Evidence map›Paper›PMID 39425885›Full record

ArticlePharmacological reports : PR2024

Comprehensive evaluation of ibuprofenate amino acid isopropyl esters: insights into antioxidant activity, cytocompatibility, and cyclooxygenase inhibitory potential.

Magdalena Perużyńska, Anna Nowak, Anna Muzykiewicz-Szymańska, Łukasz Kucharski, Joanna Klebeko, Karolina Bilska, Ewelina Kopciuch, Radosław Birger, Marek Droździk, Paula Ossowicz-Rupniewska

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Pharmacological reports : PR, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.

0numbers the graph read from it
0cells of the map it votes in
0citing papers in PubMed
–field-weighted citation impact
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

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.

2 · The registry

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.

3 · Its place in the literature

Who cites it

0 citing papers in PubMed.

No citing paper in PubMed yet.

4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

10 authors.

Magdalena PerużyńskaDepartment of Experimental and Clinical Pharmacology, Pomeranian Medical University in Szczecin, Powstańców Wielkopolskich 72, 70-111, Szczecin, Poland.ORCID http://orcid.org/0000-0002-3193-4338
Anna NowakDepartment of Cosmetic and Pharmaceutical Chemistry, Pomeranian Medical University in Szczecin, Powstańców Wielkopolskich 72, 70-111, Szczecin, Poland.ORCID http://orcid.org/0000-0002-4287-6751
Anna Muzykiewicz-SzymańskaDepartment of Cosmetic and Pharmaceutical Chemistry, Pomeranian Medical University in Szczecin, Powstańców Wielkopolskich 72, 70-111, Szczecin, Poland.ORCID http://orcid.org/0000-0003-1880-1140
Łukasz KucharskiDepartment of Cosmetic and Pharmaceutical Chemistry, Pomeranian Medical University in Szczecin, Powstańców Wielkopolskich 72, 70-111, Szczecin, Poland.ORCID http://orcid.org/0000-0003-3295-5023
Joanna KlebekoFaculty of Chemical Technology and Engineering, Department of Chemical Organic Technology and Polymeric Materials, West Pomeranian University of Technology in Szczecin, Piastów Ave. 42, 71-065, Szczecin, Poland.ORCID http://orcid.org/0000-0002-3176-5511
Karolina BilskaFaculty of Chemical Technology and Engineering, Department of Chemical Organic Technology and Polymeric Materials, West Pomeranian University of Technology in Szczecin, Piastów Ave. 42, 71-065, Szczecin, Poland.ORCID http://orcid.org/0009-0001-9635-8909
Ewelina KopciuchFaculty of Chemical Technology and Engineering, Department of Chemical Organic Technology and Polymeric Materials, West Pomeranian University of Technology in Szczecin, Piastów Ave. 42, 71-065, Szczecin, Poland.ORCID http://orcid.org/0000-0002-2829-8158
Radosław BirgerDepartment of Experimental and Clinical Pharmacology, Pomeranian Medical University in Szczecin, Powstańców Wielkopolskich 72, 70-111, Szczecin, Poland.ORCID http://orcid.org/0009-0008-6256-5695
Marek DroździkDepartment of Experimental and Clinical Pharmacology, Pomeranian Medical University in Szczecin, Powstańców Wielkopolskich 72, 70-111, Szczecin, Poland.ORCID http://orcid.org/0000-0002-6191-7168
Paula Ossowicz-RupniewskaFaculty of Chemical Technology and Engineering, Department of Chemical Organic Technology and Polymeric Materials, West Pomeranian University of Technology in Szczecin, Piastów Ave. 42, 71-065, Szczecin, Poland. possowicz@zut.edu.pl.ORCID http://orcid.org/0000-0002-2362-1809

Funding

Narodowe Centrum Badań i Rozwoju LIDER/53/0225/L-11/19/NCBR/2020
6 · The paper itself

Abstract

Nonsteroidal anti-inflammatory drugs (NSAIDs) are widely used for pain relief and inflammation management, but there are challenges related to poor solubility and bioavailability. We explored modifications of ibuprofen (IBU) by forming ionic pairs using amino acid alkyl esters to enhance solubility without compromising the ability to inhibit cyclooxygenase (COX)-1 and COX-2). We comprehensively evaluated the pharmacological properties of the IBU derivatives, focusing on antioxidant activity (based on the ability to scavenge DPPH and ABTS), biocompatibility (using human dermal fibroblasts), and COX inhibitory potential. The antioxidant activity assays significantly enhanced DPPH scavenging activity for several IBU derivatives, particularly [L-SerOiPr][IBU], suggesting potential therapeutic benefits. There was enhanced cell viability with select derivatives, indicating possible stimulatory effects on cellular proliferation. Finally, predominant COX-1 inhibition across derivatives was consistent with IBU's profile. This study provides insights into the pharmacological properties of IBU amino acid derivatives, highlighting their potential as therapeutic agents. Further exploration into structure-activity relationships and in vivo efficacy warranted to advance these derivatives toward clinical applications, offering prospects for novel NSAIDs with enhanced efficacy and reduced side effects.

Indexed as

Amino AcidsAnti-Inflammatory Agents, Non-SteroidalAntioxidantsCell SurvivalCyclooxygenase 1Cyclooxygenase InhibitorsEstersIbuprofenCell ProliferationCyclooxygenase 2FibroblastsHumansStructure-Activity RelationshipAmino AcidsAnti-Inflammatory Agents, Non-SteroidalAntioxidantsCyclooxygenase 1Cyclooxygenase 2Cyclooxygenase InhibitorsEstersIbuprofenActive pharmaceutical ingredientsAnti-inflammatory activityAntioxidant activityCyclooxygenaseIbuprofenNonsteroidal anti-inflammatory drug

Identifiers

PMID39425885
PMCPMC11582120

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Registered trials

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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.