Synthesis and characterisation of steroidal inhibitors of-amylase,-glucosidase and oxidative species
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Date
2019
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Mediterranean Journal of Nutrition and Metabolism
Abstract
BACKGROUND:Management of cellular metabolism and blood glucose levels are significant in the treatment of diabetes
mellitus and oxidative diseases. Consequently, steroid and peptide hormone-based drugs such as methylprednisolone and
insulin have been the most effective and safe methods of treatment.
OBJECTIVE: Our study investigated the digestive enzymes and oxidative species inhibitory potentials of seven derived
biologically important steroids.
METHODS: Syntheses of the steroidal inhibitors (SIs) were accomplished by functional group transformations. Char
acterisation of SIs was achieved by spectroscopic techniques; followed by in-vitro enzyme and oxidative suppression
studies.
RESULTS: NMRdata revealed the presence of a steroid backbone, azomethine, carbonyl, and oxymethine peaks while the
vibrational bands were further confirmed by the FTIR. The enzyme suppression activities of the SIs were influenced by the
presence of histidine residue and free proton groups. However, the antioxidant activities were solely dependent on the free
proton groups on the steroid backbone or the number of the histidine side chain. SIs [3, 4, and 6] exhibited a potent inhibitory
effect on the enzyme activities compared to SIs [1, 2, 5, and 7], while a potent antioxidant activity was reported by SI [5].
CONCLUSIONS:Generally,SIswithhydroxyland-aminoacidfunctionalitieshaveastrongaffinityfor the enzymeactive
site than the substrate; hence, the hydrolysis of the-1,4-glycosidic bonds of saccharide was hindered. In vivo administration
of SIs [3, 4, and 6] should take into cognizance the suppression effect at doses ≤939.49 g/mL as well as the potential to
induce abnormal bacterial fermentation of undigested carbohydrates in the colon at high concentration.
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