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Molecular Scaffolds Design and Biomedical Applications

A special issue of Molecules (ISSN 1420-3049).

Deadline for manuscript submissions: 30 November 2024 | Viewed by 1031

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Guest Editor
Department of Chemistry and Nano Science, Ewha Womans University, Seodaemun-gu, Seoul 120-750, Republic of Korea
Interests: smart materials; thermogel; tissue engineering; scaffolds; stem cell differentiation; biomedical applications
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Special Issue Information

Dear Colleagues,

Molecular scaffold design is a crucial strategy in biomedical research that offers a world of possibilities. These scaffolds can be customized to meet the specific needs of varied biomedical challenges via rational design principles, including structural optimization and functionalization with targeting ligands or therapeutic payloads. This enables the creation of custom structures with specific functions for various applications. These molecular scaffolds mimic the structure and characteristics of the extracellular matrix, providing an environment that is conducive to cell adhesion, proliferation, and differentiation. The properties of molecular scaffolds, including their mechanical strength, rate of degradation, and bioactivity, can be customized to enable their use in diverse biomedical applications, such as regenerative medicine, drug delivery, and tissue engineering.

Prof. Dr. Madhumita Patel
Guest Editor

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Keywords

  • molecular scaffolds
  • smart materials
  • biodegradation
  • drug release
  • tissue engineering
  • surface’s modifications

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Published Papers (1 paper)

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Research

24 pages, 13306 KiB  
Article
Exploration of Compounds with 2-Phenylbenzo[d]oxazole Scaffold as Potential Skin-Lightening Agents through Inhibition of Melanin Biosynthesis and Tyrosinase Activity
by Hee Jin Jung, Hyeon Seo Park, Hye Soo Park, Hye Jin Kim, Dahye Yoon, Yujin Park, Pusoon Chun, Hae Young Chung and Hyung Ryong Moon
Molecules 2024, 29(17), 4162; https://doi.org/10.3390/molecules29174162 - 2 Sep 2024
Viewed by 864
Abstract
Inspired by the potent tyrosinase inhibitory activity of phenolic compounds with a 2-phenylbenzo[d]thiazole scaffold, we explored phenolic compounds 115 with 2-phenylbenzo[d]oxazole, which is isosterically related to 2-phenylbenzo[d]thiazole, as novel tyrosinase inhibitors. Among these, compounds 3 [...] Read more.
Inspired by the potent tyrosinase inhibitory activity of phenolic compounds with a 2-phenylbenzo[d]thiazole scaffold, we explored phenolic compounds 115 with 2-phenylbenzo[d]oxazole, which is isosterically related to 2-phenylbenzo[d]thiazole, as novel tyrosinase inhibitors. Among these, compounds 3, 8, and 13, featuring a resorcinol structure, exhibited significantly stronger mushroom tyrosinase inhibition than kojic acid, with compound 3 showing a nanomolar IC50 value of 0.51 μM. These results suggest that resorcinol plays an important role in tyrosinase inhibition. Kinetic studies using Lineweaver–Burk plots demonstrated the inhibition mechanisms of compounds 3, 8, and 13, while docking simulation results indicated that the resorcinol structure contributed to tyrosinase binding through hydrophobic and hydrogen bonding interactions. Additionally, these compounds effectively inhibited tyrosinase activity and melanin production in B16F10 cells and inhibited B16F10 tyrosinase activity in situ in a concentration-dependent manner. As these compounds showed no cytotoxicity to epidermal cells, melanocytes, or keratinocytes, they are appropriate for skin applications. Compounds 8 and 13 demonstrated substantially higher depigmentation effects on zebrafish larvae than kojic acid, even at 800- and 400-times lower concentrations than kojic acid, respectively. These findings suggest that 2-phenylbenzo[d]oxazole is a promising candidate for tyrosinase inhibition. Full article
(This article belongs to the Special Issue Molecular Scaffolds Design and Biomedical Applications)
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