Journal
MATERIALS SCIENCE & ENGINEERING C-MATERIALS FOR BIOLOGICAL APPLICATIONS
Volume 69, Issue -, Pages 68-76Publisher
ELSEVIER SCIENCE BV
DOI: 10.1016/j.msec.2016.05.022
Keywords
Oleanolic acid; Amino-appended beta-cyclodextrin; Inclusion complex; Binding behavior; Water solubility; Anticancer activity
Categories
Funding
- National Natural Science Foundation of China (NNSFC) [21362016, 81260501]
- Ministry of Education of P.R. China [201410674009]
Ask authors/readers for more resources
Oleanolic acid (OA) is a pentacydic triterpenoid acid of natural abundance in plants which possesses important biological activities. However, its medicinal applications were severely impeded by the poor water solubility and resultan low bioavailability and potency. In this work, studies on solid inclusion complexes of OA with a series of amino-appended beta-cyclodextrins (ACDs) were conducted in order to address this issue. These complexes were prepared by suspension method and were well characterized by NMR, SEM, XRD, TG, DSC and Zeta potential measurement. The 2:1 inclusion mode of ACDs/OA complexes was elucidated by elaborate 2D NMR (ROESY). Besides, water solubility of OA was dramatically promoted by inclusion complexation with ACDs. Moreover, in vitro anticancer activities of OA against human cancer cell lines HepG2, HT29 and HCT116 were significantly enhanced after formation of inclusion complexes, while the apoptotic response results indicated their induction of apoptosis of cancer cells. This could provide a novel approach to development of novel pharmaceutical formulations of OA. (C) 2016 Elsevier B.V. All rights reserved.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available