Comparison of a new microcrystalline dicoumarol preparation with warfarin under routine treatment conditions.

Lockner, D.; Paul, Claudia

doi:10.1111/j.1365-2125.1979.tb05910.x

Cited by 4 publications

(2 citation statements)

References 11 publications

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“…Pristine SMZ and TMP have large sizes in water and block their widespread application. Microcrystalline form is a kind of pharmaceutical preparation to improve the absorption of drugs as reported . Crystalline powder with micrometer scale is regarded as microcrystalline .…”

Section: Introductionmentioning

confidence: 99%

“…Microcrystalline form is a kind of pharmaceutical preparation to improve the absorption of drugs as reported. 28 Crystalline powder with micrometer scale is regarded as microcrystalline. 29 Through the physical deposition, these microcrystalline drugs were deposited on the surface of BCs to rapidly form one antibacterial coating, which can quickly eradicate bacteria.…”

Section: Introductionmentioning

confidence: 99%

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Facile Surface Multi-Functionalization of Biomedical Catheters with Dual-Microcrystalline Broad-Spectrum Antibacterial Drugs and Antifouling Poly(ethylene glycol) for Effective Inhibition of Bacterial Infections

Ding

Zhu

et al. 2019

ACS Appl. Bio Mater.

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With the development of biomedical materials, the widespread use of implantable medical devices such as biomedical catheters has saved lives and improved therapeutic outcomes in the clinic. Biomedical catheters (BCs) have the ability to connect the body inside and outside and are widely used in clinical sites for fluid discharging, blood indwelling, mechanical ventilating, and so on. However, catheterrelated infections (CRIs) are common nosocomial infections with high morbidity and mortality. The pathogens in the urinary tract, blood, and lung tissue carried by BCs may be the direct cause of CRIs, and the bacterial biofilm on the surface of BCs provides a notable source of persistent diseases. Microcrystalline sulfamethoxazole (SMZ) and trimethoprim (TMP) were prepared in this study to increase both the specific surface area and water-solubility of antibacterial drugs, as well as to enhance the antibacterial and antifouling effects on the surface of BCs. As-prepared drugs and the excellent antifouling agent polyethylene glycol (PEG) were then used for the functionalization of BCs. The result indicated that the sizes of microcrystalline SMZ and TMP were 0.5−3 μm, 1−5 μm, respectively. The coating of BC-PEG-drugs exhibited excellent antibacterial efficacy in culture as well as preeminent antibacterial and antifouling abilities on the surface of BCs toward Staphylococcus aureus (S. aureus) and Escherichia coli (E. coli). Moreover, the BC-PEG-drugs groups exhibited outstanding antibacterial and antifouling abilities in vivo by an animal infection model with S. aureus. This study offers a simple and effective approach for the synthesis of antibacterial and antifouling coatings that consist of microcrystalline drugs, with promising clinical applicability.

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Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Facile Surface Multi-Functionalization of Biomedical Catheters with Dual-Microcrystalline Broad-Spectrum Antibacterial Drugs and Antifouling Poly(ethylene glycol) for Effective Inhibition of Bacterial Infections

Ding

Zhu

et al. 2019

ACS Appl. Bio Mater.

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NADPH quinone oxidoreductase 1 mediates breast cancer cell resistance to thymoquinone-induced apoptosis

Sutton

Doucette

2012

Biochemical and Biophysical Research Communications

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Inhibition of Furin/Proprotein Convertase-catalyzed Surface and Intracellular Processing by Small Molecules

Komiyama

Coppola

Larsen

et al. 2009

Journal of Biological Chemistry

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Furin is a ubiquitously expressed proprotein convertase (PC) that plays a vital role in numerous disease processes including cancer metastasis, bacterial toxin activation (e.g. anthrax and Pseudomonas), and viral propagation (e.g. avian influenza and human immunodeficiency virus). To identify small molecule inhibitors of furin and related processing enzymes, we performed high-throughput screens of chemical diversity libraries utilizing both enzyme-based and cell-based assays. The screens identified partially overlapping sets of compounds that were further characterized for affinity, mechanism, and efficacy in additional cellular processing assays. Dicoumarols were identified as a class of compounds that inhibited furin non-competitively and reversibly with K i values in the micromolar range. These compounds inhibited furin/furin-like activity both at the cell surface (protecting against anthrax toxin) and in the secretory pathway (blocking processing of the metastasis factor membrane-type 1 matrix metalloproteinase/MT1-MMP) at concentrations close to K i values. Compounds tested exhibited distinct patterns of inhibition of other furin-family PCs (rat PACE4, human PC5/6 and human PC7), showing that dicoumarol derivatives might be developed as either generic or selective inhibitors of the PCs. The extensive clinical use, high bioavailability and relatively low toxicity of dicoumarols suggests that the dicoumarol structure will be a good starting point for development of drug-like inhibitors of furin and other PCs that can act both intracellularly and at the cell surface.Furin, is a subtilisin-related serine protease and member of the proprotein convertase (PCs) 4 family that functions within the secretory and endocytic pathways and at the cell surface, cleaving proproteins at clusters of basic residues, typically of the form RX(K/R)R2 (for reviews see Refs. 1-3). The specificity of furin and its yeast homologue Kex2 correlate well with the three-dimensional structures of their catalytic domains (4, 5). Ubiquitously expressed, furin has numerous known or suspected physiological substrates that include growth factors, receptors, coagulation proteins, plasma proteins (e.g. pro-von Willebrand factor), extracellular matrix components, and protease precursors (e.g. matrix metalloproteases) (2). Although the homozygous furin knock-out mouse exhibits embryonic lethality (6), analysis of liver-specific ablation suggests functional overlap with other PCs, such as PACE4, PC5/6, and PC7, that are also widely expressed and act in the constitutive secretory pathway (7). Furin activity contributes to numerous chronic pathological conditions, including Alzheimer disease (8), other non-Alzheimer cerebral amyloidoses (9), osteoarthritis (10), atherosclerosis (11), and tumor progression and malignancy (12). Moreover, activation by host cells of bacterial toxins such as anthrax toxin, Pseudomonas exotoxin A, diphtheria toxin (13), Shiga toxin (14), and Bordetella dermonecrotic toxin (15), requires cleavage by furin or other PCs. Fu...

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Comparison of a new microcrystalline dicoumarol preparation with warfarin under routine treatment conditions.

Cited by 4 publications

References 11 publications

Facile Surface Multi-Functionalization of Biomedical Catheters with Dual-Microcrystalline Broad-Spectrum Antibacterial Drugs and Antifouling Poly(ethylene glycol) for Effective Inhibition of Bacterial Infections

Facile Surface Multi-Functionalization of Biomedical Catheters with Dual-Microcrystalline Broad-Spectrum Antibacterial Drugs and Antifouling Poly(ethylene glycol) for Effective Inhibition of Bacterial Infections

NADPH quinone oxidoreductase 1 mediates breast cancer cell resistance to thymoquinone-induced apoptosis

Inhibition of Furin/Proprotein Convertase-catalyzed Surface and Intracellular Processing by Small Molecules

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