Drug Repurposing of Voglibose, a Diabetes Medication for Skin Health

Pharmaceuticals, Journal Year: 2025, Volume and Issue: 18(2), P. 224 - 224

Published: Feb. 7, 2025

Background/Objectives: Voglibose, an α-glucosidase inhibitor commonly prescribed to manage postprandial hyperglycemia in diabetes mellitus, demonstrates potential for repurposing as anti-melanogenic agent. This study aims explore the inhibitory effects of voglibose on melanogenesis and elucidate its molecular mechanisms, highlighting possible applications treating hyperpigmentation disorders. Methods: The were investigated using B16F10 melanoma cells. Cell viability, melanin content, tyrosinase activity assessed following treatment. Western blot analysis was performed examine changes melanogenic proteins transcription factors. role signaling pathways, including PKA/CREB, MAPK, PI3K/AKT, GSK3β/β-Catenin, analyzed. Primary human skin irritation tests conducted evaluate topical safety voglibose. Results: Voglibose significantly reduced synthesis cells a dose-dependent manner. revealed decreased expression MITF, TRP-1, TRP-2, indicating inhibition melanogenesis. modulated key suppression AKT activation, while restoring GSK3β inhibit β-catenin stabilization. Human confirmed voglibose’s application, showing no adverse reactions at 50 100 μM concentrations. Conclusions: properties through modulation multiple pathways biosynthesis. Its profile efficacy suggest repurposed drug managing advancing cosmeceutical applications.

Language: Английский

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Traditional Chinese Medicine as a Source of Anti-Diabetic Agents: Investigating the potential of Leptadenia reticulata and Marsdenia tenacissima roots

Pharmacological Research - Modern Chinese Medicine, Journal Year: 2025, Volume and Issue: unknown, P. 100583 - 100583

Published: Feb. 1, 2025

Language: Английский

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A glance into Schiff-based α-glucosidase inhibitors in medicinal chemistry

Medicinal Chemistry Research, Journal Year: 2025, Volume and Issue: unknown

Published: March 4, 2025

Language: Английский

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Synthesis, in vitro, and in silico studies of 7-fluorochromone based thiosemicarbazones as α-glucosidase inhibitors

Scientific Reports, Journal Year: 2025, Volume and Issue: 15(1)

Published: March 21, 2025

Increased blood sugar is a typical manifestation of Type-2 Diabetes Mellitus (T2DM), metabolic disorder that can be effectively managed with the help α-glucosidase inhibitors. A range new chromone based thiosemicarbazone derivatives (3a-t) was synthesized and assessed due to their ability suppress in this research. Having IC50 values spanning from 6.40 ± 0.15 62.81 0.79 μM, compounds demonstrated strong inhibitory actions. The compound 3 k showed most effect among all them, by an measurement µM. It concluded through structure–activity relationship (SAR) assessment various substituents on moieties had significant impact differences inhibition. Molecular docking experiments provide light important interactions, including π-π interactions hydrogen bridges, between role carbothioamide chromenyl groups ligand attachment critical residues α-glucosidase. binding alignment, stability, structural arrangement prepared molecules catalytic pocket were explored using silico strategies such as studies, pharmacokinetic analysis, molecular dynamics simulations. This investigation directed find favorable profiles for future progress potential therapeutic agents type 2 diabetes. Importantly, when benchmarking against acarbose, lead candidate substantially greater efficacy.

Language: Английский

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Design, synthesis, and investigation of novel 5-arylpyrazole-glucose hybrids as α-glucosidase inhibitors

Scientific Reports, Journal Year: 2025, Volume and Issue: 15(1)

Published: March 22, 2025

Considering the global incidence of diabetes, developing new compounds to lower blood sugar levels has become increasingly crucial. As a result, there been growing focus on synthesis α-glucosidase inhibitors in recent years. This study investigated design, synthesis, and effects novel 5-aryl pyrazole-glucose hybrids as inhibitors. Thirteen derivatives from this class were synthesized, demonstrating superior vitro inhibitory (IC50 values ranging 0.5 438.6 µM, compared acarbose at 750.0 µM). Among them, compound 8g = µM) was selected for further investigations kinetic studies revealed that it is competitive inhibitor (Ki 0.46 Fluorescence assays indicated changes fluorescence intensity, while thermodynamic analyses suggested promoted transition enzyme into an unfolded state. Furthermore, vivo demonstrated effectively reduced rats doses comparable acarbose. Molecular docking interacted with enzyme's active site, molecular dynamics simulations showed pharmacophores engaged various interactions enzyme.

Language: Английский

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Polyphenols from Rose Pepper Spice: LC-MS/MS Characterization and Therapeutic Potential in Diabetes Mellitus Management

Food Bioscience, Journal Year: 2024, Volume and Issue: unknown, P. 105644 - 105644

Published: Dec. 1, 2024

Language: Английский

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