58 results about "Pinocembrin" patented technology

The invention discloses a pinocembrin and cyclodextrin or cyclodextrin derivative inclusion compound, wherein cyclodextrin or a cyclodextrin derivative is used to include the pinocembrin. The inclusion compound contains the pinocembrin and the cyclodextrin or cyclodextrin derivative in a molar ratio of 1:1-100. The inclusion compound can improve the water solubility of the pinocembrin and give good play of the therapeutic action of the pinocembrin. The inclusion compound is suitable for the preparation of sold dosage forms and liquid dosage forms required by clinics, including infusion solution, water injection, powder injection, oral solution, syrup, tablets, capsules, granules and dispersible tablets. The inclusion compound can be used for preparing drugs for preventing and\or treating cardiovascular and cerebrovascular diseases, particularly brain stroke, as well as drugs for preventing and\or treating bacterial and\or fungal infections.

Inclusion complexes of pinocembrin with cyclodextrin or its derivatives and their preparation are provided. The inclusion complexes can be used to make drugs.

FtsZ, the bacterial analog of tubulin, is a promising new target for developing new antibiotics. It has been shown that polyphenols inhibit the GTPase activity of FtsZ, thereby inhibiting Z-ring formation during mitosis. The present invention provides novel polyphenols compounds, which can be accessed by the synthesis of dichamametin and 2′″-hydroxy-5″-benzylisouvarinol-B as described herein. These novel compounds are useful in treating infections, particularly infections caused by gram-positive organisms. Methods of preparing the inventive compounds are also provided. The compounds are prepared by the benzylation of pinocembrin or chrysin core structure. Pharmaceutical compositions and method of using the compounds to treat disease are also provided. These compounds may be screened for antimicrobial activity as well as other biological activities such as anti-neoplastic, anti-inflammatory, immunosuppressive, and cytotoxic activity.

The invention provides a method for composite enzymolysis-assisted extraction of an active ingredient from propolis, and belongs to the extraction technology of propolis. The method comprises the following steps of: selecting high-quality rough propolis as a raw material; removing impurities, refrigerating, crushing and then homogenously mixing a certain amount of enzymolysis agent; filling the mixed raw material on a biological enzymolysis bed; performing biological enzymolysis by adjusting parameters such as enzymolysis temperature, humidity, pH, time and the like; extracting flavonoid from the propolis in a classified way in an extraction tank by controlling factors such as alcoholic strength, solid-to-liquid ratio, temperature, pressure, time and the like; and performing reduced pressure distillation by controlling concentration temperature and vacuum degree to remove impurities and moisture. The method has the obvious advantages that: 1, a propolis enzymolysis technology and a propolis alcohol extraction technology are integrally applied to production practice, and the method has a simple process and an accurate technological parameter range and is easy in realization of industrialization; 2, the contents of flavone aglycones such as myricetin, quercetin, apigenin, pinocembrin and the like in extracted active ingredient of the propolis are increased; and 3, the antioxidative activity of a propolis enzymolysis product can be obviously improved.

The present invention provides a method for synchronized preparation of pinocembrin and 2', 4'-dihydroxy chalcone from oxytropis falcate bunge. By using Tibetan herb oxytropis falcate bunge as a raw material, via steps such as heating extraction by ethanol, extraction by ethyl acetate, precipitation by petroleum ether, ordinary silica and reverse phase silica gel column chromatography, highly purified pinocembrin and 2 ', 4'-dihydroxy chalcone are obtained. The pinocembrin and 2', 4'-dihydroxy chalcone prepared by the method of the present invention both have purities greater than 98%, and both have relatively high yields and extraction rates, wherein the yield and extraction rates of the pinocembrin are respectively 0.08 % and 67.5%, and the yield and extraction rates of the 2 ', 4'-dihydroxy chalcone are respectively up to 0.24% and 88.9%.

The invention relates to the medical field, discloses applications of racemes of pinocembrin, racemes of pinocembrin salt, racemes of pinocembrin precursors or racemes of pinocembrin hydrate in preparation of medicals for preventing and treating cerebral apoplexy, and further discloses the application of racemes of pinocembrin in prevention and treatment of acute ischemic stroke.

The invention discloses an Escherichia coli engineering bacterium for synthesizing pinocembrin by using glucose as a substrate and application thereof and belongs to the field of genetic engineering or metabolic engineering. Synthetic biology and metabolic engineering means are adopted to respectively synthesize a synthesis route consisting of eight genes in pinocembrin metabolism to be introduced into Escherichia coli (BL21), accordingly the recombinant bacterium for synthesizing the flavone framework material pinocembrin by using the glucose as the substrate, and the pinocembrin yield reaches to 21mg/L after glucose serves as the unique substrate in a shake flask to be fermented for 60 hours. The synthesis route consisting of the eight genes is successfully built in the Escherichia coli, and synthesis from the glucose into the pinocembrin is achieved successfully. Certain reference significance is provided for flavonoid material production by means of a microbiological method in the future.

The invention provides an application of pinocembrin dihydrogen chalcone-7-O-[3'-O-galloyl-4',6'-hexahydroxydiphenodicarboxy]-beta-D-glucoside in preparation of a liver protection medicine. The penthorum chinense pursh macrocyclic polyphenol monomer namely pinocembrin dihydrogen chalcone-7-O-[3'-O-galloyl-4',6'-hexahydroxydiphenodicarboxy]-beta-D-glucoside has a liver protection effect, can be used for preventing and treating liver injuries, and has a definite curative effect on hepatic ischemia-reperfusion injuries and chronic liver injuries, and the effect is superior to that of positive medicine namely Gansu Granules, so that the penthorum chinense pursh macrocyclic polyphenol monomer can be used for replacing the Gansu Granules and has a good clinical application prospect.

The invention discloses a method for preparing five compounds with anti-inflammation activities from oxytropis falcate bunge by separation. The five compounds include pinocembrin, 4-hydroxyl-2-methoxychalcone, 7-hydroxyflavanone, 2, 4-dihydroxyl-dihydrochalcone and 2, 4-dihydroxyl-chalcone. The method includes the steps: (1) taking total flavone extracts of the oxytropis falcate bunge, sequentially extracting by the aid of petroleum ether and ethyl acetate, and taking ethyl acetate portions; (2) taking ethyl acetate portion drying powder, purifying by the aid of a resin, eluting by the aid of methyl alcohol, drying eluting substrates to obtain purified substrates; (3) separating the purified substrates by a preparative chromatography to obtain the pinocembrin, the 4-hydroxyl-2-methoxychalcone, the 7-hydroxyflavanone, the 2, 4-dihydroxyl-dihydrochalcone and the 2, 4-dihydroxyl-chalcone. The method is large in preparation quantity, high in product purity and suitable for industrial application.

The invention provides an efficient health-care product for supplementing selenium and a preparation method thereof. The product comprises 60-120 parts by weight of VE, 40-50 parts by weight of organic selenium, and 1800-2100 parts by weight of honey. The preparation method of the health-care product comprises weighing the VE, the organic selenium and the honey, conducting uniform mixing, and conducting refrigeration in a refrigerator until the mixture becomes a paste and no delamination exists. The health-care product for supplementing selenium is a compound containing three ingredients, and while supplementing selenium, the health-care product contains the VE so as to promote selenium absorption of organisms, reduce selenium loss in bodies, and raise the utilization rate of selenium. Meanwhile, selenium can also promote VE absorption, reduce VE loss in bodies, and raise the utilization rate of the VE as well. Besides, with the addition of honey, the health-care product becomes the selenium-VE-honey mixture; and not only the honey improves a mouth feel, but more importantly, an antioxidant component pinocembrin peculiar to the honey realizes efficacy synergy with the selenium. Meanwhile, the honey contains a plurality of vitamins and biological enzymes for efficacy complementation with the selenium. The three raw materials of the selenium, the VE and the honey stimulate one another and play the health-care effect of "1+1+1>3".

The invention relates to a method for synthetizing (R)-(plus)-pinocembrin and (S)-(minus)-pinocembrin, phloroglucinol and (S)-3-hydroxyl-3 ethyl phenylpropiolate are taken as raw materials, the hydroxyl of the phloroglucinol is protected by methyl or methoxy methyl and Weinreb amine ((S)-3-(tert-butyl dimethyl silyl)-N-methoxy-N-methyl-3-phenyl acrylic amide) which is protected by silyl carry out Weinreb reaction under the organic alkali condition, so (S)-1-[2, 4-dimethoxy-6-(methoxy-methyl)-phenyl]-3-phenyl-3-(tert-butyl dimethyl silyl)-propyl-1-ketone is obtained, the methoxy-methyl is removed under the acid condition, intramolecular Mitsunobu cyclization is carried out, and finally, the (R)-(plus)-pinocembrin is obtained after removing the methyl. According to the same method, (R)-3-hydroxyl-3 ethyl phenylpropiolate is taken as the raw material, so the (S)-(minus)-pinocembrin can be obtained.

The invention discloses a pharmaceutical composition and a preparation method thereof. The pharmaceutical composition comprises quercetin, gallic acid, quercetin-3-0-alpha-L-rhamnopyranoside, pinocembrin-7-0-beta-D-glucopyranose and 2,6-dihydroxyacetophenone-4-0-D-glucopyranose. Compared with the existing drug, the pharmaceutical composition can protect liver and reduce transaminase and relieve the jaundice symptoms, has definite therapeutic effects and has good safety.

The invention provides a pinocembrin synthesis method. The method comprises the following steps that under the room temperature condition, phloroglucinol and acetonitrile are stirred to be uniform, phosphorus oxychloride is added for a reaction, and 2,4,6-trihydroxyacetophenone is obtained; under the catalytic action of a catalyst L-proline, obtained 2,4,6-trihydroxyacetophenone and benzaldehyde are subjected to a ring closing reaction in DMF, and a crude pinocembrin product is obtained; the obtained crude pinocembrin product is subjected to recrystallization with ethyl alcohol, activated carbon is adopted for decolourization, and the pinocembrin is obtained. The synthesis method is simple in technology, low in cost, capable of saving time, high in yield and suitable for industrial production.

A medical product containing either an active ingredient of propolis which is a natural antibiotic or a grapefruit seed extract, and a manufacturing method thereof are provided. The medical product is impregnated with a solution of CAPE (caffeic acid phenethyl ester) or pinocembrin, which is an active ingredient of propolis having antibacterial effects, to increase the antibacterial activity of the medical product due to antibacterial compounds contained in the active component, or the medical product is impregnated with a solution of a grapefruit seed extract such that the extract can exhibit antibacterial activity in the medical product.

The invention discloses a method for extracting and separating a flavonoid compound pinocembrin-7-O-belta-D-glucoside from a hairy fig and application of the pinocembrin-7-O-belta-D-glucoside and belongs to the technical field of botanical pesticides. Particularly the compound is separated with the method of subjecting a hairy fig crude extract to macroporous resin column chromatography, Sephadex LH-20 gel column chromatography and recrystallization, and the compound has good bacteriostatic activity to citrus postharvest pathogen-penicillium italicum and good disease resistance to citrus blue mold and can be used for developing a novel plant source citrus preservative.

The invention relates to an application of a dihydroflavone derivative in herba penthori chinense in preparing a drug for resisting liver cell steatosis. A structural formula of the dihydroflavone derivative is as shown in formulas I-1, I-2 or I-3. The invention researches an effect of three dihydroflavones in herba penthori chinense extract for resisting the liver cell steatosis. The herba penthori chinense extract is divided into five components by adopting an MCI column, three characteristic dihydroflavones in the component V are selected to obtain pinocembrin (PCB), pinocembrin -7-O-beta-D- glucoside (PCBG) and 5-methoxyl-pinocembrin-7-O-beta-d-glucoside (MPG), the free fatty acid is adopted to induce a HepG2 cell injury model to investigate the influence of the PCBG, PCB and MPG for cell activity, fat content, TC, TG, ALT, AST, MDA, SOD and GSH-Px. The result shows that the three characteristic dihydroflavones in the herba penthori chinense respectively have the activity for resisting the liver cell steatosis.

The invention relates to the technical field of medicine, provides application of pinocembrin, pinocembrin salts, pinocembrin precursors or pinocembrin hydrates to preparation of medicines for treating demyelination diseases and further provides a pharmaceutical preparation for preventing or treating the demyelination diseases. The pharmaceutical preparation is composed of pinocembrin, pinocembrin salts, pinocembrin precursors or pinocembrin hydrates and pharmaceutically-acceptable auxiliary materials. By in-vitro pharmacodynamic experiments, pinocembrin is capable of promoting differentiation and maturation of oligodendrocyte precursor cells which are myelin sheath source cells in transcriptional level and protein level, myelin sheath related expression is increased, and certain dose dependency is shown; by in-vivo experiments, pinocembrin is capable of evidently alleviating animal disease process and disease severity and also has a remarkable inhibition effect on inflammatory cell infiltration and demyelination injuries and a remarkable effect of remyelination promotion, and a new basis is provided for treatment of the demyelination diseases and multiple sclerosis.

The invention discloses an insecticide composition containing bacopaside II, which includes the bacopaside II and pinocembrin according to the weight part ratio of 1:1-30:1. In the invention, the bacopaside II and the pinocembrin are compounded at certain ratio, so that the insecticide composition has excellent synergistic effect in prevention and treatment on bradysia odoriphaga; and especially, when the weight part ratio of the bacopaside II to the pinocembrin is 19-20:1, the synergistic effect is more significant.

The invention belongs to the field of natural compound extraction, and particularly relates to a method for extracting and detecting flavonoids from galangal. In the prior art, subcritical extractionof the flavonoids in galangal mostly adopts an organic solvent as an extraction reagent or is combined with ultrasonic extraction. The method only adopts subcritical water as the extraction reagent, and studies the optimum preparation conditions for extraction of seven substances of quercetin, pinocembrin, isorhamnetin, kaempferol, kaempferide, galangin and curcumin. A galangal extract obtained bythe preparation method can be directly applied to an oral preparation due to the fact that an organic reagent is not introduced during the preparation process. In addition, a high-performance liquidphase detection condition for the galangal extract is provided, and can simultaneously detect flavonoid compounds, and the repeatability is good. The extract and the method are applied to the preparation of cardiovascular drugs and have important production significance.

The invention discloses a pinocembrin and cyclodextrin or cyclodextrin derivative clathrate compound. Cyclodextrin or cyclodextrin derivatives are used for realizing the clathration on pinocembrin, the clathrate compound comprises the pinocembrin and cyclodextrin or cyclodextrin derivatives according to a mol ratio being 1:(1-100). The water solubility of the pinocembrin is improved, the treatment effect of the pinocembrin is more perfectly realized, the clathrate compound is suitable for being used for preparing solid preparations and liquid preparations required in clinics, and the preparations include transfusion, water injection, powder injection, oral liquid, syrup, tablets, capsules, granules and dispersible tablets. The clathrate compound can be used for preparing medicine for preventing and/or treating cardiovascular and cerebrovascular diseases, particularly cerebral apoplexy, and can also be used for preparing medicine for preventing and/or treating germ and/or fungal infection.

The invention discloses a bactericide for preventing and treating botrytis cinerea. The bactericide is prepared from quassin and pinocembrin, wherein the weight part ratio of the quassin to the pinocembrin is (1: 1) to (25: 1). By mixing the quassin and the pinocembrin under a specific proportion, the bactericide has an extremely good effect of synergistically preventing and treating the botrytis cinerea.

The present invention relates to a method for resolution of a mixture of pinocembrin optical isomers, in particular a pinocembrin racemate, using a chiral primary amine or a chiral sulfinamide. The present invention also relates to a (R)-(+)-pinocembrin obtained by the method.

The invention relates to a freeze-dried product of liposome diluent of live pseudorabies vaccine and a preparation method thereof, belonging to the technical field of veterinary biological products. It contains the following components per 1000ml of PBS: 1-6g of pinocinol, 2-8g of procurdin, 5-10g of daidzein, 1-3g of paeoniflorin, 5-10g of liposome and 5-15g of lyoprotectant. The invention has the following beneficial effects: 1) The freeze-dried product of a liposome diluent of a pseudorabies live vaccine prepared by the invention can make pigs produce antibodies in advance and reduce the blank period of immunity. 2) The freeze-dried product of a liposome diluent of live pseudorabies vaccine prepared by the present invention can not only enhance the immunity of pigs, but also prolong the protection period of the vaccine and improve the immune effect of the live vaccine of pseudorabies.

The invention discloses a method for splitting pinocembrin enantiomers through simulated moving bed chromatography. The method is characterized in that a simulated moving bed chromatographic system is adopted, a filler is amylase-tri(3,5-dimethylphenylcarbamate), a mobile phase is methanol, and the naproxen pinocembrin are split under normal phase conditions to obtain highly pure R-pinocembrin and S-pinocembrin. The simulated moving bed chromatographic system has the advantages of continuous production, high automation degree and high production efficiency.