Zhao Xiao-yan, Chen Ji-qiang, Xie Qiang-min, Tang Hui-fang, Bian Ru-lain
Zhejiang Respiratory Drugs Research Laboratory of State Food and Drug Administration of China, College of Medicine, Zhejiang University, Hangzhou 310031, China.
Zhejiang Da Xue Xue Bao Yi Xue Ban. 2003 Aug;32(4):279-82, 291. doi: 10.3785/j.issn.1008-9292.2003.04.003.
To study the effects of very late antigen(VLA) antagonist BIO-1211 on eosinophil chemotaxis, recruitment and mediator release.
Eosinophil chemotaxis was induced by platelet activating factor(PAF) in vitro and eosinophil recruitment and release were determined in vivo.
VLA antagonist BIO-1211 inhibited eosinophil chemotaxis induced by PAF. The inhibitory rates at 4x10(-11), 4x10(-10), 4x10(-9) mol x L(-1) were 24.9%, 29.9%, and 31.3%, respectively. Pretreatment by BIO-1211 1, 3 and 10 mg x kg(-1) intraperitoneally inhibited the recruitment of eosinophils in PAF in the rat induced by Sephadex in a dose dependent manner. Inhibitory rates were 60.3%, 68.9%, and 72.9%(P<0.05), respectively. BIO-1211 did not inhibit eosinophil peroxidase(EPO) release from eosinophils.
BIO-1211 inhibits eosinophil chemotaxis and recruitment, alleviates local inflammation, and may represent a new type of drug for allergic diseases.
研究极迟抗原(VLA)拮抗剂BIO - 1211对嗜酸性粒细胞趋化、募集及介质释放的影响。
体外采用血小板活化因子(PAF)诱导嗜酸性粒细胞趋化,体内测定嗜酸性粒细胞募集及释放情况。
VLA拮抗剂BIO - 1211抑制PAF诱导的嗜酸性粒细胞趋化。4×10⁻¹¹、4×10⁻¹⁰、4×10⁻⁹ mol·L⁻¹时的抑制率分别为24.9%、29.9%和31.3%。腹腔注射1、3和10 mg·kg⁻¹的BIO - 1211预处理以剂量依赖方式抑制葡聚糖诱导的大鼠PAF中嗜酸性粒细胞的募集。抑制率分别为60.3%、68.9%和72.9%(P<0.05)。BIO - 1211不抑制嗜酸性粒细胞释放嗜酸性粒细胞过氧化物酶(EPO)。
BIO - 1211抑制嗜酸性粒细胞趋化和募集,减轻局部炎症,可能代表一种新型抗过敏药物。