Laboratory of Organic and Pharmaceutical Chemistry, Department of Chemical Sciences, Faculty of Pharmacy, University of Porto, Rua de Jorge Viterbo Ferreira, 228, 4050-313 Porto, Portugal.
Interdisciplinary Center of Marine and Environmental Investigation (CIIMAR/CIMAR), Edifício do Terminal de Cruzeiros do Porto de Leixões, Av. General Norton de Matos s/n, 4050-208 Matosinhos, Portugal.
Molecules. 2019 Jan 10;24(2):243. doi: 10.3390/molecules24020243.
Marine organisms represent almost half of total biodiversity and are a very important source of new bioactive substances. Within the varied biological activities found in marine products, their antimicrobial activity is one of the most relevant. Infectious diseases are responsible for high levels of morbidity and mortality and many antimicrobials lose their effectiveness with time due to the development of resistance. These facts justify the high importance of finding new, effective and safe anti-infective agents. Among the variety of biological activities of marine xanthone derivatives, one that must be highlighted is their anti-infective properties. In this work, a literature review of marine xanthones with anti-infective activity, namely antibacterial, antifungal, antiparasitic and antiviral, is presented. Their structures, biological activity, sources and the methods used for bioactivity evaluation are described. The xanthone derivatives are grouped in three sets: xanthones, hydroxanthones and glycosylated derivatives. Moreover, molecular descriptors, biophysico-chemical properties, and pharmacokinetic parameters were calculated, and the chemical space occupied by marine xanthone derivatives is recognized. The chemical space was compared with marketed drugs and framed accordingly to the drug-likeness concept in order to profile the pharmacokinetic of anti-infective marine xanthone derivatives.
海洋生物几乎占总生物多样性的一半,是新生物活性物质的重要来源。在海洋产品中发现的各种生物活性中,其抗菌活性是最相关的一种。传染病是发病率和死亡率高的原因,而且许多抗菌药物由于耐药性的发展而随着时间的推移失去效力。这些事实证明寻找新的、有效和安全的抗感染药物非常重要。在海洋酮衍生物的各种生物活性中,必须强调的是其抗感染特性。在这项工作中,对具有抗感染活性的海洋酮,即抗菌、抗真菌、抗寄生虫和抗病毒活性进行了文献综述。描述了它们的结构、生物活性、来源以及用于生物活性评估的方法。将酮衍生物分为三组:酮、羟基酮和糖基化衍生物。此外,还计算了分子描述符、生物物理化学性质和药代动力学参数,并识别了海洋酮衍生物的化学空间。将化学空间与市售药物进行比较,并根据药物相似性概念进行框定,以分析抗感染海洋酮衍生物的药代动力学特征。