Evaluation of Anticancer and Antibacterial Activity of Four 4-Thiazolidinone-Based Derivatives
Heterocycles are commonly known for their unique features, e.g., antibacterial or anticancer properties. Although many synthetic heterocycles, such as 4-thiazolidinone (4-TZD), have been synthesized, their potential applications have not yet been fully investigated. However, many researchers have re...
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| Format: | Article |
| Language: | English |
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MDPI AG
2022-01-01
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| Series: | Molecules |
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| Online Access: | https://www.mdpi.com/1420-3049/27/3/894 |
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| author | Bartosz Skóra Anna Lewińska Anna Kryshchyshyn-Dylevych Danylo Kaminskyy Roman Lesyk Konrad A. Szychowski |
| author_facet | Bartosz Skóra Anna Lewińska Anna Kryshchyshyn-Dylevych Danylo Kaminskyy Roman Lesyk Konrad A. Szychowski |
| author_sort | Bartosz Skóra |
| collection | DOAJ |
| description | Heterocycles are commonly known for their unique features, e.g., antibacterial or anticancer properties. Although many synthetic heterocycles, such as 4-thiazolidinone (4-TZD), have been synthesized, their potential applications have not yet been fully investigated. However, many researchers have reported relevant results that can be a basis for the search for new potential drugs. Therefore, the aim of this study was to evaluate the cytotoxic, cytostatic, and antibacterial effects of certain 4-thiazolidinone-based derivatives, Les-3166, Les-5935, Les-6009, and Les-6166, on human fibroblasts (BJ), neuroblastoma (SH-SY5Y), epithelial lung carcinoma (A549), and colorectal adenocarcinoma (CACO-2) cell lines in vitro. All tested compounds applied in a concentration range from 10 to 100 µM were able to decrease metabolic activity in the BJ, A549, and SH-SY5Y cell lines. However, the action of Les-3166 was mainly based on the ROS-independent pathway, similarly to Les-6009. In turn, Les-5935 and Les-6166 were able to promote ROS production in BJ, A549, and SH-SY5Y cells, compared to the control. Les-3166, Les-6009, and Les-6166 significantly increased the caspase-3 activity, especially at the concentrations of 50 µM and 100 µM. However, Les-5935 did not induce apoptosis. Only Les-5935 showed a minor cytostatic effect on SH-SY5Y cells. Additionally, the antibacterial properties of the tested compounds against <i>P. aeruginosa</i> bacterial biofilm can be ranked as follows: Les-3166 > Les-5935 > Les-6009. Les-6166 did not show any anti-biofilm activity. In summary, the study showed that Les-5935, Les-6009, and Les-6166 were characterized by anticancer properties, especially in the human lung cancer cell. In cases of BJ, SH-SY5Y, and CACO-2 cells the anticancer usage of such compounds is limited due to effect visible only at 50 and 100 µM. |
| first_indexed | 2024-03-09T23:28:15Z |
| format | Article |
| id | doaj.art-68ec52a01c04458f935066b17d33cd9c |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-03-09T23:28:15Z |
| publishDate | 2022-01-01 |
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| spelling | doaj.art-68ec52a01c04458f935066b17d33cd9c2023-11-23T17:14:12ZengMDPI AGMolecules1420-30492022-01-0127389410.3390/molecules27030894Evaluation of Anticancer and Antibacterial Activity of Four 4-Thiazolidinone-Based DerivativesBartosz Skóra0Anna Lewińska1Anna Kryshchyshyn-Dylevych2Danylo Kaminskyy3Roman Lesyk4Konrad A. Szychowski5Department of Biotechnology and Cell Biology, Medical College, University of Information Technology and Management in Rzeszow, Sucharskiego 2, 35-225 Rzeszow, PolandDepartment of Biotechnology, Institute of Biology and Biotechnology, College of Natural Sciences, University of Rzeszow, Pigonia 1, 35-310 Rzeszow, PolandDepartment of Pharmaceutical, Organic and Bioorganic Chemistry, Danylo Halytsky Lviv National Medical University, Pekarska 69, 79010 Lviv, UkraineDepartment of Pharmaceutical, Organic and Bioorganic Chemistry, Danylo Halytsky Lviv National Medical University, Pekarska 69, 79010 Lviv, UkraineDepartment of Biotechnology and Cell Biology, Medical College, University of Information Technology and Management in Rzeszow, Sucharskiego 2, 35-225 Rzeszow, PolandDepartment of Biotechnology and Cell Biology, Medical College, University of Information Technology and Management in Rzeszow, Sucharskiego 2, 35-225 Rzeszow, PolandHeterocycles are commonly known for their unique features, e.g., antibacterial or anticancer properties. Although many synthetic heterocycles, such as 4-thiazolidinone (4-TZD), have been synthesized, their potential applications have not yet been fully investigated. However, many researchers have reported relevant results that can be a basis for the search for new potential drugs. Therefore, the aim of this study was to evaluate the cytotoxic, cytostatic, and antibacterial effects of certain 4-thiazolidinone-based derivatives, Les-3166, Les-5935, Les-6009, and Les-6166, on human fibroblasts (BJ), neuroblastoma (SH-SY5Y), epithelial lung carcinoma (A549), and colorectal adenocarcinoma (CACO-2) cell lines in vitro. All tested compounds applied in a concentration range from 10 to 100 µM were able to decrease metabolic activity in the BJ, A549, and SH-SY5Y cell lines. However, the action of Les-3166 was mainly based on the ROS-independent pathway, similarly to Les-6009. In turn, Les-5935 and Les-6166 were able to promote ROS production in BJ, A549, and SH-SY5Y cells, compared to the control. Les-3166, Les-6009, and Les-6166 significantly increased the caspase-3 activity, especially at the concentrations of 50 µM and 100 µM. However, Les-5935 did not induce apoptosis. Only Les-5935 showed a minor cytostatic effect on SH-SY5Y cells. Additionally, the antibacterial properties of the tested compounds against <i>P. aeruginosa</i> bacterial biofilm can be ranked as follows: Les-3166 > Les-5935 > Les-6009. Les-6166 did not show any anti-biofilm activity. In summary, the study showed that Les-5935, Les-6009, and Les-6166 were characterized by anticancer properties, especially in the human lung cancer cell. In cases of BJ, SH-SY5Y, and CACO-2 cells the anticancer usage of such compounds is limited due to effect visible only at 50 and 100 µM.https://www.mdpi.com/1420-3049/27/3/894anticancer propertiesheterocyclescell cyclecytotoxicitysynthetic compounds |
| spellingShingle | Bartosz Skóra Anna Lewińska Anna Kryshchyshyn-Dylevych Danylo Kaminskyy Roman Lesyk Konrad A. Szychowski Evaluation of Anticancer and Antibacterial Activity of Four 4-Thiazolidinone-Based Derivatives Molecules anticancer properties heterocycles cell cycle cytotoxicity synthetic compounds |
| title | Evaluation of Anticancer and Antibacterial Activity of Four 4-Thiazolidinone-Based Derivatives |
| title_full | Evaluation of Anticancer and Antibacterial Activity of Four 4-Thiazolidinone-Based Derivatives |
| title_fullStr | Evaluation of Anticancer and Antibacterial Activity of Four 4-Thiazolidinone-Based Derivatives |
| title_full_unstemmed | Evaluation of Anticancer and Antibacterial Activity of Four 4-Thiazolidinone-Based Derivatives |
| title_short | Evaluation of Anticancer and Antibacterial Activity of Four 4-Thiazolidinone-Based Derivatives |
| title_sort | evaluation of anticancer and antibacterial activity of four 4 thiazolidinone based derivatives |
| topic | anticancer properties heterocycles cell cycle cytotoxicity synthetic compounds |
| url | https://www.mdpi.com/1420-3049/27/3/894 |
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