Apaza Ticona Luis, Sánchez Sánchez-Corral Javier, Díaz-Guerra Martín Carolina, Calderón Jiménez Sara, López González Alejandra, Thiebaut Estrada Cristina
Organic Chemistry Unit, Department of Chemistry in Pharmaceutical Sciences, Faculty of Pharmacy, University Complutense of Madrid, Plza. Ramón y Cajal s/n, 28040 Madrid, Spain.
Department of Organic Chemistry, Faculty of Sciences, University Autónoma of Madrid, Cantoblanco, 28049 Madrid, Spain.
Pharmaceuticals (Basel). 2024 Jul 13;17(7):937. doi: 10.3390/ph17070937.
In our study, using chromatographic techniques, we isolated three bioactive compounds, which were structurally elucidated as ()-2-(3-(3,4-dimethoxyphenyl)acrylamido)--methylbenzamide (), 4-Hydroxyquinoline-2-carboxylic acid (), and ()-2-Cyano-3-(4-hydroxyphenyl)acrylic acid (), 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 is the most active with IC 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 at safe cytotoxic concentrations. Additionally, we report, for the first time, the isolation and characterisation of these nitrogenous compounds in the species. Finally, compound , isolated from , 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.
在我们的研究中,我们使用色谱技术分离出三种生物活性化合物,通过光谱方法将其结构解析为()-2-(3-(3,4-二甲氧基苯基)丙烯酰胺基)-苯甲酰胺()、4-羟基喹啉-2-羧酸()和()-2-氰基-3-(4-羟基苯基)丙烯酸()。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、胶原酶和Nrf2在内的药理学靶点的活性,在体外评估了其抗黑色素生成、抗炎、抗氧化和抗老化特性。我们的结果表明,化合物在THP-1、HEK001、WS1和HMCB细胞中的IC值分别为14.19 μM(酪氨酸酶抑制)、22.24 μM(黑色素抑制)、9.82 - 12.72 μM(NF-κB抑制)、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)和116 - 385 nM(Nrf2激活),是活性最高的。这些发现突出了在安全细胞毒性浓度下该提取物的良好特性。此外,我们首次报道了在该物种中这些含氮化合物的分离和表征。最后,从该物种中分离出的化合物是开发用于治疗与皮肤色素沉着、抗炎和抗氧化应激相关疾病的更有效、更安全化合物的有潜力的候选物。