scholarly journals Gold compounds as anticancer agents: chemistry, cellular pharmacology, and preclinical studies

2009 ◽  
Vol 30 (3) ◽  
pp. 550-580 ◽  
Author(s):  
Stefania Nobili ◽  
Enrico Mini ◽  
Ida Landini ◽  
Chiara Gabbiani ◽  
Angela Casini ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
Preclinical Studies ◽  
Cellular Pharmacology ◽  
Gold Compounds

ChemInform Abstract: Gold Compounds as Anticancer Agents: Chemistry, Cellular Pharmacology, and Preclinical Studies

ChemInform ◽  
2010 ◽  
Vol 41 (31) ◽  
pp. no-no ◽  
Author(s):  
Stefania Nobili ◽  
Enrico Mini ◽  
Ida Landini ◽  
Chiara Gabbiani ◽  
Angela Casini ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
Preclinical Studies ◽  
Cellular Pharmacology ◽  
Gold Compounds

scholarly journals Ex vivo toxicological evaluation of experimental anticancer gold(i) complexes with lansoprazole-type ligands

2019 ◽  
Vol 8 (6) ◽  
pp. 885-895
Author(s):  
Natalia Estrada-Ortiz ◽  
Elena Lopez-Gonzales ◽  
Ben Woods ◽  
Stefan Stürup ◽  
Inge A. M. de Graaf ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
Ex Vivo ◽  
Gold Complex ◽  
Ex Vivo Model ◽  
Toxicological Evaluation ◽  
Anticancer Compounds ◽  
Kidney Slices ◽  
Icp Ms ◽  
Gold Compounds ◽  
Liver And Kidney

Abstract Gold-based compounds are of great interest in the field of medicinal chemistry as novel therapeutic (anticancer) agents due to their peculiar reactivity and mechanisms of action with respect to organic drugs. Despite their promising pharmacological properties, the possible toxic effects of gold compounds need to be carefully evaluated in order to optimize their design and applicability. This study reports on the potential toxicity of three experimental gold-based anticancer compounds featuring lansoprazole ligands (1–3) studied in an ex vivo model, using rat precision cut kidney and liver slices (PCKS and PCLS, respectively). The results showed a different toxicity profile for the tested compounds, with the neutral complex 2 being the least toxic, even less toxic than cisplatin, followed by the cationic complex 1. The dinuclear cationic gold complex 3 was the most toxic in both liver and kidney slices. This result correlated with the metal uptake of the different compounds assessed by ICP-MS, where complex 3 showed the highest accumulation of gold in liver and kidney slices. Interestingly compound 1 showed the highest selectivity towards cancer cells compared to the healthy tissues. Histomorphology evaluation showed a similar pattern for all three Au(i) complexes, where the distal tubular cells suffered the most extensive damage, in contrast to the damage in the proximal tubules induced by cisplatin. The binding of representative gold compounds with the model ubiquitin was also studied by ESI-MS, showing that after 24 h incubation only ‘naked’ Au ions were bound to the protein following ligands’ loss. The mRNA expression of stress response genes appeared to be similar for both evaluated organs, suggesting oxidative stress as the possible mechanism of toxicity. The obtained results open new perspectives towards the design and testing of bifunctional gold complexes with chemotherapeutic applications.

scholarly journals Cellular pharmacology studies of anticancer agents: recommendations from the EORTC-PAMM group

2017 ◽  
Vol 81 (3) ◽  
pp. 427-441 ◽  
Author(s):  
Paola Perego ◽  
◽  
Georg Hempel ◽  
Stig Linder ◽  
Tracey D. Bradshaw ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
Cellular Pharmacology

scholarly journals Combined Effect of Caspase-Dependent and Caspase-Independent Apoptosis in the Anticancer Activity of Gold Complexes with Phosphine and Benzimidazole Derivatives

2020 ◽  
Vol 14 (1) ◽  
pp. 10
Author(s):  
Lara Rouco ◽  
Ángeles Sánchez-González ◽  
Rebeca Alvariño ◽  
Amparo Alfonso ◽  
Ezequiel M. Vázquez-López ◽  
...  
Keyword(s):  
Cell Death ◽  
Anticancer Activity ◽  
Anticancer Agents ◽  
Neuroblastoma Cells ◽  
Fluorescence Analysis ◽  
Benzimidazole Derivatives ◽  
Human Neuroblastoma ◽  
Gold Compounds ◽  
Pre Treatment ◽  
Standard Techniques

Since the potential anticancer activity of auranofin was discovered, gold compounds have attracted interest with a view to developing anticancer agents that follow cytotoxic mechanisms other than cisplatin. Two benzimidazole gold(I) derivatives containing triphenylphosphine (Au(pben)(PPh3)) (1) or triethylphosphine (Au(pben)(PEt3)) (2) were prepared and characterized by standard techniques. X-ray crystal structures for 1 and 2 were solved. The cytotoxicity of 1 and 2 was tested in human neuroblastoma SH-SY5Y cells. Cells were incubated with compounds for 24 h with concentrations ranging from 10 µM to 1 nM, and the half-maximal inhibitory concentration (IC50) was determined. 1 and 2 showed an IC50 of 2.7 and 1.6 µM, respectively. In order to better understand the type of cell death induced by compounds, neuroblastoma cells were stained with Annexin-FITC and propidium iodide. The fluorescence analysis revealed that compounds were inducing apoptosis; however, pre-treatment with the caspase inhibitor Z-VAD did not reduce cell death. Analysis of compound effects on caspase-3 activity and reactive oxygen species (ROS) production in SH-SY5Y cells revealed an antiproliferative ability mediated through oxidative stress and both caspase-dependent and caspase-independent mechanisms.

scholarly journals Auranofin and its analogs as prospective agents for the treatment of colorectal cancer

2022 ◽  
Author(s):  
Lara Massai ◽  
Damiano Cirri ◽  
Tiziano Marzo ◽  
Luigi Messori
Keyword(s):  
Colorectal Cancer ◽  
Anticancer Agents ◽  
Pharmaceutical Formulations ◽  
Therapeutic Agents ◽  
General Interest ◽  
Platinum Drugs ◽  
Cancer Death ◽  
Pharmacological Profile ◽  
Medical Treatments ◽  
Gold Compounds

Today colorectal cancer (CRC) is one of the leading causes of cancer death worldwide. This disease is poorly chemo-sensitive toward the existing medical treatments so that new and more effective therapeutic agents are urgently needed and intensely sought. Platinum drugs, oxaliplatin in particular, were reported to produce some significant benefit in CRC treatment, triggering the general interest of medicinal chemists and oncologists for metal-based compounds as candidate anti-CRC drugs. Within this frame, gold compounds and, specifically, the established antiarthritic drug auranofin with its analogs, form a novel group of promising anticancer agents. Owing to its innovative mechanism of action and its favorable pharmacological profile, auranofin together with its derivatives are proposed here as novel experimental agents for CRC treatment, capable of overcoming resistance to platinum drugs. Some encouraging results in this direction have already been obtained. A few recent studies demonstrate that the action of auranofin may be further potentiated through the preparation of suitable pharmaceutical formulations capable of protecting the gold pharmacophore from unselective reactivity or through the design of highly synergic drug combinations. The perspectives of the research in this field are outlined.

scholarly journals Breast Cancer Treatment: The Case of Gold(I)-Based Compounds as a Promising Class of Bioactive Molecules

Biomolecules ◽  
2022 ◽  
Vol 12 (1) ◽  
pp. 80
Author(s):  
Rossana Galassi ◽  
Lorenzo Luciani ◽  
Junbiao Wang ◽  
Silvia Vincenzetti ◽  
Lishan Cui ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
New Drugs ◽  
Bioactive Molecules ◽  
Gold Compound ◽  
Central Metal ◽  
Breast Cancers ◽  
Carbene Ligands ◽  
Highly Active ◽  
Gold Compounds ◽  
Recent Developments

Breast cancers (BCs) may present dramatic diagnoses, both for ineffective therapies and for the limited outcomes in terms of lifespan. For these types of tumors, the search for new drugs is a primary necessity. It is widely recognized that gold compounds are highly active and extremely potent as anticancer agents against many cancer cell lines. The presence of the metal plays an essential role in the activation of the cytotoxicity of these coordination compounds, whose activity, if restricted to the ligands alone, would be non-existent. On the other hand, gold exhibits a complex biochemistry, substantially variable depending on the chemical environments around the central metal. In this review, the scientific findings of the last 6–7 years on two classes of gold(I) compounds, containing phosphane or carbene ligands, are reviewed. In addition to this class of Au(I) compounds, the recent developments in the application of Auranofin in regards to BCs are reported. Auranofin is a triethylphosphine-thiosugar compound that, being a drug approved by the FDA—therefore extensively studied—is an interesting lead gold compound and a good comparison to understand the activities of structurally related Au(I) compounds.

scholarly journals Use of Stingless Bee Propolis and Geopropolis against Cancer—A Literature Review of Preclinical Studies

2021 ◽  
Vol 14 (11) ◽  
pp. 1161
Author(s):  
Francisco Assis Nascimento Pereira ◽  
Josianne Rocha Barboza ◽  
Cleydlenne Costa Vasconcelos ◽  
Alberto Jorge Oliveira Lopes ◽  
Maria Nilce de Sousa Ribeiro
Keyword(s):  
Chemical Composition ◽  
Literature Review ◽  
Anticancer Agents ◽  
Biological Activities ◽  
Stingless Bee ◽  
Preclinical Studies ◽  
Biological Assays ◽  
Myelocytic Leukemia ◽  
Preclinical Trials ◽  
Therapeutic Properties

Cancer is one of the major maladies affecting humankind and remains one of the leading causes of death worldwide. The investigation of the biological activities of stingless bee products, especially propolis and geopropolis, has revealed promising therapeutic properties, especially in the research on new antineoplastic agents. This literature review of preclinical trials, involving biological assays of antitumor activity and identification of the chemical composition of propolis and geopropolis of stingless bee species, describes the cytotoxicity in tumor lineages (breast, lung, ovarian, liver, mouth, pharynx, larynx, colon, stomach, colorectal, cervix, kidney, prostate, melanoma, human glioblastoma, canine osteosarcoma, erythroleukemia, human chronic myelocytic leukemia, and human promyelocytic leukemia) of propolis and geopropolis of 33 species of stingless bees. The chemical composition of propolis and geopropolis was identified, indicating that these belong to the chemical classes of phenolic acids, flavonoids, coumarins, benzophenones, anthraquinones, alkaloids, terpenes, steroids, saponins, fatty acids, and carbohydrates and are possibly responsible for the cytotoxicity in tumor cells. Apoptosis was one of the main mechanisms of cytotoxicity of extracts and substances isolated from stingless bee products. Although the results found are encouraging, other preclinical studies and clinical trials are essential for the discovery of new anticancer agents.

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