• Title/Summary/Keyword: Antiiflammatory agent

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Synthesis of 2-Aryl-5-benzoxazolepropionic Acid Derivatives as Antiinflammatory Agent (항염증제로서 2-아릴-5-벤즈옥사졸프로피온산 유도체의 합성)

  • Choi, Hong-Dae;Kowak, Yong-Sil;Geum, Dek-Hyun;Son, Byeng-Wha
    • YAKHAK HOEJI
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    • v.38 no.5
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    • pp.504-510
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    • 1994
  • A facile synthesis of 2-aryl-5-benzoxazolepropionic acid derivatives(1 0a-d), which are potent antiinflammatory agent, is reported. Methyl ${\alpha}$-(p-hydroxyphenyl)propionate(5) was prepared from Friedel-Crafts reaction of isopropoxy benzene with methyl ${\alpha}$-chloro-${\alpha}$-(methylthio) acetate(1), followed by desulfurization, methylation and clevage of ether bond. Compounds(10a-d) were made from(5) by a sequence of nitration, reduction, formation of benzoxazole ring, and hydrolysis in good yields, respectively.

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Effect of Cyperi Rhizoma on $CCI_4$ Induced Hepatotoxicity and Lipid Peroxidation (향부자 분획물의 사염화탄소로 유도된 간장해 및 지질과산화에 미치는 영향)

  • Kim, Tae-Hee;Park, Ji-Young
    • Korean Journal of Pharmacognosy
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    • v.28 no.4
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    • pp.185-191
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    • 1997
  • Cyperus rotundus L. (Cyperaceae) has been used as an analgesic and antiiflammatory agent and in the treatment of menstrual disorder in folk remedies. Cyperi Rhizomata, processed and unprocessed, were extracted with methanol and fractionated with petroleum ether, chloroform. Butanol, water. The effect of unprocessed Cyperi Rhizoma and processed Cyperi Rhizoma on $CCl_4$ induced lipid peroxidation and hepatotoxity have been tested in rats. BuOH. Water fractions of unprocessed Cyperi Rhizome enhanced the inhibition of antilipid peroxidative effects in liver lipid. In chemical parameters obtained from serum analysis. Butanol fraction of unprocessed Cyperi Rhizoma showed significant decrease in hepatotoxicity. In result, unprocessed Cyperi rhizoma has significant antilipid peroxidative effect and hepatoprotective activity.

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Effect of Aprotinin on Changes in Plasma Thromboxane $B_2$ and Endothelin-1 Concentratin after Extracorporeal Circulation (체외순환후 혈중 Thromboxane $B_2$와 Endothelin-1 농도 변화에 미치는 Aprotinin의 효과)

  • Lim, Cheong;Yun, Tae-jin;Kim, Yeon-seung;Kim, Seung-hoo;Lee, Jae-dam;Rho, Joon-Ryang;Song, Meong-Gun
    • Journal of Chest Surgery
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    • v.33 no.3
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    • pp.221-229
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    • 2000
  • Background: Thromboxane A2 and endothelin-1 are the potent vasoconstrictors affecting pulmonary pathophysiology in response to whole body inflammatin following CPB. Aprotinin, as an antiiflammatory agent, may decrease the release of such vasoactive substance from pulmonary tissues, preventing pulmonary hypertension after cardiopulmonary bypass. Material and Method: Ten mongrel dogs(Bwt. ac. 20kg) were subjected to cardioupulmonary bypass for 2 hours and postbypass pulmonary vascular resistance(0, 1, 2, 3 hours) were compared with prebypass level. The dogs were divided into 2 groups; control group(n-5) and aprotinin group(n=5). In the aprotinin group, aprotinin was administered as follows; 50,000 KIU/kg mixed in pump priming solution, 50,000 KIU/kg prebypass intravenous infusion over 30 minutes, 10,000 KIU/kg/hour postbypass continuous infusion. Prebypass and postbypass 0, 1, 2, 3 hour pulmonary vascular resistance were measured. At prebypass and postbypass 0, 90, 180 minutes, blood samples were obtained from pulmonary arterial and left atrial catherers for the assay of plasma thromboxane B2 a stable metabolite of thromboxane A2, and endothelin-1 concentrations. Result: The ratios of pustbypass over prebypass pulmonary vascular at postbypass 0, 1, 2, 3 hours were 1.28$\pm$0.20, 1.82$\pm$0.23, 1.90$\pm$0.19, 2.14$\pm$0.18 in control group, 1.58$\pm$0.18, 1.73$\pm$0.01, 1.66$\pm$0.10, 1.50$\pm$0.08 in aprotinin group ; the ratios gradually increased in control group while decreased or fluctuated after postbypass 1 hour in aprotinin group. There was statistically significant difference between control group and aprotinin group at postbypass 3 hours(P=0.014). Pulmonary arterial plasma concentration of thromboxane B2(pg/ml) at prebypass, postbypass 0, 90, 180 minutes were 346.4$\pm$61.9, 529.3$\pm$197.6, 578.3$\pm$255.8, 493.3$\pm$171.3 in control group, 323.8$\pm$118.0, 422.6$\pm$75.6, 412.3$\pm$59.9, 394.5$\pm$154.0 in aprotinin group. Left atrial concentrations were 339.3$\pm$89.2, 667.0$\pm$65.7, 731.2$\pm$192.7, 607.5$\pm$165.9 in control group, 330.0$\pm$111.2, 468.4$\pm$190.3, 425.4$\pm$193.6, 4.7.3$\pm$142.8 in aprotinin group. These results showed decrement of pulmonary thromboxane A2 generation in aprotinin group. Pulmonary arterial concentrations of endothelin-1(fmol/ml) at the same time sequence were 7.84$\pm$0.31, 13.2$\pm$0.51, 15.0$\pm$1.22, 16.3$\pm$1.73 in control group, 7.76$\pm$0.12, 15.3$\pm$0.71, 22.6$\pm$6.62, 14.9$\pm$1.11 in aprotinin group. Left atrial concentrations were 7.61$\pm$17.2, 57.1$\pm$28.4, 18.9$\pm$18.2, 31.5$\pm$20.5 in control group, 5.61$\pm$7.61, 37.0$\pm$26.2, 28.6$\pm$21.7, 37.8$\pm$30.6 in aprotinin group. These results showed that aprotinin had no effect on plasma endothelin-1 concentration after cardiopulmonary bypass. Conclusion: Administration of aprotinin during cardiopulmonary bypass could attenuate the increase in pulmonary vascular resistance after bypass. Inhibition of pulmonary thromboxane A2 generation was thought to be one of the mechanism of this effect. Aprotinin had no effect on postbypass endothelin-1 concentration.

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