Luteolin-3′-<i>O</i>-Phosphate Inhibits Lipopolysaccharide-Induced Inflammatory Responses by Regulating NF-κB/MAPK Cascade Signaling in RAW 264.7 Cells
Luteolin (LT), present in most plants, has potent anti-inflammatory properties both in vitro and in vivo. Furthermore, some of its derivatives, such as luteolin-7-<i>O</i>-glucoside, also exhibit anti-inflammatory activity. However, the molecular mechanisms underlying luteolin-3′-<i&g...
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| Format: | Article |
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MDPI AG
2021-12-01
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| Series: | Molecules |
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| Online Access: | https://www.mdpi.com/1420-3049/26/23/7393 |
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| author | Jung-Hwan Kim Tae-Jin Park Jin-Soo Park Min-Seon Kim Won-Jae Chi Seung-Young Kim |
| author_facet | Jung-Hwan Kim Tae-Jin Park Jin-Soo Park Min-Seon Kim Won-Jae Chi Seung-Young Kim |
| author_sort | Jung-Hwan Kim |
| collection | DOAJ |
| description | Luteolin (LT), present in most plants, has potent anti-inflammatory properties both in vitro and in vivo. Furthermore, some of its derivatives, such as luteolin-7-<i>O</i>-glucoside, also exhibit anti-inflammatory activity. However, the molecular mechanisms underlying luteolin-3′-<i>O</i>-phosphate (LTP)-mediated immune regulation are not fully understood. In this paper, we compared the anti-inflammatory properties of LT and LTP and analyzed their molecular mechanisms of action; we obtained LTP via the biorenovation of LT. We investigated the anti-inflammatory activities of LT and LTP in macrophage RAW 264.7 cells. We confirmed from previously reported literature that LT inhibits the production of nitric oxide and prostaglandin E<sub>2</sub>, as well as the expression of inducible NO synthetase and cyclooxygenase-2. In addition, expressions of inflammatory genes and mediators, such as tumor necrosis factor-α, interleukin-6, and interleukin-1β, were suppressed. LTP showed anti-inflammatory activity similar to LT, but better anti-inflammatory activity in all the experiments, while also inhibiting mitogen-activated protein kinase and nuclear factor-kappa B more effectively than LT. At a concentration of 10 μM, LTP showed differences of 2.1 to 44.5% in the activity compared to LT; it also showed higher anti-inflammatory activity. Our findings suggest that LTP has stronger anti-inflammatory activity than LT. |
| first_indexed | 2024-03-10T04:47:57Z |
| format | Article |
| id | doaj.art-fd8d9d35aa714ef6af7f868f18d29b4b |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-03-10T04:47:57Z |
| publishDate | 2021-12-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-fd8d9d35aa714ef6af7f868f18d29b4b2023-11-23T02:51:53ZengMDPI AGMolecules1420-30492021-12-012623739310.3390/molecules26237393Luteolin-3′-<i>O</i>-Phosphate Inhibits Lipopolysaccharide-Induced Inflammatory Responses by Regulating NF-κB/MAPK Cascade Signaling in RAW 264.7 CellsJung-Hwan Kim0Tae-Jin Park1Jin-Soo Park2Min-Seon Kim3Won-Jae Chi4Seung-Young Kim5Department of Pharmaceutical Engineering & Biotechnology, Sunmoon University, Asan 31460, KoreaDepartment of Pharmaceutical Engineering & Biotechnology, Sunmoon University, Asan 31460, KoreaNatural Product Informatics Research Center, Korea Institute of Science and Technology (KIST), Gangneung 25451, KoreaNatural Product Informatics Research Center, Korea Institute of Science and Technology (KIST), Gangneung 25451, KoreaGenetic Resources Assessment Division, National Institute of Biological Resources, Incheon 22689, KoreaDepartment of Pharmaceutical Engineering & Biotechnology, Sunmoon University, Asan 31460, KoreaLuteolin (LT), present in most plants, has potent anti-inflammatory properties both in vitro and in vivo. Furthermore, some of its derivatives, such as luteolin-7-<i>O</i>-glucoside, also exhibit anti-inflammatory activity. However, the molecular mechanisms underlying luteolin-3′-<i>O</i>-phosphate (LTP)-mediated immune regulation are not fully understood. In this paper, we compared the anti-inflammatory properties of LT and LTP and analyzed their molecular mechanisms of action; we obtained LTP via the biorenovation of LT. We investigated the anti-inflammatory activities of LT and LTP in macrophage RAW 264.7 cells. We confirmed from previously reported literature that LT inhibits the production of nitric oxide and prostaglandin E<sub>2</sub>, as well as the expression of inducible NO synthetase and cyclooxygenase-2. In addition, expressions of inflammatory genes and mediators, such as tumor necrosis factor-α, interleukin-6, and interleukin-1β, were suppressed. LTP showed anti-inflammatory activity similar to LT, but better anti-inflammatory activity in all the experiments, while also inhibiting mitogen-activated protein kinase and nuclear factor-kappa B more effectively than LT. At a concentration of 10 μM, LTP showed differences of 2.1 to 44.5% in the activity compared to LT; it also showed higher anti-inflammatory activity. Our findings suggest that LTP has stronger anti-inflammatory activity than LT.https://www.mdpi.com/1420-3049/26/23/7393luteolin-3′-<i>O</i>-phosphateanti-inflammatoryMAPKNF-κBbiorenovation |
| spellingShingle | Jung-Hwan Kim Tae-Jin Park Jin-Soo Park Min-Seon Kim Won-Jae Chi Seung-Young Kim Luteolin-3′-<i>O</i>-Phosphate Inhibits Lipopolysaccharide-Induced Inflammatory Responses by Regulating NF-κB/MAPK Cascade Signaling in RAW 264.7 Cells Molecules luteolin-3′-<i>O</i>-phosphate anti-inflammatory MAPK NF-κB biorenovation |
| title | Luteolin-3′-<i>O</i>-Phosphate Inhibits Lipopolysaccharide-Induced Inflammatory Responses by Regulating NF-κB/MAPK Cascade Signaling in RAW 264.7 Cells |
| title_full | Luteolin-3′-<i>O</i>-Phosphate Inhibits Lipopolysaccharide-Induced Inflammatory Responses by Regulating NF-κB/MAPK Cascade Signaling in RAW 264.7 Cells |
| title_fullStr | Luteolin-3′-<i>O</i>-Phosphate Inhibits Lipopolysaccharide-Induced Inflammatory Responses by Regulating NF-κB/MAPK Cascade Signaling in RAW 264.7 Cells |
| title_full_unstemmed | Luteolin-3′-<i>O</i>-Phosphate Inhibits Lipopolysaccharide-Induced Inflammatory Responses by Regulating NF-κB/MAPK Cascade Signaling in RAW 264.7 Cells |
| title_short | Luteolin-3′-<i>O</i>-Phosphate Inhibits Lipopolysaccharide-Induced Inflammatory Responses by Regulating NF-κB/MAPK Cascade Signaling in RAW 264.7 Cells |
| title_sort | luteolin 3 i o i phosphate inhibits lipopolysaccharide induced inflammatory responses by regulating nf κb mapk cascade signaling in raw 264 7 cells |
| topic | luteolin-3′-<i>O</i>-phosphate anti-inflammatory MAPK NF-κB biorenovation |
| url | https://www.mdpi.com/1420-3049/26/23/7393 |
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