Design Synthesis and Biological Implications of Antibacterial Substances

A special issue of Antibiotics (ISSN 2079-6382).

Deadline for manuscript submissions: closed (30 September 2023) | Viewed by 7115

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Division of Bioorganic Chemistry, School of Pharmacy, Saarland University, D-66123 Saarbruecken, Germany
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Dear Colleagues,

Since the discovery of the very first antibiotic, i.e., penicillin by Alexander Fleming in 1928, the field of antibiotics has taken several twists and turns. This discovery paved the way for the production of the plethora of antibiotics we witness today. The field of antibiotics, however, has gradually evolved from simple antibiotics to target-based antibiotics or even the utilization of a combination of antibiotics and adjuvants. The substances range from natural products, extracts, pure organic compounds, multifunctional agents and even nanoparticles. The overutilization of antibiotics has led to the emergence of resistance towards conventional antibiotics. Despite the production and screening of thousands of substances with antimicrobial activities each year, only a few substances are approved by FDA after clinical trials. There is, therefore, an urgent and intense need not only for the development of novel antibiotics but also for the strategies to combat resistance.

In this particular Special Issue, we would like to highlight the recent developments in the field of antibiotics. Any submissions (comprehensive reviews, research articles, communications, or commentary etc. to provide an insight in the current state of the art) are highly welcomed.

Dr. Muhammad Jawad Nasim
Guest Editor

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Published Papers (3 papers)

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Research

14 pages, 712 KiB  
Article
Daniellia oliveri (Rolfe) Hutch and Dalziel: Antimicrobial Activities, Cytotoxicity Evaluation, and Phytochemical Identification by GC-MS
by Nassifatou Koko Tittikpina, Gilbert Kirsch, Raphaël Emmanuel Duval, Patrick Chaimbault and Claus Jacob
Antibiotics 2022, 11(12), 1699; https://doi.org/10.3390/antibiotics11121699 - 25 Nov 2022
Cited by 1 | Viewed by 1573
Abstract
During a previous study that identified plants used in traditional medicine in Togo to treat infectious diseases, Daniellia oliveri was specifically reported to treat intertrigo and candidiasis. Consequently, to explore the anti-infective potential of this plant, we investigated the antibacterial and the antifungal [...] Read more.
During a previous study that identified plants used in traditional medicine in Togo to treat infectious diseases, Daniellia oliveri was specifically reported to treat intertrigo and candidiasis. Consequently, to explore the anti-infective potential of this plant, we investigated the antibacterial and the antifungal activity of the plant’s parts, as well as the cytotoxic activities of raw extracts and subsequent fractions, and the chemical composition of the most active fractions. In order to evaluate the antimicrobial activity, MICs were determined using the broth dilution method. Then, the most active fractions were evaluated for cytotoxicity by using normal human cells (MRC-5 cells) via the MTT assay. Finally, the most active and not toxic fractions were phytochemically investigated by GC-MS. Interestingly, all the raw extracts and fractions were active against the bacteria tested, with MICs ranging from 16 µg/mL to 256 µg/mL, while no antifungal activity was observed at 256 µg/mL, the highest tested concentration. Moreover, no toxicity was observed with most of the active fractions. The subsequent chemical investigation of the most interesting fractions led to identifying terpenes, phytosterols, phenolic compounds, and fatty acids as the main compounds. In conclusion, this study demonstrated that D. oliveri possesses valuable antibacterial activities in accordance with traditional use. Full article
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17 pages, 3643 KiB  
Article
Ribes nigrum L. Extract-Mediated Green Synthesis and Antibacterial Action Mechanisms of Silver Nanoparticles
by Zaruhi Hovhannisyan, Marina Timotina, Jemma Manoyan, Lilit Gabrielyan, Margarit Petrosyan, Barbara Kusznierewicz, Agnieszka Bartoszek, Claus Jacob, Mikayel Ginovyan, Karen Trchounian, Naira Sahakyan and Muhammad Jawad Nasim
Antibiotics 2022, 11(10), 1415; https://doi.org/10.3390/antibiotics11101415 - 14 Oct 2022
Cited by 10 | Viewed by 2017
Abstract
Silver nanoparticles (Ag NPs) represent one of the most widely employed metal-based engineered nanomaterials with a broad range of applications in different areas of science. Plant extracts (PEs) serve as green reducing and coating agents and can be exploited for the generation of [...] Read more.
Silver nanoparticles (Ag NPs) represent one of the most widely employed metal-based engineered nanomaterials with a broad range of applications in different areas of science. Plant extracts (PEs) serve as green reducing and coating agents and can be exploited for the generation of Ag NPs. In this study, the phytochemical composition of ethanolic extract of black currant (Ribes nigrum) leaves was determined. The main components of extract include quercetin rutinoside, quercetin hexoside, quercetin glucuronide, quercetin malonylglucoside and quercitrin. The extract was subsequently employed for the green synthesis of Ag NPs. Consequently, R. nigrum leaf extract and Ag NPs were evaluated for potential antibacterial activities against Gram-negative bacteria (Escherichia coli ATCC 25922 and kanamycin-resistant E. coli pARG-25 strains). Intriguingly, the plant extract did not show any antibacterial effect, whilst Ag NPs demonstrated significant activity against tested bacteria. Biogenic Ag NPs affect the ATPase activity and energy-dependent H+-fluxes in both strains of E. coli, even in the presence of N,N’-dicyclohexylcarbodiimide (DCCD). Thus, the antibacterial activity of the investigated Ag NPs can be explained by their impact on the membrane-associated properties of bacteria. Full article
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26 pages, 4876 KiB  
Article
Phytochemical Profiling, In Vitro Biological Activities, and In-Silico Studies of Ficus vasta Forssk.: An Unexplored Plant
by Hanan Y. Aati, Mariyam Anwar, Jawaher Al-Qahtani, Areej Al-Taweel, Kashif-ur-Rehman Khan, Sultan Aati, Faisal Usman, Bilal Ahmad Ghalloo, Hafiz Muhammad Asif, Jafir Hussain Shirazi and Aliza Abbasi
Antibiotics 2022, 11(9), 1155; https://doi.org/10.3390/antibiotics11091155 - 26 Aug 2022
Cited by 11 | Viewed by 2802
Abstract
Ficus vasta Forssk. (Moraceae family) is an important medicinal plant that has not been previously investigated for its phytochemical and biological potential. Phytochemical screening, total bioactive content, and GCMS analysis were used to determine its phytoconstituents profile. Antioxidant, antibacterial, antifungal, anti-viral, cytotoxicity, thrombolytic, [...] Read more.
Ficus vasta Forssk. (Moraceae family) is an important medicinal plant that has not been previously investigated for its phytochemical and biological potential. Phytochemical screening, total bioactive content, and GCMS analysis were used to determine its phytoconstituents profile. Antioxidant, antibacterial, antifungal, anti-viral, cytotoxicity, thrombolytic, and enzyme inhibition activities were examined for biological evaluation. The plant extract exhibited the maximum total phenolic (89.47 ± 3.21 mg GAE/g) and total flavonoid contents (129.2 ± 4.14 mg QE/g), which may be related to the higher antioxidant potential of the extract. The extract showed strong α-amylase (IC50 5 ± 0.21 µg/mL) and α-glucosidase inhibition activity (IC50 5 ± 0.32 µg/mL). Significant results were observed in the case of antibacterial, antifungal, and anti-viral activities. The F. vasta extract inhibited the growth of HepG2 cells in a dose-dependent manner. The GCMS analysis of the extract provided the preliminary identification of 28 phytocompounds. In addition, the compounds identified by GCMS were subjected to in silico molecular docking analysis in order to identify any interactions between the compounds and enzymes (α-amylase and α-glucosidase). After that, the best-docked compounds were subjected to ADMET studies which provide information on pharmacokinetics, drug-likeness, physicochemical properties, and toxicity. The present study highlighted that the ethanol extract of F. vasta has antidiabetic, antimicrobial, anti-viral, and anti-cancer potentials that can be further explored for novel drug development. Full article
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