170 results about "Caspase" patented technology

The invention belongs to the field of biological medicines, and particularly discloses application of a Ptprj agonist GJ103 in preparation of a medicine for treating acute kidney injury (AKI) induced by cisplatin. In-vivo and in-vitro experiments prove that the GJ103, by activating Ptprj, can significantly down-regulate expression of pro-apoptotic protein Bax and Cleved Caspase-3, up-regulate anti-apoptotic protein Bcl2 and reduce infiltration of inflammatory factors TNF-alpha and IL-6, so that apoptosis and inflammatory response of renal tubular epithelial cells are relieved. In in-vivo experiments, GJ103 (20-40mg / kg / day) can reduce serum creatinine and urea nitrogen levels of cis-platinum model mice and improve pathological injuries such as renal tubule dilatation; in in-vitro experiments, 20-40 [mu] M of GJ103 can inhibit apoptosis of renal tubular epithelial cells and reduce expression of renal injury markers NGAL and Kim-1. The pharmaceutical composition contains GJ103 and a pharmaceutical carrier, the preparation form can be a 4mg / mL injection (the purity is greater than or equal to 99.46%) or an oral preparation, and a new strategy is provided for clinical treatment of cisplatin renal toxicity.

The invention relates to application of 12-ketolithocholic acid in preparation of a medicine for preventing or treating acute ischemic intestinal injury. According to the application, 12-ketolithocholic acid (12-KLCA) is used for preventing or treating acute ischemic intestinal injury and is verified on a constructed classical intestinal ischemia reperfusion model, and a verification result shows that the 12-KLCA obviously improves intestinal histopathologic injury induced by intestinal ischemia reperfusion of a mouse, improves the survival rate of the mouse, and has a good application prospect in prevention or treatment of acute ischemic intestinal injury. The protein expression level of the apoptosis factor activated caspase-3 is reduced, the effect is obvious, safety and non-toxicity are achieved, and the side effect is small.

The invention discloses design and synthesis of a series of brain-targeted ginsenoside Rg1 derivatives and application of the brain-targeted ginsenoside Rg1 derivatives in treatment of Alzheimer's disease. According to the invention, ginsenoside Rg1 and polyethylene glycol with a specific chain length are covalently linked to successfully construct the derivative capable of enhancing the penetrating power of the blood-brain barrier. The series of derivatives provided by the invention not only solve the problems of poor brain targeting and insufficient stability of natural Rg1, but also can inhibit neuroinflammation by regulating and controlling an NLRP3 / caspase-1 signal channel in an LPS-induced neuroinflammation model, and finally, the learning and memory ability is remarkably improved. The product is simple and convenient in preparation process and good in biological safety, and a new candidate compound is provided for developing a new generation of Alzheimer disease treatment medicines.

The disclosure provides inducible caspase polypeptides, compositions comprising inducible caspase polypeptides and sequences encoding the same, cells modified to express the polypeptides and compositions of the disclosure, as well as methods of making and methods of using same for adoptive cell therapy.

To develop a novel plant extract having an excellent skin-conditioning effect.SOLUTION: Provided are a caspase-14 activator or an anti-oxidizing agent containing a Japanese apricot extract, and an external preparation for skin containing the caspase-14 activator or the anti-oxidizing agent.EFFECT OF THE INVENTION: According to the present invention, skin is protected from dryness, ultraviolet light and active oxygen which are harmful to skin by increasing the enzymatic activity of caspase-14 and deleting active oxygen, and a skin-conditioning effect that the external preparation for skin should include can be realized.SELECTED DRAWING: Figure 1

Abstract Described herein, in one aspect, are antigen presenting cells (APCs) comprising an exogenous nucleic acid encoding one or more candidate antigens, wherein the one or more candidate antigens are expressed and presented with MHC class I or MC class II molecules; a molecular reporter of Granzyme B (GzB) activity; and c) an exogenous inhibitor of caspase-activated deoxyribonuclease (CAD)-mediated DNA degradation, a CAD knockout, or a caspase knockout (e.g., caspase 3 knockout). Described herein, in another aspect, is a system for detection of recognized antigen presentation by an antigen presenting cell to a cytotoxic lymphocyte or NK cell. Abstract 2018 / 22761 oM - cell Target ml Target cell cell cell Target Target Target SUBSTITUTE SHEET (RULE 26) cell cell cell Target Target cell cell 1 / 28 my Isolate recognized cell Library of target cells target cells and displaying different Add T cells from sample sequence antigens antigens of interest. CTLs deliver cytotoxic granules to target cells displaying cognate antigen FIG. 1 PCT / US2018 / 036663 20 26 20 53 56 07 J ul 2 02 6 2 0 2 6 2 0 5 3 5 6 0 7 J u l 2 0 2 6 2 0 1 8 / 2 2 7 6 1 o M a n d m y 1 / 2 8 m y L i b r a r y o f t a r g e t c e l l s d i s p l a y i n g d i f f e r e n tA d d T c e l l s f r o m s a m p l e of interest. CTLs deliver c y t o t o x i c g r a n u l e s t o t a r g e t c e l l s d i s p l a y i n g c o g n a t e a n t i g e n P C T / U S 2 0 1 8 / 0 3 6 6 6 3

This invention discloses the application of the inflammasome NLRP6 as a target in screening drugs for treating epilepsy, and the application of NLRP6 expression inhibitors in the preparation of drugs for treating epilepsy. This invention reveals for the first time the role of the inflammasome NLRP6 in epileptic neuroinflammation. This invention identifies NLRP6 as a key regulator of neuroinflammation in epilepsy and investigates its role in activating the caspase-1 / IL-1β / IL-18 signaling pathway. Knockdown of NLRP6 can improve the damaging effects of epilepsy on neurons, thereby improving seizures; overexpression of NLRP6 may exacerbate seizures, neuronal damage, and neuroinflammatory responses. This invention provides a new potential target for epilepsy treatment, offering new research ideas and directions.

The present invention provides a cryoprotective additive for human sperm and a preparation method thereof. The method is to add an mTORC1 activator and a Caspase-9 inhibitor to a commercially available sperm cryoprotectant. Compared with the pure commercially available protectant, the cryoprotective additive of the present invention has an increased number of forward-moving sperm after thawing and recovery; there are more forward-moving sperm after recovery, with better forward motility and better forward motility endurance. At the same time, the mitochondrial structure and function of the sperm cells after recovery are less damaged, the mitochondrial function recovers quickly, less mitochondrial ROS is produced, apoptosis is reduced, the ability to protect the function of sperm cells is better, and it is more conducive to the long-term cryopreservation of sperm-like cells.

The application discloses application of a pyrimidinotriazine diketone derivative in preparation of a medicine for inhibiting activity of human protease caspase-1, and belongs to the technical field of medicines. In view of defects of existing caspase-1 inhibitors, the compound has the characteristics of high affinity binding to caspase-1 (K D = 8.11 μM; 8.78 μM) and strong inhibition on the activity (IC 50 = 11.90 nM-14.47 nM). The compound is used for preparation of a medicine for inhibiting the activity of caspase-1 and a medicine for treating inflammation-related diseases such as sepsis-related lung injury, acute respiratory distress syndrome or acute pancreatitis.

To provide immunoresponsive cells having IL-1 superfamily activities with spatiotemporal restriction.SOLUTION: The present invention provides an immunoresponsive cell expressing a modified pro-cytokine of the IL-1 superfamily, where the modified pro-cytokine comprises, from N-terminus to C-terminus, (a) a pro-peptide; (b) a cleavage site recognized by a protease other than caspase-1, cathepsin G, elastase or proteinase 3; and (c) a fragment of a cytokine of the IL-1 superfamily.SELECTED DRAWING: None

The invention discloses an application of a coix seed extract in preparation of a medicine for preventing and treating acute lung injury. The semen coicis extract is obtained by performing reflux extraction on semen coicis by using ethanol, recovering an extraction solvent by using a rotary evaporator and then performing evaporation concentration by using a water bath. The coix seed extract can obviously increase the thymus index, improve the pathological injury of lung tissues, reduce the level of inflammatory factors in serum and lung tissues, possibly inhibit the expression of NLRP3, Caspase-1 and GSDMD-N in NLRP3 signal channel key proteins in the lung tissues, inhibit the NLRP3 signal channel, inhibit inflammation and pyroptosis, and play a role in protecting ALI. The coix seed extract can inhibit the activation of an NLRP3 signal channel and play a role in treating the acute lung injury disease.

The invention provides a diagnosis and treatment integrated nano platform as well as a preparation method and application thereof. According to the diagnosis and treatment integrated nano platform, an organic-inorganic nano hybrid is constructed through structure optimization and function integration, four modes of PTT, PDT, SDT and CDT are organically combined innovatively, and efficient synergistic treatment of GBM is achieved through real-time monitoring of photoacoustic imaging. First, a dOMV encapsulation strategy significantly improves the ability to penetrate through the blood brain barrier. Meanwhile, the IEICO-4F has a strong near-infrared absorption characteristic and has a synergistic effect with the high catalytic activity of the mesoporous platinum nanoparticles. Under the laser / ultrasonic excitation condition, the diagnosis and treatment integrated nano platform shows excellent photo-thermal conversion performance, the Fenton reaction rate can be increased, endogenous hydrogen peroxide can be continuously catalyzed to be decomposed to generate oxygen, and the tumor hypoxia state is effectively relieved. The series of reactions further enhance the generation of ROS, activate a Caspase-1 / GSDMD mediated pyroptosis pathway, finally achieve an efficient tumor inhibition effect, and successfully break through the limitation of a single treatment mode.

The present application belongs to the technical field of hair loss treatment, and particularly relates to a phototherapy and drug synergistic intervention system for androgenetic alopecia of human scalp. In the system, the drug is angelica extract with a concentration of 0.1-500 ug / mL; the phototherapy light source is a red light LED light source with a wavelength of 600-700 nm; the light irradiance is 2-100 mW / cm 2 ; the light dose is 2-20 J / cm 2 ; the irradiation mode is steady light or pulsed light; and the synergistic intervention mode is that the phototherapy and the drug application are performed synchronously or the phototherapy is performed within 0.5-2 hours after the drug application. Experiments show that the light-drug combined intervention significantly improves cell viability, ATP level, migration ability, IGF1 and VEGF secretion, reduces ROS and MDA levels, inhibits Caspase-3 activity, regulates BCL2 / BAX expression, activates Wnt, Hh and PI3K pathways, and inhibits BMP and TGF-beta pathways. The present application provides a treatment scheme with clear timing and standardization, and realizes safe, non-invasive and efficient hair loss treatment.

The invention discloses a preparation rich in polygonatum sibiricum polypeptide and application of the preparation in diabetes mellitus. The composition is prepared from rhizoma polygonati polypeptide, semeglutide, astaxanthin, an active agent and a ferroptosis mixture. Pharmacodynamic experiments show that in a diabetic mouse model, fasting blood glucose can be remarkably reduced, the serum insulin level can be increased, renal function indexes can be improved, and expression of NLRP3 inflammation pathway related proteins (NLRP3, Caspase-1 and IL-1beta) in pancreatic tissue can be remarkably inhibited. By integrating multiple mechanisms of blood glucose reduction, oxidation resistance, inflammation resistance, ferroptosis resistance and the like, multi-target collaborative intervention is realized, the pharmaceutical composition is remarkably superior to a single component in the aspects of blood glucose reduction, pancreas islet function protection and complication alleviation, and a new clinical strategy is provided for treatment of diabetes mellitus, especially type 1 diabetes mellitus.

The invention provides medical application of a licochalcone B derivative CTG12 in preparation of an NLRP3 inflammasome inhibitor, and belongs to the technical field of biological medicine. The invention provides application of a licochalcone B derivative CTG12 in preparation of an NLRP3 inflammasome inhibitor. The invention also discloses application of the compound in preparation of drugs for preventing or treating diseases related to abnormal activation of NLRP3 inflammasomes. The synthesized compound CTG12 has the remarkable activity of inhibiting caspase-1 generated by BMDM cells, the effect is improved by about eight times compared with licochalcone B, and the compound CTG12 has the broad-spectrum and specific inhibiting effect and can effectively inhibit activation of NLRP3 inflammasomes.

The invention discloses application of TPN171H, an active fragment thereof or a derivative thereof in preparation of a medicine for treating spinal cord injury. The TPN171H shows an excellent treatment effect in spinal cord injury treatment, the levels of apoptosis factors BAX and Caspase-3 cleaved can be remarkably reduced, the level of Bcl-2 is improved, the content of a neuron marker MAP-2 is also remarkably increased, and the number of Tunel bodies and the cavitation-like structure are remarkably reduced. The intervention of the TPN171H also can reduce MNSS, and prompts that the TPN171H has the functions of promoting the spinal cord movement and coordination of the rat with spinal cord injury and improving the sensory system of the rat with spinal cord injury.

The present invention discloses an application of a medicated serum prepared from Herba Lycopodii in liver cancer cells, and belongs to the field of medical technology. The present invention provides a medicated serum prepared from Herba Lycopodii in the preparation of a drug for inhibiting the proliferation and invasion of liver cancer cells, and promoting apoptosis of liver cancer cells. The present invention verifies that the Herba Lycopodii medicated serum can effectively inhibit the proliferation and invasion of HepG2 cells, promote cell apoptosis, and inhibit the phosphorylation of mTOR protein in the mTOR signaling pathway of HepG2 cells, upregulate the expression of pro-apoptotic proteins caspase-9, caspase-3, and bax, and downregulate the expression of anti-apoptotic protein bcl-2. The present invention studies the effects of the Herba Lycopodii medicated serum on related apoptosis genes in the mTOR molecular signaling pathway of HepG2 liver cancer cells and the proliferation, invasion, and apoptosis of HepG2 liver cancer cells from the perspective of in vitro experiments, in order to provide an experimental basis for clinical application.

The present application belongs to the technical field of coordination chemistry and biomedical science, and provides a multifunctional iridium (III) complex, a preparation method and application thereof. The multifunctional iridium (III) complex (Mito-Ir) is composed of an iridium (III) complex cation and a coordination anion shown in the following formula. Mito-Ir can efficiently target mitochondria, and also has the abilities of phosphorescence imaging, type I and type II active oxygen generation, and photocatalytic oxidation of nicotinamide adenine dinucleotide. Under light irradiation, Mito-Ir triggers severe mitochondrial dysfunction through the above synergistic effect, and then specifically activates the caspase-3 / GSDME signaling pathway, and significantly induces pyroptosis; this pyroptosis-based cell death mechanism can effectively overcome the apoptosis tolerance of tumor cells, and is accompanied by the release of a large amount of inflammatory factors and damage-associated molecular patterns, stimulates immunogenic cell death, and activates the body's anti-tumor immune response.

The present disclosure relates generally to alkyne containing pharmaceutical agents, and in particular, to phenylethynyl-thiophene based compounds. More particularly, the present disclosure provides a class of compounds that can inhibit and / or attenuate apoptosis via caspase 3 for the treatment of various degenerative disorders. Additionally, the present disclosure relates to methods for treating specific degenerative disorders such as amyotrophic lateral sclerosis (ALS), Huntington's disease, epilepsy, spinal cord injury, complication due to diabetes, multiple sclerosis (MS), muscular dystrophy (MD), Parkinson's disease (PD), irritable bowel syndrome (IBS) and Alzheimer's disease (AD) in a patient comprising administering to the patient an effective amount of a present compound.

The present application relates to the field of biological medicine, in particular to a kind of muscone in the application of viral inhibitor.The viral inhibitor of the present application is used to inhibit the replication of Japanese encephalitis virus and / or porcine epidemic diarrhea virus.The present application finds that muscone has no cytotoxicity, and does not directly inactivate virus, but produces antiviral effect on Japanese encephalitis virus by inhibiting NLRP3 / Caspase-1, Caspase-9 / Caspase-3 / Bax / BCL-2, JNK / ERK / P38 and other signal pathways, and inhibits porcine epidemic diarrhea virus invasion into cells by reducing caveolin level.The antiviral effect is remarkable, the mechanism of action is clear, the selectivity is high, and the safety is better.

The invention relates to a caspase-1 responsive fluorescent probe based on FRET (Fluorescence Resonance Energy Transfer), a preparation method, application and a product, and belongs to the technical field of FRET fluorescent probes. The technical problem to be solved is to provide the FRET fluorescent probe capable of simultaneously carrying out in-vitro caspase-1 enzyme detection and in-vivo caspase-1 activity detection, and the specific technical scheme is that the FRET fluorescent probe with a chemical structure shown in a formula I is provided. The FRET fluorescent probe provided by the invention has short reaction time, is suitable for caspase-1 activity detection and pyroptosis imaging under a fluorescence confocal microscope, and can realize multi-scale imaging of pyroptosis in cell spheres and animal bodies.

The present invention provides a method for constructing a tumor cell pyroptosis model based on dual-color fluorescent labeling, the method comprising: constructing a PB vector plasmid that labels the cell pyroptosis effector gene GSDME and the histone gene H2B with dual-color fluorescent protein; screening a B16 tumor cell pyroptosis cell line that stably expresses GSDME and H2B labeled with dual-color fluorescent protein; using a Caspase-3-activated drug to stimulate the B16 tumor cell pyroptosis cell line labeled with GSDME and H2B with dual-color fluorescent protein, and visualizing the B16 tumor cell pyroptosis process and cell activity detection by fluorescence microscopy. On the one hand, the present invention can intuitively visualize the changes in cell nucleus and cell morphology when tumor cell pyroptosis occurs; on the other hand, the B16 tumor cell pyroptosis cell line model established by the present invention can be used as a powerful tool for screening drugs that induce cell pyroptosis, providing a means for further exploring the immunological molecular mechanism of visualizing cell pyroptosis.

The invention discloses application of RMTE in preparation of a medicine for preventing and controlling grass carp reovirus. The hemorrhagic disease caused by the grass carp reovirus (GCRV) is a key bottleneck restricting healthy development of the grass carp breeding industry, and the current vaccine for treating the grass carp reovirus (GCRV) has the problems of unstable immune protection effect, low protection rate for crossing of strains of different genotypes and the like, so that the research and development process of antiviral drugs is slow. The invention discloses an influence and a potential mechanism of a rhodamine B-ethyl sulfide condensation compound (RMTE) on GCRV (Growth Factor Receptor Virus) infection. Results show that the RMTE can significantly inhibit expression of VP6 and VP7 genes in GCRV infected cells, can effectively relieve expression inhibition of GCRV on GPX4, Caspase and p53 genes and promote expression of the three genes, and prove that the RMTE has a significant inhibition effect on GCRV infection and plays an antiviral effect through multiple ways. Research results provide new potential drugs and theoretical basis for prevention and control of GCRV.

The invention discloses a compound with an anti-inflammatory effect in Enshi Sichuan amur corktree, separation and application, and belongs to the technical field of medicines. The invention particularly discloses a compound which is separated from Enshi chuan amur corktree and has an anti-inflammatory effect, a separation preparation method and application. Researches prove that the compound has an inhibition effect on the expression of inflammatory factors IL-1beta and IL-17A, can inhibit the generation and secretion of an inflammatory factor IL-6 in Th17 cells, can reduce the expression level of Caspase-1 and NLRP3 proteins in colon tissues of mice, and can reduce the inflammatory response of ulcerative colitis of DSS modeling mice in a dose-dependent manner. The compound (limonin compound) with the anti-inflammatory effect in Enshi Huangchuan amur corktree can be used as a lead compound for development of anti-inflammatory drugs, and is of great significance to comprehensive utilization and development of Enshi Huangchuan amur corktree.

The invention discloses a new application of Renqingchangjue and an extract of Renqingchangjue. Specifically, the invention provides a new application of Tibetan medicine Renqingchangjue and an extract in preparation of a medicine for treating chronic atrophic gastritis, and systematically clarifies an exact molecular mechanism of the Tibetan medicine Renqingchangjue for treating CAG. The core of the invention is to reveal the core signal axis of Renqingchangjue by inhibiting TNF / NF-kB / Caspase-3 for the first time, so that the Renqingchangjue synergistically exerts the effects of resisting inflammation, resisting apoptosis and promoting mucosa repair, and provides a new intervention target and scientific basis for reversing gastric mucosa gland atrophy. The invention not only provides a modern pharmacological basis for the clinical curative effect of the Renqingchangjue, but also provides a brand new technical scheme and a protection basis for developing a medicine or a medicine composition which is based on the clear pathway target and is used for treating the chronic atrophic gastritis.

The invention discloses a meat tenderizing method for improving final tenderness by improving cell apoptosis, which is realized by injecting a disodium adenosine triphosphate solution into muscles at multiple points after a pig carcass is split into halves. According to the invention, adenosine disodium triphosphate is exogenously added, so that the energy level of muscles is improved, more muscle cells die in an apoptosis manner, and Caspase can be activated by apoptosis, so that a tenderization effect is achieved. The adenosine disodium triphosphate is colorless and odorless, and is a food additive allowed to be used in the national standard. The meat tenderizing method can maintain the original shape of the meat to a greater extent, does not influence the color of the meat, and is very good in safety at the same time.

This invention discloses the application of a "Super Brain-Boosting Capsule," belonging to the field of pharmaceutical technology. The Super Brain-Boosting Capsule is used in the preparation of drugs for treating Alzheimer's disease. The capsule enhances the mitochondrial membrane potential of Glu-treated HT22 cells by inhibiting ferroptosis. At the transcriptional level, the capsule activates the expression of key Nrf2 / HO-1 / GPX4 signaling molecules NRF2, HO-1, GPX4, SLC7A11, ACSL4, FTH1, and FPN1, while reversing the expression of Bcl-2, Caspase-3, and Caspase-9 to inhibit apoptosis in AD cells. This invention reveals that the Super Brain-Boosting Capsule, based on the Nrf2 / HO-1 / GPX4 pathway, inhibits Glu-induced ferroptosis in HT22 cells, which can treat Alzheimer's disease. This invention provides experimental evidence and direction for the further development of the Super Brain-Boosting Capsule in the prevention and treatment of Alzheimer's disease and other neurodegenerative diseases.

The present application provides chemical compounds useful, for example, in inhibiting gasdermin pore formation in a CA cell, inhibiting inflammasome-mediated death of a cell (pyroptosis); inhibiting cytokine secretion from a cell, inhibiting an inflammatory caspase in a cell, and / or covalently reacting with a cysteine of a gasdermin protein in a cell. These compounds are also useful in treating or preventing diseases or conditions in which inflammasome activation is implicated in pathogenesis. One example of such disease or condition is sepsis.

The application relates to the field of biological medicine, and discloses ascorbyl palmitate nanoliposomes capable of inducing tumor cell oncosis, a preparation method and application thereof. The nanoliposomes are constructed by inserting ascorbyl palmitate as a lipid component into a phospholipid bilayer, and are prepared by a film dispersion method from lecithin, cholesterol, pegylated phospholipid and ascorbyl palmitate. The average particle size of the nanoliposomes is 80-150 nm, the encapsulation rate is high, and the stability is good. The nanoliposomes can be administered through a tail vein, utilize the specific hydrolysis of matrix metalloproteinase MMP-2 which is highly expressed by tumor cells to hydrolyze ascorbyl palmitate, release palmitic acid and ascorbic acid, thereby inducing Caspase-independent oncosis of tumor cells, effectively overcoming apoptosis-related drug resistance, and reversing a tumor immunosuppressive microenvironment. The nanoliposomes avoid the cumulative toxicity of metal-type inducers, and provide a new safe and effective option for reversing chemotherapy resistance.

The invention belongs to the technical field of medicines, and particularly relates to an analogue of a cysteine zymogen activator (a PAC-1 analogue containing a carvone structure) and application of the analogue in cancer treatment. The invention relates to an analogue of a cysteaspase-3 activator, which is a PAC-1 analogue containing a carvone structure as shown in a formula I. The PAC-1 analogue disclosed by the invention is obtained by retaining structures such as piperazine ring and hydrazide, introducing a monoterpenoid carvone and carrying out structural modification on benzene rings on two sides, and a novel procaspase-3 activator is developed. The derivatives have stronger physiological activity. Pharmacological tests prove that the PAC-1 analogue can inhibit proliferation of various tumor cells and has good anti-cancer activity, and the preparation method of the PAC-1 analogue is simple, feasible and easy to operate.