94 results about "Tumor resistance" patented technology

The invention discloses a PARP1 selective protein degradation agent and an application of the PARP1 selective protein degradation agent in tumor resistance. The degradation agent has the following structural formula. Wherein the 3-ethyl-7-((4-(pyridine-3-yl) piperazine-1-yl) methyl) quinoxaline-2 (1H)-ketone part is a PARP1 target protein ligand, and L is a connecting unit; and B is an E3 ubiquitin ligase ligand. The PARP1 selective protein degradation agent prepared by the preparation method disclosed by the invention can be used for effectively degrading PARP1 protein, inhibiting cell proliferation and inducing tumor cell apoptosis. Meanwhile, when the compound is combined with chemotherapeutic drugs, the effect of enhancing the chemotherapeutic effect is achieved, almost no physiological toxicity exists, and the compound is expected to provide an ideal way for improving treatment of various diseases caused by PARP1 excessive activation. # imgabs0 #

The invention discloses a cordycepin derivative as well as a preparation method and application thereof. The structural general formula of the cordycepin derivative is # imgabs0. The cordycepin derivative provided by the invention is structurally modified by adopting a special group, so that not only is the stability of the cordycepin derivative improved, but also the biological activities of bacteriostasis, inflammation resistance, oxidation resistance, tumor resistance and the like are remarkably improved. Besides, the cordycepin derivative provided by the invention has certain selectivity on strains, especially on certain beneficial bacteria, in the aspect of bacteriostasis, and the application range of the cordycepin derivative is expanded.

The invention provides an alkaloid compound as well as a preparation method and an application thereof in tumor resistance. The alkaloid compound provided by the invention shows a remarkable cytotoxic effect on human non-small cell lung cancer cells A549, mouse lung adenocarcinoma cells Lewis, human triple negative breast cancer cells MDA-MB-231 and mouse breast cancer cells 4T1, and can be used for preparing medicines for treating breast cancer, lung cancer and the like.

The invention discloses a glycosylated quercetin amphiphilic prodrug, a preparation method and application of the glycosylated quercetin amphiphilic prodrug. The glycosylated quercetin amphiphilic prodrug, the preparation method of the glycosylated quercetin amphiphilic prodrug and the application of the glycosylated quercetin amphiphilic prodrug are included. According to the glycosylated quercetin amphiphilic prodrug as well as the preparation method and the application thereof, the pH-sensitive glycosylated quercetin amphiphilic prodrug is obtained through parallel connection of the boric acid ester and the hydrophilic targeting sugar molecule lactobionic acid and the hydrophobic quercetin, and the pH-sensitive glycosylated quercetin amphiphilic prodrug and clinical common anti-tumor drugs are further assembled into a nano-drug; the invention aims at improving the physicochemical / pharmacological activity of quercetin and exploring the anti-tumor effect of quercetin cooperating with clinical drugs at the same time. The glycosylated quercetin amphiphilic prodrug is designed according to a drug combination principle, a formula 3 is used as a substrate, molecular quercetin is combined to obtain the glycosylated quercetin amphiphilic prodrug, and pH-sensitive borate bonds are introduced, so that drug release and tumor resistance can be controlled, the drug has certain targeting property, and the biological activity is remarkably improved.

The invention relates to the technical field of biology, in particular to application of aldolase A protein 330 amino acid modified posttranslational protein in tumor resistance and a mutant. The aldolase A protein mutant is obtained by carrying out substitution on an amino acid sequence as shown in SEQ ID No. 1; and lysine at the 330 position is substituted by arginine. Experiments prove that the aldolase A protein mutant can significantly reduce the growth speed of mouse malignant breast cancer cells 4T1 and mouse malignant black tumor cells B16-F10 under the skin of a mouse, and shows excellent antitumor activity. A brand-new tumor treatment method is created, and the technical blank in the field is filled.

The invention discloses a flos magnoliae chloroform part extract, a preparation method thereof and application of the flos magnoliae chloroform part extract in resisting tumors and reversing tumor drug resistance. According to the method disclosed by the invention, the magnolia flower methanol extract, especially the chloroform extract thereof, is efficiently extracted by adopting operation means of extracting and separating natural products such as solvent extraction and extraction, and experiments prove that the magnolia flower chloroform extract has the activity of inhibiting the growth of tumor cells in vitro, so that the magnolia flower chloroform extract has the anti-tumor activity. Meanwhile, the chloroform part of flos magnoliae also can inhibit the expression of EGFR TKI drug-resistant pathway related proteins, so that the tumor drug resistance can be reversed. According to the invention, the raw material channel of the anti-tumor medicine is expanded, the application of the magnolia flower is expanded, the magnolia flower is developed into a new raw material of the anti-tumor medicine, and the medicinal value of the magnolia flower can be obviously improved.

The invention discloses a radix asparagi extract and an application thereof in tumor resistance, and belongs to the field of biological medicine, radix asparagi is heated and extracted with ethanol with the concentration of 60% to obtain an alcohol extract, then the alcohol extract is added into macroporous resin, then elution is performed with ethanol with the concentration of 30% and ethanol with the concentration of 60% in sequence, ethanol eluate with the concentration of 60% is collected, and concentration and drying are performed to obtain the radix asparagi extract. The radix asparagi extract disclosed by the invention has a relatively good inhibition effect on various cancer cells.

The invention discloses a preparation method and application of gold-modified cerium oxide drug-loaded nanoparticles, and the preparation method comprises the following steps: dispersing soluble cerium salt in an ethylene glycol solution of a template agent, adjusting the pH value to 5-7, then carrying out a hydrothermal reaction to obtain cerium oxide nanoparticles, then dispersing the cerium oxide nanoparticles in ultrapure water, and carrying out ultrasonic treatment to obtain the gold-modified cerium oxide drug-loaded nanoparticles. And adding gold tetrachlorate into the dispersion system, adjusting the pH value to 7-11 to obtain gold-modified cerium oxide nano-microspheres, and loading chemotherapeutic drugs to obtain the gold-modified cerium oxide drug-loaded nano-microspheres. The obtained gold-modified cerium oxide drug-loaded nano-microspheres have the advantages of multiple enzyme activities, good biocompatibility, excellent antibacterial performance and excellent photo-thermal performance, can relieve an anoxic environment in tumor treatment, consume GSH, overcome tumor drug resistance and the like, and have good application prospects in the field of tumor treatment.

The invention relates to a preparation method for producing a polyketone compound by using a recombinant strain Streptomyces coelicola A3 (2) / p15A-KOspiH3 (the preservation number is CCTCC NO: M 20241470), and also relates to an application of the polyketone compound in tumor resistance, and the structural formula of the polyketone compound is # imgabs0 #, the structural formula of the polyketone compound is as shown in the specification, the structural formula of the polyketone compound is as shown in the specification, and the structural formula of the polyketone compound is as shown in the specification. A fermentation product containing the compound can be obtained through fermentation culture of Streptomyces coelicola A3 (2) / p15A-KOspiH3, and then the compound is obtained through separation and purification of methods such as VLC normal-phase column chromatography separation, C-18 ODS reversed-phase column chromatography separation and semi-preparative HPLC. The invention aims to obtain a novel compound with an anti-tumor effect in a gene cluster of a heterologous expression actinomycete source, and the novel compound has a good application prospect.

The invention belongs to the technical field of medicine synthesis, and particularly relates to a tetravalent platinum compound as well as a preparation method and application thereof. The invention provides a tetravalent platinum compound. The tetravalent platinum compound has a structure shown as a formula a to a formula d, wherein linker is respectively connected with a Pt-containing mother nucleus and a PARP inhibitor through-O-C = O; the PARP inhibitor comprises a carboxyl-containing structure and a carboxyl-free structure; when the PARP inhibitor contains a carboxyl structure, the linker is when the PARP inhibitor does not contain the carboxyl structure, and the data of the linker as the embodiment shows that the tetravalent platinum compound provided by the invention has good anti-tumor activity and low tumor drug resistance when being used as the PARP inhibitor.

This invention relates to the application of exosomes in reversing tumor resistance to immune checkpoint (PD-1) inhibitors. A novel application of exosomes in the preparation of pharmaceutical compositions reversing tumor resistance to immune checkpoint inhibitors is disclosed. Exosomes generated from tumor cells recombinantly expressing adenylate cyclase 7 (ADCY7) can significantly reverse tumor resistance to PD-1 inhibitors, and the exosomes exhibit a synergistic effect with the PD-1 inhibitors.

The invention relates to the technical field of medical chemistry and tumor treatment, in particular to application of a novel NOX4 inhibitor ZZU026 and derivatives thereof in tumor resistance and immune response change. The preparation method of the ZZU026 comprises the following steps: replacing N, N-dimethylamino on a benzene ring of GKT137831 with morpholinyl; methoxyl is introduced into the core skeleton. The ZZU026 has a remarkable inhibiting effect on NOX4, has the functions of inhibiting tumor growth, new vascularization and immune-related diseases, regulating and controlling polarization of macrophages and the like, and can inhibit phenotype transformation of macrophages from M1 to M2 and finally inhibit proliferation and immune escape of lung cancer cells; the ZZU026 and the derivatives thereof can be prepared into drugs, health care products, tablets, particles, capsules, oral liquid or injection, and can be used for treating lung cancer and other tumors.

The invention belongs to the technical field of cancer immunotherapy, and particularly relates to iterative radiation-resistant tumor cell debris, a preparation method thereof and an application thereof in tumor resistance. The anti-radiation tumor cells generated by repeated radiation exposure show higher TMB (Tetramethylbenzidine) and induce stronger immunoreaction, so that a personalized vaccine is developed based on the method, and the frozen fragment vaccine is obtained by freeze thawing and inactivation of the radiation-resistant tumor cells. The RR-FDV exhibits enhanced immunogenicity as compared to a conventional radiosensitive counterpart. In the present disclosure, RR-FDV exhibits superior activation of antigen presenting cells, while in vivo, it recruits more dendritic cells to the vaccination site, promotes DC-mediated antigen presentation, and induces stronger antigen-specific T cell toxicity.

The invention discloses an application of an ARRB1 inhibitor in preparation of a tumor drug resistance reversal agent or a tumor drug sensitizer. It is found that by reducing ARRB1 expression, the sensitivity of human breast cancer cells to etoposide can be improved, the drug resistance of breast cancer etoposide can be reversed, and an ARRB1 inhibitor can be combined with an anti-tumor drug etoposide for use to improve the treatment effect. The invention provides a new direction for research and development of drugs for overcoming breast cancer treatment drug resistance, and has important clinical application value and development value.

The invention relates to the field of biological medicines, in particular to application of an MAGEB16 regulator in preparation of products for treating autoimmune diseases or resisting tumors. The invention provides an application of an MAGEB16 regulator in preparation of a product for treating autoimmune diseases or resisting tumors. The invention also provides an antibody combined with the surface of a tumor cell or an antigen binding fragment thereof. The application finds that the MAGEB16 protein can be expressed on the surface of a tumor cell, so that the technical scheme of directly targeting the MAGEB16 on the surface of the tumor cell through an antibody or a nucleic acid molecule and a series of technical schemes of targeting the MAGEB16 on the surface of the tumor cell become feasible technical schemes, and a new technical scheme is provided for efficient tumor resistance.

The invention provides a tumor targeted nano drug delivery system and a preparation method and application thereof, the tumor targeted nano drug delivery system comprises a PD-L1 monoclonal antibody, radix pseudostellariae cyclic peptide B and an mPEG-PLGA-NH2 nano carrier, the radix pseudostellariae cyclic peptide B is encapsulated in the mPEG-PLGA-NH2 nano carrier, and the outer surface of the mPEG-PLGA-NH2 nano carrier is modified with the PD-L1 monoclonal antibody. The tumor-targeted nano drug delivery system has good anti-cancer activity and biocompatibility, has longer circulation time and higher bioavailability, is obviously superior to free drugs in the aspects of tumor resistance and immunoregulation, and is expected to be applied to preparation of tumor-targeted drugs, especially gastric cancer-targeted drugs.

The present application relates to the application of a glyceroglycolipid compound Gingerglycolipid B in the field of biochemical application technology in the preparation of a tumor resistance reversal agent or a tumor drug sensitizer. The structure of the glyceroglycolipid compound Gingerglycolipid B is shown as follows: #imgabs0# The drug resistance or tumor drug is doxorubicin. Studies have shown that the compound has the ability to reverse MCF-7 / ADR activity when used in combination with doxorubicin at concentrations of 5, 10, and 20 μg / mL, respectively.

The invention relates to construction and application of nanoparticles taking black rice-derived beta glucan as a carrier. The construction comprises the following steps: 1) extracting black rice polysaccharide; 2) purifying black rice polysaccharide; 3) folic acid modification; and (4) preparing the nano-particles. The black rice-derived polysaccharide prepared by the construction method has few branches, the black rice-derived few-branch beta-glucan is applied to the field of drug delivery for the first time, and the modified beta-glucan is used for carrying antitumor drugs, so that a drug carrying system has dual effects of tumor resistance and tumor immunotherapy and a targeting effect at the same time.

The invention provides an antibody and an application thereof in tumor resistance. Provided are a single-domain antibody or an antigen-binding fragment thereof capable of specifically binding 4-1BB, and a multispecific antibody, the antibody having improved antitumor activity and lower hepatotoxicity.

The invention relates to wild phellinus igniarius SH-27 fermentation liquor rich in polyphenol and application of the wild phellinus igniarius SH-27 fermentation liquor, and belongs to the technical field of biological fermentation. The screened wild phellinus igniarius SH-27 contains rich active ingredients, the polyphenol content of mycelium pellets subjected to liquid culture of the wild phellinus igniarius SH-27 is 29.74 mg / g, the triterpene content is 3.52 mg / g, the polysaccharide content is 88.61 mg / g, the flavone content is 5.14 mg / g, and the average yield of polyphenol metabolites in fermentation liquor reaches 33.72 mg / L. By optimizing a liquid culture medium, the polyphenol content of the mycelium pellets can reach 46.98 mg / g, and the yield of the polyphenol metabolites in the fermentation liquor can reach 46.98 mg / g. A metabolite of the compound has huge medicinal potential in the aspects of treatment and intervention of oxidation resistance, inflammation resistance, cancer resistance, tumor resistance, diabetes and hypertension and the like. According to the method, the yield of the phellinus igniarius polyphenol metabolites is improved through optimization of a PSO-BP neural network model, and the average yield reaches 33.72 mg / L and is improved by 33.5% compared with fermentation liquor obtained under the single-factor experiment condition.

The invention discloses a synthesis method of a 2-aryl quinazoline compound. The quinazoline compound has wide biological characteristics including tumor resistance, cancer resistance, microbe resistance, bacteria resistance, virus resistance, inflammation resistance, tuberculosis resistance and obesity resistance. The previous improvement of synthesis of quinazoline is generally started from the change of catalyst types, reaction conditions and raw material types, but most synthesis routes rarely involve a series reaction of five-membered ring opening and ring closing, so that on the basis, the invention develops a method for synthesizing quinazoline by using anammoic anhydride and benzylamine as raw materials. The quinazoline compound is synthesized by a one-pot method through a tandem cyclization reaction under an alkaline condition. The synthesis method comprises the following steps: taking ammine anhydride and a benzylamine compound as substrates, and carrying out a synthesis reaction in the presence of a solvent dimethyl sulfoxide. The method has the advantages of simple reaction operation, mild conditions, low cost and the like.

The invention discloses a method for preparing aromatic benzene propargyl ketone through light induction and biological application, and belongs to the technical field of organic synthesis and biological medicine. Aromatic benzene propargyl alcohol is converted into the aromatic benzene propargyl ketone under the light induction condition; functional groups are changed before and after light induction, hydroxyalkyne without reaction activity is converted into carbonyl alkyne with click reaction activity, fluorescence enhancement can be achieved, and the method can be used for imaging and tracing; in addition, the aromatic benzene propargyl ketone can react with amino-containing compounds or biological macromolecules, so that the killing of tumor cells is realized. According to the method, light is used as a starting switch, reaction conditions are simple, controllability is good, no additional catalyst is needed, large-scale production is easy, and the method has wide application prospects in the aspects of polypeptide or protein marking, tumor resistance and the like.

The invention belongs to the field of medicines, and particularly discloses a pharmacodynamic active phenol chemical modified cis-platinum material which is at least one compound with a structural general formula 1, namely imgabs0 #. The invention also discloses preparation and application of the material. The method provided by the invention can effectively reduce toxicity and can synergistically improve the drug effect performance.

The invention discloses a preparation method and application of composite freeze-dried powder based on inonotus obliquus, and relates to the technical field of biological product preparation. The invention aims to solve the problems that the extraction efficiency and the extraction rate of effective components in inonotus obliquus are low, the stability and the activity of the effective components are difficult to maintain, and the provision condition is harsh due to low solubility of schisandra chinensis. According to the inonotus obliquus composite freeze-dried powder prepared by compounding the fructus schisandrae chinensis extract and the amomum tsao-ko alcohol extract by adopting the process disclosed by the invention, the content of crude polysaccharide is increased by 27.67%, the content of inonotus obliquus polysaccharide is increased by 23.2%, the content of beta-glucan is increased by 14.28%, the content of triterpenoids is increased by 26.2%, the content of schizandrin is increased by 40%, and the content of fructus schizandrin is increased by 20%. The compound has the potential of being used for preparing drugs with high curative effects, such as tumor resistance, blood sugar reduction, blood pressure reduction, virus resistance and aging resistance. The invention can obtain the preparation method and the application of the inonotus obliquus-based composite freeze-dried powder.

The invention belongs to the technical field of biological medicines, and particularly relates to a tumor microenvironment response type nano-drug based on linear-dendritic polymers. The preparation method comprises the following steps: connecting a dendritic fragment to a polymer skeleton through an enzyme-cleavable peptide chain, and coupling a chemotherapeutic drug to a dendritic periphery through a pH-unstable hydrazone bond to obtain an amphiphilic polymer prodrug; the stable nanoparticles are obtained by screening polymeric monomers, can be efficiently taken by tumor cells, and have advantages in tumor tissue penetration and tumor resistance; the polymer prodrug can also load an adenosine receptor antagonist drug to prepare a nano-drug, and the nano-drug reverses adenosine-mediated immunosuppression to realize a synergistic effect of the adenosine receptor antagonist drug and a chemotherapeutic drug; the nano-drug and the PD-1 antibody cooperate to further improve the immune response in vivo and the anti-TNBC effect. The polymer prodrug and nano-drug synthesized by the invention have good prospects in the aspect of treating TNBC.

The invention belongs to the field of medicines, and particularly relates to an antibody drug conjugate, and a pharmaceutical composition and application thereof. Specifically, the invention provides an antibody drug conjugate as shown in formula (I), a drug-linker for preparing the antibody drug conjugate, and an application of the antibody drug conjugate in tumor resistance. # imgabs0 #

The invention discloses a recombinant fusion protein and application thereof in preparation of anti-gastric cancer angiogenesis medicines, and relates to the technical field of biological medicines. The amino acid sequence of the recombinant fusion protein is as shown in SEQ ID NO. 1. According to the invention, the amino acid sequence of the gastric cancer vascular targeting peptide CNTGSPYEC and the potent vascular inhibitor Endostatin gene are recombined to construct the recombinant fusion protein, and the selective distribution capability of the targeting peptide is utilized to carry the anti-vascular drug Endostatin to be more specifically enriched in gastric cancer vascular endothelial cells, so that the anti-vascular effect and the anti-tumor effect are improved, and the tumor resistance of the gastric cancer vascular targeting peptide CNTGSPYEC is improved. Meanwhile, due to the fact that distribution of Endostatin in normal blood vessels and tissues is reduced, corresponding toxic and side effects can be reduced, and great significance is achieved for improving the current situation of gastric cancer anti-blood-vessel treatment.

The invention relates to a toadstool bifunctional glycopeptide for targeted immunoregulation and tumor resistance, and belongs to the technical field of biology. The molecular sequence of the morchella glycopeptide provided by the invention is LPS (Fuc) PMLLPQ, and the morchella glycopeptide molecule is obtained by connecting fucose to serine hydroxyl of a peptide chain through an alpha-glucosidic bond in an O-connection glycosylation mode. The morchella glycopeptide is identified from a morchella extract obtained by extracting morchella with pectinase by taking morchella as a substrate, is derived from edible mushrooms and is safe to use; the compound can be effectively combined with TLR4 (Toll-like receptor 4), block inflammatory response and effectively combine and inhibit VEGFR2 (vascular endothelial growth factor receptor-2), and has anti-tumor activity; meanwhile, release of LPS-induced macrophage cytokines can be inhibited, and it is further shown that the morchella glycopeptide has immunoregulation and anti-tumor activity.

The invention relates to the technical field of liqueur, in particular to liqueur and a preparation method thereof.The liqueur is prepared by soaking various medicinal and edible raw materials such as kudzuvine roots, rice, barbary wolfberry fruits, smoked plums, grapes, mulberries, poria cocos, Chinese yams, rhizoma polygonati, jujubes and ginseng in baijiu base liquor according to a specific proportion. According to the present invention, the modern analysis technology shows that the wine contains 25 active components such as resveratrol, protocatechuic acid, oleanolic acid, quercetin, kaempferol and the like, and the components achieve the synergistic effect, such that the product has effects of tumor resistance, liver protection, blood sugar reduction, blood fat reduction, oxidation resistance, inflammation resistance, nerve protection and other health-care functions, and the product has characteristics of definite component, synergistic effect, high safety, and no toxic-side effect. The preparation process is stable and controllable, and is suitable for large-scale production.

The invention relates to an antibody-drug conjugate as well as a preparation method and an application thereof in tumor resistance, in particular to an anti-HER3 antibody or an antigen binding fragment thereof and an antibody-drug conjugate connected with the antibody. The antibody-drug conjugate has a structure as shown in Ab-(L-D) n, and is covalently linked with an effective load with cytotoxicity through a linker. The anti-HER3 antibody or the antigen binding fragment thereof and the antibody-drug conjugate can be used for preparing a therapeutic agent for diagnosing, preventing and treating tumor diseases.