76 results about "Tripterine" patented technology

The invention relates to the technical field of extraction and separation of compounds in traditional Chinese medicinal materials, in particular to a method for simultaneously separating and purifying three pentacyclic triterpenoids from a tripterygium hypoglaucum root medicinal material. Three pentacyclic triterpenoid monomers are obtained through the steps of smashing, reflux extraction, normal-phase silica gel chromatography, reversed-phase high-pressure column chromatography, recrystallization and the like, the method is high in extraction efficiency and small in reagent dosage, the three pentacyclic triterpenoid compounds can be obtained at the same time, and the obtained compounds are high in purity and yield, have high social and economic value and are suitable for industrial production. The purity of the obtained plasmin, tripterine and demethylzeylasteral is high, and a foundation is laid for the preparation and production of reference substances of triterpenoid components in the roots of pyracantha fortunei, the subsequent pharmacological activity and the development of new immune drugs.

The invention discloses a tripterine-sophocarpidine self-assembled nanoparticle and application thereof in preparation of an anti-tumor drug, and belongs to the field of biological medicine. The nanoparticles are formed by self-assembly of the tripterine and the sophocarpidine through supramolecular interaction, the molar ratio of the tripterine to the sophocarpidine is 1: 1-1: 3, and the self-assembly system effectively solves the problems of low Cst solubility, poor bioavailability, rapid in-vivo removal and the like; the inhibition effect on triple negative breast cancer (TNBC) is remarkably enhanced through the synergistic effect of Cst and Mar, and a new strategy is provided for expanding the application of a traditional Chinese medicine carrier-free self-assembly nano drug delivery system in the anti-tumor field.

The invention belongs to the technical field of pet products, and particularly discloses a novel anthelmintic based on fipronil drops, which can effectively reduce the bacterial or fungal infection caused by parasites on the body surface or skin of pets by combining the antibacterial effects of fipronil, citronella extract and tripterygium wilfordii. The fipronil can quickly kill parasites, the citronella extract can further reduce breeding and contact of the parasites through a repelling effect, so that the overall effect of the medicine is accelerated, the citronella extract further reduces the secondary infection risk caused by the parasites by inhibiting growth of bacteria, and the tripterine further reduces the secondary infection risk caused by the parasites by inhibiting pathogenic microorganisms of skin. Through the synergistic effect of multiple components, the development of drug resistance of parasites to a single component can be reduced.

The invention discloses a tripterine acrylamide derivative with a structure shown as a formula III, wherein A1 and A2 are respectively and independently selected from O and NH; l is selected from-(CH2) n-and-((CH2) 2O) m (CH2) 2-, n is an integer ranging from 2 to 6, and m is an integer ranging from 1 to 6; r1 and R2 are respectively and independently selected from H, # imgabs0 # R3 and R4 are respectively and independently selected from C1-C4 alkyl, or R3 and R4 are connected with each other to form a 5-7-membered heterocyclic ring containing one oxygen atom together with an oxygen atom, or R3 and R4 are connected with each other to form a 5-7-membered heterocyclic ring together with a nitrogen atom. Compared with tripterine, the tripterine acrylamide derivative disclosed by the invention has the advantage that the inhibition effect of the tripterine acrylamide derivative on tumor cells is obviously enhanced. The invention also discloses an application of the tripterine acrylamide derivative in preparation of antitumor drugs. # imgabs1 #

The invention discloses an application of tripterine in preparation of an anti-esophageal cancer drug. The tripterine or the pharmaceutically acceptable salt thereof provided by the invention can be used for preparing medicines for preventing or treating esophageal cancer. The tripterine is adopted to achieve the effects of inhibiting proliferation of esophageal squamous carcinoma cells, inducing apoptosis of the esophageal squamous carcinoma cells, reducing the size of esophageal tumors and being small in side effect.

The invention specifically discloses a beta-diketone iridium complex as well as a preparation method and application thereof, and relates to the technical field of biological medicines. The beta-diketone iridium complex provided by the invention has high phototoxicity and low dark toxicity, can be applied to tumor cells as effective PSs of PDT, and is specifically delivered to the tumor cells by taking a traditional Chinese medicine monomer tripterine as a supplement in combination with a nano-targeting delivery technology for photodynamic / immune synergistic treatment of hypoxic tumors.

The invention discloses a novel application of tripterine in anti-inflammatory treatment of severe influenza A virus infection. The invention relates to a novel application of tripterine in anti-inflammatory treatment of severe influenza A virus infection, and discloses that tripterine can effectively inhibit inflammatory response caused by severe influenza A virus infection and reduce pathological injury of lungs without affecting antiviral immune response.

The application discloses a tripterine self-assembled nanoparticle microsphere, a preparation method and application thereof, and belongs to the technical field of biological medicines. The tripterine self-assembled nanoparticle microsphere takes tripterine self-assembled nanoparticles as a drug core, is formed by cross-linking of a sodium alginate-pectin composite carrier through calcium ions, can significantly improve drug solubility, realizes stable protection and intestinal targeting rapid release in the gastrointestinal tract, and effectively reduces drug systemic exposure and side effect risks. The preparation process is mild and simple, the obtained preparation has high targeting and safety. Pharmacodynamic results show that the microsphere can obviously improve liver steatosis, inflammation and fibrosis related to metabolic-related fatty liver hepatitis, and has better curative effect than conventional preparations. The application provides a novel oral delivery system for preventing and treating metabolic-related fatty liver hepatitis, and has good industrial and clinical transformation prospects.

The invention discloses a protective agent for lung injury caused by intestinal ischemia reperfusion, and relates to the technical field of lung injury protective agents. The method comprises the following steps: step a: a synthesis step: S1, a purification process of tripterine: stirring an obtained concentrated solution with silica gel, fully mixing the silica gel and the concentrated solution, and drying into dispersed particles to obtain a granular raw material for later use; verification is carried out by establishing a cell model and a biological model, lung cell coking can be effectively relieved, the lung can be protected against oxidative stress injury, when the biological model is modeled, an intestinal ischemia reperfusion injury model is established for a mouse by utilizing an active modeling operation, clinical lung injury conditions are simulated, and the model is used for simulating the lung injury condition. The tripterine derivative is given through oral administration or intravenous injection, and it is verified that the tripterine derivative has the effects of inhibiting lung cell coking, preventing cells from releasing histidine and various inflammatory mediators and avoiding further aggravation of inflammatory response and cell damage.

The application discloses a triazol derivative of tripterine or a pharmaceutically acceptable salt thereof, and a structure of the triazol derivative of tripterine is shown in formula III, R is selected from R1 and R3, R1 and R3 are independently selected from H, C3-C4 alkyl, halogen and R2, R2 is selected from H and C1-C4 alkyl, R4 is selected from H and C1-C4 alkyl, and n is an integer from 1 to 5. The triazol derivative of tripterine has obvious inhibiting effect on the proliferation of various tumor cells, and is obviously superior to tripterine. The application discloses a use of the triazol derivative of tripterine or the pharmaceutically acceptable salt thereof in preparation of an Hsp90 protein inhibitor. The application discloses a use of the triazol derivative of tripterine or the pharmaceutically acceptable salt thereof in preparation of an antitumor drug.

The application discloses a triptolide nano-micelle, a synthesis method and application thereof. The nano-micelle is formed by self-assembly of triptolide, metal ions and a modular functional polymer through metal coordination; and the high molecular polymer is covalently connected by a metal coordination group R1, a hydrophilic polymer main chain R2 and a functional end-capping group R3. The application constructs a micelle system by relying on the coordination of three components without an exogenous carrier, avoids potential biological safety risks accompanied by traditional nano-carriers, reduces the complexity of the synthesis process of the medicament, and significantly improves the storage stability of the preparation after freeze-drying. The obtained micelle has good water solubility, can be quickly reconstituted after freeze-drying without a freeze-drying protective agent, has an ATP response drug release characteristic in a tumor microenvironment, and can be used for antitumor drug delivery.

The invention relates to a composite hydrogel slow-release adhesive as well as a preparation method and application thereof, and relates to the technical field of natural high polymer materials. The preparation method comprises the following steps: (1) dissolving tripterine with a solvent to obtain a tripterine solution; (2) mixing the tripterine solution with a polyethyleneimine aqueous solution, and carrying out ultrasonic emulsification to obtain a tripterine-polyethyleneimine nano suspension; and (3) adding a hydrogel material into the tripterine-polyethyleneimine nano suspension, so as to prepare the hydrogel slow-release adhesive. According to the preparation method disclosed by the invention, a novel medicine carrying material for effectively repairing the infected wound surface by carrying the tripterine is realized, the medicine is continuously applied to act on the infected wound surface, and the tripterine is lastingly and slowly released to repair the infected wound surface while the wound surface is effectively protected and ulcerative focuses are sealed.

The invention provides a tripterine sulfated metabolite and application thereof in preparation of a medicine for resisting rheumatoid arthritis, and belongs to the technical field of biological medicine. The tripterine sulfated metabolite is 10-sulfated tripterine which is formed by connecting a HSO3 <-> to the 10-position carbon of the tripterine. Compared with the tripterine, the 10-sulfonated tripterine has no obvious difference in anti-rheumatoid arthritis pharmacological activity, however, the hepatotoxicity in vivo and the cytotoxicity in vitro of the 10-sulfonated tripterine are obviously reduced. The tripterine sulfated metabolite is efficient and low in toxicity, and a wide application prospect is developed for treatment of rheumatoid arthritis.

The invention discloses nanoparticles for tumor chemotherapy and immune combined treatment as well as a preparation method and application of the nanoparticles, and belongs to the technical field of biological medicines. The nanoparticles are rHF (at) Cel nanoparticles formed by wrapping tripterine (Cel) with recombinant human heavy chain ferritin (rHF). The preparation method comprises the following steps: obtaining recombinant rHF protein, mixing and assembling Cel and rHF under specific pH and temperature conditions, and purifying to obtain the recombinant rHF protein. The nanoparticles can effectively target tumor cells and release Cel to kill tumors; meanwhile, the rHF carrier can induce polarization of tumor-related macrophages from a tumor-promoting M2 type to an anti-tumor M1 type, reduce the proportion of regulatory T cells (Treg) in a tumor microenvironment and reverse an immunosuppression microenvironment. In-vitro and in-vivo experiments prove that the rHF (at) Cel nanoparticles have a remarkable killing effect on breast cancer cells and can effectively inhibit the growth of transplanted tumors of mice.

This invention belongs to the field of biomedical technology, specifically relating to triptolide liposomes (TP-lipo), their combined use, and their application in the prevention and treatment of tumors. To enhance the efficacy of triptolide in the treatment and prevention of tumors such as pancreatic cancer, cervical cancer, ovarian cancer, and colorectal cancer, and to improve its bioavailability and clinical application while reducing toxicity, this invention uses HSPC, DOPS, and cholesterol as liposome components to encapsulate triptolide monomers, thus preparing TP-lipo. Experiments have shown that TP-lipo exhibits anti-tumor activity: it directly kills tumor cells and reverses the immunosuppressive microenvironment, making it a potential drug for tumor treatment. TP-lipo, when used in combination with PD-1 antibodies, or in combination with radiotherapy, chemotherapy, or surgery, demonstrates a potent and synergistic anti-tumor effect with low toxicity. Therefore, the TP-lipo of this invention provides more clinical strategies for tumor treatment.

This invention discloses a triptolide derivative targeting PRDX3, its preparation method, and its application. The derivative has the structure shown in general formula (I) or (II). This invention also relates to the preparation method of this type of compound and its application in the preparation of antitumor drugs.

The invention belongs to the technical field of pharmaceutical chemical crystallization, and particularly relates to tripterine, a crystal form of a solvate of the tripterine, a preparation method and application of the tripterine. The crystal form is a co-crystal of the tripterine and a solvent, and the ratio of the tripterine to the solvent is (45-200) mg: (1-30) mL. And the solvent is selected from C1-C4 alcohol solvents, C3-C5 ester solvents and non-polar solvents. 22 solvates and one novel polymorphic form are prepared by slurry conversion and solvent evaporation methods. The solvate is of a unique channel type structure, and solvent molecules are embedded into a three-dimensional framework constructed by a tripterine hydrogen bond network through hydrogen bonds and Van der Waals interaction. The stability of the crystal obtained by the polar solvent is obviously superior to that of the non-polar solvent, the structure-function relationship among the solvent polarity, the crystal structure and the thermal stability is clarified, and a theoretical basis and experimental guidance are provided for the preparation design of the tripterine medicine.

The invention discloses a C-6 oxidation derivative of tripterine as well as a preparation method and application of the C-6 oxidation derivative. The tripterine derivative has a structure as shown in a general formula (I). Compared with tripterine, the tripterine derivative or pharmaceutically acceptable salt, solvate or crystal compound disclosed by the invention has the advantages that the toxic and side effects are obviously reduced, the anti-inflammatory activity is retained, and the purposes of enhancing the effect and reducing toxicity are achieved; and important tool molecules and theoretical basis are provided for searching a low-toxicity, high-efficiency and high-selectivity NLRP3 inflammasome small-molecule inhibitor and a therapeutic drug for treating related inflammatory diseases. # imgabs0 #

The invention discloses a class of tripterine derivatives for targeted inhibition of EGFR (epidermal growth factor receptor) and application of the tripterine derivatives in preparation of antitumor drugs, and belongs to the technical field of chemical pharmacy. According to the invention, tripterine and thienyl, indolyl or morpholine substituted aryl carboxylic acid are connected together through an ester bond, and a class of tripterine derivative molecules are obtained through semi-synthesis. Molecular docking experiments predict that the derivative molecules have higher EGFR targeting ability than parent nucleus tripterine, and in-vitro antitumor activity research shows that the molecules have higher inhibitory activity on lung cancer tumor cell strains, meanwhile, the toxicity of tripterine is remarkably reduced, and the molecules have certain ability of inhibiting tumor cell migration. # imgabs0 #

The invention discloses a tripterine derivative as well as a preparation method and application thereof. The tripterine derivative provided by the invention is prepared by coupling the tripterine and the sphingosine base compound, retains the anti-inflammatory and antioxidant activity of the tripterine, and has a better effect than the tripterine; meanwhile, the tripterine derivative remarkably reduces the toxicity and irritation of tripterine and improves the skin compatibility and safety, so that the risk in clinical or skin care application is reduced. The preparation method provided by the invention is simple and efficient, adopts a green coupling agent HOPO for reaction, is safe, stable and lower in cost, can prepare a safer and milder tripterine substitute raw material with a better effect, can be used for developing more anti-inflammatory, barrier repair and anti-aging skin care products or cosmetics, and has wide application prospects. And various dosage forms of external washing products such as O / W emulsion, W / O cream and the like containing the tripterine derivative are produced and prepared.

The invention relates to tripterine-luteolin-based self-assembled nanoparticles as well as a preparation method and application thereof, and belongs to the field of biological medicines. Compared with single tripterine, the tripterygium wilfordii derivative nano-particles provided by the invention have a stronger inhibition effect on tumor cells and lower toxicity, and have a good application prospect in the development of antitumor drugs.

The invention relates to the technical field of biological medicine, in particular to application of tripterine or medicinal salt thereof in preparation of medicine for treating ketoacidosis or symptoms caused by ketoacidosis. The invention provides application of tripterine or medicinal salt thereof in preparation of a medicine for treating ketoacidosis or symptoms caused by ketoacidosis. The result of the specific embodiment of the invention shows that the tripterine can obviously reduce the mouse serum beta-hydroxybutyric acid level caused by hunger; the tripterine can be used for remarkably reducing the expression of HMGCS2 in the liver of a mouse; the dapagliflozin remarkably promotes the level of beta-hydroxybutyric acid, and the tripterine remarkably reduces the level of mouse serum beta-hydroxybutyric acid caused by treatment of the dapagliflozin. Therefore, tripterine can be used for treating or improving ketoacidosis or symptoms caused by ketoacidosis. The invention provides a new technical scheme for treatment and improvement of ketoacidosis or symptoms caused by ketoacidosis.

The invention relates to an application of constructing an efficient glycosyl transferase cascade catalytic system in synthesis of novel triterpenoid glycoside. Specifically, the invention provides a glycosyl transferase mutant, a sucrose synthase SUS mutant and a cascade catalytic system containing the glycosyl transferase mutant and the sucrose synthase SUS mutant, the invention firstly discovers that the glycosyl transferase mutant UGT109A3m and the sucrose synthase SUSm are combined according to a certain proportion, and the sucrose synthase SUSm can be used for preparing the sucrose synthase. Synergistic cascade catalysis can be achieved to obtain high yield tripterine glycoside derivatives.

The invention discloses a tripterine derivative with osteoporosis treatment activity and a preparation method and application thereof, and belongs to the technical field of medicines, and the tripterine derivative is any one of general formulas I-VIII shown in the specification. According to the tripterine derivative and the preparation method thereof provided by the invention, aromatization modification is carried out on an A ring of tripterine, and different types of heterocyclic rings are introduced to the left side of the A ring, so that not only is the structural diversity of the tripterine enriched, but also the structure-function relationship is perfected by carrying out structural derivatization on the C-29 site. On the basis of retaining the osteoporosis treatment activity of the tripterine, the cytotoxicity of the tripterine is remarkably reduced, the practical application value of the tripterine serving as an osteoporosis treatment agent is effectively improved, and the tripterine derivative can be applied to treatment of osteoporosis.

The invention provides application of tripterine or a derivative thereof in preparation of a product for inhibiting neisseria gonorrhoeae, and relates to the technical field of biology and bacteriostasis. The invention particularly relates to application of tripterine or a derivative thereof in preparation of a neisseria gonorrhoeae inhibitor; or (II) application in preparation of a medicine for preventing, relieving and / or treating neisseria gonorrhoeae infection; the invention relates to a medicine for treating or preventing infection and / or complications caused by neisseria gonorrhoeae and a method for inhibiting or preventing growth of neisseria gonorrhoeae.

The invention relates to a polymer-coated self-assembled tripterine nano particle as well as a preparation method and application thereof. The nano particle comprises a nano aggregate and a polymer shell, wherein the nano aggregate is formed by self-assembling tripterine or medicinal salt of the tripterine, and the outer surface of the nano aggregate is coated with the polymer shell. According to the self-assembled tripterine nano particle disclosed by the invention, the problems of dissolution rate and solubility of the tripterine are effectively improved, and the biocompatibility of the tripterine is improved. In addition, the polymer layer coated on the surface of the nano particle enables the structure of the nano particle to be more stable, and the residence time of the tripterine in a respiratory tract system is effectively improved. Meanwhile, under the condition of using the same dosage, compared with tripterine monomer molecules or nanoparticles not coated with polymers, the product disclosed by the invention has a more excellent antibacterial effect.

The invention discloses a tripterine derivative with a structure shown as a formula I. In the tripterine derivative, R1 is selected from H, # imgabs 0 # R2 is selected from # imgabs 1 # and is an integer from 3 to 6. Compared with tripterine, the tripterine derivative disclosed by the invention has the advantages that the inhibition effect on tumor cells is enhanced, the toxicity is obviously reduced compared with that of tripterine, mitochondria can be targeted, and meanwhile, the cells can be killed by increasing the ROS level in the tumor cells. The invention also discloses an application of the tripterine derivative in preparation of antitumor drugs. The invention also discloses an application of the tripterine derivative in preparation of mitochondrial targeting antitumor drugs. # imgabs2 #

The application discloses a tripterine derivative with a structure as shown in formula I, wherein R1 is selected from H, and R2 is an integer from 3 to 6. Compared with tripterine, the tripterine derivative has enhanced inhibition effect on tumor cells, significantly reduced toxicity, can target mitochondria, and can kill cells by increasing the ROS level in tumor cells. The application further discloses a use of the tripterine derivative in preparation of an anti-tumor drug. The application further discloses a use of the tripterine derivative in preparation of a mitochondria-targeting anti-tumor drug.

The invention discloses a new application of tripterine, namely application of the tripterine in preparation of bladder cancer resisting drugs, in-vitro cell experiments prove that the tripterine shows remarkable proliferation inhibition activity on various bladder cancer cell strains including cell strains UM-UC-3, TCCSUP and T24 and a cis-platinum drug-resistant strain T24CDDP, the median inhibitory concentration (IC50) of the tripterine is 0.2688-0.5870 mu M, and the tripterine shows remarkable proliferation inhibition activity on various bladder cancer cell strains including cell strains UM-UC-3, TCCSUP and T24 and a cis-platinum drug-resistant strain T24CDDP. The further mechanism research shows that the tripterine can regulate and control the cell cycle by down-regulating the expression levels of CDK1 and CDC5L proteins in bladder cancer cells and up-regulating the expression of phosphorylated p53 (p-p53) proteins at the same time, thereby playing a role in resisting bladder cancer; the invention provides a new effective candidate drug for clinical treatment of bladder cancer, especially cis-platinum resistant bladder cancer, and has important clinical application value.

The invention relates to an application of a tripterine nano particle in preparation of an immunologic adjuvant. The tripterine nano particle comprises a nano aggregate and a polymer shell, wherein the nano aggregate is formed by self-assembly of tripterine or medicinal salt of the tripterine, and the outer surface of the nano aggregate is coated with the polymer shell. The invention develops a brand-new immunologic adjuvant strategy, namely, a product obtained by coating a nano aggregate formed by self-assembly of the tripterine or medicinal salt thereof with a polymer, and under the condition of using the same dosage, compared with tripterine free molecules or nanoparticles not coated with the polymer, the tripterine free molecules or the nanoparticles not coated with the polymer have better immunologic adjuvant effect. The product has a more remarkable effect of enhancing the immunogenicity of the vaccine. Therefore, the product can be applied as an immunologic adjuvant. Meanwhile, the preparation method of the product is simple and mild in condition, green and environment-friendly, low in cost, free of special reaction equipment and easy to popularize and apply.