Palomares-Alonso Francisca, Rojas-Tomé Irma Susana, Palencia Hernández Guadalupe, Jiménez-Arellanes María Adelina, Macías-Rubalcava Martha Lydia, González-Maciel Angélica, Ramos-Morales Andrea, Santiago-Reyes Rosalba, Castro Nelly, González-Hernández Iliana, Rufino-González Yadira, Jung-Cook Helgi
Laboratorio de Neuropsicofarmacología, Instituto Nacional de Neurología y Neurocirugía, Ciudad de México 14269, México.
Laboratorio de Neuropsicofarmacología, Instituto Nacional de Neurología y Neurocirugía, Ciudad de México 14269, México; Facultad de Ciencia y Tecnología, Universidad Simón Bolívar, Ciudad de México 03920, México.
Acta Trop. 2017 Jun;170:1-7. doi: 10.1016/j.actatropica.2017.02.023. Epub 2017 Feb 16.
Currently, neurocysticercosis treatment involves two drugs: albendazole and praziquantel; however, their efficacy is suboptimal and new cysticidal drugs are needed. The present paper reports the cysticidal activity of extracts of the bark from Prunus serotina against Taenia crassiceps cysts and the isolation and identification of the main components of the most active extract. Results showed that all extracts displayed in vitro cysticidal activity (EC=17.9-88.5μg/mL), being the methanolic the most active and selective. Also, methanolic extract exhibited in vivo efficacy at 300mg/kg which was similar to that obtained with albendazole. Bio-guided fractionation of methanolic extract led the isolation of 2,3-dihydro-5,7-dihydroxy-2-(4-hydroxyphenyl)-4H-1-benzopyran-4-one (naringenin, NGN), 3,4,5-trimethoxybenzoic acid and 1,3,5-trimethoxybenzene. NGN exhibited in vitro activity, in a time-concentration-dependent manner (EC=89.3μM]. Furthermore, NGN at a dose of 376.1μmol/kg displayed similar in vivo efficacy than those obtained with albendazole at 188.4μmol/kg. NGN also caused a high level of damage in all parasite tissue in a similar manner than that observed with the methanolic extract. This study represents the first report of the cysticidal properties of the bark of P. serotina. NGN was identified as the main active compound of this specie and other studies are required to explore the potential of this flavanone as cysticidal agent.
目前，神经囊尾蚴病的治疗涉及两种药物：阿苯达唑和吡喹酮；然而，它们的疗效并不理想，因此需要新的杀囊药物。本文报道了黑樱桃树皮提取物对肥胖带绦虫囊肿的杀囊活性，以及最具活性提取物主要成分的分离和鉴定。结果表明，所有提取物均表现出体外杀囊活性（EC = 17.9 - 88.5μg/mL），其中甲醇提取物活性最强且具有选择性。此外，甲醇提取物在300mg/kg剂量下表现出体内疗效，与阿苯达唑相当。对甲醇提取物进行生物导向分级分离，得到了2,3 - 二氢 - 5,7 - 二羟基 - 2 - (4 - 羟基苯基) - 4H - 1 - 苯并吡喃 - 4 - 酮（柚皮素，NGN）、3,4,5 - 三甲氧基苯甲酸和1,3,5 - 三甲氧基苯。NGN表现出体外活性，呈时间 - 浓度依赖性（EC = 89.3μM）。此外，376.1μmol/kg剂量的NGN在体内的疗效与188.4μmol/kg剂量的阿苯达唑相似。NGN对所有寄生虫组织造成的损伤程度也与甲醇提取物相似。本研究首次报道了黑樱桃树皮的杀囊特性。NGN被确定为该物种的主要活性化合物，还需要进一步研究以探索这种黄酮类化合物作为杀囊剂的潜力。
