35 results about "Betulinic acid" patented technology

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 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

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 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 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 present invention discloses a method for constructing a characteristic spectrum and a reference spectrum of a persimmon calyx, and their application. The method comprises the following steps: taking persimmon calyx medicinal material powder, adding an extraction solvent, extracting after quantitative determination, cooling, replenishing the lost weight with the same solvent, shaking, filtering, and collecting a subsequent filtrate to obtain a test solution; and injecting the test solution and the reference solution into an ultra-high performance liquid chromatograph to obtain a characteristic spectrum. The characteristic spectrum, with betulinic acid, oleanolic acid, and ursolic acid as characteristic components, establishes seven characteristic peaks through an efficient detection method, and can relatively comprehensively reflect information on triterpenoid components in the persimmon calyx. The method is suitable for rapid quality control of persimmon calyx medicinal materials, decoction pieces, and intermediate and finished preparations containing persimmon calyx medicinal materials or decoction pieces. The method is efficient, easy to operate, and suitable for quality monitoring in continuous production.

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.

Provided, according to one embodiment, is a plant-derived extract composition capable of increasing the expression of transglutaminase (TGM-1) and loricrin (LOR).　The present disclosure relates to, according to one embodiment, a plant-derived extract composition that comprises rosmarinic acid and has a mass ratio of betulinic acid and rosmarinic acid (betulinic acid / rosmarinic acid) of 0.25 or less.

The invention belongs to the technical field of biology, and particularly relates to application of triple active ingredients in birch juice in relieving hyperuricemia. According to the invention, firstly, the influence of birch juice on the weight, blood uric acid, blood urea nitrogen, serum creatinine and visceral organ coefficient of a hyperuricemia mouse is evaluated through animal experiments; in order to reveal the potential mechanism of the active ingredients of the birch juice for relieving the hyperuricemia, the invention further explores the ability of three main active ingredients of betulin, betulinic acid and kaempferol in the birch juice for regulating and controlling the high-grade conformation of nucleic acid in a hyperuricemia-related gene promoter region; the molecular mechanism of the triple active components in the birch juice for relieving hyperuricemia is speculated and explained from the gene level. In conclusion, the invention provides a brand-new theoretical basis and mechanism elaboration of a gene level for relieving metabolic diseases by natural functional small molecules.

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.