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Int. J. Mol. Sci. 2014, 15(5), 8235-8255; doi:10.3390/ijms15058235

Betulinic Acid in Complex with a Gamma-Cyclodextrin Derivative Decreases Proliferation and in Vivo Tumor Development of Non-Metastatic and Metastatic B164A5 Cells

1
Faculty of Pharmacy, Victor Babeş University of Medicine and Pharmacy, 2 EftimieMurgu, 300041 Timisoara, Romania
2
Institute of Pharmaceutical Technology, University of Szeged, 6 Eotvos Ut., H-6720 Szeged, Hungary
3
Department of Pharmacodynamics and Biopharmacy, University of Szeged, 6 Eotvos Str., H-6720 Szeged, Hungary
4
Faculty of Medicine, Victor Babeş University of Medicine and Pharmacy, 2 EftimieMurgu, 300041 Timisoara, Romania
5
Faculty of Medicine, Vasile Goldis University, 310045 Arad, Romania
*
Authors to whom correspondence should be addressed.
Received: 4 January 2014 / Revised: 8 April 2014 / Accepted: 10 April 2014 / Published: 9 May 2014
(This article belongs to the Section Biochemistry, Molecular and Cellular Biology)
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Abstract

Betulinic acid, a very promising anti-melanoma agent, has very low water solubility that causes low bioavailability. To overcome this inconvenience, a highly water-soluble cyclodextrin was used (octakis-[6-deoxy-6-(2-sulfanyl ethanesulfonic acid)]-γ-cyclodextrin). The complex was physico-chemically analyzed using differential scanning calorimetry (DSC), X-ray and scanning electron microscopy (SEM) methods and then in vitro tested for its antiproliferative activity by the MTT assay and by cell cycle analysis. Finally, the complex was tested in vivo using an animal model of murine melanoma developed in C57BL/6J mice, where it caused a reduction in tumor volume and weight. The study revealed the beneficial influence of betulinic acid inclusion into the cyclodextrin in terms of antiproliferative activity and in vivo tumor development. View Full-Text
Keywords: betulinic acid; DSC; X-ray diffraction; SEM; MTT test; C57BL/6J mice betulinic acid; DSC; X-ray diffraction; SEM; MTT test; C57BL/6J mice
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MDPI and ACS Style

Soica, C.; Danciu, C.; Savoiu-Balint, G.; Borcan, F.; Ambrus, R.; Zupko, I.; Bojin, F.; Coricovac, D.; Ciurlea, S.; Avram, S.; Dehelean, C.A.; Olariu, T.; Matusz, P. Betulinic Acid in Complex with a Gamma-Cyclodextrin Derivative Decreases Proliferation and in Vivo Tumor Development of Non-Metastatic and Metastatic B164A5 Cells. Int. J. Mol. Sci. 2014, 15, 8235-8255.

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