The synergistic biologic activity of oleanolic and ursolic acids in complex with hydroxypropyl-γ-cyclodextrin.

Abstract

Oleanolic and ursolic acids are natural triterpenic compounds with pentacyclic cholesterol-like structures which gives them very low water solubility, a significant disadvantage in terms of bioavailability. We previously reported the synthesis of inclusion complexes between these acids and cyclodextrins, as well as their in vivo evaluation on chemically induced skin cancer experimental models. In this study the synergistic activity of the acid mixture included inside hydroxypropyl-gamma-cyclodextrin (HPGCD) was monitored using in vitro tests and in vivo skin cancer models. The coefficient of drug interaction (CDI) was used to characterize the interactions as synergism, additivity or antagonism. Our results revealed an increased antitumor activity for the mixture of the two triterpenic acids, both single and in complex with cyclodextrin, thus proving their complementary biologic activities.

• Authors: Codruţa Soica, Camelia Oprean, Florin Borcan, Corina Danciu, Cristina Trandafirescu, Dorina Coricovac, Zorin Crăiniceanu, Cristina Adriana Dehelean, Melania Munteanu
• Journal: Molecules (Basel, Switzerland) (Molecules) Vol. 19 Issue 4 Pg. 4924-40 (Apr 17 2014) ISSN: 1420-3049 [Electronic] Switzerland
• PMID: 24747649 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Antineoplastic Agents, Phytogenic
• Drug Carriers
• Triterpenes
• gamma-Cyclodextrins
• hydroxypropyl-gamma-cyclodextrin
• 9,10-Dimethyl-1,2-benzanthracene
• Oleanolic Acid
• ursolic acid

Topics

• 9,10-Dimethyl-1,2-benzanthracene
• Animals
• Antineoplastic Agents, Phytogenic (pharmacokinetics, pharmacology)
• Biological Availability
• Cell Line, Tumor
• Cell Survival (drug effects)
• Drug Carriers
• Drug Synergism
• Female
• Humans
• Melanoma (chemically induced, drug therapy, pathology)
• Mice
• Oleanolic Acid (pharmacokinetics, pharmacology)
• Skin Neoplasms (chemically induced, drug therapy, pathology)
• Solubility
• Triterpenes (pharmacokinetics, pharmacology)
• Ultraviolet Rays
• gamma-Cyclodextrins (chemistry)