44 results about "Oroxylin A" patented technology

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 provides O-methyltransferase participating in citrus peel flavone synthesis and a coding gene and application thereof. The expression level of CitOMT1 is positively correlated with the accumulation of polymethoxylated flavones in a fruit development process of Citrus reticulata cv. Suavissima; in vitro enzyme activity assays indicate that the O-methyltransferase can be applied to catalyze specific site methylation of flavones, in particular to catalyze quercetin to produce quercetin 3',4' dimethyl ester, catalyze luteolin to produce chrysoeriol, catalyze eriodictyol to produce hesperidin and homoeriodictyol, catalyze baicalein to produce oroxylin A, and catalyze 7,8-dihydroxyflavone to produce 7-hydroxy-8-methoxy flavone. The enzyme activity assays have simple reaction conditions, do not require additional metal ions, and have high application value and research prospects.

The invention relates to the application of biological pesticide using Oroxylin A as the active ingredient in crop disease control; the Oroxylin A is 5, 7-dihydroxy-6-methoxyflavone, which is a yellow needle like crystal with the melting point ranging from 231 DEG C to 232 DEG C used for the control of crop diseases caused by fungi. The Oroxylin A is the secondary metabolite of plants widely existing in the oroxylum indicum of bignoniaceae, the scutellaria of labiatae and other species. The application of biological pesticide using Oroxylin A as the active ingredient in crop disease control has the advantages that, 1 the reagent using Oroxylin A as the active ingredient is an anti fungal infection reagent characterized in low toxicity, low residue, compatibility with environment and other characteristics, belonging to new biological pesticide and having obvious control effect to rice blast and vegetable and fruit gray mold; 2 the reagent has no or low direct bactericidal effect or bacteriostatic action, but the objective of disease control can be achieved by inducing the disease resistance responses of plants; 3 raw material source is relatively wide, and the promotion and the application of the invention are facilitated.

This invention provides a-glucosidase inhibitors isolated from Oroxylum indicum an Indian medicinal plant. Particularly, this invention provides hexane and acetone fraction of Oroxylum indicum wherein the hexane fraction comprises a-glucosidase active compounds of oroxylin A, chrysin and baicalain and acetone fraction comprises the compounds of oroxylin A, chrysin, baicalain, methoxy chrysin and oroxyloside methyl ester. This invention also relates to a process for the isolation of a-glucosidase inhibitory active compounds from the above said hexane and acetone fraction of Oroxylum indicum. This invention also provides the use of potent intestinal a-glucosidase inhibitors as active ingredients that can be used in pharmaceuticals, food products, health foods and specialized health care foods as anti hyperglycemic agent for prevention and treatment of post prandial hyperglycemia, hyperglycemia and related conditions in diabetes mellitus, obesity and disease conditions requiring hyperglycemic control as well as inhibition of a-glucosidase activity.

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 relates to an oroxylin A solid preparation and a preparing method thereof, and belongs to the field of pharmaceutical preparations. The oroxylin A solid preparation is composed of the following components by the mass percentage: 10-60% of oroxylin A, 0.5-18% of L-arginine, 20-80% of a filling agent, 1-10% of a disintegrating agent, and 0-2% of a lubricant. L-arginine can greatly improve the solubility of oroxylin A; compared with other solubilizers, L-arginine has good compatibility with oroxylin A, and can ensure that the prepared solid preparation has good stability. The solidpreparation prepared by the preparation method has the advantages of good fluidity, good compressibility, good dissolution property, good drug stability, low processing cost and the like.

An application of oroxylin A and a pro-drug thereof as a catechol-type medicine synergist belongs to the technical field of medicines. The compound is used as the catechol-type medicine synergist and has the following structure general formula (I), wherein R is hydrogen, carboxylic ester, glucuronic acid and the like substitutive groups. One or more compounds of the oroxylin A and the pro-drug thereof can be mixed with levodopa according to a certain ratio to prepare a drug composition for treatment of Parkinson's disease. The oroxylin A and the pro-drug prepared through modification thereof are improved in both solubility and transmembrane capability and are significantly prolonged in in-vivo metabolic half life period, which is longer than the in-vivo metabolic half life periods of majority of catechol-type medicines, so that the compounds have excellent medicine preparation prospect. In addition, the compounds also can be combined with a catechol-type medicine to form a compound medicine. The compound medicine can be prepared into an oral-taking slow-release preparation to further improve oral-taking bioavailability and treatment effects of the catechol-type medicines.

The invention discloses an analysis method for detecting wogonin, chrysin, oroxylin A, naringenin, hesperetin, berberine, coptisine, jatrorrhizine and palmatine in blood plasma, and applications of the method in pharmacokinetics. The analysis method has good specificity, high precision and accuracy, and wide linear range, and can be used for pharmacokinetic detection in vivo of traditional Chinese medicine compositions.

The invention discloses an oroxylin A pharmaceutical composition and application thereof in preparation of liver cancer drugs, and belongs to the technical field of medicines. The particle size of oroxylin A in the pharmaceutical composition is 1-10 microns, and oroxylin A can be prepared into granules, tablets, capsules, pills, oral solutions, oral suspensions or oral emulsions and used for preparing liver cancer treatment drugs. According to the composition, the oroxylin A is micronized by utilizing airflow crushing, so that the bioavailability of the oroxylin A can be remarkably improved.

The invention provides a synthetic method for oroxylin A. According to the invention, baicalin is used as a starting material, and oroxylin A can be synthesized by using a simple and effective chemical synthesis method.

The invention belongs to the field of tumor drugs and discloses an application of oroxylin A in preparation of an inhibitor with a targeting effect on AFP (alpha fetoprotein) of hepatoma cells. The technical scheme is the application of oroxylin A in preparation of the inhibitor with the targeting effect on AFP of the hepatoma cells. The application proves that oroxylin A can have the targeting effect on a clinical diagnostic mark AFP of hepatoma, can down-regulate protein level of AFP, is directly bound with AFP, inhibits bonding of AFP and tumor suppressor protein PTEN (phosphatase and tensin homolog), has effects of inhibiting proliferation of the hepatoma cells and inducing apoptosis of the hepatoma cells, and has better clinical value.

The invention relates to a method for controlling watermelon fusarium wilt, and belongs to the field of agricultural production techniques. A compound preparation consisting of carbendazim and oroxylin A is sprayed on leaf surfaces 1-3 times, and the one-time spraying is carried out every 7-15 days, and thus the control effect can be improved, the wax gourd sclerotiniose is effectively controlled, the consumption of effective ingredients is reduced, the pharmaceutical cost is saved, and the environment pollution is reduced.

The invention discloses a radix scutellariae soup, and application of an equivalent component group of the radix scutellariae soup to improvement of the chemosensitivity of the colon cancer on the irinotecan. The invention finds that the radix scutellariae soup can be beneficial to remarkably improving the chemosensitivity of the colon cancer on the irinotecan, namely, improving the killability ofthe irinotecan on the the colon cancer, the inhibiting effect on colon cancer cell proliferation, and the acceleration on colon cancer cell apoptosis, so that without remarkably reducing a chemotherapeutic effect of the irinotecan, the administration dosage of the irinotecan is reduced favorably, and the chemotherapy side effects of the irinotecan is relieved. The invention finds that through a composition prepared from gallic acid, scutellarin, baicalein, wogonin, glycyrrhizic acid and oroxylin A in the radix scutellariae soup, the chemosensitivity of the colon cancer on the irinotecan can be remarkably improved, and the medicine effect is basically consistent to the equivalent dosage of radix scutellariae soup; the find is helpful to develop a composition medicine with definite development components and controllable quality so as to replace the radix scutellariae soup for assisting colon cancer chemotherapy, and also helpful to adopt the composition as a quality control index to control the quality of the radix scutellariae soup.

The invention discloses application of oroxylin A and a PD-1/PD-L1 inhibitor in preparation of a medicine for treating liver cancer, and belongs to the technical field of medicines. According to the application disclosed by the invention, an experiment of treating mouse liver cancer cell H22 subcutaneous transplantation tumor by combining the oroxylin A with the PD-1/PD-L1 inhibitor proves that the combination of the oroxylin A with the PD-1/PD-L1 small-molecule inhibitor or the PD-1 monoclonal antibody can obviously improve the anti-tumor effect of independent use of the oroxylin, the PD-1/PD-L1 small-molecule inhibitor and the PD-1 monoclonal antibody, an obvious inhibition effect on the weight of an experimental animal is not generated, and more importantly, the survival time of tumor-bearing mice is obviously prolonged. Therefore, the oroxylin A can promote the curative effect of the immune checkpoint inhibitor on the liver cancer, and the combined medication mode can play a great role in the future liver cancer treatment.

The invention discloses a use of oroxylin A as a transketolase inhibitor. The transketolase inhibitor is used for treating cancer. The use of the transketolase inhibitor for treating the cancer is realized by inhibiting the activity and expression of the transketolase to inhibit a non-oxidize pentose phosphate pathway and activate a p53 signal channel, thereby playing an antitumor effect. DARTS isused for identifying a target protein directly combined with oroxylin A in the human liver cancer cell HepG2, a key enzyme-transketolase of the non-oxidize pentose phosphate pathway is discovered andis a direct combined target point of the oroxylin A, a KD value is 11.2 microM, and the interactive effect is proved by virtue of the molecular docking, enzymatic activity determination, protein expression and the antitumor effect variation after the transketolase interference. The research result shows that the oroxylin A is an effective transketolase inhibitor.

The invention discloses application of Oroxylin A in preparation of medicines for promoting liver regeneration. Experiments show that Oroxylin A can effectively protect liver, improve liver regeneration by means of improving expression level of IL-1Ra and TNF-alpha of liver cells, and promote the reshaping of the liver structure and is beneficial to restore of liver function. Experiments show that the survival rate of mice with liver injury in experimental group can be remarkably improved by Oroxylin A.

The invention belongs to the technical field of traditional Chinese medicines, and particularly discloses separation and identification of anti-migraine effective components in Duijinsan and application of the anti-migraine effective components in the Duijinsan. The anti-migraine effective components in the Duijinsan are screened and selected from any one monomeric compound or a mixture composed of more than one monomeric compound in any proportion of baicalin, chrysin-7-O-beta-D-glucuronide, oroxylin A-7-O-beta-D-glucuronide, chrysin-6-C-arabinose-8-C-glucoside and chrysin-6-C-glucose-8-C-arabinoside. A research result shows that the monomeric compound obtained through separation has a remarkable effect in an anti-migraine medicine.

The invention discloses a baical skullcap root extract-FGF1 compound. The baical skullcap root extract-FGF1 compound is a compound obtained by co-incubating a baical skullcap root extract and FGF1, wherein the baical skullcap root extract is baicalin, oroxylin A-7-O-beta-D-glucuronide or wogonoside, and the obtained compound is an FGF1-baicalin compound, an FGF1-oroxylin A-7-O-beta-D-glucuronide compound or an FGF1-wogonoside compound. The incubating comprises the following steps: 1) dissolving the baical skullcap root extract with methanol, performing blow-drying with nitrogen, and performingre-dissolving with water; and dissolving FGF1 target protein in a PBS buffer solution, performing mixing with the baical skullcap root extract aqueous solution, performing incubating at 36-38 DEG C for 25-35 min, and performing vacuum freeze-drying. The invention further discloses an application of the FGF1-baicalin compound, the FGF1-oroxylin A-7-O-beta-D-glucuronide compound or the FGF1-wogonoside compound in the aspect of promoting cell proliferation.

The invention discloses an oroxylin A solid dispersion, a preparation method and application thereof. The solid dispersion comprises oroxylin A and a composite carrier material, wherein the compositecarrier material is a mixture of hypromellose and polyacrylic resin Eudragit EPO. The preparation method comprises the steps of mixing the oroxylin A and the composite carrier material in a ratio uniformly, then adding the mixture to an extruder, performing hot melting and extrusion, extruding the materials in a strip shape from a die hole of a machine head, crushing after the extruded product iscooled, and sieving to obtain the oroxylin A solid dispersion. The solid dispersion technology is combined with the pH micro-environment technology to significantly improve the solubility and dissolution rate of the oroxylin A in the medium.

The invention discloses a method for simultaneously detecting baicalin, baicalein, wogonin and oroxylin A in radix scutellariae, which is provided by the invention. The method comprises the following steps: 1) preparing a scutellaria baicalensis sample solution to be detected and a reference substance solution; (2) detecting by adopting a high performance liquid chromatography; chromatographic conditions adopted by the high performance liquid chromatography are as follows: a mobile phase is a mixed solution of methanol and a phosphoric acid aqueous solution with the mass fraction of 0.1%-0.4%, and the volume percentage content of the methanol is 65%-70%; the elution mode is isocratic elution. By adopting the detection method disclosed by the invention, the chromatographic peaks of the baicalein, the baicalin, the wogonin and the oroxylin A can reach baseline separation, and the separation degree is greater than 1.5. According to the method, the organic solvent-phosphoric acid aqueous solution is used as the mobile phase, the elution ratio is fixed, the chromatographic peak shape is good, the separation degree and the accuracy are high, the cost is low, the detection time is shortened, the analysis efficiency is improved, and the consumption of the mobile phase is reduced.

The invention discloses a traditional Chinese medicine general flavone extract for treating cataract and a composition, a preparation method and medical application of the traditional Chinese medicine general flavone extract, traditional Chinese medicine general flavone is oroxylum indicum general flavone, and the invention further provides a quality control method of the oroxylum indicum general flavone. The oroxylum indicum general flavone contains baicalein, baicalin, oroxylin A, oroxylin B, chrysin and chrysin-7-O-glucuronide, and the total content of the six flavonoid compounds is greater than 20%.