التفاصيل البيبلوغرافية
| العنوان: |
Synthesis and anti-viral activity of a series of sesquiterpene lactones and analogues in the subgenomic HCV replicon system |
| المؤلفون: |
Der-Ren Hwang, Yu-Shan Wu, Chun-Wei Chang, Tzu-Wen Lien, Wei-Cheng Chen, Uan-Kang Tan, John T.A. Hsu and Hsing-Pang Hsieh |
| المساهمون: |
徐祖安 |
| بيانات النشر: |
Elsevier |
| سنة النشر: |
2006 |
| المجموعة: |
National Tsing Hua University Institutional Repository (NTHUR) |
| مصطلحات موضوعية: |
Sesquiterpene lactones, Parthenolide, Hepatitis C virus replicon, Anti-HCV agents |
| الوقت: |
24 |
| الوصف: |
化學工程學系 ; ©2006 Elsevier - Hepatitis C virus (HCV) infection is a severe liver disease that often leads to liver cirrhosis and hepatocellular carcinoma (HCC). Current therapy is inadequate to conquer this viral disease. In this study, we identified parthenolide (1), an active component in feverfew, a popular remedy for fever and migraine, as a lead compound with an EC50 value of 2.21 μM against HCV replication in a subgenomic RNA replicon assay system. Parthenolide is able to potentiate the interferon α-exerted anti-HCV effect. Several commercially available sesquiterpene lactones (2–5) structurally analogous to parthenolide and a series of synthesized Michael-type adducts of parthenolide (12–18) also exhibit micromolar concentrations for anti-HCV activities. Structure–activity relationship was elucidated to reveal that the spatial arrangement of the terpenoid skeleton fused with an α-methylene-γ-lactone moiety produces maximal anti-HCV activity. In addition, a strong anti-HCV potency indicates a possibility of secondary amino adducts (12–18) converting back to parthenolide or being replaced by the nucleophilic residues of proteins inside cells. This work shows that screening of natural products is a viable and fast way for identifying novel molecular diversity as potential drug leads. |
| نوع الوثيقة: |
journal/newspaper |
| وصف الملف: |
application/pdf; 295008 bytes |
| اللغة: |
English |
| تدمد: |
0968-0896 |
| العلاقة: |
Bioorganic & Medicinal Chemistry, Elsevier, Volume 14, Issue 1, 1 January 2006, Pages 83-91; http://nthur.lib.nthu.edu.tw/dspace/handle/987654321/38349Test |
| الإتاحة: |
http://nthur.lib.nthu.edu.tw/dspace/handle/987654321/38349Test |
| رقم الانضمام: |
edsbas.7E3214C2 |
| قاعدة البيانات: |
BASE |
