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Daphnetin

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Chemical Structure| 486-35-1 同义名 : 7,8-Dihydroxycoumarin;NSC 633563
CAS号 : 486-35-1
货号 : A811058
分子式 : C9H6O4
纯度 : 95%
分子量 : 178.142
MDL号 : MFCD00016977
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(280.68 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • PKC

    PKC, IC50:25.01 μM

  • EGFR/ErbB1

    EGFR, IC50:7.67 μM

  • PKA

    PKA, IC50:9.33 μM
描述 Daphnetin (7,8-dihydroxycoumarin, DAP) is a 7, 8 dihydroxy coumarin isolated from different medicinal plants of the Thymelaeaceae family and exhibits copious pharmacological activities including neuroprotection, anti-cancer, anti-malarial, anti-inflammatory, anti-parasitic and anti-arthritic activity, The inhibition of EGF receptor tyrosine kinase by daphnetin was competitive to ATP and non-competitive to the peptide substrate[3]. DAP markedly decreased cell viability and induced the apoptosis of CIA-FLS along with typical morphological and ultrastructural changes; moreover, DAP increased FasL, cytochrome c (Cyt-c), Bax, caspase-3, caspase-8, and caspase-9 mRNA expression and Bax, caspase-3, caspase-8, and caspase-9 protein expression[4]. Daphnetin attenuated H2O2-induced apoptosis in a concentration-dependent manner, reduced the cleavage of poly ADP ribose polymerase and caspase 3, and inhibited the phosphorylation of p38 MAPK and c-Jun N-terminal kinases (JNK) in H2O2-induced PC12 cells. In addition, daphnetin induced the expression of HSP70 in a dose- and time-dependent manner, and daphnetin-induced HSP70 expression was reduced by ERK 1/2 inhibitor U0126 in PC12 cells[5]. Both in vitro and in vivo results indicate that DAP exerts a protective effect against IL-1β in chondrocytes. In vitro ,DAP inhibits the expression of IL-6, IL-12, MMP-3, MMP-9 and MMP-13, induced by IL-1β in rabbit chondrocytes, and stimulates the production of IL-10. The inhibitory effect of DAP on the MMPs is partially regulated by the inhibition of the PI3K/AKT, MAPK and NF-κB signaling pathways. The effect of DAP on OA may be attributed to the suppression of inflammatory factor secretion, chondrocyte apoptosis observed by the decrease in pro-apoptotic Caspase-3 and BAX, and the activation of anti-apoptotic BCL-2[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

5.61mL

1.12mL

0.56mL

28.07mL

5.61mL

2.81mL

56.13mL

11.23mL

5.61mL
参考文献

[1]Jimenez-Orozco FA, Rosales AA, et al. Differential effects of esculetin and daphnetin on in vitro cell proliferation and in vivo estrogenicity. Eur J Pharmacol. 2011 Oct 1;668(1-2):35-41.

[2]J Yang EB, Zhao YN, et al. Daphnetin, one of coumarin derivatives, is a protein kinase inhibitor. Biochem Biophys Res Commun. 1999 Jul 14;260(3):682-5.

[3] Lovedeep Singh,et al. Mechanistic interplay of various mediators involved in mediating the neuroprotective effect of daphnetin. Pharmacol Rep. 2021 Apr 16.

[4]Mao Zheng,et al. Daphnetin induces apoptosis in fibroblast-like synoviocytes from collagen-induced arthritic rats mainly via the mitochondrial pathway, Cytokine. 2020 Sep;133:155146.

[5]Zhilin Qi,et al. Daphnetin protects oxidative stress-induced neuronal apoptosis via regulation of MAPK signaling and HSP70 expression. Oncol Lett. 2016 Sep;12(3):1959-1964.

[6]Xiaohan Zhang,et al. Chondroprotective and antiarthritic effects of Daphnetin used in vitro and in vivo osteoarthritis models. Life Sci. 2020 Jan 1;240:116857.