Acacetin

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Chemical Structure| 480-44-4 同义名 : 5,7-Dihydroxy-4'-methoxyflavone; LY064233; Acacetin. NSC 76061.; NSC 76061
CAS号 : 480-44-4
货号 : A123393
分子式 : C16H12O5
纯度 : 98%
分子量 : 284.26
MDL号 : MFCD00016936
存储条件:

Pure form Keep in dark place, inert atmosphere, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 120 mg/mL(422.14 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
描述 Acacetin is an orally active flavonoid derived from Tephroseris kirilowii (Turcz.) Holub. Acacetin (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. Acacetin (50-150 μM; 24 hours) causes G2/M cell cycle arrest and induces apoptosis and autophagy and leads to decreases in levels of PI3Kγ-p110, p-AKT, p-mTOR, p-p70S6K, and p-ULK in a dose-dependent manner[3]. Acacetin significantly inhibited the release of NO and prostaglandin E(2) and the expression of inducible NO synthase and cyclooxygenase-2 in LPS-stimulated BV-2 cells. The compound also reduced proinflammatory cytokines, TNF-α and IL-1β, and inhibited the activation of NF-κB and p38 MAPK[4]. The natural compound, acacetin, inhibits glutamate release from hippocampal synaptosomes by attenuating voltage-dependent Ca(2+) entry and effectively prevents KA-induced in vivo excitotoxicity[5]. Acacetin (1.8-56.2 mg/kg/day; ip; single dose) decreases visceral and inflammatory nociception and prevented the formalin-induced oedema[4]. Chronic acatetin (5, 15 or 45 mg/kg, p.o., once per day for three weeks) administration to mice engenders antidepressant-like efficacy on both behavior and stress axis responsivity, with serotonergic system that preferentially couples with 5-HT1A receptors being critically involved. In vitro, acacetin (1-100 nM) increased the Emax of 8-OH-DPAT[6]. Intravenous infusion of acacetin prodrug (3, 6 and 12 mg/kg) terminated experimental AF without increasing ECG QTc interval in beagle dogs. The intravenous LD50 of acacetin prodrug was 721 mg/kg in mice[7].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.52mL

0.70mL

0.35mL

17.59mL

3.52mL

1.76mL

35.18mL

7.04mL

3.52mL

参考文献

[1]Wang X, Perumalsamy H, et al. Effects and possible mechanisms of action of acacetin on the behavior and eye morphology of Drosophila models of Alzheimer's disease. Sci Rep. 2015 Nov 4;5:16127.

[2]Jung SK, Kim JE, et al. The P110 subunit of PI3-K is a therapeutic target of acacetin in skin cancer. Carcinogenesis. 2014 Jan;35(1):123-30.

[3]Zhang HW, Hu JJ, Fu RQ, Liu X, Zhang YH, Li J, Liu L, Li YN, Deng Q, Luo QS, Ouyang Q, Gao N. 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

[4]Ha SK, Moon E, Lee P, Ryu JH, Oh MS, Kim SY. Acacetin attenuates neuroinflammation via regulation the response to LPS stimuli in vitro and in vivo. Neurochem Res. 2012 Jul;37(7):1560-7

[5]Lin TY, Huang WJ, Wu CC, Lu CW, Wang SJ. Acacetin inhibits glutamate release and prevents kainic acid-induced neurotoxicity in rats. PLoS One. 2014 Feb 10;9(2):e88644

[6]Xiao WZ, Zhou WH, Ma Q, Cui WG, Mei QY, Zhao X. Serotonergically dependent antidepressant-like activity on behavior and stress axis responsivity of acacetin. Pharmacol Res. 2019 Aug;146:104310

[7]Liu H, Wang YJ, Yang L, Zhou M, Jin MW, Xiao GS, Wang Y, Sun HY, Li GR. Synthesis of a highly water-soluble acacetin prodrug for treating experimental atrial fibrillation in beagle dogs. Sci Rep. 2016 May 10;6:25743