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.

Highlights

  • Free radicals have been implicated in the etiology of several human diseases, as well as ageing

  • Hydroxyl-substituted chalcone analogs could develop into novel anti-Alzheimer’s disease (AD) drug candidates

  • A growing body of evidence indicates that increased oxidative stress resulting from free radical damage to cellular functions is associated with a number of age-related disorders including atherosclerosis and arthritis

Read more

Summary

Introduction

Free radicals have been implicated in the etiology of several human diseases, as well as ageing. A growing body of evidence suggests that AD pathogenesis involves an imbalance between free radical formation and destruction [4,5,6,7,8]. This concept originally derived from the free radical hypothesis of aging, with age-related accumulation of free radicals resulting in damaged cell components. C1–7shown in Table 1 and screened these potential compounds for anti-free radical activity in vitro for further study. We test the compounds’ effect on SOD, MDA and GSH-PX levels to evaluate the anti-oxidation activity in vivo in a free radical-injury Alzheimer’s model

Synthesis of C1–7
Activity of C1–7 in Scavenging DPPH and OH Free Radicals
Chemistry
Tests of Activity of C1–7 in Scavenging DPPH-free Radicals
Tests of Activity of C1–7 in Scavenging OH Free Radicals
Conclusions

Talk to us

Join us for a 30 min session where you can share your feedback and ask us any queries you have

Schedule a call

Disclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.