We report a new small peptide containing four amino acid residues (glycine-aspartic acid-proline-histidine) conjugated with palmitic acid (Palmitoyl-GDPH) that was synthesized, characterized and evaluated for its biological activities. The Palmitoyl-GDPH was prepared by solid phase peptide synthesis (SPPS) with high percentage purity of 98.6%. The results of circular dichroism (CD) demonstrated the feasibility and stability of Palmitoyl-GDPH secondary structure at many temperatures up to 60 °C. Palmitoyl-GDPH showed its greatest collagenase inhibition activity and nitric oxide (NO) scavenging effect of 80.00 ± 2.22% at 1.0 mg/ml and 83.40 ± 8.08% at 2.5 mg/ml, respectively. In addition, in-vitro cell based study revealed that Palmitoyl-GDPH was not toxic and possessed strong proliferative activity towards normal human dermal fibroblast (NHDF) cell line. Wound scratch assay method showed that Palmitoyl-GDPH significantly promoted the cell migration which progressed faster compared to tetracycline-treated group (positive control) by about 98.39 ± 2.79% and 95.79 ± 3.83%, respectively. Collectively, these results suggested that newly synthesized Palmitoyl-GDPH possessed a strong candidate for use as therapeutic agent and can be a novel approach in the treatment of cutaneous wounds.

我们报告了一个新的小肽，其中包含四个氨基酸残基（甘氨酸-天冬氨酸-脯氨酸-组氨酸）与棕榈酸（Palmitoyl-GDPH）共轭，已合成，表征和评估了其生物活性。棕榈酰-GDPH是通过固相肽合成（SPPS）制备的，具有98.6％的高百分比纯度。圆二色性（CD）的结果证明了在高达60°C的许多温度下棕榈酰-GDPH二级结构的可行性和稳定性。棕榈酰-GDPH在1.0 mg / ml时表现出最大的胶原酶抑制活性，对一氧化氮（NO）的清除作用分别为80.00±2.22％和2.5 mg / ml时为83.40±8.08％。此外，体外基于细胞的研究表明，棕榈酰-GDPH对正常人皮肤成纤维细胞（NHDF）细胞系无毒，并具有很强的增殖活性。伤口刮伤试验方法显示，棕榈酰-GDPH显着促进细胞迁移，与四环素处理组（阳性对照组）相比，进展更快，分别约为98.39±2.79％和95.79±3.83％。总的来说，这些结果表明，新合成的棕榈酰-GDPH具有用作治疗剂的强大候选物，并且可以是治疗皮肤伤口的新方法。