60 results about "Scutellarein" patented technology

The invention relates to a novel scutellarin aglycon 4 (1)-position carbamate derivant (1), a preparation method and the application thereof. A pharmacological experiment proves that the compounds have obvious inhibitory activity of acetylcholinesterase and have protective effect with different degrees on PC12 cell trauma induced by H2O2, so the compounds can be used for preparing the drugs for treating neurodegenerative diseases such as vascular dementia, AD (presenile dementia), etc.

The invention relates to the research field of medicinal chemistry, in particular to a novel scutellarein-6-site derivative (I), as well as a preparation method and an application thereof to medicines for preventing and treating thrombus. Pharmacological test results show that compared with scutellarin and scutellarein, the compound has better function of inhibiting platelet aggregation. The scutellarein-6-site derivative (I) provided by the invention can be used for treating a series of diseases caused by the thrombus, such as myocardial infarction, ischemia injury and so on.

The invention discloses a novel scutellarein derivative, the method for preparing the same and the application. It is proved through pharmacological test that the compound possesses obvious effect against lipid peroxidation, effect against cell damage induced by H2O2 and cell apoptosis induced by A beta, it can also inhibit Cu2+ from inducing oxidation and modification for low density lipoprotein. The compound can be used to prepare medicine that can prevent or treat neurodegenerative diseases such as Alzheimer's disease caused by free radical oxidation, and medicine that can treat inflammation, reduce blood fat and treat atherosclerosis.

The invention discloses a radix scutellariae total flavonoids aglycon extract, also a preparation method of radix scutellariae total flavonoids aglycon extract and functions of treating and resisting renal fibrosis. Content of total flavonoids aglycons in the radix scutellariae total flavonoids aglycon extract is 45-70%. The extract is mainly composed of scutellarein, wogonin, oroxylin A and other aglycons. The preparation method of the extract is as follows: crushing radix scutellariae roots, screening by a No. 1 screen; adding 1-5 times amount of water, uniformly stirring, keeping temperature for enzymolysis at 32-40 DEG C for 5-9 hours, baking under vacuum at 60 DEG C, adding 2-8 times amount of ethyl acetate, continuously extracting for 6-10 hours, depressurizing, recycling solvent, thus obtaining total flavonoids aglycon extract. The extract can obviously relieve renal fibrosis symptoms when irrigated into a mouse stomach with renal fibrosis caused by mercuric chloride moulding and when a group of mice having the extract is compared with group of mice without having the extract. Results suggest that the total flavonoids aglycon extract has a dose dependence in preventing renal fibrosis.

The invention discloses the application of radix scutellariae and flavonoid against sub-type infection of influenza virus A (H1N1), and the application of scutellarein, baicalin and total flavonoid extract of radix scutellaria in preparation of drug against novel influenza A (H1N1), influenza A (H1N1) and H3N2 sub-type of influenza virus and hygienic products. The active substances in the scutellarein, baicalin and total flavonoid extract of radix scutellaria are mixed with an excipient acceptable on pharmaceutics to prepare the preparation and the hygienic products acceptable to patients. The invention is applied to the treatment and the prevention of the novel influenza A (H1N1), influenza A (H1N1) and H3N2 sub-type influenza and has remarkable curative effect and good safety.

The invention discloses a gene related to flavone composite in radix scutellariae. The gene includes one or several in flavone synthetase gene with a sequence shown in SEQ ID No.1, flavone 6-site hydroxylase gene with a sequence shown in SEQ ID No.3 and flavone 8-site hydroxylase gene with a sequence shown in SEQ ID No.5. The invention further provides primer composite for amplifying the gene, protein encoded by the gene, a recombinant vector, host cell or transgenic cell line containing the gene and application thereof. The protein encoded by the gene disclosed by the invention can participate in synthesizing baicalein and wogonin and catalyzing synthesis and hydroxylation reaction of flavone matters of the similar structures, can provide very good basis for producing effective active matters, provides theoretical basis for producing baicalein, wogonin and aglycone of the baicalein and the wogonin in a large scale and establishes solid basis for industrially producing other related flavonoid compound.

The invention relates to application of a compound with a flavone skeleton structure as a Parkinsonism treating medicine. The compound with a flavone skeleton structure is an inhibitor for the catechol methylation transferase; and the compound specifically comprises radix scutellariae, scutellarein and structure derivatives of radix scutellariae and scutellarein, and can be used as a synergist of the Parkinsonism treating medicine levodopa. In-vitro activity test indicates that IC50 of the compound in inhibiting catechol methylation transferase can reach nanomole level, wherein the COMT(Catechol O Methyl Transferase) inhibition activity of scutellarein and the derivatives of scutellarein is superior to that of medicine tolcapone on the market. The rat overall pharmacokinetic study shows that by the joint application of scutellarein and levodopa, the blood concentration of levodopa can be obviously increased. Moreover, the compound does not generate active intermediate through metabolism activation or form toxic adduct together with biological macromolecules, thus the hepatotoxicity and nephrotoxicity caused by metabolism activation are avoided, and the compound has good prospect of patent medicine.

The invention discloses a baicalein derivative drug which can be used for the prevention and treatment of metabolic syndrome, obesity, type 2 diabetes and atherosclerotic cardiovascular disease. The baicalein derivative can increase the metabolic activity for the prevention and treatment of metabolic syndrome, obesity, type 2 diabetes and atherosclerotic cardiovascular disease by controlling and activating the activity of single adenylate activated protein kinase.

The invention discloses a method for preparing scutellarin by using Aspergillus niger AS 3.795 for hydrolyzing scutellarin-7-O-glucuronide. Aspergillus niger AS 3.795 is used for hydrolyzing scutellarin-7-O-glucuronide glucuronyl to prepare the scutellarin. The method comprises the following steps of: using Aspergillus niger AS 3.795 to biologically transform a substrate scutellarin-7-O-glucuronide, using ethyl acetate to extract transformation products from fermentation liquor and using D101 macroporous adsorption resin column chromatography and recrystallization to purify the transformation products. The purity of the prepared transformation products can reach more than 99 percent according to high performance liquid chromatography. The method has the advantages that the defect that glucuronide is difficult to hydrolyze is overcome, the scutellarin can be prepared in a large scale under moderate conditions such as normal temperature and normal pressure, the environmental protection is facilitated, the production cost is reduced and the method is suitable for industrialized production.

The invention discloses a genetically engineered bacterium for catalyzing glucose glycosylation of a flavonoids compound and an application thereof. Specifically, a Beta-glycoside hydrolases gene of a chassis biological cell is removed according to the genetically engineered bacterium, and endogenous degradation of a glycosylation product is reduced; the high-expression regulation is performed to two key enzymes of glucophosphomutase (PGM) and uridine diphosphate glucose pyrophosphorylase (UGP1) of the chassis biological cell for participating in the synthesis of glycosylated-donor uridine diphosphate glucose (UDP-Glu), and a UDP-glucuronosyltransferase gene for catalyzing the flavonoid aglycones glucose glycosylation is combined so as to obtain a genetically engineered strain for effectively catalyzing the glucose glycosylation of the flavonoids compound, and finally scutellarein is used as a catalytic substrate for fermenting for 54 h in 10 L of a fermentation tank, wherein the yield of scutellarein-7-O-glucose of the glycosylation product is up to 1200 mg / L. The used strategy provides a technology reference for biologically-catalyzing chemical micromolecular glycosylation by using a microbiological method.

The invention discloses a method for preparing scutellarein. The method comprises the following steps: taking phenol as a starting material, preparing a chalcone intermediate through bromination, methoxy substitution, friedel-crafts acylation and the like, performing oxidative cyclisation on the chalcone intermediate to obtain a key flavone intermediate 4',6-dihydroxy-5,7-dimethoxy flavone, and preparing high-purity scutellarein through demethylation of the key intermediate. According to the method, the adopted raw materials are all low in price and easy to obtain, the synthesis steps are less, the operation is simple and convenient, the production control is easy, the product yield and purity are high, and the method is suitable for scutellarin and scutellarein production.

The invention discloses a medicine composition containing inorganic arsenic compounds and application thereof. The medicine composition comprises inorganic arsenic compounds, scutellarin or scutellarein, is used for preparing medicines for treating cancers, and has a better effect on cancer cell inhibition than that by singly using inorganic arsenic compounds and that by singly using scutellarin or scutellarein. According to the medicine composition, the treatment dosage of inorganic arsenic compounds can be reduced, the cancer inhibition effect can be enhanced, and the systematic toxin of inorganic arsenic compounds can be effectively reduced.

The invention relates to a content determination method for scutellarin and scutellarein in sculellaria barbata medicinal material and formula granule of sculellaria barbata medicinal material. The content determination method is characterized in that common isocratic elution is adopted, acetonitrile-methyl alcohol-0.1 percent phosphoric acid of which the volume ratio is 12.5:(15 to 16.2):(71.3 to 72.5) is taken as a mobile phase, and the contents of the scutellarin and the scutellarein in the sculellaria barbata medicinal material and the formula granule of the sculellaria barbata medicinal material are simultaneously determined at a wavelength of 340+ / -2nm. The method is simple, convenient, fast, and easy to popularize and master; the separations of wave crests on three different chromatographic columns are good. Compared with a method of recording under a sculellaria barbata medicinal material item of the first part of the pharmacopeia, the prominent improvement is that a sample treatment process is simplified, the time and cost are saved, the determination is advanced from single component determination of the scutellarin to the simultaneous determination of the two components, the quality controllability is improved, and the defects that impurity peaks exist and the content results are inaccurate are overcome.

The invention relates to a thymus plant extract or composition and application thereof. The preparation method comprises the following steps: firstly quenching active pharmaceutical ingredients with acetone; performing acidification by use of H2SO4 with certain concentration; extracting the extracting solution with ethyl acetate for 2-3 times, thereby obtaining a thymus plant extract containing carvacrol, tanshinol, scutellarein, scutellarin, 5,4'-dyhydroxyl-6,7,8-trimethoxy flavone, oleanolic acid and rosmarinic acid. The thymus plant also provides a traditional Chinese medicine composition for treating cardiovascular and cerebrovascular disease. The traditional Chinese medicine composition is prepared from the following active pharmaceutical ingredients in parts by weight: 200-500 parts of thymus plant, 100-300 parts of curcuma roots, 100-300 parts of rhizoma sparganii, 200-400 parts of radix angelica sinensis, 100-200 parts of ginkgo leaves, 100-200 parts of licorice root, 200-400 parts of radix codonopsis pilosulae and 200-500 parts of rhizoma ligustici wallichii. The traditional Chinese medicine composition is rapid in medical effect taking and less in toxic and side effects, thereby being a favorable medicament for treating cardiovascular and cerebrovascular diseases.

The invention belongs to the technical field of nano-drug delivery, and particularly relates to a lipidosome containing an insoluble Chinese herb effective ingredient scutellarein and a preparing method thereof. By utilizing the good lipotropy (logD is 2.54 (chemspider)) of scutellarein, scutellarein can pass through a lipid bilayer and enter the inner water phase in the form of molecules, and scutellarein can be ionized into scutellarein ions under the high pH condition of the inner water phase. As a phospholipid membrane almost has no permeability for ions, the pH gradient of the inner water phase and the outer water phase of the lipidosome can be utilized to achieve the purpose of stably encapsulating scutellarein. Meanwhile, by wrapping scutellarein in the inner water phase of the lipidosome, the chemical stability of scutellarein in the storage process can be easily improved.

The invention relates to an application of scutellarein to preparing a medicine for preventing and / or treating thrombotic diseases. The invention further provides a kit containing scutellarein.

The invention provides flavones-6-hydroxylase and application thereof to scutellarin synthesis and particularly provides flavones-6-hydroxylase which is capable of catalyzing apigenin 6-coordinate hydroxylation reaction to obtain scutellarein. In addition, the invention provides a method for preparing the scutellarein into scutellarin by adoption of glycosylated transferases and glycosyl donors.

The invention provides two flavonoid compounds, namely baicalein and scutellarein, of promoting a asymmetric cell division (ACD) regulation pathway of a root tip stem cell of a plant. The two compounds have effects of promoting SCR-SHR (scarecrow-short root) combination of an ACD active regulation complex of a root tip stem cell, does not influence RBR-SHR (retinoblastoma-related-short root) combination of a non-active complex and can activate NUC (nutcraker) expression of an ACD downstream key gene. At the same time, the invention provides an application of baicalein and scutellarein in preparing an SHR-SCR protein binding promoter and an NUC gene expression promoter. A secondary metabolism product of promoting ACD regulation of the root tip stem cell of the plant is found for the first time; a new biological effect of baicalein and scutellarein is found; an important tool is provided for an in-depth study of the stem cell regulation of the plant; and a new clue is provided for the development and application of a plant stem cell technology in industries of modern agriculture, biological medicine, hairdressing, health and the like.

The invention belongs to the field of fertilizers for crops and more particularly relates to a special ecological fertilizer for improving the content of scutellarein glucoside of codonopsis pilosula. The special fertilizer is prepared from sugar beet pulp, astragalus smicus, bean dregs, potassium hydroxide, composted sheep excrement, composted chicken excrement, peat moss, urea, ammonium polyphosphate, monopotassium phosphate, ammonium molybdate, copper sulfate, zinc sulfate, rare earth elements and an active inducer. According to the special ecological fertilizer, charcoal formed by carbonization of forestry and agricultural residues is sufficiently mixed with the composted farmyard manure and chemical fertilizers to form a mixed fertilizer with the charcoal as a matrix, and therefore the utilization rate of the fertilizer is increased; meanwhile, the active inducer capable of increasing secondary metabolite of the codonopsis pilosula is added to the mixed fertilizer to increase active substances of the codonopsis pilosula and improve the quality of the codonopsis pilosula. The special ecological fertilizer is reasonable in formula and completely balanced in nutrition, and has a relatively high market value, and the yield and the quality of the codonopsis pilosula are greatly improved.

The invention discloses a scutellarin, characterized in that the scutellarin is prepared by the following steps: dissolving breviscapine in water completely, heating to 35 to 45 DEG C, keeping at the constant temperature between 35 DEG C and 45DEG C, adjusting the pH value to 2 to 6, adding digestive enzyme, keeping at the constant temperature between 35 DEG C and 45DEG C for 2 to 12 hours, concentrating, adding the concentrated solution into a polyamide column, eluting with water, eluting with 20 % to 90% ethanol, concentrating the ethanol eluent, drying. The process of the invention has high extraction yield, the scutellarin purity is high as the active ingredient of the medicinal preparation.

The invention relates to a baikal skullcap root extractive freeze dried, which uses Baikal skullcap root extractive as material, assisted with alkali assisting solvent, acidamide assisting solvent, and anti-oxidant, to make the scutellarein stable in alkali solution. The invention is simple.

The invention provides a synthetic method for scutellarein. The synthetic method comprises the following steps: subjecting a compound with a structure as shown in a formula (I) which is described in the specification to oxidative ring-closure to produce a compound with a structure as shown in a formula (2-8) which is described in the specification; and subjecting the compound with a structure as shown in the formula (2-8) to demethylation so as to produce a target compound as shown in a formula (1-2) which is described in the specification, wherein R in the formula is selected from a group consisting of C2-C5 alkylacyl groups which are unsubstituted or substituted by any one phenyl group, and benzoyl groups which are unsubstituted or arbitrarily substituted by C1-C5 alkyl groups. The synthetic method is simple in process, mild in conditions, and high yield, wherein the overall yield of the method is as high as 80.4%; and the synthetic method has good industrial application prospects.

The invention relates to the field of drug synthesis, and discloses a scutellarein aglycone prodrug and a preparation method thereof. The scutellarein aglycone prodrug takes cyclodextrin as a carrier, and a scutellarein aglycone molecule, a modified amino of an arbitrary hydroxyl of the cyclodextrin and a formaldehyde reagent commonly generate trimolecular reaction (Manich reaction) through an activated hydrogen on a C8 location of the scutellarein aglycone molecule so as to prepare the scutellarein aglycone prodrug. Compared with scutellarein aglycone, the scutellarein aglycone prodrug has more hydrophilic active groups, good biocompatibility, better water solubility and high bioavailability; and on the other hand, the preparation method of the scutellarein aglycone prodrug has the advantages of simplicity in operation, easily-obtained raw materials and moderate reaction conditions, and can be used for preparing the scutellarein aglycone prodrug in a large scale.

Provided is a method of treating SARS in mammals. The method includes administering a therapeutically effective amount of at least one composition selected from the group consisting of myricetin, scutellarein and a pharmaceutically acceptable salt thereof to a mammal in need of treatment of SARS diseases to suppress the activities of SARS coronavirus helicase.

The invention discloses a scutellarein derivative shown in a formula I, a preparation method of the scutellarein derivative, and application of the scutellarein derivative in preparing anti-tumor drugs. The preparation method comprises the following steps of using scutellarein as an initiating raw material, and synthesizing a series of scutellarein derivatives with an A ring benzodioxane structure, a B ring 4apostrophe-position connected lipid-soluble group and a water-soluble group. The preparation method has the advantages that the synthesizing method is simple, and the operability and reaction yield rate are better. The scutellarein derivative has the advantages that the activity for inhibiting proliferation of multiple tumor cells is realized, and the activity of the scutellarein derivative is better than or equivalent to the activity of scutellarein; the scutellarein derivative is expected to develop into the anti-tumor drugs. (The formula I is shown in the description).

The invention provides a compound as shown in a formula (I) which is described in the specification and a preparation method thereof, and application of the compound as shown in the formula (I) to preparation of scutellarein or scutellarin. R in the formula is selected from a group consisting of C2-C5 alkylacyl groups which are unsubstituted or substituted by any one phenyl group, and benzoyl groups which are unsubstituted or arbitrarily substituted by C1-C5 alkyl groups.

The invention discloses a polar auxin transport accelerant which comprises scutellarin or scutellarein which have functions of accelerating polar auxin transport (PAT) and resisting the inhibition function of a PAT inhibitor TIBA to root elongation, and discloses application of scutellarin and scutellarein in preparing the PAT inhibitor, and scutellarein in preparing a root elongation accelerant. The phenomenon that scutellarin and scutellarein are secondary metabolites with an acceleration function on PAT and are plant sourced PAT accelerants are discovered for the first time, scutellarin and scutellarein are used in the field of plants for the first time, a new prospect that effects of secondary metabolites are brought into play in plant physiology is widened, and relatively greatervalues of scutellarin and scutellarein can be made.

The invention discloses a method for simultaneously measuring contents of four active ingredients in fleabane flowers. The Four active ingredients include scutellarin, apigenin-7-o-glucronide, scutellarein and apigenin. According to the method, the chromatographic column employs a C18 liquid chromatographic column; the flow rate is 0.8 to 1.2ml / min; the column temperate is 25 DEG C to 35 DEG C; the detection wavelength is 335nm; the sample injection amount is 2 microliters; the mobile phase A is water; the mobile phase B is acetonitrile; the mobile phase C is 0.3% of phosphoric acid aqueous solution; and a gradient elution mode is employed. The method has advantages of high accuracy and reliability and the good scientific and reasonable effect.

The invention discloses scutellarein, which is characterized in that the scutellarein is prepared by the following steps: adding water into breviscapinun and fully dissolving the breviscapinun, heating the water solution to between 35 and 45 DEG C, keeping the water solution at the constant temperature of between 35 and 45 DEG C, adjusting the pH value to between 8.0 and 12.0, adding digestive enzyme into the water solution, keeping the water solution at the constant temperature of between 35 and 45 DEG C, placing the water solution for 2 to 12 hours, adjusting the pH value to between 2.0 and 6.5, concentrating the water solution, loading concentrate on a polyamide column, washing the polyamide column by water, then washing the polyamide column by 20 to 90 percent ethanol, keeping ethanol eluent, concentrating the eluent, and drying the concentrate to obtain the scutellarein. The extraction rate of the process method is high, the purity of the scutellarein is high, and the scutellarein can be used as an active component of a medicinal preparation.