31 results about "Aurone" patented technology

The present invention has an object to provide an agent for strengthening calcium-containing tissues, which can be safely applied; and its use: The present invention solves the object by providing an agent for strengthening calcium-containing tissues, which comprises one or more flavones, flavonols, flavanones, flavanonols, anthocyanidins, flavanols, chalcones, and aurones.

The invention discloses an aurone mannich base compound and pharmaceutically acceptable salts, a preparation method, a pharmaceutical composition and application thereof in preparation of medicines for treatment and / or prevention of neurodegeneration related diseases. The neurodegeneration related diseases include but not limited to vascular dementia, Alzheimer's disease, Parkinson's disease, Huntington's disease, HIV (human immunodeficiency virus) related dementia, multiple sclerosis, progressive lateral sclerosis of spinal cord, neuropathic pain, glaucoma and the like.

at least one aurone or a natural or synthetic derivative of aurone, or an analogue of aurone, in which the independent phenyl ring can be substituted by a heterocycle of pyrrole, imidazole, triazole, pyridine, furan, or thiophene type, is disclosed as a cosmetic agent, or as an active substance, for the manufacture either of a cosmetic composition, or of a pharmaceutical composition, notably a dermatological composition, having a melanogenesis-inhibiting activity or a depigmenting activity, or an anti-tyrosinase activity.

The invention relates to a synthesis method of a hydroxy aurone compound, and particularly relates to a preparation method of a 4-hydroxy aurone compound. The preparation method is as below: reacting raw materials comprising 2',6'-dihydroxy acetophenone and a benzaldehyde derivative; first protecting 2',6'-dihydroxy acetophenone with one hydroxy; then conducting condensation and cyclization on the 2',6'-dihydroxy acetophenoneand benzaldehyde derivative; and conducting deprotection to obtain the 4-hydroxy aurone compound. The 4-hydroxy aurone compound has a structural formula as below; and R represents any substituent group. Compared with the existing method, the preparation method provided by the invention has advantages of low price of raw materials, high yield, short reaction time, simple and mild reaction conditions, and simple operation, etc.

There is provided a gene coding for the amino acid sequence listed as SEQ ID NO: 2 or SEQ ID NO: 70, for example. Co-expression of the 4′CGT gene and AS gene in a plant lacking natural aurone synthesis ability is carried out to successfully accumulate aurones and alter the flower color to have a yellow tint. In addition to the expression of both genes, the flavonoid pigment synthesis pathway of the host plant itself is inhibited to obtain flowers with a more defined yellow color.

The invention relates to a 6-aryloxy acetoxy aurone compound and an application thereof on a pesticide, and belongs to the technical field of herbicides. The general formula of the 6-aryloxy acetoxy aurone compound is as shown in the specification, wherein R1 is hydrogen, halogen, C1-C4 haloalkyl, C1-C4 alkyl, C1-C4 alkoxy and C1-C4 alkylamino, and R2 is the hydrogen and the C1-C4 alkyl. The invention provides a lot of novel chemical structures and novel compounds. A biological activity measurement result indicates that the compound I has very high weeding activity.

Esters of flavonoids, including flavones, flavonols, flavanones, flavanols, flavanolols, isoflavones, anthocyanins, proanthocyanidins, chalcones, aurones and hydroxycoumarins conjugated by an ester bond to a ω-substituted C6 to C22 fatty acid are provided. The esters may be used in cosmetic, pharmaceutical, and nutritional preparations.

Compounds are disclosed that are designed to mimic the activity of combretastatin A-4 based on chalcone, aurone, or indanone structures, or involving benzoquinone or quinone rings. The anti-cancer activity of exemplified compounds is demonstrated in a range of in vitro and in vivo assays.

The present invention provides a protein having aurone synthase activity involved in the color of flowers such as snapdragons, a gene that encodes it, cDNA in particular, and its applications. This gene can give yellow color to the flowers of plants by introducing into plants deficient in chalcone isomerase and so forth and expressing.

The present invention provides a composition for diagnosing amyloid-related diseases, comprising a compound represented by general formula (I):wherein X represents O or the like; R1, R3, R4, R5, R6, R8 and R9 represent a hydrogen atom or the like; R2 represents a halogen atom or the like; and R7 represents a dimethylamino group or the like;or the compound labeled with a radionuclide, or a pharmaceutically acceptable salt of the compound or the labeled compound. The compound represented by general formula (I) has all of the following properties: high binding specificity to amyloid β protein, high permeability through the blood-brain barrier, and rapid clearance from sites without senile plaques in the brain.

The invention discloses an aurone compound, and a preparation method and application thereof. The aurone compound is extracted from aromatic tobacco, the 4' site is acetyl, the structural formula is shown in the specification, and the aurone compound is named as 4'-acetyl-5-hydroxy-6-methoxy aurone. The preparation method of the aurone compound comprises the following steps: treating raw materials, performing ultrasonic extraction, performing silica gel column chromatography, separating through high pressure liquid chromatography, and performing gel column chromatography. The aurone compound is applicable to the preparation of medicaments for resisting leukemia cells and / or human breast cancer cells. The aurone compound disclosed by the invention is separated out from aromatic tobacco for the first time, and the molecular formula and structure of the aurone compound can be confirmed. According to the invention, ethanol is used as solvent, thereby causing less environmental pollution, and ensuring high safety and environment friendliness; and the compound is simple in structure and easy to artificially synthesize. The compound has obvious inhibiting effect on leukemia cells (NB4) and human breast cancer cells (MCF7), and the IC50 values are respectively 2.6mu M and 1.8mu M, thus indicating that the aurone compound can be used as a lead compound of anticancer medicaments.

A composition for the diagnosis of diseases relating to amyloid which contains either a compound represented by the general formula (I): [wherein X represents O, etc.; R, R, R, R, R, R, and R each represents hydrogen, etc.; R represents halogeno, etc.; and R represents dimethylamino, etc.] or a compound obtained by labeling that compound with a radionuclide or contains a pharmaceutically acceptable salt of any of these compounds. The compound represented by the general formula (I) has high bonding specificity for amyloid ss-protein, is apt to highly pass through the blood-brain barrier, and has the property of rapidly disappearing from the areas excluding senile plaques in the brain.

Aurone, including aureusidin-6-O-glucoside, are known to have antioxidant properties. The compounds are produced in the flowers snapdragon (e.g., Antirrhinum majus) and have been suggested for potential medicinal use. The present methods use recombinant and genetic methods to produce aurone in plants and plant products. In particular, the present methods have resulted in the production of aureusidin-6-O-glucoside in the leaves of various plants.

The invention discloses a method for preparing an aurones compound, and belongs to the technical field of chemical synthesis. The preparation method comprises the following steps of: in an organic solvent, performing reaction on halogenated epoxy chalcone ketone serving as a raw material at 80-140 DEG C for 2.5-5.5 hours in the presence of a copper catalyst, a ligand and an alkaline substance; performing aftertreatment after the end of reaction to obtain the aurones compound. According to the method, halogenated epoxy chalcone ketone is used as the raw material and is reacted to obtain a series of aurones in the presence of the copper catalyst, the ligand and the alkaline substance; epoxy during reaction is subjected to ring opening and cyclization so as to obtain five-membered rings or Z type structures. The compound is high in regioselectivity and stereoselectivity, and has easily-available raw materials for reaction; the catalyst is low in cost so as to avoid using the catalyst which is high in cost and is serious in environment pollution; according to the method, raw materials can be easily obtained, the operation is easy, the reaction condition is mild, the yield is high, the catalyst is low in cost, and the yield is up to more than 80 percent; the method has high application value and social economic benefit and is suitable for industrial production.

The invention discloses an aurone mannich base compound and pharmaceutically acceptable salts, a preparation method, a pharmaceutical composition and application thereof in preparation of medicines for treatment and / or prevention of neurodegeneration related diseases. The neurodegeneration related diseases include but not limited to vascular dementia, Alzheimer's disease, Parkinson's disease, Huntington's disease, HIV (human immunodeficiency virus) related dementia, multiple sclerosis, progressive lateral sclerosis of spinal cord, neuropathic pain, glaucoma and the like.

There is provided a gene coding for the amino acid sequence listed as SEQ ID NO: 2 or SEQ ID NO: 70, for example. Co-expression of the 4′CGT gene and AS gene in a plant lacking natural aurone synthesis ability is carried out to successfully accumulate aurones and alter the flower color to have a yellow tint. In addition to the expression of both genes, the flavonoid pigment synthesis pathway of the host plant itself is inhibited to obtain flowers with a more defined yellow color.

The invention provides a method for carrying out a trans-Micheal addition reaction by taking a compound with an aurone skeleton as a receptor, and belongs to the technical field of chemical synthesis.According to the method, a reaction can be carried out under the conditions that Sc(OTf) 3 is used as a catalyst, the temperature is 80 DEG C and dichloromethane is used as a solvent. According to the method provided by the invention, the alpha-functionalized trans-Michael addition product of oxadiene is obtained through a negative hydrogen migration / aromatization / dearomatization / cyclization reaction by taking a carbonyl group conjugated with an aurone skeleton compound and a double bond as a receptor for Michael addition under the catalysis of Lewis acid. The method is simple and practical to operate, efficient and convenient in reaction, wide in substrate applicability and extremely high in atom economy.

Provided herein are semisynthetic aurones, pharmaceutical compositions, and methods of treating cancer. The semisynthetic aurone compound including a structure according to Formula (I) or pharmaceutically acceptable salt thereof, where R1 is H, an alkyl cyano, an alkyl phenyl substituted with one or more halogens, or any combination thereof, and R2 is an aromatic group, a heterocycle, or a combination thereof. The pharmaceutical composition includes the semisynthetic aurone compound and a carrier. The method includes administering to a patient in need of such treatment an effective amount of the semisynthetic aurone compound.

The present invention provides a protein having aurone synthase activity involved in the color of flowers such as snapdragons, a gene that encodes it, cDNA in particular, and its applications. This gene can give yellow color to the flowers of plants by introducing into plants deficient in chalcone isomerase and so forth and expressing.

The invention relates to aurones and extracts comprising them useful in the prophylactic and / or therapeutic treatment of an animal (including a human) with an estrogen receptor (ER) related disease or condition of the animal or human body, as well as methods, uses and other inventions related thereto.

The invention discloses an aurone compound, and a preparation method and application thereof. The aurone compound is extracted from aromatic tobacco, the 4' site is acetyl, the structural formula is shown in the specification, and the aurone compound is named as 4'-acetyl-5-hydroxy-6-methoxy aurone. The preparation method of the aurone compound comprises the following steps: treating raw materials, performing ultrasonic extraction, performing silica gel column chromatography, separating through high pressure liquid chromatography, and performing gel column chromatography. The aurone compound is applicable to the preparation of medicaments for resisting leukemia cells and / or human breast cancer cells. The aurone compound disclosed by the invention is separated out from aromatic tobacco for the first time, and the molecular formula and structure of the aurone compound can be confirmed. According to the invention, ethanol is used as solvent, thereby causing less environmental pollution, and ensuring high safety and environment friendliness; and the compound is simple in structure and easy to artificially synthesize. The compound has obvious inhibiting effect on leukemia cells (NB4) and human breast cancer cells (MCF7), and the IC50 values are respectively 2.6mu M and 1.8mu M, thus indicating that the aurone compound can be used as a lead compound of anticancer medicaments.

The invention provides a compound with an anti-inflammatory effect or a pharmaceutically acceptable salt, a solvate, an isomer, a prodrug molecule or a metabolite thereof, and the chemical formula ofthe compound is 6-hydroxy-4-methoxy-5, 7-dimethyl aurone. The compound provided by the invention has a relatively strong inhibition effect on generation of mouse RAW264.7 macrophage PGE2 induced by lipopolysaccharide (LPS), the activity of the compound is superior to that of ibuprofen, and the compound has certain anti-inflammatory activity; and mouse acetic acid twisting tests show that the compound has a certain analgesic effect.

A pyrroline derivative with a spirane structure has significant physiological activity in fields such as antibiosis and antiviral actions. The invention relates to an asymmetric synthesis method for apyrroline derivative. According to the asymmetric synthesis method, an ethyl isocyanoacetate compound and an aurone derivative are adopted for a 1,3-dipolar-cycloaddition reaction. Through the reaction, a spirane pyrroline derivative with three continuous chiral centers can be rapidly and efficiently established, and very good atom economy can be achieved. The asymmetric synthesis method is easyin substrate preparation, low in price, in addition, mild in reaction condition and simple in operation, a target compound can be prepared with a high yield and high enantioselectivity without anhydrous anaerobic operation, and the substrate application range is wide.

The invention discloses a synthesis method of an aurone compound. The synthesis method comprises the following steps of (1) uniformly stirring phenylacetylene and a phenylacetylene derivative, slowly dripping n-butyllithium, reacting for 30min, and dripping a benzaldehyde derivative to react, so as to obtain an intermediate product, wherein the mass ratio of phenylacetylene to benzaldehyde derivative is 1.6:1, and the mass ratio of n-butyllithium to benzaldehyde derivative is 1.5:1; (2) adding the intermediate product obtained in step (1) into potassium carbonate powder which is equal to 2.2 molar times of the benzaldehyde derivative, adding anhydrous toluene or phenol to fully stir and dissolve under the protection of inert gas, adding lead nitrate crystal which is equal to 2.2 molar times of the benzaldehyde derivative or potassium carbonate powder which is equal to 1 molar time of the benzaldehyde derivative, heating to reflux for 2h, purifying by a silica gel column, and diluting, so as to obtain a final product. The synthesis method has the advantages that the reaction steps are simple, the yield rate of obtained aurone compound is high, and the stereo selectivity is good.

The present invention has an object to provide an agent for strengthening calcium-containing tissues, which can be safely applied; and its use: The present invention solves the object by providing an agent for strengthening calcium-containing tissues, which comprises one or more flavones, flavonols, flavanones, flavanonols, anthocyanidins, flavanols, chalcones, and aurones.

The invention belongs to the technical field of pesticides, and particularly relates to a spiro indolinone compound, and a preparation method and application thereof. According to the preparation method, a dispiro[benzofuranone-2,3'- pyrrolidone-2',3''-indolinone] compound is obtained by dissolving an N-substituted indigo derivative, alpha-amino acid and an aurone derivative in an organic solventaccording to a certain proportion in a one-pot synthesizing mode, removing the organic solvent after a TLC detection reaction is ended and recrystallizing; and the preparation method is simple. The dispiro[benzofuranone-2,3'- pyrrolidone-2',3''-indolinone] compound disclosed by the invention shows good activity to plant virus, and particularly has a very good prevention and treatment effect on preventing and treating tobacco mosaic virus.

The invention relates to a hair colour composition, in particular a hair colour composition comprising a flavonoid, a catalyst consisting of iron (II) or cobalt (II) complexed to a non-proteinaceous heterocyclic macrocycle ligand composed of pyrrole or pyrroline subunits, and either a hydrogen peroxide generator or 0.0001 to less than 1.5% w / w hydrogen peroxide. The flavonoid is selected from the group consisting of flavones, isoflavones, flavans, isoflavans, flavanones, flavonols, flavan-3-ols, dihydroflavon ol, flavanonols, proanthocyanidins, aurones, chalcones, dihydrochalcones, flavonolignans, and derivatives thereof, wherein the hair colour composition has a pH of 4.5 to 8.0, preferably 5.5 to 7.5.

A pyrroline derivative with a spirane structure has significant physiological activity in fields such as antibiosis and antiviral actions. The invention relates to an asymmetric synthesis method for apyrroline derivative. According to the asymmetric synthesis method, an ethyl isocyanoacetate compound and an aurone derivative are adopted for a 1,3-dipolar-cycloaddition reaction. Through the reaction, a spirane pyrroline derivative with three continuous chiral centers can be rapidly and efficiently established, and very good atom economy can be achieved. The asymmetric synthesis method is easyin substrate preparation, low in price, in addition, mild in reaction condition and simple in operation, a target compound can be prepared with a high yield and high enantioselectivity without anhydrous anaerobic operation, and the substrate application range is wide.

The invention provides a method for carrying out a trans-Micheal addition reaction by taking a compound with an aurone skeleton as a receptor, and belongs to the technical field of chemical synthesis.According to the method, a reaction can be carried out under the conditions that Sc(OTf) 3 is used as a catalyst, the temperature is 80 DEG C and dichloromethane is used as a solvent. According to the method provided by the invention, the alpha-functionalized trans-Michael addition product of oxadiene is obtained through a negative hydrogen migration / aromatization / dearomatization / cyclization reaction by taking a carbonyl group conjugated with an aurone skeleton compound and a double bond as a receptor for Michael addition under the catalysis of Lewis acid. The method is simple and practical to operate, efficient and convenient in reaction, wide in substrate applicability and extremely high in atom economy.