Giresun University Faculty of Medicine, Department of Medical Microbiology, Giresun, Turkey.
Karadeniz Technical University Faculty of Science, Department of Chemistry, Trabzon, Turkey.
Turkiye Parazitol Derg. 2020 Dec 2;44(4):216-220. doi: 10.4274/tpd.galenos.2020.6900.
Leishmaniasis is an important parasitic disease in many countries, including ours. A variety of drugs are currently used for its treatment. However, certain side effects of these drugs, such as teratogenicity, hepatotoxicity and nephrotoxicity, have been reported in some patients. The goal of this research is to determine the antileishmanial effects of eight different previously synthesised compounds containing Schiff and Mannich bases (morpholine) against promastigotes by the liquid microdilution method utilising alamarBlue.
Compounds containing Schiff bases (a-d) and both Schiff bases and morpholine rings (e-h) were tested. Compounds were diluted in the range of 20000-39 μg/mL. promastigotes were added to the wells, which were then incubated at 27 °C. The proliferation of Leishmania promastigotes was evaluated after 24, 48 and 72 hours.
In this study, compounds b, c and d (MIC values 156 μg/mL, 78 μg/mL and 156 μg/mL) were found to be effective against promastigotes, whereas compound f (MIC >20000 μg/mL) was found to be more the most ineffective compound.
These compounds may be potential drug candidates for the treatment of leishmaniasis. According to the results, there is a need for further studies, such as in vivo experimental animal models and amastigote macrophage cultures for compounds showing antileishmanial effects.
利什曼病是包括我国在内的许多国家的一种重要寄生虫病。目前有多种药物用于治疗该病，但这些药物存在一定的副作用，如致畸性、肝毒性和肾毒性等，在一些患者中已有报道。本研究旨在通过利用 alamarBlue 的液体微量稀释法，测定 8 种不同的含席夫碱和曼尼希碱（吗啡啉）的合成化合物对前鞭毛体的抗利什曼原虫作用。
测试了含席夫碱的化合物（a-d）和含席夫碱和吗啡啉环的化合物（e-h）。化合物在 20000-39μg/mL 的范围内稀释。将前鞭毛体加入孔中，然后在 27°C 下孵育。在 24、48 和 72 小时后评估利什曼原虫前鞭毛体的增殖情况。
在这项研究中，化合物 b、c 和 d（MIC 值分别为 156μg/mL、78μg/mL 和 156μg/mL）被发现对前鞭毛体有效，而化合物 f（MIC＞20000μg/mL）则被发现最无效。
这些化合物可能是治疗利什曼病的潜在药物候选物。根据结果，需要进一步研究，例如在体内实验动物模型和显示抗利什曼原虫作用的巨噬细胞内阿米巴培养物中进行研究。
