里查酮 A
里查酮 A(Leachianone A)
CAS: 97938-31-3
化学式: C26H30O6
| 中文名 | 里查酮 A |
| 英文名 | Leachianone A |
| 别名 | 里查酮 A (S)-5,7-二羟基-2-(4-羟基-2-甲氧基苯基)-8-((R)-5-甲基-2-(丙-1-烯-2-基)己-4- 烯-1-基)苯并二氢吡喃-4-酮 |
| 英文别名 | Leachiane A Leachianone A (-)-Vexibidin 2'-methoxy-5,7,4'-trihydroxy-8-lavandulylflavanone (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 (2S)-5,7-dihydroxy-2-(4-hydroxy-2-methoxyphenyl)-8-[(2R)-5-methyl-2-prop-1-en-2-ylhex-4-enyl]-2,3-dihydrochromen-4-one (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 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 | 97938-31-3 |
| 化学式 | C26H30O6 |
| 分子量 | 438.51 |
| 密度 | 1?+-.0.06 g/cm3(Predicted) |
| 熔点 | 157-158℃ |
| 沸点 | 649.7±55.0 °C(Predicted) |
| 比旋光度 | -43.6 (c, 1.07 in MeOH) |
| 酸度系数 | 7.67±0.40(Predicted) |
| 存储条件 | 2-8°C |
| 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. |
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