Department of Health Sciences, Brock University, St. Catharines, ON L2S 3A1, Canada.
Centre for Bone and Muscle Health, Brock University, St. Catharines, ON L2S 3A1, Canada.
Int J Mol Sci. 2023 Mar 7;24(6):5094. doi: 10.3390/ijms24065094.
Obesity and elevated blood free fatty acid (FFA) levels lead to impaired insulin action causing insulin resistance in skeletal muscle, and contributing to the development of type 2 diabetes mellitus (T2DM). Mechanistically, insulin resistance is associated with increased serine phosphorylation of the insulin receptor substrate (IRS) mediated by serine/threonine kinases including mTOR and p70S6K. Evidence demonstrated that activation of the energy sensor AMP-activated protein kinase (AMPK) may be an attractive target to counteract insulin resistance. We reported previously that rosemary extract (RE) and the RE polyphenol carnosic acid (CA) activated AMPK and counteracted the FFA-induced insulin resistance in muscle cells. The effect of rosmarinic acid (RA), another polyphenolic constituent of RE, on FFA-induced muscle insulin resistance has never been examined and is the focus of the current study. Muscle cell (L6) exposure to FFA palmitate resulted in increased serine phosphorylation of IRS-1 and reduced insulin-mediated (i) Akt activation, (ii) GLUT4 glucose transporter translocation, and (iii) glucose uptake. Notably, RA treatment abolished these effects, and restored the insulin-stimulated glucose uptake. Palmitate treatment increased the phosphorylation/activation of mTOR and p70S6K, kinases known to be involved in insulin resistance and RA significantly reduced these effects. RA increased the phosphorylation of AMPK, even in the presence of palmitate. Our data indicate that RA has the potential to counteract the palmitate-induced insulin resistance in muscle cells, and further studies are required to explore its antidiabetic properties.
肥胖和血液游离脂肪酸(FFA)水平升高导致胰岛素作用受损,引起骨骼肌胰岛素抵抗,从而导致 2 型糖尿病(T2DM)的发生。从机制上讲,胰岛素抵抗与胰岛素受体底物(IRS)的丝氨酸磷酸化增加有关,这种增加是由包括 mTOR 和 p70S6K 在内的丝氨酸/苏氨酸激酶介导的。有证据表明,激活能量传感器 AMP 激活的蛋白激酶(AMPK)可能是对抗胰岛素抵抗的一个有吸引力的靶点。我们之前曾报道,迷迭香提取物(RE)和 RE 多酚迷迭香酸(CA)可激活 AMPK,对抗肌肉细胞中 FFA 诱导的胰岛素抵抗。迷迭香酸(RA),RE 的另一种多酚成分,对 FFA 诱导的肌肉胰岛素抵抗的影响从未被研究过,这是目前研究的重点。FFA 棕榈酸暴露于肌肉细胞(L6)中会导致 IRS-1 的丝氨酸磷酸化增加,并且减少胰岛素介导的(i)Akt 激活,(ii)GLUT4 葡萄糖转运蛋白易位和(iii)葡萄糖摄取。值得注意的是,RA 处理可消除这些作用,并恢复胰岛素刺激的葡萄糖摄取。棕榈酸处理会增加 mTOR 和 p70S6K 的磷酸化/激活,这些激酶已知与胰岛素抵抗有关,而 RA 则显著降低了这些作用。RA 增加了 AMPK 的磷酸化,即使在存在棕榈酸的情况下也是如此。我们的数据表明,RA 具有对抗肌肉细胞中棕榈酸诱导的胰岛素抵抗的潜力,需要进一步研究来探索其抗糖尿病特性。