2. Academic Validation
  3. Soybean- and Lupin-Derived Peptides Inhibit DPP-IV Activity on In Situ Human Intestinal Caco-2 Cells and Ex Vivo Human Serum

Soybean- and Lupin-Derived Peptides Inhibit DPP-IV Activity on In Situ Human Intestinal Caco-2 Cells and Ex Vivo Human Serum

  • Nutrients. 2018 Aug 13;10(8):1082. doi: 10.3390/nu10081082.
Carmen Lammi 1,  Carlotta Bollati 2,  Simonetta Ferruzza 3,  Giulia Ranaldi 4,  Yula Sambuy 5,  Anna Arnoldi 6
Affiliations

Affiliations

  • 1 Department of Pharmaceutical Sciences, University of Milan, Via Mangiagalli 25, 20133 Milan, Italy. carmen.lammi@unimi.it.
  • 2 Department of Pharmaceutical Sciences, University of Milan, Via Mangiagalli 25, 20133 Milan, Italy. carlotta.bollati@gmail.com.
  • 3 CREA-Research Centre for Food and Nutrition, Via Ardeatina 546, 00100 Rome, Italy. simonetta.ferruzza@crea.gov.it.
  • 4 CREA-Research Centre for Food and Nutrition, Via Ardeatina 546, 00100 Rome, Italy. giulia.ranaldi@crea.gov.it.
  • 5 CREA-Research Centre for Food and Nutrition, Via Ardeatina 546, 00100 Rome, Italy. yula.sambuy@crea.gov.it.
  • 6 Department of Pharmaceutical Sciences, University of Milan, Via Mangiagalli 25, 20133 Milan, Italy. anna.arnoldi@unimi.it.
PMID: 30104520 DOI: 10.3390/nu10081082
Abstract

Recent investigations have focused on food-derived Peptides as novel natural inhibitors of Dipeptidyl Peptidase IV (DPP-IV), a new target for diabetes. This study aimed to optimize fast, sensitive, and cost-effective DPP-IV assays in situ on human intestinal Caco-2 cells and ex vivo on human serum. Both assays were applied to investigate the inhibitory activity of soy and lupin Peptides. The best conditions for in situ DPP-IV activity in Caco-2 cells were obtained using 2-day cells and 50 µM Gly-Pro-AMC. Sitagliptin, used as reference inhibitor, showed a dose-dependent response with a 50% inhibition concentration (IC50) of 0.6 µM. A lower IC50 (0.2 µM) was obtained for sitagliptin on human serum incubated with the substrate for 24 h. Both assays were applied to assess the activity of Lup1 (LTFPGSAED) and Soy1 (IAVPTGVA) on DPP-IV. Lup1 and Soy1 inhibited DPP-IV in situ, with IC50 values of of 207.5 and 223.2 µM, respectively, and maintained their inhibitory activity ex vivo on circulating DPP-IV with a slightly lower potency. These assays can be used to characterize the DPP-IV inhibitory activity of food-derived molecules more accurately than in vitro biochemical tests. This combined approach also considers their effects on the circulating form of DPP-IV, correlated to metabolic diseases.

Keywords

anti-diabetic activity; bioactive peptides; dipeptidyl peptidase IV; glucose metabolism; sitagliptin.

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