Leachianone A 从槐花中分离，具有抗疟疾，抗炎和细胞毒性作用。
Leachianone A 诱导细胞凋亡 (apoptosis)。
| 生物活性 | Leachianone A, isolated fromRadix Sophorae, has anti-malarial, anti-inflammatory, and cytotoxic potent[1].
Leachianone A inducesapoptosisinvolved both extrinsic and intrinsic pathways[2]. |
体外研究
(In Vitro) | Leachianone A (0-20 μg/ml; 24-72 hours) exhibits a marked inhibition on the survival of HepG2 cells time- and dose-dependently manner, IC50values are 6.9 μg/ml, 3.4 μg/ml and 2.8 μg/ml in cells with 24-, 48- and 72-hours treatment, respectively[1].
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[1].
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[1].
Cell Viability Assay[1] | 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[1] | 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[1] | Cell Line: | HepG2 cells | | Concentration: | 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. |
|
体内研究
(In Vivo) | 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[1].
| Animal Model: | Male nude mice with human hepatoma HepG2 cells[1] | | 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. |
|
| 分子量 | |
| 性状 | |
| Formula | |
| CAS 号 | |
| 结构分类 | |
| 来源 | - Plants
- Leguminosae
- Sophora flavescens
|
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, sealed storage, away from moisture and light *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light) |
