Mathew Basil, Olli Sudar, Guru Ankeeta, Nagaraj Ramakrishanan
CSIR-Centre for Cellular and Molecular Biology, Uppal Road, Hyderabad 500 007, India.
Virupaksha Life Sciences Pvt Ltd, CRTDH, CSIR-Centre for Cellular and Molecular Biology Annexe-II, Hyderabad 500 007, India.
Bioorg Med Chem Lett. 2017 Aug 1;27(15):3264-3266. doi: 10.1016/j.bmcl.2017.06.031. Epub 2017 Jun 12.
Antibiofilm activity of several human defensin analogs that have the ability to kill planktonic bacteria, against pre-established biofilms of Escherichia coli MG1655 and Staphylococcus aureus NCTC 8530 were examined. Linear and linear fatty acylated analogs did not show any activity while disulfide constrained analogs disrupted pre-established S. aureus biofilms. Chimeric analogs of human β-defensin 1 and θ-defensin, hBTD-1 and [d]hBTD-1 were highly active against S. aureus biofilms. Among the analogs tested, only the d-enantiomer [d]hBTD-1 showed activity against E. coli biofilm. Our study provides insights into the structural requirements for the eradication of pre-established biofilms in defensin analogs.
研究了几种具有杀死浮游细菌能力的人防御素类似物对大肠杆菌MG1655和金黄色葡萄球菌NCTC 8530预先形成的生物膜的抗生物膜活性。线性和线性脂肪酰化类似物没有显示出任何活性,而二硫键约束的类似物破坏了预先形成的金黄色葡萄球菌生物膜。人β-防御素1和θ-防御素的嵌合类似物hBTD-1和[d]hBTD-1对金黄色葡萄球菌生物膜具有高活性。在所测试的类似物中,只有d-对映体[d]hBTD-1对大肠杆菌生物膜显示出活性。我们的研究为防御素类似物中根除预先形成的生物膜的结构要求提供了见解。