Caki-1, K562, HCT116, SW480, HCT-15, RKO, MRC-5
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Concentration:IC₅₀ values (9.0–66.4 μM for cancer cells; >100 μM for MRC-5)
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Incubation Time:24 h, 48 h, 72 h
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Result:Inhibited proliferation of A549 (IC50 39.1 μM), Caki-1 (IC50 66.4 μM), K562 (IC50 12.9 μM), HCT116 (IC50 9.0 μM), SW480 (IC50 27.4 μM), HCT-15 (IC50 12.5 μM), RKO (IC50 24.4 μM) cells; measured HCT116 IC50 values of 24.1 μM (24 h), 9.6 μM (48 h), 8.7 μM (72 h); showed no significant inhibition of MRC-5 cells (IC50 > 100 μM).
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Cell Line:HCT116
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Concentration:7.5, 15, 30 μM
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Incubation Time:24 h
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Result:Increased the proportion of G₂/M phase cells from 20.6% (untreated) to 38.9% at 30 μM; increased sub-G₁ cell proportion (apoptosis indicator) concentration-dependently, but the increase was not significant at 24 h.
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Cell Line:HCT116
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Concentration:7.5, 15, 30 μM
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Incubation Time:24 h
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Result:Suppressed expression of cyclin A, cyclin B1, phosphorylated cyclin B1 (Ser147), CDK2, and cdc2 in a concentration-dependent manner.\nIncreased phosphorylation of histone H2A.X (Ser139) and decreased acetylation of histone H3 (Lys9) concentration-dependently.
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Cell Line:HCT116
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Concentration:7.5, 15, 30 μM
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Incubation Time:48 h
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Result:Increased sub-G₁ cell proportion from 6.5% (untreated) to 52.0% at 30 μM; showed increased early and late apoptotic cells concentration-dependently via annexin V/FITC staining.
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-nu (female, 4-6 weeks old, HCT116 tumor xenograft)[1]
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Dosage:5 mg/kg; 10 mg/kg
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Administration:i.p.; three times a week
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Result:Reduced tumor volumes by 45.0% (5 mg/kg) and 55.7% (10 mg/kg) compared to vehicle; Increased expressions of p21 and p27, and decreased Skp2 expression in excised tumors; Showed pronounced p27 staining and diminished Skp2 and Ki-67 staining via immunohistochemistry; Observed no overt toxicity or body weight changes.
Chemical Information
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CAS No. 69506-79-2
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Masse moléculaire 328.32
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Formule C18H16O6
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SMILES
OC[C@H]1[C@H](C2=CC(O)=C(C=C2)O)OC3=CC=C(/C=C/C=O)C=C3O1
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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)
Americanin A Related Classifications
HY-N18301 Related Classifications
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