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Open AccessArticle

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

1
College of Pharmacy, Qiqihar Medical University, Qiqihar 161006, China
2
Research Institute of Medicine & Pharmacy, Qiqihar Medical University, Qiqihar 161006, China
*
Author to whom correspondence should be addressed.
Molecules 2019, 24(18), 3307; https://doi.org/10.3390/molecules24183307
Received: 12 August 2019 / Revised: 10 September 2019 / Accepted: 10 September 2019 / Published: 11 September 2019
(This article belongs to the Section Medicinal Chemistry)
Inspired by the significant bioactivity of ergosterol peroxide, we designed and synthesized four fluorescent coumarin and ergosterol peroxide conjugates 8ad 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 8ad 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. View Full-Text
Keywords: ergosterol peroxide; target probe; mitochondria; fluorescence imaging; antitumor activity ergosterol peroxide; target probe; mitochondria; fluorescence imaging; antitumor activity
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MDPI and ACS Style

Bu, M.; Li, H.; Wang, H.; Wang, J.; Lin, Y.; Ma, Y. Synthesis of Ergosterol Peroxide Conjugates as Mitochondria Targeting Probes for Enhanced Anticancer Activity. Molecules 2019, 24, 3307.

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