Isosilychristin
Isosilychristin is a P-glycoprotein inhibitor with an IC50 of 25.9 μM. Isosilychristin downregulates the expression of transmembrane efflux pumps, exerts intracellular antioxidant effects, and inhibits NO production in macrophages. Isosilychristin regulates cell cycle progression, and exerts weak antiproliferative and colony formation inhibitory effects in prostate cancer cells. Isosilychristin reduces bacterial intercellular communication and reverses the drug resistance of Staphylococcus aureus. Isosilychristin can be used in studies related to prostate cancer, inflammation and bacterial infections.
For research use only. We do not sell to patients.
- CAS No.: 77182-66-2
- Formula: C25H22O10
- Molecular Weight:482.44
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Storage:
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
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Isosilychristin acts as an oxygen radical scavenger in cell-free ORAC assays with an IC50 of 6.0 μM; it scavenges free radicals in HepG2 cells with an IC50 of 13 μM; and it inhibits LPS-induced NO production in RAW 264.7 macrophages with an IC50 of 59.8 μM[1].
Isosilychristin inhibits P-gp activity in isolated membranes with an IC50 of 25.9 μM, and completely abolishes P-gp-mediated ATP consumption at concentrations of 225 μM and above[1].
Isosilychristin (10-30 μM; 72 h co-incubation with Doxorubicin (HY-15142A)) exhibits only mild toxicity to HOC and HOC/ADR cells when used alone, and only weakly sensitizes HOC/ADR cells to doxorubicin at a concentration of 20 μM[1].
Isosilychristin (10 μM; 48 h) downregulates ABCB1 gene expression by 20% in HOC/ADR human ovarian cancer cells, while altering the expression of several other ABC transporter genes[1].
Isosilychristin (90 μM; 10 days) exerts only a slight inhibitory effect on colony formation of human prostate cancer PC3 cells (inhibition rate: 19.9%)[2].
Isosilychristin (60-90 μM; 72 h) causes a slight but statistically significant change in cell cycle distribution at 60 μM in human prostate cancer PC3 cells, and induces a mild, concentration-dependent G1-phase cell cycle arrest in human androgen-dependent prostate cancer LNCaP cells[2].
Isosilychristin reverses the oxacillin resistance of multidrug-resistant Staphylococcus aureus NEM 449 at a concentration of 30 μM; it potently inhibits AI-2-mediated quorum sensing in Vibrio campbellii ATCC BAA-1119 with an EC50 of 14.7 μM, and shows no toxicity to this bacterium even at concentrations as high as 200 μM[3].
Isosilychristin shows no toxicity to human skin fibroblasts, human renal tubular epithelial cells and human embryonic kidney cells, with the highest tested concentration reaching 200 μM[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:doxorubicin-resistant (HOC/ADR) human ovarian carcinoma cells
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Concentration:10 μM
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Incubation Time:48 h
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Result:Downregulated the expression of the ABCB1 (P-gp) gene by 20% in HOC/ADR cells.
Downregulated ABCA2, ABCB9, ABCC10, and ABCF1 genes.
Upregulated ABCD1, ABCD4, ABCE1, ABCF2, and ABCG4 genes.
Did not affect the expression of the ABCC2 (BCRP) gene.
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Cell Line:human prostate carcinoma PC3 cells
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Concentration:90 μM
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Incubation Time:10 days (treated every 48 h)
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Result:Inhibited PC3 cell colony formation by 19.9%.
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Cell Line:human prostate carcinoma PC3 cells, human androgen-dependent prostate carcinoma LNCaP cells
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Concentration:60, 90 μM
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Incubation Time:72 h
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Result:Elevated PC3 G2/M population to 17.45% and decreased G1 population to 51.77% with unmodified S phase at 60 μM over 72 h, while 90 μM brought no cell cycle variation to PC3 cells.
Elevated LNCaP G1 population and reduced S population without G2/M fluctuation under both concentrations; G1 reached 70.23% and S dropped to 19.91% at 60 μM, and G1 rose to 71.81% with S declining to 18.48% at 90 μM.
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Cell Line:human prostate carcinoma PC3 cells
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Concentration:90 μM
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Incubation Time:72 h
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Result:Did not cause significant changes in the expression levels of cyclins (D1, D3, E, A, B1), CDKs (2, 4, Cdc2), CDKIs (p21, p27), Skp2, phosphorylated Chk2 (Thr68), total Chk2, or Cdc25 phosphatases (A, B, C) relative to control.
Chemical Information
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CAS No. 77182-66-2
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Molecular Weight 482.44
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Formula C25H22O10
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SMILES
OC[C@@H]1C2=C([C@H]3OC4=CC(O)=CC(O)=C4C([C@@H]3O)=O)C=CC(O)=C2O[C@H]1C5=CC(OC)=C(C=C5)O
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Structure Classification
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Initial Source
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Isosilychristin Related Classifications
HY-184830 Related Classifications
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