Cholesterol-stabilized membrane-active nanopores with anticancer activities

Jie Shen, Yongting Gu, Lingjie Ke, Qiuping Zhang, Yin Cao, Yuchao Lin, Zhen Wu, Caisheng Wu, Yuguang Mu, Yun-Long Wu, Changliang Ren () and Huaqiang Zeng ()
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Jie Shen: Xiamen University
Yongting Gu: Xiamen University
Lingjie Ke: Xiamen University
Qiuping Zhang: Xiamen University
Yin Cao: Xiamen University
Yuchao Lin: Xiamen University
Zhen Wu: Xiamen University
Caisheng Wu: Xiamen University
Yuguang Mu: Nanyang Technological University
Yun-Long Wu: Xiamen University
Changliang Ren: Xiamen University
Huaqiang Zeng: Fuzhou University

Nature Communications, 2022, vol. 13, issue 1, 1-10

Abstract: Abstract Cholesterol-enhanced pore formation is one evolutionary means cholesterol-free bacterial cells utilize to specifically target cholesterol-rich eukaryotic cells, thus escaping the toxicity these membrane-lytic pores might have brought onto themselves. Here, we present a class of artificial cholesterol-dependent nanopores, manifesting nanopore formation sensitivity, up-regulated by cholesterol of up to 50 mol% (relative to the lipid molecules). The high modularity in the amphiphilic molecular backbone enables a facile tuning of pore size and consequently channel activity. Possessing a nano-sized cavity of ~ 1.6 nm in diameter, our most active channel Ch-C1 can transport nanometer-sized molecules as large as 5(6)-carboxyfluorescein and display potent anticancer activity (IC50 = 3.8 µM) toward human hepatocellular carcinomas, with high selectivity index values of 12.5 and >130 against normal human liver and kidney cells, respectively.

Date: 2022
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DOI: 10.1038/s41467-022-33639-5

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