250 results about "Cis-platinum" patented technology

The invention discloses a tetravalent platinum complex with a bioactive group and a preparation method of the tetravalent platinum complex. The tetravalent platinum complex is a platinum (IV) complex and has the structure shown in the formula II (please see the formula in the description), wherein in the formula II, Y is OH or Cl, and Bio represents the bioactive group. The platinum (IV) complex is prepared according to the equation in the formula III (please see the formula in the description), wherein in the formula III, Y is OH or Cl, Bio-OH represents a compound with bioactivity, TBTU represents a coupling agent O-(benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium tetrafluoroborate, TEA represents a catalyst triethylamine, DMF represents solvent N,N-dimethyl formamide, and DMSO represents solvent dimethylsulfoxide. Cis-platinum is adopted for the bottom face of an octahedron, a small-molecular targeted or medicine active group is introduced to one axial position, a hydroxyl group or helium atom is introduced into another axial position, and the anti-tumor tetravalent platinum complex overcoming cisplatin resistance is provided, so the high-efficiency and low-toxin platinum (IV) complex is obtained.

The invention relates to a nano micelle of a biodegradable macromolecular-bonding Pt(IV) anti-cancer medicament and a preparation method thereof. The structural formula of the anti-cancer medicament is defined in the specification, wherein the biodegradable macromolecule is tri-block copolymer, namely polyethylene glycol-b-polyester-b-polylysine; and tetravalency platinum coordination compound Pt(IV) is connected with a side amino on the block of polylysine on a macromolecular carrier through alpha, omega-polyethylene glycol. The carrier is non-toxic and is water-soluble, thus being convenient for reacting with the platinum(IV) coordination compound in water phase; a nano micelle form can be formed through self assembly; a platinum(IV) coordination compound is reduced to platinum(II), namely, cis-platinum, Carboplatin or Oxaliplatin, and the anti-cancer effect is known; the synthesis of the nano micelle is easy; the reduction potential of platinum(IV) is low, so that the platinum(IV) can be rapidly reduced to platinum(II) in cancer cells to take treatment effect; and the platinum(IV) is connected to the side chain of the macromolecule rather than the end of a chain, a macromolecular chain can be connected with multiple platinum(IV)s, and the content of platinum can be as high as 10-20%.

The invention belongs to the field of pharmaceutical chemistry, and relates to a furazan derivative which is prepared by combining a coumarin parent nucleus and an isomer of the coumarin parent nucleus with a furazan oxide through linking of groups with different lengths and structures. It is proved by the experiments that the furazan derivative has excellent effects on inhibiting sensitive human tumour cells and drug-resistant tumor strains, and on inhibiting activity of normal growth of HUVEC for measuring an inhibiting action of neovascularization, and on inhibiting activity of cell proliferation of cis-platinum-resistant A2780 cell strains and gemcitabine-resistant HM231 cell strains. It is shown by an initial pharmacological mechanism that by releasing nitric oxide with the high concentration, the furazan derivative can induce apoptosis of cancer cells, inhibits MEK activity, and obviously inhibits phosphorylation of MEK in an MAPK/ERK channel, thereby generating a significant effect on inhibiting growth of a tumor. According to the composition in the invention, excellent basis for obtaining candidate medicines having inhibition activity of sensitive and drug-resistant tumors and for illustrating the pharmacological action is provided.

The invention relates to the technical field of medicaments. Dimethyldiguanide belongs to a biguanides oral hypoglycemic medicament and is widely applied to pharmaceutical therapy of type 2 diabetes. The invention aims at providing a novel application of the dimethyldiguanide and particularly an application of the dimethyldiguanide in preparation of medicaments for preventing or treating the hepatocellular carcinoma. According to the application disclosed by the invention, the restriction effect of the dimethyldiguanide on the hepatocellular carcinoma is found by research from two aspects, namely, cell culture in vitro and animal experiment in vivo. Experiments find that the dimethyldiguanide has the capabilities of restricting proliferation and clone formation of a hepatocellular carcinoma cell line and causing the cell cycle arrest and apoptosis increase of the hepatocellular carcinoma cell line, and also has the capability of enhancing the hepatocellular carcinoma resisting effect of chemotherapeutics when combined with the chemotherapeutics, such as cis-platinum, doxorubicin and the like. The invention provides the novel application of the dimethyldiguanide and also provides a novel concept for prevention and treatment of the hepatocellular carcinoma.

The invention discloses an application of miltirone in preparation of antitumor drugs. The miltirone has a structure of formula I; the miltirone serves as an inhibitor of STAT3 (Signal Transducer and Activator of Transcription 3) and is capable of inhibiting growth and proliferation of tumor cells which are abnormally activated by STAT3 so as to cause the apoptosis of the tumor cells and also capable of improving sensibility of cytotoxic drugs and inhibiting formation of tumor vessels. The miltirone with the structure of formula I can inhibit STAT3 kinase Tyr705 phosphorylation level to achieve the functions of accelerating the apoptosis of the tumor cells, improving the sensibility of chemotherapy drugs and inhibiting formation of new vessels; and the proliferation of tumor cells can be significantly inhibited due to the combined combination of the miltirone with low toxicity or non-toxic concentration and adriacin doxorubicin with low toxicity or non-toxic concentration and the combined application of the miltirone and cis-platinum with low toxicity or non-toxic concentration. The functions of the miltirone with the structure of formula I have positive significance to prevention and treatment of tumors.

The invention discloses an anti-cancer medicinal aspirin platinum complex and a preparation method thereof. The method comprises the following steps of coordinating amine or heterocyclic amine on a platinum atom through a coordinated N atom and the coordination function of the platinum, introducing halogen or hydroxyl, carboxylate radical or substituted carboxylate radical through the coordination function, and oxidizing the platinum atom into tetravalent platinum, connecting aspirin molecular axially to form tetravalent platinum complex with one aspirin molecular single substitute or two aspirin molecular double substitutes axially. As the tetravalent state of the platinum is relatively inert, the toxic side effect on organs is small, and moreover, the uptake route of drug is changed, the anticancer activity of the drug is improved, the anti-tumor activity which is same to or even more excellent than that of cis-platinum is realized, and the killing function to the drug resistant cells is good. The preparation method provided by the invention is simple in structure, low in cost and suitable for industrial production.

The invention relates to the novel usage of an antimalarial medicine, in particular to the novel usage of hydroxychloroquine having sensitivity enhancing effect on various chemical anti-multiple myeloma medicaments. The novel usage is characterized in the application of hydroxychloroquine in treatment of multiple myeloma through chemotherapeutic medicaments. The hydroxychloroquine can obviously enhance the killing activity of chemotherapeutic medicines such as doxorubicine, epidoxorubicin, cis-platinum and mitoxantrone to multiple myeloma cells, and the killing activity thereof is realized by inhibiting the myeloma cell autophagy signals by hydroxychloroquine. Hydroxychloroquine can induce the quantity of the autophagy lysosomes of the multiple myeloma cells to be increased and the expression of the autophagy-associated albumen LC3-II to be increased.

The invention relates to a ruthenium complex, the structural formula of which is shown in a formula I. Compared with cis-platinum, the ruthenium complex provided by the invention is small in toxic and side effects and is good in drug absorption, strong in anti-cancer activity, strong in ability of inducing tumor cell apoptosis and strong in ability of being bonded with DNA, and shows a good function in tumor treatment. The formula is shown in the description.

The invention discloses a making method of naiad platinum with low-silver content, which comprises the following steps: reacting cis-platinum diiododiamide and silver nitrate with molar rate at 1: 2 for 3-8 h under 10-30 deg.c; filtering; adding halogenate MX [M is Na, K, Ca, Ba, NH4 or M is (CnH2n+1) 4N (n=1-4), X=Cl, Br, I] in the filtrate to remove trace silver; reacting for 0.5-1h under 10-30 deg.c; filtering; adding sodium glycolate in the solution; adjusting pH value to neutral to react for 3-10 h under 50-60 deg.c; decompressing; condensing; filtering; drying; obtaining the product; setting the molar rate of cis-platinum diiododiamide and sodium glycolate at 1: 1 and the molar rate of halogenate MX and silver nitrate at 0.1-0.01:1.

The invention discloses marine traditional Chinese medicine gracilariopsis lemaneiformis polysaccharide derived from red alga plant gracilariopsis lemaneiformis, discloses a synergistic effect of the gracilariopsis lemaneiformis polysaccharide serving as anti-tumor drugs, especially a synergist of cis-platinum for the first time, and further discloses an application of the gracilariopsis lemaneiformis polysaccharide to preparation of drugs or healthcare products or food for treating tumors. The gracilariopsis lemaneiformis polysaccharide can serve as a synergist of the anti-tumor drugs. The anti-tumor effect is achieved mainly by retraining growth and propagation of tumor cells, and the anti-tumor effect is achieved for gastric adenocarcinoma, lung cancer and carcinoma of the uterine cervix. The invention further discloses a preparation method of the gracilariopsis lemaneiformis polysaccharide and a detection method of the anti-tumor effect of the gracilariopsis lemaneiformis polysaccharide. A new way is provided for further utilization of gracilariopsis lemaneiformis serving as marine drug resources, and a new choice is provided for development of the anti-tumor drugs for treating or preventing tumors through the application of the gracilariopsis lemaneiformis polysaccharide to preparation of the anti-tumor drugs or anti-cancer healthcare products or food.

The invention provides a reduction responding covalent organic polymer and a preparation method and application thereof. The polymer provided by the invention is obtained by mixing and reacting carboxyl terminated polyethylene glycol, a compound with a structure shown in formula (I) and carboxylic cis-platinum prodrug, wherein the compound is obtained by respectively connecting 5,10,15,20-tetra(4-hydroxyphenyl) porphyrin with cis-platinum prodrug and polyethylene glycol, thus having good water solubility and biocompatibility; the obtained nano particles not only can produce singlet oxygen under laser radiation, but also can generate dissociation under the condition with high reducibility of cancer cells to release cis-platinum drugs, and has certain application in combined treatment of tumor; furthermore, the compound can also be directly used as a drug delivery system without a carrier, thus effectively avoiding use of additional carriers.

The invention provides application of an emodin anthraquinone derivative in preparation of anti-hepatocellular carcinoma drugs. The emodin anthraquinone derivative is a 1, 4-dimethyl-6, 8-dimethoxy-9, 10-anthraquinone. The derivative not only can well inhibit proliferation of hepatocellular carcinoma cells, induce their apoptosis, and also has very small toxicity to normal cells. The derivative can be used in conjunction with 5-FU, cis-platinum and other chemotherapy drugs to increase the sensitivity of the chemotherapy drugs, thus achieving the effect of inhibiting hepatocellular carcinoma cell growth. Therefore, the emodin anthraquinone derivative can be used for preparing anti-hepatocellular carcinoma drugs or adjuvant chemotherapy drugs.

The invention discloses hyaluronic acid modified mitochondria target liposome and a preparation method thereof. The mitochondria target liposome disclosed by the invention is prepared from drug carrying liposome and outer-layer modifying hyaluronic acid, wherein the drug loading liposome is liposome covered by hydrophobic drug and dequalinium chloride, and the hydrophobic drug is any one chosen from adriamycin, taxol, 10-hydroxycamptothecine, irinotecan or cis-platinum. The hyaluronic acid modified mitochondria target liposome disclosed by the invention has the beneficial effects that receptors are effectively targeted, uptake of tumor cells to liposome is improved, cell mitochondria is further targeted in the tumor cells, a function of damaging the mitochondria is achieved, tumor cell apoptosis is promoted, tumor cell growth is inhibited, and ability of overcoming multidrug resistance of the tumor cells is achieved.

The present invention relates to polymeric antitumor agent which is formed in polymeric micelle complex by intermolecular bonding or mutual interaction between styrene maleic acid copolymer (SMA) and low molecule antitumor agent which is anthracyclins drug such as pirarubicin, doxorubicin, epirbicin, daunorbicin, acralbicin, or alkaloid antitumor agent such as cis-platinum, and taxol These polymeric antitumor agents may improve specificity to cancer cells so that it improves antitumor effect, while it may not be concentrated at normal organ or tissue, so that adverse effect may be diminished. These polymeric antitumor agents may be prepared by dissolving SMA and low molecule antitumor agent in aqueous solution, then in the presence of aqueous soluble carbodiimide, amino acids, or polyamine, adjusting pH to form micelle complex and recovering polymer fraction.

The invention discloses a preparation method of an RGD peptide and penetrating peptide R8 co-modified ergosterol and cis-platinum active drug-loading liposome. The method comprises the main steps of ergosterol liposome preparation, ammonium chloride gradient formation, drug loading and co-modification. The method is simple in technology and easy to carry out, and the encapsulation rate of a drug is high; ergosterol is adopted to partially replace cis-platinum to exert efficacy, an ergosterol and cis-platinum active drug-loading liposome is obtained, the effect of resisting a lung cancer is guaranteed, the toxic and side effects of the drug are significantly reduced, and damage to human bodies is small; meanwhile, the RGD peptide and the penetrating peptide R8 serve as target heads, the targeting property is good, and the drug exertion effect is good.

The invention relates to lanthanum fullerenol and application in preparing medicaments for inhibiting tumor growth, in particular to lanthanum fullerenol nanoparticles with the general formula of M@C2m(OH)x and the application thereof in preparing medicaments for inhibiting tumor growth, wherein M is La rare earth metal, m is equal to 41 or 30, and X is equal to or larger than 10 and is less than 50; and because of the reorganization of adjacent hydroxyl groups, the quantity of O on C82 carbon cage is actually different from the quantity of H, and therefore, the general formula can be written in the form of M@C2mOXHY. Compared with cyclophosphamide, cis-platinum, taxol, and the like which are clinically and widely used, the lanthanum fullerenol M@C2m(OH)x or M@C2mOXHY has the advantages of low consumption and toxicity and high rate of tumor inhibition.

The invention discloses a new application of brusatol serving as a chemotherapeutic drug synergist, which is combined with a chemotherapeutic drug when in use. The chemotherapeutic drug comprises cis-platinum, carboplatin, oxaliplatin, 5-fluorouracil, paclitaxel, adriamycin or adriamycin. The brusatol provided by the invention can be prepared into an oral preparation or a non-oral preparation accepted pharmaceutically. The beneficial effects of the brusatol applied in preparing the chemotherapeutic drug synergist are as follows: (1) the brusatol can be used in an Nrf2 path, and the killing effect of various chemotherapeutic drugs on the cancer cells can be enhanced; (2) the growth inhibition of low-dose cis-platinum on transplantable tumor of a naked mouse can be increased by the brusatol, thus having clinical application prospects; (3) the cis-platinum content in non-small cell lung cancer cell strains can be increased by the combined use of the brusatol and the cis-platinum; and (4)the toxicity is not discovered when the brusatol and the cis-platinum are together used in the cellular level and in the mouse test work concentration.

The invention relates to a compound with the anti-cancer activity. The compound has a structure as shown in a general formula I. The compound can be extracted from cyclocarya paliurus by adopting a method which is simple, convenient and easy to operate. The compound provided by the invention can effectively inhibit proliferation of human breast cancer cells and hepatoma carcinoma cells; an effect of the compound is superior to that of a classical anti-cancer compound cis-platinum; the compound is excellent in anti-cancer activity, can be used for preparing medicines and health products, and has potential application value. The general formula I is shown in the description.

The invention provides a cis-platinum coordination compound which has a formula (I) structure or a formula (II) structure. The preparation method of the cis-platinum coordination compound is as follows: cis-platinum and a block copolymer with a formula (III) or a formula (IV) are subjected to coordination action in a water-based medium so as to generate the cis-platinum coordination compound. The cis-platinum coordination compound has good dissolubility and good biocompatibility and is degradable. In the water-based medium, the cis-platinum is protected by a poly (Gamma-propinyl-L-glutamate-g-dimercaptosuccinic acid) block and a polyethylene glycol block, so that the cis-platinum coordination compound has good stability. In addition, carboxyl contained in the cis-platinum coordination compound has PH-value sensibility, and in a lower PH-value environment, the carboxyl trends to be deprotonated, the releasing of the medicaments is promoted, and the curative effects of the medicaments are improved.

The invention discloses application of dioscin in preparing a drug-resistant osteosarcoma medicine. Drug-resistant osteosarcoma refers to an osteosarcoma cell line which has drug resistance to commonanti-tumor medicines, particularly U2OS tumor cells with drug resistance to methotrexate, doxorubicin and cis-platinum. Moreover, as a natural plant extract medicine, dioscin has wide application prospects in the field of anti-tumor medicine treatment.

The invention relates to aprepitant intravenous injection emulsion as well as a preparation method and an application thereof, and belongs to the technical field of pharmaceutics. The aprepitant intravenous injection emulsion is prepared from components in percentage by mass as follows: 0.05%-3% of aprepitant, 5%-30% of an oil phase solvent, 1.2%-18% of an emulsifier, 0.03%-0.6% of a stabilizer and 1%-5% of an isoosmotic adjusting agent, the injection emulsion further contains a pH regulating agent and the balance of water for injection, and pH value of the injection emulsion is 5.5-8.0. The aprepitant intravenous injection emulsion contains no low-carbon chain alcohol such as ethanol and the like, meanwhile, the quality requirement for a marketed product can be met by technological innovation and adjustment, and clinical use safety of the aprepitant intravenous injection emulsion is greatly improved; direct intravenous injection is utilized during clinical using, and dilution is not needed; the aprepitant intravenous injection emulsion can be used for treating acute and tardive nausea and vomiting caused by high-dose cis-platinum combined high-dose sensitizing cancer chemotherapy,and nausea and vomiting in early stage and middle stage of tumor chemotherapy are reduced.

The invention belongs to the field of pharmacotherapeutics, and particularly relates to application of 18 beta-glycyrrhetinic acid (or salt) for serving as an auxiliary treating drug capable of easing acute kidney injury caused by a chemotherapeutic drug, namely cis-platinum, wherein the 18 beta-glycyrrhetinic acid (or salt) is one of the main components of liquorice. The cis-platinum serves as a commonly-used chemotherapy drug, and clinical application thereof is restricted by kidney toxicity thereof. The levels of creatinine and urea nitrogen in the acute kidney injury induced by the cis-platinum can be inhibited by the18 beta-glycyrrhetinic acid, expression of KIM-1 injured protein is lowered, and apoptosis of renal tubular epithelial cells caused by the cis-platinum is inhibited. According to the application of the 18 beta-glycyrrhetinic acid (or salt) for serving as the auxiliary treating drug capable of easing the acute kidney injury caused by the chemotherapeutic drug, namely the cis-platinum, the effect that the 18 beta-glycyrrhetinic acid has a protecting effect on the acute kidney injury caused by the cis-platinum is discovered for the first time, a mechanism of the 18 beta-glycyrrhetinic acid is related to inhibiting of apoptosis of the renal tubular epithelial cells, and a novel potential drug is provided for Chinese medicine anti-cancer adjuvant therapy.