title: The synergistic effect of maltose enhances the anti-melanogenic activity of acarbose.
abstract: Melanocytes play an important role in maintaining epidermal homeostasis by producing melanin and protecting the skin from harmful environmental factors. However, excessive up- or down-regulation of melanin production often causes hyper- or hypo-pigmented disorders, respectively, which affect the patient's quality of life. Therefore, various strategies for modulating melanin levels have been developed by the pharmaceutical and cosmetic industries. We reported previously that voglibose, which is a well-known anti-hyperglycemic agent, could be used as an anti-melanogenic agent by inhibiting α-glucosidase activity and reducing tyrosinase protein levels. Of the other representative anti-hyperglycemic agents, acarbose showed less anti-melanogenic activity despite its potent anti-hyperglycemic efficacy. In this study, we report that acarbose exhibited considerable anti-melanogenic activity when melanocytes were co-treated with acarbose and a digestible sugar, such as maltose. Simultaneous treatment with maltose augmented the inhibitory effect of acarbose on α-glucosidase activity by enhancing its stability under physiological conditions, leading to the down-regulation of tyrosinase. These results suggest that the co-treatment of anti-hyperglycemic agents with hydrolysable sugars may be a useful tool for reducing glucosidase-associated melanogenesis as a potent sugar-based anti-melanogenic regimen.
authors.affiliation: AmorePacific Corporation R&D Center, Yongin, Gyeonggi-do, 446-729, South Korea.
authors.forename: Bum-Ho
authors.initials: BH
authors.lastname: Bin
authors.affiliation: AmorePacific Corporation R&D Center, Yongin, Gyeonggi-do, 446-729, South Korea.
authors.forename: Sung Tae
authors.initials: ST
authors.lastname: Kim
authors.affiliation: Department of Chemical Engineering, POSTECH, Pohang, 790-784, South Korea.
authors.forename: Jinhyuk
authors.initials: J
authors.lastname: Bhin
authors.affiliation: AmorePacific Corporation R&D Center, Yongin, Gyeonggi-do, 446-729, South Korea.
authors.forename: Kyounghee
authors.initials: K
authors.lastname: Byoun
authors.affiliation: AmorePacific Corporation R&D Center, Yongin, Gyeonggi-do, 446-729, South Korea. trlee@amorepacific.com.
authors.forename: Tae Ryong
authors.initials: TR
authors.lastname: Lee
authors.affiliation: AmorePacific Corporation R&D Center, Yongin, Gyeonggi-do, 446-729, South Korea. egcho@amorepacific.com.
authors.forename: Eun-Gyung
authors.initials: EG
authors.lastname: Cho
mesh_terms: D020909:Acarbose / Q000494:pharmacology*; D002460:Cell Line; D004357:Drug Synergism; D065089:Glycoside Hydrolase Inhibitors / Q000494:pharmacology*; D006801:Humans; D007004:Hypoglycemic Agents / Q000494:pharmacology*; D008320:Maltose / Q000494:pharmacology*; D008543:Melanins / Q000096:biosynthesis*; D008544:Melanocytes / Q000378:metabolism; D012880:Skin Pigmentation / Q000187:drug effects*; D000520:alpha-Glucosidases / Q000378:metabolism*
chemical_list: D065089:Glycoside Hydrolase Inhibitors; D007004:Hypoglycemic Agents; D008543:Melanins; D008320:Maltose; D000520:alpha-Glucosidases; D020909:Acarbose
keywords: Acarbose; Anti-melanogenic agent; Hyper-pigmentation; Maltose; Melanin; α-Glucosidase