scholarly journals Selenocompounds as Novel Antibacterial Agents and Bacterial Efflux Pump Inhibitors

Molecules ◽  
2019 ◽  
Vol 24 (8) ◽  
pp. 1487 ◽  
Author(s):  
Tímea Mosolygó ◽  
Annamária Kincses ◽  
Andrea Csonka ◽  
Ádám Szabó Tönki ◽  
Karolina Witek ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Multidrug Resistance ◽  
Carbonyl Compounds ◽  
Antibacterial Agents ◽  
Inhibitory Concentration ◽  
Efflux Pump ◽  
Attractive Potential ◽  
Bacterial Strains ◽  
Gram Positive Bacteria ◽  
Efflux Pump Inhibitors

Bacterial multidrug resistance is becoming a growing problem for public health, due to the development and spreading of bacterial strains resistant to antimicrobials. In this study, the antibacterial and multidrug resistance reversing activity of a series of seleno-carbonyl compounds has been evaluated. The effects of eleven selenocompounds on bacterial growth were evaluated in Staphylococcus aureus, methicillin resistant S. aureus (MRSA), Enterococcus faecalis, Escherichia coli, and Chlamydia trachomatis D. The combination effect of compounds with antibiotics was examined by the minimum inhibitory concentration reduction assay. Their efflux pump (EP) inhibitory properties were assessed using real-time fluorimetry. Relative expressions of EP and quorum-sensing genes were studied by quantitative PCR. Results showed that a methylketone selenoester had remarkable antibacterial activity against Gram-positive bacteria and potentiated the activity of oxacillin in MRSA. Most of the selenocompounds showed significant anti-chlamydial effects. The selenoanhydride and the diselenodiester were active inhibitors of the AcrAB-TolC system. Based on these results it can be concluded that this group of selenocompounds can be attractive potential antibacterials and EP inhibitors. The discovery of new derivatives with a significant antibacterial activity as novel selenocompounds, is of high impact in the fight against resistant pathogens.

Synthesis and antibacterial activity of N1-(carbazol-3-yl)amidrazones incorporating piperazines and related congeners

2016 ◽  
Vol 71 (8) ◽  
pp. 857-867 ◽  
Author(s):  
Ahmad H. Abdullah ◽  
Jalal A. Zahra ◽  
Mustafa M. El-Abadelah ◽  
Salim S. Sabri ◽  
Monther A. Khanfar ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Antibacterial Agents ◽  
Methicillin Resistant Staphylococcus Aureus ◽  
Inhibitory Concentration ◽  
Bacterial Strains ◽  
X Ray ◽  
In Vitro Antibacterial Activity ◽  
Further Development

AbstractA selected set of N1-(4-chloro-9-ethylcarbazol-3-yl)amidrazones (7a–n) has been synthesized by reacting the respective hydrazonoyl chloride 5 derived from 3-amino-9-ethylcarbazole (3), with an appropriate sec-cyclic amine (6a–n) in ethanol in the presence of triethylamine. Unexpectedly, aromatic ring chlorination occurred at C-4 of 3 during its conversion to 6 as evidenced by analytical and spectral data and further confirmed by single crystal X-ray structure determination of the amidrazone 7n. Compounds 7a–n were tested for their in vitro antibacterial activity. Among the tested bacterial strains, methicillin-resistant Staphylococcus aureus was the most susceptible to 7f and Bacillus cereus to 7b both with a minimum inhibitory concentration value of 1.56 µg mL−1. Compounds 7c, 7f, and 7h could be useful as lead structures for further development of new antibacterial agents against Gram-positive and Gram-negative pathogens.

scholarly journals Beehive Products as Antibacterial Agents: A Review

Antibiotics ◽  
2021 ◽  
Vol 10 (6) ◽  
pp. 717
Author(s):  
Rita Abou Nader ◽  
Rawan Mackieh ◽  
Rim Wehbe ◽  
Dany El El Obeid ◽  
Jean Marc Sabatier ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Honey Bee ◽  
Antibacterial Agents ◽  
Royal Jelly ◽  
Biological Activities ◽  
Vital Role ◽  
Bee Venom ◽  
Bacterial Strains ◽  
Wide Range ◽  
Life Threatening

Honeybees are one of the most marvelous and economically beneficial insects. As pollinators, they play a vital role in every aspect of the ecosystem. Beehive products have been used for thousands of years in many cultures for the treatment of various diseases. Their healing properties have been documented in many religious texts like the Noble Quran and the Holy Bible. Honey, bee venom, propolis, pollen and royal jelly all demonstrated a richness in their bioactive compounds which make them effective against a variety of bacterial strains. Furthermore, many studies showed that honey and bee venom work as powerful antibacterial agents against a wide range of bacteria including life-threatening bacteria. Several reports documented the biological activities of honeybee products but none of them emphasized on the antibacterial activity of all beehive products. Therefore, this review aims to highlight the antibacterial activity of honey, bee venom, propolis, pollen and royal jelly, that are produced by honeybees.

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

Antibiotics ◽  
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.

scholarly journals Antibacterial activity of Baccharis trimera (Less.) DC. (carqueja) against bacteria of medical interest

Revista CERES ◽  
2013 ◽  
Vol 60 (5) ◽  
pp. 731-734 ◽  
Author(s):  
Álan Alex Aleixo ◽  
Karina Marjorie Silva Herrera ◽  
Rosy Iara Maciel de Azambuja Ribeiro ◽  
Luciana Alves Rodrigues dos Santos Lima ◽  
Jaqueline Maria Siqueira Ferreira
Keyword(s):  
Antibacterial Activity ◽  
Folk Medicine ◽  
Salmonella Typhi ◽  
Bacterial Strains ◽  
Gram Positive ◽  
Gram Positive Bacteria ◽  
Clinical Interest ◽  
Antibacterial Susceptibility ◽  
Baccharis Trimera ◽  
Medical Interest

Baccharis trimera (Less.) (Asteraceae), popularly know as "carqueja", is a species commonly used in folk medicine for the treatment or prevention of diseases. In this context, the purpose of this work was to study the antibacterial activity of crude hydroalcoholic extract from Baccharis trimera against Gram-positive bacterial strains (Staphylococcus aureus ATCC 29213, Staphylococcus saprophyticus ATCC 15305, Staphylococcus epidermidis ATCC 12228, Enterococcus faecalis ATCC 19433) and Gram-negative bacteria (Escherichia coli EHEC ATCC 43895, Pseudomonas aeruginosa ATCC 27853, Klebsiella pneumoniae ATCC 27736, Salmonella typhi ATCC 19430) of clinical interest. Antibacterial susceptibility was evaluated by broth microdilution assay following the CLSI (formerly the NCCLS) guidelines. The extract from B. trimera showed antibacterial activity against Gram-positive bacteria and the most interesting result was obtained against S. epidermidis that presented Minimal Inhibitory Concentration of 250μg/mL. These results indicate that B. trimera have bacterisostatic potential against Gram-positive bacterial strains of medical interest and could serve as a base for further studies on the use of isolated compounds from this species as future antimicrobials.

scholarly journals Antibacterial Activity of the Essential Oil of Heracleum Sibiricum

2013 ◽  
Vol 8 (9) ◽  
pp. 1934578X1300800 ◽  
Author(s):  
Dragoljub L. Miladinović ◽  
Budimir S. Ilić ◽  
Tatjana M. Mihajilov-Krstev ◽  
Dejan M. Nikolić ◽  
Olga G. Cvetković ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Essential Oil ◽  
Antimicrobial Activities ◽  
Bacterial Strains ◽  
Gram Positive Bacteria ◽  
Microdilution Method ◽  
Broth Microdilution Method ◽  
Major Chemical ◽  
Total Oil ◽  
Chemical Class

The composition and antimicrobial activity of the essential oil of Heracleum sibiricum L. (Apiaceae) was studied. The aerial part of plant was hydro-distilled and chemical composition of the essential oil was analyzed by GC and GC-MS. Forty-six compounds, corresponding to 95.12% of the total oil, were identified. Esters represented the major chemical class (69.55%) while the main constituents were octyl butanoate (36.82%), hexyl butanoate (16.08%), 1-octanol (13.62%) and octyl hexanoate (8.10%). Antibacterial activity of the essential oil and reference antibiotics against nine bacterial strains was tested by the broth microdilution method. The results of the bioassays showed that essential oil had slight antimicrobial activities against all tested microorganisms (MIC and MBC values were in the range of 2431.2 to 9724.8 μg/mL). Reference antibiotics were active in concentrations between 0.5 and 16.0 μg/mL. The results confirm that Gram-positive bacteria were more susceptible to the essential oil of H. sibiricum, in comparison with Gram-negative bacteria.

QSAR analysis of 1,3-diaryl-2-propen-1-ones and their indole analogs for designing potent antibacterial agents

2009 ◽  
Vol 63 (4) ◽  
Author(s):  
Neela Bhatia ◽  
Kakasaheb Mahadik ◽  
Manish Bhatia
Keyword(s):  
Antibacterial Activity ◽  
Elemental Analysis ◽  
Antibacterial Agents ◽  
Structure Optimization ◽  
Antibacterial Activities ◽  
Bacterial Strains ◽  
Lower Toxicity ◽  
Qsar Analysis ◽  
Qsar Studies ◽  
Vlife Mds

AbstractA series of 1,3-diaryl-2-propen-1-ones and their indole analogs were synthesized and evaluated for antibacterial activity. Structures of newly synthesized compounds were confirmed by physicochemical, spectral and elemental analysis. All the compounds were screened for their antibacterial activities against four different bacterial strains. The QSAR studies were performed using Vlife MDS 3.5 software. QSAR equation revealed that selected electronic, steric and lipophilic parameters have good correlation with antibacterial activity. Best equations were selected on basis of the correlation coefficient (r 2) and the predictable ability of the equations. The present findings suggest that the 1,3-diaryl-2-propen-1-ones framework is an attractive template for structure optimization to achieve higher potency, lower toxicity, and a wider spectrum of antibacterial activity.

scholarly journals Synthesis and in vitro Antibacterial Activity of Quaternization 10-Methoxycanthin-6-one Derivatives

2019 ◽  
Author(s):  
Na Li ◽  
Jiang-Kun Dai ◽  
Dan Liu ◽  
Jin-Yi Wang ◽  
Jun-Ru Wang
Keyword(s):  
Antibacterial Activity ◽  
Natural Products ◽  
Minimum Inhibitory Concentration ◽  
Pathogenic Bacteria ◽  
Antibacterial Agents ◽  
Inhibitory Concentration ◽  
Dilution Method ◽  
In Vitro Antibacterial Activity

Natural products are an important source of antibacterial agents. Canthin-6-one alkaloids have displayed potential antibacterial activity based on our previous work. In order to improve the activity, twenty-two new 3-N-benzylated 10-methoxy canthin-6-ones were designed and synthesized through quaternization reaction. The in vitro antibacterial activity against three bacteria was evaluated by double dilution method. Four compounds (6f, 6i, 6p and 6t) displayed 2-fold superiority (minimum inhibitory concentration (MIC) = 3.91 µg/mL) against agricultural pathogenic bacteria R. solanacearum and P. syringae than agrochemical propineb. Moreover, the structure–activity relationships (SARs) were also carefully summarized in order to guide the development of antibacterial canthin-6-one agents.

scholarly journals Phytochemical analyses and antibacterial activities of Erodium, Euphorbia, Logoecia and Tamarix species

2019 ◽  
Vol 13 (11) ◽  
pp. 1013-1020
Author(s):  
Khaldoun J Al-Hadid ◽  
Nehaya Al-Karablieh ◽  
Ahmad Sharab ◽  
Ihsan Mutlak
Keyword(s):  
Antibacterial Agents ◽  
Antibacterial Activities ◽  
Microtiter Plate ◽  
Phytochemical Analysis ◽  
Bacterial Strains ◽  
Gram Positive ◽  
Gram Positive Bacteria ◽  
Phytochemical Components ◽  
Promising Source ◽  
Group D

Introduction: Resistance against commonly used antibacterial agents has become a globally recognized threat to human health. Therefore, the development of new and effective antibacterial agents is necessary to treat infections caused by resistant bacterial strains; plants are a promising source of new agents to be tested. Methodology: The minimum inhibitory concentrations (MIC) of ethanolic extracts of Erodium gruinum, Euphorbia hierosolymitana, Logoecia cuminoides, and Tamarix tetragyna against 10 Gram-negative and 5 Gram-positive bacteria were determined using agar well diffusion and microtiter plate dilution methods, respectively. The phytochemical composition of the crude extracts of the plants was determined using HPLC. Results: Pseudomonas aeruginosa ATCC 27853, Klebsiella pneumoniae, Proteus mirabilis, and Acinetobacter baumannii were sensitive to E. gruinum and E. hierosolymitana extracts. P. aeruginosa ATCC 27853 and M. catarrhalis were sensitive to L. cuminoides extract. P. aeruginosa ATCC 27853, P. mirabilis, and K. pneumoniae were sensitive to T. tetragyna extracts. For Gram-positive bacteria, Staphylococcus aureus ATCC 33591 and ATCC 43300 were sensitive to E. gruinum and E. hierosolymitana extracts. S. aureus ATCC 43300 and ATCC 33591 and Group D Streptococcus were sensitive to T. tetragyna extract. All Gram-positive bacteria were completely resistant to the extract of L. cuminoides. The major phytochemical components of the plant extracts belonged to flavonoids, tannins, terpenes, quinones, phytosterols, phytoestrogens, carbohydrates, fatty acids, and coumarin. Conclusion: The study showed the potential of the development of antibacterial agents from these plants. Phytochemical analysis revealed compounds that are candidates for new antibacterial drugs.

scholarly journals Medicinal Chemistry Updates on Bacterial Efflux Pump Modulators

2019 ◽  
Vol 25 (42) ◽  
pp. 6030-6069 ◽  
Author(s):  
Fernando Durães ◽  
Madalena Pinto ◽  
Emília Sousa
Keyword(s):  
Energy Source ◽  
Antibiotic Resistance ◽  
Efflux Pump ◽  
Efflux Pumps ◽  
The Other ◽  
Drug Uptake ◽  
Health Issues ◽  
Gram Positive ◽  
Gram Positive Bacteria ◽  
Efflux Pump Inhibitors

Antibiotic resistance is one of the most pressing health issues of our days. It can arise due to a multiplicity of factors, such as target modification, decrease in the drug uptake, changes in the metabolic pathways and activation of efflux pumps. The overexpression of efflux pumps is responsible for the extrusion of drugs, making antibiotic therapy fail, as the quantity of intracellular antibiotic is not enough to provide the desired therapeutic effect. Efflux pumps can be included in five families according to their composition, nature of substrates, energy source, and number of transmembrane spanning regions. The ABC superfamily is mainly found in Gram-positive bacteria, use ATP as an energy source, and only a limited number of ABC pumps confer multidrug resistance (MDR). On the other hand, the MFS family, most present in Gram-positive bacteria, and the RND family, characteristic of Gram-negative bacteria, are most associated with antibiotic resistance. A wide variety of inhibitors have been disclosed for both families, from either natural or synthetic sources, or even drugs that are currently in therapy for other diseases. The other two families are the SMR, which are the smallest drug efflux proteins known, and the MATE family, whose pumps can also resort to the sodium gradient as an energy source. In this review, it is intended to present a comprehensive review of the classes of efflux pump inhibitors from the various sources, highlighting their structure-activity relationships, which can be useful for medicinal chemists in the pursuit of novel efflux pump inhibitors.

scholarly journals STUDY CYTOTOXICITY, ANTIBACTERIAL ACTIVITY, AND COMPOSITIONS BY FT-IR AND GC-MS FOR ORGANIC EXTRACT OF WHITE IRAQI DESERT TRUFFLE TIRMANIA NIVEA

2020 ◽  
Vol 17 (36) ◽  
pp. 18-31
Author(s):  
Ahmad khadem HACHIM ◽  
Rashid Rahim HATEET ◽  
Tawfik Muhammad MUHSIN
Keyword(s):  
Antibacterial Activity ◽  
Minimum Inhibitory Concentration ◽  
Cell Line ◽  
Pathogenic Bacteria ◽  
Inhibitory Concentration ◽  
Biological Activities ◽  
Gas Chromatography Mass Spectrometry ◽  
Bacterial Strains ◽  
Organic Extract

The purpose of the present work aimed at exploring the potential biochemical components and biological activities of an organic extract of the white truffle Tirmania nivea collected from the Iraqi desert, then test the organic extract against the Cytotoxicity on Human Larynx carcinoma cells and selected strains of pathogenic bacteria. Fourier transform infrared spectroscopy (FTIR) and gas chromatography-mass spectrometry GC/MSS were used to analyze mycochemical compositions. The antibacterial activity and Minimum Inhibitory Concentration (MIC) and Minimum Bactericidal Concentration (MBC) was investigated using a disk diffusion agar method. The truffle extract's cytotoxicity effect against the larynx cell line (Hep-2) was assessed by the MTT assay (in vitro). FTIR results provided the presence of phenol, carboxylic acid, and alkane's functional group, The GC-MS analysis of T. nivea disclose the existence of nineteen compounds that can contribute to the pharmaceutical properties of the truffle. As for antibacterial activity result, A growth inhibition activity of truffle extract at (18-40 mm inhibition zones) against the tested pathogenic bacterial strains was detected, which minimum inhibitory concentration values ranged from 3.12 to 6.25 mg/mL for Escherichia coli (ATCC 25922) and Staphylococcus aureus (ATCC 25923) Respectively. The results of cytotoxicity shown that the organic truffle extract exhibited a high inhibitory rate (52.685%) against cell line (Hep-2) at a concentration of 1.56 ?g/mL. In this work, the results showed that the organic extracts of T. nivea are very promising as cancer cytotoxicity and antibacterial agent for future medical applications.

Sign in / Sign up

Export Citation Format

Share Document