57 results about "Betulic acid" patented technology

This invention features betulinic acid derivatives having the formula: wherein the variables are defined herein. The invention also provides related compounds and intermediates thereof, as well as pharmaceutical compositions, kits, and articles of manufacture comprising such compounds. Treatment methods and methods of manufacture are also provided.

The invention relates to a novel purpose of eucommia chemical components as blood vessel protective agents. Specifically, the invention relates to a purpose of eucommia or eucommia extracts in preparing medicines used as blood vessel protective agents and / or antihypertensive agents, or in preparing medicines used for treating and / or preventing vascular proliferation diseases. The eucommia extracts comprise at least one component selected from the following: geniposide, wogonin, Qianye extract A, alpha-oxygen-beta-D-glucopyranoside-4,2', 4'-trihydroxyl dihydrochalcone, and betulic acid. According to the invention, the 5 chemical components or the eucommia extracts comprising the 5 chemical components can be used as effective blood vessel protective agents and / or antihypertensive agents, and can be used for treating and / or preventing vascular proliferation diseases.

The invention discloses a method for synthesizing betulic acid by carrying out biocatalysis on betulin, comprising the following steps: (1) preparing armillaria luteo-uirens ZJUQH wet cells; (2) adding armillaria luteo-uirens ZJUQH wet cells into ionic liquid or a two-phase system for pre-culture to obtain a pre-culture system; (3) adding betulin solution in the pre-culture system for fermentation culture for 6-24 hours at 25-30 DEG C to obtain transformed culture solution; (4) processing the transformed culture solution to obtain betulic acid. The two-phase system is mixed solvent of ionic liquid and normal hexane, or mixed solvent of ionic liquid and phosphoric acid buffer solution. Compared with a conventional method, the inventive method has higher product yield, shorter catalytic reaction time, simple product separation, lower volatility of ionic liquid system, better biocompatibility and no pollution to the environment.

The present invention provides a method for preparing an ester of betulin at the 3-position, e.g., betulin-3-acetate, including the selective alcoholysis of a betulin-3,28-diester, e.g., betulin-3,28-diacetate; a method for preparing betulin-3-acetate including (1) acetylating betulin to provide betulin-3,28-diacetate and (2) the alcoholysis of betulin-3,28-diacetate to provide betulin-3-acetate; and a method for preparing betulinic acid (1) acetylating betulin to provide betulin-3,28-diacetate, (2) the alcoholysis of betulin-3,28-diacetate to provide betulin-3-acetate, (3) oxidizing betulin-3-acetate to provide betulinic aldehyde-3-acetate, (4) oxidizing betulinic aldehyde-3-acetate to provide betulinic acid-3-acetate, and (5) deprotecting betulinic acid-3-acetate to provide betulinic acid.

A betulinic acid nano-liposome wrapped with a nanogold spherical shell is a nano drug-loading system with the particle size being 130-200 nm, a layer of nanogold spherical shell is formed on the surface of the betulinic acid nano-liposome modified by glutathione, and the surface plasma resonant absorption wavelength ranges from 750 nm to 850 nm. A preparation method of the betulinic acid nano-liposome mainly includes the steps that glutathione serves as a raw material to prepare the betulinic acid nano-liposome, and the surface of the betulinic acid nano-liposome has mercapto functional groups; the liposome and gold nanoparticles are inoculated under mild conditions, then a gold chloride solution is added, the mixture stands still for 15-40 min at room temperature and then placed in ice bath, and finally a sodium borohydride solution is added for inoculation for 4-9 h. The method can be implemented under normal-temperature, normal-pressure and mild conditions, operation is easy, and reaction is easy to control. The prepared betulinic acid nano-liposome wrapped with the nanogold spherical shell has good photo-thermal conversion performance, and release is controllable.

The invention discloses a method for extracting betulinic acid from persimmon leaves. The method comprises the steps that dry persimmon leaves are taken to be ground, added with water to mix and wet, added with bio-enzyme for natural enzymolysis for 4-7 days, the enzymolysis raw material is added with 70-90% ethanol and extracted under refluxing for 1-3 times, the extract is concentrated under reduced pressure until the alcohol concentration is 50-60%, and stood for crystallization, crystal substances are dissolved with 5-7 times of amount of alkaline ethanol solution, undissolved substances are filtered out, filtrate is regulated through hydrochloric acid or sulfuric acid solution to be neutral and centrifuged, crude extract is dissolved with ethanol for recrystallizing, and the betulinic acid is obtained after drying. By adopting the method for extracting the betulinic acid, the raw material resources are abundant, the method is simple to operate, and the industrialization production is benefited.

The invention discloses a method for synthesizing betulic acid by microbial cell bioconversion of betulin comprising the following steps: inoculating an Armillaria luteo-virens Sacc. ZJUQH to sterilized culture solution and obtaining a pre reaction system; adding a substrate solution containing the betulin and reacting for 5-7 days at between 25 and 30 DEG C, processing the converted culture solution and obtaining the betulic acid, wherein the betulin dosage is 0. 01-0. 1 g per each litre of culture solution. Comparing with the direct plant extraction of the betulic acid method and the chemical synthesis of the betulic acid method The method of the invention has advantages of short microbial cell culture time, easy operation and control, short whole bioconversion period, safe and reliableconversion process, low cost and is suitable for the industrial production.

The invention discloses a preparation method of triterpenic acid in a jujube material. According to the preparation method of the triterpenic acid in the jujube material, by using alcohols as an extracting agent and alcohol-acid as an eluant, the jujube material is heated, refluxed and extracted; the purity of the triterpenic acid obtained by using two separation methods of macroporous absorbent resin column chromatography and preparative liquid chromatography is high, the content of the triterpenic acid exceeds 90%, and main components are betulinic acid, ursolic acid and oleanolic acid. In the preparation process, organic solvents are all recycled, so that the preparation method of the triterpenic acid in the jujube material is economic and environmentally friendly. The preparation method of the triterpenic acid in the jujube material, disclosed by the invention, has the advantages that AB-8 or HPD100 adsorption resin is adopted, the AB-8 adsorption resin and the HPD100 adsorption resin are polystyrene low polar or nonpolar polymers, the service life is relatively long, and the triterpenic acid elution efficiency is relatively high. The preparation method of the triterpenic acidin the jujube material, disclosed by the invention, has the advantages that the preparative liquid chromatography is a maximum technical characteristic different from the characteristic of the conventional technology, and online monitoring and targeted separation are adopted, so that the separation efficiency is high.

The present invention relates to 23-hyroxy betulic acid fat emulsion as anticancer medicine and its preparation process, and belongs to the field of Chinese medicine and medicament preparation technology. The fat emulsion consists of 23-hyroxy betulic acid as active component and medicinal supplementary material, and includes 23-hyroxy betulic acid in 0.5-5 g / L, emulsifier for injection in 5-20 g / L, vegetable oil for injection in 100-250 g / L and osmotic pressure regulator in 18-25 g / L except water for injection. The present invention has simple preparation process, and the prepared 23-hyroxy betulic acid fat emulsion with antitumor effect may be orally taken or intravenously injected. The prepared 23-hyroxy betulic acid fat emulsion has low toxicity, high bioavailability, slow releasing, targeting, and body energy providing effect.

The invention belongs to the technical field of high polymer materials, and relates to a method for preparing a betulinic acid polymer by using a ball mill. The method comprises the steps of adding betulinic acid, a basic catalyst, a stabilizer and a water removal agent into a ball tank of a ball mill, starting the ball mill to react, dissolving a product with an organic solvent, pouring into methanol to separate out, filtering, collecting solids, and performing vacuum drying to obtain a betulinic acid polymer. High temperature is not needed in the reaction, no solvent is needed in the reaction process, the cost is low, the separation is simple, and certain pilot scale test and industrialization prospects are achieved. The obtained polybetulinic acid is a novel high-molecular compound andis not reported before.

A kind of modified 23-hydroxy betulic acid derivatives, their preparing process, the medicinal composition containing them and their application in preventing and treating tumor are disclosed.