96results about How to "Good antitumor effect" patented technology

As an antitumor drug which is excellent in terms of antitumor effect and safety, there is provided an antibody-drug conjugate in which an antitumor compound represented by the following formula is conjugated to an antibody via a linker having a structure represented by the following formula:-L1-L2-LP-NH—(CH2)n1-La-Lb-Lc-wherein the antibody is connected to the terminal of L1, and the antitumor compound is connected to the terminal of Lc with the nitrogen atom of the amino group at position 1 as a connecting position.

The invention provides biodegradable polyurethane with an amino on the side chain and a preparation method and application thereof, belonging to the field of biomedical materials. Polyurethane is formed by a soft segment and a hard segment, wherein the soft segment is biodegradable polyester diol or biodegradable polyether diol; the hard segment is formed by aliphatic diisocyanate and a chain extender; and the hard segment is provided with the free or protected amino. The biodegradable polyurethane serves as a drug carrier, can wrap drug molecules to form drug carrying microspheres in the nanometer or micrometer scale and can be used for bonding drug molecules, fluorescent molecules and targeted molecules to prepare polyurethane bonded drugs, polyurethane fluorescent probes or polyurethane targeting carriers.

The invention relates to a DSPE-PEG2000-FA-modified nanometer paclitaxel liposome. A molar ratio of the DSPE-PEG2000-FA to egg yolk lecithin is 0.05% to 0.15%, and a particle size of the liposome is less than 150 nm. A preparation method of the DSPE-PEG2000-FA-modified nanometer paclitaxel liposome comprises the following steps: first, preparing a DSPE-PEG2000-FA into a DSPE-PEG2000-FA micelle; second, performing incubation on the phosphatidyl ethanolamine-polyethylene glycol2000-folic acid micelle and a paclitaxel liposome together to obtain a DSPE-PEG2000-FA-modified nanometer paclitaxel liposome. Materials, which are forbidden to be used in clinical practice, are not used as crude materials in the present invention. According to the invention, the DSPE-PEG2000-FA-modified nanometer paclitaxel liposome has a small particle size, and the content of the DSPE-PEG2000-FA is low; besides, the DSPE-PEG2000-FA-modified nanometer paclitaxel liposome has good drug entrapment efficiency and good colloid stability. Moreover, the DSPE-PEG2000-FA-modified nanometer paclitaxel liposome can be absorbed effectively by an ovarian cancer cell having properties of sensitiveness to folic acid (+) and drug resistance, and the cytotoxicity of folic acid dependence is displayed; therefore, the efficacy of the DSPE-PEG2000-FA-modified nanometer paclitaxel liposome is stronger than that of a paclitaxel injection.

A combination therapy for tumor is provided. Disclosed is a method of treating tumor, the method comprises administering to a patient, a compound or pharmaceutically acceptable salt thereof represented by Formula (I) and everolimus represented by Formula (II):wherein R1 is C1-6 alkyl or C3-8 cycloalkyl; R2 is a hydrogen atom or C1-6 alkoxy; and R3 is a hydrogen atom or a halogen atom.

As an antitumor drug which is excellent in terms of antitumor effect and safety and has an excellent therapeutic effect, there is provided an antibody-drug conjugate in which an antitumor compound represented by the following formula is conjugated to an anti-HER2 antibody via a linker having a structure represented by the following formula: -L1-L2-LP-NH—(CH2)n1-La-(CH2)n2—C(═O)— wherein the anti-HER2 antibody is connected to the terminal L1, and the antitumor compound is connected to the carbonyl group of the —(CH2)n2—C(═O)— moiety with the nitrogen atom of the amino group at position 1 as the connecting position.

The invention discloses an application of an ingenane diterpene compound in preparation of antitumor drug. The ingenane diterpene compound is one or more of the ingenane diterpene compound shown in a formula (1). The ingenane diterpene compound can obviously inhibit the propagation activity of breast cancer cells, compared with a traditional tumor therapeutic method, tumor inhibitory effect is good, toxic and side effects are little, targeting property is strong, the ingenane diterpene compound has no damage to normal cells, security can be guaranteed at maximum degree, the ingenane diterpene compound provides a latent novel medicine development purpose for treating breast cancer, and can be a further research as an anti-breast cancer candidate medicine.

The invention relates to preparation of glutamic acid-polyethylene glycol monostearate and application of the amphipathic target material modified nano-particles in disease target transfer. According to the amphipathic target material, glutamic acid is used as a target head, polyethylene glycol is used for improving the flexibility of the target head, and hydrophobic monostearate is used as an anchoring position with polyglycolic-polylactic acid copolymer. The target material modified nano-particles can be used as a target transfer tool of multiple anti-tumor drugs, and interacts with high-expression big neutral amino acid transporter 1 on a tumor cell membrane by the surface modified glutamic acid, so that the cell uptake and anti-tumor activity of the nano-particles can be effectively improved. The nano-particles have good stability, excellent target performance, can be used in intravenous injection, and have a relatively large market application prospect.

Provided is an antitumor agent targeting SIRPα, which inhibits binding between CD47 and SIRPα, the antitumor agent being more effective. The present invention also provides an antitumor agent capable of more effectively exhibiting an antitumor effect when used in combination with an immune checkpoint inhibitor or an antibody drug. The antitumor agent includes as an active ingredient a substance that molecularly targets an IgV domain, which is an extracellular domain of SIRPα. The antitumor agent of the present invention, including as an active ingredient a substance that molecularly targets an IgV domain of SIRPα protein, activates M1-type macrophages, which have cytotoxicity to cancer cells, and immunocompetent cells to provide an effective antitumor effect. Further, the antitumor agent can effectively exhibit an antitumor action not only on cancer cells expressing SIRPα on a cell surface but also on cancer cells not expressing the SIRPα when used in combination with, for example, an immune checkpoint inhibitor and / or an antibody drug that specifically reacts with a cancer antigen and has ADCC and ADCP activities.

The present invention discloses a disodium norcantharidinate medicine compound, its preparation method and application. Its molecular formula is C8H8O5Na2, and its molecular weight is 230.2. Said medicine is obtained by using 1 mol of norcantharidin and 2.0-2.5 mol of sodium hydroxide, making them be completely reacted at 2 deg.C-100deg.C, then making evaporation at 100deg.C-200deg.C to remove water content. Said invention also provides the application of said disodium norcantharidinate medicine compound in preparation of medicine for resisting tumor. It can be made into powder injection, liquid injection or transfusion preparation.

The invention discloses a ganoderma lucidum spore powder compound product for improving anti-tumor curative effects and a method for preparing the ganoderma lucidum spore powder compound product, and relates to the technical field of traditional Chinese medicine healthcare products. The ganoderma lucidum spore powder compound product comprises sporoderm-broken ganoderma lucidum spore powder, ganoderma lucidum, dendrobium officinale, barbary wolfberry fruits, cornus officinalis powder, astragalus, cordyceps militaris, radix adenophorae powder, radix ophiopogonis powder, lentinan, paclitaxel, rhodiola and moringa seed powder. The ganoderma lucidum spore powder compound product and the method have the advantages that synergistic effects can be realized by the ganoderma lucidum spore powder and other traditional Chinese ingredients, composite treatment effects of traditional Chinese medicine compounds can be realized, comprehensive anti-tumor effects of the ganoderma lucidum can be sufficiently realized, accordingly, effects of tonifying primordial qi, boosting vital essence, benefiting joints and strengthening muscles and bones can be realized by the ganoderma lucidum spore powder compound product, the ganoderma lucidum spore powder compound product can be used for anti-fatigue, anti-oxidation, anti-aging and anti-tumor treatment, toxic and side effects of radiotherapy and chemotherapy can eliminated, the immunity of users can be improved, and the ganoderma lucidum spore powder compound product is particularly greatly beneficial to rehabilitation of middle-aged and elderly people after various diseases are treated, improvement of immune functions and strengthening of physique.

The invention discloses a recombinant anti-PD-L1 monoclonal antibody, relates to the technical field of biological medicines, and is used for providing an effective treatment medicine for patients with advanced or metastatic cancers, in particular to the patients with ineffective or drug-resistant treatment by an existing anti-PD-L1 medicine. The complementarity determining region of the antibodyhas sequences shown in SEQ ID NO: 1 to SEQ ID NO: 6. Compared with an existing anti-PD-L1 drug, the antibody has a unique binding epitope, and is better in affinity to human PD-L1 and better in tumorinhibition effect.

The invention discloses spinosyn A and a derivative thereof as an activator of argininosuccinate synthetase 1 (ASS1) and an activator of mutant argininosuccinate synthetase ASS1G362V and application of the Spinosyn A and the derivative thereof. The spinosyn derivative has a structural general formula (I). The spinosyn and the derivative thereof are used as a medicine and an anti-tumor medicine fortreating I-type citrullinemia by activating the argininosuccinate synthetase 1 (ASS1) and the mutant argininosuccinate synthetase ASS1G362V in a targeted manner.

The invention provides a pirarubicin hydrochloride or pirarubicin lipid nanoparticle which can be used for injection and oral administration and a preparation method thereof; the invention is characterized that in the existence of a surface active agent, a carrier material packs the pirarubicin hydrochloride or pirarubicin and the prepared lipid nanoparticle has small particle size, high entrapment rate, good stability and low toxicity. The prepared lipid nanoparticle of the invention can enhance the targeting function to cancer cells, improve the inhibiting and killing function of the pirarubicin to tumor cells and improve the curative effect; the various preparation method of the pirarubicin or the pirarubicin hydrochloride lipid nanoparticle related by the invention has simple preparation technique and low cost and is applicable to industrial production on a large scale.

The invention relates to a pyrimidine derivative with an anticancer effect, belonging to the field of chemical medicines. The invention provides an application of a compound as shown in a formula I which is described in the specification or pharmaceutically acceptable salt of the compound in preparation of drugs used for treatment and / or prevention of cancers. Biological experiment results show that the series of compounds show good inhibition effect on histone arginine demethylase, wherein the IC50 of part of the compounds is at a micromolar level and show good inhibition effect on a varietyof clinically common tumor cell strains; and the IC50 of all the compounds is smaller than 1 [mu]M. The compound provided by the invention also shows good effect in vivo, and can significantly inhibittumor growth in mice. In conclusion, the pyrimidine derivative provided by the invention provides a new effective choice for developing a new generation of targeting drugs for tumor treatment, and has good application prospect.

An antiproliferative effect of IFN-α gene transduction in pancreatic cancer cells. The invention relates to expression of IFN-α to effectively induce growth suppression and cell death in pancreatic cancer cells, an effect which appeared to be more prominent when compared with other types of cancers and normal cells. Another aspect of the invention relates to targeting the characteristic genetic aberration, K-ras point mutation, in pancreatic cancer, and that the expression of antisense K-ras RNA significantly suppresses the growth of pancreatic cancer cells. When these two gene therapy strategies are combined, the expression of antisense K-ras RNA significantly enhanced IFN-α-induced cell death (1.3-3.5 fold), and suppressed subcutaneous growth of pancreatic cancer cells in mice. The invention also relates to a method of suppressing pancreatic cancer cells using double strand RNA formed by antisense and endogeneous K-ras RNA in combination with the anti-tumor activity of IFN-α. The invention relates to the combination of IFN-α and antisense K-ras RNA as an effective gene therapy strategy against pancreatic cancer. The invention also relates to a method of treating pancreatic cancer cells disseminated throughout the body by administering the inventive combination to localized pancreatic cancer cell tumor. The invention also relates to inducing indirect immunological antitumor activity to provide systemic immunity against pancreatic cancer cells.

The invention provides a single light-activated nano particle and a preparation method and application thereof, and belongs to the technical field of medicine. The single light-activated nano particlecomprises a hollow bismuth selenide nano particle, a phase-change material and a radical initiator, wherein the phase-change material and the radical initiator are loaded in the hollow bismuth selenide nano particle. The single light-activated nano particle is in laser radiation, absorbed light energy is converted to hyperthermia, cancer cells are directly killed, the phase-change material further can be prompted to melt, so that the radical initiator is released and split, generated free radical can cause cell membrane lipid peroxidation, glutathione is consumed, DNA is damaged, and thus thecancer cells are removed further. By detecting in vitro cytotoxicity and in vivo anti-cancer function, it is proved that the single light-activated nano particle has superior tumor killing capacity,and efficient photo-thermal and photodynamic combined therapy is realized through the hyperthermia and hyperthermia cascade activated free radical.

The invention provides an anti-tumor fusion protein. The fusion protein has the following first-grade amino acid sequence structure: EGFR specifically targeted oligopeptide-linking peptide 1-lidamycin apoprotein-linking peptide 2-(tuftsin)n, wherein the EGFR specifically targeted oligopeptide-linking peptide has an amino acid sequence as shown in SEQ ID No.1, the lidamycin apoprotein has an amino acid sequence as shown in SEQ ID No.2, the tuftsin has an amino acid sequence as shown in SEQ ID No.3, and n is equal to 1-3. The fusion protein is a novel protein targeting EGFR and containing LDP and Tuftsin, not only retains the phagocytosis promoting effect of the Tuftsin, but also has targeting property and has a favorable anti-tumor effect in an animal body. The invention also provides an encoding gene of the fusion protein, a strengthened fusion protein assembled with a lidamycin chromophore and application of the anti-tumor fusion protein and the strengthened fusion protein in preparation of medicines.

The present invention relates to paeonal injection emulsion for treating tumor and is preparation process. The emulsion consists of liposoluble paeonal and water soluble glossy ganoderma polysaccharide as effective components. The paeonal injection emulsion has high and fast curative effect on tumor, high medicine content, and less toxic side effect.

The invention discloses a LHRH-bonded amphiphilic biodegradable polymer, a preparation method and application, and belongs to the technical field of biomedicine and overcoming the defects that in the prior art, LHRH has difficulty in being connected with a medicinal molecule and the LHRH has poor stability in blood circulation and high in cost. The bonded LHRH amphiphilic biodegradable polymer isformed by bonding LHRH polypeptide derivatives and a diblock copolymer, or bonding the LHRH polypeptide derivatives and a triblock copolymer; and two LHRH polypeptides are included, namely a 10th-site carboxylated LHRH-10-COOH and a 6th-site glycine- dextrorotatory lysine-replaced LHRH-6-NH2. The invention also provides the preparation method of the bonded LHRH amphiphilic biodegradable polymer. The LHRH-bonded amphiphilic biodegradable polymer can prepare a medicine-loading nanoparticle with an LHRH targeting function, is applicable for a variety of medicines and has a function of targeting a cancer cell which highly expresses an LHRH receptor.

The invention discloses an anti-tumor composition in ganoderma lucidum spore oil and a preparation method thereof. The method comprises the following steps: extracting the ganoderma lucidum spore oil from wall-broken ganoderma lucidum spore powder; adding organic solvents such as petroleum ether and ethanol and purified water to extract; concentrating extracted lower-layer liquor; carrying out column separation on the concentrated liquor by using a macroporous resin column; carrying out gradient eluting by purified water, 50% ethanol and ethanol with concentration greater than or equal to 75%; and collecting the last eluate and freeze-drying the eluate to obtain the anti-tumor composition. The composition obtained by the invention can inhibit external and internal tumor cell growth, and the anti-tumor rate reaches over 56.3%.

The invention provides a sulfydryl-containing zwitterionic polypeptide modified doxorubicin derivative, a nano-micelle and a preparation method of the nano-micelle, and belongs to the field of biological medicines. The doxorubicin derivative has a structure as shown in a general formula (I). The preparation method of the doxorubicin derivative comprises the following steps of in a polar solvent, mixing sulfydryl-containing zwitterionic polypeptide with acryloylhydrazine to react, and performing crystallizing to obtain a polypeptide derivative; and dissolving the polypeptide derivative and doxorubicin hydrochloride in the polar solvent according to a molar ratio of 1: (0.2-5), adding a trifluoroacetic acid catalyst, and carrying out a stirring reaction to obtain the doxorubicin derivative.The nano-micelle prepared from the doxorubicin derivative is long in in-vivo blood circulation time, high in drug loading capacity, small in toxic and side effects, good in pH value response and goodin tumor inhibition effect.

The present invention provides a novel antimetabolic anticancer agent that has an excellent balance between antitumor effect and toxicity. Specifically, the present invention provides a medicament containing, as an active ingredient, a 5-fluorouracil derivative represented by Formula (I) or a salt thereof:wherein R1 represents a hydrogen atom or a protecting group of a hydroxy group, R2 represents a lower alkoxy-lower alkyl group or a tetrahydrofuranyl group, X represents a carbon atom or a nitrogen atom, and Y represents a halogen atom or a cyano group.

The invention discloses applications of serum thymus factor (FTS) in preparation of anti-tumor medicines, protective medicine or immunity intensified medicines for physical treatment and chemical treatment of tumor. Experimental results reveal that all groups of tumor-bearing mice and W256 rat fed with medicines are significantly different from groups fed with physiological saline and the tumor inhibition rates of all the groups fed with the medicines are more than 30 percent, thus confirming the tumor inhibition effect of the FTS. The FTS can also enhance the immunity activity and strengthen the immunity function of living organisms in a plurality of aspects; the FTS has no toxicity and less side effects; the effective wide dose scope and wide safety range. The FTS has obvious protective function to immunity indexes of living organisms, which is discovered in the study of the protective medicines for the physical and chemical treatment medicines of tumor. Therefore, the FTS can provide a new target and development for the clinical treatment of tumor.

The invention provides a nano-medicine, a preparation method thereof and an application of the nano-medicine. The nano-medicine comprises a calcium phosphate substrate, a chemotherapy medicine, a photo-thermal agent and an autophagy inhibitor, the chemotherapy medicine is sealed in the calcium phosphate substrate, the surface of the calcium phosphate substrate is modified by the photo-thermal agent, and the autophagy inhibitor is loaded into a pore of the photo-thermal agent. According to the nano-medicine, chemotherapy and thermotherapy are combined, calcium phosphate serves as a rigid substrate, the chemotherapy medicine and the photo-thermal agent are sealed in the rigid substrate of the calcium phosphate, the autophagy inhibitor of a cell is loaded on the rigid substrate, so that chemotherapy and thermotherapy effects can be improved by inhibiting autophagy, and tumor treatment effects are improved.

The invention discloses a fabrication method of cellulose membrane of a drug loading breast cancer-targeting magnetic nanoparticles. The method includes the following steps: 1. Grant the folic acid of optical activity by chemical modification, fix the prepared acid on the magnetic hydrogel, which then is be used to absorb hematoporphyrin monomethyl and cancer therapeutic drug, and finally obtain the tumor-targeting nano-drug; 2. Produce cellulose membrane by cultivating acetobacter xylinum and static fermentation, add the tumor-targeting nano-drug solution made in step 1 into the container for the cellulose membrane under dark condition until it's submerged, and carry out vacuum freeze drying after processed by the oscillator. The cellulose membrane of a drug loading tumor-targeting magnetic nanoparticles has high efficient in targeting the breast caner cell and suppressing its growth. At the same time, it can significantly reduce the dosage of conventional photosensitizer. In addition, the transdermal drug delivery would enhance the the drug effects on caner, realizing the controlled-release of the drug and largely lowering the toxic and side effects to healthy tissues.

The invention relates to solamargine liposome, which is characterized in that the liposome comprises the following raw materials: 1 part by weight of solamargine, 8 to 80 parts by weight of phospholipid, 2 to 20 parts by weight of cholesterol and 1 to 10 parts by weight of emulsifier. The invention also discloses a preparation method of the solamargine liposome. The invention has the advantages that the solamargine is coated between the two phospholipid layers of the liposome so that the water solubility is enhanced; the physical stability of the solamargine liposome is good; and the solamargine liposome can be stored for a longer time. The preparation method of the solamargine liposome is simple and mature, and is convenient to industrial production.

The invention provides sodium new houttuyfonate and application of sodium new houttuyfonate and cis-platinum in treatment of colon cancer, breast cancer, lymphoma, melanoma, lung cancer and other malignant tumors. A MTT method and a CCK-8 method are adopted to correspondingly determine sodium new houttuyfonate and inhibition effects of sodium new houttuyfonate and cis-platinum combined drug on various tumor cells (including SW620, A375, MCF-7, A549 and raji), and tests find that sodium new houttuyfonate and sodium new houttuyfonate and cis-platinum combined drug have significant inhibition effects on various tumor cells. Moreover, the combined medication shows an addition or synergistic effect, so that valuable theoretical and data support is provided for clinical treatment of malignant tumor diseases.

The invention provides a ligand antrum mucosal protein-18(AMP-18) of a laminin receptor (LR), which has an amino acid sequence as shown in SEQ ID No.1 in a sequence table. The ligand antrum mucosal protein-18(AMP-18) can bind with LR on the surface of gastric epithelial cells to inhibit the growth of stomach cancer cells and can be used to prepare drugs for treating tumor.