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卢布林地区植物群中的酪氨酸酶抑制剂——生物色谱法和斑马鱼模型在植物材料生物活性筛选中的应用

Tyrosinase Inhibitors Among Flora of Lubelskie Region-Application of Bio-Chromatographic Approach and Zebrafish Model in Bioactivity Screening of Plant Material.

作者信息

Kusio-Targońska Kamila, Kosheva Nataliia, Wojtanowski Krzysztof Kamil, Gaweł-Bęben Katarzyna, Beis Dimitris, Kukula-Koch Wirginia

机构信息

Department of Pharmacognosy with Medicinal Plants Garden, Medical University of Lublin, 20-093 Lublin, Poland.

Department of Experimental and Clinical Pharmacology, Medical University of Lublin, 20-090 Lublin, Poland.

出版信息

Molecules. 2025 Apr 29;30(9):1979. doi: 10.3390/molecules30091979.

DOI:10.3390/molecules30091979
PMID:40363787
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC12073248/
Abstract

The whitening potential of natural products is commonly assessed through spectrophotometric assays that colorimetrically measure the inhibitory effects on tyrosinase, a key enzyme in pigment formation. However, these assays fail to provide evidence about the input of individual components into the total activity of a mixture like plant extracts. This study introduced chromatographic methods to identify active natural products without isolating them from their mixtures. In this study, various plant extracts of differing polarities (EtOH, 50% EtOH, and HOH) from species growing in the Lubelskie region of Poland were evaluated for their ability to inhibit tyrosinase. The most active extract identified through spectrophotometric assays was a 50% EtOH extract from L. ( (L.) Rauschert). Subsequent HPLC-MS analysis allowed for the identification of several active compounds from different classes, including organic acids, glycosylated phenolics, and phenolic acids that interacted with the enzyme. The bioactivity of individual components was confirmed through classical spectrophotometric assays, highlighting ferulic acid (IC = 0.484 µM), quinic acid (IC = 22.90 µM), and citric acid (IC = 24.18 µM) as three representatives of different classes of molecules with inhibitory potential. Furthermore, the whitening capacity of the chamomile extract was investigated in a zebrafish model, demonstrating effective pigmentation inhibition in larvae and validating the proposed chromatographic approach.

摘要

天然产物的美白潜力通常通过分光光度法进行评估,该方法通过比色法测量对酪氨酸酶的抑制作用,酪氨酸酶是色素形成中的关键酶。然而,这些分析方法无法提供关于混合物(如植物提取物)中各个成分对总活性贡献的证据。本研究引入了色谱方法来鉴定活性天然产物,而无需将它们从混合物中分离出来。在本研究中,对来自波兰卢布林地区生长的不同极性(乙醇、50%乙醇和水)的各种植物提取物进行了酪氨酸酶抑制能力评估。通过分光光度法鉴定出的最具活性的提取物是来自L. ( (L.) Rauschert) 的50%乙醇提取物。随后的HPLC-MS分析鉴定出了几类不同的活性化合物,包括与该酶相互作用的有机酸、糖基化酚类和酚酸。通过经典分光光度法证实了各个成分的生物活性,突出了阿魏酸(IC = 0.484 µM)、奎尼酸(IC = 22.90 µM)和柠檬酸(IC = 24.18 µM)作为具有抑制潜力的不同类分子的三个代表。此外,在斑马鱼模型中研究了洋甘菊提取物的美白能力,证明其对幼虫有效抑制色素沉着,并验证了所提出的色谱方法。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0db5/12073248/28b3ef1844fc/molecules-30-01979-g006.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0db5/12073248/0cb43776a694/molecules-30-01979-g002.jpg
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本文引用的文献

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Naturally-Occurring Tyrosinase Inhibitors Classified by Enzyme Kinetics and Copper Chelation.天然酪氨酸酶抑制剂的酶动力学和铜螯合分类。
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采用超高效液相色谱-四极杆-轨道阱高分辨质谱法对L.的化学成分进行分析,并评估其抗哮喘活性。
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