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111 results about "Hepg2 cells" patented technology

HepG2 is a cell line derived from the liver tissue of a patient with hepatocellular carcinoma (HCC). It is often used as a model system for HCC as well as for studies of drug metabolism and toxicity. Cultures are adherent, with epithelial morphology, and tend to grow in small aggregates that make the counting of individual cells difficult.

LYTAC molecule for targeted degradation of GPC3 as well as preparation method and application of LYTAC molecule

The invention belongs to the technical field of biological medicine, and particularly relates to an LYTAC molecule for targeted degradation of GPC3 and a preparation method and application of the LYTAC molecule. The LYTAC molecule is composed of a target TfR1 nucleic acid aptamer and a target GPC3 nucleic acid aptamer, wherein the nucleotide sequence of the targeted TfR1 nucleic acid aptamer is as shown in SEQ ID NO: 1; the nucleotide sequence of the targeted GPC3 nucleic acid aptamer is as shown in SEQ ID NO: 2. According to the present invention, the research results show that the GPC3 protein content is not affected by the single TfR1 nucleic acid aptamer or the GPC3 nucleic acid aptamer, and the LYTAC molecule can significantly reduce the GPC3 protein content on the surfaces of Hep3B and HepG2 cells. The LYTAC molecule induces GPC3 protein degradation through a lysosome way, then proliferation and migration of liver cancer cells are inhibited, liver cancer treatment is achieved, and the LYTAC molecule has wide application prospects.
Owner:CHONGQING MEDICAL UNIVERSITY

Application of liquiritin in preparation of PPAR gamma receptor partial agonist

PendingCN120860048AOrganic active ingredientsMetabolism disorderDiseaseThiazolidinedione
The invention provides an application of liquiritin in preparation of a PPAR gamma receptor partial agonist. Through a structure-based high-throughput virtual screening technology, it is found that liquiritin can be used as a partial agonist of a PPAR gamma receptor, and the relative activation efficiency of liquiritin is 35.9% of that of rosiglitazone; in-vitro experiments prove that liquiritin can remarkably promote glucose uptake and consumption of HepG2 cells and does not induce adipocyte differentiation; in-vivo experiments prove that liquiritin can effectively improve the blood glucose level of an insulin resistance mouse model induced by high fat diet and reduce the level of serum proinflammatory factors. Compared with thiazolidinedione compounds, liquiritin not only can relieve and treat insulin resistance or related metabolic diseases, but also does not cause adverse reactions such as weight gain, fat accumulation and myocardial hypertrophy, provides a new candidate compound for developing safe and effective anti-diabetic drugs, and has a wide application prospect.
Owner:BEIJING INST OF HEART LUNG & BLOOD VESSEL DISEASES

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

Application of UBC9 gene overexpression preparation in preparation of medicine for treating metabolic dysfunction fatty liver disease

The research finds that the SUMOylation level of the liver in a clinical specimen and an animal model of the metabolic dysfunction fatty liver disease is obviously reduced. UBC9 is used as the only key E2 ligase for SUMOylation to regulate and control the SUMOylation level. The invention discloses application of a UBC9 gene overexpression preparation in drugs for treating or preventing metabolic dysfunction fatty liver diseases. Through overexpression of liver specificity UBC9 mediated by an AAV adeno-associated virus vector or overexpression of UBC9 in HepG2 cells by a lentiviral vector, lipid deposition of a C57 mouse liver induced by high fat diet and a cell model treated by palmitate can be remarkably improved, and reduction of the SUMOylation level of the mouse liver and the human HepG2 cells under the high fat background can be reversed. Therefore, the UBC9 gene overexpression preparation can be used for developing drugs for treating metabolic dysfunction fatty liver diseases.
Owner:THE FIRST AFFILIATED HOSPITAL OF MEDICAL COLLEGE OF XIAN JIAOTONG UNIV

A benzyl chromone compound, a preparation method and application thereof

The application provides a benzyl chromone compound and a preparation method and application thereof. The application takes dry fruit bodies of Leucangium alectorium as raw materials, carries out ethanol extraction, ethyl acetate extraction, then carries out rough separation on the ethyl acetate phase obtained by extraction with different proportions of dichloromethane-methanol solution, and then carries out elution separation with different proportions of methanol-water to obtain a novel structure benzyl chromone compound. The benzyl chromone compound provided by the application has significant in-vitro inhibition activity on HepG2 cell proliferation, and when the treatment concentration is below 160 muM, the inhibition activity on liver cancer cells is obviously better than that of cisplatin, and the benzyl chromone compound can be used for preparing drugs for treating and preventing liver cancer. Meanwhile, the raw material of the compound is rich in source, low in price, simple in preparation process and convenient for industrial application, so the discovery of the compound is expected to provide a promising treatment scheme for liver cancer patients, and has great significance for breaking through the bottleneck of liver cancer treatment.
Owner:HEBEI NORMAL UNIV

Magnetic layered double hydroxide, tumor-targeting drug-loaded nano-preparation, preparation method and application of tumor-targeting drug-loaded nano-preparation

The application belongs to the technical field of medicine preparation, and particularly relates to a magnetic layered double hydroxide, a targeted drug-loaded nano preparation, a preparation method and application of a tumor-targeted drug-loaded nano preparation. The preparation method of the magnetic layered double hydroxide provided by the application can prepare Fe3O4 nanoparticles with small particle size, and further prepare the magnetic layered double hydroxide which can be used as a water-soluble drug carrier. The magnetic layered double hydroxide is used for preparing the targeted drug-loaded nano preparation and the tumor-targeted drug-loaded nano preparation, and can be used for delivering water-soluble drugs such as 5-fluorouracil. The tumor-targeted drug-loaded nano preparation has good dispersity and can be actively targeted to HepG2 cells with high FR expression, has a good inhibitory effect on liver cancer cells, and is expected to provide a potential new treatment system for magnetic chemotherapy.
Owner:TIANJIN UNIV OF TRADITIONAL CHINESE MEDICINE

Ploroglucinol meroterpenoids Hypericmoses A and B, and preparation method and application of phloroglucinol meroterpenoids Hypericmoses A and B

The invention relates to phloroglucinol meroterpenoid compounds Hypercm A and B and a preparation method and application thereof, and belongs to the field of medical chemistry, the phloroglucinol meroterpenoid compounds Hypercm A and B are extracted and separated from Hypericum acalyx branches and leaves for the first time, and the structural formulas of the phloroglucinol meroterpenoid compounds Hypercm A and B are formula (I) and formula (II). The phloroglucinol meroterpenoids Hypericmoses A and B and pharmaceutically acceptable auxiliary materials have the advantages that the phloroglucinol meroterpenoids Hypericmoses A and B have obvious inhibition effects on HepG2 cells induced by oleic acid (OA) and have application potential in the field of lipid-lowering medicines, and the invention further relates to a pharmaceutical composition which comprises the phloroglucinol meroterpenoids Hypericmoses A and B and pharmaceutically acceptable auxiliary materials and has lipid-lowering effects.
Owner:THE KEY LAB OF CHEM FOR NATURAL PROD OF GUIZHOU PROVINCE & CHINESE ACADEMY OF SCI

An acly-targeting protac chimera with anti-mash activity, methods and uses

This invention belongs to the field of biotechnology and pharmaceutical technology, and discloses an ACLY-targeting PROTAC chimera with anti-MASH activity using a glycol chain as the linking chain. Its general structural formula is Formula 1: R is -(CH2-O-CH2). n -, n is 2-6. The PROTAC compound synthesized in this invention is a novel compound. In a high-fat model established using L02 and HepG2 cells, the synthesized PROTAC compound exhibits activity in reducing TG content. Compared with the warhead, the synthesized PROTAC compound shows low toxicity activity in human hepatocellular carcinoma cells HepG2, normal human hepatocytes L02, and human umbilical vein endothelial cells HUVEC, making it a novel, low-toxicity, and highly effective drug for treating non-alcoholic steatohepatitis (NAH). This invention expands the application areas of PROTAC technology while developing a highly effective treatment for NHA.
Owner:TIANJIN UNIV OF SCI & TECH

A eucalyptane-type sesquiterpene dimer compound, its preparation method and application

This invention discloses a eucalyptane-type sesquiterpene dimer compound, its preparation method, and its applications, belonging to the field of pharmaceutical preparation technology. The six eucalyptane-type sesquiterpene dimers (compounds 1-6) disclosed in this invention are novel compounds with defined stereostructures and optically pure composition, exhibiting varying degrees of cytotoxic activity against HepG2, Hep3B, and Huh7 cells. Using sorafenib as a positive control, compounds 1, 5, and 6 showed stronger cytotoxic activity against HepG2 cells than the positive control sorafenib, compound 5 exhibited the strongest cytotoxic activity against Hep3B cells, and compounds 1, 4, 5, and 6 showed stronger cytotoxic activity against Huh7 cells than the positive control sorafenib. Therefore, compounds 1-6 disclosed in this invention have the potential to be developed into anti-hepatocellular carcinoma drugs, showing promising application prospects, and also provide important theoretical support for the further development of Atractylodes macrocephala medicinal plant resources.
Owner:SOUTHWEST UNIV

Application of DVM nanoparticles in preparation of products for treating and / or preventing alcoholic liver diseases

The invention belongs to the technical field of biology, and discloses application of DVM nanoparticles in preparation of products for treating and / or preventing alcoholic liver diseases, the DVM nanoparticles contain gallic acid derivatives VM and dihydromyricetin; the mass ratio of the gallic acid derivative VM to the dihydromyricetin is 1: 3; in alcohol-induced HepG2 cells, the DVM nanoparticles can better reduce apoptosis of hepatocytes and generation of ROS, improve ADH activity, reduce AST and ALT activities in the cells and improve the hangover alleviating ability in mice, and have a more excellent liver protection effect compared with gallic acid and a positive drug silibinin.
Owner:KUNMING UNIV OF SCI & TECH

2, 6-di-tert-butyl pyrene-indolizine phenothiazine compound, preparation method thereof and application of compound in aspect of anti-cancer drugs

The invention belongs to the technical field of organic synthesis and medicinal chemistry, and particularly relates to a synthesis method of a novel polycyclic aromatic hydrocarbon derivate 2, 6-di-tert-butyl pyrene and indolizine phenothiazine compound and application of the compound in the aspect of anti-cancer drugs. The synthesis process is simple and convenient, conditions are mild, and the yield is ideal. Pharmacodynamic evaluation shows that the compound shows strong inhibitory activity on various human cancer cell lines, and the IC50 values are respectively cervical cancer Hela cells (0.17 mu M), lung cancer A549 cells (0.3 mu M), prostatic cancer PC-3 cells (0.42 mu M) and liver cancer HepG2 cells (10.79 mu M), which are respectively reduced by 109 times, 173 times, 35 times and 1.8 times compared with positive control drug cis-platinum. In addition to efficiently inhibiting cancer cells, the compound has low toxicity to normal cells, meets the basic requirements of excellent anti-cancer drugs, and shows important application value and potential in the field of research and development of novel anti-cancer drugs.
Owner:NANJING FORESTRY UNIV

Extraction and purification method and application of malus toringoides and malus toringoides tea polyphenol

The invention discloses an extraction and purification method and application of malus toringoides leaf and leaf tea polyphenol, and belongs to the field of separation and application of natural plant products. The method comprises the following steps: mixing malus toringoides fruit and leaf dry tea powder with ethanol according to a set material-to-liquid ratio, and carrying out ultrasonic treatment on the mixed solution to obtain a malus toringoides fruit and leaf tea polyphenol crude extract; adding the malus toringoides leaf and leaf polyphenol crude extract into a chromatographic column filled with macroporous resin, and performing elution adsorption with an ethanol solution after adsorption equilibrium is achieved; and recovering the eluent, and freeze-drying to obtain the purified malus toringoides leaf and leaf tea polyphenol extract. The malus toringoides leaf and leaf tea polyphenol extract obtained by the invention has strong free radical scavenging capacity, can effectively inhibit active oxygen of HepG2 cells, and can be used for researching, developing and preparing antioxidant functional foods and medicines.
Owner:ZHEJIANG FORESTRY UNIVERSITY

Salicornia polysaccharide, and preparation method and application thereof

The application discloses a Salicornia polysaccharide as well as a preparation method and application thereof. The Salicornia polysaccharide is composed of 11 kinds of monosaccharides, wherein arabinose (24.96%), galactose (30.39%) and galacturonic acid (23.20%) are main monosaccharides of the polysaccharide, and the relative molecular weight is 3.24*10 4 Da. The Salicornia polysaccharide has a very special surface morphological structure, and presents a regular sawtooth distribution. The anti-tumor activity of the Salicornia polysaccharide is researched, and it is found that the polysaccharide can inhibit the growth of HepG2 cells, and the molecular mechanism of the anti-tumor activity is that the polysaccharide can induce the apoptosis of HepG2 cells. The Salicornia polysaccharide has significant anti-tumor activity, can be used as a candidate drug for developing an anti-tumor drug, and has a wide development prospect.
Owner:YANCHENG INST OF TECH

Application of fer1l6 gene in prevention and treatment of diabetes

ActiveCN117205322BOxidative stressHepg2 cells
This invention belongs to the fields of biomedicine and molecular biology, specifically relating to the application of the FER1L6 gene in the prevention and treatment of diabetes. In this application, the expression of GLUT4 is increased by inhibiting the expression of FER1L6, thereby improving the related physiological metabolism in diabetic organisms. This physiological metabolism includes glucose uptake, lipid metabolism, and oxidative stress damage. Experimental results show that FER1L6 is highly expressed in type 2 diabetic mice and insulin-resistant HepG2 cells; reducing FER1L6 expression significantly increases GLUT4 expression, ultimately improving lipid metabolism and oxidative stress damage in diabetic mice, while also enhancing cellular glucose uptake. Therefore, it can be concluded that FER1L6 is a good regulatory target for the prevention and treatment of type 2 diabetes based on the GLUT4 pathway. Based on this target, new technical approaches can be provided for the prevention and control of type 2 diabetes.
Owner:HENAN UNIVERSITY

Novel chalcone compound as well as preparation method, pharmaceutical composition and application thereof

The invention specifically discloses a novel chalcone compound as well as a preparation method, a pharmaceutical composition and application thereof. Experimental results show that the compound shows remarkable anti-inflammatory activity in a lipopolysaccharide stimulated RAW 264.7 cell model, and the anti-inflammatory activity is obviously superior to that of a positive drug dexamethasone; the compound shows a remarkable lipid accumulation inhibition effect in a HepG2 cell model treated by free fatty acid, is obviously superior to a positive drug obeticholic acid, and can be used for developing drugs for treating the non-alcoholic fatty liver disease, including but not limited to simple fatty liver, non-alcoholic steatohepatitis and related liver cirrhosis.
Owner:CHINA JAPAN FRIENDSHIP HOSPITAL

Preparation method of chitosan oligosaccharide-sodium alginate-selenium nanoparticles and anti-liver cancer application of chitosan oligosaccharide-sodium alginate-selenium nanoparticles

The invention belongs to the field of functional food and biomedicine, and relates to a method for preparing polysaccharide modified selenium nanoparticles. A chitosan oligosaccharide-sodium alginate compound is used as a stabilizer, Na2SeO3 is used as a selenium source, Vc is used as a reducing agent, novel selenium nano-particles (COS-SA-SeNPs) are prepared through a chemical synthesis method, the stability of the particles is improved, and the optimal preparation method is determined by taking the particle size as an index. Investigating the physical and chemical stability; the interaction mode of the COS-SA-SeNPs is defined; the influence of the COS-SA-SeNPs on HepG2 cell growth is further researched, and an action mechanism of inducing HepG2 cell ferroptosis by the COS-SA-SeNPs is disclosed. According to the invention, the stability of SeNPs is improved by preparing COS-SA-SeNPs, the anti-hepatoma activity of the SeNPs is proved, and reference is provided for further development and utilization of the SeNPs in the fields of functional foods with anti-hepatoma effects, foods for special medicine, foods for special diets and the like.
Owner:BEIJING FORESTRY UNIVERSITY

A method for evaluating the bioavailability of soybean oil based on an in vitro digestion / cell co-culture model

ActiveCN116121328BMicrobiological testing/measurementMaterial analysisGastric digestionIn vitro digestion
This invention discloses a method for evaluating the bioavailability of soybean oil based on an in vitro digestion / cell co-culture model. Soybean oil is emulsified using WPI emulsifier and then digested sequentially through simulated gastric and intestinal fluids to obtain the gastric digestion products of soybean oil. Fatty acids are extracted from the intestinal digestion products of soybean oil, dissolved in dimethyl sulfoxide, and linked to fatty acid-free bovine serum albumin to obtain in vitro digestion products of soybean oil that can be absorbed by the intestines. These are then added to a cell co-culture model for cell incubation and transport. HepG2 cells from the cell co-culture model are collected, and Oil Red O staining and total triglyceride content are measured to obtain lipid deposition, thereby evaluating the bioavailability of soybean oil. The in vitro digestion / cell co-culture model of this invention is specifically designed for soybean oil digestion. This method objectively and scientifically evaluates the bioavailability of soybean oil at different metabolic stages, providing a standard basis for the scientific and healthy consumption of soybean oil and possessing significant practical value.
Owner:JIANGSU UNIV

A white tea composition, its extraction process and use

The application discloses a white tea composition and an extraction process and application thereof, and the composition is prepared from white tea, roxburgh rose, honeysuckle, mulberry and ginkgo leaves, wherein the white tea, roxburgh rose and honeysuckle are each 5-15 parts, and the ginkgo leaves are 2-8 parts; the extraction process is that the five medicinal materials are weighed according to the proportion, 45%-75% ethanol is added, microwave-assisted extraction is adopted, and the extract is collected, and the white tea composition can significantly inhibit H2O2-induced HepG2 cell oxidative damage, restore cell viability, effectively reduce intracellular ROS level, improve mitochondrial membrane potential, significantly enhance endogenous antioxidant enzyme activities such as SOD, GPX and GSH, and reduce the content of MDA, thereby providing theoretical support for application research and product development of the composition in the fields of health food, medicine and cosmetics, and embodying good application potential of the natural antioxidant. The optimized composition extraction process is stable and feasible, and the comprehensive antioxidant effect of the extract under the condition is significant.
Owner:THE KEY LAB OF CHEM FOR NATURAL PROD OF GUIZHOU PROVINCE & CHINESE ACADEMY OF SCI

Polypeptide with antioxidant activity and application thereof

The invention discloses a polypeptide with antioxidant activity and application thereof, and belongs to the technical field of biological medicine and fine chemical engineering. The amino acid sequence of the polypeptide is selected from QY, YG, YYYY, QPYY or WHYHDYKY. HPLC and MS structure confirmation shows that the synthesized polypeptide is high in purity and accurate in structure. In-vitro chemical experiments prove that the polypeptide (especially WHYHDYKY) has extremely high ABTS and DPPH free radical scavenging capacity, and the activity of the polypeptide is superior to or equal to that of glutathione (GSH). Cell experiments show that part of polypeptides (such as QY, YG, YYYY and QPYY) can significantly improve the survival rate of HepG2 cells under an oxidative damage model, and have a significant cell protection function. The polypeptide can be applied to the fields of antioxidant drugs, functional food, cosmetics, industrial antioxidants and the like according to the characteristics of the polypeptide.
Owner:HUNAN NORMAL UNIVERSITY

A zif-8 / pda composite material and a preparation method and application thereof

The application relates to the technical field of drug delivery, in particular to a ZIF-8 / PDA composite material and a preparation method and application thereof. The ZIF-8 / PDA composite material provided by the application has good feasibility in terms of loading and delivering curcumin. The ZIF-8 material is modified by polydopamine, and the loading effect of the ZIF-8 material as a carrier on drugs is improved. The characterization results show that the drug loading performance of ZIF-8@PDA is obviously improved. The in-vitro release experiment results show that CuR@ZIF-8@PDA has more significant pH response drug release characteristics, shows good inhibition on Staphylococcus aureus and Escherichia coli, the hemolysis rate is 3.1%, is within a safe range, the inhibition on HepG2 cells is stronger than that of CuR@ZIF-8, and more obvious oxidative stress reaction and cell apoptosis can be induced.
Owner:NORTHEAST AGRICULTURAL UNIVERSITY

Application of cepharanthine in preparation of medicine for preventing or treating fatty liver disease related to metabolic dysfunction

The invention relates to application of cepharanthine in preparation of medicines for preventing or treating metabolic dysfunction related fatty liver diseases (Metabolic-associated fatty liver diseases), and particularly relates to application of cepharanthine in preparation of medicines for preventing or treating metabolic dysfunction related fatty liver diseases (Metabolic-associated fatty liver diseases). The invention relates to an application of MASLD in a medicine, and belongs to the technical field of biological medicines. In an in-vivo experiment, a mouse MASLD model is established by adopting methionine choline deficiency diet induction, and the treatment effect of cepharanthine on MASLD is researched. Experimental results show that the cepharanthine can significantly reduce the levels of triglyceride, glutamic-pyruvic transaminase, glutamic oxalacetic transaminase and other indexes of MASLD mice; a pathological detection result shows that cepharanthine can effectively reduce liver lipid deposition and inflammatory infiltration. In-vitro experiments prove that cepharanthine can effectively reduce the content of free fatty acid (Free Fatty Acid); fFA (Fatty Acid) induced HepG2 (HepG2) cell lipid accumulation and lipopolysaccharides (lipopolysaccharides) induced HepG2 cell lipid accumulation and lipopolysaccharides (FFA) induced HepG2 cell lipid accumulation; the THP-1 cell inflammatory response is induced by LPS (Lipopolysaccharide). In conclusion, the cepharanthine shows remarkable anti-lipid accumulation and anti-inflammatory effects in in-vivo and in-vitro experiments, can be used for preparing the medicine for preventing or treating MASLD, and has a wide application prospect.
Owner:CHONGQING MEDICAL UNIVERSITY

Polypeptide with antioxidant activity and application thereof

The invention discloses a polypeptide with antioxidant activity and application thereof, and belongs to the technical field of biological medicine and fine chemical engineering. The amino acid sequence of the polypeptide is selected from QY, YG, YYYY, QPYY or WHYHDYKY. HPLC and MS structure confirmation shows that the synthesized polypeptide is high in purity and accurate in structure. In-vitro chemical experiments prove that the polypeptide (especially WHYHDYKY) has extremely high ABTS and DPPH free radical scavenging capacity, and the activity of the polypeptide is superior to or equal to that of glutathione (GSH). Cell experiments show that part of polypeptides (such as QY, YG, YYYY and QPYY) can significantly improve the survival rate of HepG2 cells under an oxidative damage model, and have a significant cell protection function. The polypeptide can be applied to the fields of antioxidant drugs, functional food, cosmetics, industrial antioxidants and the like according to the characteristics of the polypeptide.
Owner:HUNAN NORMAL UNIVERSITY

An alcoholic liver injury cell model and a construction method and application thereof

The application discloses an alcoholic liver injury cell model and a construction method and application thereof, and belongs to the technical field of cell models. The technical problem to be solved is to improve the stability and accuracy of the constructed alcoholic liver injury cell model. The technical solution is a construction method of an alcoholic liver injury cell model, which comprises the following steps: after HepG2 cells are digested, the cells are resuspended and diluted by using DMEM complete culture medium, the cell liquid obtained after dilution is inoculated into a hole plate, alcohol solution is added after a certain time, and a sealing plate film is added at the same time, and then incubation is continued, and the alcoholic liver injury cell model is obtained.
Owner:GUOZHEN HEALTH TECH (BEIJING) CO LTD

Multi-target combined toxicity screening method and system based on deep learning

The invention relates to a multi-target combined toxicity screening method and system based on deep learning, and belongs to the technical field of food safety and biology. The method comprises the following steps: carrying out combined co-incubation on HepG2 cells and to-be-detected samples with different concentration proportions, and labeling a subcellular structure by using a fluorescent probe; acquiring a multi-channel fluorescence image; performing cell segmentation on the image; extracting phenotypic characteristics of the cells; and based on a ResNet18 model, carrying out regression training on the extracted phenotypic features and the collaborative toxicity score calculated by the HSA model, and establishing a toxicity prediction model. Compared with a traditional combined toxicity screening method, on the premise that it is ensured that the combined toxicity effect prediction accuracy is close to that of a traditional experimental method, the multi-dimensional phenotypic characteristics of the cells are extracted through multi-organ dyeing, so that the combined toxicity effect is comprehensively analyzed, and a promising tool is provided for achieving combined toxicity high-throughput screening.
Owner:JIANGNAN UNIV

5-hydroxypyrazole compound as well as synthesis method and application thereof

The invention discloses a 5-hydroxypyrazole compound as well as a synthesis method and application thereof, and the structural formula of the 5-hydroxypyrazole compound is as follows: 3-phenoxyphenyl-3-oxo-methyl propionate derivative is used as a starting material, the starting material and benzyl bromide derivative are subjected to hydrocarbylation reaction firstly, then the starting material and hydrazine hydrate are subjected to Knorr reaction, and the 5-hydroxypyrazole compound is obtained. Finally, the 5-hydroxy-3-phenoxyphenyl pyrazole ring compound is prepared, and the prepared 5-hydroxypyrazole ring compound shows that the 5-hydroxypyrazole ring compound has a good inhibition effect on HepG2 cells and can be used for further preparing anti-cancer drugs.
Owner:SANQUAN COLLEGE OF XINXIANG MEDICAL COLLEGE

Preparation method and application of pleuromutilin and derivative thereof

The invention discloses a preparation method and application of pleuromutilin and derivatives thereof. The preparation of C7-site substituted, C8-site axial substituted and C8-site exocyclic double bond substituted derivatives of pleuromutilin is realized. The pleuromutilin derivative shows activity which is obviously superior to that of a parent compound pleuromutilin in the aspect of inhibiting proliferation of human cancer cells (such as breast cancer MDA-MB-231 cells and liver cancer HepG2 cells) with high expression of TrxR. Wherein the C8-position axially substituted derivative has particularly outstanding advantages in the aspect of inhibiting TrxR enzyme activity, and compared with a parent compound pleuromutilin and a positive control drug Jinnofen, the TrxR inhibiting efficacy of the C8-position axially substituted derivative is improved to 9 times and 16.7 times respectively.
Owner:SUZHOU UNIV

Striga aegyptiaca glycoside A, extraction method and application thereof

The application discloses strigasiaticaside A and an extraction method and application thereof, and finds, through chemical component research on the whole grass of striga asiatica, a new synbinaphthyl tetrahydrofuran lignan glycoside, that is, strigasiaticaside A, identifies the chemical structure of the new compound through nuclear magnetic resonance, mass spectrometry, ultraviolet, infrared and circular dichroism spectrum technology.The structure of the new compound is identified as (-) sesamin-5-O-beta-D-glucopyranoside.The anti-hepatitis activity of the new natural product is evaluated by using LPS stimulated HepG2 cells.The results show that when the concentration is 100 muM, the compound has a significant inhibitory effect on the production of inflammatory factors IL-10 and NF-kappa B protein, and has no cytotoxicity, indicating that the compound may have potential anti-hepatitis activity.
Owner:GANNAN MEDICAL UNIV

TB derivatives with photodynamic antibacterial and anti-tumor activity and synthesis method thereof

The invention provides a TB derivative with photodynamic antibacterial and anti-tumor activity and a synthesis method thereof, the derivative comprises a carbazole-TB-thiophene-pyridinium derivative, the structural formula of the derivative is shown in the specification, and the four derivatives have good viscosity response and aggregation-induced emission property and can efficiently and synchronously generate I-type and II-type active oxygen. The TB-CB-1, the TB-TPA-1 and the TB-TPA-2 have good photodynamic antibacterial activity on tested gram positive bacteria (G + bacteria), and the antibacterial rates of the TB-CB-1, the TB-TPA-1 and the TB-TPA-2 on the three kinds of G + bacteria are all larger than 90% when the concentration of the TB-CB-1, the TB-TPA-1 and the TB-TPA-2 is 2 mol. L <-1 >. The four compounds have strong photodynamic anti-tumor activity and large light and dark toxicity difference, the IC50 values of the TB-CB-1 to MCF-7, A549 and HepG2 cells are all greater than 100 [mu] g.mL <-1 > in the absence of illumination, and the IC50 values are respectively reduced to 1.53 [mu] g.mL <-1 > and 0.28 [mu] g.mL <-1 > under illumination; the IC50 of the TB-TPA-2 to A549 cells under a dark condition is greater than 200 [mu] g.mL <-1 >, and the illumination is reduced to 2.01 [mu] g.mL <-1 >. The invention provides a new thought for design and synthesis of a novel photodynamic antibacterial / antitumor photosensitizer.
Owner:XUZHOU NORMAL UNIVERSITY

Pharmaceutical composition having lipid-lowering effect

PendingCN122342756AFeruloyl quinic acidGolden hamster
The present application provides a kind of pharmaceutical composition with lipid-lowering effect, including luteolin, isorhamnetin, 9-hydroxy-4,7-megastigme-3-ketone, lotus leaf base, 3-O-feruloyl quinic acid, kaempferol-3-O-acacia disaccharide-7-O-glucoside, kaempferol-3-O-beta-D-acacia glycoside and ginsenoside Rg1.The composition of example 1 has lipid-lowering efficacy verified by golden hamster hyperlipidemia model and AML12, HepG2 cell fatty degeneration model, the regulation effect of the composition of example 1 on the key target points of AMPK signal pathway and NF-κB signal pathway is verified by using molecular pharmacology experiment, and the mechanism of the composition of example 1 in treating hyperlipidemia by regulating energy metabolism and anti-inflammatory mechanism is described.
Owner:XIAMEN UNIV

Honeysuckle flower-spirulina compound composition and preparation method thereof

The invention belongs to the technical field of food, and relates to a honeysuckle-spirulina compound composition and a preparation method thereof, which can be applied to preparation of hangover alleviating health care products, functional beverages or pharmaceutical compositions for adjuvant therapy of alcoholic liver injury. The preparation method comprises the following steps: (1) weighing honeysuckle powder, adding 15-25 times volume of distilled water into 1-10 parts of honeysuckle powder, stirring and extracting for 160-200 minutes in a water bath at 70-80 DEG C in a dark place, and carrying out solid-liquid separation to obtain a honeysuckle extracting solution; (2) weighing 5-20 parts of spirulina platensis powder, and preparing a spirulina platensis extraction solution according to the method in the step (1); (3) mixing the obtained honeysuckle flower extracting solution with the spirulina platensis extracting solution; wherein the matching effect of 5 parts of honeysuckle flower powder and 10 parts of spirulina powder is optimal. The compound composition can solve the problem that the honeysuckle water extract is unstable, the stability index (TSI) within 6 hours is obviously lower than that of a single raw material group, and the total phenol retention rate is higher after the gastrointestinal environment is simulated; the natural anti-alcoholism liver-protecting food has the advantages that the anti-alcoholism liver-protecting food has a synergistic anti-alcoholism liver-protecting effect, the survival rate of HepG2 cells damaged by alcohol is obviously increased, the activities of ethanol dehydrogenase and acetaldehyde dehydrogenase are improved, the activities of glutamic-pyruvic transaminase and glutamic oxalacetic transaminase are reduced, meanwhile, the scavenging rates of DPPH, ABTS and hydroxyl radicals are excellent, and a new direction is provided for development of natural anti-alcoholism liver-protecting food.
Owner:TIANJIN UNIV OF SCI & TECH