Department of Biological Sciences, Faculty of Science and Technology, Sunway University, 47500, Subang Jaya, Selangor, Malaysia.
International Center for Chemical and Biological Sciences, H.E.J. Research Institute of Chemistry, University of Karachi, Karachi, Pakistan.
Appl Microbiol Biotechnol. 2017 Jan;101(1):253-286. doi: 10.1007/s00253-016-7872-2. Epub 2016 Oct 14.
Infectious diseases remain a significant threat to human health, contributing to more than 17 million deaths, annually. With the worsening trends of drug resistance, there is a need for newer and more powerful antimicrobial agents. We hypothesized that animals living in polluted environments are potential sources of antimicrobials. Under polluted milieus, organisms such as cockroaches encounter different types of microbes, including superbugs. Such creatures survive the onslaught of superbugs and are able to ward off disease by producing antimicrobial substances. Here, we characterized antibacterial properties in extracts of various body organs of cockroaches (Periplaneta americana) and showed potent antibacterial activity in crude brain extract against methicillin-resistant Staphylococcus aureus and neuropathogenic Escherichia coli K1. The size-exclusion spin columns revealed that the active compound(s) are less than 10 kDa in molecular mass. Using cytotoxicity assays, it was observed that pre-treatment of bacteria with lysates inhibited bacteria-mediated host cell cytotoxicity. Using spectra obtained with LC-MS on Agilent 1290 infinity liquid chromatograph, coupled with an Agilent 6460 triple quadruple mass spectrometer, tissues lysates were analysed. Among hundreds of compounds, only a few homologous compounds were identified that contained the isoquinoline group, chromene derivatives, thiazine groups, imidazoles, pyrrole-containing analogs, sulfonamides, furanones, and flavanones and known to possess broad-spectrum antimicrobial properties and anti-inflammatory, anti-tumour, and analgesic properties. Further identification, characterization, and functional studies using individual compounds can act as a breakthrough in developing novel therapeutics against various pathogens including superbugs.
传染病仍然是人类健康的重大威胁，每年导致超过 1700 万人死亡。随着耐药趋势的恶化，我们需要更新、更强大的抗菌剂。我们假设生活在污染环境中的动物可能是抗菌剂的潜在来源。在污染的环境中，蟑螂等生物会遇到包括超级细菌在内的不同类型的微生物。这些生物在超级细菌的攻击下幸存下来，并通过产生抗菌物质来抵御疾病。在这里，我们描述了蟑螂（美洲大蠊）各种体器官提取物的抗菌特性，并显示粗脑提取物对耐甲氧西林金黄色葡萄球菌和神经致病性大肠杆菌 K1 具有很强的抗菌活性。分子筛柱表明，活性化合物的分子量小于 10 kDa。通过细胞毒性测定，观察到用裂解物预处理细菌可以抑制细菌介导的宿主细胞细胞毒性。使用安捷伦 1290 无限液相色谱仪和安捷伦 6460 三重四极杆质谱仪获得的 LC-MS 谱图对组织裂解物进行分析。在数百种化合物中，只鉴定出了少数含有异喹啉基团、色烯衍生物、噻嗪基团、咪唑、吡咯类似物、磺胺类、呋喃酮和黄酮类的同源化合物，这些化合物具有广谱抗菌、抗炎、抗肿瘤和镇痛特性。使用单个化合物进行进一步的鉴定、表征和功能研究，可以成为开发针对各种病原体（包括超级细菌）的新型治疗方法的突破。
