Structure-activity relationships among monoterpene inhibitors of protein isoprenylation and cell proliferation.

摘要: Abstract The monoterpene d-limonene inhibits the post-translational isoprenylation of p21ras and other small G proteins, a mechanism that may contribute to its efficacy in chemoprevention therapy chemically induced rodent cancers. In present study, relative abilities 26 limonene-like monoterpenes inhibit protein cell proliferation were determined. Many found be more potent than limonene as inhibitors proliferation. potency limonene-derived was be: monohydroxyl = ester aldehyde > thiol acid diol epoxide triol unsubstituted. All inhibited did so selective manner, such 21–26 kDa proteins preferentially affected. Perillyl alcohol, one most terpenes, reduced 50% control level at concentration 1 mM, but had no effect on 67, 47 or 17 proteins. particular, farnesylation 40% by mM perillyl alcohol. At same concentration, alcohol completely human HT-29 colon carcinoma cells. structure-activity relationships observed among support role for proliferation, suggest many warrant further investigation antitumor agents.