• 제목/요약/키워드: inhibitory mechanism

검색결과 1,033건 처리시간 0.029초

Korean Red Ginseng Extract Activates Non-NMDA Glutamate and GABAA Receptors on the Substantia Gelatinosa Neurons of the Trigeminal Subnucleus Caudalis in Mice

  • Yin, Hua;Park, Seon-Ah;Park, Soo-Joung;Han, Seong-Kyu
    • Journal of Ginseng Research
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    • 제35권2호
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    • pp.219-225
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    • 2011
  • Korean red ginseng (KRG) is a valuable and important traditional medicine in East Asian countries and is currently used extensively for botanical products in the world. KRG has both stimulatory and inhibitory effects on the central nervous system (CNS) suggesting its complicated action mechanisms. The substantia gelatinosa (SG) neurons of the trigeminal subnucleus caudalis (Vc) are involved in orofacial nociceptive processing. Some studies reported that KRG has antinociceptive effects, but there are few reports of the functional studies of KRG on the SG neurons of the Vc. In this study, a whole cell patch clamp study was performed to examine the action mechanism of a KRG extract on the SG neurons of the Vc from juvenile mice. KRG induced short-lived and repeatable inward currents on all the SG neurons tested in the high chloride pipette solution. The KRG-induced inward currents were concentration dependent and were maintained in the presence of tetrodotoxin, a voltage gated $Na^+$ channel blocker. The KRG-induced inward currents were suppressed by 6-cyano-7-nitroquinoxaline-2,3-dione, a non-N-methyl-D-aspartate (NMDA) glutamate receptor antagonist and/or picrotoxin, a gamma-aminobutyric acid $(GABA)_A$ receptor antagonist. However, the inward currents were not suppressed by d,l-2-amino-5-phosphonopentanoic acid, an NMDA receptor antagonist. These results show that KRG has excitatory effects on the SG neurons of the Vc via the activation of non-NMDA glutamate receptor as well as an inhibitory effect by activation of the $GABA_A$ receptor, indicating the KRG has both stimulatory and inhibitory effects on the CNS. In addition, KRG may be a potential target for modulating orofacial pain processing.

TNF-$\alpha$ 자극에 의한 U937 단핵구 세포의 HT29 대장 상피 세포 부착에 대한 Berberine의 PPAR$\gamma$가 아닌 NF-$\kappa$B 경로를 통한 억제 효과 (Inhibitory Effect of Berberine on TNF-$\alpha$-induced U937 Monocytic Cell Adhesion to HT29 Human Colon Epithelial Cells is Mediated through NF-$\kappa$B Rather than PPAR$\gamma$)

  • 박수영;이광익;김일엽;김정애
    • 약학회지
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    • 제54권2호
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    • pp.91-96
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    • 2010
  • Berberine, an isoquinoline alkaloid, has a wide range of pharmacological effects, including anti-inflammation. It has been reported that berberine inhibits experimental colitis through inhibition of IL-8, and that inhibitory effect of berberine on inflammatory cytokine expression is mediated through peroxisome proliferator activated receptor (PPAR)-$\gamma$. In this study, we examined the effects and action mechanism of berberine on the tumor necrosis factor (TNF)-$\alpha$-induced monocyte adhesion to HT29 human colonic epithelial cells, which is commonly used as an in vitro model of inflammatory bowel disease (IBD). Berberine significantly inhibited the TNF-$\alpha$-induced monocyte adhesion to HT29, which is similar to the effect of PDTC, a nuclear factor (NF)-$\kappa$B inhibitor. However, ciglitazone and GW, the ligands of PPAR-$\gamma$, did not suppress the TNF-$\alpha$-induced monocyte adhesion to HT29 cells. In addition, TNF-$\alpha$-induced chemokine expression and NF-$\kappa$B transcriptional activity were significantly inhibited by berberine in a concentration-dependent manner. The results suggest that inhibitory effect of berberine on colitis is mediated through suppression of NF-$\kappa$B and NF-$\kappa$B-dependent chemokine expression.

Adenosine Agonist-induced Changes in the Transmission of Sensory Signals in the Cat Spinal Cord

  • Kim, Kee-Soon;Shin, Hong-Kee;Kim, Jin-Hyuk
    • The Korean Journal of Physiology
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    • 제30권1호
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    • pp.85-96
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    • 1996
  • Adenosine and its analogues are known to possess analgesic effects and to be involved in the opiate-induced antinociception as well. This study was designed to investigate the effects of three adenosine agonists, 5'- (N-cyclopropyl) -carboxamidoadenosine(CPCA), 5'-N-ethylcarboxamidoadeno-sine (NECA) and $N^6-cyclohexyladenosine$ (CHA) on the signal transmission in the spinal cord and also to elucidate mechanisms of their actions in the anesthetized cat. All the tested adenosine agonists(i.v,) exerted inhibitory effects on the responsiveness of the wide dynamic range (WDR) cells, the inhibitory action of CHA, an adenosine $A_1$ receptor agonist, $(80{\mu}g/Kg)$ being most weak. The intravenous CPCA, an adenosine $A_2$ receptor agonist, $(20{\mu}g\;/Kg)$ and NECA, nonspecific adenosine receptor agonist, $(20{\mu}g\;/Kg)$ inhibited the responses of WDR cells to pinch and C fiber stimulation more strongly than those to brush and A fiber stimulation. CPCA (i.v.) also suppressed the responses of WDR cells to thermal stimulus. And all the CPCA-induced inhibitions were caffeine-reversible. When CPCA was directly applied onto the spinal cord or intravenously administered into the spinal cat, on average, about three quarters of the CPCA-induced inhibitory effect was abolished. On the other hand, in the animal with spinal lesions in the ipsilateral dorsolateral area, the CPCA-induced inhibition was comparable to that observed in the spinal cats. In conclusion, this study shows that adenosine agonists strongly suppress the responses of WDR cells to pinch, C fiber stimulation and thermal stimuli mainly through the supraspinal adenosine $A_2-receptors$.

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죽여의 멜라닌 생성 억제 효과 및 관련 단백질 동향 분석 (Inhibitory Melanogenesis of Bambusae caulis in Taeniam and Profiling of Related Proteins)

  • 이정현;김상범;변상요
    • KSBB Journal
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    • 제25권5호
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    • pp.478-482
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    • 2010
  • 죽여 추출물의 미백 효과를 확인하기 위하여 용매와 추출방법을 달리한 6가지의 추출물을 얻어 tyrosinase 활성 억제시험을 하였다. 그 결과 메탄올로 추출한 죽여 추출물에서 tyrosinase 활성 억제 효과가 가장 우수한 것을 확인 하였다. 세포 수준에서 죽여 추출물의 melanin 생성 억제 효과를 알아보기 위해서 B16 melanoma 세포를 이용하여 MTT assay를 실시하였고, 50 ppm의 농도 까지는 세포 독성이 나타나지 않은 것을 확인하였다. 죽여 추출물에 의한 세포 내 melanin 합성 저해 효과를 측정하기 위해 melanin contents assay를 하였고, 10 ppm 추출물을 처리한 extra cellular에서는 control 대비 68%, intra cellular에서는 74% 수준으로 melanin 합성이 저해됨을 확인하였다. 이차원전기영동을 이용하여 B16 melanoma 세포의 proteome을 분석 해 본 결과, 죽여 추출물 을 투여하지 않은 대조군에서는 171개, 추출물을 투여한 것에서는 282개의 spot을 확인하였고, 120개의 spot matching 을 확인하였다. 이 중 미백에 관련된 12개의 단백질 동향분석을 통하여, 죽여 추출물이 melanin 합성 전이나 합성 중에 관련된 메커니즘에 관련하는 것을 알 수 있었다.

Antifungal Activity of Lactic Acid Bacteria Strains Isolated from Natural Honey against Pathogenic Candida Species

  • Bulgasem, Bulgasem Y.;Lani, Mohd Nizam;Hassan, Zaiton;Yusoff, Wan Mohtar Wan;Fnaish, Sumaya G.
    • Mycobiology
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    • 제44권4호
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    • pp.302-309
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    • 2016
  • The role of lactic acid bacteria (LAB) in honey as antifungal activity has received little attention and their mechanism of inhibitory of fungi is not fully understood. In this study, LAB were isolated from honey samples from Malaysia, Libya, Saudi Arabia, and Yemen. Twenty-five isolates were confirmed LAB by catalase test and Gram staining, and were screened for antifungal activity. Four LAB showed inhibitory activity against Candida spp. using the dual agar overlay method. And they were identified as Lactobacillus plantarum HS isolated from Al-Seder honey, Lactobacillus curvatus HH isolated from Al-Hanon honey, Pediococcus acidilactici HC isolated from Tualang honey and Pediococcus pentosaceus HM isolated from Al-Maray honey by the 16S rDNA sequence. The growth of Candida glabrata ATCC 2001 was strongly inhibited (>15.0 mm) and (10~15 mm) by the isolates of L. curvatus HH and P. pentosaceus HM, respectively. The antifungal activity of the crude supernatant (cell free supernatant, CFS) was evaluated using well diffusion method. The CFS showed high antifungal activity against Candida spp. especially The CFS of L. curvatus HH was significantly (p < 0.05) inhibited growth of C. glabrata ATCC 2001, C. parapsilosis ATCC 2201, and C. tropicalis ATCC 750 with inhibitory zone 22.0, 15.6, and 14.7 mm, respectively. While CFS of P. pentosaceus HM was significantly (p < 0.05) effective against C. krusei, C. glabrata, and C. albicans with inhibition zone 17.2, 16.0, and 13.3 mm, respectively. The results indicated that LAB isolated from honey produced compounds which can be used to inhibit the growth of the pathogenic Candida species.

계혈등(鷄血藤)의 Beta-sitosterol 성분이 자궁근종세포의 증식억제와 세포자멸사의 유도에 미치는 영향 (The effect of β-sitosterol proliferation and apoptosis in human uterine leiomyoma cells)

  • 박영선;백승희
    • 대한한방부인과학회지
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    • 제18권1호
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    • pp.181-191
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    • 2005
  • Purpose : ${\beta}$-sitosterol is kind of phytosterols or plant which are structurally similar to cholesterol. This study was aimed to investigate the inhibitory effect of the ${\beta}$-sitosterol on the proliferation of human uterine leiomyoma cells and the expression of gene related the mechanism of cell apoptosis. Methods : We counted the number of death cells treated with indicated time of the ${\beta}$-sitosterol and investigated cell death rate by cell count assay. Furthermore, flow cytometry analysis and DNA fragmentation assay were used to dissect between necrosis and apoptosis. and then we observed the differential gene expression by western blot analysis. Results : 1) The inhibitory effect on the growth of uterine leiomyoma cell treated with the ${\beta}$-sitosterol $16{\mu}M$ was increased in a time dependent. 2) The result of flow cytometry analysis, subG1 phase arrest related cell apoptosis was investigated 16.97% in uterine leiomyoma cell treated with the ${\beta}$-sitosterol $16{\mu}M$ and showed the fashion of proportional time dependent. 3) The gene expression of p27, p21 related cell cycle was increased according to increasing time interval but cyclin E-CDK2 complex was decreased expression. 4) The character of apoptosis, DNA fragmentation was significantly observed on the time dependent. 5) The expression of pro-caspase 3 and PARP were decreased dependent on treatment with time dependent. Conclusion : This study showed that the ${\beta}$-sitosterol have the inhibitory effect on the proliferation of human uterine leiomyoma cell and the effect was related with apoptosis.

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흰쥐의 간손상(肝損傷)에 대한 삼(蔘)기인진탕(茵蔯湯)의 간(肝) 보호효과(保護效果) (Protective Effects of Samgiinjin-tang on Liver Injury of Rats)

  • 강재춘;이유경
    • 대한한방내과학회지
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    • 제22권3호
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    • pp.309-320
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    • 2001
  • Objectives : This study was done to investigate the protective effects of Samgiinjin-tang on liver injury of rats induced by CCI4 and d-galactosamine. Methods: All animals were divided into .5 groups, those were normal group(untreated), control group(treated with 0.9% Saline solution), sample I group(2,250mg/kg administrated), sample II group(4,500mg/kg administrated), Silymarin 200mg/kg administrated group. Liver injury of rats were induced by CCI4 and d-galactosamine, and then the serum transaminases(ALT&AST) alkaline phosphatase(ALP), lactic dehydrogenase(LDH) for enzyme activities, liver weight, lipid peroxidation and catalase, glutathione S-transferase(GST) for enzyme activities were measured. Results : The inhibitory effects on the serum ALT, AST activities in liver injury of rats induced by CCI4 were noted in both sample I and sample II group. The inhibitory effects on the serum ALP, LDH activities and the Lipid peroxidation of Mitochondria & Cytosol were noted in only sample II group. The decreased effects on the GST activities of Homogenate & Cytosol were inhibited in both sample I and sample II groups. The decreased effects on the GST activities of Mitochondria & Microsome were inhibited in sample II group. The inhibitory effects of the serum ALT, AST, LDH activities in liver injury of rats induced by d-galactosamine were noted in both sample I and sample II groups. In serum AST activities, sample II group. Conclusions : Samgiinjin-tang has protective effects against liver injury of rats induced by CCI4 and d-galactosamine. So it is required to study about the actions of mutual relation of medicines and patho-mechanism by experiment.

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삼백초 에탄올 추출물의 위출혈성 스트레스 위염 억제 효과 (Inhibitory Activities of Ethanol Extracts from Saururus chinensis L. against Stress-Induced Hemorrhagic Gastritis)

  • 박소영;조영제
    • 한국식품영양과학회지
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    • 제44권6호
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    • pp.800-808
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    • 2015
  • 천연 생리활성 물질 탐색 연구의 일환으로 삼백초로부터 위염 억제 물질을 추출하여 효능을 검정하였다. 삼백초 추출물 0.25~2 g/kg B.W.를 마우스에 경구 투여한 결과 1.5 g/kg B.W. 미만 투여량의 급성독성 실험에서 안정성을 나타내었으며 $LD_{50}$은 1.81 g/kg B.W.였다. 삼백초 추출물 0.5 g/kg B.W.를 마우스에 경구 투여한 만성독성 실험에서는 13주간의 투여기간 동안 독성이 없는 것으로 나타났다. 위염을 유발시키기 전에 삼백초 추출물을 250 및 500 mg/kg B.W. 농도로 미리 섭취시킨 결과 위출혈 및 위부종과 세포손상이 농도 의존적으로 감소하였다. 또한 사이토카인의 발현도 억제되었다. 따라서 삼백초 추출물은 스트레스성 위염에 의한 출혈 및 세포손상을 농도 의존적으로 억제하는 효과가 있으며, 그 mechanism은 염증성 사이토카인의 발현 억제에 의한 것이라 생각되었다.

Effects of Omeprazole and Caffeine Alone and in Combination with Gentamicin and Ciprofloxacin Against Antibiotic Resistant Staphylococcus Aureus and Escherichia Coli Strains

  • Bazzaz, Bibi Sedigheh Fazly;Fakori, Mahmoud;Khameneh, Bahman;Hosseinzadeh, Hossein
    • 대한약침학회지
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    • 제22권1호
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    • pp.49-54
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    • 2019
  • Objective: Antibiotic resistance is a global health problem and threatens health of societies. These problems have led to a search for alternative approaches such as combination therapy. The aim of the present study was to investigate the effect of caffeine and omeprazole in combination with gentamicin or ciprofloxacin against standard and clinically resistant isolates of Staphylococcus aureus and Escherichia coli. Methods: The minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) values of different agents against bacterial strains were determined. The interaction of non- antibiotic drugs with gentamicin and ciprofloxacin was studied in vitro using a checkerboard method and calculating fraction inhibitory concentration index (FICI). Verapamil as efflux pump inhibitor was used to evaluate the possible mechanism of bacterial resistance to antibiotics. Results: The MIC and MBC values of gentamicin against bacterial strains were in the range of $20-80{\mu}g/ml$ and $40-200{\mu}g/ml$, respectively. Caffeine and omeprazole had no intrinsic inhibitory activity against tested microorganisms. However, upon combination of caffeine with antibiotics, the synergistic effects were observed. Verapamil was able to reduce the MIC values of gentamicin (4 folds) only in some bacterial strains. Conclusion: These findings indicated that caffeine was effective in removing bacterial infection caused by S. aureus and E. coli. The relevant mechanisms of antibiotic resistance were not related to the drug efflux.

Anemarrhena asphodeloides Extract Inhibits the Mycelial Growth of Magnaporthe oryzae and Controls the Rice Blast Disease

  • Joo, Myoung Ho;Yeo, Yu Mi;Choi, Pil Son;Lee, Jae Hyeok;Yang, Kwang-Yeol;Lee, Young Jin
    • 한국자원식물학회지
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    • 제31권6호
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    • pp.695-703
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    • 2018
  • Previously, we have reported a plant extract isolated from Lysimachia foenum gracum Herba as a new environment friendly biopesticide that has the mycelial growth inhibition effect on Magnaporthe oryzae, the pathogenic fungus of the rice blast disease. For the finding of additional biopesticide candidate, we tested the mycelial growth inhibitory effects about 700 species of plant extracts on PDA media. Among them, the extract of Anemarrhena asphodeloides showed prominent inhibitory effect of which $IC_{50}$ was $139.7{\mu}g/ml$. Mycelial radii of M. oryzae were measured on PDA medium containing the four organic solvent fractions isolated from total extract from A. asphodeloides. Ethyl acetate fraction showed the impressive inhibitory effect of $IC_{50}$, $54.12{\mu}g/ml$. In the subsequent rice field test for the total extract of A. asphodeloides, we obtained encouraging 62.0% control rate of rice blast disease without any phytotoxicity. It is almost equivalent to that of chemical pesticides implying the applicability of the extract as a new biopesticide. In further study, the analysis of active ingredients of the extract would be necessary for the development of a new biopesticide and for the verification of cellular mechanism by which the mycelial growth of M. oryzae inhibited.