Barashkova Anna S, Sadykova Vera S, Salo Victoria A, Zavriev Sergey K, Rogozhin Eugene A
Shemyakin and Ovchinnikov Institute of Bioorganic Chemistry Russian Academy of Sciences, 16/10, ul. Miklukho-Maklaya, 117997 Moscow, Russia.
Gause Institute of New Antibiotics, 11 ul. Bol'shaya Pirogovskaya, 119021 Moscow, Russia.
Antibiotics (Basel). 2021 Feb 6;10(2):166. doi: 10.3390/antibiotics10020166.
High-cationic biologically active peptides of the thionins family were isolated from black cumin ( L.) seeds. According to their physicochemical characteristics, they were classified as representatives of the class I thionin subfamily. Novel peptides were called "Nigellothionins", so-called because of their source plant. Thionins are described as components of plant innate immunity to environmental stress factors. Nine nigellothionins were identified in the plant in different amounts. Complete amino acid sequences were determined for three of them, and a high degree of similarity was detected. Three nigellothionins were examined for antifungal properties against collection strains. The dominant peptide, NsW2, was also examined for activity against clinical isolates of fungi. Cytotoxic activity was determined for NsW2. Nigellothionins activity against all collection strains and clinical isolates varied from absence to a value comparable to amphotericin B, which can be explained by the presence of amino acid substitutions in their sequences. Cytotoxic activity in vitro for NsW2 was detected at sub-micromolar concentrations. This has allowed us to propose an alteration of the molecular mechanism of action at different concentrations. The results obtained suggest that nigellothionins are natural compounds that can be used as antimycotic and anti-proliferative agents.
从黑种草（L.）种子中分离出硫堇蛋白家族的高阳离子生物活性肽。根据其理化特性，它们被归类为I类硫堇蛋白亚家族的代表。新的肽被称为“黑种草硫堇蛋白”，因其来源植物而得名。硫堇蛋白被描述为植物对环境胁迫因子先天免疫的组成部分。在该植物中鉴定出九种不同含量的黑种草硫堇蛋白。确定了其中三种的完整氨基酸序列，并检测到高度相似性。检测了三种黑种草硫堇蛋白对收集菌株的抗真菌特性。还检测了主要肽NsW2对真菌临床分离株的活性。测定了NsW2的细胞毒性活性。黑种草硫堇蛋白对所有收集菌株和临床分离株的活性从无到与两性霉素B相当的值不等，这可以通过其序列中氨基酸取代的存在来解释。在亚微摩尔浓度下检测到NsW2的体外细胞毒性活性。这使我们能够提出在不同浓度下作用分子机制的改变。所得结果表明，黑种草硫堇蛋白是可作为抗真菌和抗增殖剂的天然化合物。
