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In vitro inhibitory activities of lauraceae aporphine alkaloids

机译:月桂科植物阿菲啡生物碱的体外抑制活性

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摘要

The in vitro anti-inflammatory effect of eight aporphine alkaloids isolated from the leaves of two Lauraceae plants (Pleurothyrium cinereum and Ocotea macrophylla) was evaluated through inhibition of two isozymes of cyclooxygenase (COX-1 and COX-2), 5-lipoxygenase (5-LOX), and platelet aggregation induced by PAF, AA and ADP. All alkaloids exhibited inhibitory activities against COX-2 (IC_(50) 25.9-116 μM range) and PAF- and AA-induced platelet aggregation, while only four and three of them were good COX-1 and 5-LOX inhibitors, respectively. (+)-N-acetyl-nornantenine 6 was the most potent COX-2, 5-LOX, AA and PAF inhibitor.
机译:通过抑制两种环氧合酶(COX-1和COX-2),5-脂氧合酶(5)的同工酶,评估了从两种月桂科植物的叶中分离出的8种海豚碱生物碱的体外抗炎作用。 -LOX),以及由PAF,AA和ADP诱导的血小板聚集。所有生物碱均表现出对COX-2(IC_(50)25.9-116μM范围)以及PAF和AA诱导的血小板聚集的抑制活性,而分别只有4个和3个分别是良好的COX-1和5-LOX抑制剂。 (+)-N-乙酰基-降冰片烯6是最有效的COX-2、5-LOX,AA和PAF抑制剂。

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