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20784-50-3

中文名稱 補骨脂乙素
英文名稱 ISOBAVACHALCONE
CAS 20784-50-3
分子式 C20H20O4
分子量 324.37
MOL 文件 20784-50-3.mol
更新日期 2024/10/25 15:10:13
20784-50-3 結(jié)構(gòu)式 20784-50-3 結(jié)構(gòu)式

基本信息

中文別名
補骨酯乙素
異補骨脂乙素
異補骨脂查耳酮
異補骨脂查爾酮
補骨脂乙素標(biāo)準(zhǔn)品
補骨脂乙素對照品
補骨脂乙素(異補骨脂酮
異補骨脂查爾酮(標(biāo)準(zhǔn)品)
異補骨脂查爾酮/補骨脂乙素
補骨脂乙素(異補骨脂查爾酮)
英文別名
CS-446
ISOBAVACHALCONE
Isobacachalcone
Isobavachalcone/Corylifolinin
Corylifolinin(Isobavachalcone)
(E)-4,2',4'-Trihydroxy-3'-prenylchalcone
2',4,4'-Trihydroxy-3'-prenyl-trans-chalcone
(E)-1-[2,4-Dihydroxy-3-(3-methyl-2-butenyl)phenyl]-3-(4-hydroxyphenyl)-2-propen-1-one
(E)-1-(2,4-Dihydroxy-3-(3-methylbut-2-en-1-yl)phenyl)-3-(4-hydroxyphenyl)prop-2-en-1-one
(2E)-1-[2,4-Dihydroxy-3-(3-methylbut-2-en-1-yl)phenyl]-3-(4-hydroxyphenyl)prop-2-en-1-one

物理化學(xué)性質(zhì)

外觀性狀黃色結(jié)晶粉末,可溶于甲醇、乙醇、DMSO等有機溶劑,來源于補骨脂PsoraleacorylifoliaLinn.。
熔點156.8-157.8 °C(Solv: ethyl acetate (141-78-6); hexane (110-54-3))
沸點549.0±50.0 °C(Predicted)
密度1.243±0.06 g/cm3(Predicted)
儲存條件Keep in dark place,Inert atmosphere,Store in freezer, under -20°C
酸度系數(shù)(pKa)7.99±0.40(Predicted)
形態(tài)黃色油狀

安全數(shù)據(jù)

危險性符號(GHS)GHS hazard pictograms
GHS06
警示詞危險
危險性描述H301

應(yīng)用領(lǐng)域

用途1
具有抑制脂多糖誘導(dǎo)的icam-1表達和白細(xì)胞與腦內(nèi)皮細(xì)胞粘附的作用
用途2
補骨脂乙素具有抗菌,抗癌的藥理活性作用。

常見問題列表

生物活性
Isobavachalcone (Corylifolinin) 來源于補骨脂,是一種 Akt 信號通路的有效抑制劑,可誘導(dǎo)人類癌細(xì)胞凋亡 (以 IC50 值為 7.92 μM 抑制 OVCAR-8 癌細(xì)胞生長),具有抗癌和抗增殖活性。Isobavachalcone 還能誘導(dǎo) OVCAR-8 細(xì)胞中活性氧的產(chǎn)生。
靶點

IC50: 7.92 μM (OVCAR-8 cell)

體外研究

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.
體內(nèi)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.
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