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首页> 外文期刊>The Lancet infectious diseases >Potential of marine natural products against drug-resistant bacterial infections
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Potential of marine natural products against drug-resistant bacterial infections

机译:海洋天然产品抵抗耐药细菌感染的潜力

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摘要

Natural products have been a rich source of compounds with structural and chemical diversity for drug discovery. However, antibiotic resistance in bacteria has been reported for nearly every antibiotic once it is used in clinical practice. In the past decade, pharmaceutical companies have reduced their natural product discovery projects because of challenges, such as high costs, low return rates, and high rediscovery rates. The largely unexplored marine environment harbours substantial diversity and is a large resource to discover novel compounds with novel modes of action, which is essential for the treatment of drug-resistant bacterial infections. In this Review, we report compounds derived from marine sources that have shown in-vivo and in-vitro efficacy against drug-resistant bacteria. Analysis of the physicochemical properties of these marine natural products with activity against drug-resistant bacteria showed that 60% of the compounds have oral bioavailability potential. Their overall distribution pattern of drug characteristics agrees with the observation that marketed antibacterial drugs have a polar distribution, with a lower median calculated logP. The aim of this Review is to summarise the diversity of these marine natural products, with a special focus on analysis of drug bioavailability. Such biologically active compounds, with high degrees of bioavailability, have the potential to be developed as effective drugs against infectious diseases.
机译:天然产品是具有富含药物发现的结构和化学多样性的丰富化合物来源。然而,一旦在临床实践中使用,已经报道了几乎每种抗生素都报道了细菌中的抗生素抗性。在过去的十年中,药品公司因挑战而减少了自然产品发现项目,例如高成本,低回归率和高重新发现率。主要是未开发的海洋环境港口大量多样性,并且是一种探索具有新型作用方式的新化合物的大资源,这对于治疗耐药细菌感染至关重要。在该综述中,我们报告衍生自导航含量的海洋来源的化合物和对耐药细菌的体外效果。抗耐药细菌活性的这些海洋天然产物的物理化学性质的分析表明,60%的化合物具有口服生物利用度潜力。它们的整体分布模式的药物特征同意,销售的抗菌药物具有极性分布的观察,较低的中值计算的LOGP。本综述的目的是总结这些海洋天然产品的多样性,特别关注对药物生物利用度的分析。这种具有高生物利用度的生物活性化合物具有潜在的措施,潜在的抗传染病的有效药物。

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