Núcleo de Bioensaios, Biossíntese e Ecofisiologia de Produtos Naturais (NuBBE), Departamento de Química Orgânica, Instituto de Química, Universidade Estadual de São Paulo, Araraquara 14800-900, Brazil.
Marine Biodiscovery Centre, Department of Chemistry, University of Aberdeen, Aberdeen AB24 3UE, Scotland, UK.
Molecules. 2022 Jul 22;27(15):4695. doi: 10.3390/molecules27154695.
This work evaluated the metabolic profiling of species with antitumor potential. In addition, we described the antigenotoxicity of polyphenols isolated from and a proteomic approach using HepG2 cells after treatment with these metabolites. The in vitro cytotoxic activity against HepG2, HT-29 and T98G cancer cell lines was investigated. The assessment of genotoxic damage was carried out through the comet assay. The ethanolic extract from seeds was subjected to bioassay-guided fractionation and the most active fractions were characterized. One bioactive fraction with high cytotoxicity against HT-29 human colon cancer cells (IC = 4.0 µg mL) was found, and it was characterized as a mixture of -hydroxybenzoic acid and 4-vinyl-phenol. The fruit peel (IC = 18.6 µg mL) and seed (IC = 15.2 µg mL) extracts had cytotoxic activity against the cell line T98G, and its chemical composition showed a variety of phenolic acids. The chemical composition of this species indicated a wide variety of aromatic acids, flavonoids, tannins, and carotenoids. The high concentration (ranging from 5% to 30%) of these polyphenols in the bioactive extract may be responsible for the antitumor potential. Regarding the proteomic approach, we detected proteins directly related to the elimination of ROS, DNA repair, expression of tumor proteins, and apoptosis.
这项工作评估了具有抗肿瘤潜力的 物种的代谢特征。此外，我们还描述了从 中分离出的多酚的抗原毒性，以及使用 HepG2 细胞在这些代谢物处理后的蛋白质组学方法。研究了对 HepG2、HT-29 和 T98G 癌细胞系的体外细胞毒性活性。通过彗星试验评估遗传毒性损伤。对 种子的乙醇提取物进行了基于生物测定的分段，对最活跃的片段进行了表征。发现了一种对人结肠癌细胞 HT-29 具有高细胞毒性的生物活性部分（IC = 4.0 µg mL），其特征为 -羟基苯甲酸和 4-乙烯基苯酚的混合物。 果皮（IC = 18.6 µg mL）和 种子（IC = 15.2 µg mL）提取物对 T98G 细胞系具有细胞毒性活性，其化学成分显示出多种酚酸。该物种的化学成分表明存在多种芳香酸、类黄酮、单宁和类胡萝卜素。生物活性提取物中这些多酚的高浓度（5%至 30%）可能是其抗肿瘤潜力的原因。关于蛋白质组学方法，我们检测到与 ROS 清除、DNA 修复、肿瘤蛋白表达和细胞凋亡直接相关的蛋白质。
