35 results about "Cucurbitacin B" patented technology

The invention relates to a method for extracting cucurbitacin B. The method comprises the following steps of: crushing a raw material of muskmelon pedicel, and wetting the crushed muskmelon pedicel with acidic water; adding a biological enzyme for enzymolysis for 2-4 days at 30-40 DEG C; extracting zymolytic raw materials 2-3 times with 80-95% ethanol; enabling the extracting solution to flow by a short active carbon alumina column and then concentrating until the ethanol concentration is 30-50 percent; standing and crystallizing; carrying out the cold dissolution treatment with chloroform for secondary crystallization; and dissolving under the refluxing of 90-99% ethanol, decoloring with active carbon, removing impurities, recrystallizing, and the like. The method adopted for producing the cucurbitacin B has the advantages of high product yield, low cost and simple process and is easy to operate. The invention is suitable for industrial production.

The invention discloses a traditional Chinese medicine active extract with temperance function, and a preparation method and application thereof. The main active components in the traditional Chinese medicine active extract with temperance function are cucurbitacin compounds, especially cucurbitacin B and cucurbitacin D. The invention also discloses a preparation method of the active extract, andapplication of the active extract in preparing medicines for treating alcoholic psychosis or medicines with temperance function. The active extract can be added by conventional traditional Chinese medicine preparation methods to prepare any clinical preparation after adding various auxiliary materials and carriers required by preparation of different preparation formulations. The active extract disclosed by the invention is a low-toxicity traditional Chinese medicine extract which can be used for effectively treating alcohol dependence and preparing medicines with abstinence function.

The invention belongs to the technical field of cell culture, and concretely relates to a culture medium applicable to dental pulp stem cell in vitro culture and a preparation method thereof. The culture medium applicable to dental pulp stem cell in vitro culture provided by the invention comprises a basal culture medium and an additive added in the basal culture medium, wherein the additive is prepared from the following components with final concentration: catalase with the final concentration of 3 to 5 mg / L, coenzyme Q10 with the final concentration of 0.2 to 0.4mu M, linolenic acid with the final concentration of 7 to 9mu M, platelet-derived growth factor with the final concentration of 1 to 3mu g / L, cucurbitacin B with the final concentration of 0.2 to 0.6mg / L, lipoic acid with the final concentration of 0.12 to 0.15mg / L, folic acid with the final concentration of 12 to 15mu M, carboxymethyl chitosan with the final concentration of 0.5 to 1g / L, epidermal growth factor with the final concentration of 8 to 10mu g / L, taurine with the final concentration of 7 to 10mg / L, and attachin with the final concentration of 22 to 30mu g / L. The culture medium provided by the invention is high in safety, lower in price, and beneficial for remarkably improving the proliferation speed of dental pulp stem cells.

The invention discloses an application of cucurbitacin B and analogs thereof in the preparation of drugs for treating endometrial cancer, wherein the analogs are generated by changing the groups in the R1, R2, R3, R4, R5, X, Y, a, and b positions in the cucurbitacin B molecule, and the drugs can be used to carry out an individualized treatment for endometrial cancer patients, wherein the endometrial cancer can be idiopathic or metastatic. Cucurbitacin B and analogs thereof can be any pharmaceutically acceptable cucurbitacin B and analogs thereof, the cucurbitacin B and analogs thereof have one or more components which have the function of inhibiting epidermal growth factor receptor (EGFR), the cucurbitacin B and analogs thereof can be individually used to cure cancer or can be used with other treatments or drugs, such as radiotherapy, chemotherapy, surgical therapy, other growth factor inhibitors and sex hormone inhibitors, and any drugs or methods for treating cancer. Through inhibiting the epidermal growth factor receptor (EGFR), the cucurbitacin B and analogs thereof inhibit the tumor cell proliferation so as to achieve the goal of individualized treatment, and the cucurbitacin B and analogs thereof can be individually used to treat cancer or used with other drugs or treatments for cancer treatment.

The present invention belongs to the field of medicine technology, and provides cucurbitacin refining process and preparation. The cucurbitacin refining process includes the following steps: 1. dissolving marketed cucurbitacin in C1-C4 alcohol-water dissolved ketone to obtain solution A containing cucurbitacin in 0.1-10 g each 100ml; 2. adding active carbon in0.01-10 g for each 100 ml, stirring for 1-60 min and filtering out carbon to obtain solution B; 3. adding water into solution B to reach alcohol / water volume ratio of 1 to 1-10, and stirring until the solution becomes turbid; 4. letting stand for over night; and 5. filtering, collecting precipitate and drying. The refining process can lower the toxicity of cucurbitacin product, has no altering on cucurbitacin B content and is suitable for industrial production. The cucurbitacin product may be prepared into different preparations for treating tumors, increasing peripheral blood leukocytes and treating hepatitis.

The invention discloses a traditional Chinese medicine active extract with temperance function, and a preparation method and application thereof. The main active components in the traditional Chinese medicine active extract with temperance function are cucurbitacin compounds, especially cucurbitacin B and cucurbitacin D. The invention also discloses a preparation method of the active extract, andapplication of the active extract in preparing medicines for treating alcoholic psychosis or medicines with temperance function. The active extract can be added by conventional traditional Chinese medicine preparation methods to prepare any clinical preparation after adding various auxiliary materials and carriers required by preparation of different preparation formulations. The active extract disclosed by the invention is a low-toxicity traditional Chinese medicine extract which can be used for effectively treating alcohol dependence and preparing medicines with abstinence function.

The invention provides streptomycete (Streptomyces sp.) RW-2 used as a glycosidase producing bacterium and application of the streptomycete in preparing cucurbitacin B during biotransformation of cucurbitacin B-2-O glucoside. A bacterial strain is preserved in China Center for Type Culture Collection, the address of the China Center for Type Culture Collection is Wuhan University in Wuhan, China, the postcode is 430072, the preservation number is CCTCC NO:M2013330, and the preservation date is July 17th, 2013. The streptomycete has the beneficial effects that (1) the streptomycete is a common bacterium in the fermentation industry and is safe to use without toxicity and harms; (2) the nutritional requirements of the streptomycete RW-2 are simple, the growth speed of the streptomycete RW-2 is rapid, and the streptomycete RW-2 is easily cultivated; (3) the glycosidase prepared by the streptomycete RW-2 is extracellular enzyme, thallus is removed by separating the extracellular enzyme to obtain crude enzyme, or the crude enzyme can be used as a biotransformation system after being diluted; (4) after biotransformation treatment on total cucurbitacin extracted from muskmelon pedicel, the cucurbitacin B-2-O glucoside can be almost entirely transformed into the cucurbitacin B, and the content of the cucurbitacin B can be increased by 1-2.7 times.

The invention discloses an HPLC (High Performance Liquid Chromatography) method for utilizing a chiral column to separate, identify and prepare a monomer matter from a cucurbitacin mixture. The process conditions of the HPLC method are as follows: the chiral column using an amylose derivative as a solid phase is taken as a chromatographic column; more than two mixtures of isopropanol, alcohol, methyl alcohol, acetonitrile, normal hexane, isohexane, n-pentane, trifluoroacetic acid and glacial acetic acid are taken as mobile phases; and a detection wavelength is 220nm-270nm. The HPLC method provided by the invention is characterized by simple operation, high accuracy and strong specificity. The HPLC method can be used for excellently separating matters, such as cucurbitacin B, iso-cucurbitacin B, dihydro cucurbitacin B, cucurbitacin E, and the like, from the cucurbitacin mixture, can be used for preparing various cucurbitacin monomers from the cucurbitacin mixture and also can be used for accurately measuring contents of cucurbitacin raw materials and various cucurbitacins in a prepared product.

The invention discloses application of cucurbitacin B and a derivative thereof in preparation of an anti-tumor drug-resistant drug. It is found that the cucurbitacin B inhibits proliferation of an ovarian cancer cis-platinum drug-resistant cell strain, and the IC50 values of the cucurbitacin B to C13 * and A2780DDP cells are 64.28 + / -14.54 nM and 29.20 + / -2.26 nM respectively; the apoptosis of C13 * cells is promoted, and invasion and migration of the C13 * cells are inhibited; and PI3K / Akt signal channels in C13 * and A2780DDP cells are inhibited. Therefore, the cucurbitacine B is applied to preparation of anti-tumor drug-resistant drugs. The cucurbitacine B has a good development prospect.

The invention discloses a cucumber exosome-like vesicle containing cucurbitacin B and can be used as an anticancer drug. Cucurbitacin B can be used to inhibit the proliferation of various cancer cells, but its extraction method is complicated and time-consuming. The method of isolating cucumber exosome-like vesicles to obtain cucurbitacin B has the advantages of simple and rapid operation, and the lipid bilayer of exosome-like vesicles, as the natural protective film of cucurbitacin B, can be used for a long time. maintain its stability. Moreover, the presence of the lipid bilayer also increased the uptake rate of cucurbitacin B by cells to a certain extent through the principle of similar compatibility. When acting on adenocarcinoma human alveolar basal epithelial cells (A549 cells), the maximum cell activity inhibition rate of cucumber exosome-like vesicles is twice that of cucurbitacin B standard, and the dosage is lower, which can reduce the toxicity to normal cells It has good anticancer potential and industrialization prospects, and is of great significance in clinical tumor treatment applications.

The invention discloses a method for separating cucurbitacin B from muskmelon vines by virtue of catalytic reaction. The method comprises the following steps: an extraction process, namely taking 1 part of the muskmelon vines, soaking by using ethanol, performing reflux extraction, and filtering and concentrating an extracting solution to obtain an extract; the catalytic reaction, namely adding concentrated hydrochloric acid into the extract, then adding ferric trichloride hexahydrate, stirring and reacting, cooling to the room temperature, filtering, performing water rinsing, and drying; a refining process, namely stirring and dissolving a crude product by using ethyl acetate, then adding activated carbon, decoloring, concentrating to a small volume, and standing overnight to perform crystallization; a recrystallization process, namely dissolving a like fine product by using ethanol, filtering and concentrating to a small volume while hot, standing overnight to perform crystallization, and filtering; and putting the fine product in a vacuum drying box, and drying for 8 hours to obtain a cucurbitacin B fine product. The method disclosed by the invention is wide in raw material source and low in production cost, and can be used for reducing the damages of an acid environment to cucurbitacin B; the production rate reaches more than 60%, the purity is more than 99.0%, and the wastewater BOD (biochemical oxygen demand) is less than 100; the method is suitable for the industrial production of recycling water, and can be widely applied to plant extraction industries.

The invention discloses an application of cucurbitacin B and analogs thereof in the preparation of drugs for treating endometrial cancer, wherein the analogs are generated by changing the groups in the R1, R2, R3, R4, R5, X, Y, a, and b positions in the cucurbitacin B molecule, and the drugs can be used to carry out an individualized treatment for endometrial cancer patients, wherein the endometrial cancer can be idiopathic or metastatic. Cucurbitacin B and analogs thereof can be any pharmaceutically acceptable cucurbitacin B and analogs thereof, the cucurbitacin B and analogs thereof have one or more components which have the function of inhibiting epidermal growth factor receptor (EGFR), the cucurbitacin B and analogs thereof can be individually used to cure cancer or can be used with other treatments or drugs, such as radiotherapy, chemotherapy, surgical therapy, other growth factor inhibitors and sex hormone inhibitors, and any drugs or methods for treating cancer. Through inhibiting the epidermal growth factor receptor (EGFR), the cucurbitacin B and analogs thereof inhibit the tumor cell proliferation so as to achieve the goal of individualized treatment, and the cucurbitacin B and analogs thereof can be individually used to treat cancer or used with other drugs or treatments for cancer treatment.

The invention discloses a method of preparing a natural product cucurbitacin B. According to the method, a supercritical fluid extraction method is adopted to extract a total cucurbitacin extract product from plant, then a silica gel column separation and purification manner is adopted to obtain the cucurbitacin B, and the purity of the cucurbitacin B is higher than 90%. Compared with the prior art, the method for preparing the cucurbitacin B has advantages of short time, high efficiency, small solvent using amount, low environment pollution, and suitability for large-scale production and operation.

The invention provides streptomycete (Streptomyces sp.) RW-2 used as a glycosidase producing bacterium and application of the streptomycete in preparing cucurbitacin B during biotransformation of cucurbitacin B-2-O glucoside. A bacterial strain is preserved in China Center for Type Culture Collection, the address of the China Center for Type Culture Collection is Wuhan University in Wuhan, China, the postcode is 430072, the preservation number is CCTCC NO:M2013330, and the preservation date is July 17th, 2013. The streptomycete has the beneficial effects that (1) the streptomycete is a common bacterium in the fermentation industry and is safe to use without toxicity and harms; (2) the nutritional requirements of the streptomycete RW-2 are simple, the growth speed of the streptomycete RW-2 is rapid, and the streptomycete RW-2 is easily cultivated; (3) the glycosidase prepared by the streptomycete RW-2 is extracellular enzyme, thallus is removed by separating the extracellular enzyme to obtain crude enzyme, or the crude enzyme can be used as a biotransformation system after being diluted; (4) after biotransformation treatment on total cucurbitacin extracted from muskmelon pedicel, the cucurbitacin B-2-O glucoside can be almost entirely transformed into the cucurbitacin B, and the content of the cucurbitacin B can be increased by 1-2.7 times.

The invention belongs to the technical field of medicine and discloses novel application of Cucurbitacins, namely novel application of Cucurbitacin B, Cucurbitacin B substances, Cucurbitacin BE and a pharmaceutical composition thereof in a medicine for treating ovarian cancer and improving the quantity of leukocytes of radiotherapy patients. The Cucurbitacin can also be a cucurbitacin B monomer, an isocucurbitacin B monomer, a dihydrocucurbitacin B monomer, a cucurbitacin I monomer, and a cucurbitacin O monomer. The Cucurbitacins or pharmaceutical compositions thereof can be matched with a pharmaceutically acceptable carrier and prepared into a tablet, a capsule, a granule, powder, a plaster, an ointment, an aerosol, a suspension, a syrup, an oral liquid, and an injection, and can also be prepared into special dosage forms such as a liposome, microspheres, nanoparticles and an emulsion for cavity administration, external use, oral administration and injection. The individual administration or the combined treatment can be performed, the administration dosage of the Cucurbitacins is calculated according to the total Cucurbitacins, the dosage for healthy adults is between 0.1 and 5mg / d, the best dosage is between 0.3 and 3mg / d, and the administration is performed for 1 to 4 times.