Preliminary experimental anticancer activity of cecropins.

Peptide research Pub Date : 1994-09-01
A J Moore, D A Devine, M C Bibby
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Abstract

The cecropins are a group of peptides that were first isolated from the hemolymph of the giant silk moth, Hyalophora cecropia. In preliminary studies, these novel peptides were shown to be active against several bacteria and mammalian lymphomas and leukemias in vitro. The mechanism of action of the cecropins is thought to involve pore formation at the cytoplasmic membrane. The potential anticancer activity of cecropin B, cecropin P1 and Shiva-1 was investigated against a panel of mammalian cell lines in vitro. Cell lines showed a range of sensitivities to cecropin B (IC50 3.2 to > 100 microM), and two cell lines with the multidrug-resistant phenotype were sensitive to the peptide. In vitro cecropin B activity was virtually complete within one hour. Preliminary in vivo studies showed that cecropin B increases the survival time of mice bearing murine ascitic colon adenocarcinoma cells. Future studies will address structure/activity relationships of similar peptides in order to optimize antitumor activity.

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天蚕素抗癌活性的初步实验研究。
cecropins是一组肽,首次从巨型蚕蛾Hyalophora cecropia的血淋巴中分离。在初步研究中,这些新型肽在体外被证明对几种细菌和哺乳动物淋巴瘤和白血病有活性。抗菌肽的作用机制被认为与细胞质膜上的孔形成有关。在体外对一组哺乳动物细胞系研究了cecropin B、cecropin P1和Shiva-1的潜在抗癌活性。细胞株对cecropin B具有一定的敏感性(IC50为3.2 ~ > 100 μ m),其中2株具有多药耐药表型的细胞株对该肽敏感。体外天蚕素B的活性几乎在一小时内完成。初步的体内研究表明,cecropin B可延长小鼠腹水结肠腺癌细胞的存活时间。未来的研究将进一步探讨类似肽的结构/活性关系,以优化其抗肿瘤活性。
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