Justyna Popiół, Agnieszka Gunia-Krzyżak, Karolina Słoczyńska, Kamil Piska, Natalia Kocot, Dorota Żelaszczyk, Anna Krupa, Katarzyna Wójcik-Pszczoła, Henryk Marona, Elżbieta Pękala
{"title":"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。","authors":"Justyna Popiół, Agnieszka Gunia-Krzyżak, Karolina Słoczyńska, Kamil Piska, Natalia Kocot, Dorota Żelaszczyk, Anna Krupa, Katarzyna Wójcik-Pszczoła, Henryk Marona, Elżbieta Pękala","doi":"10.1080/00498254.2024.2363332","DOIUrl":null,"url":null,"abstract":"<p><p>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 (<i>E</i>)-cinnamoyl xanthone derivative, could be an alternative. We conducted extended <i>in vitro</i> 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 <i>Cunninghamella echinulata</i> model, as well as <i>in silico</i> 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 <i>Cunninghamella echinulata</i> model. The parent compound and formed metabolite are less toxic than reference UV filters (octinoxate and octocrylene).</p>","PeriodicalId":23812,"journal":{"name":"Xenobiotica","volume":" ","pages":"266-278"},"PeriodicalIF":1.3000,"publicationDate":"2024-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"<i>In vitro</i> safety evaluation of (6-methoxy-9-oxo-9<i>H</i>-xanthen-2-yl)methyl (<i>E</i>)-3-(2,4-dimethoxyphenyl)acrylate (K-116) - the novel potential UV filter designed by means of a double chromophore strategy.\",\"authors\":\"Justyna Popiół, Agnieszka Gunia-Krzyżak, Karolina Słoczyńska, Kamil Piska, Natalia Kocot, Dorota Żelaszczyk, Anna Krupa, Katarzyna Wójcik-Pszczoła, Henryk Marona, Elżbieta Pękala\",\"doi\":\"10.1080/00498254.2024.2363332\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p>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 (<i>E</i>)-cinnamoyl xanthone derivative, could be an alternative. We conducted extended <i>in vitro</i> 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 <i>Cunninghamella echinulata</i> model, as well as <i>in silico</i> 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 <i>Cunninghamella echinulata</i> model. The parent compound and formed metabolite are less toxic than reference UV filters (octinoxate and octocrylene).</p>\",\"PeriodicalId\":23812,\"journal\":{\"name\":\"Xenobiotica\",\"volume\":\" \",\"pages\":\"266-278\"},\"PeriodicalIF\":1.3000,\"publicationDate\":\"2024-06-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Xenobiotica\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://doi.org/10.1080/00498254.2024.2363332\",\"RegionNum\":4,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"2024/6/24 0:00:00\",\"PubModel\":\"Epub\",\"JCR\":\"Q4\",\"JCRName\":\"PHARMACOLOGY & PHARMACY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Xenobiotica","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.1080/00498254.2024.2363332","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"2024/6/24 0:00:00","PubModel":"Epub","JCR":"Q4","JCRName":"PHARMACOLOGY & PHARMACY","Score":null,"Total":0}
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).
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