91 results about "Triptosine" patented technology

The invention discloses a tripterine derivate and use thereof. The tripterine derivate has a structure as shown by a formula I. When R2 is H, R1 is alkyl, amine radical, alcohol, aryl, mixed aryl or heterocyclic radical connected with tripterine through ester bonds or amido bonds, and R2 is acyl or organic acid radical when R1 is OH. The tripterine derivate can be used for preparing anticancer medicine, anti-inflammatory medicine or medicine for treating central nervous system diseases. The medicine can be made into tablets, capsules, granules, fine grains, powder, pills, plaser, oral liquid or injections.

The invention discloses a tripterine derivative, biogenetic salt of the derivative, and a preparation method and application of the biogenetic salt. The tripterine has a structure as shown in the specification. The biogenetic salt of the tripterine derivative is prepared by mixing and reacting the tripterine derivative with medicinally acceptable inorganic acid or organic acid. The tripterine derivative and the biogenetic salt of the tripterine derivative can be used for preparing medicines for resisting hepatic fibrosis. A nitrogen-containing hydrophilic group is introduced into C-28 position carboxylic acid and the tripterine derivative is salinized, so that the pharmacokinetic property is improved obviously, the bioavailability is improved, and the safety is improved.

The invention discloses the application of celastrol in the preparation of the medicine for treating cancer expressing CIP2A protein. The celastrol of the invention has the characteristics of having no obvious down regulation CIP2A protein with the cell line particularity, reducing the expressing of oncoprotein in lung cancer, liver cancer, breast cancer and gastric cancer with time and dose pendence, causing oncoprotein C-Myc steadied by CIP2A to generate corresponding retrogradation, displaying remarkable cytotoxic activity in the cell of lung cancer and liver cancer, and having effective function of anti-tumor proliferation in the transplant model of tumor of nude mice lung cancer. The celastrol has a wide application prospect in treating lung cancer, head and neck squamous cell carcinoma, carcinoma of colon, gastric cancer, liver cancer, breast cancer and other cancer expressing CIP2A oncoprotein.

The invention discloses novel tripterine derivatives. Tripterine and the tripterine derivatives can inhibit tumor cell growth. The invention discloses a method for treating cancer, inflammation and central nervous system diseases by the tripterine and the tripterine derivatives.

The invention discloses application and a preparation method of tripterine. The tripterine can be used for preparing the drug for treating brain glioma. The preparation method of the tripterine comprises the following steps: (1) mixing and crushing the above-ground vine part and underground root part of Tripterygium wilfordii, carrying out reflux extraction with ethanol, filtering and concentrating at reduced pressure; (2) ultrasonically mixing and suspending the concentrated ethanol extract with ethanol-water, standing still and pouring out supernatant; (3) separating the supernatant with adsorbent resin, carrying out sequential gradient eluting with ethanol-water, and collecting eluate; (4) concentrating the eluate at reduced pressure, purifying by silica gel column chromatography, recovering solvent and drying to obtain red powdery extract; and (5) dissolving the extract with hot ethanol to obtain saturated or unsaturated solution, standing to precipitate red crystals and drying. Compared with the prior art, the method has the advantages of high raw material utilization rate, environmental friendliness, simpleness and low cost and is suitable for industrial production; in addition the purity of the prepared product is high.

The present invention provides a new type balloon dilation catheter which includes ballon and medication material coated on stent. Said medication material comes from one or two and more than two mixtures of heparin sodium, fiber degrading enzyme, serine proteinase, batroxobin, aspirin, genistein, hirudin and its recombined product, colchicine, sirolimus, biolimus, zotarolimus, tracrolimus, pimecrolimus, simvastatin, atorvastatin, pravastatin, ciclosporin, Anti-CD34, dexamethasone, bleomycin, plicamycin, daunomycin, mitomycin C, actinomycin D, taxol, celastrol, methopterin, 5-fluorouracil, cytarabine and 6-purinethol. The balloon is made of macromolecule nylon material, and the stimulation to blood vessel is far lower than the stent with metal structure.

The invention relates to the field of Chinese medicine preparation, in particular to a method for preparing tripterine nano structure lipid carrier containing traditional Chinese medicine monomer and application of the tripterine nano structure lipid carrier in preparation of transdermal drugs used for treating psoriasis, rheumatoid arthritis, skin cancer and breast cancer. The tripterine nano structure lipid carrier is characterized by comprising the following components in parts by weight: 1 part of tripterine, 5-100 parts of mixed lipid, 0.5-10 parts of phospholipid, 0.1-15 parts of poloxamer-188 and 0.5-10 parts of vitamin E and tocopherol polyethylene glycol succinate, wherein the mixed lipid is composed of solid lipid monoglycerine and liquid lipid octylic acid/caprin according to the weight ratio of 1: 0.1-10: 1. Tripterine is prepared into the nano structure lipid carrier, the tripterine nano structure lipid carrier in a semi-solid or liquid preparation form is applied in a transdermal way, bioavailability of the tripterine can be improved, toxic response of tripterine can be reduced, and the nano structure lipid carrier provided by the invention has great clinical application value in the improvement of the treatment effect of tripterine.

The invention provides a preparation method for celastrol derivatives, products and application thereof. The preparation method takes celastrol a microbial metabolic drug, and enables microorganisms to metabolize celastrol through a special elicitor, so that a plurality of high yield celastrol derivatives based on celastrol's hydroxyl, reduction or carboxylation and other substitution modification can be obtained at the same time. Being green and environment friendly, the method provided by the invention has strong selectivity and high yield, and can make large-scale use of microorganisms to prepare celastrol derivatives. The prepared celastrol derivatives have the characteristics of high efficiency and low toxicity, etc., and can practically be used for treatment of tumors, viral diseases and nerve injury diseases, thus providing broad application prospects for celastrol derivatives.

The invention discloses a method for extracting tripterine from celastrus orbiculatus root cortex, which uses celastrus orbiculatus root cortex powder as a raw material and comprises the steps of extraction, separation, purification and recrystallization. The extraction step comprises the following steps: firstly using low-level chloralkane as a solvent; heating, reflowing and extracting the solvent, wherein the quality ratio of the root cortex powder and the solvent is 1:(3-20), and the time is not less than 2 hours; desolventizing an extracting liquid to obtain an extractum-type primary extract; adding 50-70 percent by weight of methanol or ethanol solution into the primary extract; sufficiently stirring, standing and extracting; and desolventizing the extracting liquid to obtain a densepaste rough extract. The purification step comprises the following steps: dissolving the mathnol by using the rough extract; carrying out column chromatography separation and purification on a normalphase silica gel or a reverse phase silica gel by using a solid phase; collecting eluent; desolventizing and drying to obtain a powder refined extract; and finally carrying out recrystallization by using the mixed solvent of the ethanol and the water. The method has simple separation and purification processes so as to obtain the tripterine with the purity of 98 percent.

The invention provides a preparation method for celastrol, which relates to the preparation method for extracting, separating and purifying the celastrol from the root bark of celastraceae plants. The method is characterized in that the method improves the weakness of being incapable of separating high-purity celastrol of the traditional column chromatography method (LC), which can prepare the celastrol with more than 99 percent of purity and reduce the weakness of high-cost investment of the equipment and small preparation amount at a time of the current countercurrent chromatography (CCC) method. The method can be used in industry for producing the high-purity celastrol, which uses the technical characteristics of chloroform ultrasonic extraction, double-solvent elution silica gel column chromatography, component solvent recrystallization, and the like, and is characterized by high extraction rate, high purity, easy operation, safety, reliability, low cost, industrial suitability, etc. The prepared celastrol can reach the quality standard of bulk drug of national primary new drugs, which has the usages of scientific research, standard, etc.

The invention discloses a tripterine derivative, and a preparation method and a use thereof. The tripterine derivative has a structure represented by formula I; and in the formula I, R1 is H, an alkyl group, a halogenated alkyl group, an unsaturated alkyl group, a hetero atom-containing alkyl group or an aryl group, R2 is an alkyl group, a halogen, an alkyloxy group or a nitro group, and R3 is H or an alkyl group. In the preparation method of the tripterine derivative, an indolyl group or a substituted indolyl group is introduced to the 6 position of tripterine through a Friedel-Crafts reaction under mild reaction conditions. The tripterine derivative has the characteristics of high anticancer activity, low toxicity, small side effects and stable structure in the treatment of cancers.

The present invention relates to sexual reproduction of plant containing tripterine, and is especially seed reproduction process of celastraceae plant containing tripterine. The seed reproduction process including seed treatment, young seedling culture, small seedling culture and field planting in certain conditions is favorable to the growth of root system and the synthesis and accumulation of tripterine. The present invention provides artificial culture technology of plant containing tripterine, and can improve environment while developing wild plant resource.

The invention relates to a tripterine oral self-emulsification dispersible tablet and its preparation method, which is characterized by combining a self-emulsification process and a dispersible tablet process to realize the solubilization and solidification of insoluble drugs. The tripterine self-emulsification dispersible tablet can rapidly disintegrate, disperse and carry out self-emulsification after oral administration to form micro-emulsion droplets of which the particle diameter is 10-100nm, thereby the solubility and the dissolving rate of the tripterine can be substantially enhanced. The dispersible tablet is prepared by the following steps: mixing 1-15% of tripterine by mass fraction, 5-50% of oil phase, 20-70% of emulsifier and 0-50% of coemulsifier, adding a proper amount of solid adsorption material, uniformly mixing with other auxiliary materials to obtain the dispersible tablet. The tripterine self-emulsification dispersible tablet of the invention has the advantages that the dissolution of the medicine is effectively improved, the defects of liquid self-emulsification preparations in production, storage, administration and the like can be overcome, and the preparation process is simple and practicable.

The present invention relates to a tripterine capsule for preventing and curing the diseases due to nerve injury and its preparation method. Said capsule is made up by using natural tripterine whose purity is 98% as main raw material and adding natural mycose whose purity is 98% as auxiliary material through a certain preparation process. Said tripterine capsule can be mainly used for curing the diseases of Alzheimer's disease (AD), Parkinson's disease (PD), Huntington's disease (HD) and other diseases due to nerve injury.

The invention belongs to the field of pharmaceutical preparations and discloses celastrol flexible liposome which is composed of 1 part of celastrol, 1-4 parts of sodium cholate, 2-10 parts of cholesterol and 15-40 parts of egg yolk lecithin. The invention further provides a preparation method of celastrol flexible liposome, compound celastrol flexible liposome gel and a preparation method thereof. The celastrol flexible liposome obtained by the preparation method is ideal in production process operation, safety, particle size and encapsulation rate and high in physical stability; an obtained celastrol flexible liposome suspension can be directly used for preparing the compound celastrol flexible liposome gel without going through steps of separation and purification. In addition, the compound celastrol flexible liposome gel obtained by the preparation method has good heal promoting effect on rat scald wounds.

The invention belongs to the technical field of antitumor drug preparation, and discloses application of triptolide and tripterine combined medication in preparation of antitumor drugs. Through triptolide and tripterine combined medication, triptolide and tripterine have obvious synergistic effect in the dosage range of the invention, the curative effect is effectively improved, compared with a single component or simple curative effect superposition of two components, the curative effect is more remarkable, the destruction of tumor cells is improved; the dosage of each other can be effectively reduced, the toxic and side effect can be reduced, through triptolide and tripterine combined medication, the cost is saved, the economic burden of patients is reduced, and the a new way for prevention and treatment of cancer is provided, and the application prospect in the field of medicines is broad.

The invention relates to a liquid chromatography-tandem mass spectrometry test method of wilforlide, triptonide, triptolide and tripterine. The test method includes the following steps: taking liquid samples or tissue samples, cutting into pieces and placing into a tube with a stopper; adding a certain amount of a sodium hydroxide solution into the samples to adjust the pH to be 9-10, adding ethyl acetate, oscillating for 10 minutes, and performing high speed centrifugation for 10 minutes; after separation of an organic phase, adding an organic solvent for secondary extraction, mixing the two obtained organic phases, and placing on a concentrator with the temperature of 50 DEG C for evaporation until the organic phases are dried; using an initial mobile phase to dilute the residue, enabling the obtained solution to pass through a 0.22-[um]m microporous organic membrane, and taking the filtrate for analysis by a liquid chromatography-tandem mass spectrometer. The test method provided by the invention is simple, efficient, quick, sensitive, high in accuracy and extensive in practicability, can be applied to qualitative and quantitative testing for wilforlide, triptonide, triptolide and tripterine in biological samples, and is suitable for tests on in-vitro samples and suspicious physical evidences.

The invention relates to a preparation method of tripterine, and the method comprises the following steps: crushing triperygium wilfordii roots, adding 5-7 times amount of 85-90% alcohol, refluxing for 2-3 times, and decolorizing the extracting solution by virtue of active carbon; recycling the alcohol from the destaining solution until the alcohol concentration is 55-65%, standing the destaining solution to precipitate, filtering out precipitates, dissolving the precipitates in 5-7 times amount of an alkaline alcohol solution, filtering out insolubles, adjusting the pH value of the filtered solution to 3-5, standing the solution to precipitate, filtering out precipitates, dissolving the precipitates in 3-5 times amount of the alkaline alcohol solution, filtering insolubles, adjusting the pH value of the filtered solution to 7, standing the solution to precipitate, filtering out precipitates, adding ethyl acetate into the precipitates to reflux and dissolve the precipitates, filtering the dissolvent solution, standing the filtered solution to crystallize, filtering out the crystal, adding 90-95% alcohol into the crystal, refluxing and dissolving the crystal, decolorizing the crystal alcohol solution by the active carbon, insulating and crystallizing the decolorized solution, finally drying the obtained crystal to obtain the tripterine pure product. The preparation method of the tripterine is convenient and simple, the impurity of the obtained product is high, the toxicity of used reagents is small, and the preparation method of the tripterine is suitable for industrial production.

The invention belongs to the field of biomedical-material-and-medical crossover, and particularly discloses an application of celastrol to preparing an eye drop preparation for inhibiting alkali burn corneal neovascularization and promoting corneal alkali burn healing. 7.04 g-67.55 g of triblock copolymer PEG-PCL-PEi and 0.68 g-2.11 g of the celastrol are weighed and jointly dissolved into a mixed solvent prepared from methyl alcohol and acetonitrile in the volume ratio of 1:(1-3); under ultrasonic stirring, mixed liquid is dropwise added into dissolving equivalent amount of injection water, an organic solvent is removed in a vacuum-distillation mode, dissociative celastrol is removed in an ultra-filtration mode, a medicine loading polymeric micelle is obtained, injection water is additionally added till the volume is fixed to be 100 mL, and eye drop is obtained. According to the celastrol, the PEG-PCL-PEi firstly serves as a carrier, and loads the celastrol, the eye drop is prepared, the medicine feeding mode of eye-surface dropping is achieved, and the celastrol has the milepost-type significance.

The invention discloses a silk fibroin nanoparticle. The silk fibroin nanoparticle contains silk fibroin and an active drug, wherein the silk fibroin loads the active drug, and the active drug is selected from triptolide and tripterine. The invention also discloses a preparation method and application of the silk fibroin nanoparticle. The silk fibroin nanoparticle improves the water solubility of the triptolide and tripterine and can resist to proliferation of cancer cells more effectively; and meanwhile, combined utilization of a silk fibroin nanoparticle loading triptolide (TPL-SFNPs) and a silk fibroin nanoparticle loading tripterine (CL-SFNPs) can synergistically inhibit the growth of the cancer cells, and effect is significant, so that the silk fibroin nanoparticle has good application prospects in treatment of cancers, especially pancreatic cancer.

The invention relates to a triterpene synthase of tripterygium wilfordii TwOSC1 protein and an encoding gene thereof. A recombinant expression vector with a Twosc1 gene is constructed by cloning cDNAof the Twosc1 gene onto a eukaryotic expression vector pYES2, and then the recombinant expression vector is shifted to yeast expression host bacteria, so as to acquire some triterpenoids, such as friedelin and amyrin. A mutation research result shows that amino acids 486 and 502 encoded by the Twosc1 gene are key sites, and the yield of friedelin or amyrin can be increased or reduced; a gene gun mediated interference experiment shows that the interference of the Twosc1 gene has an obvious inhibiting effect on the synthesis of celastrol in the tripterygium wilfordii; through further experiments, a gene gun mediated overexpression experiment shows that the overexpression of the Twosc1 gene can increase the yield of the celastrol in tripterygium wilfordii suspension cells; the TwOSC1 proteinand the encoding gene thereof provided by the invention can be used for biosynthesizing plant triterpenoids and cultivating high-quality tripterygium wilfordii.

The invention discloses a tripterine nanostructure lipid carrier modified by lentiviral vector and preparation method and application thereof, wherein teh tripterine nanostructure lipid carrier modified by the lentiviral vector consists of tripterine and a lipid carrier, various components comprise 1 part by weight of tripterine, 0.5 to 10 parts by weight of lentiviral vector, 5 to 100 parts by weight of lipid blends, 0.5 to 20 parts by weight of emulsifier and 5 to 100 parts by weight of stabilizer. The tripterine nanostructure lipid carrier modified by the lentiviral vector can increase nanoparticles encapsulating rate to 78-90%. The tripterine nanostructure lipid carrier modified by the lentiviral vector uses oral administration, thereby promoting absorbing of the tripterine in a body,improving bioavailability, reducing administration dosage, reducing accumulation of the tripterine in the body at last, reducing toxic reaction by combining sustained release of a nanostructure lipidcarrier, and improving clinical therapeutic effect of the tripterine at last.

The invention discloses a method for separating and purifying tripterine from a medicinal material celastrus orbiculatus, which comprises the following steps: (1) acquiring a concentrated solution from the medicinal material celastrus orbiculatus, stirring with silica gel, and drying into dispersed granules to obtain the granular raw material for later use; (2) adding silica gel in a dichloromethane-methanol solution, packing by a wet process, and balancing the separation column with the dichloromethane-methanol solution; after well balancing, feeding the granular raw material; carrying out gradient elution with an eluting agent, wherein the eluting agent is composed of a dichloromethane-methanol solution and ammonia water, and a small amount of anhydrous sodium sulfate is also added into the eluting agent with remove water in the eluting agent; collecting the eluate to obtain a tripterine crude solution; recovering the eluting agent under reduced pressure to obtain a tripterine pure product; and washing the tripterine pure product with methanol or anhydrous ethanol to obtain the tripterine monomer. By using the dichloromethane-methanol solution and ammonia water for elution, the invention has the advantages of simple technique, high efficiency, environment friendliness, high yield and high production rate, and is suitable for industrial production.

The invention relates to a new method for rapidly preparing a highly pure tripterine chemical reference substance from Common Threewingnut Root. The tripterine chemical reference substance with the purity of above 98% can be obtained through ethanol extraction of a Common Threewingnut Root medicinal material, ethyl acetate extraction, silica gel column chromatography, high performance chromatographic separation and gel purification. The method has the advantages of simple steps, easy large-scale production and high purity.

The invention belongs to the fields of biotechnology and medicine, and relates to an inhibitor capable of inhibiting the excessive proliferation of keratinocytes, an inhibitor composition, and applications of the inhibitor. The inhibitor taking triptolide, triptonide or tripterine as the representative can inhibit the excessive proliferation of the keratinocytes, specifically, the expression levels of STAT1 and p-STAT1 can be inhibited, then the expression level of miR-17-92mRNA is down-regulated, then, miR-17-92 target gene CDKN2B is regulated, the secretion levels of inflammatory factors CXCL1, CXCL10, CXCL16 and IL-6 in cells are inhibited, and finally, the cell cycle progression and immune function abnormity are inhibited; triptolide, tripterine and triptonide can effectively inhibit the proliferation of the keratinocytes, and the effective doses respectively achieve 60nM, 100nM and 80nM.