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替米沙坦-Cu(II)纳米粒子连接 2-嘧啶胺的抗氧化活性及其细胞毒性活性评价。

Antioxidant Activity of Telmisartan-Cu(II) Nanoparticles Connected 2-Pyrimidinamine and Their Evaluation of Cytotoxicity Activities.

机构信息

Research Department of Chemistry, Nehru Memorial College (Affiliated to Bharathidasan University), Puthanampatti, Tiruchirappalli District, 621007 Tamil Nadu, South India, India.

Department of Zoology, College of Sciences, King Saud University (KSU), P.O. Box 2455, Riyadh 11451, Saudi Arabia.

出版信息

Biomed Res Int. 2020 Nov 18;2020:8872479. doi: 10.1155/2020/8872479. eCollection 2020.

Abstract

Copper nanoparticles (Cu-Nps) are one of the promising materials for the advancement of nanoscience and technology. In this work, we synthesized telmisartan copper nanoparticles and 2-pyrimidinamines via Biginelli reaction using telmisartan copper nanoparticles (Cu-Nps) as a reusable catalyst. The synthesis of 2-pyrimidinamine derivatives (1a-c) was achieved in water and under solvent-free condition (Green chemistry approach). Synthesis of 2-pyrimidinamine with telmisartan copper nanoparticle (Cu-Nps-Pyr) unexpected product was also isolated from synthesis of 2-pyrimidinamine preparation. Antioxidant and cytotoxic activities were carried out both in 2-pyrimidinamine (1a-1c) and 2-pyrimidinamine with telmisartan copper nanoparticles (Cu-Nps-Pyr). The synthesized 2-pyrimidinamine derivatives (1a-c) were characterized from FT-IR, H and C NMR spectroscopy, mass and elemental analyses. The synthesized telmisartan copper nanoparticles (Cu-Nps) were characterized from UV spectroscopy, XRD, SEM, EDX, AFM (atomic force microscopy), profile, waviness, and roughness analyses. Antioxidant activity was screened based on ABTS radical scavenging and linoleic acid peroxidation performance. Cu-Nps-Pyr-1b showed substantial antioxidant (97.2%) activity against ABTS assay and 91.2% activity against AAPH assays compared with Trolox. Cytotoxicity was evaluated using HepG2, HeLa, and MCF-7 cell lines, the Cu-Nps-Pyr-1a is high in toxicities (GI = 0.01 m) against the HeLa cancel cell line compared with doxorubicin. The developed copper NPs with 2-pyrimidinamine (Cu-Nps-Pyr) could provide promising advances as antioxidant activities; this nanocomposition could be considered an anticancer treatment in future investigations.

摘要

铜纳米粒子(Cu-Nps)是纳米科学与技术发展的有前途的材料之一。在这项工作中,我们使用替米沙坦铜纳米粒子(Cu-Nps)作为可重复使用的催化剂,通过Biginelli 反应合成了替米沙坦铜纳米粒子和 2-嘧啶胺。在水和无溶剂条件下(绿色化学方法)合成了 2-嘧啶胺衍生物(1a-c)。从 2-嘧啶胺的合成中还分离出了意想不到的替米沙坦铜纳米粒子(Cu-Nps-Pyr)与 2-嘧啶胺的偶联产物。在 2-嘧啶胺(1a-1c)和替米沙坦铜纳米粒子(Cu-Nps-Pyr)中都进行了抗氧化和细胞毒性活性测试。合成的 2-嘧啶胺衍生物(1a-c)通过傅里叶变换红外光谱(FT-IR)、氢谱和碳谱(H 和 C NMR)光谱、质谱和元素分析进行了表征。替米沙坦铜纳米粒子(Cu-Nps)通过紫外可见光谱(UV 光谱)、X 射线衍射(XRD)、扫描电子显微镜(SEM)、能谱(EDX)、原子力显微镜(AFM)、形貌、波纹度和粗糙度分析进行了表征。抗氧化活性基于 ABTS 自由基清除和亚油酸过氧化性能进行筛选。与 Trolox 相比,Cu-Nps-Pyr-1b 在 ABTS 测定中表现出显著的抗氧化(97.2%)活性,在 AAPH 测定中表现出 91.2%的活性。使用 HepG2、HeLa 和 MCF-7 细胞系评估细胞毒性,Cu-Nps-Pyr-1a 对 HeLa 癌细胞系的毒性(GI = 0.01 μM)高于阿霉素。开发的具有 2-嘧啶胺的铜纳米粒子(Cu-Nps-Pyr)可能具有作为抗氧化剂的有前途的进展;这种纳米复合物在未来的研究中可以被认为是一种癌症治疗方法。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/af51/7688356/c94234b8e0d5/BMRI2020-8872479.001.jpg

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