期刊文献+

磷酸二酯酶4抑制剂Hemay005对人白细胞趋化活性的影响 被引量:2

Effects of the Phosphodiesterase 4 Inhibitor Hemay005 on Human Leukocytes Chemotaxis
下载PDF
导出
摘要 目的体外研究磷酸二酯酶4抑制剂Hemay005对人白细胞趋化活性的影响。方法体外分离和培养人外周血白细胞,用甲酰三肽(fMLP)作诱导剂,通过48孔微量趋化小室检测Hemay005人白细胞趋化功能的影响。结果 Hemay005与同类PDE4抑制剂CC-10004对fMLP诱导的人白细胞迁移均有明显抑制,抑制作用呈剂量依赖性,IC50值分别为0.188μg/ml和0.253μg/ml。结论 Hemay005可通过抑制炎性反应的中心环节-白细胞趋化而发挥抗银屑病作用。 Objective To evaluate the effects of the phosphodiesterase 4 inhibitor Hemay005 on human leukocytes chemotaxis in vitro. Methods Human peripheral leucocytes were isolated and cultured in vitro. The effects of Hemay005 on leukocytes chemotaxis in- duced by f - Met - Leu - Phe (fMLP) were detected with 48 - well chemotactic chamber assay. Results Both of Hemay005 and CC - 10004 can significantly inhibit leucocytes chemotactic activities towards fMLP and the inhibition effects were shown in a dose - dependent pattern. The 50% inhibitory concentration value (IC50) was 0. 188 and 0. 253μg/ml, respectively. Conclusion Hemay005 can play the role of antipsoriasis by inhibiting leukocytes chemotaxis which is the key step of inflammatory response.
出处 《医学研究杂志》 2012年第11期44-47,共4页 Journal of Medical Research
关键词 白细胞趋化 炎症 银屑病 磷酸二酯酶4抑制剂 Leukocytes chemotaxis Inflammation Psoriasis Phosphodiesterase 4 inhibitors
  • 相关文献

参考文献15

  • 1Monteleone G, Pallone F, MacDonald TT, et al. Psoriasis:from pathogenesis to novel therapeutic approaches [ J ]. Clin Sci (Lond), 2011, 120(1):1-11.
  • 2张艳丽,贾红侠,何焱玲.趋化因子在银屑病发病机制中的作用[J].首都医科大学学报,2010,31(5):673-677. 被引量:10
  • 3Houslay MD. Underpinning compartmentalised cAMP signalling through targeted cAMP breakdown[ J]. Trends Biochem Sci, 2010, 35(2) :91- 100.
  • 4Jacob C, Szilagyi C, Allen JM, et al. Role of PDE4 in superoxide anion generation through p44/42MAPK regulation:a cAMP and a PKA - independent mechanism[ J]. Br J Pharmacol, 2004,143 (2) :257 - 68.
  • 5Schafer PH, Parton A, Gandhi AK, et al. Apremilast, a cAMP phosphodiesterase - 4 inhibitor, demonstrates anti - inflammatory activity in vitro and in a model of psoriasis[ J]. Br J Pharmacol, 2010, 159 (4) :842 -855.
  • 6Kobayashi M, Kubo S, Hirano Y, et al. Anti - asthmatic effect of ASP3258, a novel phosphodiesterase 4 inhibitor[ J]. Int Immunopharmacol, 2012, 12(1) :50 -58.
  • 7Banner KH, Trevethick MA. PDE4 inhibition: a novel approach forthe treatment of inflammatory bowel disease [ J ]. Trends Pharmacol Sei, 2004, 25(8) :430 -436.
  • 8Heo JY, Cho YS, Cheon HG. Topical effects of roflumilast on 1 - chloro - 2,4 - dinitrobenzene - induced atopic dermatitis - like skin lesions in NC/Nga mice [ J ]. Pharmazie, 2010, 65 ( 12 ) :906 - 912.
  • 9Ryan C, Abramson A, Patel M, et al. Current investigational drugs in psoriasis [ J ]. Expert Opin Investig Drugs, 2012, 21 (4) :473 - 487.
  • 10Wong CH, Heit B, Kubes P. Molecular regulators of leucocyte chem- otaxis during inflammation [ J ]. Cardiovasc Res, 2010,86 ( 2 ) : 183 - 191.

二级参考文献52

共引文献37

同被引文献24

  • 1Albanesi C,Scarponi C,Giustizieri ML,et al.Keratinocytes in inflammatory skin diseases[J].Curr Drug Targets Inflamm Allergy,2005,4:329-334.
  • 2Dastidar SG,Rajagopal D,Ray A.Therapeutic benefit of PDE4 inhibitors inflammatory disease[J].Curr Opin Investig Drug,2007,8:364-372.
  • 3Ryan C,Abramson A,Patel M,et al.Current investigational drugs in psoriasis[J].Expert Opin Investig Drug,2012,21:473-487.
  • 4Shutty B,West C,Pellerin M,et al.Apremilast as a treatment for psoriasis[J].Expert Opin Pharmaeother,2012,13:1761-1770.
  • 5Hanel KH,Cornelissen C,Lüscher B,et al.Cytokines and the skin barrier[J].Int J Mol Sci,2013,14:6720-6745.
  • 6Borska L,Fiala Z,Krejsek J,et al.Immunologic changes in TNF-alpha,sE-selectin,sP-selectin,sICAM-1,and IL-8 in pediatric patients treated for psoriasis with the Goeckerman regimen[J].Pediatr Dermatol,2007,24:607-612.
  • 7Burnouf C,Pruniaux MP.Recent advances in PDE4 inhibitors as immunoregulators and anti-inflammatory drugs[J].Curr Pharm Des,2002,8:1255-1296.
  • 8Castro A,Jerez MJ,Gil C,et al.Cyclic nucleotide phosphodiesterascs and their role in imnmnonmdulalory responses:advances in the development of specific phosphodiesterase inhibitors[J].Med Res Rev,2005,25:229-244.
  • 9常晓萍,陈宏.肿瘤坏死因子-α在相关皮肤病发病中的作用[J].中国中西医结合皮肤性病学杂志,2009,8(1):62-64. 被引量:4
  • 10黄莹雪,李新宇.磷酸二酯酶4抑制剂抗银屑病机制研究进展[J].国际皮肤性病学杂志,2011,37(3):140-143. 被引量:1

引证文献2

二级引证文献1

相关作者

内容加载中请稍等...

相关机构

内容加载中请稍等...

相关主题

内容加载中请稍等...

浏览历史

内容加载中请稍等...
;
使用帮助 返回顶部