Highly cytotoxic DNA-interacting copper(ii) coordination compounds

Metallomics ◽  
2014 ◽  
Vol 6 (10) ◽  
pp. 1853-1868 ◽  
Author(s):  
Rosa F. Brissos ◽  
Ester Torrents ◽  
Francyelli Mariana dos Santos Mello ◽  
Wanessa Carvalho Pires ◽  
Elisângela de Paula Silveira-Lacerda ◽  
...  

Copper complexes from Schiff-base ligands show high cytotoxicity against diverse cancer cell lines, with IC50 values down to 0.23 μM.

2014 ◽  
Vol 2014 ◽  
pp. 1-12 ◽  
Author(s):  
Zahidah Ayob ◽  
Siti Pauliena Mohd Bohari ◽  
Azman Abd Samad ◽  
Shajarahtunnur Jamil

Justicia gendarussamethanolic leaf extracts from five different locations in the Southern region of Peninsular Malaysia and two flavonoids, kaempferol and naringenin, were tested for cytotoxic activity. Kaempferol and naringenin were two flavonoids detected in leaf extracts using gas chromatography-flame ionization detection (GC-FID). The results indicated that highest concentrations of kaempferol and naringenin were detected in leaves extracted from Mersing with 1591.80 mg/kg and 444.35 mg/kg, respectively. Positive correlations were observed between kaempferol and naringenin concentrations in all leaf extracts analysed with the Pearson method. The effects of kaempferol and naringenin from leaf extracts were examined on breast cancer cell lines (MDA-MB-231 and MDA-MB-468) using MTT assay. Leaf extract from Mersing showed high cytotoxicity against MDA-MB-468 and MDA-MB-231 with IC50values of 23 μg/mL and 40 μg/mL, respectively, compared to other leaf extracts. Kaempferol possessed high cytotoxicity against MDA-MB-468 and MDA-MB-231 with IC50values of 23 μg/mL and 34 μg/mL, respectively. These findings suggest that the presence of kaempferol in Mersing leaf extract contributed to high cytotoxicity of both MDA-MB-231 and MDA-MB-468 cancer cell lines.


2016 ◽  
Vol 45 (29) ◽  
pp. 11849-11863 ◽  
Author(s):  
Upendarrao Golla ◽  
Amit Adhikary ◽  
Amit Kumar Mondal ◽  
Raghuvir Singh Tomar ◽  
Sanjit Konar

Three double stranded helicates and one linear chain compound have been synthesized following similar synthetic strategy with change in the coordination of the ligands. Magnetic studies, nuclease activity and cytotoxicity on mammalian cancer cell lines have been investigated.


2021 ◽  
Author(s):  
Saima Najm ◽  
Humaira Naureen ◽  
Fareeha Anwar ◽  
Muhammad Mubbashir Khan ◽  
Rabia Ali

Abstract Background and objectives: Breast cancer presents high morbidity among women with various treatment challenges. This study aims to evaluate the repurposed lamotrigine schiff base metal (LTG-SB-M) coordinates against in-vitro MCF-7 breast cancer cell lines and in-vivo N-methylnitrosourea (NMU)-persuaded toxicity of rats’ mammary gland. Method: In-silico computational analysis and in vitro cytotoxic studies on MCF-7 breast cancer cell lines was executed to build up the assumptions. In-vivo NMU-induced anticancer potential was assessed in forty Wistar rats; assigned into five groups of 8 rats each. Group I served as normal control and received normal saline, Group II received NMU (50 mg/kg), Group III received tamoxifen, whereas; Group IV and V received LTG-SB-M derivative (LAC3, LBC3) at dose of 100 mg/kg body weight, for 15 consecutive days. Intraperitoneal injection of NMU (single dose) was given at the age of 5, 9 and 13 weeks to the rats with the three week interval. For all experimental animals; biochemical markers were assessed. DNA strand breakage alongside the hormonal profile of estrogen and progesterone was also estimated. Results: All tested compounds present significant activity against MCF-7 cell lines in vitro and NMU-induced mammary tumor in vivo. The in vivo results of tested compounds present a significant decrease in weight of organ; with reinstated renal and hepatic enzymes. Histological analysis revealed strong countenance of proteins, estrogen, and progesterone in NMU-treated rats. Conclusion: These results suggest that LTG-SB-M complex can be used as better anticancer agent against breast cancer.


2011 ◽  
Vol 21 (6) ◽  
pp. 1802-1806 ◽  
Author(s):  
Sommai Patitungkho ◽  
Shreelekha Adsule ◽  
Prasad Dandawate ◽  
Subhash Padhye ◽  
Aamir Ahmad ◽  
...  

2019 ◽  
Vol 32 (2) ◽  
pp. 441-450
Author(s):  
Ravi K. Kottalanka ◽  
Eswar Pagadala ◽  
Shiva K. Loke ◽  
S. Rex Jeya Rajkumar ◽  
Venkatesan Srinivasadesikan ◽  
...  

Titanium(IV)-complex of chemical composition [{(NNO)2Ti}3O3] (2) bearing bidentate heteroditopic Schiff base [(C5H4OH)-N=CH-C4H3-NH] (L1) ligand in titanium coordination sphere was reported and its biological significance was evaluated. The in vitro cytotoxicity of L1 and 2 were evaluated by using MTT assay on cancer cell lines (MCF-7 & A549) and observed significant cytotoxicity. Further, the LDH and NO assay studies on both L1 and 2 on cancer cell lines revealed that the enhanced cytotoxicity compared to standard anticancer drug i.e. cisplatin. The DNA binding studies of tested compounds with Ct-DNA molecule by using UV-visible and fluorescence spectra and molecular docking studies revealed that moderate to good binding interactions with test molecules. Thus, the present work contributes and implies the biological significance of Ti-complex (2) and the correlation between the structure and the biological activities of such Ti-complexes supported by Schiff base systems opens up opportunities for further exploitation of similar biologically active titanium systems.


Metallomics ◽  
2021 ◽  
Vol 13 (4) ◽  
Author(s):  
Bo Chu ◽  
Xiyu Mo ◽  
Zilu Chen ◽  
Mingling Zhang ◽  
Yuning Liang ◽  
...  

Abstract Our previously reported copper-based complexes of tropolone show nice antitumor effects, but with high cytotoxicity to normal cells, which is presumably caused by copper ions. Here, we managed to achieve this challenge by using other 3D metals to replace copper ions. We thus prepared four mononuclear 3D metal complexes [M(phen)L2] (M = Mn, Co, Ni, and Zn for 1–4, respectively). Complexes 1 and 4 show selectivity on different cancer cell lines with much lower cytotoxicity to normal cells than cisplatin. The anticancer effects for complexes 2 and 3 on the tested cancer cell lines are very poor. It revealed a tuning effect of different metal ions on the anticancer activities with those for Mn(II) and Zn(II) being much higher than those for Co(II) and Ni(II) in this system. Among them, complex 1 presents a best anticancer effect on HeLa cells comparable to cisplatin. It overcame the afore-mentioned shortage of high cytotoxicity to normal cells for the reported Cu(II) complexes. It revealed from the mechanistic studies that complex 1 mainly induces apoptosis through the mitochondrial pathway by increasing intracellular reactive oxygen species, releasing Ca2+, and activating Caspase 9 and proapoptotic gene Bax.


2006 ◽  
Vol 175 (4S) ◽  
pp. 258-258
Author(s):  
Ruth Schwaninger ◽  
Cyrill A. Rentsch ◽  
Antoinette Wetterwald ◽  
Irena Klima ◽  
Gabri Van der Pluijm ◽  
...  

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