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含 4-苯丁酸的阳离子碳硅烷树枝状分子的杀阿米巴活性对棘阿米巴原虫和棘阿米巴多形虫滋养体和包囊的作用。

Amoebicidal activity of cationic carbosilane dendrons derived with 4-phenylbutyric acid against Acanthamoeba griffini and Acanthamoeba polyphaga trophozoites and cysts.

机构信息

Department of Biomedicine and Biotechnology, Faculty of Pharmacy, University of Alcalá, 28871, Alcalá de Henares, Spain.

Department of Organic and Inorganic Chemistry, Andrés M. del Río Chemistry Research Institute (IQAR), Ramón y Cajal Health Research Institute (IRYCIS), Bioengineering, Biomaterials and Nanomedicine Networking Research Center (CIBER-BBN), University of Alcalá, 28871, Madrid, Spain.

出版信息

Sci Rep. 2022 Sep 2;12(1):14926. doi: 10.1038/s41598-022-19200-w.

Abstract

Amoebae from the genus Acanthamoeba are important pathogens responsible for severe illnesses in humans such as Acanthamoeba keratitis and granulomatous amoebic encephalitis. In the last few decades, AK diagnoses have steadily increased. Most patients suffering from AK were contact lens users and the infection was related to poor hygiene. However, therapy is not yet well established, and treatments may last for several months due to resistance. Moreover, these treatments have been described to generate cytotoxicity. Therefore, there is an urgent need to develop new therapeutic strategies against AK. In this study, the amoebicidal activity of different generation cationic carbosilane dendrons derived with 4-phenylbutyric acid was demonstrated against Acanthamoeba polyphaga and Acanthamoeba griffini trophozoites and cysts. In addition, the combination of chlorhexidine digluconate and the most effective dendron (ArCOG(SNMeI)) showed an in vitro effect against Acanthamoeba trophozoites and cysts, reducing the minimal trophozoite amoebicidal concentration as well as concentrations with cysticidal activity.

摘要

棘阿米巴属的变形虫是重要的病原体,可导致人类罹患严重疾病,如棘阿米巴角膜炎和肉芽肿性阿米巴脑炎。在过去几十年中,AK 的诊断数量稳步增加。大多数患有 AK 的患者是隐形眼镜使用者,感染与卫生条件差有关。然而,目前的治疗方法尚未完善,由于耐药性的存在,治疗可能需要持续数月。此外,这些治疗方法已被描述为具有细胞毒性。因此,迫切需要开发针对 AK 的新治疗策略。在这项研究中,不同代数的带有 4-苯基丁酸的阳离子碳硅烷树状大分子对多棘阿米巴和棘阿米巴 griffini 滋养体和包囊表现出杀阿米巴活性。此外,洗必泰葡萄糖酸酯和最有效的树状大分子(ArCOG(SNMeI))的联合使用对体外滋养体和包囊具有治疗效果,降低了最小滋养体杀阿米巴浓度以及具有杀囊活性的浓度。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2b28/9440212/c683b7977791/41598_2022_19200_Fig1_HTML.jpg

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