32 results about "Pentacyclic triterpenoid" patented technology

The invention belongs to the technical field of pharmaceutical preparations, and relates to traditional Chinese medicine self-assembled nanoparticles for enhancing anti-inflammatory activity as well as a preparation method and application of the traditional Chinese medicine self-assembled nanoparticles. The traditional Chinese medicine self-assembled nanoparticles are prepared from biphenyl cyclooctene type lignan and an oleanane type pentacyclic triterpenoid compound, wherein the mass ratio of the biphenyl cyclooctene type lignan to the oleanane type pentacyclic triterpenoid compound is 1 to (0.125 to 8). Through an anti-solvent exchange method, the carrier-free nanoparticles based on self-assembly of the traditional Chinese medicine active ingredients are prepared by utilizing spontaneous non-covalent interaction between the biphenyl cyclooctene lignan and the oleanane pentacyclic triterpenoid, so that the cytotoxicity is remarkably reduced, the biocompatibility is enhanced, and the toxic and side effects are reduced; meanwhile, the traditional Chinese medicine self-assembled nano-particles have a remarkable cellular uptake effect, the absorption and utilization efficiency of the medicine is improved, and more efficient anti-inflammatory biological activity is shown.

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 an efficient targeting anti-hepatic fibrosis nano drug delivery system and a preparation method thereof. According to the system, a pentacyclic triterpenoid compound lupeol extracted from cichorium glandulosum is taken as an active ingredient, and the hyaluronic acid modified ZIF-8 loaded lupeol nano drug delivery system (HA / Lupeol ZIF-8) is constructed aiming at the problems of poor water solubility, low stability, weak targeting property and the like of the pentacyclic triterpenoid compound lupeol. The system is synthesized by a room-temperature solution method, hydrophobic lupeol is efficiently entrapped by using a porous structure of ZIF-8, and active targeting of a CD44 receptor on the surface of the hepatic stellate cell is realized by surface modification of hyaluronic acid. The particle size of the nano drug delivery system is 50-200nm, the encapsulation efficiency is 97.4%, and the drug loading capacity is 23.8%. In a fibrotic acidic microenvironment, the ZIF-8 carrier can responsively degrade and release a drug, and effectively penetrates through a collagen deposition barrier, so that precise drug delivery is realized. According to the invention, a new strategy is provided for anti-hepatic fibrosis treatment by combining degradation of ZIF-8 in a hepatic fibrosis acidic microenvironment and active targeting bifunctional characteristics of hyaluronic acid for the first time.

This invention discloses a class of pentacyclic triterpenoid derivatives with diverse B-ring modifications, their preparation methods, and applications. This invention utilizes a chemical enzymatic method to expand the chemical space of the B-ring in pentacyclic triterpenoids, obtaining a series of pentacyclic triterpenoid derivatives with diverse B-ring modifications. Pharmacological activity screening of these pentacyclic triterpenoid derivatives revealed their good tumor-suppressive activity, providing a promising application prospect for the prevention and treatment of tumors. This invention achieves the efficient synthesis of pentacyclic triterpenoid derivatives with diverse B-ring modifications, structures that are difficult to obtain using traditional chemical methods. Systematic antiproliferative activity screening identified candidate molecules with broad-spectrum and highly efficient inhibitory effects against various human tumor cell lines. These molecules show good drug development potential, providing novel lead compounds for the innovative development of anticancer drugs.

The invention relates to the field of protein degradation, and relates to application of a pentacyclic triterpenoid compound. The invention discloses application of a pentacyclic triterpenoid compound as an E3 ligase ligand or combined oncogenic protein. The pentacyclic triterpenoid compound provided by the invention has an obvious effect of binding E3 ligase, and part of the compound has obvious binding specificity.

The invention discloses a pentacyclic triterpene acylhydrazone compound as well as a preparation method and application thereof. A series of oleanolic acid derivatives are synthesized by carrying out structural modification on carboxyl at C28 site of oleanolic acid, structural confirmation is carried out by using 1H NMR, 13C NMR, HRMS and X-ray single crystal diffraction, and the inhibition effect of the pentacyclic triterpenoid acylhydrazone compound on the activity of tumor cells A549, AGS and K562 is evaluated by taking cis-platinum as positive control and adopting a CCK-8 method. Results show that the inhibition effect of the derivatives 5, 6, 9, 10, 16, 21, 27 and 28 on tumor cells is superior to that of cis-platinum. Reference is provided for research of oleanolic acid derivatives and discovery of anti-tumor seedling compounds.

To provide pentacyclic triterpenoid C-glycoside, a method for producing the glycoside, and use of the glycoside.SOLUTION: Provided is a compound expressed by formula I. The compound can be used for producing a drug for treating metabolic diseases such as diabetes mellitus, and viral diseases caused by an influenza virus or a coronavirus.SELECTED DRAWING: None

The invention discloses a pentacyclic triterpenoid compound with anti-tumor activity and a preparation method and application thereof, and belongs to the technical field of medicines, and the structure of the compound is confirmed through comprehensive spectrum analysis. The preparation method comprises the following steps: carrying out reflux extraction on dried euphorbia pekinensis roots with ethanol, concentrating, extracting with dichloromethane, and carrying out multi-step separation and purification steps such as system combination silica gel column chromatography, medium-pressure silica gel column chromatography, Sephadex LH-20 gel chromatography and preparative high performance liquid chromatography to finally obtain the high-purity compound. In-vitro anti-tumor activity experiments show that the compound has a remarkable proliferation inhibition effect on mouse liver cancer cells Hepa1-6. The invention provides a lead compound with a novel structure for developing a novel anti-hepatoma drug.

The invention discloses a synephrine organic salt as well as a preparation method and application thereof. The synephrine and the pentacyclic triterpenoid organic acid react to generate the synephrine organic salt, and the pharmacodynamic experiment result shows that compared with the original single effective component, the synephrine organic salt has a synergistic effect, has better effects of relieving cough, eliminating phlegm and relieving asthma, is simple in synthetic route and has certain water solubility, and the synephrine organic salt can be used for preparing the medicine for treating cough and asthma. The compound preparation can be replaced to become a new medicine with clear active ingredients, definite curative effect and controllable quality.

The application discloses functions and uses of a kind of pentacyclic triterpenoid compounds in preventing and / or treating neurodegenerative diseases, and the compounds are obtained by isolating and extracting from Cynomorium songaricum Rupr medicinal materials.The inventors found that the compounds have significant protective effects on glutamic acid-induced nerve cell injury and oxygen-glucose deprivation-induced nerve cell injury during pharmacological activity evaluation of the compounds, and thus can be used for treating and preventing neurodegenerative diseases such as stroke, brain injury, amyotrophic lateral sclerosis, Huntington's disease, Parkinson's disease and Alzheimer's disease, and can be developed into drugs.

The invention discloses a pharmaceutical composition of a pentacyclic triterpenoid and capecitabine and application of the pharmaceutical composition, and belongs to the technical field of biological medicines. By reducing the hydrolysis of capecitabine in gastrointestinal tracts and livers, the pharmaceutical composition not only slows down the early release of capecitabine drug bodies in gastrointestinal tracts and livers, increases the total bioavailability of the drug bodies and 5-fluorouracil, reduces the non-uniform high distribution of capecitabine in normal tissues such as gastrointestinal tissues, but also improves the bioavailability of capecitabine in gastrointestinal tracts and livers. Reducing toxicity in these tissues; meanwhile, the effectiveness of the medicine is improved by relatively increasing the medicine distribution of the targeted tumor part. The combination will be suitable for all tumor treatment, especially solid tumor treatment.

Provided are a crystalline form of a pentacyclic triterpenoid compound and a preparation method of the crystalline form, the pentacyclic triterpenoid compound being 3-O-cyclohexanecarbonyl-11-carbonyl-beta-boswellic acid, abbreviated as CKBA, the preparation method of the crystalline form being simple in operation, the crystalline form prepared being more stable under light conditions, less change in impurities, and the crystalline form prepared being higher in solubility in organic solvents, lower in hygroscopicity, and more conducive to development of a subsequent preparation process. Further provided are a pharmaceutical composition using the crystalline form as an active ingredient, and use of the crystalline form in preparation of a medicament for treating psoriasis.

The invention discloses a pentacyclic triterpenoid compound as well as a preparation method and application thereof.The pentacyclic triterpenoid compound is a compound shown in a formula A and a formula B. The pentacyclic triterpenoid compound is extracted from peeled and demarinated stems of Tibetan medicine rubus corchorifolius. The pentacyclic triterpenoid compound has anti-inflammatory activity and anti-tumor activity; the compound has the potential of being developed into anti-inflammatory drugs and anti-tumor drugs.

The application discloses application of polyphosphate-dependent glucokinase in glycosylation modification of pentacyclic triterpenoid compounds, a sugar group donor of the glycosylation modification is sucrose, the polyphosphate-dependent glucokinase is used for converting byproduct fructose into fructose-6-phosphate, and the polyphosphate-dependent glucokinase is CgPPGK with an amino acid sequence as shown in SEQ ID NO:1 or Asp-PPGK with an amino acid sequence as shown in SEQ ID NO:2. The polyphosphate-dependent glucokinase CgPPGK or Asp-PPGK is coupled to a traditional UDP-glucose regeneration system in the application, a coupled three-enzyme UDP-glucose regeneration system is formed, consumption of fructose is realized, more UDP-glucose is generated in the reaction, glycosylation efficiency and sucrose utilization rate are improved, and the glycosylation modification capacity for a substrate is obviously higher than that of an original traditional UDP-glucose regeneration system.

The application discloses functions and uses of a kind of pentacyclic triterpenoid compounds in preventing and / or treating neurodegenerative diseases, and the compounds are obtained by isolating and extracting from Cynomorium songaricum Rupr medicinal materials.The inventors found that the compounds have significant protective effects on glutamic acid-induced nerve cell injury and oxygen-glucose deprivation-induced nerve cell injury during pharmacological activity evaluation of the compounds, and thus can be used for treating and preventing neurodegenerative diseases such as stroke, brain injury, amyotrophic lateral sclerosis, Huntington's disease, Parkinson's disease and Alzheimer's disease, and can be developed into drugs.

The present invention provides a novel and improved method for preparing stable amorphous pentacyclic triterpenoids, compositions prepared using such pentacyclic triterpenoids, and a method for mitigating the effects caused by pro-inflammatory cytokines in mammals (including humans) by providing effective doses of pentacyclic triterpenoids treated according to the present invention. Furthermore, the present invention provides effective low-dose therapeutic compositions comprising pentacyclic triterpenoids treated according to the present invention.

The present invention has isolated a new class of pentacyclic triterpenoid compounds with novel structures from jasmine roots, which have strong inhibitory activity against tumors. #imgabs0#

The invention discloses a medicinal and edible complementary food for refreshing mind and restoring consciousness and a preparation method thereof, and belongs to the technical field of medicinal and edible complementary food. Comprising the following components in parts by weight: 10-15 parts of hawthorn, 10-25 parts of himalayan teasel root, 10-20 parts of akebia trifoliate, 5-15 parts of olean, 1-8 parts of sargassum, 1-8 parts of ulva pertusa, 3-10 parts of rhizoma polygonati, 1-5 parts of poria cocos, 1-5 parts of lentils, 1-4 parts of chickpeas, 2-8 parts of oat, 2-10 parts of chestnut kernels, 1-6 parts of pumpkin seeds, 1-5 parts of grapefruit seeds, 2-8 parts of honey, 5-10 parts of cow milk and 1-2 parts of vitamins. 1-2 parts of mineral substances and 1-5 parts of beta-maltodextrin. Through scientific proportioning and reasonable compatibility of traditional Chinese medicines, the synergistic effect of various active substances is realized, through reasonable compatibility, the prepared medicinal and edible complementary food can play a more remarkable anti-fatigue role, loss of pentacyclic triterpenoids is effectively prevented through double-layer embedding, and the content of active ingredients is ensured. Animal experiments prove that the medicinal and edible complementary food can improve exercise tolerance and fatigue resistance of mice.

The present application relates to a kind of pentacyclic triterpenoids and its preparation method and application.The pentacyclic triterpenoids provided by the present application belong to methylsuccinic acylitans type triterpenoid compounds and analogs, the compound shows good inhibitory activity to cyclooxygenase-2 (COX-2), can be used for preparing anti-inflammatory drug;The present application takes oleanolic acid or ursolic acid as matrix, under the action of condensing agent, with organic diacid monomethyl ester or organic diacid monomethyl ester acyl chloride is reacted, so as to introduce specific organic diacid monomethyl ester acyl in the 3-position hydroxyl of matrix, reaction condition is mild, synthesis speed is fast, yield is high, the present application provides a kind of efficient, fast method for methylsuccinic acylitans type triterpenoid compounds and analogs.

The invention relates to a composition for oral or topical human administration and a preparation method thereof. The present invention relates to pentacyclic triterpenoid compounds wherein said triterpenoid compounds are incorporated into lipid vesicles, preferably cream globules, surrounded by three layers of membranes. The triterpenoid is preferably betulinic acid, and / or betulinol, and / or lupenol, and / or oleanolic acid, and / or ursolic acid, most preferably betulinic acid. The incorporation of the triterpenoid compound into the milk fat globules or lipid vesicles at a high payload of at least 10 to at most 50 mg / ml is preferably accomplished with high energy emulsification techniques, most preferably ultrasound treatment. The composition is present as a liquid emulsion formulation in a preferred embodiment. In another preferred embodiment, the composition is a powder, which can be prepared from a liquid embodiment of the composition by, for example, spray drying or freeze drying techniques. The composition can be preferably used as a medicament, a food supplement or a nutraceuticals for the treatment or prevention of cancer, type 2 diabetes, obesity and cardiovascular diseases.

This invention belongs to the field of modern agricultural technology and specifically relates to the use of demethylzeylasteral (DZL) in the preparation of products for controlling Phytophthora spp. This invention demonstrates the inhibitory effect of pentacyclic triterpenoid demethylzeylasteral on the activity of Phytophthora capsici and other crop fungi. Demethylzeylasteral can inhibit the fungus, sporangium release, zoospore germination, and pathogenicity, demonstrating its anti-Phytophthora spp. activity. Therefore, the compounds provided by this invention can be used to prepare small molecule inhibitors of the growth, development, and pathogenicity of Phytophthora spp., demonstrating their potential as potential anti-Phytophthora spp. drugs and possessing promising development and application value.

The invention discloses a slice treating fluid and method for preserving antigen activity in a slice, and belongs to the technical field of immunodetection. Wherein the section is obtained by utilizing a pathological section preparation technology, and the section treatment liquid comprises a pentacyclic triterpenoid compound. By utilizing the section treating fluid disclosed by the invention, the antigen activity of the paraffin-embedded tissue section can be kept for at least 9 months when the paraffin-embedded tissue section is stored at normal temperature, and the storage life of the antigen activity in the cell slide at normal temperature can be effectively prolonged.

The application belongs to the technical field of pharmaceutical preparations, and relates to a traditional Chinese medicine self-assembled nanoparticle with enhanced anti-inflammatory activity and a preparation method and application thereof. The traditional Chinese medicine self-assembled nanoparticle is composed of a biphenylcyclooctene type lignan and an oleanane type pentacyclic triterpenoid compound; wherein the mass ratio of the biphenylcyclooctene type lignan and the oleanane type pentacyclic triterpenoid compound is 1:(0.125-8). The application uses a reverse solvent exchange method to prepare a carrier-free nanoparticle based on self-assembly of traditional Chinese medicine active ingredients by using the non-covalent interaction between the biphenylcyclooctene type lignan and the oleanane type pentacyclic triterpenoid compound, significantly reduces cytotoxicity, enhances biocompatibility and reduces toxic side effects, and meanwhile, the traditional Chinese medicine self-assembled nanoparticle has a significant cell uptake effect, improves drug absorption and utilization efficiency, and exhibits higher anti-inflammatory biological activity.

The invention belongs to the technical field of medicine, and discloses a pentacyclic triterpenoid derivative and a preparation method and medical application thereof, alpha-hederin or oleanolic acid is used as a raw material, and the pentacyclic triterpenoid derivative is prepared by esterification reaction or amidation reaction aiming at carboxyl of C-28. The prepared pentacyclic triterpene derivative has anti-inflammatory, anti-oxidation and anti-apoptosis effects, the synthesis method is simple, raw materials are cheap and easy to obtain, and the pentacyclic triterpene derivative is suitable for industrial application.

The invention relates to a preparation method of a pentacyclic triterpene compound. The preparation method comprises the following steps: S1, respectively providing camellia seed meal, ribonuclease, hydrolase, alkaline protease, phosphatase and P450 hydroxylation and polymerase; s2, selecting at least three enzymes from ribonuclease, hydrolase, alkaline protease, phosphatase and P450 hydroxylation and polymerase as compound enzymes, and adding the compound enzymes, the camellia seed meal and water into the reactor at room temperature; s3, preparing a water-soluble fraction through microwave action and column chromatography; and S4, extracting the pentacyclic triterpenoid compound from the water-soluble fraction by combining HPLC (High Performance Liquid Chromatography) and GC-MS (Gas Chromatography-Mass Spectrometer). According to the preparation method of the pentacyclic triterpenoid compound, rich terpenoid compounds in camellia seed meal are utilized, depolymerases and polymerases are respectively used for separation, preparation and biosynthesis of complex polyterpenoid, waste is turned into wealth, and the productivity is improved.

The invention discloses a pharmaceutical composition for treating and / or preventing depression, and belongs to the technical field of biological medicines. The technical problem to be solved is to significantly improve depression-like behaviors and protect nerve cells, and has an obvious effect on treatment and / or prevention of depression. According to the key point of the technical scheme, the pharmaceutical composition for treating and / or preventing depression comprises a secoiridoid glycoside compound, a xanthone glycoside compound and a beta-amyrin type pentacyclic triterpenoid compound in a mass ratio of 1: (0.25-6): (0.1-5), and one or more medically acceptable auxiliary materials.

The invention relates to lubricating grease compositions containing: a base oil, a soap thickener or polyurea thickener, and at least one pentacyclic triterpene having at least one OH group. The invention also relates to the production of said compositions, and to the use thereof for lubricating lubrication points on machines that come into contact with foodstuffs and feedstuffs.

The present invention provides a cytochrome P450 oxidase gene and application of Bupleurum chinense, which is CYP716A41. The enzyme has been confirmed by catalytic experiments to have the function of catalyzing the biosynthesis intermediate of saikosaponin β-amyrin and producing erythrodiol and oleanolic acid in its C-28 multi-step oxidation. The present invention has achieved the heterologous production of erythrodiol, an intermediate in the synthesis of saikosaponin, by using the enzyme, and erythrodiol is an important synthetic intermediate of various C-28 hydroxylated oleanane-type saikosaponins and other C-28 hydroxylated site triterpenoids. The present invention further promotes the analysis of the biosynthetic pathway of saikosaponins and synthetic biology research, and has important research value for the synthesis and regulation of oleanane-type pentacyclic triterpenoids such as saikosaponins and the breeding of Bupleurum plants.

The present invention discloses a class of pentacyclic triterpenoid saponins and their derivatives for use in preventing and treating myocardial hypertrophy; belonging to the field of medicinal chemistry; the pentacyclic triterpenoid derivatives or pharmaceutically acceptable salts thereof are represented by general formula (I): the pentacyclic triterpenoid derivatives of the present invention have a good binding effect on GATA6, a potential intervention target for myocardial hypertrophy, can significantly prevent and reverse myocardial cell hypertrophy in vitro and myocardial hypertrophy in vivo, and have potential medicinal value.