63results about How to "Significant neuroprotective effect" patented technology

The invention belongs to the field of medicament technology, and especially relates to applications of a tetramethylpyrazine derivative tetramethylpyrazine nitrone to medicament preparation as well as prevention and treatment of brain injury diseases. Experiments prove that tetramethylpyrazine nitrone can improve traumatic brain injury and brain injury after subarachnoid hemorrhage; the improvements concretely comprise the following aspects: improvement of behaviors of model rats with traumatic brain injury and subarachnoid hemorrhage, reduction of cerebral infarction areas due to traumatic brain injury, improvement of vasospasm state after subarachnoid hemorrhage, and protection of brain tissues. Mechanisms of action of tetramethylpyrazine nitrone relate to inhibition of oxidative stress injuries, inhibition of inflammatory reactions, and apoptosis resistance. Tetramethylpyrazine nitrone can be used as a medicine for preventing and treating brain injury diseases, especially traumatic brain injury and subarachnoid hemorrhage, and can be prepared into various dosage forms with medicinal carriers.

The invention belongs to the technical field of medicinal chemistry and discloses a N-(1,2,3,4-tetrahydroisoquinolinyl)-feruloylagmatine-O-alkylamine compound (I) and pharmaceutically acceptable salt, and a preparation method and application thereof. The structure is as shown in a formula I. The compound (I) provided by the invention has high butyrylcholine esterase inhibiting activity, anti-oxidation activity and Abeta1-42 aggregation inhibiting activity, and has remarkable neuroprotective function on PC12 cell injury induced by hydrogen peroxide, which indicates that the compound is a multi-target-point inhibitor. The compound further shows a good effect of treating alzheimer disease in in-vivo experiments, and has low toxicity and a good clinical application prospect.

The invention provides application of sparassis crispa polysaccharide extracts to preparing medicines for treating neurodegenerative diseases, and relates to the technical field of medicines. The sparassis crispa polysaccharide extracts are prepared through fermentation, ethanol extraction and vacuum drying; and in-vitro tests prove that the remarkable neuroprotection activity effect is achieved. The sparassis crispa polysaccharide extracts are simple in preparing method and low in cost, and can be used for preparing the medicines for treating the neurodegenerative diseases such as the Parkinson's disease and the senile dementia.

Belonging to the pharmaceutical field, the invention relates to application of nicotinamide phosphoribosyltransferase (NAMPT) in preparation of neuroprotective and rehabilitation drugs. Experiments of the invention show that NAMPT recombinant protein can penetrate the blood-brain barrier to significantly reduce the volume of ischemic brain injury and alleviate white matter injury after ischemic brain injury; the NAMPT recombinant protein can significantly improve long-term behaviors after ischemic brain injury; the NAMPT recombinant protein can raise revascularization related factors to enhance revascularization after brain hypoxia and neuron regeneration after brain hypoxia, and promote post-injury neurologic function reestablishment; and by mediating oligodendrocyte regeneration and alleviating the demyelination effect of local lysolecithin, the NAMPT recombinant protein can promote restoration of white matter after injury and strengthen post-injury neurologic function reestablishment. Results show that the NAMPT recombinant protein plays a long-term neuroprotective role in drugs treating cerebral stroke, traumatic brain injury and multiple sclerosis, and can be used as a neuroprotective drug to treat acute and chronic injury caused by brain stroke.

The invention provides a new application of echinacoside. Natural micromolecule active compound echinacoside has selective peculiar protection effect on injury of nerve cells, the echinacoside can activate TrkA/B receptors, and the nerve protection effect of the echinacoside can be reversed by restraining the receptors from being activated through Trk receptor specificity inhibitors. Vein medication of the echinacoside can generate obvious nerve protection effect, and simultaneously long-time vein medication causes no obvious liver and renal toxicity.

The invention relates to the application of the neurotrophic factor conservative dopaminergic neurotrophic factor (cerebral dopamine neurotrophic factor, CDNF) in the preparation of ischemic cerebrovascular disease medicine. The inventors discovered for the first time that CDNF has the function of reducing the area of ​​cortical ischemia and improving the recovery of animal motor ability, and further found that the protective effect of CDNF on neurons and glial cells is not regulated by the endoplasmic reticulum stress pathway. CDNF can be designed as a targeted drug to prevent and treat ischemic stroke, which has great potential application value in the clinical prevention and treatment of ischemic stroke, and lays the foundation for further research on the biological function of CDNF.

The invention discloses a [3,5-disubstituted phenyl-1-(1,2,4-triazole)]benzenesulfonic acid derivative, a preparation method and applications thereof, wherein a benzoic acid raw material is substituted, an acylation reaction and a condensation cyclization reaction with substituted benzamide are performed, and a reaction is performed with a p-hydrazinobenzenesulfonic acid derivative to obtain a target product [3,5-disubstituted phenyl-1-(1,2,4-triazole)]benzenesulfonic acid derivative. According to the present invention, the compound can effectively antagonize nerve cell oxidative stress damagecaused by hydrogen peroxide, sodium nitroprusside, iron ions and copper ions, can repair mitochondrial function by scavenging free radicals and restoring mitochondrial membrane potential, and has significant protection effect on neuronal cells; and the compound has neuroprotective effects of free radical scavenging and targeting mitochondria protection, and can be used for preparing drugs for prevention and treatment of neurodegenerative diseases such as stroke, brain injury, spinal cord injury, Parkinson's disease, Alzheimer's disease, amyotrophic lateral sclerosis, and the like.

The invention discloses a tricyclic diterpenoid derivative as shown in a formula (I) and a preparation method of the tricyclic diterpenoid derivative. A series of novel tricyclic diterpenoid derivatives as shown in the formula (I) can be prepared by taking the tricyclic diterpenoid derivative as shown in a formula (5) as a leading compound through such reactions as esterification, amidation, protection, acylation and deprotection. Furthermore, the invention also provides an application of the tricyclic diterpenoid derivative in preparation of neuroprotective drugs.

The invention discloses an effective part of a traditional Chinese medicine for treating Alzheimer disease and a preparation method and an application thereof. The effective part of the traditional Chinese medicine for treating Alzheimer disease is prepared by a method consisting of the following steps of: taking 6 parts of gambir plant, 4 parts of radix bupleuri, 6 parts of angelica sinensis, 6 parts of ligusticum wallichii, 8 parts of rhizoma atractylodis, 8 parts of poria cocos and 3 parts of liquorice; adding alcohol or water of which the weight is 5-15 times more than the total weight of all medicine materials, and extracting for 2-4 times by refluxing, wherein each extraction is performed for 1.5-4 hours; combining extracting solutions, concentrating to be without the smell of alcohol, and thus obtaining the concentrated solution; and putting the concentrated solution on a macroporous resin column, eluting in gradient by using ethyl alcohol solutions with the ethyl alcohol concentrations of 0-95%, collecting ethyl alcohol eluent with the concentration of 30%-50%, recovering solvent, and thus obtaining the effective part of the traditional Chinese medicine. According to the preparation method of the effective part of the traditional Chinese medicine for treating Alzheimer disease, a certain separating means is utilized to separate the effective part from liver restricting powder, and a modern pharmacological experiment method is used for proving that the neuroprotective effect of the effective part is obviously superior to that of the extract of the liver restricting powder, and thus the preparation method can be used for preparing medicines for resisting Alzheimer disease.

The invention provides an application of sodium valproate to preparation of a medicine for restraining formation of glial scars. The structural formula of the sodium valproate is as shown in the description. Through experiment, the inventor finds that the sodium valproate has remarkable cranial nerve protecting effects, and can effectively restrain activation of primary astroglia cells and notablyrestrain the formation of the glial scars after the brain tissue of mice is damaged, so that the encephalatrophy volume of mice suffering from local cerebral ischemia can be obviously improved, the neurological symptoms of the mice can be notably improved, and restoration can be promoted; and the above situation indicates that the sodium valproate has important application value in preparation ofthe medicine for restraining the formation of the glial scars.

The invention belongs to the technical field of medicine, and relates to a (N-1,2,3,4-tetrahydroisoquinolinyl)-feruloylagmatine compound, and a preparation method and application thereof. The structure is as shown in a formula I (the formula I is as shown in the description). The (N-1,2,3,4-tetrahydroisoquinolinyl)-feruloylagmatine compound provided by the invention has excellent butyrylcholine esterase inhibiting activity, remarkable Abeta1-42 aggregation inhibiting activity, anti-oxidation activity and high neuroprotective activity on PC12 cell injury induced by hydrogen peroxide in in-vitro experiments; and the (N-1,2,3,4-tetrahydroisoquinolinyl)-feruloylagmatine (I) compound is a multi-target-point inhibitor, further shows a good effect of treating alzheimer disease in in-vivo experiments, and has low toxicity and a good clinical application prospect.

The invention belongs to the field of medical technology, and relates to an application of n-3 unsaturated fatty acid in preparation of a medicine for preventing and treating traumatic brain injury. The experimental results about the function of n-3PUFAs (polyunsaturated fatty acids) in resisting traumatic brain injury show that the n-3 unsaturated fatty acid can remarkably improve sense and motor functions of a mice after traumatic brain injury, slightly reduces the deletion of brain tissue after injury, inhibits the inflammatory response from excessive activation, promotes the repair of white matter damage, obviously reduces the degeneration and necrosis of nerve cells of CA3 area of hippocampus, and improves the study and memory functions. The n-3PUFAs has a definite neuroprotective effect in resisting brain injury, can be used for preparing nerve protective medicines, and can be used for preventing and treating acute or chronic injury caused by the traumatic brain injury.

The invention relates to the technical field of pharmaceutics and discloses the application of the compound AM-1241, namely (R,S)-3-(2-iodo-5-nitrobenzene formyl)-1-(1-methyl-2-piperidinyl methyl)-1H-indol to preparation of a drug for treating Parkinson's disease. According to the compound, a cannabinoid receptor CB2 is used as the effective target spot of Parkinson's disease treatment, and symptoms of Parkinson's disease can be relieved greatly; furthermore, a molecular mechanism shows that CB2 expression of substantia nigra and hippocampus are activated, the occurrence rate of neuronal apoptosis is reduced, and a remarkable neuroprotective effect is realized; besides, by preparing the compound into solid lipid nanoparticle preparations for administration, drug absorption rate and brain-targeting effect can be improved, so that Parkinson's disease treatment effect is further improved. It is expected to prepare the drug for treating Parkinson's disease with the compound as the effective constituent, and the drug can become the substitution of existing levodopa drugs.

The invention discloses use of neuregulin 1, belongs to the technical field of a biomedicine, and particularly relates to application of the neuregulin 1 inpreparation of a drug for treating lead encephalopathy. The characteristics of the lead encephalopathy are high expression of inflammatory cells and inflammatory factors and wide neuronal cell death. Neuron loss and nerve inflammatory reaction play a crucial role in the lead encephalopathy process. The neuregulin 1 has a significant nerve inflammatory reaction and a role of protecting cell apoptosis in the lead encephalopathy, can inhibit inflammatory activation, reduces the quantities of microglial cells and astrocytes, reduces the expression level of inflammatory cytokines COX-2, and improves the learning and memory defects caused by lead poisoning. In addition, the quantity of ErbB4 positive cells can be increased by the neuregulin 1; the inhibition apoptosis activity of anti-apoptosis protein Bc1-2 is improved; expression of pro-apoptotic protein Bax is reduced, so that apoptosis is inhibited, and neuregulin 1 has significant neuroprotective effects on the lead encephalopathy.

The invention provides compounds of the structure as shown in the description or pharmaceutical salt, a pharmaceutical composition and application of the compounds. The compounds relate to a series of carbazole and rivastigmine diads. The carbazole and rivastigmine diads are connected through proper joints, on one hand, a good nerve protection effect can be achieved, and on the other hand, proliferation of neural stem cells is promoted.

The invention discloses an acetylcholine esterase inhibitor, (N-(2-(1H-indole-3-yl)ethyl)-3-amino-6-methyl-5,6,7,8-tetrahydrothiophene [2,3-b][1,6]naphthyridin-2-carboxamide, and applications of the inhibitor in preparation of drugs for preventing and/or treating AChE-related diseases and drugs for preventing and/or treating diseases caused by Abeta-induced nerve damage. The compound provided by the invention can inhibit AChE and has a significant neuroprotective effect on the Abeta-induced nerve damage, and can be used for preparation of the drugs for preventing and/or treating related neurodegenerative diseases such as Alzheimer Disease (AD).

The invention discloses application of 5-(3', 5'-dimethoxybenzylidene)-2-sulfo-imidazole-4-one to preparation of drugs for treating cerebrovascular diseases. According to relevant researches disclosed by the invention, the compound has a remarkable cerebral nerve protection effect, can obviously reduce the volume of cerebral infarction of a focal cerebral ischemia rat and can obviously improve neurological signs; and moreover, the protection effect of an IV4 compound to cerebral ischemic injuries is related to the inhibition of the activation of lysosomal enzyme cathepsin B, so that the compound can be used for preparing drugs for preventing or treating diseases such as ischemic brain injuries, cerebral hemorrhage, cerebral thrombosis, cerebral embolism, cerebral infarction, cerebral stroke, lacunar infarction, transient ischemia attacks, cerebral arteriosclerosis and diabetic cardiovascular complications.

The invention relates to a salidroside derivative and a preparation method and application thereof, and particularly provides a compound shown in a formula I, or salt thereof, or a stereoisomer thereof, or a crystal form thereof. The salidroside derivative shown in the formula I solves the problem of poor lipid solubility of salidroside, and can overcome the defects of low bioavailability and fastmetabolism of the salidroside in clinical application; and meanwhile, the salidroside derivative can effectively resist CoCl 2-induced PC12 cell apoptosis, has an excellent neuroprotective effect ona CoCl 2-induced PC12 cell hypoxia injury model, can be used for preparing drugs for preventing and/or treating various nervous system diseases (including parkinson disease, alzheimer disease, cerebral apoplexy and the like) related to cell hypoxia injury, and has broad application prospects.

The invention discloses application of 4-methoxybenzyl alcohol in preparation of neuroprotective drugs. 4-methoxybenzyl alcohol may reduce injury of primary cortical neurons OGD/Rep of fetal rats and neuron morphological structure injury and increase survival rate of OGD/Rep injured cortex; the release of OGD/Rep injured cortical neuron NO is reduced, activity of SOD (superoxide dismutase) in cells is improved, generation of MDA (methane dicarboxylic aldehyde) is inhibited, apoptosis of nerve cells may be inhibited through significant up-regulation of Bcl-2 protein expression and down-regulation of Bax protein and Caspase-3 protein expression, neuroprotective effect is good, neuroprotective drugs may be produced, and nerve injury is reduced; in addition, the 4-methoxybenzyl alcohol may promote synapse growth of nerve cells, up-regulate synapse growth related proteins, promote repair of the nerve cells and treat nerve injury.

The invention discloses a substituted pyrazole compound represented by a formula I, and a preparation method, a pharmaceutical composition and applications thereof, wherein the compound has characteristics of good stability, excellent solubility, low cytotoxicity and remarkable neuroprotective effect, can effectively prevent and treat nerve cell injury, and is an ideal medicinal compound for preventing or treating cerebral stroke, cerebral embolism, cerebral stroke sequelae, cerebral stroke dyskinesia, mitochondrial encephalomyopathy and amyotrophic lateral sclerosis of spinal cord.

The invention provides application of a compound SB216763 to preparing cerebrovascular disease preventing and/or treating drugs and a pharmaceutical composition of the compound SB216763. The compoundSB216763 is 3-(2, 4-dichlorophenyl)-4-(1-methyl-1H-indole-3-yl)-1H-pyrrole-2, 5-diketone with a structural formula shown in the description. Experiments discover that the compound SB216763 can achievesignificant cerebral nerve protecting effects, significantly reduce the volume of acute cerebral infarction of rats with focal cerebral ischemia and improve the nerve symptoms of the rats. The drugsprepared with the compound SB216763 can be applied to preventing or treating diseases such as ischemic brain injury, cerebral thrombosis, cerebral embolism, cerebral infarction, cerebral apoplexy, lacunar infarction, transient cerebral ischemia, cerebral arteriosclerosis and diabetic cerebrovascular complications.

The invention provides a pharmaceutical composition for reducing progressive stroke and brain injury by applying rosmarinic acid and belongs to the field of pharmacy. The pharmaceutical composition isprepared from the rosmarinic acid and salidroside, wherein the mass ratio of the rosmarinic acid to the salidroside is 1 to 1. The rosmarinic acid and salidroside combined medicine provided by the invention has more remarkable function characteristics of neuroprotection, inflammatory response inhibition and the like for tMCAO rats than those of single administration and accords with an international new orientation of screening new drugs at current. The rosmarinic acid and salidroside combined medicine provided by the application is used as a novel possible neuroprotective agent and a potential neuroprotective mechanism and provides a new experimental evidence for clinical treatment and application.

The invention relates to application of a ferulic acid derivative in preparation of a medicine for convalescent care of ischemic stroke. The ferulic acid derivative is characterized in that the ferulic acid derivative is selected from 4-hydroxymethylphenol ferulic acid ester, 4-hydroxybenzylalcohol ferulic acid ester and 4-formylphenol ferulic acid ester.