• Title/Summary/Keyword: blocking effect

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The effect of flavonoids on the TREK-1 channel (TREK-1 채널에 대한 플라보노이드의 효과)

  • Kim, Yang-Mi;Kim, Kyung-Ah
    • Journal of the Korea Academia-Industrial cooperation Society
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    • v.12 no.6
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    • pp.2660-2667
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    • 2011
  • TREK-1 channel is a member of the two-pore domain potassium (K2P) channel family that is regulated by intracellular pH, membrane stretch, polyunsaturated fatty acids, temperature, and some neuroprotectant agents. TREK-1 channel can influence neuronal excitability by regulating leakage of potassium ions and resting membrane potential. TREK-1 channel has been shown to be overexpressed in prostate cancer cells. Although the importance of these properties, relatively little is known about flavonoid effects in the regulations of TREK-1 channel. The purpose of the study was to screening of flavonoids as the TREK-1 channel modulator using one of electrophysiological techniques such as excised inside-out patch configuration. We demonstrated blocking effect on TREK-1 channel by flavonoids such as epigallocatechin-3-gallate (EGCG), curcumin and quercetin in CHO cells transiently expressing TREK-1 channel. The inhibition of TREK-1 channel by quercetin and curcumin was reversible, whereas EGCG was little reversible. Quercetin, EGCG and curcumin decreased the relative channel activity to 73%, 91% and 94%, respectively. The half-inhibitory concentration (IC50) of curcumin, quercetin and EGCG was $1.04{\pm}0.19\;{\mu}M$, $1.13{\pm}0.26\;{\mu}M$ and $13.5{\pm}2.20\;{\mu}M$ in CHO cells expressing TREK-1 channel, respectively. These results indicate that flavonoids might regulate TREK-1 and this regulation might be one of the pharmacological actions of flavonoid in nervous systems and cancer cells.

A evaluation study of a fire smoke diffusion delay device installed in a great depth underground double deck tunnel (대심도 복층터널에 설치 가능한 화재연기 확산지연장치 성능 평가 연구)

  • Shin, Tae-Gyun;Moon, Jung-Joo;Yang, Yong-Won;Lee, Yun-Taek
    • Journal of Korean Tunnelling and Underground Space Association
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    • v.20 no.1
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    • pp.225-234
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    • 2018
  • Domestic urban areas are experiencing serious traffic congestion problems due to continuous population growth and increased traffic volume. In order to solve the problem of traffic congestion, the study of great depth underground double deck tunnels using underground space is being actively carried out in the urban areas. The characteristics of great depth underground double deck tunnels are low in cross section, so the spread of fire smoke is expected to spread faster than the road tunnel in case of fire. Therefore, it is necessary to provide a fire smoke delay device which delays the spread of fire smoke when a fire occurs in a tunnels. In the previous study, the diffusion effect was analyzed according to the blocking area when the fire smoke spread delay device was operated through the 3D CFD in the study of preventing the smoke spread in the case of the tunnel fire. A study on fire smoke diffusion delay device using spring elasticity which is excellent in applicability to a tunnel and economical value is studied. In this study, fire smoke spread delay system was developed to fire smoke delay was experimentally analyzed. Fire smoke delay effect of fire smoke delay device appeared. Therefore, it is considered that the can minimize the damage of the victims when installed in the great depth underground double deck tunnels.

Actions of a Gonadotropin-Releasing Hormone Antagonist on Gonadotropin II and Androgenic Steroid Hormone Secretion in Precocious Male Rainbow Trout

  • Kim Dae-Jung;Han Chang-Hee;Aida Katsumi
    • Fisheries and Aquatic Sciences
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    • v.3 no.1
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    • pp.37-43
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    • 2000
  • We used a mammalian GnRH antagonist, $[Ac-3,4-dehydro-Pro^1,\;D-p-F-Phe^2,\;D-Trp^{3.6}]$-GnRH, to examine the details of the salmon type gonadotropin-releasing hormone (sGnRH) and GnRH agonist analog $(Des-Gly^{10}$[d-Ala^6]-ethylamide GnRH; GnRHa) functions in the control of maturational gonadotropin (GTH II) secretion, in precocious male rainbow trout, in both in vivo and in vitro experiments. In the in vivo study, plasma GTH II levels increased by sGnRH or GnRHa treatment, but the response was more rapid and stronger in the GnRHa treatment group. The increase in GTH II was significantly suppressed by the GnRH antagonist, while the antagonist had no effect on basal GTH II levels in both groups. The GnRH antagonist showed stronger suppression of GTH II levels in the sGnRH treatment fish than in the GnRHa treatment fish. In addition, plasma androgenic steroid hormones (testosterone and 11-ketotestosterone) increased by the sGnRH or GnRHa treatment. The GnRH antagonist significantly inhibited the increases in plasma androgenic steroid hormone levels stimulated by the sGnRH or GnRHa, while the antagonist had no effect on basal androgenic steroid hormone levels in both groups. In the in vitro study, treatment with sGnRH or GnRHa increased GTH II release from the cultured dispersed pituitary cells, but the response was stronger in the GnRHa treatment group. The increase in GTH II release by GnRH was suppressed by adding the GnRH antagonist, dose­dependently. On the other hand, basal release of GTH II did not decrease by the GnRH antagonist treatment in both groups. These results suggest that the GnRH antagonist, $[Ac-3,4-dehydro-Pro^1,\;D-p-F-Phe^2,\;D-Trp^{3.6}]-GnRH$, used in this study is effective in blocking the action of GnRH-induced GTH II release from the pituitary gland both in vivo and in vitro.

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Anti-Obesity Effect of Ethyl Acetate Extracts from Agrimonia pilosa Ledeb. in 3T3-L1 Preadipocytes (3T3-L1 지방전구세포에서 용아초 에틸아세테이트 추출물의 항비만 효과)

  • Lee, Jung-A;Ahn, Eun-Kyung;Hong, Seong-Su;Oh, Joa-Sub
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.41 no.2
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    • pp.161-167
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    • 2012
  • To evaluate the anti-obesity effect of Agrimonia pilosa L., this study investigated that ethyl acetate extract from A. pilosa L. (EAAP) suppresses lipid accumulation and inhibits expression of adipogenic marker genes, such as peroxisome proliferator activated receptor ${\gamma}$ (PPAR${\gamma}$), CCAAT-enhancer-binding protein ${\alpha}$ (C/EBP${\alpha}$), glucose transporter 4 (GLUT4), and adiponectin in 3T3-L1 preadipocytes. We demonstrated that EAAP inhibited adipocyte differentiation and expression of PPAR${\gamma}$ and C/EBP${\alpha}$ mRNA levels in a dose-dependent manner. In addition, EAAP reduced the PPAR${\gamma}$ transcriptional activity stimulated by rosiglitazone in HEK 293T cells and decreased the expression of GLUT4 and adiponectin in 3T3-L1 cells. These results suggest that EAAP inhibits preadipocyte differentiation and adipogenesis by blocking of PPAR${\gamma}$ and C/EBP${\alpha}$ gene expression in 3T3-L1 cells.

Effect of basic fibroblast growth factor on osteopontin gene expression (Basic fibroblast growth factor가 osteopontin 유전자 발현에 미치는 영향)

  • Bae, Won-Su;Kim, Hyun-Jung;Ryoo, Hyun-Mo;Kim, Young-Jin;Nam, Soon-Hyeun
    • Journal of the korean academy of Pediatric Dentistry
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    • v.27 no.2
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    • pp.300-308
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    • 2000
  • The Fibroblast growth factors(FGFs) plays an important role in the control of osteogenesis during skeletal development. Especially, FGF-2 is a potent mesodermal inducer during embryogenesis and FGF receptors (FGFRs) messages are strongly expressed in developing bones. In this study, we investigated the effect of bFGF on osteopontin(OPN) gene expression in ST-2 cells and tried to elucidate the mechanism of its stimulatory effects. The obtain results were as follows; The treatment of bFGF(1ng/ml) upregulates OPN, fibronectin mRNA levels and downregulates type I collagen mRNA levels. But, there was no remarkable difference in alkaline phosphatase mRNA levels between two groups. The OPN gene expression increased in a dose-dependent manner up to 10ng/ml and OPN gene began to occur at around 3h with continuous increase up to 24h then decreased to basal level at 48h. 30 minutues pretreatment with cycloheximide (500ng/ml), a protein synthesis inhibitor, prior to addition bFGF resulted in blocking bFGF induced OPN expression. These results suggest that bFGF increased the level of OPN mRNA in a dose and time-dependent manner via the synthesis of certain transcriptional regulatory proteins.

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Cudrania Tricuspidata root extract (CTE) has an anti-platelet effect via cGMP-dependent VASP phosphorylation in human platelets (꾸지뽕나무 뿌리 추출물의 cGMP에 의한 VASP 인산화 기전을 통한 항혈소판 효과)

  • Ro, Ju-Ye;Cho, Hyun-Jeong
    • Journal of the Korea Academia-Industrial cooperation Society
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    • v.20 no.12
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    • pp.298-305
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    • 2019
  • Cudrania tricuspidata has been reported to have many biological activities, including anti-inflammatory, anti-cancer, and antioxidant properties. However, the effects of C. tricuspidata root extract (CTE) on human platelet aggregation induced by collagen as well as the signaling pathways involved remain unknown. In the present study, we investigated the effect of CTE on human platelets. CTE inhibited platelet aggregation via down-regulation of thromboxane A2 (TXA2) by blocking cyclooxygenase-1 (COX-1) activity and intracellular Ca2+ mobilization in collagen-induced platelets. CTE also reduced the phosphorylation of phospholipase C (PLC) γ2 and syk. CTE regulated platelet aggregation via cyclic guanosine monophosphate (cGMP)-dependent phosphorylation of vasodilator-stimulated phosphoprotein (VASP) Ser239. In addition, administration of CTE (50 and 100 mg/kg) significantly reduced hyper-aggregated platelet aggregation by collagen (5 ㎍/mL) without hepatotoxicity in HFD (high fat diet)-fed rats. Taken together, these results suggest that CTE has anti-platelet effects both in vitro and in vivo. Therefore, CTE may be an effective therapeutic and preventive agent for cardiovascular disease, and is a safe and natural product.

Protective Effects of Vitamin C against Genomic DNA Damage Caused by Genotoxicants (유전독성물질의 유전체 손상 작용에 대한 Vitamin C의 방호효과)

  • Yu, Gyeong Jin;Lee, Chun Bok
    • Journal of Life Science
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    • v.23 no.8
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    • pp.963-969
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    • 2013
  • Although it is popularly believed that vitamin C protects cells from various genotoxicants, the degrees and mechanisms of itsprotective actions are not fully understood. In this study, vitamin C's protective effects against various genotoxicants were quantified, together with subsequent analyses on the mechanisms of these protective effects. Comet assay was employed to measure the degree of DNA damage in Chinese hamster ovary cells (CHO-K1) exposed to five genotoxicants, $H_2O_2$, $HgCl_2$, N-methyl-N-nitro-N-nitrosoguanidine (MNNG), 4-nitroquinoline-1-oxide (4NQO), and UV-irradiation. In cases cells were treated with $H_2O_2$, $HgCl_2$, and 4NQO together with vitamin C, the damage to DNA decreased to the level of the control group. In cases of UV-irradiation, the protective effect of vitamin C appeared, but did not reach the control levels. Interestingly, vitamin C did not have protective effects against the genotoxicity of MNNG. The degrees of DNA damage of cells treated with vitamin C prior to exposure togenotoxicants were 28~49% lower than those of cells treated with vitamin C after being exposed to genotoxicants. In conclusion, vitamin C had strong antioxidanteffects against genotoxicants by being a primary antioxidant blocking genotoxicity reaching the cells, rather than being a secondary antioxidant acting on post-exposure DNA repair processes. However, vitamin C's protective effects appearto be limited, as there are genotoxicants, such as MNNG, whosegenotoxicityis not affected by vitamin C. Therefore, the results of this study warrant furtherstudies on toxic mechanisms of genotoxicants and their interactions with protective mechanisms of vitamin C.

Inhibitory Effects of Type IV Collagenase by Disulfiram (Disulfiram에 의한 type IV collagenase 저해효과)

  • Sin, Doo-Il;Park, Jae-Bok;Park, Kwan-Kyu;Cho, Chang-Ho;Oh, Hoon-Kyu;Choi, Chang-Hyuk;Cho, Hyun-Ji;Chang, Young-Chae
    • Journal of Life Science
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    • v.16 no.6
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    • pp.964-971
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    • 2006
  • The cancer cells, characterized by local invasion and distant metastasis, are very dependant on extracellular matrix. The expression of matrix metalloproteinases (MMPs) has been implicated in the invasion and metastasis of cancer cells. Among the human MMPs, matirx metalloproteinase-2 (MMP-2) and matrix metalloproteinse-9 (MMP-9) are key enzymes that degrade type IV collagen of the matrix. Here, we studied the effect of disulfiram, an anti-tumor compound, on the suppression of the tumor invasion and the activity of MMP-2, MMP-9 in human osteosarcoma cells (U2OS). Disulfiram had the type IV collagenase inhibitory activity, the effect of inhibition of gene and protein expression, and these inhibitions were responsible for blocking invasion through cell mediated and non-cell mediated pathways. In conclusion, disulfiram inhibited expression of MMP-2 and MMP-9, and regulated the invasion of U2OS, Caki-1 and Caski. These observations raise the possibility of clinical therapeutic applications for disulfiram used as a potential inhibitor of cancer invasion.

Stability and Sun Protection Efficacy of Sunscreens Based on the Solubility and a Combination of Organic UV Absorbers (유기 자외선 흡수제의 조합과 용해도에 따른 자외선 차단 효율의 비교 및 안정성에 관한 연구)

  • Yeon, Jae Young;Hong, Seung Deok;Choi, Se Bum;Kim, Ta Gon;Lee, Cheong Hee;Lee, Sang Gil;Pyo, Hyeong Bae
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.41 no.3
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    • pp.189-199
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    • 2015
  • In this study, we have investigated the stability of sunscreens based on the solubility of organic UV absorbers in the oil and sun protection efficacy of the products composed of a combination of organic UV absorbers to develop more stable and efficient sunscreen products. Results showed that the solubility of the organic UV absorber and stability were varied depending on the type, storage conditions and concentration of oil. It was also observed from the products in the emulsion type. Various UV absorbances were determined to the products composed of the combination of organic UV absorbers. In some combinations, a synergistic effect was observed to make an increase in absorbance compared to a single component. In other cases, specific synergistic effect was displayed only when combined with the particular component. In addition, the storage condition also affected the sunscreen efficacy. In conclusion, this study confirmed that there are various factors which could affect the UV-blocking efficiency of sunscreen products.

Anti-Inflammatory Effect of Biji (Soybean curd residue) on LPS-Stimulated RAW264.7 Cells (마우스 RAW264.7 세포에 대한 비지 추출물의 항염증 활성)

  • Park, Su Bin;Song, Hun Min;Kim, Ha Na;Park, Gwang Hun;Son, Ho-Jun;Um, Yurry;Park, Ji Ae;Jeong, Jin Boo
    • Korean Journal of Plant Resources
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    • v.31 no.2
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    • pp.117-123
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    • 2018
  • In this study, we evaluated anti-inflammatory effect of biji in LPS-stimulated RAW264.7 cells. Biji inhibited the generation of NO and $PGE_2$ through the suppression of iNOS and COX-2 expression. In addition, biji attenuated the expression of TNF-${\alpha}$ and IL-$1{\beta}$ induced by LPS. Biji blocked LPS-mediated $I{\kappa}B-{\alpha}$ degradation and subsequently inhibited p65 nucleus accumulation in RAW264.7 cells, which indicates that biji inhibits NF-${\kappa}B$ signaling. In addition, biji suppressed p38 phosphorylation induced by LPS. Our results suggests that biji may exert anti-inflammatory activity through blocking the generation of the inflammatory mediators such as NO, $PGE_2$, iNOS, COX-2, TNF-${\alpha}$ and IL-$1{\beta}$ via the inhibiting the activation of NF-${\kappa}B$ and p38. From these findings, biji has potential to be a candidate for the development of chemoprevention or therapeutic agents for inflammatory diseases.