96 results about "Pentacyclic triterpenoid" patented technology

An anti-aging composition comprising: (i) at least one biomimetic oligopeptide having a sequence of 20 amino acids or less; (ii) at least one lipoaminoacid; (iii) at least one pentacyclic triterpenoid selected from the group consisting of asiaticoside, madecassic acid, asiatic acid and madecassoside; (iv) at least one antioxidant; and (v) tetrahydropiperine; a kit comprising such composition and a method of use.

The invention relates to the pharmaceutical field, in particular to application of a series of pentacyclic triterpenoid compounds as a cholesterol ester transfer protein (CETP) inhibitor, in particular to application in factors of preparing medicines for treating cardiovascular and cerebrovascular diseases, atherosclerosis diseases and hyperlipemia. The invention further discloses a series of novel pentacyclic triterpenoid compounds, application of the compounds as the CETP inhibitor and a pharmaceutical composition.

The invention relates to field of natural medicine and medicinal chemistry, in particular to novel pentacyclic triterpene and melbine salt I of the derivative thereof. The salt compound can be used for preparing medicaments curing diabetes mellitus and complicating disease thereof, cerebral ischemia, angiocardiopathy, atherosclerosis, hepatitis, fatty liver and metabolic syndrome or tumour, descendens blood fat drugs and anti-obesity drugs. The invention also relates to the preparation method of the salt compound.

The present invention discloses an application of pentacyclic triterpenoid saponin represented by formulas (I) to (XIII) for the preparation of a medicine for preventing or treating AMPK-mediated diseases including fatty liver disease, inflammatory bowel disease, respiratory disease, diabetic complications and polycystic kidney disease. The compounds of formula (I) to (XIII) are especially usefulfor nonalcoholic simple fatty liver, nonalcoholic steatohepatitis, non-alcoholic steatohepatitis-induced cirrhosis, ulcerative colitis, Crohn's disease, chronic obstructive Pulmonary diseases, asthma,idiopathic pulmonary fibrosis, cystic fibrosis, allergic rhinitis, diabetic nephropathy, diabetic cardiomyopathy, diabetic ulcers, and autosomal dominant polycystic kidney disease. A pharmaceutical composition for preventing and treating the AMPK-mediated diseases of the present invention comprises a therapeutically effective amount of the compounds of the formula (I) to (XIII) or a pharmaceutically acceptable salt or a solvate thereof as an active ingredient and a pharmaceutically acceptable excipient.

The invention discloses pentacyclic triterpenoid cyclodextrin clathrate compound proliposome and a preparation method thereof. The main component comprises one or more of pentacyclic triterpenoid compound series, for example, ursolic acid, oleanolic acid, betulonic acid, beta-masticinic acid, cyclodextrin clathrate compound, phospholipid material and cholesterol. According to the pentacyclic triterpenoid cyclodextrin clathrate compound proliposome, the pentacyclic triterpenoid compound is clathrated through cyclodextrin to improve the hydrophilicity; the liposome is used as a carrier to clad, and the proliposome is obtained by freezing and drying. According to the pentacyclic triterpenoid cyclodextrin clathrate compound proliposome, the bioavailability and the stability of the pentacyclic triterpenoid compound can be improved; transdermal absorption is promoted, and the skin irritation is reduced. In addition, the cyclodextrin clathrate compound proliposome is of a powder shape, good in stability and rehydration reconstruction and convenient to use, and can be applied to a plurality of cosmetic dosage forms such as cream, emulsion, gel and essence.

The invention relates to the field of natural drug and medicinal chemistry, in particular to ursane-type pentacyclic triterpenoid amino acid derivatives (I), and the preparation method and the medicinal application thereof. The compounds have effect on inhibiting glycogen phosphorylase, and can be used for preparing drugs for resisting diabetes, cerebral ischemia, cardiovascular diseases, hyperlipemia, obesity, atherosclerosis and tumor. The invention also relates to the preparation method of the compounds and drug preparations containing the compounds.

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 usage of a pentacyclic triterpenoid saponins compound relates to the filed of medicines, in particular to a pentacyclic triterpenoid saponins compound for preparing lipid-lowering medicines. The pentacyclic triterpenoid saponins refers to the compound in the right formula: R is H or Beta-D-glucosyl; the structural formula of Beta-D-glucosyl is the right formula.

The invention discloses a pentacyclic triterpenoid compound shown in a formula A or B and an application of a plant extract containing the pentacyclic triterpenoid compound in the preparation of a drug for resisting hepatitis virus C. The pentacyclic triterpenoid compound has the advantages of good treatment effect, low cost and less side effects; and the invention provides a new way for the treatment of the hepatitis C virus. In the formula A, R1 is H, OH or glucoside; R2 is H, OH or glucoside; R3 is CH3, CH2OH or glucoside; R4 is CH3, CH2OH or glucoside; R5 is CH3, COOH or glucoside. In the formula B, R1' is H, OH or glucoside; R2' is H, OH or glucoside; R3' is CH3, CH2OH or glucoside; R4' is CH3, CH2OH or glucoside; R5' is H or OH; R6' is H or CH3; T7' is H or CH3; R8' is H or OH; and R9' is CH3, COOH or glucoside. The formula A and the formula B are shown in the description.

The present invention relates to a pentacyclic triterpenoid compound represented by general formula (I) and preparation method thereof, pharmaceutical composition comprising the compound, uses of the compound in preparation of drugs for treating type 2 diebetes, and uses of the compound in treating type 2 diebetes.

The invention provides a conjugate formed by pentacyclic triterpenoid and amino acid through an ester bond or an urethane bond of the formula I and the formula II, wherein R1 is hydrogen, a methyl, an isopropyl, an isobutyl, a 2-methylpropyl or a benzyl; X is H2 or O; R2 is H, CH3 or COOH; R3 is CH3 or COOH; and R4 is H or CH3.

The present invention belongs to the field of organic chemistry and relates to a multi-substituted hydrogenated naphthalene compound, the preparation methods and uses. Specifically, the present invention relates to a chiral multi-substituted ten-hydrogen and/or eight-hydrogen naphthalene compound, the synthetic method and uses. The present invention aims to provide a chiral multi-substituted ten-hydrogen and/or eight-hydrogen naphthalene compound; the oleanane-type or usu-type five-ring triterpenoid compound is used as a raw material for preparing the compound. The multi-substituted ten-hydrogen and/or eight-hydrogen naphthalene compound of the present invention can be used for synthesis of drugs or spices containing multi-hydrogen naphthalene fragments and the analogues. The method of the present invention is simple and easy, low in cost, high in production rate, and can realize industrialization.

The present invention comprises small molecule inhibitors of cell proliferative conditions, in particular cancer and conditions associated with cancer. For example, associated malignancies include ovarian cancer, cervical cancer, breast cancer, colorectal cancer, and glioblastomas, among others. Accordingly, the compounds of the present invention are useful for treating, preventing, and/or inhibiting these diseases. Thus, the present invention also comprises pharmaceutical formulations comprising the compounds and methods of using the compounds and formulations to inhibit cancer and treat, prevent, or inhibit the foregoing diseases.

The invention discloses application of a pentacyclic triterpene compound and a medicine composition, and further discloses the pentacyclic triterpene compound shown in the formula A or the formula B in the specification, and application of a stereoisomer or a tautomer or pharmaceutically acceptable salt or solvate or polymorph of the pentacyclic triterpene compound in preparing medicine for treating diseases (especially cancer) caused by cell apoptosis or cell damage and a BCL-XL inhibitor. R1, R2, R3, R4, R5, R7, R8, R9, R10 and R11 are independently selected from one of hydroxyl, hydrogen, halogen, COR13, COOR14, C1-C4 alkoxy and C1-C4 alkyl, and R6, R12, R13 and R14 are independently selected from hydrogen or C1-C5 alkyl. The pentacyclic triterpene compound has higher inhibitory activity on binding between BCL-XL and pro-apoptosis protein and has guiding significance on design and research and development of the medicine.

The invention relates to the field of medicines, and particularly relates to applications of five-ring triterpenoid compounds shown as general formulas (I), (II) or (III) or pharmaceutical acceptable salts or esters thereof as oxidized squalene cyclase inhibitors, especially applications in the field of preparation of anti-hypercholesterolemia medicines, anti-hyperlipidemia medicines, medicines for treating heart and cerebral vessels and antitumor medicines, and other fields. The R1 to R6 are defined in the specification.

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 discloses a CYP450 gene IaAO2 catalyzing the oxidation of the C-28 site of amyrin. A protein which catalyzes the oxidation of the C-28 site of amyrin is encoded, and the CYP450 gene IaAO2 can be induced and expressed in engineered strains to catalyze alpha-amyrin and beta-amyrin to be oxidized into ursolic acid and oleanolic acid separately. The nucleotide sequence of the CYP450 geneIaAO2 is as shown in SEQ ID No.1, and the amino acid sequence of the CYP450 gene IaAO2 is as shown in SEQ ID No.2. The invention further discloses an expression vector and host bacterium of the CYP450 gene IaAO2 and application of the CYP450 gene IaAO2 to preparation of triterpenoid compounds, compounds catalyzing the oxidation of the C-28 site of pentacyclic triterpenes and compounds catalyzingthe oxidation of alpha-amyrin and beta-amyrin of pentacyclic triterpenes. The invention further discloses a method for performing homologous gene modification based on the sequence characteristics ofthe gene IaAO2 and a novel gene tIaAO1 obtained by the method. The IaAO2 gene has a shorter nucleotide sequence than a homologous gene, a genetically modified organism can be constructed by using theIaAO2 gene to synthesize a pentacyclic triterpenoid compound with important economic value, and good application prospects are achieved.

The invention belongs to the field of organic chemistry and relates to a polysubstituted decalin compound, and a synthesis method and an application thereof. The structural formula of the polysubstituted decalin compound is shown above. The preparation of the polysubstituted decalin compound includes septs as follows: AB fragment which is obtained by the c-bond cleavage of an oleanane type or an ursolic alkane type pentacyclic triterpenoid compound is treated with different reduction methods to obtain a compound 2 or 3. The polysubstituted decalin compound of the invention is used to synthesize the medicine or the apice and the analogues which contain the structural fragment of the polysubstituted decalin. The invention has the advantages of simplicity, practicability, low cost, high yield and being capable of industrialization.

The invention provides an 11-bromo-12-olefin oleanane type pentacyclic triterpene compound, which has a structure as shown in formula (1). The compound has certain inhibition tumor cell growth activity, and can be used to make drugs for preventing and curing tumor diseases. Moreover, the compound has remarkable inhibition action on mice ear tumescence caused by toluene, and can be used to make anti-inflammatory agents. The structural general formula of the 11-bromo-12-olefin oleanane type pentacyclic triterpene compound as shown in formula (1) is shown in the graph.

The invention discloses a pentacyclic triterpenoid novel AMPK agonist oleanolic acid derivative and medical application thereof, and specifically, a compound shown in the formula I or the formula II or a pharmaceutically acceptable salt or an ester or a solvate of the compound can be used for preparing an AMPK agonist with activity of enhancing the phosphorylation level of AMPK and preparing a medicine for preventing or treating AMPK-mediated diseases. The novel pentacyclic triterpenoid compound has remarkable AMPK agonist activity, the activity of the novel pentacyclic triterpenoid compound is remarkably superior to that of an acknowledged AMPK agonist AICAR, and meanwhile the novel pentacyclic triterpenoid compound has better pharmacokinetic properties such as oral bioavailability and the like and very good safety.

The invention discloses derivatives of oleanolic acid and delta-oleanolic acid as pentacyclic triterpenoid novel AMPK agonists and medical application of the derivatives, and particularly relates to compounds shown as a formula I or a formula II and pharmaceutically acceptable salts or esters or solvates of the compounds. The compounds can be used for preparing AMPK agonists with activity of enhancing the phosphorylation level of AMPK and preparing drugs for preventing or treating AMPK-mediated diseases. The novel pentacyclic triterpenoid compounds disclosed by the invention have remarkable AMPK agonist activity, the activity of the novel pentacyclic triterpenoid compounds are remarkably superior to that of an acknowledged AMPK agonist AICAR, and meanwhile, the novel pentacyclic triterpenoid compounds have pharmacokinetic properties such as better oral bioavailability and the like and very good safety.

The invention discloses application of pentacyclic triterpenoid saponins in ilex pubescens, namely Ilexsaponin B2, ilexoside A, Ilexsaponin A1,3-O-beta-D-xylopyranosylspathodic acid and flaccidoside I, in preparation of anti-diabetic medicines. Five pentacyclic triterpenoid saponins in ilex pubescens are obtained by large-scale preparation, and the inhibitory activity of the five pentacyclic triterpenoid saponins on alpha-amylase is screened by a large number of experiments. Experimental results show that the five pentacyclic triterpenoid saponins have better inhibitory activity on alpha-glucuronide. Especially, the IC50 of Silverside A and ilexsaponin A1 for alpha-amylase is respectively 0.0849mg/ml and 0.2184mg/ml, thereby obtaining excellent technical effects.

The invention provides a pentacyclic triterpenoid compound and derivatives of the pentacyclic triterpenoid compound. The pentacyclic triterpenoid compound and the derivatives of the pentacyclic triterpenoid compound have the significant pseudo nerve growth factor activity and are small-molecular compounds which can pass the blood brain barrier. Thus, through addition of the pentacyclic triterpenoid compound and the derivatives of the pentacyclic triterpenoid compound to pharmaceutically acceptable carriers, drugs for preventing and treating neurodegenerative diseases such as senile dementia (particularly the Alzheimer's disease) and the like can be prepared. Or the pentacyclic triterpenoid compound and the derivatives of the pentacyclic triterpenoid compound are used as active components,food acceptable carriers are added, and food for preventing and treating the neurodegenerative diseases such as the senile dementia and the like can be prepared. The pentacyclic triterpenoid compoundand the derivatives of the pentacyclic triterpenoid compound can also be applied to preparation of food and drugs for preventing and treating the neurodegenerative diseases or improving the cognitiveability and the learning and memory ability. The general structural formula is shown in the Formula I shown in the description.