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Daphnetin
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Daphnetin图片
CAS NO:486-35-1
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品名称
瑞香素
7,8-Dihydroxycoumarin
产品介绍
Daphnetin (7,8-dihydroxycoumarin) 是一种香豆素衍生物,可来源于 GenusDaphne,是一种口服有效的蛋白激酶抑制剂 (protein kinase),对 EGFR、PKA 和 PKC 的IC50值分别为 7.67 μM、9.33 μM 和 25.01 μM。Daphnetin 触发活性氧诱导的细胞凋亡 (apoptosis) 和通过调节 AMPK/Akt/mTOR 途径诱导细胞保护性自噬(autophagy)。Daphnetin 具有抗炎活性,并抑制 TNF-α、IL-1ss、ROS 和 MDA 的产生。Daphnetin 具有杀疟活性。瑞香素可用于类风湿关节炎、癌症和抗疟疾研究。
生物活性

Daphnetin (7,8-dihydroxycoumarin), one coumarin derivative can be found inplantsof the GenusDaphne, is a potent, oral activeprotein kinaseinhibitor, withIC50sof 7.67 μM, 9.33 μM and 25.01 μM forEGFR,PKAandPKCin vitro, respectively. Daphnetin triggers ROS-induced cellapoptosisand induces cytoprotectiveautophagyby modulating the AMPK/Akt/mTOR pathway. Daphnetin has anti-inflammation activitity and inhibits TNF-α, IL-1ss, ROS, and MDA production. Daphnetin has schizontocidal activity against malaria parasites. Daphnetin can be used for rheumatoid arthritis ,cancerand anti-malarian research[1][2][3][4].

IC50& Target[4]

EGFR

7.67 μM (IC50)

Plasmodium

 

PKA

9.33 μM (IC50)

PKC

25.01 μM (IC50)

体外研究
(In Vitro)

Daphnetin (7,8-dihydroxycoumarin) (0-40 μg/mL; 24-48 hours) inhibits the proliferation of ovarian cancer cells[1].
Daphnetin (7,8-dihydroxycoumarin) (0-40 μg/mL; 24 hours; A2780 cells) induces apoptosis and increases ROS production in a dose-dependent manner[1].
Daphnetin (7,8-dihydroxycoumarin) (0-40 μg/mL; 24 hours; A2780 cells) induces autophagy through modulation of the AMPK/Akt/mTOR pathway[1].
Daphnetin (7,8-dihydroxycoumarin) (1-10 μM; plasmodium falciparum) exhibits schizontocidal activity in a dose-dependent manner[3].

Cell Viability Assay[1]

Cell Line:IOSE8C, A2780, SKOV3 and OVCAR8 cells
Concentration:0, 5, 10, 20 and 40 μg/mL
Incubation Time:24 h and 48 hours
Result:Inhibited growth in ovarian cancer cells but not in normal cells.

Apoptosis Analysis[1]

Cell Line:A2780 and SKOV3 cells
Concentration:0, 10, 20 and 40 μg/mL
Incubation Time:24 hours
Result:Increased apoptosis in a dose-dependent manner in A2780 and SKOV3 cells.

Western Blot Analysis[1]

Cell Line:A2780 and SKOV3 cells
Concentration:0, 10, 20 and 40 μg/mL
Incubation Time:24 hours
Result:Increased proapoptotic protein (Caspase 3, Bax, and PARP) expression but decreased antiapoptotic protein (Bcl2) expression.

Western Blot Analysis[1]

Cell Line:A2780 cells
Concentration:0, 10, 20 and 40 μg/mL
Incubation Time:24 hours
Result:Increased LC3 II and p62 expression in a dose-dependent manner and reduced the expression levels of p-Akt, p-mTOR, but increased the expression level of p-AMPK.
体内研究
(In Vivo)

Daphnetin (7,8-dihydroxycoumarin) (30 mg/kg; i.p.; daily; for 12 days; BALB/c nude mice) has antitumour activities in a xenograft animal model[1].
Daphnetin (7,8-dihydroxycoumarin) (2.5-10 mg/kg; i.p.; daily; for three days; C57BL/6 mice) inhibits cisplatin-induced inflammation, decreases TNF-α, IL-1β, ROS and MDA production in a dose-dependent manner in kidney tissues. Daphnetin inhibits cisplatin-induced NF-κB activation and up-regulated Nrf2 and HO-1[2].
Daphnetin (7,8-dihydroxycoumarin) (10-100 mg/kg; i.g. and i.p.; every four days, for 30 days; male Kunming outbred strain mice) displays certain schizontocidal activity in vivo[3].

Animal Model:BALB/c nude mice[1]
Dosage:30 mg/kg
Administration:Intraperitoneal injection; Daily; for 12 days
Result:Decreased tumor volume and weight in a xenograft animal model.
Animal Model:Male Kunming outbred strain mice[3]
Dosage:10, 50 or 100 mg/kg
Administration:Oral gavage and intraperitoneal injection; every four days, for 30 days
Result:Reduced the number of parasites in mice.
分子量

178.14

性状

Solid

Formula

C9H6O4

CAS 号

486-35-1

中文名称

瑞香素

结构分类
  • Phenylpropanoids
  • Coumarins
  • Phenols
  • Polyphenols
来源
  • Plants
  • Thymelaeaceae
  • Daphne
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 50 mg/mL(280.68 mM;Need ultrasonic)

H2O : 1 mg/mL(5.61 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM5.6136 mL28.0678 mL56.1356 mL
5 mM1.1227 mL5.6136 mL11.2271 mL
10 mM0.5614 mL2.8068 mL5.6136 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40%PEG300   5%Tween-80   45% saline

    Solubility: ≥ 2.5 mg/mL (14.03 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (14.03 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20%SBE-β-CDin saline)

    Solubility: ≥ 2.5 mg/mL (14.03 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (14.03 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90%corn oil

    Solubility: ≥ 2.5 mg/mL (14.03 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (14.03 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在本网站选购。