(E)-Cardamonin ((E)-Cardamomin) is a novel antagonist of hTRPA1 cation channel with an IC50 of 454 nM.
体外研究
(E)-Cardamonin ((E)-Cardamomin) selectively blocksTRPA1 activation (IC50=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.
分子式
C16H14O4
分子量
270.28
CAS号
19309-14-9
中文名称
小豆蔻明
运输条件
Room temperature in continental US; may vary elsewhere.