2018 results about "Side effect" patented technology

The invention discloses a xanthine oxidase inhibitory peptide with a kidney improving function and application thereof, and belongs to the technical field of biological medicines.The xanthine oxidase inhibitory peptide is screened out by conducting enzymolysis, separation and purification on litopenaeus vannamei processing by-products and utilizing a molecular docking technology, the amino acid sequence of the xanthine oxidase inhibitory peptide is Pro-Leu-Gly-Pro-Pro-Pro, and the amino acid sequence of the xanthine oxidase inhibitory peptide is Pro-Leu-Gly-Pro-Pro-Pro. And the half inhibition concentration of the polypeptide is 2.356 + / -0.2448 mM. The xanthine oxidase inhibitory peptide is proved to have an improvement effect on hyperuricemia mice, the improvement effect is mainly characterized by reducing the content of serum uric acid, creatinine and urea nitrogen of the hyperuricemia mice, inhibiting the activity of xanthine oxidase (XOD) in serum and livers of the mice, inhibiting synthesis of uric acid and improving kidney injury of the mice, and Toxinpred prediction shows that the xanthine oxidase inhibitory peptide has the effect of inhibiting the activity of xanthine oxidase (XOD) in the serum and livers of the mice. The xanthine oxidase inhibitory peptide is free of toxic and side effects, so that the xanthine oxidase inhibitory peptide has a wide application prospect in preparation of food or drugs for improving renal functions.

The invention discloses a drug full life cycle risk monitoring and early warning method based on multi-source data fusion, and relates to the technical field of data analysis, and the method comprises the steps: constructing a time sequence heterogeneous graph, calculating the similarity between drugs and side effect pairs in the time sequence heterogeneous graph through a comparative learning algorithm, and generating a candidate signal list; constructing a data set, and identifying hybrid factors associated with drug selection and side effect risks in the data set by using a separation characterization learning algorithm to obtain an average causal effect value; a space-time risk thermodynamic diagram is drawn, risks in the whole life cycle of the medicine are graded based on risk distribution characteristics in the space-time risk thermodynamic diagram, and a corresponding early warning strategy is triggered; and converting the early warning strategy into a risk assessment report in a standard format by using a preset report template. By accurately calculating the individual and average causal effect value, the causal relationship between the drug and the side effect of the drug is quantified, and a solid foundation is laid for deep evaluation of drug safety.

The invention relates to an application of Danjie emodin in preparation of drugs for preventing or treating drug-induced liver injury. The liver injury is drug-induced liver injury induced by acetaminophen. According to the invention, the effective component Danleaf emodin in the traditional Chinese medicine rhubarb is used for preventing and treating drug-induced liver injury induced by acetamido, and the traditional Chinese medicine composition has the characteristics of safety, reliability and small toxic and side effects. Starting from the whole, multi-target intervention is performed on drug-induced liver injury induced by acetaminophen, the levels of glutamic-pyruvic transaminase, glutamic oxalacetic transaminase and malondialdehyde in plasma are remarkably reduced, the obvious anti-inflammatory and liver cell apoptosis inhibiting effects are achieved, the good clinical application prospect is achieved, and a new way is provided for prevention and treatment of liver injury.

The invention provides a dynamic medication dosage optimization method fused with reinforcement learning. The method comprises the following steps: acquiring a first physiological index parameter of a target patient; obtaining a first diagnosis report of the target patient, wherein the first diagnosis report comprises basic information of the target patient and first disease information of the target patient; the first disease information comprises a first disease type and first disease description information; determining a first reinforcement learning algorithm corresponding to the first disease type; determining a first control parameter of the first reinforcement learning algorithm according to the first physiological index parameter and the basic information; and performing operation on the first disease description information through the first reinforcement learning algorithm and the first control parameter to obtain a first medication dosage parameter. Based on the application, the drug effect can be consistent with the physical condition of a patient, and poor drug effect and excessive side effects caused by too strong drug effect are avoided.

The invention relates to an amido-substituted aromatic heterocycle inhibitor as well as a preparation method and application thereof. Specifically, the compound disclosed by the invention has a structure as shown in a formula (I), and each group is defined in the specification. The invention further discloses a preparation method of the compound and application of the compound as a KRAS mutation inhibitor. The compound has a very good inhibition effect on KRAS mutation and has better pharmacodynamic and pharmacokinetic performance and lower toxic and side effects. # imgabs0 #

The invention discloses a preparation method of artemisia apiacea extracellular vesicles, which comprises the following steps: step 1, pre-treating artemisia apiacea, carrying out primary centrifugal treatment, removing large plant tissues and cell debris, carrying out secondary centrifugal treatment, filtering by a needle filter, and collecting; step 2, transferring the filtered suspension to a sucrose density gradient solution, then carrying out third centrifugal treatment, collecting the solution with the concentration of 30% in the layer, and carrying out fourth centrifugal treatment to obtain artemisia apiacea extracellular vesicles; the invention further discloses an artemisia apiacea extracellular vesicle, a pharmaceutical composition for treating cerebral apoplexy, a medicine and application of the artemisia apiacea extracellular vesicle in preparation of the medicine for treating cerebral apoplexy. The naturally-sourced vesicle delivery system provided by the invention is expected to have higher safety and lower toxic and side effects, and the enrichment concentration of the therapeutic component at the focus part of cerebral apoplexy is improved, so that the bioavailability and the treatment efficiency of the medicine are remarkably improved.

The invention relates to application of 1, 2, 3, 4, 6-O-pentagalloylglucose in preparation of a medicine for resisting cholestatic liver diseases, and belongs to the technical field of medicinal chemistry. The 1, 2, 3, 4, 6-O-pentagalloylglucose provided by the invention can be used for promoting bile acid excretion by reducing WDR6 protein expression. In-vivo and in-vitro experiments prove that the 1, 2, 3, 4, 6-O-pentagalloylglucose can be used for remarkably relieving the symptom of the cholestatic liver disease. In addition, the 1, 2, 3, 4, 6-O-pentagalloylglucose has no obvious toxic or side effect, and has no obvious influence on the liver function and the kidney function. The 1, 2, 3, 4, 6-O-pentagalloylglucose has a wide anti-cholestatic liver disease spectrum, and is suitable for various cholestatic liver diseases, such as primary biliary cholangitis (PBC), primary sclerosing cholangitis (PSC) and the like.

The invention discloses radix ophiopogonis powder for relieving anxiety and improving sleep. The radix ophiopogonis powder is prepared by carrying out fermentation on radix ophiopogonis through plant lactobacillus GDMCC No. 64374 and carrying out enzymolysis treatment through pullulanase. The invention further discloses a preparation method and application of the radix ophiopogonis powder. The saponin content of the radix ophiopogonis powder is obviously increased. The radix ophiopogonis powder can be prepared into products in various forms, has the effects of relieving anxiety mood and improving sleep, is high in bioavailability and free of toxic and side effects, and can be eaten for a long time. Compared with the traditional radix ophiopogonis powder, the radix ophiopogonis powder disclosed by the invention is relatively low in safety risk and more obvious in effects of relieving anxiety mood and improving sleep.

The invention belongs to the technical field of biological medicines, and relates to application of Ackermann muciniphile or its external vesicles in preparation of a drug for treating schistosomiasis. The anti-infection immunity of a host is enhanced by adjusting intestinal flora balance (recovering diversity and composition) and improving immune response (adjusting macrophage, CD8 + T cell recruitment and Th1 / Th2 balance); meanwhile, the intestinal barrier function is improved, and pathogen invasion and inflammation are reduced; hepatic granuloma and hepatic fibrosis caused by schistosome infection are obviously relieved, and the liver function is improved; the key effect of the MIF gene in immunoregulation is disclosed, and a new direction is provided for schistosomiasis immunotherapy. Besides, the probiotics are high in treatment safety and free of obvious side effects, can be combined with chemotherapy to enhance the curative effect and reduce the side effects and drug resistance of chemical drugs, provides a lasting and comprehensive adjuvant therapy scheme for the schistosomiasis, and has important clinical application potential.

The disclosure relates to the use of phosphodiesterase 1 (PDE1) inhibitors for the treatment of cancers and tumors, including for inhibiting tumor recruitment of macrophages and other cells to the tumor or cancer, for complementing and enhancing checkpoint inhibitor therapies, and for mitigating the side effects (i.e., inflammatory-related adverse events) associated with checkpoint inhibitor therapies.

The invention belongs to the technical field of drug development, and particularly relates to application of 2-fluoro-N-(2-(4-methyl-2-(m-tolyl) thiazole-5-yl) ethyl) benzenesulfonamide in preparation of drugs for treating nervous system diseases. The invention aims to provide a medicine which has small toxic and side effects and can target SLC11A2 to treat or improve nerve cell injury. According to the technical scheme, the invention relates to application of 2-fluoro-N-(2-(4-methyl-2-(m-tolyl) thiazole-5-yl) ethyl) benzenesulfonamide in preparation of a medicine for treating nervous system diseases. It is proved that the compound 2-fluoro-N-(2-(4-methyl-2-(m-tolyl) thiazole-5-yl) ethyl) benzenesulfonamide is small in toxic and side effect, and nerve cell damage can be protected or improved by targeting SLC11A2; and a new choice is provided for treating or improving nerve cell injury.

A system and method are herein disclosed. The system and method use a generative AI agent to analyze and identify synergistic blends of natural compounds for combination therapies by leveraging an array of specialized modes to access data from a multitude of sources including patient medical history (including test results, drug history, and imaging) to improve the efficacy of compounds, including traditional medicine, in line with combination therapy principles, aimed at: enhanced efficacy, decreased toxicity, improved dosage, and reduced drug resistance. In this way, the generative AI agent determines cross-therapeutic similarities and / or dissimilarities between pharmaceutical, naturopathic, homeopathic, and nutraceutical compounds along a plurality of compound property vectors such as efficiency, efficacy, toxicity, effects, side-effects, chemistry, pharmacology, pharmacokinetics, mechanisms of action, and pharmacodynamics, thereby enabling the proposition of cross-disciplinary and transdisciplinary therapeutic analyses and the identification of synergistic effects in combination therapies.

The invention belongs to the technical field of biological medicines, and particularly relates to application of poecilobdella manillensis in preparation of a medicine for treating renal injury. The invention provides a new application of poecilobdella manillensis in preparation of a medicine for treating renal injury, serum biochemical index detection proves that the poecilobdella manillensis can effectively reduce serum creatinine and blood urea nitrogen levels, increase serum albumin and total protein content, remarkably improve glomerular filtration function and protein metabolism function, and improve renal function. And the improvement degree of the traditional Chinese medicine composition is superior to that of a traditional Chinese medicine contrast. Although the curative effect is slightly poorer than that of a chemical drug group, the safety advantage is remarkable. The poecilobdella manillensis can comprehensively regulate renal function metabolism indexes, relieve kidney injury and avoid common side effects of chemical drugs, provides a new choice for clinical treatment of kidney injury, and is especially suitable for chronic kidney disease patients needing long-term treatment.

The invention relates to the technical field of biological medicines, in particular to an iRGD targeted and anti-fibrosis small molecule dual-modified exosome as well as a construction method and application thereof. The exosome utilizes the specific binding penetration enhancement effect of iRGD (the amino acid sequence is CRGDKGPDC) and a fibroblast high-expression integrin receptor, so that the enrichment efficiency of the exosome at a focus part is improved; the anti-fibrosis micromolecule Let-7a-5p can inhibit a TGF-beta signal channel by blocking Smad2 / 3 phosphorylation, and the anti-fibrosis micromolecule Let-7a-5p and the anti-fibrosis microRNA carried by the exosome generate a synergistic anti-fibrosis effect; the exosome phospholipid bilayer can also protect Let-7a-5p from enzymolysis and prolong the half-life period, and iRGD modification can reduce the non-targeted uptake rate. An animal model verifies that the double-modified exosome has a good skin fibrosis resisting effect, and side effects such as liver and kidney function damage are not found. The invention provides an effective and safe treatment scheme for resisting skin fibrosis.

The invention discloses a composition for treating prostatitis and a preparation method and application thereof. The composition is prepared from the following components in parts by weight: 5 to 15 parts of ergothioneine, 10 to 20 parts of cistanche total glycosides, 25 to 45 parts of phytosterol, 450 to 550 parts of pumpkin seed oil, 180 to 250 parts of fructus cannabis oil and 250 to 350 parts of auxiliary materials. Through the synergistic effect of various natural active components, the composition maintains the balance of overall metabolism of a body while reducing inflammation and inhibiting prostate cell proliferation, side effect risks possibly brought by a traditional single-component treatment scheme are avoided, and the composition has higher clinical application potential. The composition disclosed by the invention has a wide market application prospect and popularization value by virtue of good safety and compliance.

The present invention is directed to lipid nanoparticles using cationic cholesterol for topical delivery for nucleic acid delivery, and when administered locally, side effects caused by systemic drug delivery can be minimized and protein expression can be confined to the site of administration. In addition, the duration of protein expression at the site of administration can be increased, and thus the lipid nanoparticles can be useful in the technical field related to nucleic acid therapeutics.

The invention provides application of active decapeptide in preparation of a medicine for preventing or treating cerebral apoplexy, and belongs to the technical field of biological medicine, the active decapeptide with the amino acid sequence as shown in SEQ ID NO.1 is applied to prevention or treatment of cerebral apoplexy for the first time, the active decapeptide can effectively inhibit formation of cerebral thrombosis of zebra fish with ischemic cerebral apoplexy, and the active decapeptide can be used for preventing or treating cerebral apoplexy. The brain blood flow supply is recovered; meanwhile, the active decapeptide can significantly reduce the hemorrhagic area and hemorrhagic rate of the zebra fish brain with hemorrhagic stroke, repair brain vascular injury and inhibit the occurrence and development of hemorrhagic stroke. In addition, the active decapeptide has small toxic and side effects, and is of great significance for improving the clinical curative effect of cerebral apoplexy and reducing the medication risk when being used for research and development of novel drugs for resisting cerebral apoplexy.

The invention discloses a cape jasmine and fennel compound extract and a preparation method and application thereof, and belongs to the technical field of plant extracts.The preparation method of the cape jasmine and fennel compound extract comprises the steps that S1, a cape jasmine extract is prepared; s2, preparing a fennel extract; s3, the fennel extract and the fructus gardeniae extract are mixed according to a certain proportion to obtain the fructus gardeniae and fennel compound extract, the fennel extract prepared through the preparation method comprises an oil component and a water-soluble component, the compound extract achieves the effect of 1 + 1 > 2, has the remarkable effect of reducing blood fat and blood sugar, does not have side effects, and is suitable for large-scale popularization and application. The traditional Chinese medicine composition has an obvious regulating effect on blood pressure and blood fat of patients, has the efficacy of improving blood pressure, blood fat and blood sugar of patients, and is nontoxic and harmless to human bodies and free of side effects.

The present disclosure pertains to novel Glucagon like Peptide-1 (GLP-1) (7-37) analogs having an amino acid sequence with Leu or Ile at the C-terminal. The new analogs are potent GLP-1 agonists with reduced adverse effect and improved duration of action. The present disclosure further relates to acylated derivatives of the new analogs which have further improved potency and duration of action and are suitable for oral administration. The analogs of present disclosure may be useful in treatment of diabetes and obesity.

A pharmaceutical composition comprises a GPCR agonist fusion protein in which a GPCR agonist peptide is covalently coupled to albumin via a linker in a manner that is resistant to a retro-Michael addition. Advantageously, compositions presented herein avoid decoupling of the agonist form the albumin while retaining the agonist in a steric relationship to the albumin that allows for effective binding and activation of the GPCR while also enabling gp60-mediated transcytosis and FcRn-mediated albumin recycling. These properties enable ultra-low dosages for the GPCR agonist fusion protein to give a therapeutic effect while substantially reducing or even entirely avoiding adverse effects otherwise commonly associated with unbound agonists. Such retro-Michael resistant composition is generally achieved by conformational modification of the albumin, resulting in stereoselective coupling of the linker to the albumin.

A pharmaceutical composition comprises a GPCR agonist fusion protein wherein the GPCR agonist peptide is covalently conjugated to an albumin via a linker in a manner that is resistant to a reverse Michael addition. Advantageously, the compositions presented herein avoid uncoupling of the agonist to the albumin while maintaining the agonist and the albumin in a spatial relationship that allows efficient binding and activation of the GPCR while also enabling gp60-mediated endocytosis transport and FcRn-mediated albumin recirculation. These characteristics enable ultra-low doses of GPCR agonist fusion proteins to produce therapeutic effects while significantly reducing or even completely avoiding side effects that would otherwise be typically associated with unbound agonists. Such reverse Michael resistant compositions are typically achieved by conformationally modifying an albumin, resulting in a stereoselective coupling of a linker to the albumin.

The invention discloses a pharmaceutical composition for treating non-small cell lung cancer and application of the pharmaceutical composition. The composition comprises an IGF2BP3 inhibitor and a platinum chemotherapeutic drug. According to the combined medication scheme, the IGF2BP3 function is inhibited to block an ATF4 survival promoting signal channel mediated by the IGF2BP3 function, a synergistic effect is generated with a DNA damage mechanism of platinum drugs, the anti-tumor effect can be remarkably enhanced, chemotherapy drug resistance can be effectively reversed, toxic and side effects are expected to be reduced, and the application prospect is wide. And a new strategy is provided for overcoming the treatment problem of the non-small cell lung cancer, especially platinum-resistant non-small cell lung cancer.

The invention discloses application of a target protein circPIAS1-108aa inhibitor combined with oxaliplatin in preparation of a medicine synergistic composition for treating cancers, the specific action mechanism of circPIAS1-108aa in colon cancer treatment is found for the first time, and further research shows that by using siRNA to knock down circPIAS1-108aa, colon cancer cell proliferation can be remarkably inhibited, and the effect of treating the colon cancer can be achieved. Furthermore, the target spot protein circPIAS1-108aa inhibitor can be used for enhancing the treatment effect of the oxaliplatin. Therefore, when the circPIAS1-108aa expression is inhibited in a targeted manner and the oxaliplatin is combined for use, the circPIAS1-108aa can be obviously used for preventing and treating cancers, the dosage and toxic and side effects of the oxaliplatin are reduced, and a new synergistic strategy is provided for tumor treatment.

The invention relates to a traditional Chinese medicine composition with functions of tonifying qi and nourishing blood for livestock. The traditional Chinese medicine composition comprises the following components in parts by weight: 10-30 parts of astragalus membranaceus, 10-40 parts of spina gleditsiae, 10-20 parts of angelica sinensis, 10-20 parts of codonopsis pilosula, 10-30 parts of uniflower swisscentaury root, 10-30 parts of ligusticum wallichii, 10-20 parts of cowherb seed, 10-20 parts of fruit of liquidambar formosana hance and 1-10 parts of iron sucrose. The traditional Chinese medicine composition is scientific and reasonable in component, free of toxic and side effects and medicine residue, convenient to take and low in cost, has the functions of tonifying qi and nourishing blood, stimulating the menstrual flow and prompting lactation, and is capable of effectively treating diseases of postpartum hypogalactia, breast milk stoppage and the like which are normal in livestock.

The present invention provides compositions comprising one or more ACAT inhibitors and one or more GLP-1 receptor agonists (GLP-1 RAs). The combination therapy reduces side effects associated with high-dose GLP-1 RA monotherapy and provides durable management of weight loss by suppressing rebound of body weight, blood glucose, and cholesterol levels after treatment.

The invention provides therapeutic methods, pharmaceutical compositions, and unit dose formulations for treating movement disorders, such as using a muscarinic acetylcholine receptor inhibitor in combination with a muscarinic acetylcholine receptor activator to treat dystonia. In some aspects, the invention provides a method of treating a movement disorder in a patient, where the method comprises administering to a patient in need thereof (i) a muscarinic acetylcholine receptor inhibitor in an amount effective to treat the movement disorder and (ii) a muscarinic acetylcholine receptor activator in an amount effective to reduce the frequency and / or magnitude of at least one side effect of the muscarinic acetylcholine receptor inhibitor, to thereby treat the movement disorder.

The invention discloses a hematopoietic preparation for treating androgenetic alopecia and a preparation method of the hematopoietic preparation. The hematopoietic preparation is prepared from 5-30 parts of radix polygoni multiflori preparata, 5-30 parts of wine ligustrum lucidum ait, 5-30 parts of mulberry, 5-30 parts of eclipta, 5-30 parts of radix paeoniae alba, 5-30 parts of astragalus membranaceus and 5-30 parts of rhizoma cibotii. The medicine composition and the specific dosage are obtained through a large number of experimental screening and clinical medication experience screening. The whole formula takes tonifying liver and kidney and benefiting essence and blood as the monarch, and takes tonifying spleen and qi and removing heat to cool blood as the minister and assistant, based on the traditional Chinese medicine theory that essence is stored in kidney and is warmed on hair, by inhibiting DHT generation, resisting hair follicle apoptosis and improving scalp microcirculation, the traditional Chinese medicine composition has the remarkable effect of treating androgenetic alopecia, is weak in toxic and side effects, and can be prepared into various clinical dosage forms.

The invention discloses an application of imatinib mesylate in preparation of a targeted therapeutic drug for gastric signet ring cell carcinoma. The imatinib mesylate has an obvious inhibition effect on the growth of six patients with the pathological type of gastric signet-ring cell carcinoma, the inhibition effect is more obvious along with the increase of the concentration, the concentration and dosage dependency relationship is shown, and the half inhibitory concentration (IC50) is obviously smaller than that of a positive control drug apatinib. The medicine can play a targeted therapeutic role on the gastric signet ring cell carcinoma, and is small in toxic and side effects, economical, practical and low in cost.

The invention relates to the technical field of pharmaceutical preparations, in particular to a rapamycin multiphase release or osmotic pump type weekly-effect oral controlled-release composition and a preparation method thereof, and the rapamycin multiphase release or osmotic pump type weekly-effect oral controlled-release composition comprises a quick release layer, a slow release layer and an osmotic pump structural design. According to the application, staged or constant-rate release of rapamycin within 168 hours is realized through a multi-phase release technology or an osmotic pump technology, and the problems that an existing preparation is large in blood concentration fluctuation, high in administration frequency and low in bioavailability are solved. The composition is suitable for treating hypertrophic cardiomyopathy of cats, significantly improves cardiac functions and reduces side effects and risks, is administered once a week, and is convenient to use. The invention further provides a storage method, and the product stability is ensured. The technical scheme has remarkable clinical advantages and application prospects.

The invention belongs to the technical field of drug development, and particularly relates to application of (E)-N-benzyl-2-((5-(thiophenyl) furan-2-yl) methylene) hydrazine-1-thioformamide in preparation of drugs for treating nervous system diseases. The invention aims to provide a medicine which has small toxic and side effects and can target SLC11A2 to treat or improve nerve cell injury. According to the technical scheme, the invention relates to application of (E)-N-benzyl-2-((5-(thiophenyl) furan-2-yl) methylene) hydrazine-1-thioformamide in preparation of a medicine for treating nervous system diseases, in particular to application of (E)-N-benzyl-2-((5-(thiophenyl) furan-2-yl) methylene) hydrazine-1-thioformamide. It is proved that the compound (E)-N-benzyl-2-((5-(thiophenyl) furan-2-yl) methylene) hydrazine-1-thioformamide is small in toxic and side effect, and nerve cell damage can be protected or improved by targeting SLC11A2; and a new choice is provided for treating or improving nerve cell injury.