2274results about "Steroids" patented technology

The invention discloses a compound with anti-tumor activity. The compound has a chemical structural formula as shown in a formula (I). The compound belongs to a novel tetracyclic triterpenoid natural product, has good fat solubility and chemical stability, and can be conveniently extracted from the rhizome of a herbal medicine Polygala fallax Hemsl. And prepared into an oral or injection form. The invention also provides a preparation method and application of the compound. The compound provided by the invention can obviously inhibit the growth of mouse lung cancer and reduce the volume and weight of tumor, and can be used for treating tumor diseases.

The invention relates to a ligand-effector moiety provided with at least one saponin and antibody-effector moiety provided with at least one saponin. An aspect of the invention is a composition comprising the ligand-effector moiety provided with at least one saponin or the antibody-effector moiety provided with at least one saponin of the invention. The invention also relates to an antibody-drug conjugate comprising covalently linked saponin and to an antibody-oligonucleotide conjugate comprising covalently linked saponin. An aspect of the invention relates to a pharmaceutical composition comprising the ligand-effector moiety provided with at least one saponin or the antibody-effector moiety provided with at least one saponin of the invention, and optionally further comprising a pharmaceutically acceptable excipient. The invention also relates to the ligand-effector moiety provided with at least one saponin or the antibody-effector moiety provided with at least one saponin, for use as a medicament. The invention also relates to the ligand-effector moiety provided with at least one saponin or the antibody-effector moiety provided with at least one saponin of the invention for use in the treatment or prophylaxis of a cancer.

This invention relates to a crystalline 19-nor C3,3-disubstituted C21-pyrazolyl steroid of Formula (I),and compositions thereof. Also disclosed herein are methods of making the same and methods of using the same.

The present application provides a variety of salts of 25HC3S, including crystalline salts of 25HC3S. Provided herein are pharmaceutical formulations of the salts of the invention, and methods of treating or preventing diseases therewith, the diseases such as non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), alcoholic hepatitis, acute kidney injury (AKI), psoriasis, atherosclerosis, hypercholesterolemia, hypertriglyceridemia, alcoholic fatty liver disease (AFLD), alcoholic steatohepatitis (ASH), leptin resistance, leptin deficiency, diabetic conditions, autoimmune conditions, inflammatory conditions, and the like. Nervous system disorders, EB virus related growth, and disorders associated with fat accumulation and inflammation. Methods of making the salts of the present application are also provided.

The invention relates to the technical field of extraction and separation of compounds in traditional Chinese medicinal materials, in particular to a method for simultaneously separating and purifying three pentacyclic triterpenoids from a tripterygium hypoglaucum root medicinal material. Three pentacyclic triterpenoid monomers are obtained through the steps of smashing, reflux extraction, normal-phase silica gel chromatography, reversed-phase high-pressure column chromatography, recrystallization and the like, the method is high in extraction efficiency and small in reagent dosage, the three pentacyclic triterpenoid compounds can be obtained at the same time, and the obtained compounds are high in purity and yield, have high social and economic value and are suitable for industrial production. The purity of the obtained plasmin, tripterine and demethylzeylasteral is high, and a foundation is laid for the preparation and production of reference substances of triterpenoid components in the roots of pyracantha fortunei, the subsequent pharmacological activity and the development of new immune drugs.

The invention discloses a limonin compound and application thereof in preparation of a medicine for preventing and / or treating cancers. The structure of the limonin compound is shown as a formula I or II. The cancer is at least one of breast cancer, liver cancer, gastric cancer, esophageal cancer, leukemia, pancreatic cancer, glioma, osteosarcoma, prostatic cancer, nasopharynx cancer, cervical cancer, ovarian cancer, kidney cancer and skin cancer. According to the invention, activity screening is carried out on various natural product extracts, it is found for the first time that limonin compounds with structural formulas I and II have excellent inhibitory activity on various different types of human cancer cells, and an optional scheme is provided for broad-spectrum anti-cancer drugs. Related results also show that the compound provided by the invention can inhibit migration and invasion ability of breast cancer cells, promote cell apoptosis and retard a cell cycle. The limonin compound applied in the invention is derived from mallotus oblongifolius, the source is wide, and the production cost is low.

The invention relates to the field of biological medicine, in particular to a prodrug structure with ROS signal response performance and a preparation method and application thereof. The prodrug molecule with ROS signal response performance developed by the invention can quickly release living active molecules in a disease signal ROS-enriched environment, and plays a role in targeted therapy. The method has good universality, prodrug modification can be carried out on multiple molecules, four kinds of drug molecules approved to appear on the market are included, and it is verified that the solubility and biocompatibility of drugs can be improved, cytotoxicity can be reduced, and the effect of targeted therapy can be improved. Based on the structural characteristics of the molecules, the molecules can also be complexed with PVA hydrogel, and responsive controllable release of the medicine is further achieved.

The invention discloses a synthesis method of oxyalkyl isourea and application of the oxyalkyl isourea as a free radical alkylation reagent. According to the synthesis method, cheap and rich alcohol compounds and carbodiimide are used as raw materials, oxygen alkyl isourea is synthesized in one step under the mild condition of metal catalysis, the synthesis process is simple and convenient, the yield is high, and hectogram-level large-scale preparation can be achieved. The synthesized oxyalkyl isourea can be used as a free radical alkylation reagent to be applied to a coupling reaction of metal catalysis, so that different alkylate products rich in saturated carbon sequence structures are prepared, and the method has a good application prospect.

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 present application provides ursolic acid diethanolamine salt and ursolic acid morpholine salt. It also provides a composition comprising the salt, and a method of using the salt.

The invention provides novel application and a method of asiaticoside. The method comprises the following steps: S1, extraction: taking a centella asiatica medicinal material, performing coarse crushing, adding ethanol, performing reflux extraction, performing filtration, and combining filtrate for standby application; s2, concentrating: concentrating the ethanol extracting solution under reduced pressure until no alcohol smell exists, centrifuging, and reserving supernate for later use; s3, carrying out D101 column chromatography; s4, alumina column chromatography; s5, performing concentration; s6, drying; s7, dissolving with methanol, adding water, standing, and monitoring clear liquid and crystallization conditions in a liquid phase; s8, filtering after crystallization is finished, washing with ethanol, drying crystals under the conditions that the vacuum degree is-0.06 to-0.08 mpa and the temperature is 60-70 DEG C, and crushing and sieving dry paste to obtain asiaticoside; specifically, the new application comprises reduction of uric acid (UA), urea (UREA), creatinine (CREZ), low-density lipoprotein cholesterol (LDL-C), high-density lipoprotein cholesterol (HDL-C) and total cholesterol (CHOL) in serum of a hyperuricemia model SD rat, and reduction of damage of hyperuricemia to kidney. And the yield of asiaticoside extracted by the method is high and is about 84%.

The invention belongs to the field of organic synthetic chemistry, and relates to a preparation method of melatonin and meerythrine indole derivatives and compounds. Specifically, the indole derivative is efficiently synthesized by taking arylamine and carboxylic acid as raw materials through a one-pot two-step reaction in the presence of catalysis of ferric chloride hexahydrate (FeCl3. 6H2O), a ligand, a diazotization reagent, an additive and a solvent under the conditions of visible light irradiation, inert atmosphere and room temperature. According to the method, visible light induced iron-based LMCT catalysis and iron lewis acid catalysis functions are integrated, and efficient integration of diazotization, decarboxylation, free radical coupling and cyclization reaction is achieved. The method has the advantages that raw materials are cheap and easy to obtain, reaction conditions are mild, substrate applicability is wide, functional group compatibility is good, operation is easy, convenient and safe, and environment friendliness is achieved, gram-level scale preparation can be achieved, and a green and efficient synthesis path is provided for indole compounds with biological activity such as melatonin and meerythrine.

The invention discloses design and synthesis of a series of brain-targeted ginsenoside Rg1 derivatives and application of the brain-targeted ginsenoside Rg1 derivatives in treatment of Alzheimer's disease. According to the invention, ginsenoside Rg1 and polyethylene glycol with a specific chain length are covalently linked to successfully construct the derivative capable of enhancing the penetrating power of the blood-brain barrier. The series of derivatives provided by the invention not only solve the problems of poor brain targeting and insufficient stability of natural Rg1, but also can inhibit neuroinflammation by regulating and controlling an NLRP3 / caspase-1 signal channel in an LPS-induced neuroinflammation model, and finally, the learning and memory ability is remarkably improved. The product is simple and convenient in preparation process and good in biological safety, and a new candidate compound is provided for developing a new generation of Alzheimer disease treatment medicines.

The invention relates to equipment for preparing clobetasol propionate liniment and a preparation method of the clobetasol propionate liniment. The equipment comprises a material mixing mechanism, a barrel, a stirring shaft rotationally arranged on the barrel, stirring blades for stirring substances, a partition plate for separating the interior of the barrel, a crystallization rod for cooling materials and a drying mechanism for drying the substances. Wherein the stirring blades are fixedly arranged around the stirring shaft, and the stirring blades at the bottom are arranged around the stirring shaft in a swinging manner; the partition plate is movably arranged in the barrel around the stirring shaft; the crystallization rod is movably arranged at the bottom of the barrel; the drying mechanism communicates with the bottom of the barrel; the drying mechanism is communicated with the mixing mechanism; the partition plate is arranged between the fixed first ring frame and the rotary second ring frame; the partition plate is connected with the first ring frame and the second ring frame. The second ring frame rotates to drive the partition plate to open or separate the cylinder. The preparation method solves the problem that the preparation efficiency of clobetasol propionate is affected due to more preparation equipment caused by complex process steps in the clobetasol propionate liniment preparation process in the existing scheme.

The invention discloses a continuous preparation method of sodium tanshinone IIA sulfonate based on a single-tube thin-layer liquid membrane reactor. Comprising the following steps: (1) dissolving tanshinone IIA in an organic solvent as a feed liquid; (2) reacting gas-phase sulfur dioxide with air, and cooling to obtain sulfur trioxide mixed gas; (3) enabling the feed liquid and sulfur trioxide mixed gas to enter a single-tube thin-layer liquid membrane reactor in a parallel flow or reverse flow manner, and carrying out continuous sulfonation reaction to obtain reaction liquid; and (4) adding a sodium salt aqueous solution into the reaction solution to carry out salt forming reaction, centrifuging, drying and purifying to obtain the tanshinone IIA sodium sulfonate. According to the invention, a novel method is adopted to carry out sulfonation reaction on tanshinone IIA, and sulfur trioxide is basically completely consumed after the reaction is finished, so that the generation of waste acid is greatly reduced, and the method has important significance on environmental protection and cost reduction. The green, safe, efficient and continuous preparation of the high-purity tanshinone IIA sodium sulfonate is realized.

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 discloses a method for extracting ginsenoside based on a supercritical extraction method, and relates to the technical field of traditional Chinese medicine extraction. The ginsenoside is extracted through a supercritical extraction method, the extraction process is convenient and efficient, the purity of the ginsenoside is high, organic solvent residues are avoided, the method is green and environmentally friendly, carbon dioxide can be recycled, and the operation cost is low; through degreasing pretreatment, fat-soluble components in ginseng powder are removed, the extraction purity of saponin is increased, the solid loading capacity of supercritical extraction is reduced, the mass transfer resistance is reduced, and the extraction efficiency is improved; the ginsenoside is purified in a post-treatment mode of resin adsorption and elution, polar impurities can be further removed, glutamine is adopted for surface functionalization of the resin, acylamino and carboxyl are introduced to the surface of the resin and can form hydrogen bonds with phenolic hydroxyl groups in the ginsenoside, functional adsorption is achieved, meanwhile, impurities are removed, and the content of the ginsenoside is increased. Reaction conditions are simple and mild, and adsorption efficiency is high.

The invention discloses an oral sleep-aiding composition containing ergothioneine and a preparation method of the oral sleep-aiding composition, and relates to the technical field of sleep-aiding compositions. The oral sleep-aiding composition containing the ergothioneine is prepared from the following components in parts by mass: 0.01 to 3 parts of the ergothioneine, 0.1 to 10 parts of melatonin, 10 to 40 parts of glycine, 2 to 15 parts of magnesium salt, 30 to 70 parts of a diluent, 1 to 10 parts of an adhesive, 0.5 to 5 parts of a lubricant, 2 to 10 parts of a disintegrating agent and 0.1 to 0.5 part of an antioxidant preservative. Through the synergistic compatibility of ergothioneine, melatonin, glycine and magnesium salt, a multi-dimensional action network of oxidation resistance, neuromodulation and receptor inhibition is formed, the limitation of single-component sleep aiding is broken through, and the sleeping efficiency and the sleep maintenance capability are remarkably improved. Based on the scientific proportion of endogenous substances (ergothioneine and glycine), the metabolic burden of traditional sleep-aiding components is avoided, and in combination with the design of a sustained-release preparation, the dose-dependent side effects are reduced, and the safety of long-term taking is improved.

The invention discloses a method for extracting ecdysterone from cyanotis arachnoidea by using a deep-eutectic solvent, and belongs to the technical field of ecdysterone extraction. The method comprises the following steps: mixing a deep-eutectic solvent which takes choline chloride and a hydrogen bond donor material as raw materials with water, extracting ecdysterone in roots and stems of Cyanotis arachnoidea to obtain an ecdysterone crude extract, precipitating the ecdysterone crude extract by adding water, filtering, and adsorbing ecdysterone by using macroporous resin. Adding water for elution to obtain a deep-eutectic solvent-water mixed solution, and recovering under reduced pressure to obtain an extraction solvent for cyclic utilization; and eluting by using alcohol with different concentrations to obtain an ecdysterone crude extract, and purifying the crude extract to obtain high-purity ecdysterone. Compared with a conventional extraction method, the process method adopted by the invention has the advantages that the process is simple, efficient, green and environment-friendly, the used eutectic solvent can be recycled, the loss caused by heating volatilization in the extraction process is avoided, the ecdysterone extracted by the method is pure white, the content of ecdysterone can reach 90% or above after simple purification, and the method is suitable for industrial production. After re-purification, the purity of ecdysterone detected by high performance liquid chromatography is up to 98% or above.

The invention belongs to the technical field of organic synthesis, and particularly relates to an alkyl pentafluorosulfenyl compound and a preparation method and application thereof.The preparation method comprises the following steps that in the protective gas atmosphere, in a solvent, SF5Cl serves as a pentafluorosulfenyl source, an olefin compound serves as a reaction substrate and a free radical trapping agent, a thiol compound serves as a hydrogen source, and the alkyl pentafluorosulfenyl compound is obtained through a one-step reaction; under the action of an olefin additive, the alkyl pentafluorothio compound is constructed by a one-step method through a visible light-induced free radical process, and the olefin additive is used for inhibiting generation of a pentafluorothio chloride byproduct from a pentafluorothio source and an olefin compound. According to the method disclosed by the invention, a series of alkyl pentafluorosulfenyl compounds can be prepared by only needing olefin double bonds in substrates and selecting more substrates through the reaction, the reaction is simple, the reaction condition is mild, the reaction can be completed under visible light, the reaction time is short, the implementation is easy, and the method is suitable for industrial production. And a method support is provided for further screening the alkyl pentafluorosulfenyl compound with excellent biological activity.

This invention discloses tea saponin E3, its isolation and purification method, and its application as a killer of moon jellyfish polyps, belonging to the field of natural product chemistry. The structure of tea saponin E3 is shown below. Derived from plants, it is a natural triterpenoid saponin compound. Compared with tea saponin, it exhibits stronger killing activity against moon jellyfish polyps. Furthermore, its single component and well-defined structure facilitate standardized application and evaluation of potential ecological risks in the biocontrol of moon jellyfish polyps.

The invention discloses a Ganoderma lucidum engineering strain delta W2 after gene editing, a preparation method of the Ganoderma lucidum engineering strain delta W2, and a ganoderic acid compound 3alpha, 22alpha-diacetoxylanost-8, 24-dien-26-oic acid generated by fermentation of the Ganoderma lucidum engineering strain delta W2, and the chemical structural formula of the ganoderic acid compound is shown in the specification. The compound can effectively improve NO release of LPS-induced macrophages RAW264.7 and inhibit release of inflammatory factors TNF-alpha and IL-6, and has a wide application prospect in addition to anti-inflammatory drugs, health-care functional foods or cosmetics. # imgabs0 #

Described are compounds, compositions, and methods for delivery of therapeutic, diagnostic, or prophylactic agents (for example, a nucleic acid).

The invention discloses a pharmaceutical composition for treating or improving Parkinson's disease and application of the pharmaceutical composition. The triterpenoid saponin compounds and the nervonic acid in different proportions are combined, and experiments prove that multiple indexes of Parkinson mice can be remarkably improved when the triterpenoid saponin compounds and the nervonic acid are combined in a specific proportion, and the effect of synergistically improving the Parkinson disease or the progress of the Parkinson disease is achieved. Therefore, the pharmaceutical composition disclosed by the invention can be used for more effectively treating or improving the Parkinson's disease, and has a wide application prospect in the field of treatment of the Parkinson's disease.

The invention provides a high-potency glucocorticoid compound as well as a preparation method and application thereof. Specifically, the invention provides a high-potency glucocorticoid compound as shown in a formula I as well as a preparation method and application of the high-potency glucocorticoid compound. The glucocorticoid compound of the present invention can achieve the same effect at a lower dose, thereby minimizing side effects. # imgabs0 #

The invention provides a preparation method of dehydronandrolone acetate, and relates to the technical field of medicine synthesis. The dehydronandrolone acetate is prepared by carrying out oxidation reaction on etherates; wherein the preparation of the etherate comprises the following steps: step 1, carrying out esterification reaction on nandrolone to obtain an ester; and 2, carrying out an etherification reaction on the esterified product obtained in the step 1 to obtain an etherified product. According to the method for preparing the dehydronandrolone acetate, the dehydrogenation reaction can be completed at normal temperature, and compared with the prior art, the energy consumption and the operation complexity are remarkably reduced. The method disclosed by the invention is safe and environment-friendly, is convenient for recycling, reduces the recycling cost, avoids the problem of generating high-risk nitrosamine genotoxic impurities, and meanwhile, the chloranil is used as the dehydrogenating agent, and the reduction product is easy to recycle and reuse, so that the production cost is further reduced, and the generation of wastes is reduced.

The invention provides a compound as shown in a formula I, and a racemate, a stereoisomer, a tautomer, a nitrogen oxide, a solvate, a polymorphic substance, a metabolite, an ester, a prodrug or a pharmaceutically acceptable salt thereof. The compound has a good 17 beta-HSD1 inhibition effect, can be used for treating or preventing 17 beta-HSD1 mediated diseases and diseases, and can be used for preparing medicines for treating or preventing the 17 beta-HSD1 mediated diseases and diseases. # imgabs0 #

The present invention discloses a natural firming, anti-wrinkle and brightening plant essential oil in the field of skin care products, its preparation method and application. The components of the essential oil include frankincense oil, sandalwood oil, lavender oil, myrrh oil, helichrysum italicum oil, cistus ladaniferus oil, rosa damascena flower oil, vetiver root oil, and marine biological sterols. The marine biological sterols are composed of a mixture of ascidiasterol and sarcophytol A. This plant essential oil can be applied in skin care products such as aqueous solutions, facial masks, essence, lotions, creams, and liquid foundations. The present invention adopts a unique essential oil formula, making the product outstanding in the comprehensive effect of anti-wrinkle and brightening, and without any chemical components, and all comply with the relevant regulations of the "Technical Specifications for Cosmetics Safety", with high safety. In the plant essential oil of the present invention, marine biological sterols made of ascidiasterol and sarcophytol A are added, which have the effects of antioxidant and moisturizing by themselves, and can also improve the penetration and absorption of the essential oil, thereby further enhancing the anti-wrinkle and brightening effects.

The invention relates to a vitamin D3 and 7-dehydrocholesterol eutectic as well as a preparation method and application thereof. The eutectic is prepared from the following raw materials: vitamin D3 and 7-dehydrocholesterol in a molar ratio of (1-1.2): (1-1.2). The yield of the obtained eutectic substance is high, the preparation method is easy to operate, high-toxicity raw materials and waste residues difficult to treat do not exist, and the vitamin D3 eutectic method is more environmentally friendly and high in eutectic efficiency.

The invention relates to the technical field of organic supramolecular chemical materials, in particular to an imine gelator with tri-state red light emission, a three-dimensional network-shaped gel material of the imine gelator, a preparation method and application of the imine gelator. The gel factor is an asymmetric cholesterol-phenoxy-maleonitrile-diethylamino salicyl gel factor, and can be self-assembled in different solvents to form three-dimensional structure gel of a short rod shape, a fiber net shape and a flat strip shape; due to the highly conjugated asymmetric molecular structure, the fluorescent probe presents three-state red fluorescence emission in a solid state, a solution state and a gel state; the gelator shows intuitive colorimetric change and fluorescence'on-off 'double-signal detection performance on Fe < 3 + > and Co < 2 + > in toluene gel, and has colorimetric change, fluorescence'on-off' and gel-to-sol conversion three-signal response on Cu < 2 + >; the gelator has fluorescence'on-off 'detection response to Cu < 2 + > in a solution state, and double-state four-detection response performance to Cu < 2 + > is achieved; the gelator-Cu < 2 + > binary system has fluorescent on-off detection potential on Pb < 2 + >.