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

Five bioactive dehydroabietylamine Schiff-base derivatives (L¹-L⁵) had been synthesized from Dehydroabietylamine (L⁰), and the complex Cu(L¹)₂ had been obtained from the compound L¹ 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 L¹-L⁵ and Cu(L¹)₂ was all lower than L⁰. For MCF-7 cell, L¹, L³, L⁴, L⁵ and Cu(L¹)₂ had higher antitumor activity than L⁰. The smallest IC₅₀ value was 2.58 μM of L⁵. For A549 cell, the IC₅₀ value of the compound L⁴ was smaller than L⁰, which indicated that the compound L⁴ had higher anti-A549 activity than L⁰. For HepG2 cell, the IC₅₀ value of L⁴(0.24 μM) and L⁵ (0.14 μM) were much smaller than L⁰, which suggested L⁴ and L⁵ had higher anti-HepG2 activity. L⁵ was 180 times more effective at inhibiting cultured HepG2 cells survival than normal cells, with average IC₅₀ values of 0.14 and 25.56 μM. Furthermore, L⁰, L⁴ and L⁵ contrasting with Doxorubicin had been measured with the ability to induce apoptosis. It turned out that L⁴ and L⁵ could induce more HepG2 cells apoptosis, which suggested they may be potential antitumor drugs.