Instituto de Patología Experimental, Facultad de Ciencias de la Salud, Universidad Nacional de Salta-CONICET, Salta 4400, Argentina.
Department of Parasitology, Kochi Medical School, Kochi University, Okocho Kohasu, Nankoku, Kochi Prefecture 783-8505, Japan.
Molecules. 2020 Apr 10;25(7):1741. doi: 10.3390/molecules25071741.
The treatment of leishmaniasis includes pentavalent antimony drugs but, because of the side effects, toxicity and cases of treatment failure or resistance, the search of new antileishmanial compounds are necessary. The aims of this study were to evaluate and compare the in vitro antileishmanial activity of four green tea catechins, and to assess the efficacy of topical (-)-epigallocatechin gallate in a cutaneous leishmaniasis model. The antileishmanial activity of green tea catechins was evaluated against intracellular amastigotes, and cytotoxicity was performed with human monocytic cell line. BALB/c mice were infected in the ear dermis with and treated with topical 15% (-)-epigallocatechin gallate, intraperitoneal Glucantime, and control group. The efficacy of treatments was evaluated by quantifying the parasite burden and by measuring the lesions size. (-)-Epigallocatechin gallate and (-)-epigallocatechin were the most active compounds with IC values <59.6 µg/mL and with a selectivity index >1. Topical treatment with (-)-epigallocatechin gallate decreased significantly both lesion size and parasite burden (80.4% inhibition) compared to control group (p < 0.05), and moreover (-)-epigallocatechin gallate showed a similar efficacy to Glucantime (85.1% inhibition), the reference drug for leishmaniasis treatment.
利什曼病的治疗包括五价锑药物,但由于副作用、毒性和治疗失败或耐药的情况,因此需要寻找新的抗利什曼化合物。本研究的目的是评估和比较四种绿茶儿茶素的体外抗利什曼原虫活性,并评估局部(-)-表没食子儿茶素没食子酸酯在皮肤利什曼病模型中的疗效。绿茶儿茶素的抗利什曼原虫活性通过检测细胞内无鞭毛体进行评估,并用人单核细胞系进行细胞毒性检测。BALB/c 小鼠在耳部皮肤感染并接受局部 15%(-)-表没食子儿茶素没食子酸酯、腹腔注射葡萄糖酸锑钠和对照组治疗。通过定量寄生虫负荷和测量病变大小来评估治疗效果。(-)-表没食子儿茶素没食子酸酯和(-)-表没食子儿茶素是最有效的化合物,IC 值<59.6µg/mL,选择性指数>1。与对照组相比,局部应用(-)-表没食子儿茶素没食子酸酯显著降低了病变大小和寄生虫负荷(80.4%抑制)(p<0.05),而且(-)-表没食子儿茶素没食子酸酯与葡萄糖酸锑钠(85.1%抑制)的疗效相似,后者是治疗利什曼病的参考药物。