• Title/Summary/Keyword: Enzyme inhibition

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The Anti-Inflammatory Effects of Persicaria thunbergii Extracts on Lipopolysaccharide-Stimulated RAW264.7 Cells (Lipopolysaccharide로 처리 된 RAW264.7 세포에서 고마리 추출물의 항염증 효과)

  • Kim, Sang-Bo;Seong, Yeong-Ae;Jang, Hee-Jae;Kim, Gun-Do
    • Journal of Life Science
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    • v.21 no.12
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    • pp.1689-1697
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    • 2011
  • In this study, we investigated the anti-inflammation effect of Persicaria thunbergii (P. thunbergii) on RAW 264.7 murine macrophage cells. The anti-inflammatory activity of P. thunbergii was determined by measuring expression of the LPS-induced inflammatory proteins, inducible nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2) and nuclear factor-${\kappa}B$ (NF-${\kappa}B$), and the production of nitric oxide (NO) and prostaglandin $E_2$ ($PGE_2$). Methanol extract of P. thunbergii decreased the expression of iNOS, COX-2 and NF-${\kappa}B$, and increased the expression of HO-1 in LPS-stimulated RAW264.7 cells. Methanol extract was fractioned by n-butanol, hexane and ethyl acetate (EtOAc) and each fraction was tested for inhibitory effects on inflammation. Among the sequential solvent fractions, the EtOAc soluble fraction was investigated by the expression of prostaglandin $E_2$ ($PGE_2$), and showed decreasing form to the dose-dependent manner. EtOAc extract showed the most effective inhibitory activity of the expression of iNOS, COX-2 and NF-${\kappa}B$, and the production of NO. The study showed that P. thunbergii has anti-inflammatory activity through the decrease of NO and inhibition of iNOS, COX-2, $PGE_2$ and NF-${\kappa}B$ expression, and by the increase of HO-1 enzyme. This study needs for more investigation to find out the most effective single compound with anti-inflammatory activity.

Anti-oxidative and Anti-inflammatory Activities of Decaisnea insignis Ethanol Extract (Decaisnea insignis 에탄올 추출물의 항산화 및 항염증 활성)

  • Jin, Kyong-Suk;Lee, Ji Young;Kwon, Hyun Ju;Kim, Byung Woo
    • Journal of Life Science
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    • v.24 no.9
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    • pp.973-980
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    • 2014
  • This study was conducted to explore new nutraceutical resources from the plant kingdom possessing biological activities. To fulfill this purpose, the anti-oxidative and anti-inflammatory activities of Decaisnea insignis ethanol extract (DIEE) were evaluated. First, DIEE possessed potent scavenging activity against 1,1-diphenyl-2-picryl hydrazyl (DPPH), similar to ascorbic acid used as a positive control. Moreover, DIEE inhibited lipopolysaccharide (LPS)- and hydrogen peroxide ($H_2O_2$)-induced reactive oxygen species (ROS) in RAW 264.7 cells. Furthermore, DIEE induced the expression of an anti-oxidative enzyme, heme oxygenase 1 (HO-1), and its upstream transcription factor, nuclear factor-E2-related factor 2 (Nrf2), in a dose-dependent manner. The modulation of the HO-1 and Nrf2 expressions might be regulated by mitogen-activated protein kinases (MAPKs) and their upstream signaling pathways. On the other hand, DIEE suppressed LPS-induced nitric oxide (NO) formation without cytotoxicity. The inhibition of the NO formation was the result of the downregulation of inducible NO synthase (iNOS) by DIEE. The suppression of NO and iNOS by DIEE might be modulated by their upstream transcription factors, nuclear factor ${\kappa}B$ ($NF-{\kappa}B$), and activator protein 1 (AP-1) pathways. Taken together, these results provide important new insights that D. insignis possesses anti-oxidative and anti-inflammatory activities. Therefore, it might be utilized as a promising material in the field of nutraceuticals.

Functional Role of Peptide Segment Containing 1-25 Amino Acids in N-terminal End Region of ErmSF (ErmSF에서 특이적으로 발견되는 N-terminal end region에 존재하는 1-25번째 아미노산을 함유하는 peptide segment의 효소 활성에서의 역할)

  • Jin, Hyung-Jong
    • Korean Journal of Microbiology
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    • v.42 no.3
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    • pp.165-171
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    • 2006
  • ERM proteins transfer the methyl group to $A_{2058}$ in 23S rRNA to confer the resistance to MLS (macrolide-lincosamide-streptogramin B) antibiotics on microorganism ranging from antibiotic producers to pathogens. To define the functional role of peptide segment encompassing amino acid residues 1 to 25 in NTER (N-terminal end region) of ErmSF, one of the ERM proteins, DNA fragment encoding mutant protein deprived of that peptide was cloned and overexpressed in E. coli to obtain a purified soluble form protein to the apparent homogeneity in the yield of 12.65 mg per liter of culture. The in vitro activity of mutant protein was found to be 85% compared to wild type ErmSF, suggesting that this peptide interact with substrate to affect the enzyme activity. This diminished activity of mutant protein caused the delayed expression of antibiotic resistance in vivo, that at fIrst cells expressing mutant protein showed the retarded growth due to the antibiotic action but with time cells inhibited by antibiotic gradually recovered the viability to exert the resistance to the same extent as those with wild type protein.

Effect of Prunetin on TNF-${\alpha}$-Induced MUC5AC Mucin Gene Expression, Production, Degradation of $I{\kappa}B$ and Translocation of NF-${\kappa}B$ p65 in Human Airway Epithelial Cells

  • Ryu, Jiho;Lee, Hyun Jae;Park, Su Hyun;Sikder, Md. Asaduzzaman;Kim, Ju-Ock;Hong, Jang-Hee;Seok, Jeong Ho;Lee, Choong Jae
    • Tuberculosis and Respiratory Diseases
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    • v.75 no.5
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    • pp.205-209
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    • 2013
  • Background: We investigated whether prunetin significantly affects tumor necrosis factor-${\alpha}$ (TNF-${\alpha}$)-induced MUC5AC mucin gene expression, production, inhibitory kappa B ($I{\kappa}B$) degradation and nuclear factor kappa B (NF-kB) p65 translocation in human airway epithelial cells. Methods: Confluent NCI-H292 cells were pretreated with prunetin for 30 minutes and then stimulated with TNF-${\alpha}$ for 24 hours or the indicated periods. MUC5AC mucin gene expression and mucin protein production were measured by reverse transcription polymerase chain reaction and enzyme-linked immunosorbent assay, respectively. The effect of prunetin on TNF-${\alpha}$-induced degradation of $I{\kappa}B$ and translocation of NF-${\kappa}B$ p65 was investigated by western blot analysis. Results: We found that incubation of NCI-H292 cells with prunetin significantly inhibited mucin production and down-regulated the MUC5AC gene expression induced by TNF-${\alpha}$. Prunetin inhibited TNF-${\alpha}$-induced degradation of $I{\kappa}B$ and translocation of NF-${\kappa}B$ p65. Conclusion: This result suggests that prunetin inhibits the NF-${\kappa}B$ signaling pathway, which may explain its role in the inhibition of MUC5AC mucin gene expression and production regulated by the NF-${\kappa}B$ signaling pathway.

Antioxidant and Whitening Effects of Sorbus commixta HEDL Cortex Extract (정공피 추출물의 항산화 활성 및 미백효과에 관한 연구)

  • Kim, Tae-Hyuk;You, Jin-Kyoun;Kim, Jeong-Mi;Baek, Jong-Mi;Kim, Hyun-Sook;Park, Jeong-Hae;Choe, Myeon
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.39 no.10
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    • pp.1418-1424
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    • 2010
  • This study was performed to assess the antioxidant activities and whitening effects of Sorbus commixta HEDL cortex on melanin synthesis. The whitening effects of Sorbus commixta HEDL cortex water extracts were examined by in vitro mushroom tyrosinase assay and B16BL6 melanoma cells. We assessed inhibitory effects of Sorbus commixta HEDL cortex water extracts on expression of melanogenic enzyme proteins including tyrosinase, tyrosinase-related protein 1 (TRP-1) and tyrosinase-related protein 2 (TRP-2) in B16BL6 cells. Inhibitory effects of Sorbus commixta HEDL cortex onto free radical generation were determined by measuring DPPH and hydroxyl radical scavenging activities. Our results indicated that Sorbus commixta HEDL cortex water extracts effectively inhibited free radical generation. In DPPH radical scavenging activity, Sorbus commixta HEDL cortex water extracts had a potent anti-oxidant activity in a dose-dependent manner. They significantly inhibited tyrosinase activity in vitro and in B16BL6 melanoma cells. Also, Sorbus commixta HEDL cortex suppressed the expression of tyrosinase, TRP-1 and TRP-2 in B16BL6 melanoma cells. These results show that Sorbus commixta HEDL cortex inhibited melanin production on the melanogenesis. The underlying mechanism of Sorbus commixta HEDL cortex on whitening activity may be due to the inhibition of tyrosinase activity and tyrosinase, TRP-1, TRP-2 expression. We suggest that Sorbus commixta HEDL cortex may be contain new natural active ingredients for antioxidant and whitening cosmetics.

Acetylcholinesterase Inhibitory Effect of Green Tea Extracts According to Storage Condition (저장 조건에 따른 녹차 추출물의 acetylcholinesterase(AChE) 저해 효과)

  • Kwak, Ji Hyun;Jeong, Chang-Ho;Kim, Ji Hye;Choi, Gwi Nam;Shin, Young-Hee;Lee, Seung-Cheol;Cho, Sung Hwan;Choi, Sung-Gil;Heo, Ho Jin
    • Korean Journal of Food Science and Technology
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    • v.41 no.4
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    • pp.435-440
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    • 2009
  • Acetylcholinesterase (AChE) inhibitors, which enhance cholinergic transmission by reducing the enzymatic degradation of acetylcholine, are the only source of the compound that is currently approved for the treatment of Alzheimer's disease (AD). In these experiments, the concentration samples of green tea extracts were 100, 500, and 1,000 ${\mu}g$/mL. Among them, the highest concentration (1,000 ${\mu}g$/mL) of fresh green tea extracts showed the most potent inhibitory effect on AChE by reducing more than 40% of enzyme activity, and in a concentration-dependent pattern. In addition, we examined the effect of other storing conditions on AChE inhibition. In order to maintain storage for 3 months, the materials were held at the certain storing conditions of temperature (room temperature, 4 and $-20^{\circ}C$) and for water activity (0.81, 0.69, and 0.23). In these storing conditions, the difference in temperature did not contribute to the AChE inhibitory effect. Our presented data showed that the AChE inhibitory effect was affected by the concentration of green tea extract and by water activity (0.81). These results suggest that green tea may serve as a potential dietary source of AChE inhibitor.

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.