This study aimed to compare the quality characteristics of pomegranate juice based on the extraction methods applied: centrifugal, single-gear, and twin-gear. Changes in the metabolic activities during digestion condition were further investigated. The twin-gear method was eventually identified as the optimal method, through comprehensive evaluation of the extraction rate, particle size, proximate composition, and the mineral and vitamin contents. Pomegranate juice derived using the twin-gear method had high-levels of bioactive substances such as phenolic compounds, flavonoids, anthocyanins, and selenium. Consequently, this juice exerted significant inhibitory effects on lipid peroxidation. Phenolic compounds are known to exhibit a high-correlation with skin-lightening, anti-aging, and anti-diabetic activities. An in vitro digestion model was used to evaluate changes in the antioxidant and angiotensin converting enzyme (ACE) inhibitory activities. Compared to levels observed before digestion, the results revealed a marked increase in the 2,2′azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) radical scavenging, ferric reducing antioxidant power, and superoxide dismutase-like activities as digestion progressed through the gastric phase condition, whereas most of these effects were stabilized or inhibited as digestion progressed through the intestinal phase. The ACE inhibitory activity was observed to increase after being subjected to gastric and intestinal digestion conditions. The correlation coefficients (r 2) for ACE inhibition and antioxidant activities were in the range 0.681∼0.952, thus indicating a highly positive correlation. The findings of this study indicate that the bioactivity of pomegranate juice is enhanced, as determined by the increase in various physiological activities as well as increase in the bioaccessibility and bioavailability of bioactive substances during digestion.