Department of Biochemistry, College of Medicine and Health Sciences, United Arab Emirates University, Al Ain 17666, UAE.
Pharmaceuticals (Basel). 2014 Jan 15;7(1):58-77. doi: 10.3390/ph7010058.
Skin secretions from frogs belonging to the genera Xenopus, Silurana, Hymenochirus, and Pseudhymenochirus in the family Pipidae are a rich source of host-defense peptides with varying degrees of antimicrobial activities and cytotoxicities to mammalian cells. Magainin, peptide glycine-leucine-amide (PGLa), caerulein-precursor fragment (CPF), and xenopsin-precursor fragment (XPF) peptides have been isolated from norepinephrine-stimulated skin secretions from several species of Xenopus and Silurana. Hymenochirins and pseudhymenochirins have been isolated from Hymenochirus boettgeri and Pseudhymenochirus merlini. A major obstacle to the development of these peptides as anti-infective agents is their hemolytic activities against human erythrocytes. Analogs of the magainins, CPF peptides and hymenochirin-1B with increased antimicrobial potencies and low cytotoxicities have been developed that are active (MIC < 5 μM) against multidrug-resistant clinical isolates of Staphylococcus aureus, Escherichia coli, Acinetobacter baumannii, Stenotrophomonas maltophilia and Klebsiella pneumoniae. Despite this, the therapeutic potential of frog skin peptides as anti-infective agents has not been realized so that alternative clinical applications as anti-cancer, anti-viral, anti-diabetic, or immunomodulatory drugs are being explored.
蛙科的 Xenopus、Silurana、Hymenochirus 和 Pseudhymenochirus 属的青蛙皮肤分泌物是具有不同程度抗微生物活性和细胞毒性的宿主防御肽的丰富来源。蛙科和 Silurana 属的几种物种的去甲肾上腺素刺激的皮肤分泌物中分离出了抗菌肽、肽甘氨酸-亮氨酸酰胺 (PGLa)、蓝斑肽前体片段 (CPF) 和 Xenopsin 前体片段 (XPF) 肽。Hymenochirins 和 pseudhymenochirins 从 Hymenochirus boettgeri 和 Pseudhymenochirus merlini 中分离出来。这些肽作为抗感染剂的发展主要障碍是它们对人红细胞的溶血活性。已经开发出具有更高抗菌效力和低细胞毒性的抗菌肽、CPF 肽和 hymenochirin-1B 的类似物,对耐多药的金黄色葡萄球菌、大肠杆菌、鲍曼不动杆菌、嗜麦芽窄食单胞菌和肺炎克雷伯菌的临床分离株具有活性(MIC <5 μM)。尽管如此,青蛙皮肤肽作为抗感染剂的治疗潜力尚未实现,因此正在探索将其作为抗癌、抗病毒、抗糖尿病或免疫调节剂药物的替代临床应用。