Abad T, McNaughton-Smith G, Fletcher W Q, Echeverri F, Diaz-Peñate R, Tabraue C, Ruiz de Galarreta C M, López-Blanco F, Luis J G
Planta Med. 2000 Jun;66(5):471-3. doi: 10.1055/s-2000-8581.
The isolation and characterisation of (S)-(+)-6-methoxy-alpha-methyl-2-naphthaleneacetic acid, a well known synthetic non-steroidal anti-inflammatory drug (naproxene), from a natural source is described for the first time. We evaluated the ability of naproxene and its 7-methoxy isomer to abrogate constitutive COX-1 and inducible COX-2 activity in human A549 cells. Naproxene inhibited COX-1 (IC50 = 3.42 microM) and COX-2 (IC50 = 1.53 microM), whereas the 7-methoxy isomer had no appreciable effect on COX-1 (IC50 >> 100 microM) but also abrogated the activity of COX-2 enzyme (IC50 = 14.42 microM).
首次描述了从天然来源分离和鉴定（S）-（+）-6-甲氧基-α-甲基-2-萘乙酸，一种著名的合成非甾体抗炎药（萘普生）。我们评估了萘普生及其7-甲氧基异构体在人A549细胞中消除组成型COX-1和诱导型COX-2活性的能力。萘普生抑制COX-1（IC50 = 3.42 microM）和COX-2（IC50 = 1.53 microM），而7-甲氧基异构体对COX-1没有明显影响（IC50 >> 100 microM），但也消除了COX-2酶的活性（IC50 = 14.42 microM）。
