Division of Biomedicinal Chemistry and Cosmetics, Mokwon University, Daejeon 35349, Republic of Korea.
Department of Food Science and Technology, Jungwon University, 85, Munmu-ro, Geosan-eup, Geosan-gun, Chungbuk 28024, Republic of Korea.
Eur J Pharmacol. 2018 Aug 5;832:25-32. doi: 10.1016/j.ejphar.2018.05.016. Epub 2018 May 17.
We synthesized and investigated the effects of a novel peptide B, RRFSLLRY as a novel PAR-2 antagonist. Peptide B decreased calcium levels in HaCat cells stimulated with trypsin and PAR-2 activator (SLIGKV) and cytokeratin 14 and PCNA was decreased by peptide B. Peptides B also reduced the expression of inflammatory cytokines such as TNF-α and interleukin-6. Significant increase of oxazolone-induced transepidermal water loss (TEWL) was decreased by the addition of peptide B in hairless mice. These findings suggest that the anti-inflammatory effect of peptide B is due to inhibition of PAR-2 signaling. Skin safety of peptide B was demonstrated by performing MTT assay and human repeated insult patch test. Our findings indicate that peptide B might have potential as an anti-inflammatory agent without irritating skin for use in cosmetics and medical treatment of dermatologic disorders.
我们合成并研究了一种新型肽 B（RRFSLLRY）作为新型 PAR-2 拮抗剂的作用。肽 B 可降低胰蛋白酶和 PAR-2 激动剂（SLIGKV）刺激下 HaCat 细胞内的钙离子水平，并降低细胞角蛋白 14 和 PCNA 的表达。肽 B 还可降低 TNF-α和白细胞介素-6 等炎症细胞因子的表达。在无毛小鼠中，添加肽 B 可显著降低氧化氮酮诱导的经表皮水分丢失（TEWL）。这些发现表明，肽 B 的抗炎作用是由于抑制了 PAR-2 信号通路。通过进行 MTT 测定和人重复刺激斑贴试验，证明了肽 B 的皮肤安全性。我们的研究结果表明，肽 B 可能具有作为抗炎剂的潜力，而不会对皮肤产生刺激性，可用于化妆品和皮肤科疾病的医疗治疗。
