Composition for bkca channel activation

Abstract

The present invention relates to novel compounds capable of activating BKCa channels. The use of a composition of the present invention can effectively activate the BKCa channels, and can be used for prevention or treatment of various diseases caused by the deactivation of BKCa channels or the degradation of BKCa channel activity.

1 . A composition for BK Ca  channel activation, wherein the composition contains a flavanone derivative represented by a following chemical formula 1, or a pharmaceutically acceptable salt thereof: 
       
         
           
           
               
               
           
         
         wherein, in the chemical formula 1, R 1  is a hydrophobic substituent selected from a group consisting of hydrogen and straight-chain or branched-chain C 1 -C 15  alkyl or alkenyl; 
         wherein when R 1  is C 6 -C 15  alkyl or alkenyl, R 2  is C 1 -C 4  alkoxy, wherein when R 1  is hydrogen or C 1 -C 5  alkyl or alkenyl, R 2  is hydroxy; 
         wherein each of R 3 , R 4  and R 5  is independently hydrogen or hydroxy, wherein at least one of R 3 , R 4  and R 5  is hydroxy. 
       
     
     
         2 . The composition of  claim 1 , wherein when R 1  is C 6 -C 15  alkyl or alkenyl, R 2  is methoxy. 
     
     
         3 . The composition of  claim 1 , wherein R 1  is hydrogen, 3-methyl-2-buten-1-yl, or 2-isopropenyl-5-methyl-4-hexen-1-yl. 
     
     
         4 . The composition of  claim 3 , wherein when R 1  is hydrogen, R 2  is hydroxy. 
     
     
         5 . The composition of  claim 3 , wherein when R 1  is 3-methyl-2-butene-1-yl, R 2  is hydroxy. 
     
     
         6 . The composition of  claim 3 , wherein when R 1  is 2-isopropenyl-5-methyl-4-hexen -1-yl, R 2  is methoxy. 
     
     
         7 . The composition of  claim 1 , wherein R 4  is hydroxy, and, each of R 3  and R 5  is independently hydrogen or hydroxy. 
     
     
         8 . The composition of  claim 7 , wherein at least one of R 3  and R 5  is hydrogen. 
     
     
         9 . The composition of  claim 1 , wherein the flavanone derivative represented by the chemical formula 1 is a compound selected from a group consisting of kurarinone, naringenin and leachianone G. 
     
     
         10 . The composition of  claim 1 , wherein the composition shifts a conductance-voltage (G-V) correlation of the BK Ca  channel toward a negative voltage. 
     
     
         11 . A composition for preventing or treating BK Ca  channel activity degradation-related condition, disease or disorder, wherein the composition includes the composition for BK Ca  channel activation of  claim 1 . 
     
     
         12 . The composition of  claim 11 , wherein the BK Ca  channel activity degradation-related condition, disease or disorder is cardiovascular disease, obstructive or inflammatory airways disease, lower urinary tract disorder, impotence, anxiety and anxiety-related condition, epilepsy or pain.