scholarly journals Antibacterial Prodrugs to Overcome Bacterial Resistance

Molecules ◽  
2020 ◽  
Vol 25 (7) ◽  
pp. 1543 ◽  
Author(s):  
Buthaina Jubeh ◽  
Zeinab Breijyeh ◽  
Rafik Karaman
Keyword(s):  
Bacterial Resistance ◽  
Active Drug ◽  
Resistant Bacteria ◽  
Drug Resistant ◽  
Pharmacological Effects ◽  
New Drug ◽  
Drug Resistant Bacteria ◽  
Drug Treatments ◽  
New Treatments ◽  
Novel Antibiotics

Bacterial resistance to present antibiotics is emerging at a high pace that makes the development of new treatments a must. At the same time, the development of novel antibiotics for resistant bacteria is a slow-paced process. Amid the massive need for new drug treatments to combat resistance, time and effort preserving approaches, like the prodrug approach, are most needed. Prodrugs are pharmacologically inactive entities of active drugs that undergo biotransformation before eliciting their pharmacological effects. A prodrug strategy can be used to revive drugs discarded due to a lack of appropriate pharmacokinetic and drug-like properties, or high host toxicity. A special advantage of the use of the prodrug approach in the era of bacterial resistance is targeting resistant bacteria by developing prodrugs that require bacterium-specific enzymes to release the active drug. In this article, we review the up-to-date implementation of prodrugs to develop medications that are active against drug-resistant bacteria.

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.

scholarly journals NATURAL ANTIMICROBIALS IN THE PIPELINE AND POSSIBLE SYNERGISM WITH ANTIBIOTICS TO OVERCOME MICROBIAL RESISTANCE

2019 ◽  
pp. 15-21
Author(s):  
EMTENAN M HANAFI ◽  
ENAS N DANIAL
Keyword(s):  
Quorum Sensing ◽  
Bioactive Compounds ◽  
Biofilm Formation ◽  
Bacterial Resistance ◽  
Resistant Bacteria ◽  
Multiple Drug ◽  
Drug Resistant ◽  
Quorum Sensing Inhibitors ◽  
Drug Resistant Bacteria ◽  
Multiple Drug Resistant

The unresponsive use of antibiotics led to the appearance of multiple drug-resistant bacteria strains. Studying the mechanism by which bacteria can resist antibiotics, the so called quorum sensing and biofilm formation, enabled the researchers to find bioactive compounds, derived from eukaryotes and prokaryotes. The disrupt of this mechanism is called quorum sensing inhibitors or quorum quenchers. This article provides an overview on the current research done on such bioactive compounds, the possible use of them as antibiotic alternatives, what are the advantage and disadvantages, the source from which it has been extracted, and how it may succeed to overcome bacterial resistance. The recommendation of researchers is to use some of these natural antimicrobial compounds combined to lower doses of antibiotics for treatment, the fastest way to limit the adverse effects of the exploitation of antibiotics and to avoid bacterial resistance.

scholarly journals Current Mechanism of Bacterial Resistance to Antimicrobials

2018 ◽  
Vol 10 (01) ◽  
pp. 55-64
Author(s):  
Sonali Gangwar ◽  
Keerti Kaushik ◽  
Maya Datt Joshi
Keyword(s):  
Molecular Mechanisms ◽  
Bacterial Resistance ◽  
Antimicrobial Agents ◽  
Multidrug Resistant ◽  
Hospital Environment ◽  
Health Concern ◽  
Resistant Bacteria ◽  
Drug Resistant ◽  
Pathogenic Variants ◽  
Drug Resistant Bacteria

Serious infectious diseases are caused by bacterial pathogens that represents a serious public health concern. Antimicrobial agents are indicated for the treatment bacterial infections.Various bacteria carries several resistance genes also called multidrug resistant (MDR). Multidrug resistant organisms have emerged not only in the hospital environment but are now often identified in community settings, suggesting the reservoirs of antibiotic resistant bacteria are present outside the hospital. Drug resistant bacteria that are selected with a single drug are also frequently multi-drug resistant against multiple structurally different drugs, thus confounding the chemotherapeutic efficacy of infectious disease caused by such pathogenic variants. The molecular mechanisms by which bacteria have common resistance to antibiotics are diverse and complex. This review highlights the mechanism of bacterial resistance to antimicrobials.

scholarly journals Metallic Antibacterial Surface Treatments of Dental and Orthopedic Materials

Materials ◽  
2020 ◽  
Vol 13 (20) ◽  
pp. 4594
Author(s):  
Rushui Bai ◽  
Liying Peng ◽  
Qiannan Sun ◽  
Yunfan Zhang ◽  
Lingyun Zhang ◽  
...  
Keyword(s):  
Antibacterial Agents ◽  
Bacterial Resistance ◽  
Antibacterial Properties ◽  
Surface Treatments ◽  
Resistant Bacteria ◽  
Drug Resistant ◽  
Clinical Issue ◽  
Drug Resistant Bacteria ◽  
Antibacterial Surface ◽  
Orthopedic Materials

The oral cavity harbors complex microbial communities, which leads to biomaterial-associated infections (BAI) during dental and orthopedic treatments. Conventional antibiotic treatments have met great challenges recently due to the increasing emergency of drug-resistant bacteria. To tackle this clinical issue, antibacterial surface treatments, containing surface modification and coatings, of dental and orthopedic materials have become an area of intensive interest now. Among various antibacterial agents used in surface treatments, metallic agents possess unique properties, mainly including broad-spectrum antibacterial properties, low potential to develop bacterial resistance, relative biocompatibility, and chemical stability. Therefore, this review mainly focuses on underlying antibacterial applications and the mechanisms of metallic agents in dentistry and orthopedics. An overview of the present review indicates that much work remains to be done to deepen the understanding of antibacterial mechanisms and potential side-effects of metallic agents.

New drug discovery strategies for targeting drug-resistant bacteria

2021 ◽  
Author(s):  
Katya B. Popova ◽  
Aikaterini Valsamatzi-Panagiotou ◽  
Robert Penchovsky
Keyword(s):  
Drug Discovery ◽  
Resistant Bacteria ◽  
Drug Resistant ◽  
New Drug ◽  
Drug Resistant Bacteria

MATHEMATICAL MODELING OF BACTERIAL RESISTANCE TO ANTIBIOTICS BY MUTATIONS AND PLASMIDS

2016 ◽  
Vol 24 (01) ◽  
pp. 129-146 ◽  
Author(s):  
EDUARDO IBARGÜEN-MONDRAGÓN ◽  
JHOANA P. ROMERO-LEITON ◽  
LOURDES ESTEVA ◽  
EDITH MARIELA BURBANO-ROSERO
Keyword(s):  
Mathematical Modeling ◽  
Bacterial Infections ◽  
Bacterial Resistance ◽  
Temporal Dynamics ◽  
Deterministic Model ◽  
Transmission Model ◽  
Resistant Bacteria ◽  
Drug Resistant ◽  
Development Of Resistance ◽  
Drug Resistant Bacteria

Diversity of drugs against bacterial infections, and development of resistance to such drugs are increasing. We formulate and analyze a deterministic model for the population dynamics of sensitive and resistant bacteria to multiple bactericidal and bacteriostatic antibiotics, assuming that drug resistance is acquired through mutations and plasmid transmission. Model equilibria are determined from qualitative analysis, and numerical simulations are used to assess temporal dynamics of sensitive and drug-resistant bacteria. The model presents three possibilities: elimination of bacteria, persistence of only resistant bacteria, or coexistence of sensitive and resistant bacteria. Evolution to one of these scenarios depends on thresholds numbers involving sensitive and resistant bacteria.

scholarly journals Antibacterial Susceptibility of Clinical Isolates of Klebsiella pneumoniae in Nigeria to Carbapenems

2021 ◽  
pp. 396-401
Author(s):  
Elijah Kolawole Oladipo ◽  
Elukunbi Hilda Awoyelu ◽  
Idowu Jesulayomi Adeosun ◽  
Abiodun A Ayandele
Keyword(s):  
Klebsiella Pneumoniae ◽  
Bacterial Resistance ◽  
Diffusion Method ◽  
Resistant Bacteria ◽  
Drug Resistant ◽  
Disc Diffusion ◽  
Disc Diffusion Method ◽  
Drug Resistant Bacteria ◽  
Recent Emergence ◽  
Antibacterial Susceptibility

The emergent bacterial resistance to antibiotics, most especially Carbapenems, has become a common phenomenon. The aim of the recent study was the observation and evaluation of the antibacterial susceptibility of Klebsiella pneumoniae in clinical specimens to different Carbapenems. One hundred isolates of K. pneumoniae isolated from different clinical sites, such as leg, caesarean section (CS), head, buttock, breast, thigh, and arm were tested. Using disc diffusion method, the isolates were tested for susceptibility to different antibiotics including Tobramycin, Ciprofloxacin, Aztreonam, Colistin sulphate, Ceftriaxone, Cefepime, Cefoxitin, Ceftazidime, Ertapenem, Meropenem, and Imipenem. The results were interpreted according to the Clinical and Laboratory Standard Institute disk diffusion standard. All K. pneumoniae isolates were highly susceptible to all classes of Carbapenems: Imipenem (99%), Meropenem (96%) and Ertapenem (91%). However, they were highly resistant to Ciprofloxacin (97%), Ceftriaxone (91%) and Tobramycin (73%).  Despite the recent emergence of multi-drug resistant bacteria to Carbapenems, this study showed that Carbapenems could still be used in treating different infections caused by multi-drug resistant K. pneumoniae.

scholarly journals Exogenous Citrulline and Glutamine Contribute to Reverse the Resistance of Salmonella to Apramycin

2021 ◽  
Vol 12 ◽  
Author(s):  
Yan Yong ◽  
Yanhong Zhou ◽  
Kexin Liu ◽  
Guochang Liu ◽  
Liqin Wu ◽  
...  
Keyword(s):  
Bacterial Resistance ◽  
Tricarboxylic Acid Cycle ◽  
Animal Health ◽  
Resistant Bacteria ◽  
Drug Resistant ◽  
Bacterial Cells ◽  
Antibiotic Resistant Bacteria ◽  
Antibiotic Resistant ◽  
Drug Resistant Bacteria

Antibiotic resistance is an increasing concern for human and animal health worldwide. Recently, the concept of reverting bacterial resistance by changing the metabolic state of antibiotic-resistant bacteria has emerged. In this study, we investigated the reversal of Apramycin resistance in Salmonella. First, non-targeted metabonomics were used to identify key differential metabolites of drug-resistant bacteria. Then, the reversal effect of exogenous substances was verified in vivo and in vitro. Finally, the underlying mechanism was studied. The results showed that the metabolites citrulline and glutamine were significantly reduced in Apramycin-resistant Salmonella. When citrulline and glutamine were added to the culture medium of drug-resistant Salmonella, the killing effect of Apramycin was restored markedly. Mechanistic studies showed that citrulline and glutamine promoted the Tricarboxylic acid cycle, produced more NADH in the bacteria, and increased the proton-motive force, thus promoting Apramycin entry into the bacterial cells, and killing the drug-resistant bacteria. This study provides a useful method to manage infections by antibiotic-resistant bacteria.

scholarly journals Trends in Resistance to Cefazolin in a Military Hospital in Alkharj

2021 ◽  
pp. 413-416
Author(s):  
Nehad J. Ahmed
Keyword(s):  
Bacterial Resistance ◽  
Enterobacter Cloacae ◽  
Resistance Rate ◽  
Military Hospital ◽  
Resistant Bacteria ◽  
Gram Negative Bacteria ◽  
Drug Resistant ◽  
Bacterial Cultures ◽  
Drug Resistant Bacteria ◽  
Susceptibility Rate

Aim: This study aimed to describe the trends in resistance to cefazolin in a military hospital in Alkharj. Methodology: This was a retrospective study that was conducted in Alkharj to describe the trends in resistance to cefazolin from 1st of January 2020 to 30th of June 2021. The results of bacterial cultures were collected from the microbiology laboratory in the hospital. Results: The susceptibility rate of gram negative bacteria to cefazolin in 2020 was more than 50% except Enterobacter cloacae (susceptibility rate=0) and that the resistance of Escherichia coli to cefazolin was increased from 36% in 2020 to 48% in 2021. The present study showed that cefazolin should not use to treat infections caused by Enterobacter cloacae because of the high resistance rate (100%). Conclusion: The present study showed that the bacterial resistance of several pathogens to cefazolin was high. It is important to monitor antimicrobial susceptibility continuously and to use antibiotics wisely to minimize emergence of drug resistant bacteria.

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