109 results about "Antitumor therapy" patented technology

The invention relates to the technical field of traditional Chinese medicine processing, and discloses traditional Chinese medicine processing equipment for traditional Chinese medicine anti-tumor treatment, which comprises a crushing box, the front surface of the crushing box is fixedly connected with a first motor, the output end of the first motor is provided with crushing rollers through a coupler, and the two crushing rollers are meshed with each other through a gear set; a screen is arranged in the smashing box, a suction opening of the smashing box synchronously moves along with the carding component through a suction fan and a conveying pipe, large particles which cannot pass through the screen on the screen face can be accurately and efficiently sucked up in time, and the large particles are conveyed to the top of the smashing box again through the conveying pipe and fall into the position between the two smashing rollers to be smashed again forcibly. The trouble that traditional equipment needs to be shut down to manually return materials is avoided, the materials are smashed multiple times in the single machining process, the smashing efficiency is remarkably improved, the carding plate horizontally reciprocates above the screen, large-particle materials are continuously carded, cut and smashed, and screen holes are effectively prevented from being blocked.

The invention belongs to the technical field of biomedical materials, and discloses pH-responsive injectable hydrogel as well as a preparation method and application thereof. Comprising the following steps: (1) dissolving sodium alginate in water to form a uniform solution; (2) adding a fat-soluble small molecule drug and Fe3O4 nanoparticles into the solution, carrying out high-speed shearing dispersion under an ice-water bath condition to form a drug / nano composite system, and standing; and (3) sequentially adding a calcium carbonate suspension and glucolactone into the drug / nano composite system, uniformly stirring, and incubating until the mixture is completely cured to obtain the pH-responsive injectable hydrogel. The hydrogel obtained by the invention not only has excellent injectability and pH response release performance, but also can remarkably improve the loading efficiency of fat-soluble drugs, and provides a new technical approach for realizing local anti-tumor treatment.

The invention belongs to the technical field of nano materials and anti-tumor treatment medicines, and discloses cordyceps sinensis mycelium polysaccharide-copper selenide with dual effects of inducing tumor cell apoptosis and copper death as well as a preparation method and application thereof. The preparation method of the cordyceps sinensis mycelium polysaccharide-copper selenide comprises the following steps: taking cordyceps sinensis mycelium polysaccharide as a template, adopting a soft template method, reducing Na2SeO3 through Vc, and adding CuSO4 to prepare the cordyceps sinensis mycelium polysaccharide-copper selenide. The cordyceps sinensis mycelium polysaccharide-copper selenide can selectively kill tumor cells and induce apoptosis and copper death of the tumor cells at the same time, and has huge application potential in the aspect of tumor prevention and treatment.

This application discloses a purino[1,2-a]carbazolin derivative, its preparation method, and its application. Specifically, it discloses a compound having the structure shown in Formula I, or its stereoisomers, solvates, metabolites, pharmaceutically acceptable salts, cocrystals, or prodrugs: ; wherein R1 and R2 are each independently selected from hydrogen, hydroxyl, carboxyl, substituted or unsubstituted C1-C6 alkyl, -CONH-R3, and -COO-R4; wherein R3 is a substituted or unsubstituted C1-C5 alkyl, and the substituent can be any of cyano, halogen, alkylC1-C5 alkoxy, C1-C5 alkylsulfonyl, di(C1-C5 alkyl)amino, nitrogen-containing heterocyclic, aryl, and C1-C5 heteroaryl; R4 is selected from any of substituted or unsubstituted aryl C1-C5 alkyl and nitrogen-containing saturated heterocyclic C1-C5 alkyl. This compound can be used as a TDP1 inhibitor for antitumor therapy.

This invention provides a chlorambucil NO donor prodrug having the structure shown in Formula (I) or a pharmaceutically acceptable salt thereof: Formula (I). It involves reacting chlorambucil with a dihaloalkane to obtain a halochlorambucil intermediate; reacting the halochlorambucil intermediate with silver nitrate to obtain the chlorambucil NO donor prodrug. This invention applies the chlorambucil NO donor prodrug to the preparation of drugs for treating tumors, such as melanoma, lymphoma, leukemia, or breast cancer. This nanosystem exhibits good NO release levels under light irradiation. Cellular experiments have demonstrated its good antitumor effect, providing a new strategy for multimodal combined antitumor therapy.

The invention belongs to the technical field of biological medicine, and discloses a medicine for in-vivo engineering CAR-T and a preparation method thereof. The drug provided by the invention comprises a first RNA and a second RNA which are used for coding a chimeric antigen receptor in a specific molar ratio, the second RNA is used for coding at least two cytokines of CCL19, IL-17, IL-15, IL-2 or IL-24, by adopting the drug, the gene delivery efficiency and targeting of in-vivo engineered CAR-T can be improved, better T cell transformation and CAR + T cell generation effects are realized, the CAR-T cell depletion is reduced, and the drug has a good application prospect. According to the present invention, the CAR-T gene is constructed, such that the CAR-T gene can survive for a long time in the tumor microenvironment and continuously provide the treatment effect, has the excellent anti-tumor treatment effect, has the excellent application prospect in the in-vivo engineering CAR-T treatment, and has the important significance on the promotion of the efficient, safe and economical development of the CAR-T treatment.

Tumor-selective expression of therapeutic molecules by bacteria is achieved by one or more AND, NOR, OR, NOT and / or NAND gate genetic circuits. The therapeutic molecules can be proteins, metabolites or catabolites, and may also be immunotherapeutics or immunotherapeutic cytotoxins. Single or multiple expression components may be used. Tumor selective expression of multimeric proteins utilizes multimerization as to complete the genetic circuit. Genetic circuits that are unlinked, function to achieve a combined effect on specificity of delivery of antitumor therapeutic molecules. Compositions and methods to generate silica, PEG and Poly-HPMA coated bacteria are also provided. Compositions and methods for selectively sensing or imaging tumors are also described.

The present invention relates to an EZH1 / 2 inhibitor, a preparation thereof, and a use thereof in anti-tumor therapy, specifically comprising a compound represented by formula I or formula II, or a deuterated compound, or a stereoisomer, or a pharmaceutically acceptable salt thereof, and further comprising a pharmaceutical composition of the compound, and a use of the foregoing as an EZH1 / 2 inhibitor in the preparation of medication for treating related diseases.

This invention provides a chimeric antigen receptor comprising an NFIX-encoding gene, a self-cleaving peptide sequence F2A, and a CAR-encoding sequence. The NFIX-encoding gene is located upstream and is linked to the CAR-encoding sequence via the self-cleaving peptide sequence F2A. The sequence of the NFIX-encoding gene is shown in SEQ ID NO. 01, and the sequence of the self-cleaving peptide sequence F2A is shown in SEQ ID NO. 03. This invention also provides a chimeric antigen receptor T cell expressing the aforementioned chimeric antigen receptor. This invention further provides the application of the aforementioned chimeric antigen receptor or the aforementioned chimeric antigen receptor T cell in the preparation of drugs for treating cancer. This invention improves the antitumor therapeutic effect of CAR-T cells by introducing the NFIX expression element into engineered T cells, thereby enhancing their functional stability, proliferative capacity, and cytotoxic activity under continuous antigen stimulation.

The application discloses a 2,2'-biquinoline-4,4'-dicarboxylic aliphatic amino acid derivative, and a preparation and application thereof, and belongs to the technical field of medicines.The structure of the 2,2'-biquinoline-4,4'-dicarboxylic aliphatic amino acid derivative is shown in the following formula: wherein RNH is selected from the group consisting of structures that are stable, have low toxicity, have antitumor activity, and can be used as effective components of antitumor drugs for antitumor treatment.The preparation process of the 2,2'-biquinoline-4,4'-dicarboxylic aliphatic amino acid derivative is simple, and the 2,2'-biquinoline-4,4'-dicarboxylic aliphatic amino acid derivative is easy to be industrialized when being used for preparing antitumor drugs.

The invention belongs to the cross technical field of cell engineering, nano-drugs and biological manufacturing, and particularly discloses a drug-loaded vesicle based on denucleated cells as well as a preparation method and application of the drug-loaded vesicle. According to the invention, a cell suspension and a cytoskeleton relaxant are co-incubated to relax an actin skeleton and weaken nucleoplasm connection; then loading the treated cell suspension on a multi-layer discontinuous density gradient centrifugal medium, realizing physical separation of cell nucleuses and cytoplasm through high-speed centrifugation according to buoyancy density difference, and collecting components of a specific interface to obtain high-purity denucleated cells with a complete membrane structure; then co-incubating the denucleated cells and ROS response type lipidosome (co-carrying therapeutic siRNA and a sound-sensitive agent Ce6) prepared in advance, so that the lipidosome is wrapped or anchored by a denucleated cell membrane; finally, the composite system is subjected to extrusion treatment through a microporous membrane, the drug-loaded vesicles uniform in particle size and stable in structure are obtained, and the drug-loaded vesicles are suitable for various application scenes such as anti-tumor treatment and RNA vaccine delivery.

The invention provides a paclitaxel precursor nano-drug as well as a preparation method and application thereof, and belongs to the technical field of medicinal chemistry. Comprising a paclitaxel dimer prodrug and 7-ethyl10-hydroxy-camptothecin loaded on the paclitaxel dimer prodrug. According to the invention, a paclitaxel dimer prodrug is used as a self-assembly monomer to construct a PTX-SN38 synergistic treatment nano system, and the system has the advantages of dispersibility in water, biocompatibility, tumor specific response, synergistic treatment and the like, and can effectively solve the limitation of paclitaxel and SN38 in anti-tumor treatment.

This invention discloses a class of non-conjugated N-methyl site-linked photosensitive dyes, their preparation methods, and applications, relating to the field of fine chemical organic dye technology. The photosensitive dyes have the structure of general formula 1. These non-conjugated N-methyl site-linked photosensitive dyes possess no heavy atom modification, dual-cation characteristics, and exhibit near-infrared absorption and emission, high molar extinction coefficient, and high photosensitization efficiency, specifically generating type I and type II reactive oxygen species. They demonstrate excellent tumor cell killing ability under near-infrared light irradiation, showing promising application prospects in anti-tumor therapy.

The invention discloses application of a substance for reducing MMACHC expression in preparation of antitumor drugs, and relates to the field of molecular biology. The application discovers that MMACHC can regulate and control a metabolism reprogramming pathway of lipid metabolism under tumor conditions for the first time, and knockout of MMACHC can effectively inhibit the lipid metabolism pathway, so that proliferation and invasion of colorectal cancer cells are inhibited, and the development process of tumors is delayed; therefore, the MMACHC is used as a target spot for anti-tumor treatment, and the substance for reducing the expression of the MMACHC is used for preparing the anti-tumor medicine, so that the MMACHC has important significance on comprehensive treatment of tumors.

The invention belongs to the field of medicinal chemistry and pharmacology, and relates to application of a novel glycolipid TLR2 agonist 13-C in preparation of vaccine adjuvants and anti-tumor treatment. The compound is excellent in human TLR2 agonist activity, EC50 reaches 2.2 nM, and the compound is simple in structure, easy to prepare and excellent in solubility and has industrial application potential. In a B16-OVA tumor model, the antibody induction capacity of the compound is superior to that of a positive control drug Diprovocim, and the anti-tumor activity of the compound is more remarkable; in addition, PD-L1 expression of tumor tissue can be effectively down-regulated, and a synergistic anti-tumor effect is generated with a PD-L1 monoclonal antibody Atezolizumab. Besides, 13-C and a vaccine adjuvant QS-21 are combined for use, so that a synergistic enhancement effect is achieved, the antibody titer induced by a vaccine can be remarkably improved, antibody subtypes are enriched, meanwhile, cellular immunity and humoral immunity response of an organism are stimulated, and the effect of dual immune activation is achieved.

This invention belongs to the field of nanocarrier and immunotherapy technology, specifically relating to a lipid nanoparticle targeting tumor-associated macrophages, a combined delivery method, and its application in tumor immunotherapy. The lipid nanoparticles targeting CD206 tumor-associated macrophages constructed in this invention are used for efficient in vivo delivery of multifunctional nucleic acid molecules, achieving immune regulation, gene editing, and anti-tumor therapy. This invention achieves targeted delivery and multifunctional synergistic effects through lipid particle design, nucleic acid sequence design, and in vitro and in vivo functional verification. Through in vivo delivery of ipLNPs, macrophages can simultaneously achieve: 1) expression of anti-PD-L1 antibodies, blocking immunosuppressive signals; 2) expression of HER2-CAR structures, enhancing phagocytosis and killing ability against tumors; and 3) remodeling of the tumor immune microenvironment through CRISPR / Cas9-mediated FN1 knockout. The lipid nanoparticles constructed using this invention can solve the problem of insufficient targeting of immune cells in the tumor microenvironment by traditional LNP delivery systems.

The application discloses a kind of synergistic antitumor porphyrin-based covalent organic framework heterojunction materials and preparation method thereof, belong to biological medicine technical field. 5,10,15,20-tetra (4-aminobenzene) -21H,23H-porphyrin and 2,5-divinyl benzene formaldehyde are added to organic solvent to carry out solvothermal reaction, and porphyrin-based covalent organic framework (pCOF) is obtained;pCOF is mixed with 1,2-ethanedithiol and heated to obtain thiolated modified pCOF;Thiolated modified pCOF is stirred with glutathione aqueous solution ultrasonically, then tetra-chloroauric acid is added to carry out reaction, and synergistic antitumor porphyrin-based covalent organic framework confined gold nanocluster heterojunction material, recorded as Au@pCOF, is obtained.The Au@pCOF prepared in the application can be used as a kind of biocompatible antitumor therapeutic agent, under the irradiation of 808 nm near-infrared light, active oxygen is efficiently generated and heat is released, photothermal and photodynamic synergistic enhancement is realized, tumor cells are significantly killed, and is used for space-time integration synergistic antitumor therapy.

This invention discloses a STAT3-mutated cell product and its uses, belonging to the interdisciplinary field of genetic engineering and tumor immunotherapy. Through saturation mutation screening, this invention is the first to discover that STAT3 gain-of-function mutations promote CAR-T anti-tumor responses. Furthermore, through cell and animal experiments, it is demonstrated that activating STAT3 can alleviate CAR-T cell immune exhaustion and significantly enhance the in vivo and in vitro killing ability of CAR-T cells against tumor cells, thereby improving the efficacy of anti-tumor therapy. This invention provides a new therapeutic target and strategy for the field of tumor immunotherapy, possessing significant scientific and clinical application value.

The invention belongs to the technical field of preparation of microorganisms and medicines, and particularly relates to a compound FK228D as well as a preparation method and application thereof. The compound provided by the invention is obtained by carrying out culture and liquid fermentation on a Burkholderia thailantensis E264 [delta] tdp:: R-tdp-dep-M4spi which is a mutant strain of Burkholderia thailantensis, and separating the Burkholderia thailantensis from a fermentation liquid of the Burkholderia thailantensis E264 [delta] tdp:: R-tdp-dep-M4spi. In addition, the invention also discloses an application of the FK228 derivative or the pharmaceutically acceptable salt thereof in preparation of antitumor drugs. Experiments prove that the compound 1 produced by the burkholderia mutant strain can obviously inhibit the growth of tumor cells and has no influence on the growth of normal cells. Therefore, the compound provided by the invention is expected to gain the application value in anti-tumor treatment, a new alternative compound is provided for development and application of novel anti-tumor drugs, and the compound has remarkable economic value and social benefit.

The invention relates to a novel medical application of cinobufagin, and the cinobufagin is used as an N-myc protein inhibition / degradation agent and can be used for anti-tumor treatment of neuroblastoma and retinoblastoma.

The invention discloses a pH and enzyme dual-response type targeted DNA nano-carrier for relieving tumor cell hypoxia as well as a preparation method and application of the pH and enzyme dual-response type targeted DNA nano-carrier. The DNA nano-carrier comprises m tandem repeat units, each tandem repeat unit comprises a long single-stranded DNA repeat unit, three complementary short single-stranded DNAs and siRNA, each of the three complementary short single-stranded DNA sequences comprises a functional region and a base complementary region, and the functional region is a pH-responsive nucleic acid complementary sequence or a nucleic acid aptamer sequence for specifically targeting cancer cells; siRNA is a gene therapeutic agent for relieving tumor hypoxia, an extended positive-sense strand of siRNA comprises a 5 '-terminal extended pH response sequence and a positive-sense strand, and the 5'-terminal extended pH response sequence is complementary with a pH-responsive nucleic acid complementary sequence of the complementary short single-stranded DNA. The nano-drug carrier has excellent drug loading capacity and targeting property, can deliver anti-cancer drugs such as siRNA in a targeted manner, responds to a slightly acidic / enzyme environment of tumor cells and is quickly released, and the anti-tumor treatment effect is improved.

The application discloses a ternary supramolecular nanoparticle based on a cyclodextrin-opened cucurbituril double host, which is prepared by adding an organic solvent containing a guest hydrophobic pyridine-pyrrole boron derivative and a hydrophobic adamantyl disulfide modified antitumor drug into an aqueous solution of water-soluble cyclodextrin-opened cucurbituril, and then performing ultrasonic treatment, standing, self-assembly through host-guest interaction between molecules, dialysis in the dark, filtration and drying, so as to obtain the ternary supramolecular nanoparticle. The ternary supramolecular nanoparticle has the advantages of mild preparation conditions, simple operation, uniform size and good stability, and can significantly improve the water solubility of the hydrophobic drugs BP and AD-SS-D. The application realizes a significant synergistic effect of photodynamic therapy and chemotherapy, can effectively induce cancer cell apoptosis and inhibit the migration of the cancer cells, and has low toxicity to normal cells, and provides a safe and efficient novel nanoparticle drug delivery platform for multifunctional synergistic antitumor treatment.

The present invention consists in combining low dose intestinal radiation (ILDR) with immunotherapy or other antineoplastic treatments, in the ideal context of intestinal presence or prevalence of Christensenellaceae family members, especially for solid cancers at an advanced stage (refractory to first line chemo or immunotherapy). The invention also pertains to a bacterial composition,e.g. comprising Chistensenella bacteria, for use in the treatment of cancer in a patient, in combination with intestinal low dose radiotherapy (ILDR) and an antineoplastic treatment.

The invention discloses artificial saliva and a preparation method of artificial saliva hydrogel. The artificial saliva is prepared from the following raw materials in parts by mass: 0.5 to 1 g of KCl, 0.2 to 0.4 g of K2HPO4, 0.2 to 0.8 g of NaCl, 0.2 to 0.4 g of KH2P O4, 10.04 to 20.8 g of CaCl2, 1.5 to 3 g of Nacaboxymethlecellulose, 60 to 120 mg of brown moss alcohol, 495 to 1000 ml of natural coconut juice and 5 to 10 ml of herba sarcandrae extract. By selecting the glabrous sarcandra herb extract, anti-inflammatory and anti-tumor treatment is realized, so that the traditional Chinese medicine composition has a remarkable effect on dry mouth caused by radiotherapy; through the form of a gel bead preparation, the beverage is more portable and unique in taste. The gel beads serve as one of oral local administration preparations, and after the gel beads are exploded, drugs can target small glands which are located below oral mucosa and secrete saliva, and the rapid drug effect is achieved. Direct local administration to the oral mucosa may provide rapid drug action, activate small salivary glands within the buccal mucosa, while avoiding systemic drug exposure and off-target effect.

The invention provides an indole compound as well as a preparation method and application thereof. The structural formula of the compound is shown as a formula (I), a formula (II) or a formula (III). The compound provided by the invention is used as an ATP (adenosine triphosphate) competitive sphingosine kinase 1 (SphK1) or 2 (SphK2) inhibitor, and shows strong enzyme inhibition activity and an effect of resisting tumor cell proliferation. Experiments prove that the indole compound provided by the invention has the potential to be developed into an anti-tumor therapeutic drug and an anti-pulmonary arterial hypertension therapeutic drug, and a new direction is provided for the field of anti-cancer therapeutic drugs. The preparation method of the compound is simple, low in cost, free of dangerous reagents and suitable for industrial production.

The application discloses application of ostruthin in enhancing CAR-T cell anti-tumor function, belongs to the technical field of biological medicine, and the ostruthin can promote cell proliferation, inhibit cell exhaustion, promote the secretion of cytokines related to killing cancer cells, and further enhance the anti-tumor function of CAR-T cells in vivo and in vitro as a cell enhancer of CAR-T cells; experimental results show that when ostruthin is combined with CAR-T cells for anti-tumor treatment, compared with ostruthin or CAR-T cells alone, the combination of the two can significantly inhibit the growth of solid tumors. The application provides a new technical means for improving the tumor treatment effect of CAR-T cell immunotherapy.

The invention relates to a 3, 4, 5-trihydroxy phenylacetate compound and a preparation method and application thereof, the 3, 4, 5-trihydroxy phenylacetate compound belongs to a compound shown in a general formula I and a general formula II, R1, R2 and corresponding derivatives thereof can activate a copper death pathway mediated by endogenous copper ions, have an obvious anti-tumor effect, and have a stronger anti-tumor effect in chemotherapy of drug-resistant tumors. The tumors comprise melanoma, liver cancer, gastric cancer, breast cancer, oral squamous cell carcinoma and the like. The compound is a non-copper ion carrier compound with a brand new structure, induced copper death does not depend on exogenous copper ions, and endogenous copper ions are dissociated by reducing the content of glutathione which is a copper ion chelate in cells. The copper ions are further combined with microfilament skeleton related protein to cause disintegration of the microfilament skeleton, so that copper death is induced. The compound disclosed by the invention can be used as a potential lead compound for inducing endogenous copper ion mediated copper death for anti-tumor therapy.

The invention discloses conjugated molecule-based donor-receptor two-phase self-assembled heterojunction nanoparticles and application thereof, and relates to the field of pharmaceutical preparations. A conjugated polymer is used as an electron donor, a conjugated small molecule is used as an electron acceptor, and an amphiphilic block copolymer is used as a surfactant, so that the heterojunction nanoparticles are formed through co-assembly. In the heterojunction nano-particles, the charge separation efficiency under illumination reaches up to 97%, so that a large amount of various kinds of active oxygen including singlet oxygen (1O2), hydroxyl free radicals (. OH) and superoxide anions (O2.-) are generated, and the antibacterial and anti-tumor purposes are achieved. Besides, due to the special structural design, melanin can participate in a photocatalytic reaction, generation of active oxygen is further promoted, the killing capacity on melanin toxic tumors is improved, and a new direction is provided for developing novel nano-drugs with efficient quantum yield for antibacterial and anti-tumor treatment.

The invention relates to the technical field of nano medicines, and discloses a TNBC targeted nano drug delivery system for overcoming SG drug resistance, comprising: a fluorophore construction module for constructing an AIE fluorophore precursor and performing cationization modification; carrying out terminal modification; the preparation module is used for preparing AIE780 nanoparticles in a water phase; the coupling module is used for covalently connecting SG to the surfaces of the nanoparticles by adopting a carbodiimide-mediated amide coupling reaction; the optical performance evaluation module is used for evaluating the photothermal conversion efficiency and the active oxygen generation capability; the drug release evaluation module is used for simulating different physiological microenvironment conditions to carry out an in-vitro release experiment; the in-vitro activity evaluation module is used for evaluating in-vitro cell uptake and anti-tumor activity; the in-vivo effect verification module is used for carrying out in-vivo targeted delivery and anti-tumor treatment effect verification; according to the invention, the drug resistance of TNBC to SG is effectively overcome through a triple synergistic mechanism.

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.