70 results about "Harmine" patented technology

The present invention relates to a harmine derivative compound and the application. The compound is produced through the structural modification of the 1st, 2nd, 3rd, 7th and 9th pint of the parent nuclear of the beta-carboline of the harmine; thus the novel harmine derivative compound is synthesized with the enhanced anti-tumor activity and no toxicity of the nervous system. Through the screening research of the vitro and vivo anti-tumor model, the harmine derivative compound is found to have the significant anti-tumor activity (the tumor-inhibition rate of the tumor-bearing mice model reaches as high as 63.5 percent), have no neurotoxicity, and have the prospects of clinical application. The preparation method of the compound is simple; the collection rate is high; and the compound is used for the drugs of treating various tumor diseases.

The present invention discloses a Rhizoma Corydalis Decumbentis total alkaloids extract, its preparation method, pharmaceutical composition containing same. The total alkaloids mainly comprise : macleyine, tetrahydropalmatine, bicucalline, palmatine hydrochloride, 'xiawuning' alkaloid, corydaline harmine, other alkaloid and extract. The preparation method is : using Rhizoma Corydalis Decumbentis as material, adding right amount of polar solvent for leaching, merging the leachate, carrying out large pore adsorption resin chromatography, eluting impurity with diluted acid and alkaline aqueous solution orderly, eluting using polar organic solvent, collecting elution liquor, eliminating impurity further by alumina column adsorption, Collecting after-column liquid, concentrating liquor to obtain the Rhizoma Corydalis Decumbentis total alkaloids extract. The present invention also discloses a pharmaceutical composition containing the total alkaloids extract and uses of the pharmaceutical composition in preparing tablet, capsule, soft capsule, suppository, granula, transdermal absorption agent, drop pills, oral disintegrating agent, slow release agent, freeze-drying powder injection etc.

The invention discloses application of a Harmine derivative to preparation of antibacterial medicines. The bacteria is selected from Acinetobacter, Bacillus, Campylobacter, Chlamydia, Chlamydia trachomatis, Clostridium, Citrobacter, Escherichia, enterohemorrhagic escherichia coli, enteric bacteria, Enterococcus, Francisella, Haemophilus, helicobacter, Klebsiella Bacillus, Lester monocytogenes, Moraxella, Mycobacterium, Neisseria, proteus, Pseudomonas, Salmonella, shewanella oneidensis, Shigella, Stenotrophomonas, Staphylococcus, Streptococcus and Yersinia.

The present invention provides a method of reducing body weight in a subject in need thereof, by administering to the subject a therapeutically effective amount of a compound of Formula I. The present invention also provides methods for the treatment of obesity and disorders related to obesity and higher than recommended percentage body fat, such as type II diabetes.

The invention discloses a fatty acid-trimethyl chitosan polymer modified by a lactobionic acid, a preparation method and an application. The fatty acid-trimethyl chitosan polymer modified by the lactobionic acid is an active targeting nano micelle carrier material. A trimethyl chitosan with a good water-solubility is used as a carrier material, the hydrophobic modification is performed by a fatty acid, and then the surface modification is performed by the lactobionic acid to obtain a polymer micelle with the lactobionic acid which mediates tumor tissue target. Harmine is used as a model drug to prepare a drug-loaded nano-micelle in a rubbing and self-assembly mode. A test confirms that the drug loading capacity and encapsulated ratio of the drug-loaded nano-micelle are high, the slow-release property is achieved, cells are effectively taken in through a lactobionic acid receptor pathway, and distribution of drugs on the tumor tissue is increased, so that the curative effect is improved, the toxic and side effect is reduced, and targeted therapy is achieved. The fatty acid-trimethyl chitosan polymer modified by the lactobionic acid, the preparation method and the application provide an ideal novel drug carrier and a preparation form for antitumor drugs with slightly solubility.

This invention relates to compounds of general formula (I), wherein R1, R2, R3, R4 and R5 are as defined in the specification; intermediates used in their preparation, preparation processes and use thereof. The present invention produces new harmine derivatives with enhanced antitumour activity and lower nervous system toxicity by structurally modification of the parent structure of β-carboline of harmines at position 1, 2, 3, 7 and 9. The compounds of the present invention can be prepared easily with high yield. They can be used in manufacture of a variety of antitumour medicines and medicines used in treatment of tumour diseases in combination of light or radiation therapy.

The present invention provides a method of promoting bone growth in a subject in need thereof, by administering to the subject a therapeutically effective amount of a compound of Formula I. The present invention also provides methods for the treatment of renal disease and cancer.

Human therapeutic treatment compositions comprise at least two of a curcumin component, a harmine component, and an isovanillin component, and preferably all three in combination. The agents are effective for the treatment of human conditions, especially human cancers.

Human therapeutic treatment compositions comprise at least two of a curcumin component, a harmine component, and an isovanillin component, and preferably all three in combination. The agents are effective for the treatment of human conditions, especially human cancers.

The present invention discloses a harmine compound, wherein the chemical structure formula is represented by a formula (I), R1 is selected from phenyl, p-nitrophenyl, p-methoxyphenyl, 3,4,5-trimethoxyphenyl, p-trifluoromethylphenyl and p-chlorophenyl, R2 is selected from ethyl, isopropyl, 2-pyridyl and 2-chlorophenyl, and R3 is selected from hydrogen and ethyl. According to the present invention, the compound provides good inhibition effects on multiple pathogenic bacteria, especially provides good inhibition and prevention and control effects on peronophthora litchi chen, has advantages of small molecular weight, simple structure, easy synthesis and the like, can effectively inhibit hypha growth, sporangium production and sporangium germination of peronophthora litchi chen, has good potential in prevention and control of peronophthora litchi chen disease, and is expected to become a new pesticide fungicide, such that the small molecule compound of the present invention can be used as the new pesticide for prevention and control of the peronophthora litchi chen disease so as to be developed and can provide the new way and means for prevention and control of the peronophthora litchi chen disease.

The present disclosure relates to a pharmaceutical composition, a health functional food composition, and a method for preventing or treating a brain disease or diabetes. The pharmaceutical composition, health functional food composition, and method includes at least one active ingredient that is chlorhexidine, thioguanosine, mebendazole, fenbendazole, colchicine, farnesol, trimethobenzamide hydrochloride, disulfuram, azathioprine, mebeverine hydrochloride, zaprinast, tosufloxacin hydrochloride, efavirenz, thiostrepton, probenecid, entacapone, harmine hydrochloride, flunisolide, thimerosal, hexestrol, sulfaquinoxaline sodium salt, monensin sodium salt, raloxifene hydrochloride, 2-chloropyrazine, or topotecan.

Human therapeutic treatment compositions comprise at least two of a curcumin component, a harmine component, and an isovanillin component, and preferably all three in combination. The agents are effective for the treatment of human conditions, especially human cancers.

The invention discloses a method for analyzing an active component in harmel grass. The method comprises the following steps of: constructing a finger print, analyzing the active component in a qualitative manner through the finger print, detecting the content of the active component through an HPLC (high performance liquid chromatography) method, wherein the finger print comprises a TLC (thin-layer chromatography) finger print and / or HPLC finger print. According to the invention, the constructed finger print has excellent reproducibility and specificity, and has good stability, precision and application sample recovery ratio on the content detection method of the active component, can realize qualitative and quantitative analysis of various active components such as vasicine, peganine, harmine, deacetylation harmel glycoside and harmel glycoside in the harmel grass, can fully evaluate the quality of the harmel grass, and can provide scientific reference for medicinal value of research and development on harmel grass; and the analyzing method provided by the invention has the advantages of simplicity in operation, velocity, economy, strong operability and the like, and can carry out popularization and application.

The invention discloses a method for extracting peganum harmala alkaloid under microwave assistance. The method comprises the following steps: drying a peganum harmala plant to a constant weight, using ethanol with volume concentration of 60-95% as a solvent, extracting for 8-12 minutes under microwave heating assistance at a solid-liquid ratio of 10-50 ml / g and an extracting temperature of 60-100 DEG C, filtering to obtain an extracting solution, concentrating the extracting solution until no alcohol smell exists, coating the extracting solution on a preparative high performance liquid chromatography C18 reverse phase silica gel column, using 0.1 mol / L of ammonium acetate buffer salt solution and acetonitrile with a volume ratio of 70:30 to 96:4 as an elution phase, separating and preparing at a flow speed of 1.0 mL / min and within a temperature range of 20-40 DEG C, online monitoring via ultraviolet 280 nm, collecting eluant with a specific absorption peak, and volatilizing to obtain the following three alkaloids: vasicine, banisterine and harmine. The method is simple, convenient, feasible and controllable, and the yield of the alkaloid of the method is higher than that of the existing extraction methods.

The invention relates to the technical field of application of a harmine derivative, and particularly discloses the application of a harmine derivative to preparation of drugs for treating cystic echinococcosis for the first time. In-vitro pharmacodynamic experiment data prove that the harmine derivative can reduce the survival rate of echinococcosis granulosis cyst remarkably; In-vivo pharmacodynamic experiment data prove that the efficacy of the harmine derivative and the efficacy of albendazole are similar in treating cystic echinococcosis; in-vitro-and-vivo safety evaluation experiment data prove that the toxicity of the harmine derivative is lower than that of a harmine monomer with cystic echinococcosis resisting activity. Therefore, a new approach is provided for treating cystic echinococcosis.

The invention discloses an anti-CA (candida albicans) product combining harmine hydrochloride and fluconazole and an application of the product and belongs to the technical field of medicines. The combined antifungal function of fluconazole and harmine hydrochloride on drug-resistant CA are researched with multiple methods. The effective concentration of fluconazole to harmine hydrochloride is 1:32 (mu g / mL, for CA3) or 1:16 (mu g / mL, for CA2) when fluconazole and harmine hydrochloride are combined to be applied, the minimum inhibitory concentration is 8 mu g / mL and 0.25 mu g / mL (for CA3) or 0.5 mu g / mL (for CA4). When harmine hydrochloride and fluconazole are combined, the antibacterial activity of fluconazole for drug-resistant CA can be enhanced, the coordinated antifungal action can be generated, the drug resistance of drug-resistant CA to fluconazole can be reversed, and a research direction is provided for development of new drugs and new application of old drugs.

The invention relates to the field of tumor target treatment, and in particular relates to a harmine derivative anti-tumor prodrug with target characteristic. The invention discloses a junctional complex for structuring 2-deoxidation-D-deoxyglucose (II) and the harmine derivative anti-tumor drug which have tumor targets. Pharmacodynamic tests prove that the compound (II) is targeted to tumors, the water solubility of a tumor drug is improved, so that an anti-tumor effect is increased, and neurotoxicity is reduced.

In one aspect, the invention provides compounds of Formula I, and salts, hydrates and isomers thereof. In another aspect, the invention provides a method of promoting bone formation in a subject in need thereof by administering to the subject a therapeutically effective amount of a compound of Formula I, Formula II, or Formula III. The present invention also provides orthopedic and periodontal devices, as well as methods for the treatment of renal disease and cancer, using a compound of Formula I, Formula II, or Formula III.

The invention relates to determination of alkaloid content in decumbent corydalis tuber total alkaloid extractive. The determination method comprises the following steps: (1) preparing a decumbent corydalis tuber total alkaloid extractive solution; (2) preparing a standard solution; (3) respectively sucking the extractive solution and the standard solution of an equal amount, and carrying out UFLC determination to obtain a UFLC chromatogram; and (4) analyzing chromatographic peaks of protopine, bicuculline, xiawuning alkaloid, corydaline harmine, tetrahydropalmatine and palmatine in the chromatogram, and calculating contents thereof by an external standard method. Besides, the invention also provides a method for establishing a UFLC finger print of decumbent corydalis tuber total alkaloidextractive. The determination method can quickly and accurately determine contents of six main alkaloids in decumbent corydalis tuber total alkaloid extractive, and the UFLC finger print of decumbentcorydalis tuber total alkaloid extractive can be used for the overall control on substance groups in decumbent corydalis tuber total alkaloid extractive, thereby controlling the quality of extractivefrom the macro analysis perspective.

Human therapeutic treatment compositions comprise at least two of a curcumin component, a harmine component, and an isovanillin component, and preferably all three in combination. The agents are effective for the treatment of human conditions, especially human cancers.

The invention discloses a method for extracting peganum harmala alkaloid under microwave assistance. The method comprises the following steps: drying a peganum harmala plant to a constant weight, using ethanol with volume concentration of 60-95% as a solvent, extracting for 8-12 minutes under microwave heating assistance at a solid-liquid ratio of 10-50 ml / g and an extracting temperature of 60-100 DEG C, filtering to obtain an extracting solution, concentrating the extracting solution until no alcohol smell exists, coating the extracting solution on a preparative high performance liquid chromatography C18 reverse phase silica gel column, using 0.1 mol / L of ammonium acetate buffer salt solution and acetonitrile with a volume ratio of 70:30 to 96:4 as an elution phase, separating and preparing at a flow speed of 1.0 mL / min and within a temperature range of 20-40 DEG C, online monitoring via ultraviolet 280 nm, collecting eluant with a specific absorption peak, and volatilizing to obtain the following three alkaloids: vasicine, banisterine and harmine. The method is simple, convenient, feasible and controllable, and the yield of the alkaloid of the method is higher than that of the existing extraction methods.

The invention relates to the technical field of medicines, in particular to application of a natural medicine in preparation of antibacterial medicines. According to the invention, various natural medicines can be used for preparing antibacterial medicines; mangiferin has a good inhibition effect on the growth of acinetobacter baumannii; the methyl caffeate has a good inhibition effect on acinetobacter baumannii; the invention also finds that harmine can be used as a synergist of meropenem to enhance the antibacterial effect of meropenem on klebsiella pneumoniae; single use of harmine or meropenem cannot inhibit the growth of klebsiella pneumonia, but when 128 [mu] g / mL harmine and 4 [mu] g / mL meropenem are combined for use, the growth of klebsiella pneumonia can be significantly inhibited, and the growth rate can be reduced to 5% or below.

The invention relates to a preparation method of dehydro-harmine, which comprises the steps of smashing harmel seeds which are taken as a material, adding appropriate ammonia water, mixing uniformly, carrying out ammoniation for 10-20 hours, adding a 70-80% carbinol solution with 3-5 times as quantity as that of the material for soaking for 2-3 times, filtering soaking liquid, adding a chloroform solution, collecting a chloroform layer, recycling the chloroform, carrying out separation preparation on solid by a petroleum ether-ethyl acetate-carbinol-hydrosolvent system through using a high-speed counter current chromatograph, collecting dehydro-harmine fluid, recycling reagents, and drying under a low-temperature vacuum condition, so that pure dehydro-harmine is obtained. The method is applicable to the preparation of the dehydro-harmine with high purify.

Human therapeutic treatment compositions comprise at least two of a curcumin component, a harmine component, and an isovanillin component, and preferably all three in combination. The agents are effective for the treatment of human conditions, especially human cancers.

A derivative of β-carboline alkaloid harmine, 10,12-diheptanoyl-11-hydroxy-3-methyl-β-carboline, prepared by a Friedel-Crafts acylation of harmine is reported as a novel potent antitubercular drug.

Human therapeutic treatment compositions comprise at least two of a curcumin component, a harmine component, and an isovanillin component, and preferably all three in combination. The agents are effective for the treatment of human conditions, especially human cancers.

The invention discloses a method for analyzing an active component in harmel grass. The method comprises the following steps of: constructing a finger print, analyzing the active component in a qualitative manner through the finger print, detecting the content of the active component through an HPLC (high performance liquid chromatography) method, wherein the finger print comprises a TLC (thin-layer chromatography) finger print and / or HPLC finger print. According to the invention, the constructed finger print has excellent reproducibility and specificity, and has good stability, precision and application sample recovery ratio on the content detection method of the active component, can realize qualitative and quantitative analysis of various active components such as vasicine, peganine, harmine, deacetylation harmel glycoside and harmel glycoside in the harmel grass, can fully evaluate the quality of the harmel grass, and can provide scientific reference for medicinal value of research and development on harmel grass; and the analyzing method provided by the invention has the advantages of simplicity in operation, velocity, economy, strong operability and the like, and can carry out popularization and application.

Human therapeutic treatment compositions comprise at least two of a curcumin component, a harmine component, and an isovanillin component, and preferably all three in combination. The agents are effective for the treatment of human conditions, especially human cancers.

Human therapeutic treatment compositions comprise at least two of a curcumin component, a harmine component, and an isovanillin component, and preferably all three in combination. The agents are effective for the treatment of human conditions, especially human cancers.