Soica Codruţa, Oprean Camelia, Borcan Florin, Danciu Corina, Trandafirescu Cristina, Coricovac Dorina, Crăiniceanu Zorin, Dehelean Cristina Adriana, Munteanu Melania
Faculty of Pharmacy, Victor Babeş University of Medicine and Pharmacy, 2nd Eftimie Murgu Sq., Timişoara 300041, Romania.
Faculty of Medicine, Victor Babeş University of Medicine and Pharmacy, 2nd Eftimie Murgu Sq., Timişoara 300041, Romania.
Molecules. 2014 Apr 17;19(4):4924-40. doi: 10.3390/molecules19044924.
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.
齐墩果酸和熊果酸是具有五环类胆固醇样结构的天然三萜化合物，这使得它们的水溶性极低，在生物利用度方面是一个显著的缺点。我们之前报道了这些酸与环糊精之间包合物的合成，以及它们在化学诱导的皮肤癌实验模型上的体内评估。在本研究中，使用体外试验和体内皮肤癌模型监测了包含在羟丙基 -γ-环糊精（HPGCD）中的酸混合物的协同活性。药物相互作用系数（CDI）用于将相互作用表征为协同作用、相加作用或拮抗作用。我们的结果表明，两种三萜酸的混合物无论是单一形式还是与环糊精形成复合物，其抗肿瘤活性均有所增强，从而证明了它们具有互补的生物学活性。
