l (6-甲氧基-9-氧代-9H-氧杂蒽-2-基)甲基(E)-3-(2,4-二甲氧基苯基)丙烯酸酯(K-116)的体外安全性评估--这是一种通过双发色团策略设计的新型潜在紫外线过滤器。

IF 1.3 4区 医学 Q4 PHARMACOLOGY & PHARMACY
Xenobiotica Pub Date : 2024-06-01 Epub Date: 2024-06-24 DOI:10.1080/00498254.2024.2363332
Justyna Popiół, Agnieszka Gunia-Krzyżak, Karolina Słoczyńska, Kamil Piska, Natalia Kocot, Dorota Żelaszczyk, Anna Krupa, Katarzyna Wójcik-Pszczoła, Henryk Marona, Elżbieta Pękala
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引用次数: 0

摘要

为了减少过度暴露于紫外线辐射所造成的不良影响,有必要使用局部光保护剂。尽管对紫外线过滤剂设定了很高的标准,但其中许多过滤剂可能会导致不良反应的发生。新合成的(E)-肉桂酰黄酮衍生物 K-116 可以作为一种替代品。我们对化合物 K-116 进行了广泛的体外安全性评估。研究内容包括评估对皮肤组织的潜在刺激性、评估表皮渗透性、评估光毒性和致突变性。此外,还对 K-116 化合物的生态安全性进行了评估,包括考察其在棘皮杉菌模型中的降解途径,以及对母体化合物及其降解产物的毒性进行硅模拟。研究结果表明,在未来应用条件下测试的 K-116 化合物不会穿透表皮,因此不会对皮肤产生刺激。研究结果表明,K-116 浓缩物不具有光毒性和诱变性。生态安全研究表明,K-116 浓缩物在棘皮蘑菇模型中的生物降解率为 27%。母体化合物和形成的代谢物的毒性低于参考紫外线过滤剂(辛氧酸酯和辛丙烯)。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
In vitro safety evaluation of (6-methoxy-9-oxo-9H-xanthen-2-yl)methyl (E)-3-(2,4-dimethoxyphenyl)acrylate (K-116) - the novel potential UV filter designed by means of a double chromophore strategy.

The use of topical photoprotection is necessary to reduce adverse effects caused by excessive exposure to ultraviolet radiation. Despite the high standards set for UV filters, many of them may contribute to the occurrence of adverse effects. The newly synthesised compound K-116, the (E)-cinnamoyl xanthone derivative, could be an alternative. We conducted extended in vitro safety evaluation of compound K-116. The research included assessment of irritation potential on skin tissue, evaluation of penetration through the epidermis, and assessment of phototoxicity, and mutagenicity. Additionally, the eco-safety of compound K-116 was evaluated, including an examination of its degradation pathway in the Cunninghamella echinulata model, as well as in silico simulation of the toxicity of both the parent compound and its degradation products. The research showed that compound K-116 tested in future application conditions is deprived of skin irritant potential additionally it does not penetrate through the epidermis. Results showed that K-116 concentrate is not phototoxic and not mutagenic. The eco-safety studies showed that it undergoes biodegradation in 27% in Cunninghamella echinulata model. The parent compound and formed metabolite are less toxic than reference UV filters (octinoxate and octocrylene).

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来源期刊
Xenobiotica
Xenobiotica 医学-毒理学
CiteScore
3.80
自引率
5.60%
发文量
96
审稿时长
2 months
期刊介绍: Xenobiotica covers seven main areas, including:General Xenobiochemistry, including in vitro studies concerned with the metabolism, disposition and excretion of drugs, and other xenobiotics, as well as the structure, function and regulation of associated enzymesClinical Pharmacokinetics and Metabolism, covering the pharmacokinetics and absorption, distribution, metabolism and excretion of drugs and other xenobiotics in manAnimal Pharmacokinetics and Metabolism, covering the pharmacokinetics, and absorption, distribution, metabolism and excretion of drugs and other xenobiotics in animalsPharmacogenetics, defined as the identification and functional characterisation of polymorphic genes that encode xenobiotic metabolising enzymes and transporters that may result in altered enzymatic, cellular and clinical responses to xenobioticsMolecular Toxicology, concerning the mechanisms of toxicity and the study of toxicology of xenobiotics at the molecular levelXenobiotic Transporters, concerned with all aspects of the carrier proteins involved in the movement of xenobiotics into and out of cells, and their impact on pharmacokinetic behaviour in animals and manTopics in Xenobiochemistry, in the form of reviews and commentaries are primarily intended to be a critical analysis of the issue, wherein the author offers opinions on the relevance of data or of a particular experimental approach or methodology
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