Showing posts with label Ebselen. Show all posts
Showing posts with label Ebselen. Show all posts

Wednesday, 19 February 2025

Antioxidant Activity of Selenium Containing Analogues: A Review of Glutathione Peroxidase and Antioxidant Mechanism | Chapter 3 | Chemistry and Biochemistry: Research Progress Vol. 3

This chapter provides information published in recent years on the chemical forms, particularly on the antioxidant and prooxidant activities of organoselenium compounds. In the present study, a series of functional mimics of synthetic antioxidant organoselenium compounds such as ebselen, Allyl               selenides, selenenate esters, Diferrocenyldiselenides, spirodioxyselenurane, spirodiazaselenuranes and its glutathione peroxidase (GPx) catalytic activity are discussed. The first synthetic compound ebselen and its related compounds show significant antioxidant activity. Therefore, initial successes of ebselen exhibited beneficial effects in clinical trials. Further, diferrocenyldiselenides containing tert-amino substituents exhibited excellent GPx activity in the presence of PhSH and imported remarkably higher activity than that of ebselen. In addition, spirodioxyselenurane and spirodiazaselenuranes are structurally interesting compounds and the stability of these compounds highly depends on the nature of the substituents attached to the nitrogen atom. The high concentration of peroxides addition the selenium centre in the spirocyclic compounds undergoes further oxidation to produce the corresponding selenurane oxides, which are stable at room temperature. The overall use of synthetic reagents is becoming increasingly popular for pre-clinical studies and bio-medicinal applications. 

 

Author (s) Details

Devappa S. Lamani
Department of Chemistry, Basaveshawar Science College, Bagalkot, Rani Channamma University, Karnataka, India.

 

Shekappa D. Lamani
Department of Chemistry, BLADE’S SB Arts and KCP Science College, Vijayapur, Karnataka, India.

 

Please see the book here:- https://doi.org/10.9734/bpi/cbrp/v3/4291

Wednesday, 2 June 2021

Effect of Orally Ebselen (SPI-1005) towards Glutathione and Malondialdehyde Blood Level and Otoacoustic Emissions Result in Soldiers with Acoustic Trauma Risk | Chapter 5 | Technological Innovation in Pharmaceutical Research Vol. 5

 Excessive noise exposure can cause acoustic trauma to the inner ear structure (cochlea) by creating mechanical and metabolic (oxidative) stress (TA). Oxidative stress, which is induced by an increase in free radical ROS/RNS in the organs of Corti, causes apoptosis and necrosis of cochlear hair cells. Increased malondialdehyde (MDA), decreased glutathione peroxidase (GPx) enzyme, and aberrant otoacoustic emission value were all signs of oxidative stress (refer). Endogenous antioxidant enyzme (superoxide dismutase/SOD, catalase/CAT, and GPx) mediated the defence mechanism against oxidative stress. The glutation peroxidase mimic's cellular mechanism was identical to that of GPx. The goal of this study was to see how a glutathione peroxidase mimic affected glutathione peroxidase and malondialdehyde levels in blood, as well as otoacoustic emission values in troops who were at danger of TA from a Howitzer 105 artillery weapon explosion. The study's design was a randomised, double-blind, placebo-controlled clinical trial on 34 new recruit troops in the Indonesian Army's Artillery Academy, during which the soldiers were trained to fire the Howitzer 105 artillery weapon, from July 7th to July 10th, 2014 in Cimahi and Batujajar. The participants were split into two groups: the exposure group (the ones who got the treatment) and the control group During the training, the exposure group received 200mg of glutathione peroxidase mimetic (Ebselen SPI 1005) orally once daily, while the control group received nothing. Before and after firing training, the levels of malondialdehyde and glutathione peroxidase in the blood, pure tone audiometry, and otoacoustic emission value (DPOAEs) were assessed in those two groups. The data was evaluated using parametric and nonparametric methods, as well as NNT (95 percent confidence interval) and significance value (p0.05). According to the findings of this study, the number of auditory trauma events in the control group was 23.5 percent, whereas the exposure group had 0 percent. The exposure group was 0%, and the DPOAEs test revealed that the control group was 47.1 percent abnormal/refer, while the exposure group was 100 percent normally/pass, with a statistically significant difference (p0.051). The group given Ebselen SPI 1005 had an increase of 82.4 percent erythrocyte GPx (NNT, 95 percent CI=1.889 [1.1593.016]; p=0.004), an increase of 88.2 percent plasma GPx (NNT, 95 percent CI=1.417 [0.970-1.775]; p0.001), a decrease of 100 percent erythrocyte MDA (NNT, 95 percent CI=2.125 [1.335-3.987]; p=0.01), a decrease in plasma MDA of 94.1 percent (NNT, 95 percent CI=2.125 [1.29-3.904]; p=0.01), and a 100 percent normal/pass DPOAEs value (NNT, 95 percent CI = 2.125 [1.335-3.987]; p=0.01). Giving Ebselen SPI 1005 to soldiers at risk of acoustic harm while firing a Howitzer 105 artillery weapon raised GPx levels in the blood, decreased MDA levels in the blood, and resulted in regular DPOAEs readings (pass).

Author (s) Details

S. Sasongko
ENT Department, Gatot Soebroto Army Central Hospital, Indonesia.

T. Boesoirie
ENT Department, Medical Faculty, Padjadjaran University, Indonesia.

I. Parwati
Clinical Pathologic Department, Medical Faculty, Padjadjaran University, Indonesia.

H. Sastramihardja
Clinical Pharmacological Department, Medical Faculty, Padjadjaran University, Indonesia.

J. Bashirudin
ENT Department, Medical Faculty, Indonesia University, Indonesia.

View Book : https://stm.bookpi.org/TIPR-V5/article/view/1241