Manju Kumari Saroj
University of Delhi, India
Title: An experimental and theoretical Investigation of inclusion complexes of Indole Chalcones in ï¢-Cyclodextrin
Biography
Biography: Manju Kumari Saroj
Abstract
Indole chalcone (IC) derivatives form an important group of chalcones with biological activities such as anti-inflammatory, neuro-protective, anti-amoebic, anti-cancer etc. In addition, various chalcones are also recognized for their wide antimicrobial activity, and they can be employed as efficient drugs for the treatment of several diseases, like malaria or tuberculosis. Despite a variety of potential applications of chalcones in medicinal chemistry, these compounds generally have limited pharmacological uses because of low dissolution rate and bioavailability. There are multiple techniques designed to increase the solubility of a drug, including the use of micelles, liposomes, nanoparticles and nanodispersions. Among the existing techniques, the formation of inclusion complexes with encapsulating agents such as
β-cyclodextrin (b-CD), is frequently employed.
The present study focuses on the formation of inclusion complexes of IC derivatives with b-CD, which involves absorption and steady state fluorescence spectroscopies. The stoichiometries and binding constants (Kin) of these complexes have been investigated by monitoring their absorbance and fluorescence spectral profiles. The data are analyzed by Benesi-Hildebrand plots as well as Job’s method, which indicate 1:1 stoichiometry of IC:b-CD complexes. Fluorescence measurements are also used to investigate the effect of temperature on the stability of inclusion complexes. Stability of IC:b-CD complexes is significantly affected with variation in substituents on the phenyl ring and temperature. The stability of the inclusion complex observed to decreases with increase in temperature. All the experimental results and the geometrical data obtained using PM3 semiempirical method illustrate the partial inclusion of IC derivatives from the phenyl ring side in β-CD cavity. The binding process of IC derivatives with b-CD is found to be exothermic in nature and seems to be controlled by electrostatic and hydrophobic forces.