Antiviral escin derivatives from the seeds of Aesculus turbinata Blume (Japanese horse chestnut)

Bioorganic & Medicinal Chemistry Letters
Ji Won KimWon Keun Oh

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 compou...Continue Reading

Citations

Jun 13, 2020·Natural Products and Bioprospecting·Ilkay Erdogan Orhan, F Sezer Senol Deniz
May 21, 2020·Journal of Translational Medicine·Negar MoradianNima Rezaei
Oct 13, 2020·Revista Brasileira De Farmacognosia : Orgão Oficial Da Sociedade Brasileira De Farmacognosia·Kazhila C Chinsembu
Dec 29, 2020·Journal of Immunoassay & Immunochemistry·Alice GrigoreRadu Albulescu
Nov 13, 2020·Frontiers in Pharmacology·Junqing HuangJia-Xu Chen
Jul 3, 2021·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Avez SharipovJamoliddin Razzokov

❮ Previous
Next ❯

Methods Mentioned

BETA
column chromatography
deacylation

Software Mentioned

DS
CDOCKER

Related Concepts

Related Feeds

Antifungals (ASM)

An antifungal, also known as an antimycotic medication, is a pharmaceutical fungicide or fungistatic used to treat and prevent mycosis such as athlete's foot, ringworm, candidiasis, cryptococcal meningitis, and others. Discover the latest research on antifungals here.

Antivirals (ASM)

Antivirals are medications that are used specifically for treating viral infections. Discover the latest research on antivirals here.

Antifungals

An antifungal, also known as an antimycotic medication, is a pharmaceutical fungicide or fungistatic used to treat and prevent mycosis such as athlete's foot, ringworm, candidiasis, cryptococcal meningitis, and others. Discover the latest research on antifungals here.

Antivirals

Antivirals are medications that are used specifically for treating viral infections. Discover the latest research on antivirals here.