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脱氢枞胺席夫碱衍生物及其铜(II)配合物对肿瘤细胞具有高抗癌活性。

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

作者信息

Zhao Fengyi, Wang Weifan, Lu Wen, Xu Li, Yang Shilong, Cai Xu-Min, Zhou Mengyi, Lei Meng, Ma Mengtao, Xu Hai-Jun, Cao Fuliang

机构信息

College of Forestry, Nanjing Forestry University, Nanjing, 210037, PR China; Co-Innovation Center for Sustainable Forestry in Southern China, Nanjing Forestry University, Nanjing, PR China.

College of Chemical Engineering, Nanjing Forestry University, Nanjing, 210037, PR China.

出版信息

Eur J Med Chem. 2018 Feb 25;146:451-459. doi: 10.1016/j.ejmech.2018.01.041. Epub 2018 Feb 4.

Abstract

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

摘要

已由脱氢枞胺(L)合成了五种具有生物活性的脱氢枞胺席夫碱衍生物(L - L),并由化合物L与乙酸铜(II)制得配合物Cu(L)。研究了它们对Hela(宫颈)、MCF - 7(乳腺)、A549(肺)、HepG2(肝脏)和HUVEC(脐静脉,正常细胞)的体外活性。L - L和Cu(L)的毒性均低于L。对于MCF - 7细胞,L、L、L、L和Cu(L)的抗肿瘤活性均高于L。L的最小IC值为2.58μM。对于A549细胞,化合物L的IC值小于L,这表明化合物L对A549的活性高于L。对于HepG2细胞,L(0.24μM)和L(0.14μM)的IC值远小于L,这表明L和L对HepG2具有更高的活性。L抑制培养的HepG2细胞存活的效果比正常细胞高180倍,平均IC值分别为0.14和25.56μM。此外,已测定了L、L和L与阿霉素相比诱导细胞凋亡的能力。结果表明,L和L可诱导更多HepG2细胞凋亡,这表明它们可能是潜在的抗肿瘤药物。

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