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Sorafenib, a multikinase inhibitor is used to treat hepatocellular and renal carcinoma. However, a low solubility impedes its bioavailability and thus, effectiveness. This study aims to enhance its effectiveness by using novel camel milk casein nanoparticles as a delivery system. This study evaluates the cytotoxicity of sorafenib encapsulated in camel milk casein nanoparticles against human hepatocarcinoma cells (HepG2 cells) in vitro. Optimal drug loaded nanoparticles were stable for 1 month, had encapsulation efficiency of 96%, exhibited a particle size of 230 nm, zeta potential of -14.4 and poly disparity index of 0.261. Treatment with it led to cell morphology and DNA fragmentation as a characteristic of apoptosis. Flow cytometry showed G1 phase arrest of cell cycle and 26% increased apoptotic cells population upon treatment as compared to control. Sorafenib-loaded casein nanoparticles showed 6-fold increased ROS production in HepG2 cells as compared to 4-fold increase shown by the free drug. Gene and protein expression studies done by qPCR and western blotting depicted upregulation of tumor suppressor gene p53, pro-apoptotic Bax, and caspase-3 along with downregulated anti-apoptotic Bcl-2 gene and protein expression which further emphasized death by apoptosis. It is concluded regarding the feasibility of these casein nanoparticles as a delivery system with enhanced therapeutic outcomes against hepatocellular carcinoma cells., (© 2024 Wiley-VCH GmbH.)

The present work is a preliminary report of synthesis of a series of targeted 4,6‐O‐ethylidene‐β‐D‐glucopyranosylamine glycoconjugate quinoline 4‐carboxylic acid derivatives followed by a quick evaluation of their anti‐inflammatory and anticancer activities. Compounds C5 and C8 exhibited highest anti‐inflammatory activity against human COX‐2 enzyme. Anticancer studies were also performed in vitro which revealed C8 as a promising candidate against HeLa, human cervical cancer cell lines. The anti‐inflammatory and anticancer activity was further confirmed by molecular docking studies for all the synthesized molecules. That all the compounds showed potency, seems to validate our initial hypothesis concerning a positive correlation between anticancer and anti‐inflammatory activity for the designed quinoline glycoconjugates. [ABSTRACT FROM AUTHOR]