36 results about "Pentacyclic triterpenoids" patented technology

The present invention relates to a pentacyclic triterpanoid derivative of multiple-oxide substitution of the A ring and the medicine salt or solvate of the derivative, and the present invention also relates to the preparation method, the drug combination, and medical use of the derivative. The compound of the present invention has the functions of inhibiting the activity of six human tumor cell strains in vitro, such as human prostate cancer cell (PC-3), nasopharyngeal carcinoma cells (CNE), oral squamous carcinoma cell(KB), human lung cancer cell (A549), human hepatoma cell (BEL-7404), and human cervix cancer cell (Hela), and the function of the invention is at the same magnitude of the positive control of cisplatin, thereby the compound can be used as expected antitumor drug. The compound of the present invention also inhibits the alpha glucosidase strongly, and the inhibiting effect is greater than the positive control of acarbose, thereby the compound can be used as expected medicine for preventing and treating diabetes and the treatment of the virus diseases.

The invention discloses derivatives of 3-O-caffeoyloleanane type pentacyclic triterpene represented by general formula (I) in the specification (R1 and R2 in the general formula (I) are selected from -CH3, COOH, COOQ, CONQ2, or COSQ, wherein Q is hydrogen, alkyl, substituted alkyl, aryl, or substituted aryl; X is -C=O or CH2; and Y-Z is -CH2-CH2-, cis-CH=CH-, or trans-CH=CH-), a preparation method thereof, and pharmaceutically acceptable esters or salts thereof. The invention also discloses a medicinal composition. The composition comprises an effective dose of the derivatives of 3-O-caffeoyloleanane type pentacyclic triterpene or the pharmaceutically acceptable esters or salts thereof, and pharmaceutically acceptable carriers thereof. The invention also discloses an application of the derivatives of 3-O-caffeoyloleanane type pentacyclic triterpene or the pharmaceutically acceptable esters or salts thereof in the preparation of anti-inflammatory medicines, antiallergic medicines, liver protection medicines, antivirus medicines and the like.

The invention discloses a method for preparing a non-pollution feed additive containing active ingredients of apricot leaves. In the invention, the apricot leaves are used as raw materials, cell walls of the apricot leaves are decomposed by adopting the method of Yeast fermentation, and then the active ingredients and nutritive matters in cells are completely released, thereby greatly increasing the types and the contents of the active ingredients of the apricot leaves in feed additive finished products, and removing poison materials (prussiate) at the same time. By adopting the method, the prepared non-pollution feed additive containing the active ingredients of the apricot leaves does not contain any chemical composition and toxic matters, is safe and environment-friendly, has high levels of the contents of pentacyclic triterpenoids, flavone, dietary fiber and protein, and is a novel, green and efficient.

The invention belongs to the technical field of medicine, and concretely relates to caffeoyl substituted pentacyclic triterpenoid derivatives as shown in a formula I and a purpose thereof in preparing medicaments or health products for preventing and treating brain injury and / or neurological dysfunction and / or cognitive dysfunction caused by cerebral ischemia, hypoglycemia and cerebral anoxia. Experiments verify that the derivatives is capable of protecting nerve cells under conditions of hypoglycemia and hypoxia, can substantially improve neurological damage induced by cerebral ischemia, and thus is expected to be developed as medicaments for preventing and treating the brain injury caused by the cerebral ischemia, the hypoglycemia and the cerebral anoxia as well as improving corresponding neuroethology functions.

The invention relates to the pharmacy field, concretely relates to a use of a series of pentacyclic triterpene compounds as enterovirus EV71 inhibitors, and especially relates to an application in the preparation of medicines for preventing and treating EV71 infection induced hand-foot-and-mouth diseases and complications thereof, such as synanche, myocarditis, pulmonary edema, encephalitis, herpes, septicemia, hypertension, hyperglycemia, cognitive function disorder, poliomyelitis-like paralysis and many nerve system associated diseases. The invention also discloses medicinal compositions of the series of the pentacyclic triterpene compounds as enterovirus EV71 inhibitors.

The invention relates to an extraction method of lupin alkane type pentacyclic triterpenoids in the leaves of Schefflera octophylla (Lour.) Harms through ionic liquid extraction. The method comprisesthe following steps: mixing the dried Schefflera octophylla (Lour.) Harms leaf powder with extractant; carrying out ultrasonic extraction at room temperature; centrifugalizing to obtain supernatant liquid after the ultrasonic extraction is finished; taking the supernatant so that the triterpenoids is obtained. The extractant consists of ionic liquid ([BMIM] BF4, [BMIM] Br, [BMIM] PF6 or [HMIM] PF6) and 70 percent of ethanol. The experiments prove that the total content of compound A (3 alpha-hydroxy-lup-20(29)-alkene-23,28-diacid) and compound B (3 alpha- hydroxy-lup-20(29)-alkene-23,28-diacid28-0-alpha-L-rhamnosyl-(1->4)-o-beta-D-glucose-(1->6)-beta-D-glucoside) was 288.03 mg / g (n=6). Compared with the traditional extraction method, the total extraction rate of the two compounds in the leaves of Schefflera octophylla (Lour.) Harms after the addition of ion liquid can reach 28.80%.

The invention discloses application of ursane pentacyclic triterpenoids in preparing tumor radiotherapy sensitivity drugs. A general molecular formula of the ursane pentacyclic triterpenoids is shownin a formula I. It is found for the first time that the ursane pentacyclic triterpenoids can increase the sensitivity of tumor cells to irradiation by inhibiting the activity of SUMO-specific proteases 1 (SENP1), and the ursane pentacyclic triterpenoids are expected to become new tumor radiotherapy sensitivity drugs. (Please see the description for the formula).

The invention relates to an anti-fatigue chewing gum containing bamboo rutabaga extract. Its main components and weight percent content are: 40%-55% of gum base; 5%-10% of pentacyclic triterpenoids extracted from Zhuru; 30%-40% of powdered sugar; 4%-6% of glycerin; glucose pulp 3%-6%; peppermint oil 0.5%-1%. The formula of the chewing gum is scientific and reasonable. It not only has the attributes and taste of ordinary chewing gum, but also has anti-fatigue effect because of the extract of bamboo rutabaga. It stays in the oral cavity for a longer time, making it easier for people to absorb, and the health care effect is more obvious.

The invention discloses application of compounds as shown in formula I or salt thereof and total saponin ingredients containing the compounds in preparing anti-tumor medicines. Researches show that the compounds as shown in the formula I and the total saponin have strong effects on inhibiting proliferation of human hepatocellular carcinoma cells, human gastric carcinoma cells, human colon cancer cells, human breast cancer cells and a melanoma cell strain, and the compounds as shown in the formula I, combined with chemotherapeutic drugs, have excellent attenuating and synergistic effects.

The invention provides an application of an oleanane type pentacyclic triterpene ester derivative in preparation of a medicine for delaying aging and treating aging disease, and the medicine is prepared by a pharmaceutical acceptable carrier or an excipient of the oleanane type pentacyclic triterpene ester derivative. The oleanane type pentacyclic triterpene ester derivative can obviously prolong the activity of yeast replicability life, and be used for preparing the medicine for delaying aging and treating aging disease. A structural formula of the oleanane type pentacyclic triterpene ester derivative is shown as following.

The invention provides an application of an oleanane pentacyclic triterpene ester derivative in preparation for medicine for treating senile dementia, and the senile dementia comprises neurodegenerative disease. The medicine is prepared by the oleanane pentacyclic triterpene ester derivative and a pharmaceutically acceptable carrier or an excipient. The oleanane pentacyclic triterpene ester derivative has obvious activity analogous with a nerve growth factor, and can be used for preparing the neurodegenerative disease medicine for treating senile dementia. According to the invention, a structural formula of the oleanane pentacyclic triterpene ester derivative is shown as follows.

The invention discloses a plant extract additive as well as a preparation method and application thereof, the additive comprises the following raw material components in percentage by mass: 20%-70% of pentacyclic triterpenoid active substances, 10%-50% of rosemary leaf powder and 10%-30% of eucommia ulmoides leaf extract, and the plant extract additive is prepared by mixing the raw materials. The plant extract additive has the advantages of being low in cost, rich in nutritional ingredients, high in content, green, environmentally friendly and the like, can improve the utilization rate of feed as a feed additive in livestock and poultry breeding, has the effects of resisting oxidation, enhancing the immunity of livestock and poultry organisms and protecting livers, can meet the requirements of livestock and poultry for essential amino acids, and has a wide application prospect. And the feed additive can completely replace the effect of antibiotics to a certain extent, can well replace more traditional additives, and has high use value and good application prospects.

Disclosed are a pentacyclic triterpene compound represented by general formula (I) and pharmaceutical compositions containing the compound. Also disclosed is use of the compound in preparation of a PS1 / BACE1 interaction inhibitor, and uses thereof in preparation of drugs for treating Alzheimer's disease. Disclosed for the first time is that a pentacyclic triterpene compound represented by general formula (I) can be used as a PS1 / BACE1 inhibitor, having activity of inhibiting PS1 / BACE1 interaction, and can reduce generation of Aβ and be used in preparation of drugs for treating Alzheimer's disease.

The invention relates to novel gypsophila elegans oleanane type pentacyclic triterpenoids represented by structure formulae (I, II, III and IV). The invention further relates to a pharmaceutical composition containing the components serving as active components, and application of the compounds and the pharmaceutical composition in medicines for treating gastric adenocarcinoma and adenocarcinoma of the lung. The structure formulae are shown in the specification.

The invention discloses a medicine for preventing thrombus formation or formed thrombus dissolution and a preparation method of the medicine, and belongs to the field of medicines. The medicine comprises a herba gei active compound combination, wherein the herba gei active compound combination is separated from herba gei extraction, potential hepatotoxic compounds are removed, and the herba gei active compound combination comprises polyphenol compounds and / or pentacyclic triterpenoids. When the medicine is given to a tested mammal, thrombus formation can be prevented and formed thrombus can be dissolved in blood of the mammal. The medicine mainly inhibits thrombus formation in blood and dissolves formed thrombus through a synergistic effect with blood coagulation factors / fibrinolytic factors in blood, so that different diseases or disease states caused by thrombus formation and thromboembolism in different tissues or organs are prevented and treated.

The invention relates to novel gypsophila elegans oleanane type pentacyclic triterpenoids represented by structure formulae (I, II, III and IV). The invention further relates to a pharmaceutical composition containing the components serving as active components, and application of the compounds and the pharmaceutical composition in medicines for treating gastric adenocarcinoma and adenocarcinoma of the lung. The structure formulae are shown in the specification.

The present invention relates to a pharmaceutical composition comprising two components, the first component being selected from forskolin, isoforskolin or a pharmaceutically acceptable salt thereof; and the second component is selected from pentacyclic triterpenoids or pharmaceutically acceptable salts thereof. According to the pharmaceutical composition disclosed by the invention, forskolin / isoforskolin and the pentacyclic triterpenoids are combined for use, and compared with independent use of the two components, the pharmaceutical composition disclosed by the invention can achieve a remarkable synergistic effect on prevention and treatment of metabolic, fibrosis and liver diseases, so that the pharmaceutical composition has a wide medicinal prospect in the aspect of improving diseases such as obesity, non-alcoholic fatty liver disease, liver injury, hepatic fibrosis and the like.

The invention discloses a pentacyclic triterpenoid TGR5 receptor stimulant, a preparation method and application of the pentacyclic triterpenoid TGR5 receptor stimulant. The structure of the pentacyclic triterpenoid TGR5 receptor stimulant is as shown in a formula I, and the definition of each substituent is as shown in the specification and claims. According to the pentacyclic triterpenoid compound, the solubility is increased, the permeability is improved, the TGR5 receptor agonist activity is remarkably improved, Caco-2 monolayer cells can be penetrated, and the in-vivo drug effect exertion of the compound after oral administration is guaranteed. The TGR5 receptor stimulant is expected to be further developed into a medicine for treating metabolic diseases represented by diabetes.

The invention discloses a metformin / ursolic acid nanometer oral preparation and a preparation method thereof, which uses self-assembly nanotechnology to self-assemble metformin and pentacyclic triterpenoid natural product ursolic acid into a particle size of 180-220 nm left and right nanoparticles, and together with the main auxiliary materials, additional auxiliary materials, and stabilizers to make nano oral preparations, the nano oral preparations obtained in the present invention have the effect of sustained release, and can reduce the side effects caused by common oral metformin hydrochloride preparations.

The present invention relates to a pentacyclic triterpenoid compound represented by general formula (I) and a preparation method thereof, a pharmaceutical composition containing the compound, the application of the compound in the preparation of a drug for treating type 2 diabetes, and the The application of said compound in the treatment of type 2 diabetes.

The invention discloses a method for preparing a non-pollution feed additive containing active ingredients of apricot leaves. In the invention, the apricot leaves are used as raw materials, cell walls of the apricot leaves are decomposed by adopting the method of Yeast fermentation, and then the active ingredients and nutritive matters in cells are completely released, thereby greatly increasing the types and the contents of the active ingredients of the apricot leaves in feed additive finished products, and removing poison materials (prussiate) at the same time. By adopting the method, the prepared non-pollution feed additive containing the active ingredients of the apricot leaves does not contain any chemical composition and toxic matters, is safe and environment-friendly, has high levels of the contents of pentacyclic triterpenoids, flavone, dietary fiber and protein, and is a novel, green and efficient.

The invention provides a method for detecting pentacyclic triterpenoids by using APCI as an ion source and using LC / MS. The method does not need to be derivatized and can detect three isomers within 6 minutes ,high sensitivity.

The invention relates to an application of an oleanane-type pentacyclic triterpene compound in preventing and treating bacterial diseases of agricultural crops and a method for preventing and treating bacterial diseases of agricultural crops using the oleanane-type pentacyclic triterpene compound. The present invention does not utilize the direct bacteriostasis of oleane-type pentacyclic triterpenoids, but improves the resistance of crops to bacterial diseases by soaking seeds before sowing or soaking roots before transplanting or spraying leaves after transplanting ability, and ultimately achieve the purpose of disease resistance. More importantly, the prevention and control method provided by the present invention only needs to be used once before planting to achieve the purpose of alleviating bacterial diseases, which greatly reduces the control cost of conventional pesticides.

The invention relates to use of pentacyclic triterpenoids compounds in preparing bacterial hemolysin inhibitors, provides a new use of pentacyclic triterpenoids compounds, and discloses that the pentacyclic triterpenoid compounds can neutralize the activity of bacterial hemolysin, reduce the damage of bacteria to host cells and the death caused by infection of model animals; inhibiting the activity of hemolysin can achieve the protective effect on the body; the pentacyclic triterpenoids compounds can be used to prepare drugs for hemolysin-producing bacterial infection.

The invention provides a pentacyclic triterpene compound and its application as an inhibitor of human intestinal carboxylesterase, belonging to the technical field of biomedicine. The pentacyclic triterpenoids have a 11-deoxy-glycyrrhetinic acid skeleton structure, which can potently and selectively inhibit the activity of human intestinal carboxylesterase subtype 2, thereby improving the bioavailability of oral prodrugs , and reduce the intake of intestinal esters. In addition, the inhibitor can also slow down the delayed diarrhea caused by irinotecan. In vitro activity assays found that the IC50 of this type of compound inhibiting human carboxylesterase 2 can reach 0.02 micromolar, and the ratio of the IC50 of inhibiting human carboxylesterase 1 to the IC50 of inhibiting human carboxylesterase 2 can reach 1020, and this type of compound The safety is good, and it also has the advantages of simple preparation process and high yield, suggesting that this type of compound has a good application prospect.

The present invention relates to a pharmaceutical composition, which comprises two components, the first component is selected from forskolin, isofaskolin or pharmaceutically acceptable salts thereof; the second component is selected from five Cyclic triterpenoids or pharmaceutically acceptable salts thereof. The pharmaceutical composition of the present invention uses forskolin / iforeskolin and pentacyclic triterpenoids in combination, compared with using the two components alone, it can prevent and treat metabolic, fibrosis, and liver diseases It has a significant synergistic effect, so it has broad medicinal prospects in the treatment, prevention, and improvement of diseases such as obesity, non-alcoholic fatty liver, liver injury, and liver fibrosis.

The invention relates to the application of an oleanane-type pentacyclic triterpene compound in preventing and treating fungal diseases of crops and a method for using the same to prevent and control fungal diseases of crops. The present invention does not utilize the direct antibacterial effect of oleanane-type pentacyclic triterpenes, but improves the resistance of crops to fungal diseases by soaking seeds before sowing or soaking roots before transplanting or spraying leaves after transplanting ability, and finally achieve the purpose of disease resistance. More importantly, the prevention and control method provided by the invention only needs to be applied once before planting to achieve the purpose of alleviating the disease, which greatly reduces the control cost of conventional pesticides.

The invention belongs to the field of pharmacy of traditional Chinese medicines, relating to an extract of effective parts of total saponins in pterocephalus hookeri as well as a preparation method and application thereof. By taking the content of the total saponins in the pterocephalus hookeri as an index, the extract of the total saponins in the pterocephalus hookeri provided by the invention has the characteristics of high content of the total saponins, controllable and stable quality and obvious drug effect. The main component of the extract is oleanane type pentacyclic triterpene saponins, and the content of the total saponins is 50%-90%. The preparation method provided by the invention is economical and simple in extraction technique and is applicable to industrial production. The obtained extract has obvious function of restraining the tumor cell proliferation, and can be applied in preparation of anti-tumor drugs.

The invention discloses an application of phthalic acid in hair growth promotion. The phthalic acid can be used as a unique active component for preparing a medicine or a reagent for promoting hair growth. The phthalic acid is an oleanolic acid derivative and belongs to a pentacyclic triterpenoid derivative, experiments prove that the phthalic acid group has a promoting effect on mouse hair growth, and hair growth is rapid; the invention provides a new application of the phthalic acid in promoting hair growth, and active ingredients of the phthalic acid are high in safety and small in toxic and side effects, so that the phthalic acid has a wide application prospect in the fields of pharmaceutical preparations, cosmetics, care products, beauty products and the like for preventing, nursing and treating less hair and alopecia and promoting hair health and growth.

Provided are a caffeoyl substituted pentacyclic triterpene derivative as represented by formula (I) and pharmaceutical composition containing the same. Also provided are uses of the derivative in the preparation of drugs or health-care products for preventing and treating brain injury induced by cerebral ischemia, glucose deprivation, and cerebral anoxia, and / or nervous dysfunction, and / or cognitive dysfunction.