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NIAID Data Ecosystem2026-05-01 收录
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https://figshare.com/articles/dataset/S1_Data_-/22780956
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资源简介:
Algal extracts are sources of bioactive substances with applications in the development of novel alternative drugs against several diseases, including trichomoniasis sexually transmitted infection caused by Trichomonas vaginalis. Factors such as clinical failures and resistant strains limit the success of the existing drugs available for treating this disease. Therefore, searching for viable alternatives to these drugs is essential for the treatment of this disease. The present study was conducted for, in vitro and in silico characterization of extracts obtained from marine macroalgae Gigartina skottsbergii at stages gametophidic, cystocarpic, and tetrasporophidic. In addition, antiparasitic activity of these extracts against the ATCC 30236 isolate of T. vaginalis, their cytotoxicity, and gene expression of trophozoites after treatment were evaluated. The minimum inhibitory concentration and 50% inhibition concentration were determined for each extract. Results: In vitro analysis of the extracts’ anti-T. vaginalis activity revealed an inhibitory effect of 100%, 89.61%, and 86.95% for Gigartina skottsbergii at stages gametophidic, cystocarpic, and tetrasporophidic, respectively, at 100 μg/mL. In silico analysis revealed the interactions between constituents of the extracts and enzymes from T. vaginalis, with significant free energy values obtained for the binding. None of the extract concentrations exhibited cytotoxic effects on VERO cell line compared to control, while cytotoxicity on HMVII vaginal epithelial cells line was observed at 100 μg/mL (30% inhibition). Gene expression analysis revealed differences in the expression profile of T. vaginalis enzymes between the extract-treated and control groups. According to these results, Gigartina skottsbergii extracts exhibited satisfactory antiparasitic activity.

藻类提取物是多种生物活性物质的来源,可用于开发针对多种疾病的新型替代药物,其中包括由阴道毛滴虫(Trichomonas vaginalis)引发的性传播感染——滴虫病。临床治疗失败与耐药菌株等因素,制约了当前用于治疗该疾病的现有药物的应用效果。因此,寻找安全可行的药物替代方案,对该疾病的治疗而言至关重要。本研究针对采集自处于配子体、果孢子体及四分孢子体阶段的海洋大型藻类斯科茨比杉藻(Gigartina skottsbergii)的提取物,开展了体外(in vitro)与计算机模拟(in silico)表征分析。此外,本研究还评估了这些提取物针对阴道毛滴虫ATCC 30236分离株的抗寄生虫活性、细胞毒性,以及给药后滋养体(trophozoite)的基因表达情况,并测定了每种提取物的最低抑菌浓度(MIC)与半数抑制浓度(IC₅₀)。研究结果:体外抗阴道毛滴虫活性分析显示,在100 μg/mL浓度下,处于配子体、果孢子体及四分孢子体阶段的斯科茨比杉藻提取物对该寄生虫的抑制率分别为100%、89.61%及86.95%。计算机模拟分析表明,提取物中的活性成分与阴道毛滴虫的酶类存在特异性结合相互作用,且结合过程的自由能值具有统计学显著性。与对照组相比,所有浓度的提取物均未对VERO细胞系产生细胞毒性;但在100 μg/mL浓度下,提取物对HMVII阴道上皮细胞系表现出细胞毒性,抑制率达30%。基因表达分析结果显示,提取物给药组与对照组的阴道毛滴虫酶类表达谱存在显著差异。综合上述实验结果可知,斯科茨比杉藻提取物展现出令人满意的抗寄生虫活性。
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2023-05-08
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