2. Academic Validation
  3. 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.
PMID: 36320275 DOI: 10.1039/d2ra03562f
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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