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过硫酸氢钾复合盐作为一种安全稳定的维生素 C 衍生物，可应用于护肤领域。

Persulfated Ascorbic Acid Glycoside as a Safe and Stable Derivative of Ascorbic Acid for Skin Care Application.

机构信息

Associate Laboratory i4HB-Institute for Health and Bioeconomy, University of Porto, 4050-313 Porto, Portugal.

UCIBIO-Applied Molecular Biosciences Unit, Laboratory of Pharmaceutical Technology, Faculty of Pharmacy, University of Porto, 4050-313 Porto, Portugal.

出版信息

Molecules. 2024 Sep 27;29(19):4604. doi: 10.3390/molecules29194604.

DOI:10.3390/molecules29194604
PMID:39407535
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11477482/
Abstract

The pursuit of cosmetic ingredients with proven efficacy and safety that meet consumer needs drives the advancement of new products. Ascorbic acid (AA) is utilized in cosmetic products, predominantly for its potent antioxidant properties. Nonetheless, its instability compromises its efficacy. In this work, ascorbyl 2--glucoside persulfate (AAGS) was synthesized, characterized, and evaluated regarding its safety profile and potential bioactivities and the results were compared to AA and its glycoside AAG. Pre-formulation studies were performed to assess the stability of the compounds and their compatibility with typical excipients commonly used in topical formulations. AAGS did not affect the metabolic activity of keratinocyte, macrophage, and monocyte cell lines, up to 500 µM. AAGS also exhibited a non-prooxidant and non-sensitizing profile and anti-allergic activity by impeding the allergen-induced maturation of THP-1 cells. When compared to AA and AAG, AAGS was shown to be more stable at pH values between 5 and 7, as well as superior thermostability and photostability. AAGS demonstrated higher stability in metal solutions of Fe(II) and Mg(II) than AA. AAGS demonstrated similar DPPH radical scavenging activity compared to AA. These results provide useful information for the development of new AA derivatives, highlighting AAGS as a novel cosmetic ingredient.

摘要

追求具有功效和安全性的美容成分，以满足消费者的需求，推动了新产品的研发。抗坏血酸（AA）被广泛应用于化妆品中，主要因其具有强大的抗氧化性能。然而，其不稳定性限制了其功效。本研究合成、表征了抗坏血酸 2--葡萄糖苷过硫酸盐（AAGS），并评估了其安全性、潜在生物活性，将结果与 AA 及其糖苷 AAG 进行了比较。通过预配方研究评估了化合物的稳定性及其与常用的局部制剂赋形剂的相容性。在高达 500µM 的浓度下，AAGS 不会影响角质形成细胞、巨噬细胞和单核细胞系的代谢活性。AAGS 还表现出非促氧化剂和非致敏特性，并通过阻碍变应原诱导的 THP-1 细胞成熟来表现出抗过敏活性。与 AA 和 AAG 相比，AAGS 在 pH 值为 5 到 7 之间更稳定，热稳定性和光稳定性更好。AAGS 在 Fe(II)和 Mg(II)的金属溶液中比 AA 更稳定。AAGS 对 DPPH 自由基的清除活性与 AA 相当。这些结果为新型 AA 衍生物的开发提供了有用的信息，突出了 AAGS 作为一种新型的化妆品成分。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8b10/11477482/6b311f5b8467/molecules-29-04604-g010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8b10/11477482/e4d091f8236a/molecules-29-04604-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8b10/11477482/50655c170f3f/molecules-29-04604-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8b10/11477482/75bdbf17e8c3/molecules-29-04604-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8b10/11477482/1eb0653407db/molecules-29-04604-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8b10/11477482/af76fcebb127/molecules-29-04604-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8b10/11477482/ada12377edcd/molecules-29-04604-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8b10/11477482/f7811bb5e4ae/molecules-29-04604-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8b10/11477482/ee9b4b931cff/molecules-29-04604-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8b10/11477482/3cf83ccffa79/molecules-29-04604-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8b10/11477482/6b311f5b8467/molecules-29-04604-g010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8b10/11477482/e4d091f8236a/molecules-29-04604-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8b10/11477482/50655c170f3f/molecules-29-04604-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8b10/11477482/75bdbf17e8c3/molecules-29-04604-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8b10/11477482/1eb0653407db/molecules-29-04604-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8b10/11477482/af76fcebb127/molecules-29-04604-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8b10/11477482/ada12377edcd/molecules-29-04604-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8b10/11477482/f7811bb5e4ae/molecules-29-04604-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8b10/11477482/ee9b4b931cff/molecules-29-04604-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8b10/11477482/3cf83ccffa79/molecules-29-04604-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8b10/11477482/6b311f5b8467/molecules-29-04604-g010.jpg

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