78 results about "Flavonoid derivatives" patented technology

A method for the treatment of leukemia by internal administration of a composition including one or more compounds that inhibit cytokines and one or more antioxidants, optionally formulated in a pharmaceutically acceptable carrier. The composition of the present invention may further include optional ingredients such as flavonoids, flavonoid derivatives, and compounds that regulate cell differentiation and / or cell proliferation. A method for the internal administration of a composition for the purpose of treating leukemia involves the administration of an effective amount of a composition including one or more compounds that inhibit cytokines and one or more antioxidants to a person who has leukemia. Compositions useful in the method are also disclosed.

A cannabis-based flavonoid pharmaceutical composition including any one or more selected from among the group of Cannflavin A, Cannflavin B. Cannflavin C, Chrysoeriol, Cosmosiin, Flavocannabiside and their derivatives selected from among the group of Geraldol, Rhamnetin, Isorhamnetin, Rhamnazin, or their synthases, for the prevention and treatment of certain cancers that can be treated by therapeutically targeting oncogenic factors including kinases, sirtuins, bromodomains, matrix metalloproteinases and histone acetylases. Some of the cancers that can be treated by use of cannabis flavonoids based on the inhibition of these therapeutic targets include but are not limited to brain, breast, colon, renal liver, lung, pancreatic, pigmented villonodular synovitis, prostate, leukemia, melanomam, tenosynovial giant cell tumor, as well as any other cancers that overexpress the oncogenic factors inhibited, by the cannabis flavonoids or their derivatives herein identified.

The invention belongs to the field of medicinal chemistry, and relates to flavonoid derivatives and application thereof in preparing a medicinal composition for treating diseases related with dopamine transport protein. The flavonoid derivatives of the invention have a structure of a formula (I). A biological evaluation result shows that a compound of the invention represents better activation function on the dopamine transport protein compared with the prior art, can adjust the transport of dopamine by promoting the transport function of the dopamine transport protein, maintain extracellular dopamine concentration balance, and can be prepared into dopamine transport protein agonist used for treating mental diseases and neurological diseases. R1 is selected from hydroxy, alkoxyl of C1 to C8, ester group of C1 to C8, glucoside and halogen; R2 is selected from hydrogen, C7-hydroxy, C7-alkoxyl, C7-ester and C7-halogen respectively; and R3 is selected from the hydrogen respectively, or contain one or a plurality of substituent groups on a benzene ring, wherein the substituent groups are selected from the hydroxy, alkoxyl, ester group, aryl (heteroaryl), the hydrogen and glycoside group respectively.

The invention relates to polyphenols substances, a synthesis method thereof and the use thereof, in particular to a flavonoid derivative, a preparation method thereof and the use thereof, and solves the problem that the conventional natural flavonoids compounds are difficult to extract and obtain and cannot be widely used. The structural formula (I) of an intermediate and the structural formula (II) of a final product are shown below, wherein R1, R2 and R3 are respectively selected from hydrogen, C1-C8 alkyl, halogen, nitro, C1-C8 alkoxy and amino; and R1, R2 and / or R3 can be fused with a benzene ring to form a substituted or unsubstituted fused ring compound; R4 and R5 are respectively selected from C1-C8 alkyl, C1-C8 alkoxy and alkylene; R may be H, methoxy-methoxy or methoxy; and b ring is a benzene ring or a heterocyclic compound. The derivative can be used for preparing medicaments for resisting tumors and cardiovascular and cerebrovascular diseases and inhibitors of protein tyrosine kinases, opens up a new way for preparing the medicaments and brings a new breakthrough to the medicament field; and the synthesis method has the advantages of mild condition and convenient operation.

The present invention belongs to the field of pharmaceutical chemistry, and, in particular, disclosed therein are a flavonoid derivative and use thereof. Disclosed is a flavonoid derivative having the structure of general formula (I) or a pharmaceutically acceptable salt thereof. This compound can be used in the preparation of drugs for preventing or treating central nervous system diseases.

Therapeutic compositions capable of removing excess nitric oxide are provided. The therapeutic compositions include nitronyl nitroxide monoradicals, B12 derivatives, flavonoid derivatives, the like and combinations thereof. The therapeutic compositions can be utilized in a number of suitable applications, such as to prevent or treat intradialytic hypotension during dialysis.

The present invention provides a cannabis-based flavonoid pharmaceutical composition including any one or more selected from the group of Apigenin, Cannflavin A, Cannflavin B, Cannflavin C, Chrysoeriol, Cosmosiin, Flavocannabiside, Kaempferol, Luteolin, Myricetin, Orientin, Isoorientin (Homoorientin), Quercetin, (+)-Taxifolin, Vitexin, and Isovitexin, or their synthases, for the prevention and treatment of certain diseases of the CNS system and related disorders.

The invention relates to a flavonol sulfonic ester derivative and a relative synthesis method, wherein the formula of the flavonoid derivative is represented as right and provided with a flavonoid skeleton, R1, R2, R3, R4 and R5 are H, OH, aromatic sulfonic acid ester group and benzyloxy which can be same or different, the flavonol (quercetin or kaempferol) is reacted with aryl sulfonyl chloride selectively in the presence of organic alkali or inorganic alkali catalyst in organic solvent, or quercetin or kaempferol is selectively protected in organic solvent to be reacted with aryl sulfonyl chloride and de-protection. The invention has simple synthesis, mild reaction conditions and high yield. The invention improves the physiological activity of quercetin, improves relative solubility and resolves the defects in clinical application as low biological utilization, bad adsorption, low effect expression and low activity, and the product can be used as ester soluble anticancer agent, with strong inhibition on the growth of cancer cell and high biological utilization.

Disclosed is a method for enzymatic synthesis of esters of flavonoid and flavonoid derivatives, according to which a reaction medium containing an organic solvent, a glycosylated flavonoid or aglycon flavonoid, an acyl group donor, and an enzymatic catalyst is produced, b) additional quantities of flavonoid and / or acyl donor are optionally added during the reaction, and c) the obtained esters are separated from the enzymatic particles and the solvent. The inventive method is characterized by maintaining the concentration of water and / or alcohol which are formed during the reaction to below 150 mM. Advantageously, the molar ratio of flavonoid to acyl donor in the reaction medium is maintained in the range from 0.01 to 20.00 during the reaction.

The invention belongs to the technical field of beverages, and specifically relates to an akebia trifoliate pectin beverage and a preparation method thereof. Nano level carbon-based solid acid is taken as the catalyst to extract peels of akebia trifoliate so as to obtain akebia trifoliate pectin extract; and then akebia trifoliate pectin extract is taken as the raw material to prepare the akebia trifoliate pectin beverage. The prepared akebia trifoliate pectin beverage contains flavonoid derivatives, which have multiple bioactivities and functions of preventing bacteria and viruses and nourishing liver.

The invention relates to a method for preparing flavonoid derivative containing a pyrazole structural unit, which includes the following steps that: bis(trichloromethyl) carbonate and N,N-dimethylformamide as materials are pre-reacted, so that Vilsmeier reagent is prepared, flavanone-4-hydrazone compound shown as the formula (I) is added in the Vilsmeier reagent under the temperature of 0 DEG C to 5 DEG C, reaction then takes place for 2 to 6 hours after the temperature is raised to 30 DEG C to 80 DEG C, and after the reaction is finished, reaction solution is separated and purified, so that the flavonoid derivative containing the pyrazole structural unit, shown as the formula (II), is obtained; the ratio between the flavanone-4-hydrazone compound, the bis(trichloromethyl) carbonate and the N,N-dimethylformamide is 1:0.6 to 2:2.4 to 7.2; in the formula (I) and the formula (II), R1 of ring A is H or CH3, ring B is unsubstituented, monosubstituented or multisubstituented, n is 1 or 2, and R2 is H, Cl and CH3O. The invention has the advantages of mild reaction conditions, easy operation, high reaction yield, little pollution, environment-friendliness and the like.

The invention discloses a composition and a method for promoting hair growth. The composition comprises flavonoid derivatives and an adenosine compound and especially comprises catechin derivatives and adenosine as active ingredients, and a cosmetic or a pharmaceutically acceptable carrier. In a better embodiment of the invention, the composition comprises a supernatant from a hair follicle mastoid cell culture.

An oral composition for the prevention, reduction or treatment of radiation injury including one or more compounds that regulates cell differentiation and / or cell proliferation, and one or more antioxidants, optionally formulated in a pharmaceutically acceptable carrier for an oral composition. The composition of the present invention may further include optional ingredients such as flavonoids, flavonoid derivatives, selenium, selenium compounds, anti-inflammatories, organic germanium, Korean ginseng, American ginseng, Siberian ginseng and B-complex vitamins. A method for the administration of an oral composition for the purpose of preventing, reducing or treating radiation injury involves orally administering an effective amount of a composition including one or more compounds that regulates cell differentiation and / or cell proliferation, and one or more antioxidants to a person before, during or after radiation exposure. The compositions and methods can be employed to prevent, reduce or treat radiation injury caused by a wide variety of types of radiation exposure.

The invention provides a flavone derivative for treating pancreatic cancer, gastric cancer, leukemia, esophageal cancer, cervical cancer, osteosarcoma, lung cancer, prostate cancer, colon cancer, breast cancer, liver cancer, glioma, ovarian cancer and other diseases and a preparation method thereof.

The present invention relates to a novel geranyl flavonoid derivative with improved water-solubility or a pharmaceutically acceptable salt thereof, a method for preparing the same, and a method for treating cancer using the same. Particularly, the novel geranyl flavonoid derivative of the present invention inhibits the expression of STAT3 target protein by suppressing the phosphorylation of STAT3 (Signal Transducers and Activators of Transcription 3) protein, suggesting that it has cancer cell growth inhibiting effect in various cancer cell lines. Also, the compound of the invention has the effect of reducing the size and weight of a tumor significantly in vivo, so that the geranyl flavonoid derivative or the pharmaceutically acceptable salt thereof can be efficiently used for the treatment of cancer.

The invention relates to a method for producing derivatives of O-α-glucosylated flavonoid, comprising at least one step of incubating a glucansucrase with a flavonoid and at least one sucrose, the flavonoid being a flavonoid which is monohydroxylated or hydroxylated in a non-vicinal manner on the B cycle. The invention also relates to novel O-α-glucosylated flavonoid derivatives, and to the use thereof.

The present invention provides a cannabis-based flavonoid pharmaceutical composition including any one or more selected from the group of Apigenin, Cannflavin A, Cannflavin B, Cannflavin C, Chrysoeriol, Cosmosiin and Flavocannabiside or their synthases, for the prevention and treatment of certain ocular diseases and related disorders.

A method for synthesizing flavonoid derivatives comprises: using o-propargyl alcohol phenol as a raw material, adding an organic solvent to fully dissolve the raw material at room temperature, then adding hydriodic acid, reacting at 40 to 60 DEG C for 1 to 2 hours, after the reaction is finished, spin-drying a reaction solution, separating the reaction solution by silica gel column chromatographyto obtain a target effluent, allowing the effluent to stand in a test tube for 1 to 48 hours, and then converting the effluent into flavonoid compounds, wherein the molar ratio of o-propargyl alcoholphenol to hydroiodic acid is 1:1.5 to 2; the organic solvent is a C1-C4 halogenated hydrocarbon or acetonitrile or nitromethane. The method has the characteristics of mild reaction condition, simple operation, simple and easy raw material, high reaction yield, and the like, and is a good synthesis method with good popularization and application prospect.

The invention discloses a flavonoid derivative as well as a preparation method and application thereof. The flavonoid derivative has a molecular formula of C21H20O6, and has a structural formula of aformula I shown in the description. The preparation method of the flavonoid derivative comprises the following steps: (1) performing bacterium culture on (Nigrospora sphaerica) ZMT05 in a bacterium culture medium; and (2) performing fermentation culture on the bacterium obtained in the step (1) in a fermentation culture medium (containing pagoda tree flowers), performing digestion with an ethanolaqueous solution or a methanol aqueous solution, performing vacuum concentration, further performing extraction by using an organic solvent, and performing further purification through silica gel column chromatography and recrystallization, so as to obtain the flavonoid derivative. The flavonoid derivative disclosed by the invention has good functions of inhibiting citrus penicillium and gloeosporium musarum, can be used as a microbial agricultural antibacterial agent, is feasible in large-scale production of raw materials, and has wide application prospects.

The present invention relates to a cosmetic composition for improving skin wrinkles, which contains biflavonoid derivatives as an active ingredient. The cosmetic composition containing the biflavonoid derivatives of the present invention not only is safe for application on the skin without side-effects but also improves wrinkles caused by UV through procollagen production and MMP-I inhibition.

A Liquid, comprising an hydrophobic flavonoid derivative electrochemically non-active, that is capable of restoring its electrochemical activity, the concentration of the flavonoid derivative being 10 ppm by weight or less, and an organic substance in an amount of 90% by weight or more.

The invention discloses application of a flavonoid derivative GL-V9 and anthracycline antibiotics in preparation of a leukemia treatment medicine, and belongs to the technical field of medicines. It is found that the flavonoid derivative GL-V9 combined with low-dose anthracycline antibiotics can significantly inhibit growth of acute myelogenous leukemia (AML) cells, MTT experiments and U937 cell nude mouse transplantation tumor models verify that the GL-V9 and the low-dose anthracycline antibiotics can play a synergistic anti-AML effect, and the application potential of the combined administration mode in treatment of AML is prompted.

The invention provides an application of a flavonoid derivative GL-V9 in preparation of anti-melanoma drugs. Further research finds that the GL-V9 can significantly inhibit the growth activity of human melanoma A375 cells, and the inhibition rate of the GL-V9 can be close to 100% under a proper concentration condition. Moreover, the GL-V9 can significantly promote early and late apoptosis of A375 cells, and has application prospects in development of anti-melanoma drugs.

The invention provides a flavonoid derivative for treating osteoporosis as well as a pharmaceutical composition and application thereof. The flavonoid derivative has a chemical structure shown as thefollowing formula A. The structural formula is as shown in the description. The product disclosed by the invention is the flavonoid derivative. The influence of estrogen on the reproductive system does not exist in the human body, but the activity of the estrogen can be increased, and the flavonoid derivative has the characteristic of estrogenic osteoporosis resistance and can achieve effects of reducing bone loss and increasing bone mineral density. The main anti-osteoporosis mechanisms are that (1) osteocyte proliferation can be promoted, bone collagen synthesis and mineralization of the bone matrix can be promoted, and the bone mass is increased; (2) proliferation and differentiation of osteoclast precursor cells can be reduced, the activity of the osteoclast is inhibited, and bone resorption is reduced; and (3) calcitonin secretion is increased by virtue of the estrogenic effect, and bone resorption resistance is indirectly produced.

Research finds that a flavonoid derivative GL-V9 can significantly induce expression of antigen-presenting complex on the surface of tumor cells and enhance the potential of tumor cell immunity, which is further proved through a surface antigen detection experiment by a flow cytometer, indicating that the GL-V9 has the application potential of a tumor immunomodulator, and provides a new way and means for effectively treating tumors, especially human melanoma.

A novel flavonoid derivative compound 6-CEPN can protect a brain against ischemia / reperfusion (I / R) injury by attenuating peroxynitrite-mediated mitochondrial autophagy. The infarct volume and neurological impairment score of acute ischemic stroke is significantly improved by 6-CEPN. It is found that the 6-CEPN inhibites excess mitochondrial autophagy activation during brain I / R injury, accompanied by a reduction in the production of peroxynitrite. Specifically, the 6-CEPN inhibites the expression ratio of LC3-II / I and Drp1 in the mitochondrial fraction in a dose-dependent manner, as well as the protein expression of the iNOS and NADPPH oxidase subunit p47phox.

The invention relates to a flavonoid derivative and a preparation method and application thereof. A coupling reaction is used to prepare the flavonoid derivative, 4'-OH is replaced with an amino substituted substance, and a nitrogen-containing derivative is synthesized on a flavonoid skeleton. By introducing the amino substituted substance, hydrogen bonding of the flavonoid derivative and a target protein can be regulated, and at the same time, an ester water partition coefficient can be also regulated, so that the flavonoid derivative can pass a blood-brain barrier relatively well, and thereby plays a role in inhibiting tumor cells. An anti-proliferative activity research of the flavonoid derivative in tumor cells HEL and PC3 is studied by MTT assay, results show that the flavonoid derivative has good anti-proliferative activity against the tumor cells HEL and PC3, and has higher antitumor activity than natural flavonoid apigenin, and the anti-proliferative effect of the flavonoid derivative is similar to that of clinical anti-tumor drug cisplatin.

The invention relates to an application of a flavonoid derivative CPU-008 (7-{4-[bis-(2-hydroxy-ethyl)-amino]-butoxy}-5-hydroxy-8-methoxy-2-phenyl-benzopyran-4-ketone) in preparation of an anti-lymphoma medicine. The CPU-008 can inhibit the growth activity of lymphoma cells, and can cause the apoptosis of the lymphoma cells by reducing the mitochondrial membrane potential of the lymphoma cells.