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001-es BibID:BIBFORM091222
035-os BibID:(WoS)000615458000001 (Scopus)85100492364
Első szerző:Gyöngyösi Alexandra (táplálkozástudományi szakember)
Cím:Basic Pharmacological Characterization of EV-34, a New H2S-Releasing Ibuprofen Derivative / Alexandra Gyöngyösi, Vivien Verner, Ilona Bereczki, Attila Kiss-Szikszai, Rita Zilinyi, Árpád Tósaki, István Bak, Anikó Borbás, Pál Herczegh, István Lekli
Dátum:2021
ISSN:1420-3049
Megjegyzések:Background: Cardioprotective effects of H2S are being suggested by numerous studies. Furthermore, H2S plays a role in relaxation of vascular smooth muscle, protects against oxidative stress, and modulates inflammation. Long-term high-dose use of NSAIDs, such as ibuprofen, have been associated with enhanced cardiovascular risk. The goal of the present work is the synthesis and basic pharmacological characterization of a newly designed H2S-releasing ibuprofen derivative. Methods: Following the synthesis of EV-34, a new H2S-releasing derivative of ibuprofen, oxidative stability assays were performed (Fenton and porphyrin assays). Furthermore, stability of the molecule was studied in rat serum and liver lysates. H2S-releasing ability of the EC-34 was studied with a hydrogen sulfide sensor. MTT (3-(4,5-dimethylthiazol 2-yl)-2,5-(diphenyltetrazolium bromide)) assay was carried out to monitor the possible cytotoxic effect of the compound. Cyclooxygenase (COX) inhibitory property of EV-34 was also evaluated. Carrageenan assay was carried out to compare the anti-inflammatory effect of EV-34 to ibuprofen in rat paws. Results: The results revealed that the molecule is stable under oxidative condition of Fenton reaction. However, EV-34 undergoes biodegradation in rat serum and liver lysates. In cell culture medium H2S is being released from EV-34. No cytotoxic effect was observed at concentrations of 10, 100, 500 mu M. The COX-1 and COX-2 inhibitory effects of the molecule are comparable to those of ibuprofen. Furthermore, based on the carrageenan assay, EV-34 exhibits the same anti-inflammatory effect to that of equimolar amount of ibuprofen (100 mg/bwkg). Conclusion: The results indicate that EV-34 is a safe H2S releasing ibuprofen derivative bearing anti-inflammatory properties.
Tárgyszavak:Orvostudományok Gyógyszerészeti tudományok idegen nyelvű folyóiratközlemény külföldi lapban
folyóiratcikk
Megjelenés:Molecules. - 26 : 3 (2021), p. 1-12. -
További szerzők:Verner Vivien Bereczki Ilona (1981-) (vegyész, antibiotikumkémikus) Kiss-Szikszai Attila (1975-) (vegyész) Zilinyi Rita Tósaki Árpád (1958-) (kísérletes farmakológus, gyógyszerész) Bak István (1975-) (vegyész, analitikus, farmakológus) Borbás Anikó (1965-) (vegyész) Herczegh Pál (1947-) (vegyész, antibiotikumkémikus) Lekli István (1981-) (gyógyszerész)
Pályázati támogatás:GINOP-2.3.2-15-2016-00043
GINOP
EFOP-3.6.1-16-2016-00022
EFOP
NKFIH-1150-6/2019
Egyéb
NKFIH-K-124719
Egyéb
NKFIH-K-132870
Egyéb
TKP2020-IKA-04
Egyéb
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