238 results about "Antineoplastic drug" patented technology

The present invention relates to the compositions, methods, and applications of a novel approach to selective cellular targeting. The purpose of this invention is to enable the selective delivery and / or selective activation of effector molecules to target cells for diagnostic or therapeutic purposes. The present invention relates to multi-functional prodrugs or targeting vehicles wherein each functionality is capable of enhancing targeting selectivity, affinity, intracellular transport, activation or detoxification. The present invention also relates to ultra-low dose, multiple target, multiple drug chemotherapy and targeted immunotherapy for cancer treatment.

The objective of the present invention is to provide a pharmaceutical composition and a therapeutic method that are specifically effective against at least one disease selected from multiple endocrine neoplasia, type IIA, multiple endocrine neoplasia, type IIB, familial medullary thyroid carcinoma, thyroid carcinoma, papillary thyroid carcinoma, sporadic medullary thyroid carcinoma, Hirschsprung disease, pheochromocytoma, parathyroid hyperplasia and mucosal neuromas of the gastrointestinal tract.4-(3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy)-7-methoxy-6-quinolinecarboxamide and analogs thereof are specifically effective against at least one disease selected from multiple endocrine neoplasia, type IIA, multiple endocrine neoplasia, type IIB, familial medullary thyroid carcinoma, thyroid carcinoma, papillary thyroid carcinoma, sporadic medullary thyroid carcinoma, Hirschsprung disease, pheochromocytoma, parathyroid hyperplasia and mucosal neuromas of the gastrointestinal tract.

Novel poly-substituted pteridinediones (lumazines), and mono- or polysubstituted 2-thiolumazines, 4-thiolumazines or 2,4-dithiolumazines, having disclosed substituents in positions 1, 3, 6 and 7 of the pteridine ring, and pharmaceutically acceptable salts thereof, being represented by the general formula (I). are useful as biologically active ingredients in preparing pharmaceutical compositions especially for the treatment or prevention of a CNS disorder, a cell proliferative disorder, a viral infection, an immune or auto-immune disorder or a transplant rejection. Combinations of the pteridine derivatives of the invention with an immunosuppressant or immunomodulator drug, an antineoplastic drug or an antiviral agent, providing potential synergistic effects, are also disclosed.

The invention discloses pyridylpyrimidyl amine compounds or pyridylpyridyl amine compounds disclosed as Formula I and application thereof in preparing antineoplastic drugs, belonging to the technical field of drugs. The compounds can selectively inhibit CDK4 and CDK6, enable G1-period tumor cells to stop growth and G1-period tumor cells to reduce, can effectively lower the phosphorylation of the tumor inhibiting protein Rb in the Ser780 site, and thus, can be used for various diseases caused by cell cycle control maladjustment participated by CDK4 and CDK6. The compounds are especially suitable for treating malignant tumors, and have the characteristics of high selectivity, high activity and high tumor cell proliferation resistance.

The invention discloses a panax notoginseng polysaccharide extract and a preparation method, preparations and applications thereof. The panax notoginseng polysaccharide extract is prepared by taking waste residues produced after panax notoginseng saponins are extracted as raw materials through the steps of extraction, concentration, purification, drying, crushing and detection, wherein the content of panax notoginseng polysaccharides is not less than 15%. The preparation method of the panax notoginseng polysaccharide extract comprises the steps of extraction, concentration, purification, drying, crushing and detection, and specifically comprises the steps of adding waste residues produced after panax notoginseng saponins are extracted into purified water for extracting, carrying out filtration and concentration on the obtained object, adding ethanol into the obtained object for precipitating, and carrying out filtration, purification and drying on the obtained product so as to obtain a target dried product. Pharmaceutical excipients are added into the panax notoginseng polysaccharide extract to be prepared into powder, capsules, granules, tablets or pills; and the panax notoginseng polysaccharide extract is applied to the preparation of antineoplastic drugs and immunity enhancing drugs. According to the invention, waste residues produced after panax notoginseng saponins are extracted are reused, thereby changing waste material into things of value, facilitating the comprehensive utilization of panax notoginseng resources, reducing the cost and improving the economic benefits.

The invention relates to the technical field of medicinal chemistry, in particular to a 2-aminothiazoles compound or acceptable slat in pharmaceutical science, a preparing method thereof, pharmaceutical composition comprising the same, and application thereof in antineoplastic drug preparation.

The invention provides an antineoplastic drug screening cell model utilizing STAT3 as target, belonging to the field of biomedicine. The model is created by a reporting system carrier containing an STAT3 specific binding sequence on the basis of active cells with constitutive STAT3, and the model is used for screening treatment medicine of carcinomatous changes and tumors caused by STAT3 constitutive activation. The active cells with the constitutive STAT3 are utilized, so the reporter gene in the model cell is situated at an overactive state, and no additional stimulant is necessary; besides, the obtained stable cell model can be directly used for screening the compounds, thereby not only greatly reducing the screening cost, but also simplifying the whole screening process from cell cultivation, STAT3 activation, compound feed and detection to cell cultivation, compound feed and detection, shortening the screening period, reducing the operation steps, and improving the stability, efficiency and usability of the system, so that the model is more suitable for high throughput medicine screening.

The invention provides the appraisal and selective method for the antineoplastic drug based on the cell micrograph information, which uses a sort of selection and appraisal hardware system to appraisal and select the antineoplastic drug by different fluorescence dye marking and measuring the multicellular parameter change in cell. The hardware system is made up of the high precision electric hydrous platform, the fluorescence vision system, the image collecting and processing system and working station. The diacetoxyl fluoresceine dyeing measures the active cell number; the double dyeing method of Hoechst33342 and iodized pyridine appraise the drug inducing the cell die; the three dyeing method of FDA, Hoechst33342 and PI analyzes the die mode induced by drug. The invention can measure at least two kinds of single cell or cell subgroup which expresses different drone cell organ. The method is in reason and can be used in study of drug action mechanism and selecting the high hedonic drug and toxicity analyzing, which can be used in selecting drug and appraising the drug toxicity.

Systems and methods are disclosed herein for applying near-infrared optical energies and dosimetries to alter the bioenergetic steady-state trans-membrane and mitochondrial potentials (ΔΨ-steady) of all irradiated cells through an optical depolarization effect. This depolarization causes a concomitant decrease in the absolute value of the trans-membrane potentials ΔΨ of the irradiated mitochondrial and plasma membranes. Many cellular anabolic reactions and drug-resistance mechanisms can be rendered less functional and / or mitigated by a decrease in a membrane potential ΔΨ, the affiliated weakening of the proton motive force Δp, and the associated lowered phosphorylation potential ΔGp. Within the area of irradiation exposure, the decrease in membrane potentials ΔΨ will occur in bacterial, fungal and mammalian cells in unison. This membrane depolarization provides the ability to potentiate antimicrobial, antifungal and / or antineoplastic drugs against only targeted undesirable cells.

The invention discloses a traditional Chinese medicine composition with an antineoplastic effect, and a preparation method and an application thereof. The traditional Chinese medicine composition comprises the following raw materials in parts by weight: 15-30 parts of barbed skullcap herb, 15-30 parts of oldenlandia diffusa, 15-30 parts of rabdosia rubescens, 3-15 parts of radix sophorae flavescentis, 5-15 parts of curcuma zedoary, 5-15 parts of stir-baked fructus arctii, 5-15 parts of red ginseng, 5-30 parts of astragalus mongholicus, 6-12 parts of bighead atractylodes rhizome, 10-15 parts of poria cocos, 6-15 parts of radix paeoniae alba, 5-15 parts of Chinese angelica, and 3-20 parts of radix glycyrrhizae preparata. According to the traditional Chinese medicine composition, traditional Chinese medicine proportioning prescription is conducted by a theory of treatment based on syndrome differentiation according to a. traditional Chinese medicine theory; and clinical experimental results indicate that the traditional Chinese medicine composition has a better killing effect on cells of various tumors such as a gastric cancer, a liver cancer and a lung cancer, is wide in application scope, has no adverse effect clinically and is safe and reliable to take, and a new-generation antineoplastic drug is expected to be developed.

A method for encapsulating cisplatin and other positively-charged drugs into liposomes having a different lipid composition between their inner and outer membrane bilayers is disclosed. The liposomes are able to reach primary tumors and their metastases after intravenous injection to animals and humans. The encapsulated cisplatin has a high therapeutic efficacy in eradicating a variety of solid human tumors including but not limited to breast carcinoma and prostate carcinoma. Combination of the encapsulated cisplatin with encapsulated doxorubicin or with other antineoplastic drugs are claimed to be of therapeutic value. Also of therapeutic value in cancer eradication are claimed to be combinations of encapsulated cisplatin with a number of anticancer genes including but not limited to p53, IL-2, IL-12, angiostatin, and oncostatin encapsulated into liposomes as well as combinations of encapsulated cisplatin with HSV-tk plus encapsulated ganciclovir.

The disclosure relates to methods of ameliorating or preventing cardiotoxicity caused by anti-neoplastic agents, such as doxorubicin, by administering to a patient oxypurinol, salt or derivatives thereof, before, during or after administration of the anti-neoplastic agent.

The invention discloses a degradable orthopedics drug carrier system with osteo inductivity and a preparation method thereof. The drug carrier system essentially consists of the carrier material which is biological activity glass setting solid and the carried therapeutic drug. And the carrier material is the solid body carrier material with certain strength which is obtained through the fast curing after the reaction of highly reactive boron-containing biological activity glass and cured buffer liquid after the reaction. The carrier material can carry various drugs without thermal stability restriction, such as antibiotics, bone growth factors, antituberculosis drugs, antineoplastic drugs, which are used for the treatment of orthopedics diseases, thus composing the integrated drug carrier system. The drug carrier system can degrade automatically under the function of human tissue fluid in a human body with a porous structure left during the degradation which provides diffusion channels for the sustainable releasing of the drugs, thus achieving the effect that the drugs are chronically and uniformly released. The drug carrier system has good biocompatibility, biological activity and osteo inductivity and can be applied to the treatment of various diseases of orthopedics.

A method to enhance the cytotoxic activity of an antineoplastic drug comprising administering an effective amount of the antineoplastic drug to a host exhibiting abnormal cell proliferation in combination with an effective cytotoxicity-increasing amount of an antioxidant. The invention also includes a method to decrease the toxicity to an antineoplastic agent or increase the therapeutic index of an antineoplastic agent administered for the treatment of a solid growth of abnormally proliferating cells, comprising administering an antioxidant prior to, with, or following the antineoplastic treatment.

The invention discloses a targeted sustained release medicine carrying nanoparticle and a preparation method thereof. A mixture of a carrier I containing tumor targeted molecules and a carrier II containing antineoplastic drugs serves as a carrier of the nanoparticle, an organo-siloxane reagent easily hydrolyzed serves as a silane coupling reagent, and the nanoparticle which has a core-shell structure including that drugs are wrapped in the core through chemical bond connection and in a physical mode and the targeted molecules are exposed outside is obtained through micro emulsion technical preparation. The drugs are wrapped on the nanoparticle through a chemical method and the physical method, the mass fraction of the drugs in a nanoparticle is increased, preliminary-stage release is slowed down, and later-stage release is supplemented. The organo-siloxane reagent forms another layer of shell on a macromolecule two-block interface layer due to strong hydrolysis of the organo-siloxane reagent and the characteristic that the organo-siloxane reagent and a hydrophilic chain of amphipathy block polymers easily form hydrogen bonds, and therefore the effect of slow-release is strengthened.

An implantable medical device such as a catheter includes an outer controlled-release layer with a pharmacologically active ingredient for helping to prevent the occurrence or recurrence of cancer, or an immunosuppressive drug. The outer layer includes a bioactive material such as paclitaxel or other drug known to help reduce the incidence of formation of tumors or other cancerous items within the body of a patient.

The invention relates to a paclitaxel lipid microsphere injection and a manufacturing method thereof. In the invention, a paclitaxel lipid microsphere injection that does not contain polyoxyethylene castor oil is prepared. The medicine 90-98 per cent paclitaxel is coated in the oil phase and the oil-water interfacial film of the lipid microsphere. Thus the toxicity and stimulation of paclitaxel in clinic use are largely reduced, and the adverse reaction resulted from the excipient in the existing paclitaxel injection is prevented. With low stimulation, low toxicity and high efficiency, the preparation as a antineoplastic drug is administrated by intravenous injection.

The invention relates to a preparation method of functionalized nano-carbon tube antineoplastic drug carrier and an application of functionalized nano-carbon tube camptothecin composite in treating Hela cervical carcinoma cells in vitro, belonging to an antineoplastic drug carrier. The preparation method comprises the following steps: mixing sulphuric acid with nitric acid to prepare mixed acid; putting a nano-carbon tube into the mixed acid for carrying out ultrasonic processing; separating centrifugally; washing the mixture with distilled water to be neutral to obtain a short nano-carbon tube; mixing the short nano-carbon tube with triblock copolymer water solution; using a 200 nm microporous filtering film to filter to obtain multi-wall nano- carbon tube aqueous phase system; adding camptothecin solution into the aqueous phase system for centrifugal separation and filtration to obtain triblock copolymer nano-carbon tube camptothecin; and uniformly scattering the complex into physiological saline to obtain stable camptothecin multi-wall nano- carbon tube complex. The invention has the advantages of obvious tumor cell inhibition in treating Hela cervical carcinoma cells in vitro, broad-spectrum anti-tumor activity and simple preparation method.

The invention provides a camptothecin-site 20 norcantharidate derivative with a structural formula as shown in I which is described in the specification, and a preparation method and antineoplastic application thereof. Results of activity test prove that the camptothecin-site 20 norcantharidate derivative as shown in I is an appropriate candidate antineoplastic drug, especially a candidate drug for resisting liver cancers, stomach cancers and colorectal cancers. Compared with positive contrast drugs, i.e., camptothecin and cantharidin, the camptothecin-site 20 norcantharidate derivative has improved water solubility and stability; and the camptothecin-site 20 norcantharidate derivative is sensitive to acid and can be easily hydrolyzed. Moreover, the preparation method for the camptothecin-site 20 norcantharidate derivative employs easily available raw materials, has high yield and is easy to operate and implement.

A dendric cell tumor vaccine carrying withered heat shock tumor cells for preparing antineoplastic medicine and decreasing immune escape is prepared through treating tumor cells by heat shock method, inducing the wither of tumor cells, preparing dendric cells, and carrying the withered heat shock tumor cells.

The invention discloses a triazolyl-containing amino-dithio formic ether compound as well as a preparation method and application of the compound which is taken as a new antineoplastic medicament lead compound, belonging to the field of pharmaceutical chemistry. According to the invention, 1, 2, 3-triazole active fragment is introduced into the structure of amino-dithio formic ether by click chemistry, thus the preparation method is simple, efficient and environment-friendly. The triazolyl-containing amino-dithio formic ether compound has the structure general formula shown in the specification, and has excellent antineoplastic activity for multiple tumour cells, can be used as a candidate or lead compound for the further development to be applied to the preparation of the antineoplastic medicaments.

The invention discloses a tumor cell membrane / nuclear membrane double-targeting tumor nano-drug slow-release system and preparation and application thereof. The tumor cell membrane / nuclear membrane double-targeting tumor nano-drug slow-release system is a nano particle composed of a nucleus and a shell, wherein the shell is composed of an aptamer, PEG and nano liposomes, and the aptamer is connected with the nano liposome through the PEG and capable of specifically recognizing a tumor cell; the nucleus is composed of a nano material modified by polypeptide and an antineoplastic drug carried by the nano material modified by the polypeptide, and the polypeptide is capable of penetrating through a cell nucleus nuclear membrane. It is proved through experiments that the tumor cell membrane / nuclear membrane double-targeting tumor nano-drug slow-release system can inhibit tumor growth and prolong the survival time of a tumor-bearing animal and can be used for treating a tumor.

The invention discloses a preparation method of injectable nano-composite hydrogel having a pH sensitive property, wherein the preparation method comprises the following steps: 1. preparing materials: preparing lyophilized graphene oxide, and having cyclodextrin having a pH sensitive property; 2. preparing a cyclodextrin nanoparticle emulsion which contains antineoplastic drugs and has a pH sensitive property; and 3. preparing a composite hydrogel drug carrier. The injectable nano-composite hydrogel having the pH sensitive property prepared by the invention is applicable to a composite drug carrier for disease treatment and for drug controlled release. The product disclosed by the invention is consistent with basic requirements of the drug carrier in performance and is capable of controlling drug release; and the product is huge in social and economic benefits.

The invention discloses a drug-loaded nanoparticle with reductive responsiveness and a preparation method and applications thereof. The structural formula of the drug-loaded nanoparticle with reductive responsiveness is as follows:, wherein x is 45, y is 15, and z is 20, or x is 45, y is 12, and z is 6. The diameter of the drug-loaded nanoparticle disclosed by the invention is 91-109 nm. PEG hydrophilic segments constitute a hydrophilic shell layer of the polymer nanoparticle, and polyphosphoesters of which a side group contains disulfide bonds constitute a hydrophobic core. The block polymer can be formed into a micelle by self-assembling in water, and then pharmaceutical molecules are loaded in the hydrophobic core of the carrier nanoparticle through a physical embedding effect, so that the drug solubility is greatly increased, the cycling time is prolonged, and the vascular permeability enhancement effect (i.e. enhanced permeability and retention EPR effect enhancement) is passively targeted to tumor tissues. The nano drug carrier can entrap various hydrophobic antineoplastic drugs such as hydrophobic drugs such as doxorubicin, paclitaxel, gefitinib, camptothecin, and the like.

The invention discloses a resveratrol benzene acrylamide derivative, a preparing method and an application thereof. The resveratrol benzene acrylamide derivative has a structure shown in general formula (1) and general formula (2): the resveratrol benzene acrylamide derivative has an obvious effect of growth inhibition for a human body breast cancer cell line (MCF-7), a human body lung cancer cell line (A549) and a human body melanoma cell line (B16-F10), thereby the resveratrol benzene acrylamide derivative can be used for preparing antineoplastic drugs.

The present invention discloses a cyclic pentapeptide with anti-tumour activity, which is cyclic (leucyl-N-methylleucyl-leucyl-leucyl-N-methylleucyl) and the constitutional formula of which is shown in the formula (I). The cyclic pentapeptide of the present invention is separated from galaxaura filamentosa in the South China Sea, and in vitro experiments show that the cyclic pentapeptide has strong inhibiting effect on human hepatoma cell lines (HepG2), human hepatoma cell lines (BEL-7402), human mammary cancer cell lines (MCF-7), human colon cancer cell lines (LOVO), human lung cancer cell lines (PC84045) and human nasopharyngeal cancer (CNE) and can keep the mitotic cycle of BEL-7402 hepatoma cells in G2 / M phase. The present invention provides a pilot compound for the research and the development of new anti-tumour drugs and is valuable for the exploitation of the marine pharmaceutical resources of China.

The invention relates to a multi-layer composite dual-drug-loaded microsphere as well as a preparation method and an application thereof in preparing antineoplastic drugs. In a preferred preparation method, the multi-layer composite dual-drug-loaded microsphere is mainly composed of two model drugs, chitosan and glucan; according to the preparation method, a chitosan microsphere self-assembled template is prepared by virtue of a double-emulsification-crosslinking method, then on the basis of an electrostatic interaction between polyelectrolytes having different charges, the glucan is adsorbed on the surface of the chitosan microsphere so as to form a glucan / chitosan dual-layer composite drug-loaded microsphere, and based on an electrostatic adsorption interaction between the chitosan and the glucan on the surface of the dual-layer composite drug-loaded microsphere, the chitosan / glucan / chitosan multi-layer composite dual-drug-loaded microsphere is formed. An in vitro release test on the multi-layer composite dual-drug-loaded microsphere having pH responsivity provided by the invention shows that the multi-layer composite dual-drug-loaded microsphere has a good sustained-release effect, and an in vitro antineoplastic cell activity test shows that the multi-layer composite dual-drug-loaded microsphere has a good inhibitory effect.

The invention discloses a preparation method of an antineoplastic drug carrier having dual-lymphatic targeting. The preparation method comprises the following steps: preparing drug-loaded chitosan nanoparticles: adding an antineoplastic drug solution to a chitosan solution and stirring; and adding a sodium tripolyphosphate solution and stirring, so as to obtain the drug-loaded chitosan nanoparticles; and preparing the dual-lymphatic targeting antineoplastic drug carrier: dispersing the drug-loaded chitosan nanoparticles in water, adding a cross-linking agent, sodium hyaluronate and LyP-1 and stirring so as to obtain the dual-lymphatic targeting antineoplastic drug carrier. The preparation method disclosed by the invention is simple in process, and the method is capable of achieving massive preparation in one time with a high drug-loading capacity. The prepared antineoplastic drug carrier is stable in physical and chemical properties and is capable of keeping a uniform morphology for a long time without agglomeration. The antineoplastic drug carrier is high in tumor targeting rate, and is capable of accurately positioning and retaining in lymphatic metastatic tumor and releasing antineoplastic drugs therein.

The invention belongs to the field of pharmacy, and particularly relates to whole process targeting polypeptide molecule targeting a brain capillary vessel endothelial cell, a tumor neovascular endothelial cell, a tumor mimic blood vessel, a tumor cell and a tumor stem cell, and a stable optimized polypeptide molecule thereof, and an application of modified compound and a drug delivery system in the diagnosis and treatment of tumors. The invention relates to the application of the whole process targeting polypeptide WVAP and a WVAP modified drug and a polymer carrier material, and the application thereof in the construction of tumor imaging and a targeted therapy delivery system, the results show that WVAP can cross a blood-brain barrier, can target tumor neovascularization and cross blood-tumor barrier, and target tumor mimicry blood vessels, the tumor cells and the cancer stem cells; the nano drug delivery system constructed by the WVAP modified polymer carrier material can effectively deliver the encapsulated drug into the brain, targets the tumor tissue, and significantly improves the antitumor efficacy.