Antiviral escin derivatives from the seeds of Aesculus turbinata Blume (Japanese horse chestnut).
Bioorg Med Chem Lett
; 27(13): 3019-3025, 2017 07 01.
Article
em En
| MEDLINE
| ID: mdl-28527823
ABSTRACT
Porcine epidemic diarrhea virus (PEDV) causes severe diarrhea and high fatality of piglets, influencing the swine industry. Japanese horse chestnut (seed of Aesculus turbinata) contains many saponin mixtures, called escins, and has been used for a long time as a traditional medicinal plant. Structure-activity relationship (SAR) studies on escins have revealed that acylations at C-21 and C-22 with angeloyl or tigloyl groups were important for their cytotoxic effects. However, the strong cytotoxicity of escins makes them hard to utilize for other diseases and to develop as nutraceuticals. In this research, we investigated whether escin derivatives 1-7 (including new compounds 2, 3, 5 and 6), without the angeloyl or tigloyl groups and with modified glycosidic linkages by hydrolysis, have PEDV inhibitory effects with less cytotoxicity. Compounds 1-7 had no cytotoxicity at 20µM on VERO cells, while compounds 8-10 showed strong cytotoxicity at similar concentrations on PEDV. Our results suggest that escin derivatives showed strong inhibitory activities on PEDV replication with lowered cytotoxicity. These studies propose a method to utilize Japanese horse chestnut for treating PEDV and to increase the diversity of its bioactive compounds.
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Base de dados:
MEDLINE
Assunto principal:
Antivirais
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Sementes
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Aesculus
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Escina
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Vírus da Diarreia Epidêmica Suína
Idioma:
En
Ano de publicação:
2017
Tipo de documento:
Article