Chili is a spicy plant and is widely used in traditional medicine. Capsaicin and dihydrocapsaicin belong to the capsaicinoid group, which is produced from chili. This study aims to investigate the antidiabetic properties and anti-melanin synthesis of capsaicinoids by studying the inhibitory activity of capsaicin and dihydrocapsaicin with α-glucosidase, α-amylase, and tyrosinase. The results revealed that dihydrocapsaicin with IC50 had 4.13-fold and 3.00-fold for α-glucosidase and α-amylase, respectively, which are lower than capsaicin. Moreover, the IC50 of capsaicin with tyrosinase had 1.73 times less than dihydrocapsaicin. The inhibition constant (Ki ) also supported that the dihydrocapsaicin had higher inhibitory activity than capsaicin against α-glucosidase and α-amylase, but lower inhibitory activity than capsaicin on tyrosinase. Capsaicin and dihydrocapsaicin functioned in mixed-type inhibition on each enzyme, except that capsaicin functioned in competitive inhibition of tyrosinase. The results indicated that capsaicin and dihydrocapsaicin had more potent anti-melanin synthesis than antidiabetic properties. PRACTICAL APPLICATIONS: This study presents the inhibition potential of capsaicin and dihydrocapsaicin on antidiabetes and anti-melanin properties by standard methods for inhibitory activity against α-glucosidase, α-amylase, and tyrosinase. We suggest the application of these results in the development of antidiabetes and anti-melanin drugs for pharmaceutical and cosmetic industries.