1. Academic Validation
  2. Synthesis of phthalide derivatives and evaluation on their antiplatelet aggregation and antioxidant activities

Synthesis of phthalide derivatives and evaluation on their antiplatelet aggregation and antioxidant activities

  • J Asian Nat Prod Res. 2020 Dec;22(12):1176-1187. doi: 10.1080/10286020.2019.1681982.
Xin Fang 1 Qiang Ma 1 Kai-Xia Zhang 2 Song-Yun Yao 2 Yi Feng 1 Yong-Sheng Jin 2 Shuang Liang 1
Affiliations

Affiliations

  • 1 Innovation Research Institute of Traditional Chinese Medicine, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.
  • 2 School of Pharmacy, Second Military Medical University, Shanghai 200433, China.
Abstract

As part of our continuing efforts to discover structurally interesting bioactive phthalide derivatives, 23 of them with a structure incorporating thiophen or halogens were designed and synthesized, 17 of which are previously unreported. In vitro antiplatelet aggregation activity screening showed that 14b could significantly inhibit platelet aggregation induced by arachidonic acid, compared with edaravone (p < 0.01). Meanwhile, oxidative damage models using SH-SY5Y and PC12 cells induced by H2O2 were built to evaluate the antioxidant activity of the phthalide derivatives. In SH-SY5Y cells, compared with aspirin, 1a significantly increased the relative cell survival rate (p < 0.05). Compared with edaravone, 1a (p < 0.01) and 15b (p < 0.05) significantly increased the relative cell survival rate. In PC12 cells, 1a (p < 0.01), 15b (p < 0.01), and 12a (p < 0.05) remarkably increased the cell survival rate compared with edaravone. The present study identified lead structures to develop potential anti-ischemic stroke agents.

Keywords

Phthalide derivative; antioxidation; antiplatelet aggregation.

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