99 results about "Betulin" patented technology

Betulin and dihydrobetulin acyl derivatives according to the present invention have been found to have potent anti-HIV activity. The compounds of the present invention have Formula I as described herein, or pharmaceutically acceptable salts thereof; wherein R1 is a C2-C20 substituted or unsubstituted carboxyacyl or ester thereof; R2 is hydrogen, halogen, hydroxyl or —OR3, R3 is C2-C20 substituted or unsubstituted carboxyacyl; and R4 is hydrogen or C(C6H5)3; wherein the dashed line represents an optional double bond between C20 and C29.

The present invention provides for pharmaceutical compositions that includes a triterpene (e.g., betulin) and an essential oil (Vicks® Vapor Rub). The present invention also provides for a cosmetic formulation that includes a triterpene (e.g., betulin) and an essential oil (Vicks® Vapor Rub). The present invention also provides a method of treating a fungal infection that includes administering (e.g., topically applying) an effective amount of the pharmaceutical composition to the tissue afflicted with the fungal infection, or the tissue at risk of being afflicted with the fungal infection.

The present invention relates to novel synthetic derivatives of betulin and the use of such derivatives as pharmaceuticals. The present invention is directed to novel compounds of Formula I: or a pharmaceutically acceptable salt or prodrug thereof.

Personal care compositions and formulations, which include conventional concentrations of known hair and skin altering components and a cosmetically acceptable amount of oil-soluble betulin and allo-betulin esters or ethers derived from betulin or allo-betulin in effective amounts are disclosed.

Methods of treating a fungal or yeast infection and of killing or inhibiting fungi or yeast are disclosed. The methods use derivatives of triterpenes that are abundant in birch bark and other plants. The triterpenes include betulin, allobetulin, and lupeol.

The invention discloses a method for extracting betulin from birch barks, comprising the following steps: firstly, crushed birch barks are added into an ethanol water solution, undergo reflux extraction under auxiliary processing of ultrasonic waves, and then are filtrated for removal of residue, and an extract is obtained; secondly, solid powder is separated out after decompression and concentration of the extract, and then dried to the constant weight so as to obtain betulin coarse products; and thirdly, the betulin coarse products are added into an organic solvent, undergo ultrasonic treatment and then stand, crystals are separated out, and the betulin is obtained after the separated crystals are dried to the constant weight. The method has a simple operation flow, short extraction time, low production cost and high safety, and provides a better method and a better platform for further development and utilization of natural products.

The invention relates to a method for extracting and purifying the betulin from birch bark. The invention comprises the following procedures, cutting the birch bark into the bark particles, heating, refluxing and extracting by aqueous ethanol solution, filtering, vacuum concentration of the filtrate, cooling, collecting and drying the separated crude betulin. The method of the invention can obtain the betulin with the purity of more than 90 percent, and has the advantages of simple process, lower cost and being suitable for the industrial production.

The invention provides methods for separating outer birch bark from inner birch bark. The invention also provides methods for isolating betulin; lupeol; betulinic acid; 9,10-epoxy-18-hydroxyoctadecanoic acid; 9,10,18-trihydroxyoctadecanoic acid; polyphenolic polymers and fatty acids from birch bark.

The present invention provides a process of preparing betulin-28-aldehyde from betulin. The process includes contacting betulin with a compound of formula (I), e.g., TEMPO (2,2,6,6-tetramethylpiperidine 1-oxyl) for a period of time effective to provide betulin-28-aldehyde. The present invention also provides a process of preparing betulinic acid. The process includes contacting betulin with a composition that includes: sodium hypochlorite (NaOCl); sodium chlorite (NaClO2), potassium chlorite (KClO2), or a combination thereof; and a compound of formula (I), e.g., TEMPO (2,2,6,6-tetramethylpiperidine 1-oxyl); for a period of time effective to provide betulinic acid.

The present invention relates to a compound extract of fomes yucafensis and betulin, its preparation method and preparation. Said preparation method includes the following steps: (1), respectively pulverizing fomes yucafensis and betulin; (2), mixing (by weight portion) 2-8 portions of fomes yucafensis powder and 3.5-11.5 portions of betulin powder; soaking the obtained mixturein water, heating to make water extraction, taking out supernatant fluid to obtain the supernatant fluid A; (3), adding water into the mixture extracted by step 2 and making water extraction, taking out supernatant fluid to obtain supernatant fluid B; (4), mixing the above-mentioned two supernatant fluids to obtain their mixed liquor, removing protein, lipid and impurity; and (5), concentrating and drying said mixed liquor so as to obtain the invented compound extract of fomes yucafensis and belutin.

The invention relates to betulin derivatives, and to the use thereof as agents against protozoa of the genus Leishmania and against leishmaniasis in applications of pharmaceutical industry.

The instant application is directed to bidesmosidic betulin and betulinic acid saponin derivatives of formula (I), and use thereof as antitumor agents. In particular, said compounds are effective in treating lung carcinomas, colorectal adenocarcinomas, breast adenocarcinomas, and prostate adenocarcinomas. Methods of synthesizing said compounds through selective glycosylation of the C-28 and C-3 position, and diagnostic methods for identifying tumours suitable for treatment by said compounds are also disclosed.

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 reliable conversion process, low cost and is suitable for the industrial production.

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 relates to a preparation method of extract of downy leaf of white birch, its new medicine application and medicine composition containing said extract. It using water to repeatedly soak downy leaf ow hite birch to prepare the extract of downy leaf ow hite birch, and said extract can be used to prepare the medicine with the functions of transquilizing the mind, resisting anxiety and resisting depression.

The present invention provides for compositions that includes a triterpene (e.g., betulin) and a carrier (e.g., lanolin). The compositions are useful for skin care (e.g., as cosmetic formulations), and as therapeutic formulations, e.g., for treating topical fungal infections.

The invention discloses a bio-based hemodialysis membrane and a preparation method thereof. The hemodialysis membrane is prepared from polylactic acid, laminarin, thiolated chitosan, silk fibroin, sodium ascorbyl phosphate, cellulose acetate, dithiothreitol, stachyose, betulin caffeate, ammonium persulfate, ferulic acid, hydroxyethyl starch, N-benzyl glycine hydrochloride, deoxycholic acid, polyhydroxyalkanoate, hexamethylenediamine, hyaluronic acid, benzoperoxide and dimethyl sulfoxide. According to the prepared hemodialysis membrane, the tensile strength is not lower than 7.0 MPa, the transmittance of urea is higher than 86%, the transmittance of beta2 microglobulin is higher than 66%, the rejection rate of macromolecular protein is higher than 95%, the biocompatibility is good, coagulation, thrombus, inflammation, poisoning and other adverse reactions do not exist, and an application prospect is wide.

Betulin and dihydrobetulin acyl derivatives according to the present invention have been found to have potent anti-HIV activity. The compounds of the present invention have Formula I as described herein, or pharmaceutically acceptable salts thereof; wherein R1 is a C2-C20 substituted or unsubstituted carboxyacyl or ester thereof; R2 is hydrogen, halogen, hydroxyl or —OR3, R3 is C2-C20 substituted or unsubstituted carboxyacyl; and R4 is hydrogen or C(C6H5)3; wherein the dashed line represents an optional double bond between C20 and C29.

The invention belongs to the field of biological engineering, and particularly relates to a method for improving the content of betulin and oleanolic acid in a birch cell by utilizing MeJA (methyl-jasmonate) and SA (salicyl acid), which comprises the following steps of: inoculating a birch tissure culture seedling stem to NT + 0.1 mg / L of 6-BA and 0.01 mg / L of TDZ culture mediums to induce birch callus, and obtaining a birch suspension cell with high content of total triterpenes through multi-time subculture, screening and suspension culture; inoculating the screened cell into the same liquid culture medium, wherein the inoculation amount is 3g / 100ml; adding 100mu Mum / L of MeJA and 50mg / L of SA when the shake culture is performed at the seventh day; after 24-48h, obtaining the product; and detecting the content of total triterpenes, betulin and oleanolic acid in the cell. Through the comparison of the two kinds of processing methods, the content of total triterpenes is improved by 21.6-31.7%, the content of oleanolic acid is improved by 277.4-369.34%, and the content of betulin is improved by 44.42-179.58%. The application of the invention provides a new path for solving the problem of shortage of natural plant drug resources and realizing large-scale industrial production of betulin and oleanolic acid drugs.

The invention discloses a novel external wall heat insulating foaming putty, which is mainly formed by the following materials with percentage by weight, 15-25% H2O, 0.05-0.15 preservative agent, 0.8-1.5% acrylate, 0.2-0.5% dispersing agent, 1-1.5% anti-freeze agent, 0.5-2% NH4 HCO3, 1-2% 12 carbon betulin, 3-5% wood fiber or polypropylene fiber, 0.4-0.6% water-loss reducer, 10-20% propyl benzene emulsion, 20-30% CaCO3 powder, 30-40% talcum powder, 3-5% polyphenylene particle and 0.5-1.5% wax emulsion. The external wall heat insulating foaming putty adopts the self-foaming principle, provides heat insulating effect through adding polyphenylene particle in heat-insulating mortar, has excellent heat insulating effect, and can be extensively applied on the external walls of buildings.

The invention relates to a foam formulation comprising an emulsion, comprising an oil phase and an aqueous phase, wherein the emulsion comprises at least one triterpenoid. Further the invention relates to anemulsion comprising an oil phase and an aqueous phase, wherein the emulsion comprises at least one triterpenoid selected from the group consisting of betulin, betulinic acid, lupeol, erythrodiol, oleanolic acid, (C1-C6) alkyl esters of the aforementioned acids, or mixtures thereof, and wherein the oil phase comprises at least one membrane-forming substance forming a lamellar arranged membrane in the emulsion.

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 invention belongs to the field of natural organic chemistry and relates to a method for enriching and purifying betulin in birch barks by utilizing a batch distillation-macroporous absorption resin method. The method has the advantages of good adsorption selectivity to betulin, quickness of adsorption and resolution, larger adsorption capacity, convenience and quickness of extraction, rich raw material source, low production cost, obvious separation effect and high extraction purity, can be used for obtaining a semi-finished betulin product with a content higher than 35 percent and a finished betulin product with a content higher than 98 percent and overcomes the defects of relatively lower conventional extraction ratio and low extraction purity. In the invention, macroporous absorption resin having stable physical and chemical properties, larger surface area, higher exchange speed, higher mechanical strength, strong antipollution capacity and good heat stability is used, which can selectively adsorb the betulin from the solution through physical adsorption, thus the invention has the advantages of quickness of adsorption and resolution and larger adsorption capacity.

The invention provides improved processes for the extraction of betulin, lupeol, betulinic acid, suberinic acids, and / or other organic compounds and compositions from birch bark. In some embodiments, the birch bark can be physically processed prior to the extraction process, which can further improve the yield of the extraction. The bark processing can include, but is not limited to, one or more of pelletizing the bark, baling the bark, pucking the bark, or compressing the bark, to a form that is more dense per volume unit than prior to the processing.

The invention provides novel compounds that are quaternary amine derivatives of betulin and other triterpenes. The compounds have antibacterial, antifungal, and surfactant properties.

The invention discloses a method to distill lupeol from birch genus plant that includes the following steps: smashing the dry birch bark, using methylene chloride to take back flowing and distilling, recycling methylene chloride, placing for deposition, filtering, removing filtrate and the washing deposit by a little cyclohexane several time to remove the low polarity impurity; recrystallizing for three times by absolute ethyl alcohol and acetone, the lupeol would be gained. The invention has the advantage of low cost, common raw material, simple technology.

The present invention provides birch bark pellets that include outer birch bark. The present invention also provides methods of manufacturing birch bark pellets from outer birch bark. The present invention also provides methods for obtaining a natural product from birch bark pellets. The birch bark pellets are manufactured from outer birch bark that includes relatively low amounts of inner birch bark and wood. The birch bark pellets meet the requirement for extraction, to obtain e.g., betulin and / or lupeol from the pellets.

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.