人源性双亲性穿膜肽PKV14的合成及其对BHK-21细胞的影响

目的合成人源性双亲性穿膜肽RRTLRRRRAAQRCG(PKV14),并研究其细胞穿膜效果和对细胞活性的影响。方法采用固相合成法合成PKV14,采用高效液相色谱和质谱对PKV14进行验证,使用荧光显微镜和酶标仪观察PKV14在BHK-21细胞系中的穿膜效果,采用MTT实验法检测PKV14的细胞毒性。结果合成了PKV14肽段,并且PKV14对于BHK-21细胞系的穿膜效率极高,细胞毒性实验表明PKV14对BHK-21细胞活性无影响。结论 PKV14是具有高穿膜活性,安全低毒的新型人源性细胞穿膜肽,有作为药物载体的潜力。

Synthesis of human-derived amphipathic cell-penetrating peptide PKV14 and effect on BHK-21 cell

Objective To synthesize the human-derived amphipathic cell-penetrating peptide RRTLRRRRAAQRCG (PKV14), and investigate the effect on cell membrane penetration and its cytotoxicity. Methods PKV14 was synthesized by a solid-phase peptide synthesis. HPLC and MS analysis methods were applied to identifying its structure. The penetrating effects of PKV14 in BHK-21 cells were tested by fluorescence microscopy and microplate reader. The cytotoxicity of PKV14 was tested by MTT method. Results PKV14 was synthesized successfully and it was confirmed that PKV14 had a very high penetrating efficiency in BHK-21 cells. Cytotoxicity test showed that PKV14 had no effect on the activity of BHK-21 cells. Conclusion PKV14 is a novel human cell penetrating peptide with high penetrating activity, safety, and low toxicity which has potential as a drug carrier.