PDF(Pubmed)
Abstract：
Chalcone (1,3-diaryl-2-propen-1-one) is an α, β-unsaturated ketone that serves as an active constituent or precursor of numerous natural substances, exhibiting a broad spectrum of pharmacological effects. In this study, the classical Claisen-Schmidt condensation method was used to synthesize the chalcone derivative 2\',4\'-dimethoxychalcone (DTC) and evaluate its pharmacological activity. By upregulating the expression of the epithelial cell marker E-cadherin and downregulating the expression of the mesenchymal cell marker vimentin, DTC was found to inhibit transforming growth factor-β1 (TGF-β1)-induced epithelial-mesenchymal transition (EMT) process in A549 cells, maintaining the cells\' epithelial-like morphology and reducing the ability of the cells to migrate. Additionally, DTC demonstrated the ability to decrease the expression levels of nitric oxide (NO), tumor necrosis factor (TNF-α), interleukin-6 (IL-6), and interleukin-1β (IL-1β) in RAW264.7 cells, suggesting a possible anti-inflammatory effect. Furthermore, DTC was found to exhibit bacteriostatic activity against Staphylococcus aureus (S. aureus), Proteus vulgaris (P. vulgaris), methicillin-resistant Staphylococcus aureus (MRSA), and Candida albicans (C. albicans), indicating that this chemical may possess broad-spectrum antibacterial activity.
摘要：
查尔酮（1,3-二芳基-2-丙烯-1-酮）是α，β-不饱和酮，作为许多天然物质的活性成分或前体，表现出广谱的药理作用。在这项研究中,经典的Claisen-Schmidt缩合方法用于合成查尔酮衍生物2'，4'-二甲氧基查耳酮（DTC）并评估其药理活性。通过上调上皮细胞标志物E-cadherin的表达和下调间充质细胞标志物波形蛋白的表达，发现DTC抑制A549细胞中转化生长因子-β1(TGF-β1)诱导的上皮-间质转化(EMT)过程,维持细胞上皮样形态，降低细胞迁移能力。此外,DTC显示出降低一氧化氮（NO）表达水平的能力，肿瘤坏死因子（TNF-α），白细胞介素-6（IL-6），和白细胞介素-1β（IL-1β）在RAW264.7细胞，提示可能的抗炎作用。此外，发现DTC对金黄色葡萄球菌具有抑菌活性(S.金黄色葡萄球菌)，变形杆菌(P.vulgaris)，耐甲氧西林金黄色葡萄球菌(MRSA),和白色念珠菌(C.albicans),表明这种化学物质可能具有广谱抗菌活性。
