In vitro and in vivo cysticidal activity of extracts and isolated flavanone from the bark of Prunus serotina: A bio-guided study

• Published in: Acta tropica 2017-06, Vol.170, p.1-7
• Main Authors: 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
• Format: Article
• Language: English
• Subjects: 2,3-Dihydro-5,7-dihydroxy-2-(4-hydroxyphenyl)-4H-1-benzopyran-4-one [naringenin]; Albendazole - pharmacology; Animals; Anthelmintics - pharmacology; Cysticercosis - drug therapy; Cysticidal activity; Female; Flavanones - pharmacology; Mice; Mice, Inbred BALB C; Plant Extracts - pharmacology; Prunus avium; Prunus serotina; Selectivity index; Taenia - drug effects; Taenia crassiceps cysts
• ISSN: 0001-706X; 1873-6254
• DOI: 10.1016/j.actatropica.2017.02.023

The present paper reports the activity of Prunus serotina against Taenia crassiceps cysts and the isolation and identification of naringenin as the main active compound. [Display omitted] •The in vitro cysticidal activity of extracts from P. serotina was demonstrated.•The methanolic extract of P. serotina exhibited in vivo activity.•Naringenin was isolated and identified as the main active compound of P. serotina.•The in vivo efficacy of naringenin was similar to that obtained with albendazole. 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 (EC50=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 (EC50=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.