28 results about "L-Hyoscyamine" patented technology

The invention discloses an application of an overexpressed bellseed AlbHLH175 gene in increasing tropine alkaloid and precursor content thereof, by creating an AlbHLH175 overexpressed transgenic hairy root strain and analyzing expression quantities of AlbHLH175 and TAs biosynthetic genes in the transgenic strain, results show that the AlbHLH175 can positively regulate expression of seven biosynthetic genes, namely AlODC, AlPMT, AlMPO, AlPYKS, AlCYP82M3, AlPPAR and AlHDH, and the expression quantity of the AlbHLH175 and TAs biosynthetic genes in the transgenic strain is analyzed. Therefore, accumulation of putrescine, N-methyl putrescine, tropinone, tropine, conpin, scopolamine, anisodamine and scopolamine is promoted, and an excellent gene resource is provided for creating a stable and high-yield TAs new germplasm of the bellflower through biological breeding and molecular design.

The invention relates to a biochemical method for preparing scopolamine, and belongs to the technical field of bioengineering. The invention aims to realize efficient conversion from scopolamine to scopolamine and improve the yield and industrial applicability of a target product. The invention provides a biochemical method for preparing scopolamine. The biochemical method comprises the following steps: adding scopolamine 6 beta hydroxylase into a culture medium containing L-scopolamine; the amino acid sequence of the hyoscyamine 6 beta hydroxylase is shown as any one of SEQ ID NO.1-5. The invention further discloses a preparation method of the hyoscyamine 6 beta hydroxylase. And the biochemical engineering method for realizing efficient and high-selectivity synthesis of scopolamine is realized.

The invention provides a hyoscyamine 6 beta hydroxylase mutant as well as a preparation method and application thereof. The hyoscyamine 6 beta hydroxylase mutant at least has the following two sites or amino acid mutation in functional equivalent sites compared with wild hyoscyamine 6 beta hydroxylase: the 14th site and the 97th site; the wild type hyoscyamine 6 beta hydroxylase has an amino acid sequence as shown in SEQ ID NO: 1. The obtained hyoscyamine 6 beta hydroxylase mutant has higher hydroxylation activity, and meanwhile, the epoxidation capacity disappears or is reduced. In industrial application, the catalytic efficiency can be remarkably improved, reagent waste is reduced, the production cost is saved, generation of redundant by-products in chemical reaction is reduced, and environmental pollution is reduced.

This invention belongs to the field of pharmaceutical technology, specifically relating to the application of a traditional Chinese medicine composition in the preparation of drugs for improving cognitive impairment. By weight, the traditional Chinese medicine composition comprises: 225-300 parts rhubarb, 50-75 parts pig bile powder, 90-120 parts aster, 360-480 parts scrophularia, 180-240 parts immature bitter orange peel, and 180-240 parts areca nut. This invention is the first to demonstrate that a composition of six traditional Chinese medicines, including scrophularia, rhubarb, and areca nut, significantly improves memory acquisition (induced by scopolamine), consolidation (induced by sodium nitrite), and retrieval impairments, covering the entire process of memory formation, encoding, storage, and retrieval, thus overcoming the limitations of existing drugs that only target a single memory stage.

The invention provides a construction method of a mouse dry eye model, and belongs to the technical field of animal model construction. The construction method comprises the following steps: dripping a benzalkonium chloride solution into the ocular surface of a mouse, injecting a scopolamine solution into the mouse in a subcutaneous manner, placing the mouse in a dry environment, and modeling to obtain the mouse dry eye model. The formation of the mouse dry eye model is induced through a dry environment and a compound condition of benzalkonium chloride and scopolamine. According to the mouse dry eye model, the tear secretion amount is remarkably reduced, ocular surface inflammation occurs, and the dry eye syndrome can be well simulated. The model can be used for screening medicines for treating the xerophthalmia and carrying out other researches on the xerophthalmia, and has a good application prospect.

The invention discloses a quality detection method of scopolamine butylbromide, and relates to the technical field of medicine detection.The method comprises the steps that a sample to be detected is prepared into a test solution, and solubility and the pH value are detected; respectively carrying out specific identification on the sample by adopting a spectrum method and a chemical method; separating and detecting impurities in the sample by adopting a high performance liquid chromatography; determining the content of scopolamine butylbromide in the sample by adopting a potentiometric titration method; carrying out sterility test on the test solution by adopting a membrane filtration method; and comparing the obtained detection data with a preset quality standard, and comprehensively evaluating the quality data. According to the method disclosed by the invention, the content of the scopolamine butylbromide in the raw material medicine is subjected to quality detection according to a plurality of detection standards from physical properties, chemical identification, impurity spectrum, main component content to preparation safety, so that the quality of the scopolamine butylbromide can be more comprehensively evaluated, and the detection accuracy is improved.

This invention relates to a small molecule compound composition and its applications, belonging to the field of biotechnology. The small molecule compound composition of this invention includes NU7441, GW9662, and D609, or their stereoisomers. This invention is the first to discover that this small molecule compound combination can effectively inhibit oxidative damage to corneal epithelial cells caused by hyperosmolarity and significantly improve the survival rate of corneal epithelial cells. In vivo animal experiments show that, compared with the control group, the experimental group of mice injected with scopolamine-induced dry eye model mice, given eye drops containing the small molecule compound combination, showed significantly reduced corneal defects and increased tear secretion. The small molecule compound combination can effectively prevent corneal epithelial damage, has high efficacy, and no obvious drug toxicity. This small molecule compound combination may become a potent and effective drug for the clinical treatment of dry eye in the future.

The present invention relates to a composition for the prevention, improvement, or treatment of memory impairment or cognitive impairment comprising a black pepper (Piper nigrum) extract, and more specifically, to a composition for the prevention, improvement, or treatment of memory impairment or cognitive impairment induced by scopolamine comprising a black pepper 70% (v / v) ethanol extract as an active ingredient. It was confirmed that the black pepper extract of the present invention, particularly the black pepper ethanol extract, contains a high content of piperine and effectively inhibits the inflammatory response induced in LPS-stimulated microglia without cytotoxicity compared to Indian pepper (Piper longum) or black pepper methanol extract. Furthermore, the black pepper extract of the present invention showed memory-enhancing effects in the Y-maze test and passive avoidance test using mice with memory impairment induced by scopolamine, and since the BDNF-CREB pathway activation effect was confirmed, it can be usefully utilized as a composition for the prevention, improvement, or treatment of memory impairment or cognitive impairment induced by scopolamine.

The invention relates to a traditional Chinese medicine composition for improving hypomenorrhea and application thereof, and belongs to the technical field of biological medicine. The herba leonuri, the anisodamine and the Dingkundan are combined to form the composition, efficacy complementation can be achieved, it is guaranteed that the medicine takes effect quickly, the long-acting treatment effect is maintained, meanwhile, the side effect caused by long-term single medication is avoided, the treatment safety and tolerance are improved, the menstrual volume can be remarkably increased, endometrial blood circulation can be improved, and the curative effect is improved. The hypomenorrhea is effectively improved. The medicines in the composition are all approved compliant medicines, the source is clear, the quality is controllable, the administration scheme is simple and easy to implement, the composition is suitable for clinical popularization and application, and a novel safe, efficient and reproducible treatment method is provided for hypomenorrhea.

The invention provides a construction method of a rat xerophthalmia model, which utilizes scopolamine hydrobromide and 1% atropine sulfate ophthalmic gel to jointly induce xerophthalmia so as to induce comprehensive symptoms of rat xerophthalmia. After scopolamine hydrobromide is subcutaneously injected into a rat and atropine ophthalmic gel is dropwise added to eyes of the rat, difference appears in tear secretion, tear film rupture time and cornea staining detection from the second week, the symptom stability can last for more than one month, and obvious difference also exists in pathological examination of an anatomical end point and a TUNEL test. Hypodermic injection of scopolamine hydrobromide can inhibit parsympathetic nerve excitation so as to inhibit gland secretion, so that lacrimal secretion is insufficient; and meanwhile, the atropine ophthalmic gel can inhibit parasympathetic nerves, so that the threshold value of tear secretion is increased, and the tear secretion is reduced. The xerophthalmia model has the advantages that the modeling time is short, the modeling process is not limited by environment temperature and humidity, and model animals after modeling have small individual differences and high symptom specificity.

The invention discloses a hyoscyamine derivative and a preparation method thereof, relates to the field of drug synthesis, and aims to provide an effective and safe drug molecule for inhalation / local pulmonary administration. According to the invention, a linear polyethylene glycol chain containing seven ethylene glycol repeating units is introduced into a hydroxyl site of hyoscyamine, and quaternization is carried out on a nitrogen atom of the hyoscyamine, so that the hyoscyamine derivative is prepared. The derivative is specially designed for inhalation / local lung drug delivery, through structural modification, systemic absorption and central penetration of the compound are reduced, local exposure of the lung is improved, residence time in the lung is prolonged, and meanwhile good atomization performance is taken into account.

This invention relates to the technical field of wound care spray formulations, providing a wound repair spray based on herbal extracts and its preparation method. The invention first uses an alkaline alcohol / aqueous solution of *Broomia spp.* leaf extract, neohesperidin, and scopolamine hydrobromide as the extraction system, employing heated ultrasonic extraction. After extraction, dilute HBr is added dropwise to adjust to a weakly acidic state, yielding an extract of *Broomia spp.* leaf extract, neohesperidin extract, and scopolamine hydrobromide extract. This extract is then compounded with extracts of *Bletilla striata*, *Ampelopsis japonica*, *Sanguisorba officinalis*, *Phellodendron chinense*, *Scutellaria baicalensis*, *Polygonum cuspidatum*, and *Platycladus orientalis* leaf extracts to obtain the wound repair spray. During the extraction process, the extract system is stable, homogeneous, clear, and transparent, without precipitation or stratification. The resulting wound repair spray is gentle on the skin and has minimal irritation to wounds. Through the synergistic effect of *Broomia spp.* leaf extract, neohesperidin, and scopolamine hydrobromide, a multi-layered closed loop of antioxidant, anti-inflammatory, blood-activating, and repairing effects is formed. Combined with the addition of natural herbal medicines, it can achieve rapid and efficient wound repair.

The application discloses a kind of drug composition for treating pseudomyopia and preparation method thereof, belong to the field of medicine.The application provides the method that scopolamine is combined with tometilcaine in the preparation of the drug for treating pseudomyopia.A kind of drug composition for treating pseudomyopia is also provided.The scopolamine tometilcaine compound eye drops of the application, active ingredients are extracted from plants and crystallized into salt, prepared into compound eye drops, curative effect is remarkable, side effect is low, process is simple, cost is low, medication, carrying, storage is convenient.

The invention discloses hyoscyamine 6 beta hydroxylase and application thereof, and belongs to the technical field of bioengineering. The invention aims to provide the hyoscyamine 6 beta hydroxylase with high activity. The invention provides hyoscyamine 6 beta hydroxylase. The amino acid sequence of the hyoscyamine 6 beta hydroxylase is as shown in SEQ ID NO. 4. The novel H6H enzyme with higher bifunctional catalytic efficiency is explored, and the key technical requirements of improving the biological manufacturing capacity of scopolamine are met.

The invention relates to the technical field of medicines, in particular to application of anisodamine hydrobromide. The invention provides new application of anisodamine hydrobromide, and researches show that anisodamine hydrobromide can improve rat vital sign changes caused by CLP, improve lung tissue morphology and regulate related target proteins, so that the anisodamine hydrobromide has a good treatment effect on sepsis and / or septic shock.

The present invention relates to novel compounds of formula (I) and pharmaceutically acceptable salts thereof, which are capable of modulating the GLP-1 receptor; the invention also relates to salts, solvates, stereoisomers or tautomers thereof, pharmaceutical compositions, processes for their preparation and therapeutic uses.

The utility model discloses extraction equipment for a gastric spasmolysis drug anisodamine hydrobromide. The extraction equipment comprises a bottom frame, an extraction tank fixedly mounted on one side of the top of the bottom frame, a pressurizing and shunting tank fixedly mounted on one side of the extraction tank, and an electric cabinet fixedly mounted on the top of the bottom frame and positioned between the extraction tank and the pressurizing and shunting tank. And a conveying pump and a material guide pump are fixedly mounted at the bottom of the electric control box on the bottom frame. A material pumping pipe and a material discharging pipe are mounted at the two ends of the material guiding pump respectively, and one end of the material discharging pipe is in butt joint with the extraction tank. The two ends of the delivery pump are in butt joint with the extraction tank and the pressurizing flow dividing tank respectively. Discharging pipes with different heights are installed on the two sides of the pressurizing flow dividing tank in a penetrating mode. According to the utility model, the density of the residual liquid in the pressurized shunting tank is changed according to the adjustment of the pressure intensity. And the sewage passes through the biological filter membrane and is discharged from the cleaning holes. It is guaranteed that no liquid remains in the pressurizing flow dividing tank, and extraction of the next group of medicine is not affected.

The application discloses a kind of extraction methods of scopolamine and hyoscyamine in Qiangqi Tannicar Capsules and content determination method.The extraction method comprises the following steps: Qiangqi Tannicar Capsules and the filtrate obtained by mixing first solvent are mixed, dried, and the residue is obtained;The first solvent is an alcohol solution containing acid;The filtrate obtained by mixing the residue with the second solvent is placed in an activated solid-phase extraction column, and is eluted by washing and eluting;The eluent of the solid-phase extraction column is a mixture of acetonitrile and concentrated ammonia water;The volume ratio of acetonitrile and concentrated ammonia water is 75-98:2-25.The application uses solid-phase extraction technology to avoid using chloroform, reduces the risk in the content determination process, and solid-phase extraction only needs 20 minutes.The total extraction time can be 35-65 minutes.The application realizes the enrichment and separation of scopolamine and hyoscyamine, provides a reference for the establishment of quality standards for Qiangqi Tannicar Capsules, and has important significance for the quality control of the variety.

The invention discloses a phenyllactic acid UDP-glycosyl transferase mutant and application thereof, and belongs to the technical field of biological medicine, the phenyllactic acid UDP-glycosyl transferase mutant PLA-UGT-M5 with improved catalytic efficiency is obtained through a directed evolution method, the mutant simultaneously contains five amino acid substitutions F19S, G21E, N128S, I209L and I292V, metabolites are detected in yeast cells, and the activity of the metabolites is improved. The catalytic efficiency is obviously higher than that of a wild type. Further functional verification shows that the PLA-UGT-M5 can remarkably promote biosynthesis of the scopolamine and the scopolamine in a yeast cell factory and a belladonna hairy root system, has a good metabolic engineering application prospect, provides a key tool for efficient biosynthesis of the scopolamine and the scopolamine, and has important industrial application potential.

This invention discloses a hyoscyamine derivative and its preparation method, relating to the field of drug synthesis, and aims to provide an effective and safe drug molecule for inhalation / local pulmonary administration. The invention prepares the hyoscyamine derivative by introducing a linear polyethylene glycol chain containing seven ethylene glycol repeating units at the hydroxyl position of hyoscyamine and quaternizing its nitrogen atom. This derivative is specifically designed for inhalation / local pulmonary administration. Through the above structural modification, it achieves reduced systemic absorption and central penetration of the compound, increased local lung exposure, and prolonged pulmonary retention time, while also maintaining good nebulization performance.

The invention discloses a closed-loop transcranial stimulation system and a closed-loop transcranial stimulation method. 0.3 mg of scopolamine and 3 mg of midazolam are intramuscularly injected before an operation; after a patient enters a room, sufentanil is subjected to intravenous injection induced by right subclavian vein and radial artery puncture general anesthesia, propofol is subjected to target-control infusion, the plasma target concentration is 3.0 mu g / mL, vecuronium bromide is 0.15 mg / kg, tracheal intubation is performed after 5 min, general anesthesia maintains target-control infusion of propofol, and after the patient enters the room, the target-control infusion of propofol is performed. A TMS stimulation coil electricity-magnetism-heat-stress model, a single-phase and double-phase pulse discharge circuit model and a neuron dynamic response model under the action of a TMS are established, and the influence of TMS system parameters on space-time distribution characteristics of an intracranial induced electric field and neuron membrane potential can be accurately expressed. Behavior perception and system auditory stimulation are combined to be applied to nursing intervention of severe craniocerebral injury coma patients, self-repairing and consciousness awakening of the brain functions of the patients can be effectively promoted, and meanwhile recovery of limb functions and daily life ability of the patients is facilitated.

The invention discloses a method for researching a mild cognitive impairment action mechanism of a cornu cervi pantotrichum polypeptide based on a Wnt / beta-catenin signal channel, relates to the technical field of mechanism analysis, and solves the problem of difficulty in realizing spanning from basic research to clinical transformation in the prior art. Randomly dividing the rats into five groups of blank control, model, positive control and VAP high / low dose, continuously performing intragastric administration on each group for 18 days, and feeding distilled water into the blank and model groups; 2 mg / kg scopolamine is injected into abdominal cavities of the model group after 18 days and 2 hours, and normal saline is injected into the blank group; the scopolamine model is used for measuring the 2min static / motion time of the rat by using an open field experiment, and the unilateral common carotid artery ligation model is used for measuring the escape latency / platform penetration times by using a water maze; the method comprises the following steps: taking blood, separating a hippocampal region, and carrying out HE dyeing, ELISA and Western blot; sPSS 21.0 analysis and single factor variance analysis are used for evaluating the difference and Plt; 0.05 or Plt; 0.01 has statistical significance.

The invention discloses hyoscyamine 4 beta-hydroxylase and application thereof, a dioxygenase coding gene hyoscyamine 4 beta-hydroxylase (H4H) capable of hydroxylating hyoscyamine is found through genomics mining analysis, the catalytic activity of the hyoscyamine 4 beta-hydroxylase is confirmed through enzyme activity analysis of prokaryotic recombinant protein, products are prepared through escherichia coli fermentation and separation, and the hyoscyamine 4 beta-hydroxylase is obtained through fermentation and separation of the prokaryotic recombinant protein. The product is confirmed to be 4 beta-hydroxyscopolamine through analysis and calculation of a secondary mass spectrum, a two-dimensional nuclear magnetic spectrum and electron circular dichroism, and a theoretical basis is laid for development and utilization of subsequent novel drug molecules.

The present application relates to a kind of extraction and purification method of alkaloids in Datura stramonium, which comprises hydrochloric acid solution soaking, filter residue and filtrate are obtained by filtering, ammonia water test solution is used to adjust pH value, shake extraction, remove solvent, obtain Datura stramonium alkaloid extract, set chromatographic column elution procedure, elution is carried out, and the purity of alkaloids in Datura stramonium is obtained by collecting fraction detection calculation.The extraction step of the present application is simple, ethanol impregnation is reduced, can avoid that tannin, pigment and other components in Datura stramonium enter alkaloid extract in large quantities, can reduce the difficulty of subsequent purification, improve the life of purification medium, and save cost;And the reverse phase chromatography used in the purification part of the present application reduces the use of organic phase, is environmentally friendly, saves cost;While reverse phase chromatography has better separation effect, and the purity of prepared hyoscyamine and scopolamine is higher.

This invention provides a scopolamine-soluble press-fit acupoint patch, its preparation method, and its application. The patch includes: a fixing sheet; an adhesive sheet adhered to one side of the fixing sheet for attaching to human skin, the adhesive sheet having perforations; and a needle body comprising a fixedly connected base and a needle shaft, the base being bonded between the adhesive sheet and the fixing sheet, the needle shaft extending outward through the perforations to penetrate the stratum corneum of the skin to deliver the drug and simultaneously stimulate acupoints. At least one needle shaft is loaded with scopolamine. The fixing sheet connects to the adhesive sheet, thereby fixing the base. Compared to traditional soluble microneedle arrays, the soluble press-fit needles in this acupoint patch significantly extend the needle length, enhancing the acupoint stimulation efficacy, while achieving controlled drug release through a soluble matrix. Experiments show that this acupoint patch exhibits good behavioral improvement effects in treating a motion sickness model.

The application discloses a phenyllactic acid UDP-glycosyltransferase mutant and application thereof, and belongs to the technical field of biological medicine. A phenyllactic acid UDP-glycosyltransferase mutant PLA-UGT-M5 with improved catalytic efficiency is obtained through a directed evolution method. The mutant simultaneously contains five amino acid substitutions F19S, G21E, N128S, I209L and I292V. Metabolic products are detected in yeast cells, and the mutant shows a catalytic efficiency significantly higher than that of a wild type. Further functional verification shows that the PLA-UGT-M5 can significantly promote the biosynthesis of scopolamine and hyoscyamine in a yeast cell factory and a belladonna hairy root system, has a good metabolic engineering application prospect, provides a key tool for the efficient biosynthesis of scopolamine and hyoscyamine, and has important industrial application potential.

The invention discloses a pharmaceutical composition for treating pseudomyopia and a preparation method thereof, and belongs to the field of medicines. The invention provides a method for jointly using scopolamine and tropicamide in preparation of a medicine for treating pseudomyopia. The invention also provides a pharmaceutical composition for treating pseudomyopia. According to the scopolamine and tropicamide compound eye drops, active ingredients are extracted from plants and then crystallized into salt, the compound eye drops are prepared, the curative effect is remarkable, the side effect is low, the process is simple, the cost is low, and medication, carrying and storage are convenient.

The present disclosure relates to pharmaceutical compositions comprising hyoscyamine or a pharmaceutically acceptable salt thereof dissolved or suspended in a vehicle comprising a semi-fluorinated alkane.