Pentaclethra eetveldeana Leaves from Four Congo-Brazzaville Regions: Antioxidant Capacity, Anti-Inflammatory Activity and Proportional Accumulation of Phytochemicals.

Oxidative stress and inflammation play a key role in the occurrence of neurodegenerative diseases. Traditionally, Pentaclethra eetveldeana leaves are used in dementia treatment. Therefore, this study aimed to evaluate the antioxidant and anti-inflammatory activities as well as the phytochemical composition of Pentaclethra eetveldeana leaves from four Congo-Brazzaville regions. The 1.2-diphenyl-1-picrylhydrazyl radical-scavenging, ß-carotene bleaching and molybdenum reduction assays were used to assess the antioxidant activity. The protein denaturation and erythrocyte membrane stabilization tests were used to analyze the anti-inflammatory activity. Phytochemical screening, the quantification of polyphenols by spectrophotometry, as well as the determination of extraction yields were carried out. It was found that the extracts reduced molybdenum; furthermore, compared to ascorbic acid, they showed better antiradical activity and inhibited lipid peroxidation. Moreover, globally, the membrane-stabilizing power of the aqueous extracts was superior or comparable to diclofenac, while the same extracts were less effective for the inhibition of denaturation. All of the aqueous extracts contained polyphenols, saponins, alkaloids, anthraquinones, reducing sugar and cardiotonic glycosides. The total polyphenols, tannins and proanthocyanidins are produced proportionally from one region to another. Finally, the leaves from Brazzaville and Boundji contain flavonols, while those from Makoua and Owando contain flavones. Thus, Pentaclethra eetveldeana leaves contribute to traditional dementia treatment through their antioxidant and anti-inflammatory properties.

Synthesis and GABA uptake inhibitory properties of 6-aryl iminoxymethyl substituted nipecotic acids.

Nipecotic acid derivatives bearing an aryl iminoxymethyl side chain at the position 6 were synthesised and tested for their GABA uptake inhibitory properties. Contrarily to the N-substituted derivatives 2, 3 the introduction of the oxime function in the side chain of analogues of the active nipecotic derivative 4 does neither increase, nor maintain the activity.

Syntheses and GABA uptake properties of 6-ether- and 6-enol ether-substituted nipecotic acids.

6-aralkylether- and 6-arylenol-ether-substituted nipecotic acids were synthesized. These analogues are poor GABA uptake inhibitors. The electronegative region concept developed in the N-substituted nipecotic acid series cannot be transferred on the side chain of this series of 6-substituted analogues.