scholarly journals Antibiotics resistance - a stumbling block to antibiotics research

2019 ◽  
Vol 10 (3) ◽  
pp. 2008-2013
Author(s):  
Sivasankari Marimuthu ◽  
Arul Jayanthi Antonisamy ◽  
Sankar Malayandi ◽  
Karthikeyan Rajendran
Keyword(s):  
Antimicrobial Properties ◽  
Structural Features ◽  
Antibiotics Resistance ◽  
Antimicrobial Compounds ◽  
Resistance Development ◽  
Synthetic Compounds ◽  
Development Of Resistance ◽  
Serious Infections ◽  
New Antibiotics ◽  
Antibiotic Discovery

Antibiotics are natural or synthetic substances that inhibit the growth of infectious microorganisms and prevent from them, causing serious infections. Though the discovery of penicillin was claimed to be accidental, later on, systematic procedures for antibiotic discovery was introduced by Waksman through his streptomycin discovery. Adopting Waksman's platform, many researchers are exploring natural sources in search of antibiotics. On the other hand, the development of resistance to antibiotics is growing at a rate faster than the discovery of new antibiotics. While a number of semi synthetic and synthetic compounds with antimicrobial properties are emerging to combat the above problem, the microorganisms are in no way working inferior to resist the actions of such substances. In fact, the development of resistance by microorganisms to above said alternatives are observed at an even faster rate than the natural antimicrobial compounds obtained from microbes. The reason behind such a faster resistance development is due to the similar structural features of semi-synthetic and synthetic compounds to natural antibiotics from microbes. The treatment of infectious diseases becomes a big task and requires a greater concern nowadays to avoid increased rates of mortality. This is an alarming condition demanding for the discovery and development of new antimicrobial compounds that would end up as a better solution for the existing problem and avoid the development of resistance. This review presents the background of antibiotics discovery and resistance development and also provides an insight into the available strategies to combat the problem.

scholarly journals Antimicrobial Compounds Isolated from Endolichenic Fungi: A Review

Molecules ◽  
2021 ◽  
Vol 26 (13) ◽  
pp. 3901
Author(s):  
A. Nethma Wethalawe ◽  
Y. Vindula Alwis ◽  
Dinusha N. Udukala ◽  
Priyani A. Paranagama
Keyword(s):  
Antimicrobial Properties ◽  
Structural Features ◽  
Antimicrobial Compounds ◽  
Future Studies ◽  
Antiviral Compounds ◽  
New Antibiotics ◽  
Photosynthetic Organism ◽  
Endolichenic Fungi ◽  
The Common ◽  
Promising Source

A lichen is a symbiotic relationship between a fungus and a photosynthetic organism, which is algae or cyanobacteria. Endolichenic fungi are a group of microfungi that resides asymptomatically within the thalli of lichens. Endolichenic fungi can be recognized as luxuriant metabolic artists that produce propitious bioactive secondary metabolites. More than any other time, there is a worldwide search for new antibiotics due to the alarming increase in microbial resistance against the currently available therapeutics. Even though a few antimicrobial compounds have been isolated from endolichenic fungi, most of them have moderate activities, implying the need for further structural optimizations. Recognizing this timely need and the significance of endolichenic fungi as a promising source of antimicrobial compounds, the activity, sources and the structures of 31 antibacterial compounds, 58 antifungal compounds, two antiviral compounds and one antiplasmodial (antimalarial) compound are summarized in this review. In addition, an overview of the common scaffolds and structural features leading to the corresponding antimicrobial properties is provided as an aid for future studies. The current challenges and major drawbacks of research related to endolichenic fungi and the remedies for them have been suggested.

scholarly journals Antimicrobial Polymers: The Potential Replacement of Existing Antibiotics?

2019 ◽  
Vol 20 (11) ◽  
pp. 2747 ◽  
Author(s):  
Nor Fadhilah Kamaruzzaman ◽  
Li Peng Tan ◽  
Ruhil Hayati Hamdan ◽  
Siew Shean Choong ◽  
Weng Kin Wong ◽  
...  
Keyword(s):  
Antimicrobial Resistance ◽  
Antimicrobial Properties ◽  
Antimicrobial Activities ◽  
Direct Application ◽  
Antimicrobial Compounds ◽  
Antimicrobial Polymers ◽  
Synthetic Compounds ◽  
Global Challenge ◽  
Polymeric Carriers ◽  
Natural Peptides

Antimicrobial resistance is now considered a major global challenge; compromising medical advancements and our ability to treat infectious disease. Increased antimicrobial resistance has resulted in increased morbidity and mortality due to infectious diseases worldwide. The lack of discovery of novel compounds from natural products or new classes of antimicrobials, encouraged us to recycle discontinued antimicrobials that were previously removed from routine use due to their toxicity, e.g., colistin. Since the discovery of new classes of compounds is extremely expensive and has very little success, one strategy to overcome this issue could be the application of synthetic compounds that possess antimicrobial activities. Polymers with innate antimicrobial properties or that have the ability to be conjugated with other antimicrobial compounds create the possibility for replacement of antimicrobials either for the direct application as medicine or implanted on medical devices to control infection. Here, we provide the latest update on research related to antimicrobial polymers in the context of ESKAPE (Enterococcus faecium, Staphylococcus aureus, Klebsiella pneumoniae, Acinetobacter baumannii, Pseudomonas aeruginosa, and Enterobacter spp.) pathogens. We summarise polymer subgroups: compounds containing natural peptides, halogens, phosphor and sulfo derivatives and phenol and benzoic derivatives, organometalic polymers, metal nanoparticles incorporated into polymeric carriers, dendrimers and polymer-based guanidine. We intend to enhance understanding in the field and promote further work on the development of polymer based antimicrobial compounds.

Antimicrobial properties of actively purified secondary metabolites isolated from different marine organisms

2020 ◽  
Vol 21 ◽  
Author(s):  
Nilushi Indika Bamunu Arachchige ◽  
Fazlurrahman Khan ◽  
Young-Mog Kim
Keyword(s):  
Secondary Metabolites ◽  
Pathogenic Bacteria ◽  
Antimicrobial Agents ◽  
Bacterial Species ◽  
Antimicrobial Properties ◽  
Antimicrobial Effect ◽  
Cost Effective ◽  
Resistance Mechanisms ◽  
Marine Organisms ◽  
Antimicrobial Compounds

Background: The treatment of infection caused by pathogenic bacteria becomes one of the serious concerns globally. The failure in the treatment was found due to the exhibition of multiple resistance mechanisms against the antimicrobial agents. Emergence of resistant bacterial species has also been observed due to prolong treatment using conventional antibiotics. To combat these problems, several alternative strategies have been employed using biological and chemically synthesized compounds as antibacterial agents. Marine organisms considered as one of the potential sources for the isolation of bioactive compounds due to the easily available, cost-effective, and eco-friendly. Methods: The online search methodology was adapted for the collection of information related to the antimicrobial properties of marine-derived compounds. These compound has been isolated and purified by different purification techniques, and their structure also characterized. Furthermore, the antibacterial activities have been reported by using broth microdilution as well as disc diffusion assays. Results: The present review paper describes the antimicrobial effect of diverse secondary metabolites which are isolated and purified from the different marine organisms. The structural elucidation of each secondary metabolite has also been done in the present paper, which will help for the in silico designing of the novel and potent antimicrobial compounds. Conclusion: A thorough literature search has been made and summarizes the list of antimicrobial compounds that are isolated from both prokaryotic and eukaryotic marine organisms. The information obtained from the present paper will be helpful for the application of marine compounds as antimicrobial agents against different antibiotic-resistant human pathogenic bacteria.

scholarly journals Silver (I) N-Heterocyclic Carbene Complexes: A Winning and Broad Spectrum of Antimicrobial Properties

2021 ◽  
Vol 22 (5) ◽  
pp. 2497
Author(s):  
Filippo Prencipe ◽  
Anna Zanfardino ◽  
Michela Di Napoli ◽  
Filomena Rossi ◽  
Stefano D’Errico ◽  
...  
Keyword(s):  
Bacterial Infections ◽  
Antimicrobial Agents ◽  
Antimicrobial Properties ◽  
Resistance Mechanisms ◽  
Heterocyclic Carbenes ◽  
Significant Activity ◽  
Bacterial Strains ◽  
Development Of Resistance ◽  
Starting Point ◽  
Catalytic Chemistry

The evolution of antibacterial resistance has arisen as the main downside in fighting bacterial infections pushing researchers to develop novel, more potent and multimodal alternative drugs.Silver and its complexes have long been used as antimicrobial agents in medicine due to the lack of silver resistance and the effectiveness at low concentration as well as to their low toxicities compared to the most commonly used antibiotics. N-Heterocyclic Carbenes (NHCs) have been extensively employed to coordinate transition metals mainly for catalytic chemistry. However, more recently, NHC ligands have been applied as carrier molecules for metals in anticancer applications. In the present study we selected from literature two NHC-carbene based on acridinescaffoldand detailed nonclassicalpyrazole derived mono NHC-Ag neutral and bis NHC-Ag cationic complexes. Their inhibitor effect on bacterial strains Gram-negative and positivewas evaluated. Imidazolium NHC silver complex containing the acridine chromophore showed effectiveness at extremely low MIC values. Although pyrazole NHC silver complexes are less active than the acridine NHC-silver, they represent the first example of this class of compounds with antimicrobial properties. Moreover all complexesare not toxic and they show not significant activity againstmammalian cells (Hek lines) after 4 and 24 h. Based on our experimental evidence, we are confident that this promising class of complexes could represent a valuable starting point for developing candidates for the treatment of bacterial infections, delivering great effectiveness and avoiding the development of resistance mechanisms.

scholarly journals Development of Resistance in Wild-Type and Hypermutable Pseudomonas aeruginosa Strains Exposed to Clinical Pharmacokinetic Profiles of Meropenem and Ceftazidime Simulated In Vitro

2007 ◽  
Vol 51 (10) ◽  
pp. 3642-3649 ◽  
Author(s):  
Beate Henrichfreise ◽  
Irith Wiegand ◽  
Ingeborg Luhmer-Becker ◽  
Bernd Wiedemann
Keyword(s):  
Pseudomonas Aeruginosa ◽  
Parent Strain ◽  
Resistance Mechanisms ◽  
In Vitro Models ◽  
Wild Type ◽  
Resistance Development ◽  
Development Of Resistance ◽  
Pharmacokinetic Profiles ◽  
Mutant Prevention Concentration

ABSTRACT In this study we investigated the interplay of antibiotic pharmacokinetic profiles and the development of mutation-mediated resistance in wild-type and hypermutable Pseudomonas aeruginosa strains. We used in vitro models simulating profiles of the commonly used therapeutic drugs meropenem and ceftazidime, two agents with high levels of antipseudomonal activity said to have different potentials for stimulating resistance development. During ceftazidime treatment of the wild-type strain (PAO1), fully resistant mutants overproducing AmpC were selected rapidly and they completely replaced wild-type cells in the population. During treatment with meropenem, mutants of PAO1 were not selected as rapidly and showed only intermediate resistance due to the loss of OprD. These mutants also replaced the parent strain in the population. During the treatment of the mutator P. aeruginosa strain with meropenem, the slowly selected mutants did not accumulate several resistance mechanisms but only lost OprD and did not completely replace the parent strain in the population. Our results indicate that the commonly used dosing regimens for meropenem and ceftazidime cannot avoid the selection of mutants of wild-type and hypermutable P. aeruginosa strains. For the treatment outcome, including the prevention of resistance development, it would be beneficial for the antibiotic concentration to remain above the mutant prevention concentration for a longer period of time than it does in present regimens.

scholarly journals Population Structure, Fungicide Resistance Profile, and sdhB Mutation Frequency of Botrytis cinerea from Strawberry and Greenhouse-Grown Tomato in Greece

Plant Disease ◽  
2015 ◽  
Vol 99 (2) ◽  
pp. 240-248 ◽  
Author(s):  
Sotirios Konstantinou ◽  
Thomas Veloukas ◽  
Michaela Leroch ◽  
George Menexes ◽  
Matthias Hahn ◽  
...  
Keyword(s):  
Botrytis Cinerea ◽  
Fungicide Resistance ◽  
Sensu Stricto ◽  
Sdhb Mutation ◽  
Resistance Development ◽  
Low Frequencies ◽  
Resistance Profile ◽  
Development Of Resistance ◽  
Crete Island ◽  
Of Greece

Botrytis cinerea is a pathogen with high genetic variability that has also shown high risk for fungicide resistance development. In total, 1,169 isolates obtained from strawberry (n = 297) and tomato (n = 872) in five geographic regions of Greece were tested for their sensitivity to several botryticides. A high frequency of isolates with multiple resistance to carbendazim, cyprodinil, pyraclostrobin, and boscalid was found in isolates from strawberry. In the isolates from tomato, the predominant phenotype was that of dual resistance to carbendazim and cyprodinil in the Crete island, of single resistance to carbendazim in the region of Preveza, and of sensitive isolates in the region of Kyparissia. None of the tested isolates was found to be fludioxonil resistant. High frequencies of boscalid-resistant phenotypes were observed in the strawberry isolates, while boscalid-resistance frequency in the tomato isolates was lower. H272R was the predominant sdhB mutation, associated with resistance to boscalid, in all the sampled isolates, while other sdhB mutations were found at low frequencies. B. cinerea group S, identified by the presence of a 21-bp insertion in the transcription factor mrr1 gene, was predominant within the tomato isolates obtained from all three sampled regions, with frequencies ranging from 62 to 75% of the isolates; whereas, within strawberry isolates, B. cinerea was predominant, with frequencies of 75 to 95%. Correlations of isolate genotype and fungicide resistance profile showed that B. cinerea sensu stricto isolates were more prone to the development of resistance to boscalid compared with the Botrytis group S isolates, which may explain the observed predominance of B. cinerea sensu stricto in strawberry fields.

scholarly journals Evaluation of Resistance Development in Bemisia tabaci Genn. (Homoptera: Aleyrodidae) in Cotton against Different Insecticides

Insects ◽  
2021 ◽  
Vol 12 (11) ◽  
pp. 996
Author(s):  
Muhammad Zaryab Khalid ◽  
Sohail Ahmed ◽  
Ibrahim Al-ashkar ◽  
Ayman EL Sabagh ◽  
Liyun Liu ◽  
...  
Keyword(s):  
Bemisia Tabaci ◽  
The Other ◽  
Resistance Development ◽  
Susceptible Population ◽  
Low Level ◽  
Development Of Resistance ◽  
Major Pest ◽  
Selection For ◽  
High Level ◽  
Very High

Cotton is a major crop of Pakistan, and Bemisia tabaci (Homoptera: Aleyrodidae) is a major pest of cotton. Due to the unwise and indiscriminate use of insecticides, resistance develops more readily in the whitefly. The present study was conducted to evaluate the resistance development in the whitefly against the different insecticides that are still in use. For this purpose, the whitefly population was selected with five concentrations of each insecticide, for five generations. At G1, compared with the laboratory susceptible population, a very low level of resistance was observed against bifenthrin, cypermethrin, acetamiprid, imidacloprid, thiamethoxam, nitenpyram, chlorfenapyr, and buprofezin with a resistance ratio of 3-fold, 2-fold, 1-fold, 4-fold, 3-fold, 3-fold, 3-fold, and 3-fold, respectively. However, the selection for five generations increased the resistance to a very high level against buprofezin (127-fold), and to a high level against imidacloprid (86-fold) compared with the laboratory susceptible population. While, a moderate level of resistance was observed against cypermethrin (34-fold), thiamethoxam (34-fold), nitenpyram (30-fold), chlorfenapyr (29-fold), and acetamiprid (21-fold). On the other hand, the resistance was low against bifenthrin (18-fold) after selection for five generations. A very low level of resistance against the field population of B. tabaci, at G1, showed that these insecticides are still effective, and thus can be used under the field conditions for the management of B. tabaci. However, the proper rotation of insecticides among different groups can help to reduce the development of resistance against insecticides.

scholarly journals Comparative Study of the Effect of Solvents on the Efficacy of Neonicotinoid Insecticides Against Malaria Vector Populations Across Africa

2022 ◽  
Author(s):  
Magellan Tchouakui ◽  
Tatiane Assatse ◽  
Leon M. J. Mugenzi ◽  
Benjamin D. Menze ◽  
Daniel Nguiffo-Nguete ◽  
...  
Keyword(s):  
Democratic Republic Of Congo ◽  
Natural Populations ◽  
Resistance Mechanisms ◽  
Lower Mortality ◽  
Malaria Vectors ◽  
Cross Resistance ◽  
Metabolic Resistance ◽  
Resistance Development ◽  
Development Of Resistance ◽  
Bottle Test

Abstract Background New insecticides with a novel mode of action such as neonicotinoids have recently been recommended for public health by WHO. Resistance monitoring of such novel insecticides requires a robust protocol to monitor the development of resistance in natural populations. In this study, we comparatively used three different solvents to assess the susceptibility of malaria vectors to neonicotinoids across Africa.MethodsMosquitoes were collected from May to July 2021 from three agricultural settings in Cameroon (Njombe-Penja, Nkolondom, and Mangoum), the Democratic Republic of Congo (Ndjili-Brasserie), Ghana (Obuasi), and Uganda (Mayuge). Using the CDC bottle test, we compared the effect of three different solvents (ethanol, acetone, MERO) on the efficacy of neonicotinoids against Anopheles gambiae s.l. In addition, TaqMan assays were used to genotype key pyrethroid-resistant markers in An. gambiae and to evaluate potential cross-resistance between pyrethroids and clothianidin.ResultsLower mortality were observed when using absolute ethanol or acetone alone as solvent (11.4- 51.9% mortality in Nkolondom, 31.7- 48.2% in Mangoum, 34.6- 56.1% in Mayµge, 39.4- 45.6% in Obuasi, 83.7- 89.3% in Congo and 71.05- 95.9% in Njombe pendja) compared to acetone + MERO for which 100% mortality were observed for all the populations. Synergist assays (PBO, DEM and DEF) revealed a significant increase of mortality suggesting that metabolic resistance mechanisms are contributing to the reduced susceptibility. A negative association was observed between the L1014F-kdr mutation and clothianidin resistance with a greater frequency of homozygote resistant mosquitoes among the dead than among survivors (OR=0.5; P=0.02). However, the I114T-GSTe2 was in contrast significantly associated with a greater ability to survive clothianidin with a higher frequency of homozygote resistant among survivors than other genotypes (OR=2.10; P=0.013). ConclusionsThis study revealed a contrasted susceptibility pattern depending on the solvents with ethanol/acetone resulting to lower mortality, thus possibly overestimating resistance, whereas the MERO consistently showed a greater efficacy of neonicotinoids but it could prevent to detect early resistance development. Therefore, we recommend monitoring the susceptibility using both acetone alone and acetone+MERO (8-10µg/ml for clothianidin) to capture the accurate resistance profile of the mosquito populations.

scholarly journals Succinate dehydrogenase inhibitor (SDHI) fungicide resistance prevention strategy

2011 ◽  
Vol 64 ◽  
pp. 119-124 ◽  
Author(s):  
A.H. McKay ◽  
G.C. Hagerty ◽  
G.B. Follas ◽  
M.S. Moore ◽  
M.S. Christie ◽  
...  
Keyword(s):  
New Zealand ◽  
High Risk ◽  
Succinate Dehydrogenase ◽  
Fungicide Resistance ◽  
Fungal Pathogens ◽  
Resistance Management ◽  
Resistance Development ◽  
Development Of Resistance ◽  
Action Committee ◽  
Succinate Dehydrogenase Inhibitor

Succinate dehydrogenase inhibitor (SDHI) fungicides are currently represented in New Zealand by eight active ingredients bixafen boscalid carboxin fluaxapyroxad fluopyram isopyrazam penthiopyrad and sedaxane They are either currently registered or undergoing development in New Zealand for use against a range of ascomycete and basiodiomycete pathogens in crops including cereals ryegrass seed apples pears grapes stonefruit cucurbits and kiwifruit These fungicides are considered to have medium to high risk of resistance development and resistance management is recommended by the Fungicide Resistance Action Committee (FRAC) in Europe Guidelines are presented for use of SDHI fungicides in New Zealand to help avoid or delay the development of resistance in the fungal pathogens that they target

scholarly journals Thinking Outside the Bug: Molecular Targets and Strategies to Overcome Antibiotic Resistance

2019 ◽  
Vol 20 (6) ◽  
pp. 1255 ◽  
Author(s):  
Ana Monserrat-Martinez ◽  
Yann Gambin ◽  
Emma Sierecki
Keyword(s):  
Antibiotic Resistance ◽  
Bacterial Infections ◽  
Rational Design ◽  
Disease Onset ◽  
Resistant Bacteria ◽  
Antibiotic Resistant ◽  
New Antibiotics ◽  
Resistant Strains ◽  
Vancomycin Resistant ◽  
Antibiotic Discovery

Since their discovery in the early 20th century, antibiotics have been used as the primary weapon against bacterial infections. Due to their prophylactic effect, they are also used as part of the cocktail of drugs given to treat complex diseases such as cancer or during surgery, in order to prevent infection. This has resulted in a decrease of mortality from infectious diseases and an increase in life expectancy in the last 100 years. However, as a consequence of administering antibiotics broadly to the population and sometimes misusing them, antibiotic-resistant bacteria have appeared. The emergence of resistant strains is a global health threat to humanity. Highly-resistant bacteria like Staphylococcus aureus (methicillin-resistant) or Enterococcus faecium (vancomycin-resistant) have led to complications in intensive care units, increasing medical costs and putting patient lives at risk. The appearance of these resistant strains together with the difficulty in finding new antimicrobials has alarmed the scientific community. Most of the strategies currently employed to develop new antibiotics point towards novel approaches for drug design based on prodrugs or rational design of new molecules. However, targeting crucial bacterial processes by these means will keep creating evolutionary pressure towards drug resistance. In this review, we discuss antibiotic resistance and new options for antibiotic discovery, focusing in particular on new alternatives aiming to disarm the bacteria or empower the host to avoid disease onset.

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