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Int. J. Mol. Sci. 2012, 13(11), 14992-15011; doi:10.3390/ijms131114992
Article

Betulin Complex in γ-Cyclodextrin Derivatives: Properties and Antineoplasic Activities in In Vitro and In Vivo Tumor Models

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Received: 24 August 2012 / Revised: 23 October 2012 / Accepted: 24 October 2012 / Published: 15 November 2012
(This article belongs to the Section Biochemistry, Molecular Biology and Biophysics)
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Abstract

Given the present high incidence of melanoma and skin cancer, interest in potential drugs of plant origin has increased significantly. Pentacyclic lupane-type triterpenes are widely distributed in plants, offering numerous pharmacological benefits. Betulin is an important compound in the bark of Betula pendula Roth and has important therapeutic properties, including antitumor activities. Its biological effect is limited by its poor water solubility, which can be improved by cyclodextrin complexation. The best results have been obtained by using a novel cyclodextrin derivative, octakis-[6-deoxy-6-(2-sulfanyl ethanesulfonate)]-γ-CD. The complexes between betulin and the previously mentioned cyclodextrin were analyzed by scanning electron microscopy (SEM)and differential scanning calorimetry (DSC) and pharmacologically evaluated in vitro (MTT and immunocytochemistry tests) and in vivo in C57BL/6J mice. The solubility of betulin is improved by cyclodextrin complexation, which creates a stable complex that improves the in vitro and in vivo properties of the active compound.
Keywords: melanoma; betulin; cyclodextrin; MTT; immunocytochemistry; C57BL/6J mice; antitumor activity melanoma; betulin; cyclodextrin; MTT; immunocytochemistry; C57BL/6J mice; antitumor activity
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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Şoica, C.; Dehelean, C.; Danciu, C.; Wang, H.M.; Wenz, G.; Ambrus, R.; Bojin, F.; Anghel, M. Betulin Complex in γ-Cyclodextrin Derivatives: Properties and Antineoplasic Activities in In Vitro and In Vivo Tumor Models. Int. J. Mol. Sci. 2012, 13, 14992-15011.

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