35 results about "Fangchinoline" patented technology

A method for obtaining purified bisbenzylisoquinoline alkaloids from the roots of Stephania Tetrandra involves obtaining, from the roots of Stephania Tetrandra, a precipitate comprising tetrandrine, fangchinoline and compounds which constitute impurities, contacting the precipitate with chloroform to form a chloroform solution in which tetrandrine and fangchinoline is dissolved, separating the chloroform solution containing dissolved tetrandrine and fangchinoline from undissolved impurities, removing chloroform from the chloroform solution to obtain a chloroform extract solid having an enriched tetrandrine and fangchinoline content relative to the precipitate, contacting the chloroform extract solid with cool benzene to form a combination comprising undissolved fangchinoline and a benzene solution in which tetrandrine is dissolved, separating the benzene solution from the undissolved fangchinoline from the first solid, removing benzene from the first benzene solution to form a benzene extract which comprises tetrandrine, and subjecting the benzene extract which comprises tetrandrine and subjecting the undissolved fangchinoline to further operations to obtain purified tetrandrine and fangchinoline, separately. The method has the advantages of being able to achieve higher yields of tetrandrine as well as fangchinoline while using lower amounts of benzene, and does not require the use of chromatographic separation columns.

The invention relates to the field of detection on traditional Chinese medicine quality, relates to a method for rapidly detecting index composition in Chinese herbal medicine compound preparation, and especially relates to a rapid detection method for index composition in a Chinese herbal medicine compound preparation radix-stephaniae-tetrandrae radix-astragali soup. According to the method, methanol with the concentration of 50% is employed for ultrasonic extraction, and an HPLC-DAD process is applied to simutaneously determine the content of fangchinoline, tetrandrine, calycosin-7-glucoside, liquiritin and glycyrrhizic acid in radix stephaniae tetrandrae, radix astragali and radix glycyrrhizae in the radix-stephaniae-tetrandrae radix-astragali soup at one time. The method solves the problem that quality control is simultaneously performed on stephaniae tetrandrae, radix astragali and radix glycyrrhizae in the radix-stephaniae-tetrandrae radix-astragali soup, and avoids time and reagent waste caused by multiple detection on the five index compositions. The method is simple in operation and high in working efficiency and precision.

The invention belongs to the technical field of pharmacy, and particularly discloses a stephania hainanensis total alkaloid extract extracted from stephania hainanensis tubers and a preparation method thereof. The preparation process is as follows: material (stephania hainanensis dry tubers); grinding; soaking in a moderate amount of 0.01 to 10 percent of hydrochloric acid or sulfuric acid; 1 to 4 times of ultrasonic extraction; filtration; storng-acid cation exchange resin purification; solvent recovery for drying; and stephania hainanensis total alkaloid extract. The extract mainly comprises L-tetrahydropalmatine, palmatine, fangchinoline, hanfangchin and other active ingredients, the percentage by weight of stephania hainanensis total alkaloid is greater than or equal to 70 percent, the percentage by weight of the palmatine is greater than or equal to 20 percent, and the percentage by weight of the fangchinoline is greater than or equal to 40 percent. Reports on the stephania hainanensis total alkaloid extraction process are not found in related literatures so far, the operation flow of the method is simple, the purity of the product is high, the efficacy is remarkable, and the method disclosed by the invention is applicable to industrial production and the exploitation and utilization of local stephania hainanensis resources.

The invention discloses a new use of bisbenzylisoquinoline compound shown in formula (I) or pharmaceutically acceptable salt thereof except for tetrandrine and fangchinoline. The use is application of the bisbenzylisoquinoline compound shown in formula (I) or pharmaceutically acceptable salt thereof in preparing a medicine or healthcare product for treating insomnia and improving sleep. The bisbenzylisoquinoline compound shown in formula (I) or pharmaceutically acceptable salt thereof can be used as an effective component and made into any dosage form. The result of animal experiment indicates that: the bisbenzylisoquinoline compound shown in formula (I) or pharmaceutically acceptable salt thereof can obviously prolong the total sleep time of normal rats and mouse, including REM (rapid eye movement) sleep time and NREM (non-rapid eye movement) sleep time. The application disclosed by the invention is suitable for various types of insomnia or sleep disorders.

The invention relates a method for separating and purifying fangchinoline and tetrandrine from stephania tetrandra. The stephania tetrandra is taken as a raw material, and the method comprises the following steps of: (1) preparation of crude extract; (2) pre-separation of acid dissolution and alkaline sedimentation; and (3) purification of a high-speed reverse flow chromatograph to obtain the fangchinoline and tetrandrine with purities over 98%. According to the method disclosed by the invention, alkaloid in the stephania tetrandra medicinal material is extracted by alcohol, pre-separated by the acid dissolution and alkaline sedimentation and purified by the high-speed reverse flow chromatograph, and the technical process is green and environemtal-friendly and does not have serious damageto the environment.

The invention relates to application of a compound fangchinoline with a tetrahydroisoquinoline parent nucleus in the aspect of resisting conjunctival melanoma and research on an action mechanism of the compound fangchinoline. Specifically, experiments show that fangchinoline directly targets far-end upstream binding protein 2 (FUBP2), so that gene expression of c-Myc protein is reduced, expression of key proteins RAD51 and BRCA1 of c-Myc downstream homologous recombination (HR) pathways is reduced, and the purpose of inhibiting tumor replication is achieved. The compound disclosed by the invention can be administrated together with cisplatin or olaparib to increase the anti-conjunctival melanoma drug effect and reduce the drug toxicity, so that the compound has a good clinical application prospect.

The invention discloses a compound algistat which is prepared from berberine, fangchinoline and sanguinarine hydrate. The invention also discloses a preparation method and application of the compound algistat. The compound algistat is an environment-friendly algistat, through the combination and advantage complementary of multiple typical alkaloid compounds, the multiple algae causing algae blooms can be effectively suppressed at the same time, thereby greatly improving the algicidal efficiency. The compound algistat provided by the invention has an effective inhibition rate of 80% to 92% or more within 96h on three kinds of green algae such as microcystis aeruginosa, chlorella pyrenoidosa and scenedesmusobliqnus.

The invention discloses a preparation method for tetrandrine and fangchinoline and belongs to the technical field of drug preparation. Lipotropy tertiary amine total alkali is adopted, and the preparation method comprises two steps that firstly, a medium pressure silica gel chromatography column method is used for separation, and elution is carried out through petroleum ether-ethyl acetate-diethylamine; secondly, purification is carried out through a preparation high performance liquid chromatography, methyl alcohol-water serves as a mobile phase, and finally, eluent is concentrated and evaporated to dryness. The method has the advantages that operation is convenient and quick and purity and the extraction rate are high.

The invention provides application of fangji root extract and fangchinoline in pharmacy. Fangji root extract and fangchinoline are used as components of an acetylcholinesterase inhibitor, and the acetylcholinesterase inhibitor is used for preparing a medicine for preventing and treating Alzheimer disease. The invention provides the application of fangji root extract and fangchinoline in pharmacy,provides a new drug candidate source for preventing and treating Alzheimer disease, and has important significance in the aspects of improving the clinical treatment effect of the Alzheimer disease and reducing the toxic and side effects of drugs.

The invention discloses a sulfonyl fangchinoline compound as well as a preparation method and application thereof. The sulfonyl fangchinoline compound has a structure as shown in a formula (I) or a formula (I'). According to the formula (I) or formula (I'), R is selected from alkyl, aryl, benzyl, heterocyclyl, substituted alkyl, substituted aryl, substituted benzyl and substituted heterocyclyl; the substituent group of the substituted alkyl is halogen or nitro; the substituent group of the substituted aryl, the substituent group of the substituted benzyl and the substituent group of the substituted heterocyclyl are one or more of halogen, alkyl and nitro; Y is selected from one-molecule inorganic acid and organic acid or two-molecule inorganic acid and organic acid. The compound has a bisbenzylisoquinoline parent nucleus structure, has sulfonyl characteristics, has a good XOD inhibition effect, and can be used for treating and improving gout, reducing uric acid and the like.

The present invention relates to a preparation extracted from Stephania tetrandra S. Moor and its use for manufacture of medecine for enhancing the sensitivity or effect of chemotherapy, enhancing the sensitivity of radiotherapy, improving the level of leukocytes in body, and having antineoplastic and antianaphylaxis effects. Said preparation is mainly composed of tetrandrine and fangchinoline with the ratio of 9:1 to 8:2 (moles), which is obtained by the following process: (1) the powder or piece of Stephania tetrandra S. Moor is extracted with dilute acid with the cool acid extract being collected; and washed with water with the aqueous extract being collected; then the cool acid extract and aqueous extract are combined, adjusted with base pH 10 to 12, kept overnight; (2) the fluid of Step (1) is filtered, the solid dried, pulverized to give Powder 1; (3) Powder 1 is heated under reflux in alcohol for 30 min.; (4) the alcohol extract from Step (3) is concentrated, kept, filtered to give Solid 2; (5) Solid 2 is dissolved in warm ammoniac ethanol, kept for crystallization. The present invention also relates to the use of tetrandrine and the pharmaceutically acceptable salt thereof for manufacture of medecine for improving the level of leukocytes in body.

The invention provides a method for extracting tetrandrine and fangchinoline from radix stephaniae tetrandrae. The method comprises the following specific steps: pulverizing dry radix stephaniae tetrandrae, adding bacillus subtilis and yeast for fermentation, performing alcohol extraction, filtration and concentration to a concentrated liquid, adding hydrochloric acid to adjust the pH value, and performing butanol extraction to obtain an aqueous phase A and a butanol extracting solution A; adding sodium hydroxide and hydrochloric acid into the butanol extracting solution A to adjust the pH value, and performing butanol extraction, concentration, sodium carbonate solution dissolving, filtration and ethanol crystallization to obtain the tetrandrine; adding sodium hydroxide into the aqueous phase A to adjust the pH value, and performing butanol extraction, concentration, sodium carbonate solution dissolving, filtration and ethanol crystallization to obtain the fangchinoline. The method can effectively increase the yield of alkaloid of the radix stephaniae tetrandrae, reduce the difficulty of wastewater treatment and improve the utilization rate of radix stephaniae tetrandrae resources.

The invention discloses an application of fangchinoline for preparing medicine for treating or preventing HIV. The fangchinoline can dosage-dependently inhibit the copying of HIV-1 under in-vitro condition, and can inhibit the copying of HIV-1 by the percentage of more than 97% under nontoxic concentration on cell. The fangchinoline acts on the later period in a virus copying period, and the action mechanism is different from all the antiviral drugs on the market, and the effect target is new. The fangchinoline is taken as an effective component of traditional Chinese medicinal materials such as Radix Stephaniae Tetrandrae, the source is wide, the fangchinoline has the advantages of safety and low toxicity, and has wide prospect for exploitation of anti-HIV-1 drugs.

The invention provides a method for simultaneously measuring contents of tetrandrine and fangchinoline in the medicinal material of the root of fangji. The method comprises the following steps: step A, preparing an extracting solution; to be specific, smashing the root of fangji, weighing a proper amount of powder, extracting 2% of hydrochloric acid methanol, carrying out room temperature ultrasound processing, carrying out preliminary filtering by using a piece of medium-speed filter paper, taking filter liquor and carrying out filtering by using a microporous filter membrane to obtain an extracting solution using tetrandrine and fangchinoline as reference substances; step B, adjusting detection conditions of a high performance liquid chromatograph under conditions of having the chromatographic column of Agilent ZORBAX Extend-C18 (4.68250 mm, 5 microns), the mobile phases of acetonitrile and 0.08% of triethylamine water at a ratio of 75 to 25, an isocratic elution mode, a sampling size of 8 microlitres, a flowing speed of 1.0mL.min-1, a column temperature of 25 DEG C, and a detection wavelength of 282nm; and step C, carrying out feeding, waiting for test sample and reference substance results, and calculating contents of tetrandrine and fangchinoline in all test samples respectively according to an external standard method for calculation with a peak area. After long-term repeated verification, the method is verified to have advantages of high accuracy, precision, and specificity, and high durability of the chromatographic condition.

The invention relates to the technical field of bio-preparation of a fangchinoline derivative, in particular to a fangchinoline derivative with anticancer activity as well as a preparation method andapplication of the fangchinoline derivative. The molecular structure of the fangchinoline derivative is shown in the specification. The novel tetrandrine derivative is synthesized, has an anti-canceractivity effect and is high in activity. The biological activity of the fangchinoline is improved by performing structural modification on the fangchinoline, and the fangchinoline has important practical significance for researching and developing novel anti-cancer drugs. According to the fangchinoline derivative with the anticancer activity, fangchinoline is used as a raw material for related structural modification, the synthesis method is simple, the price of the raw material is low, and the structure is novel.

The invention relates to the field of medicine, in particular to a new medical use of a bisbenzylisoquinoline alkaloid compound. The invention provides an application of fangchinoline in the preparation of a medicine for preventing and treating ulcerative colitis. Preferably, fangchinoline is used as a unique active ingredient for preparing the medicine for preventing and treating ulcerative colitis. Fangchinoline can be used for preparing the medicine for preventing and treating ulcerative colitis.

The invention provides a technology for inhibiting activity of acetylcholin esterase. The technology comprises a pharmaceutical composition for inhibiting the activity of acetylcholin esterase, an Alzheimer disease prevention and treatment medicine, a production method of the pharmaceutical composition and a production method of the Alzheimer disease prevention and treatment medicine. The pharmaceutical composition comprises fangchinoline and berberine at a mole ratio of 1:5-2:1. The inventors combine fangchinoline and berberine by reference to a clue and a method of compound compatibility oftraditional Chinese medicines; an obvious synergic compatibility effect can be generated in an aspect of inhibition of acetylcholin esterase; and the use dosage and toxicity of a single medicine are reduced.

The invention discloses a preparation method of a traditional Chinese medicine anti-allergic agent tetrandrine. The method comprises the following steps of: S1, extraction of total alksloid: putting 100g of stephania tetrandra powder into a 500ml round-bottom flask, adding 300ml of ethanol, conducting heating and refluxing in a water bath for 1h, filtering out an ethanol extracted solution, adding200ml of ethanol into decoction dregs again, performing extraction once again by the same method, combining the two extracted solutions, performing filtering, and conducting concentrating until no alcohol smell into a syrup. According to the invention, the solvent is added many times, main components in the stephania tetrandra powder are prepared in terms of total alkaloid, stephania tetrandra total alkaloid and mixed crystals. In the preparation process, through mutual superposition operation of filtration and extraction, the pH of materials in the corresponding steps is adjusted, after thetarget component is subjected to liquid-liquid extraction twice, tetrandrine and the fangchinoline are respectively obtained, then the two substances are separated through solubility difference, the raw material utilization rate is effectively increased, and the production cost is reduced.

Spur is a common frequently-occurring disease and is poor in effect and easy to relapse when being treated by adopting common medicines or adopting methods such as manipulation, drawing, physiotherapy, acupuncture, small acupotomy, operation and the like. Aiming at the spur disease pathogenesis, the invention provides a plaster for treating the spur and a preparation method thereof. The plaster comprises the following components: 5-10g of artificial moschus, 15-25g of dragon's blood, 30-60g of angelica root, 18-40g of natural indigo, 30-50g of manchurian wildginger, 20-50g of Chinese ephedra, 30-50g of cowherb seed, 40-60g of prepared common monkshood mother root, 40-60g of prepared radix aconiti kusnezoffii, 30-70g of rhizoma corydalis, 30-50g of indian iphigenia bulb, 50-80g of grifola, 30-50g of fangchinoline, 45-80g of herba siegesbeckiae, 30-60g of uniflower swisscentaury root, 50-60g of rhizoma homalomenae, 30-65g of medcinal evodia fruit, 40-75g of arisaema with bile, 10-15g of scorpion, 30-70g of mustard seed, 100-450g of garlic, 10-30g of Japanese buttercup herb, 1000-1500g of sesame oil and 500-1000g of dimethyl sulfoxide. The plaster has the advantages of convenience for use, low cost, no side effects, no drug anaphylaxis reactions, and high cure rate up to 95 percent.

The invention belongs to the technical field of chemical pesticide synthesis, and particularly relates to a compound fangchinoline-carbamate derivative with bactericidal activity. The compound is prepared by carrying out a one-step addition reaction on natural product fangchinoline with alkyl or aryl isocyanate in dichloromethane and triethylamine at room temperature, and the yield is high. An antibacterial activity screening test proves that the fangchinoline-carbamate derivative has a relatively good inhibition effect on fusarium graminearum or phomopsis spp., and activity of the fangchinoline-carbamate derivative is superior to or equal to activity of bactericidal pesticide azoxystrobin with a relatively large usage amount.

The invention discloses a compound algistat which is prepared from berberine, fangchinoline and sanguinarine hydrate. The invention also discloses a preparation method and application of the compound algistat. The compound algistat is an environment-friendly algistat, through the combination and advantage complementary of multiple typical alkaloid compounds, the multiple algae causing algae blooms can be effectively suppressed at the same time, thereby greatly improving the algicidal efficiency. The compound algistat provided by the invention has an effective inhibition rate of 80% to 92% or more within 96h on three kinds of green algae such as microcystis aeruginosa, chlorella pyrenoidosa and scenedesmusobliqnus.

The invention discloses a crystal form I of fangchinoline-7-propionate, which uses Cu-Ka radiation, and X-ray powder diffraction expressed by an angle of 2[theta] has characteristic peaks at 9.96, 12.42, 13.72, 14.18, 19.61, 20.06 and 25.02 + / -0.2. The crystal form has the advantages of high stability, high bio-availability and easiness in preparation.

The invention relates to a purification method of fangchinoline. The method comprises the following specific steps: (1) refluxing or quenching and extracting fangchinoline medical powder by utilizing an alcohol solution, recovering solvents from the extracting solution until no alcohol flavor exists, and acidifying until the solution is acidic; and (2) performing alkaline regulation on the acidic solution, extracting with chloroform, filtering the extract through an ODS (Ozone Depleting Substance) silicagel column by a dry method, eluting with a methanol-water or acetonitrile-water mixed solvent, recovering solvents from the eluent and drying to obtain the fangchinoline. The purification method has the advantages of low energy consumption, low preparation period and high product purity.

The invention relates a method for separating and purifying fangchinoline and tetrandrine from stephania tetrandra. The stephania tetrandra is taken as a raw material, and the method comprises the following steps of: (1) preparation of crude extract; (2) pre-separation of acid dissolution and alkaline sedimentation; and (3) purification of a high-speed reverse flow chromatograph to obtain the fangchinoline and tetrandrine with purities over 98%. According to the method disclosed by the invention, alkaloid in the stephania tetrandra medicinal material is extracted by alcohol, pre-separated by the acid dissolution and alkaline sedimentation and purified by the high-speed reverse flow chromatograph, and the technical process is green and environemtal-friendly and does not have serious damageto the environment.

The invention provides an acetylcholinesterase inhibitor and a production method thereof, a medicine for preventing and treating Alzheimer's disease and a production method of the medicine. The acetylcholinesterase inhibitor comprises Fangchinoline and coptisine, wherein the mole ratio of the Fangchinoline to the coptisine is (1 to 5) to (2 to 1). The thought and the method of the compatibility ofa Chinese herbal compound are used for reference, and the Fangchinoline and the coptisine are combined, so that the acetylcholinesterase inhibitor can generate obvious synergistic compatibility effects in the respect of acetylcholinesterase inhibition, and the usage dosage of a single medicine and the toxin are reduced.

Spur is a common frequently-occurring disease and is poor in effect and easy to relapse when being treated by adopting common medicines or adopting methods such as manipulation, drawing, physiotherapy, acupuncture, small acupotomy, operation and the like. Aiming at the spur disease pathogenesis, the invention provides a plaster for treating the spur and a preparation method thereof. The plaster comprises the following components: 5-10g of artificial moschus, 15-25g of dragon's blood, 30-60g of angelica root, 18-40g of natural indigo, 30-50g of manchurian wildginger, 20-50g of Chinese ephedra,30-50g of cowherb seed, 40-60g of prepared common monkshood mother root, 40-60g of prepared radix aconiti kusnezoffii, 30-70g of rhizoma corydalis, 30-50g of indian iphigenia bulb, 50-80g of grifola,30-50g of fangchinoline, 45-80g of herba siegesbeckiae, 30-60g of uniflower swisscentaury root, 50-60g of rhizoma homalomenae, 30-65g of medcinal evodia fruit, 40-75g of arisaema with bile, 10-15g ofscorpion, 30-70g of mustard seed, 100-450g of garlic, 10-30g of Japanese buttercup herb, 1000-1500g of sesame oil and 500-1000g of dimethyl sulfoxide. The plaster has the advantages of convenience for use, low cost, no side effects, no drug anaphylaxis reactions, and high cure rate up to 95 percent.

The invention provides a method for determining multi-component content of a Jingyaokang capsule. The method comprises the following steps: S1, preparation of a mixed reference substance solution, precisely weighing strychnine, alpha-cypress alkali, periplocin, 11-carbonyl-beta-frankincense acid, curcuma zedoary bicyclo-enone, hydroxysafflor yellow A, naringin, tetrandrine, fangchinoline and beta-ecdysterone respectively, and dissolving the above materials in a solvent to obtain the mixed reference substance solution for later use; s2, preparation of a test solution, taking the Jingyaokang capsule, adding a solvent for extraction, performing filtering, and taking filtrate to obtain the test solution for later use; s3, content determination, precisely sucking the reference substance solution and the test solution respectively, injecting the solutions into a liquid chromatograph, and performing determining to obtain the content. According to the determination method, the contents of tenchemical components such as strychnine, alpha-jacosinine, periplocin, 11-carbonyl-beta-masticinic acid and naringin in the Jingyaokang capsule are determined, and the quality of the Jingyaokang capsule can be better controlled.

The invention provides a radix stephaniae tetrandrae mixture for veterinary use and a preparation method thereof. The sustained-release accessories in the formula can form a biological corrosion framework of medicine molecules; after the medicine is injected into an animal body, the diffusion speed of the medicine can be reduced to realize sustained release, and the administration times for the animal can be reduced while guaranteeing the efficacy; the dregs after distilling cinnamon are decocted again with poria cocos and polyporus umbellatus, so that the leaching amount of active ingredients in the cinnamon, poria cocos and polyporus umbellatus can be increased; and the radix stephaniae tetrandrae is extracted separately, so that the loss of the total amount of alkaloids is reduced, the yield of tetrandrine and fangchinoline is increased, and then the efficacy of the medicine is better. Compared with a radix stephaniae tetrandrae mixture prepared by a common conventional method, by adopting the radix stephaniae tetrandrae mixture for veterinary use, provided by the invention, the medicine taking times by an animal can be reduced, the stress response of the animal is reduced, the content of the active ingredients, namely tetrandrine and fangchinoline, is higher, and the efficacy is better.

The invention relates to a method for separating and determining tetrandrine and fangchinoline. The method comprises the following steps: 1, dissolving a Stephania tetrandra root raw drug or a traditional Chinese medicinal preparation containing the Stephania tetrandra root in methanol, carrying out ultrasonic treatment, and filtering; and 2, carrying out high performance liquid chromatography detection on the filtrate obtained in step 1, wherein the mobile phase is a methanol-water mixed solution with the volume ratio of 65:35, 1g / L of sodium octanesulfonate is added, the pH value is adusted by acetate acid gracial to 3, the flow velocity is 1mL / min, and the sample introduction amount is 10[mu]L. The method adopting methanol dissolving to carry out sample pretreatment has the advantages of simple operation and low cost, the whole chromatography process time is 14min, the lowest detection limits of tetrandrine and fangchinoline are 0.28mg / L and 0.13mg / L respectively, the linear ranges of the tetrandrine and fangchinoline are 125-4000mg / L and 47-1500mg / L respectively, the linear correlation coefficient is good, the recovery rate of the method is greater than 90%, and RSD is less than 10%.