Background: Tuberculosis affects millions of people worldwide. The emergence of drug-resistant strains has made treatment more difficult. A drug discovery project initiated to screen natural products identified a lead stilbene compound, and structure function analysis of hundreds of analogs led to the discovery of the SK-03-92 stilbene lead compound with activity against several non-tuberculoid mycobacteria.
Methods: For this study, an MIC analysis and intracellular killing assay were performed to test SK-03-92 against grown in vitro as well as within murine macrophage cells.
Results: The MIC analysis showed that SK-03-92 had activity against in the range of 0.39 to 6.25 μg/mL, including activity against single-drug-resistant strains. Further, an intracellular kill assay demonstrated that the SK-03-92 lead compound killed cells within murine macrophage cells.
Conclusion: Together, the data show the SK-03-92 lead compound can kill bacteria within mammalian macrophages.
Download full-text PDF |
Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC10525840 | PMC |
| http://dx.doi.org/10.3390/antibiotics12091385 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Theranostic drugs represent an emerging path to deliver on the promise of precision medicine. However, bottlenecks remain in characterizing theranostic targets, identifying theranostic lead compounds, and tailoring theranostic drugs. To overcome these bottlenecks, we present the Theranostic Genome, the part of the human genome whose expression can be utilized to combine therapeutic and diagnostic applications.
View Article and Find Full Text PDFFuture increase in compound soil drought-heat extremes exacerbated by vegetation greening.
Nat Commun
December 2024
Institute of Carbon Neutrality, Sino-French Institute for Earth System Science, College of Urban and Environmental Sciences, Peking University, Beijing, China.
Compound soil drought and heat extremes are expected to occur more frequently with global warming, causing wide-ranging socio-ecological repercussions. Vegetation modulates air temperature and soil moisture through biophysical processes, thereby influencing the occurrence of such extremes. Global vegetation cover is broadly expected to increase under climate change, but it remains unclear whether vegetation greening will alleviate or aggravate future increases in compound soil drought-heat events.
View Article and Find Full Text PDFPhotoswitch dissociation from a G protein-coupled receptor resolved by time-resolved serial crystallography.
Nat Commun
December 2024
PSI Center for Life Sciences, Villigen PSI, Switzerland.
G protein-coupled receptors (GPCRs) are the largest family of cell surface receptors in humans. The binding and dissociation of ligands tunes the inherent conformational flexibility of these important drug targets towards distinct functional states. Here we show how to trigger and resolve protein-ligand interaction dynamics within the human adenosine A receptor.
View Article and Find Full Text PDFtargeting of AmpC beta-lactamases in : unveiling Piperenol B as a potent antimicrobial lead.
J Biomol Struct Dyn
December 2024
Department of Biotechnology, School of Bioengineering, College of Engineering and Technology, SRM Institute of Science and Technology, Kattankulathur, Chengalpattu, Tamilnadu, India.
Antimicrobial Resistance poses a major threat to human health worldwide. Microorganisms develop multi-drug resistance due to intrinsic factors, evolutionary chromosomal alterations, and horizontal gene transfer. , a common nosocomial bacterium, can cause various infections and is classified as multidrug-resistant.
View Article and Find Full Text PDFNovel Cinnamic Acid Derivatives Containing Naproxen as NLRP3 Inhibitors: Synthesis and Evaluation of Their Biological Activity.
Chem Biodivers
December 2024
Wuyi University, School of Pharmacy and Food Engineering, Yingbin Street NO.99, 529020, Jiangmen, CHINA.
Long-term use of naproxen can lead to serious side effects. Inspired by the biological activity of cinnamic acid, a series of cinnamic acid derivatives containing naproxen were designed, synthesized and explored their anti-inflammatory activities and mechanism in vitro. Our results indicated that all of naproxen derivatives showed more significant inhibition against lipopolysaccharide (LPS)-induced nitric oxide (NO) production and had lower degree of cytotoxicity than that of naproxen.
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!