• Title/Summary/Keyword: Mechanism of action

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Convergence Studies of NO Homeostasis in Cellular Signalling (세포의 신호전달 과정에서 NO 항상성에 관한 융복합 연구)

  • Oh, Hee-Kyun;Do, Eun-Young;Park, Hae-Ryoung
    • Journal of Digital Convergence
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    • v.13 no.12
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    • pp.461-467
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    • 2015
  • Saussurea lappa is known for a variety of physiological activities as a component but has not known to show the effect of the cellular signaling pathway. We investigated the anti-inflammatory effects by Saussurea lappa ethanol extract on the LPS(lipopolysaccharide) induced nitric oxide (NO) production by RAW 264.7 cell line. It shows the expressions of iNOS and COX-2 at the transcriptional level (RT-PCR). The Saussurea lappa ethanol extract showed transcriptional expression levels of pro-inflammatory cytokine TNF- and IL-$1{\beta}$ induced by LPS(lipolysaccharide) in RAW264.7 cell line. Saussurea lappa ethanol extract reduced the LPS-induced expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) at the RNA levels in a concentration-dependent manner. The finding that ethanol extract of Saussurea lappa has an influence on NO (nitric oxide) homeostasis in the study of the action mechanism on the macrophage-mediated inflammatory reaction was considered in terms of convergence. And it is to provide an important basis for the prevention and treatment of inflammatory diseases in the future.

Usefulness of Meyerhold's 'Biomechanics' as an Alternative for a Method of Actor Training II - Focused on the Actual Training Program of 'Biomechanics' (배우 훈련 방법의 대안으로서 메이어홀드 '인체역학'의 효용성 II - '인체역학'의 실제 훈련 프로그램을 중심으로)

  • Cho, Han-Jun
    • The Journal of the Korea Contents Association
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    • v.14 no.11
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    • pp.89-101
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    • 2014
  • The 'Biomechanics', which was devised to systematically train actor's material and medium, is evaluated as the first approach to an acting method in earnest with Stanislavsky's 'System'. Especially, due to the psycho-physical features of 'Biomechanics' that helps an actor to master a mechanism of human being such as stimulus, impulse and reaction, it was valued as an alternative for a naturalistic acting method that was excessively focused on the actor's emotional expression. However, the 'Biomechanics' is not utilized with activity in a field of actor training in Korea compared with Stanislavsky's 'The Method of Physical Action' which has a similar starting point as the psycho-physical feature. It is because of a political reason that a study for Meyerhold was officially forbidden in Russia until the mid-twentieth century. It is also because of a limit that incorporeal features of the 'Biomechanics' could not but be explained only by publications, especially translation. In this sense, as part of seeking for a new alternative of acting methods in Korea, this study will explore a possibility of applying the 'Biomechanics' to the actual actor training field through correct understanding of it.

Inhibition of protoporphyrinogen oxidase activity and selectivity of new compound EK-5439 (신규 화합물 EK-5439의 선택성 및 protoporphyrinogen oxidase 저해활성)

  • Hong, K.S.;Kim, H.R.;Jeon, D.J.;Lee, B.H.;Song, J.H.;Cho, K.Y.;Hwang, I.T.
    • The Korean Journal of Pesticide Science
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    • v.8 no.2
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    • pp.79-87
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    • 2004
  • 3-Chloro-2-[4-chloro-2-fluoro-5-(5-methyl-3-phenyl-4,5-dihydroisoxazol-5-ylmethoxy)-phenyl]-4,5,6,7-tetrahy dro-2H-indazole(EK-5439) demonstrated rice selectivity and herbicidal activity on annual weeds, such as Echinochloa oryzicola, Monochoria vaginalis, Lindernia pyxidaria, Rotala indica, Aneilema keisak, Cyperus difformis, and Ludwigia prostrata at doses of 16-63 g a.i./ha. However, the application window was limited from pre-emergence to 5 days after transplanting. The control efficacy of EK-5439 on barnyardgrass was 4 times higher than that of oxadiazon. EK-5439 was excellently safe to the 16 different transplanted rice cultivars treated 2 days after transplanting. These compounds have the mechanism of action on the chlorophyll biosynthesis like protoporphyrinogen IX oxidase inhibitors.

Selective Mechanism of Oxvfluorfen and Chlormethoxynil in Crops and Weed Species (Oxyfluorfen과 Chlormethoxynil의 선택작용성(選擇作用性))

  • Lee, J.H.;Pyon, J.Y.;Lee, J.Y.
    • Korean Journal of Weed Science
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    • v.14 no.4
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    • pp.280-290
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    • 1994
  • The germination and the nutrient culture tests in the growth chamber and pot experiment under two types of soil conditions were conducted to determine the selectivity of oxyfluorfen and chlormethoxynil in crops and weeds and for characterization of selective mode of action, the absorption study was also conducted with different absorption methods and application time using $^{14}C$-oxyfluorfen. Oxyfluorfen showed more growth inhibitory effects than chlormethoxynil. In the nutrient culture test, rice growth was greatly inhibited at 2-leaf stage than at 4-leaf stage, and the shoot parts were more inhibited than the root parts. By preemergence application of both herbicides, higher growth inhibition was observed in sandy loam soil than in clay loam soil. Absorption and translocation of $^{14}C$-oxyfluorfen were higher by foliar application than by root treatment, and selectivity of crops and weed species may be explained partly by the amount of absorption.

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Preclinical Study of DA-5018, a Non-narcotic Analgesic Agent

  • Kim, Soon-Hoe
    • Proceedings of the PSK Conference
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    • 2000.04a
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    • pp.70-81
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    • 2000
  • DA-5018 is a synthetic capsaicin derivative under development as a non-narcotic a analgesic ag$\varepsilon$nt. DA-50 18 showed a potent analgesic activity against acute and chronic pain m model(Tablel, 2.), but it had a narrow margin of safety. DA-5018 did not bind to opioid(${\kappa}, {\delta}, {\mu}$), NKl, CGRP receptors in vitro and its analgesic effect was not antagonized by naloxone, a and it did not develop analgesic tolerance. In addition DA-5018 had no inhibitory effects against c cyclooxygenase and 5-lipooxygenase activities. DA-5018 significantly increased the relcase of substance P from the slices of the rat spinal cord. These results suggest that DA-50 18 is not a narcotic nor aspirin-like analgesic and the release of substance P is one of analgesic mechanism of action of DA-5018. We found that DA-5018 was almost ten times more potent and was at l least IOO-times less irritable compared to capsaicin. Accordingly development of topical formula was adopted. Topical formula was desiged and screened by flux test of DA-5018 using hairless mouse skin and several formulas were selected. With these topical formulas we a assessed the analgesic efficacy and carried out the toxicity, skin irritation and pharmacokinetic studies. In streptozotocin-induced hyperalgesic rat and 50 % galactose-fed hyperalgesic rat as diabetic pain models, DA-5018 cream increased the pain thresh이ds up to 77.0% and 24.4% respectively, while Zostrix-HP(capsaicin cream) incr$\varepsilon$as cd by 65.9% and 21.0%. DA-5018 c cream showed a good analgesic effect as welI in FCA-induced arthritic rat. DA-5018 cream did not show any toxicological signs in acute and chronic toxicity test and had little skin irritation in car swclIing and scratching t$\varepsilon$st. Pharmacokinetics of DA-50 18 were studied after topical application of ${14}^C$-Iabelled or unlabelIed DA-5018 cream. Plasma and skin concentrations c except applied skin wcre below the dctection limit and after 7-day cummulative application, plasma concentrations were also below detection limit DA-50 18 may have an advantag$\varepsilon$ ov$\varepsilon$r c capsaicin and is now being developed as a topical agent for the treatment of pains. DA-50 18 cream was approved for Korean IND and is now under a Phase II clinical study for arthritic pain a after finising Phase I study. DA-50 18 was also liscensed out to Stiefel Company in America in

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Cultivated Orostachys japonicus Induces Apoptosis in Human Colon Cancer Cells (인체 대장암 세포주 SW480에서 재배 와송의 세포 사멸 유도 효과)

  • Kim, Jae-Yong;Jung, Eun-Jung;Won, Yeong-Seon;Lee, Ju-Hye;Shin, Dong-Young;Seo, Kwon-Il
    • Korean Journal of Food Science and Technology
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    • v.44 no.3
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    • pp.317-323
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    • 2012
  • This study was performed to elucidate the anticancer activities and the mechanism of chloroform fractions from cultivated Orostachys japonicus (CFCOJ) in human colon cancer cells. CFCOJ markedly decreased viable cell numbers in both a dose-dependent and time-dependent manner within SW480 cells. Cell death induced by CFCOJ increased cell populations in the sub-G1 phase, as well as the formation of apoptotic bodies, nuclear condensation, and induced DNA fragmentation. CFCOJ-induced apoptosis was associated with the activation of initiator caspase-8 and -9, as well as the effector caspase-3. CFCOJ also stimulated Bid cleavage, indicating that the apoptotic action of caspase-8-mediated Bid cleavage leads to the activation of caspase-9. CFCOJ increased the expression of the proapoptotic protein, Bax, and decreased the expression of the antiapoptotic protein, Bcl-2. These results indicate that CFCOJ exert anticancer effects on human colon cancer SW480 cells through a caspase-dependent apoptotic pathway.

Improvement Effect of Non-alcoholic Fatty Liver Disease by Curcuma longa L. Extract (강황 추출물의 비알코올성 지방간 질환 개선 효과)

  • Lee, Young Seob;Lee, Dae Young;Kwon, Dong Yeul;Kang, Ok Hwa
    • Korean Journal of Medicinal Crop Science
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    • v.28 no.4
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    • pp.276-286
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    • 2020
  • Background: Non-alcoholic fatty liver disease (NAFLD) is a chronic liver disease associated with multiple metabolic disorders. The medicinal plant Curcuma longa L. is widely distributed in Asia and has been used to treat a spectrum diseases in clinical practice. To date, there are inadequate reports of the effects of C. longa 50% EtOH extract (CE) on NAFLD. Therefore, in this study, we evaluate the CE on an NAFLD animal and elucidate the mechanism of action. Methods and Results: C57BL/6J mice fed a methionine-choline deficient diet (MCD) were treated with CE or milk thistle, and changes in inflammation and stetosis were assessed. Experimental animals were divided into six group (n = 10); Normal, MCD, MCD + CE 50 mg/kg/day (CE 50), MCD + CE 100 mg/kg/day (CE 100), MCD + CE 150 mg/kg/day (CE 150), and the Control, MCD + Milk thistle 150 mg/kg/day (MT 150). Body weight, liver weight, liver function, and histological changes were assessed in experimental animals. Quantitative real-time polymerase chain reaction and western blot analyses were performed on samples collected after 4 weeks of treatment. We observed that CE administration improved MCD-diet-induced lipid accumulation, and triglyceride (TG) and total cholesterol (TC) levels in serum. Treatment with CE also decreased hepatic lipogenesis through modulation of the sterol regulatory element binding protein-1 (SREBP-1), CCAAT-enhancer binding protein α (C/EBPα), fatty acid synthase (FAS), and peroxisome proliferator-activated receptor γ (PPARγ) expresion. In addition, the use of CE increased adenosine monophosphate-activated protein kinase (AMPK) phosphorylation and inhibited the up-regulation of toll-like receptor (TLR)-2 and TLR-4 signaling and the production of inflammatory mediators. Conclusions: In this report, we observed that CE regulated lipid accumulation in an MCD dietinduced NAFLD model by decreasing lipogenesis. These data suggeste that CE could effectively protect mice against MCD-induced NAFLD, by inhibiting the TLR-2 and TLR-4 signaling cascades.

Depigmenting Effects of Mistletoe (Viscum album var. coloratum) Extracts (겨우살이 추출물의 미백 효과)

  • Hah, Young-Sool;Kim, Eun-Ji;Goo, Young Min;Kil, Young Sook;Sin, Seung Mi;Kim, Sang Gon;Kang, Ha Eun;Yoon, Tae-Jin
    • Journal of Life Science
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    • v.32 no.5
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    • pp.355-361
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    • 2022
  • Melanin pigments are the main cause of skin color. They are produced in melanocytes and then transferred to keratinocytes, which eventually gives the skin surface a variety of colors. Although many skin-lightening or depigmenting agents have been developed, the demand for materials to reduce pig- mentation is still increasing. Here, we tried to find materials for skin-lightening or depigmentation using natural compounds and found that mistletoe (Viscum album var. coloratum) extracts (ME) had an inhibitory effect on tyrosinase activity. As a result, ME significantly reduced pigmentation in human primary melanocytes. In addition, a promoter reporter assay revealed that ME inhibited the transcription of microphthalmia-associated transcription factor (MITF), melanophilin (MLPH), tyrosinase-related protein-2 (TRP-2), and tyrosinase (TYR) genes in HM3KO melanoma cells. In addition, ME decreased the protein level for pigmentation-related molecules, such as TYR and TRP-1. Furthermore, it markedly inhibited the melanogenesis of zebrafish embryos, an in vivo evaluation model for pigmentation. To elucidate the action mechanism of ME, we investigated its effects on intracellular signaling. Eventually, the ME dramatically decreased the phosphorylation of the cAMP responsive element binding protein (CREB), AKT, and ERK. The data suggest that ME may inhibit the melanogenesis pathway by regulating the signaling pathway related to pigmentation. Taken together, these data propose that ME can be developed as a depigmenting or skin-lightening agent.

Breakthrough Cancer Pain (돌발성 암성 통증)

  • Seo, Min Seok;Shim, Jae Yong
    • Journal of Hospice and Palliative Care
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    • v.18 no.1
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    • pp.1-8
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    • 2015
  • Breakthrough cancer pain is a transient exacerbation of pain that occurs despite relatively well controlled background pain with around-the-clock analgesia. It is highly prevalent in patients with cancer pain, with an overall prevalence of 70~90%. Breakthrough cancer pain has several negative effects on quality of life, including a decrease in functional status and social relationship, and higher incidence of anxiety/depression. It also places a detrimental burden on their families, society, and the healthcare system. According to the pathogenic mechanism, breakthrough cancer pain is classified into two categories: idiopathic (or spontaneous) pain and incident pain. Episodes of breakthrough cancer pain have typical characteristics, including rapid onset (5~10 min), severe intensity, and short duration (30~60 min). However, there are some variations in timing and severity of pain among patients and episodes. Therefore, a thorough assessment of pain episodes is needed and management plan must be individualized to provide optimal treatment. Several immediate-release formulations such as oxycodone, morphine, and hydromorphone are widely used despite relatively slow onset of action. Recent studies have shown that transmucosal fentanyl preparations were effective for faster control of breakthrough pain. We hope to improve management of breakthrough cancer pain with more efficient analgesics in line with currently available evidence.

Absorption, Translocation and Metabolism of Naproanilide in Rice and Paddy Weeds under Different Temperature Conditions (수도(水稻)와 잡초(雜草)에서 온도조건(溫度條件)에 따른 Naproanilide의 흡수(吸收), 이행(移行) 및 대사(代謝)에 관(關)한 연구(硏究))

  • Park, C.W.;Pyon, J.Y.;Kim, Y.W.
    • Korean Journal of Weed Science
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    • v.11 no.3
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    • pp.187-194
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    • 1991
  • Absorption and translocation, and metabolism studies using $^{14}C$-naproanilide were conducted to determine selective mode of action of naproanilide in rice and paddy weeds under different temperature conditions. Absorption amount of $^{14}C$-naproanilide was greater in Cyperus serotinus and Sagittaria pygmaea than rice and Echinochloa crusgalli. Especially, absorption of $^{14}C$-naproanilide in C. serotinus was increased twice at 32 $^{\circ}C$ and 48 hour exposure conditions. $^{14}C$-naproanilide in roots was translocated to shoots very little in rice and E. crusgalli, but S. pygmaea somewhat greater translocation than the other species. In C. serotinus and S. pygmaea, susceptible weeds, metabolic rates of naproanilide into phytotoxic NOP (2-(2-naphthoxy)-propionic acid) and NOPM (methyl 2-(2-naphthoxy) propionate) were significantly greater than in rice and E. crugalli, tolerant species. Consequently, differential uptake by roots and the difference in activation metabolism of naproanilide among species may explain the possible mechanism of selectivity.

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