Abstract：
OBJECTIVE: To determine the anti-amoebic activity of benzofuran/benzothiophene-possessing compounds against Acanthamoeba castellanii of the T4 genotype.
RESULTS: A series of benzofuran/benzothiophene-possessing compounds were tested for their anti-amoebic activities, in particular, to block encystation and excystation processes in amoebae. Cytotoxicity of the compounds were evaluated using lactate dehydrogenase (LDH) assays. The amoebicidal assay results revealed significant anti-amoebic effects against A. castellanii. Compounds 1p and 1e showed the highest amoebicidal activity, eliminating 68% and 64% of the amoebae, respectively. These compounds remarkably repressed both the encystation and excystation processes in A. castellanii. Furthermore, the selected compounds presented minimal cytotoxic properties against human cells, as well as considerably abridged amoeba-mediated cytopathogenicity when compared to the amoebae alone.
CONCLUSIONS: Our findings show that benzofuran/benzothiophene derivatives depict potent anti-amoebic activities; thus these compounds should be used as promising and novel agents in the rationale development of therapeutic strategies against Acanthamoeba infections.
RESULTS: A series of benzofuran/benzothiophene-possessing compounds were tested for their anti-amoebic activities, in particular, to block encystation and excystation processes in amoebae. Cytotoxicity of the compounds were evaluated using lactate dehydrogenase (LDH) assays. The amoebicidal assay results revealed significant anti-amoebic effects against A. castellanii. Compounds 1p and 1e showed the highest amoebicidal activity, eliminating 68% and 64% of the amoebae, respectively. These compounds remarkably repressed both the encystation and excystation processes in A. castellanii. Furthermore, the selected compounds presented minimal cytotoxic properties against human cells, as well as considerably abridged amoeba-mediated cytopathogenicity when compared to the amoebae alone.
CONCLUSIONS: Our findings show that benzofuran/benzothiophene derivatives depict potent anti-amoebic activities; thus these compounds should be used as promising and novel agents in the rationale development of therapeutic strategies against Acanthamoeba infections.
摘要：
目的：测定含苯并呋喃/苯并噻吩的化合物对T4基因型棘阿米巴的抗阿米巴活性。
结果：测试了一系列具有苯并呋喃/苯并噻吩的化合物的抗阿米巴活性，特别是,阻止变形虫的包藏和灭绝过程。使用乳酸脱氢酶(LDH)测定法评价化合物的细胞毒性。杀变形虫试验结果揭示了对卡氏A.castellanii的显著抗阿米巴作用。化合物1p和1e显示出最高的杀阿米巴活性，消除了68%和64%的变形虫，分别。这些化合物显着抑制了A.castellanii的包封和脱落过程。此外，选定的化合物对人类细胞具有最小的细胞毒性，与单独的变形虫相比，变形虫介导的细胞致病性也大大减弱。
结论：我们的研究结果表明，苯并呋喃/苯并噻吩衍生物具有有效的抗阿米巴活性；因此，这些化合物应作为有希望的新型药物用于开发针对棘阿米巴感染的治疗策略。
结果：测试了一系列具有苯并呋喃/苯并噻吩的化合物的抗阿米巴活性，特别是,阻止变形虫的包藏和灭绝过程。使用乳酸脱氢酶(LDH)测定法评价化合物的细胞毒性。杀变形虫试验结果揭示了对卡氏A.castellanii的显著抗阿米巴作用。化合物1p和1e显示出最高的杀阿米巴活性，消除了68%和64%的变形虫，分别。这些化合物显着抑制了A.castellanii的包封和脱落过程。此外，选定的化合物对人类细胞具有最小的细胞毒性，与单独的变形虫相比，变形虫介导的细胞致病性也大大减弱。
结论：我们的研究结果表明，苯并呋喃/苯并噻吩衍生物具有有效的抗阿米巴活性；因此，这些化合物应作为有希望的新型药物用于开发针对棘阿米巴感染的治疗策略。
