Gordon Joel S, Wolanin Peter M, Gonzalez Arnold V, Fela David A, Sarngadharan Gopal, Rouzard Karl, Perez Eduardo, Stock Jeffry B, Stock Maxwell B
Signum Biosciences, Monmouth Junction, New Jersey, USA.
J Invest Dermatol. 2008 Mar;128(3):643-54. doi: 10.1038/sj.jid.5701061. Epub 2007 Sep 20.
N-acetyl-S-farnesyl-L-cysteine (AFC), a modulator of G protein and G-protein coupled receptor signaling, inhibits neutrophil chemotaxis and other inflammatory responses in cell-based assays. Here, we show topical AFC inhibits in vivo acute inflammation induced by 12-O-tetradecanoyl-phorbol-13-acetate (TPA) and arachidonic acid using the mouse ear model of inflammation. AFC inhibits edema, as measured by ear weight, and also inhibits neutrophil infiltration as assayed by direct counting in histological sections and by measuring myeloperoxidase (MPO) activity as a neutrophil marker. In addition, AFC inhibits in vivo allergic contact dermatitis in a mouse model utilizing sensitization followed by a subsequent challenge with 2,4-dinitrofluorobenzene. Unlike the established anti-inflammatories dexamethasone and indomethacin, AFC's action was restricted to the site of application. In this mouse model, both dexamethasone and indomethacin inhibited TPA-induced edema and MPO activity in the vehicle-treated, contralateral ear. AFC showed no contralateral ear inhibition for either of these end points. A marginally significant decrease due to AFC treatment was seen in TPA-induced epidermal hyperplasia at 24 hours. This was much less than the 90% inhibition of neutrophil infiltration, suggesting that AFC does not act by directly inhibiting protein kinase C.
N-乙酰基-S-法尼基-L-半胱氨酸(AFC)是一种G蛋白和G蛋白偶联受体信号传导的调节剂,在基于细胞的实验中可抑制中性粒细胞趋化性和其他炎症反应。在此,我们利用小鼠耳部炎症模型表明,局部应用AFC可抑制由12-O-十四烷酰佛波醇-13-乙酸酯(TPA)和花生四烯酸诱导的体内急性炎症。通过耳部重量测量,AFC可抑制水肿,并且通过组织学切片直接计数以及测量作为中性粒细胞标志物的髓过氧化物酶(MPO)活性来检测,AFC还可抑制中性粒细胞浸润。此外,在一个小鼠模型中,AFC可抑制体内过敏性接触性皮炎,该模型先进行致敏,随后用2,4-二硝基氟苯进行激发。与已有的抗炎药地塞米松和吲哚美辛不同,AFC的作用仅限于应用部位。在这个小鼠模型中,地塞米松和吲哚美辛均可抑制载体处理的对侧耳部中TPA诱导的水肿和MPO活性。对于这两个终点,AFC均未显示出对侧耳部抑制作用。在24小时时,TPA诱导的表皮增生因AFC处理而出现轻微但显著的降低。这远低于对中性粒细胞浸润90%的抑制作用,表明AFC并非通过直接抑制蛋白激酶C起作用。