Mailisa Wiska, Annisa Windy Dwi, Permatasari Fitri Aulia, Amalia Riezki, Ivansyah Atthar Luqman, Iskandar Ferry, Rachmawati Heni
Research Group of Pharmaceutics - School of Pharmacy, Institut Teknologi Bandung, Ganesa 10, Bandung 40132, Indonesia.
Research Center for Nanosciences and Nanotechnology, Institut Teknologi Bandung, Ganesa 10, Bandung 40132, Indonesia.
ACS Omega. 2023 Mar 6;8(11):10077-10085. doi: 10.1021/acsomega.2c07398. eCollection 2023 Mar 21.
The alteration of ACE2 expression level, which has been studied in many diseases, makes the topic of ACE2 inducer potential crucial to be explored. The ACE2 inducer could further be designed to control the ACE2 expression level, which is appropriate to a specific case. An in vitro study of well-characterized carbon dots (CDs), made from citric acid and urea, was performed to determine their ability to modulate the ACE2 receptor. Gene expression of ACE2 was quantified using concentrations adjusted for IC50 results from CDs viability assays in HEK 293 and A549 cell lines. RT-qPCR was used to assess the expression of the ACE2 gene and its induction effect in normal cell lines (HEK-293A). According to the results of the tests, ACE2 is expressed in HEK-293A cell lines, and diminazene aceturate can increase ACE2 expression. The effect of CDs on ACE2 gene expression was further examined on the cell lines that had previously been induced with diminazene aceturate, which resulted in upregulation of the ACE2 expression level. An in silico study has been done by using a molecular docking approach. The molecular docking results show that CDs can make strong interactions with ACE2 amino acid residues through hydrophobic interaction, π-π interaction, π-cation interaction, and ionic interaction.
在许多疾病中都对血管紧张素转换酶2（ACE2）表达水平的改变进行了研究，这使得探索ACE2诱导剂的潜力这一话题至关重要。可以进一步设计ACE2诱导剂来控制ACE2的表达水平，以适用于特定情况。对由柠檬酸和尿素制成的特性明确的碳点（CDs）进行了体外研究，以确定它们调节ACE2受体的能力。使用根据HEK 293和A549细胞系中CDs活力测定的IC50结果调整的浓度对ACE2的基因表达进行定量。逆转录定量聚合酶链反应（RT-qPCR）用于评估ACE2基因的表达及其在正常细胞系（HEK-293A）中的诱导作用。根据测试结果，ACE2在HEK-293A细胞系中表达，乙酰氧苄胺嘧啶可增加ACE2表达。在先前用乙酰氧苄胺嘧啶诱导的细胞系上进一步研究了CDs对ACE2基因表达的影响，结果导致ACE2表达水平上调。通过分子对接方法进行了计算机模拟研究。分子对接结果表明，CDs可以通过疏水相互作用、π-π相互作用、π-阳离子相互作用和离子相互作用与ACE2氨基酸残基产生强烈相互作用。
