Inhibition of HMG-CoA reductase activity and cholesterol permeation through Caco-2 cells by caffeoylquinic acids from Vernonia condensata leaves

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• 作者：Ana A. Arantes^a ; ^b ; Pedro L. Falé ; ^a ; ^b ; Larissa C.B. Costa^c ; Rita Pacheco^a ; ^d ; Lia Ascensã ; o^e ; Maria Luí ; sa Serralheiro^a ; ^b ; ^{mlserralheiro@fc.ul.pt" class="auth_mail" title="E-mail the corresponding author}
• 关键词：Vernonia condensata ; HMG-CoA reductase ; Chlorogenic acid ; Cynarin ; Cholesterol ; Caco-2 cells
• 刊名：Revista Brasileira de Farmacognosia
• 出版年：2016
• 出版时间：November-December 2016
• 年：2016
• 卷：26
• 期：6
• 页码：738-743
• 全文大小：666 K

文摘

The aim of this study was to provide scientific knowledge to support the use of Vernonia condensata Baker, Asteraceae, beverages for their alleged hypocholesterolemic properties by testing their action as HMG-CoA reductase inhibitors and their capacity to lower dietary cholesterol permeation. Chlorogenic acid, and other caffeoylquinic acids derivatives were identified as the main components of these beverages by LC–MS/MS. No changes in the composition were notice after the in vitro gastrointestinal digestion and no toxicity against Caco-2 and HepG2 cell lines was detected. Cholesterol permeation through Caco-2 monolayers was reduced in 37% in the presence of these herbal teas, and the caffeoylquinic acids permeated the monolayers in 30–40% of their initial amount in 6 h. HMG-CoA reductase activity was reduced with these beverages, showing an IC₅₀ of 217 μg ml⁻¹. It was concluded that caffeoylquinic acids, the major components, justified 98% of the enzyme inhibition measured.