91 results about "Anthracycline Antibiotics" patented technology

The invention discloses an engineering bacterium through anthracene nucleus antibiotic and appliance, which is characterized by the following: inserting or replacing restriction enzymes site of dnmV gene nucleic acid order of sky blue rufus streptomycete with antibiotic against property gene and surface cerubidin synthetic gene; blocking-up engineering bacterium of dnmV gene; or transforming expressing carrier of anthracene nucleus antibiotic synthetic gene to lead streptomycin (S.lividans)TK24; extracting expressing plasmid from S.lividans TK24; leading-in sky blue rufus streptomycete gene only with antibiotic against property gene to block dnmV gene; blocking-up abrupt change bacterium. This invention can produce cerubidin and/or analogue, such as anthracene nucleus antibiotic.

The invention discloses a two-photon fluorescence probe for detecting peroxynitrite as well as a preparation method and application of the two-photon fluorescence probe. The two-photon fluorescence probe has the structural formula as shown in the description. The two-photon fluorescence probe is named as TPNIR-FP. The two-photon fluorescence probe adopts a Nile red derivative as a fluorescent group and an alpha-keto-amide functional group as an ONOO-reaction group, can rapidly respond to ONOO- (within 10 seconds), and in addition is high in sensitivity and good in selectivity. The two-photon fluorescence probe can be applied to imaging research on ONOO- in antharcycline antibiotic induced cardiac muscle cell and cardiac muscle tissue damage.

The present invention is based, in part, on the discovery that amplification of human chromosome 8q22-23 regions and over-expression of 8q22-23 genes (e.g., LAPTM4B and YWHAZ) is associated with and predictive of resistance to anthracycline-type chemotherapy. Accordingly, the invention relates to compositions, kits, and methods for predicting the response of cancer cells, e.g., breast, prostate, lung, ovarian, pancreatic, liver, and colon malignancies to anthracyclines.

A method for treating multiple myeloma in newly diagnosed or previously treated patients is described. The method comprises administering a composition consisting of a combination of chemotherapeutic agents of an anthracycline antibiothic, preferably entrapped in a liposome, dexamethasone, and thalidomide, and, optionally, a reduced dose of vincristine.

The invention discloses a compound drug-carrying liposome as well as a preparation method and application thereof. The compound drug-carrying liposome comprises a long-circulating liposome and medicinal active ingredients coated by the long-circulating liposome, wherein the long-circulating liposome is a liposome of which the surface is modified by distearoyl phosphoethanolamine-methoxy polyethylene glycol 2000; the medicinal active ingredients refer to anthracycline antibiotics and resveratrol. The preparation method of the compound drug-carrying liposome comprises preparing a liposome source, the distearoyl phosphoethanolamine-methoxy polyethylene glycol 2000 and the medicinal active ingredients into the compound drug-carrying liposome, wherein the medicinal active ingredients refer to anthracycline antibiotics and resveratrol. The compound drug-carrying liposome disclosed by the invention has inhibitory activity on the development of drug-sensitive tumors, can effectively inhibit the development of chemotherapeutic drug-tolerant tumors and is small in side effect, thereby achieving a great clinical application value.

The invention relates to a biosynthesis gene cluster of kosinostatin, and in particular relates to cloning, sequencing, analysis, functional study and application of the biosynthesis gene cluster of the kosinostatin, which is an antharcycline antibiotic with antitumor activity and generated from micromonospora sp.TP-A0468. The whole gene cluster comprises 55 genes in all, that is, 17 II-type polyketone synthetase (PKS) related genes, 8 non-ribosome polypeptide synthetase (NRPS) related genes, 9 glycosyl synthetic related genes, 6 special post-modifying genes, 7 antibiotic genes, 5 conditioning genes and 3 genes without definite functions. Through the genetic manipulation of the biosynthesis genes, the biosynthesis of kosinostatin can be blocked, the output is changed, or novel compounds are produced. The gene cluster can be applied to gene engineering, protein expression, enzymatic catalytic reaction and the like of antharcycline compounds, and can also be used for finding and discovering compounds, genes or proteins for medicines, industry or agriculture.

A gene set, kit and method predict the efficiency of anthracyclines-based treatment of breast cancer.

A method of synthesizing R1, R2-substituted-4′ (ax. or eq.)-OH anthracyclines and their corresponding salts of Formula (1) from daunorubicin or N-Trifluoroacetyl-4-R1-derivatives of daunorubicin, wherein R1 is defined as H, OH, and 4′-HO is defined as ax[ial]. The method includes producing N-Trifluoroacetyl daunorubicin and treating the N-Trifluoroacetyldaunorubicin or N-Trifluoroacetyl-4-R₁-derivatives of daunorubicin, wherein R₁ is defined as H, OH, with dimethylsulfoxide activated by different acylating agents. The attained intermediate product is then treated with a strong base (ex. tertiary amines) resulting in the 4′-keto-N-Trifluoroacetyl-4-R₁ daunorubicin wherein R₁ is defined as H, OH, OMe. The 4′-keto-N-Trifluoroacetyl-4-R₁-daunorubicin is reacted with a reducing agent, a derivative of a borohydride of an alkaline metal MHBL₃ , to produce N-Trifluoroacetyl-4′-epi-4-R₁-daunorubicin. The N-Trifluoroacetyl-4′-epi-4-R₁-daunorubicin undergoes hydrolysis in a basic solution to produce a derivate of an anthoacyclin which is halogenized [by complex halogenides] to form a 14-Hal-derivative. This result is then hydrolyzed by well-known methods in the presence of a formate of an alkaline metal to form the desired final compound.

The method for synthesizing 4-R-substituted anthracycline antibiotics and corresponding salts thereof from 4-demethyldaunorubicin comprises the following steps: treating 4-demethyldaunorubicin with a sulfonating agent to form 4-demethyldaunorubicin Methyl-4-sulfonyl-R3-daunorubicin; then in an inert atmosphere, in an aprotic polar solvent, in the temperature range of about 30-100 ° C, in the presence of a transition metal catalyst to make 4- Demethyl-4-R3-sulfonyl-daunorubicin reacts with reducing agent. Then, the protected 4-desmethoxy-4-R-daunorubicin is hydrolyzed in alkaline solution to form 4-R-substituted anthracycline antibiotics. The new method eliminates the step of forming a stereospecific glycoside between the aglycone and the aminoglycoside. The method also increases the yield of the final product by up to 30 to 40%.

The invention discloses a new Chemomycin A and preparing method and drug component and application in the tumour prevention drug, which is characterized by the following: separating Angucycline from Nocardia Mediterranei Var. Kanglensis 1747-64 to obtain the product; displaying excellent anti-tumour activity in the external activity test.

The present invention discloses a nucleotide sequence which roots in an anthracycline and produces the partial gene dnrX1 and the gene fragment dnrX 2 of the dnrX 1 of streptomyces coeruleorubidus (Streptomyces coeruleorubidus), and an express vector containing the sequences. The present invention also discloses a gene disruption engineering strain which disrupts the treptomyces coeruleorubidus of the dnrX gene by adopting the express vectors with an exchange and homologous recombination method. When the gene disruption engineering strain is used to produce the anthracycline, the acidizing treatment is not required, adriacin which is not produced by a wild fungus can be produced, and the output of the adriacin and the daunorubicin can be greatly increased.

A method of treating ovarian, tubal and peritoneal cancer is revealed. It comprises administering an effective amount of a pharmaceutical composition (including a copper chelator, a platinum-based chemotherapeutic agent and an anthracycline) to a subject in need thereof for reducing concentration of intracellular copper ions and promoting activation of transcription factor Sp1 and human copper transporter 1 (hCTR1).

The invention provides preparation and applications of a pH and ATP response-type nano carrier. The pH and ATP response-type nano carrier comprises a nucleic acid nano carrier and an anti-tumor drug immobilized on the nucleic acid nano carrier; the anti-tumor drug is anthracycline antibiotics; and the nucleic acid nano carrier comprises an ATP aptamer double helix structure and an i-motif stem loop structure. The pH and ATP response-type nano carrier provided by the invention utilizes the characteristics of tumor cell high-concentration ATP to promote dissociation of aptamers and complementarysequences thereof; and utilizes the acidic environment of tumor cells to promote the i-motif conformational change and to realize the efficient and rapid release of drugs in cells.

The present invention relates to a group of novel compound Chemomicin B,C,D and its preparation method, pharmaceutical composition containing Chemomicin B,C,D as active ingredients and its uses of Chemomicin B,C,D in preparing antineoplastic drug. Chemomicin B,C,D is Angucyclinone antibiotic separated from Nocardia Mediterranei Var.Kanglensis 1747-64 culture. In vitro activity test prove Chemomicin B,C,D has strong suppressing activity for human oesophagus cancer cell KYSE150 and has good development prospect as a novel antineoplastic drug.

The invention discloses an application of anthracene nucleus antibiotic and its pharmaceutical salt for treating ocular inflammation. The invention found that the anthracene nucleus antibiotic and its pharmaceutical salt have good effect on treatment of exogenous ocular inflammation and endogenous ocular inflammation, and especially the anthracene nucleus antibiotics can be prepared to prolonged action preparations such as a nano preparation, a microballoon preparation, liposome and hydrogel, the curative effect can be directly performed on ocular surface and eye ground, the toxicity of anthracene nucleus antibiotic is reduced, administration dosage is simultaneously enlarged through ophthalmic administration by prolonged action preparations, the duration time of drug effect is long, the medicament curative effect is stronger than that of the common preparations of the anthracene nucleus antibiotic, when the ophthalmic administration is carried out, the anthracene nucleus antibiotic has good treatment effect for exogenous and endogenous ocular surface, and eye ground inflammation, and especially has good treatment effect for the ocular surface and eye ground diseases caused by external wound, so that the problems of certain eyes inflammation with long treatment and more severe eye diseases due to eyes inflammation can be solved.

The invention discloses a new compound having an anthracycline antibiotic structure, and a preparation method and an application thereof. The anthracycline antibiotic coupled nonlinear multi-block copolymer has better effects on treatment of oculopathy compared with other forms of drugs or medicaments.

The invention relates to the technical field of traditional Chinese medicines, in particular to a drug composition for preventing and treating cardiotoxicity induced by anthracycline antibiotics and application for the drug composition. Experiments prove that glycyrrhizin can weaken the cardiotoxicity caused by doxorubicin, lower a myocardial enzyme level and improve an inflammatory response, so that the lethality caused by doxorubicin cardiotoxicity is lowered, and the drug composition has the remarkable protective effect to the cardiotoxicity induced by the doxorubicin. The drug compositioncan be used for preventing and lightening the cardiotoxicity induced by anthracycline antibiotics and has the clinical practicability.

The invention provides a targeted anti-tumor drug system and a preparation method thereof. The targeted anti-tumor drug system comprises an aptamer carrier and anti-tumor drugs immobilized onto the aptamer carrier, wherein the anti-tumor drugs are anthracycline antibiotics and porphyrin; and the aptamer carrier is an aptamer subjected to annealing treatment. The targeted anti-tumor drug system andthe preparation method thereof provided by the invention aim to perform targeted loading on dual anti-tumor drugs based on the guiding role and high-selectivity effect of the aptamer, and the aim ofrealizing dual inhibition of tumor proliferation is achieved by combining chemotherapy and photodynamic therapy.

The invention relates to a novel pharmaceutical composition. Cytosine arabinoside and antharcycline antibiotics are co-encapsulated to prepare the pharmaceutical composition. The provided pharmaceutical composition can stably maintain the ratio of cytosine arabinoside to antharcycline antibiotics to be in a range in human body; the synergistic effect can be exerted maximally; and the pharmaceutical composition is used to treat proliferative diseases of a hematopoietic system, in particular, acute leukemia.

A method for the aralkylation of anthracyclins by utilizing an aralkylating agent R_3-CH₂X (for example, BnBr) in accordance with the reaction pathway describe by the scheme shown in FIG. 1. The present invention recognizes that 4-R₁, 3′-N₃-Daunomycines are suitable substrates for selective 4′-O-benzylation, yielding 4-R₁, 3′-N₃-4′-O-Aralkyl-Daunorubicines (in particular, 4′-O-Bn-Daunomycines). Thus, the present invention provides a pathway for a simple production of 4′-O-aralkylated derivatives of anthracyclines which can be effectively used to produce anthracyclines.

The invention discloses application of a flavonoid derivative GL-V9 and anthracycline antibiotics in preparation of a leukemia treatment medicine, and belongs to the technical field of medicines. It is found that the flavonoid derivative GL-V9 combined with low-dose anthracycline antibiotics can significantly inhibit growth of acute myelogenous leukemia (AML) cells, MTT experiments and U937 cell nude mouse transplantation tumor models verify that the GL-V9 and the low-dose anthracycline antibiotics can play a synergistic anti-AML effect, and the application potential of the combined administration mode in treatment of AML is prompted.