37 results about "Swainsonine" patented technology

A process for purifying swainsonic contained in loco weed includes extracting macropolar alkaloid crude product by cationic exchange, further extracting with alkaline chloroform, silica gel chromatography to obtain swainsonic crude product and finally sublimating by steps. Its advantages are low cost and high purity.

The invention discloses a method for synthesizing a swainsonine antigen, comprising the following steps of: firstly performing a reaction between halo alkyl aryl fatty acid and alcohol to generate halo alkyl aryl fatty acid ester, followed by a reaction between halo alkyl aryl fatty acid ester and swainsonine to generate a quaternary ammonium salt with a structure of aromatic nucleus, performing a reaction between the quaternary ammonium salt and sodium hydroxide for deesterification to generate a sodium salt, adjusting the pH value by the use of hydrochloric acid to generate SW-halo alkyl aryl fatty acid; condensing SW-halo alkyl aryl fatty acid with bovine serum albumin (BSA) to produce SW-BSA, sieving through a glucan gel column chromatography for desalination, freeze drying, determining the proportion of BSA and SW, and adding an immunoadjuvant for emulsification to obtain the SW immune antigen. The antigen is white and oily with the effective content being 5mg / mL and the effective immune period being 12 months. The effective protection rate reaches more than 90%.

A separation method of swainsonine-producing endophytic fungi in glabrous crazyweed comprises the following steps of: acquiring mycelium of the strain and a broth through a bio-fermentation method, carrying out ultrasonic extraction, quantitatively and qualitatively detecting swainsonine by thin-layer chromatography and gas chromatography technologies after solvent extraction, and identifying swainsonine-producing endophytic fungi through morphological and molecular biology methods. The result shows that one out of six separated strains of endophytic fungi can generate swainsonine and the output is 16.7338 mg / L. After identification, the strain is fusarium proliferatum. In comparison with present strains for the production of swainsonine, swainsonine provided by the invention has high output. The bio-fermentation method for the production of swainsonine doesn't influence the meadow ecological environment. The separation method provided by the invention solves the problem of swainsonine sources and provides strain supports, thus establishing a theoretical foundation for future industrial production of swainsonine. The invention has a wide development prospect.

The present invention belongs to the field of chemical synthesis, and relates to a preparation method of (-)-Swainsonine having anti-cancer activity. According to the present invention, the technical route has characteristics of simple operation, simple route and high yield, and the used reagents are the commonly used reagents; and the cost can be significantly reduced, the 10-100 g-scale preparation can be easily prepared in the laboratory, and the method is suitable for large-scale preparation.

A biological fermenting process for purifying swainsonine includes such steps as biological fermenting engineering with pulse rhizoctonia 7-3 strain to culture its mycelia containing high content of swainsonine, extracting in alcohol solvent, cationic exchange, silica-gel column chromatography and segmental sublimation. Its advantages are low cost, high purity (more than or equal to 99%) and high output rate.

The present invention belongs to the technical field of phyto-extraction processes, in particular to a process for purifying swainsonine from plants belonging to the oxytropis or astragalus of leguminosae. Aimed at the defects of the prior art, which include a long period of extraction, environmental pollution, high extraction cost and low purity, the technical scheme put forward by the present invention is a process for purifying swainsonine from plants belonging to the oxytropis and astragalus of leguminosae orderly includes the following steps: (1) Maximum-polarity organic component aqueous extract is obtained by ultrasonic pure water extraction; (2) Crude swainsonine extract is separated out by polar macroporous adsorption resin; (3) After step-by-step sublimations, a pure swainsonine product is produced. Compared with the prior proprietary technology, the present invention has the following advantages: (1) short extraction period; (2) environmental pollution reduction; (3) low extraction cost; (4) increased extraction rate and purity; (5) strong practicability.

The invention relates to a process for separating and extracting swainsonine from Oxytropis chinensis in Gansu. The present invention adopts the countercurrent extraction method to degrease and remove impurities with chloroform under acidic conditions, and then use n-butanol countercurrent extraction under alkaline conditions to obtain the crude total alkaloids. The obtained crude total alkaloids were separated by silica gel column chromatography to obtain crude swainsonine, and then recrystallized to obtain pure swainsonine. The purification process of the invention is completed in four steps, the extraction cost is low, the process is simple, the product purity is high, and the whole extraction process is suitable for industrialized production.

The invention belongs to the technical field of bio-pharmaceuticals, and in particular relates to a method for separating swainsonine-generating endophytic fungi. For solving the problems of low yield and loss caused by strain variation of the prior art, the invention adopts a technical proposal that the method for separating swainsonine-generating endophytic fungi comprises the following steps: 1) separation, which includes removing dust with deionized water, separating leaf, stem and flow, sterilizing surface, absorbing water, cutting, inoculating tissue blocks on the surface of a culture medium respectively, culturing the inoculated tissue blocks in a culture box, selecting edge hyphae when the hyphae grow on the periphery of the surface of the culture medium, inoculating the edge hyphae on the surface of an agar medium, and placing the inoculated edge hyphae in a culture medium for culture, inoculating a bacterial colony growing on a PDA culture medium on the surface of the cultural medium again when the bacterial colony growing on a PDA culture medium is not purification, and repeating the previous operation process till a purified bacterial strain is obtained; and 2) screening by classic thin-layer chromatography. The method has the advantages of high extraction efficiency, simplicity, and easy implementation.

The invention discloses an ELISA (enzyme-linked immuno sorbent assay) detection method of a rabbit swainsonine-resistant antibody, and a kit. The indirect ELISA method is adopted for detecting the rabbit serum swainsonine-resistant antibody, and comprises the following steps of: coating; sealing; adding to-be-detected serum and positive and negative serum; adding IgG-HRP (immunoglobulin G-Horse Radish Peroxidase); adding substrate solution; and suspending. Through the implementation of the method, the immune effect of a rabbit is judged rapidly, sensitively and accurately; and the ELISA detection method is simple and feasible, and is suitable for scientific research institutions and livestock raising systems of grass roots.

The present invention relates to one kind of plant extractive for treating cancer, and the plant extractive can suppress tumor cell and raise body's immunity obviously. The plant extractive of the present invention is swainsonine extracted from thinleaf crazyweed as one kind of leguminous plant. Swainsonine is used through cooperating with poly IC or IL-2.

The invention discloses a feed capable of accelerating growth of chicken. The feed comprises the following raw materials by weight: 50 to 56 parts of corn, 16 to 20 parts of wheat bran, 10 to 13 parts of fine rice bran, 8 to 10 parts of pomace, 5 to 6 parts of stevia rebaudiana, 2 to 3 parts of dragon's tongue leaf, 5 to 7 parts of Stachys sieboldi Miq, 2 to 3 parts of goosegrass herb, 2 to 3 parts of root of pear, 4 to 5 parts of vegetable sponge of luffa, 3 to 4 parts of plantago, 4 to 5 parts of jerusalem artichoke, 2 to 3 parts of fruit of swainsonine, 3 to 4 parts of Crownofhorns Euphoriae herb, 2 to 4 parts of corydalis tuber, 6 to 8 parts of a flavoring agent, 1 to 2 parts of garden burnet, 0.04 to 0.06 part of threonine, 0.08 to 0.1 part of methionine and 0.06 to 0.08 part of ammonium chloride. According to the invention, a traditional production method for a feed is improved; through reasonable usage of a fumigating material for fumigation, odorous smell of some traditional Chinese medicinal materials is improved, full mixing of the raw materials is better realized, a nutritive value of the feed is strengthened, taste of the feed is further improved through addition of the flavoring agent, demands for the feed by chicken are increased, and growth and development of chicken are accelerated.

The invention belongs to the fermentation engineering technical field, in particular relates to the technics of producing swainsonine fermented by beauveria. The invention provides the technics of producing the swainsonine fermented by the beauveria to overcome the problems of the hard reproduction and the high cost of the prior art. In order to overcome the problems of the prior art, the technical scheme adopted by the invention is the process of producing the swainsonine fermented by the beauveria. The process successively includes the following steps: first, mycelium is obtainedthe through biological fermentation of the beauveria; second, the extraction of the swainsonine in the mycelium: firstly, the extraction of the total extract of the mycelium: the myceilium extraction concentrated solution is obtained by a ultrasonic method; secondly, the extraction of swainsonine crude products: the swainsonine crude products can be obtained by repeated extraction; thirdly, the extraction of the pure swainsonine: the pure swainsonine is obtained by the sublimation technology.

The invention discloses Arthrobacter sp. HW08 for degrading swainsonine, which is preserved in a common microbe center of the China Microbial Culture Preservation Commission in September 28th, 2009 and has the preservation number of CGMCC No. 3313. The bacterial colony of a bacterial strain is in a circular shape and gradually changed into faint yellow from oyster white with the prolongation of culture time, has a smooth, moist and raised surface and neat edges and is non-transparent; and the bacterial strain is cultured within 48 hours in an inorganic salt culture medium, basically belongs to a stab cell, has the size of 0.3-0.5 micrometer*0.5-1.0 micrometer, is gradually changed into a ball shape after cultured for 48 hours and has the diameter about 0.60-0.8 micrometer. The bacterial strain is obtained by separating and screening from soil embedding yellowflower crazyweed herbs (loco weeds) and has the capacity of efficiently degrading the swainsonine, i.e. toxins of the loco weeds.

The invention provides an extracting process of swainsonine in astragalus strictus. The extracting process comprises the following steps of: directly crushing by using roots and / or stems of astragalus strictus as materials, adding petroleum ether to form a solution; ultrasonically degreasing the solution after 3-5 hours, and recycling petroleum ether; controlling the moisture content of the ultrasonically degreased materials to 30%-70%; using methanol with concentration of 85%-90% as a solvent, soaking for 0.5 hour-1 hour to carry out microwave extraction for 35 seconds-40 seconds at the microwave output power of 650 W-700W to obtain an extricated solution, wherein the weight volume ratio of the materials to the methanol is 1:45g / ml-50g / ml; evaporating the extracted solution for 25 minutes-30 minutes under the normal pressure at 130 DEG C-140 DEG C, and evaporating for 15 minutes-25 minutes by reducing the pressure to 0.3 MP-0.5MP to obtain a swainsonine pure product. The extracting process of the swainsonine in the astragalus strictus can be used for realizing further improving the extracting efficiency of the swainsonine on the basis of shortening the extracting time.

The invention discloses Swainsonine for treating immunity inflammation. The Swainsonine is used for preparing a medicine for treating rheumatoid arthritis. Compared with terfenadine and diclofenac sodium, the Swainsonine has the clear curative effect and is disclosed for the first time. Due to the fact that the Swainsonine is of the brand new skeleton type and has the high inhibitory activity for rheumatoid arthritis, the Swainsonine has outstanding substantive features and meanwhile has the remarkable progress on preventing and treating the rheumatoid arthritis.

The invention provides a swainsonine derivative and a preparation method of a research reagent of the swainsonine derivative. The swainsonine is prepared through the following synthesis steps: a, adding chloroacetic acid and potassium hydroxide by taking swainsonine as a raw material and taking water as a solvent; b, feeding hematoporphyrin into thionyl chloride, and then adding cordycepin; and c, pouring the product obtained in the step a into the product obtained in the step b, and dropwise adding newly prepared potassium ethoxide into the obtained mixture, so that a swainsonine derivative solution is obtained. The swainsonine derivative disclosed by the invention is a product derived on the basis of a swainsonine structure, and by comparing, the difference is as follows: an enriched heterocyclic ring is connected, so that the swainsonine derivative disclosed by the invention has a function of enriching cancer cells, and can allow drugs to tend to parts with tumors but allow the drug concentration of other parts to be little.

The invention provides a method for preparing swainsonine by solid fermentation, and relates to the technical field of separation and purification of secondary metabolites of fungi. The method includes performing solid culture on plant endophytes producing swainsonine, performing extraction on the obtained fermentation product with a water-containing organic solvent, followed by extraction with petroleum ether, ethyl acetate and an alkaline water saturated n-butanol solution to obtain an alkaline n-butanol layer; and subjected the alkaline n-butanol layer to silica gel column chromatography and preparative liquid chromatography to obtain the pure product of swainsonine. Compared with the existing swainsonine extraction method, the method provided by the invention shortens the extraction time and saves the extraction cost, and the purity of the prepared swainsonine can reach 99%. The method provided by the invention saves the problems of high cost, long time and great difficulty in obtaining the pure product of swainsonine by the prior art.

The invention discloses an Oxytropis embellisia strain FEL1a-AVB3 that is used for swainsonine synthesis and preserved in China Center for Type Culture Collection with the preservation date of October 8th, 2008 and CCTCC NO. of M 208142. The invention further discloses a strain separation method. The FEL1a-AVB3 strain parasitizes inside tissues of astragalus variabilis including leaf, stem, flower and seed, accretes with the astragalus variabilis and does not cause diseases of the astragalus variabilis, in vitro cultivation discovers that the FEL1a-AVB3 strain can generate SW, participates in the SW biosynthesis of the astragalus variabilis and is closely related with toxicity of the astragalus variabilis, and consequently SW content in the astragalus variabilis can be lowered by inhibiting the FEL1a-AVB3 growth in the astragalus variabilis, and the goal for reducing the astragalus variabilis toxication of animals can be achieved.

The invention provides a 8, 8-difluoro-swainsonine [(-)-Swainsonine] derivative and a preparation method thereof. The preparation method includes following steps: reacting S-tert-butyl sulfonamide with acrolein to prepare S-sulfoximine; reacting S-sulfoximine, zinc powder and difluro ethyl bromoacetate (BrCF2CO2Et) to generate a compound shown as a formula 4; reducing the compound shown as the formula 4 to obtain aldehyde; subjecting aldehyde directly to Wittig reaction to obtain alpha, beta-unsaturated ester; reducing the alpha, beta-unsaturated ester to obtain primary alcohol; adding mesyl on primary hydroxyl of the primary alcohol; enablig an obtained compound to be in intramolecular nucleophilic substitution reaction to obtain a compound shown as a formula 11; removing sulfinyl from the compound shown as the formula 11 to obtain a hydrochloride; adding allyl on the hydrochloride to obtain a compound shown as a formula 3; using the compound shown as the formula 11 as a raw material to prepare a target product. The compound prepared serves as both a glycosidase inhibitor and monosaccharide having inhibition selectivity.

A biological fermenting process for purifying swainsonine includes such steps as biological fermenting engineering with pulse rhizoctonia 7-3 strain to culture its mycelia containing high content of swainsonine, extracting in alcohol solvent, cationic exchange, silica-gel column chromatography and segmental sublimation. Its advantages are low cost, high purity (more than or equal to 99%) and high output rate.

The invention discloses a swainsonine derivative, which has the following chemical structural formula: the swainsonine derivative can be obtained by reacting aspirin and swainsonine through an acid chloride esterification method. Compared with swainsonine, the derivative has stronger antiviral activity and can be used to prepare antiviral drugs, such as anti-canine distemper virus drugs.

The invention provides application of swainsonine, and the swainsonine is used as a plant hopper repellent for preventing and controlling plant hoppers of crops, so that the crops can be protected from being damaged by the plant hoppers. The inventor shows that swainsonine has an excellent repelling effect on plant hoppers through a large number of indoor biological activity tests, particularly on rice brown plant hoppers, and field tests show that after the swainsonine is sprayed to the rice, the harm of the brown plant hoppers, laodelphax striatellus and sogatella furcifera to the rice can be obviously inhibited. The invention provides a new method for using swainsonine, and also provides a green, safe and efficient new repellent for preventing and controlling plant hoppers of crops. The invention further provides a method for extracting swainsonine from industrial cannabis sativa, the swainsonine can be effectively extracted through the method, the raw material source of the swainsonine is widened, meanwhile, the utilization range of the industrial cannabis sativa is widened, and a new thought and a new method are provided for a new plant protection technology.

The invention discloses a swainsonine antigen, which has the following chemical structure formula: wherein, BSA is bovine serum albumin. Its preparation process includes: (1) swainsonine reacts with glutaric acid monoethyl chloride to obtain compound I: compound I is dechlorinated under the action of alkali, and acidified to obtain compound II: Under the action of propyl)-3-ethylcarbodiimide hydrochloride and 1-hydroxybenzotriazole, the compound II is condensed with BSA to obtain the described swainsonine antigen. The synthesis process of the swainsonine antigen of the invention is simple, easy to operate, low in cost and high in coupling ratio, and the antigen can produce high-titer antibodies, opening up a new way for the rational development and utilization of locoweed plants.

The invention discloses a method for separating swainsonine by using counter-current chromatography. According to the invention, methyl tert-butyl ether, n-butanol and water are mixed and then stood for layering so as to form a solvent system for a counter-current chromatographic stationary phase and a counter-current chromatographic mobile phase; the stationary phase is pumped into a separation column of a counter-current chromatographic instrument at a great flow velocity; after the separation column is full of the stationary phase, the instrument is started, the main engine of the counter-current chromatographic instrument is allowed to rotate at a set rotating speed, and then the mobile phase is pumped into the separation column at a certain flow velocity; after the two phases reach dynamic balance in the separation column, sample introduction is carried out through a sample introduction valve; fractions are collected by an automatic fraction collector; and thin layer chromatography and high performance liquid chromatography are used for detection, fractions containing a swainsonine component are combined together, then a solvent is recovered, and recrystallization is carried out so as to obtain swainsonine with a purity greater than 90%. The method provided by the invention has the advantages of easiness, convenience, fastness, a good separation effect, a great preparation quantity, small loss of a sample, low separation cost, high product purity and suitability for industrial production.

The invention discloses Arthrobacter sp. HW08 for degrading swainsonine, which is preserved in a common microbe center of the China Microbial Culture Preservation Commission in September 28th, 2009 and has the preservation number of CGMCC No. 3313. The bacterial colony of a bacterial strain is in a circular shape and gradually changed into faint yellow from oyster white with the prolongation of culture time, has a smooth, moist and raised surface and neat edges and is non-transparent; and the bacterial strain is cultured within 48 hours in an inorganic salt culture medium, basically belongs to a stab cell, has the size of 0.3-0.5 micrometer*0.5-1.0 micrometer, is gradually changed into a ball shape after cultured for 48 hours and has the diameter about 0.60-0.8 micrometer. The bacterial strain is obtained by separating and screening from soil embedding yellowflower crazyweed herbs (loco weeds) and has the capacity of efficiently degrading the swainsonine, i.e. toxins of the loco weeds.

The invention relates to novel 3, 5, and / or 6 swainsonine analogues, processes for their preparation and their use as therapeutic agents. The invention also relates to pharmaceutical compositions containing the compounds and their use as therapeutics.