A study of host-guest complexation between amodiaquine and native cyclodextrin. Characterization in solid state and its in-vitro anticancer activity

作者：Murugan Moorthiraman; Sivakumar Krishnamoorthy; Rajamohan Rajaram^*

来源：Journal of Macromolecular Science, Part A: Pure and Applied Chemistry , 2016, 53(5): 282-289.

DOI：10.1080/10601325.2016.1151646

• XRD
• in vitro anticancer activity
• beta-cyclodextrin
• Amodiaquine
• Patch-Dock server
• inclusion complex

Amodiaquine (AQ) has been used widely as an antimalarial drug. Amodiaquine is a mannich base 4-amino quinolone with a mode of action similar to that of chloroquine. The inclusion complex of AQ with beta-Cyclodextrin (beta-CD) in solution phase is studied from the ground and excited state with UV-Visible and fluorescence spectroscopy, respectively. A binding constant and stoichiometric ratio between AQ and beta-CD are calculated by BH equation. The solid complexes are prepared by physical method (PM), kneading method (KM) and co-precipitation method (CP). The solid complex is characterized by Fourier transform infrared spectroscopy, scanning electron microscopy and powder X-ray diffraction. The CP method gives the solid product with a better yield than that of physical mixture and KM products. The orientation and structure of the complex are proposed based on the analysis of Patch-Dock server. The anticancer activity also performed for pure AQ and their complex with beta-CD. It is clearly shown that an improvement of anticancer activity of AQ while forming complex with beta-CD. The solid inclusion complex behaves as the better anticancer ability than AQ alone.

• 出版日期2016-5-3