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Biodistribution and Anticancer Characteristics of Les-3833, A Novel 4-thiazolidinone-Based Lead Compound

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Department of Biochemistry, Danylo Halytsky Lviv National Medical University, Pekarska Street 69a, 79010 Lviv, Ukraine
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Department of Pharmaceutical, Organic and Bioorganic Chemistry, Danylo Halytsky Lviv National Medical University, Pekarska Street 69a, 79010 Lviv, Ukraine
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Department of Public Health, Dietetics and Lifestyle Disorders, Faculty of Medicine, University of Information Technology and Management in Rzeszow, Sucharskiego 2, 35-225 Rzeszow, Poland
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Department of Regulation of Cell Proliferation and Apoptosis, Institute of Cell Biology, National Academy of Sciences of Ukraine, Drahomanov Street 14/16, 79005 Lviv, Ukraine
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International Research and Innovation in Medicine Program, Cedars-Sinai Medical Center, 6500 Wilshire Blvd., 21st floor, Suite 2102, Los Angeles, CA 90048-5502, USA
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Authors to whom correspondence should be addressed.
Sci. Pharm. 2020, 88(2), 18; https://doi.org/10.3390/scipharm88020018
Received: 1 March 2020 / Revised: 18 March 2020 / Accepted: 25 March 2020 / Published: 30 March 2020
Recently, we identified the promising anticancer potential of the synthetic 4-thiazolidinone-based anticancer lead compound Les-3833 which demonstrated tumor-suppressing action in vitro and in vivo. Based on the results of previous studies, the aim of this research was to investigate the cytotoxicity in vitro and the biodistribution in laboratory mice to support the biotherapeutic drug development of Les-3833. Les-3833 (2.5 mg/kg) was intravenously injected into male Balb/c mice. Measurements were performed at 5 min, 15 min, 1 h, 4 h, and 24 h time points in blood plasma, brain, liver, and kidney using high-performance liquid chromatography/tandem mass spectrometry. After the administration of Les-3833, the maximum level of this compound was observed in plasma at 2.08 min. In the brain, the mean maximum concentration of Les-3833 was 7.17 ng/mL at 5 min, while after 15 min, it was not found. In the liver, at 5 min, the maximum concentration was 1190 ng/g. At 15 min, concentration of Les-3833 in the liver decreased by 14.3%; at 6 h by 22.8%; and after 24 h by 64.7%. Its maximum concentration in kidney was 404 ng/g within 5–15 min, at 1 h it decreased by 36.1%, and after 24 h by 49.3%. Thus, Les-3833 was rapidly taken up by different organs from the bloodstream, partially metabolized in the liver, and excreted mainly through the kidneys, while in the brain, a very low concentration could be observed for only a short period of time. View Full-Text
Keywords: BALB/C mice; cytotoxicity; biodistribution; 4-thiazolidinone derivative BALB/C mice; cytotoxicity; biodistribution; 4-thiazolidinone derivative
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Kobylinska, L.; Lozynskii, A.; Lesyk, R.; Stoika, R.; Vari, S.G. Biodistribution and Anticancer Characteristics of Les-3833, A Novel 4-thiazolidinone-Based Lead Compound. Sci. Pharm. 2020, 88, 18.

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