Abstract
In order to improve the metabolic stability and bioavailability of scutellarin, some derivatives of its main metabolite (scutellarein) were designed and synthesized. The antioxidant activities of these target products were assessed by measuring its scavenging capacities toward DPPH and the protective effects on H2O2-induced cytotoxicity in PC12 cells. The results showed that the target compound 7g had a higher antioxidant activity than scutellarin. Thus 7g may be considered as a novel potent anti-Alzheimers Disease drug candidate.
Keywords: Alzheimer's disease, Antioxidant, Derivative, Metabolism, Scutellarein, Scutellarin, Synthesize, anti-Alzheimer's Disease drug candidate, DPPH, cytotoxicity, PC12, Alzheimer's disease (AD), pathophysiological, neuroprotection, amyloid β protein, peroxynitrate
Letters in Drug Design & Discovery
Title: Design, Synthesis and Biological Evaluation of Scutellarein Derivatives as Potential Anti-Alzheimers Disease Candidates Based on Metabolic Mechanism
Volume: 9 Issue: 1
Author(s): Shu-Lin Song, Nian-Guang Li, Yu-Ping Tang, Zhen-Jiang Wang, Li-Hua Qian, Hao Tang and Jin-Ao Duan
Affiliation:
Keywords: Alzheimer's disease, Antioxidant, Derivative, Metabolism, Scutellarein, Scutellarin, Synthesize, anti-Alzheimer's Disease drug candidate, DPPH, cytotoxicity, PC12, Alzheimer's disease (AD), pathophysiological, neuroprotection, amyloid β protein, peroxynitrate
Abstract: In order to improve the metabolic stability and bioavailability of scutellarin, some derivatives of its main metabolite (scutellarein) were designed and synthesized. The antioxidant activities of these target products were assessed by measuring its scavenging capacities toward DPPH and the protective effects on H2O2-induced cytotoxicity in PC12 cells. The results showed that the target compound 7g had a higher antioxidant activity than scutellarin. Thus 7g may be considered as a novel potent anti-Alzheimers Disease drug candidate.
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Cite this article as:
Song Shu-Lin, Li Nian-Guang, Tang Yu-Ping, Wang Zhen-Jiang, Qian Li-Hua, Tang Hao and Duan Jin-Ao, Design, Synthesis and Biological Evaluation of Scutellarein Derivatives as Potential Anti-Alzheimers Disease Candidates Based on Metabolic Mechanism, Letters in Drug Design & Discovery 2012; 9 (1) . https://dx.doi.org/10.2174/157018012798192946
DOI https://dx.doi.org/10.2174/157018012798192946 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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