13 results about "Pentacyclic triterpenoids" 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.

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 present application belongs to the technical field of quality control of traditional Chinese medicine, and particularly relates to a quality control method of Ledum palustre L. The quality control method provided by the present application comprises the following processes: S1, identification: thin layer chromatography identification is respectively performed by taking ursolic acid, hyperoside, rutin, aesculetin and aesculin as the control; S2, inspection: the moisture content, total ash content, acid insoluble ash content and alcohol-soluble extract content of the medicinal material are determined; S3, content determination: the total content of volatile oil, three five-ring triterpenes (betulinic acid, oleanolic acid and ursolic acid) and two flavonoid glycosides (hyperoside and preussin) in the medicinal material is determined by using high performance liquid chromatography. The present application combines multi-index component analysis and thin layer chromatography identification, has strong specificity and good reproducibility, can comprehensively and effectively control the quality of Ledum palustre L., and ensures the medicinal effectiveness and safety of Ledum palustre L.

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 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 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.

The invention discloses a pentacyclic triterpenoid derivative or a pharmaceutical salt thereof. The structural general formula of the pentacyclic triterpenoid derivative is selected from one of the following structures: # imgabs0 #. The pentacyclic triterpenoid derivative can be used as a programmed cell necrosis inhibitor; or the compound can be used for preparing medicines for preventing and treating related diseases such as inflammation, neurodegeneration, infectious diseases or ischemic diseases caused by programmed cell necrosis.

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.