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

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 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 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 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 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 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 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.