Farnesol, a C15 terpene alcohol that is ubiquitous in nature, is a component of plant essential oils and is a quorum sensing molecule in Candida albicans [1]. Farnesol exerts the pro-inflammatory effect by increasing the levels of IL-6, TNF-α, and COX-2 in macrophage cells[2]. Farnesol has been widely used in various cell models and animal models to inhibit tumor growth[3].
In vitro, Farnesol treatment for 24 hours significantly inhibited the viability of A549 cells and Caco-2 cells, with IC50 values of 4.6mM and 3.9mM, respectively[4]. Treatment with 20μM Farnesol for 48 hours significantly inhibited the growth of MCF-7 cells, induced the expression of THRβ1 mRNA and protein, and prevented the binding of THRβ1 to DNA[5]. Treatment of H460 cells with 250μM Farnesol for 24 hours induced endoplasmic reticulum stress and unfolded protein response, promoted cell apoptosis, accompanied by the activation of MEK1/2[6].
In vivo, Farnesol treatment via oral administration at a dose of 100mg/kg/day for 5 weeks restored the cytokine secretion capacity of peritoneal macrophages in asthmatic mice, and reduced the levels of IL-6, TNF-α and inducible nitric oxide synthase (iNOS)[7]. Oral administration of 50mg/kg Farnesol daily for 5 weeks significantly reduced tumor growth in a prostate cancer mouse model[8].
References:
[1] Chandran S S, Kealey J T, Reeves C D. Microbial production of isoprenoids[J]. Process biochemistry, 2011, 46(9): 1703-1710.
[2] Ghosh S, Howe N, Volk K, et al. Candida albicans cell wall components and farnesol stimulate the expression of both inflammatory and regulatory cytokines in the murine RAW264. 7 macrophage cell line[J]. FEMS Immunology & Medical Microbiology, 2010, 60(1): 63-73.
[3] Jung Y Y, Hwang S T, Sethi G, et al. Potential anti-inflammatory and anti-cancer properties of farnesol[J]. Molecules, 2018, 23(11): 2827.
[4] Yilmaz Öztürk B, Feyzullazade N, Dağ İ, et al. The investigation of in vitro effects of farnesol at different cancer cell lines[J]. Microscopy Research and Technique, 2022, 85(8): 2760-2775.
[5] Duncan R E, Archer M C. Farnesol induces thyroid hormone receptor (THR) β1 but inhibits THR-mediated signaling in MCF-7 human breast cancer cells[J]. Biochemical and biophysical research communications, 2006, 343(1): 239-243.
[6] Joo J H, Liao G, Collins J B, et al. Farnesol-induced apoptosis in human lung carcinoma cells is coupled to the endoplasmic reticulum stress response[J]. Cancer research, 2007, 67(16): 7929-7936.
[7] Ku C M, Lin J Y. Farnesol, a sesquiterpene alcohol in herbal plants, exerts anti‐inflammatory and antiallergic effects on ovalbumin‐sensitized and‐challenged asthmatic mice[J]. Evidence‐Based Complementary and Alternative Medicine, 2015, 2015(1): 387357.
[8] Park J S, Kwon J K, Kim H R, et al. Farnesol induces apoptosis of DU145 prostate cancer cells through the PI3K/Akt and MAPK pathways[J]. International journal of molecular medicine, 2014, 33(5): 1169-1176.
Farnesol是一种在自然界普遍存在的C15萜烯醇，是植物精油的组成部分，也是白色念珠菌的群体感应分子[1]。Farnesol通过增加巨噬细胞中IL-6、TNF-α和COX-2的水平发挥促炎作用[2]。Farnesol已被广泛用于各种细胞模型和动物模型，以抑制肿瘤生长[3]。
在体外，Farnesol处理24小时显著抑制了A549细胞和Caco-2细胞的活力，IC50值分别为4.6mM和3.9mM[4]。使用20µM的Farnesol处理48小时，显著抑制了MCF-7细胞的生长，诱导了THRβ1 mRNA和蛋白的表达，并阻止了THRβ1与DNA的结合[5]。使用250µM的Farnesol处理H460细胞24小时，诱导了内质网应激和未折叠蛋白反应，促进了细胞凋亡，并伴有MEK1/2的激活[6]。
在体内，每日口服给予100mg/kg剂量的Farnesol，持续5周，恢复了哮喘小鼠腹腔巨噬细胞的细胞因子分泌能力，并降低了IL-6、TNF-α和诱导型一氧化氮合酶（iNOS）的水平[7]。每日口服50mg/kg剂量的Farnesol，持续5周，显著降低了前列腺癌小鼠模型中的肿瘤生长[8]。