里查酮 A
中文名称:
里查酮 A
中文同义词:
里查酮 A
英文名称:
(2S)-5,7-Dihydroxy-2,3-dihydro-2α-(2-methoxy-4-hydroxyphenyl)-8-[(R)-5-methyl-2-(1-methylethenyl)-4-hexenyl]-4H-1-benzopyran-4-one
英文同义词:
2-methoxy-5,7,4-trihydroxy-8-lavandulylflavanone;(2S)-5,7-Dihydroxy-2,3-dihydro-2α-(2-methoxy-4-hydroxyphenyl)-8-[(R)-5-methyl-2-(1-methylethenyl)-4-hexenyl]-4H-1-benzopyran-4-one;Leachianone A;Leachiane A;(-)-Vexibidin;(S)-5,7-Dihydroxy-2-(4-hydroxy-2-Methoxyphenyl)-8-((R)-5-Methyl-2-(prop-1-en-2-yl)hex-4-en-1-yl)chroMan-4-one;4H-1-Benzopyran-4-one, 2,3-dihydro-5,7-dihydroxy-2-(4-hydroxy-2-methoxyphenyl)-8-[(2R)-5-methyl-2-(1-methylethenyl)-4-hexen-1-yl]-, (2S)-
CAS号:
97938-31-3
分子式:
C26H30O6
分子量:
438.51
EINECS号:
相关类别:
标准品;植物提取物;标准品 -对照药材;黄酮
Mol文件:
97938-31-3.mol
沸点
649.7±55.0 °C(Predicted)
密度
1?+-.0.06 g/cm3(Predicted)
储存条件
Sealed in dry,2-8°C
酸度系数(pKa)
7.67±0.40(Predicted)
生物活性
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)。
体外研究
Leachianone A (0-20 μg/ml; 24-72 hours) exhibits a marked inhibition on the survival of HepG2 cells time- and dose-dependently manner, IC 50 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 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.
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.
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.
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
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.
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.
