46 results about "NITRIC OXIDE SYNTHASE 1" patented technology

The invention discloses an application of squalene or a pharmaceutically acceptable salt thereof in preparation of a medicine for preventing or treating endotoxemia. Experiments show that squalene significantly relieves LPS-induced endotoxemia liver injury through a multi-target mechanism, squalene not only relieves inflammatory response by inhibiting release of inflammatory factors, but also relieves oxidative stress by activating an antioxidant pathway, and the squalene has dual action mechanisms. The invention further provides application of the squalene-containing composition to preparation of the medicine for treating endotoxemia, squalene and glucocorticoid show a synergistic effect in the aspect of inhibiting TNF-alpha, AST can be reduced more remarkably by combining squalene and glucocorticoid, and the effect of dual inhibition of inflammatory mediators is achieved. Besides, the composition of the inducible nitric oxide synthase and squalene is applied to the preparation of the medicine for treating endotoxemia, and the inducible nitric oxide synthase inhibitor can inhibit the activity of iNOS, so that the excessive generation of nitric oxide is reduced, and the inflammatory reaction is further inhibited synergistically.

To provide 2-aminopyridine derivative compounds for use as inhibitors of nitric oxide synthase.SOLUTION: Disclosed are 2-aminopyridine derivative compounds for use as inhibitors of nitric oxide synthase (NOS). In particular, the field of the present invention relates to 2-aminopyridine derivative compounds for use as inhibitors of neuronal nitric oxide synthase (nNOS), which are formulated as pharmaceutical compositions for treating nNOS-associated diseases and disorders such as Alzheimer's disease, Parkinson's disease, and Huntington's disease, as well as amyotrophic lateral sclerosis, cerebral palsy, stroke / ischemic brain injury, and migraine headaches.SELECTED DRAWING: Figure 1

To provide an andrographis paniculata diterpene lactone compound as well as extraction method and application thereof.SOLUTION: The andrographis paniculata diterpene lactone compound provided by the invention has a structure as shown in any one of formulas 1-7 and is novel in structure. The andrographis paniculata diterpene lactone compound extracted and separated from andrographis paniculata has a good anti-inflammatory effect, and has a good down-regulation effect on secretion of NO, interleukin-6 (IL-6), tumor necrosis factor-α (TNF-α) and interleukin-1β (IL-1β) in a lipopolysaccharide (LPS) induced mouse mononuclear macrophage (RAW264.7 cell) inflammation model; the compound also has a good inhibition effect on expression of inducible nitric oxide synthase (INOS) and cyclooxygenase-2 (COX-2) proteins, and can be applied to preparation of anti-inflammatory drugs.SELECTED DRAWING: Figure 1

The invention provides a tissue engineering heart valve stent with a sulfonated nano-enzyme coating as well as a preparation method and application of the tissue engineering heart valve stent, and belongs to the technical field of medical materials. The invention relates to a tissue engineering heart valve stent with a sulfonated nano-enzyme coating, which comprises an acellular matrix carrier, ruthenium / iridium-tannic acid nano-enzyme loaded on the acellular matrix carrier, and a sulfonated polymer coating fixed on the acellular matrix carrier and / or the surface of nano-particles through ultraviolet polymerization, the ruthenium / iridium-tannic acid nano-enzyme is formed by tannic acid TA, Ru < 3 + > and Ir < 3 + > through coordination. According to the invention, through double bionic activities of superoxide dismutase and nitric oxide synthase of ruthenium / iridium-tannic acid nano-enzyme and through the super-hydrophilicity and electrically neutral surface of the sulfonated polymer coating, collaborative regulation and control of O2-NO cascade catalysis and interface functions in a pathological microenvironment are realized; the structural and functional in-situ regeneration of the tissue engineering heart valve stent is promoted.

The composition for predicting Alzheimer's disease prognosis comprising a detection reagent that specifically binds to any one or more genes selected from the group consisting of Nos1 (Nitric oxide synthase 1), Aph1B (Anterior pharynx defective 1 homolog B), Ryr3 (Ryanodine receptor 3), Atf6 (Activating transcriptional factor 6), Ip3r (Inositol trisphosphate receptor), Nep (Neprilysin), Cdk5 (cyclin dependent kinase 5) and Abad (Amyloid beta-binding alcohol dehydrogenase), a kit, and a method for providing information on Alzheimer's disease prognosis of the present invention can rapidly and accurately predict the prognosis of Alzheimer's disease, and can determine the prognosis for a drug by comparing the expression level before and after drug administration, so that an appropriate treatment direction can be determined according to the predicted prognosis. Therefore, they have an effect that can greatly contribute to the reduction of mortality due to Alzheimer's disease.

The present invention provides NOS inhibitors such as iNOS inhibitors, or a pharmaceutically acceptable salt, ester, prodrug, complex, solvate, hydrate, or isomer thereof, in any crystalline form or in amorphous form. The inhibitors include 1,1 or 1,2 substituted-ethyl carbamimido thioates, cyclic compounds substituted with a carbamimidoyl sulfanylethylphenyl group and a carbamimidoylsulfanyl group, compounds substituted with a carbamimidoyl sulfanylethyl phenylmethyl group, bis-carbamimidoylsulfanylethyl substituted compounds, 2-propoxypyridine derivatives, alkylamine or heteroalkylamine derivatives, n-aminoethyl n-phenyl amine derivatives, and saturated heterocyclic fused benzene derivatives. Pharmaceutical products comprising the NOS inhibitors such as iNOS inhibitors and the applications thereof in prophylaxis and / or treatment of inflammatory diseases, and proliferative diseases such as cancer including gastro-intestinal, colorectal, gynecological, pancreatic, head and neck, esophageal, breast, lung, and central nervous system tumors, among others, are also provided.

The invention relates to modulation of oral health by nitric oxide synthase pathways. Pharmaceutical compositions and methods for treating or preventing diseases and conditions associated with or characterized by at least one of xerostomia and periodontal disease by modulating the nitric oxide synthase pathway are provided, as well as animal models and drug screening methods. This modulation may be accomplished by administering tetrahydrobiopterin (BH4), or a prodrug and / or salt thereof. Treatment and prevention of xerostomia may also have downstream effects of preventing periodontitis, decayed teeth, parotid gland enlargement, lip inflammation and dehiscence (cheilitis), tongue and buccal mucosa inflammation or ulcer, oral candidiasis, salivary gland infection (salivary adenitis), halitosis, and oral mucosa dehiscence and dehiscence.

The invention discloses an application of nitric oxide synthase neurons in an island leaf cortex II layer in preparation of a medicine for treating osteoporosis, and systematically reveals a nerve stress induced bone metabolism imbalance mechanism by constructing a chronic heterologous pressure stress mouse model and combining an enzyme-linked immunosorbent assay and a high-resolution micro-CT (Computed Tomography) technology; the method comprises the following steps: accurately positioning specific nerve connection between nNOS neurons of an island leaf cortex II layer and bone tissues for the first time by adopting a reverse cross-polysynaptic virus tracing technology, and determining that the region is a key central target point regulated and controlled by a brain-bone axis; the activity of target neurons is specifically intervened through a chemical genetics technology, it is proved that activation can induce the phenotype of osteoporosis, and pathologic indexes are remarkably improved through inhibition.

The invention belongs to the technical field of biological medicine, and particularly relates to coriaria sinica lactone compounds, a preparation method thereof and application of the coriaria sinica lactone compounds in anti-inflammatory activity. The coriaria sinica lactone compound can significantly inhibit a TLR4 / NF-kappa B signal channel to inhibit downstream inflammatory protein nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) and further inhibit inflammatory BV2 cells from generating nitric oxide, the inhibition rate can reach 65.5%, and it is indicated that the coriaria sinica lactone compound has an application prospect in treatment of neuroinflammatory diseases.

Disclosed are 2-aminopyridine derivative compounds for use as inhibitors of nitric oxide synthase (NOS). In particular, the field of the invention relates to 2-aminopyridine derivative compounds for use as inhibitors of neuronal nitric oxide synthase (nNOS), which are formulated as pharmaceutical compositions for treating diseases and disorders associated with nNOS such as Alzheimer's, Parkinson's, and Huntington's diseases, and amyotrophic lateral sclerosis, cerebral palsy, stroke / ischemic brain damage, and migraine headaches.

The present invention provides NOS inhibitors such as iNOS inhibitors including alkylamine or heteroalkylamine derivatives, or a pharmaceutically acceptable salt, ester, prodrug, complex, solvate, hydrate, or isomer thereof, in any crystalline form or in amorphous form. Pharmaceutical products comprising the NOS inhibitors such as iNOS inhibitors and the applications thereof in prophylaxis and / or treatment of inflammatory diseases, and proliferative diseases such as cancer including gastro-intestinal, colorectal, gynecological, pancreatic, head and neck, esophageal, breast, lung, and central nervous system tumors, among others, are also provided.

The invention relates to application of 6 '-O-caffeoyl arbutin in preparation of a medicine for treating dementia, and belongs to the technical field of biological medicine. The 6 '-O-caffeoyl arbutin disclosed by the invention has a remarkable dementia treatment value, the action mechanism accurately fits the core pathological process of dementia, a neuroprotective effect is played by relieving oxidative stress and inhibiting inflammatory reaction, oxidative stress related indexes such as superoxide dismutase (SOD), catalase (CAT) and glutathione (GSH) can be effectively adjusted, and the dementia treatment effect is improved. The release of lactic dehydrogenase (LDH) and malondialdehyde (MDA) and the level of damage-induced nitric oxide synthase (I NOS) are reduced, so that the NMDA-induced PC12 cell damage is protected.

A pharmaceutical composition for producing a safe amount of nitric oxide (NO) in vivo and use thereof. The pharmaceutical composition comprises the following components: an NO toxicity decreasing agent, an optional NO extender, and a nitric oxide synthase inducer. Provided is the pharmaceutical composition which has high versatility and extremely effectively treats pathogenic microorganism infections. A new medicinal activity of 5-methyltetrahydrofolic acid, NMN, and dehydroascorbic acid is found, which has a variety of active effects on an immune system caused by pathogen infection, and capable of being used for treating or preventing disease caused by virus infections and other pathogen infections.

The invention discloses a sesquiterpene compound as well as a preparation method and application thereof, and relates to the technical field of medicines. The invention provides a sesquiterpene compound and discloses new activity of the sesquiterpene compound, namely the sesquiterpene compound is used for remarkably inhibiting generation of inflammatory BV2 cell NO and remarkably inhibiting oxidative stress SH-SY5Y cell damage. The sesquiterpene compound can significantly inhibit TLR4 / NF-kappa B signal channels to inhibit expression of downstream inflammatory protein nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2), and has an application prospect in treatment of neuroinflammatory diseases. The invention can obtain the sesquiterpene compound as well as the preparation method and the application thereof.

The application discloses a kind of micro bone-blood vessel symbiosis based on gene activation and its preparation method and application.The system includes: the amorphous calcium phosphate nanoparticles of L-arginine, bovine serum albumin and alendronate sodium co-modified loaded BMP-2 mRNA;Methacrylic acid gel hydrogel microspheres encapsulating the nanoparticle;And E7 peptide grafted on the surface of hydrogel microspheres.It is captured by E7 peptide bone marrow mesenchymal stem cells, and delivers BMP-2 mRNA to activate intracellular BMP-2 and endothelial-type nitric oxide synthase expression, while using L-arginine to drive in-situ synthesis of nitric oxide, to synergistically enhance stem cell osteogenic differentiation and promote vascular sprouting ability, realize the vascularization synchronous regeneration of bone defect.The system solves the problem of unstable exogenous nitric oxide donor and bone-vessel regeneration decoupling, and has excellent biocompatibility and bone repair efficiency.

A process for the preparation of racemic and optically active (1E,NE)-N-(1-aminoethylidene)-3-(4-chlorophenyl)-4-phenyl-N′-((4-(trifluoromethyl)phenyl)sulfonyl)-4,5-dihydro-1H-pyrazole-1-carboximidamide in high enantiomerical purity is provided.

The invention relates to a composition and a preparation method of a reproduction nursing external preparation with effects of inhibiting bacteria, relieving and improving male functions. The invention discloses an external preparation for male reproduction nursing. The plant essential oil comprises natural plant extracts (clove, herba epimedii, ginseng, dendrobium officinale, tribulus terrestris, radix sophorae flavescentis, fructus cnidii, saw palmetto fruit and aloe vera), nutritional ingredients (arginine, hydrolyzed collagen zinc, nicotinic acid, tocopherol, biotin and B-group vitamin yeast polypeptide) and compound essential oil (tea tree oil, jasmine flower oil, iris oil, cananga odorata flower oil and sandalwood oil). The composition can be prepared into spray, cream, lotion and other dosage forms. The preparation improves erectile function, enhances microcirculation, relieves pressure, improves sexual desire and realizes precise adjustment of male function and protection of gonad axis through mechanisms of inhibiting bacteria, diminishing inflammation, improving testosterone concentration, enhancing nitric oxide synthase activity, promoting vasodilatation, blocking neural signals, delaying ejaculation and the like.

The invention relates to the technical field of microbial infection treatment and molecular biology, and provides a method for inhibiting formation of a staphylococcus aureus biofilm, which is realized by inhibiting nitrosation modification of MgrA protein in staphylococcus aureus so as to inhibit formation of the biofilm. The inhibitor is nitric oxide synthase and is used for inhibiting nitrosation modification of the MgrA protein; the nitrosation modification for inhibiting the MgrA protein is realized by applying a nitric oxide synthase (NOS) inhibitor; the invention reveals that the staphylococcus aureus endogenous nitric oxide can promote the formation of a biofilm by modifying and regulating the 12th cysteine of the protein MgrA for the first time; based on the target spot, research proves that the MgrA modification level can be effectively reduced and the removal of the biofilm can be enhanced through multiple means such as gene mutation, NOS inhibitor or combination of the NOS inhibitor and antibiotics, and a new strategy and a potential drug development approach are provided for preventing and treating staphylococcus aureus intractable biofilm infection.

A novel microparticle which comprises a miRNA that regulates the production of nitric oxide, is a nitric oxide production promoter, and is capable of regulating the expression of a protein and / or a gene associated with erectile dysfunction; a prophylactic or therapeutic agent for erectile dysfunction; a method for improving erectile dysfunction; the particles are preferably exosomes; it is preferable that the microparticles comprise, as a miRNA for regulating the production of nitric oxide, miRNA having a gene related to the expression of nitric oxide synthase as a target gene, and are an expression promoter for nitric oxide synthase.

Preparation method and application of diterpenoid, relate to the application technical field of diterpenoid.The present application separates two new compounds of diterpenoid A and diterpenoid B from a strain of Hericium fermentation extract, and discloses chemical structural formula of the two compounds, and corresponding nuclear magnetic, mass spectrum, infrared and ultraviolet data, and its function of significantly inhibiting the production of inflammatory BV2 cell NO.Diterpenoid B has 24% of the promotion rate of axon growth of PC-12 cell, and simultaneously has significant inhibition of TLR4 / NF-κB signal path to inhibit downstream inflammatory proteins of nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2), and diterpenoid A and diterpenoid B both show significant anti-neuroinflammatory activity.The present application can obtain the preparation method and application of diterpenoid.

To identify a component capable of inhibiting an increase in the expression of nitric oxide synthase, and to provide an expression inhibitor of nitric oxide synthase.SOLUTION: An expression inhibitor of nitric oxide synthase comprises, as active ingredients, glycyrrhetinic acid and at least one selected from an extract of Equisetum arvense and an extract of Tilia japonica.SELECTED DRAWING: None

The invention belongs to the technical field of biological medicine, and particularly relates to low-molecular-weight stemona polysaccharide (STP-3-2) as well as a preparation method and application thereof, and the weight-average molecular weight (Mw) of the low-molecular-weight stemona polysaccharide (STP-3-2) is between 15 kDa and 5 kDa. The preparation method comprises the following steps: taking dry tuberous roots of stemona tuberosa, extracting to obtain non-starch total polysaccharide of stemona tuberosa, and separating and purifying to obtain the low-molecular-weight stemona tuberosa polysaccharide. The polysaccharide can obviously activate macrophages, enhance the phagocytic function of the macrophages, promote secretion of nitric oxide (NO), tumor necrosis factor-alpha (TNF-alpha) and interleukin-6 (IL-6) and up-regulate expression of inducible nitric oxide synthase (iNOS), IL-6 and TNF-alpha mRNA, shows obvious immunological enhancement activity, does not have obvious toxic or side effects, and can be used for preparing the immunopotentiator. The polypeptide can be used for preparing medicines or functional foods for treating and / or preventing diseases such as immunosuppression and the like, and has a wide application prospect.

The present invention relates to the use of bacterial compositions having an arginine deiminase activity (inhibition of nitric oxide synthase by conversion of L-arginine to L-citrulline) of 1-1,000 μmol L-citrulline / h / g composition and a sphingomyelinase (ceramide generation) activity of 0.01-1.000 nmoles ceramides / h / g composition in the treatment and / or prophylaxis of airway diseases caused by viruses such as influenza viruses, coronaviruses, as SARS-CoV, MERS-CoV and SARS-CoV-2, avian viruses, respiratory syncytial virus (VRS), rhinoviruses, pneumoviruses, or respiratory failure induced or aggravated by viral infections, angina pectoris, pulmonary heart, respiratory distress, pulmonary edema, neonatal asphyxia, myocardial infarction, heart failure, respiratory failure Pickwick syndrome, pulmonary hypertension, pneumonia or even cystic fibrosis (CF) aggravated by viral infections.

Disclosed are 2-aminopyridine derivative compounds for use as inhibitors of nitric oxide synthase (NOS). In particular, the field of the invention relates to 2-aminopyridine derivative compounds for use as inhibitors of neuronal nitric oxide synthase (nNOS), which are formulated as pharmaceutical compositions for treating diseases and disorders associated with nNOS such as Alzheimer's, Parkinson's, and Huntington's diseases, and amyotrophic lateral sclerosis, cerebral palsy, stroke / ischemic brain damage, and migraine headaches.

A novel Lactobacillus rhamnosus KBL2290 strain exhibits various activities such as improving intestinal flora, anti-inflammatory, and strengthening intestinal tight junctions. The strain may increase intestinal flora of Akkermansia genus, Lactobacillus genus, Ruminococcus genus or Prevotella genus, suppress an expression of interleukin 1-beta (IL-1B), interleukin 2 (IL-2), interleukin 4 (IL-4), interleukin 12p40 (IL-12p40), interleukin 13 (IL-13), or interleukin 17A (IL-17A), suppresses an expression of chemokine ligand 2 (CCL2) or chemokine ligand 1 (CXCL1), suppress an expression of cyclooxygenase 2 (Cox-2) or nitric oxide synthase (iNOS), promote an expression of interleukin 10 (IL-10) or transforming growth factor-β (TGF-β), and increase an expression of Zo-1 or Occludin. A pharmaceutical composition including the strain may prevent or treat inflammatory bowel disease.

This invention discloses the application of Dendrobium huoshanense protocorms in anti-fatigue and kidney-tonifying and aphrodisiac effects. Combining Dendrobium huoshanense protocorms with Cistanche deserticola, American ginseng, Rubus idaeus, Cornus officinalis, and Lycium barbarum significantly enhances the anti-fatigue and kidney-tonifying and aphrodisiac effects of the formula. Compared with Cistanche deserticola alone, adding Dendrobium huoshanense protocorms significantly prolongs the exhaustive swimming time in mice, reduces serum urea nitrogen and lactic acid levels, increases liver glycogen content, and increases muscle glycogen content. Compared with Cistanche deserticola alone, adding Dendrobium huoshanense protocorms significantly increases serum superoxide dismutase activity, reduces serum malondialdehyde content, increases serum testosterone content, increases penile nitric oxide synthase activity, and increases penile nitric oxide and cyclic guanosine monophosphate content in penile tissue.

Microparticles that contain miRNA that controls the production of nitric oxide and are an agent for promoting the production of nitric oxide are new microparticles that enable controlling the expression of a protein and / or a gene related to erectile dysfunction; a preventive drug or a therapeutic drug for erectile dysfunction; a method for improving erectile dysfunction; it is preferable that the microparticles be exosomes; and it is preferable that the microparticles of the present disclosure contain miRNA targeting a gene concerning the expression of nitric oxide synthase as the miRNA that controls the production of nitric oxide, and be an agent for promoting the expression of nitric oxide synthase.

The invention discloses a protein nitrosation modification regulation compound as shown in a formula I as well as a preparation method and application of the protein nitrosation modification regulation compound. The compound disclosed by the invention can be used for simultaneously combining calcium / calmodulin dependent kinase II alpha (CaMKII alpha) and nerve type nitric oxide synthase (nNOS), promoting the interaction of the two proteins and up-regulating the nitrosation modification level of the CaMKII alpha, and can be used for preventing and / or treating diseases mediated by the CaMKII alpha.

Halophthalimides are disclosed. The halophthalimides may inhibit TNF-α activity, TNF-α synthesis, inflammation, inducible nitric oxide synthase, SARS-CoV-2 virus, or any combination thereof. The halophthalimides may be administered to a subject with a traumatic brain injury, an inflammatory disorder, an autoimmune disorder, a neurodegenerative disease, a viral infection, or any combination thereof. The disclosed halophthalimides have a structure according to Formula I, or a stereoisomer or pharmaceutically acceptable salt, solvate, or hydrate thereof,where R5 isAt least one of R2-R4 or Re is halo.

The invention discloses a preparation method of alcohol-free extracted lavender polysaccharide and application of the alcohol-free extracted lavender polysaccharide in anti-aging products. The lavender polysaccharide (LAPC) is extracted from a lavender raw material by adopting a hot water extraction method in combination with a membrane separation technology, the yield is 4.8-8.6%, the polysaccharide content is 15-30%, the uronic acid content is 15-30%, and the pH value is 6.0-6.7. An anti-aging activity experiment in an aging mouse model induced by D-galactose shows that the LAPC prepared by the invention can remarkably improve the activity of antioxidant enzyme in an aging mouse body; the cell morphology of liver and kidney tissues is effectively improved; multiple serum biochemical indexes are recovered to be normal; the expression level of proinflammatory factors is reduced; the activity of acetylcholin esterase and nitric oxide synthase in brain tissues is inhibited; and the expression of a p53 / p21 protein signal channel is down-regulated. The LAPC provided by the invention has remarkable anti-aging activity. The provided preparation method of the lavender polysaccharide is simple, convenient and efficient, does not need complex chemical reagents, and has the potential of being developed into low-toxicity and efficient anti-aging cosmetics or medicine raw materials.