Preparation, characterization and therapeutic properties of gum arabic-stabilized gallic acid nanoparticles

Abstract

Gallic acid (GA) is a natural phenolic compound with therapeutic effects that are often challenged by its rapid metabolism and clearance. Therefore, GA was encapsulated using gum arabic into nanoparticles to increase its bioavailability. The formulated nanoparticles (GANPs) were characterized for physicochemical properties and size and were then evaluated for antioxidant and antihypertensive effects using various established in vitro assays, including 1,1-diphenyl-2-picrylhydrazyl (DPPH), nitric oxide scavenging (NO), β-carotene bleaching and angiotensin-converting enzyme (ACE) inhibitory assays. The GANPs were further evaluated for the in vitro cytotoxicity, cell uptake and cell migration in four types of human cancer cell lines including (MCF-7, MDA-MB231) breast adenocarcinoma, HepG2 hepatocellular cancer, HT-29 colorectal adenocarcinoma, and MCF-10A breast epithelial cell lines. The GANPs demonstrated potent antioxidant effects and have shown promising anti-cancer properties in a dose-dependent manner with a predilection toward HepG2 and MCF7 cancer cells. The uptake of GANPs was successful in the majority of cancer cells with a propensity to accumulate in the nuclear region of the cells. The HepG2 and MCF7 cancer cells also had a significantly higher percentage of apoptosis and were more sensitive to gallic acid nanoparticle treatment in the cell migration assay. This study is the first to confirm the synergistic effects of gum arabic in the encapsulation of gallic acid by increasing the selectivity towards cancer cells and enhancing the antioxidant properties. The formulated nanoparticles also had remarkably low toxicity in normal cells. Based on these findings, GANPs may have promising therapeutic applications towards the development of more effective treatments with a probable targeting precision in cancer cells.

Pt-Coated Au Nanoparticle Toxicity Is Preferentially Triggered Via Mitochondrial Nitric Oxide/Reactive Oxygen Species in Human Liver Cancer (HepG2) Cells

“…A standard of sodium nitrite (1–100 μM) prepared in culture media was similarly run for calculation purposes as conducted by various investigators. 66 , 67 Data has been presented as % of NO concentration in untreated control cells.…”

Polyhydroxybenzoic acid derivatives as potential new antimalarial agents

“…[18] In contrast, an acidic molecule is not often recognized as a promising structure to cross the intestinal barrier, even if some transporters exist on enterocytes, for example, the monocarboxylic acid transporter. [17] S C H E M E | 5 of 13 This trend prompted us to prepare esters of the selected benzoic scaffolds 11-15 and to explore the impact of the alkyl chain on the in vitro activity against 3D7 (17)(18)(19)(20)(21)(22)(23). Surprisingly, we observed a similar range of activity for all the structures related to 11 (IC 50 ~28 µM, Table 2).…”

“…[15][16][17] This phenolic compound also showed some pharmacological activities, including antitrypanosome, antibacterial, and antiplasmodial, without high toxicity in various cell lines, or during in vivo studies (ED 50 > 80 mg/kg in mice) (Table 1). [18][19][20][21][22][23][24][25][26][27][28] On the contrary, some derivatives from this scaffold have already been studied for anti-Plasmodium purposes and have shown interesting inhibitory effects (IC 50 ~10 µM). [20,29] We decided to work on these polyphenols, despite their known PAINS (pan-assay interference compounds) potential, for various reasons.…”

Colon Available Bioactive Compounds Exhibits Anticancer Effect onIn-VitroModel of Colorectal Cancer

“…In the spectrum of gallic acid (Figure 9D) there is a broad band at 3194.61 cm −1 related to OH stretching and hydrogen bonds between phenolic hydroxyl groups. The COOH stretch/bend is observed at 1255.93 cm −1 Aromatic ring stretching is observed at 1454.44 cm −1 [58]. C-O stretching is at 1021.45 cm −1 In the spectrum of quercetin (Figure 9E) there is a broad band at 3194.61 cm −1 related to OH stretching and hydrogen bonds between phenolic hydroxyl groups.…”