Betulin complex in γ-cyclodextrin derivatives: properties and antineoplasic activities in in vitro and in vivo tumor models.

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.

• Authors: Codruta Soica, Cristina Dehelean, Corina Danciu, Hai Ming Wang, Gerhard Wenz, Rita Ambrus, Florina Bojin, Mariana Anghel
• Journal: International journal of molecular sciences (Int J Mol Sci) Vol. 13 Issue 11 Pg. 14992-5011 (Nov 15 2012) ISSN: 1422-0067 [Electronic] Switzerland
• PMID: 23203108 (Publication Type: Journal Article)

Chemical References

• Antineoplastic Agents
• Drug Combinations
• Triterpenes
• gamma-Cyclodextrins
• betulin
• Caspase 2

Topics

• Animals
• Antineoplastic Agents (chemistry, pharmacology, toxicity)
• Calorimetry, Differential Scanning
• Caspase 2 (genetics, metabolism)
• Cell Line, Tumor
• Cell Survival (drug effects)
• Disease Models, Animal
• Drug Combinations
• Flow Cytometry
• Gene Expression
• Immunohistochemistry
• Male
• Melanoma (drug therapy, genetics, metabolism, pathology)
• Mice
• Triterpenes (chemistry, pharmacology)
• Tumor Burden (drug effects)
• Xenograft Model Antitumor Assays
• gamma-Cyclodextrins (chemistry, pharmacology, toxicity)