Plants Fagonia cretica L. and Hedera nepalensis K. Koch contain natural compounds with potent dipeptidyl peptidase-4 (DPP-4) inhibitory activity

Samreen Saleem, Laila Jafri, Ihsan Ul Haq, Leng Chee Chang, Danielle Calderwood, Brian D. Green, Bushra Mirza*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

85 Citations (Scopus)

Abstract

Ethnopharmacological relevance
The two plants investigated here (Fagonia cretica L. and Hedera nepalensis K. Koch) have been previously reported as natural folk medicines for the treatment of diabetes but until now no scientific investigation of potential anti-diabetic effects has been reported. 


Materials and methods
In vitro inhibitory effect of the two tested plants and their five isolated compounds on the dipeptidyl peptidase 4 (DPP-4) was studied for the assessment of anti-diabetic activity. 

Results
A crude extract of Fagonia cretica possessed good inhibitory activity (IC50value: 38.1 μg/ml) which was also present in its n-hexane (FCN), ethyl acetate (FCE) or aqueous (FCA) fractions. A crude extract of Hedera nepalensis (HNC) possessed even higher inhibitory activity (IC50value: 17.2 μg/ml) and this activity was largely retained when further fractionated in either ethyl acetate (HNE; IC50: 34.4 μg/ml) or n-hexane (HNN; 34.2 μg/ml). Bioactivity guided isolation led to the identification of four known compounds (isolated for the first time) from Fagonia cretica: quinovic acid (1), quinovic acid-3β-O-β-d-glycopyranoside (2), quinovic acid-3β-O-β-d-glucopyranosyl-(28→1)-β-d-glucopyranosyl ester (3), and stigmasterol (4) all of which inhibited DPP-4 activity (IC50: 30.7, 57.9, 23.5 and >100 μM, respectively). The fifth DPP-4 inhibitor, the triterpenoid lupeol (5) was identified in Hedera nepalensis (IC50: 31.6 μM). 

Conclusion
The experimental study revealed that Fagonia cretica and Hedera nepalensis contain compounds with significant DPP-4 inhibitory activity which should be further investigated for their anti-diabetic potential.

Original languageEnglish
Pages (from-to)26-32
Number of pages7
JournalJournal of Ethnopharmacology
Volume156
Early online date26 Aug 2014
DOIs
Publication statusPublished - 28 Oct 2014

Keywords

  • Diabetes
  • Dipeptidyl peptidase 4 (DPP-4) inhibition
  • Fagonia cretica
  • Hedera nepalensis
  • Incretin

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery

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