17 results about "Pentacyclic triterpenoid" patented technology

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 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.

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 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 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 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 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.

This invention discloses a betulinic acid derivative, its preparation method, and its uses. Using betulinic acid, a natural lupin-type pentacyclic triterpenoid, as the parent compound, a series of betulinic acid derivatives based on C-2 and C-3 position structural modifications were synthesized sequentially via oxidation and Claisen condensation reactions. These betulinic acid derivatives exhibit excellent α-glucosidase inhibitory activity. Their chemical structures differ significantly from existing clinical drugs, and their parent compounds are derived from natural products. This invention holds promise for overcoming the gastrointestinal adverse reactions and other drawbacks of traditional α-glucosidase inhibitors, providing new drug candidates for diabetes treatment. Furthermore, the raw materials for this invention are relatively widely available, facilitating subsequent scale-up production and process optimization, and possessing the potential for further development into clinical drug candidates.