Mahajan Girish Badrinath, Balachandran Lakshmi
Anti-infective screening and Prokaryote isolation, Department of Natural Products, Piramal Life Sciences Limited, 1-Nirlon Complex, Off Western Express Highway, Goregaon (East), Mumbai-400 063, India.
Front Biosci (Elite Ed). 2012 Jan 1;4(1):240-53. doi: 10.2741/373.
The discovery of Penicillin in 1928 and that of Streptomycin in 1943, has been pivotal to the exploration of nature as a source of new lead molecules. Globally, the microbiologist today is acknowledged as a crucial player in the drug discovery program. The microbial products, especially those from actinomycetes have been a phenomenal success for the past seven decades. Bioprospecting for new leads are often compounded by the recurrence of known antibiotics in newer microbial isolates. Despite all these deterrents, actinomycetes have proved to be a sustained mine of novel antibiotics, which selectively destroys the pathogens without affecting the host tissues. Each of these antibiotics is unique in their mode of action. Their versatility and immense economic value is something, which is extremely noteworthy. The anti-infective turn-over of over 79 billion US dollars in 2009, includes about 166 antibiotics and derivatives such as the Beta-lactam peptide antibiotics, the macrolide polyketide erythromycin, tetracyclines, aminoglycosides, daptomycin, tigecycline, most of which are produced by actinomycetes (1). Actinomycetes continue to play a highly significant role in drug discovery and development. Among the bioactive compounds that have been obtained so far from microbes, 45 % are produced by actinomycetes, 38 % by fungi and 17 % by unicellular eubacteria (2). Further many chemically synthesized drugs owe their origin to natural sources. In this review article, we highlight the recent antibiotics from actinomycetes with emphasis on their source, structures, activity, mechanism of action and current status.
1928年青霉素的发现以及1943年链霉素的发现，对于探索作为新先导分子来源的自然至关重要。在全球范围内，微生物学家如今被公认为药物研发计划中的关键角色。在过去的七十年里，微生物产物，尤其是放线菌产生的产物取得了巨大成功。寻找新先导物的生物勘探常常因新的微生物分离物中出现已知抗生素而变得复杂。尽管存在所有这些阻碍，但放线菌已被证明是新型抗生素的持续来源，这些抗生素能选择性地破坏病原体而不影响宿主组织。每种抗生素的作用方式都很独特。它们的多功能性和巨大的经济价值非常值得关注。2009年抗感染药物销售额超过790亿美元，其中包括约166种抗生素及其衍生物，如β-内酰胺肽抗生素、大环内酯聚酮类红霉素、四环素、氨基糖苷类、达托霉素、替加环素，其中大部分是由放线菌产生的（1）。放线菌在药物研发中继续发挥着非常重要的作用。在迄今为止从微生物中获得的生物活性化合物中，45%由放线菌产生，38%由真菌产生，17%由单细胞真细菌产生（2）。此外，许多化学合成药物也起源于天然来源。在这篇综述文章中，我们重点介绍了放线菌产生的最新抗生素，包括它们的来源、结构、活性、作用机制和现状。
