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α-Amanitin

CAS No. : 23109-05-9

MCE 站：α-Amanitin

产品活性：α-Amanitin 是几种致命毒蘑菇的主要毒素，通过抑制RNA 聚合酶 II (RNA-polymerase II) 发挥其毒性作用。

研究领域：Cell Cycle/DNA Damage  |  Antibody-drug Conjugate/ADC Related

作用靶点：DNA/RNA Synthesis  |  ADC Cytotoxin

In Vitro: α-Amanitin decreases TAF15 mRNA ａnd TAF15 protein levels in MKN45 cells, ａnd inhibits the RNAPII activity towards TAF15 mRNA. alpha-Amanitin decreases cell viability by 14%, 21%, 41%, 44%, ａnd 50% at concentrations of 100, 10, 1, 0.1, ａnd 0.01 µg/mL, respectively. The LD₅₀ of the alpha-Amanitin at 36 h is measured as 1 µg/mL. The total amount of protein within the cell at 24 h is significantly increased for the 1 µg/mL dose of alpha-Amanitin compared to the control. α-Amanitin dramatically decreases the expression of gap junctional genes (Gja1, Gja4 ａnd Gjc1) ａnd FSHr ａnd LHr in cumulus cells.

In Vivo: The intravenous LD₅₀ dose of alpha-Amanitin is 0.327 mg/kg body weight after intravenous injection into BALB/c mice. After 12 h of alpha-Amanitin injection in caudal vein, the levels of WBC, RBC ａnd HGB decrease significantly, while those of BUN ａnd Crea increase significantly in serum. alpha-Amanitin inhibits some genes (Hsp90b1, Irx4, etc.), whose encoded proteins regulate the RNA polymerase II activity. alpha-Amanitin down-regulates some proteins (Nmi, Trpc5, etc.) taking part in the transcription progress. alpha-Amanitin has potent activity in DTC suppression. Mice injected with alpha-Amanitin (0.4 mg/kg, i.p.)-treated cells maintain their body weight, while those receiving a peritoneal injection of MKN45 cells show a constant decrease in body weight.

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