71results about How to "Inhibitory function" patented technology

This disclosure concerns novel quinazoline compounds of Formula (I) as defined in the specification and compositions comprising such novel compounds. These compounds are useful anticancer agents, especially in inhibiting the function of the EGF receptor tyrosine kinases, HERl tyrosine kinase, and HER2 tyrosine kinase. Thus, the disclosure also concerns a method of treating hyperproliferative diseases or conditions, such as various cancers and benign prostate hyperplasia (BPH), by use of these novel compounds or a composition comprising such novel compounds.

The acidifying agent as fodder additive is compounded with several kinds of organic acid with lactic acid as main component and / or organic acid salt, and features that it has total organic acid amount of 45-53 wt% and silica hydrate as carrier. The acidifying agent has good compatibility and strong acidifying effect, and its coated product has no corrosion and harm, and no destruction to protein and vitamins and may be mixed well with various feed components.

The invention discloses the application of schisandrin B in the preparation of tumor treating drugs, especially in the preparation of tumor cell multidrug resistance reversal agents and tumor chemotherapy drugs. The compound can also be used in combination with other drugs to further improve the reversal effect. Schizandrin B can effectively reverse the multidrug resistance of tumors. The compound acts on P-glycoprotein and can completely inhibit the function of P-glycoprotein, so it has clinical application significance; in addition, Schizandrin B has low toxicity, but It is toxic to certain tumor cells, so Schizandrin B has good application prospects in clinical tumor chemotherapy, especially as a drug for reversing multidrug resistance of tumor cells.

The present invention relates to a fusion protein consisting of an extracellular domain of PD-L1 and a modified immunoglobulin Fc region. The extracellular domain of PD-L1 and a fragment thereof have an excellent immunomodulatory function, and can be used as a drug for immunomodulation when coupled to a modified immunoglobulin Fc region. Accordingly, the PD-L1 fusion protein according to the present invention has been proven to have an excellent effect in inflammatory bowel disease, colitis, psoriasis, asthma, and arthritis disease models, and thus can be used very effectively in treatment of said diseases.

The invention provides Fu moxibustion traditional Chinese pharmaceutical oil and a preparation method thereof. The traditional Chinese pharmaceutical oil is prepared from the following raw materials in parts by weight: 2 to 8 parts of cortex cinnamomi oil, 5 to 10 parts of wintergreen oil, 5 to 10 parts eucalyptus oil, 1 to 5 parts of mint oil, 1 to 5 parts of rose oil, 1 to 5 parts of lavender oil, 2 to 8 parts of rhizoma acori graminei oil, 2 to 8 parts of clove oil, 1 to 5 parts of ginger oil, and 2 to 8 parts of ethyl alcohol. The Fu moxibustion traditional Chinese pharmaceutical oil has the effects of dispelling the wind, invigorating the blood circulation, dispelling cold, diminishing inflammation, relieving pain, quieting the heart, soothing the nerves and calming. Based on the yin-yang theory in the traditional Chinese medicine theory, the drug effects can be quickly played through exhaling, exterior syndrome relieving and warming of the externally applied drug. Due to the action of the ethyl alcohol, the drug can quickly penetrate through skin and permeate into muscular striae, and the effects of dispelling the wind, invigorating the collateral, diminishing inflammation and relieving pain can be obtained. The kind of medium medicine can dispel cold through warmness to achieve the effects of dispelling the wind, removing cold, clearing heat, diminishing inflammation, invigorating the blood circulation, activating meridians and relieving pain.

The invention discloses a docetaxel nanometer micelle, a preparation method and application of the micelle to prepare medicines for treating tumor or drug-resistant tumor. The docetaxel nanometer micelle comprises 1 part by weight of docetaxel, 10-100 parts by weight of a carrier material and 0-10 parts of oil, wherein the average particle size of the docetaxel nanometer micelle is 10-200 nm. According to the preparation, the water solubility of docetaxel is substantially improved, the stability of the preparation is improved, the cycling time of docetaxel in blood is prolonged, the toxic and side effects of conventional preparations are reduced, docetaxel nanometer micelle can be driven to be targeted to tumor tissue through EPR effect, so that the anti-tumor curative effect of docetaxel is improved, and the docetaxel nanometer micelle overcomes the multidrug resistance of tumor.

The invention relates to a composite microsphere for co-loading adriamycin nanoparticles and ginsenoside rh2 and a preparation method thereof, wherein the preparation method comprises the following steps: (1) preparing adriamycin hydrochloride and a nanoparticle carrier material into doxorubicin polyelectrolyte nanoparticles; (2) dispersing the adriamycin polyelectrolyte nanoparticles in water toform a nano-particle suspension, and dispersing the nano-particle suspension in an organic solution containingginsenoside rh2 and a high-molecular polymer to prepare S / W1 / O colostrum; (3) adding the S / W1 / O colostrum into an aqueous solution containing an emulsifier to prepare S / W1 / O / W2 complex milk; (4) solidifying the S / W1 / O / W2 complex emulsion into microspheres, collecting the microspheres, washing and drying. The microsphere prepared by the method can achieve the sequential release, slow release of doxorubicin hydrochloride and ginsenoside rh2,and has the advantages of low burst release rate and high encapsulation rate.

The invention relates to a medicament which is a Chinese traditional medicine composition preventing and treating osteoporosis, also to a preparation method thereof, belonging to the technical field of medicament. The medicament is mainly made from 25-40% of rhizoma drynariae, 20-35% of barrenwort, 10-25% of radix achyranthis bidentatae, 10-25% of eucommia and 5-15% of antler sheets. The preparation processes are weighing rhizoma drynariae, barrenwort, radix achyranthis bidentatae, eucommia and antler sheets, sequentially extracting radix achyranthis bidentatae with alcohol and filtering to obtain filtrate I and dregs, decocting dregs, rhizoma drynariae, barrenwort and antler sheets with water, filtering to obtain filtrate II, combining the filtrate I and II, and concentrating to make into liquid medicine containing active components. The Chinese traditional medicine formulation provided by the invention has low side effect and relatively good effect on preventing and treating primary osteoporosis.

The invention belongs to the fields of gene functions and applications, and specifically discloses an application of an FKBP11 gene in prevention and treatment of aortic dissection. In-vitro cell experiments show that vascular endothelial cell SiRNA-mediated FKBP11 gene silencing can inhibit activation of an NF-kB signal pathway, the expression of a proinflammatory cytokine is decreased, and migration of macrophage to an aortic middle layer is inhibited, so that the degradation of a middle-layer substrate is inhibited, and results show that the FKBP11 inhibitor can prevent and treat occurrenceof aortic dissection, and provides theoretical basis and clinical basis for new targets and new strategies for prevention, relieving and / or treatment of aortic dissection.

The invention provides a traditional Chinese medicine composition for treating intercostal neuralgia and a preparation method of the traditional Chinese medicine composition. The traditional Chinese medicine comprises the following internal medicines in parts by weight: 10-20 parts of angelica sinensis, 10-20 parts of astragalus membranaceus, 10-20 parts of root of red-rooted salvia, 10-20 parts of peach kernel, 10-20 parts of flowers carthami, 10-20 parts of rhizoma cyperi, 10-20 parts of radix paeoniae alba, 10-20 parts of caulis spatholobi, 10-20 parts of ligusticum wallichii, 10-20 parts of radix rehmanniae preparata, 10-20 parts of citrus chirocarpus, 10-20 parts of curcuma zedoary, 10-20 parts of large-leaved gentian, 10-20 parts of radix bupleuri, 10-20 parts of radix curcumae and 10-20 parts of inula flower, and the following external medicines in parts by weight: 10-20 parts of caulis spatholobi, 10-20 parts of ligusticum wallichii, 10-20 parts of roots of common peony, 10-20 parts of radices sileris, 10-20 parts of rhizoma bletillae, 10-20 parts of radix angelicae, 10-20 parts of angelica sinensis, 10-20 parts of corydalis tuber, 10-20 parts of tenuifolia, 10-20 parts of roots of red-rooted salvia, 10-20 parts of radix clematidis, 10-20 parts of ground beeltle and10-20 parts of earthworm. The traditional Chinese medicine composition disclosed by the invention is reasonable in compatibility of medicines, and has strong and lasting anti-inflammatory action, the infectious and infectious inflammations can be restricted, congestion is relieved, the permeability of a blood capillary is reduced, reaction of inflammatory cells and the like is restricted, the function of phagocyte is restricted, a lysosome membrane is stabilized, alexin can be prevented from participating into inflammatory response, and tissue damage repair after inflammation is restricted.

An application of the biphenyl cyclooctadiene lignan in preparing the medicine for treating tumor by poisoning the tumor cells and reversing the resistance of tumor cells to multiple medicines is disclosed.

The invention relates to the discovery that 3-deoxyglucosone (3DG) and other alpha-dicarbonyl sugars associated diseases and disorders are present and produced in the skin. Further, the invention relates to the discovery that amadorase, an enzyme that mediates 3DG synthesis, is also present in the skin. Thus, the invention further relates to methods of inhibiting production and function of 3-deoxyglucosone and other alpha-dicarbonyl sugars in skin thereby treating or prevention various diseases, disorders or conditions. Additionally, the invention relates to treatment of various diseases, disorders or conditions associated with or mediated by oxidative stress since 3DG induces ROS and AGEs, which are associated with the inflammatory response caused by oxidative stress.

The invention discloses a slow virus vector. Preparation and application of the slow virus vector comprise the following steps: firstly, aiming at a FoxP3 gene sequence of a mouse, designing specific short hairpin RNA which comprises a sense strand and an antisense strand, and then carrying the short hairpin RNA into pENTR / U6 plasmids; then using a Lenti virus shRNA expression vectors system to carry out slow virus package in 293 FT cells to obtain the slow virus vector carried with the short hairpin RNA; and introducing the slow virus vector carried with the short hairpin RNA into Treg cells of CD4+CD25+ so as to reduce the function of the Treg cells and inhibit the growth of melanoma.

The invention discloses a vector for carrying out site-specific mutagenesis on MSTN (Myostatin) and site-specific integration on PPARgamma (Peroxisome Proliferator-activated Receptor gamma) at the same time, and recombinant cells. The vector comprises a Cas9 cutting expression vector and a targeting vector. According to the vector disclosed by the invention, a recombinant cell strain can be constructed by carrying out co-transfection on host cells by the Cas9 cutting expression vector and the targeting vector, the recombinant cell strain can be used as nuclear transfer donor cells for producing transgenic cloned embryo, function exertion of the MSTN can be inhibited, and meanwhile, specific expression of the PPARgamma in skeletal muscle cells can be realized, so that support is provided for quickly and efficiently developing high-quality transgenic beef new products.

The present invention discloses an application of artesunate in preparation of a drug for inhibiting tumor cell drug resistance, and at the same time discloses a pharmaceutical preparation prepared from the artesunate and a method for inhibiting the tumor cell drug resistance in vitro. Experiments show that lysosomal functions have a certain relationship with the tumor cell drug resistance and areone of mechanisms of the tumor cell drug resistance. The artesunate can inhibit the lysosomal functions, increases lysosomal pH, decreases lysosomal enzyme activity, reduces elimination of disablingmitochondria, and thus induces cell apoptosis. Therefore, the artesunate has a better cytotoxic effect on the drug resistance cells with the higher lysosomal functions, can be used as the drug for inhibiting the tumor cell drug resistance and is used for adjuvant treatment of tumors.

A method for removing bacteria of chlamydomonas reinhardtii through kresoxim-methyl, ampicillin and cefotaxime mixed antibacterial agents comprises the following steps: inoculating mixed and pollutedchlamydomonas through a TAP solid culture medium flat plate, and culturing; preparing a mixed antibacterial agent flat plate which is a TAP solid culture medium in which kresoxim-methyl, ampicillin and cefotaxime are added, and waiting for later use; transferring and marking the mixed and polluted chlamydomonas which is cultured on the TAP solid culture medium to the antibacterial agent mixed TAPsolid culture medium flat plate for culturing; and transferring and marking the antibacterial chlamydomonas from the antibacterial flat plate to a common TAP solid culture medium flat plate to cultureagain. According to the method, kresoxim-methyl, ampicillin and cefotaxime are used in match to effectively remove the bacteria and fungus pollution in the chlamydomonas culture process; the method has the characteristics of being high in wide popularization scope, efficient, and low in toxicity, and is extremely high in value of popularization and application in storing of precious chlamydomonasand accuracy improving of following experiments.

The invention discloses an acidifying agent for forage addition. The acidifying agent concretely comprises, by mass, 30-40% of lactic acid, 8-15% of formic acid, 7-11% of fumaric acid and 34-55% of white carbon black. The acidifying agent has good compatibleness.

The invention discloses an anti-avian influenza virus neuraminidase N2 monoclonal antibody and encoding engine and application thereof, and belongs to the technical field of biomedicine. The anti-avian influenza virus neuraminidase N2 monoclonal antibody specifically identifies avian influenza virus neuraminidase protein N2, and has the ability to inhibit neuraminidase activity and neutralize virus. According to the anti-avian influenza virus neuraminidase N2 monoclonal antibody and encoding engine and application thereof, the gene sequence and the amino acid sequence of light-heavy chain variable region of the anti-avian influenza virus neuraminidase N2 monoclonal antibody are further cloned, and the uniqueness of the gene sequence and the amino acid sequence is confirmed. The related monoclonal antibody and the variable region gene and amino acid sequence can be used for diagnosis, therapeutic development and the like of the N2 avian influenza virus, and have wide clinical application value.

The present invention provides the use of SphK2 inhibitor ABC294640 in the preparation of a drug for promoting hematopoietic and immune system reconstruction after bone marrow transplantation. ABC294640 can increase the number and function of hematopoietic stem, and enhance its ability to differentiate into many blood cells and immune cells, which can help patients quickly through the critical period after transplantation. The invention provides a novel drug source for treating complications of various hematopoietic dysfunction of bone marrow transplantation patients.

The invention discloses an isolated bidirectional AC / DC conversion circuit and a control method thereof. The conversion circuit comprises an input filter, an input transformer, an AC rectifier unit, an energy storage filter unit, a DC. DC conversion unit, output energy storage unit. The circuit of the invention can make the circuit work in different modes of rectification, inversion or standby modes according to external communication commands or judgement of other external voltage and current signals. At the same time, the input transformer can realize the energy storage function of the circuit in inverter or rectifier mode, at the same time, it can effectively restrain the common-mode current of the AC side and the AC anti-bias detection function, and effectively reduce the common-mode interference of the AC rectifier unit to the ground.

The invention discloses adenylate cyclase containing an FYVE structural domain from phytophthora sojae as well as an encoding gene and application of the adenylate cyclase. The adenylate cyclase is prepared from phytophthora sojae. The adenylate cyclase PsZFAC containing the FYVE structural domain has an amino acid sequence as shown in SEQ ID No. 4, and a coding gene of the adenylate cyclase PsZFAC has a nucleotide sequence as shown in SEQ ID No. 3. The main function of the PsZFAC protein is to control the formation of phytophthora sojae sporangium. The gene provided by the invention has a very high application value in controlling phytophthora sojae root rot, and a bactericide developed by taking the protein as an action target has important practical significance in controlling the occurrence and prevalence of phytophthora sojae root rot.

The present invention relates to an epitope of leucine-rich and immunoglobulin-like domains 1 (Lrig-1), which is an antigen present on the surface of a regulatory T cell, and an antibody or antigen-binding fragment specifically binding thereto.

The invention relates to a pendulum-type damping anti-galloping device consisting of a yoke plate, a damping vibration attenuation structure (a spring structure and a damper) and a double-pendulum. The structure of the anti-galloping device saves the advantages of the conventional double-pendulum anti-galloping device and adopts the damping vibration attenuation structure. When the wires of the overhead transmission line gallop, the pendulum-type damping anti-galloping device itself serves the functions of energy cushioning, energy absorption and energy consumption and finally achieves the purpose of galloping inhibition. The anti-galloping device has the advantages of simple structure, good anti-galloping performance and easy installation,is matched with various spacing rods, is economicand is suitable for large-scale popularization and application.

The invention provides an application of CUL7 in glioma diagnosis, treatment and prognosis. Specifically, the invention proves that CUL7 expression is increased along with the increase of the malignancy degree of the glioma and is in negative correlation with a survival rate. The down regulation of the CUL7 inhibits the proliferation and the colony formation of glioma cells. Meanwhile, researchesdiscover that the CUL7 expression is increased along with the increase of the malignancy degree of the glioma and is in the negative correlation with the survival rate, the down regulation of the CUL7inhibits the proliferation and the colony formation of the glioma cells as well as inhibits the invasion and the migration of the glioma cells, meanwhile, the apoptosis of the glioma cells can be accelerated, and a glioma cell cycle is retarded. Meanwhile, the invention discovers that miR-3940 can target the CUL7 and further inhibit the proliferation, the invasion and the migration of the glioma,a reference is provided for the targeted treatment of the glioma, and therefore, the invention has a good practical application value.

The invention discloses a 10-acetyl dithranol hydrogel and a preparation method thereof. The hydrogel is prepared from the raw materials by weight proportion as follows: 3g-23.7g of 10-acetyl dithranol, 17g-23g of salicylic acid, 120g-160g of glycerol, 8g-12g of carbomer-940, 0.5g-1.5g of ethyl hydroxy benzoate, 7ml-12ml of triethanolamine, 0.5g -1.5g of ascorbic acid, 3ml-7ml of ethanol, 0.5ml-1.5ml of essence and 700ml-850ml of purified water. The 10-acetyl dithranol hydrogel has the advantages of inhibiting the proliferation of epidermal cells by reducing DNA synthesis, inhibiting the respiration of mitochondrion, recovering relevant enzyme in skin lesion caused by psoriasis, and inhibiting the functions of monocytes. As the increasing concentration therapy is adopted, the drug stays at the skin lesion for 24 hours; when the transient touch therapy is adopted, the irritation can be reduced.

The invention belongs to the technical field of pesticide and particularly relates to a composition of a bactericide containing bixafen and dimoxystrobin. The effective components of the bactericide composition are bixafen and dimoxystrobin, and the weight ratio of the bixafen to the dimoxystrobin is (30:1):(1:30). The composition adopts the bactericide bixafen and the dimoxystrobin which are different in action mechanisms to be mixed for use, has an obvious synergistic effect on wheat powdery mildew, wheat rust and wheat scab, and effectively controls drug resistance generated by pathogenic microorganisms. Field tests show that when the ratio of the bixafen to the dimoxystrobin is 10:1, after the composition has been used for 7 days, the control effect on wheat rust is up to 93.36%, the control effect on wheat powdery mildew is up to 94.04%, and the control effect on wheat scab is up to 91.57%, and all the control effects are obviously higher than those of a single dosage of bixafen and a single dosage of dimoxystrobin.

The invention discloses a docetaxel nano-micelle, a preparation method and its application in the preparation of medicines for treating tumors or drug-resistant tumors. Described docetaxel nano-micelle comprises: docetaxel 1 weight part; Carrier material 10-100 weight part; Oil 0-10 weight part, wherein, the average particle diameter of described docetaxel nano-micelle is 10-200nm. The preparation can greatly increase the water solubility of docetaxel and the stability of the preparation, prolong the circulation time of docetaxel in the blood, reduce the toxic and side effects of existing preparations, and passively target tumor tissues through the EPR effect, thereby improving Antitumor efficacy of docetaxel, and can overcome multidrug resistance of tumors.

The invention discloses an application of a small-molecule inhibitor ML385 in the aspect of inhibiting tumor cells PD-L1. Furthermore, the ML385 inhibitor inhibits the function of PD-L1 in tumor cells and activates the anti-tumor immune function of T cells. The embodiment of the invention also provides an application of the small-molecule inhibitor ML385 in the aspect of inhibiting tumor cells PD-L1 and PD-L2. Furthermore, the ML385 inhibitor destroys the core site of PD-L1L2-SE identified by the NRF2 by inhibiting the combination of the NRF2 and the MAF, so that the expression of PD-L1 and PD-L2 is inhibited. The embodiment of the invention further provides a medicine for killing tumor cells, and the medicine is characterized by comprising the small-molecule inhibitor ML385. Furthermore, the medicine further comprises an anti-PD-L1 antibody or an anti-PD-L2 antibody. According to the embodiment of the invention, experiments prove that the small molecule inhibitor ML385 obviously inhibits the expression of PDL1 in breast cancer cells SUM159 and MDA-MB-231.

The invention discloses a silicon-based hydrophobic and bacteriostatic powder coating for an electric power switch cabinet. The silicon-based hydrophobic and bacteriostatic powder coating is prepared from raw materials in parts by weight as follows: 0.7-1 part of zinc pyrithione, 0.08-0.2 parts of lanthanum oxide, 2-4 parts of sodium 3-hydroxybenzoate, 5-7 parts of 8-hydroxyquinoline, 10-14 parts of polyethylene glycol octylphenol ether, 36-40 parts of tetrabutyl titanate, 20-25 parts of cyclohexanol, 100-120 parts of unsaturated polyester resin, 2-3 parts of sodium carboxymethyl cellulose, 0.4-1 part of diisopropylethanolamine, 4-5 parts of lauryl mercaptan, 3-4 parts of maleated rosin, 0.6-1 part of butylmercaptooxo-stannane, 3-4 parts of triethanolamine borate, 0.3-1 part of 2-mercaptobenzimidazole and 14-20 parts of tetraethyl orthosilicate. Tetraethyl orthosilicate is taken as a precursor, and by the aid of added silica sol, not only are strength and hydrophobicity of the powder coating effectively improved, but also compatibility of the components is effectively improved.