240 results about "Bleomycin" patented technology

The invention discloses an application of MSC (mesenchymal stem cell) exosomes in preparation of a pharmaceutic preparation for treating PF (pulmonary fibrosis). The MSC exosomes are adopted to treat PF of a mouse, the survival rate of the mouse can be remarkably increased, the PF pulmonary lesions caused by BLM (bleomycin) are relieved, the mouse lung tissue pathological score is reduced, and accordingly, the MSC exosomes have wide application prospect in the aspect of preparation of the pharmaceutic preparation for treating PF.

The invention provides a pharmaceutical composition for treating embolism and a preparation method thereof, the pharmaceutical composition comprises a hydroxyl-contained biocompatible polymer materialand a monomer containing unsaturated double bonds and anion groups, as well as a polymer generated by polymerization reaction of an optional vinyl monomer, wherein the polymerization is initiated through free radicles, and bleomycin or pingyangmycin is combined on the anion groups of the generated polymer. The preparation method combines the bleomycin or the pingyangmycin on a carrier of the polymer, thereby being capable of fully playing the dual effects of an anti-tumor antibiotic and a hardening agent owned by the bleomycin or the pingyangmycin during the embolism treatment. The anion partof the polymer can be properly combined with the bleomycin or the pingyangmycin which is rich in amino groups, thereby not only realizing the higher drug loading, but also leading the drug in an emboliaztion agent to be exchanged by cation in human body, and further realizing the slow release. In addition, the embolic carrier of the polymer has the advantages of simple prepration technology andlow cost, thereby being applicable to large-scale industrial production.

The invention discloses an application of umbilical cord mesenchymal stem cells in preparation of a pharmaceutical preparation for treating the PF (pulmonary fibrosis). When FN-gamma pretreated mesenchymal stem cells are adopted to treat PF of mice, the survival rate of the mice can be increased obviously, BLM (bleomycin) induced PF pulmonary lesion can be relieved, the pulmonary histopathologic score of the mice can be reduced obviously, and the umbilical cord mesenchymal stem cells have broad application prospect in preparation of medicines for treating the PF.

During lung injury, p53 expression increases, inducing plasminogen activator inhibitor-1 (PAI-1) while inhibiting expression of urokinase-type plasminogen activator (uPA) and its receptor (uPAR), resulting in apoptosis of lung epithelial cells (LECs). In the bleomycin lung injury model, p53 and PAI-1 are induced while uPA and uPAR are inhibited. A 20 residue peptide DGIWKASFTTFTVTKYWFYR termed PP-1 (the Cav-1 scaffolding domain) or peptide NYHYLESSMTALYTLGH, termed PP-2, protected LECs from bleomycin-induced apoptosis in vitro and in vivo and prevented subsequent pulmonary fibrosis by attenuating lung epitheilial damage. Pharmaceutical compositions, peptide multimers and deliverable polypeptides comprising the above peptides are dislcosed. The peptides and functional variants, peptide multimers, cell-targeted polyepeptides and pharmaceutical compositions are used in methods for inhibiting apoptosis of injured or damaged lung epithelial cells and for treating acute lung injury and consequent pulmonary fibrosis.

Alkanoyl L-carnitines of the formula:where R is hydrogen or a C2-8 alkanoyl group and X- is an anion of a pharmaceutically acceptable salt, are used in conjunction with anticancer agents such as taxol or bleomycin to improve the therapeutic index and reduce side effects typical of anticancer chemotherapy.

The present invention provides a new type balloon dilation catheter which includes ballon and medication material coated on stent. Said medication material comes from one or two and more than two mixtures of heparin sodium, fiber degrading enzyme, serine proteinase, batroxobin, aspirin, genistein, hirudin and its recombined product, colchicine, sirolimus, biolimus, zotarolimus, tracrolimus, pimecrolimus, simvastatin, atorvastatin, pravastatin, ciclosporin, Anti-CD34, dexamethasone, bleomycin, plicamycin, daunomycin, mitomycin C, actinomycin D, taxol, celastrol, methopterin, 5-fluorouracil, cytarabine and 6-purinethol. The balloon is made of macromolecule nylon material, and the stimulation to blood vessel is far lower than the stent with metal structure.

The invention relates to a medicament for treating idiopathic pulmonary fibrosis. Dried ginger, schisandra, seed of snakegourd, cassia twig, bupleurum, pinellia, codonopsis pilosula, radix glycyrrhizae preparata, ginger and jujube are used as raw material medicaments and can be prepared into any common oral preparation. The medicament of the invention has the efficacy of removing evil diseases, conditioning cold and heat, relating lung qi and relieving cough and asthma, and can be used for treating the idiopathic pulmonary fibrosis. Animal test results show that the medicament of the invention can relieve abnormal change of PF I rat lung tissue, regulate free radical metabolism in a model body of rat pulmonary fibrosis, enhance the activity of GSH-Px and S0D, reduce the content of MDA and NO and effectively reduce PDGF, TGF-beta 1 and TNF-a levels in blood serum, and has the functions of preventing and treating pulmonary damage and fibrosis caused by bleomycin. Clinical tests prove that the total effective rate of the medicament for treating the idiopathic pulmonary fibrosis is up to 88.5%.

The invention relates to a preparation method and application of an ultrasonic control type anti-tumor drug delivery system. The problems that existing tumor treatment drugs are low in drug loading capacity, are leaked when delivered, are low in tumor response sensitivity, slow in release and prone to causing drug resistance, and can not be controlled in vitro are solved effectively. The ultrasonic control type anti-tumor drug delivery system is established with hollow mesoporous titanium dioxide as the base body by being internally loaded with perfluorohexane and drug bleomycin, wrapped by an endogenous biological membrane-erythrocyte membrane and modified by tumor homing peptides; a nanoscale particle size distribution drug delivery system is prepared with hollow mesoporous titanium dioxide as the base body by being internally loaded with perfluorohexane and model drug bleomycin, wrapping surfaces of hollow mesoporous titanium dioxide by RBC, and being wrapped by an endogenous biological membrane-erythrocyte membrane; a tumor drug delivery system with a remote ultrasonic control function is established by modifying tumor homing peptide NGR tail ends with diacyl lipid.

The invention provides a novel compound having a structural formula (I), and a pharmaceutically acceptable salts formed by the compound. The compound is obtained by fermentation culture of producing bacteria thereof. The compound is the novel compound of a bleomycin group, has better antitumor activity than that of the clinical bleomycin, and can be used for preparing an antitumor medicament.

The invention discloses a dual-ring hairpin probe mediate label-free strand displacement amplification method for detecting bleomycin. The method includes the steps that when bleomycin exists, a dual-ring hairpin probe fractures at a recognition site, and a triggering sequence is released; the triggering sequence and a ring part of a signal probe are combined and subjected to a strand displacement amplification reaction under the effect of a polymerase and a nicking enzyme, and finally a great number of G-four-chain sequences are generated. At the same time, a primer chain extends to open the signal probe, and therefore the G-four-chain sequences packaged in the neck of the signal probe can be exposed. Finally, NMM molecules are bound to the G-four-chain sequences to generate fluorescence signals, and bleomycin is quantified through the detected fluorescence signals. As the triggering sequence is designed at the neck of the dual-ring hairpin probe, background signals of a detection system are reduced; by combining bleomycin cutting and the strand displacement amplification reaction, bleomycin can be detected sensitively, and the detection limit is 0.34 nm. The method has the advantages of being easy to operate, free of labeling and good in specificity.

The invention relates to a recombinant bacillus subtilis for expressing cellobiose-2-epimerase based on a D-alanine defective screening marker, as well as a construction method and an application of the recombinant bacillus subtilis, belonging to the technical field of genetic engineering of enzyme. According to the invention, bacillus subtilis 1A751 is taken as an original strain, D-alanine racemase genes (dal) on the chromosome of the bacillus subtilis 1A751 strain are knocked out, so that D-alanine defective bacillus subtilis 1A751 (dal<->) is obtained; by taking cellobiose-2-epimerase (CE enzyme) from thermoanaerobacter tengcongensis as a parent, fusing a P43 promoter on the upstream of the parent to establish P43-TsCE, establishing P43-TsCE to plasmid pUB110 to obtain pUB-P43-TsCE, and replacing antibiotics resistance genes kanamycin and bleomycin on the plasmid pUB-P43-TsCE with (dal), so as to construct pUB-P43-TsCE-dal; and transforming pUB-P43-TsCE-dal into host 1A751 (dal<->), and thus obtaining the recombinant bacillus subtilis for expressing cellobiose-2-epimerase, wherein the preservation number is CCTCC NO: M 2015582. The total enzyme activity of fermentation liquor reaches 7U / mL, and thus the recombinant bacillus subtilis has an important industrial application value.

The invention relates to the technical field of biomedicines, and concretely relates to a microbial fermentation preparation method of bleomycin derivatives. The method is characterized in that SB9026 (with the preservation number of CCTCC M2011292) fermentation strains are cultured, an appropriate seed culturing medium, a fermentation culturing medium and culturing conditions are selected, pilot scale amplification of the above microbial fermentation preparation method is carried out in a fermentation tank, and the temperature, the rotating speed, the pH value and raw material supplementation are regulated to adjust in order to establish the large-scale microbial fermentation preparation method of novel active bleomycin derivatives 6'-dehydroxy-BLMs. The preparation method shortens the fermentation preparation period of the 6'-dehydroxy-BLMs, improves the fermentation yield of the 6'-dehydroxy-BLMs, increases the proportion of the 6'-dehydroxy-BLMs in total metabolites, and is convenient for subsequent separation and purification. The chemical structure of the bleomycin derivatives is represented by a general formula shown in the specification.

During lung injury, p53 expression increases, inducing plasminogen activator inhibitor-1 (PAI-1) while inhibiting expression of urokinase-type plasminogen activator (uPA) and its receptor (uPAR), resulting in apoptosis of lung epithelial cells (LECs). In the bleomycin lung injury model, p53 and PAI-1 are induced while uPA and uPAR are inhibited. A 20 residue peptide DGIWKASFTTFTVTKYWFYR termed PP-1 (the Cav-1 scaffolding domain) or peptide NYHYLESSMTALYTLGH, termed PP-2, protected LECs from bleomycin-induced apoptosis in vitro and in vivo and prevented subsequent pulmonary fibrosis by attenuating lung epitheilial damage. Pharmaceutical compositions, peptide multimers and deliverable polypeptides comprising the above peptides are dislcosed. The peptides and functional variants, peptide multimers, cell-targeted polyepeptides and pharmaceutical compositions are used in methods for inhibiting apoptosis of injured or damaged lung epithelial cells and for treating acute lung injury and consequent pulmonary fibrosis.

The invention relates to a drug application of a chemical substance wedelolactone for treatment of pulmonary fibrosis. The chemical substance wedelolactone is derived from a traditional Chinese medicine eclipta, and the structure is determined through spectral data; the wedelolactone can significantly improve the degree of model mouse lung tissue pulmonary fibrosis after intragastric administration, reduce NO (Nitrogen Oxide) and MDA (Methylene dioxyamphetamine) contents reflecting degree of lung injury, HYP (Hydroxyproline) content reflecting collagen deposition in the lung tissues, and cell factor TGF-beta 1 (Transforming Growth Factor) content causing pulmonary fibrosis, and inhibit human embryo lung fibroblast proliferation in vitro and HYP content of the human embryo lung fibroblast. In-vivo and in-vitro experiments show that wedelolactone can obviously improve bleomycin induced mouse pulmonary fibrosis, so that the wedelolactone can be taken as a novel drug for treating pulmonary fibrosis.

The invention relates to a method for detecting the content of bleomycins (BLMs), belonging to the technical fields of electrochemical luminescence and sensors. According to the method, an electrochemical luminescence agent is utilized for marking DNA (deoxyribonucleic acid) to prepare a probe (Ru-DNA), and a carboxylated carbon nanoparticle modified electrode is utilized for constructing a carboxylated carbon nanoparticle modified electrode electrochemical luminescence biosensor through a competitive effect between an electrostatic repulsion force and a pi-pi accumulation action on the basis of non-covalent-bond self-assembly principles of the DNA and the carbon nanoparticle. Target objects, namely the bleomycins, act on the DNA probes to cut the DNA, the DNA probes adsorbing on the carbon nanoparticle modified electrode are reduced, and weak electrochemical luminescence signals are generated, thereby realizing the measurement of the bleomycins. The method has the advantages of simplicity and rapidness.

The invention discloses a schizochytrium sp. genetic engineering strain overexpressing a squalene synthetase gene, as well as a construction method and application of the schizochytrium sp. genetic engineering strain. Schizochytrium sp. ATCC1381 is adopted as an original strain, an overexpression vector is constructed in escherichia coli through the means of genetic engineering, bleomycin is selected as a screening resistance gene, the highly conserved sequence 18S rRNA of eucaryon is used as a homologous arm, a linear overexpressed fragment is electro-transformed into the schizochytrium sp toobtain a genetic engineering strain with high yield of squalene, and a theoretical basis is laid for microbial produced squalene and product industrialization.

Alkanoyl L-carnitines of the formula: where R is hydrogen or a C2-8 alkanoyl group and X- is an anion of a pharmaceutically acceptable salt, are used in conjunction with anticancer agents such as taxol or bleomycin to improve the therapeutic index and reduce side effects typical of anticancer chemotherapy.

The invention discloses episomal expression vectors for Candida utilis, and a construction method and application thereof, belonging to the field of genetic engineering. The episomal expression vectors use a pichia yeast expressing vector pGAPZalphaA as a basic skeleton; the promoter of Candida utilis, the promoter of Saccharomyces cerevisiae or the promoter of Pichia pastoris is used for replacing a GAP promoter on the vector pGAPZalphaA; a G418 resistant gene is used for replacing a bleomycin gene on the vector pGAPZalphaA; and an autonomously replicating sequence of Candida utilis is inserted into the PscI site of the vector pGAPZalphaA. The expression vectors constructed in the invention contain different promoters. The objective of the invention is to construct the expression vectorsapplicable to Candida utilis, and the constructed expression vectors are applied to engineered Candida utilis strains for high-efficiency expression of foreign proteins.

The invention belongs to the traditional Chinese medicine field and relates to the preparation of effective parts of astragalus mongholicus and hedysarum polybotrys and selection thereof for pulmonary fibrosis model intervention so as to obtain further study on the effective parts having the optimal curative effect. An interstitial pulmonary fibrosis model of rats is established through modeling; and compared with the normal rats, the rats having interstitial pulmonary fibrosis have obvious difference and pathologic change typical cases in various related detection indexes and pathologic changes. The various effective parts of astragalus mongholicus and hedysarum polybotrys are capable of suppressing various related indexes of the interstitial pulmonary fibrosis model of rats induced by bleomycin and preventing the development of interstitial pulmonary fibrosis, wherein low and medium dose groups of hedysarum polybotrys flavone have the optimal effect. The degree of the effect of the effective parts of astragalus mongholicus and hedysarum polybotrys on stopping the progress of interstitial pulmonary fibrosis is related to appropriate concentrations of equivalent dugs. Through comprehensive assessment, the hedysarum polybotrys flavone is better in influence on the lung function, HA, LN, HYP and the like of the rats having interstitial pulmonary fibrosis than other effective parts.

The invention discloses a noninvasive fabricating method for a pulmonary fibrosis animal model. The method comprises the steps: the method that the bacterium solution dropping is poured inside a lower trachea through an endoscope is adopted, and a nasal zero degree 4 # hard-type endoscope, a xenon lamp cold light source and a Panasonic KS-822 video monitoring system are utilized; a rat is placed in a dryer with 26 cm diameter, and the ether anesthesia is carried out on the rat, the 200 microlitre of the medicine bleomycin is ejected inside the trachea, the medicine is fully flowed into the bronchus along with the airflow when inhaling air, elastic fixings clamped on the four limbs of the rat are removed, the rat is placed into a rat cage to wait for the anabiosis, the anabiosis period ranges from 30 sec to 60 sec, and the rat is placed into a constant temperature animal house for feeding; the activity, the feeding and the spirit conditions of the inoculated rat are observed every day, and the corresponding data is recorded.

The invention discloses application of obaculactone in preparation of drugs for treating pulmonary fibrosis, chronic pneumonia and chronic bronchitis and a chronic obstructive pulmonary disease or asthma, and further discloses the related drugs. Obaculactone can effectively and dose-dependently improve the bleomycin-induced mouse pulmonary fibrosis damage and the inflammation symptoms generated in the pathogenic process of the mouse pulmonary fibrosis damage through oral administration. Detection on collagen synthesis shows that obaculactone can dose-dependently regulate down generation of alpha-SMA and collagen, and the effect is based on inhibition of obaculactone on a TGF-beta signal channel in the mouse pulmonary fibrosis tissue. The results show that obaculactone can be applied to multiple inflammation-mediated chronic lung diseases including the pulmonary fibrosis, the chronic pneumonia, silicosis, the chronic bronchitis, the chronic obstructive pulmonary disease and the asthma.

New uses for phenylketone carboxylate compounds and substituted aromatic compounds of Formula I, Formula I.1, Formula I.2, Formula IA, Formula IB, Formula IC and Formula II and their pharmaceutical acceptable salts for the treatment of cancer. The use of a combination of two of these compounds is described and the use of the combination of one of these compounds with an anticancer agent such as decarbazine, doxorubicin, daunorubicin, cyclophosphamide, busulfex, busulfan, vinblastine, vincristine, bleomycin, etoposide, topotecan, irinotecan, taxotere, taxol, 5-fluorouracil, methotrexate, gemcitabine, cisplatin, carboplatin and chlorambucil.

The invention discloses an application of glycosyl modified polyphenol compounds as drugs for relieving paraquat poisoning and treating pulmonary fibrosis. The glycosyl modified polyphenol compounds have the structure shown in the description. The glycosyl modified polyphenol compounds have a good oxidation resistance function and a lung protection function and have a notable protection function on lung injury caused by paraquat, and a mechanism is related with reduction of formation of oxygen radicals, relieving of oxidative stress and inflammatory reaction, increase of content of GSH in blood serum and SOD in lung tissue and reduction of content of MDA and HYP in lung tissue. The glycosyl modified polyphenol compounds can effectively inhibit bleomycin-induced pulmonary fibrosis of mice,and the mechanism is related with reduction of expression of TGF-beta 1, IL-6, alpha-SMA, P-smad2, type I collagen and type III collagen in lung tissue, increase of content of GSH and SOD in blood serum and reduction of the content of HYP in lung tissue.

The invention relates to the biotechnical field, and in particular relates to a recombination cell line and a method for determining the titer of baculovirus. A construction method of the recombination cell line for determining the titer of the baculovirus comprises the following steps: constructing reporter plasmids; transfecting Sf9 insect cells through the reporter plasmids; screening the transfected Sf9 insect cells through a culture medium containing bleomycin and fetal bovine serum to obtain single cell clones; continuously screening the single cell clones through the culture medium containing the bleomycin to obtain the recombination cell line. According to the recombination cell line and the method for determining the titer of the baculovirus, the titer of the baculovirus can be quickly determined, and a determination result is accurate.

The invention discloses a method for preparing an animal pulmonary fibrosis model. According to the method, bleomycin is applied to a primate, the application dose of the bleomycin is 7 mg / Kg for each time, and application is performed once for each week and totally performed twice. The invention further provides a rhesus monkey pulmonary fibrosis model prepared with the method and an application of the rhesus monkey pulmonary fibrosis model. The rhesus monkey pulmonary fibrosis model is established successfully, an operation process is simple and easy to repeat, and the model can be used for new biotechnological drug evaluation which cannot be finished by a rodent model and has bright clinical application prospects.

The invention discloses an antioxidant application of artemisitene, and identifies artemisitene as the activator of Nrf2 for the first time in the world. In the cell level, artemisitene can activate Nrf2 and downstream antioxidant protective effect of Nrf2. In a mouse model, artemisitene can prominently inhibit the lung injury induced by bleomycin. As the chemical activator of Nrf2, artemisitene and derivatives thereof have a wide application aspect, can be used as food additive, can prevent human tissue or organism from damages caused by harmful substances or carcinogen, and can prevent or inhibit the happening, development and progress of diseases related with oxidative stress such as diabetes, cardiovascular diseases, neurodegenerative diseases, chronic kidney diseases, lung diseases, and the like.

The invention provides application of pazopanib hydrochloride to preparing medicines for treating pulmonary fibrosis diseases, and further provides a medicine composition. The medicine composition contains the pazopanib hydrochloride, excipients and pharmaceutically acceptable salt, ester and hydrates of the pazopanib hydrochloride or compositions of the salt, the ester and the hydrates. The application and the medicine composition have the advantages that excellent effects can be realized by the pazopanib hydrochloride for pulmonary fibrosis, adverse reaction can be prevented, bleomycin-induced pulmonary fibrosis in mice can be relieved, and the medicine composition has an excellent application prospect for treating, relieving and improving the pulmonary fibrosis diseases.

The invention relates to application of obakunone to preparation of a medicine for preventing and treating lung injury and pulmonary fibrosis. The medicine consists of obakunone and pharmaceutically acceptable auxiliaries and additives, wherein the obakunone accounts for 3-25% by mass of the medicine. The obakunone in the medicine can inhibit mouse lung injury and pulmonary fibrosis induced by Bleomycin and regulate lymphokine expression related to inflammation of mouse lung injury induced by Bleomycin, and not only is remarkable in effects of preventing and treating lung injury and pulmonary fibrosis, but also has the advantages of low toxicity and no liver or kidney injury.

The invention relates to a temperature-controlled sustained-release injection containing an anti-cancer drug, which consists of the anti-cancer drug and an amphiphilic block copolymer hydrogel and has the temperature-sensitive gelatinization feature, the temperature-controlled sustained-release injection is flowable liquid in the environment that is lower than the body temperature and can be automatically converted to the water-insoluble gel that can not flow and be biodegradable for absorption in an endotherm, thus allowing the drug to have the local sustained release in a tumor and maintain the effective drug concentration for a plurality of weeks to a plurality of months; the temperature-controlled sustained-release injection can be injected in the tumor or the tumor periphery or be arranged in the postoperative tumor cavity, thus significantly reducing the systemic reaction of the drug, strengthening the treatment effects of chemotherapy, radiotherapy and other non-surgical therapies, and being used for the treatment of the tumors in different stages. The anti-cancer drug can be vincristine, vinorelbine, navelbine, vindesine, vinleurosine, vinrosidine, cephalotaxine, bleomycin, daunomycin, aclarubicin, epirubicin, idarubicin, pirarubicin, valrubicin, mitomycin C, actinomycin D, losoxantrone, mitoxantrone, mitozolomide, temozolomide and so on.