Metabolomics assisted fingerprint of Hypericum perforatum chemotypes and assessment of their cytotoxic activity

• DOI: 10.1016/j.fct.2018.02.057
• Publication Date: 2018-02-27T18:43:11Z
• Authors: Eirini Sarrou; Lefki-Pavlina Gia...; Domenico Masuero; Daniele Perenzoni; Ioannis S. Viziri...; Maria Irakli; Paschalina Chatzo...; Stefan Martens
• Keywords: 0301 basic medicine; 0303 health sciences; Plants, Medicinal; Cell Survival; Plant Extracts; Cytotoxicity; Plant Components, Aerial; Settore BIO/15 - BIOLOGIA FARMACEUTICA; 630; 3. Good health; Anthocyanins; 03 medical and health sciences; Tandem Mass Spectrometry; 615; Hypericum perforatum; Humans; Metabolomics; 14. Life underwater; Phenolics; Caco-2 Cells; Caco-2 cells; Chromatography, High Pressure Liquid; Hypericum

Hypericum perforatum is known as an important medicinal plant, used for the treatment of several diseases, while its pharmacological properties are attributed to the presence of a wide range of secondary metabolites. Due to the great chemotypic variability of Hypericum species in the nature, and the demand for standardized herbal products, a detailed phytochemical investigation was carried out on different parts (herba, leaf, flowers) from wild collected and cultivated populations, using advanced chromatographic tools. Liquid Chromatographic analysis (LC-MS/MS MRM) revealed significant variability in the secondary metabolites content of the examined methanolic extracts. The most common derivatives belong to 9 groups i.e. benzoic acids, phenylpropanoids, coumarins, flavones, flavonols, flavan-3-ols, anthocyanins, phloroglucinols and naphtodianthrones. The main polyphenolic compounds were catechin, epicatechin, quercetin, quercetin 3-O-rhamnoside, quercetin 3-O-glucoside, neochlorogenic acid, proanthocyanidins (A and B series) and cyanidin-3-O-glucoside. In addition, the content of the characteristic compounds hypericin and hyperforin in herba crude extracts ranged between 0.5 and 1.7 mg/g and 0.6-3.3 mg/g respectively. The cytotoxic activity of the crude extracts was assessed at concentrations ranged between 0.01 and 100 μg/mL, on Caco-2 intestinal cancer cell cultures, and a cytotoxic behavior was shown only at the highest concentration of 100 μg/mL.