具有抗氧化活性以及抑制酪氨酸酶、黑色素、透明质酸酶、弹性蛋白酶和胶原酶潜力的茜草化合物

Pharmaceuticals Pub Date : 2024-07-13 DOI:10.3390/ph17070937
L. Apaza Ticona, J. Sánchez Sánchez-Corral, Carolina Díaz-Guerra Martín, Sara Calderón Jiménez, Alejandra López González, Cristina Thiebaut Estrada
{"title":"具有抗氧化活性以及抑制酪氨酸酶、黑色素、透明质酸酶、弹性蛋白酶和胶原酶潜力的茜草化合物","authors":"L. Apaza Ticona, J. Sánchez Sánchez-Corral, Carolina Díaz-Guerra Martín, Sara Calderón Jiménez, Alejandra López González, Cristina Thiebaut Estrada","doi":"10.3390/ph17070937","DOIUrl":null,"url":null,"abstract":"In our study, using chromatographic techniques, we isolated three bioactive compounds, which were structurally elucidated as (E)-2-(3-(3,4-dimethoxyphenyl)acrylamido)-N-methylbenzamide (1), 4-Hydroxyquinoline-2-carboxylic acid (2), and (E)-2-Cyano-3-(4-hydroxyphenyl)acrylic acid (3), using spectroscopic methods. The anti-melanogenic, anti-inflammatory, antioxidant, and anti-aging properties were evaluated in vitro by measuring the activity of pharmacological targets including tyrosinase, melanin, NF-κB, hyaluronidase, elastase, collagenase, and Nrf2. Our results show that compound 1 is the most active with IC50 values of 14.19 μM (tyrosinase inhibition), 22.24 μM (melanin inhibition), 9.82–12.72 μM (NF-κB inhibition), 79.71 μM (hyaluronidase inhibition), 80.13 μM (elastase inhibition), 76.59 μM (collagenase inhibition), and 116–385 nM (Nrf2 activation) in the THP-1, HEK001, WS1, and HMCB cells. These findings underscore the promising profiles of the aqueous extract of R. urticifolius at safe cytotoxic concentrations. Additionally, we report, for the first time, the isolation and characterisation of these nitrogenous compounds in the R. urticifolius species. Finally, compound 1, isolated from R. urticifolius, is a promising candidate for the development of more effective and safer compounds for diseases related to skin pigmentation, protection against inflammation, and oxidative stress.","PeriodicalId":509865,"journal":{"name":"Pharmaceuticals","volume":null,"pages":null},"PeriodicalIF":0.0000,"publicationDate":"2024-07-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Rubus urticifolius Compounds with Antioxidant Activity, and Inhibition Potential against Tyrosinase, Melanin, Hyaluronidase, Elastase, and Collagenase\",\"authors\":\"L. Apaza Ticona, J. Sánchez Sánchez-Corral, Carolina Díaz-Guerra Martín, Sara Calderón Jiménez, Alejandra López González, Cristina Thiebaut Estrada\",\"doi\":\"10.3390/ph17070937\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"In our study, using chromatographic techniques, we isolated three bioactive compounds, which were structurally elucidated as (E)-2-(3-(3,4-dimethoxyphenyl)acrylamido)-N-methylbenzamide (1), 4-Hydroxyquinoline-2-carboxylic acid (2), and (E)-2-Cyano-3-(4-hydroxyphenyl)acrylic acid (3), using spectroscopic methods. The anti-melanogenic, anti-inflammatory, antioxidant, and anti-aging properties were evaluated in vitro by measuring the activity of pharmacological targets including tyrosinase, melanin, NF-κB, hyaluronidase, elastase, collagenase, and Nrf2. Our results show that compound 1 is the most active with IC50 values of 14.19 μM (tyrosinase inhibition), 22.24 μM (melanin inhibition), 9.82–12.72 μM (NF-κB inhibition), 79.71 μM (hyaluronidase inhibition), 80.13 μM (elastase inhibition), 76.59 μM (collagenase inhibition), and 116–385 nM (Nrf2 activation) in the THP-1, HEK001, WS1, and HMCB cells. These findings underscore the promising profiles of the aqueous extract of R. urticifolius at safe cytotoxic concentrations. Additionally, we report, for the first time, the isolation and characterisation of these nitrogenous compounds in the R. urticifolius species. Finally, compound 1, isolated from R. urticifolius, is a promising candidate for the development of more effective and safer compounds for diseases related to skin pigmentation, protection against inflammation, and oxidative stress.\",\"PeriodicalId\":509865,\"journal\":{\"name\":\"Pharmaceuticals\",\"volume\":null,\"pages\":null},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2024-07-13\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Pharmaceuticals\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.3390/ph17070937\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Pharmaceuticals","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.3390/ph17070937","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
引用次数: 0

摘要

在我们的研究中,我们利用色谱技术分离出了三种生物活性化合物,并利用光谱方法阐明了它们的结构,即(E)-2-(3-(3,4-二甲氧基苯基)丙烯酰胺基)-N-甲基苯甲酰胺(1)、4-羟基喹啉-2-羧酸(2)和(E)-2-氰基-3-(4-羟基苯基)丙烯酸(3)。通过测量药理学靶标(包括酪氨酸酶、黑色素、NF-κB、透明质酸酶、弹性蛋白酶、胶原酶和 Nrf2)的活性,在体外评估了化合物的抗黑色素生成、抗炎、抗氧化和抗衰老特性。结果表明,化合物 1 的活性最高,其 IC50 值分别为 14.19 μM(抑制酪氨酸酶)、22.24 μM(抑制黑色素)、9.82-12.72 μM(抑制 NF-κB)、79.71 μM(透明质酸酶抑制)、80.13 μM(弹性蛋白酶抑制)、76.59 μM(胶原酶抑制),以及在 THP-1、HEK001、WS1 和 HMCB 细胞中的 116-385 nM(Nrf2 激活)。这些发现强调了 R. urticifolius 水提取物在安全细胞毒性浓度下的前景。此外,我们还首次报告了这些含氮化合物在 R. urticifolius 物种中的分离和特征。最后,从 R. urticifolius 中分离出的化合物 1 有希望成为一种候选化合物,用于开发更有效、更安全的化合物,以治疗与皮肤色素沉着、炎症防护和氧化应激有关的疾病。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Rubus urticifolius Compounds with Antioxidant Activity, and Inhibition Potential against Tyrosinase, Melanin, Hyaluronidase, Elastase, and Collagenase
In our study, using chromatographic techniques, we isolated three bioactive compounds, which were structurally elucidated as (E)-2-(3-(3,4-dimethoxyphenyl)acrylamido)-N-methylbenzamide (1), 4-Hydroxyquinoline-2-carboxylic acid (2), and (E)-2-Cyano-3-(4-hydroxyphenyl)acrylic acid (3), using spectroscopic methods. The anti-melanogenic, anti-inflammatory, antioxidant, and anti-aging properties were evaluated in vitro by measuring the activity of pharmacological targets including tyrosinase, melanin, NF-κB, hyaluronidase, elastase, collagenase, and Nrf2. Our results show that compound 1 is the most active with IC50 values of 14.19 μM (tyrosinase inhibition), 22.24 μM (melanin inhibition), 9.82–12.72 μM (NF-κB inhibition), 79.71 μM (hyaluronidase inhibition), 80.13 μM (elastase inhibition), 76.59 μM (collagenase inhibition), and 116–385 nM (Nrf2 activation) in the THP-1, HEK001, WS1, and HMCB cells. These findings underscore the promising profiles of the aqueous extract of R. urticifolius at safe cytotoxic concentrations. Additionally, we report, for the first time, the isolation and characterisation of these nitrogenous compounds in the R. urticifolius species. Finally, compound 1, isolated from R. urticifolius, is a promising candidate for the development of more effective and safer compounds for diseases related to skin pigmentation, protection against inflammation, and oxidative stress.
求助全文
通过发布文献求助,成功后即可免费获取论文全文。 去求助
来源期刊
自引率
0.00%
发文量
0
×
引用
GB/T 7714-2015
复制
MLA
复制
APA
复制
导出至
BibTeX EndNote RefMan NoteFirst NoteExpress
×
提示
您的信息不完整,为了账户安全,请先补充。
现在去补充
×
提示
您因"违规操作"
具体请查看互助需知
我知道了
×
提示
确定
请完成安全验证×
copy
已复制链接
快去分享给好友吧!
我知道了
右上角分享
点击右上角分享
0
联系我们:info@booksci.cn Book学术提供免费学术资源搜索服务,方便国内外学者检索中英文文献。致力于提供最便捷和优质的服务体验。 Copyright © 2023 布克学术 All rights reserved.
京ICP备2023020795号-1
ghs 京公网安备 11010802042870号
Book学术文献互助
Book学术文献互助群
群 号:481959085
Book学术官方微信