Kuraridine

Names

[ Name ]:
Kuraridine

[Synonym ]:
6'-methoxy-2,4,2',4'-tetrahydroxy-3'-lavandulylchalcone
kuraridin
kuraridine
(E)-1-[2,4-Dihydroxy-3-(2-isopropenyl-5-methyl-hex-4-enyl)-6-methoxy-phenyl]-3-(2,4-dihydroxy-phenyl)-propenone

Biological Activity

[Description]:

Kuraridine is a prenylated flavonol extract from the roots of Sophora flavescens. Kuraridine an inhibitory effect on cGMP specific phosphodiesterase type 5 (PDE5) and has an IC50 of 0.64 μM[1].

[Related Catalog]:

Signaling Pathways >> Metabolic Enzyme/Protease >> Phosphodiesterase (PDE)

Research Areas >> Others

[Target]

PDE5:0.64 μM (IC50)

[In Vitro]

Kuraridine shows potent inhibitory activity (IC50=0.64 μM) against cGMP PDE5 with 2.0- and 12.9-fold selectivity over PDE3 and PDE4, respectively[1]. Kuraridine induces pronounced chloride inward currents in the absence of GABA. Thecurrents does not exceed 10% of the maximal IGABA induced by a saturating GABA concentration (1 mM)[2]. Kuraridine induces a concentration–response curves for IGABA enhancement (EC50=4.0±2.4 μM) in Xenopus oocytes expressing GABAA receptors composed of α1, β2, and γ2S subunits[2].

[References]

[1]. Hye Joo Shin, et al. A prenylated flavonol, sophoflavescenol: a potent and selective inhibitor of cGMP phosphodiesterase 5. Bioorg Med Chem Lett. 2002 Sep 2;12(17):2313-6.

[2]. Xinzhou Yang, et al. HPLC-based activity profiling for GABAA receptor modulators from the traditional Chinese herbal drug Kushen (Sophora flavescens root). Mol Divers. 2011 May;15(2):361-72.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₆H₃₀O₆

[ Molecular Weight ]:
438.51300

[ Exact Mass ]:
438.20400

[ PSA ]:
107.22000

[ LogP ]:
5.50480