The invention describes the use of water-soluble analogues of the natural trichogine peptide GA IV as biocompatible plant protection products. This peptide belongs to the peptaibolic family, natural secondary metabolites of fungi of the genus Trichoderma, biological control agents widely used in field tests as antagonists of many phytopathogenic microorganisms. Some of these analogues have been patented against important plant pathogenic microorganisms, particularly downy mildew  that affects grapevines.

Patent Status

PENDING

Priority Number

IT102018000006817

Priority Date

29/06/2018

License

INTERNATIONAL

Market

The market for plant protection products is very broad and includes a wide range of products used to protect plants from diseases, insect infestations, and other environmental stresses.  Against phytopathogenic microorganisms there are currently in commerce no environmentally friendly alternatives to synthetic fungicides. Plant protection companies are very interested in developing new environmentally friendly and effective products in accordance with European Union Directives and Regulations.

  • TAM: $63 billion in 2023 (market for plant protection products in general, not just peptides).
  • SAM: about 1.3 billion (value of plant protection product production in Italy).
  • SOM: $1.3 mln (estimated 0.1% of TAM).

Problem

To protect grapevines, cereals, and pome fruit trees in an environmentally friendly way from important phytopathogens such as Plasmopara viticola, Botrytis cinerea, Pyricularia oryzae, Fusarium graminearum, and Penicillium expansum, there is an increasing demand for biopesticides.. It is estimated that, because of the global warming, the incidence of downy mildew  (Plasmopara viticola) may significantly increase, consequently causing a strong impact on the European wine economy, which  annually produces millions of liters of wine. In the region of Piedmont, Italy, alone, about 16 million euros are spent annually to combat this disease.  In general, the use of biopesticides, is increasingly encouraged by European Union Directives and Regulations which underline the need to use substances that guarantee “a high level of protection of human and animal health and environment, improving agricultural production.” Even copper, one of the few treatments currently used to control downy mildew , has  potential environmental consequences and is classified as a “candidate substance for substitution”.

Current Technology Limits

Among the most difficult phytopathogens to fight is Plasmopara viticola, causal agent of grapevine downy mildew  The traditionally used active ingredient for combatting this fungal pathogen is copper. This heavy metal tends to accumulate in the soil with consequent risks to the environment and particularly to aquatic and soil organisms.

As an alternative to copper, products based on peptaibolic peptides with antimicrobial activity could be used.These peptides are naturally produced by fungi of the genus Trichoderma in the form of “heterogeneous mixtures” and cause of the  poor water solubility which makes it difficult to distribute in the field. Furthermore, they are not very stable to sunlight.

Killer Application

Key applications of the technology concern the use of water-soluble analogs of the natural peptaibolic trichogin GA IV as biocompatible plant protection products against important plant pathogenic microorganisms. Specifically, peptides find application in the treatment of:

  • Grapevine, against downy mildew (Plasmopara viticola)
  • Fruit and vegetable crops, against gray mold (Botrytis cinerea)
  • Cereal crops, against the main pathogenic (Pyricularia oryzae) and mycotoxigenic (Fusarium graminearum and Aspergillus flavus) fungi.

Our Technology and Solution

The patented peptides are synthetic analogs of the natural peptaibolic trichogin GA IV, chosen because it consists of only 11 amino acids, and is therefore easy to produce. Some glycine residues were replaced with Lysines to make peptides more water-soluble, These analogs, produced by simple standard peptide synthesis are active against the important phytopathogens of fruits, vegetables, and cereal crops (Plasmopara viticola, Botrytis cinerea, Penicillium italicum, Penicillium digitatum, Penicillium expansum, Fusarium graminearum, and Pyricularia oryzae).

The use of our water-soluble analogues makes it possible to avoid the poor reproducibility associated with the use of both peptaibolics as such,  i.e., “natural extracts” produced by fungi of the genus Trichoderma, which consist of heterogeneous mixtures with poor solubility.

The synthetic peptides were initially tested in vitro against various fruit, vegetable and cereal pathogens, and proved to be particularly effective in inhibiting disease development even at low micromolar concentrations. The efficacy  of one of the peptides against downy mildew was confirmed after two years of open field grapevine trials, with a level of protection comparable to that obtained by treating with a copper-based formulation.

Advantages

  • Water soluble;
  • Biocompatible;
  • Known composition;
  • Stable under sunlight;
  • Effective against grapevine downy mildew.

Roadmap

This patent has been selected for funding within the Proof of Concept program @Unipd funded by the Italian ministry of Economics. The project developed a cost-effective and environmentally sustainable peptide synthesis protocol that made it possible to halve  production costs at €10 per gram. The current TRL corresponds to 6 since the efficacy of the peptides has already been confirmed in the open field as the result of a two-year trial. We are looking for a company to collaborate with on the scale-up phase of the developed synthesis protocol to produce peptides on a large scale, as well as to start the process of registering the product for market introduction.

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