629 results about "Aglycone" patented technology

Isoflavones are modified by esterification at one or more of the C4′, C5, C6, and C7 positions to promote bioavailability, and especially to enhance solubility over the corresponding unesterified isoflavones. Preferred modifications produce a carboxylic acid hemiester or a phosphate ester which is biologically hydrolysable. Preferred starting isoflavones are genistin and daidzin, and still more preferably comprises an aglycone form such as genistein or daidzein. Esterified isoflavones may be employed therapeutically or prophylactically for a variety of conditions, provided as a dietary supplement, or added to natural or processed food-stuffs. Further preferred uses include incorporation of contemplated compounds into topical formulations, and especially cosmetic topical formulations.

The present invention is one kind of 17-hydroxy C27 steroid compound and its synthesis and use. The synthesis process of the present invention is simple and suitable for industrial production in synthesizing pennogenin as well as dihydro pennogenin and OSW-1 aglycone analog.

The invention relates to a herba epimedii aglycone phospholipid compound or a cyclo-herba epimedii aglycone phospholipid compound, which is characterized by being composed of herba epimedii aglycone or cyclo-herba epimedii aglycone and phospholipid, wherein the mass ratio of the herba epimedii aglycone or the cyclo-herba epimedii aglycone and the phospholipid is 1:0.5 to 5. The phospholipid in theherba epimedii aglycone phospholipid compound or the cyclo-herba epimedii aglycone phospholipid compound has the positive function on treating the osteoporosis, and the medicine and the phospholipidin the phospholipid compound of the herba epimedii aglycone or cyclo-herba epimedii aglycone medicine has the synergic function on treating the osteoporosis; after the phospholipid and the herba epimedii aglycone or the cyclo-herba epimedii aglycone are prepared into the compound, the dissolvability thereof is improved greatly, and the disadvantages of poor water solubility and fat solubility andlow bioavailability are solved; the herba epimedii aglycone phospholipid compound or the cyclo-herba epimedii aglycone phospholipid compound has simple preparation process and moderate reaction condition, and is suitable to industrialized big production. The invention discloses a preparation method thereof.

A process for preparing high-purity momordicoside from fructus momordicae includes such steps as pulverizing, reflux extracting in alcohol, filtering to obtain extract A, suspending it in water, extracting in ethyl acetate 1-3 times, recovering ethyl acetate mother liquid, extracting in n-butanol 1-3 times, recovering n-butanol to obtain extract B, passing it through polyamide column, water washing, concentrating to obtain coarse saponin, chromatography by silica gel column, eluting with chloroform-methanol-water, collecting coarse momordicoside V, chromatography, water washing, eluting with alcohol, and collecting product.

The present invention belongs to the technical field of biological pharmacy, and in particular relates to a preparation and purification method of tetra-hydroxyl xanthone mango aglycone (norathyriol), and an application thereof in hypoglycemic medicine. Based on biological experiments, mango glycoside is used as raw material; under the condition with phenol and hydroiodic acid, carbon-carbon bonds are broken to produce the crude product of mango aglycone; the crude product is separated and purified through silica gel column chromatography so that the mango aglycone is separated; the yield rate reaches 12 percent, the purity is higher than 95 percent, and the reproduction performance is good; the IGTT of C57BL / 6 normal mice is effectively improved with the norathyriol; and simultaneously the quantity of insulin secretion induced by glucose in vivo for the C57BL / 6 normal mice can be improved with the norathyriol. Therefore, the mango aglycone can be applied for preparation of hypoglycemic medicine.

The present invention relates to methods and pharmaceutical compositions for treating obesity or obesity-related disorders in a subject suffering from or predisposed to developing obesity or an obesity-related disorder, or for inhibiting the infectivity of HIV, by administering oleuropein, an analogue or derivative thereof, or the major metabolites of oleuropein including oleuropein aglycone, hydroxytyrosol, and elenolic acid or their analogues, or derivatives thereof, an iridoid glycoside, or a secoiridoid glycoside or analogues or derivatives thereof, or any combination of the foregoing including olive leave extract. The invention also relates to methods for screening / diagnosing a subject having, or predisposed to having obesity or a related disorder by measuring the expression profiles of an adipogenic gene selected from PPARγ2, LPL and αP2 gene and gene product, or other adipogenic, lipogenic, or lipolytic genes and gene products in an individual. The invention further provides for screening for novel oleuropein analogues.

The invention discloses a full chemical synthesis method for mangiferin aglycones. In a process of full chemical synthesis, the mangiferin aglycones are prepared from 3,4-methyl dihydroxybenzoate serving as an initiative raw material through six chemical reactions and steps. The synthetic process of the full chemical synthesis of the mangiferin aglycones has the advantages of short synthetic routes, mild condition of a synthetic reaction and high yield, and can be used for large-scale production.

The invention relates to an endotoxin adsorbent, which in detail relates to a method of preparing endotoxin adsorbent for blood perfusion. The method employs spherical agarose gel with good biocompatibility as base material, employs epichlorohydrin, hexamethylene diamine, 1, 1'-carbonyldiimidazole as activating agent, and bonds polymyxin B for endotoxin removal. The invention is characterized in that it overcomes the toxicity of cyanogen bromide and instability of aglycone, improves the safty and reliability of operation, reducesnon-specific adsorption through bonding polymyxin B with 1, 1'-carbonyldiimidazole, and improves biocompatibility of adsorbent and suits for treating endotoxemia. The invention is also characterized by simple experimental procedure and high clearance for endotoxin.

A method of synthesizing 4-R-substituted anthracyclines and their corresponding salts from 4-demethyldaunorubicin includes the steps of treating 4-demethyldaunorubicin with a sulfonylating agent to form 4-demethyl-4-sulfonyl-R3-daunorubicin. 4-Demethyl-4-R3-sulfonyl-daunorubicin is then subject to a reducing agent in the presence of a transition metal catalyst in a temperature range of about 30° C. to about 100° C. in a polar aprotic solvent in an inert atmosphere. Protected 4-demethoxy-4-R-daunomycin then undergoes hydrolysis in a basic solution to form the 4-R-substituted anthracyclines. The novel method lacks the step of forming a stereospecific glycoside bond between aglycone and aminoglycoside. The method also increases the yield of the final product up to 30 to 40%.

The invention relates to a burdock fruit extract, its preparing process and use thereof, wherein the extract comprises 51-80 wt% of total lignanoids compound with burdock aglycone as the main ingredient and burdock glycosides, and 20-49 wt% of other constituents.

The invention relates to a preparation method of epimedium aglycone, which comprises the steps that dried epimedium is pulverized or cut into segments, 30-95% ethanol or 30-100% methanol is added for reflux extraction, the extract solution is decompressed and concentrated to obtain paste, 10-100 ml of acetate-sodium acetate buffer solution with the pH of 3.5-9.0 is added into each gram of paste, snailase is added for hydrolysis, the mass ratio of enzyme to paste is 0.05-5, the reaction temperature is 15 to 80 DEG C, the reaction time is 2 to 72h, the reaction solution is centrifuged, the precipitate is dissolved with an organic solvent, filtration is carried out to obtain filtrate, the solvent is steamed away to obtain crude epimedium aglycone, and pure epimedium aglycone is obtained after recrystallization. The invention has the characteristic that the epimedium extract is directly converted into high-purity aglycone in one step by utilizing the strong enzymic hydrolysis of the snailase so as to simplify the operation steps with strong purposiveness and high conversion rate, and has the advantages of no pollution and large-scale production. The invention overcomes the shortcomings of large destruction on the aglycone, serious pollution, poor purposiveness, low conversion rate, difficult separation and purification and the like of the prior art.

The invention provides an epimedium aglycone liposome. The liposome consists of the following components in percentage by weight: 50 to 85 percent of soya bean lecithin, 10 to 35 percent of cholesterin and 2 to 25 percent of epimedium aglycone; the surface of the liposome is a phospholipid bimolecular layer, and hydrophilic groups on the outer part of the bimolecular layer form a hydrophilic cap; hydrophilic groups on the inner part of the bimolecular layer form an inner water phase, and hydrophobic groups between the bimolecular layer form a hydrophobic region; and the epimedium aglycone is coated between the phospholipid double layer of the liposome, and the absolute value of the Zeta electric potential is more than 40mV after the liposome is hydrated. The epimedium aglycone liposome has the characteristics that: 1, the preparation method is simply and easily implemented, the raw material, namely the soya bean lecithin has good bio-compatibility, and can be biodegradable, and the raw material is also wide in source and low in cost; 2, by utilizing the nanometer technology, the traditional Chinese medicine active ingredient, namely epimedium aglycone is coated between the phospholipid double layer of the liposome, so that the water solubility is improved; and 3, the epimedium aglycone liposome has better physical stability, and after being stood for quite a long time, the epimedium aglycone liposome has no delamination and flocculation. The invention also discloses a method for preparing the epimedium aglycone liposome.

The reagent, pharmaceutical formulation, kit, and methods of the invention provides a new approach for treating pancreatic cancers. The invention provides the use of Na+e / K+-ATPase inhibitors, such as cardiac glycosides (e.g. ouabain and proscillaridin, etc.), either alone or in combination with other standard therapeutic agents (chemo- or radio-therapies, etc.) for treating pancreatic cancers. The subject Na+ / K+-ATPase inhibitors, such as cardiac glycosides, including bufadieneolides or their corresponding aglycones (e.g., proscillaridin, scillaren, and scillarenin, etc.), especially in oral formulations and / or solid dosage forms containing more than 1 mg of active ingredients.

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.

A novel, scaleable and improved process for preparing pentostatin and its analogs is disclosed. The method comprises the diastereospecific synthesis of the nucleobase from commercially available L-Dialkyl tartarates.

The invention discloses application of fructus forsythiae aglycone in preparing a medicament for preventing or treating liver injury or liver failure, and belongs to the medical field. The fructus forsythiae aglycone is a traditional Chinese medicine monomer obtained by extracting from the conventional fructus forsythiae, and is shown to have better treatment effect for the liver injury caused by acetaminopben, the livery injury caused by anti-tumor drug cis-platinum, acute or chronic livery injury caused by carbon tetrachloride, the livery injury caused by D-galactosamine and the liver failure caused by the D-galactosamine and lipopolysaccharide according to an animal test, has effect, which is better than that of fructus forsythiae and fructus forsythiae aglycone, in treating liver injury or liver failure. The fructus forsythiae aglycone is exact in curative effect and low in side effect for treating the liver injury and the liver failure, and has wide medical application prospect.

The invention relates to the field of medicinal chemistry, and discloses a method for preparing mangiferin aglycone. The method comprises that: step 1, 2-halogenate-4,5-dimethoxy benzoic acid and 1,3,5-trimethoxy benzene are subjected to Friedel-Crafts reaction, so a compound which has a structure in a formula IV is generated; step 2, the compound in the formula IV is selectively demethylated, and a compound which has the structure in the formula V is generated; step 3, the compound in the formula V is cyclized, and a compound which has the structure in the formula VI is generated; and step 4, the compound in the formula VI is completely demethylated, and mangiferin aglycone is generated. The method for preparing mangiferin aglycone improves the synthetic yield of the mangiferin aglycone, has the characteristics of cheap and easily-obtained raw materials, less synthetic steps, convenience in operation, easiness in control and high product purity, and can be widely applied in industrial production.

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 reagent, pharmaceutical formulation, kit, and methods of the invention provides a new approach to treat refractory cancers using Na+ / K+-ATPase inhibitors, such as cardiac glycosides, including bufadienolides or their corresponding aglycones (e.g., proscillaridin, scillaren, and scillarenin, etc.), especially in oral formulations and / or solid dosage forms containing more than 1 mg of active ingredients.

The present invention provides a method of treatment or management of various adaptogenic conditions, such as, stress in mammals, more particularly, humans, comprising administering Withania somnifera plant extract. A high purity extract composition comprising withanolide glycosides, oligosaccharides, withanolide aglycones and a minimum level of polysaccharides, and a pharmaceutically, veterinary or nutritionally acceptable carrier(s) is disclosed. Preferably, the composition of the present invention can be devoid of any alkaloids or contains trace levels of alkaloids. The method of treatment or management of stress administering the composition comprising Withania somnifera of the present invention does not suffer from any one of the abovementioned side effects even after prolonged use. A method of preconditioning a mammalian patient to improve the patient's resistance and reaction to subsequently encountered stress is described.

The invention discloses a process for extracting and separating isoflavones from kudzu vine, which comprises the steps of disintegrating kudzu vine to 60-150 meshes, loading into a liquid dynamic continuous flow upstream extraction device for alcohol extraction, combining the extract liquid and filtering, concentrating the filtrate to obtain total isoflavones extract, and separating the total isoflavones extract to obtain puerarin and soybean aglycone.

The invention relates to a method for detecting dammarane tetracyclic triterpenoid saponin and secondary aglycone. The inventive method uses high-efficiency liquid color spectrum-mass spectrum coupled device, wherein the conditions of high-efficiency liquid color spectrum comprises: color spectrum column is ODSC18 column; the column temperature is 20-38Deg. C; the conditions of mass spectrum comprise: the ion source is Turbo Ionspray source; the ejecting voltage is 3000-5000V; the Tem is 250-300Deg. C; the detector uses triplicate four-electrode serial mass spectrum detection and positive ion detection; the scanning method uses multi-reaction detection (MRM); CE is 17-36V; DP is 8-110V; the ion detection comprises: processing impact induce dissociation on the quasi-molecule ion peak of said saponin of first-stage scanning mass spectrum, to obtain the second-stage fragment ion; and uses multi-reaction detection (MRM) scanning method to analyze the ion reaction quantitatively, to represent the blood drug density of monomer saponin and secondary aglycone.

The invention discloses a method for converting astragalosides to prepare cycloastragenol by two-step enzymolysis; the method comprises the specific steps of using astragalosides as a substrate, using two different hydrolases to hydrolyze and break beta-xyloside bond at site C3 of the astragalosides and beta-glucoside bond at the site C6 respectively to obtain aglycone cycloastragenol of the astragalosides, extracting, performing silica-gel column chromatography, recrystallizing with ethanol, and purifying to obtain the finished cycloastragenol up to 95% and higher in purity. The problem that damage of three-membered ring structure of astragalosides during the preparation of cycloastragenol by a chemical process causes massive byproducts is solved, the defects of traditional cycloastragenol preparation methods, such as low substrate conversion rate, step complexity and environmental pollution, are overcome. The method has the advantages that substrate specificity is high, the substrate astragalosides is completely converted, the steps are simple, the conditions are mild, the cost is low, and the method is a mild biological preparation method, has no environmental pollution and is suitable for industrial production.

The invention belongs to the technical field of biological pharmacy, and in particular relates to suppressive activity detection of tetrahydroxy norathyriol on protein-tyrosine-phosphatase (PTP) 1B, improvement of resistance function of insulin and accpication in medicament for PTP1B related diseases. Proved by in vitro enzyme suppression experiments, the invention testifies that mango aglycone is the competitive suppressant of restructuring humanized PTP1B with IC50 value being 9.2 mu m; mango aglycone can ensure the sensitivity of C57BL / 6 normal mouse and ob / ob diabetes model mouse on insulin to be obviously improved, and reduce blood sugar of experimental animals, which suggests that mango aglycone is a novel suppressant of PTP1B, and can be taken as potential lead compound to be applied in preparing medicament for curing insulin resistance related diabetes, obesity and other metabolic syndrome, tumor and other PTP1B related diseases.

Aminoalkyl glucosaminide phosphate (AGP) compounds that are adjuvants and immunoeffectors are described and claimed. The compounds have a 2-deoxy-2-amino glucose in glycosidic linkage with an aminoalkyl (aglycon) group. Compounds are phosphorylated at the 4 or 6 carbon on the glucosaminide ring and comprise three 3-alkanoyloxyalkanoyl residues. The compounds augment antibody production in immunized animals as well as stimulate cytokine production and activate macrophages. Compositions and methods for using the compounds as adjuvants and immunoeffectors are also disclosed.

The invention relates to a preparation method of hydrated icariin which belongs to the synthesis field of natural compounds. The preparation method of the hydrated icariin is characterized in that the hydrated icariin is obtained from icariin after two steps of the hydrolysis reaction of hydrochloride and cellulose. The desugarization hydrolysis is complete. The chemical structure of barrenwort aglycone can be changed, which changes the barrenwort aglycone into the hydrated icariin. The yield is high. The treatment after the reaction is convenient. And the purity of products fully complies with the medical standards.

A method of producing a flavonoid aglycone concentrate from plant material containing a suitable flavonoid glycoside and / or conjugate thereof comprising the steps of: (i) enzymatically converting the flavonoid glycoside or conjugate thereof into the flavonoid aglycone; and (ii) adjusting the pH to render the flavonoid aglycone relatively insoluble and forming a concentrate containing the same.

The invention discloses a liposome preparation containing antineoplastic metallic complex which is derived by hydrophilic polymers and aglycones, in one embodiment, the antineoplastic metallic complex includes Oxaliplatin, the hydrophilic polymers include polyethylene glycol, the aglycone is transferrin. In accordance with the invention, the transferring expressed on the surface of the tumor cell can facilitate the absorption of agent in the liposome by the tumor cells. The invention also provides the pharmaceutical composition containing the liposome and method for application.

The invention provides a method for producing non-bitter and tasty stevioside powder. It is determined that the bitter taste of stevioside is mainly caused from aglycone part. The invention includes the aglycone physically in extracted and condensed stevioside solution, then continues condensation, crystallization, drying and granule production. The invention is characterized by maintained sweetness, no damage to original atom structure, simple process and low cost.