Evaluation of Antioxidant, Anti-urease, Lipoxygenase, and Butyrylcholinesterase Inhibition Activities of Isatin Thiazole Derivatives Using Nano Formulations

This study investigates the enzyme inhibition and antioxidant activities of various nanoparticles loaded with three isatin thiazole derivatives. For drug encapsulation, two different nanoparticle systems were examined: polysaccharide-based nanoparticles, including alginate-chitosan nanoparticles (ACN) and gum-chitosan nanoparticles (GCN), and polymer-lipid hybrid nanoparticles based on the lipid soya lecithin in combination with either sodium alginate (PLHN-A) or gum acacia (PLHN-G). The biological activities of the drug-loaded nanoparticles were evaluated against key targets, including antioxidant activity, urease, lipoxygenase, and butyrylcholinesterase. The results were expressed as mean ± SEM, using eserine, butylated hydroxyanisole (BHA), and thiourea as reference standards. Among the tested systems, PLHN-A loaded with derivative-3 (D3) exhibited the highest antioxidant activity (30.2 ± 0.45). Alginate-chitosan nanoparticles loaded with derivative-3 (ACN-D3) demonstrated notable anti-urease activity (21.2 ± 0.12), while derivative-1(D1) encapsulated in the same nanoparticle system (ACN-D1) exhibited significant lipoxygenase inhibition (13.4 ± 0.48). Gum-chitosan nanoparticles loaded with derivative-1 (GCN-D1) demonstrated strong butyrylcholinesterase inhibition (IC50 = 21.6 ± 0.17 µM). Overall, ACN and PLHN-A with all three derivatives (D1, D2 and D3) emerged as promising candidates due to their excellent antioxidant and enzyme inhibition properties, underscoring the effect of nanoparticle composition on their biological activity and therapeutic potential.

Khadim Mohi Uddin, Najia Mansoor, Syed Imran Ali, Mohsin Ali, Mansoor Ahmed, Mehwish Solangi, Shazia Haider, and Khalid Mohammed Khan