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In vitro and in silico studies reveal antidiabetic properties of arylbenzofurans from the root bark of Morus mesozygia Stapf.
Olufolabo, Katherine Olabanjo; Lüersen, Kai; Oguntimehin, Samuel Ayoolu; Nchiozem-Ngnitedem, Vaderament-A; Agbebi, Emmanuel Ayodeji; Faloye, Kolade Olatubosun; Nyamboki, Divinah Kwamboka; Rimbach, Gerald; Matasyoh, Josphat Clement; Schmidt, Bernd; Moody, Jones Olanrewaju.
Afiliación
  • Olufolabo KO; Department of Pharmacognosy, Faculty of Pharmacy, Olabisi Onabanjo University, Ago-Iwoye, Nigeria.
  • Lüersen K; Department of Pharmacognosy, Faculty of Pharmacy, University of Ibadan, Ibadan, Nigeria.
  • Oguntimehin SA; Institute of Human Nutrition and Food Science, University of Kiel, Kiel, Germany.
  • Nchiozem-Ngnitedem VA; Department of Pharmacognosy, Faculty of Pharmacy, University of Ibadan, Ibadan, Nigeria.
  • Agbebi EA; Institut für Chemie, University of Potsdam, Potsdam, Germany.
  • Faloye KO; Department of Pharmacognosy and Natural Products, College of Pharmacy, Afe Babalola University, Ado-Ekiti, Nigeria.
  • Nyamboki DK; Department of Chemistry, Faculty of Science, Obafemi Awolowo University, Ile Ife, Nigeria.
  • Rimbach G; Department of Chemistry, Faculty of Sciences, Egerton University, Egerton, Kenya.
  • Matasyoh JC; Institute of Human Nutrition and Food Science, University of Kiel, Kiel, Germany.
  • Schmidt B; Department of Chemistry, Faculty of Sciences, Egerton University, Egerton, Kenya.
  • Moody JO; Institut für Chemie, University of Potsdam, Potsdam, Germany.
Front Pharmacol ; 15: 1338333, 2024.
Article en En | MEDLINE | ID: mdl-38482058
ABSTRACT
Diabetes remains an important disease worldwide with about 500 million patients globally. In tropical Africa, Morus mesozygia is traditionally used in the treatment of diabetes. Biological and phytochemical investigation of the root bark extracts of the plant led to the isolation of a new prenylated arylbenzofuran named 7-(3-hydroxy-3-methylbutyl)moracin M (1) and two congeners, moracins P (2) and M (3). When compared to acarbose (IC50 = 486 µM), all the isolated compounds are better inhibitors of α-glucosidase with in vitro IC50 values of 16.9, 16.6, and 40.9 µM, respectively. However, they were not active against α-amylase. The compounds also demonstrated moderate inhibition of dipeptidyl peptidase-4 (DPP4). Based on in silico docking studies, all isolates (1, 2, and 3) exhibit binding affinities of -8.7, -9.5, and -8.5 kcal/mol, respectively against α-glucosidase enzyme (PDB 3AJ7). They are stabilized within the α-glucosidase active site through hydrogen bonds, pi interactions, and hydrophobic interactions. This study provides scientific support for the traditional use of Morus mesozygia in the treatment of diabetes as well as adding to the repository of α-glucosidase inhibitory agents.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Idioma: En Revista: Front Pharmacol Año: 2024 Tipo del documento: Article País de afiliación: Nigeria Pais de publicación: Suiza

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Idioma: En Revista: Front Pharmacol Año: 2024 Tipo del documento: Article País de afiliación: Nigeria Pais de publicación: Suiza