30 results about "Nitidine chloride" patented technology

The invention discloses a method for separating purified nitidine chloride by using a cation exchange resin, which comprises the following steps of: (1) mixing crushed shinyleaf pricklyash root decoction pieces and a solvent for backflow extraction; and (2) regulating the pH value of sample liquid by using acid-base after the extract is filtered, performing the dynamic or static adsorption on the extract by using the cation exchange resin which has a special adsorbability for the nitidine chloride, performing desorption by using an organic acid or mixed liquid of an inorganic acid and an organic solvent, and centrifuging the stripping liquid to obtain the deposit of the nitidine chloride, wherein the resin after the desorption can be reused after being washed by a desorbing agent. The method can rapidly and efficiently separating the nitidine chloride and effectively reduce the cost and environmental pollution; and the transfer rate of the nitidine chloride is over 85 percent; and the crystalline purity is greater than 90 percent.

The invention relates to a 2,3-dioxyethyl-5-methyl-8,9-dimethoxy benzophenanthridine derivative disclosed as Formula I, a synthesis method and application thereof in preparing medicines for inhibiting tumor cell activity. The 50% inhibition concentrations IC50 of the 2,3-dioxyethyl-5-methyl-8,9-dimethoxy benzophenanthridine-hydrochloride and hydrobromide for four cancer cell strains of stomach cancer (MGC-803), liver cancer (BEL7402), human nasopharyngeal carcinoma (CNE) and human lung adenocarcinoma (A549) are respectively lower than those of nitidine chloride, and are much lower than those of 5-FU (control drug).

The invention discloses a method for preparing target antineoplastic drug chlorinated nitidine compound, products thereof and an injection containing the products. The method for preparing the target antineoplastic drug chlorinated nitidine compound comprises the steps of pre-treating the chlorinated nitidine to acquire carboxylic acid-modified chlorinated nitidine, then using amphiphilic polymers to implement non-covalent functionalized modification on the outer wall of a single-wall carbon nano tube that is cut to be 20-500 nm long, and coupling the carboxylic acid-modified chlorinated nitidine with the single-wall carbon nano tube after the non-covalent functionalized modification by means of esterification and amidation reactions to acquire the compound. The preparation method of the compound is simple, the solubility of the resulting products can reach 5.0mg/mL, and the antineoplastic target is strong, thus favorably settling the problems of low solubility and strong toxicity of the chlorinated nitidine; in addition the invention can be applied clinically as a substitute for the chlorinated nitidine and provides a new water-soluble compound for the clinical trial of the chlorinated nitidine.

The invention provides application of nitidine chloride to the preparation of a medicament for resisting autoimmunity disease and graft versus host disease. An experiment shows that the nitidine chloride can inhibit the proliferation of human dendritic cells in vitro, inhibit the human dendritic cells from promoting the proliferation reaction of allogeneic T cells and strengthen the capacity of secreting interleukin 10 of the human dendritic cells. Meanwhile, in an experimental autoimmunity disease cerebrospinal meningitis model, when used in vivo, the nitidine chloride can reduce the average clinical score of a mouse and inhibit the spinal marrow infiltration degree of monocytes and can obviously improve the secretion level of the interleukin 10 in the blood serum of the mouse. In a heart transplantation experiment, when used in vivo, the nitidine chloride can prolong the survival time of the transplanted heart. In a delayed type hypersensitivity reaction model, when used in vivo, the nitidine chloride can reduce the ear swelling degree of the mouse. Both in-vivo and in-vitro results show that the nitidine chloride has a certain effect of resisting the autoimmunity disease and the graft versus host disease. The medicament is a preparation which consists of the nitidine chloride serving as an active ingredient and a pharmaceutical carrier. The medicament can be prepared into an oral preparation, an injection, a suppository or an external preparation and the like.

The invention discloses an application of nitidine chloride in resisting osteoporosis and in preventing and treating bone loss diseases caused by osteoclasts; the inventor, through researches, discovers that the nitidine chloride can inhibit the formation of the osteoclasts and a bone absorption function in a dose-dependent mode for the first time; it discovers that the nitidine chloride, by intervening RANKL-activated NF-kB and NFAT signaling pathways, can develop an effect of inhibiting the osteoclasts; and by establishing an ovariectomized osteoporosis mouse model, it further provides the effect of the nitidine chloride on the osteoclasts. The nitidine chloride can be used as an ideal medicine for preventing and treating the bone loss diseases caused by the osteoclasts in the future.

The invention discloses a preparation method for high-purity nitidine chloride as well as a quality control method of high-purity nitidine chloride. The preparation method is characterized by comprising the following steps of: crushing radix zanthoxyli roots, heating up, refluxing and extracting by using acid alcohol; repeatedly grinding alcohol extract by chloroform; dissolving the obtained precipitates by using methanol, adjusting pH of the solution by using hydrochloric acid, and obtaining nitidine chloride coarse crystals by recrystallization; carrying out recrystallization by using methanol for further improving the purity; preparing by using reverse phase silica gel C-18 and separating by using high-performance liquid chromatography; detecting every part of collected eluant by utilizing an analysis type high performance liquid chromatograph; combining nitidine chloride components with the same retention time, and purity of 90%-98% and more than 98%; concentrating under reduced pressure to obtain nitidine chloride components with purity of 90%-98% and nitidine chloride components with purity bigger than 98%; and carrying out quality control by adopting a thin-layer chromatographic analysis method and a liquid-phase chromatographic analysis method. According to the preparation method disclosed by the invention, not only can the purity of the nitidine chloride be improved, but also the production cost can be reduced.

The invention discloses a method for purifying nitidine chloride. The method comprises the following steps: after smashing a nitidine medicinal material, reflux-extracting by using acidity alcohol solution, merging acid alcohol extracting solution, regulating the pH value by using acid-base, stewing and filtering; alcohol-precipitating, refrigerating, filtering, and concentrating to obtain the extracting solution as sample solution; uniformly mixing the sample solution and normal phase silica gel or aluminium oxide, drying by distillation, separating and purifying through the normal phase silica gel or aluminium oxide, eluting by using ethyl acetate-absolute ethyl alcohol, recycling a solvent, collecting fractions, dissolving by using methyl alcohol, merging the fractions with the high content through the TLC identification and recrystallizing, to obtain a product as the nitidine chloride; and executing the HPLC assay, wherein the transfer rate is more than 80%, and the crystallization purity is higher than 90%. The method is capable of efficiently separating and purifying the nitidine chloride, and is suitable for the large-scale production. The toxicity is small, few solvents are used, the economic value is high, the environmental pollution is small, and the purity is high.

The invention provides applications of nitidine chloride in preparing medicines for preventing/treating sepsis. According to the pharmacodynamics study on the prevention and treatment for the sepsis by adopting nitidine chloride, the prevention and treatment effects of nitidine chloride on the sepsis are studied from the aspects of survival rate, histopathologic changes and serum inflammatory factors of LPS-induced sepsis mice. Nitidine chloride can obviously improve the survival rate of the sepsis mice to 80%, obviously improve the histopathologic changes of the liver and lung tissues of the sepsis mice, reduce the level of proinflammatory factors in the serum of the sepsis mice, and increase the level of anti-inflammatory factors. The cell adoptive transfer experiment proves that for the sepsis mice injected through caudal vein, the survival rate of the sepsis mice is obviously improved, and therefore, nitidine chloride can be used for preparing the medicines for preventing/treating the sepsis. The medicine provided by the invention is a medicinal composition composed of the active ingredient, namely, nitidine chloride and the pharmaceutic adjuvants, and belongs to a preparation for oral administration, injection or percutaneous drug delivery.

The invention belongs to the technical field of application of natural compounds, and discloses application of nitidine chloride in preparation of a urease inhibitor. The nitidine chloride has a remarkable urease inhibition effect, has the characteristics of simple structure, good safety and the like, has good application value and development prospect, and can be used as a urease inhibitor in the fields of plant fertilizers, feed additives, medicines and the like.

The invention discloses high-temperature-resistant printing ink with a fruit flavor. The high-temperature-resistant printing ink is characterized by being prepared from the following raw materials in parts by weight: 27-35 parts of E-12 epoxy resin, 6-9 parts of isopropyl stearate, 4-7 parts of ricinoleic acid, 8-11 parts of propylene glycol cyclohexyl ether, 7-10 parts of ethyl alcohol, 0.02-0.05 part of pancid, 0.2-0.4 part of melamine, 0.01-0.03 part of nitidine chloride, 2-3 parts of tea tree essential oil, 0.7-1.2 parts of magnesium hydrate, 0.2-0.5 part of sodium thiosulfate, 4-5 parts of volcanic ash, 7-10 parts of egg-shell meal, 3-5 parts of cod-liver oil, 12-15 parts of peach juice, 13-16 parts of pear juice, 4-6 parts of organic pigment, and 5-8 parts of an auxiliary. According to the invention, the routine is broken, and peach juice and pear juice are added into the raw materials, so that prepared printing ink has a fruit flavor, and the problem of the irritant ink flavor is completely solved; meanwhile, other components are added, so that the prepared printing ink is high temperature resistant, good in visibility, waterproof, drug resistant, good in toughness, and high in fastness.

The invention discloses a synthetic method of nitidine chloride. The synthetic method comprises the following steps: 1) dissolving 3,4-dimethoxybenzoic acid in a first organic solvent, adding thionyl chloride to react, evaporating out the solvent from reactants to obtain an intermediate 1; 2) dissolving the intermediate 1 by use of the first organic solvent, adding 3,4-methylenedioxy naphthylamine, and performing nucleophilic substitution reaction to obtain an intermediate 2; 3) dissolving the intermediate 2 in the first organic solvent, adding boron trifluoride diethyl etherate and di(trifluoroacetoxyl) iodobenzene to react, removing the solvent from the reactants, performing column chromatography on obtained residues on silica gel to obtain an intermediate 3; 4) dissolving the intermediate 3 in a second organic solvent, and performing lithium aluminum hydride reduction, dehydration and dimethyl sulfate methylation under an atmosphere protection condition, and then treating with sodium chloride to obtain the target product nitidine chloride. The synthetic method disclosed by the invention is relatively simple in synthesis route and relatively high in yield of the target product and the yield is higher than 27%.

The invention discloses a method for determining the content of nitidine chloride in radix zanthoxyli toothpaste, and belongs to the field of chemical detection. The method is accurate, simple and convenient and can be used for controlling the content of nitidine chloride in the radix zanthoxyli toothpaste. The method comprises the following sub-steps sequentially: firstly, extracting nitidine chloride from radix zanthoxyli with ethanol, and collecting ethanol extract; secondly, determining the content of nitidine chloride in the ethanol extract with HPLC (high performance liquid chromatography). The method can be used for determining the content of nitidine chloride in the radix zanthoxyli toothpaste.

The invention discloses a method for preparing nitidine chloride from a total alkali extract of zanthoxylum nitidum stems and branches. The method comprises the steps: adding an alcohol-water solventwith the amount 6-12 times the mass parts of the zanthoxylum nitidum stems and branches into the zanthoxylum nitidum stems and branches, carrying out reflux extraction for 1-3 times for 1-3 h each time, merging filtrates, recovering alcohol and concentrating to a thick paste, and thus obtaining the total alkali extract of the zanthoxylum nitidum stems and branches; adding column-layer chromatographic silica gel with the amount of 2-10 times that of the thick paste to the obtained thick paste, placing in a chromatography column, carrying out solid-liquid extraction separation with ethyl acetateand methanol, merging fractions with same results by thin layer chromatography, and carrying out repeated concentration, precipitation and suction filtration, to obtain a crude compound; recrystallizing with a methanol solvent to obtain a high-purity monomer compound, carrying out primary identification of the components of the monomer compound by thin layer chromatography and a melting point determination method, and identifying the monomer compound obtained from separation to be nitidine chloride according to the physical properties of the compound and thin layer identifying. The method forextracting nitidine chloride from zanthoxylum nitidum is simple and feasible, high in yield, simple to operate and high in separation efficiency.

The invention discloses a thin-layer chromatographic identification method for Zanthoxylum dissitum Hemsl. According to the thin-layer chromatographic identification method, magnoflorine and nitidine chloride are taken as reference substances, specific spots of thin-layer chromatography of the Zanthoxylum dissitum Hemsl are determined, and the method can be used for identifying the Zanthoxylum dissitum Hemsl and distinguishing the Zanthoxylum dissitum Hemsl and the zanthoxylum nitidum. The method is good in repeatability, high in accuracy degree, good in separation, clear in spots, simple, feasible, rapid, low in cost and suitable for distinguishing Zanthoxylum dissitum Hemsl and Zanthoxylum nitidum and quality control and authenticity identification of Zanthoxylum dissitum medicinal materials. The method is good in safety, economical, environment-friendly, safe, high in efficiency and good in application prospect.

The invention discloses a method for measuring the content of nitidine chloride in radix zanthoxyli toothpaste. The method is accurate, simple, fast and convenient, and can be used for controlling the content of nitidine chloride in radix zanthoxyli toothpaste. The method belongs to the field of chemical detection. The method comprises the following steps in sequence: 1, extracting the nitidine chloride in radix zanthoxyli with methanol and collecting a methanol extracting solution; and 2, measuring the content of the nitidine chloride in the methanol extracting solution by using HPLC. The method can be used for measuring the content of the nitidine chloride in the radix zanthoxyli toothpaste.

The invention discloses a preparation method of nitidine chloride. The method comprises the following steps of 1) catalyzing 4,5-dimethoxy-2-(methoxycarbonyl) phenylboronic acid to react with azobenzene bornene to obtain an intermediate 1 by using a metal palladium/ligand; 2) dissolving the intermediate 1 with an organic solvent, then adding trifluoroacetic acid, and conducting a room temperaturereaction to obtain an intermediate 2; 3) methylating the intermediate 2, oxidizing, reducing, and treating with hydrochloric acid to obtain the nitidine chloride. The synthetic route of the method issimpler, and the total synthesis yield of the nitidine chloride is as high as 72% or more.

The invention provides an application of a nano-carrier MIL-100(Fe) in loading nitidine chloride. The invention belongs to the technical field of nano-carrier research. According to the preparation method disclosed by the invention, the nano MIL-100(Fe) is synthesized by using a hydrothermal method; the MIL-100(Fe) has a high loading capacity of 33.43 wt% on NC through a loading experiment, the NCcan be released progressively in a phosphate buffer solution (pH=7.4) after the loaded NC is loaded with the MIL-100(Fe), and 68% of NC is released within 4 days. The toxicity of NC-MIL-100(FE) to ahealthy hepatocyte line LO2 is significantly reduced, and the inhibitory activity to a hepatoma carcinoma cell line HepG2 is higher.