生物活性

Acacetin (5,7-Dihydroxy-4'-methoxyflavone) is an orally active flavonoid derived from Tephroseris kirilowii (Turcz.) Holub. Acacetin docks in the ATP binding pocket of PI3Kγ. Acacetin causes cell cycle arrest and induces apoptosis and autophagy in cancer cells. Acacetin has potent anti-cancer and anti-inflammatory activity and has the potential for pain-related diseases research^[1][2].

体外研究
(In Vitro)

Acacetin (5,7-Dihydroxy-4'-methoxyflavone; 10-200 μM; 24 hours) decreases cell viabilities in a dose-dependent manner. Acacetin has little effect on human normal glial cell line HEB and non-tumorigenic epithelial cell line MCF-10A^[1].
Acacetin (50-150 μM; 24 hours) causes G2/M cell cycle arrest and induces apoptosis and autophagy^[1].
Acacetin (50-150 μM; 24 hours) leads to decreases in levels of PI3Kγ-p110, p-AKT, p-mTOR, p-p70S6K, and p-ULK in a dose-dependent manner^[1].Cell Viability Assay^[1]

体内研究
(In Vivo)

Acacetin (5,7-Dihydroxy-4'-methoxyflavone; 5, 20 mg/kg/day; orally; for 3 days) significantly suppresses microglial activation in an LPS-induced neuroinflammation mouse model^[2].
Acacetin (25 mg/kg/day; orally; for 3 days) reduces neuronal cell death in an animal model of ischemia^[2].
Acacetin (1.8-56.2 mg/kg/day; ip; single dose) decreases visceral and inflammatory nociception and prevented the formalin-induced oedema^[3].

分子量

284.26

Formula

C??H??O?

CAS 号

480-44-4

中文名称

金合欢素；刺槐黄素

SMILES

O=C1C=C(C2=CC=C(OC)C=C2)OC3=CC(O)=CC(O)=C13

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

溶解性数据

In Vitro: 

DMSO : ≥ 37 mg/mL (130.16 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

*

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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 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    90% corn oil

Solubility: ≥ 2.08 mg/mL (7.32 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (7.32 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 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

参考文献

[1]. Hong-Wei Zhang, et al. Flavonoids inhibit cell proliferation and induce apoptosis and autophagy through downregulation of PI3Kγ mediated PI3K/AKT/mTOR/p70S6K/ULK signaling pathway in human breast cancer cells. Sci Rep. 2018 Jul 26;8(1):11255.

[2]. Sang Keun Ha, et al. Acacetin attenuates neuroinflammation via regulation the response to LPS stimuli in vitro and in vivo. Neurochem Res. 2012 Jul;37(7):1560-7.

[3]. A I Carballo-Villalobos, et al. Evidence of mechanism of action of anti-inflammatory/antinociceptive activities of acacetin. Eur J Pain. 2014 Mar;18(3):396-405.