천년초의 Taxifolin이 마우스대식세포(RAW 264.7 cell)에 미치는 항염증활성

김재영 ( Jaeyoung Kim ),이용화 ( Yonghwa Lee ),안현진 ( Hyeon Jin An ),이재덕 ( Jae Duk Lee ),이용섭 ( Yongsub Yi ) 한국응용생명화학회 2015 Journal of Applied Biological Chemistry (J. Appl. Vol.58 No.3

본 연구는 항산화 효과가 뛰어난 천년초를 이용하여 taxifolin을 순수분리하고 항염증 효과를 연구하였다. 천년초는 잎과 열매로 나누어 추출하였고 추출공정으로는 먼저 메탄올을 이용하여 조추출물을 추출하였다. 이렇게 얻어진 조추출물의 항산화 효과를 측정하였는데. 잎 추출물에서 38.33±1.07 μg/mL로 높은 항산화활성을 나타내었다. high performance liquid chromatography를 이용하여 taxifolin을 분리하고 확인하였다. 이렇게 얻어진 taxifolin을 이용하여 항염증 효과를 측정하였다. Taxifolin의 농도별 세포독성 측정에서는 500 μM 농도까지 처리 하였을 때 특별한 세포독성을 나타내지는 않았다. lipopolysaccharide에 의해 유도된 RAW 264.7 cell을 이용한 taxifolin의 염증성 cytokine측정실험에서는 IL-6의 발현양을 500 μM 처리시 2139.75±1.64pg/mL로 대조군에 비하여 47%까지 저해하였다. 하지만 TNF-α의 발현량은 대조군에 비하여 5%만 감소하였다. 염증성지표의 NO의 생성량은 500 μM 처리시 17.43±0.27 μM로 대조군에 비하여 57%까지 감소 시켰으며, 이와 관련된 COX-2 단백질의 발현양은 약 66% 이상 감소시켰다. 따라서 천년초에서 추출한 taxifolin은 항염증 효과가 있음을 확인할 수 있다. This study was performed to investigate the antiinflammatory activities of taxifolin from Opuntia humifusa. A potent anti-oxidant activity was shown from the leaf extract at IC50 value of 38.33±1.07 μg/mL and fruit extract at IC50 value of 40.23±2.21 μg/mL by 1,1-diphenyl-2-picrylhydrazyl assay. Fraction of taxifolin from leaf extract identified using high performance liquid chromatography and gas chromatography/mass spectrometry. The results of cell viability indicated that taxifolin did not show cytotoxicity on RAW 264.7 cells at 500 μM of concentration. The result showed that taxifolin inhibited lipopolysaccharide (LPS)-induced production of Nitrite oxide. In addition, taxifolin inhibited LPS-induced tumor necrosis factor-α and interleukin-6 production by cytokine assay and cyclooxygenase-2 expression by western blot analysis, meaning taxifolin has a significant anti-inflammatory effect. Our results suggested that taxifolin from Opuntia humifusa showed anti-inflammatory activities.

Taxifolin Inhibited the Nitric Oxide Production and Expression of Pro-inflammatory Cytokine mRNA in Lipopolysaccharide-stimulated RAW264.7 Cells

Rhee, Man-Hee,Endale, Mehari,Kamruzzaman, SM,Lee, Whi-Min,Park, Hwa-Jin,Yoo, Myung-Jo,Cho, Jae-Youl The Korean Society for Biomedical Laboratory Scien 2008 Journal of biomedical laboratory sciences Vol.14 No.3

In previous works, we found that solvent extract of Opuntia humifusa Raf., a member of the lactaceae family, displayed potent anti-oxidative and anti-inflammatory activities. Thus, all solvent fractions, except for the water layer, showed potent scavenging effects. According to activity-guided fractionation, one of active radical scavenging principles in the ethyl acetate fraction was found to be taxifolin. In this study, we investigated whether taxifolin showed anti-oxidative activity. In addition, taxifolin modulated nitric oxide (NO) release and the expression of pro-inflammatory cytokine mRNA such as interleukin-$1{\beta}$ (IL-$1{\beta}$), IL-6, granulocyte-macrophage colony-stimulating factor (GM-CSF), and TNF-${\alpha}$. Taxifolin showed potent anti-oxidant activity with the $IC_{50}\;of\;8.5{\pm}1.4\;and\;9.3{\pm}1.0{\mu}M$ using xanthine/xanthine oxidase (XO) assay and 2,2-Diphenyl-lpicrylhydrazyl radical (DPPH) assay, respectively. We next determined the role of taxifolin on the immunomodulating activity using murine macrophage cell line RAW264.7 cells. Taxifolin dose-dependently inhibited NO production in lipopolysaccharide (LPS)-activated RAW264.7. It also significantly blocked the expression of inducible NO synthase (iNOS) mRNA in the LPS-stimulated RAW264.7 cells. In addition, taxifolin potently suppressed the expression of IL-$1{\beta}$, IL-6 and GM-CSF mRNA in LPS-activated RAW264.7 cells, but not that of TNF-${\alpha}$ Moreover, taxifolin significantly inhibited the transcriptional activity of nuclear factor-${\kappa}B$ (NF-${\kappa}B$) and activator protein -1 (AP-1). These results suggest that taxifolin may downregulate inflammatory iNOS, IL-$1{\beta}$, IL-6 and GM-CSF gene expressions through inhibition of NF-K and AP-1 activation in LPS-stimulated RAW264.7 cells.

Anti-inflammatory effect of taxifolin in TNF-α/IL-17A/IFN-γ induced HaCaT human keratinocytes

Park Jung Eun,Kwon Hee Jun,Lee Hwa Jin,Hwang Hyung Seo 한국응용생명화학회 2023 Applied Biological Chemistry (Appl Biol Chem) Vol.66 No.-

Taxifolin, a bioactive flavonoid, has been attracting attention as a beneficial and valuable phytochemical due to its antioxidant, anticancer, and anti-inflammatory properties. Recently, an improvement effect of taxifolin against psoriasis has been reported in an animal experimental model. However, its exact mechanism of action at molecular and cellular levels is not known. Thus, the purpose of this study was to verify the anti-inflammatory effect of taxifolin on psoriasis at cellular/molecular level using HaCaT human keratinocytes. First, a CCK-8 assay was performed to evaluate cytotoxicity of taxifolin. Results revealed that taxifolin was a relatively safe material, showing no cytotoxicity at concentrations up to 300 μg/mL. In TNF-α-induced HaCaT cells, taxifolin significantly inhibited mRNA expression levels of pro-inflammatory cytokines (IL-1α, IL-1-β, and IL-6) and chemokines (CXCL8 and CCL20). The ability of taxifolin to regulation expression of inflammatory cytokine genes was associated with phosphorylation of IκB/STAT3 protein. In addition, taxifolin inhibited expression levels of IL-1α/β, IL-6, CXCL8, and CCL20 by inhibiting IκB/STAT3 protein phosphorylation upon stimulation of TNF-α, IL-17A, and IFN-γ. These results show that taxifolin has the potential to be developed as a treatment for psoriasis and skin inflammation.

Taxifolin Inhibited the Nitric Oxide Production and Expression of Pro-inflammatory Cytokine mRNA in Lipopolysaccharide-stimulated RAW264.7 Cells

Man Hee Rhee,Mehari Endale,SM Kamruzzaman,Whi Min Lee,Hwa-Jin Park,Myung-Jo Yoo,Jae Youl Cho 대한의생명과학회 2008 Biomedical Science Letters Vol.14 No.3

In previous works, we found that solvent extract of Opuntia humifusa Raf., a member of the lactaceae family, displayed potent anti-oxidative and anti-inflammatory activities. Thus, all solvent fractions, except for the water layer, showed potent scavenging effects. According to activity-guided fractionation, one of active radical scavenging principles in the ethyl acetate fraction was found to be taxifolin. In this study, we investigated whether taxifolin showed anti-oxidative activity. In addition, taxifolin modulated nitric oxide (NO) release and the expression of pro-inflammatory cytokine mRNA such as interleukin-1β (IL-1β), IL-6, granulocyte-macrophage colony-stimulating factor (GM-CSF), and TNF-α. Taxifolin showed potent anti-oxidant activity with the IC?? of 8.5±1.4 and 9.3±1.0 μM using xanthine/xanthine oxidase (XO) assay and 2,2-Diphenyl-lpicrylhydrazyl radical (DPPH) assay, respectively. We next determined the role of taxifolin on the immunomodulating activity using murine macrophage cell line RAW264.7 cells. Taxifolin dosedependently inhibited NO production in lipopolysaccharide (LPS)-activated RAW264.7. It also significantly blocked the expression of inducible NO synthase (iNOS) mRNA in the LPS-stimulated RAW264.7 cells. In addition, taxifolin potently suppressed the expression of IL-1β, IL-6 and GM-CSF mRNA in LPS-activated RAW264.7 cells, but not that of TNF-α. Moreover, taxifolin significantly inhibited the transcriptional activity of nuclear factor-κB (NF-κB) and activator protein -1 (AP-1). These results suggest that taxifolin may downregulate inflammatory iNOS, IL-1β, IL-6 and GM-CSF gene expressions through inhibition of NF-K and AP-1 activation in LPS-stimulated RAW264.7 cells.

The Improvement of Skin Inflammation by Taxifolin in Psoriasis Model using TNF-α/IL-17A/IFN-γ Induced HaCaT Cells

Jung Eun PARK,Hyung Seo HWANG,Hwa Jin LEE 한국생물공학회 2021 한국생물공학회 학술대회 Vol.2021 No.10

Taxifolin, a type of flavonoid compound of Hovenia dulcis Thunb., has pharmacological effects such as anti-inflammatory, anti-oxidant, anti-viral, anti-tumor and whitening activities. Recently, several animal clinical reports of taxifolin suggest its role on reducing the severity of psoriasis, but the available evidence on cellular/㏖ecular level of taxifolin is unclear. Therefore, this study was investigated the mechanism of action on the skin improvement and psoriatic skin regulation by taxifolin. Taxifolin significantly decreased mRNA levels of cytokines (IL-1α/β/-8) and chemokine(CCL20) in the TNF-α-induced HaCaT keratinocyte and inhibited phosphorylation of MAPK, IκB and STAT3. Furthermore, taxifolin specifically reduced the mRNA levels of IL-1α/β/-6/-8 and CCL20 in TNF-α/IL-17/IFN-γ induced HaCaT cell, strongly suggested its role in treatment of psoriasis. From these results, we confirmed that taxifolin has a function on the regulation of psoriatic skin inflammation through the MAPK/IκB/STAT3 signal pathway.

The Chemopreventive Effect of Taxifolin Is Exerted through ARE-Dependent Gene Regulation

Lee, Saet Byoul,Cha, Kwang Hyun,Selenge, Dangaa,Solongo, Amgalan,Nho, Chu Won Pharmaceutical Society of Japan 2007 Biological & pharmaceutical bulletin Vol.30 No.6

<P>Phase II detoxification enzymes are responsible for the detoxification and elimination of activated carcinogens, and thus act as important biomarkers for chemoprevention. In this study, we tested the chemopreventive activity of taxifolin, a flavanon compound purified from a mongolian medicinal plant, by measuring quinone reductase (QR) activity in HCT 116 cells. Taxifolin induced significant QR activity, but displayed relatively low cytotoxicity in cells (chemoprevention index=5.75). To identify the target genes regulated by taxifolin, DNA microarray was performed with a 3K human cancer chip containing 3096 human genes associated with carcinogenesis. Significant analysis of microarray (SAM) revealed 428 differentially expressed (DE) genes as statistically significant, with a false discovery rate (FDR) of 57.2% (delta=0.3366). Sixty-five genes, including a few detoxification enzymes (<I>NQO1</I>, <I>GSTM1</I>) and an antioxidant enzyme (<I>TXNRD1</I>), were up-regulated and 363 genes were down-regulated in the presence of 60 μ<SMALL>M</SMALL> taxifolin. In view of the finding that selected genes of interest contained antioxidant response element (ARE), we hypothesize that taxifolin modulates chemopreventive genes through activation of the ARE. Transient transfection experiments using the ARE QR-CAT construct demonstrate that taxifolin significantly activates ARE, but not xenobiotic response element (XRE). In conclusion, taxifolin acts as a potential chemopreventive agent by regulating genes <I>via</I> an ARE-dependent mechanism.</P>

슈퍼홍미 쌀품종 탁시폴린(Taxifolin) 성분의 환경변이

류수노(Su Noh Ryu) 한국육종학회 2018 한국육종학회지 Vol.50 No.1

본 연구는 쌀에 함유된 혈당을 저하하는 탁시폴린 성분에 대한 육종소재로서 기본정보를 얻고자 수행하였다. 슈퍼홍미 벼 품종으로부터 탁시폴린 성분을 분리하고 분광학적 방법에 의해 확인하였다. 또한 HPLC로 검량선을 작성하고 정량분석을 하였다. 다양한 유색미 품종 중에서 슈퍼홍미와 슈퍼홍미 유래계통에서만 탁시폴린 함량이 확인되었다. 슈퍼홍미의 탁시폴린 함량은 재배지역에 따라서 쌀 100 g에 32 mg에서 68 mg의 함량변이를 보였다. 이들 성분의 함량은 중북부지역에서 재배되었을 때보다 남부지역에서 재배되었을 때 높게 나타났다. 천립중은 재배지역에 따라서 23.5 g에서 27.8 g의 변이를 보였다. 탁시폴린 성분은 슈퍼홍미의 이삭뿐만 아니라 종자의 호분층에도 다량 함유되어 있어 이들 식물체를 기능성 소재로 이용할 수 있을 것으로 사료된다. 따라서 탁시폴린 성분이 다량 함유된 슈퍼홍미는 식량으로서뿐만 아니라 기능성 식품소재로서 높은 가치가 있을 것으로 기대된다. This study was conducted to obtain general information for rice breeding materials high in taxifolin content. The taxifolin was isolated from the rice variety, ‘Superhongmi’, and was identified by means of spectral methods and quantitative analysis using a high performance liquid chromatography (HPLC). The taxifolin content of the ‘Superhongmi’ variety was ranged between 32mg and 68mg per 100g seed that differs depending on cultivated regions. The taxifolin content was lower grown at mid north than those at south region. A large amount of taxifolin was found in the aleurone layer of seed as well as in the node of spike of the ‘Superhongmi’. The weight of 1,000 grains was ranged between 23.5g and 27.8g that varied depending on cultivated regions. This variety showed heading in the 6th of September, and its fertility ratio was about 83% in sejong region. These results suggest that the taxifolin-rich rice variety, ‘Superhongmi’, is a good source of functional and stable food.

건강기능식품 프랑스해안송껍질추출물 중 UPLC-MS/MS를 이용한 Ferulic acid, Caffeic acid, Catechin, Taxifolin 동시분석법 개발 연구

오재명,김지안,허수정,최윤희,오금순 한국식품위생안전성학회 2019 한국식품위생안전성학회지 Vol.34 No.5

This study was conducted to develop a simultaneous analysis method for ferulic acid, caffeic acid, catechin and taxifolin from Health Functional Food (HFF) Pinus Pinaster bark extract. The simultaneous analytical method for ferulic acid, caffeic acid, catechin and taxifolin is carried out using UPLC-MS/MS. The method validation was performed to determine selectivity, linearity, accuracy, limit of detection (LOD), limit of quantification (LOQ) and precision for ferulic acid, caffeic acid, catechin and taxifolin. LC-MS/MS method was established using an Acquity UPLC BEH C 18 Column and was applied for these 4 compounds. Product-ion traces, at m/z 194.2 → 133, 180.2 → 135, 290.3 → 245, 304.3 → 248, were used for quantitative analysis of ferulic acid, caffeic acid, catechin and taxifolin, respectively. Excellent linearity (r 2 =0.999) was observed for ferulic acid, caffeic acid, catechin and taxifolin in the concentration range (50-2500 mg/L). The observed recoveries of these 4 compounds were found to be between 84.9 and 104.9%, while precision was between 1.20 and 4.43% relative standard deviation (% RSD).

진달래뿌리추출물과 이로부터 분리한 taxifolin-3-O-alpha-L-arabinopyranoside의 항노화 활성

김태양,권혁철,이춘몽,이광식,이건국 한국화장품미용학회 2018 한국화장품미용학회지 Vol.8 No.3

In this experiment, we evaluated the anti-aging activity of Rhododendron mucronulatum root extract and taxifolin-3-O-alp ha-L-arabinopyranoside isolated from it. R. mucronulatum root extract showed half maximal DPPH radical scavenging concen tration at 850 ㎍/㎖ and half maximal elastase inhibitory concentration at 5,100 ㎍/㎖. Among solvent fractions of R.mucronul atum root extract, ethyl acetate fraction showed the highest DPPH radical scavenging concentration at 1.56 ㎍/㎖ and half ma ximal elastase inhibitory concentration at 525 ㎍/㎖. Also, ethyl acetate fraction showed the highest type-1-procollagen biosyn thesis activity. The type-1-procollagen biosynthesis level of taxifolin-3-O-alpha-L-arabinopyranoside was tested in human de rmal fibroblast cells. Results showed that taxifolin-3-O-alpha-L-arabinopyranoside increased type I procollagen biosythesis lev el in a dose-dependent manner. These results indicate R.mucronulatum root extracts and taxifolin-3-O-alpha-L-arabinopyrano side could be used as an anti-aging ingredients for functional cosmetics.

A Rapid, Green and Controllable Strategy to Fabricate Electrodeposition of Reduced Graphene Oxide Film as Sensing Materials for Determination of Taxifolin

Yanju Wu,Mingxiu Lv,Bei Li,Junda Ge,Lin Gao 성균관대학교(자연과학캠퍼스) 성균나노과학기술원 2015 NANO Vol.10 No.3

The electrodeposition of a film of reduced graphene oxide (ERGO) with well-dispersed on a glassy carbon electrode (GCE) was achieved using cyclic voltammetry (CV) in a graphene oxide (GO) colloidal solution. Using square wave adsorptive stripping voltammetry (SWASV), the ERGO film was applied for the first time, in developing a high-sensitive electrochemical sensor for detection of taxifolin. Compared with bare GCE, the resulting electrodes (ERGO/GCE) exhibited excellent response toward the oxidation of taxifolin by significantly enhancing the oxidation peak currents and the decreased peak-to-peak separation. Under selected conditions, the reduction peak currents had linear relationship with taxifolin concentration in the range of 5.0 x 10-8 - 1.5 x 10-5 mol L-1, with detection limit of 4.0 x 10-9 mol L-1. Besides, the method was successfully applied to the quantitative determination of taxifolin in the Prince's-feather fruit with satisfactory results.