scholarly journals Recent advancement in polyphenols as potential antibacterial agents: A comprehensive review

2021 ◽  
Vol 01 ◽  
Author(s):  
Vivek Ahluwalia ◽  
Nusrat Iqbal ◽  
Samsul Alam ◽  
Vinod Kumar ◽  
Lalitesh K. Thakur ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Antibiotic Resistance ◽  
Antibacterial Agents ◽  
Dietary Habits ◽  
Antioxidant Properties ◽  
Antibacterial Properties ◽  
Polyphenolic Compounds ◽  
Antibacterial Compounds ◽  
Recent Advancement ◽  
Food Commodities

: New molecules of natural origin with antibacterial properties are urgently required to control the antibiotic resistance. Worldwide, antibiotic resistance is key threats due to non-judicious and incongruous use of antibiotics. Researchers are focusing on identifying molecules from plant biodiversity that could have both antioxidant and antibacterial properties in one molecule. Much importance on natural antibacterial compounds has been given to the polyphenolic compounds from food commodities. The roles of dietary habits in disease prevention have been credited to presence of polyphenols with antioxidant properties. Polyphenols are secondary metabolites with manifold vital roles including antibacterial activity. Numerous mechanisms like bacterial membrane destruction, destruction of virulence factors, inhibition of the enzymes activity and toxins had been reported for antibacterial activity. Also, hydroxyl, alkyl and acetate moiety on aromatic nucleus influences both antioxidant and antibacterial activity. In this review, details are summarized concerning the antibacterial properties of the key polyphenolic compounds with antioxidant properties.

Fluoroquinolone-3-carboxamide Amino Acid Conjugates: Synthesis, Antibacterial Properties And Molecular Modeling Studies

2020 ◽  
Vol 17 (1) ◽  
pp. 71-84
Author(s):  
Riham M. Bokhtia ◽  
Siva S. Panda ◽  
Adel S. Girgis ◽  
Hitesh H. Honkanadavar ◽  
Tarek S. Ibrahim ◽  
...  
Keyword(s):  
Experimental Data ◽  
Antibacterial Activity ◽  
Amino Acid ◽  
Bacterial Infections ◽  
Antibacterial Agents ◽  
Antibacterial Properties ◽  
Computational Studies ◽  
Protecting Group ◽  
Amino Acid Conjugates ◽  
Molecular Modeling Studies

Background: Bacterial infections are considered as one of the major global health threats, so it is very essential to design and develop new antibacterial agents to overcome the drawbacks of existing antibacterial agents. Method: The aim of this work is to synthesize a series of new fluoroquinolone-3-carboxamide amino acid conjugates by molecular hybridization. We utilized benzotriazole chemistry to synthesize the desired hybrid conjugates. Result: All the conjugates were synthesized in good yields, characterized, evaluated for their antibacterial activity. The compounds were screened for their antibacterial activity using methods adapted from the Clinical and Laboratory Standards Institute. Synthesized conjugates were tested for activity against medically relevant pathogens; Escherichia coli (ATCC 25922), Pseudomonas aeruginosa (ATCC 27856) Staphylococcus aureus (ATCC 25923) and Enterococcus faecalis (ATCC 19433). Conclusion: The observed antibacterial experimental data indicates the selectivity of our synthesized conjugates against E.Coli. The protecting group on amino acids decreases the antibacterial activity. The synthesized conjugates are non-toxic to the normal cell lines. The experimental data were supported by computational studies.

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 UHPLC-HESI-OT-MS-MS Biomolecules Profiling, Antioxidant and Antibacterial Activity of the “Orange-Yellow Resin” from Zuccagnia punctata Cav.

Antioxidants ◽  
2020 ◽  
Vol 9 (2) ◽  
pp. 123 ◽  
Author(s):  
Jessica Gómez ◽  
Mario J. Simirgiotis ◽  
Sofía Manrique ◽  
Beatriz Lima ◽  
Jorge Bórquez ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Liquid Chromatography ◽  
Metabolite Profiling ◽  
Antioxidant Properties ◽  
Antibacterial Properties ◽  
Ultrahigh Resolution ◽  
Antioxidant Power ◽  
Orange Yellow ◽  
Ms Analysis ◽  
Orbitrap Ms

This research was designed to investigate the metabolite profiling, phenolics, and flavonoids content as well as the potential antioxidant and antibacterial, properties of orange-yellow resin from Zuccagnia punctata Cav (ZpRe). Metabolite profiling was obtained by a ultrahigh resolution liquid chromatography orbitrap MS analysis (UHPLC-ESI-OT-MS-MS). The antioxidant properties were screened by four methods: 2,2-diphenyl-1-picrylhydrazyl assay (DPPH), trolox equivalent antioxidant activity assay (TEAC), ferric-reducing antioxidant power assay (FRAP), and lipid peroxidation in erythrocytes (LP)). The antibacterial activity was evaluated according to the Clinical and Laboratory Standards Institute (CLSI) rules. The resin displayed a strong DPPH scavenging activity (IC50 = 25.72 µg/mL) and showed a percentage of inhibition of LP close to that of the reference compound catechin (70% at 100 µg ZpRe/mL), while a moderated effect was observed in the FRAP and TEAC assays. The resin showed a content of phenolic and flavonoid compounds of 391 mg GAE/g and 313 mg EQ/g respectively. Fifty phenolics compounds were identified by ultrahigh resolution liquid chromatography orbitrap MS analysis (UHPLC-PDA-OT-MS) analysis. Thirty-one compounds are reported for the first time, updating the knowledge on the chemical profile of this species. The importance of the biomolecules identified support traditional use of this endemic plant. Furthermore, additional pharmacological data is presented that increase the potential interest of this plant for industrial sustainable applications.

scholarly journals Eleucine indicaPossesses Antioxidant, Antibacterial and Cytotoxic Properties

2011 ◽  
Vol 2011 ◽  
pp. 1-6 ◽  
Author(s):  
Adel S. Al-Zubairi ◽  
Ahmad Bustamam Abdul ◽  
Siddig Ibrahim Abdelwahab ◽  
Chew Yuan Peng ◽  
Syam Mohan ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Human Cancer ◽  
Antioxidant Properties ◽  
Antibacterial Properties ◽  
Diffusion Method ◽  
Total Phenolic ◽  
Significant Activity ◽  
Human Cancer Cell Lines

The use of evidence-based complementary and alternative medicine is increasing rapidly.Eleucine indica(EI) is traditionally used in ailments associated with liver and kidneys. The therapeutic benefit of the medicinal plants is often attributed to their antioxidant properties. Therefore, the aim of this study was to screen the hexane, dicholoromethane, ethyl acetate (EA) and methanol extracts (MeTH) of EI for their antioxidant, antibacterial and anti-cancer effects using total phenolic contents (TPCs) and DPPH, disc diffusion method and MTT cytotoxicity assays, respectively. The MeTH was showed to have the highest TPC and scavenging activity (77.7%) on DPPH assay, followed by EA (64.5%), hexane (47.19%) and DCM (40.83%) extracts, whereas the MeTH showed no inhibitory effect on all tested bacteria strains. However, the EA extract exhibited a broad spectrum antibacterial activity against all tested bacteria exceptBacillus subtilis, in which this bacterium was found to be resistant to all EI extracts. Meanwhile, hexane extract was demonstrated to have a remarkable antibacterial activity against methicillin resistantStaphylococcus aureus(MRSA) andPseudomonas aeruginosa, while the dicholoromethane extract did not exhibit significant activity againstP. aeruginosa. None of the extracts showed significant cytotoxic activity towards MCF-7, HT-29 and CEM-SS human cancer cell lines after 72 h incubation time (IC50> 30 μg/ml). These results demonstrate that the extract prepared from the EI possesses antioxidant activityin vitroin addition to antibacterial properties. Further investigations are needed to verify the antioxidant effectsin vitroandin vivo.

scholarly journals Design, Synthesis and Antibacterial Activity of some 3,6-Dimethlyquinoxaline-2-Hydrazone Derivatives

2021 ◽  
pp. 48-61
Author(s):  
F. O. Taiwo ◽  
C. A. Obafemi ◽  
D. A. Akinpelu ◽  
T. O. Iyiola
Keyword(s):  
Antibacterial Activity ◽  
Antibacterial Properties ◽  
Bacterial Strains ◽  
Design Synthesis ◽  
Antibacterial Compounds ◽  
Synthetic Compounds ◽  
Aromatic Ketones ◽  
Bactericidal Effects ◽  
Test Organisms ◽  
Zones Of Inhibition

Aims: This aims of this study was to continue the effort to synthesis new quinoxaline-based heterocycles and study its antibacterial properties. Objective: This study was designed to reacts 3,6-dimethylquinoxaline-2-hydrazine with some substituted aromatic ketones and study their antibacterial properties on some locally and clinically isolated bacterial strains. Materials and Methods: Five 3,6-dimethylquinoxaline-2-hydrazone derivatives were synthesized from the reactions of 3,6-dimethylquinoxaline-2-hydrazine with various substituted aromatic ketones. The products were then tested for their potential antibacterial properties. Results: All the synthesized compounds were found to be active against all the bacterial strains investigated in this study. It was observed that the zones of inhibition observed for the synthesized compounds against the test organisms ranged between 15 mm and 38 mm. The MIC observed for the synthesized compounds ranged between 0.0313mg/mL and 0.125 mg/mL, while that of the standard antibiotic, streptomycin, varied between 0.0313 mg/mL and 0.500 mg/mL and those observed for tetracycline falls between 0.0313 mg/mL and 0.500 mg/mL. The minimum bactericidal concentrations exhibited by the synthesized compounds ranged between 0.0625 mg/mL and 0.250 mg/mL Discussion and conclusion: The study concluded that all the compounds exhibited appreciable bactericidal effects against all the bacterial strains, which is an indication that such synthetic compounds possessed broad spectrum activities and such compounds could be useful in formulation of antibacterial compounds which could be used to mitigates infections caused by pathogens that are now developing resistance against the available antibiotics.

scholarly journals Improved Antibacterial Activity of Water-Soluble Nanoformulated Kaempferol and Combretastatin Polyphenolic Compounds

2021 ◽  
Vol 2021 ◽  
pp. 1-12
Author(s):  
Y. Santhosh Kumar ◽  
Langeswaran Kulanthaivel ◽  
G. S. Hikku ◽  
R. Saravanan ◽  
Thangavelu Lakshmi ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Water Solubility ◽  
Release Kinetics ◽  
Antibacterial Properties ◽  
Polyphenolic Compounds ◽  
Water Soluble ◽  
Aureus Strain ◽  
Significant Activity ◽  
Molecular Vibrations ◽  
Pump System

Kaempferol and combretastatin are polyphenolic compounds derived from plant sources which are known for their antibacterial activity. However, owing to their large size and water insolubility, their antibacterial activity is limited. In this context, the present study focused on the nanoformulation of kaempferol (NF-k) and combretastatin (NF-c) and their influence on water solubility and antibacterial properties. The NF-k and NF-c were prepared using the solvent evaporation method and were thoroughly characterized for evaluating the morphology, molecular vibrations, size, etc. Based on the results, it is observed that the pristine forms of kaempferol and combretastatin drugs get nanoformulated and completely soluble in water. Using particle size analyzer, the particle sizes of NF-k and NF-c were estimated as 334 nm and 260 nm, respectively, which are very fine compared to pristine kaempferol and combretastatin (5193 nm and 1217 nm, respectively). The molecular vibrations that exist in NF-k and NF-c were confirmed by the Fourier transform infrared spectra, where the nanoformulated drug showed lower intensities than the pristine form of kaempferol and combretastatin. The drug release kinetics of the nanoformulated drugs were carried out using the dialysis membrane method and were compared with their pristine forms. Owing to the size effect, the NF-k and NF-c release up to 50% of the drug in a sustained manner till 50 h showing twofold higher concentration than the control where it released 25%. The antibacterial activity was assessed by measuring the optical density at 600 nm using UV-vis spectrophotometer and displayed significant activity against gram-positive Staphylococcus aureus strain. The mechanisms behind the antibacterial activity of NF-k and NF-c were discussed in detail. The activation of ATP-dependent efflux pump system and the blockage of porin channels could be the cause for the bactericidal activity. Our understanding of efflux pumps and their role in antibacterial activity is still in its early stages. No studies have been performed to date using nanoformulations of kaempferol and combretastatin to investigate their roles. This complicates the determination of the exact mechanisms acting against bacterial growth when using nanoformulation drugs. Our increasing knowledge of water-soluble nanoformulation drugs and their roles in reduced bacterial activity will pave the way to developing effective treatments in the future.

IN VITRO EVALUATION OF ANTIBACTERIAL AND ANTIOXIDANT PROPERTIES OF AN INDIAN MEDICINAL PLANT: CELASTRUS PANICULATUS WILLD

2020 ◽  
Vol 9 (1) ◽  
Author(s):  
Pradeep K Naik ◽  
Debasmita Dubey ◽  
Priya Cheruvanachari ◽  
Animesh Pattnaik ◽  
Swaraj K Babu
Keyword(s):  
Antioxidant Activity ◽  
Antibacterial Activity ◽  
Antioxidant Properties ◽  
Antibacterial Properties ◽  
Resistant Bacteria ◽  
Dilution Method ◽  
Phytochemical Analysis ◽  
Leaf Extracts ◽  
Dpph Method ◽  
Celastrus Paniculatus

Aim: To evaluate the antibacterial efficacy, the presence of different phytoconstituents of the leaf extracts of Indian plant Celastrus paniculatus against 6 antibiotic-resistant bacteria along with the evaluation of their antioxidant potentiality. Methods: The leaf extracts were prepared using 4 solvents, water, methanol, n-butanol, and acetone. The antibacterial property was evaluated using agar well diffusion and micro-broth dilution method. Qualitative phytochemical analysis was performed using standard protocols for each solvent extract to check for the presence of the secondary metabolites and phytochemicals which attributes to the antibacterial effectivity of C. paniculatus. Further, the antioxidant potentiality of all the 4 leaf-solvent-extracts was estimated using the DPPH method. Results: The n-butanol leaf extract exhibited the highest antibacterial and antioxidant activity, followed by acetone, methanol extracts. The aqueous extracts exhibited negligible antibacterial activity. Conclusion: This study validated the antibacterial properties of C. paniculatus leaf extracts against both gram-positive and negative bacteria and the phytochemical analysis revealed the presence of many secondary importance which can be attributed to its therapeutic properties. Hence, this plant can be further used as a complementary or alternative choice of drug for combatting multidrug-resistant bacterial pathogens. Keywords: Antibiotic resistance; Medicinal plants; Celastrus Paniculatus; Antibacterial activity, Phytochemical Analysis; Antioxidant activity

Design and Discovery of New Antibacterial Agents: Advances, Perspectives, Challenges

2019 ◽  
Vol 25 (38) ◽  
pp. 4972-5006 ◽  
Author(s):  
Josef Jampilek
Keyword(s):  
Small Molecules ◽  
Bacterial Infections ◽  
Antibacterial Agents ◽  
Bacterial Resistance ◽  
Antibacterial Properties ◽  
Molecular Scaffolds ◽  
Antibacterial Compounds ◽  
Drug Classes ◽  
First Choice ◽  
Wide Range

Background: Emerging resistance of bacterial pathogens to clinically used drugs, including not only first-choice but also second- and third-choice drugs, is alarming, but since the 1990s only a modest number of new, first in class, drugs for systemic administration have been marketed for the treatment of bacterial infections. Objective: This article provides a review of recently reported new antibacterial chemotherapeutics approved for clinical practice, antibacterial chemotherapeutics in clinical trials and antibacterial agents under development. Discussion: Antibacterial agents include new antibacterial compounds of used drug classes and new antibacterial agents with a novel mode of action. In addition, particular attention is given to agents decreasing bacterial resistance, i.e. to compounds that do not have significant intrinsic bacteriostatic or bactericidal activity, but in combination with antibacterial drugs are able to restore the effect of these drugs or demonstrate synergistic antibacterial properties together with the drugs. Conclusion: This review is specifically focused on small molecules rather than on peptides and discusses a wide range of various molecular scaffolds.

scholarly journals ANTIBACTERIAL ACTIVITY OF “ANASTATICA HIEROCHUNTICA L.” AGAINST SOME BACTERIAL STRAINS RESPONSIBLE FOR WOMEN’S URO-GENITAL INFECTION

2018 ◽  
Vol 11 (7) ◽  
pp. 222
Author(s):  
Elhassan Benyagoub ◽  
Nouria Nabbou ◽  
Dalila Razni ◽  
Snoussi Moghtet
Keyword(s):  
Antibacterial Activity ◽  
Antibiotic Resistance ◽  
Antibacterial Properties ◽  
Genital Infection ◽  
Bacterial Strains ◽  
Resistance Profile ◽  
Gram Positive Bacteria ◽  
Natural Substances ◽  
Antibiotic Resistance Profile ◽  
Antibacterial Potential

Objective: The purpose of this work is to study the biological activity of Anastatica hierochuntica L., against nine bacterial strains responsible for women’s uro-genital infection (UGI).Methods: The plant was collected from Tindouf region (far southwest Algeria). In this study, we performed an evaluation of antibacterial activity of three macerates of two vegetative parts (seeds and stems) by two methods (disc and wells diffusion methods), with a description of the antibiotic resistance profile of isolated bacterial strains by antibiogram method.Results: According to the results, the antibiotic resistance profile of the tested bacterial strains showed an increased resistance against several antibiotics families. The evaluation of the antibacterial potential of macerates showed that methanolic and aqueous macerates of the seeds were more active against Gram-positive bacteria compared to Gram-negative bacteria.Conclusion: The preliminary results of this study allowed us to predict that natural substances in the plant can be considered as an important source to possess compounds with significant antibacterial properties and thus suggest their application in the pharmaceutical industry.

scholarly journals In Vitro Evaluation of Palestinian Propolis as a Natural Product with Antioxidant Properties and Antimicrobial Activity against Multidrug-Resistant Clinical Isolates

2020 ◽  
Vol 2020 ◽  
pp. 1-10
Author(s):  
Jamila Daraghmeh ◽  
Hamada Imtara
Keyword(s):  
Pseudomonas Aeruginosa ◽  
Antibacterial Activity ◽  
Radical Scavenging Activity ◽  
Antioxidant Properties ◽  
Radical Scavenging ◽  
Antibacterial Properties ◽  
Reducing Power ◽  
Multidrug Resistant ◽  
Clinical Isolates ◽  
Total Phenolic

The present work reveals, for the first time, the antioxidant and antibacterial properties of propolis samples collected from different regions of Palestine. The content on bioactive compounds has been estimated by total phenolic and flavone and flavonol content, while their antioxidant activity has been determined by radical scavenging methods of 1,2-diphenyl-1-picrylhydrazyl radical (DPPH), 2,2′-azino-bis (3-ethylbenzothiazoline-6-sulphonic acid) radical (ABTS), and ferric reducing power assay (FRAP). The disc diffusion, minimum inhibitory concentration (MIC), and minimum bactericidal concentration (MBC) methods were carried out to evaluate the antibacterial activity of Palestinian propolis against multidrug-resistant clinical isolates, including Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, and Streptococcus faecalis. The results showed that the total phenolic content ranged from 9.62 mg to 124.94 mg gallic acid equivalent GAE/g of propolis, and the flavone and flavonol content ranged from 1.06 to 75.31 mg quercetin equivalent QE/g of propolis. The samples S6 from Al-Khalil presented the strongest radical scavenging activity toward DPPH, ABTS free radicals, and FRAP assay with IC50 values of 0.02, 0.03, and 0.05 mg/mL, respectively. The results of antibacterial activity indicated that the propolis samples inhibit the growth of Gram-positive strains better than Gram-negative ones. In addition, a strong correlation was observed between the pH, resin, balsam, total phenolic, flavones and flavonol, and total antioxidant capacity (TAC) from one side and the antibacterial activity of propolis samples except on Pseudomonas aeruginosa.

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