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Antiamoebic effects of sesquiterpene lactones isolated from the zoanthid Palythoa aff. clavata
Bioorganic Chemistry ( IF 4.5 ) Pub Date : 2021-01-27 , DOI: 10.1016/j.bioorg.2021.104682
Rubén L Rodríguez-Expósito 1 , Nathália Nocchi 2 , María Reyes-Batlle 1 , Ines Sifaoui 1 , Blanca Suárez-Gómez 2 , Ana R Díaz-Marrero 2 , Maria L Souto 2 , José E Piñero 1 , José J Fernández 2 , Jacob Lorenzo-Morales 1
Affiliation  

Opportunistic parasitic protozoa of genus Acanthamoeba are responsible to cause severe infections in humans such as Acanthamoeba Keratitis or Amoebic Granulomatous Encephalitis. Current treatments are usually toxic and inefficient and there is a need to access new therapeutic agents. The antiamoebic effects of nephthediol (1) and fourteen germacranolide and eudesmanolide sesquiterpene lactones (25, 712) isolated from the indigenous zoanthid Palythoa aff. clavata collected at the coast of Lanzarote, Canary Islands were studied against Acanthamoeba castellanii Neff, and the clinical strains A. polyphaga and A. griffini. 4-epi-arbusculin A (11) presented the lowest IC50 value (26,47 ± 1,69 µM) against A. castellanii Neff and low cytotoxicity against murine macrophages, followed by isobadgerin (2), which also showed to be active against A. castellanii Neff cysts. The studies on the mode of action of compounds 2 and 11 revealed these sesquiterpene lactones induce mechanisms of PDC on A. castellanii Neff.



中文翻译:

从 zoanthid Palythoa aff 中分离出的倍半萜内酯的抗阿米巴作用。克拉瓦塔

棘阿米巴属的机会性寄生原生动物是导致人类严重感染的原因,例如棘阿米巴角膜炎或阿米巴肉芽肿性脑炎。当前的治疗通常有毒且效率低下,因此需要获得新的治疗剂。nephthediol(的antiamoebic效果1)和14 germacranolide和eudesmanolide倍半萜内酯(2 - 57 - 12从土著zoanthid隔离)Palythoa AFF。研究了在加那利群岛兰萨罗特岛海岸收集的clavata对抗棘阿米巴卡斯泰拉尼夫,以及临床菌株A. polyphagaA. griffini。4- epi- arbusculin A ( 11 )对A. castellanii Neff 的IC 50值最低(26,47 ± 1,69 µM),对鼠巨噬细胞的细胞毒性低,其次是 isobadgerin ( 2 ),后者也显示出活性针对A. castellanii Neff 囊肿。对化合物211作用方式的研究揭示了这些倍半萜内酯在A. castellanii Neff上诱导 PDC 的机制。

更新日期:2021-02-08
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