里查酮 A

生物活性体外研究体内研究里查酮 A 试剂级价格

里查酮 A

CAS号:97938-31-3
英文名:(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
中文名:里查酮 A
CBNumber:CB72218147
分子式:C26H30O6
分子量:438.51
MOL File:97938-31-3.mol

里查酮 A化学性质

沸点 :649.7±55.0 °C(Predicted)
密度 :1?+-.0.06 g/cm3(Predicted)
储存条件 :2-8°C
溶解度 :Soluble in Chloroform,Dichloromethane,Ethyl Acetate,DMSO,Acetone,etc.
形态 :Powder
酸度系数(pKa) :7.67±0.40(Predicted)

里查酮 A性质、用途与生产工艺

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.

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.