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 Inhibition of trichothecene toxins by ancymidol

Details
Inventors: Desjardins, Anne E.;
Assignee: The United States of America, as represented by the Secretary of (Washington, DC)
Primary Examiner: Weimar; Elizabeth C.
Assistant Examiner:
Attorney, Agent or Firm: Silverstein; M. Howard, McConnell; David G., Ribando; Curtis P.

The compound ancymidol, a known potent plant growth retardant and weak fungicide, has now been found to inhibit biosynthesis of trichothecene toxins on substrates susceptible to growth of trichothecene-producing fungi. These fungi are known to contaminate cereal grains, forage crops, and potatoes. The effective level of ancymidol addition for toxin inbibition is substantially less than that required for control of fungal growth.

DETAILED DESCRIPTION OF THE INVENTION The name "ancymidol" is generic for .
alpha.
-cyclopropyl-.
alpha.
-(p-methoxyphenyl)-5-pyrimidinemethanol and identifies the compound represented by the structural formula I, below.
##STR1## Pure ancymidol is characterized as a white crystalline solid having a melting point of 110.
degree.
-111.
degree.
C.
Ancymidol is freely soluble in DMSO, acetone, methanol, chloroform, and other polar solvents; moderately soluble in aromatic hydrocarbons such as benzene; and only slightly soluble in saturated hydrocarbon solvents.
In water it is soluble at levels of approximately 650 p.
p.
m.
at 25.
degree.
C.
Ancymidol is relatively nontoxic as indicated by oral feeding studies over a 3-month period with rats and dogs.
In the studies, all test animals survived without significant changes at 8000 p.
p.
m.
of the feed, corresponding to a dose in the dogs of 20 mg.
/kg.
body weight ("Technical Report on `A-REST`," Lilly Research Laboratories).
In accordance with the objective of the invention, it is envisioned that ancymidol may be applied to any liquid or solid substrate susceptible to contamination with trichothecenes.
As secondary fungal metabolites, the toxins are associated with the senescent fungus.
All substrates susceptible to growth of the fungus are therefore targets for treatment.
Of particular interest are cereal grains, forage crops, and potatoes, especially those which are stored for extended periods.
It is sufficient to commence treatment at any time during the primary phase of fungal growth.
However, as a practical matter, it would be efficacious to treat the grain or other crop material at the time of storage.
Ancymidol may be formulated with one of the aforementioned solvents or with any suitable carrier or vehicle as known in the art.
Solutions of ancymidol in DMSO are readily miscible with water.
The compound is unstable under acidic conditions, and it is therefore important to maintain the formulation at pH 4 or greater.
The ancymidol formulation may be sprayed onto the substrate or otherwise applied by any conventional means



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