Leachianone A

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Leachianone A 是一种潜在的抗毒剂，它对镉诱导的细胞毒性具有抑制作用。

Leachianone A is a potential antitoxic agent, it shows inhibitory effects on cadmium- Induced cytotoxicity.(In Vitro):Leachianone A, isolated from Radix Sophorae, possessed a profound cytotoxic activity against human hepatoma cell line HepG2 in vitro, with an IC50 value of 3.4microg/ml post-48-h treatment. Its action mechanism via induction of apoptosis involved both extrinsic and intrinsic pathways. Its anti-tumor effect was further demonstrated in vivo by 17-54% reduction of tumor size in HepG2-bearing nude mice, in which no toxicity to the heart and liver tissues was observed.(In Vivo):Intravenous injection of 20 mg/kg and 30 mg/kg Leachianone A once daily for 30 days significantly reduced tumor volume in LA-treated nude mice by 17-54% compared to nude mice given vehicle alone.

Leachianone A (0-20 μg/ml; 24-72 hours) exhibits a marked inhibition on the survival of HepG2 cells time- and dose-dependently manner, IC50 values are 6.9 μg/ml, 3.4 μg/ml and 2.8 μg/ml in cells with 24-, 48- and 72-hours treatment, respectively.Leachianone A (10-30 μg/ml; 48 hours) indicates that at low concentration of LA (10 μg/ml), a substantial amount of cells is primarily in the early phase of apoptosis, at higher concentrations, induces a shift of the cell population to late apoptotic/ necrotic stage.Leachianone A (10-30 μg/ml; 48 hours) decreases the precursor of caspase-3 in a dose-dependent manner, reduces the protein level of the pro-forms of upstream initiator caspases, caspases-8 and -9, decreases two downstream substrates, namely inhibitor of caspase-activated DNase(ICAD) and poly-ADP-ribose polymerase (PARP) in HepG2 cells. Cell Viability Assay Cell Line:HepG2 cells Concentration:0 μg/ml, 2 μg/ml, 4 μg/ml, 6 μg/ml, 8 μg/ml, 10 μg/ml, 12 μg/ml, 14 μg/ml, 16 μg/ml, 18 μg/ml, 20 μg/ml Incubation Time:24-72 hours Result:Inhibited HepG2 cells survival.Apoptosis Analysis Cell Line:HepG2 cells Concentration:48 hours Incubation Time:10, 20, and 30 μg/ml Result:Induced the proportion of annexin V-stained cells in both the early and late apoptotic stage.Western Blot Analysis Cell Line:HepG2 cellsConcentration:48 hours Incubation Time:10, 20, and 30 μg/ml Result:Decreased the protein expression of caspase-3, caspases-8 and -9, reduced ICAD and PARP protein expression.

Leachianone A (intravenously injection; 20 mg/kg, 30 mg/kg; once daily; 30 days) significantly diminishes the tumor volume by 17-54% in LA-treated nude mice, when compared with those solely given the vehicle. Animal Model:Male nude mice with human hepatoma HepG2 cells Dosage:20 mg/kg; 30 mg/kg Administration:Intravenously injection; 20 mg/kg, 30 mg/kg; once daily; 30 days Result:Suppressed the tumor growth in vivo.

Isokurarinone

GPCR/G Protein

SGLT

SGLT

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97938-31-3

438.52

C26H30O6

>98% (HPLC)

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COc1cc(O)ccc1[C@@H]1CC(=O)c2c(O)cc(O)c(C[C@@H](CC=C(C)C)C(C)=C)c2O1

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(-20℃)

With Ice Pack

≥ 2 years