Institute for Medical Microbiology, Immunology and Parasitology, University Hospital Bonn, Venusberg-Campus 1, 53127, Bonn, Germany; German Center for Infection Research (DZIF), Partner Site Bonn-Cologne, Bonn, Germany.
Griffin Institute (formerly Northwick Park Institute for Medical Research), London, HA1 3UJ, United Kingdom.
Int J Parasitol Drugs Drug Resist. 2021 Dec;17:27-35. doi: 10.1016/j.ijpddr.2021.07.005. Epub 2021 Jul 28.
Filariae are vector-borne nematodes responsible for an enormous burden of disease. Human lymphatic filariasis, caused by Wuchereria bancrofti, Brugia malayi, and Brugia timori, and onchocerciasis (caused by Onchocerca volvulus) are neglected parasitic diseases of major public health significance in tropical regions. To date, therapeutic efforts to eliminate human filariasis have been hampered by the lack of a drug with sufficient macrofilaricidal and/or long-term sterilizing effects that is suitable for use in mass drug administration (MDA) programs, particularly in areas co-endemic with Loa loa, the causative agent of loiasis. Emodepside, a semi-synthetic cyclooctadepsipeptide, has been shown to have broad-spectrum efficacy against gastrointestinal nematodes in a variety of mammalian hosts, and has been approved as an active ingredient in dewormers for cats and dogs. This paper evaluates, compares (where appropriate) and summarizes the in vitro effects of emodepside against a range of filarial nematodes at various developmental stages. Emodepside inhibited the motility of all tested stages of filariae frequently used as surrogate species for preclinical investigations (Acanthocheilonema viteae, Brugia pahangi, Litomosoides sigmodontis, Onchocerca gutturosa, and Onchocerca lienalis), human-pathogenic filariae (B. malayi) and filariae of veterinary importance (Dirofilaria immitis) in a concentration-dependent manner. While motility of all filariae was inhibited, both stage- and species-specific differences were observed. However, whether these differences were detected because of stage- and/or species-specific factors or as a consequence of variations in protocol parameters among the participating laboratories (such as purification of the parasites, read-out units, composition of media, incubation conditions, duration of incubation etc.) remains unclear. This study, however, clearly shows that emodepside demonstrates broad-spectrum in vitro activity against filarial nematode species across different genera and can therefore be validated as a promising candidate for the treatment of human filariases, including onchocerciasis and lymphatic filariasis.
丝虫是一种通过媒介传播的线虫,会导致巨大的疾病负担。由班氏吴策线虫、马来布鲁线虫和帝汶布鲁线虫引起的人类淋巴丝虫病,以及由盘尾丝虫引起的盘尾丝虫病(河盲症),是热带地区具有重要公共卫生意义的被忽视寄生虫病。迄今为止,由于缺乏具有足够的杀微丝蚴和/或长期绝育效果的药物,用于大规模药物治疗(MDA)计划的治疗工作受到了阻碍,特别是在与罗阿罗阿(引起罗阿丝虫病的病原体)共同流行的地区。埃莫德匹肽是一种半合成的环八肽,已被证明对多种哺乳动物宿主的胃肠道线虫具有广谱疗效,并已被批准作为猫和狗驱虫剂的有效成分。本文评估、比较(在适当的情况下)和总结了埃莫德匹肽对不同发育阶段的一系列丝虫的体外作用。埃莫德匹肽以浓度依赖的方式抑制了经常用作临床前研究替代物种的丝虫的所有测试阶段的运动(旋尾丝虫、布氏犬丝虫、链尾丝虫、埃及盘尾丝虫和奥氏盘尾丝虫)、人类致病性丝虫(马来布鲁线虫)和兽医重要的丝虫(犬恶丝虫)。虽然所有丝虫的运动都受到抑制,但观察到了阶段和物种特异性差异。然而,这些差异是由于阶段和/或物种特异性因素还是由于参与实验室之间的方案参数变化(例如寄生虫的纯化、读数单位、培养基成分、孵育条件、孵育时间等)引起的,尚不清楚。然而,本研究清楚地表明,埃莫德匹肽对不同属的丝虫具有广谱的体外活性,因此可以作为治疗人类丝虫病(包括盘尾丝虫病和淋巴丝虫病)的有前途的候选药物进行验证。