Following considerable research efforts on antimicrobial effects by cationic and amphiphilic peptides during the last couple of decades, increasing focus has recently been placed on additional host defense and other biological functions by such peptides, such as anti-inflammatory and anticancer effects. Regarding the latter, it has been increasingly understood that amphiphilic peptides present interesting opportunities not only for reaching selective cancer cell toxicity, but also for promoting uptake of other anticancer therapeutics and of nanopariculate delivery systems containing such drugs. While there is an emerging understanding of the direct antimicrobial function of amphiphilic peptides through bacterial membrane destabilization, the mechanisms underlying their anticancer effects remain less clear. Here, we therefore provide a brief overview on factors affecting toxicity of amphiphilic peptides against tumor and non-malignant cells, and also describe how such peptides can be combined with conjugation moieties or drug delivery systems for increased anticancer effects.

在过去的几十年中，对阳离子和两亲性肽的抗微生物作用进行了大量研究工作之后，近来越来越多的注意力集中在这类肽的其他宿主防御和其他生物学功能上，例如抗炎和抗癌作用。关于后者，人们越来越多地了解，两亲性肽不仅提供了选择性的癌细胞毒性，而且还促进了其他抗癌治疗药物的吸收，从而提供了有趣的机会。以及含有此类药物的纳米颗粒递送系统。尽管对两亲性肽通过细菌膜失稳的直接抗菌功能有了新的认识，但其抗癌作用的潜在机制仍不清楚。因此，在此，我们简要概述了影响两亲性肽对肿瘤和非恶性细胞毒性的因素，并描述了这些肽如何与缀合部分或药物递送系统结合以增强抗癌作用。