Alpha-glucosidase inhibitory and antiplasmodial properties of terpenoids from the leaves of Buddleja saligna Willd

J Enzyme Inhib Med Chem. 2016;31(1):63-6. doi: 10.3109/14756366.2014.1003927. Epub 2015 Feb 19.

Abstract

In our continuing search for biologically active natural product(s) of plant origin, Buddleja saligna, a South African medicinal plant, was screened in line with its traditional use for antidiabetic (yeast alpha glucosidase inhibitory) and antiplasmodial (against a chloroquine sensitive strain of Plasmodium falciparum (NF54)) activities. The hexane fraction showed the most promising activity with regards to its antidiabetic (IC(50) = 260 ± 0.112 µg/ml) and antiplasmodial (IC(50) = 8.5 ± 1.6 µg/ml) activities. Using activity guided fractionation three known terpenoids (betulonic acid, betulone and spinasterol) were isolated from this species for the first time. The compounds displayed varying levels of biological activities (antidiabetic: 27.31 µg/ml ≥ IC(50) ≥ 5.6 µg/ml; antiplasmodial: 14 µg/ml ≥ IC(50) ≥ 2 µg/ml) with very minimal toxicity.

Keywords: Alpha-glucosidase; Buddleja saligna; antidiabetic; antiplasmodial; terpenoids.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antimalarials / chemistry
  • Antimalarials / isolation & purification
  • Antimalarials / pharmacology*
  • Buddleja / chemistry*
  • Dose-Response Relationship, Drug
  • Glycoside Hydrolase Inhibitors / chemistry
  • Glycoside Hydrolase Inhibitors / isolation & purification
  • Glycoside Hydrolase Inhibitors / pharmacology*
  • Molecular Structure
  • Parasitic Sensitivity Tests
  • Plant Leaves / chemistry*
  • Plasmodium falciparum / drug effects*
  • Structure-Activity Relationship
  • Terpenes / chemistry
  • Terpenes / isolation & purification
  • Terpenes / pharmacology*
  • Yeasts / enzymology
  • alpha-Glucosidases / metabolism*

Substances

  • Antimalarials
  • Glycoside Hydrolase Inhibitors
  • Terpenes
  • alpha-Glucosidases