Silva I C, Polaquini C R, Regasini L O, Ferreira H, Pavan F R
Faculdade de Ciências Farmacêuticas, UNESP - Universidade Estadual Paulista, Araraquara, São Paulo 14800-903, Brazil; Departamento de Bioquímica e Microbiologia, Instituto de Biociências, Universidade Estadual Paulista, Rio Claro, Brazil.
Departamento de Química e Ciências Ambientais, Instituto de Biociências, Letras e Ciências Exatas, Universidade Estadual Paulista, São José do Rio Preto, Brazil.
Food Chem Toxicol. 2017 Jul;105:300-307. doi: 10.1016/j.fct.2017.04.033. Epub 2017 Apr 25.
Gallic acid and its derivatives are phenolic compounds widely used as food supplements in the form of capsules, liquid extracts, and ointments owing to their good antioxidant properties. Besides, these compounds are potent inhibitors of fungi, bacteria, and some viruses and possess strong antiproliferative and chemopreventive activities. However, gallic acid derivatives are also known to exert harmful effects like mutagenicity and cytotoxicity. The present study aimed to understand and explore the toxicological risks of these compounds. For this, a series of alkyl gallates with side chains varying from five to eight carbons (pentyl, hexyl, heptyl, and octyl gallates) were evaluated for their cytotoxic and pro-apoptotic potential. In addition, the genotoxic effects of alkyl gallates were measured in HepG2 cells using the single cell gel electrophoresis (SCGE)/comet assay and the cytokinesis-blocked micronucleus (CBMN) test. In both the tests, the substances did not induce any significant differences when compared to the control group. In addition, alkyl gallates exhibited a chemopreventive effect, thereby considerably reducing the mutagenicity caused by H2O2. In conclusion, our results suggest that alkyl gallates are non-genotoxic, non-mutagenic, and pro-apoptotic agents, which may serve as suitable and promising candidates for preventing chemically-induced chromosomal damage.
没食子酸及其衍生物是酚类化合物，由于其良好的抗氧化性能，它们以胶囊、液体提取物和软膏的形式被广泛用作食品补充剂。此外，这些化合物是真菌、细菌和一些病毒的有效抑制剂，并具有强大的抗增殖和化学预防活性。然而，没食子酸衍生物也已知会产生如致突变性和细胞毒性等有害影响。本研究旨在了解和探索这些化合物的毒理学风险。为此，评估了一系列侧链碳数从五到八的烷基没食子酸酯（戊基、己基、庚基和辛基没食子酸酯）的细胞毒性和促凋亡潜力。此外，使用单细胞凝胶电泳（SCGE）/彗星试验和胞质分裂阻滞微核（CBMN）试验在HepG2细胞中测量了烷基没食子酸酯的遗传毒性作用。在这两个试验中，与对照组相比，这些物质均未诱导出任何显著差异。此外，烷基没食子酸酯表现出化学预防作用，从而大大降低了由H2O2引起的致突变性。总之，我们的结果表明，烷基没食子酸酯是非遗传毒性、非致突变性和促凋亡剂，它们可能是预防化学诱导的染色体损伤的合适且有前景的候选物。
