Effect of ligand substitution in pyrazolone based binary and ternary Cu(II) complexes on DNA binding, protein binding and anti-cancer activity on A549 lung carcinoma cell lines

Polyhedron ◽  
2014 ◽  
Vol 80 ◽  
pp. 20-33 ◽  
Author(s):  
Komal M. Vyas ◽  
R.N. Jadeja ◽  
Dipak Patel ◽  
R.V. Devkar ◽  
Vivek K. Gupta
2017 ◽  
Vol 46 (40) ◽  
pp. 13745-13755 ◽  
Author(s):  
Daniel Salvador-Gil ◽  
Lourdes Ortego ◽  
Raquel P. Herrera ◽  
Isabel Marzo ◽  
M. Concepción Gimeno

Unprecedented α-hydrazidophosphonate group 11 metal complexes have been prepared, with various coordination modes of ligands to metal atoms. They present an excellent cytotoxic activity in HeLa (cervical carcinoma) and A549 (lung carcinoma) cell lines, with IC50values among the lowest found in silver or copper complexes.


2001 ◽  
Vol 34 (2) ◽  
pp. 193-202 ◽  
Author(s):  
Masafumi Tomita ◽  
Toshiko Okuyama ◽  
Tetsuya Ishikawa ◽  
Kazuo Hidaka ◽  
Tsutomu Nohno

2022 ◽  
Vol 34 (2) ◽  
pp. 289-296
Author(s):  
Ahmed A. Emara ◽  
Ahmed M. Darwesh ◽  
Mohamed A. Mostafa ◽  
Ahmed A. Ahmed ◽  
Khaled W. Rashad ◽  
...  

Cucurbitacins are a class of highly oxidized tetracyclic triterpenoids. It’s hydrophobic properties and poor solubility in water, polymeric micellar systems exhibited improved antitumor efficacy because of a better solubilization and targeting after local and/or systemic administration. The aim of the present work was to evaluate the anticancer activity of CEG-AgNPs against benzo[a]pyren (BaP)-induced lung carcinoma. CEG-AgNPs was prepared, characterized and evaluated for its cytotoxic activity against A549 lung carcinoma cell line. Also, the anticancer activity of CEG-AgNPs (70.25 mg/kg) against BaP-induced lung carcinoma was evaluated in vivo, using 30 adult mice for 43 days. IC50 of CEG-AgNPs against A549 lung carcinoma cell line were approximately 94.47 μg/mL. Administration of BaP (50 mg/kg b.w.) to mice induced lung carcinoma with a significant increase in lung MMP-2, MMP-9, MMP-12, MDA, IL-6 and NF-κB as well as significant decreased in lung CAT, GPx and GSH level. Also, treatment with BaP produced significant increase in lung VEGF-C, COX-2 and Bcl-2 gene expression as compared to control group. Daily oral administration of CEG-AgNPs to mice treated with BaP showed a significant protection against-induced increase in lung MMP-2, MMP-9, MMP-12, MDA, IL-6 and NF-κB levels. The treatment also resulted in a significant increase in lung CAT, GPx and GSH level. In addition, the CEG-AgNPs could inhibit lung VEGF-C, COX-2 and Bcl-2 gene expression as compared to BaP treated mice. The histological and MRI examination showed that a significant normalization has been observed through in CEG-AgNPs treated mice. The biochemical, histological and MRI results showed that CEG-AgNPs have potent anticancer activity against BaP-induced lung carcinoma through modulating multiple cellular behaviours and signaling pathways leading to the suppression of adaptive immune responses.


Molecules ◽  
2019 ◽  
Vol 25 (1) ◽  
pp. 7 ◽  
Author(s):  
Xin Zhang ◽  
Yamei Li ◽  
Zhengping Feng ◽  
Yaling Zhang ◽  
Ye Gong ◽  
...  

Multifloroside (4), together with 10-hydroxyoleoside 11-methyl ester (1), 10-hydroxyoleoside dimethyl ester (2), and 10-hydroxyligustroside (3), are all secoiridoids, which are naturally occurring compounds that possess a wide range of biological and pharmacological activities. However, the anti-cancer activity of 1–4 has not been evaluated yet. The objective of this work was to study the anti-cancer activities of 1–4 in the human epidermoid carcinoma cell lines A431 and the human non-small cell lung cancer (NSCLC) cell lines A549. The results indicate that 1–4 differ in potency in their ability to inhibit the proliferation of human A431 and A549 cells, and multifloroside (4) display the highest inhibitory activity against A431 cells. The structure-activity relationships suggest that the o-hydroxy-p-hydroxy-phenylethyl group may contribute to the anti-cancer activity against A431 cells. Multifloroside treatment can also inhibit cell colony formation, arrest the cell cycle in the S-phase, increase the levels of reactive-oxygen-species (ROS), and mitochondrial membrane potential (MMP), but it did not significantly induce cell apoptosis at low concentrations. The findings indicated that multifloroside (4) has the tendency to show selective anti-cancer effects in A431 cells, along with suppressing the colony formation, inducing S cell cycle arrest, ROS production, and increasing MMP.


2008 ◽  
Vol 16 (7) ◽  
pp. 3626-3631 ◽  
Author(s):  
Stanton Hon Lung Kok ◽  
Roberto Gambari ◽  
Chung Hin Chui ◽  
Marcus Chun Wah Yuen ◽  
Eva Lin ◽  
...  

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