172 results about "Tripterine" 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 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 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 provides compounds of formula I:

or a salt thereof. The invention also provides pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods using the compounds of formula I.

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.

Triptolide derivatives and application thereof relate to triptolide. Triptolide and the derivatives thereof has different-degree anticancer activity on HepG2 cell and MCF-7 cell. A method for using tRXRalpha and RXRalpha to evaluate the anticancer activity and toxic and side effects of triptolide and the derivatives thereof is firstly provided. The triptolide and the derivatives thereof are confirmed to have the anticancer activity closely related to the tRXRalpha protein expression lowering capacity, and the stronger rRXRalpha lowering capacity, the higher anticancer acitivty. Also the technical scheme firstly confirms that reduction of the toxic and side effects of the triptolide derivatives is related to the stability of normal-cell full-length RXRalpha protein, and the stronger protection effect of the derivatives on full-length RXRalpha, the smaller toxic and side effects.

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 provides an endophytic fungus for producing triptolide. The endophytic fungus is a Penicillium steckii strain NS-12 and is collected in China General Microbiological Culture Collection Center, and the collection number is CGMCC No. 4928. Fermentation culture conditions for producing the triptolide by using the endophytic fungus are that: a potato dextrose agar (PDA) liquid culture medium (the liquid loading capacity is 100ml/500ml) is used, the shake culture is performed by a shaker at the rotating speed of 150r/min, the culture temperature is 28 DEG C, and the culture time is 72 to 144h. Through suspension culture, the strain can secrete a considerable amount of triptolide out of cells in a short time; the method is remarkably superior to an acquisition way of the traditional plant cultivation; and the strain has good industrialized application prospect.

The invention discloses common threewingnut root sesquiterpene synthase TwNES as well as a coding gene and application thereof. According to the common threewingnut root sesquiterpene synthase TwNES as well as the coding gene and application thereof disclosed by the invention, a Twnes gene is obtained by cloning common threewingnut root suspension cells, and this gene is a key enzyme gene which is acquired from common threewingnut root for the first time and is synthesized by sesquiterpenoids components. Proved by experiments, TwNES protein disclosed by the invention not only can catalyze FPP to form nerolidol ((E)-nerolidol), but also can catalyze GGPP to form geranyl linalool ((E, E)-geranyllinalool), plays an important role in the synthesis of sesquiterpenoids alkaloids in common threewingnut root, and also has important theoretical and practical significance in the adjustment and production of plant sesquiterpenoids compounds and in the cultivation of high-quality common threewingnut root.

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.

The invention relates to the technical field of medicines, in particular to a targeting inducible nitric oxide synthase (iNOS) triptolide prodrug, and a preparation method and application thereof. R1of the triptolide targeting prodrug is L-arginine, L-arginine methyl ester, L-Nomega-NO-arginine, L-N omega-NO-arginine methyl ester, L-proline, L-citrulline, L-thiocitrulline or L-ornithine. The highexpression characteristic of the inducible nitric oxide synthase (iNOS) at an inflammatory site is utilized, and the triptolide is semi-synthesized by an iNOS specific substrate (group) to prepare the prodrug, the toxicity of the triptolide is reduced and the bioavailability are improved through the targeting property of the prodrug, the anti-inflammatory effect is significantly better than thatof the triptolide, and the triptolide can be effectively developed and utilized.

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 present invention relates to one kind of compound triptolide alcohol preparation for being injected into articular cavity to treat osteoarthritis. It includes triptolide alcohol solution of 1*10<-4> to 5*10<-2> mg/ml concentration and gel liquid mixed in the volume ratio of 1 to 1-9. It has medicine slow releasing effect, and this can prolong the action period of medicine, reduce consumption of triptolide alcohol and lower the toxic side effect of the medicine. It can inhibit the further development of osteoarthritis in early and middle phase, improve the environment inside the joint and promote the regeneration and repair of articular cartilage to reach the aim of cure osteoarthritis.

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 relates to the field of traditional Chinese medicine extract, and particularly discloses application of tripterygium wilfordii root extract triptophenolide (CAS number:74285-86-2) as an androgen receptor antagonist and application of triptophenolide to preparation of drugs for treating androgen disorders and drugs for male contraception. A reliable androgen activity screening method is constructed, the inhibiting effect of various kinds of traditional Chinese medicine extract on androgen receptor activity is tested, and finally it is found that the tripterygium wilfordii root extract triptophenolide is a novel androgen receptor antagonist and can inhibit activity of wild type and mutability androgen receptors. Further, anti-prostrate-cancer activity of triptophenolide is tested, and it is found that triptophenolide has good activity for AR (androgen receptor) positive prostrate cancer cells such as LNCaP and 22 RV1.

The invention discloses medicine composition for treating a fish gill rot disease and the medicine composition comprises the following traditional Chinese medicines in parts by weight: 10-30 parts of thunder god vine, 10-20 parts of gallnut, 15-30 parts of humifuse euphorbia herb, 5-10 parts of chinaberry leaf, 10-25 parts of houttuynia cordata and 5-15 parts of greater celandine herb. The invention further discloses a preparation method of the medicine composition. The humifuse euphorbia herb, chinaberry leaf and houttuynia cordata in the medicine composition have the efficacy of bacteria resistance and bacteriostasis and can better prevent and treat the fish gill rot disease as effective constituents. According to the preparation method, the supercritical CO2 extraction method is adopted to extract effective constituents in the thunder god vine, so that the activity and content of each of triptolide, tripterine and total alkaloids are maintained and higher. The preparation method is simple and practical, and the medicine composition is suitable for large-scale production.

The invention belongs to the field of medicines, and discloses a tripterine derivative and a preparation method and application thereof. The tripterine derivative is coupled with dipeptide on 29-position carboxylic acid of tripterine through formation of amido bonds, and carboxyl of the dipeptide is connected with tert-butyl. According to the tripterine derivative, the cytotoxicity of tripterine can be reduced, the stability is improved, and the selectivity to tumor cells is enhanced, so that the practical application value of tripterine as an anti-cancer component is improved.

The invention belongs to the field of biotechnology and medicine and relates to an inhibitor capable of inhibiting a killing effect of CD8<+>T cells on melanocytes, inhibitor composition and an application to vitiligo preventing and treating drugs. When dose of triptolide, celastrol or wilforlide A are in 5-10 nM, the inhibitor capable of inhibiting the killing effect of the CD8<+>T cells on the melanocytes can inhibit the expression level of STAT1 (signal transducer and activator of transcription 1) in keratinocytes, then the expression level of IRF1 is down-regulated, secretion of CXCL10 and CXCL16 in the keratinocytes is inhibited, and chemotaxis of CXCL10 and CXCL16 on the CD8<+>T cells is further reduced, so that the killing effect of the CD8<+>T cells on the melanocytes is inhibited; the inhibitor capable of inhibiting the killing effect of the CD8<+>T cells on the melanocytes is a tripterygium wilfordii terpenoid and particularly is triptolide, celastrol or triptonide.