97 results about "Flavone derivatives" patented technology

Compositions of matter and methods wherein chalcone and flavone derivatives are administered to human or veterinary patients for the treatment of bladder or urinary tract cancer. Compounds of the invention include 2′-hydroxy-4,4′,6′-trimethoxychalcone (Flavokawain A).

The use of flavone derivatives of formula (I) in which R1, R2, R3, R4 and R5 independently represent hydrogen, hydroxy or an ester group; R6 represents hydrogen, hydroxy, an ester group or an O-glycoside group such as O-rhamnose, O-glucoside, O-retinoside or O-xyloside; and represents a single bond or a double bond; or the pharmaceutically acceptable salts thereof as TNFα antagonists or inhibitors.

The present invention relates to flavone derivatives in the structure as shown, and their preparation process and intermediate. These compounds have excellent PDE5 inhibiting activity, and may be applied in treating sexual disorder and vasoconstriction related diseases.

The invention relates to a fluorescence enhancement type hydrogen sulfide fluorescent probe and particularly relates to a fluorescence enhancement type hydrogen sulfide fluorescent probe based on flavone derivatives. Flavone derivatives are directly reacted with 2,4-dinitrofluorobenzene, and a reaction product is subjected to column chromatography to generate a pure probe product. According to the fluorescence enhancement type hydrogen sulfide fluorescent probe, probe molecules have the maximum absorption wavelengths of 460nm, relatively good solubility in a 1.5mM CTAB water solution and stable optical performance; by adding the probe molecules together with hydrogen sulfide, the absorption wavelengths are blueshifted from 460nm to 450nm, and the intensity of a fluorescence spectrum is continuously enhanced at 612nm and is maximally enhanced by 96 times. According to the fluorescence enhancement type hydrogen sulfide fluorescent probe, the deficiencies that an existing fluorescent probe is slow in response to hydrogen sulfide and high in detection line, and detection wavelengths are in a visible light region are overcome; the probe molecules are high in sensitivity, stable in optical performance, relatively high in synthetic yield, strong in capability of identifying hydrogen sulfide, high in response speed, wide in detection range and low in detection lower limit, the response range is 0-50 mu M, and the detection limit is 0.09 mu M; therefore, the fluorescent probe has practical application values in the fields of biological chemistry, environmental science and the like.

A fluoric isoflavone derivative and its preparing process are disclosed. Said derivative can be used to prepare the medicines for treating cancer, hypertension, hyperglycemia, dysphoria and bacterialand viral diseases. Its advantages are high curative effect and low poison.

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 invention relates to the medicine field and provides an application of flavone derivative as anti-oxidation and anti-anoxia drugs or food. The compound has the structural formula on the right. The preparation method of the flavone derivative comprises the following operation steps: the whole herb of Uncinata Spikemoss Herb is ground and extracted by solvent or water in a reflux way; an initial extract is obtained by filtering or centrifugally removing undissolved substances and decompression drying; the initial extract is dispersed in water of equal volume and again extracted by chloroform, ethyl acetate and normal butanol sequentially; ethyl acetate extract liquor is taken and decompressed and dried in vacuum to obtain the ethyl acetate extract; and the flavone derivative is obtained by chromatography separation and refining.

The disclosed polymethoxyflavone derivative with anticancer activity belongs to the acceptable sodium salt, potassium salt, sulfate, hydrochlorate, halogen compound or ester compound of the compound with general formula shown as (I)~(IV) or itself. This product also has small side effect with low cost.

The invention relates to an isoflavone derivative and a preparation method and application thereof, which belong to the field of chemical medicaments. The technical problem solved by the invention is to provide the isoflavone derivative and the preparation and the application thereof. The isoflavone derivative has a structural formula as shown by (I), wherein R1 and R2 in the structural formula are C1-C5 alkyls. The isoflavone derivative has a significant effect of resisting Coxsackie viruses, can be used for preparing medicaments for resisting the Coxsackie viruses, and has an intensive application prospect.

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.

The invention discloses perilla seed-tartary buckwheat bran spot-removing and shaping tea, which is characterized by comprising the following components in parts by weight: 40-45 parts of rutin, 40-45 parts of cubeb litsea tree fruit, 40-45 parts of perilla seed, 40-45 parts of white mulberry boot-bark, 40-45 parts of tuber fleeceflower root, 40-45 parts of ginseng and 25-30 part of glycyrrhizic acid. The tea is made from natural raw materials and contains remarkable rutin, alpha-linolenic acid, saponin, vitamin E and a flavone derivative. The tea contains various beneficial ingredients, so that fat synthesis can be prevented, and fat accumulation is prevented and eliminated. The tea has spot-removing and weight-losing functions.

The invention concerns novel flavone and isoflavone derivatives of formulae (Ia) and (Ib) wherein: X represents a group of formula —COOR, or —PO(OR)2; R represents a hydrogen atom or an alkaline or alkaline-earth metal, or a lower alkyl group; R1 represents a hydroxy group, a lower alkoxy group or an acyloxy group; R2 and R3, identical or different, represent a hydrogen or halogen atom, or a trifluoromethyl group, a trichloromethyl group, a hydroxy group, an alkoxy group or an acyloxy group comprising 1 to 5 carbon atoms, or R2 and R3 can combine to form an alkylene dioxy group. The invention is useful for rheumatic diseases.

The invention discloses a flavone derivative and the application thereof. The flavone derivative is a compound with multiple target points and multiple functions for preventing Alzheimer's diseases. The compound and a pharmaceutical salt thereof can be applied to preparation of corresponding medicines, and the compound can be also applied to antioxidants, multiple enzyme inhibitors and metal chelating agents.

The present invention provides one kind of nitrogen atom-containing polysubstituted flavone derivatives, 2-substituent phenyl-5, 7-dioxy-8-amino methylene flavone derivatives, which are synthesized through introducing different amino methylene structures into the 8-position of flavone kernel. Pharmacological activity experiments shows that the 2-substituent phenyl-5, 7-dioxy-8-amino methylene flavone derivatives have certain antitumor activity, high selectivity and cell period inhibiting effect and may be applied in antitumor medicine. The present invention has the general structural expression of the 2-substituent phenyl-5, 7-dioxy-8-amino methylene flavone derivatives shown.

Disclosed herein is the extraction, separation, and preparation of plant medicinal extracts to provide compositions containing enriched and isolated flavone derivatives of formula I and long chain fatty acid derivatives of formula II from natural plants, wherein R1, R2, R3, R4, R5, X, A, B and n1 are as defined in the specification. These extracts are used to control, i.e., prevent and treat, prostate diseases.

Disclosed is a use of flavones derivatives and flavanone derivatives in preparation of sedative and hypnotic drugs.

The invention discloses a CYP1B1 enzyme targeting probe precursor for radioactivity <18> F labeling. The probe precursor comprises an affinity ligand capable of being combined with CYP1B1 enzyme, a chelating group capable of being used for 18F rapid labeling and a connecting chain used for connecting the ligand and the chelating group; wherein the connecting chain comprises a plurality of ethyleneglycol fragments; the affinity ligand is an alpha-naphthalene flavone derivative, and the chelating group capable of being used for 18F rapid labeling is a 1, 4, 7-triazacyclononane-1, 4-diacetic acid molecule. The CYP1B1 enzyme targeting probe precursor is a molecular probe precursor which can be combined with tumor-specific expressed CYP1B1 enzyme and can be used for 18F labeling, and after radiolabeling, the level of the CYP1B1 enzyme in tumors can be displayed in PET imaging, so that the tumors are visualized. The invention can effectively promote the application of a molecular imaging technology in tumor diagnosis.

The invention discloses a biflavone derivative fluorescent probe, a preparation method thereof and application of the biflavone derivative fluorescent probe in brain glioma imaging. The chemical nameof the biflavone derivative fluorescent probe is 1, 4-phenyl bis (4-oxo-4H-benzopyran-2, 3-diyl) diacrylate (PPDC), and the molecular formula of the biflavone derivative fluorescent probe is C30H22O8.The probe PPDC is obtained through two-step synthesis, shows great Stokes shift (261 nm), and can effectively overcome the defect of biological application blockage caused by fluorescence self-absorption. Fluorescence analysis research shows that the compound can be used for high-sensitivity detection of cysteine with the detection limit being 0.01 mu M; in addition, the probe can be used for effectively distinguishing interferent glutathione and homocysteine of cysteine in an organism. Accurate detection of trace cysteine in brain glial cells is helpful for early diagnosis of brain glioma. In view of the defects of current brain glioma in early detection and accurate excision, the method is expected to realize accurate surgical navigation in clinical surgical excision of the brain glioma, and has a good application prospect.

The invention relates to a method for synthesizing a 3-aryl flavone or coumarin compound through photo-initiation, and applications of the 3-aryl flavone or coumarin compound. The synthesis method comprises the following steps: exciting a flavone substance by visible light under an alkaline condition, and carrying out a monon transfer reaction with an aryl halide to initiate free radicals so as togenerate a 3-aryl flavone derivative in one step. According to the invention, the photoreaction activity of flavone and coumarin compounds under alkaline conditions is utilized, and the 3-aryl flavone or coumarin compound is synthesized through a one-step method by initiating free radicals through a single electron transfer reaction between a photo-excited flavone or coumarin compound and aryl halide, so that the method is simple and efficient, raw materials and reagents are cheap and easy to obtain, the reaction yield is high, few byproducts are produced, and the chemical and regioselectivity of the reaction is high.

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 invention provides a flavone derivative, a preparation method and application thereof, and a whitening product containing the flavone derivative. The flavone derivative is a compound provided witha structure shown as a formula I or a formula II. The flavone derivative is prepared through the method that flavonoid compounds and phenylacetaldehyde compounds are taken as raw materials, and underthe acid environment, reaction is conducted in an organic solvent. Styryl is adopted to modify the flavonoid compounds, the obtained flavone derivative can significantly inhibit melanin production and resist oxidation, the effect of the flavone derivative is superior than the effect of the unmodified flavonoid compounds and alpha-arbutin commonly used in the market, and the flavone derivative canbe used for preparing products such as whitening skin care products, cosmetics, drugs, health care products or foods.

The invention belongs to the technical field of medicine, and relates to hydroxy flavone derivatives and application of platelet aggregation resistance thereof. A structural general formula of the hydroxy flavone derivatives is shown as follow; and acid addition salts applicable to the hydroxy flavone derivatives and analogs thereof pharmaceutically can be used as the platelet aggregation inhibitor. In a structural formula I and a structural formula II, R1, R2, R3, R4 and R5 are the same or different, and can be H, halogen, OH, CF3, NO2, NH2, CH3 and OCH3; and R' and R'' are the same or different, and can be the H, the halogen, CH2OH, COOH and CH2Cl. The method for synthesizing compounds is prepared by Baker Venkataraman recomposition and concentrated sulfuric acid cyclization and other methods. The method for synthesizing the compounds is simple, is applicable to industrial production, and is steadier than natural analogs. A biological activity assay shows that the compounds have activities of analgesis, anti-inflammation and anticoagulation, and are the platelet aggregation inhibitor.

The invention discloses a crystal form of a 7, 8-dihydroxy flavone derivative and a preparation method and application thereof. The crystal form A of the 7, 8-dihydroxy flavone derivative shown as a formula I has high solubility in water, high stability in a high-humidity condition, extremely low hygroscopicity and high bioavailability, and the preparation method is simple. The crystal form A is of important value in optimization and development of drug.

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 invention discloses a flavone derivative-copper complex as well as a preparation method and application thereof. 6,2-flavonoid dicarboxylic acid and N-methyl pyrrolidone are adopted as ligands, copper ions are adopted as central ions, a complex of flavone derivative-copper is prepared through reactions, and the structure of the complex is represented. The invention furthermore studies anti-tumor activity of the flavone derivative-copper complex, control tests show that the complex has cytotoxicity on malignant cells, but has very low toxicity on normal cells. Due to formation of the flavone derivative-copper complex, the anti-tumor activity of a flavone compound is improved, and the complex has the potential of being applied to medicine development.

A soluble antioxidant flavone derivative, its production and use are disclosed. The process is sulfonating for daidzin or genistein and salting. It can remove hydroxyl-free radical or superoxide anion free radical.

The present invention provides a 3′,4′,5-trimethoxy flavone derivative and a pharmaceutically acceptable salt thereof, preparation thereof, and a pharmaceutical composition for the treatment and prevention of dry eye syndrome comprising the same as an active ingredient.The 3′,4′,5-trimethoxy flavone derivative and its pharmaceutically acceptable salt inhibit corneal damage through excellent stimulatory action on mucus secretion in the conjunctiva and therefore may be effective as a prophylactic or therapeutic agent for dry eye syndrome.