43 results about "Avermectines" patented technology

Provided are methods and compounds for treating (or for use in manufacturing a pharmaceutical dosage form to treat) viral infections by administering avermectin-based bioavailable highly permeable compounds. The compounds, compositions, and methods provided are particularly useful for the treatment of SARS-CoV-2, dengue, chikungunya, yellow fever, Zika and other viral infections.

Disclosed are formulations and dosage forms of avermectins, and particularly of ivermectin. The disclosed compositions may be used in methods for the treatment and prevention of pain in humans.

The invention belongs to the technical field of pesticides, and relates to an acaricidal composition and application thereof, the acaricidal composition comprises an active component A and an active component B, the active ingredient A is a compound shown in a formula (I), and the active ingredient B is abamectin. The acaricidal composition can prevent and treat various pest mites, shows a synergistic effect in a certain proportion range, and can reduce the dosage, reduce the use cost, prolong the lasting period and delay the development of the drug resistance of the pest mites.

Provided herein are compositions for the prevention and treatment of demodex blepharitis in a subject and processes of treatment or prevention of demodex blepharitis. The compositions may include at least one avermectin compound selected from 5-O-demethyl-22,23-dihydroavermectin A1a or 5-O-demethyl-25-de(1-methylpropyl)-22,23-dihydro-25-(1-methylethyl)avermectin A1a, or a combination thereof, and melatonin, wherein an aggregate concentration of the avermectin compound is optionally less than 1 wt %. Further devices are provided that include wipe including a woven or non-woven membrane and a treatment composition, the treatment composition including melatonin, one or more anti-microbial compounds, and optionally one or more pharmaceutically acceptable excipients and processes of treatment or prevention of demodex blepharitis in a subject using the wipe, alone or optionally further with the composition as provided herein.

The invention provides a root-knot nematode biocontrol peptide, the amino acid sequence of the root-knot nematode biocontrol peptide is HLVPGFTWQHIRDIP, the root-knot nematode biocontrol peptide provided by the invention is derived from bacillus megatherium, can provide a root-knot nematode prevention and control effect which is not inferior to abamectin at low concentration, and has a promoting effect on the growth of roots and leaves of tobacco. The invention also provides a recombinant expression preparation method and application of the root-knot nematode biocontrol peptide.

The present application relates to a kind of methods for deglucosylation and purification of abamectin, abamectin paste is washed with hot water 2-3 times to remove sugar, the hot water washing method is as follows: then according to the mass volume ratio of abamectin paste and hot water 1g: 1-1.5mL, hot water with temperature of 75-80 ℃ is added to abamectin paste, stir for 1h, start cooling when temperature drops to T1, stop stirring, stratify after standing, then continue to cool to T2, the upper water layer is extracted, and it is finished.The present application replaces traditional deglucosylation solvent toluene with hot water to remove sugar and impurities of abamectin, which is environmentally friendly, avoids a series of problems caused by toluene residues, and reduces the cost of deglucosylation.

The invention provides a purification method of an abamectin crystal, and relates to the technical field of biological pharmacy. The invention relates to a purification method of an abamectin crystal. The purification method comprises the following steps: S1, crystallizing an abamectin extract to obtain a crystal; s2, carrying out crystallization treatment on the crystal by using methanol with the pH value of 4.0-6.5 and the mass concentration of 80-95% to obtain a recrystallized crystal; and S3, carrying out crystallization treatment on the recrystallized crystal by using methanol with the mass concentration of 80-95% to obtain an abamectin crystal. According to the method, the content of impurities influencing clarity in the crystal can be reduced, and the clarity of the abamectin crystal is improved.

The present application relates to the field of agricultural organic chemistry, and provides an abamectin B 2a Carbamate derivatives, preparation method and application thereof, by introducing nitrogen-containing lipophilic functional groups at C4" position of abamectin B 2a Carbamate derivatives, by modifying and modifying the structure of abamectin B 2a Carbamate derivatives, by modifying and modifying the structure of abamectin B 2a Carbamate derivatives, by modifying and modifying the structure of abamectin B 2a Carbamate derivatives, by modifying and modifying the structure of abamectin B 2a Carbamate derivatives can be used for preventing and treating harmful organisms that harm ornamental plants and crops, especially organisms that harm fruits, flowers, leaves, stems, tubers or roots of plants, and also can be used for protecting growing plants from the invasion of harmful organisms.

The invention belongs to the technical field of gene detection, and particularly relates to a tetranychus urticae cytochrome P450 gene and application thereof to detection and / or monitoring of avermectin resistance of tetranychus urticae. The CYP392A13 gene shows up-regulated expression in a tetranychus urticae resistant population, and the correlation between the target gene and the avermectin resistance of the tetranychus urticae is further confirmed from the back side and the front side through RNAi and in-vitro metabolic activity tests. Therefore, the specific primer pair, the primer group, the kit and the method for detecting the abamectin resistance of the tetranychus urticae are researched and developed, if the expression quantity of a target gene in a population to be detected is obviously higher than that of a tetranychus urticae sensitive population, the population to be detected has the abamectin resistance; a key molecular tool is provided for establishing an abamectin resistance early warning system, and a drug resistance treatment strategy can be formulated in time.

The present invention belongs to the field of genetic engineering, and specifically relates to a branched-chain amino acid absorption expression system, a recombinant vector, a recombinant bacterium and its application. The branched-chain amino acid absorption expression system comprises a promoter and a gene for absorbing branched-chain amino acids; wherein the nucleotide sequence of the promoter is as shown in SEQ.ID.NO.1 or SEQ.ID.NO.2; the nucleotide sequence of the gene for absorbing branched-chain amino acids is as shown in SEQ.ID.NO.6 or SEQ.ID.NO.7. The present invention provides a branched-chain amino acid absorption expression system for increasing the yield of the polyketide compound avermectin, and constructs and prepares recombinant bacteria through genetic engineering transformation. In fermentation production, the absorption and utilization of branched-chain amino acid substrates by the strain is promoted, and the unit yield of avermectin is effectively increased.

This invention discloses a method for preparing avermectin nanoparticles supported on zein-sodium lignin sulfonate, and its applications. The preparation method involves dissolving avermectin and zein in an organic solvent to form a solution (stream 1), and dissolving sodium lignin sulfonate or modified sodium lignin sulfonate in deionized water to form a solution (stream 2). Both streams are simultaneously injected into a dual-channel confined counter-current mixer for rapid mixing. The resulting nanoparticle suspension is then collected, completing the preparation process. This invention utilizes the compatibility of hydrophobic zein with avermectin, combined with the self-assembly properties of zein and the use of sodium lignin sulfonate or modified sodium lignin sulfonate as a stabilizer, to prepare avermectin nanoparticles with high drug encapsulation efficiency and excellent drug release performance. Furthermore, these nanoparticles exhibit excellent resistance to UV photodegradation, effectively reducing the photodegradation of avermectin. The method is simple, rapid, and easy to control.

The application discloses a hapten of abamectin B1a and / or its structural analog, an artificial antigen and application thereof. The application connects a spacer to abamectin after hydrolysis to obtain a hapten of abamectin B1a and / or its structural analog, and then connects a carrier protein to prepare an artificial antigen, and further prepare a monoclonal antibody. A chemiluminescence immunoassay method is established according to specific recognition of the antibody and the antigen, and abamectin residues in a sample are detected. The method can be used for trace detection of abamectin residues, and can avoid a complicated pretreatment step. The detection limit is 0.03 ng / mL, the IC 50 (50% inhibitory concentration) is 0.1 ng / mL, and the linear range IC 20 ~IC 80 is 0.04-0.20 ng / mL.

The invention discloses an acetamido abamectin injection and a preparation method thereof, and belongs to the technical field of veterinary drug preparations. The injection comprises the following components in percentage by weight: 1%-10% of acetamido abamectin, 5%-20% of a sustained-release material, 0.1%-1% of an antioxidant, 5%-15% of a cosolvent and the balance of oil for injection. Wherein the sustained-release material is a polylactic acid-glycolic acid copolymer or polycaprolactone with a specific proportion and molecular weight, the antioxidant is selected from an efficient antioxidant such as tert-butylhydroquinone, the cosolvent is common cosolvent such as propylene glycol, and the oil for injection is soybean oil, sesame oil or corn oil and the like which meet the standard of veterinary drug poeia. The preparation method comprises the steps of oil phase preparation, medicine dissolution, mixing, antioxidant addition, filtration, filling and the like. The injection provided by the invention has the characteristics of long-acting slow release and high stability, can effectively prolong the plasma concentration duration time and reduce the administration frequency, and is simple in preparation process and suitable for large-scale industrial production.

The invention provides a separation and purification method of abamectin, and belongs to the technical field of biopesticide refining. According to the invention, high-speed counter-current chromatography (HSCCC) is adopted to separate an abamectin active compound (1%-99%), and a target product is obtained. Compared with the traditional process, the method has the advantages that the high-speed counter-current chromatography is simple to operate, short in production cycle, monitorable in process and good in repeatability, the used mobile phase can be recycled, industrial wastewater generated in the process of the traditional extraction method is greatly reduced, the later wastewater treatment cost is reduced, and the process is green, environment-friendly, non-toxic and harmless. The purity of abamectin B1a in the target product is greater than or equal to 99.5%, and the purity of obtained B1b is greater than or equal to 94.5%.

The invention discloses an abamectin fermentation culture medium and a fermentation process, and relates to the technical field of culture media. The abamectin fermentation culture medium is prepared from 15 g / L to 30 g / L of glucose, 81 g / L to 103 g / L of dextrin, 8 g / L to 12 g / L of corn steep liquor, 11 g / L to 15 g / L of soybean cake powder, 0.2 g / L to 0.5 g / L of ammonium sulfate, 0.2 g / L to 0.5 g / L of dipotassium phosphate, 0.05 g / L to 0.2 g / L of monopotassium phosphate, 0.05 g / L to 0.32 g / L of manganese sulfate, 0.3 g / L to 0.5 g / L of cobalt chloride, 0.6 g / L to 1.8 g / L of sodium chloride, 0.05 g / L to 0.25 g / L of a defoaming agent and 2.4 g / L to 5.2 g / L of silanization modified aluminum oxide. According to the technical scheme, glucose and dextrin are adopted as carbon sources, corn steep liquor, soybean cake powder and ammonium sulfate are adopted as nitrogen sources, and silanization modified aluminum oxide is added, so that the element production capacity of thalli is improved, and the titer of abamectin B1a is improved.

Palatable oral dosage formulations are provided including an effective amount of an isoxazoline parasiticidal agent, an avermectin, and a pyrazinoisoquinoline, and optionally one or more additional active ingredients, such as a tetrahydropyrimidine.

The invention discloses water dispersible granules based on emamectin benzoate and abamectin and a preparation process of the water dispersible granules, and relates to the technical field of pharmacy, and the water dispersible granules are prepared from emamectin benzoate, abamectin, modified eucalyptus oil, a wetting agent, a disintegrating agent, a binder and filler in a weight ratio of (5-20): (3-15): (5-8): (4-10): (6-12): (3-7): (40-65). And reacting the modified eucalyptus oil with maleic anhydride to obtain an esterification product, and reacting the esterification product with methoxypolyethylene glycol to obtain the modified eucalyptus oil. The water dispersible granule is good in water solubility and high in dispersion uniformity, and the stability of the product is improved.

The invention belongs to the technical field of gene detection, and particularly relates to a tetranychus urticae cytochrome P450 gene and application thereof to detection and / or monitoring of avermectin resistance of tetranychus urticae. The CYP392A13 gene shows up-regulated expression in a tetranychus urticae resistant population, and the correlation between the target gene and the avermectin resistance of the tetranychus urticae is further confirmed from the back side and the front side through RNAi and in-vitro metabolic activity tests. Therefore, the specific primer pair, the primer group, the kit and the method for detecting the abamectin resistance of the tetranychus urticae are researched and developed, if the expression quantity of a target gene in a population to be detected is obviously higher than that of a tetranychus urticae sensitive population, the population to be detected has the abamectin resistance; a key molecular tool is provided for establishing an abamectin resistance early warning system, and a drug resistance treatment strategy can be formulated in time.

Palatable oral dosage formulations are provided including an effective amount of an isoxazoline parasiticidal agent, an avermectin, and a pyrazinoisoquinoline, and optionally one or more additional active ingredients, such as a tetrahydropyrimidine.

The invention belongs to the technical field of pesticides, and particularly relates to a composition containing abamectin compounds and application of the composition, and the composition can be used in combination with necessary formula components to prepare various dosage forms of products. The composition contains an abamectin compound and a p-phenylenediamine compound, and the mass ratio of the abamectin compound to the p-phenylenediamine compound is (100: 1)-(1: 100). According to the composition, the half-life period of the abamectin compound is prolonged, and degradation of the abamectin compound is delayed; meanwhile, the composition can relieve the oxidative stress effect induced by the drug, relieve the stress effect of the abamectin compound on non-target organisms, and avoid yield reduction and crop death caused by phytotoxicity.

The present invention relates to a preparation method of avermectin. The method comprises the following steps: using avermectin B1 as a raw material, preparing an avermectin crude product through protection reaction, oxidation reaction, imidization reaction, reduction and deprotection reaction, and acylation reaction; then subjecting the avermectin crude product to crystallization treatment by a nitric acid crystallization method, and drying the product to obtain an avermectin finished product; wherein the nitric acid crystallization method comprises the following steps: dissolving the avermectin crude product in ethyl acetate, adding pure water and 10% nitric acid solution at room temperature, adjusting the solution pH to 5-6, then standing and stratifying, discarding the ethyl acetate layer, adding an alkaline solution with a weight concentration of 20% to the aqueous layer, adjusting the pH to 7-8 for crystallization, then filtering, and washing the wet crystals with pure water. The method greatly improves product yield, product purity, and reduces the impurity content and solvent residue of the product, so that the product can not only meet the national standards of my country, but also meet the standards of the USP of the United States.

The invention belongs to the technical field of molecular detection, and particularly relates to a GluCl2 subunit mutation site-based detection reagent for drug resistance of spider mites to abamectin and a PCR-RFLP (polymerase chain reaction-restriction fragment length polymorphism) detection method. The GluCl gene sequence in a tetranychus urticae population collected from a field is analyzed to find that a new mutation site T76S exists on a GluCl2 subunit, the mutation exists in a field population with multiple abamectin resistance, and the mutation frequency of the site is increased after abamectin treatment. In the process of identifying the mutation site, the mutation site is identified; according to the present invention, the specific recognition site (T 'CAG) of the DdeI restriction enzyme in the sequence is identified, such that the amplification primer is designed, the PCR-RFLP method for T76S mutation site detection is established, and the method has characteristics of rapid enzyme digestion reaction, simple operation, pollution resistance, short time, accurate experiment result, and easy determination.

According to the fermentation culture medium and the optimization method thereof, amino acid chelated cobalt with a proper concentration is added into a streptomyces avermitilis fermentation culture medium, so that trace elements are supplemented, and meanwhile, the fermentation culture medium has the dual functions of an amino acid enhancer, so that the titer of the abamectin is remarkably improved, and the yield of the abamectin is improved. And the method has a very good industrial application prospect.

This application relates to the field of pesticide production technology, specifically disclosing a fermentation production process for avermectin and avermectin itself. The avermectin fermentation production process involves inoculating *Streptomyces avermectin* into a culture medium for fermentation. The fermentation process is divided into five stages: 0-20 hours for the adaptation period, 21-80 hours for the growth period, 81-250 hours for the stationary period, and 251-300 hours for the aging period. The aeration rate during the adaptation period is 2000-2500 L / h, during the growth period it is 3000-3200 L / h, during the stationary period it is 2200-2500 L / h, and during the aging period it is 1900-2100 L / h. This avermectin fermentation process can achieve an avermectin yield of 6.89-7.11 g / L, effectively increasing avermectin production. Furthermore, the flexible adjustment of the aeration rate can effectively reduce gas waste, conserve resources, and improve overall economic efficiency.

Disclosed are formulations and dosage forms of avermectins, and particularly of ivermectin. The disclosed compositions may be used in methods for the treatment and prevention of various neurological disorders in humans.

The invention discloses an avermectin quick-release and sustained-release dual-effect solid pesticide and a preparation method thereof. The composition is as follows: avermectin active ingredient 1%-20%, surfactant 1%-30%, sustained-release carrier 0.5%-10%, quick-release carrier 40%-90%. The quick-release and sustained-release dual-effect solid pesticide of the present invention can not only combine systems with different release characteristics in one-step preparation to play a synergistic role, but also integrates the micron and nano dual-size characteristics, giving the system richer properties, and its solid preparation form can also significantly improve the preparation stability and storage and transportation convenience and safety, overcome the problems of agglomeration, flocculation, sedimentation caused by the interaction of electrostatic attraction and van der Waals forces during the water dispersion process, and maintain its ideal application effect.

The application discloses a solid culture medium for fermenting avermectin by using agricultural wastes and an application thereof, and belongs to the technical field of microbial fermentation. In order to solve problems of large water resource and organic reagent consumption, high energy consumption, high cost, environmental unfriendliness and the like in the production of avermectin by using liquid fermentation, and to solve the problem of low utilization rate of agricultural wastes, the optimal agricultural wastes are screened as the solid fermentation culture medium of Streptomyces avermitilis, and the green solid fermentation strategy of Streptomyces avermitilis is developed by optimizing the solid fermentation culture medium of Streptomyces avermitilis and fermentation process parameters, so as to reduce the fermentation cost, reduce the waste of equipment energy consumption, water resource and the generation of waste water and waste residue, and to realize the application of avermectin at a lower cost and in a green and environmental-friendly manner.

The application relates to the technical field of pesticide production, and particularly discloses a preparation method of an avermectin B1a / B2a metabolite. The method uses hydroxyl-protected avermectin B1a / B2a as a starting material, adopts a catalytic system of a copper salt or a manganese salt transition metal salt and pyridine, completes a selective oxidation reaction of a mother nucleus 8a position under the condition of oxygen pressurization at room temperature, and then removes a hydroxyl protective group to obtain a target 8a position carbonyl metabolite. The application uses clean and easily obtained oxygen as an oxygen source, replaces a high amount of chromium heavy metal oxidant in a traditional process, significantly reduces the amount of a catalyst, has mild reaction conditions, has excellent reaction region selectivity, is stable in product yield and purity, is simple in process operation and easy to industrialize, can provide a reliable material preparation path for pesticide residue standard preparation, environmental risk assessment and new pesticide lead compound screening, and has good industrial application prospect.

A compound represented by general formula (I) (wherein n represents an integer of 0-2) or a pharmaceutically acceptable salt thereof; x represents CH, CF, CCl, N, CHCH = N, CHCH = CH or CHCH = CF; y represents O, NH or a single bond; z represents a hydroxyl group or an oxo group; r1 represents a hydrogen atom, a C1-C6 alkyl group, a 3-to 6-membered cycloalkyl group, a 4-to 8-membered heterocycloalkyl group, a 6-to 10-membered aryl group, a 5-to 10-membered heteroaryl group, a C2-C6 alkenyl group, a C2-C6 alkynyl group, a group represented by-CO-R2, a group represented by-COO-R2, a group represented by-CONH-R2, or a group represented by-B (OR4) OR5, and these groups may be substituted; r2, R4, and R5 each represent a hydrogen atom, an alkyl group, or the like. # imgabs0 #

The present invention relates to the technical field of rodent pest control. Disclosed are the use of avermectin and a rodenticide formulation. The avermectin has a structure represented by formula (I). The present invention uses a strategy of "new use for old drugs", uses commercially available pesticides as candidate compounds, and uses mouse thrombin as a target to single out pesticide avermectin strongly bound to thrombin, which can activate the activity of mouse thrombin and promote blood coagulation. The present invention has the advantages of low cost, good rodenticidal killing effect, acute and chronic efficacy, good palatability, easy degradation, and the like.