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Research: HWANG and colleagues,
Listed in Issue 133
Abstract
HWANG and colleagues, Division of Biotechnology and Pharmaceutical Research, National Health Research Institutes, Miaoli County 350, Taiwan, Republic of China, have synthesized and described a potential herbal remedy for Hepatitis C.
Abstract: Hepatitis C is a severe liver disease that often leads to liver cirrhosis and liver carcinoma. Current therapy is inadequate to conquer this viral disease. This study identified parthenolide, an active component in feverfew (a popular remedy for fever and migraine), as a lead compound (with an EC50 value of 2.21 microM) against Hepatitis C virus replication. Parthenolide is able to potentiate the immune system’s own anti-virus effect. Several commercially available sesquiterpene lactones structurally analogous to parthenolide and a series of synthesized Michael-type adducts of parthenolide also exhibit micromolar concentrations for anti- Hepatitis C virus activities. Structure-activity relationship was elucidated to reveal that the spatial arrangement of the terpenoid skeleton fused with an alpha-methylene-gamma-lactone moiety produces maximal anti-Hepatitis C virus activity. This work shows that screening of natural products is a viable and fast way for identifying novel molecular diversity as potential drug leads.
Background
Methodology
Results
Conclusion
References
Hwang DR et al. Synthesis and anti-viral activity of a series of sesquiterpene lactones and analogues in the subgenomic HCV replicon system. Bioorganic & Medicinal Chemistry 14 (1): 83-91, Jan 1, 2006.