ABSTRACT: Antarctic krill (Euphausia superba) obtained from the huge biomass in Antarctic waters is an important food product in Japan. Antarctic krill peptide powder (AKPP) prepared from the tail meat by enzymatic hydrolysis significantly decreased the systolic blood pressure in spontaneously hypertensive rats by a single oral administration (1, 10, or 100 mg). Presumably, the effect of AKPP was through inhibition of the conversion of angiotensin, which mediates blood pressure elevation, from its inactive propeptide to the mature angiotensin. Two potent angiotensin I-converting enzyme (ACE) inhibitory peptides were isolated from AKPP by high-performance liquid chromatography (HPLC) and identified as Val-Trp (IC50= 2.75 μg/mL; 12.9 μM) and Leu-Lys-Tyr (IC50= 4.26 μg/mL; 10.1 μM). Val-Trp and Leu-Lys-Tyr comprised 0.025%± 0.0023% (w/w) and 0.018%± 0.0023% (w/w) of AKPP, respectively, as measured by electrospray ionization mass spectrometry (ESI-MS). The contributions of Val-Trp and Leu-Lys-Tyr to the ACE inhibitor activity of AKPP were 17.7%± 1.60% and 8.04%± 1.03%, respectively, suggesting that these 2 peptides constitute a substantial portion of the overall ACE inhibitor potential of AKPP.