肉豆蔻木脂素的体外代谢初步研究

目的建立诱导的大鼠肝微粒体药物代谢酶体外转化模型,评价肉豆蔻木脂素的体外代谢情况,为规模化制备肉豆蔻木脂素的代谢产物提供方法.方法将肉豆蔻木脂素与苯巴比妥诱导的大鼠肝微粒体药物代谢酶共温孵,用高效液相色谱法检测肉豆蔻木脂素及其代谢产物.结果肉豆蔻木脂素在苯巴比妥诱导的大鼠肝微粒体药物代谢酶作用下,可以被代谢,并且发现了7个代谢产物.结论建立的肝微粒体药物代谢酶模型可靠有效,可用于肉豆蔻中肉豆蔻木脂素的体外代谢研究.     

基于HPLC指纹图谱和多成分含量测定结合化学计量学的暖宫七味丸质量评价研究

目的 建立HPLC指纹图谱与多成分含量测定方法,结合化学计量学分析,评价暖宫七味丸（Nuangong Qiwei Pills,NQP）的质量。方法 采用RP-HPLC法,色谱柱为Grace Alltima HP C18柱（250 mm×4.6 mm,5μm）;流动相为甲醇-水,梯度洗脱;体积流量为1.0 mL/min;检测波长为220 nm。对4家生产企业14批NQP进行指纹图谱及4种指标性化学成分含量测定,利用化学模式识别法通过SPSS 20.0对含量测定数据进行聚类分析和通过SIMCA 14.1软件对NQP 4种定量成分进行主成分分析（principal component analysis,PCA）并将共有峰按峰面积进行差异性分析。结果 建立了NQP指纹图谱,共匹配出21个共有峰,分别归属沉香、丁香、肉豆蔻、豆蔻4味药材,指纹图谱相似度>0.98;对照品指认沉香四醇（6号峰）、丁香酚（8号峰）、肉豆蔻木脂素（14号峰）、去氢二异丁香酚（20号峰）4种化学成分,质量分数分别为0.120～0.416、1.574～5.018、0.103～0.205、0.093～0.139 mg/...     

Myrislignan Attenuates Lipopolysaccharide‐induced Inflammation Reaction in Murine Macrophage Cells Through Inhibition of NF‐κB Signalling Pathway Activation

Myrislignan is a new kind of lignan isolated from Myristica fragrans Houtt. Its antiinflammatory effects have not yet been reported. In the present study, the antiinflammatory effects and the underlying mechanisms of myrislignan in lipopolysaccharide (LPS)‐induced inflammation in murine RAW 264.7 macrophage cells were investigated. Myrislignan significantly inhibited LPS‐induced production of nitric oxide (NO) in a dose‐dependent manner. It inhibited mRNA expression and release of interleukin‐6 (IL‐6) and tumour necrosis factor‐α (TNF‐α). This compound significantly inhibited mRNA and protein expressions of inducible NO synthase (iNOS) and cyclooxygenase‐2 (COX‐2) dose‐dependently in LPS‐stimulated macrophage cells. Further study showed that myrislignan decreased the cytoplasmic loss of inhibitor κB‐α (IκB‐α) protein and the translocation of NF‐κB from cytoplasm to the nucleus. Our results suggest that myrislignan may exert its antiinflammatory effects in LPS‐stimulated macrophages cells by inhibiting the NF‐κB signalling pathway activation. Copyright © 2012 John Wiley & Sons, Ltd.