1. Academic Validation
  2. Total Synthesis, Discovery and Biological Evaluation of Daldinin A Derivatives for Improving Hyperglycemia-Induced Endothelial Cell Death

Total Synthesis, Discovery and Biological Evaluation of Daldinin A Derivatives for Improving Hyperglycemia-Induced Endothelial Cell Death

  • Chem Pharm Bull (Tokyo). 2021;69(8):760-767. doi: 10.1248/cpb.c21-00211.
Qianqian Sun 1 Shuyu Hu 1 Yu Song 1 Runqing Zhu 1 Luohao Li 1 Jing Li 1 Tao Zhang 1 Qinghe Gao 1 Yakun Wang 1 Lizhen Fang 1
Affiliations

Affiliation

  • 1 School of Pharmacy, Xinxiang Medical University.
Abstract

Daldinins are a novel type of naturally occurring tricyclic heterocycles isolated from Daldinia concentrica. In this study, four daldinin A derivatives with different alkyl side chains were synthesized using the same synthetic protocol. Bioactivity tests first indicated that the daldinin A derivatives showed significant protection for endothelial cells against damage caused by high glucose. The derivative compound with three carbon atoms on the alkyl side exhibited the best effect.

Keywords

bioactivity; daldinin; endothelial cell; natural product derivative; total synthesis.

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