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Synthesis and Bio-Activity Evaluation of Scutellarein as a Potent Agent for the Therapy of Ischemic Cerebrovascular Disease

Scutellarein, the main metabolite of scutellarin in vivo, has relatively better solubility, bioavailability and bio-activity than scutellarin. However, it is very difficult to obtain scutellarein in nature compared with scutellarin. Therefore, the present study focused on establishing an efficient r...

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Autores principales: Qian, Li-Hua, Li, Nian-Guang, Tang, Yu-Ping, Zhang, Li, Tang, Hao, Wang, Zhen-Jiang, Liu, Li, Song, Shu-Lin, Guo, Jian-Ming, Ding, An-Wei
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Molecular Diversity Preservation International (MDPI) 2011
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3233465/
https://www.ncbi.nlm.nih.gov/pubmed/22174659
http://dx.doi.org/10.3390/ijms12118208
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author Qian, Li-Hua
Li, Nian-Guang
Tang, Yu-Ping
Zhang, Li
Tang, Hao
Wang, Zhen-Jiang
Liu, Li
Song, Shu-Lin
Guo, Jian-Ming
Ding, An-Wei
author_facet Qian, Li-Hua
Li, Nian-Guang
Tang, Yu-Ping
Zhang, Li
Tang, Hao
Wang, Zhen-Jiang
Liu, Li
Song, Shu-Lin
Guo, Jian-Ming
Ding, An-Wei
author_sort Qian, Li-Hua
collection PubMed
description Scutellarein, the main metabolite of scutellarin in vivo, has relatively better solubility, bioavailability and bio-activity than scutellarin. However, it is very difficult to obtain scutellarein in nature compared with scutellarin. Therefore, the present study focused on establishing an efficient route for the synthesis of scutellarein by hydrolyzing scutellarin. The in vitro antioxidant activities of scutellarein were evaluated by measuring its scavenging capacities toward DPPH, ABTS(+•), (•)OH free radicals and its protective effect on H(2)O(2)-induced cytotoxicity in PC12 cells using MTT assay method. The results showed that essential point to the synthesis was the implementation of H(2)SO(4) in 90% ethanol in N(2) atmosphere; scutellarein had stronger antioxidant activity than scutellarin. The results have laid the foundation for further research and the development of scutellarein as a promising candidate for ischemic cerebrovascular disease.
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spelling pubmed-32334652011-12-15 Synthesis and Bio-Activity Evaluation of Scutellarein as a Potent Agent for the Therapy of Ischemic Cerebrovascular Disease Qian, Li-Hua Li, Nian-Guang Tang, Yu-Ping Zhang, Li Tang, Hao Wang, Zhen-Jiang Liu, Li Song, Shu-Lin Guo, Jian-Ming Ding, An-Wei Int J Mol Sci Article Scutellarein, the main metabolite of scutellarin in vivo, has relatively better solubility, bioavailability and bio-activity than scutellarin. However, it is very difficult to obtain scutellarein in nature compared with scutellarin. Therefore, the present study focused on establishing an efficient route for the synthesis of scutellarein by hydrolyzing scutellarin. The in vitro antioxidant activities of scutellarein were evaluated by measuring its scavenging capacities toward DPPH, ABTS(+•), (•)OH free radicals and its protective effect on H(2)O(2)-induced cytotoxicity in PC12 cells using MTT assay method. The results showed that essential point to the synthesis was the implementation of H(2)SO(4) in 90% ethanol in N(2) atmosphere; scutellarein had stronger antioxidant activity than scutellarin. The results have laid the foundation for further research and the development of scutellarein as a promising candidate for ischemic cerebrovascular disease. Molecular Diversity Preservation International (MDPI) 2011-11-18 /pmc/articles/PMC3233465/ /pubmed/22174659 http://dx.doi.org/10.3390/ijms12118208 Text en © 2011 by the authors; licensee MDPI, Basel, Switzerland. http://creativecommons.org/licenses/by/3.0 This article is an open-access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/3.0/).
spellingShingle Article
Qian, Li-Hua
Li, Nian-Guang
Tang, Yu-Ping
Zhang, Li
Tang, Hao
Wang, Zhen-Jiang
Liu, Li
Song, Shu-Lin
Guo, Jian-Ming
Ding, An-Wei
Synthesis and Bio-Activity Evaluation of Scutellarein as a Potent Agent for the Therapy of Ischemic Cerebrovascular Disease
title Synthesis and Bio-Activity Evaluation of Scutellarein as a Potent Agent for the Therapy of Ischemic Cerebrovascular Disease
title_full Synthesis and Bio-Activity Evaluation of Scutellarein as a Potent Agent for the Therapy of Ischemic Cerebrovascular Disease
title_fullStr Synthesis and Bio-Activity Evaluation of Scutellarein as a Potent Agent for the Therapy of Ischemic Cerebrovascular Disease
title_full_unstemmed Synthesis and Bio-Activity Evaluation of Scutellarein as a Potent Agent for the Therapy of Ischemic Cerebrovascular Disease
title_short Synthesis and Bio-Activity Evaluation of Scutellarein as a Potent Agent for the Therapy of Ischemic Cerebrovascular Disease
title_sort synthesis and bio-activity evaluation of scutellarein as a potent agent for the therapy of ischemic cerebrovascular disease
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3233465/
https://www.ncbi.nlm.nih.gov/pubmed/22174659
http://dx.doi.org/10.3390/ijms12118208
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