• 제목/요약/키워드: $P2Y_{12}$ Inhibitors

검색결과 93건 처리시간 0.025초

Comparison of safety and analgesic efficacy of diclofenac sodium with etodolac after surgical extraction of third molars: a randomized, double-blind, double-dummy, parallel-group study

  • Vaghela, Jitendra H.;Shah, Jigna H.;Patel, Jaladhi H.;Purohit, Bhargav M.
    • Journal of Dental Anesthesia and Pain Medicine
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    • 제20권1호
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    • pp.19-27
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    • 2020
  • Background: Surgical extraction of third molars is associated with postoperative pain and swelling at the extraction site. Pain is commonly managed using non-steroidal anti-inflammatory drugs (NSAIDs). Postoperative pain is usually moderate to severe in the first 12 h postoperatively and lasts for 3-5 days. However, with NSAIDs, these symptoms usually subside within 24 h. Diclofenac sodium and etodolac are NSAIDs, more selectively cyclooxygenase-2 inhibitors, with good analgesic efficacies. Methods: We compared the safety and analgesic efficacy of diclofenac sodium with etodolac peroral after surgical extraction of third molars in a double-blind, double-dummy, parallel-group study. The subjective pain improvement and pain relief after 2, 6, 24, 48, and 72 h using the visual analogue scale were measured as the study outcome. Results: Etodolac was equivalent to diclofenac sodium in pain alleviation at all postoperative time periods. No significant differences were found between diclofenac sodium and etodolac groups (P > 0.05). Both study medications were well tolerated and safe with mild adverse effects in only a few participants. Conclusion: Diclofenac sodium and etodolac are comparable in terms of analgesic efficacy and safety after surgical removal of third molars.

고혈압-연관 단백질 부활효소 C의 활성과 물리치료의 상관성 (The Activity of Hypertension-related Protein Kinase C and the Relationship of Physical Therapy)

  • 김중환
    • The Journal of Korean Physical Therapy
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    • 제20권3호
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    • pp.61-68
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    • 2008
  • Purpose: Protein kinase C (PKC) is a member of a family of serine/threonine kinases that are activated by diacylglycerol (DG) and PKC stimulants. PKC play a key role in signal transduction, including muscle contraction, cell migration, apoptosis, cell proliferation and differentiation. However, the mechanism relating mitogen-activated protein kinases (MAPKs) and PKC, especially in the volume-dependent hypertensive state, remains unclear. Methods: In the present study, I investigated the relationship between PKC and MAPKs for isometric contraction, PKC translocation, and enzymatic activity from normotensive sham-operated rats (NSR) and aldosterone-analogue deoxycorticosterone acetate (DOCA) hypertensive rats (ADHR). Results: Systolic blood pressure was significantly increased in ADHR than in NSR. Physiological salt solution (PSS)-induced resting tension and the intracellular $Ca^{2+}$ concentration ([$Ca^{2+}{_i}$]) were different in the ADHR and NSR. The expression of PKC$\alpha$, PKC$\beta$II, PKC$\delta$, PKC$\varepsilon$ and PKC$\xi$ were different between the cytoplasmic and membranous fractions. However, expression of the PKC isoforms did not differ for the ADHR and NSR. The use of 12-deoxyphorbol 13-isobutyrate (DPB, a PKC stimulant) induced isometric contraction in $Ca^{2+}$-free medium, which was diminished in muscle strips from ADHR as compared to NSR. Increased vasoconstriction and phosphorylation induced by the use of 1 ${\mu}$M DPB were inhibited by treatment with 10 ${\mu}$M PD098059 and 10 ${\mu}$M SB203580, inhibitors of extracellular-regulated protein kinase 1/2 (ERK1/2) and p38 MAPK from ADHR, respectively. Conclusion: These results suggest that the development of aldosterone analogue-induced hypertension is associated with an altered blood pressure, resting tension, [$Ca^{2+}{_i}$], and that the $Ca^{2+}$-independent contraction evoked by PKC stimulants is due to the activation of ERK1/2 and p38 MAPK in volume-dependent hypertension. Therefore, it is suggested that PKC activity affects volume-dependent hypertension and the need to develop cardiovascular disease-specialized physical therapy.

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패류의 호흡대사에 관한 연구(II) 담수산 패류, Cristaria plicata spatiosa (CLESSIN), 아가미 조직의 산화적 대사와 그 효소분에 대하여 (Study in the Respiratory Metabolism in Some Bivalves(II) on the Oxidative Metabolism and its Enzyme System in the Gill Tissue of the Fresh Water Mussel, Cristaria plicata spatiosa (CLESSIN))

  • 한문희;김동준;최희정
    • 한국동물학회지
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    • 제4권1호
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    • pp.7-12
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    • 1961
  • 1) Respiratory metabolism patterns and its enzyme systems in the gill tissue of the fresh water mussels, Cristaria plicata were investigated through the examination on the effects of respiratory enzyme inhibitors, (KCN, NAF) and succinoxidase assay, while studying the effects of neutral salts (NaCL, KCL, CaCl2) and pH on oxygen consumption of the gill tissue. 2) In the limited concentration of KCL (0.3mM) and NaCl (0.4mM) solutions, oxygen consumption of the intact gill tissue was accelerated, but in CaCl2(0.5mM) solution, it showed no significant effect. The oxygen consumption was gradually decreased at the above concentrations of these limitations. The optimum pH for the respiration of the gill was 7.3. 3)Cyanide in 10-8M solution inhibited 88.8% of the respiration of the intact gill tissue. Methylene blue accelerated the respiration of the noral gill tissue, and slightly but significantly reversed the cyaniide poisoned respiration. 4)Oxygen consumption of the gill homogenate was apparently increased by the mixed addition of succinate, cytochrome c and activators (AlCl3 and CaCl2). This results suggested that succinoxidase system acts on the respiratory pattern of the gil tissue. 5) It was able to recognize that the enolase, which acts on the anaerobic glycolytic system, participated in the tissue respiration of the gill for NaF in 5$\times$10-2 M solution inhibited 55.5% of the respiration of the same intact tissue.

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Long-term clinical outcome of acute myocardial infarction according to the early revascularization method: a comparison of primary percutaneous coronary interventions and fibrinolysis followed by routine invasive treatment

  • Min, Hyang Ki;Park, Ji Young;Choi, Jae Woong;Ryu, Sung Kee;Kim, Seunghwan;Song, Chang Sup;Kim, Dong Shin;Song, Chi Woo;Kim, Se Jong;Kim, Young Bin
    • Journal of Yeungnam Medical Science
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    • 제34권2호
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    • pp.191-199
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    • 2017
  • Background: This study was conducted to provide a comparison between the clinical outcomes of primary percutaneous coronary intervention (PCI) and that of fibrinolysis followed by routine invasive treatment in ST elevation myocardial infarction (STEMI). Methods: A total of 184 consecutive STEMI patients who underwent primary PCI or fibrinolysis followed by a routine invasive therapy were enrolled from 2004 to 2011, and their major adverse cardiovascular events (MACEs) were compared. Results: Among the 184 patients, 146 patients received primary PCI and 38 patients received fibrinolysis. The baseline clinical characteristics were similar between both groups, except for triglyceride level ($68.1{\pm}66.62$ vs. $141.6{\pm}154.3mg/dL$, p=0.007) and high density lipoprotein level ($44.6{\pm}10.3$ vs. $39.5{\pm}8.1mg/dL$, p=0.005). The initial creatine kinase-MB level was higher in the primary PCI group ($71.5{\pm}114.2$ vs. $35.9{\pm}59.9ng/mL$, p=0.010). The proportion of pre-thrombolysis in MI 0 to 2 flow lesions (92.9% vs. 73.0%, p<0.001) was higher and glycoprotein IIb/IIIa inhibitors were administered more frequently in the primary PCI group. There was no difference in the 12-month clinical outcomes, including all-cause mortality (9.9% vs. 8.8%, p=0.896), cardiac death (7.8% vs. 5.9%, p=0.845), non-fatal MI (1.4% vs. 2.9%, p=0.539), target lesion revascularization (5.7% vs. 2.9%, p=0.517), and stroke (0% vs. 0%). The MACEs free survival rate was similar for both groups (odds ratio, 0.792; 95% confidence interval, 0.317-1.980; p=0.618). The clinical outcome of thrombolysis was not inferior, even when compared with primary PCI performed within 90 minutes. Conclusion: Early fibrinolysis with optimal antiplatelet and antithrombotic therapy followed by appropriate invasive procedure would be a comparable alternative to treatment of MI, especially in cases of shorter-symptom-to-door time.

Alteration of X-linked Inhibitors of Apoptosis (XIAP) Expression in Rat Model with DEN-induced Hepatocellular Carcinogenesis

  • Chang, Jae-Jin;Jeon, Su-Yeon;Song, Ji-Ye;Kim, Jin-Hee;Li, Lan;Park, Dae-Hun;Lee, Yun-Lyul;Park, Jeong-Joo;Woo, Dong-Wook;Kim, Gi-Jin;Lee, Min-Jae
    • Molecular & Cellular Toxicology
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    • 제4권4호
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    • pp.278-284
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    • 2008
  • The X-linked inhibitor of apoptosis (XIAP) is a member of a novel family of inhibitors of apoptosis and has several BIR domains (BIR1, BIR2, and BIR3) and a carboxy-terminal RING zinc-finger. Since suppressionof apoptosis is fundamentally important for carcinogenesis and tumor growth, we investigated the expression and function of XIAP in DEN-induced carcinogenesis using rat model. Wistar rats were injected intraperitoneally with DEN at a dose of 50 mg/kg in twice a week for 12 weeks (Group II) and 16 weeks (Group III) followed by the recovery periods, respectively. The evaluation of DEN-induced carcinogenesis carried out the blood, RT-PCR, histopathological and western blot analysis. The level of blood chemistry including GOT/GPT, albumin, and total bilirubin were significantly exchanged comparing to control and Group I/Group II. The expression of albumin and collagen mRNA were significantly exchanged (P<0.05) in both groups. In addition, AFP mRNA expression decreased more after recovery periods than Group II. XIAP was expressed constitutively in normal rat liver as well as DEN-induced Groups I and Group II. In addition, XIAP expression increased more in Group I with 4 weeks recovery periods than Group I. However, XIAP expression shown to increase in Group lI, otherwise, it was decreased in Group II with 10 weeks repair periods. Taken together, these results suggest the alteration of XIAP expression could be involved in hepatocellular carcinogenesis.

"유-그레나"의 명암배양에 따르는 유기질의 이용과 호흡 및 생장에 대하여 (SOME PHYSIOLOGICAL STUDIES ON THE UTILIZATION OF ORGANIC SUBSTRATES BY EUGLENA GRACILIS VAR. BACILLA 10616 IN LIGHT AND IN DARKNESS)

  • Lee, Min-Jai
    • Journal of Plant Biology
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    • 제2권1호
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    • pp.1-12
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    • 1959
  • 1) The comparative studies of the quantitative measurement of growth characteristics and utilization of substrates by Euglena gracilis var. bacilla 10616 in the light and in darkness have been carried out. Eodogenous respiration, effect of respiratory inhibitors and responses to the added substrates for the exogenous respiration are also investigated. 2) All cultures are grown in the open air under the continuous illumination of fluorescent light of 3500 lux at room termperature, the growth rate of the culture in the basal medium added 0.5% lactate is found to be the highest. The growth rate decreases successively for the cultures of 0.5% sucinate, 0.5% Na-acetate, 0.5% malate, and control. There is no growth in the basal meidum added 0.5% butyrate and 0.5% hydroquinone. The similar results are obtained for the mentioned cultures in the darkness. However, the growth rate in basal medium added 0.5% glucose and 0.5% sucrose does seem to increase in the darkness unlike the illumination. 3) The endogenous rate of respiration for the organism cultured photosynthetically is about 12.94ul 02/mg/hr, in basal medium and the respiratory quotient is about 0.84. The rate is decreased by starvations to 6.5ul 02/mg/hr, about to a half, but the respiratory quotient does net change. 4) The oxygen consomption during initial 2 hours in suspending solution ranging from pH 4.5 to pH 9.3 is highest at pH 4.5 in which the algae had grown, at pH 5.5 and at pH 6.9. 5) Endogenous respiration of the cells is strongly inhibited by 0.1M of potassium cyanide, malomic acid, sodium fluoride and iodo-acetic acid. It is also strongly inhibited by 0.01M of potassium cyanide. 6) The respiratory response to added substrates for the exogenous respiration in the organism is coincided with the rate in the basal medium added the substrate in light and in darkness, whether the cells are fed or starved. 7) According to the results of this study, there seems to be the flexibility of the interconversion between photosynthesis and chemosynthesis, heterotropic mode of metabolism, in Euglena gracilis var. bacillaris, and that this organism utilizes the lactate most. It also may be suggested that the enayme systems linked in the each steps of Embden-Myerhof-Parnas path way and TCA cycle seem to exist in this organism.

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사과(Ralls Janet) Polyphenol Oxidase의 효소학적(酵素學的) 성질(性質) (Enzymatic Characteristics of Polyphenol Oxidase from Apple (Ralls Janet))

  • 정기택;서승교;송형익
    • 한국식품영양과학회지
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    • 제12권4호
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    • pp.316-322
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    • 1983
  • 사과 및 그 가공품의 효소적갈변(酵素的褐變)에 대한 기초적(基礎的) 자료(資料)를 얻고 나아가서 그 방지책(防止策)을 조사(調査)하는 목적으로 국광으로 부터 polyphenol oxidase(EC 1.10.3.1)를 추출(抽出)하여 그 일반적(一般的) 성질(性質)을 검토(檢討)하였다. 국광 polyphenol oxidase의 반응최적(最適) pH는 6.0이었으며 최적(最適) 반응온도(反應溫度)는 $30^{\circ}C$였다. 본효소(本酵素) pH 4.0에서 가장 안정성(安定性)이 높았으며, pH 5.0~9.0에서도 80% 이상(以上)의 활성(活性)을 나타내었다. 열(熱)에 대한 안정성(安定性)은 $40^{\circ}C$ 1시간(時間) 처리(處理)조건에서도 극히 안정(安定)하였으며 $60^{\circ}C$에서 30분(分) 처리(處理)로 효소(酵素) 활성(活性)이 50% 감소(減少)되었다. $Cu^{2+}$, $Fe^{3+}$, $Mg^{2+}$, $Mn^{2+}$의 첨가(添加)로 활성(活性)이 저해(沮害)되었다. 본효소(本酵素)에 대한 가장 효과적(效果的)인 저해제(沮害劑)는 cysteine, sodium, metabisulfite, ascorbate인 것으로 나타났다. 국광 polyphenol oxidase는 o-diphenol인 chlorogenic acid와 catechol을 크게 산화(酸化)시키는 것으로 보아 o-diphenol화합물(化合物)이 주(主) 기질(基質)인 것으로 생각되었다.

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Production of $\alpha$-Glucosidase Inhibitor by $\beta$-Glucosidase Inhibitor-Producing Bacillus lentimorbus B-6

  • Kim, Kyoung-Ja;Yang, Yong-Joon;Kim, Jongkee
    • Journal of Microbiology and Biotechnology
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    • 제12권6호
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    • pp.895-900
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    • 2002
  • A soil microorganism producing ${\alpha}$- and ${\beta}$-glucosidase inhibitors was identified as Bacillus lentimorbus, based on the fatty acid and morphological analyses, along with biochemical and physiological tests. The ${\alpha}$-glucosidase inhibitor was highly produced by this strain in a culture medium containing $0.25\%$ of sodium glutamate and $0.5\%$ of glucose, pH 8.0 at $30^{\circ}C$ for 2 days. The ${\alpha}$-glucosidase inhibitor from culture filtrate of his strain was identified as water soluble, organic solvent nonextractable, and heat stable. In addition to ${\alpha}$-glucosidase inhibitor, this strain also produced ${\beta}$-glucosidase inhibitor in he same culture medium and this inhibitor showed an antifugal activity against Botrytis cinerea. While the production of ${\alpha}$- glucosidase inhibitor was decreased by a glucose concentration higher than $1\%$, the production of ${\beta}$-glucosidase inhibitor was lot Influenced by a glucose concentration higher than $20\%$. The ${\alpha}$-glucosidase inhibitor from culture filtrate of this strain was separated from the ${\beta}$-glucosidase inhibitor through Sephadex G-100 column chromatography.

The Purification and Characterization of Bacillus subtilis Tripeptidase (PepT)

  • Park, Yong-Seek;Cha, Myung-Hoon;Yong, Whan-Mi;Kim, Hyo-Joon;Chung, Il-Yup;Lee, Young-Seek
    • BMB Reports
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    • 제32권3호
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    • pp.239-246
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    • 1999
  • A tripeptidase (PepT) was purified to homogeneity from Bacillus subtilis through four sequential chromatographies including DEAE-Sepharose ion exchange, hydroxylapatite, mono-Q FPLC ion exchange, and Superose-12 FPLC gel filtration. The apparent molecular mass of the enzyme was 49,200 Da and 51,400 Da as determined by sodium dodecylsulfatepolyacrylamide gel electrophoresis (SDS-PAGE) and gel filtration chromatography, respectively, and the enzyme exists in a monomeric form. The physicochemical properties of the enzyme were as follows: optimum pH at 7.5, optimum temperature at $60^{\circ}C$, and pI at 4.9. The $K_m$ and $V_{max}$ values of the enzyme were 4.3 mM and 2.5 mmol/min/mg, respectively, with MetAla-Ser as substrate. The B. subtilis PepT requires $Co^{2+}$ ion(s) for activation, while it is inactivated by EOTA and 1,10-phenanthroline, suggesting that it is a metalloprotein. The enzyme was not inhibited by any of serine protease, aspartic protease, or leucine aminopeptidase inhibitors. The enzyme showed comparable activities towards four different substrates including Met-Ala-Ser, Leu-Gly-Gly, Leu-Ser-Phe, and Leu-Leu-Tyr. The amino terminal sequence of PepT determined by Edman degradation was found to be MKEEIIERFTTYVXV and turned out to be identical to that of PepT deduced from a cloned B. subtilis pepT.

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Luciferase reporter gene assay를 이용한 단삼(丹蔘)추출물의 소염, 진통작용에 대한 in vitro 연구 (In Vitro Study of Anti-inflammatory and Analgesic Effects of Salvia Miltiorrhiza (SM) Extracts Using Luciferase Reporter Gene Assay)

  • 김희은;민상연;김장현
    • 대한한의학회지
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    • 제29권3호
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    • pp.88-99
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    • 2008
  • Objectives: In order to identify the anti-inflammatory and analgesic properties of Salvia miltiorrhiza (Dan-Sam), widely used in Korean traditional medicine, an in vitro screening system was designed using pGL3, a luciferase reporter vector, and the tumor necrosis factor (TNF)-${\alpha}$ and cyclooxygenase (COX)-2 as target genes. Methods: The promoter regions of each gene were generated by PCR using the human chromosome as template DNA, and inserted into pGL3 vector with Kpn I and Hind III. The final construct was transfected into human myelomonocytic leukemia cells (U-937) that could be differentiated and activated by phorbol 12-myristate 13-acetate (PMA) or lipopolysaccharide (LPS). Using this system, the anti-inflammatory and analgesic effects of several herbal extracts regarded to have the medicinal effects of diminishing body heat and complementing Qi were tested. The chemicals PD98059 and berberine chloride were used as controls of the transcriptional inhibitors of TNF-${\alpha}$ and COX-2, respectively. Results: Salvia miltiorrhiza (Dan-Sam) demonstrated significant decrease of TNF-${\alpha}$ and COX-2 mRNA in the in vitro assay system. In MTT assay, Salvia miltiorrhiza (Dan-Sam) did not significantly inhibit the survival and proliferation of human myelomonocytic leukemia cells (U-937). Conclusions: Salvia miltiorrhiza (Dan-Sam) was found to exhibit the significant medicinal properties of anti-inflammatory and analgesic effects.

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