With the increasing resistance of bacteria to current antibiotics, novel compounds are urgently needed to treat bacterial infections. Streptozotocin (STZ) is a natural product that has broad-spectrum antibiotic activity, albeit with limited use because of its toxicity to pancreatic β cells. In an attempt to derivatize STZ through structural modification at the C3 position, we performed the synthesis of three novel STZ analogues by making use of our recently developed regioselective oxidation protocol. Keto-STZ () shows the highest inhibition of bacterial growth (minimum inhibitory concentration (MIC) and viability assays), but is also the most cytotoxic compound. Pre-sensitizing the bacteria with GlcNAc increased the antimicrobial effect, but did not result in complete killing. Interestingly, -STZ () revealed moderate concentration-dependent antimicrobial activity and no cytotoxicity towards β cells, and deoxy-STZ () showed no activity at all.
Download full-text PDF |
Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7235802 | PMC |
| http://dx.doi.org/10.3390/antibiotics9040182 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Identification and Characterization of a New Thermophilic κ-Carrageenan Sulfatase.
J Agric Food Chem
January 2025
Faculty of Chemistry, Biotechnology, and Food Science, NMBU Norwegian University of Life Sciences, P.O. Box 5003, 1432 Aas, Norway.
Carrageenans are sulfated polysaccharides found in the cell wall of certain red seaweeds. They are widely used in the food industry for their gelling and stabilizing properties. In nature, carrageenans undergo enzymatic modification and degradation by marine organisms.
View Article and Find Full Text PDFExploring the Inhibition of α-Carbonic Anhydrase by Sulfonamides: Insights into Potential Drug Targeting.
Int J Mol Sci
December 2024
Neurofarba Department, Section of Pharmaceutical Sciences, University of Florence, Via Ugo Schiff 6, Sesto Fiorentino, 50019 Florence, Italy.
, the causative agent of toxoplasmosis, is a protozoan parasite capable of infecting a wide range of hosts, posing significant health risks, particularly to immunocompromised individuals and congenital transmission. Current therapeutic options primarily target the active tachyzoite stage but are limited by issues such as toxicity and incomplete efficacy. As a result, there is an urgent need for alternative therapies that can selectively target parasite-specific mechanisms critical for metabolic processes and host-parasite interactions.
View Article and Find Full Text PDFExploring the Chemical Features and Biomedical Relevance of Cell-Penetrating Peptides.
Int J Mol Sci
December 2024
Research Unit on Computational Biology and Drug Design, Children's Hospital of Mexico Federico Gómez, Mexico City 06720, Mexico.
Cell-penetrating peptides (CPPs) are a diverse group of peptides, typically composed of 4 to 40 amino acids, known for their unique ability to transport a wide range of substances-such as small molecules, plasmid DNA, small interfering RNA, proteins, viruses, and nanoparticles-across cellular membranes while preserving the integrity of the cargo. CPPs exhibit passive and non-selective behavior, often requiring functionalization or chemical modification to enhance their specificity and efficacy. The precise mechanisms governing the cellular uptake of CPPs remain ambiguous; however, electrostatic interactions between positively charged amino acids and negatively charged glycosaminoglycans on the membrane, particularly heparan sulfate proteoglycans, are considered the initial crucial step for CPP uptake.
View Article and Find Full Text PDFEffects of Doping on Elastic Strain in Crystalline Ge-Sb-Te.
Materials (Basel)
December 2024
School of Materials Science and Engineering, Kumoh National Institute of Technology, Gumi 39177, Republic of Korea.
Phase-change random access memory (PcRAM) faces significant challenges due to the inherent instability of amorphous GeSbTe (GST). While doping has emerged as an effective method for amorphous stabilization, understanding the precise mechanisms of structural modification and their impact on material stability remains a critical challenge. This study provides a comprehensive investigation of elastic strain and stress in crystalline lattices induced by various dopants (C, N, and Al) through systematic measurements of film thickness changes during crystallization.
View Article and Find Full Text PDFAffecting of Glyphosate Tolerance and Metabolite Content in Transgenic Overexpressing Gene from .
Plants (Basel)
December 2024
State Key Laboratory for Biology of Plant Diseases and Insect Pests, Institute of Plant Protection, Chinese Academy of Agricultural Sciences, Beijing 100193, China.
Long-term use of the global non-selective herbicide glyphosate for weed control has caused resistance in weeds. Overproducing of the target of glyphosate 5-enolpyruvylshikimate-3-phosphate synthase (EPSPS) is one of the resistance mechanisms in weeds. However, few studies have measured the effects on tolerance levels and metabolite content in model plant species overexpressing from weeds.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!