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Studies on antitumor activity of acyclic retinoid e 5166 polyprenoic acid i. action characteristics on human cancer cells



Studies on antitumor activity of acyclic retinoid e 5166 polyprenoic acid i. action characteristics on human cancer cells



Acta Scholae Medicinalis Universitatis in Gifu 38(3): 498-509



Inhibitory effects and characteristics of synthetic retinoid E5166 (polyprenoic acid) on growth of HeLa S3 cells derived from human cervical carcinoma were investigated in vitro. When cells were cultured with E5166 or retinoic acid for seven days, the concentration of E5166 and retinoic acid required for 50% cell growth inhibition were 1.3 .times. 10-5 M and 2.7 .times. 10-6 M, respectively. A reduction in cell proliferation rate which became apparent after 48 hours of the treatment was time-dependent, concentration-dependent and reversible. By exposure to E5166, the cells were assumed a flattened appearance and inhibited to form multilayers and the saturation density was reduced. Furthermore, anchorage independent growth of cells were inhibited by E5166. The cell adhesiveness to substratum was enhanced similarly with E5166 and retinoic acid suggesting cell surface alterlations by both retinoids. Incorporation rates of [3H]-E5166 into HeLa S3 cells for 24 hours and for 50 hours were approximately 2.6% and 4.5% to total radioactivity added in the medium, respectively. These data indicate that E5166 taken up by HeLa S3 cells shows that growth inhibitory effects on the cells and its possible mechanisms are discussed.

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Accession: 007831016

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