Synthesis Ruthenium complexes Functionalized with Benzothiophene and their Antibacterial activity against Staphylococcus aureus

New effective antimicrobial agents with novel mode of action are urgently need due to the continued emergence of drug-resistant bacteria. Here, three ruthenium complexes functionalized with benzothiophene: [Ru(phen)2(BTPIP)](ClO4)2 (Ru(II)-1), [Ru(dmp)2(BTPIP)](ClO4)2...

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

International Journal of Molecular Sciences ◽

10.3390/ijms20071699 ◽

2019 ◽

Vol 20 (7) ◽

pp. 1699 ◽

Cited By ~ 7

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.

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Novel Seleno- and Thio-Urea Containing Dihydropyrrol-2-One Analogues as Antibacterial Agents

Antibiotics ◽

10.3390/antibiotics10030321 ◽

2021 ◽

Vol 10 (3) ◽

pp. 321

Author(s):

Shekh Sabir ◽

Tsz Tin Yu ◽

Rajesh Kuppusamy ◽

Basmah Almohaywi ◽

George Iskander ◽

...

Keyword(s):

Antibacterial Activity ◽

Antibiotic Resistance ◽

Quorum Sensing ◽

Antibacterial Agents ◽

Inhibitory Concentration ◽

Resistant Bacteria ◽

Drug Resistant ◽

Positive Bacterium ◽

Quorum Sensing Inhibition ◽

Drug Resistant Bacteria

The quorum sensing (QS) system in multi-drug-resistant bacteria such as P. aeruginosa is primarily responsible for the development of antibiotic resistance and is considered an attractive target for antimicrobial drug discovery. In this study, we synthesised a series of novel selenourea and thiourea-containing dihydropyrrol-2-one (DHP) analogues as LasR antagonists. The selenium DHP derivatives displayed significantly better quorum-sensing inhibition (QSI) activities than the corresponding sulphur analogues. The most potent analogue 3e efficiently inhibited the las QS system by 81% at 125 µM and 53% at 31 µM. Additionally, all the compounds were screened for their minimum inhibitory concentration (MIC) against the Gram-positive bacterium S. aureus, and interestingly, only the selenium analogues showed antibacterial activity, with 3c and 3e being the most potent with a MIC of 15.6 µM.

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Synergistic Antibacterial Activity of Lantana camara L., Parthenium hysterophorus L., Cannabis sativa L. and Justicia adhatoda L. Leaves Extract against Procured Multi-drug Resistant Bacteria In Vitro

European Journal of Medicinal Plants ◽

10.9734/ejmp/2021/v32i330379 ◽

2021 ◽

pp. 34-40

Author(s):

Jyoti Chandola ◽

Pooja Singh ◽

Rishabh Garg ◽

Narotam Sharma

Keyword(s):

Antibacterial Activity ◽

Medicinal Plants ◽

Cannabis Sativa ◽

Lantana Camara ◽

Parthenium Hysterophorus ◽

Resistant Bacteria ◽

Drug Resistant ◽

Drug Resistant Bacteria ◽

Weed Plants ◽

Justicia Adhatoda

The scientific study of this research has been focused on synergistic antibacterial activity of two weed plants, Lantana camara L., Parthenium hysterophorus L. alongwith two medicinal plants, Cannabis sativa L., Justicia adhatoda L. against multi- drug resistant (MDR) bacteria. Dried leaf powders of the plants were extracted using air-dried method followed by the ethanol- solvent extraction method for the crude extract of the leaves. The crude extracts were tested for antibacterial activity against three MDR bacteria, that is, one Gram positive bacteria- Staphylococcus aureus and two Gram negative bacteria- Escherichia coli and Proteus mirabilis. Out of 18 antibiotics tested against procured bacteria, Staphylococcus aureus was resistant to 10 out of 10 tested antibiotics, Escherichia coli was resistant to 4 out of 12 tested antibiotics and Proteus mirabilis was resistant to 9 out of 10 tested antibiotics. The tested weed plants and the medicinal plants when combined together showed more zone of inhibition against multidrug resistant bacteria ( Two combinations of phytochemicals Lantana camara, Cannabis sativa and Lantana camara, Cannabis sativa, Justicia adhatoda, Parthenium hysterophorus showed maximum zones of inhibition, that is, 30 mm) as compared to when these plants were tested solitarily, showing pronounced antibacterial activity. These findings showed that the antibacterial activity enhanced when they were combined together and this potential could be used against various infectious diseases with more research and modification in this area. Weed plants also holds as much importance as the medicinal plants although not to that extent, but they clearly inhibit the growth of bacteria and this property of weeds along with the medicinal plants holds a promising future in treating many diseases caused by multi-drug resistant bacteria on the pharmaceutical level.

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Quorum Sensing Inhibition in Chromobacterium violaceum, Antibacterial Activity and GC-MS Analysis of Centaurea praecox (Oliv. & Hiern) Extracts

Letters in Applied NanoBioScience ◽

10.33263/lianbs94.15691577 ◽

2020 ◽

Vol 9 (4) ◽

pp. 1569-1577

Keyword(s):

Antibacterial Activity ◽

Quorum Sensing ◽

Research Strategy ◽

Chromobacterium Violaceum ◽

Resistant Bacteria ◽

Drug Resistant ◽

Control Drug ◽

Ms Analysis ◽

Drug Resistant Bacteria

The quorum sensing (QS) mechanism has become a viable research strategy for the discovery of plant-derived anti-virulent agents to control drug-resistant bacteria. The increasing incidences of drug-resistant bacteria and the effort to curb it necessitate this study. We investigated the QS inhibitory potential of Centaurea praecox extracts on Chromobacterium violaceum (CV), antibacterial activity, and determination of chemical composition using GC-MS. C. praecox was subjected to sequential extraction using hexane (HEX), dichloromethane (DCM), ethyl acetate (EA), ethanol (ET), and aqueous (AQ) solvents. The extracts were subsequently evaluated for antibacterial activity using disc diffusion and QS violacein inhibition using spectrophotometry. The antibacterial effects of the extracts were moderate on gram-positive bacteria at 4 mg/mL in the order: HEX >EA >DCM >ET =AQ. However, the DCM extract demonstrated the most effective violacein inhibition of ≥80% at 0.3 mg/mL. QS violacein inhibitions were generally found to be concentration-dependent in the order: DCM >EA >HEX >ET =AQ with efficacies of ≥ 90% inhibition at ≥ 0.6 mg/mL. GC-MS analysis on the most potent DCM extract revealed N-vinylmethanimine, N-ethyl formamide, and propanamide among components identified. We concluded that C. praecox DCM extract contains bioactive chemicals as QS inhibitors and potential anti-virulent agents capable of combating the pathogenicity of drug-resistant bacteria in vivo.

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Vacancy‐Induced Antibacterial Activity of XS 2– y Quantum Dots against Drug‐Resistant Bacteria for Treatment of Bacterial Keratitis

Small ◽

10.1002/smll.202004677 ◽

2020 ◽

Vol 16 (42) ◽

pp. 2004677

Author(s):

Huiyuan Li ◽

Xiao Wang ◽

Xiaofei Zhao ◽

Guanhua Li ◽

Fengyan Pei ◽

...

Keyword(s):

Quantum Dots ◽

Antibacterial Activity ◽

Resistant Bacteria ◽

Bacterial Keratitis ◽

Drug Resistant ◽

Drug Resistant Bacteria

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An unexpected discovery toward novel membrane active sulfonyl thiazoles as potential MRSA DNA intercalators

Future Medicinal Chemistry ◽

10.4155/fmc-2019-0303 ◽

2020 ◽

Vol 12 (19) ◽

pp. 1709-1727 ◽

Cited By ~ 1

Author(s):

Yuan-Yuan Hu ◽

Juan Wang ◽

Tie-Jun Li ◽

Rammohan R Yadav Bheemanaboina ◽

Mohammad Fawad Ansari ◽

...

Keyword(s):

Mammalian Cells ◽

Antibacterial Agents ◽

Antimicrobial Agents ◽

Methicillin Resistant Staphylococcus Aureus ◽

Inhibitory Concentration ◽

Resistant Bacteria ◽

Drug Resistant ◽

Dna Intercalators ◽

Dna Targeting ◽

Drug Resistant Bacteria

Aim: With the increasing emergence of drug-resistant bacteria, the need for new antimicrobial agents has become extremely urgent. This work was to develop sulfonyl thiazoles as potential antibacterial agents. Results & methodology: Novel hybrids of sulfonyl thiazoles were developed from commercial acetanilide and acetylthiazole. Hybrids 6e and 6f displayed excellent inhibitory efficacy against clinical methicillin-resistant Staphylococcus aureus (MRSA) (minimum inhibitory concentration = 1 μg/ml) without obvious toxicity toward normal mammalian cells (RAW 264.7). The combination uses were found to improve the antimicrobial ability. Further preliminary antibacterial mechanism experiments showed that the active molecule 6f could effectively interfere with MRSA membrane and insert into MRSA DNA. Conclusion: Compounds 6e and 6f could serve as potential DNA-targeting templates toward the development of promising antimicrobial agents.

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Recombinant HNP-1 Produced by Escherichia coli Triggers Bacterial Apoptosis and Exhibits Antibacterial Activity against Drug-Resistant Bacteria

Microbiology Spectrum ◽

10.1128/spectrum.00860-21 ◽

2022 ◽

Author(s):

Qi Xie ◽

Yin Wang ◽

Mengmeng Zhang ◽

Shujia Wu ◽

Wei Wei ◽

...

Keyword(s):

Escherichia Coli ◽

Antibacterial Activity ◽

Mass Production ◽

Recombinant Protein Expression ◽

Cost Effective ◽

Resistant Bacteria ◽

Drug Resistant ◽

Effective Solution ◽

Drug Resistant Bacteria ◽

Human Neutrophil Peptide

Human neutrophil peptide-1 (HNP-1) is a promising antibiotic candidate, but its clinical application has been hampered by the difficulty of mass production and an inadequate understanding of its bactericidal mechanisms. In this study, we demonstrated that recombinant protein expression combined with ultrafiltration may be a simple and cost-effective solution to HNP-1 production.

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Selection and dissemination of antimicrobial resistance in Agri-food production

Antimicrobial Resistance and Infection Control ◽

10.1186/s13756-019-0623-2 ◽

2019 ◽

Vol 8 (1) ◽

Cited By ~ 13

Author(s):

Guyue Cheng ◽

Jianan Ning ◽

Saeed Ahmed ◽

Junhong Huang ◽

Rizwan Ullah ◽

...

Keyword(s):

Heavy Metals ◽

Antimicrobial Resistance ◽

Food Production ◽

Food Industry ◽

Antimicrobial Agents ◽

Food Sources ◽

Resistant Bacteria ◽

Drug Resistant ◽

Food And Agriculture ◽

Drug Resistant Bacteria

Abstract Public unrest about the use of antimicrobial agents in farming practice is the leading cause of increasing and the emergences of Multi-drug Resistant Bacteria that have placed pressure on the agri-food industry to act. The usage of antimicrobials in food and agriculture have direct or indirect effects on the development of Antimicrobial resistance (AMR) by bacteria associated with animals and plants which may enter the food chain through consumption of meat, fish, vegetables or some other food sources. In addition to antimicrobials, recent reports have shown that AMR is associated with tolerance to heavy metals existing naturally or used in agri-food production. Besides, biocides including disinfectants, antiseptics and preservatives which are widely used in farms and slaughter houses may also contribute in the development of AMR. Though the direct transmission of AMR from food-animals and related environment to human is still vague and debatable, the risk should not be neglected. Therefore, combined global efforts are necessary for the proper use of antimicrobials, heavy metals and biocides in agri-food production to control the development of AMR. These collective measures will preserve the effectiveness of existing antimicrobials for future generations.

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Tackling Antibiotic Resistance with Compounds of Natural Origin: A Comprehensive Review

Biomedicines ◽

10.3390/biomedicines8100405 ◽

2020 ◽

Vol 8 (10) ◽

pp. 405 ◽

Cited By ~ 1

Author(s):

Francisco Javier Álvarez-Martínez ◽

Enrique Barrajón-Catalán ◽

Vicente Micol

Keyword(s):

Antimicrobial Agents ◽

New Technologies ◽

Protein Biosynthesis ◽

Natural Compounds ◽

Network Pharmacology ◽

Resistant Bacteria ◽

Drug Resistant ◽

Antimicrobial Compounds ◽

Natural Antimicrobial ◽

Drug Resistant Bacteria

Drug-resistant bacteria pose a serious threat to human health worldwide. Current antibiotics are losing efficacy and new antimicrobial agents are urgently needed. Living organisms are an invaluable source of antimicrobial compounds. The antimicrobial activity of the most representative natural products of animal, bacterial, fungal and plant origin are reviewed in this paper. Their activity against drug-resistant bacteria, their mechanisms of action, the possible development of resistance against them, their role in current medicine and their future perspectives are discussed. Electronic databases such as PubMed, Scopus and ScienceDirect were used to search scientific contributions until September 2020, using relevant keywords. Natural compounds of heterogeneous origins have been shown to possess antimicrobial capabilities, including against antibiotic-resistant bacteria. The most commonly found mechanisms of antimicrobial action are related to protein biosynthesis and alteration of cell walls and membranes. Various natural compounds, especially phytochemicals, have shown synergistic capacity with antibiotics. There is little literature on the development of specific resistance mechanisms against natural antimicrobial compounds. New technologies such as -omics, network pharmacology and informatics have the potential to identify and characterize new natural antimicrobial compounds in the future. This knowledge may be useful for the development of future therapeutic strategies.

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