Ovalitenone
Ovalitenone is a flavonoid found in the plant Millettia peguensis and acts as a CYP1A1/CYP1B1 inhibitor with IC50 values of 0.28 and 0.6 μM, respectively. Ovalitenone significantly decreases the levels of N-cadherin, snail, and slug while increasing E-cadherin, thereby inhibiting the EMT pathway. Ovalitenone also inhibits the regulatory signaling pathways of focal adhesion kinase (FAK), ATP-dependent tyrosine kinase (AKT), mammalian target of rapamycin (mTOR), and cell division cycle 42 (Cdc42). Ovalitenone inhibits the proliferation, migration, invasion, epithelial-mesenchymal transition, and cancer stem cell-like phenotype of lung cancer cells. Ovalitenone can be used in lung cancer-related research.
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- CAS. Nr.: 64280-22-4
- Formel: C19H14O6
- Molecular Weight:338.31
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Biologische Aktivität
Beschreibung
IC50 & Target
[2]|
CYP1A1 0.28 μM (IC50, Sacchrosomes™) |
CYP1B1 0.6 μM (IC50, Sacchrosomes™) |
CYP1A1 0.48 μM (IC50, HEK293) |
CYP1B1 1.5 μM (IC50, HEK293) |
In Vitro
Ovalitenone (10-200 µM; 7 days) reduces the number and size of colonies in H460 and A549 cells[1].
Ovalitenone (10-200 µM; 24-72 h) inhibits H460 and A549 migration[1].
Ovalitenone (50-200 µM; 24 h) inhibits the invasion of H460 and A549 cells through Matrigel[1].
Ovalitenone (10-200 µM; 24 h) reduces filopodia formation in H460 and A549 cells[1].
Ovalitenone (50-200 µM; 14 days) inhibits anchorage-independent growth of H460 and A549 cells[1].
Ovalitenone (50-200 µM; 14-21 days) reduces primary and secondary sphere formation in H460 and A549 cells[1].
Ovalitenone (10-200 µM; 24 h) inhibits EMT markers in H460 and A549 cells by decreasing N-cadherin, snail, and slug and increasing E-cadherin[1].
Ovalitenone (10-200 µM; 24 h) inhibits AKT/mTOR signaling in H460 and A549 cells[1].
Ovalitenone (50-200 µM; 24 h) inhibits the expression of EMT markers in H460 and A549 cells, decreasing N-cadherin and snail and increasing E-cadherin[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:H460 and A549 cells
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Concentration:10, 50, 100, 200 µM
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Incubation Time:24 h (viability); 24, 48, 72 h (proliferation)
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Result:Ovalitenone at concentrations lower than 200 µM did not significantly affect viability of H460 or A549 cells at 24 h.
In proliferation assays, ovalitenone at 10, 50, 100, 200 µM had no effect at 24 h; at 48 h, ovalitenone at 50, 100, 200 µM significantly decreased proliferation in a dose-dependent manner; at 72 h, ovalitenone at 10, 50, 100, 200 µM significantly decreased proliferation in both cell lines.
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Cell Line:H460 and A549 cells
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Concentration:10, 50, 100, 200 µM (nuclear staining); 100, 200 µM (Annexin V/PI)
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Incubation Time:24 h (nuclear staining); 24, 48, 72 h (Annexin V/PI)
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Result:Ovalitenone at 0-200 µM had no effect on apoptosis or necrosis in H460 and A549 cells at 24, 48, and 72 h by Hoechst 33342/PI staining.
Flow cytometry with Annexin V/PI showed that ovalitenone at 100 and 200 µM did not cause apoptosis or necrosis in either cell line at 24, 48, or 72 h.
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Cell Line:H460 and A549 cells
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Concentration:10, 50, 100, 200 µM
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Incubation Time:7 days
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Result:Ovalitenone at 50, 100, and 200 µM decreased colony size in H460 and A549 cells.
Colony number was also assessed: ovalitenone at 50, 100, and 200 µM showed dose-dependent reductions in colony number (%) for H460 and A549 compared with the control, with control colony number set to 100%.
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Cell Line:H460 and A549 cells
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Concentration:10, 50, 100, 200 µM
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Incubation Time:24, 48, 72 h
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Result:Ovalitenone inhibited H460 and A549 cell migration at 50, 100, and 200 µM at 24, 48, and 72 h.
Ovalitenone at 10 µM did not significantly inhibit migration.
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Cell Line:H460 and A549 cells
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Concentration:10, 50, 100, 200 µM
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Incubation Time:24 h (pre-incubation); 24 h (invasion)
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Result:Ovalitenone was able to inhibit H460 and A549 cell invasion through the Matrigel layer.
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Cell Line:H460 and A549 cells
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Concentration:50, 100, 200 µM
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Incubation Time:24 h (pre-incubation); 14 days (growth)
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Result:Exhibited a significantly reduced ability to form colonies, and ovalitenone attenuated the growth of the cells as indicated by the decrease in colony number and size when compared with the untreated control in both cells.
The colony numbers of H460 cells were significantly reduced by ovalitenone at 50, 100, and 200 µM to 31.05%, 51.48%, and 73.20%, respectively, and the percentages of colony size in response to ovalitenone at 50, 100, and 200 µM were 33.82%, 50.61%, and 63.41%, respectively.
The colony numbers of A549 cells were significantly reduced by ovalitenone at 50, 100, and 200 µM to 38.93%, 50.37%, and 74.06%, respectively, and the percentages of colony size in response to ovalitenone at 50, 100, and 200 µM were 31.62%, 49.92%, and 66.36%, respectively.
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Cell Line:H460 and A549 cells
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Concentration:10, 50, 100, 200 µM
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Incubation Time:24 h
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Result:Ovalitenone significantly decreased cellular levels of N-cadherin and snail, and increased E-cadherin in a dose-dependent manner in H460 and A549 cells.
Slug levels were also decreased in ovalitenone-exposed cells.\nOvalitenone decreased p-mTOR (Ser2448) in H460 and A549 cells at 50, 100, and 200 µM.
Ovalitenone at 50, 100, and 200 µM significantly reduced p-AKT (Ser473) in H460 cells; in A549 cells, significant reduction was found only at 100 and 200 µM.
Cdc42 and p-FAK (Tyr397) were not affected by ovalitenone in either cell line.
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Cell Line:H460 and A549 cells
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Concentration:50, 100, 200 µM
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Incubation Time:24 h
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Result:Immunofluorescence showed that ovalitenone significantly decreased N-cadherin and snail levels, whereas it upregulated E-cadherin in H460 cells and in A549 cells.
Chemical Information
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CAS. Nr. 64280-22-4
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Molecular Weight 338.31
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Formel C19H14O6
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SMILES
O=C(CC(C1=CC=C2OC=CC2=C1OC)=O)C3=CC=C4OCOC4=C3
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Structure Classification
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Initial Source
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[1]. Sanookpan K, et al. Ovalitenone Inhibits the Migration of Lung Cancer Cells via the Suppression of AKT/mTOR and Epithelial-to-Mesenchymal Transition. Molecules (Basel, Switzerland). 2021 Jan 26;26(3):638. [Content Brief]
[2]. Sharma R, et al. Furanoflavones pongapin and lanceolatin B blocks the cell cycle and induce senescence in CYP1A1-overexpressing breast cancer cells. Bioorganic & medicinal chemistry. 2018 Dec 15;26(23-24):6076-6086. [Content Brief]
[4]. Sung CJ, et al. Fucoidan from Sargassum hemiphyllum inhibits the stemness of cancer stem cells and epithelial-mesenchymal transitions in bladder cancer cells. International journal of biological macromolecules. 2022 Nov 30;221:623-633. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Ovalitenone Related Classifications
HY-N15267 Related Classifications
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