National Research Center for Protozoan Diseases, Obihiro University of Agriculture and Veterinary Medicine, Nishi 2-13, Inada-cho, 080-8555, Obihiro, Hokkaido, Japan.
Department of Pharmacology and Therapeutics, Faculty of Veterinary Medicine, Damanhour University, Damanhour 22511, AlBeheira, Egypt.
Molecules. 2020 Jan 27;25(3):550. doi: 10.3390/molecules25030550.
() and Rhus coriaria (R. coriaria) have been documented to have various pharmacologic activities. The current study assessed the in vitro as well as in vivo inhibitory efficacy of a methanolic extract of (MEBV) and an acetone extract of R. coriaria (AERC) on six species of piroplasm parasites. The drug-exposure viability assay was tested on three different cell lines, namely mouse embryonic fibroblast (NIH/3T3), Madin-Darby bovine kidney (MDBK) and human foreskin fibroblast (HFF) cells. Qualitative phytochemical estimation revealed that both extracts containing alkaloid, tannin, saponins and terpenoids and significant amounts of flavonoids and polyphenols. The GC-MS analysis of MEBV and AERC revealed the existence of 27 and 20 phytochemical compounds, respectively. MEBV and AERC restricted the multiplication of Babesia (B.) bovis, B. bigemina, B. divergens, B. caballi, and Theileria (T.) equi at the half-maximal inhibitory concentration (IC) of 0.84 ± 0.2, 0.81 ± 0.3, 4.1 ± 0.9, 0.35 ± 0.1 and 0.68 ± 0.1 µg/mL and 85.7 ± 3.1, 60 ± 8.5, 90 ± 3.7, 85.7 ± 2.1 and 78 ± 2.1 µg/mL, respectively. In the cytotoxicity assay, MEBV and AERC inhibited MDBK, NIH/3T3 and HFF cells with half-maximal effective concentrations (EC) of 695.7 ± 24.9, 931 ± 44.9, ˃1500 µg/mL and 737.7 ± 17.4, ˃1500 and ˃1500 µg/mL, respectively. The experiments in mice showed that MEBV and AERC prohibited B. microti multiplication at 150 mg/kg by 66.7% and 70%, respectively. These results indicate the prospects of these extracts as drug candidates for piroplasmosis treatment following additional studies in some clinical cases.
()和秦皮(Rhus coriaria)已被证明具有多种药理活性。本研究评估了甲醇提取物(MEBV)和丙酮提取物(AERC)对六种梨形虫寄生虫的体外和体内抑制功效。药物暴露活力测定在三种不同的细胞系上进行,即小鼠胚胎成纤维细胞(NIH/3T3)、Madin-Darby 牛肾(MDBK)和人包皮成纤维细胞(HFF)。定性植物化学估计表明,两种提取物均含有生物碱、单宁、皂苷和萜类化合物,以及大量的类黄酮和多酚。MEBV 和 AERC 的 GC-MS 分析分别显示存在 27 和 20 种植物化学化合物。MEBV 和 AERC 将牛巴贝斯虫(B. bovis)、双芽巴贝斯虫(B. bigemina)、分歧巴贝斯虫(B. divergens)、马媾疫巴贝斯虫(B. caballi)和马媾疫锥虫(T. equi)的繁殖抑制在半最大抑制浓度(IC)为 0.84 ± 0.2、0.81 ± 0.3、4.1 ± 0.9、0.35 ± 0.1 和 0.68 ± 0.1 µg/mL 和 85.7 ± 3.1、60 ± 8.5、90 ± 3.7、85.7 ± 2.1 和 78 ± 2.1 µg/mL。在细胞毒性测定中,MEBV 和 AERC 抑制 MDBK、NIH/3T3 和 HFF 细胞的半最大有效浓度(EC)分别为 695.7 ± 24.9、931 ± 44.9、>1500 µg/mL 和 737.7 ± 17.4、>1500 和>1500 µg/mL。在小鼠实验中,MEBV 和 AERC 以 150mg/kg 剂量分别将微小巴贝斯虫的繁殖抑制了 66.7%和 70%。这些结果表明,这些提取物有希望成为梨形虫病治疗的候选药物,但需要在一些临床病例中进行进一步研究。