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Synthesis and Bioactivity of Diastereomers of the Virulence Lanthipeptide Cytolysin

机译:毒性多肽多肽胞溶素的非对映异构体的合成及生物活性

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摘要

Cytolysin, a two-component lanthipeptide comprising cytolysin S (CylL(s)") and cytolysin L (CyILL"), is the only family member to exhibit lytic activity against mammalian cells in addition to synergistic antimicrobial activity. A subset of the thioether cross-links of CylLs" and CylL(L)," have LL stereochemistry instead of the canonical DL stereochemistry in all previously characterized lanthipeptides. The synthesis of a CylLs" variant with DL stereochemistry is reported. Its antimicrobial activity was found to be decreased, but not its lytic activity against red blood cells. Hence, the unusual LL stereochemistry is not responsible for the lytic activity.
机译:溶细胞素是包含溶细胞素S(CylL(s)“)和溶细胞素L(CyILL”)的两组分瘦肽,是除协同抗微生物活性之外,还具有针对哺乳动物细胞的裂解活性的家族成员。 CylLs和CylL(L)的硫醚交联子集具有LL立体化学,而不是所有先前表征的瘦肽中的经典DL立体化学。据报道具有DL立体化学的CylLs”变体的合成。发现其抗菌活性降低,但其对红细胞的裂解活性并未降低。因此,异常的LL立体化学对裂解活性不负责。

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