Elucidation of Phosphodiesterase-1 Inhibitory Effect of Some Selected Natural Polyphenolics Using In Vitro and In Silico Methods

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dc.contributor.authorRauf, Abdur
dc.contributor.authorOrhan, Ilkay Erdogan
dc.contributor.authorErtas, Abdulselam
dc.contributor.authorTemel, Hamdi
dc.contributor.authorBen Hadda, Taibi
dc.contributor.authorSaleem, Muhammad
dc.contributor.authorRaza, Muslim
dc.date.accessioned2024-04-24T17:18:34Z
dc.date.available2024-04-24T17:18:34Z
dc.date.issued2017
dc.departmentDicle Üniversitesien_US
dc.description.abstractBackground: Polyphenols are organic compounds widely found in plants and possess many diverse biological activities. In the current study, eleven polyphenolic compounds [ rutin (1), trans-ferulic acid (2), epigallaocatechin gallate (3), fumaric acid (4), chlorogenic acid (5), gallic acid (6), trans-resveratrol (7), propyl gallate (8), (+)-catechin (9), quercetin (10), and kaempferol-3-O-beta-D- galactoside (11)] have been evaluated for their in vitro inhibitory activity against phosphodiesterase- 1 (PDE-1). The active compounds 1, 5, 6, and 7 possessed IC50 values of 173.90 perpendicular to 2.58, 36.67 +/- 1.60, 325.19 +/- 3.62, and 323.81 +/- 4.25 mu M, respectively. In silico experiments were performed to elucidate the binding patterns of inhibitor molecules with the active sites of the enzymes. Result: Molecular docking studies have shown that compounds 1 and 5 have better docking results than standard inhibitor (EDTA) against the PDE-1. In conclusion, chlorogenic acid, rutin, gallic acid, and resveratrol could be promising PDE-1 inhibitors and leads to identify new drug candidates against PDE-1-associated disorders.en_US
dc.identifier.doi10.2174/1568026616666160824103615
dc.identifier.endpage417en_US
dc.identifier.issn1568-0266
dc.identifier.issn1873-4294
dc.identifier.issue4en_US
dc.identifier.pmid27558680
dc.identifier.scopus2-s2.0-85011950256
dc.identifier.scopusqualityQ2
dc.identifier.startpage412en_US
dc.identifier.urihttps://doi.org/10.2174/1568026616666160824103615
dc.identifier.urihttps://hdl.handle.net/11468/18829
dc.identifier.volume17en_US
dc.identifier.wosWOS:000392081500005
dc.identifier.wosqualityQ2
dc.indekslendigikaynakWeb of Science
dc.indekslendigikaynakScopus
dc.indekslendigikaynakPubMed
dc.language.isoenen_US
dc.publisherBentham Science Publ Ltden_US
dc.relation.ispartofCurrent Topics in Medicinal Chemistry
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.subjectPolyphenolicsen_US
dc.subjectPhosphodiesteraseen_US
dc.subjectEnzyme Inhibitionen_US
dc.subjectIn Silicoen_US
dc.subjectChlorogenic Aciden_US
dc.titleElucidation of Phosphodiesterase-1 Inhibitory Effect of Some Selected Natural Polyphenolics Using In Vitro and In Silico Methodsen_US
dc.titleElucidation of Phosphodiesterase-1 Inhibitory Effect of Some Selected Natural Polyphenolics Using In Vitro and In Silico Methods
dc.typeReview Articleen_US

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