Department of Genetics, Faculty of Natural Sciences, Comenius University, Mlynská dolina B1, Ilkovičova 6, 842 15 Bratislava, Slovakia.
Cancer Research Institute, Biomedical Research Center, SAS, Dúbravská cesta 9, 845 05 Bratislava, Slovakia.
Molecules. 2017 Jan 21;22(1):167. doi: 10.3390/molecules22010167.
Hyperforin (HF), a substance that accumulates in the leaves and flowers of L. (St. John's wort), consists of a phloroglucinol skeleton with lipophilic isoprene chains. HF exhibits several medicinal properties and is mainly used as an antidepressant. So far, the antigenotoxicity of HF has not been investigated at the level of primary genetic damage, gene mutations, and chromosome aberrations, simultaneously. The present work is designed to investigate the potential antigenotoxic effects of HF using three different experimental test systems. The antigenotoxic effect of HF leading to the decrease of primary/transient promutagenic genetic changes was detected by the alkaline comet assay on human lymphocytes. The HF antimutagenic effect leading to the reduction of gene mutations was assessed using the Ames test on the standard (TA97, TA98, and TA100) bacterial strains, and the anticlastogenic effect of HF leading to the reduction of chromosome aberrations was evaluated by the in vitro mammalian chromosome aberration test on the human tumor cell line HepG2 and the non-carcinogenic cell line VH10. Our findings provided evidence that HF showed antigenotoxic effects towards oxidative mutagen zeocin in the comet assay and diagnostic mutagen (4-nitroquinoline-1-oxide) in the Ames test. Moreover, HF exhibited an anticlastogenic effect towards benzo(a)pyrene and cisplatin in the chromosome aberration test.
金丝桃素（HF）是贯叶连翘叶和花中的一种物质，由具有亲脂性异戊二烯链的间苯三酚骨架组成。HF 具有多种药用特性，主要用作抗抑郁药。到目前为止，尚未同时在初级遗传损伤、基因突变和染色体畸变水平上研究 HF 的抗原毒性。本工作旨在使用三种不同的实验测试系统研究 HF 的潜在抗原毒性作用。通过人淋巴细胞碱性彗星试验检测 HF 导致原发性/瞬时诱变遗传变化减少的抗原毒性作用。使用标准（TA97、TA98 和 TA100）细菌菌株的 Ames 试验评估 HF 的抗突变作用，导致基因突变减少，以及在人肿瘤细胞系 HepG2 和非致癌细胞系 VH10 上进行体外哺乳动物染色体畸变试验评估 HF 的抗断裂作用，导致染色体畸变减少。我们的研究结果提供了证据表明，HF 在彗星试验中对氧化诱变剂 zeocin 和 Ames 试验中的诊断诱变剂（4-硝基喹啉 1-氧化物）表现出抗原毒性作用。此外，HF 在染色体畸变试验中对苯并（a）芘和顺铂表现出抗断裂作用。
