335 results about "Scutellarin" patented technology

The present invention discloses a slow-released medicine preparation with the function of promoting blood circulation, removing staiss, removing obstruction in the channels to relieve pain. In particular it is a slow-released medicine preparation containing breviscapine. The described breviscapine is scutellarin or 4-hydroxy ba icalein-7-O-beta-D-pyrangluconate methyl ester.

The invention discloses a 4'-carbamate derivative of scutellarin shown in formula (I), a preparation method of the compound and application of the compound in preparing medicines for preventing and / or treating various symptoms and diseases caused by acetyl cholinesterase and / or mediated by free radicals, such as vascular dementia and Alzheimer's disease. In the formula, each of R1, R2 and R3 independently represents H, C1-C12 alkyl or R6CO, wherein R6 represents C1-C12 alkyl, but R1, R2 and R3 are not H at the same time; each of R4 and R5 independently represents H, C1-C12 alkyl, C1-C6 fatty alcohol, or an ester formed by the C1-C6 fatty alcohol and C1-C6 carboxylic acid, the C1-C6 carboxylic acid, or an ester formed by the C1-C6 carboxylic acid and the C1-C6 fatty alcohol; or R4NR5 represents a morpholine ring, a piperidine ring, a 4-benzyl piperidine ring, a piperazine ring, the piperazine ring with the 4-position substituted by C1-C12 alkyl, or a tetrahydropyrrole ring.

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.

Belonging to the field of pharmaceutical chemical engineering, the invention in particular relates to a variety of scutellarin aglycone crystal forms and a preparation method thereof. The invention also relates to application of the scutellarin aglycone crystal forms in preparation of drugs preventing and / or treating cardiovascular and cerebrovascular diseases, rheumatism arthritis, stroke sequelae and the like. The scutellarin aglycone crystal forms provided by the invention have good stability, and can overcome the poor oral absorption and low bioavailability problems of scutellarin.

The invention discloses an adsorption resin method separation technology of scutellarin in a fleabane flower extract. Based on scutellarin and fleabane flower essence A which have very similar structures, the difference of intermolecular hydrogen bonding capacities is formed, an amide functional group capable of forming hydrogen bonds is introduced on a macroporous adsorption resin skeleton, highly selective adsorption is carried out on the scutellarin by the synergic action of dewatering and the hydrogen bonds, a commercially available extract is used as a raw material, and a specimen with the content of the scutellarin more than 98% and the content of the fleabane flower essence A less than 0.5% is prepared by a one-step continuous technology of adsorption and desorption. The invention avoids using a poisonous organic solvent with low boiling point and does not need the assistance of other purification methods, so that the invention has simple operation and is environment-friendly, resin can be recycled simultaneously, the production cost is greatly reduced, and the invention is suitable for large-scale industrial production. The obtained specimen can meet the requirements for further enhancing the quality standard of a breviscapine preparation, reducing clinical side reactions and the like, and the invention has favorable application prospect.

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 method for preparing scutellarin aglycone. In the method, 95 percent ethanol is used as reaction solution; and scutellarin undergoes hydrolysis reaction in 3 to 8 mol / L organic acid alcohol solution under the protection of an inert gas to prepare high-purity scutellarin aglycone. Due to the adoption of the method for preparing the scutellarin aglycone provided by the invention, an optimal preparation process for the scutellarin aglycone is determined; the overall preparation method has the characteristics of fast reaction speed and high efficiency; the obtained scutellarin aglycone has the characteristics of high yield and high purity; and the method for preparing the scutellarin aglycone provided by the invention has high operability and can realize industrialized mass production.

The invention provides a medicinal composition containing caffeic acid ester and scutellarin. The composition is a composition for injection, and comprises, by weight, 45-95% of caffeic acid ester and 5-25% of scutellarin. The invention also provides application of the composition in preparation of drugs for treating cardiovascular and cerebrovascular diseases.

The invention relates to the field of the quality control on traditional Chinese medicine, specifically to a quality control method for erigeron breviscapus(Vant.) hand-mazz. The method comprises a fingerprint detection method and a multiple-indicative content detection method for erigeron breviscapus (Vant.) hand-mazz, wherein the fingerprint detection method employs UPLC detection method, through which 24 characteristic peaks are found and 8 characteristic peaks are ascribed. By using content detection method for erigeron breviscapus(Vant.) hand-mazz., the UPLC-PDA method, contents of following constituents are determined: erigeroside, chlorogenic acid, breviscpini glycoside, Scutellarin, 3,4-0-dicaffeoylquinic acid, 3,5-0-dicaffeoylquinic acid and 4,5-0-dicaffeoylquinic acid. Compared with the prior art, the fingerprint detection method and the multiple-indicative content detection method for erigeron breviscapus (Vant.) hand-mazz are improved in the invention, so that the quality of erigeron breviscapus (Vant.) hand-mazz. can be controlled in a convenient, rapid and accurate manner, thereby ensuring the quality of erigeron breviscapus (Vant.) hand-mazz. stable, uniform and controllable.

The related preparation method for high-pure scutellarin drug comprises: 1. adding 200wt% water into container with material and alkaline solution (pH > 9) to adjust liquid to pH value as 4-8 for complete dissolution; 2. adding solvent with weight more than 3 times at 18-35Deg, depositing, keeping static, filtering, and cleaning precipitum with solvent; 3. transferring precipitum into solvent with 10-60wt% solvent, adjusting pH to 1-2 with acid, depositing, filtering, cleaning with water to neutrality, and drying to obtain the final product.

The invention relates to a method for content determination of multiple components in traditional Chinese medicinal preparation Shuanghuanglian for injection, aiming at solving the problems of an existing method for content determination of Shuanghuanglian for injection which is complex in sample processing, time, labor and detection equipment-consuming to detect Shuanghuanglian, and long in detection period. The detection method provided by the invention can be used for synchronously determining the contents of more than 10 components such as forsythin, forsythiaside A, caffeic acid, neochlorogenic acid, chlorogenic acid, cryptochlorogenin acid, isochlorogenic acid A, isochlorogenic acid C, baicalin, scutellarin and oroxylin-7-O-glucuronic acid in the Shuanghuanglian for injection, and meanwhile monitoring a fingerprint spectrum. The method can be used for completing previous detection in one time just by one detection system, and is more accurate, stable, comprehensive and rapid in control over the quality of the Shuanghuanglian for injection.

The invention relates to plastic-tunnel erigeron breviscapus (vant.) low-tunnel direct seeding planting technology. The technology is characterized by changing transplanting to direct seeding and adopting such technical measures as arching, film mulching and the like. The technology has the following advantages: the moisture is controlled in rainy seasons and the temperature is raised in winter, thus providing better growth environment for erigeron breviscapus (vant.) low-tunnel; the yield and quality are improved; more than 340-360kg of dry products of erigeron breviscapus (vant.) low-tunnelcrude drugs are obtained per mu; the average scutellarin is 2.8%; the content of the impurities is below 2%; the pesticide residual quantity is low; various diseases caused by pathogen infection of roots are effectively controlled; and meanwhile, the cost input in the transplanting process can be saved by direct seeding, thus lowering the planting cost.

An application of the scutellaria extract in preparing the medicine for esophagus cancer is disclosed, and it features that scutellarin, scutellaroside, or their mixture can be used to prepare the pharmacologically receptable sale for suppressing the splitting of cancer cell, inducing the withering of cancer cell and inhibiting the generation of the blood vessel inside esophagus cancer.

The invention discloses a method for extracting scutelloside and scutellarin from baikal skullcap root. The method comprises the following steps of: (1) performing ultrasonic extraction on a solvent; (2) adsorbing Fe3O4 magnetic nanoparticles; and (3) performing desorption. The method is simple and rapid; separation of an absorption carrier and a feed liquid can be realized by additionally applying a magnetic field; scutelloside and scutellarin can be eluted selectively through different eluents, so that loss of raw materials and energy consumption is avoided, and cost is reduced effectively; and Fe3O4 magnetic nanoparticles can be used circularly, so that cost can be saved effectively.

The invention discloses a novel scutellarin derivative as well as a preparation method and a pharmaceutical composition thereof. The compound is prepared by the two-step reaction of methyl etherification and acetylation of the scutellarin functioning as an initial raw material and the separation and has the chemical name of 4',5,6-trimethoxy-8-(3,4,5-triacetyl-glucuronic acid)-scutellarin. The compound and the pharmaceutical composition thereof can be used for treating cardiovascular and cerebrovascular disease, phlegmasia and tumor and has the advantages of good dissolvability, high bioavailability and remarkable curative effect.

The invention provides related substances in a vegetable drug extract-scutellarin and a detection method of the related substances. According to the method, an accurate detection result can be obtained, the interference caused by other substances is avoided, a double effect is achieved, an identification result is relatively objective, accurate, precise and stable.

The invention discloses a method for preparing scutellarin and analogues thereof. The method comprises the following steps of: preparing a 7-OH receptor compound from naringenin; preparing a uronic acid donor compound from glucuronic acid 3,6 lactone; and reacting the 7-OH receptor compound with the uronic acid donor compound to obtain scutellarin or analogues thereof finally. In the method, naringenin is taken as a raw material, and is cheap and readily available; a reaction route is flexible, and a series of analogues of scutellarin are convenient to obtain; and the obtained analogues of scutellarin have higher bioavailability.

The invention belongs to a medicine technology field, relates to a new scutellarin compound and the application of the new scutellarin. The invention precisely relates to the new scutellarin compound for treating cardiocerebral vascular diseases. The general formula of the hydroxyethyl (hydroxypropyl or hydroxybutyl) scutellarin compound in the invention is (I), in which R4 is H or Alkyl; R1, R2 and R3 are hydroxyethyl (hydroxypropyl or hydroxybutyl) or H, among which at least one of R1, R2 and R3 is the hydroxyethyl (hydroxypropyl or hydroxybutyl). The new scutellarin compound is substantially used in the prevention and treatment of cardiocerebral vascular diseases, Alzheimer diseases, cerebral infarction, cerebral ischemia and other varied diseases caused by the cerebral ischemi, etc.

A freeze-dried powder injection of the mixture of scutellarin and scutelloside extracted from scutellaria root features high stability. Its preparing process is also disclosed.

The invention relates to a method for extracting high-purity scutellarin from breviscapin. The method comprises the following steps: the breviscapin raw material is extracted by using organic solvent, the filtrate is added with clarifying agent for coagulation and clarifying, the coagulated and clarified filtrate is absorbed by macroporous absorbent resin and is eluted with water, the water eluent is concentrated through a reverse osmosis membrane or nanofiltration membrane, the concentrated solution is added with the organic solvent for standing and precipitation, the sediment is filtered and collected, the aqueous solution of the organic solvent is added and stirred to be suspendible, and after standing a night, the sediment is filtered, collected and washed to be near-neutral with water to obtain the high-purity scutellarin after drying. The alkali is not used in the entire process, the clarifier is used for removing the water insoluble matter, the impurity removal is carried out by using the macroporous absorbent resin, the concentration is carried out by using the reverse osmosis membrane or the nanofiltration membrane, the scutellarin plant salt is prevented from being heated and degraded in water, the content of the prepared scutellarin can reach above 97 percent, the quality is stable, the process is simple and the pollution is little.

The invention belongs to the field of natural medicine and medicinal chemistry and relates to a scutellarin aglycone nitrogen mustard derivative and a preparation method and application thereof, in particular to a scutellarin aglycone nitrogen mustard derivative of which 4'-OH is combined with benzoic acid nitrogen mustard and a preparation method and antitumor activity thereof. The structure of the scutellarin aglycone nitrogen mustard derivative and pharmaceutically acceptable salt thereof is as shown in the general formula I, wherein R and n are as described in claims and the specification.The formula I is shown in the description.

The invention relates to a method for preparing scutellarin bulk drug with a purity above 99%. The method comprises the following steps: (1) adopting macroporous resin with a type of D101 or AB-8 macroporous resin, and water as a solvent, and filling a column; (2) preparing a breviscarpin on-column solution; (3) feeding the on-column solution in the step (2) into the macroporous resin column in the step (1), eluting with water as an eluent until the eluate substantially becomes colorless, and collecting the eluate; (4) concentrating the eluate under the reduced pressure at 60 to 70 DEG C into 1 / 10 to 1 / 20 of the original volume; (5) adding acetone or ethanol with the amount 10-15 times of the concentrate, stirring, standing, precipitating, filtering, and washing out the mother liquid in the precipitate with acetone to obtain a breviscarpin salt; and (6) adding 30% to 50% acetone aqueous solution with the amount 5-10 times of the volume of the breviscarpin salt, stirring, regulating the pH to 1-2 with organic acid, standing, filtering to obtain precipitate, and washing with water to neutrality to obtained the scutellarin bulk drug with high purity.

The invention relates to a process for preparing a high-purity bulk drug in pharmaceutics. The process comprises the following steps: (1) adding water with the weight 2-15 times of the weight of a crude product into the breviscapine crude product, stirring, then adding arginine, lysine or hydroxylysine with the weight 35-55% of the weight of the crude product, heating at the temperature of 45 DEG C until boiling off to prepare a stable water solution, filtering and removing the discarded filter residue; (2) adding acid phosphate with the weight 0.1-2.0 times of the weight of the breviscapine crude product into the hot filtrate and preparing the acid phosphate into a water solution with the weight percent of 10-30%; then adding an organic solvent with the volume 2-3 times of the volume of merging liquid and crystallizing scutellarin; and (3) adding the water with the weight more than 10 times of the weight of the breviscapine crude product into the crystal, boiling off, then adding a transforming agent of organic acid with the weight 0.2-1.0 time of the weight of the breviscapine crude product after cooling the solution to the temperature below 60 DEG C and reducing scutellarin salt into the scutellarin so as to obtain the high-purity scutellarin raw material after filtering a precipitate and drying.

The invention provides a kind of scutellarin pro-drug taking carboxymethyl chitose as vector, and the preparation method, which takes carboxymethyl chitose as vector, takes dicyclo hexylcar bodiimide (DCC)as condensing agent, and produces new-type scutellarin pro-drug through reaction between carboxy group of scutellarin and amino of chitose. There are more active carboxy groups on main chain of scutellarin pro-drug, which is favorable for increasing pro-drug water solubility and biological utilization rate of scutellarin. The preparation method is simple and is easy to carry out.

The present invention relates to breviscpini health care wine and a method for manufacturing the same, belonging to the health care beverage field. The breviscpini which is collected in the present year is adopted as raw material, which is soaked in liquor after pretreatment and drying. The breviscpini dry material and the liquor are mixed according to a weight ratio of 1 to 10-75, and are concocted to produce filter residue and filtrate. The filtrate is blended for producing the health care wine, the filter residue is soaked in the liquor which is 5 to 15 times more than the filter residue by weight for 10 to 30 days to produce secondary filtrate. The secondary filtrate is blended for producing the health care wine. The wine has the efficacy of the folk common soaked wine; meanwhile, the wine has the functions of improving sleep, promoting blood circulation, relieving fatigue and reducing blood pressure and blood fat, etc.

The invention relates to the field of pharmaceutical chemistry study, in particular to a novel scutellarin aglycone methylate product based on in-vivo metabolic mechanism as well as a preparation method of the novel scutellarin aglycone methylate product and an application of the novel scutellarin aglycone methylate product to thrombus prevention and treatment medicine. Pharmacological experiment results show that the scutellarin aglycone methylate product provided by the invention has pharmacological effects of better solubility, antioxidation, cell damage inhabitation and the like, and can be developed into novel medicine for preventing and treating thrombotic diseases.

The invention discloses a preparation method of scutellarin, comprising the following steps of: (1) refluxing and extracting a medicinal material of erigeron breviscapus with ethanol; (2) filtering a leaching solution in the last step and carrying out pressure reduction to recover ethanol to obtain extract for later use; (3) respectively extracting with petroleum ether, ethyl acetate and normal butanol to obtain a petroleum ether extraction part, an ethyl acetate extraction part and a normal butanol extraction part; (4) dissolving the ethyl acetate part with ethanol; (5) adding silica gel and stirring, naturally drying, porphyrizing and sieving to obtain fine powder; (6) through gel column chromatography, carrying out gradient elution on the petroleum ether and the ethyl acetate and collecting by section; and (7) carrying out gel column chromatography on the ethyl acetate extraction part and elution by the petroleum ether and isopropanol and checking and combining same speckle parts according to a thin layer to obtain a compound of scutellarin. The scutellarin extract is used as an active component and is used for preparing a medicine for preventing and treating neurodegenerative diseases. The method can be used for preparing the scutellarin the purity of which is as high as 95 percent; and the raw material can be used for preparing a medicine for treating senile dementia and serves the human health.

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 relates to a manufacture method for high purity scutellarin bulk drug. It includes the following steps: adding scutellarin raw extractive into the container, adding water and adjusting the pH value to target value, whisking to fully dissolve; adding deposition solvent into the liquid, depositing, standing, filtering and washing by deposition solvent; transferring the deposition to suitable container, adding water for dissolving, adding solvent to make the liquid has a certain range of solvent ratio, whisking, filtering, adding acid to adjust the pH value to target value, depositing, washing to neutral, drying; repeating the previous steps for several times, the scutellarin with the content over 98% could be gained.