• 제목/요약/키워드: blocking effect

검색결과 904건 처리시간 0.03초

Corni Fructus attenuates testosterone-induced benign prostatic hyperplasia by suppressing 5α-reductase and androgen receptor expression in rats

  • Hwangbo, Hyun;Kwon, Da He;Choi, Eun Ok;Kim, Min Yeong;Ahn, Kyu Im;Ji, Seon Yeong;Kim, Jong Sik;Kim, Kyung-Il;Park, No-Jin;Kim, Bum Hoi;Kim, Gi-Young;Hong, Su-Hyun;Park, Cheol;Jeong, Ji-Suk;Choi, Yung Hyun
    • Nutrition Research and Practice
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    • 제12권5호
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    • pp.378-386
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    • 2018
  • BACKGROUND/OBJECTIVES: Benign prostatic hypertrophy (BPH) is a major cause of abnormal overgrowth of the prostate mainly in the elderly. Corni Fructus has been reported to be effective in the prevention and treatment of various diseases because of its strong antioxidant effect, but its efficacy against BPH is not yet known. This study was designed to evaluate the therapeutic efficacy of Corni Fructus water extract (CF) in testosterone-induced BPH rats. MATERIALS/METHODS: To induce BPH, rats were intraperitoneal injected with testosterone propionate (TP). Rats in the treatment group were orally administered with CF with TP injection, and finasteride, which is a selective inhibitor of $5{\alpha}$-reductase type 2, was used as a positive control. RESULTS: Our results showed that the increased prostate weight and histopathological changes in BPH model rats were suppressed by CF treatment. CF, similar to the finasteride-treated group, decreased the levels of testosterone and dihydrotestosterone by TP treatment in the serum, and it also reduced $5{\alpha}$-reductase expression and concentration in prostate tissue and serum, respectively. In addition, CF significantly blocked the expression of the androgen receptor (AR), AR co-activators, and proliferating cell nuclear antigen in BPH rats, and this blocking was associated with a decrease in prostate-specific antigen levels in serum and prostate tissue. CONCLUSIONS: These results suggest that CF may weaken the BPH status through the inactivation of at least $5{\alpha}$-reductase and AR activity and may be useful for the clinical treatment of BPH.

Polyphenols of Rubus coreanum Inhibit Catecholamine Secretion from the Perfused Adrenal Medulla of SHRs

  • Yu, Byung-Sik;Na, Duck-Mi;Kang, Mi-Young;Lim, Dong-Yoon
    • The Korean Journal of Physiology and Pharmacology
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    • 제13권6호
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    • pp.517-526
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    • 2009
  • The present study was attempted to investigate whether polyphenolic compounds isolated from wine, which is brewed from Rubus coreanum Miquel (PCRC), may affect the release of catecholamines (CA) from the isolated perfused adrenal medulla of the spontaneously hypertensive rats (SHRs), and to establish its mechanism of action. PCRC $(20\sim180\;{\mu}g/ml)$ perfused into an adrenal vein for 90 min relatively dose-dependently inhibited the CA secretory responses to ACh (5.32 mM), high $K^+$ (56 mM), DMPP $(100\;{\mu}M)$ and McN-A-343 $(100\;{\mu}M)$. PCRC itself did not affect basal CA secretion (data not shown). Also, in the presence of PCRC $(60\;{\mu}g/ml)$, the CA secretory responses to veratridine (a selective $Na^+$ channel activator $(10\;{\mu}M)$, Bay-K-8644 (a L-type dihydropyridine $Ca^{2+}$ channel activator, $10\;{\mu}M$), and cyclopiazonic acid (a cytoplasmic $Ca^{2+}$-ATPase inhibitor, $10\;{\mu}M$) were significantly reduced, respectively. In the simultaneous presence of PCRC $(60\;{\mu}g/ml)$ and L-NAME (an inhibitor of NO synthase, $30\;{\mu}M$), the inhibitory responses of PCRC on the CA secretion evoked by ACh, high $K^+$, DMPP, and Bay-K-8644 were considerably recovered to the extent of the corresponding control secretion compared with that of PCRC-treatment alone. The level of NO released from adrenal medulla after the treatment of PCRC $(60\;{\mu}g/ml)$ was greatly elevated compared with the corresponding basal level. Taken together, these results demonstrate that PCRC inhibits the CA secretion from the isolated perfused adrenal medulla of the SHRs evoked by stimulation of cholinergic receptors as well as by direct membrane-depolarization. It seems that this inhibitory effect of PCRC is mediated by blocking the influx of calcium and sodium into the adrenal medullary chromaffin cells of the SHRs as well as by inhibition of $Ca^{2+}$ release from the cytoplasmic calcium store at least partly through the increased NO production due to the activation of NO synthase.

분체와 유화제의 상호 관계성에 기인한 저점도 W/O 및 W/S 에멀젼의 안정성 연구 (Synergistic Interaction in W/O and W/S Emulsions Stabilized by a Mixture of Powders and Surfactant)

  • 인소현;조환일;강내규;한종섭;박선규;이천구
    • 대한화장품학회지
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    • 제42권1호
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    • pp.15-28
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    • 2016
  • 유중 수형 에멀젼은 우수한 수분 증발 차단력 및 통기성 밀폐막 형성 등의 장점에도 불구하고 저점도 안정화가 쉽지 않아 다양한 화장품 제형 적용에 한계성을 지녀왔다. 본 연구에서는 유중 수형 에멀젼 형성에 있어 비이온성 유화제와 분체, 양이온성 유화제 간의 상호 관계가 제형의 안정성에 미치는 영향을 규명하였다. 비이온성 유화제와 분체 존재 하에 양이온 유화제의 농도가 증가함에 따라 초기에는 유화 안정성이 향상되다가 일정 농도 이상에서는 하락되고, 더욱 농도가 증가하면 전상이 일어나는 경향성이 관찰되었다. 이를 통해, 비이온성 유화제 1.0 ~ 4.0 wt% 사용 조건에서 실리콘 계 마이크로 사이즈 분체 2.5 wt%와 양이온 유화제 0.1 ~ 0.5 wt%를 사용할 경우 흐름성 있는 범위의 점도까지(2000 ~ 5000 cps) 낮추면서도 분체의 분산성과 안정성을 효과적으로 높인 유중 수형 에멀젼의 제조가 가능함을 확인하였다.

수직형 유동층로에서 제조된 인공경량 세골재의 특성 (Characteristics of artificial lightweight fine aggregates manufactured by using a vertical fluidizing furnace)

  • 강승구
    • 한국결정성장학회지
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    • 제19권1호
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    • pp.54-59
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    • 2009
  • 기존의 로타리 킬른으로는 융착 현상 때문에 3 mm 이하 크기의 세골재를 제조하기 어려웠다. 이를 해결할 수 있는 수직형 유동층로를 설계, 제작하고 이로부터 점토 : 석분슬러지 :폐백토 =60 : 30 : 10(wt%)조성의 성형체를 소성하여 비중 $1.1{\sim}1.7$, 흡수율 $11{\sim}19%$의 다양한 특성을 갖는 경량 세골재를 제조하였다. 골재를 발포시키기 위한 최소 소성온도는 $1130^{\circ}C$이었다. $1140^{\circ}C$ 이상으로 소성된 시편은 전형적인 발포 경량골재 특성을 보였으며, 표면에 균열이 크게 벌어져서 내부 층이 드러나 보였다. 그러나 표면에 발생된 균열은 black core 내부로 진행되지 않았기 때문에 흡수율에 영향을 주지 않았다. 소성온도가 증가하면 골재의 shell 두께는 감소하고 black core 영역은 넓어졌으나 유지시간은 미세구조에 따른 영향을 주지 않았다. 소성온도가 증가되면 표면에 액상 발생량이 증가하여 골재의 흡수율은 감소하였다. 또한 소성시간도 골재 흡수율에 큰 영향을 주었는데, 이는 액상을 형성하고 또 생성된 액상이 표면의 개기공을 막아 폐기공으로 변화시키는데 시간이 필요하기 때문인 것으로 생각된다.

DSRC 시스템에서 릴레이 프로토콜 (Relay Protocol in DSRC System)

  • 최광주;최경원;조경국;윤동원;박상규
    • 대한전자공학회논문지TC
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    • 제43권9호
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    • pp.32-39
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    • 2006
  • DSRC(Dedicated Short Range Communications : 근거리 전용 무선통신)는 차량의 고속 이동시에 차량과 기지국 사이 근거리 통신영역 내에서 무선으로 접속하여 텔레매틱스 서비스를 제공하고 교통정보 수집에 활용이 가능하다. 현재 DSRC는 5.8GHz의 주파수 대역을 사용하고 있으나 전파 자체의 직진성이 우수하기 때문에 앞에 장애물이나 다른 차량이 존재하는 경우 가시선 확보의 어려움이 발생하고 이로 인해 음영 현상과 통신 장애가 발생할 수 있다. 본 논문에서는 DSRC 문제점 중에 하나인 가시선 방해로 인한 음영현상을 해결하고 통신율을 높이기 위한 방안으로 현재 실제로 적용되고 있는 TTA의 DSRC 표준방식인 '5.8GHz 대역 노변기지국과 차량단말기 사이의 근거리전용 무선통신 표준'의 프로토콜을 알아보고, 릴레이 프로토콜(relay Protocol)의 통신 과정과 릴레이 프로토콜의 구조를 제안한다. 제안된 릴레이 프로토콜을 DSRC 시스템과 차량간 통신에 응용하여 고정 릴레이 프로토콜과 이동 릴레이 프로토콜을 고려한다. 릴레이 프로토콜은 추후에 DSRC를 이용한 차량간 통신으로까지 적용되어 차량 운전자간의 화상통화나 차량간의 안전거리 확보를 통한 사고 방지 등에 효과적으로 응용되리라 예상된다.

Influence of Cilnidipine on Catecholamine Release Evoked by Cholinergic Stimulation and Membrane Depolarization in the Perfused Rat Adrenal Gland

  • Lim, Dong-Yoon;Woo, Seong-Chang;Ko, Suk-Tai
    • 한국응용약물학회:학술대회논문집
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    • 한국응용약물학회 2001년도 추계학술대회 및 정기총회
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    • pp.95-95
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    • 2001
  • Ciinidipine (FRC-8635) is a newly synthesized novel DHP type of organic Ca$\_$2+/channel blockers that have been developed so far in Japan (Yoshimoto et al., 1991 : Hosono et at., 1992). It also has a blocking action on L-type voltage-dependent Ca$\^$2+/channel (VDCCs) in the rabbit basilar artery (Oike et al., 1990) and a slow-onset and long-lasting hypotensive action in clinical and experimental studies (Ikeda et al., 1992 ; Tominaga et al., 1997). Recent electrophysiological data indicate that cilnidipine might be a dual-channel antagonist for peripheral neuronal N-type and vascular L-type Ca$\^$2+/channels (Oike et al., 1990 ; Fujii et al., 1997; Uneyama et at., 1997). However, little is known about the involvement of N-type VDCCs in contributing to the muscarinic receptor-mediated CA secretion. Therefore, the present study was attempted to investigate the effect of cilinidipine on secretion of catecholamines (CA) evoked by ACh, high K$\^$+/, DMPP and McN-A-343 from the isolated perfused rat adrenal gland. Cilnidipine (1-10 ${\mu}$M) perfused into an adrenal vein for 60 min produced dose- and time-dependent inhibition in CA secretory responses evoked by ACh (5.32${\times}$10$\^$-3/M), DMPP (10$\^$-4/ M for 2 min) and McN-A-343 (10$\^$-4/ M for 2 min). However, lower dose of lobeline did not affect CA secretion by high K$\^$+/(5.6${\times}$10$\^$-2/ M), higher dose of it reduced greatly CA secretion of high K$\^$+/. Cilnidipine itself did also fail to affect basal catecholamine output. Furthermore, in adrenal glands loaded with cilnidipine (10 ${\mu}$M), CA secretory response evoked by Bay-K-8644 (10 ${\mu}$M), an activator of L-type Ca$\^$2+/channels was markedly inhibited while CA secretion by cyclopiazonic acid (10 ${\mu}$M), an inhibitor of cytoplasmic Ca$\^$2+/-ATPase was no affected. Moreover, $\omega$-conotoxin GVIA (1 ${\mu}$M), given into the adrenal gland for 60 min, also inhibited time-dependently CA secretory responses evoked by ACh and high K$\^$+/.

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Vaccinium bracteatum Thunb. Exerts Anti-Inflammatory Activity by Inhibiting NF-κB Activation in BV-2 Microglial Cells

  • Kwon, Seung-Hwan;Ma, Shi-Xun;Ko, Yong-Hyun;Seo, Jee-Yeon;Lee, Bo-Ram;Lee, Taek Hwan;Kim, Sun Yeou;Lee, Seok-Yong;Jang, Choon-Gon
    • Biomolecules & Therapeutics
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    • 제24권5호
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    • pp.543-551
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    • 2016
  • This study was designed to evaluate the pharmacological effects of Vaccinium bracteatum Thunb. methanol extract (VBME) on microglial activation and to identify the underlying mechanisms of action of these effects. The anti-inflammatory properties of VBME were studied using lipopolysaccharide (LPS)-stimulated BV-2 microglial cells. We measured the production of nitric oxide (NO), inducible NO synthase (iNOS), cyclooxygenase (COX)-2, prostaglandin $E_2$ ($PGE_2$), tumor necrosis factor-alpha (TNF-${\alpha}$), interleukin-1 beta (IL-$1{\beta}$), and interleukin-6 (IL-6) as inflammatory parameters. We also examined the effect of VBME on intracellular reactive oxygen species (ROS) production and the activity of nuclear factor-kappa B p65 (NF-${\kappa}B$ p65). VBME significantly inhibited LPS-induced production of NO and $PGE_2$ and LPS-mediated upregulation of iNOS and COX-2 expression in a dose-dependent manner; importantly, VBME was not cytotoxic. VBME also significantly reduced the generation of the pro-inflammatory cytokines TNF-${\alpha}$, IL-$1{\beta}$, and IL-6. In addition, VBME significantly dampened intracellular ROS production and suppressed NF-${\kappa}B$ p65 translocation by blocking $I{\kappa}B-{\alpha}$ phosphorylation and degradation in LPS-stimulated BV2 cells. Our findings indicate that VBME inhibits the production of inflammatory mediators in BV-2 microglial cells by suppressing NF-${\kappa}B$ signaling. Thus, VBME may be useful in the treatment of neurodegenerative diseases due to its ability to inhibit inflammatory mediator production in activated BV-2 microglial cells.

Anti-Inflammatory Effect of Ixeris dentata on Ultraviolet B-Induced HaCaT Keratinocytes

  • Kim, Sung-Bae;Kang, Ok-Hwa;Keum, Joon-Ho;Mun, Su-Hyun;An, Hyun-Jin;Jung, Hyun-Ju;Hong, Seung-Heon;Jeong, Dong-Myong;Kweon, Kee-Tae;Kwon, Dong-Yeul
    • Natural Product Sciences
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    • 제18권1호
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    • pp.60-66
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    • 2012
  • Human skin is the first line of defense for the protection of the internal organs of the body from different stimuli. Ultraviolet B (UVB) irradiation induces skin damage and inflammation through the secretion of various cytokines, which are immune regulators produced by cells. To prevent the initiation of skin inflammation, keratinocytes that have been irreversibly damaged by radiation must be removed through the apoptotic mechanism. Ixeris dentata (family: Asteraceae) is a perennial medicinal herb indigenous to Korea. It has been used in Korea, China, and Japan to treat in digestion, pneumonia, diabetes, hepatitis, and tumors. To gain insight into the anti-inflammatory effects of I. dentata, we examined its influence on UVB-induced pro-inflammatory cytokine production in human keratinocytes (HaCaT cells), by observing cells that were stimulated with UVB in the presence or absence of I. dentata. In the present study, pro-inflammatory cytokine production was determined by performing enzyme-linked immunosorbent assay, reverse transcription polymerase chain reaction, and western blot analysis to measure the activation of mitogen-activated protein kinase (MAPKs). I. dentata inhibited UVBinduced production of the pro-inflammatory cytokine interleukin (IL)-6 in a dose-dependent manner. Further, I. dentata inhibited the UVB-induced expression of cyclooxygenase (COX)-2. Furthermore, I. dentata inhibited the phosphorylation of c-Jun NH2-terminal kinase and p38 MAPKs, suggesting that it inhibits the secretion of the pro-inflammatory cytokines IL-6 and IL-8, and COX-2 expression, by blocking MAPK phosphorylation. These results suggest that I. dentate can potentially protect against UVB-induced skin inflammation.

N-(4-[$^{18}F$Fluoromethylbenzyl)spiperone : 유력한 도파민 $D_2$ 수용체 선택성 방사성리간드 (N-(4-[$^{18}F$]Fluoromethylbenzyl)spiperone : A Selective Radiotracer for In Vivo Studies of Dopamine $D_2$ Receptors)

  • 김상은;최연성;지대윤;이경한;최용;김병태
    • 대한핵의학회지
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    • 제31권4호
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    • pp.421-426
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    • 1997
  • [$^{18}F$]FMBS는 도파민 $D_2$ 수용체 방사성추적자로서 유망한 성질을 지니고 있다. [$^{18}F$]FMBS는 비교적 높은 특이결합/비특이결합 비를 제공하며, 그 체내결합은 도파민 $D_2$ 수용체에 대하여 높은 특이성과 선택성을 보인다. 도파빈 $D_2$ 수용체 측정을 위한 보다 적합한 PET 방사성추적자를 얻기 위해서는 [$^{18}F$]FMBS의 낮은 뇌섭취와 느린 역학을 개선할 수 있는 화학적 구조의 변형이 시도되어야 하며, [$^{18}F$]FMBS는 이러한 시도의 골격이 될 수 있을 것으로 믿는다.

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실리콘/수소/질소의 결합에 따른 MONOS 커패시터의 계면 특성 연구 (Interface Traps Analysis as Bonding of The Silicon/Nitrogen/Hydrogen in MONOS Capacitors)

  • 김희동;안호명;서유정;장영걸;남기현;정홍배;김태근
    • 대한전자공학회논문지SD
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    • 제46권12호
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    • pp.18-23
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    • 2009
  • 본 연구는 실리콘 기판과 실리콘 산화막 사이의 계면 트랩 밀도와 게이트 누설 전류를 조사하여, Metal-Oxide-Nitride-Oxide-Silicon (MONOS) 메모리 소자의 계면 트랩 특성의 수소-질소 열처리 효과를 조사하였다. 고속열처리 방법으로 850도에서 30초 동안 열처리한 MONOS 샘플들을 질소 가스와 수소-질소 혼합 가스를 사용하여 450도에서 30분 동안추가 퍼니스 열처리 공정을 수행하였다. 열처리 하지 않은 것, 질소, 수소-질소로 열처리 한 세 개의 샘플 중에서, 커패시터-전압 측정 결과로부터 수소-질소 열처리 샘플들이 가장 적은 계면 트랩 밀도를 갖는 것을 확인하였다. 또한, 전류-전압 측정 결과에서, 수소-질소 열처리 소자의 누설전류 특성이 개선되었다. 위의 실험 결과로부터, 수소-질소 혼합 가스로 추가 퍼니스 열처리의해 실리콘 기판과 산화막 사이의 계면 트랩 밀도를 상당히 줄일 수 있었다.