Lipidated α/Sulfono-α-AA heterogeneous peptides as antimicrobial agents for MRSA |
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| Institution: | 1. Department of Chemistry, University of South Florida, 4202 East Fowler Avenue, Tampa, FL 33620, United States;2. College of Chemistry and Chemical Engineering, Central South University, Changsha 410083, PR China;3. School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, PR China;1. Department of Chemistry, Lomonosov Moscow State University, Leninskie Gory, 1–3, Moscow 119991, Russian Federation;2. EDASA Scientific, Via Stingi 37, San Salvo 66050, Italy;3. Department of Molecular Microbiology and Immunology, Nagasaki University Graduate School of Biomedical Sciences, 1-12-4 Sakamoto, Nagasaki 852-8523, Japan;4. Dulbecco Telethon Laboratory of Prions & Amyloids, Department of Cellular, Computational and Integrative Biology (CIBIO), University of Trento, Via Sommarive 9, Trento 38123, Italy;5. A.N. Nesmeyanov Institute of Organoelement Compounds, Russian Academy of Sciences, Vavilov St. 28, Moscow, Russian Federation;1. Department of Radiation Oncology, Emory University School of Medicine, USA;2. Department of Radiology and Image Sciences, Emory University School of Medicine, USA;3. Winship Cancer Institute, Atlanta, GA 30322, USA;1. Laboratory for Chemistry and Life Science, Institute of Innovative Research, Tokyo Institute of Technology, 4259 Nagatsuta-cho, Midori-ku, Yokohama 226-8503, Japan;2. School of Life Science and Technology, Tokyo Institute of Technology, 4259 Nagatsuta-cho, Midori-ku, Yokohama 226-8501, Japan;1. Department of Phytochemistry, Medicinal Plants and Drugs Research Institute, Shahid Beheshti University, G. C., Evin, 1983963113 Tehran, Iran;2. Swiss Tropical and Public Health Institute, Basel, Switzerland;3. University of Basel, Basel, Switzerland;4. National and Medical Sciences Research Center, University of Nizwa, P.O. Box 33, Birkat Al-Mauz, Nizwa 611, Oman;1. Department of Pesticide Chemistry, College of Science, China Agricultural University, Beijing, China;2. State Key Laboratory for Biology of Plant Diseases and Insect Pests, Institute of Plant Protection and Shenzhen Agricultural Genome Research Institute, Chinese Academy of Agricultural Sciences, Beijing, China |
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| Abstract: | Though antibiotics have been used for decades to treat bacterial infections, there is a great need for new treatment methods. Bacteria are becoming resistant to conventional antibiotics, as is the case with Methicillin resistant Staphylococcus aureus (MRSA). Herein we report the design of a series of lipidated α/Sulfono-α-AA heterogeneous peptides as mimics for Host Defense Peptides (HDPs). Utilizing fluorescence microscopy and depolarization techniques, our compounds demonstrate the ability to kill Gram-positive bacteria through cell membrane disruption. This mechanism of action makes it difficult for bacteria to develop resistance. Further time kill studies and hemolytic assays have also proven these compounds to be efficient in their ability to eradicate bacteria cells while remaining non-toxic to human red blood cells. This new class of peptidomimetics shows promise for the future antibiotic treatment of MRSA. |
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| Keywords: | Host Defense Peptides Peptidomimetics Bacterial resistance Lipidation Antimicrobial |
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