Abstract
Hyperforin (HF), a substance that accumulates in the leaves and flowers of Hypericum perforatum 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 Salmonella typhimurium (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.
Highlights
In recent years, the interest in herbal remedies as preventive and therapeutical medicines has been increasing
Since it has been demonstrated that HF exhibits antioxidant properties [17], it was a high probability that it could exhibit antigenotoxic activities
To the best of our knowledge, this was the first time the potential antigenotoxicity of HF was examined at three different levels simultaneously; primary/promutagenic DNA lesions, gene mutations, and chromosome aberrations
Summary
The interest in herbal remedies as preventive and therapeutical medicines has been increasing. Some studies have indicated the importance of natural products with potent antigenotoxic activities [1,2,3]. One of the most popular medicinal herbs is the perennial herb Hypericum perforatum (Hypericaceae), known as St. John’s wort [4]. H. perforatum contains numerous biologically active components, including naphtodianthrone derivatives (e.g., hypericin), phloroglucinol derivatives (e.g., hyperforin; HF), flavonoids, procyanidines, tannins, essential oils, phenylpropanes, xanthones, and other hydrosoluble compounds [5]. H. perforatum has been used for the treatment of premenstrual syndrome, burns, bruises, eczema, dyspepsia and gastric ulcers, biliary disorders, swellings, Molecules 2017, 22, 167; doi:10.3390/molecules22010167 www.mdpi.com/journal/molecules
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