• Title/Summary/Keyword: trolox

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A Novel Urotensin II Receptor Antagonist, KR-36996 Inhibits Smooth Muscle Proliferation through ERK/ROS Pathway

  • Kim, Tae-Ho;Lee, Dong Gil;Kim, Young-Ae;Lee, Byung Ho;Yi, Kyu Yang;Jung, Yi-Sook
    • Biomolecules & Therapeutics
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    • v.25 no.3
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    • pp.308-314
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    • 2017
  • Urotensin II (UII) is a mitogenic and hypertrophic agent that can induce the proliferation of vascular cells. UII inhibition has been considered as beneficial strategy for atherosclerosis and restenosis. However, currently there is no therapeutics clinically available for atherosclerosis or restenosis. In this study, we evaluated the effects of a newly synthesized UII receptor (UT) antagonist, KR-36996, on the proliferation of SMCs in vitro and neointima formation in vivo in comparison with GSK-1440115, a known potent UT antagonist. In primary human aortic SMCs (HASMCs), UII (50 nM) induced proliferation was significantly inhibited by KR-36996 at 1, 10, and 100 nM which showed greater potency ($IC_{50}$: 3.5 nM) than GSK-1440115 ($IC_{50}$: 82.3 nM). UII-induced proliferation of HASMC cells was inhibited by U0126, an ERK1/2 inhibitor, but not by SP600125 (inhibitor of JNK) or SB202190 (inhibitor of p38 MAPK). UII increased the phosphorylation level of ERK1/2. Such increase was significantly inhibited by KR-36996. UII-induced proliferation was also inhibited by trolox, a scavenger for reactive oxygen species (ROS). UII-induced ROS generation was also decreased by KR-36996 treatment. In a carotid artery ligation mouse model, intimal thickening was dramatically suppressed by oral treatment with KR-36996 (30 mg/kg) which showed better efficacy than GSK-1440115. These results suggest that KR-36996 is a better candidate than GSK-1440115 in preventing vascular proliferation in the pathogenesis of atherosclerosis and restenosis.

Hydrogen Peroxide-induced Alterations in Na+-phosphate Cotransport in Renal Epithelial Cells

  • Jung, Soon-Hee
    • Korean Journal of Clinical Laboratory Science
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    • v.41 no.2
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    • pp.83-92
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    • 2009
  • This study was undertaken to examine the effect of oxidants on membrane transport function in renal epithelial cells. Hydrogen peroxide ($H_2O_2$) was used as a model oxidant and the membrane transport function was evaluated by measuring $Na^+$-dependent phosphate ($Na^+$-Pi) uptake in opossum kidney (OK) cells. $H_2O_2$ inhibited $Na^+$-Pi uptake in a dose-dependent manner. The oxidant also caused loss of cell viability in a dose-dependent fashion. However, the extent of inhibition of the uptake was larger than that in cell viability. $H_2O_2$ inhibited $Na^+$-dependent uptake without any effect on $Na^+$-independent uptake. $H_2O_2$-induced inhibition of $Na^+$-Pi uptake was prevented completely by catalase, dimethylthiourea, and deferoxamine, suggesting involvement of hydroxyl radical generated by an iron-dependent mechanism. In contrast, antioxidants Trolox, N,N'-diphenyl-p-phenylenediamine, and butylated hydroxyanisole did not affect the $H_2O_2$ inhibition. Kinetic analysis indicated that $H_2O_2$ decreased Vmax of $Na^+$-Pi uptake with no change in the Km value. Phosphonoformic acid binding assay did not show any difference between control and $H_2O_2$-treated cells. $H_2O_2$ also did not cause degradation of $Na^+$-Pi transporter protein. Reduction in $Na^+$-Pi uptake by $H_2O_2$ was associated with ATP depletion and direct inhibition of $Na^+$-$K^+$-ATPase activity. These results indicate that the effect of $H_2O_2$ on membrane transport function in OK cells is associated with reduction in functional $Na^+$-pump activity. In addition, the inhibitory effect of $H_2O_2$ was not associated with lipid peroxidation.

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Antioxidant Activity of Rosa rugosa Thunberg and Effect on Serum Lipid Level in High Fat Diet-induced Mice (해당화 열매 추출 분말의 항산화 활성과 고지방 식이로 유도된 Mice의 혈청지질 수준에 미치는 영향)

  • Choi, Kyung-Soon;Kim, Yong-Hwan;Lee, Ki-Won;Shin, Kyung-Ok
    • The Korean Journal of Food And Nutrition
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    • v.28 no.2
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    • pp.320-327
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    • 2015
  • Since Korean ancient times, powder of Rosa rugosa Thunberg has been used as a folk remedy. This study was conducted to verify the effects of Rosa rugosa Thunberg powder on in vitro antioxidant properties and serum lipid levels of high-fat diet-induced mice from a nutritional viewpoint. In the case of Rosa rugosa Thunberg powders, measurement of TPC, ABTS radical scavenging activity of trolox, DPPH radical scavenging activity, and measured value of FRAP were higher in ethanol extract than water extracts. For LDL-cholesterol concentration, mice fed 10% powder of Rosa rugosa Thunberg with high-fat diets showed a high numerical value compared with other groups (p<0.05). When testing for triglyceride concentrations in blood, mice fed 10% and 20% powder of Rosa rugosa Thunberg with high-fat diets showed the lowest numerical values (p<0.05). When testing for blood insulin concentrations, the high-fat diet group showed higher levels than compared to the control group (p<0.05). When testing for blood leptin concentrations, the high-fat diet group was $5.88{\pm}3.53ng/dL$, whereas mice fed 10% powder of Rosa rugosa Thunberg with high-fat diets showed a blood leptin level of $10.36{\pm}5.96ng/dL$ (p<0.05). Therefore, results prove that powder of Rosa rugosa Thunberg reduces triglyceride concentrations in the blood, and could be used as an excellent natural antioxidant in the future.

Hyaluronidase Inhibitory and Antioxidant Activities of Enzymatic Hydrolysate from Jeju Island Red Sea Cucumber (Stichopus japonicus) for Novel Anti-aging Cosmeceuticals

  • Ding, Yuling;Jiratchayamaethasakul, Chanipa;Kim, Eun-A;Kim, Junseong;Heo, Soo-Jin;Lee, Seung-Hong
    • Journal of Marine Bioscience and Biotechnology
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    • v.10 no.2
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    • pp.62-72
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    • 2018
  • An active ingredient with hyaluronidase (HAse) inhibitory effect is one of the anti-aging approaches in cosmeceuticals. Here, red sea cucumbers (RSCs), Stichopus japonicus, from Jeju Island were evaluated to examine their HAse inhibitory and antioxidant activity effect. In this study, RSCs were extracted by six enzymatic hydrolysis (Alcalase; Al, Trypsin; Try, Neutrase; Neu, Pepsin; Pep, Alpha-chymotrypsin; Chy and Protamex; Pro). Alcalase hydrolysate (AlH) showed the highest antioxidant capacities for both of oxygen radical absorbance capacity (ORAC) and trolox equivalent antioxidant capacity (TEAC) methods, compared to those of other hydrolysates, at $66.59{\pm}0.78{\mu}M\;TE/mg$ and $135.78{\pm}3.24{\mu}M\;TE/mg$, respectively. Furthermore, AlH performed the highest capacity of HAse inhibitory with $IC_{50}$ value of 3.21 mg/ml. Thus, RSCs hydrolyzed by Al were chosen to determine the cellular antioxidant activity and hyaluronic acid (HA) production effect on Human immortalized keratinocyte cell line (HaCaT). The results showed that AlH improved the cell viabilities and intracellular reactive oxygen species (ROS) induced by 2,2'-Azobis(2-amidinopropane) dihydrochloride (AAPH) were significantly decreased. In addition, AlH increased HA amount by regulating HYAL2 and HAS2 expressions in the HaCaT cells. Taken together, AlH of RSCs collected from Jeju Island showed HAse inhibitory and antioxidant activities against skin-aging which shows its potentials can be an optional natural bioactive ingredient for novel cosmeceuticals.

Antioxidative and Hepatocyte Protective Effects of Guava (Psidium guajava L.) Leaves Cultivated in Korea (국내산 구아바(Psidium guajava L.) 잎 추출물의 항산화 활성 및 간세포 보호효과)

  • Cheon, Wonyoung;Seo, Dongyeon;Kim, Younghwa
    • The Korean Journal of Food And Nutrition
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    • v.32 no.1
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    • pp.33-40
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    • 2019
  • The purpose of this study was to evaluate the antioxidant and hepatocyte protective effects of guava (Psidium guajava L.) leaves cultivated in Korea. The contents of the total polyphenol of the extract was 271.57 mg gallic acid equivalent (GAE)/g residue. Antioxidant activities of leaf extract were evaluated by examining the free radical scavenging ability. 2,2'-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) and ${\alpha}-{\alpha}$-diphenyl-${\beta}$-picrylhydrazyl (DPPH) free radical scavenging activities of the extract were 1133.23 mg trolox equivalent antioxidant capacity (TEAC)/g residue and 721.68 mg TEAC/g residue, respectively. The hepatocyte protective effect of guava leaf extract was examined in HepG2 cells. Against tert-butyl hydroperoxide (TBHP), the viability of HepG2 cells were increased by the treatment of leaf extract. In addition, guava leaf extract led to the inhibition of reactive oxygen species (ROS) generated in HepG2 cells. The leaf extract increased the activity of glutathione (GSH), glutathione reductase (GR), and glutathione peroxidase (GPx) against oxidative stress. These results suggested that guava leaves might be regarded as a potential source natural antioxidant and a hepatoprotective material.

Nutritional and antioxidative properties of black goat meat cuts

  • Kim, Hye-Jin;Kim, Hee-Jin;Jang, Aera
    • Asian-Australasian Journal of Animal Sciences
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    • v.32 no.9
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    • pp.1423-1429
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    • 2019
  • Objective: In this study, we evaluated the nutritional value and antioxidant activity of black goat loin (BGL) and black goat rump (BGR) meat. Methods: We evaluated the proximate compositions, collagen and mineral contents, and fatty acid compositions of BGL and BGR with respect to their nutritional value. The levels of bioactive compounds such as L-carnitine, creatine, creatinine, carnosine, and anserine were also measured. The ferric reducing antioxidant power (FRAP), 2,2-azinobis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) radical scavenging, and oxygen radical absorption capacity (ORAC) were assessed to evaluate the antioxidant activity of BGL and BGR. Results: BGR showed higher collagen, Fe, Ca, P, and Na contents than did BGL (p<0.05). Notably, the Ca/P ratio was high in both BGR and BGL (1.82 and 1.54, respectively), thus satisfying the recommendation that the Ca/P ratio is between 1 and 2. BGL showed a significantly higher content of desirable fatty acids (stearic acid and total unsaturated fatty acids) than did BGR. In addition, the levels of creatine, carnosine, and anserine in BGL were higher than those in BGR (p<0.05). There was no significant difference in the antioxidant activity between BGL and BGR, as assessed by FRAP (both $15.92{\mu}mol$ Trolox equivalent [TE]/g of dry matter [DM]), ABTS (12.51 and $12.90{\mu}mol\;TE/g\;DM$, respectively), and ORAC (101.25 and $99.06{\mu}mol\;TE/g\;DM$, respectively) assays. Conclusion: This was a primary study conducted to evaluate the differences in nutritional value and antioxidant activity between loin and rump cuts of black goat meat. Our results provide fundamental knowledge that can help understand the properties of black goat meat.

Evaluation of Clinical Usefulness of Herbal Mixture HO-Series for Improving Hangover (복합생약 HO-Series의 숙취개선 임상적 유용성 평가)

  • Chang, Bo Yoon;Bae, Jin Hye;Kim, Da Eun;Kim, Dae Sung;Cho, Hyoung Kwon;Kim, Sung Yeon
    • Korean Journal of Pharmacognosy
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    • v.51 no.4
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    • pp.278-290
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    • 2020
  • The purpose of this study is to investigate the hangover relieving effect of HO-series. HO-S1 is an herbal mixture, which consists of extracts from Flower of Pueraria lobata Ohwi, Glycyrrhiza glabra Linné, Fruit of Lycium chinense Miller, Poria cocos Wolf, Acanthopanax sessiliflorum Seeman, Scutellaria baicalensis Georgi, Atractylodes lancea De Candlle and Zingiber officinale Roscoe. HO-S2 is a candidate that has been performed to ultra filtration based on HO-S1. HO-S3 is a mixture of amino acids and vitamins based on HO-S2. HO-01 is the final beverage base produced based on HO-S3. The antioxidant activity of HO-series was similar to that of vitamin C or trolox. The production of t-BHP induced reactive oxygen species(ROS) was significantly blocked in the presence of HO-series. In vivo study, AUC of alcohol and acetaldehyde concentrations in HO-S2 and HO-S3 treated groups significantly decreased. Hepatic alcohol dehydrogenase(ADH) and acetaldehyde dehydrogenase(ALDH) activity were significantly higher in HO-S2 and HO-S3 treated groups. And 2E1 activity and glutathione were significantly elevated, while the malondialdehyde level was not significantly in liver tissue. After alcohol exposure, the sensitivity scores of blood alcohol and acetaldehyde concentration and hangover symptoms were significantly decreased in the HO-01 intake group compared with the non-intake group. ALDH activity was significantly increased in the HO-01 intake group. HO-series have antioxidant activity and a protective effect from ROS. HO-S2, HO-S3 and HO-01 are potentially highly beneficial in relieving hangover, as it scavenges reactive free radicals and boosts the endogenous antioxidant system.

Antioxidant and Hepatoprotective Activities of Bitter Melon (Momordica charantia Linn.) Leaves against Oxidative Stress (산화적 스트레스에 대한 여주(Momordica charantia Linn.)잎의 항산화 활성 및 간세포 보호능)

  • Jeon, Ahyeong;Cheon, Wonyoung;Yoon, Jimin;Kim, Dae-Jung;Kim, Younghwa
    • Journal of the Korean Society of Food Culture
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    • v.35 no.6
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    • pp.597-604
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    • 2020
  • This study examined the bioactive compound content and the antioxidant activities of bitter melon (Momordica charantia Linn.) leaves. The content of vitamin C, beta-carotene, and total carotenoids was 69.77, 45.68, and 65.08 mg/100 g, respectively. To investigate the antioxidant capacity, bitter melon leaves were extracted using various concentrations of ethanol (60, 80, or 100%). Highest content of total polyphenols (18.07 mg gallic acid equivalent/g) and flavonoids (4.53 mg cathechin equivalent/g) was found in the 100% ethanolic extract of the leaves (E100). Also, the E100 extract showed the highest levels of 2,2'azino-bis-3-ethylbenzothiazoline-6-sulfonic acid (ABTS) and α-α-diphenyl-β-picrylhydrazyl (DPPH) free radical scavenging activities. Reducing power was also the highest (39.21 mg Trolox equivalent/g) in E100 extract. The E100 extract effectively inhibited lipid peroxidation by 91.45% compared to the control group. Also, the E100 extract showed a cytoprotective effect against oxidative stress in HepG2 cells and decreased the generation of intracellular reactive oxygen species. These results suggest that bitter melon leaves could be regarded as a potential source of natural antioxidants.

Quality characteristics and antioxidant activities of jams according to varying ratios of aronia (아로니아 첨가 비율에 따른 프리저브 잼의 품질 특성 및 항산화 활성)

  • Im, Sang Hwi;Kim, Kyeoung Cheol;Kim, Ju-Sung
    • Korean Journal of Food Science and Technology
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    • v.54 no.2
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    • pp.141-146
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    • 2022
  • This study investigated the quality characteristics and antioxidant activities of preserved jams prepared by mixing various ratios of aronia and sugar. To analyze the quality characteristics, the total sugar, pH, moisture, maximum stress, hardness, total phenolics, 1,1-diphenyl-2-picrylhydrazyl (DPPH), trolox-equivalent antioxidant capacity (TEAC), ferric reducing antioxidant power (FRAP), oxygen radical absorbance capacity (ORAC), and sensory characteristics of the preserved jams were measured. Lower aronia contents resulted in higher total sugar content, hardness, and strength, as well as lower moisture, total phenolic content, and DPPH, TEAC, FRAP, and ORAC values. In terms of the sensory characteristics, an aronia content of 30%, which was determined to have strong sweetness and texture, resulted in the lowest overall acceptability. In contrast, the highest preference was shown to an aronia content of 40%. In this study, quality characteristics and antioxidant activity experiments were conducted based on various ratios of aronia and sugar. The results are expected to be used as preliminary data for developing products that use domestic aronia.

Purification and Characterization of Antioxidant Peptides from Lotus Nelumbo nucifera Seed Protein (연자육(Lotus Nelumbo nucifera Seed) 단백질로부터 항산화 펩타이드 분리 정제 및 특성)

  • Chathuri K. Marasinghe;Hyun-Woo Kim;Won-Kyo Jung;Jae-Young Je
    • Korean Journal of Fisheries and Aquatic Sciences
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    • v.56 no.1
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    • pp.21-27
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    • 2023
  • Lotus Nelumbo nucifera seed protein (LSP) was isolated by alkaline solubilization after removing fat and phenolics by hexane and ethanol treatment. Antioxidant peptides from LSP were produced with Alcalase® and pepsin and hydroxyl radical scavenging activities were determined. LSP-Alcalase® hydrolysates showed higher hydroxyl radical scavenging activity than LSP-pepsin hydrolysates. To purify antioxidant peptides, LSP-Alcalase® hydrolysates were subjected to high performance liquid chromatography (HPLC) separation on the C18 column and the active fraction was further purified using a SuperdexTM peptide 10/300 GL column. Finally, the active fraction (F8-2) was evaluated for antioxidant activities by 2,2-diphenyl-1-picrylhydrazyl (DPPH), hydroxyl radical scavenging, and oxygen radical absorbance capacity (ORAC) assays. The EC50 values of the F8-2 were 105.81±0.02 ㎍/mL for DPPH and 32.26±0.02 ㎍/mL for hydroxyl radical and the F8-2 exhibited 7.22 μM trolox equivalent (TE)/100 ㎍ F8-2. Glutathione (GSH), which is a positive control, showed EC50 values of 19.87±0.01 ㎍/mL for DPPH and 15.95±0.03 ㎍/mL for hydroxyl radical and an ORAC value of 14.17±0.03 μM TE/100 ㎍ GSH. Finally, sixteen peptides were identified by liquid chromatography-tandem mass spectrometry (LC-MS/MS). Among them, Ile-Tyr and Leu-Tyr showed higher antioxidant scores.