132 results about "Evodiamine" patented technology

The invention relates to the technical field of medicines. The content of DNA topoisomerase I (TopoI) in tumor cells is substantially higher the content of the TopoI in normal tissues, and an inhibitor of the TopoI is listed as one of six types of antitumor drugs which are primarily researched by an American NCI (National Cancer Institute). The invention aims to obtain evodiamine derivatives withstrong antitumor activities by modifying the structure of evodiamine. The evodiamine structure of the evodiamine compounds is represented by general formula (I) in the specification. The invention also provides an application of the evodiamine compounds and medicinal salts thereof in preparing topoisomerase inhibitors and antitumor drugs.

The invention relates to the field of natural medicines and medicinal chemistry and particularly relates to derivatives with modified 13-N of evodiamine. The invention discloses a preparation method of the 13-N furazan NO donor substituted evodiamine derivatives and evaluation of the anti-tumor activity. The structure of the compounds is shown in the specification, wherein R1 and R2 are (CH2)n or (CH2)n1O(CH2)n2, and n, n1 and n2 are integers between 1 and 8.

The invention discloses substituted-evodiamine anti-tumor and antifungal compounds and a preparation method thereof. The compounds have a general structural formula (I), wherein R represents: (1) benzyl or substituted benzyl; (2) benzoyl or substituted benzoyl; (3) linear or branched alkyl having 2 to 6 carbon atoms; and (4) an ester group. The substituted-evodiamine compounds of the invention have good anti-tumor activities for various tumor cells, provide a new way for deep research and development of new anti-tumor medicaments and can be used for preparing new anti-tumor medicaments.

The invention relates to an action of ferulic acid on enhancing the drug effect of some medicaments and a purpose thereof, wherein the medicaments mainly comprise alkaloid medicaments including matrine, kushenin, sophocarpine, hyoscyamine, narceine, hanfangchin A, jamaicin, morphine, codeine, evodiamine, strychnine, catharanthine, vincristine, taxol, verticine, peimine, peiminine, ephedrine, pseudoephedrine, wilfordine, triptolide, tripdiolide and the like, and flavonoid medicaments including puerarin, ginsenoside, ginsengenin, mangiferin, scutelloside, alkannin, meletin, rutin, hesperidin, daidzin, soybean isoflavone, daidzein, carthamin, catechin and the like. The ferulic acid and the medicaments can form a compound or a medicament compound, or the ferulic acid and the medicaments can generate a chemical reaction (including salification, esterification, amidation, ketonization, etherification and the like), and / or the ferulic acid and the medicaments can generate a synergistic effect and an additive effect.

The invention relates to a high performance liquid chromatography-mass spectrometry (HPLC-MS) quantitative method for measuring 10 components of a fructus evodiae formula granule. The method is characterized in that a HPLC-MS technology is used; acetonitrile is taken as the A phase; acetic acid (0.12%)-ammonium acetate (1 mmol / L) is taken as the B phase; gradient elution with four scale transformations is performed; the flowing speed is 0.8 mL / min; the column temperature is 40 DEG C; in a multiple reaction monitoring (MRM) mode, positive ions and negative ions are monitored at the same time, the ion source is an ESI source, the atomized gas (GS1) is N2, the auxiliary gas (GS2) is N2; nitrogen gas is used during the whole process; the collision gas pressure is medium; the resolutions of Q1 and Q3 are both UNIT; the method can detect 10 components in the fructus evodiae formula granule, namely chlorogenic acid, caffeic acid, rutin, hyperin, hesperidin, dehydroevodiamine, limonin, evodiamine, rutaecarpin, and evocarpine; 10 components can be all detected in 22 minutes, and the method is rapid and accurate and is not disturbed.

The invention relates to an adjuvant for improving the effectiveness of a dendritic cell vaccine, which is a traditional Chinese medicine monomer, namely evodiamine.

The invention discloses a method for synthesizing evodiamine by a carbonylation reaction three-step method. The method comprises that N, N-dimethylaniline as a reaction material undergoes an oxidativecarbonylation reaction to produce N-methylisatoic anhydride, the N-methylisatoic anhydride undergoes an aminolysis reaction to produce N-(2-indolylethyl)-2-(methylamino)benzamide and the N-(2-indolylethyl)-2-(methylamino)benzamide undergoes a cyclization reaction to produce an evodiamine compound. The method is a novel synthesis method, utilizes simple and easily available reaction raw materials,has simple synthesis processes, is carried out under mild reaction conditions, is easy to operate, satisfies the development requirements of green chemistry, and successfully synthesizes the evodiamine.

The invention relates to a natural pharmaceutical composition, a preparation method thereof and an application thereof in preparing an attenuating synergistic medicament in radiotherapy and chemotherapy of cancer. The natural pharmaceutical composition is composed of concentrated extract of decoctions of dried ginger and evodia rutaecarpa, gingerol, evodia rutaecarpa extract and evodiamine in proportion of (1-4):(3-7):(2-9):(2-3). The composition provided by the invention has good curative effects on vomit and the like caused by the side effects of radiotherapy and chemotherapy of cancer, and also plays an effect on inhibiting tumor.

The present invention provides a drug for treating hyperuricemia and gout, ie., evodiamine dispersion tablets. The evodiamine dispersion tablets are the preparation prepared from the following raw materials and additives, by weight, 7-13 parts of evodiamine, 30-50 parts of a solid dispersion water-soluble carrier material, 70-90 parts of a filler, and 8-14 parts of a disintegrating agent. The present invention further provides a preparation method and uses of the dispersion tablets. The evodiamine dispersion tablets of the present invention have characteristics of short disintegration time and high dispersion uniformity. According to the present invention, the dissolution of the insoluble drug evodiamine in the solid preparation can be significantly improved, the absorption of the evodiamine in the human body is prompted, the bioavailability of the drug is increased, and new selections are provided for clinical medication for treatments of hyperuricemia and gout.

The invention discloses an evodiamine derivative. The chemical structural formula is as follows. At cellular level, such a compound has activity equivalent to and even higher than activity of known antitumor active compounds, such as evodiamine. The evodiamine derivative disclosed by the invention has the advantages of mild synthesis condition, insensitivity to water, oxygen, and the like, easilyacquired and low-cost reaction raw materials, simple operation, easiness in separating and purifying products, high yield, easiness in industrial production, and the like. An MTT process is adopted for determining anti-proliferative effect of the evodiamine derivative prepared according to the invention to tumor cell lines and normal cell lines. Such a compound has a novel structure and obvious antitumor activity.

The invention belongs to the field of pharmaceutic preparations, and relates to a formula and a preparation method of an evodiamine nanoemulsion. The evodiamine nanoemulsion prepared by the invention can be used for improving the solubility of medicines and enhancing the bioavailability and the pharmacological activity.

Compositions and methods are provided for reversing and / or inhibiting inflammation, e.g., by inhibiting prostaglandin and / or COX-2 production, using one or more indolequinazoline alkaloids, preferably in combination with butylated hydroxytoluene. The preferred indolequinazoline alkaloids are rutaecarpine, evodiamine, and dehydroevodiamine, which are naturally found in unpurified form in the traditional Chinese medicine Wu Chu Yu made from the fruit of the herb, Evodia rutaecarpa.

The invention discloses application of evodiamine and rutaecarpine in preparation of a medicine for enhancing the activation of NLRP3 inflammasomes. The evodiamine and the rutaecarpine can generate active Caspase-1 by enhancing activiation of macrophage inflammasomes so as to release manure inflammatory mediators such as IL-1beta and promote pyroptosis of sensitized macrophages. The activity of the evodiamine and the rutaecarpine can be used for enhancing the inflammatory response intensity of a human body and treating related diseases of insufficient activation of inflammasome including pulmonary tuberculosis and oral tuberculosis caused by intracellular infection of mycobacterium tuberculosis, diseases caused by listeria monocytogenes, related diseases caused by other intracellular infection bacteria, related diseases caused by pathogenic fungal infection, furunculosis, dental-root periapical diseases, chronic gastritis, chronic enteritis, dysentery and diarrhea and the like.

The invention discloses an organic chemical synthesis method, in particular a method for chemically synthesizing evodiamine. Indole acetonitrile is taken as a raw material, and the method comprises the following steps of: performing catalytic hydrogenation on palladium carbon to prepare tryptamine; mixing with ethyl formate to form solution for a formylation reaction, and dissolving the reactants in solution of dichloromethane; adding trifluoroacetic acid for cyclization, and preparing another intermediate in a reflux state from N-methylanthranilic acid and excessive ethyl chloroformate; and finally, subjecting two intermediates to condensation reaction in a non-polar solvent system. The method for chemically synthesizing the evodiamine has the advantages of rich raw material source, low price of the raw material, capacities of improving the yield and fulfilling the aim of reducing the production cost by optimizing reaction conditions, environmental friendliness and suitability for large-scale industrial production. The product can be widely applied to pharmaceutical industry.

The invention relates to the fields of natural drugs and medicinal chemistry, particularly a preparation method of evodiamine N-13 combined nitrogen mustard derivatives and application of the evodiamine N-13 combined nitrogen mustard derivatives in preparing antineoplastic drugs. The structure of the evodiamine combined nitrogen mustard derivatives and pharmaceutically acceptable salts thereof isdisclosed as a general formula I, wherein n, m and p are as described in the claims and specification. The evodiamine derivatives provided by the invention have better antineoplastic effects, and canbe used for further preparing antineoplastic drugs.

The invention relates to a method for separating evodiamine and rutaecarpin from fructus evodiae. The method provided by the invention takes fructus evodiae as a raw material. The method for preparingthe evodiamine and rutaecarpin comprises the following steps: taking the raw material, adding a certain amount of solvent, extracting, and recycling the solvent, so that fructus evodiae extract is obtained; degreasing the extract with a low polarity solvent and a mixture, and then washing with diluted hydrochloric acid or sulfuric acid, nitric acid or phosphoric acid solution; taking residual solids, namely obtaining the residual solids by filtering or centrifuging; carrying out adjustment reaction on the residual solids, and filtering or centrifuging; dissolving the solids with dichloromethane, chloroform, acetone or ethyl acetate again, filtering or centrifuging, obtaining two parts, namely solids and a liquid, taking the solid and liquid parts, reacting respectively, obtaining a evodiamine crude product and a rutaecarpin crude product, and then carrying out crystallization and recrystallization so as to finally obtain high-purity evodiamine and rutaecarpin crystals.

The invention discloses a pharmaceutical composition for treating hyperlipidemia as well as a preparation method and applications. The pharmaceutical composition comprises the following ingredients in parts by weight: 1-10 parts of evodiamine, and 5-15 parts of berberine. The pharmaceutical composition is prepared by combining active ingredients of natural pharmaceutical raw materials or the extract of active ingredients of pharmaceutical raw materials, is simple in constituents, is affirmed for curative effect, is not required for being decocted for administration, is convenient to carry and take after being prepared into tablets, capsules, pills, granules and oral liquid. Compared with the traditional natural pharmaceutical formulation, the composition has the advantages of less impurity content, high purity, clear action mechanism and stable character, is capable of better controlling the product quality in industrialization, and the like.

The invention relates to 10-hydroxyevodiamine type anti-tumor compounds, a preparation method of the 10-hydroxyevodiamine type anti-tumor compounds and an application of the 10-hydroxyevodiamine type anti-tumor compounds in preparing an anti-tumor drug. The 10-hydroxyevodiamine type anti-tumor compounds have a structure shown in the formula I. The compounds are newly found topoisomerase inhibitors with brand new structures, most of compounds have broad-spectrum antitumor activity, and the IC50 (half maximal inhibitory concentration) of a part of derivatives to tested three tumors is smaller than 0.001 mu g / mL and is superior to that of compounds (10-hydroxyevodiamine) with similar structures and best activity in the prior art.

The invention belongs to the technical field of medicine, and provides a multi-targeted micromolecular anti-cancer drug based on topoisomerase 1 (Top1), topoisomerase 2 (Top2) and histone deacetylase(HDAC) and a preparation method of the multi-targeted micromolecular anti-cancer drug. The general molecular formulas of the compound are shown in the formulas I and II. Through pharmacological experiments, it is shown that the compound has high inhibitory activity to the topoisomerase 1, the topoisomerase 2 and the histone deacetylase, and has high in-vitro anti-tumor activity and excellent in-vivo anti-tumor effects. The invention further provides a preparation method of the derivative and application of the derivative in preparing a topoisomerase inhibitor, a histone deacetylase inhibitor and the anti-tumor drug.

The invention relates to a processing method and detection method for integrating processing and preparing of evodia rutaecarpa in producing areas. The method directly dries in the shade, dries in thesun or dries by baking the fresh medicinal material of the evodia rutaecarpa, the processing method combines the initial processing in the producing areas of the evodia rutaecarpa and the processingof decoction pieces, and the fresh evodia rutaecarpa is directly processed into the evodia rutaecarpa decoction pieces. On the basis of the existing research on the evodia rutaecarpa, a evodia rutaecarpa one-test multiple evaluation method is established, the content of dehydroevodiamine, limonin, evodiamine, rutaecarpine and rutaecarpine in the evodia rutaecarpa is taken as indexes, a fingerprintspectrum and pharmacodynamics experiments are combined to integrally and systematically research the integrated technology of processing and preparing the evodia rutaecarpa in the producing areas, comparison research on decoction pieces processed by a traditional method is carried out, a scientific basis is provided for the standardization of the integrated technology of processing and preparingthe evodia rutaecarpa in the producing areas and a quality detection method of the evodia rutaecarpa, and the quality of the decoction pieces of the evodia rutaecarpa medicinal material and the safetyand the effectiveness of clinical application are improved.

The invention relates to the compounds isolated from Evodia rutaecarpa (Juss.), in that has been demonstrated to inhibit topoisomerase I. Evodiamine, an alkaloidal compound is reported the topoisomerase I inhibitory activity. The effect of evodiamine acts by stabilizing the covalent complex between topoisomerase I and DNA, which results in a blockade of DNA replication and transcription.

The invention discloses application of dendritic macromolecular polyamide-amine in evodiamine. The dendritic macromolecular polyamide-amine has the effect of promoting absorption of insoluble traditional Chinese medicinal ingredients and is G4-generation PAMAM-co-OEG or G4-generation PAMAM-NH2, and the usage concentrations of both of them W / V is 0.1%. The dendritic macromolecular polyamide-amine has the advantages that the toxicity and absorption promoting effect of PAMAM Dendrimers are systematically researched at different levels of animals, cells and the like layer upon layer, and it is proved that the PAMAM Dendrimers can safely and effectively promote absorption of the insoluble ingredients. Therefore, the dendritic macromolecular polyamide-amine can serve an absorption promoter to be used in the fields of foods and drugs and is wide in application, high in efficiency and low in toxicity. Especially in the field of medicine, the PAMAM Dendrimers can improve the bioavailability of drugs, novel pharmaceutical excipients can be further developed, and thus the current utilization situation of traditional Chinese medicine is improved.

The invention provides application of an evodiamine derivative in preparation of a medicine for treating superficial fungal infection. The evodiamine derivative disclosed by the invention is prepared by taking a methyl anthranilate compound and tryptamine as initial raw materials through amine-ester exchange and a one-step ring closing reaction catalyzed by Lewis acid. The evodiamine derivative disclosed by the invention can show good antibacterial activity on three fungi, namely trichophyton rubrum, trichophyton mentagrophytes and candida albicans. Moreover, cell walls, cell membranes and organelles of fungal spores are destroyed to a certain extent, the hydrophobicity of fungal biomembranes can be influenced to a certain extent, phenomena of dark red erythema, skin hardening and generation of a large amount of scurf caused by errhysis spots of skin subjected to dermabrasion treatment can be obviously relieved, and phenomena of thickened epidermal layer of skin tissue, small-area epidermal layer necrosis, cuticle small-area parakeratosis and the like are avoided. The evodiamine derivative has low toxicity and low drug resistance and can be applied to preparation of drugs for treating the superficial fungal infection.

The invention belongs to the field of medicaments, and provides the application of evodiamine in preparation of medicaments for treating alzheimer disease. The evodiamine can improve main symptoms of alzheimer disease, namely loss of learning and memory capability. The delay of the progression of alzheimer disease is mainly realized by: 1, inhibiting excessive activation of microglia in brain tissues, and lowering over-expression of cytokines IL-1, IL-6 and TNF-alpha; and 2, lowering expression of cycloxygenase-2, and inhibiting an inflammatory reaction of the central nervous system. Researches of curative effect and molecular mechanism on the evodiamine treating alzheimer disease prove that the evodiamine has quite good treating effect and has huge potential of becoming a clinical treatment medicament.

The invention relates to an extract containing evodiamine (EVO) and rutaecarpin (RUT) and a preparation method thereof. The invention further relates to a medical application of the extract. The ratio of the EVO to the RUT in the extract containing EVO and RUT provided by the invention is (1-10):(1-5). Compared with a chemically-synthesized monomer, the extract in a specific ratio has the advantages: the absorption of EVO and RUT can be improved remarkably, and the bioavailability of EVO and RUT is increased; and the extract is purity-dependent. The extract disclosed by the invention can be used for alleviating pain.

The invention provides an evodiamine derivative. The evodiamine derivative is prepared by taking an anthranilic acid compound and tryptamine as initial raw materials through a condensation reaction and a one-step ring closing reaction catalyzed by lewis acid. The evodiamine derivative prepared by the preparation method disclosed by the invention has dual inhibition effects on topoisomerase I / II, so a broad-spectrum anti-tumor effect is achieved. The derivative can induce apoptosis of cancer cells and retard proceeding to a G2 / M period in a concentration-dependent manner, and has an effect of inhibiting invasion and migration of cancer cells in vitro. The derivative has a good tumor growth inhibition effect in a nude mouse transplantation tumor model, has no obvious toxicity at a cell level and an animal level, has good safety and can be applied to preparation of anti-tumor drugs.

The invention relates to the field of natural medicine and medicinal chemistry, in particular to a derivative for modifying an N-13 locus of evodiamine, especially the evodiamine derivative substituted by an N-13-locus ADT-OH type H2S donor and a preparation method thereof and application in preparation of medicine resistant to tumors. The evodiamine derivative substituted by the ADT-OH type H2S donor and a pharmaceutically acceptable salt structure of the derivative are shown as the formula I, wherein n is shown in the claims and the description. The formula I is shown in the description.

Composition for treating the asthenic cold type migraine comprises ingredients as follows: 3.0-4.0 parts of ginsenoside Rb1 by weight and 1.0 part of evodiamine (Ev) by weight; preferably, 3.0-4.0 parts of the ginsenoside Rb1 by weight, 1.0 part of the Ev by weight, 0.15-0.60 part of rutaevine (Rv) by weight, 0.50-2.0 parts of limonin(Li) by weight; more preferably, 3.0-4.0 parts of the ginsenoside Rb1 by weight, 1.0 part of the Ev by weight, 0.15-0.60 part of Rv by weight, 0.50-2.0 parts of Li by weight, 0.60-4.0 parts of ginsenoside Rg1 by weight and 0.02-0.25 part of rutaecarpin (Ru). Essential ingredients, namely, the Rb1 and the Ev, which are effective in treating the asthenic cold type migraine, are provided, and main active ingredients, namely, the Rg1, the Rv, the Li and the Ru, are matched and combined on the basis, and the composition which has the optimum curative effect on the asthenic cold type migraine is determined.

The invention discloses a temperature / pH responsive double-drug-loaded composite nano particle and a preparation method and use thereof. The temperature / pH responsive double-drug-loaded composite nanoparticle is obtained by sequentially preparing BBR@MSNp (NIPAM-co-MA), an LB film and LEBM. The preparation method comprises the steps that berberine (BBR) is loaded onto a specific-temperature and pH double-response functional nano particle, and then the nano particle is creatively coated with evodiamine (EVO), and the temperature / pH responsive double-drug-loaded composite nano particle is prepared. In vitro and in vivo experiments show that a targeted drug delivery system can accurately locate to a tumor site and achieve effective drug release. The EVO and BBR are subjected to combined administration through a temperature / pH responsive double-drug-loaded nano drug delivery system for the treatment of cancer, especially, a synergistic effect on the treatment of liver cancer, cervical cancer and breast cancer is achieved, and the curative effect is remarkable.