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Steroidal Glycosides with Antiproliferative Activities from Digitalis trojana
Author(s) -
Kirmizibekmez Hasan,
Masullo Milena,
Festa Michela,
Capasso Anna,
Piacente Sonia
Publication year - 2014
Publication title -
phytotherapy research
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.019
H-Index - 129
eISSN - 1099-1573
pISSN - 0951-418X
DOI - 10.1002/ptr.5012
Subject(s) - glycoside , propidium iodide , apoptosis , phenylethanoid , cell cycle , phytochemical , cell culture , chemistry , flow cytometry , cell growth , cytotoxicity , biochemistry , pharmacology , biology , stereochemistry , programmed cell death , microbiology and biotechnology , in vitro , genetics
The phytochemical investigation of Digitalis trojana led to the isolation of two cardiac glycosides (1, 2), one pregnane glycoside (3), three furostanol type saponins (4–6), along with three cleroindicins (7–9), four phenylethanoid glycosides (10–13), two flavonoids (14, 15) and two phenolic acid derivatives (16, 17). The structure elucidation of the isolates was carried out by NMR experiments as well as ESI‐MS. The cytotoxic activity of compounds 1–13 against a small panel of cancer cell lines, namely MCF‐7, T98G, HT‐29, PC‐3, A375 and SH‐SY5Y, was investigated. Compounds 1–6 showed antiproliferative activity against human breast MCF‐7 and colon HT‐29 cancer cell lines with IC 50 values ranging from 8.3 to 50 μM. In order to understand the mechanism involved in the cell death, the active compounds were tested as pro‐apoptotic agents using propidium iodide staining by flow cytometry method. No significant increase was observed in the apoptosis of the MCF‐7 and HT‐29 cancer cells. Moreover, the effects of the active compounds on cell proliferation were assessed on the same cancer cell lines by cell cycle analysis of DNA content using flow cytometry. No significative changes were observed in the cell cycle of MCF‐7, while significant changes in G 2 /M cell cycle phase of HT‐29 cells were observed after treatment with digitalin (1), cariensoside (3) and 22‐ O ‐methylparvispinoside B (6) at 10 μM. Copyright © 2013 John Wiley & Sons, Ltd.