SD-8, a novel therapeutic agent active against multidrug-resistant Gram positive cocci |
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Authors: | Biswajit Mishra Vipul Kumar Srivastava Rama Chaudhry Rishi Kumar Somvanshi Abhay Kumar Singh Kamaldeep Gill Ramesh Somvanshi Ishan Kumar Patro Sharmistha Dey |
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Institution: | (1) Department of Biophysics, All India Institute of Medical Sciences, Ansari Nagar, New Delhi, 110029, India;(2) Department of Microbiology, All India Institute of Medical Sciences, New Delhi, India;(3) Division of Pathology, Indian Veterinary Research Institute, Izatnagar, Bareilly, UP, India;(4) School of Studies in Neuroscience, Jiwaji University, Gwalior, MP, India; |
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Abstract: | Anti-bacterial drug resistance is one of the most critical concerns among the scientist worldwide. The novel antimicrobial
decapeptide SD-8 is designed and its minimal inhibitory concentration and therapeutic index (TI) was found in the range of
1–8 μg/ml and 45–360, respectively, against major group of Gram positive pathogens (GPP). The peptide was also found to be
least hemolytic at a concentration of 180 μg/ml, i.e., nearly 77 times higher than its average effective concentration. The
kinetics assay showed that the killing time is 120 min for methicillin-sensitive Staphylococcus aureus (MSSA) and 90 min for methicillin-resistant S. aureus (MRSA). Membrane permeabilization is the cause of peptide antimicrobial activity as shown by the transmission electron microscopy
studies. The peptide showed the anti-inflammatory property by inhibiting COX-2 with a K
D and K
i values of 2.36 × 10−9 and 4.8 × 10−8 M, respectively. The peptide was also found to be effective in vivo as derived from histopathological observations in a Staphylococcal
skin infection rat model with MRSA as causative organism. |
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Keywords: | |
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