The Synergistic Biologic Activity of Oleanolic and Ursolic Acids in Complex with Hydroxypropyl-γ-Cyclodextrin

Molecules

Codruᘺ Soica²  Camelia Oprean²  Florin Borcan²  Corina Danciu²  Cristina Trandafirescu²  Dorina Coricovac²  Zorin Crăiniceanu¹  Cristina Adriana Dehelean² 

[1]Faculty of Medicine, Victor Babeş University of Medicine and Pharmacy, 2nd Eftimie Murgu Sq., Timişoara 300041, Romania

[2]Faculty of Pharmacy, Victor Babeş University of Medicine and Pharmacy, 2nd Eftimie Murgu Sq., Timişoara 300041, Romania

[3] E-Mails:

关键词: oleanolic acid;    ursolic acid;    cyclodextrin;    DMBA;    TPA;    mouse model;    synergism;   

DOI  :  10.3390/molecules19044924

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
© 2014 by the authors; licensee MDPI, Basel, Switzerland.