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Desmethoxyyangonin

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Chemical Structure| 15345-89-8 同义名 : 去甲氧基醉椒素 ;5,6-Dehydrokavain;Demethoxyyangonin;trans-5,6-Dehydrokavain;NSC 112161;NSC 68686
CAS号 : 15345-89-8
货号 : A851979
分子式 : C14H12O3
纯度 : 98%
分子量 : 228.243
MDL号 : MFCD00221730
存储条件：

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 15 mg/mL(65.72 mM)，配合低频超声，并水浴加热至45℃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 Monoamine oxidases (MAOs) are mitochondrial bound enzymes, which catalyze the oxidative deamination of monoamine neurotransmitters. Inside the brain, MAOs are present in two isoforms: MAO-A and MAO-B. The activity of MAO-B is generally higher in patients affected by neurodegenerative diseases like Alzheimer's and Parkinson's[2]. Kava-kava, a psychoactive beverage, induces relaxation, improves social interaction, promotes sleep and plays an important role in the sociocultural life in the islands of the South Pacific. Kava pyrones, the major constituents of kava kava, are generally considered to be responsible for the pharmacological activity in humans and animals. Desmethoxyyangonin, one of the six major kava pyrones found in the Piper methysticum (kava-kava) plant, is a reversible inhibitor of MAO-B. As the most potent kava pyrone, desmethoxyyangonin displays a competetive inhibition pattern with mean Ki 0.28 µM[3]. A small dose of kava extract (20 mg/kg body weight i.p.) caused changes in rat behaviour and concentrations of dopamine in the nucleus accumbens. Higher doses (120 mg/kg i.p.) increased the levels of dopamine[4]. Among the kava pyrones, only desmethoxyyangonin markedly induced the expression of CYP3A23[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

4.38mL

0.88mL

0.44mL

21.91mL

4.38mL

2.19mL

43.81mL

8.76mL

4.38mL
参考文献

[1]Uebelhack R, et al. Inhibition of platelet MAO-B by kava pyrone-enriched extract from Piper methysticum Forster (kava-kava). Pharmacopsychiatry. 1998 Sep;31(5):187-92.

[2]Carradori S, D'Ascenzio M, Chimenti P, Secci D, Bolasco A. Selective MAO-B inhibitors: a lesson from natural products. Mol Divers. 2014;18(1):219-243.

[3]Uebelhack R, Franke L, Schewe HJ. Inhibition of platelet MAO-B by kava pyrone-enriched extract from Piper methysticum Forster (kava-kava). Pharmacopsychiatry. 1998;31(5):187-192.

[4]Baum SS, Hill R, Rommelspacher H. Effect of kava extract and individual kavapyrones on neurotransmitter levels in the nucleus accumbens of rats. Prog Neuropsychopharmacol Biol Psychiatry. 1998;22(7):1105-1120.

[5]Ma Y, Sachdeva K, Liu J, et al. Desmethoxyyangonin and dihydromethysticin are two major pharmacological kavalactones with marked activity on the induction of CYP3A23. Drug Metab Dispos. 2004;32(11):1317-1324.