Conlon J Michael, Woodhams Douglas C, Raza Haider, Coquet Laurent, Leprince Jérôme, Jouenne Thierry, Vaudry Hubert, Rollins-Smith Louise A
Department of Biochemistry, Faculty of Medicine and Health Sciences, United Arab Emirates University, 17666 Al-Ain, United Arab Emirates.
Toxicon. 2007 Sep 15;50(4):498-506. doi: 10.1016/j.toxicon.2007.04.017. Epub 2007 May 3.
Two peptides with differential cytolytic activity against bacteria, a fungus pathogenic to amphibians, and mammalian cells were isolated from norepinephrine-stimulated skin secretions of the Lemur leaf frog Hylomantis lemur Boulenger, 1882. Dermaseptin-L1 (GLWSKIKEAAKAAGKAALNAVTGLVNQGDQPS) was active against the Gram-negative bacterium Escherichia coli (MIC=8 microM) but inactive against the Gram-positive bacterium Staphylococcus aureus. This peptide inhibited growth of zoospores of the chytrid fungus Batrachochytrium dendrobatidis at concentrations above 25 microM but did not completely inhibit growth at 100 microM. Phylloseptin-L1 (LLGMIPLAISAISALSKL.NH2) was active against S. aureus (MIC=8 microM) but was inactive against E. coli. This peptide also inhibited growth of B. dendrobatidis zoospores at concentrations above 25 microM with complete inhibition at 100 microM. Dermaseptin-L1 showed selective cytolytic activity against HepG2 human hepatoma-derived cells (LC50=45 microM) compared with human erythrocytes (LC50=200 microM) whereas phylloseptin-L1 was approximately equipotent against both HepG2 cells (LC50=35 microM) and erythrocytes (LC50=40 microM).
从1882年的狐猴叶蛙(Hylomantis lemur Boulenger)去甲肾上腺素刺激的皮肤分泌物中分离出两种对细菌、一种两栖类致病真菌和哺乳动物细胞具有不同溶细胞活性的肽。皮肤防御素-L1(GLWSKIKEAAKAAGKAALNAVTGLVNQGDQPS)对革兰氏阴性菌大肠杆菌有活性(MIC = 8 microM),但对革兰氏阳性菌金黄色葡萄球菌无活性。该肽在浓度高于25 microM时抑制蛙壶菌(Batrachochytrium dendrobatidis)游动孢子的生长,但在100 microM时未完全抑制生长。叶状防御素-L1(LLGMIPLAISAISALSKL.NH2)对金黄色葡萄球菌有活性(MIC = 8 microM),但对大肠杆菌无活性。该肽在浓度高于25 microM时也抑制蛙壶菌游动孢子的生长,在100 microM时完全抑制。与人类红细胞(LC50 = 200 microM)相比,皮肤防御素-L1对人肝癌衍生的HepG2细胞表现出选择性溶细胞活性(LC50 = 45 microM),而叶状防御素-L1对HepG2细胞(LC50 = 35 microM)和红细胞(LC50 = 40 microM)的活性大致相当。