- 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
- 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。
- 小豆蔻明具有抗菌、止呕、健脾的作用。
- 用于含量测定/鉴定/药理实验等
(R)-(-)-4-烯基-2-戊醇;(R)-(-)-4-戊烯-2-醇;(R)-(-)-4-戊烯酸基-2-醇;(2R)-4-戊烯-2-醇;(R)-戊-4-烯-2-醇; (R)-(-)-2-HYDROXYPENT-4-ENE;(R)-(-)-PENTEN-2-OL;(r)-(-)-4-penten-2-ol;(1R)-1-Methyl-3-butene-1-ol;(2R)-4-Pentene-2-ol;(2R)-pent-4-en-2-ol;4-Penten-2-ol, (2R)-;(
R
)-(?)-4-Penten-2-ol