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与没食子酸共轭的肽制剂(Gal-Pep)的抗氧化和抗衰老潜力

Antioxidant and anti-aging potential of a peptide formulation (Gal-Pep) conjugated with gallic acid.

作者信息

Lee Hoomin, Kim Kwanwoo, Oh Cheolwoo, Park Chi-Hu, Aliya Sheik, Kim Hyoung-Shik, Bajpai Vivek K, Huh Yun Suk

机构信息

Department of Biological Sciences and Bioengineering, Nano Bio High-Tech Materials Research Center, Inha University Incheon 22212 Republic of Korea

Department of Biosystems and Bioengineering, Inha University Incheon 22212 Republic of Korea.

出版信息

RSC Adv. 2021 Sep 16;11(47):29407-29415. doi: 10.1039/d1ra03421a. eCollection 2021 Sep 1.

Abstract

Skin is highly vulnerable to premature aging due to external stress, therefore, in this study, a peptide formulation, (galloyl)-KTPPTTP (Gal-Pep) was synthesized by combining TPPTTP peptide, and gallic acid (GA). All peptides were synthesized on 2-chlorotrityl chloride resin using solid-phase peptide synthesis (SPPS), and analyzed on an electrospray ionization (ESI)/quadrupole-time-of-flight (Q-TOF) tandem mass spectroscopy (MS) system. Initially, Gal-Pep showed no toxicity below the concentration 100 μM with cell survival rate of 88% for keratinocytes and fibroblasts. The reactive oxygen species (ROS) scavenging activity of Gal-Pep was more stable compared to GA alone; and after four weeks at room temperature, its ROS scavenging activity remained higher than 50%. Moreover, the peptide formulation, Gal-Pep also exhibited elastase inhibitory effect in CCD-1064Sk fibroblast cells. Based on the results of RT-qPCR, it was proved in this study that Gal-Pep increased the expression of PGC-1α to prevent oxidative stress, and validated its potential as an anti-aging agent through increasing the expression of type I collagen and by decreasing the expression of matrix metalloproteinase-1 (MMP1). The findings obtained reinforce the suggestion that the peptide formulation synthesized in this study could be used as a natural antioxidant and anti-aging agent for its cosmetic applications.

摘要

皮肤由于外部压力极易过早老化,因此,在本研究中,通过将TPPTTP肽与没食子酸(GA)结合,合成了一种肽制剂(没食子酰基)-KTPPTTP(Gal-Pep)。所有肽均使用固相肽合成(SPPS)在2-氯三苯甲基氯树脂上合成,并在电喷雾电离(ESI)/四极杆-飞行时间(Q-TOF)串联质谱(MS)系统上进行分析。最初,Gal-Pep在浓度低于100μM时无毒性,角质形成细胞和成纤维细胞的细胞存活率为88%。与单独的GA相比,Gal-Pep的活性氧(ROS)清除活性更稳定;在室温下放置四周后,其ROS清除活性仍高于50%。此外,肽制剂Gal-Pep在CCD-1064Sk成纤维细胞中也表现出弹性蛋白酶抑制作用。基于RT-qPCR的结果,本研究证明Gal-Pep可增加PGC-1α的表达以预防氧化应激,并通过增加I型胶原蛋白的表达和降低基质金属蛋白酶-1(MMP1)的表达来验证其作为抗衰老剂的潜力。所获得的研究结果进一步表明,本研究中合成的肽制剂因其在化妆品中的应用,可作为一种天然抗氧化剂和抗衰老剂。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a30e/9040627/f41baa3f02e7/d1ra03421a-f1.jpg

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