• 제목/요약/키워드: Inhibitory Activity

검색결과 7,150건 처리시간 0.039초

Inhibitory Effects of Epigallocatechin-3-Gallate on Microsomal Cyclooxygenase-1 Activity in Platelets

  • Lee, Dong-Ha;Kim, Yun-Jung;Kim, Hyun-Hong;Cho, Hyun-Jeong;Ryu, Jin-Hyeob;Rhee, Man Hee;Park, Hwa-Jin
    • Biomolecules & Therapeutics
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    • 제21권1호
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    • pp.54-59
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    • 2013
  • In this study, we investigated the effect of (-)-epigallocatechin-3-gallate (EGCG), a major component of green tea catechins from green tea leaves, on activities of cyclooxygenase (COX)-1 and thromboxane synthase (TXAS), thromboxane $A_2$ ($TXA_2$) production associated microsomal enzymes. EGCG inhibited COX-1 activity to 96.9%, and TXAS activity to 20% in platelet microsomal fraction having cytochrome c reductase (an endoplasmic reticulum marker enzyme) activity and expressing COX-1 (70 kDa) and TXAS (58 kDa) proteins. The inhibitory ratio of COX-1 to TXAS by EGCG was 4.8. These results mean that EGCG has a stronger selectivity in COX-1 inhibition than TXAS inhibition. In special, a nonsteroid anti-inflammatory drug aspirin, a COX-1 inhibitor, inhibited COX-1 activity by 11.3% at the same concentration ($50{\mu}M$) as EGCG that inhibited COX-1 activity to 96.9% as compared with that of control. This suggests that EGCG has a stronger effect than that of aspirin on inhibition of COX-1 activity. Accordingly, we demonstrate that EGCG might be used as a crucial tool for a strong negative regulator of COX-1/$TXA_2$ signaling pathway to inhibit thrombotic disease-associated platelet aggregation.

생약의 류코트리엔 $B_4$ 수용체결합 저해작용 검색 (Screening of Leukotriene $B_4$ Receptor Antagonist Activity from the Herbal Drugs)

  • 이화진;류재하
    • 생약학회지
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    • 제31권3호
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    • pp.273-279
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    • 2000
  • Leukotriene $B_4\;(LTB_4)$ is a pro-inflammatory mediator synthesized in myeloid cells from arachidonic acid. Elevated levels of $LTB_4$ have been found in a number of inflammatory diseases and levels are related to disease activity in some of these. Because $LTB_4$ interacts with cells through specific cell surface receptors, $LTB_4$ receptor blockade is the most specific approach to reduce the pathogenic role of $LTB_4$. In order to find $LTB_4$ receptor antagonist from plants, we screened the $LTB_4$ receptor antagonistic activity of the methanol extract and solvent fractions of herbal drugs. The ability of samples to inhibit specific binding of $[^3H]-LTB_4$ to human peripheral neutrophils was used as assay to evaluate the antagonistic activity of plant materials. Among the tested methanol extracts of herbal drugs, Mori Radicis Cortex, Perillae Semen, Armeniacae Semen and Sophorae subprostratae Radix showed potent inhibitory activity above 70% at the concentration of $100\;{mu}g/ml$. The inhibitory activities of $LTB_4$ binding to human neutrophils were evaluated for several solvent fractions at three different concentrations. Especially, hexane soluble fractions of Anemarrhenae Rhizoma and Embeliae Radix, and ethyl acetate soluble fractions of Aristolochiae Fructus, Magnoliae Cortex and Zingiberis Rhizoma crudus showed moderate activity at $25\;{mu}g/ml$. These fractions were promising candidates for the study of the activity-guided chromatographic purification of active compounds. Silica gel column chromatography of hexane soluble fractions of Anemarrhenae Rhizoma and Embeliae Radix gave very active sub-fractions, AA-4 and ES-4, and their inhibition activities of $LTB_4$ binding to human neutrophil at $30\;{mu}g/ml$ were 78% and 62%, respectively. From these results we could anticipate new $LTB_4$ receptor antagonist from herbal drugs, and the block of $LTB_4$ effects may provide beneficial in neutrophil mediated diseases such as inflammation and bronchial asthma.

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구증구포 처리 대두 추출물의 항산화 활성 및 Angiotensin-I Converting Enzyme 저해 효과 (Effect on Angiotensin-I Converting Enzyme Inhibition and Antioxidant Activities of Soybean (Glycine max L.) following Steaming and Drying Nine Times)

  • 김현영;서혜영;서우덕;이미자;최만수;함현미
    • 한국식품영양학회지
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    • 제33권2호
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    • pp.167-173
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    • 2020
  • To increase the functional material content of soybean, a repetitive steaming and drying process was used. We investigated the changes in the total polyphenol content, the antioxidant activity, and the angiotensin-I converting enzyme (ACE) inhibition in soybean following nine rounds of steaming and drying. Soybean was steamed 9 times for 2 h and then dried 9 times from 55℃ to 73℃ for 3 h. The total polyphenol content in the soybean reached a maximum value of 60.47 mg GAE eq./100 g at 73℃ while the total polyphenol content in the raw soybean reached 25.17 mg GAE eq./100 g. In the raw soybean samples, the DPPH radical scavenging activity (5 mg/mL) was 8.04% but it increased by 43.29% after drying 9 times to 73℃. ABTS radical scavenging activity also improved following 9 rounds of steaming and drying. ACE inhibitory activity of the soybean dried 9 times at 73℃ was 58.94% at 10 mg/mL. These results showed that steaming and drying soybean 9 times enhanced the antioxidant activity and the ACE inhibitory activity of soybean. Therefore, more research on the biological and anti-hypertensive activity of soybean using this steaming and drying method is necessary.

남해산 고사리의 이화학적 특성 및 항산화 활성 (Physicochemical Characteristics and Antioxidant Activity of Bracken (Pteridium aquilinum Kuhn) in Namhae)

  • 심혜진;황초롱;강재란;강민정;신정혜
    • 한국식품조리과학회지
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    • 제31권3호
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    • pp.288-295
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    • 2015
  • In this study, we investigate the physicochemical characteristics of dried bracken (Pteridium aquilinum Kuhn) harvested in Namhae. The moisture, ash, crude protein and crude lipid content was $10.79{\pm}0.31%$, $6.16{\pm}0.04%$, $33.20{\pm}0.40%$ and $2.45{\pm}0.27%$, respectively. The total mineral (Ca, Fe, K, Mg, Na, Mn) content was $36720.1{\pm}495.7mg/kg$, with K being the highest at $31890.0{\pm}503.8mg/kg$. The total free amino acid content was 704.41 mg/100 g, the amount of methionine, citrulline and sarcosine being higher than the others. The water and 50% ethanol extracts from the dried bracken were evaluated for the total poly phenolic compound content, antioxidant activity and xanthine oxidase and ${\alpha}$-glucosidase inhibitory activity. The total polyphenol content in the 50% ethanol extract ($1574.86{\pm}18.31mg/100g$) was higher than in the water extract ($1240.24{\pm}16.32mg/100g$). The DPPH and ABT radical scavenging activity was increased according to the concentration of bracken extract, and the activity in the 50% ethanol extract was higher than in the water extract. In addition, the xanthine oxidase and ${\alpha}$-glucosidase inhibitory activity was also higher in the 50% ethanol extract than in the water extract. In conclusion, bracken has great antioxidative and antidiabetic effects and can be used as a preventive agent for oxidation and diabetes.

만응환(萬應丸) 에탄올 추출물의 메티실린 내성 포도상구균에 대한 항균활성 및 내성억제 효과 (Antibacterial Activity and Inhibition of Resistance in Methicillin-resistant Staphylococcus aureus by Maneung-hwan Ethanol Extract)

  • 나용수;김종규;송용선
    • 한방재활의학과학회지
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    • 제30권1호
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    • pp.31-45
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    • 2020
  • Objectives In this study, we investigated the antimicrobial activity of a 70% ethanol extract of Maneung-hwan (MEH), which is prescribed by practitioners of oriental medicine for use against methicillin-resistant Staphylococcus aureus (MRSA). Methods The antibacterial activity of MEH against MRSA strains was evaluated using the disc diffusion method, broth microdilution method (minimal inhibitory concentration, MIC), checkerboard dilution test, and time-kill test. The mechanism of action of MEH was investigated by bacteriolysis using detergents or ATPase inhibitors Additionally, mRNA and protein expression were investigated by quantitative reverse transcription-polymerase chain reaction and western blot assay, respectively. Results The MIC of MEH was 25~1,600 ㎍/mL against all the tested bacterial strains. We showed that MEH extract exerts strong antibacterial activity. In the checkerboard dilution test, the fractional inhibitory concentration index of MEH in combination with antibiotics indicated synergism or partial synergism against S. aureus. The time-kill study indicated that the growth of the tested bacteria was considerably inhibited after a 24-h treatment with MEH and selected antibiotics. To measure the cell membrane permeability, MEH (3.9 ㎍/mL) was combined with Triton X-100 (TX) at various concentrations N,N-dicyclohexylcarbodimide (DCCD) was also tested as an ATPase inhibitor. TX and DCCD cooperation against S. aureus exhibited synergistic action. Accordingly, the antimicrobial activity of MEH in the context of cell membrane rupture and ATPase inhibition was assessed. Additionally, the expression of genes and proteins associated with resistance was reduced after exposing MRSA to MEH. Conclusions These results suggest that MEH possesses antibacterial activity and acts as a potential natural antibiotic against MRSA.

에센셜 오일이 항균 활성에 미치는 효과 (The Effect of Essential Oils on Antimicrobial Activity)

  • 박상남;강윤정
    • 융합정보논문지
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    • 제10권4호
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    • pp.104-114
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    • 2020
  • 본 연구는 식물에서 항생제로 알려진 11 가지 에센셜 오일(피톤치드)을 선별 한 후 혼합한 정유를 사용하여 최고의 항생제를 조사하였다. 최소억제농도 (MIC)와 최소사멸농도 (MBC) 측정 결과 Essential Oil B와 E가 목적 균의 억제효과가 높았다. 이 실험에 사용 된 S. aureus를 함유하는 모든 그람 양성 박테리아는 높은 항생제 활성을 나타냈다. 그리고 그람 양성 박테리아에서 A. baumanii와 곰팡이에서 C. albicans만이 높은 항생제 활동을 보였다. 우리의 실험에 사용 된 에센셜 오일은 항생제 활성이 뛰어난 천연 항생제 및 자연 의학의 에센셜 오일을 사용한 주요 연구와 비교할 때 더 우수한 항생제 활성을 보였다. 시험에 사용한 공시물질인 Essential Oil이 어떤 항균활성의 기전을 가지는지 알 수 없으나 다른 선행 연구결과와 비교해 볼 때 세포벽의 합성저해기전으로 해석하고 있다. 이러한 결과로부터, 항생제 활성을 갖는 일부 물질 또는 기능성 제품이 개발 될 것으로 예상된다.

HSV-1 ICP27 represses NF-κB activity by regulating Daxx sumoylation

  • Kim, Ji Ae;Choi, Mi Sun;Min, Jung Sun;Kang, Inho;Oh, Jeongho;Kim, Jin Chul;Ahn, Jeong Keun
    • BMB Reports
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    • 제50권5호
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    • pp.275-280
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    • 2017
  • Herpes simplex virus type 1 ICP27 is a multifunctional protein responsible for viral replication, late gene expression, and reactivation from latency. ICP27 interacts with various cellular proteins, including Daxx. However, the role of interaction between ICP27 and Daxx is largely unknown. Since Daxx is known to repress $NF-{\kappa}B$ activity, there is a possibility that ICP27 may influence the inhibitory effect of Daxx on $NF-{\kappa}B$ activity. In this study, we tested whether ICP27 affects the $NF-{\kappa}B$ activity through its interaction with Daxx. Interestingly, ICP27 enhanced the Daxx-mediated repression of $NF-{\kappa}B$ activity. In addition, we found that sumoylation of Daxx regulates its interaction with p65. ICP27 binds to Daxx, inhibits Daxx sumoylation, and enhances p65 deacetylation induced by Daxx. Consequently, ICP27 represses the $NF-{\kappa}B$ activity, by elevating the inhibitory effect of Daxx on $NF-{\kappa}B$ activity through desumoylation of Daxx.

비타민나무 잎으로부터 항산화활성 관련 Flavonol Glycoside 분리 (Isolation of Flavonol Glycoside Related to Antioxidant Activity from Hippophae rhamnoides Leaves)

  • 이지원;박주희;김주성;최은영;한상노;성은수;유창연;권용수;김명조
    • 한국약용작물학회지
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    • 제19권4호
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    • pp.251-256
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    • 2011
  • The leaves of Hippophae rhamnoides were extracted with methanol and then further fractioned with hexane, ethyl acetate, butanol and water in order to investigate biological activity. Two flavonol glycosides were isolated and identified from ethyl acetate soluble fraction, which showed the strongest antioxidant activity ($RC_{50}$ = 4.33 ${\mu}g/ml$). Isolated two compounds have shown strong free radical scavenging activity. Especially, quercetin 3-O-glucoside ($RC_{50}$ = 2.60 ${\mu}g/ml$) was more active than ${\alpha}$-tocopherol ($RC_{50}$ = 4.67 ${\mu}g/ml$). Total phenol and flavonoid contents were the highest to 4.17 and 1.14 mg/ml in the ethyl acetate soluble fraction. In addition, ethyl acetate soluble fraction was shown to the strongest ${\alpha}$-glucosidase inhibitory activity ($IC_{50}$ = 137.88 ${\mu}g/ml$) among the fractions. The results suggest that leaves of H. rhamnoides could be a potential source of natural antioxidant.

대사증후군 개선을 위한 뽕잎, 오디, 누에 분말의 혼합 비율 최적화 (Optimization of Mixing Ratio of Mulberry Leaf, Mulberry Fruit, and Silkworm for Amelioration of Metabolic Syndrome)

  • 김민주;김현숙;김애정
    • 한방비만학회지
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    • 제18권2호
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    • pp.83-95
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    • 2018
  • Objectives: The aim of this study was optimized mixing ratio of mulberry leaf, mulberry fruit, and silkworm for amelioration of the metabolic syndrome by using response surface method (RSM). Methods: Antioxidant, antidiabetic and antihypertensive activities of fifteen mixed powder of mulberry leaf, mulberry fruit, and silkworm by RSM were measured as indicators of metabolic syndrome. Results: The optimal mixing ratio of mulberry leaves, mulberry fruits, and silkworm with the greatest antioxidant, antidiabetic and antihypertensive activities was as follows: 2.5890 of mulberry leaf (A), 0.1222 of mulberry fruit (B), 2.9999 of silkworm (C). At this time, it was predicted that the total polyphenol content was estimated to be 185.51 tannic acid equivalent mg/g, 1, 1-diphenyl-2-picrylhy drazyl radical scavenging activity 84.77%, 1-deoxynojirimycin content 415.66 mg/100 g, ${\alpha}-glucosidase$ inhibitory activity 64.31%, ${\gamma}-aminobutyric$ acid content 267.77 mg/100 g, potassium content 1,899.11 mg/100 g, and angiotensin-converting-enzyme inhibitory activity was estimated to be 73.78%. Conclusions: It was concluded that the significant effect of the mulberry leaf, mulberry fruit, and silkworm on the metabolic syndrome-related biological activity indices (antioxidant activity, antidiabetic activity and antihypertensive activity) was as follows: 2.5890 of mulberry leaf (A), 0.1222 of mulberry fruit (B), 2.9999 of silkworm (C).

Root-Knot Nematode (Meloidogyne incognita) Control Using a Combination of Lactiplantibacillus plantarum WiKim0090 and Copper Sulfate

  • Kim, Seulbi;Kim, Ho Myeong;Seo, Hye Jeong;Yeon, Jehyeong;Park, Ae Ran;Yu, Nan Hee;Jeong, Seul-Gi;Chang, Ji Yoon;Kim, Jin-Cheol;Park, Hae Woong
    • Journal of Microbiology and Biotechnology
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    • 제32권8호
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    • pp.960-966
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    • 2022
  • Lactic acid bacteria (LAB) exert antagonistic activity against root-knot nematodes, mainly by producing organic acids via carbohydrate fermentation. However, they have not yet been used for root-knot nematode (Meloidogyne incognita) control owing to a lack of economic feasibility and effectiveness. In this study, we aimed to isolate organic acid-producing LAB from kimchi (Korean traditional fermented cabbage) and evaluated their nematicidal activity. Among the 234 strains isolated, those showing the highest nematicidal activity were selected and identified as Lactiplantibacillus plantarum WiKim0090. Nematicidal activity and egg hatch inhibitory activity of WiKim0090 culture filtrate were dose dependent. Nematode mortality 3 days after treatment with 2.5% of the culture filtrate was 100%, with a 50% lethal concentration of 1.41%. In pot tests, the inhibitory activity of an L. plantarum WiKim0090-copper sulfate mixture on gall formation increased. Compared to abamectin application, which is a commercial nematicide, a higher control value was observed using the WiKim0090-copper sulfate mixture, indicating that this combination can be effective in controlling the root-knot nematode.