Discipline of Chemistry, Indian Institute of Technology Gandhinagar, 382355, Palaj, Gujarat, India.
Discipline of Biological Engineering, Indian Institute of Technology Gandhinagar, 382355, Palaj, Gujarat, India.
Chemistry. 2022 May 25;28(30):e202200203. doi: 10.1002/chem.202200203. Epub 2022 Apr 20.
Endoplasmic reticulum (ER) has emerged as one of the interesting sub-cellular organelles due to its role in myriads of biological phenomena. Subsequently, visualization of the structure-function and dynamics of ER remained a major challenge to understand its involvement in different diseased states including cancer. To illuminate the ER, herein we have designed and synthesized γ-resorcyclic acid-based small molecules, which showed remarkable aggregation-induced emission (AIE) property in water. This AIE property was originated from the dual intramolecular H-bonding leading to the self-assembled 2D aggregation confirmed by pH- and temperature-dependent fluorescence quenching studies as well as scanning electron microscopy. These small molecules illuminated the sub-cellular ER in HeLa cervical cancer cells as well as non-cancerous RPE-1 human retinal epithelial cells within 1 h. These novel small molecules have the potential to light up ER chemical biology in diseased states.
内质网 (ER) 作为细胞内细胞器之一,由于其在众多生物学现象中的作用而备受关注。因此,要了解 ER 在不同疾病状态(包括癌症)中的作用,对其结构-功能和动力学进行可视化仍然是一个主要挑战。为了阐明 ER,我们在此设计并合成了基于γ-Resorcylic 酸的小分子,它们在水中表现出显著的聚集诱导发射(AIE)特性。这种 AIE 特性源于双重的分子内氢键,导致自组装的 2D 聚集,这一点通过 pH 和温度依赖的荧光猝灭研究以及扫描电子显微镜得到了证实。这些小分子在 HeLa 宫颈癌细胞和非癌性 RPE-1 人视网膜上皮细胞中,在 1 小时内即可照亮细胞内的内质网。这些新型小分子有可能照亮疾病状态下的内质网化学生物学。