补骨脂乙素

中文名称:

补骨脂乙素

中文同义词:

异补骨脂查尔酮;补骨脂乙素(异补骨脂查尔酮);补骨脂乙素(异补骨脂酮;异补骨脂查尔酮/补骨脂乙素;ISOBAVACHALCONE 异补骨脂查尔酮/补骨脂乙素;补骨酯乙素;异补骨脂乙素;ISOBAVACHIN异补骨脂查尔酮标准品

英文名称:

ISOBAVACHALCONE

英文同义词:

ISOBAVACHALCONE;(E)-1-[2,4-Dihydroxy-3-(3-methyl-2-butenyl)phenyl]-3-(4-hydroxyphenyl)-2-propen-1-one;(E)-4,2,4-Trihydroxy-3-prenylchalcone;2,4,4-Trihydroxy-3-prenyl-trans-chalcone;Isobacachalcone;2-Propen-1-one,1-[2,4-dihydroxy-3-(3-methyl-2-butenyl)phenyl]-3-(4-hydroxyphenyl)-, (2E)-;(2E)-1-[2,4-Dihydroxy-3-(3-methylbut-2-en-1-yl)phenyl]-3-(4-hydroxyphenyl)prop-2-en-1-one;CS-446

CAS号:

20784-50-3

分子式:

C20H20O4

分子量:

324.37

EINECS号:

相关类别:

中药对照品;标准品;对照品,标准品;植物提取物;对照品;植提标准品;标准品-对照品;分析试剂标准品;对照品-中药对照品;PI3K/Akt/mTOR;Akt;mTOR;PI3K;查尔酮;标准品 -中药标准品;标准品，对照品;合成中间体

Mol文件:

20784-50-3.mol

熔点

156.8-157.8 °C(Solv: ethyl acetate (141-78-6); hexane (110-54-3))

沸点

549.0±50.0 °C(Predicted)

密度

1.243±0.06 g/cm3(Predicted)

储存条件

Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

形态

Yellow oil.

酸度系数(pKa)

7.99±0.40(Predicted)

生物活性

Isobavachalcone (Corylifolinin) 来源于补骨脂，是一种 Akt 信号通路的有效抑制剂，可诱导人类癌细胞凋亡 (以 IC50 值为 7.92 μM 抑制 OVCAR-8 癌细胞生长)，具有抗癌和抗增殖活性。Isobavachalcone 还能诱导 OVCAR-8 细胞中活性氧的产生。

靶点

IC50: 7.92 μM (OVCAR-8 cell)

体外研究

Isobavachalcone (6.0-48.0 μM; 72 hours; OVCAR-8, PC3, A549, MCF-7, L-02 and HUVEC cells) treatment inhibits the proliferation of human cancer cells. Isobavachalcone inhibits PC3, A549, MCF-7, L-02 and HUVEC cells growth with IC50 values of 15.06 μM, 32.2 μM, 28.29 μM, 31.61 μM and 31.3 μM, respectively. Isobavachalcone (0-18 μM; 6 hours; OVCAR-8 and PC3 cells) treatment results in a concentration-and time-dependent down-regulation of the Ser-473 phosphorylation of Akt and GSK3b phosphorylation. Isobavachalcone (0-18 μM; 72 hours; OVCAR-8 and PC3 cells) treatment causes apoptosis via caspase- and ROS-involved mitochondrial pathway. Cell Proliferation Assay Cell Line: OVCAR-8, PC3, A549, MCF-7, L-02 and HUVEC cells Concentration: 6.0-48.0 μM Incubation Time: 72 hours Result: Inhibited the proliferation of human cancer cells. Western Blot Analysis Cell Line: OVCAR-8 or PC3 cells Concentration: 0 μM, 6 μM, 12 μM, and 18 μM Incubation Time: 6 hours Result: A concentration-and time-dependent down-regulation of the Ser-473 phosphorylation of Akt. GSK3b phosphorylation was also inhibited in a concentration- and time-dependent manner. Apoptosis Analysis Cell Line: OVCAR-8 cells and PC3 cells Concentration: 0 μM, 6 μM, 12 μM, and 18 μM Incubation Time: 72 hours Result: Led to dose dependent increase of apoptosis.

Cell Line:

OVCAR-8, PC3, A549, MCF-7, L-02 and HUVEC cells

Concentration:

6.0-48.0 μM

Incubation Time:

72 hours

Result:

Inhibited the proliferation of human cancer cells.

Cell Line:

OVCAR-8 or PC3 cells

Concentration:

0 μM, 6 μM, 12 μM, and 18 μM

Incubation Time:

6 hours

Result:

A concentration-and time-dependent down-regulation of the Ser-473 phosphorylation of Akt. GSK3b phosphorylation was also inhibited in a concentration- and time-dependent manner.

Cell Line:

OVCAR-8 cells and PC3 cells

Concentration:

0 μM, 6 μM, 12 μM, and 18 μM

Incubation Time:

72 hours

Result:

Led to dose dependent increase of apoptosis.

体内研究

Isobavachalcone (20 mg/kg; intraperitoneal injection; for 0.5-24 hours; female Kunming mice) treatment results in an increase in blood glucose levels, reaching a maximum within 1 hour and maintaining until 4 hours post-dosing. Animal Model: Seven-week-old specific pathogen-free female Kunming mice (18-22 g) Dosage: 20 mg/kg Administration: Intraperitoneal injection; for 0.5, 1, 2, 4, 6, 8, 12, 24 hours Result: Increased in blood glucose levels.

Animal Model:

Seven-week-old specific pathogen-free female Kunming mice (18-22 g)

Dosage:

20 mg/kg

Administration:

Intraperitoneal injection; for 0.5, 1, 2, 4, 6, 8, 12, 24 hours

Result:

Increased in blood glucose levels.

化学性质

黄色结晶粉末，可溶于甲醇、乙醇、DMSO等有机溶剂，来源于补骨脂PsoraleacorylifoliaLinn.。

用途

补骨脂乙素具有抗菌，抗癌的药理活性作用。