title: α-Glucosidase inhibition, 15-lipoxygenase inhibition, and brine shrimp toxicity of extracts and isolated compounds from Terminalia macroptera leaves.
abstract: BACKGROUND
  Terminalia macroptera Guill. & Perr. (Combretaceae), a tree that grows in West Africa, has been used in traditional medicine against a variety of diseases such as hepatitis, gonorrhea, skin diseases, and diabetes.
  
  
  OBJECTIVE
  To investigate enzyme inhibitory activity against α-glucosidase and 15-lipoxygenase (15-LO) and toxicity against brine shrimp of extracts and compounds from T. macroptera leaves.
  
  
  METHODS
  Methanol extract, ethyl acetate, and butanol extracts obtained from the methanol extract, six isolated polyphenols (chebulagic acid, chebulic acid trimethyl ester, corilagin, methyl gallate, narcissin, and rutin), and shikimic acid were evaluated for enzyme inhibition and toxicity.
  
  
  RESULTS
  In enzyme inhibition assays, all extracts showed high or very high activity. Chebulagic acid showed an IC50 value of 0.05 µM towards α-glucosidase and 24.9 ± 0.4 µM towards 15-LO, in contrast to positive controls (acarbose: IC50 201 ± 28 µM towards α-glucosidase, quercetin: 93 ± 3 µM towards 15-LO). Corilagin and narcissin were good 15-LO and α-glucosidase inhibitors, as well, while shikimic acid, methyl gallate, and chebulic acid trimethyl ester were less active or inactive. Rutin was a good α-glucosidase inhibitor (IC50 ca. 3 µM), but less active towards 15-LO. None of the extracts or the isolated compounds seemed to be very toxic in the brine shrimp assay compared with the positive control podophyllotoxin.
  
  
  CONCLUSIONS
  Inhibition of α-glucosidase in the gastrointestinal tract may be a rationale for the medicinal use of T. macroptera leaves against diabetes in traditional medicine in Mali. The plant extracts and its constituents show strong inhibition of the peroxidative enzyme 15-LO.
authors.affiliation: Section of Pharmaceutical Chemistry, School of Pharmacy, University of Oslo , Blindern, Oslo , Norway and.
authors.forename: Anh Thu
authors.initials: AT
authors.lastname: Pham
authors.forename: Karl Egil
authors.initials: KE
authors.lastname: Malterud
authors.forename: Berit Smestad
authors.initials: BS
authors.lastname: Paulsen
authors.forename: Drissa
authors.initials: D
authors.lastname: Diallo
authors.forename: Helle
authors.initials: H
authors.lastname: Wangensteen
mesh_terms: D000818:Animals; D001156:Artemia; D065089:Glycoside Hydrolase Inhibitors / Q000302:isolation & purification / Q000494:pharmacology* / Q000633:toxicity; D020128:Inhibitory Concentration 50; D016859:Lipoxygenase Inhibitors / Q000302:isolation & purification / Q000494:pharmacology* / Q000633:toxicity; D008302:Mali; D016488:Medicine, African Traditional; D010936:Plant Extracts / Q000008:administration & dosage / Q000494:pharmacology* / Q000633:toxicity; D018515:Plant Leaves; D029766:Terminalia / Q000737:chemistry*; D018675:Toxicity Tests
chemical_list: D065089:Glycoside Hydrolase Inhibitors; D016859:Lipoxygenase Inhibitors; D010936:Plant Extracts
keywords: Chebulagic acid; corilagin; diabetes; flavonoids; polyphenols; tannins