Drug Repurposing of Voglibose, a Diabetes Medication for Skin Health
<b>Background/Objectives:</b> Voglibose, an α-glucosidase inhibitor commonly prescribed to manage postprandial hyperglycemia in diabetes mellitus, demonstrates potential for repurposing as an anti-melanogenic agent. This study aims to explore the inhibitory effects of voglibose on melano...
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MDPI AG
2025-02-01
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| author | Hyeon-Mi Kim Chang-Gu Hyun |
| author_facet | Hyeon-Mi Kim Chang-Gu Hyun |
| author_sort | Hyeon-Mi Kim |
| collection | DOAJ |
| description | <b>Background/Objectives:</b> Voglibose, an α-glucosidase inhibitor commonly prescribed to manage postprandial hyperglycemia in diabetes mellitus, demonstrates potential for repurposing as an anti-melanogenic agent. This study aims to explore the inhibitory effects of voglibose on melanogenesis and elucidate its molecular mechanisms, highlighting its possible applications in treating hyperpigmentation disorders. <b>Methods:</b> The anti-melanogenic effects of voglibose were investigated using B16F10 melanoma cells. Cell viability, melanin content, and tyrosinase activity were assessed following voglibose treatment. Western blot analysis was performed to examine changes in melanogenic proteins and transcription factors. The role of signaling pathways, including PKA/CREB, MAPK, PI3K/AKT, and GSK3β/β-Catenin, was analyzed. Primary human skin irritation tests were conducted to evaluate the topical safety of voglibose. <b>Results:</b> Voglibose significantly reduced melanin synthesis and tyrosinase activity in B16F10 cells in a dose-dependent manner. Western blot analysis revealed decreased expression of MITF, TRP-1, and TRP-2, indicating the inhibition of melanogenesis. Voglibose modulated key signaling pathways, including the suppression of PKA/CREB, MAPK, and AKT activation, while restoring GSK3β activity to inhibit β-catenin stabilization. Human skin irritation tests confirmed voglibose’s safety for topical application, showing no adverse reactions at 50 and 100 μM concentrations. <b>Conclusions:</b> Voglibose demonstrates anti-melanogenic properties through the modulation of multiple signaling pathways and the inhibition of melanin biosynthesis. Its safety profile and efficacy suggest its potential as a repurposed drug for managing hyperpigmentation and advancing cosmeceutical applications. |
| format | Article |
| id | doaj-art-5985758799bc419c88c3a3baa64dcf67 |
| institution | DOAJ |
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| spelling | doaj-art-5985758799bc419c88c3a3baa64dcf672025-08-20T03:12:12ZengMDPI AGPharmaceuticals1424-82472025-02-0118222410.3390/ph18020224Drug Repurposing of Voglibose, a Diabetes Medication for Skin HealthHyeon-Mi Kim0Chang-Gu Hyun1Jeju Inside Agency and Cosmetic Science Center, Department of Chemistry and Cosmetics, Jeju National University, Jeju 63243, Republic of KoreaJeju Inside Agency and Cosmetic Science Center, Department of Chemistry and Cosmetics, Jeju National University, Jeju 63243, Republic of Korea<b>Background/Objectives:</b> Voglibose, an α-glucosidase inhibitor commonly prescribed to manage postprandial hyperglycemia in diabetes mellitus, demonstrates potential for repurposing as an anti-melanogenic agent. This study aims to explore the inhibitory effects of voglibose on melanogenesis and elucidate its molecular mechanisms, highlighting its possible applications in treating hyperpigmentation disorders. <b>Methods:</b> The anti-melanogenic effects of voglibose were investigated using B16F10 melanoma cells. Cell viability, melanin content, and tyrosinase activity were assessed following voglibose treatment. Western blot analysis was performed to examine changes in melanogenic proteins and transcription factors. The role of signaling pathways, including PKA/CREB, MAPK, PI3K/AKT, and GSK3β/β-Catenin, was analyzed. Primary human skin irritation tests were conducted to evaluate the topical safety of voglibose. <b>Results:</b> Voglibose significantly reduced melanin synthesis and tyrosinase activity in B16F10 cells in a dose-dependent manner. Western blot analysis revealed decreased expression of MITF, TRP-1, and TRP-2, indicating the inhibition of melanogenesis. Voglibose modulated key signaling pathways, including the suppression of PKA/CREB, MAPK, and AKT activation, while restoring GSK3β activity to inhibit β-catenin stabilization. Human skin irritation tests confirmed voglibose’s safety for topical application, showing no adverse reactions at 50 and 100 μM concentrations. <b>Conclusions:</b> Voglibose demonstrates anti-melanogenic properties through the modulation of multiple signaling pathways and the inhibition of melanin biosynthesis. Its safety profile and efficacy suggest its potential as a repurposed drug for managing hyperpigmentation and advancing cosmeceutical applications.https://www.mdpi.com/1424-8247/18/2/224B16F10drug repurposingmelanogenesissignaling pathwaysvoglibose |
| spellingShingle | Hyeon-Mi Kim Chang-Gu Hyun Drug Repurposing of Voglibose, a Diabetes Medication for Skin Health Pharmaceuticals B16F10 drug repurposing melanogenesis signaling pathways voglibose |
| title | Drug Repurposing of Voglibose, a Diabetes Medication for Skin Health |
| title_full | Drug Repurposing of Voglibose, a Diabetes Medication for Skin Health |
| title_fullStr | Drug Repurposing of Voglibose, a Diabetes Medication for Skin Health |
| title_full_unstemmed | Drug Repurposing of Voglibose, a Diabetes Medication for Skin Health |
| title_short | Drug Repurposing of Voglibose, a Diabetes Medication for Skin Health |
| title_sort | drug repurposing of voglibose a diabetes medication for skin health |
| topic | B16F10 drug repurposing melanogenesis signaling pathways voglibose |
| url | https://www.mdpi.com/1424-8247/18/2/224 |
| work_keys_str_mv | AT hyeonmikim drugrepurposingofvogliboseadiabetesmedicationforskinhealth AT changguhyun drugrepurposingofvogliboseadiabetesmedicationforskinhealth |