PDF(Pubmed)
Abstract：
In this innovative research, we aim to reveal pyrazole-based Schiff bases as new multi-target agents. In this context, we re-synthesized three sets of pyrazole-based Schiff bases, 5a-f, 6a-f, and 7a-f, to evaluate their biological applications. The data from in vitro biological assays (including antioxidant and scavenging activities, anti-diabetes, anti-Alzheimer\'s, and anti-inflammatory properties) of the pyrazole-based Schiff bases 5a-f, 6a-f, and 7a-f showed that the six pyrazole-based Schiff bases 5a, 5d, 5e, 5f, 7a, and 7f possess the highest biological properties among the compounds evaluated. The cytotoxicity against lung (A549) and colon (Caco-2) human cancer types, as well as normal lung (WI-38) cell lines, was evaluated. The data from the cytotoxicity investigation demonstrated that the three Schiff bases 5d, 5e, and 7a are active against lung (A549) cells, while the two Schiff bases 5e and 7a exhibited the highest cytotoxicity towards colon (Caco-2) cells. Additionally, the enzymatic activities against caspase-3 and Bcl-2 of the six pyrazole-based Schiff bases 5a, 5d, 5e, 5f, 7a, and 7f were evaluated. Furthermore, we assessed the in silico absorption, distribution, metabolism, and toxicity (ADMT) properties of the more potent pyrazole-based Schiff bases. After modifying the structures of the six pyrazole-based Schiff bases, we plan to further extend the studies in the future.
摘要：
在这项创新研究中，我们的目标是揭示基于吡唑的席夫碱作为新的多靶点药物。在这种情况下，我们重新合成了三组基于吡唑的席夫碱，5a-f,6a-f,7a-f，评估它们的生物学应用。来自体外生物测定的数据(包括抗氧化和清除活性，抗糖尿病,抗阿尔茨海默氏症，和抗炎特性）的吡唑基席夫碱5a-f，6a-f,和7a-f表明，六个吡唑基席夫碱5a，5d,5e,5f,7a,和7f在所评估的化合物中具有最高的生物学特性。对肺癌（A549）和结肠癌（Caco-2）的细胞毒性，以及正常肺（WI-38）细胞系，进行了评估。细胞毒性研究的数据表明，三种希夫碱5d，5e,和7a对肺（A549）细胞有活性，而两种希夫碱基5e和7a对结肠(Caco-2)细胞表现出最高的细胞毒性。此外,六种基于吡唑的席夫碱5a对caspase-3和Bcl-2的酶活性，5d,5e,5f,7a,和7f进行了评估。此外，我们评估了硅吸收，分布，新陈代谢，和毒性（ADMT）性质的更有效的吡唑基席夫碱。在修饰了六种基于吡唑的席夫碱的结构后，我们计划在未来进一步扩展研究。
