Abstract
The dried rhizome of Ligusticum chuanxiong Hort. (Umbelliferae) is a traditional Chinese medicine (TCM) herb for the prevention and treatment of inflammatory and cardiovascular diseases. However, the role of phthalide lactones from Ligusticum chuanxiong in the therapeutic actions is not yet fully understood. In the present study, two phthalide lactones from the herb, Z-ligustilide and senkyunolide A, were identified and characterized as inhibitors of lipopolysaccharide (LPS)-induced TNF-α production in monocytes. The results of gene expression studies showed that the observed TNF-α suppression was related to their inhibitory activity on TNF-α mRNA transcription. Furthermore, the two phthalides exhibited significant suppressive effects on TNF-α-mediated nuclear factor-κB (NF-κB) activation in reporter gene assays. Taken together, the results suggest that Z-ligustilide and senkyunolide A may have potential applications in the treatment of inflammation and related diseases based on their inhibitory activity on TNF-α production and TNF-α bioactivity. New insights into the therapeutic basis of the TCM herb, Ligusticum chuanxiong, are presented.
Abbreviations
TCM:traditional Chinese medicine
LPS:lipopolysaccharide
TNF-α:tumor necrosis factor-α
NF-κB:nuclear factor-κB
MAPK:mitogen-activated protein kinase
RT-PCR:reverse transcription polymerase chain reaction
Key words
TNF-α - LPS - monocytes - NF-κB - phthalide lactones -
Ligusticum chuanxiong
- Umbelliferae
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Yi-Yu Cheng
Pharmaceutical Informatics Institute
College of Pharmaceutical Sciences
Yuquan Campus
Zhejiang University
Hangzhou 310027
People’s Republic of China
Phone: +86-571-87952509
Fax: +86-57-87951138
Email: Chengyy@zju.edu.cn
