Section of Pharmaceutical Chemistry, Department of Biological, Chemical and Pharmaceutical Sciences and Technologies (STEBICEF), University of Palermo, Via Archirafi 32, 90123 Palermo, Italy.
Department of Earth and Sea Science (DiSTeM), University of Palermo, Viale delle Scienze Blg. 16, 90128 Palermo, Italy.
Int J Mol Sci. 2023 Mar 15;24(6):5650. doi: 10.3390/ijms24065650.
The demand for new molecules to counter bacterial resistance to antibiotics and tumor cell resistance is increasingly pressing. The Mediterranean seagrass is considered a promising source of new bioactive molecules. Polypeptide-enriched fractions of rhizomes and green leaves of the seagrass were tested against Gram-positive (e.g., , ) and Gram-negative bacteria (e.g., , ), as well as towards the yeast . The aforementioned extracts showed indicative MIC values, ranging from 1.61 μg/mL to 7.5 μg/mL, against the selected pathogens. Peptide fractions were further analyzed through a high-resolution mass spectrometry and database search, which identified nine novel peptides. Some discovered peptides and their derivatives were chemically synthesized and tested in vitro. The assays identified two synthetic peptides, derived from green leaves and rhizomes of , which revealed interesting antibiofilm activity towards , and (BIC equal to 17.7 μg/mL and 70.7 μg/mL). In addition, the natural and derivative peptides were also tested for potential cytotoxic and apoptosis-promoting effects on HepG2 cells, derived from human hepatocellular carcinomas. One natural and two synthetic peptides were proven to be effective against the "in vitro" liver cancer cell model. These novel peptides could be considered a good chemical platform for developing potential therapeutics.
对能够克服细菌对抗生素的耐药性和肿瘤细胞耐药性的新型分子的需求日益迫切。地中海海草被认为是新型生物活性分子的有前途的来源。对该海草的根茎和绿叶中富含多肽的部分进行了针对革兰氏阳性菌(例如, , )和革兰氏阴性菌(例如, , )以及酵母 的测试。上述提取物对所选病原体的指示性 MIC 值范围为 1.61 μg/mL 至 7.5 μg/mL。肽部分通过高分辨率质谱和数据库搜索进行了进一步分析,鉴定出了 9 种新型肽。一些发现的肽及其衍生物已被化学合成并进行了体外测试。这些检测鉴定出两种合成肽,分别来自 和 的绿叶和根茎,它们对 、 和 (BIC 等于 17.7 μg/mL 和 70.7 μg/mL)表现出有趣的抗生物膜活性。此外,还测试了天然肽及其衍生物对源自人肝癌的 HepG2 细胞的潜在细胞毒性和促进细胞凋亡作用。一种天然肽和两种合成肽被证明对“体外”肝癌细胞模型有效。这些新型肽可以被认为是开发潜在治疗剂的良好化学平台。