A compound composition of psoralen and matrine, a bactericide and application thereof

Abstract

The application provides a compound composition of psoralen and matrine, a fungicide and application; the mass ratio of psoralen to matrine is (4-1):(1-4). The compound of psoralen and natural product matrine can not only prevent and treat rice blast, but also can be used for preventing and treating rice sheath blight. The binary compound fungicide has remarkable synergistic effect on preventing and treating rice blast and rice sheath blight. The effective components of the compound fungicide are all plant source natural products, and the compound fungicide has the characteristics of safety to non-target organisms and environmental friendliness, and therefore, the compound fungicide has wide application prospect as a new generation of plant source fungicide in green pest control.

Description

Technical Field

[0001] This invention belongs to the field of agricultural fungicides, specifically relating to a compound composition of psoralen and matrine, a fungicide and its application. The combination of these two substances is used to prevent and control rice blast and rice sheath blight, which is a new use and application technology invention of fungicides. Background Technology

[0002] Rice is a vital global food crop. However, rice sheath blight and rice blast cause enormous economic losses to rice production every year, representing two of the three major fungal diseases affecting rice. Currently, chemical control remains a crucial method for rice disease management. However, due to the long-term and repeated use of chemical pesticides, pathogen resistance and pesticide residues are becoming increasingly prominent issues. With growing public concern for green food and environmental safety, there is an urgent need to develop new environmentally friendly green pesticides for crop pest and disease control. Applying natural product pesticides, especially plant-derived pesticides, is one of the important approaches to green pest control at present. Compared with traditional chemical pesticides, plant-derived pesticides have advantages such as good environmental compatibility, diverse biological activities, safety for higher animals and natural enemies of pests, less likelihood of pests developing resistance, and milder efficacy.

[0003] Psoralea corylifolia L., also known as Po Gu Zhi, Po Gu Zhi, and Hu Jiu Zi, is an annual erect herb native to the Jinsha River Valley in Yunnan (Xishuangbanna) and Sichuan. Its fruit is used medicinally; it is pungent, bitter, and very warm in nature, entering the kidney meridian, and has the effects of warming and tonifying kidney yang, and strengthening the spleen and stomach. Extraction and analysis have revealed that the main chemical components of Psoralea corylifolia include coumarins, terpenoids, and flavonoids. Extensive research has been conducted on the efficacy of Psoralea corylifolia, discovering its pharmacological activities such as anti-tumor and anti-osteoporosis activity. One of the main components of Psoralea corylifolia, psoralen (PSO), belongs to the coumarin class of compounds and, in addition to its anti-tumor and anti-osteoporosis effects, also possesses estrogen-like effects such as antioxidant and cardiovascular protection. Currently, the main active ingredient in psoralen, benzoyl propionate, has been registered for the control of tea blast disease, rice blast, and apple rot.

[0004] Matrine is an alkaloid extracted from the dried roots, plants, and fruits of the legume *Sophora flavescens* using organic solvents such as ethanol. Numerous bioactivity tests have demonstrated that matrine exhibits good inhibitory activity against various pathogens. Currently, matrine fungicides on the market are mainly used to control gray mold, soft rot, powdery mildew, downy mildew, and anthracnose. Matrine is widely used in the control of pests and diseases in fruits, vegetables, and tea crops, and there are many reports on its mixed use in production. For example, matrine and azadirachtin are registered for the control of tea green leafhoppers; matrine and nicotine are registered for the control of fall webworms; and matrine and pyrethrum are registered for the control of aphids on cruciferous vegetables. However, there are currently no reports on the use of matrine and psoralen in agricultural pest and disease control. Summary of the Invention

[0005] The purpose of this invention is to provide a binary compound of psoralen and the natural product matrine, which can be used simultaneously for the prevention and control of rice blast and sheath blight.

[0006] The specific technical solution is as follows:

[0007] A compound composition of psoralen and matrine, wherein the mass ratio of psoralen to matrine is (4-1):(1-4).

[0008] Optionally, the ratio of psoralen to matrine by mass is (2-1):(1-2).

[0009] The psoralen and matrine compound composition described in this invention is used in the preparation of plant fungicides. For example, the plant fungicide is used to control rice blast and / or rice sheath blight.

[0010] A bactericide composed of psoralen and matrine, wherein the active ingredient of the bactericide is any of the psoralen and matrine compound compositions described in this invention.

[0011] Optionally, the active ingredient may have a mass percentage content of 2% to 10%.

[0012] Optionally, the content of psoralen is 0.1% to 10%, and the content of matrine is 0.1% to 20%.

[0013] Optionally, the bactericide is a soluble liquid with a weight percentage of:

[0014] Psoralen 0.1%–10%, matrine 0.1%–20%, solvent 5%–30%, surfactant 10%–30%, antifreeze 1%–10%.

[0015] Optionally, the bactericide is a wettable powder with a weight percentage of:

[0016] Psoralen 0.1%–10%, matrine 0.1%–20%, filler or carrier 1%–30%, wetting agent 1%–20%, dispersant 1%–20%.

[0017] A drug for the prevention and control of rice blast disease, wherein the active ingredient is a compound composition of psoralen and matrine as described in any one of the present invention.

[0018] A drug for controlling rice sheath blight, the active ingredient of which is a compound composition of psoralen and matrine as described in any one of the present invention.

[0019] The advantages of this invention are:

[0020] This invention utilizes the combination of psoralen and matrine to prepare agricultural fungicides, which exhibit significant synergistic effects at specific concentrations. Detailed Implementation

[0021] The technical solution of the present invention will be described in detail below with reference to specific embodiments, as follows:

[0022] This invention discloses a compound composition of psoralen and matrine, wherein the mass ratio of psoralen to matrine is (4-1):(1-4).

[0023] Optionally, the ratio of psoralen to matrine by mass is (2-1):(1-2).

[0024] The psoralen and matrine compound composition of the present invention is used in the preparation of plant fungicides. For example, plant fungicides are used to control rice blast and / or rice sheath blight.

[0025] A bactericide composed of psoralen and matrine, wherein the active ingredient of the bactericide is any one of the psoralen and matrine combinations of the present invention.

[0026] Optionally, the active ingredient may have a mass percentage content of 2% to 10%.

[0027] The bactericide is a soluble liquid with the following weight percentage:

[0028] The ingredients include: psoralen 0.1%–10%, matrine 0.1%–20%, solvent 5%–30%, surfactant 10%–30%, and antifreeze 1%–10%. The solvent is one or a mixture of two or more of methanol, ethanol, dimethylformamide, or cyclohexanone. The antifreeze is one or a mixture of two or more of ethylene glycol, propylene glycol, glycerin, or urea. The surfactant is a nonionic surfactant with a hydrophilic-lipophilic balance of 12–18, and one or a mixture of two or more of alkyl polyoxyethylene ether, fatty acid polyoxyethylene ester, phenethylphenol polyoxyethylene ether, long-chain fatty alcohol polyoxyethylene ether, polyoxyethylene alkylolamide, OP-10, Well201, No. 500, 602, Well205, and M30.

[0029] The fungicide is a wettable powder, with the following weight percentage:

[0030] The composition includes: psoralen 0.1%–10%, matrine 0.1%–20%, filler or carrier 1%–30%, wetting agent 1%–20%, and dispersant 1%–20%. The filler or carrier is one or a mixture of two or more of kaolin, diatomaceous earth, attapulgite, bentonite, or silica. The wetting agent is one or a mixture of two or more of sodium dodecyl sulfate, separating powder, and octylphenol polyoxyethylene ether. The dispersant is one or a mixture of two or more of lignin sulfonate, alkylnaphthalene sulfonate condensate, polycarboxylate, polyoxyethylene polyoxypropylene ether block copolymer, carboxymethyl cellulose, and polyvinyl alcohol.

[0031] Example 1: In vitro determination of the toxicity of psoralen and matrine.

[0032] The virulence of psoralen and matrine against the pathogens was determined using the mycelial growth rate method. Psoralen stock solution was dissolved in methanol to concentrations of 50,000, 25,000, 12,500, 6,250, and 3,125 μg / ml; matrine was dissolved in methanol to concentrations of 100,000, 50,000, 25,000, 12,500, and 6,250 μg / ml. 0.2 mL of each stock solution was pipetted into 100 mL of PDA medium to prepare media containing psoralen at final concentrations of 100, 50, 25, 12.5, and 6.25 μg / ml; and media containing matrine at final concentrations of 200, 100, 50, 25, 12.5, and 6.25 μg / ml. Select a 0.5 cm diameter colony disc of pathogenic bacteria and place it in the center of a petri dish (mycelial side down). Use 0.2 mL of methanol as a control. Incubate the petri dishes at 25°C. Then, measure the colony diameter using the cross-hatching method. Using the blank control as a standard, calculate the inhibition rate according to the following formula. Calculate the effective inhibitory concentration (EC50) using DPS software. 50The rice blast fungus and rice sheath blight fungus strains used in this experiment were all preserved in our laboratory. They were isolated from diseased plant debris using standard strain isolation methods and identified using standard strain identification methods. The specific pathogen numbers are for strains obtained by different individuals at different times and have no special meaning.

[0033]

[0034] Table 1. Indoor toxicity determination of psoralen and matrine against rice sheath blight pathogen.

[0035]

[0036] As shown in Table 1, the effective inhibitory concentrations of psoralen and matrine against rice sheath blight were 45.8063 and 99.1135 μg / ml, respectively, indicating that psoralen and matrine have good inhibitory effects on rice sheath blight.

[0037] Table 2. Indoor toxicity determination of psoralen and matrine against rice blast fungus.

[0038]

[0039] Table 2 shows that the effective inhibitory concentrations of psoralen and matrine against rice blast fungus were 30.5221 and 67.5142 μg / ml, respectively. This indicates that psoralen and matrine have strong toxicity against rice blast fungus.

[0040] Example 2: Synergistic effect of different ratios of psoralen and matrine

[0041] The virulence of psoralen and matrine against the pathogen was determined using the reference mycelial growth rate method at different ratios. Mycelial cakes were transferred to PDA plates containing a series of compound reagents and incubated at 25°C for 2 days. When the colony diameter in the blank control group exceeded 2 / 3 of the entire petri dish diameter, the diameter of all colonies was measured. Each treatment was repeated three times, and the mycelial growth inhibition rate and the effective inhibitory concentration (EC50) were calculated. 50 The synergistic coefficient of the mixed drug is calculated according to the following formula. When the synergistic coefficient is greater than 1.5, it is a synergistic effect; between 0.5 and 1.5, it is an additive effect; and less than 0.5, it is an antagonistic effect (a and b are the proportions of psoralen and matrine in the compound, EC). 50 (A) and EC 50 (B) is the effective medium concentration of psoralen and matrine, EC 50 (Exp) is the concentration at which the theoretical inhibition occurs, EC 50 (Obs) represents the actual measured concentration of inhibition.

[0042]

[0043] Table 3. Virulence determination of different ratios of psoralen and matrine against rice sheath blight pathogen.

[0044]

[0045] Table 3 shows that the toxicity of psoralen and matrine against rice sheath blight varies with different ratios, with synergistic coefficients ranging from 0.5700 to 2.1500. The synergistic coefficients of the above ratios are all greater than 0.5, indicating that they all exhibit an additive effect. In particular, when the mass ratio of psoralen to matrine is 1:4 to 4:1, the synergistic coefficients are all greater than 1.5, indicating that psoralen and matrine have a significant synergistic effect against rice sheath blight under the above ratios.

[0046] Table 4. Virulence determination of different ratios of psoralen and matrine against rice blast fungus.

[0047]

[0048]

[0049] Table 4 shows that when the ratio of psoralen to matrine is 1:10 to 10:1, the synergistic effect coefficient is between 0.5400 and 2.1547, all greater than 0.5, indicating that they have an additive effect at the above ratios. In particular, when the ratio is 1:4 to 4:1, the synergistic effect coefficient is greater than 1.5, indicating that when the ratio is 1:4 to 4:1, the combined action of psoralen and matrine has a significant synergistic effect in controlling rice sheath blight.

[0050] Example 3: Production of 2% Sophora flavescens·Psoralen Soluble A

[0051] Accurately weigh 100 kg of 10% psoralen raw material and 100 kg of 10% matrine raw material. Incubate the two active ingredient solutions at 2M... 3 Mix thoroughly in the mixing tank. Accurately measure 400 kg of ethanol and add it to the mixing tank, then mix thoroughly again. Next, accurately add 250 kg of emulsifier Well201 and 150 kg of urea to the mixing tank, and mix thoroughly. Continue stirring for 1 hour. A soluble product of 1 ton of psoralen and matrine composition is prepared.

[0052] Sampling analysis revealed that the content of psoralen was 1%, and the content of matrine was 1%. The product was packaged into 100 aluminum cans, each coated with a barrier material. The cans were sealed and labeled to identify the product as 2% soluble liquid product A.

[0053] Example 4: Production of 10% Sophora flavescens·Psoralen wettable powder B

[0054] Accurately weigh 400 kg of 20% matrine raw material and 200 kg of 10% psoralen raw material. Add 150 kg of kaolin as a carrier, 150 kg of sodium dodecyl sulfate as a wetting agent, and 100 kg of polyvinyl alcohol as a dispersant. Coarsely pulverize and finely pulverize the above materials separately, then continue mixing with a mixer for 1 hour until homogeneous.

[0055] The sampled product was tested and found to contain 8% matrine and 2% psoralen, resulting in 1 ton of wettable powder product B with a total effective component content of 10%.

[0056] Example 5: The efficacy of psoralen and matrine compound in controlling rice blast and rice sheath blight.

[0057] The efficacy of the compound pesticide against rice blast and rice sheath blight was demonstrated in Hanzhong, Shaanxi Province. Rice blast control was achieved with two applications: once at the late booting stage (heading stage) and once at the heading stage. Rice sheath blight control was achieved with two applications: once at the peak tillering stage and once at the late tillering stage. The experimental setup included treatments of the aforementioned soluble concentrate A and wettable powder B. Jinggangmycin (28% SP) served as the control for rice sheath blight; methamidophos (40% WP) served as the control for rice blast. Each treatment was replicated in three plots, each 50m². 2 .

[0058] Table 5. Field control efficacy of psoralen and matrine compound against rice sheath blight.

[0059]

[0060] Note: According to Fisher's minimum significance test, different letters after the values ​​in the same column indicate that there is a significant difference between the values ​​(P = 0.05).

[0061] As shown in Table 5, field efficacy trials indicate that both soluble agent A and wettable powder B have good control effects on rice sheath blight, with control efficacy exceeding 75%, comparable to the control agent jinggangmycin.

[0062] Table 6. Field control efficacy of psoralen and matrine compound against rice blast.

[0063]

[0064] Note: According to Fisher's minimum significance test, different letters after the values ​​in the same column indicate that there is a significant difference between the values ​​(P = 0.05).

[0065] As shown in Table 6, field efficacy trials indicate that both soluble agent A and wettable powder B have good control effects against rice blast, with control efficacy exceeding 75%, which is comparable to that of the control agent, isoprothiolane.

[0066] Although the present invention has been described in detail above with general descriptions and specific embodiments, modifications or improvements can be made to it, which will be obvious to those skilled in the art. Therefore, all such modifications or improvements made without departing from the spirit of the present invention fall within the scope of protection claimed by the present invention.

Claims

1. A compound composition of psoralen and matrine, characterized in that, The mass ratio of psoralen to matrine is (4-1):(1-4).

2. The compound composition of psoralen and matrine according to claim 1, characterized in that, The ratio of psoralen to matrine by mass is (2-1):(1-2).

3. The application of the compound composition of psoralen and matrine as described in claim 1 or 2 in the preparation of plant fungicides.

4. A bactericide composed of psoralen and matrine, characterized in that, The active ingredient of the bactericide is a compound composition of psoralen and matrine as described in any one of claims 1-2.

5. The bactericide compounded with psoralen and matrine according to claim 4, characterized in that, The mass percentage of the active ingredient is 2% to 10%.

6. The bactericide compounded with psoralen and matrine according to claim 4, characterized in that, The psoralen content is 0.1% to 10%, and the matrine content is 0.1% to 20%.

7. The bactericide compounded with psoralen and matrine according to claim 4, characterized in that, The bactericide is a soluble liquid with a weight percentage of: Psoralen 0.1%–10%, matrine 0.1%–20%, solvent 5%–30%, surfactant 10%–30%, antifreeze 1%–10%.

8. The bactericide compounded with psoralen and matrine according to claim 4, characterized in that, The bactericide is a wettable powder with the following weight percentage: Psoralen 0.1%–10%, matrine 0.1%–20%, filler or carrier 1%–30%, wetting agent 1%–20%, dispersant 1%–20%.

9. A drug for controlling rice blast disease, characterized in that, The active ingredient is a compound composition of psoralen and matrine as described in any one of claims 1-2.

10. A drug for controlling rice sheath blight, characterized in that, The active ingredient is a compound composition of psoralen and matrine as described in any one of claims 1-2.

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