42 results about "CARCINOMA COLON" patented technology

The application discloses application of a naphthalene nitrile derivative in preparation of an antitumor pharmaceutical composition, in particular, application of a 2-(imino)-naphthalene nitrile derivative in preparation of an antitumor pharmaceutical composition. The 2-(imino)-naphthalene nitrile derivative provided by the application has a significant inhibiting effect on colon cancer, liver cancer, lung cancer, prostate cancer, cervical cancer, neuroglioma and breast cancer, exhibits excellent antitumor characteristics, can be used as a leading drug molecule for resisting tumors, and has a good development and application prospect in development of antitumor drugs.

The present disclosure is concerned with compounds and compositions for use in the prevention and treatment of cancer associated with FBOX21 mediated p85a ubiquitination such as, for example, cancer (e.g., sarcoma, a carcinoma, a hematological cancer, a solid tumor, breast cancer, cervical cancer, gastrointestinal cancer, colorectal cancer, brain cancer, skin cancer, prostate cancer, ovarian cancer, thyroid cancer, testicular cancer, pancreatic cancer, liver cancer, endometrial cancer, melanoma, a glioma, leukemia, lymphoma, chronic myeloproliferative disorder, myelodysplastic syndrome, myeloproliferative neoplasm, non-small cell lung carcinoma, renal cancer, lung cancer, colon cancer, cervical cancer, and plasma cell neoplasm (myeloma)). This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

Disclosed are methods for detecting and treating cancers (such as carcinoma, leukemia, lung cancer, colon cancer, central nervous system (CNS) cancer, melanoma, ovarian cancer, renal cancer, oral cancer, prostate cancer and / or breast cancer). The method may include receiving a sample from a patient (such as a sample from a biopsy, a sample from an extracellular vesicle, or a sample from a circulating tumor cell). The method may include determining whether a LY6C protein or a phosphorylated ANXA2 protein is detected in the sample. The method may include treating a patient for cancer by targeting the LY6C protein when the LY6C protein is detected (e.g., using photoimmunotherapy (PIT) or near infrared photoimmunotherapy (NIR-PIT)). or treating a patient for cancer by targeting an ANXA2 protein (e.g, using inhibitors, decoys, etc.) when the phosphorylated ANXA2 protein is detected.

The invention provides a hedera helix extract as well as an extraction method and application thereof, and belongs to the technical field of medicinal plant extraction. According to the method, natural eutectic solvents are screened, and the interaction of the solvents is determined by adopting an infrared spectrum; on the basis of single factor investigation, a response surface method is used for modeling and optimizing an extraction process of eight active components in the hedera helix so as to improve the extraction rate, and a scanning electron microscope is used for exploring the permeation effect of a natural eutectic solvent combined with an ultrasonic-assisted extraction method on plant cells from a microscopic perspective; finally, determining that the natural eutecticevaporate solvent is combined with an ultrasonic-assisted extraction method through a cell counting kit-8 method and an active oxygen detection method to obtain the hedera helix extract which has a stronger inhibition effect on HT-29 colon cancer cells.

The invention discloses fluoroalkyl substituted azafluorene and pyridopyrimidino isoindole compounds as well as a synthesis method and application thereof, and belongs to the technical field of organic synthesis and drug discovery. The preparation method comprises the following steps: mixing a 3-alkenyl-1, 2, 4-oxadiazolone compound 1, a fluoroalkyl acetylenic ketone compound 2, a catalyst, an additive and an organic solvent, and carrying out heating reaction to prepare a fluoroalkyl substituted azafluorene compound 3 and / or a fluoroalkyl substituted pyridopyrimidino isoindole compound 4. Experimental research discovers that the compound disclosed by the invention has the activity of obviously inhibiting proliferation of Hela and HCT-116 cancer cells, so that the compound disclosed by the invention has obvious anti-cancer activity on cervical cancer and / or colon cancer, has potential medicinal value, and provides a new structural unit for drug screening.

The present invention belongs to the field of microorganisms, and specifically relates to the use of Lactobacillus rhamnosus AFY01 and a product thereof in inflammatory colon cancer. Provided is a strain of Lactobacillus rhamnosus AFY01 with the deposit number of CGMCC No. 27362. The AFY01 can effectively alleviate weight loss in mice with colon cancer and colon shortening caused by intestinal inflammation and edema, reduce the colon coefficient of mice, reduce the visceral index and reduce the occurrence of intestinal tumors in mice, alleviate intestinal inflammation, and promote intestinal tumor cell apoptosis to slow down the development of colon cancer. By means of the present invention, the strain resources are expanded, thus providing technical support for the prevention and treatment of intestinal cancers.

The application belongs to the technical fields of synthesis of compounds and pharmaceutical applications, and discloses an anti-tumor pterostilbene piperazine conjugate as well as a preparation method and application thereof. The pterostilbene, piperazine and various substituents are spliced in one molecule by using a molecular hybridization method, a novel anti-tumor pterostilbene piperazine conjugate is synthesized, and it is found through anti-tumor activity research that the anti-tumor activity of the conjugate is obviously higher than that of the two pharmacophores alone, and the conjugate has the potential to become a novel anti-tumor drug. The pterostilbene piperazine conjugate is synthesized, and it is found for the first time that the compound has good anti-tumor activity, can significantly inhibit the proliferation of various tumor cells in vitro, including hepatocarcinoma, triple-negative breast cancer, colon cancer and ovarian cancer cells, has little toxicity to normal cells, and can inhibit the migration ability of tumor cells. Therefore, the compound synthesized by the application has good anti-tumor application prospect.

The embodiment of the application discloses a kind of vein bionics microfluidic chip and its preparation and application method of simulating multi-organ interconnection.The chip includes a chip main body, and its microfluid channel system integrates at least three organ simulation units: a lung simulation chamber for culturing lung cells to simulate upstream organs that can produce systemic effects;An upstream colon cancer cell culture chamber for three-dimensional culture of colon cancer cells to simulate tumor primary lesions;And a downstream liver cell culture chamber for three-dimensional co-culture of liver cells and vascular endothelial cells to simulate the target organ of liver, and the three simulation chambers are communicated with each other by a vein bionics microfluid network, which simulates the complex blood circulation system of human body (including pulmonary circulation and systemic circulation), can realize the signal molecule transmission between organs, and simulate the invasion and metastasis process of colon cancer cells to the target organ of liver via the circulatory system after being affected by upstream lung signals.

This invention belongs to the field of pharmaceutical technology and specifically relates to the use of apigenin derivatives in the preparation of anti-tumor drugs. The structure of the apigenin derivative is shown below: wherein the groups are defined as described in the specification. The compounds of this invention effectively inhibit the proliferation of renal cancer Caki-1 cells, human gastric cancer cells SNU-5, lung cancer cells, and human colon cancer cells HCT 116 in vitro. They also exhibit good inhibitory activity against renal cancer Caki-1 cells in vivo, demonstrating promising application prospects.

The invention relates to a flavonol compound dysosmaflavonoids I as well as a preparation method and application thereof, and can effectively solve the problems of preparation of the flavonol compound and preparation of antitumor drugs, the flavonol compound is dysosmaflavonoids I extracted and separated from dysosmaflavonoids I, has a growth inhibition effect on human liver cancer cells HepG2 and human colon cancer cells SW480, and can be used for preparing antitumor drugs. And the method has good practical application value.

The invention provides a nitrogen-containing polycyclic aromatic compound as well as a preparation method and application thereof. The nitrogen-containing polycyclic aromatic compound has a structure as shown in a formula I and has excellent broad-spectrum anti-tumor activity. The compound especially shows a certain degree of inhibition rate on gastric cancer cells AGS, cervical cancer cells Hela, cervical cancer cells SiHa, lung cancer cells A549, liver cancer cells HuH-7, liver cancer cells Mahlavu, breast cancer cells MCF-7, triple negative breast cancer MDA-MA-231, colon cancer cells HCT116, esophageal squamous cell carcinoma TE-1, pancreatic ductal adenocarcinoma SUIT-2, multiple myeloma KMS-11, osteosarcoma U-2 OS, endometrial cancer HEC-151, colorectal cancer DLD-1 and the like. Therefore, the compound shown in the formula I can be used as a lead compound for research of novel broad-spectrum antitumor drugs.

The invention relates to application of dronedarone in preparation of antitumor drugs, tumors comprise human liver cancer cells HepG2, human liver cancer cells Bel-7404, human colon cancer cells HCT15, human cervical cancer cells Hela, human gastric cancer cells HGC27 and human ovarian cancer cells SKOV3, and a large number of experiments show that dronedarone can promote death of the tumor cells, inhibit growth of the tumor cells, inhibit growth of the tumor cells and inhibit growth of the tumor cells. And the composition has an anti-tumor effect, and the indication range is expanded. The compound can be used for treating and preventing cancers, and a novel medicine application is provided for treating cancers. The invention belongs to new use of old drugs, saves time cost and labor cost of many researches on safety, and is beneficial to acceleration of research and development and clinical application of anti-tumor drugs of dronedarone.

The disclosure features, inter alia, immunogenic XBP1-, CD138-, and CS1-derived peptides (and pharmaceutical compositions thereof). The peptides can be used in a variety of methods such as methods for inducing an immune response, methods for producing an antibody, and methods for treating a cancer (e.g., breast cancer, colon cancer, pancreatic cancer, a blood cancer, e.g., leukemia or a plasma cell disorder such as multiple myeloma or Waldenstrom's macroglobulinemia). The peptides (and pharmaceutical compositions comprising the peptides) can be used, e.g., in a method of treating a precancerous condition such as smoldering multiple myeloma. The peptides can also be included in MHC molecule multimer compositions and used in, e.g., methods for detecting a T cell in a population of cells.

Disclosed are methods for detecting and treating cancers (such as carcinoma, leukemia, lung cancer, colon cancer, central nervous system (CNS) cancer, melanoma, ovarian cancer, renal cancer, oral cancer, prostate cancer and / or breast cancer). The method may include receiving a sample from a patient (such as a sample from a biopsy, a sample from an extracellular vesicle, or a sample from a circulating tumor cell). The method may include determining whether a LY6C protein or a phosphorylated ANXA2 protein is detected in the sample. The method may include treating a patient for cancer by targeting the LY6C protein when the LY6C protein is detected (e.g., using photoimmunotherapy (PIT) or near infrared photoimmunotherapy (NIR-PIT)). or treating a patient for cancer by targeting an ANXA2 protein (e.g, using inhibitors, decoys, etc.) when the phosphorylated ANXA2 protein is detected.

The present invention relates to an alkyl diamine-substituted bis-aromatic heterocyclic thioether compound, a preparation thereof, and an application thereof in the preparation of drugs for treating and / or preventing tumors. The structural formula of the compound is as shown in formula (I): the compound has a clear growth-inhibitory effect on various human tumor cells, with good inhibitory activity against breast cancer, liver cancer, pancreatic cancer, kidney cancer, lung cancer, gastric cancer, glioma, ovarian cancer, prostate cancer, esophageal cancer, melanoma, nasopharyngeal carcinoma, colon cancer, cervical cancer, lymphoma, leukemia and other such tumors, wherein the effective IC50 concentration of the compound against tumor cells, such as breast cancer, pancreatic cancer, lung cancer, glioma, ovarian cancer, esophageal cancer, melanoma, colon cancer, cervical cancer, is lower than cisplatin, and experiments show that the compound has broad-spectrum anti-tumor activity. Experiments have further detected that the compound exhibits the effect of degrading PD-L1 proteins, and is a PD-L1 immunomodulator. The present invention provides a new approach for using alkyl diamine-substituted bis-aromatic heterocyclic thioether compounds in the preparation of drugs for treating and / or preventing tumors.

This invention relates to the preparation of 10-trifluoromethoxycamptothecin compounds and their use in antitumor drugs. The structural formula of these compounds is shown below. In vitro cytotoxicity screening results show that 10-trifluoromethoxycamptothecin compounds possess broad-spectrum antitumor activity, exhibiting strong inhibitory activity against human hepatocellular carcinoma cells (HepG2), human non-small cell lung cancer cells (A549), human colon cancer cells (SW480), human cholangiocarcinoma cells (QBC939), human breast cancer cells (MCF-7), human pancreatic cancer cells (PANC-1), and human pancreatic cancer cells (BxPC-3). Compounds 10-trifluoromethoxycamptothecin I and 7-ethyl-10-trifluoromethoxycamptothecin II showed strong inhibitory effects against all seven tested tumor cell lines, with IC50 values ​​exceeding 100%. 50 The concentrations were 0.913–0.0661 μM and 4.932–0.0578 μM, respectively, both significantly superior to the control drug topotecan. Among them, compounds I and II exhibited the strongest inhibitory activity against the BxPC-3 cell line, with IC50 values ​​of [missing value]. 50 The values ​​were 0.0661±0.0065μM and 0.0578±0.0043μM, respectively. Therefore, 10-trifluoromethoxycamptothecin compounds hold promise for development into a novel antitumor drug.

The invention relates to a phthalazinone compound containing an aryl malonamide structure and application of the phthalazinone compound, and belongs to the technical field of medicines, the phthalazinone compound containing the aryl malonamide structure has a structure shown in a general formula (I), and the phthalazinone compound containing the aryl malonamide structure can be pharmaceutically added with acid to form salt. Pharmacological activity screening results show that the compound has significant inhibition effects on human breast cancer cells MDA-MB-453, human lung adenocarcinoma cells A549 and human colon cancer cells HCT116, and has good prospects in development and application of antitumor drugs.

The application discloses a pterostilbene paeonol chalcone amide derivative shown in a general formula (I) or a pharmaceutically acceptable salt thereof, the compound has a good inhibiting effect on human lung cancer cell A549, human hepatoma cell HepG2, colon cancer cell HCT116 and human osteosarcoma cell U-2OS tumor cell, and shows a certain inhibiting effect on HDAC1, 2, 3, 6 and 8, and has the potential of being used as an HDAC inhibitor type antitumor drug. The method for preparing the compound has the characteristics of easy availability of raw materials, simple operation and high yield.

The invention relates to the technical field of biological medicines, and particularly discloses a drug-resistant cell line MC38-IR for immunotherapy of mouse colon cancer as well as a preparation method and application of the drug-resistant cell line MC38-IR. The cell line is preserved in the China Center for Type Culture Collection, and the preservation number is CCTCC NO: C2025358. Experimental results show that the MC38-IR cell line has a remarkable PD-1 antibody drug resistance characteristic while maintaining the in-vitro proliferation and migration capabilities of parent cells. An in-vivo experiment shows that the tumor volume of a mouse inoculated with the cell line is not obviously inhibited after PD-1 antibody treatment, the lifetime has no statistical difference compared with that of a control group, and the parent MC38 cell shows obvious treatment response. The invention solves the problem of lack of colon cancer immunotherapy drug resistance models in the prior art, provides an important tool for researching drug resistance mechanisms, screening reverse drug resistance drugs and developing combined treatment strategies, and has higher scientific research and clinical application values.

The invention relates to the technical field of natural product extraction, and discloses a preparation method of purple corn anthocyanin with the efficacy of inhibiting hela cells and Caco-2 cells of colon cancer, and the preparation method comprises the following steps: crushing purple corn cobs to prepare an acid solution; the method comprises the following steps: weighing purple corn cob powder, adding an acid solution, mixing, extracting, and drying an extracting solution to obtain a purple corn anthocyanin crude extract; and carrying out graded alcohol precipitation by using 20%, 40%, 60%, 80% and 100% ethanol solutions, and collecting 20%-40% and 80%-100% ethanol precipitation parts to obtain a target separated extract. According to the purple corn anthocyanin prepared by the preparation method disclosed by the invention, polar components with the highest activity are directionally enriched through an ethanol fractional precipitation process, and the components have a remarkable inhibition effect on the activity of in-vitro cells hela cells and Caco-2 cells of colon cancer and have a remarkable effect of inhibiting the colon cancer.

Heterocyclic compounds, their stereoisomers and their pharmaceutically acceptable salts are useful in the treatment of many types of cancers, such as cancers of the breast, prostate, pancreatic, gastric, lung, colon, rectum, esophagus cancer, duodenum, tongue, pharynx, liver, kidney, bile duct, uterine body, cervix, ovaries, urinary bladder, and skin. Other cancers to be treated include brain tumor, neurinoma, clear cell carcinoma, non-small cell lung cancer, small cell lung cancer, hemangioma, malignant lymphoma, malignant melanoma, thyroid cancer, bone tumor, vascular fibroma, glioblastoma, Neuroblastoma, sarcoma, neuroendocrine tumors, retinoblastoma, penile cancer, pediatric solid cancer, renal cell carcinoma, lymphoma, myeloma, leukemia, acute myelogenous leukemia (AML), chronic myelogenous leukemia (CML), chronic neutrophilic leukemia (CNL), chronic eosinophilic leukemia (CEL), chronic lymphocytic leukemia (CLL), acute lymphoblastic leukemia (ALL), hairy cell leukemia, cutaneous T-cell lymphoma (CTCL), multiple myeloma (MM), myeloproliferative neoplasms (MPN), Myelodysplastic syndrome (MDS), polycythemia vera (PV), essential thrombocythemia, essential thrombocytosis (ET), and myelofibrosis (MF), and also including their metastases.

The invention relates to a 7-ethyl-10-hydroxycamptothecin polymer which has a structural formula as shown in (I), R is S or S-S, m is an integer selected from 20-200, and n is an integer selected from 2-40. The 7-ethyl-10-hydroxycamptothecine SN38 is subjected to structural modification by using beta-CD-PEG, and an-S-or-S-S-ligand with a redox function is used as a connecting arm to prepare the amphiphilic polymer-drug conjugate beta-CD-PEG-R-SN38, so that the water solubility and the stability of the SN38 are improved; meanwhile, the beta-CD-PEG-R-SN38 is prepared into self-assembled nanoparticles, and the self-assembled nanoparticles are high in drug loading capacity, moderate in particle size, uniform in dispersion, low in toxicity and good in biocompatibility, and show an obvious tumor growth inhibition effect in cell tumor-bearing nude mouse models of H22 liver cancer, 4T1 mouse breast cancer, SW480 colon cancer, KB oral epidermal cancer and the like.

The present application relates to a kind of preparation of new indole camptothecin derivatives and its use in antitumor, the structure of the compound general formula is shown as follows.In vitro cytotoxic activity screening results show that new indole camptothecin derivatives have broad-spectrum antitumor activity, to human hepatoma cell (HepG2), human non-small cell lung cancer cell (A549), human colon cancer cell (SW480), human intrahepatic cholangiocarcinoma cell (RBE), human breast cancer cell (MCF-7), human pancreatic cancer cell (BxPC3), human bladder cancer cell (T24), human bladder cancer cell (umuc3) show strong inhibitory activity. Among them, the antitumor activity of compound D-18 is most outstanding, and shows strong inhibition to the 8 tumor cell lines measured, IC 50 The range is 0.2585-10.69 μM, significantly better than the control drug irinotecan, and comparable to topotecan activity. Therefore, indole camptothecin derivatives are expected to be developed into a new antitumor drug.

The present invention discloses a multi-cell membrane-mediated biomimetic nano / gene delivery platform, its preparation method, and its pharmaceutical application for colon cancer targeting, belonging to the field of biomedicine. Zinc oxide nanoparticles and a miR21 antagonist are self-assembled in vitro to prepare a NPs nanocomplex. The NPs nanocomplex is then assembled with colon cancer cell membranes and macrophage membranes to construct a double-membrane-camouflaged biomimetic nano / gene delivery platform (M@NPs). This delivery platform can be used for in vivo delivery of gene drugs without the mediation of viral vectors. Based on the principles of homologous targeting mediated by tumor cell membranes and immune escape mediated by macrophage membranes, it achieves targeted delivery of nano / gene drugs for colon cancer treatment.

The application provides a camellia oleifera meal extract, an extraction method thereof and application of the camellia oleifera meal extract in preparation of an anti-colon cancer drug, and relates to the technical field of medicines.The extraction method can effectively regulate active ingredients in the camellia oleifera meal extract by performing heat treatment on the camellia oleifera meal before extraction, so that the sensitivity and inhibitory effect on colon cancer cells are improved.

The invention discloses application of an METTL14 inhibitor in preparation of a medicine for treating malignant tumors carrying DNA outside chromosomes, and belongs to the technical field of medicines. A human colon cancer cell HT29-4 containing ecDNA and an ovarian cancer cell UACC-1598-4 are selected as research objects, an METTL14 stable knock-down and overexpression cell model is constructed through a lentivirus-mediated RNA interference technology, and the knock-down and overexpression efficiency is verified through Western Blot. Kyotype analysis shows that the quantity of ecDNA is reduced by knocking down the METTL14, and the quantity of the ecDNA is increased by overexpressing the METTL14. The copy number of DHFR and EIF5A2 genes carried by ecDNA is detected through qPCR, and the result shows that the copy number is decreased after METTL14 is knocked down, and the copy number of overexpression groups is increased. EdU proliferation experiments and cell scratch experiments show that knock-down of METTL14 inhibits proliferation and migration ability of tumor cells containing ecDNA, and overexpression promotes the phenotypes. The invention provides an effective treatment means for the intractable tumor driven by the ecDNA.

The invention discloses a photoresponse self-assembly type PROTAC as well as a preparation method and application of the photoresponse self-assembly type PROTAC. A light cyclization addition reaction of 9, 10-phenanthrenequinone and electron-rich olefin is utilized to realize space-time controllable coupling of a target protein POI ligand and an E3 ligase ligand. The preparation method comprises the following steps: covalently coupling a 1, 9, 10-phenanthrenequinone molecule with an E3 ligase ligand, covalently coupling an electron-rich olefin group with a POI targeting ligand, and respectively administering. Afterwards, the optical fiber probe is inserted into a colon cancer part with a cavity, local illumination provided by the optical fiber is utilized to induce a cyclization addition reaction, complete and active PROTAC molecules are formed, specific degradation of key target protein (such as BRD4) of colon cancer is achieved, and the degradation process is dynamically monitored in real time. According to the invention, the molecular weight of PROTAC is reduced and the cell permeability of molecules of PROTAC is improved in a split delivery-in-situ assembly-dynamic monitoring mode, and meanwhile, space-time specific activation is realized by utilizing light control, and the toxicity of non-target tissues is reduced.

The invention provides a pathological slice image classification method and system based on attention enhancement dual-network dynamic weighting integration, and relates to the field of medical image processing and machine learning. The method comprises the following steps: firstly, acquiring five types of pathological section images of colonic adenocarcinoma, normal colon and the like, and dividing a data set after preprocessing and enhancing; constructing a UNet-LSCA attention network (capturing local lesion details) and a VGG network (extracting global semantic features), and training and storing an optimal weight by adopting a consistent strategy in a unified environment; then the UNet-LSCA weight is traversed through grid search, the optimal weight is screened through double indexes of the classification accuracy and the macro average F1 score, and a classification result is obtained through weighted fusion of the double-model prediction probability; and finally, the performance is verified through multi-dimensional evaluation. According to the method, local-global feature complementation is realized, the classification precision and stability are improved, and reliable technical support is provided for auxiliary diagnosis of lung / colon cancer subtypes.

The invention provides a 4-substituted phenylacetamide compound as well as a preparation method and application thereof. The structural formula of the compound is shown as a formula (I) or (II). The compound provided by the invention is a sphingosine kinase 2 (SphK2) targeting micromolecule, can effectively inhibit SphK2 enzyme activity and proliferation and migration of cancer cells such as human liver cancer (HepG2), mouse liver cancer (Hepa1-6), human colon cancer (HCT116), mouse colon cancer (MC-38), cervical cancer (MCF-7), gastric cancer (HGC-27) and the like, and has a better inhibition effect than that of a known inhibitor ABC294640; the polypeptide has the potential of being developed into a novel anti-cancer treatment drug. The synthesis steps of the compound are simple, the requirement on equipment is low, the operation is simple, the reaction yield can be greatly improved, and the production cost is further saved.

The invention discloses a BRD4 protein inhibitor as well as a preparation method and application thereof, and belongs to the technical field of medicines. The invention provides a BRD4 protein inhibitor, in particular a pyridone derivative with a novel structure, and the BRD4 protein inhibitor has BRD4 protein inhibition activity better than that of a positive drug JQ-1. Tests prove that the compound provided by the invention shows relatively high activity, and the prepared compound has good BRD4 protein inhibition activity, and particularly shows relatively good activity in resisting colon cancer cell proliferation. In addition, the invention also provides a method for preparing the BRD4 protein inhibitor, and the method has the advantages of short synthetic route, simple preparation process and easy operation, and can meet the needs of large-scale industrial production.