研究VLA24 拮抗剂BIO-1211对嗜酸粒细胞趋化、聚集和释放的影响。方法：采用离体方法测定血小板活化因子（PAF） 诱导的嗜酸性粒细胞反应，整体方法观察嗜酸性粒细胞聚集和释放反应。结果：BIO-1211能明显抑制PAF对嗜酸性粒细胞的趋化作用，BIO-12114×10-11、4×10-10、4×10-9 mol·L-1的抑制率分别为2419%、2919%、3113%。BIO-12111、3、10mg·kg- 1单次腹腔给药，呈剂量依赖性抑制大鼠葡聚糖凝胶引起的腹腔嗜酸粒细胞聚集，抑制率分别为013%、6819% 和7219% （P<0105），但不能抑制嗜酸性粒细胞释放嗜酸细胞过氧化物酶。结论：BIO-1211抑制嗜酸性粒细胞趋化和聚集, 减轻局部炎症反应, 有可能发展成为一种新的抗变态反应性药物。

目的：比较RR-福莫特罗和rac-福莫特罗对人支气管舒张作用。方法：将内径2～4mm、长15mm的人支气管螺旋条置入持续供氧的浴槽内，静息张力为1g，以蓄积给药法测定RR-福莫特罗（10 pmol•L-1～3.2 Lmol•L-1）和rac-福莫特罗（10 pmol•L-1～3.2 Lmol•L-1）在静息情况下，及氨甲酰胆碱（10 Lmo l•L-1）或组胺（100 Lmol•L-1）引起收缩情况下的张力改变。结果：RR-福莫特罗在静息状况下支气管舒张作用强于rac-福莫特罗（P<0.05）。RR-福莫特罗和rac-福莫特罗对抗由氨甲酰胆碱和组胺引起的收缩，且RR-福莫特罗的对抗作用强于rac-福莫特罗（P<0.05）。结论：RR-福莫特罗对人支气管的舒张作用强于rac-福莫特罗。

To study the inductive expression of human phosphodiesterase 4A (hPDE4A) in yeast cell GL62 and investigate the inhibitory effects of theophylline, rolipram, and acetamide-45 on PDE4A activity of the expressed product in yeast cell GL62. METHODS: Yeast cell GL62 were transfected with human PDE4A gene cloned in the expression plasmid p138NB. Expression was induced by adding CuSO4 to a final concentration of 150μmol/L, and the expressed product was extracted. The activity of PDE4A was detected by HPLC. RESULTS: Yeast cell GL62 expressed a certain protein at CuSO4 150μmol/L, the size of the expressed product was between 62 kDa and 83 kDa, the activity of PDE4A of the expressed product at 3 h was in maximum (188±23)μmol×g-1×min-1, and the Km was (17.7±2.6) mmol/L. Theophylline, rolipram, and acetamide-45 could inhibit the activity of PDE4A extracted from yeast cell GL62. The IC50 (95% confidence limits) of theophylline, rolipram, and acetamide-45 were 1642 (989-2727), 4.58 (3.45-6.08), and 275 (170-444) mmol/L respectively. CONCLUSION: PDE4A expressed in yeast cell GL62 is biologically active. Theophylline, rolipram, and acetamide-45 can inhibit the PDE4A activity. The expressed product in yeast cell GL62 may be used in the research work of PDE4 and its inhibitors.

目的：评价环孢素A气雾给药对豚鼠哮喘模型的药效。方法：用乙酰胆碱（ACh）或组胺诱导抗原攻击后的致敏豚鼠气道阻力pC200、支气管肺泡灌洗液（BALF）和肺组织切片中的嗜酸性粒细胞（EOS）变化观察环孢素A气雾给药后的抗气道高反应性和炎症作用。结果：环孢素AlOg•L-1、20g•L-1气雾给药和地塞米松（0.5mg-1kg ip）增加PC200值，能预防ACh或组胺引起的气道高反应性。环孢素A5g-L-1对组胺引起的气道高反应性也有作用，对Ach不显著．环孢素A10g•L-1、20g•L-1气雾给药能明显减少BAIF中的EOS浸润。与溶媒组比较，地塞米松0.5mg•kg-1增加了BALF中的中性粒细胞数日，与三组环孢素A比较有显著差异。在肺组织学研究中，环孢素A20g•L-1和地塞米松0.5mg•kg-1可抑制支气管和细支气管上皮和上皮表面结缔组织的EOS浸润。结论：环孢素A气雾吸入给药能明显对抗致敏豚鼠气道高反应性和炎症反应，为其治疗哮喘提供了一个可选择的给药途径。

To compare the bronchodilating and antiinflammatory effects of oral racemic formoterol (rac-FMT) and (R,R)-formoterol (R,R-FMT). METHODS: The changes of lung resistance (RL), dynamic lung compliance (Cdyn), and the accumulation of inflammatory cells in bronchoalveolar lavage fluids (BALF) induced by ovalbumin aerosol in sensitized guinea pigs and mice were investigated in vivo. RESULTS: Mean value increase of RL and mean value reduction of Cdyn from 1 to 30 min after antigen challenge were up to 101%