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In Silico and Experimental Studies of Concanavalin A: Insights into Its Antiproliferative Activity and Apoptotic Mechanism

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Abstract

Concanavalin A (ConA), a mannose/glucose-binding legume lectin, has been reported to induce tumor cell death via a mitochondria-mediated autophagic pathway; however, the precise mechanism by which induces cell death remains to be discovered. In this study, we simulated the three-dimensional structure of ConA monomer, its dimer, and tetramer forms and reported its molecular dynamics simulations and phylogenetic analysis. Subsequently, we showed that ConA possessed remarkable antiproliferative effects on HepG2 cells. Further data showed that there was a link among its hemagglutinating, sugar-binding, and antiproliferative activities. In addition, we found that ConA induced apoptosis in HepG2 cells. Then, we demonstrated that the treatment of ConA caused mitochondrial transmembrane potential (MMP) collapse, cytochrome c release, and activation of caspase. In conclusion, we demonstrate that there is a positive correlation between carbohydrate-binding activity and antiproliferative activity of ConA. In addition, we confirm that ConA induces HepG2 cell death through a mitochondrial apoptotic pathway.

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Acknowledgment

We thank Dr. Hao Peng (Sichuan University) for his critical review of this manuscript.

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  1. College of Life Sciences, Sichuan University, Chengdu, 610064, China

    Zhongyu Liu, Xufeng Li, Xianping Ding & Yi Yang

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  1. Zhongyu Liu
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  2. Xufeng Li
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  3. Xianping Ding
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  4. Yi Yang
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Correspondence to Zhongyu Liu or Yi Yang.

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Liu, Z., Li, X., Ding, X. et al. In Silico and Experimental Studies of Concanavalin A: Insights into Its Antiproliferative Activity and Apoptotic Mechanism. Appl Biochem Biotechnol 162, 134–145 (2010). https://doi.org/10.1007/s12010-009-8694-9

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  • DOI: https://doi.org/10.1007/s12010-009-8694-9

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