Lin Wei-Ju, Chien Yi-Lun, Pan Chia-Yu, Lin Tai-Lang, Chen Jyh-Yih, Chiu Shu-Jun, Hui Cho-Fat
Marine Research Station, Institute of Cellular and Organismic Biology, Academia Sinica, 23-10 Dahuen Rd., Jiaushi, Ilan 262, Taiwan.
Peptides. 2009 Feb;30(2):283-90. doi: 10.1016/j.peptides.2008.10.007. Epub 2008 Oct 21.
Epinecidin-1, a synthetic 21-mer antimicrobial peptide originally identified from grouper (Epinephelus coioides), specifically exhibited high antimicrobial activities against both Gram-negative and Gram-positive bacteria. In the current study we report on the in vitro cytotoxicity of the peptide, an important factor before it can be considered for further applications in cancer therapy. The cytotoxicity of epinecidin-1 was investigated against several cancer cells (A549, HA59T/VGH, HeLa, HepG2, HT1080, RAW264.7, and U937) and normal cells (AML-12, NIH3T3, and WS-1) with the MTT assay, and the inhibition of cancer cell growth was confirmed by a soft agar assay and scanning electron microscopy. However, cell variations were detected with AO/EtBr staining, while apoptosis and necrosis gene expressions in HT1080 cells after treatment with the epinecidin-1 peptide and Nec-1 showed that epinecidin-1 had an anti-necrosis function in HT1080 cells. The data presented here indicate that epinecidin-1 has in vitro antitumor activity against the HT1080 cell line, and functions like lytic peptides. In addition, our results suggest that epinecidin-1 may prove to be an effective chemotherapeutic agent for human fibrosarcoma cells in the future.
表没食子儿茶素-1是一种最初从石斑鱼(Epinephelus coioides)中鉴定出的合成21肽抗菌肽,对革兰氏阴性菌和革兰氏阳性菌均表现出高抗菌活性。在本研究中,我们报告了该肽的体外细胞毒性,这是其在癌症治疗中进一步应用前的一个重要因素。通过MTT法研究了表没食子儿茶素-1对几种癌细胞(A549、HA59T/VGH、HeLa、HepG2、HT1080、RAW264.7和U937)和正常细胞(AML-12、NIH3T3和WS-1)的细胞毒性,并用软琼脂试验和扫描电子显微镜证实了对癌细胞生长的抑制作用。然而,用AO/EtBr染色检测到细胞变化,而用表没食子儿茶素-1肽和Nec-1处理后HT1080细胞中的凋亡和坏死基因表达表明,表没食子儿茶素-1在HT1080细胞中具有抗坏死功能。此处给出的数据表明,表没食子儿茶素-1对HT1080细胞系具有体外抗肿瘤活性,其功能类似于裂解肽。此外,我们的结果表明,表没食子儿茶素-1未来可能被证明是一种有效的人纤维肉瘤细胞化疗药物。