약학회지 (YAKHAK HOEJI)
- 제42권6호
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- Pages.558-566
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- 1998
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- 0377-9556(pISSN)
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- 2383-9457(eISSN)
리포폴리사카라이드에 의해 유도되는 대식세포의 프로스타글란딘 생합성을 저해하는 천연물의 탐색
Inhibitory Activities of Natural Products on Lipopolysaccharide Induced Prostaglandin Production in Mouse Macrophages
- 노민수 ((주)태평양 기술연구원) ;
- 하준용 ((주)태평양 기술연구원) ;
- 이창훈 ((주)태평양 기술연구원) ;
- 이우영 ((주)태평양 기술연구원) ;
- 이수환 (아주대학교 의과대학) ;
- 이정준 (생명공학연구소)
- Noh, Min-Soo (Pharmaceutical Research Institute, Pacific Co.) ;
- Ha, Jun-Yong (Pharmaceutical Research Institute, Pacific Co.) ;
- Lee, Chang-Hoon (Pharmaceutical Research Institute, Pacific Co.) ;
- Lee, Woo-Young (Pharmaceutical Research Institute, Pacific Co.) ;
- Lee, Soo-Hwan (Department of Physiology, School of Medicine, Ajou University) ;
- Lee, Jung-Joon (Korea Research Institute of Bioscience and Biotechnology, KIST)
- 발행 : 1998.12.01
초록
Two isoforms of cyclooxygenase (COX) have been identified - COX-1, which is constitlitively expressed in most tissues, and the inducible form, COX-2, of which expression is induced by inflammatory signals and mitogens. It has been considered that the beneficial effects of NSAIDs are due to the inhibition of COX-2 activity and the side effects are from the inhibition of COX-1 activity. Therefore, it is essential to develop selective COX-2 inhibitor for developing new GI-tolerable NSAIDS. To discover new leads for developing selective COX-2 inhibitors, three-hundred extracts of natural products were primarily screened with the system of prostaglandin accumulation in LPS-stimulated mouse peritoneal macrophages. To identify whether these inhibitory activities of crude extracts on the accumulation of Prostaglandins were derived from direct action against COX-2, the effects of selected extracts on exogenous arachidonic acid-derived production of prostaglandins by LPS-stimulated macrophages were determined. Among them, 5 methanol extracts of natural products, such as Zingiberis Rhizoma, Alpinae Officinarum Rhizoma, Caryophilli Flos, Scutellariae Radix, Dalbergia ordorifera. inhibited more than 70% of the prostaglandin production in LPS-stimulated mouse peritoneal macrophages at a con-centration of 1