A very toxic anthracycline-type antineoplastic related to DAUNORUBICIN, obtained from Actinomadura carminata.
Exclusive legal rights or privileges applied to inventions, plants, etc.
The process that reverts CELL NUCLEI of fully differentiated somatic cells to a pluripotent or totipotent state. This process can be achieved to a certain extent by NUCLEAR TRANSFER TECHNIQUES, such as fusing somatic cell nuclei with enucleated pluripotent embryonic stem cells or enucleated totipotent oocytes. GENE EXPRESSION PROFILING of the fused hybrid cells is used to determine the degree of reprogramming. Dramatic results of nuclear reprogramming include the generation of cloned mammals, such as Dolly the sheep in 1997.
A genetic process by which the adult organism is realized via mechanisms that lead to the restriction in the possible fates of cells, eventually leading to their differentiated state. Mechanisms involved cause heritable changes to cells without changes to DNA sequence such as DNA METHYLATION; HISTONE modification; DNA REPLICATION TIMING; NUCLEOSOME positioning; and heterochromatization which result in selective gene expression or repression.
A novel composition, device, or process, independently conceived de novo or derived from a pre-existing model.
The segment of GASTROINTESTINAL TRACT that includes the small intestine below the DUODENUM, and the LARGE INTESTINE.
The outward appearance of the individual. It is the product of interactions between genes, and between the GENOTYPE and the environment.
A common and benign breast disease characterized by varying degree of fibrocystic changes in the breast tissue. There are three major patterns of morphological changes, including FIBROSIS, formation of CYSTS, and proliferation of glandular tissue (adenosis). The fibrocystic breast has a dense irregular, lumpy, bumpy consistency.
The agent of South American trypanosomiasis or CHAGAS DISEASE. Its vertebrate hosts are man and various domestic and wild animals. Insects of several species are vectors.
A nitrofuran thiazine that has been used against TRYPANOSOMIASIS.
Agents destructive to the protozoal organisms belonging to the suborder TRYPANOSOMATINA.
Infection with the protozoan parasite TRYPANOSOMA CRUZI, a form of TRYPANOSOMIASIS endemic in Central and South America. It is named after the Brazilian physician Carlos Chagas, who discovered the parasite. Infection by the parasite (positive serologic result only) is distinguished from the clinical manifestations that develop years later, such as destruction of PARASYMPATHETIC GANGLIA; CHAGAS CARDIOMYOPATHY; and dysfunction of the ESOPHAGUS or COLON.
An agency of the PUBLIC HEALTH SERVICE concerned with the overall planning, promoting, and administering of programs pertaining to maintaining standards of quality of foods, drugs, therapeutic devices, etc.
Process that is gone through in order for a drug to receive approval by a government regulatory agency. This includes any required pre-clinical or clinical testing, review, submission, and evaluation of the applications and test results, and post-marketing surveillance of the drug.
Endosseous dental implantation where implants are fitted with an abutment or where an implant with a transmucosal coronal portion is used immediately (within 1 week) after the initial extraction. Conventionally, the implantation is performed in two stages with more than two months in between the stages.
Methods of creating machines and devices.
Synthesized magnetic particles under 100 nanometers possessing many biomedical applications including DRUG DELIVERY SYSTEMS and CONTRAST AGENTS. The particles are usually coated with a variety of polymeric compounds.
Nanometer-sized particles that are nanoscale in three dimensions. They include nanocrystaline materials; NANOCAPSULES; METAL NANOPARTICLES; DENDRIMERS, and QUANTUM DOTS. The uses of nanoparticles include DRUG DELIVERY SYSTEMS and cancer targeting and imaging.
Spectroscopic method of measuring the magnetic moment of elementary particles such as atomic nuclei, protons or electrons. It is employed in clinical applications such as NMR Tomography (MAGNETIC RESONANCE IMAGING).
The study of MAGNETIC PHENOMENA.
Binary classification measures to assess test results. Sensitivity or recall rate is the proportion of true positives. Specificity is the probability of correctly determining the absence of a condition. (From Last, Dictionary of Epidemiology, 2d ed)
An amino alcohol with a long unsaturated hydrocarbon chain. Sphingosine and its derivative sphinganine are the major bases of the sphingolipids in mammals. (Dorland, 28th ed)
A group of enzymes that transfers a phosphate group onto an alcohol group acceptor. EC 2.7.1.
Derivatives of PHOSPHATIDIC ACIDS that lack one of its fatty acyl chains due to its hydrolytic removal.
A subfamily of lysophospholipid receptors with specificity for LYSOSPHINGOLIPIDS such as sphingosine-1-phosphate and sphingosine phosphorylcholine.
Derivatives of propylene glycol (1,2-propanediol). They are used as humectants and solvents in pharmaceutical preparations.
A course of study offered by an educational institution.
Any of the infectious diseases of man and other animals caused by species of MYCOBACTERIUM.
MYCOBACTERIUM infections of the lung.
Tuberculosis resistant to chemotherapy with two or more ANTITUBERCULAR AGENTS, including at least ISONIAZID and RIFAMPICIN. The problem of resistance is particularly troublesome in tuberculous OPPORTUNISTIC INFECTIONS associated with HIV INFECTIONS. It requires the use of second line drugs which are more toxic than the first line regimens. TB with isolates that have developed further resistance to at least three of the six classes of second line drugs is defined as EXTENSIVELY DRUG-RESISTANT TUBERCULOSIS.
A species of gram-positive, aerobic bacteria that produces TUBERCULOSIS in humans, other primates, CATTLE; DOGS; and some other animals which have contact with humans. Growth tends to be in serpentine, cordlike masses in which the bacilli show a parallel orientation.
Tuberculosis resistant to ISONIAZID and RIFAMPIN and at least three of the six main classes of second-line drugs (AMINOGLYCOSIDES; polypeptide agents; FLUOROQUINOLONES; THIOAMIDES; CYCLOSERINE; and PARA-AMINOSALICYLIC ACID) as defined by the CDC.
Acquiring information from a patient on past medical conditions and treatments.
The ability of bacteria to resist or to become tolerant to several structurally and functionally distinct drugs simultaneously. This resistance may be acquired through gene mutation or foreign DNA in transmissible plasmids (R FACTORS).
A hexamethyl-2,4,6-triamine derivative of 1,3,5-triazine.
Hydrolysate of DNA in which purine bases have been removed.
An anthracycline produced by Streptomyces galilaeus. It has potent antineoplastic activity.
A compound produced from succinyl-CoA and GLYCINE as an intermediate in heme synthesis. It is used as a PHOTOCHEMOTHERAPY for actinic KERATOSIS.
Genus of coniferous yew trees or shrubs, several species of which have medicinal uses. Notable is the Pacific yew, Taxus brevifolia, which is used to make the anti-neoplastic drug taxol (PACLITAXEL).
A malignancy of mature PLASMA CELLS engaging in monoclonal immunoglobulin production. It is characterized by hyperglobulinemia, excess Bence-Jones proteins (free monoclonal IMMUNOGLOBULIN LIGHT CHAINS) in the urine, skeletal destruction, bone pain, and fractures. Other features include ANEMIA; HYPERCALCEMIA; and RENAL INSUFFICIENCY.
A mercaptoethylamine compound that is endogenously derived from the COENZYME A degradative pathway. The fact that cysteamine is readily transported into LYSOSOMES where it reacts with CYSTINE to form cysteine-cysteamine disulfide and CYSTEINE has led to its use in CYSTINE DEPLETING AGENTS for the treatment of CYSTINOSIS.

Induction of MDR1 gene expression by anthracycline analogues in a human drug resistant leukaemia cell line. (1/30)

The effects of 4-demethoxydaunorubicin (idarubicin, IDA) and MX2, a new morpholino-anthracycline, on up-regulation of the MDR1 gene in the low-level multidrug resistant (MDR) cell line CEM/A7R were compared at similar concentrations (IC10, IC50 and IC90) over a short time exposure (4 and 24 h). The chemosensitivity of each drug was determined by a 3-day cell growth inhibition assay. Compared with epirubicin (EPI), IDA and MX2 were 17- and eightfold more effective in the CEM/A7R line respectively. No cross-resistance to 5-FU was seen in the CEM/A7R line. Verapamil (5 microM) and PSC 833 (1 microM), which dramatically reversed resistance to EPI in the CEM/A7R line, had no sensitizing effect on the resistance of this line to MX2, but slightly decreased resistance to IDA. The sensitivity to 5-FU was unchanged by these modulators. The induction of MDR1 mRNA expression by IDA, MX2 and 5-FU was analysed by Northern blotting and semiquantitatively assessed by scanning Northern blots on a phosphorimager. The relative level of MDR1 expression was expressed as a ratio of MDR1 mRNA to the internal RNA control glyceraldehyde-3-phosphate dehydrogenase (GAPDH). IDA, MX2 and 5-FU differentially up-regulated MDR1 mRNA in the CEM/A7R line in a dose-dependent manner. Both IDA and MX2 induced MDR1 expression within 4 h. 5-FU up-regulated MDR1 expression only when drug exposure was prolonged to 24 h. Based on MRK 16 binding, flow cytometric analysis of P-glycoprotein (Pgp) expression paralleled the increase in MDR1 mRNA levels. For the three anthracyclines, the increase in MDR1 expression was stable in cells grown in the absence of drug for more than 3 weeks after drug treatment. The induction of MDR1 expression by 5-FU was transient, associated with a rapid decrease in the increased Pgp levels which returned to baseline 72 h after the removal of 5-FU. This study demonstrates that MDR1 expression can be induced by analogues of anthracyclines not pumped by Pgp, and that this induction appears to be stable despite a 3-week drug-free period.  (+info)

KRN8602 (MX2-hydrochloride): an active new agent for the treatment of recurrent high-grade glioma. (2/30)

PURPOSE: To assess the efficacy and toxicity of KRN8602 when administered as an intravenous bolus to patients with recurrent high-grade malignant glioma. PATIENTS AND METHODS: Patients with recurrent or persistent anaplastic astrocytoma or glioblastoma multiforme who had not received recent chemotherapy or radiotherapy and were of good performance status (Eastern Cooperative Oncology Group score < or = 2) were treated with an intravenous bolus of 40 mg/m(2) KRN8602 every 28 days. Tumor responses were assessed radiologically and clinically after every second cycle of therapy. Treatment was continued until documented progression or a total of six cycles. RESULTS: A median of three cycles (range, one to six cycles) of KRN8602 was administered to 55 patients, 49 of whom received at least two cycles and were, therefore, assessable for response. The overall response rate (disease stabilization or better) was 43% (95% confidence interval, 29% to 58%). There were three complete responses, one partial response, seven minor responses, and 10 patients with stable disease. The median time to progression was 2 months (range, 1.5 to 37 months) and overall survival was 11 months (range, 1.5 to 40 months). Neutropenia was the most common toxicity, although it was generally of brief duration, and there were only seven episodes of febrile neutropenia in 176 cycles delivered. Nonhematologic toxicity was mostly gastrointestinal (nausea and vomiting, diarrhea) and events were grade 2 or lower except for a single episode of grade 3 vomiting. CONCLUSION: KRN8602 is an active new agent with minimal toxicity in the treatment of relapsed or refractory high-grade glioma. Further studies with KRN8602 in combination with other cytotoxics and in adjuvant treatment of gliomas are warranted.  (+info)

Production of new anthracycline antibiotics 1-hydroxy-oxaunomycin and 6-deoxyoxaunomycin by limited biosynthetic conversion using a daunorubicin-negative mutant. (3/30)

A limited biosynthetic conversion of some known anthracyclinones using a specific daunorubicin-nonproducing mutant provided four new anthracycline antibiotics: 1-Hydroxy-10-methoxycarbonyl-13-deoxocarminomycin; 1-hydroxy-13-deoxocarminomycin; 1-hydroxyoxaunomycin and 6-deoxyoxaunomycin. Their isolation and purification from bioconversion broth, structural determination and antitumor activities against leukemic L1210 cells are described.  (+info)

Carminomycin, 14-hydroxycarminomycin and its novel carbohydrate derivatives potently kill human tumor cells and their multidrug resistant variants. (4/30)

The new hydrophilic derivatives of 14-hydroxycarminomycin were obtained using 13-dimethyl ketal of 14-bromocarminomycin (6) as the starting compound. The reductive alkylation of 6 with melibiose or D-galactose followed by hydrolysis of the corresponding intermediate bromoketals 9 and 11 produced 3'-N-[-alpha-D-(galactopyranosyl-(1 --> 6)-O-D-1-desoxyglucit-1-yl]-14-hydroxycarminomycin (10) and 3'-N-(1-desoxy-D-galactit-1-yl)-14-hydroxycarminomycin (12), respectively. These novel derivatives 10 and 12 were less toxic than carminomycin or 14-hydroxycarminomycin for leukemia (K562) and breast carcinoma (MCF-7) cells. Importantly, carminomycin, 14-hydroxycarminomycin and compounds 10 and 12 were similarly active for wild type cells and their multidrug resistant (MDR) sublines, K562i/S9 and MCF-7Dox.  (+info)

Altered expression of topoisomerase IIalpha contributes to cross-resistant to etoposide K562/MX2 cell line by aberrant methylation. (5/30)

KRN 8602 (MX2) is a novel morpholino anthracycline derivative having the chemical structure 3'-deamino-3'-morpholino-13-deoxo-10-hydroxycarminomycin hydrochloride. To investigate the mechanisms of resistance to MX2, we established an MX2-resistant phenotype (K562/MX2) of the human myelogeneous leukaemia cell line (K562/P), by continuously exposing a suspension culture to increasing concentrations of MX2. K562/MX2 cells were more resistant to MX2 than the parent cells, and also showed cross-resistance to etoposide and doxorubicin. Topoisomerase (Topo) IIalpha protein levels in K562/MX2 cells were lower of those in K562/P cells on immunoblot analysis and decreased expression of Topo IIalpha mRNA was seen in K562/MX2 cells. Topoisomerase II catalytic activity was also reduced in the nuclear extracts from K562/MX2 cells when compared with K562/P cells. Aberrant methylated CpG of Topo IIalpha gene was observed in K562/MX2 cells when compared with the parent line on methylation-specific restriction enzyme analysis. To overcome the drug resistance to MX2 and etoposide, we investigated treatment with 5-Aza-2'-deoxycytidine (5AZ), which is a demethylating agent, in K562/MX2 cells. 5-Aza-2'-deoxycytidine treatment increased Topo IIalpha mRNA expression in K562/MX2 cells, but not in K562/P cells, and increased the cytotoxicity of MX2 and etoposide. Methylated CpG was decreased in K562/MX2 cells after 5AZ treatment. We concluded that the mechanism of drug resistance to MX2 and etoposide in K562/MX2 cells might be the combination of decreased expression of Topo IIalpha gene and increased methylation, and that 5AZ could prove to be a novel treatment for etoposide-resistant cell lines, such as K562/MX2.  (+info)

Cellular pharmacology of MX2, a new morpholino anthracycline, in human pleiotropic drug-resistant cells. (6/30)

We previously reported that MX2, a new morpholino anthracycline, showed marked effects on pleiotropic drug-resistant sublines of murine P388 leukemia in vivo as well as in vitro. In this study we examine the in vitro cytotoxicity against pleiotropic drug-resistant sublines of human tumor cell lines. MX2 was effective against multidrug-resistant sublines of four human tumor cell lines; these cells, having a 4.8- to 200-fold cross-resistance to Adriamycin (ADM) showed only a 0.7- to 2.3-fold resistance to MX2 compared with the sensitive cells. To elucidate the mechanism by which MX2 overcomes multidrug resistance, the intracellular pharmacology of MX2 in human myelogenous leukemia K562 and its ADM-resistant subline (K562/ADM) was examined. Both K562 and K562/ADM cells accumulated MX2 more easily than ADM, and the intracellular accumulation of MX2 attained a steady state in both cell lines within 30 min of incubation at 37 degrees C. The amount of MX2 that accumulated in K562/ADM at a steady state was only 1.3 times lower than that in K562. However, ADM was accumulated slowly in both cell lines compared with MX2, and the intercellular concentration reached a steady state in K562/ADM after 90 min of incubation and in K562 after more than 120 min. K562/ADM cells accumulated a 3.3-fold lower concentration of ADM than K562 after 120 min of exposure. The steady-state concentration of ADM in K562/ADM was 8.3 times lower than that of MX2. In addition, greater than 70% of MX2 was retained in both cell lines after 150 min of incubation in the absence of this drug. Verapamil, a calcium antagonist, hardly augmented the cytotoxicity of MX2 against K562/ADM, and no distinct effect of this drug on both the time course and the maximal level of accumulation of MX2 was observed. Interestingly, MX2 effectively inhibited ATP/Mg2(+)-dependent [3H]vincristine binding to K562/ADM membrane preparations, indicating that MX2 could be transported outside the cell by an active efflux pump. The high intracellular accumulation and retention of MX2 in K562/ADM through the rapid influx of the drug into the cells may be one of the reasons why MX2 circumvents pleiotropic drug resistance.  (+info)

Comparative ultrastructural studies of nucleoli of tumor cells treated with adriamycin and the newer anthracyclines, carminomycin and marcellomycin. (7/30)

This study was designed to determine the effects of several antitimor anthracyclines, including Adriamycin and its analogs, carminomycin and marcellomycin, on the ultrastructure of nucleoli of Novikoff hepatoma cells. Adriamycin and carminomycin, which are structurally related, induce nucleolar segregation following the formation of conspicuous fibrillar centers. Marcellomycin did not induce formation of nucleolar fibrillar centers. Instead, numerous microspherules formed following treatment with marcellomycin; later complete nucleolar segregation developed. The microspherules were observed to be in various stages of extrusion from the nucleolar body. This microspherule "migration" appeared to be both time and drug concentration dependent. These results show that the rate and extent of nucleolar ultrastructural aberration may be related to structural differences of the various anthracyclines.  (+info)

Carminomycin I is an apoptosis inducer that targets the Golgi complex in clear cell renal carcinoma cells. (8/30)

 (+info)

Effects of the structural analogues, adriamycin (ADM), daunomycin (DNM), carminomycin (CMM), 4-demethoxydaunomycin (4D-DNM), pyrromycin (PYM), marcellomycin (MCM), and aclacinomycin (ACM) upon total cell RNA synthesis and the appearance of total RNA and poly(A)+-RNA in the cytoplasm of uninduced Friend erythroleukemia cells were investigated. The anthracyclines inhibited cellular RNA synthesis with IC50 values of 1-3 microM (ADM, DNM), 0.3-0.5 microM (CMM, 4D-DNM, PYM), and 0.06 microM (MCM, ACM). IC50 values for the appearance of total RNA in the cytoplasm were consistently 2-3 times lower than those for total cell RNA synthesis for each anthracycline. IC50 values for the inhibition of poly(A)+-RNA in the cytoplasm by ADM, DNM, and CMM were equivalent to those for total RNA synthesis. The values for MCM and ACM were 2-3 times higher than those for total RNA synthesis. The kinetic actions of drug-induced inhibition of poly(A)+-RNA appearance in the cytoplasm and inhibition of total RNA synthesis ...
Development of industrial producers of antibacterial (ristomycin, linkomycin, apramycin, tobramycin, heliomycin, eremomycin) and antitumor (daunorubycin, carminomycin, bleomycin, olivomycin, bruneomycin) ...
There is a distinctly different electrical pattern involving the contractile cells. In this case, there is a rapid depolarisation, followed by a plateau phase and then repolarisation. This phenomenon accounts for the long refractory periods required for the cardiac muscle cells to pump blood effectively before they are capable of firing for a second time. These cardiac myocytes normally do not initiate their own electrical potential, although they can do so, but rather wait for an impulse to reach them.. Contractile cells demonstrate a much more stable resting phase than conductive cells at approximately −80 mV for cells in the atria and −90 mV for cells in the ventricles. Despite this initial difference, the other components of their action potentials are virtually identical. In both cases, when stimulated by an action potential, voltage-gated channels rapidly open, beginning the positive-feedback mechanism of depolarisation. This rapid influx of positively charged ions raises the membrane ...
The experiments revealed that the creation of a wound generates a complex series of calcium signals in the surrounding tissue: First comes a rapid influx of
Buy high quality 20-Deoxo-5-O-[3,6-dideoxy-3-(dimethylamino)-β-D-glucopyranosyl]-20-(1-piperidinyl)tylonolide 1003024-01-8 from toronto research chemicals Inc.
Overview of the California Gold Rush, the rapid influx of fortune seekers in California that began after gold was found at Sutters Mill on the American River in early 1848. The Gold Rush reached its peak in 1852. According to estimates, more than 300,000 people came to the territory during the Gold Rush.
The rapid influx of synthetic opioids into Florida is sparking an emergency warning from federal agents who say the deadly substances are seeping into cocaine supplies...
Involved in the biosynthesis of aklavinone which is an important precursor common to the formation of the clinically significant anthracyclines such as carminomycin, daunorubicin (daunomycin), rhodomycin, aclacinomycin T (aklavin) and aclacinomycin A (aclarubicin). These compounds are aromatic polyketide antibiotics that exhibit high cytotoxicity and are widely applied in the chemotherapy of a variety of cancers. Catalyzes the NADPH-specific conversion of aklaviketone to yield aklavinone. It can also convert maggiemycin and 7-oxodaunomycinone to epsilon-rhodomycinone and daunomycinone, respectively.
Myron Rolle - or one of his colleagues - picks up the phone and begins dialing. On the other end, their patients are about to get some bad news.Procedures on their benign brain tumor need to be put on hold.Treatment for their chronic degenerative spine thats causing radiculopathy has to wait.Their elective neurological surgeries have been postponed or canceled, forced to take a backseat for the time being as Massachusetts General Hospital deals with the rapid influx of
Acetylcholine (ACh) is a neurotransmitter widely distributed in the central (and also peripheral, autonomic and enteric) nervous system (CNS). In the CNS, ACh facilitates many functions, such as learning, memory, attention and motor control. When released in the synaptic cleft, ACh binds to two distinct types of receptors: Ionotropic nicotinic acetylcholine receptors (nAChR) and metabotropic muscarinic acetylcholine receptors (mAChRs). The activation of nAChR by ACh leads to the rapid influx of Na+ and Ca2+ and subsequent cellular depolarization. Activation of mAChRs is relatively slow (milliseconds to seconds) and, depending on the subtypes present (M1-M5), they directly alter cellular homeostasis of phospholipase C, inositol trisphosphate, cAMP, and free calcium. In the cleft, ACh may also be hydrolyzed by acetylcholinesterase (AChE) into choline and acetate. The choline derived from ACh hydrolysis is recovered by a presynaptic high-affinity choline transporter (CHT ...
Acetylcholine (ACh) is a neurotransmitter widely distributed in the central (and also peripheral, autonomic and enteric) nervous system (CNS). In the CNS, ACh facilitates many functions, such as learning, memory, attention and motor control. When released in the synaptic cleft, ACh binds to two distinct types of receptors: Ionotropic nicotinic acetylcholine receptors (nAChR) and metabotropic muscarinic acetylcholine receptors (mAChRs). The activation of nAChR by ACh leads to the rapid influx of Na+ and Ca2+ and subsequent cellular depolarization. Activation of mAChRs is relatively slow (milliseconds to seconds) and, depending on the subtypes present (M1-M5), they directly alter cellular homeostasis of phospholipase C, inositol trisphosphate, cAMP, and free calcium. In the cleft, ACh may also be hydrolyzed by acetylcholinesterase (AChE) into choline and acetate. The choline derived from ACh hydrolysis is recovered by a presynaptic high-affinity choline transporter (CHT ...
Acetylcholine (ACh) is a neurotransmitter widely distributed in the central (and also peripheral, autonomic and enteric) nervous system (CNS). In the CNS, ACh facilitates many functions, such as learning, memory, attention and motor control. When released in the synaptic cleft, ACh binds to two distinct types of receptors: Ionotropic nicotinic acetylcholine receptors (nAChR) and metabotropic muscarinic acetylcholine receptors (mAChRs). The activation of nAChR by ACh leads to the rapid influx of Na+ and Ca2+ and subsequent cellular depolarization. Activation of mAChRs is relatively slow (milliseconds to seconds) and, depending on the subtypes present (M1-M5), they directly alter cellular homeostasis of phospholipase C, inositol trisphosphate, cAMP, and free calcium. In the cleft, ACh may also be hydrolyzed by acetylcholinesterase (AChE) into choline and acetate. The choline derived from ACh hydrolysis is recovered by a presynaptic high-affinity choline transporter (CHT ...
Anthracycline antibiotics are inducers of an immunogenic form of apoptosis that has immunostimulatory properties because of the release of damage-associated molecular patterns. To study the mechanisms used by the innate immune system to sense this immunogenic form of cell death, we established an in vivo model of cell death induced by intraperitoneal injection of doxorubicin, a prototype of anthracyclines. The acute sterile inflammation in this model is characterized by rapid influx of neutrophils and increased levels of IL-6 and monocyte chemotactic protein-1. We demonstrate that acute inflammation induced by doxorubicin is associated with apoptosis of monocytes/macrophages and that it is specific for doxorubicin, an immunogenic chemotherapeutic. Further, the inflammatory response is significantly reduced in mice deficient in myeloid differentiation primary response gene 88 (MyD88), TLR-2 or TLR-9. Importantly, a TLR-9 antagonist reduces the recruitment of neutrophils induced by doxorubicin. By ...
The title compound (9S)-2′-O-benzoyl-9,11-[carbonylbis(oxy)]-9-deoxo-5-O-(-D-desosaminyl)-12,21-anhydro-9-hydroxyerythronolide A… Expand ...
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Euro NCAP Mazda MX-5 2015 güvenlik değerlendirmeleri: ayrıntılı sonuçlar, çarpışma testi resimleri, videoları ve yorumlar
The genotoxicity of two new anthracycline antitumor antibiotics, aclacinomycin A and marcellomycin, which are potent cytostatic agents similar to Adriamycin and daunomycin, was investigated in various assays. In contrast to Adriamycin and daunomycin, both agents were devoid of mutagenic activity in the Salmonella-microsome assay as well as in a mammalian cell assay using V79 Chinese hamster cells. In primary rat hepatocytes, aclacinomycin A was active in inducing unscheduled DNA synthesis, whereas marcellomycin was not. After single i.v. doses of the 10% lethal dose, marcellomycin (15 mg/kg) did induce mammary tumors in female Sprague-Dawley rats, whereas aclacinomycin A (15 mg/kg) proved to be nontumorigenic. In conjunction with previous data, these results indicate that: (a) cytostatic and genotoxic properties of anthracyclines can be clearly separated; (b) alkylation of the primary amino group of their sugar moieties can abolish or greatly reduce mutagenic activity; and (c) poor correlations ...
Background: Streptococcus pneumoniae (the pneumococcus) remains a leading cause of infectious mortality worldwide. Acquisition of the pneumococcus occurs at the nasopharyngeal mucosa and elicits a rapid influx of neutrophils (PMNs) to the nasal lumen. However, the pneumococcus efficiently eludes clearance by PMNs and persists in the nasopharynx weeks after the acute inflammatory response recedes, amplifying the risk of invasive disease. A growing number of studies implicate the secreted phospholipid platelet-activating factor (PAF) as an important local mediator of PMN recruitment and activation in response to mucosal infections. While the pneumococcus has been shown to secrete a cell wall-bound esterase, Pce, which efficiently hydrolyzes PAF in vitro, it remains unknown whether regulation of local PAF concentration influences pneumococcal survival during colonization. Methods: We make use of atraumatic colonization of the murine nasopharynx to model carriage in the human upper respiratory ...
0147]In another specific embodiment, the methods of the invention encompass administration of a composition of the invention in combination with the administration of one or more prophylactic/therapeutic agents that are anti-cancer agents such as, but not limited to: acivicin, aclarubicin, acodazole hydrochloride, acronine, adozelesin, aldesleukin, altretamine, ambomycin, ametantrone acetate, aminoglutethimide, amsacrine, anastrozole, anthramycin, asparaginase, asperlin, azacitidine, azetepa, azotomycin, batimastat, benzodepa, bicalutamide, bisantrene hydrochloride, bisnafide dimesylate, bizelesin, bleomycin sulfate, brequinar sodium, bropirimine, busulfan, cactinomycin, calusterone, caracemide, carbetimer, carboplatin, carmustine, carubicin hydrochloride, carzelesin, cedefingol, chlorambucil, cirolemycin, cisplatin, cladribine, crisnatol mesylate, cyclophosphamide, cytarabine, dacarbazine, dactinomycin, daunorubicin hydrochloride, decarbazine, decitabine, dexormaplatin, dezaguanine, dezaguanine ...
0164] Additional examples of anti-cancer agents (e.g., chemotherapeutic) that can be used in conjunction with the presently disclosed subject matter, including pharmaceutical compositions and dosage forms and kits of the presently disclosed subject matter, include, but are not limited to: acivicin; aclarubicin; acodazole hydrochloride; acronine; adozelesin; aldesleukin; altretamine; ambomycin; ametantrone acetate; aminoglutethimide; amsacrine; anastrozole; anthramycin; asparaginase; asperlin; azacitidine; azetepa; azotomycin; batimastat; benzodepa; bicalutamide; bisantrene hydrochloride; bisnafide dimesylate; bizelesin; bleomycin sulfate; brequinar sodium; bropirimine; busulfan; cactinomycin; calusterone; caracemide; carbetimer; carboplatin; carmustine; carubicin hydrochloride; carzelesin; cedefingol; chlorambucil; cirolemycin; cisplatin; cladribine; crisnatol mesylate; cyclophosphamide; cytarabine; dacarbazine; dactinomycin; daunorubicin hydrochloride; decitabine; dexormaplatin; dezaguanine; ...
17685523] Characterization of rhodosaminyl transfer by the AknS/AknT glycosylation complex and its use in reconstituting the biosynthetic pathway of aclacinomycin A. (J Am Chem Soc. , 2007 ...
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We have investigated the metabolism and disposition, in rabbits, of menogaril (7-OMEN), a new anthracycline antibiotic recently introduced into clinical trials. 7-OMEN was administered by rapid i.v. injection at a dosage of 2.5 mg/kg. 7-OMEN and metabolites were assayed by high performance liquid chromatography. Plasma concentrations of 7-OMEN declined in biexponential fashion with a terminal half-life of 2.7 h. The area under the plasma concentration versus time curve was 1.3 µM × h. The systemic clearance of 7-OMEN was 57.6 ml/min/kg. No metabolite of 7-OMEN was detected in plasma. At 8 h after treatment, the cumulative urinary and biliary excretions of 7-OMEN equivalents amounted to 1.3 and 3.4% of the total administered dose, respectively. 7-OMEN was the predominant fluorescent compound in urine, but four metabolites were also seen. In bile, 7-OMEN represented only 9.6% of the cumulative excretion and six metabolites were observed. Among the organs, lungs contained the highest concentrations of
Chemical Entities of Biological Interest (ChEBI) is a freely available dictionary of molecular entities focused on small chemical compounds.
110D: Anthracycline-DNA interactions at unfavourable base-pair triplet-binding sites: structures of d(CGGCCG)/daunomycin and d(TGGCCA)/adriamycin complexes.
110D: Anthracycline-DNA interactions at unfavourable base-pair triplet-binding sites: structures of d(CGGCCG)/daunomycin and d(TGGCCA)/adriamycin complexes.
... carubicin MeSH D09.408.051.059.200.175 - doxorubicin MeSH D09.408.051.059.200.175.200 - epirubicin MeSH D09.408.051.059.200.300 ...
Literature References: Anthracycline antitumor antibiotic, related to daunorubicin and doxorubicin, q.q.v. Isoln from Actinomadura carminata: G. F. Gauze et al., Antibiotiki 18, 675 (1973); M. G. Brazhnikova et al., ibid. 678. Antitumor activity: V. A. Shorin et al., ibid. 681. Physico-chemical characteristics, structure: M. G. Brazhnikova et al., J. Antibiot. 27, 254 (1974). Pharmacokinetics, pharmacodynamics, toxicity study: L. E. Goldberg et al., Antibiotiki 19, 57 (1974). Production: M. G. Brazhnikova et al., SU 508076 (1976 to Inst. Antibiot. Res., USSR), C.A. 86, 15215 (1977). Stereochemistry: eidem, J. Antibiot. 29, 469 (1976). Synthesis from daunomycinone: G. Cassinelli et al., ibid. 31, 178 (1978). Molecular pharmacology: V. H. DuVernay et al., Cancer Res. 40, 387 (1980). Analysis in human serum: S. E. Fandrich, K. A. Pittman, J. Chromatogr. 223, 155 (1981). Early clinical studies: L.H. Baker et al., Cancer Treat. Rep. 63, 899 (1979). Embryotoxicity and teratogenicity study: I. ...
Carubicin intercalates into DNA and interacts with topoisomerase II, thereby inhibiting DNA replication and repair and RNA and ... Carubicin. Known as: 5,12-naphthacenedione, 8-acetyl-10-[(3-amino-2,3,6-trideoxy-.alpha-L-lyxo-hexopyranosyl)oxy]-7,8,9,10- ...
... carubicin hydrochloride; carzelesin; cedefingol; celecoxib (COX-2-specific inhibitor); chlorambucil; cirolemycin; cisplatin; ...
... carubicin hydrochloride; carzelesin; cedefingol; chlorambucil; cirolemycin; cladribine; crisnatol mesylate; cyclophosphamide; ...
Antineoplastic (carubicin). ZINC03830923. −0.504. Antineoplastic (idarubicin). ZINC11592781. −0.472. Anabolic steroid (analogue ...
... carubicin hydrochloride; carzelesin; cedefingol; chlorambucil; cirolemycin; cisplatin; cladribine; crisnatol mesylate; ...
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... carubicin MeSH D09.408.051.059.200.175 - doxorubicin MeSH D09.408.051.059.200.175.200 - epirubicin MeSH D09.408.051.059.200.300 ...
... carubicin hydrochloride; carzelesin; cedefingol; chlorambucil; cirolemycin; cisplatin; cladribine; crisnatol mesylate; ...
Carubicin Hydrochloride; Carzelesin; Cedefingol; Chlorambucil; Cirolemycin; Cisplatin; Cladribine; Crisnatol Mesylate; ...
Carubicin Hydrochloride; Carzelesin; Cedefingol; Cirolemycin; Cisplatin; Cladribine; Crisnatol Mesylate; Cyclophosphamide; ...
... carubicin hydrochloride; carzelesin; cedefingol; celecoxib (COX-2 inhibitor); chlorambucil; cirolemycin; cisplatin; cladribine ...
Carubicin(Antineoplastic.). *Carumonam(Antibacterial.). *Carvacrol(Has been used as anti-infective; anthelmintic (Nematodes).) ...
Cactinomycin, Carubicin, Carzinophilin, Chromomycins, Dactinomycin, Daunorubicin, 6- Diazo-5-OXO-Leucine, Doxorubicin, ...
Carubicin. 1. + +. 175. Methionyl Aminopeptidases. 1. + +. 176. Pyridoxine. 1. + +. 177. Peroxidases. 1. + +. ...
... carubicin hydrochloride; carzelesin; cedefingol; chlorambucil; cirolemycin; cisplatin; cladribine; crisnatol mesylate; ...
... carubicin, carumonam, carvedilol, carzenide, carzolamide, cathine, cathinone, cefaclor, cefadroxil, cefaloniumi, cefaloram, ...
... carubicin carubicin HCl carzelesin Casodex CAT (cytosine arabinoside, Adriamycin, 6-thioguanine) CAT (cytosine arabinoside, ...
Bodrogi, I., Baki, M., Liszka, G., Frang, D., Kisbenedek, L., Gunter, A., Magasi, P., Mohacsi, L., Nemere, G., Pinter, J., Rosdy, E., Ruszinko, B., Scultety, S., Szomor, L., Wabrosch, G., Rosta, A., Sugar, J., Ringwald, G. & Eckhardt, S., jan. 1 1990, In : Magyar Urologia. 2, 2, p. 121-131 11 p.. Research output: Article ...
... carubicin hydrochloride; carzelesin; cedefingol; celecoxib (COX-2 inhibitor); chlorambucil; cirolemycin; cisplatin; cladribine ...
Carubicin Hydrochloride; Carzelesin; Cedefingol; Chlorombucil; Cirolemycin; Cisplatin; Cladribine; Crisnatol Mesylate; ...
Carubicin .. Carminomicin .. Carminomycin I .. Carminomycin II .. Carminomycin III .. Carubicin Hydrochloride .. ... Hydrochloride, Carubicin .. NSC 180,024 .. NSC 180024 .. NSC180,024 .. NSC180024 .. Carminomycin .. Karminomycin .. A very ... D04.615.562.050.200.150 Carubicin .. D04.615.562.050.200.175 Doxorubicin .. D04.615.562.050.200.175.200 Epirubicin .. D04.615. ... D09.408.051.059.200.150 Carubicin .. D09.408.051.059.200.175 Doxorubicin .. D09.408.051.059.200.175.200 Epirubicin .. D09.408. ...
Carubicin (MeSH) * Chromatography, High Pressure Liquid (MeSH) * Cross-Linking Reagents (MeSH) * DNA Adducts (MeSH) ...
Carubicin(Antineoplastic.). *Carumonam(Antibacterial.). *Carvacrol(Has been used as anti-infective; anthelmintic (Nematodes).) ...
... carubicin hydrochloride; carzelesin; cedefingol; chlorambucil; cirolemycin; cladribine; crisnatol mesylate; cyclophosphamide; ...
... carubicin hydrochloride; carzelesin; cedefingol; chlorambucil; cirolemycin; cladribine; crisnatol mesylate; cyclophosphamide; ...
carubicin*abbreviated injury scale*stroke. Genomes and Genes. *BRCA1 products*env products*GP6 products*granzyme B products* ...
Epirubicin, Pirarubicin, Zorubicin, and Carubicin. Suitable compounds have the. structures:. Other suitable anthracyclines are ...
Evens AM, Kanakry JA, Sehn LH, Kritharis A, Feldman T, Kroll A, Gascoyne RD, Abramson JS, Petrich AM, Hernandez-Ilizaliturri FJ, Al-Mansour Z, Adeimy C, Hemminger J, Bartlett NL, Mato A, Caimi PF, Advani RH, Klein AK, Nabhan C, Smith SM, Fabregas JC, Lossos IS, Press OW, Fenske TS, Friedberg JW, Vose JM, Blum KA. Gray zone lymphoma with features intermediate between classical Hodgkin lymphoma and diffuse large B-cell lymphoma: characteristics, outcomes, and prognostication among a large multicenter cohort. Am J Hematol. 2015 Sep; 90(9):778-83 ...