de la Salud Bea Roberto, Petraglia Adam F, Ascuitto Michael R, Buck Quentin M
Department of Chemistry, Rhodes College, 2000 North Parkway, Memphis, TN 38112, USA.
Antibiotics (Basel). 2017 Jun 28;6(3):13. doi: 10.3390/antibiotics6030013.
Seven analogs of the natural, α-helix peptides IsCT1 and IsCT2-found in the venom of scorpion -have been synthesized and tested to compare their antibacterial and hemolytic activity against natural peptides. In general, results show that increasing hydrophobicity by substituting positions 5 and 9 of the sequences with alanine, valine, and leucine, enhances antibacterial activity. However, this also increases hemolytic activity. The analog with an increased net positive charge from +1 to +3 produces moderate bacterial growth inhibition but also has high hemolytic activity. On the other hand, the analog with a negative net charge (-1) has low antibacterial properties but also no cytotoxicity under the tested conditions, a similar result was found for five of the seven studied analogs.
已合成并测试了蝎子毒液中发现的天然α-螺旋肽IsCT1和IsCT2的七种类似物,以比较它们与天然肽相比的抗菌和溶血活性。总体而言,结果表明,通过用丙氨酸、缬氨酸和亮氨酸取代序列的第5位和第9位来增加疏水性,可增强抗菌活性。然而,这也会增加溶血活性。净正电荷从+1增加到+3的类似物产生中等程度的细菌生长抑制,但也具有高溶血活性。另一方面,净电荷为负(-1)的类似物具有低抗菌特性,但在测试条件下也没有细胞毒性,在七个研究的类似物中有五个得到了类似的结果。