• Nutrition Research and Practice
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• 제13권6호
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• pp.473-479
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• 2019

BACKGROUND/OBJECTIVES: Anti-inflammatory and antioxidative activities of luteolin and luteolin-7-O-glucoside were compared in galactosamine (GalN)/lipopolysaccharide (LPS)-induced hepatitic ICR mice. MATERIALS/METHODS: Male ICR mice (6 weeks old) were divided into 4 groups: normal control, GalN/LPS, luteolin, and luteolin-7-O-glucoside groups. The latter two groups were administered luteolin or luteolin-7-O-glucoside (50 mg/kg BW) daily by gavage for 3 weeks after which hepatitis was induced by intraperitoneal injection of GalN and LPS (1 g/kg BW and $10{\mu}g/kg\;BW$, respectively). RESULTS: GalN/LPS produced acute hepatic injury by a sharp increase in serum AST, ALT, and $TNF-{\alpha}$ levels, increases that were ameliorated in the experimental groups. In addition, markedly increased expressions of cyclooxygenase (COX)-2 and its transcription factors, nuclear factor $(NF)-{\kappa}B$ and activator protein (AP)-1, were also significantly attenuated in the experimental groups. Compared to luteolin-7-O-glucoside, luteolin more potently ameliorated the levels of inflammatory mediators. Phase II enzymes levels and NF-E2 p45-related factor (Nrf)-2 activation that were decreased by GalN/LPS were increased by luteolin and luteolin-7-O-glucoside administration. In addition, compared to luteolin, luteolin-7-O-glucoside acted as a more potent inducer of changes in phase II enzymes. Liver histopathology results were consistent with the mediator and enzyme results. CONCLUSION: Luteolin and luteolin-7-O-glucoside protect against GalN/LPS-induced hepatotoxicity through the regulation of inflammatory mediators and phase II enzymes.

• Nutrition Research and Practice
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• 제7권6호
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• pp.423-429
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• 2013

Luteolin is a flavonoid found in abundance in celery, green pepper, and dandelions. Previous studies have shown that luteolin is an anti-inflammatory and anti-oxidative agent. In this study, the anti-inflammatory capacity of luteolin and one of its glycosidic forms, luteolin-7-O-glucoside, were compared and their molecular mechanisms of action were analyzed. In lipopolysaccharide (LPS)-activated RAW 264.7 cells, luteolin more potently inhibited the production of nitric oxide (NO) and prostaglandin E2 as well as the expression of their corresponding enzymes (inducible NO synthase (iNOS) and cyclooxygenase-2 (COX-2) than luteolin-7-O-glucoside. The molecular mechanisms underlying these effects were investigated to determine whether the inflammatory response was related to the transcription factors, nuclear factor (NF)-${\kappa}B$ and activator protein (AP)-1, or their upstream signaling molecules, mitogen-activated protein kinases (MAPKs) and phosphoinositide 3-kinase (PI3K). Luteolin attenuated the activation of both transcription factors, NF-${\kappa}B$ and AP-1, while luteolin-7-O-glucoside only impeded NF-${\kappa}B$ activation. However, both flavonoids inhibited Akt phosphorylation in a dose-dependent manner. Consequently, luteolin more potently ameliorated LPS-induced inflammation than luteolin-7-O-glucoside, which might be attributed to the differentially activated NF-${\kappa}B$/AP-1/PI3K-Akt pathway in RAW 264.7 cells.

• 대한약학회:학술대회논문집
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2-2
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• pp.102.2-103
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• 2003

It has been previously reported that luteolin and luteolin-7-glucoside displayed the potent anti-oxidant and anti-inflammatory effects, which have also been successful in reducing vascular smooth muscle cells(VSMCs) proliferation. In this study, a possible anti-proliferative effect and its mechanism on rat aortic VSMCs by luteolin and luteolin-7-glucoside were investigated. Luteolin significantly inhibited the platelet-derived growth factor(PDGF)-BB-induced proliferation of rat aortic VSMCs. While luteolin-7-glucoside weakly inhibited the proliferation. (omitted)

• Natural Product Sciences
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• 제23권3호
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• pp.183-191
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• 2017

Luteolin 5-O-glucoside is the major flavonoid from Korean thistle, Cirsium maackii. We previously reported the anti-inflammatory activities of luteolin 5-O-glucoside in lipopolysaccharide (LPS)-stimulated RAW 264.7 cells. In this study, we determined the anti-inflammatory mechanisms of luteolin 5-O-glucoside through the inhibition of nitric oxide (NO) production in vitro and in vivo. Results revealed that luteolin 5-O-glucoside dose-dependently inhibited NO production and expression of iNOS and COX-2 in LPS-induced RAW 264.7 cells. Luteolin 5-O-glucoside also significantly inhibited the translocation of $NF-{\kappa}B$, the activation of MAPKs, and ROS generation in LPS-induced RAW 264.7 cells. In addition, protein expressions of Nrf-2 and HO-1 were also upregulated by luteolin 5-O-glucoside treatment. Moreover, luteolin 5-O-glucoside inhibited ${\lambda}-carrageenan-induced$ mouse paw edema by 65.34% and 48.31% at doses of 50 and 100 mg/kg body weight, respectively. These findings indicate potential anti-inflammatory effect of luteolin 5-O-glucoside particularly by downregulating $NF-{\kappa}B$ and upregulating HO-1/Nrf-2 pathway.

• 한국식품영양과학회지
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• 제29권1호
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• pp.106-110
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• 2000

We investigated the active oxygen scavenging activity and active compound from Humulus japonicus. The ethyl acetate and butanol fraction exhibited strong scavenging effects on hydroxyl radical. Furthermore active compound was isolated and purified using Amberlite XAD-2 column chromatography and preparative HPLC from ethyl acetate fracton, and major compound was identified as a luteolin-7-O-$\beta$-D-glucoside by the MS, UV, 1H-NMR and 13C-NMR analyses. Luteolin-7-O-$\beta$-D-glucoside exhibited strong scavenging effect on active oxygens such as superoxide radical, hydroxyl radical and hydrogen peroxide.

• Fisheries and Aquatic Sciences
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• 제24권12호
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• pp.428-436
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• 2021

The aim of this study was to isolate and identify secondary metabolites from Sonchus brachyotus and evaluate their antioxidant and anti-inflammatory activities. In this study, we isolated three flavonoids from a 70% EtOH extract by Medium Pressure Liquid Chromatography (MPLC) and prep-High-Performance Liquid Chromatography (HPLC). To evaluate the biological activities (antioxidant and anti-inflammatory) of these flavonoids, their in vitro inhibitory activities against lipopolysaccharide (LPS)-induced reactive oxygen species (ROS) generation, nitric oxide (NO) production, and prostaglandin E₂ (PGE₂) secretion were determined. We successfully identified three flavonoids, namely luteolin (1), luteolin-7-O-β-D-glucoside (2), and luteolin-7-O-β-D-glucuronide (3) by spectral analyses. Luteolin (1) at 20 ㎍/mL inhibited ROS generation, NO production, and PGE₂ secretion by 48.6%, 61.28% and 12.10%, respectively, and luteolin-7-O-β-D-glucoside (2) inhibited NO and PGE₂ generation by 67.03% and 20.82%, respectively. Luteolin (1) and luteolin-7-O-β-D-glucoside (2) showed similar anti-inflammatory activities; however, luteolin (1) was observed to be a stronger antioxidant. Besides antioxidant and anti-inflammatory activities, S. brachyotus extract containing luteolin (1) and luteolin-7-O-β-D-glucoside (2) is considered to possess diverse biological activities. The results indicate that S. brachyotus is an edible medicinal plant, which is believed to be significant resource of functional foods.

• Archives of Pharmacal Research
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• 제11권3호
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• pp.247-249
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• 1988

Apigenin, apigenin-7-O-glucoside, luteolin-7-O-glucoside and linarin were isolated from Elscholtzia cristata (Labiatae).

• 한국응용약물학회:학술대회논문집
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• 한국응용약물학회 1994년도 춘계학술대회 and 제3회 신약개발 연구발표회
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• pp.209-209
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• 1994

천연자원으로부터 얻어진 항암 또는 세포독성물질로는 주로 alkaloid, lignan, terpenoid, macrolide 등에 속하는 물질들이고 그 중 sesquiterpene lactone계열 화합물에서 세포독성 및 항종양 활성이 있는 물질이 다수 얻어졌으며 그 대부분은 국화과의 식물에서 분리 보고되고 있다. Achillea 속 식물은 국화과에 속하는 다년생초본으로 남한에는 톱풀과 산톱풀 2종만이 자생한다. screening 결과 이 두 식물에는 segquiterpene lactone 화합물과 Peroxide등 다수의 활성성분이 함유되어 있을 것으로 기대되어 본 연구에 착수하였다. 두 식물의 각 분획에 대하여 SNU-1(위암세포주)과 SNU-354(간암세포주)를 이용해 검색한 결과 두 식물 모두 MC ext.와 MeOH ext.에서 현저한 세포독성을 보였으며 현재 MC ext. 로부터 세포독성물질의 분리를 수행하고 있다. EtOAc ext.는 세포독성은 거의 나타내지 않았으나 flavonoid 성분이 다수 존재함을 확인하였으며 면역활성 및 enzyme inhibition등의 활성을 검토하고자 화합물을 분리하였다. 그 결과 톱풀로 부터는 luteolin-7-0-glucoside와 apigenin-7-0-glucoside를 그리고 산톱풀로부터는 luteolin-7-0-glucoside, apigenin-7-0-glucoside, luteolin, apigenin을 분리 확인 동정하였다.

• 한국응용약물학회:학술대회논문집
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• 한국응용약물학회 1994년도 춘계학술대회 and 제3회 신약개발 연구발표회
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• pp.210-210
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• 1994

천연자원으로부터 얻어진 항암 또는 세포독성물질로는 주로 alkaloid, lignan, terpenoid, macrolide 등에 속하는 물질들이고 그 중 sesquiterpene lactone계열 화합물에서 세포독성 및 항종양 활성이 있는 물질이 다수 얻어졌으며 그 대부분은 국화과의 식물에서 분리 보고되고 있다. Achillea 속 식물은 국화과에 속하는 다년생초본으로 남한에는 톱풀과 산톱풀 2종만이 자생한다. screening 결과 이 두 식물에는 segquiterpene lactone 화합물과 Peroxide등 다수의 활성성분이 함유되어 있을 것으로 기대되어 본 연구에 착수하였다. 두 식물의 각 분획에 대하여 SNU-1(위암세포주)과 SNU-354(간암세포주)를 이용해 검색한 결과 두 식물 모두 MC ext.와 MeOH ext.에서 현저한 세포독성을 보였으며 현재 MC ext. 로부터 세포독성물질의 분리를 수행하고 있다. EtOAc ext.는 세포독성은 거의 나타내지 않았으나 flavonoid 성분이 다수 존재함을 확인하였으며 면역활성 및 enzyme inhibition등의 활성을 검토하고자 화합물을 분리하였다. 그 결과 톱풀로 부터는 luteolin-7-0-glucoside와 apigenin-7-0-glucoside를 그리고 산톱풀로부터는 luteolin-7-0-glucoside, apigenin-7-0-glucoside, luteolin, apigenin을 분리 확인 동정하였다.

• Archives of Pharmacal Research
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• 제25권3호
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• pp.313-319
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• 2002

A total of eight flavonoids (1-8), including a novel $quercetin-7-o-(6"-o-acetyl)-{\beta}-D-glucopyranoside$ (6) and seven known flavonoids, luteolin (1), quercetin (2), luteolin $7-o-{\beta}-D-glucopyranoside$ (3), $luteolin-7-o-(6"-Ο-acetyl)-{\beta}-D-glucopyranoside$ (4) quercetin $7-o-{\beta}-D-glucopyranoside$ (5), acacetin 7-o-{\beta}-D-glucuronide (7) and apigenin-6-C-{\beta}-D-glucopyrano $syl-8-C-{\beta}-D-glucopyranoside$ (8), have been isolated from the leaves of the safflower (Carthamus tinctorius L.) and identified on the basis of spectroscopic and chemical studies. The antioxidative activity of these flavonoids was evaluated against 2-deoxyribose degradation and rat liver microsomal lipid peroxidation induced by hydroxyl radicals generated via a Fenton-type reaction. Among these flavonoids, luteolin-acetyl-glucoside (4) and quercetin-acetyl-glucoside (6) showed potent antioxidative activities against 2-deoxyribose degradation and lipid peroxidation in rat liver microsomes. Luteolin (1), quercetin (2), and their corresponding glycosides (3 & 5) also exhibited strong antioxidative activity, while acacetin glucuronide (7) and apigenin-6,8-di-C-glucoside (8) were relatively less active.