Inhibition of alpha-glucosidase by synthetic derivatives of lupane, oleanane, ursane and dammarane triterpenoids

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Abstract

A variety of new and earlier synthesized lupane, oleanane, ursane and dammarane triterpenoids have been investigated for their inhibitory activity against α-glucosidase. 2,3-Indole-21β-acetyl-20β,28-epoxy-18α,19β.-ursane and 3-oxo-3A-homo-3a-aza-20(S)-hydroxydammar-24(25)-ene were synthesized for the first time. The compounds 3, 4, 8-11 and 14 demonstrated strong in vitro inhibitory activity towards α-glucosidase with IC50 values of 37.5-115.1 μgM. 3-Deoxy-3a-homo-3a-aza-28-cinnamoyloxy-20(29)-lupene, with an IC50 of 6.67 μgM was 60-fold more active than the market drug acarbose.

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Khusnutdinova, E. F., Smirnova, I. E., Giniyatullina, G. V., Medvedeva, N. I., Yamansarov, E. Y., Kazakov, D. V., … Huong, D. T. (2016). Inhibition of alpha-glucosidase by synthetic derivatives of lupane, oleanane, ursane and dammarane triterpenoids. Natural Product Communications, 11(1), 33–35. https://doi.org/10.1177/1934578x1601100112

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