文章基本信息

标题：Ochnaflavone, Naturally Occurring Biflavonoid, Inhibits Phospholipase A2 Dependent Phosphatidylethanolamine Degradation in a CCl4-Induced Rat Liver Microsome
本地全文：下载
作者：Tae Chul Moon ; Hwa Shin Hwang ; Zhejiu Quan 等
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：2006
卷号：29
期号：12
页码：2359-2361
DOI：10.1248/bpb.29.2359
出版社：The Pharmaceutical Society of Japan
摘要：This study investigated the protective effects of a group IIA secretory phospholipase A₂ (sPLA₂-IIA) inhibitor, ochnaflavone, on the progression of carbon tetrachloride (CCl₄)-induced acute liver injury in rat liver microsomes in vitro . When rat liver was incubated at 37 °C in the presence of CCl₄, the level of phosphatidylethanolamine (PE) degradation increased markedly compared with the control. The rat 14 kDa platelet PLA₂ antibody, R377, suppressed the degradation of PE. Pretreating the microsome with ochnaflavone (2—16 μ M ) reduced the level of PE degradation in a dose dependent manner. In addition, p -bromophenacy bromide ( p -BPB), which is a PLA₂ inhibitor, also inhibited PE degradation. However, the inhibitory activity was weaker than that of ochnaflavone. Further investigation showed that ochnaflavone not only inhibited the purified rat platelet sPLA₂ activity in a dose dependent manner with an IC₅₀ value of 3.45 μ M , when arachidonyl PE was used as a substrate, but also inhibited lipid peroxidation in a dose dependent manner with an IC₅₀ value of 7.16 μ M . This result suggests that ochnaflavone prevents the progression of CCl₄-induced PE hydrolysis by inhibiting the endogenous sPLA₂ activity.
关键词：ochnaflavone;biflavonoid;secretory phospholipase A2;CCl4;rat liver microsome;lipid peroxidation