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Rational Optimizations of the Marine-Derived Peptide Sungsanpin as Novel Inhibitors of Cell Invasion
Chemistry & Biodiversity ( IF 2.3 ) Pub Date : 2023-01-18 , DOI: 10.1002/cbdv.202201221
Anpeng Li 1 , Jihua Zou 2 , Xiaobin Zhuo 1 , Shuai Chen 1 , Xiaoyun Chai 1 , Conghao Gai 1 , Xiang Li 1 , Qingjie Zhao 1 , Yan Zou 1
Chemistry & Biodiversity ( IF 2.3 ) Pub Date : 2023-01-18 , DOI: 10.1002/cbdv.202201221
Anpeng Li 1 , Jihua Zou 2 , Xiaobin Zhuo 1 , Shuai Chen 1 , Xiaoyun Chai 1 , Conghao Gai 1 , Xiang Li 1 , Qingjie Zhao 1 , Yan Zou 1
Affiliation
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Cancer metastasis, including cell invasion, is a major cause of poor clinical outcomes and death in numerous cancer patients. In recent years, many efforts have been made to develop potent therapeutic molecules from naturally derived peptides. Sungsanpin is a naturally derived lasso peptide that inhibits A549 cell invasion. We aimed to evaluate the potential of sungsanpin derivatives as candidates for anti-invasion drugs. We synthesized an analog of sungsanpin (Sun A) using a solid-phase peptide synthesis strategy (SPPS) and further modified its structure to improve its anti-invasion activity. All peptides were tested for their proliferative inhibition and anti-invasion activities in the A549 cell lines. Octapeptide S3 and cyclooctapeptide S4 upregulated the expression of TIMP-1 and TIMP-2 mRNA effectively and thus improved the inhibitory effect on the invasion of A549 cells. The two peptides can inhibit the invasion of A549 cells by up to 60 %, suggesting that they have potential as lead molecules for the development of peptide inhibitors.
中文翻译：
海洋衍生肽宋三平作为新型细胞侵袭抑制剂的合理优化
癌症转移，包括细胞侵袭，是许多癌症患者临床结果不佳和死亡的主要原因。近年来，人们做出了许多努力来从天然衍生的肽中开发有效的治疗分子。Sungsanpin是一种天然衍生的套索肽，可抑制 A549 细胞侵袭。我们旨在评估成三平衍生物作为抗侵袭药物候选物的潜力。我们合成了sungsanpin的类似物(Sun A) 采用固相肽合成策略 (SPPS) 并进一步修饰其结构以提高其抗入侵活性。测试了所有肽在 A549 细胞系中的增殖抑制和抗侵袭活性。八肽S3和环八肽S4有效上调TIMP-1和TIMP-2 mRNA的表达，从而提高对A549细胞侵袭的抑制作用。这两种肽可以抑制高达 60% 的 A549 细胞侵袭，表明它们具有作为开发肽抑制剂的先导分子的潜力。
更新日期：2023-01-18
中文翻译：
海洋衍生肽宋三平作为新型细胞侵袭抑制剂的合理优化
癌症转移，包括细胞侵袭，是许多癌症患者临床结果不佳和死亡的主要原因。近年来，人们做出了许多努力来从天然衍生的肽中开发有效的治疗分子。Sungsanpin是一种天然衍生的套索肽，可抑制 A549 细胞侵袭。我们旨在评估成三平衍生物作为抗侵袭药物候选物的潜力。我们合成了sungsanpin的类似物(Sun A) 采用固相肽合成策略 (SPPS) 并进一步修饰其结构以提高其抗入侵活性。测试了所有肽在 A549 细胞系中的增殖抑制和抗侵袭活性。八肽S3和环八肽S4有效上调TIMP-1和TIMP-2 mRNA的表达，从而提高对A549细胞侵袭的抑制作用。这两种肽可以抑制高达 60% 的 A549 细胞侵袭，表明它们具有作为开发肽抑制剂的先导分子的潜力。
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