TY - JOUR
T1 - Giganteone A and malabaricone C as potential pharmacotherapy for diabetes mellitus
AU - Sivasothy, Yasodha
AU - Leong, Kok Hoong
AU - Loo, Kong Yong
AU - Adbul Wahab, Siti Mariam
AU - Othman, Muhamad Aqmal
AU - Awang, Khalijah
N1 - Funding Information:
The authors acknowledge the Ministry of Higher Education, Malaysia for the Fundamental Research Grant FP002-2018A and University of Malaya for providing the University Research Grants RP001-2012 and BK002-2015 which have made this work possible.
Publisher Copyright:
© 2021 Informa UK Limited, trading as Taylor & Francis Group.
Copyright:
Copyright 2021 Elsevier B.V., All rights reserved.
PY - 2022/3/19
Y1 - 2022/3/19
N2 - The use of antidiabetic agents which control glycemic levels in the blood and simultaneously inhibit oxidative stress is an important strategy in the prevention of Diabetes Mellitus and its complications. In our previous study, malabaricone C (3) and its dimer, giganteone A (5) exhibited significant DPPH free radical scavenging activities which were lower than the activity of the positive control, ascorbic acid. These compounds were evaluated for their α-glucosidase inhibitory activities at different concentrations (0.02–2.5 mM) in the present study. Compounds 3 (IC50 59.61 µM) and 5 (IC50 39.52 µM) were identified as active alpha-glucosidase inhibitors, each respectively being 24 and 37 folds more potent than the standard inhibitor, acarbose. Based on the molecular docking studies, compounds 3 and 5 docked into the active site of the α-glucosidase enzyme, forming mainly hydrogen bonds in the active site.
AB - The use of antidiabetic agents which control glycemic levels in the blood and simultaneously inhibit oxidative stress is an important strategy in the prevention of Diabetes Mellitus and its complications. In our previous study, malabaricone C (3) and its dimer, giganteone A (5) exhibited significant DPPH free radical scavenging activities which were lower than the activity of the positive control, ascorbic acid. These compounds were evaluated for their α-glucosidase inhibitory activities at different concentrations (0.02–2.5 mM) in the present study. Compounds 3 (IC50 59.61 µM) and 5 (IC50 39.52 µM) were identified as active alpha-glucosidase inhibitors, each respectively being 24 and 37 folds more potent than the standard inhibitor, acarbose. Based on the molecular docking studies, compounds 3 and 5 docked into the active site of the α-glucosidase enzyme, forming mainly hydrogen bonds in the active site.
KW - giganteone A
KW - malabaricone C
KW - malabaricone E
KW - Myristica cinnamomea King
KW - α-glucosidase inhibitory activity
UR - http://www.scopus.com/inward/record.url?scp=85101032573&partnerID=8YFLogxK
U2 - 10.1080/14786419.2021.1885405
DO - 10.1080/14786419.2021.1885405
M3 - Article
C2 - 33593208
AN - SCOPUS:85101032573
SN - 1478-6419
VL - 36
SP - 1581
EP - 1586
JO - Natural Product Research
JF - Natural Product Research
IS - 6
ER -
