a-Amylase and a-glucosidase inhibitors from Zanthoxylum chalybeum Engl, root bark

A systematic analysis of the root bark of Zanthoxylum chalybeum was conducted to establish the antidiabetic potential of isolated compounds based on its ethnomedicinal use to manage diabetes. Chromatographic separation of alkaloid extracts led to isolation of three undescribed amides, chaylbemide A...

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Bibliographic Details
Published in:Fitoterapia 2020-10, Vol.146, p.1-7
Main Authors: Ochieng, Charles O, Nyongesa, Daniel W, Yamo, Kevin O, Onyango, Joab O, Langat, Moses K
Format: Article
Language:English
Subjects:
Acarbose
Alkaloids
Amides
Amylases
Bark
Diabetes
Diabetes mellitus
Glucosidase
Glycosidases
Lignans
NMR
Nuclear magnetic resonance
Spectrometry
Triterpenoids
Zanthoxylum
α-Amylase
α-Glucosidase
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Summary:A systematic analysis of the root bark of Zanthoxylum chalybeum was conducted to establish the antidiabetic potential of isolated compounds based on its ethnomedicinal use to manage diabetes. Chromatographic separation of alkaloid extracts led to isolation of three undescribed amides, chaylbemide A (1), chalybemide B (2) and chalybemide C (3) alongside the known fagaramide (4); four known benzophenanthridine alkaloids skim-mianine (5), norchelerythrine (6), 6-acetonyldihydrochelerythrine (7) and 6-hydroxy-N-methyl decarine (8). The alkaloid free extracts yielded three known lignans, ailanthoidol (9), 2,3-epoxy-6,7-methylenedioxy coniferyl alcohol (10), sesamine (11), together with five known triterpenoids, lupeol (12), lupanone (13), 3a,20-dihy-droxy-28-lupanoic acid (14), 20-hydroxy-3-oxo-28-lupanoic acid (15) and 3a,20,28-trihydroxylupane (16). The structures of the compounds were established based on ID and 2D NMR spectroscopic and mass spectrometric experiments. Compounds 1-8 displayed inhibitory activities against both a-amylase and a-glycosidase in the range of IC50 = 43.22-49.36 pM which showed no significant (P > 0.05) difference to the positive control acarbose (IC50 = 42.67; 44.88 pM). The results confirmed anti-hyperglycemic potential of alkaloids from Z. chalybeum which lends credence to its use towards management of diabetes susceptibilities.
ISSN:0367-326X
1873-6971
DOI:10.1016/j.fitote.2020.104719