2. Academic Validation
  3. Synthesis of Ergosterol Peroxide Conjugates as Mitochondria Targeting Probes for Enhanced Anticancer Activity

Synthesis of Ergosterol Peroxide Conjugates as Mitochondria Targeting Probes for Enhanced Anticancer Activity

  • Molecules. 2019 Sep 11;24(18):3307. doi: 10.3390/molecules24183307.
Ming Bu 1,  Hongling Li 2,  Haijun Wang 3,  Jing Wang 4,  Yu Lin 5,  Yukun Ma 6
Affiliations

Affiliations

  • 1 College of Pharmacy, Qiqihar Medical University, Qiqihar 161006, China. [email protected].
  • 2 College of Pharmacy, Qiqihar Medical University, Qiqihar 161006, China. [email protected].
  • 3 College of Pharmacy, Qiqihar Medical University, Qiqihar 161006, China. [email protected].
  • 4 College of Pharmacy, Qiqihar Medical University, Qiqihar 161006, China. [email protected].
  • 5 College of Pharmacy, Qiqihar Medical University, Qiqihar 161006, China. [email protected].
  • 6 Research Institute of Medicine & Pharmacy, Qiqihar Medical University, Qiqihar 161006, China. [email protected].
PMID: 31514398 DOI: 10.3390/molecules24183307
Abstract

Inspired by the significant bioactivity of ergosterol peroxide, we designed and synthesized four fluorescent coumarin and ergosterol peroxide conjugates 8a-d through the combination of ergosterol peroxide with 7-N,N-diethylamino Coumarins fluorophore. The cytotoxicity of synthesized conjugates against three human Cancer cells (HepG2, SK-Hep1, and MCF-7) was evaluated. The results of fluorescent imaging showed that the synthesized conjugates 8a-d localized and enriched mainly in mitochondria, leading to significantly enhanced cytotoxicity over ergosterol peroxide. Furthermore, the results of biological functions of 8d showed that it could suppress cell colony formation, invasion, and migration; induce G2/M phase arrest of HepG2 cells, and increase the intracellular ROS level.

Keywords

antitumor activity; ergosterol peroxide; fluorescence imaging; mitochondria; target probe.

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