Cycloartenyl ferulate is a derivative of γ-oryzanol with varied biological activity, including diabetes mellitus treatment. This research focused on improving the cycloartenyl ferulate accumulation in germinated rice by gamma irradiation under saline conditions. Moreover, the inhibitory potential of cycloartenyl ferulate against carbohydrate hydrolysis enzymes (α-glucosidase and α-amylase) was investigated through in vitro and in silico techniques. The results revealed that cycloartenyl ferulate increased in germinated rice under saline conditions upon gamma irradiation. A suitable condition for stimulating the highest cycloartenyl ferulate concentration (852.20±20.59 μg/g) in germinated rice was obtained from the gamma dose at 100 Gy and under 40 mM salt concentration. The inhibitory potential of cycloartenyl ferulate against α-glucosidase (31.31±1.43%) was higher than against α-amylase (12.72±1.11%). The inhibition mode of cycloartenyl ferulate against α-glucosidase was demonstrated as a mixed-type inhibition. A fluorescence study confirmed that the cycloartenyl ferulate interacted with the α-glucosidase's active site. A docking study revealed that cycloartenyl ferulate bound to seven amino acids of α-glucosidase with a binding energy of -8.8 kcal/mol and a higher binding potential than α-amylase (-8.2 kcal/mol). The results suggested that the gamma irradiation technique under saline conditions is suitable for stimulating γ-oryzanol, especially cycloartenyl ferulate. Furthermore, cycloartenyl ferulate demonstrated its potential as a candidate compound for blood glucose management in diabetes mellitus treatment.