Cytotoxic Activity Against SH-SY5Y Neuroblastoma Cells of Heterocyclic Compounds Containing gem-Dichlorocyclopropane and/or 1,3-Dioxacycloalkane Fragments

Kuzmina, U. Sh.; Раскильдина, Г. З.; Ishmetova, D. V.; Sakhabutdinova, G. N.; Dzhumaev, Sh. Sh.; Borisova, Yu. G.; Vakhitova, Yu. V.; Злотский, С. С.

doi:10.1007/s11094-022-02574-6

Cited by 6 publications

(2 citation statements)

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“…Additionally, their SI values were 2.4-3.3-fold higher than those of P7, and comparable to those of CB1H, thus establishing that the nanomanipulation of CB1H using P7 led to an improvement in both the cytotoxic properties and the SI values of both CB1H and P7. Finally, CB1H-P7 NPs were over 10-fold more effective than the best-performing molecule belonging to a library of compounds whose cytotoxic activity was recently reported against the SHSY 5Y cells used in this study after 48 h of exposure [ 65 ]. As mentioned above, upon nano-formulation of CB1H using P7, the antitumor effects of both P7 and CB1H were improved.…”

Section: Resultsmentioning

confidence: 84%

“…The concentrations of each sample administered to cells have been detailed in Table S1 available in Section S2 of SM. Although compounds with IC 50 values over 30 µM were recently reported as molecules with selective cytotoxic activity against SHSY 5Y NB cells [ 65 ], to assess the actual potential of our compounds for developing new promising agents against NB cells, we take as a reference compound the N-(4-hydroxyphenyl)-retinamide or fenretinide (4-HPR).…”

Section: Resultsmentioning

confidence: 99%

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Pyrazole-Enriched Cationic Nanoparticles Induced Early- and Late-Stage Apoptosis in Neuroblastoma Cells at Sub-Micromolar Concentrations

et al. 2023

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Neuroblastoma (NB) is a severe form of tumor occurring mainly in young children and originating from nerve cells found in the abdomen or next to the spine. NB needs more effective and safer treatments, as the chance of survival against the aggressive form of this disease are very small. Moreover, when current treatments are successful, they are often responsible for unpleasant health problems which compromise the future and life of surviving children. As reported, cationic macromolecules have previously been found to be active against bacteria as membrane disruptors by interacting with the negative constituents of the surface of cancer cells, analogously inducing depolarization and permeabilization, provoking lethal damage to the cytoplasmic membrane, and cause loss of cytoplasmic content and consequently, cell death. Here, aiming to develop new curative options for counteracting NB cells, pyrazole-loaded cationic nanoparticles (NPs) (BBB4-G4K and CB1H-P7 NPs), recently reported as antibacterial agents, were assayed against IMR 32 and SHSY 5Y NB cell lines. Particularly, while BBB4-G4K NPs demonstrated low cytotoxicity against both NB cell lines, CB1H-P7 NPs were remarkably cytotoxic against both IMR 32 and SHSY 5Y cells (IC50 = 0.43–0.54 µM), causing both early-stage (66–85%) and late-stage apoptosis (52–65%). Interestingly, in the nano-formulation of CB1H using P7 NPs, the anticancer effects of CB1H and P7 were increased by 54–57 and 2.5–4-times, respectively against IMR 32 cells, and by 53–61 and 1.3–2 times against SHSY 5Y cells. Additionally, based on the IC50 values, CB1H-P7 was also 1-12-fold more potent than fenretinide, an experimental retinoid derivative in a phase III clinical trial, with remarkable antineoplastic and chemopreventive properties. Collectively, due to these results and their good selectivity for cancer cells (selectivity indices = 2.8–3.3), CB1H-P7 NPs represent an excellent template material for developing new treatment options against NB.

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Section: Resultsmentioning

confidence: 84%

Section: Resultsmentioning

confidence: 99%