ArticlePharmacological reports : PR2022
Effect of tricyclic 1,2-thiazine derivatives in neuroinflammation induced by preincubation with lipopolysaccharide or coculturing with microglia-like cells.
Article in Pharmacological reports : PR, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 papers, 1 of them a synthesis that pooled it.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
5 citing papers in PubMed, 1 synthesis or guideline pooled it, 6 citations in OpenAlex.
- A Hierarchical Framework for In Vitro Models of Alzheimer's Disease.WIREs mechanisms of diseasePooled it
- Anti-Inflammatory Activity of 1,2-Benzothiazine 1,1-Dioxide Derivatives.Pharmaceuticals (Basel, Switzerland) · 2025Review
- Anti-Inflammatory Properties of Novel 1,2-Benzothiazine Derivatives and Their Interaction with Phospholipid Model Membranes.Membranes · 2024Article
- Article
- Green Synthetic Methods of Oxazine and Thiazine Scaffolds as Promising Medicinal Compounds: A Mini-review.Current organic synthesis · 2024Review
Corrections and comments
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Authors and funding
6 authors at 1 institution in 1 country.
Funding
Abstract
backgroundAlzheimer's disease (AD) is considered the most common cause of dementia among the elderly. One of the modifiable causes of AD is neuroinflammation. The current study aimed to investigate the influence of new tricyclic 1,2-thiazine derivatives on in vitro model of neuroinflammation and their ability to cross the blood-brain barrier (BBB).
methodsThe potential anti-inflammatory effect of new tricyclic 1,2-thiazine derivatives (TP1, TP4, TP5, TP6, TP7, TP8, TP9, TP10) was assessed in SH-SY5Y cells differentiated to the neuron-like phenotype incubated with bacterial lipopolysaccharide (5 or 50 μg/ml) or THP-1 microglial cell culture supernatant using MTT, DCF-DA, Griess, and fast halo (FHA) assays. Additionally, for cultures preincubated with 50 µg/ml lipopolysaccharide (LPS), a cyclooxygenase (COX) activity assay was performed. Finally, the potential ability of tested compounds to cross the BBB was evaluated by computational studies. Molecular docking was performed with the TLR4/MD-2 complex to assess the possibility of binding the tested compounds in the LPS binding pocket. Prediction of ADMET parameters (absorption, distribution, metabolism, excretion and toxicity) was also conducted.
resultsThe unfavorable effect of LPS and co-culture with THP-1 cells on neuronal cell viability was counteracted with TP1 and TP4 in all tested concentrations. Tested compounds reduced the oxidative and nitrosative stress induced by both LPS and microglia activation and also reduced DNA damage. Furthermore, new derivatives inhibited total COX activity. Additionally, new compounds would cross the BBB with high probability and reach concentrations in the brain not lower than in the serum. The binding affinity at the TLR4/MD-2 complex binding site of TP4 and TP8 compounds is similar to that of the drug donepezil used in Alzheimer's disease. The ADMET analysis showed that the tested compounds should not be toxic and should show high intestinal absorption.
conclusionsNew tricyclic 1,2-thiazine derivatives exert a neuroregenerative effect in the neuroinflammation model, presumably via their inhibitory influence on COX activity and reduction of oxidative and nitrosative stress.
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