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Valeriana rigida Ruiz & Pav. Root Extract: A New Source of Caffeoylquinic Acids with Antioxidant and Aldose Reductase Inhibitory Activities.

ABSTRACT: Valeriana rigida Ruiz & Pav. (V. rigida) has long been used as a herbal medicine in Peru; however, its phytochemicals and pharmacology need to be scientifically explored. In this study, we combined the offline 2,2-diphenyl-1-picryl-hydrazyl-hydrate (DPPH)-/ultrafiltration-high-performance liquid chromatography (HPLC) and high-speed counter-current chromatography (HSCCC)/pH-zone-refining counter-current chromatography (pH-zone-refining CCC) to screen and separate the antioxidants and aldose reductase (AR) inhibitors from the 70% MeOH extract of V. rigida, which exhibited remarkable antioxidant and AR inhibitory activities. Seven compounds were initially screened as target compounds exhibiting dual antioxidant and AR inhibitory activities using DPPH-/ultrafiltration-HPLC, which guided the subsequent pH-zone-refining CCC and HSCCC separations of these target compounds, namely 3-O-caffeoylquinic acid, 4-O-caffeoylquinic acid, 5-O-caffeoylquinic acid, 3,4-O-di-caffeoylquinic acid, 3,5-O-di-caffeoylquinic acid, 4,5-O-di-caffeoylquinic acid, and 3,4,5-O-tri-caffeoylquinic acid. These compounds are identified for the first time in V. rigida and exhibited remarkable antioxidant and AR inhibitory activities. The results demonstrate that the method established in this study can be used to efficiently screen and separate the antioxidants and AR inhibitors from natural products and, particularly, the root extract of V. rigida is a new source of caffeoylquinic acids with antioxidant and AR inhibitory activities, and it can be used as a potential functional food ingredient for diabetes.

SUBMITTER: Zuo G

PROVIDER: S-EPMC8152971 | biostudies-literature |

REPOSITORIES: biostudies-literature

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Project description:Graphical abstract Highlights • The most active fraction of Piper crocatum Ruiz & Pav (FIV), originated from methanol extracts and wash benzene-soluble extracts, has diabetic wound healing activities on wounded hyperglycemia fibroblasts.• FIV ameliorates collagen deposition through decreasing p53 expressions, increasing αSMA, SOD1 and E-cadherin expressions.• FIV ameliorates wound closure through decreasing p53 expressions, increasing αSMA and E-cadherin expressions.• Fibroblasts can be used as a therapeutic target that mimics the condition of diabetic wounds at least in the 10th passage. Introduction Piper crocatum Ruiz & Pav (P. crocatum) has been reported to accelerate the diabetic wound healing process empirically. Some studies showed the benefits of P. crocatum in treating various diseases but its mechanisms in diabetic wound healing have never been reported. In the present study we investigated the diabetic wound healing activity of the active fraction of P. crocatum on wounded hyperglycemia fibroblasts (wHFs). Methods Bioassay-guided fractionation was performed to get the most active fraction. The selected active fraction was applied to wHFs within 72 h incubation. Mimicking a diabetic condition was done using basal glucose media containing an additional 17 mMol/L D-glucose. A wound was simulated via the scratch assay. The collagen deposition was measured using Picro-Sirius Red and wound closure was measured using scratch wound assay. Underlying mechanisms through p53, αSMA, SOD1 and E-cadherin were measured using western blotting. Results We reported that FIV is the most active fraction of P. crocatum. We confirmed that FIV\(7.81 µg/ml, 15.62 µg/ml, 31.25 µg/ml, 62.5 µg/ml, and 125 µg/ml) induced the collagen deposition and wound closure of wHFs. Furthermore, FIV treatment (7.81 µg/ml, 15.62 µg/ml, 31.25 µg/ml) down-regulated the protein expression level of p53 and up-regulated the protein expression levels of αSMA, E-cadherin, and SOD1. Discussion/conclusions Our findings suggest that ameliorating collagen deposition and wound closure through protein regulation of p53, αSMA, E-cadherin, and SOD1 are some of the mechanisms by which FIV of P. crocatum is involved in diabetic wound healing therapy.

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Valeriana rigida Ruiz & Pav. Root Extract: A New Source of Caffeoylquinic Acids with Antioxidant and Aldose Reductase Inhibitory Activities.

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