Colloidal gold nanoparticle conjugates of gefitinib
Colloidal gold nanoparticle conjugates of gefitinib
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DOI：
10.1016/j.colsurfb.2014.08.021
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发表时间：
2014-11-01
影响因子：
5.8
通讯作者：
Joo, Sang-Woo
中科院分区：
文献类型：
--
作者：
Anh Thu Ngoc Lam;Yoon, Jinha;Joo, Sang-Woo
吉非替尼（Gefitinib，GF）是美国食品药品监督管理局批准的用于治疗肺癌的表皮生长因子受体（EGFR）酪氨酸激酶抑制剂。我们通过自组装制备了GF抗癌药物的胶体金纳米颗粒（AuNP）缀合物，以测试其对A549，NCI-H460和NCI-H1975肺癌细胞的效力。通过紫外维斯吸收光谱和表面增强拉曼散射研究了GF在金纳米粒子表面的吸附。进行密度泛函理论计算以估计药物-金纳米粒子复合物的能量稳定性。计算结果表明，GF中喹唑啉环的N1氮原子比N3氮原子更稳定地与Au原子簇结合。通过透射电子显微镜和暗视野显微镜检查GF涂覆的金纳米颗粒的内化。在处理48小时后，对于A549、NCI-H460和NCI-H1975肺癌细胞，具有EGFR抗体的AuNP GF缀合物的细胞活力测试显示出比游离GF高得多的减少。(C)2014爱思唯尔有限公司版权所有。
Gefitinib (GF) is a US Food and Drug Administration-approved epidermal growth factor receptor (EGFR)tyrosine kinase inhibitor for treating the lung cancers. We fabricated colloidal gold nanoparticle (AuNP) conjugates of the GF anticancer drug by self-assembly to test their potency against A549, NCI-H460, and NCI-H1975 lung cancer cells. GF adsorption on AuNP surfaces was examined by UV vis absorption spectra and surface-enhanced Raman scattering. Density functional theory calculations were performed to estimate the energetic stabilities of the drug-AuNP composites. The N1 nitrogen atom of the quinazoline ring of GF was calculated to be more stable than the N3 in binding Au cluster atoms. The internalizations of GF-coated AuNPs were examined by transmission electron and dark-field microscopy. A cell viability test of AuNP GF conjugates with the EGFR antibody exhibited much higher reductions than free GF for A549, NCI-H460, and NCI-H1975 lung cancer cells after treatment for 48 h. (C) 2014 Elsevier B.V. All rights reserved.