scholarly journals The Triprenylated Anthranoid Ferruginin A, a Promising Scaffold for the Development of Novel Antibiotics against Gram-Positive Bacteria

Antibiotics ◽  
2022 ◽  
Vol 11 (1) ◽  
pp. 84
Author(s):  
Bruno Casciaro ◽  
Francesca Ghirga ◽  
Floriana Cappiello ◽  
Valeria Vergine ◽  
Maria Rosa Loffredo ◽  
...  
Keyword(s):  
Antimicrobial Agents ◽  
Therapeutic Index ◽  
Human Keratinocytes ◽  
Bioactive Molecules ◽  
Primary Sources ◽  
Gram Negative Bacteria ◽  
Gram Positive ◽  
Substructure Search ◽  
Gram Positive Bacteria ◽  
Further Development

In today’s post-antibiotic era, the search for new antimicrobial compounds is of major importance and nature represents one of the primary sources of bioactive molecules. In this work, through a cheminformatics approach, we clustered an in-house library of natural products and their derivatives based on a combination of fingerprints and substructure search. We identified the prenylated emodine-type anthranoid ferruginin A as a novel antimicrobial compound. We tested its ability to inhibit and kill a panel of Gram-positive and Gram-negative bacteria, and compared its activity with that of two analogues, vismione B and ferruanthrone. Furthermore, the capability of these three anthranoids to disrupt staphylococcal biofilm was investigated, as well as their effect on the viability of human keratinocytes. Ferruginin A showed a potent activity against both the planktonic and biofilm forms of Gram-positive bacteria (i.e., Staphylococcus aureus and S. epidermidis) and had the best therapeutic index compared to vismione B and ferruanthrone. In conclusion, ferruginin A represents a promising scaffold for the further development of valuable antimicrobial agents.

scholarly journals Bacteriocins, Antimicrobial Peptides from Bacterial Origin: Overview of Their Biology and Their Impact against Multidrug-Resistant Bacteria

2020 ◽  
Vol 8 (5) ◽  
pp. 639 ◽  
Author(s):  
Alexis Simons ◽  
Kamel Alhanout ◽  
Raphaël E. Duval
Keyword(s):  
Antimicrobial Resistance ◽  
Bacterial Infections ◽  
Antimicrobial Agents ◽  
Multidrug Resistant ◽  
Resistant Bacteria ◽  
Gram Negative Bacteria ◽  
Multidrug Resistant Bacteria ◽  
Gram Negative ◽  
Gram Positive Bacteria ◽  
Further Development

Currently, the emergence and ongoing dissemination of antimicrobial resistance among bacteria are critical health and economic issue, leading to increased rates of morbidity and mortality related to bacterial infections. Research and development for new antimicrobial agents is currently needed to overcome this problem. Among the different approaches studied, bacteriocins seem to be a promising possibility. These molecules are peptides naturally synthesized by ribosomes, produced by both Gram-positive bacteria (GPB) and Gram-negative bacteria (GNB), which will allow these bacteriocin producers to survive in highly competitive polymicrobial environment. Bacteriocins exhibit antimicrobial activity with variable spectrum depending on the peptide, which may target several bacteria. Already used in some areas such as agro-food, bacteriocins may be considered as interesting candidates for further development as antimicrobial agents used in health contexts, particularly considering the issue of antimicrobial resistance. The aim of this review is to present an updated global report on the biology of bacteriocins produced by GPB and GNB, as well as their antibacterial activity against relevant bacterial pathogens, and especially against multidrug-resistant bacteria.

Antimicrobial Flavonoids from Artocarpus anisophyllus Miq. and Artocarpus lowii King

2014 ◽  
Vol 71 (1) ◽  
Author(s):  
Shajarahtunnur Jamil ◽  
Siti Mariam Abdul Lathiff ◽  
Siti Awanis Abdullah ◽  
Noraini Jemaon ◽  
Hasnah Mohd Sirat
Keyword(s):  
Antimicrobial Agents ◽  
Inhibition Zone ◽  
Antimicrobial Activities ◽  
Diffusion Method ◽  
Gram Negative Bacteria ◽  
Gram Positive ◽  
Gram Positive Bacteria ◽  
Qualitative Assay ◽  
Concentration Methods ◽  
Strong Antimicrobial Activity

Antimicrobial activities of flavonoids isolated from the leaves and heartwoods of Artocarpus anisophyllus Miq. and Artocarpus lowii King were evaluated. Gram positive bacteria (Staphylococcus aureus and Bacillus cereus), Gram negative bacteria (Escherichia coli and Pseudomonas putida) and fungi (Candida albicans and Candida glabrata) were used in this study. Disc diffusion method was used as the qualitative assay while minimum inhibitory concentration and minimum microbicidal concentration methods were used as the quantitative assays. Artocarpin (8) showed strong antimicrobial activity towards all bacteria with inhibition zone diameter more than 11 mm and minimum microbicidal concentration value of 0.45 mg/mL. Isobavachalcone (3) exhibited strong antibacterial activity towards Gram positive bacteria with minimum microbicidal concentration value of 0.45 mg/mL. The findings of this study revealed that the isolated flavonoids from A. anisophyllus and A. lowii have potential to be developed as antimicrobial agents.

scholarly journals Utilization of shrimp waste for the recovery of valuable bioactive compounds

2018 ◽  
Author(s):  
◽  
Nosihle Dlamini
Keyword(s):  
Polyethylene Glycol ◽  
Hydrochloric Acid ◽  
Bioactive Molecules ◽  
Gram Negative Bacteria ◽  
Shrimp Waste ◽  
Processing Waste ◽  
Gram Positive ◽  
Gram Negative ◽  
Gram Positive Bacteria ◽  
Peg 600

Shrimp waste is a major by-product of crustacean processing and represents an interesting source of bioactive molecules. In addition, its use increases the sustainability of processing fishery products. The present study reports a process developed for recovering bioactive molecules from shrimp waste through the use of chemical methods. The samples of shrimp were confirmed to be from the species Haliporoides triarthrus. The recovery of chitin was 30% of the processing waste and 30-60% chitosan (CH) from chitin. CH was characterized by FTIR analysis and exhibited a degree of deacetylation (DDA) of 72%. From the demineralization extract, CaCO3 was extracted and confirmed by FTIR. Based on a kinetic study of acid hydrolysis, it was demonstrated that chitin can be quantitatively hydrolysed into glucosamine (GlN), N-acetyl glucosamine (GlcNAc) and their respective oligomers with 32% hydrochloric acid at 60oC and qualitatively from CH with 32% hydrochloric acid at 80oC. The oligomer mixed fractions were desalted by activated charcoal extraction and the components of each fraction were analysed by TLC and HPLC. Chitooligosaccharides (COS) and N-acetly chitooligosaccharides (NAcCOS) with degrees of polymerization (DP) ranging from 2 to 6 were obtained from CH and chitin, respectively. The antimicrobial activities of chitosan, COS and NAcCOS were investigated against five gram-negative bacteria and five gram-positive bacteria. Chitosan exhibited stronger bacteriostatic effects against gram- positive bacteria than gram-negative bacteria in the presence of 1% chitosan. The oligomers showed no bacteriostatic or bactericidal effects on all tested bacteria. A total 30.74± 0.078 µg.g-1 astaxanthin was extracted with 90% acetone from the species; Haliporoides triarthrus and TLC analysis indicated that the species contained both astaxanthin and its esters. Chitosan films were obtained by solution casting of blends of chitosan with glycerol, polyethylene glycol 200 (PEG-200) and polyethylene glycol 600 (PEG-600) as plasticizers. Films were characterized by FTIR, XRD diffraction, TGA, and SEM analysis. The tensile strength and elongation at break properties of the films were also evaluated. CH films and CH/GLY blended films were translucent in appearance and the CH/PEG 200 and CH/PEG 600 films were opaque. The CH films yielded mechanically resistant films without the use of a plasticizer. These data point to the feasibility of an integrated process for isolating highly bioactive molecules, such as oligosaccharides, with a broad spectrum of applications from shrimp processing waste.

scholarly journals Antimicrobial Activity and Action Mechanisms of Arg-Rich Short Analog Peptides Designed from the C-Terminal Loop Region of American Oyster Defensin (AOD)

Marine Drugs ◽  
2021 ◽  
Vol 19 (8) ◽  
pp. 451
Author(s):  
Jung-Kil Seo ◽  
Dong-Gyun Kim ◽  
Ji-Eun Lee ◽  
Kwon-Sam Park ◽  
In-Ah Lee ◽  
...  
Keyword(s):  
Amino Acids ◽  
Antimicrobial Activity ◽  
Antimicrobial Agents ◽  
Gram Negative Bacteria ◽  
Significant Activity ◽  
Gram Positive ◽  
American Oyster ◽  
Gram Negative ◽  
Gram Positive Bacteria ◽  
Loop Region

American oyster defensin (AOD) was previously purified from acidified gill extract of the American oyster, Crassostrea virginica. AOD is composed of 38 amino acids with three disulfide bonds and exhibits strong antimicrobial activity against Gram-positive bacteria as well as significant activity against Gram-negative bacteria. Here, to develop promising peptides into antibiotic candidates, we designed five arginine-rich analogs (A0, A1, A2, A3, and A4), predicted their loop and extended strand/random structures—including nine amino acids and a disulfide bond derived from the C-terminus of AOD—and described their antimicrobial and cytotoxic effects, as well as their modes of action. In our experimental results, the A3 and A4 analogs exhibited potent antimicrobial activity against all test organisms—including four Gram-positive bacteria, six Gram-negative bacteria, and Candida albicans—without cell toxicity. A sequence of experiments, including a membrane permeabilization assay, DNA binding study, and DNA polymerization inhibition test, indicated that the two analogs (A3 and A4) possibly did not act directly on the bacterial membrane but instead interacted with intracellular components such as DNA or DNA amplification reactions. AOD analogs also showed strong bacterial inhibition activity in the plasma environment. In addition, analog-treated microbial cells clearly exhibited membrane disruption, damage, and leakage of cytoplasmic contents. Collectively, our results suggest that two analogs, A3 and A4, have potent antimicrobial activity via DNA interaction and have the potential for development into novel antimicrobial agents.

Synthesis and antimicrobial activity of sulphamethoxazole-based ureas and imidazolidine-2,4,5-triones

2015 ◽  
Vol 69 (8) ◽  
Author(s):  
Martin Krátký ◽  
Jana Mandíková ◽  
František Trejtnar ◽  
Vladimír Buchta ◽  
Jiřina Stolaříková ◽  
...  
Keyword(s):  
Fungal Pathogens ◽  
Antimicrobial Agents ◽  
Oxalyl Chloride ◽  
Atypical Mycobacteria ◽  
Gram Negative Bacteria ◽  
Gram Positive ◽  
Urea Derivatives ◽  
Gram Negative ◽  
Gram Positive Bacteria

AbstractProgression of drug resistance among bacterial and fungal pathogens justifies the development of novel antimicrobial agents. Thus, a series of novel sulphamethoxazole-based ureas and imidazolidine- 2,4,5-triones have been designed and synthesised. The urea derivatives were obtained by the reaction of sulphamethoxazole and isocyanates, and their cyclisation to imidazolidine-2,4,5-triones was performed via oxalyl chloride. All synthesised derivatives were evaluated in vitro to determine their activity against gram-positive and gram-negative bacteria, fungi, Mycobacterium tuberculosis, and atypical mycobacteria and their cytotoxicity. The growth of mycobacteria was inhibited within the range of 4-1000 μM and M. tuberculosis was the least-susceptible strain. 4-(3-Heptylureido)- N-(5-methylisoxazol-3-yl)benzenesulphonamide was identified as the most promising compound because it exhibited the highest activity against atypical mycobacteria at minimum inhibitory concentrations, from 4 μM, and with acceptable toxicity (selectivity indices for M. avium and M. kansasii higher than 16 and 62.5, respectively). Gram-positive bacteria, including methicillinresistant Staphylococcus aureus, were inhibited at concentrations starting from 125 μM, whereas the investigated derivatives exhibited almost no antifungal potency and activity against gram-negative species.

Antimicrobial Properties of α-Dicarbonyl and Related Compounds

1983 ◽  
Vol 46 (4) ◽  
pp. 325-329 ◽  
Author(s):  
J. M. JAY ◽  
G. M. RIVERS ◽  
W. E. BOISVERT
Keyword(s):  
Antimicrobial Agents ◽  
Antimicrobial Properties ◽  
Broth Culture ◽  
Plate Count ◽  
Gram Negative Bacteria ◽  
Gram Positive ◽  
Gram Negative ◽  
Gram Positive Bacteria ◽  
Plate Count Agar ◽  
Enzyme Substrate

By surface plating on plate count agar, 0.005 M (430 ppm) of the α-dicarbonyl compound, diacetyl, inhibited 28 of 40 organisms with the medium at pH 6 but only 11 at pH 8. Diacetyl was more effective against gram-negative bacteria and yeasts than non-lactic gram-positive bacteria and least effective against lactic acid bacteria. Acetoin, butanedioldiacetate and five butanediol isomers were considerably less effective than diacetyl, although all were more effective at pH 6 than 8. Diacetylmonoxime and diacetyldioxime were more effective than the diols and were less affected by pH of medium than diacetyl. Phenylglyoxal (PG) and 1,2-cyclohexanedione (CHD) ranked closest to diacetyl but, unlike the latter, they were more effective against gram-positive bacteria and less so against fungi and gram-negative bacteria. All 12 compounds were more effective against selected organisms by pour plating and in broth culture than by surface plating. Like diacetyl, CHD and PG are α, α-dicarbonyls and are widely used as arginine reactive agents resulting in the blockage of enzyme-substrate reactions. Although their antimicrobial activity may be due to this property, they apparently affect different enzymes than diacetyl because their antimicrobial spectra were different. The possibility of a class of food-use antimicrobial agents bearing α-dicarbonyl groups is suggested by the findings of this study.

scholarly journals Synthesis and Evaluation of Some Coumarin Based Schiff's Bases as Potential Antimicrobial Agents'

2012 ◽  
Vol 9 (4) ◽  
pp. 2079-2088 ◽  
Author(s):  
Vishakha Bansode ◽  
Meenakshi N. Deodhar
Keyword(s):  
Antimicrobial Activity ◽  
Antimicrobial Agents ◽  
Gram Negative Bacteria ◽  
Gram Positive ◽  
Gram Negative ◽  
Gram Positive Bacteria ◽  
H Nmr ◽  
Nmr Data ◽  
Bacteria And Fungi

A series of the title compounds 3-(4-(4, 5-dihydro-5-(substituted phenyl)-1H-3-pyrazolyl) phenylimino) methyl)-4-chloro-2H-chromen-2-one 5(a-g) have been synthesized. These compounds were characterized on the basis of their spectral (IR,1H NMR) data and evaluated for antimicrobial activityin vitroagainst gram positive bacteria, gram negative bacteria and fungi. The compound (5b) was found to be the most active with MIC of 20 µg/ml against all the tested organisms.

Rapid demonstration of septic or infectious arthritis due to Gram-negative bacteria

1992 ◽  
Vol 50 (1) ◽  
pp. 686-687
Author(s):  
Jacob S. Hanker ◽  
Paul R. Gross ◽  
Beverly L. Giammara
Keyword(s):  
Chronic Arthritis ◽  
Blood Cultures ◽  
Gram Negative Bacteria ◽  
Infectious Arthritis ◽  
Bacterial Arthritis ◽  
Gram Positive ◽  
Gram Negative ◽  
Gram Positive Bacteria

Blood cultures are positive in approximately only 50 per cent of the patients with nongonococcal bacterial infectious arthritis and about 20 per cent of those with gonococcal arthritis. But the concept that gram-negative bacteria could be involved even in chronic arthritis is well-supported. Gram stains are more definitive in staphylococcal arthritis caused by gram-positive bacteria than in bacterial arthritis due to gram-negative bacteria. In the latter situation where gram-negative bacilli are the problem, Gram stains are helpful for 50% of the patients; they are only helpful for 25% of the patients, however, where gram-negative gonococci are the problem. In arthritis due to gram-positive Staphylococci. Gramstained smears are positive for 75% of the patients.

Antibacterial activity of magnesium oxide nanoparticles prepared by Calcination method

2019 ◽  
Vol 10 (03) ◽  
Author(s):  
Elaf Ayad Kadhem ◽  
Miaad Hamzah Zghair ◽  
Sarah , Hussam H. Tizkam, Shoeb Alahmad Salih Mahdi ◽  
Hussam H. Tizkam ◽  
Shoeb Alahmad
Keyword(s):  
Antibacterial Activity ◽  
Magnesium Oxide ◽  
Diffusion Method ◽  
Oxide Nanoparticles ◽  
Gram Negative Bacteria ◽  
Gram Positive ◽  
Gram Negative ◽  
Gram Positive Bacteria ◽  
Magnesium Oxide Nanoparticles ◽  
Agar Disc

magnesium oxide nanoparticles (MgO NPs) were prepared by simple wet chemical method using different calcination temperatures. The prepared NPs were characterized by Electrostatic Discharge (ESD), Scanning Electron Microscope (SEM) and X-ray Diffraction (XRD). It demonstrates sharp intensive peak with the increase of crystallinty and increase of the size with varying morphologies with respect to increase of calcination temperature. Antibacterial studies were done on gram negative bacteria (E.coli) and gram positive bacteria (S.aureus) by agar disc diffusion method. The zones of inhibitions were found larger for gram positive bacteria than gram negative bacteria, this mean, antibacterial MgO NPs activity more active on gram positive bacteria than gram negative bacteria because of the structural differences. It was found that antibacterial activity of MgO NPs was found it has directly proportional with their concentration.

BAKTERI PADA KARANG SCLERACTINIA DI KAWASAN PERAIRAN BUNAKEN, MOROTAI DAN RAJA AMPAT

2020 ◽  
Vol 8 (1) ◽  
pp. 122
Author(s):  
Eghbert Eghbert Elvan Eghbert Elvan Ampou ◽  
Iis Iis Triyulianti ◽  
Nuryani Widagti ◽  
Suciadi Catur Nugroho ◽  
Yuli Pancawati
Keyword(s):  
Scleractinian Coral ◽  
Gram Negative Bacteria ◽  
Hard Coral ◽  
Field Sampling ◽  
Bacterial Isolation ◽  
Gram Positive ◽  
Coral Mucus ◽  
Gram Negative ◽  
Gram Positive Bacteria

Research on hard coral (Scleractinian coral) contaminated with bacteria is still not much done, especially in Indonesian waters. This study took samples of coral mucus in 2010 at 3 (three) different locations, namely Bunaken (May); Morotai (September) and Raja Ampat (November), which focused on the analysis of Research on hard coral (Scleractinian coral) contaminated with bacteria is still not much done, especially in Indonesian waters. This study took samples of coral mucus in 2010 at 3 (three) different locations, namely Bunaken (May); Morotai (September) and Raja Ampat (November), which focused on the analysis of gram-positive and gram-negative bacteria. The method used for field sampling is time swim, which is by diving at a depth of 5-10 meters for ± 30 minutes and randomly taking samples of coral mucus using siring or by taking directly on corals (reef branching). Mucus samples were analyzed by bacterial isolation in the laboratory. The result shows that there were differences between gram-positive and gram-negative bacteria in the three research sites and that gram-positive bacteria were higher or dominant. Further research that can identify the bacteria species and explain its relationship to the ecosystem is highly recommended.Keywords: Bacteria, Scleractinian coral, gram-positive and -negative, Bunaken, Morotai, Raja Ampat  AbstrakPenelitian tentang karang keras (Scleractinian coral) yang terkontaminasi bakteri masih belum banyak dilakukan, terutama di perairan Indonesia. Penelitian ini mengambil sampel mucus karang pada tahun 2010 di 3 (tiga) lokasi berbeda, yakni Bunaken (Mei); Morotai (September) dan Raja Ampat (November), yang difokuskan pada analisis bakteri gram postif dan gram negatif. Metode yang digunakan untuk pengambilan sampel di lapangan adalah time swim, yaitu dengan penyelaman pada kedalaman 5-10 meter selama ±30 menit dan mengambil sampel mucus karang secara acak menggunakan siring atau dengan mengambil langsung pada karang (fraksi cabang). Sampel mucus dianalisis dengan cara isolasi bakteri di laboratorium. Hasil analisis menunjukkan bahwa ada perbedaan antara bakteri gram positif dan gram negative di tiga lokasi survei dan bakteri gram positif lebih tinggi atau dominan. Penelitian lebih lanjut yang dapat menentukan jenis bakteri serta menjelaskan hubungannya dengan ekosistem sangat disarankan untuk dilakukan.Kata Kunci : Bakteri, Scleractinian coral, gram positif dan negatif, Bunaken, Morotai, Raja Ampat

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