4-Thiazolidinone-based derivatives do not affect differentiation of mouse embryo fibroblasts (3T3-L1 cell line) into adipocytes

Szychowski, Konrad A.; Skóra, Bartosz; Kryshchyshyn‐Dylevych, Anna; Kaminskyy, Danylo; Tobiasz, Jakub; Lesyk, Roman; Gmiński, Jan

doi:10.1016/j.cbi.2021.109538

Cited by 11 publications

(4 citation statements)

References 40 publications

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“…Another 4-TZD derivative, Les-4368 ( Figure 4 ), induced apoptosis in mammalian leukemia cells via G 0 /G 1 arrest and ROS production [ 5 ]. Interestingly, Les-3377 caused ROS production in mouse embryo fibroblasts (3T3-L1), without significant changes in the case of Les-2194 and Les-3640 [ 45 ]. As shown by, e.g., Kaminskyy et al and Abd Al Moaty et al, the ability to induce ROS overproduction is one of the well-described anticancer strategies, based on which the new TZD-based derivatives are being designed [ 5 , 46 ].…”

Section: Resultsmentioning

confidence: 99%

“…In turn, Szychowski et al (2021) showed a Les-3377-induced decrease in metabolic activity in BJ cells [ 13 ]. Another study of Les-3377 showed decreased metabolic activity in 3T3-L1 cells at 2 and 10 μM of the compound [ 45 ]. Finiuk et al (2023) described a decrease in metabolic activity in SCC-15 cells exposed to 4-TZD derivatives Les-6287, Les-6294, and Les-6328 ( Figure 4 ) [ 50 ].…”

Section: Resultsmentioning

confidence: 99%

“…Moreover, the PPARγ agonist (rosiglitazone) increased PPARγ protein expression in the CACO-2 cell line, and the PPARγ antagonist (GW9662) increased protein expression in the SCC-15 cell line [ 53 ], which is similar to our results obtained for the A549 cells. In turn, other 4-TZD derivatives, i.e., Les-3377 and Les-3640 (2 μM), induced increased PPARγ protein expression in the 3T3-L1 cell line [ 45 ]. Szychowski et al (2021) reported increased PPARγ protein expression caused by 10 μM Les-3377 and Les-3640 in SCC-15 cells [ 13 ].…”

Section: Resultsmentioning

confidence: 99%

Section: Ros Productionmentioning

confidence: 85%

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Role of 4-Thiazolidinone–Pyrazoline/Indoline Hybrids Les-4369 and Les-3467 in BJ and A549 Cell Lines

Kosińska,

Skóra,

Holota

et al. 2024

Cells

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Cancer is one of the most important problems of modern societies. Recently, studies have reported the anticancer properties of rosiglitazone related to its ability to bind peroxisome proliferator receptor γ (PPARγ), which has various effects on cancer and can inhibit cell proliferation. In this study, we investigated the effect of new 4-thiazolidinone (4-TZD) hybrids Les-4369 and Les-3467 and their effect on reactive oxygen species (ROS) production, metabolic activity, lactate dehydrogenase (LDH) release, caspase-3 activity, and gene and protein expression in human foreskin fibroblast (BJ) cells and lung adenocarcinoma (A549) cells. The ROS production and caspase-3 activity were mainly increased in the micromolar concentrations of the studied compounds in both cell lines. Les-3467 and Les-4369 increased the mRNA expression of PPARG, P53 (tumor protein P53), and ATM (ATM serine/threonine kinase) in the BJ cells, while the mRNA expression of these genes (except PPARG) was mainly decreased in the A549 cells treated with both of the tested compounds. Our results indicate a decrease in the protein expression of AhR, PPARγ, and PARP-1 in the BJ cells exposed to 1 µM Les-3467 and Les-4369. In the A549 cells, the protein expression of AhR, PPARγ, and PARP-1 increased in the treatment with 1 µM Les-3467 and Les-4369. We have also shown the PPARγ modulatory properties of Les-3467 and Les-4369. However, both compounds prove weak anticancer properties evidenced by their action at high concentrations and non-selective effects against BJ and A549 cells.

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