Cassialoin
Cassialoin is an orally active anthrone-C-glucoside natural product with antitumor activity, which is found in the heartwood of Cassia garrettiana. Cassialoin is metabolized to the active substance Chrysophanol‑9‑anthrone. Cassialoin does not directly inhibit the activities of VEGFR‑2 and MMP‑9 in vitro, nor does it directly inhibit vascular lumen formation and cell migration in vitro. Cassialoin increases the number of IFN-γ-positive CD8+ T cells and natural killer cells in the small intestine or spleen, and enhances IFN-γ production by splenocytes induced by Concanavalin A (HY-P2149). Cassialoin inhibits tumor growth and peritoneal invasion in colon cancer xenograft models. Cassialoin can be used for research on colon cancer.
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- CAS No.: 60462-09-1
- 화학식: C21H22O9
- 분자량:418.39
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
In Vitro
Cassialoin (1-100 μM; 24-72 h) does not affect the proliferation of human umbilical vein endothelial cells at concentrations up to 100 μM[2].
Cassialoin does not alter the expression of VEGFR-2 or VEGF-induced VEGFR-2 phosphorylation in human umbilical vein endothelial cells; nor does it exert a direct inhibitory effect on VEGF-induced tube formation, HUVEC migration, or MMP-9 secretion[2].
Cassialoin (1-100 μM; 6 h) does not significantly inhibit hypoxia-induced VEGF production in colon 26 cells at concentrations up to 100 μM[2].
Cassialoin (0.1-1 μM; 48 h) enhances Concanavalin A (HY-P2149)-induced IFN-γ production in splenocytes from colon cancer 26 cell tumor-bearing mice, but exerts no such effect on splenocytes from normal mice[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:colon 26 murine colon carcinoma cells
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Concentration:1, 10, 100 μM
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Incubation Time:6 h
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Result:Showed no effect on VEGF production under hypoxic conditions at concentrations of 1, 10, and 100 μM.
VEGF production as a percentage of control was 101.4% at 1 μM, 89.6% at 10 μM, and 85.1% at 100 μM.
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Cell Line:human umbilical vein endothelial cells
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Concentration:100 μM
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Incubation Time:24, 48, 72 h
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Result:Did not affect the proliferation of human umbilical vein endothelial cells.
In Vivo
Cassialoin (5-10 mg/kg; oral administration; twice daily; for 6 days) inhibits colon 26 tumor-induced neovascularization in the dorsal air sac model of BALB/c mice[2].
Cassialoin (50 mg/kg; single oral administration) is metabolized to Chrysophanol‑9‑anthrone and Chrysophanol (HY-13595) in the stomach and small intestine of mice, and is further metabolized to Aloe‑emodin (HY-N0189) in the blood circulation[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c (male; 5 weeks old at receipt; acclimated for 1 week; subcutaneous colon 26 tumor model with abdominal metastasis induced by subcutaneous injection of 3×104 colon 26 cells into the back on day 0)[2]
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Dosage:2.5 mg/kg; 5 mg/kg; 10 mg/kg
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Administration:p.o.; twice daily (08.00 and 20.00 hours); 25 consecutive days
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Result:Reduced final tumor weight and abdominal tumor‑invasion incidence in a dose‑dependent manner at oral 2.5‑10 mg/kg, achieving 22.5% relative tumor weight and 13.3% invasion incidence at 10 mg/kg.
Elevated splenic lymphocyte, CD4⁺ T, CD8⁺ T and NK‑cell populations across 2.5‑10 mg/kg oral doses, with peak lymphocyte and CD4⁺ T‑cell values at 5 mg/kg.
Lowered tumor PCNA‑positive proliferative cell counts, CD31‑positive angiogenic area and HIF‑1α‑positive cell counts, while augmenting tumor apoptotic cell numbers with increasing oral 2.5‑10 mg/kg doses.
Increased small‑intestinal IFN‑γ‑positive cell counts dose‑dependently over 2.5‑10 mg/kg; exerted variable modulatory effects on small‑intestinal CD8⁺ T and NK‑cell counts across tested oral doses.
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Animal Model:BALB/c (male; 5 weeks old at receipt; acclimated for 1 week; dorsal air-sac colon 26-packed chamber model induced by implantation of a nitrocellulose membrane chamber packed with 3×104 colon 26 cells)[2]
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Dosage:5 mg/kg; 10 mg/kg
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Administration:p.o.; twice daily; days 1-6
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Result:Significantly reduced the area of neovascularization induced by colon 26 cell-packed chambers compared to control mice at both 5 mg/kg and 10 mg/kg doses.
Chemical Information
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CAS No. 60462-09-1
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분자량 418.39
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화학식 C21H22O9
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SMILES
O=C1C2=C(C=CC=C2O)C(O)([C@H]3[C@@H]([C@H]([C@@H]([C@@H](CO)O3)O)O)O)C4=CC(C)=CC(O)=C14
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Structure Classification
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Initial Source
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Cassialoin Related Classifications
HY-N21609 Related Classifications
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