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Anticancer activity and possible mode of action of 4‐ O ‐podophyllotoxinyl 12‐hydroxyl‐octadec‐ Z ‐9‐enoate
Author(s) -
Ma Guoyi,
Khan Shabana I.,
Mustafa Jamal,
Walker Larry A.,
Khan Ikhlas A.
Publication year - 2005
Publication title -
lipids
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.601
H-Index - 120
eISSN - 1558-9307
pISSN - 0024-4201
DOI - 10.1007/s11745-005-1386-0
Subject(s) - podophyllotoxin , etoposide , chemistry , in vitro , apoptosis , mode of action , flow cytometry , topoisomerase , cell cycle , cell culture , stereochemistry , pharmacology , biochemistry , microbiology and biotechnology , biology , chemotherapy , genetics
4‐ O ‐Podophyllotoxinyl 12‐hydroxyl‐octadec‐ Z ‐9‐enoate (PHEFE) is a structurally novel FA analog of podophyllotoxin. In the present study, in vitro effects of PHEFE on a panel of 60 human tumor cell lines and its potential modes of anticancer action were investigated. FHEFE exhibited strong growth‐inhibitory action in a number of solid tumor cells in vitro . It did not inhibit tubulin polymerization as podophyllotoxin does; rather, it inhibited the catalytic activity of topoisomerase II. Flow cytometry and staining assay with 4,6‐diamidine‐2‐phenylindole dihydrochloride showed that PHEFE blocked the cell cycle at the G 2 /M phase and induced apoptosis in HL‐60 cells. These analyses suggest that PHEFE has promising anticancer characteristics that differ from podophyllotoxin and etoposide.