89 results about "Gambogic acid" patented technology

The invention describes a nutraceutical composition and method for preventing/treating cancer comprised of A) quinones (2,3-dimethoxy-5-methyl-1,4-benzoquinone, thymoquinone, tocopherolquinone) B) compounds capable of maximizing oxidative mitochondrial function preferably riboflavin, FAD, FMN, 6,7-Dimethyl-8-(1-D-ribityl)lumazine, ribitol, 5,6-dimethylbenzimidazole, tetrahydrobiopterin, vitamin B₁, lipoic acid, biotin, vitamin B₆, vitamin B₁₂, folate, B3, C and pantothenate C) lactic acid dehydrogenase inhibitors; 2′,3,4′5,7-pentahydroxyflavone, epigallocatechin gallate, quercetin, citric acid, rosemary, black walnut, clove, nutmeg, licorice root, coriander, cinnamon, ginger root, myrrh gum and green tea D) alkalizing agents: aloe vera, chlorella, wheat grass, apple cider vinegar, burdock root, kudzu root, alfalfa, barley grass, spirulina, parsley leaf, calcium, magnesium, potassium or bicarbonate salts E) potent tumoricidal herbs; gromwell root, wild yam, beth root, teasel root, balm of gilead bud, frankincense, bakuchi seed, dichroa root, kochia seed, kanta kari, sweet myrrh, galbanum, garcinia fruit, mace, white sage and tumoricial plant derived constituents: gambogic acid, shikonin, diosmin or boswellic acid F) an antiproliferative herb (speranskia or goldenseal) and G) a pharmaceutically acceptable carrier.

The present invention is directed to novel derivatives of gambogic acid and analogs thereof. The present invention also relates to the discovery that novel derivatives of gambogic acid are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention can be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.

The invention relates to a neo-gambogic acid SLN (solid lipid nanoparticle) and a preparation method thereof. The neo-gambogic acid SLN comprises a therapeutically effective amount of neo-gambogic acid, medicinal phosphatide, a surfactant and a lipid material. In the invention, the neo-gambogic acid is prepared into SLNs (solid lipid nanoparticles), thereby improving the solubility of the neo-gambogic acid, reducing the irritability, improving the bioavailability, and prolonging the action time of medicaments in a human body, in addition, the neo-gambogic acid SLNs can be gathered partially in the human body so as to play the targeted action of the SLNs and exert the anti-cancer therapeutic action of the SLNs better.

The invention discloses a gambogic acid cyclized analog, a preparation method and application thereof. The semi-synthesized gambogic acid cyclized analog is obtained by the extracted and purified gambogic acid through chemical synthesis and has a structural general formula I-III as the right formula, wherein substituent groups of A ring, B ring, C ring, R1, R2, R3, R4, R5, R6, R7, R7, R8, R9, R10, R11 or/and R12 contain glycosyl group, polyhydroxy, amino acid group, acyloxy group, phosphoric acid oxygen group, sulphonic acid oxygen group, alkoxyl group, aromatic oxygen group, heterocyclic oxygen group, mercapto group, substituted mercapto group, primary amine and secondary amines groups or/and substituted primary amine and secondary amines groups, and chain hydrocarbon or and cyclic group containing oxygen, sulphur, nitrogen, carbon or/and phosphor atoms, and one or combination of the substitution groups. The gambogic acid cyclized analog has anti-tumor, antivirus, antibacterial and antifungal pharmacology activities, can be used as anti-tumor, antivirus, immune, antibacterial and antifungal medicaments, and can be applied together with the known anti-tumor, antivirus, immune, antibacterial and antifungal medicaments.

The invention relates to the field of medicinal chemistry, in particular to a garcinia derivative (I), a preparation method thereof and the application of the derivative in pharmacy. The derivative is a structural analogue of a garcinia natural product such as gambogic acid and has the molecular weight which is lower than that of the gambogic acid, and hetero atoms and hydrophilic groups are introduced or further salified, so that the absorbability of a gastrointestinal tract is improved; and the derivative has an antitumor effect and can be used for preparing antitumor medicaments.

The invention discloses a drug containing gambogic acid compound and a preparation method of inclusion compound containing the gambogic acid compound. Cyclodextrin and derivative inclusion compound of the gambogic acid compound of the invention is the cyclodextrin and derivative inclusion compound of various effective components with biological activity in traditional Chinese medicine-gamboge. The preparation mainly contains powder and injection preparation, freeze-dry powder and injection preparation, troche (plain tablet, coating tablet, delayed release tablet and controlled release tablet), capsule, microcapsule, emulsion, micro emulsion and lipid body, etc. The inclusion compound containing the gambogic acid compound is added into the drug by the invention, thereby reducing toxicity and irritation of the drug, strengthening water-solubility, stability, security, etc. and having important theoretical and utility value for the gambogic acid compound in clinical application.

The invention relates to an extraction technology of gambogic acid, which comprises the following steps of firstly, crushing gamboge, uniformly mixing with silica, diatomite, quartz powder or polyacrylamide the quantity of which is 0.5-5 times as much as that of the crushed gamboge, installing a chromatography column, adding an organic solvent, washing, collecting eluent, concentrating the eluent, and recovering a solvent to obtain a gambogic acid primary extractive; secondly, dissolving the gambogic acid primary extractive into triethylamine or pyridine, fully oscillating to form a salt, adding distilled water, stirring, standing, pump filtering, and drying to obtain a crude gambogic acid salt product; thirdly, dissolving the obtained crude gambogic acid salt product into the solvent to prepare a saturated solution, crystallizing to obtain gambogic acid salt crystals, pump filtering, and drying to obtain gambogic acid salts; fourthly, extracting the gambogic acid salts with hydrochloric acid and diethyl ether, separating liquid, taking a diethyl ether layer, reducing the pressure, recovering a diethyl ether solution, and drying to finally obtain solid gambogic acid. The inventionhas the advantages of simple steps, recycled solvent, rapid extraction speed, high purity and high yield.

The invention discloses an erythrocyte membrane-coated co-supporting gambogic acid and indocyanine green albumin nanoparticle and a preparation method and application thereof. The nanoparticle comprises a drug-loaded nano core and an erythrocyte membrane wrapped outside the drug-loaded nano core. The nanoparticle has high biocompatibility and dispersibility, heat is generated under the irradiationof lasers, tumor cells can be killed, the nanoparticle also has great fluorescence performance, a combination therapy mode of photothermal therapy and chemotherapy under a fluorescence imaging mode can be guided, and through the modification of erythrocytes on the surface of the nanoparticle, long circulation in a living body is achieved, so that the therapeutic effect of the drug-loaded nanoparticle is improved.

The invention discloses a polyethylene glycol-gambogic acid liposome, which is composed of a polyethylene glycol-gambogic acid conjugate, polyethylene glycol, vitamin E, cholesterol and phospholipid in a weight ratio of 1-10:0.5-2:0.05-0.2:1-4:10-30. According to the invention, an amphiphilic polymer PEG and an antitumor drug gambogic acid are connected with an ester bond into a conjugate amphipathic PEG-GA, and the PEG-GA is inserted into a liposome bimolecular layer to construct a nano targeted drug delivery system, the water solubility of the drug can be improved, also the drug stability and antitumor effect can be enhanced, drug accumulation in normal tissue can be reduced, the survival time of tumor-bearing mice is prolonged, the treatment efficacy is improved and the toxic and side effects are reduced. The invention also provides a preparation method and application of the liposome, and the liposome can be applied to treatment of lung cancer, ovarian cancer, breast cancer, colorectal cancer, melanoma, head and neck cancer, lymphoma or brain tumors.

The invention relates to an application of gambogic acid in preparing an inflammation inhibitor, in particular to an application of the gambogic acid in preparing medicaments for treating inflammatory factor mediated inflammatory diseases such as endotoxin shock and the like. The gambogic acid has a chemical formula of C38H44O8 and a molecular weight of 628.75, and can be used for preparing the medicaments for treating the inflammatory factor mediated inflammatory diseases such as endotoxin shock and the like, wherein the inflammatory diseases comprise rheumatic arthritis, inflammatory bowel disease, neurodegenerative disease, septic shock and the like. Approved by pharmacological experiments, the gambogic acid can effectively inhibit inflammatory factors such as tumor necrosis factor (TNFalpha), interleukin 6 (IL-6) and nitric oxide (NO), and can be used as an inflammation inhibitor for preparing the medicaments for treating the inflammatory factor mediated inflammatory diseases such as rheumatic arthritis, inflammatory bowel disease, neurodegenerative disease, septic shock and the like.

The invention relates to a preparation method and application of a multifunctional bionic nano-drug, which can effectively enhance the photodynamic therapy of tumors, and adopts the technical scheme that the multifunctional bionic nano-drug is characterized in that a chemotherapeutic drug gambogic acid is entrapped on a polylactic acid-glycolic acid copolymer to obtain a drug-loaded nano-core, the capsule-like membrane-cancer cell membrane composite membrane is coated on the outer side of the nano inner core through ultrasonic extrusion to form the multifunctional bionic nano drug.The multifunctional bionic nano-drug TCPG prepared by the preparation method disclosed by the invention has good biocompatibility; The anti-tumor effect of the nano-drug is effectively improved through a strategy of combining specific homologous targeting and enhanced photodynamic therapy, and the nano-drug is an innovation in nano-drugs.

The present invention relates to glioblastoma inhibiting compounds, in particular gambogic acid amid and derivatives thereof for the treatment of glioblastoma. Moreover, methods for determining whether a treatment with the compounds of the invention is suitable for a patient are disclosed.

The invention provides a method for ultrasonic extraction and content determination for total gambogic acid in gamboge medicinal materials, comprising the following steps of: drying the gamboge medicinal materials, crushing and then passing through a 40-mesh sieve, weighing crude powders, mixing with 50-100% ethanol solution in a solution-material ratio of 5:(1-20):1, extracting for 5-20 minutes at a temperature of 20-60 DEG C and an extraction frequency of 20-70 kHz to obtain a total gambogic acid extract, filtering, decompressing the filtrate to recover a solvent, concentrating into an extractum shape, and drying under a reduced pressure to obtain a total gambogic acid powder; and detecting the content of total gambogic acid in the gamboge medicinal materials and the extractive by ultraviolet spectrophotometry. The method provided by the invention is simple in extraction process flow, easy to control operation, and effectively shortens in extraction time; and the ultraviolet spectrophotometry is good in detection repeatability, simple in operation, high in accuracy, and capable of being used for quality control for the gamboge medicinal materials or the extractive.

The invention aims at providing a method of efficiently extracting and separating gambogic acid and neogambogic acid from gamboge, serving as a traditional Chinese medicine. The method comprises the following steps: crushing the gamboge, carrying out microwave extraction, and concentrating to obtain an extract A; leaching with petroleum ether, dissolving and filtering with ethanol, and carrying out chromatographic separation by virtue of a simulated moving bed to obtain a component B rich in the gambogic acid and a component C containing the gambogic acid and the neogambogic acid; and recovering a solvent, drying to obtain products, including the gambogic acid with the purity to be above 95 percent and a mixture of 10-20 percent of the gambogic acid and 30-50 percent of the neogambogic acid, in two specifications. The method of extracting the effective components of the gamboge, serving as the traditional Chinese medicine, is simple in step and high in product purity and is capable of simultaneously obtaining the products, including the gambogic acid and the neogambogic acid, in two specifications, fully extracting and separating the effective components from the raw materials and improving the production efficiency while saving the raw material resources.

The invention relates to gambogic acid derivatives as well as a preparation method and application thereof. The derivatives with the structures are mainly characterized in that a plurality of C-30 carboxyl reduced and aminated compounds are obtained for the first time through modifying the C-12, C-29 and C-30 positions of gambogic acid. Biological tests prove that the compounds have anti-tumor activity and can be used for preparing anti-tumor drugs, and the derivatives can be used as lead compounds so that an approach is developed for finding novel anti-tumor drugs. In the formula, R1 is hydroxyl, alkyl or benzyl; R2 is non-substituent, hydroxyl or alkyl, and at the moment, C-12 can form a single bond or double bonds with oxygen; R3 and R4 are respectively methyl, ester group, methylene alcohol, formyl and substituted amino group.

The invention discloses a natural and biodegradable N-long-chain alkyl-N-arginine chitosan derivative as well as a micellar preparation method thereof and application of using the natural and biodegradable N-long-chain alkyl-N-arginine chitosan derivative as a solubilizing and absorption prompting nanometer carrier of gambogic acid which is difficult to dissolve by being taken orally and difficult to absorb.

The invention relates to a preparation method and applications of gambogic acid self-assembled polymer nanoparticles. The preparation method comprises the following steps: adding polyethylene glycol, epsilon-caprolactone, stannous octoate and methylbenzene into a three-necked bottle, and carrying out oil bath reaction at 130 DEG C for 12h under the stirring state and under the protection of N2; after the reaction, removing methylbenzene through rotary evaporation; dissolving the product by adopting dichloromethane, slowly dropwise adding the obtained solution into plenty of cold petroleum ether for precipitation, operating repeatedly, and carrying out suction filtration to obtain a polymer material; taking gambogic acid, placing gambogic acid into an eggplant-shaped bottle, adding acetonitrile for dissolving gambogic acid, adding the polymer material into the obtained solution for dissolving, removing acetonitrile through rotary evaporation, after removing of acetonitrile, a layer of medicinal film is formed on the wall of the bottle, placing the bottle into a vacuum drying oven, removing trace amount of acetonitrile, adding purified water into the bottle, carrying out hydration treatment under 65 DEG C, placing the obtained solution into an ice-water bath, carrying out ultrasound treatment for twice under the power of 315W, wherein each time of ultrasound treatment lasts for 2 min, and after the ultrasound treatment, filtering the obtained solution by a 0.45 [mu] m filter membrane. The prepared nanoparticles are high in encapsulation efficiency, high in drug loading capacity, and good in stability.

The invention discloses a gambogic acid-galactose-HPMA (N-(2-hydroxypropyl)methacrylamide) high-molecular copolymer. The structural formula is shown as (I) in the specification. In the formula, x=5-10 mol%, y=5-10 mol%, z=80-90 mol%, Mn=2.2*10<4>, and Mw/Mn=1.45. A preparation method comprises the following steps: preparing a galactose derivative C by taking D-galactose as a preparation raw material; reacting gambogic acid oxalamide and methylacryloyl to prepare a gambogic acid derivative D; and finally, performing condensation on the galactose derivative C, the gambogic acid derivative D and HPMA to obtain the gambogic acid-galactose-HPMA high-molecular copolymer. After being used in a drug for treating a neoplastic disease, the copolymer has a targeted intelligent drug release functional and achieves a favorable inhibition effect for liver cancer, lung cancer and colon cancer.

The present invention relates to a gambogic acid derivative, a preparation method and uses thereof. The structure formula of the derivative is represented by a formula (I). The preparation method comprises: in an inert solvent, carrying out a reaction of gambogic acid and p-aminomethyl benzoate (formula (III)) or chloromethyl benzoate. The gambogic acid derivative can be used for preparing compositions, anti-tumor drugs, antifungal drugs or anti-angiogenesis drugs, or combining with other anti-cancer active ingredients to be used. In addition, the gambogic acid derivative provides good activity for plural types of tumor cells, and presents good tumor cell targeting performances so as to establish a foundation for development of novel drugs.

The invention discloses a gambogic acid core-shell structure composite nanometer preparation and a preparation method thereof. According to the composite nanometer preparation, poly-(gamma-glutamic acid)alpha-benzyl ester is adopted as a nuclear material, hyaluronic acid grafted with retinoic acid is adopted as a shell material, the nuclear material is located inside the nanometer preparation in ananoparticle mode, pi-pi stacking and lyophobic impact force is used for loading gambogic acid, an amphipathy material adopts lipophilic retinoic acid to be arranged around nanoparticles in a wrapping mode, a hydrophilic hyaluronic acid chain is located on the outermost side of the nanometer preparation, and the shell material achieves the effects of protecting medicine inside a core, maintainingthe stability of the nanometer preparation and achieving active targeting. The preparation mainly has the advantages that the nanometer preparation is controllable in preparation technology, good instability and high in packaging rate, has the active targeting capability, can well solve the problems affecting the druggability of gambogic acid that the water solubility is poor, instability is caused, metabolic clearance is likely to be caused, can improve the anti-neoplastic activity of gambogic acid, and can eliminate the existing slight toxic and side effect of the gambogic acid.

The invention provides an ultrasonic administration microbubble compound carrying an anti-tumor drug as well as a preparation method and application of the ultrasonic administration microbubble compound. The compound is prepared by connection of cationic microbubbles and an anti-tumor drug-PLGA nanoparticles through attraction of positive and negative charges. According to the preparation method, the GA-PLGA nano-particles are prepared by utilizing an ultrasonic emulsification effect, and the CMB and the GA-PLGA nano-particles are connected through charge attraction to form the CMBS-GA-PLGA micro-bubble compound due to the fact that the cationic micro-bubbles carry positive charges and the GA-PLGA nano-particles carry negative charges. The micro-bubbles generate a series of alternative changes such as expansion, shrinkage, oscillation and implosion under the effect of ultrasound, so that the permeability of a cell membrane is improved, the phenomenon is called as 'sound pore effect', gambogic acid can better act on glioblastoma cells by utilizing the 'sound pore effect' of the micro-bubbles under the action of ultrasound, and a new thought is expected to be provided for treatment of glioma.

The invention discloses ready-to-eat cooked chestnut kernels with long-time storage. The ready-to-eat cooked chestnut kernels are prepared by the following steps: processing chestnuts, baking for three times, packaging and sterilizing. Compared with the prior art, the ready-to-eat cooked chestnut kernels disclosed by the invention have the following advantages that the preparation method is simple; due to no addition of chemical additives, environmental-friendly and safe effects are achieved; the chestnut kernels are baked for three times, are soaked with a gambogic acid solution before the second baking, and then are baked at high temperature to damage the cell walls of microorganisms and disturb the synthesis of the cell walls, so that the effect of preventing the chestnuts from going bad is achieved; and the surfaces of the chestnut kernels are sprayed by using needles of pinus massoniana before the third baking, and an anti-oxidation layer can be formed on the surfaces of the chestnut kernels, so that the color change can be effectively prevented, the nutritional value and mouthfeel are maintained for a long time, and the storage time of the ready-to-eat cooked chestnut kernels at normal temperature is prolonged.

The invention relates to a gambogic acid separating and purifying production process, which includes crushing, extracting, medium-pressure silicagel column chromatography and ODS (octadecyl silane) refining. The process is simple in procedure, low in cost, short in cycle and high in yield, gambogic acid purity is up to more than 99%, and the process is suitable for large-scale industrial preparation of high-purity gambogic acid. The gambogic acid needs to be well ground to facilitate better extraction, and most high-polarity impurities can be quickly removed by extraction. Column efficiency is higher and separation degree is higher by means of 300-400-mesh silicagel chromatographic separation at medium pressure, and purity can reach more than 99% after ODS refining.

The invention discloses a preparation method for novel TiO2 nano crystal whisker materials commonly-loaded with gambogic acid. The preparation method comprises the following steps: firstly, mixing hydrated titanium oxide and potassium carbonate and roasting to obtain potassium dititanate; completely exchanging K<+1> ions from the potassium dititanate by a hydrochloric acid liquid to obtain hydrated potassium dititanate; carrying out a hydrothermal reaction on the hydrated potassium dititanate and a glucose liquid; washing and drying in vacuum; and finally, roasting in the air atmosphere of 510-550 DEG C to obtain the product. With the adoption of the preparation method, nano particles with strong photocatalytic effects, small grain diameters, good water dispersibility, high encapsulation efficiency and slow release property can be obtained. A TiO2 nano crystal whisker prepared by the preparation process through adopting a chemical co-precipitation method is a novel anti-tumor preparation integrating chemotherapy, phototherapy and thermotherapy, and has a plurality of advantages of light targeting property, slow release, small side effects and the like, so that the TiO2 nano crystal whisker is the novel anti-tumor preparation which has a very good application prospect.

The invention relates to the field of medicinal chemistry and in particular relates to garcinia triazole derivatives (9), a preparation method of the derivatives and medical application of the derivatives in pharmacy. R1, R2 and n are defined as the specification. The derivatives are structural analogues of a garcinia natural product, namely gambogic acid, have the antitumor effects and can be used for preparing antitumor medicines. The structural formula is as shown in the specification.