57 results about "Gossypol Acetate" patented technology

This invention is about a medicament for gynaecological diseases therapy; specifically about a slow release agent and double-layer slow release medicament those contain gossypol acetate and other drugs. The gossypol acetate slow release medicament contains gossypol acetate, potassium chloride, vitamin B1, vitamin B6, hydropropyl methylcellulose, and other skeleton materials. While the double-layer slow release medicament is proportionally composed of gossypol acetate, potassium chloride, vitamin B1, vitamin B6, hydropropyl methylcellulose, and other skeleton materials; and its snap release layer is proportionally composed of gossypol acetate, crosslinked polyketals, and other disintegration agent.

The invention discloses a method using gossypol acetic acid to synthesize the antitumor derivative of Apogossypolone, which comprises four steps as follows: the concentrated strong alkaline solution is added in the gossypol acetic acid for reaction under a certain temperature to obtain the product of Apogossypol after removing aldehyde group; the protective agent is added in the Apogossypol according to a certain proportion for reaction under a proper temperature to obtain the product of Hexa-acetylapogossypol; the oxidant is added for oxidation of the Hexa-acetylapogossypol under a proper temperature, and the product of Tetra-acetylapogossypol is obtained after reaction; and the de-protection agent is added for de-protection of the Tetra-acetylapogossypol to obtain the product of Apogossypolone with the molecular weight being 490 and the color being brick red. The synthesizing method of the antitumor derivative of Apogossypolone by using gossypol acetic acid has the advantages that the structure of the natural drug of gossypol acetic acid is changed via the four steps of chemical reactions; and compared with the natural gossypol acetic acid, the obtained product of Apogossypolone has the characteristics of small molecular weight, better stability and higher antitumor activity.

The present invention discloses production method of a male contraceptive raw material drug, acetic gossypol, consisting of the raw material crushing, the mixing and extraction, the filtration, the concentration, the chromatography, the secondary concentration, the repeated crystallization and so on. The present invention is of the good product quality and the convenient production.

The invention discloses lyophilized emulsion preparation for injection of levo-gossypol and acetate of the levo-gossypol and a preparation method thereof. The lyophilized emulsion preparation for the injection of the levo-gossypol and the acetate of the levo-gossypol consists of levo-gossypol or levo gossypol acetate, oleic acid, glycerol, emulsifying agent, cryoprotectant, oil for injection, potential of hydrogen (pH) conditioning agent, antioxidant and water for injection. Mixture of granulesten and Span 80 serves as the emulsifying agent, mixture of trehalose and human serum albumin servesas the cryoprotectant, and the prepared lyophilized emulsion preparation is strong in salability and high in bioavailability.

The invention relates to the technical field of fertilizers, and specifically relates to a urease inhibitor composition. The composition is prepared from gossypol acetate and polyvinylpyrrolidone (PVP). According to the invention, a significant synergistic effect between PVP and gossypol acetate is found, and an appropriate compatibility proportion is found, so that good synergistic and solubilizing effects are achieved, and compared with the gossypol acetate, the obtained composition is convenient to use, powder is easier to store, the application effect is better, and the technical defects that existing urease inhibitors are uneasily dispersed in water, inconvenient to use and high in toxicity, and have residues are overcome, therefore, the urease inhibitor composition has an important practical popularization and application value, and provides powerful technical support for applying gossypol acetate as a urease inhibitor for inhibiting soil urease to coated slow release fertilizers or used with fertilizers.

The invention discloses Rhodosporidium paludigenum for degrading gossypol and application thereof, belonging to the field of microorganisms. A strain of the Rhodosporidium paludigenum HJ-D-20 is preserved in China General Microbiological Culture Collection Center on Nov. 26th, 2010 and has a culture preservation number of CGMCC No.4372. The strain has the degradation rate of 90.78% to gossypol acetate and the CP (Crude Protein) enhancement rate of 24.68%, has favorable stability, and ensures cotton seed meal to reach a use standard so as to increase the utilization rate of the cotton seed meal. The Rhodosporidium paludigenum disclosed by the invention has great importance for alleviating the shortage in protein resources, reducing soybean import and cotton seed meal export to Japan at low price, controlling the continuous increase of the price of the protein resources and reinforcing nation power.

The invention discloses levo-gossypol for treating tumors or a cyclodextrin clathrate compound of an acetate thereof, which consists of levo-gossypol or a levo-gossypol acetate, polyethylene glycol and hydroxypropyl-beta-cyclodextrin, wherein the polyethylene glycol is one of polyethylene glycol 1500 or polyethylene glycol 2000; a mass ratio of the levo-gossypol or the levo-gossypol acetate to the polyethylene glycol is 1:(0.3-1.2); the average substitution degree of the hydroxypropyl-beta-cyclodextrin is between 4.6 and 6.5; and a mass ratio of the levo-gossypol or the levo-gossypol acetate to the hydroxypropyl-beta-cyclodextrin is 1:(7.0-12.0). The levo-gossypol for treating the tumors or the cyclodextrin clathrate compound of the acetate thereof has the advantages of high bioavailability and stability, large medicine carrying amount and the like.

The invention belongs to the technical field of processing oil crops. Specifically relates to a clean production process of high-purity gossypol. It provides a simple, cheap and efficient clean production process for obtaining high-purity free gossypol, and can realize large-scale industrial preparation of free gossypol. Compared with the existing process, this process does not use acetic acid to convert gossypol to gossypol acetate, and then converts gossypol acetate to gossypol, and uses simulated moving bed chromatography continuous separation technology to directly obtain a purity of 98% Ur degree of high -purity glycol, from the source of the source, except for cotton oil soap -to -foot processing acidized oil, preparing wastewater, waste residue and acetic acid waste solvents accompanied by glycol, realizing the green cleaning of cotton oil soap foot processing, eliminating it, eliminating it It has greatly improved the quality and yield of gossypol and the co-produced cotton oil fatty acid, greatly increased the added value of cotton oil soapstock, and has broad application prospects in the field of cottonseed processing. .

The invention discloses a preparation method of gossypol acetate intravenous injection fatty emulsion. In the method, gossypol acetate is used as an active constituent, ethyl oleate or middle-chain fatty acid triglyceride is used as an oil phase, soya bean lecithin is used as a surface active agent, absolute ethyl alcohol or PEG (Polyethylene Glycol) 400 is used as a cosurfactant, and sterilized water for injection is used as a water phase. The method comprises the following steps of: (1) dissolving the gossypol acetate in diethyl ether and then mixing with the oil phase, the surface active agent and the cosurfactant; decompressing and evaporating to remove the diethyl ether and preserving at a constant temperature for later use; (2) heating the sterilized water for injection and preserving at a constant temperature for later use; (3) mixing liquids obtained in the steps (1) and (2) at a constant temperature of 60 or 70 DEG C and stirring until a transparent and homogeneous solution is formed; making the volume constant and then repeatedly homogenizing by using a homogenizer; and filtering by using a millipore filter membrane. Proved by researches, the gossypol acetate intravenous injection fatty emulsion prepared by using the method has good slow release and targeting effects and good stability.

The invention provides gossypol acetate degrading bacteria S1 capable of degrading free gossypol. The gossypol acetate degradation bacteria S1 are identified to be the Rhizopusoryzae. The Rhizopusoryzae has the main biological characteristic that the Rhizopusoryzae is black, circular, is a sporangiospore, has rhixoid and no flagellum, and can not move; the Rhizopusoryzae can grow in a potato agar culture medium and can grow in a Czapek culture medium to ferment sucrose; and the Rhizopusoryzae can grow by taking 0.3% gossypol acetate as an only carbon source. The gossypol acetate degrading bacteria S1 have the important meanings for remitting the shortage of protein resources, reducing the soybean import and the cotton seed meal low-price export to Japan, controlling the continuous rising of the protein resources price, and enhancing the national power.

The invention relates to a compound oral preparation containing gossypol acetate and other drugs. The compound oral preparation mainly contains gossypol acetate, potassium chloride, vitamin B1 and vitamin B6; and is available in the form of capsule, enteric-coated capsule, sustained-release capsule, soft capsule, oral liquid, tablet, dispersible tablet, enteric-coated tablet, sustained-release tablet or powder. The preparation has no bitter taste, high bioavailability and function for treating gynecological diseases such as essential uterine bleeding, hysteromyoma, menorrhagia and endometriosis.

The invention discloses a novel application of gossypol acetate in the field of pharmacy, and in particular relates to an application of gossypol acetate in preparing medicines for preventing, relieving and/or treating reye's syndrome, and belongs to the field of pharmacy. Reye's syndrome is a cryptogenic acute encephalopathy syndrome in the childhood phase, and studies discover that loss or mutation of MeCP2 gene has a direct causal relationship with the reye's syndrome, and loss of the MeCP2 gene can cause reye's syndrome developing on a mouse. Experiments indicate that the content of the MeCP2 gene in the brain of a rat can be remarkably increased by administrating the rat with gossypol acetate, so that the content of the MeCP2 gene in the brain of a patient can be remarkably increased by using the gossypol acetate for preventing, relieving and treating the reye's syndrome caused by MeCP2 mutation, the development of the nerve cell of the patient can be promoted, functions of the nervous system can be restored, and the possibility of healing the patient can be increased. Therefore, according to the application of the gossypol acetate in preparing the medicine for resisting reye's syndrome, the medicine can be used for preventing, relieving and/or treating the reye's syndrome.

The invention relates to the technical field of gossypol and gossypol acetate, and discloses a preparation method for the gossypol and a preparation method for the gossypol acetate. The preparation method for the gossypol comprises the following steps: extracting; separating and purifying; refining. The purity of the gossypol prepared by the preparation method for the gossypol disclosed by the invention reaches 98.0 to 99.6 percent; on the premise of meeting the requirement on the purity of a gossypol product, the cost of the reagents, such as borax and diethyl ether, used in the preparation method for the gossypol disclosed by the invention is low, and the using amounts of the reagents and the water are small, so that the extracting cost of the preparation method for the gossypol disclosed by the invention is low; meanwhile, the preparation method for the gossypol disclosed by the invention can improve the yield of the gossypol; in addition, the preparation method for the gossypol disclosed by the invention is wide in raw material application range and low in requirements on raw materials, and can treat the gossypol-containing raw materials with complex impurity compositions.

The invention discloses a method for removing plant viruses in tomato plants by gossypol acetate. Aiming at the problem that virus antagonists in current production mainly have an efficacy of inhibiting virus replication, proliferation and the like, and an effective plant virus removal method for realizing viral disease treatment is not provided yet, adopting gossypol acetate for treating the tomato plants can completely remove tomato yellow leaf curl viruses in some tomato plants and remarkably decrease the content of the tomato yellow leaf curl viruses in plants incomplete in virus removal, and positive treatment of plant viral diseases is benefited. Compared with methods for controlling bemisia tabaci amount by adoption of disease and insect resistant varieties and chemical or physical means, methods for inhibiting viruses by adoption of virus antagonists, and the like in traditional tomato yellow leaf curl virus prevention and control in production, the method for removing the plant viruses in the tomato plants by gossypol acetate has advantages that treatment of the viral diseases can be realized, unique action mode and high safety are achieved, and the method has a great application prospect.

The invention discloses a method for preparing gossypol acetate from cottonseed cake, cottonseed meal, or cotton root bark. The method comprises the following steps: (1) parching and grinding the cottonseed cake, cottonseed meal, or cotton root bark into the high-energy mill, put grinding auxiliary agent, 1 to 10 wt % of the cottonseed cake, cottonseed meal, or cotton root bark in to the high-energy mill for solid-state grinding. (2) mixing the ground power obtained from step 1 with water, and extracting and filtrating while churning and finally combining the filtrates. (3) putting the filtrate obtained from step 2 into acetic acid, churning for crystallization of the gossypol acetate crude product. (4) recrystalizing the crude product of gossypol acetate obtained through step 3, using aether 20 to 25 times of the weight of gossypol acetate, and finally the refined gossypol acetate is obtained. The invention overcomes the defects of low extraction yield, complicated technological equipments, high cost, non-recyclable menstruum in the existing organic solvent extraction method. The method of the invention is high in extraction yield, simple in process, cheap in equipment investment, moderate in operating condition, friendly to environment and high in purity.

The invention relates to a combined drug for treating tumors, in particular to a combined drug of gossypol acetate and a chemotherapeutic drug. The combined drug has a good synergistic interaction effect, and has a stronger effect of inhibiting tumors than a single drug; moreover, the combined drug has the effect of chemosensitization, and can effectively reduce the drug resistance of tumor cellsto the chemotherapeutic drug. According to the combined drug, a new and more effective treatment scheme is provided for clinical treatment of tumor diseases, and the clinical application prospect is good.

The invention provides a gossypol acetate-containing thermosensitive gel preparation. The gossypol acetate-containing thermosensitive gel preparation is characterized by comprising the following components: gossypol acetate accounting for 0.02-1 percent by mass of the gossypol acetate-containing thermosensitive gel preparation, poloxamer accounting for 16-25 percent by mass of the gossypol acetate-containing thermosensitive gel preparation, a preservative accounting for 0.05-0.3 percent by mass of the gossypol acetate-containing thermosensitive gel preparation, deionized water accounting for 72.7-83.83 percent by mass of the gossypol acetate-containing thermosensitive gel preparation and lactic acid accounting for 0.1-1.0 percent by mass of the gossypol acetate-containing thermosensitive gel preparation, wherein the PH of the gossypol acetate-containing thermosensitive gel preparation is 4.5-5.5. The gossypol acetate-containing thermosensitive gel preparation is in a liquid state at room temperature and is convenient for drug administration; after the gossypol acetate-containing thermosensitive gel preparation is administrated into a vagina, phase transformation occurs due to the temperature rise, and in-situ gelation occurs in the vagina, so that close contact between the preparation and a mucosal tissue can be achieved; and the gossypol acetate-containing thermosensitive gel preparation can penetrate into vaginal mucosal folds to be fully spread and can stay in the vagina for some time to achieve a long-lasting effect.

The invention discloses a purification technology of a crude gossypol acetate product. The purification technology comprises steps as follows: dissolving with acetone, sufficient dissolving by ultrasonic waves, filtering through filter paper, evaporation and concentration, dissolving with glacial acetic acid, re-dissolving by the ultrasonic waves, post-processing and the like. The purification technology of the crude gossypol acetate product has the advantages that crude gossypol is filtered by the filter paper under normal pressure, cotton oil is adsorbed by the filter paper, the purification effect is good, the time is short, little repetition is required, the product purity can be mastered basically according to the color of the filter paper, a finished product with the purity being 97% or higher can be obtained once, secondary dissolving is avoided, and accordingly, the production cost of the product is reduced by 30%.

The invention discloses a preparation method of gossypol acetate calcium alginate gel microspheres. Gossypol acetate is dissolved into N,N-dimethyl acetamide; epsilon-polylysine, diclofenac potassiumand potassium chloride are dissolved into water; the solution is uniformly mixed to obtain a stock solution; calcium chloride is dissolved into water; sodium alginate is dissolved into water to be prepared into a solution with the mass concentration being 1 to 2 percent; the stock solution is added into the sodium alginate solution; stirring is performed till the uniform mixing; a micro quantity injection pump is used for dripping the solution into the calcium chloride solution; gelatinization is performed for 20 to 40min to obtain microspheres. A buffer solution is used for flushing the microspheres to obtain the gossypol acetate calcium alginate gel microspheres. The gossypol acetate calcium alginate gel microspheres have the advantages of high embedding rate, good swelling property andgood medicine release property.

The invention relates to the technical field of chemical engineering, in particular to a slow release fertilizer for inhibiting soil urease activity and a preparation method. Urea, humic acid, potassium sulfate, urea phosphate, gossypol acetate and tung oil serve as raw materials and are granulated and coated to prepare the slow release fertilizer. The slow release fertilizer has the advantages of high efficiency, low cost, no toxicity and no pollution.

The invention discloses a systhesiz method of 1, 1 '-deoxygossypol . The method comprises the following steps: 1, taking gossypol acetate I as a starting material, taking gossypol acetate I as a starting material, and removing aldehyde groups to obtain apogossypol II; 2, acetylating the aspogossypol II to obtain aspogossypol III; 3, selectively removing acetyl of the aspogossypol III to obtain an intermediate IV; 4, protecting phenolic hydroxyl of the intermediate IV to obtain an intermediate V; 5, removing acetyl from the intermediate V to obtain an intermediate VI; 6, protecting phenolic hydroxyl of the intermediate VI to obtain an intermediate VII; 7, reducing the protected phenolic hydroxyl group of the VII of the intermediate to obtain a 1, 1'- deoxygossypol precursor VIII; and 8, removing a methoxy group of the 1, 1'- deoxygossypol precursor VIII to obtain a target product 1, 1 '-deoxygossypol . Reaction raw materials are cheap and easy to obtain, synthesis process steps are fewer, the total yield is as high as 45%, reaction conditions are mild, and safety is high. The method is simple in technological process and post-treatment, easy to operate and good in industrial prospect.

The invention discloses a method for preparing gossypol acetate based on solid phase synthesis, belonging to the field of chemistry. The method comprises the following steps: by taking cotton seed power as a raw material, performing solvent extraction, and resin bonding and adsorption, analyzing acetic acid, filtering, concentrating, and washing to obtain high-concentration gossypol acetate. The gossypol acetate is prepared by adopting a solid phase synthesis technology, the raw materials do not need to be degreased, and the purity of the gossypol acetate can achieve 100%. According to the method, the preparation technology of the gossypol acetate is shortened, the usage amount of the solvent is reduced on a large scale, the use of aniline can be avoided, and the residual toxicity problems of aniline on the surface of the gossypol acetate can be overcome.

The embodiment of the invention discloses an LRPPRC negative regulating agent and application thereof. According to the implementation manner of the LRPPRC negative regulating agent, compared with theprior art, high-expression LRPPRC in tumor cells is taken as a therapeutic target, gossypol acetate is taken as a targeted therapeutic drug, and through specific binding of the therapeutic target andthe targeted therapeutic drug, the aim of inhibiting growth of the tumor cells can be achieved; meanwhile, the gossypol acetate is a clinically applicable compound, so that the LRPPRC negative regulating agent is high in safety, simple in mode of administration, wide in raw material resource, low in price and capable of reducing the treatment costs for the patient.

The invention provides gossypol acetate degrading bacteria S3 capable of degrading free gossypol. The gossypol acetate degrading bacteria S3 are identified to be the Candidaoleophila. The Candidaoleophila has the main biological characteristic that the Candidaoleophila is olive candida, white, circular, propagated in a budding way, white pseudohypha, and regularity in edge; the Candidaoleophila can grow in a potato agar culture medium and can grow in a Czapek culture medium to ferment sucrose; and the Candidaoleophila can grow by taking 0.3% gossypol acetate as an only carbon source. The degrading ratio of the predominant bacteria S3 to gossypol is 60.44%, and the CP (cellulose propionate) improving ratio is 26.02%. Furthermore, a bacterial strain is very good in stability, so that cotton seed meal achieves the use standard, and the use ratio of the cotton seed meal is enhanced. The gossypol acetate degrading bacteria S3 have the important meanings for remitting the shortage of protein resources, reducing the soybean import and the cotton seed meal low-price export to Japan, controlling the continuous rising of the protein resources price, and enhancing the national power.

The invention discloses a novel gossypol Schiff base derivative with antineoplastic activity and a synthetic method thereof. The compound uses Rhodamine 123 and gossypol acetate as starting materialsto react in a non-polar organic solvent, a crude product is obtained after the reaction ends, and Schiff base compound A and compound B are obtained through recrystallization and silica gel column chromatography isolation. The method is few in reaction steps, mild in reaction condition and high in raw material utilization rate, and is applicable for industrial production.

The invention discloses bacillus subtilis capable of efficiently degrading gossypol and application thereof, the bacillus subtilis is classified and named as bacillus subtilis and is preserved in China General Microbiological Culture Collection Center on November 4, 2020, the preservation number is CGMCC No.21103, and the preservation address is Beijing in China. The bacillus subtilis is a microbial strain allowed to be used in the catalog of varieties of feed additives (2013) and can grow by taking gossypol acetate as a sole carbon source, the gossypol degradation rate by liquid fermentation is as high as 94%, the gossypol degradation rate of cottonseed meal by single-bacterium solid-state fermentation is 90.7%, by the combined fermentation of the bacillus subtilis, yeast and lactic acid bacteria with the gossypol degradation as the main function, the degradation rate of the cottonseed meal is higher than 90%, and the crude protein content, the acid-soluble protein content and the total acid content are further increased, so that the bacillus subtilis can be effectively applied to livestock and poultry feeds, particularly to broiler feed, the palatability and the digestibility of the feeds are improved, the broiler production performance is improved, and the death and culling rate is reduced.