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Title: Concise synthesis of a new triterpenoid saponin from the roots of : gypsophila oldhamiana and its derivatives as α-glucosidase inhibitors
Authors: Liu, Q
Guo, T
Li, F
Li, D
Issue Date: 2016
Publisher: Royal Society of Chemistry
Source: New journal of chemistry, 2016, v. 40, no. 11, p. 9537-9549 How to cite?
Journal: New journal of chemistry 
Abstract: The first synthesis of the triterpenoid saponin 1 and its derivatives 2-3 was efficiently achieved in an efficient and practical strategy with an odourless 2-methyl-5-tert-butylphenyl (Mbp) thioglycoside and a N-phenyltrifluoroacetimidate donor as a key step, and their inhibitory activities against α-glucosidase and α-amylase were evaluated in vitro. The preliminary structure-activity relationship studies demonstrated that C4-CHO and C4-CH2OH were not essential to α-glucosidase inhibitory activity. Among the three compounds, compound 3 exhibited remarkably potent inhibitory activity against α-glucosidase with an IC50 value of 9.17 μM. According to Ki determined at 9.35 μM from the intercept on a Dixon plot, the more potent saponin 3 against α-glucosidase may be a noncompetitive inhibition pattern. In parallel, the lipophilicity of compounds 1-3 was calculated as a prediction for pharmacological potency. According to the predicted logP values, lipophilicity may correlate with the evaluated biological potency.
ISSN: 1144-0546
DOI: 10.1039/c6nj01602b
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