Laboratório de Biofísica Celular e Inflamação, Pontifícia Universidade Católica do Rio Grande do Sul (PUCRS), 6681 Ipiranga Ave., RS, 90619-900, Porto Alegre, Brazil.
Laboratório de Biotecnologia Vegetal, PUCRS, Porto Alegre, Brazil.
Naunyn Schmiedebergs Arch Pharmacol. 2023 May;396(5):925-937. doi: 10.1007/s00210-022-02361-w. Epub 2022 Dec 15.
Coumaric acid is a phenolic compound found in medicinal plants. Its use has been reported in the treatment of inflammatory diseases, prevention of alterations induced by oxidative stress, as well as acetaminophen-induced hepatotoxicity. Thus, this study evaluated coumaric acid as a potential treatment for liver fibrosis. Cell proliferation was assessed by the trypan blue exclusion technique and the cytotoxicity of coumaric acid was performed using an LDH assay. Mechanisms of cell apoptosis were evaluated by flow cytometry. The expression of genes associated with apoptosis, cell cycle control, and fibrosis was assessed by qPCR. The production of lipid droplets was quantified by oil red staining. The experiments performed showed that the treatment with coumaric acid was able to reduce cell proliferation without causing cell cytotoxicity or apoptosis. Coumaric acid was able to inhibit the expression of cyclin D1 and CDK's (CDK2, CDK4, and CDK6), increasing p53 and p21, which could lead to cell cycle arrest. Treatment with coumaric acid was also able to revert the activated phenotype of GRX cells to their quiescent state. Thus, our results suggest that coumaric acid has a potential therapeutic effect against liver fibrosis.
香豆酸是一种在药用植物中发现的酚类化合物。其已被报道可用于治疗炎症性疾病、预防氧化应激诱导的改变以及对乙酰氨基酚诱导的肝毒性。因此,本研究评估了香豆酸作为治疗肝纤维化的潜在药物。细胞增殖通过台盼蓝排除技术进行评估,香豆酸的细胞毒性通过 LDH 测定进行评估。通过流式细胞术评估细胞凋亡的机制。通过 qPCR 评估与细胞凋亡、细胞周期控制和纤维化相关的基因的表达。通过油红染色定量测定脂滴的产生。进行的实验表明,香豆酸处理能够减少细胞增殖,而不会导致细胞毒性或细胞凋亡。香豆酸能够抑制 cyclin D1 和 CDK(CDK2、CDK4 和 CDK6)的表达,增加 p53 和 p21,从而导致细胞周期停滞。香豆酸处理还能够使 GRX 细胞的激活表型恢复到静止状态。因此,我们的结果表明香豆酸具有治疗肝纤维化的潜在疗效。