Mencherini T, Cau A, Bianco G, Della Loggia R, Aquino R P, Autore G
Dipartimento di Scienze Farmaceutiche, University of Salerno, Italy.
J Pharm Pharmacol. 2007 Jun;59(6):891-7. doi: 10.1211/jpp.59.6.0016.
Flavonoids, natural compounds widely distributed in the plant kingdom, are reported to affect the inflammatory process and to possess anti-inflammatory as well as immunomodulatory activity in-vitro and in-vivo. Since nitric oxide (NO) produced by inducible nitric oxide synthase (iNOS) is one of the inflammatory mediators, the effects of the ethanol/water (1:1) extract of the leaves of Apium graveolens var. dulce (celery) on iNOS expression and NO production in the J774.A1 macrophage cell line stimulated for 24 h with Escherichia coli lipopolysaccharide (LPS) were evaluated. The extract of A. graveolens var. dulce contained apiin as the major constituent (1.12%, w/w, of the extract). The extract and apiin showed significant inhibitory activity on nitrite (NO) production in-vitro (IC50 0.073 and 0.08 mg mL(-1) for the extract and apiin, respectively) and iNOS expression (IC50 0.095 and 0.049 mg mL(-1) for the extract and apiin, respectively) in LPS-activated J774.A1 cells. The croton-oil ear test on mice showed that the extract exerted anti-inflammatory activity in-vivo (ID50 730 microg cm(-2)), with a potency seven-times lower than that of indometacin (ID50 93 microg cm(-2)), the non-steroidal anti-inflammatory drug used as reference. Our results clearly indicated the inhibitory activity of the extract and apiin in-vitro on iNOS expression and nitrite production when added before LPS stimulation in the medium of J774.A1 cells. The anti-inflammatory properties of the extract demonstrated in-vivo might have been due to reduction of iNOS enzyme expression.
黄酮类化合物是广泛分布于植物界的天然化合物，据报道，它们在体外和体内均能影响炎症过程，并具有抗炎和免疫调节活性。由于诱导型一氧化氮合酶（iNOS）产生的一氧化氮（NO）是炎症介质之一，因此评估了旱芹（芹菜）叶乙醇/水（1:1）提取物对经大肠杆菌脂多糖（LPS）刺激24小时的J774.A1巨噬细胞系中iNOS表达和NO产生的影响。旱芹提取物的主要成分是芹菜苷（占提取物的1.12%，w/w）。该提取物和芹菜苷对LPS激活的J774.A1细胞体外亚硝酸盐（NO）产生（提取物和芹菜苷的IC50分别为0.073和0.08 mg mL(-1)）和iNOS表达（提取物和芹菜苷的IC50分别为0.095和0.049 mg mL(-1)）均表现出显著的抑制活性。对小鼠进行巴豆油耳肿胀试验表明，该提取物在体内具有抗炎活性（ID50为730 μg cm(-2)），其效力比用作对照的非甾体抗炎药吲哚美辛（ID50为93 μg cm(-2)）低7倍。我们的结果清楚地表明，在J774.A1细胞培养基中，在LPS刺激前加入提取物和芹菜苷，它们在体外对iNOS表达和亚硝酸盐产生具有抑制活性。提取物在体内表现出的抗炎特性可能是由于iNOS酶表达的降低。
