High anticancer potency on tumor cells of dehydroabietylamine Schiff-base derivatives and a copper(II) complex

Five bioactive dehydroabietylamine Schiff-base derivatives (L-1-L-5) had been synthesized from Dehydroabietylamine (L-0), and the complex Cu(L-1)(2) had been obtained from the compound L-1 and copper(II) acetate. Their activities against Hela (cervix), MCF-7 (breast), A549 (lung), HepG2 (liver) and HUVEC (umbilical vein, normal cell) in vitro were investigated. The toxicity of L-1-L-5 and Cu(L-1)(2) was all lower than L-0. For MCF-7 cell, L-1, L-3, L-4, L-5 and Cu(L-1)(2) had higher antitumor activity than L. The smallest IC50 value was 2.58 AM of L-5. For A549 cell, the IC50 value of the compound L-4 was smaller than L, which indicated that the compound L-4 had higher anti-A549 activity than L. For HepG2 cell, the IC50 value of L-4 (0.24 mu M) and L-5 (0.14 mu M) were much smaller than L-0, which suggested L-4 and L-5 had higher anti-HepG2 activity. L-5 was 180 times more effective at inhibiting cultured HepG2 cells survival than normal cells, with average IC50 values of 0.14 and 25.56 AM, Furthermore, L, L-4 and L-5 contrasting with Doxorubicin had been measured with the ability to induce apoptosis. It turned out that L-4 and L-5 could induce more HepG2 cells apoptosis, which suggested they may be potential antitumor drugs. (C) 2018 Elsevier Masson SAS. All rights reserved.