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123 results about "IC50" patented technology

The half maximal inhibitory concentration (IC₅₀) is a measure of the potency of a substance in inhibiting a specific biological or biochemical function. IC₅₀ is a quantitative measure that indicates how much of a particular inhibitory substance (e.g. drug) is needed to inhibit, in vitro, a given biological process or biological component by 50%. The biological component could be an enzyme, cell, cell receptor or microorganism.

Amitriptyline hapten and preparation method thereof, amitriptyline antigen and preparation method thereof, antibody, kit and application

The invention belongs to the technical field of biochemical engineering, and particularly relates to an amitriptyline hapten and a preparation method thereof, an amitriptyline antigen and a preparation method thereof, an antibody, a kit and application. The amitriptyline hapten has a structural formula shown as a formula (I) or a formula (II). Compared with an existing structure, the amitriptyline hapten prepared by the invention has a better immune effect. The obtained antibody is high in titer, strong in specificity and high in affinity, the LOD of amitriptyline by using an Elisa method established by the antibody is 0.013 ng / mL, the IC50 of amitriptyline is 0.865 ng / mL, the quantitative detection range is 0.07-470.3 ng / mL, the detection sensitivity is high, and the linear range is wide.
Owner:CENT SOUTH UNIV

Method for saline-alkaline-resistant screening and stress-resistant tissue culture seedling raising of bamboo reed

The invention relates to the technical field of agricultural breeding, in particular to a bamboo reed saline-alkaline resistant screening and stress-resistant tissue culture seedling raising method which comprises the following steps: step 1, pretreatment; step 2, dynamic salt stress screening: placing the seed stems in a mixed salt-alkali solution with gradient increasing, culturing, measuring the bud length and root length growth rate of axillary buds of the seed stems, fitting a salt concentration-growth rate curve, and extracting a semi-inhibitory concentration IC50 and a maximum tolerance concentration MTC; step 3, salt tolerance grade classification; 4, carrying out stress-resistant tissue culture seedling culture: carrying out in-vitro culture on the axillary bud explant of the high-salt-resistant variety in a culture medium, and inducing clumpy buds and rooting in combination with a salt-resistant inducer; 5, domestication and transplanting: performing gradual salt stress domestication on the tissue culture seedlings, transplanting the tissue culture seedlings into a saline-alkaline environment, and monitoring the adaptability of the tissue culture seedlings in the saline-alkaline environment. According to the method disclosed by the invention, the efficient cultivation system of the suitable-to-grow bamboo reed seedlings in the saline-alkali soil is established by fusing dynamic stress response analysis and stress resistance phenotype directional strengthening technologies.
Owner:JIANGSU ACAD OF AGRI SCI

Anti-trifloxystrobin monoclonal antibody and application thereof

The invention discloses an anti-trifloxystrobin monoclonal antibody and an application thereof. A light chain variable region of the anti-trifloxystrobin monoclonal antibody has an amino acid sequence as shown in SEQ ID No.1, and a heavy chain variable region of the anti-trifloxystrobin monoclonal antibody has an amino acid sequence as shown in SEQ ID No.2. The monoclonal antibody has good affinity to trifloxystrobin, the half inhibitory concentration (IC50) of the monoclonal antibody is 4.55 ng / mL, the detection limit (IC10) of the monoclonal antibody is 1.34 ng / mL, the linear range (IC20-IC80) of the monoclonal antibody is 2.11-9.83 ng / mL, the cross reaction rate of the monoclonal antibody to structural analogues such as enestroburin, picoxystrobin and metoxystrobin is smaller than 1%, and the monoclonal antibody is high in specificity and has the advantages of being good in thermal stability, high in organic solvent and acid-base tolerance and high in sensitivity. The method is suitable for detecting trifloxystrobin residues in different environments.
Owner:SOUTH CHINA AGRICULTURAL UNIVERSITY

Hybridoma cell strain secreting mefos monoclonal antibody and application of hybridoma cell strain

The invention relates to a hybridoma cell strain capable of secreting a mefos monoclonal antibody and application of the hybridoma cell strain, and belongs to the technical field of immunodetection. According to the invention, the hybridoma cell strain capable of secreting the fenofos monoclonal antibody is obtained through screening, the fenofos monoclonal antibody has high specificity and high sensitivity to the fenofos, IC50 to the fenofos is 0.231 ng / mL, and the fenofos monoclonal antibody has no cross reaction to structural analogues of the fenofos, such as triazophos, diazinon, phorate, acetyl phorate, methamidophos and the like; therefore, low-concentration isoprophos can be accurately detected.
Owner:JIANGNAN UNIV

Hybridoma cell strain secreting dextromethorphan monoclonal antibody and application thereof

The invention relates to a hybridoma cell strain capable of secreting dextromethorphan monoclonal antibody and application of the hybridoma cell strain, and belongs to the technical field of immunodetection. The monoclonal antibody secreted by the hybridoma cell strain disclosed by the invention has good sensitivity and specificity on dextromethorphan, wherein the IC50 value on the dextromethorphan is 0.162 ng / mL. The monoclonal antibody provided by the invention has no cross reaction on structural analogues of dextromethorphan, such as fentanyl, thilazine, papaverine, morphine and medetomidine, and has good specificity, so that the dextromethorphan with low concentration can be accurately detected.
Owner:JIANGNAN UNIV

Application of imatinib mesylate in preparation of targeted therapeutic drug for gastric signet ring cell carcinoma

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.
Owner:ZHONGKE BOLIN (LIAONING) BIOLOGICAL RESEARCH CO LTD

Safrole hapten and application of safrole hapten in immunoassay detection of safrole

The invention provides a safrole hapten and application of the safrole hapten in detection of safrole through immunoassay. The structure of the safrole hapten is shown in the specification. The two safrole haptens provided by the invention have spacer arms with proper lengths, and after the safrole haptens are coupled with carrier protein, the haptens can be fully exposed, and recognition of the spacer arms can be avoided as much as possible. The safrole hapten is used for preparing an artificial antigen and an antibody, and the obtained safrole monoclonal antibody is high in titer, strong in specificity and high in affinity. An immunoassay method constructed on the basis of the safrole artificial antigen and antibody has high specificity and sensitivity, the lowest detection limit LOD is 0.09 ng / mL, the half inhibitory concentration IC50 is 2.05 ng / mL, the quantitative detection range is 0.28-14.89 ng / mL, no cross reaction exists on safrole analogues, and rapid qualitative and quantitative detection can be conducted on safrole in a sample.
Owner:LICHENG TESTING & CERTIFICATION GRP CO LTD

5, 9-di-tert-butyl naphtho-indolizino phenothiazine compound as well as preparation method and application thereof

The invention relates to a 5, 9-di-tert-butyl naphtho-indolizine phenothiazine compound as well as a preparation method and medical application thereof. The compound is efficiently synthesized through Ullmann coupling and palladium-catalyzed intramolecular arylation reaction. In-vitro anti-tumor activity research shows that the compound has remarkable selective inhibitory activity on various human tumor cell lines, and particularly, the inhibitory effect on non-small cell lung cancer A549 cells (IC50 = 0.21 mu M) is improved by two orders of magnitude compared with that of cis-platinum; iC50 (half maximal inhibitory concentration) of other cell lines are as follows: 1.26 mu M of prostate cancer PC-3 cells, 6.78 mu M of liver cancer HepG2 cells, 7.99 mu M of cervical cancer Hela cells and 25.46 mu M of breast cancer MCF-7 cells. Preliminary toxicity experiments prove that the compound has the characteristic of low cytotoxicity. The compound can be used as a novel high-efficiency low-toxicity anti-tumor lead compound, and provides an important structural basis for the development of anti-cancer drugs.
Owner:NANJING FORESTRY UNIV

A broad-spectrum neutralizing antibody against novel coronavirus and its application

This invention provides a human antibody with neutralizing ability against the JN.1 variant of SARS-CoV-2 and its application, belonging to the field of biomedical technology. The antibody comprises a heavy chain sequence as shown in SEQ ID NO:1 and a light chain sequence as shown in SEQ ID NO:2; or comprises a heavy chain sequence as shown in SEQ ID NO:3 and a light chain sequence as shown in SEQ ID NO:4. The antibody of this invention binds to the extracellular domain of the JN.1 variant spike protein via ECG. 50 The value was significantly lower than that of its parent antibody, with a binding capacity increase of 3 to 5 times or more. In the pseudovirus neutralization experiment, the antibody showed a half-maximal neutralizing concentration (IC50) against JN.1 pseudovirus. 50 The antibody also showed significantly better performance than the parent antibody, with a neutralizing activity increase of 3 to 24 times or more. Furthermore, the antibody's melting temperature exceeded 75°C, demonstrating good thermal stability.
Owner:ACADEMY OF MILITARY MEDICAL SCIENCES

Golden lotus glycoside C, its preparation method and application

This invention relates to a novel substance with in vitro anti-inflammatory activity, its preparation method, and its application. The chemical name of maltol-3-1'-ethoxyhexane-1”,2”,3”,4”,5”,6”-hexaol-(4'-2”)-glucopyranoside is C. 21 H 34 O 13 Preparation method: 1. Extract *Trollius chinensis* with 70% ethanol (v / v); 2. Concentrate the extract until no alcohol odor remains and load it onto a D101 macroporous resin column; 3. Elute the fraction from the D101 macroporous resin with 30% ethanol, separate by silica gel column chromatography and gel column chromatography, and then obtain *Trollius chinensis* glycoside C using high-performance liquid chromatography. *Trollius chinensis* glycoside C is used to prepare anti-inflammatory drugs. The IC50 of *Trollius chinensis* glycoside C in this invention inhibits the release of pro-inflammatory factors TNF-α and IL-6 from LPS-stimulated mouse macrophages (RAW264.7). 50 The concentrations were 22.8 μmol / L and 31.0 μmol / L, respectively, indicating that it has good in vitro anti-inflammatory activity. This invention belongs to the field of research on effective components of natural drugs.
Owner:QIQIHAR MEDICAL UNIVERSITY

Hybridoma cell strain secreting cy3.5 monoclonal antibody and application thereof

This invention relates to a hybridoma cell line that secretes a Cy3.5 monoclonal antibody and its application, belonging to the field of immunoassay. The hybridoma cell line of this invention was deposited on November 12, 2025, at the China General Microbiological Culture Collection Center (CGMCC), located at No. 3, Courtyard 1, Beichen West Road, Chaoyang District, Beijing, with accession number CGMCC No. 46741. The Cy3.5 monoclonal antibody secreted by this cell line exhibits excellent affinity and sensitivity to Cy3.5, with an IC50 of [missing value]. 50 Reaching 10 ng / mL, the IC50 for Cy5.5 50 An immunoassay product based on this hybridoma cell line, with a concentration of up to 50 ng / mL, can be used for the detection of Cy3.5 and its analogues, providing an efficient detection method and means for the residual detection of Cy3.5.
Owner:JIANGNAN UNIV

NLRP3 inhibitor as well as preparation method and application thereof

The invention discloses an NLRP3 inhibitor as well as a preparation method and application thereof. Specifically, the invention relates to a compound shown as a formula (NLRP3i-3) or a pharmaceutically acceptable salt thereof, the formula (I) is COCCNc1nc2c (c (= O) n (C) c (= O) n2C) n1Cc1cc (OC) ccc1N, and the chemical name is 8-((4-amino-2-methoxybenzyl)-7, 9-dimethyl-7, 9-dihydro-8H-purine-6, 8-diketone. The invention also provides a preparation method of the compound, a pharmaceutical composition containing the compound, and application of the compound in preparation of drugs for preventing and / or treating NLRP3-mediated diseases. The disease is preferably myocardial ischemia reperfusion injury. Experimental results show that the compound provided by the invention has excellent NLRP3 inhibitory activity (IC50lt, 100nM), and has high selectivity to NLRP3 inflammasomes; good pharmacokinetic characteristics are achieved in a rat body, and the bioavailability is high; in myocardial ischemia reperfusion injury models of mice and rats, the composition can significantly reduce myocardial infarction area, reduce myocardial enzyme level, alleviate inflammatory response and improve heart function; preliminary toxicological evaluation shows that the safety is good. Therefore, the compound disclosed by the invention is expected to be developed into a novel medicine for treating NLRP3 related diseases such as myocardial ischemia-reperfusion injury.
Owner:PINXUANJIE TECH CO LTD

Application of radish seed extract-based active component as angiotensin converting enzyme inhibitor

The invention belongs to the field of biological medicine, and particularly relates to application of an active component based on a radish seed extract as an angiotensin converting enzyme inhibitor. The active ingredient is sinapine (sinapine) or nasturtoside (Gluconatutin), and the active ingredient is one or more than one of the active ingredients. According to the invention, affinity ultrafiltration is combined with a UPLC-Orbitrap-MS method, potential inhibitors are rapidly screened and identified on line from radish seeds, the affinity of active compounds and ACE is researched by combining molecular docking through ACE activity inhibition experiments, and finally two potential ACE inhibitors, namely sinapine and nasturtoside, are determined by combining an affinity ultrafiltration RBA value, IC50 and a binding force of molecular docking. And further research is carried out after screening, so that the research range is greatly reduced, the time of new drug discovery and research and development processes is saved, and the screening cost and risk are reduced.
Owner:SHANDONG UNIV OF TRADITIONAL CHINESE MEDICINE

Walnut-derived xanthine oxidase inhibitory peptide and application thereof

The invention discloses a walnut-derived xanthine oxidase inhibitory peptide and application thereof, and belongs to the technical field of bioactive peptide biology. The amino acid sequence of the xanthine oxidase inhibitory peptide provided by the invention is as shown in SEQ ID No. 1. Through in-vitro activity determination, the IC50 value of the inhibitory peptide is 3.34 mg / mL, and it is proved that the inhibitory peptide has high inhibitory activity on xanthine oxidase. Besides, the inhibitory peptide can reduce the levels of creatinine, urea nitrogen, adenosine deaminase, glutamic oxalacetic transaminase and glutamic-pyruvic transaminase, regulate the expression of kidney uric acid resorption protein URAT1, uric acid excretion protein GLUT9 and ABCG2, and significantly reduce the generation of uric acid, can be used for inhibiting xanthine oxidase and preventing or improving hyperuricemia, is applied to preparation of drugs for improving hyperuricemia, and has broad application prospects. The medicine takes the active peptide as the only active ingredient or one of the active ingredients, and has a good application prospect.
Owner:JILIN AGRICULTURAL UNIV

Preparation and application of a hybridoma cell strain and its secreted uniform monoclonal antibody recognizing tylosin / tilmicosin

This invention belongs to the field of immunology and discloses a hybridoma cell line and the preparation and application of its secreted monoclonal antibody that uniformly recognizes tylosin / tilmicosin. The monoclonal antibody hybridoma cell line is named DES-AOAA-14D5, with accession number CGMCC NO: 45303. This invention utilizes decarboxymethyl tylosin and oxycarboxymethyl hydroxylamine to synthesize a hapten, conjugates a carrier protein to prepare a complete antigen, immunizes mice, and, through cell fusion and screening techniques, prepares a hybridoma cell line that can secrete a monoclonal antibody that uniformly recognizes tylosin / tilmicosin. IC50 50 The effective concentrations were 1.59 and 1.72 ng / mL, respectively, with a cross-reactivity rate as high as 92.44%. An immunoassay method for the simultaneous and accurate detection of tylosin / tilmicosin in milk was established using this antibody. The cut-off value for both tylosin and tilmicosin was 16 ng / mL, and no cross-reactivity was observed with other structural analogs. The detection method of this invention shows promising application prospects.
Owner:HENAN AGRICULTURAL UNIVERSITY

A tyrosine-based HDAC inhibitor, its synthesis method and application

ActiveCN122079826Agood antitumor activityReduce entropy lossUrea derivatives preparationOrganic compound preparationHydroxamic acidTyrosine
This invention belongs to the field of pharmaceutical preparation technology, specifically relating to an HDAC inhibitor based on a tyrosine backbone, its synthesis method, and its application. The invention uses L-tyrosine as the backbone, with its aromatic ring as the Cap region, linked by a flexible alkyl chain via an ether bond, and terminated by an isohydroxamic acid group (ZBG). The tyrosine backbone provides a rigid structure, reducing entropy loss and enhancing hydrophobic interactions with the HDAC surface. By introducing substituents (such as halogens, methyl groups, etc.) onto the tyrosine benzene ring, the affinity with the HDAC active pocket is further optimized. The prepared compound b19 exhibits an HDAC inhibition capacity of 100%. 50 The concentration reached 26.8 nM, exhibiting superior antitumor activity compared to SAHA, especially against solid tumors such as HeLa cells with IC50. 50 It is 0.55 μM.
Owner:THE SECOND PEOPLES HOSPITAL OF SHANDONG PROVINCE (SHANDONG PROVINCIAL EAR NOSE & THROAT HOSPITAL SHANDONG PROVINCIAL INST OF EAR NOSE & THROAT)

Method for separating and purifying protein from Tianshan red deer wrinkled stomach and application

The invention discloses a method for separating and purifying protein from Tianshan red deer wrinkled stomach.The method comprises the steps that the Tianshan red deer wrinkled stomachs serve as research objects, adipose tissue and connective tissue of the fresh Tianshan red deer wrinkled stomachs are stripped, and then drying and degreasing treatment is conducted; the method comprises the following steps: extracting, freezing and thawing and centrifuging active proteins by using a freezing and thawing method, dialyzing supernate, freezing and drying to obtain crude protein powder, and purifying by using an ultrafiltration tube, HW-55F size exclusion chromatography and C8 reverse chromatography in combination with high performance liquid chromatography to finally obtain three high-purity Tianshan red deer wrinkled stomach proteins with anti-tumor activity, which are respectively named as S1, S2 and S3. The yields are respectively 1.10%, 1.11% and 0.61%, and the protein contents are 87.14% + / -2.16%, 84.65% + / -3.29% and 82.06% + / -1.25%. The IC50 of the inhibitory activity of the three proteins on HCT-116 colon cancer cells is respectively 55.89 [mu] g / mL + / -2.97, 4.44 [mu] g / mL + / -0.23 and 11.31 [mu] g / mL + / -0.75.
Owner:XINJIANG TECH INST OF PHYSICS & CHEM CHINESE ACAD OF SCI

Application of Cornu Cervi Colla in the Treatment of Zebra Fish Bone Injury

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.
Owner:SHANDONG ACAD OF CHINESE MEDICINE

Use of N-methylatanine in the preparation of fungal inhibitors

This invention provides the application of N-Methylatanine in the preparation of fungal inhibitors, belonging to the field of antifungal drug technology. The N-Methylatanine of this invention is of natural origin and has low toxicity, exhibiting IC50 activity against normal human lung epithelial cells. 50 The concentration is >40 μM; it exhibits significant antibacterial effects. At a concentration of 100 μM, its inhibition rates against *Epidermophyton floccosum*, *Trichophyton rubrum*, and *Microsporum gypseum* reached 99.385±0.8%, 102.17±1.956%, and 100±0.115%, respectively. This invention provides a new approach for the treatment of fungal infections of the skin in humans and animals.
Owner:KUNMING INST OF BOTANY CHINESE ACAD OF SCI

Cyclic peptide PT-C10 and application thereof in antitumor drugs

The invention relates to a novel cyclopeptide medicine PT-C10 with anti-tumor activity. The amino acid sequence of the novel cyclopeptide medicine PT-C10 is shown as SEQ ID NO: 1. The cyclic peptide has a good killing effect on renal cell carcinoma cells and is suitable for treating renal cell carcinoma. The invention also provides a preparation method of the cyclopeptide through microwave-promoted Fmoc protection solid-phase synthesis, and an application of the cyclopeptide in preparation of antitumor drugs. Experimental results show that the IC50 of the cyclopeptide PT-C10 to the 786-O kidney cancer cells is 42.23 mu M, and the IC50 of the cyclopeptide PT-C10 to the A498 kidney cancer cells is 15.53 mu M, so that the cyclopeptide PT-C07 can obviously reduce the cell viability of the 786-O and the A498 and shows obvious killing efficacy. The cyclic peptide PT-C10 provides a new treatment strategy for patients with renal cell carcinoma, and is expected to improve the treatment effect and the life quality of the patients.
Owner:KETONOBEI BIOMEDICAL TECH (BEIJING) CO LTD

Affinity labeling of DNA-linked ligands for high throughput ligand binding assays and the uses thereof

ActiveUS12669497B2Protein targetAffinity labeling
The present application relates to an assay method using affinity crosslinking of DNA-linked ligands to proteins to enable small molecule screening and determination of apparent affinity constants of ligands to the proteins. This method has been applied to determine 96 compounds' dissociation constants to a protein target simultaneously, and directly determine a compound's IC50 against five protein targets concurrently in crude cell lysates. Additionally, this approach was used to screen a Library of Pharmacologically Active Compounds (LOPAC) library against dihydrofolate reductase (eDHFR), enabling the discovery of a novel eDHFR inhibitor (IC50=7.9 μM). An assay kit and the method of uses are within the scope of this disclosure.
Owner:PURDUE RES FOUND

Temozolomide spherocrystal based on nano confinement crystallization regulation, method and application

The invention discloses a temozolomide spherocrystal based on nano confinement crystallization regulation and a method and application thereof. The preparation method of the temozolomide spherocrystal based on nano confinement crystallization regulation and control comprises the following steps: dissolving glycyrrhizic acid and temozolomide in pure water under an ultrasonic condition, adjusting the pH value to 3-4, heating until the solution is clear, and cooling to 0-5 DEG C under a stirring condition to obtain the temozolomide spherocrystal based on nano confinement crystallization regulation and control. Compared with the temozolomide raw material I crystal form, the temozolomide spherocrystal disclosed by the invention shows excellent nasal administration characteristics, including uniform particle size, high sphericity and excellent fluidity. Cell experiments show high cytotoxicity (IC50 = 51.9 [mu] g mL <-1 >) to glioblastoma, and in vivo experiments prove efficient brain targeting ability of the polypeptide. The preparation method has the characteristics of mild preparation conditions, easiness in process control, good reproducibility, high brain targeting property and the like, and is suitable for treating cancers delivered into the brain through the nose.
Owner:GUANGDONG UNIV OF PETROCHEMICAL TECH +2

Antiviral polypeptide and application thereof

The invention discloses an antiviral polypeptide and application thereof. The amino acid sequence of the polypeptide is shown as SEQ ID NO: 1 or 2. The invention discovers that the antiviral polypeptide shows remarkable broad-spectrum inhibitory activity on DNA (deoxyribonucleic acid) virus (HSV-1), RNA (ribonucleic acid) virus (H1N1) and enveloped virus (VSV), and the inhibition rates of the antiviral polypeptide on the DNA virus (HSV-1), the RNA virus (H1N1) and the enveloped virus (VSV) respectively reach 50.54%-75.18%, 73.06%-96.30% and 64.78%-98.68% under the concentration of 10 mu M. Meanwhile, the polypeptide has excellent safety, the half toxicity concentration in each cell line is higher than 50 mu M, and the cell survival rate under the effective antiviral concentration exceeds 90%. The invention effectively overcomes the technical defects of narrow spectrum, easy generation of drug resistance and insufficient safety of the existing antiviral drug, and provides an important candidate molecule for developing a new generation of antiviral drugs.
Owner:GUANGZHOU NAT LAB

Small-molecule inhibitor CTP13 targeting SLC25A1 and application of small-molecule inhibitor CTP13

The invention belongs to the field of molecular targeted therapy, and discloses a small-molecule inhibitor CTPI3 of a targeted mitochondrial citric acid transporter SLC25A1 and application of the small-molecule inhibitor CTPI3 in tumor therapy. On the basis of an existing inhibitor CTPI2 structure, molecular design is carried out through an induced fit docking (IFD) module of Schrdinger software, and CTPI3 is obtained. Experiments show that the median inhibitory concentration (IC50) of CTPI3 on acute myelogenous leukemia (AML) cell lines (such as Kasumi-1 and THP1) and primary AML cells is obviously lower than that of CTPI2, the synergistic effect of CTPI3 and Venetoclax is enhanced, the mitochondrial ATP yield is reduced, and the TCA cycle metabolite level is affected. Animal experiments prove that CTPI3 can significantly prolong the lifetime of AML model mice and reduce leukemia load (spleen weight is reduced, and bone marrow and peripheral blood GFPcells are reduced), and has no significant toxicity (liver, kidney and brain histopathology is normal). The invention provides an efficient and safe new candidate drug for SLC25A1 targeted therapy.
Owner:THE FIRST HOSPITAL OF CHINA MEDICIAL UNIV

Gp130-loaded engineered extracellular vesicle and application thereof

The invention discloses a gp130-loaded engineered extracellular vesicle and application thereof, belongs to the technical field of biological medicines, and relates to a medicine, which comprises a scaffold protein EN144 membrane externally hung gp130 protein-loaded engineered extracellular vesicle, the scaffold protein EN144 membrane externally hung gp130 protein-loaded engineered extracellular vesicle, and the gp130 protein-loaded engineered extracellular vesicle. The sequence of the scaffold protein EN144 is SEQ ID NO: 1; according to the present invention, the EN144-EVhgp130 provides the anti-inflammatory effect in a variety of diseases; the consistency of in-vivo and in-vitro research results shows that the EN144-EVhgp130 and the EN144-EVmgp130 can be used for effectively inhibiting the generation of sepsis inflammatory factors on RNA (Ribonucleic Acid) and protein levels; compared with a clinically approved drug TCZ, the EN144-EVhgp130 shows a higher survival rate and more remarkable inflammation improvement in a sepsis mouse model, and the IC50 of the EN144-EVhgp130 is lower than that of the TCZ.
Owner:NANJING EVLIXIR BIOTECH INC

Pharmaceutical application of a targeting CD36 inhibitor

The present invention discloses a pharmaceutical application of a CD36 inhibitor. Based on the CD36 protein structure, through the Virtual Flow virtual drug screening platform, the top 100 small molecules are screened from the drug target library for actual screening to screen for active small molecules that inhibit the function of the CD36 protein, and the effectiveness of the active small molecules of CD36 is characterized by inhibiting the oxLDL uptake level. Six potential active compounds including F449-4678 are screened out from the active small molecules. Through MST small molecule and protein binding affinity test, Dil-oxLDL flow cytometry is used to detect the IC50 of the small molecule inhibitor, and CCK-8 is used to detect cell proliferation; in addition, it is verified on LLC-LUC xenograft tumor mice that when the active small molecule is administered to the mice, it can effectively inhibit the growth of tumors, thereby achieving an anti-tumor effect.
Owner:CHINA PHARM UNIV

A small molecule peptide with antioxidant activity, FDRIW, and its applications.

This invention discloses a small molecule peptide, FDR1W, with antioxidant activity and its applications, belonging to the field of enzymatic hydrolysis processing technology. The amino acid sequence of the FDR1W is shown in SEQ ID NO.1. The FDR1W is used in the preparation of health products with antioxidant activity and in the preparation of drugs with inhibitory oxidative stress effects. This invention screened and obtained a small molecule peptide with high scavenging activity against DPPH free radicals, IC50. 50 =3.63 mg / ml, which has the potential to be used as an antioxidant functional product.
Owner:OCEAN UNIV OF CHINA +1

Anti-ochratoxin A antibody and application thereof

The invention discloses an antibody for resisting ochratoxin A and application of the antibody. According to the invention, an artificial antigen obtained by coupling the ochratoxin A and a carrier protein is used as an immunogen to prepare the monoclonal antibody against the ochratoxin A. The ochratoxin A can be sensitively and specifically detected by using the monoclonal antibody, and the lowest limit of detection (LOD) of the monoclonal antibody is 0.18 ng / mL. In addition, the half inhibition (IC50) of icELISA (Enzyme-Linked Immunosorbent Assay), which is established by utilizing the monoclonal antibody for resisting the ochratoxin A, on the ochratoxin A is 1.42 ng / mL, and the linear range is 0.34 ng / mL to 5.40 ng / mL. The invention provides the antibody capable of being used for detecting the ochratoxin A and the method for detecting the ochratoxin A, and the antibody and the method have the advantages of being simple, convenient, rapid, high in specificity, wide in linear range and high in sensitivity.
Owner:SOUTH CHINA AGRICULTURAL UNIVERSITY

Antibody specifically binding to serpentine rhzomorph and application thereof

The invention discloses an antibody specifically bound with serpentine rhzomorph and application of the antibody, and belongs to the technical field of detection. The invention provides an antibody which is simple to prepare and low in cost and detection limit. The antibody is a full-length antibody and comprises a heavy chain variable region VH and a light chain variable region VL, the amino acid sequence of the heavy chain variable region VH is as shown in SEQ ID NO.1, and the amino acid sequence of the light chain variable region is as shown in SEQ ID NO.2. When the antibody provided by the invention is used for detection, the detection limit is relatively low, and high-sensitivity detection of DAS can be realized. When the antibody provided by the invention is detected by a competitive ELISA (enzyme-linked immunosorbent assay) detection method, the IC50 is 7.61 ng / mL, and the detection limit of the antibody is 2.67-21.68 ng / mL, namely the scalar addition corresponding to the inhibition rate of 20-80%. And the crossover rate of the serpentine rhzomorph analogue is less than 1%.
Owner:JIANGNAN UNIV

Antarctic krill-derived xanthine oxidase inhibitory peptide and application thereof

This invention discloses a xanthine oxidase inhibitory peptide derived from Antarctic krill and its applications, belonging to the field of biotechnology, specifically relating to bioactive peptide technology. Using Antarctic krill protein as raw material, this invention obtains the xanthine oxidase inhibitory peptide WRIPSRL, with the amino acid sequence shown in SEQ ID NO: 1, through virtual screening, molecular docking, and in vitro activity verification techniques. This invention utilizes the BIOPEP-UWM platform for virtual hydrolysis, and obtains candidate peptides through PeptideRanker activity prediction and ToxinPred toxicity screening; then, molecular docking is performed with the xanthine oxidase crystal structure 1N5X using the Autodock Vina algorithm to screen for high-affinity peptides; in vitro activity assays show that the IC50 of the WRIPSRL peptide is high. 50 The value was 1.04 mM, and the inhibition rate reached 48.68% at a concentration of 1 mM.
Owner:OCEAN UNIV OF CHINA +1