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聚乳酸-羟基乙酸共聚物微球包裹(-)-荜澄茄素用于急性期治疗的体内外杀锥虫活性评价

In Vivo and in Silico Trypanocidal Activity Evaluation of (-)-Cubebin Encapsulated in PLGA Microspheres as Potential Treatment in Acute Phase.

机构信息

Núcleo de Pesquisas em Ciências Exatas e Tecnológicas, Universidade de Franca, 14404-600, Franca-SP, Brazil.

出版信息

Chem Biodivers. 2021 Jun;18(6):e2100052. doi: 10.1002/cbdv.202100052. Epub 2021 Apr 27.

DOI:10.1002/cbdv.202100052
PMID:33905595
Abstract

In this study, the trypomastigotes of a Y strain of Trypanosoma cruzi were inoculated intraperitoneally into male BALB/c mice weighing approximately 25 g each, which were divided into groups for evaluation of the trypanocidal activity. For the treatment of experimental groups, encapsulated and unencapsulated (-)-cubebin, Benznidazole, and two groups as negative controls were used. The encapsulated (-)-cubebin showed a 68.1 % encapsulation efficiency. The parasitemia peak of substances remained around the 9 day after the observed reduction in the number of circulating trypomastigotes. The encapsulated (-)-cubebin and (-)-cubebin unloaded showed a decrease of 61.3 % and 58.5 % in the number of parasites as compared to the negative control, respectively. Moreover, animals treated with encapsulated (-)-cubebin had a higher survival time as compared to the other groups. In conclusion, the results obtained were more promising for encapsulated (-)-cubebin as compared to unloaded particles.

摘要

在这项研究中,将一株克氏锥虫 Y 株的锥虫感染到每只体重约 25 克的雄性 BALB/c 小鼠的腹腔内,将这些小鼠分为几组,以评估杀锥虫活性。为了治疗实验组,使用了包封和未包封的(-)-胡椒碱、苯并咪唑和两组阴性对照。封装的(-)-胡椒碱的封装效率为 68.1%。在观察到循环锥虫数量减少后,物质的寄生虫血症峰值仍保持在第 9 天左右。与阴性对照组相比,封装的(-)-胡椒碱和未加载的(-)-胡椒碱的寄生虫数量分别减少了 61.3%和 58.5%。此外,用封装的(-)-胡椒碱治疗的动物的存活时间比其他组更长。总之,与未加载的颗粒相比,封装的(-)-胡椒碱的结果更有希望。

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