141 results about "Arctigenin" patented technology

A composition for medicine having arctigenin and a method for preparing the same. The composition includes arctigeni, oil, emulsifier and water which is capable of producing emulsion for oral taking and intravenous.

The invention discloses a blautia sp. AUH-JLD56 and an application thereof in the conversion of arctigenin, and belongs to the technical field of bacterium. The preservation number of blautia sp. AUH-JLD56 is CGMCC No. 8032. The application of blautia sp. AUH-JLD56 comprises following steps: (1) culture of bacterium strain AUH-JLD56; (2) co-culture of a substrate, namely a coarse product of arctigenin, and a bacterium strain AUH-JLD56 and separation and purification of metabolite. The bacterium strain AUH-JLD56 can high effectively convert a coarse product of arctigenin in the traditional Chinese medicine actium lappa to 3'-demethylated-arctigenin, solves the 3'-demethylated-arctigenin resource shortage problem, and lays a foundation for researching and developing microorganism metabolite of pharmacological active substance in actium lappa.

The invention relates to a method of preparing antivirus and antitumor natural medicine arctigenin, and its characteristic: crushing the Arctium lappaL., using organic solvent to degrease, and obtaining a crude arctiin, then using snailase to make fermentation and enzymolysis the on the crude arctiin in an enzyme reaction system, and finally terminating the enzymolysis reaction by alcohol-containing water-soluble organic solvent and extracting enzymolysis products, then separating the enzymolysis products by using silica gel column chromatography and solvent recrystallization, purifying and obtaining the pure arctigenin; the yield of the method is increased by at last over 20 times as compared with that of separating natural-existing arctigenin in plants like Arctium lappaL.

The present invention is use of arctigenin in preparing medicine for preventing and treating chronic kidney failure and kidney fibrosis. The present invention also provides medicine composition with arctigenin as active component for preventing and treating chronic kidney failure and kidney fibrosis. When the medicine composition is applied in preventing and treating chronic kidney failure and kidney fibrosis, the injection has dosage of 30mg-1000 mg, preferably 30-500 mg, and the orally taken dosage is 50-2000 mg, preferably 50-800 mg.

The invention relates to an arctigenin carboxamide derivative, a preparation method thereof, a composition comprising the arctigenin carboxamide derivative and medical uses thereof, and particularly relates to the arctigenin carboxamide derivative shown in a general formula(I) or a pharmaceutically acceptable salt thereof, the preparation method thereof, the pharmaceutical composition comprising the arctigenin carboxamide derivative and the medical uses thereof. The arctigenin carboxamide derivative shown in the general formula(I) or the pharmaceutically acceptable salt thereof can be used for inhibiting formation of amyloid beta, so that the arctigenin carboxamide derivative shown in the general formula(I) or the pharmaceutically acceptable salt thereof can be used for preparation of drugs for treatment or prevention of alzheimer's disease (AD) or for improvement of memory.

A composition for medicine having arctigenin and a method for preparing the same, in particular the arctigenin is involved in a cyclodextrin derivative, which mixture ratio is in a range of 1g:3g-30g, and the composition can effectively increase solubility and bioavailability of the arctigenin.

The invention relates to a preparation method of arctigenin, which comprises the following steps: after pulverizing great burdock fruit, carrying out zymohydrolysis according to a self inherent hydrolase; extracting the medicinal material after zymohydrolysis to obtain a crude extract of the arctigenin and then purifying the crude extract of the arctigenin by a silica gel column chromatography method and a solvent recrystallization method to obtain a purified product of the arctigenin. The purity of the arctigenin is greater than or equal to 98%, and the yield is more than 2%. The arctigenin can be used as a bulk drug and is applied to the medicaments of various relevant diseases. The preparation method of the arctigenin has the advancement and the practical value that the method does not need to adopt an inflammable and explosive organic solvent to degrease the medicinal material, and the self inherent hydrolase of the great burdock fruit is also utilized to directly prepare the arctigenin from the medicinal material. The method is simple, convenient and practical and is more suitable for industrialized production. The preparation method adopts the self inherent hydrolase of the medicinal material for preparation and converts a compound, which is very rare at home and abroad at present.

Present Invention relates to a skin whitening cosmetic composition comprising arctiin, arctigenin or a mixture thereof as an active ingredient. The disclosed composition can control or inhibit the synthesis of melanin by acting on a melanin synthesis route of α-MSH secreted by UV, and thus show an excellent whitening effect compared to a conventional skin whitening cosmetic. Also, the composition has high formulation stability and low skin irritation.

The invention relates to the following general formula compound (I) and use of the general formula compound in preparing anti-inflammatory and anti-endotoxin medicines. In formula I, R is an acid solubilizing side chain of hydroxide radical in an arctigenin molecule, and can be an acid group or side chain imported through alkylation reaction or acylating reaction, such as sulphonic acid ester, sulfuric acid ester, organic phosphate, succinate, propionic ether, butyric ester, semi-succinate, semi-glutaric acid ester, semi-tartrate, semi-phthalic acid ester, m-benzene sulfonic acid ester and so on.

The invention relates to application of arctigenin as shown in general formula (1) and its derivative in preparing medicaments for improving body tolerance (resisting fatigue), and application of pharmaceutical compositions containing arctigenin and its derivative for improving body tolerance (resisting fatigue). The arctigenin and its derivative play a promoting role in AMPK phosphorylation. Whole animal tests show that compounds of the invention can enhance fatigue tolerance and can be used for anti-fatigue treatment.

The invention discloses a preparation method of high-purity arctigenin. The preparation method of the high-purity arctigenin does not need a heating return flow method to extract arctigenin constituents, does not need an enzymolysis method and a column chromatography, and directly uses ethyl acetate diacolation to extract arctiin in burdock, the potential of hydrogen (PH) value of a diacolation concentrated solution is adjusted to be 3.0-4.0, the arctiin is directly hydrolyzed to become an arctigenin crude product, and an opposite phase preparative liquid chromatography optimized by a large number of experiments is adopted to obtain the high-purity arctigenin. The preparation method of the high-purity arctigenin is reasonable and in the entire preparation process design, high in preparation efficiency, strong in operability, and suitable for industrialized mass production.

The invention provides a method for preparing arctigenin, which includes the steps: arctiin is used as a substrate, Beta-glucosidase enzyme liquid produced by the fermentation of aspergillus niger CGMCC No. 2594 is used as a catalyzer, the subsrate and the catalyzer are transformed in a shaker at the temperature of 20 DEG C to 50 DEG C and at the speed of 100r / min to 200r / min for 40h to 64h; and the transformed solution is separated and purified to obtain the arctigenin. The method has the advantages of: 1. mild reaction conditions and being environmental-friendly; 2. simple preparation process of a biocatalyst, namely the Beta-glucosidase enzyme liquid, needing no complex zymoprotein separation and purification as well as low cost; 3. simple operation and relatively high biological transformation efficiency; and 4. easy amplification of the biological transformation process and easy realization of large scale industrialized production. By utilizing the method for producing, the molar yield of the arctigenin can reach 94.7 percent and the purity of the product can reach 99.7 percent.

The invention relates to a composition containing 50 to 99 parts by weight of arctiin with the purity of more than 90 percent or 1 to 50 parts by weight of arctigenin and a preparation method thereof, and the functions of the composition are the treatment and the prevention of diabetic retinopathy. In the invention, by extracting the arctiin and the arctigenin, the pharmacological, toxicological and clinical trial results show that the composition of arctiin or arctigenin of the invention has the advantages of strong treatment effect and small toxicity and side effects in the treatment of the diabetic retinopathy.

The present invention provides the application of arctiin or arctigenin in preparing medicine for preventing and treating diabetes and its complication. The present invention also provides the application of arctiin or arctigenin in preparing medicine composition for preventing and treating diabetes and its complication, and the medicine composition may be administrated through oral taking, injection or local application.

The invention provides a novel medical application of arctigenin, belonging to the field of medicine. According to the application of arctigenin in treating angiogenesis diseases provided by the invention, the arctigenin is applied to treating angiogenesis diseases, a good angiogenesis inhibiting effect is shown in a chorioallantoic membrane model test of a chicken embryo, which reminds that the arctigenin can be applied to treatment or auxiliary treatment of angiogenetic diseases. The medical application of arctigenin which inhibits angiogenesis reminds that the arctigenin has wide medical application prospect in treating diseases such as tumor and other pathological angiogenesis diseases such as diabetic retinopathy, psoriasis, atherosclerosis, rheumatoid arthritis and the like.

The invention relates to an anti-cancer pharmaceutical composition comprising arctigenin and a tyrosine kinase inhibitor. Compared to single-component medicines, the pharmaceutical composition provided by the invention has synergic anti-cancer activity in the aspect of non-small-cell lung carcinoma inhibiting. The invention also provides a micro emulsion preparation of the pharmaceutical composition.

The invention relates to the ligninoglycosides distilling material of the caulis trachelospermi and the distilling process. The overall distilling material includes the trachelosperogenin, the nortrachelosperogenin, the arctigenin and the matairesinol, the said four genins account for the exceeding eighty percentage of the overall distilling material. The producing process of distilling the ligninoglycosides overall distilling matetial from the caylis trachelosperogenin includes the ferment, the distilling and the dipping in the cream, translating the ligninoglycosides in the cream into the genins by the method of dispelling or enzyme melting, producing the coarse article of the ligninoglycosides and the purification. The invention is easy to produce and to handle. The cost is low. The output and the chief content of the efficient ingredient are improved greatly using the acid melting and the enzyme melting. So the invention provides a craftwork fitting for the industrialized producing of distilling the ligninoglycosides from the nature plate trachelospermi.

The invention relates to a method for preparing arctigenin from burdock. A process of the method comprises: taking burdock medicinal materials as raw materials; grinding the raw materials; performing methanol reflux extraction for 2 to 3 times; performing activated carbon decolorizing; concentrating the obtained product to have no alcohol after microfiltration and ultrafiltration; regulating pH; adding compound enzyme and stirring for enzymatic hydrolysis; centrifuging the obtained product; dissolving centrifugation objects in chloroform; standing the obtained product for crystallization; and dissolving coarse crystals in 90 percent methanol and 99 percent methanol for recrystallization. The process has the advantages of simple operation and short cycle.

The invention provides application of arctigenin in preparation of anti-infectious immunity drugs, which belongs to the field of medicine. Arctigenin is a natural monomer extracted from the traditional Chinese medicine burdock; it is discovered that arctigenin can substantially improve the clearance index and the phagocytic index of an immunocompromised patient and enhance non-specific immunity of the patient, exerts good treatment effects on infection caused by parasites, bacteria and viruses and especially has an excellent treatment effect on infectious diseases caused by Gram-positive bacteria. Arctigenin has the advantages of definite therapeutic effects, small toxic and side effects and wide medical application prospects when used for treatment of infectious diseases.

The invention discloses an application of heat-resisting beta-glucosidase mutants N223T, G224F and N223T / G224F to transforming arctiin into arctigenin. Amino acid sequences of the heat-resisting beta-glucosidase mutants N223T, G224F and N223T / G224F are indicated in SEQ: ID NO.1, ID NO.2 and ID NO.3. The arctiin is hydrolyzed to prepare the arctigenin by the aid of heat-resisting beta-glucosidase and the mutants thereof, and as compared with wild-type enzyme, the heat-resisting beta-glucosidase has the advantages of high transformation efficiency, fewer reaction by-products, high yield and purity, easiness in separation and purification, less chemical pollution and the like.

The invention discloses a solid tumor inhibiting medicine composition composed of arctigenin and a pyrimidine nucleotide synthetic inhibitor, wherein a weight ratio of the components is 1:0.001-1000, and preferably 1:0.01-100. Pharmacodynamic tests show that, the medicine composition provides substantial synergetic effects in the treatments of solid tumors, especially leukemia. The medicine composition provided by the invention has advantages of wide tumor inhibiting spectrum, small side effect, low treatment cost, and good prospect in clinical application.

The invention provides a 4-(4-(3, 4-dimethoxy benzene methyl)-2-carbonyl) tetrahydrofurfuryl-2-methoxyphenol 2-amino-3-methyl butyric acid ester hydrochloride for resisting tumors, and belongs to the field of research of anti-tumor drugs. Experimental results indicate that the 4-(4-(3, 4-dimethoxy benzene methyl)-2-carbonyl) tetrahydrofurfuryl-2-methoxyphenol 2-amino-3-methyl butyric acid ester hydrochloride has obvious inhibition effect on hepatocarcinoma 22 solid tumor-bearing mice, immune organs of organisms can be protected to some extent, and immune functions of the organisms are enhanced.

A process for preparing arctiin and arctigenin used to prepare meticines features that the liquid extract of arctium fruit passes through a polyamid column for separating and purifying.

Present Invention relates to a skin whitening cosmetic composition comprising arctiin, arctigenin or a mixture thereof as an active ingredient. The disclosed composition can control or inhibit the synthesis of melanin by acting on a melanin synthesis route of alpha-MSH secreted by UV, and thus show an excellent whitening effect compared to a conventional skin whitening cosmetic. Also, the composition has high formulation stability and low skin irritation.

The invention belongs to the technical field of drug synthesis, and particularly relates to novel arctigenin amino-acid ester derivatives, and a preparation method and application thereof. The structure of the arctigenin amino-acid ester derivatives is disclosed as General Formula I. The preparation method comprises the following steps: dissolving amino acids and arctigenin in a solvent, adding a condensing agent in an ice bath, stirring at room temperature or in a heating state for 1-24 hours, and tracking the reaction by thin-layer chromatography; and after the reaction finishes, evaporating to remove the solvent, and purifying by silica gel column chromatography to obtain the arctigenin amino-acid ester derivatives. The preparation method is reasonable in design and easy for synthesis. The synthesized compounds have a novel chemical structure; the in-vitro cell activity experiment proves that the most synthesized amino-acid ester derivatives have an obvious neural protection action; and the compounds I-2, I-5 and I-6 have higher activity than arctigenin, and thus, provide new therapeutic drugs for preventing and treating parkinsonism and other neurodegenerative diseases.

The invention provides a method for separating burdock oil, arctiin, arctigenin, lappaol E and lappaol H from burdock. The method for separating the burdock oil, arctiin, arctigenin, lappaol E and lappaol H from the burdock comprises the following steps: firstly degreasing burdock through CO2 supercritical fluid extraction, separating to obtain the burdock oil and degreased burdock powder, carrying out water-alcohol extraction and concentration on the degreased burdock powder to obtain extract, carrying out CH2Cl2 extraction on the extract, loading the extract onto a silica gel column to be subjected to chromatography, carrying out dichloromethane-methanol gradient elution, carrying out thin-layer chromatography, and purifying, so as to obtain the arctiin, lappaol E, arctigenin and lappaol H. The method provided by the invention has the advantages that multiple products can be separated by adopting one continuous route only, raw materials are fully utilized, resources are saved, a degreasing process does not pollute the environment, the obtained burdock oil has high nutritive value, and the arctiin, arctigenin, lappaol E and lappaol H are high in purity and can be independently or mixed with other substances to be applied to the medicinal and edible field as raw materials.

Provided are a conjugate of memantine and arctigenin, and a pharmaceutical composition comprising the conjugate. The conjugate can treat diseases associated with Aβ or Tau protein pathways, such as Alzheimer's disease or Parkinson's disease.

The invention discloses a pharmaceutical composition for treating diabetes and complication thereof, and particularly relates to a composition containing arctigenin and PioglitaZone or pharmaceutically acceptable salts thereof and to the purpose of the composition in preparing medicines for treating diabetes, diabetic complication and diseases related to diabetes.

The invention discloses a method for simultaneously measuring contents of arctiin, glycyrrhizic acid and pulegone in traditional Chinese medicine. The method comprises the steps that firstly, arctigenin, glycyrrhizinate and pulegone standard substances and a sample containing fructus arctii, licorice root and schizonepeta spikes (or schizonepeta) are taken respectively to be dissolved in a methanol aqueous solution, and a standard solution and a sample solution are prepared respectively; secondly, the standard solution and the sample solution which are identical in volume are taken to be injected into an efficient liquid chromatograph, then the peak area of the standard solution and the test solution is measured, and the contents of arctiin, glycyrrhizic acid and pulegone in the sample are obtained. The quick and accurate method is provided for measuring the contents of arctiin, glycyrrhizic acid and pulegone in traditional Chinese medicine containing fructus arctii, licorice root and schizonepeta spikes (or schizonepeta) and in extracts or preparations of the traditional Chinese medicine.