SKINMED R&D Center, Daejeon 34037, Republic of Korea.
College of Pharmacy, Chungbuk National University, Cheongju 28160, Republic of Korea.
Int J Mol Sci. 2024 Jul 18;25(14):7860. doi: 10.3390/ijms25147860.
Wrinkles, one of the most common signs of aging, are primarily caused by the continuous contraction of muscles. Muscle contraction is induced by the binding of acetylcholine (ACh), released at the neuromuscular junction, to nicotinic acetylcholine receptor (nAChR) present on the muscle cell surface. In this study, we aimed to develop a wrinkle-improving peptide that inhibits the binding of ACh to nAChR using peptide phage display technology. Our peptide showed a remarkably high binding affinity to nAChR subunit α1, with a value below 1 µM, and was found to inhibit the action of ACh through its interaction with these receptors. Furthermore, it increased collagen synthesis in skin cells and upregulated the expression of the aquaporin-3 (AQP3) and hyaluronan synthase-2 (HAS2) genes. These results confirm that the peptide effectively inhibits muscle contraction and enhances skin elasticity and hydration, contributing to its wrinkle-reducing effects. Clinical studies on humans observed significant improvement in wrinkles after three weeks of use, with substantial reduction observed after six weeks. In conclusion, these findings demonstrate the efficacy of the peptide (named Medipep) in reducing wrinkles.
皱纹是衰老的最常见标志之一,主要是由于肌肉的持续收缩引起的。肌肉收缩是由乙酰胆碱(ACh)在神经肌肉接头处释放,并与肌肉细胞膜表面的烟碱型乙酰胆碱受体(nAChR)结合引起的。在这项研究中,我们旨在使用肽噬菌体展示技术开发一种抑制 ACh 与 nAChR 结合的改善皱纹肽。我们的肽对 nAChR 亚基 α1 表现出极高的结合亲和力,其值低于 1µM,并通过与这些受体相互作用来抑制 ACh 的作用。此外,它还能增加皮肤细胞中的胶原蛋白合成,并上调水通道蛋白-3(AQP3)和透明质酸合酶-2(HAS2)基因的表达。这些结果证实,该肽能有效抑制肌肉收缩,增强皮肤弹性和保水能力,从而减少皱纹。对人类的临床研究表明,使用三周后皱纹明显改善,六周后皱纹明显减少。总之,这些发现证明了这种名为 Medipep 的肽在减少皱纹方面的功效。