49 results about "Betulinic acid" patented technology

The invention belongs to the technical field of food microorganisms, and relates to lactobacillus plantarum and application thereof in preparation of products for relieving insomnia. The preservation number of the lactobacillus plantarum is GDMCC No: 65061. The lactobacillus plantarum can be applied to efficient fermentation of spina date seed juice, the content of GABA, polypeptide, total phenols and total flavonoids in the spina date seed juice is increased, and the content of spinosin, 6 ''-feruloyl spinosin, jujuboside A, jujuboside B and betulinic acid is increased; the reduction of whole brain coefficient and the increase of liver coefficient caused by long-term insomnia are relieved, the bad condition caused by long-term insomnia in a hippocampus DG region in the brain of the mouse is improved, the sleep time of the mouse is prolonged, and the insomnia symptom of the mouse is relieved; the content of inhibitory neurotransmitters 5-hydroxytryptamine, melatonin and gamma-aminobutyric acid in the hypothalamus of the mouse is increased, the content of excitatory neurotransmitter glutamic acid is reduced, and the reduction of organism immunity and oxidative stress of brain tissues caused by insomnia are relieved.

The invention belongs to the field of biosynthesis, and particularly relates to a saccharomyces cerevisiae engineering bacterium for producing glycosyl donor UDP-arabinose as well as a construction method and application of the saccharomyces cerevisiae engineering bacterium. According to the invention, UDP-Glc dehydrogenase, UDP-GlcA decarboxylase, UDP-Xyl-4-epimerase or UDP-Glc-epimerase are sequentially expressed in WAT11, so that a synthetic route of UDP-Ara is introduced into the saccharomyces cerevisiae for the first time; de novo synthesis of Ara-oleanolic acid is realized by introducing a synthetic route of arabinosyl transferase and oleanolic acid; the yeast containing the UDP-Ara synthetic pathway and the arabinosyl transferase gene can also utilize betulinic acid to generate Ara-betulinic acid. The invention solves the problem of yeast total synthesis of the arabinosyl donor, provides a new biotechnology platform for production of natural glycoside compounds, and has important theoretical value and wide application prospect.

The invention relates to betulinic acid type saponin derivatives as well as a preparation method and application thereof, and belongs to the technical field of biological medicines. The structural general formula of the betulinic acid type saponin derivative is # imgabs0, R1 is selected from hydroxyl or-O-G, and G is monosaccharide; r2 is selected from dopamine, 5-aminovaleric acid, 4-aminobutyric acid or 3-aminopropionic acid and the like and salts thereof. The betulinic acid type saponin derivative does not show obvious cytotoxicity to THP-1 macrophages, and can obviously reduce the release of IL-6 and IL-1beta in the THP-1 macrophages induced by LPS (lipopolysaccharide). Compared with betulinic acid and positive control medicine mesalazine, the pharmaceutical composition has better anti-inflammatory activity, has the treatment effect of improving diarrhea and hemafecia of mice with colitis remarkably superior to those of betulinic acid and positive control medicine mesalazine, has the treatment effect of dermatitis superior to that of positive control medicine dexamethasone, and does not have obvious toxic or side effects such as weight loss and immunosuppression. Therefore, the betulinic acid type saponin derivative has good in-vivo and in-vitro safety and druggability.

The invention provides zein-chondroitin sulfate composite nanoparticles loaded with betulinic acid as well as a preparation method and application of the zein-chondroitin sulfate composite nanoparticles, and belongs to the technical field of medicines. The betulinic acid-loaded zein-chondroitin sulfate composite nanoparticles are prepared from betulinic acid, zein and chondroitin sulfate by adopting an anti-solvent method, and the zein and the chondroitin sulfate are compounded through protein-polysaccharide, so that the betulinic acid-loaded zein-chondroitin sulfate composite nanoparticles are prepared. The betulinic acid is embedded in particles formed by protein-polysaccharide in an amorphous state, the prepared composite nanoparticles are stable in structure and uniform in distribution, the particle size ranges from 160 nm to 190 nm, the encapsulation efficiency reaches 94.05%, the slow release characteristic and the water dispersibility are excellent, and the antitumor activity of the betulinic acid can be improved.

The invention discloses betulinic acid derivatives containing amide and secondary amine structures and a preparation method and application of the betulinic acid derivatives, and belongs to the technical field of medicines.The betulinic acid derivatives are obtained by conducting structural modification on betulinic acid, and it is proved through an in-vitro thioflavin (Th) T fluorescence experiment that the betulinic acid derivatives have a good application prospect. The compounds can effectively inhibit aggregation of beta-amyloid protein (A beta) 42, can be used as candidate drugs for treating Alzheimer's disease, and have good application prospects in clinic.

The present invention discloses the use of betulinic acid in the preparation of an anti-Tubulic Mosaic Virus preparation, relating to the technical field of agricultural plant protection. The present invention used 10 mg / L of betulinic acid to continuously root-irrigate Nicotiana benthamiana plants for 5 days, and found that betulinic acid treatment significantly inhibited TuMV infection and reduced viral accumulation levels compared to the control group. Betulinic acid, as a plant-derived substance, has its own degradation pathway and has the advantages of being safe, economical, and pollution-free, meeting the requirements of sustainable agricultural development and green environmental protection. The present invention makes it possible to use betulinic acid for the prevention and treatment of plant viruses, providing a new approach for the prevention and treatment of plant viruses.

The invention discloses application of betulinic acid 28-O-beta-D-glucoside in medicines, and particularly relates to application of betulinic acid 28-O-beta-D-glucoside in preparation of medicines for treating or preventing inflammatory bowel diseases. The invention discloses application of betulinic acid 28-O-beta-D-glucoside (BA-6) in prevention and treatment of inflammatory bowel diseases for the first time aiming at the problems that existing medicines for treating the inflammatory bowel diseases (IBD) are limited in curative effect, slow in effect taking, multiple in side effects, high in long-term use risk, large in individual difference, high in treatment cost, likely to cause immunoreactions and the like. The technical progress of obviously improving the acute colitis symptom is realized. Results of a cytotoxicity experiment and an acute toxicity experiment show that the betulinic acid 28-O-beta-D-glucoside (BA-6) does not have obvious biotoxicity on a cellular level or an animal level.

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

A device (100) for identifying betulinic acid and trimethoxyellagic acid as antidiabetic compounds in purified extract from the stem bark of Anogeissus leiocarpus, wherein the device (100) comprises: a collection unit (102) for collecting stem bark samples of Anogeissus leiocarpus; a processing unit (104) connected to the collection unit (102) for pulverizing the collected samples, wherein the pulverized samples are subjected to cold maceration with 90-100% v / v ethanol to extract ethanolic extracts; a segmentation unit (106) connected to the processing unit (104) for splitting the ethanolic extract using ethyl acetate and n-hexane solvents; a column chromatography unit (108) connected to the segmentation unit (106) for triggering precipitation by adding cold acetone to the ethanolic extract; A solution and adsorption unit (110) comprises a container (110a) connected to the column chromatography unit (108) for dissolving the precipitate with a mixture of dichloromethane (DCM) and methanol, and a glass column (110b) for adsorbing the dissolved precipitate; an evaporation unit (112) connected to the solution and adsorption unit (110) to evaporate the solvent mixture and obtain a free-flowing powder from the dissolved precipitate; and a plurality of evaluation units (114) connected to the evaporation unit (112) for identifying properties of the stem bark of Anogeissus leiocarpus.

The invention discloses a betulinic acid derivative and application of the betulinic acid derivative in preparation of anti-stress and anti-aging drugs, and belongs to the field of medicines.The betulinic acid derivative has the structural formula shown in the formula I. # imgabs0 # R1 is H or acyl; x is O or NH; # imgabs 1 # represents a double bond or a single bond; r2 is H, C1-C5 straight-chain alkyl, C3-C6 mono-cycloalkyl, polycycloalkyl or substituted / unsubstituted six-membered heterocyclic radical containing one nitrogen or oxygen atom. The betulinic acid derivative can improve the activity of cell telomerase, prolong the telomere length, practically prolong the life of drosophila melanogaster and play a role in delaying senescence.

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.

The present invention discloses a preparation method and application of betulinic acid silicon phthalocyanine. The method uses betulinic acid as a ligand to synthesize a betulinic acid axially substituted silicon phthalocyanine complex. The method comprises the following steps: (1) reflux filtering white dichlorosilicon phthalocyanine, potassium carbonate and betulinic acid in a toluene solution; (2) purifying the crude product with an eluent on a silica gel column and drying it to obtain betulinic acid silicon phthalocyanine. The Bai‑SiPc prepared by this method has good biocompatibility and strong phototoxicity, and is a type of photosensitizer with excellent photodynamic therapy performance.

The present invention discloses a betulinic acid derivative prepared from active ingredients of birch, and its preparation method and application. The betulinic acid derivative has a structure shown in formula (I): #imgabs0# wherein R is selected from substituted or unsubstituted C 6～12 Aryl, substituted or unsubstituted C 5～12 The present invention uses the betulic acid structure as the parent core to design and synthesize a series of betulic acid derivatives, which exhibit high α-glucosidase inhibitory activity and can be used as α-glucosidase inhibitors to treat or prevent diabetes.

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 invention provides a culture medium for inducing type C1 iNKT cells, a culture method thereof and applications thereof, relating to the technical field of cell culture. The culture medium comprises a DC culture medium and an iNKT culture medium. The DC culture medium comprises GM-CSF, IL-4, TNF-α, LPS, 7DW8-5 and autologous plasma. The iNKT culture medium comprises IL-2, IL-7, IL-15, IL-21, 7DW8-5, lupeol, betulinic acid, resveratrol and autologous plasma. Meanwhile, a culture method corresponding to the culture medium is also provided. The type C1 iNKT cells obtained after being cultured with the culture medium of the present invention for 14 days can secrete a relatively high level of IFN-γ without the stimulation of target cells, and the proportion of type C1 iNKT cells in CD3+ T cells increases significantly. Such a culture medium and a culture method can be used in the fields of inducing the growth and expansion of type C1 iNKT cells, exosome extraction, etc., so as to efficiently obtain target cells and target factors.

The invention discloses a pharmaceutical composition for improving oral bioavailability of isepamicin sulfate and a preparation method of the pharmaceutical composition, and belongs to the technical field of pharmaceutical preparations. The pharmaceutical composition oil for improving the oral bioavailability of the isepamicin is prepared from the following raw materials: betulinic acid, polyethylene glycol, the isepamicin and an emulsifier. According to the invention, a synergistic solubilizing system is constructed by combining betulinic acid and polyethylene glycol (PEG) for use, so that the dissolution rate of the medicine and the intestinal absorption efficiency are remarkably improved by adopting the strategy of the synergistic solubilizing system disclosed by the invention. Experiments show that the composition can improve the oral bioavailability of isepamicin to 25%, and the method has the advantages that the bioavailability of the medicine can be greatly improved, the process flow is simple and convenient, the product is excellent in stability, and a solid foundation is laid for further clinical application of the composition.

The present invention relates to the field of drug treatment for chronic myeloid leukemia (CML), and specifically to the application of birch sap combined with imatinib mesylate (Gleevec) in the treatment of chronic myeloid leukemia. Birch sap contains rich birch polysaccharides and pentacyclic triterpenoids such as betulinic acid and betulin, which can effectively induce apoptosis of leukemia drug-resistant cells, enhance the sensitivity of drug-resistant cells to drugs, reverse the secondary drug resistance generated by imatinib mesylate during treatment, and reduce the levels of arginine vasopressin (AVP) and lactic acid in the blood, increase the content of human liver glycogen, and effectively alleviate the common treatment side effects such as water retention and systemic edema, physical decline, fatigue, nausea, and vomiting caused by taking imatinib mesylate. Compared with the use of drugs alone, the combined use of birch sap can effectively enhance the therapeutic effect of imatinib mesylate on chronic myeloid leukemia and reduce drug side effects.

The present invention relates to a betulinic acid saponin derivative, a preparation method and an application thereof, and belongs to the field of biomedicine technology. The betulinic acid saponin derivative of the present invention has the general structural formula: 1 Selected from hydroxyl or -O-G, G is a monosaccharide; R 2 Selected from dopamine, 5-aminovaleric acid, 4-aminobutyric acid or 3-aminopropionic acid and their salts. The betulic acid saponin derivative did not show obvious cytotoxicity to THP-1 macrophages, and could significantly reduce the release of IL-6 and IL-1β in LPS-induced THP-1 macrophages. It also has better anti-inflammatory activity, and its therapeutic effect on improving diarrhea and bloody stools in colitis mice is significantly better than that of betulic acid and the positive control drug mesalazine, while its therapeutic effect on dermatitis is better than that of the positive control drug dexamethasone, and there are no obvious toxic side effects such as weight loss and immunosuppression. This shows that the betulic acid saponin derivative has good in vitro and in vivo safety and drugability.

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 discloses a betulinic acid hydroxamic acid derivative or a pharmaceutical salt thereof. The structure of the betulinic acid hydroxamic acid derivative is selected from one of the following structures: # imgabs0 #. The invention also provides an application of the betulinic acid hydroxamic acid derivative or the pharmaceutical salt thereof in preparation of a CD73 small-molecule inhibitor. The invention provides a novel betulinic acid hydroximic acid derivative which has good CD73 inhibitory activity, and part of compounds show activity superior to that of betulinic acid, so that the betulinic acid hydroximic acid derivative can be used as a CD73 inhibitor antitumor drug.

The invention discloses a synthesis method of 3-O-carbohydrate chain betulinic acid aglycone glycoside and 28-COO-carbohydrate chain aglycone glycoside, and belongs to the field of carbohydrate chemistry, and the synthesis method comprises the following steps: # imgabs0 # R1, R2, R3, R6 and R7 are respectively and independently selected from alkyl, aryl, silyl or acyl; r5 is selected from alkanoyl or aroyl; a compound 1 is used as a raw material and is subjected to glycosylation reaction to obtain a compound 7, and the compound 7 is subjected to glycosylation reaction and deprotection reaction to obtain compounds I and II.

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.