Departamento de Parasitologia, Instituto de Ciências Biomédicas, Universidade de São Paulo, São Paulo-SP, Brazil.
FEMS Microbiol Lett. 2011 Nov;324(1):64-72. doi: 10.1111/j.1574-6968.2011.02386.x. Epub 2011 Sep 12.
Microplusin is an antimicrobial peptide isolated from the cattle tick Rhipicephalus (Boophilus) microplus. Its copper-chelating ability is putatively responsible for its bacteriostatic activity against Micrococcus luteus as microplusin inhibits respiration in this species, which is a copper-dependent process. Microplusin is also active against Cryptococcus neoformans (MIC(50) = 0.09 μM), the etiologic agent of cryptococcosis. Here, we show that microplusin is fungistatic to C. neoformans and this inhibitory effect is abrogated by copper supplementation. Notably, microplusin drastically altered the respiratory profile of C. neoformans. In addition, microplusin affects important virulence factors of this fungus. We observed that microplusin completely inhibited fungal melanization, and this effect correlates with the inhibition of the related enzyme laccase. Also, microplusin significantly inhibited the capsule size of C. neoformans. Our studies reveal, for the first time, a copper-chelating antimicrobial peptide that inhibits respiration and growth of C. neoformans and modifies two major virulence factors: melanization and formation of a polysaccharide capsule. These features suggest that microplusin, or other copper-chelation approaches, may be a promising therapeutic for cryptococcosis.
微菌素是从牛蜱 Rhipicephalus (Boophilus) microplus 中分离出来的一种抗菌肽。其螯合铜的能力可能是其对微球菌属(Micrococcus luteus)具有抑菌活性的原因,因为微菌素抑制了该物种的呼吸,而呼吸是一个依赖铜的过程。微菌素对新型隐球菌(Cryptococcus neoformans)(MIC(50) = 0.09 μM)也有活性,新型隐球菌是隐球菌病的病原体。在这里,我们表明微菌素对新型隐球菌具有抑菌作用,而铜的补充会消除这种抑制作用。值得注意的是,微菌素极大地改变了新型隐球菌的呼吸谱。此外,微菌素还影响了这种真菌的重要毒力因子。我们观察到微菌素完全抑制了真菌的黑色素形成,而这种效应与相关酶漆酶的抑制作用相关。此外,微菌素还显著抑制了新型隐球菌的荚膜大小。我们的研究首次揭示了一种能够抑制新型隐球菌的呼吸和生长并改变两种主要毒力因子(黑色素形成和多糖荚膜形成)的铜螯合抗菌肽。这些特征表明,微菌素或其他铜螯合方法可能是治疗隐球菌病的一种有前途的方法。