Ferrándiz M L, Gil B, Sanz M J, Ubeda A, Erazo S, González E, Negrete R, Pacheco S, Payá M, Alcaraz M J
Departamento de Färmacologia, Universidad de Valencia, Facultad de Farmacia, Spain.
J Pharm Pharmacol. 1996 Sep;48(9):975-80. doi: 10.1111/j.2042-7158.1996.tb06016.x.
The effects of bakuchiol, a meroterpenoid isolated from the leaves of Psoralea glandulosa L., on phospholipase A2 (PLA2) activity from different sources, human neutrophil responses, zymosan air pouch and topical inflammation in mice, were investigated. This natural product was a weak inhibitor of secretory and intracellular PLA2 but dose-dependently reduced the formation of LTB4 and TXB2 by human neutrophils and platelet microsomes, respectively. In addition, bakuchiol inhibited degranulation in human neutrophils, whereas superoxide generation was not affected. In mice, bakuchiol decreased cell migration, myeloperoxidase activity and eicosanoid levels in the air pouch inflammation induced by zymosan. After topical administration, this compound was effective as an inhibitor of oedema and myeloperoxidase activity in the 12-O-tetradecanoylphorbol 13-acetate (TPA)-induced ear oedema and significantly reduced the PGE2 content and ear oedema in the arachidonic acid-induced response. Bakuchiol is a natural anti-inflammatory agent able to control leukocytic functions such as eicosanoid production, migration and degranulation in the inflammatory site.
研究了从腺叶补骨脂（Psoralea glandulosa L.）叶片中分离得到的半萜类化合物补骨脂酚对不同来源的磷脂酶A2（PLA2）活性、人中性粒细胞反应、酵母聚糖气袋及小鼠局部炎症的影响。该天然产物是分泌型和细胞内PLA2的弱抑制剂，但分别剂量依赖性地减少人中性粒细胞和血小板微粒体中白三烯B4（LTB4）和血栓素B2（TXB2）的生成。此外，补骨脂酚抑制人中性粒细胞的脱颗粒，而超氧化物生成不受影响。在小鼠中，补骨脂酚可减少酵母聚糖诱导的气袋炎症中的细胞迁移、髓过氧化物酶活性和类花生酸水平。局部给药后，该化合物在12-O-十四烷酰佛波醇-13-乙酸酯（TPA）诱导的耳水肿中作为水肿和髓过氧化物酶活性的抑制剂有效，并在花生四烯酸诱导的反应中显著降低前列腺素E2（PGE2）含量和耳水肿。补骨脂酚是一种天然抗炎剂，能够控制炎症部位的白细胞功能，如类花生酸生成、迁移和脱颗粒。
