Institute for Nanobiomedical Technology and Membrane Biology, West China Hospital, Sichuan University, 610041 Chengdu, Sichuan, China.
Biotechnol Lett. 2010 Apr;32(4):463-9. doi: 10.1007/s10529-009-0175-2. Epub 2009 Dec 3.
The anticancer properties and mechanism of action of a hybrid peptide -P18 were investigated. It had significant cytotoxic activity against human melanoma cells and low toxicity to normal NIH-3T3 cells. It also induced cell death via necrosis rather than classical apoptosis. The peptide targets the cells membrane, causing a sustained depolarization of transmembrane potential resulting in the cells swelling and bursting, thereby triggering cytolysis. P18 peptide initially binds to the melanoma cell membrane via electrostatic interaction, causing the cell membrane to rupture. The effect may be mediated by the amphiphilic alpha-helical structure of P18 peptide, coupled with changes in ion channels and an increase in plasma membrane permeability that eventually leads to melanoma cell death.
研究了一种杂合肽 -P18 的抗癌特性和作用机制。它对人黑色素瘤细胞具有显著的细胞毒性,而对正常 NIH-3T3 细胞的毒性较低。它还通过坏死而非经典凋亡诱导细胞死亡。该肽靶向细胞膜,导致跨膜电位持续去极化,导致细胞肿胀和破裂,从而触发细胞溶解。P18 肽最初通过静电相互作用与黑色素瘤细胞膜结合,导致细胞膜破裂。这种作用可能是由 P18 肽的两亲性 α-螺旋结构介导的,同时还伴随着离子通道的变化和质膜通透性的增加,最终导致黑色素瘤细胞死亡。