alexa Abstract | Synthesis and characterization of cephradine metal complexes as Alzheimer disease therapeutic agent: An in vitro kinetic study on acetyl cholinesterase and monoamine oxidase

Journal of Chemical and Pharmaceutical Research
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Cephradine metal complexes with Cr(III), Mn(II), Fe(III), Co(II), Cu(II), Zn(II), Cd(II), Hg(II) , mixed metals (Fe,Co) and (Fe,Cu) were synthesized and characterized by physicochemical and spectroscopic methods. Inhibitions of acetylcholinesterase, monoamine oxidase (MAO-B&A) by the prepared complexes were investigated. The brain AChE and MAO-A & B from Egyptian Mediterranean buffalo (Bas Buballus) was purified by ammonium sulphate precipitation and Sephadex G-25. The effect of the metallo cephradine on the activity of pure AChE and also (MAOB& A) were carried out in vitro by using standard colorimetric assays. The results revealed that AChE was inhibited by manganese and copper cephradine complexes in 1:1 and 3:1 (M:L) molar ratio, respectively as uncompetitive inhibitors with an enzyme-inhibitor dissociation constant (Ki value) of 21.75and 11.72 μmol/min/mg/protein and IC50 equals to 5.78 and 20 μM ,respectively. Also, the inhibition of MAO-B &A was tested for synthesized cephradine metal complexes. The mixed metal (Fe,Cu) cephradine complex is the best inhibitor for MAO-B as uncompetitive inhibitor. Enzyme-inhibitor dissociation constant (Ki value) and IC50 were 36.61μmol/min/mg/protein and 80.69 μM, respectively. From this study, it was found that Mn(II) in 1:1 and Cu(II) in 3:1 (M:L) molar ratio cephradine complexes act as potent inhibitors for AChE, while, the mixed metal (Fe,Cu) cephradine complex was a potent inhibitor for MAO-B. So, these three metallocephradine can be used for preventing neurodegenerative diseases such as Alzheimer΄s disease

Author(s): Mamdouh S Masouda Alaa E AliDoaa A Ghareeb and Nessma M Nasr


Cephradine, Metal complexes, AChE, MAO, Alzheimer disease, cephradine metal complexes

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