梣酮

梣酮用途

Fraxinellone 是从芸苔科植物 Dictamnus dasycarpus 的根皮中分离出来的。 Fraxinellone 是 PD-L1 抑制剂,可抑制 HIF-1α 蛋白质合成,而不会影响 HIF-1α 蛋白质降解。 Fraxinellone 通过靶向 PD-L1,有可能成为癌症治疗的有价值的候选药物。

梣酮名称

[ CAS 号 ]:
28808-62-0

[ 中文名 ]:
梣酮

[ 英文名 ]:
Fraxinellone

[中文别名 ]:

[英文别名 ]:

梣酮生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 干细胞及 Wnt 通路 >> STAT

研究领域 >> 癌症

信号通路 >> JAK/STAT信号通路 >> STAT

信号通路 >> 免疫及炎症 >> PD-1/PD-L1

[体外研究]

Fraxinellone(0-100μM；12小时)使A549细胞中PD-L1阳性细胞的百分比从20.4%降低至11.4%[1]。细胞活力测定[1]细胞系：A549细胞浓度：0μM,10μM,30μM,100μM孵育时间：12小时结果：抑制PD-L1阳性细胞的百分比。

[体内研究]

与对照组相比,Fraxinellone(口服强饲法；30和100 mg/kg；每3天；30天)显着抑制女性无胸腺BALB/c裸鼠的肿瘤生长,减少HIF-1α,pTyr705 STAT3,PD-L1和VEGF染色[1]。动物模型：BALB/c裸鼠[1]剂量：30和100mg/kg给药：口服强饲法；30和100mg/kg；每三天；30天结果：显着抑制肿瘤生长。

[参考文献]

[1]. Xing Y, et al. Fraxinellone has anticancer activity in vivo by inhibiting programmed cell death-ligand 1 expression by reducing hypoxia-inducible factor-1α and STAT3. Pharmacol Res. 2018 Sep;135:166-180.

梣酮物理化学性质

[ 密度 ]:
1.2±0.1 g/cm3

[ 沸点 ]:
372.9±30.0 °C at 760 mmHg

[ 熔点 ]:
116ºC

[ 分子式 ]:
C₁₄H₁₆O₃

[ 分子量 ]:
232.275

[ 闪点 ]:
179.3±24.6 °C

[ 精确质量 ]:
232.109940

[ PSA ]:
39.44000

[ LogP ]:
2.85

[ 外观性状 ]:
固体;White to Almost white powder to crystal

[ 蒸汽压 ]:
0.0±0.8 mmHg at 25°C

[ 折射率 ]:
1.552

[ 储存条件 ]:
-20°C;避免加热

梣酮毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: TI3767000

CHEMICAL NAME :: Phthalide, 3-(3-furyl)-3a,4,5,6-tetrahydro-3a,7-dimethyl-

CAS REGISTRY NUMBER :: 28808-62-0

LAST UPDATED :: 198910

DATA ITEMS CITED :: 5

MOLECULAR FORMULA :: C14-H16-O3

MOLECULAR WEIGHT :: 232.30

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 274 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: PLMEAA Planta Medica. (Georg Thieme Verlag, Postfach 732, D-7000 Stuttgart 1, Fed. Rep. Ger.) V.1- 1953- Volume(issue)/page/year: 53,399,1987

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 116 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: PLMEAA Planta Medica. (Georg Thieme Verlag, Postfach 732, D-7000 Stuttgart 1, Fed. Rep. Ger.) V.1- 1953- Volume(issue)/page/year: 53,399,1987

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 430 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: PLMEAA Planta Medica. (Georg Thieme Verlag, Postfach 732, D-7000 Stuttgart 1, Fed. Rep. Ger.) V.1- 1953- Volume(issue)/page/year: 53,399,1987

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 355 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: PLMEAA Planta Medica. (Georg Thieme Verlag, Postfach 732, D-7000 Stuttgart 1, Fed. Rep. Ger.) V.1- 1953- Volume(issue)/page/year: 53,399,1987 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 424 mg/kg

SEX/DURATION :: female 5-8 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - female fertility index (e.g. # females pregnant per # sperm positive females; # females pregnant per # females mated)

REFERENCE :: PLMEAA Planta Medica. (Georg Thieme Verlag, Postfach 732, D-7000 Stuttgart 1, Fed. Rep. Ger.) V.1- 1953- Volume(issue)/page/year: 53,399,1987

梣酮安全信息

[ 符号 ]:

GHS06

[ 信号词 ]:
Danger

[ 危害声明 ]:
H301

[ 警示性声明 ]:
P301 + P310

[ 危害码 (欧洲) ]:
Xn

[ 安全声明 (欧洲) ]:
24/25

[ 危险品运输编码 ]:
UN 2811 6.1/PG III

[ RTECS号 ]:
TI3767000

[ 包装等级 ]:
III

梣酮

梣酮用途

梣酮名称

梣酮生物活性

梣酮物理化学性质

梣酮毒性和生态

CHEMICAL IDENTIFICATION

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

梣酮安全信息

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