Antineoplastic activity of the thiazolo[5,4-b]quinoline derivative D3CLP in K-562 cells is mediated through effector caspases activation

González-Sánchez, Ignacio; Solano, José D.; Loza-Mejía, Marco A.; Olvera-Vázquez, Susana; Rodríguez‐Sotres, Rogelio; Morán, Julio; Lira‐Rocha, Alfonso; Cerbón, Marco

doi:10.1016/j.ejmech.2011.02.063

Cited by 40 publications

(29 citation statements)

References 27 publications

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“…Mitochondrial function was determined by the MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium) assay as previously described [26]. MTT is actively metabolized to formazan by healthy mitochondria.…”

Section: Methodsmentioning

confidence: 99%

Prolactin-induced neuroprotection against glutamate excitotoxicity is mediated by the reduction of [Ca2+]i overload and NF-κB activation

et al. 2017

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Prolactin (PRL) is a peptidic hormone that displays pleiotropic functions in the organism including different actions in the brain. PRL exerts a neuroprotective effect against excitotoxicity produced by glutamate (Glu) or kainic acid in both in vitro and in vivo models. It is well known that Glu excitotoxicity causes cell death through apoptotic or necrotic pathways due to intracellular calcium ([Ca2+] i) overload. Therefore, the aim of the present study was to assess the molecular mechanisms by which PRL maintains cellular viability of primary cultures of rat hippocampal neurons exposed to Glu excitotoxicity. We determined cell viability by monitoring mitochondrial activity and using fluorescent markers for viable and dead cells. The intracellular calcium level was determined by a fluorometric assay and proteins involved in the apoptotic pathway were determined by immunoblot. Our results demonstrated that PRL afforded neuroprotection against Glu excitotoxicity, as evidenced by a decrease in propidium iodide staining and by the decrease of the LDH activity. In addition, the MTT assay shows that PRL maintains normal mitochondrial activity even in neurons exposed to Glu. Furthermore, the Glu-induced intracellular [Ca2+]i overload was attenuated by PRL. These data correlate with the reduction found in the level of active caspase-3 and the pro-apoptotic ratio (Bax/Bcl-2). Concomitantly, PRL elicited the nuclear translocation of the transcriptional factor NF-κB, which was detected by immunofluorescence and confocal microscopy. To our knowledge, this is the first report demonstrating that PRL prevents Glu excitotoxicity by a mechanism involving the restoration of the intracellular calcium homeostasis and mitochondrial activity, as well as an anti-apoptotic action possibly mediated by the activity of NF-κB. Overall, the current results suggest that PRL could be of potential therapeutic advantage in the treatment of neurodegenerative diseases.

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Section: Methodsmentioning

confidence: 99%

Prolactin-induced neuroprotection against glutamate excitotoxicity is mediated by the reduction of [Ca2+]i overload and NF-κB activation

et al. 2017

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“…Thus, the activation status of the cell appears to have a major influence on drug metabolism. In this regard, PBMC have been used in toxicity assays in response to polysaccharides [40] and anti-tumor drugs [41,42].…”

Section: Monocytes In Drug Metabolismmentioning

confidence: 99%

In vitrodrug metabolism testing using blood-monocyte derivatives

Gómez-Icazbalceta

González-Sánchez

Moreno

et al. 2013

Expert Opinion on Drug Metabolism & Toxicology

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The use of monocytes, macrophages, dendritic or Kupffer cells, to test drug metabolism, has serious limitations because these cells express lower levels of cytochrome P450 enzymes than PHH. The best available option, to replace PHH, have been tumor cell lines such as HepaRG, as well as immortalized hepatocytes from adult or fetal sources. Monocyte-derived NeoHep cells are novel and easily accessible cells, which express many drug metabolizing enzymes at levels comparable to PHH. These cells allow drug evaluation under a diverse genetic background. While these cells are in the early stages of evaluation and do need to be examined more thoroughly, they constitute a promising new tool for in vitro drug testing.

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“…On the other hand, quinoline containing compounds have only been used for the treatment of malaria [10], beginning with quinine, which is a 4,6-substitued quinoline. Recently, the antitumor activity of quinolines as anticancer agents [11] and specially against breast cancer cell lines, with chloroquinoline being the most apoptosis-inducing agent, has been reported [12]. All differentiation-inducing quinolines caused growth suppression in MCF-7 and MCF 10 A cells.…”

Section: Introductionmentioning

confidence: 98%

Synthesis and anticancer activity of some novel trifluoromethylquinolines carrying a biologically active benzenesulfonamide moiety

Al‐Dosari

Ghorab

Alsaid

et al. 2013

European Journal of Medicinal Chemistry

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Antineoplastic activity of the thiazolo[5,4-b]quinoline derivative D3CLP in K-562 cells is mediated through effector caspases activation

Cited by 40 publications

References 27 publications

Prolactin-induced neuroprotection against glutamate excitotoxicity is mediated by the reduction of [Ca2+]i overload and NF-κB activation

Prolactin-induced neuroprotection against glutamate excitotoxicity is mediated by the reduction of [Ca2+]i overload and NF-κB activation

In vitrodrug metabolism testing using blood-monocyte derivatives

Synthesis and anticancer activity of some novel trifluoromethylquinolines carrying a biologically active benzenesulfonamide moiety

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