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首页> 外文期刊>Medicinal chemistry >Synthesis, characterization, and molecular structure of a novel zinc (II) complex: assessment of impact of MDR1Pgp expression on its cytotoxic activity.
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Synthesis, characterization, and molecular structure of a novel zinc (II) complex: assessment of impact of MDR1Pgp expression on its cytotoxic activity.

机译：新型锌（II）配合物的合成，表征和分子结构：评估MDR1Pgp表达对其细胞毒活性的影响。

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摘要

Zinc(II)complex (3) {bis(3-ethoxy-2-hydroxy-benzylidene)-N,N'-bis(2,2-dimethyl-3-aminopropyl)ethylene diamine}-zinc(II); [(3-OEt-ENBDMPI)Zn(II)] was obtained in situ by a ligand exchange reaction involving zinc(II) acetylacetonate and the Schiff-base ligand obtained in situ. For assessing ability of 3 to act as a transport substrate of multidrug resistance (MDR1) P-glycoprotein (Pgp), its cytotoxic activity was evaluated in human epidermal carcinoma drug-sensitive KB 3-1 (Pgp-) and drug resistant KB 8-5 (Pgp+) cells. Compared with its cationic gallium(III) counterpart 4 showing cytotoxicity profiles consistent with its recognition as a Pgp substrate, the neutral zinc(II) complex 3 did not display cytotoxicity profiles (at pharmacologically relevant concentrations <10 microM) modified by expression of Pgp. Further, 3 was found be slightly more toxic against KB 8-5 cells compared to KB 3-1 cells at higher concentration. The neutral zinc (II) complex 3 was also found to be considerably less toxic against Pgp-lacking cells compared to its cationic gallium(III) counterpart 4. Additionally, the neutral zinc(II) complex 3 demonstrated considerably more toxicity against Pgp expressing KB 8-5 cells (> 10 microM) compared with its cationic counterpart 4 displaying minimal effect at highest concentration. The results suggest that differential cytotoxic activity of 3 and 4 in drug-resistant human epidermal carcinoma KB 8-5 (Pgp+) cells could result from variation in the overall charge of the molecules.
机译：锌（II）络合物（3）{双（3-乙氧基-2-羟基-亚苄基）-N，N′-双（2，2-二甲基-3-氨基丙基）乙二胺}-锌（II）; [（3-OEt-ENBDMPI）Zn（II）]是通过涉及乙酰丙酮锌（II）和就地获得的席夫碱配体的配体交换反应原位获得的。为了评估3充当多药耐药性（MDR1）P糖蛋白（Pgp）的转运底物的能力，在人表皮癌药物敏感KB 3-1（Pgp-）和耐药KB 8中评估了其细胞毒性活性。 5（Pgp +）个细胞。与它的阳离子镓（III）对应物4显示出与被识别为Pgp底物一致的细胞毒性谱相比，中性锌（II）配合物3没有显示出通过Pgp表达修饰的细胞毒性谱（在药理学相关浓度<10 microM时）。此外，发现在较高浓度下，与KB 3-1细胞相比，3对KB 8-5细胞的毒性稍强。还发现中性锌（II）配合物3对缺少Pgp的细胞的毒性比其阳离子镓（III）对应物4低得多。此外，中性锌（II）配合物3对表达KB的Pgp表现出明显更高的毒性与它的阳离子对应物4相比，8-5细胞（> 10 microM）在最高浓度下显示出最小的作用。结果表明，耐药的人表皮癌KB 8-5（Pgp +）细胞中3和4的不同细胞毒活性可能是由于分子总电荷的变化所致。

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