Inhibitor of α-Glucosidase (AGH, EC 3.2.1.20). Tyr-Tyr-Pro-Leu which showed a potent inhibition against yeast AGH was selected as a skeleton peptide. As summarized five peptides were synthesized , and the AGH inhibition was determined. Substitution of Leu by Gly at the C-terminus of Tyr-Pro-Leu exhibited a similar AGH inhibition (IC50 = 5.0 mM ), whereas a 6-fold reduction of in hibition activity was observed with Tyr-Pro-Tyr (IC50 = 25.8 mM ). These results indicate that aliphatic amino acids, e.g. Leu or Gly at the C-terminus of the tri-peptide was more favorable than aromatic ones to inhibit AGH. Table 1 AGH inhibitory activity of synthetic analogues of the peptide isolated from muscle hydrolyzate a
Sequence
| IC50 (mM)
| Tyr-Tyr-Pro-Leu | 3.7 ± 0.02 | Tyr-Pro-Leu | 3.9 ± 0.02 | Pro-Leu
| No inhibition
| Tyr-Pro
| 16.8 ± 0.08
| Tyr-Pro-Gly
| 5.0 ± 0.01
| Tyr-Pro-Tyr
| 25.8 ± 0.12
| a The analogue peptides were synthesized on the basis of the sequence of Tyr-Tyr-Pro-Leu isolated from the hydrolyzate.
|