59 results about "Sapogenin" patented technology

The invention belongs to the technical field of medicinal chemistry, and particularly relates to a dammarane sapogenin-isatin derivative and application thereof in anti-tumor treatment. The dammarane sapogenin-isatin conjugate is constructed by taking dammarane sapogenin as a mother nucleus, deriving the dammarane sapogenin and chloroacetic acid and then introducing an indolone structural unit, and R1, R2 and R3 are as described in the claims and the specification. According to the invention, isatin fragments and ginsenoside are coupled for the first time, the anti-tumor activity of the compounds is systematically evaluated, and the action mechanism research of the compounds in colorectal cancer and other tumors is further developed. Results show that the obtained compound has relatively good anti-tumor efficacy, tumor cell selectivity, relatively low toxicity and relatively high bioavailability, and shows good patent medicine potential and wide market prospects.

The invention relates to the technical field of agricultural product processing, in particular to a preparation method and application of high-activity medicinal and edible lily tea drink dried flowers. The method solves the problem that active ingredients such as flavonoids, aromatics, steroid saponins and alkaloids are easy to lose in the existing dried lily preparation. In the prepared dried medical lily flowers, the relative concentration of honeysuckle glycoside is larger than or equal to 1460 micrograms / g, the relative concentration of benzene and substituted derivatives thereof is larger than or equal to 960 micrograms / g, the relative concentration of steroid sapogenin-O-glucose is larger than or equal to 2120 micrograms / g, the relative concentration of choline is larger than or equal to 699 micrograms / g, the medical value and edible quality of the dried medical lily flowers are remarkably improved, and the method is suitable for large-scale production.

The invention provides an application of hederagenin in preparation of a medicine used as an SKP2 degradation agent, and particularly provides an application of hederagenin in preparation of a medicine used as an SKP2 degradation agent. The invention also provides a PROTAC compound, which comprises a target protein POI ligand, an E3 ubiquitin ligase ligand and a linking chain Linker, the general formula of the ligand-Linker-E3 ligase ligand is as follows: a POI ligand-Linker-E3 ligase ligand. The invention also provides a preparation method and application of the PROTAC compound. The PROTAC design based on HED improves the tumor tissue targeting property, and shows low toxicity in an in-vivo experiment. The invention provides a novel SKP2 (SKP2) degradation agent. The degradation agent is expected to be capable of efficiently inducing ubiquitination degradation of SKP2 protein, and a treatment strategy with higher potential and clinical application prospect is provided for overcoming the limitation of the prior art by enhancing the specific killing capability on SKP2 high-expression tumor cells and verifying the remarkable tumor inhibition effect and good safety of the degradation agent in an animal model.

This invention belongs to the field of biomedical technology, specifically relating to a rapid purification method for umbilical cord MSC exosomes and their application in the preparation of drugs for treating COPD. This invention discloses a method for rapidly purifying umbilical cord mesenchymal stromal cell (MSC) exosomes and a pharmaceutical composition comprising umbilical cord MSC exosomes and yamosaponin. In this pharmaceutical composition, the umbilical cord MSC exosomes and yamosaponin synergistically enhance the dynamic compliance of COPD rats, reduce airway resistance, decrease pulmonary inflammation, and repair pulmonary dysfunction. This invention provides a new technical solution for the preparation of drugs for treating or improving COPD.

Disclosed herein are compounds and methods of use thereof effective for the treatment of neurodegenerative diseases such as amyotrophic lateral sclerosis (ALS), a disease that affects nerve cells in the brain and spinal cord, eventually causing loss of muscle strength. The compounds of the disclosure include, cutamesine, a synthetic sigma receptor agonist selective for the 81 receptor, and also a chaperone protein of the central nervous system that plays a key role in the modulation of calcium ions and apoptosis, as well as a sapogenin, such as smilagenin, a non-peptide neurotrophic factor that aids in the reversal of free radical neurotoxicity.

This invention discloses a low-allergen compound oral liquid for middle-aged and elderly people that protects the liver, stabilizes blood pressure, blood sugar, and blood lipids, combats aging, aids sleep, and prevents Alzheimer's disease. It belongs to the field of food and medicine homology health food technology. The invention uses kudzu root extract, Japanese raisin tree fruit extract, mulberry leaf extract, jujube seed saponins, Acer truncatum seed oil (nervonic acid), blueberry anthocyanins, bitter melon small molecule peptides, wolfberry polysaccharides, γ-aminobutyric acid, and chrysanthemum flavonoids as core active ingredients, refined with a prebiotic system. This invention achieves comprehensive conditioning effects for middle-aged and elderly people through the synergistic action of five pathways: liver protection and metabolism, vascular regulation, anti-oxidation and anti-aging, nerve calming, and brain nerve repair. It simultaneously nourishes and protects the liver, stabilizes blood pressure, blood sugar, and blood lipids, delays aging, improves intractable insomnia, enhances memory, slows brain atrophy, and prevents Alzheimer's disease. This formula strictly avoids eight common allergens, is pure and mild, and contains no irritating additives, making it suitable for long-term use by middle-aged and elderly people with weak constitutions. This product is an oral liquid formulation, with small molecule extraction, strong permeability, rapid absorption, low gastrointestinal burden, stable production process, and high safety. It has extremely high clinical promotion value and industrialization prospects.

The invention relates to a method for synthesizing (R)-3-methylheptanoic acid. According to the method, the application range of steroid sapogenin degradation waste is further expanded. According to the method disclosed by the invention, the (R)-3-methyl-heptanoic acid can be conveniently obtained by taking the (R)-4-methyl-gamma-butyric acid lactone obtained by degrading steroid sapogenin as a raw material. According to the method provided by the invention, the use of highly toxic and controlled reagents is avoided, high-risk reactions such as hydrogenation in the prior art are avoided, and the method is mild in reaction condition and low in synthesis cost. Meanwhile, the utilization rate of steroid sapogenin resources is increased, and waste generated in the utilization process of the steroid sapogenin resources is reduced.

The invention relates to a saponin metabolic pathway, in particular to paris polyphylla glycosyl transferase PpUGT73YD1 and application of the paris polyphylla glycosyl transferase PpUGT73YD1 in synthesis of steroid saponin. The amino acid sequence of the glycosyl transferase is shown as SEQ ID NO: 2. The invention also provides a gene for coding the glycosyl transferase, an expression box, a vector or host bacteria containing the gene, and application of the glycosyl transferase in a glycosyl transfer reaction. The glycosyl transferase can catalyze the reaction of polyphyllin V and UDP-rhamnose to generate polyphyllin III, or catalyze the reaction of polyphyllin VI and UDP-rhamnose to generate pennogenin-3-O-rhamnosyl-(1-> 2)-[rhamnosyl-(1-> 4)]-glucoside, and lays a foundation for the biosynthesis and pharmacological research and development of polyphyllin.

The invention discloses a Thomasclavia ramosa CMLF06 strain, saponin converting enzyme and application of the Thomasclavia ramosa CMLF06 strain and the saponin converting enzyme, the Thomasclavia ramosa CMLF06 strain is preserved in China General Microbiological Culture Collection Center, the preservation address is No.3, No.1 yard, Beichen West Road, Chaoyang District, Beijing, the preservation date is January 25, 2024, and the preservation number is CGMCC NO. 41093. The invention further discloses a method for preparing the saponin converting enzyme. The Thhomasclavia ramosa CMLF06 strain can convert ginsenoside to generate rare ginsenoside and sapogenin, the saponin converting enzyme GE001065 can convert ginsenoside and notoginsenoside to generate various rare ginsenoside in the presence of ethanol, the activity and stability of the enzyme GE001065 in an ethanol solution and a methanol solution are remarkably improved, the enzyme GE001065 shows an activation effect in various alcohols, and the enzyme GE001065 can be used for preparing the rare ginsenoside. The method can be used in the fields of medicine and functional food.

The invention relates to the technical field of medical cosmetology, and discloses a sustained-release drug-loaded microsphere and a preparation process thereof.Epoxy groups of epoxy polyester react with terminal carboxyl groups of polylactic acid to obtain comb-type polylactic acid with polyester as a main chain and polylactic acid molecular chains as side chains, the comb-type polylactic acid has a three-dimensional comb-type network structure, and the sustained-release drug-loaded microsphere is prepared through a single emulsion solvent evaporation method. The prepared microspheres have a large space network, coating and loading required by a target are effectively achieved, a main chain contains a large number of hydroxyl groups, the hydroxyl groups and substances such as sapogenin, polysaccharide and polyphenol in saponin and essential oil can form acting force such as hydrogen bonds, and the adsorption performance and the drug loading capacity of the microspheres on a target drug are further improved. The side chain of the microsphere is degradable polylactic acid, and the main chain contains a large number of degradable ester groups and a large number of hydroxyl groups, so that the water absorption of the microsphere can be improved, the hydrolysis of the microsphere is accelerated, and the microsphere has higher biological decomposition rate and degradation performance and is green and environment-friendly.

The invention discloses an application of sanguisorba officinalis sapogenin in preparation of a medicine for treating gout. Compared with the prior art, it is found for the first time that sanguisorba sapogenin can treat gout, especially acute gouty arthritis. Animal research proves that the sanguisorba sapogenin can remarkably relieve joint swelling and tissue damage caused by acute gouty arthritis by inhibiting release of inflammatory factors such as IL-1beta and TNF-alpha. Meanwhile, the sanguisorba sapogenin can also remarkably reduce the level of serum uric acid, and also has a certain treatment effect on gout in a remission stage and a chronic stage. Therefore, the sanguisorba officinalis sapogenin can be used for treating gout and has the potential and prospect of being prepared into the anti-gout medicine.

The application belongs to the technical field of organic synthesis, and particularly relates to a benzimidazole alkyl bromide salt-anemarrhena saponin aglycone derivative, a preparation method and application thereof. The benzimidazole alkyl bromide salt-anemarrhena saponin aglycone derivative provided by the application has a structure shown in formula 1 or formula 2. The application combines an anemarrhena saponin aglycone skeleton and a benzimidazole skeleton, and the obtained benzimidazole alkyl bromide salt-anemarrhena saponin aglycone derivative with the structure shown in formula 1 or formula 2 has significant antitumor activity. The antitumor growth inhibition activity of the benzimidazole alkyl bromide salt-anemarrhena saponin aglycone derivative provided by the application is better than that of cisplatin (DDP), an anticancer drug.

The invention discloses a novel application of hederagenin in preparation of a medicine for maintaining the dryness of alveolar II epithelial cells, the hederagenin is definitely used for preparing the medicine for maintaining the dryness of the alveolar II epithelial cells for the first time, and the repairing effect of the hederagenin on ATII dry damage is verified through in-vivo and in-vitro experiments. A brand new treatment strategy is provided for lung diseases such as acute lung injury, pulmonary fibrosis and the like which are characterized by ATII dry failure, the technical blank of intervention of natural active ingredients in ATII dry is filled up, a new way which is efficient, low in cost and easy to obtain is provided for ATII dry maintenance, the concentration of a medicine prepared from the natural active ingredients is screened, and the clinical application prospect is wide. An important theoretical basis is provided for further medication and medicine preparation, meanwhile, the pharmacological application range of the hederagenin is expanded, and a new target and a new strategy are provided for subsequent intervention treatment of lung diseases such as acute lung injury and pulmonary fibrosis needing injury repair.

The composition and / or combinations includes diosgenin and at least one other agent selected from vitamin D and α-lactalbumin and its use in the regularization of the menstrual cycle and in the reduction of ovarian cysts, in particular in women affected with polycystic ovarian syndrome (PCOS) phenotype D.

The application relates to the technical field of biological medicine, and discloses a preparation method of a hederosapogenin STING channel inhibitor, which comprises the following steps: taking appropriate hederosapogenin and aromatic compounds, adding N,N-dimethylformamide as a reaction solvent, and adding appropriate K2CO3; stirring under a heating reflux state for a certain time, monitoring the reaction process through thin layer chromatography until the reaction is completed; after the reaction is completed, the N,N-dimethylformamide is evaporated under reduced pressure, the obtained residue is dissolved in dichloromethane, and the residue is extracted and washed with deionized water and saturated brine in sequence; the organic layer is collected, dried with anhydrous sodium sulfate, filtered, evaporated under reduced pressure, and a crude product is obtained; the crude product is separated and purified through a silica gel column chromatography, and a target compound, namely a STING channel inhibitor derivative, is obtained. The hederosapogenin is chemically modified to synthesize a derivative with high STING channel activity, which is used for treating immune and inflammation related diseases.

The invention provides a medicine containing hederagenin and application of the medicine in regulating and controlling lysozyme to block gastritis-cancer transformation, the interaction relation between hederagenin and a key target spot is preliminarily determined by combining the key target spot LYZ of gastric inflammation-cancer screened by early-stage bioinformatics and applying a molecular docking technology, and then verification is performed by applying in-vivo and in-vitro experiments. Results of research discover that the common component hederagenin of astragalus membranaceus-curcuma zedoary and the key target LYZ of the gastric inflammation-cancer have an interaction relationship, and in-vivo and in-vitro experiments prove that the hederagenin can regulate and control the key target LYZ of the gastric inflammation-cancer, so that a new foundation is laid for further screening of core medicine components and optimization of traditional Chinese medicine formulas. The research and development of effective drugs for preventing and treating early gastric cancer have important significance.

The invention relates to the technical field of platycodon grandiflorum preparation, in particular to a black platycodon grandiflorum composite concentrated solution as well as a preparation method and application thereof. The preparation method comprises the following steps: steaming fresh platycodon grandiflorum, drying after steaming, and steaming and drying for 9 times in total to obtain black platycodon grandiflorum; the preparation method comprises the following steps: mixing black platycodon grandiflorum with water, carrying out water extraction, and concentrating the extract liquid after water extraction to obtain the black platycodon grandiflorum extract. Fresh platycodon grandiflorum is steamed and dried for nine times, part of saponin is hydrolyzed and converted into secondary sapogenin which is more easily absorbed by a human body, meanwhile, effective components are highly concentrated, the black platycodon grandiflorum with an excellent effect is prepared, the black platycodon grandiflorum is prepared into the black platycodon grandiflorum concentrated solution, the taste of the black platycodon grandiflorum can be improved, and the black platycodon grandiflorum has the effects of improving the immunity of the human body and improving the immunity of the human body. In-vivo and in-vitro experiments show that the black platycodon grandiflorum concentrated solution provided by the invention has the effects of improving gastric ulcer and protecting gastric mucosa.

The invention relates to the technical field of traditional Chinese medicine analysis, in particular to a construction method of a characteristic spectrum of a traditional Chinese medicine compound preparation for treating senile dementia. The method is creatively characterized in that detection of characteristic peaks is realized through extraction, preparation and purification of an extract and specific gradient selection under a specific mobile phase condition. According to the method, seven chemical components in the traditional Chinese medicine compound preparation can be analyzed, seven characteristic peaks including epimedin C, ginsenoside Rd, pachymic acid, dehydrotumuloic acid, alpha-asarone, polygala mountain ketone III and tenuigenin are identified, verification research on specificity, precision, repeatability and stability is carried out on the method, and it is proved that the method is accurate and reliable. The technical means is used as a method for overall evaluation of the traditional Chinese medicine compound preparation, and a quality control system of the traditional Chinese medicine compound preparation is comprehensively improved.

The invention discloses a hederagenin C-2 heterocyclic oxime ester derivative as well as a preparation method and application thereof, and belongs to the technical field of organic chemistry. The structure of the derivative is shown in the specification, and in the formula, R represents furan, thiazole, oxazole, thiophene or 2, 3-dimethoxybenzene. Pharmacological tests show that the hederagenin C-2 heterocyclic oxime ester derivatives (H3W-FN, H3W-SZ, H3W-EZ, H3W-SF and H3W-OB) prepared by the invention all have MDR reversal activity, and part of the hederagenin C-2 heterocyclic oxime ester derivatives (H3W-SZ) have better MDR reversal activity than verapamil, so that the sensitivity (plt; 0.01), is a P-gp inhibitor with more excellent MDR reverse activity, and can be combined with common antitumor drugs to exert good antitumor activity.

The invention discloses an application of geitogenin in prevention or treatment of neurodegenerative diseases, in-vitro cell experiments and animal model researches prove that the geitogenin can significantly down-regulate the expression level of HSD17B10 or inhibit the enzymatic activity of HSD17B10; therefore, the nerve cell survival is improved, the neuroinflammation is reduced, the epileptic seizure frequency is reduced, and the cognitive function is improved. Furthermore, it is proved that the Gemtogenin can significantly reduce the HSD17B10 protein level in vitro and in vivo, improve cognitive impairment and reduce the epileptic seizure frequency, and the Gemtogenin has good safety and application prospects. According to the invention, the new application of the geitogenin in preparing the medicine for preventing or treating the neurodegenerative diseases and the epilepsy is provided for the first time, and a new way and means are provided for treating the neurodegenerative diseases and the epilepsy.

Described in this application are host cells comprising heterologous polynucleotides encoding enzymes for producing triterpene glycosides (e.g., prosapogenin) and precursors or derivatives thereof. Methods of culturing the host cells are also included herein. Also described are methods of producing a product of interest, such as triterpene glycosides (e.g., prosapogenin) and precursors or derivatives thereof, using the host cells described herein.

The invention provides application of a composition containing oridonin and sasapogenin to preparation of an anti-tumor drug. The composition comprises oridonin and sasapogenin. In-vitro experiments prove that the anti-tumor effect of the combined use of the oridonin and the sasapogenin is obviously superior to that of a single component, the survival rate of non-small cell lung cancer cells can be obviously reduced by the combined use of the oridonin and the sasapogenin, and the q value calculated by a Kinghuang's formula can prove that when the molar ratio of the oridonin to the sasapogenin is 1: (0.1-0.3), the survival rate of the non-small cell lung cancer cells can be obviously reduced. The two compounds have an excellent synergistic anti-tumor effect.

The present invention belongs to the technical field of pharmaceuticals. Disclosed are a pharmaceutical composition for treating a TDP-43 proteinopathy, and a preparation method therefor and the use thereof. The pharmaceutical composition comprises at least one of each of compounds of class A and compounds of class B. The compounds of class A comprise at least one of sodium aescinate, a sodium aescinate derivative, hederagenin or a hederagenin derivative; and the compounds of class B comprise at least one of dehydrated icaritin, a dehydrated icaritin derivative, diosmin or a diosmin derivative. The pharmaceutical composition has a good therapeutic effect on the TDP-43 proteinopathy.

The invention discloses a method for determining the content of sapindus saponin by an acid hydrolysis gravimetric method. The method comprises the following steps: firstly, carrying out column chromatography purification on a sample by using AB-8 macroporous resin; hydrolyzing and purifying the sample by using sulfuric acid with a certain concentration at 121 DEG C, and carrying out suction filtration to obtain a precipitate (sapogenin); weighing the precipitate (sapogenin), and calculating the saponin content coefficient of the sapindus according to a relational expression between the precipitate (sapogenin) and the saponin content; and determining the content of the sapindus saponin according to the content coefficient of the sapindus saponin and the content of the crude saponin hydrolysis precipitate. On the basis of acid hydrolysis of the saponin, a relation coefficient between sapogenin and the saponin content of the sapindus saponin under the specified sulfuric acid concentration is provided, and the accurate content (+ / -5%) of the saponin in a purified sample is simply and rapidly measured. The invention provides a novel method for rapidly determining the content of natural soapberry saponin.

The application relates to application of a smilagenin compound in preparation of a medicine for treating diseases caused by abnormal mitochondrion function, characterized in that the structural formula of the compound is shown in general formula (I). Through activity test of the smilagenin compound in related in-vivo and in-vitro models, it is found that many derivative compounds have superior cell protection activity, especially for various brain neuron cells related to mitochondrion, and the compounds have unexpected protection activity and very excellent blood-brain permeability, so that the compounds have potential wide application and great value for treating various diseases caused by abnormal mitochondrion function, make up for the deficiency of the smilagenin compound in the prior art, and have important scientific and commercial application value.

The invention provides UDP-glucose transferase for catalyzing glycosylation at C2'site of aescin, a gene, a primer group and application, and belongs to the technical field of aescin. The method is based on aesculus chinensis genome and transcriptome data analysis; according to the present invention, the UGT gene for catalyzing the C2'site of the protoaescinogenin-3-O-beta-D-glucopyranuronide is excavated, and the tobacco transient expression system is utilized to verify that the AcUGT94AK1, the AcUGT94AK3 and the AcUGT94AK6 can catalyze the protoaescinogenin-3-O-beta-D-glucopyranuronide to form the protoaescinogenin-3-O-beta-D-glucopyranuronide-(1-> 2)-beta-D-glucoside, such that the UGT gene can be used for catalyzing the C2 'site of the protoaescinogenin-3-O-beta-D-glucopyranuronide; the invention not only provides an important gene element for biosynthesis of aescin compounds, but also provides a key gene locus for molecular breeding of aesculus chinensis, and provides a theoretical basis for glycosylation modification of other triterpenoid saponins.

This invention provides a composition for alleviating fatty liver and its application, belonging to the field of pharmaceutical technology. The composition of this invention comprises the following components: dihydroberberine, neoruscosaponin, physalicylate, and trans-trimethoxyresveratrol, wherein the final concentrations of dihydroberberine, neoruscosaponin, physalicylate, and trans-trimethoxyresveratrol are all 5-15 μM. The composition of this invention can effectively alleviate hepatic fat accumulation, impaired liver function, and oxidative stress damage to the liver, and as a new product for the prevention and treatment of fatty liver, it has good application prospects.

The present invention relates to a composition for use in a method of treating a liver disease, preferably metabolic dysfunction-associated steatohepatitis (MASH). The composition comprises: • An effective amount of at least one saponin active ingredient (preferably ginsenoside or diosgenin) • And / or an effective amount of at least one anthelmintic (preferably niclosamide or nitazoxanide) • And / or an effective amount of at least one mitochondrial uncoupler.

The invention discloses an application of Gitogenin (Gitogenin, GIT) in preparation of a medicine for preventing or treating hypertrophic cardiomyopathy and diseases caused by the hypertrophic cardiomyopathy. According to the application disclosed by the invention, the prevention or treatment of the hypertrophic cardiomyopathy by the Gitogenin is proposed for the first time, and experiments find that the in-vitro treatment of the Gitogenin can obviously inhibit the phenotype of myocardial cell hypertrophy; gitogenin is applied to gavage treatment on a mouse with hereditary hypertrophic cardiomyopathy caused by gene mutation, and the Gitogenin is found to obviously relieve pathological cardiac hypertrophy of the mouse and improve the cardiac function. The Gitogenin can be used for preparing the medicine for resisting the hereditary hypertrophic cardiomyopathy, and a new way and means are provided for treating the hypertrophic cardiomyopathy; in addition, the Gitogenin is clearly reported to be a main natural steroid component separated from a whole plant of a plant Tribulus longipetaus (a caltrop plant), the biological safety of the Gitogenin to organisms is high, and the Gitogenin has a good application prospect in clinic.

The invention discloses a hederagenin C-23 heterocyclic ester derivative as well as a preparation method and application thereof, and belongs to the technical field of organic chemistry. The structure of the derivative is shown in the specification, wherein R represents pyrazole, thiazole, oxazole, furan, pyrimidine, pyrazine or indole. Pharmacological tests show that part of hederagenin C-23 heterocyclic ester derivatives (T-BZ, T-SZ, T-EZ, T-MD and TBQ) prepared by the invention have better MDR reversal activity than verapamil, can significantly increase the sensitivity (p < 0.0001) of drug-resistant KBV cells to paclitaxel, are P-gp inhibitors with more excellent MDR reversal activity, can be used in combination with common antitumor drugs, and can be used for preparing drugs for treating tumors. The good anti-tumor activity is realized.