Teneva Ivanka, Batsalova Tsvetelina, Moten Dzhemal, Petkova Zhana, Teneva Olga, Angelova-Romova Maria, Antova Ginka, Dzhambazov Balik
Department of Botany and Biological Education, Faculty of Biology, Paisii Hilendarski University of Plovdiv, 24 Tsar Assen Str., 4000 Plovdiv, Bulgaria.
Department of Developmental Biology, Faculty of Biology, Paisii Hilendarski University of Plovdiv, 24 Tsar Assen Str., 4000 Plovdiv, Bulgaria.
Int J Mol Sci. 2025 May 26;26(11):5086. doi: 10.3390/ijms26115086.
Cyanobacterial extracts offer significant potential for the development of new natural antioxidants and biologically active compounds with applications in various industries. Data on the genus are limited; therefore, the aim of the present study was to investigate the anticancer, antioxidant and anti-inflammatory activity of extracts prepared from strains of this genus. Cytotoxicity and anticancer activity were evaluated by in vitro tests with four cell lines using the MTT assay. The assessment of antioxidant activity was performed by the DPPH and ABTS methods in combination with the calculation of the total phenolic content. Anti-inflammatory activity was investigated using the LPS-stimulated macrophage model (RAW264.7) and subsequent measurement of the levels of secreted cytokines IL-6 and TNF-α. The lipid content and fatty acid composition of the non-polar extracts were determined by gas chromatography (GC). To elucidate the mechanism of cytotoxicity/anticancer action of the non-polar extracts, the effects of stearidonic acid, which was detected in four of the studied cyanobacterial strains, were additionally tested on the same cell lines. A molecular docking analysis was performed simulating the interaction between stearidonic acid and its target molecules and receptors (ALOX5, COX-2, NF-kB and PPAR-γ). In all cancer cell lines (but not in the normal one), dose-dependent cytotoxic effects were observed after exposure to different concentrations of non-polar extracts. The most pronounced inhibitory effect was observed on the HT-29 cell line, with an IC value of 106.27 µg/mL. A dose-dependent antioxidant effect was established for all tested extracts, measured by both DPPH and ABTS methods. All non-polar extracts reduced the production of pro-inflammatory cytokines IL-6 and TNF-α in LPS-stimulated macrophages RAW264.7, and the effects were dose-dependent. Analysis of the fatty acid composition revealed 26 different fatty acids. Our conclusion is that the strains exhibit anticancer, antioxidant, and anti-inflammatory activity and could be a promising source for the production of natural products.
蓝藻提取物在开发新型天然抗氧化剂和生物活性化合物方面具有巨大潜力,这些化合物可应用于各个行业。关于该属的数据有限;因此,本研究的目的是调查从该属菌株制备的提取物的抗癌、抗氧化和抗炎活性。通过使用MTT法对四种细胞系进行体外试验来评估细胞毒性和抗癌活性。通过DPPH和ABTS方法结合总酚含量的计算来评估抗氧化活性。使用LPS刺激的巨噬细胞模型(RAW264.7)并随后测量分泌的细胞因子IL-6和TNF-α的水平来研究抗炎活性。通过气相色谱(GC)测定非极性提取物的脂质含量和脂肪酸组成。为了阐明非极性提取物的细胞毒性/抗癌作用机制,还在相同的细胞系上测试了在四种研究的蓝藻菌株中检测到的硬脂酸的作用。进行了分子对接分析,模拟硬脂酸与其靶分子和受体(ALOX5、COX-2、NF-κB和PPAR-γ)之间的相互作用。在所有癌细胞系中(但在正常细胞系中未观察到),暴露于不同浓度的非极性提取物后观察到剂量依赖性细胞毒性作用。在HT-29细胞系上观察到最明显的抑制作用,IC值为106.27μg/mL。通过DPPH和ABTS方法测定,所有测试提取物均具有剂量依赖性抗氧化作用。所有非极性提取物均降低了LPS刺激的巨噬细胞RAW264.7中促炎细胞因子IL-6和TNF-α的产生,且作用呈剂量依赖性。脂肪酸组成分析揭示了26种不同的脂肪酸。我们的结论是,该属菌株具有抗癌、抗氧化和抗炎活性,可能是生产天然产物的有前途的来源。