Issue 41, 2019

Biological evaluation of optically pure chiral binuclear copper(ii) complexes based on a rosin derivative as highly potential anticancer agents

Abstract

Two optically pure chiral binuclear copper(II) complexes [Cu2(μ-Cl)2L2]·CH2Cl2 (1) and Cu2L4 (2) based on the natural product rosin derivative N-(5-dehydroabietyl-1,3,4-thiadiazole)-2-substituted pyridinecarboxamide (HL) were prepared, fully characterized and their biological activities were evaluated. The circular dichroism (CD), fluorescence spectroscopy, and DNA melting studies indicate that 1 and 2 interact with calf thymus DNA (CT DNA) via intercalation. It can be concluded that 1 and 2 have a strong affinity to bovine serum albumin (BSA) based on the fluorescence and CD spectral evidence. The MTT assay illustrates that the selective cytotoxic activity of 1 is better than that of HL, 2, cisplatin and oxaliplatin. The exposure of 1 to MCF-7 cells resulted in cell cycle arrest in the G1 phase, apoptosis, mitochondrial dysfunction and an elevated ROS level. The western blot analysis results indicate that 1 might induce apoptosis through intrinsic and extrinsic pathways, autophagy and DNA damage in MCF-7 cells. Furthermore, the down-regulated VEGFR2, MMP-2 and MMP-9 expression levels indicate that 1 should have the ability to resist metastasis and angiogenesis. Thus, based on the above described results 1 has high potential value for anticancer applications.

Graphical abstract: Biological evaluation of optically pure chiral binuclear copper(ii) complexes based on a rosin derivative as highly potential anticancer agents

Supplementary files

Article information

Article type
Paper
Submitted
10 Maijs 2019
Accepted
20 Aug. 2019
First published
21 Aug. 2019

Dalton Trans., 2019,48, 15646-15656

Biological evaluation of optically pure chiral binuclear copper(II) complexes based on a rosin derivative as highly potential anticancer agents

B. Fei, S. Tu, Z. Wei, P. Wang, J. Long, C. Qiao and Z. Chen, Dalton Trans., 2019, 48, 15646 DOI: 10.1039/C9DT01942A

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