Preparation and Evaluation of 6-Gingerol Derivatives as Novel Antioxidants and Antiplatelet Agents

Ginger (Zingiber officinale) is widely used as a spice and a traditional medicine. Many bioactivities have been reported for its extracts and the isolated compounds, including cardiovascular protective effects. Different pathways were suggested to contribute to these effects, like the inhibition of...

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Elmentve itt :
Bibliográfiai részletek
Szerzők: Ahmed Sara Hassan Hassan
Gonda Tímea
Agbadua Orinamhe Godwin
Girst Gábor
Berkecz Róbert
Kúsz Norbert
Tsai Meng-Chun
Chin-Chung Wu
Balogh György Tibor
Hunyadi Attila
Dokumentumtípus: Cikk
Megjelent: 2023
Sorozat:ANTIOXIDANTS 12 No. 3
Tárgyszavak:
doi:10.3390/antiox12030744

mtmt:33709440
Online Access:http://publicatio.bibl.u-szeged.hu/26790
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520 3 |a Ginger (Zingiber officinale) is widely used as a spice and a traditional medicine. Many bioactivities have been reported for its extracts and the isolated compounds, including cardiovascular protective effects. Different pathways were suggested to contribute to these effects, like the inhibition of platelet aggregation. In this study, we synthesised fourteen 6-gingerol derivatives, including eight new compounds, and studied their antiplatelet, COX-1 inhibitor, and antioxidant activities. In silico docking of selected compounds to h-COX-1 enzyme revealed favourable interactions. The investigated 6-gingerol derivatives were also characterised by in silico and experimental physicochemical and blood–brain barrier-related parameters for lead and preclinical candidate selection. 6-Shogaol (2) was identified as the best overall antiplatelet lead, along with compounds 3 and 11 and the new compound 17, which require formulation to optimize their water solubility. Compound 5 was identified as the most potent antioxidant that is also promising for use in the central nervous system (CNS). 
650 4 |a Kémiai tudományok 
650 4 |a Általános orvostudomány 
700 0 1 |a Gonda Tímea  |e aut 
700 0 1 |a Agbadua Orinamhe Godwin  |e aut 
700 0 1 |a Girst Gábor  |e aut 
700 0 1 |a Berkecz Róbert  |e aut 
700 0 1 |a Kúsz Norbert  |e aut 
700 0 1 |a Tsai Meng-Chun  |e aut 
700 0 2 |a Chin-Chung Wu  |e aut 
700 0 2 |a Balogh György Tibor  |e aut 
700 0 2 |a Hunyadi Attila  |e aut 
856 4 0 |u http://publicatio.bibl.u-szeged.hu/26790/3/33709440_cserelt.pdf  |z Dokumentum-elérés