105 results about "Chrysin" patented technology

The invention discloses a chrysin nitrogen-containing derivative. Nitrogen-containing groups are introduced to a chrysin structure to synthesize the chrysin nitrogen-containing derivative with a novel structure. The molecular structure of the chrysin nitrogen-containing derivative is shown as (I), wherein R represents fatty amidogens of C1-C20, aromatic amidogens of C6-C20, heterocycle-containing amidogens of C1-C20 and alcohol amidogens or benzyl amidogens of C1-C20, and n represents the carbon chains of C2-C20. The derivative can have the biological activities of some similar alkaloids and simultaneously enlarge polarities, and the synthesized derivative presents a certain alkalinity, which is convenient to achieve the purpose of improving the water solubility with inorganic acid or organic acid finished salts.

The invention provides a preparation method of flavonoid glycosides in scutellaria baicalensis. The method is suitable for quickly preparing four flavonoid glycosides comprising baicalin, wogonoside, chrysin-6-C-alpha-L-Arabic glucoside-8-C-beta-D-glucoside and oroxylinA-7-O-glucuronide. The preparation method comprises the following steps of: pulverizing scutellaria baicalensis and then adding water to extract; sequentially carrying out alcohol precipitation and high-speed centrifugation; after membrane separation, loading nonpolar macroporous absorption resin and eluting by alcohol / water; collecting eluent and concentrating and drying to obtain a scutellaria baicalensis macroporous resin component; and obtaining a scutellaria baicalensis effective component through parallel preparing liquid-phase chromatographic separation by using acetonitrile water as a flow phase. The preparation method has good selectivity and high purity of the obtained compound and greatly improves the separation and purification efficiency. The preparation process has high repeatability and good maneuverability, is easy to realize standardization and industrialization and has certain guidance effects on quickly obtaining flavones active constituents in the scutellaria baicalensis.

The invention discloses a chrysin-1,2,3-triazole compound having an antibacterial activity, and its preparation method. A technical scheme adopted in the invention is mainly characterized in that the structural general formula of the chrysin-1,2,3-triazole compound having antibacterial activity is shown in the specification; and in the structural general formula, R can be a halogen atom, a halogenated alkyl group, an alkyl group, an alkoxy group or a nitro group, n1 is not less than 1, and n2 is not less than 0. The invention also discloses the preparation method of the compound, and uses of the compound. The chrysin-1,2,3-triazole compound has an excellent antibacterial performance, can be well used for controlling the animal and plant diseases caused by bacteria and fungi, and has great application prospects in the medicine field, the pesticide field and the like.

The invention belongs to the technical field of medicine, and relates to a method for preparing flavonoids and total flavonoids in Linaria vulgaris and application thereof. The flavonoids and the total flavonoids come from flavonoid compounds in the Linaria vulgaris (including flavonoid compounds such as pectolinarin, aglycon, acetyl pectolinarin, acetyl linarin, acetyl linarin, hesperidin, robinin, hispidulin, luteolin, vanilla lignin, chrysin and the like). Dried whole herbs of the Linaria vulgaris are subjected to reflux extraction by water or alcohol, then a macroporous resin is used to send to a column, alcohols with different concentrations are used for elution, eluents are collected, then different elution flow ingredients pass through a silica gel chromatographic column, a polyamide chromatographic column, a gel chromatographic column and the like, to obtain various compositions, and the content of an obtained total flavonoid substance is more than 60 percent. The flavonoid compounds can be used for preparing medicines for treating angiocardiopathy, cough, and asthma. An extraction method of the invention is simple, practical and cheap, and is suitable for industrialized production.

This invention is to provide multiple specific inhibitors of cytochrome P450 isozyme CYP2C9. These inhibitors can be derived from any combinations with the following compounds including: Tamarixetin, Formononetin, isoliquritigenin, Phloretin, luteolin, Quercitrin, quercetin, myricetin, Wongonin, Puerarin, Genistein, Nordihydroguaiaretic acid, Narigenin, Capillarisin, Chrysin, Fisefin, eriodictyol, 6-Gingerol, Isorhamneti, isoquercitrin, Morin, (+)-Taxifolin, isovitexin, 3-Phenylpropyl Acetate, Oleanolic acid, ursolic acid, β-Myrcene, cinnamic acid, Luteolin-7-Glucoside, Liquiritin, (+)Limonene, Homoorientin, Swertiamarin, Embelin, Daidzein, Poncirin, (−)-Epicatechin, ergosterol. These natural products can be used to enhance the bioavailability of therapeutic agents (drugs).

FtsZ, the bacterial analog of tubulin, is a promising new target for developing new antibiotics. It has been shown that polyphenols inhibit the GTPase activity of FtsZ, thereby inhibiting Z-ring formation during mitosis. The present invention provides novel polyphenols compounds, which can be accessed by the synthesis of dichamametin and 2′″-hydroxy-5″-benzylisouvarinol-B as described herein. These novel compounds are useful in treating infections, particularly infections caused by gram-positive organisms. Methods of preparing the inventive compounds are also provided. The compounds are prepared by the benzylation of pinocembrin or chrysin core structure. Pharmaceutical compositions and method of using the compounds to treat disease are also provided. These compounds may be screened for antimicrobial activity as well as other biological activities such as anti-neoplastic, anti-inflammatory, immunosuppressive, and cytotoxic activity.

The present invention discloses an effective component of total flavonoid extracted from Chinese medicine Chinese lobelia and a preparation method thereof. The preparation material mainly contains apigenin, luteolin, diosmetin, chrysin flavonoid, linarin, dafion, and indican compounds and other derivatives with the dafion as the mother nucleus. The present invention can be obtained by the methods of macroporous absorption resin, polyamide chromatography, solvent extraction and other methods.

The invention relates to a method for simultaneous determination of caffeic acid and 8 flavonoids in propolis by using high performance liquid chromatography. Simultaneous quantitative determination of flavonoids and caffeic acid has not been reported so far. The method provided by the invention is characterized in that a high performance liquid chromatograph is used for determination, the method comprises the procedures consisting of preparation of standard stock solutions, preparation of standard intermediate solutions, preparation of standard working solutions, drafting of standard curves, treatment of samples and determination of the samples, and in the procedure of preparation of the standard stock solutions, a caffeic acid standard stock solution, a rutin standard stock solution, a quercetin standard stock solution, a myricetin standard stock solution, an apigenin standard stock solution, a kaempferol standard stock solution, a pinocembrin standard stock solution, a chrysin standard stock solution and a galangin standard stock solution can be obtained. According to the invention, high performance liquid chromatography is employed for simultaneous determination of caffeic acid and 8 flavonoids in propolis, and pre-treatment of samples is easy and convenient and is rapid to operate.

The invention relates to the technical field of medicinal chemistry, and particularly relates to a chrysin amide derivative type compound as well as a preparation method and medical application thereof. The structural formula of the compound provided by the invention is represented by the formula III, wherein a substituent R in the compound is 2-(aminomethyl)-1-ethylpyrrolidine, piperazine, 1-(2-diethyl aminoethyl) piperidine, N, N-dimethylethylenediamine, N, N-diethyl ethylenediamine or 4-piperidinopiperidine. Those compounds can be applied to the preparation of anticancer medicaments.

The invention relates to the fields of pharmaceutical chemistry and particularly provides a series of nitric oxide-donating chrysin derivatives, which are prepared by modifying the chrysin at position 5 and position 7. The nitric oxide-donating chrysin derivatives release nitric oxide and chrysin derivatives in vivo and therefore can conduct functions of reducing blood sugar and blood pressure, promoting angiogenesis, improving a vascular endothelial function and lipid metabolism disorders and can be used in the preparation of medicaments for treating diabetes, diabetic cardiovascular complications, metabolic syndrome and endothelial dysfunction.

The invention synthesizes novel porphyrin-chrysin derivatives. Porphyrin molecules are used as a carrier, the tumor tissue aggregation effect of the porphyrin molecules is used, meanwhile, the property that the porphyrin molecules can produce singlet oxygen to kill tumor cells is used and combined with natural anti-tumor activity of chrysin, so that the novel anti-tumor compounds are obtained, anda new direction is provided for research on anti-tumor drugs.

The invention relates to a chrysin derivative and preparation thereof and application thereof in treating hyperuricemia, and belongs to the field of pharmaceutical synthesis. By using easily-obtained natural product chrysin as a starting material and selectively introducing active functional groups containing fluorine atoms, chrysin derivatives (I) and (II) are synthesized; a synthetic method is simple and is well operable and high in reaction yield, the obtained chrysin derivatives has significantly enhanced anti-hyperuricemia activity when compared to lead compound chrysin and is useful in treating hyperuricemia.

The invention discloses a chrysin non-natural amino acid derivative or pharmacologically-acceptable hydrate and salt thereof. The chrysin non-natural amino acid derivative comprises a stereoisomer ora tautomer. The chrysin non-natural amino acid derivative comprises the following preparation steps: preparing 5-hydroxy-7-propargylflavone by chrysin and propargyl bromide under the action of alkali;preparing (L / D)-N3-Boc amino acid methyl ester by (L / D)-halogenated-Boc amino acid methyl ester and NaN3 under the action of CuI / L-proline sodium; reacting the 5-hydroxy-7-propargylflavone and the (L / D)-N3-Boc amino acid methyl ester under the action of CuSO4.5H2O / sodium ascorbate, removing Boc groups and hydrolyzing to prepare the chrysin amino acid derivative. The chrysin non-natural amino acidderivative disclosed by the invention has an anti-cancer effect and can be used in preparation of an anti-cancer drug.

The invention discloses a method for synthesizing 5,7-dihydroxy flavone. The method comprises the following steps of: acetylating 1,3,5-trimethoxybenzene to generate 2,4,6-trimethoxybenzene ethyl ketone; condensing the 2,4,6-trimethoxybenzene ethyl ketone and methyl benzoate to generate 1-(2'-4'-6')-trimethoxy-3-phenyl-1,3-propanedione; and performing cyclization and demethylation on the 1-(2'-4'-6')-trimethoxy-3-phenyl-1,3-propanedione to prepare the 5,7-dihydroxy flavone so as to obtain chrysin. In the method, the 1,3,5-trimethoxybenzene is directly taken as a starting raw material, a target product is obtained by performing friedel-crafts acylation reaction, ester exchange, cyclization and demethylation, and the cyclization and the demethylation are performed in one step instead of two steps. The method has the advantages of low cost, low environmental pollution, low equipment requirement and mass production.

The invention relates to an oroxylum indicum general flavone extraction and purification method. Ethyl alcohol backflow and macroporous resin adsorption are used for separating, extracting and purifying oroxylum indicum general flavone, non-flavonoid impurities are removed as many as possible, and finally enrichment is carried out to obtain the high-purity general flavone. The oroxylum indicum general flavone comprises five chemical components including semen oroxyli glycoside B, semen oroxyli glycoside A, chrysin-7-O-beta-D-glucuronide, baicalein and chrysin. The invention further provides application of the oroxylum indicum general flavone to prepating medicine for treating liver cancers. In-vitro pharmacological tests show that the general flavone has the obvious restraining effect on proliferation of liver cancer cells and trends to have the obvious dose-effect relationship, and meanwhile the pharmacological effect is obviously improved along with increase of the purity of the general flavone; in addition, oroxylum indicum general flavone matter analysis studying is carried out, the material basis of oroxylum indicum for playing a role in anti-cancer pharmacological effect is defined, and the material basis and the experiment basis are laid for developing clinical application of oroxylum indicum general flavone enrichment matter, anti-cancer new medicine researching and development and industrial production.

The invention discloses a flavonoid chrysin and amine cyclodextrin clathrate, the amine cyclodextrin is amino-substituted beta-cyclodextrin, amine cyclodextrin and chrysin can generate clathration, ionic interaction of amine cyclodextrin and a phenolic hydroxyl group in amino and chrysin molecular structure is generated, chrysin water solubility of chrysin can be greatly increased, and a chrysin liquid preparation is conveniently formed. The clathrate has the advantages of water solubility, good stability and good external antineoplastic activity. The preparation method is simple, condition is mild, operation is easy, the method can be used for developing a novel chrysin preparation, and has important practical value.

The invention relates to the technical field of medicine detection, and in particular relates to a phlegm-heat clearing injection fingerprint spectrum establishment method and a fingerprint spectrum thereof; the phlegm-heat clearing injection is prepared from scutellaria baicalensis, bear gall powder, cornu gorais, honeysuckle and fructus forsythiae, and a phlegm-heat clearing injection fingerprint spectrum is established by detecting the phlegm-heat clearing injection components by adopting an ultra-high performance liquid chromatography method; the method specifically comprises the followingsteps of S1, preparing a reference substance solution: taking a proper amount of caffeic acid, neochlorogenic acid, chlorogenic acid, cryptochlorogenic acid, 3, 4-dicaffeoylquinic acid and 3, 5-dicaffeoylquinic acid, 4, 5-dicaffeoylquinic acid, forsythiaside D, baicalin, scutellarin, chrysin-7-O-glucuronide, oroxylin-7-O-glucuronide and a wogonin reference substance, and adding methanol to prepare a solution which is 20-50 [mu]g in 1ml. according to the phlegm-heat clearing injection fingerprint spectrum establishment method provided by the invention, the method is simple and convenient to operate, stable in result, high in reproducibility and high in precision.

The invention discloses a method for extracting chrysin from passiflora edulis fruit residue obtained after juicing, which comprises: adding chrysin from passiflora edulis fruit residue obtained after juicing into low-carbon alcohol, regulating the pH value of the obtained mixed solution to 9 to 12 by using alkaline solution, and performing refluxing extraction for 1 to 3 times, 1 to 2 hours eachtime; combining extracting solution, cooling and pumping under vacuum; regulating the pH value of the filtrate to 1 to 3 by using an acid; standing, precipitating, and filtering under vacuum; dissolving a filter cake in ethyl acetate, filtering, and concentrating filtrate to obtain extract; adding low-carbon alcohol into the extract and regulating the pH value to 9 to 12 by using alkaline solution, heating, dissolving and cooling; regulating the pH value to 5 to 7 by using an acid, standing, precipitating, and filtering under vacuum; and washing an obtained filter cake, dying and thus obtaining chrysin. In the method disclosed by the invention, the juiced passiflora edulis fruit residue treated as a waste is used as a raw material for extraction, so the waste is recycled and resources aresaved effectively; and the production method disclosed by the invention is low in production cost, makes a process simple and easy to control, requires short production period and is suitable for industrial production.

The invention discloses a berberine-chrysin pharmaceutical eutectic crystal and a preparation method thereof and belongs to the technical field of pharmaceutical crystallization. The berberine-chrysinpharmaceutical eutectic crystal is prepared by dissolving berberine hydrochloride, chrysin and sodium hydroxide in ethanol according the ratio; a eutectic crystal structure unit comprises berberine cations, chrysin anions and chrysin molecules at the mol ratio of 1 to 1 to 2 and a molecular formula is [C20H18N O4]+[C15H9O4]-2[C15 H10 O4]. The preparation method disclosed by the invention has theadvantages of simplicity and feasibility, low cost and high crystal yield; the relative bioavailability of the chrysin of the prepared pharmaceutical eutectic crystal in rats is remarkably improved relative to the relative bioavailability of the pure chrysin, and the relative bioavailability is 1.7 times as much as the relative bioavailability of the pure chrysin.

The invention provides a small molecule inhibitor of Ebola pseudovirus, particularly small molecule inhibitor of Ebola pseudovirus, wherein the small molecule inhibitor is selected from dPPA, mallotoxin, galangin, epigallocatechin, piceatannol and chrysin. According to the present invention, the experimental results show that the inhibitor can effectively inhibit the entry of Ebola virus into cells.

The invention discloses a method of preparing chrysin. The method comprises the following steps: S1, synthesizing 2'-hydroxyl-4', 6'-dimethoxyl chalcone by 1, 3, 5-triethoxy benzene and cinnamic acid under catalysis of boron trifluoride diethyl etherate; S2, generating 5, 7'-dimethoxyl flavone by 2'-hydroxyl-4', 6'-dimethoxyl chalcone under catalysis of a single substance iodine; and S3, fully demethylating 5, 7'-dimethoxyl flavone to generate chrysin. The method of preparing chrysin provided by the invention improves the synthetic yield of chrysin, is few in synthetic step, low in cost, easy to control and simple to operate, and has a high industrial application prospect, and the raw materials are easily available.

The invention provides a pharmaceutical composition for improving complications of high-fat and high-sugar diet. The pharmaceutical composition comprises flavonoid and an alpha-glucosidase inhibitor, wherein the flavonoid is at least one selected from the group consisting of monomer baicalein, monomer chrysin, organic salts of the monomers and inorganic salts of the monomers, and the alpha-glucosidase inhibitor is one selected from the group consisting of monomer acarbose, monomer voglibose, monomer migltol, organic salts of the monomers and inorganic salts of the monomers. The composition provided by the invention can effectively reduce the dosage of the alpha-glucosidase inhibitor; desired effects can be obtained by mixing the flavonoid with the alpha-glucosidase inhibitor with a dosage 0.01 to 0.75 time of a normal dosage; the disadvantages of a great dosage and great side-effects in individual usage of the alpha-glucosidase inhibitor are overcome; the disadvantages of unobvious hypoglycemic effect, a great dosage, a long administration period and the like in individual usage of the flavonoid are overcome; and the disadvantages of complex components and difficult quality control of a traditional Chinese medicine compound drug are overcome.

The invention belongs to the technical field of Chinese traditional medicine application, and specifically relates to application of chrysin to preparation of drugs for treating obesity-related metabolically triggered inflammations. According to the invention, the chrysin promotes the replacement activation of IL-4 activated mouse macrophages, promotes the release of anti-inflammatory cytokines IL-10, and promotes the rise of enzyme activity of typical labeled molecule arginine for the replacement activation of the macrophages, the up-regulation of surface molecules MGL1 / 2 and the up-regulation of classical molecules CD206, Ym1 and Fizz. Especially, in fat mice C57 / B6 induced by high-fat feeding, the chrysin is capable of inhibiting the release of proinflammatory cytokines TNF-alpha, AST (Aspartate Transaminase) and ALT (Alanine Transferase) in blood serum, increasing the release of the anti-inflammatory cytokines IL-10, alleviating the lesion of liver and adipose tissues, inhibiting the phagocytic function of the peritoneal macrophages, the antigen presentation ability and the release ability of NO, and lowering the expression of the typically activated surface molecules CCR7 and CD80 of the macrophages. According to the invention, a new drug for treating the obesity-related metabolically triggered inflammations is developed.

The invention provides a 6, 8-bis(hydroxymethyl) chrysin, 6, 8-bis(hydroxymethyl) ether chrysin and a method for preparing the same. A preparation process comprises the following steps that: 6, 8-bis(hydroxymethyl) chrysin is obtained by using chrysin as lead compound to react with formaldehyde and potassium hydroxide in methanol; then 6, 8-bis(hydroxymethyl) ether chrysin-5, 7-dihydroxy-6, 8-bis(methoxymethyl) flavone, 5, 7-dihydroxy-6, 8- bis(ethoxy methyl) flavone and 5, 7-dihydroxy-6, 8-bis(butoxy methyl) flavone are synthesized by using the 6, 8-bis(hydroxymethyl) chrysin as an intermediate to react with methanol, ethanol and butanol; a pure product of a compound of the invention can be obtained through recrystallization. The invention also provides a medicine and a composition for treating cardiovascular and cerebrovascular diseases, wherein the medicine and the composition contain the 6, 8-bis(hydroxymethyl) chrysin or 6, 8-bis(hydroxymethyl) ether chrysin with effective therapeutic dose, as well as acceptable vector in pharmacy.

Disclosed are the compositions comprising bioactive components Oroxylin A, Baicalein, Chrysin, and their glucuronides Oroxylin A-7-glucuronide, Baicalein-7-glucuronide and Chrysin-7-glucuronide, isolated from the bark of Oroxylum indicum, and the process of isolating the said bioactives.

The invention discloses pecan leaf extract total flavone with uric-acid lowering effect and a preparation method and application thereof. The pecan leaf extract total flavone contains pinostrobin, pinostrobin chalcone, chrysin and cardamonin whose total mass percentage is 50% or above. The total flavone in pecan leaf is prepared on the basis of the pecan leaf, efficacy of the pecan leaf is developed, and novel medicinal resources of the pecan leaf are expanded. The pecan leaf extract total flavone can remarkably lower serum uric acid level of model rats and can be used for medicaments and healthcare products having main functions of preventing and treating hyperuricemia.

The invention relates to the technical field of pharmaceutical chemistry and in particular relates to a chrysin amide derivative as well as a preparation method and medical application of the derivative. A structural formula of the chrysin amide derivative provided by the invention is shown as a formula I; a substituent group R in the compound is a series of acylamino. The chrysin amide derivativeprovided by the invention has the characteristics of good water solubility, stability and pharmacological activity; the preparation method of each chrysin amide derivative is the same and comprises the following steps: connecting 7th-site hydroxyl of chrysin with ethyl bromoacetate and then hydrolyzing; finally, carrying out amide condensation reaction on a series of amide compounds respectively,so as to obtain a series of chrysin amide derivatives. A pharmacodynamic screening experiment result shows that compared with the chrysin, the compound has better water solubility and better uric acid lowering and gout and inflammation resisting effects and is a compound which has a prospect of being developed into a novel anti-gout drug.

The invention provides an application of flavonoids compounds in the preparation of a T lymphocyte subsets regulating drug. The innovative discovery of the invention is that the flavonoids compounds can regulate the proportion of T lymphocyte subsets, so that the effect of immune system is regulated, and the related pathological injury can be cured. Specifically, the proportion of a CD4+IFN-gamma+Th1 cell subset, a CD4+IL-17+Th17 cell subset and a CD4+CD3e+CD62L+ThO cell subset can be lowered, and the proportion of CD4+CD25+Fo8*p3+Treg cell subset is increased. Chrysin can maintain the integrity of the blood-retinal barrier of an EAU mouse, inhibit the macrophage infiltration, and inhibit the intraocular inflammation. At the same time, the expression quantity of retinas STAT1, STAT3 and phosphorylated protein is inhibited. Based on new properties of the flavonoids, the flavonoids can be applied for curing a plurality of diseases with the effect of proportional imbalance of T cell subsets.

Indian trumpetflower seed is a common traditional Chinese medicine and contains main chemical components of flavonoid compounds, such as baicalein, chrysin, Oroxin A, Oroxin B, baicalin and the like, wherein the Oroxin B is a special component of the Indian trumpetflower seed and can serve as an important index for quality control of the Indian trumpetflower seed medicinal material. An identification method and a contrast for the special component have not been present under the item of Indian trumpetflower seed in the first part of 2005 version Chinese Pharmacopoeia. The Oroxin B prepared by separation serving as a contrast in a thin-layer identification method for the specificity of the traditional Chinese medicine Indian trumpetflower seed, has been written under the item of the traditional Chinese medicine Indian trumpetflower seed in the first part of 2010 version Chinese Pharmacopoeia, and is about to serve as the content of Chinese Pharmacopoeia to be published and implemented. A method for preparing the special component of traditional Chinese medicine Indian trumpetflower seed, namely Oroxin B is invented by scientific research personnel of Institute of Chinese Materia Medica, China Academy of Chinese Medical Sciences through years of experiments. The Oroxin B is prepared by ethanol extraction, polyamide separation, and glucan gel purification.