A potential antitumor agent, (6-amino-1-methyl-5-nitrosouracilato-N3)-triphenylphosphine-gold(I): Structural studies and in vivo biological effects against experimental glioma

Illán‐Cabeza, Nuria A.; García-García, Antonio R.; Martínez-Martos, José Manuel; Ramírez-Expósito, María Jesús; Peña-Ruiz, Tomás; Moreno‐Carretero, Miguel N.

doi:10.1016/j.ejmech.2013.03.067

Cited by 22 publications

(13 citation statements)

References 81 publications

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“…The depletion in GSH correlated with increased lipid peroxidation and protein oxidation. Increased GSSG levels correlated with increased H 2 O 2 production by the tumor, as well as to the changes in the activity of the GSH-related antioxidant enzymes [6]. These results are in accordance with those obtained in patients, where a significant depletion of GSH levels in astrocytoma, meningioma, metastatic and other types of brain tumors was also found by Navarro and col [46] when compared with their peritumoral tissues.…”

Section: Glutathione As the Main Non-enzymatic Antioxidant Defence Sysupporting

confidence: 87%

“…In animal models, increased levels of lipid peroxidation have been found in the serum of animals with C6 glioma implanted in the subcutaneous region when compared with non-tumor healthy control animals [6]. However, using transplacental ethylnitrosourea (ENU)-induced glioma, no changes in TBARS levels were observed in plasma of animals with glioma in comparison with healthy controls.…”

Section: Oxidative Stress Biomarkersmentioning

confidence: 99%

“…Finally, the role of SOD 3 in cancer is less well understood and probably it effects in cancer are mediated through the tumor microenvironment due to it extracellular localization [51]. In animals with C6 implanted-gliomas it has been described significant increased levels of serum SOD compared with the healthy control group [6]. However, the results described for other authors in human patients show a great heterogeneity; thus, lower levels of SOD have been described in brain tumor cases when compared with controls [52, 53], as well as a proportionate decrease of SOD activity with increasing grades of malignancy in brain tumors [54].…”

Section: Enzymatic Antioxidant Defence Systemsmentioning

confidence: 99%

“…Brain tumorigenesis (such as other tumor types) has been associated with oxidative stress that is reflected by an imbalance between free radicals production and antioxidant mechanisms. In fact, the resulting oxidative stress promotes various pathological reactions which contribute to different pathologies including carcinogenesis [6]. In these conditions, free radicals may be generated in excess from endogenous sources (mitochondria and peroxisomes, but also from inflammatory cell activation or neurotransmitter oxidation) and also exogenous sources as environmental agents, drugs, irradiation and chemicals.…”

Section: Introductionmentioning

confidence: 99%

“…Both systems act to prevent or decrease damages caused by free radicals in excess. However, they are controlled by polymorphic genes which can be altered by free radicals, leading to dysfunctions [6]. It is known that the modulation of intracellular levels of ROS plays a key role in the maintenance of cellular homeostasis, in fact, different levels of ROS may induce different responses; low and moderate levels of ROS may act as modulator of cellular proliferation and differentiation and also may be involved in the expression of antioxidant genes, but high levels induce severe cellular damages and also cellular death [23].…”

Section: Introductionmentioning

confidence: 99%

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The Delicate Equilibrium between Oxidants and Antioxidants in Brain Glioma

Ramírez-Expósito¹,

Martínez-Martos²

2019

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Gliomas are the most frequent brain tumors in adult population and unfortunately the adjuvant therapies are not effective. Brain tumorigenesis has been related both with the increased levels of free radicals as inductors of severe damages in healthy cells, but also with the reduced response of endogenous enzyme and non-enzymatic antioxidant defenses. In turn, both processes induce the change to malignant cells. In this review we analyzed the role of the imbalance between free radicals production and antioxidant mechanism in the development and progression of gliomas but also the influence of redox status on the two major distinctive forms of programmed cell death related to cancer: apoptosis and autophagy. These data may be the reference to the development of new pharmacological options based on redox microenvironment for glioma treatment.

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Section: Glutathione As the Main Non-enzymatic Antioxidant Defence Sysupporting

confidence: 87%

Section: Oxidative Stress Biomarkersmentioning

confidence: 99%

Section: Enzymatic Antioxidant Defence Systemsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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The Delicate Equilibrium between Oxidants and Antioxidants in Brain Glioma

Ramírez-Expósito¹,

Martínez-Martos²

2019

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Synthesis and biological evaluation of novel salicylidene uracils: Cytotoxic activity on human cancer cell lines and inhibitory action on enzymatic activity

Poslu,

Aslan,

Koz

et al. 2023

Archiv der Pharmazie

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A series of salicylidene uracil (1–18) derived from 5‐aminouracil and substituted salicylaldehydes were analyzed for cytotoxic activity and enzyme inhibitory potency. Nine out of eighteen derivatives (6–8, 10, 12–15, 18) are novel molecules synthesized for the first time in this work, and other derivatives were previously synthesized by our group. The compounds were characterized by Proton nuclear magnetic resonance, carbon nuclear magnetic resonance, fourier transform infrared spectroscopy, and elemental analysis. All compounds were tested for their in vitro cytotoxicity against PC‐3 (human prostate adenocarcinoma), A549 (human alveolar adenocarcinoma), and SHSY‐5Y (human neuroblastoma) cancer cell lines and the nontumorigenic HEK293 (human embryonic kidney cells) cell line. The 3,5‐di‐tert‐butylsalicylaldehyde derived compound (8) was toxic to PC‐3 human prostate adenocarcinoma cells, showing a promising IC50 value at 7.05 ± 0.76 μM. The present study also aimed to evaluate the inhibitory effects of the compounds against several key enzymes, namely carbonic anhydrase I and II (CA I and CA II), acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and glutathione reductase (GR), which are implicated in various global disorders, such as Alzheimer's disease, epilepsy, cancer, malaria, diabetes, and glaucoma. The inhibitory profiles of the tested compounds were assessed by determining their Ki values, which ranged from 2.96 to 9.24 nM for AChE, 3.78 to 12.57 nM for BChE, 8.42 to 25.74 nM for CA I, 7.24 to 19.74 nM for CA II, and 0.541 to 1.124 μM for GR. Molecular docking studies were also performed for all compounds. Most derivatives exhibited much more effective inhibitory action compared with clinically used standards. Thus, our findings indicate that the salicylidene derivatives presented in this study are promising drug candidates that need further evaluation.

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