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Cytotoxicity and inhibition of lipid peroxidation activity of resveratrol/cyclodextrin inclusion complexes

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Abstract

Resveratrol (Res) is a plant-based polyphenol compound and is known to inhibit the growth of a variety of cancer cells and protect lipoproteins against oxidative damage. However the poor solubility and labile property may constitute a serious problem for its bioavailability. The problem could be overcome by the formation of inclusion complexes with cyclodextrins (CDs). The aim of this work is to include Res by β-cyclodextrin (β-CD) and 2-hydroxypropyl-β-cyclodextrin (HP-CD) to form the Res/β-CD and Res/HP-CD inclusion complexes and evaluate their cytotoxicity on cancer cells and inhibition of lipid peroxidation activity. The complexes are characterized by powder X-ray diffraction, fourier transform infrared spectroscopy and scanning electron microscopy. The cytotoxicity of the two complexes has been evaluated by methylthiazoletetrazolium reduction assay on two cancer cell lines (cervical carcinoma cells HeLa and hepatocellular liver cancer cells Hep3B) and one normal cell line (umbililical vein endothelial cell HUVEC). The results showed that the two complexes exhibit high cytotoxicity on two cancer cells, especially for Hep3B, and show no significant effect on normal cells. The Res/HP-CD complex shows higher cytotoxicity on the two cancer cells than that of the Res/β-CD complex. The inhibition of lipid peroxidation induced by Fe2+/ascorbate of the two inclusion complexes has been determined by thiobarbituric acid assay. The inhibition rate shows a linear increase with the increase of CDs concentration, and the Res/HP-CD complex shows stronger inhibition activity than that of the Res/β-CD complex. The results of this work indicate a potential for using the Res/CD complexes to inhibit human cancer growth and lipoproteins peroxidation.

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Acknowledgments

This work was supported by the Excellent Youth Foundation of Hubei National Science Foundation (2009CDA075), the Open Research Fund of Key Laboratory of Monitoring and Control of Tropical Agricultural and Forest Invasive Alien Pests, Ministry of Agriculture (MACKL1006) and the Open Research Fund of Hubei Novel Reactor & Green Chemical Technology Key Laboratory (RGCT201004).

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Correspondence to Rong Chen.

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Lu, Z., Chen, R., Fu, R. et al. Cytotoxicity and inhibition of lipid peroxidation activity of resveratrol/cyclodextrin inclusion complexes. J Incl Phenom Macrocycl Chem 73, 313–320 (2012). https://doi.org/10.1007/s10847-011-0058-8

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  • DOI: https://doi.org/10.1007/s10847-011-0058-8

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