In Vitro Cytotoxic Effects of Secondary Metabolites Present in <i>Sarcopoterium Spinosum</i> L.

• Main Authors: Jozef Hudec, Jan Mojzis, Marta Habanova, Jorge A. Saraiva, Pavel Hradil, Tibor Liptaj, Lubomir Kobida, Miroslav Haban, Maria Holovicova, Dominika Zvercova
• Format: Article
• Language: English
• Published: MDPI AG 2021-06-01
• Series: Applied Sciences
• Subjects: <i>Sarcopoterium spinosum</i> (L.); medicinal plants; cytotoxicity; inhibition; stachydrine; benzalkonium chloride
• Online Access: https://www.mdpi.com/2076-3417/11/11/5300

<i>Sarcopoterium spinosum</i> (L.) is a medicinal plant traditionally used for the treatment of various diseases including cancer in the Near- and Middle East. The fractions and constituents of the ethanol extract of <i>S. spinosum</i> were screened for in vitro cytotoxic activities on Jurkat (acute T-lymphoblastic leukemia), HeLa (cervical adenocarcinoma), MCF-7 (mammary gland adenocarcinoma), Caco-2 (human colorectal adenocarcinoma), and MDA-MB-231 (mammary gland adenocarcinoma) cell lines using the MTT (3-(dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay. The ethanol extract was subsequently re-extracted with ethyl acetate and in its sub-fraction obtained by column chromatography three compounds (stachydrine, benzalkonium chloride and rutine) were the first time identified by nuclear magnetic resonance (NMR) analyses. The most active subfraction showed cytotoxic activity against HeLa, MCF-7, and Caco-2 cell lines. The three compounds mentioned, as standards of high-performance liquid chromatography (HPLC) quality, were studied individually and in combination. Cytotoxic activity observed might be due to the presence of benzalkonium chloride and rutin. Benzalkonium chloride showed the strongest growth suppression effect against HeLa cells (IC₅₀ 8.10⁻⁷ M) and MCF-7 cells (IC₅₀ 5.10⁻⁶ M). The mixture of stachydrine and benzalkonium chloride allowed a synergistic cytotoxic effect against all tested cancer and normal cells to be obtained. Anti-cancer activity of the plant extract of <i>S. spinosum</i> remains under-investigated, so this research describes how the three major compounds identified in the ethyl acetate extract can exert a significant dose dependent in vitro cytotoxicity.