Bezerra da Silva Cristiane, Pott Arnildo, Elifio-Esposito Selene, Dalarmi Luciane, Fialho do Nascimento Kátia, Moura Burci Ligia, de Oliveira Maislian, de Fátima Gaspari Dias Josiane, Warumby Zanin Sandra Maria, Gomes Miguel Obdulio, Dallarmi Miguel Marilis
Department of Pharmacy, Federal University of Paraná (UFPR), Av. Pref. Lothário Meissner 3400, Jardim Botânico, Curitiba 80210-170, Brazil.
Department of Biology, Federal University of Mato Grosso do Sul (UFMS), Av. Senador Filinto Müller, Campo Grande 79046-460, Brazil.
Molecules. 2016 Jan 11;21(1):53. doi: 10.3390/molecules21010053.
Dugesia tigrina is a non-parasitic platyhelminth, which has been recently utilized in pharmacological models, regarding the nervous system, as it presents a wide sensitivity to drugs. Our trials aimed to propose a model for an in vivo screening of substances with inhibitory activity of the enzyme acetylcholinesterase. Trials were performed with four drugs commercialized in Brazil: donepezil, tacrine, galantamine and rivastigmine, utilized in the control of Alzheimer's disease, to inhibit the activity of acetylcholinesterase. We tested five concentrations of the drugs, with an exposure of 24 h, and the mortality and the inhibition of acetylcholinesterase planarian seizure-like activity (pSLA) and planarian locomotor velocity (pLMV) were measured. Galantamine showed high anticholinesterasic activity when compared to the other drugs, with a reduction of 0.05 μmol·min(-1) and 63% of convulsant activity, presenting screw-like movement and hypokinesia, with pLMV of 65 crossed lines during 5 min. Our results showed for the first time the anticholinesterasic and convulsant effect, in addition to the decrease in locomotion induced by those drugs in a model of invertebrates. The experimental model proposed is simple and low cost and could be utilized in the screening of substances with anticholinesterasic action.
虎纹涡虫是一种非寄生性扁形虫，由于其对药物具有广泛的敏感性，最近已被用于有关神经系统的药理模型中。我们的试验旨在提出一种体内筛选具有乙酰胆碱酯酶抑制活性物质的模型。试验使用了在巴西商业化的四种药物：多奈哌齐、他克林、加兰他敏和卡巴拉汀，这些药物用于控制阿尔茨海默病，以抑制乙酰胆碱酯酶的活性。我们测试了五种药物浓度，暴露24小时，并测量死亡率以及对乙酰胆碱酯酶涡虫癫痫样活动（pSLA）和涡虫运动速度（pLMV）的抑制作用。与其他药物相比，加兰他敏显示出高抗胆碱酯酶活性，惊厥活性降低0.05 μmol·min⁻¹和63%，呈现螺旋状运动和运动减退，5分钟内pLMV为65条交叉线。我们的结果首次显示了这些药物在无脊椎动物模型中的抗胆碱酯酶和惊厥作用，以及对运动的降低作用。所提出的实验模型简单且成本低，可用于筛选具有抗胆碱酯酶作用的物质。
