38results about How to "Increase fat solubility" patented technology

The invention belongs to the field of preparation of sedation maintaining agents, and particularly relates to a sedation maintaining agent administrated through oral mucosa and a preparation method of the sedation maintaining agent. Bamboo leaf polysaccharide and pigskin collagen peptide are heated and mixed with chlorogenic acid and butyl acetate under the catalytic action of lanthanum nitrate, and the obtained moisturizing adhesive has biocompatibility, can be stably adhered to oral mucosa and can promote salivary secretion of children; nanoparticles obtained through freeze spray drying are uniformly dispersed in a copolymer solution containing sodium salicylate and polyacrylate, and the obtained nervous system regulator can balance excitability of sympathetic nerves and parasympathetic nerves of children; the emotion relieving composition contains modified felwort powder obtained through esterification reaction, the modified felwort powder is mixed with a moisturizing adhesive and a nervous system regulator, and the prepared sedation maintaining medicament administrated through the oral mucosa protects oral health of children in the oral operation anesthesia process, is free of irritation, improves anxiety emotion and does not affect postoperative awakening.

The invention provides a functional rare earth growth factor and a preparation method and application thereof, the rare earth growth factor comprises PEG-MoS2 and nano cerium oxide particles CeO2-NPs in a mass ratio of 1: (0.2-5), the PEG-MoS2 is a solid phase material with the surface modified with PEG, and the solid phase material is MoS2. The two materials of PEG-MoS2 and CeO2NPs are compounded, the rare earth growth factor obtained after compounding can effectively remove active oxygen existing in a wound, and the wound healing rate is effectively increased.

The invention relates to a preparation method of a mogroside phospholipid complex. The preparation method comprises the following steps: (1) mixing a mogroside extract and lecithin according to a certain proportion to obtain a first turbid solution; (2) adding tetrahydrofuran into the first turbid solution obtained in the step (1) to obtain a second turbid solution, and performing ultrasonic treatment on the second turbid solution to uniformly disperse the second turbid solution to obtain a first reaction solution; (3) stirring the first reaction solution obtained in the step (2) until the first reaction solution is clear and transparent to obtain a second reaction solution; (4) carrying out reduced pressure evaporation on the second reaction liquid obtained in the step (3) to remove tetrahydrofuran so as to obtain an oily film; and (5) adding a proper amount of chloroform into the oily film obtained in the step (4) to obtain a third turbid solution, filtering the obtained third turbid solution through a microporous filter membrane to obtain a filtrate, carrying out rotary evaporation to obtain the filtrate, and removing the chloroform to obtain the momordica grosvenori saponin phospholipid compound. Compared with the MGE, the fat solubility of the MGE-PC is improved by 4.34 times; and the absorption rate of MGE-PC is obviously improved by 2.7 times.

The invention discloses a beta-lactamase inhibitor and application thereof, the beta-lactamase inhibitor has a structure as shown in the following formula (I) or a pharmaceutically acceptable salt or an isomer or a deuterated substance of the beta-lactamase inhibitor, and the beta-lactamase inhibitor can increase the combination of a compound fat-soluble group and an amide and a sulfonic group in an avibactam structure and increase the fat solubility of the structure; the active metabolite avibactam can be quickly and completely released under the action of the biological enzyme, so that the oral bioavailability of the avibactam is effectively improved, the avibactam can be orally administrated, and the problem that the avibactam cannot be orally administrated is solved. # imgabs0 #

The invention discloses a method for preparing high-purity estra-1, 3, 5 (10)-triene-3, 15 alpha, 16 alpha, 17 beta-tetrol (abbreviated as estratrol), which is characterized in that 3-hydroxy-17 beta-hydroxyestra-1, 3, 5 (10), 15-tetraene is used as a raw material, and the estratrol is prepared by three steps of phenolic hydroxyl group protection, asymmetric dihydroxylation and hydrolysis. According to the preparation method, 3-hydroxy-17beta-hydroxyestra-1, 3, 5 (10), 15-tetraene is taken as a raw material, 3-hydroxyl is protected by alkoxy-substituted benzoyl, asymmetric dihydroxyl reaction is carried out through catalytic oxidation of potassium osmate, double alpha-hydroxyl is introduced to 15, 16-positions, chemical reagents and catalysts with high cost are not needed in the preparation method, and the preparation method is simple and easy to implement. The dihydroxylation has the advantages of high stereoselectivity, easiness in purification and separation, mild reaction conditions and simplicity and convenience in operation, and high-efficiency preparation of high-purity estetrol (more than or equal to 99.5%) can be realized.

The invention belongs to the technical field of medicinal chemistry, and particularly relates to a hydrazino-modified natural polyamine-naphthalimide conjugate as well as a preparation method and application thereof. The preparation method comprises the following steps: firstly, introducing hydrazino to the tail end of a polyamine chain, further prolonging the length of the polyamine chain, and finally, conjugating parent nucleus naphthalimide to synthesize a series of hydrazino-modified natural polyamine-naphthalimide conjugates. The compound synthesized by the invention comprises a substituent-free type of parent nucleus naphthalimide, a 3-site amino substituted type of parent nucleus naphthalimide and a 4-site chlorine substituted type of parent nucleus naphthalimide. The conjugate disclosed by the invention solves the problems of poor solubility, relatively complicated clinical compatibility, poor patient immunity in clinical application of chemotherapeutic drugs and the like of the naphthalimide analogue represented by the dinafide in the prior art, and also has relatively good targeting property. According to the conjugate disclosed by the invention, the targeting property and bioavailability of a drug on tumor cells can be improved by utilizing the polyamine transporter highly expressed on the surfaces of the tumor cells, and the toxic and side effects on normal cells are reduced.

The present invention provides a compound DOTA-HX2-DZ and its application, belonging to the field of biomedical technology. The present invention optimizes the molecular structure of DZ-HX2-DOTA, designs and adopts a special linker, and solves the problem of limited anti-tumor efficacy caused by the poor performance of radiolabeled drugs in the prior art, such as stability, lipid solubility and tumor retention time. The compound of the present invention can significantly reduce the risk of delabeling of radioactive metal ions in the in vivo environment, ensuring that it can stably play a role in the targeted site; the molecule has excellent lipid solubility and can more easily penetrate the cell membrane and vascular barrier, thereby improving the bioavailability of the drug, prolonging the in vivo circulation time, and prolonging the tumor retention time, thereby improving the treatment efficiency. The DZ-HX2-DOTA of the present invention has a broad spectrum of tumor targeting, and can be used for diagnosis and treatment of various types of malignant tumors.

The invention discloses a 1, 8-disubstituted tryptanthrin derivative and application of the 1, 8-disubstituted tryptanthrin derivative to prevention and treatment of phytopathogen and anti-tumor activity, the general formula of the derivative is shown in (I), and the test result of the compound shown in the general formula on the bacterial activity of phytopathogen shows that the compound has a good antibacterial effect on Xanthomonas oryzae pv. Oryzae, Xanthomonas citri pv. Citri and the like, and can be used for preventing and treating the phytopathogen. The method can be used for developing novel agricultural bactericides. Meanwhile, results of the compound shown in the general formula on tumor cells show that the compound has good in-vitro anti-tumor activity on human chronic myelogenous leukemia cells K562, human lung cancer cell lines A549, human liver cancer cells HepG2, human prostate cancer cells PC3 and the like, and can be used for researching novel anti-tumor drugs. # imgabs0 #

The present invention belongs to the field of biomedicine technology and discloses an anti-glycation amino acid derivative having a structure of general formula I or an isomer of general formula I: #imgabs0# wherein R 1 is selected from the group consisting of alanine, threonine, proline, asparagine, glutamine, leucine, tryptophan, serine, valine, methionine, tyrosine, histidine, L-aspartic acid-4-tert-butyl ester, L-aspartic acid-1-tert-butyl ester, glycine, isoleucine, phenylalanine, lysine, arginine, cysteine, L-glutamic acid-5-tert-butyl ester, and the residue after condensation of L-glutamic acid-1-tert-butyl ester, R 2 Select one of the following structures: -C 15 H 29 ,‑C 15 H 31 ,‑C 15 H 27 , ‑CHOHC 14 H 27 , ‑CHOHC 14 H 29 The present invention also discloses a synthesis method and application of anti-glycation amino acid derivatives. Such compounds improve the fat solubility of amino acid compounds, which is conducive to penetration into the skin, and show excellent effects in anti-oxidation, anti-glycation, skin barrier repair, tissue healing and the like.

The invention relates to an N-terminal acetylation and C-terminal ethylamine dual-modified LMN-NKA polypeptide derivative or a pharmaceutically acceptable salt and a preparation method thereof. The chemical name of the LMN-NKA polypeptide derivative is N-acetyl-L-aspartic acid-L-lysine-L-phenylalanine-L-valine-glycine-N-methyl-L-leucine-L-n-leucine-ethylamine, and the structural general formula of the LMN-NKA polypeptide derivative is Ac-Asp-Lys-Phe-Val-Gly-NMe-Leu-Nle-NHCH2 CH3, and the structural general formula of the LMN-NKA polypeptide derivative is shown in the description. According to the dual-modification strategy, the binding activity of the NK2 receptor can be specifically reserved, the enzymolysis stability is high, the transmembrane efficiency is high, the lipid solubility is high, and the physicochemical property is stable. The LMN-NKA polypeptide derivative or the pharmaceutically acceptable salt thereof disclosed by the invention is particularly suitable for preparing a medicine for treating diseases related to an NK2 receptor.

The present invention relates to vincamine derivatives and preparation methods and applications thereof, and belongs to the technical field of preparation of vincamine derivatives. The vincamine derivatives disclosed in the present invention have the following advantages: (i) modification of the tail chain increases the lipid solubility of vincamine compounds, and does not affect the cerebral blood flow regulation of vincamine itself, which helps the carried drug to penetrate the blood-brain barrier, and exerts a brain protective effect, improving brain microcirculation disorders; (ii) the tertiary amine group in the parent nucleus structure of vincamine derivatives has the property of being ionizable under acidic conditions, and can achieve efficient carrying and lysosomal escape of nucleic acid drugs through charge adsorption, thereby improving intracellular transport; (iii) vincamine derivatives inherit various pharmacological activities inherent in vincamine and have high safety. Therefore, the vincamine derivatives disclosed in the present invention have good application prospects in brain-targeted delivery of drugs for treating brain diseases.

The invention relates to the field of fluorescent dyes, in particular to a near-infrared fluorescent dye for brain imaging as well as a preparation method and application of the near-infrared fluorescent dye. The near-infrared fluorescent dye for brain imaging has the advantages of novel structure, good biocompatibility, large Stokes shift, high light stability, high fluorescence signal-to-noise ratio and the like; the near-infrared fluorescent dye prepared by the invention is simple in preparation process, mild in reaction condition, short in synthesis path and beneficial to industrial production, and has a wide application prospect.

The present invention relates to fruit preservation technology, and in particular to an application of a preservative in the preservation of citrus fruits on the tree and in storage. In particular, the present invention relates to a method for treating citrus fruits, the method comprising: soaking the fruits in a solution containing isooctyl loropylacetate, or spraying the fruits with a solution containing isooctyl loropylacetate; the treatment is a treatment on the tree or a post-harvest treatment. The present invention also relates to the use of isooctyl loropylacetate for preserving citrus fruits on the tree or after harvest, or improving the internal and / or external quality of citrus fruits.

The invention belongs to the technical field of chemical synthesis, and particularly relates to a compound clobetasol propionate derivative and a preparation method thereof. The compound clobetasol propionate derivative has a structure as shown in a general formula (I). The clobetasol propionate derivative is prepared by carrying out esterification reaction on 11-site hydroxyl of clobetasol propionate and acid, the reaction condition is simple, the yield is higher, the clobetasol propionate derivative is easy to separate and purify, and the fat solubility of the clobetasol propionate subjected to structure optimization is improved. The invention provides possibility for subsequent activity test, and provides a novel method for structural modification of the compound. Hectogram-level preparation can be conveniently realized in a laboratory, and the method is suitable for large-scale production. # imgabs0 #

The invention discloses an HDAC6 inhibitor, a medicinal composition and application, relates to the technical field of medicines, and solves the technical problems that the existing HDAC6 is poor in selectivity and poor in brain permeability and metabolic stability. The HDAC6 inhibitor disclosed by the invention is selected from any one or more of compounds with structural formulas as shown in formulas 1-13, meanwhile, the invention provides a preparation method of the compounds with the formulas 1-13, and on the basis, the invention further provides a medicinal composition comprising the inhibitor and a pharmaceutically acceptable carrier or auxiliary material thereof. According to the HDAC6 inhibitor provided by the invention, the inhibition activity is effectively improved, the subtype selectivity, fat solubility and metabolic stability to molecules are improved, and the HDAC6 inhibitor has high brain penetration.

The invention relates to a dodecaurea cage type molecule as well as a preparation method and application thereof, and belongs to the technical field of chemical synthesis and pharmaceutical preparations. The molecule is non-toxic and neutral, the ureido part in the molecule has a plurality of hydrogen bond donors and acceptors, and the molecule has a three-dimensional cavity capable of completely coating a bottom object and can simulate protein binding sites and functions. An organic ammonium sulfate salt is used as a template, and a tripodal triurea precursor based on N bridging reacts with diisocyanate or dicarbamate to obtain a dodecaurea molecular cage. The molecule can be used as a universal tool to chelate different types of phosphate / phosphonate drugs through hydrogen bonds, so that the electronegativity of the phosphate / phosphonate drugs is reduced, the lipid solubility of the phosphate / phosphonate drugs is improved, and the membrane transport efficiency of the phosphate / phosphonate drugs is improved.

The invention discloses a 2-fluoro-3-aliphatic amine tryptanthrin derivative and application of the compound to prevention and treatment of phytopathogen and anti-tumor activity, the general formula of the derivative is as shown in (I), and the test result of the compound as shown in the general formula to the bacterial activity of phytopathogen shows that the compound can be used for preparing the 2-fluoro-3-aliphatic amine tryptanthrin derivative. The compound has a good antibacterial effect on Xanthomonas oryzae pv. Oryzae, Xanthomonas citri pv. Citri and the like, and can be used for developing novel agricultural bactericides. Meanwhile, results of the compound shown in the general formula on tumor cells show that the compound has good in-vitro anti-tumor activity on human chronic myelogenous leukemia cells K562, human lung cancer cell lines A549, human liver cancer cells HepG2, human prostate cancer cells PC3 and the like, and can be used for researching novel anti-tumor drugs. # imgabs0 #

This application relates to the field of polymer materials technology, specifically disclosing a high-efficiency, long-lasting antibacterial polyester composite material and its preparation method; the high-efficiency, long-lasting antibacterial polyester composite material comprises the following raw materials in parts by weight: 80-95 parts of polyester melt, 0.5-5 parts of composite antibacterial agent, 0.1-1 parts of dispersant, and 0.5-3 parts of interface compatibilizer; the composite antibacterial agent is a complex of nano-zinc dioxide and organic quaternary ammonium salt, wherein the organic quaternary ammonium salt is a double long-chain quaternary ammonium salt; the use of double long-chain quaternary ammonium salt in this application can compensate for the slow onset of action of nano-zinc dioxide, and nano-zinc dioxide can slowly release zinc ions to achieve a long-lasting protective effect. The combination of the two promotes the preparation of polyester material to achieve both good immediate contact sterilization and long-lasting protection.

The invention discloses a high-voltage lithium cobalt oxide lithium ion battery electrolyte and a lithium ion battery thereof, the electrolyte capable of adapting to high-voltage lithium cobalt oxide is designed from the angle of electrolyte, and the cycle life of the lithium cobalt oxide battery can be prolonged. The key point of the invention is to provide an additive applied to a high-voltage lithium cobalt oxide battery electrolyte. The additive is fluorophenylacetonitrile and simultaneously contains-F and-CN functional groups, and the F functional group has strong electronegativity, high stability and good fat solubility, so that the molecular activity can be improved, and a stable negative electrode-electrolyte interfacial film (SEI) rich in LiF can be formed on the surface of a negative electrode through reaction; the-CN functional group not only can remove H2O and HF in the electrolyte, but also can be deposited on the surface of the lithium cobalt oxide to form a surface protection film, so that the electrochemical performance of the electrolyte is improved.

The invention relates to the technical field of paclitaxel, and particularly discloses difluoromethylated paclitaxel and a preparation method thereof. The invention relates to difluoromethylated paclitaxel. The difluoromethylated paclitaxel comprises direct difluoromethylated paclitaxel and deoxidized difluoromethylated paclitaxel. The difluoromethylated paclitaxel provided by the invention can be used in clinical drugs, and has the advantages of improved drug utilization rate, high selectivity, high target cell pertinence and the like. In addition, the preparation method has the advantages of mild reaction conditions, high yield, wide substrate applicability and the like.

To provide a means capable of simultaneously and accurately analyzing a component derived from a carrier for liquid phase peptide synthesis with, for example, a target peptide. A method for simultaneously analyzing a carrier for liquid phase peptide synthesis, a component derived from the carrier for liquid phase peptide synthesis, an amino acid to which the carrier for liquid phase peptide synthesis is bound, and a peptide compound to which the carrier for liquid phase peptide synthesis is bound, with a target peptide or final target peptide, the analysis method using high-performance liquid chromatography or supercritical fluid chromatography using an alcohol as an eluent.

This application relates to the field of biomedicine, specifically to the use of small molecule compounds in the preparation of drugs for the treatment and / or prevention of α-synuclein diseases, wherein the small molecule compounds are selected from at least one of AO-365 / 43264238 and AG-670 / 40728295. The small molecule compounds provided in this invention can precisely target and interfere with α-syn-VAPB interactions, improving neuronal damage caused by abnormal aggregation of α-synuclein, thereby safely and effectively treating and / or preventing α-synuclein diseases, particularly Parkinson's disease.

The invention discloses a method for preparing fat-soluble acylated chlorogenic acid through an enzyme method, and belongs to the technical field of immobilized enzyme development and fat-soluble antioxidant processing. The invention discloses a method for preparing fat-soluble acylated chlorogenic acid by an enzymic method, which comprises the following steps of: catalyzing chlorogenic acid and fatty acid vinyl ester to generate ester exchange reaction by using hydrophobic micron-sized silicon-based carrier immobilized lipase; acylated chlorogenic acid products with fat solubility and oxidation resistance, such as acetyl chlorogenic acid, butyryl chlorogenic acid, capryloyl chlorogenic acid and lauroyl chlorogenic acid, are directionally synthesized. According to the self-made immobilized lipase catalyst based on the hydrophobic micron-sized silicon-based carrier, the defects of unstable enzyme activity, difficulty in separation, low reuse efficiency and the like in the existing process for preparing fat-soluble acylated chlorogenic acid by an enzyme method are overcome; oriented, efficient and rapid synthesis of a series of acylated chlorogenic acid products with fat solubility and oxidation resistance is achieved, the preparation process is simple, safe and reliable, and the industrial application potential is huge.

The present application relates to a kind of high-stable pyrylium alcohol derivatives with light protection, whitening activity and its preparation method and application.The present application is based on the molecular structure of pyrylium alcohol and is connected with different cinnamic acid side chain, obtains a series of cinnamic acid side chain modified pyrylium alcohol derivatives.The pyrylium alcohol derivatives of the present application can effectively improve the chemical stability of pyrylium alcohol, effectively solve the discoloration and inactivation problem of pyrylium alcohol in cosmetic formula.The pyrylium alcohol derivatives of the present application have excellent chemical stability, have the ability of rapid oxidation resistance, and can realize precise synergistic effect at cell level, the activity of inhibiting melanin, antioxidant and light protection in organism is significantly better than pyrylium alcohol.The pyrylium alcohol derivatives of the present application have higher fat solubility and lower effective concentration, can be used for preparing whitening, antioxidant, light protection and other cosmetics, and have important market value.

The invention belongs to the technical field of cosmetics, and particularly relates to anti-aging essence and a preparation method thereof. The anti-aging essence is prepared from components in percentage by mass as follows: 3%-8% of a fermentation extracting solution, 0.5%-2% of a chlorogenic acid-L-ascorbic acid fatty acid ester compound, 0.2%-0.5% of ethylenediamine tetraacetic acid disodium salt, 1%-1.5% of betaine, 1.2%-1.5% of beta-glucan, 0.05%-0.2% of carbomer, 0.1%-0.2% of triethanolamine, 3%-6% of a humectant and the balance of water. A proper extraction process and a proper biological fermentation process are selected, and active ingredients in the grapes and the kiwi fruits are fully reserved; through synergistic cooperation of all the components, the prepared anti-aging essence is stable in component and has a good moisturizing effect and anti-aging capacity.

The invention provides a preparation method for asymmetrically synthesizing a nucleoside prodrug intermediate or prodrug based on copper catalysis of a P (V) precursor, which comprises the following steps of: reacting a nucleoside compound with racemic phosphamide under a metal catalysis condition in the presence of an organic solvent, alkali, a chiral ligand, a # imgabs0 # molecular sieve and a catalyst; a series of phosphorus center chiral nucleoside prodrug intermediates or prodrugs are generated. The asymmetric synthesis method provided by the invention is simple to operate, economical and efficient, and the obtained target compound has the characteristics of good substrate universality and high diastereoselectivity, and has good application potential in the fields of virus resistance and tumor resistance.

The invention relates to the technical field of biological medicines, and particularly discloses a stem cell preparation for treating cerebral apoplexy and a preparation method thereof. The stem cell preparation for treating the cerebral apoplexy is prepared by combining optimized umbilical cord mesenchymal stem cells and traditional Chinese medicine microcapsules, and the umbilical cord mesenchymal stem cells are optimized by using a functional aid formed by compounding panax notoginseng saponins, alkannin and catechin. Natural traditional Chinese medicines of gastrodia elata, radix puerariae and saussurea involucrata are subjected to multiple extraction with absolute ethyl alcohol and a bacterium enzyme solution to prepare the traditional Chinese medicine microcapsule. The natural active ingredients and the stem cells play a synergistic role, and the prepared stem cell preparation has the advantages of high stability and high safety, has a remarkable targeted treatment effect on ischemic cerebral apoplexy, and has an important application value in prevention and treatment of cardiovascular and cerebrovascular diseases.

The invention provides an eicosapentaenoic acid derivative, a preparation method and application thereof and a medicine for preventing and treating nervous system diseases, and belongs to the technical field of medicines. The eicosapentaenoic acid derivative provided by the invention has a structure as shown in a formula I, is an ester derivative of eicosapentaenoic acid (EPA), is high in lipid solubility, and can improve the pharmacological effect of the EPA. Pharmacological experiments show that the EPA derivative has a better nerve cell protection effect than EPA, and the medicinal value of EPA is expected to be expanded. And the formula I of the # imgabs0 # is shown in the specification.

The invention discloses a pyridine [3, 2-d] pyrimidine-2-amine derivative as well as a preparation method and application thereof. The pyridine [3, 2-d] pyrimidine-2-amine derivative can be used as a TLR7 / 8 dual agonist and is used for treating diseases related to TLR activity, such as diseases, tumors, inflammatory diseases and the like caused by virus (such as HBV (Hepatitis B Virus) and HIV (Human Immunodeficiency Virus)) infection. Particularly, the pyridine [3, 2-d] pyrimidine-2-amine derivative provided by the invention has better physicochemical properties, druggability, heart safety and oral bioavailability, and has very good research and application values in the field of medicines.

The application provides a viscosity-responsive luminescent probe, a preparation method and application. The luminescent probe has an ultra-sensitive viscosity response performance, and the viscosity response range thereof covers the viscosity change range of edible oil. After the luminescent probe is added into the edible oil, the fluorescence intensity has a high correlation with the content of the polar component in the edible oil. The change of the polar component of the edible oil is obtained by using the response of the luminescent probe to the viscosity change of the edible oil, so that the rapid and sensitive detection of the polarity of the frying oil is realized.