Nickel and zinc complexes of testosterone N4-substituted thiosemicarbazone: Selective cytotoxicity towards human colorectal carcinoma cell line HCT 116 and their cell death mechanisms.,Journal of Inorganic Biochemistry

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Nickel and zinc complexes of testosterone N4-substituted thiosemicarbazone: Selective cytotoxicity towards human colorectal carcinoma cell line HCT 116 and their cell death mechanisms.
Journal of Inorganic Biochemistry ( IF 3.8 ) Pub Date : 2020-05-04 , DOI: 10.1016/j.jinorgbio.2020.111097
Mok Piew Heng ₁ , Kae Shin Sim ₁ , Kong Wai Tan ₂

Affiliation

Two new Schiff base ligands (TE and TF) were prepared from conjugation of testosterone with 4-(4-ethylphenyl)-3-thiosemicarbazide and 4-(4-fluorophenyl)-3-thiosemicarbazide, respectively. Their nickel (NE and NF) and zinc (ZE and ZF) complexes were reported. X-ray crystallography revealed a distorted square planar geometry was adopted by NE. The compounds demonstrated excellent selectivity towards the colorectal carcinoma cell line HCT 116 despite their weak preferences towards the prostate cancer cell lines (PC-3 and LNCaP). Against HCT 116, all these compounds were able to arrest cell cycle at G0/G1 phase and induce apoptosis via mitochondria-dependent (TE, NE, and TF) and extrinsic apoptotic pathway (ZE, NF, and ZF). Moreover, only ZE was able to act as topoisomease I poison and halt its enzymatic reactions although all compounds presented excellent affinity towards DNA.

中文翻译：

睾丸素N4取代的硫代半脲的镍和锌复合物：对人大肠癌细胞HCT 116的选择性细胞毒性及其细胞死亡机制。

分别由睾酮与4-（4-乙基苯基）-3-硫代氨基脲和4-（4-氟苯基）-3-硫代氨基脲共轭制备了两个新的席夫碱配体（TE和TF）。据报道它们的镍（NE和NF）和锌（ZE和ZF）配合物。X射线晶体学显示NE采用了扭曲的正方形平面几何形状。尽管这些化合物对前列腺癌细胞系（PC-3和LNCaP）的偏爱性弱，但它们对结直肠癌细胞系HCT 116表现出优异的选择性。针对HCT 116，所有这些化合物均能够在G0 / G1期停滞细胞周期，并通过线粒体依赖性（TE，NE和TF）和外在凋亡途径（ZE，NF和ZF）诱导凋亡。此外，

更新日期：2020-05-04

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