US2007053998A1PendingUtilityA1

Butanol extract of Bidens pilosa

Assignee: ACADEMIA SINICAPriority: Sep 2, 2005Filed: Sep 2, 2005Published: Mar 8, 2007
Est. expirySep 2, 2025(expired)· nominal 20-yr term from priority
C07H 15/10A61P 3/10A61K 36/28A61P 37/00
47
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Claims

Abstract

A compound of the formula: wherein R 1 is H, alkyl, aryl, or cyclyl; R 2 is pyranose; R 3 is H or alkyl; m is 2, 3, 4, 5, or 6; n is 0, 1, 2, or 3; o is 0, 1, 2, 3, 4; and p is 1, 2, 3, or 4. Also disclosed is use of the compound to inhibit Th1 differentiation, promote Th2 differentiation, and treat certain disorders.

Claims

exact text as granted — not AI-modified
1 . An extract prepared by a method comprising: 
 stirring a pulverized  Bidens pilosa  plant in water to form a suspension,    collecting an aqueous solution from the suspension, and    extracting the aqueous solution with butanol to provide an extract.    
   
   
       2 . The extract of  claim 1 , wherein the pulverized  Bidens pilosa  plant is stirred in boiling water.  
   
   
       3 . A method of inhibiting Th1 cell differentiation, comprising administering to a subject in need thereof an effective amount of the extract of  claim 1 .  
   
   
       4 . A method of inhibiting Th1 cell differentiation, comprising administering to a subject in need thereof an effective amount of the extract of  claim 2 .  
   
   
       5 . A method of promoting Th2 cell differentiation, comprising administering to a subject in need thereof an effective amount of the extract of  claim 1 .  
   
   
       6 . A method of promoting Th2 cell differentiation, comprising administering to a subject in need thereof an effective amount of the extract of  claim 2 .  
   
   
       7 . A method of inhibiting Th1 cell differentiation and promoting Th2 cell differentiation, comprising administering to a subject in need thereof an effective amount of the extract of  claim 1 .  
   
   
       8 . A method of inhibiting Th1 cell differentiation and promoting Th2 cell differentiation, comprising administering to a subject in need thereof an effective amount of the extract of  claim 2 .  
   
   
       9 . A compound of the following formula:  
     
       
         
         
             
             
         
       
       wherein R 1  is H, alkyl, aryl, or cyclyl; R 2  is pyranose; R 3  is H or alkyl; m is 2, 3, or 4; n is 0; o is 0, 1, 2, 3, 4; and p is 1, 2, 3, or 4.  
     
   
   
       10 . The compound of  claim 9 , wherein R 1  is methyl, R 2  is β-glucopyranose, R 3  is H, m is 4, o is 2, and p is 1.  
   
   
       11 . A method of inhibiting Th1 cell differentiation, comprising administering to a subject in need thereof a compound of the following formula:  
     
       
         
         
             
             
         
       
       wherein R 1  is H, alkyl, aryl, or cyclyl; R 2  is pyranose; R 3  is H or alkyl; m is 2, 3, 4, 5, or 6; n is 0, 1, 2, or 3; o is 0, 1, 2, 3, 4; and p is 1, 2, 3, or 4.  
     
   
   
       12 . The method of  claim 11 , wherein R 1  is methyl, R 2  is β-glucopyranose, and R 3  is H.  
   
   
       13 . The method of  claim 12 , wherein m is 4, n is 0, o is 2, and p is 1.  
   
   
       14 . The method of  claim 12 , wherein m is 3, n is 1, o is 2, and p is 2.  
   
   
       15 . The method of  claim 12 , wherein m is 3, n is 1, o is 2, and p is 1.  
   
   
       16 . A method of promoting Th2 cell differentiation, comprising administering to a subject in need thereof a compound of the following formula:  
     
       
         
         
             
             
         
       
     
     wherein R 1  is H, alkyl, aryl, or cyclyl; R 2  is pyranose; R 3  is H or alkyl; m is 2, 3, 4, 5, or 6; n is 0, 1, 2, or 3; o is 0, 1, 2, 3, 4; and p is 1, 2, 3, or 4.  
   
   
       17 . The method of  claim 16 , wherein R 1  is methyl, R 2  is β-glucopyranose, and R 3  is H.  
   
   
       18 . The method of  claim 17 , wherein m is 4, n is 0, o is 2, and p is 1.  
   
   
       19 . The method of  claim 17 , wherein m is 3, n is 1, o is 2, and p is 2.  
   
   
       20 . The method of  claim 17 , wherein m is 3, n is 1, o is 2, and p is 1.  
   
   
       21 . A method of inhibiting Th1 cell differentiation and promoting Th2 cell differentiation, comprising administering to a subject in need thereof a compound of the following formula:  
     
       
         
         
             
             
         
       
       wherein R 1  is H, alkyl, aryl, or cyclyl; R 2  is pyranose; R 3  is H or alkyl; m is 2, 3, 4, 5, or 6; n is 0, 1, 2, or 3; o is 0, 1, 2, 3, 4; and p is 1, 2, 3, or 4.  
     
   
   
       22 . The method of  claim 21 , wherein R 1  is methyl, R 2  is β-glucopyranose, and R 3  is H.  
   
   
       23 . The method of  claim 22 , wherein m is 4, n is 0, o is 2, and p is 1.  
   
   
       24 . The method of  claim 22 , wherein m is 3, n is 1, o is 2, and p is 2.  
   
   
       25 . The method of  claim 22 , wherein m is 3, n is 1, o is 2, and p is 1.  
   
   
       26 . A method of treating a Th1-mediated disorder, comprising administering to a subject in need thereof an effective amount of the extract of  claim 1 , wherein the Th1-mediated disorder is non-obese diabetes, Crohn's colitis, autoimmune hemolytic anemia, rheumatoid arthritis, autoimmune encephalitis, multiple sclerosis, or autoimmune myocarditis.  
   
   
       27  The method of  claim 26 , wherein the Th1-mediated disorder is non-obese diabetes.  
   
   
       28 . A method of treating a Th1-mediated disorder, comprising administering to a subject in need thereof a compound of the following formula:  
     
       
         
         
             
             
         
       
       wherein R 1  is H, alkyl, aryl, or cyclyl; R 2  is pyranose; R 3  is H or alkyl; m is 2, 3, 4, 5, or 6; n is 0, 1, 2, or 3; o is 0, 1, 2, 3, 4; and p is 1, 2, 3, or 4; the Th1-mediated disorder being non-obese diabetes, Crohn's colitis, autoimmune hemolytic anemia, rheumatoid arthritis, autoimmune encephalitis, multiple sclerosis, or autoimmune myocarditis.  
     
   
   
       29 . The method of  claim 28 , wherein R 1  is methyl, R 2  is β-glucopyranose, and R 3  is H.  
   
   
       30 . The method of  claim 29 , wherein m is 4, n is 0, o is 2, and p is 1.  
   
   
       31 . The method of  claim 29 , wherein m is 3, n is 1, o is 2, and p is 2.  
   
   
       32 . The method of  claim 29 , wherein m is 3, n is 1, o is 2, and p is 1.  
   
   
       33 . The method of  claim 28 , wherein the Th1-mediated disorder is non-obese diabetes.

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