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Membranes
Volume 14
Issue 12
10.3390/membranes14120274
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Article

Anti-Inflammatory Properties of Novel 1,2-Benzothiazine Derivatives and Their Interaction with Phospholipid Model Membranes

by
Berenika M. Szczęśniak-Sięga
1,*,
Jadwiga Maniewska
1,
Benita Wiatrak
2,
Tomasz Janek
3,
Paulina Nowotarska
4 and
Żaneta Czyżnikowska
5,*
1
Department of Medicinal Chemistry, Faculty of Pharmacy, Wroclaw Medical University, Borowska 211, 50-556 Wroclaw, Poland
2
Department of Pharmacology, Faculty of Medicine, Wroclaw Medical University, J. Mikulicza-Radeckiego 2, 50-345 Wroclaw, Poland
3
Department of Biotechnology and Food Microbiology, Faculty of Biotechnology and Food Science, Wroclaw University of Environmental and Life Sciences, Chełmońskiego 37, 51-630 Wroclaw, Poland
4
Department of Biostructure and Animal Physiology, Wroclaw University of Environmental and Life Sciences, Norwida 25/27, 50-375 Wroclaw, Poland
5
Department of Basic Chemical Sciences, Faculty of Pharmacy, Wroclaw Medical University, Borowska 211a, 50-556 Wroclaw, Poland
*
Authors to whom correspondence should be addressed.
Membranes 2024, 14(12), 274; https://doi.org/10.3390/membranes14120274
Submission received: 13 November 2024 / Revised: 5 December 2024 / Accepted: 16 December 2024 / Published: 18 December 2024
(This article belongs to the Special Issue Recent Advances in Biomembrane Models for Studying Interactions with Bio-/Molecules)
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Abstract

The design of novel anti-inflammatory drugs remains a critical area of research in the development of effective treatments for inflammatory diseases. In this study, a series of 1,2-benzothiazine was evaluated through a multifaceted approach. In particular, we investigated the potential interactions of the potential drugs with lipid bilayers, an important consideration for membrane permeability and overall pharmacokinetics. In addition, we evaluated their ability to inhibit cyclooxygenase 1 and cyclooxygenase 2 activity and selectivity using both a cyclooxygenase inhibition assay and molecular docking simulations. To evaluate their therapeutic potential, we performed in vitro assays to measure cytokine mRNA expression in inflamed cells. The antioxidant activity was evaluated using both in vitro assays, such as 2,2-diphenyl-1-picrylhydrazyl and 2,2-azino-bis-3-ethylbenzothiazoline-6-sulphonic acid scavenging, to determine the compounds’ capacity to neutralize free radicals and reduce oxidative stress. Theoretical calculations, including density functional theory, were used to predict the reactivity profiles of the compounds.
Keywords: 1,2-benzothiazine derivatives; drug–membrane interaction; anti-inflammatory activity; antioxidant properties 1,2-benzothiazine derivatives; drug–membrane interaction; anti-inflammatory activity; antioxidant properties

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MDPI and ACS Style

Szczęśniak-Sięga, B.M.; Maniewska, J.; Wiatrak, B.; Janek, T.; Nowotarska, P.; Czyżnikowska, Ż. Anti-Inflammatory Properties of Novel 1,2-Benzothiazine Derivatives and Their Interaction with Phospholipid Model Membranes. Membranes 2024, 14, 274. https://doi.org/10.3390/membranes14120274

AMA Style

Szczęśniak-Sięga BM, Maniewska J, Wiatrak B, Janek T, Nowotarska P, Czyżnikowska Ż. Anti-Inflammatory Properties of Novel 1,2-Benzothiazine Derivatives and Their Interaction with Phospholipid Model Membranes. Membranes. 2024; 14(12):274. https://doi.org/10.3390/membranes14120274

Chicago/Turabian Style

Szczęśniak-Sięga, Berenika M., Jadwiga Maniewska, Benita Wiatrak, Tomasz Janek, Paulina Nowotarska, and Żaneta Czyżnikowska. 2024. "Anti-Inflammatory Properties of Novel 1,2-Benzothiazine Derivatives and Their Interaction with Phospholipid Model Membranes" Membranes 14, no. 12: 274. https://doi.org/10.3390/membranes14120274

APA Style

Szczęśniak-Sięga, B. M., Maniewska, J., Wiatrak, B., Janek, T., Nowotarska, P., & Czyżnikowska, Ż. (2024). Anti-Inflammatory Properties of Novel 1,2-Benzothiazine Derivatives and Their Interaction with Phospholipid Model Membranes. Membranes, 14(12), 274. https://doi.org/10.3390/membranes14120274

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