4-氨甲基苯氧基苯并硼唑 AN3057 作为原发性阿米巴脑膜脑炎的潜在治疗选择。
The 4-Aminomethylphenoxy-Benzoxaborole AN3057 as a Potential Treatment Option for Primary Amoebic Meningoencephalitis.
机构信息
Department of Parasitology, Faculty of Science, Charles University, BIOCEV, Vestec, Czech Republic.
Institute of Biotechnology, Czech Academy of Sciences, BIOCEV, Vestec, Czech Republic.
出版信息
Antimicrob Agents Chemother. 2023 Feb 16;67(2):e0150622. doi: 10.1128/aac.01506-22. Epub 2023 Jan 23.
Abstract
Primary amoebic meningoencephalitis is a rare but fatal central nervous system (CNS) disease caused by the "brain-eating amoeba" Naegleria fowleri. A major obstacle is the requirement for drugs with the ability to cross the blood-brain barrier, which are used in extremely high doses, cause severe side effects, and are usually ineffective. We discovered that the 4-aminomethylphenoxy-benzoxaborole AN3057 exhibits nanomolar potency against N. fowleri, and experimental treatment of infected mice significantly prolonged survival and demonstrated a 28% relapse-free cure rate.
摘要
原发性阿米巴脑膜脑炎是一种罕见但致命的中枢神经系统（CNS）疾病，由“食脑变形虫”福氏耐格里阿米巴引起。主要障碍是需要具有穿透血脑屏障能力的药物，这些药物需要以极高的剂量使用，会引起严重的副作用，而且通常无效。我们发现 4-氨甲基苯氧基苯并恶硼烷 AN3057 对福氏耐格里阿米巴具有纳摩尔效力，对感染小鼠的实验性治疗显著延长了存活时间，并显示出 28%的无复发治愈率。
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