Background: The ether lipid analogue 1-octadecy-2-methyl-rac-glycero-3
-phosphocholine (ET-18-OCH3) is known to have plasma membrane interact
ing antitumor activity. However, the mechanism and the mode of action
of its activity remain to be elucidated fully. Materials and Methods:
In this study, the proportion of the inhibitory effects resulting eith
er fiom direct cell kill or from cytostasis induced by (ET-18-OCH3) al
one or in combination with heat in BG-I human ovarian carcinoma cells
was quantitated. Results: The magnitude of both cell kill and cytostas
is in BG-I cells was dependent on the concentration of ET-18-OCH3 and
the duration of exposure. Cell kill, induced by exposure to 2 or. 8 mu
M ET-18-OCH3 for 1-14 days could be expressed as a simple exponential
function of exposure dose (concentration x time). As assayed by colon
y formation, cell survival after continuous exposure to the drug was s
ignificantly reduced from that measured when the drug was removed and
the cells were incubated for 14 days in drug-free medium: Conclusions:
We conclude that ET-18-OCH3 induces substantial cytostasis as well as
cell kill in BG-I cells and that this cytostasis is directly proporti
onal to the amount of cell kill induced These data are important in de
termining appropriate treatment regimens using ET-18-OCH3 either alone
or in combination with other anticancer agents.