Cytotoxic Activity and G1 Cell Cycle Arrest of a Dienynone fromEchinacea pallida

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.

The Inhibitory Effect of Echinacea purpurea and Echinacea pallida on BT-549 and Natural Killer Cells

“…The results of the first three aims of this study are quite significant because they support an anti-cancer study that determined a ketopolyacetylene, pentadeca-(8Z,13Z)-dien-11-yn-Z-one, from the root of E pallida demonstrated anti-tumor activity against another breast cancer cell line, MCF-7. 11 The results also supports the results of experiments that indicated chicoric acid decreased the growth of MCF-7 at high dosages as well. 29 The cytotoxic effect of chicoric acid has been noted to reduce telomerase activity and induce apoptosis via DNA fragmentation in human colon cancer cells.…”

“…23 In addition, it could be due to the isobutyl amides, other active components of Echinacea, which are present in E purpurea in high concentrations. 11 Moreover, chicoric acid and the isobutyl amides could have been working synergistically, along with the other active components in the crude extracts of E purpurea, against the proliferation of BT-549 in the study. In addition, the water soluble extracts of E purpurea root and E purpurea leaf exhibited anti-tumor activity against BT-549 at a lower dosage than the crude extracts of E purpurea root and E purpurea leaf.…”

“…A more recent cancer study indicated that pentadeca-(8Z,13Z)-dien-11-yn-Z-one, a ketopolyacetylene derived from the root of E. pallida, exhibited anti-tumor activity on a breast cancer cell line (MCF-7). 11 In vitroand In vivo studies of Echinacea and NK cells have been conducted as well. An in vitro study indicated that water soluble extracts of Echinacea activated the cytotoxicity of NK cells.…”

Bauer ketones 23 and 24 from Echinacea paradoxa var. paradoxa inhibit lipopolysaccharide-induced nitric oxide, prostaglandin E2 and cytokines in RAW264.7 mouse macrophages

“…paradoxa were in agreement with the earlier results. Apart from its anti-inflammatory activity, Bauer ketone 24 (compound 2) from E. pallida has also been reported to inhibit the growth of human cancer cell lines possibly by arresting the cell cycle in the G1 phase and promoting apoptotic cell death (Chicca et al, 2010). Bauer ketone 24 (compound 2) is evidently permeable above 10 × 10 −6 cms −1 across the Caco-2 monolayer, suggesting potential oral bioavailability (Chicca et al, 2008).…”

Malaysian Medicinal Plants’ Potential for Breast Cancer Therapy

“…3. Inhibiting proliferation via the activation of caspase-3 and caspase-9, up-regulation of the ratio of bax/bcl-2 protein expression in Ardisia brevicaulis [61] Artocarpus obtusus [50,62] Ardisia brecaulis [63], Carica papaya [64] Catharanthus roseus [118][119], Costus speciosus [121][122], Cucuma zedoaria [65], Dysoxylum cauliforum [66], Goniosthalamus macrophyllus [137][138], Gynura procumbens [139], Lawsonia inermis [56,[146][147], Leea indica [148][149], Nepthelium lappaceum [56,156] Pandanus amarylfolius [41], Phyla nodiflora [67], Physalis minima [52,78], Rhodiola rosea [68], Vernonia amygdalina [65] and Schima wallichi [38]. 4.…”