Potent In Vitro Phosphodiesterase 1 Inhibition of Flavone Isolated from Pistacia integerrima Galls

Primer Autor
Rauf, Abdur
Co-autores
Bawazeer, Sami
Herrera-Bravo, Jesus
Raza, Muslim
Naz, Humaira
Gul, Somia
Muhammad, Naveed
Almarhoon, Zainab M.
Mabkhot, Yahia N.
Ramadan, Mohamed Fawzy
Setzer, William N.
Dastan, Sevgi Durna
Mahmud, Shafi
Sharifi-Rad, Javad
Título
Potent In Vitro Phosphodiesterase 1 Inhibition of Flavone Isolated from Pistacia integerrima Galls
Editorial
HINDAWI LTD
Revista
BIOMED RESEARCH INTERNATIONAL
Lenguaje
en
Resumen
To prospect an isozyme-specific, effective inhibitor against the physiologically-crucial enzyme phosphodiesterase 1 (PDE1), phytochemicals from Pistacia integerrima galls were screened. The chloroform fraction of gall extract was subjected to column chromatographic which led to the isolation of compound 1, elucidated to be 5-hydroxy-7-methoxy-2-(4-methoxyphenyl)-4H-chromen-4-one (a flavone). In vitro and in silico PDE1 inhibitory activity of the compound 1 was investigated. EDTA, a known PDE1 inhibitor, was used as the reference. The flavone exhibited in vitro attenuation towards snake venom PDE1. IC50 response was superior to the standard chelator. An in silico molecular docking study was carried out using 3D structure of PDE1 to study the binding interactions of compound 1. The docking study predicted that flavone had a lower binding affinity (-7.6 kcal/mol) and total energy (-95 kcal/mol) score compared to EDTA. The minimal energy associated with the ligand-protein complex implied that isolated compound 1 can serve as a therapeutic agent against PDE1 enzyme-provoked ailments like asthma, hypertension, schizophrenia, and erectile dysfunction.
Tipo de Recurso
artículo original
doi
10.1155/2022/6116003
Formato Recurso
PDF
Palabras Claves
PISTAGREMIC ACID
ANTIOXIDANT
EXTRACT
DOCKING
UPDATE
LEAVES
VENOM
Ubicación del archivo
http://dx.doi.org/10.1155/2022/6116003
Categoría OCDE
Biotecnología y Microbiología Aplicada
Medicina
Investigación y Experimental
Materias
ÁCIDO PISTAGRÁMICO
ANTIOXIDANTE
EXTRACTO
DOCKING
ACTUALIZACIÓN
HOJAS
VENENO
Disciplinas de la OCDE
Bioquímica
Farmacología y Farmacia
Otros Temas de Medicina Básica
Título de la cita (Recomendado-único)
Potent In Vitro Phosphodiesterase 1 Inhibition of Flavone Isolated from Pistacia integerrima Galls
Identificador del recurso (Mandatado-único)
artículo original
Versión del recurso (Recomendado-único)
version publicada
License
CC BY 4.0
Condición de la licencia (Recomendado-repetible)
CC BY 4.0
Derechos de acceso
acceso abierto
Access Rights
acceso abierto
Id de Web of Science
WOS:000810504800004
Colecciones
Colección Publicaciones Científicas
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