1. Academic Validation
  2. Polyphosphoric acid-promoted one-pot synthesis and neuroprotective effects of flavanones against NMDA-induced injury in PC12 cells

Polyphosphoric acid-promoted one-pot synthesis and neuroprotective effects of flavanones against NMDA-induced injury in PC12 cells

  • RSC Adv. 2022 Oct 3;12(43):28098-28103. doi: 10.1039/d2ra03562f.
Enhua Wang 1 Lishou Yang 2 3 Qian Yang 1 Fanghong Yang 1 Ji Luo 1 Menglan Gan 1 Xue Wang 1 Shanmin Song 1 Yang Lei 1 Xiaosheng Yang 2 3
Affiliations

Affiliations

  • 1 Department of Food and Medicine, Guizhou Vocational College of Agriculture Qingzhen 551400 P. R. China 515538011@qq.com.
  • 2 State Key Laboratory of Functions and Applications of Medicinal Plants, Guizhou Medical University Guiyang 550014 P. R. China gzcnp@sina.cn.
  • 3 The Key Laboratory of Chemistry for Natural Products of Guizhou Province and Chinese Academy of Sciences Guiyang 550014 P. R. China.
Abstract

We report herein an efficient polyphosphoric acid (PPA) promoted one-pot protocol for the synthesis of flavanone derivatives from 2-hydroxyacetophenones and benzaldehydes. A variety of flavanones were produced in moderate to excellent yields and evaluated for their neuroprotective effects against N-methyl-d-aspartate (NMDA)-induced excitotoxicity in PC12 cells. Derivatives bearing electron-donating groups exhibited better neuroprotective activity. Compound 3m demonstrated the best protective potency and reversed the intracellular calcium (CA2+) influx caused by NMDA, suggesting that flavanones protected the PC12 cells against NMDA-induced neurotoxicity via inhibition of CA2+ overload.

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