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Revolutionizing Quinolone Development for DNA Gyrase Targeting; Discovering the Promising Approach to Fighting Microbial Infections
Available online: 16 October 2024More LessDNA gyrase is a type II topoisomerase enzyme that can cause negative supercoiling in DNA by using the energy produced by ATP hydrolysis. There are two main types of topoisomerases: type I and type II. Type I enzymes cut a single strand of DNA and are further classified as type IA if they connect to a 5′ phosphate of DNA, or type IB if they link to a 3′ phosphate. Type II topoisomerases break both strands, creating a staggered double-strand break.
Antimicrobial resistance is a major concern for the global healthcare system. Resistance is the ability of microorganisms to neutralize and withstand antimicrobial drugs previously used to treat microbial infections. Some known classes of DNA gyrase inhibitors are coumarins, cyclothialidines, and quinolones. Antimicrobial medicines such as quinolones have been widely used to treat microbiological diseases. However, the increased use of quinolones has led to the emergence of quinolone-resistant bacteria, which poses a serious risk to public health. Microorganisms can cause resistance due to changes in the target enzymes, DNA gyrase, and topoisomerase IV, which are responsible for transcription and DNA replication. Additionally, differences in drug entry and efflux may also play a role in resistance. Plasmids that produce the Qnr protein can mediate resistance to quinolones by protecting the quinolone targets from inhibition. This review aims to revolutionize the discovery of quinolone-based antibiotics, specifically targeting DNA gyrase, a critical enzyme in bacterial DNA replication, to enhance the efficacy and specificity of anti-microbail agents against microbial infections.
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Antibacterial and Insecticidal Activities of Bacillus licheniformis SKS7 Methanolic Extract
Available online: 07 October 2024More LessBackgroundMicrobes are a rich source of antibacterial and anti-insect molecules. Due to rising antibiotic and anti-insect resistance in various sectors of the society, it is important to identify new compounds that may address these issues.
Aims and ObjectiveThis study aimed to explore the bacteria isolated from soil to identify new molecules with antibacterial and anti-insect activity. Further, the current study is aimed at testing and characterizing antimicrobial and insecticidal properties of methanolic extracts from four different soil bacteria
MethodsThis study reports the isolation and characterization of soil bacteria by morphological, biochemical, and molecular analysis. The antibacterial potential of methanolic extracts of four bacterial strains were tested using an agar well diffusion assay, along with development and survival of Spodoptera litura. Fractionation of the methanolic extract was performed by chromatography, and the separated fractions were tested for their antibacterial activity.
ResultsThe bacteria belong to Bacillus, Exiguobacterium, and Microbacterium species. The extract of Bacillus licheniformis SKS7 exhibited maximum antibacterial activity against all tested microbes, including human pathogens. Extract from the same microbe also showed maximum anti-insect activity against Spodoptera litura by significantly increasing the pupal period by as much as 80% and hence extending the time to adult emergence. Morphological abnormalities like deformed wings, deformed pupae, and failure to emerge from pupae were also observed. Purification of the extract by HPLC and gel permeation chromatography helped us to observe a low molecular weight protein that may be responsible for its antibacterial activity.
ConclusionMethanolic extract of Bacillus licheniformis SKS7 contains bioactive molecules with antibacterial and anti-insect activities. Further characterization and identification of these molecules may form the basis for the development of novel antibacterial drugs and insecticidal molecules in the future.
from microbes has slowed since the late 1980s due to hardships in finding novel active compounds and reg
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A Comprehensive Review on the Antimicrobial Activities and Structure-Activity Relationships (SARs) of Rhodanine Analogues
Available online: 25 September 2024More LessRhodanines are five-member heterocyclics having sulfur, nitrogen, and oxygen atoms in their ring structure and exhibit potent as well as a broad range of pharmacological activities. They are thiazolidine derivatives and are well-known in medicinal chemistry for their wide spectrum of antimicrobial activities. Various modifications can be made to the structure of the rhodanine ring. Studies in recent years have validated the possibility of the potential of rhodanine derivatives to exhibit antimicrobial activity against both Gram-positive and Gram-negative bacterial strains, as well as mycobacterial and fungal strains. In this review, the synthesis, biological activity, and Structure-activity Relationships (SARs) of molecules based on rhodanine against different microbes have been described
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