Folic acid-modified mesoporous silica nanoparticles with pH-responsiveness loaded with Amp for an enhanced effect against anti-drug-resistant bacteria by overcoming efflux pump systems

2018 ◽  
Vol 6 (7) ◽  
pp. 1923-1935 ◽  
Author(s):  
Xu Chen ◽  
Yanan Liu ◽  
Ange Lin ◽  
Na Huang ◽  
Liquan Long ◽  
...  
Keyword(s):  
Folic Acid ◽  
Multidrug Resistance ◽  
Mesoporous Silica ◽  
Efflux Pump ◽  
Mesoporous Silica Nanoparticles ◽  
Resistant Bacteria ◽  
Drug Resistant ◽  
Pump System ◽  
Drug Resistant Bacteria ◽  
Antibiotic Failure

Efflux pump system-mediated bacterial multidrug resistance is one of the main causes of antibiotic failure.

Copper nanoparticles as an efflux pump inhibitor to tackle drug resistant bacteria

RSC Advances ◽  
2015 ◽  
Vol 5 (17) ◽  
pp. 12899-12909 ◽  
Author(s):  
Lowrence Rene Christena ◽  
Vimalanathan Mangalagowri ◽  
Prabhakaran Pradheeba ◽  
Khan Behlol Ayaz Ahmed ◽  
Bastin Infanta Sandhiya Shalini ◽  
...  
Keyword(s):  
Copper Nanoparticles ◽  
Efflux Pump ◽  
Resistant Bacteria ◽  
Drug Resistant ◽  
Efflux Pump Inhibitor ◽  
Drug Resistant Bacteria

Casein capped copper nanoparticles at sub inhibitory concentrations function as an efflux pump inhibitor and restores susceptibility to antibiotics in drug resistant bacteria.

scholarly journals Mass Balance Study of the Engineered Cationic Antimicrobial Peptide, WLBU2, Following a Single Intravenous Dose of 14C-WLBU2 in Mice.

2020 ◽  
Vol 15 ◽  
Author(s):  
Jan H. Beumera ◽  
Jianxia Guo ◽  
Evan C. Ray ◽  
Jonas Scemama ◽  
Robert A. Parise ◽  
...  
Keyword(s):  
Multidrug Resistance ◽  
Antimicrobial Peptides ◽  
Mass Balance ◽  
Bacterial Infections ◽  
Resistant Bacteria ◽  
Drug Resistant ◽  
Balance Study ◽  
Drug Resistant Bacteria ◽  
Mouse Tissues ◽  
Mass Balance Study

Background: To address multidrug resistance we developed engineered cationic antimicrobial peptides (eCAPs). Lead eCAP WLBU2 displays potent activity against drug-resistant bacteria and effectively treats lethal bacterial infections in mice reducing bacterial loads to undetectable levels in diverse organs. Background: To address multidrug resistance we developed engineered cationic antimicrobial peptides (eCAPs). Lead eCAP WLBU2 displays potent activity against drug-resistant bacteria and effectively treats lethal bacterial infections in mice reducing bacterial loads to undetectable levels in diverse organs. Objective: To support development of WLBU2, we conducted a mass balance study. Methods: CD1 mice were administered 10, 15, 20 and 30 mg/kg QDx5 WLBU2 or a single dose of [14C]-WLBU2 at 15 mg/kg IV. Tolerability, tissue distribution and excretion were evaluated with liquid scintillation and HPLCradiochromatography. Results: The maximum tolerated dose of WLBU2 is 20 mg/kg IV. We could account for greater than >96% of the radioactivity distributed within mouse tissues at 5 and 15 min. By 24 h, only ~40-50% of radioactivity remained in the mice. The greatest % of the dose was present in liver, accounting for ~35% of radioactivity at 5 and 15 min, and ~ 8% of radioactivity remained at 24 h. High radioactivity was also present in kidneys, plasma, red blood cells and lungs, while less than 0.2% of radioactivity was present in brain, fat, or skeletal muscle. Urinary and fecal excretion accounted for 12.5 and 2.2% of radioactivity at 24 h. Conclusion: WLBU2 distributes widely to mouse tissues and is rapidly cleared with a terminal radioactivity half-life of 22 h, a clearance of 27.4 mL/h/kg, and a distribution volume of 0.94 L/kg. At 2-100 µg-eq/g, the concentrations of 14CWLBU2 appear high enough in the tissues to account for inhibition of microbial growth.

scholarly journals 1,2,4-Oxadiazole/2-Imidazoline Hybrids: Multi-target-directed Compounds for the Treatment of Infectious Diseases and Cancer

2019 ◽  
Vol 20 (7) ◽  
pp. 1699 ◽  
Author(s):  
Anton Shetnev ◽  
Sergey Baykov ◽  
Stanislav Kalinin ◽  
Alexandra Belova ◽  
Vladimir Sharoyko ◽  
...  
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Antibacterial Activity ◽  
Efflux Pump ◽  
Ductal Adenocarcinoma ◽  
Resistant Bacteria ◽  
Drug Resistant ◽  
Gram Negative ◽  
Drug Resistant Bacteria ◽  
Efflux Pump Inhibitors

Replacement of amide moiety with the 1,2,4-oxadiazole core in the scaffold of recently reported efflux pump inhibitors afforded a novel series of oxadiazole/2-imidazoline hybrids. The latter compounds exhibited promising antibacterial activity on both Gram-positive (Staphylococcus aureus, Bacillus subtilis) and Gram-negative (Escherichia coli, Pseudomonas fluorescens) strains. Furthermore, selected compounds markedly inhibited the growth of certain drug-resistant bacteria. Additionally, the study revealed the antiproliferative activity of several antibacterial frontrunners against pancreas ductal adenocarcinoma (PANC-1) cell line, as well as their type-selective monoamine oxidase (MAO) inhibitory profile.

Novel Antibiotics from Marine Sources

2011 ◽  
Vol 4 (3) ◽  
pp. 1446-1461 ◽  
Author(s):  
E.A. Martis ◽  
G M Doshi ◽  
G V Aggarwal ◽  
P P Shanbhag
Keyword(s):  
Pharmaceutical Industry ◽  
Resistant Bacteria ◽  
Drug Resistant ◽  
Drug Resistant Bacteria ◽  
Terrestrial Life ◽  
New Antibiotics ◽  
Antibiotic Compounds ◽  
New Generation ◽  
Novel Antibiotics ◽  
Untapped Resource

With the emergence of newer diseases, resistant forms of infectious diseases and multi-drug resistant bacteria, it has become essential to develop novel and more effective antibiotics. Current antibiotics are obtained from terrestrial life or made synthetically from intermediates. The ocean represents virtually untapped resource from which novel antibiotic compounds can be discovered. It is the marine world that will provide the pharmaceutical industry with the next generation of antibiotics. Marine antibiotics are antibiotics obtained from marine organisms. Scientists have reported the discovery of various antibiotics from marine bacteria (aplasmomycin, himalomycins, and pelagiomycins), sponges (Ara C, variabillin, strobilin, ircinin-1, aeroplysin, 3,5-dibromo-4-hydroxyphenylacetamide), coelenterates (asperidol and eunicin), mollusks (laurinterol and pachydictyol), tunicates (geranylhydroquinone and cystadytins), algae (cycloeudesmol, aeroplysinin-1(+), prepacifenol and tetrabromoheptanone), worms (tholepin and 3,5-dibromo-4-hydroxybezaldehyde), and actinomycetes (marinomycins C and D). This indicates that the marine environment, representing approximately half of the global diversity, is an enormous resource for new antibiotics and this source needs to be explored for the discovery of new generation antibiotics. The present article provides an overview of various antibiotics obtained from marine sources.

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