Abstract
In the present study, a further investigation of the cytotoxic activity of an acetylenic constituent of Echinacea pallida roots, namely, pentadeca-(8 Z,13 Z)-dien-11-yn-2-one, was performed, revealing a concentration-dependent cytotoxicity on several human cancer cell lines, including leukemia (Jurkat and HL-60), breast carcinoma (MCF-7), and melanoma (MeWo) cells. As part of its mechanism of action, the ability of this constituent to arrest the cell cycle in the G1 phase was demonstrated on HL-60 cells. Furthermore, a stability test of the target compound over 72 h was carried out, indicating that the cytotoxic activity can be attributed mainly to the genuine, not oxidized, molecule.
Highlights
Used Echinacea species (E. pallida, E. angustifolia, and E. purpurea, family Asteraceae) are among the most widely used medicinal plants, mainly for their immunomodulatory, anti-inflammatory and antioxidant properties [1, 2]
A bioassay-guided fractionation study has indicated that polyacetylenes and polyenes, which are present in high concentration in E. pallida lipophilic root extracts [6,7,8] but not detected in those from E. purpurea and E. angustifolia [9], are responsible for this activity [10]
Note: Data are from three experiments carried out in triplicate; a 5-Fluorouracil was the positive control for MCF-7 and HL-60; cisplatin was the positive control for Jurkat and MeWo
Summary
Used Echinacea species (E. pallida, E. angustifolia, and E. purpurea, family Asteraceae) are among the most widely used medicinal plants, mainly for their immunomodulatory, anti-inflammatory and antioxidant properties [1, 2]. N-Hexane extracts from the roots of the three above-mentioned Echinacea species have demonstrated in vitro anticancer activity on human cancer cell lines and E. pallida extracts have shown the greatest potency [5]. Pentadeca-(8Z,13Z)-dien-11-yn-2-one (l" Fig. 1) has been revealed to be a potent cytotoxic compound that is able to induce apoptotic cell death at low micromolar concentrations in human cancer cell lines (pancreatic MIA PaCa-2 and colonic COLO320) [10].
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