Abstract

(1) Background: Many flavonoids have been reported to exhibit pharmacological activity; a preparatory study confirmed that Coreopsis lanceolata flowers (CLFs) contained high flavonoid structure content; (2) Methods: CLFs were extracted in aqueous methanol (MeOH:H2O = 4:1) and fractionated into acetic ester (EtOAc), normal butanol (n-BuOH), and H2O fractions. Repeated column chromatographies for two fractions led to the isolation of two aurones and two flavonols; (3) Results: Four flavonoids were identified based on a variety of spectroscopic data analyses to be leptosidin (1), leptosin (2), isoquercetin (3), and astragalin (4), respectively. This is the first report for isolation of 2–4 from CLFs. High-performance liquid chromatography (HPLC) analysis determined the content levels of compounds 1–4 in the MeOH extract to be 2.8 ± 0.3 mg/g (1), 17.9 ± 0.9 mg/g (2), 3.0 ± 0.2 mg/g (3), and 10.9 ± 0.9 mg/g (4), respectively. All isolated compounds showed radical scavenging activities and recovery activities in Caco-2, RAW264.7, PC-12, and HepG2 cells against reactive oxygen species. MeOH extract, EtOAc fraction, and 1–3 suppressed NO formation in LPS-stimulated RAW 264.7 cells and decreased iNOS and COX-2 expression. Furthermore, all compounds recovered the pancreatic islets damaged by alloxan treatment in zebrafish; (4) Conclusions: The outcome proposes 1–4 to serve as components of CLFs in standardizing anti-oxidant, pro-inflammatory inhibition, and potential anti-diabetic agents.

Highlights

  • Humans living in the modern era enjoy many advantages such as economical leisure, improvement of living standard, and growth of medicine

  • The materials, equipment, and methods used for evaluation of recovery efficacy of extract (CLF), fractions (CLFE, CLFB, and CLFW), and flavonoids 1–4 from C. lanceolata flowers on pancreatic islet damaged by alloxan in zebrafish are described in Supplementary Material S8 and a previous study [48,49,50]

  • Action of Diazoxide on Alloxan-Induced Diabetic Zebrafish The materials, equipment, and methods used for action of diazoxide on alloxaninduced diabetic zebrafish are described in supplementary material S8 and previous studies [48,49,50]

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Summary

Introduction

Humans living in the modern era enjoy many advantages such as economical leisure, improvement of living standard, and growth of medicine. Diabetes is a disease with a high concentration of glucose in the blood due to a lack of insulin secretion or poor functioning [3]. These types of diabetes include type 1 and type 2 diabetes [4]. Blood glucose and insulin concentrations rise abnormally and persistent hyperglycemia causes complications that result in retinopathy and nephropathy [6]. Voglibose, and other synthetic hypoglycemic agents are commonly used [8], but they have a high risk of hypoglycemia and may have side effects [9]. In order to overcome the side effects of synthetic hypoglycemic agents, researches on diabetes prevention and adjuvant therapy using natural materials have been actively carried out

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