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Synthesis and Antimicrobial Evaluation of 1,4-Naphthoquinone Derivatives as Potential Antibacterial Agents
Authors:Dr. Palanisamy Ravichandiran  Prof. Maciej Masłyk  Dr. Sunirmal Sheet  Dr. Monika Janeczko  Dr. Dhanraj Premnath  Prof. Ae Rhan Kim  Prof. Byung-Hyun Park  Prof. Myung-Kwan Han  Prof. Dong Jin Yoo
Affiliation:1. Department of Life Science, Department of Energy Storage/Conversion Engineering of Graduate School, and Hydrogen and Fuel Cell Research Center, Chonbuk National University, Jeollabuk-do, 54896 Republic of Korea;2. Department of Molecular Biology, Faculty of Biotechnology and Environmental Sciences, The John Paul II Catholic University of Lublin, ul. Konstantynów 1i, 20-708 Lublin, Poland;3. Department of Forest Science and Technology, College of Agriculture and Life Sciences, Chonbuk National University, 567 Baekje-daero, Deokjin-gu, Jeonju-si, 561-756, Jeollabuk-do Republic of Korea;4. Department of Biotechnology, Karunya Institute of Technology and Science, School of Agriculture and Biosciences, Karunya Nagar, Coimbatore, 641114, Tamil Nadu India;5. R&D Center for CANUTECH, Business Incubation Center, Department of Bioenvironmental Chemistry, Chonbuk National University, Jeollabuk-do, 54896 Republic of Korea.;6. Department of Biochemistry, Chonbuk National University Medical School, Jeollabuk-do, 54896 Republic of Korea;7. Department of Microbiology, Chonbuk National University Medical School, Jeollabuk-do, 54896 Republic of Korea
Abstract:1,4-Naphthoquinones are an important class of compounds present in a number of natural products. In this study, a new series of 1,4-naphthoquinone derivatives were synthesized. All the synthesized compounds were tested for in vitro antimicrobial activity. In this present investigation, two Gram-positive and five Gram-negative bacterial strains and one pathogenic yeast strain were used to determine the antibacterial activity. Naphthoquinones tested for its antibacterial potencies, among seven of them displayed better antimicrobial activity against Staphylococcus aureus (S. aureus; 30–70 μg/mL). Some of the tested compounds showed moderate to low antimicrobial activity against Pseudomonas aeruginosa (P. aeruginosa) and Salmonella bongori (S. bongori; 70–150 μg/mL). In addition, most active compounds against S. aureus were evaluated for toxicity to human blood cells using a hemolysis assay. For better understanding, reactive oxygen species (ROS) generation, time-kill kinetic study, and apoptosis, necrosis responses were investigated for three representative compounds.
Keywords:naphthoquinone derivatives  antimicrobial activity  hemolysis  reactive oxygen species  necrosis
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