Application of echinocandin antifungal drug in prevention and treatment of agricultural diseases

Abstract

The invention is suitable for the technical field of agricultural bactericides, and provides application of an echinocandin antifungal drug in prevention and treatment of agricultural diseases. According to the present invention, the two common echinocandin antifungal drugs such as the anidulafungin and the Rezafungin acetate, which are common in the field of medicine, are firstly applied to prevention and control of crop diseases; prevention and control tests are carried out on crop fungal diseases such as sclerotiniose, corn southern leaf blight, tomato gray mold, rice blast and crop anthracnose, and results show that the two drugs can significantly inhibit the growth of pathogenic fungal hyphae, and compared with an existing agricultural commercial bactericide carbendazim, the bactericidal composition shows higher inhibitory activity and has the characteristics of high efficiency and low toxicity. The invention lays a foundation for deep research and application of echinocandin drugs in the agricultural field, has a wide market prospect, effectively improves the crop disease prevention and control level, and promotes grain yield increase and quality safety.

Description

Technical Field

[0001] The present invention belongs to the technical field of agricultural fungicides, and particularly relates to the use of echinocandin antifungal drugs in the prevention and control of agricultural diseases. Background Art

[0002] Plant diseases are important factors threatening the healthy development of agriculture and food security, causing huge yield losses every year. For example, sclerotinia rot caused by Sclerotinia sclerotiorum occurs widely on various crops and is prone to cause withering and lodging; southern leaf blight of maize caused by Bipolaris maydis can occur throughout the growth period of maize, affecting the photosynthesis of plants; Botrytis cinerea infects tomato fruits and leaves, causing gray mold and resulting in significant yield reduction; rice blast caused by Magnaporthe grisea not only seriously affects the yield and quality of rice, but also increases the economic burden on farmers; anthracnose caused by Colletotrichum graminicola appears on various cash crops, easily leading to lesions or even rot on fruits, stems, leaves and other parts.

[0003] In recent years, chemical fungicides have played an important role in the prevention and control of crop diseases. However, long-term use has led to an increase in pathogen resistance, and at the same time, the environmental safety and human and animal health problems caused are becoming increasingly prominent. In the face of the continuous evolution of pathogens and the enhancement of resistance to existing chemical agents, the development of new pesticides with high efficiency, low toxicity and low residue has become an urgent need.

[0004] Anidulafungin and Rezafungin acetate are common echinocandin antifungal drugs in clinical practice. They mainly inhibit the biosynthesis of (1,3)-β-D-glucan in the fungal cell wall and have good inhibitory effects on a variety of pathogenic fungi. Anidulafungin is an efficient antifungal drug in medicine, especially having the best effect on Candida pathogens (such as Candida albicans, Candida glabrata, etc.), and also having certain activity against Aspergillus. Its treatment scope covers candidemia, invasive candidiasis and esophageal candidiasis, and is particularly suitable for critically ill or drug-resistant patients. Clinical studies have confirmed its effectiveness and safety in a variety of complex clinical scenarios, making it an important choice for the treatment of systemic fungal infections. Rezafungin acetate has good efficacy and safety in the treatment of bloodstream infections. However, up to now, there have been no relevant reports on the application of Anidulafungin and Rezafungin acetate in the field of agricultural disease prevention and control. Therefore, the present invention proposes the use of echinocandin antifungal drugs in the prevention and control of agricultural diseases. Summary of the Invention

[0005] The object of the present invention is to provide the use of echinocandin antifungal drugs in preventing and controlling agricultural diseases, aiming to solve the problems raised in the above-mentioned background art.

[0006] The object of the present invention is achieved through the following technical solutions:

[0007] The use of echinocandin antifungal drugs as fungicides in preventing and controlling agricultural diseases, wherein the echinocandin drugs are selected from one of anidulafungin and rezafungin acetate.

[0008] Further, the agricultural disease is a crop disease caused by Sclerotinia sclerotiorum.

[0009] Further, the agricultural disease is a crop disease caused by Bipolaris maydis.

[0010] Further, the agricultural disease is a crop disease caused by Botrytis cinerea.

[0011] Further, the agricultural disease is a crop disease caused by Magnaporthe oryzae.

[0012] Further, the agricultural disease is a crop disease caused by Colletotrichum spp.

[0013] Compared with the prior art, the beneficial effects of the present invention are as follows:

[0014] The present invention first applies two common echinocandin antifungal drugs in the medical field, anidulafungin and rezafungin acetate, to the prevention and control of crop diseases to expand their new uses and achieve "new uses for old drugs". Control tests were carried out on representative and severely harmful crop fungal diseases such as sclerotinia rot, southern leaf blight of maize, tomato gray mold, rice blast, and crop anthracnose. The results show that these two echinocandin antifungal drugs can significantly inhibit the mycelial growth of pathogenic fungi and exhibit stronger inhibitory activity compared with the existing agricultural commercial fungicide carbendazim, and have the characteristics of high efficiency and low toxicity. The present invention lays a foundation for the in-depth research and application of echinocandin drugs in the agricultural field, has a broad market prospect, can effectively improve the prevention and control level of crop diseases, and promote grain yield increase and quality safety. Detailed Embodiments

[0015] In order to have a clearer understanding of the technical features, objects, and beneficial effects of the present invention, the technical solutions of the present invention are described in detail below, but it should not be construed as a limitation on the implementable scope of the present invention.

[0016] The present invention provides the use of an echinocandin antifungal drug as a fungicide in preventing and controlling agricultural diseases. The echinocandin antifungal drug is selected from one of anidulafungin and rezafungin acetate (the structural formula is shown in formula I).

[0017] Formula I:

[0018] The echinocandin antifungal drug can prevent and control crop diseases caused by sclerotinia sclerotiorum, corn leaf spot caused by corn leaf blight fungus, tomato gray mold caused by Botrytis cinerea, rice blast caused by Magnaporthe grisea, and anthracnose caused by Colletotrichum graminicola.

[0019] The specific implementation of the present invention is described in detail below in conjunction with specific embodiments.

[0020] Example 1: Indoor antibacterial activity determination and results;

[0021] This example adopts the mycelium growth rate method, and the specific operation process is as follows:

[0022] According to the set concentration gradient, the test compounds (anidulafungin, rezafungin acetate) were added to the culture medium that was sterilized and cooled to about 50°C. After being fully mixed, the drugs were diluted into a series of concentrations to prepare drug-containing culture medium.

[0023] During the experimental preparation stage, each culture dish was inoculated with a pathogen block with a diameter of 5 mm, and 3 replicates were set for each concentration; carbendazim was used as a control agent to determine the inhibitory activity of the compound against the selected 5 plant pathogenic fungi.

[0024] In the subsequent culture stage, the inoculated culture dish was placed under 25°C culture conditions for cultivation. When the control colonies treated with carbendazim grew to more than 2 / 3 of the area in the culture dish, the colony diameter (mm) under each concentration treatment was determined by the cross method, and the average value was taken to represent the colony growth level, and the inhibition rate of the agent on mycelial growth was calculated. The statistical analysis of differences was performed using Graphpadprism9 software. Finally, the inhibitory effects of anidulafungin and rezafungin acetate on sclerotinia, corn leaf blight, gray mold, rice blast and anthracnose were determined, and the results are shown in Tables 1 and 2.

[0025] Table 1. Inhibitory activity of echinocandin antifungal drugs against plant pathogenic fungi

[0026]

[0027] Note: “-” indicates not measured.

[0028] Table 2. Toxicity analysis of echinocandin antifungal drugs against phytopathogenic fungi

[0029]

[0030] From the results of Table 1 and Table 2, it can be seen that the two echinocandin antifungal drugs (anidulafungin, rezafungin acetate) involved in the present invention show excellent inhibitory effects against Sclerotinia sclerotiorum, Bipolaris maydis, Botrytis cinerea, Magnaporthe oryzae and Colletotrichum spp., which are significantly higher than those of the agricultural commercial fungicide carbendazim at the same concentration. In particular, anidulafungin has the strongest antibacterial activity against Sclerotinia sclerotiorum, Botrytis cinerea and Magnaporthe oryzae, and its EC 50 values are 0.0219, 0.0689, 0.0995 μg / ml respectively, which means that only a very low drug concentration can achieve an ideal antibacterial effect.

[0031] In summary, the two echinocandin antifungal drugs involved in the present invention show significant inhibitory activity against agricultural pathogens and can open up a new application way for the prevention and control of crop diseases.

[0032] The above is only the preferred embodiment of the present invention. It should be pointed out that for those skilled in the art, without departing from the concept of the present invention, several deformations and improvements can also be made, which should also be regarded as the protection scope of the present invention, and these will not affect the implementation effect of the present invention and the practicability of the patent.

Claims

1. Use of echinocandin antifungal drugs as fungicides in preventing and controlling agricultural diseases, characterized in that: The echinocandin drug is selected from one of anidulafungin and rezafungin acetate.

2. The use of the echinocandin antifungal drug as a fungicide in preventing and controlling agricultural diseases according to claim 1, characterized in that: The agricultural disease is a crop disease caused by Sclerotinia sclerotiorum.

3. The use of the echinocandin antifungal drug as a fungicide in preventing and controlling agricultural diseases according to claim 1, characterized in that: The agricultural diseases are crop diseases caused by Bacteroides maydis.

4. The use of the echinocandin antifungal drug as a fungicide in preventing and controlling agricultural diseases according to claim 1, characterized in that: The agricultural diseases are crop diseases caused by Botrytis cinerea.

5. The use of the echinocandin antifungal drug as a fungicide in preventing and controlling agricultural diseases according to claim 1, characterized in that: The agricultural diseases are crop diseases caused by rice blast fungi.

6. The use of the echinocandin antifungal drug as a fungicide in preventing and controlling agricultural diseases according to claim 1, characterized in that: The agricultural diseases are crop diseases caused by anthrax bacteria.

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