73 results about "Boldine" patented technology

A method administers quaternary ammonium anti-cholinergic muscarinic receptor antagonists in combination with acetyl-cholinesterase inhibitors to treat either cognitive impairment or acute delirium. This therapy results in a modification of a cognitive disorder or disease, namely a slow down in the disease progression. In one preferred embodiment, the disease is dementia with Lewy Bodies. New formulations for quaternary ammonium anti-cholinergic muscarinic receptor antagonists are also disclosed.

A composition and a method for using the composition to delay the onset of the symptoms of Alzheimer's disease in humans, comprising curcumin, piperine, oleic acid, oleanolic acid, ursolic acid, galantamine, and huperzine A, among other compounds. Curcumin is an antioxidant, while galantamine and huperzine A inhibit the activity of acetylcholinesterase in the brain. Piperine and oleic acid increase the bioavailability and gastrointestinal absorption of curcumin, galantamine, huperzine A, and other nutrients.

A method administers quaternary ammonium anti-cholinergic muscarinic receptor antagonists in combination with acetyl-cholinesterase inhibitors to treat either cognitive impairment or acute delirium. This therapy results in a modification of a cognitive disorder or disease, namely a slow down in the disease progression. In one preferred embodiment, the disease is dementia with Lewy Bodies. New formulations for quaternary ammonium anti-cholinergic muscarinic receptor antagonists are also disclosed.

The invention relates to a lotus leaf extract, a monomer component and application thereof. An active monomer component of the extract is aporphine alkaloid and comprises 2-hydroxy-1-methoxy-aporphine, nuciferine and N-nornuciferine. The lotus leaf extract and the monomer component have good inhibition to acetylcholinesterase, and can be developed into medicaments for treating the diseases such as Alzheimer's disease, glaucoma, asthenic bulbar paralysis, intestinal obstruction and the like.

The present invention relates to an application of acetylcholinesterase inhibitor for curing diabetes. The described inhibitor includes all the compounds which can inhibit acetylcholinesterase activity and have the action for curing diabetes. The invented experimental results show that these inhibitors have the actions of inhibiting beta-cell death and reducing blood sugar concentration of diabetic model mouse, and can effectively cure or improve diabetes symptom.

Described herein are systems and methods for applying extremely low duty-cycle stimulation sufficient to treat chronic inflammation with progressively longer delays (off periods) from an initial stimulation. In particular, described herein are supra-threshold pulses of electrical stimulation sufficient to result in a long-lasting (e.g., >48 hours) inhibition of pro-inflammatory cytokines and / or effects of chronic inflammation; the delay between initial doses (which may be single-pulse doses) may be extended for subsequent doses, potentially dramatically enhancing battery and device longevity.

The present invention refers to biochemistry, namely to new peptide compounds having the ability to selectively block the muscle-type nicotinic acetylcholine receptor. The claimed compounds have common formula (I): X1-X2-X3-Pro-X4-Pro-X5 (SEQ ID NO: 54), where X1 is chosen within H, Ac—, Palm-; X2 is chosen within Trp, Tyr; X3 is chosen within Trp, Tyr; X4 is chosen within Lys, Orn, Dbu, Dpr, Arg; X5 is chosen within —OH, —NH2, —OCH3, —OC2H5, —NH—C6H5. The invention can be applied in cosmetics for smoothing mimic and age-related wrinkles

The invention discloses new application of fucoxanthin to preparation of medicine for treating the alzheimer disease. The application is characterized in that fucoxanthin is used in the aspect of preparation of the medicine for treating the alzheimer disease, particularly in the aspect of preparation of medicine inhibiting acetylcholin esterase and the aspect of preparation of medicine inhibiting Abeta fibrosis. The application has the advantage that fucoxanthin has the inhibition function on acetylcholin esterase and Abeta fibrosis.

This invention discloses that a combination of two drugs, from two different and previously unrelated categories, provides effective and long-lasting relief from neuropathic pain. Both drugs can be taken orally, in a convenient, painless, non-invasive manner that does not require injections. One drug in this combination is an alpha2 adrenergic agonist, exemplified by clonidine. The other drug in the pain-relieving combination has a tri-cyclo-alkyl-amine (TCAA) structure. At least some TCAA drugs have antagonist (receptor-blocking) activity at two entirely different classes of neuronal receptors: the muscarinic subclass of acetylcholine (ACh) receptors, and the NMDA subclass of glutamate receptors. Such drugs include ethopropazine, normally used as an anti-cholinergic drug, and desipramine, normally used as an anti-depressant. Tests by the Applicants have shown that at least some TCAA drugs can relieve neuropathic pain to a limited extent, but at the doses required to relieve pain, they cause adverse side effects, and any pain relief is relatively brief and short-lived. However, when a TCAA drug such as ethopropazine is administered together with an alpha2 adrenergic agonist such as clonidine, these drugs mutually potentiate one another's neuropathic pain-relieving action, and provide potent and sustained neuropathic pain relief, even when each agent is administered at a low dosage that is below its threshold for causing adverse side effects. Accordingly, this drug combination can provide safe and effective relief of neuropathic pain and possibly other types of chronic and / or intractable pain, at dosages which are so low that they do not pose serious risks of adverse side effects.

The invention provides novel medical application of butylphthalide, i.e. the application of the butylphthalide in the preparation of a medicament for treating the bronchial asthma. The experimental research on the spasmolysis of the butylphthalide on the isolated tracheal smooth muscle of a guinea pig and the influence of the butylphthalide on the incubation period of asthma of the guinea pig shows that the butylphthalide in the concentration range of 3.68*10-6 to 3.68*10-4g / mL has obvious spasmolysis on the tracheal smooth muscle of the guinea pig in the isolated spasticity caused by 5*10-6g / mL of acetylcholine or histamine. On the basis of continuously applying the butylphthalide to the guinea pig which is sensitive for the acetylcholine and the histamine for 10 days, a mixture of the acetylcholine and the histamine is atomized and sucked and the incubation period of asthma is observed. A result shows that 30 mg / kg and 90 mg / kg of butylphthalide has an effect of relieving the tracheospasm of the guinea pig, which is caused by the acetylcholine and the histamine. Therefore, the butylphthalide has a treatment effect on the asthma guinea pig and the treatment effect of the butylphthalide on the asthma guinea pig is related to the effect of inhibiting Ca2+ inner flow and expanded tracheal smooth muscle of the butylphthalide.

The invention relates to isoquinoline-type alkaloid for preventing and treating cervical cancer, belonging to the fields of preparation technique of natural medicament extractives and antitumor medicines. The invention also relates to applications of bulbocapnine, isocorydine, isoboldine, N-methyl hernovine, dicranostigma alkaloid or pharmaceutically acceptable salts or esters thereof in the preparation of medicaments for preventing and treating cervical cancer.

The invention discloses a novel inhalant containing glucocorticoid and bronchodilator, that is, inhalable particles containing glucocorticoid and other medicine, wherein, the other medicine is selected from one of the following medicines: beta 2 receptor stimulant, anticholinergic agent, theophylline agent, leukotriene receptor antagonist, mast cell stabilizer and antihistamine.

The invention provides for methods for treating gastric cancer or colon cancer in a subject by administering a cholinergic antagonist, a Botulinum toxin, a NGF inhibitior, a TRK inhibitor, or performing a surgical denervation. The invention provides for inhibiting stem cells growth by administering a cholinergic antagonist, a Botulinum toxin, a NGF inhibitior, a TRK inhibitor, or performing a surgical denervation. The invention provides for stimulating regeneration of the colon or stomach by administering a cholinergic agonist.

Determination of anticholinergic M3 receptor and antibody is used to diagnose sicca syndrome. It has excellent sensitivity and specificity.

The invention discloses a chrysanthemum florescence regulator containing choline chloride and glycine betaine. The chrysanthemum florescence regulator containing the choline chloride and the glycine betaine firstly takes the choline chloride and the glycine betaine as regulators of chrysanthemum florescence, is matched with a plant growth regulator, a phosphatic fertilizer and a potash fertilizer in use, can regulate the physiological activity of chrysanthemum, enhance photosynthetic efficiency and improve antioxidant ability through carrying out spraying treatment on chrysanthemum plants in a full-blossom period, is conducive to growth of stems, leaves and flowers of the plants, makes the chrysanthemum plants grow exuberantly, increases flower diameters, prolongs the florescence and makes up for the defects of light and temperature control technology and planting by stages. As the requirement for facilities is low, the chrysanthemum florescence regulator can greatly reduce manpower, material resources and financial resources, and has remarkable effects and unique advantages in the chrysanthemum florescence regulation aspect.

The present invention relates to an alpha7 nicotinic acetylcholine receptor ligand and a preparation method thereof. The ligand includes an agonist and an imaging agent, the agonist is a 1,4-diazabicyclo [3.2.2] nonane-benzo heterocyclic derivative, and the imaging agent is 125I and 18F-trifluoromethyl marker. The derivatives both have good brain uptake, the absorption values in different regions of the brain are basally consistent with the distribution of alpha7nAChR receptors, the uptake of the derives is highest in hippocampus, thalamus, cortex and other regions where the alpha7nAChR receptors targetedly distribute, and the derives can be blocked by known alpha7nAChR ligands but can not be blocked by alpha4beta2 medicine. Therefore, the 1,4-diazabicyclo [3.2.2] nonane-benzo heterocyclic derivative and the 125I and 18F-trifluoromethyl marker are potential agonist and imaging agent for alpha7 nicotinic acetylcholine receptors.

The invention provides icariin derivatives disclosed as Formula I. The icariin derivatives provided by the invention have in-vitro acetylcholine ester inhibiting activity, and have better drug effects than icariin, thereby providing a new option for clinical medicines for treating senile dementia.

The invention discloses application of berberine or other pharmaceutically acceptable salts in preparing a M3 receptor selective inhibitor medicine. The medicine is used for treating acute pancreatitis, lung cancers and colon cancers, self-immunity sialadenitis, asthma, respiratory tract inflammation, lung diseases and cardiovascular diseases, relieving panic, or treating excessive activity of bladders, and is used for inhibiting the enhancing of Ca<2+> signals in pancreatic acinar cells caused by M3 receptor-mediated acetyl choline and L-arginine.

The invention discloses an application of pentapeptide KLPGF in inhibiting AChE activity. The amino acid sequence of AChE inhibiting peptide is Lys-Leu-Ro-Gly-Phe (KLPGF). The KLPGF activity peptide can effectively inhibit the AChE activity, improve the level of brain neurotransmitter acetyl choline and play the effect of preventing senile dementia. The AChE inhibiting peptide is simple in structure, safe and free from toxicity; the AChE inhibiting property is strong and can be used for developing healthcare food or drug for assisting to release or treat the senile dementia.

The invention discloses a saturated heterocyclic nitrogen containing caffeic acid derivative separated from nightshades, or pharmacological acceptable salt of the caffeic acid derivative. The compound is a hydroxycholine M receptor antagonist and can be used for treating diseases of spasm, stenocardia, cholecystalgia, renal colic, visceral spasm and the like. An unmarked cell-targeting pharmacological technique is adopted, research on dose-effect relationship displays DMR response signals caused by antagonistic acetylcholine with compound dose dependency and shows that the compound has high hydroxycholine M receptor antagonistic activity. Compared with known M receptor antagonist atropine, scopolamine and the like, the compound is large in structural difference, and selectivity on muscle glands and the nervous system can be expectedly improved; current research shows that a hydroxycholine M receptor is related to diseases of spasm, analgesia, calm, schizophrenia and the like, and an efficient new ligand definite in action target can be provided for the related diseases.

The invention relates to the field of medicinal chemistry, in particular to a class of donepezil-BHT heterozygotes. The donepezil-BHT heterozygotes serving as multifunctional acetylcholinesterase (AChE) inhibitors and monoamine oxidase B (MAO-B) inhibitors have a great in-vitro antioxidation effect and have a great neuroprotective effect on hydrogen peroxide (H2O2)-induced oxidative damage of PC12nerve cells and bacterial lipopolysaccharide (LPS) stimulated BV-2 inflammatory injuries, it is proved by animal experiments that the donepezil-BHT heterozygotes have a great effect on improvement ofthe cognitive function, and it is considered that the donepezil-BHT heterozygotes can be used as drug candidates for treatment of Alzheimer's disease. A most preferred compound structure is shown inthe description.

The invention relates to a composition for improving cerebral neurotrophic function. The composition comprises, by weight, 91.1-99.8% of asparagus extract, 0-2.4% of phosphatidylserine, 0-2.4% of fungal extract, 0.09-1.6% of theanine and 0.09-2.0% of gamma-aminobutyric acid. The asparagus extract is solid powder or liquid, and refers to the extract, with asparagus saponin content not less than 0.3g / 100g, extracted from one or multiple of asparagus stems, leaves or leftovers; the fungal extract refers to the extract from one or multiple of shiitake mushroom, glossy ganoderma, hericium erinaceus, pleurotus cornucopiae and pleurotus eryngii; extraction solvents of the asparagus extract and the fungal extract both refer to water or mixture of ethyl alcohol and water. The composition can promote growth of the brain derived neurotrphic factor by increasing content of hippocampus acetyl choline, improve mechanisms such as neurotrophic growth factor gene expression, and play a role in improving the cerebral neurotrophic function.

The invention discloses dimers Vc1.1-dimer, RgIA-dimer and PeIA-dimer. The dimer alpha-conotoxin Vc1.1, RgIA and PeIA are polypeptide compounds. The Vc1.1-dimer, RgIA-dimer and PeIA-dimer are synthesized by designing a linker containing two alkynyl functional groups, modifying wild polypeptide and introducing a nitrine functional group to carrying out a click reaction further. The dimers have thebeneficial effects that the activity and selectivity of alpha-conotoxin to alpha9aphla10 acetyl choline acceptors are improved by way of the dimers, so that a novel polypeptide drug for treating painand tumors is developed conveniently.

A 7-amino-1,4-dihydroisoquinoline-3(2H)-one derivative, a synthetic method and an application thereof. The invention belongs to the technical field of medicines and relates to the 7-amino-1,4-dihydroisoquinoline-3(2H)-one compound, the synthetic method, and the application thereof in medicine The compound is represented as the general formula (I), wherein X is (CH2)<n-1>CO, n = 1-10; or is NH(CH2)<n-2>CO, n = 2-10; or is NHCO(CH2)<n-3>CO, n = 3-10; Y is CO(CH2)<n-1>, n = 1-10; or is CO(CH2)<n-2>NH, n = 2-10; or is CO(CH2)<n-3>CONH, n = 3-10, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 refers to different substituent groups. The invention also discloses the structures and synthetic methods of these compounds and in-vitro acetylcholin esterase inhibition activity of the compounds. The compounds can be further developed into a novel drug for treating Alzheimer's disease.