In vitro: (E)-Cardamonin selectively blocksTRPA1 activation (IC50=454 nM) while does not interact with TRPV1 nor TRPV4 channel. Docking analysis of (E)-Cardamonin demonstrates a compatible interaction with A-967079-binding site of TRPA1. (E)-Cardamonin does not significantly reduce HEK293 cell viability, nor does it impair cardiomyocyte constriction. (E)-Cardamonin 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. Cardamonin (Cardamomin) also acts as an aryl hydrocarbon receptor (AhR) activator.
In vivo: (E)-Cardamonin (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.
J Inflamm Res. 2023 Nov 27;16:5601-5612.
The Nrf2 Pathway Alleviates Overloading Force-Induced TMJ Degeneration by Downregulating Oxidative Stress Reactions
(E)-Cardamonin purchased from AbMole
| Cell Experiment | |
|---|---|
| Cell lines | HEK293 cells |
| Preparation method | HEK293 cells were seeded into 96-well plates at a cell density of 3.5 x 10^4 cells per well, the plates were kept at 37℃ with 5% CO2 overnight. On the following day, cardamonin was added to the cells from a top concentration of 90 μM. The cells treated in the absence of the test compound were the negative control. |
| Concentrations | 90 μM. |
| Incubation time | 24 h |
| Animal Experiment | |
|---|---|
| Animal models | female C57BL/6 mice |
| Formulation | -- |
| Dosages | 50 mg/kg |
| Administration | oral gavage |
| Molecular Weight | 270.28 |
| Formula | C16H14O4 |
| CAS Number | 19309-14-9 |
| Solubility (25°C) | DMSO ≥ 55 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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