Cytotoxic evaluation of natural and synthetic callipeltins: a revision of cytotoxicity of callipeltin B

The cytotoxic evaluation of natural and synthetic callipeltins is described. Cyclic depsipeptide callipeltin B and linear peptides callipeltins E and M synthesized by us showed no cytotoxic activity. In contrast, natural callipeltin B purified from Callipelta sp. showed CC50 = 130 μM against Hela cells. We found that purified callipeltin B included the contamination of callipeltins C and H at a ratio of approximately 15%. These results suggested that the cytotoxicity of natural callipeltin B was derived from callipeltins C and H.

本研究对天然与合成卡丽培肽素（callipeltins）的细胞毒性评价进行了阐述。本团队合成的环状酯肽类卡丽培肽素B（callipeltin B）以及线性肽类卡丽培肽素E、M均未表现出细胞毒性活性。与之相对，从卡丽培属（Callipelta sp.）物种中纯化得到的天然卡丽培肽素B，针对海拉细胞（Hela）的半数细胞毒性浓度（CC50）为130 μM。本研究发现，所纯化的卡丽培肽素B样品中存在约15%的卡丽培肽素C与卡丽培肽素H污染。上述结果表明，天然卡丽培肽素B所表现出的细胞毒性实际来源于共污染的卡丽培肽素C与H。