PDF(Pubmed)
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.
摘要：
在我们的研究中,使用色谱技术，我们分离出三种生物活性化合物,在结构上阐明为（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），使用光谱学方法。抗黑色素生成，抗炎,抗氧化剂，和抗衰老特性在体外通过测量包括酪氨酸酶，黑色素,NF-κB,透明质酸酶，弹性蛋白酶,胶原酶,Nrf2我们的结果表明，化合物1是最有活性的，IC50值为14.19μM（酪氨酸酶抑制），22.24μM（黑色素抑制），9.82-12.72μM（NF-κB抑制），79.71μM（透明质酸酶抑制），80.13μM（弹性蛋白酶抑制），76.59μM（胶原酶抑制），在THP-1、HEK001、WS1和HMCB细胞中和116-385nM(Nrf2激活)。这些发现强调了在安全的细胞毒性浓度下杀尿叶的水提取物的有希望的概况。此外,我们报告,第一次,这些含氮化合物在R.urtifolius物种中的分离和表征。最后,化合物1，分离自R.urticifolius，是开发与皮肤色素沉着相关的疾病的更有效和更安全的化合物的有希望的候选人，防止炎症，和氧化应激。
