The Synthesis and Evaluation of Novel Hydroxyl Substituted Chalcone Analogs with in Vitro Anti-Free Radicals Pharmacological Activity and in Vivo Anti-Oxidation Activity in a Free Radical-Injury Alzheimer’s Model

doi:10.3390/molecules18021693

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Molecules 2013, 18(2), 1693-1703; doi:10.3390/molecules18021693

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The Synthesis and Evaluation of Novel Hydroxyl Substituted Chalcone Analogs with in Vitro Anti-Free Radicals Pharmacological Activity and in Vivo Anti-Oxidation Activity in a Free Radical-Injury Alzheimer’s Model

Ying Pan^1,†, Yicun Chen^2,†, Qingnan Li³, Xiaoyu Yu¹, Jinzhi Wang¹ and Jinhong Zheng^1,*

¹ Department of Chemistry, Shantou University Medical College, Shantou 515041, Guangdong, China ² Department of Pharmacology, Shantou University Medical College, Shantou 515041, Guangdong, China ³ Shantou Central Hospital, Shantou 515041, Guangdong, China ^† These authors contributed equally to this work.

* Author to whom correspondence should be addressed.

Received: 29 November 2012; in revised form: 20 December 2012 / Accepted: 20 January 2013 / Published: 28 January 2013

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Abstract: Alzheimer’s disease (AD) pathogenesis involves an imbalance between free radical formation and destruction. In order to obtain a novel preclinical anti-AD drug candidate, we synthesized a series of novel hydroxyl chalcone analogs which possessed anti-free radical activity, and screened their effects on scavenging 2,2-diphenyl-1-picrylhydrazyl (DPPH) and OH free radicals in vitro. Compound C7, 4,2'-dihydroxy-3,5-dimethoxychalcone was found to have potent activity in these anti-free radical activity tests. Further research revealed that C7 could elevate glutathione peroxidase (GSH-PX) and super oxide dismutase (SOD) levels and lower malonaldehyde (MDA) level in vivo in the Alzheimer’s model. The indication of C7’s effect on AD needs further study.

Keywords: Alzheimer’s; free radical injury; polypheols; hydroxyl-substituted chalcones

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MDPI and ACS Style

Pan, Y.; Chen, Y.; Li, Q.; Yu, X.; Wang, J.; Zheng, J. The Synthesis and Evaluation of Novel Hydroxyl Substituted Chalcone Analogs with in Vitro Anti-Free Radicals Pharmacological Activity and in Vivo Anti-Oxidation Activity in a Free Radical-Injury Alzheimer’s Model. Molecules 2013, 18, 1693-1703.

AMA Style

Pan Y, Chen Y, Li Q, Yu X, Wang J, Zheng J. The Synthesis and Evaluation of Novel Hydroxyl Substituted Chalcone Analogs with in Vitro Anti-Free Radicals Pharmacological Activity and in Vivo Anti-Oxidation Activity in a Free Radical-Injury Alzheimer’s Model. Molecules. 2013; 18(2):1693-1703.

Chicago/Turabian Style

Pan, Ying; Chen, Yicun; Li, Qingnan; Yu, Xiaoyu; Wang, Jinzhi; Zheng, Jinhong. 2013. "The Synthesis and Evaluation of Novel Hydroxyl Substituted Chalcone Analogs with in Vitro Anti-Free Radicals Pharmacological Activity and in Vivo Anti-Oxidation Activity in a Free Radical-Injury Alzheimer’s Model." Molecules 18, no. 2: 1693-1703.

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