158 results about "Dose dependence" patented technology

The invention relates to the technical field of biological medicine, in particular to an antibody aiming at staphylococcus aureus enterotoxin B and application thereof. A heavy chain variable region of the antibody provided by the invention comprises CDR sequences as shown in SEQ ID NO.1-3, and a light chain variable region of the antibody comprises CDR sequences as shown in SEQ ID NO.9-11. The antibody has high affinity, can specifically bind to staphylococcus aureus SEB, can block binding of SEB and MHC II / TCR, significantly inhibits cytokine storm, shows a dose-dependent protection effect in an MRSA systemic infection model, and can be used for preparing an MRSA systemic infection model. The monoclonal antibody can be used for treating, preventing or diagnosing the infection of the staphylococcus aureus, provides a solution of non-antibiotic therapy for SEB poisoning and drug-resistant staphylococcus aureus infection, and has important clinical and public health values.

The invention belongs to the technical field of microorganisms, and particularly relates to application of bifidobacterium longum in preparation of products for prevention, treatment and / or adjuvant treatment of pneumonia. The preservation number of the bifidobacterium longum is GDMCC No: 65969, and the bifidobacterium longum can improve the body weight decrease trend of a pneumonia mouse and reduce the lung visceral organ index of LPS increase; the content of pro-inflammatory factors such as IL-1beta, TNF-alpha and IL-6 in serum is remarkably reduced, mRNA expression of inflammation-related genes such as COX-2, IFN-gamma and TNF-alpha in lung tissue is reduced, and dose dependence is achieved; meanwhile, alveolar structure damage and inflammatory cell infiltration of mouse lung tissue are relieved, and lung tissue pathological damage is repaired. The strain can be used as a core component for developing pneumonia prevention or adjuvant therapy related products, provides a novel microbial intervention means for pneumonia prevention and treatment, and has important application value.

The invention discloses a novel immunologic adjuvant, a composition containing the immunologic adjuvant and a pharmaceutical composition. The immunologic adjuvant is picrasidine S. The immunologic adjuvant composition comprises picrasidine S and optionally one or more other types of immunologic adjuvants, such as an aluminum adjuvant. The pharmaceutical composition comprises an antigen and the immunologic adjuvant composition. Experiments prove that the picrasidine S can effectively stimulate dendritic cells to generate cell factors IFN-beta and IL-6, and has PS dose dependence; picrasidine S plays an important role in enhancing specific humoral immune response of different types of antigens, and has a stronger effect than an aluminum adjuvant; the picrasidine S immunity can enhance the anti-tumor immune response in different tumor models. According to the invention, a new candidate drug is provided for research and development of a new generation of vaccine adjuvants, and meanwhile, the medical application of the picrasidine S is also widened.

The invention discloses a formula for reducing phlegm and resolving masses, and a preparation method and application of freeze-dried powder of the formula for reducing phlegm and resolving masses, and belongs to the technical field of traditional Chinese medicines. The traditional Chinese medicine composition inhibits triple negative breast cancer adhesion-metastasis by regulating an FAK / SRC pathway, and comprises the following components by weight: 10-20 g of poria cocos, 10-20 g of rhizoma bolbostemmae, 10-20 g of radix trichosanthis, 5-12 g of curcuma zedoary, 10-20 g of selfheal, 10-20 g of oyster (smashed and decocted first), and 5-12 g of uniflower swisscentaury root. In-vitro experiments show that HTSJF can inhibit TNBC cell invasion, migration and adhesion (P is less than 0.01) in a dose-dependent manner, and along with reduction of the phosphorylation level of an FAK / SRC pathway, it is prompted that HTSJF inhibits TNBC transfer by regulating the pathway. In-vivo experiments prove that the HTSJF can obviously inhibit the reduction of TNBC pulmonary metastasis focus (P is less than 0.05) and recover part of normal pulmonary alveolar structures, and the inhibition effect of the HTSJF on TNBC pulmonary metastasis is further proved.

The invention relates to an application of Avasimibe in preparation of a medicine for treating nasopharynx cancer or oral cancer, and belongs to the field of tumor targeted therapy. An in-vitro cell experiment and an in-vivo animal model experiment verify the anti-tumor effect of the compound. Experiments show that Avasimibe can significantly inhibit the activity, proliferation ability, healing ability and cloning ability of nasopharynx cancer cells and oral cancer cells, can regulate cell cycle arrest in a dose-dependent manner, and induces cell apoptosis. In vivo experiments, the tumor volume of nude mice in an Avasimibe treatment group is remarkably reduced, serum cholesterol is remarkably reduced, and serum biochemical analysis shows that compared with a control group, the Avasimibe treatment group has no statistical difference in indexes such as aspartate transaminase (AST) / glutamic-pyruvic transaminase (ALT) and creatinine (Cr). The invention provides a new indication for resisting nasopharynx cancer and oral cancer for the existing compound Avassimibe, has the clinical advantages of low toxicity and capability of overcoming drug resistance, and provides a new treatment choice for patients with nasopharynx cancer and oral cancer.

The invention discloses an application of DL-3-phenyllactic acid in treatment of cardiac mucinoma. Based on metabonomics, it is found that the level of endogenous DL-3-phenyllactic acid in serum of a patient is remarkably reduced, pharmacodynamic verification is conducted by means of a cardiac mucinoma tissue-derived cardiac mucinoma organ model of the patient, it is proved that DL-3-phenyllactic acid can inhibit proliferation of cardiac mucinoma organs in a dose-dependent mode, and the half inhibitory concentration IC50 value of DL-3-phenyllactic acid is 95.52 mu M. The DL-3-phenyllactic acid can inhibit proliferation of cardiac mucinoma organs in a dose-dependent mode. Network pharmacological analysis indicates that the drug action mechanism may involve key targets such as AKT1 and SRC. The invention discloses the therapeutic efficacy of the DL-3-phenyllactic acid on the cardiac mucinoma for the first time, and provides a solid preclinical experimental basis for developing the DL-3-phenyllactic acid into the medicine for treating the cardiac mucinoma. The invention has non-obvious and important clinical application value.

The application discloses a use of phenazine-1-carboxylic acid or a pharmaceutically acceptable salt thereof in preparation of a medicine for inhibiting African swine fever virus. The application uses a double reporter virus rASFV-Gluc / EGFP co-expressing green fluorescent protein and Gaussia luciferase to screen 246 natural small molecule compounds, and finds that phenazine-1-carboxylic acid has a significant inhibiting effect on replication of the ASFV; further evaluation of the inhibiting effect finds that the half maximal cytotoxicity concentration of PCA on target cells of primary porcine alveolar macrophages is 470.5 muM, and the half maximal inhibitory concentration of PCA on the ASFV in PAMs is 1.59 muM. According to a dose-dependent inhibiting experiment result, when the concentration of PCA is 25 muM, the inhibiting effect on the ASFV can reach more than 100 times. The application has application prospects in preparation of medicines or preparations against the ASFV.

The invention relates to application of (E)-2-(4-(dimethylamino) styryl)-6-methoxy-3-methylbenzo [d] thiazole-3-onium in preparation of anti-cancer drugs, and belongs to the technical field of medical application, the structure of (E)-2-(4-(dimethylamino) styryl)-6-methoxy-3-methylbenzo [d] thiazole-3-onium is as shown in the following formula I, the (E)-2-(4-(dimethylamino) styryl)-6-methoxy-3-methylbenzo [d] thiazole-3-onium can inhibit the growth of gastric cancer cells, inhibit the proliferation, invasion and migration of the gastric cancer cells by promoting the autophagy and mitochondrial rupture of AGS and HGC-27 cells of the gastric cancer cells, and block the gastric cancer cells in the G1 stage. Furthermore, in-vivo experiments of mice prove that ZWK-3 can inhibit tumor growth of the mice, shows obvious dose dependence, and does not influence the body weight and visceral indexes of the mice at the same time. Formula I.

This application discloses the application of dasabuvir as a TRPV4 inhibitor in improving diseases caused by increased TRPV4 expression or enhanced activity, particularly ulcerative colitis. Specifically, it relates to the biomedical field. Dasabuvir is a novel TRPV4 inhibitor that can improve symptoms in a DSS-induced mouse ulcerative colitis model and is suitable for use in TRPV4 inhibitor drugs and ulcerative colitis drugs. In HEK-293 cells overexpressing TRPV4, dasabuvir can dose-dependently inhibit the increase in intracellular calcium ion concentration induced by the TRPV4-specific agonist GSK1016790A within a concentration range of 0.03-30 μM, with an IC50 concentration of [missing information]. 50 At a concentration of 0.27 μM, Dasabuvir is a highly active TRPV4 inhibitor. In a DSS-induced ulcerative colitis model, Dasabuvir can improve weight loss, reduce the disease activity index, alleviate colonic shortening, reduce histopathological changes, and inhibit the expression of inflammatory factors, thus improving ulcerative colitis.

This invention discloses a heterozygous sesquiterpene tricyclic epoxy compound derived from the strain *Arthrum oligosporum*, its preparation method, and its applications, belonging to the field of natural product chemistry. This invention provides a heterozygous sesquiterpene tricyclic epoxy compound derived from *Arthrum oligosporum* (… A.oligospora ) AOL_ s00210g57 Anthrobotrisin D, a novel heterozygous sesquiterpene tricyclic epoxy compound from a gene knockout strain, has been shown in vitro to possess excellent anti-inflammatory activity, significantly inhibiting lipopolysaccharide-induced inflammatory responses in mouse microglia. It exhibits a clear dose-dependent inhibitory trend at multiple levels, including NO release, protein and mRNA expression of inflammatory factors (TNF-α, IL-1β, IL-6), and iNOS protein and mRNA expression. Furthermore, at a concentration of 33 μM, its anti-inflammatory effect is comparable to that of the clinically proven positive drug dexamethasone, and in some aspects, it is even superior. This invention not only provides a new lead compound for the development of anti-inflammatory drugs but also opens up new directions for developing new drugs from the unique microbial resource of nematode-preying fungi.

The invention discloses an application of distension hippocampus submicron powder in preparation of a composition for acetaminophen-induced liver injury. The application of the superfine powder form of the hippocampus japonicus which can be cultured on a large scale to the APAP liver injury is developed, the effect is equivalent to or superior to that of NAC, the advantages of dose dependence and multi-target protection are achieved, sustainable utilization of marine medicinal materials is promoted, and a novel, safe and effective strategy is provided for clinical prevention and treatment of the liver injury.

The invention discloses a nagilactone C liposome, a preparation method thereof and an application of the nagilactone C liposome in treatment of acute lung injury, conventional nagilactone C is prepared into the liposome with good solubility, and the liposome is used for treating the acute lung injury and has good anti-inflammatory activity. The liposome of the compound Nag C is prepared for the first time, it is found for the first time that the liposome of the compound Nag C can treat LPS-induced acute lung injury of mice, the Nagilactone C liposome can relieve inflammation-induced lung tissue cell apoptosis, and the protection effect shows obvious dose dependence.

The invention discloses ginseng polysaccharide GP40030-1 as well as a preparation method and application thereof, and belongs to the technical field of biological medicines. The ginseng polysaccharide GP40030-1 provided by the invention can obviously promote the proliferation of mouse macrophages RAW264.7 and effectively improve the phagocytic ability of cells, is dose-dependent in a concentration range of 12.5-100 mu g / mL, shows excellent immunomodulatory activity, and has a wide application prospect in the aspect of preparing medicines, functional foods or health products for enhancing immunity.

This invention discloses an endothelin A receptor antagonist-albumin fusion protein and its application in preventing and treating hypotension during anesthesia induction. The fusion protein is formed by chemically coupling BQ-123 with human serum albumin (HSA). BQFu significantly enhances its antihypertensive effect by prolonging the half-life of BQ-123 and improving plasma stability. Experiments show that BQFu dose-dependently inhibits the decrease in mean arterial pressure (MAP) in a propofol-induced hypotension model, with a sustained and stable effect in the high-dose group (30 mpk), shortening the recovery time to 20.8 ± 10.5 min, while maintaining BQ-123 activity. This invention provides a long-acting and safe prevention and treatment strategy for hypotension during anesthesia induction.

The application discloses application of a PRMT3 inhibitor SGC707 in preparation of a drug for treating pulmonary fibrosis, and for the first time verifies that a selective PRMT3 inhibitor SGC707 can dose-dependently inhibit expression of fibrosis markers such as COL1A1 and alpha-SMA in fibroblasts induced by TGF-beta 1 in vitro; in a bleomycin (BLM) induced mouse pulmonary fibrosis model, SGC707 administration can significantly improve lung tissue collagen deposition, reduce inflammatory cell infiltration, repair alveolar structure damage, and effectively down-regulate expression levels of fibrosis related proteins in lung tissues. It is proved that PRMT3 is a functional target with important intervention value in pulmonary fibrosis, SGC707 has definite anti-pulmonary fibrosis activity in vitro and in vivo, and a new drug strategy is provided for treatment of pulmonary fibrosis.

The Cardio-Tox Tissue Engineered Model (TEEM) invention provides a robust in vitro model for cardiotoxicity evaluation using three-dimensional (3D) human heart microtissues to quantify dose-dependent changes in electromechanical activity, resulting in a comprehensive cardiotoxicity and arrhythmia risk assessment of test compounds. The invention also provides a predictive in vitro screening platform for pro-arrhythmic toxicity testing using human three-dimensional cardiac microtissues. The invention enables the screening of environmental and pharmaceutical compounds, chemicals, and toxicants to establish safe human exposure levels.

The application provides a 5-hydroxymethylfurfural recognition aptamer and application, wherein the 5-hydroxymethylfurfural recognition aptamer comprises the following nucleotide sequence: 5'-GGGAGGACAGATACGGTGGGA-3'. The 5-hydroxymethylfurfural recognition aptamer provided by the application comprises good dose-dependent detection capability for 5-hydroxymethylfurfural, can rapidly realize accurate detection of 5-hydroxymethylfurfural in food, and has high detection convenience and does not need to rely on large and precise instruments.

The present invention discloses the application of deer horn glue in the treatment of zebrafish bone injury, belonging to the technical field of fish bone injury. The present invention prepared deer horn glue and used LPS induction to establish a zebrafish bone injury model for comprehensive evaluation. The IC50 of deer horn glue in zebrafish was 206.3 μg / mL; the treatment with deer horn glue could alleviate the inhibitory effects of LPS on cartilage development and bone formation in a dose-dependent manner; it could significantly reduce the green fluorescence intensity of macrophages and inhibit the activation of macrophages induced by LPS; it inhibited the excessive secretion of inflammatory factors IL-6, IL-1β and NO; it significantly restored the mRNA levels of bone-related genes COL2α1 and Sox9a. This study confirmed that deer horn glue could alleviate zebrafish bone injury caused by LPS and at the same time inhibit the macrophage-mediated inflammatory cascade reaction, providing a basis for the treatment of fish bone diseases.

The invention discloses application of physcion in preparation of a medicine for reducing liver cell lipid deposition, and particularly relates to application of physcion in preparation of a medicine for preventing and treating lipid deposition fatty liver. In-vitro cell experiments prove that the physcion shows low toxicity and a wide safety range in a human normal hepatocyte line THLE3, a human hepatoma cell line HepG2 and a mouse normal hepatocyte line AML12, and can obviously reduce the level of oleic acid-induced intracellular triglyceride in a dose-dependent manner, so that the physcion can be used for preparing a medicine for treating liver cancer. Oil red O staining results also visually show that lipid droplet accumulation in cells can be effectively reduced; according to the invention, the technical prejudice that the emodin monomethyl ether is regarded as a potential hepatotoxic component in the prior art is overcome, a safe and effective new choice is provided for the treatment of the lipid deposition fatty liver, and the pharmaceutical composition has a wide clinical application prospect.

The present invention discloses a semicarbazide derivative and its preparation method and application, which belongs to the technical field of anti-lung cancer targeted drugs. The semicarbazide derivative of the present invention can inhibit the growth of H1299 cells in a dose-dependent manner, but has little toxicity to normal lung epithelial cells BEAS-2B. The semicarbazide derivative of the present invention can significantly inhibit the cloning of non-small cell lung cancer cells A549 and H1299, so it has a significant inhibitory effect on the proliferation of non-small cell lung cancer. The semicarbazide derivative provided by the present invention can inhibit the protein expression of GPX4 in non-small cell lung cancer A549 cells, and by inhibiting the protein expression of GPX4, promote the ferroptosis of non-small cell lung cancer cells, thereby playing a role in suppressing tumors.

The invention discloses a product for treating radiation damage. According to the application, GP532 is subjected to random mutation, a phage mutation library is established, and the mutation library is activated and screened by using TLR5-dependent NF-kappa B, so that 9E1 is obtained. 9E1 shows dose-dependent stimulation of TLR5 dependent NF-kB activation in vitro; an effective prevention effect is shown in an in-vivo mouse radiation injury model, and a new way is provided for effective treatment of radiation injury.

The invention discloses an NK cell exosome, a preparation method thereof and application of the NK cell exosome in preparation of drugs for targeted treatment of rectal cancer through meridian points, and belongs to the field of biological medicine and traditional Chinese medicine. The invention provides a method for preparing a high-purity NK cell and a high-concentration and high-potency NK cell exosome. Experimental results show that the NK cell exosome obtained by the method provided by the invention can efficiently kill tumor cells and has dose dependence; animal experiments show that the NK cell exosome prepared by the invention can significantly inhibit tumor growth; clinical cases show that accurate targeted therapy can be realized through meridian point injection of the NK exosome, indexes of a rectal cancer patient are recovered to be normal, and clinical relief is realized. According to the invention, a modern exosome technology and a traditional Chinese medicine meridian point treatment method are combined for the first time, a cell derivative medicine for treating the advanced rectal cancer is provided, and a theoretical and practical basis is provided for clinical treatment of the advanced rectal cancer.

This application discloses the use of itaconic acid derivatives in the preparation of drugs for treating candidemia, belonging to the field of biomedical technology. The itaconic acid derivatives proposed in this application are dimethyl itaconic acid and / or 4-octyl itaconic acid. Dimethyl itaconic acid exhibits a dose-dependent therapeutic effect in model mice, with an optimal dose of 1200 mg / kg improving survival rate and reducing kidney damage; 4-octyl itaconic acid can enhance the anti-Candida albicans ability of macrophages and regulate the expression of inflammatory factors. The application of the itaconic acid derivatives proposed in this application in the treatment of candidemia works through immunomodulation, circumventing fungal resistance. Furthermore, the drugs are low in toxicity, have good biocompatibility, and use a universal experimental system, providing a new approach for the clinical treatment of candidemia with broad application prospects. This application also protects pharmaceutical compositions for treating candidemia with dimethyl itaconic acid and / or 4-octyl itaconic acid as active ingredients.

The invention relates to a traditional Chinese medicine preparation, in particular to application of a compound live brain soothing capsule in preparation of a medicament for treating insomnia. The dosage of the medicine is 200 mg / kg. Experiments show that the sleep improvement effect of the compound Shuonaoshu capsule on an anesthesia reviving experiment evaluation test medicine, a high-dose group (200 mg / kg) of the compound Shuonaoshu capsule can effectively prolong sleep time, dose dependence exists, sleep quality can be moderately improved, the higher the concentration is, the more obvious the improvement effect is, and the more obvious the effect is. The invention reveals that the compound Liangjinshu capsule has a treatment effect on insomnia, and is expected to provide a certain experimental basis for the development of new drugs for insomnia.

The invention belongs to the technical field of medicines, and particularly discloses an oral squamous cell carcinoma inhibitor and application thereof. The inhibitor takes rutin as an active component. In-vitro experiments prove that rutin can significantly inhibit proliferation, clone formation, migration and invasion ability of OSCC cells in a dose-dependent manner, and effectively induce cell apoptosis. The action mechanism of the rutin is as follows: the rutin can directly target STAT3 protein and inhibit phosphorylation of the STAT3 protein so as to regulate and control a downstream BCL2 / CASP3 apoptosis pathway, thereby playing a role in treating OSCC. Molecular docking results further show that rutin and STAT3 have strong binding capacity. The invention discloses a new application of rutin as an STAT3 inhibitor in treating oral squamous cell carcinoma, and provides a new strategy and a candidate compound for developing high-efficiency and low-toxicity OSCC treatment medicines.

The application discloses an indole dione piperazine alkaloid compound and a preparation method and application thereof, and belongs to the technical field of marine natural products. The Aspergillus sp. SYPHU504 is preserved in the Guangdong Microbial Culture Collection Center on August 26, 2024, and the preservation number is GDMCC No: 65055. The indole dione piperazine alkaloid compound and a pharmaceutically acceptable salt, isomer or solvate thereof are prepared from a fermentation culture of the Aspergillus sp. SYPHU504. It is found through experiments that the indole dione piperazine alkaloid compound can significantly inhibit the proliferation of leukemia cell strains K562 and RS4:11 in a dose-dependent manner. Therefore, the indole dione piperazine alkaloid compound is expected to be developed into a safe and effective novel anti-leukemia drug, and has important significance for the development of Chinese marine drug resources.

The invention discloses a CD147 nano antibody G45 as well as a preparation method and application thereof, and belongs to the technical field of molecular biology and immunology. A phage display technology is used for screening from a natural alpaca nano antibody phage library, finally three nano antibody genes are selected and cloned into pCold II, and prokaryotic expression recombinant plasmids are successfully constructed; the method comprises the following steps: carrying out inducible expression for 20 hours under the conditions that the final concentration of IPTG (isopropyl-beta-d-thiogalactoside) is 0.2 mmoL / L, the temperature is 16 DEG C and the speed is 100 rpm / min, carrying out nickel column purification, and then carrying out Coomassie brilliant blue dyeing and Western blot identification, so as to determine and obtain the CD147 nano antibody which is named as A8, B8 and G45; the binding activity of the three nano antibodies and the CD147 protein is detected through indirect ELISA (enzyme-linked immuno sorbent assay). The result shows that the CD147 antigen and the three nano antibodies have binding activity and are dose-dependent. Under the same conditions, when the incubation concentration of the nano-antibody is as low as about 0.625 g / mL, the G45 binding effect is good, the amino acid sequence of the nano-antibody is shown as SEQ ID NO.7, and the nucleotide sequence of the nano-antibody is shown as SEQ ID NO.10. The invention provides a more accurate method for high-sensitivity detection of CD147.

The invention discloses an application of a small molecule drug ATWLPPR Peptide TFA in resisting mycobacterium bovis infection, and belongs to the field of biological medicine, the small molecule drug ATWLPPR Peptide TFA is an agonist of a target host factor NRP1, and then the inhibition effect of the ATWLPPR Peptide TFA on mycobacterium bovis in vitro and in vivo is researched. An in-vitro bacterial loading titration result shows that the ATWLPPR Peptide TFA treatment can present dose-dependent inhibition of the mycobacterium bovis to adhere to A549 cells. Mouse experiment results show that ATWLPPR Peptide TFA treatment can inhibit mice from being infected with mycobacterium bovis, pathological injuries of mouse lung tissues are effectively relieved, and a brand new direction is provided for prevention and control of mycobacterium bovis.

This invention discloses the application of total paeoniflorin in the preparation of drugs for the treatment of head and neck squamous cell carcinoma, belonging to the field of biomedical technology. Addressing the bottlenecks in current treatments for head and neck squamous cell carcinoma, such as high toxicity of radiotherapy and chemotherapy, low response rates to immunotherapy, and easy resistance to targeted drugs, this invention provides a method for preparing total paeoniflorin and a drug-loaded preparation technology based on hydrogels obtained from modified chitosan. Total paeoniflorin can dose-dependently inhibit the proliferation rate, colony formation ability, and in vitro migration ability of SCC7, FADU, and CAL27 head and neck squamous cell carcinoma cell lines, and significantly induce apoptosis. This invention utilizes the multi-target effects of total paeoniflorin to exert anti-head and neck squamous cell carcinoma effects through modulation of the tumor microenvironment and enhancement of immune surveillance. Furthermore, the loaded drug exhibits good sustained-release properties and biosafety, providing a new, highly effective, and low-toxicity strategy for the treatment of head and neck squamous cell carcinoma, and has significant clinical application value.

The application relates to the technical field of biological medicine, and discloses application of Nilotinib in preparation of a drug for inhibiting p53-AKT interaction. Relying on a double-fluorescence reporting system NanoBRET system, high-throughput screening is completed at a live cell level, and it is determined that a tyrosine kinase inhibitor Nilotinib can inhibit p53-AKT interaction. Function verification shows that Nilotinib can dose-dependently destroy a p53-AKT complex in HEK293T tool cells and U87MG, T98G and other glioma cells, release the inhibition of p53 function, and induce cell apoptosis. The above results illustrate a new path of precise intervention with the "p53-AKT interface" as a target, and provide experimental basis for redirecting Nilotinib to overcome p53-related drug resistance.