115 results about "Hepatoma cell" patented technology

The invention relates to the field of natural products, in particular to a dimer compound of guaiane type sesquiterpenes and uric acid as well as an extraction and separation method and application of the dimer compound. According to the invention, a new dimer compound of guaiane type sesquiterpene and uric acid is extracted and separated from carpesium abrotanoides in Guizhou, and it is found that the dimer compound has relatively strong anti-tumor activity. The compound has strong inhibitory activity on breast cancer, prostate cancer, nasopharynx cancer, liver cancer, lung cancer, leukemia, pancreatic cancer, glioma, osteosarcoma, skin cancer, cervical cancer, ovarian cancer, kidney cancer and esophageal cancer, and provides an optional scheme for broad-spectrum anti-cancer drugs. Moreover, in human prostate cancer cells PC3, human cervical cancer cells Hela, human liver cancer cells HepG2 and human glioma cells U87 which are resistant to paclitaxel, the compound also shows strong anti-cancer activity, which indicates that the compound has the potential of treating patients resistant to paclitaxel.

The invention discloses application of chidamide in preparation of an anti-hepatoma drug synergist, and belongs to the technical field of medicines. According to the preparation for effectively improving the treatment effect of the anti-hepatoma medicine, chidamide serves as a sensitizer of the anti-tumor medicine, uptake of the anti-hepatoma medicine by hepatoma cells is promoted by up-regulating OATP1B3 protein expression in hepatoma tissue, accumulation of the medicine in the hepatoma tissue is increased, and therefore the anti-tumor effect of the medicine is improved. Combination of chidamide and the anti-liver cancer drug can synergistically enhance the toxicity of the drug to liver cancer, and the drug combination has biological safety and has great clinical application prospects.

The embodiment of the invention discloses a heavy chain variable region and a light chain variable region of an anti-GPC3 monoclonal antibody and application of the heavy chain variable region and the light chain variable region. The high-affinity anti-GPC3 sequence is obtained through screening, the binding specificity of the high-affinity anti-GPC3 sequence and the GPC3 antigen is high, and dissociation is slow. The sequence is used as an extracellular targeting domain to construct GPC3-CAR, after macrophages are transduced through lentivirus, CAR-M can specifically recognize GPC3 positive target cells, activate intracellular signal channels and remarkably improve in-vitro phagocytosis and killing activity, the hepatoma cell lysis effect is better, and technical support is provided for anti-hepatoma application.

The invention discloses application of sodium cantharidinate in preparation of a medicine for promoting CD3 + T cell proliferation, sodium cantharidinate acts on CD3 + T cells, proliferation of the CD3 + T cells can be promoted, human immunity can be effectively improved, and human lung cancer cells H460, human lung cancer cells A549 and human liver cancer cells HepG2 can be effectively killed.

The application relates to a synthesis method of red luminescent carbon dots with a targeting diagnosis and treatment potential of hepatocellular carcinoma, which comprises the following steps: 1) adding 5-fluorouracil and indocyanine green into deionized water, uniformly mixing, and forming a uniform mixed solution; 2) heating the mixed solution obtained in the step 1) at 160-200 DEG C for 5-9 h, and cooling to room temperature; 3) filtering and dialyzing the solution obtained in the step 2), and obtaining a pure 5-FICD solution; and 4) freeze-drying the solution obtained in the step 3), and obtaining the product. The method takes anticancer drug 5-fluorouracil and photosensitizer indocyanine green as precursors, synthesizes a low-toxicity red light carbon dot through a simple hydrothermal method, improves the shortcoming that a chemotherapy drug has a large side effect, and realizes the targeted killing of hepatocellular carcinoma cells.

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.

The application belongs to the technical field of biology and medicine, and discloses a PROTAC compound with a carbon chain as a connecting chain, which is developed based on a PROTAC technology, and a structural general formula of the PROTAC compound is formula 1: wherein R is -(CH2) n -, and n is 3-8. The synthesized PROTAC compound is a new compound, has a TG content reducing activity in a high-fat model established by L02 and HepG2, and has a low-toxicity activity in human hepatoma cells HepG2, human normal liver cells L02 and human umbilical vein endothelial cells HUVEC compared with a warhead. The synthesized PROTAC compound is a new type of anti-non-alcoholic fatty liver disease drug with low toxicity and high efficiency. The application of the PROTAC technology is widened while developing an efficient treatment of anti-non-alcoholic fatty liver disease.

The invention relates to the technical field of medicines, in particular to an enantiomer-atesane type diterpenoid compound as well as a preparation method and an application of the enantiomer-atesane type diterpenoid compound. The enantiomer-atesane diterpenoid compound disclosed by the invention is derived from plants, has anti-tumor activity, has cytotoxicity to human leukemia cells, human liver cancer cells and human cervical cancer cells, and is relatively good in inhibitory activity. Wherein the compound 3 has the best effect, the IC50 values of the compound 3 to three human tumor cells are 7.5 + / -1.2 micromole per liter, 9.8 + / -1.0 micromole per liter and 10.1 + / -0.9 micromole per liter respectively, and the activity of the compound 3 is equivalent to that of a positive control drug mitomycin. Particularly, the compound 3 also has good cytotoxicity to drug-resistant liver cancer cells (Huh7-LR cells), and the IC50 value of the compound 3 is 9.6 + / -1.1 micromole per liter. The compound 3 shows huge potential as a lead compound by virtue of the novel chemical structure and potent cytotoxicity shown in various cell lines.

The application belongs to the technical field of biological medicine, and particularly relates to a galactosamine-doxetaxel conjugate as well as a preparation method and application thereof. First, doxetaxel and 3,3'-diseleno-dipropionic acid are used as raw materials, and after heating reaction, 3,3'-diseleno-dipropionic acid doxetaxel is obtained. Then, the obtained 3,3'-diseleno-dipropionic acid doxetaxel and galactosamine are used as raw materials, and after heating reaction, galactosamine-3,3'-diseleno-dipropionic acid doxetaxel conjugate is obtained through column chromatography separation and purification. The obtained conjugate can be specifically recognized by endogenous lectin receptors (such as asialoglycoprotein receptor ASGPR) which are highly expressed on the surface of hepatoma cells, so as to be taken up by hepatoma cells through a receptor-mediated pathway, and has application prospect in the direction of hepatoma targeted treatment.

The invention belongs to the field of biological medicine, and particularly relates to siRNA for inhibiting INHBE gene expression and a conjugate and application thereof. According to the present invention, the corresponding siRNA is designed according to the INHBE gene, and the siRNA is delivered to the liver by coupling GalNAc so as to interfere the INHBE mRNA at the liver position, such that the expression of the INHBE protein can be effectively reduced, the healthy fat storage can be promoted, and the obesity treatment effect can be further achieved. The siRNA and the siRNA conjugate provided by the invention can be used for remarkably inhibiting proliferation of human liver cancer cells Hep-G2, and have an effect on inhibiting mouse liver INHBE mRNA, so that the siRNA and the siRNA conjugate provided by the invention have a good prospect in application of obesity.

This invention discloses a method for preparing fucoidan from *Sargassum hemifolia* and its application in the preparation of anti-hepatocellular carcinoma drugs. Experimental results show that *Sargassum hemifolia* fucoidan Fb has a strong inhibitory effect on HepG2 hepatocellular carcinoma cells, significantly stronger than the inhibitory effects of *Sargassum henryi* polysaccharide Fh and *Sargassum fusiforme* polysaccharide SFPS on HepG2 hepatocellular carcinoma cells. After treatment of HepG2 hepatocellular carcinoma cells with *Sargassum hemifolia* fucoidan DF1 and DF2, apoptosis is ultimately induced through the interaction and cooperation of exogenous (death receptor pathway) and endogenous (mitochondrial pathway). *Sargassum hemifolia* fucoidan possesses strong antitumor activity and therefore can be used to prepare anti-hepatocellular carcinoma drugs.

This invention discloses a nanoparticle-based drug delivery system, MPL@ICC, its synthesis method, and its applications. The MPL@ICC system consists of hollow, porous nano-MnO2, a hydrophilic targeting complex on its surface, and an acid-responsive drug, INH-CA, and a photosensitizer loaded internally. It possesses both targeted transport and controlled release capabilities against human hepatocellular carcinoma cells (HepG2), allowing it to accumulate within these cells and achieve photodynamic therapy (PDT) and free radical-induced immune killing within the tumor. Simultaneously, it directly kills tumor cells and transforms them from non-immunogenic to immunogenic, mediating an anti-tumor immune response and achieving immunogenic cell death (ICD). This overcomes the shortcomings of ICD-induced cancer treatment strategies, which often fail to produce strong and durable therapeutic effects, and does not induce normal cell apoptosis, thus possessing controllability, effectiveness, and safety.

This invention discloses a mixed hepatocyte terahertz quantitative detection system, electronic device, and medium, comprising: a spectral preprocessing module for acquiring a mixed hepatocyte time-domain spectrum and converting it into a mixed hepatocyte terahertz frequency-domain spectrum using a fast Fourier transform; calculating the refractive index and absorption coefficient to obtain frequency-domain signals of the refractive index and absorption coefficient, and processing them using Gram angle sum field and Gram angle difference field to obtain Gram angle sum field map and Gram angle difference field map; an image feature extraction module for extracting gradient features from the Gram angle sum field map and Gram angle difference field map using gradient histograms; extracting grayscale features from the Gram angle sum field map and Gram angle difference field map using grayscale histograms; fusing the gradient features and grayscale features to obtain image features; and a hepatocyte cancer cell content quantitative detection module for inputting the image features into a pre-trained hepatocyte cancer cell content quantitative detection model to obtain the proportion of hepatocyte cancer cells.

A method for inhibiting expression of receptor tyrosine kinase EPHA2, which comprises inhibiting expression of receptor tyrosine kinase EPHA2 of tumor cells by regulating expression of a ubiquitin ligase RNF114, and the mode of regulating the ubiquitin ligase RNF114 comprises knocking down expression level of RNF114 protein by RNA interference technology, or knocking out RNF114 protein expression gene by CRISPR / Cas9 method. The present application uses biochemical and tumor molecular biology means to study ubiquitination of receptor tyrosine kinase EPHA2 regulated by ubiquitin ligase RNF114 and its role in proliferation and migration of hepatocarcinoma cells. Meanwhile, the present application effectively knocks down or knocks out expression of RNF114 in hepatocarcinoma cells by designing specific siRNA, shRNA and sgRNA, and finds that the proliferation and migration ability of hepatocarcinoma cells can be effectively inhibited.

The invention provides dimerized guaiane sesquiterpene lactone 1-25 shown in a structural formula as well as a pharmaceutical composition, a preparation method and application thereof, and belongs to the technical field of medicines. The preparation method disclosed by the invention comprises the following steps: carrying out Diels-Alder reaction / deprotection on guaiane diene and divinyl ketone, so as to obtain the dimerization guaiane sesquiterpene lactone 1 to 25. The dimerized guaiane sesquiterpene lactone has inhibitory activity on human hepatoma cell lines HepG2, Huh7 and SK-Hep-1, and the compound 17 can significantly inhibit growth of transplanted tumors in nude mice, can form a pharmaceutical composition with a pharmaceutically acceptable carrier, and can be used for preparing anti-hepatoma drugs.

The application belongs to the technical field of molecular biology and drug screening, and provides a method for screening phenylhydrazine sulfate based on a key binding amino acid site of SOCS5-CP and application thereof, which comprises the following steps: key amino acid sites of SOCS5-CP binding are screened through alanine virtual point mutation, and a binding pocket is determined; a ligand molecule is used to perform virtual screening by taking the binding pocket as a docking area, and a compound with the best binding energy is obtained; the obtained drug is screened through AMDET; the selected compound is used for subsequent in-vitro cell experiments, and further screening is performed; the application uses the method of molecular docking and virtual screening in combination with in-vitro experiments for screening, and finds that phenylhydrazine sulfate can be stably combined at the key amino acid sites of SOCS5-CP, in-vitro experiments show that phenylhydrazine sulfate can effectively inhibit the binding of SOCS5-CP, and further down-regulate the protein expression level of HIF1a in hepatoma cells, and also has a significant inhibitory effect on the invasion and migration ability of primary hepatocellular carcinoma.

This invention provides seven guaiacol-type sesquiterpene dimers of structural formula (I), artemisinin dimers A-G (compounds 1-7), their preparation methods, pharmaceutical compositions thereof, and their applications, belonging to the field of pharmaceutical technology. These compounds exhibit inhibitory activity against human liver cancer cell lines HepG2, Huh7, and SK-Hep-1, and can be combined with pharmaceutically acceptable carriers to form pharmaceutical compositions, enabling the preparation of anti-liver cancer drugs.

The invention relates to a synthesis method of a benzoyl hydrazone derivative and an antitumor activity research of the benzoyl hydrazone derivative. A series of benzoyl hydrazone derivatives are synthesized by modifying benzamide and hydrazone. The synthesis method is simple, convenient and efficient, and has better selectivity and yield. In-vitro cell experiments show that the synthesized derivatives have remarkable anti-tumor activity, and especially in the aspect of inhibiting the growth of U87 (human brain astroblastoma cells), SGC-7901 (human gastric cancer cells) and HepG2 (human liver cancer cells), part of the derivatives show a low nanomole-level IC50 value. Researches show that the benzoyl hydrazone derivatives may play an anti-tumor role by inhibiting tumor cell proliferation, inducing apoptosis and other mechanisms, and have the potential to become novel anti-tumor drugs. The synthesis method of the compound, the antitumor activity and the mechanism research of the compound provide effective thinking and basis for developing new antitumor drugs, and the compound has a wide application prospect.

The invention provides a DNA frame confinement probe, a preparation method thereof and application of the DNA frame confinement probe in drawing cell membrane interface small molecule mercaptan fluctuation. The probe comprises a framework and functional components, the functional components comprise a small molecule thiol response unit, a cell membrane targeting unit and a fluorescent unit, and the functional components are connected to the framework. The framework is of a regular tetrahedral structure and is formed by an S1-8th chain, an S2-overhang chain, an S3-overhang chain and an S4 chain through base complementary pairing and self-assembly. The small molecule thiol response unit is a fluorescent probe CyS2 and is coupled with the S1-8th chain through a copper-free click chemical reaction. The cell membrane targeting unit is formed by combining a Chol-Capture oligonucleotide chain with a complementary sequence at the tail end of a S2-overhang chain and a complementary sequence at the tail end of a S3-overhang chain. And the fluorescence unit is marked at the 3'end of the S2-overhang chain by an Alexa Fluor 488 fluorescence molecule. The DFP-C provided by the invention can specifically target a cell membrane interface, and space-time dynamic imaging of cell membrane interface small molecular biological thiol flux is realized in various liver cancer cells at subcellular spatial resolution.

The application belongs to the technical field of tumor immunotherapy, and particularly relates to a SLAMF7-GPC3 bispecific antibody-expressed biomimetic nanovesicle and a preparation method and application thereof. The SLAMF7-GPC3 bispecific antibody-expressed biomimetic nanovesicle is composed of biological cells, and the cell surface expresses the SLAMF7-GPC3 bispecific antibody. The gene sequence of the bispecific antibody is shown as SEQ ID NO. 7. The biomimetic nanovesicle can improve the half-life of the bispecific antibody, retain good tissue permeability and targeting thereof, simultaneously recognize SLAMF7 antigens on lymphocytes and GPC3 antigens on liver cancer cells, activate various immune cells by using the expression of SLAMF7 on the immune cells, has a synergistic killing ability on tumor cells expressing GPC3 target proteins, and is expected to remodel the tumor microenvironment through SLAMF7 signals, and has a good application prospect.

The invention belongs to the field of organic synthesis and metal catalysis, and discloses an indolodiazepine derivative as well as a preparation method and application thereof. The indolodiazepine derivative has a structure as shown in the specification. The preparation method of the indolodiazepine derivative comprises the following steps: mixing a substrate indole compound with unsubstituted cyclopropanol, a catalyst, an oxidizing agent and a solvent, then carrying out a heating reaction, and after the reaction is finished, purifying the obtained reaction liquid to obtain the functionalized indolodiazepine derivative. The indolodiazepine derivative disclosed by the invention has a good inhibition effect on a HepG2 human hepatoma cell line, and can provide more material basis for the development of novel anti-cancer drugs.

The application discloses an alpha-linolenic acid and metal iridium coupling compound, a preparation method and application thereof, and relates to the field of medicine, in particular to an alpha-linolenic acid and metal iridium coupling compound, which has good antitumor activity on human cervical cancer cells, human hepatoma cells and mouse breast cancer cells. The preparation method is simple and easy to operate, and the product has good antitumor activity.

This invention belongs to the field of liver cancer chips and drug evaluation, specifically disclosing a liver cancer chip based on a microporous array, its preparation method, and its applications. The liver cancer chip of this invention involves the overall design and modeling of a resin chip mold, including a concentration gradient generation module and a microporous array cell culture module. The resin mold is then printed using surface projection micro-stereolithography, and finally bonded using a template replication method and plasma treatment to obtain a complete liver cancer chip. The liver cancer chip prepared by this invention can be used for in vitro drug evaluation. Its concentration gradient generation module can stably generate multiple drug concentrations, while its downstream microporous array cell culture module can efficiently generate uniformly sized and highly active liver cancer cell spheroids, which is expected to be promoted and applied in personalized, high-throughput drug evaluation.

The invention discloses a preparation method and application of a urea triazole derivative which is simple and easy to operate, cheap and easily available in raw materials, high in reaction efficiency and good in inhibition effect on human liver cancer cells Huh-7, and belongs to the technical field of medicine synthesis. According to the key points of the technical scheme, the urea triazole derivative molecule has a structure, or R1 is hydrogen atom, fluorine, chlorine, bromine, iodine, nitryl, alkyl (such as methyl, ethyl or alkynyl) or alkoxy (such as methoxyl) and various substituent groups, R2 is phenyl derivative or benzyl derivative, and X is oxygen atom or sulfur atom. The invention designs and synthesizes a urea triazole derivative with a novel structure, and the compound has a good inhibition effect on human liver cancer cells Huh-7.

The application discloses a milk-derived small molecular peptide, which has an amino acid sequence of Phe-Gly-Gly-Leu-Met (FGGLM) and a molecular weight of 523.64 Da. The small molecular peptide has the characteristics of inhibiting the activity of pancrelipases (PL) and reducing the accumulation of triglyceride (TG) content in oleic acid-induced human hepatoma (Hepg2) cells. The small molecular peptide can be applied to the preparation of preparations for treating or assisting in treating hyperlipidemia and obese people, and has the characteristics of simple preparation, suitability for industrial production and market promotion and application.

The invention relates to the technical field of biological medicine, and particularly discloses an Rnaseh2c protein inhibitor and application thereof, and the technical key point is as follows: the inhibitor is a compound 8019-9386 and is named as Rnaseh2c-In1. The inhibitor Rnaseh2c-In1 provided by the scheme of the invention can directly inhibit proliferation of liver cancer cells (Hepa1-6), lung cancer cells (LLC), gastric cancer cells (MFC) and colorectal cancer cells (MC38), has relatively strong inhibitory activity, provides important guiding significance for research and preparation of antitumor drugs, and has a wide application prospect.

The invention relates to the field of bioengineering, in particular to a function-synergetic bionic gene editing carrier system as well as a preparation method and application thereof. The invention provides a gene editing expression box. The gene editing expression box comprises a cancer cell specific promoter, a CXCL9 gene, an sgBAG3 gene and an sgHSP70 gene. A bionic lipid carrier with protein adsorption resistance, cancer cell targeting and membrane fusion delivery is constructed, and an integrated gene editing CRISPR system capable of highly expressing CXCL9 protein factors in cancer cells and double editing tumor cell BAG3 and HSP70 genes is entrapped, so that a multifunctional synergetic bionic gene editing carrier system is constructed; according to the invention, in-vivo delivery stability of the CRISPR system, cancer cell targeting accuracy and intracellular release high efficiency are realized, liver cancer cell gene editing efficiency is improved, a T cell killing enhancement effect tumor immune microenvironment is constructed, and effective cancer resistance of the CRISPR system in a tumor environment is realized.

The invention belongs to the technical field of nano-drug systems, and particularly relates to a nano-drug system loaded with siRNA and a small molecule drug and a preparation method and application of the nano-drug system loaded with siRNA and the small molecule drug, the preparation method comprises the steps that a circular DNA template containing a siRNA molecule sequence is designed and synthesized, a long tandem repeat RNA chain containing a pre-designed siRNA molecule is synthesized through a rolling cycle transcription (RCT) reaction, and nucleic acid particles RNs are formed through self-assembly. After a small-molecule inhibitor CB839 is embedded into RNs, the nano-drug system LNPs (at) RNCPsGPC3 loading siRNA and small-molecule drugs at the same time is obtained through the steps of surface modification, biocompatible lipid membrane coating, targeted peptide modification and the like, the delivery efficiency, biosafety and compatibility of siRNA and CB839 can be greatly improved, liver cancer cells are specifically targeted, and the application prospect is wide. Dependent amino acid metabolic pathways in tumor cells are blocked, and the GCN2-eIF2alpha-ATF4 pathway axis capable of actively recovering microenvironment balance is inhibited, so that the tumor cells are killed.

The invention provides arteannuin A1A4 (artemannuins A1A4, 14), arteannuin B1B4 (artemannuins B1B4, 57), arteannuin C1C2 (artemannuins C1, C2, 8 and 9) and arteannuin DH (artemannuins DH, 1014), a pharmaceutical composition of the arteannuin A1A4, the arteannuin B1B4, the arteannuin C1C2, the arteannuins C1, C2, 8 and 9) and the arteannuin DH, and a preparation method and application of the arteannuin A1A4, the arteannuin B1B4, the arteannuin C1C2, the arteannuin C1C2, the arteannuin DH and the arteannuin DH, and belongs to the technical field of medicine. The 14 cadinane type sesquiterpene dimers shown in the structural formula (I) have an inhibiting effect on human hepatoma cell lines HepG2, Huh7 and SK-Hep-1, can form a pharmaceutical composition with a pharmaceutically acceptable carrier or excipient, and can be used for preparing anti-hepatoma drugs.