Vago T, Baldi G, Colombo D, Barbareschi M, Norbiato G, Dallegri F, Bevilacqua M
Servizio di Endocrinologia, Ospedale L. Sacco (Vialba), Milan, Italy.
Antimicrob Agents Chemother. 1994 Nov;38(11):2605-11. doi: 10.1128/AAC.38.11.2605.
Many antimycotic agents negatively affect the natural immune response. Typically, these drugs impair polymorphonuclear leukocyte (PMN) production of superoxide anion, chemotaxis, or the killing of pathogens. Allylamines are a new class of antimycotic compounds with a new mechanism of antifungal action, i.e., inhibition of the fungal squalene epoxidase. The trial that we describe aimed to evaluate the effects of two allylamines, terbinafine and naftifine, on selected functions of PMNs, i.e., superoxide anion production, chemotaxis, and killing of Candida albicans blastospores. Terbinafine and naftifine on their own did not affect superoxide anion production when they were added to PMNs. When PMNs were preincubated with allylamines and were then stimulated by N-formyl-Met-Leu-Phe or phorbol 12-myristate 13-acetate, superoxide anion production was increased (priming effect). Since intracellular free calcium (Ca2+i) is involved in the control of superoxide anion production, we evaluated the effects of the allylamines on the Ca2+i concentration ([Ca2+]i). In the presence of terbinafine or naftifine, the [Ca2+]i increased in a dose-dependent manner; the source of Ca2+i was not extracellular since it was not affected by extracellular calcium chelation with ethylene glycol-bis(beta-aminoethyl ether)-N,N,N',N'-tetraacetic acid. In the presence of terbinafine or naftifine, chemotaxis of PMNs was not impaired. Terbinafine and naftifine slightly but significantly increased the killing of C. albicans blastospores (P < 0.05 at 10 and 100 microM). In conclusion, in contrast to imidazole-like drugs, the allylamine antimycotic compounds terbinafine and naftifine enhance selected functions of PMNs.
许多抗真菌药物会对天然免疫反应产生负面影响。通常,这些药物会损害多形核白细胞(PMN)产生超氧阴离子的能力、趋化性或杀灭病原体的能力。烯丙胺类是一类新型抗真菌化合物,具有全新的抗真菌作用机制,即抑制真菌角鲨烯环氧酶。我们所描述的这项试验旨在评估两种烯丙胺类药物,特比萘芬和萘替芬,对PMN特定功能的影响,即超氧阴离子的产生、趋化性以及对白色念珠菌芽生孢子的杀灭作用。当将特比萘芬和萘替芬单独添加到PMN中时,它们自身并不会影响超氧阴离子的产生。当PMN与烯丙胺类药物预孵育,然后用N-甲酰甲硫氨酰亮氨酰苯丙氨酸或佛波醇12-肉豆蔻酸酯13-乙酸酯刺激时,超氧阴离子的产生会增加(启动效应)。由于细胞内游离钙(Ca2+i)参与超氧阴离子产生的调控,我们评估了烯丙胺类药物对Ca2+i浓度([Ca2+]i)的影响。在存在特比萘芬或萘替芬的情况下,[Ca2+]i呈剂量依赖性增加;Ca2+i的来源并非细胞外,因为它不受乙二醇双(β-氨基乙基醚)-N,N,N',N'-四乙酸对细胞外钙的螯合作用影响。在存在特比萘芬或萘替芬的情况下,PMN的趋化性并未受损。特比萘芬和萘替芬略微但显著地增强了对白色念珠菌芽生孢子的杀灭作用(在10和100微摩尔时P < 0.05)。总之,与咪唑类药物不同,烯丙胺类抗真菌化合物特比萘芬和萘替芬增强了PMN的特定功能。