Abstract

A series of chromatographic separations performed on the ethanol extracts of the peels of Citrus grandis has led to the characterization of forty compounds, including seventeen coumarins, eight flavonoids, two triterpenoids, four benzenoids, two steroids, one lignan, one amide, and five other compounds, respectively. The chemical structures of the purified constituents were identified on the basis of spectroscopic elucidation, including 1D- and 2D-NMR, UV, IR, and mass spectrometric analysis. Most of the isolated compounds were examined for their inhibition of superoxide anion generation and elastase release by human neutrophils. Among the isolates, isomeranzin (3), 17,18-dihydroxybergamottin (12), epoxybergamottin (13), rhoifolin (19), vitexicarpin (22) and 4-hydroxybenzaldehyde (29) displayed the most significant inhibition of superoxide anion generation and elastase release with IC50 values ranged from 0.54 to 7.57 μM, and 0.43 to 4.33 μM, respectively. In addition, 7-hydroxy-8-(2′-hydroxy-3′-methylbut-3′-enyl)coumarin (8) and 17,18-dihydroxybergamottin (12) also exhibited the protection of neurons against Aβ-mediated neurotoxicity at 50 μM.

Highlights

  • The genus Citrus is composed of various species grown all over the tropical and subtropical regions

  • The dried peels of C. grandis were extracted with EtOH and the resulting extract was filtered and concentrated

  • The EtOH extracts were suspended in distilled water and successively partitioned with EtOAc to afford EtOAc layer and water layer, respectively

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Summary

Introduction

The genus Citrus is composed of various species grown all over the tropical and subtropical regions. The peels of mature fruits of C. grandis have been used in traditional Chinese medicine for treating the common cold and cancer, and relieving exhaustion [12]. Many natural products such as flavonoids, coumarins, and terpenoids have been isolated from C. grandis [2,3,4,5,6,7,8,9,10,11]. In a previous study [34], Citrus flavonoids were reported to exhibit anti-inflammatory and neuroprotective bioactivities. In the present study we wish to explore other bioactive principles of peels of C. grandis

Results and Discussion
Inhibitory
Compounds
Results are are to
General
HD andIII
Materials
Extraction and Isolation
Preparation of Human Neutrophils
Inhibition of Superoxide Anion Generation
Inhibition of Elastase Release
Statistical Analysis
Neuroprotective Activity
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