Bio-Organic Chemistry Unit, Institute of Biomolecular Chemistry, Consiglio Nazionale delle Ricerche, Via Campi Flegrei 34, Pozzuoli, 80078 Naples, Italy.
Consorzio Italbiotec, Via Gaudenzio Fantoli, 16/15, 20138 Milano, Italy.
Mar Drugs. 2021 Nov 16;19(11):640. doi: 10.3390/md19110640.
The marine environment is potentially a prolific source of small molecules with significant biological activities. In recent years, the development of new chromatographic phases and the progress in cell and molecular techniques have facilitated the search for marine natural products (MNPs) as novel pharmacophores and enhanced the success rate in the selection of new potential drug candidates. However, most of this exploration has so far been driven by anticancer research and has been limited to a reduced number of taxonomic groups. In this article, we report a test study on the screening potential of an in-house library of natural small molecules composed of 285 samples derived from 57 marine organisms that were chosen from among the major eukaryotic phyla so far represented in studies on bioactive MNPs. Both the extracts and SPE fractions of these organisms were simultaneously submitted to three different bioassays-two phenotypic and one enzymatic-for cytotoxic, antidiabetic, and antibacterial activity. On the whole, the screening of the MNP library selected 11 potential hits, but the distribution of the biological results showed that SPE fractionation increased the positive score regardless of the taxonomic group. In many cases, activity could be detected only in the enriched fractions after the elimination of the bulky effect due to salts. On a statistical basis, sponges and molluscs were confirmed to be the most significant source of cytotoxic and antimicrobial products, but other phyla were found to be effective with the other therapeutic targets.
海洋环境是具有重要生物活性的小分子的潜在丰富来源。近年来,新型色谱相的发展以及细胞和分子技术的进步,促进了海洋天然产物(MNPs)作为新型药效团的寻找,并提高了选择新的潜在药物候选物的成功率。然而,到目前为止,这种探索主要是由抗癌研究驱动的,而且仅限于少数分类群。在本文中,我们报告了一项关于从迄今为止在生物活性 MNPs 研究中代表的主要真核生物门中选择的 57 种海洋生物中获得的 285 个天然小分子的内部天然小分子文库的筛选潜力的测试研究。这些生物体的提取物和 SPE 馏分同时提交给了三种不同的生物测定法——两种表型和一种酶法——用于细胞毒性、抗糖尿病和抗菌活性。总的来说,MNPs 文库的筛选选择了 11 种潜在的有效成分,但生物结果的分布表明,无论分类群如何,SPE 分级都会增加阳性评分。在许多情况下,在消除由于盐分引起的体积效应后,仅在富集馏分中才能检测到活性。从统计学上讲,海绵和软体动物被证实是细胞毒性和抗菌产品的最主要来源,但其他门也被发现对其他治疗靶点有效。