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129 results about "Neurotoxicity" patented technology
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Neurotoxicity is a form of toxicity in which a biological, chemical, or physical agent produces an adverse effect on the structure or function of the central and/or peripheral nervous system. It occurs when exposure to substance – specifically, a neurotoxin – alters the normal activity of the nervous system in such a way as to cause permanent or reversible damage to nervous tissue. This can eventually disrupt or even kill neurons, which are cells that transmit and process signals in the brain and other parts of the nervous system. Neurotoxicity can result from organ transplants, radiation treatment, certain drug therapies (e.g., substances used in chemotherapy), recreational drug use, and exposure to heavy metals, bites from certain species of venomous snakes, pesticides, certain industrial cleaning solvents, and certain naturally occurring substances. Symptoms may appear immediately after exposure or be delayed. They may include limb weakness or numbness, loss of memory, vision, and/or intellect, uncontrollable obsessive and/or compulsive behaviors, delusions, headache, cognitive and behavioral problems and sexual dysfunction. Note there is strong evidence that chronic mold exposure in homes can lead to neurotoxicity which may not appear for months to years of exposure. All symptoms listed above are consistent with mold mycotoxin accumulation.
Application of compound for inhibiting phosphorylation of ARMC10 in preparation of medicine for antagonizing tin-induced nervous system injury
The invention relates to the technical field of related drugs for nerve injury caused by heavy metal pollution, in particular to application of a compound for inhibiting phosphorylation of ARMC10 in preparation of drugs for antagonizing tin-induced nervous system injury. Exposure of trimethyltin chloride induces nerve cell mitochondrial dysfunction, and the key mechanism is ARMC10 serine 43 site abnormal phosphorylation. Phosphorylated protein causes excessive mitochondrial fission, membrane potential collapse and energy metabolism disorder, resulting in neuron damage. Based on the target spot, a compound for antagonizing tin-induced nervous system injury is obtained through screening, protein phosphorylation can be specifically inhibited, mitochondrial dynamic unbalance and dysfunction induced by trimethyltin chloride are effectively reversed, and neurotoxicity is relieved. According to the technical scheme, the technical problem that in the prior art, no medicine for effectively antagonizing tin-induced nervous system injury exists can be solved, and the compound has the application potential for treating the nervous system injury and cognitive impairment caused by tin exposure.
Owner:ARMY MEDICAL UNIV
Application of serratia marcescens in preparation of medicine for treating gradual freezing
PendingCN121570501ANervous disorderBacteria material medical ingredientsAmyotrophic lateral sclerosisSerratia species
The invention discloses an application of serratia marcescens in preparation of a medicine for preventing or treating gradual freezing (amyotrophic lateral sclerosis, ALS) or frontotemporal dementia (FTD). Specifically, the serratia marcescens of the present invention can improve the phenotype of an asymptomatic and frontotemporal dementia model S59L by reducing mitochondrial unfolded protein response (UPRmt); meanwhile, expression of excitatory amino acid glutamic acid can be reduced, excitatory neurotoxicity can be relieved, and ALS and FTD phenotypes can be relieved through cooperation of the two.
Owner:CAPITAL UNIVERSITY OF MEDICAL SCIENCES
Pharmaceutical composition for treating Alzheimer's disease and preparation and detection methods thereof
PendingCN120585963ANervous disorderMaterial analysis by observing effect on chemical indicatorMedicinal herbsNeurotransmitter systems
The invention provides a pharmaceutical composition for treating Alzheimer's disease. The pharmaceutical composition is prepared from the following raw materials in parts by weight: 10-15 parts of ginseng, 10-15 parts of rhizoma acori graminei, 10-15 parts of polygala tenuifolia, 15-20 parts of rhizoma polygonati, 15-20 parts of ginkgo leaves and 5-10 parts of schisandra chinensis. Therefore, the ginseng and the ginkgo leaves jointly regulate a cholinergic system and cerebral blood flow, and the cognitive function is enhanced; the rhizoma acori graminei and the ginkgo leaves cooperate to inhibit aggregation of beta-amyloid protein, improve cerebral circulation and relieve neurotoxicity. Polygonatum sibiricum and Chinese magnoliavine fruit protect nerve cells through anti-oxidation and anti-inflammatory effects and reduce nerve injury. Schizandrin further stabilizes a neurotransmitter system and enhances the synergistic effect of other medicinal materials, a multi-layer treatment network of Abeta deposition inhibition, cholinergic system regulation, anti-inflammation and anti-oxidation and nerve protection is integrally formed, and the core pathological link of the Alzheimer's disease is comprehensively intervened, so that the cognitive function is improved, and the disease progress is delayed.
Owner:SHAANXI XIZHOU PHARM CO LTD
Method for predicting peripheral neurotoxicity induced by treatment of colorectal cancer through oxaliplatin
The invention discloses a method for predicting peripheral neurotoxicity induced by treatment of colorectal cancer through oxaliplatin, and relates to the technical field of drug application, and the method comprises the following steps: obtaining pre-drug patient information before treatment of a patient with oxaliplatin and clinical feature data after use; processing and feature analysis are carried out based on pre-drug patient information and clinical feature data, and a core feature data set related to neurotoxin is determined; and based on the core feature data set, predicting the oxaliplatin-induced peripheral neurotoxicity of the patient by adopting a pre-trained gradient boosting decision tree model, and outputting a prediction risk result. According to the method, the occurrence risk of peripheral neurotoxicity can be accurately predicted according to clinical indexes so as to guide clinical accurate medication.
Owner:AFFILIATED HOSPITAL OF JIANGNAN UNIV
Toxicity-enhanced neurotoxin recombinant protein and application thereof
ActiveCN120775067BPolypeptide with localisation/targeting motifAntibody mimetics/scaffoldsBinding peptideCell membrane
The application provides a toxicity-enhanced neurotoxin recombinant protein and application thereof, and belongs to the technical field of biological medicine. The recombinant protein comprises a botulinum toxin type A receptor binding domain and at least one GM1 binding peptide inserted into the botulinum toxin type A receptor binding domain, and the recombinin protein can recognize and bind to ganglioside GM1. The short peptide sequence capable of binding to ganglioside GM1 is introduced into the botulinum toxin type A receptor binding domain to obtain the recombinant protein, the binding capacity of the recombinant protein to ganglioside GM1 is enhanced, the target recognition and binding capacity of the recombinant protein to the nerve cell membrane are improved, the overall affinity and endocytosis efficiency of the recombinant protein to the nerve cell are improved, and the neurotoxicity of the botulinum toxin is enhanced. The application not only improves the binding efficiency of BoNT / A in the in-vitro nerve cell model, but also shows a higher toxicity level in the functional verification, and shows a good clinical conversion prospect.
Owner:NORTHWEST A & F UNIV
Dihydrotriticale flavones, methods for their preparation and uses thereof
The present application relates to the technical field of medicine, and in particular to a dihydrotricin, a preparation method and use thereof, the preparation method comprising the following steps: taking compound A, diisopropylethylamine and bromomethyl methyl ether to prepare compound B; taking compound C, diisopropylethylamine and bromomethyl methyl ether to prepare compound D; taking compound B and compound D, adding sodium hydroxide to prepare compound E; taking compound E, adding hydrochloric acid to prepare dihydrotricin after washing, separation, and concentration. The preparation method realizes efficient and large-scale synthesis of dihydrotricin. It is first confirmed that dihydrotricin can significantly resist A 1‑42 Oligomer-induced neurotoxicity has broad prospects in preventing and treating middle and late AD and delaying the progression of AD.
Owner:SHENZHEN SECOND PEOPLES HOSPITAL (SHENZHEN INST OF TRANSLATIONAL MEDICINE)
Application of dehydrounionine in the preparation of drugs that reduce polymyxin toxicity
This invention provides the application of dehydrouncitonin in the preparation of drugs that reduce polymyxin toxicity, belonging to the field of pharmaceutical technology. This invention uses dehydrouncitonin in combination with polymyxin. The combined use of dehydrouncitonin and polymyxin E increased the viability of HEK293T and RAW264.7 cells to 87.7% and 94.3%, respectively, with highly significant differences compared to the control, indicating that treatment with dehydrouncitonin in combination with polymyxin E can significantly inhibit the cytotoxic effect of polymyxin E. This invention uses a mouse model to demonstrate that treatment with dehydrouncitonin in combination with polymyxin E can significantly reduce the neurotoxicity and nephrotoxicity of polymyxin E alone in mice, specifically manifested in improved neurobehavioral effects and improved histopathological effects on brain and kidney tissues. This invention uses dehydrouncitonin in combination with polymyxin E to significantly inhibit the cytotoxic, neurotoxic, and nephrotoxic effects of polymyxin E.
Owner:CHINA AGRI UNIV
Pharmaceutical composition for treating pulmonary fibrosis complicated with depression and application thereof
The invention discloses a pharmaceutical composition for treating pulmonary fibrosis complicated with depression and application of the pharmaceutical composition, and belongs to the field of biological medicine. The pharmaceutical composition provided by the invention comprises harmine and deoxyvasicine, wherein the optimal mass ratio of harmine to deoxyvasicine is 1: 1.25. The curative effect of the pharmaceutical composition is verified by constructing a pulmonary fibrosis and depression combined mouse model, and experimental results show that the pharmaceutical composition provided by the invention can significantly improve the anti-fibrosis effect, can also effectively reduce the neurotoxicity of harmine, shows a synergistic effect, and can be used for preparing anti-fibrosis drugs for treating or preventing the fibrosis. And the curative effect and the safety are both improved. The invention lays a foundation for developing a safe and efficient novel medicine for treating pulmonary fibrosis combined with depression, and has important application value and wide application prospect in treatment of patients with pulmonary fibrosis combined with depression.
Owner:FIRST AFFILIATED HOSPITAL OF XINJIANG MEDICAL UNIVERSITY
Defibrotide for the prevention and treatment of cytokine release syndrome and neurotoxicity associated with immunodepletion
ActiveUS12527811B2Polypeptide with localisation/targeting motifOrganic active ingredientsNeurotoxicityImmunotherapy
The present disclosure provides method of preventing, lessening the effects, or treating cytokine release syndrome (CRS) or related disorders, and / or neurotoxicity associated with immunotherapy comprising administering defibrotide. The defibrotide can be administered after the immunotherapy begins or be administered prophylactically before immunotherapy begins or before the patient develops CRS and / or neurotoxicity.
Owner:RICHARDSON PAUL G
Nasal injection type baicalein hydrogel as well as preparation method and application thereof
The invention discloses nasal injection type baicalein hydrogel as well as a preparation method and application thereof. The preparation method comprises the following steps: dissolving carboxymethyl chitosan in water, stirring to form a uniform carboxymethyl chitosan solution, then adding a 4-formylphenylboronic acid / baicalein solution, and then continuously stirring until yellow transparent hydrogel is formed, namely the nasal injection type baicalein hydrogel is obtained. The hydrogel has self-healing ability and proper viscosity, can be adhered to the epithelium of the nasal cavity and is continuously released in the microenvironment of the nasal cavity, so that the brain entering efficiency of the baicalein is remarkably improved; neurotoxic oligomers formed by abnormal aggregation of alpha-syn can be reduced; neuroinflammation can be relieved by regulating and controlling phenotypic polarization of microglial cells M2; oxidative stress can be improved by removing excessive ROS, dopaminergic neuron apoptosis is reduced, and the compound can be used for treating Parkinson's disease and has a good application prospect.
Owner:GUANGZHOU UNIVERSITY OF CHINESE MEDICINE
Compositions for treating neurodegenerative diseases and methods thereof
Disclosed herein are compounds and methods of use thereof effective for the treatment of neurodegenerative diseases such as amyotrophic lateral sclerosis (ALS), a disease that affects nerve cells in the brain and spinal cord, eventually causing loss of muscle strength. The compounds of the disclosure include, cutamesine, a synthetic sigma receptor agonist selective for the 81 receptor, and also a chaperone protein of the central nervous system that plays a key role in the modulation of calcium ions and apoptosis, as well as a sapogenin, such as smilagenin, a non-peptide neurotrophic factor that aids in the reversal of free radical neurotoxicity.
Owner:RAYA THERAPEUTIC INC
Method for screening key neurotoxic substances in food raw materials and their products by combining caenorhabditis elegans model with metabolomics
This invention discloses a method for screening key neurotoxic substances in food raw materials and their products using a *C. elegans* model combined with metabolomics. Food samples are processed to prepare a stock solution, which is then used to cultivate *C. elegans*. The sample exhibiting the greatest neurotoxicity to the nematodes is identified by analyzing the number of *C. elegans* movements and neuronal fluorescence images. Subsequently, key neurotoxic substances in food are systematically screened using a combination of non-targeted liquid chromatography-tandem mass spectrometry (LC-MS / MS) and a metabolomics platform. This application establishes a novel method for screening neurotoxic substances by combining nematode activity with non-targeted LC-MS / MS determination and a non-targeted metabolic platform, clarifying key neurotoxic substances in food and providing a theoretical basis for food quality control and high-quality development.
Owner:SOUTH CHINA AGRICULTURAL UNIVERSITY
A photosensitizer targeting beta amyloid and its preparation method and application
The application discloses a photosensitizer targeting beta amyloid, and a preparation method and application thereof. The photosensitizer is a photosensitizer with A-D-A configuration, and a structural formula thereof is shown as formula I. The photosensitizer synthesized in the application has a longer emission wavelength, and after being combined with beta amyloid, the fluorescence signal is obviously enhanced, and can effectively generate singlet oxygen, that is, the photosensitizer can target mark A beta protein, and is used for fluorescence imaging of the A beta protein; and after the photosensitizer synthesized in the application is combined with beta amyloid in the brain of an Alzheimer's disease (AD) model mouse, the cognitive ability of the AD mouse can be effectively improved, A beta-mediated neurotoxicity can be reduced, and clearance of A beta plaques can be promoted, that is, the photosensitizer can be used for early diagnosis and treatment of Alzheimer's disease.
Owner:SOUTH CHINA UNIV OF TECH
Use of fractalkine in the preparation of a medicament for preventing or treating repair of white matter damage
This invention provides the application of fractalkine in the preparation of drugs for the prevention or treatment of white matter injury repair. In animal models of cerebral hemorrhage, it was found that the mass effect of hematoma in the basal ganglia and the neurotoxic products generated by its lysis lead to damage to surrounding white matter fiber bundles. Fractalkine plays an important role in regulating microglial activation after cerebral hemorrhage to promote white matter repair.
Owner:THE SECOND AFFILIATED HOSPITAL OF CHONGQING MEDICAL UNIV
A method and system for assessing car-t treatment-related neurotoxicity based on behavioral characteristics
ActiveCN121003418BDiagnostic signal processingEnsemble learningCross correlation analysisComputational physics
The application discloses a method and system for evaluating CAR-T treatment related neurotoxicity based on behavior characteristics, relates to the technical field of medical behavior analysis, and provides the following scheme, which comprises the following steps: synchronously collecting angular velocity time series data of double upper limbs of a patient and electromyographic signals corresponding to muscle surfaces of the double upper limbs; performing frequency band optimization filtering on the angular velocity time series data of the double upper limbs respectively; generating angular velocity waveforms; taking a wave peak time point of the angular velocity waveform as a reference; extending forward for a preset time length; and calculating an energy integral curve of the electromyographic signals. The angular velocity time series data of the double upper limbs is processed through frequency band optimization to generate angular velocity waveforms, the energy integral curve of the electromyographic signals is extracted forward based on the wave peak time point of the angular velocity, candidate time points are obtained, and local cross-correlation analysis is enabled to locate and intercept points when the wave peak value is lower than a preset threshold, so that the problem of missing weak tremor signals is solved, effective detection and reliable interception of low-amplitude tremors are realized, and weak signal features are avoided from being lost.
Owner:SUN YAT SEN UNIV
Use of gallic acid in the preparation of a medicament for preventing or treating peripheral neuropathy
The application relates to a pharmaceutical application technology, in particular to application of gallic acid in preparation of a medicine for preventing or treating peripheral neuropathy. The peripheral neuropathy is acute peripheral neuropathy caused by using a chemotherapy drug, oxaliplatin. The gallic acid has a protective effect on acute peripheral nerve toxicity of mice induced by oxaliplatin. The medicine, gallic acid, can be used as an adjuvant of a chemotherapy drug for cancer treatment, and has a significant alleviating effect on nerve toxicity caused by chemotherapy.
Owner:JIANGSU PROVINCE INST OF TRADITIONAL CHINESE MEDICINE
Umami peptide without nervous excitatory toxicity as well as preparation process and application of umami peptide
The invention provides an umami peptide without nervous excitatory toxicity and a preparation process and application thereof, the umami peptide is extracted from broad bean protein, and the amino acid sequence is shown as SEQ ID NO.1 and / or SEQ ID NO.2. Compared with a traditional umami substance-sodium glutamate (monosodium glutamate MSG), the umami peptide has the characteristics of activating umami receptors TAS1R1 / TAS1R3 without acting on sodium glutamate receptors such as NMDA and the like, and has the advantages that the umami peptide can be used for preparing the umami peptide. No NMDA receptor mediated excitatory neurotoxicity exists; meanwhile, the umami peptide can stimulate intestinal endocrine cells (STC-1) to secrete GLP-1.
Owner:ZHEJIANG UNIV
Microorganism-intestine-brain axis-based neurotoxicity antagonist screening and evaluation method
The invention belongs to the field of bioengineering and neurotoxicity prevention and control, and particularly relates to a neurotoxicity antagonist screening and evaluating method based on a microorganism-intestine-brain axis. The screening method of the neurotoxicity antagonist comprises the following steps: establishment of a neurotoxicity animal model, verification of the neurotoxicity model, sequencing of intestinal flora and screening of key flora, coupling analysis of flora-cranial nerve indexes, verification of candidate microorganisms, screening of core bacterial metabolites, verification of the core bacterial metabolites and verification of the core bacterial metabolites. According to the method, through behavior-neurotransmitter-inflammation-gene / mitochondrial function multi-level index linkage, a reproducible recovery index (RI) index is established, and quantitative screening and grading judgment of candidate strains and metabolites of the candidate strains on nerve injury repair are achieved.
Owner:NANJING AGRICULTURAL UNIVERSITY +1
Application of HIF-1alpha inhibitor in preparation of product for inducing transformation of astrocytes from pro-inflammatory type to anti-inflammatory type
The invention belongs to the technical field of biological medicines, and relates to application of an HIF-1alpha inhibitor in preparation of a product for inducing transformation of astrocytes from a pro-inflammatory type to an anti-inflammatory type. The invention reveals that activation of an HIF-1 signal channel is an important mechanism for driving neuroinflammatory response and pro-inflammatory A1 type astrocyte formation, and inhibition of HIF-1 activation can effectively promote generation of neuroprotective A2 type astrocytes. By applying the HIF-1alpha small-molecule inhibitor KC7F2 to astrocytes, HIF-1alpha activation is blocked, and the astrocytes are promoted to be converted from a proinflammatory A1 phenotype to an anti-inflammatory A2 phenotype, so that inflammatory response is inhibited, neurotoxicity is reduced, and a neuron microenvironment is improved. The invention provides a novel intervention strategy based on HIF-1alpha signal regulation and control, and a novel theoretical basis and a novel potential drug treatment scheme are provided for treatment of nervous system injury and related neurodegenerative diseases.
Owner:SUZHOU INST OF NANO TECH & NANO BIONICS CHINESE ACEDEMY OF SCI
Caenorhabditis elegans exposure evaluation method based on neural behavior multi-parameter integration
The invention relates to the technical field of biological detection and toxicological evaluation, and discloses a neural behavior multi-parameter integration-based caenorhabditis elegans exposure evaluation method which comprises the following specific steps: S1, synchronous culture of caenorhabditis elegans; s2, pollutant exposure treatment; s3, multi-parameter behavior detection; s4, data standardization processing; and S5, constructing a comprehensive evaluation model, and performing weighted integration on four core parameters including the movement speed, the chemotactic index, the synaptic spot density and the calcium signal amplitude after standardization to construct a neurotoxicity index NTI. According to the method disclosed by the invention, a multi-layer and multi-dimensional neurotoxicity evaluation system is constructed by integrating four types of neurobehavior parameters including motion behaviors, chemotactic reactions, synaptic morphology and neuron calcium signals, and the defect that a traditional single endpoint index cannot comprehensively reflect overall disturbance of a neural regulation network is overcome; by utilizing the high homology of the nervous system of caenorhabditis elegans and the human nerve gene, the clinical correlation and mechanism analysis capability of environmental pollutant neurotoxicity evaluation are remarkably improved.
Owner:SOUTHEAST UNIV
Gel emplastrum for treating oxaliplatin peripheral neurotoxicity and preparation method of gel emplastrum
PendingCN121971569ANervous disorderPharmaceutical non-active ingredientsAngelica Sinensis RootBlood drug concentration
The invention provides a gel emplastrum for treating oxaliplatin peripheral neurotoxicity and a preparation method, and relates to the field of traditional Chinese medicine, the gel emplastrum comprises a backing layer, an emplastrum layer and an anti-sticking layer; the paste layer is a gel layer formed by traditional Chinese medicine extract and a matrix for loading the traditional Chinese medicine extract; the traditional Chinese medicine extract is prepared from a traditional Chinese medicine composition; the traditional Chinese medicine composition comprises astragalus membranaceus, angelica sinensis, vinegar rhizoma sparganii, vinegar curcuma zedoary, cassia twig, achyranthes bidentata and pheretima in a mass ratio of 6: 3: 2: 2: 2: 4: 2. The matrix comprises a framework material, a cross-linking agent, a cross-linking regulator, a thickening agent, a humectant, a complexing agent, pure water, a preservative, a penetration enhancer, a thermal inductance regulator and a high-performance emulsifying thickening agent. The problems that in the prior art, a formula for promoting blood circulation to remove blood stasis is inconvenient to use in a soaking and washing main use mode, the patient compliance is poor, the speed of medicine entering the body of a patient is not easy to control, the blood concentration in the body of the patient is difficult to maintain stably, and the peripheral neurotoxicity treatment progress is difficult to control can be solved.
Owner:AFFILIATED HOSPITAL OF JIANGNAN UNIV
N-methyl-D-aspartic acid receptor interference peptide and application thereof
PendingCN120904290ANervous disorderPeptide/protein ingredientsHippocampal regionAspartic acid receptors
The invention discloses an N-methyl-D-aspartic acid receptor NR2B subunit interference peptide and an application of the N-methyl-D-aspartic acid receptor NR2B subunit interference peptide. Through reasonable design and synthesis, the interference peptide can be specifically combined with endogenous neurotoxic metabolite quinolinic acid (QA), and the combination between the QA and NR2B is blocked in a competitive mode, so that the NR2B-mediated excitatory neurotoxic reaction is selectively inhibited. The polypeptide can remarkably reverse neuron damage and shows an excellent nerve protection effect. In an obesity-related cognitive impairment model and an Alzheimer's disease mouse model, the interference peptide recovers neuronal synaptic injury in a hippocampus region by blocking a QA-NR2B signal channel, effectively improves cognitive hypofunction, and provides an innovative intervention strategy for prevention and treatment of neurodegenerative diseases.
Owner:XUZHOU MEDICAL UNIVERSITY
Device for preventing peripheral nerve injury caused by chemotherapy
The invention provides a device for preventing peripheral nerve injury caused by chemotherapy. The device is used for at least solving the technical problem of peripheral nerve injury caused by chemotherapy in the prior art. The invention provides a device for preventing peripheral nerve injury caused by chemotherapy, which comprises a first heat exchange area which has a first temperature, can be in direct or indirect contact with skin and covers one or more positions close to an artery position, a palm position and a sole position, and a second heat exchange area which has a second temperature and can be in direct or indirect contact with the skin and covers one or more positions close to the artery position, the palm position and the sole position. The second heat exchange area can make direct or indirect contact with the skin and cover at least one position of the positions not in the first heat exchange area, the heat exchange assembly exchanges heat with the first heat exchange area and the second heat exchange area, the first heat exchange area is kept at the first temperature, and at least part of the second heat exchange area is kept at the second temperature. The first heat exchange area for cooling and the second heat exchange area for heating are arranged according to the blood flow direction of the blood vessel, the blood flow can be reduced, neurotoxicity or complications can be reduced, and the body temperature is kept.
Owner:THE THIRD AFFILIATED HOSPITAL OF ZHEJIANG CHIENSE MEDICAL UNIV
Neurotoxicity-free VSV vector recombinant oncolytic virus carrying Marburg virus deficient G protein
The invention discloses a neurotoxicity-free VSV vector recombinant oncolytic virus carrying Marburg virus deficient G protein, which is characterized in that a G protein coding gene of wild VSV is replaced by a coding gene of Marburg virus deficient G protein through a reverse genetic manipulation technology, so as to save and obtain a recombinant oncolytic virus VSV-MARG-delta MLD capable of being autonomously replicated. The invention has the advantages of no neurotoxicity and efficient oncolytic activity.
Owner:ZHEJIAN DIFFERENCE BIOLOGICAL TECH CO LTD
Monoacylglycerol lipase (MAGL) inhibitors for the treatment of pain and related medical disorders
This invention discloses a novel class of monoacylglycerol lipase (MAGL) small molecule inhibitors, as well as their pharmaceutically acceptable compositions, methods of preparation, and uses. The MAGL small molecule inhibitors are represented by formula (I), having the specific substituents and definitions described herein. The disclosed MAGL small molecule inhibitors exhibit excellent MAGL enzyme inhibitory activity. This invention includes these compounds or their pharmaceutically acceptable compositions for the treatment and / or prevention of MAGL-related conditions such as multiple sclerosis, Alzheimer's disease, Parkinson's disease, amyotrophic lateral sclerosis, traumatic brain injury, neurotoxicity, stroke, epilepsy, anxiety, migraine, depression, hepatocellular carcinoma, colorectal cancer lesions, ovarian cancer, neuropathic pain, chemotherapy-induced neuropathy, acute pain, chronic pain, and / or pain-related spasticity.
Owner:YICHANG HUMANWELL PHARMA CO LTD
Application of cGAS-STING pathway inhibitor in relieving AAV-induced neural immune response
The invention relates to the technical field of biological medicine, and particularly discloses application of a cGAS-STING pathway inhibitor in relieving neural immune response induced by AAV, and the technical key points are as follows: it is found that high-dose AAV can activate a cGAS-STING signal pathway in a nervous system, resulting in inflammatory response, glial cell activation, T cell infiltration and neuron damage; the cGAS-STING pathway is inhibited by means of gene knockout (Stin < + / ->), pharmacological inhibition (such as STING inhibitor H-151) or virus-mediated gene knockout (shSTING) and the like, so that the AAV-induced immune response and neurotoxicity can be effectively reduced, and meanwhile, the expression of a transgenic product carried by the AAV vector is improved. The scheme provided by the invention provides a new strategy and means for optimizing the safety-effectiveness balance of AAV gene therapy.
Owner:JINAN UNIVERSITY
High-flux toxicity pre-evaluation substitution method based on acetylcholin esterase target
PendingCN121950997AEnsure comparabilityGuaranteed standardizationHydrolasesMicrobiological testing/measurementEngineeringNerve cells
The invention discloses a high-flux toxicity pre-evaluation substitution method based on an acetylcholin esterase target. By integrating an SH-SY5Y nerve cell endogenous AChE and recombinant exogenous AChE dual detection system and relying on an automatic screening system constructed by integrating core equipment such as an automatic pipetting workstation, a constant-temperature incubator and a multifunctional microplate reader, a high-flux toxicity pre-evaluation substitution method based on an AChE target is successfully established and is used for evaluating the neurotoxicity of a compound, and the method has the advantages of high sensitivity, high sensitivity, high sensitivity and the like. The method solves the limitation that a single screening method in the prior art cannot evaluate factors such as target inhibition, cell permeability and metabolic transformation at the same time, and the method is simple, convenient, rapid, high in accuracy and suitable for large-scale primary screening of the AChE inhibitor and early warning of neurotoxicity risks.
Owner:DALIAN UNIV OF TECH
Neuro-attenuating ketamine and norketamine compounds, derivatives thereof, and methods
The present invention is directed to novel neuro-attenuating norketamine (NANKET) compounds according to any one of formulas (I—shown below), (I-A) and (I-B), or any of the compounds described in Tables A-D, or in any of the Examples provided herein, and pharmaceutically acceptable salts thereof, novel pharmaceutical formulations and novel methods of uses thereof. The present invention also features novel oral neuro-attenuating ketamine (NAKET) and neuro-attenuating norketamine (NANKET) modified-release pharmaceutical formulations, and novel methods of administration thereof, which ensure the steady release of a therapeutically effective amount of ketamine, norketamine, or derivatives thereof from the oral modified-release pharmaceutical formulations without neurologically toxic spikes in plasma concentration of the ketamine, norketamine, or derivatives during the release periods.
Owner:ACADIA PHARMACEUTICALS INC
Toxicity-enhanced neurotoxin recombinant protein
ActiveCN120775067APolypeptide with localisation/targeting motifAntibody mimetics/scaffoldsBinding peptideCell membrane
The invention provides a toxicity-enhanced neurotoxin recombinant protein and application thereof, and belongs to the technical field of biological medicines. The recombinant protein comprises an A-type botulinum toxin receptor binding domain and at least one GM1 binding peptide inserted into the A-type botulinum toxin receptor binding domain, and the recombinant protein can recognize and bind to ganglioside GM1. The oligopeptide sequence capable of being combined with the ganglioside GM1 is introduced into the A-type botulinum toxin receptor binding structural domain, and the recombinant protein is obtained, so that the combining capacity of the A-type botulinum toxin receptor binding structural domain to the ganglioside GM1 is enhanced, the targeting recognition and combining capacity of a nerve cell membrane of the A-type botulinum toxin receptor binding structural domain is further improved, the overall affinity and endocytosis efficiency of the A-type botulinum toxin receptor binding structural domain and the nerve cell membrane are improved, and the aim of treating the neurotoxin is achieved. The neurotoxicity of the carnotoxin is enhanced. According to the invention, not only is the binding efficiency of BoNT / A in an in-vitro nerve cell model improved, but also a higher toxicity level is shown in functional verification, and a good clinical transformation prospect is shown.
Owner:NORTHWEST A & F UNIV
Anti-epileptic stiff silkworm polypeptide as well as preparation method and application thereof
The invention belongs to the technical field of biological medicines, and provides an anti-epileptic stiff silkworm polypeptide as well as a preparation method and application thereof. The bombyx batryticatus polypeptide is a peptide fragment with an amino acid sequence as shown in SEQ ID No.1, and is RFAFPAWI (PP6). The method comprises the following steps: preparing a peptide extract in stiff silkworm by simulating gastrointestinal digestion, identifying peptide in stiff silkworm polypeptide by using Nano LC-MS / MS, and carrying out difference analysis; differential peptides with potential anti-epileptic activity are obtained through virtual screening, and the anti-epileptic stiff silkworm polypeptide PP6 with potential anti-epileptic activity is synthesized. PP6 has a neuroprotection effect on PC12 cell neurotoxicity damaged by glutamic acid (Glu) by adjusting a GABA signal channel, and has an anti-epileptic effect on an epileptic mouse induced by pentaerythrityl tetrazole (PTZ). Therefore, PP6 may be a new leading peptide compound for developing epileptic drugs, and the anti-epileptic polypeptide can be widely applied to the fields of medicines, foods and the like to achieve the anti-epileptic target.
Owner:SHANXI UNIV OF CHINESE MEDICINE