| 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) |
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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. |
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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. |
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| 结构分类 | - Phenylpropanoids
- Coumarins
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| 来源 | - Plants
- Thymelaeaceae
- Daphne
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 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 | 1 mM | 5.6136 mL | 28.0678 mL | 56.1356 mL | | 5 mM | 1.1227 mL | 5.6136 mL | 11.2271 mL | | 10 mM | 0.5614 mL | 2.8068 mL | 5.6136 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。 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。 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。
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