Occidiofungin, a unique antifungal glycopeptide produced by a strain of burkholderia contaminans

Abstract

The present invention is directed to novel antifungal glycopeptide compounds and salts thereof produced by a strain of Burkholderia contaminans useful for preventing or treating fungal infection or disease in animals and plants and the bacterial strain that produces the compounds.

1 . An antifungal cyclic glycopeptide compound, and pharmaceutically and agriculturally acceptable salts thereof, for preventing or treating fungal infection or disease and having the following formula (I): 
       
         
           
           
               
               
           
         
       
       wherein Asn1, NAA2, Trp3, BHT4, Lys5, Gly6, Asn7, and Serb are amino acid residues. 
     
     
         2 . An antifungal cyclic glycopeptide compound, and pharmaceutically and agriculturally acceptable salts thereof, for preventing or treating fungal infection or disease and having the following formula (II): 
       
         
           
           
               
               
           
         
         wherein BHN1, NAA2, Trp3, BHT4, Lys5, Gly6, Asn7, and Ser8 are amino acid residues. 
       
     
     
         3 . The antifungal compound according to either of  claim 1  or  2 , wherein the amino acid residue NAA2 further comprises an attached acyl group and a xylose sugar. 
     
     
         4 . The antifungal compound according to  claim 3 , wherein the amino acid residue NAA2 has the structure: 
       
         
           
           
               
               
           
         
       
     
     
         5 . The antifungal compound according to  claim 3 , wherein the compound is effective against fungal plant, animal, and human pathogens. 
     
     
         6 . The antifungal compound according to  claim 3 , wherein the compound disrupts cell membrane morphology of fungal plant, animal, and human pathogens. 
     
     
         7 . A pharmaceutical composition comprising the antifungal compound according to either one of  claim 1  or  2  and at least one pharmaceutically acceptable carrier or diluent. 
     
     
         8 . The composition of  claim 7 , wherein the at least one carrier or diluent is an agriculturally acceptable carrier or diluent. 
     
     
         9 . The antifungal compound of  claim 5 , wherein the compound is derived from the fungal bacterial strain  Burkholderia contaminans.    
     
     
         10 . An isolated bacterial strain MS14 wherein the said bacterial strain belongs to the species  Burkholderia contaminans , the genetic DNA fragment thereof being sequenced and deposited into Genbank with the accession number EU938698, said strain having a genomic region responsible for an increased activity for producing at least one antifungal compound. 
     
     
         11 . The isolated bacterial strain of  claim 10 , wherein the at least one antifungal compound is the antifungal cyclic glycopeptide compound of  claim 1 . 
     
     
         12 . The isolated bacterial strain of  claim 10 , wherein the at least one antifungal compound is the antifungal cyclic glycopeptide compound of  claim 2 .