中文同义词:
小豆蔻明;(E)-1-(2,4-二羟基-6-甲氧基苯基)-3-苯基丙-2-烯-1-酮;豆寇明(小豆蔻明;小豆蔻明, >98%;小豆蔻明, 来源于草豆蔻;小豆蔻明、豆蔻素、小豆蔻查耳酮;豆寇明(小豆蔻明,豆蔻素,小豆蔻查耳酮);豆蔻素、小豆蔻查耳酮
英文同义词:
Alpinetin chalcone;Chalcone, 2, 4-dihydroxy-6-methoxy-;(E)-2,4-Dihydroxy-6-methoxychalcone;(E)-1-(2,4-Dihydroxy-6-methoxyphenyl)-3-phenylprop-2-en-1-one;Cardamonin;(E)-1-(2,4-Dihydroxy-6-methoxyphenyl)-3-phenyl-2-propen-1-one;2-Propen-1-one, 1-(2,4-dihydroxy-6-methoxyphenyl)-3-phenyl-, (2E)-;CARDAMONIN(RG)
相关类别:
小分子抑制剂，天然产物;植物提取物;对照品;小分子抑制剂;中药对照品;标准品;Chalcones;Inhibitors;对照品-中药对照品;查尔酮;标准品 -中药标准品;分析试剂-对照品;标准品，对照品
沸点
484.5±45.0 °C(Predicted)
密度
1.282±0.06 g/cm3(Predicted)
酸度系数(pKa)
7.00±0.40(Predicted)
理化性质
小豆蔻明(Cardamonin)，为黄色针晶，易溶于甲醇、乙醇、醋酸乙酯，乙醚，稀碱溶液，难溶于水，与醋酸铅反应呈黄色沉淀。小豆蔻明可以明显抑制络氨酸酶的活性，同时可以有效抑制黑色素细胞增殖和黑色素的合成，效果明显超过其他成分。
生物活性
(E)-Cardamonin ((E)-Cardamomin) 是新颖的hTRPA1阳离子通道拮抗剂，IC50值为454 nM。
靶点
Target Value
NF-κB
(Cell-free assay)
TRPA1
(Cell-free assay) 454 nM
TRPA1
(Cell-free assay)
454 nM
体外研究
(E)-Cardamonin ((E)-Cardamomin) selectively blocksTRPA1 activation (IC 50 =454 nM) while does not interact with TRPV1 nor TRPV4 channel. Docking analysis of cardamonin demonstrates a compatible interaction with A-967079-binding site of TRPA1. (E)-Cardamonin ((E)-Cardamomin) does not significantly reduce HEK293 cell viability, nor does it impair cardiomyocyte constriction. (E)-Cardamonin ((E)-Cardamomin) suppresses the expression of Tgase-2, cyclooxygenase-2 (COX-2), and p65 (nuclear factor-κB) in a concentration-dependent manner, and restores the expression of IκB in MG63 and Raw264.7 cells.
体内研究
(E)-Cardamonin ((E)-Cardamomin) (3-30 mg/kg, orally administered) significantly inhibits PBQ-induced writhing. CDN also produces a significant, dose-dependent increase in the withdrawal response latencies in carrageenan-induced hyperalgesia.
化学性质
黄色结晶性粉末，可溶于甲醇、乙醇、DMSO等有机溶剂，来源于草豆蔻。
危险品运输编号
UN 3077 9 / PGIII
