CAS |
38183-03-8 |
Chinese Name |
7,8-二羟基黄酮 |
English Name |
7,8-Dihydroxyflavone |
Synonyms |
7,8-DHF |
Molecular Formula |
C15H10O4 |
Molecular Weight |
254.24 |
Solubility |
Soluble in DMSO ≥20mg/mL |
Purity |
HPLC≥98% |
Appearance |
Light yellow to green Solid |
Storage |
Powder:2-8℃,2 years;Insolvent(Mother Liquid):-20℃,6 months;-80℃,1 year |
EC |
EINECS 253-812-4 |
MDL |
MFCD00006836 |
SMILES |
O=C1C=C(C2=CC=CC=C2)OC3=C(O)C(O)=CC=C13 |
InChIKey |
COCYGNDCWFKTMF-UHFFFAOYSA-N |
InChI |
InChI=1S/C15H10O4/c16-11-7-6-10-12(17)8-13(19-15(10)14(11)18)9-4-2-1-3-5-9/h1-8,16,18H |
PubChem CID |
1880 |
Target Point |
Trk Receptor |
Passage |
Protein Tyrosine Kinase/RTK;Neuronal Signaling |
Background |
7,8-Dihydroxyflavone is a potent and selective TrkB agonist. |
Biological Activity |
7,8-Dihydroxyflavone (7,8-DHF) 是有效的、选择性的TrkB受体激动剂(Kd≈320 nM)。TrkB受体是脑源性神经营养因子的主要信号受体。[1-3] |
IC50 |
TrkB receptor:320nM(Kd) [1] |
In Vitro |
250nM 7,8-DHF特异性激活TrkB,而不激活TrkA或TrkC。除了大脑皮质和海马神经元,7,8-DHF还保护其他细胞如视网膜神经节细胞(RGC)和PC12细胞免受氧化应激诱导的凋亡和细胞死亡。因此,7,8-DHF具有神经保护作用[1]。 |
In Vivo |
7,8-Dihydroxyflavone是一种具有生物效应的化合物,对小鼠进行腹腔注射或口服给药后,7,8-Dihydroxyflavone能够穿过血脑屏障、激活TrkB及其下游PI3K/Akt和MAPK。7,8-DHF在外伤性脑损伤时促进皮层神经元的生存能力、减少其凋亡。在受伤后3小时进行7,8-DHF给药,7,8-DHF能通过PI3K/Akt信号通路途径减少组织损伤。7,8-DHF的处理在小鼠中并不诱导任何明显的毒性作用,长期给药对小鼠没有毒性。7,8-DHF对阿尔茨海默病有较强的治疗效果,能通过激活肌肉TrkB抑制肥胖[1]。 |
Cell Experiment |
PC12 cells以104/孔的密度接种于96孔板。用1-25 μM 7,8-DHF对细胞进行预处理,处理1小时,然后将细胞用6-OHDA处理24小时。在7,8-DHF处理前,加入PI3K抑制剂LY294002或MEK抑制剂PD98059孵育30分钟。实验结束后,PC12细胞用20 μl MTT溶液孵育4小时(37 C),深蓝色的甲瓒产物溶解于150μl DMSO中,测定其在570 nm处的吸光值。[3] |
Animal Experiment |
Animal Models: Wistar雄性大鼠;APPswe/PS1dE9 雄性转基因小鼠; Dosages: 0.1 mg/kg,0.3 mg/kg,1 mg/kg和3 mg/kg(大鼠);0.1 mg/kg(小鼠);Administration: 腹腔注射[2] |
Data Literature Source |
[1] Liu C,et al. Transl Neurodegener. 2016,5:2. [2] Bollen E,et al. Behav Brain Res. 2013,257:8-12. [3] Han XH,et al. Neurosci Lett. 2014,581:85-8. |
Unit |
Bottle |
Specification |
20mg 50mg 100mg |