scholarly journals Enantioselective Study on the Biodegradation of Verapamil and Cytalopram by Chiral Capillary Electrophoresis

Separations ◽  
2021 ◽  
Vol 8 (3) ◽  
pp. 29
Author(s):  
Yolanda Martín-Biosca ◽  
Laura Escuder-Gilabert ◽  
Salvador Sagrado ◽  
María José Medina-Hernández

Many of the currently available drugs are chiral compounds that are marketed as racemates or, to a lesser extent, in the form of one of the enantiomers since a pair of enantiomers may have different toxicological and ecotoxicological properties compared to each other. The evaluation of enantioselectivity in biodegradation processes is essential for environmental risk assessment. The objective of this research is to study the enantioselectivity in the biodegradation of two common chiral drugs, citalopram and verapamil, using highly sulphated-γ-cyclodextrin (HS-γ-CD) as chiral selector in Capillary Electrophoresis. Biodegradation experiments were performed in batch mode using a minimal salt medium inoculated with an activated sludge and supplemented with the corresponding enantiomeric mixture. The cultures were incubated at 20 °C for 28 days. Abiotic degradation of verapamil and citalopram enantiomers was also assessed. The concentration of the enantiomers of verapamil and citalopram were monitored using 0.7% and 0.1% m/v HS-γ-CD solutions as chiral selector, respectively. Separations were carried out using the complete filling technique. The results of biodegradability tests indicate that citalopram could be considered potentially persistent while verapamil is presumed to be a non-persistent compound. No evidence of enantioselectivity was observed in any of the biodegradation processes.

2013 ◽  
Author(s):  
◽  
Myalowenkosi Innocent Sabela

The present work involves the interaction studies of chiral compounds with the Human Serum Albumin (HSA) protein using computational and experimental methods. The HSA protein has multiple binding sites that forms the basis for its exceptional ability to interact with many organic and inorganic molecules, which makes this protein an important regulator of intercellular fluxes and the pharmacokinetic behaviour of many drugs. This study was undertaken to evaluate the related pharmacokinetic and enantioselective binding parameters of the racemic catechin enantiomers with the HSA. Accordingly, this work involved a method development for the chiral separation of a racemic compound, by capillary electrophoresis-electrokinetic chromatography (CE-EKC) with a highly sulphated beta-cyclodextrin (HS--CD) as a chiral selector. The experimental work was supported by two molecular docking studies. The first included the mimicking of the host-guest interactions between a chiral selector and an enantiomeric compound. The second study included the estimation of the pseudo enantioselective (ES) binding of catechin to HSA. Overall, it was found that CE-EKC is the preferred method for the(±)-catechin binding to HSA protein evaluation. Moreover, the technique used in this work is not restricted to HSA or polyphenols, but can also be applied to other proteins and ligands that possess chirality. Furthermore, the molecular docking approaches also proved to be very useful for the evaluation of chiral recognition systems and for elucidation of the ligand-protein interactions.


2020 ◽  
Vol 44 (3) ◽  
pp. 958-972 ◽  
Author(s):  
Yu Zhao ◽  
Jinlong Wang ◽  
Yanru Liu ◽  
Zhen Jiang ◽  
Yongbo Song ◽  
...  

In this study, carboxymethyl-6-(4-methoxybenzylamino)-β-cyclodextrin (CMCDPN) was synthesized for the first time and managed to be used as a chiral selector to enantioseparate 13 kinds of chiral drugs by capillary electrophoresis.


2014 ◽  
Vol 36 (2) ◽  
pp. 305-311 ◽  
Author(s):  
Hadi Tabani ◽  
Mojtaba Mahyari ◽  
Ali Sahragard ◽  
Ali Reza Fakhari ◽  
Ahmad Shaabani

1998 ◽  
Vol 800 (1) ◽  
pp. 69-76 ◽  
Author(s):  
Salvatore Fanali ◽  
Claudia Desiderio ◽  
Georg Schulte ◽  
Stefan Heitmeier ◽  
Dirk Strickmann ◽  
...  

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