367 results about "Triptolide" patented technology

The present invention is triptolide alcohol derivative, its pharmaceutically acceptable salt and optical isomer, their synthesis process and the application as antiphlogistic, immunological regulator and relevant disease treating agent.

Compounds useful as immunosuppressive, anti-inflammatory and anticancer agents and methods of their preparation and use are described. The compounds are analogs or derivatives of triptolide and related compounds, modified at the 5- and / or 6-position relative to the naturally occurring compounds.

Inflammatory disorders, including obliterative airway disease, renal fibrosis, diabetic nephropathy, and liver fibrosis are treated with immunosuppressive triptolide compounds, in particular triptolide compounds effective to inhibit TGF-β production in a patient afflicted with such a disorder.

A method for studying toxicity of drugs by using model organism zebra fish comprises the following steps of: selecting 100 to 200 adult zebra fishes, respectively disposing in bottles containing a solution of 30 to 50 mL, keeping the temperature in the bottles substantially constant at 22 to 25 DEG C, randomly grouping, each group containing 10 to 20 fishes, wherein the solution in one of the groups is pure water (blank), the solutions in other groups are medicinal solutions with different concentrations, and 0.5% to 2% dimethylsulfoxide (DMSO) can be added to assist dissolving a drug that has poor water solubility, when an additional solvent comparison group prepared by adding 0.5% to 2% DMSO into the pure water is needed; recording the death number of zebra fishes in the medicinal solutions of different concentrations within 24 h, and calculating the death rate (%); calculating median lethal dose-LD50 by Bliss method according to the experiment result; and representing the acute toxicity by the value of LD50. According to the method, the LD50s of zebra fish of triptolide, matrine and emodin are respectively 5.39*10<-3>, 112.3 and 1.08*10<3> mug / mL. The method can objectively reflect the toxicity of drugs.

The invention relates to a triptolide nano lipsome gelling agent of external use and its preparation method, which comprises externally used gelling agent composed of 10-70% of triptolide alcohol nano liposome turbid liquor and 90-30% of blank gel, wherein the weight ratio content of the triptolide alcohol in the total gelling agent is 0.1-2.0%, and the triptolide alcohol alcohol nano liposome turbid liquor comprises 0.7-4.2% of triptolide alcohol, 14-64% of phosphatides, 3.5-16% of cholesterin, 0.7-3.2% of anti-oxidant, 0.7-3.2% of surface active agent, and hydration medium. Its preparing process is also disclosed in the invention.

Compounds and methods for use in immunosuppressive and anti-inflammatory treatment are described. The compounds are triptolide analogs with improved water solubility and low toxicity.

In certain aspects, the invention relates to use of PKD2 agonists, such as triptolide and triptolide derivatives, to regulate calcium release. In other aspects, the invention relates to use of PKD2 agonists to treat or aid in the treatment of any condition in which a calcium channel, such as the gene product of PKD 1 and / or PKD2, is mutated; calcium signaling is abnormal; or both, such as polycystic kidney disease.

The invention provides a preparation method of triptolide and ramification and composition of the triptolide. After an elicitor plays a role in tripterygium suspended cell sap, a high yield of triptolide and ramification of the triptolide can be gotten. The extractive gotten by the method has a good effect on inhibiting tumors, a hepatitis b virus and a human immunodeficiency virus (HIV); the extractive can be prepared into soft capsules, or hard capsules, or dropping pills or troches, or dispersible tablets, or granules, or injection, or oral liquid, or suppository which are applied in oral or skin or mucous membrane or rectal way, by that the extractive is used for being solely or being matched with other drugs or adding auxiliary materials which can be acceptable in pharmacy.

The invention provides four triptolide derivatives and a preparation method of corresponding agents, which uses triptolide as raw material, via acylation and nucleophilic substitution to obtain triptolide derivative to be reacted with acid or alkyl halide to obtain a corresponding salt which can be added with one or more pharmaceutically acceptable adjuvants to prepare relative agent-freeze-driedpowder.

The invention discloses a method for separating triptolide from thunder god vine leaves. Thunder god vine leave powders are extracted by ethanol, the ethanol is firstly distributed by an ethyl acetate-water system, the top phase is steamed to obtain ethyl acetate extractive matter, the extractive matter is then distributed by a sherwood oil- methanol system, and the bottom phase is steamed to obtain methanol extractive matter. The sampling amount of column chromatography step is reduced by the twice distribution. The eluent is steamed by simple column chromatography to obtain the crude product of triptolide, the crude product of triptolide is distributed by a quaternionic biphase system, impurities such as coloring matter, and the like are removed, the sampling amount of high-speed reverse-current coloring matter step is reduced, and the competitive product of triptolide is obtained by refining high-speed reverse-current coloring matter. The purity of the competitive product of triptolide is about 95%, and the yield is 0.008% higher than leaves. The solvent in the method does not contain chloro-solvent which is harmful to environment and human bodies.

The present invention discloses a technique for separating out and purifying triptolide monomer from common threewingnut root. The technique is carried out according to the following technical steps: (A) heating and extraction: after ethanol or methanol is warmly soaked, dregs are removed; (B) solvent extraction: organic solvent is adopted to extract concentrated solution in order to enrich the product; (C) chromatographic column chromatography: with neutral alumina or silica gel as filler, dichloromethane-methanol or chloroform-methanol is used to carry out gradient elution, and cut fraction is collected by stages; (D) high-efficiency preparation and liquid phase separation; (E) crystallization: two-phase solvent crystallization is adopted to use petroleum ether-ethyl acetate, dichloromethane-methanol or methylene dichloride-ethyl acetate to crystallize the cut fraction collected by stages, so that the colorless spiculate crystal product of triptolide, the purity of which reaches over 99.5 percent, can be obtained. The technique, which has the advantages of simplicity, rapidness, little solvent consumption, economy, environment-friendliness and high yield, can prepare a large amount of the product for one time, thus having high economic and academic values.

Methods for extraction, isolation, and purification of therapeutically useful compounds from Tripterygium wilfordii are described. Extraction steps employing aqueous base and a hydrocarbon solvent, respectively, are found to increase the efficiency of the process and reduce the amount of material that must be removed by chromatography.

The invention provides an efficient and non-toxic broad-spectrum insectofungicide as well as a preparation method and a use method thereof. The insectofungicide comprises the following components in parts by weight: 100 parts of water, 15-23 parts of alkaloids from tripterygium wilfordii, 1-5 parts of triptolide, 5-10 parts of omphalin, 3-8 parts of chamaejasmine, 8-20 parts of nicotine, 4-8 parts of capsaicine, 1-2 parts of suberosin and 1-3 parts of benzylpenicillin sodium, wherein the alkaloids from tripterygium wilfordii are extracted from roots, stems and leaves of tripterygium wilfordii; the triptolide is extracted from the root of tripterygium wilfordii; the omphalin is extracted from omphalialapidescens sclerotium; the chamaejasmine is extracted from stellera chamaejasme L.; the tobacco stalk cellulose is extracted from the branches and leaves of the tobaccos; the capsaicine is extracted from the capsicum fruits; and the suberosin contains sanshool and sanshoamide and is extracted from the pepper fruits. The insectofungicide is non-toxic and harmless to human and livestock, does not pollute the environment and the crops and has no toxic residues. The product has the effectof controlling the diseases and insect pests of the crops, fruit trees and vegetables.

Compounds having the structure I: are useful for inducing cell death (apoptosis) and in immunosuppression. In structure I,CR1R2 is selected from CHOH, C═O, CHF, CF2 and C(CF3)OH;CR6 and CR13 are selected from CH, COH and CF;CR7R8, CR9R10 and CR11R12 are selected from CH2, CHOH, C═O, CHF and CF2; andCR3R4R5 is selected from CH3, CH2OH, C═O, COOH, CH2F, CHF2 and CF3;such that: at least one of R1-R13 comprises fluorine;no more than two of CR3R4R5, CR6, CR7R8, CR9R10, CR11R12, and CR13 comprises fluorine or oxygen;and, when CR1R2 is CHOH, CR3R4R5 is not CH2F.

Compounds having the structure I: are useful for inducing cell death (apoptosis) and in immunosuppression. In structure I, R1 is H or R, R being selected from lower alkyl, alkenyl, alkynyl, and allenyl, or, R1 together with R2=O (oxo); R2=OH, or, R1 and R2 together=O (oxo); CR3R5 and CR4R6 are selected from CH2, CHOH and CROH; at least one of R1, R5 and R6 is R; and at least one of CR3R5 and CR4R6 is CH2.

The invention discloses insect and mould inhibitor and application thereof. The insect and mould inhibitor is characterized by comprising 0.01-10% of acting agent, 5-95% of dissolving agent, 1-40% of stabilizing agent, 1-20% of infiltration aid and 1-30% of fixed film forming agent, wherein the acting agent is thunder god vine alkaloids or(and) triptolide. The acting agent is a green and natural plant active component, is far higher than other synthetic poisonous preparation in human settlement compatibility, and has incomparable environmental protecting performance; and meanwhile, the acting agent is from the plant of thunder god vine, is better in formula compatibility, is added with the stabilizing agent, the infiltration aid and the fixed film forming agent for providing the basic guarantee to the excellent performance of the product, and can serve as the insect and mould inhibitor to be applied to woods and wood products.

Compounds having the structure I:are useful for inducing cell death (apoptosis) and in immunosuppression. In structure I,CR1R2 is selected from CHOH, C═O, CHF, CF2 and C(CF3)OH;CR6 and CR13 are selected from CH, COH and CF;CR7R8, CR9R10 and CR11R12 are selected from CH2, CHOH, C═O, CHF and CF2; andCR3R4R5 is selected from CH3, CH2OH, C═O, COOH, CH2F, CHF2 and CF3;such that: at least one of R1-R13 comprises fluorine;no more than two of CR3R4R5, CR6, CR7R8, CR9R10, CR11R12, and CR13 comprises fluorine or oxygen;and, when CR1R2 is CHOH, CR3R4R5 is not CH2F.

The invention discloses fifteen new triptolide derivatives, a medicinal composition containing one or more of the derivatives, and uses of the derivatives in the inhibition of the generation of NO by macrophages, especially anti-inflammation and immunological suppression, as medicines. The above compounds treat triptolide as a raw material, the fourteenth hydroxy group of triptolide and aromatic groups comprising benzoic acid, cinnamic acid and benzene sulfonic acid analogs are acylated to form ester derivatives. Active evaluation shows that the compounds have substantial inhibition activities on the generation of the inflammation factor NO by the macrophages.

The invention provides a target hydrophilic polymer-triptolide conjugate (I), wherein P represents a water-soluble polymer; D represents triptolide; T represents a target molecule; and L and Z represent linking groups. The conjugate improves water solubility of triptolide, reduces toxicity of triptolide and prolongs circulating half-life period of triptolide in a living body.

The present invention relates to the following water-soluble triptolide derivatives with immunosuppression activity. Said invention provides their structure formulas and their synthesis method, and their application for curing acive immunodeficiency disease and immunosuppression associated inflammation.

The invention relates to the technical field of honey identification, in particular to a method for identifying presence of tripterygium glycoside honey in honey. Particularly, the application finds out that triptolide can be applied to identification of the tripterygium glycoside honey as a feature identification material. The invention provides a method for identifying the honey by LC-Q-TOF or LC / MS / MS on this basis, and specific detection conditions are optimized. The method for identifying the tripterygium glycoside honey is firstly constructed and is of important significance in consumption safety of the honey.

The invention discloses a tripterygium wilfordii diterpene synthase TwGES1 and an encoding gene and application thereof. Twges1 genes are obtained through cloning from tripterygium wilfordii suspension cells; and the genes are key enzyme genes obtained through synthesis of diterpene components from tripterygium wilfordii. Experiments prove that TwGES1 proteins can catalyze GGPP to form geranyl linalool ((E, E)-geranyl linalool), can catalyze FPP to form nerolidol ((E)-nerolidol), not only have important significance on biological synthesis of such diterpene compounds as triptolide in the tripterygium wilfordii and but also have important theoretical and practical significance on adjustment and production of plant diterpene compounds and cultivation of high-quality tripterygium wilfordii.

The invention discloses a method for extracting triptolide from tripterygium wilfordii, which is characterized in that dried tripterygium wilfordii rootstocks are compressed by chloric alkane for extraction. The method comprises the steps that: the dried tripterygium wilfordii rootstocks and the alkane are mixed according to a certain material-liquid ratio and put into a compressing reaction kettle for extraction; solid maters and fluid matters in the mixture obtained by the extraction are separated to obtain an extract solution; after being put together, the extract solution is decompressed and concentrated to obtain triptolide crude products. The operating technology is mainly characterized by simple operation, smooth processes, recyclable reagents, small energy consumption, low production cost, high yield and high purity.

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 discloses a polyene high-oxidation androstane compound, i.e., androstane-4, 6, 8 (9), 13 (14)-tetraene-3, 11, 16-triketone. The compound is extracted from epigynum auritum plant. Experiments prove that the compound has an obvious suppression effect on Balb / c mouse spleen lymphopoiesis stimulated by ConA (concanavalin) and has activity equivalent to that of the conventional immunosuppression active substances, i.e., triptolide and dexamethasone.

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 present invention discloses a breast cancer treatment triptolide liposome preparation and a preparation method thereof, wherein the breast cancer treatment triptolide liposome preparation is a liposome preparation prepared from a breast cancer treatment traditional Chinese medicine active effective component triptolide. The preparation method comprises: adopting an ethanol injection method to prepare liposomes to obtain the breast cancer (breast cancer and triple-negative breast cancer) treatment triptolide liposome preparation. According to the breast cancer treatment triptolide liposome preparation, in vivo animal anti-cancer pharmacological experiment results show that: significant growth inhibition effects are provided for breast cancer and triple-negative breast cancer, and anti-cancer activity of the breast cancer treatment triptolide liposome preparation is respectively and significantly higher than anti-cancer activities of chemotherapy drugs such as paclitaxel and cisplatin. In addition, the triptolide liposome preparation provides a higher anti-cancer effect than the triptolide non-liposome preparation.