Inhibitory Activities of Natural Products on Lipopolysaccharide Induced Prostaglandin Production in Mouse Macrophages
리포폴리사카라이드에 의해 유도되는 대식세포의 프로스타글란딘 생합성을 저해하는 천연물의 탐색
노, 민수; 하, 준용; 이, 창훈; 이, 우영; 이, 수환; 이, 정준
Yakhakhoe chi, 42(6):558-566, 1998
Yakhakhoe chi; Journal of the Pharmaceutical Society of Korea; 약학회지
Two isoforms of cyclooxygenase (COX) have been identified - COX-1, which is constitutively 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 benificial effects of NSAIDs are due to the inhibition of COX-2 activity and the side effects are from the inhibition of COX-1 activity. There-fore, 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 pro-ducts 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 prostaglandin 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 concentration of 1 μg/ml.
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