2. Academic Validation
  3. Synthesis of novel 1-phenyl-benzopyrrolizidin-3-one derivatives and evaluation of their cytoneuroprotective effects against NMDA-induced injury in PC12 cells

Synthesis of novel 1-phenyl-benzopyrrolizidin-3-one derivatives and evaluation of their cytoneuroprotective effects against NMDA-induced injury in PC12 cells

  • Bioorg Med Chem. 2022 Apr 1;59:116675. doi: 10.1016/j.bmc.2022.116675.
Lishou Yang 1,  Qian Yang 2,  Enhua Wang 2,  Juan Yang 1,  Qiji Li 1,  Jiafu Cao 1,  Li Wang 1,  Xiu Liao 1,  Yan Yang 1,  Xiaosheng Yang 3
Affiliations

Affiliations

  • 1 State Key Laboratory of Functions and Applications of Medicinal Plants, Guizhou Medical University, Guiyang 550014, PR China; The Key Laboratory of Chemistry for Natural Products of Guizhou Province and Chinese Academy of Sciences, Guiyang 550014, PR China.
  • 2 Department of Medicine and Food, Guizhou Vocational College of Agriculture, Guiyang 550041, PR China.
  • 3 State Key Laboratory of Functions and Applications of Medicinal Plants, Guizhou Medical University, Guiyang 550014, PR China; The Key Laboratory of Chemistry for Natural Products of Guizhou Province and Chinese Academy of Sciences, Guiyang 550014, PR China. Electronic address: gzcnp@sina.cn.
PMID: 35202968 DOI: 10.1016/j.bmc.2022.116675
Abstract

A range of novel 1-phenyl-benzopyrrolizidin-3-one derivatives were synthesized and evaluated for neuroprotective effects against N-methyl-ᴅ-aspartate (NMDA)-induced injury in PC12 cells. Interestingly, derivatives that 1-phenyl moiety bearing electron-donating group, especially benzyloxy, and the trans-forms exhibited better protective activity against NMDA-induced neurotoxicity. Compound 11 m demonstrated the best neuroprotective potency and shown a dose-dependent prevention. The increased intracellular calcium (Ca2+) influx caused by NMDA in PC12 cells was reversed in the case of compound 11 m pretreatment at 15 μM. These results suggested that the synthesized 1-phenyl-benzopyrrolizidin-3-one derivatives exerted neuroprotective effect on NMDA-induced excitotoxicity in PC12 cells associated with inhibition of Ca2+ overload and can be further optimized for the development of neuroprotective agents.

Keywords

1-Phenyl-benzopyrrolizidin-3-one; Excitotoxicity; N-methyl-ᴅ-aspartate; Neuroprotective effect; PC12 cells.

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