中药调控NF-κB活性的研究进展

核因子-κB(nuclear factor-κB,NF-κB)是真核细胞内广泛存在的一种转录因子,在免疫、炎症、肿瘤等众多疾病的发生发展中起着重要作用。近年来大量研究发现很多对NF-κB相关疾病具有显著疗效的中药都表现出对NF-κB的活性抑制作用,通过在细胞及分子水平上对中药的作用机理分析表明,中药中确实存在着一些活性成分,能够在细胞或分子水平上调节NF-κB的活性,发挥治疗的作用。因此,提示中药可作为筛选NF-κB活性抑制药物的天然资源库,从中筛选NF-κB活性抑制药物是可行的。本文对具有NF-κB活性抑制作用的中药提取物、单体中药、单味中药和中药复方做了综述。

Suppressing progress of pancreatitis through selective inhibition of NF-κB activation by using NAC

Objective: To explore the characteristics of NF-闎 activation in the progress of pancreatitis, the relationship with expression of TNF- in the inflammatory reaction, and prevent the exacerbation of pancreatitis by using NAC. Method: Forty-eight rats were divided into three groups: therapy (group C), pancreatitis (group B) and control (group A). NAC served as the inhibitor of NF-闎 activation. In the time intervals of 1.5, 3.0, 6.0, 12.0 hour, NF-闎 activation was detected with flow cytometry (FCM) and the expression of TNF- mRNA and protein with in situ hybridization (ISH) and enzyme-linked immuno-sorbent assay (ELISA) respectively. Meanwhile, the level of lipase and amylase in the serum was assayed and the pathological change was evaluated. Result: NF-闎 activation in the pancreatitis group was higher than that in the control group (P<0.01), peaked at 3 hours, and was depressed by the inhibitor of NF-闎, NAC. The expression of TNF- as well as the level of lipase and amylase in the serum also rose synchronously with activation of NF-闎. In contrast to group A, it was significantly different (P<0.01) in group B. After using NAC in group C, all of these values were decreased and the in-flammatory reaction in the pancreas abated evidently. The pathology changes of the pancreas were shown to be alleviated in group C. Conclusion: First, NF-闎 activity is intensively initiated in the course of pancreatitis and shown to have closely relationship with the release of cytokines. Second, use of NAC markedly depressed NF-闎 activation. TNF- expression is down regulated by cytokines. It is suggested that NAC probably acts as a useful agent for treatment of pancreatitis by indirectly inhibiting activation of NF-闎.

Secondary metabolites from a deep-sea-derived Aspergillus versicolor F77

Chemical examination of fermentation products of a deep-sea-derived fungus Aspergillus versicolor F77 led to the isolation of two new compounds acetyl-sydonol(1)and 2-hydroxydiorcinol D(2),a new natural product 1-(2,4-dimethoxyphenyl)-1,2-dihydro-3 H-pyrazol-3-one(3),together with four known compounds sydonol(4),(S)-sydonic acid(5),aspergillusene A(6)and diorcinol D(7).Their structures were determined through the extensive spectroscopic analysis and comparison with the reported data in literature.Compound 6 showed moderate NF-κB inhibitory activity.

粗榧中2个新三尖杉酯碱类成分研究

采用硅胶、ODS、Sephadex LH-20和半制备HPLC等色谱技术,从粗榧中分离得到9个cephalotaxine型生物碱成分,分别为8-oxodeoxyharringtonine(1)、8-oxonordeoxyharringtonine(2)、cephafortunine A(3)、8-oxocephalotaxine(4)、deoxyharringtonine(5)、acetylcephalotaxine(6)、cephalotaxine(7)、epicephalotaxine(8)和cephalotaxinone(9)。化合物1和2为首次报道的新三尖杉酯碱类化合物,新化合物采用HR-ESI-MS、NMR、ECD等技术确定其结构。化合物1~3和5显示出显著的NF-κB转录抑制活性,其IC;分别为(3.91±0.70)、(2.99±0.45)、(7.84±0.51)、(1.46±0.17)μmol·L;。

中国南海海绵Luf fariella sp.的次生代谢产物研究

目的研究中国南海海绵Luffariellasp.的次生代谢产物及生物活性。方法利用硅胶柱色谱、C18反相柱色谱,半制备HPLC等方法对海绵提取物进行分离纯化,通过核磁共振、质谱、紫外、红外等波谱学技术,并结合文献理化数据,确定化合物的结构。对分离得到的化合物进行了NF-κB抑制活性评价实验。结果分离鉴定了6个含α、β-不饱和γ–内酯环的二倍半萜类化合物,结构确定为Hippolide H(1)、Hippolide F(2)、Hippolide G(3)、Hippolide E(4)、6Z-neomanoalide(5)、6E-neomanoalide(6)。在NF-κB抑制活性评价实验中,化合物1、4、6具有较好的NF-κB抑制活性。结论南海海绵Luffariellasp.可代谢具有NF-κB抑制活性的二倍半萜类化合物。