35results about How to "High inhibitory activity" patented technology

Provided is a substituted spiropyrido[1,2-a]pyrazine derivative or a pharmaceutically acceptable salt thereof, which is useful as an anti-HIV agent. The present invention relates to a compound represented by the following formula [I] or [II] or a pharmaceutically acceptable salt thereof:

wherein each symbol is as defined in the specification.

[Problem] Provided is a novel 1,3,4,8-tetrahydro-2H-pyrido[1,2-a]pyrazine derivative or a pharmaceutically acceptable salt thereof, or a solvate thereof, which is useful as an anti-HIV agent.

[Solving Means] The present invention provides a compound represented by the following formula [I]

wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof, or a solvate thereof.

The invention discloses a phosphate tetrahydroberberine drug eutectic and a preparation method thereof. The tetrahydroberberine and phosphate are added and mixed in isopropanol water solution, ethanol water solution or methanol water solution according to the molar ratio; the acquired mixed solution is volatilized under the room temperature. The prepared tetrahydroberberine drug eutectic is a triclinic system, and the space group is P-1, and its axial length (i) is FORMULA; the axial angle is FORMULA. The tetrahydroberberine drug eutectic prepared by the invention inherits the pharmacological activity of tetrahydroberberine, its solubleness, dissolution rate, antibiosis bacillus coli and staphylococcus aureus activities are significantly improved in relative to the tetrahydroberberine, thereby saving drug dosage; the method is good for developing to be drug preparation, and the tetrahydroberberine can be widely applied to the medicine field.

The invention relates to an application of 3,14,9-acetyl andrographolide in the preparation of an proinflammatory cytokine, wherein, the proinflammatory cytokine comprises any one of TNF-Alpha, IL-1Alpha, IL-1Beta, IL-2, IL-4, IL-6, IL-8, IL-10, IFN-Gamma and NO.

The invention provides a B-norcholestane benzimidazole compound as well as a preparation method and application thereof. The general structural formula of the compound is as shown in the specification, wherein R refers to any one of H or COCH3; R1 refers to F, NO2, CF3, H, CH3 or OCH3; and R2 refers to H or CH3. The B-norcholestane benzimidazole compound disclosed by the invention has high inhibitory activity on human cervical carcinoma cell lines, human lung carcinoma cell lines and human liver cancer cells. The B-norcholestane benzimidazole compound disclosed by the invention is low in toxicity and low in injury of normal cells, has an effective effect of inhibiting the cancer cells during low concentration, basically does not cause drug injury to normal cells and can be applied to preparing medicines for treating the cancers.

The invention provides an ACE inhibitory peptide in fermented milk and the preparation method thereof, which relates to the inhibitory peptide of an enzyme and the preparation method thereof. The invention aims at solving the problems that the existing chemical ACE inhibitor has severe side effect, and due to the adoption of a biological enzyme method, biological ACE inhibitor has high requirements for production conditions, complicated production process, expensive equipment cost and bitter product. The ACE inhibitory peptide in the fermented milk mainly comprises four kinds of small molecular peptide the amino acid sequences of which are KPAGDF, KAALSGM, KKAAMAM and LDHVPGGAR. The invention has the preparation: 1. fermented milk preparation; 2. filtration, enzyme extermination, centrifugation and ultrafiltration; 3. refrigeration and desiccation. The ACE inhibitory peptide in the fermented milk is milk protein peptide with biological activity, which has no side effect on a human body, and the ACE inhibitory peptide is edible and highly secure without any bitterness; the ACE inhibitory peptide can withstand high temperature of 90 DEG C without degeneration. The method for preparing the ACE inhibitory peptide in the fermented milk has the advantages of low requirements for production conditions, simple production process, no need for expensive equipment, low cost, high security, no bitter product, and the like.

The invention provides an antitumor medicament composition with the capabilities of reducing toxicity and enhancing efficacy and application of the antitumor medicament composition. According to the antitumor medicament composition provided by the invention, panax notoginseng saponins R7 and oridonin are active ingredients with the functions of reducing the toxicity and enhancing the efficacy. The antitumor medicament composition has obvious synergistic interaction in various tumor cells and is capable of obviously reducing toxicity to various human normal cells compared with a singly used medicament, reducing damages to an organism and exerting obvious functions of reducing the toxicity and enhancing the efficacy. Due to the specific effects of reducing the toxicity and enhancing the efficacy, the antitumor medicament composition can be widely applied to treating human cancers.

The invention discloses a 2-N-aryl-4-N-aryl-5-fluoropyrimidine compound as well as preparation and application thereof. The compound has a structural formula (I) shown in the description, in the formula, Ar is substituted or unsubstituted aryl; and the substituent group on the aryl is alkyl, alkoxy, halogen or 4-methyl piperazine-1-yl. Experiment results show that the 2-N-aryl-4-N-aryl-5-fluoropyrimidine compound is capable of effectively inhibiting FGFR4V550L, and can be used as a potential FGFR4V550 seedling compound with high inhibitory activity.

The invention discloses a pegylated F polypeptide as well as a preparation method and application thereof. According to the technical scheme, pegylation modification is carried out on F polypeptide, that is, azide tetrapolyethylene glycol is modified on amino of the F polypeptide, so that the pegylation F polypeptide has remarkable human cervical cancer HeLa cell inhibition activity. Wherein the inhibition activity of the azido tetrapolyethylene glycol F1 polypeptide on HeLa cells is improved by about 3.7 times compared with that of the F1 polypeptide before modification; the inhibitory activity of the azido tetrapolyethylene glycol F3 polypeptide on HeLa cells is improved by about 6 times compared with that of the unmodified F3 polypeptide.

The invention discloses a double-target inhibitor as well as a preparation method and application thereof. The double-target inhibitor has a structure shown as a formula (I), wherein R1 is H, an electron-withdrawing group or an electron-donating group; R is alkyl; n is equal to 1 to 5. The double-target inhibitor provided by the invention can be used for selectively inhibiting HDAC6 and IC50 values on HDAC1 and HDAC8 are greater than 20 muM; the double-target inhibitor is used as a prodrug to be subjected to hydrolysis reaction in cells, and tubulin and an HDAC double-target inhibitor can be released; the inhibition activity of histone deacetylase on solid tumors is improved; the double-target inhibitor has a relatively good inhibition effect on tumor cells. The formula (I) is shown in thedescription.

The invention discloses a preparation method of a fermented chrysanthemum cold dressing sauce with alpha-glucosidase inhibitory activity. The preparation method specially comprises the following steps: frying spice with big fire, performing grinding for later use, knotting shallots, performing putting into a pot, adding rapeseed oil, performing frying, adding a sweet chili sauce, chopped garlic, chopped onion and water, performing stir-frying, adding spice and a tomato sauce, performing decocting, performing braising with heat, finally, adding seasonings, performing uniform stir-frying and performing taking out of a pot; and then sequentially mixing chrysanthemums with dogwood and longan aril according to a certain proportion, then adding sugar, bifidobacterium and fruit and vegetable zymophyte, performing shaking table fermentation to obtain fermentation liquor, then adding saccharomycetes and acetic acid bacteria into the fermentation liquor, and performing secondary fermentation toobtain a finished product. The fermented chrysanthemum cold dressing sauce with alpha-glucosidase inhibitory activity, capable of remarkably improving biological accessibility has the functions of stably reducing blood glucose, being high in safety and reducing the occurrence rate of cardiovascular complications.

The invention discloses a method for preparing low-fishiness and low-bitterness functional food from acid soluble protein of tilapia meat. The method comprises steps as follows: the acid soluble protein of the tilapia meat, tea polyphenol and water in a mass ratio being 320-380:1-10:1,000 are mixed, papain is added in the proportion of 30,000-60,000 U/g of the acid soluble protein of the tilapia meat, enzymolysis is performed for 4-8 h at the pH of 6-7 and the temperature of 35-55 DEG C, an enzymatic hydrolysate is obtained after insoluble substances are removed, the enzymatic hydrolysate is heated to be boiled and then is rapidly cooled to the normal temperature, a filtrate is obtained through ultrafiltration and is dried, and the low-fishiness and low-bitterness functional food is obtained. According to the method, the protein component significantly contributing to activity of a final product can be enriched, and off-flavor impurities contained in raw materials can be removed; with the addition of an antioxidant in an enzymolysis process, generation of compounds resulting in off flavor is reduced, the off flavor of the final product is reduced effectively on the whole, and compared with a product obtained through direct enzymolysis of the tilapia meat, the activity of the final product is increased by 10% or higher.

The invention provides a seed treating agent containing clothianidin, fludioxonil and ipconazole and application of the seed treating agent. The weight ratio of clothianidin to fludioxonil to ipconazole is (15-25): (1-2): (1-2). The seed treating agent can be used for controlling crop diseases and insect pests in seed treatment.

The invention provides an oridonin and docetaxel toxicity reducing and efficacy enhancing antitumor drug composition and application thereof. Active ingredients playing the roles of toxicity reduction and efficacy enhancement are oridonin and docetaxel. The medicine composition has an obvious synergistic interaction effect on various tumor cells, obviously has smaller toxicity on various normal cells of a human body in comparison with single use of a medicine, reduces harm on the body, and plays the roles of reducing toxicity and enhancing efficacy. Owing to the specific toxicity reducing and efficacy enhancing effects, the medicine composition can be widely used for treating cancers of human bodies.

The invention discloses blood-glucose-reducing Mulgedium tataricum tea and a preparation method thereof, belonging to technical field of preparation of health tea drink. The blood-glucose-reducing Mulgedium tataricum tea is prepared from 1-3 parts of Mulgedium tataricum, 1-3 parts of corn stigma and 1-3 parts of lotus leaf through drying, mixing, crushing and sieving. The preparation method comprises the following steps: (1) taking 1-3 parts by mass of Mulgedium tataricum, 1-3 parts by mass of corn stigma and 1-3 parts by mass of lotus leaf; and (2) drying the raw materials in the step (1), mixing, crushing, sieving by a 40-mesh screen, packaging into bags, and sterilizing to prepare the blood-glucose-reducing Mulgedium tataricum tea. According to the blood-glucose-reducing Mulgedium tataricum tea, the inhibition activity of alpha-glucosidase of Mulgedium tataricum is used as a main function for reducing blood glucose, the diuresis-promoting, heat-clearing and choleretic effects of corn stigma and the heat-clearing, lipid-lowering and anti-oxidation functions of the lotus leaf are combined, the postprandial blood glucose value can be reduced, the diabetic ketoacidosis risk is avoided, and the damage of diabetic complication to a human body can be prevented. The preparation method has simple operation steps, has low equipment requirements and is favorable for large-scale production.

The present invention relates to novel compounds as autotoxin inhibitors for treatment and prophylaxis of conditions or a disorder caused by autotaxin activation or increased concentration of lysophosphatidic acid, and also a pharmaceutical composition containing the same.

The novel compounds of the present invention are autotoxin inhibitors, and by inhibiting the production of lysophosphatidic acid, they are useful for treatment or prophylaxis of cardiovascular disorder, cancer, metabolic disorder, kidney disorder, liver disorder, inflammatory disorder, nervous system disorder, respiratory system disorder, fibrotic disease, ocular disorder, cholestatic and other forms of chronic pruritus, or acute or chronic organ transplant rejection.

The invention relates to a sterilization composition. Effective ingredients consist of radix platycodonis and pyraclostrobin according to the weight ratio of (15 to 1):(1 to 20). The sterilization composition obtained by mixing the radix platycodonis and the pyraclostrobin is used for preventing and treating powdery mildew of cucumber and potato late blight; the synergistic interaction effect is obvious; the radix platycodonis is the synergist of the pyraclostrobin; the inhibition activity on the pyraclostrobin can be obviously improved. Through the mixing of the radix platycodonis and the pyraclostrobin, the use of chemicals of pyraclostrobin can also be reduced; the residue of the chemicals is reduced. Meanwhile, through the mixing of the radix platycodonis and the pyraclostrobin, the generation of the germ drug resistance can also be delayed; the prevention and treatment effects are improved.

The invention discloses a nano photo-catalytic purification fabric and a manufacturing method thereof. By a hydrothermal reaction of graphene-chitosan composite aerogel micropowder and a titanium source in an acidic solution, a nano purification finishing agent is prepared, and by impregnating a base fabric in a mixed solution of the nano light purification finishing agent and water, executing baking and then executing washing with water and drying, the nano photo-catalytic purification fabric is obtained. The nano photo-catalytic purification fabric has long-acting mildew-proof and antibacterial functions, has the effect of purifying air and removing formaldehyde, can continuously and stably release negative ions, meets the diversified demands of consumers in pursuit of comfort, green, environmental protection, health care and the like, can be popularized on a large scale, and has higher economic and social benefits.

The invention provides a 2, 2 '-dipyridyl and uracine-1-acetic acid copper tetrafluoroborate complex as well as a preparation method and application thereof, and belongs to the technical field of copper complexes. The preparation method comprises the following steps: preparing a 2, 2 '-dipyridyl and uracil 1-base acetic acid copper tetrafluoroborate complex (X1) from uracil 1-base acetic acid, tetrafluoroborate tetrafluoroborate (acetonitrile) copper (I) and 2, 2'-dipyridyl as raw materials, and preparing the 2, 2 '-dipyridyl and uracil 1-base acetic acid copper tetrafluoroborate complex (X1). The basic unit of X1 is composed of a copper ion, two 2, 2-bipyridine molecules, a uracil-1-yl acetic acid anion and a free tetrafluoroborate, and the geometric shape around the copper ion is a distorted octahedron. Experiments show that the interaction mode of X1 and CT-DNA is an electrostatic mode, and the quenching constant KSV of X1 and a calf thymus DNA system with ethidium bromide (EB) is 4.102 * 10 < 3 > M <-1 >. The inhibitory activity of the compound on MDA-MB-231 and HCT116 is remarkably improved, IC50 results are respectively 12.32 +/-1.58 and 8.56 +/-0.52, and the anti-cancer activity of the compound is further improved after the compound is irradiated by an infrared lamp.

The invention discloses a plant whitening extract and application thereof to whitening cosmetics. The plant whitening extract provided by the invention is extracted from natural medicinal plants, in addition, the extraction process is green and safe, and the obtained extract can inhibit the formation of skin melanin from a plurality of ways and achieve the skin whitening effect; and meanwhile, the plant whitening extract also has the effects of moisturizing, nourishing, bacterium inhibition, sun screening and the like. The plant whitening extract also has good skin whitening and brightening effects when being used in whitening cosmetics.

The invention belongs to the technical field of physical processing, and relates to a technology for soaking and enriching gamma aminobutyric acid in coffee leaves through cooperation of ultrasound and sodium glutamate. The method comprises the steps that coffee leaves are soaked in a sodium glutamate solution with the mass concentration being 0.5%-2.0% and the pH being 5.0-6.0, gamma aminobutyricacid is enriched through ultrasound, the ultrasound frequency is 20-60 KHz, single frequency or double frequency or triple frequency can be selected, the power is 60-300 W, the ultrasound temperatureis 20-40 DEG C, and after treatment is conducted for 5-45 min, the coffee leaves are subjected to standing treatment at 26-28 DEG C; freeze-drying, crushing and filtering with a screen are performedto obtain enriched coffee leaves; according to the method, the content of gamma aminobutyric acid in the coffee leaves is increased to 2.6 times, and the ACE inhibitory activity of the enriched coffeeleaves is increased by 37.6%; the process is simple, the obtained coffee leaf powder can be used for preparing antihypertensive beverages, and high-valued processing of coffee leaves is achieved.

The invention discloses a protein tyrosine phosphatase selective inhibitor and a preparation method thereof, and relates to the field of protein tyrosine phosphatase inhibition. The protein tyrosine phosphatase selective inhibitor is a functionalized carrier-protein tyrosine phosphatase selective ligand-vanadium coordination compound, can be used for preparing drugs for treating diabetes, tumors or obesity, can reduce the effective use concentration while improving the enzyme inhibition activity, and does not generate adverse reaction to the body. The preparation method comprises the following steps: mixing a vanadium compound with a protein tyrosine phosphatase selective ligand, and loading the obtained compound onto a functional carrier to form a functional carrier-protein tyrosine phosphatase selective ligand-vanadium coordination compound.

The invention provides an ATX inhibitor as well as a preparation method and application thereof. The ATX inhibitor is a compound with a structure shown in a formula I or pharmaceutically acceptable salt, ester, isomer, solvate, prodrug or isotope label of the compound. Compared with an existing ATX inhibitor GLPG-1690, the ATX inhibitor disclosed by the invention has higher inhibition activity, and has excellent medicine effect, in-vitro/in-vivo pharmacokinetics and safety and a good clinical application prospect.

The invention belongs to a marine chemical engineering technology, and particularly relates to a novel 6-oxadiazole/thiadiazole chitooligosaccharide derivative and a preparation and application thereof. The derivative is shown as a general formula I, and in the formula I, X is O or S and n is 2-10. The derivative disclosed by the invention has relatively good solubility, a novel structure and verystrong bacterium killing capability.

The invention belongs to the technical field of active peptides, and particularly relates to a composite ACE inhibitory peptide with a synergistic effect and a preparation method and application thereof. The pea peptide and the corn peptide are compounded according to the ratio of 1: (0.75-1), and the ACE activity of the pea peptide and the ACE activity of the corn peptide are synergistic. The result of the embodiment shows that the IC50 value of the composite ACE inhibitory peptide is 0.547-0.636 mg/mL and is obviously superior to that of single pea peptide and single corn peptide under the same concentration, the composite ACE inhibitory peptide has good ACE inhibitory activity, the content of essential amino acid is high, the composite ACE inhibitory peptide can be better absorbed and utilized by human bodies, and the utilization rate of pea protein and corn protein is increased.

The invention discloses resveratrol carbon quantum dots as well as a preparation method and application thereof. The resveratrol carbon quantum dots are prepared by a resveratrol Res pyrolysis method, can enhance the inhibitory activity of pyocyanin, change the phospholipid composition of a cell membrane and inhibit the expression of fatty acid synthesis related genes, and has an application prospect in preparation of drugs for resisting pseudomonas aeruginosa infection.

A nitrogenous heterocyclic compound, a preparation method, an intermediate, a composition, and an application. The present invention provides a nitrogenous heterocyclic compound as represented by formula I, pharmaceutically acceptable salts thereof, enantiomers thereof, diastereoisomers thereof, tautomers thereof, solvates thereof, metabolites thereof, or prodrugs thereof. The compound has high inhibitory activity against ErbB2 tyrosine kinase, has good inhibitory activity against human breast cancer cells BT-474, human gastric cancer cells NCI-N87 and the like with high expression of ErbB2, and in addition has relatively weak inhibitory activity against EGFR kinase, that is, the compound is an EGFR/ErbB2 double target inhibitor that attenuates EGFR kinase inhibitory activity or a small-molecule inhibitor having selectivity for an ErbB2 target. (I)

The invention relates to a triazolotetrazine compound containing morpholine and quinoline rings as well as a preparation method and application thereof, and belongs to the technical field of medicine synthesis. The invention aims to provide a novel anti-tumor compound, and provides a triazolotetrazine compound containing morpholine and quinoline rings as well as a preparation method and application thereof. The preparation method of the triazolotetrazine compound comprises the steps that inorganic strong base, glycollic acid and 4-chloroquinoline are subjected to a reaction, and after the reaction is finished, the reaction system is adjusted to be acidic; and a reaction is carried out on an intermediate and 4-(6-hydrazino-1, 2, 4, 5-tetrazine-3-yl) morpholine under the action of a condensing agent, and then a cyclization reaction is carried out under the action of phosphorus oxychloride to obtain the triazolo tetrazine compound containing morpholine and quinoline rings, wherein the triazolo tetrazine compound can be used for preparing drugs or functional foods for treating and resisting tumors. The compound has the advantages of inhibition activity on c-Met kinase, in-vitro anti-tumor activity, short reaction route and easiness in operation.

The invention belongs to the field of natural medicinal chemistry, and particularly relates to a preparation method of N-methyl-2,3,7,8-tetrahydroxy benzophenanthridine quaternary ammonium salt used for inhibiting DDC (dopa decarboxylase), and application of the N-methyl-2,3,7,8-tetrahydroxy benzophenanthridine quaternary ammonium salt to pharmacy. The DDC is also called as aromatic amino acid decarboxylase; mammal enteric microorganism and self secreted DDC can catalyze aromatic amino acid to generate decarboxylated degradation in intestinal tracts and peripheral tissues; the absorption and utilization rate of the aromatic amino acid is reduced. Compared with a commercial DDC inhibiter, the prepared N-methyl-2,3,7,8-tetrahydroxy benzophenanthridine quaternary ammonium salt has a fire-new DDC inhibition mechanism.

The invention relates to a naphthyridine derivative which can be used for inhibiting monoamine oxidase (MAO), and particularly can be used for selectively inhibiting MAO-B. The compound has development and application prospects, and can be used for treating brain injury, cerebral apoplexy, traumatic brain injury, anxiety disorder, mood disorder, autism, vascular dementia, Alzheimer's disease and other diseases.