103results about How to "Good tumor suppressor effect" patented technology

The invention discloses a magnetic nano-grade material with a cell-targeting property, and a biomedical application thereof. The magnetic nano-grade material can be specifically bound with highly expressed transferrin receptors on tissue cell surfaces, and can enter the cells. The material can be bound with various high-transferring-receptor-expression tissue cells with broad spectrum and specificity, such that high-efficiency cell targeting property can be realized on animal models. The material can be used as a magnetic resonance contrast agent and a fluorescent molecular probe in disease diagnosis, and can be used as a medicine carrier in disease treatment.

Disclosed herein is a method for suppressing the growth of cancer cells in a mammal in need of such treatment comprising administering to said mammal a cancer cell suppressing amount of a diphenylmethylpiperazine represented by the following general formula [1]:wherein R represents:or a pharmaceutically acceptable salt thereof.Compared with conventional anticancer agents, these agents are less toxic and exert an excellent carcinostatic effect on various solid cancers. Moreover, these anticancer agents inhibit the proliferation of fibroblasts, which makes them efficacious against pulmonary fibrosis and proliferative keloid lesions.

The invention discloses a double-targeting polypeptide-antibody-drug conjugate, and a prepared method and antineoplastic application thereof. The double-targeting polypeptide-antibody-drug conjugate structurally includes four components of (A), tumor specificity targeting polypeptide; (B), an antineoplastic drug; (C), a mitochondria target functional group; and (D), hydrazone bonds used for connecting the polypeptide and the antineoplastic drug. The tumor specificity targeting polypeptide is connected with the antineoplastic drug by a connecting arm comprising the hydrazone bonds; the antineoplastic drug is connected with the mitochondria target functional group by chemical bonds; and the tumor specificity targeting polypeptide is suitable for targeting the conjugate to a tumour cell and marker protein LAPTM4B carried on the surface of the tumour cell is used as a specificity target. A molecular target is combined with an organelle target, selective uptake of the drug in the tumour cell can be increased, an acting site of a DOX drug can be transferred form cell nucleus to mitochondria, and therefore the condition that the tumour cell is killed by drug resistance is avoided.

A self-assembly short peptide R418 consists of an anti-tumor bioactive peptide section S18, a self-assembly peptide section RADA16-I and a connection peptide section, and the amino acid sequence is described in sequence table SEQ ID NO.1. The characterizations of an atomic force microscope and a transmission electron microscope prove that R418 molecule has the characteristic of forming nano fiber through self assembly in a solution. In vitro cell experiment shows that the self-assembly short peptide R418 can remarkably cause the death of tumor cells K562, Jurkat and MDA-MB-435S and has lower cytotoxicity on NIH3T3 cell. Beastie living body imaging experiments show that: after self assembly, the holding time of the local concentration of the R418 in an in vivo tumor region is much longer than the holding time of the local concentration of the S18. In accordance with beastie living body imaging experiments, animal tumor inhibition experiments show that: the self-assembly short peptide R418 has better tumor inhibition effect as compared with short peptide S18.

The present invention discloses a nucleic acid construct. The nucleic acid construct is characterized in that the nucleic acid construct has a structure as shown in the formula car-[(IRES)-f]<m>, wherein the IRES is a sequence of an internal ribosome entry site, f encodes a functional protein F, m is 0 or a non-0 natural number, car encodes a CAR, the CAR comprises (a) an extracellular binding domain that specifically recognizes CLDN18.2, (b) a hinge domain, (c) a transmembrane domain, (d) a costimulating intracellular domain, and (e) a signal transduction domain, the extracellular binding domain comprises scFv, and the amino acid sequences and functions of the extracellular binding structural domain are described in the specification. The CAR molecule provided by the invention has excellent safety and effectiveness and shows a very good tumor inhibition effect.

The invention provides a deuterated compound shown as a formula (I) or an optical isomer, a tautomer, a pharmaceutically acceptable salt, a prodrug, a hydrate or a solvate thereof. Compared with a compound before deuteration, the deuterated compound disclosed by the invention shows better pharmacokinetics, higher highest blood concentration, higher exposure and longer half-life period, and has more excellent metabolic performance. Moreover, the deuterated compound provided by the invention can effectively inhibit the activity of FAK, and has a very good application prospect in preparation of an FAK inhibitor and / or a drug for treating cancers. Meanwhile, the deuterated compound and an anti-cancer drug (such as a PD-1 inhibitor) are combined for use, so that the synergistic effect can be achieved, the tumor inhibition effect is remarkably improved, and a better choice is provided for clinical treatment of cancers.

The invention belongs to the field of traditional Chinese medicines and relates to a traditional Chinese medicine composition cooperatively used in radiotherapy. The traditional Chinese medicine composition cooperatively used in the radiotherapy is prepared from the following raw materials in parts by weight: 8-20 parts of angelica sinensis, 5-15 parts of the rhizome of chuanxiong, 5-15 parts of radix paeoniae alba, 3-10 parts of pinellia ternate, 10-25 parts of codonopsis pilosula, 5-15 parts of rhizoma polygonati, 10-20 parts of the root of bidentate achyranthes, 3-10 parts of dogwood, 10-20 parts of peach kernel, 5-15 parts of pseudo-ginseng, 8-20 parts of mushroom, 5-12 parts of rehmannia glutinosa, 10-20 parts of the root of kudzu vine, 3-10 parts of dried tangerine or orange peel, 5-15 parts of membrane of chicken gizzard, 3-10 parts of dandelion, 3-10 parts of glossy privet fruit, 5-12 parts of epimedium, 10-15 parts of the fruit of Chinese wolfberry, 10-20 parts of toad skin, 3-10 parts of rhizoma anemarrhenae, 5-15 parts of oldenlandia diffusa, 5-15 parts of burdock, 5-25 parts of astragalus membranaceus, and 10-20 parts of liquorice. The traditional Chinese medicine composition cooperatively used in the radiotherapy, which is disclosed by the invention, has the advantages that the toxic and side effects of the radiotherapy can be reduced, the sensitivity of cancer cells can be reinforced, and the like.

The invention discloses a targeted photodynamic nano probe based on upconversion nano particles and an ultrathin silicon dioxide layer. The nano probe comprises an upconversion nano particle kernel, an ultrathin silicon dioxide shell layer covering the surface of the kernel, and methylene blue and polyethylene glycol-folic acid loaded on the shell layer. The established UCNPs@SiO2 / MB / PEG-FA nano probe is distributed in a cancer cell cytoplasm by virtue of endocytosis of receptor mediation and generates active oxygen under the excitation of near-infrared rays, so that the potential of a mitochondrial membrane in the cell can be reduced to induce the irreversible cell death of the cancer cell. The established UCNPs@SiO2 / MB / PEG-FA nano probe has excellent tumor inhibition effect in the animalexperiment.

The invention relates to application of a curcumin derivative Ca 37 in preparation of a drug for treating a prostate cancer disease, and relates to the field of biology and pharmacy. The object is to provide a use of the curcumin derivative in treatment of the prostate cancer disease. The application provided by the invention is mainly characterized in that the proliferation of prostate cancer cells PC(Prostate Cancer)-3 which are independent of male hormones is inhibited by the curcumin derivative, and the effect is obviously better than that of curcumin itself, the decrease of the capacity function of the PC-3 cells, i.e., oxygen glycolysis and oxidative phosphorylation, apoptosis starting and autophagy defects are induced, and the growth inhibition function mainly depends on the generation of reactive oxygen species.

The invention discloses a solid tumor inhibiting medicine composition composed of arctigenin and a pyrimidine nucleotide synthetic inhibitor, wherein a weight ratio of the components is 1:0.001-1000, and preferably 1:0.01-100. Pharmacodynamic tests show that, the medicine composition provides substantial synergetic effects in the treatments of solid tumors, especially leukemia. The medicine composition provided by the invention has advantages of wide tumor inhibiting spectrum, small side effect, low treatment cost, and good prospect in clinical application.

The invention relates to designing and application of a prodrug based on a gemcitabine structure. According to the prodrug, a phosphate ester long-chain group is introduced to the position 5'-OH of a gemcitabine five-membered sugar ring, so fat-solubility and membrane permeability of the prodrug are improved. In tumors lacking nucleic acid transport protein, the fat-soluble prodrug can enter the tumors through passive diffusion and active transport to inhibit growth of the tumors. Moreover, the prodrug can be orally taken, thereby obtaining a better or same curative effect of tumor growth inhibition compared with intraperitoneal injection of gemcitabine.

The invention relates to a preparation method of a pyridine-modified dendrimer copper complex hybrid nanomaterial. The method comprises: (1) modifying a pyridine group on a dendrimer at an amino terminal through an amido bond, acetylizing to obtain an acetylized dendrimer macromolecule-pyridine compound G5.NHAc-Pyr; (2) directly complexing a bivalent copper ion and the acetylized dendrimer macromolecule-pyridine compound G5.NHAc-Pyr in (1) to form a hybrid nanometer material G5.NHAc-Pyr / Cu. The pyridine-modified dendrimer copper complex hybrid nanomaterial prepared through the method has favorable water solubility and colloidal stability, has an inhibitive ability on tumor cells and a certain r1 relaxation rate at the same time, can be applied to chemotherapy and MR imaging of rat tumors,and has a diagnosis and treatment integration effect.

The invention belongs to the field of bio-pharmaceuticals and particularly relates to expression, purification and self-assembly of TRAIL variant proteins. A recombinant protein is expressed by plasmids comprising the TRAIL fusion proteins in escherichia coli, and the recombinant protein with high activity is produced. The recombinant proteins adopt a centrifugal mode for simple and rapid purification. The purified proteins are self-assembled into particles being 200 nanometers under the physiological conditions. After intravenous injection to a tumor transplantation mouse, the recombinant protein is effectively gathered in the tumor location of the mouse. The recombinant protein is injected into the tumor transplantation mouse in an intraperitoneal injection mode, and tumor growth is effectively suppressed. The recombinant protein subjected to simple process purification is used for oncotherapy.

The invention provides a stable polypeptide inhibitor for targeting HDAC. The amino acid sequence structure of the stable polypeptide inhibitor is shown in specification. The invention also provides application of the stable polypeptide inhibitor targeting HDAC in preparation of a drug for inhibiting the enzymatic activity of HDAC family. The invention also provides application of the stable polypeptide inhibitor targeting HDAC in preparation of a drug for inhibiting tumor stem cells with high expression of HDAC1. The invention further provides application of the stable polypeptide inhibitor targeting HDAC in preparation of a drug for treating human ovarian teratoma or testicular embryonic carcinoma. Experiments of cell proliferation, apoptosis and cell cycle arrest prove that the polypeptide can effectively inhibit proliferation of the tumor stem cells, and the polypeptide has no obvious tissue damage or toxicity to mice at a high dose.

The invention discloses an imidazo[1,2-a]pyridine compound, and a preparation method and applications thereof. The imidazo[1,2-a]pyridine compound can inhibit the activity of NEK2 kinases as an NEK2 micro-molecular inhibitor with a novel structure. The invention also discloses effects of the imidazo[1,2-a]pyridine compound in inhibition of proliferation of tumor cells and inhibition of growth of the tumor cells in animal bodies through inducing cell cycle stopping and apoptosis.

The present invention relates to a method for preparing cells for cancer treatment and a kit for cancer treatment comprising cells prepared by the method. The preparation method of the present invention can provide F cells, which, in spite of having no difference in the proliferative capacity compared with mesenchymal stem cells expressing cytosine deaminase, which are harvested and used immediately after the culture, exhibit a very excellent tumor suppressive effect through the treatment together with 5-FC and induce a remarkable synergistic effect exceeding an effect from combinative treatment with an existing anticancer drug in cases of a combinative treatment with another anticancer drug. Therefore, the present invention can be utilized for a kit for cancer treatment comprising such F cells, and thus can be favorably used to maximize the effect of existing cancer treatments.

The invention belongs to the field of tumor treatment and the field of molecular immunology, and relates to an antibody for resisting human epidermal growth factor receptor 2 (HER2), as well as a medical composition and use of antibody, in particular to the antibody for resisting Her2 or an antigen binding fragment of the antibody for resisting Her2. The antibody for resisting Her2 comprises a first heavy chain and a second heavy chain, wherein according to the first heavy chain, a variable region of heavy chain (VH) of the first heavy chain comprises a complementarity-determining region (CDR) of which the amino acid sequence is SEQ ID No: 1-3, and the amino acid sequence of the CH of the first heavy chain is as shown in SEQ ID No: 7; according to the second heavy chain, a variable region of heavy chain (VH) of the second heavy chain comprises a complementarity-determining region (CDR) of which the amino acid sequence is SEQ ID No: 4-6, and the amino acid sequence of the CH of the first heavy chain is as shown in SEQ ID No: 8. Compared with the combination of two antibodies of trastuzumab and pertuzumab, the antibody disclosed by the invention has higher cell direct killing activity and higher antibody dependent cellmediated cytotoxicity (ADCC) activity; the complement-dependentcytotoxicity (CDC) activity of the two antibodies of trastuzumab and pertuzumab is equivalent to that of the antibody disclosed by the invention; the antibody disclosed by the invention adopts a structure of a normal antibody; and fucose is also knocked out, so that the ADCC activity is improved.

The invention relates to a temperature-sensitive liposome preparation of vinblastine medicaments and a preparation method thereof. The temperature-sensitive liposome preparation includes vinblastine medicament, temperature-sensitive phosphatide and optional long circulating material. A molar ratio of temperature-sensitive phosphatide to optional long circulating material is 70:30-92:8; and a weight ratio of vinblastine medicament to blank liposome is 1:10-1:50. The invention employs a pH gradient active drug loading method to reach an entrapment rate of 90.0-99%. The liposome preparation with heat sensitivity of the present invention can make the liposome to passively target a tumour position and release a lot of medicament simultaneously, so as to improve curative effect and reduce toxic and side effects on the whole body.

The invention provides a 4-substituted anilino-podophyllotoxine derivative which refers to a 4'-O-demethyl-4-deoxy-4-substituted anilino-podophyllotoxine derivative. A series of compounds with anti-cancer activity is synthetized by taking the traditional drug etoposide as a lead compound by structural transformation; primary in vitro screening and in vivo antitumor tests show that the compounds have better anti-tumor activity, wherein when the compound GL3 improves the anti-tumor action, the toxicity of the compound GL3 is obviously reduced, and thereby, the compound GL3 can be used for preparing anti-tumor drugs which has higher antitumor activity and lower toxicity and has effect on multi-drug drug resistant tumors. The structural general formula of the 4-substituted anilino-podophyllotoxine derivative is shown in the specification.

The invention provides high polymer CA4 bonding medicine and a preparation method thereof. The bonding medicine has a structure shown in the formula (I). By grafting CA4 to a specific polymer carrier, the obtained bonding medicine can be enriched on tumor vessels and slowly released, the function of breaking tumor vessels is achieved for a long time at tumor parts, and an outstanding tumor restraining effect is achieved. The problems that CA4P acting time is short and treatment effect is not good enough are effectively solved, and the medicine has wide development prospects in the tumor treatment field. In addition, the preparation method is simple, raw materials are wide in source, mass production can be achieved, and industrialization can be achieved.

The invention belongs to the technical field of medicines, and particularly relates to application of combined stephanine and an autophagy inhibitor for preparing drugs for treating a liver cancer. Itis found that drug combination of the cepharanthine hydrochloride and the autophagy inhibitor has a good cancer inhibition effect in vitro and vivo, more treatment solid tumor schemes are provided, and two combined drugs are wide in source and are economic and effective. According to the application of the combined stephanine and the autophagy inhibitor for preparing the drugs for treating the liver cancer, it is firstly found that by using the autophagy inhibitor to reinforce the antitumor effect of the cepharanthine hydrochloride in vitro and vivo, the antitumor effect of the cepharanthinehydrochloride in vitro and vivo is verified on a vivo mouse model, and a novel scheme for effectively and feasibly treating a solid tumor is provided.

The invention particularly relates to an LAG-3 protein affinity cyclopeptide and application thereof. The amino acid sequence of the affinity cyclopeptide is shown in SEQ ID NO.1 or SEQ ID NO.2 or SEQID NO.3. The invention further provides a drug composition or kit containing the cyclopeptide. The affinity cyclopeptide can achieve affinity with extracellular domains of LAG-3 protein, stop interaction between LAG-3 / MHC-II molecules, and then achieve the anti-tumor effect.

The invention discloses steroid saponin compounds and a preparation method and application thereof. The preparation method comprises the following steps of: extracting tribulus terrestris linn by using an extraction agent to obtain extract; performing high performance liquid chromatography on the extract to obtain the compounds shown as a formula I and / or a formula II in the claim 1, wherein the high performance liquid chromatography comprises the following steps of: taking mixed solution consisting of acetonitrile and water in a volume ratio of 35 to 65 as a mobile phase, wherein the flow rate of the mobile phase is 4ml / minute; collecting an elution peak with retention time of 9.798 to 10.798 minutes to obtain the compound shown as the formula I; and collecting the elution peak with the retention time of 13.423 to 14.423 minutes to obtain the compound shown as the formula II. An experiment shows that: the two steroid saponin compounds have good effect of suppressing tumors, and can suppress a plurality of tumors; and the method for preparing the steroid saponin compounds has the advantages of simple operation, low cost and high yield. Therefore, the compounds have wide application prospect in preventing and / or treating the tumors.

The invention discloses drug-loading nanoparticles based on a ferulic acid polymer, a preparation method and applications thereof. According to the present invention, ferulic acid and SOCl2 are used as raw materials, and are subjected to a condensation polymerization reaction in a pyridine alkaline environment to prepare a polymer PFA, wherein the polymer PFA is non-biotoxic, has good biocompatibility and good degradability, can be prepared into a nanoparticle material, can further be used as a drug carrier for loading hydrophobic drugs, has stable properties, and has a particle size of less than 200 nm; the drug-loading nanoparticles can achieve the long-circulating delivery of anticancer drugs in vivo, are easily permeated and accumulated in the tumor site, and can enhance the targetingeffect of drugs at the tumor site by using the EPR effect so as to enhance the treatment effect and reduce the toxic-side effect on the human body; the preparation method has advantages of simple reaction process, few reaction steps, short reaction cycle, good repeatability and the like; and the drug-loading nanoparticles have good application prospects and broad development space in the medical field.

The invention provides an aspirin derivative. The aspirin derivative has a structure as shown in a formula (I) which is described in the specification. The aspirin prodrug with the structure has the capability of sensitively releasing aspirin or salicylic acid under the stimulation of active oxygen or ultraviolet light; furthermore, the sensitive aspirin prodrug with the structure is combined to aspecific polymer carrier; an obtained bonding drug can be enriched to tumor tissues and rapidly release the drug, so that the bonding drug has a wide development prospect in the fields of reducing inflammation of the tumor tissues, improving a tumor immunosuppression microenvironment and inhibiting tumor growth. The aspirin polymer prodrug provided by the invention can be enriched at a tumor or inflammatory site, improve the in-vivo metabolic pathway of aspirin, and can effectively solve the problems of short action time and poor curative effect of micromolecular aspirin. Moreover, the preparation method provided by the invention is simple, wide in raw material source and capable of realizing batch production and industrialization.

The invention discloses an elastin-like polypeptide temperature-responsive nano-material, and a preparation method and application thereof. The nano-material disclosed by the invention is a material prepared by modifying a nanoparticle with an elastin-like polypeptide. The elastin-like polypeptide has responsiveness to a tumor microenvironment and is A1) or A2), wherein A1) refers to a protein with an amino acid sequence as shown in a sequence 1 in a sequence table, A2) refers to a protein which is obtained by inserting a cysteine residue or a polypeptide containing the cysteine residue into the amino acid sequence of a protein P and has same functions, and the protein P is prepared by subjecting a polypeptide as shown in site 17 to 21 in the sequence 1 to repetition 30 to 100 times. The nanoparticle has surface plasmon resonance effect and is a gold nanoparticle, silver nanoparticle, platinum nanoparticle or gold-silver nanoparticle. Experimental results show that the nano-material provided by the invention has a high photothermal conversion rate and good tumor inhibitory effect and can be used for treating tumors.

The invention relates to a preparation method and application of an amphiphilic polymer. The problems that an insoluble drug is poor in absorption and treatment effect and low in bioavailability and has more adverse effects can be effectively solved. According to the technical scheme, the amphiphilic polymer is formed by connecting a N-vinyl pyrrolidone monomer with maleic acid Guerbet eicosanol monoester, the maleic acid Guerbet eicosanol monoester is generated through esterification of maleic anhydride and 2-octyl-dodecane Guerbet alcohol, a free radical polymerization reaction is conducted in n-heptane by taking lauroyl peroxide as an initiating agent and taking N-vinyl pyrrolidone and the maleic acid Guerbet eicosanol monoester as monomers, and then the amphiphilic polymer is obtained. According to the preparation method and application of the amphiphilic polymer, the insoluble drug is embedded into polymeric micelles by taking the amphiphilic polymer as a carrier material to prepare an insoluble drug-loaded micelle injection, a very good tumor inhibiting effect is achieved, the toxicity is low, the water solubility of the insoluble drug can be enhanced, the bioavailability of the drug can be improved, and the toxic and side effects of the drug can be reduced.

The invention relates to a copper peroxide transdermal microneedle system and a preparation method and application thereof. The copper peroxide transdermal microneedle system comprises a microneedle substrate and at least one microneedle body distributed on the microneedle substrate, and each microneedle body comprises a matrix and copper peroxide nanoparticles.

The invention relates to a temperature-sensitive liposome preparation of vinblastine medicaments and a preparation method thereof. The temperature-sensitive liposome preparation includes vinblastine medicament, temperature-sensitive phosphatide and optional long circulating material. A molar ratio of temperature-sensitive phosphatide to optional long circulating material is 70:30-92:8; and a weight ratio of vinblastine medicament to blank liposome is 1:10-1:50. The invention employs a pH gradient active drug loading method to reach an entrapment rate of 90.0-99%. The liposome preparation with heat sensitivity of the present invention can make the liposome to passively target a tumour position and release a lot of medicament simultaneously, so as to improve curative effect and reduce toxic and side effects on the whole body.

The invention relates to a preparation process and application of MCP (Modified Pectin), and particularly relates to a preparation process of a degradable pectin with different molecular weight ranges and application of the degradable pectin in the anti-tumor field. The preparation process of the MCP comprises the following steps: dissolving and swelling a pectin by using water; sterilizing for 10 hours under an ultraviolet lamp; regulating a solution to be alkaline (the NaOH concentration is 0.01-0.05 mol / L) by using a NaOH solution; degrading at certain temperature (30-70 DEG C) for a period of time (1-4 hours), and then regulating by using 3 mol / L HCl until the pH is equal to 3; reacting at room temperature for 22 hours; and carrying out membrane dialysis, desalination, concentration and freeze drying on a product to obtain the MCP. The preparation process disclosed by the invention is favorable to obtaining the MCP with different molecular weight distributions. The MCP has pancreatic cancer resistant activity and is capable of preferably inhibiting the proliferation of a tumor cell and higher in medical value.