• Biomolecules & Therapeutics
• /
• 제22권4호
• /
• pp.282-287
• /
• 2014

We show that silymarin, a polyphenolic flavonoid isolated from milk thistle (Silybum marianum), inhibits cytokine mixture (CM: TNF-${\alpha}$, IFN-${\gamma}$, and IL-$1{\beta}$)-induced production of nitric oxide (NO) in the pancreatic beta cell line MIN6N8a. Immunostaining and Western blot analysis showed that silymarin inhibits iNOS gene expression. RT-PCR showed that silymarin inhibits iNOS gene expression in a dose-dependent manner. We also showed that silymarin inhibits extracellular signal-regulated protein kinase-1 and 2 (ERK1/2) phosphorylation. A MEK1 inhibitor abrogated CM-induced nitrite production, similar to silymarin. Treatment of MIN6N8a cells with silymarin also inhibited CM-stimulated activation of NF-${\kappa}B$, which is important for iNOS transcription. Collectively, we demonstrate that silymarin inhibits NO production in pancreatic beta cells, and silymarin may represent a useful anti-diabetic agent.

• 생약학회지
• /
• 제40권3호
• /
• pp.178-183
• /
• 2009

In DPPH radical and nitric oxide scavenging ability, the extract of lowest temperature condition(40-15H ; 15 hours at $40^{\circ}C$ for drying) exhibited highest activity. The total phenolic and flavonoid contents of each extracts were found to be $120.4{\sim}193.3\;mg$/g and $86.91{\sim}94.55\;mg$/g respectively. It is shown that 40-15H was the highest content in each compound. In antimicrobial activity, a lower drying temperature conditions were found to be more strong activities in disc diffusion assay and each extracts showed MIC of identical level against every tested microbial strains. However 100-2H(2 hours at $100^{\circ}C$ for drying) was exhibited MIC of slightly low level against some strains. And every extract showed fine cell viabilities($101.7{\sim}122.9%$) against RAW 264.7 cell. In anti-proliferation activity against AGS, each extract showed a similar inhibition activity. However in anti-proliferation activity against HeLa, a lower drying temperature conditions showed more strong activities.

• Toxicological Research
• /
• 제27권2호
• /
• pp.71-76
• /
• 2011

We demonstrate that baicalein, a bioactive flavonoid originally isolated from Scutellaria baicalensis, inhibits LPS-induced expression of iNOS gene in RAW 264.7 cells. Treatment of peritoneal macrophages and RAW 264.7 cells with baicalein inhibited LPS-stimulated nitric oxide production in a dose-related manner. Immunohistochemical staining of iNOS and RT-PCR analysis showed that the decrease of NO was due to the inhibition of iNOS gene expression in RAW 264.7 cells. Immunostaining of p65, EMSA, and reporter gene assay showed that baicalein inhibited NF-${\kappa}$B nuclear translocation, DNA binding, and transcriptional activation, respectively. Collectively, these series of experiments indicate that baicalein inhibits iNOS gene expression by blocking NF-${\kappa}$B nuclear translocation. Due to the critical role that NO release plays in mediating inflammatory responses, the inhibitory effects of baicalein on iNOS suggest that baicalein may represent a useful anti-inflammatory agent.

• 한국식품조리과학회지
• /
• 제29권5호
• /
• pp.573-580
• /
• 2013

We investigated the physiological activities of extracts from Lindera obtusiloba Blume leaf and twig (LLW: water extract from Lindera obtusiloba Blume leaf, LLE: 50% ethanol extract from Lindera obtusiloba Blume leaf, LTW: water extract from Lindera obtusiloba Blume twig, LTE: 50% ethanol extract from Lindera obtusiloba Blume twig). Total polyphenol and total flavonoid contents of LTE were 445.38 mg/g and 302.09 mg/g, respectively. The electron donating ability (95.38%) of LTE was higher than that of the LLE (93.76%), LTW (88.09%), and LLW (82.06%). The oxygen radical absorbance capacity of extracts were improved with 50% ethanol condition, rather than hot water. Superoxide radical scavenging activity and FRAP activity of the extracts were improved with an increase of treatment concentration. All the extracts($1,000{\mu}g/mL$) stimulated a production of nitric oxide (NO) in macrophage RAW264.7 cells. In particular, the NO stimulating activity of LTE was superior to that of LLE, LTW, and LLW. The antitumor activity of LTE ($500{\mu}g/mL$) in A549, HeLa and SNU719 was 55.63%, 83.87% and 68.11%, respectively. The UVB-induced MMP-1 production in HS68 cells was suppressed by the treatment of LTE (88.28%), LLE (83.96%), LTW (80.59%) and LLW (76.08%).

• Biomolecules & Therapeutics
• /
• 제24권1호
• /
• pp.57-61
• /
• 2016

Fisetin, a natural flavonoid found in a variety of vegetables and fruits, has been shown to possess many biological functions. The present study was undertaken to investigate the influence of fisetin on vascular smooth muscle contractility and to determine the mechanism involved. Denuded aortic rings from male rats were used and isometric contractions were recorded and combined with molecular experiments. Fisetin significantly relaxed fluoride-, thromboxane $A_2$- or phorbol ester-induced vascular contraction suggesting as a possible anti-hypertensive on the agonist-induced vascular contraction regardless of endothelial nitric oxide synthesis. Furthermore, fisetin significantly inhibited fluoride-induced increases in pMYPT1 levels and phorbol ester-induced increases in pERK1/2 levels suggesting the mechanism involving the inhibition of Rho-kinase activity and the subsequent phosphorylation of MYPT1 and MEK activity and the subsequent phosphorylation of ERK1/2. This study provides evidence regarding the mechanism underlying the relaxation effect of fisetin on agonist-induced vascular contraction regardless of endothelial function.

• 한국약용작물학회지
• /
• 제23권1호
• /
• pp.49-56
• /
• 2015

Edible berries are rich in anthocyanins and phenolic acids, compounds that possess antioxidant, anti-inflammatory, and other biological activities. Antioxidant and anti-inflammatory activities of five berries including acaiberry (Euterpe oleracea Mart.), Aronia/black chokeberry (Aronia melanocarpa), blueberry (Vaccinium angustifolium), black currant (Ribes nigrum L.), and cranberry (Vaccinium macrocarpon) were assessed. The Aronia G (prepared by GreenField s.c.) exhibited the highest antioxidant activities as shown in total phenolic (138.81 mg CAE/g), flavonoid (3.68 mg QE/g), and anthocyanin (20.31 mg/g) contents compared to the other berries. It also showed the strongest scavenging activities such as DPPH (69.69 mg vitamin C/g) and ABTS radical scavenging activity ($757.79{\mu}mol$ trolox/g). Aronia G exhibited strong ferric reducing antioxidant power ($553.98{\mu}mol$ vitamin C/g), and oxygen radical absorbance capacity ($820.92{\mu}mol$ trolox/g). In addition, black currant and Aronia showed stronger inhibition of nitric oxide production in lipopolysaccharide-stimulated RAW 264.7 cell than the other berries. According to the above results, the Aronia and other edible berries have notably high level of antioxidant activities and they could be used as a potential source of natural antioxidants.

• 대한의생명과학회지
• /
• 제26권2호
• /
• pp.109-113
• /
• 2020

Dangyuja (Citrus maxima (Burm.) Merr.) is a native fruit of great economic importance in Jeju island in Korea. To provide experimental evidence for the antioxidant and anti-inflammation properties on extraction ethanol concentration of Dangyuja, 2 cultivars, including 30-year-old and 120-year-old were evaluated. 30-year-old Dangyuja 50%, 70% ethanol extracts had the highest polyphenol and flavonoid content, and the strongest 2,2'-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) radical scavenging activity. To investigate the anti-inflammatory activity of Dangyuja ethanol extracts, we used BV-2 microglia cells and induced inflammation using lipopolysaccharide (LPS). Then, we measured levels of inflammatory mediators as nitric oxide (NO). Among the 6 extracts, 30-year-old Dangyuja 50% ethanol extracts show the highest anti-inflammatory activity. The results suggest that 30-year-old Dangyuja 50% ethanol extracts provides significant health benefits and may be used for developing new functional materials.

• 약학회지
• /
• 제54권5호
• /
• pp.392-397
• /
• 2010

The aim of present study was to investigate the possible influence and related mechanism of additional alcohol on the flavonoid- induced arterial relaxation. Agonist-induced vascular smooth muscle contractions involve the activation of thick or thin filament pathway. However, there are no reports addressing the question whether this pathway is involved in quercetin-induced relaxation cotreated with alcohol in rat aortae contracted with phorbol ester, fluoride or thromboxane $A_2$ mimetic U-46619. We hypothesized that cotreated alcohol plays a role in vascular relaxation evoked by quercetin in rat aortae. Endothelium-denuded arterial rings from male Sprague-Dawley rats were used and isometric contractions were recorded using a computerized data acquisition system. Quercetin inhibited phorbol ester, fluoride or thromboxane $A_2$-induced contraction regardless of endothelial function. However, alcohol didn't decrease any agonist-induced contraction. Interestingly, only in thromboxane $A_2$-induced contraction, synergistic results were observed in aortae denuded and cotreated with quercetin and alcohol suggesting that additional pathways different from antioxidation or endothelial nitric oxide synthesis might be involved in the vasorelaxation. In conclusion, in the agonists-contracted rat aortae, quercetin and alcohol together showed synergistic response regardless of endothelial function in an agonist-dependent manner.

• 대한의생명과학회지
• /
• 제27권3호
• /
• pp.161-169
• /
• 2021

The present study, antioxidant and anti-inflammatory effects were measured of 6 endemic plants in Indonesian extracted by hot water or ethanol. The Nipa Fruticans Wurmb ethanol extract (NFWE) and Orthosiphon aristatus ethanol extract (OAE) showed the highest polyphenol and flavonoid contents of 203.70 and 33.70 ㎍/mg, respectively. Antioxidant activity of OAE was highest in DPPH radical scavenging activity (77.49% at 10 ㎍/mL) and ABTS⁺ radical scavenging activity (93.36% at 10 ㎍/mL). FRAP activity was significantly higher in NFWE than other extracts. Anti-inflammatory effects of 6 endemic plants in Indonesian extracted by hot water or ethanol were examined using nitric oxide (NO) inhibition assays. In the LPS-induced BV2 cells, OAE showed the highest inhibition of NO production without toxicity. The results of this study, suggest that OAE is a potential functional raw material for antioxidant and anti-inflammatory.

• 한국식생활문화학회지
• /
• 제35권6호
• /
• pp.605-612
• /
• 2020

In this study, 11 plant extracts from Bangladesh were used to evaluate the total phenolic and flavonoid content, in vitro antioxidant activities using 2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2-azinobis-(3-ethylbenzthiazolin-6-sulfonic acid) (ABTS), and ferric reducing antioxidant power (FRAP) assay. Also, the inhibitory effect of nitric oxide (NO) production in RAW 264.7 macrophage cell line and the neuroprotective effect on H2O2-induced PC12 cells were tested. Our results revealed that Piper betle L. showed the highest total phenolic content (162.2 mg GAE/g extract) among the 11 plants from Bangladesh. Most plants showed strong radical scavenging effects and ferric reducing antioxidant power. Besides, Piper betle L. protected PC12 neuronal cells against H2O2 related oxidative stress in LPS-induced PC12 cells. Regarding the anti-inflammatory effect, Piper betle L. significantly inhibited NO accumulation in LPS-induced RAW 264.7 cells. Our results provide evidence that Piper betle L. could be useful for the development of functional health foods.