Edgerton M, Koshlukova S E, Araujo M W, Patel R C, Dong J, Bruenn J A
Departments of Oral Biology, State University of New York at Buffalo, Buffalo, New York 14214, USA.
Antimicrob Agents Chemother. 2000 Dec;44(12):3310-6. doi: 10.1128/AAC.44.12.3310-3316.2000.
Salivary histatins are a family of basic histidine-rich proteins in which therapeutic potential as drugs against oral candidiasis is apparent, considering their potent in vitro antifungal activity and lack of toxicity to humans. Histatin 5 (Hst 5) kills the fungal pathogen Candida albicans via a mechanism that involves binding to specific sites on the yeast cell membrane and subsequent release of cellular ATP in the absence of cytolysis. We explored the killing pathway activated by Hst 5 and compared it to those activated by other antifungal agents. The candidacidal activity of human neutrophil defensin 1 (HNP-1) shared very similar features to Hst 5 cytotoxic action with respect to active concentrations and magnitude of induction of nonlytic ATP efflux, depletion of intracellular ATP pools, and inhibitor profile. Hst 5 and HNP-1 are basic proteins of about 3 kDa; however, they have unique primary sequences and solution structures that cannot explain how these two molecules act so similarly on C. albicans to induce cell death. Our finding that HNP-1 prevented Hst 5 binding to the candidal Hst 5 binding protein suggests that the basis for the overlapping actions of these two naturally occurring antimicrobial proteins may involve interactions with shared yeast components.
唾液组蛋白是一类富含组氨酸的碱性蛋白质家族,鉴于其强大的体外抗真菌活性以及对人体无毒,其作为抗口腔念珠菌病药物的治疗潜力显而易见。组蛋白5(Hst 5)通过一种机制杀死真菌病原体白色念珠菌,该机制包括与酵母细胞膜上的特定位点结合,随后在不发生细胞溶解的情况下释放细胞内ATP。我们探究了由Hst 5激活的杀伤途径,并将其与其他抗真菌剂激活的途径进行比较。就活性浓度、非裂解性ATP外排的诱导幅度、细胞内ATP池的消耗以及抑制剂谱而言,人类中性粒细胞防御素1(HNP - 1)的杀念珠菌活性与Hst 5的细胞毒性作用具有非常相似的特征。Hst 5和HNP - 1是约3 kDa的碱性蛋白质;然而,它们具有独特的一级序列和溶液结构,无法解释这两种分子如何在白色念珠菌上如此相似地发挥作用以诱导细胞死亡。我们发现HNP - 1可阻止Hst 5与念珠菌Hst 5结合蛋白结合,这表明这两种天然存在的抗菌蛋白重叠作用的基础可能涉及与酵母共享成分的相互作用。