PDF(Pubmed)
Abstract：
Natural products play a significant role in providing the current demand as antiparasitic agents, which offer an attractive approach for the discovery of novel drugs. The present study aimed to evaluate in vitro the potential impact of seaweed Padina pavonica (P. pavonica) extract in combating Acanthamoeba castellanii (A. castellanii). The phytochemical constituents of the extract were characterized by Gas chromatography-mass spectrometry. Six concentrations of the algal extract were used to evaluate its antiprotozoal activity at various incubation periods. Our results showed that the extract has significant inhibition against trophozoites and cysts viability, with complete inhibition at the high concentrations. The IC50 of P. pavonica extract was 4.56 and 4.89 µg/mL for trophozoites and cysts, respectively, at 24 h. Morphological alterations of A. castellanii trophozoites/cysts treated with the extract were assessed using inverted and scanning electron microscopes and showed severe damage features upon treatment with the extract at different concentrations. Molecular Docking of extracted compounds against Acanthamoeba cytochrome P450 monooxygenase (AcCYP51) was performed using Autodock vina1.5.6. A pharmacokinetic study using SwissADME was also conducted to investigate the potentiality of the identified bioactive compounds from Padina extract to be orally active drug candidates. In conclusion, this study highlights the in vitro amoebicidal activity of P. pavonica extract against A. castellanii adults and cysts and suggests potential AcCYP51 inhibition.
摘要：
天然产物在提供抗寄生虫剂的当前需求方面发挥着重要作用，这为新药的发现提供了一种有吸引力的方法。本研究旨在体外评估海藻Padinapavonica的潜在影响(P.pavonica）提取物在对抗棘阿米巴castellanii（A.卡斯特拉尼）。采用气相色谱-质谱法对提取物的植物化学成分进行了表征。使用六种浓度的藻类提取物在不同的孵育期评估其抗原生动物活性。我们的结果表明，提取物对滋养体和囊肿的活力有显著的抑制作用，在高浓度下完全抑制。pavonica提取物的IC50为4.56和4.89µg/mL的滋养体和囊肿，分别,在24小时。使用倒置和扫描电子显微镜评估用提取物处理的A.castellanii滋养体/囊肿的形态变化，并在用不同浓度的提取物处理后显示出严重的损伤特征。使用Autodockvina1.5.6进行提取的化合物对棘阿米巴细胞色素P450单加氧酶（AcCYP51）的分子对接。还进行了使用SwissADME的药代动力学研究，以调查从Padina提取物中鉴定的生物活性化合物作为口服活性药物候选物的潜力。总之,这项研究强调了巴文草提取物对卡氏A.castellanii成虫和囊肿的体外杀变形虫活性，并提出了潜在的AcCYP51抑制作用。
