Bioactivity-guided isolation of immunomodulatory compounds from the fruits of Ligustrum lucidum
Copyright © 2021 Elsevier B.V. All rights reserved..
ETHNOPHARMACOLOGICAL RELEVANCE: The fruits of Ligustrum lucidum (FLL) W.T. Aiton (Oleaceae) is included in the 2020 "Chinese Pharmacopoeia" and is widely used in traditional Chinese medicine as a tonic. In recent years, FLL has been reported to improve immune function, but the bioactive compounds and mechanisms of FLL remain poorly characterized.
AIM OF THE STUDY: To identify FFL compounds with strong immune activity and explore their molecular mechanisms.
MATERIALS AND METHODS: The phagocytic activity of RAW264.7 macrophages and proliferation activity of spleen lymphocytes were used to guide the isolation of bioactive compounds from FLL extracts. Lymphocyte subpopulations, Ca2+ concentrations, and surface molecule expression were analyzed using flow cytometry. Cytokine secretion was examined using ELISA. FITC-OVA uptake was observed using fluorescence microscopy. NF-κB activation was analyzed using western blotting.
RESULTS: The extraction and isolation produced ten compounds, namely oleuropeinic acid, nuezhenide, isonuezhenide, salidroside, isoligustrosidic acid, ligulucidumosides A, 8(E)-nuezhenide, hydroxytyrosol, oleuropein, and p-hydroxyphenethyl 7-β-D-glucosideelenolic acid ester were isolated and identified from FLL-Bu-30%. Immunoactivity experiments showed that hydroxytyrosol had the strongest macrophage phagocytotic and lymphocyte proliferation-promoting activities. Further studies showed that hydroxytyrosol could significantly enhance lymphocyte subsets CD3+, CD4+/CD8+, and CD3+CD4-CD8-, promote IL-4, IFN-γ, and TNF-α secretion, and increase intracellular Ca2+ concentrations. In addition, the results from RAW264.7 macrophages showed that hydroxytyrosol increased FITC-OVA uptake, induced TNF-α and IL-1β production, upregulated MHC-II, CD80, and CD86 expression, promoted cytoplasmic IκB-α degradation, and increased nuclear NF-κB p65 levels.
CONCLUSION: Our study provides substantial evidence regarding the mechanism of the immunomodulatory effects of compounds from FLL.
Medienart: |
E-Artikel |
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Erscheinungsjahr: |
2021 |
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Erschienen: |
2021 |
Enthalten in: |
Zur Gesamtaufnahme - volume:274 |
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Enthalten in: |
Journal of ethnopharmacology - 274(2021) vom: 28. Juni, Seite 114079 |
Sprache: |
Englisch |
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Beteiligte Personen: |
Liu, Jia [VerfasserIn] |
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Links: |
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Anmerkungen: |
Date Completed 15.11.2021 Date Revised 15.11.2021 published: Print-Electronic Citation Status MEDLINE |
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doi: |
10.1016/j.jep.2021.114079 |
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funding: |
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Förderinstitution / Projekttitel: |
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PPN (Katalog-ID): |
NLM323541496 |
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500 | |a published: Print-Electronic | ||
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520 | |a Copyright © 2021 Elsevier B.V. All rights reserved. | ||
520 | |a ETHNOPHARMACOLOGICAL RELEVANCE: The fruits of Ligustrum lucidum (FLL) W.T. Aiton (Oleaceae) is included in the 2020 "Chinese Pharmacopoeia" and is widely used in traditional Chinese medicine as a tonic. In recent years, FLL has been reported to improve immune function, but the bioactive compounds and mechanisms of FLL remain poorly characterized | ||
520 | |a AIM OF THE STUDY: To identify FFL compounds with strong immune activity and explore their molecular mechanisms | ||
520 | |a MATERIALS AND METHODS: The phagocytic activity of RAW264.7 macrophages and proliferation activity of spleen lymphocytes were used to guide the isolation of bioactive compounds from FLL extracts. Lymphocyte subpopulations, Ca2+ concentrations, and surface molecule expression were analyzed using flow cytometry. Cytokine secretion was examined using ELISA. FITC-OVA uptake was observed using fluorescence microscopy. NF-κB activation was analyzed using western blotting | ||
520 | |a RESULTS: The extraction and isolation produced ten compounds, namely oleuropeinic acid, nuezhenide, isonuezhenide, salidroside, isoligustrosidic acid, ligulucidumosides A, 8(E)-nuezhenide, hydroxytyrosol, oleuropein, and p-hydroxyphenethyl 7-β-D-glucosideelenolic acid ester were isolated and identified from FLL-Bu-30%. Immunoactivity experiments showed that hydroxytyrosol had the strongest macrophage phagocytotic and lymphocyte proliferation-promoting activities. Further studies showed that hydroxytyrosol could significantly enhance lymphocyte subsets CD3+, CD4+/CD8+, and CD3+CD4-CD8-, promote IL-4, IFN-γ, and TNF-α secretion, and increase intracellular Ca2+ concentrations. In addition, the results from RAW264.7 macrophages showed that hydroxytyrosol increased FITC-OVA uptake, induced TNF-α and IL-1β production, upregulated MHC-II, CD80, and CD86 expression, promoted cytoplasmic IκB-α degradation, and increased nuclear NF-κB p65 levels | ||
520 | |a CONCLUSION: Our study provides substantial evidence regarding the mechanism of the immunomodulatory effects of compounds from FLL | ||
650 | 4 | |a Journal Article | |
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700 | 1 | |a Fan, Yunpeng |e verfasserin |4 aut | |
700 | 1 | |a Song, Xiaoping |e verfasserin |4 aut | |
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