2011 ◽  
Vol 56 (1) ◽  
pp. 148-153 ◽  
Author(s):  
Marisa H. Miceli ◽  
Stella M. Bernardo ◽  
T. S. Neil Ku ◽  
Carla Walraven ◽  
Samuel A. Lee

ABSTRACTInfections and thromboses are the most common complications associated with central venous catheters. Suggested strategies for prevention and management of these complications include the use of heparin-coated catheters, heparin locks, and antimicrobial lock therapy. However, the effects of heparin onCandida albicansbiofilms and planktonic cells have not been previously studied. Therefore, we sought to determine thein vitroeffect of a heparin sodium preparation (HP) on biofilms and planktonic cells ofC. albicans. Because HP contains two preservatives, methyl paraben (MP) and propyl paraben (PP), these compounds and heparin sodium without preservatives (Pure-H) were also tested individually. The metabolic activity of the mature biofilm after treatment was assessed using XTT [2,3-bis-(2-methoxy-4-nitro-5-sulfophenyl)-2H-tetrazolium-5-carboxanilide] reduction and microscopy. Pure-H, MP, and PP caused up to 75, 85, and 60% reductions of metabolic activity of the mature preformedC. albicansbiofilms, respectively. Maximal efficacy against the mature biofilm was observed with HP (up to 90%) compared to the individual compounds (P< 0.0001). Pure-H, MP, and PP each inhibitedC. albicansbiofilm formation up to 90%. A complete inhibition of biofilm formation was observed with HP at 5,000 U/ml and higher. When tested against planktonic cells, each compound inhibited growth in a dose-dependent manner. These data indicated that HP, MP, PP, and Pure-H havein vitroantifungal activity againstC. albicansmature biofilms, formation of biofilms, and planktonic cells. Investigation of high-dose heparin-based strategies (e.g., heparin locks) in combination with traditional antifungal agents for the treatment and/or prevention ofC. albicansbiofilms is warranted.


Molecules ◽  
2021 ◽  
Vol 26 (11) ◽  
pp. 3213
Author(s):  
Alon Ben David ◽  
Eran Diamant ◽  
Eyal Dor ◽  
Ada Barnea ◽  
Niva Natan ◽  
...  

Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) is responsible for the coronavirus disease 2019 (COVID-19) global pandemic. The first step of viral infection is cell attachment, which is mediated by the binding of the SARS-CoV-2 receptor binding domain (RBD), part of the virus spike protein, to human angiotensin-converting enzyme 2 (ACE2). Therefore, drug repurposing to discover RBD-ACE2 binding inhibitors may provide a rapid and safe approach for COVID-19 therapy. Here, we describe the development of an in vitro RBD-ACE2 binding assay and its application to identify inhibitors of the interaction of the SARS-CoV-2 RBD to ACE2 by the high-throughput screening of two compound libraries (LOPAC®1280 and DiscoveryProbeTM). Three compounds, heparin sodium, aurintricarboxylic acid (ATA), and ellagic acid, were found to exert an effective binding inhibition, with IC50 values ranging from 0.6 to 5.5 µg/mL. A plaque reduction assay in Vero E6 cells infected with a SARS-CoV-2 surrogate virus confirmed the inhibition efficacy of heparin sodium and ATA. Molecular docking analysis located potential binding sites of these compounds in the RBD. In light of these findings, the screening system described herein can be applied to other drug libraries to discover potent SARS-CoV-2 inhibitors.


Author(s):  
Friedrich Nachtmann ◽  
Günter Atzl ◽  
Wolf Dieter Roth
Keyword(s):  

1990 ◽  
Vol 47 (7) ◽  
pp. 1567-1571
Author(s):  
Larry J. Schaaf ◽  
Dennis H. Robinson ◽  
Gregory J. Vogel ◽  
Bradley G. Wulf ◽  
Kristin D. Drda ◽  
...  
Keyword(s):  

1985 ◽  
Vol 42 (6) ◽  
pp. 1352-1355
Author(s):  
Danial E. Baker ◽  
Garold S. Yost ◽  
Vickie L. Craig ◽  
R. Keith Campbell

2016 ◽  
Vol 8 (2) ◽  
pp. 453-459 ◽  
Author(s):  
Hong Zhi Zhang ◽  
Rong Sheng Li ◽  
Ni Wang ◽  
Li Qi ◽  
Cheng Zhi Huang ◽  
...  

The fluorescence quenching of CdTe QDs could be induced by heparin sodium via hydrogen bonding, which was then recovered by lysine through a strong electrostatic interaction.


1992 ◽  
Vol 26 (10) ◽  
pp. 1211-1214 ◽  
Author(s):  
Jose A. Nieto-Rodriguez ◽  
M.A. Garcìa-Martìn ◽  
M.D. Barreda-Hernandez ◽  
M.J. Hervàs ◽  
O. Cano-Real

OBJECTIVE: To determine whether heparin sodium, when added to fluids infused through a peripheral catheter, reduces some local catheter-related problems (i.e., phlebitis, catheter obstruction, and extravasation of fluid) and extends the catheter's useful life. DESIGN: Prospective, double-blind, placebo-controlled. SETTING: Internal medicine ward of a general hospital with 400 beds. PATIENTS: Eighty-one consecutive acute collaborating patients who had a venous catheter in the forearm, inserted by nurses with more than one year of professional experience. INTERVENTION: Heparin sodium 1000 units/mL or NaCl 0.9% was added to compatible infusion fluids just before they were given to the patients. The final concentration of heparin was 1 unit/mL. MEASUREMENTS: Length of time until catheters were removed and reasons for their removal. RESULTS: The heparin group had a lower rate of local catheter-related problems than the placebo group (34.3 vs. 61.5 percent, respectively, p<0.05; 95 percent confidence interval for the difference 4.3 to 50.1 percent). The catheter's mean life in the heparin group was longer than that of the placebo group (98.9 ± 55.2 vs. 66.2 ± 47.2 h, respectively, p<0.05; 95 percent confidence interval for the difference 9.15 to 56.25 h). This effect was mainly attributable to prevention of noninflammatory catheter-related problems (e.g., obstruction, extravasation) and to a delay in the appearance of phlebitis. CONCLUSIONS: Heparin sodium, when added to infusion fluids to a final concentration of 1 unit/mL, diminishes local intravenous catheter-related problems and extends the catheter's life.


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