ABSTRACT
OBJECTIVE: The goal of the present study is to examine pretreatment with Schiff bases and derivatives of pregabalin along with their metal (Zn and Cu) complexes on the severity of epilepsy, latency time, duration of convulsions, seizure score and survival rate in mice. METHODS: To achieve the goal, a molecular docking study of analogues was carried out on a specific molecular target, such as the alpha-2δ receptor (PDB ID: 6ND9); which revealed the significant binding affinity of the analogs to their respective target. Based on the docking information, all pregabalin derivatives were synthesized and in-vivo antiepileptic effect was confirmed by applying the PTZ model that prioritized the most crucial significant points responsible for biological activity. RESULTS: The test compounds markedly increased the latency of the first seizure and reduced the frequency of seizures throughout the body and frequent spinning and jumps. Additionally, treatment with pregabalin derivatives in mice that received PTZ significantly reduced the duration of seizures and seizure score. However, it increased the survival rate of the mice. DISCUSSION: Since the newly synthesized compounds were more active as compared to the parent drug in some respects; therefore, the expansion of the project can be planned to explore clinical side of the drugs in the future.
Docking studies of Schiff bases and derivatives of Pregabalin along with their Zn and Cu metal complexesPretreatment with Schiff bases and derivatives of pregabalin along with their metal (Zn and Cu)PTZ Model of epilepsyObservation of different parameters including; the severity of epilepsy, latency time, duration of convulsions, seizure score and survival rate in miceNewly synthesized compounds were more active as compared to the parent drug.
Subject(s)
Anticonvulsants , Epilepsy , Mice , Animals , Anticonvulsants/pharmacology , Anticonvulsants/therapeutic use , Pregabalin/pharmacology , Pregabalin/therapeutic use , Molecular Docking Simulation , Seizures/drug therapy , Seizures/metabolism , Epilepsy/drug therapyABSTRACT
Heavy metals and persistent organic pollutants are causing detrimental effects on the environment. The seepage of heavy metals through untreated industrial waste destroys the crops and lands. Moreover, incineration and combustion of several products are responsible for primary and secondary emissions of pollutants. This review has gathered the remediation strategies, current bioremediation technologies, and their primary use in both in situ and ex situ methods, followed by a detailed explanation for bioremediation over other techniques. However, an amalgam of bioremediation techniques and nanotechnology could be a breakthrough in cleaning the environment by degrading heavy metals and persistant organic pollutants.
