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https://doi.org/10.37358/Rev.Chim.1949

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Revista de Chimie (Rev. Chim.), Year 2008, Volume 59, Issue 8,

https://doi.org/10.37358/RC.08.8.1912

Cristina A. Dehelean, Codruţa Soica, Camelia Peev, Alexandra T. Gruia, Edward Seclaman

Physico-chemical and Molecular Analysis of Antitumoral Pentacyclic Triterpenes in Complexation with Gamma-cyclodextrin

Abstract:

Pentacyclic triterpens determine anticancer, anti-inflammatory and antiviral activity. The major problem of this type of triterpens is their low water solubility which can be increased by cyclodextrin complexation. The aim of present study was to analyze the products between pentacyclic triterpens (betulinic acid, betulin) and g-cyclodextrin (GCD). GCD is a natural cyclodextrin with 8 units of glucopyranose, obtained by enzymatic degradation of amylose; it is used as host-molecule for the accommodation of large molecules like steroids, spironolactone, triterpenes. In order to obtain the inclusion complexes of pentacyclic triterpenes with GCD, 1:2 molar ratio and two preparation methods (physical mixing, kneading) were used. The inclusion complexes were analyzed by in vitro dissolution tests and X-ray diffraction. The molecules of the two components were analyzed by computational chemistry to see if they are sterically compatible.
Keywords:
GCD; betulinic acid; betulin; inclusion complexation; solubility

Issue: 2008, Volume 59, Issue 8
Pages:
Publication date: 2008/9/9
https://doi.org/10.37358/RC.08.8.1912
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