63results about How to "Dose-dependent improvement" patented technology

The invention to insecticide with folium and atractylodes extract as active ingredients. The insecticide is composed of folium and atractylodes extract and organic dissolvent. The volume ratio of folium extract and atractylodes extract is 1:(2-10). The concentration of the mixture of folium and atractylodes extract in the organic dissolvent is 0.3v / v%-12.0v / v%. The insecticide has a kill effect over national standard B level, evident dose dependence, and good helminthicide.

The invention relates to 4-cycloaminoalkoxy-3-methoxycinnamates, and a preparation method and application thereof. The preparation method is characterized by comprising the following steps: 1. preparing ferulic acid acyl chlorides from the initial raw material ferulic acid under the conditions of a first solvent and an acylating agent; 2. carrying out reaction on the ferulic acid acyl chlorides and alcohol or phenol in a second solvent under the first alkaline condition to obtain corresponding ferulates; and 3. carrying out reaction on the ferulates and 1-substituted-4-chloroalkylpiperidine in a third solvent under the second alkaline condition to generate the 4-cycloaminoalkoxy-3-methoxycinnamates. The compounds have favorable effects on treating and / or preventing neurodegeneration related diseases, including but not limited to vascular dementia, Alzheimer's disease, Parkinson's disease, Huntington's disease, HIV (human immunodeficiency virus) related dementia, multilocular sclerosis, progressive lateral spinal sclerosis, neuropathic pains, glaucoma and the like.

The invention belongs to the technical field of organic synthesis and particularly relates to a cyclamine alkylamide ferulate compound as well as a preparation method and application thereof. The preparation method comprises the following steps: enabling potassium phthalimide serving as a start raw material to react with 1-substituted-4-haloalkyl piperidine under the effects of a solvent and alkali to obtain a phthalimide alkylamine compound; performing hydrazinolysis of the phthalimide alkylamine compound and hydrazine hydrate to obtain a primary amine compound; and adding ferulic acid, a condensing agent and a solvent into the primary amine compound for a condensation reaction to obtain a product of cyclamine alkylamide ferulate compound. The cyclamine alkylamide ferulate compound provided by the invention is of a simple chemical structure, the chemical reactions in the preparation process are thorough, the product yield is high, the operation is convenient, the cost is low, and the product can be used for perfectly treating the neurodegenerative diseases.

The invention successfully screens a virus strain VR18 suitable for building an animal model of CA16 infection and builds the animal model of the CA16 virus infection by infecting a suckling mouse with the virus strain VR18. The invention also relates to a method for building the animal model of the CA16 injection and the use of the virus stain VR18 in the building of the animal model of the CA16infection and the like. The method provides valuable experiment data for study on CA16 vaccines.

The invention relates to 4-amino alkoxy-3-methoxy cinnamic acid benzamide compounds as well as preparation methods and applications thereof. The preparation methods of the compounds comprise the following steps: step 1, ferulic acid is taken as a starting material and subjected to a reaction with substituted aniline under the conditions of a first solvent and a condensing agent, and corresponding ferulic acid benzamide compounds are obtained; step 2, the ferulic acid benzamide compounds are subjected to a reaction with a dihalogenated alkyl compound under the condition of a second solvent and a first alkaline condition, and a corresponding halogen compounds are obtained; step 3, the halogen compounds are subjected to a reaction with an organic amine compound under the condition of a third solvent, and the 4-amino alkoxy-3-methoxy cinnamic acid benzamide compounds are obtained. The compounds have a remarkable inhibiting effect on acetylcholinesterase, the IC50 is 0.01 mu M-5 mu M, and the inhibitory activity on acetylcholinesterase is greatly higher than that on butyrylcholinesterase, so that the compounds have certain selective inhibiting effect on acetylcholinesterase.

The invention relates to a 4-cyclamine alkoxy-3-methoxyl cinnamic acid benzamide compound, a preparation method and application of the compound.The chemical structure general formula of the compound is shown as a formula (I) (please see the formula in the description), wherein m represents 1-12, R1 represents C1-C12 alkyl or benzyl or substituted benzyl, X represents C1-C12 alkyl or benzyl or substituted benzyl, phenyl of which a benzene ring is substituted with 1-4 groups selected from F, Cl, Br, I, C(1-4) alkyl, C(1-4) alkoxy, trifluoromethyl, trifluoromethoxy, nitryl, a cyano group, and the substituent groups can be located at any position of the benzene ring.Accordingly, the compound has the significant inhibiting effect on acetylcholinesterase, the IC50 of the compound is 0.01-5 micromoles per liter, the inhibiting activity on acetylcholinesterase is greatly higher than the inhibiting activity on butyrylcholine esterase, and therefore the compound has the certain selective inhibiting effect on acetylcholinesterase.

An application of schisandrin A in treating the drug-resistant tumor is disclosed. It can be used in conjunction with antineoplastic for increasing the sensitivity of tumor to antineoplastic.

The invention belongs to the technical field of organic synthesis and particularly relates to a 4-carbamate-3-methoxy cinnamate benzamide compound as well as a preparation method and use thereof. The preparation method comprises the following steps: by utilizing ferulic acid as a starting raw material to react with substituted aniline in the presence of a solvent and a condensing agent, so as to obtain corresponding ferulic acid benzamide compounds; carrying out acylation reaction on the ferulic acid benzamide compounds and a corresponding acylating agent acyl chloride in the presence of a proper solvent under an alkaline condition, so as to obtain the product 4-carbamate-3-methoxy cinnamate benzamide compound. The 4-carbamate-3-methoxy cinnamate benzamide compound has the advantages that the structure is simple, the reaction is thorough, the product yield is high, the operation is convenient, the cost is low, and neurodegenerative diseases such as vascular dementia, Alzheimer's disease, Parkinson's disease, Huntington's disease, HIV-related dementia, multiple sclerosis, progressive spinal lateral sclerosis, neuropathic pain, glaucoma and the like can be well treated.

The invention discloses the application of dioscin to the preparation of a renal injury protection medicament. Dioscin has a renal injury protection effect, and can be used for preparing the renal injury protection medicament. Dioscin has an obvious lowering effect on NO (Nitric Oxide), TNOS (Total Nitric Oxide Synthase), iNOS (Inducible Nitric Oxide Synthase), MDA (Malondialdehyde), BUN (Blood Urea Nitrogen) and SCr (Serum Creatinine) rise caused by renal injury, has an obvious increasing effect on the reduction of SOD (Superoxide Dismutase), GSH (Glutathione), GSH-Px (Glutathione Peroxidase) and CAT (Catalase) relative to a Model group, and is dose-dependent. After the intervention of dioscin, the phenomena of large-area renal tubular epithelial cell swelling, brush border disappearance, degenerative necrosis of a part of epithelial cells, blockage of lumens by necrotic and exfoliative cellular debris and the like, which are caused by renal injury are obviously alleviated. Dioscin can be used for preparing a medicinal preparation as an active ingredient according to clinical medication needs. Dioscin has the advantages of safety (no toxic or side effects), effectivity, economy, practicability and the like.

The invention discloses triptolide and application of composition of triptolide to preparation of medicine for resisting esophageal cancer. A research proves that the triptolide has an obvious inhibition effect on proliferation of human esophageal cancer cells, represents the obvious dose dependence and has the prospect that the triptolide is developed and prepared into the medicine for resistingthe esophageal cancer. The triptolide and natural compound erianin having the effect of resisting the esophageal cancer also have the effect of cooperatively inhibiting the proliferation of the humanesophageal cancer cells, and therefore, the triptolide and the erianin can be prepared into a medicine composition for chemotherapy of the human esophageal cancer.

The invention relates to application of 3,15-dicarbonyl gibberellic acid methyl ester (GA) in reversing tumor multidrug resistance. A compound GA provided in the invention has favorable activity on the reversing tumor multidrug resistance (MDR), the GA acting on K562 / A02 has higher drug susceptibility and can obviously reverse the drug resistance of the K562 / A02 for ADM (Archer Daniels Midland); the effect mechanism of the GA for reversing the multidrug resistance of K562 / A02 cells is realized by increasing the contents of chemotherapeutic drugs in the drug-resistance cells to prevent the chemotherapeutic drugs from being discharged outwards and promote the apoptosis of the drug-resistance cells, and has no obvious relevance with the expression of down-regulated drug-resistance genes mdr-1, thereby prompting that the action mechanism of the GA is relevant to the outward discharging pump function of inhibiting the drug-resistance cells P-gp and inducing the apoptosis of the drug-resistance cells; and the compound GA has lower toxicity, and therefore the compound GA has favorable application prospect on clinical tumor chemotherapy and particularly on resisting clinical tumor drug resistance.

The invention provides an application of notoginseng saponins Rg 1 in preparing medicine for treating pulmonary interstitial fibrosis. Pharmacological experiments show that if in vitro, the notoginseng saponins Rg 1 can inhibit the activity of human embryonic lung fibroblast and has good dose-dependent; if in vivo, the notoginseng saponins Rg 1 can decrease the lung coefficientand the lung hydroxyproline content of a mouse with pulmonary interstitial fibrosis; the notoginseng saponins Rg 1 can also reduce the pulmonary alveolitis and the degree of pulmonary interstitial fibrosis of the mouse with pulmonary interstitial fibrosis; the raw materials of the notoginseng saponins Rg 1 are easy to obtain, and can be prepared into various common dosage forms such as tablets, capsules, and injections; and the preparation method is simple.

The invention belongs to marine functional food and particularly relates to marine functional food capable of inhibiting prostatic cancer. The marine functional food belongs to a squid ink polypeptide active matter prepared through extracting squid ink by an acid method. A specific method comprises the steps that hydrochloric acid is added into the preprocessed squid ink, the leaching is carried out under the conditions that the hydrochloric acid concentration is 0.02 to 0.03 mol / L, the acid lifting material liquid ratio (the volume ratio of double distilled water to raw material squid ink) is 1:(1-2), the acidolysis time is 2 to 3 hours, the acidolysis temperature is 35 DEG C to 40 DEG C, finally, the leaching liquid is centrifuged to obtain clear liquid, and the obtained clear liquid is the coarse squid ink polypeptide active matter. Rich marine biological squid ink is adopted, the squid ink polypeptide is purified by methods of acid method extraction, concentration and the like, in addition, the optimal acidolysis process is obtained through an orthogonal test, and the most squid ink polypeptide active matters are obtained. CCK-8 method detection shows that the squid ink polypeptide has the obvious proliferation inhibition effect on DU-145 and PC-3 cells of the prostatic cancer, can inhibit the DU-145 and PC-3 cell proliferation and can induce the apoptosis of the cells, so the prostatic cancer is inhibited.

The invention relates to a 4-amine alkoxy-3-methoxyl cinnamic acid ester compound, a preparation method and application of the compound.The preparation method of the compound comprises the following steps that 1, a ferulic acid acyl chloride compound is obtained by taking ferulic acid as a staring material under the condition of in first solvent under the condition of an acylating agent; 2, the ferulic acid acyl chloride compound reacts with alcohol or phenol in second solvent under a first alkaline condition to obtain a corresponding cinnamic acid ester compound; 3, the cinnamic acid ester compound reacts with a dihalogen alkyl compound in third solvent under a second alkaline condition to generate a corresponding halogen compound; 4, the halogen compound reacts with an organic amine compound in fourth solvent to obtain the 4-amine alkoxy-3-methoxyl cinnamic acid ester compound.Accordingly, the compound has the significant inhibiting effect on acetylcholinesterase, the inhibiting activity on acetylcholinesterase is greatly higher than the inhibiting activity on butyrylcholine esterase, and the certain selective inhibiting effect on acetylcholinesterase is achieved.

The invention discloses bio-pharmaceutical application of three eupnane triterpenes to preparation of a Gli gene inhibitor and a medicine for preventing and curing the liver cancer. The bio-pharmaceutical application finds that Meliasenins B, C and D obviously inhibit the propagation of a HepG2 cell by inhibiting the expression of genes Gli1 and Gli2, the inhibition effect shows obvious dose dependence, and the Meliasenins B, C and D are effective inhibitors of the genes Gli1 and Gli2 and can be used to prepare the medicine for preventing and curing the liver cancer. The technician in the field knows that inhibiting the expression of the genes Gli1 and Gli2 is a relatively mature anti-cancer molecule passage, and the Meliasenins B, C and D play a role in resisting the liver cancer right through the passage. The bio-pharmaceutical application also finds that the naringenin reduces the toxicity of the Meliasenins B, C and D on the normal liver cell of people, but does not affect the toxicity of the Meliasenins B, C and D on the liver cancer cell.

The invention belongs to the field of pharmacy and particularly relates to application of ginkgoneolic acid in preparing medicines for treating immunological diseases. The application of ginkgoneolic acid in preparing medicine for treating immunological diseases can be used for declaring a new drug in class 1 of chemical medicines particularly in terms of treating in immunological enteritis and widens the application of the compound .

The invention discloses a preparation method and use of a compound with A beta aggregation inhibition activity and belongs to the field of microbial medicines. The compound with A beta aggregation inhibition activity is shown in the structural formula I and is prepared from streptomycete X210408 with a preservation number of CCTCC NO: M 2015103 by fermentation and separation. The compound shown in the structural formula I has A beta aggregation inhibition activity and good dosage dependence. The compound can be used for preparation of an A beta aggregation inhibitor and can be used for preparing drugs for treating Alzheimer's disease and other types of dementia. The compound provides a novel approach for treating Alzheimer's disease.

The invention provides a composite of breviscapinum and panax notoginseng saponins Rg1 for treating pulmonary fibrosis, wherein the weight ratio of the breviscapinum to the panax notoginseng saponins Rg1 is 2-5:1-2. The invention also provides application of the composite in the preparation of a medicament for treating the pulmonary fibrosis. The composite of the breviscapinum and the panax notoginseng saponins Rg1 is formulated in a certain proportion and has the advantages of favorable pulmonary fibrosis resistance, remarkable effect and little side effects. Raw materials of the composite are easily obtained and can be prepared in various common dosage forms, such as tablets, capsules, injections and the like, through a conventional method with simple preparation method. The pharmacological action of the composite is obvious; in vitro, the composite can inhibit the activity of human embryonic lung fibroblasts and has favorable dosage dependence; and in vivo, the composite can lower the lung coefficient of a mouse with the pulmonary fibrosis and the content of hydroxyproline of lung tissues and also relieve the alveolitis of the mouse with the pulmonary fibrosis and reduce the degree of the pulmonary fibrosis.

The invention discloses biomedical application of triptonide to preparation of a Gli gene inhibitor and a liver cancer prevention and control drug. The invention finds out that the triptonide can be used for remarkably inhibiting proliferation of liver cancer cells through inhibiting expression of Gli1 and Gli2 genes and the inhibition effect has remarkable dosage dependence; the triptonide is aneffective inhibitor of the Gli1 and Gli2 genes and can be used for preparing the liver cancer prevention and control drug. The technicians in the field know that the expression of the Gli1 and Gli2 genes is a relatively developed anti-cancer molecular pathway and the triptonide plays a role of resisting liver cancer through the pathway. Meanwhile, the triptonide is the effective inhibitor of the expression of the Gli1 and Gli2 genes; the triptonide also can be used for preparing drugs for treating diseases related to high expression of the Gli1 and Gli2 genes.

The invention discloses a cell line method pyrogen detection method and a kit. The method includes following steps: (1) a pyrogen material standard solution and a to-be-detected sample solution is prepared; (2) the pyrogen material standard solution or the to-be-detected sample solution are respectively added into a HL-60 cell-containing cell culture solution for culture, and cultured cell supernatant is taken; and (3) the content of cytokine IL-6 in the cultured cell supernatant of the step (2). According to the method, human body pyrogen reaction can be simulated, Gram-negative bacterium sourced, Gram-positive bacterium sourced and yeast sourced pyrogen materials can be qualitatively and quantitatively analyzed, sensitivity is high, and the method is simple and easy. The kit includes the pyrogen material standard solution, a cytokine IL-6 detection agent and HL-60 cells, the kit has the advantages of simple operation, capability of pyrogen material qualitative and quantitative analysis, and high sensitivity.

The invention discloses application of baicalein in preparation of a medicine for treating malignant mesothelioma. According to the application, tests discover that the baicalein can be used for treating the malignant mesothelioma through inhibiting the migration, invasion and propagation of malignant mesothelioma cells and inducing apoptosis of the malignant mesothelioma cells, has obvious dose dependence and can be developed into the medicine for treating the malignant mesothelioma. According to the application, it is further discovered through the tests that the baicalein can be used for strengthening the sensitivity of the malignant mesothelioma cells to chemotherapeutics (cisplatin), so that the antitumor effect is strengthened, the dose of the chemotherapeutics is reduced, and toxicor side reactions are reduced.

The invention relates to 6-(pyridine-4-yl)-4-substituted amino quinazoline and quinoline compounds having PI3K inhibitory activity, which are compounds of formula (I) structure (as shown in the description), or solvates, enantiomers, diastereoisomers, tautomers or any-ratio mixtures of their pharmaceutically acceptable salts, including racemic mixtures. The 6-(pyridine-4-yl)-4-substituted amino quinazoline and quinoline compounds have good inhibitory action against PI3K, show good antitumor effect, and has a good prospect in the preparation of drugs for treatment of diseases responsive to PI3Kalpha and / or PI3K delta. The invention also relates to pharmaceutical application of the compounds as PI3K inhibitors.

The invention relates to 4-cycloaminoalkoxy-3-methoxycinnamates, and a preparation method and application thereof. The preparation method is characterized by comprising the following steps: 1. preparing ferulic acid acyl chlorides from the initial raw material ferulic acid under the conditions of a first solvent and an acylating agent; 2. carrying out reaction on the ferulic acid acyl chlorides and alcohol or phenol in a second solvent under the first alkaline condition to obtain corresponding ferulates; and 3. carrying out reaction on the ferulates and 1-substituted-4-chloroalkylpiperidine in a third solvent under the second alkaline condition to generate the 4-cycloaminoalkoxy-3-methoxycinnamates. The compounds have favorable effects on treating and / or preventing neurodegeneration related diseases, including but not limited to vascular dementia, Alzheimer's disease, Parkinson's disease, Huntington's disease, HIV (human immunodeficiency virus) related dementia, multilocular sclerosis, progressive lateral spinal sclerosis, neuropathic pains, glaucoma and the like.

The invention discloses biomedical application of ophiobollin to preparation of a Gli gene inhibitor and a liver cancer prevention and treatment drug. The invention discovers that ophiobollin A and Cand 6-epi-ophiobolin N can significantly inhibit the proliferation of liver cancer cells through inhibiting Gli1 and Gli2 gene expression, and the inhibiting effect shows an obvious dosage dependence;the ophiobollin A and C and the 6-epi-ophiobolin N are effective inhibitors for Gli1 and Gli2 genes and can be used for preparing the liver cancer prevention and treatment drug. Technical personnel in the field know that the inhibition of the Gli1 and Gli2 gene expression is a more mature anticancer molecular pathway, and the ophiobollin A and C and the 6-epi-ophiobolin N play an anti-cancer rolethrough the pathway. The prior art does not disclose research results of the invention.

The invention is directed at a method for predicting a patient's responsiveness to a CHK1 inhibitor. The method includes providing a sample from a test patient who is being treated with a DNA damaging agent; and determining for the presence of an activated CHK1 signal transduction pathway molecule, wherein the presence of an activated CHK1 signal transduction pathway molecule is indicative that a CHK1 inhibitor should be administered to the patient.

The invention discloses application of nobilonine in preparing drugs for resisting multiple myeloma; the test result shows that the nobilonine can effectively inhibit the proliferation of human multiple myeloma cell, has obvious dose dependence, and can be developed into a drug for resisting human multiple myeloma.

The invention discloses a compound with antiviral activity and a preparation method and application of the compound. The compound has a structure shown in a formula (I) and can be prepared and obtained by fermentation and separation of a mutant strain with the deletion of the enterocin gene cluster of Streptomycete qinglanensis 1772205. A high-resolution mass spectrum and a nuclear magnetic resonance spectrum technology are adopted to confirm the structure of the compound. The compound with a structure shown as in the formula (I) has relatively strong antiviral activity and can be used for preparing medicines for treating viruses.

The invention provides the application of notoginseng saponin Rg1 in the preparation of medicine for treating pulmonary interstitial fibrosis. The present invention has been verified by pharmacological tests that notoginseng saponin Rg1 can inhibit the activity of human embryonic lung fibroblasts in vitro, and has a good dose dependence; in vivo, it can reduce the lung coefficient and lung tissue hydroxyprophylaxis in mice with pulmonary interstitial fibrosis. It can also reduce the degree of alveolitis and pulmonary fibrosis in mice with pulmonary interstitial fibrosis; and the raw material of notoginseng saponin Rg1 is easy to get, and can be made into various commonly used dosage forms by conventional methods, such as tablets, Capsules, injections, etc., the preparation method is simple.

The invention discloses a cell line method pyrogen detection method and a kit. The method includes following steps: (1) a pyrogen material standard solution and a to-be-detected sample solution is prepared; (2) the pyrogen material standard solution or the to-be-detected sample solution are respectively added into a HL-60 cell-containing cell culture solution for culture, and cultured cell supernatant is taken; and (3) the content of cytokine IL-6 in the cultured cell supernatant of the step (2). According to the method, human body pyrogen reaction can be simulated, Gram-negative bacterium sourced, Gram-positive bacterium sourced and yeast sourced pyrogen materials can be qualitatively and quantitatively analyzed, sensitivity is high, and the method is simple and easy. The kit includes the pyrogen material standard solution, a cytokine IL-6 detection agent and HL-60 cells, the kit has the advantages of simple operation, capability of pyrogen material qualitative and quantitative analysis, and high sensitivity.