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Biological evaluation of four selected African medicinal plants for their trypanocidal properties, mode of action, and chemical compounds.

机译：对四种选定的非洲药用植物的锥虫杀灭特性，作用方式和化合物的生物学评估。

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摘要

Extracts of Anogeissus leiocarpus, Fagara zanthoxyloides, Pseudocedrela kotschyi, and Terminalia glaucescens were evaluated for their in vitro antiproliferative properties against Trypanosoma cruzi and for cytotoxicity on control NIH 3T3 fibroblast cells. The methanol root bark extract of A.leiocarpus showed a significantly higher potency (IC50 = 0.82 mug/ml) than the other three extracts and nifurtimox, which was used as a positive control. However, no significant differences in the antitrypanosomal activity were found among the other three treatments. F.zanthoxyloides had an IC50 of 6.42 mug/ml. P.kotschyi showed an IC50 of 8.94 mug/ml, with 9.04 mug/ml for T.glaucescens and 7.70 mug/ml for nifurtimox. The cytoxicity experiments indicated that extracts of A. leiocarpus and P.kotschyi are significantly less toxic for fibroblasts than extracts of F.zanthoxyloides, T.glaucescens and nifurtimox. The oral acute toxicity results revealed that methanol extracts of A.leiocarpus and P.kotschyi were also not toxic in BAL/C mice, as aspartate aminotransferase (AST) and alanine aminotransferase (ALT) measurements were within normal ranges. A.leiocarpus and P.kotschyi extracts were, therefore, selected for subsequent experiments because of their higher selectivity values. Also treatment of T.cruzi epimastigotes with the extracts yielded minimum inhibitory concentrations (MICs) of 36.82 mug/ml for A.leiocarpus and 540 mug/ml for P.kotschyi. The results of other experiments indicated that the trypanocidal activity of the extracts may be mediated by apoptosis, as evident from the demonstration of in situ DNA nicking of treated parasites, the detection of a caspase-3 like activity and the externalization of phosphatidylserine on surface membranes of treated parasites. Morphological studies by electron microscopy showed swelling of surface membrane and disruption of the flagellum in parasites that were treated with the two extracts. These results collectively demonstrate that A.leiocarpus and P.kotschyi extracts are very active against T.cruzi and should be considered as sources for the isolation of potential anti-trypanosomal compounds.
机译：评估了黑皮芦荟，Fagara zanthoxyloides，Pseudocedrela kotschyi和Terminalia glaucescens的提取物对克鲁斯锥虫的体外抗增殖特性以及对对照NIH 3T3成纤维细胞的细胞毒性。面包果的甲醇根皮提取物显示出比其他三种提取物和硝呋替莫斯更高的效价（IC50 = 0.82杯/毫升），后者被用作阳性对照。但是，在其他三种治疗方法中，抗胰锥虫活性没有显着差异。 F.zanthoxyloides的IC50为6.42杯/毫升。 P.kotschyi的IC50为8.94马克杯/毫升，其中T.glaucescens的IC50为9.04马克杯/毫升，硝呋替莫为7.70马克杯/毫升。细胞毒性实验表明，比起F.zanthoxyloides，T.glaucescens和nifurtimox的提取物，紫果曲霉和科奇奇的提取物对成纤维细胞的毒性要小得多。口服急性毒性结果表明，由于天门冬氨酸转氨酶（AST）和丙氨酸转氨酶（ALT）的测定均在正常范围内，因此，A.leiocarpus和P.kotschyi的甲醇提取物对BAL / C小鼠也无毒性。因此，由于其较高的选择性，因此选择了椰果和科奇奇提取物进行后续实验。同样，用提取物处理克鲁氏短鞭毛虫的最小抑菌浓度（MIC）对油果阿胶菌为36.82杯/毫升，对科氏假单胞菌为540杯/毫升。其他实验结果表明，提取物的锥虫杀伤活性可能是由细胞凋亡介导的，这可以从处理过的寄生虫的原位DNA切口证明，caspase-3样活性的检测以及表面磷脂酰丝氨酸的外在化中得到证明。治疗的寄生虫。通过电子显微镜进行的形态学研究表明，用两种提取物处理过的寄生虫中，其表面膜肿胀和鞭毛破裂。这些结果共同证明，沙棘果和P.kotschyi提取物对克鲁兹酵母非常有活性，应被视为分离潜在抗锥虫化合物的来源。

著录项

  • 作者

    Kenguele, Hilaire Moundounga.;

  • 作者单位

    Howard University.;

  • 授予单位 Howard University.;
  • 学科 Biology Parasitology.
  • 学位 Ph.D.
  • 年度 2009
  • 页码 129 p.
  • 总页数 129
  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类
  • 关键词

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