Department of Otolaryngology-Head and Neck Surgery, Huai'an Hospital Affiliated to Xuzhou Medical University, Huai'an, Jiangsu 223300, P.R. China.
Department of Clinical Laboratory, Huai'an Hospital Affiliated to Xuzhou Medical University, Huai'an, Jiangsu 223300, P.R. China.
Int J Mol Med. 2018 Jul;42(1):193-207. doi: 10.3892/ijmm.2018.3593. Epub 2018 Mar 27.
Non-alcoholic fatty liver disease (NAFLD) comprises a spectrum of liver damage characterized by abnormal hepatic fat accumulation and inflammatory response. Although the molecular mechanisms responsible for the disease are not yet fully understood, the pathogenesis of NAFLD likely involves multiple signals. The identification of effective therapeutic strategies to target these signals is of utmost importance. Carnosic acid (CA), as a phenolic diterpene with anticancer, anti-bacterial, anti-diabetic and neuroprotective properties, is produced by many species of the Lamiaceae family. Myristoylated alanine-rich C-kinase substrate (MARCKS) is a major protein kinase C (PKC) substrate in many different cell types. In the present study, wild-type C57BL/6 and MARCKS-deficient mice were randomly divided into the normal chow- or high-fat (HF) diet-fed groups. The HF diet increased the fasting glucose and insulin levels, and promoted glucose intolerance in the wild-type mice. MARCKS deficiency further upregulated intolerance, fasting glucose and insulin. The HF diet also promoted hepatic steatosis, serum alanine transaminase (ALT) and aspartate transaminase (AST) activity, inflammation and lipid accumulation in the wild-type mice. These responses were accelerated in the MARCKS-deficient mice. Importantly, increased inflammation and lipid accumulation were associated with phosphoinositide 3-kinase (PI3K)/AKT, NLR family pyrin domain containing 3 (NLRP3)/nuclear factor-κB (NF-κB) and sterol regulatory element binding protein-1c (SREBP-1c) signaling pathway activation. The mice treated with CA exhibited a significantly improved glucose and insulin tolerance. The production of pro-inflammatory cytokines and lipid accumulation were suppressed by CA. Significantly, MARCKS was reduced in mice fed the HF diet. CA treatment upregulated MARCKS expression compared to the HF group. Furthermore, the activation of the PI3K/AKT, NLRP3/NF-κB and SREBP-1c signaling pathways was inhibited by CA. Taken together, our data suggest that CA suppresses inflammation and lipogenesis in mice fed a HF diet through MARCKS regulation. Thus, CA may be prove to be a useful anti-NAFLD agent.
非酒精性脂肪性肝病(NAFLD)包括一系列以肝内脂肪异常积聚和炎症反应为特征的肝损伤。尽管导致该病的分子机制尚不完全清楚,但 NAFLD 的发病机制可能涉及多种信号。因此,确定针对这些信号的有效治疗策略非常重要。迷迭香酸(CA)是一种具有抗癌、抗菌、抗糖尿病和神经保护作用的酚二萜,由唇形科的许多物种产生。肌醇六磷酸酰丝氨酸丰富的蛋白激酶 C 底物(MARCKS)是许多不同细胞类型中蛋白激酶 C(PKC)的主要底物。在本研究中,野生型 C57BL/6 和 MARCKS 缺陷型小鼠被随机分为正常饲料或高脂肪(HF)饮食喂养组。HF 饮食增加了野生型小鼠的空腹血糖和胰岛素水平,并促进了葡萄糖不耐受。MARCKS 缺陷进一步加重了不耐受、空腹血糖和胰岛素水平。HF 饮食还促进了野生型小鼠的肝脂肪变性、血清丙氨酸转氨酶(ALT)和天冬氨酸转氨酶(AST)活性、炎症和脂质积聚。在 MARCKS 缺陷型小鼠中,这些反应加速。重要的是,炎症和脂质积聚的增加与磷酸肌醇 3-激酶(PI3K)/蛋白激酶 B(AKT)、NLR 家族 pyrin 结构域包含 3(NLRP3)/核因子-κB(NF-κB)和固醇调节元件结合蛋白-1c(SREBP-1c)信号通路的激活有关。用 CA 治疗的小鼠表现出明显改善的葡萄糖和胰岛素耐量。CA 抑制促炎细胞因子的产生和脂质积聚。值得注意的是,HF 饮食喂养的小鼠 MARCKS 减少。CA 治疗与 HF 组相比,上调 MARCKS 表达。此外,CA 抑制了 PI3K/AKT、NLRP3/NF-κB 和 SREBP-1c 信号通路的激活。综上所述,我们的数据表明,CA 通过调节 MARCKS 抑制高脂肪饮食喂养小鼠的炎症和脂肪生成。因此,CA 可能被证明是一种有用的抗非酒精性脂肪性肝病药物。