Peptide toxin formulation

Abstract

Procedures are described which use solvents to increase the topical insecticidal activity of toxic insect peptides. These procedures comprise drying the peptides, if needed, followed by the addition of either: 1) a polar organic solvent, with or without water, to a dried peptide, or 2) the addition of polar aprotic solvent or other adjuvant to the dried peptide, followed by the addition of either: 1) a polar organic solvent, with or without water, (where a polar aprotic solvent is added first) or 2) a polar aprotic solvent or other adjuvant to the peptide polar organic solvent (where the polar organic solvent is added first), to the peptide formulation.

We claim: 
     
         1 . A process for increasing the topical insecticidal activity of a peptide that is toxic to insects comprising making a topical toxic peptide formulation comprised of the following three components mixed together; 1) a peptide that is toxic to insects with 2) a polar aprotic solvent and 3) a polar organic solvent according to the following procedure:
 a) selecting a peptide that is toxic to insects and that is less than about 200 amino acids and greater than about 10 amino acids; and   b) mixing a first type of solvent with said peptide, wherein said first type of solvent is either a polar aprotic solvent or a polar organic solvent, to make a first solvent peptide mixture;   c) mixing a second type of solvent with said first solvent peptide mixture, wherein said second type of solvent is not the same type of solvent as said first type of solvent and is either a polar aprotic solvent or a polar organic solvent, to make a topical toxic peptide formulation;   
       wherein said polar aprotic solvent is selected from: dimethyl sulfoxide (DMSO)., dimethylformamide, dioxane and hexamethylphosphorotriamide and 
       wherein said polar organic solvent is selected from propanol and all its isomers, methyl ethyl ketone, diethyl ketone, acetonitrile, and ethyl acetoacetate saving said topical toxic peptide formulation. 
     
     
         2 . (canceled) 
     
     
         3 . (canceled) 
     
     
         4 . The process of  claim 1  wherein said polar aprotic solvent is selected from: dimethyl sulfoxide (DMSO) or MSO® and said polar organic solvent is propanol. 
     
     
         5 . The process of  claim 1  wherein said peptide is lyophylized before the first solvent is mixed with the peptide. 
     
     
         6 . The process of  claim 1  wherein said first solvent is a polar aprotic solvent. 
     
     
         7 . The process of  claim 1  wherein said polar aprotic solvent is from about 60% to about 99% percent, and said polar organic solvent is about 40% to about 1%, of the total solvent volume. 
     
     
         8 . The process of  claim 1  wherein said polar aprotic solvent is from about 75% to about 95%, and the polar organic solvent is about 25 to about 5%, of the total solvent volume. 
     
     
         9 . The process of  claim 1  wherein said polar aprotic solvent is from about 80% to about 90% of the total solvent volume and the polar organic solvent is from about 20% to about 10% of the total solvent volume. 
     
     
         10 . The process of  claim 1  wherein said peptide is any topical toxic peptide selected from a selected or derived from a toxic peptide from any species of spider, scorpion, snake, mite, snail, slug or plant and any peptides having 50% or greater homology to any such peptide. 
     
     
         11 . The process of  claim 1  wherein the length of said peptide is from about 20 to less than about 100 amino acids in length. 
     
     
         12 . The process of  claim 1  wherein said peptide has from 1-5, internal difulfide bonds. 
     
     
         13 . The process of  claim 1  wherein said peptide is selected from a spider or scorpion. 
     
     
         14 . The process of  claim 1  wherein said peptide is selected from the Australian funnel web spider of genus  Atrax  or  Hadronyche.    
     
     
         15 . The process of  claim 1  wherein said peptide is selected from any sequence in the sequence listing or any sequence having 50% or greater homology to any of the listed sequences. 
     
     
         16 . The process of  claim 15  wherein said peptide is selected from any of the sequences in the sequence listing. 
     
     
         17 . The process of  claim 16  wherein said peptide is selected from any of the following sequences: SEQ ID NO: 60, SEQ ID NO: 117, SEQ ID NO: 118, or SEQ ID NO: 119. 
     
     
         18 . A topical toxic peptide formulation made according to the process of  claim 1  and comprising the following:
 a) a peptide toxic to insects, as defined in  claim 1 ; 
 b) a polar organic solvent, as defined in  claim 1 ; 
 c) a polar aprotic solvent or adjuvant, as defined in  claim 1 ; 
 d) wherein said polar organic solvent comprises from about 70 to about 99 percent (%) of the final volume of the formulation; 
 e) wherein said polar aprotic solvent or adjuvant comprises from about 30, to about 1 percent (%) of the final volume of the formulation; 
 f) an optional water phase, wherein said water phase comprises from 0 (zero), to about 10 percent (%) of the final volume of the formulation. 
 
     
     
         19 . A topical toxic peptide formulation as described in,  claim 18 , wherein said topical toxic peptide is from about 20 to less than about 100 amino acids in length. 
     
     
         20 . The control of an insect with the topical toxic peptide formulation of  claim 18  wherein the topical toxic peptide formulation is applied to the insect's environment.