Olaya María Del Pilar, Vergel Nadezdha Esperanza, López José Luis, Viña María Dolores, Guerrero Mario Francisco
Departamento de Farmacia, Facultad de Ciencias, Universidad Nacional de Colombia, Bogotá, D.C., Colombia.
Biomedica. 2019 Sep 1;39(3):491-501. doi: 10.7705/biomedica.4299.
Parkinson's disease is the second most common neurodegenerative disease. Monoamine oxidase B inhibitors are used in the treatment of this disease concomitantly with levodopa or as monotherapy. Several substituted coumarins have shown activity as inhibitors of monoamine oxidase B.
To evaluate the possible antiparkinsonian effects of the coumarin analogue FCS005 (3-methyl-7H-furo[3,2-g]chromen-7-one) in mouse models, as well as its inhibitory activity towards monoamine oxidases (MAO) and its antioxidant activity.
FCS005 was synthesized and the reversal of hypokinesia was evaluated in the reserpine and levodopa models. Moreover, in the haloperidol model, its anticataleptic effects were evaluated. Additionally, the monoamine oxidase inhibitory activity and antioxidant activity of FCS005 were evaluated using in vitro and ex vivo studies, respectively.
FCS005 (100 mg/kg) caused the reversal of hypokinesia in the reserpine and levodopa models. This furocoumarin also presented anti-cataleptic effects at the same dose. Besides, it showed selective inhibitory activity towards the MAO-B isoform and antioxidant activity.
These results attribute interesting properties to the compound FCS005. It is important to continue research on this molecule considering that it could be a potential antiparkinsonian agent.
帕金森病是第二常见的神经退行性疾病。单胺氧化酶B抑制剂可与左旋多巴联合使用或作为单一疗法用于治疗该疾病。几种取代香豆素已显示出作为单胺氧化酶B抑制剂的活性。
评估香豆素类似物FCS005（3-甲基-7H-呋喃并[3,2-g]色烯-7-酮）在小鼠模型中可能的抗帕金森病作用，以及其对单胺氧化酶（MAO）的抑制活性和抗氧化活性。
合成FCS005，并在利血平和左旋多巴模型中评估运动迟缓的逆转情况。此外，在氟哌啶醇模型中评估其抗僵住效应。另外，分别通过体外和体内研究评估FCS005的单胺氧化酶抑制活性和抗氧化活性。
FCS005（100mg/kg）在利血平和左旋多巴模型中引起运动迟缓的逆转。这种呋喃香豆素在相同剂量下也表现出抗僵住效应。此外，它对MAO-B同工型表现出选择性抑制活性和抗氧化活性。
这些结果赋予了化合物FCS005有趣的特性。鉴于它可能是一种潜在的抗帕金森病药物，继续对该分子进行研究很重要。
