2. Academic Validation
  3. Semisynthesis of novel magnolol-based Mannich base derivatives that suppress cancer cells via inducing autophagy

Semisynthesis of novel magnolol-based Mannich base derivatives that suppress cancer cells via inducing autophagy

  • Eur J Med Chem. 2020 Nov 1;205:112663. doi: 10.1016/j.ejmech.2020.112663.
Ting Xu 1,  Zhiyuan Zheng 1,  Yong Guo 2,  Li-Ping Bai 3
Affiliations

Affiliations

  • 1 State Key Laboratory of Quality Research in Chinese Medicine, Macau Institute for Applied Research in Medicine and Health, Macau University of Science and Technology, Taipa, Macau, China.
  • 2 State Key Laboratory of Quality Research in Chinese Medicine, Macau Institute for Applied Research in Medicine and Health, Macau University of Science and Technology, Taipa, Macau, China; School of Pharmaceutical Sciences, Key Laboratory of Advanced Drug Preparation Technologies, Ministry of Education, Zhengzhou University, Zhengzhou, 450001, Henan Province, China. Electronic address: guoyong_122@zzu.edu.cn.
  • 3 State Key Laboratory of Quality Research in Chinese Medicine, Macau Institute for Applied Research in Medicine and Health, Macau University of Science and Technology, Taipa, Macau, China; Guangdong-Hong Kong-Macao Joint Laboratory of Respiratory Infectious Disease, Macau University of Science and Technology, China. Electronic address: lpbai@must.edu.mo.
PMID: 32791403 DOI: 10.1016/j.ejmech.2020.112663
Abstract

Magnolol, a natural bioactive neolignan, was found in the bark of a traditional Chinese medicine Magnoliae officinalis ("Hou Po" in Chinese). In this study, thrity-two magnolol-based Mannich base derivatives 3a-p and 4a-p were synthesized, and evaluated for their anti-proliferative activities against a panel of human tumor cell lines (T47D, MCF-7, Hela and A549). Among all derivatives, compound 3p displayed the most potent antiproliferative activity against T47D, MCF-7 and Hela cell lines with IC50 values of 0.91, 3.32 and 1.71 μM, respectively. Compared with the parental magnolol and the positive drug cisplatin, 3p exhibited up to 76.1-fold and 10.3-fold enhancement of cytotoxic effect on T47D Cancer cells, respectively. Mechanism study revealed that the most potent derivative 3p suppressed Cancer cells via inducing Autophagy. Moreover, 3p also possessed suppressive effects on migration of T47D and Hela Cancer cells. In addition, some interesting structure-activity relationships (SARs) were also summarized.

Keywords

Anti-cancer; Autophagy; Magnolol derivative; Mannich base; Semisynthesis.

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