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Full-Text Articles in Medicine and Health Sciences
Synthesis And Inhibitory Activity Of Machaeridiol-Based Novel Anti-Mrsa And Anti-Vre Compounds And Their Profiling For Cancer-Related Signaling Pathways, Mallika Kumarihamy, Siddharth Tripathi, Premalatha Balachandran, Bharathi Avula
Synthesis And Inhibitory Activity Of Machaeridiol-Based Novel Anti-Mrsa And Anti-Vre Compounds And Their Profiling For Cancer-Related Signaling Pathways, Mallika Kumarihamy, Siddharth Tripathi, Premalatha Balachandran, Bharathi Avula
Faculty and Student Publications
Three unique 5,6-seco-hexahydrodibenzopyrans (seco-HHDBP) machaeridiols A–C, reported previously from Machaerium Pers., have displayed potent activities against methicillin-resistant Staphylococcus aureus (MRSA), vancomycin-resistant Enterococcus faecium, and E. faecalis (VRE). In order to enrich the pipeline of natural product-derived antimicrobial compounds, a series of novel machaeridiol-based analogs (1–17) were prepared by coupling stemofuran, pinosylvin, and resveratrol legends with monoterpene units R-(−)-α-phellandrene, (−)-p-mentha-2,8-diene-1-ol, and geraniol, and their inhibitory activities were profiled against MRSA ATCC 1708, VRE ATCC 700221, and cancer signaling pathways. Compounds 5 and 11 showed strong in vitro activities with MIC values of 2.5 μg/mL and 1.25 μg/mL against MRSA, respectively, and …
Synergistic Antibacterial Activity With Conventional Antibiotics And Mechanism Of Action Of Shikonin Against Methicillin‐Resistant Staphylococcus Aureus, Qian Qian Li, Hee Sung Chae, Ok Hwa Kang, Dong Yeul Kwon
Synergistic Antibacterial Activity With Conventional Antibiotics And Mechanism Of Action Of Shikonin Against Methicillin‐Resistant Staphylococcus Aureus, Qian Qian Li, Hee Sung Chae, Ok Hwa Kang, Dong Yeul Kwon
Faculty and Student Publications
Methicillin‐resistant Staphylococcus aureus (MRSA) is a troublesome pathogen that poses a global threat to public health. Shikonin (SKN) isolated from Lithospermum erythrorhizon (L. erythro-rhizon) possesses a variety of biological activities. This study aims to explore the effect of the combined application of SKN and traditional antibiotics on the vitality of MRSA and the inherent anti-bacterial mechanism of SKN. The synergies between SKN and antibiotics against MRSA and its clinical strain have been demonstrated by the checkerboard assay and the time‐kill assay. The effect of SKN on disrupting the integrity and permeability of bacterial cell membranes was verified by a nucleotide …