• Title/Summary/Keyword: Enzyme inhibition

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Chiral effect of fenoxaprop-ethyl on rice (Orysa sativa) and barnyardgrass (Echinochloa crus-galli) (벼와 피에 대한 Fenoxaprop-ethyl의 이성체효과)

  • Kim, Tae-Joon;Kim, Jin-Seog;Cho, Jeong-Sup;Chang, Hae-Sung;Cho, Kwang-Yun
    • The Korean Journal of Pesticide Science
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    • v.5 no.2
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    • pp.58-61
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    • 2001
  • A greenhouse study was conducted to evaluate the effect of R(+), S(-) and racemic mixture of fenoxaprop-ethyl on rice and barnyardgrass. In addition, in wire acetyl-coenzyme A carboxylase inhibition to those chiral compounds was determined. In the greenhouse trial, the R(+) and S(-) fenoxaprop showed respectively tile highest and the lowest biological activity on both plants. This dose-response in whole plant level was consistent with the result of in vitro dose-response of acetyl-coenzyme A carboxylase. These results corfirmed tllat the R(+) isomer is biologically more active than the S(-) isomer, and the target site of fenoxaprop is the enzyme acetyl-coenzyme A carboxylase. It was an interesting result that rice safety was improved in the S(-) isomer compared with the R(+), and the respective selectivity index was 1.5 and 0.57 in a greenhouse experiment; however, those values resulting from ACCase assay were not substantially different each other at in vitro level. Those results suggested that the fundamental selectivity of fenoxaprop-ethyl between rice and barnyardgrass would not exist at target site level.

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Inhibitory Activity of the Extracts from the Pigmented Rice Brans on Inflammatory Reactions (유색미 겨 추출물의 염증반응 억제활성)

  • Choi, Sun-Phil;Kang, Mi-Young;Nam, Seok-Hyun
    • Applied Biological Chemistry
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    • v.47 no.2
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    • pp.222-227
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    • 2004
  • Effects of the extracts from bran part of the pigmented rices on inflammation was evaluated by determining their inhibitory action on the production of nitric oxides, histamines and matrix metalloproteinase(MMP) from inflammatory leukocytes. Effects on the production of nitric oxides in a macrophage cell line, RAW264.7 cells, were determined, demonstrating that any significant difference was not detected between the normal rice and the pigmented rice extracts. Inhibitory effects on the histamine-release from a basophilic cell line, RBL-2H3, were examined, showing 3.6 to 5.4-fold increase in the inhibitory activity compared to that of the normal rices. Among the pigmented rice cultivars tested, especially, inhibitory activity of LK1-3-6-12-1-1 was the greatest. Using RAW264.7 cells, we examined the effect of the pigmented rice extracts on the MMP activity. The results showed that the enzyme activity increased with the increasing concentration of the normal rice extract. However, the pigmented rice extracts, except LK1A-2-12-1-l, acted to decrease the MMP activity with their increasing concentrations. The results described above showed the superiority of the pigmented rice extracts in inhibition on release of histamine and MMP, pivotal factors for causing inflammatory responses, from the leukocytes.

Experimental Study on Anti-inflammatory, Antitussive, and Expectoration Effects of Friltillariae Thunbergii Bulbus (절패모(浙貝母)의 항염 및 진해거담 효과에 대한 실험연구)

  • Kim, Jin Hoo;Yang, Won Kyung;Lee, Su Won;Lyu, Yee Ran;Kim, Seung Hyung;Park, Yang Chun
    • The Journal of Internal Korean Medicine
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    • v.41 no.3
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    • pp.339-349
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    • 2020
  • Objective: This study aimed to evaluate anti-inflammatory and antitussive expectoration effects of Friltillariae Thunbergii Bulbus (FTB) in a mouse model. Materials and Methods: To evaluate the anti-inflammatory effects of the FTB, we conducted in vitro experiments using RAW264.7 cells. An MTT assay and enzyme-linked immunosorbent assay (ELISA) were carried out to examine the anti-inflammatory effects of FTB. The expectorant effect on phenol red secretion, the antitussive effect on cough induced by ammonia solution, and leukocyte increased inhibition effects in acute airway inflammation in the animal model were confirmed. Results: FTB did not show cytotoxicity in the experimental group at 10, 30, 50, 100, 300, or 500 ㎍/ml and significantly inhibited the increase of NO, TNF-α and IL-6 in the experimental groups at 30, 50, 100, 300, and 500 ㎍/ml concentrations. In sputum, cough, and acute airway inflammation animal models, FTB significantly increased phenol red secretion in the 400 mg/kg administration group. FTB significantly reduced the number of coughs and significantly increased cough delay time in both 200 and 400 mg/kg dose groups. FTB decreased the white blood cell count in BALF (bronchoalveolar lavage fluid) in the 400 mg/kg administration group. Conclusion: Our study revealed that FTB elicits antitussive and expectorant effects by inhibiting inflammatory cytokines, increasing sputum secretion, suppressing cough, and reducing inflammatory cells. We concluded that FTB is a highly promising agent for respiratory tract infection with therapeutic opportunities.

Blood Pressure Modulating Effects of Black Raspberry Extracts in vitro and in vivo (복분자 추출물의 항고혈압 활성)

  • Lee, Jung-Hyun;Choi, Hye Ran;Lee, Su Jung;Lee, Min Jung;Ko, Young Jong;Kwon, Ji Wung;Lee, Hee Kwon;Jeong, Jong Tae;Lee, Tae-Bum
    • Korean Journal of Food Science and Technology
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    • v.46 no.3
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    • pp.375-383
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    • 2014
  • This study aimed to investigate the effects of 50% ethanol extract of ripe black raspberry (Rubus occidentalis, RBR) on hypertension in human umbilical vein endothelial cells (HUVECs) and in spontaneously hypertensive rats (SHR). Angiotensin converting enzyme (ACE) inhibition and activation of nitric oxide production by endothelial nitric oxide synthase were significantly regulated by RBR in HUVEC cells. Moreover, the SHR showed significantly higher levels of blood pressure, ACE, renin, endothelin-1, and interleukin-6 than Wistar Kyoto rats (WKY). However, treatment with captopril and RBR decreased the levels of these hypertension-related events in the SHR. The renal arteriole showed greater media thickness/lumen diameter (%) in the SHR than in the WKY. However, media thickness/lumen diameter (%) was reduced in SHR by treatment with captopril and RBR. In addition, the number of eosinophilic cardiac muscle cells was decreased in the heart muscles after treatment with captopril and RBR. Therefore, this study suggests that 50% ethanol extract of RBR may be useful for the prevention and treatment of high blood pressure.

The Effects of Fermented Anchovy on the Bromobenzene-Induced Hepatic Lipid Peroxidation in vitro (시험관내에서 멸치액젓이 Bromobenzene유발 간조직 지질과산화에 미치는 효과)

  • Park, Jong-Ok;Choi, Jong-Won;Kim, Hee-Sook;Ryu, Byung-Ho
    • Korean Journal of Food Science and Technology
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    • v.32 no.5
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    • pp.1179-1185
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    • 2000
  • Fermented anchovy was used to investigate its effects on the formation of lipid peroxide and the activities of epoxide or free radical generating enzyme in vitro in bromobenzene-treated rats. All solvent fractions from fermented anchovy not only showed the strong antioxidative activities on linoleic acid autooxidation, but also reduced bromobenzene-induced hepatic lipid peroxidation. The activities of aniline hydroxylase and aminopyrine N-demethylase elevated by bromobenzene were recovered to the level of normal rats by adding the solvent fractions of fermented anchovy. But, xanthine oxidase and aldehyde oxidase activities were not affected by fermented anchovy. These results suggest that reduction of the bromobenzene-induced hepatic lipid peroxidation is caused by inhibition on the epoxide formation, not on free radical generation.

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Effects of 17β-Estradiol on Colonic Permeability and Inflammation in an Azoxymethane/Dextran Sulfate Sodium-Induced Colitis Mouse Model

  • Song, Chin-Hee;Kim, Nayoung;Sohn, Sung Hwa;Lee, Sun Min;Nam, Ryoung Hee;Na, Hee Young;Lee, Dong Ho;Surh, Young-Joon
    • Gut and Liver
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    • v.12 no.6
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    • pp.682-693
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    • 2018
  • Background/Aims: Intestinal barrier dysfunction is a hallmark of inflammatory bowel diseases (IBDs) such as ulcerative colitis. This dysfunction is caused by increased permeability and the loss of tight junctions in intestinal epithelial cells. The aim of this study was to investigate whether estradiol treatment reduces colonic permeability, tight junction disruption, and inflammation in an azoxymethane (AOM)/dextran sodium sulfate (DSS) colon cancer mouse model. Methods: The effects of $17{\beta}$-estradiol (E2) were evaluated in ICR male mice 4 weeks after AOM/DSS treatment. Histological damage was scored by hematoxylin and eosin staining and the levels of the colonic mucosal cytokine myeloperoxidase (MPO) were assessed by enzyme-linked immunosorbent assay (ELISA). To evaluate the effects of E2 on intestinal permeability, tight junctions, and inflammation, we performed quantitative real-time polymerase chain reaction and Western blot analysis. Furthermore, the expression levels of mucin 2 (MUC2) and mucin 4 (MUC4) were measured as target genes for intestinal permeability, whereas zonula occludens 1 (ZO-1), occludin (OCLN), and claudin 4 (CLDN4) served as target genes for the tight junctions. Results: The colitis-mediated induced damage score and MPO activity were reduced by E2 treatment (p<0.05). In addition, the mRNA expression levels of intestinal barrier-related molecules (i.e., MUC2, ZO-1, OCLN, and CLDN4) were decreased by AOM/DSS-treatment; furthermore, this inhibition was rescued by E2 supplementation. The mRNA and protein expression of inflammation-related genes (i.e., KLF4, NF-${\kappa}B$, iNOS, and COX-2) was increased by AOM/DSS-treatment and ameliorated by E2. Conclusions: E2 acts through the estrogen receptor ${\beta}$ signaling pathway to elicit anti-inflammatory effects on intestinal barrier by inducing the expression of MUC2 and tight junction molecules and inhibiting pro-inflammatory cytokines.

Effects of Cactus Extracts on Human Intestinal Microflora (선인장 추출물이 인체 장내미생물에 미치는 영향)

  • Ra, Bo-Hyun;Lee, Woon-Jong;Cho, Yun-Won;Kim, Kwang-Yup
    • Journal of agriculture & life science
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    • v.43 no.3
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    • pp.45-54
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    • 2009
  • This study was designed to investigate the effect of cactus (Opuntia ficus-indica var. saboten) extracts on the intestinal bacteria, antioxidative activity and angiotensin -I-converting enzyme(ACE) inhibitory activity. The antimicrobial activities were measured using the 96well-plate method and disc plate method with concentration of 20mg of cactus extract. The stem extract of cactus was inhibitory against Eubacterium limosum, Clostridium perfringens, C. butyricum, C. difficile and Staphylococcus aureus, but was not inhibitory against Bacteroides fragilis, Bifidobacterium bifidum, Lactobacillus acidophilis, Streptococcus thermophilus. The fruit extract of cactus showed no inhibition against Bacteroides fragilis, Bifidobacterium bifidum, Lactobacillus acidophilis, and Streptococcus thermophilis. Their inhibitory activities were not reduced after heat and pH treatment. Antioxidative effects of cactus extracts showed high total polyphenol and flavonoid contents and high activity against free radical DPPH. The stem and fruit extract of cactus showed strong ACE inhibitory activities of 88.8% and 69.2%, respectively. In conclusion cactus (Opuntia ficus-indica var. saboten) extract might be utilized as a functional food material to control intestinal microflora.

Screeening of Natural Plant Resources with Acetylcholine esterase inhibitory activity and Effect on Scopolamine-induced Memory Impairment (천연식물자원으로부터 Acetylcholine esterase 저해 활성 탐색 및 인지기능에 미치는 영향)

  • Choi, Jang Won;Won, Mu-Ho;Joo, Han-Seung
    • Journal of agriculture & life science
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    • v.45 no.6
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    • pp.213-226
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    • 2011
  • This study was performed to investigate the effect of essential oils and ethanolic extracts of approximately 650 plant species on acetylcholine esterase (AChE) enzyme activity using Ellman's colorimetric method in 96-well microplates. The results showed that the ethanolic extracts from twig of Sophora subprostrata, twig of Phellodendron amurense, seed of Corylopsis coreana, and essential oil (EO) from Citrus paradisi, Cupressus sempervirens, Ocimum basilicum, Pinus sylvestris and Rosmarinus officinalis inhibited more than 80% of AChE activity. Among these, EO from Pinus sylvestris, C. sempervirens and C paradisi exhibited higher values of AChE inhibitory activity, which were 75, 84 and 99% at a concentration of 50 ug/ml, respectively. Finally, EO from C paradisi (grapefruit, GEO) showed the highest inhibitory activity towards AChE, which showed 91% of inhibition at a concentration of 20 ug/ml. We also examined the anti-dementia effects of GEO in mouse by passive avoidance test and Morris water maze test. The model mouse (male, ICR) of dementia (negative control) was induced by administration of scopolamine (1 mg/kg body weight). The latency time of sample group administrated with GEO (100 mg/kg, p.o.) increased significantly as compared with negative control on passive avoidance test. There were significant recovery from the scopolamine-induced deficits on learning and memory in water maze test through daily administrations with GEO (100 mg/kg, p.o.). From these results, we conclude that GEO treatment might enhance the cognitive function, suggesting that the EO of C. paradis may be a potential candidate for improvement of perceptive ability and dementia.

Effects of Autoclaved Morinda officinalis Root Extract on the Suppressive Efficacy of MMP-1 Enzyme (고온고압 처리된 파극천 추출물의 MMP-1 발현 억제 효능 증진)

  • Kang, Jung Wook;Oh, Jung Young;Bae, Jun Tae;Kim, Jin Hwa;Lee, Geun Soo;Pyo, Hyeong Bae
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.41 no.1
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    • pp.35-43
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    • 2015
  • Morinda officinalis (Rubiaceae) is a medicinal herb that has traditionally been used for the treatment of skin inflammation. The present study was to investigate the inhibitory efficacy of matrix metalloproteinases-1 (MMP-1) of the extracts of the root of M. officinalis, which was autoclaved at $132^{\circ}C$ and $1.2kgf/cm^2$ for 15 min using an autoclave. The composition of the extracts were compared with that prepared without autoclaved treatment. Total phenol and flavonoid contents were analyzed for the autoclaved M. officinalis root extract (AME) and M. officinalis root extract (ME). Results showed that the autoclaved AME contained total phenol and flavonoid contents 1.5-fold times more than those from ME. AME showed DPPH and superoxide radical scavenging activities as 79.25% and 94.5%, respectively, at the concentration of $500{\mu}g/mL$. In anti-inflammatory assay, AME inhibited the activity of COX-2 and 5-LOX metabolites. In addition, AME showed higher an inhibition rate in MMP-1 expression than ME in UVA-irradiated human dermal fibroblast (HDF) without any significant cytotoxicity. UVB-induced cytotoxicity and cell death were effectively suppressed by AME. In conclusion, autoclaving the M. officinalis root increased the phenol and flavonoid contents. The extracts of the autoclaved M. officinalis enhanced the antioxidant, anti-inflammatory and anti-MMP-1 effects. Thus, the extracts could be an useful active ingredient in cosmetics.

Utilization of Multiple Carbon Sources by Plant Cells

  • Lee, Taek-Kyun;Suh, Jung-Bin;Kim, Se-Hee;Lee, Sun-Min;Lee, Woo-Sung
    • Proceedings of the Zoological Society Korea Conference
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    • 1999.10b
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    • pp.11-11
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    • 1999
  • ;It has been reported that suspension-cultured rice cells grown on mixed carbon sources of glucose (GIc) and acetate exhibited diauxic growth in which acetate was the preferred carbon source (Lee and Lee, 1996). Carrot (Daucus carota L.) suspension cells, showing a diauxic growth very similar to that of rice cells, were used to delineate the mechanisms underlying this preferential use of acetate over GIc. Uptakes of both GIc and 3-0-methylglucose (3-0MG), a non-metabolizable GIc analogue, were similarly inhibited when acetate or butylate, weak acids which are capable of transporting protons into the cytosol, were present in the uptake assay mixture containing cells harvested during the GIc-utilizing second growth phase. Inhibition of GIc uptake by these weak acids was similar when equivalent experiments were carried out with isolated plasma membranes. It was further shown that Glc uptake, which requires a proper proton gradient across the plasma membranes, was inhibited during the first growth phase by acetate-mediated alkalization of growth medium and/or simultaneous acidification of cytosol. This study strongly suggests that Glc utilization in plant cells is inhibited by co-presenting carbon source(s) which can alter the proton gradient across the plasma membrane. We further examined diauxic growth in culture containing GIc and malate. Unlike the case in the culture with GIc and acetate, carrot cells used GIc first. Malate was utilized only after Glc is depleted from medium. These results indicate that GIc can be a preferred or less-preferred carbon source depending on the competing carbon source. It was noted that malate was not directly taken up by cells. Instead it was converted extracellularly into fumarate which was subsequently transported into cells. During the malate-growth phase malate uptake was negligible, and fumarate uptake was active and pH-sensitive. It was shown that fumarase released into medium was responsible for the extracellular conversion of malate into fumarate. An immunoblot experiments showed that fumarase antibody raised against Arabidopsis fumarase provided positive signals only in medium in malate culture, not in fumarate or GIc cultures. This study demonstrates the first example in that fumarase, a mitochondria marker enzyme, can be present in places other than mitochondria.ndria.

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