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http://ir.cmu.edu.tw/ir/handle/310903500/29404
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題名: | Humic acid induces apoptosis in human endothelial cells |
作者: | Hseu, YC;Huang, HW;Wang, SY;Chen, HY;Lu, FJ;Gau, RJ;Yang, HL |
貢獻者: | 健康照護學院營養系;China Med Univ, Inst Nutr, Taichung 40421, Taiwan;Fooyin Inst Technol, Dept Med Technol, Kaohsiung, Taiwan;Natl Sun Yat Sen Univ, Inst Biomed Sci, Kaohsiung 80424, Taiwan;Natl Taiwan Univ, Coll Med, Dept Biochem, Taipei 10018, Taiwan |
日期: | 2002 |
上傳時間: | 2010-09-24 14:33:55 (UTC+8) |
出版者: | ACADEMIC PRESS INC ELSEVIER SCIENCE |
摘要: | Because the metabolites of arachidonic acid participate in many physiopathological responses, including inflammation and platelet aggregation, cyclooxygenase inhibitors are important in the treatment of associated diseases. A biologically active compound, 5-ethyl-4-methoxy-2-phenylquinoline (KTC-5), selectively and concentration dependently inhibited aggregation of platelets from man and ATP release caused by arachidonic acid (200 mum) and collagen (10 mug mL(-1)) without affecting the aggregation caused by thrombin (0.1 U mL(-1)) and U46619 (2 mum). The IC50 value (drug concentration inhibiting maximum response by 50%) of KTC-5 for aggregation induced by arachidonic acid and collagen was 0.11 +/- 0.04 mum and 0.20 +/- 0.03 mum, respectively. This inhibitory effect of KTC-5 was reversible and time dependent. KTC-5 specifically inhibited intracellular calcium mobilization initiated by arachidonic acid or collagen without affecting that caused by thrombin or U46619 in human platelets. Furthermore, KTC-5 inhibited thromboxane B-2 and prostaglandin D-2 formation provoked by arachidonic acid. The IC50 value of KTC-5 for arachidonic-acid-induced thromboxane B-2 formation was 0.07 +/- 0.02 mum. Based on these observations, the data indicated that KTC-5 potently inhibited human platelet aggregation and ATP release mainly via the inhibition of the cyclooxygenase-1 activity. Moreover, KTC-5 inhibited lipopolysaccharide-induced prostaglandin E-2 formation in RAW264.7 cells in the presence of external arachidonic acid with an IC50 value of 0.17 +/- 0.06 mum. Immunoblot analysis showed that KTC-5 did not affect the cyclooxygenase-2 expression in the presence of lipopolysaccharide on RAW264.7 cells. This result indicated that KTC-5 affects the activity of cyclooxygenase-2. According to these data, we concluded that KTC-5 is a cyclooxygenase inhibitor for both subtypes. |
關聯: | TOXICOLOGY AND APPLIED PHARMACOLOGY 182(1):34-43 |
顯示於類別: | [營養學系暨碩士班 ] 期刊論文
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