野鸦椿酸 TN1134

Product Introduction
Bioactivity


英文名: Euscaphic acid

描述: Euscaphic acid 是来源于枣的一种三萜，是DNA 聚合酶抑制剂，可诱导细胞凋亡。它抑制小牛 DNA 聚合酶 α 和大鼠 DNA 聚合酶 β 的IC50值分别为 61 和 108 μM。

体外活性: Isolated aorta was used to test the anti-contraction effects and the possible mode of action(s) of the EA (1*10 -7 M) and (3*10 -7 M) isolated from Crataegus azarolus var. aronia L. Euscaphic acid showed high anti-contraction effects on norepinephrin (NE), (1*10 -9 -10 -4 M) induced contraction in aortic smooth muscle cells in endothelium-intact, endothelium-denuded, and aortic rings pre-incubated with potassium (K + )-channels blocker (tetraethylammonium, TEA), prostaglandin I 2 (PGI ) inhibitor (indomethacin) and cyclic guanosine monophosphate (cGMP) inhibitor ( methylene blue). On the other hand, other K 2 channels subtype blockers glibenclamide (GLIB); barium chloride (BaCl ) and 4-aminopyridine (4-AP) demonstrated that adenosine triphosphate sensitive K + (K ATP ), inwardly rectifying K 2 + (K ir ) and voltage-dependent K ) channels played no role in anti-contraction induced by EA. Furthermore, the role of L-types calcium (Ca ) channels in EA anti-contractile effects on aortic smooth muscle cells was proved, by using the Ca -channel blocker verapamil, as indicated by the production of a potent anti-contraction effect . The results of the current study indicate that the anti-contraction effects of EA may be due to the activation of calcium dependent, K ) channels and blocking of L-type Ca ++ channels.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 50 mg/mL (102.31 mM)


关键字: Inhibitor | PI3K | inhibit | Euscaphic acid | Apoptosis | Phosphoinositide 3-kinase | DNA/RNA Synthesis

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