24 results about "Betulinic acid" patented technology

The application belongs to the technical field of medicine, and discloses application of SERPINE1 protein or a coding gene thereof as a new target for hepatitis B virus treatment. The application first discloses that SERPINE1 promotes autophagy flux by directly combining PIKfyve protein, thereby significantly inhibiting HBV replication and HBsAg expression. Based on this, the application establishes a multi-dimensional target verification platform, and first discovers that a natural compound, betulinic acid, is a high-affinity agonist (KD=1.46 µM) of SERPINE1. In-vivo and in-vitro experiments prove that betulinic acid can effectively reduce the levels of HBsAg and HBV DNA, and has good safety. In addition, betulinic acid and entecavir show a synergistic antiviral effect (CI<1). The application provides a new target and treatment strategy for realizing functional cure of hepatitis B.

The present application belongs to the field of medicine, and particularly relates to betulinic acid nucleoside derivatives for preventing or treating cancer. Some compounds provided by the present application exhibit excellent inhibitory activity on test cancer cells, and particularly have unexpected inhibitory activity on colon cancer or prostate cancer cells. The compounds provided by the present application are expected to be used for preventing or treating colon cancer, prostate cancer and other cancers or symptoms related thereto.

The invention belongs to the technical field of nano biological materials, and discloses a preparation method and application of a betulinic acid self-assembly nano composite system loaded with dihydromyricetin, and the nano composite system takes betulinic acid as a carrier and dihydromyricetin as an active component. The assembly mechanism of the prepared nano assembly system is as follows: the hydrogen bond interaction generated by combining the phenolic hydroxyl group of the dihydromyricetin molecule with the carbonyl group in the betulinic acid molecule and the carbonyl group in the carboxyl group in the betulinic acid molecule is the main non-covalent interaction force. The nano-composite system has good biocompatibility, and the HT-29 cells have a good uptake effect on the nano-composite system. The method has certain research and application prospects in the field of nano biological materials.

To provide wound-healing formulations containing solid birch bark extracts that may be applied to the skin without worsening the patient's condition.SOLUTION: A solid birch bark extract comprises at least about 70 wt.% of betulin, and one or more triterpenes selected from the group consisting of betulinic acid, oleanolic acid, erythrodiol, and lupeol.SELECTED DRAWING: None

The invention discloses betulinic acid used as a livestock feed additive for improving the meat quality of livestock. According to the present invention, the color of pork can be significantly improved, the shearing force and the water loss rate of pork can be reduced, and the meat quality can be improved, such that the grade and the commodity value of pork can be improved, and high economic benefits can be directly provided for the livestock breeding industry.

The invention relates to the technical field of fat reduction, in particular to a degradable fat reduction line and a preparation method thereof. The degradable fat reducing line is prepared from the following raw materials in parts by weight: 1.5 to 2 parts of L-carnitine (PDA) microspheres, 10 to 15 parts of lysozyme-copolymer and 6 to 9 parts of betulinic acid-polymer. The prepared degradable fat reducing line is good in fat reducing effect and high in biocompatibility.

The present application belongs to the technical field of quality control of traditional Chinese medicine, and particularly relates to a quality control method of Ledum palustre L. The quality control method provided by the present application comprises the following processes: S1, identification: thin layer chromatography identification is respectively performed by taking ursolic acid, hyperoside, rutin, aesculetin and aesculin as the control; S2, inspection: the moisture content, total ash content, acid insoluble ash content and alcohol-soluble extract content of the medicinal material are determined; S3, content determination: the total content of volatile oil, three five-ring triterpenes (betulinic acid, oleanolic acid and ursolic acid) and two flavonoid glycosides (hyperoside and preussin) in the medicinal material is determined by using high performance liquid chromatography. The present application combines multi-index component analysis and thin layer chromatography identification, has strong specificity and good reproducibility, can comprehensively and effectively control the quality of Ledum palustre L., and ensures the medicinal effectiveness and safety of Ledum palustre L.

The invention provides a method for increasing the yield of betulinic acid produced from phellinus igniarius, and relates to the technical field of medicinal fungus culture. According to the method for increasing the yield of betulinic acid produced from phellinus igniarius, liquid strains of phellinus igniarius are inoculated into a PGO solid culture medium to be cultured, and the PGO solid culture medium is prepared from 20 g of ginseng powder, 15 ml of water and 2 g of soybean oil. According to the invention, the defects in the prior art are overcome, the phellinus igniarius is effectively promoted to produce betulinic acid by optimizing the formula of the culture medium, and a new direction is provided for the development of a phellinus igniarius culture product with high betulinic acid content.

The invention discloses a betulinic acid derivative as well as a synthesis method and application thereof. According to the betulinic acid derivative, the carboxyl position of betulinic acid C-28 is subjected to structural modification, and four halogenated aniline derivatives are obtained. Wherein the derivatives b, d and e show strong activity on staphylococcus aureus, the derivatives d and e also show strong activity on vancomycin-resistant staphylococcus aureus (VRSA), and the derivative o strongly inhibits streptococcus pneumoniae. Compared with a parent skeleton, the four derivatives show significantly enhanced antibacterial efficacy. Experimental data prove that the derivatives d and e and further derivatives thereof may provide a promising strategy for resisting drug-resistant gram-positive pathogens, and the derivative d can be further developed into a novel therapeutic agent for biofilm-mediated drug-resistant infection.

This invention provides a method for increasing the production of betulinic acid from *Sanghuang* bao's mushroom, relating to the field of medicinal fungal culture technology. The method involves inoculating a liquid strain of *Sanghuang* bao's mushroom into a PGO-added solid culture medium, wherein the PGO solid culture medium formulation is 20g ginseng powder + 15ml water + 2g soybean oil. This invention overcomes the shortcomings of existing technologies by effectively promoting the production of betulinic acid from *Sanghuang* bao's mushroom through optimized culture medium formulation, providing a new direction for the development of *Sanghuang* bao's mushroom culture products with high betulinic acid content.

The present application relates to the technical field of cosmetic raw materials, and particularly relates to a cosmetic composite raw material for removing acne spots and a preparation method thereof. The preparation method of the cosmetic composite raw material for removing acne spots comprises the following steps: preparation of betulinic acid-ostruthin co-assembled nanoparticles, double modification of mannose, preparation of retinol slow-release particles, and preparation of the cosmetic composite raw material. The present application realizes efficient acne spot removal through the synergy of multiple components. The core components, such as betulinic acid, have multiple anti-inflammatory and antibacterial effects, ostruthin inhibits melanin production, glutathione lightens old pigments, retinol and salicylic acid accelerate keratin metabolism, the co-assembly of betulinic acid-ostruthin nanoparticles improves bioavailability, modified mannose / epsilon-polylysine layer-by-layer embedding realizes retinol slow-release synergism, the synergy among the components enhances the effects of spot lightening and anti-inflammation, and the modified mannose can also repair the skin barrier, so that the effect of targeted treatment and barrier repair for removing acne spots is finally realized.

The invention relates to a composition for oral or topical human administration and a preparation method thereof. The present invention relates to pentacyclic triterpenoid compounds wherein said triterpenoid compounds are incorporated into lipid vesicles, preferably cream globules, surrounded by three layers of membranes. The triterpenoid is preferably betulinic acid, and / or betulinol, and / or lupenol, and / or oleanolic acid, and / or ursolic acid, most preferably betulinic acid. The incorporation of the triterpenoid compound into the milk fat globules or lipid vesicles at a high payload of at least 10 to at most 50 mg / ml is preferably accomplished with high energy emulsification techniques, most preferably ultrasound treatment. The composition is present as a liquid emulsion formulation in a preferred embodiment. In another preferred embodiment, the composition is a powder, which can be prepared from a liquid embodiment of the composition by, for example, spray drying or freeze drying techniques. The composition can be preferably used as a medicament, a food supplement or a nutraceuticals for the treatment or prevention of cancer, type 2 diabetes, obesity and cardiovascular diseases.

The invention relates to the technical field of cosmetic raw materials, in particular to a cosmetic composite raw material for removing acne spots and a preparation method of the cosmetic composite raw material. The invention relates to a preparation method of a cosmetic composite raw material for removing acne spots. The preparation method comprises the following steps: preparing betulinic acid-cnidium lactone co-assembled nanoparticles, performing dual modification on mannan, preparing retinol sustained-release particles and preparing the cosmetic composite raw material. According to the invention, efficient acne spot removal is realized through cooperation of multiple components, the core component betulinic acid and the like have multiple anti-inflammatory and antibacterial effects, the cnidium lactone and the like inhibit melanogenesis, glutathione reduces old pigment, retinol and salicylic acid accelerate keratin metabolism, and bioavailability is improved through betulinic acid-cnidium lactone co-assembly nanocrystallization; modified mannan / epsilon-polylysine is embedded layer by layer to realize slow release and synergism of retinol, the components synergistically enhance the spot fading and anti-inflammatory effects, and modified mannan can repair the skin barrier to finally realize the acne spot removing effects of targeted therapy and barrier repair.

The application provides application of white birch acid in calcite inhibition. The molecular structure of the white birch acid contains functional groups such as hydroxyl, carboxyl and carbon six-membered ring, which are hydrophilic groups and solidophilic groups, have strong adsorption on calcite, make the white birch acid easy to be adsorbed with the calcite, and are not easy to be adsorbed with the fluorite ore. The excellent selectivity expands the floatability difference between the calcite and the fluorite ore, so that the selectivity of the fluorite ore flotation method based on the white birch acid is excellent, and the flotation effect is good. Compared with the existing inhibitors such as water glass, the white birch acid has stronger selectivity when used as the fluorite ore flotation inhibitor, and can obtain better flotation effect under the condition of smaller dosage, and the white birch acid is non-toxic and has small environmental pollution.

The invention belongs to the technical field of medicines, and discloses application of SERPINE1 protein or a coding gene thereof as a new target spot for treating hepatitis B virus. The invention reveals that SERPINE1 promotes autophagy flux by being directly combined with PIKfyve protein for the first time, so that HBV replication and HBsAg expression are remarkably inhibited. On the basis, a multi-dimensional target verification platform is established, the fact that the natural compound betulinic acid is a high-affinity agonist (KD = 1.46 mu M) of SERPINE1 is found for the first time, and in-vivo and in-vitro experiments prove that the betulinic acid can effectively reduce the HBsAg and HBV DNA level and is good in safety. In addition, the combination of betulinic acid and entecavir shows a synergistic antiviral effect (CIlt; 1). The invention provides a brand-new target spot and a treatment strategy for realizing functional cure of hepatitis B.

The invention discloses a betulinic acid derivative and application of the betulinic acid derivative in preparation of a medicine for treating and / or preventing novel coronavirus. The betulinic acid derivative provided by the scheme of the invention can effectively block the combination of novel coronavirus spike protein (RBD) and human angiotensin converting enzyme 2 (hACE2), inhibit the novel coronavirus from entering host cells through a cell surface infection way, and provide a valuable reference for developing effective drugs for inhibiting the transmission of the novel coronavirus.

The invention relates to novel application of betulin, in particular to application of betulin in prevention and treatment of cognitive impairment after stroke, and belongs to the field of biological pharmacy. The betulin can obviously improve cognitive impairment and neuronal impairment of post-stroke cognitive impairment, obviously improve cognitive impairment and neuropathological change of post-stroke cognitive impairment, and can play a role in improving post-stroke cognitive impairment. According to the invention, betulinol ester is creatively used for preventing and treating cognitive impairment after stroke; the betulin disclosed by the invention can be used as a medicine for preventing and treating cognitive impairment after stroke, and also can be used as an adjuvant therapy for preventing and treating cognitive impairment after stroke clinically. The traditional Chinese medicine composition has good social benefits and is worthy of clinical popularization and application.

The betulinic acid extraction device comprises a containing box, a stirring frame and a separation barrel, a containing cavity is formed in the containing box, and a containing opening is formed in the upper side of the containing cavity; the stirring frame is arranged in the containing cavity, a vertically-arranged containing cavity is formed in the stirring frame, and the containing cavity corresponds to the containing opening; a plurality of through holes are formed in the surface of the separation barrel and used for separating solid and liquid inside and outside the separation barrel. According to the betulinic acid extraction device, when the stirring frame rotates, liquid on the outer side of the containing cavity is driven to move, so that the liquid in the separation barrel is also driven, solids and the liquid in the separation barrel are fully mixed, and the betulinic acid extraction efficiency is improved; and the other separation barrel filled with the unextracted raw materials is loaded into the accommodating box for next extraction, so that the material changing process is fast, the extracting solution only contains a small amount of fixed powder, the coarse filtering procedure is reduced, and the process difficulty is greatly reduced.

The invention relates to the technical field of functional food, in particular to a composition with the effects of reducing blood sugar and regulating blood fat and application of the composition. The invention provides a composition with the effects of reducing blood sugar and regulating blood fat, the composition comprises a cyclocarya paliurus triterpenoic acid compound and a selenoprotein additive, and the effect is optimal when the mass ratio of ursolic acid to oleanolic acid to betulinic acid to arjiurolic acid in the cyclocarya paliurus triterpenoic acid compound is optimized to be 1: 3.21: 3.37: 0.74 through a response surface experiment. According to the invention, the cyclocarya paliurus triterpene component and the selenium food nutrition enhancer are used at the same time, so that the cyclocarya paliurus selenium food nutrition enhancer can reduce blood sugar, regulate blood fat and increase the antioxidant capacity of the body, also has the functions of inhibiting postprandial blood sugar rise, relieving insulin resistance and protecting liver islet, and can meet the selenium intake of 50-200 micrograms per day of adults recommended by Chinese Nutrition Association; the health-care food can be used as a novel functional food to be applied to prevention and health care of sub-health people with hyperglycemia and hyperlipidemia.

The invention discloses a method for increasing the yield of betulinic acid synthesized by saccharomyces cerevisiae, and belongs to the field of bioengineering and metabolic engineering. According to the invention, a synthetic route of betulinic acid is constructed in saccharomyces cerevisiae. Through overexpression of key genes such as tHMG1, IDI, ERG20, ERG9 and ERG1, construction and optimization of an IUP pathway and adoption of a multi-copy integration and promoter optimization strategy, the expression level of RoCYP01 is enhanced, the RoCYP01 gene is further subjected to rational design and directional modification, the substrate specificity and catalytic efficiency of the RoCYP01 gene are optimized, and the yield of the target product betulinic acid reaches 118.65 mg / L. In addition, by increasing supply of cofactors, conditions in the fermentation process are optimized, and the final yield of betulinic acid is successfully increased to 425.2 mg / L by adopting a continuous feeding culture strategy.

The invention relates to a nano degradation agent based on molecular chaperone autophagy and a preparation method and application thereof. The nano degradation agent comprises PAMAM, and the surface of the PAMAM is coupled with a protein targeting ligand and an Hsc70 protein targeting small molecule; the Hsc70 protein targeting small molecule comprises ursolic acid and / or betulinic acid. The preparation method of the nano degradation agent for targeted degradation of multiple proteins is simple and convenient to operate, the synthesis path is clear, target proteins can be delivered into lysosome in cells through a chaperone-mediated autophagy (CMA) path to be efficiently degraded, and the nano degradation agent can be used for resisting tumors and treating and researching multiple diseases of the tumors.

A COMPOSITION FOR TREATING KERATIN MATERIAL AND METHODS THEREOF The present disclosure provides a composition (A) comprising: a. oleanolic acid, its salts, solvates, or their mixtures thereof; b. ursolic acid, its salts, solvates, or their mixtures thereof; c. betulinic acid, its salts, solvates, or their mixtures thereof; and d. micromeric acid, its salts, solvates, or their mixtures thereof. The present disclosure further provides a rosemary extract and a composition (B). The present disclosure also provides a process for preparing the composition (A), the extract and methods thereof.

The invention provides a method for directionally regulating and controlling the morphology of a ZnO / CuO piezoelectric catalyst based on betulinic acid self-assembly and piezoelectric application of the ZnO / CuO piezoelectric catalyst, belongs to the technical field of environmental functional materials, and aims to solve the technical problem of low heterojunction catalytic activity. According to the method, betulinic acid is taken as a dynamic soft template and a structure-directing agent, reaction conditions are regulated and controlled, the ZnO / CuO piezoelectric catalyst with the multilevel morphology is successfully prepared, the ZnO / CuO piezoelectric catalyst comprises three representative ZnO / CuO piezoelectric catalysts with a shuttle-shaped structure, a star-shaped structure and a sea urchin-shaped structure, and the three structures have the trend of sharp protrusions and strain gradient increase. The multi-stage morphology piezoelectric material prepared by the invention shows excellent piezoelectric catalytic performance under a low-frequency mechanical stirring condition, and the catalytic activity of the multi-stage morphology piezoelectric material shows UPsgt; sPSgt, SPSgt; aPSgt, APSgt; and the RPS changes regularly. Particularly, the catalyst with the sea urchin-shaped structure shows the most excellent catalytic performance on degradation of rhodamine B dye. The invention not only provides a new way for the application of the high-performance piezoelectric catalyst in the field of environmental restoration, but also provides an important reference for the development of a supermolecule mediated catalyst morphology controllable synthesis strategy.

This invention discloses a betulinic acid derivative, its preparation method, and its uses. Using betulinic acid, a natural lupin-type pentacyclic triterpenoid, as the parent compound, a series of betulinic acid derivatives based on C-2 and C-3 position structural modifications were synthesized sequentially via oxidation and Claisen condensation reactions. These betulinic acid derivatives exhibit excellent α-glucosidase inhibitory activity. Their chemical structures differ significantly from existing clinical drugs, and their parent compounds are derived from natural products. This invention holds promise for overcoming the gastrointestinal adverse reactions and other drawbacks of traditional α-glucosidase inhibitors, providing new drug candidates for diabetes treatment. Furthermore, the raw materials for this invention are relatively widely available, facilitating subsequent scale-up production and process optimization, and possessing the potential for further development into clinical drug candidates.