Structure-Activity Relationship of Phytoestrogen Analogs as ER alpha/beta Agonists with Neuroprotective Activities
- Authors
- Cho, Hye Won; Gim, Hyo Jin; Li, Hua; Subedi, Lalita; Kim, Sun Yeou; Ryu, Jae-Ha; Jeon, Raok
- Issue Date
- Jan-2021
- Publisher
- PHARMACEUTICAL SOC JAPAN
- Keywords
- phytoestrogen; estrogen receptor agonist; structure activity relationship; anti-neuroinflmmation
- Citation
- CHEMICAL & PHARMACEUTICAL BULLETIN, v.69, no.1, pp 99 - 105
- Pages
- 7
- Journal Title
- CHEMICAL & PHARMACEUTICAL BULLETIN
- Volume
- 69
- Number
- 1
- Start Page
- 99
- End Page
- 105
- URI
- https://scholarworks.sookmyung.ac.kr/handle/2020.sw.sookmyung/146838
- DOI
- 10.1248/cpb.c20-00706
- ISSN
- 0009-2363
1347-5223
- Abstract
- A set of isollavononid and llavonoid analogs was prepared and evaluated for estrogen receptor alpha (ER alpha) and ER beta transactivation and anti-neuroinflammatory activities. Structure activity relationship (SAR) study of naturally occurring phytoestrogens, their metabolites, and related isollavone analogs revealed the importance of the C-ring of isoflavonoids for ER activity and selectivity. Docking study suggested putative binding modes of daidzein 2 and dehydroequol 8 in the active site of ER alpha and ER beta, and provided an understanding of the promising activity and selectivity of dehydroequol 8. Among the tested compounds, equol 7 and dehydroequol 8 were the most potent ER alpha/beta agonists with ER beta selectivity and neuroprotective activity. This study provides knowledge on the SAR of isollavonoids for further development of potent and selective ER agonists with neuroprotective potential.
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